ATE296809T1 - 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren - Google Patents

3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren

Info

Publication number
ATE296809T1
ATE296809T1 AT00980587T AT00980587T ATE296809T1 AT E296809 T1 ATE296809 T1 AT E296809T1 AT 00980587 T AT00980587 T AT 00980587T AT 00980587 T AT00980587 T AT 00980587T AT E296809 T1 ATE296809 T1 AT E296809T1
Authority
AT
Austria
Prior art keywords
csbp
kinase inhibitors
compounds
chinazoline
dihydro
Prior art date
Application number
AT00980587T
Other languages
English (en)
Inventor
Jerry L Adams
Michael J Bower
Jeffrey Charles Boehm
Don E Griswold
David C Underwood
Original Assignee
Smithkline Beecham Corp
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 Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Application granted granted Critical
Publication of ATE296809T1 publication Critical patent/ATE296809T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/78—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80—Oxygen atoms
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
    • 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
    • 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
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • 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
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/06—Antigout agents, e.g. antihyperuricemic or uricosuric agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • 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
    • A61P25/28—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
    • 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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/16—Antivirals for RNA viruses for influenza or rhinoviruses
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/04—Antineoplastic agents specific for metastasis
    • 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
    • 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
    • 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
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • 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
    • A61P9/10—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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
    • Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
    • Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Diabetes (AREA)
  • Pulmonology (AREA)
  • Virology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Communicable Diseases (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pain & Pain Management (AREA)
  • Cardiology (AREA)
  • Endocrinology (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Molecular Biology (AREA)
  • Psychiatry (AREA)
AT00980587T 1999-11-23 2000-11-21 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren ATE296809T1 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US16697599P 1999-11-23 1999-11-23
PCT/US2000/031894 WO2001038314A1 (en) 1999-11-23 2000-11-21 3,4-dihydro-(1h)quinazolin-2-one compounds as csbp/p38 kinase inhibitors

Publications (1)

Publication Number Publication Date
ATE296809T1 true ATE296809T1 (de) 2005-06-15

Family

ID=22605428

Family Applications (1)

Application Number Title Priority Date Filing Date
AT00980587T ATE296809T1 (de) 1999-11-23 2000-11-21 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren

Country Status (8)

Country Link
US (1) US7053098B1 (de)
EP (1) EP1233951B1 (de)
JP (1) JP2003514900A (de)
AT (1) ATE296809T1 (de)
AU (1) AU1783201A (de)
DE (1) DE60020595T2 (de)
ES (1) ES2241675T3 (de)
WO (1) WO2001038314A1 (de)

