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公开(公告)号：US10093683B2
公开(公告)日：2018-10-09
申请号：US15305421
申请日：2015-04-21
发明人： Yeon-Hee Lim , Zhuyan Guo , Amjad Ali , Scott D. Edmondson , Weiguo Liu , Gioconda V. Gallo-Etienne , Heping Wu , Ying-Duo Gao , Andrew W. Stamford , Younong Yu , Nancy J. Kevin , Rajan Anand , Deyou Sha , Santhosh F. Neelamkavil , Zahid Hussain , Puneet Kumar , Remond Moningka , Joseph L. Duffy , Jiayi Xu , Yu Jiang , Anjan Chakrabarti , Hiroki Sone
IPC分类号： C07D498/20 , C07F9/6561 , C07D487/10 , C07D498/10 , C07D471/10
摘要： The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more compounds of Formula (I), and methods for using the compounds of Formula (I) for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.
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公开(公告)号：US09868738B2
公开(公告)日：2018-01-16
申请号：US15512081
申请日：2015-09-14
发明人： Kun Liu , Shuwen He , Jared N. Cumming , Andrew W. Stamford
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , A61K45/06 , A61P25/00
摘要： In its many embodiments, the present invention provides certain C-6 spirocarbocyclic iminothiadiazine compounds, including compounds Formula (I) or a tautomer thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1A, R1B, R2, RA, ring A, RA, m, L1, RL, ring C, RC, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
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公开(公告)号：US20170240539A1
公开(公告)日：2017-08-24
申请号：US15518804
申请日：2015-10-09
发明人： Andrew W. Stamford , Zhi-Qiang Yang , Milana Maletic , Senlin Cai , Xiaobang Duan , Jianhua Cao
IPC分类号： C07D417/06 , C07D417/14
CPC分类号： C07D417/06 , C07D417/14
摘要： The present invention relates to cyclic sulfonamide derivatives of Formula (I) or a pharmaceutically acceptable salt thereof.
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公开(公告)号：US20170233382A1
公开(公告)日：2017-08-17
申请号：US15503035
申请日：2015-08-10
申请人： Steven P. MILLER , Carmela MOLINARO , David THAISRIVONGS , Feng XU , Richard DESMOND , Hongming LI , Qinghao CHEN , Andrew STAMFORD , Zhiguo Jake SONG , Lushi TAN , Merck Sharp & Dohme Corp.
发明人： Steven P. Miller , Carmela Molinaro , David Thaisrivongs , Feng Xu , Richard Desmond , Hongming Li , Qinghao Chen , Andrew W. Stamford , Zhiguo Jake Song , Lushi Tan
IPC分类号： C07D417/12 , C07C313/06 , C07C311/33 , C07D213/81
CPC分类号： C07D417/12 , C07C303/40 , C07C311/33 , C07C311/35 , C07C313/06 , C07D213/81
摘要： This invention provides processes for the preparation of verubecestat (Compound of Formula (I)), a potent inhibitor of BACE-1 and BACE-2. In addition, the invention provides certain synthetic intermediates which are useful, among other things, for the preparation of the Compound of Formula (I).
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5.发明授权Iminothiadiazine dioxide compounds as BACE inhibitors, compositions, and their use 有权作为BACE抑制剂，组合物及其用途的二氢化二氮杂二恶烷化合物公开(公告)号：US09428475B2
公开(公告)日：2016-08-30
申请号：US14221650
申请日：2014-03-21
IPC分类号： A61K31/549 , C07D285/18 , A61K31/00 , A61K31/54 , A61K45/06 , C07D403/12 , C07D401/14 , C07D401/12 , C07D403/04 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D213/89 , C07D417/10 , C07C309/30 , C07D487/04 , C07D213/26 , A61K31/495 , C07D239/14
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): (I) and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, L2-, and L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (Aβ) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination nation with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimers disease, are also disclosed.
