BENZOTIAZOLTSIKLOBUTILAMINA derivatives as ligands of histamine H3 receptors and pharmaceutical compositions thereof, process for the selective modulation effects of histamine H3 receptor and methods for treating conditions or disorders modulated by histamine H3 receptor

摘要

1. Derivatives of benzothiazole cyclobutylamine, covered by the General structural formula (I):! ! where m is 0 or 1; ! one of R1 and R2 is selected from the group consisting of hydrogen, acyl, acyloxy group, alkenyl, alkoxy, alkoxyalkoxy group, alkoxyalkyl, alkoxycarbonyl, alkoxyimino group, alkoxy sulfonyl, alkyl, alkylcarbonyl, alkylsulfonyl, cycloalkyl, amido -, haloalkoxy, haloalkyl, halogen, hydroxy group, hydroxyalkyl, mercapto, nitro, alkylthio group, -NRARB, (NRARB) carbonyl, -SO2N (R14a) (R14b), N (R14a) SO2 (R14b), a group of the formula - L2-R6 and a group of the formula-L3a-R6a-L3b-R6b; ! the other of R1 and R2 is selected from the group consisting of hydrogen, cyano, halogen, alkyl, cycloalkyl, fluoroalkyl, alkoxy, alkoxyalkyl, fluoroalkoxy, alkylthio, —SO2N (R14a) (R14b) and —N (R14a) SO2 (R14b); ! each of R3a and R3b is independently selected from the group consisting of hydrogen, cyano, halogen, alkyl, cycloalkyl, fluoroalkyl, alkoxy, alkoxyalkyl, fluoroalkoxy, alkylthio, —SO2N (R14a) (R14b) and —N (R14a) SO2 (R14b); ! each of R4 and R5 is independently selected from the group consisting of alkyl, fluoroalkyl, hydroxyalkyl, alkoxyalkyl and cycloalkyl, or R4 and R5 taken together with the nitrogen atom to which each is attached form a non-aromatic ring; ! R6 represents aryl, heterocycle or heterocycloalkyl; ! R6a represents an aryl or heterocycle; ! R6b represents an aryl or heterocycle; ! L is a bond or alkylene; ! L2 is a bond, -O-, alkylene, -C (= O) -, -S-, -SO2N (R14a) -, -N (R14a) SO2--, -C (O) N (R14a) -, -N (R14a) C (O) - and -N (R15) -; ! each of L3a and L3b is independently selected from the group consisting of, -O-, alkylene, -C (= O) -, -S-, -SO2N (R14a) -, -N (R14a) SO2--, -C (O) N (R14a) -, -N (R14a) C (O) - and -N