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1. (WO1988007043) PHARMACOLOGICALLY ACTIVE CHOLINERGIC COMPOSITIONS, AND METHODS FOR MAKING SAME AND USE THEREOF IN TREATING DISEASE

Pub. No.:    WO/1988/007043    International Application No.:    PCT/US1988/000687
Publication Date: Sep 22, 1988 International Filing Date: Mar 9, 1988
IPC: C07D 405/04
Applicants: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW
BETH ISRAEL HOSPITAL
Inventors: SCHULMAN, Jerome, M.
GOYAL, Raj, K.
Title: PHARMACOLOGICALLY ACTIVE CHOLINERGIC COMPOSITIONS, AND METHODS FOR MAKING SAME AND USE THEREOF IN TREATING DISEASE
Abstract:
Compounds useful as cholinergic drugs are disclosed which have formula A-B and pharmaceutically acceptable salts thereof having the formula [(A-B)Q]+qM-q, wherein M is a pharmaceutically acceptable anion, Q is a proton or lower alkylating group, q is an integer from 1 to 3, A is a saturated or unsaturated five- or six-membered heterocyclic moiety having formula (I) and B is a saturated or unsaturated five-membered heterocyclic moiety having formula (II), wherein R?1 and R2¿ are each independently hydrogen, halo, branched or straight-chain C¿1?-C6 alkyl, branched or straight-chain C1-C6 haloalkyl, branched or straight-chain C1-C6 alkoxy, hydroxyl, keto or aryl; Y is -N= or α; Z is -N=, α, -O-, -S-, β; and R?3, R4 and R5¿ are each independently H, lower alkyl or aryl; W is -O-, -N=, or -S-; m is an integer from 1 to 5; n is an integer from 0 to 7; p is 0 or 1; and wherein, on a given molecule, when m is 2, or more, the R1's can be the same or different and two R1's can form a carbocyclic or heterocyclic moiety fused onto adjacent positions of A and when p is 1, the two W's can be the same or different; and when n is 2 or more, the R2's can be the same or different and two R2's can form a carbocyclic or heterocyclic moiety fused onto adjacent positions of B. Pharmaceutical compositions useful in treating disorders of the central and peripheral nervous system of mammals, comprising an effective amount of the aforesaid compounds, can be administered orally or intravenously.