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1. 发明授权

US4665079A Antibacterial agents 失效
公开(公告)号：US4665079A
公开(公告)日：1987-05-12
申请号：US692820
申请日：1985-01-23
申请人： Townley P. Culbertson , John M. Domagala , Thomas F. Mich , Jeffrey B. Nichols
发明人： Townley P. Culbertson , John M. Domagala , Thomas F. Mich , Jeffrey B. Nichols
IPC分类号： C07D498/00 , A61K31/435 , A61K31/47 , A61P31/04 , C07C45/00 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D403/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D471/10 , C07D487/04 , C07D487/10 , C07D498/06 , C07D519/00 , A61K31/495
CPC分类号： C07D207/08 , C07C205/45 , C07C45/00 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10
摘要： Novel naphthyridine-, quinoline- and benzoxazine-carboxylic 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.

2. 发明授权

US4638067A Antibacterial agents 失效
公开(公告)号：US4638067A
公开(公告)日：1987-01-20
申请号：US764357
申请日：1985-08-12
申请人： Townley P. Culbertson , John M. Domagala , Thomas F. Mich , Jeffrey B. Nichols
发明人： Townley P. Culbertson , John M. Domagala , Thomas F. Mich , Jeffrey B. Nichols
IPC分类号： C07C45/00 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D401/14 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06 , C07D498/06 , C07D519/00 , C07D215/02
CPC分类号： C07D207/08 , C07C205/45 , C07C45/00 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06
摘要： Novel naphthyridine-, quinoline- and benzoxazine-carboxylic 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.

3. 发明授权

US4604401A Antibacterial agents III 失效
标题翻译：抗菌剂三
公开(公告)号：US4604401A
公开(公告)日：1986-08-05
申请号：US633151
申请日：1984-07-20
申请人： Thomas F. Mich , Townley P. Culbertson , John M. Domagala
发明人： Thomas F. Mich , Townley P. Culbertson , John M. Domagala
IPC分类号： A61K31/47 , A61P31/04 , C07D215/58 , C07D401/04 , C07D471/04 , C07D487/10 , C07D215/22
CPC分类号： C07D401/04 , C07D215/58 , C07D471/04 , C07D487/10
摘要： Novel 1-amino-naphthyridine- and quinoline-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新型1-氨基 - 萘啶和喹啉羧酸以及其制备，配制和用于治疗细菌感染的方法。

4. 发明授权

US4571396A Antibacterial agents 失效
公开(公告)号：US4571396A
公开(公告)日：1986-02-18
申请号：US708565
申请日：1985-03-11
申请人： Marland P. Hutt , Thomas F. Mich , Townley P. Culbertson
发明人： Marland P. Hutt , Thomas F. Mich , Townley P. Culbertson
IPC分类号： C07D451/02 , A61K31/47 , A61K31/495 , A61P31/04 , C07D213/74 , C07D213/75 , C07D215/56 , C07D401/04 , C07D405/12 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08 , C07D498/00 , C07D519/00
CPC分类号： C07D213/74 , C07D213/75 , C07D215/56 , C07D405/12 , C07D451/04 , C07D471/04 , C07D471/08 , C07D487/08
摘要： Novel naphthyridine-, quinoline- and benzoxazine-carboxylic 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.

