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AR039985A1 - Compuesto de pirimidinona, composicion farmaceutica que lo comprende y su uso para la elaboracion de esta ultima - Google Patents

Compuesto de pirimidinona, composicion farmaceutica que lo comprende y su uso para la elaboracion de esta ultima

Info

Publication number
AR039985A1
AR039985A1 ARP030101617A ARP030101617A AR039985A1 AR 039985 A1 AR039985 A1 AR 039985A1 AR P030101617 A ARP030101617 A AR P030101617A AR P030101617 A ARP030101617 A AR P030101617A AR 039985 A1 AR039985 A1 AR 039985A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
heteroaralkyl
compound
aralkyl
hydrogen
Prior art date
Application number
ARP030101617A
Other languages
English (en)
Original Assignee
Smithkline Beecham Corp
Cytokinetics Inc
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, Cytokinetics Inc filed Critical Smithkline Beecham Corp
Publication of AR039985A1 publication Critical patent/AR039985A1/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
    • C07D239/36—One oxygen atom as doubly bound oxygen atom or as unsubstituted hydroxy radical
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/10—Antimycotics
    • 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
    • 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
    • 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
    • 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
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/12—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/56—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, attached to ring carbon atoms
    • 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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • 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
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/08—1,2,4-Triazoles; Hydrogenated 1,2,4-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/06—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Composición farmacéutica que comprende un excipiente farmacéutico y un compuesto, sal o solvato del mismo, del compuesto de fórmula (1); dicha composición puede comprender adicionalmente un agente quimioterapéutico distinto del compuesto de fórmula (1). Uso del compuesto de fórmula (1) para elaborar un medicamento para tratar enfermedades y trastornos de proliferación celular modulando la actividad de KSP, tales como cáncer, hiperplasia, restenosis, hipertrofia cardiaca, trastornos inmunes e inflamación. Reivindicación 1: Un compuesto de pirimidinona caracterizado porque tiene la estructura de fórmula(1) en la cual: R1 se escoge entre hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido y heteroaralquilo opcionalmente sustituido; R2 y R2' se escogen independientemente entre hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido y heteroaralquilo opcionalmente sustituido; o R2 y R2' tomados conjuntamente forman un anillo de 3 a 7 miembros opcionalmente sustituidos; R4 y R5 se escogen independientemente entre hidrógeno, alquilo opcionalmente sustituido, alcoxi opcionalmente sustituido, halógeno, hidroxilo, nitro, ciano, dialquilamino, alquilsulfonilo, alquisulfonamido, alquilsulfanilo, carboxialquilo, carboxamido, aminocarbonilo, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroaralquilo opcionalmente sustituido y heteroarilo opcionalmente sustituido; o R4 y R5 tomados conjuntamente con los átomos de carbono a los que están unidos forman un anillo carbocíclico alifático de 5, 6 ó 7 miembros opcionalmente sustituido; R3 se selecciona entre el grupo que consiste en imidazolilo opcionalmente sustituido, imidazolinilo opcionalmente sustituido, -NHR6; -N(R6)(COR7); -N(R6)(SO2R7a); y -N(R6)(CH2R7b); R7 se escoge entre hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroaralquilo opcionalmente sustituido, R8O y R14-NH-; R7a se escoge entre alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, heteroaralquilo opcionalmente sustituido y R14-NH-; R7b se escoge entre hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido y heteroaralquilo opcionalmente sustituido; R6 se escoge entre hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heterociclilo opcionalmente sustituido y heteroaralquilo opcionalmente sustituido; R8 se escoge entre alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y heteroaralquilo opcionalmente sustituido; y R14 es hidrógeno, alquilo opcionalmente sustituido, arilo opcionalmente sustituido, aralquilo opcionalmente sustituido, heteroarilo opcionalmente sustituido, y heteroaralquilo opcionalmente sustituido; incluidos los estereoisómeros individuales y las mezclas de estereoisómeros; una sal farmacéuticamente aceptable de un compuesto de fórmula (1); un solvato farmacéuticamente aceptable de un compuesto de fórmula (1); o un solvato farmacéuticamente aceptable de una sal farmacéuticamente aceptable de un compuesto de fórmula (1).
ARP030101617A 2002-05-09 2003-05-08 Compuesto de pirimidinona, composicion farmaceutica que lo comprende y su uso para la elaboracion de esta ultima AR039985A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US37965802P 2002-05-09 2002-05-09

Publications (1)

Publication Number Publication Date
AR039985A1 true AR039985A1 (es) 2005-03-09

Family

ID=29420548

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP030101617A AR039985A1 (es) 2002-05-09 2003-05-08 Compuesto de pirimidinona, composicion farmaceutica que lo comprende y su uso para la elaboracion de esta ultima

Country Status (20)

Country Link
US (2) US7166595B2 (es)
EP (1) EP1503993A4 (es)
JP (1) JP2006508030A (es)
KR (1) KR20050036911A (es)
CN (1) CN100491358C (es)
AR (1) AR039985A1 (es)
AU (1) AU2003223786A1 (es)
BR (1) BR0309892A2 (es)
CA (1) CA2485148A1 (es)
IL (2) IL165046A0 (es)
IS (1) IS7520A (es)
MX (1) MXPA04011074A (es)
MY (1) MY140767A (es)
NO (1) NO20045043L (es)
NZ (1) NZ537076A (es)
PL (1) PL373412A1 (es)
RU (1) RU2004135554A (es)
TW (1) TW200406387A (es)
WO (1) WO2003094839A2 (es)
ZA (1) ZA200409881B (es)

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AU2003223786A1 (en) 2003-11-11
WO2003094839A2 (en) 2003-11-20
CN100491358C (zh) 2009-05-27
MY140767A (en) 2010-01-15
US20070135432A1 (en) 2007-06-14
KR20050036911A (ko) 2005-04-20
TW200406387A (en) 2004-05-01
IL165046A0 (en) 2005-12-18
PL373412A1 (en) 2005-08-22
RU2004135554A (ru) 2006-01-20
US7482343B2 (en) 2009-01-27
CA2485148A1 (en) 2003-11-20
BR0309892A2 (pt) 2011-04-05
WO2003094839A8 (en) 2004-06-24
MXPA04011074A (es) 2005-06-08
US7166595B2 (en) 2007-01-23
CN1665788A (zh) 2005-09-07
NZ537076A (en) 2007-06-29
NO20045043L (no) 2005-02-08
EP1503993A2 (en) 2005-02-09
WO2003094839A3 (en) 2004-09-16
EP1503993A4 (en) 2006-05-03
JP2006508030A (ja) 2006-03-09
US20040077662A1 (en) 2004-04-22
ZA200409881B (en) 2006-04-26

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