US4143042A
Expired / Lapsed
US
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1-azaxanthone-3-carboxylic acids
Assignee: Takeda Pharmaceutical Co Ltd
•
Filing: 1978-02-27
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Granted: 1979-03-06
•
Expires: 1998-02-27
Abstract
Abstract The present invention relates to novel 1-azaxanthone-3-carboxylic acid and its derivatives usable for effective medicines for the treatment of allergic diseases, which are shown by the following formula (I) ##STR1## wherein R 1 is hydrogen, alkyl, phenyl, carboxyl, hydroxyl, alkoxy or amino group which may be unsubstituted or substituted by one alkyl, m is 0, 1 or 2 and R 2 is alkyl, alkoxy, halogen, nitro, hydroxy, carboxyl, butadienylene (--CH═CH--CH═CH--) which forms a benzene ring with any adjacent carbon atoms or amino group which may be unsubstituted or substituted by at least one alkyl, and their physiologically acceptable salts.
Inventors
- 👤 Akira Nohara
- 👤 Hirosada Sugihara
- 👤 Kiyoshi Ukawa
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-10-26 19:25
CPC Classifications
C; C07; C07D; C07D491/00; C07D491/02; C07D491/04; C07D311/00; C07D311/02; C07D311/04; C07D311/58
Claims Analysis
Total Claims: 59
Claim 1
Independent Claim
89 words
A compound of the formula: ##STR6## wherein m is 0, 1 or 2; R 1 is hydrogen, C 1-6 alkyl, phenyl, carboxy hydroxy, C 1-4 alkoxy, amino or C 1-3 alkylamino; each R 2 is independently C 1-6 alkyl, C 1-4 alkoxy, halogen, nitro, hydroxy, carboxy, amino, C 1-3 alkylamino or di(C 1-3 alkyl) amino; or when m is 2 the two R 2 groups may be independently as defined above or may form together with adjacent ring carbon atoms the butadienylene group, or a physiologically acceptable salt thereof.
Claim 2
Dependent Claim
89 words
A compound of the formula: ##STR6## wherein m is 0, 1 or 2; R 1 is hydrogen, C 1-6 alkyl, phenyl, carboxy hydroxy, C 1-4 alkoxy, amino or C 1-3 alkylamino; each R 2 is independently C 1-6 alkyl, C 1-4 alkoxy, halogen, nitro, hydroxy, carboxy, amino, C 1-3 alkylamino or di(C 1-3 alkyl) amino; or when m is 2 the two R 2 groups may be independently as defined above or may form together with adjacent ring carbon atoms the butadienylene group, or a physiologically acceptable salt thereof.
Claim 3
Dependent Claim
11 words
A compound as claimed in claim 1, wherein m is 0.
Claim 4
Dependent Claim
11 words
A compound as claimed in claim 1, wherein m is 1.
Claim 5
Dependent Claim
11 words
A compound as claimed in claim 1, wherein m is 2.
Claim 6
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 1 is hydrogen.
Claim 7
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 1 is C 1-6 alkyl.
Claim 8
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 1 is amino.
Claim 9
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 1 is C 1-3 alkylamino.
Claim 10
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 1 is carboxyl.
Claim 11
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 1 is hydroxy.
Claim 12
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 1 is C 1-4 alkoxy.
Claim 13
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 2 is hydrogen.
Claim 14
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 2 is C 1-6 alkyl.
Claim 15
Dependent Claim
12 words
A compound of claim 13, wherein R 2 is in the 7-position.
Claim 16
Dependent Claim
14 words
A compound as claimed in claim 1, wherein R 2 is C 1-4 alkoxy.
Claim 17
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 2 is halogen.
Claim 18
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 2 is nitro.
Claim 19
Dependent Claim
19 words
A compound as claimed in claim 1, wherein R 2 is amino, C 1-3 alkylamino or di(C 1-3 alkyl)amino.
Claim 20
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 2 is hydroxy.
Claim 21
Dependent Claim
12 words
A compound as claimed in claim 1, wherein R 2 is carboxyl.
Claim 22
Dependent Claim
16 words
A compound as claimed in claim 4, wherein the two R 2 groups are from butadienylene.
Claim 23
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-2-methyl-1-azaxanthone-3-carboxylic acid.
Claim 24
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-methyl-1-azaxanthone-3-carboxylic acid.
Claim 25
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-methoxy-2-methyl-1-azaxanthone-3-carboxylic acid.
Claim 26
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2,7,9-trimethyl-1-azaxanthone-3-carboxylic acid.
Claim 27
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-chloro-2-methyl-1-azaxanthone-3-carboxylic acid.
Claim 28
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-nitro-2-methyl-1-azaxanthone-3-carboxylic acid.
Claim 29
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2n-propyl-1-azaxanthone-3-carboxylic acid.
Claim 30
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-2-phenyl-1-azaxanthone-3-carboxylic acid.
Claim 31
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-ethyl-1-azaxanthone-3-carboxylic acid.
Claim 32
Dependent Claim
13 words
A compound as claimed n claim 1, wherein the compound is 2-amino-1-azaxanthone-3-carboxylic acid.
Claim 33
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-methoxy-1-azaxanthone-3-carboxylic acid.
Claim 34
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7,9-dimethyl-1-azaxanthone-3-carboxylic acid.
Claim 35
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-chloro-1-azaxanthone-3-carboxylic acid.
Claim 36
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 1-azaxanthone-3-carboxylic acid.
Claim 37
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-chloro-1-azaxanthone-3-carboxylic acid.
Claim 38
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-nitro-1-azaxanthone-3-carboxylic acid.
Claim 39
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-1-azaxanthone-3-carboxylic acid.
Claim 40
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-chloro-1-azaxanthone-2,3-dicarboxylic acid.
Claim 41
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-1-azaxanthone-2,3-dicarboxylic acid.
Claim 42
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7,9-dimethyl-1-azaxanthone-2,3-dicarboxylic acid.
Claim 43
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-2-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 44
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 45
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-2-methoxy-1-azaxanthone-3-carboxylic acid.
Claim 46
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-ethyl-2-methylamino-1-azaxanthone-3-carboxylic acid.
Claim 47
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-methyl-1-azaxanthone-3-carboxylic acid.
Claim 48
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-isopropyl-1-azaxanthone-3-carboxylic acid.
Claim 49
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-9-methoxy-1-azaxanthone-3-carboxylic acid.
Claim 50
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-n-butyl-1-azaxanthone-3-carboxylic acid.
Claim 51
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-benzo[h]-1-azaxanthone-3-carboxylic acid.
Claim 52
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-8-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 53
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-methyl-2-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 54
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-methoxy-2-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 55
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-hydroxy-7,9-dimethyl-1-azaxanthone-3-carboxylic acid.
Claim 56
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-n-butyl-2-hydroxy-1-azaxanthone-3-carboxylic acid.
Claim 57
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is benzo[h]-1-azaxanthone-3-carboxylic acid.
Claim 58
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 7-isopropyl-1-azaxanthone-3-carboxylic acid.
Claim 59
Dependent Claim
13 words
A compound as claimed in claim 1, wherein the compound is 2-amino-7-dimethylamino-1-azaxanthone-3-carboxylic acid.
References Cited (Backward Citations)
US3931205A
Cited
US4066655A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1982-03-05 | 1982-09-04 | 1983-03-06 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1986-03-05 | 1986-09-04 | 1987-03-06 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1990-03-05 | 1990-09-04 | 1991-03-06 | $7700.00 | Window Closed / Lapsed |