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公开(公告)号：US10894775B2
公开(公告)日：2021-01-19
申请号：US16341591
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu , Chuanman Huang
IPC分类号： C07D221/20 , C07D211/16 , C07D211/96
摘要： In its many embodiments, the present invention provides certain piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, Y, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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2.发明申请公开(公告)号：US20200247754A1
公开(公告)日：2020-08-06
申请号：US16341595
申请日：2017-10-09
申请人： Michael T. RUDD , Zhaoyang MENG , Jenny WAI , David Jonathan BENNETT , Edward J. BRNARDIC , Nigel J. LIVERTON , Shawn J. STACHEL , Yongxin HAN , Paul TEMPEST , Jiuxiang ZHU , Xuewang XU , Bin ZHU , Merck Sharp & Dohme Corp.
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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3.发明授权公开(公告)号：US11655216B2
公开(公告)日：2023-05-23
申请号：US16341595
申请日：2017-10-09
申请人： Merck Sharp & Dohme Corp. , Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
发明人： Michael T. Rudd , Zhaoyang Meng , Jenny Wai , David Jonathan Bennett , Edward J. Brnardic , Nigel J. Liverton , Shawn J. Stachel , Yongxin Han , Paul Tempest , Jiuxiang Zhu , Xuewang Xu , Bin Zhu
IPC分类号： C07D221/20 , C07D401/12 , C07D417/12 , C07D405/12 , C07D211/22 , C07D401/14 , C07D417/14
CPC分类号： C07D221/20 , C07D211/22 , C07D401/12 , C07D401/14 , C07D405/12 , C07D417/12 , C07D417/14
摘要： In its many embodiments, the present invention provides certain substituted aryl and heteroaryl ether compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3, L, R4, L1, Q, and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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4.发明申请公开(公告)号：US20180354901A1
公开(公告)日：2018-12-13
申请号：US15780289
申请日：2016-11-29
申请人： Michael T. Rudd , David Jonathan Bennett , Jenny Wai , Zhaoyang Meng , Merck Sharp & Dohme Corp.
IPC分类号： C07D211/16 , C07D401/14 , C07D211/44 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D417/14 , C07D451/02
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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5.发明授权公开(公告)号：US11149036B2
公开(公告)日：2021-10-19
申请号：US16621959
申请日：2018-06-22
申请人： John J. Acton, III , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd. , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/048 , C07D498/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US20160159744A1
公开(公告)日：2016-06-09
申请号：US15047213
申请日：2016-02-18
发明人： Christopher James Bungard , Antonella Converso , Pablo De Leon , Barbara Hanney , Timothy John Hartingh , Jesse Josef Manikowski , Peter J. Manley , Robert Meissner , Zhaoyang Meng , James J. Perkins , Michael T. Rudd , Youheng Shu
IPC分类号： C07D215/48 , C07D409/04 , C07D401/06 , C07D417/14 , C07D417/06 , C07D401/14 , C07D471/04 , C07D401/04 , C07D413/06
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), 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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7.发明申请公开(公告)号：US20190000824A1
公开(公告)日：2019-01-03
申请号：US16062500
申请日：2016-12-19
发明人： John J. Acton, III , Jianming Bao , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Jenny Miu-Chun Wai
IPC分类号： A61K31/4439 , A61K31/437 , A61P25/16 , A61P25/18 , A61P25/28
CPC分类号： A61K31/4439 , A61K31/437 , A61P25/16 , A61P25/18 , A61P25/28 , C07D401/14 , C07D405/14 , C07D471/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine 5 receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US09636337B2
公开(公告)日：2017-05-02
申请号：US15047224
申请日：2016-02-18
发明人： Christopher James Bungard , Antonella Converso , Pablo De Leon , Barbara Hanney , Timothy John Hartingh , Jesse Josef Manikowski , Peter J. Manley , Robert Meissner , Zhaoyang Meng , James J. Perkins , Michael T. Rudd , Youheng Shu
IPC分类号： A61K31/47 , A61K31/506 , A61K31/4985 , A61K31/496 , A61K31/4709 , A61K31/541 , A61K31/5377 , C07D401/14 , C07D413/14 , C07D215/48 , C07D401/04 , C07D401/06 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
CPC分类号： C07D413/14 , A61K31/47 , A61K31/4709 , A61K31/496 , A61K31/4985 , A61K31/506 , A61K31/5377 , A61K31/541 , C07D215/48 , C07D401/04 , C07D401/06 , C07D401/14 , C07D409/04 , C07D413/06 , C07D417/06 , C07D417/14 , C07D471/04 , C07D491/10
摘要： The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) wherein ring A, RQ, -L-, R1, n, R2, and R3 are as defined herein. The compounds of the invention are useful as non-competitive mGluR2 antagonists, or mGluR2 negative allosteric modulators (NAMs), and in methods of treating a patient (preferably a human) for diseases or disorders in which the mGluR2-NAM receptor is involved, including potentially Alzheimer's disease, cognitive impairment, schizophrenia and other mood disorders, pain disorders and sleep disorders, by administering to the patient a therapeutically effective amount of a compound of the invention, or a pharmaceutically acceptable salt thereof. The invention is also directed to pharmaceutical compositions comprising a compound of the invention, or a pharmaceutically acceptable salt thereof, (optionally in combination with one or more additional active ingredients), 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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9.发明授权公开(公告)号：US10933056B2
公开(公告)日：2021-03-02
申请号：US16674546
申请日：2019-11-05
发明人： John J. Acton, III , Jianming Bao , Melissa Egbertson , Xiaolei Gao , Scott T. Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Michael T. Rudd , Oleg B. Selyutin , David M. Tellers , Ling Tong , Jenny Miu-Chun Wai
IPC分类号： C07D401/14 , C07D405/14 , C07D471/04 , A61K31/4439 , A61P25/28 , A61P25/18 , A61P25/16 , A61K31/437
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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10.发明授权公开(公告)号：US10752587B2
公开(公告)日：2020-08-25
申请号：US15780289
申请日：2016-11-29
IPC分类号： C07D211/16 , C07D401/14 , C07D409/14 , C07D401/06 , C07D487/08 , C07D413/14 , C07D451/02 , C07D417/14 , C07D211/46 , C07D211/10 , C07D211/54 , C07D211/44
摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein ring A, ring B, R1, R2, R3, L, R4, X, Z, Li, Q and R5 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, are useful as Liver X-β receptor (LXRβ) agonists, and may be useful for treating or preventing pathologies related thereto. Such pathologies include, but are not limited to, inflammatory diseases and diseases characterized by defects in cholesterol and lipid metabolism, such as Alzheimer's disease.
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