MXPA03010583A - Derivados de pirimidina utiles como inhibidores de cox-2 selectivos. - Google Patents

Derivados de pirimidina utiles como inhibidores de cox-2 selectivos.

Info

Publication number
MXPA03010583A
MXPA03010583A MXPA03010583A MXPA03010583A MXPA03010583A MX PA03010583 A MXPA03010583 A MX PA03010583A MX PA03010583 A MXPA03010583 A MX PA03010583A MX PA03010583 A MXPA03010583 A MX PA03010583A MX PA03010583 A MXPA03010583 A MX PA03010583A
Authority
MX
Mexico
Prior art keywords
6alkyl
group
substituted
6alkoxy
formula
Prior art date
Application number
MXPA03010583A
Other languages
English (en)
Inventor
Naylor Alan
Original Assignee
Glaxo Group Ltd
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 Glaxo Group Ltd filed Critical Glaxo Group Ltd
Publication of MXPA03010583A publication Critical patent/MXPA03010583A/es

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
    • C07D239/02—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
    • C07D239/28—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 hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)

Abstract

La presente invencion proporciona los compuestos de la formula (l), en donde: R1 es seleccionado del grupo que consiste de H, alquiloC1-6, alquiloC1-2 substituido de uno a cinco atomos de fluor, alqueniloC3-6, cicloalquiloC3-10alquiloC0-6, cicloalquilo puenteado por C4-12, A(CR4R5), y b(CR4R5)n; R2 es un alquiloC1-2 substituido de uno a cinco atomos de fluor; R3 es seleccionado del grupo que consiste de alquiloC1-6, NH2 y R7CONH; R4 y R5 son seleccionados independientemente de H o alquiloC1-6; A es un heteroarilo de 5- o 6- miembros no substituido o un arilo de 6-miembros no substituido, o un heteroarilo de 5- o 6-miembros o un arilo de 6-miembros substituido por uno o mas de R6; R6 es seleccionado del grupo que consiste de halogeno, alquiloC1-6, alquiloC1-6 substituido con uno o mas atomos de fluor, alcoxiC1-6, aicoxiC1-6 substituido con uno o mas de F, NH2SO2 y alquiloC1-6SO2; B es seleccionado del grupo que consiste de la formula (I) y (II) y en donde (IV) define el punto de adicion del anillo; R7 es seleccionado del grupo que consiste de H, alquiloC1-6 OCOalquiloC1-6 y alquiloC1-6 OCONHalquiloC1-6; y n es de 0 a 4. Los compuestos de la formula (I) son inhibidores potentes y selectivos de COX-2 y se utilizan en el tratamiento del dolor, fiebre e inflamacion de una variedad de condiciones y enfermedades.
MXPA03010583A 2001-05-25 2002-05-23 Derivados de pirimidina utiles como inhibidores de cox-2 selectivos. MXPA03010583A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0112802.4A GB0112802D0 (en) 2001-05-25 2001-05-25 Pyrimidine derivatives
PCT/GB2002/002415 WO2002096885A1 (en) 2001-05-25 2002-05-23 Pyrimidine derivatives useful as selective cox-2 inhibitors

Publications (1)

Publication Number Publication Date
MXPA03010583A true MXPA03010583A (es) 2004-03-09

Family

ID=9915322

Family Applications (1)

Application Number Title Priority Date Filing Date
MXPA03010583A MXPA03010583A (es) 2001-05-25 2002-05-23 Derivados de pirimidina utiles como inhibidores de cox-2 selectivos.

Country Status (29)

