Claims for Patent: 4,367,233

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	Approval Date	Patent No.	Expiredate
Smith & Nephew, Inc.	SANTYL	collagenase	Ointment	101995	06/04/1965		2039-03-29