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PE20221040A1 - Compuestos moduladores de glp-1r - Google Patents

Compuestos moduladores de glp-1r

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Publication number
PE20221040A1
PE20221040A1 PE2022000662A PE2022000662A PE20221040A1 PE 20221040 A1 PE20221040 A1 PE 20221040A1 PE 2022000662 A PE2022000662 A PE 2022000662A PE 2022000662 A PE2022000662 A PE 2022000662A PE 20221040 A1 PE20221040 A1 PE 20221040A1
Authority
PE
Peru
Prior art keywords
alkyl
glp
fluorobenzyl
methoxyethyl
benzo
Prior art date
Application number
PE2022000662A
Other languages
English (en)
Inventor
Stephen E Ammann
Gediminas J Brizgys
James S Cassidy
Elbert Chin
Chienhung Chou
Jeromy J Cottell
Michael Graupe
Chao-I Hung
Kavoos Kolahdouzan
Scott D Schroeder
Nathan D Shapiro
Daniel G Shore
Suzanne M Szewczyk
James G Taylor
Rhiannon Thomas-Tran
Nathan E Wright
Zheng-Yu Yang
Sheila M Zipfel
Original Assignee
Gilead Sciences Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Gilead Sciences Inc filed Critical Gilead Sciences Inc
Publication of PE20221040A1 publication Critical patent/PE20221040A1/es

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    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • A61K31/33—Heterocyclic compounds
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

Esta referido a un compuesto de Formula I-A-I, en donde: Anillo A y Anillo B son arilo o heteroarilo, opcionalmente sustituidos; R1 es alquilo, alquenilo, alquinilo, entre otros; R2 es H, alquilo, haloalquilo, cicloalquilo, entre otros; R3 es H, alquilo, arilo, CN, entre otros; R5a y R5b son H, alquilo, haloalquilo, alcoxialquilo, halogeno, entre otros; X1, X2, X3 son -N=, -C(H)=, -C(R8)=; V es -C(O)-, -O-, -N(R6a)-, -C(R6b)(R6c)-; Y es -N(R7)-, -O-, -S-, -S(O)-, -S(O)2-, -S(O)(=NH)-, o -S(O)(=NR7)-. Entre los compuestos preferidos tenemos los siguientes: acido 2-(4-(6-((4-ciano-2-fluorobencil)oxi)piridin-2-il)bencil)-1-(2-metoxietil)- 1H-benzo[d]imidazol-6-carboxilico; acido 2-((3'-((4-ciano-2-fluorobencil)oxi)-3-fluoro-[1,1'-bifenil]-4-il)metil)-1- (2-metoxietil)-1H-benzo[d]imidazol-6-carboxilico; entre otros. Estos compuestos actuan como agonistas o moduladores del receptor del peptido 1 similar al glucagon (GLP-1R) y se emplean en el tratamiento de enfermedades metabolicas y enfermedades relacionadas, como esteatohepatitis no alcoholica (NASH), obesidad y diabetes tipo 2.
PE2022000662A 2019-10-25 2020-10-22 Compuestos moduladores de glp-1r PE20221040A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962926270P 2019-10-25 2019-10-25
US202063028187P 2020-05-21 2020-05-21
PCT/US2020/056867 WO2021081207A1 (en) 2019-10-25 2020-10-22 Glp-1r modulating compounds

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PE20221040A1 true PE20221040A1 (es) 2022-06-17

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US (2) US11702404B2 (es)
EP (1) EP4048664A1 (es)
JP (2) JP7558267B2 (es)
KR (1) KR20220092909A (es)
CN (1) CN114630823B (es)
AU (2) AU2020369568B2 (es)
BR (1) BR112022007627A2 (es)
CA (1) CA3157525A1 (es)
CL (1) CL2022001030A1 (es)
CO (1) CO2022005077A2 (es)
CR (1) CR20220178A (es)
DO (1) DOP2022000087A (es)
IL (1) IL292399A (es)
MX (1) MX2022004874A (es)
PE (1) PE20221040A1 (es)
PH (1) PH12022550932A1 (es)
