AR069306A1 - Derivados de metil- bencimidazol como moduladores de receptor x de farnesoide(fxr) - Google Patents

Derivados de metil- bencimidazol como moduladores de receptor x de farnesoide(fxr)

Info

Publication number
AR069306A1
AR069306A1 ARP080104952A ARP080104952A AR069306A1 AR 069306 A1 AR069306 A1 AR 069306A1 AR P080104952 A ARP080104952 A AR P080104952A AR P080104952 A ARP080104952 A AR P080104952A AR 069306 A1 AR069306 A1 AR 069306A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
fluor
heterocyclyl
cycloalkyl
heteroaryl
Prior art date
Application number
ARP080104952A
Other languages
English (en)
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR069306A1 publication Critical patent/AR069306A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/12—Drugs for disorders of the urinary system of the kidneys
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Diabetes (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Child & Adolescent Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Psychology (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Proceso para obtenerlos, composicion farmacéutica y uso para fabricar medicamentos para tratar niveles altos de lípidos y colesterol, cáncer gastrointestinal, osteoporosis, Parkinson y Alzheimer. Reivindicacion 1: Compuestos de la formula (1) en la que R1 es cicloalquilo, alquilo inferior, cicloalquil-alquilo inferior, arilo, aril-alquilo inferior, heteroarilo, heteroaril-alquilo inferior, heterociclilo o heterociclil-alquil inferior, dichos cicloalquilo, arilo, heteroarilo o heterociclilo pueden estar opcionalmente sustituidos por 1-4 sustituyentes elegidos con independencia entre el grupo formado por hidroxi, halogeno, alquilo inferior, alcoxi inferior, fluor-alquilo inferior y fluor-alcoxi inferior; R2 es hidrogeno o alquilo inferior; R3 es cicloalquilo, alquilo inferior, cicloalquil-alquilo inferior, arilo, heteroaril-alquilo inferior, heterociclilo o heterociclil-alquilo interior, dichos cicloalquilo, arilo, heteroarilo o heterociclilo pueden estar opcionalmente sustituidos por 1-4 sustituyentes elegidos con independencia entre el grupo formado por hidroxi, halogeno, alquilo inferior, alcoxi interior, fluor-alquilo inferior, fluor-alcoxi inferior y alcoxi inferior-carbonilo; R4 es arilo, cicloalquilo, heteroarilo o heterociclilo, dichos arilo, cicloalquilo, heteroarilo o heterociclilo pueden estar opcionalmente sustituidos por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, alquilo inferior, alcoxi inferior, hidroxi, dioxo-alquileno inferior, fluor-alquilo inferior y fluor-alcoxi inferior; R5 y R6 con independencia entre sí son hidrogeno, hidroxi, hidroxi-alquilo inferior, alcoxi inferior, alquilo inferior, fluor-alquilo inferior o fluor-alcoxi inferior; R7, R8, R9 y R10 con independencia entre sí son hidrogeno, halogeno, hidroxi, alquilo inferior, alcoxi inferior, fluor-alquilo inferior o fluor-alcoxi inferior; y las sales y ésteres - farmacéuticamente aceptables de los mismos.
ARP080104952A 2007-11-15 2008-11-13 Derivados de metil- bencimidazol como moduladores de receptor x de farnesoide(fxr) AR069306A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP07120737 2007-11-15

Publications (1)

Publication Number Publication Date
AR069306A1 true AR069306A1 (es) 2010-01-13

Family

ID=40551982

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080104952A AR069306A1 (es) 2007-11-15 2008-11-13 Derivados de metil- bencimidazol como moduladores de receptor x de farnesoide(fxr)

Country Status (16)

Country Link
US (2) US7825258B2 (es)
EP (1) EP2222645B1 (es)
JP (1) JP5222953B2 (es)
KR (1) KR101176721B1 (es)
CN (1) CN101855214B (es)
AR (1) AR069306A1 (es)
AU (1) AU2008323017B2 (es)
BR (1) BRPI0818813A2 (es)
CA (1) CA2704074A1 (es)
CL (1) CL2008003372A1 (es)
ES (1) ES2403592T3 (es)
IL (1) IL205207A0 (es)
MX (1) MX2010005164A (es)
PE (1) PE20090999A1 (es)
TW (1) TW200924755A (es)
WO (1) WO2009062874A2 (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2734034A1 (en) * 2008-09-11 2010-03-18 F. Hoffmann-La Roche Ag New benzimidazole derivatives
CN102186830A (zh) 2008-10-15 2011-09-14 霍夫曼-拉罗奇有限公司 新型苯并咪唑衍生物
US8309581B2 (en) * 2009-09-29 2012-11-13 Hoffmann-La Roche Inc. Benzimidazole derivatives
WO2011107494A1 (de) 2010-03-03 2011-09-09 Sanofi Neue aromatische glykosidderivate, diese verbindungen enthaltende arzneimittel und deren verwendung
SG10201607230SA (en) * 2012-06-19 2016-10-28 Intercept Pharmaceuticals Inc Preparation, Uses And Solid Forms Of Obeticholic Acid
US9895380B2 (en) 2013-09-11 2018-02-20 Inserm (Institut National De La Sante Et De La Recherche Medicale) Methods and pharmaceutical compositions for the treatment of hepatitis B virus infection
WO2018153933A1 (en) 2017-02-21 2018-08-30 Genfit Combination of a ppar agonist with a fxr agonist
JP2020515564A (ja) 2017-03-30 2020-05-28 アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル エピソーマルウイルスの持続性及び発現を低下させるための方法及び医薬組成物
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

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2338147A1 (en) * 1998-07-20 2000-02-03 Kuo-Long Yu Substituted benzimidazole antiviral agents
RU2004126671A (ru) 2002-02-06 2005-04-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Гетероарилсоединения, полезные в качестве ингибиторов gsk-3
WO2005002520A2 (en) * 2003-07-01 2005-01-13 Merck & Co., Inc. Ophthalmic compositions for treating ocular hypertension
CN101479249B (zh) * 2006-06-29 2012-10-10 霍夫曼-拉罗奇有限公司 苯并咪唑衍生物、其制备方法、它们作为fxr激动剂的用途及含有它们的药物制剂
CA2697167C (en) * 2007-08-27 2013-07-16 F. Hoffmann-La Roche Ag Benzimidazole derivatives used as fxr agonists

Also Published As

Publication number Publication date
US7825258B2 (en) 2010-11-02
AU2008323017B2 (en) 2012-12-20
CL2008003372A1 (es) 2010-01-04
KR101176721B1 (ko) 2012-08-23
AU2008323017A1 (en) 2009-05-22
BRPI0818813A2 (pt) 2015-04-22
CA2704074A1 (en) 2009-05-22
IL205207A0 (en) 2010-12-30
WO2009062874A3 (en) 2009-07-09
JP5222953B2 (ja) 2013-06-26
ES2403592T3 (es) 2013-05-20
US20100331371A1 (en) 2010-12-30
CN101855214A (zh) 2010-10-06
US20090131482A1 (en) 2009-05-21
PE20090999A1 (es) 2009-07-20
CN101855214B (zh) 2012-12-26
WO2009062874A2 (en) 2009-05-22
EP2222645A2 (en) 2010-09-01
TW200924755A (en) 2009-06-16
MX2010005164A (es) 2010-05-27
JP2011503136A (ja) 2011-01-27
EP2222645B1 (en) 2013-03-20
KR20100071102A (ko) 2010-06-28
US8008503B2 (en) 2011-08-30

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