Title:
芳香族アミノ酸誘導体及び医薬組成物
Document Type and Number:
Japanese Patent JP4705756
Kind Code:
B2
Abstract:
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.
Inventors:
Hitoshi Endo
Yoshikatsu Kanai
Kenji Tsujihara
Kunio Saito
Yoshikatsu Kanai
Kenji Tsujihara
Kunio Saito
Application Number:
JP2003565949A
Publication Date:
June 22, 2011
Filing Date:
February 03, 2003
Export Citation:
Assignee:
Hitoshi Endo
International Classes:
C07C229/36; A61K31/198; A61K31/275; A61K31/343; A61K31/352; A61K31/40; A61K31/404; A61K31/4184; A61K31/4188; A61K31/421; A61K31/422; A61K31/423; A61K31/426; A61K31/427; A61K31/437; A61K31/44; A61K31/4402; A61K31/4406; A61K31/4409; A61K31/4418; A61K31/4439; A61K31/454; A61K31/47; A61K31/4725; A61K31/506; A61K31/538; A61K31/541; A61P35/00; A61P43/00; C07C233/47; C07C233/69; C07C255/54; C07C271/10; C07D207/325; C07D207/327; C07D209/08; C07D213/30; C07D213/55; C07D213/74; C07D215/14; C07D215/20; C07D235/18; C07D239/42; C07D263/32; C07D263/56; C07D265/36; C07D277/20; C07D277/24; C07D277/30; C07D277/66; C07D277/82; C07D307/79; C07D307/82; C07D307/83; C07D307/91; C07D311/30; C07D401/04; C07D413/04; C07D417/04; C07D471/04; C07D471/06; C07D487/04; C07D207/32
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Attorney, Agent or Firm:
Shintaro Nogawa