Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1996-06-20
1998-08-11
Ivy, C. Warren
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
546112, C07D22122, A61K 31435
Patent
active
057927758
ABSTRACT:
The present invention provides a family of tropane analogs. More particularly, the present invention provides a family of 4' and 4',4"-substituted-3.alpha.-(diphenylmethoxy)tropane analogs having the formula ##STR1## in which R is a functional group including, but not limited to, hydrogen, alkyl, alkoxy, arylalkyl, aryloxyalkyl, cinnamyl and acyl; and R.sup.1 and R.sup.2 are independently selected and are functional groups including, but not limited to, hydrogen, alkyl, alkoxy, hydroxy, halogen, cyano, amino and nitro. The benztropine analogs of the present invention have a high affinity for the dopamine transporter and inhibit dopamine uptake, but they do not exhibit a cocaine-like behavioral profile. Moreover, the present invention provides methods of using such benztropine analogs to treat cocaine abuse, to image dopamine transporter/cocaine binding sites, and to diagnose and/or monitor neurodegenerative disorders (e.g., Parkinson's disease). In addition, the present invention provides pharmaceutical compositions comprising a benztropine analog of the present invention and a pharmaceutically acceptable carrier or excipient.
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Allen Andrew C.
Izenwasser Sari
Katz Jonathan L.
Kline Richard H.
Newman Amy Hauck
Ivy C. Warren
M. Mach D. Margaret
The United States of America as represented by the Department of
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