公开(公告)号：US20190016734A1

公开(公告)日：2019-01-17

申请号：US16076813

申请日：2017-02-06

申请人： Wen-Lian WU ,  Jared N. MING ,  Brandon M. TAOKA ,  Xing DAI ,  Merck Sharp & Dohme Corp.

发明人： Wen-Lian Wu ,  Jared N. Cumming ,  Brandon M. Taoka ,  Xing Dai

IPC分类号： C07D513/02 ,  A61P25/28

摘要： In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, 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.

公开(公告)号：US10689401B2

公开(公告)日：2020-06-23

申请号：US16076813

申请日：2017-02-06

申请人： Merck Sharp & Dohme Corp. ,  Wen-Lian Wu ,  Jared N. Cumming ,  Brandon M. Taoka ,  Xing Dai

发明人： Wen-Lian Wu ,  Jared N. Cumming ,  Brandon M. Taoka ,  Xing Dai

IPC分类号： C07D513/02 ,  C07D513/04 ,  C07D513/10 ,  A61P25/28

摘要： In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, 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.

公开(公告)号：US20190218223A1

公开(公告)日：2019-07-18

申请号：US16324596

申请日：2017-08-10

申请人： Jared N. CUMMING ,  Kevin D. DYKSTRA ,  Alan HRUZA ,  Derun LI ,  Hong LIU ,  Haiqun TANG ,  Brandon M. TAOKA ,  Andreas VERRAS ,  Shawn P. WALSH ,  Wen-Lian WU ,  Merck Sharp & Dohme Corp.

发明人： Jared N. Cumming ,  Kevin D. Dykstra ,  Alan Hruza ,  Derun Li ,  Hong Liu ,  Haiqun Tang ,  Brandon M. Taoka ,  Andreas Verras ,  Shawn P. Walsh ,  Wen-Lian Wu

IPC分类号： C07D487/04 ,  C07D519/00 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  A61P3/10

CPC分类号： C07D487/04 ,  A61P3/10 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.

公开(公告)号：US10414774B2

公开(公告)日：2019-09-17

申请号：US16324596

申请日：2017-08-10

申请人： Merck Sharp & Dohme Corp. ,  Jared N. Cumming ,  Kevin D. Dykstra ,  Alan Hruza ,  Derun Li ,  Hong Liu ,  Haiqun Tang ,  Brandon M. Taoka ,  Andreas Verras ,  Shawn P. Walsh ,  Wen-Lian Wu

发明人： Jared N. Cumming ,  Kevin D. Dykstra ,  Alan Hruza ,  Derun Li ,  Hong Liu ,  Haiqun Tang ,  Brandon M. Taoka ,  Andreas Verras ,  Shawn P. Walsh ,  Wen-Lian Wu

IPC分类号： C07D487/04 ,  C07D519/00 ,  A61P3/10 ,  C07D498/04 ,  C07D513/04 ,  C07D471/04

摘要： Described herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. The compounds of Formula I act as Cyp8b1 inhibitors and can be useful in preventing, treating or acting as a remedial agent for diabetes and cardiovascular disease.

公开(公告)号：US11466047B2

公开(公告)日：2022-10-11

申请号：US16611624

申请日：2018-05-07

申请人： Merck Sharp & Dohme Corp. ,  Wen-Lian Wu ,  Jongwon Lim ,  Jared N. Cumming ,  Benjamin Wesley Trotter ,  Wonsuk Chang

发明人： Wen-Lian Wu ,  Jongwon Lim ,  Jared N. Cumming ,  Benjamin Wesley Trotter ,  Wonsuk Chang

IPC分类号： C07H21/00 ,  C07H21/04 ,  A61P35/00 ,  A61P37/02 ,  C07H21/02

摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Ya, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US20210206796A1

公开(公告)日：2021-07-08

申请号：US16771814

申请日：2018-12-17

申请人： Brian M. ANDRESEN ,  Frank BENNETT ,  Wonsuk CHANG ,  Matthew Lloyd CHILDERS ,  Jared N. CUMMING ,  Jongwon LIM ,  Min LU ,  Benjamin Wesley TROTTER ,  Wen-Lian WU ,  Merck Sharp & Dohme Corp.

