EP1382603A1 — NITROGENOUS FUSED−RING COMPOUND HAVING PYRAZOLYL GROUP AS SUBSTITUENT AND MEDICINAL COMPOSITION THEREOF

USPTO Abstract

The present invention provides a compound having an excellent inhibitory action on activation of STAT6 and a pharmaceutical composition thereof. Inparticular, it provides a compound represented by the following formula (I), a salt thereof or a hydrate of them. In the formula, X represents a nitrogen-containing condensed aromatic heterocyclic group such as imidazo[1,2-a]pyridine, benzimidazole, quinazoline, quinoline, or 2,1-benzisoxazole and has (R 4 ) n as substituent groups; Y represents a C 3-8 cycloalkyl group, C 4-8 cycloalkenyl group, 5- to 14-membered non-aromatic heterocyclic group, C 6-14 aromatic hydrocarbon cyclic group or 5- to 14-membered aromatic heterocyclic group; n in (R 4 ) n is 0, 1, 2 or 3, and Z groups independently represent (1) hydrogen atom, (2) amino group, (3) halogen atom, (4) hydroxyl group, (5) nitro group, (6) cyano group, (7) azido group, (8) formyl group, (9) hydroxyamino group, (10) sulfamoyl group, (11) guanodino group, (12) oxo group, (13) C 2-6 alkenyl group, (14) C 1-6 alkoxy group, (15) C 1-6 alkylhydroxyamino group, (16) halogenated C 1-6 alkyl group, (17) halogenated C 2-6 alkenyl group, (18) (i) C 3-7 cycloalkyl group, (ii) C 3-7 cycloalkenyl group, (iii) 5- to 14-membered non-aromatic heterocyclic group, each of which may have one or more substituent groups Q, or (19) formula -M 1 -M 2 -M 3 , R 1 represents (1) hydrogen atom, (2) halogen atom, (3) hydroxyl group, (4) nitro group, (5) cyano group, (6) halogenated C 1-6 alkyl group, (7) C 2-6 alkyl group substituted with a hydroxyl or cyano group, (8) C 2-6 alkenyl group, or (9) formula -L 1 -L 2 -L 3 , and R 2 represents a hydrogen atom or a protecting group; and R 3 represents a hydrogen atom, halogen atom, cyano group, amino group, C 1-4 alkyl group or halogenated C 1-4 alkyl group.