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1. 发明授权

US09273040B2 Benzoxazolinone compounds with selective activity in voltage-gated sodium channels 有权
标题翻译：在电压门控钠通道中具有选择性活性的苯并恶唑啉酮化合物
公开(公告)号：US09273040B2
公开(公告)日：2016-03-01
申请号：US14353488
申请日：2012-10-26
申请人： Mark E. Layton , Joseph E. Pero , Hannah Fiji , Michael J. Kelly, III , Pablo de Leon , Michael A. Rossi , Kevin F. Gilbert , Anthony J. Roecker , Zhijian Zhao , Swati I P. Mercer , Scott Wolkenberg , James Mulhearn , Lianyun Zhao , Dansu Li
发明人： Mark E. Layton , Joseph E. Pero , Hannah Fiji , Michael J. Kelly, III , Pablo de Leon , Michael A. Rossi , Kevin F. Gilbert , Anthony J. Roecker , Zhijian Zhao , Swati I P. Mercer , Scott Wolkenberg , James Mulhearn , Lianyun Zhao , Dansu Li
IPC分类号： A61K31/00 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/107 , C07D493/10
CPC分类号： C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/107 , C07D493/10
摘要： Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式（A）的化合物或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。还描述了包含式（A）化合物或其盐的药物制剂，以及使用其制备神经性疼痛障碍的方法。

2. 发明授权

US10519147B2 Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels 有权
公开(公告)号：US10519147B2
公开(公告)日：2019-12-31
申请号：US16061815
申请日：2016-12-15
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
发明人： Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
IPC分类号： C07D417/12 , A61K45/06 , C07D277/52 , C07D285/135 , A61P25/02 , A61P25/04 , A61P11/14 , A61P17/04
摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

3. 发明申请

US20180362518A1 DIAMINO-ALKYLAMINO-Linked ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 审中-公开
公开(公告)号：US20180362518A1
公开(公告)日：2018-12-20
申请号：US16061815
申请日：2016-12-15
申请人： Thomas J. GRESHOCK , James MULHEARN , Liangqin GUO , Ting ZHANG , Deping WANG , Ronald M. KIM , Mark E. LAYTON , Michael J. KELLY, III , Rajan ANAND , Tianying JIAN , Philippe NANTERMET , Anthony J. ROECKER , Walter WON , Gang ZHOU , Merck Sharp & Dohme Corp.
发明人： Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
IPC分类号： C07D417/12 , C07D285/135 , C07D277/52 , A61P11/14 , A61P17/04 , A61P25/04 , A61P25/02
CPC分类号： C07D417/12 , A61K45/06 , A61P11/14 , A61P17/04 , A61P25/02 , A61P25/04 , C07D277/52 , C07D285/135
摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.

4. 发明授权

US10968210B2 Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels 有权
公开(公告)号：US10968210B2
公开(公告)日：2021-04-06
申请号：US16345913
申请日：2017-11-13
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
发明人： Thomas J. Greshock , James Mulhearn , Anthony J. Roecker , Tianying Jian , Gang Zhou , Liangqin Guo , Walter Won , Ting Zhang , Rajan Anand , John E. Stelmach , Deping Wang , Ronald M. Kim , Mark E. Layton , Christopher S. Burgey , Philippe G. Nantermet
IPC分类号： C07D417/12 , C07D417/14 , C07D277/52 , C07D471/04 , C07D487/10 , C07D401/12 , C07D471/08 , C07D471/10 , C07D487/04 , C07D487/08
摘要： Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.

5. 发明授权

US09024032B2 Inhibitors of catechol O-methyl transferase and their use in the treatment of psychotic disorders 有权
标题翻译：儿茶酚O-甲基转移酶的抑制剂及其在治疗精神病中的应用
公开(公告)号：US09024032B2
公开(公告)日：2015-05-05
申请号：US13582601
申请日：2011-02-28
申请人： Scott Wolkenberg , James C. Barrow , Michael S. Poslusney , Scott T. Harrison , B. Wesley Trotter , James Mulhearn , Kausik K. Nanda , Peter J. Manley , Zhijian Zhao , Jeffrey W. Schubert , Nathan Kett , Amy Zartman
发明人： Scott Wolkenberg , James C. Barrow , Michael S. Poslusney , Scott T. Harrison , B. Wesley Trotter , James Mulhearn , Kausik K. Nanda , Peter J. Manley , Zhijian Zhao , Jeffrey W. Schubert , Nathan Kett , Amy Zartman
IPC分类号： A61K31/44 , C07D211/90 , C07D213/69 , A61K31/4412 , A61K31/4418 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/4709 , A61K31/4725 , A61K31/5377 , A61K31/541 , A61K31/69 , A61K45/06 , C07D213/73 , C07D213/74 , C07D401/10 , C07D401/14 , C07D413/10 , C07D413/12 , C07D417/10 , C07D471/04 , C07F5/02 , C07D401/04 , C07D401/06
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。

