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1. 发明申请

WO2009146343A1 NOVEL SUBSTITUTED PYRAZOLES, 1,2,4-OXADIAZOLES, AND 1,3,4-OXADIAZOLES 审中-公开
标题翻译：新型取代的吡咯，1,2,4-氧杂环己烷和1,3,4-氧杂双环
公开(公告)号：WO2009146343A1
公开(公告)日：2009-12-03
申请号：PCT/US2009/045368
申请日：2009-05-28
申请人： MERCK & CO., INC. , BARROW, James, C. , HARRISON, Scott , MULHEARN, James , SUR, Cyrille , WILLIAMS, David, L. , WOLKENBERG, Scott
发明人： BARROW, James, C. , HARRISON, Scott , MULHEARN, James , SUR, Cyrille , WILLIAMS, David, L. , WOLKENBERG, Scott
IPC分类号： C07D271/06
CPC分类号： C07D231/12 , C07D271/06 , C07D271/10 , C07D403/04 , C07D413/04 , C07D413/14 , C07D417/04 , F22B35/001 , F22B35/002 , F22B37/00 , F23C9/00 , F23J15/006 , F23J15/06 , F23L7/007 , Y02E20/344 , Y02E20/363
摘要： The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted pyrazole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者淀粉样斑块水平的变化来测量化合物的效果的新型淀粉样蛋白结合化合物和方法。更具体地说，本发明涉及在正电子发射断层摄影（PET）成像中使用本发明化合物作为示踪剂的方法，以在体内研究脑中的淀粉样蛋白沉积物以允许诊断阿尔茨海默氏病。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的吡唑衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

2. 发明申请

WO2009155024A1 NOVEL SUBSTITUTED INDOLES 审中-公开
标题翻译：新的替代品
公开(公告)号：WO2009155024A1
公开(公告)日：2009-12-23
申请号：PCT/US2009/045403
申请日：2009-05-28
申请人： MERCK & CO., INC. , BARROW, James, C. , HARRISON, Scott , MULHEARN, James , WOLKENBERG, Scott
发明人： BARROW, James, C. , HARRISON, Scott , MULHEARN, James , WOLKENBERG, Scott
IPC分类号： A01N43/56 , A61K31/405
CPC分类号： C07D471/04 , C07D401/04 , C07D401/14
摘要： The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted indole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者淀粉样斑块水平的变化来测量化合物的效果的新型淀粉样蛋白结合化合物和方法。更具体地说，本发明涉及在正电子发射断层摄影（PET）成像中使用本发明化合物作为示踪剂的方法，以在体内研究脑中的淀粉样蛋白沉积物以允许诊断阿尔茨海默氏病。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的吲哚衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

3. 发明申请

WO2009155017A2 NOVEL SUBSTITUTED AZABENZOXAZOLES 审中-公开
标题翻译：新型取代的AZABENZOXAZOLES
公开(公告)号：WO2009155017A2
公开(公告)日：2009-12-23
申请号：PCT/US2009/045376
申请日：2009-05-28
申请人： MERCK & CO., INC. , BARROW, James, C. , HARRISON, Scott , MULHEARN, James , SUR, Cyrille , WILLIAMS, David, L. , WOLKENBERG, Scott
发明人： BARROW, James, C. , HARRISON, Scott , MULHEARN, James , SUR, Cyrille , WILLIAMS, David, L. , WOLKENBERG, Scott
IPC分类号： C07D498/04 , C07D519/00 , A61P25/28 , A61K31/4353
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds.
摘要翻译：本发明涉及通过测量活体患者淀粉样斑块水平的变化来测量化合物的效果的新型淀粉样蛋白结合化合物和方法。更具体地说，本发明涉及在正电子发射断层摄影（PET）成像中使用本发明化合物作为示踪剂的方法，以在体内研究脑中的淀粉样蛋白沉积物以允许诊断阿尔茨海默氏病。因此，本发明涉及新型淀粉样蛋白结合化合物作为诊断用途。本发明还涉及测量阿尔茨海默病治疗剂的临床疗效的方法。具体地，本发明涉及新的芳基或杂芳基取代的氮杂苯并恶唑衍生物，组合物，以及用于制备这些化合物的治疗用途和方法。

