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1. 发明授权

US4764608A Process for the manufacture of spiro-linked pyrrolidine-2,5-dione derivatives 失效
标题翻译：用于制备螺连接的吡咯烷-2,5-二酮衍生物的方法
公开(公告)号：US4764608A
公开(公告)日：1988-08-16
申请号：US072050
申请日：1987-07-10
申请人： Kuniyoshi Masuzawa , Kyuya Okamura , Kazunori Kasuga , Shizuyoshi Fujimori , Susumu Kinoshita , Hiroshi Matsukubo
发明人： Kuniyoshi Masuzawa , Kyuya Okamura , Kazunori Kasuga , Shizuyoshi Fujimori , Susumu Kinoshita , Hiroshi Matsukubo
IPC分类号： C07B61/00 , C07D471/20 , C07D498/20 , C07D513/20 , C07D279/10 , C07D221/00 , C07D273/01
CPC分类号： C07D471/20 , C07D498/20 , C07D513/20
摘要： This invention relates to novel processes for the manufacture of spiro-linked pyrrolidine-2,5-diones of formula; ##STR1## which have a potent inhibitory activity on aldose reductase and are useful for reduction and prevention of chronic diabetic complications.The invented processes are useful as improved and convenient method for a large scale manufacture.
摘要翻译：本发明涉及用于制备式的螺环吡咯烷-2,5-二酮的新方法; 其对醛糖还原酶具有有效的抑制活性，并且可用于减少和预防慢性糖尿病并发症。本发明的方法可用于大规模制造的改进和方便的方法。

2. 发明授权

US4749789A Process for the manufacture of spiro-linked pyrrolidine 2,5-diones 失效
标题翻译：用于制备螺连接的吡咯烷2,5-二酮的方法
公开(公告)号：US4749789A
公开(公告)日：1988-06-07
申请号：US72004
申请日：1987-07-10
申请人： Kuniyoshi Masuzawa , Kyuya Okamura , Shizuyoshi Fujimori , Susumu Kinoshita , Hiroshi Matsukubo
发明人： Kuniyoshi Masuzawa , Kyuya Okamura , Shizuyoshi Fujimori , Susumu Kinoshita , Hiroshi Matsukubo
IPC分类号： C07B61/00 , C07D471/20 , C07D498/20 , C07D513/20 , C07D279/10 , C07D241/00 , C07D295/08
CPC分类号： C07D471/06 , C07D471/20 , C07D498/06 , C07D498/20 , C07D513/06 , C07D513/20
摘要： This invention relates to novel processes for the manufacture of spiro-linked pyrrolidine-2,5-diones of the formula; ##STR1## which have a potent inhibitory activity on aldose reductase and are useful for reduction and prevention of chronic diabetic complications.The invented processes are useful as improved and convenient method for a large scale manufacture.
摘要翻译：本发明涉及用于制备下式的螺环吡咯烷-2,5-二酮的新方法：其对醛糖还原酶具有有效的抑制活性，并且可用于减少和预防慢性糖尿病并发症。本发明的方法可用于大规模制造的改进和方便的方法。

3. 发明授权

US4942245A Benzimidazole Derivatives 失效
标题翻译：苯并咪唑衍生物
公开(公告)号：US4942245A
公开(公告)日：1990-07-17
申请号：US180065
申请日：1988-04-11
申请人： Kuniyoshi Masuzawa , Kyuya Okamura , Keigo Nishino , Mitsuo Ohashi , Katsuya Awano
发明人： Kuniyoshi Masuzawa , Kyuya Okamura , Keigo Nishino , Mitsuo Ohashi , Katsuya Awano
IPC分类号： C07D235/12 , C07D235/28
CPC分类号： C07D235/28 , C07D235/12
摘要： Benzimidazole derivatives of the following formula, ##STR1## wherein R.sup.1 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 6 or dimethylaminopropyl group, R.sup.2 indicates hydrogen atom or lower alkanoyl group having carbon atoms of 1 to 3, R.sup.3 indicates hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or lower alkanoyl group having carbon atoms of 1 to 3, X indicates sulfur atom, sulfinyl group, sulfonyl group, amino group or methylene group, A indicates alkylene group having carbon atoms of 1 to 12, which alkylene group may optionally be substituted by hydroxy group or lower alkyl group having carbon atoms of 1 to 3, --(CHR')N--CR".dbd.CR"--(CHR')M--, ##STR2## (in which R' and R" are each independently hydrogen atom, lower alkyl group having carbon atoms of 1 to 3 or hydroxy group, and n and m are equal to 0, 1, 2 or 3) and Y indicates oxygen atom or sulfur atom; their acid or alkali salts and hydrate thereof are useful as antiallergic agents.

