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1. 发明申请

WO2004046133A1 AMINO-HETEROCYCLES AS VR-1 ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译： AMINO-HETEROCYCLES作为VR-1拮抗剂治疗疼痛
公开(公告)号：WO2004046133A1
公开(公告)日：2004-06-03
申请号：PCT/GB2003/004969
申请日：2003-11-14
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , C07D401/14 , C07D403/12 , C07D405/14 , C07D471/04
摘要： the present invention provides a compound of formula (I): wherein V represents NR 5 , O, S, SO or S(O) 2 ; W and X each independently represent CH or N; Y represents N, CH or C-Ar 2 , with the proviso that at least one, but no more than two, of W, X and Y are N; Z represents CH or C-Ar 2 , with the proviso that when Y is N or CH then Z is C-Ar 2 , and with the further proviso that when Y is C-Ar 2 then Z is CH; Ar 1 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; Ar 2 represents an aromatic ring selected from phenyl, pyridyl, pyrimidinyl and pyridazinyl which is optionally fused and substituted; R 1 represents halogen, hydroxy, oxo, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, haloC 1-6 alkyl, hydroxyC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 3-7 cycloalkyl, C 3-7 cycloalkoxy, C 3-5 cycloalkylC 1-4 alkyl, cyano, nitro, SR 6 , SOR 6 , SO 2 R 6 , COR 6 , NR 3 COR 6 , CONR 3 R 4 , NR 3 SO 2 R 6 , SO 2 NR 3 R 4 , -(CH 2 ) m carboxy, esterified -(CH 2 ) m carboxy or -(CH 2 ) m NR 3 R 4 ; R 2 represents hydrogen, halogen, hydroxy, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, unsubstituted phenyl or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; R 3 and R 4 are each independently hydrogen, C 1-6 alkyl, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl or fluoroC 1-6 alkyl; or R 3 and R 4 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 C 1-4 alkoxy, which ring may optionally contain as one of the said ring atoms an oxygen or a sulfur atom, S(O), S(O) 2 , or NR 5 ; R 5 represents hydrogen, C 1-4 alkyl, hydroxyC 1-4 alkyl or C 1-4 alkoxyC 1-4 alkyl; R 6 represents hydrogen, C 1-6 alkyl, fluoroC 1-6 alkyl, C 3-7 cycloalkyl, unsubstituted phenyl, or phenyl substituted with one or two groups selected from halogen, C 1-6 alkyl, haloC 1-6 alkyl, C 3-7 cycloalkyl, C 1-6 alkoxy or haloC 1-6 alkoxy; 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.
摘要翻译：本发明提供式（I）化合物：其中V表示NR 5，O，S，SO或S（O）2; W和X各自独立地表示CH或N; Y表示N，CH或C-Ar2，条件是W，X和Y中至少一个，但不超过两个为N; Z表示CH或C-Ar2，条件是当Y为N或CH时，则Z为C-Ar2，进一步条件是当Y为C-Ar 2时，Z为CH; Ar 1表示含有选自氮，氧和硫的一个，两个，三个或四个杂原子的稠合的9或10元杂双环体系，其中所述环系中的至少一个环是芳族的; Ar2表示任选稠合和取代的选自苯基，吡啶基，嘧啶基和哒嗪基的芳环; R 1表示卤素，羟基，氧代，C 1-6烷基，C 2-6烯基，C 2-6炔基，卤代C 1-6烷基，羟基C 1-6烷基，C 1-6烷氧基，卤代C 1-6烷氧基，羟基C 1-6烷氧基，C 3-7环烷基，C 3-7环烷氧基，C 3-8环烷基C 1-4烷基，氰基，硝基，SR 6，SOR 6，SO 2 R 6，COR 6，NR 3 COR 6，CONR 3 R 4，NR SO 2 R 6，SO 2 NR 3 R 4， - （CH 2）m羧基，酯化 - （CH 2）m羧基或 - （CH 2）m NR 3 R 4; R 2表示氢，卤素，羟基，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基，卤代C 1-6烷氧基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或卤代C 1-6烷氧基; R 3和R 4各自独立地为氢，C 1-6烷基，C 2-6烯基，C 2-6炔基，C 3-7环烷基或氟C 1-6烷基; 或R 3和R 4并且它们所连接的氮原子一起形成4至7个环原子的杂脂肪族环，任选地被一个或两个选自羟基或C 1-4烷氧基的基团取代，该环可任选地被含有所述环原子之一为氧或硫原子，S（O），S（O）2或NR 5; R 5表示氢，C 1-4烷基，羟基C 1-4烷基或C 1-4烷氧基C 1-4烷基; R 6表示氢，C 1-6烷基，氟C 1-6烷基，C 3-7环烷基，未取代的苯基或被一个或两个选自卤素，C 1-6烷基，卤代C 1-6烷基，C 3-7环烷基，C 1-6烷氧基或C 1-6烷基的基团取代的苯基 haloC1-6alkoxy; m为零或1至4的整数; n为0或1至3的整数; 或其药学上可接受的盐，N-氧化物或其前药; 包含它的药物组合物; 其用于治疗方法; 使用它来制造用于治疗VR-1相关病症的药物，例如其中疼痛和/或炎症占优势的病症; 和治疗方法

