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公开(公告)号:US09815846B2
公开(公告)日:2017-11-14
申请号:US15128689
申请日:2015-03-23
发明人: Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Yi-Heng Chen , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Swati P. Mercer , Kerim Babaoglu , Dongfang Meng , Jane Wu , Ping Liu , Harold B. Wood , Jianming Bao , Chun Sing Li , Qinghua Mao , Zhiqi Qi
IPC分类号: C07D491/107 , C07C233/66 , C07D213/75 , C07D403/12 , C07D401/12 , C07D417/12 , C07D239/42 , C07D401/04 , C07D413/12 , C07D417/14 , C07D401/14 , C07D405/12 , C07D413/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07D401/06 , C07D413/06 , C07D403/06
CPC分类号: C07D491/107 , C07C233/66 , C07D213/75 , C07D231/12 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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公开(公告)号:US20170114071A1
公开(公告)日:2017-04-27
申请号:US15128689
申请日:2015-03-23
发明人: Helen Mitchell , Mark E. Fraley , Andrew J. Cooke , Craig A. Stump , Yi- Heng Chen , Xu-Fang Zhang , Casey C. McComas , Kathy Schirripa , Melody McWherter , Swati P. Mercer , Kerim Babaoglu , Dongfang Meng , Jane Wu , Ping Liu , Harold B. Wood , Jianming Bao , Chun Sing Li , Qinghua Mao , Zhiqi Qi
IPC分类号: C07D491/107 , C07D403/12 , C07D401/12 , C07C233/66 , C07D417/12 , C07D239/42 , C07D401/04 , C07D413/12 , C07D417/14 , C07D401/14 , C07D405/12 , C07D413/14 , C07D403/14 , C07D405/14 , C07D471/04 , C07D401/06 , C07D413/06 , C07D403/06 , C07D213/75
CPC分类号: C07D491/107 , C07C233/66 , C07D213/75 , C07D231/12 , C07D239/42 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04
摘要: The present invention is directed to six membered heteroaryl benzamide compounds of formula (I), which are tropomyosin-related kinase (Trk) family protein pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA.
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公开(公告)号:US20210188818A1
公开(公告)日:2021-06-24
申请号:US16755177
申请日:2018-10-08
发明人: John Acton , David Annunziato Candito , J. Michael Ellis , Peter H. Fuller , Hakan Gunaydin , Blair T. Lapointe , Weiguo Liu , Joey L. Methot , Santhosh F. Neelamkavil , Barbara Pio , Vladimir Simov , Harold B. Wood
IPC分类号: C07D403/14 , C07D401/14 , C07D498/10 , C07D498/04 , C07D413/14 , C07D519/00 , C07D405/14
摘要: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.
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公开(公告)号:US20210069288A1
公开(公告)日:2021-03-11
申请号:US17005686
申请日:2020-08-28
发明人: Hubert Josien , Abbas Walji , Harold B. Wood , Fa-Xiang Ding , Jian Liu , Thomas Joseph Tucker , Michael Man-Chu Lo , Liangqin Guo
摘要: Disclosed are compounds of Formula A, or a pharmaceutically acceptable salt thereof: where A, X, R1, and R2 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
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公开(公告)号:US20190389909A1
公开(公告)日:2019-12-26
申请号:US16446940
申请日:2019-06-20
发明人: Harold B. Wood , Hubert B. Josien , Thomas Joseph Tucker , Angela Dawn Kerekes , Ling Tong , Abbas M. Walji , Anilkumar G. Nair , Fa-Xiang Ding , Elisabetta Bianchi , Danila Branca , Chengwei Wu , Yusheng Xiong , Sookhee Nicole HA , Jian Liu , Sobhana Babu Boga
摘要: Disclosed are compounds of Formula I, or a salt thereof: where A, B, D, X, R1, R2 and R8 are as defined herein, which compounds have properties for antagonizing PCSK9. Also described are pharmaceutical formulations comprising the compounds of Formula I or their salts, and methods of treating cardiovascular disease and conditions related to PCSK9 activity, e.g. atherosclerosis, hypercholesterolemia, coronary heart disease, metabolic syndrome, acute coronary syndrome, or related cardiovascular disease and cardiometabolic conditions.
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公开(公告)号:US09018224B2
公开(公告)日:2015-04-28
申请号:US14358241
申请日:2012-11-09
发明人: Scott Edmondson , Zhiyong Hu , Ping Liu , Gregori J. Morriello , Jason W. Szewczyk , Bowei Wang , Liping Wang , Harold B. Wood , Cheng Zhu , Yuping Zhu , Zhiqiang Guo
IPC分类号: A01N43/54 , A61K31/505 , C07D513/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/04 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04 , C07D239/42 , C07D403/12 , C07D403/14 , C07D405/12 , C07D409/12
CPC分类号: C07D513/04 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.
