MD20160121A2 - Pirazolopiridine şi pirazolopirimidine - Google Patents

Pirazolopiridine şi pirazolopirimidine Download PDF

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MD20160121A2
MD20160121A2 MDA20160121A MD20160121A MD20160121A2 MD 20160121 A2 MD20160121 A2 MD 20160121A2 MD A20160121 A MDA20160121 A MD A20160121A MD 20160121 A MD20160121 A MD 20160121A MD 20160121 A2 MD20160121 A2 MD 20160121A2
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Moldova
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alkyl
cycloalkyl
phenyl
heteroaryl
halo
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MDA20160121A
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Russian (ru)
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Йотам Уодсворт КОЭ
Кристоф Мартин Денхардт
Питер Джоунс
Йогеш Анил Сабнис
Джозеф Вальтер СТРОБАХ
Флориан Мишель Уэйкенхат
Гэвин Алистер Уитлок
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Pfizer Inc.
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Application filed by Pfizer Inc. filed Critical Pfizer Inc.
Publication of MD20160121A2 publication Critical patent/MD20160121A2/ro

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Abstract

Invenţia se referă la un compus având structura (I):(I)sau la o sare farmaceutic acceptabilă a acestuia, sau un solvat farmaceutic acceptabil al compusului menţionat sau sare farmaceutic acceptabilă, unde A şi A′ sunt independent C sau N, unde C poate fi nesubstituit sau substituit prin halo sau C1-C6 alchil; R şi R0 sunt independent selectaţi din grupa care constă din H, C1-C6 alchil, hidroxi(C1-C6 alchil), fenil(C1-C6 alchil) şi -(CH2)n-W, unde W este C3-C8 cicloalchil, fenil, naftil, heteroaril sau heterociclu cu 5 sau 6 membri care conţine 1…3 atomi de N, S şi/sau O, -SO2-R′, -NHSO2-R′, -NR″SO2-R′ şi SR′, unde R′ şi R″ sunt independent C1-C6 alchil sau C3-C8 cicloalchil etc.; unde fiecare dintre alchilul, cicloalchilul, heterociclul, fenilul, naftilul sau heteroarilul menţionat poate fi nesubstituit sau substituit prin fenil, heteroaril etc.; sau R, R0 şi atomul N, de care ei sunt legaţi, formează împreună un inel heterociclic monociclic sau biciclic care poate fi nesubstituit sau substituit cu (a) halo, hidroxi, heteroaril, C1-C6 alchil, C1-C6 alcoxi etc., sau (b) -(CH2)n-W, unde W este C3-C8 cicloalchil, fenil etc.; R1 este H, halo sau ciano; R2 şi R2′ sunt independent H, C1-C6 alchil, ciano, C1-C6 alcoxi, C1-C6 alchiltio sau C3-C8 cicloalchil, unde alchil, alcoxi sau cicloalchil este opţional substituit cu unu sau mai mulţi atomi de fluor; X este o legătură, -CO-, -CONH-, -SO2-, -SONH- sau -(CH2)m-; R3 este H, C1-C4 alchil, fenil, naftil, heteroaril sau heterociclu cu 5 sau 6 membri care conţine 1…3 atomi de N, un heteroaril sau heterociclu cu 5 membri etc., sau (c) 2 atomi de O sau S şi 0…2 atomi de N; unde fiecare dintre fenilul, naftilul, heteroarilul sau heterociclul menţionat este opţional substituit cu alchil, un substituent -Y-R4 şi/sau 1…4 substituenţi, fiecare fiind selectat independent din R5; cu condiţia că atunci când X este -CO- sau -SO2-, R3 nu este H; Y este o legătură, -(CH2)m- sau -O-; R4 este (a) H, C1-C6 alchil, C3-C8 cicloalchil, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8 etc.; (b) fenil sau naftil, fenilul şi naftilul menţionaţi fiind substituiţi opţional cu 1…5 substituenţi selectaţi dintre C1-C6 alchil, C3-C8 cicloalchil, halo, ciano, -OR6, -NR7R8 etc.; sau (c) un heteroaril monociclic saturat sau parţial nesaturat cu 3…8 membri etc.; R6 este H, C1-C6 alchil sau C3-C8 cicloalchil etc.; R7 şi R8 sunt fiecare independent H, C1-C6 alchil sau C3-C8 cicloalchil sau sunt luaţi împreună cu atomul de azot la care ei sunt ataşaţi pentru a forma un inel heterociclic saturat cu 4, 5 sau 6 membri, ce conţine 1...2 atomi de azot sau un atom de azot şi unul de oxigen, unde alchilul C1-C6 menţionat este substituit opţional cu C3-C8 cicloalchil, halo etc.; inelul heterociclic menţionat fiind substituit opţional prin una sau mai multe grupe C1-C6 alchil sau C3-C8 cicloalchil; R9 este C1-C6 alchil sau C3-C8 cicloalchil; m şi n sunt independent 0, 1, 2 sau 3. Invenţia de asemenea se referă la sărurile şi solvaţii farmaceutic acceptabili ai acestor compuşi; la compoziţiile care conţin asemenea compuşi şi la utilizarea acestor compuşi în tratamentul diferitor boli, în special astmul şi COPD.
MDA20160121A 2014-05-14 2015-04-30 Pirazolopiridine şi pirazolopirimidine MD20160121A2 (ro)

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US201461993138P 2014-05-14 2014-05-14
PCT/IB2015/053174 WO2015173683A1 (en) 2014-05-14 2015-04-30 Pyrazolopyridines and pyrazolopyrimidines

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US (2) US9518052B2 (ro)
EP (1) EP3143021B1 (ro)
JP (1) JP6663857B2 (ro)
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