AU780009B2 - Heterocyclic compounds and methods of use thereof - Google Patents

Heterocyclic compounds and methods of use thereof Download PDF

Info

Publication number
AU780009B2
AU780009B2 AU69482/00A AU6948200A AU780009B2 AU 780009 B2 AU780009 B2 AU 780009B2 AU 69482/00 A AU69482/00 A AU 69482/00A AU 6948200 A AU6948200 A AU 6948200A AU 780009 B2 AU780009 B2 AU 780009B2
Authority
AU
Australia
Prior art keywords
substituted
unsubstituted
mmol
disorders
pain
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.)
Ceased
Application number
AU69482/00A
Other languages
English (en)
Other versions
AU6948200A (en
Inventor
Leo Solomon Bleicher
Nicholas D. P. Cosford
Rowena V. Cube
Stephen D. Hess
Ian A. Mcdonald
Benito Munoz
Edwin J. Schweiger
Mark A. Varney
Jean-Michel Vernier
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.)
Merck Sharp and Dohme LLC
Original Assignee
Merck and Co Inc
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 US09/387,135 external-priority patent/US6956049B1/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of AU6948200A publication Critical patent/AU6948200A/en
Application granted granted Critical
Publication of AU780009B2 publication Critical patent/AU780009B2/en
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK & CO., INC.
Assigned to MERCK SHARP & DOHME CORP. reassignment MERCK SHARP & DOHME CORP. Request to Amend Deed and Register Assignors: MERCK SHARP & DOHME CORP.
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/28—Radicals substituted by singly-bound oxygen or sulphur atoms
    • C07D213/30—Oxygen atoms
    • 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
    • A61P1/14—Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/28—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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/34—Tobacco-abuse
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/06—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom
    • C07D213/16—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom containing only hydrogen and carbon atoms in addition to the ring nitrogen atom containing only one pyridine ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/22—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D277/24—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D277/38—Nitrogen atoms
    • C07D277/40—Unsubstituted amino or imino radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
    • C07D285/01—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/06—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to the ring carbon atoms
    • C07D333/08—Hydrogen atoms or radicals containing only hydrogen and carbon atoms

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pulmonology (AREA)
  • Immunology (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Urology & Nephrology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Ophthalmology & Optometry (AREA)
  • Psychology (AREA)
  • Obesity (AREA)
  • Dermatology (AREA)
  • Transplantation (AREA)
  • Diabetes (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Cardiology (AREA)
  • Nutrition Science (AREA)
AU69482/00A 1999-08-31 2000-08-31 Heterocyclic compounds and methods of use thereof Ceased AU780009B2 (en)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US38707399A 1999-08-31 1999-08-31
US09/387135 1999-08-31
US09/387,135 US6956049B1 (en) 1999-08-31 1999-08-31 Methods of modulating processes mediated by excitatory amino acid receptors
US09/387073 1999-08-31
PCT/US2000/023923 WO2001016121A1 (en) 1999-08-31 2000-08-31 Heterocyclic compounds and methods of use thereof

Publications (2)

Publication Number Publication Date
AU6948200A AU6948200A (en) 2001-03-26
AU780009B2 true AU780009B2 (en) 2005-02-24

Family

ID=27011738

Family Applications (1)

Application Number Title Priority Date Filing Date
AU69482/00A Ceased AU780009B2 (en) 1999-08-31 2000-08-31 Heterocyclic compounds and methods of use thereof

Country Status (5)

