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1. 发明公开

EP0366193A2 Novel antimicrobial quinolonyl lactams 失效
标题翻译：新型抗菌喹诺酮内酰胺
公开(公告)号：EP0366193A2
公开(公告)日：1990-05-02
申请号：EP89202646.9
申请日：1989-10-19
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
IPC分类号： C07D499/88 , C07D519/00 , C07D487/04 , C07D401/12 , C07D471/04 , C07D501/20 , C07D513/04 , C07D417/14 , C07D498/047 , C07D401/14 , C07D499/84
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14 , C07D463/12 , C07D463/20 , C07D463/22 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula:
wherein

(1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties similar to those known in the art to have antimicrobial activity;
(2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity; and
(3) Y, together with R 5 , form a variety of non-ester linking moieties between the lactam-containing moiety and the quinolone moiety.
摘要翻译：抗菌喹诺酮内酰胺化合物，其包含通过非酯连接部分连接至喹诺酮部分的3-羧基的含内酰胺部分。这些化合物具有下式：其中（1）R 3，R 4和R 5与键“a”和“b”一起形成多种类似于本领域已知的具有抗微生物活性的含内酰胺部分 ; （2）A，R 6，R 7和R 8形成与本领域已知的具有抗微生物活性的那些类似的各种喹诺酮或萘啶结构中的任一种; 和（3）Y与R5一起在含内酰胺部分和喹诺酮部分之间形成各种非酯连接部分。

2. 发明公开

EP0366189A3 Novel antimicrobial lactam-quinolones 失效
标题翻译：新型抗微生物乳酸
公开(公告)号：EP0366189A3
公开(公告)日：1992-01-02
申请号：EP89202635.2
申请日：1989-10-18
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： White, Ronald Eugene , Demuth, Thomas Prosser, Jr.
IPC分类号： C07D501/20 , C07D519/00 , C07D401/12 , C07D498/047 , C07D477/00 , C07D463/00 , C07D498/053 , C07D499/88 , C07D499/84 , C07D513/04 , C07D487/04
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D463/18 , C07D463/22 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula: wherein
( 1 ) A', A 2 , A3, R 1 , R 4 and R 6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have animicrobial activity; and (2) R' or R 3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula:
wherein (3) R 10 , R 11 , R 12 , R 13 , and R 14 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and (4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphone, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.

3. 发明公开

EP0366641A3 Novel antimicrobial quinolonyl lactam esters 失效转让
标题翻译：新型抗微生物蛋黄酱乳酪
公开(公告)号：EP0366641A3
公开(公告)日：1991-12-11
申请号：EP89870152.9
申请日：1989-10-20
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： White, Ronald Eugene , Demuth, Thomas Prosser, Jr.
IPC分类号： C07D499/88 , C07D519/00 , C07D477/00 , C07D487/04 , C07D498/047 , C07D498/053 , C07D463/00 , C07D513/04 , C07D417/14 , C07D401/12 , C07D499/84
CPC分类号： C07D401/12 , C07D417/14 , C07D463/18 , C07D477/10 , C07D487/04 , C07D499/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula:
wherein
(1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and (2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.

4. 发明公开

EP0366640A3 Novel antimicrobial fluoroquinolonyl cephems 失效转让
标题翻译：新型抗微生物氟代喹啉CEPHEMS
公开(公告)号：EP0366640A3
公开(公告)日：1992-01-02
申请号：EP89870151.1
申请日：1989-10-20
申请人： Norwich-Eaton Pharmaceuticals, Inc.
发明人： Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
IPC分类号： C07D501/26 , A61K31/545
CPC分类号： C07D501/34 , C07D501/26
摘要： Antimicrobial fluoroquinolonyl cephems of the formula:
wherein
(1) R¹ and R² are groups among those known in the art for substitution at the 7-position of an antimicrobially-active cephem; (2) R³ is a substituted or unsubstituted, nitrogen-containing, heterocyclic moiety; and (3) R⁴ is hydrogen, halogen, lower alkoxy or cyclic alkoxy, amino, nitro or cyano. Preferably, R³ is substituted or unsubstituted piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R⁴ is preferably hydrogen or halogen.

