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1. 发明申请

WO2006120481A3 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：调节VANILLOID-1受体（VR1）的功能的2,3-取代的双键双嘧蚜嘧啶-4（3H） - 酮
公开(公告)号：WO2006120481A3
公开(公告)日：2007-01-11
申请号：PCT/GB2006050100
申请日：2006-05-10
申请人： MERCK SHARP & DOHME , BAYLISS TRACY , BROWN REBECCA ELIZABETH , HOLLINGWORTH GREGORY JOHN , JONES A BRIAN
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).
摘要翻译：可用作治疗化合物的式（I）化合物，特别是用于治疗通过调节香草素-1受体（VR1，也称为TRPV1）的功能而改善的其它疾病。

2. 发明专利

CA2602395A1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 未知
公开(公告)号：CA2602395A1
公开(公告)日：2006-09-28
申请号：CA2602395
申请日：2006-03-21
申请人： MERCK SHARP & DOHME
发明人： ROGERS LAUREN , HOLLINGWORTH GREGORY JOHN , BAYLISS TRACY , BROWN REBECCA ELIZABETH , MOYES CHRISTOPHER RICHARD , JONES A BRIAN
IPC分类号： C07D473/32 , A61K31/522 , A61P29/00 , C07D471/04 , C07D473/18 , C07D495/04 , C07D513/04 , C07D519/00
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, 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.

3. 发明专利

CA2607933A1 2,3-SUBSTITUTED FUSED BICYCLIC PYRIMIDIN-4(3H)-ONES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 未知
公开(公告)号：CA2607933A1
公开(公告)日：2006-11-16
申请号：CA2607933
申请日：2006-05-10
申请人： MERCK SHARP & DOHME
发明人： HOLLINGWORTH GREGORY JOHN , BROWN REBECCA ELIZABETH , JONES A BRIAN , BAYLISS TRACY
IPC分类号： C07D473/04 , A61K31/52 , A61P25/04 , A61P29/00
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, also known as TRPV1).

4. 发明专利

AU2004292382A1 E-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 未知
公开(公告)号：AU2004292382A1
公开(公告)日：2005-06-09
申请号：AU2004292382
申请日：2004-10-27
申请人： MERCK SHARP & DOHME
发明人： BROWN REBECCA ELIZABETH , JONES A BRIAN , BURKAMP FRANK , BAYLISS TRACY , NEDUVELIL JOSEPH GEORGE
IPC分类号： A61K31/4545 , A61K31/46 , A61P25/04 , C07D211/38 , C07D401/04 , C07D451/04
摘要： Compounds of formula (I): wherein: A 1 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; A 2 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; L is a bond or C 1-6 alkylene; R 1 and R 2 independently chosen from hydrogen and C 1-6 alkyl or R 1 and R 2 may, together, form a methylene or ethylene bridge; W is halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; X is O, S or NR 3 or X, together with the atom to which it is attached, and Y, form an unsaturated five-membered ring together with A 2 ; Y is a bond, C 1-4 alkylene, NH or NH(CH 2 ) 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).

5. 发明专利

AU2006226084A1 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists 未知
公开(公告)号：AU2006226084A1
公开(公告)日：2006-09-28
申请号：AU2006226084
申请日：2006-03-21
申请人： MERCK SHARP & DOHME
发明人： BAYLISS TRACY , BROWN REBECCA ELIZABETH , JONES A BRIAN , ROGERS LAUREN , HOLLINGWORTH GREGORY JOHN , MOYES CHRISTOPHER RICHARD
IPC分类号： C07D473/32 , A61K31/522 , A61P29/00 , C07D471/04 , C07D473/18 , C07D495/04 , C07D513/04 , C07D519/00
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, 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.

6. 发明专利

AU2004290626A1 Bicyclic pyrimidin-4-(3H)-ones and analogues and derivatives thereof which modulate the function of the vanilloid-1 receptor (VR1) 未知
公开(公告)号：AU2004290626A1
公开(公告)日：2005-06-02
申请号：AU2004290626
申请日：2004-11-12
申请人： MERCK SHARP & DOHME
发明人： HOLLINGWORTH GREGORY JOHN , JARVIS REBECCA ELIZABETH , SPAREY TIMOTHY JASON , JONES A BRIAN , BAYLISS TRACY
IPC分类号： C07D471/04 , C07D473/18 , C07D473/22 , 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).

7. 发明专利

AU2006245520A1 2,3-substituted fused bicyclic pyrimidin-4(3H)-ones which modulate the function of the vanilloid-1 receptor (VR1) 未知
公开(公告)号：AU2006245520A1
公开(公告)日：2006-11-16
申请号：AU2006245520
申请日：2006-05-10
申请人： MERCK SHARP & DOHME
发明人： JONES A BRIAN , BROWN REBECCA ELIZABETH , BAYLISS TRACY , HOLLINGWORTH GREGORY JOHN
IPC分类号： A61K31/52 , A61P25/04 , A61P29/00 , 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 (VR1, also known as TRPV1).

8. 发明专利

CA2545725A1 BICYCLIC PYRIMIDIN-4-(3H)-ONES AND ANALOGUES AND DERIVATIVESTHEREOF WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 未知
公开(公告)号：CA2545725A1
公开(公告)日：2005-06-02
申请号：CA2545725
申请日：2004-11-12
申请人： MERCK SHARP & DOHME
发明人： SPAREY TIMOTHY JASON , BAYLISS TRACY , JARVIS REBECCA ELIZABETH , JONES A BRIAN , HOLLINGWORTH GREGORY JOHN
IPC分类号： C07D471/04 , A61K31/522 , A61P25/04 , C07D473/18 , C07D473/22 , 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).

9. 发明专利

AU2006226084B2 2,3-substituted fused pyrimidin-4(3H)-ones as VR1 antagonists 未知
公开(公告)号：AU2006226084B2
公开(公告)日：2011-09-08
申请号：AU2006226084
申请日：2006-03-21
申请人： MERCK SHARP & DOHME
发明人： BAYLISS TRACY , BROWN REBECCA ELIZABETH , JONES A BRIAN , ROGERS LAUREN , HOLLINGWORTH GREGORY JOHN , MOYES CHRISTOPHER RICHARD
IPC分类号： C07D473/32 , A61K31/522 , A61P29/00 , C07D471/04 , C07D473/18 , C07D495/04 , C07D513/04 , C07D519/00
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 CH; when n is two or three, V is CH, O or NR; 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 R groups; and R and R are independently hydrogen, hydroxy, halogen or Calkyl; 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, NRR or S(O)NRR where NRR is as defined above, Calkyl, Calkenyl, Calkynyl, haloCalkyl, Calkoxy, haloCalkoxy, Calkylthio, haloCalkylthio,Ccycloalkyl, hydroxyCalkyl, 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.

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