Country Link
EP (1) EP1214303A1 (de)
JP (2) JP4815083B2 (de)
AU (1) AU780009B2 (de)
CA (1) CA2383524C (de)
WO (1) WO2001016121A1 (de)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7462619B2 (en) 1999-08-31 2008-12-09 Merck & Co., Inc. Pyridazine, pyrimidine and pyrazine ethyne compounds
EP1214303A1 (de) * 1999-08-31 2002-06-19 Merck & Co., Inc. Heterozyklische verbindungen und methode zu ihrer verwendung
US6774138B2 (en) * 1999-08-31 2004-08-10 Merck & Co., Inc. Thiazolyl(pyridyl)ethyne compounds
US7365074B2 (en) 1999-08-31 2008-04-29 Merck & Co., Inc. Pyridazine, pyrimidine and pyrazine ethyne compounds
EP1349839B8 (de) * 2000-12-04 2005-06-22 F. Hoffmann-La Roche Ag Phenylethenyl- oder phenylethinylderivate als glutamatrezeptorantagonisten
JP2005524712A (ja) 2002-05-07 2005-08-18 ニューロサーチ、アクティーゼルスカブ 新規アザシクロエチニル誘導体
EP1556142A4 (de) * 2002-10-24 2006-11-08 Merck & Co Inc Alkyn-derivate als tracer für die metabotrope glutamat-rezeptor-bindung
EP1602645A4 (de) 2003-03-07 2008-12-03 Astellas Pharma Inc Stickstoffhaltiges heterocyclisches derivat mit 2,6-disubstituiertem styrylrest
TWI292318B (en) 2003-03-10 2008-01-11 Hoffmann La Roche Imidazol-4-yl-ethynyl-pyridine derivatives
US7531529B2 (en) 2003-06-05 2009-05-12 Roche Palo Alto Llc Imidazole derivatives
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
JP4395512B2 (ja) 2003-06-12 2010-01-13 エフ．ホフマン−ラ ロシュ アーゲー グルタミン酸受容体アンタゴニストであるヘテロアリール置換イミダゾール誘導体
US7452909B2 (en) * 2003-09-04 2008-11-18 Hoffman-La Roche Inc. Imidazole derivatives
GB0322612D0 (en) * 2003-09-26 2003-10-29 Novartis Ag Organic compounds
WO2005044266A1 (en) * 2003-10-31 2005-05-19 Astrazeneca Ab Alkynes i
CA2549965A1 (en) * 2003-10-31 2005-05-19 Astrazeneca Ab Alkynes iii
JP2007509935A (ja) * 2003-10-31 2007-04-19 アストラゼネカ アクチボラグ アルキンズｉｉ
EP1721905A4 (de) * 2004-03-05 2009-11-18 Taisho Pharmaceutical Co Ltd Thiazolderivat
EP1729771B1 (de) 2004-03-22 2009-10-14 Eli Lilly & Company Pyridyl-derivate und ihre verwendung als mglu5-rezeptorantagonisten
KR101057032B1 (ko) * 2004-06-01 2011-08-16 에프. 호프만-라 로슈 아게 Ｍｇｌｕ5 수용체 길항제로서 피리딘-4-일-에틴일-이미다졸및 피라졸
EP1756086B1 (de) * 2004-06-01 2008-06-04 F.Hoffmann-La Roche Ag Pyridin-4-yl-ethynylimidazole und -pyrazole als antagonisten des mglu5-rezeptors
GB0413605D0 (en) 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
EP1893608B1 (de) * 2004-10-07 2011-08-17 Merck Sharp & Dohme Corp. Thiazolyl-mglur5-antagonisten und verfahren zu ihrer verwendung
RS54853B1 (sr) 2006-12-21 2016-10-31 Hoffmann La Roche Polimorfi antagonista mglur5 receptora
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
TWI538905B (zh) * 2010-12-22 2016-06-21 Ｈ 朗德貝克公司 雙環［３．２．１］辛基醯胺衍生物及其用途
MX343701B (es) * 2011-12-23 2016-11-16 Crystal Pharma Sau Procedimiento para alquinilar 17-cetoesteroides 16-sustituidos.
EP2953933A1 (de) * 2013-02-07 2015-12-16 Merck Patent GmbH Substituierte acetylenderivate und deren verwendung als positive allosterische modulatoren von mglur4
CN106146391A (zh) * 2015-04-15 2016-11-23 中国科学院上海药物研究所 5-芳香炔基取代的苯甲酰胺类化合物及其制备方法、药物组合物和用途
PT3303316T (pt) 2015-06-03 2020-04-27 Hoffmann La Roche Derivados de etinilo
JP2019081709A (ja) * 2016-03-18 2019-05-30 石原産業株式会社 有害生物防除剤

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996003406A1 (en) * 1994-07-28 1996-02-08 Agouron Pharmaceuticals, Inc. Compounds useful as antiproliferative agents and garft inhibitors
WO1999002497A2 (en) * 1997-07-11 1999-01-21 Novartis Ag Pyridine derivatives

