CN109867630A - 新型glp-1受体调节剂 - Google Patents

新型glp-1受体调节剂 Download PDF

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CN109867630A
CN109867630A CN201910207853.5A CN201910207853A CN109867630A CN 109867630 A CN109867630 A CN 109867630A CN 201910207853 A CN201910207853 A CN 201910207853A CN 109867630 A CN109867630 A CN 109867630A
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compound
present
aryl
certain embodiments
alkyl
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马库斯·F·勃姆
埃丝特·马丁伯勒
玛妮莎·穆尔加尼
田宫淳子
黄黎明
亚当·R·耶格尔
埃努格尔斯伊·布拉哈马查理
托马斯·福勒
安德鲁·诺瓦克
拉姆基·玛格哈尼
迈克尔·科奈格斯
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Receptos LLC
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Gene Second International Ltd
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    • A61K31/155—Amidines (), e.g. guanidine (H2N—C(=NH)—NH2), isourea (N=C(OH)—NH2), isothiourea (—N=C(SH)—NH2)
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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CN201910207853.5A 2013-06-11 2014-06-11 新型glp-1受体调节剂 Pending CN109867630A (zh)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201361833737P 2013-06-11 2013-06-11
US61/833,737 2013-06-11
US201461981643P 2014-04-18 2014-04-18
US61/981,643 2014-04-18
CN201480044849.7A CN105593225B (zh) 2013-06-11 2014-06-11 新型glp-1受体调节剂

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Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12234236B1 (en) 2023-09-14 2025-02-25 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP6007417B2 (ja) 2011-05-31 2016-10-12 レセプトス エルエルシー 新規ｇｌｐ−１受容体安定剤および調節剤
AU2012352349B2 (en) 2011-12-12 2017-08-17 Receptos Llc Carboxylic acid derivatives comprising four cycles acting as GLP-1 receptor modulators for therapy of diseases such as diabetes
CN109867630A (zh) 2013-06-11 2019-06-11 赛尔基因第二国际有限公司 新型glp-1受体调节剂
EP3172199B1 (en) 2014-07-25 2020-07-01 Celgene International II Sarl Pyrimidine derivatives as glp-1 receptor modulators
AU2015360364B2 (en) 2014-12-10 2020-04-30 Receptos Llc GLP-1 receptor modulators
EA202092441A1 (ru) 2016-06-07 2021-05-21 Джакобио Фармасьютикалс Ко., Лтд. Новые гетероциклические производные, применимые в качестве ингибиторов shp2
KR20240026521A (ko) 2017-03-23 2024-02-28 자코바이오 파마슈티칼스 컴퍼니 리미티드 Shp2 억제제로서 유용한 신규한 헤테로환형 유도체
ES2937835T3 (es) * 2017-04-28 2023-03-31 Receptos Llc Nuevos moduladores del receptor de GLP-1
CN112839935A (zh) 2018-09-26 2021-05-25 北京加科思新药研发有限公司 可用作shp2抑制剂的新型杂环衍生物
CN109608524B (zh) * 2018-11-09 2022-06-03 北京志道生物科技有限公司 兼具dpp-4抑制及glp1r激活活性的多肽衍生物、制备和应用
CN119841865A (zh) 2020-02-07 2025-04-18 加舒布鲁姆生物公司 杂环glp-1激动剂
FI4143183T3 (fi) 2020-04-29 2026-01-07 Gasherbrum Bio Inc Heterosyklisiä glp-1-agonisteja
CN111548311B (zh) * 2020-06-04 2021-04-23 山西医科大学 一种小分子glp-1r激动剂及其应用
PE20231181A1 (es) 2020-08-06 2023-08-11 Gasherbrum Bio Inc Agonistas del glp-1 heterociclicos
CN119137124A (zh) 2022-03-09 2024-12-13 加舒布鲁姆生物公司 杂环glp-1激动剂
WO2023179542A1 (en) 2022-03-21 2023-09-28 Gasherbrum Bio , Inc. 5,8-dihydro-1,7-naphthyridine derivatives as glp-1 agonists for the treatment of diabetes
WO2023198140A1 (en) 2022-04-14 2023-10-19 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
CN114989204A (zh) * 2022-06-16 2022-09-02 西北工业大学 一种葡萄糖响应自修复凝胶用的二苯乙炔类液晶态交联剂的制备方法

Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995012611A1 (en) * 1993-11-01 1995-05-11 Japat Ltd. Endothelin receptor antagonists
JPH11189586A (ja) * 1997-12-25 1999-07-13 Kirin Brewery Co Ltd キノリン誘導体、イソキノリン誘導体、およびシンノリン誘導体、並びに抗炎症剤および抗アレルギー剤
CN1281430A (zh) * 1997-08-22 2001-01-24 霍夫曼-拉罗奇有限公司 芳酰基苯丙氨酸衍生物
CN1288457A (zh) * 1998-01-20 2001-03-21 田边制药株式会社 α4介导的细胞粘着的抑制剂
US20030149083A1 (en) * 1999-11-18 2003-08-07 Ajinomoto Co. Inc Phenylalanine derivatives
CN1119340C (zh) * 1997-07-31 2003-08-27 伊兰药品公司 抑制vla－4介导的白细胞粘着的氨基甲酰氧基化合物
WO2003070709A1 (en) * 2002-02-20 2003-08-28 Ajinomoto Co.,Inc. Novel phenylalanine derivative
EP1700850A1 (en) * 2003-12-22 2006-09-13 Ajinomoto Co., Inc. Novel phenylalanine derivative
CN1918118A (zh) * 2004-02-17 2007-02-21 石原产业株式会社 硫代酰胺类化合物或其盐、以及包含它们的细胞因子产生抑制剂
CN1938283A (zh) * 2004-02-10 2007-03-28 詹森药业有限公司 作为α4整联蛋白拮抗剂的哒嗪酮
CN101360711A (zh) * 2005-11-23 2009-02-04 阿斯利康(瑞典)有限公司 L-苯丙氨酸衍生物及其作为整联蛋白拮抗剂的用途
WO2011094890A1 (en) * 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
CN104080767A (zh) * 2011-12-12 2014-10-01 瑞塞普托斯公司 新的glp-1受体调节剂

