Amino acid derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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514539, 514562, 560 10, 560 12, 560 16, 562420, 562427, 562429, A61K 3121

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active

061660728

ABSTRACT:
Described herein are compounds having the general formula: ##STR1## wherein: Ar.sup.1 and Ar.sup.2 are independently selected aryl groups, optionally substituted with substituents selected from the group consisting of alkyl, cycloalkyl, alkoxy, alkanoyl, aralkyl, aralkyloxy, halo, NO.sub.2, Ph, CF.sub.3, CN, OH, methylenedioxy, ethylenedioxy, SO.sub.2 NRR', NRR', CO.sub.2 R (where R and R' are independently selected from the group consisting of H and alkyl) and a second aryl group, which may be substituted as above;
wherein any cycloalkyl or aryl substituent is linked to Ar.sup.1 or Ar.sup.2 by a bridging element which may be a single bond, a vinylene group, an ethynylene group, a Z group, a --Z--(CH.sub.2).sub.n -- group, a --(CH.sub.2).sub.n --Z-- group, or a --Z--(CH.sub.2).sub.n --Z-- group, where Z represents an O atom, a S atom, an NH group or an N-alkyl group, and n is an integer from 1 to 4;
wherein Ar.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;
wherein Ar.sup.1 and Ar.sup.2 may be attached to the central atom to which they are connected by a single bond, an alkylene, alkenylene or alkynylene group;
R.sup.3 is selected from the group consisting of H and aryl, which may be substituted as for Ar.sup.1 ;
R.sup.4 and R.sup.5 are independently selected from the group consisting of H, alkyl, alkanoyl, benzoyl and benzyl.

REFERENCES:
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Dhar et al., "Design, Synthesis and Evaluation of Substituted Triarylnipecotic Acid Derivatives as GABA Uptake Inhibitors: Identification of a Ligand with Moderate Affinity and Selectivity for the Cloned Human GABA Transporter GAT-3", J. Med. Chem., 37:2334-2342, 1994.
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Pless, "Properties and suitability of the 10, 11-dihydro-5 H-dibenzo[a, d]cyclohepten-5-yl-group (=5-dibenzosuberyl group) as a new protecting group for amines, amino-acids, alcohols, thiols andcarboxylic acids", Helvetica Chemica Acta, 59:499-512, 1976.
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