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1. 发明申请

WO2006122200A1 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： 2,3-取代的双酚二吡啶-4（3H） - 调节VANILLOID-1受体（VR1）的功能
公开(公告)号：WO2006122200A1
公开(公告)日：2006-11-16
申请号：PCT/US2006/018119
申请日：2006-05-10
申请人： MERCK SHARP & DOHME LIMITED , NEUROGEN CORPORATION , BROWN, Rebecca Elizabeth , HUMPRIES, Alexander Charles , ROGERS, Lauren , BAYLISS, Tracey , JONES, A., Brian , MOYES, Christopher Richard , HOLLINGWORTH, Gregory John , BLUM, Charles, A. , ZHENG, Xiaozhang , BAKTHALVATCHALAM, Rajagopal , CAPITOSTI, Scott
发明人： BROWN, Rebecca Elizabeth , HUMPRIES, Alexander Charles , ROGERS, Lauren , BAYLISS, Tracey , 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).
摘要翻译：使用式（I）化合物：用于制备用于治疗通过调节香草素-1受体（VR1，也称为TRPV1）的功能而改善的病症的药物。

2. 发明申请

WO2006100520A1 2,3-SUBSTITUTED FUSED PYRIMIDIN-4(3H)-ONES AS VR1 ANTAGONISTS 审中-公开
标题翻译：作为VR1拮抗剂的2,3-取代的氟吡啶-4（3H） - 酮
公开(公告)号：WO2006100520A1
公开(公告)日：2006-09-28
申请号：PCT/GB2006/050060
申请日：2006-03-21
申请人： MERCK SHARP & DOHME LIMITED , BAYLISS, Tracy , BROWN, Rebecca Elizabeth , HOLLINGWORTH, Gregory John , JONES, A. Brian , MOYES, Christopher Richard , ROGERS, Lauren
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 CH 2 ; when n is two or three, V is CH 2 , O or NR 5 ; 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 1 groups; and R 7 and R 8 are independently hydrogen, hydroxy, halogen or C 1-4 alkyl; 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, NR 2 R 3 or S(O) r NR 2 R 3 where NR 2 R 3 is as defined above, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, haloC 1-6 alkylthio,C 3-7 cycloalkyl, hydroxyC 1-6 alkyl, 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.
摘要翻译：式（I）的化合物，其中W为式（1）; A是苯环，含有1,2或3个独立地选自O，N和S的杂原子的f元环杂芳环，条件是不存在不超过一个O或S原子，或含有1个或6个杂芳环 2或3个N原子; n为零，一，二或三; 当n为0或1时，V为CH 2 2; 当n为2或3时，V为CH 2，O或NR 5; 当V为CH 2时，由V形成的键和相邻碳环原子任选地与苯环稠合，含有1,2或3个独立地选自O，N和S的杂原子的五元杂芳环，条件是不再有存在一个O或S，或含有1,2或3个N原子的六元杂芳环; 该环任选地被一个或多个R 1基团取代; R 7和R 8独立地是氢，羟基，卤素或C 1-4烷基; Z是苯环，含有一个，两个，三个或四个独立地选自O，N或S，至多一个杂原子是O或S的杂原子的五元杂芳环或含有一个，二个或三个N原子，任选地被一个或多个选自卤素，羟基，氰基，硝基，NR 2 R 3或S（O）其中NR 2 R 3如上所定义，C 1和R 2如上定义，其中R 1，R 2，R 3， C 1-6烷基，C 2-6链烯基，C 2-6亚炔基，卤代C 1-6烷基，C <亚 > 1-6个烷氧基，卤代C 1-6烷氧基，C 1-6烷硫基，卤代C 1-6烷硫基，C 3-7环烷基，羟基C 1-6烷基，含有独立选自O，N和S的1,2或3个杂原子的五元杂芳环，条件是不再有存在一个O或S原子，或含有1,2或3个N原子的6元杂芳环; 或其药学上可接受的盐或N-氧化物; 包含它们的药物组合物; 用于治疗方法的化合物; 以及用于制备用于治疗作为VR1拮抗剂的疼痛的药物的化合物的使用，包括诸如抑郁症，GERD，瘙痒和尿失禁的病症。

3. 发明申请

WO2006120481A2 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：WO2006120481A2
公开(公告)日：2006-11-16
申请号：PCT/GB2006/050100
申请日：2006-05-10
申请人： MERCK SHARP & DOHME LIMITED , 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。

4. 发明申请

WO2005080391A1 PRODRUGS OF SUBSTITUTED AMINO HETEROBICYCLES 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）功能的替代氨基杂环化合物的产物
公开(公告)号：WO2005080391A1
公开(公告)日：2005-09-01
申请号：PCT/GB2005/000548
申请日：2005-02-16
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
发明人： BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D487/04
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).
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）的功能而改善的疼痛和其它病症。

5. 发明公开

EP1718647A1 PRODRUGS OF SUBSTITUTED AMINO HETEROBICYCLES WHICH MODULATE THE FUNCTION OF THE VANILLOID-1 RECEPTOR (VR1) 审中-公开
标题翻译：前药取代AMINOHETEROBICYCLEN THAT香草素-1受体（VR1）MODULATE的操作
公开(公告)号：EP1718647A1
公开(公告)日：2006-11-08
申请号：EP05708361.0
申请日：2005-02-16
申请人： Merck Sharp & Dohme Limited
发明人： BURKAMP, Frank , CASTRO PINEIRO, Jose Luis , HOLLINGWORTH, Gregory John
IPC分类号： C07D471/04 , C07D487/04 , A61K31/4985 , A61P29/00
CPC分类号： C07D471/04 , C07D487/04
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).

6. 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).

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