US4110449A
Expired / Lapsed
US
⏱️ 0.0 years remaining
2-substituted benzisothiazol-3-ones
Assignee: ER Squibb and Sons LLC
•
Filing: 1977-05-23
•
Granted: 1978-08-29
•
Expires: 1997-05-23
Abstract
Abstract 2-Substituted benzisothiazol-3-ones 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; X is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; Y is C or N, where Y is C, --------represents a single or double bond, and when Y is N, --------represents a single bond, p is 0 or 2, A is an alkylene group containing 2 to 5 carbons in the normal chain; and B is a single bond or an alkylene group containing from 1 to 3 carbons in the normal chain, and physiologically acceptable acid-addition salts thereof. These compounds have antiinflammatory activity, sedative and muscle relaxant activity. Pharmaceutical compositions containing such compounds and methods for using such compounds are also provided.
Inventors
- 👤 Peter C. Wade
- 👤 B. Richard Vogt
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-08 15:11
CPC Classifications
C; C07; C07D; C07D275/00; C07D275/04; C07D275/06; C07D211/00; C07D211/04; C07D211/68; C07D211/70
Claims Analysis
Total Claims: 25
Claim 1
Independent Claim
110 words
A compound of the structure ##STR95## 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; X is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; Y is C or N, where Y is C, represents a double bond, and when Y is N, represents a single bond, A is an alkylene group containing 2 to 5 carbons; and B is a single bond or an alkylene group containing from 1 to 3 carbons, and physiologically acceptable acid-addition salts thereof.
Claim 2
Dependent Claim
110 words
A compound of the structure ##STR95## 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; X is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; Y is C or N, where Y is C, represents a double bond, and when Y is N, represents a single bond, A is an alkylene group containing 2 to 5 carbons; and B is a single bond or an alkylene group containing from 1 to 3 carbons, and physiologically acceptable acid-addition salts thereof.
Claim 3
Dependent Claim
9 words
The compound of claim 1 having the structure ##STR96##
Claim 4
Dependent Claim
9 words
The compound of claim 1 having the structure ##STR97##
Claim 5
Dependent Claim
12 words
The compound of claim 1 wherein R and R 1 are hydrogen.
Claim 6
Dependent Claim
18 words
The compound of claim 1 wherein R is in the 5- or 6-position and R 1 is hydrogen.
Claim 7
Dependent Claim
24 words
The compound of claim 2 wherein R is hydrogen, A is (CH 2 ) 2 , B is a single bond, X is hydrogen.
Claim 8
Dependent Claim
24 words
The compound of claim 3 wherein R is hydrogen, A is (CH 2 ) 2 , B is a single bond, X is hydrogen.
Claim 9
Dependent Claim
19 words
The compound of claim 1 wherein A is --(CH 2 ) 2 -- or --(CH 2 ) 3 --.
Claim 10
Dependent Claim
12 words
A compound as defined in claim 1 having the name 2-[2-(3,6-dihydro-4-phenyl-1(2H)-pyridinyl)ethyl]-1,2-benzisothiazol-3(2H)-one, 1,1-dioxide.
Claim 11
Dependent Claim
16 words
A compound as defined in claim 1 having the name 2-[(4-phenyl-1-piperazinyl)ethyl]-1,2-benzisothiazol-3(2H)-one, 1,1-dioxide, or its hydrochloride salt.
Claim 12
Dependent Claim
112 words
A compound of the structure ##STR98## 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; X is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; Y is C or N, where Y is C, represents a single or double bond, and when Y is N, represents a single bond, A is an alkylene group containing 2 to 5 carbons; and B is a single bond or an alkylene group containing from 1 to 3 carbons, and physiologically acceptable acid-addition salts thereof.
Claim 13
Dependent Claim
112 words
A compound of the structure ##STR98## 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; X is hydrogen, halogen, lower alkyl, lower alkoxy, or trifluoromethyl; Y is C or N, where Y is C, represents a single or double bond, and when Y is N, represents a single bond, A is an alkylene group containing 2 to 5 carbons; and B is a single bond or an alkylene group containing from 1 to 3 carbons, and physiologically acceptable acid-addition salts thereof.
Claim 14
Dependent Claim
15 words
A compound as defined in claim 11 having the name 2-[2-(3,6-dihydro-4-phenyl-1(2H)-pyridinyl)ethyl]-1,2-benzisothiazol-3(2H)-one or its hydrochloride salt.
Claim 15
Dependent Claim
9 words
The compound of claim 11 having the structure ##STR99##
Claim 16
Dependent Claim
24 words
The compound of claim 13 wherein R is hydrogen, A is (CH 2 ) 2 , B is a single bond, X is hydrogen.
Claim 17
Dependent Claim
9 words
The compound of claim 11 having the structure ##STR100##
Claim 18
Dependent Claim
9 words
The compound of claim 11 having the structure ##STR101##
Claim 19
Dependent Claim
12 words
The compound of claim 11 wherein R and R 1 are hydrogen.
Claim 20
Dependent Claim
27 words
A composition which comprises a compound of claim 1 in a physiologically acceptable vehicle, said compound being present in an effective amount for treating an inflammatory condition.
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 18.
Claim 22
Dependent Claim
21 words
A method for treating anxiety in a mammalian host, which comprises administering an effective amount of the composition of claim 18.
Claim 23
Dependent Claim
27 words
A composition which comprises a compound of claim 11 in a physiologically acceptable vehicle, said compound being present in an effective amount for treating an inflammatory condition.
Claim 24
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 21.
Claim 25
Dependent Claim
21 words
A method for treating anxiety in a mammalian host, which comprises administering an effective amount of the composition of claim 21.
References Cited (Backward Citations)
US2751392A
Cited
US3457272A
Cited
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1981-08-28 | 1982-02-27 | 1982-08-29 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1985-08-28 | 1986-02-27 | 1986-08-29 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1989-08-28 | 1990-02-27 | 1990-08-29 | $7700.00 | Window Closed / Lapsed |