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Last Updated: March 31, 2020

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Claims for Patent: 4,367,233

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Summary for Patent: 4,367,233
Title: Inhibitors of mammalian collagenase
Abstract:A method of inhibiting mammalian collagenase by using .alpha.-phenyl-2-(aza)benzothiazolylthioglycolic acids and derivatives thereof, and the pharmaceutically acceptable salts thereof.
Inventor(s): Clark; Donald E. (Norristown, PA), Grant; Norman H. (Wynnewood, PA)
Assignee: American Home Products Corporation (New York, NY)
Application Number:06/307,711
Patent Claims:1. A method of inhibiting collagenase in mammals afflicted with a disease state in which collagen is broken down by collagenase, which comprises administering to such an afflicted mammal an amount sufficient to reverse said collagenase-induced collagen break down of a collagenase inhibitor having the formula: ##STR4## wherein R.sub.1 is hydrogen, halo, nitro, amino, lower alkyl, lower alkoxy, trifluoromethyl or hydroxy; R.sub.2 is fluorine, chlorine, bromine, lower alkyl, lower alkoxy, amino, nitro or trifluoromethyl; R.sub.3 is hydroxy, lower alkoxy, amino, hydroxy(lower)alkylamino, N-(lower)alkanoylamino(lower)alkoxy or N-arylcarbamoyl(lower)alkylthio; and where the dotted lines represent optional double bonds in the 5,6- and 7,8-positions, and the pharmacologically acceptable salts thereof.

2. The method of claim 1, wherein the inhibitor is .alpha.-(2-benzothiazolylthio)benzeneacetic acid.

3. The method of claim 1, wherein the inhibitor is .alpha.-(5-chlorobenzothiazol-2-ylthio)benzeneacetic acid.

4. The method of claim 1, wherein the inhibitor is the sodium salt of .alpha.-(5-chlorobenzothiazol-2-ylthio)benzeneacetic acid.

5. The method of claim 1, wherein the inhibitor is .alpha.-(5-chlorobenzothiazol-2-ylthio)-.alpha.-(p-chlorophenyl)acetic acid.

6. The method of claim 1, wherein the inhibitor is .alpha.-(p-chlorophenyl)-.alpha.-(benzothiazol-2-ylthio)acetic acid.

7. The method of claim 1, wherein the inhibitor is .alpha.-(5-chloro-2-benzothiazolylthio)benzene acetic acid, ethyl ester.

8. The method of claim 1, wherein the inhibitor is .alpha.-(5-chlorobenzothiazol-2-ylthio)-.alpha.-phenylacetamide.

9. The method of claim 1, wherein the inhibitor is .alpha.-[(5-chloro-2-benzothiazolyl)thio]-N-(2-hydroxyethyl)benzeneacetami de.

10. The method of claim 1, wherein the inhibitor is .alpha.-[(5-chloro-2-benzothiazolyl)thio]acetic acid, [2-(acetylamino)ethyl]-ester.

11. The method of claim 1, wherein the inhibitor is .alpha.-[(5-chloro-2-benzothiazolyl)thio]benzeneethanethioc acid S-[2-(2-naphthalenylamino)-2-oxoethyl]ester.

12. The method of claim 1, wherein the inhibitor is .alpha.-phenyl-.alpha.-[(4,5,6,7-tetrahydrobenzothiazol-2-yl)thio]acetic acid.

13. The method of claim 1, wherein the inhibitor is .alpha.-[(6-nitro-2-benzothiazolyl)thio]benzeneacetic acid.

Details for Patent 4,367,233

Applicant Tradename Biologic Ingredient Dosage Form BLA Number Approval Date Patent No. Assignee Estimated Patent Expiration Status Orphan Source
Smith And Nephew SANTYL collagenase OINTMENT;TOPICAL 101995 001 1965-06-04   Start Trial American Home Products Corporation (New York, NY) 2039-03-29 RX search
>Applicant >Tradename >Biologic Ingredient >Dosage Form >BLA >Number >Approval Date >Patent No. >Assignee >Estimated Patent Expiration >Status >Orphan >Source

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