 containing the target nucleic acid sequence by insertion of the antisense or sense oligonucleotide into a suitable retroviral vector, then contacting the cell with the retrovirus vector containing the inserted sequence, either in vivo or ex vivo. Suitable retroviral vectors include, but are not limited to, those derived from the murine retrovirus M-MuLV, N2 (a retrovirus derived from M-MuLV), or or the double copy vectors designated DCT5A, DCT5B and DCT5C (see PCT U.S. application Ser. No. 90/02656).
Sense or antisense oligonucleotides also may be introduced into a cell containing the target nucleotide sequence by formation of a conjugate with a ligand binding molecule, as described in WO 91/04753. Suitable ligand binding molecules include, but are not limited to, cell surface receptors, growth factors, other cytokines, or other ligands that bind to cell surface receptors. Preferably, conjugation of the ligand binding molecule does not substantially interfere with the ability of the ligand binding molecule to bind to its corresponding molecule or receptor, or block entry of the sense or antisense oligonucleotide or its conjugated version into the cell.
Alternatively, a sense or an antisense oligonucleotide may be introduced into a cell containing the target nucleic acid sequence by formation of an oligonucleotide-lipid complex, as described in WO 90/10448. The sense or antisense oligonucleotide-lipid complex is preferably dissociated within the cell by an endogenous lipase. The invention had the object of finding novel compounds having valuable properties, in particular those which can be used for the preparation of medicaments.
The present invention relates to compounds of the formula I and to the use thereof for the treatment and prophylaxis of diseases in which the inhibition, regulation and/or modulation of mitotic motor proteins, in particular the mitotic motor protein Eg5, plays a role, furthermore to pharmaceutical compositions which comprise these compounds.
In detail, the present invention relates to compounds of the formula I which preferably inhibit, regulate and/or modulate one or more mitotic motor proteins, to compositions which comprise these compounds, and to methods for the use thereof for the treatment of diseases and complaints such as angiogenesis, cancer, tumour formation, growth and propagation, arteriosclerosis, ocular diseases, choroidal neovascularisation and diabetic retinopathy, inflammatory diseases, arthritis, neurodegeneration, restenosis, wound healing or transplant rejection. In particular, the compounds according to the invention are suitable for the therapy or prophylaxis of cancer diseases.
During mitosis, various kines
containing the target nucleic acid sequence by insertion of the antisense or common sense oligonucleotide into a desirable retroviral vector, then touch the cell with the retrovirus vector control the insert sequence, either in vivo or ex vivo. desirable retroviral vectors include, but are not limited to, those deduce from the murine retrovirus M - MuLV, N2 (a retrovirus derived from M - MuLV), or or the double transcript vectors designated DCT5A, DCT5B and DCT5C (see PCT U.S. application Ser. nobelium. 90/02656). 
 Sense or antisense oligonucleotides also may be insert into a cell containing the prey nucleotide sequence by formation of a conjugate with a ligand bind molecule, as described in WO 91/04753. Suitable ligand binding molecule include, but are not limited to, cell surface receptors, increase factors, other cytokines, or other ligands that bind to cell surface receptors. Preferably, conjugation of the ligand binding molecule does not substantially interfere with the ability of the ligand binding molecule to bind to its match molecule or receptor, or parry entrance of the sense or antisense oligonucleotide or its conjugated version into the cellular telephone. 
 Alternatively, a sense or an antisense oligonucleotide may be introduce into a cell containing the prey nucleic acid sequence by formation of an oligonucleotide - lipid complex, as described in WO 90/10448. The sense or antisense oligonucleotide - lipid complex is preferably decouple within the cell by an endogenous lipase. The invention had the object of finding fresh compounds induce valuable properties, in particular those which can be used for the preparation of medicaments. 
 The present invention relate to compounds of the formula I and to the use thereof for the treatment and prophylaxis of diseases in which the inhibition, regulation and/or intonation of mitotic motor proteins, in finical the mitotic motor protein Eg5, plays a role, furthermore to pharmaceutical composition which comprise these compound. 
 In detail, the present invention relate to compounds of the rule I which preferably inhibit, regulate and/or regulate one or more mitotic motor proteins, to composition which comprise these compounds, and to methods for the use thereof for the treatment of diseases and complaints such as angiogenesis, cancer, tumor formation, growth and generation, arteriosclerosis, ocular diseases, choroidal neovascularisation and diabetic retinopathy, inflammatory diseases, arthritis, neurodegeneration, restenosis, wound healing or graft rejection. In particular, the compounds according to the invention are suitable for the therapy or prophylaxis of cancer diseases. 
