An ink cartridge includes a hollow ink tank body, a cover member connected to the hollow ink tank body, a hollow tube and a pressure regulator arranged inside the hollow ink tank body. The cover member has an air vent penetrating therethrough, and a first through-hole protrusion adjacent to the air vent and extending forwards the hollow ink tank body. The pressure regulator includes a holder, a resilient member arranged inside the holder, an elastic plate connected to the resilient member and abutting against the holder, a secure member disposed over the elastic plate, and a thin film covered the secure member. The pressure regulator further has a through-hole projection extending outwardly therefrom for connecting the hollow tube that connects to the first through-hole protrusion of the cover, so that the atmospheric air passes through the pressure regulator via the hollow tube after a sealing film is removed.

1. Field of the Invention
The present invention relates to an ink cartridge adapted for an ink jet printer, and particularly relates to an ink cartridge that can improve the ink leakage problem at both the inlet and outlet of ink cartridge.
2. Background of the Invention
The ink jet recording technology is such as to record characters and images directly on a recording medium (such as paper, cloth, or plastic sheet) by discharging ink from fine nozzles thereto. Conventionally, the recording apparatus has been utilized as a printer serving and provided as the output terminal of a copying machine, a facsimile equipment, a printer, a word processor, a work station or the like; or as a handy or portable printer used for such an information processing system as a personal computer, a host computer, an optical disc device or a video apparatus. In a conventional recording apparatus, ink is supplied to a recording head from an ink tank constructed as a cartridge.
Although increasing the negative pressure prevents ink from seeping out of the recording head, the negative pressure has an upper limit. If the negative pressure is too high, ink cannot overcome the negative pressure and jet from the recording head. On the other hand, the ink cartridge must be able to adjust the negative pressure in the ink tank automatically by keeping the negative pressure during a suitable range. U.S. Pat. No. 6,783,219 B2, entitled "Ink Cartridge", one of the relative documents, provides an elastic member for unidirectional ventilation by a pressure difference between inside and outside the hollow ink tank body without both air inlet hole and porous member. A pressure regulator referred in the prior art is used to maintain the pressure and the ink flows to the printhead continuously. Nevertheless, ink leakage problems of the pressure regulator may occur during storage, delivery and printing operation. Alternatives of regulator pressure have been explored but have failed to adequately address the leakage issue.
It is desirable to develop a new and improved ink cartridge to substantially resolve the leakage problems and provide better, more advantageous overall results.


The present invention relates to a dispensing device for dispensing a liquid or viscous substance, preferably foodstuff. At least one pump means (4) is provided to perform pump motions for sucking said substance (2) into the dispensing device (1) and dispense or discharge it therefrom. The pump means (4) is provided to divide inner parts of the dispensing device (1) into at least one suction chamber (30) and at least one dispensing or discharge chamber (31) which are interconnected through at least one transfer chamber (32). The pump means (4) is during a first pump motion in one direction (A) provided to suck substance (2) into the suction chamber (30) and simultaneously dispense or discharge substance (2) from the discharge chamber (31). The pump means (4) is during a second pump motion in the opposite direction (D) relative to the first pump motion provided to feed substance (2) from the suction chamber (30) and through the transfer chamber (32) into the discharge chamber (31).

Dispensing devices for dispensing or discharging viscous foodstuff are known from U.S. Pat. No. 5,452,826. Such dispensing devices comprise a pump means which during a pump stroke sucks foodstuff out of an inner container and which during a reversed pump stroke discharges foodstuff.
Such a dispensing device has a limited pump speed, because after every discharge or outfeed one has to wait until the pump means has refilled the pump chamber.


This invention relates to a process for preparing an alkylsulfonic anhydride comprising contacting. (A) a dehydrated phosphoric acid with PA1 (B) an alkylsulfonic acid having 1 to 6 carbon atoms, under conditions of temperature and pressure to result in the substituted absence of phosphoric/alkylsulfonic mixed anhydride and production of a mixture of alkylsulfonic acid and its corresponding anhydride at a conversion of at least 10% of alkylsulfonic acid to the corresponding alkylsulfonic anhydride.

Methanesulfonic anhydride finds many applications in the synthesis of certain methyl sulphonates. In the prior art process of L. N. Owen & Whitelaw, S. P., described in J. Chem. Soc., p 3723 (1953), methanesulfonic anhydride was prepared by refluxing methanesulfonic acid with thionyl chloride for 3 hours, resulting in a crude product.
In another prior art process, methanesulfonic acid was mixed with phosphorus oxide at certain conditions by R. C. Paul, S. K. Sharma, R. D. Sharma and K. C. Malhotra as described in Chemistry and Industry, page 702, June 17, 1991.

Process for preparing alkylsulfonic anhydrides


A twin recliner operable manually for permitting selective position of a seat back with respect to the seat cushion through a range of reclined positions to a selected use position. Said twin recliner comprising: a master and a slave recliner, a shaft arm member with a longitudinal cleavage on one side and a plurality of peripheral stepping arrangement on the other side, an external spring means with one end hooked to the lower portion of the activating lever and the other end locked to the longitudinal cleavage of the shaft to facilitate a nominal return rate of the actuating lever, a rotatable cam mounted on the third of said plurality of stepping arrangement having a projection is engaged with the slot of the lower housing to receive a rotary drive directly from the actuating lever to disengage inner sectors, a guiding plate with a central passage mounted on the fourth of the stepping arrangement of the shaft member to provide a synchronized movement of the inner sectors.

All vehicles are now equipped with seats having a recliner mechanism that can be selectively actuated for permitting the angular position of the seat back to be varied with respect to the seat cushion.
Generally, seat reclining mechanism includes a lower and upper arm mounted on the seat cushion and seat back respectively, to house a locking cum unlocking means, which is effected by a rotatable cam operated by a splined shaft which passes through the lower and upper arms of the recliner. Spiral springs that are mounted on the shaft, are disposed between the two arms of the recliner to apply radial forces on the cam for rotation during locking and unlocking operations.
U.S. Pat. No. 6,626,495 discloses a seat recliner mechanism having a manual control member on a shaft hinge for actuating a cam which in turn helps in disengagement of the first toothed pawls or inner sector member, with the second toothed seat back arm member to allow pivotal movement of the seat back arm which is connected to the seat back to a reclined position.
In the aforementioned seat reclining device, the actuating mechanism includes a hinge shaft directly connected to the cam. The cam is also hooked with the spiral spring. As a result there are two forces acting on the actuating member i.e., the cam. Sometimes, this may result in uneven forces acting on the cam and hence operational difficulties arise as well as increasing the operating effort. The guide walls that guide the pawls or the inner sectors may wear out due to irregular shape and manufacturing process.
The recliner also becomes safety critical mechanism because in the event of a collision the recliner should be able to withstand the impact forces that act on the seat and thus on the recliner, without any major deformations or breakage. The necessity of twin recliner becomes significant when the seat size is increased such that a single recliner fails to endure the subjected loads. Thereby the concept wherein the two recliners share both static and fatigue loads forms an important background of this invention.
U.S. Pat. No. 6,474,740,issued Nov. 5, 2002 and U.S. Pat. No. 6,609,756,issued Aug. 26, 2003,also specifies a reclining device similar to the above mentioned claiming to have reduced rotational friction and noise respectively.
The constraints that limit the functioning of the twin recliner assembly include failure of recliners to operate simultaneously due to loss in transmission, very high operating forces, teeth breakage because of shock forces, slippage due to undershooting and overshooting, endurance failure, so on and so forth.
In the present trend it is desirable to provide a recliner with the simplest mechanism with high strength, less friction between the components and thus free movement of the components for operational ease.
Thus the objective of this invention has been to enhance the operating characteristics of a twin recliner assembly by fulfilling the load carrying and fatigue life requirements and also by reducing the loss in the actuating mechanism between the master and the slave recliners. Further the objective has been to reduce the operating effort and provide a recliner assembly which is designed so as to eliminate the problems in the individual assembly also. It is therefore desirable to have an improved recliner which is easy to both manufacture and operate and is failsafe.


An electrical power supply for powering electrical pump instrumentation and process control equipment associated with a pump having a rotating member. The power supply includes an electrical current generator driven by the rotating member of the pump, and a voltage regulator for regulating the output of the generator.

The prior art utilizes essentially three basic techniques for supplying electrical power to equipment, such as pressure transmitters, temperature transmitters, vibration sensors, and the like, located near or attached to a pump. The first technique involves hard wiring directly to each piece of electrical equipment. The second technique involves providing the electrical equipment with internal batteries or external batteries. The third technique involves providing the electrical equipment with a combination of a rechargeable battery and solar panel. The solar panel powers the equipment during daylight hours and charges the battery for use during night hours.
Hard wiring electrical power directly to the electrical equipment has the highest installation cost of the three methods mentioned above. In most facilities conduit and wiring must be purchased and installed from the power panel to where the pump is located. Battery powered electrical equipment has a lower installation cost but a higher maintenance cost in terms of checking battery condition and performing battery replacement. Battery powered electrical equipment with rechargeable batteries charged via solar panels reduces the need to check battery condition and battery replacement, but requires adequate light hours to recharge the batteries.
Accordingly, a technique for supplying electrical power to equipment located near or attached to a pump is needed that avoids the disadvantages of the prior art.

