AR065799A1 - Moduladores cannabinoides hexahidrocicloheptapirazol - Google Patents

Moduladores cannabinoides hexahidrocicloheptapirazol

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Publication number
AR065799A1
AR065799A1 ARP080101147A ARP080101147A AR065799A1 AR 065799 A1 AR065799 A1 AR 065799A1 AR P080101147 A ARP080101147 A AR P080101147A AR P080101147 A ARP080101147 A AR P080101147A AR 065799 A1 AR065799 A1 AR 065799A1
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Argentina
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hydroxy
halogen
positions
optionally substituted
alkyl
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ARP080101147A
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Janssen Pharmaceutica Nv
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Publication of AR065799A1 publication Critical patent/AR065799A1/es

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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • AHUMAN NECESSITIES
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    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/4161,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/04Heterocyclic 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

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  • Obesity (AREA)
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  • Heart & Thoracic Surgery (AREA)
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Abstract

Estos compuestos son utiles para tratar, mejorar o prevenir un síndrome, trastorno o enfermedad mediado por el receptor cannabinoide, tales como obesidad, trastornos metabolicos, enfermedades intestinales e infarto de miocardio. Reivindicacion 1:Un compuesto que tiene una estructura de acuerdo con la formula (1), o una sal, isomero, profármaco, metabolito o polimorfo del mismo donde las líneas discontinuas entre las posiciones 2-3 y posiciones 3a-8a en la formula (1) representan ubicacionespara cada uno de los dos dobles enlaces presentes cuando X1R1 está presente; las líneas discontinuas entre las posiciones 3-3a y posiciones 8a-1 en formula (1) representan ubicaciones para cada uno de los dos dobles enlaces presentes cuando X2R2está presente; la línea discontinua entre la posicion 8 y X4R4 en la formula (1) representa una ubicacion para un doble enlace; X1 está ausente o es alquileno inferior; X2 está ausente o es alquileno inferior; donde solo uno de X1R1 y X2R2 estánpresentes; X3 está ausente, es alquileno inferior, alquilideno inferior o -NH-; cuando la línea discontinua entre la posicion 8 y X4R4 está ausente, X4 está ausente, o es alquileno inferior, cuando la línea discontinua entre la posicion 8 y X4R4está presente, X4 está ausente; X5 está ausente o es alquileno inferior; R1 se selecciona entre hidrogeno, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), alquilo inferior-sulfonilo, arilo,cicloalquilo C3-12 o heterociclilo, donde cada arilo, cicloalquilo C3-12 o heterociclilo está opcionalmente sustituido en una o más posiciones con halogeno, aminosulfonilo, alquilo inferior-aminosulfonilo, alquilo (opcionalmente sustituido en una omás posiciones con halogeno, hidroxi o alcoxi inferior), hidroxi o alcoxi inferior (opcionalmente sustituido en una o más posiciones con halogeno o hidroxi); R2 se selecciona entre hidrogeno, alquilo (opcionalmente sustituido en una o más posicionescon halogeno, hidroxi o alcoxi inferior), alquilo inferior-sulfonilo, arilo, cicloalquilo C3-12 o heterociclilo, donde cada arilo, cicloalquilo C3-12 o heterociclilo está opcionalmente sustituido en una o más posiciones con halogeno, aminosulfonilo,alquilo inferior-aminosulfonilo, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), hidroxi o alcoxi inferior (opcionalmente sustituido en una o más posiciones con halogeno o hidroxi); R3 es -C(O)-Z1(R6), -SO2-NR7-Z2(R8) o -C(O)-NR9-Z3(R10); cuando la línea discontinua entre la posicion 8 y X4R4 está ausente, X4 está ausente o es alquileno inferior y R4 es hidroxi, alquilo inferior, alcoxi inferior, halogeno, arilo, cicloalquilo C3-12 oheterociclilo, donde cada arilo, cicloalquilo C3-12 o heterociclilo está opcionalmente sustituido en una o más posiciones con hidroxi, oxo, alquilo inferior (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior),alcoxi inferior (opcionalmente sustituido en una o más posiciones con halogeno o hidroxi) o halogeno; cuando la línea discontinua entre la posicion 8 y X4R4 está presente, X4. está ausente y R4, es CH-arilo o CH-heterociclilo, donde cada arilo oheterociclilo está opcionalmente sustituido en una o más posiciones con hidroxi, oxo, alquilo inferior (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), alcoxi inferior (opcionalmente sustituido en una o másposiciones con halogeno o hidroxi) o halogeno; R5 es hidrogeno, hidroxi, oxo, halogeno, amino, alquilo inferior-amino, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), alcoxi inferior (opcionalmentesustituido en una o más posiciones con halogeno o hidroxi), carboxi carbonilalcoxi, carbamoilo, carbamoilalquilo, arilo, ariloxi, arilalcoxi o heterociclilo; R6 es arilo, cicloalquilo C3-12 o heterociclilo cada uno opcionalmente sustituido con uno omás hidroxi, oxo, halogeno, amino, alquilo inferior-amino, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), alcoxi inferior (opcionalmente sustituido en una o más posiciones con halogeno o hidroxi),carboxi, carbonilalcoxi, carbamoilo, carbamoilalquilo, arilo, ariloxi, arilalcoxi o heterociclilo; R7 es hidrogeno o alquilo inferior; R8 es hidrogeno, arilo, cicloalquilo C3-12 o heterociclilo, donde arilo, cicloalquilo C3-12 o heterociclilo estáncada uno opcionalmente sustituido con uno o más hidroxi, oxo, halogeno, amino, alquilo inferior-amino, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior), alcoxi inferior (opcionalmente sustituido enuna o más posiciones con halogeno o hidroxi), carboxi, carbonilalcoxi, carbamoilo, carbamoilalquilo, arilo, ariloxi, arilalcoxi o heterociclilo; R9 es hidrogeno o alquilo inferior; R10 es hidrogeno, arilo, cicloalquilo C3-12 o heterociclilo, dondecada arilo, cicloalquilo C3-12 o heterociclilo está opcionalmente sustituido con uno o más hidroxi, oxo, halogeno, amino, alquilo inferior-amino, alquilo (opcionalmente sustituido en una o más posiciones con halogeno, hidroxi o alcoxi inferior),alcoxi inferior (opcionalmente sustituido en una o más posiciones con halogeno o hidroxi), carboxi, carbonilalcoxi, carbamoilo, carbamoilalquilo, aminosulfonilo, alquilo inferior-aminosulfonilo, arilo, ariloxi, arilalcoxi o heterociclilo; Z1 y Z2están ausentes o son alquilo; y Z3 está ausente, -NH-, -SO2- o alquilo (donde alquilo está opcionalmente sustituido en una o más posiciones con halogeno, hidroxi, alquilo inferior, alcoxi inferior, carboxi o carbonilalcoxi).
ARP080101147A 2007-03-20 2008-03-19 Moduladores cannabinoides hexahidrocicloheptapirazol AR065799A1 (es)

