abstract |
REFERS TO AN AMINE SUBSTITUTED FOR FORMULA X WHERE R1 IS C1-C6 ALKYL, -CH2-S (O) 0-2- (C1-C6 ALKYL), -CH2-CH2-S (O) 0-2- (ALKYL C1-C6), C2-C6 ALKENYL, C2-C6 ALKYNYL, AMONG OTHERS; R2 IS H, C1-C6 ALKYL, C2-C6 ALKENYL, C2-C6 ALKINYL, - (CH2) 0-4-R2-1 WHERE R2-1 IS R1-ARYL OR R1-HETEROARYL, R1-HETEROARYL IS PYRIDINYL, PYRIMIDINYL , QUINOLINYL, BENZOTHENYL, AMONG OTHERS; R1-ARYL IS PHENYL, 1-NAPHTHYL, 2-NAPHTHYL, INDANYL, AMONG OTHERS; Rc IS C1-C10 ALKYL, - (CH2) -0-3- (C3-C8 CYCLOALKYL), AMONG OTHERS; RN IS RN-1-XN- WHERE XN IS CO, SO2; RN-1 IS -RN-ARYL, -RN-HETEROARYL, AMONG OTHERS; R3 IS H, C1-C6 ALKYL, AMONG OTHERS. PREFERRED COMPOUNDS ARE N1 - {(1S-2R) -1- (3,5-DIFLUOROBENZYL) -2-HYDROXY-3 - [(3-METOXYBENZYL) AMINO] PROPYL} -5-METHYL-N3, N3-DIPROPYLISOPHTHALAMIDE, N1 - {(1S-2R) -1- (3,5-DIFLUOROBENZYL) -3 - [(2-FURYLMETHYL) -AMINE] -2-HYDROXYPROPYL} -5-METHYL-N3, N3-DIPROPYLISOPHTHALAMIDE, AMONG OTHERS. COMPOUNDS DERIVED FROM AMINE ARE INHIBITORS OF ß-SECRETASE REDUCING THE DEPOSITS OR PLATES OF ß- AMYLOID USEFUL FOR THE TREATMENT OR PREVENTION OF ALZHEIMER'S DISEASE |