Self contained pump electrical equipment power supply


An output compensating device capable of optimally compensating output signals of an image sensor composed of a number of light-sensor circuits, each of which represents a unit pixel and is capable of producing in a photoelectric converting element a sensor current proportional to a quantity of light falling thereon, converting the current into a voltage signal by a MOS type transistor with a logarithmic output characteristic in a weak inverse state, initializing itself by removing a charge accumulated in a parasitic capacitor of the photoelectric converting element by changing a drain voltage of the transistor to a value lower than a normal value for a specified time and outputting a pixel signal having a logarithmic characteristic at a large quantity of the sensor current and a pixel signal having a non-logarithmic characteristic at a small quantity of the sensor current. This device has a means for compensating each pixel signal from the image sensor for an offset value and outputting a resulting signal if said signal has an output characteristic within a logarithmic response region or a non-logarithmic region depending on the output condition and, if not, further compensating the offset-compensated signal for its gain and outputting a resulting signal, thus ensuring the optimal compensation of each pixel signal of the image sensor in accordance with its output state.

The present invention relates to an output compensating device for an image sensor and, more specifically, to an output compensating device for compensating for variations in pixel outputs of a MOS type image sensor.
Japanese Laid-Open Patent Publication No. 2000-329616 discloses a conventional MOS transistor type image sensor, in which a light sensor circuit used as a unit pixel comprises, as shown in FIG. 1, a photo-diode PD operating as a photoelectric converting element for producing a sensor current proportional to the quantity of incident light Ls falling thereon, a transistor Q1 having a logarithmic output characteristic in a weak inverse state for converting the sensor current produced in the photodiode into a voltage signal Vpd, a transistor Q2 for amplifying the voltage signal Vpd and a transistor Q3 for outputting a sensor signal in accordance with a timing pulse of a readout signal Vs and which circuit is characterized by its a wide dynamic range obtained by giving the output a logarithmic characteristic, thereby achieving the high sensitivity of detecting a light signal. In addition, the light sensor circuit is provided with a means for changing a drain voltage VD of the transistor Q1 to a value lower than a normal value for a specified period to remove a charge accumulated in a parasitic capacitor C of the photodiode PD to initialize the circuit. The light sensor circuit can thus obtain a voltage signal Vpd corresponding to the quantity of incident light Ls even if the sensor current absurdly changed, thereby eliminating the possibility of occurrence of afterglow of each pixel even at a small quantity of incident light.
As shown in FIG. 3, the above-described light sensor circuit may output a signal with a logarithmic characteristic at a normal quantity of sensor current corresponding to a normal quantity of incident light to a photodiode but it may not maintain the logarithmic output characteristic and may have a substantially linear output characteristic at a decreased sensor current due to a delay of charging the parasite capacitor of the photodiode. In FIG. 3, WA represents a region of responding with a non-logarithmic characteristic output and WB represents a region of responding with a logarithmic characteristic output.
However, the conventional image sensor using the light sensor circuits, in which a sensor current proportional to incident light is produced in a photo-electric converting element and converted into a voltage signal by using a MOS type transistor having logarithmic output characteristic in a weak inverse state, still involves such a problem that it cannot be free from the occurrence of unwanted afterglow of each pixel with a decreased quantity of incident illumination falling on the photoelectric converting element.
The MOS type image sensor may suffer variations in output characteristics of pixel signals, which may be resulted from structure-derived variations in output characteristics and variations in temperature characteristics of respective light sensor circuits.
Japanese Laid-Open Patent Publication No. 2000-175108 discloses a conventional image sensor using the light sensor circuits as respective pixels, in which a sensor current proportional to incident light is produced in a photo-electric converting element and converted into a voltage signal by using a MOS type transistor having logarithmic output characteristic in a weak inverse state, wherein variations in its output with a change in temperature (as shown in FIG. 37) are compensated for according to the image sensor temperature detected by a temperature sensor.
FIG. 41 shows a construction of a conventional image sensor, in which a sensor signal AlSig from the image sensor 7 is compensated for temperature variations by doing digital operations according to a temperature signal Atemp detected by a temperature sensor 12.
In the image sensor of FIG. 41, each of sensor signals AlSig output from the image sensor 7 is converted by an A-D converter IADC into a digital signal DlSig that is then transferred to a digital temperature compensation circuit DCAL. A temperature signal Atemp from a temperature sensor 12 provided in the image sensor 7 is also converted by an A-D converter TADC into a digital signal Dtemp that is then transferred to a lookup table LUT of characteristic offset compensation values preset versus variable temperatures. An offset compensation value DtempOFS corresponding to the currently detected temperature of the image sensor 7 is selected from the lookup table LUT and given to the digital temperature compensation circuit DCAL by which the digital sensor signal DlSig is corrected by adding to or subtracting from the signal the given offset compensation value DtempOFS. The compensated digital sensor signal can thus be obtained. When compensating sensor signals from the image sensor are processed by the digital compensation circuit, each of pixel sensor signals and a temperature detection signal from the temperature sensor are necessarily converted by A-D converters into digital signals. However, if sensor signals might vary in a wide range as the temperature changes, the A-D converter for converting the sensor signals must be set to a wide input range. This limits the use of the A-D converter. Furthermore, the temperature compensation of sensor signals by calculations may require the provision of a complicated compensating configuration.

Output-compensating device for image sensor


A combination including a harvester, a generator vehicle, and a transport vehicle including a chassis, a motor, a plurality of traction devices, and a control unit aligning the transport vehicle in relation to at least one of the harvester and a previous path of the harvester. A method of positioning a train of transport vehicles in relation to a path of the harvester.

On occasion, a tractor may not have enough weight to provide sufficient traction to tow trailers containing heavy, harvested crops. For example, the trailers may weigh twice as much as the tractor making it difficult for the weight of the tractor to provide sufficient traction, resulting in slippage of the tractor's wheels. Further, under adverse weather conditions, the tractor may experience even greater slippage because of wet soil or mud. To take advantage of the trailer's weight, a tractor can be mechanically coupled to a drive axle of a trailer. As a result, the tractor's power drives the trailer and the weight of the trailer and the harvested crop enhance the traction at the driven wheels of the trailer.


High-performance overprint varnishes, well-suited for the protective coating of a wide variety of substrates, e.g., papers, cardboards and packaging materials, include a composite latex and characteristically a polyethylene wax emulsion, the composite latex comprising the copolymerizate of at least one hydrophobic monomer within an aqueous solution of a styrene/maleic anhydride resin, the styrene/maleic anhydride resin having a molecular weight ranging from 500 to 5,000 and an acid number of at most 500, and the amount by weight of the styrene/maleic anhydride resin in the copolymerizate ranging from 5% to 50%.

1. Technical Field of the Invention
The present invention relates to novel overprint varnishes, and, more especially, to high-performance overprint varnishes comprising composite latices prepared by polymerizing at least one hydrophobic monomer within a matrix solution/dispersion of a particular styrene/maleic anhydride(SMA) resin.
By "overprint varnishes" are intended surface-improvement protective compositions designed to impart to treated surfaces, for example printed or unprinted papers and cardboards, enhanced resistance to external agents and influences, and, in particular, enhanced resistance to friction, moisture, and temperature, and even an improved appearance, for example improved glossiness.
2. Description of the Prior Art
Conventional overprint varnishes comprise aqueous compositions based on composite latices of the styrene/acrylate polymer-styrene/maleic anhydride resin type.
Thus, EP-A-675,177 (Goodrich) describes shell/core latices prepared via the polymerization of mixtures of hydrophobic monomers, such as butyl methacrylate, 2-ethylhexyl acrylate, and styrene in an aqueous styrene/maleic anhydride resin solution, this resin being rendered soluble by salification with a volatile nitrogenous base such as ammonia.

High-performance overprint varnishes comprising composite SMA latices


A printing apparatus discriminates whether received print data is print data converted into a job packet constructed by a header portion and a data portion or print data which is not converted into a job packet and switches the processing operation in accordance with the print data.

1. Field of the Invention
The invention relates to a printing apparatus for processing print data which is transmitted from a host computer to generate the print data in accordance with an instruction of the user, generating image data, and actually printing into a media such as a paper or the like. The invention also relates to a print control method of such a printing apparatus and a recording medium in which a print control program for such a print control method has been stored.
2. Related Background Art
A printing system which satisfies functions such that not only a printing apparatus prints print data that is generated from a host computer but also an information obtaining and an environmental setting of the printing apparatus are performed from the host computer has been known.
FIG. 1 is a diagram for explaining a first print data processing method embodying a method of performing an information obtaining and an environmental setting of a printing apparatus from a host computer.
In FIG. 1, reference numeral 100 denotes a host computer; 150 a printing apparatus; and 180 a predetermined communication medium for connecting the host computer 100 and printing apparatus 150.
Further, the host computer 100 is constructed by: an application section 101 for providing a graphic user interface to the user and generating image data adapted to a purpose of the user; a printer driver 102 for converting the image data generated by the application section 101 into page description language (hereinafter, abbreviated to PDL) data which can be printed by the printing apparatus 150; a transmission buffer 103 for temporarily storing the PDL data formed by the printer driver 102; an I/F driver 104 for transmitting the PDL data stored in the transmission buffer to the printing apparatus 150 and transmitting and receiving information to/from the printing apparatus 150; and a utility section 105 for obtaining the information of the printing apparatus 150 and providing it to the graphic user interface and for changing the environmental setting of the printing apparatus 150 in accordance with a demand of the user.
The printing apparatus 150 is constructed by: an I/F driver 151 for receiving the PDL data and environmental setting transmitted from the host computer 100 and transmitting the information of the printing apparatus 150; a reception buffer 152 for temporarily holding all of the data received by the I/F driver 151 and serving as a buffer device of a delay of processes at the post stage; a JL parser 153 for analyzing the reception data and discriminating by a predetermined job control language (hereinafter, abbreviated to JL) whether the host computer has requested to obtain the information of the printing apparatus or the host computer has transmitted the PDL data, thereby distributing processes; a PDL translator 154 for performing a translating process of the PDL data distributed by the JL parser 153 and converting into a drawing object suitable to draw; a database 158 for storing the information of the printing apparatus set by the JL and providing the information to the JL parser and PDL translator 154; a drawing buffer 155 for temporarily storing the drawing object formed by the PDL translator 154 until it is actually printed; a drawing section 156 for generating a bit map image by actually drawing the drawing object temporarily stored in the drawing buffer 155; and a printer engine 157 for receiving a bit map image generated by the drawing section 156 and printing into a media such as a paper or the like by a well-known printing technique.
The first print data processing method has the following two problems. First, there is a problem such that since a channel to transmit and receive the print data (PDL data) and a channel to obtain the information of the printing apparatus are the same, the transmission and reception of the print data and the information obtaining cannot be simultaneously performed. Second, there is a problem such that since the print data is recognized by the JL parser 153, the print data temporarily stored in the reception buffer 152 is not recognized and management information regarding this print data cannot be returned to the host computer 100.

