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Last Updated: February 24, 2020

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Patent: 4,424,354

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Summary for Patent: 4,424,354
Title: Inhibitors of mammalian collagenase
Abstract:Mammalian collagenase is inhibited by compounds of the formula ##STR1## or salts thereof, wherein R is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl; R.sub.1 is of 3 to 8 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, aryl or arylalkyl; R.sub.2 is hydrogen, ##STR2## R.sub.3 is ##STR3## R.sub.4 is hydrogen, methyl, ethyl, or ##STR4## R.sub.5 and R.sub.6 are each independently selected as --OCH.sub.3 or --OCH.sub.2 CH.sub.3 or are combined as --OCH.sub.2 CH.sub.2 O-- or --O--(CH.sub.2).sub.3 --O--; R.sub.7 and R.sub.8 are each independently selected as hydrogen, methyl or ethyl or are combined as --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 --O--CH.sub.2 CH.sub.2 --; R.sub.9 is hydrogen, methyl, ethyl ##STR5## m is an integer from 0 to 7; p is an integer from 1 to 3; AA.sub.n is an amino acid chain of from one to three amino acids; n is 1 or 1, 2 or 1, 2, 3; when p is 1, AA.sub.n is AA.sub.1 ; when p is 2, AA.sub.n is AA.sub.1 -AA.sub.2 ; when p is 3, AA.sub.n is AA.sub.1 -AA.sub.2 -AA.sub.3 ; AA.sub.1 is glycine or alanine; AA.sub.2 is glycine or alanine; AA.sub.3 is leucine, glutamine or isoleucine. A method of reducing the adverse effects of mammalian collagenase in a mammalian host in need thereof, which comprises administering to the mammal an effective amount of a compound having the above formula is within the scope of the invention.
Inventor(s): Sundeen; Joseph E. (Yardley, PA), Dejneka; Tamara (Skillman, NJ)
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:06/424,735
Patent Claims:see list of patent claims

Details for Patent 4,424,354

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 E. R. Squibb & Sons, Inc. (Princeton, NJ) 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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