H4 receptor inhibitors to treat tinnitus

摘要

A histamine type 4 (H4R) receptor inhibitor for use in the treatment of tinnitus, wherein said H4R inhibitor is selected from: - 1 - [(5-chloro-1H-indole-2-yl) carbonyl] -4-methylpiperazine, - 4 - ((3R) -3-5 aminopyrrolidin-1-yl) -6,7-dihydro-5H-benzo [6,7] cyclohepta [1,2-d] pyrimidin-2-ylamine , - cis-4- (piperazin-1-yl) -5,6,7a, 8,9,10,11,11a-octahydrobenzofuro [2,3-h] quinazolin-2-amine, - 7- (furan- 2-yl) -4- (piperazin-1-yl) quinazolin-2-amine, - 1- (7- (2-amino-6- (4-methylpiperazin-1-yl) pyrimidin-4-yl) -3 , 4-dihydroisoquinolin-2 (1H) -yl) -2-cyclopentyletanone, - 1 - [(5-chloro-1H-benzimidazol-2-yl) carbonyl] -4-methylpiperazine maleate, - N4- (cyclopropylmethyl) -6 - [(3R) -3- (methylamino) pyrrolidin-1-yl] pyrimidine-2,4-diamine, - N4- (cyclopropylmethyl) -6 - [(3R) -3- (methylamino) pyrrolidin-1-yl] pyrimidine-2,4-diamine tartrate, - (R) -4- (3-amino-pyrrolidin-1-yl) -6-isopropyl-pyrimidin-2-ylamine, - 2-isobutyl-6- (3- (methylamino) ) azetidin-1-yl) pyrimidin-4-amine, - 2-isobutyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) p irimidin-4-amine, - 2-cyclohexylmethyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, - 2- (4-fluorobenzyl) -6- (3- ( methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-cyclopropyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-tert-butyl-6- (3 - (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-isopropyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2- (cyclopropylmethyl) -6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 6- (3- (methylamino) azetidin-1-yl) -2- (phenoxymethyl) pyrimidin-4-amine, - 2-cyclopropyl- 6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, - 2-tert-butyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin -4-amine, - 2-isopropyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, - 6 - ((3R) -3- (methylamino) pyrrolidin-1 -il) -2- (phenoxymethyl) pyrimidin-4-amine, - 6- (3-aminoazetidin-1-yl) -2-isobutylpyrimidin-4-amine, - 2-isobutyl-6- (3-methyl-3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 6 - ((3R) -3-aminopyrrolidin-1-yl) -2-isobutylpyrimidin-4-amine, - 2-cyclobutyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-cyclobutyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, - 2- cyclopentyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-cyclopentyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine , - 2- (2,2-dimethylpropyl) -6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2- (2,2-dimethylpropyl) -6 - ((3R) - 3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, 2- (2-cyclopentylethyl) -6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine, - 2-Cyclohexylmethyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-cyclopropylmethyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4 -amine, - 2-cyclohexyl-6- (3- (methylamino) azetidin-1-yl) pyrimidin-4-amine, - 2-cyclohexyl-6 - ((3R) -3- (methylamino) pyrrolidin-1-yl ) pyrimidin-4-amine, and - 2- (4-fluorobenzyl) -6 - ((3R) -3- (methylamino) pyrrolidin-1-yl) pyrimidin-4-amine.