CN113874019A - 用于治疗nash/nafld及相关疾病的包含作为glp-1r激动剂的苯并二氧杂环戊烯的组合 - Google Patents

用于治疗nash/nafld及相关疾病的包含作为glp-1r激动剂的苯并二氧杂环戊烯的组合 Download PDF

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CN113874019A
CN113874019A CN202080037376.3A CN202080037376A CN113874019A CN 113874019 A CN113874019 A CN 113874019A CN 202080037376 A CN202080037376 A CN 202080037376A CN 113874019 A CN113874019 A CN 113874019A
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China
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methyl
piperidin
carboxylic acid
benzodioxol
benzimidazole
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Pending
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CN202080037376.3A
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Chinese (zh)
Inventor
G·E·阿斯普内斯
S·W·巴格利
J·M·柯托
M·道林
D·J·埃德蒙斯
D·费尔南多
M·E·弗拉纳根
二木建太郎
D·A·格里菲斯
K·瓦尔
G·英格尔
W·焦
S·M·拉卡斯
Y·连
C·利伯拉基斯
A·T·隆德雷甘
A·M·马蒂奥韦茨
D·W·彼得罗夫斯基
R·B·鲁格里
K·维格尔斯沃斯
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Pfizer Corp SRL
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Pfizer Corp SRL
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
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CN202080037376.3A 2019-05-20 2020-05-15 用于治疗nash/nafld及相关疾病的包含作为glp-1r激动剂的苯并二氧杂环戊烯的组合 Pending CN113874019A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962850133P 2019-05-20 2019-05-20
US62/850,133 2019-05-20
PCT/IB2020/054637 WO2020234726A1 (en) 2019-05-20 2020-05-15 Combinations comprising benzodioxol as glp-1r agonists for use in the treatment of nash/nafld and related diseases

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CN113874019A true CN113874019A (zh) 2021-12-31

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US (1) US20220387402A1 (enExample)
EP (2) EP4578460A3 (enExample)
JP (1) JP7672201B2 (enExample)
CN (1) CN113874019A (enExample)
AR (1) AR118965A1 (enExample)
CA (1) CA3140972C (enExample)
ES (1) ES3039586T3 (enExample)
TW (1) TW202110446A (enExample)
WO (1) WO2020234726A1 (enExample)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114728955A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728954A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
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

