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1. 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。

2. 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

3. 发明申请

WO2007054739A1 TETRAHYDROINDOLE DERIVATIVES 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四氢吡啶衍生物
公开(公告)号：WO2007054739A1
公开(公告)日：2007-05-18
申请号：PCT/GB2006/050368
申请日：2006-11-03
申请人： MERCK SHARP & DOHME LIMITED , BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
发明人： BURKAMP, Frank , CHECKSFIELD, Graham, David , FLETCHER, Stephen, Robert , LEWIS, Stephen, John , MCIVER, Edward, Giles , OAKLEY, Paul, Joseph , TEALL, Martin, Richard
IPC分类号： C07D209/30 , C07D209/42 , C07D209/08 , C07D405/04 , C07D231/56 , C07D209/86 , C07D401/04 , A61K31/403 , A61K31/404 , A61K31/416 , A61P25/28
CPC分类号： C07D209/30 , C07D209/08 , C07D209/10 , C07D209/12 , C07D209/42 , C07D209/86 , C07D231/56 , C07D401/04 , C07D403/04 , C07D405/04 , C07D409/04
摘要： Tetrahydroindole derivatives of formula (I): are disclosed. These compounds modulate the activity of gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：公开了式（I）的四氢吲哚衍生物：这些化合物调节γ-分泌酶的活性，因此可用于治疗或预防阿尔茨海默病。

4. 发明申请

WO2005047280A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
公开(公告)号：WO2005047280A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004730
申请日：2004-11-09
申请人： MERCK SHARP & DOHME LIMITED , MERCK & CO. INC. , CAI, Dongwei , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： CAI, Dongwei , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula(I): Y-J-NH-Z (I) wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently elected from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions containing the same; the compound for use in therapy; and use of the compound for the manufacture of a medicament for treating or preventing diseases requiring administration of an antagonist of the vanilloid-1 (VR1) receptor.
摘要翻译：本发明提供式（I）化合物：YJ-NH-Z（I）其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1 -4-烷氧基，卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选地被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 3-5环烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基 ; 其中J在NH和Y彼此间位置取代; Z是任选被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基的取代基取代的苯基或吡啶基; 或其药学上可接受的盐; 含有该组合物的药物组合物; 用于治疗的化合物; 以及该化合物在制备用于治疗或预防需要施用香草素-1（VR1）受体拮抗剂的疾病的药物中的用途。

