发明名称 COMPOUNDS AND METHODS FOR THE TREATMENT OF CYSTIC FIBROSIS
摘要 The invention relates to a compound of Formula I and methods of treating cystic fibrosis comprising the step of administering a therapeutically effective amount of a compound of Formula I or IA to a patient in need thereof:;
申请公布号 US2014371238(A1) 申请公布日期 2014.12.18
申请号 US201414210238 申请日期 2014.03.13
申请人 FLATLEY DISCOVERY LAB 发明人 Zawistoski Michael P.;Barsukov Yevgen;Cole Bridget M.;Nugent Richard A.
分类号 C07D211/96;A61K31/437;A61K45/06;C07D401/12;A61K31/4545;A61K31/497;C07D413/12;A61K31/454;A61K31/506;C07D405/14;C07D401/14;C07D417/12;C07D471/04;A61K31/4468 主分类号 C07D211/96
代理机构 代理人
主权项 1. A compound of Formula I or an ester or prodrug thereof: wherein n is 0, 1, 2, 3, 4, 5, 6 or 7; each X is independently selected from —CR100, —N—, —COR100, —CN(R100)(R101), —CSR100—C—C(O)NR100, and —CN(R100)C(O)R101; A1 is absent, —[C(R100)(R101)]— —C(O)—, —C(S)—, —S(O)—, —C(O)N(R100)— or —S(O)2—, —S(O)2N(R100)(R101), —N[C(R100)(R101)]m—, —N(R100)C(O)—, —N(R100)C(S)—, —N(R100)S(O)—, —N(R101)C(O)N(R100)— or —N(R100)S(O)2—, —N(R100)S(O)2N(R100)(R101); wherein m is 0, 1, 2, 3, 4, 5, 6 or 7;wherein each R100 and R101 is hydrogen, deuterium, halogen, alkyl, cycloalkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aliphatic, substituted aliphatic, aryl and substituted aryl, heterocycle, substituted heterocycle, heteroaryl or substituted heteroaryl; alternatively two of R100 and R101 groups together with the atoms to which they are attached and any intervening atoms may form an additional optionally substituted, 3, 4, 5, 6 or 7 membered ring; A2 is absent, —[C(R100)(R101)]m— —C(O)—, —C(S)—, —S(O)—, —C(O)N(R100)— or —S(O)2—, —S(O)2N(R100)(R101); each R1 is independently selected from hydrogen, deuterium, halogen, alkyl, cycloalkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl —OR100, —SR100, —S(O)—, S(O)2—, —S(O)2N(R100)(R101), —NR100R101, —C(O)R100, —C(O)OR100, —C(O)NR100R101, —N(R100)C(O)R101, —CF3, —CN, —NO2, —N3, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, alkylthio or substituted alkylthio; alternatively two of R1 groups together with the atoms to which they are attached and any intervening atoms may form an additional optionally substituted 3, 4, 5, 6 or 7 membered ring; Cy1 is absent, alkyl, cycloalkyl, substituted cycloalkyl, aryl, substituted aryl, heteroaryl or substituted heteroaryl; wherein when Cy1 is phenyl and A1 is absent or C1-C4 alkyl, the phenyl group is substituted with a group selected from halogen, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aryl, substituted aryl, heterocyclyl, substituted heterocyclyl, heteroaryl, or substituted heteroaryl —OR100, —SR100, —S(O)—, S(O)2—, —S(O)2N(R100)(R101) —NR100R101, —C(O)R100, —C(O)OR100, —C(O)NR100R101, —N(R100)C(O)R101, —CF3, —CN, —NO2, —N3, acyl, alkoxy, substituted alkoxy, alkylamino, substituted alkylamino, dialkylamino, substituted dialkylamino, alkylthio or substituted alkylthio;wherein when Cy1 is cyclobutyl, cyclopentyl or furan, Cy2 is substituted with a group other than —OCF3, —CF3, —OCH3, —Cl or —F; and, Cy2 is alkyl, cycloalkyl, substituted cycloalkyl aryl, substituted aryl, heteroaryl or substituted heteroaryl.
地址 Charlestown MA US