Families Citing this family (25)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU1909200A (en) 1998-11-04 2000-05-22 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
DE60023025T2 (de) 1999-11-23 2006-07-13 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
JP2003517471A (ja) * 1999-11-23 2003-05-27 スミスクライン・ビーチャム・コーポレイション ３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オンおよびそのＣＳＢＰ／ｐ３８キナーゼ阻害剤としての使用
EP1235814B1 (de) 1999-11-23 2004-11-03 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)CHINAZOLIN-2-ON-VERBINDUNGEN ALS CSBP/p38-KINASE-INHIBITOREN
EP1233951B1 (de) 1999-11-23 2005-06-01 SmithKline Beecham Corporation 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
US7235551B2 (en) 2000-03-02 2007-06-26 Smithkline Beecham Corporation 1,5-disubstituted-3,4-dihydro-1h-pyrimido[4,5-d]pyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
AUPR213700A0 (en) 2000-12-18 2001-01-25 Biota Scientific Management Pty Ltd Antiviral agents
WO2004004725A2 (en) 2002-07-09 2004-01-15 Boehringer Ingelheim Pharma Gmbh & Co. Kg Pharmaceutical compositions of anticholinergics and p38 kinase inhibitors in the treatment of respiratory diseases
US8436006B2 (en) 2004-08-06 2013-05-07 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8383637B2 (en) 2004-08-06 2013-02-26 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US8426429B2 (en) 2004-08-06 2013-04-23 Jansssen Pharmaceutica N.V. 2-amino-quinazoline derivatives useful as inhibitors of β-secretase (BACE)
US20060035893A1 (en) 2004-08-07 2006-02-16 Boehringer Ingelheim International Gmbh Pharmaceutical compositions for treatment of respiratory and gastrointestinal disorders
PE20060777A1 (es) 2004-12-24 2006-10-06 Boehringer Ingelheim Int Derivados de indolinona para el tratamiento o la prevencion de enfermedades fibroticas
WO2006137421A1 (ja) * 2005-06-21 2006-12-28 Kyowa Hakko Kogyo Co., Ltd. 局所投与剤
ES2360957T3 (es) 2005-10-25 2011-06-10 Janssen Pharmaceutica Nv Derivados de 2-amino-3,4-dihidro-pirido(3,4-d)-pirimidina utiles como inhibidores de la beta-secretasa (bace).
US7868022B2 (en) 2006-02-06 2011-01-11 Janssen Pharmaceutica Nv 2-amino-quinoline derivatives useful as inhibitors of β-secretase (BACE)
WO2007092846A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. 2-AMINO-3,4-DIHYDRO-QUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF β-SECRETASE (BACE)
WO2007092839A2 (en) 2006-02-06 2007-08-16 Janssen Pharmaceutica N.V. Macrocycle derivatives useful as inhibitors of beta-secretase (bace)
WO2008011032A1 (en) 2006-07-17 2008-01-24 Amgen Inc. Quinazoline and pyridopyrimidine derivatives as p38 kinase inhibitors
EP1992344A1 (de) 2007-05-18 2008-11-19 Institut Curie P38 Alpha als therapeutisches Target für Erkrankungen, die mit einer FGFR3- Mutation assoziiert sind
EP2238111B1 (de) 2008-01-28 2013-01-16 Janssen Pharmaceutica NV Als beta-sekretase (bace)-hemmer geeignete 6-substituierte thio-2-amino-chinolinderivate
US8916704B1 (en) 2013-10-02 2014-12-23 King Fahd University Of Petroleum And Minerals Dihydroquinone derivatives of piperidine and piperazine
US20190060286A1 (en) 2016-02-29 2019-02-28 University Of Florida Research Foundation, Incorpo Chemotherapeutic Methods
NZ762856A (en) 2017-10-05 2020-07-31 Fulcrum Therapeutics Inc P38 kinase inhibitors reduce dux4 and downstream gene expression for the treatment of fshd
US10342786B2 (en) 2017-10-05 2019-07-09 Fulcrum Therapeutics, Inc. P38 kinase inhibitors reduce DUX4 and downstream gene expression for the treatment of FSHD

