公开(公告)号：US07759387B2

公开(公告)日：2010-07-20

申请号：US10574982

申请日：2004-09-30

申请人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V. S. V. Rao ,  Ravindra Dattatraya Gupte ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza

发明人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V. S. V. Rao ,  Ravindra Dattatraya Gupte ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza

IPC分类号： A61K31/40 ,  C07D209/44

CPC分类号： C07D401/06 ,  C07D209/46 ,  C07D413/04

摘要： This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.

摘要翻译： 本发明涉及通式（I）的新的稠合双环化合物：其中符号在本文中定义为含有化合物的药物组合物，制备化合物的方法，以及单独或与其它组合使用化合物的方法 治疗剂。 这些化合物是血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂，因此可用于抑制血小板聚集和治疗血栓性疾病和其它疾病。

公开(公告)号：US07964628B2

公开(公告)日：2011-06-21

申请号：US12795824

申请日：2010-06-08

申请人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V. S. V. Rao ,  Ravindra Dattatraya Gupte ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza

发明人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V. S. V. Rao ,  Ravindra Dattatraya Gupte ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza

IPC分类号： A61K31/40 ,  C07D209/44

CPC分类号： C07D401/06 ,  C07D209/46 ,  C07D413/04

摘要： This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.

摘要翻译： 本发明涉及通式（I）的新的稠合双环化合物：其中符号在本文中定义为含有化合物的药物组合物，制备化合物的方法，以及单独或与其它组合使用化合物的方法 治疗剂。 这些化合物是血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂，因此可用于抑制血小板聚集和治疗血栓性疾病和其它疾病。

公开(公告)号：US20100256161A1

公开(公告)日：2010-10-07

申请号：US12795824

申请日：2010-06-08

申请人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V.S.V Rao ,  Ravindra Dattatraya Gupte ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan

发明人： Bansi Lal ,  Ashok Kumar Gangopadhyay ,  Vadlamudi V.S.V Rao ,  Ravindra Dattatraya Gupte ,  Radha Bhaskar Panicker ,  Eleanor Pinto De Souza ,  Gopal Vishnu Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan

IPC分类号： A61K31/496 ,  A61P7/02 ,  A61P9/10 ,  A61P11/00 ,  A61P19/10 ,  A61P29/00 ,  A61P37/06 ,  A61P17/06 ,  A61P35/04 ,  A61P19/02 ,  A61K31/4035 ,  A61K31/454 ,  A61K31/4245

CPC分类号： C07D401/06 ,  C07D209/46 ,  C07D413/04

摘要： This invention relates to novel fused bicyclic compounds of the general formula (I): wherein the symbols are defined herein, to pharmaceutical compositions containing the compounds, processes for preparing the compounds, and to methods of using the compounds, alone or in combination with other therapeutic agents. The compounds are antagonists of the platelet glycoprotein IIb/IIIa fibrinogen receptor complex, and are therefore useful for the inhibition of platelet aggregation, and for the treatment of thrombotic diseases and other diseases.

摘要翻译： 本发明涉及通式（I）的新的稠合双环化合物：其中符号在本文中定义为含有化合物的药物组合物，制备化合物的方法，以及单独或与其它组合使用化合物的方法 治疗剂。 这些化合物是血小板糖蛋白IIb / IIIa纤维蛋白原受体复合物的拮抗剂，因此可用于抑制血小板聚集和治疗血栓性疾病和其它疾病。

公开(公告)号：US08163730B2

公开(公告)日：2012-04-24

申请号：US12854761

申请日：2010-08-11

申请人： Bansi Lal ,  Somesh Sharma ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Asha Kulkarni-Almeida ,  Sapna Parikh ,  Radha Bhaskar Panicker ,  Anagha Damre ,  Ravindra Gupte

发明人： Bansi Lal ,  Somesh Sharma ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Asha Kulkarni-Almeida ,  Sapna Parikh ,  Radha Bhaskar Panicker ,  Anagha Damre ,  Ravindra Gupte

IPC分类号： A61K31/554 ,  C07D281/16

CPC分类号： C07D327/02

摘要： Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.

