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    • 5. 发明授权
      EP1562934B1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 有权
    • AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
    • 氨基杂环AS VR-1拮抗剂治疗疼痛的
    • EP1562934B1
    • 2008-03-26
    • EP03775557.6
    • 2003-11-14
    • MERCK SHARP & DOHME LTD.
    • BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen Robert , HOLLINGWORTH, Gregory John , JONES, A. Brian , MCIVER, Edward Giles , MOYES, Christopher Richard , ROGERS, Lauren
    • C07D401/12 , C07D403/12 , C07D401/14 , C07D405/14 , C07D471/04 , A61K31/4709 , A61K31/4725 , A61P29/00
    • C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
    • the present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C-Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar2, with the proviso that when Y is N or CH then Z is C-Ar2, and with the further proviso that when Y is C-Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, -(CH2)mcarboxy, esterified -(CH2)mcarboxy or -(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.
    • 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 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 7. 发明授权
      EP1866310B1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
    • 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS
    • 2,3-取代的稠合嘧啶-4- VR1拮抗剂（3H） - 酮ALS
    • EP1866310B1
    • 2012-07-11
    • EP06710177.4
    • 2006-03-21
    • MERCK SHARP & DOHME LTD.
    • BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian , MOYES, Christopher Richard , ROGERS, Lauren
    • C07D473/32 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/522 , A61P29/00
    • C07D473/18 , C07D471/04 , C07D495/04
    • 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.
    • 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 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 8. 发明公开
      EP1562934A1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 有权
    • AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN
    • 氨基杂环AS VR-1拮抗剂治疗疼痛的
    • EP1562934A1
    • 2005-08-17
    • EP03775557.6
    • 2003-11-14
    • MERCK SHARP & DOHME LTD.
    • BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen Robert , HOLLINGWORTH, Gregory John , JONES, A. Brian , MCIVER, Edward Giles , MOYES, Christopher Richard , ROGERS, Lauren
    • C07D401/12 , C07D403/12 , C07D401/14 , C07D405/14 , C07D471/04 , A61K31/4709 , A61K31/4725 , A61P29/00
    • C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
    • the present invention provides a compound of formula (I): wherein V represents NR5, O, S, SO or S(O)2; W and X each independently represent CH or N; Y represents N, CH or C-Ar2, with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar2, with the proviso that when Y is N or CH then Z is C-Ar2, and with the further proviso that when Y is C-Ar2 then Z is CH; Ar1 represents a fused 9 or 10 membered heterobicyclic ring system containing one, two, three or four heteroatoms selected from nitrogen, oxygen and sulfur, wherein at least one of the rings in said ring system is aromatic; Ar2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R1 represents halogen, hydroxy, oxo, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, haloC1-6alkyl, hydroxyC1-6alkyl, C1-6alkoxy, haloC1-6alkoxy, hydroxyC1-6alkoxy, C3-7cycloalkyl, C3-7cycloalkoxy, C3-5cycloalkylC1-4alkyl, cyano, nitro, SR6, SOR6, SO2R6, COR6, NR3COR6, CONR3R4, NR3SO2R6, SO2NR3R4, -(CH2)mcarboxy, esterified -(CH2)mcarboxy or -(CH2)mNR3R4; R2 represents hydrogen, halogen, hydroxy, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, haloC1-6alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; R3 and R4 are each independently hydrogen, C1-6alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl or fluoroC1-6alkyl; or R3 and R4 and the nitrogen atom to which they are attached together form a heteroaliphatic ring of 4 to 7 ring atoms, optionally substituted by one or two groups selected from hydroxy or C1-4alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O)2, or NR5; R5 represents hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R6 represents hydrogen, C1-6alkyl, fluoroC1-6alkyl, C3-7cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C1-6alkyl, haloC1-6alkyl, C3-7cycloalkyl, C1-6alkoxy or haloC1-6alkoxy; m is either zero or an integer from 1 to 4; n is either zero or an integer from 1 to 3; or a pharmaceutically acceptable salt, N-oxide or a prodrug thereof; a pharmaceutical composition comprising it; its use in methods of treatment; use of it for the manufacture of a medicament for treating VR-1 related conditions such as those in which pain and/or inflammation predominate; and methods of treatment using it.
    • 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 Global Dossier Espacenet 法律信息 同族专利 专利引用
    • 10. 发明公开
      EP1866310A1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
    • 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS
    • 2,3-取代的稠合嘧啶-4- VR1拮抗剂（3H） - 酮ALS
    • EP1866310A1
    • 2007-12-19
    • EP06710177.4
    • 2006-03-21
    • MERCK SHARP & DOHME LTD.
    • BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian , MOYES, Christopher Richard , ROGERS, Lauren
    • C07D473/32 , C07D471/04 , C07D495/04 , C07D513/04 , A61K31/522 , A61P29/00
    • C07D473/18 , C07D471/04 , C07D495/04
    • 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.
    • 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 Global Dossier Espacenet 法律信息 同族专利 专利引用
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