Diflouro pentapeptide derivative anti-inflammatory agents

Details Diflouro pentapeptide derivative anti-inflammatory agents Diflouro pentapeptide derivative anti-inflammatory agents

1994-10-05

1998-06-02

Tsang, Cecilia J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Peptide containing doai

530329, 530330, A61K 3800, C07K 706, C07K 700

Patent

active

057600023

ABSTRACT:
The subject invention involves anti-inflammatory compounds having the following structure: ##STR1## wherein: a) --X is cyclic alkyl, having from 4 to 15 carbon atoms; branched alkyl, having from 6 to 15 carbon atoms; or aryl having from 6 to 15 carbon atoms;
(b) n is an integer from 0 to 2;
(c) --V-- is --OC(O)--, --N(Q)C(O)--, --N(Q)C(S)--, --C(O)--, --SO2-- or --P(O)(OH)--;
(d) --Q is hydrogen; or straight or branched chain alkyl, saturated or unsaturated with 1 or 2 double bonds, having from 1 to 6 carbon atoms; or --Q and --X are covalently linked forming a cyclic moiety which includes the nitrogen to which --Q is bonded and from 5 to 20 carbon atoms;
(e) Z is --O-- or --NH--; when V is --OC(O)--, --Z-- is --NH--;
(f) --R1 is a hydrophobic moiety;
(g) --R2 is a hydrophobic moiety;
(h) --R3 is --(CH2)m--A--NH2 or --(CH2)m--A--B--C(NH2).dbd.NH wherein m is an integer from 1 to about 6, --A--is a covalent bond or p-phenyl or p-cyclohexyl, and --B-- is a covalent bond or --NH--;
(i) --R4 is a hydrophobic moiety;
(j) --R5 is --(CH2)m--A--NH2 or --(CH2)m--A--B--C(NH2).dbd.NH wherein m is an integer from 1 to about 6, --A-- is a covalent bond or p-phenyl or p-cyclohexyl, and --B-- is a covalent bond or --NH--; and
(k) --Y is hydrogen or methyl.
The subject invention also involves pharmaceutical compositions comprising the above compounds, and methods for treating inflammation or pain using such compounds and compositions.

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