5. 发明授权

EP0366641B1 Novel antimicrobial quinolonyl lactam esters 失效转让
标题翻译：新型抗菌喹诺酮内酰胺酯
公开(公告)号：EP0366641B1
公开(公告)日：2000-07-05
申请号：EP89870152.9
申请日：1989-10-20
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： White, Ronald Eugene , Demuth, Thomas Prosser, Jr.
IPC分类号： C07D499/88 , C07D519/00 , C07D477/00 , C07D487/04 , C07D503/00 , C07D505/00 , C07D463/00 , C07D513/04 , C07D417/14 , C07D401/12 , C07D499/87
CPC分类号： C07D401/12 , C07D417/14 , C07D463/18 , C07D477/10 , C07D487/04 , C07D499/00 , C07D505/00 , C07D513/04

6. 发明公开

EP0366643A2 Novel antimicrobial dithiocarbamoyl quinolones 失效
标题翻译： Antimikrobielle二硫代氨基甲酰喹诺酮。
公开(公告)号：EP0366643A2
公开(公告)日：1990-05-02
申请号：EP89870161.0
申请日：1989-10-24
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
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
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D503/00 , C07D505/00 , C07D513/04
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.
摘要翻译：其中（1）A 1，A 2，A 3，R 1，R 3，R 4和R 6中的至少一个具有下列通式的抗微生物二硫代氨基甲酰喹诺酮化合物：形成与本领域已知的具有抗微生物活性的各种喹诺酮和相关杂环结构中的任何一种; 和（2）（1）R 1是X，R 3是X，或者R 1和R 3都是X; 和（2）X是-R 1 - 5（R 1）6）（R 1）7或-R 1 - 5 -R 1 其中（a）（1）R 1为未取代的烷基，碳环或杂环; R 1，R 2，和（2）R 1是氢; 烷基; 烯基; 碳环杂环; 或（3）当X为R 1 -5（-N 1 R 6）（R 1）7），R 1和R 5为5时，可以一起包含包含R 1和R 5之间的氮原子的杂环键合; （b）R 1是C（= S）-S-M，其中M是药学上可接受的盐或可生物水解的酯; 和（c）（1）R 1 8是烷基，碳环或杂环; 和（2）R 1 <9>是氢; 烷基; 烯基; 碳环杂环; 或（3）R 1 8和R 9可以一起包含包含R 1和R 3的氮原子的杂环键合; 及其药学上可接受的盐和生物可水解的酯，及其水合物。

7. 发明公开

EP0366641A2 Novel antimicrobial quinolonyl lactam esters 失效转让
标题翻译：新型抗菌喹诺酮内酰胺酯
公开(公告)号：EP0366641A2
公开(公告)日：1990-05-02
申请号：EP89870152.9
申请日：1989-10-20
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： White, Ronald Eugene , Demuth, Thomas Prosser, Jr.
IPC分类号： C07D499/88 , C07D519/00 , C07D477/00 , C07D487/04 , C07D498/047 , C07D498/053 , C07D463/00 , C07D513/04 , C07D417/14 , C07D401/12 , C07D499/84
CPC分类号： C07D401/12 , C07D417/14 , C07D463/18 , C07D477/10 , C07D487/04 , C07D499/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolonyl lactam esters comprising a lactam-containing moiety linked, by an ester group, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula:
wherein

(1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form certain lactam-containing moieties similar to those known in the art to have antimicrobial activity; and
(2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.
摘要翻译：包含通过酯基连接到喹诺酮部分的3-羧基的含内酰胺部分的抗微生物喹诺酮内酯。这些化合物具有下式：其中（1）R 3，R 4和R 5与键“a”和“b”一起形成某些类似于本领域已知的具有抗微生物活性的含内酰胺部分; 和（2）A，R6，R7和R8形成与本领域已知的具有抗微生物活性的那些类似的各种喹诺酮或萘啶结构中的任一种。

8. 发明公开

EP0366189A2 Novel antimicrobial lactam-quinolones 失效
标题翻译： Antimikrobielle Lactam-Quinolone。
公开(公告)号：EP0366189A2
公开(公告)日：1990-05-02
申请号：EP89202635.2
申请日：1989-10-18
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： White, Ronald Eugene , Demuth, Thomas Prosser, Jr.
IPC分类号： C07D501/20 , C07D519/00 , C07D401/12 , C07D498/047 , C07D477/00 , C07D463/00 , C07D498/053 , C07D499/88 , C07D499/84 , C07D513/04 , C07D487/04
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D463/18 , C07D463/22 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D501/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial lactam-quinolone compounds comprising a lactam-containing moiety linked to a quinolone moiety, of the formula:
wherein

