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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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/02Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00Drugs for disorders of the senses
    • A61P27/02Ophthalmic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D513/00Heterocyclic 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
    • C07D513/02Heterocyclic 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
    • C07D513/04Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Engineering & Computer Science (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Rheumatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Neurosurgery (AREA)
  • Vascular Medicine (AREA)
  • Obesity (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Ophthalmology & Optometry (AREA)
  • Hematology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (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
EP1434585A1 (en) 2001-10-12 2004-07-07 Warner-Lambert Company LLC Alkyne matrix metalloproteinase inhibitors
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
US6747147B2 (en) 2002-03-08 2004-06-08 Warner-Lambert Company Oxo-azabicyclic compounds
CA2492391A1 (en) * 2002-07-17 2004-01-22 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
EP1536786A1 (en) * 2002-07-17 2005-06-08 Warner-Lambert Company Llc Combination of an allosteric inhibitor of matrix metalloproteinase-13 with celecoxib or valdecoxib
AU2003250466A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc 3-isoquinolinone derivatives as matrix metalloproteinase inhiitors
PA8578101A1 (es) * 2002-08-13 2004-05-07 Warner Lambert Co Derivados de heterobiarilo como inhibidores de metaloproteinasa de la matriz
EP1537098A1 (en) 2002-08-13 2005-06-08 Warner-Lambert Company LLC Monocyclic derivatives as matrix metalloproteinase inhibitors
BR0313384A (pt) 2002-08-13 2005-07-12 Warner Lambert Co Derivados de cromona como inibidores de metaloproteinases de matriz
AU2003250470A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidinone fused bicyclic metalloproteinase inhibitors
WO2004014909A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Fused tetrahydropyridine derivatives as matrix metalloproteinase inhibitors
AU2003249540A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Fused bicyclic metalloproteinase inhibitors
WO2004014866A1 (en) 2002-08-13 2004-02-19 Warner-Lambert Company Llc Azaisoquinoline derivatives as matrix metalloproteinase inhibitors
AU2003250471A1 (en) 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidine-2,4-dione derivatives as matrix metalloproteinase inhibitors
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
EP1828152B1 (en) 2004-12-08 2008-08-20 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
TW201249844A (en) 2010-12-20 2012-12-16 Incyte Corp N-(1-(substituted-phenyl)ethyl)-9H-purin-6-amines as PI3K inhibitors
WO2012125629A1 (en) 2011-03-14 2012-09-20 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
KR102030609B1 (ko) 2011-09-02 2019-10-11 인사이트 홀딩스 코포레이션 Pi3k 억제제로서 헤테로시클릴아민
AR090548A1 (es) 2012-04-02 2014-11-19 Incyte Corp Azaheterociclobencilaminas biciclicas como inhibidores de pi3k
WO2015191677A1 (en) 2014-06-11 2015-12-17 Incyte Corporation Bicyclic heteroarylaminoalkyl phenyl derivatives as pi3k inhibitors
DK3831833T3 (da) 2015-02-27 2022-11-14 Incyte Holdings Corp Fremgangsmåder til fremstillingen af en pi3k-inhibitor
US9732097B2 (en) 2015-05-11 2017-08-15 Incyte Corporation Process for the synthesis of a phosphoinositide 3-kinase inhibitor
WO2016183063A1 (en) 2015-05-11 2016-11-17 Incyte Corporation Crystalline forms of a pi3k inhibitor
CN119258070A (zh) 2018-06-01 2025-01-07 因赛特公司 治疗pi3k相关病症的给药方案

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
ATE206416T1 (de) * 1995-06-02 2001-10-15 Warner Lambert Co Trizyklische verbindungen als matrix- metalloproteinase inhibitoren
NZ334897A (en) * 1996-12-09 2001-02-23 Warner Lambert Co Medicaments for treating and preventing heart failure and ventricular dilatation
PA8539301A1 (es) * 2001-02-14 2002-09-30 Warner Lambert Co Inhibidores de la metaloproteinasa de la matriz
BR0207216A (pt) * 2001-02-14 2004-03-09 Warner Lambert Co Derivados de tieno 2,3-d-pirimidindiona como inibidores de metaloproteinase matriz
PA8539401A1 (es) * 2001-02-14 2002-10-28 Warner Lambert Co Quinazolinas como inhibidores de mmp-13
EP1434585A1 (en) * 2001-10-12 2004-07-07 Warner-Lambert Company LLC Alkyne matrix metalloproteinase inhibitors
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
WO2004014365A1 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Phthalimide derivatives as matrix metalloproteinase inhibitors
AU2003249540A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Fused bicyclic metalloproteinase inhibitors
AU2003253165A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidine fused bicyclic metalloproteinase inhibitors
WO2004014384A2 (en) * 2002-08-13 2004-02-19 Warner-Lambert Company Llc Cyclic compounds containing zinc binding groups as matrix metalloproteinase inhibitors
AU2002368151A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Matrix metalloproteinase inhibitors and methods for identification of lead compounds
AU2003249477A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Heterobicylcic metalloproteinase inhibitors
AU2003250470A1 (en) * 2002-08-13 2004-02-25 Warner-Lambert Company Llc Pyrimidinone fused bicyclic metalloproteinase inhibitors

Also Published As

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

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