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）。

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。

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。

公开(公告)号：US5639884A

公开(公告)日：1997-06-17

申请号：US400113

申请日：1995-03-06

申请人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria Gabriella Brasca ,  Sergio Penco

发明人： Franco Buzzetti ,  Silvia Fustinoni ,  Maria Gabriella Brasca ,  Sergio Penco

IPC分类号： A61K31/425 ,  A61K31/428 ,  A61K31/47 ,  A61K31/472 ,  A61P35/00 ,  A61P43/00 ,  C07D217/24 ,  C07D275/06 ,  C07D401/06 ,  C07D417/06 ,  C12N9/99

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 1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; 其中当（Ar）R 1 R 2基团同时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，它们可用作抗增殖剂。