发明名称 Quinazoline carboxamide azetidines
摘要 The invention provides novel quinazoline carboxamide azetidine compounds according to Formula (I) and use for the treatment of hyperproliferative diseases, such as cancer.
申请公布号 US8946247(B2) 申请公布日期 2015.02.03
申请号 US201113989199 申请日期 2011.11.11
申请人 Merck Patent GmbH 发明人 Huck Bayard R.;Jones Reinaldo;Xiao Yufang;Neagu Constantin;Bankston Donald;Goutopoulos Andreas
分类号 A61K31/517;C07D239/72 主分类号 A61K31/517
代理机构 Millen, White, Zelano & Branigan, P.C. 代理人 Millen, White, Zelano & Branigan, P.C.
主权项 1. A compound of Formula (II′)and/or its stereoisomers or tautomers, or pharmaceutically acceptable salts of each of the foregoing, including mixtures thereof in all ratios, wherein: R1, R2 are H, R3′, R3″ independently are H, LA or Hal, R4, R5, R6, R7, R8, independently are H, Hal, LA, OH, SH, O(LA), NH2, NH(LA), N(LA)2, NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), NHCONH(LA), NHCONH2, NHSO2(LA), CO(LA), SO2NH2, SO2(LA) or SO2Hal, or R5, R6 together with the phenyl group they are attached to, may form a 9 or 10 membered bicyclic ring system, in which 1 or 2 of the non-phenyl carbon atoms may be independently replaced by NH, O or S, in which the cycle formed by R5 and R6 may be unsubstituted or mono- or disubstituted by Hal or LA, or one of R5, R6, R7 may be Ar1, O(Ar1), NH(Ar1), CONH(Ar1), NHCO(Ar1), NHCONH(Ar1), NHSO2(Ar1), CO(Ar1) or SO2(Ar1),while the other two of R5, R6, R7 are not Ar1, O(Ar1), NH(Ar1), CONH(Ar1), NHCO(Ar1), NHCONH(Ar1), NHSO2(Ar1), CO(Ar1) or SO2(Ar1), Ar1 is a monocyclic aromatic homo- or heterocycle having 0, 1, 2 or 3 N, O and/or S atoms and 5 or 6 skeleton atoms, which may be unsubstituted or, independently of one another, mono-, di- or trisubstituted by Hal, LA, OH, SH, O(LA), NH2, NH(LA), N(LA), NO2, CN, OCN, SCN, COOH, COO(LA), CONH2, CONH(LA), CON(LA)2, NHCO(LA), CHO, CO(LA), SO2NH2, SO2(LA) and/or SO2Hal, LA is unbranched or branched, linear alkyl having 1, 2, 3 or 4 C atoms, wherein 1, 2 or 3 H atoms may be replaced by Hal, Hal is F, Cl or Br.
地址 Darmstadt DE