Family Cites Families (148)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2833779A (en) 1956-10-29 1958-05-06 American Cyanamid Co Substituted pyrazoles
US3707475A (en) 1970-11-16 1972-12-26 Pfizer Antiinflammatory imidazoles
US3929807A (en) 1971-05-10 1975-12-30 Ciba Geigy Corp 2-Substituted-4(5)-(aryl)-5(4)-(2,3 or -4-pyridyl)-imidazoles
US3940486A (en) 1971-05-10 1976-02-24 Ciba-Geigy Corporation Imidazole derivatives in the treatment of pain
US3703475A (en) 1971-06-21 1972-11-21 Continental Oil Co Preparation of oil soluble sulfonic acids useful as dispersant additives
US4058614A (en) 1973-12-04 1977-11-15 Merck & Co., Inc. Substituted imidazole compounds and therapeutic compositions therewith
US4199592A (en) 1978-08-29 1980-04-22 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl-2-nitroimidazoles
CA1175431A (en) 1980-07-25 1984-10-02 Alfred Sallmann Tri-substituted imidazole derivatives, processes for their manufacture, pharmaceutical preparations containing them, and their use
GB2123831B (en) 1981-07-20 1986-01-15 Ciba Geigy Ag Trisubstituted oxazo compounds
US4503065A (en) 1982-08-03 1985-03-05 E. I. Du Pont De Nemours And Company Antiinflammatory 4,5-diaryl 1-2-halo imidazoles
JPS60226882A (ja) 1984-04-24 1985-11-12 Nippon Zoki Pharmaceut Co Ltd 新規ピリミドピリミジン誘導体
US4565875A (en) 1984-06-27 1986-01-21 Fmc Corporation Imidazole plant growth regulators
US4686231A (en) 1985-12-12 1987-08-11 Smithkline Beckman Corporation Inhibition of 5-lipoxygenase products
IL83467A0 (en) 1986-08-15 1988-01-31 Fujisawa Pharmaceutical Co Imidazole derivatives,processes for their preparation and pharmaceutical compositions containing the same
KR930700104A (ko) 1990-06-12 1993-03-13 원본미기재 5-리프옥시게나제 및 사이클로옥시게나제 경로 개재된 질병의 억제
FR2665898B1 (fr) 1990-08-20 1994-03-11 Sanofi Derives d'amido-3 pyrazole, procede pour leur preparation et compositions pharmaceutiques les contenant.
IE913473A1 (en) 1990-10-15 1992-04-22 Fujisawa Pharmaceutical Co Quinazoline derivatives and their preparation
JPH06504779A (ja) 1990-12-13 1994-06-02 スミスクライン・ビーチャム・コーポレイション 新規ｃｓａｉｄｓ
AU9169991A (en) 1990-12-13 1992-07-08 Smithkline Beecham Corporation Novel csaids
JPH06502178A (ja) 1990-12-31 1994-03-10 藤沢薬品工業株式会社 イミダゾトリアジン誘導体
JP3375659B2 (ja) 1991-03-28 2003-02-10 テキサス インスツルメンツ インコーポレイテツド 静電放電保護回路の形成方法
IL102764A0 (en) 1991-08-16 1993-01-31 Merck & Co Inc Quinazoline derivatives,and pharmaceutical compositions containing them
GB9816837D0 (en) 1998-08-04 1998-09-30 Zeneca Ltd Amide derivatives
EP0624159B1 (de) 1992-01-13 1998-11-25 Smithkline Beecham Corporation Pyridyl-substituierte imidazole
US5716972A (en) 1993-01-13 1998-02-10 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US6008235A (en) 1992-01-13 1999-12-28 Smithkline Beecham Corporation Pyridyl substituted imidazoles
US5916891A (en) 1992-01-13 1999-06-29 Smithkline Beecham Corporation Pyrimidinyl imidazoles
US5656644A (en) 1994-07-20 1997-08-12 Smithkline Beecham Corporation Pyridyl imidazoles
IL104369A0 (en) 1992-01-13 1993-05-13 Smithkline Beecham Corp Novel compounds and compositions
GB9303993D0 (en) 1993-02-26 1993-04-14 Fujisawa Pharmaceutical Co New heterocyclic derivatives
US5593992A (en) 1993-07-16 1997-01-14 Smithkline Beecham Corporation Compounds
US5670527A (en) 1993-07-16 1997-09-23 Smithkline Beecham Corporation Pyridyl imidazole compounds and compositions
