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AR057625A1 - Compuestos de pirimidinona o pirimidinationa, procesos de obtencion, compuestos intermediarios, composiciones farmaceuticas y usos. - Google Patents

Compuestos de pirimidinona o pirimidinationa, procesos de obtencion, compuestos intermediarios, composiciones farmaceuticas y usos.

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Publication number
AR057625A1
AR057625A1 ARP060105122A ARP060105122A AR057625A1 AR 057625 A1 AR057625 A1 AR 057625A1 AR P060105122 A ARP060105122 A AR P060105122A AR P060105122 A ARP060105122 A AR P060105122A AR 057625 A1 AR057625 A1 AR 057625A1
Authority
AR
Argentina
Prior art keywords
alkyl
cr10r11
heteroaryl
aryl
halogen
Prior art date
Application number
ARP060105122A
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English (en)
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Smithkline Beecham Corp
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Application filed by Smithkline Beecham Corp filed Critical Smithkline Beecham Corp
Publication of AR057625A1 publication Critical patent/AR057625A1/es

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    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • 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
    • 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
    • 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
    • A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
    • A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
    • 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
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    • 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
    • C07D239/38—One sulfur atom
    • C07D239/40—One sulfur atom as doubly bound sulfur atom or as unsubstituted mercapto radical
    • 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
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    • 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
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    • 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
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    • 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
    • C07D401/04—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 directly linked by a ring-member-to-ring-member bond
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/04—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Chemical & Material Sciences (AREA)
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  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

