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1. 发明授权

US5753648A Tricyclic benzazepine vasopressin antagonists 失效
公开(公告)号：US5753648A
公开(公告)日：1998-05-19
申请号：US672150
申请日：1996-06-27
申请人： Jay Donald Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
发明人： Jay Donald Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
IPC分类号： A61K31/00 , A61K31/495 , A61K31/4985 , A61K31/55 , A61K31/551 , A61K31/5513 , A61K31/5517 , A61P1/00 , A61P1/16 , A61P5/36 , A61P5/42 , A61P7/00 , A61P7/08 , A61P7/10 , A61P9/00 , A61P9/12 , A61P13/00 , A61P13/12 , A61P15/00 , A61P15/06 , A61P43/00 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14 , C07D487/12 , C07D513/00 , C07D515/00
CPC分类号： C07D487/04 , C07D471/14 , C07D487/14
摘要： Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.

2. 发明授权

US5700796A 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：US5700796A
公开(公告)日：1997-12-23
申请号：US671442
申请日：1996-06-27
申请人： Jay Donald Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
发明人： Jay Donald Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
IPC分类号： A61K31/495 , A61K31/55 , A61P1/16 , A61P7/08 , A61P9/00 , A61P9/12 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14
摘要： Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
摘要翻译：在V1和/或V2受体上表现出拮抗剂活性并表现出体内血管升压素拮抗剂活性的通式I的三环化合物：如图所示，其显示出体内血管加压素拮抗剂活性的拮抗剂活性，使用这些化合物治疗特征在于肾脏过度再吸收水的疾病的方法，以及制备此类化合物的方法。

3. 发明授权

US5536718A 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：US5536718A
公开(公告)日：1996-07-16
申请号：US373132
申请日：1995-01-17
申请人： Jay D. Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
发明人： Jay D. Albright , Aranapakam M. Venkatesan , John P. Dusza , Fuk-Wah Sum
IPC分类号： A61K31/495 , A61K31/55 , A61P1/16 , A61P7/08 , A61P9/00 , A61P9/12 , C07D471/04 , C07D471/14 , C07D487/04 , C07D487/14
CPC分类号： C07D471/14 , C07D487/04 , C07D487/14
摘要： Tricyclic compound of the general Formula I: ##STR1## as defined herein which exhibit antagonist activity at V.sub.1 and/or V.sub.2 receptors and exhibit in vivo vasopressin antagonist activity, methods for using such compounds in treating diseases characterized by excess renal reabsorption of water, and process for preparing such compounds.
摘要翻译：通式I的三环化合物：如本文所定义的在V1和/或V2受体上显示拮抗剂活性并显示体内血管加压素拮抗剂活性的式I化合物，使用这些化合物治疗特征在于过量肾脏重吸收水的疾病的方法，以及这些化合物的制备方法。

4. 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。

5. 发明授权

US06939870B2 Substituted-3-indolyl-4-piperidino-alkyl heterocycles for the treatment of depression 失效
公开(公告)号：US06939870B2
公开(公告)日：2005-09-06
申请号：US10652424
申请日：2003-08-29
申请人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
发明人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
IPC分类号： C07D401/14 , C07D471/04 , C07D417/14 , A61K31/53 , A61K31/549 , A61P25/24 , C07D403/14
CPC分类号： C07D401/14 , A61K31/4745 , A61K31/517 , A61K31/53 , A61K31/549 , C07D471/04
摘要： A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.

6. 发明授权

US06358980B1 Alkynyl containing hydroxamic acid compounds as matrix metalloproteinase/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/抑制剂
公开(公告)号：US06358980B1
公开(公告)日：2002-03-19
申请号：US09492686
申请日：2000-01-27
申请人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
发明人： Jeremy I. Levin , Aranapakam M. Venkatesan , James M. Chen , Arie Zask , Vincent P. Sandanayaka , Mila T. Du , Jannie L. Baker
IPC分类号： A61K31445
CPC分类号： C07D309/08 , A61K31/351 , A61K31/435 , A61K31/445 , A61K31/496 , C07D211/60 , C07D211/62 , C07D211/66
摘要： Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.
摘要翻译：下列化合物：可用于治疗关节炎，肿瘤转移，组织溃疡，创伤愈合异常，牙周病，骨病，糖尿病（胰岛素抵抗）和HIV感染。

7. 发明授权

US07332506B2 Substituted-3-indolyl-4-piperidino-alkyl heterocycles for the treatment of depression 失效
标题翻译：用于治疗抑郁症的取代的3-吲哚基-4-哌啶子基 - 烷基杂环
公开(公告)号：US07332506B2
公开(公告)日：2008-02-19
申请号：US11511150
申请日：2006-08-28
申请人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
发明人： Aranapakam M. Venkatesan , Jamie M. Davis , Yansong Gu
IPC分类号： A61K31/4375 , A61P25/24
CPC分类号： C07D401/14 , A61K31/4745 , A61K31/517 , A61K31/53 , A61K31/549 , C07D471/04
摘要： A compound represented by the formula I: wherein A represents the following heterocycles: and R1-9 are as defined herein, a composition containing this compound and methods for treating disorders of the serotonin-affected neurological systems utilizing such a compound or composition.
摘要翻译：由式I表示的化合物：其中A表示以下杂环：R 1〜9 - 如本文所定义，含有该化合物的组合物和用于治疗血清素受影响的神经系统的疾病的方法利用这样的化合物或组合物。

8. 发明授权

US07276611B2 Process for synthesizing beta-lactamase inhibitor intermediates 失效
标题翻译： β-内酰胺酶抑制剂中间体的合成方法
公开(公告)号：US07276611B2
公开(公告)日：2007-10-02
申请号：US10844243
申请日：2004-05-12
申请人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
发明人： Michael William Winkley , Anita Wai-Yin Chan , Ivo L. Jirkovsky , Kenneth Alfred Martin Kremer , Joseph Zeldis , Antonia Aristotelevna Nikitenko , Henry Lee Strong , Tarek Mansour , Gulnaz Khafizova , Aranapakam M. Venkatesan
IPC分类号： C07D231/54
CPC分类号： C07D498/04 , C07D487/04
摘要： There is provided a process for the preparation of bicyclicheteroaryl carboxaldehydes having the structural Formula I where X and Y are defined in the specification The bicyclic heteroaryl carboxaldehydes are useful as intermediates in the preparation of β-lactamase inhibitors.
摘要翻译：提供了一种制备具有结构式I的双环杂芳基羧醛的方法，其中X和Y在说明书中定义。双环杂芳基羧醛可用作制备β-内酰胺酶抑制剂的中间体。

9. 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。

10. 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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