ZA200810481B - Benzimidazole derivatives, method for the production thereof, their use as FXR agonists and pharmaceutical preparations containing the same - Google Patents

Benzimidazole derivatives, method for the production thereof, their use as FXR agonists and pharmaceutical preparations containing the same

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Publication number
ZA200810481B
ZA200810481B ZA200810481A ZA200810481A ZA200810481B ZA 200810481 B ZA200810481 B ZA 200810481B ZA 200810481 A ZA200810481 A ZA 200810481A ZA 200810481 A ZA200810481 A ZA 200810481A ZA 200810481 B ZA200810481 B ZA 200810481B
Authority
ZA
South Africa
Prior art keywords
production
same
pharmaceutical preparations
preparations containing
benzimidazole derivatives
Prior art date
Application number
ZA200810481A
Other languages
English (en)
Inventor
Gregory Martin Benson
Konrad Bleicher
Alexander Chucholowski
Henrietta Dehmlow
Uwe Grether
Bernd Kuhn
Rainer E Martin
Eric J Niesor
Narendra Panday
Hans Richter
Franz Schuler
Xavier Marie Warot
Matthew Wright
Minmin Yang
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=38462503&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=ZA200810481(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of ZA200810481B publication Critical patent/ZA200810481B/xx

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
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    • A61P19/00Drugs for skeletal disorders
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P3/04Anorexiants; Antiobesity agents
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    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
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    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • 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
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P9/12Antihypertensives
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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
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    • 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
    • C07D401/04Heterocyclic 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
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    • C07D401/06Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
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    • 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
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  • Animal Behavior & Ethology (AREA)
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  • Life Sciences & Earth Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
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  • Diabetes (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
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  • Hematology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
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  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA200810481A 2006-06-29 2008-12-10 Benzimidazole derivatives, method for the production thereof, their use as FXR agonists and pharmaceutical preparations containing the same ZA200810481B (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP06116302 2006-06-29

Publications (1)

Publication Number Publication Date
ZA200810481B true ZA200810481B (en) 2009-12-30

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ID=38462503

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Application Number Title Priority Date Filing Date
ZA200810481A ZA200810481B (en) 2006-06-29 2008-12-10 Benzimidazole derivatives, method for the production thereof, their use as FXR agonists and pharmaceutical preparations containing the same

Country Status (17)

Country Link
US (1) US7645785B2 (ru)
EP (1) EP2038259A1 (ru)
JP (1) JP4970538B2 (ru)
KR (1) KR101237623B1 (ru)
CN (1) CN101479249B (ru)
AR (1) AR061666A1 (ru)
AU (1) AU2007263807B2 (ru)
BR (1) BRPI0713946A2 (ru)
CA (1) CA2655395C (ru)
CL (1) CL2007001869A1 (ru)
IL (1) IL195748A0 (ru)
MX (1) MX2008015923A (ru)
NO (1) NO20085121L (ru)
RU (1) RU2424233C2 (ru)
TW (1) TWI329638B (ru)
WO (1) WO2008000643A1 (ru)
ZA (1) ZA200810481B (ru)