发明人： Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

IPC分类号： C07H21/00 ,  A61P37/04

摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US11685761B2

公开(公告)日：2023-06-27

申请号：US16771814

申请日：2018-12-17

申请人： Merck Sharp & Dohme Corp. ,  Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

发明人： Brian M. Andresen ,  Frank Bennett ,  Wonsuk Chang ,  Matthew Lloyd Childers ,  Jared N. Cumming ,  Jongwon Lim ,  Min Lu ,  Benjamin Wesley Trotter ,  Wen-Lian Wu

IPC分类号： C07H21/00 ,  A61P37/04 ,  C07H21/02 ,  A61K31/7084 ,  C07H21/04

CPC分类号： C07H21/00 ,  A61K31/7084 ,  A61P37/04 ,  C07H21/02 ,  C07H21/04 ,  C07B2200/07

摘要： A class of polycyclic compounds of general formula (I), wherein Base1, Base2, Y, Za, Xa, Xa1, Xb, Xb1, Xc, Xc1, Xd, Xd1, R1, R1a, R2, R2a, R3, R4, R4a, R5, R6, R6a, R7, R7a, R8, R8a, and R9 are defined herein, that may be useful as inductors of type I interferon production, specifically as STING active agents, are provided. Also provided are processes for the synthesis and use of compounds.

公开(公告)号：US20160222032A1

公开(公告)日：2016-08-04

申请号：US15021011

申请日：2014-09-08

申请人： Jack D. SCOTT ,  Wen-Lian WU ,  Jared N. CUMMING ,  MERCK SHARP & DOHME CORP.

发明人： Jack D. Scott ,  Wen-Lian Wu ,  Jared N. Cumming

IPC分类号： C07D513/10 ,  A61K45/06 ,  C07D417/12 ,  A61K31/547 ,  C07D519/00

CPC分类号： C07D513/10 ,  A61K31/547 ,  A61K45/06 ,  C07D279/16 ,  C07D417/12 ,  C07D471/04 ,  C07D519/00 ,  A61K2300/00

摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): or a tautomers and/or stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoisomers, wherein RL, X, Y, R1A, R1B, R2, R3, m, and RA 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.

摘要翻译： 在其许多实施方案中，本发明提供某些C5-螺亚氨基二氮嗪二氧化物化合物，包括式（I）化合物：或其互变异构体和/或立体异构体，以及所述化合物，所述互变异构体和所述立体异构体的药学上可接受的盐，其中RL， X，Y，R 1A，R 1B，R 2，R 3，m和RA如本文所定义。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

公开(公告)号：US20160016975A1

公开(公告)日：2016-01-21

申请号：US14774204

申请日：2014-03-11

申请人： Eric J. GILBERT ,  Jared N. CUMMING ,  Jack D. SCOTT ,  Wen-Lian WU ,  Duane A. BURNETT ,  Andrew W. STAMFORD ,  MERCK SHARP & DOHME CORP.

发明人： Eric J. Gilbert ,  Jared N. Cumming ,  Jack D. Scott ,  Wen-Lian Wu ,  Duane A. Burnett ,  Andrew W. Stamford

IPC分类号： C07D513/10

CPC分类号： C07D513/10

摘要： In its many embodiments, the present invention provides certain C2-azaspiro substituted iminothiazine dioxide compounds. 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.

摘要翻译： 在其许多实施方案中，本发明提供某些C2-氮杂螺环取代的亚氨基噻嗪二氧化物化合物。 本发明的新化合物可用作BACE抑制剂和/或用于治疗和预防与其相关的各种病症。 还公开了包含一种或多种这样的化合物（单独和与一种或多种其它活性剂组合）的药物组合物及其制备和使用方法，包括用于治疗阿尔茨海默氏病的药物组合物。

公开(公告)号：US10071998B2

公开(公告)日：2018-09-11

申请号：US15543608

申请日：2016-01-15

申请人： Merck Sharp & Dohme Corp.

发明人： Wen-Lian Wu ,  Shuwen He ,  Shawn P. Walsh ,  Jared N. Cumming

IPC分类号： C07D417/14 ,  C07D417/12

CPC分类号： C07D417/14 ,  A61P3/10 ,  A61P9/04 ,  A61P25/16 ,  A61P25/28 ,  A61P27/06 ,  C07D417/12

摘要： In its many embodiments, the present invention provides certain iminothiazine dioxide compounds, including compounds Formula (I): or a tautomers thereof, and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, ring A, RA, m, ring B, RB, and n 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.