JP6144913B2 - 代謝異常の治療に使用されるｇタンパク質共役受容体４３（ｇｐｒ４３）作動薬としてのピロリジンカルボン酸誘導体、医薬組成物および方法 - Google Patents

代謝異常の治療に使用されるｇタンパク質共役受容体４３（ｇｐｒ４３）作動薬としてのピロリジンカルボン酸誘導体、医薬組成物および方法 Download PDF

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JP6144913B2
JP6144913B2 JP2012543780A JP2012543780A JP6144913B2 JP 6144913 B2 JP6144913 B2 JP 6144913B2 JP 2012543780 A JP2012543780 A JP 2012543780A JP 2012543780 A JP2012543780 A JP 2012543780A JP 6144913 B2 JP6144913 B2 JP 6144913B2
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methoxy
cyano
biphenyl
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phenyl
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JP2013514330A (ja
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ホヴェイダ，ハミド
シルス，ディディエ
ズト，ルディヴィン
パルク，ジュリエン
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オゲダ エス．エー．
オゲダ エス．エー．
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JP2012543780A 2009-12-18 2010-12-17 代謝異常の治療に使用されるｇタンパク質共役受容体４３（ｇｐｒ４３）作動薬としてのピロリジンカルボン酸誘導体、医薬組成物および方法 Active JP6144913B2 (ja)

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EP09306270 2009-12-18
EP09306270.1 2009-12-18
US37337010P 2010-08-13 2010-08-13
US61/373,370 2010-08-13
US37601310P 2010-08-23 2010-08-23
US61/376,013 2010-08-23
PCT/EP2010/070040 WO2011073376A1 (en) 2009-12-18 2010-12-17 Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disordersas as agonists of g- protein coupled receptor 43 (gpr43)

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JP6144913B2 true JP6144913B2 (ja) 2017-06-07

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Families Citing this family (21)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NO2513053T3 (enExample) * 2009-12-18 2018-03-03
JP6232384B2 (ja) 2012-01-06 2017-11-15 ノバルティス アーゲー 複素環式化合物およびその使用方法
AU2013290100A1 (en) 2012-07-11 2015-01-29 Elcelyx Therapeutics, Inc. Compositions comprising statins, biguanides and further agents for reducing cardiometabolic risk
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
EP2961746B1 (en) 2013-02-28 2018-01-03 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
CN105916500A (zh) * 2013-11-27 2016-08-31 欧洲筛选有限公司 用于治疗炎性疾病的化合物、药物组合物和方法
CN107108581B (zh) * 2014-08-21 2020-06-23 百时美施贵宝公司 作为强效rock抑制剂的回接苯甲酰胺衍生物
KR101656662B1 (ko) 2014-11-18 2016-09-12 한국생명공학연구원 2-옥소-1,2,3,4-테트라하이드로피리미딘-5-카르복사미드 유도체를 유효성분으로 함유하는 대사성 질환 예방 또는 치료용 약학적 조성물
BR102018007822A2 (pt) 2017-04-20 2018-11-06 Gilead Sciences, Inc. composto, métodos para inibir pd-1, pd-l1 e/ou interação de pd-1/pd-l1 e para tratamento de câncer, composição farmacêutica, e, kit para tratamento de ou prevenção de câncer ou uma doença ou condição
CN107033015B (zh) * 2017-06-02 2019-04-30 南京欧信医药技术有限公司 一种药物中间体的合成方法
WO2019160882A1 (en) 2018-02-13 2019-08-22 Gilead Sciences, Inc. Pd-1/pd-l1 inhibitors
KR102591947B1 (ko) 2018-04-19 2023-10-25 길리애드 사이언시즈, 인코포레이티드 Pd-1/pd-l1 억제제
PE20210642A1 (es) 2018-07-13 2021-03-23 Gilead Sciences Inc Inhibidores de pd-1/pd-l1
US11236085B2 (en) 2018-10-24 2022-02-01 Gilead Sciences, Inc. PD-1/PD-L1 inhibitors
JP2022522534A (ja) 2019-04-02 2022-04-19 アリゴス セラピューティクス インコーポレイテッド Ｐｒｍｔ５を標的にする化合物
WO2021018786A1 (en) 2019-07-26 2021-02-04 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of ffar2 agonists for the treatment of bacterial superinfections post-viral infection
CN110981779B (zh) * 2019-11-23 2021-02-26 武汉理工大学 R-2-(2,5-二氟苯基)吡咯烷的合成方法
CA3180417A1 (en) 2020-06-10 2021-12-16 Guillaume Dutheuil Synthesis of (2s,5r)-5-(2-chlorophenyl)-1-(2'-methoxy-[1,1'-biphenyl]-4-carbonyl)pyrrolidine-2-carboxylic acid
US12503475B2 (en) 2020-09-03 2025-12-23 Centessa Pharmaceuticals (Uk) Limited Bicyclic-heterocycle derivatives and their uses as orexin-2 receptor agonists
WO2022207935A1 (en) 2021-04-02 2022-10-06 Orexia Therapeutics Limited 2-(3-ethynylbenzyl)-substituted heterocycle derivatives as orexin-2 agonists
KR20250084188A (ko) 2022-10-11 2025-06-10 에픽스 테라퓨틱스 (2s,5r)-5-(2-클로로페닐)-1-(2'-메톡시-[1,1'-비페닐]-4-카르보닐)피롤리딘-2-카르복실산의다형체 및 이의 제조 방법

