CA2772815A1 - New benzimidazole derivatives and their use as fxr agonists - Google Patents

New benzimidazole derivatives and their use as fxr agonists Download PDF

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Publication number
CA2772815A1
CA2772815A1 CA2772815A CA2772815A CA2772815A1 CA 2772815 A1 CA2772815 A1 CA 2772815A1 CA 2772815 A CA2772815 A CA 2772815A CA 2772815 A CA2772815 A CA 2772815A CA 2772815 A1 CA2772815 A1 CA 2772815A1
Authority
CA
Canada
Prior art keywords
difluoro
chloro
phenyl
benzoimidazole
benzoimidazol
Prior art date
Legal status (The legal status 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 status listed.)
Abandoned
Application number
CA2772815A
Other languages
English (en)
French (fr)
Inventor
Gregory Martin Benson
Konrad Bleicher
Song Feng
Uwe Grether
Bernd Kuhn
Rainer E. Martin
Jean-Marc Plancher
Hans Richter
Markus Rudolph
Sven Taylor
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
F Hoffmann La Roche AG
Original Assignee
F Hoffmann La Roche AG
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 F Hoffmann La Roche AG filed Critical F Hoffmann La Roche AG
Publication of CA2772815A1 publication Critical patent/CA2772815A1/en
Abandoned legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic 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
    • C07D401/02—Heterocyclic 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
    • C07D401/04—Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • 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
    • 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
    • A61P3/06—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
    • 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
    • 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
    • C07D235/18—Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/10—Heterocyclic 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 carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic 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
    • C07D403/12—Heterocyclic 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
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
CA2772815A 2009-09-29 2010-09-27 New benzimidazole derivatives and their use as fxr agonists Abandoned CA2772815A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP09171700 2009-09-29
EP09171700.9 2009-09-29
PCT/EP2010/064217 WO2011039130A1 (en) 2009-09-29 2010-09-27 New benzimidazole derivatives and their use as fxr agonists

Publications (1)

Publication Number Publication Date
CA2772815A1 true CA2772815A1 (en) 2011-04-07

Family

ID=43033176

Family Applications (1)

Application Number Title Priority Date Filing Date
CA2772815A Abandoned CA2772815A1 (en) 2009-09-29 2010-09-27 New benzimidazole derivatives and their use as fxr agonists

Country Status (12)

Country Link
US (1) US8309581B2 (en:Method)
EP (1) EP2483247A1 (en:Method)
JP (1) JP5503007B2 (en:Method)
KR (1) KR101477872B1 (en:Method)
CN (1) CN102574812B (en:Method)
AU (1) AU2010303146A1 (en:Method)
BR (1) BR112012006986A2 (en:Method)
CA (1) CA2772815A1 (en:Method)
IL (1) IL218037A0 (en:Method)
IN (1) IN2012DN01234A (en:Method)
MX (1) MX2012002479A (en:Method)
WO (1) WO2011039130A1 (en:Method)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX377523B (es) 2013-09-11 2025-03-10 Inst Nat Sante Rech Med Metodos y composiciones farmaceuticas para el tratamiento de la infeccion por el virus de la hepatitis b.
CN108072684B (zh) * 2016-11-11 2020-06-16 中国科学院广州生物医药与健康研究院 法尼醇x受体的新配体及其筛选方法和应用
EP3585374B1 (en) 2017-02-21 2023-07-19 Genfit Combination of a ppar agonist with a fxr agonist
EP3600293A1 (en) 2017-03-30 2020-02-05 Institut National de la Sante et de la Recherche Medicale (INSERM) Methods and pharmaceutical compositions for reducing persistence and expression of episomal viruses

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2888847B1 (fr) * 2005-07-22 2007-08-31 Sanofi Aventis Sa Derives de n-(heteriaryl)-1-heteorarylalkyl-1h-indole-2- carboxamides, leur preparation et application en therapeutique
KR101237623B1 (ko) 2006-06-29 2013-02-26 에프. 호프만-라 로슈 아게 벤즈이미다졸 유도체, 이의 제조방법, ｆｘｒ 작용물질로서이의 용도, 및 이를 함유하는 약학 제제
DE102007008420A1 (de) 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate
AU2008291148B2 (en) * 2007-08-27 2011-03-17 F. Hoffmann-La Roche Ag Benzimidazole derivatives used as FXR agonists
ES2403592T3 (es) * 2007-11-15 2013-05-20 F. Hoffmann-La Roche Ag Nuevos derivados de bencimidazol y su empleo como agonsitas del FXR
BRPI0918809A2 (pt) * 2008-09-11 2015-12-01 Hoffmann La Roche compostos derivados de benzimidazol, processo para a sua manufatura, composições farmacêuticas que os compreendem, método para o tratamento terapêutico e/ou profilático de enfermidades que são afetadas por moduladores de fxr e uso dos compostos
KR20110069173A (ko) * 2008-10-15 2011-06-22 에프. 호프만-라 로슈 아게 신규한 벤즈이미다졸 유도체

Also Published As

Publication number Publication date
MX2012002479A (es) 2012-03-26
BR112012006986A2 (pt) 2016-04-12
CN102574812B (zh) 2016-03-30
US8309581B2 (en) 2012-11-13
JP2013505977A (ja) 2013-02-21
IL218037A0 (en) 2012-04-30
WO2011039130A1 (en) 2011-04-07
IN2012DN01234A (en:Method) 2015-05-15
KR101477872B1 (ko) 2014-12-30
AU2010303146A1 (en) 2012-04-19
US20110077273A1 (en) 2011-03-31
JP5503007B2 (ja) 2014-05-28
EP2483247A1 (en) 2012-08-08
CN102574812A (zh) 2012-07-11
KR20120063536A (ko) 2012-06-15
HK1171746A1 (zh) 2013-04-05

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Legal Events

Date Code Title Description
EEER Examination request

Effective date: 20150915

FZDE Discontinued

Effective date: 20171219