Title:
QUINAZOLINE DERIVATIVE, PREPARATION THEREOF AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME FOR ANTI-TUMOR ACTIVITY IN HOMOIOTHERMIC ANIMAL
Document Type and Number:
Japanese Patent JP3160111
Kind Code:
B2
Abstract:
PURPOSE: To provide the new compounds having anti-tumor activity which exert no toxic symptoms with respect to liver and kidney.
CONSTITUTION: The compounds are those represented by formula I, e.g. 2-{p-[N-(2methyl-4-oxo-3,4-dihydroqunazolin-6-ylmethyl)-N-(prop-2-ynyl) amino]benzamide}-4-(tetrazol-5-yl) lactic acid, which are obtained by allowing compounds of formula II (R4 is H or a protective group) and compounds of formula III (R5 is a protective group) to react with each other and subsequently removing protective groups. In formula I, R1 is 1-4C alkyl; the quinazoline ring may optionally bear one or two further substituents selected from halogen, 1-4C alkyl and 1-4C alkoxy on 5-, 7- or 8-position; R2 is H or 1-4C alkyl; R3 is H, 1-4C alkyl, 3-4C alkenyl, 3-4C alkynyl, hydroxy-2-4C alkyl, halogen-(2-4C) alkyl, cyano-(2-4C)alkyl; Ar is phenylene or heterocyclene optionally substituted by one or two substituent(s) selected from halogen, 1-4C alkyl, 1-4C alkoxy.
Inventors:
Stephen John Pegg
James Michael Wardleworth
James Michael Wardleworth
Application Number:
JP5052593A
Publication Date:
April 23, 2001
Filing Date:
March 11, 1993
Export Citation:
Assignee:
Zeneca Limited
Beati G International Limited
Beati G International Limited
International Classes:
A61K31/505; A61K31/495; A61K31/517; A61P35/00; C07D239/88; C07D239/95; C07D257/04; C07D401/14; C07D403/12; (IPC1-7): C07D403/12; A61K31/517; A61P35/00
Domestic Patent References:
| JP2218668A | ||||
| JP61282368A | ||||
| JP5692876A |
Foreign References:
| EP0459730A2 |
Other References:
【文献】欧州特許出願公開459730(EP,A2)
Attorney, Agent or Firm:
Toshio Yano (1 outside)