Printing apparatus, print control method, and recording medium storing print control program therein


A drive unit, for example for a windshield wiper, is of the type-including a casing containing a motor, a drive shaft extending through bearings and seal, the bearings and seal being mounted in a sleeve portion of the casing, and a speed reducing mechanism coupling the motor with the drive shaft. The anterior part of the sleeve portion includes a thickened portion having a bore of reduced radius, in which is formed the seat for the seal.

It is well known that windshield wiper blades are driven in contact with the windshield of a motor vehicle, over a given sector of the latter and with a predetermined pressure, by means of a windshield wiper arm which is coupled to a drive unit having a motor that drives a speed reducing means, and which transforms the initial rotary movement of the motor directly or indirectly into alternating or oscillating motion of the drive shaft and wiper arm.
The drive unit conventionally has an electric motor, the rotor of which extends along the interior of a closed casing, the speed reducing means generally comprising a gearing system, with one of the gears being coupled, either directly or through a crank and connecting rod system, to the drive shaft which projects outside the casing of the drive unit, and which serves to actuate the windshield wiper arm.
As is again already known, the gear system carries, inter alia, on one of its toothed wheels, electrical contacts which enable the windshield wiper arm or arms to be selectively driven at variable speeds, and to be stopped, in such a way that the wipers will always be parked in a fixed lower position so as not to interfere with the visibility of the driver of the vehicle.
The drive shaft projects from the surface of the vehicle bodywork, and the presence of the above mentioned electrical contacts necessitates that the drive shaft must be mounted so that it is sealed from the ingress of water or impurities, so as to ensure that no short circuiting will occur within the drive unit. Such an arrangement is described in the specification of French published patent application No. FR 2 165 540A, in which the motor shaft is surrounded by a sleeve, the anterior portion of which (i.e. the portion remote from the speed reducing means) has an opening into which an O-ring seal can be introduced, together with a bearing comprising a ring of a material having a low coefficient of friction. The O-ring seal bears, at the side of the motor/speed reducing means, on a shoulder, and is retained opposite to the shoulder in an axial position by means of a member which is fitted at the front of the sleeve. This member is itself retained in the sleeve by means of a circlip or by any other similar retaining means.
Although such a mounting works very well in practice, it is relatively costly, in particular to the extent that it requires a substantial amount of machining, and also the fitting of an additional member which has to be retained in position by fastening or retaining means, which also have to be fitted and which increase manufacturing costs.

Mounting for a drive shaft, in particular for a windshield wiper drive unit


A CD-vinyl record player comprising a CD door, small turntable, bearing element, record player axle, mini-bearing, big turntable, record player main base, CD motor frame, turntable frame, CD main base, bearing, bearing cover, and CD motor. The CD door is connected to the small turntable through a mini-bearing, and the record player axle is installed in the center of the CD door. The bearing element is above the CD door and connected to the record player axle. The big turntable is above the record player main base. The bottom of the record player main base connects to the turntable frame. The CD motor frame is above CD main base. The bearing is at the center of record player main base, and has the bearing cover on top. The CD motor is at center of the bottom of the turntable frame. The invention combines a vinyl record player and CD player into one player.

1. Field of the Invention
The present invention relates to the technical field of record players. Specifically, the present invention relates to the technology of a CD-vinyl record player.
2. Background
With improvement in living standards, modern record players have been improved and once again have become nostalgically fashionable, and have gradually returned to modern consumer life. Modern record players combine modern sound technology with the classical design of vinyl record players, resulting in perfect blend of functionality, style and decorative design, bringing consumers an authentically elegant feel. However, in such existing vinyl record players, there is only the record player, the operation of the player is complicated, and the player does not provide easy music selection functions. Such record players have a playback for a relatively short period of time and do not provide density recording.


A method of controlling a welding system includes controlling a weld current supplied to an electrode at a current ramp rate and determining an arc length based at least in part on the controlled weld current and a changing arc voltage. The arc length includes a distance between the electrode and a workpiece, and the arc voltage includes a voltage between the electrode and the workpiece.

The invention relates generally to welding systems, and particularly to control of a welding system for gas-metal arc welding (GMAW), also known as metal inert gas (MIG) welding systems.
Arc welding systems generally comprise a power supply that applies electrical current to an electrode so as to pass an arc between the electrode and a workpiece, thereby heating the electrode and the workpiece to create a weld. In many systems, such as gas metal arc welding systems (GMAW), the electrode consists of a wire which is advanced through a welding torch. As the electrode is heated by the arc, the electrode melts and is joined to molten metal of the work piece to form the weld.
Advanced forms of MIG welding are based upon generation of pulsed power in the welding power supply, which may be known as pulsed gas metal arc welding (GMAW-P). That is, various pulsed regimes may be carried out in which current pulses and/or voltage pulses are commanded by the power supply control circuitry to regulate the formation and deposition of metal droplets from the welding wire, to sustain a desired heating and cooling profile of the weld pool, to control shorting between the wire and the weld pool, and so forth.
By controlling the supply of voltage and current to the electrode, a GMAW system may control the manner in which the electrode is melted and deposited by the arc. Controlling the arc length between the electrode and the workpiece may affect the energy applied and/or how the electrode is deposited by the arc. Some GMAW systems may attempt to maintain a constant arc length by controlling the weld voltage supplied to the torch. However, an arc voltage across the arc length may be only a part of the weld voltage between the torch and the workpiece.

Extraction of arc length from voltage and current feedback


The present invention relates to novel compounds which are protein kinase C inhibitors, methods for their preparation, intermediates therefor and pharmaceutical compositions comprising them. More particularly, the present invention relates to compounds of formula (I):