5. 发明申请

WO2005047279A1 SUBSTITUTED NITROGEN-CONTAINING SIX-MEMBERED AMINO-HETEROCYCLES AS VANILLOID-1 RECEPTOR ANTAGONISTS FOR TREATING PAIN 审中-公开
标题翻译：用作治疗疼痛的VANILLOID-1受体拮抗剂的含有NITRUTED的含六聚氨基甲酰胺的氨基酸
公开(公告)号：WO2005047279A1
公开(公告)日：2005-05-26
申请号：PCT/GB2004/004719
申请日：2004-11-09
申请人： MERCK SHARP & DOHME LIMITED , HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
发明人： HOLLINGWORTH, Gregory, John , JONES, A., Brian , MCIVER, Edward, Giles , MOYES, Christopher, Richard , ROGERS, Lauren
IPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
CPC分类号： C07D401/04 , C07D401/14 , C07D403/04 , C07D471/04
摘要： The present invention provides a compound of formula (I): Y-J-NH-Z wherein: Y is a quinoline or isoquinoline optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; J is pyridine, pyridazine, pyrazine, pyrimidine or triazine optionally substituted with one or two substituents independently chosen from hydroxy, halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 3-5 cycloalkyl, C 1-4 alkoxy, hydroxyC 1- 4 alkyl, cyano, hydroxy, C 1-4 cycloalkoxy, C 1-4 alkylthio, haloC 1-4 alkoxy, nitro, Q, (CH 2 ) p Q, NR 2 R 3 , -(CH 2 ) p NR 2 R 3 and -O(CH 2 ) p NR 2 R 3 ; wherein J is substituted at positions meta to each other by NH and Y; and Z is phenyl or pyridyl optionally substituted with one or two substituents independently selected from halogen, haloC 1-4 alkyl, C 1-4 alkyl, C 1-4 alkoxy, haloC 1-4 alkoxy, nitro and amino; Q is phenyl, a five-membered heterocyclic ring containing one, two, three or four heteroatoms chosen from O, N and S, at most one heteroatom being O or S, or a six-membered heterocyclic ring containing one, two or three nitrogen atoms, optionally substituted by C 1-4 alkyl; each R 2 and R 3 is chosen from H and C 1-4 alkyl, or R 2 and R 3 , together with the nitrogen atom to which they are attached, may form a six-membered ring optionally containing an oxygen atom or a further nitrogen atom, which ring is optionally substituted by C 1-4 alkyl or Q; p is 1, 2 or 3; or a pharmaceutically acceptable salt thereof; pharmaceutical compositions comprising it; its use in methods of therapy; use of it for manufacturing medicaments; and methods of using it to treat diseases requiring administration of a VR1 antagonist such as pain, cough, GERD and depression.
摘要翻译：本发明提供式（I）化合物：YJ-NH-Z其中：Y是喹啉或异喹啉，其任选地被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基卤代C 1-4烷氧基，硝基和氨基; J是吡啶，哒嗪，吡嗪，嘧啶或三嗪，任选被一个或两个独立地选自羟基，卤素，卤代C 1-4烷基，C 1-4烷基，C 3-5烃基，C 1-4烷氧基，羟基C 1-4烷基，氰基，羟基，C 1 （CH 2）pQ，NR 2 R 3， - （CH 2）p NRR R 3和-O（CH 2）p NRR 2，其中R 1，R 2， > - [R <3>; 其中J在NH和Y彼此间位置取代; Z是任选被一个或两个独立地选自卤素，卤代C 1-4烷基，C 1-4烷基，C 1-4烷氧基，卤代C 1-4烷氧基，硝基和氨基的取代基取代的苯基或吡啶基; Q是苯基，含有一个，两个，三个或四个选自O，N和S，至多一个杂原子是O或S的杂原子的五元杂环，或含有一个，两个或三个氮的六元杂环任选被C 1-4烷基取代的原子; 每个R 2和R 3选自H和C 1-4烷基，或R 2和R 3与它们所连接的氮原子一起可以形成任选含有氧原子或另外的氮原子，该环任选被C 1-4烷基或Q取代; p为1,2或3; 或其药学上可接受的盐; 包含它的药物组合物; 其用于治疗方法; 使用它制造药物; 以及使用它来治疗需要施用VR1拮抗剂例如疼痛，咳嗽，GERD和抑郁症的疾病的方法。

