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Last Updated: September 18, 2021

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Claims for Patent: 4,263,293

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Summary for Patent: 4,263,293
Title: Heterocyclic containing amides as inhibitors of mammalian collagenase
Abstract:Mammalian collagenase is inhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl; R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl; R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; and n is an integer of 1 to 20.
Inventor(s): Sundeen; Joseph E. (Yardley, PA), Dejneka; Tamara (Skillman, NJ)
Assignee: E. R. Squibb & Sons, Inc. (Princeton, NJ)
Application Number:06/154,748
Patent Claims:1. A compound having the formula ##STR14## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;

R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;

R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; and

n is an integer of 1 to 20.

2. A compound in accordance with claim 1 wherein R.sub.3 is 2-methylpropyl.

3. A compound in accordance with claim 1 wherein R.sub.1 is hydrogen, acetyl or benzoyl.

4. A compound in accordance with claim 1 wherein n is an integer of 2, 3 or 4.

5. The compound in accordance with claim 1 (.+-.)-2-[(acetylthio)methyl]-4-methyl-N-[2-(4-morpholinyl)ethyl]pentanami de.

6. The compound in accordance with claim 1 (.+-.)-2-[(acetylthio)methyl]-4-methyl-N-[2-(1-piperidinyl)ethyl]pentanami de.

7. The compound in accordance with claim 1 2-(mercaptomethyl)-4-methyl-N-[2-(4-morpholinyl)ethyl]pentanamide.

8. The compound in accordance with claim 1 2-(mercaptomethyl)-4-methyl-N-[2-(1-piperidinyl)ethyl]pentanamide.

9. A method for reducing the adverse effects of mammalian collagenase in a mammal host in need thereof, which comprises administering to said mammal an effective amount of a compound having the formula ##STR15## wherein R.sub.1 is hydrogen, alkanoyl of 2 to 10 carbon atoms or arylcarbonyl;

R.sub.2 is 1-pyrrolidinyl, 1-piperidinyl, 4-morpholinyl, 1-piperazinyl, or 4-alkyl-1-piperazinyl;

R.sub.3 is alkyl of 3 to 8 carbon atoms, cycloalkyl, aryl, or arylalkyl; and

n is an integer of 1 to 20.

10. A method in accordance with claim 9 wherein the mammalian host has rheumatoid arthritis.

Details for Patent 4,263,293

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 ⤷  Free Forever 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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