6. 发明申请

US20130084346A1 INHIBITORS OF CATECHOL O-METHYL TRANSFERASE AND THEIR USE IN THE TREATMENT OF PSYCHOTIC DISORDERS 有权
公开(公告)号：US20130084346A1
公开(公告)日：2013-04-04
申请号：US13582601
申请日：2011-02-28
申请人： Scott Wolkenberg , James C. Barrow , Michael S. Poslusney , Scott T. Harrison , B. Wesley Trotter , James Mulhearn , Kausik K. Nanda , Peter J. Manley , Zhijian Zhao , Jeffrey W. Schubert , Nathan Kett , Amy Zartman
发明人： Scott Wolkenberg , James C. Barrow , Michael S. Poslusney , Scott T. Harrison , B. Wesley Trotter , James Mulhearn , Kausik K. Nanda , Peter J. Manley , Zhijian Zhao , Jeffrey W. Schubert , Nathan Kett , Amy Zartman
IPC分类号： C07D213/69 , C07D401/10 , A61K31/4439 , C07D213/73 , C07D213/74 , C07F5/02 , A61K31/69 , A61K31/444 , C07D401/14 , C07D471/04 , A61K31/4725 , A61K31/4709 , A61K45/06 , C07D413/10 , A61K31/5377 , A61K31/4545 , C07D417/10 , A61K31/541 , C07D413/12 , A61K31/4418
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.

7. 发明申请

US20110076230A1 Novel Substituted Indoles 审中-公开
标题翻译：新型取代吲哚
公开(公告)号：US20110076230A1
公开(公告)日：2011-03-31
申请号：US12995353
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Scott Wolkenberg
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Scott Wolkenberg
IPC分类号： A61K51/00 , A61K49/00 , A61K49/06 , A61K31/4439 , A61K31/437 , C07D471/04 , C07D401/04 , C07D401/14 , A61K31/497 , A61P25/28 , A61P25/18
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。

8. 发明申请

US20110081297A1 Novel Substituted Pyrazoles, 1,2,4-Oxadiazoles, and 1,3,4-Oxadiazoles 审中-公开
标题翻译：新型取代的吡唑，1,2,4-恶二唑和1,3,4-恶二唑
公开(公告)号：US20110081297A1
公开(公告)日：2011-04-07
申请号：US12995412
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
IPC分类号： A61K49/10 , C07D413/04 , A61K31/4439 , A61P25/28 , A61K49/00 , A61K49/04 , C07D413/10 , A61K31/4245 , C07D231/12 , A61K31/415 , C07D471/02 , A61K31/437
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。

9. 发明授权

US08530483B2 Substituted azabenzoxazoles 有权
标题翻译：取代的氮杂苯并唑
公开(公告)号：US08530483B2
公开(公告)日：2013-09-10
申请号：US12995314
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg , Eric Hostetler
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg , Eric Hostetler
IPC分类号： A01N43/90 , A01N43/42 , A61K31/519 , A61K31/44 , C07D239/00 , C07D471/00 , C07D491/00 , C07D513/02 , C07D515/02 , C07D471/02 , C07D491/02 , C07D498/02
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to novel amyloid binding compounds of formula (I) 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, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH.
摘要翻译：本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。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或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH。

10. 发明申请

US20110085985A1 NOVEL SUBSTITUTED AZABENZOXAZOLES 有权
标题翻译：新型取代的AZABENZOXAZOLES
公开(公告)号：US20110085985A1
公开(公告)日：2011-04-14
申请号：US12995314
申请日：2009-05-28
申请人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
发明人： James C. Barrow , Scott Harrison , James Mulhearn , Cyrille Sur , David L. Williams , Scott Wolkenberg
IPC分类号： A61K31/437 , C07D498/04 , C07D519/00 , A61K31/5377 , A61K49/00 , A61K49/04 , A61K49/06 , A61P25/28 , A61P25/18
CPC分类号： C07D498/04 , C07D519/00
摘要： The present invention relates to novel amyloid binding compounds of formula (I) 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, or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof, wherein: X is O or S; A and Y independently are N, or CH;
摘要翻译：本发明涉及式（I）的新型淀粉样蛋白结合化合物和通过测定活体患者淀粉样斑块水平的变化来测定化合物的效果的方法。更具体地说，本发明涉及使用本发明化合物作为正电子发射断层摄影（PET /）成像中的示踪剂来研究脑中淀粉样蛋白沉积物以允许诊断阿尔茨海默病的方法。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或其药学上可接受的盐，溶剂合物或体内可水解的酯的治疗用途和方法，其中：X是O或S; A和Y独立地为N或CH;

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