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11951140B2 (en) 2011-02-04 2024-04-09 Seed Health, Inc. Modulation of an individual's gut microbiome to address osteoporosis and bone disease
US12279989B2 (en) 2011-02-04 2025-04-22 Seed Health, Inc. Method and system for increasing beneficial bacteria and decreasing pathogenic bacteria in the oral cavity
US11998479B2 (en) 2011-02-04 2024-06-04 Seed Health, Inc. Method and system for addressing adverse effects on the oral microbiome and restoring gingival health caused by sodium lauryl sulphate exposure
US12257272B2 (en) 2015-12-24 2025-03-25 Seed Health, Inc. Method and system for reducing the likelihood of developing depression in an individual
US11969445B2 (en) 2013-12-20 2024-04-30 Seed Health, Inc. Probiotic composition and method for controlling excess weight, obesity, NAFLD and NASH
US12005085B2 (en) 2013-12-20 2024-06-11 Seed Health, Inc. Probiotic method and composition for maintaining a healthy vaginal microbiome
US11980643B2 (en) 2013-12-20 2024-05-14 Seed Health, Inc. Method and system to modify an individual's gut-brain axis to provide neurocognitive protection
US12246043B2 (en) 2013-12-20 2025-03-11 Seed Health, Inc. Topical application to treat acne vulgaris
US11998574B2 (en) 2013-12-20 2024-06-04 Seed Health, Inc. Method and system for modulating an individual's skin microbiome
US12329783B2 (en) 2013-12-20 2025-06-17 Seed Health, Inc. Method and system to improve the health of a person's skin microbiome
US10934279B2 (en) * 2018-06-13 2021-03-02 Pfizer Inc. GLP-1 receptor agonists and uses thereof
TWI809334B (zh) * 2019-12-10 2023-07-21 美商輝瑞股份有限公司 ２－（（４－（（Ｓ）－２－（５－氯吡啶－２－基）－２－甲基苯并〔ｄ〕〔１，３〕二氧呃－４－基）哌啶－１－基）甲基）－１－（（（Ｓ）－氧呾－２－基）甲基）－１Ｈ－苯并〔ｄ〕咪唑－６－羧酸１，３－二羥基－２－（羥基甲基）丙烷－２－胺鹽之固體形式
FI4097099T3 (fi) 2020-02-07 2024-07-30 Gasherbrum Bio Inc Heterosyklisiä glp-1-agonisteja
GB202001856D0 (en) * 2020-02-11 2020-03-25 Inorbit Therapeutics Ab Compounds useful in inhibiting ketohexokinase and methods of making and using the same
JP2021134211A (ja) * 2020-02-24 2021-09-13 ファイザー・インク Ｎａｆｌｄ／ｎａｓｈおよび関連疾患の処置のための組合せ
JP2022058085A (ja) * 2020-02-24 2022-04-11 ファイザー・インク ジアシルグリセロールアシルトランスフェラーゼ２阻害剤とアセチル－ＣｏＡカルボキシラーゼ阻害剤との組合せ
CR20230066A (es) 2020-08-06 2023-05-29 Gasherbrum Bio Inc Agonistas del glp-1 heterocíclicos
JP2023538949A (ja) * 2020-08-28 2023-09-12 ガシャーブラム・バイオ・インコーポレイテッド ヘテロ環ｇｌｐ－１アゴニスト
US20230089073A1 (en) 2021-01-28 2023-03-23 Carmot Therapeutics, Inc. Gpcr receptor agonists, pharmaceutical compositions comprising the same, and methods for their use
CN117222631A (zh) * 2021-03-24 2023-12-12 诚益生物(美国)公司 苯基-[1,3]二氧杂环戊烯并[4,5-c]吡啶基-苯基-、苯基-[1,3]二氧杂环戊烯并[4,5-c]吡啶基-杂芳基-或苯基-[1,3]二氧杂环戊烯并[4,5-c]吡啶基-哌啶基-甲基-氧杂环丁烷基甲基-1h-苯并[d]咪唑-甲酸衍生物及其使用方法
WO2022219495A1 (en) * 2021-04-12 2022-10-20 Novartis Ag 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
CA3215916A1 (en) * 2021-04-12 2022-10-20 Novartis Ag 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
JP2024516291A (ja) * 2021-05-03 2024-04-12 カーモット セラピューティクス インコーポレイテッド ベンゾイミダゾイルｇｌｐ－１受容体アゴニスト、それを含む医薬組成物、及びそれらの使用方法
WO2023025201A1 (zh) * 2021-08-24 2023-03-02 南京明德新药研发有限公司 咪唑并环类化合物及其应用
KR20240054335A (ko) * 2021-08-31 2024-04-25 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,1,3-디히드록시-2-(히드록시메틸)프로판-2-아민 염의 고체 형태
CN118948849A (zh) 2021-09-08 2024-11-15 盐野义制药株式会社 用于预防和治疗与抗肥胖作用有关的疾病的药物
US20250115612A1 (en) 2021-10-05 2025-04-10 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes and octahydrofuro[3,4-b]pyrazines as glp-1 receptor modulators
US20240417393A1 (en) 2021-10-05 2024-12-19 Astrazeneca Ab Certain 2,5-diazabicyclo[4.2.0]octanes 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
US20250066338A1 (en) 2021-12-16 2025-02-27 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
US20250042882A1 (en) 2021-12-16 2025-02-06 Astrazeneca Ab Certain 3-azabicyclo[3.1.0]hexanes as glp-1 receptor modulators
EP4476212A1 (en) * 2022-02-10 2024-12-18 Novartis AG 2-((4-((s)-2-(4-chloro-2-fluorophenyl)-2-methylbenzo[d][1,3]dioxol-4-yl)piperidin-1-yl)methyl)-1-(((s)-oxetan-2-yl)methyl)-1h-imidazole derivatives as activators of the glp1 receptor for the treatment of obesity
EP4490155A1 (en) 2022-03-09 2025-01-15 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
EP4508047A1 (en) 2022-04-14 2025-02-19 Gasherbrum Bio, Inc. Heterocyclic glp-1 agonists
WO2024125602A1 (en) 2022-12-15 2024-06-20 Gasherbrum Bio, Inc. Salts and solid forms of a compound having glp-1 agonist activity
WO2024228213A1 (en) * 2023-05-03 2024-11-07 Dr. Reddy's Laboratories Limited Crystalline forms of danuglipron
WO2025057134A2 (en) 2023-09-14 2025-03-20 Ascletis Pharma (China) Co., Limited Glp-1r agonist and therapeutic method thereof
WO2025080818A1 (en) * 2023-10-10 2025-04-17 Sagimet Biosciences Inc. Combinations of fasn inhibitors and glp-1 agonists for liver diseases
US12291530B1 (en) 2023-11-24 2025-05-06 Ascletis Pharma (China) Co., Limited GLP-1R agonist and therapeutic method thereof