Un compuesto de pirimidinona o pirimidinationa de la formula (1) en la que: X es O o S; R1 y R2 se seleccionan, independientemente, entre el grupo que consiste en H, halogeno, CN, alquilo C1-10, alquenilo C2-6, cicloalquilo, cicloalquil-alquilo C1- 6, arilo, aril-alquilo C1-6, heterociclilo, heteroarilo, (CR10R11)xNR5R6, C(O)OR5, C(O)NR5R6, NR5C(O)R6, (CR10R11)xOR5 y NC(O)R5, opcionalmente sustituidos, excepto para H, halogeno y CN, de 1 a 3 veces, independientemente, con halogeno, CN, alquilo C1-4, arilo, heteroarilo, C(O)OR19, O-(CR19R20)q-O, C(O)R19, CF3, OCF3, NO2, C(O)NR19R20, (CR10R11)z-OR19, (CR10R11)zNR19R20 y (CR10R11)xS(O)mR19; o R1 y R2 juntos forman un anillo de 5 a 8 miembros opcionalmente sustituido, que contiene opcionalmente de 1 a 3 heteroátomos seleccionados entre N, O y S, donde los sustituyentes opcionales se seleccionan, independientemente, en cada caso, de 1 a 3 veces, entre el grupo que consiste en halogeno, alquilo C1-4, (CR10R11)z-S(O)mR5, (CR10R11)zOR5, (CR10R11)zNR5R6, C(O)R5 y C(O)OR5; o R1 y R2 juntos forman un anillo heteroarilo opcionalmente sustituido, donde los sustituyentes opcionales se seleccionan, independientemente, en cada caso, de 1 a 3 veces, entre el grupo que consiste en halogeno, alquilo C1-4, (CR10R11)z-S(O)mR5, (CR10R11)zOR5, (CR10R11)zNR5R6, C(O)R5 y C(O)OR5; o cuando R1 es NR5R6, R5 y R6 pueden unirse para formar un anillo de 5 a 7 miembros, opcionalmente sustituido con alquilo C1-4 o halogeno; R5 y R6 representan, independientemente, en cada caso, H, alquilo C1-4, cicloalquilo, cicloalquil-alquilo C1-6, alquenilo C2-6, heterociclilo, heterociclil-alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo o heteroaril-alquilo C1-6, donde cada resto, excepto H, está opcionalmente sustituido, independientemente, de 1 a 3 veces, con halogeno o alquilo C1-4; R10 y R11 representan, independientemente, en cada caso H o alquilo C1-4; R19 y R20 representan, independientemente, en cada caso, H, alquilo C1-4, cicloalquilo, cicloalquil-alquilo C1-6, alquenilo C2-6, heterociclilo, heterociclil-alquilo C1-4, arilo, aril-alquilo C1-6, heteroarilo o un resto heteroaril-alquilo C1-6, donde cada resto, excepto H, puede estar sustituido, independientemente, de 1 a 3 veces con halogeno o alquilo C1-4; R3 representa arilo o heteroarilo, opcionalmente sustituido, independientemente, de 1 a 3 veces, con alquilo C1-4, halogeno, CN o CF3; R4 se selecciona entre el grupo que consiste en cicloalquil-alquilo C1-4, heteroarilo, heterociclilo, arilo, heteroaril-alquilo C1-2, heterociclil-alquilo C1-2, cicloalquil-alquenilo C2, aril-alquenilo C2, heteroaril-alquenilo C2 y heterociclil-alquenilo C2, donde cada resto está opcionalmente sustituido, independientemente, de 1 a 3 veces, con alquilo C1-4, F, CF3 o Cl; m es 0, 1 o 2; x es 0, 1, 2 o 3; q es 1, 2 o 3; y z es 0, 1, 2, 3 o 4; o una de sus sales farmacéuticamente aceptables. Composicion farmacéutica que lo comprende y su uso para preparar un medicamento para antagonizar un receptor de calcio, en el tratamiento de una enfermedad o trastorno por una homeostasis osea o mineral anormal, tal como osteosarcoma, enfermedad periodontal, curacion de fracturas, osteoartritis, artritis reumatoide, enfermedad de Paget, hipercalcemia humoral, malignidad y osteoporosis. Método de síntesis de dicho compuesto y compuestos intermedios de aplicacion en el mismo. Reivindicacion 1: Un compuesto de pirimidinona o pirimidinationa, caracterizado porque es de la formula (1) en la que: X es O o S; R1 y R2 se seleccionan, independientemente, entre el grupo que consiste en H, halogeno, CN, alquilo C1-10, alquenilo C2-6, cicloalquilo, cicloalquil-alquilo C1-6, arilo, aril-alquilo C1-6, heterociclilo, heteroarilo, (CR10R11)xNR5R6, C(O)OR5, C(O)NR5R6, NR5C(O)R6, (CR10R11)xOR5 y NC(O)R5, opcionalmente sustituidos, excepto para H, halogeno y CN, de 1 a 3 veces, independientemente, con halogeno, CN, alquilo C1-4, arilo, heteroarilo, C(O)OR19, O-(CR19R20)q-O, C(O)R19, CF3, OCF3, NO2, C(O)NR19R20, (CR10R11)z-OR19, (CR10R11)zNR19R20 y (CR10R11)xS(O)mR19; o R1 y R2 juntos forman un anillo de 5 a 8 miembros opcionalmente sustituido, que contiene opcionalmente de 1 a 3 heteroátomos seleccionados entre N, O y S, donde los sustituyentes opcionales se seleccionan, independientemente, en cada caso, de 1 a 3 veces, entre el grupo que consiste en halogeno, alquilo C1-4, (CR10R11)z-S(O)mR5, (CR10R11)zOR5, (CR10R11)zNR5R6, C(O)R5 y C(O)OR5; o R1 y R2 juntos forman un anillo heteroarilo opcionalmente sustituido, donde los sustituyentes opcionales se seleccionan, independientemente, en cada caso, de 1 a 3 veces, entre el grupo que consiste en halogeno, alquilo C1-4, (CR10R11)z-S(O)mR5, (CR10R11)zOR5, (CR10R11)zNR5R6, C(O)R5 y C(O)OR5; o cuando R1 es NR5R6, R5 y R6 pueden unirse para formar un anillo de 5 a 7 miembros, opcionalmente sustituido con alquilo C1-4 o halogeno; R5 y R6 representan, independientemente, en cada caso, H, alquilo C1-4, cicloalquilo, cicloalquil-alquilo C1-6, alquenilo C2-6, heterociclilo, heterociclil-alquilo C1-6, arilo, aril-alquilo C1-6, heteroarilo o heteroaril-alquilo C1-6, donde cada resto, excepto H, está opcionalmente sustituido, independientemente, de 1 a 3 veces, con halogeno o alquilo C1-4; R10 y R11 representan, independientemente, en cada caso H o alquilo C1-4; R19 y R20 representan, independientemente, en cada caso, H, alquilo C1-4, cicloalquilo, cicloalquil-alquilo C1-6, alquenilo C2-6, heterociclilo, heterociclil-alquilo C1-4, arilo, aril-alquilo C1-6, heteroarilo o un resto heteroaril-alquilo C1-6, donde cada resto, excepto H, puede estar sustituido, independientemente, de 1 a 3 veces con halogeno o alquilo C1-4; R3 representa arilo o heteroarilo, opcionalmente sustituido, independientemente, de 1 a 3 veces, con alquilo C1-4, halogeno, CN o CF3; R4 se selecciona entre el grupo que consiste en cicloalquil-alquilo C1-4, heteroarilo, heterociclilo, arilo, heteroaril-alquilo C1-2, heterociclil-alquilo C1-2, cicloalquil-alquenilo C2, aril-alquenilo C2, heteroaril-alquenilo C2 y heterociclil-alquenilo C2, donde cada resto está opcionalmente sustituido, independientemente, de 1 a 3 veces, con alquilo C1-4, F, CF3 o Cl; m es 0, 1 o 2; x es 0, 1, 2 o 3; q es 1, 2 o 3; y z es 0, 1, 2, 3 o 4; o una de sus sales farmacéuticamente aceptables.
ARP060105122A 2005-11-22 2006-11-22 Compuestos de pirimidinona o pirimidinationa, procesos de obtencion, compuestos intermediarios, composiciones farmaceuticas y usos. AR057625A1 (es)