6. 发明申请

WO2010100431A1 PYRROLOPYRIMIDINES USED AS KINASE INHIBITORS 审中-公开
标题翻译：用作激酶抑制剂的吡咯烷酮
公开(公告)号：WO2010100431A1
公开(公告)日：2010-09-10
申请号：PCT/GB2010/000394
申请日：2010-03-04
申请人： MEDICAL RESEARCH COUNCIL TECHNOLOGY , MCIVER, Edward, Giles , HOUGH, Joane
发明人： MCIVER, Edward, Giles , HOUGH, Joane
IPC分类号： C07D487/04 , A61K31/519 , A61P19/00 , A61P19/02 , A61P25/28 , A61P27/06 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： The invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: R 1 is -NR 7 (CO)R 11 ; R 2 is aryl, heteroaryl, fused aryl-C 3-6- heterocycloalkyl or fused heteroaryl-C 3-6- heterocycloalkyl, each of which is optionally substituted; each R 7 is selected from hydrogen, C 1-6- alkyl and C 3-7- cycloalkyl, wherein said C1-6-alkyl is optionally substituted by one or more halogens; each R 11 is independently selected from C 1-6 -alkyl, C 3-7- cycloalkyl, C 1-6 alkyl-C 3-7- cycloalkyl, C^-heterocycloalkyl, aryl and heteroaryl, each of which may be optionally substituted. Further aspects of the invention relate to pharmaceutical compositions comprising the same, and methods for treating or preventing a disorder selected from cancer, septic shock, Primary open Angle Glaucoma (POAG), hyperplasia, rheumatoid arthritis, psoriasis, artherosclerosis, retinopathy, osteoarthritis, endometriosis, chronic inflammation and Alzheimer's disease. Another aspect of the invention relates to the use of a compound as described above in the preparation of a medicament for the prevention or treatment of a disorder caused by, associated with or accompanied by any abnormal kinase activity, wherein the kinase is selected from TBK1, ERK8, CDK2, MARK3, YES1, VEG-FR, IKKepsilon and combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐或酯，其中：R 1是-NR 7（CO）R 11; R 2是芳基，杂芳基，稠合芳基-C 3-6 - 杂环烷基或稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被取代; 每个R 7选自氢，C 1-6 - 烷基和C 3-7 - 环烷基，其中所述C 1-6 - 烷基任选被一个或多个卤素取代; 每个R 11独立地选自C 1-6 - 烷基，C 3-7 - 环烷基，C 1-6烷基-C 3-7 - 环烷基，C 1-6 - 杂环烷基，芳基和杂芳基，它们各自可以任选地被取代。本发明的其它方面涉及包含其的药物组合物，以及用于治疗或预防选自癌症，败血性休克，原发性开角型青光眼（POAG），增生，类风湿性关节炎，牛皮癣，动脉粥样硬化，视网膜病，骨关节炎，子宫内膜异位症，慢性炎症和阿尔茨海默病。本发明的另一方面涉及如上所述的化合物在制备用于预防或治疗由与任何异常激酶活性相关或伴随任何异常激酶活性引起的病症的药物中的用途，其中所述激酶选自TBK1， ERK8，CDK2，MARK3，YES1，VEG-FR，IKKepsilon及其组合。

7. 发明申请

WO2009122180A1 PYRIMIDINE DERIVATIVES CAPABLE OF INHIBITING ONE OR MORE KINASES 审中-公开
标题翻译：可抑制一种或多种动物的吡咯烷酮衍生物
公开(公告)号：WO2009122180A1
公开(公告)日：2009-10-08
申请号：PCT/GB2009/000878
申请日：2009-04-02
申请人： MEDICAL RESEARCH COUNCIL , MCIVER, Edward, Giles , BRYANS, Justin, Stephen , SMILJANIC, Ela , LEWIS, Stephen, John , HOUGH, Joanne , DRAKE, Thomas
发明人： MCIVER, Edward, Giles , BRYANS, Justin, Stephen , SMILJANIC, Ela , LEWIS, Stephen, John , HOUGH, Joanne , DRAKE, Thomas
IPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04 , A61K31/506 , A61P35/00 , A61P25/28
CPC分类号： C07D239/48 , C07D401/12 , C07D403/12 , C07D407/12 , C07D407/14 , C07D409/12 , C07D409/14 , C07D413/12 , C07D471/04
摘要： A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, formula (I): wherein: R 1 is C 3-8 -cycloalkyl; X is O, NR 7 or C 3-6 -heterocycloalkyl; R 2 is aryl, heteroaryl, fused or unfused aryl-C 3-6 -heterocycloalkyl or fused or unfused heteroaryl-C 3-6 -heterocycIoalkyl, each of which is optionally substituted by one or more substitutents selected from aryl, heteroaryl, C 1-6 -alkyl, C 3-7 -cycloalkyl and a group A, wherein said C 1-6 -alkyl group is optionally substituted by one or more substituents selected from aryl, heteroaryl, R 10 and a group A, said heteroaryl group is optionally substituted by one or more R 10 groups; and wherein said C 3-6 -heterocycloalkyl group optionally contains one or more groups selected from oxygen, sulfur, nitrogen and CO; R 3 is C 1-6 -alkyl optionally substituted by one or more substituents selected from aryl, heteroaryl, -NR 4 R 5 , -OR 6 , -NR 7 (CO)R 6 , -NR 7 (CO)NR 4 R 5 , -NR 7 SO 2 R 6 , -NR 7 COOR 7 , -CONR 4 R 5 , C 3-6 -heterocycloalkyl and formula (a, b, c): wherein R 4-7 and A are as defined in the claims. Further aspects relate to the use of said compounds in the treatment of various therapeutic disorders, and more particularly as inhibitors of one or more kinases.
摘要翻译：本发明的第一方面涉及式（I）化合物或其药学上可接受的盐或酯，式（I）：其中：R 1为C 3-8 - 环烷基; X是O，NR 7或C 3-6 - 杂环烷基; R 2是芳基，杂芳基，稠合或未稠合的芳基-C 3-6 - 杂环烷基或稠合或未稠合的杂芳基-C 3-6 - 杂环烷基，其各自任选被一个或多个选自芳基，杂芳基，C 1-6 - 烷基 C 3-7 - 环烷基和基团A，其中所述C 1-6 - 烷基任选被一个或多个选自芳基，杂芳基，R 10和A基团的取代基取代，所述杂芳基任选地被一个或多个R 10 组; 并且其中所述C 3-6杂环烷基任选地含有一个或多个选自氧，硫，氮和CO的基团; R 3是任选被一个或多个选自芳基，杂芳基，-NR 4 R 5，-OR 6，-NR 7（CO）R 6，-NR 7（CO）NR 4 R 5，-NR 7 SO 2 R 6，-NR 7 COOR 7，-CONR 4 R 5，C 3 -6-杂环烷基和式（a，b，c）：其中R 4-7和A如权利要求中所定义。其它方面涉及所述化合物在治疗各种治疗性疾病中的用途，更具体地涉及一种或多种激酶的抑制剂。

