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1. 发明申请

WO2008107478A1 QUINOLINONE DERIVATIVES AS PARP AND TANK INHIBITORS 审中-公开
标题翻译：喹诺酮衍生物作为PARP和坦克抑制剂
公开(公告)号：WO2008107478A1
公开(公告)日：2008-09-12
申请号：PCT/EP2008/052764
申请日：2008-03-07
申请人： JANSSEN PHARMACEUTICA NV , VIALARD, Jorge Eduardo , ANGIBAUD, Patrick René , MEVELLEC, Laurence Anne , MEYER, Christophe , FREYNE, Eddy Jean Edgard , PILATTE, Isabelle Noëlle Constance , ROUX, Bruno , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ADELINET, Christophe Denis , MARCONNET-DECRANE, Laurence Françoise Bernadette , MACRITCHIE, Jacqueline Anne , DUFFY, James Edward Stewart , OWENS, Andrew Pate , STORCK, Pierre-Henri , PONCELET, Virginie Sophie
发明人： VIALARD, Jorge Eduardo , ANGIBAUD, Patrick René , MEVELLEC, Laurence Anne , MEYER, Christophe , FREYNE, Eddy Jean Edgard , PILATTE, Isabelle Noëlle Constance , ROUX, Bruno , PASQUIER, Elisabeth Thérèse Jeanne , BOURDREZ, Xavier Marc , ADELINET, Christophe Denis , MARCONNET-DECRANE, Laurence Françoise Bernadette , MACRITCHIE, Jacqueline Anne , DUFFY, James Edward Stewart , OWENS, Andrew Pate , STORCK, Pierre-Henri , PONCELET, Virginie Sophie
IPC分类号： C07D215/22 , A61K31/4704
CPC分类号： C07D215/227 , C07D401/06 , C07D401/12 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： The present invention provides compounds of Formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds, wherein R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , n, m and X have defined meanings.
摘要翻译：本发明提供式（I）化合物，它们作为PARP抑制剂的用途以及包含所述化合物的药物组合物，其中R 1，R 2， R 3，R 4，R 5，R 6，R 7，R 7，R 7， / sup>，n，m和X定义了含义。

2. 发明申请

WO2004101539A1 CYCLIC SULFONAMIDES FOR INHIBITION OF GAMMA-SECRETASE 审中-公开
标题翻译：用于抑制GAMMA-分泌酶的循环磺酰胺
公开(公告)号：WO2004101539A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/002013
申请日：2004-05-07
申请人： MERCK SHARP & DOHME LIMITED , DINNELL, Kevin , HARRISON, Timothy , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
发明人： DINNELL, Kevin , HARRISON, Timothy , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
IPC分类号： C07D285/16
CPC分类号： C07D279/02
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in the treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

3. 发明申请

WO2004101538A1 CYCLOHEXYL SULPHONES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译： CYCLOHEXYL SULPHONES作为GAMMA-SECRETASE抑制剂
公开(公告)号：WO2004101538A1
公开(公告)日：2004-11-25
申请号：PCT/GB2004/001973
申请日：2004-05-07
申请人： MERCK SHARP & DOHME LIMITED , DINNELL, Kevin , HARRISON, Timothy , GIBSON, Karl, Richard , JELLEY, Richard, Alexander , NADIN, Alan, John , OAKLEY, Paul Joseph , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
发明人： DINNELL, Kevin , HARRISON, Timothy , GIBSON, Karl, Richard , JELLEY, Richard, Alexander , NADIN, Alan, John , OAKLEY, Paul Joseph , OWENS, Andrew, Pate , SHAW, Duncan, Edward , WILLIAMS, Brian, John
IPC分类号： C07D285/16
CPC分类号： C07D279/02
摘要： Compounds of formula (I): inhibit gamma-secretase and hence find use in treatment or prevention of Alzheimer's disease.
摘要翻译：式（I）化合物：抑制γ-分泌酶，因此可用于治疗或预防阿尔茨海默氏病。

