US4218476A
Expired / Lapsed
US
⏱️ 0.0 years remaining
Anti-thrombotic N-alkylthioakylamino benzenesulfonamides
Assignee: Phadia AB
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Filing: 1978-08-03
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Granted: 1980-08-19
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Expires: 1998-08-03
Abstract
Abstract New compounds of the general formula I ##STR1## wherein R 1 and R 2 each independently represent an alkyl group containing 1 to 4 carbon atoms, or an alkoxy group containing 1 to 3 carbon atoms, or halogen, R 3 represents hydrogen, halogen, an alkyl group containing 1 to 4 carbon atoms, an alkoxy group containing 1 to 3 carbon atoms, an amino group or a nitro group, A represents ##STR2## which is bonded to the benzene ring by its sulphur or nitrogen atom and in which R 4 is hydrogen or an alkyl group containing 1 to 4 carbon atoms; together with salts thereof with physiologically acceptable acids and, when R 4 is hydrogen, with physiologically acceptable bases are described. The compounds are of use in inhibiting thrombosis formation, in treating thrombosis and in fibronolytic therapy. Various methods of producing the new compounds are described involving the building up of the --A--CH 2 --CH 2 --S--CH 2 CH 2 NH 2 side chain from aromatic precursors having an incomplete side chain or by introducing at least one of the R 1 , R 2 or R 3 substituents into a precursor lacking that substituent or from an amino-protected precursor.
Inventors
- 👤 Aake N. Joensson
- 👤 Ferenc Merenyi
- 👤 Pinchas Moses
- 👤 Lennart E. Karlsson
- 👤 Gunnar Hanshoff
Bibliographic Details
Application Number
—
Jurisdiction
US
Data Source
google_patents
Last Synchronized
2026-11-06 15:00
CPC Classifications
C; C07; C07D; C07D209/00; C07D209/02; C07D209/44; C07D209/48; A; A61; A61P; A61P7/00; A61P7/02; C07C; C07C309/00
Claims Analysis
Total Claims: 19
Claim 1
Independent Claim
125 words
A di-orthosubstituted benzene compound characterised in that it has the general formula (I) ##STR21## wherein R 1 and R 2 each independently represent an alkyl group containing 1 t b 4 carbon atoms, or analkoxy group containing 1 to 3 carbon atoms, or halogen, R 3 represents hydrogen, halogen, an alkyl group containing 1 to 4 carbon atoms, an alkoxy group containing 1 to 3 carbon atoms, an amino group or a nitro group, A represents ##STR22## which is bonded to the benzene ring by its sulphur or nitrogen atom and in which R 4 is hydrogen or an alkyl group containing 1 to 4 carbon atoms; together with salts thereof with physiologically acceptable acids and, when R 4 is hydrogen, with physiologically acceptable bases.
Claim 2
Dependent Claim
125 words
A di-orthosubstituted benzene compound characterised in that it has the general formula (I) ##STR21## wherein R 1 and R 2 each independently represent an alkyl group containing 1 t b 4 carbon atoms, or analkoxy group containing 1 to 3 carbon atoms, or halogen, R 3 represents hydrogen, halogen, an alkyl group containing 1 to 4 carbon atoms, an alkoxy group containing 1 to 3 carbon atoms, an amino group or a nitro group, A represents ##STR22## which is bonded to the benzene ring by its sulphur or nitrogen atom and in which R 4 is hydrogen or an alkyl group containing 1 to 4 carbon atoms; together with salts thereof with physiologically acceptable acids and, when R 4 is hydrogen, with physiologically acceptable bases.
Claim 3
Dependent Claim
21 words
A compound according to claim 1, wherein the sulphonamide group A is bonded to the benzene ring by its sulphur atom.
Claim 4
Dependent Claim
18 words
A compound according to claim 1 or 2, wherein R 1 and R 2 both represent methyl groups.
Claim 5
Dependent Claim
11 words
A compound according to claim 3, wherein R 4 is H.
Claim 6
Dependent Claim
19 words
A compound according to claim 3 wherein R 3 is H or a para methyl propyl or butyl group.