8. 发明申请

WO2010106333A1 COMPOUNDS 审中-公开
标题翻译：化合物
公开(公告)号：WO2010106333A1
公开(公告)日：2010-09-23
申请号：PCT/GB2010/000498
申请日：2010-03-19
申请人： MEDICAL RESEARCH COUNCIL TECHNOLOGY , MCIVER, Edward, Giles , SMILJANIC, Ela , HARDING, Denise, Jamilla , HOUGH, Joanne
发明人： MCIVER, Edward, Giles , SMILJANIC, Ela , HARDING, Denise, Jamilla , HOUGH, Joanne
IPC分类号： C07D471/04 , A61K31/437 , A61P25/28 , A61P35/00
CPC分类号： C07D471/04
摘要： A compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein R 1 is selected from: aryl; heteroaryl; -NHR 3 ; fused aryl-C 4-7 -heterocycloalkyI; -CONR 4 R 5 ; -NHCOR 6 ; -C 3-7 -cycloalkyl; -O-C 3-7 -cycloalkyl; -NR 3 R 6 ; and optionally substituted -C 1-6 alkyl; wherein said aryl, heteroaryl, fused aryl-C 4-7 -heterocycloalkyl and C 4-7 -heterocycloalkyl are each optionally substituted; R 2 is selected from hydrogen, aryl, C 1-6 -alkyl, C 2-6 -alkenyl, C 3-7 -cycloalkyl, heteroaryl, C 4-7 heterocycloalkyl and halogen, wherein said C1-6 -alkyl, C 2-6 -alkenyl, aryl, heteroaryl and C 4-7 -heterocycloalkyl are each optionally substituted. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).
摘要翻译：式（I）化合物或其药学上可接受的盐或酯，其中R 1选自：芳基; 杂; -NHR 3; 稠合芳基C4-7-杂环烷基; -CONR4R5; -NHCOR6; -C3-7环烷基; -O-C 3-7 - 环烷基; -NR3R6; 和任选取代的C 1-6烷基; 其中所述芳基，杂芳基，稠合芳基C 4-7 - 杂环烷基和C 4-7 - 杂环烷基各自任选被取代; R2选自氢，芳基，C 1-6 - 烷基，C 2-6烯基，C 3-7 - 环烷基，杂芳基，C 4-7杂环烷基和卤素，其中所述C 1-6 - 烷基，C 2-6 - 烯基，芳基，杂芳基和C 4-7 - 杂环烷基各自任选被取代。其它方面涉及制备式（I）化合物的药物组合物，治疗用途和方法。

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