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AU8122791A - Benzimidazoles - Google Patents

Benzimidazoles

Info

Publication number
AU8122791A
AU8122791A AU81227/91A AU8122791A AU8122791A AU 8122791 A AU8122791 A AU 8122791A AU 81227/91 A AU81227/91 A AU 81227/91A AU 8122791 A AU8122791 A AU 8122791A AU 8122791 A AU8122791 A AU 8122791A
Authority
AU
Australia
Prior art keywords
benzimidazoles
isomers
mixtures
salts
image
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.)
Granted
Application number
AU81227/91A
Other versions
AU640505B2 (en
Inventor
Michael Dr Entzeroth
Norbert Dr Hauel
Berthold Dr Narr
Uwe Dr Ries
Jacques Dr Van Meel
Wolfgang Dr Wienen
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.)
Boehringer Ingelheim Pharma GmbH and Co KG
Original Assignee
Dr Karl Thomae GmbH
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
Priority claimed from DE4023369A external-priority patent/DE4023369A1/en
Application filed by Dr Karl Thomae GmbH filed Critical Dr Karl Thomae GmbH
Publication of AU8122791A publication Critical patent/AU8122791A/en
Application granted granted Critical
Publication of AU640505B2 publication Critical patent/AU640505B2/en
Anticipated expiration legal-status Critical
Expired legal-status Critical Current

Links

Classifications

    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory 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
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A61P25/26—Psychostimulants, e.g. nicotine, cocaine
    • 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
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • 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
    • 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
    • A61P9/08—Vasodilators for multiple indications
    • 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
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08—Radicals containing only hydrogen and carbon atoms
    • 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
    • C07D403/14—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 three or more hetero rings

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychiatry (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Vascular Medicine (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Urology & Nephrology (AREA)
  • Child & Adolescent Psychology (AREA)
  • Obesity (AREA)
  • Pulmonology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Toys (AREA)
  • Instructional Devices (AREA)

Abstract

The invention relates to benzimidazoles of the general formula <IMAGE> in which R1 to R4 are as defined in Claim 1, mixtures of their 1-, 3-isomers, and their salts, which have valuable properties. The novel compounds are, in particular, angiotensin antagonists.
AU81227/91A 1990-07-23 1991-07-23 Benzimidazoles Expired AU640505B2 (en)

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
DE4023369 1990-07-23
DE4023369A DE4023369A1 (en) 1990-07-23 1990-07-23 New 1-bi:phenylyl:methyl benzimidazole derivs.
DE4031287A DE4031287A1 (en) 1990-07-23 1990-10-04 BENZIMIDAZOLE, MEDICAMENTS CONTAINING THESE COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF
DE4031287 1990-10-04
DE4105324A DE4105324A1 (en) 1990-07-23 1991-02-20 BENZIMIDAZOLE, MEDICAMENTS CONTAINING THESE COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF
DE4105324 1991-02-20

Publications (2)

Publication Number Publication Date
AU8122791A true AU8122791A (en) 1992-01-30
AU640505B2 AU640505B2 (en) 1993-08-26

Family

ID=27201487

Family Applications (1)

Application Number Title Priority Date Filing Date
AU81227/91A Expired AU640505B2 (en) 1990-07-23 1991-07-23 Benzimidazoles

Country Status (18)

Country Link
EP (1) EP0468470B1 (en)
JP (1) JP2539113B2 (en)
AT (1) ATE151766T1 (en)
AU (1) AU640505B2 (en)
CA (1) CA2047496C (en)
CS (1) CS230491A3 (en)
DE (1) DE59108658D1 (en)
DK (1) DK0468470T3 (en)
ES (1) ES2100907T3 (en)
FI (1) FI105811B (en)
GR (1) GR3024027T3 (en)
HU (1) HUT58298A (en)
IE (1) IE912563A1 (en)
IL (1) IL98933A (en)
NO (1) NO178927C (en)
NZ (1) NZ239089A (en)
PT (1) PT98414B (en)
RU (1) RU1836357C (en)

Cited By (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU630431B2 (en) * 1989-03-15 1992-10-29 Janssen Pharmaceutica N.V. (5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl)carbamates
AU637356B2 (en) * 1989-02-23 1993-05-27 British Bio-Technology Limited Novel benzimidazole derivatives
AU661129B2 (en) * 1992-04-11 1995-07-13 Dr. Karl Thomae Gmbh Benzimidazoles
US5556981A (en) * 1992-06-03 1996-09-17 Eli Lilly And Company Angiotensin II antagonist intermediates
AU672262B2 (en) * 1993-02-15 1996-09-26 Bayer Aktiengesellschaft Heterocyclically substituted phenyl-cyclohexane-carboxylic acid derivatives
AU675433B2 (en) * 1991-02-06 1997-02-06 Dr. Karl Thomae Gmbh Benzimidazoles