The present invention relates to novel compounds which are protein kinase C inhibitors, methods for their preparation, intermediates therefor and pharmaceutical compositions comprising them.
Protein kinase C (PKC) is a family of phospholipid-dependent serine/threonine-specific protein kinases which play an important role in cellular growth control, regulation and differentiation.
Since the activation of PKC has been implicated in several human disease processes, including various forms of cancer, different forms of inflammatory and/or immunological disorders as well as some neurological disorders, inhibition of PKC could be of therapeutic value in treating these conditions.
Several classes of compounds have been identified as PKC inhibitors, e.g. isoquinoline sulphonamides, sphingosine and related sphingolipids, indolocarbazoles and bisindolylmaleimides.
EP 0 328 026 describes the use of certain bisindolylmaleimides, a class of compounds related to the indolocarbazoles, in medicaments for the treatment of various conditions.
Although PKC inhibitors are described in the prior art, there is a need for specific anti-inflammatory and immuno suppressive compounds, which are suitable for oral administration, and for inhalation. Furthermore, there is a need for such compounds, which are more soluble and less colored than the presently known PKC inhibitors.
The present invention provides kinase inhibitors which are particularly PKC inhibitors. methods for their preparation and intermediates used for their preparation.
The kinase inhibitors of the present invention are surprisingly more soluble and less colored than the kinase inhibitors, especially the PKC inhibitors. known in the prior art.
The present invention also provides the use of the compounds of the present invention for the treatment of inflammatory, immunological, bronchopulmonary, cardiovascular, oncological or CNS-degenerative disorders.
Also provided by the present invention are pharmaceutical compositions comprising a compound according to the present invention, as active ingredient, together with a pharmaceutically acceptable adjuvant, diluent or carrier.
The present invention provides a compound of formula (I):
wherein: one of Ar1 and Ar2 is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X is O or, when one of Ar1 and Ar2 is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl and the other is optionally substituted heteroaryl then X may also be S; and R is H, OH, NH2 or C1-6 alkyl (itself optionally substituted by amino or hydroxy); or a salt or solvate thereof, or a solvate of a salt thereof; provided that when X is O, R is hydrogen and one of Ar1 and Ar2 is phenyl or phenyl optionally mono-substituted by halogen or C1-4 alkyl then the other is not 3,4-methylenedioxyphenyl, unsubstituted benzthiazol-2-yl, a phthalimide or 1,8-naphthalimide.
Heteroaryl includes monocyclic, bicyclic and tricyclic heteroaryl. Heteroaryl includes pyridinyl, pyridin-2-onyl, thienyl, furyl, pyrrolyl, pyrazolyl, quinolinyl, isoquinolinyl, xanthen-9-yl, quinolizin-3-yl, benzothienyl, benzofuryl, indazolyl, 9H-pyrido[3,4-b]indolyl, 1H-pyrrolo[2,3-b]pyridinyl, 6,7,8,9-tetrahydro-pyrido[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, indolyl and benzothiophenyl. In one aspect the present invention provides a compound of formula (I) wherein Ar1 and Ar2 are both bicyclic heteroaryl (wherein each heteroaryl has a single heteroatom, such as a N, O or S atom).
It is preferred that aryl is phenyl or naphthyl.
In another aspect Ar1 and Ar2 are selected from pyridinyl, pyridin-2-onyl, thienyl, furyl, pyrrolyl, pyrazolyl, quinolinyl, isoquinolinyl, xanthen-9-yl, quinolizin-3-yl, benzothienyl, benzofuryl, indazolyl, 9H-pyrido[3,4-b]indolyl, 1H-pyrrolo[2,3-b]pyridinyl, 6,7,8,9-tetrahydro-pyrido[1,2-a]indolyl, 2,3-dihydro-1H-pyrrolo[1,2-a]indolyl, indolyl, benzothiophenyl, naphthyl and phenyl.
In a further aspect the present invention provides a compound of formula (I) wherein heteroaryl and bicyclic heteroaryl are, independently, substituted indolyl, such as substituted indol-3-yl, for example substituted at the 1 position.
In another aspect the optional substituents on the heteroaryl (such as mono-, bi- or tri-cyclic heteroaryl) and aryl groups are selected from the group comprising: halo, cyano, nitro, hydroxy, CO2(C1-4 alkyl), C1-8 alkyl (optionally substituted by halo, hydroxy, cyano, C1-4 alkoxy (optionally substituted by NH2, CO2(C1-4 alkyl)), NRaRb, SC(xe2x95x90NH)NH2, C(xe2x95x90NH)NRcRd, Nxe2x95x90C(Re)NRfRg, N(Rh)C(xe2x95x90O)Ri, NHC(xe2x95x90NH)NH2, heterocyclyl (optionally substituted by C1-4 alkyl or phenyl(C1-4)alkyl), phenyl (optionally substituted by C1-4 alkyl (itself optionally substituted by amino), C(xe2x95x90NH)ORj, C(xe2x95x90NH)NRkRl), pyridinyl (optionally substituted by C1-4 alkyl (itself optionally substituted by amino))), C5-6 cycloalkyl (optionally substituted by hydroxy, NRmRn or alkyl (itself optionally substituted by NRoRp)), C5-6 cycloalkenyl (optionally substituted by NRqRr or alkyl (itself optionally substituted by NRsRt)), heterocyclyl (optionally substituted by C1-4 alkyl or C1-4 haloalkyl), phenyl (optionally substituted by halo), C1-6 alkoxy (optionally substituted by phenyl), phenoxy and amino (optionally substituted by C1-4 alkyl); wherein Ra, Rb, Rm, Rn, Ro, Rp, Rq, Rr, Rs and Rt are, independently, hydrogen or C1-4 alkyl (itself optionally substituted by hydroxy, phenyl, CO2H or CO2(C1-4 alkyl)); and, Rc, Rd, Re, Rf, Rg, Rh, Ri, Rj, Rk and Rl are, independently, hydrogen, C1-4 alkyl or phenyl(C1-4)alkyl; or Rk and Rl join to form a heterocyclic ring (such as morpholine).
In a further aspect X is oxygen.
Salts of the compounds of formula (I) are preferably pharmaceutically acceptable salts. pharmaceutically acceptable salts of compounds of the present invention are preferably those well known in the art as being suitable and are, for example, acid addition salts (such as hydrochloride, hydrobromide or acetate salts) or a salt of a compound of formula (I) with an alkyl halide (such as methyl bromide).
Solvates of the compounds or salts of the present invention are conveniently hydrates, such as monohydrates or dihydrates.
Compounds of the present invention include all stereoisomers and mixtures thereof in all proportions.
In a still further aspect the present invention provides a compound of formula (II) or (II):
wherein: Ar1 and Ar2 are optionally substituted heteroaryl or optionally substituted aryl: R is hydrogen or C1-3 alkyl; X is O or, when Ar1 or Ar2 is optionally substituted heteroaryl X may also be S; R1 and R2 are each independently H, C1-6 alkyl, halogen, C1-3 alkoxy, benzyloxy, hydroxy, cyano, fluoro substituted (C1-3) alkyl, carboxy or carbo(C1-3)alkoxy; R3 is H, C1-6 alkyl, benzyl, C1-3 alkoxy substituted benzyl, hydroxy(C1-6)alkyl, hydroxy(C3-7)cycloalkyl, nitrile(C1-6)alkyl, azido(C1-6)alkyl, amino(C1-6)alkyl, amino(C3-7)cycloalkyl, aminomethyl(C3-7)cycloalkyl, amino(C5-7)cycloalkenyl, (mono- or di- C1-6alkyl) amino(C1-6)alkyl, benzylamino(C1-6)alkyl, (mono- or di-C1-6alkyl) amino(C3-7)cycloalkyl, (mono- or di-C1-6alkyl) aminomethyl(C3-7)cycloalkyl, (amino(C3-7)alkylphenyl)(C1-3)alkyl, amino(C1-3)alkylphenyl, guanidino(C1-6)alkyl, amidino(C1-6)alkyl, amidinothio(C1-6)alkyl, [N,N-di-(C1-6)alkyl]amidino(C1-6)alkyl, amidino(C1-3)alkylphenyl, [N,N-mono- or di-(C1-6)alkyl]amidino(C1-3)alkylphenyl, (N-benzyl)amidino(C1-3)alkylphenyl, (4-morpholinyl)imino(C1-3)alkylphenyl, benzimic acid methyl ester(C1-3)alkyl, hydroxy(C1-3)alkylamino (C1-6)alkyl, carboxy(C1-3)alkylamino (C1-6)alkyl, carboxymethyl(C1-3)alkylamino (C1-6)alkyl, amino(C1-3)alkyloxy (C2-6)alkyl, formamide(C1-6)alkyl, (N,N-dimethyl)imidoformamide(C1-6)alkyl, or a group of the formula
xe2x80x94(CH2)n-Het
in which n is an integer of 0-6, and Het is an optionally substituted 5- or 6-membered heterocyclic group; R4 is H, C1-3 alkyl or together with R3, forms an annulated ring which may be substituted by hydroxy(C1-3) alkyl or amino(C1-3) alkyl; or a salt or a solvate thereof, or a solvate of such a salt. preferred are compounds of formula (II) and (III) in which Ar1 or Ar2 is optionally substituted bicyclic heteroaryl.
In another aspect the present invention provides a compound of formula (XV):
wherein R, R1, R2, R3 and R4 are as defined above and Ar2 is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl.
In yet another aspect the present invention provides a compound of formula (IV):
wherein R1-R4 are as defined in formula (II) and (III); R5 is H, C1-6 alkyl, benzyl, hydroxy(C1-6)alkyl or amino(C1-6)alkyl; R6 and R7 are each independently H, C1-3 alkyl, halogen, fluorosubstituted C1-3 alkyl, C1-3 alkoxy, benzyloxy, hydroxy, cyano, carboxy or carbo(C1-3)alkoxy; or a salt or solvate thereof, or a solvate of such a salt.
For compounds of formula (IV), the following independent preferences apply: R3 or R5 is aminopropyl, aminobutyl, aminopentyl, aminocyclopentyl, aminomethylcyclopentyl, (dimethylamino)methylcyclopentyl guanidinopropyl, amidinopropyl, amidinobutyl, amidinothiopropyl, ethylaminopropyl, dimethylaminopropyl, dimethylaminobutyl, morpholinopropyl, methylpiperazinopropyl, methylpiperidinyl, piperidinomethyl, benzylpiperidinomethyl, diethylaminocyclopentyl or dimethylaminocyclopentyl;
R1, R2, R6 and R7 are each independently methyl, methoxy, cyano or halogen, preferably F or Cl.
In yet another aspect he present invention provides compounds of formula (I):
wherein:
Ar1 and Ar2 are
i) the same or different bicyclic heteroaromatic group(s), or
ii) independently bicyclic heteroaromatic group, and an optionally substituted aromatic or heteroaromatic group,
X is O or S, and
R is H, OH, NH2, C1-6alkyl, aminoC1-6alkyl or hydroxyC1-6alkyl,
and salts and solvates thereof and solvates of such salts.
In preferred embodiments of formula (I), when Ar1 and/or Ar2 are a bicyclic heteroaromatic or heteroaromatic group they include a single heteroatom selected from N, O and S.
In yet more preferred embodiments of formula (I), Ar1 and/or Ar2 are selected from benzothiophene, naphthyl, optionally substituted phenyl and optionally substituted indolyl. Optional substituents for Ar1 and/or Ar2 include aminopropyl, aminobutyl, ethylaminopropyl propyl, ethylaminobutyl, dimethylaminopropyl, dimethylaminobutyl, aminocyclopentyl, ethylaminocyclopentyl, dimethylaminocyclopentyl, amidinoalkyl, amidinothioalkyl and guanidinoalkyl.
Preferred embodiments of formula (I) are compounds of formula (II) and (III)
wherein:
Ar is an optionally substituted aromatic, heteroaromatic or bicyclic heteroaromatic group
R is hydrogen or C1-3 alkyl
R1 and R2 are each independently H, C1-6 alkyl, halogen, C1-3 alkoxy, bensyloxy, hydroxy, carboxy, carboC1-3alkoxy, carbamoyl and C1-3 alkylcarbamoyl.
