发明名称 ENZYME INHIBITORS
摘要 Compounds of formula (I), inhibit HDAC activity: wherein A, B and D independently represent═CH—or═N—; W is—CH═CH—Or—CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intra-cellular carboxylesterase enzymes to a carboxylic acid group; R2 and R3 are selected from the side chains of a natural or non-nat-ural alpha amino acid, provided that neither R2 nor R3 is hydrogen, or R2 and R3, taken together with the carbon to which they are attached, form a 3-6 membered saturated cycloalkyl or heterocyclyl ring; Y is a bond,—C(═O)—,—S(═O)2—,—C(═O)O—,—C(═O)NR′—,—C(═5)—NR′,—C(═NH)NR′or—S(═O)2NR—wherein R′is hydrogen or optionally substituted C1—C6 alkyl; L1 is a divalent radical of formula—(Alk1)m,(Q)n(Alk2)p—wherein m, n, p, Q, Alk1 and Alk2 are as defined in the claims; X1 represents a bond;—C(═O); or—S(═O)2—;—NR4C(═O)—,—C(═O)NR4—,—NR4C(═O)NR5—,—NR4S(═O)2—, or—S(═O)2NR4—wherein R4 and R5 are independently hydrogen or optionally substituted C1-C6 alkyl; and z is 0 or 1.
申请公布号 US2012149736(A1) 申请公布日期 2012.06.14
申请号 US201013202105 申请日期 2010.02.25
申请人 DONALD ALASTAIR DAVID GRAHAM;MOFFAT DAVID FESTUS CHARLES;BELFIELD ANDREW JAMES;NORTH CARL LESLIE;JONES STEWART ANDREW WAYNE;CHROMA THERAPEUTICS LTD. 发明人 DONALD ALASTAIR DAVID GRAHAM;MOFFAT DAVID FESTUS CHARLES;BELFIELD ANDREW JAMES;NORTH CARL LESLIE;JONES STEWART ANDREW WAYNE
分类号 A61K31/44;A61K31/196;A61K31/216;A61P1/00;A61P3/10;A61P7/00;A61P11/00;A61P11/06;A61P17/06;A61P19/02;A61P25/00;A61P29/00;A61P35/00;C07C259/06;C07D213/56 主分类号 A61K31/44
代理机构 代理人
主权项
地址