MX386752B - Agonistas del receptor farnesoide x y usos de los mismos. - Google Patents

Agonistas del receptor farnesoide x y usos de los mismos.

Info

Publication number
MX386752B
MX386752B MX2018003388A MX2018003388A MX386752B MX 386752 B MX386752 B MX 386752B MX 2018003388 A MX2018003388 A MX 2018003388A MX 2018003388 A MX2018003388 A MX 2018003388A MX 386752 B MX386752 B MX 386752B
Authority
MX
Mexico
Prior art keywords
farnesoid
receptor agonists
compounds
methods
receptor
Prior art date
Application number
MX2018003388A
Other languages
English (en)
Other versions
MX2018003388A (es
Inventor
Johnny Y Nagasawa
Nicholas D Smith
Steven P Govek
Original Assignee
Metacrine 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 Metacrine Inc filed Critical Metacrine Inc
Publication of MX2018003388A publication Critical patent/MX2018003388A/es
Publication of MX386752B publication Critical patent/MX386752B/es

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    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
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    • C07C233/77—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/80—Carboxylic acid amides having carbon atoms of carboxamide groups bound to carbon atoms of six-membered aromatic rings having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
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    • A61K31/167—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
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Abstract

Se describen aquí compuestos que son agonistas del receptor farnesoide X, métodos para preparar tales compuestos, composiciones farmacéuticas y medicamentos que comprenden tales compuestos, y métodos para usar tales compuestos en el tratamiento de condiciones, enfermedades o trastornos asociados con la actividad del receptor farnesoide X.
MX2018003388A 2015-09-16 2016-09-16 Agonistas del receptor farnesoide x y usos de los mismos. MX386752B (es)

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Families Citing this family (37)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US10377717B2 (en) 2015-09-16 2019-08-13 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
WO2017049172A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
KR20180052678A (ko) 2015-09-16 2018-05-18 메타크린, 인크. 파네소이드 x 수용체 아고니스트 및 이의 용도
WO2018170165A1 (en) * 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN110637011B (zh) * 2017-03-15 2024-05-14 奥加诺沃公司 法尼醇x受体激动剂及其用途
AU2018236275B2 (en) * 2017-03-15 2022-05-12 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof
US20200131129A1 (en) * 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN110251498A (zh) * 2018-03-12 2019-09-20 厦门大学 一类调节法尼醇受体活性的化合物及其用途
WO2019089665A1 (en) 2017-11-01 2019-05-09 Bristol-Myers Squibb Company Alkene spirocyclic compounds as farnesoid x receptor modulators
EP3704107B1 (en) 2017-11-01 2023-04-12 Bristol-Myers Squibb Company Multicyclic compounds as farnesoid x receptor modulators
JP2021501785A (ja) 2017-11-02 2021-01-21 カリコ ライフ サイエンシーズ エルエルシー 統合的ストレス経路の調節剤
WO2020061114A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists for the treatment of disease
JP2022500395A (ja) * 2018-09-18 2022-01-04 メタクリン，インク． ファルネソイドｘ受容体アゴニストの結晶形態
HRP20251321T1 (hr) * 2018-09-18 2025-12-05 Eli Lilly And Company Agonisti farnezoid x receptora i njihova primjena
WO2020061118A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2020061117A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2020061116A1 (en) * 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN113056264A (zh) * 2018-09-18 2021-06-29 梅塔科林公司 法尼醇x受体激动剂及其用途
JP2022504697A (ja) * 2018-10-24 2022-01-13 メタクリン，インク． Ｓｓａｏ阻害剤とその使用
BR112021015930A2 (pt) 2019-02-15 2021-10-05 Bristol-Myers Squibb Company Compostos de amida substituídos úteis como moduladores de receptor farnesoide x
KR102905880B1 (ko) * 2019-02-15 2025-12-29 브리스톨-마이어스 스큅 컴퍼니 파르네소이드 x 수용체 조정제로서의 치환된 비시클릭 화합물
CN113727973B (zh) * 2019-02-15 2025-08-29 百时美施贵宝公司 可用作类法尼醇x受体调节剂的取代酰胺化合物
AR118050A1 (es) 2019-02-15 2021-09-15 Bristol Myers Squibb Co Compuestos bicíclicos sustituidos como moduladores del receptor farnesoide x
AU2020312735A1 (en) 2019-07-18 2021-12-16 Enyo Pharma Method for decreasing adverse-effects of interferon
CN114980887A (zh) 2019-12-20 2022-08-30 特纳亚治疗股份有限公司 氟代烷基-噁二唑及其用途
US20230060715A1 (en) 2020-01-15 2023-03-02 INSERM (Institut National de la Santé et de la Recherche Médicale) Use of fxr agonists for treating an infection by hepatitis d virus
TW202143958A (zh) * 2020-03-18 2021-12-01 美商梅塔克林公司 用於治療疾病之法尼醇x(farnesoid x)受體促效劑
CN120732855A (zh) * 2020-03-18 2025-10-03 伊莱利利公司 用于治疗疾病的法尼醇x受体激动剂
MX2022011582A (es) 2020-03-18 2022-12-13 Metacrine Inc Formas cristalinas de un agonista del receptor farnesoide x.
BR112022018553A2 (pt) 2020-03-18 2022-11-29 Metacrine Inc Formulações de um agonista do receptor x farnesoide
US20230201222A1 (en) * 2020-05-13 2023-06-29 Children's Hospital Medical Center Alleviation of liver injury by activating the signaling pathway mediated by farnesoid x receptor
CN116829139A (zh) * 2020-12-22 2023-09-29 北海医疗私人有限公司 用于治疗非酒精性脂肪性肝炎的包含含氧的结构增强的脂肪酸的联合治疗剂
US20240100125A1 (en) 2021-01-14 2024-03-28 Enyo Pharma Synergistic effect of a fxr agonist and ifn for the treatment of hbv infection
CN117320722A (zh) 2021-04-28 2023-12-29 埃尼奥制药公司 使用fxr激动剂作为联合治疗强烈增强tlr3激动剂的作用
WO2022235842A1 (en) 2021-05-04 2022-11-10 Tenaya Therapeutics, Inc. 2-fluoroalkyl-1,3,4-oxadiazol-5-yl-thiazol, hdac6 inhibitors for use in the treatment of metabolic disease and hfpef
CN116925049A (zh) * 2023-06-27 2023-10-24 广东药科大学 新型联苯类衍生物、其制备方法及其作为药物的用途
CN117285504A (zh) * 2023-09-07 2023-12-26 桂林医学院 一种氨基苯乙酰胺类衍生物及其制备方法和应用

