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.

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.

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.

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.

发明人： Michael T. Rudd ,  David Jonathan Bennett ,  Jenny Wai ,  Zhaoyang Meng

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.

公开(公告)号：US10752587B2

公开(公告)日：2020-08-25

申请号：US15780289

申请日：2016-11-29

申请人： Merck Sharp & Dohme Corp.

发明人： Michael T. Rudd ,  David Jonathan Bennett ,  Jenny Wai ,  Zhaoyang Meng

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.

公开(公告)号：US20180305332A1

公开(公告)日：2018-10-25

申请号：US15774655

申请日：2016-11-07

申请人： Merck Sharp & Dohme Corp.

发明人： Shawn J. Stachel ,  David Jonathan Bennett ,  Edward J. Brnardic ,  Nigel J. Liverton ,  Peter J. Manley ,  Zhaoyang Meng ,  Kausik K. Nanda ,  Michael T. Rudd ,  Jenny Wai

IPC分类号： C07D401/04 ,  C07D401/14 ,  C07D413/14 ,  C07D471/10 ,  C07D417/14 ,  C07D405/14

CPC分类号： C07D401/04 ,  A61K31/451 ,  C07D211/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/10

摘要： In its many embodiments, the present invention provides certain substituted bispiperidinyl compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, 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.

公开(公告)号：US10961215B2

公开(公告)日：2021-03-30

申请号：US16341602

申请日：2017-10-09

申请人： 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

IPC分类号： C07D401/04 ,  C07D211/26 ,  C07D405/14

摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be 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.

公开(公告)号：US20200039951A1

公开(公告)日：2020-02-06

申请号：US16341602

申请日：2017-10-09

申请人： 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

IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D211/26

摘要： In its many embodiments, the present invention provides certain substituted N-aryl and N-heteroaryl piperidine compounds of the Formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, L, R4, L1, Q, R5 and R6 are as defined herein. The novel compounds of the invention, and pharmaceutically acceptable compositions comprising a compound thereof, may be 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.

公开(公告)号：US20060173023A1

公开(公告)日：2006-08-03

申请号：US11334931

申请日：2006-01-19

申请人： Michael Wood ,  Dai-Shi Su ,  Jenny Wai

发明人： Michael Wood ,  Dai-Shi Su ,  Jenny Wai

IPC分类号： A61K31/506 ,  A61K31/454 ,  A61K31/42 ,  A61K31/401

CPC分类号： A61K31/401 ,  A61K31/42 ,  A61K31/454 ,  A61K31/506 ,  C07C237/22 ,  C07D205/04 ,  C07D207/22 ,  C07D209/20 ,  C07D211/60 ,  C07D239/28 ,  C07D261/18 ,  C07D413/06

摘要： Compounds disclosed herein are bradykinin B1 antagonist compounds useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

公开(公告)号：US20050085667A1

公开(公告)日：2005-04-21

申请号：US10503502

申请日：2003-02-04

申请人： Michael Wood ,  Neville Anthony ,  Mark Bock ,  Dong-Mei Feng ,  Scott Kuduk ,  Dai-Shi Su ,  Jenny Wai

发明人： Michael Wood ,  Neville Anthony ,  Mark Bock ,  Dong-Mei Feng ,  Scott Kuduk ,  Dai-Shi Su ,  Jenny Wai

IPC分类号： C07D249/08 ,  A61K31/235 ,  A61K31/341 ,  A61K31/343 ,  A61K31/352 ,  A61K31/36 ,  A61K31/381 ,  A61K31/4035 ,  A61K31/41 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4196 ,  A61K31/42 ,  A61K31/421 ,  A61K31/4245 ,  A61K31/426 ,  A61K31/44 ,  A61K31/4406 ,  A61K31/498 ,  A61K31/50 ,  A61K31/505 ,  A61P1/02 ,  A61P19/02 ,  A61P29/00 ,  A61P29/02 ,  A61P43/00 ,  C07C233/50 ,  C07C237/24 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D213/89 ,  C07D231/12 ,  C07D231/14 ,  C07D233/64 ,  C07D233/90 ,  C07D237/24 ,  C07D239/28 ,  C07D241/44 ,  C07D257/04 ,  C07D261/18 ,  C07D263/34 ,  C07D271/06 ,  C07D271/08 ,  C07D277/20 ,  C07D277/56 ,  C07D307/33 ,  C07D307/56 ,  C07D307/68 ,  C07D309/30 ,  C07D317/68 ,  C07D333/24 ,  C07D333/40 ,  C07D333/70 ,  C07D403/12 ,  C07D413/12

CPC分类号： C07C237/24 ,  C07C237/22 ,  C07C2601/02 ,  C07D209/48 ,  C07D213/81 ,  C07D213/82 ,  C07D231/12 ,  C07D237/24 ,  C07D239/28 ,  C07D241/44 ,  C07D249/08 ,  C07D249/10 ,  C07D257/04 ,  C07D261/18 ,  C07D263/34 ,  C07D271/06 ,  C07D307/68 ,  C07D317/68 ,  C07D333/38 ,  C07D333/70 ,  C07D403/12 ,  C07D413/12

摘要： N-Biphenyl(substituted methyl) aminocycloalkanecarboxamide derivatives are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.

摘要翻译： N-联苯（取代的甲基）氨基环烷基甲酰胺衍生物是缓激肽B1拮抗剂或反向激动剂，其可用于治疗或预防与缓激肽B1途径相关的疼痛和炎症等症状。