R3 is H, C1-6alkyl, bensyl, C1-3alkoxy substituted bensyl, hydroxyC1-6alkyl, hydroxiC3-7cykloalkyl, nitrileC1-6alkyl, azidoC1-6alkyl, aminoC1-6alkyl, aminoC3-7cycloalkyl, (mono- or di-C1-6alkyl) aminoC1-6alkyl, (mono- or di-C1-6alkyl) aminoC3-7cycloalkyl, (aminoC1-3alkylphenyl)C1-3alkyl, aminoC1-3alkylphenyl, guanidinoC1-6alkyl, amidinoC1-6alkyl, amidinothioC1-6alkyl, aminoC1-6 alkoxy substituted alkyl, aminoC1-6 hydroxy substituted alkyl, aminoC1-6 amino substituted alkyl or a group of the formula
xe2x80x94(CH2)n-Het
in which
n is an integer of 1-6, and
Het is an optionally substituted 5- or 6-membered heterocyclic group
R4 is H, C1-3 alkyl or together with R3, forms an annulated ring which may be substituted by hydroxyC1-3 alkyl or aminoC1-3 alkyl,
and salts and solvates thereof and solvates of such salts.
More preferred embodiments of formula (I) are compounds of formula (II) and (III), in which Ar is an optionally substituted bicyclic heteroaromatic group.
Even more preferred embodiments of formula (I) are compounds of formula (IV)
wherein
R1-R4 are as defined in formula (II) and (III),
R5 is H, C1-6 alkyl, bensyl, hydroxyC1-6 alkyl, aminoC1-6 alkyl,
R6 and R7 are each independently H, C1-3 alkyl, halogen, C1-3 alkoxy, bensyloxy, hydroxy, carboxy, carboC1-3alkoxy, carbamoyl and C1-3 alkylcarbamoyl,
and salts and solvates thereof and solvates of such salts.
For compounds of formula (IV), the following independent preferences apply:
xe2x80x94R3 or R5 is aminoethyl, aminopropyl, aminobutyl, aminomethyl benzyl, aminocyclopentyl guanidinopropyl, amidinobutyl, amidinothiopropyl, ethylaminopropyl, ethylaminobutyl, dimethylaminopropyl, dimethylaminobutyl, ethylaminocyclopentyl, or dimethylaminocyclopentyl.
xe2x80x94R1, R2, R6 and R7 are each independently halogen, preferably F or Cl.
Preferred compounds according to the present invention include:
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4dihydro-[1,2,4]triazol-3-one
4-[1-(4-Aminobutyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4dihyro-[1,2,4]triazol-3-one
4-[1-(5-Aminopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Dimethylamino-propyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Dimethylamino-butyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Ethylamino-propyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(1H-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
5-(5-Fluoro-1-methyl-indol-3-yl)-4-[5-fluoro-1-(3-morpholin-4-yl-propyl)-indol-3-yl]-2,4-dihydro-[1,2,4]triazol-3-one
5-(5-Fluoro-1-methyl-indol-3-yl)-4-{5-fluoro-1-[3-(4-methyl-piperazin-1-yl)-propyl]indol-3-yl }-2,4-dihydro-[1,2,4]triazol-3-one
2-(3-{5-Fluoro-3-[3-(5-fluoro-1-methyl-indol-3-yl)-5-oxo-1,5-dihydro-[1,2,4]triazol-4-yl]-indol-1-yl}-propyl)-isothiourea
N-(3-{5-Fluoro-3-[3-(5-fluoro-1-methyl-indol-3-yl)-5-oxo-1,5-dihydro-[1,2,4]triazol-4-yl-indol-1-yl}-propyl]-guanidine
5-{5-Fluoro-3-[3-(5-fluoro-1-methyl-indol-3-yl)-5-oxo-1,5-dihydro-[1,2,4]triazol-4-yl]indol-1-yl}-butanamidine
5-{5-Fluoro-3-[3-(5-fluoro-1-methyl-indol-3-yl)-5-oxo-1,5-dihydro-[1,2,4]triazol-4-yl]indol-1-yl}-pentanamidine
4-[1(S)-(3(S)-Aminocyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(R)-(3(R)-Aminocyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(R)-Aminocyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(R)-(3(S)-Aminocyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(S)-Aminocyclopentyl)-indol-3-yl]-5-(1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(S)-Dimethylamino-cyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(S)-Diethylamino-cyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(R)-Aminomethyl-cyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1(S)-(3(R)-Dimethylaminomethyl-cyclopentyl)-5-fluoro-indol-3-yl]-5-(5-fluoro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
5-(5-Fluoro-1-methyl-indol-3-yl)-4-(5-fluoro-1-piperidin-4-ylmethyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
5-(5-Fluoro-1-methyl-indol-3-yl)-4-[5-fluoro-1-(1-methyl-piperidin-4-yl)-indol-3-yl)-2,4dihydro-[1,2,4]triazol-3-one
4-[1-(1-Benzyl-piperidin-4-ylmethyl)-5-fluoro-indol-3-yl]-5(5-fluoro-1-methyl-indol-3yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(1,5-dimethyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(5-chloro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(5-cyano-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-fluoro-indol-3-yl]-5-(5-methoxy-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-[1-(3-Aminopropyl)-5-chloro-indol-3-yl]-5-(5-chloro-1-methyl-indol-3-yl)-2,4-dihydro-[1,2,4]triazol-3-one
4-(1-Methyl-indol-3-yl)-5-(8-aminomethyl-6,7,8,9-tetrahydro-pyrido[1,2-a]indol-10-yl)-2,4-dihydro-[1,2,4]triazol-3-one
or a salt or solvate thereof or a solvate of such a salt.
Preparation of the Compounds of the Invention
Compounds of formula (I) may be synthesized in the following ways:
(a) Compounds of formula (I), in which R is C1-3 alkyl (optionally substituted by amino or hydroxy), comprising alkylating a compound of formula (I) in which R is hydrogen with the corresponding C1-3 alkyl (optionally substituted by amino or hydroxy) alkylating agent.
(b) Compounds of formula (I), in which R is H may be synthesized by intramolecular condensation of a compound of formula (VI):
in which Ar1 and Ar2 are as defined for formula (I).
(c) Compounds of formula (I) may be synthesized by converting a compound of formula (I) to a salt, especially a pharmaceutically acceptable salt thereof, or vice versa; or converting a salt, especially a pharmaceutically acceptable salt of a compound of formula (I) into a different salt, especially a pharmaceutically acceptable salt.
The condensation may be conveniently performed in the presence of trimethylsilyl triflate or bistrimethylsilyl acetamide, and a base e.g. triethylamine in dimethyl formamide at a temperature in the range of from about 100xc2x0 C. to about 160xc2x0 C., suitably from 115xc2x0 C. to 145xc2x0 C. and preferably at about 130xc2x0 C., for a period of time in the range of from about 5 min to about 6 h, suitably from 15 min to 3 h, preferably for about 1h.
A compound of formula (I) wherein Ar1, Ar2 and/or R carries one or more functional groups which might be sensitive to, or interfere with, the reaction conditions in the processes in (a) or (b), can be prepared by using a corresponding starting material in which the functional group(s) is suitably protected and then deprotected at the end of the process of (a) or (b).
Functional groups that might be sensitive to or interfere with the reaction conditions in processes (a) or (b), as well as suitable protecting groups and deprotecting methods, are evident to those skilled in the art.
The starting materials for the above processes (a), (b) and (c) may be made by the methods described herein and particularly by those methods set out in the Examples or by methods analogous thereto. Other conventional methods for making the starting materials will be evident to those skilled in the art.
A compound of formula (II) or (III), or a salt thereof, in which at least one of R3 or Ar carries an amino or hydroxy group can be prepared by deprotecting the corresponding compound of formula (II) and (III) wherein said amino or hydroxy group is protected.
In the processes described above, the protecting groups and conditions for deprotection are well known to those skilled in the art. Suitable protecting groups for amino groups are e.g t-butoxy carbonyl groups and the deprotecting agent may be trifluoroacetic acid in a suitable solvent e.g. a mixture of acetonitrile and water. The hydroxy groups may be protected as their corresponding tert-butyldimethylsilyl (TBDMS) oxy groups and the deprotecting agent may be acetic acid in e.g. water. The deprotecting step may be carried out in a suitable solvent, e.g. tetrahydrofuran at about 60-80xc2x0 C., e.g. for about 2 hours.
The use of protecting groups is fully described in xe2x80x9cProtective Groups in Organic Chemistryxe2x80x9d, edited by J. W. F. McOmie, Plenum Press (1973) and xe2x80x9cProtective Groups in Organic Synthesisxe2x80x9d, 2nd edition, T. W. Greene and P. G. M. Wutz, Wiley-Interscience (1991).
Compounds of formula (II) or (III), in which R3 is an alkyl carrying an amino group, may be prepared by reduction of a compound of formula (IX) or (X) respectively:
wherein R, R1, R2, R4 and Ar are as defined for formula (II) and (III), and R311 is an alkyl group.
In the process above, the conditions for the reduction are well known to those skilled in the art. Suitable conditions for the reduction of the azido group are e.g. hydrogenation on Pd/C at atmospheric pressure or the use of Staudinger conditions i.e. triphenyl phosphine in pyridine, followed by addition of ammonia (aq).
Compounds of formula (II) or (III), in which R3 is an alkyl carrying a thioamidino, monoalkyl amino, dialkyl amino, or a trialkyl amino group may be prepared by reaction of a compound of formula (XI) or (XII), respectively, with thiourea, or a suitable monoalkyl-, diakyl- or trialkyl amine:
wherein R, R1, R2, R4 and Ar are as defined in formula (II) and (III), R311 is an alkyl group and LG is a leaving group, e.g. mesylate or bromide.
Compounds of formula (XI) and (XII) may be synthesized by transforming under standard conditions well known to the person skilled in the art the alcohol function in compounds of formula (XIII) and (XIV):
wherein R, R1, R2, R4 and Ar are as defined in formula (II) and (III) and R311 is an alkyl group.
Compounds of formula (II) in which R3 is alkyl or phenylalkyl carrying an amidino or a guanidino group may be synthesized using standard methods, from compounds of formula (XV) corresponding to formula (II), but in which R3 is alkyl carrying a nitrile or primary amine, by reacting with hydrogen chloride in ethanol followed by ammonia in methanol or by reacting with 3,5-dimethylpyrazole-1-carboxamidinium nitrate in refluxing ethanol and in the presence of a base, respectively.
Compounds of formula (II) or (III), as defined above, wherein R3 is alkyl carrying an amidino or guanidino group can be prepared by: (i) reacting a compound of formula (II) or (III), in which R3 is alkyl carrying a nitrile, with hydrogen chloride in ethanol followed by ammonia in methanol; or, (ii) reacting a compound of formula (II) or (III), in which R3 is alkyl carrying a primary amine, with 3,5-dimethylpyrazole-1-carboxamidinium nitrate in refluxing ethanol in the presence of a base.
Compounds of formula (II) or (III), as defined above, wherein R3 is alkyl or phenylalkyl carrying a N-substituted or N,N-di-substituted amidino group, can be prepared by reacting a compound of formula (II) or (III), in which R3 is alkyl or phenyl alkyl carrying a nitrile, with hydrogen chloride in methanol, followed by treatment with the appropriate amine in methanol.