( 1 ) A', A 2 , A3, R 1 , R 4 and R 6 generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have animicrobial activity; and
(2) R' or R 3 contain a linking moiety, linking the quinolone moiety to a lactam-containing moiety having the formula:
wherein
(3) R 10 , R 11 , R 12 , R 13 , and R 14 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties known in the art to have antimicrobial activity; and
(4) the linking moiety includes (for example) carbamate, dithiocarbamate, urea, thiourea, isouronium, isothiouronium, guanidine, carbonate, trithiocarbonate, reversed carbamate, xanthate, reversed isouronium, reversed dithiocarbamate, reversed isothiouronium, amine, imine, ammonium, heteroarylium, ether, thioether, phosphone, phosphoramide, phosphate, sulfonamide, ester, thioester, amide, and hydrazide groups.
摘要翻译：包含与喹诺酮部分连接的含内酰胺部分的抗微生物内酰胺 - 喹诺酮化合物，其具有下式：其中（1）A 1，A 2，A 3，R 1， 4＆gt;和R 6通常形成本领域已知的各种喹诺酮，萘啶或相关的环状部分以具有抗微生物活性; 和（2）R 1或R 3含有连接部分，将喹诺酮部分与具有下式的含内酰胺的部分连接：其中（3）R 1，R 1 > 1，R 1，R 2，R 1，R 3和R 4与键“a”和“b”一起形成各种含内酰胺本领域已知的具有抗微生物活性的部分; 连接部分包括（例如）氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异嘌呤，异硫脲，胍，碳酸酯，三硫代碳酸酯，反相氨基甲酸酯，黄原酸酯，反式异卤素，反式二硫代氨基甲酸酯，反式异硫脲，胺，亚胺，杂芳基，醚，硫醚，膦，磷酰胺，磷酸酯，磺酰胺，酯，硫酯，酰胺和酰肼基。

9. 发明公开

EP0366193A3 Novel antimicrobial quinolonyl lactams 失效
标题翻译：新型抗微生物喹诺酮类LACTAMS
公开(公告)号：EP0366193A3
公开(公告)日：1992-01-08
申请号：EP89202646.9
申请日：1989-10-19
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
IPC分类号： C07D499/88 , C07D519/00 , C07D487/04 , C07D401/12 , C07D471/04 , C07D501/20 , C07D513/04 , C07D417/14 , C07D498/047 , C07D401/14 , C07D499/84
CPC分类号： C07D401/12 , C07D401/14 , C07D417/14 , C07D463/12 , C07D463/20 , C07D463/22 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D503/00 , C07D505/00 , C07D513/04
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked, by a non-ester linking moiety, to the 3-carboxy group of a quinolone moiety. These compounds are of the formula:
wherein
(1) R 3 , R 4 , and R 5 , together with bonds "a" and "b", form any of a variety of lactam-containing moieties similar to those known in the art to have antimicrobial activity; (2) A, R 6 , R 7 , and R 8 form any of a variety of quinolone or naphthyridine structures similar to those known in the art to have antimicrobial activity; and (3) Y, together with R 5 , form a variety of non-ester linking moieties between the lactam-containing moiety and the quinolone moiety.

10. 发明公开

EP0366643A3 Novel antimicrobial dithiocarbamoyl quinolones 失效
标题翻译：新型抗微生物二硫代喹啉喹诺酮类
公开(公告)号：EP0366643A3
公开(公告)日：1991-12-04
申请号：EP89870161.0
申请日：1989-10-24
申请人： Norwich Eaton Pharmaceuticals, Inc.
发明人： Demuth, Thomas Prosser, Jr. , White, Ronald Eugene
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
CPC分类号： C07D401/04 , C07D215/56 , C07D401/12 , C07D401/14 , C07D417/14 , C07D455/04 , C07D471/04 , C07D477/10 , C07D487/04 , C07D499/00 , C07D503/00 , C07D505/00 , C07D513/04
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.

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