Carbamate analogs of thiaphysovenine, pharmaceutical...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/40 (2006.01)

Patent

CA 2119782

Substituted carbamates of tricyclic compounds which have a cyclic sulfer atom, having the formula: (See formula I) wherein R1 is H or a linear or branched chain C1- C10 alkyl group; and R2 is selected from the group consisting of a linear or branched chain -C1-C10 alkyl group, and (See formula I) wherein R3 and R4 are independently selected from the group consisting of H and a linear or branched chain C1-C10 -alkyl group; and with the proviso that when one of R1 or R2 is a H or a methyl group the other of R1 or R2 is not H and optical isomers of the 3aS series, provide highly potent and selective cholinergic agonist and blocking activity and are useful as pharmaceutical agents. Cholinergic disease are treated with these compounds such as glaucoma, Myasthenia Gravis, Alzheimer's disease. Methods for inhibiting esterases, acetylcholinesterase and butyryl-cholinesterase are also provided.

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