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71. 发明专利

CZ220599A3 CAMPTOTHECINE ANALOGS, THEIR USE AS MEDICAMENTS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEREOF 未知
公开(公告)号：CZ220599A3
公开(公告)日：1999-09-15
申请号：CZ220599
申请日：1997-12-05
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , PLA RODAS FRANCESE , POMMIER JACQUES , ULIBARRI GERARD
IPC分类号： C07D491/22 , A61K31/435 , A61K31/4375 , A61K31/4709 , A61K31/4745 , A61P31/12 , A61P33/00 , A61P33/02 , A61P33/06 , A61P35/00 , A61P35/04 , C07D471/14 , C07D498/22
摘要： The invention concerns novel counterparts of camptothecin and particularly the products complying with the following formulae: -5-ethyl-9,10-difluoro-4,5-dihydro-5-hydroxy-12- (4-methyl piperidinomethyl) -1H-oxepino[3', 4':6,7]indolizino[1,2-b] quinolein-3,15(4H,13H)-dione; -5-ethyl-12-diethylaminomethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-1H-oxepino [3',4':6,7] indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; -5-ethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-12- (4-methyl piperidinomethyl) -1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral or parasiticide medicines.

72. 发明专利

NO992998A 未知
公开(公告)号：NO992998A
公开(公告)日：1999-08-18
申请号：NO992998
申请日：1999-06-18
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , RODAS FRANCESC PLA , POMMIER JACQUES , ULIBARRI GERARD
IPC分类号： C07D491/22 , A61K31/435 , A61K31/4375 , A61K31/4709 , A61K31/4745 , A61P31/12 , A61P33/00 , A61P33/02 , A61P33/06 , A61P35/00 , A61P35/04 , C07D471/14 , C07D498/22
CPC分类号： C07D471/14

73. 发明专利

NO992997L 未知
公开(公告)号：NO992997L
公开(公告)日：1999-08-18
申请号：NO992997
申请日：1999-06-18
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , HARNETT JERRY , ROLLAND ALAIN , LIBERATORE ANNE-MARIE , LANCO CHRISTOPHE
IPC分类号： A61K31/4375 , A61K31/5365 , A61P35/00 , A61P43/00 , C07D471/14 , C07D491/22 , C07D498/22 , A61K31/47
摘要： The invention concerns novel counterparts of camptothecin and in particular products complying with the following formulae: 8-ethyl-8,9-dihydro-8-hydroxy-1-benzyl-2H,10H,12H-[1,3]oxazino[5,6-f]oxepino[3',4':6,7]indolizino[1,2-b]quinolein-10,13(15H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoethoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their method of preparation, their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral and parasiticide medicines.

74. 发明专利

FR2757514B1 未知
公开(公告)号：FR2757514B1
公开(公告)日：1999-02-12
申请号：FR9615774
申请日：1996-12-20
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , PLA RODAS FRANCESC , POMMIER JACQUES , ULIBARRI GERARD
IPC分类号： C07D491/22 , A61K31/435 , A61K31/4375 , A61K31/4709 , A61K31/4745 , A61P31/12 , A61P33/00 , A61P33/02 , A61P33/06 , A61P35/00 , A61P35/04 , C07D471/14 , C07D498/22 , A61K31/47
摘要： The invention concerns novel counterparts of camptothecin and particularly the products complying with the following formulae: -5-ethyl-9,10-difluoro-4,5-dihydro-5-hydroxy-12- (4-methyl piperidinomethyl) -1H-oxepino[3', 4':6,7]indolizino[1,2-b] quinolein-3,15(4H,13H)-dione; -5-ethyl-12-diethylaminomethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-1H-oxepino [3',4':6,7] indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; -5-ethyl-9-fluoro-4,5-dihydro-5-hydroxy-10-methyl-12- (4-methyl piperidinomethyl) -1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral or parasiticide medicines.

