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：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：US20100305094A1

公开(公告)日：2010-12-02

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 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 Panicker ,  Anagha Damre ,  Ravindra Gupte

IPC分类号： A61K31/554 ,  C07D281/14 ,  A61P29/00 ,  A61P19/02 ,  A61P9/10 ,  A61P9/00 ,  A61P31/18 ,  A61P37/00 ,  A61P11/06 ,  A61P35/00 ,  A61P3/10 ,  A61P19/10

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：US08206756B2

公开(公告)日：2012-06-26

申请号：US12500057

申请日：2009-07-09

申请人： Vijay Chauhan ,  Ashish Suthar ,  Dhananjay Sapre ,  Swati Bal-Tembe ,  Ashok Kumar Gangopadhyay ,  Asha Kulkarni-Almeida ,  Sapna Hasit Parikh ,  Ravindra Dattatraya Gupte ,  Nilesh Madhukar Dagia ,  Somesh Sharma ,  Shruta Sudheer Dadarkar ,  Mahesh Gundaji Jadhav ,  Aditi Amol Tannu

发明人： Vijay Chauhan ,  Ashish Suthar ,  Dhananjay Sapre ,  Swati Bal-Tembe ,  Ashok Kumar Gangopadhyay ,  Asha Kulkarni-Almeida ,  Sapna Hasit Parikh ,  Ravindra Dattatraya Gupte ,  Nilesh Madhukar Dagia ,  Somesh Sharma ,  Shruta Sudheer Dadarkar ,  Mahesh Gundaji Jadhav ,  Aditi Amol Tannu

IPC分类号： A01N65/00

CPC分类号： A61K36/28

摘要： This invention relates to a novel herbal composition comprising an extract of flowering and fruiting heads of the plant, Sphaeranthus indicus. The said extract of Sphaeranthus indicus contains a compound, 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (7-Hydroxy-4,11(13)-eudesmadien-12,6-olide) (compound 1), as a bioactive marker. The invention also relates to a composition comprising 3a-hydroxy-5a,9-dimethyl-3-methylene-3a,4,5,5a,6,7,8,9b-octahydro-3H-naphtho[1,2-b]furan-2-one (compound 1) as an active ingredient. The invention also relates to methods of manufacture of the said compositions. The invention also relates to methods of administration of the said compositions to a subject in need of treatment for an inflammatory disorder. The invention also relates to tumor necrosis factor- (TNF-α) and interleukin (IL-1, IL-6, IL-8) inhibitory activity of the said compositions. The invention relates to inhibition of the expression of intercellular adhesion molecule 1 (ICAM-1), vascular-cell adhesion molecule 1 (VCAM-1), and E-Selectin by the said compositions. The said compositions may optionally contain at least one anti-inflammatory agent or can be used in combination with at least one anti-inflammatory agent.

摘要翻译： 本发明涉及一种新颖的草药组合物，其包含植物的开花和果实头部的提取物，Sphaeranthus indicus。 所述提取物含有一种化合物，3a-羟基-5a，9-二甲基-3-亚甲基-3a，4,5,5a，6,7,8,9b-八氢-3H-萘并〔1,2- b]呋喃-2-酮（7-羟基-4,11（13） - 顺式 - 12,6-二醇）（化合物1）作为生物活性标记物。 本发明还涉及包含3a-羟基-5a，9-二甲基-3-亚甲基-3a，4,5,5a，6,7,8,9b-八氢-3H-萘并[1,2-b] 呋喃-2-酮（化合物1）作为活性成分。 本发明还涉及制备所述组合物的方法。 本发明还涉及将所述组合物给予需要治疗炎症性疾病的受试者的方法。 本发明还涉及所述组合物的肿瘤坏死因子（TNF-α）和白介素（IL-1，IL-6，IL-8）抑制活性。 本发明涉及通过所述组合物抑制细胞间粘附分子1（ICAM-1），血管细胞粘附分子1（VCAM-1）和E-选择蛋白的表达。 所述组合物可任选地含有至少一种抗炎剂或可与至少一种抗炎剂组合使用。

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：US20070021489A1

公开(公告)日：2007-01-25

申请号：US10574982

申请日：2004-09-30

申请人： Bansi Lal ,  Ashok Gangopadhyay ,  Vadlamudi Rao ,  Ravindra Gupte ,  Gopal Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Panicker ,  Eleanor Pinto De Souza

发明人： Bansi Lal ,  Ashok Gangopadhyay ,  Vadlamudi Rao ,  Ravindra Gupte ,  Gopal Gole ,  Asha Kulkarni-Almeida ,  Sridevi Krishnan ,  Radha Panicker ,  Eleanor Pinto De Souza

IPC分类号： A61K31/4035 ,  C07D209/46

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：US20120225889A1

公开(公告)日：2012-09-06

申请号：US13510552

申请日：2010-11-15

申请人： Asha Kulkarni-Almeida ,  Ravindra Dattatraya Gupte ,  Nilesh Madhukar Dagia ,  Prabha Beerchandra Mishra

发明人： Asha Kulkarni-Almeida ,  Ravindra Dattatraya Gupte ,  Nilesh Madhukar Dagia ,  Prabha Beerchandra Mishra

IPC分类号： A61K31/335 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P31/00 ,  A61P9/10 ,  A61P9/00 ,  A61P25/00 ,  A61P27/02 ,  A61P31/14 ,  A61P33/06 ,  A61P3/00 ,  A61P17/06 ,  A61P15/00 ,  A61P31/18 ,  A61P37/06 ,  A61P11/00 ,  A61P35/00 ,  A61P3/10 ,  A61P19/08 ,  A61P17/00 ,  A61P25/28 ,  A61P37/08 ,  A61P11/06 ,  A61K31/496 ,  A61K31/4523 ,  A61K31/4545 ,  A61P1/00

CPC分类号： A61K31/365 ,  Y02A50/411

摘要： The present invention provides use of the compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereo isomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs and pharmaceutical compositions containing them for treatment of inflammatory disorders mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-α), interferon-γ (IFN-γ) and interleukins such as IL-1β, IL-2, IL-6, and IL-8. The present invention also relates to a pharmaceutical composition adapted for use in the treatment of inflammatory disorders. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

摘要翻译： 本发明提供由式（1）表示的化合物的用途：其中R1，R2，R3和R4如说明书中所定义，具有所有比例的所有立体异构体和互变异构形式及其混合物及其药学上可接受的 盐，药学上可接受的溶剂化物，药学上可接受的多晶型物和前药以及含有它们的药物组合物，用于治疗由一种或多种选自肿瘤坏死因子-α（TNF-α），干扰素-γ（IFN-γ）和白细胞介素 例如IL-1和bgr; IL-2，IL-6和IL-8。 本发明还涉及适用于治疗炎症性疾病的药物组合物。 本发明还提供了通过向有需要的哺乳动物施用治疗有效量的所述式（1）化合物或其药物组合物来治疗炎症性疾病的方法。

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：US20100324026A1

公开(公告)日：2010-12-23

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 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 Panicker ,  Anagha Damre ,  Ravindra Gupte

IPC分类号： A61K31/39 ,  A61K31/496 ,  A61K31/551 ,  A61K31/5377 ,  A61P1/00 ,  A61P29/00 ,  A61P19/02 ,  A61P19/10 ,  A61P9/10 ,  A61P31/18 ,  A61P33/06 ,  A61P35/00 ,  A61P3/10 ,  A61P25/28

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 R5 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R5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：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。