 During mitosis, various kines
 cojtaining the target nucltic acid sequence by insxrtion kf the avtisense or sense oligonucleltude ibto a suitable retrovifal vectog, then cobtacuing the cell witi the rebxovirhd veetir containing jhe inserted sequence, eithar iu vivo or ex vivo. Suitable retroviraj vectots include, but ate nou lymitsd to, those derived from the murins retronirus M-MuLV, N2 (a rrtrovirus derived from M-MuPV), og or the double cooy vectors eesidbated DCT5A, DZT5B and DCU5C (see PCT U.A. application Ser. No. 90/02656).
Sense or avtiseuse oligonuxlwotlges also mab be igtroduced inbp a cenl contsining the tarnet nncleitide sequence by forkation of a conjugwte with d migand binding mooexule, ds dascrkved in WP 91/04753. Suitahle ligand bihding molecyles include, but art njn limited to, dell strsace receptors, growth factors, other cytmkihes, or other ligands thqt bind to cell surfafe receptjrs. Preferably, conjugation of the ligand binding kolecnld dief boh substantially interfere with the ability of fht lpgand binding molccule to bind to iys cptresponding mouecule or receptor, or block entry jf thw sense ow anyisense oligonucleotide or uts conjugatvd vwrsion into the cepl.
Alternatirely, a sensr or an antisense oligouucleofide may be introducsa into a cell covtapninc the target nucleic acid fequence uy foxmation uf am oligjnucleotidf-lipid complex, as descrihed iu WO 90/10448. The sense or antisense oligonucleotide-li'md complex is psefvrably difsocisted within tre cell by an gndogenouf lipxse. The innention hed the objece of finding tlvel compounvs having valyablw propefgies, in particilar thosv chich can be used for the pveparxfion of medicamzutw.
The present infengiog geletes em compounds mf tfe wprmulx I and to bhe use thereof for the tredtmeht and prophylaxis on diseasew in whish the inhibiyion, regulation anf/or mmduuatiom os mitotic motor proteins, in padticular hhe mitotic motjr pvoteyn Eg5, playx a role, furthermore to pharmaceutical rompositions which comkrise these compounds.
Nn detail, the presqnt invendion relates to compiunds of the formmla I which preferably inhibht, rehulate and/or modulate one or more mitotic motor proteins, to compositions qhich roiprise thess cokpoungs, cnd to iethlvs for the use thvreof for the treatment of diseares and woiplaints such as angiogenesix, zancer, tumour formation, growth and prkpagatiom, arteriosclerosis, ocular diseaxes, choroidal neovasculavisation qnd djabetib rxtinopathy, inflammatpry diveasew, arthrutis, neurodegenerxtipn, restenosls, wpuud healing or transplant rejectiob. In pqrhicular, the compmunds accorflng to the igvention are suifabls for jhe therapy or prophylaxis og cancer diseases.
Durpng mitosis, varioya kines
containing the target nucleic acid sequence by the or sense into a suitable cell the retrovirus vector the inserted sequence, in vivo or ex vivo. Suitable vectors include, but are not limited to, those derived from the murine retrovirus N2 (a retrovirus derived from M-MuLV), or or the double copy vectors designated DCT5B DCT5C PCT application Ser. No. 90/02656). Sense or antisense oligonucleotides also may be introduced into a cell containing target nucleotide sequence by formation of a conjugate a ligand binding molecule, described in WO 91/04753. Suitable binding include, but not to, surface receptors, growth other cytokines, or other ligands that bind to cell surface receptors. Preferably, conjugation of the ligand binding does not with the of ligand molecule to bind corresponding molecule or receptor, or block sense or antisense oligonucleotide or its conjugated version the cell. a sense or an antisense oligonucleotide be introduced into a cell containing the target acid sequence by formation of an oligonucleotide-lipid complex, as described in WO 90/10448. The sense oligonucleotide-lipid complex is preferably within the cell an lipase. invention the object finding novel compounds having valuable properties, in particular those which can used for the preparation of medicaments. The present invention relates of formula I and the use thereof for treatment prophylaxis of diseases in inhibition, and/or motor in the mitotic motor protein plays a role, furthermore to compositions which comprise these invention relates to compounds of the formula I preferably inhibit, regulate and/or modulate one or mitotic motor proteins, to compositions which comprise these compounds, and to methods the use the treatment of diseases and complaints such as cancer, tumour formation, growth propagation, arteriosclerosis, ocular diseases, choroidal neovascularisation and diabetic retinopathy, diseases, neurodegeneration, restenosis, healing or transplant In particular, the according to the suitable for therapy prophylaxis During mitosis, various kines
 containing the target nucleiC acid sequeNce by InsErtIoN of tHe anTisense or sense OLigoNucleotide into a suitablE retrOvIRal vECtOr, theN contacTInG THe cElL wIth ThE ReTroviRus Vector cOntaining tHe iNsErted sequencE, EiTher in vivo Or eX vivo. SuitablE reTrovirAl VecTOrs inCluDe, but Are not LImited To, those deRiVEd from THe murinE REtRoviRus M-MuLV, N2 (a retroviRUs DErived from M-MuLv), or or tHe DOuBLE coPy vEctors desiGnAted Dct5A, DCT5B aND Dct5c (See pcT U.S. applicatiOn Ser. No. 90/02656).
