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1. 发明授权

US6140318A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US6140318A
公开(公告)日：2000-10-31
申请号：US168622
申请日：1998-10-08
申请人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
IPC分类号： A61P31/06 , C07D487/04 , A61K31/395 , A01N43/60 , C07D413/00 , C07D487/00
CPC分类号： C07D487/04
摘要： Compounds of formula I are disclosed. ##STR1## as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B.The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
摘要翻译：公开了式I化合物。以及其药学上可接受的盐。萘磺叠胺被包括至少一个阳离子基团-A-Q-L-B的各种取代基取代。本发明的碳青霉烯类药物对抗敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

2. 发明授权

US06399597B1 1,8-naphthosultamylmethyl carbapenem antibacterial compounds, compositions containing such compounds and methods treatment 失效
标题翻译： 1,8-萘磺酰甲基碳青霉烯类抗菌化合物，含有这些化合物的组合物和方法处理
公开(公告)号：US06399597B1
公开(公告)日：2002-06-04
申请号：US09531994
申请日：2000-03-20
申请人： Lovji D. Cama , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger , Wanying Sun
IPC分类号： C07D47714
CPC分类号： C07D487/04
摘要： Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group —A—Q—L—B. The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
摘要翻译：公开了式I的化合物以及其药学上可接受的盐。萘磺隆被各种取代基取代，包括至少一个阳离子基团-AQLB。本发明的碳青霉烯类对敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

3. 发明授权

US06294529B1 Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06294529B1
公开(公告)日：2001-09-25
申请号：US09421690
申请日：1999-10-07
申请人： Lovji D. Cama , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger , Wanying Sun
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I are disclosed. as well as pharmaceutically acceptable salts thereof. The naphthosultam is substituted with various substituent groups including at least one cationic group -A-Q-L-B, wherein A-Q-L-B represents a side chain wherein: A is a C1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of —O—, —S—, NRa—, —C(O)— and —CH═CH—; Q represents in which: b is 2 or 3; and X− is a charge balancing group; L represents a C1-8 alkylene group, unsubstituted or substituted with 1-3 Rc groups, and is interrupted or terminated by 1-3 of —CH═CH—, —C(O)—, —C(O)NRd—, —Het(Re)—, —C(O)—Het(Re)—, —C(O)NRa—Het(Re)—, —O—,—S—, —S(O)—, —SO2—, —CO2—, NRa—, —N+(Ra)2— B represents The carbapenems of the invention are effective against susceptible bacterial organisms, including methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
摘要翻译：公开了式I的化合物以及其药学上可接受的盐。萘并磺胺被包括至少一个阳离子基团-AQLB的各种取代基取代，其中AQLB表示侧链，其中：A是直链或支链的C1-6亚烷基，并且任选地被1-2的-O-O - ， - S - ，NR a - ， - C（O） - 和-CH = CH-; Q表示其中：b为2或3; X为电荷平衡基团; L为C1-8亚烷基并且被1-3个R c基团取代，并被1-3个-CH = CH-，-C（O） - ， - C（O）NR d - ， - H（Re） - ， - C（O）-Het（Re） - ， - C（O）NR a -Het（Re） - ， - O - ， - S - ， - S（O） - ， - SO 2 - ， - -N +（Ra）2-B代表本发明的碳青霉烯类对敏感细菌生物有效，包括耐甲氧西林金黄色葡萄球菌（MRSA），耐甲氧西林葡萄球菌（MRSE）和耐甲氧西林凝固酶阴性葡萄球菌（MRCNS）。