2. 发明申请

WO2004099177A1 SUBSTITUTED-1-PHTHALAZINAMINES AS VR-1 ANTAGONISTS 审中-公开
标题翻译：作为VR-1拮抗剂的替代1-苯二胺
公开(公告)号：WO2004099177A1
公开(公告)日：2004-11-18
申请号：PCT/GB2004/001942
申请日：2004-05-04
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JONES, Brian, A. , MCIVER, Edward, Giles
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JONES, Brian, A. , MCIVER, Edward, Giles
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): in which Ar and R 1 are phenyl or a heteroaromatic group, R 2 is generally hydrogen, R 3 is hydrogen or alkyl and X, Y and Z are generally CH or N as VR-1 antagonists; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in therapy; use of it to manufacture medicaments to treat pain or inflammation; and methods of treating pain or inflammation.
摘要翻译：本发明提供式（I）化合物：其中Ar和R 1为苯基或杂芳基，R 2通常为氢，R 3为氢或烷基，X，Y和Z为通常CH或N作为VR-1拮抗剂; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗; 使用它来制造治疗疼痛或炎症的药物; 以及治疗疼痛或炎症的方法。

3. 发明申请

WO2004014865A1 PHENYLPYRIDAZINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：作为GABA受体配体的苯基吡啶衍生物
公开(公告)号：WO2004014865A1
公开(公告)日：2004-02-19
申请号：PCT/GB2003/003376
申请日：2003-08-04
申请人： MERCK SHARP & DOHME LIMITED , BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
发明人： BLACKABY, Wesley, Peter , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert , JENNINGS, Andrew , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , STREET, Leslie, Joseph , THOMAS, Steve , VAN NIEL, Monique, Bodil , WILSON, Kevin
IPC分类号： C07D237/24
CPC分类号： C07D231/12 , C07D233/56 , C07D237/08 , C07D237/14 , C07D237/20 , C07D237/24 , C07D249/08 , C07D401/04 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D409/04 , C07D417/14
摘要： A class of 4-phenylpyridazine derivatives of Formula (I), being selective ligands for GABA A receptors, in particular having high affinity for the α2 and/or α3 and or α5 subunit thereof, are accordingly of benefit in the treatment and/or prevention of adverse conditions of the central nervous system, including anxiety, convulsions and cognitive disorders.
摘要翻译：一类式（I）的4-苯基哒嗪衍生物，作为GABA A受体的选择性配体，特别是对α2和/或其α3和α5亚基具有高亲和力，因此在治疗和/或预防中枢神经系统的不利条件，包括焦虑，抽搐和认知障碍。