75. 发明专利

FR2757515A1 New camptothecin oxepine analogue prodrug derivatives 未知
公开(公告)号：FR2757515A1
公开(公告)日：1998-06-26
申请号：FR9615775
申请日：1996-12-20
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , HARNETT JERRY , ROLLAND ALAIN , LIBERATORE ANNE MARIE
IPC分类号： A61K31/47 , A61P35/00 , C07D471/14 , C07D491/22
摘要： Camptothecin (CT) oxepine analogue derivatives (I) are new: (a) CT analogues in which the hydroxy-lactone ring of CT is replaced by a beta -hydroxy-lactone (or the corresponding beta -hydroxy-acid obtained by opening the lactone ring), where the compound contains an optionally substituted oxazine ring grafted onto positions 10 and 11 of the 'A' ring; (b) CT analogues in which the hydroxy-lactone ring of CT is replaced by a beta -hydroxy-lactone protected by a readily cleavable protecting group (or the corresponding protected beta -hydroxy-acid obtained by opening the lactone ring); and (c) compounds of formula (I'), in racemic and/or enantiomeric form, and their salts. R1 = alkyl, alkenyl, alkynyl, haloalkyl, alkoxyalkyl or alkylthioalkyl; R2-R4 = H, halo, haloalkyl, alkyl, alkenyl, CN, cyanoalkyl, NO2, nitroalkyl, amido, amidoalkyl, hydrazino, hydrazinoalkyl, azido, azidoalkyl, (CH2)mQ, O(CH2)mNR6R7, OCONR6R7, OCO(CH2)mCOOR6, (CH2)nN=X, OCON=X, Ar or Ar-alkyl; or R3+R4 = chain consisting or 3 or 4 members selected from CH, CH2, O, S, N and NR9; Q = NR6R7, OR6, COOR6, NR6COR8, COR8, OCOR8 or OCON=X; R5 = H, halo, haloalkyl, alkyl, alkoxy, alkoxyalkyl, alkylthioalkyl, cycloalkyl, cycloalkylalkyl, CN, cyanoalkyl, alkylsulphonylalkyl, hydroxyalkyl, NO2, (CH2)mQ', (CH2)2P(S)R12R13, (CH2)nN=X, OCON=X, Ar or Ar-alkyl; Q' = COR8, NR6COR8, NR6R7, N(Me)(CH2)nNR6R7, OCOR8, OCONR6R7, S(O)qR11, P(O)R12R13 or OCON=X; X = chain of O, S, CH2, CH, N, NR9 and COR10 units, completing a 4-7 membered heterocycle; R6, R7 = H, alkyl, hydroxyalkyl, alkylaminoalkyl, aminoalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkoxyalkyl, haloalkyl, Ar or Ar-alkyl; R8 = H, alkyl, hydroxyalkyl, NH2, alkylamino, alkylaminoalkyl, aminoalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkoxy, alkoxyalkyl, haloalkyl, Ar or Ar-alkyl; R9 = H, alkyl, haloalkyl or Ar; R10 = H, alkyl, haloalkyl, alkoxy or Ar; R11 = alkyl, aryl, (CH2)mOR14, (CH2)mSR14, (CH2)2NR14R15 or (CH2)mN=X; R12, R13 = alkyl, aryl, alkoxy, aryloxy or NH2; R14, R15 = H, alkyl or aryl; R16 = H or OR21; R17 = OR6 or NR6R7; or R16+R17 = O (completing a fused oxepino ring); R18, R19 = H, halo, alkyl, alkoxy or OH; R20 = H or halo; R21 = H, alkyl, CHO or CO(CH2)mMe; Rp = H or readily cleavable group, preferably CO-A-NR22R23; A = alkylene (not restricted to 'lower'), optionally substituted by OH (optionally esterified or salified), halo, COOH (optionally esterified or salified), NH2 or mono- or dialkylamino (not restricted to 'lower'); R22, R23 = H, alkyl, hydroxyalkyl, alkylaminoalkyl, aminoalkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkoxyalkyl, haloalkyl, Ar or Ar-alkyl; or NR22R23 = 5-7 membered ring (optionally substituted and optionally containing a further O, N or S heteroatom); m = 0-6; n = 1 or 2; q = 0-2; Ar = aryl (optionally substituted by 1-4 of alkyl, halo, NO2, NH2, alkylamino, haloalkyl, hydroxyalkyl, alkoxy and alkoxyalkyl); all alkyl, alkenyl and alkynyl moieties are 'lower', i.e. up to 6C; provided that if Rp = H, then R3+R4 form a 3- or 4-membered chain.