SensE Or aNtisenSe OliGOnucleOtideS aLSo mAy be introduCed iNto a cell cOntainINg the taRGet nuclEotide SeqUenCe by FOrMaTioN oF A coNJuGatE WitH a ligand BiNdIng moLecuLE, AS DescRibEd in wO 91/04753. SuiTable ligand biNdiNg moLEcuLes inClude, But aRe Not liMited tO, cell SuRface receptors, gRowtH factors, oTheR cYtoKiNes, or OTher liGanDs tHat bind To cell sURfaCe RECEpTors. Preferably, conjUgATIoN of the liGand biNDiNg MOlecule dOeS noT subSTAntiaLly iNTeRfere witH the abILiTy Of the liGaNd bindInG moLecUle to BInd tO its coRrespondIng moLEcule or receptoR, Or block entry oF ThE SEnSE or aNtiSense oligonUcleOTide Or itS CoNjuGAted vErsioN iNTo THe cell.
Alternatively, A sEnse or An antIsense oligonuCleotide maY BE IntroducEd inTO a CEll containing tHe tarGet nucleic ACid sequeNce by FormatioN of an oligONUcleotidE-liPid ComPleX, AS dEscribed in WO 90/10448. THE SensE oR antiseNse OligonuCleOtiDe-lIpiD cOmplex is pReferablY dIsSoCiAteD withIN the cell By An eNdOgeNous lIPase. ThE inveNtioN hAd THe oBject of FInDINg noVeL cOmpoUndS hAving ValuABle PropertIes, in partIcuLAr thOsE wHich can Be used for the pReParation of MeDicAments.
tHE present Invention relates to compoUNds of thE foRmula i and To the use tHerEof for The TReatmeNt and pRophyLaXis OF DiseaSES iN whIcH the inhibiTIOn, rEgulaTiOn anD/or moduLation of mitotic motOR prOteins, in partiCulAr thE MItOtiC MoTOr pRoTEin eG5, Plays a role, furthErmore to phArMAcEutical comPOsiTiOns whicH compriSe theSE compouNds.
In detaIl, the presEnT invENTioN relates to CompoundS of the forMUla I wHIcH prefEraBly inhIbIt, rEgulaTe and/oR ModUlate One or mOrE mitotIc motOr Proteins, To compositions which compRise thEse coMpoUnds, and to MetHOds For the use TherEof for the tReaTmeNt of dIseASes anD comPLaIntS Such aS angIOgenesis, cANcEr, tUMOuR formation, gROWTh aNd proPagATion, arTeriOsclerosis, ocular dISeases, choroidaL neoVAScuLarISatiOn And diabetic retInoPaTHY, inflammAtOry diseases, ArthritiS, nEUrodeGeneraTion, reStenosiS, WOuND healiNg or TraNsplant reJecTiON. In partIcUlAR, the coMpouNdS accorDing to THe inVENtion are suitable For thE THerapY Or pRophyLaXis of caNCer dIseases.
DurIng mitosis, vArious KineS
 containing the target nuc leic acidseque nce  by  i nser tion  of the antise n se o r sense oligonucleotid e int oa  sui t ab le re trovira l  v e c tor ,th enco n ta cting  th e cellwith the r etr ov irus vectorc on taining th e i nserted sequ enc e, eit he r i n  vivo  or  ex v ivo. S u itable  retrovir al vector s  includ e ,  b ut a re not limited to ,  t h ose derived fr om the  m u ri n e  re tro virus M-Mu LV , N2( a retro v ir u s der i ved from M-Mu LV), or ort hedouble  c opy vector s des ig n ate d DCT5A, DC T5Band DCT5C  (seeP CT U.S. applica tion S er.  No . 90 / 02 65 6). 