Country Link
US (2) US7026327B2 (es)
EP (2) EP1390351B1 (es)
JP (1) JP4291688B2 (es)
KR (1) KR100889427B1 (es)
CN (1) CN1255387C (es)
AR (1) AR036028A1 (es)
AT (2) ATE325103T1 (es)
AU (1) AU2002302764B2 (es)
BR (1) BR0209787A (es)
CA (1) CA2448192A1 (es)
CO (1) CO5540311A2 (es)
CZ (1) CZ20033204A3 (es)
DE (2) DE60211149T2 (es)
DK (1) DK1390351T3 (es)
ES (2) ES2316918T3 (es)
GB (1) GB0112802D0 (es)
HK (1) HK1063311A1 (es)
HU (1) HUP0401280A3 (es)
IL (1) IL158799A0 (es)
MX (1) MXPA03010583A (es)
MY (1) MY130750A (es)
NO (1) NO326949B1 (es)
NZ (1) NZ529719A (es)
PL (1) PL366514A1 (es)
PT (1) PT1390351E (es)
SI (1) SI1390351T1 (es)
TW (1) TWI327140B (es)
WO (1) WO2002096885A1 (es)
ZA (1) ZA200308826B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0021494D0 (en) 2000-09-01 2000-10-18 Glaxo Group Ltd Chemical comkpounds
GB0112810D0 (en) 2001-05-25 2001-07-18 Glaxo Group Ltd Pyrimidine derivatives
GB0112802D0 (en) 2001-05-25 2001-07-18 Glaxo Group Ltd Pyrimidine derivatives
ATE325115T1 (de) 2002-08-19 2006-06-15 Glaxo Group Ltd Pyrimidinderivate als selektive cox-2-inhibitoren
GB0221443D0 (en) 2002-09-16 2002-10-23 Glaxo Group Ltd Pyridine derivates
GB0227443D0 (en) * 2002-11-25 2002-12-31 Glaxo Group Ltd Pyrimidine derivatives
US20070142411A1 (en) * 2003-11-19 2007-06-21 James Hagan Use of cyclooxygenase-2 selective inhibitors for the treatment of schizophrenic disorders
EP1687000A2 (en) * 2003-11-19 2006-08-09 Glaxo Group Limited Use of cyclooxygenase-2 inhibitors for the treatment of depressive disorders
WO2021050700A1 (en) * 2019-09-13 2021-03-18 The Broad Institute, Inc. Cyclooxygenase-2 inhibitors and uses thereof

Family Cites Families (32)

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Publication number Priority date Publication date Assignee Title
US3149109A (en) * 1962-02-20 1964-09-15 Searle & Co Certain 4-trifluoromethyl-2-(oxy/thio) pyrimidines
GB1121922A (en) * 1966-06-17 1968-07-31 Ici Ltd Pyrimidine derivatives
US5474995A (en) * 1993-06-24 1995-12-12 Merck Frosst Canada, Inc. Phenyl heterocycles as cox-2 inhibitors
ES2193609T3 (es) * 1993-11-30 2003-11-01 Searle & Co Pirazolil-bencenosulfonamidas sustituidas y su uso como inhibidores de la ciclooxigenasa ii.
CN1118454C (zh) 1994-09-09 2003-08-20 日本新药株式会社 杂环衍生物和医药
US5596008A (en) 1995-02-10 1997-01-21 G. D. Searle & Co. 3,4-Diaryl substituted pyridines for the treatment of inflammation
WO1996041645A1 (en) 1995-06-12 1996-12-27 G.D. Searle & Co. Combination of a cyclooxygenase-2 inhibitor and a leukotriene b4 receptor antagonist for the treatment of inflammations
US5700816A (en) 1995-06-12 1997-12-23 Isakson; Peter C. Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitor and a leukotriene A4 hydrolase inhibitor
US6020343A (en) * 1995-10-13 2000-02-01 Merck Frosst Canada, Inc. (Methylsulfonyl)phenyl-2-(5H)-furanones as COX-2 inhibitors
JPH09241161A (ja) 1996-03-08 1997-09-16 Nippon Shinyaku Co Ltd 医 薬
JPH09266197A (ja) * 1996-03-28 1997-10-07 Mitsubishi Electric Corp 半導体装置およびその製造方法
SI0912518T1 (en) 1996-07-18 2003-12-31 Merck Frosst Canada & Co. Substituted pyridines as selective cyclooxygenase-2 inhibitors
TWI235060B (en) 1996-10-15 2005-07-01 Searle & Co Pharmaceutical compositions comprising substituted pyrazolyl benzenesulfonamide derivatives for use in treating or preventing an epithelial cell-derived neoplasia
AR038955A1 (es) 1996-12-05 2005-02-02 Amgen Inc Compuestos de pirimidinona y piridona sustituidos y metodos para su uso
CA2296014A1 (en) 1997-07-03 1999-01-14 Frank W. Hobbs Aryl-and arylamino-substituted heterocycles as corticotropin releasing hormone antagonists
ES2231757T3 (es) * 1997-09-05 2005-05-16 Glaxo Group Limited Composiciones farmaceutica que comprenden derivados de 2,3-diaril-pirazolo (1,5-b) piridazina.
US5972986A (en) * 1997-10-14 1999-10-26 G.D. Searle & Co. Method of using cyclooxygenase-2 inhibitors in the treatment and prevention of neoplasia
DE19909541A1 (de) 1998-03-06 1999-10-14 American Cyanamid Co Herbizide 2-Aryloxy- bzw. 2-Arylthio-6-arylpyrimidine
US6306866B1 (en) * 1998-03-06 2001-10-23 American Cyanamid Company Use of aryl-substituted pyrimidines as insecticidal and acaricidal agents
US6313072B1 (en) * 1999-02-18 2001-11-06 American Cyanamid Company Herbicidal 2-aryloxy-or 2-arylthio-6-arylpyrimidines
ATE261444T1 (de) * 1999-02-27 2004-03-15 Glaxo Group Ltd Pyrazolopyridine
GB9927844D0 (en) * 1999-11-26 2000-01-26 Glaxo Group Ltd Chemical compounds
GB9930358D0 (en) * 1999-12-22 2000-02-09 Glaxo Group Ltd Process for the preparation of chemical compounds
GB0002336D0 (en) * 2000-02-01 2000-03-22 Glaxo Group Ltd Medicaments
GB0002312D0 (en) * 2000-02-01 2000-03-22 Glaxo Group Ltd Medicaments
GB0003224D0 (en) 2000-02-11 2000-04-05 Glaxo Group Ltd Chemical compounds
GB0021494D0 (en) 2000-09-01 2000-10-18 Glaxo Group Ltd Chemical comkpounds
US6756498B2 (en) * 2001-04-27 2004-06-29 Smithkline Beecham Corporation Process for the preparation of chemical compounds
GB0112802D0 (en) 2001-05-25 2001-07-18 Glaxo Group Ltd Pyrimidine derivatives
GB0112810D0 (en) 2001-05-25 2001-07-18 Glaxo Group Ltd Pyrimidine derivatives
GB0112803D0 (en) 2001-05-25 2001-07-18 Glaxo Group Ltd Pyrimidine derivatives
US6861249B1 (en) * 2002-04-09 2005-03-01 David Kent Microbial spray for animal waste