US5593991A (en) 1993-07-16 1997-01-14 Adams; Jerry L. Imidazole compounds, use and process of making
IL110296A (en) 1993-07-16 1999-12-31 Smithkline Beecham Corp Imidazole compounds process for their preparation and pharmaceutical compositions containing them
WO1995003297A1 (en) 1993-07-21 1995-02-02 Smithkline Beecham Corporation Imidazoles for treating cytokine mediated disease
DK0724588T3 (da) 1993-09-17 2000-05-15 Smithkline Beecham Corp Lægemiddelbindende protein
US5869043A (en) 1993-09-17 1999-02-09 Smithkline Beecham Corporation Drug binding protein
US5783664A (en) 1993-09-17 1998-07-21 Smithkline Beecham Corporation Cytokine suppressive anit-inflammatory drug binding proteins
US5705502A (en) 1993-10-01 1998-01-06 Novartis Corporation Pharmacologically active pyrimidineamine derivatives and processes for the preparation thereof
US5543520A (en) 1993-10-01 1996-08-06 Ciba-Geigy Corporation Pyrimidine derivatives
ES2167377T3 (es) 1993-10-01 2002-05-16 Novartis Ag Derivados de piridina farmacologicamente activos y procedimientos para la preparacion de los mismos.
CA2148931A1 (en) 1993-10-01 1995-04-13 Jurg Zimmermann Pyrimidineamine derivatives and processes for the preparation thereof
AU1046895A (en) * 1993-11-05 1995-05-23 Merck & Co., Inc. New quinazolines as inhibitors of hiv reverse transcriptase
EP0727998B1 (de) 1993-11-08 2004-01-21 Smithkline Beecham Corporation Oxazole zur behandlung von zytokinvermittelten erkrankungen
US5559137A (en) 1994-05-16 1996-09-24 Smithkline Beecham Corp. Compounds
US5545669A (en) 1994-06-02 1996-08-13 Adams; Jerry L. Anti-inflammatory compounds
AU709370B2 (en) 1995-01-12 1999-08-26 Smithkline Beecham Corporation Novel compounds
US5658903A (en) * 1995-06-07 1997-08-19 Smithkline Beecham Corporation Imidazole compounds, compositions and use
US5739143A (en) 1995-06-07 1998-04-14 Smithkline Beecham Corporation Imidazole compounds and compositions
CA2228136A1 (en) 1995-08-10 1997-02-20 Merck & Co., Inc. 2-substituted aryl pyrroles, compositions containing such compounds and methods of use
WO1997005878A1 (en) 1995-08-10 1997-02-20 Merck & Co., Inc. 2,5-substituted aryl pyrroles, compositions containing such compounds and methods of use
AU702146B2 (en) 1995-10-06 1999-02-11 Merck & Co., Inc. Substituted imidazoles having anti-cancer and cytokine inhibitory activity
AU7529096A (en) 1995-10-31 1997-05-22 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
WO1997016441A1 (en) 1995-10-31 1997-05-09 Merck & Co., Inc. Substituted aryl pyrroles, compositions containing such compounds and methods of use
WO1997016442A1 (en) 1995-10-31 1997-05-09 Merck & Co., Inc. Substituted pyridyl pyrroles, compositions containing such compounds and methods of use
ZA9610687B (en) 1995-12-22 1997-09-29 Smithkline Beecham Corp Novel synthesis.
AP9700912A0 (en) 1996-01-11 1997-01-31 Smithkline Beecham Corp Novel cycloalkyl substituted imidazoles
ZA97175B (en) 1996-01-11 1997-11-04 Smithkline Beecham Corp Novel substituted imidazole compounds.
CN1213306A (zh) 1996-01-11 1999-04-07 史密丝克莱恩比彻姆公司 新的取代咪唑化合物
EP0883402A4 (de) 1996-01-11 1999-08-11 Smithkline Beecham Corp Neue cycloalkyl substituierte imidazole
JP2000507224A (ja) 1996-03-08 2000-06-13 スミスクライン・ビーチャム・コーポレイション Ｃｓａｉｄ化合物の血管形成の抑制物質としての使用
