公开(公告)号：US09227973B2

公开(公告)日：2016-01-05

申请号：US14399762

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark Fraley ,  Tesfaye Biftu ,  Cheng Zhu ,  Anilkumar Nair

IPC: C07D471/10 ,  C07D471/20 ,  C07D519/00

CPC classification number: C07D471/20 ,  C07D471/10 ,  C07D519/00

Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的吡啶衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US20150087641A1

公开(公告)日：2015-03-26

申请号：US14399712

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark Fraley ,  Tesfaye Biftu ,  Cheng Zhu ,  Anilkumar Nair

IPC: C07D498/04

CPC classification number: C07D498/04

Abstract: The present invention is directed to heterocyclic compounds which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的杂环化合物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US20140329798A1

公开(公告)日：2014-11-06

申请号：US14358241

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Edmondson ,  Zhiyong Hu ,  Ping Liu ,  Gregori J. Morriello ,  Jason W. Szewczyk ,  Bowei Wang ,  Liping Wang ,  Harold B. Wood ,  Cheng Zhu ,  Yuping Zhu ,  Zhiqiang Guo

IPC: C07D513/04 ,  C07D239/42 ,  C07D405/12 ,  C07D409/12 ,  C07D498/04 ,  C07D487/04 ,  C07D403/14 ,  C07D401/14 ,  C07D403/12 ,  C07D471/04

CPC classification number: C07D513/04 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included

Abstract translation: 披露式（I）的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法

公开(公告)号：US09018224B2

公开(公告)日：2015-04-28

申请号：US14358241

申请日：2012-11-09

Applicant: Merck Sharp & Dohme Corp.

Inventor： Scott Edmondson ,  Zhiyong Hu ,  Ping Liu ,  Gregori J. Morriello ,  Jason W. Szewczyk ,  Bowei Wang ,  Liping Wang ,  Harold B. Wood ,  Cheng Zhu ,  Yuping Zhu ,  Zhiqiang Guo

IPC: A01N43/54 ,  A61K31/505 ,  C07D513/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04 ,  C07D239/42 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D409/12

CPC classification number: C07D513/04 ,  C07D239/42 ,  C07D401/04 ,  C07D401/14 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04 ,  C07D498/04

Abstract: Substituted cyclopropyl compounds of the formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing type 2 diabetes and similar conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR-119. Pharmaceutical compositions and methods of treatment are also included.

Abstract translation: 披露式（I）的取代的环丙基化合物及其药学上可接受的盐可用于治疗或预防2型糖尿病和类似病状。 该化合物可用作G蛋白偶联受体GPR-119的激动剂。 还包括药物组合物和治疗方法。

公开(公告)号：US20150099771A1

公开(公告)日：2015-04-09

申请号：US14399762

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark Fraley ,  Tesfaye Biftu ,  Cheng Zhu ,  Anilkumar Nair

IPC: C07D471/20 ,  C07D519/00

CPC classification number: C07D471/20 ,  C07D471/10 ,  C07D519/00

Abstract: The present invention is directed to pyridine derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的吡啶衍生物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。

公开(公告)号：US10000454B2

公开(公告)日：2018-06-19

申请号：US15310488

申请日：2015-05-19

Applicant: Merck Sharp & Dohme Corp.

Inventor： Tesfaye Biftu ,  Purakkattle Biju ,  Timothy A. Blizzard ,  Zhengxia Chen ,  Matthew J. Clements ,  Mingxiang Cui ,  Jessica L. Frie ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Anilkumar G. Nair ,  Christopher W. Plummer ,  Cheng Zhu

IPC: C07D221/16 ,  A61K31/435 ,  A61K31/444 ,  C07D401/12 ,  C07D405/12 ,  A61K31/192 ,  A61K31/438 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/538 ,  A61K31/55 ,  A61K45/06 ,  C07C61/39 ,  C07D215/14 ,  C07D401/04 ,  C07D413/12

CPC classification number: C07D221/16 ,  A61K31/192 ,  A61K31/366 ,  A61K31/397 ,  A61K31/435 ,  A61K31/438 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/538 ,  A61K31/55 ,  A61K45/06 ,  C07C61/39 ,  C07C2602/08 ,  C07C2603/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US09932311B2

公开(公告)日：2018-04-03

申请号：US15023124

申请日：2014-09-30

Applicant: Merck Sharp & Dohme Corp.