5. 发明授权

US4311698A 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：US4311698A
公开(公告)日：1982-01-19
申请号：US112655
申请日：1980-01-31
申请人： Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss , Townley P. Culbertson
发明人： Theodore H. Haskell , Thomas F. Mich , Dietrich Schweiss , Townley P. Culbertson
IPC分类号： C07D213/80 , C07D213/85 , C07D501/24 , C07D521/00 , A61K31/545 , C07D501/34 , C07D501/56
CPC分类号： C07D213/80 , C07D213/85 , C07D231/12 , C07D233/56 , C07D249/08
摘要： Novel organic amide compounds which are N-[6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl]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-6-[(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinic 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-[6-(acylaminoacylamino or aminoacylamino)phenyl]-1,2-dihydro-2-oxonicotinyl]-2-substituted glycine. Pharmaceutical compositions containing said compounds and methods for treating infections using said compositions are also disclosed.
摘要翻译：具有广谱抗菌效用的N- [6 - [（酰氨基酰氨基或氨酰氨基）苯基] -1,2-二氢-2-氧代烟酰基]头孢菌素化合物的新型有机酰胺化合物是通过（a）使游离氨基酸适当的头孢菌素或其酸盐或甲硅烷基化衍生物或其配合物与相应的N-6 - [（酰氨基酰基氨基或氨酰基氨基）苯基] -1,2-二氢-2-氧代烟酸的反应性衍生物或（b）使游离氨基酸7-氨基头孢烷酸或相关化合物或其酸式盐或甲硅烷基化衍生物与相应的DN- [6-（酰氨基酰基氨基或氨酰基氨基）苯基] -1,2-二氢-2-氧代烟酰基] -2- 取代甘氨酸。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。

6. 发明授权

US4777175A Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US4777175A
公开(公告)日：1988-10-11
申请号：US907340
申请日：1986-09-15
申请人： Townley P. Culbertson , John M. Doma , Thomas F. Mich , Jeffrey B. Nichols
发明人： Townley P. Culbertson , John M. Doma , Thomas F. Mich , Jeffrey B. Nichols
IPC分类号： A01N43/90 , C07C45/00 , C07D205/04 , C07D207/08 , C07D207/09 , C07D207/14 , C07D207/16 , C07D207/24 , C07D207/26 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D317/22 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06 , C07D498/06 , C07D519/00 , A01N43/42 , A01N43/48 , C07D215/02
CPC分类号： C07D207/08 , C07C205/45 , C07C45/00 , C07D205/04 , C07D207/09 , C07D207/14 , C07D207/16 , C07D207/277 , C07D213/74 , C07D215/56 , C07D265/36 , C07D317/22 , C07D401/04 , C07D407/12 , C07D409/04 , C07D413/06 , C07D417/04 , C07D471/04 , C07D487/04 , C07D487/10 , C07D491/06
摘要： Novel naphthyridine-, quinoline- and benzoxazine-carboxylic 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：描述了新的萘啶，喹啉和苯并恶嗪羧酸作为抗菌剂，以及用于制备，配制和用于治疗细菌感染的方法，包括用于制造抗菌剂的某些新型中间体的描述。

7. 发明授权

US4550103A Antibacterial 1-oxo-benzoquinolizine-2-carboxylic acids 失效
标题翻译：抗菌1-氧代 - 苯喹啉-2-羧酸
公开(公告)号：US4550103A
公开(公告)日：1985-10-29
申请号：US632999
申请日：1984-07-20
申请人： Thomas F. Mich , Townley P. Culbertson
发明人： Thomas F. Mich , Townley P. Culbertson
IPC分类号： A61K31/47 , A61P31/04 , C07D207/09 , C07D207/14 , C07D207/26 , C07D207/277 , C07D455/04 , C07D487/10 , A01N43/42
CPC分类号： C07D207/277 , C07D207/09 , C07D207/14 , C07D455/04 , C07D487/10
摘要： Novel 10-amino-9-fluoro- and 9-fluoro-6,7-dihydro-5-methyl-1-oxo-8-(heterocyclyl)1H,5H-benzo (ij)-2-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：新的10-氨基-9-氟 - 和9-氟-6,7-二氢-5-甲基-1-氧代-8-（杂环基）1H，5H-苯并（ij）-2-羧酸作为抗菌剂是以及其制备，配制和用于治疗细菌感染的方法。