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IT1062206B (it) 1974-02-01 1983-09-20 Rotta Research Lab S P A A S Derivati della tirosina attivi sulla muscolatura liscia
DE2423536A1 (de) 1974-05-15 1975-11-27 Bayer Ag 3-amino-phenylessigsaeure-derivate, verfahren zu ihrer herstellung sowie ihre verwendung als herbizide
SK94393A3 (en) * 1992-09-11 1994-08-10 Thomae Gmbh Dr K Cyclic derivatives of urea, process for their production and their pharmaceutical agents with the content of those
US5424286A (en) 1993-05-24 1995-06-13 Eng; John Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same
US6174905B1 (en) 1996-09-30 2001-01-16 Mitsui Chemicals, Inc. Cell differentiation inducer
EP0996459B1 (en) 1997-01-07 2005-09-21 Amylin Pharmaceuticals, Inc. Use of exendins and agonists thereof for the reduction of food intake
HUP0003921A3 (en) 1997-07-31 2001-03-28 Wyeth Corp Sulfonylated dipeptide compounds which inhibit leukocyte adhesion mediated by vla-4, pharmaceutical compositions comprising thereof and their use
US6583139B1 (en) 1997-07-31 2003-06-24 Eugene D. Thorsett Compounds which inhibit leukocyte adhesion mediated by VLA-4
CN1276785A (zh) * 1997-08-22 2000-12-13 霍夫曼-拉罗奇有限公司 N－烷酰基苯丙氨酸衍生物
US6191171B1 (en) 1997-11-20 2001-02-20 Merck & Co., Inc. Para-aminomethylaryl carboxamide derivatives
US6197794B1 (en) * 1998-01-08 2001-03-06 Celltech Therapeutics Limited Phenylalanine derivatives
JP2002538081A (ja) 1998-12-07 2002-11-12 ソシエテ・ドゥ・コンセイユ・ドゥ・ルシェルシュ・エ・ダプリカーション・シャンティフィック・エス・ア・エス Ｇｌｐ−１の類似体
NZ512663A (en) 1999-01-14 2004-05-28 Amylin Pharmaceuticals Inc Novel exendin agonist formulations and methods of administration thereof
AU3487500A (en) * 1999-02-08 2000-08-25 Lion Bioscience Ag Thiazole derivatives and combinatorial libraries thereof
JP3795305B2 (ja) * 1999-07-19 2006-07-12 田辺製薬株式会社 医薬組成物
TWI302149B (en) 1999-09-22 2008-10-21 Bristol Myers Squibb Co Substituted acid derivatives useful as antiodiabetic and antiobesity agents and method
RU2270193C2 (ru) * 1999-12-06 2006-02-20 Ф.Хоффманн-Ля Рош Аг 4-пиридинил-n-ацил-l-фенилаланины
RU2281283C2 (ru) 2000-03-07 2006-08-10 Санофи-Авентис Дойчланд Гмбх Замещенные 3-фенил-5-алкокси-1,3,4-оксадиазол-2-оны и их применение для ингибирования гормоночувствительной липазы
US6960597B2 (en) * 2000-06-30 2005-11-01 Orth-Mcneil Pharmaceutical, Inc. Aza-bridged-bicyclic amino acid derivatives as α4 integrin antagonists
SK287781B6 (sk) * 2000-08-18 2011-09-05 Ajinomoto Co., Inc. Fenylalanínové deriváty, farmaceutický prípravok s ich obsahom a ich použitie
JP4895067B2 (ja) * 2000-09-29 2012-03-14 味の素株式会社 新規フェニルアラニン誘導体
AU2002350217A1 (en) 2001-12-04 2003-06-17 Bristol-Myers Squibb Company Glycinamides as factor xa inhibitors
EP1454898A4 (en) * 2001-12-13 2006-12-13 Ajinomoto Kk NEW PHENYL ALANIDE DERIVATIVES
WO2003089410A1 (en) * 2002-04-19 2003-10-30 Kyowa Hakko Kogyo Co., Ltd. Phenylalanine derivative
US20070276034A1 (en) 2002-05-31 2007-11-29 Luke Esposito Compounds, compositions and methods for the treatment of synucleinopathies
PT1537116E (pt) 2002-09-04 2010-09-03 Schering Corp Pirazolopirimidinas adequadas para o tratamento de doenças cancerosas
WO2004022561A1 (en) 2002-09-04 2004-03-18 Schering Corporation Pyrazolopyrimidines as cyclin-dependent kinase inhibitors
US20040152750A1 (en) 2002-12-20 2004-08-05 Kodra Janos Tibor Novel glucagon antagonists
EP1595870B1 (en) * 2003-02-20 2015-09-23 Ajinomoto Co., Inc. Process for producing phenylalanine derivative having quinazolinedione skeleton and intermediate for the same
EA008798B1 (ru) 2003-06-13 2007-08-31 Лабораториос С.А.Л.В.А.Т., С.А. НОВЫЕ БЕНЗАМИДЫ В КАЧЕСТВЕ PPARγ МОДУЛЯТОРОВ
US7618981B2 (en) * 2004-05-06 2009-11-17 Cytokinetics, Inc. Imidazopyridinyl-benzamide anti-cancer agents
WO2006117743A1 (en) 2005-05-03 2006-11-09 Ranbaxy Laboratories Limited Substituted aromatic compounds as antidiabetic agents
WO2006127595A1 (en) 2005-05-23 2006-11-30 Arena Pharmaceuticals, Inc. 5-aminopyrazole carboxylic acid derivatives and methods of treatment of metabolic-related disorders thereof
US7825139B2 (en) 2005-05-25 2010-11-02 Forest Laboratories Holdings Limited (BM) Compounds and methods for selective inhibition of dipeptidyl peptidase-IV
WO2006137450A1 (ja) * 2005-06-21 2006-12-28 Ajinomoto Co., Inc. フェニルアラニン誘導体の結晶、その製造方法及びその使用
EP2049490A1 (en) * 2006-06-09 2009-04-22 Astra Zeneca AB N-(benzoyl)-o- [2- (pyridin- 2 -ylamino) ethyl]-l-tyrosine derivatives and related compounds as a5b1 antagonists for the treatment of solid tumors
EP1878730A1 (en) 2006-07-12 2008-01-16 Bayer Schering Pharma Aktiengesellschaft Substituted isoxazolines, pharmaceutical compositions containing the same, methods of preparing the same, and uses of the same
CN101589028B (zh) * 2006-11-22 2014-02-19 味之素株式会社 具有喹唑啉二酮骨架的苯丙氨酸衍生物的制备方法及制备中间体
WO2008064823A1 (en) * 2006-11-27 2008-06-05 Ucb Pharma, S.A. Bicyclic and heterobicyclic derivatives, processes for preparing them and their uses
WO2008112939A2 (en) 2007-03-13 2008-09-18 Board Of Regents, The University Of Texas System Composition and method for making oligo-benzamide compounds
EP2155720B1 (en) 2007-06-08 2013-07-17 Advinus Therapeutics Private Limited Pyrrole-2-carboxamide derivatives as glucokinase activators, their process and pharmaceutical application
EP2205085A1 (en) * 2007-09-25 2010-07-14 Merck Sharp & Dohme Corp. 2-aryl or heteroaryl indole derivatives
EP2853529A1 (en) * 2010-03-29 2015-04-01 Ajinomoto Co., Inc. Crystals of salts of phenylalanine derivatives
US8501982B2 (en) 2010-06-09 2013-08-06 Receptos, Inc. GLP-1 receptor stabilizers and modulators
JP6007417B2 (ja) 2011-05-31 2016-10-12 レセプトス エルエルシー 新規ｇｌｐ−１受容体安定剤および調節剤
US8999975B2 (en) * 2011-09-19 2015-04-07 Boehringer Ingelheim International Gmbh Substituted N- [1-cyano-2- (phenyl) ethyl] -2-azabicyclo [2.2.1] heptane-3-carboxamide inhibitors of cathepsin C
CN109867630A (zh) 2013-06-11 2019-06-11 赛尔基因第二国际有限公司 新型glp-1受体调节剂
EP3172199B1 (en) 2014-07-25 2020-07-01 Celgene International II Sarl Pyrimidine derivatives as glp-1 receptor modulators

