| abstract |
Provided are a long-acting prodrug of Rasagiline, preparation method and use thereof. The long-acting prodrug of Rasagiline has a structure of formula (I), wherein T is absent, or T is selected from (II); each of R 1 and R 2 is independently selected from H, D, and alkyl; W is absent, or W is selected from (CH 2 ) n , wherein n is an integer selected from 1 to 15; X is absent, or X is selected from (CH 2 ) m , wherein m is an integer selected from 1 to 10; Y is absent, or Y is selected from -C(=O)NH-, -NHC(=O)-; R 3 is selected from substituted or unsubstituted C 1 -C 30 alkyl, substituted or unsubstituted C 2 -C 30 alkenyl, substituted or unsubstituted C 2 -C 30 alkynyl, substituted or unsubstituted C 3 -C 30 cycloalkyl, cholane aliphatic group, -R 3a -C(=O)O-R 3b , -R 3a -OC(=O)-R 3b , -R 3a -C(=O)NH-R 3b , -R 3a -NHC(=O)-R 3b , -R 3a -S(=O) 1-2 O-R 3b and -R 3a -OS(=O) 1-2 -R 3b . The provided prodrug of Rasagiline has a high melting point and low solubility, and it can form a drug reservoir in the body after being administered if it is made in a form of injection, prolonging the release rate of the prodrug in the body and achieving an effect of long-acting treatment. |