USRE32310EExpiredUtility

Derivatives of A-21978C cyclic peptides

Priority: May 21, 1982Filed: Sep 23, 1985Granted: Dec 16, 1986
Est. expiryMay 21, 2002(expired)· nominal 20-yr term from priority
C12R 2001/045C12R 2001/62A61K 38/00C12N 1/205C07K 7/08
65
PatentIndex Score
50
Cited by
31
References
8
Claims

Abstract

A-21978C cyclic peptide derivatives of the formula ##STR1## wherein R is a substituted benzoyl group of the formula ##STR2## R 2 is C 8 -C 15 alkyl; X is hydrogen, chloro, bromo, iodo, nitro, C 1 -C 3 alkyl, hydroxy, C 1 -C 3 alkoxy, or C 1 -C 3 alkylthio; and R 1 is hydrogen or an amino-protecting group; and the salts thereof, are useful new semisynthetic antibacterial agents or intermediates to such agents.

Claims

exact text as granted — not AI-modified
I claim: 
     
       1. An A-21978C cyclic peptide derivative of the formula: ##STR14## wherein R is a substituted benzoyl group of the formula ##STR15## R 2  is C 8  -C 15  alkyl; X is hydrogen, chloro, bromo, iodo, nitro, C 1  -C 3  alkyl, hydroxy, C 1  -C 3  alkoxy, or C 1  -C 3  alkylthio; and R 1  is hydrogen or an amino-protecting group; and the salts thereof. 
     
     
       2. A compound of claim 1 wherein R 2  is C 10  -C 13  alkyl and salts thereof. 
     
     
       3. A compound of claim 2 wherein R 2  is dodecyl and its salts. 
     
     
       4. A compound of claim 1, 2 or 3 wherein X is hydrogen and the salts thereof. 
     
     
       5. The compound of claim 2 wherein R 2  is p-(n-dodecyl) and X is hydrogen and its salts. 
     
     
       6. A compound of claim 1, 2 or 3 wherein X is selected from chloro, bromo, or iodo, and the salts thereof. 
     
     
       7. A compound of claim 1, 2, 3 or 5 wherein R 1  is an amino-protecting group and the salts thereof. 
     
     
       8. A compound of claim 7 wherein the amino-protecting group is tert-butoxycarbonyl and the salts thereof.

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