Family Cites Families (26)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3542788A (en) 1968-06-12 1970-11-24 Searle & Co 1-amino-5-phenyl-2-pyrrolepropionic acid and congeners
US4006075A (en) 1975-01-06 1977-02-01 Exxon Research And Engineering Company Method of regenerating a cracking catalyst with substantially complete combustion of carbon monoxide
DE3421295A1 (de) 1984-06-08 1985-12-12 Basf Ag, 6700 Ludwigshafen Neue pyrrolidincarbonsaeurederivative, verfahren zu ihrer herstellung
JPH06104658B2 (ja) * 1988-06-23 1994-12-21 三菱化成株式会社 ピロールカルボン酸誘導体
FR2678938B1 (fr) * 1991-07-10 1993-10-08 Rhone Poulenc Rorer Sa Derives de pyrrolidine, leur preparation et les medicaments les contenant.
GB9206757D0 (en) * 1992-03-27 1992-05-13 Ferring Bv Novel peptide receptor ligands
AU1856997A (en) 1996-02-02 1997-08-22 Merck & Co., Inc. Method for raising hdl cholesterol levels
JP3005469B2 (ja) 1996-06-05 2000-01-31 住友軽金属工業株式会社 内面スズめっき長尺銅管の製造方法
US6177464B1 (en) 1997-03-14 2001-01-23 Sepracor, Inc. Ring opening metathesis of alkenes
EP1278743A4 (en) 2000-05-05 2003-05-14 Smithkline Beecham Corp NEW ANTI-INFECTIOUS ACTIVE SUBSTANCES
US7105556B2 (en) * 2001-05-30 2006-09-12 Bristol-Myers Squibb Company Conformationally constrained analogs useful as antidiabetic and antiobesity agents and method
DE60221875T2 (de) 2001-11-02 2007-12-20 Glaxo Group Ltd., Greenford 4-(6-gliedrige)-heteroaryl-acyl-pyrrolidinderivate als hcv-inhibitoren
FI20030014A0 (fi) 2003-01-03 2003-01-03 Orion Corp Prolyylioligopeptidaasia inhiboivaa aktiivisuutta omaavia yhdisteitä
US20040142379A1 (en) * 2003-01-16 2004-07-22 Carlsberg Research Laboratory Affinity fishing for ligands and proteins receptors
US7544699B2 (en) * 2003-08-08 2009-06-09 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions, and methods of use
WO2005014532A1 (en) * 2003-08-08 2005-02-17 Transtech Pharma, Inc. Aryl and heteroaryl compounds, compositions and methods of use
TW200528107A (en) * 2003-11-25 2005-09-01 Nissan Chemical Ind Ltd T-type calcium channel inhibitor
WO2005122379A2 (en) * 2004-05-27 2005-12-22 The Regents Of The University Of California Alpha-4 beta-1 integrin ligands for imaging and therapy
AU2005289810A1 (en) 2004-09-22 2006-04-06 Arena Pharmaceuticals, Inc. GPR43 and modulators thereof for the treatment of metabolic-related disorders
US7759337B2 (en) 2005-03-03 2010-07-20 Amgen Inc. Phthalazine compounds and methods of use
US7425633B2 (en) * 2005-08-26 2008-09-16 National Health Research Institutes Pyrrolidine compounds
US8202902B2 (en) * 2006-05-05 2012-06-19 The Regents Of The University Of Michigan Bivalent SMAC mimetics and the uses thereof
US20090004140A1 (en) * 2007-06-26 2009-01-01 Yao-Ling Qiu 4-substituted pyrrolidine as anti-infectives
US20090233972A1 (en) 2008-03-12 2009-09-17 Yat Sun Or Substituted heterocycles as anti-infectives
US20100074863A1 (en) 2008-09-17 2010-03-25 Yat Sun Or Anti-infective pyrrolidine derivatives and analogs
NO2513053T3 (enExample) * 2009-12-18 2018-03-03

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