New eseroline derivs. having anti-cholinesterase activity - used for treating Alzheimer's disease, pain myasthenia gravis, glaucoma, memory dysfunction and neuromuscular disorders

摘要

Eseroline derivs. of formula (I) are new, where W is a substit. (a)-(f): (a) R1-CH(COOR2)-, where R1 is H, -CH(CH3)2, CH2CH(CH3)2 or CH(CH3)CH2CH3; and R2 is H or 1-20C acyl; (b) -A-COOR3, where A is 2-8C alkyl opt. contg. one or more ethylenic unsaturations; 2-8C ketoalkyl, 2-8C hydroxyalkyl opt. esterified with an organic acid; and R3 is H or 1-20C alkyl opt. contg. one or more ethylenic unsaturations provided that when R3 is H, A must be different from ketoalkyl; (c) R4OM, where R4 is H or CH3-(L)m-CO-; L is a bivalent 1-20C alkyl opt. contg. one or more ethylenic unsaturations, m is 0-1, and M is 1-20C bivalent alkyl opt. substd. with an aryl gp., a bivalent alicyclic 3-7C gp. or is a bivalent aryl gp.; (d) R5R6N-(CH2)n-, where R5 and R6 are H or 1-20C alkyl, and n is 1-20; gp. of formula (e), where R8 is -(CH2)o-, CH3-(CH2)p-CH, (CH3CH2)2C, CH2=C-CH2-, or gp. of formula (i) or (ii); o is 1-8; p is 1-3; and R9 is H or CH3; and gp. of formula (f), where R11 is H or COOH, R10 is H or 2-20C acyl, the carbon atom indicated with the asterisk when R11 is COOH is an asymmetric C and is characterised by having L, D or (D, L) configuration; HY is a pharmaceutically acceptable organic or inorganic acid; and x may be 0-3 in the case of monofunctional acids provided that x is 3 only when W is R5R6N-(CH2)n- or 1/2 and Y3 in the case of respectively bisfunctional or trifunctional acids; HY may be e.g. tartaric acid, citric acid, salicylic acid, maleic acid, HCl, phosphoric acid or sulphonic acid.