公开(公告)号：US09051329B2

公开(公告)日：2015-06-09

申请号：US14125116

申请日：2012-07-02

申请人： Wen-Lian Wu

发明人： Wen-Lian Wu

IPC分类号： A61K31/505 ,  C07D491/00 ,  C07D487/14 ,  A61K31/519 ,  A61K31/529

CPC分类号： C07D487/14 ,  A61K31/519 ,  A61K31/529

摘要： The present invention is directed to novel tricyclic heterocycles of structural formula (I) which are inhibitors of the dipeptidyl peptidase-IV enzyme and which are useful in the treatment or prevention of diseases in which the dipeptidyl peptidase-IV enzyme is involved, such as diabetes and particularly Type 2 diabetes. 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 the dipeptidyl peptidase-IV enzyme is involved.

摘要翻译： 本发明涉及结构式（I）的新型三环杂环，其为二肽基肽酶-IV酶的抑制剂，其可用于治疗或预防涉及二肽基肽酶-IV酶的疾病，例如糖尿病 特别是2型糖尿病。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及二肽基肽酶-IV酶的疾病中的用途。

公开(公告)号：US20070072863A1

公开(公告)日：2007-03-29

申请号：US11504860

申请日：2006-08-16

申请人： Chad Bennett ,  Wen-Lian Wu ,  Duane Burnett

发明人： Chad Bennett ,  Wen-Lian Wu ,  Duane Burnett

IPC分类号： A61K31/519 ,  A61K31/503 ,  A61K31/4745 ,  C07D487/14 ,  C07D471/14

CPC分类号： C07D495/14 ,  C07D471/14 ,  C07D487/14

摘要： In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J1-J3, X, Z, and R1-R4 are as defined herein) useful as metabotropic glutamate receptor (mGluR) antagonists, particularly as selective metabotropic glutamate receptor 1 antagonists, pharmaceutical compositions containing the compounds, and methods of treatment using the compounds and compositions to treat diseases associated with metabotropic glutamate receptor (e.g., mGluR1) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

摘要翻译： 在其许多实施方案中，本发明提供式I的三环化合物（其中J 1，X 3，X，Z和R 1） 可用作代谢型谷氨酸受体（mGluR）拮抗剂，特别是作为选择性代谢型谷氨酸受体1拮抗剂的药物组合物，以及使用该化合物和组合物的治疗方法 治疗与代谢型谷氨酸受体（例如，mGluR1）相关的疾病，例如疼痛，偏头痛，焦虑症，尿失禁和神经变性疾病如阿尔茨海默氏病。

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：US20050137210A1

公开(公告)日：2005-06-23

申请号：US11018990

申请日：2004-12-21

申请人： Duane Burnett ,  Wen-Lian Wu ,  Martin Domalski ,  Mary Caplen ,  Richard Spring ,  Jean Lachowicz

发明人： Duane Burnett ,  Wen-Lian Wu ,  Martin Domalski ,  Mary Caplen ,  Richard Spring ,  Jean Lachowicz

IPC分类号： A61K31/277 ,  A61K31/405 ,  A61K31/44 ,  A61K31/445 ,  A61K31/495 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D211/28 ,  C07D295/155 ,  C07D295/205

CPC分类号： C07D295/205 ,  A61K45/06 ,  C07C255/57 ,  C07C257/14 ,  C07C257/18 ,  C07D209/08 ,  C07D209/86 ,  C07D211/14 ,  C07D213/53 ,  C07D215/26 ,  C07D215/48 ,  C07D233/64 ,  C07D295/073 ,  C07D295/112 ,  C07D295/155 ,  C07D317/58 ,  C07D319/18 ,  C07D333/20 ,  C07D405/12

摘要： The present invention provides compounds, which, are novel antagonists for D1 receptors as well as methods for preparing such compounds. In another embodiment, the invention provides pharmaceutical compositions comprising such D1 receptor antagonists as well as methods of using them to treat CNS disorders, obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

摘要翻译： 本发明提供了作为D 1受体的新型拮抗剂的化合物以及制备这些化合物的方法。 在另一个实施方案中，本发明提供包含这种D 1受体拮抗剂的药物组合物以及使用它们治疗CNS障碍，肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

公开(公告)号：US20050054628A1

公开(公告)日：2005-03-10

申请号：US10926557

申请日：2004-08-26

申请人： Duane Burnett ,  Wen-Lian Wu ,  Thavalakulamgara Sasikumar ,  William Greenlee ,  Mary Caplen ,  Tao Guo ,  Rachael Hunter

发明人： Duane Burnett ,  Wen-Lian Wu ,  Thavalakulamgara Sasikumar ,  William Greenlee ,  Mary Caplen ,  Tao Guo ,  Rachael Hunter

IPC分类号： A61P3/04 ,  A61P3/10 ,  C07D401/06 ,  C07D401/12 ,  A61K31/46

CPC分类号： C04B35/632 ,  C07D401/06 ,  C07D401/12

摘要： The present invention discloses compounds of formula I wherein Ar, Y, m, n, R1 and R4 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

摘要翻译： 本发明公开了其中Ar，Y，m，n，R 1和R 4在本文中定义的式I化合物，所述化合物是黑色素浓缩激素（MCH）的新型拮抗剂，以及制备方法 这样的化合物。 在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

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：US20050049269A1

公开(公告)日：2005-03-03

申请号：US10924070

申请日：2004-08-23

申请人： Wen-Lian Wu ,  Duane Burnett ,  Mary Ann Caplen

发明人： Wen-Lian Wu ,  Duane Burnett ,  Mary Ann Caplen

IPC分类号： A61P3/04 ,  A61P3/06 ,  A61P3/10 ,  C07D401/06 ,  C07D401/14 ,  C07D417/14 ,  A61K31/4747 ,  A61K31/454 ,  C07D43/02

CPC分类号： C07D401/06 ,  C07D401/14 ,  C07D417/14

摘要： The present invention discloses compounds of formula I wherein Ar, X, R1 and R11 are herein defined, said compounds being novel antagonists for melanin-concentrating hormone (MCH), as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such MCH antagonists as well as methods of using them to treat obesity, metabolic disorders, eating disorders such as hyperphagia, and diabetes.

摘要翻译： 本发明公开了其中Ar，X，R 1和R 11在本文中定义的式I化合物，所述化合物是用于黑色素浓缩激素（MCH）的新型拮抗剂，以及制备此类化合物的方法。 在另一个实施方案中，本发明公开了包含这样的MCH拮抗剂的药物组合物以及使用它们治疗肥胖，代谢紊乱，进食障碍如食欲过盛和糖尿病的方法。

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：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：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.