Acylated oligopeptide derivatives having cell signal inhibiting activity
AssigneeThe United States of America as represented by the Department of Health and Human Services
InventorsTerrence R. Burke, Jr., Zhu-jun Yao, C. Richter King
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Abstract
The invention relates to an acylated peptide, namely a compound of formula (I), wherein n is 0 to 15, X is oxalyl PTI is the bivalent radical of tyrosine or (preferably) the bivalent radical of phosphotyrosine or a phosphotyrosine mimetic, AA stands for a bivalent radical of a natural or unnatural amino acid, and Y is secondary amino group, or a salt thereof, said compound being useful for the treatment of diseases that respond to inhibition of the interaction of (a) protein(s) comprising (an) SH2 domain(s) and a protein tyrosine kinase or a modified version thereof.
Claims19
A compound of the formula I,
- wherein
- n is 0 to 15,
- X is oxalyl,
- PTI is a bivalent radical of phosphotyrosine or of an amino acid selected from the group consisting of phosphonomethyl-phenylalanine, phosphono-(α-fluoro)methyl-phenylalanine, phosphono-(α,α-difluoro)methyl-phenylalanine, phosphono-(α-hydroxy)methyl-phenylalanine, O-sulfo-tyrosine, phosphonophenylalanine, dicarboxymethoxy-phenylalanine, aspartic acid, glutamic acid, phosphoserine and phosphothreonine, each of which is present in the (D,L)-, D- or L-form;
- AA stands for a bivalent radical of a natural or unnatural amino acid, and
- Y is a secondary amino group,
- or a salt thereof.
A compound of the formula I,
- wherein
- n is 0 to 15,
- X is oxalyl,
- PTI is a bivalent radical of tyrosine or phosphotyrosine, or a bivalent radical of an amino acid selected from the group consisting of phosphonomethyl-phenylalanine, phosphono-(α-fluoro)methyl-phenylalanine, phosphono-(α,α-difluoro)methyl-phenylalanine, phosphono-(α-hydroxy)methyl-phenylalanine, O-sulfo-tyrosine, phosphonophenylalanine, dicarboxymethoxy-phenylalanine, aspartic acid, glutamic acid, phosphoserine and phosphothreonine, each of which is present in the (D,L)-, D- or L-form,
- AA stands for a bivalent radical of a natural or unnatural amino acid, and
- Y is a monosubstituted amino selected from the group consisting of lower alkylamino, octylamino, halonaphthyloxy-lower alkylamino, naphthyloxy-lower alkylamino, phenyl-lower alkylamino, di-phenyl-lower alkylamino, (mono- or di-halo-phenyl)-lower alkylamino, naphthalenyl-lower alkylamino, hydroxy-naphthalenyl-lower alkylamino, phenanthrenyl-lower alkylamino;
- cycloalkylamino;
- and cycloalkyl-lower alkylamino;
- or a salt thereof.
Dependencies are inferred from the claim text.