Citations (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4465850A (en) * 1980-09-02 1984-08-14 Merck & Co., Inc. Treatment of brain injury due to gray matter edema with (indanyloxy) butanoic acids
WO2012042433A1 (en) * 2010-09-30 2012-04-05 Pfizer Inc. N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS
US20130331349A1 (en) * 2010-12-20 2013-12-12 Irm Llc Compositions and methods for modulating fxr
US20170183328A1 (en) * 2015-12-29 2017-06-29 Pfizer Inc. Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
US20180051012A1 (en) * 2016-08-19 2018-02-22 Pfizer Inc. Diacylglycerol acyl transferase 2 inhibitors
WO2018109607A1 (en) * 2016-12-16 2018-06-21 Pfizer Inc. Glp-1 receptor agonists and uses thereof
WO2019102311A1 (en) * 2017-11-21 2019-05-31 Pfizer Inc. Crystalline 2-amino-2-(hydroxymethyl)propane-1,3-diol salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid
CN112533674A (zh) * 2018-06-13 2021-03-19 辉瑞公司 Glp-1受体激动剂及其用途

Family Cites Families (40)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA1146866A (en) 1979-07-05 1983-05-24 Yamanouchi Pharmaceutical Co. Ltd. Process for the production of sustained release pharmaceutical composition of solid medical material
DE3065190D1 (en) 1979-11-05 1983-11-10 Beecham Group Plc Enzyme derivatives, and their preparation
DE3438830A1 (de) 1984-10-23 1986-04-30 Rentschler Arzneimittel Nifedipin enthaltende darreichungsform und verfahren zu ihrer herstellung
JP2527107B2 (ja) 1991-04-16 1996-08-21 日本新薬株式会社 固体分散体の製造方法
US5340591A (en) 1992-01-24 1994-08-23 Fujisawa Pharmaceutical Co., Ltd. Method of producing a solid dispersion of the sparingly water-soluble drug, nilvadipine
JP3265680B2 (ja) 1992-03-12 2002-03-11 大正製薬株式会社 経口製剤用組成物
US5612359A (en) 1994-08-26 1997-03-18 Bristol-Myers Squibb Company Substituted biphenyl isoxazole sulfonamides
DE19504832A1 (de) 1995-02-14 1996-08-22 Basf Ag Feste Wirkstoff-Zubereitungen
TW536540B (en) 1997-01-30 2003-06-11 Bristol Myers Squibb Co Endothelin antagonists: N-[[2'-[[(4,5-dimethyl-3-isoxazolyl)amino]sulfonyl]-4-(2-oxazolyl)[1,1'-biphenyl]-2-yl]methyl]-N,3,3-trimethylbutanamide and N-(4,5-dimethyl-3-isoxazolyl)-2'-[(3,3-dimethyl-2-oxo-1-pyrrolidinyl)methyl]-4'-(2-oxazolyl)[1,1'-biphe
ATE364374T1 (de) 1997-08-11 2007-07-15 Pfizer Prod Inc Feste pharmazeutische dispersionen mit erhöhter bioverfügbarkeit
IL140622A0 (en) 1998-07-06 2002-02-10 Bristol Myers Squibb Co Biphenyl sufonamide derivatives, pharmaceutical compositions containing the same and methods for the preparation thereof
US6488375B2 (en) 1999-10-28 2002-12-03 Ocular Sciences, Inc. Tinted contact lens and method for making same
MY125533A (en) 1999-12-06 2006-08-30 Bristol Myers Squibb Co Heterocyclic dihydropyrimidine compounds
CA2439152C (en) 2001-02-28 2008-06-17 Merck & Co., Inc. Acylated piperidine derivatives as melanocortin-4 receptor agonists
NZ534582A (en) 2002-02-27 2006-03-31 Pfizer Prod Inc ACC inhibitors
US20040127504A1 (en) * 2002-09-06 2004-07-01 Cowart Marlon D. Benzimidazoles that are useful in treating sexual dysfunction
PT1753748E (pt) 2004-05-12 2009-08-28 Pfizer Prod Inc Derivados de prolina e a sua utilização como inibidores de dipeptidil peptidase iv
CA2568056A1 (en) 2004-05-25 2005-12-08 Pfizer Products Inc. Tetraazabenzo[e]azulene derivatives and analogs thereof
PA8660701A1 (es) 2005-02-04 2006-09-22 Pfizer Prod Inc Agonistas de pyy y sus usos
ES2487967T3 (es) 2006-04-20 2014-08-25 Pfizer Products Inc. Compuestos amido heterocíclicos condensados con fenilo para la prevención y el tratamiento de enfermedades mediadas por la glucoquinasa
CN101541809A (zh) 2006-11-29 2009-09-23 辉瑞产品公司 螺环酮乙酰基-CoA羧化酶抑制剂
US20090036425A1 (en) 2007-08-02 2009-02-05 Pfizer Inc Substituted bicyclolactam compounds
CA2724603A1 (en) 2008-05-28 2009-12-03 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
CA2724774C (en) 2008-05-28 2013-06-25 Pfizer Inc. Pyrazolospiroketone acetyl-coa carboxylase inhibitors
EP2318370A1 (en) 2008-07-29 2011-05-11 Pfizer Inc. Fluorinated heteroaryls
CN102149717B (zh) 2008-08-28 2014-05-14 辉瑞大药厂 二氧杂-双环[3.2.1]辛烷-2，3，4-三醇衍生物
TW201038580A (en) 2009-02-02 2010-11-01 Pfizer 4-amino-5-oxo-7,8-dihydropyrimido[5,4-f][1,4]oxazepin-6(5H)-yl)phenyl derivatives
WO2010103438A1 (en) 2009-03-11 2010-09-16 Pfizer Inc. Substituted indazole amides and their use as glucokinase activators
AU2010222589B2 (en) 2009-03-11 2012-08-16 Pfizer Inc. Benzofuranyl derivatives used as glucokinase inhibitors
JP2012520868A (ja) 2009-03-20 2012-09-10 ファイザー・インク ３−オキサ−７−アザビシクロ［３．３．１］ノナン
CN102378574B (zh) * 2009-03-30 2013-11-20 转化技术制药公司 取代的偶氮蒽衍生物、药物组合物及其使用方法
JP2012526096A (ja) 2009-05-08 2012-10-25 ファイザー・インク Ｇｐｒ１１９調節因子
WO2010128425A1 (en) 2009-05-08 2010-11-11 Pfizer Inc. Gpr 119 modulators
JP2012528847A (ja) 2009-06-05 2012-11-15 ファイザー・インク Ｇｐｒ１１９調節因子としてのｌ−（ピペリジン−４−イル）−ピラゾール誘導体
WO2011005611A1 (en) 2009-07-09 2011-01-13 Merck Sharp & Dohme Corp. Neuromedin u receptor agonists and uses thereof
CH702192A1 (de) 2009-11-04 2011-05-13 New Dent Ag Keramisches Implantat.
SG185515A1 (en) * 2010-05-13 2012-12-28 Amgen Inc Nitrogen heterocyclic compounds useful as pde10 inhibitors
JOP20190060A1 (ar) * 2016-09-26 2019-03-26 Chugai Pharmaceutical Co Ltd مشتق بيرازولو بيريدين له تأثير مساعد لمستقبل glp-1
CN106271089B (zh) 2016-09-30 2019-01-25 英诺激光科技股份有限公司 一种激光薄膜刻蚀装置及方法
JP7348179B2 (ja) 2018-07-05 2023-09-20 株式会社Ｎｔｔドコモ 端末、無線通信方法、基地局及びシステム

