US4698349A
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US
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Quinolizinone compounds, and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents
Assignee: Astellas Pharma Inc
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Filing: 1985-08-30
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Granted: 1987-10-06
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Expires: 2005-08-30
Abstract
Abstract The invention relates to novel quinolizinone compounds, of inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R 1 is carboxy, carbamoyl Y 1 , phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl, R 7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl; R 2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and R 3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy; or pharmaceutically acceptable salts thereof.
Inventors
- 👤 Yoshihiko Kitaura
- 👤 Teruo Oku
- 👤 Hideo Hirai
- 👤 Tosiyuki Yamamoto
- 👤 Masashi Hashimoto
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-27 18:00
CPC Classifications
C; C07; C07D; C07D455/00; A; A61; A61P; A61P1/00; A61P1/04; A61P37/00; A61P37/08; A61P43/00; C07D455/02; C07D455/03; C07D455/04; C07D455/06; C07F; C07F7/00; C07F7/02; C07F7/08; C07F7/18; C07F7/1804; Y; Y02; Y02P; Y02P20/00; Y02P20/50; Y02P20/55
Claims Analysis
Total Claims: 18
Claim 1
Independent Claim
134 words
A compound of the formula: ##STR6## wherein R 1 is carboxy, carbamoyl, phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl, R 7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl; R 2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and R 3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and P-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy; or pharmaceutically acceptable salts thereof.
Claim 2
Dependent Claim
134 words
A compound of the formula: ##STR6## wherein R 1 is carboxy, carbamoyl, phenylcarbamoyl which may have hydroxy, cyano or thiocarbamoyl, R 7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl; R 2 is hydrogen, hydroxy, lower alkyl or lower alkoxy; and R 3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and P-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy; or pharmaceutically acceptable salts thereof.
Claim 3
Dependent Claim
80 words
A compound of claim 1, wherein R 1 is carboxy, carbamoyl, phenylcarbamoyl, phenylcarbamoyl having hydroxy, cyano or thiocarbamoyl, R 7 is hydrogen or phenyl, R 2 is hydrogen, hydroxy, lower alkyl or lower alkoxy, R 3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkoxycarbonyl, carboxy, lower alkenyloxy, phenyl, naphthyl, biphenyl, phenyl having a lower alkyl, phenyl having a halogen, phenyl having a lower alkoxy, phenylthio, benzoyl, phenyl(lower)alkyl, benzenesulfonyl, phenylamino having a lower alkyl on the nitrogen atom, or phenoxy.
Claim 4
Dependent Claim
52 words
A compound of claim 2, wherein R 1 is carboxy, carbamoyl, phenylcarbamoyl, 2-hydroxyphenylcarbamoyl, cyano or thiocarbamoyl, R 2 is hydrogen, hydroxy, methyl, ethyl or methoxy, and R 3 is hydrogen, hydroxy, methyl, methoxy, isopropoxy, n-butoxy, ethoxycarbonyl, carboxy allyloxy, phenyl, naphthyl, biphenyly, 3-methylphenyl, phenoxy, 4-chlorophenyl, 2-methylphenyl, 3-methoxyphenyl, benzyl, phenylthio, benzoyl, benzenesulfonyl or N-methylanilino.
Claim 5
Dependent Claim
10 words
A compound of claim 1, wherein R 1 is carboxy.
Claim 6
Dependent Claim
2 words
4H-Quinolizin-4-one-3-carboxylic acid.
Claim 7
Dependent Claim
2 words
4H-Quinolizin-4-one-3-carboxylic acid.
Claim 8
Dependent Claim
2 words
1-Phenyl-4H-quinolizin-4-one-3-carboxylic acid.
Claim 9
Dependent Claim
2 words
1-Phenyl-4H-quinolizin-4-one-3-carboxylic acid.
Claim 10
Dependent Claim
2 words
1-Phenoxy-4H-quinolizin-4-one-3-carboxylic acid.
Claim 11
Dependent Claim
2 words
1-Phenoxy-4H-quinolizin-4-one-3-carboxylic acid.
Claim 12
Dependent Claim
2 words
1-Benzoyl-4H-quinolizin-4-one-3-carboxylic acid.
Claim 13
Dependent Claim
2 words
1-Benzoyl-4H-quinolizin-4-one-3-carboxylic acid.
Claim 14
Dependent Claim
30 words
An antiulcerative composition comprising an antiulcerative effective amount of a compound of claim 1 or pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable, substantially non-toxic carrier or excipient.
Claim 15
Dependent Claim
35 words
A method for treating ulcer disease in human beings or animals which comrpises administering an antiulceratively effective amount of a compound of claim 1 or pharmaceutically acceptable salt thereof to said human beings or animals.
Claim 16
Dependent Claim
30 words
An antiallergic composition comprising an antiallergically effective amount of a compound of claim 1 or pharmaceutically acceptable salt thereof in association with a pharmaceutically acceptable, substantially non-toxic carier or excipient.
Claim 17
Dependent Claim
35 words
A method for treating allergic disease in human beings or animals which comprises administering an antiallergically effective amount of a compound of claim 1 or pharmaceutically acceptable salt thereof to said human beings or animals.
Claim 18
Dependent Claim
95 words
A compound of claim 4, wherein R 7 and R 2 are each hydrogen, and R 3 is lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, naphthyl, biphenylyl, phenyl having one or more substituents selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolythio, xylylthio, cumenylthio, naphthylthio and biphenylylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenyloxy and tolyloxy.
References Cited (Backward Citations)
No citation records indexed.
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