摘要翻译： 在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）：（I）的化合物并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5 ，R9，环A，环B，m，n，p，-L1-，L2-和L3-是独立选择和如本文所定义的。 令人惊奇地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与β-淀粉样蛋白（Aβ）生产相关的各种病症的优点的性质。 还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物及其制备和用于治疗与淀粉样蛋白β（Aβ）蛋白（包括阿尔茨海默病）相关的病理学的方法。
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6.发明授权Iminothiadiazine dioxide compounds as brace inhibitors, compositions, and their use 有权作为支架抑制剂，组合物及其用途的二氢化二氮杂二恶烷化合物公开(公告)号：US09029362B2
公开(公告)日：2015-05-12
申请号：US14221640
申请日：2014-03-21
IPC分类号： A61K31/54 , C07C309/30 , A61K31/00 , A61K45/06 , C07D403/12 , C07D401/14 , C07D401/12 , C07D403/04 , C07D417/04 , C07D417/12 , C07D417/14 , C07D471/04 , C07D495/04 , C07D285/18 , C07D213/89 , C07D417/10 , A61K31/549 , C07D213/26 , A61K31/495 , C07D239/14
CPC分类号： A61K31/549 , A61K31/00 , A61K31/495 , A61K31/54 , A61K45/06 , C07C309/30 , C07D213/26 , C07D213/89 , C07D239/14 , C07D285/18 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/12 , C07D417/04 , C07D417/10 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04 , A61K2300/00
摘要： In its many embodiments, the present invention provides certain iminothiadiazine dioxide compounds, including compounds Formula (I): and include stereoisomers thereof, and pharmaceutically acceptable salts of said compounds stereoisomers, wherein each of R1, R2, R3, R4, R5, R9, ring A, ring B, m, n, p, -L1-, -L2-, and -L3- is selected independently and as defined herein. The novel iminothiadiazine dioxide compounds of the invention have surprisingly been found to exhibit properties which are expected to render them advantageous as BACE inhibitors and/or for the treatment and prevention of various pathologies related to β-amyloid (“Aβ”) production. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use in treating pathologies associated with amyloid beta (Aβ) protein, including Alzheimer's disease, are also disclosed.
摘要翻译： 在其许多实施方案中，本发明提供了某些亚氨基二嗪二氧化物化合物，包括式（I）化合物：并包括其立体异构体，以及所述化合物立体异构体的药学上可接受的盐，其中R1，R2，R3，R4，R5，R9， 环A，环B，m，n，p，-L 1 - ， - 2 - 和-L 3 - 独立地如本文所定义。 令人惊讶地发现本发明的新型亚氨基二嗪二氧化物化合物表现出预期使其作为BACE抑制剂和/或用于治疗和预防与“淀粉样蛋白”（“A”）生产有关的各种病理学的优点的性质。 还公开了包含一种或多种这样的化合物（单独并与一种或多种其它活性剂组合）的药物组合物，及其制备和用于治疗与淀粉样蛋白β（Aβ）蛋白（包括阿尔茨海默氏病）相关的病理学的方法。
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公开(公告)号：US20150105354A1
公开(公告)日：2015-04-16
申请号：US14575418
申请日：2014-12-18
发明人： Zhaoning Zhu , Brian McKittrick , Zhong-Yue Sun , Yuanzan C. Ye , Johannes H. Voigt , Corey Strickland , Elizabeth M. Smith , Andrew W. Stamford , William J. Greenlee , Robert D. Mazzola, JR. , John Caldwell , Jared N. Cumming , Lingyan Wang , Yusheng Wu , Ulrich Iserloh , Tao Guo , Thuy X.H. Le , Kurt W. Saionz , Suresh D. Babu , Rachael C. Hunter
IPC分类号： C07D233/88 , C07D401/04 , A61K31/4439 , C07D405/06 , A61K31/4178 , C07D401/06 , A61K31/454 , C07D407/06 , C07D403/06 , A61K31/5377 , C07D235/02 , A61K31/4184 , A61K31/655 , C07D405/14 , C07D401/14 , A61K31/4545 , A61K31/4725 , A61K45/06 , A61K31/4168
CPC分类号： C07D233/88 , A61K31/4168 , A61K31/4178 , A61K31/4184 , A61K31/4439 , A61K31/454 , A61K31/4545 , A61K31/4725 , A61K31/5377 , A61K31/655 , A61K45/06 , C07D233/46 , C07D233/70 , C07D235/02 , C07D239/22 , C07D239/70 , C07D271/07 , C07D273/00 , C07D295/15 , C07D401/04 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/10 , C07D403/12 , C07D405/06 , C07D405/10 , C07D405/14 , C07D407/06 , C07D409/04 , C07D409/06 , C07D409/10 , C07D409/14 , C07D413/10 , C07D413/12 , C07D417/06 , Y02A50/411
