发明名称 Guanidine compound
摘要 [Problem];The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases.;[Means for Solution];The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that the compound or a salt thereof of the present invention exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. In addition, the present invention relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound or a salt thereof of the present invention, and an excipient.
申请公布号 US9556160(B2) 申请公布日期 2017.01.31
申请号 US201514671397 申请日期 2015.03.27
申请人 Astellas Pharma Inc. 发明人 Yoshihara Kousei;Suzuki Daisuke;Yamaki Susumu;Yamada Hiroyoshi;Mihara Hisashi;Seki Norio
分类号 C07D413/04;C07D401/12;A61K31/5377;A61K31/4412;C07D413/12;C07D205/04;C07D211/60;C07D211/78;C07D213/38;C07D213/64;C07D213/74;C07D217/06;C07D217/22;C07D237/20;C07D239/26;C07D239/42;C07D241/20;C07D277/42;C07D277/46;C07D277/56;C07D295/06;C07D295/08;C07D295/18;C07D295/20;C07D309/08;C07D309/14;C07D401/04;C07D401/14;C07D403/04;C07D403/06;C07D403/12;C07D405/12;C07D405/14;C07D413/14;C07D239/48;C07D267/10;C07D239/34;C07D295/192 主分类号 C07D413/04
代理机构 Oblon, McClelland, Maier & Neustadt, L.L.P. 代理人 Oblon, McClelland, Maier & Neustadt, L.L.P.
主权项 1. A compound represented by the formula (I) or a salt thereof: wherein A is Q1 is CRQ12 or N, Q2 is CRQ22 or N, Q4 is CRQ42 or N, Q5 is CRQ52 or N, RQ12, RQ22, RQ42 and RQ52 are the same as or different from each other, and are H, lower alkyl, O-(lower alkyl), or N(lower alkyl)2, R1, R2, R3 and R4 are the same as or different from each other, and are H, halogen, or lower alkyl, E is a single bond, or lower alkylene which may be substituted with oxo (═O), G is a single bond, O, NH, or N(lower alkyl), J is a single bond or lower alkylene, L is O or NH, N(lower alkyl), U is a single bond, O, NH, N(lower alkyl which may be substituted with O-(lower alkyl)), SO2, or lower alkylene which may be substituted with oxo (═O), V is a single bond, O, NH, N(lower alkyl), or lower alkylene which may be substituted with OH, O-(lower alkyl), or oxo (═O), W is a single bond, SO, SO2, or lower alkylene, X is H, OH, NH2, lower alkyl which may be substituted with halogen, O-(lower alkyl which may be substituted with OH), NH(lower alkyl which may be substituted with oxo (═O)), N(lower alkyl which may be substituted with O-(lower alkyl) or oxo (═O))2, NH—SO2-(lower alkyl), N(lower alkyl)-SO2-(lower alkyl), cycloalkyl which may be substituted with group(s) selected from Group GXA1 below, O-(cycloalkyl), cycloalkenyl which may be substituted with group(s) selected from Group GXA1 below, aryl which may be substituted with group(s) selected from Group GXA1 below, O-(aryl which may be substituted with O-(lower alkyl)), or a hetero ring group which may be substituted with group(s) selected from Group GXA1 below, and GXA1 is i) halogen,ii) OH,iii) lower alkyl which may be substituted with group(s) selected from the group consisting of halogen; OH; O-(lower alkyl which may be substituted with OH, aryl, O-(lower alkyl), or oxo (═O)); NH2; NH(lower alkyl which may be substituted with OH); N(lower alkyl)2; NH(cycloalkyl); NH(hetero ring group); cycloalkyl which may be substituted with OH; aryl which may be substituted with O-(lower alkyl), COOH, or COO-(lower alkyl which may be substituted with aryl); hetero ring group(s) which may be substituted with O-(lower alkyl), oxo (═O), NH(lower alkyl which may be substituted with oxo (═O)), or lower alkyl; and oxo (═O),iv) O-(lower alkyl which may be substituted with OH, O-(lower alkyl), aryl, hetero ring group(s) (in which the hetero ring group may be substituted with lower alkyl which may be substituted with cycloalkyl or oxo (═O)), or oxo (═O)),v) NH-(lower alkyl which may be substituted with O-(lower alkyl) or oxo (═O)),vi) N(lower alkyl which may be substituted with oxo (═O))2,vii) NH-(aryl which may be substituted with COOH or COO-(lower alkyl)),viii) cycloalkyl which may be substituted with group(s) selected from the group consisting of lower alkyl which may be substituted with OH; COOH; and COO-(lower alkyl),ix) aryl which may be substituted with group(s) selected from the group consisting of halogen; lower alkyl (in which the lower alkyl may be substituted with COOH or COO-(lower alkyl)); O-(lower alkyl); COOH; and COO-(lower alkyl),x) hetero ring group(s) which may be substituted with group(s) selected from the group consisting of OH; halogen; lower alkyl which may be substituted with OH, O-(lower alkyl), or oxo (═O); O-(lower alkyl which may be substituted with O-(lower alkyl)); and oxo (═O),xi) O-(hetero ring group),xii) SO2-(lower alkyl which may be substituted with O-(lower alkyl)),xiii) SO2-(cycloalkyl),xiv) SO2-(aryl),xv) NHSO2-(lower alkyl), orxvi) oxo (═O).
地址 Tokyo JP