EP0888335A4 (de) * 1996-03-13 2002-01-02 Smithkline Beecham Corp Neue pyrimidinverbindungen und ihre anwendung in der behandlung, von cytokinin-vermittler krankheiten
EP0889887A4 (de) 1996-03-25 2003-06-11 Smithkline Beecham Corp Behandlung von verletzungen des zentralen nervensystems
EP0889888A4 (de) 1996-03-25 2003-01-08 Smithkline Beecham Corp Behandlung von verletzungen des zentralen nervensystems
EP0906099A4 (de) 1996-04-03 2001-02-07 Merck & Co Inc Verfahren zur behandlung von krebs
US6875769B2 (en) 1996-05-23 2005-04-05 Pfizer Inc. Substituted6,6-hetero-bicyclicderivatives
EP0906307B1 (de) 1996-06-10 2005-04-27 Merck & Co., Inc. Substituierte imidazole mit cytokinin-inhibirender wirkung
EE03680B1 (et) 1996-07-18 2002-04-15 Merck Frosst Canada & Co. / Merck Frosst Canada &Cie. Asendatud püridiinid, nende kasutamine ja farmatseutilised kompositsioonid
JP2001506230A (ja) 1996-08-09 2001-05-15 スミスクライン・ビーチャム・コーポレイション 新規ピペラジン含有化合物
EP0956018A4 (de) 1996-08-21 2000-01-12 Smithkline Beecham Corp Imidazolverbindungen, deren zusammensetzungen und verwendung
WO1998016230A1 (en) 1996-10-17 1998-04-23 Smithkline Beecham Corporation Methods for reversibly inhibiting myelopoiesis in mammalian tissue
CN1246856A (zh) 1996-11-19 2000-03-08 安姆根有限公司 芳基和杂芳基取代的稠合吡咯抗炎药
JP2000514088A (ja) 1996-11-20 2000-10-24 メルク エンド カンパニー インコーポレーテッド グルカゴンアンタゴニストとしてのトリアリール置換イミダゾール
JP2002514196A (ja) 1996-12-05 2002-05-14 アムジエン・インコーポレーテツド 置換ピリミジノンおよびピリドン化合物ならびに使用方法
ZA9711092B (en) 1996-12-11 1999-07-22 Smithkline Beecham Corp Novel compounds.
US6147080A (en) 1996-12-18 2000-11-14 Vertex Pharmaceuticals Incorporated Inhibitors of p38
US5929076A (en) 1997-01-10 1999-07-27 Smithkline Beecham Corporation Cycloalkyl substituted imidazoles
HUP0002842A3 (en) 1997-04-24 2002-01-28 Ortho Mcneil Pharm Inc Substituted imidazoles, process for producing them, pharmaceutical compositions containing them, their use and their intermediates
MA26487A1 (fr) 1997-04-29 2004-12-20 Smithkline Beecham Corp Heterocyclecetohydrazides inhibiteurs de proteases, procede pour leur preparation et compositions pharmaceutiques les contenant .
JP2002502380A (ja) 1997-05-22 2002-01-22 ジー．ディー．サール アンド カンパニー ｐ３８キナーゼ阻害剤としてのピラゾール誘導体
PL336990A1 (en) 1997-05-22 2000-07-31 Searle & Co 3(5)-heteroaryl group substituted pyrazoles as inhibitors of kinase p 38
US6514977B1 (en) 1997-05-22 2003-02-04 G.D. Searle & Company Substituted pyrazoles as p38 kinase inhibitors
IL132991A (en) 1997-05-22 2005-11-20 Searle & Co Substituted pyrazoles, pharmaceutical compositionscomprising them and their use as p38 inase inhibi tors
WO1998052558A1 (en) 1997-05-23 1998-11-26 Bayer Corporation INHIBITION OF p38 KINASE ACTIVITY BY ARYL UREAS
ATE335735T1 (de) 1997-06-12 2006-09-15 Aventis Pharma Ltd Imidazolyl-cyclische acetale
US20020156104A1 (en) 1997-06-13 2002-10-24 Jerry L. Adams Novel pyrazole and pyrazoline substituted compounds
CA2294137A1 (en) 1997-06-19 1998-12-23 Smithkline Beecham Corporation Novel aryloxy substituted pyrimidine imidazole compounds
US6093742A (en) 1997-06-27 2000-07-25 Vertex Pharmaceuticals, Inc. Inhibitors of p38
GB9713726D0 (en) 1997-06-30 1997-09-03 Ciba Geigy Ag Organic compounds
CA2295021A1 (en) 1997-06-30 1999-01-28 Ortho-Mcneil Pharmaceutical, Inc. 2-substituted imidazoles useful in the treatment of inflammatory diseases
