AR035349A1 - Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos - Google Patents

Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos

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Publication number
AR035349A1
AR035349A1 ARP010104760A ARP010104760A AR035349A1 AR 035349 A1 AR035349 A1 AR 035349A1 AR P010104760 A ARP010104760 A AR P010104760A AR P010104760 A ARP010104760 A AR P010104760A AR 035349 A1 AR035349 A1 AR 035349A1
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Argentina
Prior art keywords
alkyl
mono
halogen
compounds
alkoxy
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ARP010104760A
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English (en)
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Smithkline Beecham Plc
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Publication of AR035349A1 publication Critical patent/AR035349A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D221/00Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00
    • C07D221/02Heterocyclic compounds containing six-membered rings having one nitrogen atom as the only ring hetero atom, not provided for by groups C07D211/00 - C07D219/00 condensed with carbocyclic rings or ring systems
    • C07D221/04Ortho- or peri-condensed ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • 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
    • 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
    • A61P3/08Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/12Antihypertensives
    • CCHEMISTRY; METALLURGY
    • C04CEMENTS; CONCRETE; ARTIFICIAL STONE; CERAMICS; REFRACTORIES
    • C04BLIME, MAGNESIA; SLAG; CEMENTS; COMPOSITIONS THEREOF, e.g. MORTARS, CONCRETE OR LIKE BUILDING MATERIALS; ARTIFICIAL STONE; CERAMICS; REFRACTORIES; TREATMENT OF NATURAL STONE
    • C04B35/00Shaped ceramic products characterised by their composition; Ceramics compositions; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/622Forming processes; Processing powders of inorganic compounds preparatory to the manufacturing of ceramic products
    • C04B35/626Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B
    • C04B35/63Preparing or treating the powders individually or as batches ; preparing or treating macroscopic reinforcing agents for ceramic products, e.g. fibres; mechanical aspects section B using additives specially adapted for forming the products, e.g.. binder binders
    • C04B35/632Organic additives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/68Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
    • C07D211/72Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D211/74Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/36Sulfur atoms
    • 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Ceramic Engineering (AREA)
  • Manufacturing & Machinery (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Rheumatology (AREA)
  • Structural Engineering (AREA)
  • Materials Engineering (AREA)
  • Inorganic Chemistry (AREA)
  • Hematology (AREA)
  • Pain & Pain Management (AREA)
  • Obesity (AREA)
  • Endocrinology (AREA)
  • Emergency Medicine (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Immunology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pyridine Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Compuestos de pirimidinona de fórmula (1) en la que: R1 es un grupo arilo, opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquiltio C1-6, hidroxi, halógeno, CN, y mono a perfluoroalquilo C1-4, mono a perfluoro-alcoxi C1-4 arilo, y arilalquilo C1-4; R2 es halógeno, alquilo C1-3, alcoxi C1-3, hidroxialquilo C1-3, alquiltio C1-3, alquilsulfinilo C1-3, aminoalquilo C1-3, mono- o di-alquil C1-3 aminoalquilo C1-3, alquil C1-3 carbonilaminoalquilo C1-3, alcoxi C1-3 alquil C1-3 carbonilaminoalquilo C1-3, alquil C1-3 sulfonilaminoalquilo C1-3, alquil C1-3 carboxi, alquil C1-3 carboxialquilo C1-3; R3 es hidrógeno, halógeno, alquilo C1-3, o hidroxialquilo C1-3; o R2 y R3 junto con los átomos de carbono del anillo de piridona a los que están unidos forman un anillo carbocíclico condensado de 5- o 6-miembros; o R2 y R3 junto con los átomos de carbono del anillo de piridona a los que están unidos forman un anillo benzo o heteroarílico condensado, opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes, que pueden ser iguales o diferentes, seleccionados de halógeno, alquilo C1-4, ciano, alcoxi C1-3-alquilo C1-3, alcoxi C1-4, o alquil C1-4 tio, o mono a perfluoroalquilo C1-4; R4 es hidrógeno, alquilo C1-6 que puede estar sustituido o no sustituido con 1, 2 o 3 sustituyentes seleccionados de hidroxi, halógeno, OR7, COR7, carboxi, COOR7, CONR9R10, NR9R10, NR7COR8, mono- o di-(hidroxialquil C1-6) amino y N-hidroxialquil C1-6-N-alquil C1-6 amino; o R4 es Het-alquilo C0-4 en el que Het es un anillo heterociclilo de 5 a 7 miembros que comprende N y opcionalmente O o S, y en el que N puede estar sustituido con COR7, COOR7, CONR9R10, o alquilo C1-6 opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de hidroxi, halógeno, OR7, COR7, carboxi, COOR7, CONR9R10 o NR9R10, por ejemplo, piperidin-4-ilo, pirrolidin-3-ilo; R5 es un arilo o un anillo heteroarílico opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquil C1-6 tio, arilalcoxi C1-6, hidroxi, halógeno, CN, COR7, carboxi, COOR7, NR7COR8, CONR9R10, SO2NR9R10, NR7SO2R8, NR9R10, mono a perfluoroalquilo C1-4 y mono a perfluoroalcoxi C1-4; R6 es un arilo o un anillo heteroarílico que está además opcionalmente sustituido con 1, 2, 3 o 4 sustituyentes que pueden ser iguales o diferentes seleccionados de alquilo C1-6, alcoxi C1-6, alquil C1-6 tio, alquil C1-6 sulfonilo, arilalcoxi C1-6, hidroxi, halógeno, CN, COR7, carboxi, COOR7, CONR9R10, NR7COR8, SO2NR9R10, NR7SO2R8, NR9R10, mono a perfluoroalquilo C1-4 y mono a perfluoro-alcoxi C1-4, o alquilo C5-10; R7 y R8 son independientemente hidrógeno o alquilo C1-12, por ejemplo alquilo C1-4 (v-g- metilo o etilo); R9 y R10 que pueden ser iguales o diferentes se seleccionan cada uno de hidrógeno, o alquilo C1-12, o R9 y R10 junto con el nitrógeno al que están unidos forman un anillo de 5- a 7 miembros que contiene opcionalmente uno o más heteroátomos adicionales seleccionados de oxígeno, nitrógeno y azufre, y está opcionalmente sustituido con uno o dos sustituyentes seleccionados de hidroxi, oxo, alquilo C1-4, alquil C1-4 carboxi, arilo, v-g- fenilo, o aralquilo, v-g- bencilo, por ejemplo, morfolina o piperazina; y X es un grupo alquileno C2-4 (opcionalmente sustituido con 1, 2 o 3 sustituyentes seleccionados de metilo y etilo), CH=CH, (CH2)nS o (CH2)nO en las que n es 1, 2 o 3. Estos compuestos son inhibidores de la enzima Lp-PLA2 y son de utilidad en terapia, en particular para tratar arteriosclerosis. También se dan a conocer: composiciones farmacéuticas que los comprenden, el uso de tales compuestos en la fabricación de medicamentos, y un proceso para la preparación de dichos compuestos. El proceso para preparar un compuesto de fórmula (1) comprende hacer reaccionar un compuesto ácido de fórmula (2) en la que X, R1, R2 y R3 son como se definen aquí anteriormente, con un compuesto de amino de fórmula (3): R6-R5-CH2NHR4 en la que R4, R5 y R6 son como se definen aquí anteriormente; en condiciones de formación de amidas.
ARP010104760A 2000-10-10 2001-10-10 Compuestos de pirimidinona, composiciones farmaceuticas que los comprenden, uso de tales compuestos en la fabricacion de medicamentos y proceso para la preparacion de dichos compuestos AR035349A1 (es)