4. 发明申请

WO2004031139A1 CYCLOHEXYL SULPHONES AS GAMMA-SECRETASE INHIBITORS 审中-公开
标题翻译： CYCLOHEXYL SULPHONES作为GAMMA-SECRETASE抑制剂
公开(公告)号：WO2004031139A1
公开(公告)日：2004-04-15
申请号：PCT/GB2003/004196
申请日：2003-09-25
申请人： MERCK SHARP & DOHME LIMITED , CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , THOMSON, Joanne , WILLIAMS, Susannah
发明人： CHURCHER, Ian , HARRISON, Timothy , KERRAD, Sonia , NADIN, Alan, John , OWENS, Andrew, Pate , SHAW, Duncan, Edward , THOMSON, Joanne , WILLIAMS, Susannah
IPC分类号： C07C317/30
CPC分类号： C07D213/70 , A61K31/10 , C07C317/30 , C07C2601/14 , C07D213/74 , C07D231/18 , C07D233/42 , C07D249/12 , C07D257/04 , C07D261/10 , C07D275/03 , C07D277/36 , C07D295/088 , C07D307/64 , C07D333/34
摘要： Compounds of formula (I) inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.
摘要翻译：式（I）化合物通过γ-分泌酶抑制APP的加工，因此可用于治疗或预防阿尔茨海默氏病。

5. 发明申请

WO02083139B1 INHIBITORS OF AKT ACTIVITY 审中-公开
标题翻译： AKT活性抑制剂
公开(公告)号：WO02083139B1
公开(公告)日：2002-12-27
申请号：PCT/US0210880
申请日：2002-04-08
申请人： MERCK & CO INC , MERCK SHARP & DOHME , BARNETT STANLEY F , OWENS ANDREW PATE
发明人： BARNETT STANLEY F , OWENS ANDREW PATE
IPC分类号： A61K31/5025 , C07D487/04
CPC分类号： C07D487/04 , A61K31/5025
摘要： The present invention is directed to compounds comprising a triazolo[4,3- b ]pyridazine moiety which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.
摘要翻译：本发明涉及包含抑制丝氨酸/苏氨酸蛋白激酶Akt活性的三唑并[4,3-b]哒嗪部分的化合物。本发明还涉及含有本发明化合物的化学治疗组合物和用于治疗癌症的方法，其包括施用本发明的化合物。

6. 发明申请

WO0138326A3 IMIDAZO-PYRIDINE DERIVATIVES AS LIGANDS FOR GABA RECEPTORS 审中-公开
标题翻译：咪达唑啶衍生物作为GABA受体的配体
公开(公告)号：WO0138326A3
公开(公告)日：2002-05-10
申请号：PCT/GB0004451
申请日：2000-11-22
申请人： MERCK SHARP & DOHME , CRAWFORTH JAMES MICHAEL , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , HARRISON TIMOTHY , OWENS ANDREW PATE , ROWLEY MICHAEL , TEALL MARTIN RICHARD
发明人： CRAWFORTH JAMES MICHAEL , GOODACRE SIMON CHARLES , HALLETT DAVID JAMES , HARRISON TIMOTHY , OWENS ANDREW PATE , ROWLEY MICHAEL , TEALL MARTIN RICHARD
IPC分类号： A61K31/437 , A61K31/444 , A61P1/08 , A61P3/04 , A61P15/00 , A61P21/00 , A61P23/00 , A61P25/00 , A61P25/06 , A61P25/18 , A61P25/22 , A61P25/24 , A61P27/16 , A61P43/00 , C07B61/00 , C07D471/04
CPC分类号： C07D471/04
摘要： A class of 3-phenylimidazo[1,2-a]pyridine derivatives, substituted at the meta position of the phenyl ring by an optionally substituted aryl or heteroaryl group which is directly attached or bridged by an oxygen atom or a -NH- linkage, are selective ligands for GABAA receptors, in particular having high affinity for the alpha 2 and/or alpha 3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of disorders of the central nervous system, including anxiety and convulsions.
摘要翻译：一类3-苯基咪唑并[1,2-a]吡啶衍生物，其通过任选取代的被氧原子连接或桥连的芳基或杂芳基在苯环的间位取代或-NH-键是GABA A受体的选择性配体，特别是对其α2和/或α3亚基具有高亲和力，因此有益于治疗和/或预防中枢神经系统疾病，包括焦虑和抽搐。

