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1. 发明授权

US5547941A Cyclic dinucleoside diphosphorothioates, related compounds and pharmaceutical compositions 失效
标题翻译：环状二核苷二磷酸硫酸酯，相关化合物和药物组合物
公开(公告)号：US5547941A
公开(公告)日：1996-08-20
申请号：US354888
申请日：1994-12-09
申请人： Carlo Battistini , Silvia Fustinoni , Maria G. Brasca , Domenico Ungheri
发明人： Carlo Battistini , Silvia Fustinoni , Maria G. Brasca , Domenico Ungheri
IPC分类号： A61K31/70 , A61P31/12 , A61P31/18 , C07H19/10 , C07H19/20 , C07H21/00 , C07H21/04 , C07H19/213 , C07H21/02
CPC分类号： C07H19/10 , C07H19/20
摘要： There are provided compounds of formula (I) ##STR1## wherein each group B is, independently, a naturally occurring or modified heterocyclic base linked through a nitrogen or a carbon atom of the ring to the sugar moiety;each group X is a, independently, hydrogen, fluorine, hydroxy, or a C.sub.1 -C.sub.6 alkoxy group;each group Y is, independently, hydrogen, sulphidryl or hydroxy; and the pharmaceutically acceptable salts thereof.A process for their preparation and pharmaceutical compositions comprising them are also described. The compounds of this invention can be useful as antivirals, particularly as anti-HIV (Human Immunodeficiency Virus) agents, namely as drugs to be used against AIDS (Acquired Immunodeficiency Syndrome) therapeutically and/or prophylatically.
摘要翻译：提供式（I）化合物（I）其中每个基团B独立地是通过环的氮或碳原子与糖部分连接的天然存在或修饰的杂环碱基; 每个基团X独立地是氢，氟，羟基或C 1 -C 6烷氧基; 每个基团Y独立地是氢，硫代或羟基; 及其药学上可接受的盐。还描述了其制备方法和包含它们的药物组合物。本发明的化合物可用作抗病毒剂，特别是作为抗HIV（人类免疫缺陷病毒）试剂，即用于治疗和/或预防用于抗艾滋病（获得性免疫缺陷综合征）的药物）。

2. 发明授权

US5587385A Arylidene-heterocyclic derivatives and process for their preparation 失效
标题翻译：亚芳基杂环衍生物及其制备方法
公开(公告)号：US5587385A
公开(公告)日：1996-12-24
申请号：US452288
申请日：1995-05-26
申请人： Franco Buzzetti , Silvia Fustinoni , Maria G. Brasca , Sergio Penco
发明人： Franco Buzzetti , Silvia Fustinoni , Maria G. Brasca , Sergio Penco
IPC分类号： C07D217/24 , C07D275/06 , C07D401/06 , C07D417/06 , A61K31/47 , A61K31/475 , C07D401/08
CPC分类号： C07D275/06 , C07D217/24 , C07D401/06 , C07D417/06
摘要： The invention relates to compounds of formula ##STR1## wherein Ar is mono- or bicyclic ring system chosen from benzene, naphthalene, tetrahydronaphthalene, quinoline and indole;Het is ##STR2## R is hydrogen, halogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.1 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 acyloxy, cyano, nitro, amino or --COOR.sub.3 in which R.sub.3 is as defined above;R.sub.2 is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.6 alkyl; and the pharmaceutically acceptable salts thereof, and wherein when at the same time the (Ar) R.sub.1 R.sub.2 group represents unsubstituted phenyl or 4-chloro-, 4-cyano-, 4-amino- or 3,4-dimethoxy-phenyl and Het is a 4-homophthalimide group, then R is other than hydrogen, which are useful as anti-proliferative agents.
摘要翻译：本发明涉及式（I）的化合物，其中Ar是选自苯，萘，四氢萘，喹啉和吲哚的单环或双环体系; Het是R 3是氢或C 1 -C 6烷基的氢，卤素，羟基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3; R 1是氢，羟基，C 1 -C 6烷基，C 1 -C 6烷氧基，C 2 -C 6酰氧基，氰基，硝基，氨基或-COOR 3，其中R 3如上所定义; R2是氢，卤素，羟基或C1-C6烷基; 并且其中当同时（Ar）R 1 R 2基团表示未取代的苯基或4-氯 - ，4-氰基 - ，4-氨基 - 或3,4-二甲氧基 - 苯基且Het为 4-高邻苯二甲酰亚胺基，则R不是氢，其可用作抗增殖剂。

