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公开(公告)号：EP1154767B1
公开(公告)日：2006-02-15
申请号：EP00903824.1
申请日：2000-02-15
发明人： DAVIS, Peter, David
IPC分类号： A61K31/195 , A61P35/00 , A61P17/00 , A61P27/02
CPC分类号： A61K31/223 , A61K31/27
摘要： Vascular damaging agents for use in treating diseases involving angiogenesis are provided which are compounds of formula: A-X-B, wherein A is a substituted cis-stilbene moiety, X a linker bond, atom or group and B is a moiety derived from an inhibitor of the formation or action of nitric oxide in mammalian systems specifically an inhibitor of nitric oxide synthase, and hydrates, pharmaceutically acceptable salts and prodrugs thereof. There are also provided compositions containing such compounds.
摘要翻译： 提供了用于治疗涉及血管生成的疾病的血管损伤剂，其为式AXB化合物，其中A为取代的顺式 - 二苯乙烯部分，X为连接键，原子或基团，B为衍生自地层的抑制剂的部分 或一氧化氮在哺乳动物系统中的作用，特别是一氧化氮合酶抑制剂，及其水合物，其药学上可接受的盐和前药。 还提供了含有这些化合物的组合物。
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公开(公告)号：EP1140745B1
公开(公告)日：2003-10-22
申请号：EP99962468.7
申请日：1999-12-24
IPC分类号： C07C13/547 , A61K31/165 , A61K31/22 , A61K31/19
CPC分类号： A61K31/165
摘要： The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R )- wherein R is hydrogen, hydroxy, C1-7alkoxy, -OR or -NR R (wherein R is a group -Y R (wherein Y is a direct bond, -C(O)-, -C(S)-, -S-, -C(O)O, -C(O)NR -, -SO2- or -SO2NR - (wherein R and R , which may be the same or different, each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl) and R is as defined herein, and R includes hydrogen; R , R and R are as defined herein and are preferably methyl; R , R and R are as defined herein with the proviso that R is not hydroxy, alkoxy, substituted alkoxy, -OPO3H2, -O-C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）化合物的用途：其中X是-C（O） - ，-C（S） - ，-C = NOH或-CH（R 7） - ，其中R 7 其中Y 1是氢，羟基，C 1-7烷氧基，-OR 8或-NR 8 R 9（其中R 8是基团-Y 1 R 10（其中Y 1是 -C（O） - ，-C（S） - ， - S - ， - C（O）O，-C（O）NR 11 - ， - SO 2 - 或-SO 2 NR 12 - （其中R 11和R 12可以相同或不同，各自独立地表示氢，C 1-3烷基或C 1-3烷氧基C 2-3烷基）且R 10如本文所定义，并且R 9， 包括氢; R 1，R 2和R 3如本文所定义且优选为甲基; R 4，R 5和R 6如本文所定义， R5不是羟基，烷氧基，取代的烷氧基，-OPO3H2，-OC1-7烷酰基或苄氧基;以及它们的盐在制备用于在温血动物例如人类中产生血管破坏作用的药物中的用途 本发明还涉及式（I）化合物，含有它们的药物组合物， 它们的制备方法以及使用这些化合物在温血动物例如人体中产生血管破坏作用的治疗方法。 式（I）化合物及其药学上可接受的盐可用于治疗许多疾病状态，包括癌症和类风湿性关节炎。
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3.发明公开
公开(公告)号：EP1161235A1
公开(公告)日：2001-12-12
申请号：EP00903832.4
申请日：2000-02-15
发明人： DAVIS, Peter David
IPC分类号： A61K31/198 , A61K31/44 , A61K31/66 , A61P35/00 , A61P17/06 , A61P27/00 , A61P9/10 , A61P19/02 , A61K45/06
CPC分类号： A61K45/06 , A61K31/155 , A61K31/165 , A61K31/17 , A61K31/195 , A61K31/35 , A61K31/065 , A61K2300/00
摘要： Compositions for the inhibition of the formation of new vasculature by angiogenesis are provided comprising the combination of a vasculature damaging agent and an inhibitor of the formation or action of nitric oxide in mammalian systems. There are also provided the use of said combinations in medicaments and kits of said compounds and treatment employing said materials.
