JP5503007B2 - 新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 - Google Patents

新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 Download PDF

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Publication number
JP5503007B2
JP5503007B2 JP2012531341A JP2012531341A JP5503007B2 JP 5503007 B2 JP5503007 B2 JP 5503007B2 JP 2012531341 A JP2012531341 A JP 2012531341A JP 2012531341 A JP2012531341 A JP 2012531341A JP 5503007 B2 JP5503007 B2 JP 5503007B2
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JP
Japan
Prior art keywords
difluoro
phenyl
chloro
benzimidazole
cyclohexylmethyl
Prior art date
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Expired - Fee Related
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JP2012531341A
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English (en)
Japanese (ja)
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JP2013505977A (ja
Inventor
ベンソン，グレゴリー・マーチン
ブライヒャー，コンラート
フェン，ソン
グレター，ウーヴェ
クーン，ベルント
マルティン，ライナー・エー
プランシャー，ジャン−マルク
リヒター，ハンス
ルドルフ，マルクス
テイラー，スヴェン
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F Hoffmann La Roche AG
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F Hoffmann La Roche AG
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Publication of JP2013505977A publication Critical patent/JP2013505977A/ja
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Expired - Fee Related legal-status Critical Current
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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)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Diabetes (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
JP2012531341A 2009-09-29 2010-09-27 新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用 Expired - Fee Related JP5503007B2 (ja)

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 (2)

Publication Number Publication Date
JP2013505977A JP2013505977A (ja) 2013-02-21
JP5503007B2 true JP5503007B2 (ja) 2014-05-28

Family

ID=43033176

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2012531341A Expired - Fee Related JP5503007B2 (ja) 2009-09-29 2010-09-27 新規なベンゾイミダゾール誘導体及びｆｘｒアゴニストとしてのそれらの使用

Country Status (12)

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

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3043865T3 (da) 2013-09-11 2021-02-01 Univ Claude Bernard Lyon Fremgangsmåder og farmaceutiske sammensætningr til behandlingen af hepatitis b-virusinfektion
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
KR20190117632A (ko) 2017-02-21 2019-10-16 장피트 Ppar 효현제와 fxr 효현제의 병용
WO2018178260A1 (en) 2017-03-30 2018-10-04 INSERM (Institut National de la Santé et de la Recherche Médicale) 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
RU2424233C2 (ru) 2006-06-29 2011-07-20 Ф.Хоффманн-Ля Рош Аг Производные бензимидазола, методы их получения, применение их в качестве агонистов фарнезоид-х-рецептора (fxr) и содержащие их фармацевтические препараты
DE102007008420A1 (de) 2007-02-21 2008-08-28 Merck Patent Gmbh Benzimidazolderivate
EP2188263B1 (en) * 2007-08-27 2012-06-27 F. Hoffmann-La Roche AG Benzimidazole derivatives used as fxr agonists
EP2222645B1 (en) * 2007-11-15 2013-03-20 F. Hoffmann-La Roche AG Benzimidazole derivatives and their use as fxr agonists
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
AU2009304169A1 (en) * 2008-10-15 2010-04-22 F. Hoffmann-La Roche Ag New benzimidazole derivatives

Also Published As

Publication number Publication date
EP2483247A1 (en) 2012-08-08
HK1171746A1 (zh) 2013-04-05
MX2012002479A (es) 2012-03-26
US20110077273A1 (en) 2011-03-31
CN102574812B (zh) 2016-03-30
CA2772815A1 (en) 2011-04-07
CN102574812A (zh) 2012-07-11
US8309581B2 (en) 2012-11-13
BR112012006986A2 (pt) 2016-04-12
IL218037A0 (en) 2012-04-30
KR20120063536A (ko) 2012-06-15
AU2010303146A1 (en) 2012-04-19
WO2011039130A1 (en) 2011-04-07
IN2012DN01234A (https=) 2015-05-15
JP2013505977A (ja) 2013-02-21
KR101477872B1 (ko) 2014-12-30

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