TW517055B (en) 1997-07-02 2003-01-11 Smithkline Beecham Corp Novel substituted imidazole compounds
AU8381098A (en) 1997-07-02 1999-01-25 Smithkline Beecham Corporation Novel cycloalkyl substituted imidazoles
AR016294A1 (es) 1997-07-02 2001-07-04 Smithkline Beecham Corp Compuesto de imidazol sustituido, composicion farmaceutica que la contiene, su uso en la fabricacion de un medicamento y procedimiento para supreparacion
US6362193B1 (en) 1997-10-08 2002-03-26 Smithkline Beecham Corporation Cycloalkenyl substituted compounds
WO1999018942A1 (en) 1997-10-10 1999-04-22 Imperial College Innovations Ltd. Use of csaidtm compounds for the management of uterine contractions
JP2002515891A (ja) * 1997-12-19 2002-05-28 スミスクライン・ビーチャム・コーポレイション 新規なピペリジン含有化合物
AU1924699A (en) 1997-12-19 1999-07-12 Smithkline Beecham Corporation Compounds of heteroaryl substituted imidazole, their pharmaceutical compositionsand uses
ES2155817T3 (es) 1997-12-22 2007-06-16 Bayer Pharmaceuticals Corp. Inhibicion de la actividad de la quinasa p38 utilizando ureas heterociclicas sustituidas con arilo y heteroarilo.
US6162613A (en) 1998-02-18 2000-12-19 Vertex Pharmaceuticals, Inc. Methods for designing inhibitors of serine/threonine-kinases and tyrosine kinases
JP2002513562A (ja) 1998-05-04 2002-05-14 バーテックス ファーマシューティカルズ インコーポレイテッド 結晶化可能なｊｎｋ複合体
IL139169A0 (en) 1998-05-05 2001-11-25 Hoffmann La Roche Pyrazole derivatives as p-38 map kinase inhibitors
GB9809869D0 (en) 1998-05-09 1998-07-08 Medical Res Council Inhibition of protein kinases
MY132496A (en) 1998-05-11 2007-10-31 Vertex Pharma Inhibitors of p38
EP1077971A1 (de) 1998-05-14 2001-02-28 G.D. SEARLE & CO. Substituierte 1,5-diarylpyrazole als p38 kinase inhibitoren
ID26236A (id) 1998-05-15 2000-12-07 Astrazeneca Ab Turunan benzamida untuk pengobatan penyakit yang diperantarai oleh sitokina
CA2328699A1 (en) 1998-05-15 1999-11-25 Dearg Sutherland Brown Benzamide derivatives for the treatment of diseases mediated by cytokines
KR20010025087A (ko) 1998-05-22 2001-03-26 스튜어트 알. 수터 신규한 2-알킬 치환된 이미다졸 화합물
DE69929689T2 (de) 1998-05-22 2006-11-02 Scios Inc., Fremont Heterocyclische Verbindungen und Verfahren zur Behandlung von Herzversagen und anderer Erkrankungen
JP2002516325A (ja) 1998-05-26 2002-06-04 スミスクライン・ビーチャム・コーポレイション 新規な置換イミダゾール化合物
EP1086085A1 (de) * 1998-06-12 2001-03-28 Vertex Pharmaceuticals Incorporated P38 inhibitoren
AU4395399A (en) 1998-07-02 2000-01-24 Sankyo Company Limited Five-membered heteroaryl compounds
US6207687B1 (en) 1998-07-31 2001-03-27 Merck & Co., Inc. Substituted imidazoles having cytokine inhibitory activity
MXPA01000895A (es) 1998-08-04 2002-08-20 Astrazeneca Ab Derivados de amida utiles como inhibidores de la produccion de citocinas.
WO2000010563A1 (en) 1998-08-20 2000-03-02 Smithkline Beecham Corporation Novel substituted triazole compounds
AU772477B2 (en) 1998-08-28 2004-04-29 Scios Inc. Inhibitors of p38-alpha kinase
US6184226B1 (en) 1998-08-28 2001-02-06 Scios Inc. Quinazoline derivatives as inhibitors of P-38 α
JP2002526482A (ja) 1998-09-18 2002-08-20 バーテックス ファーマシューティカルズ インコーポレイテッド ｐ３８のインヒビター
ATE254105T1 (de) 1998-09-25 2003-11-15 Astrazeneca Ab Benzamid-derivate und ihre verwendung als cytokine inhibitoren
JP2002526538A (ja) 1998-10-01 2002-08-20 アストラゼネカ アクチボラグ 化学化合物
