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1. 发明授权

US06825354B2 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and TACE inhibitors 失效
标题翻译：含有异羟肟酸的炔基作为基质金属蛋白酶和TACE抑制剂
公开(公告)号：US06825354B2
公开(公告)日：2004-11-30
申请号：US10055502
申请日：2001-11-13
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
IPC分类号： C07D21172
CPC分类号： C07D209/48 , C07C317/44 , C07C317/50 , C07C323/60 , C07C2601/14 , C07D207/34 , C07D213/56 , C07D215/48 , C07D215/54 , C07D217/26 , C07D295/088 , C07D309/04 , C07D311/84 , C07D333/20 , C07D333/60 , C07D335/02
摘要： Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：该化合物可用于治疗由TNF-α介导的疾病状况，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化，克罗恩病和退行性软骨损失。

2. 发明授权

US06340691B1 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase and tace inhibitors 失效
标题翻译：含有异羟肟酸化合物的炔基作为基质金属蛋白酶和抑制剂
公开(公告)号：US06340691B1
公开(公告)日：2002-01-22
申请号：US09492977
申请日：2000-01-27
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , Derek C. Cole , James M. Chen , Jamie M. Davis , George T. Grosu
IPC分类号： C07D21140
CPC分类号： C07D209/48 , C07C317/44 , C07C317/50 , C07C323/60 , C07C2601/14 , C07D207/34 , C07D213/56 , C07D215/48 , C07D215/54 , C07D217/26 , C07D295/088 , C07D309/04 , C07D311/84 , C07D333/20 , C07D333/60 , C07D335/02
摘要： Compounds of the formula are useful in treating disease conditions mediated by TNF-&agr;, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease and degenerative cartilage loss.
摘要翻译：该化合物可用于治疗由TNF-α介导的疾病状况，例如类风湿性关节炎，骨关节炎，败血症，AIDS，溃疡性结肠炎，多发性硬化，克罗恩病和退行性软骨损失。

