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1. 发明授权

US5097032A Antibacterial agents - II 失效
标题翻译：抗菌剂 - 二
公开(公告)号：US5097032A
公开(公告)日：1992-03-17
申请号：US537548
申请日：1990-06-13
申请人： John M. Domagala , Thomas F. Mich , Joseph P. Sanchez
发明人： John M. Domagala , Thomas F. Mich , Joseph P. Sanchez
IPC分类号： C07D401/04 , C07D471/04 , C07D487/10 , C07D498/06 , C07D519/00
CPC分类号： C07D401/04 , C07D471/04 , C07D487/10
摘要： Novel naphthyridine-, quinoline- and benzoxazinecarboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections including the description of certain novel intermediates used in the manufacture of the antibacterial agents.
摘要翻译：描述了作为抗菌剂的新型萘啶，喹啉和苯并恶嗪羧酸以及其制备，配制和用于治疗细菌感染的方法，包括用于制备抗菌剂的某些新型中间体的描述。

2. 发明授权

US4977154A 5-amino and 5-hydroxy-6-fluoroquinolones as antibacterial agents 失效
标题翻译： 5-氨基和5-羟基-6-氟喹诺酮作为抗菌剂
公开(公告)号：US4977154A
公开(公告)日：1990-12-11
申请号：US918568
申请日：1986-10-20
申请人： Joseph P. Sanchez , Ashok K. Trehan
发明人： Joseph P. Sanchez , Ashok K. Trehan
IPC分类号： A61K31/495 , C07D215/56 , C07D401/04 , C07D471/04
CPC分类号： C07D215/56 , C07D401/04 , C07D471/04
摘要： Novel 7-piperazine derivatives of 5-amino- and 5-hydroxy-1-cyclopropyl-1,4-dihydro-4-oxoquinoline-3-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.
摘要翻译：描述了作为抗菌剂的5-氨基和5-羟基-1-环丙基-1,4-二氢-4-氧代喹啉-3-羧酸的新型7-哌嗪衍生物及其制备，配制和使用的方法在治疗细菌感染。

3. 发明授权

US4477449A Certain 1,8-naphthyridine compounds useful as antibacterial agents 失效
标题翻译：某些用作抗菌剂的1,8-萘啶化合物
公开(公告)号：US4477449A
公开(公告)日：1984-10-16
申请号：US468836
申请日：1983-03-01
申请人： Joseph P. Sanchez
发明人： Joseph P. Sanchez
IPC分类号： C07D471/04 , A61K31/435
CPC分类号： C07D471/04
摘要： Certain substituted 1,4-dihydro-4-oxo-7-(3-thiazolidinyl or 4-thiomorpholinyl)-1,8-naphthyridine-3-carboxylic acids and derivatives are disclosed as antibacterial agents.
摘要翻译：公开了某些取代的1,4-二氢-4-氧代-7-（3-噻唑烷二基或4-硫代吗啉基）-1,8-萘啶-3-羧酸及其衍生物作为抗菌剂。

4. 发明授权

US4851418A Naphthyridine antibacterial agents containing an .alpha.-amino acid in the side chain of the 7-substituent 失效
标题翻译：在7-取代基的侧链中含有α-氨基酸的萘吡啶抗菌剂
公开(公告)号：US4851418A
公开(公告)日：1989-07-25
申请号：US220177
申请日：1988-07-20
申请人： Joseph P. Sanchez
发明人： Joseph P. Sanchez
IPC分类号： C07D215/56 , A61K31/435 , A61K31/4427 , A61K31/445 , A61K31/47 , A61K31/495 , A61K31/55 , A61P31/04 , C07D401/04 , C07D417/04 , C07D471/04 , C07D471/08 , C07D487/08
CPC分类号： C07D401/04 , C07D471/04
摘要： Novel quinolone and naphthyridine antibacterial agents are herein described having improved in vivo activity both orally and subcutaneously where the 7-side chain of such compounds contain an .alpha.-amino acid; also described are its corresponding optical isomers, methods of preparation as well as compositions and methods of treating infections diseases.