4. 发明申请

WO2002081474A1 TRIAZOLOPHTHALAZINE / QUINOLINE / ISOQUINOLINE DERIVATIVES WHICH ARE LIGANDS FOR GABA-A RECEPTORS CONTAINING THE ALPHA 5 SUBTYPE 审中-公开
标题翻译：用于含有ALPHA 5亚型的GABA-A受体的配体的三唑盐/喹啉/异喹啉衍生物
公开(公告)号：WO2002081474A1
公开(公告)日：2002-10-17
申请号：PCT/GB2002/001502
申请日：2002-03-28
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert
发明人： BLURTON, Peter , BURKAMP, Frank , FLETCHER, Stephen, Robert
IPC分类号： C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention provides a compound of formula (I): in which R 1 is an aromatic or heteroaromatic ring, M is a bond, -CH 2 -, -O- or -S-, R 2 , R 3 and R 4 are as defined herein, and X, Y and Z generally define a 1,2,4-triazolo[3,4-a]phthalazine, 1,2,3-triazolo[1,5-a]quinoline or 1,2,4-triazolo[3,4-a]isoquinoline core, as a ligand for GABA-A receptors containing the alpha 5 subtype and which is preferably an inverse agonist thereat and is thus useful for enhancing cognition in conditions such as Alzheimer's disease, compositions containing it, its use in therapy, use of it for making medicaments and methods of treatment using it.
摘要翻译：本发明提供式（I）化合物：其中R 1是芳族或杂芳族环，M是一个键，-CH 2 - ， - O-或-S-，R 2，R 3 和R 4如本文所定义，X，Y和Z通常定义1,2,4-三唑并[3,4-a]酞嗪，1,2,3-三唑并[1,5-a] 喹啉或1,2,4-三唑并[3,4-a]异喹啉核，作为含有α5亚型的GABA-A受体的配体，优选为其反向激动剂，因此可用于增强作为阿尔茨海默病，含有它的组合物，其在治疗中的用途，其用于制备药物的用途和使用它的治疗方法。

5. 发明申请

WO2006008558A1 ARYLACETIC ACIDS AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER’S DISEASE 审中-公开
标题翻译：用于治疗阿尔茨海默病的ARYLACETIC酸和相关化合物
公开(公告)号：WO2006008558A1
公开(公告)日：2006-01-26
申请号：PCT/GB2005/050114
申请日：2005-07-19
申请人： MERCK SHARP & DOHME LIMITED , BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
发明人： BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
IPC分类号： A61K31/215
CPC分类号： A61K31/215
摘要： Compounds of formula I are useful in treatment of diseases associated with the deposition of β-amyloid in the brain.
摘要翻译：式I化合物可用于治疗与脑中β-淀粉样蛋白沉积相关的疾病。

6. 发明授权

EP1773315B1 ARYLACETIC ACIDS AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE 有权
标题翻译： Arylacetic及相关化合物用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1773315B1
公开(公告)日：2008-01-16
申请号：EP05758960.8
申请日：2005-07-19
申请人： Merck Sharp & Dohme Limited
发明人： BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
IPC分类号： A61K31/215 , A61P25/28
CPC分类号： A61K31/215
摘要： Compounds of formula I are useful in treatment of diseases associated with the deposition of ß-amyloid in the brain.

7. 发明公开

EP1773315A1 ARYLACETIC ACIDS AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER'S DISEASE 有权
标题翻译： Arylacetic及相关化合物用于治疗阿尔茨海默氏病的治疗
公开(公告)号：EP1773315A1
公开(公告)日：2007-04-18
申请号：EP05758960.8
申请日：2005-07-19
申请人： Merck Sharp & Dohme Limited
发明人： BLURTON, Peter , BURKAMP, Frank , CHURCHER, Ian , HARRISON, Timothy , NEDUVELIL, Joseph
IPC分类号： A61K31/215 , A61P25/28
CPC分类号： A61K31/215
摘要： Compounds of formula I are useful in treatment of diseases associated with the deposition of β-amyloid in the brain.

