公开(公告)号：WO2012118945A3

公开(公告)日：2014-04-10

申请号：PCT/US2012027237

申请日：2012-03-01

Applicant: MERCK SHARP & DOHME ,  BENNETT CHAD E ,  BURNETT DUANE A ,  LI HONGMEI ,  CHEN YONGGANG ,  MCCRACKEN TROY ,  VICAREL MONICA

Inventor： BENNETT CHAD E ,  BURNETT DUANE A ,  LI HONGMEI ,  CHEN YONGGANG ,  MCCRACKEN TROY ,  VICAREL MONICA

IPC: A01N43/54 ,  C07D239/42 ,  C07D471/22

CPC classification number: C07D487/04 ,  A61K31/155 ,  A61K31/427 ,  A61K31/519 ,  A61K31/522 ,  A61K31/64 ,  A61K45/06 ,  C07D473/18 ,  C07D473/28 ,  A61K2300/00

Abstract: The present invention is directed to novel bicyclic 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.

Abstract translation: 本发明涉及结构式（I）的新型双环杂环，其是二肽基肽酶-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：WO2012139425A1

公开(公告)日：2012-10-18

申请号：PCT/CN2012/000497

申请日：2012-04-12

Applicant: SCHERING CORPORATION ,  WU, Wen-Lian ,  BURNETT, Duane A. ,  STAMFORD, Andrew W. ,  CUMMING, Jared N. ,  BENNETT, Chad Edward ,  GILBERT, Eric J. ,  PENG, Xuanjia ,  SCOTT, Jack D. ,  YU, Younong

Inventor： WU, Wen-Lian ,  BURNETT, Duane A. ,  STAMFORD, Andrew W. ,  CUMMING, Jared N. ,  BENNETT, Chad Edward ,  GILBERT, Eric J. ,  PENG, Xuanjia ,  SCOTT, Jack D. ,  YU, Younong

IPC: C07D279/12 ,  C07D417/12 ,  C07D417/14 ,  C07D417/04 ,  A61K31/54 ,  A61K31/541 ,  A61P25/28 ,  A61P25/16

CPC classification number: C07D279/12 ,  A61K31/54 ,  A61K31/541 ,  A61K45/06 ,  C07D417/04 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention discloses certain iminothiazine compounds and mono- and dioxides thereof, including compounds Formula (I): and tautomers and stereoisomers thereof, and pharmaceutically acceptable salts of said compounds, said tautomers and said stereoismers, wherein each of variables shown in the formula are as defined herein. The compounds of the invention may be 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 uses, including Alzheimer's disease, are also disclosed.

Abstract translation: 本发明公开了某些亚氨基噻嗪化合物及其一氧化二氮和二氧化物，包括式（I）化合物及其互变异构体和立体异构体，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，其中式 如本文所定义。 本发明的化合物可用作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，及其制备和用途的方法，包括阿尔茨海默氏病。

公开(公告)号：WO2008033468A3

公开(公告)日：2008-08-14

申请号：PCT/US2007019934

申请日：2007-09-13

Applicant: SCHERING CORP ,  BURNETT DUANE A ,  MCKITTRICK BRIAN

Inventor： BURNETT DUANE A ,  MCKITTRICK BRIAN

IPC: C07D487/10 ,  A61K31/4747 ,  A61P3/06 ,  A61P25/02

CPC classification number: C07D487/10

Abstract: Disclosed are compounds of the formula (I), wherein Z 1 is -CH 2 - or -C(O)-, R 4 and R 5 are carbon chains (and optionally, together can form a C 2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R 1 and R 3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula (I).

Abstract translation: 公开了式（I）的化合物，其中Z 1是-CH 2 - 或-C（O） - ，R 4和 R 5是碳链（并且可选地，一起可以形成C 2 H 2桥），u和v独立地是0-3的整数，使得总和为3 至5，且R 2为杂芳基，R 1和R 3如本文所定义。 还公开了治疗疼痛的方法，以及使用式（I）化合物抑制胆固醇吸收的方法。

公开(公告)号：WO2008033431A1

公开(公告)日：2008-03-20

申请号：PCT/US2007/019871

申请日：2007-09-13

Applicant: SCHERING CORPORATION ,  BURNETT, Duane, A. ,  MC KITTRICK, Brian, A.

