New bivalent gamma-carboline derivatives, useful as anti-dementia drugs, cognition enhancers and/or substance for increasing memory capacity

摘要

Bivalent gamma -carboline derivatives (I), are new. Bivalent gamma -carboline derivatives having a structure of formula (I), are new. R1, R9 : absent, H, haloalkyl, haloalkoxy, hydroxyalkyl with linear or branched alkyl, aminoalkyl, linear or branched alkyl, aryl, or heteroaryl; R2-R8, R10-R16 : absent, H, halogen, haloalkyl, haloalkoxy, alkoxy with linear or branched alkyl, hydroxy, amino, nitro, linear or branched alkyl, alkylthio, alkylamino, aryl, heteroaryl, aryloxy, haloaryloxy, arylthio or arylamino; X : branched alkylene, -(CH 2) n1, -(CH 2)-Ar-(CH 2) n2, or -(CH 2) n3-Z-(CH 2) n3; Z : O, S, NR; R : H, acyl, alkyl; ring A, ring A1a : aromatic; ring C, ring C1a : aromatic or partially or completely hydrogenated, when ring C is aromatic or is non-hydrogenated to nitrogen adjacent to the carbon atoms and R1 and R9 are present so that the nitrogen is positively charged; Y1 : halide, sulfate, hydrogensulftate, phosphate and other inorganic anions, alkanoate, benzoate, where the number and value of the anions is determined so that the sum of the charges is balanced; n1 : 1-12; n2 : 1-5; and n3 : 1-6. An independent claim is included for preparing (I). [Image] ACTIVITY : Nootropic. MECHANISM OF ACTION : Cholinesterase inhibitor; N-methyl-D-aspartate receptor antagonist.