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AR058557A1 - Derivados de pirimidina, procesos de preparacion, y composiciones farmaceuticas que los comprenden - Google Patents

Derivados de pirimidina, procesos de preparacion, y composiciones farmaceuticas que los comprenden

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Publication number
AR058557A1
AR058557A1 ARP060105613A ARP060105613A AR058557A1 AR 058557 A1 AR058557 A1 AR 058557A1 AR P060105613 A ARP060105613 A AR P060105613A AR P060105613 A ARP060105613 A AR P060105613A AR 058557 A1 AR058557 A1 AR 058557A1
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AR
Argentina
Prior art keywords
alkyl
group
independently selected
cycloalkyl
optionally
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ARP060105613A
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Pfizer Ltd
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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
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/48—Two nitrogen atoms
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/02—Nasal agents, e.g. decongestants
    • A—HUMAN NECESSITIES
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    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/16—Central respiratory analeptics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00—Drugs for disorders of the urinary system
    • A61P13/10—Drugs for disorders of the urinary system of the bladder
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P15/00—Drugs for genital or sexual disorders; Contraceptives
    • A61P15/10—Drugs for genital or sexual disorders; Contraceptives for impotence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/02—Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P31/12—Antivirals
    • 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
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/08—Antiallergic 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
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • 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
    • C07D239/50—Three nitrogen atoms
    • 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
    • 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
    • C07D403/12—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 chain containing hetero atoms as chain links
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    • 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
    • C07D405/12—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 linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
    • 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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D497/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms
    • C07D497/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having oxygen and sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D497/08—Bridged systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pulmonology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Neurosurgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Gynecology & Obstetrics (AREA)
  • Endocrinology (AREA)
  • Reproductive Health (AREA)
  • Oncology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Otolaryngology (AREA)
  • Vascular Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Reivindicacion 1: Un compuesto de formula (1): o una sal o solvato farmacéutica y/o veterinaria aceptable del mismo, en la que: R1 es alquiloC1-8, cicloalquilC3-7-alquiloC-06 opcionalmente sustituido con metilo, alcoxialquilo que contiene 3 a 8 átomos de carbono, het-alquiloC0-6, CF3-alquiloC1-6, CF3OalquiloC2-3, aril-alquiloC0-6 o hidroxialquiloC1-6; R2 es het, con la condicion de que el grupo het contenga al menos un átomo de nitrogeno o esté sustituido con un grupo que contenga al menos un átomo de nitrogeno; o R2 es NH(CH2)2NH2, NH(CH2)2NHCH3, o NH(CH2)2NH(CH3)2; R3 es H, alquilo C1-8, (CH2)p-cicloalquilo C3-7, alcoxialquilo que contiene 3 a 8 átomos de carbono, (CH2)nCF3, (CH2)xOCF3 o hidroxialquiloC1-6; o R3 y R2 junto con el átomo de nitrogeno al que están unidos forman un grupo heterocíclico no aromático de 4 a 8 miembros que contiene opcionalmente uno o más heteroátomos adicionales o grupos seleccionados independientemente entre N, O, S, S(O) y S(O)2, en el que el grupo heterocíclico es opcionalmente un grupo bicíclico unido mediante un enlace puente, un grupo bicíclico espiro o está opcionalmente condensado a un grupo carbocíclico de 3, 4, 5 o 6 miembros o un grupo heterocíclico de 4, 5 o 6 miembros que contiene al menos un miembro del anillo seleccionado independientemente entre N, O, D, S(O) y S(O)2, y en el que el sistema de anillos como un todo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre alquiloC1-6, NR6R7, (CH2)a-cicloalquilo C3-7, alcoxialquilo que contiene 2 a 8 átomos de carbono, (CH2)bhet1, (CH2)cCF3, (CH2)yOCF3, (CH2)darilo