3. 发明授权

US5576330A Biologically active 3-substituted oxindole derivatives useful as anti-angiogenic agents 失效
标题翻译：用作抗血管生成剂的生物活性3-取代羟吲哚衍生物
公开(公告)号：US5576330A
公开(公告)日：1996-11-19
申请号：US354215
申请日：1994-12-12
申请人： Franco Buzzetti , Antonio Longo , Maria G. Brasca , Fabrizio Orzi , Angelo Crugnola , Dario Ballinari , Mariangela Mariani
发明人： Franco Buzzetti , Antonio Longo , Maria G. Brasca , Fabrizio Orzi , Angelo Crugnola , Dario Ballinari , Mariangela Mariani
IPC分类号： C07D401/06 , A61K31/40 , A61K31/403 , A61K31/404 , A61K31/47 , A61K31/475 , A61K31/505 , A61K31/675 , A61K31/70 , A61K38/04 , A61P27/02 , A61P29/00 , A61P35/00 , C07D209/34 , A61K31/015
CPC分类号： A61K31/70 , A61K31/40 , A61K31/47 , A61K31/475 , A61K31/505 , A61K31/675 , A61K38/04 , Y10S514/825 , Y10S514/863 , Y10S514/866 , Y10S514/886 , Y10S514/908
摘要： The new use of a compound of formula (I) ##STR1## wherein Y is a bicyclic ring selected from naphthalene, tetralin, quinoline, isoquinoline and indole;n is zero or an integer of 1 to 3;R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or C.sub.2 -C.sub.6 alkanoyl;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro, or NHR, wherein R is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl;R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.2 -C.sub.6 alkanoyloxy, carboxy, nitro or NHR, wherein R is as defined above;R.sub.5 is hydrogen, C.sub.1 -C.sub.6 alkyl or halogen; or a pharmaceutically acceptable salt thereof;and wherein when Y is naphthalene then n is zero or an integer of 1 to 3, whereas when Y is tetralin, quinoline, isoquinoline or indole then n is zero, 1 or 2; and wherein when the bicyclic ring Y is naphthalene, quinoline, isoquinoline or indole, then each of the substituents OR.sub.1, R.sub.2 and oxindolylidene may be independently on either of the aryl or heteroaryl moieties of said bicyclic ring, whereas only the benzene moiety is substituted when Y is tetralin;and wherein when Y is naphthalene, tetralin, quinoline or isoquinoline, then R.sub.2 is hydrogen, halogen, cyano or C.sub.1 -C.sub.6 alkyl and R.sub.3, R.sub.4 and R.sub.5 are hydrogen; whereas when Y is indole, then R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.6 alkyl, cyano, carboxy, nitro or --NHR, in which R is as defined above, R.sub.3 is hydrogen or C.sub.1 -C.sub.6 alkyl, R.sub.4 is hydrogen, hydroxy, C.sub.1 -C.sub.6 alkoxy, C.sub.1 -C.sub.6 alkanoyloxy, carboxy, nitro or --NHR, wherein R is as defined above, and R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.6 alkyl;as anti-angiogenic agent is disclosed.
摘要翻译：式（I）化合物（I）的新用途其中Y是选自萘，四氢化萘，喹啉，异喹啉和吲哚的双环; n为0或1〜3的整数， R1是氢，C1-C6烷基或C2-C6烷酰基; R2是氢，卤素，C1-C6烷基，氰基，羧基，硝基或NHR，其中R是氢或C1-C6烷基; R3是氢或C1-C6烷基; R 4是氢，羟基，C 1 -C 6烷氧基，C 2 -C 6烷酰氧基，羧基，硝基或NHR，其中R如上定义; R5是氢，C1-C6烷基或卤素; 或其药学上可接受的盐; 当Y为萘时，n为0或1〜3的整数，Y为四氢化萘，喹啉，异喹啉或吲哚时，n为0,1或2。并且其中当双环Y为萘，喹啉，异喹啉或吲哚时，则所述取代基OR 1，R 2和羟吲哚基中的每一个可以独立地表示在所述二环的芳基或杂芳基部分上，而只有苯部分被取代， Y是四氢化萘; 其中当Y为萘，四氢化萘，喹啉或异喹啉时，则R2为氢，卤素，氰基或C1-C6烷基，R3，R4和R5为氢; 而当Y为吲哚时，R 2为氢，卤素，C 1 -C 6烷基，氰基，羧基，硝基或-NHR，其中R如上定义，R 3为氢或C 1 -C 6烷基，R 4为氢，羟基， C 1 -C 6烷氧基，C 1 -C 6烷酰氧基，羧基，硝基或-NHR，其中R如上所定义，R 5是氢，卤素或C 1 -C 6烷基; 作为抗血管生成剂被公开。