76. 发明专利

MX9710228A NUEVOS ANALOGOS DE CAMPTOTECINA, PROCEDIMIENTOS DE PREPARACION, SU APLICACION COMO MEDICINAS Y LAS COMPOSICIONES FARMACEUTICAS QUE LOS COMPRENDEN. 未知
公开(公告)号：MX9710228A
公开(公告)日：1998-03-31
申请号：MX9710228
申请日：1996-06-21
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , RODAS FRANCESCO PLA , POMMIER JACQUES , ULIBARRI GERARD
IPC分类号： A61K31/47 , A61K31/4745 , A61K31/475 , A61K31/496 , A61K31/5377 , A61P31/12 , A61P33/00 , A61P33/02 , A61P35/00 , A61P43/00 , C07D209/00 , C07D213/02 , C07D213/61 , C07D213/64 , C07D213/66 , C07D215/08 , C07D221/00 , C07D313/00 , C07D413/10 , C07D471/14 , C07D487/04 , C07D491/04 , C07D491/044 , C07D491/22 , C07D498/14
摘要： Se describe un análogo de camptotecina caracterizado en que la hidroxi lactona de la camptotecina es un beta-hidroxi lactona o el ácido de beta-hidroxi correspondiente, que resulta a partir de la abertura de la lactona, o un derivado del ácido de beta-hidroxi, o una sal farmacéuticamente aceptable del mismo. En particular, se describen los compuestos de las formulas (I) y (II). También se describen métodos para preparar los compuestos de las formulas (I) y (II), composiciones farmacéuticas que contienen los compuestos, y su uso, particularmente como inhibidores de topoisomerasa y fármacos antitumorales.

77. 发明专利

CA2275345C FORMES PRODROGUES ET ANALOGUES DE LA CAMPTOTHECINE, LEUR APPLICATION COMME MEDICAMENTS 未知
公开(公告)号：CA2275345C
公开(公告)日：2010-01-26
申请号：CA2275345
申请日：1997-12-05
申请人： SOD CONSEILS RECH APPLIC
发明人： BIGG DENNIS , LAVERGNE OLIVIER , HARNETT JERRY , ROLLAND ALAIN , LIBERATORE ANNE-MARIE , LANCO CHRISTOPHE
IPC分类号： C07D498/22 , A61K31/4375 , A61K31/47 , A61K31/5365 , A61P35/00 , A61P43/00 , C07D471/14 , C07D491/22
摘要： L'invention concerne de nouveaux analogues de la camptothécine et en particulier les produits répondant aux formules suivantes: 8-éthyl-8,9-dihydro-8-hydroxy-1-benzyl-2H, 10H, 12H-[1,3]oxazino[5,6-.function.]oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-10,13(15H)-dione; 5-éthyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoéthoxy)-1H-oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-3,15(4H,13H)-dione; 5-éthyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1H-oxépino[3',4':6,7]indolizino[1,2-b]quinoléine-3,15(4H,13H)-dione; leur procédé de préparation, leur application comme médicaments, les compositions pharmaceutiques les renfermant et leur utilisation pour la réalisation de médicaments antitumoraux, antiviraux ou antiparasitaires.