Claim 7
Dependent Claim
19 words
A compound according to claim 5 which is N-(5-amino-3-thiapentyl)-2,6-dimethylbenzene sulphonamide, or N-(5-amino-3-thiapentyl)-2,4,6-trimethylbenzene sulphonamide, or N-(5-amino-3-thiapentyl)-2,6-dimethyl-4-ispropylbenzene sulphonamide or N-(5-amino-3-thiapentyl)-2,6-dimethyl-4-tert.-butylbenzene sulphonamide.
Claim 8
Dependent Claim
11 words
A compound according to claim 2 wherein R 4 is H.
Claim 9
Dependent Claim
19 words
A compound according to claim 2 wherein R 3 is H or a para methyl, propyl or butyl group.
Claim 10
Dependent Claim
39 words
A pharmaceutical composition comprising a compound or salt according to any one of claims 1, 2, 7 or 8 in an amount effective for inhibiting or combatting thrombosis or for supplementing fibronolytic therapy together with a pharmaceutically acceptable carrier.
Claim 11
Independent Claim
60 words
A method or treatment for inhibiting formation of thrombosis or combatting thrombosis or supplementing fibrnolytic therapy which comprises administering to a host in need of such treatment a compound or salt according to any one of claims 1, 2, 7 or 8 in an amount effective for inhibiting formation of thrombosis or for combatting thrombosis or for supplementing fibronolytic therapy.
Claim 12
Dependent Claim
32 words
A pharmaceutical composition comprising a compound or salt according to claim 3 in an amount effective for inhibiting or combatting thrombosis or for supplementing fibronolytic therapy together with a pharmaceutically acceptable carrier.
Claim 13
Dependent Claim
32 words
A pharamaceutical composition comprising a compound or salt according to claim 4 in an amount effective for inhibiting or combatting thrombosis or for supplementing fibronolytic therapy together with a pharamaceutically acceptable carrier.
Claim 14
Dependent Claim
32 words
A pharmaceutical composition comprising a compound or salt according to claim 5 in an amount effective for inhibitng or combatting thrombosis or for suplementing fibronolytic therapy together with a pharmaceutically acceptable carrier.
Claim 15
Dependent Claim
32 words
A pharmaceutical composition comprising a compound or salt according to claim 6 in an amount effective for inhibiting or combatting thrombosis or for supplementing fibronolytic therapy together with a pharmaceutically acceptable carrier.
Claim 16
Dependent Claim
53 words
A method or treatment for inhibiting formation of thrombosis or combatting thrombosis or supplementing fibronolytic therapy which comprises administering to a host in need of such treatment a compound or salt according to claim 3 in an amount effective of inhibiting formation of trombosis or for combatting thrombosis or for supplementing fibronolytic therapy.
Claim 17
Dependent Claim
53 words
A method or treatment for inhibiting formation of thrombosis or combatting thrombosis or supplementing fibronolytic therapy which comprises administering to a host in need of such treatment a compound or salt according to claim 4 in an amount effective for inhibiting formation of thrombosis or for combatting thrombosis or for supplementing fibronolytic therapy.
Claim 18
Dependent Claim
53 words
A method or treatment for inhibiting formation of thrombosis or combatting thrombosis or supplementing fibronolytic therapy which comprises administering to a host in need of such treatment a compound or salt according to claim 5 in an amount effective for inhibiting formation of thromobosis or for combatting thrombosis or for supplementing fibronolytic therapy.
Claim 19
Dependent Claim
53 words
A method or treatment for inhibiting formation of thrombosis or combatting thrombosis or supplementing fibronlytic therapy which comprises administering to a host in need of such treatment a compound or salt according to claim 6 in an amount effective for inhibiting formation of thrombosis or for combatting thrombosis or for supplementing fibronolytic therapy.
References Cited (Backward Citations)
USPTO Annuity & Maintenance Windows
| Annuity Stage | Window Opens | Payment Deadline | Surcharge Period Until | Estimated Fee | Status |
|---|---|---|---|---|---|
| 3.5 Years (Year 4) | 1983-08-19 | 1984-02-18 | 1984-08-19 | $2000.00 | Window Closed / Lapsed |
| 7.5 Years (Year 8) | 1987-08-19 | 1988-02-18 | 1988-08-19 | $3760.00 | Window Closed / Lapsed |
| 11.5 Years (Year 12) | 1991-08-19 | 1992-02-18 | 1992-08-19 | $7700.00 | Window Closed / Lapsed |