4. 发明授权

US5436235A 3-aryl-glycidic ester derivatives 失效
标题翻译： 3-芳基 - 缩水甘油酯衍生物
公开(公告)号：US5436235A
公开(公告)日：1995-07-25
申请号：US16980
申请日：1993-02-12
申请人： Franco Buzzetti , Maria G. Brasca , Silvia Fustinoni , Sergio Penco
发明人： Franco Buzzetti , Maria G. Brasca , Silvia Fustinoni , Sergio Penco
IPC分类号： A61K31/335 , A61K31/336 , A61K31/40 , A61K31/47 , A61P9/00 , A61P35/00 , A61P43/00 , C07D303/48 , C07D405/04 , C07D27/56
CPC分类号： C07D405/04 , C07D303/48
摘要： The present invention relates to 3-aryl-oxirane derivatives of the formula ##STR1## wherein Ar is 4'-quinoline or 5'-quinoline; each of R and R.sub.1 independently is hydrogen or C.sub.1 -C.sub.6 alkoxy; one of X and Y is hydrogen, cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, and the other of X and Y is cyano, --COOR.sub.2 or --CONR.sub.3 R.sub.4, wherein R.sub.2 is C.sub.1 -C.sub.6 alkyl and each of R.sub.3 and R.sub.4 independently is hydrogen or C.sub.1 -C.sub.6 alkyl, and pharmaceutically acceptable salts thereof, which are useful in therapy as tyrosine kinase inhibitors, in particular as anti-proliferative agents, typically as anti-cancer agents, in the treatment of psoriasis and in inhibiting the development of atheromatous plaque.
摘要翻译：本发明涉及式为“IMAGE”的3-芳基 - 环氧乙烷衍生物，其中Ar为4'-喹啉或5'-喹啉; R和R 1各自独立地是氢或C 1 -C 6烷氧基; X和Y中的一个是氢，氰基，-COOR 2或-CONR 3 R 4，X和Y中的另一个是氰基，-COOR 2或-CONR 3 R 4，其中R 2是C 1 -C 6烷基，R 3和R 4各自独立地是氢或C 1 -C6烷基和其药学上可接受的盐，其可用于治疗作为酪氨酸激酶抑制剂，特别是作为抗增殖剂（通常作为抗癌剂）用于治疗牛皮癣和抑制动脉粥样硬化斑块发展。

5. 发明授权

US4973674A Chiral synthesis of anthracyclines from substituted anthraquinones 失效
标题翻译：从取代的蒽醌手性合成蒽环类
公开(公告)号：US4973674A
公开(公告)日：1990-11-27
申请号：US179989
申请日：1988-04-11
申请人： Maria G. Brasca , Sergio Penco
发明人： Maria G. Brasca , Sergio Penco
IPC分类号： A61K31/70 , A61K31/7028 , A61K31/7034 , A61K31/704 , A61P31/04 , C07H15/10 , C07H15/252 , C07H23/00 , C07H15/244
CPC分类号： C07H15/10 , C07H15/252 , C07H23/00
摘要： Anthracycline glycosides of formula (I): ##STR1## wherein R.sub.1 and R.sub.2 are independently selected from hydrogen, methyl, ethyl or methoxy and pharmaceutically acceptable acid addition salts thereof, which are useful in treatment of human cancer, are prepared by a stereospecific condensation of a derivative of daunosamine of general formula (II): ##STR2## wherein R.sub.3 is an alkyl, perfluoroalkyl or aryl group and R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are independently selected from alkyl, aryl or aralkyl having up to ten carbon atoms, with a quinone quinizarine epoxide of general formula (III) ##STR3## and conversion of the product obtained to the anthracycline glycoside of formula (I) or salt thereof.

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