78. 发明专利

NO324973B1 未知
公开(公告)号：NO324973B1
公开(公告)日：2008-01-14
申请号：NO992997
申请日：1999-06-18
申请人： SOD CONSEILS RECH APPLIC
发明人： ROLLAND ALAIN , HARNETT JERRY , LIBERATORE ANNE-MARIE , LANCO CHRISTOPHE , BIGG DENNIS C H , LAVERGNE OLIVIER
IPC分类号： C07D498/22 , A61K31/4375 , A61K31/5365 , A61P35/00 , A61P43/00 , C07D471/14 , C07D491/22
摘要： The invention concerns novel counterparts of camptothecin and in particular products complying with the following formulae: 8-ethyl-8,9-dihydro-8-hydroxy-1-benzyl-2H,10H,12H-[1,3]oxazino[5,6-f]oxepino[3',4':6,7]indolizino[1,2-b]quinolein-10,13(15H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxoethoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione; 5-ethyl-9,10-difluoro-4,5-dihydro-5-(2-amino-1-oxopropoxy)-1H-oxepino[3',4':6,7]indolizino[1,2-b]quinolein-3,15(4H,13H)-dione. The invention also concerns their method of preparation, their application as medicines, the pharmaceutical compositions containing them and their use in producing tumoricidal, antiviral and parasiticide medicines.

79. 发明专利

NO324882B1 未知
公开(公告)号：NO324882B1
公开(公告)日：2007-12-27
申请号：NO20000995
申请日：2000-02-28
申请人： SOD CONSEILS RECH APPLIC
发明人： CAZAUX JEAN-BERNARD , BRETON CHRISTINE LE , MANGINOT ERIC , BIGG DENNIS C H , LAVERGNE OLIVIER
IPC分类号： C07D491/04 , C07D491/22 , A61K31/435 , A61K31/4353 , A61K31/4375 , A61P31/12 , A61P33/00 , A61P35/00 , C07D491/044
摘要： Two optically pure beta-hydroxy lactone camptothecin analogs (+)-5-ethyl-9,10-difluoro-5-hydroxy-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-3,15-dione (I) and (+)-9-chloro-5-ethyl-5-hydroxy-10-methyl-12-(4-methylpiperidinomethyl)-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-c)quinoline-2,15-dione (II), as well as one of its salts, (+)-1-(9-chloro-5-ethyl-5-hydroxy-10-methyl-3,15-dioxo-4,5,13,15-tetrahydro-1H,3H-oxepino(3',4':6,7)indolizino(1,2-b)quinoline-12-yl methyl)-4-methyl-hexahydropyridinium chloride (III) and intermediates (M) are new. Optically pure beta-hydroxy lactone camptothecin analogs of formulae (I) and (II), as well as salts of (II) of formulae (III) are new. Independent claims are also included for industrial intermediates of formula (M) and their preparation. R = 1-10C alkyl, especially ethyl.

80. 发明专利

DK1461326T3 未知
公开(公告)号：DK1461326T3
公开(公告)日：2007-12-10
申请号：DK02799849
申请日：2002-12-24
申请人： SOD CONSEILS RECH APPLIC
发明人： GALCERA CONTOUR MARIE-ODILE , LAVERGNE OLIVIER , BREZAK PANNETIER MARIE-CHRISTI , PREVOST GREGOIRE
IPC分类号： C07D277/64 , A61K31/423 , A61K31/428 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/5377 , A61P17/14 , A61P25/28 , A61P29/00 , A61P31/12 , A61P33/00 , A61P35/00 , A61P37/00 , A61P37/06 , A61P37/08 , A61P43/00 , C07D263/56 , C07D263/57 , C07D413/04 , C07D413/12 , C07D417/04 , C07D417/12 , C07D417/14 , C07D521/00
摘要： The invention concerns the use as cdc25 phosphatase inhibitors, in particular cdc25-C phosphatase, and CD45 phosphatase, of compounds of general formula (I), wherein: W represents O or S. In accordance with the invention, the compounds of general formula (I) can in particular be used for preparing a medicine for cancer treatment.

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