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61. 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。

62. 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。

63. 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。

64. 发明申请

WO1998024439A1 USE OF NK-1 RECEPTOR ANTAGONISTS FOR TREATING SEVERE ANXIETY DISORDERS 审中-公开
标题翻译：使用NK-1受体拮抗剂治疗严重的恶心病
公开(公告)号：WO1998024439A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006683
申请日：1997-11-25
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , CURTIS, Neil, Roy , ELLIOTT, Jason, Matthew , HARRISON, Timothy , HOLLINGWORTH, Gregory, John , JACKSON, Philip, Stephen , KULAGOWSKI, Janusz, Jozef , RUPNIAK, Nadia, Melanie , SEWARD, Eileen, Mary , SWAIN, Christopher, John , WILLIAMS, Brian, John
发明人： MERCK SHARP & DOHME LIMITED
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist in a medicament adapted for oral administration for the treatment or prevention of severe anxiety disorders without concomitant therapy with other anti-anxiety agents, methods of treatment using such an NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译：本发明提供口服活性的长效中枢神经系统渗透性NK-1受体拮抗剂在适于口服给药以治疗或预防严重焦虑症的药物中的用途，而不与其他抗焦虑剂并用治疗，方法使用这种NK-1受体拮抗剂的治疗剂和包含它的药物组合物。

65. 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。

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