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AR049771A1 - Derivados de pirimidina para uso como ligandos del receptor vaniloide y su empleo en tratamientos - Google Patents

Derivados de pirimidina para uso como ligandos del receptor vaniloide y su empleo en tratamientos

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Publication number
AR049771A1
AR049771A1 ARP050100490A ARP050100490A AR049771A1 AR 049771 A1 AR049771 A1 AR 049771A1 AR P050100490 A ARP050100490 A AR P050100490A AR P050100490 A ARP050100490 A AR P050100490A AR 049771 A1 AR049771 A1 AR 049771A1
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AR
Argentina
Prior art keywords
nrara
alkyl
orb
disorders
inflammatory
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Application number
ARP050100490A
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English (en)
Inventor
Hui-Ling Wang
Chenera Balan
Elizabeth M Doherty
Jim Falsey
Vijay Keshav Gore
Jodie Katon
Mark Henry Norman
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Amgen Inc
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Publication of AR049771A1 publication Critical patent/AR049771A1/es

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    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
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    • 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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    • 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
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    • 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
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    • C07—ORGANIC CHEMISTRY
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    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D471/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Immunology (AREA)
  • Rheumatology (AREA)
  • Reproductive Health (AREA)
  • Endocrinology (AREA)
  • Psychiatry (AREA)
  • Nutrition Science (AREA)
  • Ophthalmology & Optometry (AREA)
  • Otolaryngology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Eteres de pirimidina y composiciones que los contienen para el tratamiento de dolores agudos, inflamatorios o neuropáticos, dolores dentales, dolores de cabeza en general, migrana, dolor de cabeza ôen racimoö, síndromes mixtos vasculares y no vasculares, dolor de cabeza por tension, inflamacion general, artritis, enfermedades reumáticas, osteoartritis, enfermedad inflamatoria intestinal, trastornos oculares inflamatorios, trastornos, trastornos vesiculares inflamatorios o inestables, psoriasis, molestias de la piel con componentes inflamatorios, patologías inflamatorias cronica, dolor inflamatorio e hiperalgesia y alodinia asociadas, dolor neuropático e hiperalgesia y alodinia asociadas, dolor neuropático diabético, causalgia, dolor mantenido por el simpático, síndrome de deaferenciacion, asma, danos o disfunciones de tejidos epiteliales, herpes simples, trastornos de motilidad visceral en las regiones respiratorias, genitourinaria, gastrointestinal o vascular, heridas, quemaduras, reacciones alérgicas de la piel, prurito, vitiligo, trastornos gastrointestinales generales, ulceras gástricas, ulceras duodenales, diarrea, lesiones gástricas inducidas por agentes necrotizantes, crecimiento del cabello, rinitis vasomotora o alérgica, trastornos bronquiales o trastornos de la vesícula. Reivindicacion 1: Un compuesto que tiene la estructura de formula (1), o cualquier sal o hidrato farmacéuticamente aceptable del mismo, donde: X es N o C; donde, cuando X es N, la línea punteada representa un enlace simple, y cuando X es C, entonces la línea punteada representa un enlace simple o doble; R1 es un anillo de 5, 6 o 7 miembros, parcialmente saturado o no saturado que contiene 1, 2, 3 o 4 átomos seleccionados de N, O y S, donde los átomos de carbono del anillo están sustituidos por 0, 1 o 2 grupos oxo y el anillo es sustituido por 0, 1, 2 o 3 sustituyentes seleccionados entre alquilo C1-8, haloalquilo C1-4, halo, ciano, nitro, -C(=O)Rb, - C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -Oalquilo C2-6NRaRa, -Oalquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, - N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaalquilo C2-6NRaRa y -NRaalquilo C2-6ORa; o R1 es fenilo sustituido por 1, 2 o 3 sustituyentes seleccionados entre alquilo C1-8, haloalquilo C1- 4, halo, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -Oalquilo C2-6NRaRa, -Oalquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, -S(=O)2N(Ra)C(=O)ORb, - S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaalquilo C2-6NRaRa y -NRaalquilo C2-6ORa; R2 es un anillo bicíclico de 8, 9, 10 u 11 miembros saturado o no saturado que contiene 1, 2, 3 o 4 átomos seleccionados entre N, o y S, donde los átomos de carbono del anillo están sustituidos por 0, 1 o 2 grupos oxo y el anillo es sustituido por 0, 1, 2 o 3 sustituyentes seleccionados entre alquilo C1-8, haloalquilo C1-4, halo, ciano, nitro, -C(=O)Rb, -C(=O)ORb, -C(=O)NRaRa, -C(=NRa)NRaRa, -ORa, -OC(=O)Rb, -OC(=O)NRaRa, -OC(=O)N(Ra)S(=O)2Rb, -Oalquilo C2-6NRaRa, -Oalquilo C2-6ORa, -SRa, -S(=O)Rb, -S(=O)2Rb, -S(=O)2NRaRa, -S(=O)2N(Ra)C(=O)Rb, - S(=O)2N(Ra)C(=O)ORb, -S(=O)2N(Ra)C(=O)NRaRa, -NRaRa, -N(Ra)C(=O)Rb, -N(Ra)C(=O)ORb, -N(Ra)C(=O)NRaRa, -N(Ra)C(=NRa)NRaRa, -N(Ra)S(=O)2Rb, -N(Ra)S(=O)2NRaRa, -NRaalquilo C2-6NRaRa y -NRaalquilo C2-6ORa; R3 y R3' son independientemente, en cada caso, H, metilo o etilo; o R3 y R3' juntos pueden combinarse con el átomo de carbono al cual están ligados para formar un ciclopropilo; R4 es H o metilo; Ra es independientemente, en cada caso, H o Rb; y Rb es independientemente, en cada caso, fenilo, bencilo o alquilo C1-6, estando el fenilo, bencilo y alquilo C1-6 sustituidos por 0, 1, 2 o 3 sustituyentes seleccionados entre halo, alquilo C1-4, haloalquilo C1-3, -Oalquilo C1-4, -NH2, -NHalquilo C1-4 y -N(alquilo C1-4)alquilo C1-4.
ARP050100490A 2004-02-11 2005-02-11 Derivados de pirimidina para uso como ligandos del receptor vaniloide y su empleo en tratamientos AR049771A1 (es)

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EP (1) EP1720868B1 (es)
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MY139645A (en) 2009-10-30
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TWI295670B (en) 2008-04-11
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CN1953976A (zh) 2007-04-25
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AU2005212517A1 (en) 2005-08-25

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