Families Citing this family (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UY30048A1 (es) * 2005-12-23 2007-07-31 Astrazeneca Ab Derivados sustituidos de la n,2-(1h-benzimidazol-1-il) acetamida, composiciones farmacéuticas conteniéndolos, procesos de preparación y aplicaciones
US20160331729A9 (en) 2007-04-11 2016-11-17 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
US11241420B2 (en) 2007-04-11 2022-02-08 Omeros Corporation Compositions and methods for prophylaxis and treatment of addictions
EP2025674A1 (de) 2007-08-15 2009-02-18 sanofi-aventis Substituierte Tetrahydronaphthaline, Verfahren zu ihrer Herstellung und ihre Verwendung als Arzneimittel
CN102083799B (zh) * 2007-08-27 2013-10-16 霍夫曼-拉罗奇有限公司 用作fxr激动剂的苯并咪唑衍生物
EP2222645B1 (en) * 2007-11-15 2013-03-20 F. Hoffmann-La Roche AG Benzimidazole derivatives and their use as fxr agonists
US7816540B2 (en) 2007-12-21 2010-10-19 Hoffmann-La Roche Inc. Carboxyl- or hydroxyl-substituted benzimidazole derivatives
EP2321282B1 (en) * 2008-09-11 2013-03-27 F. Hoffmann-La Roche AG New benzimidazole derivatives
ES2444791T3 (es) 2008-10-15 2014-02-26 F. Hoffmann-La Roche Ag Nuevos derivados de benzimidazol
US8309581B2 (en) * 2009-09-29 2012-11-13 Hoffmann-La Roche Inc. Benzimidazole derivatives
US20120263646A1 (en) * 2009-10-15 2012-10-18 Guerbet Imaging agents and their use for the diagnostic in vivo of neurodegenerative diseases, notably alzheimer's disease and derivative diseases
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
MX2015006710A (es) * 2012-11-28 2016-01-15 Intercept Pharmaceuticals Inc Tratamiento de las enfermedades pulmonares.
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
CN105102448B (zh) 2013-02-28 2018-03-06 百时美施贵宝公司 作为rock1和rock2抑制剂的苯基吡唑衍生物
CA2923090C (en) 2013-09-11 2018-08-21 Poxel Methods and pharmaceutical compositions for the treatment of hepatitis b virus infection
EP3214076A4 (en) * 2014-10-28 2018-07-25 Shionogi & Co., Ltd. Heterocyclic derivative having ampk activating effect
WO2017168451A1 (en) * 2016-03-31 2017-10-05 Shiv Nadar University Derivatives of imidazole and benzimidazole, method of preparation and use thereof
WO2018013776A1 (en) 2016-07-14 2018-01-18 Bristol-Myers Squibb Company Tricyclic heteroaryl-substituted quinoline and azaquinoline compounds as par4 inhibitors
CN109689649B (zh) 2016-07-14 2022-07-19 百时美施贵宝公司 经二环杂芳基取代的化合物
KR102398941B1 (ko) * 2016-07-27 2022-05-17 패들락 테라퓨틱스, 인코포레이티드 Pad4의 공유결합성 억제제
EP3512514A1 (en) * 2016-09-14 2019-07-24 Novartis AG Novel regimes of fxr agonists
CN106905241B (zh) * 2017-02-14 2020-03-17 沈阳药科大学 1,2-二取代苯并咪唑衍生物及其应用
JP2020508316A (ja) 2017-02-21 2020-03-19 ジェンフィGenfit Pparアゴニストとfxrアゴニストとの組合せ
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
CN110536890B (zh) 2017-04-26 2023-08-15 巴斯利尔药物国际股份公司 制备呋咱并苯并咪唑及其晶型的方法
CN111741946B (zh) * 2017-12-29 2022-09-23 厦门宝太生物科技股份有限公司 吲哚胺2,3-双加氧酶抑制剂以及它们在医学上的应用
CN111471011B (zh) * 2017-12-29 2021-06-01 杭州阿诺生物医药科技有限公司 高活性吲哚胺2,3-双加氧酶抑制剂的制备方法
CN111072604B (zh) * 2018-10-18 2022-11-04 广东东阳光药业有限公司 α-氨基酰胺衍生物及其用途
KR102119150B1 (ko) * 2018-10-23 2020-06-04 한국원자력의학원 N-1h-벤지미다졸-2-일-3-(1h-피롤-1-일) 벤자미드를 유효성분으로 함유하는 암 예방 또는 치료용 약학적 조성물
CN112409281B (zh) * 2020-08-20 2022-11-18 上海大学 (e)-3-(3-氯-2-氟-6-(1h-四氮唑-1-基)苯基)丙烯酸的合成方法

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997012613A1 (en) * 1995-10-05 1997-04-10 Warner-Lambert Company Method for treating and preventing inflammation and atherosclerosis
WO2001021634A1 (en) * 1999-09-21 2001-03-29 Lion Bioscience Ag Benzimidazole derivatives and combinatorial libraries thereof
US6855714B2 (en) * 2001-07-06 2005-02-15 Schering Aktiengesellschaft 1-alkyl-2-aryl-benzimidazole derivatives, their use for the production of pharmaceutical agents as well as pharmaceutical preparations that contain these derivatives
SG159380A1 (en) * 2002-02-06 2010-03-30 Vertex Pharma Heteroaryl compounds useful as inhibitors of gsk-3
WO2003080803A2 (en) 2002-03-21 2003-10-02 Smithkline Beecham Corporation Methods of using farnesoid x receptor (fxr) agonists

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JP4970538B2 (ja) 2012-07-11
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IL195748A0 (en) 2009-09-01
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US7645785B2 (en) 2010-01-12
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