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4.发明授权USE OF COLCHINOL DERIVATIVES AS VASCULAR DAMAGING AGENTS 失效VERWENDUNG VON COLCHINOLDERIVATE ZURGEFÄSSSCHÄDIGUNG
公开(公告)号：EP1001785B1
公开(公告)日：2006-08-02
申请号：EP98932374.6
申请日：1998-07-06
发明人： DOUGHERTY, Graeme
IPC分类号： A61K31/66 , A61K31/165 , A61K31/27 , C07C13/547
CPC分类号： A61K31/661 , A61K31/135 , A61K31/165 , A61K31/17 , A61K31/18 , A61K31/196 , A61K31/216 , A61K31/27 , C07C217/74 , C07C233/23 , C07C271/24 , C07C275/28 , C07C307/08 , C07C311/07 , C07C2601/08 , C07C2603/32 , C07F9/12
摘要： Colchinol derivatives of formula (I) wherein R1, R2, R3 and R6 are each independently H, optionally substituted alkyl, cycloalkyl, alkenyl, alkynyl, aralkyl, alkanoyl, PO3H2; X is carbonyl (CO), thiocarbonyl (CS), methylene (CH2) or a group CHR4; R4 is OH, O-alkyl or NR8R9; R5 and R7 are each independently H, alkyl, halogen, hydroxy, alkoxy, nitro or amino; R8 is H, optionally substituted alkyl, cycloalkyl, alkanoyl, thioalkanoyl, aryl, heteroaryl, arylcarbonyl, heteroarylcarbonyl, alkoxycarbonyl, aryloxycarbonyl, aminocarbonyl, alkylaminocarbonyl, dialkylaminocarbonyl, arylaminocarbonyl, alkylsulfonyl, arylsulfonyl, aminosulfonyl, alkylaminosulfonyl, dialkylaminosulfonyl or arylaminosulfonyl; and R9 is H, alkyl or cycloalkyl and the pharmaceutically acceptable salts, solvates, and hydrates thereof have been found to be useful for treatment of diseases involving angiogenesis. Some of these compounds are novel. Particularly preferred are those compounds in which R6 is PO3H2.
摘要翻译： 甲基呋喃醇的衍生物R1，R2，R3和R6各自独立地为H，任选取代的烷基，环烷基，烯基，炔基，芳烷基，烷酰基，PO 3 H 2; X是羰基（CO），硫代羰基（CS），亚甲基（CH 2）或基团CHR 4; R4是OH，O-烷基或NR8R9; R 5和R 7各自独立地为H，烷基，卤素，羟基，烷氧基，硝基或氨基; R 8是H，任选取代的烷基，环烷基，烷酰基，硫代烷酰基，芳基，杂芳基，芳基羰基，杂芳基羰基，烷氧基羰基，芳氧基羰基，氨基羰基，烷基氨基羰基，二烷基氨基羰基，芳基氨基羰基，烷基磺酰基，芳基磺酰基，氨基磺酰基，烷基氨基磺酰基，二烷基氨基磺酰基或芳基氨基磺酰基; 且R 9为H，烷基或环烷基; 已经发现其药学上可接受的盐，溶剂合物和水合物可用于治疗涉及血管生成的疾病。 这些化合物中的一些是新的。 特别优选的是其中R 6是PO 3 H 2的那些化合物。
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公开(公告)号：EP1154767B9
公开(公告)日：2006-06-28
申请号：EP00903824.1
申请日：2000-02-15
发明人： DAVIS, Peter, David
IPC分类号： A61K31/195 , A61P35/00 , A61P17/00 , A61P27/02
CPC分类号： A61K31/223 , A61K31/27
摘要： Vascular damaging agents for use in treating diseases involving angiogenesis are provided which are compounds of formula: A-X-B, wherein A is a substituted cis-stilbene moiety, X a linker bond, atom or group and B is a moiety derived from an inhibitor of the formation or action of nitric oxide in mammalian systems specifically an inhibitor of nitric oxide synthase, and hydrates, pharmaceutically acceptable salts and prodrugs thereof. There are also provided compositions containing such compounds.
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公开(公告)号：EP1272199B1
公开(公告)日：2005-01-19
申请号：EP01915490.5
申请日：2001-03-27
IPC分类号： A61K31/661 , A61K31/282 , A61K31/337 , A61K41/00 , A61P35/00
CPC分类号： A61K31/661 , A61K31/66 , A61K33/24 , A61K41/0038 , A61K31/555 , A61K31/335 , A61K2300/00
摘要： The invention relates to a method for the production of a vascular damaging effect in a warm-blooded animal such as a human, which comprises administering to said animal an effective amount of ZD6126 or a pharmaceutically acceptable salt thereof, before, after or simultaneously with an effective amount of one of the following therapies: i) ionising radiation; ii) a platinum anti-tumour agent; and iii) a taxane. The invention also relates to the use of ZD6126 and one of the above therapies in the manufacture of a medicament for use in the production of a vascular damaging effect in a warm-blooded animal such as a human and to pharmaceutical compositions and kits each comprising ZD6126 and one of a platinum anti-tumour agent and a taxane.
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公开(公告)号：EP1154767A1
公开(公告)日：2001-11-21
申请号：EP00903824.1
申请日：2000-02-15
发明人： DAVIS, Peter, David
IPC分类号： A61K31/195 , A61P35/00 , A61P17/00 , A61P27/02
CPC分类号： A61K31/223 , A61K31/27
摘要： Vascular damaging agents for use in treating diseases involving angiogenesis are provided which are compounds of formula: A-X-B, wherein A is a substituted cis-stilbene moiety, X a linker bond, atom or group and B is a moiety derived from an inhibitor of the formation or action of nitric oxide in mammalian systems specifically an inhibitor of nitric oxide synthase, and hydrates, pharmaceutically acceptable salts and prodrugs thereof. There are also provided compositions containing such compounds.