Inventor： Tesfaye Biftu ,  Purakkattle Biju ,  Steven L. Colletti ,  Mingxiang Cui ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Nam Fung Kar ,  Anilkumar Nair ,  Ravi Nargund ,  Donald M. Sperbeck ,  Cheng Zhu

IPC: C07D221/16 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06

CPC classification number: C07D221/16 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20170081287A1

公开(公告)日：2017-03-23

申请号：US15310488

申请日：2015-05-19

Applicant: Tesfaye BIFTU ,  Purakkattle BIJU ,  Timothy A. BLIZZARD ,  Zhengxia CHEN ,  Matthew J. CLEMENTS ,  Mingxiang CUI ,  Jessica L. FRIE ,  William K. HAGMANN ,  Bin HU ,  Hubert JOSIEN ,  Anilkumar G. NAIR ,  Christopher W. PLUMMER ,  Cheng ZHU ,  Merck Sharp & Dohme Corp.

Inventor： Tesfaye Biftu ,  Purakkattle Biju ,  Timothy A. Blizzard ,  Zhengxia Chen ,  Matthew J. Clements ,  Mingxiang Cui ,  Jessica L. Frie ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Anilkumar G. Nair ,  Christopher W. Plummer ,  Cheng Zhu

IPC: C07D221/16 ,  A61K31/438 ,  C07D405/12 ,  C07D401/12 ,  A61K31/444 ,  C07C61/39 ,  A61K31/192 ,  A61K31/4725 ,  A61K31/4709 ,  A61K31/538 ,  C07D413/12 ,  A61K31/55 ,  C07D215/14 ,  A61K31/47 ,  C07D401/04 ,  A61K45/06

CPC classification number: C07D221/16 ,  A61K31/192 ,  A61K31/366 ,  A61K31/397 ,  A61K31/435 ,  A61K31/438 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/4985 ,  A61K31/538 ,  A61K31/55 ,  A61K45/06 ,  C07C61/39 ,  C07C2602/08 ,  C07C2603/12 ,  C07D215/14 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12 ,  A61K2300/00

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

公开(公告)号：US20160207887A1

公开(公告)日：2016-07-21

申请号：US15023124

申请日：2014-09-30

Applicant: MERCK SHARP & DOHME CORP.

Inventor： Tesfaye Biftu ,  Purakkattle Biju ,  Steven L. Colletti ,  Mingxiang Cui ,  William K. Hagmann ,  Bin Hu ,  Hubert Josien ,  Nam Fung Kar ,  Anilkumar Nair ,  Ravi Nargund ,  Donald M. Sperbeck ,  Cheng Zhu

IPC: C07D221/16 ,  A61K45/06 ,  C07D405/12 ,  A61K31/444 ,  A61K31/435 ,  C07D401/12

CPC classification number: C07D221/16 ,  A61K31/435 ,  A61K31/444 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12

Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslip idemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.

Abstract translation: 结构式（I）的新型化合物及其药学上可接受的盐是G蛋白偶联受体40（GPR40）的激动剂，可用于治疗，预防和抑制G蛋白偶联受体 受体40.本发明的化合物可用于治疗2型糖尿病，以及通常与该疾病相关的病症，包括肥胖症和脂质疾病，例如混合型或糖尿病型血脂异常，高脂血症，高胆固醇血症， 和高甘油三酯血症。

公开(公告)号：US09296750B2

公开(公告)日：2016-03-29

申请号：US14399438

申请日：2013-05-03

Applicant: Merck Sharp & Dohme Corp.

Inventor： Ian M. Bell ,  Mark Fraley ,  Tesfaye Biftu ,  Cheng Zhu ,  Anilkumar Nair

IPC: C07D471/10 ,  C07D491/22 ,  C07D471/04 ,  C07D491/107 ,  C07D491/20

CPC classification number: C07D471/10 ,  C07D471/04 ,  C07D491/107 ,  C07D491/20 ,  C07D491/22

Abstract: The present invention is directed to spirolactam analogs which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which CGRP is involved, such as migraine. 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 CGRP is involved.

Abstract translation: 本发明涉及作为CGRP受体的拮抗剂的螺内酰胺类似物，其可用于治疗或预防涉及CGRP的疾病，例如偏头痛。 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CGRP的疾病中的用途。