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1. 发明授权

US4497816A 7-(4-Pyridyl)-1,8-naphthyridine derivatives and their antibacterial compositions 失效
标题翻译： 7-（4-吡啶基）-1,8-萘啶衍生物及其抗菌组合物
公开(公告)号：US4497816A
公开(公告)日：1985-02-05
申请号：US519513
申请日：1983-08-01
申请人： Jun-ichi Matsumoto , Yoshiro Nishimura , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Yoshiro Nishimura , Shinichi Nakamura
IPC分类号： A61K31/44 , A61P31/04 , C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： A 7-(4-pyridyl)-1,8-naphthyridine compound of the formula ##STR1## wherein R.sub.1 is a hydrogen atom, an ethyl or vinyl group, and R.sub.2 is a hydrogen atom or a lower alkyl group having 1 to 6 carbon atoms,and a salt thereof.The compounds represented by the formula are useful in antibacterial compositions or intermediates thereof.
摘要翻译：式（Ia）的7-（4-吡啶基）-1,8-萘啶化合物，其中R1是氢原子，乙基或乙烯基，R2是氢原子或具有1-6个碳原子的低级烷基原子及其盐。由式表示的化合物可用于抗菌组合物或其中间体。

2. 发明授权

US4359578A Naphthyridine derivatives and salts thereof useful as antibacterial agents 失效
标题翻译：萘吡啶衍生物及其盐可用作抗菌剂
公开(公告)号：US4359578A
公开(公告)日：1982-11-16
申请号：US68966
申请日：1979-08-23
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/495
CPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , Y10S514/96 , Y10S514/962
摘要： This invention relates to 1,8-naphthyridine compounds of the formula ##STR1## wherein X is a halogen atom especially fluorine atom,R.sub.1 is an ethyl group or a vinyl group, andR.sub.2 is a hydrogen atom or a lower alkyl group, their salts and processes for the preparation of them.The 1,8-naphthyridine compounds and their salts are useful as antibacterial agents and intermediates thereof.

3. 发明授权

US4352803A Novel naphthyridine derivatives, intermediates thereof, processes for preparation thereof, and use thereof 失效
标题翻译：新型萘啶衍生物，其中间体，其制备方法及其用途
公开(公告)号：US4352803A
公开(公告)日：1982-10-05
申请号：US264824
申请日：1981-05-18
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/495
CPC分类号： C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , Y10S514/96 , Y10S514/962
摘要： This invention relates to 1,8-naphthyridine compounds of the formula ##STR1## wherein X is a halogen atom especially fluorine atom,R.sub.1 is an ethyl group or a vinyl group, andR.sub.2 is a hydrogen atom or a lower alkyl group, their salts and processes for the preparation of them.The 1,8-naphthyridine compounds and their salts are useful as antibacterial agents and intermediates thereof.
摘要翻译：本发明涉及下式的1,8-萘啶化合物，其中X是卤原子，特别是氟原子，R 1是乙基或乙烯基，R 2是氢原子或低级烷基，它们的盐以及它们的制备过程。 1,8-萘啶化合物及其盐可用作抗菌剂及其中间体。

4. 发明授权

US4341784A Naphthyridine derivatives 失效
标题翻译：萘啶衍生物
公开(公告)号：US4341784A
公开(公告)日：1982-07-27
申请号：US187081
申请日：1980-09-15
申请人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
发明人： Jun-ichi Matsumoto , Yoshiyuki Takase , Yoshiro Nishimura
IPC分类号： C07D487/02 , A61K31/435 , A61P31/04 , C07D471/04 , A61K31/44
CPC分类号： C07D471/04 , Y02P20/55
摘要： The present invention provides a 1,8-naphthyridine compound of the formula ##STR1## wherein R is hydrogen, methyl, ethyl or propyl, and a nontoxic pharmaceutically acceptable salt thereof, and a process for preparing a 1,8-naphthyridine compound of the above formula which comprises(A) reacting a compound of the formula ##STR2## wherein Y is halogen, lower alkoxy, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, lower alkylsulfonyloxy or arylsulfonyloxy, and R.sub.1 is hydrogen or lower alkyl,with a compound of the formula ##STR3## wherein R.sub.2 is hydrogen or a protective group for the amino group, and R is as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(B) decomposing a compound of the formula ##STR4## wherein A .crclbar. is a fluorine-containing anion, and R.sub.1 and R.sub.2 are as defined above,and when a reaction product in which R.sub.1 is lower alkyl and/or R.sub.2 is the amino protective group is obtained, treating it with an acid or base, and/or reductively cleaving it,(C) treating a compound of the formula ##STR5## wherein R'.sub.1 is hydrogen or lower alkyl, R'.sub.2 is hydrogen or a protective group for the amino group, provided that R'.sub.1 and R'.sub.2 are not hydrogen atoms at the same time, and R is as defined above,with an acid or base, and/or reductively cleaving it, and optionally converting the resulting compound to a nontoxic pharmaceutically acceptable salt thereof.The 1,8-naphthyridine compound is useful as an antibacterial agent.
摘要翻译：本发明提供式IMA图示的1,8-萘啶化合物，其中R是氢，甲基，乙基或丙基，及其无毒的药学上可接受的盐，以及制备1,8-萘啶化合物的方法其包含（A）使式（I）的化合物其中Y为卤素，低级烷氧基，低级烷硫基，低级烷基亚磺酰基，低级烷基磺酰基，低级烷基磺酰氧基或芳基磺酰氧基，R 1为氢或低级烷基，其中R2是氢或氨基保护基的式“IMAGE”，R的定义同上，当R1是低级烷基和/或R2是氨基保护基的反应产物得到时，将其处理（B）分解其中A（ - ）为含氟阴离子的式“IMAGE”的化合物，并且R 1和R 2如上所定义，当反应其中R1是低级烷基和/或 r R2是得到的氨基保护基团，用酸或碱处理，和/或还原性地裂解它;（C）处理下式化合物其中R'1是氢或低级烷基，R'2 是氢或氨基的保护基团，条件是R 1和R 2不同时为氢原子，R为如上所定义，与酸或碱反应，和/或还原性地裂解，和任选地将所得化合物转化为无毒的药学上可接受的盐。 1,8-萘啶化合物可用作抗菌剂。

