DOP2002000334A - Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz - Google Patents

Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz

Info

Publication number
DOP2002000334A
DOP2002000334A DO2002000334A DO2002000334A DOP2002000334A DO P2002000334 A DOP2002000334 A DO P2002000334A DO 2002000334 A DO2002000334 A DO 2002000334A DO 2002000334 A DO2002000334 A DO 2002000334A DO P2002000334 A DOP2002000334 A DO P2002000334A
Authority
DO
Dominican Republic
Prior art keywords
alkyl
pyrimidines
bicycle
aryl
matrix metaloproteinase
Prior art date
Application number
DO2002000334A
Other languages
English (en)
Inventor
Richard Dennis Dyer
William Glen Harter
James Lester Hicks
Adam Richard Johnson
Jie Jack Li
William Howard Roark
Kevon Ray Shuler
Original Assignee
Warner Lambert Co
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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of DOP2002000334A publication Critical patent/DOP2002000334A/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61P1/02—Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • 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
    • 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
    • A61P19/08—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
    • 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
    • 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
    • A61P3/06—Antihyperlipidemics
    • 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
    • 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
    • A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • 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
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Public Health (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Ophthalmology & Optometry (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Son inhibidores selectivos de MMP-13 las pirimidinas bicíclicas de la Fórmula I o una sal farmacéuticamente aceptable de las mismas, en la que R1 es hidrógeno o alquilo; R2, R3 y R4 incluyen hidrógeno, halo, alquilo, CCCH2m arilo, C02 alquilo, CO2CH2 arilo, COHN alquilo y CONHCH2m arilo; y X es O, S, SO, S02, CH2, C=O, CHOH, NH o NR5. Un compuesto de Fórmula I, o una sal farmacéuticamente aceptable del mismo, es útil para tratar el cáncer o la artritis.
DO2002000334A 2001-02-14 2002-01-29 Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz DOP2002000334A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US26878001P 2001-02-14 2001-02-14

Publications (1)

Publication Number Publication Date
DOP2002000334A true DOP2002000334A (es) 2002-08-30

Family

ID=23024440

Family Applications (1)

Application Number Title Priority Date Filing Date
DO2002000334A DOP2002000334A (es) 2001-02-14 2002-01-29 Pirimidinas biciclicas como inhibidores de metaloproteinasas de matriz

Country Status (13)

Country Link
US (1) US20060040957A1 (es)
EP (1) EP1362054A1 (es)
JP (1) JP2004518733A (es)
BR (1) BR0207861A (es)
CA (1) CA2436371A1 (es)
DO (1) DOP2002000334A (es)
GT (1) GT200200027A (es)
MX (1) MXPA03006168A (es)
PA (1) PA8538101A1 (es)
PE (1) PE20020961A1 (es)
SV (1) SV2003000881A (es)
TN (1) TNSN02011A1 (es)
WO (1) WO2002064599A1 (es)

Families Citing this family (35)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6924276B2 (en) 2001-09-10 2005-08-02 Warner-Lambert Company Diacid-substituted heteroaryl derivatives as matrix metalloproteinase inhibitors
US6962922B2 (en) 2001-10-12 2005-11-08 Warner-Lambert Company Llc Alkynylated quinazoline compounds
MXPA04002537A (es) 2001-10-12 2004-05-31 Warner Lambert Co Alquinos como inhibidores de metaloproteinasa de matriz.
US6894057B2 (en) 2002-03-08 2005-05-17 Warner-Lambert Company Oxo-azabicyclic compounds
US6747147B2 (en) 2002-03-08 2004-06-08 Warner-Lambert Company Oxo-azabicyclic compounds
EP1531904A1 (en) * 2002-07-17 2005-05-25 Warner-Lambert Company LLC Combination of an allosteric inhibitor of matrix metalloproteinase-13 with a selective inhibitor of cyclooxygenase-2 that is not celecoxib or valdecoxib
BR0312727A (pt) * 2002-07-17 2005-04-19 Warner Lambert Co Combinação de um inibidor alostérico da metaloproteinase-13 de matriz com celecoxib ou valdecoxib
AU2003250470A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidinone fused bicyclic metalloproteinase inhibitors
PA8578101A1 (es) 2002-08-13 2004-05-07 Warner Lambert Co Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
AU2003253186A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Fused tetrahydropyridine derivatives as matrix metalloproteinase inhibitors
MXPA05001603A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados monociclicos como inhibidores de metaloproteinasa de matriz.
MXPA05001786A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados de azaisoquinolina como inhibidores de la metaloproteinasa de matriz.
WO2004014375A2 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Fused bicyclic metalloproteinase inhibitors
MXPA05001783A (es) 2002-08-13 2005-04-25 Warner Lambert Co Derivados de pirimidina-2,4-diona como inhibidores de las metaloproteinasas de matriz.
CA2497658A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Chromone derivatives as matrix metalloproteinase inhibitors
WO2004014378A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc 3-isoquinolinone derivatives as matrix metalloproteinase inhiitors
US20040142950A1 (en) * 2003-01-17 2004-07-22 Bunker Amy Mae Amide and ester matrix metalloproteinase inhibitors
US7247654B2 (en) 2003-06-04 2007-07-24 Bristol-Myers Squibb Company 3,4-disubstituted benzamidines and benzylamines, and analogues thereof, useful as serine protease inhibitors
US20060247231A1 (en) * 2003-12-18 2006-11-02 Warner-Lambert Company Llc Amide and ester matrix metalloproteinase inhibitors
US7570259B2 (en) 2004-06-01 2009-08-04 Intel Corporation System to manage display power consumption
US7576098B2 (en) 2004-12-08 2009-08-18 Bristol-Myers Squibb Company Heterocyclic compounds as inhibitors of factor VIIa
EP2448938B9 (en) 2009-06-29 2015-06-10 Incyte Corporation Pyrimidinones as pi3k inhibitors
WO2011075643A1 (en) 2009-12-18 2011-06-23 Incyte Corporation Substituted heteroaryl fused derivatives as pi3k inhibitors
EP2558463A1 (en) 2010-04-14 2013-02-20 Incyte Corporation Fused derivatives as i3 inhibitors
US9062055B2 (en) 2010-06-21 2015-06-23 Incyte Corporation Fused pyrrole derivatives as PI3K inhibitors
JP5961187B2 (ja) 2010-12-20 2016-08-02 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Pi3k阻害剤としてのn−(1−(置換フェニル)エチル)−9h−プリン−6−アミン
US9108984B2 (en) 2011-03-14 2015-08-18 Incyte Corporation Substituted diamino-pyrimidine and diamino-pyridine derivatives as PI3K inhibitors
US9126948B2 (en) 2011-03-25 2015-09-08 Incyte Holdings Corporation Pyrimidine-4,6-diamine derivatives as PI3K inhibitors
MX389479B (es) 2011-09-02 2025-03-20 Incyte Holdings Corp Heterociclilaminas como inhibidores de fosfoinositida 3-cinasas (pi3k)
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
US10077277B2 (en) 2014-06-11 2018-09-18 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as PI3K inhibitors
SG10201912302VA (en) 2015-02-27 2020-02-27 Incyte Corp Salts of pi3k inhibitor and processes for their preparation
WO2016183060A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
US9988401B2 (en) 2015-05-11 2018-06-05 Incyte Corporation Crystalline forms of a PI3K inhibitor
IL278889B2 (en) 2018-06-01 2025-11-01 Incyte Corp Dosing regimen for the treatment of pi3k related disorders

