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1. 发明公开

KR20120118086A Hydroxymethyl pyrrolidines as beta 3 adrenergic receptor agonists 审中-公开
标题翻译：羟甲基吡咯烷作为β3肾上腺素能受体激动剂
公开(公告)号：KR20120118086A
公开(公告)日：2012-10-25
申请号：KR20127026256
申请日：2009-04-02
申请人： MERCK SHARP & DOHME
发明人： BERGER RICHARD , CHANG LEHUA , EDMONDSON SCOTT D , GOBLE STEPHEN D , HA SOOKHEE NICOLE , KAR NAM FUNG , KOPKA IHOR E , LI BING , MORRIELLO GREGORI J , MOYES CHRIS R , SHEN DONG MING , WANG LIPING , ZHU CHENG
IPC分类号： C07D417/12 , A61K31/428 , A61P13/00 , C07D403/12
CPC分类号： C07D487/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： 본 발명은 화학식 Ia의 화합물, 이의 약제학적 조성물 및 β3-아드레날린성 수용체의 활성화에 의해 매개되는 질환의 치료 또는 예방에 있어서 이를 사용하는 방법을 제공한다.
화학식 Ia

2. 发明专利

JP2012020961A HYDROXYMETHYL PYRROLIDINE AS β3 ADRENOCEPTOR AGONIST 有权
标题翻译：羟丙基吡咯烷作为β3ADRENOCEPTOR AGONIST
公开(公告)号：JP2012020961A
公开(公告)日：2012-02-02
申请号：JP2010159938
申请日：2010-07-14
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・エンド・ドーム・コーポレイション
发明人： BERGER RICHARD , CHANG LEHUA , EDMONDSON SCOTT D , GOBLE STEPHEN D , HA SOOKHEE NICOLE , KAR NAM FUNG , KOPKA IHOR E , LI BING , MORRIELLO GREGORI J , MOYES CHRIS R , SHEN DONG-MING , WANG LIPING , ZHU CHENG
IPC分类号： C07D207/09 , A61K31/4025 , A61K31/41 , A61K31/416 , A61K31/4178 , A61K31/4192 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/498 , A61K31/502 , A61K31/517 , A61K31/519 , A61K31/53 , A61P7/12 , A61P13/06 , A61P13/10 , C07D207/16 , C07D207/325 , C07D401/12 , C07D401/14 , C07D403/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
CPC分类号： C07D487/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide a new β3-adrenergic receptor agonist.SOLUTION: The compound is represented by formula I [wherein m is 0-4; n is 0-5; q is 0-4; X is -CO- or the like; Y is 1-5C alkanediyl or the like; Z is phenyl or the like; Ris 1-5C alkyl which may be replaced with 1-5 halogen atoms or the like; Ris a halogen or the like; Ris 1-6C alkyl which may be replaced with 1-5 groups selected from halogens or the like]. The pharmaceutical composition including the compound is useful for treating or preventing diseases mediated by β3AR activation.
摘要翻译：要解决的问题：提供新的β3肾上腺素能受体激动剂。解决方案：该化合物由式I表示[其中m为0-4; n为0-5; q为0-4; X是-CO-等; Y为1-5C烷二基等; Z是苯基等; R 1是可以被1-5个卤素原子等取代的1-5C烷基; R 2 是卤素等; R 3是可以被选自卤素等的1-5个基团取代的1-6C烷基]。包含该化合物的药物组合物可用于治疗或预防β3AR活化介导的疾病。版权所有（C）2012，JPO＆INPIT