5. 发明授权

US4886810A Quinoline derivatives, pharmaceutical composition and method of use 失效
标题翻译：喹啉衍生物，药物组合物和使用方法
公开(公告)号：US4886810A
公开(公告)日：1989-12-12
申请号：US042806
申请日：1987-04-27
申请人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hiroshi Egawa , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hiroshi Egawa , Shinichi Nakamura
IPC分类号： A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/535 , A61K31/54 , A61P31/04 , C07D215/56 , C07D401/04 , C07D413/04
CPC分类号： C07D215/56 , C07D401/04
摘要： The present invention relates to quinoline derivatives of the formula ##STR1## wherein Z is an amino group or a halogen atom, R is ##STR2## in which R.sub.1 is a hydrogen atom, a lower alkyl or haloalkyl group, R.sub.2 is a hydrogen atom or a lower alkyl group, R.sub.3 is a lower alkyl or haloalkyl group, R.sub.4 is a hydrogen atom or a lower alkyl group, R.sub.5 and R.sub.6 are the same or different and each represents a hydrogen atom or a lower alkyl group, or R.sub.5 and R.sub.6, together with the nitrogen atom to which they are attached, form a heterocyclic ring, and n is 0 or 1, with the proviso that when Z is an amino group, R is (B);and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.
摘要翻译：本发明涉及式（I）的喹啉衍生物，其中Z为氨基或卤素原子，R为（A）或（IMA）（B），其中R 1为氢原子，低级烷基或卤代烷基，R2为氢原子或低级烷基，R3为低级烷基或卤代烷基，R4为氢原子或低级烷基，R5和R6相同或不同，分别表示氢原子或低级烷基，或R 5和R 6与它们所连接的氮原子一起形成杂环，n为0或1，条件是当Z为氨基时，R为（ B）; 及其酯及其盐及其制备方法。这些化合物显示出优异的抗菌活性，并且是有用的抗菌剂。

6. 发明授权

US4795751A 5-substituted-6,8-difluoroquinolines useful as antibacterial agents 失效
标题翻译：可用作抗菌剂的5-取代-6,8-二氟喹啉
公开(公告)号：US4795751A
公开(公告)日：1989-01-03
申请号：US928297
申请日：1986-10-28
申请人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hiroshi Egawa , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hiroshi Egawa , Shinichi Nakamura
IPC分类号： C07D401/04 , A61K20060101 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/535 , A61K31/55 , A61P31/04 , C07D215/00 , C07D215/22 , C07D215/56 , C07D241/04 , C07D243/08 , C07D401/02 , C07D413/04 , C07D487/08 , A61K31/53
CPC分类号： C07D401/04 , C07D215/56
摘要： The present invention relates to a quinoline derivative of the formula ##STR1## wherein Z is an amino group or a halogen atom, R.sub.1 is a hydrogen atom or a methyl or ethyl group, R.sub.2 is a hydrogen atom or a methyl or fluoromethyl group, R.sub.3 and R.sub.4 are the same or different and each represents a hydrogen atom or a methyl group, and n is 1 or 2;and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.
摘要翻译：本发明涉及下式的喹啉衍生物，其中Z为氨基或卤原子，R 1为氢原子或甲基或乙基，R 2为氢原子或甲基或氟甲基，R 3 和R4相同或不同，各自表示氢原子或甲基，n为1或2; 及其酯及其盐及其制备方法。这些化合物显示出优异的抗菌活性，并且是有用的抗菌剂。