4. 发明授权

US4980470A 8-alkoxyquinolonecarboxylic acid and salts thereof 失效
标题翻译： 8-烷氧基喹诺酮羧酸及其盐
公开(公告)号：US4980470A
公开(公告)日：1990-12-25
申请号：US3822
申请日：1987-01-16
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/47 , A61K31/495 , A61P31/04 , C07D215/56 , C07D401/04
CPC分类号： C07D215/56 , C07D401/04
摘要： Quinolonecarboxylic acid derivatives of the following formula: ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.
摘要翻译：下式的喹诺酮羧酸衍生物：其中R表示氢原子或低级烷基，R1表示低级烷基，R2表示氢原子，氨基或硝基，X表示卤素原子，Z表示卤素原子，哌嗪子基，N-甲基哌嗪基，3-甲基哌嗪基，3-羟基吡咯烷子基或下式的吡咯烷子基（这里，n为0或1，R 3表示氢原子或低级烷基基团，R4表示氢原子，低级烷基，R5表示氢原子，低级烷基，酰基或烷氧基羰基），其水合物及其药学上可接受的盐可用作抗菌剂。

5. 发明授权

US4894458A Quinolonecarboxylic acid derivatives and their preparation 失效
标题翻译：喹诺酮羧酸衍生物及其制备方法
公开(公告)号：US4894458A
公开(公告)日：1990-01-16
申请号：US233363
申请日：1988-08-18
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/47 , A61K31/495 , A61K31/55 , A61P31/04 , C07D215/56 , C07D401/04
CPC分类号： C07D215/56 , C07D401/04
摘要： Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R indicates straight or branched lower alkyl, R.sup.1 indicates cycloalkyl having 3 to 6 carbon atoms, straight or branched lower alkyl, halogenoalkyl, alkenyl, hydroxyalkyl, lower alkylamino or substituted or non-substituted phenyl, R.sup.2 indicates hydrogen, halogen, nitro or amino, X indicates halogen, Z indicates halogen, azetidino, pyrrolidino, piperidino, morpholino, thiomorpholino, piperazino or homopiperazino of the following formula, ##STR2## (here, n is 1 or 2, R.sup.3 indicates hydrogen, lower alkyl, lower acyl, acyloxycarbonyl or benzyl, R.sup.4 and R.sup.5 indicate hydrogen, lower alkyl, aminoalkyl, hydroxyalkyl or phenyl each independently), or pyrrolidino or piperidino of the following formula, ##STR3## (here, k is 0, 1 or 2, l is 0, 1 or 2, m is 0 or 1, R.sup.6 indicates hydrogen, lower alkyl or hydroxy, R.sup.7 indicates hydrogen, lower alkyl, halogenoalkyl or hydroxyalkyl, R.sup.8 indicates hydrogen, lower alkyl, lower acyl, alkoxycarbonyl or benzyl), the hydrates and pharmaceutically acceptable acid addition or alkali salts thereof are useful as antibacterial agents.
摘要翻译：下式的喹诺酮羧酸衍生物，其中R表示直链或支链的低级烷基，R1表示碳原子数为3〜6的环烷基，直链或支链的低级烷基，卤代烷基，链烯基，羟基烷基，低级烷基氨基或取代或未取代的苯基，R 2表示氢，卤素，硝基或氨基，X表示卤素，Z表示卤素，氮杂环丁烷基，吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代，哌嗪基或下式的高哌嗪基：（这里，n为1或2， R3表示氢，低级烷基，低级酰基，酰氧基羰基或苄基，R4和R5表示氢，低级烷基，氨基烷基，羟基烷基或苯基各自独立地），或下式的吡咯烷子基或哌啶子基，其中，，1或2，l为0,1或2，m为0或1，R6表示氢，低级烷基或羟基，R7表示氢，低级烷基，卤代烷基或羟烷基，R8表示氢，低级烷基，低级酰基，烷氧基羰基或苄基），其水合物及其药学上可接受的酸加成盐或碱盐可用作抗菌剂。