3. 发明专利

JP2011201897A Hydroxymethyl pyrrolidine as beta 3 adrenergic receptor agonist 有权
标题翻译：羟丙基吡咯烷作为3型ADRENERGIC受体激动剂
公开(公告)号：JP2011201897A
公开(公告)日：2011-10-13
申请号：JP2011107738
申请日：2011-05-13
申请人： Merck Sharp & Dohme Corp , メルク・シャープ・エンド・ドーム・コーポレイション
发明人： BERGER RICHARD , CHANG LEHUA , EDMONDSON SCOTT D , GOBLE STEPHEN D , HA SOOKHEE NICOLE , KAR NAM FUNG , KOPKA IHOR E , LI BING , MORRIELLO GREGORI J , MOYES CHRIS R , SHEN DONG-MING , WANG LIPING , ZHU CHENG
IPC分类号： C07D403/12 , A61K31/4025 , A61K31/41 , A61K31/4155 , A61K31/416 , A61K31/4192 , A61K31/4196 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/437 , A61K31/4375 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/502 , A61K31/506 , A61K31/517 , A61K31/519 , A61K31/53 , A61K45/00 , A61P13/10 , C07D207/09 , C07D401/12 , C07D403/14 , C07D413/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/04 , C07D495/04
CPC分类号： C07D487/04 , C07D401/12 , C07D403/12 , C07D417/12 , C07D471/04
摘要： PROBLEM TO BE SOLVED: To provide pharmaceutical compositions and a method for treatment or prophylaxis of disorders mediated through β 3 adrenergic receptor using the compositions.SOLUTION: There are provided a compound represented by formula (I) or a pharmaceutically acceptable salt thereof and use of the pharmaceutical compositions containing a second active agent (wherein X is -CO- or -SO2-; Y is selected from the group consisting of: (1) 1-5C alkanediyl, 2-5C alkenediyl, and 2-5C alkynediyl; Z is selected from the group consisting of: (1) phenyl, (2) a 5- or 6-membered heterocyclic ring with from 1 to 4 heteroatoms selected from oxygen, sulfur and nitrogen, (3) a benzene ring fused to a 5-10C carbocyclic ring, (4) a heterocyclic ring combined with (2)).
摘要翻译：要解决的问题：提供药物组合物和使用该组合物治疗或预防由β3肾上腺素能受体介导的病症的方法。溶液：提供由式（I）表示的化合物或其药学上可接受的盐，并且使用含有第二活性剂（其中X为-CO-或-SO 2 - ; Y选自：（1）1-5C烷二基，2-5C亚乙基和2-5C炔二基的药物组合物; Z为选自：（1）苯基，（2）具有1至4个选自氧，硫和氮的杂原子的5或6元杂环，（3）与5-10C稠合的苯环碳环，（4）与（2）结合的杂环）。

4. 发明申请

WO2013169574A2 ALIPHATIC SPIROLACTAM CGRP RECEPTOR ANTAGONISTS 审中-公开
标题翻译： ALIPHATIC SPIROLACTAM CGRP受体拮抗剂
公开(公告)号：WO2013169574A2
公开(公告)日：2013-11-14
申请号：PCT/US2013039373
申请日：2013-05-03
申请人： MERCK SHARP & DOHME , BELL IAN M , FRALEY MARK , BIFTU TESFAYE , ZHU CHENG , NAIR ANILKUMAR , MITCHELL HELEN
发明人： BELL IAN M , FRALEY MARK , BIFTU TESFAYE , ZHU CHENG , NAIR ANILKUMAR , MITCHELL HELEN
IPC分类号： A61K31/55
CPC分类号： C07D471/20 , A61K9/4858 , A61K31/45 , A61K31/451 , A61K31/4523
摘要： The present invention is directed to aliphatic spirolactam 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.
摘要翻译：本发明涉及作为CGRP受体的拮抗剂的脂族螺内酰胺衍生物，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。

6. 发明专利

ES2747973T3 Compuestos tricíclicos antidiabéticos 未知
公开(公告)号：ES2747973T3
公开(公告)日：2020-03-12
申请号：ES14862098
申请日：2014-11-10
申请人： MERCK SHARP & DOHME
发明人： BIFTU TESFAYE , BIJU PURAKKATTLE , COLLETTI STEVEN L , DANG QUN , DHONDI PAWAN K , GUDE CANDIDO , JOSIEN HUBERT , KAR NAM FUNG , NAIR ANILKUMAR G , NARGUND RAVI P , YANG DE-YI , XIAO DONG , ZHU CHENG
IPC分类号： C07D221/16 , A61K31/435 , A61P3/10 , C07D401/12 , C07D487/04 , C07D487/10
摘要： Un compuesto de fórmula estructural I:**Fórmula** o una sal farmacéuticamente aceptable del mismo; en la que A es fenilo; B se selecciona del grupo que consiste en: (1) fenilo, y (2) piridilo; R1 se selecciona del grupo que consiste en: (1) halógeno, (2) -CN, (3) -alquilo C1-6, (4) -(CH2)rOalquilo C1-6, (5) -(CH2)r-cicloalquilo C3-6, y (6) -(CH2)r-O-(CH2)r-cicloalquilo C3-6, en donde cada CH2, -alquilo C1-6, -Oalquilo C1-6 y -cicloalquilo C3-6 está sin sustituir o sustituido con uno a cuatro sustituyentes seleccionados de halógeno, -alquilo C1-6 y -(CH2)v-cicloalquilo C3-6; R2 es halógeno; cada R3, cuando está presente, se selecciona independientemente del grupo que consiste en: (1) halógeno, (2) -CN, (3) -alquilo C1-6, y (4) -(CH2)u-cicloalquilo C3-6, en donde cada CH2, alquilo C1-6 y cicloalquilo C3-6 está sin sustituir o sustituido con uno a tres sustituyentes seleccionados de halógeno; R4 se selecciona del grupo que consiste en: (1) -(CH2)pcicloalquilo C3-6, (2) -O(CH2)pcicloalquilo C3-6, (3) -(CH2)p-cicloheteroalquilo C2-10, (4) arilo, y (5) heteroarilo, en donde R4 está sin sustituir o sustituido con uno, dos, tres, cuatro o cinco sustituyentes seleccionados de R5; R5 se selecciona del grupo que consiste en: (1) -(CH2)shalógeno, (2) -alquilo C1-6, (3) -(CH2)s-O-alquilo C1-6, (4) -(CH2)sOH, (5) -(CH2)sCN, (6) -(CH2)sSO2alquilo C1-6, (7) -(CH2)sSO2-(CH2)t-cicloalquilo C3-6, (8) -CF3, (9) -OCHF2, (10) -OCF3, (11) -SCH3, (12) -NH2, (13) oxo, (14) -NHSO2alquilo C1-6, (15) -NHCOalquilo C1-6, (16) -NH(alquilo C1-6), y (17) -N(alquilo C1-6)2, en donde cada CH2, alquilo C1-6 y cicloalquilo C3-6 está sin sustituir o sustituido con uno a tres sustituyentes seleccionados de halógeno, alquilo C1-6 y -(CH2)wOH; m es 0, 1, 2 o 3; n es 1 o 2; p es 0, 1, 2, 3 o 4; r es 0, 1, 2 o 3; s es 0, 1, 2 o 3; t es 0, 1, 2 o 3; u es 0, 1, 2 o 3; v es 0, 1, 2 o 3; y w es 0, 1, 2 o 3.

