PE20080259A1 - Compuestos y metodos para modular fxr - Google Patents

Compuestos y metodos para modular fxr

Info

Publication number
PE20080259A1
PE20080259A1 PE2007000629A PE2007000629A PE20080259A1 PE 20080259 A1 PE20080259 A1 PE 20080259A1 PE 2007000629 A PE2007000629 A PE 2007000629A PE 2007000629 A PE2007000629 A PE 2007000629A PE 20080259 A1 PE20080259 A1 PE 20080259A1
Authority
PE
Peru
Prior art keywords
alkyl
methyl
haloalkyl
compounds
ilmetoxy
Prior art date
Application number
PE2007000629A
Other languages
English (en)
Inventor
Michael Gregory Bell
Robert Anthony Doti
Michael James Genin
Peter Ambrose Lander
Tianwei Ma
Nathan Bryan Mantlo
Jason Matthew Ochoada
Lindsay Scott Stelzer
Ryan Edward Stites
Alan M Warshawsky
Matthew Scott Dowling
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20080259A1 publication Critical patent/PE20080259A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I DONDE p 0-1; X1 y X2 SON C, N CON LA CONDICION DE QUE AMBOS X1 y X2 NO SON N; R1 y R2 SON H, ALQUILO C1-C3, HALOALQUILO C1-C3, ENTRE OTROS; R4b ES H, ALQUILO C1-C3, HALOALQUILO C1-C3, ENTRE OTROS; R5 y R5a SON CADA UNO H, ALQUILO C1-C3; R6 ES H, ALQUILO C1-C3, HALOALQUILO C1-C3, ENTRE OTROS; L1 ES ENLACE, ETINILO, ALQUILO C1-C3, ENTRE OTROS; Ar1 ES INDOLILO, BENZOTIENILO, NAFTILO, ENTRE OTROS; R7 ES -COOH, -ALQUILO C1-C3COOH, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: ACIDO 4-[({4-[3-(2,6-DICLOROFENIL)-5-TRIFLUOROMETIL-3H-[1,2,3]TRIAZOL-4-ILMETOXI]-2-METILOFENIL}-METILAMINO)-METILO]-2-METIL-BENZOICO; ACIDO 3-[({4-[3-(2,6-DICLORO-FENIL)-5-ISOPROPIL-3H-[1,2,3]TRIAZOL-4-ILMETOXI]-2-METIL-FENIL}-METIL-AMINO)-METILO]-BENZOICO; ENTRE OTROS. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA Y A UN PROCEDIMIENTO DE PREPARACION. LOS COMPUESTOS DESCRITOS SON AGONISTAS SELECTIVOS PARA EL FXR (RECEPTOR FARMESOIDE X) UTILES EN EL TRATAMIENTO DE DISLIPIDEMIA, ATEROESCLEROSIS, DIABETES Y ENFERMEDADES RELACIONADAS
PE2007000629A 2006-05-24 2007-05-22 Compuestos y metodos para modular fxr PE20080259A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US80810406P 2006-05-24 2006-05-24
US87000106P 2006-12-14 2006-12-14

Publications (1)

Publication Number Publication Date
PE20080259A1 true PE20080259A1 (es) 2008-04-10

Family

ID=38626336

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2007000629A PE20080259A1 (es) 2006-05-24 2007-05-22 Compuestos y metodos para modular fxr

Country Status (16)

Country Link
US (1) US8106077B2 (es)
EP (1) EP2029558B1 (es)
JP (1) JP5225984B2 (es)
AR (1) AR061101A1 (es)
AT (1) ATE460403T1 (es)
AU (1) AU2007267692B2 (es)
BR (1) BRPI0711875A2 (es)
CA (1) CA2651373A1 (es)
CL (1) CL2007001451A1 (es)
DE (1) DE602007005256D1 (es)
EA (1) EA014720B1 (es)
ES (1) ES2340221T3 (es)
MX (1) MX2008014959A (es)
PE (1) PE20080259A1 (es)
TW (1) TW200812982A (es)
WO (1) WO2007140174A2 (es)