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US73906705P 2005-11-22 2005-11-22
US73873105P 2005-11-22 2005-11-22

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CA2684633A1 (en) * 2007-04-20 2008-10-30 Schering Corporation Pyrimidinone derivatives and methods of use thereof
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FR2937321B1 (fr) * 2008-10-21 2010-10-22 Rhodia Operations Procede de fabrication de composes comprenant des fonctions nitriles
US9498471B2 (en) 2011-10-20 2016-11-22 The Regents Of The University Of California Use of CDK9 inhibitors to reduce cartilage degradation
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GB201217330D0 (en) 2012-09-28 2012-11-14 Univ Cardiff Therapeutic for treating inflammatory lung disorders
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CA2929394C (en) 2013-12-19 2021-11-16 Sunshine Lake Pharma Co., Ltd. Nitrogenous heterocyclic derivatives and their application in drugs
US10183949B2 (en) 2014-08-29 2019-01-22 The University Of Tokyo Pyrimidinone derivative having autotaxin-inhibitory activity
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KR20080080136A (ko) 2008-09-02
EP1951244A4 (en) 2010-08-25
IL191477A0 (en) 2009-02-11
EA200801414A1 (ru) 2008-10-30
UY29962A1 (es) 2007-06-29
BRPI0618900A2 (pt) 2011-09-27
WO2007062370A3 (en) 2007-11-22
CA2630117A1 (en) 2007-05-31
JP2009516756A (ja) 2009-04-23
EP1951244A2 (en) 2008-08-06
WO2007062370A2 (en) 2007-05-31
TW200738649A (en) 2007-10-16
MA30042B1 (fr) 2008-12-01
US20090137557A1 (en) 2009-05-28

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