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1.发明申请SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开SPIROPIPERIDINEβ-分泌酶抑制剂治疗ALZEIMER'S DISEASE
公开(公告)号：WO2008054698A2
公开(公告)日：2008-05-08
申请号：PCT/US2007/022819
申请日：2007-10-29
IPC分类号： A01N43/42
CPC分类号： C07D471/10
摘要： The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及式（I）的螺哌啶化合物，它们是β-分泌酶的抑制剂并且可用于治疗β-分泌酶参与的疾病，例如 作为阿尔茨海默氏病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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公开(公告)号：WO2011011312A1
公开(公告)日：2011-01-27
申请号：PCT/US2010/042419
申请日：2010-07-19
申请人： MERCK SHARP & DOHME CORP. , DE LEON, Pablo , EGBERTSON, Melissa , HILLS, Ivory, D. , JOHNSON, Adam Wayne , MACHACEK, Michelle
发明人： DE LEON, Pablo , EGBERTSON, Melissa , HILLS, Ivory, D. , JOHNSON, Adam Wayne , MACHACEK, Michelle
IPC分类号： A61K31/47
CPC分类号： A61K31/47 , C07D215/22 , C07D215/227 , C07D401/14 , C07D409/04 , C07D409/14
摘要： The present invention is directed to quinolinone compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
摘要翻译： 本发明涉及可用作治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病的治疗剂的喹啉酮化合物。 本发明还涉及这些化合物用于治疗神经和精神疾病如精神分裂症，精神病或亨廷顿病以及与纹状体功能减退或基底神经节功能障碍相关的疾病的用途。
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3.发明申请2-AMINOIMIDAZOLE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开用于治疗阿尔茨海默病的2-氨基咪唑β-分泌酶抑制剂
公开(公告)号：WO2009108550A1
公开(公告)日：2009-09-03
申请号：PCT/US2009/034377
申请日：2009-02-18
申请人： MERCK & CO., INC. , HILLS, Ivory, D. , COBURN, Craig, A. , GRAHAM, Samuel, L. , MOORE, Keith, P. , NANTERMET, Philippe, G. , RAJAPAKSE, Hemaka, A. , STACHEL, Shawn, J. , ZHU, Hong
发明人： HILLS, Ivory, D. , COBURN, Craig, A. , GRAHAM, Samuel, L. , MOORE, Keith, P. , NANTERMET, Philippe, G. , RAJAPAKSE, Hemaka, A. , STACHEL, Shawn, J. , ZHU, Hong
IPC分类号： A01N43/50 , A61K31/415
CPC分类号： C07D233/88 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/14 , C07D403/06 , C07D403/10 , C07D405/06 , C07D405/10 , C07D409/10 , C07D413/10
摘要： The present invention is directed to 2-aminoimidazole compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默病的式（I）的2-氨基咪唑化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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4.发明申请
公开(公告)号：WO2011153120A1
公开(公告)日：2011-12-08
申请号：PCT/US2011/038490
申请日：2011-05-31
申请人： MERCK SHARP & DOHME CORP. , BUDZIK, Brian, W. , COLLETTI, Steven, L. , DAVIS, Jennifer, R. , HILLS, Ivory, D. , SEIFRIED, Darla, D. , STANTON, Matthew, G.
发明人： BUDZIK, Brian, W. , COLLETTI, Steven, L. , DAVIS, Jennifer, R. , HILLS, Ivory, D. , SEIFRIED, Darla, D. , STANTON, Matthew, G.
CPC分类号： C07C217/46 , A61K9/1272 , A61K47/18 , C07C43/15 , C07C217/44 , C07D205/04 , C07D207/08 , C07D295/084 , C07D317/28 , C12N15/87
摘要： The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
摘要翻译： 本发明提供了可以与其它脂质组分如胆固醇和PEG-脂质组合使用以与寡核苷酸形成脂质纳米颗粒的新型阳离子脂质。 本发明的目的是提供一种阳离子脂质支架，由于肝中脂质水平降低，其表现出增强的功效以及较低的肝毒性。 本发明使用具有一个短脂链的低分子量阳离子脂质以增强siRNA的体内递送的效率和耐受性。
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公开(公告)号：WO2010077752A1
公开(公告)日：2010-07-08
申请号：PCT/US2009/067412
申请日：2009-12-10
申请人： MERCK SHARP & DOHME CORP. , SELNICK, Harold G. , WOOD, Michael R. , MCWHERTER, Melody , HILLS, Ivory D. , STUMP, Craig A.
IPC分类号： A01N43/50
CPC分类号： C07D471/10 , C07D235/02 , C07D471/20 , C07D491/10 , C07D519/00
摘要： The present invention is directed to imidazolinone derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
摘要翻译： 本发明涉及作为CGRP受体的拮抗剂的咪唑啉酮衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及CGRP的疾病中的用途。
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6.发明申请SPIROPIPERIDINE BETA-SECRETASE INHIBITORS FOR THE TREATMENT OF ALZHEIMER'S DISEASE 审中-公开用于治疗阿尔茨海默病的螺旋剂β-分泌酶抑制剂
公开(公告)号：WO2008054698A3
公开(公告)日：2008-06-19
申请号：PCT/US2007022819
申请日：2007-10-29
发明人： STAUFFER SHAUN R , HILLS IVORY D , NOMLAND ASHLEY
CPC分类号： C07D471/10
摘要： The present invention is directed to spiropiperidine compounds of formula (I) which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.
摘要翻译： 本发明涉及作为β-分泌酶的抑制剂并且可用于治疗其中涉及β-分泌酶的疾病如阿尔茨海默氏病的式（I）的哌啶哌啶化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在治疗涉及β-分泌酶的疾病中的用途。
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