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14 条记录 (耗时 0.019 秒)

    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS
    2.
    发明公开
    NON-BASIC MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS AND METHODS 审中-公开
    对于糖尿病，肥胖的治疗和相关疾病合适的1-（杂）芳基吡嗪-2-酮衍生物

    公开(公告)号：EP2173725A2

    公开(公告)日：2010-04-14

    申请号：EP08772437.3

    申请日：2008-07-07

    申请人： Bristol-Myers Squibb Company

    发明人： STEIN, Philip, D. ,  BISAHA, Sharon, N. ,  AHMAD, Saleem ,  NGU, Khehyong ,  WASHBURN, William, N.

    IPC分类号： C07D241/18 ,  C07D401/12

    CPC分类号： C07D241/18 ,  C07D401/12

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I, wherein, R1, R2, R3, R8, and R9 are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression or anxiety by administration of a therapeutically effective dose of a compound according to Formula I.

    AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    5.
    发明公开
    AZOLOPYRROLONE MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
    用于黑色素浓缩激素THE DEEN受体1 AZOLOPYRROLONE作为拮抗剂

    公开(公告)号：EP2346873A1

    公开(公告)日：2011-07-27

    申请号：EP09793349.3

    申请日：2009-10-08

    申请人： Bristol-Myers Squibb Company

    发明人： DEVASTHALE, Pratik ,  WASHBURN, William, N. ,  WANG, Wei ,  HERNANDEZ, Andres ,  AHMAD, Saleem ,  ZHAO, Guohua

    IPC分类号： C07D487/04 ,  A61K31/4015 ,  A61P3/00

    CPC分类号： C07D487/04

    摘要： The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula (I) including all pharmaceutically acceptable salts and stereoisomers thereof: wherein A is a monocyclic aryl or monocyclic heteroaryl; W is a direct bond, -0-, or -N(R
    6 )-, provided that if W is a direct bond, D must be a cyclic amine that is attached to A via the nitrogen atom of said cyclic amine; D is a direct bond, substituted or unsubstituted C
    1 to C
    4 alkyl, substituted or unsubstituted C
    3 to C
    7 cycloalkyl, cycloalkylalkyl, or a 4 to 6 membered cyclic amine; B and E are independently N or CH provided that both are not CH;

    C-ARYL GLUCOSIDE SGLT2 INHIBITORS
    7.
    发明授权
    C-ARYL GLUCOSIDE SGLT2 INHIBITORS 有权
    C-芳基糖苷-SGLT2-INHIBITOREN

    公开(公告)号：EP1224195B1

    公开(公告)日：2005-05-18

    申请号：EP00968595.9

    申请日：2000-10-02

    申请人： BRISTOL-MYERS SQUIBB COMPANY

    发明人： ELLSWORTH, Bruce ,  WASHBURN, William, N. ,  SHER, Philip, M. ,  WU, Gang ,  MENG, Wei

    IPC分类号： C07H15/203 ,  A61K31/70 ,  A61P3/10

    CPC分类号： C07H15/203 ,  A61K31/70 ,  A61K31/7034 ,  A61K45/06 ,  C07C43/225 ,  C07C45/46 ,  C07C49/84 ,  A61K2300/00

    摘要： SGLT2 inhibiting compounds are provided having formula (I) where R?1, R2, and R2a¿ are independently hydrogen, OH, OR5, lower alkyl, CF¿3?, OCHF2, OCF3, SR?5i¿ or halogen, or two of R?1, R2 and R2a¿ together with the carbons to which they are attached can form an annelated five, six or seven membered carbocycle or heterocycle; R?3 and R4¿ are independently hydrogen, OH, OR5a, OAryl, OCH¿2?Aryl, lower alkyl, cycloalkyl, CF3, -OCHF2, -OCF3, halogen, -CN, -CO2R?5b, -CO¿2H, -COR6b, -CH(OH)R6c, -CH(OR?5h)R6d, -CONR6R6a¿, -NHCOR5c, -NHSO¿2R?5d, -NHSO¿2?Aryl, Aryl, -SR?5e, -SOR5f, SO¿2R5g, SO2Aryl, or a five, six or seven membered heterocycle, or R?3 and R4¿ together with the carbons to which they are attached form an annelated five, six or seven membered carbocycle or heterocycle; R?5, R5a, R5b, R5c, R5d, R5e, R5f, R5g, R5h, and R5I¿ are independently lower alkyl; R?6, R6a, R6b, R6c and R6d¿ are independently hydrogen, alkyl, aryl, alkylaryl or cycloalkyl, or R?6 and R6a¿ together with the nitrogen to which they are attached form an annelated five, six or seven membered heterocycle; A is O, S, NH, or (CH¿2?)n where n is 0 - 3. A method is also provided for treating diabetes and related diseases employing an SGLT2 inhibiting amount of the above compound alone or in combination with another antidiabetic agent or other therapeutic agent.

    PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS
    8.
    发明公开
    PYRIDONE ANALOGS USEFUL AS MELANIN CONCENTRATING HORMONE RECEPTOR-1 ANTAGONISTS 审中-公开
    PYRIDON ANALOGA ALS“MELANIN CONCENTRATING HORMONE RECEPTOR-1”ANTAGONISTEN

    公开(公告)号：EP2405913A1

    公开(公告)日：2012-01-18

    申请号：EP10707791.9

    申请日：2010-03-09

    申请人： Bristol-Myers Squibb Company

    发明人： AHMAD, Saleem ,  WASHBURN, William, N. ,  HERNANDEZ, Andres, S. ,  ROBL, Jeffrey, A. ,  NGU, Khehyong ,  WANG, Zhenghua

    IPC分类号： A61K31/4412 ,  A61P3/04 ,  C07D213/38 ,  C07D213/74 ,  C07D213/30 ,  C07D213/32 ,  C07D213/26 ,  C07D213/68 ,  C07D401/04 ,  A61K31/4409 ,  A61K31/4427

    CPC分类号： C07D213/38 ,  A61K31/4412 ,  A61K31/4427 ,  C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/68 ,  C07D401/04

    摘要： MCHR1 antagonists are provided having the following Formula I: wherein A
    1 and A
    2 are independently C or N; E is C or N; D
    1 is a bond, -CR
    8 R
    9 X-, -XCR
    8 R
    9 -, -CHR
    8 CHR
    9 -, -CR
    10 =CR
    10' -, -C≡C-, or 1,2-cyclopropyl; X is O, S or -NR
    11 ; R
    1 , R
    2 , and R
    3 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, lower cycloalkoxy, -CF
    3 , -OCF
    3 , -OR
    12 and -SR
    12 ; G is O or S; D
    2 is lower alkyl, lower cycloalkyl, lower alkylcycloalkyl, lower cycloalkylalkyl, lower cycloalkoxyalkyl or lower alkycycloalkoxy; Z
    1 and Z
    2 are independently hydrogen, halogen, lower alkyl, lower cycloalkyl, lower alkoxy, lower cycloalkoxy, halo, -CF
    3 , -OCONR
    14 R
    14' , -CN, -CONR
    14 R
    14' , -SOR
    12 , -SO
    2 R
    12 , -NR
    14 COR
    14' , -NR
    14 CO
    2 R
    14' , -CO
    2 R
    12 , NR
    14 SO
    2 R
    12 or -COR
    12 provided that if Z
    1 is -CH
    3 and one of R
    1 , R
    2 , or R
    3 is F, then Z
    2 cannot be H;; R
    5 , R
    6 , and R
    7 are independently selected from the group consisting of hydrogen, halogen, lower alkyl, lower cycloalkyl, -CF
    3 , -SR
    12 , lower alkoxy, lower cycloalkoxy, -OCH
    2 OMe, -CN, -CONR
    14 R
    14' , SOR
    12 , SO
    2 R
    12 , NR
    14 COR
    14' , NR
    14 CO
    2 R
    12 , CO
    2 R
    12 , NR
    14 SO
    2 R
    12 and -COR
    12 ; R
    8 , R
    9 , R
    10 , R
    10' , R
    11 are independently hydrogen or lower alkyl; R
    12 is lower alkyl or lower cycloalkyl; and R
    14 and R
    14' are independently H, lower alkyl, lower cycloalkyl or R
    14 and R
    14' together with the N to which they are attached form a ring having 4 to 7 atoms. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.