AROMATIC AMINO ACID DERIVATIVES AND MEDICINAL COMPOSITIONS

摘要

Aromatic amino acid compounds (I) are new. Aromatic amino acid compounds of formula (I) and their salts are new. [Image] X : halo, alkyl or alkoxy; Y : O or NH; p : 0-1; m : 0-2; n : 0-5; R 1H or amino protecting group; R 2halo, aroylamino (optionally N-substituted by Alk), phenyl (substituted by phenyl, phenoxy, pyridyl, pyrimidyl or quinolyl and optionally further substituted by halo, CN, OH, COOH, OAlk, COOAlk, phenyl, N(Alk) 2), naphthyl or tetrahydronaphthyl [both optionally substituted by OH, OAlk or N(Alk) 2(optionally substituted by OH or halo)], monocyclic, unsaturated heterocyclyl containing N, O and/or S (substituted by lower alkyl, phenyl, naphthyl or tetrahydroquinolyl and optionally further substituted by halo, OH or phenyl) or optionally unsaturated or partially unsaturated, fused heterocyclyl containing O, N and/or S {optionally substituted by oxo, COOH, NH 2, Alk, OAlk, cycloalkyl, N(Alk) 2COOAlk, CON(Alk) 2, phenyl or monocyclic optionally unsaturated heterocyclyl [optionally substituted by halo, OH, Alk, OAlk, phenyl N(Alk) 2, OCOAlk, N(lower haloalkyl) 2or N(Alk)(lower hydroxyalkyl)]}; and Alk : lower alkyl; provided that: (i) when R 3= naphthyl then n = 0 or 2; (ii) when R 3= hydroxynaphthyl and X = Cl then m is not 0; and (iii) when R 3= heterocyclyl then m = 1 or 2 and l = 1. ACTIVITY : Cytostatic. In tests on ICR mice implanted with sarcoma 180 cells, 3-(2-naphthyloxy)-L-phenylalanine methyl ester hydrochloride (Ia) (100 mg/kg), exhibited a T/C value for tumor weight of 41.3 %. MECHANISM OF ACTION : LAT-Inhibitor-1.