发明公开
- 专利标题: Novel antimicrobial dithiocarbamoyl quinolones
- 专利标题(中): Antimikrobielle二硫代氨基甲酰喹诺酮。
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申请号: EP89870161.0申请日: 1989-10-24
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公开(公告)号: EP0366643A2公开(公告)日: 1990-05-02
- 发明人: Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
- 申请人: Norwich Eaton Pharmaceuticals, Inc.
- 申请人地址: 17 Eaton Avenue Norwich New York 13815 US
- 专利权人: Norwich Eaton Pharmaceuticals, Inc.
- 当前专利权人: Norwich Eaton Pharmaceuticals, Inc.
- 当前专利权人地址: 17 Eaton Avenue Norwich New York 13815 US
- 代理机构: Canonici, Jean-Jacques
- 优先权: US261948 19881024; US418029 19891012
- 主分类号: C07D215/56
- IPC分类号: C07D215/56 ; C07D471/04 ; C07D498/06 ; C07D513/04 ; C07D519/00 ; C07D487/08 ; C07D401/04 ; C07D498/04 ; C07D471/06 ; C07D513/06 ; C07D413/04
摘要:
Antimicrobial dithiocarbamoyl quinolone compounds of the general formula:
wherein
(1) A¹, A², A³, R¹, R³, R⁴, and R⁶ form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and
(2)
(1) R¹ is X, R³ is X, or both R¹ and R³ are X; and
(2) X is -R¹⁵-N(R¹⁶)(R¹⁷) or -R¹⁵-R¹⁸-N(R¹⁹)(R¹⁷), where (a) (1) R¹⁵ is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁶ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) when X is R¹⁵-N(R¹⁶)(R¹⁷), R¹⁶ and R¹⁵ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁵ and R¹⁶ are bonded;
(b) R¹⁷ is C(=S)-S-M, where M is a pharmaceutically-acceptable salt or biohydrolyzable ester; and
(c) (1) R¹⁸ is alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁹ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) R¹⁸ and R¹⁹ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁸ and R¹⁹ are bonded;
and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.
wherein
(1) A¹, A², A³, R¹, R³, R⁴, and R⁶ form any of a variety of quinolone and related heterocyclic structures similar to those known in the art to have antimicrobial activity; and
(2)
(1) R¹ is X, R³ is X, or both R¹ and R³ are X; and
(2) X is -R¹⁵-N(R¹⁶)(R¹⁷) or -R¹⁵-R¹⁸-N(R¹⁹)(R¹⁷), where (a) (1) R¹⁵ is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁶ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) when X is R¹⁵-N(R¹⁶)(R¹⁷), R¹⁶ and R¹⁵ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁵ and R¹⁶ are bonded;
(b) R¹⁷ is C(=S)-S-M, where M is a pharmaceutically-acceptable salt or biohydrolyzable ester; and
(c) (1) R¹⁸ is alkyl, a carbocyclic ring, or a heterocyclic ring; and
(2) R¹⁹ is hydrogen; alkyl; alkenyl; a carbocyclic ring; a heterocyclic ring; or
(3) R¹⁸ and R¹⁹ may together comprise a heterocyclic ring including the nitrogen atom to which R¹⁸ and R¹⁹ are bonded;
and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.
公开/授权文献
- EP0366643A3 Novel antimicrobial dithiocarbamoyl quinolones 公开/授权日:1991-12-04
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