TW (2) TWI790492B (es)
WO (1) WO2021081207A1 (es)

Families Citing this family (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP3860998B1 (en) 2018-10-05 2023-12-27 Annapurna Bio Inc. Compounds and compositions for treating conditions associated with apj receptor activity
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
PH12021552557A1 (en) * 2019-04-12 2022-07-04 Qilu Regor Therapeutics Inc Glp-1r agonists and uses thereof
TWI751585B (zh) * 2019-06-28 2022-01-01 美商美國禮來大藥廠 類升糖素肽1受體促效劑
PE20221040A1 (es) 2019-10-25 2022-06-17 Gilead Sciences Inc Compuestos moduladores de glp-1r
PE20221422A1 (es) * 2019-11-15 2022-09-20 Ildong Pharmaceutical Co Ltd Agonista del receptor glp-1 y uso de este
KR20210059584A (ko) * 2019-11-15 2021-05-25 일동제약(주) Glp-1 수용체 작용제 및 이의 용도
WO2021112538A1 (en) 2019-12-02 2021-06-10 Hyundai Pharm Co., Ltd. Glp-1 receptor agonist
US12121511B2 (en) 2020-01-29 2024-10-22 Gilead Sciences, Inc. GLP-1R modulating compounds
ES2986788T3 (es) 2020-02-07 2024-11-12 Gasherbrum Bio Inc Agonistas heterocíclicos de GLP-1
CN115279750B (zh) * 2020-03-18 2024-06-21 株式会社Lg化学 Glp-1受体激动剂、包含该激动剂的药物组合物及其制备方法
CA3171173A1 (en) * 2020-03-18 2021-09-23 Young Kwan Kim Glp-1 receptor agonist, pharmaceutical composition comprising same, and method for preparing same
IL300155A (en) 2020-08-06 2023-03-01 Gasherbrum Bio Inc Heterocyclic GLP-1 agonists
WO2022031994A1 (en) * 2020-08-06 2022-02-10 Qilu Regor Therapeutics Inc. Glp-1r agonists and uses thereof
CN116406360A (zh) 2020-08-28 2023-07-07 加舒布鲁姆生物公司 杂环glp-1激动剂
EP4225742A4 (en) 2020-10-05 2024-11-06 Enliven Inc. 5- 6-AZAINDOL COMPOUNDS FOR INHIBITING BCR-ABL TYROSINE KINASES
EP4227299A1 (en) * 2020-10-12 2023-08-16 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Benzimidazolone glp-1 receptor agonist and use thereof
EP4229050A4 (en) * 2020-10-13 2024-12-11 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
CN114478497B (zh) * 2020-11-12 2023-10-20 杭州中美华东制药有限公司 芳基烷基酸类glp-1受体激动剂及其用途
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
US20240246959A1 (en) * 2020-11-27 2024-07-25 Shenzhen Salubris Pharmaceuticals Co., Ltd. Benzimidazole derivative and preparation method therefor and medical use thereof
CN114591308B (zh) * 2020-12-03 2024-03-08 苏州闻泰医药科技有限公司 一类glp-1r受体激动剂化合物及其用途
EP4304711A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
EP4304712A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
US20240208952A1 (en) * 2021-03-22 2024-06-27 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Thiophene glp-1 receptor agonist and use thereof
JPWO2022202864A1 (es) 2021-03-24 2022-09-29
KR20220140429A (ko) * 2021-04-08 2022-10-18 주식회사 엘지화학 Glp-1 수용체 효능제, 이를 포함하는 약학적 조성물 및 이의 제조방법
EP4271672A1 (en) 2021-04-21 2023-11-08 Gilead Sciences, Inc. Carboxy-benzimidazole glp-1r modulating compounds
EP4271674B1 (en) 2021-04-21 2025-02-12 Gilead Sciences, Inc. Carboxy-benzimidazole glp-1r modulating compounds
TWI843104B (zh) 2021-05-20 2024-05-21 美商美國禮來大藥廠 類升糖素肽1受體促效劑
EP4361145A1 (en) 2021-06-24 2024-05-01 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Glp-1 receptor agonist and composition and use thereof
CN113480534B (zh) * 2021-07-23 2022-05-13 广州必贝特医药股份有限公司 苯并咪唑或氮杂苯并咪唑-6-羧酸类化合物及其应用
US20240360109A1 (en) * 2021-08-04 2024-10-31 Shanghai Hansoh Biomedical Co., Ltd. Cycloalkene derivative regulator, preparation method therefor, and application thereof
