US4104388A
Expired / Lapsed
US
⏱️ 0.0 years remaining
3-Substituted benzisothiazole, 1,1-dioxides
Assignee: ER Squibb and Sons LLC
•
Filing: 1977-05-23
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Granted: 1978-08-01
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Expires: 1997-05-23
Abstract
Abstract 3-Substituted benzisothiazole, 1,1-dioxides are provided having the structure ##STR1## wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro; R 1 is hydrogen, lower alkoxy or halogen with the proviso that R 1 can be lower alkoxy or halogen only when R is lower alkoxy or halogen, respectively; Y is C or N, where Y is C, may represent a double bond, and when Y is N, represents a single bond, A is a single bond or an alkylene group containing from 1 to 4 carbons, and B is hydrogen, hydroxyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl, with the proviso that when Y is C, B is phenyl or substituted phenyl, and when Y is N and B is hydrogen, A has at least 1 carbon and when B is hydroxyl, A has at least 2 carbons; and physiologically acceptable acid-addition salts thereof where Y is N. These compounds are useful as antiinflammatory agents.
Inventors
- 👤 Peter C. Wade
- 👤 Thomas P. Kissick
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-05 18:38
CPC Classifications
C; C07; C07D; C07D275/00; C07D275/04; C07D275/06; C07D417/00; C07D417/02; C07D417/04
Claims Analysis
Total Claims: 21
Claim 1
Independent Claim
154 words
A compound of the structure ##STR28## wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro, R 1 is hydrogen, lower alkoxy or halogen with the proviso that R 1 can be lower alkoxy or halogen only when R is lower alkoxy or halogen, respectively; Y is C or N, where Y is C, represents a single bond or a double bond, and when Y is N, represents a single bond, A is a single bond or an alkylene group containing from 1 to 4 carbons, and B is hydrogen, hydroxyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl, with the proviso that when Y is C, B is phenyl or substituted phenyl, and when Y is N and B is hydrogen, A has at least 1 carbon and when B is hydroxyl, A has at least 2 carbons; and physiologically acceptable acid-addition salts thereof where Y is N.
Claim 2
Dependent Claim
154 words
A compound of the structure ##STR28## wherein R is hydrogen, halogen, lower alkyl, lower alkoxy, or nitro, R 1 is hydrogen, lower alkoxy or halogen with the proviso that R 1 can be lower alkoxy or halogen only when R is lower alkoxy or halogen, respectively; Y is C or N, where Y is C, represents a single bond or a double bond, and when Y is N, represents a single bond, A is a single bond or an alkylene group containing from 1 to 4 carbons, and B is hydrogen, hydroxyl, phenyl or phenyl substituted with halogen, lower alkyl, lower alkoxy, or trifluoromethyl, with the proviso that when Y is C, B is phenyl or substituted phenyl, and when Y is N and B is hydrogen, A has at least 1 carbon and when B is hydroxyl, A has at least 2 carbons; and physiologically acceptable acid-addition salts thereof where Y is N.
Claim 3
Dependent Claim
9 words
The compound of claim 1 having the structure ##STR29##
Claim 4
Dependent Claim
9 words
The compound of claim 1 having the structure ##STR30##
Claim 5
Dependent Claim
9 words
The compound of claim 1 having the structure ##STR31##
Claim 6
Dependent Claim
10 words
The compound of claim 1 wherein R 1 is H.
Claim 7
Dependent Claim
18 words
The compound of claim 1 wherein R is in the 5- or 6-position and R 1 is H.
Claim 8
Dependent Claim
20 words
The compound of claim 1 wherein R 1 is lower alkoxy or halogen, and R is lower alkoxy or halogen.
Claim 9
Dependent Claim
16 words
The compound of claim 7 wherein R and R 1 occupy the 5- and 6-positions, respectively.
Claim 10
Dependent Claim
12 words
The compound of claim 2 wherein B is phenyl or substituted phenyl.
Claim 11
Dependent Claim
12 words
The compound of claim 3 wherein B is phenyl or substituted phenyl.
Claim 12
Dependent Claim
12 words
The compound of claim 4 wherein B is phenyl or substituted phenyl.
Claim 13
Dependent Claim
26 words
The compound of claim 4 wherein B is hydrogen, A has at least 1 carbon or B is hydroxyl and A has at least 2 carbons.
Claim 14
Dependent Claim
18 words
The compound of claim 9 wherein R and R 1 are H, and A is a single bond.
Claim 15
Dependent Claim
18 words
The compound of claim 10 wherein R and R 1 are H and A is a single bond.
Claim 16
Dependent Claim
28 words
The compound of claim 4 wherein R and R 1 are H, A is a single bond, CH 2 or (CH 2 ) 2 and B is phenyl.
Claim 17
Dependent Claim
17 words
The compound of claim 12 wherein A is --(CH 2 ) 2 -- and B is hydroxyl.
Claim 18
Dependent Claim
15 words
The compound of claim 4 wherein A is a single bond and B is phenyl.
Claim 19
Dependent Claim
21 words
A compound as defined in claim 1 having the name 3-(4-phenyl-1-piperazinyl)-1,2-benzisothiazole, 1,1-dioxide, 3-(3,6-dihydro-4-phenyl-1(2H)-pyridinyl)-1,2-benzisothiazole, 1,1-dioxide, 4-(1,2-benzisothiazol-3-yl)-1-piperazineethanol, S,S-dioxide hydrochloride, or 3-(4-methyl-1-piperazinyl)-1,2-benzisothiazole, 1,1-dioxide hydrochloride.
Claim 20
Dependent Claim
23 words
A composition for treating an inflammatory condition which comprises an effective amount of a compound of claim 1 in a physiologically acceptable vehicle.
Claim 21
Dependent Claim
23 words
A method for treating an inflammatory condition in a mammalian host, which comprises administering an effective amount of the composition of claim 19.
References Cited (Backward Citations)
US2751392A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-07-31 | 1982-01-30 | 1982-08-01 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-07-31 | 1986-01-30 | 1986-08-01 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-07-31 | 1990-01-30 | 1990-08-01 | $7700.00 | Window Closed / Lapsed |