8. 发明授权

US4207320A Amino-substituted imidazo[1,2-a:3,4-a']diquinolin-15-ium salts compositions and method of use 失效
标题翻译：氨基取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐组合物和使用方法
公开(公告)号：US4207320A
公开(公告)日：1980-06-10
申请号：US937234
申请日：1978-08-28
申请人： David B. Capps , Mario M. Angelo , Townley P. Culbertson
发明人： David B. Capps , Mario M. Angelo , Townley P. Culbertson
IPC分类号： C07D215/04 , C07D215/18 , C07D215/26 , C07D471/14 , A61K31/535
CPC分类号： C07D215/04 , C07D215/18 , C07D215/26 , C07D471/14
摘要： Amino-substituted imidazo[1,2-a:3,4-a']diquinolin-15-ium salts having the formula I: ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, C.sub.4 -C.sub.6 cycloalkyl, di(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, 4-morpholinyl or 2,2-dimethylhydrazino;R.sub.2 is hydrogen, lower alkyl, lower alkylamino, di(lower alkyl)amino, C.sub.4 -C.sub.6 cycloalkylamino, lower alkoxy(lower alkyl)amino, 1-azetidinyl, 1-pyrrolidinyl, 1-piperidinyl, methyl-1-pyrrolidinyl, methyl-1-piperidinyl, hexahydro-1H-azepin-1-yl, 4-morpholinyl, benzylamino, N-methylbenzylamino or 2-phenylethylamino;R.sub.3 is hydrogen or methyl;X is an anion;with the proviso that at least one of R.sub.1 and R.sub.2 is other than hydrogen, lower alkyl or C.sub.4 -C.sub.6 cycloalkyl; and with the further proviso that when R.sub.2 is dimethylamino, at least one of R.sub.1 and R.sub.3 is other than hydrogen, and intermediates used in the preparation thereof are disclosed. The compounds of the invention are prepared by amination of the corresponding chloro or fluoro-substituted imidazo [1,2-a:3,4-a']diquinolin-15-ium salts; either the halo substituted intermediates or the amino substituted salts may be further treated, typically using ion exchange techniques to obtain a variety of physiologically acceptable amino-substituted [1,2-a:3,4-a']diquinolin-15-ium salts which exhibit antifungal activity.
摘要翻译：具有式I的氨基取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐其中R 1是氢，低级烷基，C 4 -C 6环烷基，二（低级烷基）氨基，1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基，甲基-1-吡咯烷基，甲基-1-哌啶基，4-吗啉基或2,2-二甲基肼; R2是氢，低级烷基，低级烷基氨基，二（低级烷基）氨基，C4-C6环烷基氨基，低级烷氧基（低级烷基）氨基，1-氮杂环丁烷基，1-吡咯烷基，1-哌啶基，甲基-1-吡咯烷基， 1-哌啶基，六氢-1H-吖庚因-1-基，4-吗啉基，苄基氨基，N-甲基苄基氨基或2-苯乙基氨基; R3是氢或甲基; X是阴离子; 条件是R 1和R 2中的至少一个不是氢，低级烷基或C 4 -C 6环烷基; 并且进一步的条件是当R 2是二甲基氨基时，R 1和R 3中的至少一个不是氢，并且公开了其制备中使用的中间体。本发明的化合物是通过胺化相应的氯或氟取代的咪唑并[1,2-a：3,4-a']二喹啉-15-盐制备的; 可以进一步处理卤代替中间体或氨基取代的盐，通常使用离子交换技术获得各种生理上可接受的氨基取代的[1,2-a：3,4-a']二喹啉-15-盐其具有抗真菌活性。

9. 发明授权

US5081254A Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US5081254A
公开(公告)日：1992-01-14
申请号：US538858
申请日：1990-06-15
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： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
CPC分类号： C07D207/08 , C07D207/09 , C07D207/12 , C07D207/20 , C07D211/34 , C07D211/52 , C07D211/70 , C07D215/56 , C07D401/04
摘要： A 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.
摘要翻译：描述了可用作抗菌剂的新一系列喹啉，萘啶和苯并恶嗪羧酸。还描述了制备化合物以及新型中间体的新方法，它们的制备方法及其在治疗细菌感染中的用途。

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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