AR059985A1 - Tetrahidro-pirimidoazepinas como moduladores de trpv1 - Google Patents

Tetrahidro-pirimidoazepinas como moduladores de trpv1

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Publication number
AR059985A1
AR059985A1 ARP070101128A ARP070101128A AR059985A1 AR 059985 A1 AR059985 A1 AR 059985A1 AR P070101128 A ARP070101128 A AR P070101128A AR P070101128 A ARP070101128 A AR P070101128A AR 059985 A1 AR059985 A1 AR 059985A1
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AR
Argentina
Prior art keywords
alkyl
substituted
independently
halo
saturated monocyclic
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ARP070101128A
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English (en)
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Janssen Pharmaceutica Nv
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Publication of AR059985A1 publication Critical patent/AR059985A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
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    • A61P1/14Prodigestives, e.g. acids, enzymes, appetite stimulants, antidyspeptics, tonics, antiflatulents
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  • Organic Chemistry (AREA)
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  • General Health & Medical Sciences (AREA)
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  • Urology & Nephrology (AREA)
  • Pulmonology (AREA)
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Abstract

Dichos compuestos pueden ser usados en composiciones farmacéuticas y para tratar trastornos y afecciones médicas intermediadas por TRPV1 Por lo tanto, los compuestos pueden ser administrados por ejemplo en dolor, prurito, tos, asma y enfermedad inflamatoria del intestino. Reivindicacion 1: Un compuesto de formula (1): donde: R1 es -H; NRaRb; un grupo -alquilo C1-6, -alquiloO C1-6, -S-alquilo C1-6, o -SO2-alquilo C1-6 no sustituido o sustituido con un sustituyente -OH, -Oalquilo C1-4, - NReRf, o halo sustituido; o un grupo cicloalquilo monocíclico no sustituido o sustituido con un -alquilo C1-6, -OH, -Oalquilo C1-4, -NReRf, o halo; donde Ra y Rb cada uno independientemente es -H; -alquilo C1-6, un grupo -alquilo C2-3 sustituido con -OH, -Oalquilo C1-4, -NRcRd, o halo sustituido; o un cicloalquilo monocíclico saturado, -alquilo C1-(cicloalquilo monocíclico saturado), heterocicloalquilo monocíclico saturado, -alquilo C1-(heterocicloalquilo monocíclico saturado), fenilo, o un grupo bencilo no sustituido o sustituido con uno, dos o tres porciones independientemente seleccionadas del grupo que consiste en -alquilo C1-6, OH, -Oalquilo C1-4, -NRpRq, y halo sustituidos, o Ra y Rb tomados conjuntamente con su nitrogeno de union forman un grupo heterocicloalquilo monocíclico saturado no sustituido o sustituido con uno, dos o tres porciones independientemente seleccionadas del grupo que consiste en -alquilo C1-6, -OH, -Oalquilo C1-4, -NRpRq, halo, -CO2H, y sustituyentes bencilo; donde Rc y Rd son cada uno independientemente -H o -alquilo C1-6, o Rc y Rd tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; donde Rp y Rq son cada uno independientemente -H o -alquilo C1-6 o Rp y Rq tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; donde Re y Rf son cada uno independientemente -H o -alquilo C1-6, o Re y Rf tomados conjuntamente con su nitrogeno de union forman un heterocicloalquilo monocíclico saturado; R2 es -H o -alquilo C1-6, R3 es un grupo fenilo, bencilo, fenetilo, indanilo, tiazolilo, tiofenilo, piridilo, pirimidinilo, pirazinilo, piridazinilo, quinolinilo, o isoquinolinilo no sustituido o sustituido con uno, dos, o tres sustituyentes Rg; donde cada sustituyente Rg es -alquilo C1-6, -OH, -Oalquilo C1-6, fenoxi, -CN, -NO2, N(Rh)Ri, -C(O)N(Rh)Ri, -N(Rh)C(O)Ri, -N(Rh)SO2 alquilo C1-6, -C(O)alquilo C1-6, -S(O)0-2-alquilo C1-6, -SO2CF3, SO2N(Rh)Ri, -SCF3, halo, -CF3, -OCF3, -COOH, C(O)Oalquilo C1-6, -C(Rj)2-CN, o -C(Rj)2-OH; o dos sustituyentes Rg adyacentes tomados conjuntamente forman -Oalquilo C1-2O-; donde Rh y Ri son cada uno independientemente -H o -alquilo C1-6; donde cada Rj es independientemente -H o -alquilo C1-6; y Ar es un grupo fenilo, piridilo, imidazolilo, pirimidinilo, piridazinilo, o un grupo heteroarilo fusionado-bicíclico no sustituido o sustituido con uno, dos o tres sustituyentes Rk; donde cada sustituyente Rk es independientemente -alquilo C1-6, -OH, -Oalquilo C1-6, fenoxi, -CN, -NO2, N(Rl)Rm, -C(O)N(Rl)Rm, N(Rl)C(O)Rm, -N(Rl)SO2 alquilo C1-6, -N(Rl)SO2CF3, -C(O)alquilo C1-6, -S(O)0-2-alquilo C1-6, -SO2CF3, SO2N(Rl)Rm, -SCF3, halo, -CF3, - OCF3, -COOH, o -C(O)Oalquilo C1-6; o dos sustituyentes Rk adyacentes tomados conjuntamente forman -Oalquilo C1-2O-; donde Rl y Rm son cada uno independientemente -H, -alquilo C1-6, o -CF3; o una sal farmacéuticamente aceptable, un profármaco farmacéuticamente aceptable o un metabolito de dicho compuesto farmacéuticamente activo.
ARP070101128A 2006-03-21 2007-03-20 Tetrahidro-pirimidoazepinas como moduladores de trpv1 AR059985A1 (es)

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US78541506P 2006-03-21 2006-03-21

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EP (1) EP2024368B1 (es)
JP (1) JP5232768B2 (es)
KR (1) KR101461376B1 (es)
CN (1) CN101448835B (es)
AR (1) AR059985A1 (es)
AU (1) AU2007227203B2 (es)
BR (1) BRPI0709034B1 (es)
CA (1) CA2646977C (es)
CR (1) CR10387A (es)
DK (1) DK2024368T3 (es)
EA (1) EA017069B1 (es)
EC (1) ECSP088807A (es)
ES (1) ES2474152T3 (es)
HK (1) HK1129888A1 (es)
HR (1) HRP20140664T1 (es)
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