5. 发明授权

US4840956A Novel disubstituted-7-pyrrolidinoquinoline antibacterial agents 失效
标题翻译：新型二取代-7-吡咯烷基喹啉抗菌剂
公开(公告)号：US4840956A
公开(公告)日：1989-06-20
申请号：US144301
申请日：1988-01-14
申请人： John M. Domagala , Susan E. Hagen , Joseph P. Sanchez , Marjorie S. Solomon
发明人： John M. Domagala , Susan E. Hagen , Joseph P. Sanchez , Marjorie S. Solomon
IPC分类号： C07D401/04
CPC分类号： C07D401/04
摘要： Disubstituted 7-pyrrolidinoquinoline- and -napthylridine-3-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.
摘要翻译：描述作为抗菌剂的二取代的7-吡咯烷基喹啉 - 和 - 萘基-3-羧酸以及其制备，配制和用于治疗细菌感染的方法。

6. 发明授权

US4771055A 7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-quinoline-carboxylic acids 失效
标题翻译： 7 - [[3-（氨基甲基）-3-烷基] -1-吡咯烷基] - 喹啉羧酸
公开(公告)号：US4771055A
公开(公告)日：1988-09-13
申请号：US39438
申请日：1987-04-21
申请人： John M. Domagala , Susan E. Hagen , Joseph P. Sanchez
发明人： John M. Domagala , Susan E. Hagen , Joseph P. Sanchez
IPC分类号： A61K31/435 , A61K31/47 , A61P31/04 , A61P35/00 , C07D207/09 , C07D401/04 , C07D471/04 , C07D215/56
CPC分类号： C07D401/04 , C07D471/04
摘要： Novel, orally active antibacterial agents are described and characterized as 7-[[3-(aminomethyl)-3-alkyl]-1-pyrrolidinyl]-6-fluoro-1,4-dihydro-4-oxo-3-quinoline carboxylic acids or corresponding 1,8-naphthyridine derivatives as well as methods for their manufacture.
摘要翻译：描述了新型口服活性抗菌剂，并将其表征为7 - [[3-（氨基甲基）-3-烷基] -1-吡咯烷基] -6-氟-1,4-二氢-4-氧-3-喹啉羧酸酸或相应的1,8-萘啶衍生物及其制备方法。

7. 发明授权

US4735949A Disubstituted-7-pyrrolidinonaphthyridine antibacterial agents 失效
标题翻译：二取代-7-吡咯烷基萘啶抗菌剂
公开(公告)号：US4735949A
公开(公告)日：1988-04-05
申请号：US64439
申请日：1987-06-22
申请人： John M. Domagala , Susan E. Prugh , Joseph P. Sanchez , Marjorie S. Solomon
发明人： John M. Domagala , Susan E. Prugh , Joseph P. Sanchez , Marjorie S. Solomon
IPC分类号： C07D401/04 , A61K31/44 , C07D471/04
CPC分类号： C07D401/04
摘要： Disubstituted 7-pyrrolidinoquinoline- and -naphthyridine-3-carboxylic acids as antibacterial agents are described as well as methods for their manufacture, formulation, and use in treating bacterial infections.
摘要翻译：描述作为抗菌剂的二取代的7-吡咯烷基喹啉和 - 萘啶-3-羧酸以及其制备，配制和用于治疗细菌感染的方法。

