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AR101297A1 - IMIDAZOPIRIDAZINE COMPOUNDS AS PDE4 INHIBITORS - Google Patents

IMIDAZOPIRIDAZINE COMPOUNDS AS PDE4 INHIBITORS

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Publication number
AR101297A1
AR101297A1 ARP150102349A ARP150102349A AR101297A1 AR 101297 A1 AR101297 A1 AR 101297A1 AR P150102349 A ARP150102349 A AR P150102349A AR P150102349 A ARP150102349 A AR P150102349A AR 101297 A1 AR101297 A1 AR 101297A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
members
group
heterocycloalkyl
independently selected
Prior art date
Application number
ARP150102349A
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Spanish (es)
Original Assignee
Pfizer
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Publication date
Application filed by Pfizer filed Critical Pfizer
Publication of AR101297A1 publication Critical patent/AR101297A1/en

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Abstract

Composiciones farmacéuticas que comprenden los compuestos, tratamiento de enfermedades medidas por PDE4 usando éstos compuestos. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde: R¹ se selecciona a partir del grupo que consiste de porciones de -(CH₂)ₘ-C₃₋₈ cicloalquilo, -(CH₂)ₘ-(4 a 10 miembros)heterocicloalquilo, -(CH₂)ₘ-C₆₋₁₀ arilo y -(CH₂)ₘ-(5 a 14 miembros)heteroarilo y, en donde sea químicamente permisible, el C₃₋₈-cicloalquilo, (4 a 10 miembros)heterocicloalquilo, C₆₋₁₀-arilo y (5 a 14 miembros)heteroarilo son opcionalmente sustituidas con uno a cinco R²; cuando están presentes, cada R² se selecciona independientemente a partir del grupo que consiste de halógeno, oxo, ciano, hidroxi, -SF₅, nitro, C₁₋₆ alquilo opcionalmente sustituido, C₂₋₆ alquenilo opcionalmente sustituido, C₂₋₆ alquinilo opcionalmente sustituido, C₁₋₆ alquiltio opcionalmente sustituido, C₁₋₆ alcoxi opcionalmente sustituido, -N(R⁴)(R⁵), -N(R⁴)(C=(O)R⁵), -C(=O)N(R⁴)(R⁵), -C(=O)-O-N(R⁴)(R⁵), -C(=O)-R⁴, -C(=O)-OR⁴, y C₃₋₈ cicloalquilo opcionalmente sustituido; cuando están presentes, cada R³ se selecciona independientemente a partir del grupo que consiste de halógeno, ciano, hidroxi, -SF₅, nitro, C₁₋₆ alquilo opcionalmente sustituido, C₂₋₆ alquenilo opcionalmente sustituido, C₂₋₆ alquinilo opcionalmente sustituido, C₁₋₆ alquiltio opcionalmente sustituido, C₁₋₆ alcoxi opcionalmente sustituido, -N(R⁴)(R⁵), -N(R⁴)(C=(O)R⁵), -C(=O)N(R⁴)(R⁵), -C(=O)-O-N(R⁴)(R⁵), -C(=O)-R⁴ y -C(=O)-OR⁴; R⁴ y R⁵ cada uno se selecciona independientemente a partir del grupo que consiste de hidrógeno y C₁₋₆ alquilo opcionalmente sustituido; R⁶ y R⁷ cada uno se selecciona independientemente a partir del grupo que consiste de hidrógeno, C₁₋₆ alquilo opcionalmente sustituido, -(CH₂)ₙ-C₃₋₈ cicloalquilo, -(CH₂)ₙ-(4 a 10 miembros)heterocicloalquilo, -(CH₂)ₙ-C₆₋₁₀ arilo y -(CH₂)ₙ-(5 a 10 miembros)heteroarilo, y en donde sea químicamente permisible, el C₃₋₈-cicloalquilo, (4 a 10 miembros)heterocicloalquilo, C₆₋₁₀-arilo y (5 a 10 miembros)heteroarilo son opcionalmente sustituidos con uno a cinco R⁸; o R⁶ y R⁷ tomados juntos con el nitrógeno al que se fijan forman un (4 a 10 miembros)heterocicloalquilo, y en donde sea químicamente permisible, el (4 a 10 miembros)heterocicloalquilo es opcionalmente sustituido con uno a cinco R⁹; cuando están presentes, cada R⁸ se selecciona independientemente a partir del grupo que consiste de halógeno, oxo, ciano, hidroxi, -SF₅, nitro, C₁₋₆ alquilo opcionalmente sustituido, C₂₋₆ alquenilo opcionalmente sustituido, C₂₋₆ alquinilo opcionalmente sustituido, C₁₋₆ alquiltio opcionalmente sustituido, C₁₋₆ alcoxi opcionalmente sustituido, -N(R⁴)(R⁵), -N(R⁴)(C=(O)R⁵), -C(=O)N(R⁴)(R⁵), -C(=O)-O-N(R⁴)(R⁵), -C(=O)-R⁴ y -C(=O)-OR⁴; cuando están presentes, cada R⁹ se selecciona independientemente a partir del grupo que consiste de halógeno, oxo, ciano, hidroxi, -SF₅, nitro, C₁₋₆ alquilo opcionalmente sustituido, C₂₋₆ alquenilo opcionalmente sustituido, C₂₋₆ alquinilo opcionalmente sustituido, C₁₋₆ alquiltio opcionalmente sustituido, C₁₋₆ alcoxi opcionalmente sustituido, -N(R⁴)(R⁵), -N(R⁴)(C=(O)R⁵), -C(=O)N(R⁴)(R⁵), -C(=O)-O-N(R⁴)(R⁵), -C(=O)-R⁴ y -C(=O)-OR⁴; b esta representado por un entero seleccionado a partir de 0, 1, 2 ó 3; m está representado por un entero seleccionado a partir de 0, 1 ó 2; y n está representado por un entero seleccionado a partir de 0, 1, 2, 3 ó 4.Pharmaceutical compositions comprising the compounds, treatment of diseases measured by PDE4 using these compounds. Claim 1: A compound of formula (1), or a pharmaceutically acceptable salt thereof, wherein: R¹ is selected from the group consisting of portions of - (CH₂) ₘ-C₃₋₈ cycloalkyl, - (CH₂) ₘ - (4 to 10 members) heterocycloalkyl, - (CH₂) ₘ-C₆₋₁₀ aryl and - (CH₂) ₘ- (5 to 14 members) heteroaryl and, where chemically permissible, C₃₋₈-cycloalkyl, (4 to 10 members) heterocycloalkyl, C₆₋₁₀-aryl and (5 to 14 members) heteroaryl are optionally substituted with one to five R²; when present, each R² is independently selected from the group consisting of halogen, oxo, cyano, hydroxy, -SF₅, nitro, C₁₋₆ optionally substituted alkyl, C₂₋₆ optionally substituted alkenyl, C₂₋₆ optionally substituted alkynyl, C₁₋₆ optionally substituted alkylthio, C₁₋₆ optionally substituted alkoxy, -N (R⁴) (R⁵), -N (R⁴) (C = (O) R⁵), -C (= O) N (R⁴) (R⁵) , -C (= O) -ON (R⁴) (R⁵), -C (= O) -R⁴, -C (= O) -OR⁴, and optionally substituted C₃₋₈ cycloalkyl; when present, each R³ is independently selected from the group consisting of halogen, cyano, hydroxy, -SF₅, nitro, C₁₋₆ optionally substituted alkyl, C₂₋₆ optionally substituted alkenyl, C₂₋₆ optionally substituted alkynyl, C₁₋ ₆ optionally substituted alkylthio, C₁₋₆ optionally substituted alkoxy, -N (R⁴) (R⁵), -N (R⁴) (C = (O) R⁵), -C (= O) N (R⁴) (R⁵), - C (= O) -ON (R⁴) (R⁵), -C (= O) -R⁴ and -C (= O) -OR⁴; R⁴ and R⁵ are each independently selected from the group consisting of hydrogen and optionally substituted C₁₋₆ alkyl; R⁶ and R⁷ are each independently selected from the group consisting of hydrogen, C₁₋₆ optionally substituted alkyl, - (CH₂) ₙ-C₃₋₈ cycloalkyl, - (CH₂) ₙ- (4 to 10 members) heterocycloalkyl, - (CH₂) ₙ-C₆₋₁₀ aryl and - (CH₂) ₙ- (5 to 10 members) heteroaryl, and where chemically permissible, C₃₋₈-cycloalkyl, (4 to 10 members) heterocycloalkyl, C₆₋₁₀- aryl and (5 to 10 members) heteroaryl are optionally substituted with one to five R⁸; or R⁶ and R⁷ taken together with the nitrogen to which they are attached form a (4 to 10 members) heterocycloalkyl, and where chemically permissible, the (4 to 10 members) heterocycloalkyl is optionally substituted with one to five R⁹; when present, each R⁸ is independently selected from the group consisting of halogen, oxo, cyano, hydroxy, -SF₅, nitro, C₁₋₆ optionally substituted alkyl, C₂₋₆ optionally substituted alkenyl, C₂₋₆ optionally substituted alkynyl, C₁₋₆ optionally substituted alkylthio, C₁₋₆ optionally substituted alkoxy, -N (R⁴) (R⁵), -N (R⁴) (C = (O) R⁵), -C (= O) N (R⁴) (R⁵) , -C (= O) -ON (R⁴) (R⁵), -C (= O) -R⁴ and -C (= O) -OR⁴; when present, each R⁹ is independently selected from the group consisting of halogen, oxo, cyano, hydroxy, -SF₅, nitro, C₁₋₆ optionally substituted alkyl, C₂₋₆ optionally substituted alkenyl, C₂₋₆ optionally substituted alkynyl, C₁₋₆ optionally substituted alkylthio, C₁₋₆ optionally substituted alkoxy, -N (R⁴) (R⁵), -N (R⁴) (C = (O) R⁵), -C (= O) N (R⁴) (R⁵) , -C (= O) -ON (R⁴) (R⁵), -C (= O) -R⁴ and -C (= O) -OR⁴; b is represented by an integer selected from 0, 1, 2 or 3; m is represented by an integer selected from 0, 1 or 2; and n is represented by an integer selected from 0, 1, 2, 3 or 4.

ARP150102349A 2014-08-06 2015-07-24 IMIDAZOPIRIDAZINE COMPOUNDS AS PDE4 INHIBITORS AR101297A1 (en)

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US201462033684P 2014-08-06 2014-08-06

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AR101297A1 true AR101297A1 (en) 2016-12-07

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