Persons skilled in the art will appreciate that, in order to obtain compounds of the invention in an alternative, and, on some occasions, more convenient, manner, the individual process steps mentioned herein may be performed in a different order, and/or the individual reactions may be performed at a different stage in the overall route. This will e.g. on factors such as the nature of other functional groups present in a particular substrate, the availability of key intermediates and the protecting group strategy (if any) to be adopted.
Novel intermediates as described hereinbefore and their use in the manufacture of other compounds of the present invention also form part of the invention. Thus, according to a further aspect of the invention there is provided an intermediate compound of formula (VI), (IX), (X), (XI), (XII), (XIII) or (XIV) as defined hereinbefore, or a protected derivative of any of these compounds.
Prodrugs
It will also be appreciated by those skilled in the art that, although certain protected derivatives of compounds of formula (I), (II), (III), (IV) and (XV), which may be made prior to a final deprotection stage, may not possess pharmacological activity as such, they may be administered parenterally or orally and thereafter metabolized in the body to form compounds of the invention which are pharmacologically active. Such derivatives may therefore be described as xe2x80x9cprodrugsxe2x80x9d. Moreover, certain compounds of formula (I), (II), (III), (IV) and (XV) may act as prodrugs of other compounds of formula (I), (II), (III), (IV) and (XV).
All prodrugs of compounds of formula (I), (II), (III), (IV) and (XV) are included within the scope of the present invention.
Medical and Pharmaceutical Use
Also provided according to the present invention are compounds of the present invention for use in medical therapy; the use of compounds of the present invention in the manufacture of medicaments for use in the treatment of the conditions described herein: and methods of medical therapy comprising the administration of a therapeutically effective amount of a compound of the present invention to an individual requiring such therapy.
The term xe2x80x98medical therapyxe2x80x99 as used herein is intended to include prophylactic, diagnostic and therapeutic regimens carried out in vivo or ex vivo on humans or other mammals.
The compounds of formula (I), (II), (III), (IV) and (XV) and pharmaceutically acceptable salts thereof, are useful because they demonstrate pharmacological activity. In particular they demonstrate activity as kinase inhibitors, especially PKC inhibitors, e.g. as is shown by their activity in the in vitro assays described in Jirousek, M. J. et al, J. Med. Chem. 1996, 39, 2664-2671; or as described in Granet, R. A. et al, Analyt. Biochem. 1987; 163, 458-463; Olsson, H. et al, Cell Signal 1989, 1, 405-410; and Chakravarthy, B. R. et al, Analyt. Biochem. 1991, 196, 144-150.
The compounds of the invention are indicated for use in the treatment of inflammatory, immunological. bronchopulmonary, cardiovascular, oncological or CNS-degenerative disorders; preferably for oral or topical treatment of inflammatory and/or immunological disorders, such as the oral or topical treatment of airway diseases involving inflammatory conditions, e.g. asthma, chronic obstructive pulmonary disease (COPD), including chronic bronchitis and emphysema; or atopic diseases, e.g. rhinitis or atopic dermatitis; inflammatory bowel diseases, e.g. Crohn""s disease or colitis; autoimmune diseases e.g. multiple sclerosis, diabetes, atherosclerosis, psoriasis, systemic lupus erythematosus or rheumatoid arthritis; malignant diseases, e.g. skin or lung cancer; HIV infections or AIDS; or for inhibiting rejection of organs/transplants. The compounds of the invention are also indicated for use in treatment of heart failure, and in treatment of diabetic patients with macular edema or diabetic retinopathy.
Thus, in a further aspect the present invention provides the use of a compound of formula (I):
wherein: one of Ar1 and Ar2 is optionally substituted bicyclic heteroaryl or optionally substituted tricyclic heteroaryl and the other is optionally substituted heteroaryl or optionally substituted aryl; X is O or S; and R is H, OH, NH2 or C1-6 alkyl (itself optionally substituted by amino or hydroxy); or a salt, solvate or hydrate thereof, or a solvate or a hydrate of a salt thereof: in the manufacture of a medicament for use in the treatment of inflammatory, immunological, bronchopulmonary, cardiovascular, oncological or CNS disorders.
A method of treating a PKC mediated disease state in mammals which comprises administering to a mammal in need of such treatment an effective amount of a compound of formula (I) as defined in the preceding paragraph or a salt, solvate or hydrate thereof, or a solvate or a hydrate of a salt thereof.
Pharmaceutical Preparations
The dose of the compound to be administered will depend on the relevant indication, the age, weight and sex of the patient and may be determined by a physician. The dosage will preferably be in the range of from 0.01 mg/kg to 10 mg/kg.
The compounds may be administered topically, e.g. to the lung and/or the airways, in the form of solutions, suspensions, HFA aerosols or dry powder formulations, e.g. formulations in the inhaler device known as the Turbuhaler(copyright); or systemically, e.g. by oral administration in the form of tablets, pills, capsules, syrups, powders or granules, or by parenteral administration, e.g. in the form of sterile parenteral solutions or suspensions, or by rectal administration, e.g. in the form of suppositories.
The compounds of the invention may be administered on their own or as a pharmaceutical composition comprising the compound of the invention in combination with a pharmaceutically acceptable diluent, adjuvant and/or carrier. Particularly preferred are compositions not containing material capable of causing an adverse, e.g. an allergic, reaction.
Dry powder formulations and pressurized HFA aerosols of the compounds of the invention may be administered by oral or nasal inhalation. For inhalation the compound is desirably finely divided. The finely divided compound preferably has a mass median diameter of less than 10 xcexcm, and may be suspended in a propellant mixture with the assistance of a dispersant, such as a C8-C20 fatty acid or salt thereof, (e.g. oleic acid), a bile salt. a phospholipid, an alkyl saccharide, a perfluorinated or polyethoxylated surfactant, or other pharmaceutically acceptable dispersant.
The compounds of the invention may also be administered by means of a dry powder inhaler. The inhaler may be a single or a multi dose inhaler, and may be a breath actuated dry powder inhaler.
One possibility is to mix the finely divided compound with a carrier substance, e.g. a mono-, di- or polysaccharide, a sugar alcohol, or another polyol. Suitable carriers are sugars, e.g. lactose, glucose, raffinose, melezitose, lactitol, maltitol, trehalose, sucrose, mannitol; and starch. Alternatively the finely divided compound may be coated by another substance. The powder mixture may also be dispensed into hard gelatin capsules, each containing the desired dose of the active compound.
Another possibility is to process the finely divided powder into spheres which break up during the inhalation procedure. This spheronized powder may be filled into the drug reservoir of a multidose inhaler, e.g. that known as the Turbuhaler(copyright) in which a dosing unit meters the desired dose which is then inhaled by the patient. With this system the active compound, with or without a carrier substance, is delivered to the patient.
For oral administration the active compound may be admixed with an adjuvant or a carrier, e.g. lactose, saccharose, sorbitol, mannitol; a starch, e.g. potato starch, corn starch or amylopectin; a cellulose derivative; a binder, e.g. gelatin or polyvinylpyrrolidone, and/or a lubricant, e.g. magnesium stearate, calcium stearate, polyethylene glycol, a wax, paraffin. and the like, and then compressed into tablets. If coated tablets are required, the cores, prepared as described above, may be coated with a concentrated sugar solution which may contain e.g. gum arabic, gelatin, talcum, titanium dioxide, and the like. Alternatively, the tablet may be coated with a suitable polymer dissolved in a readily volatile organic solvent.
For the preparation of soft gelatin capsules, the compound may be admixed with e.g. a vegetable oil or polyethylene glycol. Hard gelatin capsules may contain granules of the compound using either the above mentioned excipients for tablets. Also liquid or semisolid formulations of the drug may be filled into hard gelatin capsules.
Liquid preparations for oral application may be in the form of syrups or suspensions, for example solutions containing the compound, the balance being sugar and a mixture of ethanol, water, glycerol and propylene glycol. Optionally such liquid preparations may contain coloring agents. flavoring agents, saccharine and/or carboxymethylcellulose as a thickening agent or other excipients known to those skilled in art.
The compounds of the invention may also be administered in conjunction with other compounds used for the treatment of the above conditions.
The following Examples are intended to illustrate, but in no way limit the scope of the invention.
All reactions were performed in dried glassware in an argon or nitrogen atmosphere at room temperature, unless otherwise noted. Tetrahydrofuran (THF) was distilled from sodium benzophenone ketyl under N2 prior to use. N,N-Dimethyl formamide (DMF) was distilled from calcium hydride and stored over molecular sieves. All other solvents and reagents were used as received.
1H-NMR spectra were recorded on a Varian Inova-400 or Unity-500+ instrument. The central solvent peak of chloroform-d (xcex4H 7.27 ppm), dimethylsulfoxide-d6 (xcex4H 2.50 ppm) or methanol-d4 (xcex4H 3.35 ppm) were used as internal references. Low-resolution mass spectra were recorded on an Autospec-Q, Fisons Analytical, double focusing sector instrument equipped with a LSIMS interface. Low resolution mass spectra were also obtained on a Hewlett Packard 1 100 LC-MS system equipped with an APCI ionization chamber.
Analytical HPLC was run on a Hewlett Packard LC-MS 1100, using a C-18 reversed phase column and eluting with the following general system: acetonitrile:water (20:80 to 90:10 gradient) containing 0.1% TFA. Preparative LC was run on a Kromasil KR-100-10-C18 column (250xc3x9750 mm), using different proportions of acetonitrile:water as eluent, containing 0.1% TFA.
Reversed-phased column chromatography was done with pre-packed columns (Merck, Lobar, LiChroprep RP-18 equipped with a peristaltic pump) using methanol:water and 0.1% acid (TFA, HCl. or HBr) as eluent.
Flash chromatography was performed on silica (Merck 40-63 xcexcm) with the eluents indicated in the specific Examples.
IR was run on a Perkin Elmer 16 PC FT-IR.

