| 摘要 |
The invention relates to substituted indazole derivatives with a general formula I: where L is -CO-NH- or -СН=N-; A1 is -N, -CH or N-(CH2)n R1; A2 is -N or -СН; R1 is hydrogen or -(С1-С3)alkyl with a straight or branched chain; -(C1-C3)-alkyl, in which one, two, or three hydrogen atoms are substituted by a halogen atom; -(C1-C3)-alkoxy or halogen-(C1-C3)-alkoxy, mono or dihydroxy-(C1-C3)-alkyl; R2 and R3 simultaneously or independently of each other are halogen, hydroxy, halogen-(C1-C3)-alkyl, (C1-C3)-alkoxy, -О-(C1-C3)-alkoxy; where R2 and R3 simultaneously or independently of each other are aryl substituted С3-С5 alkyl under the condition that А is -СН; and where R2 and R3 simultaneously or independently of each other are heteroaryl, substituted with С3-С4 alkyl, under the condition that А is =N; and each n is an independent integer 0, 1, 2 or 3, their pharmaceutically acceptable salts, isomers or their mixtures, which find an application as in vitro selective and reversing МАО-В inhibitors with high levels of enzyme inhibition (IC50) in a subnanomolar range. They are applicable for the prevention and treatment of acute and chronic neurological, cognitive, and neurodegenerative diseases, and particularly for the prevention and treatment of neurodegenerative diseases such as Parkinson's disease, Alzheimer's, and dementia. 4 claims, 6 figures |