Families Citing this family (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IE70593B1 (en) * 1989-09-29 1996-12-11 Eisai Co Ltd Biphenylmethane derivative the use of it and pharmacological compositions containing same
DE4225756A1 (en) * 1992-01-22 1994-03-10 Thomae Gmbh Dr K Benzimidazoles, medicaments containing these compounds and process for their preparation
US5594003A (en) * 1991-02-06 1997-01-14 Dr. Karl Thomae Gmbh Tetrahydroimidazo[1,2-a]pyridin-2-yl-(benzimidazol-1-yl)-methyl-biphenyls useful as angiotensin-II antagonists
US5602127A (en) * 1991-02-06 1997-02-11 Karl Thomae Gmbh (Alkanesultam-1-yl)-benzimidazol-1-yl)-1yl)-methyl-biphenyls useful as angiotensin-II antagonists
SI9210098B (en) * 1991-02-06 2000-06-30 Dr. Karl Thomae Benzimidazoles, drugs with this compounds, and process for their preparation
US5591762A (en) * 1991-02-06 1997-01-07 Dr. Karl Thomae Gmbh Benzimidazoles useful as angiotensin-11 antagonists
US5798364A (en) * 1992-03-26 1998-08-25 Merck Patent Gesellschaft Mit Beschrankter Haftung Imidazopyridines
EP0531874A1 (en) * 1991-09-10 1993-03-17 Tanabe Seiyaku Co., Ltd. Imidazopyridine derivatives and process for preparation thereof
EP0543263A3 (en) * 1991-11-16 1993-08-25 Dr. Karl Thomae Gmbh Benziimidazoles, pharmaceuticals containing them and process for their preparation
DE4219534A1 (en) * 1992-02-19 1993-12-16 Thomae Gmbh Dr K Substituted biphenylyl derivatives, pharmaceutical compositions containing them and methods for their preparation
DE4207904A1 (en) * 1992-03-12 1993-09-16 Thomae Gmbh Dr K SUBSTITUTED BENZIMIDAZOLYL DERIVATIVES, MEDICAMENTS CONTAINING SUCH COMPOUNDS AND METHOD FOR THE PRODUCTION THEREOF
DE4237656A1 (en) * 1992-06-13 1993-12-16 Merck Patent Gmbh benzimidazole derivatives
GB9218449D0 (en) 1992-08-29 1992-10-14 Boots Co Plc Therapeutic agents
DE4408497A1 (en) * 1994-03-14 1995-09-21 Thomae Gmbh Dr K Benzimidazoles, medicaments containing these compounds and process for their preparation
US5753672A (en) * 1994-04-19 1998-05-19 Tanabe Seiyaku Co., Ltd. Imidazopyridine derivatives and process for preparing the same
BR9508178A (en) * 1994-06-29 1997-11-18 Smithkline Beecham Corp Vitronectin receptor antagonists
ES2244979T3 (en) * 1995-12-28 2005-12-16 Fujisawa Pharmaceutical Co., Ltd. DERIVATIVES OF BENZIMIDAZOL.
TW453999B (en) 1997-06-27 2001-09-11 Fujisawa Pharmaceutical Co Benzimidazole derivatives
SE9903028D0 (en) 1999-08-27 1999-08-27 Astra Ab New use
DE10314702A1 (en) * 2003-03-31 2004-10-21 Boehringer Ingelheim Pharma Gmbh & Co. Kg Process for the preparation of telmisartan
ES2284068T3 (en) * 2003-10-16 2007-11-01 Teva Pharmaceutical Industries Limited PREPARATION OF CANDESARTAN CILEXETILO.
WO2006044648A1 (en) * 2004-10-15 2006-04-27 Teva Pharmaceutical Industries Ltd. Process for preparing telmisartan
US7879802B2 (en) 2007-06-04 2011-02-01 Synergy Pharmaceuticals Inc. Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
US8969514B2 (en) 2007-06-04 2015-03-03 Synergy Pharmaceuticals, Inc. Agonists of guanylate cyclase useful for the treatment of hypercholesterolemia, atherosclerosis, coronary heart disease, gallstone, obesity and other cardiovascular diseases
AU2009256157B2 (en) 2008-06-04 2014-12-18 Bausch Health Ireland Limited Agonists of guanylate cyclase useful for the treatment of gastrointestinal disorders, inflammation, cancer and other disorders
JP2011528375A (en) 2008-07-16 2011-11-17 シナジー ファーマシューティカルズ インコーポレイテッド Guanylate cyclase agonists useful for the treatment of gastrointestinal disorders, inflammation, cancer, and other disorders
US8829035B2 (en) 2009-05-29 2014-09-09 Sumitomo Chemical Company, Limited Agent for treatment or prevention of diseases associated with activity of neurotrophic factors
US9616097B2 (en) 2010-09-15 2017-04-11 Synergy Pharmaceuticals, Inc. Formulations of guanylate cyclase C agonists and methods of use
AU2014235209B2 (en) 2013-03-15 2018-06-14 Bausch Health Ireland Limited Guanylate cyclase receptor agonists combined with other drugs
JP2016514671A (en) 2013-03-15 2016-05-23 シナジー ファーマシューティカルズ インコーポレイテッド Guanylate cyclase agonists and uses thereof
AU2014274812B2 (en) 2013-06-05 2018-09-27 Bausch Health Ireland Limited Ultra-pure agonists of guanylate cyclase C, method of making and using same
ES2806135T3 (en) * 2013-06-21 2021-02-16 Zenith Epigenetics Ltd New bicyclic bromodomain inhibitors
US9636328B2 (en) 2013-06-21 2017-05-02 Zenith Epigenetics Ltd. Substituted bicyclic compounds as bromodomain inhibitors
CA2919948C (en) 2013-07-31 2020-07-21 Zenith Epigenetics Corp. Novel quinazolinones as bromodomain inhibitors
WO2016022312A1 (en) * 2014-08-05 2016-02-11 Bristol-Myers Squibb Company Heterocyclic kinase inhibitors
WO2016087936A1 (en) 2014-12-01 2016-06-09 Zenith Epigenetics Corp. Substituted pyridinones as bromodomain inhibitors
HK1245248B (en) 2014-12-11 2020-05-15 恒翼生物医药(上海)股份有限公司 Substituted heterocycles as bromodomain inhibitors
US10231953B2 (en) 2014-12-17 2019-03-19 Zenith Epigenetics Ltd. Inhibitors of bromodomains