摘要： Disclosed are compounds of the formula I or a stereoisomer, tautomer, or pharmaceutically acceptable salt or solvate thereof, wherein W is a bond, —C(═S)—, —S(O)—, —S(O)2—, —C(═O)—, —O—, —C(R6)(R7)—, —N(R5)— or —C(═N(R5))—; X is —O—, —N(R5)— or —C(R6)(R7)—; provided that when X is —O—, U is not —O—, —S(O)—, —S(O)2—, —C(═O)— or —C(═NR5)—; U is a bond, —S(O)—, —S(O)2—, —C(O)—, —O—, —P(O)(OR15)—, —C(═NR5)—, —(C(R6)(R7))b— or —N(R5)—; wherein b is 1 or 2; provided that when W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, U is not —S(O)—, —S(O)2—, —O—, or —N(R5)—; provided that when X is —N(R5)— and W is —S(O)—, —S(O)2—, —O—, or —N(R5)—, then U is not a bond; and R1, R2, R3, R4, R5, R6, and R7 are as defined in the specification; and pharmaceutical compositions comprising the compounds of formula I. Also disclosed is the method of inhibiting aspartyl protease, and in particular, the methods of treating cardiovascular diseases, cognitive and neurodegenerative diseases, and the methods of inhibiting of Human Immunodeficiency Virus, plasmepins, cathepsin D and protozoal enzymes.Also disclosed are methods of treating cognitive or neurodegenerative diseases using the compounds of formula I in combination with a cholinesterase inhibitor or a muscarinic antagonist.
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公开(公告)号：US10822338B2
公开(公告)日：2020-11-03
申请号：US15738178
申请日：2016-07-05
发明人： Amjad Ali , Xianhai Huang , Yeon-Hee Lim , Rongze Kuang , Heping Wu , Rajan Anand , Younong Yu , Edward Metzger , Michael Man-Chu Lo , Pauline C. Ting , Andrew W. Stamford , Paul Tempest
IPC分类号： C07D487/04 , C07D491/153
摘要： The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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公开(公告)号：US20180362530A1
公开(公告)日：2018-12-20
申请号：US15738178
申请日：2016-07-05
发明人： Amjad Ali , Xianhai Huang , Yeon-Hee Lim , Rongze Kuang , Heping Wu , Rajan Anand , Younong Yu , Edward Metzger , Michael Man-Chu LO , Pauline C. Ting , Andrew W. Stamford , Paul Tempest
IPC分类号： C07D487/04 , C07D491/153
摘要： The present invention is directed to compounds of generic formula (I): or pharmaceutically acceptable salts thereof that are believed to be useful as an A2A-receptor antagonist. The invention is further directed to methods of treating a patient (preferably a human) for diseases or disorders in which the A2A-receptor is involved. The invention further involves use of the compounds as an A2A-receptor antagonist and/or inhibitor for the preparation of a medicament for the treatment and/or prevention of diseases associated with inhibiting the receptor, which includes central nervous system disorders such as Parkinson's disease. The invention is also directed to pharmaceutical compositions which include an effective amount of a compound of formula (I), or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, and the use of the compounds and pharmaceutical compositions of the invention in the treatment of such diseases.
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公开(公告)号：US20180230152A1
公开(公告)日：2018-08-16
申请号：US15507577
申请日：2015-08-28
发明人： Xing Dai , Kallol Basu , Duane DeMong , Sarah W. Li , Michael Miller , Jack D. Scott , Andrew W. Stamford
IPC分类号： C07D487/04 , C07D413/14 , C07D403/14 , C07D401/14 , A61P25/16
CPC分类号： C07D487/04 , A61P25/16 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D413/14
摘要： The present invention is directed to substituted certain reversed indazole compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R9, and A 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. 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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