Patent ID: 6642228
Filing Date: 2003-11-04
Classification: A61K,A61P,C07D

Abstract:
A method of treating diseases selected from the group consisting of ocular tension, carcinoma, sarcoma and tumentia comprising administering to a patient a therapeutically effective amount of an &agr;1B adrenoceptor antagonist compound represented by the formula (I) or a pharmacologically acceptable acid addition salt thereof: (wherein Ar is indolyl, naphthalenyl, quinolinyl, benzimidazolyl, benzofuranyl, benzothiophenyl, benzisoxazolyl, or 2-ketobenzimidazolinyl, each of which is unsubstituted or substituted with the groups selected from the group consisting of halogen, nitro group, acylamino group having 1 to 9 carbon atoms, amino group, alkylamino group having 1 to 8 carbon atoms, arylamino group having 6 to 15 carbon atoms, dialkylamino group having 2 to 16 carbon atoms, diarylamino group having 12 to 20 carbon atoms, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, alkoxy group having 1 to 8 carbon atoms, aryloxy group having 1 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, haloalkoxy group having 1 to 8 carbon atoms, cyano group, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, alkylthio group having 1 to 8 carbon atoms, and arylthio group having 6 to 15 carbon atoms;R1 is hydrogen, alkyl having 1 to 6 carbon atoms, aryl having 6 to 12 carbon atoms, alkenyl having 2 to 9 carbon atoms, or cycloalkyl having 3 to 8 carbon atoms; Bâ€”Nâ€”R1 forms a ring structure and is piperidine or 2,3,6-trihydropyridine, each of which is unsubstituted or substituted with the groups selected from the group consisting of halogen, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, hydroxyalkyl group having 1 to 8 carbon atoms, alkylcarbonyl group having 2 to 9 carbon atoms, arylcarbonyl group having 7 to 16 carbon atoms, and aralkyl group having 7 to 15 carbon atoms; n denotes an integer of 0 or 1; A is alkylene having 2 to 8 carbon atoms, phenylene, or cycloalkylene having 3 to 8 carbon atoms, each of which is unsubstituted or substituted with the groups selected from the group consisting of halogen, nitro group, acylamino group having 1 to 9 carbon atoms, amino group, alkylamino group having 1 to 8 carbon atoms, arylamino group having 6 to 15 carbon atoms, dialkylamino group having 2 to 16 carbon atoms, diarylamino group having 12 to 20 carbon atoms, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, alkoxy group having 1 to 8 carbon atoms, aryloxy group having 6 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, haloalkoxy group having 1 to 8 carbon atoms, cyano group, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, alkylthio group having 1 to 8 carbon atoms, and arylthio group having 6 to 15 carbon atoms; Q is: 2) â€”NR2R3, wherein each of R2 and R3 is independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 8 carbon atoms, alkenyl having 2 to 9 carbon atoms, aryl having 6 to 15 carbon atoms, or aralkyl having 7 to 15 carbon atoms (wherein the aryl moiety of the aryl and aralkyl may be substituted with the groups selected from the group consisting of halogen, nitro group, acylamino group having 1 to 9 carbon atoms, amino group, alkylamino group having 1 to 8 carbon atoms, arylamino group having 6 to 15 carbon atoms, dialkylamino group having 2 to 16 carbon atoms, diarylamino group having 12 to 20 carbons atoms, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, alkoxy group having 1 to 8 carbon atoms, aryloxy group having 6 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, haloalkoxy group having 1 to 8 carbon atoms, cyano group, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, alkylthio group having 1 to 8 carbon atoms, and arylthio group having 6 to 15 carbon atoms), or â€”NR2R3 together forms piperidine, pyrrolidine, 1,3,4-trihydroisoquinoline, isoindoline, piperazine, morpholine, 2-piperidone, 2-pyrrolidone, indoline, 2,3,4-trihydroquionoline, 2,3,4-trihydroquinoxaline, dihydrobenzoxazine, benzothiane, phthalamide, or guanidine, each of which is unsubstituted or substituted with the groups selected from the group consisting of halogen, nitro group, acylamino group having 1 to 9 carbon atoms, amino group, alkylamino group having 1 to 8 carbon atoms, arylamino group having 6 to 15 carbon atoms, dialkylamino group having 2 to 16 carbon atoms, diarylamino group having 12 to 20 carbon atoms, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, alkoxy group having 1 to 8 carbon atoms, aryloxy group having 6 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, haloalkoxy group having 1 to 8 carbon atoms, cyano group, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, alkylthio group having 1 to 8 carbon atoms, and arylthio group having 6 to 15 carbon atoms; or (wherein each of R4, R5, R6 is independently hydrogen, alkyl having 1 to 6 carbon atoms, cycloalkyl having 3 to 8 carbon atoms, alkenyl having 2 to 9 carbon atoms, aryl having 6 to 15 carbon atoms, or aralkyl having 7 to 15 carbon atoms (wherein the aryl moiety of the aryl and aralkyl may be substituted with the groups selected from the group consisting of halogen, nitro group, acylamino group having 1 to 9 carbon atoms, amino group, alkylamino group having 1 to 8 carbon atoms, arylamino group having 6 to 15 carbon atoms, dialkylamino group having 2 to 16 carbon atoms, diarylamino group having 12 to 20 carbon atoms, hydroxy, alkyl group having 1 to 8 carbon atoms, aryl group having 6 to 15 carbon atoms, alkoxy group having 1 to 8 carbon atoms, aryloxy group having 6 to 15 carbon atoms, haloalkyl group having 1 to 8 carbon atoms, haloalkoxy group having 1 to 8 carbon atoms, cyano group, aminosulfonyl group having 0 to 15 carbon atoms, carboxyl group, alkoxycarbonyl group having 2 to 9 carbon atoms, aminocarbonyl group having 1 to 15 carbon atoms, alkylthio group having 1 to 8 carbon atoms, and arylthio group having 6 to 15 carbon atoms; or R4 and R5 together form an imidazoline ring)).