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1. 发明公开

EP1881988A1 2,3-SUBSTITUTED FUSED BICYCLIC PYRIMIDIN-4(3H)-ONES MODULATING THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：香草素-1受体（VR1）调制的功能取代的2,3-稠合双环嘧啶-4（3H） - 酮
公开(公告)号：EP1881988A1
公开(公告)日：2008-01-30
申请号：EP06759506.6
申请日：2006-05-10
申请人： MERCK SHARP & DOHME LTD. , NEUROGEN CORPORATION
发明人： BROWN, Rebecca Elizabeth , HUMPHRIES, Alexander Charles , ROGERS, Lauren , BAYLISS, Tracy , JONES, A., Brian , MOYES, Christopher Richard , HOLLINGWORTH, Gregory John , BLUM, Charles, A. , ZHENG, Xiaozhang , BAKTHALVATCHALAM, Rajagopal , CAPITOSTI, Scott
IPC分类号： C07D495/04 , C07D513/04 , C07D473/00 , A61K31/495 , A61P11/00 , A61P29/00
CPC分类号： C07D495/04 , C07D473/00 , C07D513/04
摘要： The use of a compound of formula (I): for the manufacture of a medicament for the treatment of conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1, also known as TRPV1).

2. 发明公开

EP1888586A2 2,3-SUBSTITUTED FUSED BICYCLIC PYRIMIDIN-4(3H)-ONES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译： 2,3-取代的嘧啶稠合双环嘧啶-4（3H） - 酮，香草素-1受体的功能（VR1）MODULATE
公开(公告)号：EP1888586A2
公开(公告)日：2008-02-20
申请号：EP06727195.7
申请日：2006-05-10
申请人： MERCK SHARP & DOHME LTD.
发明人： BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian
IPC分类号： C07D473/04 , A61K31/52 , A61P25/04 , A61P29/00
CPC分类号： C07D473/04
摘要： Compounds of formula (I) which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VRl, also known as TRPVl).

3. 发明授权

EP1866310B1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
标题翻译： 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.

4. 发明公开

EP1687306A1 BICYCLIC PYRIMIDIN-4-(3H)-ONES AND ANALOGUES AND DERIVATIVES THEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：双环嘧啶-4-（3H） - 酮和其类似物和衍生物，香草素-1受体的功能（VR1）MODULATE
公开(公告)号：EP1687306A1
公开(公告)日：2006-08-09
申请号：EP04798536.1
申请日：2004-11-12
申请人： MERCK SHARP & DOHME LTD.
发明人： BAYLISS, Tracy , HOLLINGWORTH, Gregory, John , JARVIS, Rebecca, Elizabeth , JONES, A., Brian , SPAREY, Timothy, Jason
IPC分类号： C07D471/04 , C07D495/04 , C07D513/04 , C07D473/22 , C07D473/18 , A61K31/522 , A61P25/04
CPC分类号： C07D473/22 , C07D471/04 , C07D473/18 , C07D473/24 , C07D495/04 , C07D513/04
摘要： Compounds of formula (I); which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).

5. 发明公开

EP1866310A1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 有权
标题翻译： 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.

6. 发明公开

EP1682141A1 4-FLUORO-4-(PYRIDIN-2-YL)-PIPERIDINE-1-CARBOXAMIDE DERIVATIVES AND RELATED COMPOUNDS WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) FOR THE TREATMENT OF PAIN 审中-公开
标题翻译： 4-氟-4-（吡啶-2-基）哌啶-1-羧酸衍生物和相关化合物为香草素-1受体中的作用（VR1）的疼痛的治疗的调制
公开(公告)号：EP1682141A1
公开(公告)日：2006-07-26
申请号：EP04769034.2
申请日：2004-10-27
申请人： MERCK SHARP & DOHME LTD.
发明人： BAYLISS, Tracy , BROWN, Rebecca Elizabeth , BURKAMP, Frank , JONES, A. Brian , NEDUVELIL, Joseph George
IPC分类号： A61K31/4545 , A61K31/46 , C07D211/38 , C07D401/04 , C07D451/04 , A61P25/04
CPC分类号： C07D451/04 , C07D401/04
摘要： Compounds of formula (I): wherein: A1 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from O, N and S, at most one heteroatom being O or S; A2 is phenyl, a six-membered aromatic heterocycle containing one, two or three nitrogen atoms, or a five-membered aromatic heterocycle containing up to four heteroatoms chosen from 0, N and S, at most one heteroatom being O or S; L is a bond or C1-6alkylene; R1 and R2 independently chosen from hydrogen and C1-6alkyl or Rl and R2 may, together, form a methylene or ethylene bridge; W is halogen, C1-6alkyl, haloC1-6alkyl, C1-6alkoxy or haloC1-6alkoxy; X is O, S or NR3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A2; Y is a bond, C1-4alkylene, NH or NH(CH2)1-3; or a pharmaceutically acceptable salt thereof; other substituents are defined in claim 1; which are useful as therapeutic compounds, particularly in the treatment of pain and other conditions ameliorated by the modulation of the function of the vanilloid-1 receptor (VR1).

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