Stat3/5 activation inhibitor

Abstract

The present invention provides a STAT3/5 activation inhibitor containing an aromatic compound represented by the general formula or a salt thereof as an active ingredient: Wherein X 1 represents a nitrogen atom or a group —CH═, R 1 represents a group —Z—R 6 , in which Z represents a group —CO—, a group —CH(OH)— or the like, R 6 represents a 5- to 15-membered monocyclic, dicyclic or tricyclic saturated or unsaturated heterocyclic group having 1 to 4 nitrogen atoms, oxygen atoms or sulfur atoms, R 2 represents a hydrogen atom or a halogen atom, Y represents a group —O—, a group —CO—, a group —CH(OH)— or a lower alkylene group, and A represents a group

1 - 57 . (canceled) 
     
     
         58 . A method for preventing or treating a symptom or disease associated with activation of STAT5 comprising administering, to a patient in need thereof, an effective amount of aromatic compound or a salt thereof as an active ingredient, wherein the compound is a compound selected from the group consisting of:
 (1) N-[6-(4-{[2-(4-piperonylpiperazin-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridin-3-yl]-3,4-dichlorobenzamide,   (2) N-{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}-N-{4-[(5-{methyl[4-(trifluoromethyl)benzyl]amino}pyridin-2-yl)oxy]phenyl}acetamide   (3) N-(6-{4-[3-(4-piperonylpiperazin-1-yl)-3-oxopropyl]phenoxy}pyridin-3-yl)-4-trifluoromethylbenzamide,   (4) N-[4-(4-{[2-(4-piperonylpiperazin-1-yl)-2-oxoethyl]methylamino}phenoxy)phenyl]-4-trifluoromethylbenzamide,   (5) N-[6-(4-{[2-(4-piperonylpiperazin-1-yl)-2-oxoethyl]ethylamino}-2-methoxyphenoxy)pyridin-3-yl]-4-trifluoromethylbenzamide,   (6) N-[6-(4-{[2-(4-piperonylpiperazin-1-yl)-2-oxoethyl]methylamino}-2-methylphenoxy)pyridin-3-yl]-4-trifluoromethylbenzamide, and   (7) N-[6-{[4-(4-pivaloylbenzyl)piperazin-1-yl]oxomethyl}phenoxy)pyridin-3-yl]-3,4-dichlorobenzamide,   or a salt thereof.   
     
     
         59 . A method for preventing or treating a symptom or disease associated with activation of STAT5 comprising administering, to a patient in need thereof, an effective amount of aromatic compound or a salt thereof as an active ingredient, wherein the compound is a compound selected from the group consisting of:
 N-(6-{[4-(4-{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}piperazin-1-yl)phenyl](methyl)amino}pyridin-3-yl)-4-(trifluoromethyl)benzamide,   N-{6-[(4-{3-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-3-oxopropyl}phenyl)(methyl)amino]pyridin-3-yl}-4-(trifluoromethyl)benzamide,   6-{4-[{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}(methyl)amino]-3-(trifluoromethyl)phenoxy}-N-[4-(trifluoromethyl)phenyl]pyridine-3-carboxamide,   N-[6-(4-{3-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-3-oxopropyl}phenoxy)pyridin-3-yl]-4-(trifluoromethyl)benzamide,   N-(4-{4-[{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}(methyl)amino]phenoxy}phenyl)-4-(trifluoromethyl)benzamide,   N-{6-[4-(4-{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}piperidin-1-yl)-2-methylphenoxy]pyridin-3-yl}-4-(trifluoromethyl)benzamide,   N-(6-{4-[{2-[4-(1,3-benzodioxol-5-ylmethyl)piperazin-1-yl]-2-oxoethyl}(methyl)amino]-2-methylphenoxy}pyridin-3-yl)-4-(trifluoromethyl)benzamide,   or a salt thereof.   
     
     
         60 . The method according to  claim 58 , wherein the symptom or disease associated with activation of STAT5 is autoimmune disease, allergy or hyperprolactinemia. 
     
     
         61 . The method according to  claim 59 , wherein the symptom or disease associated with activation of STAT5 is autoimmune disease, allergy or hyperprolactinemia.