Family Cites Families (58)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR950702544A (ko) 1992-08-11 1995-07-29 구사이 요시히로 비페닐메탄 유도체 및 이를 함유하는 약제
BR0010651A (pt) * 1999-05-17 2002-03-19 Novo Nordisk As Composto, uso de um composto, composição farmacêutica, e, método para o tratamento e/ou prevenção de distúrbios ou de doenças mediadas por uma ação antagonìstica de glucagon
CA2372887A1 (en) 1999-05-25 2000-11-30 Sepracor Inc. Heterocyclic analgesic compounds and their use
US6645980B1 (en) 2000-05-25 2003-11-11 Sepracor Inc. Heterocyclic analgesic compounds and methods of use thereof
US6511980B2 (en) 2000-05-05 2003-01-28 Ortho Mcneil Pharmaceutical, Inc. Substituted diamine derivatives useful as motilin antagonists
AU2001291830A1 (en) 2000-09-25 2002-04-02 Actelion Pharmaceuticals Ltd. Substituted amino-aza-cycloalkanes useful against malaria
FR2815032B1 (fr) 2000-10-10 2003-08-08 Pf Medicament Nouveaux derives d'aminophenyle piperazine ou d'amino phenyle piperide inhibiteurs de proteines prenyl transferase ainsi que leurs preparations
FR2825706B1 (fr) 2001-06-06 2003-12-12 Pf Medicament Nouveaux derives de benzothienyle ou d'indole, leur preparation et leur utilisation comme inhibiteurs de proteines prenyl transferase
CA2468761A1 (en) 2001-10-31 2003-05-08 Morphochem Aktiengesellschaft Fuer Kombinatorische Chemie Novel anticancer compounds
FR2839974B1 (fr) 2002-05-24 2004-07-16 Pf Medicament Derives de phenyl-furane ou de phenyl-thiophene,leur preparation et leur application a titre de medicament
AU2003249983A1 (en) 2002-07-18 2004-02-09 Actelion Pharmaceuticals Ltd Piperidines useful for the treatment of central nervous system disorders
JP2006508061A (ja) * 2002-09-20 2006-03-09 ファイザー・プロダクツ・インク エストロゲン受容体に対するアミドおよびスルホンアミドリガンド
WO2004046162A2 (en) * 2002-11-14 2004-06-03 The Scripps Research Institute Non-steroidal fxr agonists
US20050143449A1 (en) 2002-11-15 2005-06-30 The Salk Institute For Biological Studies Non-steroidal farnesoid X receptor modulators and methods for the use thereof
GB0309781D0 (en) * 2003-04-29 2003-06-04 Glaxo Group Ltd Compounds
EP3042895A1 (en) 2003-07-30 2016-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7759348B2 (en) 2003-07-30 2010-07-20 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
US7754711B2 (en) 2003-07-30 2010-07-13 Xenon Pharmaceuticals Inc. Pyridazine derivatives and their use as therapeutic agents
ES2634841T3 (es) 2003-10-14 2017-09-29 Pfizer Products Inc. Derivados bicíclicos [3.1.0] como inhibidores del transportador de glicina
WO2005058822A1 (en) * 2003-12-17 2005-06-30 Actelion Pharmaceuticals Ltd Substituted amino-cycloalkanes
WO2005097760A1 (en) * 2004-03-26 2005-10-20 Rigel Pharmaceuticals, Inc. Heterocyclic anti-viral compounds comprising metabolizable moieties and their uses
JP2006199656A (ja) 2005-01-24 2006-08-03 Kowa Co アミド基を有する環状アミン化合物
MY144229A (en) 2006-01-26 2011-08-15 Xenon Pharmaceuticals Inc Pyridazine derivatives and their use as therapeutic agents
WO2007093603A1 (en) 2006-02-17 2007-08-23 Neurosearch A/S 1-phenethylpiperidine derivatives and their use as opioid receptor ligands
US20100261758A1 (en) 2006-03-28 2010-10-14 Novartis Ag Heterocyclic amides for use as pharmaceuticals
US20080081824A1 (en) 2006-09-29 2008-04-03 Bristol-Myers Squibb Company Substituted piperidines as modulators of chemokine receptor activity
WO2008065500A2 (en) * 2006-11-30 2008-06-05 Pfizer Products Inc. Heteroaryl amides as type i glycine transport inhibitors
