发明名称 Compositions and methods for inhibition of the JAK pathway
摘要 The invention encompasses compounds having formula I and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, are therapeutically useful.
申请公布号 US8962643(B2) 申请公布日期 2015.02.24
申请号 US200711678488 申请日期 2007.02.23
申请人 Rigel Pharmaceuticals, Inc. 发明人 Li Hui;Argade Ankush;Tso Kin;Thota Sambaiah;Carroll David;Sran Arvinder;Cooper Robin;Singh Rajinder;Bhamidipati Somasekhar;Taylor Vanessa;Masuda Esteban
分类号 C07D403/12;A61K31/505;C07D239/48;C07D401/12;C07D409/12;C07D417/12 主分类号 C07D403/12
代理机构 Klarquist Sparkman, LLP 代理人 Young Travis;Klarquist Sparkman, LLP
主权项 1. A compound of the formula I:or pharmaceutically acceptable salt thereof, wherein: ring A is phenyl; p is 0, 1, 2 or 3; q is 0, 1, 2 or 3; X is selected from the group consisting of hydrogen, alkyl, substituted alkyl, hydroxy, alkoxy, substituted alkoxy, amino, substituted amino, carboxyl, carboxyl ester, cyano, halo, nitro, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkynyl, substituted cycloalkynyl; Y is alk-SO2N(R4)R5 or alk-N(R4)SO2R5; alk is selected from the group consisting of straight or branched chain C1-6 alkylene group, cycloalkylene and substituted cycloalkylene; R1 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, cycloalkynyl, substituted cycloalkynyl, cycloalkyl and substituted cycloalkyl; each R2 independently is selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, alkynyl, substituted alkynyl, cycloalkynyl, substituted cycloalkynyl, alkynyloxy, amino, substituted amino, aryl, substituted aryl, aryloxy, substituted aryloxy, cyano, cycloalkyl, substituted cycloalkyl, cycloalkoxy, substituted cycloalkoxy, heteroaryl, substituted heteroaryl, heteroaryloxy, substituted heteroaryloxy, heterocyclic, substituted heterocyclic, heterocyclyloxy, substituted heterocyclyloxy, aminoacyl, aminoacyloxy, carboxyl, carboxyl ester, carbonate ester, nitro, and halo; Z1, Z2, and Z3 each independently is carbon or nitrogen, wherein no more than one of Z1, Z2, and Z3 is N; each R3 independently is selected from the group consisting of alkyl, substituted alkyl, alkoxy, substituted alkoxy, alkynyl, substituted alkynyl, cycloalkynyl, substituted cycloalkynyl, alkynyloxy, amino, substituted amino, aryl, substituted aryl, aryloxy, substituted aryloxy, cyano, cycloalkyl, substituted cycloalkyl, cycloalkoxy, substituted cycloalkoxy, heteroaryl, substituted heteroaryl, heteroaryloxy, substituted heteroaryloxy, heterocyclic, substituted heterocyclic, heterocyclyloxy, substituted heterocyclyloxy, aminoacyl, aminoacyloxy, carboxyl, carboxyl ester, carbonate ester, nitro, halo and aminosulfonyl; or R6 and one of R3, together with the intervening atoms bound thereto form a heterocyclic or a substituted heterocyclic fused to the ring containing Z1, Z2 and Z3; or R7 and one of R3, together with the intervening atoms bound thereto form a heterocyclic or a substituted heterocyclic fused to the ring containing Z1, Z2 and Z3; or R4 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl and M+, wherein M+ is a counterion selected from the group consisting of K+, Na+, Li+ and +N(R8)4, wherein R8 is hydrogen or alkyl, and the nitrogen of —SO2N(R4)R5 or —N(R4)SO2R5 is N−; R5 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, amine, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, and acyl; or R4 and R5 together with the intervening atom or atoms bound thereto form a heterocyclic or a substituted heterocyclic group; R6 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocyclic, carboxyl, carboxyl ester, aryl, substituted aryl, heteroaryl, substituted heteroaryl, acyl and M+, wherein M+ is a counterion selected from the group consisting of K+, Na+, Li+ or +N(R8)4, wherein R8 is hydrogen or alkyl, and the nitrogen of —SO2N(R6)R7 or —N(R6)SO2R7 is N−; or R6 and R7 together with the intervening atom or atoms bound thereto, form a heterocyclic or a substituted heterocyclic group; and R7 is selected from the group consisting of hydrogen, alkyl, substituted alkyl, amine, cycloalkyl, substituted cycloalkyl, heterocyclic, substituted heterocyclic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, carboxyl, carboxyl ester, and acyl.
地址 South San Francisco CA US