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8.发明公开VASCULAR DAMAGING AGENTS FOR ADMINISTRATION AS AN INTRAVENOUS INFUSION 审中-公开GEFÄSSCHÄDIGENDE手段给药的静脉内输注
公开(公告)号：EP1758593A1
公开(公告)日：2007-03-07
申请号：EP05742587.8
申请日：2005-05-11
IPC分类号： A61K31/661 , A61P35/00
CPC分类号： A61K31/661
摘要： The invention concerns the use of a vascular damaging agent or a pharmaceutically acceptable salt thereof in the manufacture of a medicament for administration as an intravenous infusion to a warm-blooded animal such as a human over a time period of more than 1 hour for use in the production of a vascular damaging effect in said warm-blooded animal. The invention also concerns kits adapted for intravenous infusion of a vascular damaging agent over a time period of more than 1 hour and to methods for providing a vascular damaging effect in a warm-blooded comprising administering a vascular damaging agent to the warm-blooded animal over a time period of more than 1 hour.
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公开(公告)号：EP1140745A1
公开(公告)日：2001-10-10
申请号：EP99962468.7
申请日：1999-12-24
IPC分类号： C07C13/547 , A61K31/165 , A61K31/22 , A61K31/19
CPC分类号： A61K31/165
摘要： The invention relates to the use of compounds of formula (I): wherein X is -C(O)-, -C(S)-, -C=NOH, or -CH(R7)- wherein R7 is hydrogen, hydroxy, C¿1-7?alkoxy, -OR?8 or -NR8R9¿ (wherein R8 is a group -Y1R10 (wherein Y1 is a direct bond, -C(O)-, -C(S)-, -S-, -C(O)O, -C(O)NR11-, -SO¿2?- or -SO2NR?12¿- (wherein R?11 and R12¿, which may be the same or different, each independently represents hydrogen, C¿1-3?alkyl or C1-3alkoxyC2-3alkyl) and R?10¿ is as defined herein, and R9 includes hydrogen; R?1, R2 and R3¿ are as defined herein and are preferably methyl; R?4, R5 and R6¿ are as defined herein with the proviso that R5 is not hydroxy, alkoxy, substituted alkoxy, -OPO¿3?H2, -O-C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.
摘要翻译： 本发明涉及式（I）化合物的用途：其中X是-C（O） - ，-C（S） - ，-C = NOH或-CH（R 7） - ，其中R 7是氢，羟基， （其中Y1是直接键，-C（O） - ， - C（S） - ， - S - ， - -C（O）O，-C（O）NR 11 - ， - SO 2 2 - 或-SO 2 NR 12 R 12 - （其中R 11和R 12可以相同或不同，各自独立地代表氢， C 1-3 - 烷基或C 1-3烷氧基C 2-3烷基）和R 10'如本文所定义，且R 9包括氢; R 14，R 2和R 3如本文所定义且优选为甲基; R 14， R 5和R 6如本文所定义，条件是R 5不是羟基，烷氧基，取代的烷氧基，-OPO 3 H 2，-O-C 1-7烷酰基或苄氧基;及其盐在制备药物中的用途， 本发明还涉及式（I）化合物，含有它们的药物组合物，它们的方法 制备方法以及使用该化合物治疗温血动物例如人的血管损伤作用的方法。 式（I）化合物及其药学上可接受的盐可用于治疗许多疾病状态，包括癌症和类风湿性关节炎。
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公开(公告)号：EP1140078B1
公开(公告)日：2007-08-29
申请号：EP00900294.0
申请日：2000-01-14
发明人： DAVIS, Peter David
IPC分类号： A61K31/4184 , A61P9/00 , C07D235/32 , C07F9/6506
CPC分类号： C07F9/65068 , A61K31/4184 , A61K31/675 , C07D235/32
摘要： 5(6)-substituted benzimidazole-2-carbamates of formula (I) wherein Alk is an alkyl group, X is oxygen, sulphur, sulphinyl, sulphonyl, carbonyl (CO), thiocarbonyl (CS), sulphonyloxy, NH, iminomethylene (C=NH), N-hydroxyiminomethylene, N-alkoxyiminomethylene, dialkoxymethylene, 1,3-dioxolan-2yl, 1,1-ethenyl, a group CHR3 or a bond, R1 is hydrogen, alkylaminocarbonyl or alkoxycarbonyl, R2 is hydrogen, alkoxycarbonyl, cyanomethyl, cyanoethyl, alkoxymethyl or acetoxymethyl. R3 is hydrogen, hydroxy, alkoxy or amino, A is an optionally substituted aromatic, optionally substituted heteroaromatic, optionally substituted heterocycloalkyl, optionally substituted alkyl or optionally substituted cycloalkyl group and the pharmaceutically acceptable salt, solvates and hydrates thereof, can be used in the preparation of medicaments for the treatment of diseases involving neovascularisation.
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