TW200838526A (en) 2006-12-01 2008-10-01 Astellas Pharma Inc Carboxylic acid derivatives
JP2010512418A (ja) 2006-12-11 2010-04-22 ワイス エルエルシー イオンチャネルモジュレータ−としてのカルボキサミド誘導体
CA2689575A1 (en) 2007-06-20 2008-12-24 Merck Sharp & Dohme Corp. Cetp inhibitors derived from benzoxazole arylamides
WO2009076747A1 (en) * 2007-12-19 2009-06-25 Boehringer Ingelheim International Gmbh Viral polymerase inhibitors
WO2010001869A1 (ja) * 2008-06-30 2010-01-07 武田薬品工業株式会社 ４置換ベンゼン化合物およびその用途
JP2010077109A (ja) * 2008-08-28 2010-04-08 Takeda Chem Ind Ltd 複素環化合物およびその用途
JP2012533553A (ja) * 2009-07-15 2012-12-27 アボット・ラボラトリーズ ピロロピリジン系キナーゼ阻害薬
EP2454243A2 (en) * 2009-07-15 2012-05-23 Merck Serono SA Tetrazole derivatives
FR2963005B1 (fr) 2010-07-23 2012-08-17 Sanofi Aventis Derives d'oxadiazoles et de pyridazines, leur preparation et leur application en therapeutique
SMT201700325T1 (it) 2011-03-23 2017-09-07 Trevena Inc Ligandi del recettore degli oppioidi e metodi per l’uso e la produzione dei medesimi
US9492763B2 (en) 2011-07-13 2016-11-15 M. Technique Co., Ltd. Method for producing microparticles having controlled crystallite diameter
CA2893663A1 (en) * 2012-12-05 2014-06-12 Chiesi Farmaceutici S.P.A. Phenylethylpyridine derivatives as pde4-inhibitors
RU2543485C2 (ru) * 2013-02-26 2015-03-10 Андрей Александрович Иващенко Гетероциклические агонисты рецепторов желчных кислот tgr5, фармацевтическая композиция, способы их получения и применения
GB201316824D0 (en) * 2013-09-23 2013-11-06 R & D Vernalis Ltd New Chemical Entities
US10077268B2 (en) 2014-03-13 2018-09-18 Salk Institute For Biological Studies FXR agonists and methods for making and using
KR20160133529A (ko) * 2014-03-13 2016-11-22 더 솔크 인스티튜트 포 바이올로지칼 스터디즈 펙사라민 유도체 및 이의 제조와 사용 방법
US20150258052A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Methods of using fexaramine and agents that increase sympathetic nervous system activity to promote browning of white adipose tissue
CA2942403A1 (en) 2014-03-13 2015-09-17 Salk Institute For Biological Studies Fxr agonists and methods for making and using
US10301268B2 (en) 2014-03-13 2019-05-28 The Salk Institute For Biological Studies Analogs of fexaramine and methods of making and using
WO2016149111A1 (en) 2015-03-13 2016-09-22 Salk Institute For Biological Studies Treating latent autoimmune diabetes of adults with farnesoid x receptor agonists to activate intestinal receptors
EP3350164A4 (en) 2015-09-16 2019-03-27 Metacrine, Inc. FARNESOID-X RECEPTOR AGONISTS AND USES THEREOF
KR20180052678A (ko) 2015-09-16 2018-05-18 메타크린, 인크. 파네소이드 x 수용체 아고니스트 및 이의 용도
US10377717B2 (en) 2015-09-16 2019-08-13 Metacrine, Inc. Farnesoid X receptor agonists and uses thereof
WO2017049172A1 (en) 2015-09-16 2017-03-23 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
AU2018236275B2 (en) 2017-03-15 2022-05-12 Eli Lilly And Company Farnesoid X receptor agonists and uses thereof
US20200131129A1 (en) 2017-03-15 2020-04-30 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018170165A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
WO2018170167A1 (en) 2017-03-15 2018-09-20 Metacrine, Inc. Farnesoid x receptor agonists and uses thereof
CN110637011B (zh) 2017-03-15 2024-05-14 奥加诺沃公司 法尼醇x受体激动剂及其用途
WO2020061114A1 (en) 2018-09-18 2020-03-26 Metacrine, Inc. Farnesoid x receptor agonists for the treatment of disease
JP2022500395A (ja) 2018-09-18 2022-01-04 メタクリン，インク． ファルネソイドｘ受容体アゴニストの結晶形態

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