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Application Number Priority Date Filing Date Title
GBGB0024808.8A GB0024808D0 (en) 2000-10-10 2000-10-10 Novel compounds

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AR035349A1 true AR035349A1 (es) 2004-05-12

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Country Status (29)

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US (2) US20040063753A1 (es)
EP (2) EP1326841B1 (es)
JP (1) JP4212354B2 (es)
KR (1) KR100824134B1 (es)
CN (2) CN1951917B (es)
AR (1) AR035349A1 (es)
AT (1) ATE538096T1 (es)
AU (2) AU2002210524B2 (es)
BR (1) BRPI0114576B1 (es)
CA (1) CA2425268C (es)
CY (2) CY1112442T1 (es)
CZ (1) CZ304558B6 (es)
DK (2) DK1326841T3 (es)
ES (2) ES2378059T3 (es)
GB (1) GB0024808D0 (es)
GC (1) GC0000307A (es)
HK (2) HK1144941A1 (es)
HU (1) HU230767B1 (es)
IL (2) IL155278A0 (es)
MX (1) MXPA03003176A (es)
MY (1) MY135766A (es)
NO (1) NO325107B1 (es)
NZ (1) NZ525225A (es)
PL (1) PL207560B1 (es)
PT (2) PT2258688E (es)
SI (2) SI2258688T1 (es)
TW (1) TWI293293B (es)
WO (1) WO2002030904A1 (es)
ZA (1) ZA200302785B (es)

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