6. 发明授权

US4791118A Quinolonecarboxylic acid derivatives and their preparation 失效
标题翻译：喹诺酮羧酸衍生物及其制备方法
公开(公告)号：US4791118A
公开(公告)日：1988-12-13
申请号：US903424
申请日：1986-09-04
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/47 , A61P31/04 , C07D401/04
CPC分类号： C07D401/04
摘要： Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R is hydrogen atom or lower alkyl group, Alk is lower alkylene group and X is hydrogen atom or halogen atom; the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agent.
摘要翻译：下式的喹诺酮羧酸衍生物，其中R是氢原子或低级烷基，Alk是低级亚烷基，X是氢原子或卤原子; 其水合物及其药学上可接受的盐可用作抗菌剂。

7. 发明授权

US4753953A Pyridonecarboxylic acid derivatives and antibacterial pharmaceutical compositions thereof 失效
标题翻译：吡啶酮羧酸衍生物及其抗菌药物组合物
公开(公告)号：US4753953A
公开(公告)日：1988-06-28
申请号：US876420
申请日：1986-06-20
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/47 , A61P31/04 , C07D215/56 , C07D401/04 , C07D498/06
CPC分类号： C07D215/56 , C07D401/04
摘要： Pyridonecarboxylic acid derivatives of the following formula, ##STR1## wherein R is hydrogen atom or lower alkyl group, R.sup.1 is lower alkyl group, cycloalkyl group or haloalkyl group, Y is hydrogen atom or halogen atom, or Y and R.sup.1 are ##STR2## which work together, R.sup.2 is hydrogen atom, lower alkyl group, alkoxycarbonyl group or acyl group and n is 0 or 1; the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.
摘要翻译：下式的吡咯烷酮羧酸衍生物，其中R是氢原子或低级烷基，R 1是低级烷基，环烷基或卤代烷基，Y是氢原子或卤素原子，或者Y和R 1是一起工作，R2为氢原子，低级烷基，烷氧基羰基或酰基，n为0或1; 其水合物和药学上可接受的盐可用作抗菌剂。

8. 发明授权

US5043450A 8-alkoxyquinolonecarboxylic acid and salts thereof 失效
标题翻译： 8-烷氧基喹诺酮羧酸及其盐
公开(公告)号：US5043450A
公开(公告)日：1991-08-27
申请号：US600828
申请日：1990-10-22
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/47 , A61K31/495 , A61P31/04 , C07D215/56 , C07D401/04
CPC分类号： C07D215/56 , C07D401/04
摘要： Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R indicates a hydrogen atom or lower alkyl group, R.sup.1 indicates a lower alkyl group, R.sup.2 indicates a hydrogen atom, amino group or nitro group, X indicates a halogen atom, and Z indicates a halogen atom, piperazino group, N-methylpiperazino group, 3-methylpiperazino group, 3-hydroxypyrrolidino group, or pyrrolidino group of the following formula, ##STR2## (here, n is 0 or 1, R.sup.3 indicates a hydrogen atom or lower alkyl group, R.sup.4 indicates a hydrogen atom, lower alkyl group or substituted lower alkyl group and R.sup.5 indicates a hydrogen atom, lower alkyl group, acyl group or alkoxycarbonyl group), the hydrates and pharmaceutically acceptable salts thereof are useful as antibacterial agents.

9. 发明授权

US4826982A Quinolonecarboxylic acid derivatives 失效
标题翻译：喹诺酮羧酸衍生物
公开(公告)号：US4826982A
公开(公告)日：1989-05-02
申请号：US902606
申请日：1986-09-02
申请人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
发明人： Kuniyoshi Masuzawa , Seigo Suzue , Keiji Hirai , Takayoshi Ishizaki
IPC分类号： A61K31/495 , A61P31/04 , C07D215/56 , C07D401/04
CPC分类号： C07D215/56
摘要： Quinolonecarboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each independently hydrogen atom or lower alkyl group; the hydrates or the pharmaceutically acceptable acid addition or alkali salts thereof are useful as an antibacterial agent.
摘要翻译：下式的喹诺酮羧酸衍生物，其中R 1，R 2，R 3和R 4各自独立地为氢原子或低级烷基; 水合物或其药学上可接受的酸加成盐或碱盐可用作抗菌剂。

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