7. 发明申请

WO1996007649A1 MORPHOLINE DERIVATIVES AND THEIR USE AS THERAPEUTIC AGENTS 审中-公开
标题翻译：吗啉衍生物及其用作治疗药物
公开(公告)号：WO1996007649A1
公开(公告)日：1996-03-14
申请号：PCT/GB1995002039
申请日：1995-08-30
申请人： MERCK SHARP & DOHME LIMITED , FINKE, Paul , HARRISON, Timothy , LEWIS, Richard, Thomas , MACLEOD, Angus, Murray , OWENS, Andrew, Pate
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07D265/32
CPC分类号： C07D413/06 , C07D265/32
摘要： The present invention relates to compounds of formula (I) wherein: R , R , R , R and R are selected from a variety of suitable aromatic substituents; R is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, or C2-4alkyl substituted by C1-4alkoxy or hydroxy; R is hydrogen, C1-6alkyl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, phenyl, C2-4alkyl substituted by C1-4alkoxy or hydroxy, or the group C(=NR )NR R ; or R and R , together with the nitrogen atom to which they are attached, form an optionally substituted saturated heterocyclic ring of 4 to 7 ring atoms which may optionally contain in the ring one oxygen or sulphur atom or a group selected from NR , S(O) or S(O)2; or R and R , together with the nitrogen atom to which they are attached, form a piperidino ring substituted by a spiro-fused indene or indoline group, each of which may be unsubstituted or substituted; R is hydrogen, C1-4alkyl, hydroxyC1-4alkyl or C1-4alkoxyC1-4alkyl; R and R are each independently hydrogen or C1-4alkyl, or R and R are joined so, together with the carbon atoms to which they are attached, there is formed a C5-7 ring; X is selected from -CH2CH2-, -COCH2- or -CH2CO-; and Y is hydrogen, or C1-4alkyl optionally substituted by a hydroxyl group; or a pharmaceutically acceptable salt thereof. The compounds are of particular use in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
摘要翻译：本发明涉及式（I）化合物，其中：R 1，R 2，R 3，R 4和R 5选自多种合适的芳族取代基; R 6是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基或被C 1-4烷氧基或羟基取代的C 2-4烷基; R 7是氢，C 1-6烷基，C 3-7环烷基，C 3-7环烷基C 1-4烷基，苯基，被C 1-4烷氧基或羟基取代的C 2-4烷基，或C（= NR c）NR a R ; 或R 6和R 7与它们所连接的氮原子一起形成任选取代的4至7个环原子的饱和杂环，其可任选地在环中含有一个氧或硫原子或基团选自NR 8，S（O）或S（O）2; 或R 6和R 7与它们所连接的氮原子一起形成被螺稠合的茚或二氢吲哚取代的哌啶子基环，其各自可以是未取代的或取代的; R 8是氢，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 9a和R 9b各自独立地为氢或C 1-4烷基，或者R 9a和R 9b连接在一起，与它们所连接的碳原子一起形成C5-7 环; X选自-CH 2 CH 2 - ， - COCH 2 - 或-CH 2 CO-; 和Y是氢或任选被羟基取代的C 1-4烷基; 或其药学上可接受的盐。该化合物特别用于治疗或预防疼痛，炎症，偏头痛，呕吐和带状疱疹后神经痛。