CN115703766A (zh) * 2021-08-10 2023-02-17 天地恒一制药股份有限公司 Glp-1受体激动剂及其用途
CN117242067B (zh) * 2021-08-30 2025-03-25 杭州德睿智药科技有限公司 作为glp1r激动剂的新型芳醚取代杂环类化合物
EP4400105A1 (en) 2021-09-08 2024-07-17 Shionogi & Co., Ltd Medicine for prevention and treatment of diseases linked to anti-obesity activity
AU2022349020A1 (en) * 2021-09-27 2024-05-09 Terns Pharmaceuticals, Inc. Benzimidazole carboxylic acids as glp-1r agonists
EP4412707A1 (en) 2021-10-05 2024-08-14 Astrazeneca AB Certain 2,5-diazabicyclo[4.2.0]octanes as glp-1 receptor modulators
WO2023057429A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
WO2023057414A1 (en) 2021-10-05 2023-04-13 Astrazeneca Ab Certain octahydrofuro[3,4- b]pyrazines as glp-1 receptor modulators
TWI843243B (zh) * 2021-10-22 2024-05-21 大陸商盛世泰科生物醫藥技術（蘇州）股份有限公司 作為glp-1受體激動劑的化合物、包含其的藥物組成物及其用途
IL312364A (en) 2021-10-25 2024-06-01 Luehr Gary W Compounds as GLP-1R agonists
WO2023111145A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
WO2023111144A1 (en) 2021-12-16 2023-06-22 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
JP2025504508A (ja) * 2022-01-24 2025-02-12 ガシャーブラム・バイオ・インコーポレイテッド ヘテロ環式ｇｌｐ－１アゴニスト
KR20240148000A (ko) * 2022-02-28 2024-10-10 애슬레티스 바이오사이언스 코., 엘티디. Glp-1r 조절 화합물
US20230271949A1 (en) * 2022-02-28 2023-08-31 Ascletis Bioscience Co., Ltd. Glp-1r modulating compounds
JP2025508097A (ja) 2022-03-08 2025-03-21 広州市聯瑞制葯有限公司 ベンゾビシクロ系化合物及びその製造方法と応用
EP4467538A1 (en) * 2022-05-20 2024-11-27 Chengdu Di'Ao Jiuhong Pharmaceutical Factory Benzimidazole or azabenzimidazole compound, preparation method therefor and use thereof
WO2024028795A1 (en) * 2022-08-04 2024-02-08 Zydus Lifesciences Limited Heterobicyclic compounds as oral glp1r agonists
WO2024041609A1 (zh) * 2022-08-24 2024-02-29 广州市联瑞制药有限公司 苯并双环类化合物及其制备方法和应用
WO2024046342A1 (zh) * 2022-08-30 2024-03-07 广州市联瑞制药有限公司 苯并双环类化合物及其制备方法和应用
WO2024051749A1 (zh) * 2022-09-06 2024-03-14 德睿智药(苏州)新药研发有限公司 一种glp-1r激动剂化合物的多晶型物及其制备方法与用途
WO2024063143A1 (ja) 2022-09-22 2024-03-28 塩野義製薬株式会社 Ｇｌｐ－１受容体アゴニスト作用を有する縮合環化合物
WO2024102625A1 (en) 2022-11-11 2024-05-16 Eli Lilly And Company Glucagon-like peptide 1 receptor agonists
WO2024107781A1 (en) 2022-11-16 2024-05-23 Eli Lilly And Company Glucagon-like peptide 1 receptor agonists
CN118184637A (zh) * 2022-12-13 2024-06-14 杭州中美华东制药有限公司 Glp-1受体激动剂的新晶型和制备方法及其药物组合物和用途
CN118496200A (zh) * 2023-02-14 2024-08-16 成都康弘药业集团股份有限公司 吲唑啉酮类化合物及其制备方法和用途
US20240360122A1 (en) * 2023-03-29 2024-10-31 Terns (Suzhou) Biotechnology Co., Ltd. Polymorphic forms and salts of a glp-1r agonist
WO2024206878A1 (en) * 2023-03-29 2024-10-03 Terns Pharmaceuticals, Inc. Compounds as glp-1r agonists
WO2024212742A1 (zh) * 2023-04-10 2024-10-17 上海研健新药研发有限公司 一种glp-1r激动剂，其制备方法和应用
WO2024263537A1 (en) * 2023-06-23 2024-12-26 Merck Sharp & Dohme Llc Use of a long-acting oxyntomodulin derivative for treament of fatty liver disease
CN119330949A (zh) * 2023-07-21 2025-01-21 石药集团中奇制药技术（石家庄）有限公司 一类多环化合物及其用途
US12234236B1 (en) 2023-09-14 2025-02-25 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Family Cites Families (60)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2261844T3 (es) 1998-08-07 2006-11-16 Applied Research Systems Ars Holding N.V. Mimeticos de la fsh para el tratamiento de la infertilidad.