4. 发明申请

WO2011109254A1 INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
标题翻译： CATECHOL O-METHYL TRANSFERASE的抑制剂及其在治疗心理疾病中的应用
公开(公告)号：WO2011109254A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/026399
申请日：2011-02-28
申请人： MERCK SHARP & DOHME CORP. , WOLKENBERG, Scott , BARROW, James, C. , POSLUSNEY, Michael, S. , HARRISON, Scott, T. , TROTTER, B. Wesley , MULHEARN, James , NANDA, Kausik, K. , MANLEY, Peter, J. , ZHAO, Zhijian , SCHUBERT, Jeffrey, W. , KETT, Nathan , ZARTMAN, Amy
发明人： WOLKENBERG, Scott , BARROW, James, C. , POSLUSNEY, Michael, S. , HARRISON, Scott, T. , TROTTER, B. Wesley , MULHEARN, James , NANDA, Kausik, K. , MANLEY, Peter, J. , ZHAO, Zhijian , SCHUBERT, Jeffrey, W. , KETT, Nathan , ZARTMAN, Amy
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07F5/025 , A61K31/4412 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D213/69 , C07D213/73 , C07D213/74 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/14 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04
摘要： The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
摘要翻译：本发明涉及作为儿茶酚O-甲基转移酶（COMT）的抑制剂的4-吡啶酮化合物，可用于治疗和预防涉及COMT酶的神经和精神疾病和疾病。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预防或治疗涉及COMT的疾病中的用途。

5. 发明申请

WO2011109267A1 INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
公开(公告)号：WO2011109267A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/026424
申请日：2011-02-28
申请人： MERCK SHARP & DOHME CORP. , WOLKENBERG, Scott , HARRISON, Scott, T. , BARROW, James, C. , ZHAO, Zhijian , MELAMED, Jeffrey , KETT, Nathan , ZARTMAN, Amy
发明人： WOLKENBERG, Scott , HARRISON, Scott, T. , BARROW, James, C. , ZHAO, Zhijian , MELAMED, Jeffrey , KETT, Nathan , ZARTMAN, Amy
IPC分类号： A01N43/90 , A61K31/505 , A61K31/519
CPC分类号： C07D401/14 , A61K31/505 , A61K31/513 , A61K31/519 , A61K45/06 , C07D239/54 , C07D239/553 , C07D401/04 , C07D401/10 , C07D403/10 , C07D405/10 , C07D409/10 , C07D413/10 , C07D417/10 , C07D471/04 , C07D498/04
摘要： The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.

6. 发明申请

WO2011109261A1 INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS 审中-公开
标题翻译：儿茶素O-甲基转移酶抑制剂及其在治疗精神障碍中的应用
公开(公告)号：WO2011109261A1
公开(公告)日：2011-09-09
申请号：PCT/US2011/026414
申请日：2011-02-28
申请人： MERCK SHARP & DOHME CORP. , WOLKENBERG, Scott , BARROW, James, C. , HARRISON, Scott, T. , TROTTER, B. Wesley , NANDA, Kausik, K. , MANLEY, Peter, J. , ZHAO, Zhijian
发明人： WOLKENBERG, Scott , BARROW, James, C. , HARRISON, Scott, T. , TROTTER, B. Wesley , NANDA, Kausik, K. , MANLEY, Peter, J. , ZHAO, Zhijian
IPC分类号： A01N43/40 , A61K31/44
CPC分类号： C07D213/69 , C07D211/86 , C07D213/84 , C07D213/85 , C07D401/04 , C07D413/10 , C07D417/04
摘要： The present invention relates to 4-pyridinone compounds which are inhibitors of catechol O-methyltransferase (COMT), and are useful in the treatment and prevention of neurological and psychiatric disorders and diseases in which COMT enzyme is involved. The present invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which COMT is involved.
摘要翻译：本发明涉及作为儿茶酚O-甲基转移酶（COMT）抑制剂的4-吡啶酮化合物，并且可用于治疗和预防其中涉及COMT酶的神经病学和精神病学障碍和疾病。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预防或治疗其中涉及COMT的疾病中的用途。

7. 发明申请

WO2009054984A1 HETEROCYCLE PHENYL AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：杂环苯胺类T型钙通道拮抗剂
公开(公告)号：WO2009054984A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/012039
申请日：2008-10-23
申请人： MERCK & CO., INC. , BARROW, James, C. , COLEMAN, Paul, J. , REGER, Thomas, S. , SCHLEGEL, Kelly-ann, S. , SHU, Youheng , YANG, Zhi-Qiang
发明人： BARROW, James, C. , COLEMAN, Paul, J. , REGER, Thomas, S. , SCHLEGEL, Kelly-ann, S. , SHU, Youheng , YANG, Zhi-Qiang
IPC分类号： C07D213/65 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04 , A61K31/44 , A61P25/08
CPC分类号： C07D401/12 , C07D213/65 , C07D405/12 , C07D413/12 , C07D417/12 , C07D487/04
摘要： The present invention is directed to heterocycle phenyl amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
摘要翻译：本发明涉及作为T型钙通道拮抗剂的杂环苯酰胺化合物，其可用于治疗或预防涉及T型钙通道的疾病和疾病。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预防或治疗涉及T型钙通道的疾病中的用途。