Abstract: X is O or S; and

Abstract: R is H, OH, NH2 or C1-6 alkyl (itself optionally substituted by amino or hydroxy); or a salt or solvate thereof, or a solvate of a salt thereof; and the use of such compounds in medical therapies.


The present invention includes an electrical connector system utilizing a single piece slide lever system which is lockable in a pre-staged and in a final fully seated position. The slide lever is used to mechanically assist the mating of male and female connectors. The slide lever may also be received inside of a flexible grommet to provide a mechanical assist in making a seal between the grommet and a panel. The locking features and the slide lever may be selectively released to move the slide lever from a pre-staged position (open position) to a final seated position (closed position) locking the two connector pieces together. Likewise, the locking features on the slide lever may be released to move the slide lever from a final fully seated (closed) position back to a pre-staged (open) position to disconnect the connector pieces all while the slide lever is contained within the flexible grommet.

Flexible rubber grommets have been used to provide water-tight seals around electrical connectors that extend from one panel to another in a vehicle, such as from a door panel to a body panel. Usually the grommet includes a first sealing end which has sealing lips that are inserted into an aperture in a first panel. A grommet conduit portion extends from the first sealing end and terminates with a second sealing end. A first connector piece is received inside of a housing of the second sealing end and a wire harness extends through the conduit portion and through the aperture in the first panel. A second connector piece is provided and includes a wire harness extending through an aperture in a second panel. The first and second connector pieces are mated together and the second sealing end of the grommet includes sealing lips that are inserted manually into the aperture in the second panel to provide a water-tight seal surrounding the two connector pieces. This method of assembling a connector piece is labor intensive and, due to space constraints, is often extremely difficult for the assembler to manually insert the second sealing end of the grommet into the aperture of the second panel.
The use of slide levers to mechanically assist the connection of mating connector pieces has been known. FIG. 6 illustrates such a known system including a first connector 210 having a body portion 212 with a plurality of metal terminals received therein and a surrounding housing 214. A slide lever is provided for slidable movement in a channel provided between the body portion and the outer housing. The slide lever includes a plunger portion 216 connected to a bridge 218 and two spaced apart parallel elongated lever arms 220. The lever arms 220 each include a slot formed therein generally in a diagonal direction with respect to the longitudinal axis of elongated lever arms. The system is shipped in an open pre-staged position utilizing a separate wedge piece 222 that is snapped onto the lever arms 220 and between the bridge 218 and the housing 214 or body portion 212 to prevent downward movement of the lever. The second mating connector housing (not shown) includes an outwardly extending pin that is received in the channel formed in the lever arms. For assembly of the two connector pieces, the second connector housing is placed in engagement with the housing 214 of the first connector and the wedge 222 is removed by an operator and the plunger 216 depressed causing the two connector pieces to be mated together as the pin rides along the diagonal slot of the lever arms 220. However, the separate wedge piece 222 can become dislodged during shipment causing the slide lever to be moved to a closed position. Further, the mating connector housing cannot be disconnected and the slide lever moved back to a pre-staged position without the use of the wedge piece 222 which may not be available in the field.
The present invention provides alternatives to and advantages over the prior art.


An orbit insertion device for artificial satellite aiming to explore a planet with unknown characteristics. A plurality of sensors send a plurality of measured states of the artificial satellite. A planetary attraction constant estimator calculates a planetary attraction constant based on the plurality of measured states. A drag force coefficient estimator calculates a drag force coefficient based on the plurality of measured states. A rate of convergence calculation unit calculates a rate of convergence based on the drag force coefficient. A fictitious control calculation unit calculates a fictitious control based on the planetary attraction constant, the drag force coefficient and the rate of convergence. A normalized thrust calculation unit calculates a normalized thrust based on the fictitious control. A plurality of thrusters generate a thrust based on the normalized thrust.

The present invention relates to an orbit insertion device for artificial satellite aimed to explore a planet of unknown characteristics such as planetary mass density, planetary radius and atmospheric composition.
U.S. Pat. No. 5,595,360 discloses an apparatus for translating a spacecraft from one orbit to another by generating a thrust of a force in timing sequences, both of which are predetermined based on known characteristics of a planet. U.S. Pat. No. 6,213,432 discloses a method for inserting a space vehicle into a target orbit of a planet through a spiral trajectory pre-calculated based on known characteristics of a planet. U.S. Pat. No. 6,341,749 B1 discloses an apparatus for translating a spacecraft from an orbit to another using a nonlinearly varying thrust minimizing transfer time and fuel calculated based on known characteristics of a planet.
The prior arts in U.S. Pat. Nos. 5,595,360, 6,213,432, and 6,341,749 B1, if applied to orbit insertion for artificial satellite aimed to explore a planet of unknown characteristics, fail to insert the artificial satellite into a target orbit since the prior arts are not able to calculate a thrust required by an orbit insertion without a pre-knowledge on the characteristics of the planet.

Orbit insertion device for artificial satellite aimed to explore a planet of unknown characteristics


In summary, the invention is related to the discovery of a class of compounds which inhibits the reaction of a polyepoxide with a curing agent at low temperatures. More particularly the invention relates to an epoxy resin composition comprising. a) a polyepoxide; and PA0 b) a cure inhibitor comprising boric acid.