8. 发明申请

WO1993001165A2 AROMATIC COMPOUNDS, COMPOSITIONS CONTAINING THEM AND THEIR USE IN THERAPY 审中-公开
标题翻译：芳香化合物，包含它们的组合物及其在治疗中的使用
公开(公告)号：WO1993001165A2
公开(公告)日：1993-01-21
申请号：PCT/GB1992001241
申请日：1992-07-08
申请人： MERCK SHARP & DOHME LIMITED , OWENS, Andrew, Pate , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： C07C271/16
CPC分类号： C07D295/185 , A61K38/00 , C07C211/29 , C07C217/48 , C07C217/64 , C07C229/10 , C07C229/14 , C07C229/36 , C07C233/18 , C07C233/22 , C07C233/73 , C07C237/06 , C07C237/08 , C07C237/20 , C07C255/13 , C07C255/24 , C07C255/54 , C07C271/16 , C07C271/20 , C07C271/22 , C07C275/10 , C07C275/24 , C07C275/28 , C07C311/04 , C07C2601/02 , C07D207/28 , C07D241/08 , C07D295/092 , C07K5/06026
摘要： Compounds of formula (I) and salts and prodrugs thereof wherein, Q is optionally substituted phenyl, heteroaryl or naphthyl; X and Y are each H, C1-6 alkyl, C2-6 alkenyl or X and Y are together =O; Z is O or S; R is H, optionally substituted C1-6 alkyl, optionally substituted phenyl(C1-4 alkyl), C2-6 alkylene, COC1-6 alkylhalo, COR , COOR , CONHR , COC1-6alkylNR R or CONR C1-6alkylCONR R ; R is substituted C1-6 alkyl, optionally substituted phenyl(C1-4 alkyl), C2-6 alkylene, C1-6alkylhalo, COR , COOR , CONHR , COC1-6alkylNR R or CONR C1-6alkylCONR R ; or R and R together form a chain (CH2)p optionally substituted by oxo; R is H or C1-6 alkyl; R is H, C1-6 alkyl or phenyl; and R is optionally substituted (CH2)qphenyl; are tachykinin antagonists useful for treating pain.
摘要翻译：式（I）化合物及其盐和前药，其中Q为任选取代的苯基，杂芳基或萘基; X和Y各自为H，C 1-6烷基，C 2-6烯基或X和Y一起为= O; Z是O或S; R 1是H，任选取代的C 1-6烷基，任选取代的苯基（C 1-4烷基），C 2-6亚烷基，COC 1-6烷基卤素，COR a，COOR a，CONHR a，COCl C 1-6烷基NR a R a或CONR a C 1-6烷基CONR a R b; R 2是取代的C 1-6烷基，任选取代的苯基（C 1-4烷基），C 2-6亚烷基，C 1-6烷基卤素，COR a，COOR a，CONHR a，COC 1-6烷基， R b或CONR C 1-6烷基CONR a R b; 或R 1和R 2一起形成任选被氧代取代的链（CH 2）p; R 3是H或C 1-6烷基; R 4是H，C 1-6烷基或苯基; 和R 5是任选取代的（CH 2）q苯基; 是用于治疗疼痛的速激肽拮抗剂。

9. 发明申请

WO2011058112A1 FUSED BICYCLIC PYRAZOLE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：作为激酶抑制剂的熔融双相吡唑衍生物
公开(公告)号：WO2011058112A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/067308
申请日：2010-11-11
申请人： UCB PHARMA S.A. , ALLEN, Daniel, Rees , BÜRLI, Roland , OWENS, Andrew, Pate , SHARPE, Andrew
发明人： ALLEN, Daniel, Rees , BÜRLI, Roland , OWENS, Andrew, Pate , SHARPE, Andrew
IPC分类号： C07D487/04 , A61K31/519 , A61P29/00 , A61P35/00
CPC分类号： C07D487/04
摘要： A series of substituted pyrazolo[3,4- b ]pyridine and pyrazolo[3,4- d ]pyrimidine derivatives, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：作为P13激酶的选择性抑制剂的一系列取代的吡唑并[3,4-b]吡啶和吡唑并[3,4-d]嘧啶衍生物因此在医学中有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害性或眼科疾病。

10. 发明申请

WO2011058108A1 QUINOLINE AND QUINOXALINE DERIVATIVES AS KINASE INHIBITORS 审中-公开
标题翻译：喹啉和喹啉衍生物作为激酶抑制剂
公开(公告)号：WO2011058108A1
公开(公告)日：2011-05-19
申请号：PCT/EP2010/067304
申请日：2010-11-11
申请人： UCB PHARMA S.A. , ALLEN, Daniel, Rees , BÜRLI, Roland , HAUGHAN, Alan, Findlay , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SHARPE, Andrew
发明人： ALLEN, Daniel, Rees , BÜRLI, Roland , HAUGHAN, Alan, Findlay , MATTEUCCI, Mizio , OWENS, Andrew, Pate , RAPHY, Gilles , SHARPE, Andrew
IPC分类号： C07D403/04 , C07D487/04 , A61K31/517 , A61P29/00 , A61P25/28 , A61P35/00 , A61P9/00
CPC分类号： C07D403/04 , C07D487/04
摘要： A series of quinoline and quinoxaline derivatives, substituted by an optionally substituted bicyclic heteroaryl moiety consisting of two fused six-membered aromatic rings attached via an alkylene chain optionally linked to a heteroatom, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
摘要翻译：由任选取代的双环杂芳基部分取代的一系列喹啉和喹喔啉衍生物，由任选连接至杂原子的亚烷基链连接的两个稠合六元芳环构成，作为PI3激酶的选择性抑制剂，因此在医学上有益，例如在治疗炎症，自身免疫，心血管，神经变性，代谢，肿瘤，伤害感受或眼科疾病中。

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