Also Published As

Publication number Publication date
DK1390351T3 (da) 2006-08-07
JP4291688B2 (ja) 2009-07-08
EP1493735B1 (en) 2008-10-29
ES2316918T3 (es) 2009-04-16
CA2448192A1 (en) 2002-12-05
KR20040030629A (ko) 2004-04-09
NO326949B1 (no) 2009-03-16
GB0112802D0 (en) 2001-07-18
KR100889427B1 (ko) 2009-03-23
WO2002096885A1 (en) 2002-12-05
ZA200308826B (en) 2005-02-14
CO5540311A2 (es) 2005-07-29
US20050032821A1 (en) 2005-02-10
NO20035206D0 (no) 2003-11-24
US20050187235A1 (en) 2005-08-25
CZ20033204A3 (en) 2004-03-17
ATE412637T1 (de) 2008-11-15
HUP0401280A3 (en) 2009-06-29
AR036028A1 (es) 2004-08-04
EP1493735A1 (en) 2005-01-05
ES2262809T3 (es) 2006-12-01
DE60211149T2 (de) 2006-09-07
HUP0401280A2 (hu) 2004-12-28
TWI327140B (en) 2010-07-11
NZ529719A (en) 2006-02-24
AU2002302764B2 (en) 2005-12-01
ATE325103T1 (de) 2006-06-15
IL158799A0 (en) 2004-05-12
DE60211149D1 (de) 2006-06-08
SI1390351T1 (sl) 2006-10-31
DE60229669D1 (de) 2008-12-11
HK1063311A1 (en) 2004-12-24
CN1255387C (zh) 2006-05-10
CN1537104A (zh) 2004-10-13
JP2005511485A (ja) 2005-04-28
EP1390351B1 (en) 2006-05-03
BR0209787A (pt) 2004-06-01
MY130750A (en) 2007-07-31
PT1390351E (pt) 2006-06-30
PL366514A1 (en) 2005-02-07
NO20035206L (no) 2003-11-24
US7026327B2 (en) 2006-04-11
EP1390351A1 (en) 2004-02-25

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