JP2002526388A (ja) 1998-10-07 2002-08-20 スミスクライン・ビーチャム・コーポレイション 発作を管理するための新規な処置
AU1127700A (en) 1998-10-20 2000-05-08 Omeros Medical Systems, Inc. Irrigation solution containing mapk inhibitors and their use for treating pain and inflammation
NZ510760A (en) 1998-10-23 2003-08-29 F Bicyclic nitrogen heterocycles
WO2000026209A1 (en) 1998-11-03 2000-05-11 Novartis Ag Anti-inflammatory 4-phenyl-5-pyrimidinyl-imidazoles
AU1909200A (en) 1998-11-04 2000-05-22 Smithkline Beecham Corporation Pyridin-4-yl or pyrimidin-4-yl substituted pyrazines
US6350744B1 (en) 1998-11-20 2002-02-26 Merck & Co., Inc. Compounds having cytokine inhibitory activity
DK1131318T3 (da) 1998-11-20 2004-06-01 Searle Llc Fremgangsmåde til fremstilling af 5-substituerede pyrazoler under anvendelse af dithietaner
DK1140916T3 (da) 1998-12-16 2003-03-10 Aventis Pharma Ltd Heteroaryl-cykliske acetaler
EP1142890B1 (de) 1998-12-25 2005-08-03 Teikoku Hormone Mfg. Co., Ltd. Aminopyrazol derivate
JP2002534385A (ja) 1999-01-08 2002-10-15 スミスクライン・ビーチャム・コーポレイション 新規化合物
WO2000041698A1 (en) 1999-01-13 2000-07-20 Bayer Corporation φ-CARBOXY ARYL SUBSTITUTED DIPHENYL UREAS AS p38 KINASE INHIBITORS
UA73492C2 (en) 1999-01-19 2005-08-15 Aromatic heterocyclic compounds as antiinflammatory agents
JP2000281588A (ja) 1999-03-30 2000-10-10 Sankyo Co Ltd ガンの予防又は治療薬及びそのスクリーニング方法
ES2239596T3 (es) 1999-06-03 2005-10-01 Teikoku Hormone Mfg. Co., Ltd. Compuestos de pirazol sustituidos.
NZ515711A (en) 1999-06-24 2004-01-30 Pharmacia Corp Combination of tumors necrocis factor (TNF) antagonists and COX-2 inhibitors for the treatment of inflammation
EP1223924A4 (de) 1999-09-17 2004-07-14 Smithkline Beecham Corp Verwendung von csaids bei rhinovirus-infektionen
DE60015594T2 (de) 1999-11-22 2005-10-27 Smithkline Beecham P.L.C., Brentford Imidazolderivate und deren verwendung als raf kinase inhibitoren
EP1235814B1 (de) 1999-11-23 2004-11-03 Smithkline Beecham Corporation 3,4-DIHYDRO-(1H)CHINAZOLIN-2-ON-VERBINDUNGEN ALS CSBP/p38-KINASE-INHIBITOREN
JP2003517471A (ja) 1999-11-23 2003-05-27 スミスクライン・ビーチャム・コーポレイション ３，４−ジヒドロ−（１Ｈ）−キナゾリン−２−オンおよびそのＣＳＢＰ／ｐ３８キナーゼ阻害剤としての使用
DE60023025T2 (de) * 1999-11-23 2006-07-13 Smithkline Beecham Corp. 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
EP1233951B1 (de) 1999-11-23 2005-06-01 SmithKline Beecham Corporation 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
AR030053A1 (es) 2000-03-02 2003-08-13 Smithkline Beecham Corp 1h-pirimido [4,5-d] pirimidin-2-onas y sales, composiciones farmaceuticas, uso para la fabricacion de un medicamento y procedimiento para producirlas
EP1305050A2 (de) 2000-07-24 2003-05-02 Boehringer Ingelheim Pharmaceuticals Inc. Verbesserte orale darreichungsforme
AU2002231283A1 (en) 2000-10-19 2002-04-29 Smith Kline Beecham Corporation Use of p38 inhibitors for the treatment of smoke inhalation
WO2002060869A2 (en) 2000-10-19 2002-08-08 Smithkline Beecham Corporation Use of p38 inhibitors for the treatment of inflammation-enhanced cough
CN100525768C (zh) 2000-10-23 2009-08-12 史密丝克莱恩比彻姆公司 新化合物
US20040053943A1 (en) 2000-11-20 2004-03-18 Adams Jerry L. Novel compounds
CA2431904A1 (en) 2000-12-20 2002-08-01 Merck & Co., Inc. (halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents
BR0309053A (pt) 2002-04-19 2005-02-22 Smithkline Beecham Corp Compostos

