AROMATIC AMINO ACID DERIVATIVES AND MEDICINAL COMPOSITIONS

WIPO Patent Application WO/2003/066574

A1

Aromatic amino acid derivatives represented by the following general formula (I) or pharmacologically acceptable salts thereof: (I) wherein R¹ represents hydrogen or an amino-protecting group; R² represents hydrogen, alkylaralkyl or aryl; R³ represents (1) halogeno, (2) aroylamino, (3) phenyl substituted by lower alkyl, phenyl, phenoxy, etc., (4) naphthyl or tetrahydronaphthyl optionally substituted by hydroxy, lower alkoxy or di(lower alkyl)amino, (5) an N-, O- and/or S-containing unsaturated monocyclic heterocycle group substituted by lower alkyl, phenyl, naphthyl or tetrahydroquinolyl, or (6) an N-, O- and/or S-containing fused heterocycle group, which may be unsaturated or partly saturated, optionally substituted by oxo, carboxy, amino, lower alkyl, etc.; X represents halogeno, alkyl or alkoxy; Y represents oxygen or nitrogen; l is 0 or 1; m is 0, 1 or 2; and n is an integer of from 0 to 5. These compounds inhibit a transporter (LAT1) of essential amino acids which are one of the main nutrients for cancer cells and induce depletion of the essential amino acids in the cancer cells, thereby inhibit the proliferation of the cancer cells.

JP4658940	Benzimidazole derivative as a factor Xa inhibitor
JP6141831	A CD3 joint molecule combinable with humans and nonhuman CD3

ENDO HITOSHI (JP)
KANAI YOSHIKATSU (JP)
TSUJIHARA KENJI (JP)
SAITO KUNIO (JP)

PCT/JP2003/001081

August 14, 2003

February 03, 2003

Click for automatic bibliography generation  

ENDO HITOSHI (JP)
KANAI YOSHIKATSU (JP)
TSUJIHARA KENJI (JP)
SAITO KUNIO (JP)

A61P35/00; A61P43/00; C07C229/36; C07C233/47; C07C233/69; C07C255/54; C07C271/10; C07D207/325; C07D209/08; C07D213/30; C07D213/74; C07D215/14; C07D235/18; C07D239/42; C07D263/32; C07D263/56; C07D265/36; C07D277/24; C07D277/66; C07D307/79; C07D307/82; C07D307/83; C07D307/91; C07D311/30; C07D401/04; C07D413/04; C07D417/04; C07D471/06; C07D207/32; (IPC1-7): C07C229/36; C07C255/54; C07D207/333; C07D209/08; C07D213/30; C07D213/74; C07D215/20; C07D263/32; C07D263/56; C07D277/24; C07D307/80; C07D307/91; C07D311/30; C07D317/64; C07D401/04; C07D413/04; C07D417/04; C07D471/04; A61K31/198; A61K31/277; A61K31/343; A61K31/352; A61K31/36; A61K31/402; A61K31/404; A61K31/421; A61K31/422; A61K31/423; A61K31/426; A61K31/44; A61K31/4439; A61K31/47; A61P35/00; A61P43/00; A61K31/437; A61K31/454; A61K31/505; A61K31/506; A61K31/5375; A61K31/54; A61K31/4725; C07D215/14

WO1998000137A1	1998-01-08
WO1996038415A1	1996-12-05
WO2000071101A2	2000-11-30
WO1996040745A2	1996-12-19

US5364876A	1994-11-15
JP2000342270A	2000-12-12

SUCHOLEIKI I. ET AL.: "New polyoxyalkyleneamine-grafted paramagnetic supports for solid-phase synthesis and bioapplications", TETRAHEDRON LETTERS, vol. 42, 2001, pages 3279 - 3282, XP004235289
KOEHRLE J. ET AL.: "Rat liver iodothyronine monodeiodinase", THE JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 261, no. 25, 1986, pages 11613 - 11622, XP002968439
BLANEY J.M. ET AL.: "Computer graphics in drug design: molecular modeling of thyroid hormone-prealbumin interactions", J. MED. CHEM., vol. 25, 1982, pages 785 - 790, XP002968440
DIETRICH S.W. ET AL.: "Thyroxine analogues. 23. Quantitative structure-activity correlation studies of in vivo and in vitro thyromimetic activities", J. MED. CHEM., vol. 20, no. 7, 1977, pages 863 - 880, XP002968441
JORGENSEN E.C. ET AL.: "Thyroxine analogs. 20. Substituted 1- and 2-naphthyl ethers of 3,5-diiodothyrosine", J. MED. CHEM., vol. 14, no. 11, 1971, pages 1023 - 1026, XP002968442
KANAI Y. ET AL., JOURNAL OF BIOLOGICAL CHEMISTRY, vol. 273, 1998, pages 23629
See also references of EP 1481965A4

Nogawa, Shintaro (1-3 Nishitenma 5-chome, Kita-k, Osaka-shi Osaka, JP)

View/Download PDF      PDF Help

Previous Patent: METAL SALTS OF CARNITINES, DIETARY SUPPLEMENTS CONTAINING SAME AND DIETARY KITS FOR COUNTERACING SEX...

Next Patent: PROCESS FOR THE SYNTHESIS OF N−ACYL−2−AMINO−4−ALKOXY−5−NITROBENZOIC ACIDS