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公开(公告)号：WO2012110833A2
公开(公告)日：2012-08-23
申请号：PCT/GB2012/050374
申请日：2012-02-20
申请人： ALMAC SCIENCES (SCOTLAND) LIMITED , ANDERSON, David , MALTMAN, Beatrice , DUNSMORE, Colin , HARRISON, Timothy , COTTON, Graham , TIRNAVEANU, Adina-elana
发明人： ANDERSON, David , MALTMAN, Beatrice , DUNSMORE, Colin , HARRISON, Timothy , COTTON, Graham , TIRNAVEANU, Adina-elana
IPC分类号： C07D209/82 , C07D215/14 , C07D241/46 , C07D265/38 , C07D271/12 , C07D279/22 , C07D307/80 , C07D333/60 , C07C229/36 , C07C309/40 , G01N33/542
CPC分类号： C07D279/22 , C07D209/82 , C07D215/14 , C07D241/46 , C07D265/38 , C07D271/12 , C07D307/80 , C07D333/60 , G01N33/542 , G01N2500/02 , G01N2500/04
摘要： The present invention relates to fluorescence lifetime modulators, conjugates comprising fluorescence lifetime modulators moieties and methods of making them. The present invention further relates to the use of the fluorescence lifetime modulators and conjugates comprising the fluorescence lifetime modulator moieties for measuring the activity and detection of enzymes and for the study of protein-protein and protein-ligand interactions.
摘要翻译： 本发明涉及荧光寿命调节剂，包含荧光寿命调节剂部分的缀合物及其制备方法。 本发明进一步涉及包含荧光寿命调节剂部分的荧光寿命调节剂和缀合物在测量酶的活性和检测以及研究蛋白质 - 蛋白质和蛋白质 - 配体相互作用中的用途。
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公开(公告)号：WO2006123182A3
公开(公告)日：2007-01-11
申请号：PCT/GB2006050107
申请日：2006-05-16
CPC分类号： A61K31/10
摘要： Sulphones of formula (I) are disclosed for use in treatment of cancer.
摘要翻译： 公开了用于治疗癌症的式（I）的手机。
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3.发明申请
公开(公告)号：WO2006123184A2
公开(公告)日：2006-11-23
申请号：PCT/GB2006/050109
申请日：2006-05-16
CPC分类号： A61K31/10
摘要： Compounds of formula (I) are disclosed for treatment of cancer.
摘要翻译： 公开了式（I）化合物用于治疗癌症。
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4.发明申请ARYLACETIC ACIDS AND RELATED COMPOUNDS FOR TREATMENT OF ALZHEIMER’S DISEASE 审中-公开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
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。
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公开(公告)号：WO2003013506A1
公开(公告)日：2003-02-20
申请号：PCT/GB2002/003559
申请日：2002-07-31
申请人： MERCK SHARP & DOHME LIMITED , HANNAM, Joanne, Claire , HARRISON, Timothy , MADIN, Andrew , SPAREY, Timothy, Jason
IPC分类号： A61K31/38
CPC分类号： C07D333/34
摘要： There is disclosed a novel class of sulphonamido-substituted bridged bicycloalkyl derivatives comprising a substituent on the bridgehead position. The compounds modulate the production of β-amyloid from amyloid precursor protein, and hence are useful in the treatment of Alzheimer's disease.
摘要翻译： 公开了一类新颖的磺酰胺基取代的桥连双环烷基衍生物，其包含桥头位置上的取代基。 该化合物调节淀粉样前体蛋白质中β-淀粉样蛋白的产生，因此可用于治疗阿尔茨海默氏病。
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公开(公告)号：WO1998024447A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006940
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
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , 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 for the manufacture of a medicament adapted for oral administration for the treatment or prevention of cognitive disorders, methods of medical 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CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防认知障碍的药物中的用途，使用这种NK- 1受体拮抗剂和包含它的药物组合物。
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7.发明申请
公开(公告)号：WO1998024444A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006690
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
IPC分类号： A61K31/535
CPC分类号： A61K31/661 , A61K31/00 , A61K31/395 , A61K31/438 , A61K31/445 , A61K31/451 , A61K31/5375 , A61K31/5377 , A61K31/675 , C07D211/56 , C07D491/10 , Y10S514/81 , Y10S514/811 , Y10S514/812 , Y10S514/813
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of substance use disorders, methods of treatment using such a NK-1 receptor antagonist and pharmaceutical compositions comprising the same.
摘要翻译： 本发明提供口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防物质使用障碍的药物中的用途，使用这种NK- 1受体拮抗剂和包含其的药物组合物。
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公开(公告)号：WO1998024442A1
公开(公告)日：1998-06-11
申请号：PCT/EP1997006687
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
IPC分类号： A61K31/535
CPC分类号： A61K31/445 , A61K9/2018 , A61K31/5375
摘要： The present invention provides the use of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist for the manufacture of a medicament adapted for oral administration for the treatment or prevention of sexual dysfunctions, methods of treatment using such an NK-1 receptor antagonist and pharmaceutical compositions comprising it.
摘要翻译： 本发明提供了口服活性的长效CNS渗透剂NK-1受体拮抗剂在制备适于口服给药以治疗或预防性功能障碍的药物中的用途，使用这种NK-1 受体拮抗剂和包含它的药物组合物。
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9.发明申请AZACYCLIC COMPOUNDS, PROCESSES FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM 审中-公开亚胺化合物，其制备方法和含有它们的药物组合物
公开(公告)号：WO1993004040A1
公开(公告)日：1993-03-04
申请号：PCT/GB1992001503
申请日：1992-08-13
申请人： MERCK SHARP & DOHME LIMITED , BAKER, Raymond , HARRISON, Timothy , SWAIN, Christopher, John , WILLIAMS, Brian, John
IPC分类号： C07D207/12
CPC分类号： C07D401/04 , C07D205/04 , C07D207/12 , C07D211/42 , C07D211/76 , C07D409/04
摘要： Compounds of formula (I), and salts and prodrugs thereof wherein n is 1, 2 or 3; X represents O or S; R1 represents optionally substituted phenyl; R2 represents aryl, heteroaryl, benzhydryl, or benzyl; R?4 and R5¿ each independently represent H, halo, CH¿2OR?9, C1-6alkyl, oxo, CO2R10 or CONR?10R11; R8¿ represents H, COR9, CO2R10 or optionally substituted C¿1-6?alkyl; R?9¿ represents H, C¿1-6?alkyl or phenyl; and R?10 and R11¿ each independently represent H or C¿1-6?alkyl; are tachykinin antagonists. They and compositions thereof are useful in medicine.
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公开(公告)号：WO2006123183A3
公开(公告)日：2007-06-14
申请号：PCT/GB2006050108
申请日：2006-05-16
IPC分类号： A61K31/5415 , A61P35/00
CPC分类号： A61K31/10 , A61K31/54 , A61K31/5415
摘要： Coumpounds of Formula (I) are disclosed for treatment of cancer.
摘要翻译： 公开了治疗癌症的式（I）化合物。
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