8. 发明授权

US4311699A Aminoacid derivatives of cephalosporin compounds 失效
标题翻译：头孢菌素化合物的氨基酸衍生物
公开(公告)号：US4311699A
公开(公告)日：1982-01-19
申请号：US112656
申请日：1980-01-31
申请人： Theodore H. Haskell , Thomas F. Mich , Joseph P. Sanchez , Dietrich Schweiss
发明人： Theodore H. Haskell , Thomas F. Mich , Joseph P. Sanchez , Dietrich Schweiss
IPC分类号： C07D239/36 , C07D501/24 , C07D521/00 , A61K31/545 , C07D501/34 , C07D501/56
CPC分类号： C07D239/36 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel organic amide compounds which are N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]cephalosporin compounds having broad spectrum antibacterial utility are provided by (a) reacting the free amino acid of the appropriate cephalosporin or the acid salt or silylated derivative or complex thereof with a reactive derivative of the corresponding N-2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidine carboxylic acid or (b) reacting the free amino acid 7-aminocephalosporanic acid or a related compound or the acid salt or silylated derivative thereof with a reactive derivative of the corresponding D-N-[2-[(acylaminoacylamino or aminoacylamino)phenyl]-4-hydroxy-5-pyrimidinylcarbonyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：通过（a）使适当头孢菌素的游离氨基酸反应，得到具有广谱抗菌效用的N- [2 - [（酰氨基酰氨基或氨基酰氨基）苯基] -4-羟基-5-嘧啶基羰基]头孢菌素的新型有机酰胺化合物或其相应的N-2 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -4-羟基-5-嘧啶羧酸的反应性衍生物的酸式盐或甲硅烷基化衍生物或其配合物，或（b）使游离氨基酸7- 氨基头孢烷酸或相关化合物或其酸盐或甲硅烷基化衍生物与相应的DN- [2 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -4-羟基-5-嘧啶基羰基] -2-取代的甘氨酸的反应性衍生物。还公开了含有所述化合物的药物组合物和使用所述组合物治疗感染的方法。

9. 发明授权

US5620997A Isothiazolones 失效
标题翻译：异噻唑啉酮
公开(公告)号：US5620997A
公开(公告)日：1997-04-15
申请号：US456149
申请日：1995-05-31
申请人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
发明人： Gary L. Bolton , John M. Domagala , Edward F. Elslager , Rocco D. Gogliotti , Terri S. Purchase , Joseph P. Sanchez , Bharat K. Trivedi
IPC分类号： A61K31/428 , A61K31/437 , A61K31/4439 , A61K31/506 , A61K31/519 , A61K31/5377 , A61P9/10 , A61P29/00 , A61P31/12 , A61P31/14 , C07D275/04 , C07D417/04 , C07D513/04 , C07D513/14 , C07D275/06 , A61K31/41
CPC分类号： C07D275/04 , C07D513/04 , C07D513/14
摘要： Isothiazolones having the general structure ##STR1## where A is a monocyclic or bicyclic ring which may contain up to 3 heteroatoms selected from O, S, and N; R.sup.1 and R.sup.2 are substituent groups such as alkyl, alkoxy, hydroxy, nitro, cyano, amino, and carboxy; and R.sup.5 is alkyl, cycloalkyl, phenyl, and Het. The isothiazolones are useful as anti-retroviral agents, anti-inflammatory agents, and anti-atherosclerotic agents.
摘要翻译：具有一般结构的异噻唑酮，其中A是可以含有至多3个选自O，S和N的杂原子的单环或双环; R1和R2是取代基，例如烷基，烷氧基，羟基，硝基，氰基，氨基和羧基; R5是烷基，环烷基，苯基和Het。异噻唑酮可用作抗逆转录病毒剂，抗炎剂和抗动脉粥样硬化剂。

10. 发明授权

US4929613A Antibacterial agents 失效
公开(公告)号：US4929613A
公开(公告)日：1990-05-29
申请号：US222608
申请日：1988-07-25
申请人： Townley P. Culbertson , John M. Domagala , Susan E. Hagen , Joseph P. Sanchez
发明人： Townley P. Culbertson , John M. Domagala , Susan E. Hagen , Joseph P. Sanchez
IPC分类号： A61K31/47 , A61P31/04 , C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/18 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04 , C07D405/02
CPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
摘要： The novel series of quinoline-, naphthyridine- and benzoxazine-carboxylic acids useful as antibacterial agents is described. Novel methods for preparing the compounds as well as novel intermediates are also described as are methods for their formulation and the use thereof in treating bacterial infections.

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