4. 发明授权

US5994345A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5994345A
公开(公告)日：1999-11-30
申请号：US168419
申请日：1998-10-08
申请人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
发明人： Lovji D. Cama , Robert R. Wilkening , Ronald W. Ratcliffe , Kenneth J. Wildonger , Wanying Sun
IPC分类号： C07D477/14 , C07D521/00 , A61K31/395 , A61K31/695 , C07D519/00
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14
摘要： Carbapenems substituted with a naphthosultam at position 2 and linked through a CH.sub.2 group are disclosed. Pharmaceutical compositions and methods of treatment are also included. The naphthosultam is substituted with at least one cationic group --A--Q--L--B. ##STR1## A--Q--L--B represents a side chain wherein in part: A is a C.sub.1-6 alkylene group, straight or branched, and optionally interrupted or terminated by 1-2 of --O--, --S--, NR.sup.a --, --C(O)-- and CH.dbd.CH--Q is ##STR2## L represents a C.sub.1-8 alkylene group, straight or branched, and unsubstituted or substituted with 1-3 R.sup.c groups andB represents ##STR3## The carbapenems of the present invention are useful against gram positive microorganisms, especially methicillin resistant Staphylococci.
摘要翻译：公开了在位置2被萘并磺隆取代并通过CH2基团连接的碳青霉烯。还包括药物组合物和治疗方法。萘磺酸钠被至少一个阳离子基团-A-Q-L-B取代。 AQLB表示侧链，其中部分是：A是直链或支链的C1-6亚烷基，并且任选地被1-2，-O - ， - NR - ， - C（O） - 或 CH = CH-Q是L表示直链或支链的未取代或被1-3个Rc基团取代的C 1-8亚烷基，B表示本发明的碳青霉烯类可用于革兰氏阳性微生物，特别是耐甲氧西林葡萄球菌。

5. 发明授权

US07087599B2 Estrogen receptor modulators 有权
公开(公告)号：US07087599B2
公开(公告)日：2006-08-08
申请号：US09782855
申请日：2001-02-14
申请人： Dann LeRoy Parker, Jr. , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger
发明人： Dann LeRoy Parker, Jr. , Ronald W. Ratcliffe , Robert R. Wilkening , Kenneth J. Wildonger
IPC分类号： A61K31/535 , A61K31/12 , C07D295/00 , C07C251/18 , C07C49/225
CPC分类号： C07D295/088 , C07C39/42 , C07C45/28 , C07C45/46 , C07C45/63 , C07C45/65 , C07C45/68 , C07C45/69 , C07C45/71 , C07C45/72 , C07C45/73 , C07C45/74 , C07C45/75 , C07C49/747 , C07C49/755 , C07C59/90 , C07C205/45 , C07C251/44 , C07C255/47 , C07C2603/18 , C07D333/22 , C07C49/84
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.

6. 发明授权

US5496816A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5496816A
公开(公告)日：1996-03-05
申请号：US359770
申请日：1994-12-20
申请人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
发明人： Timothy A. Blizzard , Ronald W. Ratcliffe , Sherman T. Waddell , Sandra P. Szumiloski , Robert R. Wilkening , Kenneth J. Wildonger
IPC分类号： C07D477/00 , A61K31/397 , A61K31/42 , A61K31/425 , A61K31/495 , A61P31/04 , C07D477/20 , A61K31/40 , C07D487/04
CPC分类号： C07D477/20
摘要： Carbapenems of the formula: ##STR1## are disclosed as useful antibacterial agents. Pharmaceutical compositions and methods of use are also disclosed.
摘要翻译：以下公式的碳青霉烯类似物：作为有用的抗菌剂被公开。还公开了药物组合物和使用方法。

7. 发明授权

US06291448B1 Carbapenem antibacterial compounds, compositions containing such compounds and method of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US06291448B1
公开(公告)日：2001-09-18
申请号：US09338640
申请日：1999-06-23
申请人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
发明人： Timothy A. Blizzard , Robert R. Wilkening , Ronald W. Ratcliffe
IPC分类号： C07D47714
CPC分类号： C07D477/14
摘要： Compounds of formula I: as well as pharmaceutically acceptable salts thereof useful as carbapenam antibacterial agents are disclosed wherein X is CR2R2, NR2, or O.
摘要翻译：公开了式I化合物及其可药用盐作为碳青霉烯抗菌剂，其中X为CR2R2，NR2或O.