EP1429759A4 (en) 2001-09-26 2004-12-15 Bristol Myers Squibb Co COMPOUNDS FOR TREATING HEPATITIS C VIRUS
WO2004099192A2 (en) 2003-04-30 2004-11-18 The Institutes Of Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids as inhibitors of protein tyrosine phosphatase-1b
WO2005014543A1 (ja) 2003-08-06 2005-02-17 Japan Tobacco Inc. 縮合環化合物及びそのｈｃｖポリメラーゼ阻害剤としての利用
US20060122222A1 (en) 2004-11-18 2006-06-08 The Institutes For Pharmaceutical Discovery, Llc Heterocycle substituted carboxylic acids
KR20070092297A (ko) 2004-12-21 2007-09-12 데브젠 엔브이 Ｋｖ4 이온 채널 활성을 갖는 화합물
PL1940786T3 (pl) 2005-09-16 2010-12-31 Arrow Therapeutics Ltd Pochodne bifenylowe i ich zastosowanie w leczeniu zapalenia wątroby typu C
JP2009532381A (ja) 2006-03-31 2009-09-10 アストラゼネカ アクチボラグ 二環式ベンズイミダゾール化合物、および代謝型グルタミン酸受容体増強剤としての該化合物の使用
WO2008033455A2 (en) 2006-09-13 2008-03-20 The Institutes For Pharmaceutical Discovery, Llc Biphenyl and heteroaryl phenyl derivatives as protein tyrosine phosphatases inhibitors
CA2736970A1 (en) 2008-09-12 2010-03-18 Biolipox Ab Pyrimidinone derivatives for use as medicaments
US20110294853A1 (en) 2008-09-12 2011-12-01 Benjamin Pelcman Bis Aromatic Compounds for Use in the Treatment of Inflammation
WO2010046780A2 (en) 2008-10-22 2010-04-29 Institut Pasteur Korea Anti viral compounds
US8563575B2 (en) * 2010-06-24 2013-10-22 Takeda Pharmaceutical Company Limited Fused heterocyclic compounds
JP2014525932A (ja) 2011-08-15 2014-10-02 インターミューン， インコーポレイテッド リゾホスファチド酸レセプターアンタゴニスト
CN103059014B (zh) * 2011-10-21 2016-05-18 北京韩美药品有限公司 新型杂芳基氨基衍生物
EA028626B1 (ru) 2012-06-11 2017-12-29 Юсб Байофарма Спрл БЕНЗИМИДАЗОЛЫ, МОДУЛИРУЮЩИЕ TNF-α
US10011585B2 (en) 2014-07-28 2018-07-03 Merck Sharp & Dohme Corp. Factor XIa inhibitors
KR20160066490A (ko) 2014-12-02 2016-06-10 주식회사 씨앤드씨신약연구소 헤테로사이클 유도체 및 그의 용도
JP6771469B2 (ja) 2015-01-20 2020-10-21 ベーリンガー インゲルハイム アニマル ヘルス ユーエスエイ インコーポレイテッド 駆虫性化合物、組成物及びこれらの使用方法
US20170035881A1 (en) * 2015-10-19 2017-02-09 Acerta Pharma B.V. Therapeutic Combinations of an IRAK4 Inhibitor and a BTK Inhibitor
BR112018068703B1 (pt) 2016-03-16 2024-02-06 Kura Oncology, Inc. Inibidores substituídos de menin-mll e métodos de uso
ES2877573T3 (es) * 2016-03-30 2021-11-17 Ishihara Sangyo Kaisha Compuesto de piridazinona o su sal, y herbicida que los contiene
UA122035C2 (uk) 2016-12-16 2020-08-25 Пфайзер Інк. Агоністи рецептора glp-1 та їх застосування
JP7249950B2 (ja) 2017-03-27 2023-03-31 カーデュリオン・ファーマシューティカルズ・リミテッド・ライアビリティ・カンパニー ヘテロ環化合物
US20200308165A1 (en) 2017-09-13 2020-10-01 D.E. Shaw Research, Llc Compounds as Ras Inhibitors and Use Thereof
MX2020008387A (es) 2018-05-08 2020-12-11 Vtv Therapeutics Llc Usos terapeuticos de agonistas glp1r.
