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AR036028A1 - Compuesto de pirimidina, procedimiento para su preparacion, composiciones farmaceuticas formuladas con dichos compuestos y uso de los compuestos en la preparacion de las composiciones mencionadas - Google Patents

Compuesto de pirimidina, procedimiento para su preparacion, composiciones farmaceuticas formuladas con dichos compuestos y uso de los compuestos en la preparacion de las composiciones mencionadas

Info

Publication number
AR036028A1
AR036028A1 ARP020101915A ARP020101915A AR036028A1 AR 036028 A1 AR036028 A1 AR 036028A1 AR P020101915 A ARP020101915 A AR P020101915A AR P020101915 A ARP020101915 A AR P020101915A AR 036028 A1 AR036028 A1 AR 036028A1
Authority
AR
Argentina
Prior art keywords
alkyl
compound
formula
group
compounds
Prior art date
Application number
ARP020101915A
Other languages
English (en)
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 AR036028A1 publication Critical patent/AR036028A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/34One oxygen atom
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Engineering & Computer Science (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Compuestos de pirimidina de fórmula (1) en la que: R1 se selecciona del grupo constituido por H, alquilo C1-6, alquilo C1-2 sustituido con 1 a 5 átomos de flúor, alquenilo C3-6, alquinilo C3-6, cicloalquil C3-10-alquilo C0-6, cicloalquilo puente C4-12, A(CR4R5)n y B(CR4R5)n; R2 es alquilo C1-2 sustituido con 1 a 5 átomos de flúor; R3 se selecciona del grupo constituido por alquilo C1-6, NH2 y R7CONH; R4 y R5 se seleccionan independientemente entre H o alquilo C1-6; A es un heteroarilo insustituido de 5 o 6 miembros o un arilo insustituido de 6 miembros, o un heteroarilo de 5 o 6 miembros o un arilo de 6 miembros sustituidos con uno o más R6; R6 se selecciona del grupo constituido por halógeno, alquilo C1-6, alquilo C1-6 sustituido con uno o más átomos de flúor, alcoxi C1-6, alcoxi C1-6 sustituido con uno o más F, NH2SO2 y alquil C1-6-SO2; B se selecciona del grupo constituido por el grupo de fórmulas (2), donde: ) define el punto de unión del anillo; R7 se selecciona del grupo constituido por H, alquilo C1-6, alcoxi C1-6, alquil C1-6-O-alquilo C1-6, fenilo, HO2C-alquilo C1-6, alquil C1-6-OCO-alquilo C1-6, alquil C1-6-OCO, H2N-alquilo C1-6, alquil C1-6-OCONH-alquilo C1-6 y alquil C1-6-CONH-alquilo C1-6; y n es 0 a 4. Dichos compuestos son de aplicación en medicina veterinaria, en función de su selectiva actividad inhibidora de las enzimas COX-2, particularmente en el tratamiento de dolores - agudos - crónicos - estados febriles e inflamatorios mediados por dichas enzimas, inclusive dolores menopáusicos. Se describen además los objetos restantes, invocados en el título, inclusive un procedimiento para la preparación de dichos compuestos caracterizado porque comprende: A) hacer reaccionar un alcohol R1OH o una de sus derivados protegidos con un compuesto de la fórmula (3), y después, y si fuera necesario, (B), interconvertir un compuesto de la fórmula (1) en otro compuesto de la fórmula (1); y/o (C), desproteger un derivado protegido de un compuesto de la fórmula (1). Una composición farmacéutica que comprende un compuesto de la fórmula (1) en mezcla con uno o más vehículos o excipientes fisiológicamente aceptables. Uso de un compuesto de la fórmula (1) para preparar un agente terapéutico para el tratamiento de un trastorno que está mediado por la COX-2, por ejemplo, un trastorno inflamatorio.
ARP020101915A 2001-05-25 2002-05-23 Compuesto de pirimidina, procedimiento para su preparacion, composiciones farmaceuticas formuladas con dichos compuestos y uso de los compuestos en la preparacion de las composiciones mencionadas AR036028A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GBGB0112802.4A GB0112802D0 (en) 2001-05-25 2001-05-25 Pyrimidine derivatives

Publications (1)

Publication Number Publication Date
AR036028A1 true AR036028A1 (es) 2004-08-04

Family

ID=9915322

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020101915A AR036028A1 (es) 2001-05-25 2002-05-23 Compuesto de pirimidina, procedimiento para su preparacion, composiciones farmaceuticas formuladas con dichos compuestos y uso de los compuestos en la preparacion de las composiciones mencionadas

Country Status (28)

