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    Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha
    6.
    发明授权
    Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha 有权
    融合的三环化合物作为肿瘤坏死因子-α的抑制剂

    公开(公告)号：US07834052B2

    公开(公告)日：2010-11-16

    申请号：US11667580

    申请日：2005-11-08

    申请人： Bansi Lal ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Pravin Gagare ,  Sunil Jadhav ,  Shashikant Patil

    发明人： Bansi Lal ,  Usha Ghosh ,  Swati Bal-Tembe ,  Tulsidas More ,  Pravin Gagare ,  Sunil Jadhav ,  Shashikant Patil

    IPC分类号： A61K31/38 ,  C07D497/00

    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。

    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors
    8.
    发明授权
    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors 失效
    三环胍衍生物作为钠 - 质子交换抑制剂

    公开(公告)号：US08183234B2

    公开(公告)日：2012-05-22

    申请号：US12827277

    申请日：2010-06-30

    申请人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More ,  Anil Ghate ,  Jacqueline Trivedi ,  Sapna Parikh

    发明人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More ,  Anil Ghate ,  Jacqueline Trivedi ,  Sapna Parikh

    IPC分类号： A61P7/00 ,  A61P9/00

    CPC分类号： C07D327/08

    摘要： Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidinocarbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.

    摘要翻译： 公开了具有式1的稠合三环的胍衍生物，其中U是C（O），CR a R b，O，NR a或S（O）m; V是CRaRb或NRa; W为S（O）m; 其中R a是H，烷基，环烷基，烯基或芳烷基; Rb是H，烷基，OH，ORa或OCORa，m是整数0,1或2; R1，R2，R3，R4，R5，R6，R7和R8如本文所定义，条件是R 1，R 2，R 3，R 4，R 5，R 6，R 7或R 8中的至少一个是胍基或胍基羰基。 这些衍生物是钠 - 质子交换抑制剂，并且可用作治疗例如与缺血和再灌注相关的器官疾病，心律失常，心脏肥大，高血压，细胞增殖性疾病和糖尿病的药物。

    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors
    10.
    发明授权
    Tricyclic guanidine derivatives as sodium-proton exchange inhibitors 失效
    三环胍衍生物作为钠 - 质子交换抑制剂

    公开(公告)号：US07834001B2

    公开(公告)日：2010-11-16

    申请号：US11667583

    申请日：2005-11-08

    申请人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More

    发明人： Bansi Lal ,  Swati Bal-Tembe ,  Usha Ghosh ,  Arun Kumar Jain ,  Tulsidas More

    IPC分类号： C07D327/08 ,  A61K31/382

    CPC分类号： C07D327/08

    摘要： Guanidine derivatives having a condensed tricyclic ring of formula 1: are disclosed, wherein U is C(O), CRaRb, O, NRa or S(O)m; V is CRaRb or NRa; W is S(O)m; wherein Ra is H, alkyl, cycloalkyl, alkenyl or aralkyl; Rb is H, alkyl, OH, ORa or OCORa, and m is the integer 0, 1 or 2; R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein with the proviso that at least one of R1, R2, R3, R4, R5, R6, R7 or R8 is guanidino or guanidino carbonyl. These derivatives are sodium-proton exchange inhibitors and are useful as medicaments for the treatment of, for example, organ disorders associated with ischemia and reperfusion, cardiac arrhythmia, cardiac hypertrophy, hypertension, cell proliferative disorders and diabetes.

    摘要翻译： 公开了具有式1的稠合三环的胍衍生物，其中U是C（O），CR a R b，O，NR a或S（O）m; V是CRaRb或NRa; W为S（O）m; 其中R a是H，烷基，环烷基，烯基或芳烷基; Rb是H，烷基，OH，ORa或OCORa，m是整数0,1或2; R1，R2，R3，R4，R5，R6，R7和R8如本文所定义，条件是R 1，R 2，R 3，R 4，R 5，R 6，R 7或R 8中的至少一个是胍基或胍基羰基。 这些衍生物是钠 - 质子交换抑制剂，并且可用作治疗例如与缺血和再灌注相关的器官疾病，心律失常，心脏肥大，高血压，细胞增殖性疾病和糖尿病的药物。