Also Published As

Publication number Publication date
ES2241675T3 (es) 2005-11-01
WO2001038314A1 (en) 2001-05-31
EP1233951A4 (de) 2003-05-21
JP2003514900A (ja) 2003-04-22
EP1233951B1 (de) 2005-06-01
EP1233951A1 (de) 2002-08-28
DE60020595D1 (de) 2005-07-07
AU1783201A (en) 2001-06-04
DE60020595T2 (de) 2006-03-16
US7053098B1 (en) 2006-05-30

Similar Documents

Publication Publication Date Title
DE60020595D1 (de) 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
NO20031794L (no) Nye forbindelser
DE60023025D1 (de) 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p39-kinase-inhibitoren
DE69917296D1 (de) Neue substituierte triazolverbindungen
BR9810342A (pt) Novos compostos imidazola substituìdos
MY141144A (en) 1, 5-disubstituted-3,4-dihydro-1h-pyrimido 4,5-dipyrimidin-2-one compounds and their use in treating csbp/p38 kinase mediated diseases
NO983189L (no) Nye substituerte imidazolforbindelser
DE69918422D1 (de) Phthalazinone pde iii/iv hemmer
PT935465E (pt) Compostos novos de imidazole substituido
DK0889886T5 (da) Hidtil ukendte, i 6-stilling substituerede phenanthridiner
BR0215360A (pt) Derivados de indolina úteis como inibidores de proteìna quinase
EE200000033A (et) Uudsed tetrasoolderivaadid
ATE281439T1 (de) 3,4-dihydro-(1h)chinazolin-2-on-verbindungen als csbp/p38-kinase-inhibitoren
IS7507A (is) Ný efnasambönd
MXPA03003478A (es) Compuestos heterociclicos 2-sustituidos y su uso para tratar resistencia a multiples farmacos.
UY26980A1 (es) Nuevos compuestos
UY24784A1 (es) Nuevos compuestos de imidazol sustituidos

Legal Events

Date Code Title Description
RER Ceased as to paragraph 5 lit. 3 law introducing patent treaties