Inventor： BURNETT, Duane, A. ,  MC KITTRICK, Brian, A.

IPC: C07D471/10 ,  A61K31/438 ,  A61P3/06 ,  A61P3/10

CPC classification number: C07D471/10

Abstract: The present invention relates to Spirocyclic Azetidinone Compounds, compositions comprising a Spirocyclic Azetidinone Compound and methods for treating or preventing a disorder of lipid metabolism, pain, diabetes, a vascular condition, demyelination or nonalcoholic fatty liver disease, comprising administering to a patient an effective amount of a Spirocyclic Azetidinone Compound.

Abstract translation: 本发明涉及螺环氮杂环丁酮化合物，包含螺环氮杂环丁酮化合物的组合物和治疗或预防脂质代谢紊乱，疼痛，糖尿病，血管病症，脱髓鞘或非酒精性脂肪性肝病的方法，包括向患者施用有效量 的螺环氮杂环丁酮化合物。

公开(公告)号：WO2007032854A1

公开(公告)日：2007-03-22

申请号：PCT/US2006/031944

申请日：2006-08-16

Applicant: SCHERING CORPORATION ,  BENNETT, Chad, E. ,  GREENLEE, William, J. ,  KNUTSON, Chad, E. ,  BURNETT, Duane, A.

Inventor： BENNETT, Chad, E. ,  GREENLEE, William, J. ,  KNUTSON, Chad, E. ,  BURNETT, Duane, A.

IPC: C07D495/14 ,  A61P25/00 ,  A61P13/00 ,  A61P25/06 ,  A61P25/22 ,  A61P25/04

CPC classification number: C07D487/22 ,  C07D495/14

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula (I) (wherein J 1 -J 3 , X, Z, and R 1 , R 3 , and R 4 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.

Abstract translation: 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 3，Z 1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，其包含用于作为代谢型谷氨酸受体（mGluR）拮抗剂的组合物，其中R 3，R 3和R 4如本文所定义） 化合物和使用化合物和组合物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病的治疗方法。

公开(公告)号：WO2007024593A1

公开(公告)日：2007-03-01

申请号：PCT/US2006/031972

申请日：2006-08-16

Applicant: SCHERING CORPORATION ,  BENNETT, Chad, E. ,  WU, Wen-Lian ,  BURNETT, Duane, A.

Inventor： BENNETT, Chad, E. ,  WU, Wen-Lian ,  BURNETT, Duane, A.

IPC: C07D495/14 ,  A61K31/519 ,  A61P25/00

CPC classification number: C07D495/14 ,  C07D471/14 ,  C07D487/14

Abstract: In its many embodiments, the present invention provides tricyclic compounds of formula I (wherein J 1 -J 3 , X, Z, and R 1 -R 4 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., mGluRI ) such as, for example, pain, migraine, anxiety, urinary incontinence and neurodegenerative diseases such Alzheimer's disease.

Abstract translation: 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，mGluRI）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：WO2005034947A1

公开(公告)日：2005-04-21

申请号：PCT/US2004/032494

申请日：2004-09-30

Applicant: SCHERING CORPORATION ,  SASIKUMAR, Thavalakulamgara, K. ,  BURNETT, Duane, A.

Inventor： SASIKUMAR, Thavalakulamgara, K. ,  BURNETT, Duane, A.

IPC: A61K31/4184

CPC classification number: C04B35/632 ,  C07D235/30 ,  C07D401/12 ,  C07D403/12

Abstract: The present invention discloses compounds of formula I formula I wherein Ar, Z, m, n, p, R 1 and R 8 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.

