DERIVATIVES OF 2-PYRIDIN-2-YL-PYRAZOL-3(2H)-ONE, PREPARATION AND THERAPEUTIC USE THEREOF

摘要

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 —CH2, —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, —CH2-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) —SO2—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, —CH2-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 —CH2-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.

主权项

1. A compound of formula (I): wherein: 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 —CH2, —CH(R′)—, —N(R′)—, an oxygen atom or a sulfur atom, provided that when X is a sulfur atom, m+n do not equal 2; it being understood that R′ represents —(C1-C5)alkyl, —(C1-C5)alkoxy, —CH2-aryl, —C(O)R5 or —COOR5 with R5 as defined below; R1 represents oxo, —COOR5, —W—OH or —W—NR5R6, with W, R5 and R6 as defined below; R2 represents hydrogen or a group chosen from (i) groups —(C1-C5)alkyl, (ii) groups —(C1-C5)alkoxy, (iii) groups —COOR5, (iv) groups —NR5R6, (v) groups —C(O)—NR5R6, (vi) groups —SO2—NR3R4, (vii) heteroaryl groups optionally substituted with a group —(C1-C5)alkyl, (viii) groups —W-aryl, (ix) groups —W-heteroaryl, (x) groups —O—W-aryl, (xi) groups —O—W-heteroaryl and (xii) groups —O—W—NR5R6, with W, R3, R4, R5 and R6 as defined below; R3 and R4, (i) which may be identical or different, represent, independently of each other, hydrogen, —(C1-C5)alkyl, —(C3-C6)cycloalkyl, aryl, heteroaryl, —CH2-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 —(C1-C5)alkyl and —CH2-aryl; W is —(C1-C5)alkylene, optionally substituted with one or more hydroxyl groups; and R5 and R6, which may be identical or different, represent, independently of each other, hydrogen, —(C1-C5)alkyl or —(C3-C6)cycloalkyl; in the form of the base or of an acid-addition salt.