DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF
申请人:ALTENBURGER Jean-Michel
公开号:US20110301148A1
公开(公告)日:2011-12-08
The invention relates to compounds corresponding to formula (I), in the form of the base or of an acid-addition salt:
in which n is equal to 0, 1, 2, 3 or 4; m is equal to 0, 1 or 2; o is equal to 0 or 1; X represents a group —CH
2
, —CH(R′)—, —NH(R′)— or a heteroatom chosen from O and S, it being understood that R′ represents a group —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH
2
-aryl, —C(O)R5 or —COOR5; R1 represents an oxo group, —COOR5, —W—OH or —W—NR5R6; R2 represents an H atom or a group chosen from the groups (i) —(C1-C5)alkyl, (ii) —(C1-C5)alkoxy, (iii) —COOR5, (iv) —NR5R6, (v) —C(O)—NR5R6, (vi) —SO
2
—NR3R4, (vii) heteroaryl optionally substituted with a group —(C1-C5)alkyl, (viii) —W-aryl, (ix) —W-heteroaryl, (x) —O—W-aryl, (xi) —O—W-heteroaryl and (xii) —O—W—NR5R6; it being understood that R3 and R4, (i) which may be identical or different, represent, independently of each other, an H atom, a group —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH
2
-heteroaryl, —(C1-C5)alkyl-NR5R6, —W—OH or —W—NR5R6; or (ii) form, together with the nitrogen atom that bears them, a heterocycloalkyl group optionally substituted with one or more groups chosen from the groups —(C1-C5)alkyl and —CH
2
-aryl; W is a group —(C1-C5)alkylene, optionally substituted with one or more hydroxyl groups; R5 and R6, which may be identical or different, represent, independently of each other, a hydrogen atom or a group chosen from the groups —(C1-C5)alkyl and the groups —(C3-C6)cycloalkyl, and also the process for preparing them and the therapeutic uses thereof.
该发明涉及与化学式(I)对应的化合物,以其碱形式或酸盐形式存在:
其中n等于0、1、2、3或4;m等于0、1或2;o等于0或1;X代表一个基团—CH2、—CH(R′)—、—NH(R′)—或从O和S中选择的杂原子,其中R′代表一个基团—(C1-C5)烷基、—(C1-C5)烷氧基、—CH2-芳基、—C(O)R5或—COOR5;R1代表一个氧代基、—COOR5、—W—OH或—W—NR5R6;R2代表一个氢原子或从以下基团中选择的一个:(i) —(C1-C5)烷基、(ii) —(C1-C5)烷氧基、(iii) —COOR5、(iv) —NR5R6、(v) —C(O)—NR5R6、(vi) —SO2—NR3R4、(vii) 可选地被基团—(C1-C5)烷基取代的杂芳基、(viii) —W-芳基、(ix) —W-杂芳基、(x) —O—W-芳基、(xi) —O—W-杂芳基和(xii) —O—W—NR5R6;其中R3和R4,(i) 可能相同也可能不同,独立地代表一个氢原子、一个基团—(C1-C5)烷基、—(C3-C6)环烷基、芳基、杂芳基、—CH2-杂芳基、—(C1-C5)烷基-NR5R6、—W—OH或—W—NR5R6;或(ii) 与携带它们的氮原子一起形成一个杂环烷基基团,可选地取代一个或多个从以下基团中选择的基团:—(C1-C5)烷基和—CH2-芳基;W代表一个基团—(C1-C5)烷基,可选地取代一个或多个羟基;R5和R6,可能相同也可能不同,独立地代表一个氢原子或从以下基团中选择的一个:—(C1-C5)烷基和—(C3-C6)环烷基,以及其制备方法和治疗用途。