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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 |
International Patent Family for US Patent 4,424,354
| Country | Patent Number | Estimated Expiration |
|---|---|---|
| United States of America | 4382081 | Start Trial |
| Japan | H0422907 | Start Trial |
| Japan | S57212157 | Start Trial |
| European Patent Office | 0067429 | Start Trial |
| Germany | 3270583 | Start Trial |
| Canada | 1248296 | Start Trial |
| >Country | >Patent Number | >Estimated Expiration |