Country Link
US (2) US7026327B2 (es)
EP (2) EP1493735B1 (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) DE60229669D1 (es)
DK (1) DK1390351T3 (es)
ES (2) ES2262809T3 (es)
GB (1) GB0112802D0 (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
DE60305053T2 (de) 2002-08-19 2006-08-31 Glaxo Group Ltd., Greenford 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
US20070270428A1 (en) * 2003-11-19 2007-11-22 James Hagan Use of Cyclooxygenase-2 Inhibitors for the Treatment of Depressive Disorders
EP4027993A4 (en) * 2019-09-13 2023-09-20 The Broad Institute Inc. CYCLO-OXYGENASE 2 INHIBITORS AND THEIR USES

Family Cites Families (32)

* Cited by examiner, † Cited by third party
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
CA2276946A1 (en) 1993-11-30 1995-06-08 G.D. Searle & Co. Substituted pyrazolyl benzenesulfonamides and pharmaceutical compositions containing the same
US5945426A (en) 1994-09-09 1999-08-31 Nippon Shinyaku Co., Ltd. Derivatives of pyrimidine for treating acute cerebrovascular disorders
US5596008A (en) 1995-02-10 1997-01-21 G. D. Searle & Co. 3,4-Diaryl substituted pyridines for the treatment of inflammation
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
US6342510B1 (en) 1995-06-12 2002-01-29 G. D. Searle & Co. Treatment of inflammation and inflammation-related disorders with a combination of a cyclooxygenase-2 inhibitors and a leukotriene B4 receptor antagonist
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
IL127441A (en) * 1996-07-18 2003-02-12 Merck Frosst Canada Inc Substituted pyridines, pharmaceutical compositions comprising them and their use in the preparation of anti-inflammatory medicaments or as selective cyclooxygenase-2 inhibitors
CN100558356C (zh) 1996-10-15 2009-11-11 G.D.瑟尔公司 应用环加氧酶-2抑制剂治疗和预防肿瘤形成的方法
AR038955A1 (es) 1996-12-05 2005-02-02 Amgen Inc Compuestos de pirimidinona y piridona sustituidos y metodos para su uso
EP0994860A1 (en) 1997-07-03 2000-04-26 Du Pont Pharmaceuticals Company Aryl-and arylamino-substituted heterocycles as corticotropin releasing hormone antagonists
ATE317845T1 (de) * 1997-09-05 2006-03-15 Glaxo Group Ltd Pharmazeutische zusammensetzung, enthaltend 2,3- diaryl-pyrazolo(1,5-b)pyridazin derivate
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
WO2000052008A1 (en) * 1999-02-27 2000-09-08 Glaxo Group Limited Pyrazolopyridines
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
GB0112803D0 (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
GB0112810D0 (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
HUP0401280A2 (hu) 2004-12-28
US7026327B2 (en) 2006-04-11
BR0209787A (pt) 2004-06-01
US20050032821A1 (en) 2005-02-10
DE60211149D1 (de) 2006-06-08
CN1537104A (zh) 2004-10-13
SI1390351T1 (sl) 2006-10-31
EP1390351B1 (en) 2006-05-03
DE60229669D1 (de) 2008-12-11
ES2262809T3 (es) 2006-12-01
EP1493735A1 (en) 2005-01-05
NZ529719A (en) 2006-02-24
HK1063311A1 (en) 2004-12-24
PL366514A1 (en) 2005-02-07
JP2005511485A (ja) 2005-04-28
ES2316918T3 (es) 2009-04-16
DK1390351T3 (da) 2006-08-07
AU2002302764B2 (en) 2005-12-01
TWI327140B (en) 2010-07-11
KR100889427B1 (ko) 2009-03-23
DE60211149T2 (de) 2006-09-07
GB0112802D0 (en) 2001-07-18
CO5540311A2 (es) 2005-07-29
EP1493735B1 (en) 2008-10-29
NO326949B1 (no) 2009-03-16
NO20035206L (no) 2003-11-24
IL158799A0 (en) 2004-05-12
JP4291688B2 (ja) 2009-07-08
US20050187235A1 (en) 2005-08-25
HUP0401280A3 (en) 2009-06-29
CN1255387C (zh) 2006-05-10
PT1390351E (pt) 2006-06-30
MXPA03010583A (es) 2004-03-09
CA2448192A1 (en) 2002-12-05
ATE412637T1 (de) 2008-11-15
MY130750A (en) 2007-07-31
WO2002096885A1 (en) 2002-12-05
KR20040030629A (ko) 2004-04-09
EP1390351A1 (en) 2004-02-25
ZA200308826B (en) 2005-02-14
ATE325103T1 (de) 2006-06-15
CZ20033204A3 (en) 2004-03-17
NO20035206D0 (no) 2003-11-24

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