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1. (WO1991009024) QUINAZOLINE-3-ALKANOIC ACID DERIVATIVE, SALT THEREOF, AND PRODUCTION THEREOF
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/009024 International Application No.: PCT/JP1990/001600
Publication Date: 27.06.1991 International Filing Date: 10.12.1990
IPC:
C07D 239/80 (2006.01) ,C07D 239/95 (2006.01) ,C07D 239/96 (2006.01) ,C07D 401/06 (2006.01) ,C07D 403/04 (2006.01) ,C07D 405/06 (2006.01) ,C07D 409/06 (2006.01) ,C07D 413/06 (2006.01) ,C07D 521/00 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
78
with hetero atoms directly attached in position 2
80
Oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
95
with hetero atoms directly attached in positions 2 and 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
239
Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70
condensed with carbocyclic rings or ring systems
72
Quinazolines; Hydrogenated quinazolines
95
with hetero atoms directly attached in positions 2 and 4
96
Two oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
403
Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
405
Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
409
Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
521
Heterocyclic compounds containing unspecified hetero rings
Applicants:
KYORIN PHARMACEUTICAL CO., LTD. [JP/JP]; 5, Kanda Surugadai 2-chome Chiyoda-ku Tokyo 101, JP (AllExceptUS)
FUJIMORI, Shizuyoshi [JP/JP]; JP (UsOnly)
OHNOTA, Michiro [JP/JP]; JP (UsOnly)
HIRATA, Yoshihiro [JP/JP]; JP (UsOnly)
MURAKAMI, Koji [JP/JP]; JP (UsOnly)
Inventors:
FUJIMORI, Shizuyoshi; JP
OHNOTA, Michiro; JP
HIRATA, Yoshihiro; JP
MURAKAMI, Koji; JP
Agent:
MINOURA, Kiyoshi; Hanabusa Bldg. 16, Kanda-Kitanorimono-cho Chiyoda-ku Tokyo 101, JP
Priority Data:
1/32109711.12.1989JP
Title (EN) QUINAZOLINE-3-ALKANOIC ACID DERIVATIVE, SALT THEREOF, AND PRODUCTION THEREOF
(FR) DERIVE DE L'ACIDE QUINAZOLINE-3-ALCANOIQUE, SELS DERIVES DE CE COMPOSE ET SA PRODUCTION
Abstract:
(EN) A quinazoline-3-alkanoic acid derivative of general formula (I), which has both of platelet agglutination inhibition and aldose reductase inhibition activities, salts thereof, process for producing the same, and a medicine containing the same, wherein R represents hydrogen or a protective group of the carboxyl group; R' represents lower alkyl, alkenyl, alkynyl, lower alkoxy, lower alkylthio, halogen, phenyl (which may be substituted with 1 to 3 substituents selected from among lower alkyl, lower alkoxy, halogen, trifluoromethyl, carboxyethylene, and ethoxy-carbonylethylene groups), naphthyl, heterocycle (which may be substituted with 1 to 3 lower alkyl groups), cycloalkyl, or benzoyl (which may be substituted with lower alkyl or halogen); R2 and R3 may be the same or different from each other and each represents hydrogen, halogen, lower alkyl, lower alkoxy, optionally substituted aralkyl, nitro, imidazolyl, imidazolylmethyl, or -NR4R5 wherein R4 and R5 may be the same or different from each other and each represents hydrogen or lower alkyl, or they are combined with each other to form a 5- or 6-membered heterocycle which may contain other heteroatom(s); X represents carbonyl, thiocarbonyl or methylene (which may be substituted with lower alkyl); A represents lower alkylene or lower alkenylene; and n is an integer of 1 to 3.
(FR) Dérivé de l'acide quinazoline-3-alcanoïque correspondant à la formule générale (I), présentant une activité inhibant aussi bien l'agglutination des plaquettes que l'aldose réductase, sels dérivés de ce composé, procédé de production de ce composé et médicament le contenant. Dans la formule, R représente hydrogène ou un groupe de protection du groupe carboxyle; R' représente alkyle inférieur, alcényle, alkynyle, alcoxy inférieur, alkylthio inférieur, halogène, phényle (qui peut être substitué par 1 à 3 substituants sélectionnés parmi des groupes alkyle inférieur, alcoxy inférieur, halogène, trifluorométhyle, carboxyéthylène et éthoxy-carbonyléthylène), naphtyle, hétérocycle (qui peut être substitué par 1 à 3 groupes alkyle inférieur), cycloalkyle, ou benzoyle (qui peut être substitué par alkyle inférieur ou halogène); R2 etR3 peuvent être identiques ou différents et représentent chacun hydrogène, halogène, alkyle inférieur, alcoxy inférieur, aralkyle éventuellement substitué, nitro, imidazolyle, imidazométhyle, ou -NR4R5 où R4 et R5 peuvent être identiques ou différents et représentent chacun hydrogène ou alkyle inférieur, ou sont combinés entre eux pour former un hétérocycle à 5 ou 6 éléments pouvant contenir un ou plusieurs autres hétéroatomes; X représente carbonyle, thiocarbonyle ou méthylène (qui peut être substitué par alkyle inférieur); A représente alkylène inférieur ou alcénylène; et n est un entier compris entre 1 et 3.
Designated States: AU, CA, HU, KR, US
European Patent Office (BE, CH, DE, ES, FR, GB, IT, NL, SE)
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)
Also published as:
EP0456835ES2087991US5234928CA2046603DE000069027021KR1019920701174
AU1991068905