摘要翻译： 公开了式1化合物，其中V是CH 2; W为S（O）m; m是整数0,1或2; U是O，C（O），CR 13 R 14或NR 15; 其中R 13为H，烷基; R14是H，OH，OR13或OCOR13; R 15是H，烷基，环烷基，烯基，C（O）R 13，C（O）OR 13或烷基氨基羰基; R1，R2，R3，R4，R5，R6，R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α（TNF-α）的抑制剂，可用作治疗和预防由增加的TNF-α活性引起的疾病，特别是炎症的药物。

公开(公告)号：US07964631B2

公开(公告)日：2011-06-21

申请号：US12854745

申请日：2010-08-11

申请人： Bansi Lal ,  Somesh Sharma ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Pravin Gagare ,  Sunil Jadhav ,  Shashikant Patil ,  Asha Kulkarni-Almeida ,  Sapna Parikh ,  Radha Bhaskar Panicker ,  Anagha Damre ,  Ravindra Gupte

发明人： Bansi Lal ,  Somesh Sharma ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Pravin Gagare ,  Sunil Jadhav ,  Shashikant Patil ,  Asha Kulkarni-Almeida ,  Sapna Parikh ,  Radha Bhaskar Panicker ,  Anagha Damre ,  Ravindra Gupte

IPC分类号： A61K31/38

CPC分类号： C07D327/02

摘要： Compounds of formula 1: are disclosed, wherein V is CH2; W is S(O)m; m is the integer 0, 1 or 2; U is O, C(O), CR13R14 or NR15; where R13 is H, alkyl; R14 is H, OH, OR13 or OCOR13; R15 is H, alkyl, cycloalkyl, alkenyl, C(O)R13, C(O)OR13 or alkylaminocarbonyl; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. These compounds are inhibitors of tumor necrosis factor-alpha (TNF-α) and are useful as medicaments for the treatment and prevention of disorders caused by increased TNF-α activity, in particular inflammations.

摘要翻译： 公开了式1化合物，其中V是CH 2; W为S（O）m; m是整数0,1或2; U是O，C（O），CR 13 R 14或NR 15; 其中R 13为H，烷基; R14是H，OH，OR13或OCOR13; R 15是H，烷基，环烷基，烯基，C（O）R 13，C（O）OR 13或烷基氨基羰基; R1，R2，R3，R4，R5，R6，R7和R8如本文所定义。 这些化合物是肿瘤坏死因子-α（TNF-α）的抑制剂，可用作治疗和预防由增加的TNF-α活性引起的疾病，特别是炎症的药物。

公开(公告)号：US20100034746A1

公开(公告)日：2010-02-11

申请号：US12532009

申请日：2008-03-18

申请人： Ravindra Dattatraya Gupte ,  Aditi Amol Tannu ,  Radha Bhaskar Panicker ,  Somesh Sharma

发明人： Ravindra Dattatraya Gupte ,  Aditi Amol Tannu ,  Radha Bhaskar Panicker ,  Somesh Sharma

IPC分类号： A61K49/00 ,  A61P7/02

CPC分类号： A01K67/027 ,  A01K2207/30 ,  A01K2207/35 ,  A01K2227/105 ,  A01K2267/035

摘要： The present invention relates to a method for evaluating a test compound for antithrombotic activity, thrombolytic activity, or a combination thereof. This method can include providing or employing a donor test animal and a recipient test animal. The donor and recipient test animals can have been pretreated with test compound. The donor test animal can be configured to provide oxygenated blood to the recipient test animal through a thrombus inducing system. This method also includes initiating transport of blood from the donor test animal to the recipient test animal through the thrombus inducing system. The method can include interrupting respiration of the recipient test animal and determining the length of time that the recipient test animal survives. In this method, a survival time longer than a predetermined threshold time indicates that the test compound has antithrombotic activity, thrombolytic activity, or a combination thereof.

摘要翻译： 本发明涉及评价抗血栓活性试验化合物，溶栓活性或其组合的方法。 该方法可以包括提供或使用供体测试动物和接受者测试动物。 供体和受体试验动物可以用试验化合物进行预处理。 供体测试动物可以被配置为通过血栓诱导系统向受体测试动物提供氧合血液。 该方法还包括通过血栓诱导系统启动血液从供体测试动物运送到接受者测试动物。 该方法可以包括中断受体测试动物的呼吸并确定接受者测试动物存活的时间长短。 在该方法中，比预定阈值时间长的存活时间表明测试化合物具有抗血栓形成活性，溶栓活性或其组合。