Claims
- 1. A compound selected from the group consisting of 6-substituted 7-unsubstituted 1,2-benzisothiazolin-3-ones depicted by the formula: ##STR48## and the pharmaceutically acceptable acid addition salts thereof wherein
- R.sup.1 when taken independently of R.sup.2 is chloro, bromo, fluoro, nitro, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms or an aromatic substituent selected from the group consisting of phenoxy, benzyloxy and phenylthio which aromatic substituent is unsubstituted or substituted with alkyl of 1 to 4 carbon atoms or halo;
- R.sup.2 when taken independently of R.sup.1 is hydrogen, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms;
- R.sup.1 and R.sup.2 taken together are trimethylene, tetramethylene or pentamethylene;
- R.sup.3 is hydrogen, halo, alkyl of 1 to 4 carbon atoms or alkoxy of 1 to 4 carbon atoms; and
- R.sup.5 is alkyl of 1 to 4 carbon atoms.
- 2. A compound according to claim 1 wherein
- R.sup.1 when taken independently of R.sup.2 is chloro, bromo, fluoro, nitro, methyl or an aromatic substituent selected from the group consisting of phenoxy, benzyloxy and phenylthio which aromatic substituent is unsubstituted or substitued with halo;
- R.sup.2 when taken independently of R.sup.1 is hydrogen, methyl or methoxy;
- R.sup.1 and R.sup.2 taken together are trimethylene, tetramethylene or pentamethylene; and
- R.sup.3 is hydrogen, halo, methyl or methoxy.
- 3. A compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is of the formula: ##STR49##
- 4. A compound according to claim 3 wherein R.sup.5 is methyl.
- 5. A compound according to claim 4 wherein
- R.sup.1 taken independently of R.sup.2 is chloro, nitro, methyl, methoxy, ethoxy, butoxy, phenoxy, benzyloxy, phenylthio or chlorophenylthio;
- R.sup.2 is hydrogen or methoxy; and
- R.sup.3 is hydrogen or methyl.
- 6. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-methylpiperid-4-ylmethyl)-6-phenoxy-1,2-benzisothiazolin-3-one.
- 7. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-methylpiperid-4-ylmethyl-6-phenylthio-1,2-benzisothiazolin-3-one.
- 8. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-methylpiperid-4-ylmethyl)-5,6-tetramethylene-1,2-benzisothiazolin-3-one.
- 9. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-methylpiperid-3-yl)-6-chloro-1,2-benzisothiazolin-3-one.
- 10. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-isopropylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolin-3-one.
- 11. The compound according to claim 1 wherein said 6-substituted 7-unsubstituted 1,2-benzisothiazolidin-3-one is 2-(1-methylpiperid-4-ylmethyl)-6-chloro-1,2-benzisothiazolidin-3-one.
- 12. The hydrochloride salt of the compound according to claim 11.
- 13. A compound according to claim 1 which is a salt of said 1,2-benzoisothiazolin-3-one with an acid selected from the group consisting of oxalic acid, 1,5-naphthalenedisulfonic acid, hydrochloric acid, hydrobromic acid, phosphoric acid, sulfuric acid, methanesulphonic acid, acetic acid, tartaric acid, lactic acid, succinic acid, citric acid, malic acid, maleic acid, sorbic acid, aconitic acid, salicyclic acid, phthalic acid, embonic acid, and enanthic acid.
- 14. An antithrombotic pharmaceutical composition comprising an antithrombotically effective amount of a compound according to claim 1 in combination with a pharmaceutically acceptable carrier.
- 15. The method of achieving an antithrombotic effect in a human or other warm blooded animal in need thereof which comprises administering thereto an antithrombotically effective amount of a compound according to claim 1.
Priority Claims (1)
Number |
Date |
Country |
Kind |
2602643 |
Jan 1976 |
DEX |
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CROSS REFERENCE
This is a division of Ser. No. 760,555 filed Jan. 19, 1977, now U.S. Pat. No. 4,156,729.
US Referenced Citations (4)
Non-Patent Literature Citations (1)
Entry |
Fischer, R. et al., Arzneimittel Forsch, 14 (12), pp. 1301-1306 (1964). |
Divisions (1)
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Number |
Date |
Country |
Parent |
760555 |
Jan 1977 |
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