Applications Claiming Priority (1)

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US11/688,552 US8378117B2 (en) 2005-09-23 2007-03-20 Hexahydro-cycloheptapyrazole cannabinoid modulators

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US (1) US8378117B2 (es)
EP (1) EP2139328A4 (es)
JP (1) JP2010529949A (es)
KR (1) KR20100015602A (es)
CN (1) CN101677557A (es)
AR (1) AR065799A1 (es)
AU (1) AU2008229202A1 (es)
BR (1) BRPI0809037A2 (es)
CA (1) CA2681468A1 (es)
CL (1) CL2008000799A1 (es)
CO (1) CO6220909A2 (es)
IL (1) IL200957A0 (es)
MX (1) MX2009010157A (es)
NZ (1) NZ579649A (es)
PE (1) PE20090061A1 (es)
TW (1) TW200901976A (es)
UA (1) UA98487C2 (es)
WO (1) WO2008115705A2 (es)

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CO6220909A2 (es) 2010-11-19
UA98487C2 (en) 2012-05-25
WO2008115705A3 (en) 2009-01-15
KR20100015602A (ko) 2010-02-12
CA2681468A1 (en) 2008-09-25
JP2010529949A (ja) 2010-09-02
CL2008000799A1 (es) 2008-09-26
EP2139328A4 (en) 2010-07-07
BRPI0809037A2 (pt) 2014-09-16
CN101677557A (zh) 2010-03-24
EP2139328A2 (en) 2010-01-06
US20080070968A1 (en) 2008-03-20
WO2008115705A2 (en) 2008-09-25
NZ579649A (en) 2011-12-22
US8378117B2 (en) 2013-02-19
TW200901976A (en) 2009-01-16
AU2008229202A1 (en) 2008-09-25
MX2009010157A (es) 2009-10-12
PE20090061A1 (es) 2009-01-26
IL200957A0 (en) 2010-05-17

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