Family Cites Families (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3705153A (en) * 1969-05-14 1972-12-05 Sumitomo Chemical Co Novel thiazolyacetic acids and salts thereof
DE2426878A1 (de) * 1974-06-04 1976-01-08 Basf Ag Verfahren zur herstellung von 1,2,4oxadiazolen
JPS58219169A (ja) * 1982-06-15 1983-12-20 Takeda Chem Ind Ltd オキサゾ−ル酢酸誘導体
JPS62142168A (ja) * 1985-10-16 1987-06-25 Mitsubishi Chem Ind Ltd チアゾ−ル誘導体及びそれを有効成分とするロイコトリエンきつ抗剤
JP2745073B2 (ja) * 1989-10-27 1998-04-28 チッソ株式会社 フェニルアセチレン化合物
FR2663850B1 (fr) * 1990-07-02 1994-01-14 Gird Galderma Composition pharmaceutique ou cosmetique contenant en association un retinouide et un sterol.
DE4023742A1 (de) * 1990-07-26 1992-01-30 Gruenenthal Gmbh Substituierte phenylacetylene, diese enthaltende arzneimittel und verfahren zur herstellung dieser verbindungen und arzneimittel
US5270312A (en) * 1990-11-05 1993-12-14 Warner-Lambert Company Substituted piperazines as central nervous system agents
JP3899126B2 (ja) * 1995-01-06 2007-03-28 ターガセプト，インコーポレイテッド 中枢神経系疾患の予防及び治療のための医薬組成物
WO1997009311A1 (de) * 1995-09-07 1997-03-13 F. Hoffmann-La Roche Ag Neue 4-(oxyalkoxyphenyl)-3-oxy-piperidine zur behandlung von herz- und niereninsuffizienz
JPH09235276A (ja) * 1995-12-27 1997-09-09 Takeda Chem Ind Ltd オキサゾール誘導体、その製造法および用途
JP4056589B2 (ja) * 1996-07-19 2008-03-05 武田薬品工業株式会社 複素環化合物、その製造法および用途
ZA986594B (en) * 1997-07-25 1999-01-27 Abbott Lab Urokinase inhibitors
EP1020445B1 (de) * 1997-10-02 2008-08-13 Eisai R&D Management Co., Ltd. Kondensierte pyridinderivate
US6187777B1 (en) * 1998-02-06 2001-02-13 Amgen Inc. Compounds and methods which modulate feeding behavior and related diseases
JP2000119253A (ja) * 1998-08-11 2000-04-25 Dai Ichi Seiyaku Co Ltd 新規なスルホニル誘導体
EP1214303A1 (de) * 1999-08-31 2002-06-19 Merck & Co., Inc. Heterozyklische verbindungen und methode zu ihrer verwendung

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1996003406A1 (en) * 1994-07-28 1996-02-08 Agouron Pharmaceuticals, Inc. Compounds useful as antiproliferative agents and garft inhibitors
WO1999002497A2 (en) * 1997-07-11 1999-01-21 Novartis Ag Pyridine derivatives

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BRIT J PHARMACOL. 126, SUPPL PROC, MARCH 1999, P 249 *

Also Published As

Publication number Publication date
WO2001016121A1 (en) 2001-03-08
AU6948200A (en) 2001-03-26
JP4815083B2 (ja) 2011-11-16
JP2011098969A (ja) 2011-05-19
CA2383524C (en) 2010-09-28
CA2383524A1 (en) 2001-03-08
JP2003508390A (ja) 2003-03-04
EP1214303A1 (de) 2002-06-19

Similar Documents

Publication Publication Date Title
AU780009B2 (en) Heterocyclic compounds and methods of use thereof
AU2008319308B2 (en) P2X3, receptor antagonists for treatment of pain
US6774138B2 (en) Thiazolyl(pyridyl)ethyne compounds
JP3295143B2 (ja) ベンズアニリド誘導体
CN102993084B (zh) 作为促代谢谷氨酸受体的调节剂的新型炔基衍生物
JP2005533858A (ja) 化合物
JP5635727B2 (ja) チアゾリルｍｇｌｕｒ５アンタゴニスト及びそれらの使用のための方法
US6956049B1 (en) Methods of modulating processes mediated by excitatory amino acid receptors
AU2002365892A1 (en) Metabotropic glutamate receptor-5 modulators
BG103686A (bg) Тиазолови бензенсулфонамиди като бета3 агонисти за лечението на диабет и затлъстяване
JPH10510512A (ja) 尿素誘導体とａｃａｔ阻害剤としての用途
KR20050085790A (ko) 11-베타-하이드록시스테로이드 탈수소효소-1 억제제로서의트리아졸 유도체
JP2002541253A (ja) トリアリールイミダゾール
JP2006523701A (ja) ナトリウムチャネルブロッカーとしてのビアリール置換チアゾール、オキサゾール、およびイミダゾール
JP2017522277A (ja) 代謝型グルタミン酸受容体の負のアロステリックモジュレーター（ｎａｍｓ）とその使用
WO2007037543A1 (ja) ビアリールアミド誘導体
JP2004532856A (ja) アポリポタンパク質ｂ阻害剤としてのビアリールカルボキサミド化合物
JP2011006408A (ja) 神経栄養因子の活性が関与する疾患の治療または予防剤
WO2007062193A1 (en) Heterocycle-substituted 3-alkyl azetidine derivatives
US10954228B2 (en) 1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
SK35198A3 (en) Heteroaryl-substituted acryloylguanidine derivatives and medicinal composition thereof
JP2012500223A (ja) Ｍａｐキナーゼインヒビターとしての尿素誘導体
JP2005513018A (ja) Ａｌｋ５阻害剤としてのチアゾリル置換トリアゾール類
US20030073862A1 (en) Compounds
US7365074B2 (en) Pyridazine, pyrimidine and pyrazine ethyne compounds