Variation in the aromatic ring of cromakalim: antihypertensive activity of pyranopyridines and 6-alkyl-2H-1-benzopyrans
摘要:
The synthesis and antihypertensive activity in the spontaneously hypertensive rat of two new series of analogues related to cromakalim (1) are described. In the first series, where the benzopyran nucleus has been replaced by a pyranopyridine nucleus, the position of the nitrogen atom has been found to be critical for activity, and the most potent compounds are the pyrano[3,2-c]pyridines. In the second series, where the powerful electron-withdrawing cyano group of compound 1 has been replaced by alkyl and phenyl groups, the order of antihypertensive potency is ethyl, isopropyl, tert-butyl greater than propyl, cyclopentyl greater than methyl greater than phenyl.
SUBSTITUTED PYRROLO[2,3-D] PYRIMIDINES, THEIR PREPARATION AND THEIR THERAPEUTIC APPLICATION
申请人:SANOFI
公开号:EP4105218A1
公开(公告)日:2022-12-21
Disclosed are compounds of formula (I), or a pharmaceutically acceptable salt thereof, wherein R1 and R2 are defined herein. Also disclosed are methods of using such compounds as inhibitors of LRRK2, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating neurodegenerative diseases such as Parkinson's disease,