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：US20070299050A1

公开(公告)日：2007-12-27

申请号：US11667580

申请日：2005-11-08

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 ,  A61K31/38 ,  A61K31/496 ,  A61P1/00 ,  A61P19/00 ,  A61P25/00 ,  A61P37/00 ,  C07D281/12 ,  C07D327/00 ,  C07D411/02

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的化合物，其中V是CH 2 2; W是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是H，烷基; R 14是H，OH，OR 13或OCOR 13; 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; R 1，R 2，R 3，R 4，R 5， R 6，R 7和R 8是如本文所定义的。 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：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。