8. 发明申请

WO2008075109A1 SUBSTITUTED PIPERIDINES HAVING PROTEIN KINASE INHIBITING ACTIVITY 审中-公开
标题翻译：具有蛋白激酶抑制活性的替代哌啶
公开(公告)号：WO2008075109A1
公开(公告)日：2008-06-26
申请号：PCT/GB2007/050776
申请日：2007-12-20
申请人： ASTEX THERAPEUTICS LIMITED , THE INSTITUTE OF CANCER RESEARCH:ROYAL CANCER HOSPITAL , CANCER RESEARCH TECHNOLOGY LIMITED , ASTRAZENECA AB , WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
发明人： WOODHEAD, Steven, John , FREDERICKSON, Martyn , HAMLETT, Christopher , WOODHEAD, Andrew, James , VERDONK, Marinus, Leendert , SORE, Hannah, Fiona , WALKER, David, Winter , BLURTON, Peter , COLLINS, Ian , CHEUNG, Kwai, Ming , CALDWELL, John , DA FONSECA MCHARDY, Tatiana, Faria , LUKE, Richard, William, Arthur , MATUSIAK, Zbigniew, Stanley , LEACH, Andrew , MORRIS, Jeffrey, James
IPC分类号： C07D471/04 , C07D473/34 , C07D487/04 , C07D519/00 , A61K31/437 , A61K31/52 , A61P35/00
CPC分类号： C07D487/04 , C07D471/04 , C07D473/34 , C07D519/00
摘要： The invention provides PKA and PKB kinase-inhibiting compounds of the formula (I); or salts, solvates, tautomers or N-oxides thereof, wherein E is a five membered heteroaryl ring containing 1, 2, 3 or 4 heteroatoms selected from O, N and S provided that no more than 1 heteroatom may be other than N; q and r are each is 0 or 1; provided that q+r is 1 or 2; T is N or a group CR 5 ; J 1 -J 2 is N=C(R 6 ), (R 7 )C=N, (R 8 )N- C(O), (R 8 ) 2 C-C(O), N=N or (R 7 )C=C(R 6 ); Q 3 is a bond or a saturated C 1-3 hydrocarbon linker group optionally substituted by fluorine and hydroxy; G is NR 2 R 3 , CN or OH; m and n are each 0 or 1, provided that m+n is 1 or 2, and provided also that m or n are each 0 when the adjacent ring member of ring E is S or O; R 1a and R 1b are the same or different and each is hydrogen or a substituent R 10 ; or R 1a and R 1b together with the carbon atoms or heteroatoms to which they are attached form a 5 or 6-membered aryl or heteroaryl ring, wherein the aryl or heteroaryl rings are optionally substituted by one or more substituents R 10 ; and R 2 , R 3 , R 4 , R 5 , R 7 , R 6 , R 8 , and R 10 are as defined in the claims.
摘要翻译：本发明提供了式（I）的PKA和PKB激酶抑制化合物; 或其盐，溶剂合物，互变异构体或N-氧化物，其中E是含有1,2,3或4个选自O，N和S的杂原子的五元杂芳基环，条件是不超过1个杂原子可以不是N; q和r各自为0或1; q + r为1或2; T是N或CR 5; J 1是N = C（R 6），（R 7）C = N，（R 8）N C（O），（R 8）2 CC（O），N = N或（R 0 > 7 ）C = C（R ^{6 ）; Q 3是任选被氟和羟基取代的键或饱和C 1-3烃连接基团; G是NR 2 R 3，CN或OH; m和n各自为0或1，条件是m + n为1或2，并且当环E的相邻环构件为S或O时，m或n各自为0; R 1a和R 1b相同或不同，各自为氢或取代基R 10; 或R 1a和R 1b与它们所连接的碳原子或杂原子一起形成5或6元芳基或杂芳基环，其中芳基或杂芳基环任选地被一个或多个取代基R 10取代; R 2，R 3，R 4，R 5，R 7， R 6，R 8和R 10如权利要求中所定义。}

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