7. 发明专利

MA43128A INHIBITEURS DU FACTEUR XIA 未知
公开(公告)号：MA43128A
公开(公告)日：2018-09-05
申请号：MA43128
申请日：2016-10-24
申请人： MERCK SHARP & DOHME
发明人： ALI AMJAD , BARA THOMAS , EDMONDSON SCOTT D , GAO YING-DUO , HARPER BART , LIM YEON-HEE , LIU WEIGUO , MERTZ ERIC , NEELAMKAVIL SANTHOSH F , SHEN DONG-MING , SUN WANYING , XU JIAYI , YANG MENG , ZHOU WEI , ZHU CHENG
IPC分类号： A61K31/44 , A61K31/4418 , A61K31/4427 , C07D213/02 , C07D213/04 , C07D401/06

8. 发明专利

AU2012339870B2 Substituted cyclopropyl compounds useful as GPR119 agonists 未知
公开(公告)号：AU2012339870B2
公开(公告)日：2017-06-29
申请号：AU2012339870
申请日：2012-11-09
申请人： MERCK SHARP & DOHME
发明人： EDMONDSON SCOTT , HU ZHIYONG , LIU PING , MORRIELLO GREGORI J , SZEWCZYK JASON W , WANG BOWEI , WANG LIPING , WOOD HAROLD B , ZHU CHENG , ZHU YUPING , GUO ZHIQIANG
IPC分类号： C07D401/00
摘要： 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

9. 发明专利

CA2770475C NOVEL PYRROLIDINE DERIVED BETA 3 ADRENERGIC RECEPTOR AGONISTS 未知
公开(公告)号：CA2770475C
公开(公告)日：2017-06-27
申请号：CA2770475
申请日：2010-08-24
申请人： MERCK SHARP & DOHME
发明人： EDMONDSON SCOTT D , CHANG LEHUA , KAR NAM FUNG , MORRIELLO GREGORI J , MOYES CHRISTOPHER J , SHEN DONG-MING , ZHU CHENG , ANTHONY NEVILLE J , JONES PHILIP , SMITH GRAHAM F , SCOTT MARK E , THOMPSON CHRISTOPHER F , JUNG JOON , CAMMARANO CAROLYN , HOFFMAN DAWN MARIE
IPC分类号： C07D403/12 , A61K31/33 , C07D207/08 , C07D401/12 , C07D405/12 , C07D413/12 , C07D417/12
摘要： The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ß3-adrenoceptor.

10. 发明专利

AU2015263620A1 Antidiabetic tricyclic compounds 未知
公开(公告)号：AU2015263620A1
公开(公告)日：2016-10-20
申请号：AU2015263620
申请日：2015-05-19
申请人： MERCK SHARP & DOHME
发明人： BIFU TESFAYE , BIJU PURAKKATTLE , BLIZZARD TIMOTHY A , CHEN ZHENGXIA , CLEMENTS MATTHEW J , CUI MINGXIANG , FRIE JESSICA L , HAGMANN WILLIAM K , HU BIN , JOSIEN HUBERT , NAIR ANILKUMAR , PLUMMER CHRISTOPHER W , ZHU CHENG
IPC分类号： C07D221/16 , A61K31/415 , A61K31/438 , A61P3/10 , C07D401/12 , C07D405/12
摘要： 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.

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