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1. 发明申请

WO1991016327A1 ANTIMICROBIAL QUINOLONYL LACTAMS 审中-公开
标题翻译：抗微生物喹诺酮类LACTAMS
公开(公告)号：WO1991016327A1
公开(公告)日：1991-10-31
申请号：PCT/US1991002476
申请日：1991-04-12
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D501/28
CPC分类号： C07D477/14 , C07D477/20 , C07D499/00 , C07D499/88 , C07D501/00
摘要： Antimicrobial quinolonyl lactam compounds comprising a lactam-containing moiety linked to a quinolone moiety, of formula (I), wherein (1) A , A , A , R , and R generally form any of a variety of quinolone, naphthyridine or related cyclic moieties known in the art to have antimicrobial activity; and (2) R is part of a linking moiety, linking hte quinolone moiety to a lactam-containing moiety having formula (II), wherein (3) R , R , R , R , and R , 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, ester, thioester, amide, and hydrazide groups.
摘要翻译：包含与式（I）的喹诺酮部分连接的含内酰胺部分的抗微生物喹诺酮内酰胺化合物，其中（1）A 1，A 2，A 3，R 1和R 4 >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 6是连接部分的一部分，将喹诺酮部分与具有式（II）的含内酰胺部分连接，其中（3）R 10，R 11，R 12， R 13和R 14与键“a”和“b”一起形成本领域已知的具有抗微生物活性的各种含内酰胺的部分; 连接部分包括（例如）氨基甲酸酯，二硫代氨基甲酸酯，脲，硫脲，异脲，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，酯，硫酯，酰胺和酰肼基团。

2. 发明申请

WO1990004595A1 NOVEL ANTIMICROBIAL FLUOROQUINOLONYL CEPHEMS 审中-公开
标题翻译：新型抗微生物氟代喹啉CEPHEMS
公开(公告)号：WO1990004595A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004768
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D501/48
CPC分类号： C07D501/34 , C07D501/26
摘要： Antimicrobial fluoroquinolonyl cephems of formula (I), wherein (1) R?1 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 unsubstitued piperazine, 3-aminopyrrolidine, or 3-aminomethylpyrrolidine. R4 is preferably hydrogen or halogen.

3. 发明申请

WO1990004591A1 NOVEL ANTIMICROBIAL DITHIOCARBAMOYL QUINOLONES 审中-公开
标题翻译：新型抗微生物二硫代喹啉喹诺酮
公开(公告)号：WO1990004591A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004806
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D401/04
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 general formula (I), wherein A?1, 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 R1 is X, R3 is X, or both R?1 and R3¿ are X; and X is -R?15-N(R16)(R17) or -R15-R18-N(R19)(R17¿), where R15 is nil, alkyl, a carbocyclic ring, or a heterocyclic ring; and R16 is hydrogen, alkyl, alkenyl, a carbocyclic ring, a heterocyclic ring; or when X is R?15-N(R16)(R17), R16 and R15¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?15 and R16¿ are bonded; R17 is C(=S)-S-M, where M is a pharmaceutically acceptable salt or biohydrolyzable ester; and R18 is alkyl, a carbocyclic ring, or a heterocyclic ring; and R19 is hydrogen, alkyl, alkenyl, a carbocyclic ring, a heterocyclic ring; or R?18 and R19¿ may together comprise a heterocyclic ring including the nitrogen atom to which R?18 and R19¿ are bonded; and pharmaceutically-acceptable salts and biohydrolyzable esters thereof, and hydrates thereof.

4. 发明申请

WO1992014474A1 METHODS FOR THE TREATMENT OF OSTEOPOROSIS 审中-公开
标题翻译：治疗骨质疏松症的方法
公开(公告)号：WO1992014474A1
公开(公告)日：1992-09-03
申请号：PCT/US1992000854
申请日：1992-01-31
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , McOSKER, Jocelyn, Elaine
IPC分类号： A61K31/66
CPC分类号： A61K31/66 , A61K31/565 , A61K2300/00
摘要： Methods of treatment for osteoporosis in a human or other animal subject, comprising: administering a bone-active phosphonate to said subject, at a level of at least about 0.1 LED per day of said treatment; and administering an estrogen hormone to said subject at a level of from about 0.2 to about 0.8 LED per day of said treatment. The bone-active phosphonate is preferably a bisphosphonate, or a phosphonoalkyl phosphonate.
摘要翻译：治疗人或其他动物受试者的骨质疏松症的方法，包括：以所述治疗的每天至少约0.1LL的水平向所述受试者施用骨 - 活性膦酸盐; 并且以所述治疗的每天约0.2至约0.8L LED的水平向所述受试者施用雌激素。骨活性膦酸盐优选为双膦酸盐或膦酰基烷基膦酸盐。

5. 发明申请

WO1990004594A1 NOVEL ANTIMICROBIAL QUINOLONYL LACTAM ESTERS 审中-公开
标题翻译：新型抗微生物喹诺酮乳酸酯
公开(公告)号：WO1990004594A1
公开(公告)日：1990-05-03
申请号：PCT/US1989004803
申请日：1989-10-24
申请人： NORWICH EATON PHARMACEUTICALS, INC.
发明人： NORWICH EATON PHARMACEUTICALS, INC. , DEMUTH, Thomas, Prosser, Jr. , WHITE, Ronald, Eugene
IPC分类号： C07D489/00
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 formula (I), wherein (1) R?3, R4, and R5¿, 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, R7, and R8¿ form any of a variety of quinolone or napthyridine structures similar to those known in the art to have antimicrobial activity.

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