发明名称 Sulfonamide derivatives
摘要 The present invention relates to compounds of the formula; and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.
申请公布号 US8907101(B2) 申请公布日期 2014.12.09
申请号 US201313968561 申请日期 2013.08.16
申请人 Pfizer Limited;Icagen, Inc. 发明人 Beaudoin Serge;Laufersweiler Michael Christopher;Markworth Christopher John;Marron Brian Edward;Millan David Simon;Rawson David James;Reister Steven Michael;Sasaki Kosuke;Storer Robert Ian;Stupple Paul Anthony;Swain Nigel Alan;West Christopher William;Zhou Shulan
分类号 A61K31/44;C07D211/72;C07D401/00;C07F9/6539;A61K31/675;A61K31/454;C07D285/08;A61K31/433;C07D263/50;A61K45/06;A61K31/4439;C07D413/12;C07D417/14;A61K31/501;A61K31/427;C07D275/03;A61K31/506;A61K31/4545;C07D401/12;C07D417/12;A61K31/496 主分类号 A61K31/44
代理机构 代理人 Dixon J. Michael
主权项 1. A compound of the formula (I): whereinZ is selected from the group consisting of 2-thiazolyl, 4-thiazolyl, 1-thia-3,4-diazolyl, and 1-thia-2,4-diazolyl, in which each may be optionally substituted on a ring carbon atom with one or more substituents selected from the group consisting of halo, cyano, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C4)alkyl, (C1-C4)alkyl-S—, amino, (C1-C4)alkylamino, di(C1-C4)alkylamino, amino(C1-C4)alkyl, (C1-C4)alkylamino(C1-C4)alkyl, and di[(C1-C4)alkyl]amino(C1-C4)alkyl; Y1, Y2, Y3 and Y4 are each independently CH or CR1;each R1 is independently selected from the group consisting of halo, cyano, amino, hydroxy, (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, (C1-C4)alkoxy(C1-C4)alkyl, —C(O)H, —C(O)(C1-C4)alkyl, and —C(O)N(R2)2;each R2 is independently hydrogen, (C1-C4)alkyl, halo(C1-C4)alkyl, hydroxy(C1-C4)alkyl, or (C3-C6)cycloalkyl; or, where a nitrogen is substituted with two R2 groups, each independently selected from (C1-C4)alkyl, halo(C1-C4)alkyl, or hydroxy(C1-C4)alkyl, they may be taken together with the N atom to which they are attached to form a 4- to 6-membered ring which, when so formed, may therefore optionally be substituted with hydrogen, alkyl, halo, hydroxy, hydroxyalkyl or haloalkyl;B is phenyl which may be optionally substituted with one or more substituents selected from the group consisting of halo, cyano, hydroxy, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, cyano(C1-C4)alkyl, amino, (C1-C4)alkylamino, di(C1-C4)alkylamino, amino(C1-C4)alkyl, (C1-C4)alkylamino(C1-C4)alkyl, di[(C1-C4)alkyl]amino(C1-C4)alkyl, trifluoromethylthio, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkyl, —C(O)R2, —C(O)OR2, —OC(O)R2, —C(O)—N(R2)2, —CH2—C(O)R2, —CH2—C(O)OR2, —CH2—OC(O)R2, —CH2—C(O)—N(R2)2, S(O)2R2, S(O)2N(R2)2, (C3-C8)cycloalkyl, and (C3-C8)cycloalkyl(C1-C4)alkyl;X is absent; C is selected from the group consisting of pyrazolyl; pyridinyl; pyridazinyl; and, pyrimidinyl, in which each may be optionally substituted on a ring carbon atom with one or more substituents selected from the group consisting of halo, cyano, hydroxy, (C1-C4)alkyl, halo(C1-C4)alkyl, (C1-C4)alkoxy, halo(C1-C4)alkoxy, N(R2)2, (R2)2N(C1-C4)alkyl, trifluoromethylthio, hydroxy(C1-C4)alkyl, (C1-C4)alkoxy(C1-C4)alkyl, —C(O)R2, —C(O)OR2, —OC(O)R2, —C(O)—N(R2)2, —CH2—C(O)R2, —CH2—C(O)OR2, —CH2—OC(O)R2, —CH2—C(O)—N(R2)2, S(O)2R2, S(O)2N(R2)2, (C3-C8)cycloalkyl(C1-C4)alkyl, (C3-C8)cycloalkoxy, (C3-C8)cycloalkylamino, (C3-C8)cycloalkylamino(C1-C4)alkyl, (C3-C8)cycloalkyl(C1-C4)alkylamino, (C3-C8)cycloalkyl(C1-C4)alkylamino(C1-C4)alkyl, (C3-C8)cycloalkyl(C1-C4)alkoxy;or a tautomer thereof, or a pharmaceutically acceptable salt or solvate of the compound of formula (I), or its tautomer.
地址 Sandwich GB