Patent Citations (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4465850A (en) * 1980-09-02 1984-08-14 Merck & Co., Inc. Treatment of brain injury due to gray matter edema with (indanyloxy) butanoic acids
WO2012042433A1 (en) * 2010-09-30 2012-04-05 Pfizer Inc. N1-PYRAZOLOSPIROKETONE ACETYL-CoA CARBOXYLASE INHIBITORS
US20130331349A1 (en) * 2010-12-20 2013-12-12 Irm Llc Compositions and methods for modulating fxr
US20170183328A1 (en) * 2015-12-29 2017-06-29 Pfizer Inc. Substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors
US20180051012A1 (en) * 2016-08-19 2018-02-22 Pfizer Inc. Diacylglycerol acyl transferase 2 inhibitors
WO2018109607A1 (en) * 2016-12-16 2018-06-21 Pfizer Inc. Glp-1 receptor agonists and uses thereof
US20180170908A1 (en) * 2016-12-16 2018-06-21 Pfizer Inc. GLP-1 Agonists and Uses Thereof
WO2019102311A1 (en) * 2017-11-21 2019-05-31 Pfizer Inc. Crystalline 2-amino-2-(hydroxymethyl)propane-1,3-diol salt of 4-(4-(1-isopropyl-7-oxo-1,4,6,7-tetrahydrospiro[indazole-5,4'-piperidine]-1'-carbonyl)-6-methoxypyridin-2-yl)benzoic acid
CN112533674A (zh) * 2018-06-13 2021-03-19 辉瑞公司 Glp-1受体激动剂及其用途

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114728955A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728954A (zh) * 2019-11-29 2022-07-08 广东东阳光药业有限公司 Tropifexor的新晶型及其制备方法
CN114728954B (zh) * 2019-11-29 2023-10-17 广东东阳光药业股份有限公司 Tropifexor的新晶型及其制备方法
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

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