公开(公告)号：EP0311948A3

公开(公告)日：1990-05-09

申请号：EP88116770.4

申请日：1988-10-10

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Kuroda, Tsuyoshi ,  Uemori, Satoru ,  Moriguchi, Akihiko ,  Ikeda, Yoshifumi

IPC分类号： C07D413/04 ,  A61K31/535

CPC分类号： C07D413/04

摘要： A quinolonecarboxylic acid compound of the formula I
wherein R¹ is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a substituted phenyl group by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R² is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxy­carbonyl group, R³ is a hydrogen atom, an alkyl group or an aralkyl group, or R² and R³ together with the adjacent nitrogen atom form heterocyclic ring, R⁴ is a hydrogen atom or an alkyl group, R⁵ is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is integer of 1 to 3, and a salt thereof, and pharmaceutical use thereof. Said compounds exhibit antibacterial activities and are useful for the treatment of various infectious diseases.

公开(公告)号：EP0212260A1

公开(公告)日：1987-03-04

申请号：EP86109786.3

申请日：1986-07-16

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Uemori, Satoru ,  Kuroda, Tsuyoshi ,  Moriguchi, Akihiko

IPC分类号： C07D499/68 ,  C07D499/14

CPC分类号： C07D499/00

摘要： A process for preparing a stable Bacampicillin 6β-halopenicillanate which comprises reacting Bacampicillin hydrochloride with an alkali metal salt or an amine salt of 6β-halopenicillanic acid under heating. The salt produced by the method of the present invention is remarkably stable against coloration and thermal decomposition in the long term storage.

摘要翻译： 制备稳定的卡泊菌素6β-卤代青霉烷酸的方法，其包括在加热下使卡泊舒林盐酸盐与6β-卤代青霉烷酸的碱金属盐或胺盐反应。 通过本发明的方法生产的盐对于长期储存中的着色和热分解是非常稳定的。

公开(公告)号：EP0311948A2

公开(公告)日：1989-04-19

申请号：EP88116770.4

申请日：1988-10-10

申请人： Yoshitomi Pharmaceutical Industries, Ltd.

发明人： Araki, Kazuhiko ,  Kuroda, Tsuyoshi ,  Uemori, Satoru ,  Moriguchi, Akihiko ,  Ikeda, Yoshifumi

IPC分类号： C07D413/04 ,  A61K31/535

CPC分类号： C07D413/04

摘要： A quinolonecarboxylic acid compound of the formula I
wherein R¹ is an alkyl group, a cycloalkyl group, a haloalkyl group, an alkenyl group, mono- or di-alkylamino groups, a phenyl group or a substituted phenyl group by one to three substituents selected from the group consisting of a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group or an amino group, R² is a hydrogen atom, an alkyl group, a cycloalkyl group, an acyl group or an alkoxy­carbonyl group, R³ is a hydrogen atom, an alkyl group or an aralkyl group, or R² and R³ together with the adjacent nitrogen atom form heterocyclic ring, R⁴ is a hydrogen atom or an alkyl group, R⁵ is a hydrogen atom, an alkyl group, an aralkyl group or an ester residue which is readily hydrolyzable in vivo, X is a hydrogen atom, a halogen atom or an alkyl group, n is integer of 1 to 3, and a salt thereof, and pharmaceutical use thereof.
Said compounds exhibit antibacterial activities and are useful for the treatment of various infectious diseases.

摘要翻译： 其中R 1为烷基，环烷基，卤代烷基，链烯基，单 - 或二 - 烷基氨基，苯基或取代的苯基的喹啉酮羧酸化合物，其中R 1为 一至三个选自卤素原子，烷基，烷氧基，羟基，硝基或氨基的取代基，R 2是氢原子，烷基，环烷基 ，酰基或烷氧基羰基，R 3是氢原子，烷基或芳烷基，或R 2和R 3与相邻的氮原子一起形成杂环，R 4， 是氢原子或烷基，R 5是氢原子，烷基，芳烷基或在体内容易水解的酯残基，X是氢原子，卤素原子或烷基， n为1〜3的整数，及其盐及其药物用途。 所述化合物表现出抗菌活性，可用于治疗各种感染性疾病。