Claims for Patent: 4,235,885

Summary for Patent: 4,235,885

Title:	Inhibitors of mammalian collagenase
Abstract:	Mammalian collagenase is inhibited by compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is hydrogen or alkanoyl of 2 to 10 carbon atoms; R.sub.2 is hydroxy, amino, or ##STR2## R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR3## R.sub.4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; and m is 0 or an integer of 1 to 9.
Inventor(s):	Sundeen; Joseph E. (Yardley, PA), Dejneka; Tamara (Skillman, NJ)
Assignee:	E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:	06/051,915
Patent Claims:	1. A method for reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR29## or a salt thereof wherein R.sub.1 is hydrogen or alkanoyl of 2 to 10 carbon atoms; R.sub.2 is hydroxy, amino or ##STR30## R.sub.3 is hydrogen, alkyl of 1 to 4 carbon atoms, ##STR31## R.sub.4 is hydroxy, amino, arginine, leucine, glutamine, alanine or glycine; and m is 0 or an integer of 1 to 9. 2. A method in accordance with claim 1 wherein the mammalian host has rheumatoid arthritis. 3. A method in accordance with claim 1 wherein R.sub.1 is hydrogen. 4. A method in accordance with claim 1 wherein R.sub.1 is alkanoyl of 2 to 10 carbon atoms. 5. A method in accordance with claim 3 wherein R.sub.2 is hydroxy. 6. A method in accordance with claim 3 wherein R.sub.2 is amino. 7. A method in accordance with claim 3 wherein R.sub.2 is ##STR32## 8. A method in accordance with claim 7 wherein m is 0. 9. A method in accordance with claim 7 wherein m is an integer of 1 to 9. 10. A method in accordance with claim 7 wherein R.sub.3 is hydrogen. 11. A method in accordance with claim 7 wherein R.sub.3 is alkyl of 1 to 4 carbon atoms. 12. A method in accordance with claim 7 wherein R.sub.3 is ##STR33## 13. A method in accordance with claim 7 wherein R.sub.3 is ##STR34## 14. A method in accordance with claim 3 wherein R.sub.4 is hydroxy. 15. A method in accordance with claim 3 wherein R.sub.4 is amino. 16. A method in accordance with claim 3 wherein R.sub.4 is arginine, leucine, glutamine, alanine or glycine. 17. A method in accordance with claim 3 wherein the compound administered is 2-(mercaptomethyl)-4-methylpentanoic acid, ammonium salt. 18. A method in accordance with claim 3 wherein the compound administered is 2-(mercaptomethyl)-4-methylpentanamide. 19. A method in accordance with claim 3 wherein the compound administered is N-[2-(mercaptomethyl)-4-methyl-1-oxopentyl]glycine. 20. A method in accordance with claim 3 wherein the compound administered is N-[6-[2-[(acetylthio)methyl]-4-methyl-1-oxopentyl]-1-oxohexyl]-L-argini ne. 21. A method in accordance with claim 3 wherein the compound administered is N-[6-[[2-(mercaptomethyl)]-4-methyl-1-oxopentyl]amino-1-oxohexyl]-L-arg inine. 22. A method in accordance with claim 3 wherein the compound administered is 6-[[2-[(acetylthio)methyl]-4-methyl-1-oxopentyl]amino]hexanamide. 23. A method in accordance with claim 3 wherein the compound administered is N-[N-[2-(mercaptomethyl)-4-methyl-1-oxopentyl]glycyl]-L-arginine. 24. A method in accordance with claim 3 wherein the compound administered is N-[5-[[2-(mercaptomethyl)-4-methyl-1-oxopentyl]amino]-1-oxopentyl]-L-ar ginine. 25. A method in accordance with claim 3 wherein the compound administered is N-[8-[[2-(mercaptomethyl)-4-methyl-1-oxopentyl]amino]-1-oxooctyl]-L-arg inine.

Details for Patent 4,235,885

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