Abstract translation: 本发明公开了式I化合物，其中Ar，Z，m，n，p，R 1和R 8在本文中定义，所述化合物是黑色素浓缩激素（MCH）的新型拮抗剂，以及 作为制备这些化合物的方法。 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：WO2012138678A1

公开(公告)日：2012-10-11

申请号：PCT/US2012/032039

申请日：2012-04-04

Applicant: MERCK SHARP & DOHME CORP. ,  WU, Wen-Lian ,  BURNETT, Duane, A. ,  GREENLEE, William, J.

Inventor： WU, Wen-Lian ,  BURNETT, Duane, A. ,  GREENLEE, William, J.

IPC: A01N43/16 ,  A61K31/35

CPC classification number: A61K31/5377 ,  A61K31/35 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/453 ,  A61K31/496 ,  A61K31/665 ,  A61K45/06 ,  C07D493/04

Abstract: Disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein each of the substituents is given the definition as set forth in the specification and claims. Also disclosed are pharmaceutical compositions containing the compound of Formula (I) and use of the compound in the treatment of neurodegenerative diseases or conditions such as Alzheimer's disease.

Abstract translation: 本文公开了式（I）的化合物及其药学上可接受的盐，其中每个取代基被给出如说明书和权利要求书中所阐述的定义。 还公开了含有式（I）化合物和该化合物在治疗神经变性疾病或病症如阿尔茨海默病中的用途的药物组合物。

公开(公告)号：WO2008033468A2

公开(公告)日：2008-03-20

申请号：PCT/US2007/019934

申请日：2007-09-13

Applicant: SCHERING CORPORATION ,  BURNETT, Duane, A. ,  MCKITTRICK, Brian

Inventor： BURNETT, Duane, A. ,  MCKITTRICK, Brian

IPC: C07D487/10 ,  A61K31/4747 ,  A61P25/02 ,  A61P3/06

CPC classification number: C07D487/10

Abstract: Disclosed are compounds of the formula (I), wherein Z 1 is -CH 2 - or –C(O)-, R 4 and R 5 are carbon chains (and optionally, together can form a C 2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R2 is heteroaryl, and R 1 and R 3 are as defined herein. Also disclosed are methods of treating pain, and methods of inhibiting the absorption of cholesterol using a compound of formula (I).

Abstract translation: 公开了式（I）的化合物，其中Z 1是-CH 2 - 或-C（O） - ，R 2是 - R 4和R 5是碳链（并且任选一起可以形成C = 2桥），u和v独立地是0- 3，使得和为3至5，且R 2为杂芳基，并且R 1和R 3如本文所定义。 还公开了使用式（I）化合物治疗疼痛的方法和抑制胆固醇吸收的方法。

公开(公告)号：WO2008033447A1

公开(公告)日：2008-03-20

申请号：PCT/US2007/019901

申请日：2007-09-13

Applicant: SCHERING CORPORATION ,  MCKITTRICK, Brian ,  SMITH, Elizabeth, M. ,  BENNETT, Chad, E. ,  BURNETT, Duane, A. ,  KNUTSON, Chad, E.

Inventor： MCKITTRICK, Brian ,  SMITH, Elizabeth, M. ,  BENNETT, Chad, E. ,  BURNETT, Duane, A. ,  KNUTSON, Chad, E.

IPC: A61K31/397 ,  C07D471/10 ,  C07D487/10 ,  A61K31/438 ,  A61P29/00

CPC classification number: C07D471/10 ,  C07D487/10

Abstract: Disclosed are compounds of formula (I) wherein Z 1 is -CH 2 - or -C(O)-, R 4 and R 5 are carbon chains (and optionally, together can form a C 2 bridge), u and v are independently an integer of 0-3 such that there sum is from 3 to 5, and R 2 is heteroaryl, and R 1 and R 3 are as defined herein. Also disclosed are methods of treating pain using a compound of formula (I).

Abstract translation: 公开了式（I）的化合物，其中Z 1是-CH 2 - 或-C（O） - ，R 4和R 4， SUP> 5是碳链（并且可选地，一起可以形成C 2 H 2桥），u和v独立地是0-3的整数，使得总和为3至5 R 2是杂芳基，R 1和R 3如本文所定义。 还公开了使用式（I）化合物治疗疼痛的方法。