e hidroxialquiloC1-6, con la condicion de que el sistema de anillos como un todo contenga al menos dos átomos de nitrogeno o contenga un átomo de nitrogeno y esté sustituido con un grupo que contenga al menos un átomo de nitrogeno; R4 es H; o R1 y R4 junto con el átomo de nitrogeno al que están unidos forman un grupo heterocíclico no aromático de 4 a 8 miembros que opcionalmente contiene uno o más heteroátomos adicionales o grupos seleccionados independientemente entre N, O, S, S(O) y S(O)2, en los que el grupo heterocíclico es opcionalmente un grupo bicíclico unido mediante un enlace puente o está opcionalmente condensado a un grupo carbocíclico de 3, 4, 5, o 6- miembros o un grupo heterocíclico de 4, 5 o 6 miembros que contiene al menos un miembro del anillo seleccionado independientemente entre N, O, S, S(O) y S(O)2, y en el que el sistema de anillos como un todo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre alquiloC1-6, fluoro, NR9R10, (CH2)e-cicloalquilo C3-7, alcoxialquilo que contiene 2 a 8 átomos de carbono, (CH2)fhet1, (CH2)gCF3, (CH2)zOCF3, (CH2)harilo e hidroxialquilo C1-6; R5 es H o NR11R12; R6 y R7 cada uno se selecciona independientemente enrte H, alquiloC1-6 y (CH2)j-cicloalquiloC3-7; o R6 y R7, junto con el átomo de nitrogeno al que están unidos, forman un grupo heterocíclico de 4, 5 o 6 miembros; R8 es H o alquiloC1-3; R9 y R10 cada uno se selecciona independientemente entre H, alquiloC1-6 y (CH2)k-cicloalquiloC3-7; o R9 y R10, junto con el átomo de nitrogeno al que están unidos, forman un grupo heterocíclico de 4, 5 o 6 miembros; R11 y R12 cada uno se selecciona independientemente entre H, alquiloC1-6 y (CH2)l-cicloalquiloC3-7; o R11 y R12, junto con el átomo de nitrogeno al que están unidos, forman un grupo heterocíclico de 4, 5 o 6 miembros; R13 y R14 cada uno se selecciona independientemente entre H, alquiloC1-6 y (CH2)m-cicloalquilo C3-7; o R13 y R14, junto con el átomo de nitrogeno al que están unidos, forman un grupo heterocíclico de 4, 5 o 6 miembros; a, b, c, d, e, f, g, h, j, k, l, m, y p cada uno se seleccional independientemente entre 0, 1, 2 y 3; n es 1, 2 o 3; x es 2 o 3, en el que si x es 3, entonces el grupo (CH2)3 puede reemplazarse por un grupo alquilo ramificado que contiene 3 átomos de carbono; y y z cada uno se selecciona independientemente entre 1, 2 y 3 arilo es fenilo, naftilo, antracilo o fenantrilo, cada uno opcionalmente sustituido con uno o más grupos seleccionados independientemente entre alquiloC1-8, alcoxiC1-8, OH, halo, CF3, CHF2, OCF3, OCHF2, SCF3, hidroxi-alquiloC1-6, alcoxiC1-4-alquiloC1-6, alquilC1-4-S-alquiloC1-4, arilo1, het1, O-arilo1, O-het1, S-arilo1, Shet1, CF2CF3, CH2CF3, CF2CH3, C(O)NR13R14, cicloalquiloC3-8, cicloalquilC3-7-alquiloC1-4, cicloalquilC3-7-alcoxiC1-4, cicloalquil C3-7-O-alquiloC1-4, cicloalquilC3-7-alcoxiC1-4-alquiloC1-4, O-cocloalquiloC3-7 y S-cicloalquiloC3-7, en el que los grupos arilo1 y het1 están opcionalmente sustituidos con al menos un grupo seleccionado entre alquiloC1-6, cicloalquiloC3- 7, alcoxiC1-6, O-cicloalquiloC3-7, halo, CN, OH, CF3, CHF2, OCF3, OCHF2, hidroxialquiloC1-6, alcoxiC1-4-alquiloC1-4, S-alquilo C1-6 y SCF3; het es un grupo heterocíclico no aromático de 4 a 8 miembros que contiene al menos un heteroátomo o grupo seleccionado independientemente entre N, O, S, S(O) y S(O)2, en el que el grupo heterocíclico es opcionalmente un grupo heterocíclico es opcionalmente un grupo bicíclico unido mediante un enlace puente o está opcionalmente condensado a un grupo carbocíclico de 3, 4, 5, o 6 miembros o un grupo heterocíclico de 4, 5, o 6 miembros que contiene al menos un miembro del anillo seleccionado independientemente entre N, O, S, S(O) y S(O)2, y en el que el sistema de anillos como un todo está opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente entre alquiloC1-6, NR6R7, (CH2)a-cicloalquiloC3-7, alcoxialquilo que contiene 2 a 8 átomos de carbono, (CH2)bhet1, (CH2)cCF3, (CH2)yOCF3, (CH2)darilo e hidroxialquiloC1-6; arilo1 es fenilo, naftilo, antracilo o fenantrilo; y het1 es un heterociclo aromático o no aromático de 4, 5 o 6 miembros que contiene al menos un heteroátomo de N, O o S, opcionalmente condensado a un grupo carbocíclico de 4, 5 o 6- miembros o un segundo heterociclo de 4, 5 o 6 miembros que contiene al menos un heteroátomo de N, O o S.
ARP060105613A 2005-12-20 2006-12-19 Derivados de pirimidina, procesos de preparacion, y composiciones farmaceuticas que los comprenden AR058557A1 (es)

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US (1) US7943628B2 (es)
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JP (1) JP5166280B2 (es)
KR (2) KR20120025010A (es)
CN (1) CN101341134B (es)
AP (1) AP2008004486A0 (es)
AR (1) AR058557A1 (es)
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EA (1) EA200801381A1 (es)
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