Beta-amino acids
AssigneeWisconsin Alumni Research Foundation
InventorsSamuel H. Gellman, Daniel H. Appella, Hee-Seung Lee, Paul LePlae, Emilie Porter, Xifang Wang, Matthew Woll
Life of this patent
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Abstract
Disclosed are β-amino acid monomers containing cylcoalkyl, cycloalkenyl, and heterocylic substituents which encompass the α and β carbons of the peptide backbone and β-polypeptides made from such monomers. Method of generating combinatorial libraries of polypeptides containing the β-peptide residues and libraries formed thereby are disclosed.
Claims9
A composition comprising a polypeptide comprising the formula:
- wherein Z is selected from the group consisting of:
- and wherein each residue's X and Y combined, together with the carbon atoms to which they are bonded, independently define a substituted or unsubstituted C3-C8 cycloalkyl, cycloalkenyl or heterocyclic ring having one or more nitrogen atoms as the sole heteroatom, the substituents being selected from the group consisting of hydroxy, linear or branched C1-C6-alkyl, alkenyl, alkynyl;
- hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkyloxy, C1-C6-alkyloxy-C1-C6-alkyl, amino, mono- or di-C1-C6-alkylamino, carboxamido, carboxamido C1-C6-alkyl, sulfonamido, sulfonamido-C1-C6-alkyl, urea, cyano, fluoro, thio, C1-C6-alkylthio, mono- or bicyclic aryl, mono- or bicyclic heteraryl having up to 5 heteroatoms selected from N, O, and S;
- mono- or bicyclic aryl-C1-C6-alkyl, and heteroaryl-C1-C6-alkyl;
- or X and Y are independently selected from the group consisting of hydroxy, linear or branched C1-C6-alkyl, alkenyl, alkynyl;
- hydroxy-C1-C6-alkyl, amino-C1-C6-alkyloxy, C1-C6-alkyloxy-C1-C6-alkyl, amino, mono- or di-C1-C6-alkylamino, carboxamido, carboxamido-C1-C6-alkyl, sulfonamido, sulfonamido-C1-C6-alkyl, urea, cyano, fluoro, thio, C1-C6-alkylthio, mono- or bicyclic aryl, mono- or bicyclic heteraryl having up to 5 heteroatoms selected from N, O, and S;
- mono- or bicyclic aryl-C1-C6-alkyl, and heteroaryl-C1-C6-alkyl;
- and
- wherein m is 1, and
- wherein n and p are 1.
A composition comprising a polypeptide comprising the formula:
- wherein Z is a single bond;
- and
- each residue's X and Y combined, together with the carbon atoms to which they are bonded, independently define a substituted C4-C6 cycloalkyl, cycloalkenyl, or heterocyclic ring having one nitrogen atom as the sole hetero atom;
- wherein m is 1, and
- wherein n and p are 1.
A composition comprising a polypeptide comprising the formula
- wherein X and Y combined, together with the carbon atoms to which they are bonded, independently define a substituted C3-C8 cycloalkyl, cycloalkenyl or heterocyclic ring having one or more nitrogen atoms as the sole heteroatom, the substituents being selected from the group consisting of hydroxy, linear or branched C1-C6-alkyl, alkenyl, alkynyl;
- hydroxy-C1-C6-alkyl, amino-C1-C6-alkyl, C1-C6-alkyloxy, C1-C6-alkyloxy-C1-C6-alkyl, amino, mono- or di-C1-C6-alkylamino, carboxamido, carboxamido-C1-C6-alkyl, sulfonamido, sulfonamido-C1-C6-alkyl, urea, cyano, fluoro, thio, C1-C6-alkylthio, mono- or bicyclic aryl, mono- or bicyclic heteraryl having up to 5 heteroatoms selected from N, O, and S;
- mono- or bicyclic aryl-C1-C6-alkyl, and heteroaryl-C1-C6-alkyl;
- and
- n is a positive integer greater than 3.
Dependencies are inferred from the claim text.