Selective inhibitors of biogenic amine transporters

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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546 94, 546146, 546150, 548427, 548428, A61K 3140, A61K 3147, C07D40306, C07D47108

Patent

active

055740600

ABSTRACT:
The present invention provides a compound having the structure: ##STR1## wherein X, Y, and Z are independently H, Cl, Br, F, OCH.sub.3, I, or an alkyl group having 1 to 6 carbon atoms; and R is ##STR2## wherein n is 0 to 6, X' and Y' are independently H, Cl, F, CH.sub.3, C.sub.2 H.sub.5, C.sub.3 H.sub.7, C.sub.4 H.sub.9, OCH.sub.3, OH, CF.sub.3, OCF.sub.3, NO.sub.2, NH.sub.2, N(CH.sub.3).sub.2, NHCOCH.sub.3, NCS, NHCOCH.sub.2 Br, or N.sub.3, and (CH.sub.2).sub.n, if present, may be substituted with OH, OCH.sub.3, or an alkyl or alkenyl group having 1 to 3 carbon atoms. The present invention also provides a pharmaceutical composition comprising the compound above and a pharmaceutically acceptable carrier. The present invention further provides a method for treating a disease characterized by a dopamine deficiency which comprises administering to a subject in need of such treatment an amount of the pharmaceutical composition above effective to treat the disease.

REFERENCES:
patent: 5244888 (1993-09-01), DeBernardis et al.
Ordway, J. Pharm. Exp. Therapeutics 247, 379(1988).
"Synthesis and Ligand Binding at PCT Sites 1 and 2 for Hexahydro-2-Substituted-1-Methylindeno[1,2-b]Pyrroles" Carroll et al., Med. Chem. Res (1993) 3:178-182.
"RTI-4793-14, a New Ligand with High Affinity and Selectivity for the (+)-MK801-Insensitive [.sup.3 H]1-[1-(2-thienyl) cyclohexyl]piperidine Binding Site (PCP Site 2) of Guinea Pig Brain", Goodman et al., Synapse 16:59-65 (1994).
"Hydrindene Derivatives as Potential Oral Hypoglycemic Agents: N-Alkyl 1,2,3,3a,4,8b-Hexahydroindeno[1,2-b]pyrroles", De et al., Journal of Pharmaceutical Sciences, vol. 62, No. 8, Aug. 1973, pp. 1363-1364.
"Indolizines II: Search for Potential Oral Hypoglycemic Agents", Journal of Pharmaceutical Sciences, vol. 64, No. 2, Feb. 1975, pp. 249-252.
"Structure Activity Studies on the Interaction of Biogenic Amine Reuptake Inhibitors and Potassium Channel Blockers with MK-801 Sensitive (PCT Site 1) and Insensitive (PCP Site 2) [.sup.3 H]TCP Binding Sites in Guinea Pig Brain", Rothman et al., Multiple Sigma and PCP Receptor Ligands: Mechanisms for Neuromodulation and Neuroprotection, NPP Books, 1992, pp. 137-146.
"[.sup.3 H]1-[2-(2-Thienyl)Cyclohexyl]Piperidine Labels Two High-Affinity Binding Sites in Human Cortex: Further Evidence for Phencyclidine Binding Sites Associated with the Biogenic Amine Reuptake Complex", Akunne et al., Synapse 8:289-300 (1991).
"The Psychotomimetic Drug Phencyclidine Labels Two High Affinity Binding Sites in Guinea Pig Brain: Evidence for N-Methyl-D aspartate-Coupled and Dopamine Reuptake Carrier-Associated Phencyclidine Binding Sites", Rothman et al., Molecular Pharmacology, 36:887-896, 1989.
"MPTP Lesions of the Nigrostriatal Dopaminergic Projection Decrease [.sup.3 H]1-[1-(2-Thienyl)Cyclohexyl]-Piperidine Binding to PCT Site 2: Further Evidence that PCP Site 2 is Associated with the Biogenic Amine Reuptake Complex", Akunne et al, Neurochemical Research, vol. 17, No. 3, 1992, pp. 261-264.

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