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吡唑并吡啶及吡唑并嘧啶
专利权人:
PFIZER INC.
发明人:
COE, JOTHAM WADSWORTH,柯 乔桑 瓦德斯瓦兹,柯 喬桑 瓦德斯瓦茲,DEHNHARDT, CHRISTOPH MARTIN,德哈特 克里斯多弗 马丁,德哈特 克里斯多弗 馬丁,JONES, PETER,琼斯 彼得,瓊斯 彼得,SABNIS, YOGESH ANIL,萨柏尼斯 优格区 安尼尔,薩柏尼斯 優格區 安尼爾,STROHBACH, JOSEPH WALTER,史托贝奇 乔,柯 乔桑 瓦德斯瓦兹,柯 喬桑 瓦德斯瓦茲,德哈特 克里斯多弗 马丁,德哈特 克里斯多弗 馬丁,琼斯 彼得,瓊斯 彼得,萨柏尼斯 优格区 安尼尔,薩柏尼斯 優格區 安尼爾,史托贝奇 乔
申请号:
TW104115312
公开号:
TWI591067B
申请日:
2015.05.13
申请国别(地区):
TW
年份:
2017
代理人:
摘要:
A compound having the structure: or a pharmaceutically acceptable salt thereof, or a pharmaceutically acceptable solvate of said compound or pharmaceutically acceptable salt, wherein A and A' are independently C or N, where C may be unsubstituted or substituted by halo or C1-C6 alkyl; R and R0 are independently selected from the group consisting of H, C1-C6 alkyl, hydroxy(C1-C6 alkyl), phenyl(C1-C6 alkyl), and -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N, S and/or O atoms, -SO2-R’, -NHSO2-R’, -NR”SO2-R’ and SR’, where R’ and R” are independently C1-C6 alkyl or C3-C8 cycloalkyl, etc.; wherein each of said alkyl, cycloalkyl, heterocyclic, phenyl, naphthyl or heteroaryl may be unsubstituted or substituted by phenyl, heteroaryl, etc.; or, R and R0 and the N atom to which they are bonded together form a monocyclic or bicyclic heterocyclic ring which may be unsubstituted or substituted by (a) halo, hydroxy, heteroaryl, C1-C6 alkyl, C1-C6 alkoxy, etc., or (b) -(CH2)n-W, where W is C3-C8 cycloalkyl, phenyl, etc.; R1 is H, halo or cyano; R2 and R2’ are independently H, C1-C6 alkyl, cyano, C1-C6 alkoxy, C1-C6 alkylthio, or C3-C8 cycloalkyl where alkyl, alkoxy, or cycloalkyl is optionally substituted by one or more fluorine atoms; X is a bond, -CO-, -CONH-, -SO2-, -SONH-, or -(CH2)m--; R3 is H, C1-C4 alkyl, phenyl, naphthyl, 5- or 6-membered heteroaryl or heterocyclic containing 1-3 N atoms, a 5-membered heteroaryl or heterocyclic, etc., or (c) 2 O or S atoms and 0-2 N atoms; wherein each of said phenyl, naphthyl, heteroaryl or heterocyclic is optionally substituted by alkyl, 1 substituent -Y-R4 and/or 1-4 substituents each independently selected from R5; with the proviso that when X is -CO- or -SO2-, R3 is not H; Y is a bond, -(CH2)m- or -O-; R4 is (a) H, C1-C6 alkyl, C3-C8 cycloalkyl, halo, oxo, -OR6, -NR7R8, -SR6, -SOR9, -SO2R9, -COR6, -OCOR6, -COOR6, -NR6COR6, -CONR7R8, etc.; (b) phenyl or naphthyl,
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