BR112014014909A2 - agonistas de tgr5 não sistêmicos - Google Patents

agonistas de tgr5 não sistêmicos

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Publication number
BR112014014909A2
BR112014014909A2 BR112014014909A BR112014014909A BR112014014909A2 BR 112014014909 A2 BR112014014909 A2 BR 112014014909A2 BR 112014014909 A BR112014014909 A BR 112014014909A BR 112014014909 A BR112014014909 A BR 112014014909A BR 112014014909 A2 BR112014014909 A2 BR 112014014909A2
Authority
BR
Brazil
Prior art keywords
tgr5 agonists
systemic
compounds
systemic tgr5
agonists
Prior art date
Application number
BR112014014909A
Other languages
English (en)
Inventor
Spencer Andrew
Carreras Christopher
Charmot Dominique
g lewis Jason
W Jacobs Jeffrey
Navre Marc
Reich Nicholas
Finn Patricia
Chen Tao
Original Assignee
Ardelyx 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 Ardelyx Inc filed Critical Ardelyx Inc
Publication of BR112014014909A2 publication Critical patent/BR112014014909A2/pt

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    • C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
    • C07D241/38—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems with only hydrogen or carbon atoms directly attached to the ring nitrogen atoms
    • C07D241/40—Benzopyrazines
    • C07D241/42—Benzopyrazines with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to carbon atoms of the hetero ring
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
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    • A61K31/5375—1,4-Oxazines, e.g. morpholine
    • A61K31/5377—1,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic System
    • C07F9/02—Phosphorus compounds
    • C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/6536—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having nitrogen and sulfur atoms with or without oxygen atoms, as the only ring hetero atoms
    • C07F9/6544—Six-membered rings
    • C07F9/6547—Six-membered rings condensed with carbocyclic rings or carbocyclic ring systems

Abstract

resumo "agonistas de tgr5 não sistêmicos" trata-se de compostos que tem a seguinte estrutura (i): (i) ou um estereoisômero, tautômero, sal farmaceuticamente aceitável ou pró-fármaco do mesmo, em que r1, r2, r3, r4, r8, r9, r10, r11, r12, a1, a2, x, y e z são conforme definido no presente documento. os usos de tais compostos como anta-gonistas de tgr5 e para o tratamento de diversas indicações, que incluem diabetes mellitus do tipo ii também são fornecidos.
BR112014014909A 2011-12-21 2012-12-21 agonistas de tgr5 não sistêmicos BR112014014909A2 (pt)

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Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN106316975A (zh) * 2015-06-15 2017-01-11 山东轩竹医药科技有限公司 酰胺类化合物及其作为tgr5激动剂的应用
WO2017042380A1 (en) 2015-09-11 2017-03-16 Universite De Lille 2 Droit Et Sante Novel 5-amino-2-thioimidazole compounds and their use
WO2017059057A1 (en) * 2015-09-30 2017-04-06 The Regents Of The University Of California Nano-adhesive and surface primer compound and use thereof
TW202246215A (zh) 2015-12-18 2022-12-01 美商亞德利克斯公司 作為非全身ｔｇｒ５促效劑之經取代之４－苯基吡啶化合物
WO2017134188A1 (en) 2016-02-03 2017-08-10 Universite De Lille 2 Droit Et Sante Novel dihydropyridinone and dihydropyrimidinone compounds and their use
CN106397174B (zh) * 2016-08-24 2018-12-21 河北诚信集团有限公司 一种制备3,6-二氯-2-甲氧基苯甲酸的方法
CN106543180B (zh) * 2016-10-28 2018-03-30 南京正大天晴制药有限公司 苯甲酸利格列汀晶型及其制备方法
CN108440455B (zh) * 2018-04-11 2019-06-14 上海馨远医药科技有限公司 一种3-氧杂环丁烷羧酸的制备方法
HUE061559T2 (hu) 2018-06-07 2023-07-28 Idorsia Pharmaceuticals Ltd Alkoxi-helyettesített piridinil származékok mint LAP1 receptor antagonisták és fibrózis kezelésében való alkalmazásuk
BR112021004656A2 (pt) 2018-09-26 2021-06-01 Jiangsu Hengrui Medicine Co., Ltd. conjugado fármaco-ligante de análogo exatecano, método para preparar o mesmo e aplicação do mesmo
AR119162A1 (es) 2019-06-18 2021-12-01 Idorsia Pharmaceuticals Ltd Derivados de piridin-3-ilo
WO2021071837A1 (en) 2019-10-07 2021-04-15 Kallyope, Inc. Gpr119 agonists
CN112794844B (zh) * 2019-11-13 2023-03-21 中国科学院上海药物研究所 酯类化合物及其制备方法和应用、酯类软药
TW202128227A (zh) 2019-12-12 2021-08-01 大陸商江蘇恆瑞醫藥股份有限公司 抗密蛋白抗體藥物偶聯物及其醫藥用途
EP4095148A4 (en) 2020-01-22 2023-07-26 Jiangsu Hengrui Medicine Co., Ltd. ANTI-TROP-2 ANTIBODY EXATECAN ANALOGUE CONJUGATE AND MEDICAL USE THEREOF
AU2021243073A1 (en) 2020-03-25 2022-10-13 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Pharmaceutical composition comprising antibody drug conjugate and use thereof
KR20220157425A (ko) 2020-03-25 2022-11-29 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 항체 약물 접합체의 제조 방법
AU2021240756A1 (en) 2020-03-25 2022-11-17 Jiangsu Hengrui Pharmaceuticals Co., Ltd. Anti-PSMA antibody-exatecan analogue conjugate and medical use thereof
US20230183419A1 (en) * 2020-04-23 2023-06-15 The Regents Of The University Of Michigan Biodegradable Copolymers and Nanofibrous Scaffold Thereof
CA3178994A1 (en) 2020-05-19 2021-11-25 Iyassu Sebhat Ampk activators
CN116390925A (zh) 2020-06-26 2023-07-04 卡尔优普公司 Ampk活化剂
CN111763173B (zh) * 2020-07-14 2022-11-01 河南大学 苯乙基咪唑类衍生物及其用途
CA3190491A1 (en) 2020-08-24 2022-03-03 Hua Medicine (Shanghai) Ltd. Preparation of substituted acrylate compound
CN114516839A (zh) * 2020-11-20 2022-05-20 湖南海利常德农药化工有限公司 吡唑醚类化合物及其制备方法与应用
KR102600176B1 (ko) * 2021-10-18 2023-11-10 주식회사 사피엔스바이오 신규한 화합물 및 이를 포함하는 약학적 조성물

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20050228016A1 (en) * 2002-06-13 2005-10-13 Enrique Michelotti Tetrahydroquinolines for modulating the expression of exogenous genes via an ecdysone receptor complex
GB0517740D0 (en) * 2005-08-31 2005-10-12 Novartis Ag Organic compounds
US8309734B2 (en) * 2008-10-29 2012-11-13 Hoffmann-La Roche Inc. Substituted pyridines as GPBAR1 agonists
US8420647B2 (en) * 2010-01-21 2013-04-16 Hoffmann-La Roche Inc. 4-phenoxy-nicotinamide or 4-phenoxy-pyrimidine-5-carboxamide compounds

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JP2015506349A (ja) 2015-03-02
AU2012358359A1 (en) 2014-07-24
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MX2014007600A (es) 2014-09-12
US20150148311A1 (en) 2015-05-28

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