Family Cites Families (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL129612B1 (en) * 1980-07-24 1984-05-31 Rhone Poulenc Ind Process for preparing novel derivatives of 2,3,6,7-tetrahydrothiazole/3,2-a/pirymidin-5-one
EP0049902A3 (en) * 1980-10-15 1982-09-01 Teijin Limited Novel thiazolo(3,2-a)pyrimidines, derivatives thereof, processes for production thereof, and pharmaceutical use thereof
US4302585A (en) * 1980-12-22 1981-11-24 American Home Products Corporation 3-Hydroxy-3-substituted phenylthiazolo[2,3-b]quinazoline-2-alkanoic acids and their lactones
US4383996A (en) * 1981-12-28 1983-05-17 Teijin Limited Derivative of thiazolo[3,2-a]pyrimidine and a process for the preparation thereof and a drug containing it
JPH0710865B2 (ja) * 1987-06-26 1995-02-08 日本バイエルアグロケム株式会社 ニトロ置換ヘテロ環式化合物及び殺虫剤
US5082838A (en) * 1989-06-21 1992-01-21 Takeda Chemical Industries, Ltd. Sulfur-containing fused pyrimidine derivatives, their production and use
DK0828726T3 (da) * 1995-06-02 2002-01-21 Warner Lambert Co Tricykliske inhibitorer af matrixmetalloproteinaser
MXPA99001974A (es) * 1996-12-09 2002-03-27 Warner Lambert Co Metodo para tratar y prevenir fallas cardiacas y dilatacion ventricular.
PA8539301A1 (es) * 2001-02-14 2002-09-30 Warner Lambert Co Inhibidores de la metaloproteinasa de la matriz
MXPA03004926A (es) * 2001-02-14 2005-02-14 Warner Lambert Co Inhibidores de metaloproteinasas de matriz basados en pirimidinonas fusionadas.
PA8539401A1 (es) * 2001-02-14 2002-10-28 Warner Lambert Co Quinazolinas como inhibidores de mmp-13
MXPA04002537A (es) * 2001-10-12 2004-05-31 Warner Lambert Co Alquinos como inhibidores de metaloproteinasa de matriz.
US6962922B2 (en) * 2001-10-12 2005-11-08 Warner-Lambert Company Llc Alkynylated quinazoline compounds
US6894057B2 (en) * 2002-03-08 2005-05-17 Warner-Lambert Company Oxo-azabicyclic compounds
US20040006077A1 (en) * 2002-06-25 2004-01-08 Bernard Gaudilliere Thiazine and oxazine derivatives as MMP-13 inhibitors
WO2004014384A2 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
WO2004014365A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
AU2003253165A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidine fused bicyclic metalloproteinase inhibitors
AU2003250470A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidinone fused bicyclic metalloproteinase inhibitors
WO2004014867A2 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Matrix metalloproteinase inhibitors and methods for identification of lead compounds
WO2004014375A2 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Fused bicyclic metalloproteinase inhibitors
AU2003249477A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Heterobicylcic metalloproteinase inhibitors

Also Published As

Publication number Publication date
PE20020961A1 (es) 2002-10-26
SV2003000881A (es) 2003-01-13
EP1362054A1 (en) 2003-11-19
US20060040957A1 (en) 2006-02-23
GT200200027A (es) 2002-11-15
TNSN02011A1 (fr) 2005-12-23
WO2002064599A1 (en) 2002-08-22
PA8538101A1 (es) 2002-09-17
MXPA03006168A (es) 2005-02-14
BR0207861A (pt) 2004-03-23
JP2004518733A (ja) 2004-06-24
CA2436371A1 (en) 2002-08-22

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