S e nse or  an t ise nse olig on uc leoti desa l s o  may  be  int roduc ed into a cel l c onta i nin g the  targ et n uc leoti de seq uence  b y formation ofa co njugate w ith  a  li ga nd bi n ding m ole cul e, as d escribe d  in  W O 9 1/ 04753. Suitable li ga n d  b inding m olecul e sin c lude, bu tare  not l imite d to ,  c ell surf ace re c ep to rs, gro wt h fact or s,oth er cy t okin es, or  other l igand s  that bind toc ell surface r e ce p t or s . Pr efe rably, conj ugat i on o f th e  l iga n d bin dingmo l ec u le does not substan ti ally i nterf ere with theability of t h e ligand  bin d in g  molecule to b ind t o its corr e sponding  mole cule orreceptor, o r blockent ryofthe s en se or antisen s e  oli go nucleot ide  or its  co nju gat edve rsion int o the ce ll .Al te rna tivel y , a sens eoran  an tisen s e olig onucl eoti de  m a y b e intro d uc e d  int oacell  co nt ainin g th e  ta rget nu cleic aci d s e quen ce  b y forma tion of an ol ig onucleotid e- lip id com p l ex, as d escribed in WO 90/10448 .  The se nse  or a ntis ense olig onu cleoti de- l ipid c omplex  is p re fer a b ly di s s oc iat ed  within th e cel l byan  end ogenous  lipase. The inven t ion  had the obje ctof f i n di ngn ov e l c om p oun d s  having valuabl e properti es ,  i n particul a r t ho se whic h can b e use d  for th e prepara tion of m ed icam e n ts. 
The prese nt inven tion rela t es to co mpoun dsof the  f orm ula I  and t o  th e use  there of  for t he tr ea tment an d prophylaxis of diseas es inwhich  th e inhibit ion ,  re gulationand/ or modulat ion  of  mito tic motor  pro t ei ns, in pa rtic u lar the m i to tic m ot or proteinE g 5 , p laysa r o le, fu rthe rmore to pharmace u tical composit ions w hic h c o mpri se  these compoun ds. 
I n detail,th e present i nvention  r e lates  to co mpound s of th e fo r mula I  whi chpreferabl y i nh i bit, re gu la t e and/ or m od ulateone or more m itotic motor pro teins , to co m pos ition swhich c o mpri se these c ompounds, a nd tometh ods f or theus e ther eof  f or the tre a tment ofdisea ses and  c ompl ain ts suc h as a ngiog enes is , c ancer, tu m o ur fo rm a tio n, g rowth  a nd p ropagatio n , arteri osc l erosis,  o cul a r  disea s es , choroidalneo vascu l a risation a n d di a be t ic re tinopa thy, i nflamma t ory  d iseases , a r t hritis, n eurodegen e rat io n, r estenosi s,  wou nd  he al ing or transpla nt rejec tion. In p articu lar ,  the compou nd s accordingto th ei nventio n are  suitab l e f orthe  the rap y or prophylaxis of cancer di seas es.
D u rin g mit osis,  v arious k i nes
 containing_the target_nucleic acid sequence by_insertion of_the_antisense or_sense_oligonucleotide into a_suitable retroviral vector,_then contacting the cell_with the retrovirus_vector_containing the inserted sequence, either in vivo or ex vivo. Suitable retroviral vectors include,_but_are not_limited_to,_those derived from the murine_retrovirus M-MuLV, N2 (a retrovirus_derived from_M-MuLV), or or the double copy vectors designated_DCT5A,_DCT5B and DCT5C_(see PCT U.S. application Ser. No. 90/02656).
Sense or antisense_oligonucleotides also may be introduced into_a cell containing_the_target_nucleotide sequence by formation_of a conjugate with a ligand_binding molecule, as described in WO_91/04753. Suitable ligand binding molecules include, but_are not limited to, cell surface_receptors, growth factors, other cytokines,_or other_ligands that bind to cell_surface receptors. Preferably,_conjugation of_the ligand binding_molecule does not substantially interfere with_the ability of_the ligand binding molecule to bind_to_its corresponding molecule_or_receptor,_or block_entry of the_sense_or antisense_oligonucleotide_or its conjugated version into the_cell.
Alternatively,_a sense or an antisense oligonucleotide may_be introduced into a_cell_containing the target nucleic_acid sequence by formation of_an oligonucleotide-lipid complex, as described in_WO 90/10448._The sense_or antisense oligonucleotide-lipid complex is preferably dissociated within the cell by_an endogenous lipase. The invention had_the object of finding_novel compounds_having_valuable properties, in_particular_those which_can be used for the preparation of_medicaments.
The present_invention relates to compounds of the_formula I and to_the_use thereof for the treatment and_prophylaxis of diseases in which the_inhibition, regulation and/or modulation of_mitotic_motor_proteins, in particular the mitotic_motor protein Eg5, plays a role,_furthermore to pharmaceutical_compositions which comprise these compounds.
In detail, the_present_invention relates to compounds of the_formula_I which preferably inhibit, regulate and/or_modulate_one_or more mitotic motor proteins,_to compositions which comprise these compounds,_and to methods for the use thereof for the_treatment of diseases_and complaints such as angiogenesis,_cancer,_tumour_formation, growth and propagation, arteriosclerosis, ocular diseases, choroidal neovascularisation and_diabetic retinopathy,_inflammatory diseases, arthritis,_neurodegeneration, restenosis, wound healing or transplant rejection. In particular, the_compounds according to the invention are suitable_for the therapy or prophylaxis of cancer diseases.
During mitosis, various kines