摘要翻译: 披露式(I)的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。
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公开(公告)号:US11174248B2
公开(公告)日:2021-11-16
申请号:US16755177
申请日:2018-10-08
发明人: John Acton , David Annunziato Candito , J. Michael Ellis , Peter H. Fuller , Hakan Gunaydin , Blair T. Lapointe , Weiguo Liu , Joey L. Methot , Santhosh F. Neelamkavil , Barbara Pio , Vladimir Simov , Harold B. Wood
IPC分类号: A61K31/506 , C07D403/14 , C07D401/14 , C07D405/14 , C07D413/14 , C07D498/04 , C07D498/10 , C07D519/00
摘要: The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1A, R1B, X, Y, RZ and R2 are as defined herein, which are potent inhibitors of LRRK2 kinase and useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.
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公开(公告)号:US11161854B2
公开(公告)日:2021-11-02
申请号:US16755172
申请日:2018-10-08
申请人: Merck Sharp & Dohme Corp. , David Annunziato Candito , Thomas H. Graham , John Acton , Ryan Wing-Kun Chau , Joanna L. Chen , J. Michael Ellis , Peter H. Fuller , Anmol Gulati , Hakan Gunaydin , Solomon Kattar , Mitchell Henry Keylor , Blair T. Lapointe , Ping Liu , Weiguo Liu , Joey L. Methot , Santhosh F. Neelamkavil , Vladimir Simov , Ling Tong , Harold B. Wood
发明人: David Annunziato Candito , Thomas H. Graham , John Acton , Ryan Wing-Kun Chau , Joanna L. Chen , J. Michael Ellis , Peter H. Fuller , Anmol Gulati , Hakan Gunaydin , Solomon Kattar , Mitchell Henry Keylor , Blair T. Lapointe , Ping Liu , Weiguo Liu , Joey L. Methot , Santhosh F. Neelamkavil , Vladimir Simov , Ling Tong , Harold B. Wood
IPC分类号: C07D491/10 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D413/14 , C07D487/08 , C07D498/04 , C07D498/10 , C07D519/00
摘要: The present invention is directed to substituted certain reversed indazolyl-spiro[2.2]pentane-carbonitrile derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, X, Y, and Z are as defined herein, which are potent inhibitors of LRRK2 kinase and may be useful in the treatment or prevention of diseases in which the LRRK2 kinase is involved, such as Parkinson's Disease and other diseases and disorders described herein. 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 LRRK-2 kinase is involved.
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公开(公告)号:US20180030036A1
公开(公告)日:2018-02-01
申请号:US15534029
申请日:2015-12-07
申请人: Ting ZHANG , Yi-Heng CHEN , Liangqin GUO , Alan HARUZA , Tianying JIAN , Bing LI , Dongfang MENG , Dann L. PARKER, JR. , Edward C. SHERER , Harold B. WOOD , Isao SAKURADA , MERCK SHARP & DOHME CORP. , MOCHIDA PHARMACEUTICAL CO., LTD
发明人: Ting Zhang , Yi-Heng Chen , Liangqin Guo , Alan Hruza , Tianying Jian , Bing Li , Dongfang Meng , Dann L. Parker , Edward C. Sherer , Harold B. Wood , Isao Sakurada
IPC分类号: C07D403/12 , C07D401/14 , C07D401/12 , C07D471/04
CPC分类号: C07D403/12 , C07D401/12 , C07D401/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D471/04
摘要: The present invention provides a compound of Formula I, and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing unstable angina, refractory angina, myocardial infarction, transient ischemic attacks, atrial fibrillation, thrombotic stroke, embolic stroke, deep vein thrombosis, disseminated intravascular coagulation, ocular build up of fibrin, and reocclusion or restenosis of recanalized vessels. The compounds are selective Factor IXa inhibitors.
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公开(公告)号:US20140329798A1
公开(公告)日:2014-11-06
申请号:US14358241
申请日:2012-11-09
发明人: Scott Edmondson , Zhiyong Hu , Ping Liu , Gregori J. Morriello , Jason W. Szewczyk , Bowei Wang , Liping Wang , Harold B. Wood , Cheng Zhu , Yuping Zhu , Zhiqiang Guo
IPC分类号: C07D513/04 , C07D239/42 , C07D405/12 , C07D409/12 , C07D498/04 , C07D487/04 , C07D403/14 , C07D401/14 , C07D403/12 , C07D471/04
CPC分类号: C07D513/04 , C07D239/42 , C07D401/04 , C07D401/14 , C07D403/12 , C07D403/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , C07D498/04
摘要: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included
摘要翻译: 披露式(I)的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法
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