Patent Citations (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995012611A1 (en) * 1993-11-01 1995-05-11 Japat Ltd. Endothelin receptor antagonists
CN1119340C (zh) * 1997-07-31 2003-08-27 伊兰药品公司 抑制vla－4介导的白细胞粘着的氨基甲酰氧基化合物
CN1281430A (zh) * 1997-08-22 2001-01-24 霍夫曼-拉罗奇有限公司 芳酰基苯丙氨酸衍生物
JPH11189586A (ja) * 1997-12-25 1999-07-13 Kirin Brewery Co Ltd キノリン誘導体、イソキノリン誘導体、およびシンノリン誘導体、並びに抗炎症剤および抗アレルギー剤
CN1288457A (zh) * 1998-01-20 2001-03-21 田边制药株式会社 α4介导的细胞粘着的抑制剂
US20030149083A1 (en) * 1999-11-18 2003-08-07 Ajinomoto Co. Inc Phenylalanine derivatives
WO2003070709A1 (en) * 2002-02-20 2003-08-28 Ajinomoto Co.,Inc. Novel phenylalanine derivative
EP1700850A1 (en) * 2003-12-22 2006-09-13 Ajinomoto Co., Inc. Novel phenylalanine derivative
CN1938283A (zh) * 2004-02-10 2007-03-28 詹森药业有限公司 作为α4整联蛋白拮抗剂的哒嗪酮
CN1918118A (zh) * 2004-02-17 2007-02-21 石原产业株式会社 硫代酰胺类化合物或其盐、以及包含它们的细胞因子产生抑制剂
CN101360711A (zh) * 2005-11-23 2009-02-04 阿斯利康(瑞典)有限公司 L-苯丙氨酸衍生物及其作为整联蛋白拮抗剂的用途
WO2011094890A1 (en) * 2010-02-02 2011-08-11 Argusina Inc. Phenylalanine derivatives and their use as non-peptide glp-1 receptor modulators
CN104080767A (zh) * 2011-12-12 2014-10-01 瑞塞普托斯公司 新的glp-1受体调节剂

Non-Patent Citations (3)

* Cited by examiner, † Cited by third party
Title
徐斯盛等: "新型抗糖尿病药物的研究进展", 《中国药科大学学报》 *
易凡等: "GLP-1生物学及基于GLP-1的抗糖尿病药物研究(英文)", 《JOURNAL OF CHINESE PHARMACEUTICAL SCIENCES》 *
赵琳琳等: "胰高血糖素样肽-1类似物药物的研究进展", 《中国现代应用药学》 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US12234236B1 (en) 2023-09-14 2025-02-25 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

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