3. 发明授权

US5914339A Substituted 1,3-benzodioxoles 失效
标题翻译：取代的1,3-苯并二恶烷
公开(公告)号：US5914339A
公开(公告)日：1999-06-22
申请号：US854199
申请日：1997-05-09
申请人： Fuk-Wah Sum , Adam M. Gilbert , George T. Grosu , Michael S. Malamas , Aranapakam M. Venkatesan , Gerardo D. Francisco
发明人： Fuk-Wah Sum , Adam M. Gilbert , George T. Grosu , Michael S. Malamas , Aranapakam M. Venkatesan , Gerardo D. Francisco
IPC分类号： C07D317/68 , C07D413/06 , A61K31/42 , A61K31/36 , C07D263/06 , C07D317/58
CPC分类号： C07D413/06 , C07D317/68
摘要： The present invention provides new compounds having anti-diabetic and/or antihyperglycemia and/or anti-obesity activity, as well as pharmaceutical compositions and methods of treatment utilizing the compounds and processes for making the compounds, the compounds having the formula (II): ##STR1## wherein: R.sub.1 and R.sub.6 are independently hydrogen, C.sub.1 to C.sub.6 alkyl, trifluoromethyl, cyano, C.sub.1 to C.sub.6 alkoxy, or halogen;R.sub.2 is hydrogen or C.sub.1 to C.sub.6 trialkylsilyl;R.sub.3 is hydrogen or C.sub.1 to C.sub.6 alkoxycarbonyl;or R.sub.2 and R.sub.3 are joined to form a ring: ##STR2## wherein R' is hydrogen, C.sub.1 to C.sub.6 alkyl, or aryl; R.sub.4 and R.sub.5 are independently hydrogen or C.sub.1 to C.sub.6 alkyl;R.sub.7 and R.sub.8 are independently OR.sub.9 or NR.sub.10 R.sub.11 ;R.sub.9 is hydrogen, C.sub.1 to C.sub.12 alkyl, C.sub.1 to C.sub.12 cycloalkyl, C.sub.1 to C.sub.12 silylalkyl, aryl, arylalkyl, alkoxyalkyl, heteroaryl, --CHR.sub.12 COOR.sub.13, --CHR.sub.12 C(O)R.sub.13, --CHR.sub.12 CONR.sub.1 R.sub.11, --CHR.sub.12 OCOOR.sub.13, or --CHR.sub.12 OC(O)R.sub.13, with the provision that R.sub.9 is not hydrogen in both R.sub.7 and R.sub.8 ;R.sub.10 and R.sub.11 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aralkyl, aryl, furanylalkyl, or alkoxycarbonylalkyl;R.sub.12 and R.sub.13 are independently hydrogen, C.sub.1 to C.sub.12 alkyl, aryl, or aralkyl; and the pharmaceutically acceptable salts thereof, the enantiomers thereof, the racemic mixtures thereof, and the diastereomeric mixtures thereof.
摘要翻译：本发明提供具有抗糖尿病和/或抗高血糖和/或抗肥胖活性的新化合物，以及利用该化合物的药物组合物和治疗方法以及制备该化合物的方法，具有式（II）的化合物：其中：R 1和R 6独立地为氢，C 1至C 6烷基，三氟甲基，氰基，C 1至C 6烷氧基或卤素; R2是氢或C1-C6三烷基甲硅烷基; R3是氢或C1-C6烷氧基羰基; 或R2和R3连接形成环：其中R'是氢，C1-C6烷基或芳基; R4和R5独立地是氢或C1-C6烷基; R7和R8独立地是OR9或NR10R11; R 9是氢，C 1至C 12烷基，C 1至C 12环烷基，C 1至C 12甲硅烷基烷基，芳基，芳基烷基，烷氧基烷基，杂芳基，-CHR 12 COOR 13，-CHR 12 C（O）R 13，-CHR 12 CONR1R 11，-CHR 12 COOOR 13或-CHR 12 OC（O）R 13 ，其中R7和R8中的R9不是氢; R 10和R 11独立地为氢，C 1至C 12烷基，芳烷基，芳基，呋喃基烷基或烷氧基羰基烷基; R 12和R 13独立地为氢，C 1至C 12烷基，芳基或芳烷基; 及其药学上可接受的盐，其对映异构体，其外消旋混合物及其非对映体混合物。

4. 发明授权

US5521173A Tricyclic benzazepine vasopressin antagonists 失效
标题翻译：三环苯并氮平加压素拮抗剂
公开(公告)号：US5521173A
公开(公告)日：1996-05-28
申请号：US373125
申请日：1995-01-17
申请人： Aranapakam M. Venkatesan , Jay D. Albright , George T. Grosu
发明人： Aranapakam M. Venkatesan , Jay D. Albright , George T. Grosu
IPC分类号： A61K31/495 , A61K31/55 , A61P1/16 , A61P11/00 , A61P13/02 , A61P15/00 , C07D487/04
CPC分类号： C07D487/04
摘要： Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.
摘要翻译：式I中的三环二氮杂：其中A，B，D，E，F，Y和Z在说明书中定义，化合物具有加压素和催产素拮抗剂活性。

5. 发明授权

US5780471A Tricyclic benzazepine vasopressin antagonists 失效
公开(公告)号：US5780471A
公开(公告)日：1998-07-14
申请号：US652198
申请日：1996-05-23
申请人： Aranapakam M. Venkatesan , Jay D. Albright , George T. Grosu
发明人： Aranapakam M. Venkatesan , Jay D. Albright , George T. Grosu
IPC分类号： A61K31/495 , A61K31/55 , A61P1/16 , A61P11/00 , A61P13/02 , A61P15/00 , C07D487/04 , A61K31/50 , C07D241/36 , C07D471/00
CPC分类号： C07D487/04
摘要： Tricyclic diazepines of the Formula I: ##STR1## wherein A, B, D, E, F, Y, and Z are defined in the specification which compounds have vasopressin and oxytocin antagonist activity.

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