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4820843A (en) * 1987-05-22 1989-04-11 E. I. Du Pont De Nemours And Company Tetrazole intermediates to antihypertensive compounds
US4880804A (en) * 1988-01-07 1989-11-14 E. I. Du Pont De Nemours And Company Angiotensin II receptor blocking benzimidazoles
EP0400835A1 (en) * 1989-05-15 1990-12-05 Merck & Co. Inc. Substituted benzimidazoles as angiotensin II antagonists
WO1991000281A2 (en) * 1989-06-30 1991-01-10 E.I. Du Pont De Nemours And Company Fused-ring aryl substituted imidazoles
IE70593B1 (en) * 1989-09-29 1996-12-11 Eisai Co Ltd Biphenylmethane derivative the use of it and pharmacological compositions containing same
IL95975A (en) * 1989-10-24 1997-06-10 Takeda Chemical Industries Ltd N-benzyl- 2-alkylbenzimidazole derivatives, their production and pharmaceutical compositions containing them
IL96019A0 (en) * 1989-10-31 1991-07-18 Fujisawa Pharmaceutical Co Imidazole derivatives,processes for the preparation thereof and pharmaceutical compositions containing the same

Cited By (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU637356B2 (en) * 1989-02-23 1993-05-27 British Bio-Technology Limited Novel benzimidazole derivatives
AU630431B2 (en) * 1989-03-15 1992-10-29 Janssen Pharmaceutica N.V. (5(6)-(benzisoxa-, benzisothia- or indazol-3-yl)-1H-benzimidazol-2-yl)carbamates
AU675433B2 (en) * 1991-02-06 1997-02-06 Dr. Karl Thomae Gmbh Benzimidazoles
AU661129B2 (en) * 1992-04-11 1995-07-13 Dr. Karl Thomae Gmbh Benzimidazoles
US5556981A (en) * 1992-06-03 1996-09-17 Eli Lilly And Company Angiotensin II antagonist intermediates
US5569768A (en) * 1992-06-03 1996-10-29 Eli Lilly And Company Angiotensin II antagonists
US5693633A (en) * 1992-06-03 1997-12-02 Eli Lilly And Company Angiotensin II antagonists
AU672262B2 (en) * 1993-02-15 1996-09-26 Bayer Aktiengesellschaft Heterocyclically substituted phenyl-cyclohexane-carboxylic acid derivatives

Also Published As

Publication number Publication date
HUT58298A (en) 1992-02-28
EP0468470A1 (en) 1992-01-29
CA2047496C (en) 2001-10-23
ES2100907T3 (en) 1997-07-01
JP2539113B2 (en) 1996-10-02
NZ239089A (en) 1994-07-26
IE912563A1 (en) 1992-01-29
PT98414A (en) 1992-05-29
CA2047496A1 (en) 1992-01-24
RU1836357C (en) 1993-08-23
FI105811B (en) 2000-10-13
ATE151766T1 (en) 1997-05-15
IL98933A (en) 1995-12-31
DK0468470T3 (en) 1997-09-22
JPH04253966A (en) 1992-09-09
FI913503A0 (en) 1991-07-22
NO178927C (en) 1996-07-03
FI913503A7 (en) 1992-01-24
DE59108658D1 (en) 1997-05-22
HU912456D0 (en) 1991-12-30
GR3024027T3 (en) 1997-10-31
NO178927B (en) 1996-03-25
EP0468470B1 (en) 1997-04-16
NO912859L (en) 1992-01-24
PT98414B (en) 1999-01-29
AU640505B2 (en) 1993-08-26
NO912859D0 (en) 1991-07-22
CS230491A3 (en) 1992-02-19
IL98933A0 (en) 1992-07-15

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