This invention relates to epoxy resin compositions containing compounds which inhibit the cure of the epoxy resins at lower temperatures. The invention further relates to compositions useful for curing epoxy resins which comprise curing agents for the epoxy resins and the inhibitor described above. The invention further relates to coatings prepared from such inhibited resin compositions, and to materials coated with or encapsulated in such inhibited resin compositions. The invention further relates to laminates, prepregs, encapsulated materials and composites prepared from such inhibited resin compositions.
Epoxy resins are used in a variety of applications, as powder coatings, as electrical encapsulates, in composites, in solution coatings, in prepregs and in laminates. In many of these uses, it is desirable to partially cure the epoxy resin in a controllable manner, such that at a later time, when desired, the epoxy resin can be fully cured. In many uses it is desirable to contact a curing agent for an epoxy resin with an epoxy resin in the presence of a catalyst for the reaction and have the composition remain stable, that is uncured for a period of time. At present it is quite difficult to control the curing of an epoxy resin and retain the stability of a composition comprising an epoxy resin, a curing agent and catalyst for the reaction of the epoxy resin with the curing agent.
In some uses the epoxy resin, curing agent, and catalyst are contacted in solution and then applied as a coating on a substrate. In such uses, in order to achieve optimal properties in the eventually cured epoxy resin, the solvent or solvents must be removed. Often it is desirable to remove these solvents before significant curing takes place, otherwise the solvent may be entrapped in the cured epoxy resin, thereby adversely affecting the final properties of the cured resin. Often, the solvent is removed by exposing the coated article to elevated temperatures. At such temperatures the epoxy resin may have a tendency to begin to cure and entrap the solvent, thereby adversely affecting the final properties.
Cured and partially cured epoxy resins are used in laminates. A common process used in preparing glass laminates involves passing a glass cloth to be coated with an epoxy resin composition through a bath containing the resin, a curing agent for the resin and a catalyst for the curing reaction. Generally the bath contains one or more organic solvents in which the various components are dissolved or dispersed, with a solids contents of between about 45 and about 90 percent. The glass is resident in the bath for time sufficient to coat it with a mixture of the resin, curing agent and catalyst for the curing reaction. Thereafter the coated glass is passed through a heated zone to remove remaining solvent by evaporation. Generally, this zone is at a temperature of between 120.degree. and 200.degree. C. The residence time in this zone is sufficient to allow the solvents to be completely volatilized away. Thereafter the glass cloth, coated with the resin, curing agent and catalyst from which the solvents have been removed, may be controllably partially cured by exposing it to temperatures at which curing occurs. Such a product is referred to as a prepreg. The prepregs may then be stacked or formed into a shape and exposed to conditions under which the curing agent and resin completes the cure. In general, this involves contacting the various components of a laminate at elevated temperatures under pressure, for a period of time sufficient for the epoxy resin to further cure. Usually the pressure is provided by some kind of a press. Once the laminate is removed from the press it may, optionally, be exposed to elevated temperature for a period of time to complete the curing reaction. In this curing process the resin coating on the glass cloth flows and mixes with the coating on adjacent glass clothes thereby resulting in a fusing of the glass layers together, via the cured epoxy resin.
High glass transition temperatures are desirable for many uses, therefore methods of increasing the glass transition temperatures are desired. It is further desired to significantly decrease the time necessary to achieve complete cure. Prepreg producers and laminators desire a composition which facilitates faster processing. This allows the more efficient utilization of processing equipment. In order to facilitate faster processing the coated substrates must be exposed to higher temperatures or the epoxy resin compositions must contain higher levels of catalysts. Unfortunately, both solutions result in less control over the curing reaction and solvent can be trapped in the final product thereby affecting the ultimate properties.
In one embodiment, a process referred to as continuous pressing technology is used. In this process the prepregs are contacted at much higher temperatures than in conventional laminate processing for shorter periods, e.g. at temperatures around 210.degree. C. for 2 to 4 minutes. It is very difficult to achieve complete cure under such conditions. One potential solution to this is to add a larger amount of catalyst or accelerator to the epoxy resin. Unfortunately if additional catalyst is added in the coating bath, then the ability to remove the solvent without significant curing of the epoxy resin, or to controllably partially cure the epoxy resin, is significantly reduced.
What is needed is an epoxy resin composition that does not undergo significant cure at temperatures at which solvents may be removed. What is further needed is an epoxy resin that can be controllably B-staged or partially advanced. What is further needed is an epoxy resin composition which allows the use of higher concentrations of curing catalysts or accelerators, which are stable at temperatures at which solvent is removed, and which allow controllable B-staging or partial advancement. What is further needed is an epoxy resin composition which when coated on a substrate can be processed faster without hurting the ultimate properties.
Frequently, for many products prepared using epoxy resins and cured epoxy resins several different entities may perform different parts of the manufacturing process. For example, one entity may make the resin, a second entity may make the resin formulations used to impregnate the reinforcing material, and a third may make a prepreg, or other article to be used. While a forth would make the final product such as a laminate or printed circuit board. Frequently the entity producing the prepreg or laminate has no expertise or desire to make the formulation. Therefore, it is desirable that a formulator be able to make a composition useful in coating the materials to be laminated. The problem is that if the epoxy resin curing agent and catalyst are preformulated, the formulation may not have significant longterm storage stability. Under such circumstances the formulation may undergo curing and therefore not be useful to the prepreg or laminate manufacturer. What is further needed is an epoxy resin composition containing a curing agent and accelerator for the cure which has significant stability at ambient temperatures for several weeks.

Cure inhibited epoxy resin compositions and laminates prepared from the compositions


A mechanical, pneumatic, magnetic and/or electronic method for assisting the user operation of a trigger and/or actively and rapidly returning the trigger mechanism to its firing position at the completion of a firing sequence in a paintball gun. The trigger assistance mechanism reduces the amount of force required by the user to move the trigger to begin the firing sequence. After the firing sequence has been completed, the trigger assistance mechanism provides assistance to the trigger to move it to its pre-firing resting position. Alternatively, the trigger assistance mechanism replaces the mechanical linkage between the trigger and the cocking/firing mechanism of the paintball gun such that a pneumatic actuating ram is used to initiate the cocking/firing sequence.

The present invention generally relates to a mechanism for assisting the user in the operation of a trigger in a gun mechanism. More specifically, the present invention relates to a mechanical, pneumatic, magnetic or electronic method for assisting the user in the operation of a trigger and/or actively and rapidly returning the trigger mechanism to its firing position at the completion of a firing sequence for use with a paintball gun.
As the game and sport of paintball has grown, an increasing reliance on volume fire has evolved. This reliance on an increase in volume fire is evidenced by the introduction of electronically enhanced guns, improved paintball magazines and paintball feeding mechanisms, improved high speed valves and regulators and a host of other technologies all having a common goal of increasing the rate of fire from the paintball gun.
The goal of increasing the rate at which paintballs can be fired is complicated by an industry prohibition on "fully automatic" firing mechanisms, multiple shot weapons or other enhancements which allow the user to fire more than one paintball per trigger cycle of the weapon. Therefore, an objective throughout the paintball industry is to enhance the rate of fire through various means which maintain the operation of the paintball gun in a true "semi-automatic" firing mode in which one projectile is expelled per complete cycle of the trigger/gun mechanism. Further, a desire exists to eliminate, assist or equalize the force exerted by the use throughout the trigger cycle and to provide a powered or assisted method of returning the trigger to the ready position at the end of the firing sequence.
Despite previously mentioned solutions and enhancements, there are currently no methods available for an "assisted" trigger mechanism in a paintball gun. In principle, an assisted trigger mechanism utilizes the user's own mechanical action of pulling or releasing a trigger mechanism as the initiating force, after which mechanical, pneumatic, electronic, magnetic or a combination of these means is introduced and automatically perform some or all of the trigger cycle.
In currently available paintball guns, a simple trigger mechanism relies on mechanical force from the user to release a captured sear. A hammer, retained by the sear and under spring tension, is released, allowing the hammer to impact a valve stem, thereby opening the valve and firing a projectile and then, utilizing gas blowback to reset the sear.
In order to understand the scope of the present invention, it is necessary to understand that there are currently four "classes" of paintball gun design, each of which has a different configuration but all of which operate on the same principles of design.
The first of the four mechanisms of paintball gun operation is classified as a blowback configuration. This type of gun utilizes a mechanically operated sear connected to the trigger, a spring operated hammer connected mechanically to a bolt, and a spring operated valve mechanism. The bolt is located above the hammer in a separate body channel which is in communication with the gun barrel. In operation, the user first "cocks" the system by pulling a cocking knob connected to the bolt. This causes the hammer to be moved behind the sear and compresses the hammer spring.
When the trigger is pulled, the trigger actuates a sear, releasing the hammer. Under spring tension, the hammer moves forward. Since the bolt is connected to the hammer, when the hammer moves forward, the bolt moves forward as well to push a paintball into the barrel. When the bolt is at its furthest point of forward travel, a gas passage in the bolt is in communication with a vent hole from the valve. Simultaneously, the hammer impacts a valve stem in the face of the valve, opening the valve and releasing a preset amount of pressurized gas. This gas vents through the bolt, thus firing a paintball, and against the hammer, pushing the hammer and the bolt back into the cocked position. At its rearmost point of travel, the sear once again captures the hammer completing the cycle.
The next type of paintball gun uses a "blow forward" type of mechanism in which the bolt is retained by the sear, which is mechanically linked to the trigger. The bolt rides on a tube that communicates with the valve and is retained by the sear under pressure, effectively acting as a seal on the valve system. When the trigger is actuated, the bolt is released. Gas pressure from the valve pushes the bolt forward, which in turn pushes a paintball into the barrel. Once the bolt has reached its furthest point of travel, the gas passage is opened, allowing the gas to flow through the face of the bolt, thus firing the paintball. A spring located forward of the bolt returns the bolt where it is again captured by the sear, thus completing the cycle.
An "autococking" style of semi-automatic paintball guns operate in the same basic manner as the blowback semi-automatic. However, the design is based on what was originally a pump operated paintball gun where the pumping action has been pneumatically automated. This style of design therefore has several additional mechanisms.
In the autococking style mechanism, when the trigger is pulled, the hammer is released, striking the valve and sending gas through the bolt and down the barrel, thus firing a paintball. Gas is also vented to a low pressure regulator, which in turn supplies a three-way valve. The three-way valve is connected to a pneumatic ram, which in turn is mechanically linked to a cocking mechanism and to the bolt.
Gas from the regulator is introduced into the three-way valve which first operates the ram to push the cocking mechanism rearward, pulling the bolt back, allowing a new projectile to enter the barrel and resetting the hammer on the sear. Gas is then vented from the three-way valve, which operates to reverse the flow of gas to the ram, which in turn pulls the bolt and cocking mechanism forward, completing the cycle.
The final type of paintball gun is classified as an electric paintball gun. In some cases, electric paintball guns replaced some or all of the mechanical systems mentioned above with electronic or electromechanical systems. For example, one widely distributed model substitutes an electronic switch connected to a solenoid for the mechanical sear.
In each of the types of paintball guns discussed above, the firing rate of paintballs is limited by the rate at which a human finger can depress and release the trigger of the paintball gun. Since the rate at which a human finger can pull a trigger is somewhat limited by the mechanical action of the trigger mechanism, it is an object of the present invention to provide assistance to the user when pulling the trigger and actively assist in returning the trigger to its initial position.