DOPAMINE D1 RECEPTOR AGONIST PRO-DRUG COMPOUNDS & DERIVATIVES

摘要

The invention provides a pro−drug compound of Formula (A): wherein: R1 = alkanoyl (2−6 carbon atoms), benzoyl, 2−methylbenzoyl, 3−methylbenzoyl, 4−methylbenzoyl, 2−methoxybenzoyl, 3−methoxybenzoyl, 4−methoxybenzoyl, thiophene−2−carbonyl, thiophene−3−carbonyl, phenylacetyl, 3−phenylpropanoyl, 3−phenylacryloyl; R2 = H, halogen, cyano, nitro, alkyl (1−4 carbon atoms), CF3, CONHR (R = H, alkyl (1−4 carbon atoms)); R3 = H, alkyl (1−4 carbon atoms), allyl; R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring, or R5 = hydrogen and R5 and R6 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring; R7 and R8 can independently be hydrogen, halogen, CF3, CN, NO2 or NH2; or a mono −hydroxy benzazepine derivative of Formula (B): wherein: R1 = H, halogen, cyano, nitro, alkyl (1−4 carbon atoms), CF3, CONHR (R = H, alkyl (1−4 carbon atoms)); R2 = H, alkyl (1−4 carbon atoms), allyl; R3 and R4 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring, or R3 = hydrogen and R4 and R5 together form a furan, dihydrofuran, thiophene, dihydrothiophene, cyclopentane, benzene, cyclohexane ring; R6 and R7 can independently be hydrogen, halogen, CF3, CN, NO2 or NH2; R8 = hydrogen, methyl; and a pharmaceutical composition comprising or consisting of said compound or derivative together with a pharmaceutically acceptable excipient or carrier, for treatment of neurodegenerative disease, for example, Parkinson's disease.