8. 发明授权

US5985844A Homoerythromycin A derivatives modified at the 4"-and 8A-positions 失效
标题翻译：在4“和8A位修饰的红霉素A衍生物
公开(公告)号：US5985844A
公开(公告)日：1999-11-16
申请号：US855242
申请日：1992-03-26
申请人： James V. Heck , William J. Leanza , Ronald W. Ratcliffe , Thomas N. Salzmann , Kothandaraman Shankaran , Michael J. Szymonifka , Robert R. Wilkening
发明人： James V. Heck , William J. Leanza , Ronald W. Ratcliffe , Thomas N. Salzmann , Kothandaraman Shankaran , Michael J. Szymonifka , Robert R. Wilkening
IPC分类号： C07H17/08
CPC分类号： C07H17/08
摘要： Compounds of the formula: ##STR1## where R is hydrogen, hydroxyl, alkyl or acyl, R' and R" together are oxo, hydroxyimino or alkoxyimino, and R' and R" independently are hydrogen, hydroxyl, acyloxy, or amino substituted by any of hydrogen, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, alkoxycarbonyl, aralkoxycarbonyl, alkylsulfonyl or arylsulfonyl, and n is 0 or 1, and the pharmaceutically acceptable salts thereof. The compounds are macrolide antibiotics and are also useful as intermediates to the synthesis of other macrolide antibiotics. Pharmaceutical compositions and methods of their use are also provided for.
摘要翻译：下式的化合物：其中R是氢，羟基，烷基或酰基，R'和R“一起是氧代，羟基亚氨基或烷氧基亚氨基，R'和R”独立地是氢，羟基，酰氧基或被任何的氢，烷基羰基，芳基羰基，芳烷基羰基，烷氧基羰基，芳烷氧基羰基，烷基磺酰基或芳基磺酰基，n为0或1，及其药学上可接受的盐。这些化合物是大环内酯类抗生素，也可用作合成其他大环内酯抗生素的中间体。还提供了其使用的药物组合物和方法。

9. 发明授权

US07432284B2 Estrogen receptor modulators 有权
标题翻译：雌激素受体调节剂
公开(公告)号：US07432284B2
公开(公告)日：2008-10-07
申请号：US10528008
申请日：2003-09-15
申请人： Dann LeRoy Parker , Robert R. Wilkening , Dongfang Meng , Ronald W. Ratcliffe
发明人： Dann LeRoy Parker , Robert R. Wilkening , Dongfang Meng , Ronald W. Ratcliffe
IPC分类号： A61K31/445 , A61K31/122 , C07D211/06 , C07C49/115
CPC分类号： C07C255/56 , C07C45/28 , C07C45/46 , C07C45/63 , C07C45/676 , C07C45/68 , C07C45/73 , C07C49/747 , C07C49/755 , C07C255/47 , C07C2603/30 , C07C47/575
摘要： The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, metastatic bone disease, Pagets disease, periodontal disease, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
摘要翻译：本发明涉及其化合物及其衍生物，其合成及其作为雌激素受体调节剂的用途。本发明的化合物是雌激素受体的配体，因此可用于治疗或预防与雌激素功能相关的各种病症，包括：骨丢失，骨折，骨质疏松症，转移性骨病，佩吉特氏病，牙周病，软骨变性，子宫内膜异位症，子宫肌瘤疾病，潮热，LDL胆固醇水平升高，心血管疾病，认知功能障碍，脑退行性疾病，再狭窄，男子乳腺发育不良，血管平滑肌细胞增殖，肥胖症，失禁和癌症，特别是乳房，子宫和前列腺。

10. 发明授权

US5756725A Carbapenem antibacterial compounds, compositions containing such compounds and methods of treatment 失效
标题翻译：碳青霉烯抗菌化合物，含有这些化合物的组合物和治疗方法
公开(公告)号：US5756725A
公开(公告)日：1998-05-26
申请号：US825786
申请日：1997-04-08
申请人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
发明人： Robert R. Wilkening , Ronald W. Ratcliffe , Timothy A. Blizzard
IPC分类号： C07D20060101 , C07D477/14 , C07D519/00 , C07D521/00 , C07D487/04 , A61K31/395
CPC分类号： C07D231/12 , C07D233/56 , C07D249/08 , C07D477/14
摘要： The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2-position with a naphthosultam linked through a CH.sub.2 group. The naphthosultam is further substituted with various substituent groups including at least one cationic group. The compounds are represented by formula I: ##STR1## Pharmaceutical compositions and methods of use are also included.
摘要翻译：本发明涉及碳青霉烯类抗菌剂，其中碳青霉烯核在2-位被用CH2链连接的萘磺酰胺代替。萘磺叠胺进一步被包括至少一个阳离子基团的各种取代基取代。化合物由式I表示：还包括药物组合物和使用方法。

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