公开(公告)号：EP2325180A1

公开(公告)日：2011-05-25

申请号：EP10175975.1

申请日：2008-09-30

申请人： F. Hoffmann-La Roche AG

发明人： Bartkovitz, David Joseph ,  Cai, Jianping ,  Chu, Xin-Jie ,  Li, Hongju ,  Lovey, Allen John ,  Vu, Binh Thanh ,  Zhao, Chunlin

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/454 ,  A61P35/00

CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D417/14 ,  C07D471/10

摘要： There are provided compounds of the formula

or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V 3 , V 2 , R 1 , R 2 , R 3 , R 4 and R 5 are as herein described, processes for obtaining said compounds and pharmaceutical preparations containing them. These compounds are useful as anticancer agents, in particular as agents in the treatment of solid tumors.

摘要翻译： 提供下式的化合物或其药学上可接受的盐，其中X，Y，Z，V 3，V 2，R 1，R 2，R 3，R 4和R 5如本文所述， 化合物和含有它们的药物制剂。 这些化合物可用作抗癌剂，特别是作为治疗实体瘤的药物。

公开(公告)号：EP0367124A1

公开(公告)日：1990-05-09

申请号：EP89119941.6

申请日：1989-10-27

申请人： F. HOFFMANN-LA ROCHE AG

发明人： Bartkovitz, David Joseph ,  Keith, Dennis Dalton ,  Mook, Robert ,  Wei, Chung Chen

IPC分类号： C07D499/84 ,  A61K31/43

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： The compounds of the general formula
in which R is hydrogen, a readily hydrolyzable ester group or a protecting group, R¹ is hydrogen and R² is hydrogen or an acyl group, or R¹ and R² taken together are the group
in which n is 5, 6 or 7,
X is fluoro, thiocyanato, azido or the group R 3a CO₂-
R 3a is C₂- to C₁₆-alkyl, aryl, a heterocycle, -(CH₂) m -aryl, -(CH₂) m -heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R³ is C₁- to C₁₆-alkyl, aryl, a heterocycle, -(CH₂) m -aryl, a -(CH₂) m -heterocycle, a heterocycle-lower alkenyl or aryl-lower alkenyl, R⁴ and R 4′ independently are hydrogen, lower alkyl, lower alkenyl or lower alkynyl, R a is hydrogen, halogen, amino, amino-lower alkyl, carboxy, carbamoyl, carboxy-lower alkyl, carbamoyl-lower alkyl or lower carbalkoxy-lower alkyl, m is from 1 to 4 and p is 3, 4 or 5, provided that X is other than fluoro when R is a protecting group, a hydrate, a readily hydrolyzable ester or salt thereof, or a hydrate of the ester or the salt, when R is hydrogen are useful as anti-bacterial agents for the prevention and treatment of bacterial infections in mammals, including humans.

摘要翻译： 其中R是氢，容易水解的酯基或保护基，R 1是氢和R 2是氢或酰基，或R 1和R 2一起形成通式的化合物是其中n是5,6的基团 或7，X是氟，氰硫基，叠氮基或基团R3aCO 2 -R 3a是C 2 -C 16烷基，芳基，杂环， - （CH 2）m - 芳基， - （CH 2）m-杂环，杂环 - 低级链烯基 或芳基低级链烯基，R 3是C 1 -C 16烷基，芳基，杂环， - （CH 2）m - 芳基， - （CH 2）m - 杂环，杂环低级链烯基或芳基低级链烯基，R 4和 低级烷基，低级烯基或低级炔基，Ra是氢，卤素，氨基，氨基 - 低级烷基，羧基，氨基甲酰基，羧基 - 低级烷基，氨基甲酰基 - 低级烷基或低级烷氧基 - 低级烷基，m是 1至4且p为3,4或5，条件是当R为保护基，水合物，易水解的酯或盐或e的水合物时，X不是氟 当R是氢时，该化合物或盐可用作预防和治疗哺乳动物包括人的细菌感染的抗菌剂。