8. 发明申请

WO2009042094A2 HIV PROTEASE INHIBITORS 审中-公开
标题翻译：艾滋病病毒蛋白酶抑制剂
公开(公告)号：WO2009042094A2
公开(公告)日：2009-04-02
申请号：PCT/US2008/010972
申请日：2008-09-22
申请人： MERCK & CO., INC. , COBURN, Craig, A. , VACCA, Joseph, P. , RAJAPAKSE, Hemaka, A. , JONES, Kristen, L. G. , NANTERMET, Philippe , BARROW, James, C. , MOORE, Keith, P. , THEBERGE, Cory , WALJI, Abbas, M.
发明人： COBURN, Craig, A. , VACCA, Joseph, P. , RAJAPAKSE, Hemaka, A. , JONES, Kristen, L. G. , NANTERMET, Philippe , BARROW, James, C. , MOORE, Keith, P. , THEBERGE, Cory , WALJI, Abbas, M.
IPC分类号： A61K31/675
CPC分类号： C07C311/41 , C07C311/18 , C07C311/29 , C07C2601/02 , C07C2601/08
摘要： Compounds of Formula A are disclosed: (A), wherein X A , k, R 1 , R 2 , R 3 , R 4 , R 5 , R 5A , R 6 and R 7 are defined herein. The compounds encompassed by Formula A include compounds which are HIV protease inhibitors and other compounds which can be metabolized in vivo to HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
摘要翻译：公开了式A的化合物：（A），其中XA，k，R1，R2，R3，R4，R5，R5A，R6和R7如本文所定义。由式A包括的化合物包括可以在体内代谢为HIV蛋白酶抑制剂的HIV蛋白酶抑制剂和其它化合物的化合物。化合物及其药学上可接受的盐可用于预防或治疗HIV感染以及预防，治疗或延迟艾滋病的发病。化合物及其盐可以用作药物组合物中的成分，任选与其它抗病毒剂，免疫调节剂，抗生素或疫苗组合使用。

9. 发明申请

WO2007002884A3 4-FLUORO-PIPERIDINE T-TYPE CALCIUM CHANNEL ANTAGONISTS 审中-公开
公开(公告)号：WO2007002884A3
公开(公告)日：2007-01-04
申请号：PCT/US2006/025496
申请日：2006-06-28
申请人： MERCK & CO., INC. , BARROW, James, C. , LINDSLEY, Craig, W. , SHIPE, William, D. , YANG, Zhiqiang , WISNOSKI, David
发明人： BARROW, James, C. , LINDSLEY, Craig, W. , SHIPE, William, D. , YANG, Zhiqiang , WISNOSKI, David
IPC分类号： A61K31/495 , C07D295/00 , C07D211/00
摘要： The present invention is directed to 4-fluoro-piperidine compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.

10. 发明申请

WO2009054983A1 HETEROCYCLE AMIDE T-TYPE CALCIUM CHANNEL ANTAGONISTS 审中-公开
标题翻译：杂交酰胺T型钙通道拮抗剂
公开(公告)号：WO2009054983A1
公开(公告)日：2009-04-30
申请号：PCT/US2008/012038
申请日：2008-10-23
申请人： MERCK & CO., INC. , BARROW, James, C. , REGER, Thomas, S. , SHU, Youheng , YANG, Zhi-Qiang
发明人： BARROW, James, C. , REGER, Thomas, S. , SHU, Youheng , YANG, Zhi-Qiang
IPC分类号： C07D223/10
CPC分类号： C07D405/12 , C07D401/12 , C07D413/12 , C07D487/04
摘要： The present invention is directed to heterocycle amide compounds which are antagonists of T-type calcium channels, and which are useful in the treatment or prevention of disorders and diseases in which T-type calcium channels are involved. 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 T-type calcium channels are involved.
摘要翻译：本发明涉及作为T型钙通道拮抗剂的杂环酰胺化合物，其可用于治疗或预防涉及T型钙通道的疾病和疾病。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预防或治疗涉及T型钙通道的疾病中的用途。

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