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TW200906823A (en) * 2007-07-16 2009-02-16 Lilly Co Eli Compounds and methods for modulating FXR
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
US8217064B2 (en) 2007-12-20 2012-07-10 Envivo Pharmaceuticals, Inc. Tetrasubstituted benzenes
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EP2128158A1 (en) 2008-05-26 2009-12-02 Phenex Pharmaceuticals AG Heterocyclic cyclopropyl-substituted FXR binding compounds
WO2010034649A1 (en) * 2008-09-25 2010-04-01 F. Hoffmann-La Roche Ag 2,3-substituted indazole or 4,5,6,7-tetrahydro-indazoles as fxr modulators against dyslipidemia and related diseases
EP2289883A1 (en) 2009-08-19 2011-03-02 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
US8252826B2 (en) 2010-03-24 2012-08-28 Hoffmann-La Roche Inc. Cyclopentyl- and cycloheptylpyrazoles
EP2582709B1 (de) 2010-06-18 2018-01-24 Sanofi Azolopyridin-3-on-derivate als inhibitoren von lipasen und phospholipasen
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ES2536667T3 (es) * 2010-11-09 2015-05-27 F. Hoffmann-La Roche Ag Derivados de triazol como ligandos de receptores Gaba
CU24152B1 (es) 2010-12-20 2016-02-29 Irm Llc 1,2 oxazol-8-azabiciclo[3,2,1]octano 8 il como moduladores de fxr
US8871758B2 (en) 2011-03-08 2014-10-28 Sanofi Tetrasubstituted oxathiazine derivatives, method for producing them, their use as medicine and drug containing said derivatives and the use thereof
US8828995B2 (en) 2011-03-08 2014-09-09 Sanofi Branched oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8828994B2 (en) 2011-03-08 2014-09-09 Sanofi Di- and tri-substituted oxathiazine derivatives, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
US8710050B2 (en) 2011-03-08 2014-04-29 Sanofi Di and tri- substituted oxathiazine derivatives, method for the production, method for the production thereof, use thereof as medicine and drug containing said derivatives and use thereof
EP2766349B1 (de) 2011-03-08 2016-06-01 Sanofi Mit carbozyklen oder heterozyklen substituierte oxathiazinderivate, verfahren zu deren herstellung, diese verbindungen enthaltende arzneimittel und deren verwendung
EP2545964A1 (en) 2011-07-13 2013-01-16 Phenex Pharmaceuticals AG Novel FXR (NR1H4) binding and activity modulating compounds
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IN2014DN11027A (es) * 2012-06-26 2015-09-25 Aniona Aps
RS61540B1 (sr) 2013-09-11 2021-04-29 Inst Nat Sante Rech Med Postupci i farmaceutske kompozicije za tretiranje infekcije hepatitis b virusa
JP2017505770A (ja) 2014-01-24 2017-02-23 シンアフィックス ビー.ブイ. (ヘテロ)アリール1,3−双極子化合物と(ヘテロ)シクロアルキンとの環化付加のためのプロセス
EP3006939A1 (en) 2014-10-06 2016-04-13 Gilead Sciences, Inc. Histidine-rich Glycoprotein as a marker for hepatic Farnesoid X receptor activation
US10208081B2 (en) 2014-11-26 2019-02-19 Enanta Pharmaceuticals, Inc. Bile acid derivatives as FXR/TGR5 agonists and methods of use thereof
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CN114144185A (zh) 2019-05-30 2022-03-04 英特塞普特医药品公司 用于治疗胆汁淤积性肝病的包含fxr激动剂和贝特类的药物组合物
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JP2024517181A (ja) 2021-04-28 2024-04-19 ウエヌイグレックオ・ファーマ 組合せ治療としてfxrアゴニストを使用するtlr3アゴニストの効果の強い増強

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Also Published As

Publication number Publication date
US20090093524A1 (en) 2009-04-09
TW200812982A (en) 2008-03-16
JP2009538333A (ja) 2009-11-05
MX2008014959A (es) 2008-12-09
JP5225984B2 (ja) 2013-07-03
EP2029558B1 (en) 2010-03-10
AU2007267692B2 (en) 2012-06-14
CA2651373A1 (en) 2007-12-06
AR061101A1 (es) 2008-08-06
ATE460403T1 (de) 2010-03-15
DE602007005256D1 (de) 2010-04-22
EA014720B1 (ru) 2011-02-28
ES2340221T3 (es) 2010-05-31
US8106077B2 (en) 2012-01-31
WO2007140174A2 (en) 2007-12-06
BRPI0711875A2 (pt) 2012-01-10
WO2007140174A3 (en) 2008-03-20
EA200870569A1 (ru) 2009-06-30
AU2007267692A1 (en) 2007-12-06
CL2007001451A1 (es) 2008-01-11
EP2029558A2 (en) 2009-03-04

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