US 2009/0156509 A1 · Tri-peptide Inhibitors of Serine Elastases

Abstract

The present invention provides compounds of formula (I): where X is R1—(CR3R4)nOC(O)—; R1—(CR3R4)nC(O)—; R1—C(O)NH(CR3R4)nOC(O)—; R1—C(O)NH(CR3R4)nC(O)—; R1—C(O)(CR3R4)nOC(O)—; or R1—C(O)(CR3R4)nC(O)—; where R1 is optionally substituted C5-10 aryl or heteroaryl; OH or NH2; where R3 and R4 are independently H or methyl; and n is 0 to 6; and Y is —CF3 or one of: where R2 is C1-8 alkyl optionally substituted with halo or —OH; —(CR6R7)p—C5-6 aryl optionally substituted with halo, —OH, C1-8 alkyl, C1-8 haloalkyl, —(CH2)mC(O)NH2 or —(CH2)mOCH3; where R6 and R7 are independently H or methyl; m is 0 to 4, and p is 0 or 1 or a pharmaceutically acceptable salt, ester, metabolite or prodrug thereof

Claims17

Dependent claims

A compound of the formula (I):

where X is R1—(CR3R4)nOC(O)—;
R1—(CR3R4)nC(O)—;
R1—C(O)NH(CR3R4)nOC(O);
R1—C(O)NH(CR3R4)nC(O)—;
R1—C(O)(CR3R4)nOC(O)—;
or R1—C(O)(CR3R4)nC(O);
where R1 is optionally substituted C5-10 aryl or heteroaryl;
OH or NH2;
where R3 and R4 are independently H or methyl;
and
n is 0 to 6;
and
Y is —CF3 or one of
where R2 is C1-8 alkyl optionally substituted with halo or —OH;
or —(CR6R7)p—C5-6 aryl optionally substituted with halo, —OH, C1-8 alkyl, C1-8 haloalkyl, —(CH2)mC(O)NH2 or —(CH2)mOCH3;
where R6 and R7 are independently H or methyl;
m is 0 to 4, and p is 0 or 1 or a pharmaceutically acceptable salt, ester, metabolite or prodrug thereof.

14 more elements

Dependencies are inferred from the claim text.

Tri-peptide Inhibitors of Serine Elastases

Life of this patent

Tri-peptide Inhibitors of Serine Elastases

Life of this patent

Abstract

Claims17