7. 发明授权

US4382937A Naphthyridine derivatives and their use as anti-bacterials 失效
标题翻译：萘啶衍生物及其作为抗菌剂的用途
公开(公告)号：US4382937A
公开(公告)日：1983-05-10
申请号：US351924
申请日：1982-02-24
申请人： Jun-ichi Matsumoto , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Shinichi Nakamura
IPC分类号： C07D213/75 , C07D213/77 , C07D471/04 , A61K31/44
CPC分类号： C07D213/75 , C07D213/77 , C07D471/04
摘要： A 1,8-naphthyridine compound of the formula ##STR1## wherein R is a vinyl or 2-fluoroethyl group, andR.sub.1 and R.sub.2 are the same or different and each represents a hydrogen atom or a lower alkyl group having 1 to 4 carbon atoms,and the esters thereof and salts thereof. For example, 7-(3-amino-1-pyrrolidinyl)-6-fluoro-1,4-dihydro-4-oxo-1-vinyl-1,8-naphthyridine-3-carboxylic acid and nontoxic salts thereof, which are covered by the aforesaid compound, are useful as an antibacterial agent.
摘要翻译：式（I）的1,8-萘啶化合物，其中R是乙烯基或2-氟乙基，R 1和R 2相同或不同，各自表示氢原子或具有1〜 4个碳原子，以及它们的酯及其盐。例如，7-（3-氨基-1-吡咯烷基）-6-氟-1,4-二氢-4-氧代-1-乙烯基-1,8-萘啶-3-羧酸及其无毒盐，其中被上述化合物覆盖，可用作抗菌剂。

8. 发明授权

US5013841A Oxo quinoline derivatives 失效
标题翻译：氧喹啉衍生物
公开(公告)号：US5013841A
公开(公告)日：1991-05-07
申请号：US389900
申请日：1989-08-04
申请人： Jun-ichi Matsumoto , Akira Minamida , Masahiro Fujita , Tohru Hirose , Junji Nakano , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Akira Minamida , Masahiro Fujita , Tohru Hirose , Junji Nakano , Shinichi Nakamura
IPC分类号： C07D401/04 , A61K20060101 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/497 , A61P31/04 , C07D20060101 , C07D215/56 , C07D295/14
CPC分类号： C07D215/56
摘要： A quinoline derivative of the formula ##STR1## wherein Z is an amino group or a halogen atom, and R.sub.1, R.sub.2 and R.sub.3 are the same or different and each represents a hydrogen atom or a lower alkyl group having 1 to 5 carbon atoms,and an ester thereof and a salt of the derivative or the ester and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful as antibacterial agents.

9. 发明授权

US4649144A Antibacterial 7-(3-amino-1-pyrrolidinyl)-1-cyclopropyl-6-fluoro-1,4-dihydro-4-oxo-1,8- naphthyridine-3-carboxylic acid derivatives 失效
标题翻译：抗菌7-（3-氨基-1-吡咯烷基）-1-环丙基-6-氟-1,4-二氢-4-氧代-1,8-二氮杂萘-3-羧酸衍生物
公开(公告)号：US4649144A
公开(公告)日：1987-03-10
申请号：US632853
申请日：1984-07-20
申请人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hitoshi Uno , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Teruyuki Miyamoto , Hitoshi Uno , Shinichi Nakamura
IPC分类号： C07D487/04 , A61K31/435 , A61K31/4375 , A61P31/04 , C07D207/12 , C07D207/14 , C07D213/61 , C07D213/78 , C07D213/80 , C07D213/85 , C07D401/04 , C07D471/04
CPC分类号： C07D213/78 , C07D207/12 , C07D207/14 , C07D213/61 , C07D213/80 , C07D213/85 , C07D401/04 , C07D471/04
摘要： The present invention relates to a 1,8-naphthyridine derivative of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are the same or different and each hydrogen or lower alkyl having 1 to 5 carbon atoms; and esters thereof and salts thereof and processes for preparation thereof. These compounds show excellent antibacterial activity and are useful antibacterial agents.
摘要翻译：本发明涉及下式的1,8-萘啶衍生物，其中R 1，R 2和R 3相同或不同，每个氢或具有1至5个碳原子的低级烷基; 及其酯及其盐及其制备方法。这些化合物显示出优异的抗菌活性，并且是有用的抗菌剂。

10. 发明授权

US4496566A Naphthyridine derivatives 失效
标题翻译：萘啶衍生物
公开(公告)号：US4496566A
公开(公告)日：1985-01-29
申请号：US333181
申请日：1981-12-21
申请人： Jun-ichi Matsumoto , Shinichi Nakamura
发明人： Jun-ichi Matsumoto , Shinichi Nakamura
IPC分类号： A01N43/90 , A23L3/3544 , A61K31/495 , A61P31/04 , C07D213/74 , C07D213/75 , C07D213/77 , C07D471/04 , A61K31/47 , C07D401/04
CPC分类号： C07D213/75 , C07D213/74 , C07D213/77 , C07D471/04
摘要： A 1,8-naphthyridine compound of the formula ##STR1## wherein R.sub.1 is a lower alkyl group, and the esters and salts thereof. The 1,8-naphthyridine compound of the formula (I) in which R.sub.1 is a methyl group is useful as an antibacterial agent.
摘要翻译：其中R1是低级烷基的式“IMAGE”的1,8-萘啶化合物及其酯和盐。其中R 1为甲基的式（I）的1,8-萘啶化合物可用作抗菌剂。

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