US10934279B2 (en) 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
ES2943510T3 (es) 2018-06-15 2023-06-13 Pfizer Agonistas del receptor GLP-1 y usos del mismo
WO2020033413A2 (en) 2018-08-07 2020-02-13 Tosk, Inc. Modulators of ras gtpase
PE20211871A1 (es) * 2018-11-22 2021-09-21 Qilu Regor Therapeutics Inc Agonistas de glp-1r y usos de los mismos
US10954221B2 (en) 2019-04-12 2021-03-23 Qilu Regor Therapeutics Inc. GLP-1R agonists and uses thereof
PH12021552557A1 (en) 2019-04-12 2022-07-04 Qilu Regor Therapeutics Inc Glp-1r agonists and uses thereof
TWI751585B (zh) 2019-06-28 2022-01-01 美商美國禮來大藥廠 類升糖素肽1受體促效劑
CN112294760A (zh) 2019-07-26 2021-02-02 张晋宇 一种液体制剂及其应用
WO2021018023A1 (zh) 2019-08-01 2021-02-04 济南泰达领创医药技术有限公司 小分子glp-1受体调节剂
CN112409331B (zh) 2019-08-21 2024-02-20 上海翰森生物医药科技有限公司 杂环类衍生物抑制剂、其制备方法和应用
PE20221040A1 (es) 2019-10-25 2022-06-17 Gilead Sciences Inc Compuestos moduladores de glp-1r
KR20210053680A (ko) 2019-11-04 2021-05-12 주식회사 엘지화학 광변조 디바이스의 제조 방법
PE20221422A1 (es) 2019-11-15 2022-09-20 Ildong Pharmaceutical Co Ltd Agonista del receptor glp-1 y uso de este
WO2021112538A1 (en) 2019-12-02 2021-06-10 Hyundai Pharm Co., Ltd. Glp-1 receptor agonist
US12121511B2 (en) 2020-01-29 2024-10-22 Gilead Sciences, Inc. GLP-1R modulating compounds
ES2986788T3 (es) 2020-02-07 2024-11-12 Gasherbrum Bio Inc Agonistas heterocíclicos de GLP-1
CN115697999A (zh) 2020-02-13 2023-02-03 加舒布鲁姆生物公司 杂环glp-1激动剂
CA3171173A1 (en) 2020-03-18 2021-09-23 Young Kwan Kim Glp-1 receptor agonist, pharmaceutical composition comprising same, and method for preparing same
KR20220157486A (ko) 2020-03-27 2022-11-29 화이자 인코포레이티드 2-[(4-(6-[(4-시아노-2-플루오로벤질)옥시]피리딘-2-일)피페리딘-1-일)메틸]-1-[(2s)-옥세탄-2-일메틸]-1h-벤즈이미다졸-6-카르복실산 또는 그의 제약상 염을 사용한 제2형 당뇨병 또는 비만 또는 과체중의 치료
TW202144340A (zh) 2020-04-03 2021-12-01 大陸商江蘇恆瑞醫藥股份有限公司 稠合咪唑類衍生物、其製備方法及其在醫藥上的應用
CN113493447B (zh) 2020-04-03 2024-06-11 轩竹(北京)医药科技有限公司 Glp-1受体激动剂
HUE068535T2 (hu) 2020-05-27 2025-01-28 Qilu Regor Therapeutics Inc GLP-1R agonisták sója és kristályformái és azok felhasználásai
KR102588241B1 (ko) 2020-06-04 2023-10-11 항저우 사이윈드 바이오사이언시즈 컴퍼니 리미티드 5원 헤테로방향족 이미다졸 화합물 및 이의 용도
CN113816948B (zh) 2020-06-19 2023-08-11 江苏恒瑞医药股份有限公司 稠合咪唑类衍生物、其制备方法及其在医药上的应用
WO2022031994A1 (en) * 2020-08-06 2022-02-10 Qilu Regor Therapeutics Inc. Glp-1r agonists and uses thereof
MX2023002108A (es) 2020-08-21 2023-07-11 Terns Pharmaceuticals Inc Compuestos como agonistas de glp-1r.
WO2022068772A1 (zh) 2020-09-29 2022-04-07 深圳信立泰药业股份有限公司 一种苯并咪唑类衍生物及其制备方法和医药用途
EP4227299A1 (en) 2020-10-12 2023-08-16 Hangzhou Zhongmeihuadong Pharmaceutical Co., Ltd. Benzimidazolone glp-1 receptor agonist and use thereof
EP4247804A1 (en) 2020-11-20 2023-09-27 Gilead Sciences, Inc. Polyheterocyclic glp-1 r modulating compounds
US20240246959A1 (en) 2020-11-27 2024-07-25 Shenzhen Salubris Pharmaceuticals Co., Ltd. Benzimidazole derivative and preparation method therefor and medical use thereof
EP4304712A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
EP4304711A1 (en) 2021-03-11 2024-01-17 Gilead Sciences, Inc. Glp-1r modulating compounds
US20240300928A1 (en) * 2021-04-08 2024-09-12 Lg Chem, Ltd. Glp-1 receptor agonist, pharmaceutical composition comprising same, and method for preparing same
CN113480534B (zh) 2021-07-23 2022-05-13 广州必贝特医药股份有限公司 苯并咪唑或氮杂苯并咪唑-6-羧酸类化合物及其应用

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