利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

6 条记录 (耗时 0.016 秒)

    2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS
    2.
    发明授权
    2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
    2,3-取代的稠合嘧啶-4- VR1拮抗剂（3H） - 酮ALS

    公开(公告)号：EP1866310B1

    公开(公告)日：2012-07-11

    申请号：EP06710177.4

    申请日：2006-03-21

    申请人： MERCK SHARP & DOHME LTD.

    发明人： BAYLISS, Tracy ,  BROWN, Rebecca Elizabeth ,  HOLLINGWORTH, Gregory John ,  JONES, A. Brian ,  MOYES, Christopher Richard ,  ROGERS, Lauren

    IPC分类号： C07D473/32 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/522 ,  A61P29/00

    CPC分类号： C07D473/18 ,  C07D471/04 ,  C07D495/04

    摘要： A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six- membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, at most one heteroatom being O or S, or a six- membered heteroaromatic ring containing one, two or three N atoms, optionally substituted by one or more groups chosen from halogen, hydroxy, cyano, nitro, NR2R3 or S(O)rNR2R3 where NR2R3 is as defined above, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, haloC1-6alkylthio,C3-7cycloalkyl, hydroxyC1-6alkyl, a five-membered heteroaromatic ring containing 1, 2or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; or a pharmaceutically acceptable salt or N-oxide thereof; pharmaceutical compositions comprising them; the compounds for use in methods of treatment; and use of the compounds for manufacturing medicaments for treating pain as VRl antagonists, including conditions such as depression, GERD, itch and urinary incontinence.

    2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS
    5.
    发明公开
    2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
    2,3-取代的稠合嘧啶-4- VR1拮抗剂（3H） - 酮ALS

    公开(公告)号：EP1866310A1

    公开(公告)日：2007-12-19

    申请号：EP06710177.4

    申请日：2006-03-21

    申请人： MERCK SHARP & DOHME LTD.

    发明人： BAYLISS, Tracy ,  BROWN, Rebecca Elizabeth ,  HOLLINGWORTH, Gregory John ,  JONES, A. Brian ,  MOYES, Christopher Richard ,  ROGERS, Lauren

    IPC分类号： C07D473/32 ,  C07D471/04 ,  C07D495/04 ,  C07D513/04 ,  A61K31/522 ,  A61P29/00

    CPC分类号： C07D473/18 ,  C07D471/04 ,  C07D495/04

    摘要： A compound of formula (I), wherein W is formula (1); A is a benzene ring, a fÊve-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six- membered heteroaromatic ring containing 1, 2 or 3 N atoms; n is zero, one, two or three; when n is zero or one, V is CH2; when n is two or three, V is CH2, O or NR5; when V is CH2, the bond formed by V and an adjacent carbon ring atom is optionally fused to a phenyl ring, a five-membered heteroaromatic ring containing 1, 2 or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; the ring being optionally substituted by one or more R1 groups; and R7 and R8 are independently hydrogen, hydroxy, halogen or C1-4alkyl; Z is a phenyl ring, a five-membered heteroaromatic ring containing one, two, three or four heteroatoms independently chosen from O, N or S, at most one heteroatom being O or S, or a six- membered heteroaromatic ring containing one, two or three N atoms, optionally substituted by one or more groups chosen from halogen, hydroxy, cyano, nitro, NR2R3 or S(O)rNR2R3 where NR2R3 is as defined above, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, C1-6alkylthio, haloC1-6alkylthio,C3-7cycloalkyl, hydroxyC1-6alkyl, a five-membered heteroaromatic ring containing 1, 2or 3 heteroatoms independently chosen from O, N and S, providing that no more than one O or S atom is present, or a six-membered heteroaromatic ring containing 1, 2 or 3 N atoms; or a pharmaceutically acceptable salt or N-oxide thereof; pharmaceutical compositions comprising them; the compounds for use in methods of treatment; and use of the compounds for manufacturing medicaments for treating pain as VRl antagonists, including conditions such as depression, GERD, itch and urinary incontinence.