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    • 4. 发明专利
      AU2006226084A1 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists 未知
    • 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists
    • AU2006226084A1
    • 2006-09-28
    • AU2006226084
    • 2006-03-21
    • MERCK SHARP & DOHME
    • BAYLISS TRACY , BROWN REBECCA ELIZABETH , JONES A BRIAN , ROGERS LAUREN , HOLLINGWORTH GREGORY JOHN , MOYES CHRISTOPHER RICHARD
    • C07D473/32 , A61K31/522 , A61P29/00 , C07D471/04 , C07D473/18 , C07D495/04 , C07D513/04 , C07D519/00
    • 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, 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; 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 VR1 antagonists, including conditions such as depression, GERD, itch and urinary incontinence.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 7. 发明专利
      CA2545384A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 未知
    • SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN
    • CA2545384A1
    • 2005-05-26
    • CA2545384
    • 2004-11-09
    • MERCK SHARP & DOHME
    • MOYES CHRISTOPHER RICHARD , ROGERS LAUREN , MCIVER EDWARD GILES , JONES BRIAN A , HOLLINGWORTH GREGORY JOHN
    • C07D401/04 , A61K31/4725 , A61P43/00 , C07D401/14 , C07D403/04 , C07D471/04
    • The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alkyl, C1- 4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC1-4alky l, C1-4alkyl, C3-5cycloalkyl, C1-4alkoxy, hydroxyC1- 4alkyl, cyano, hydroxy, C1 - 4cycloalkoxy, C1-4alkylthio, haloC1-4alkoxy, nitro, Q, (CH2)pQ, NR2R3, - (CH2)pNR2R3 and -O(CH2)pNR2R3; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted wi th one or two substituents independently selected from halogen, haloC1-4alkyl, C1- 4alkyl, C1-4alkoxy, haloC1-4alkoxy, nitro and amino; Q is phenyl, a five- membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-member ed heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C1-4alkyl; each R2 and R3 is chosen from H and C1-4alkyl, or R2 and R3, together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C1-4alkyl or Q; p is 1, 2 or 3 ; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
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