Reverse-turn mimetics and methods relating thereto
AssigneeMolecumetics, Ltd.
InventorsMarcin Stasiak, Michael Kahn
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Abstract
Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins having the following structure are disclosed: wherein A, R1, R2, R2a, R3, R3a and R4 are as defined herein. Such compounds have utility over a wide range of fields, including use as diagnostic and therapeutic agents. In particular, compounds of this invention are useful in pharmaceutical compositions as anti-inflammatory agents. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
Claims18
A method for treating an inflammatory or cell adhesion-mediated disease comprising administering to a warm-blooded animal in need thereof an effective amount of a composition comprising a compound having the structure:
- or a pharmaceutically acceptable salts or stereoisomers thereof, wherein
- A is —(CR5R5a)n— where n is 1, 2 or 3;
- R2, R3 and R5 are, at each occurrence, the same or different and independently an amino acid side chain moiety or amino acid side chain derivative, a peptide or peptide derivative, a linker or a solid support;
- R2a, R3a and R5a are, at each occurrence, the same or different and independently hydrogen, hydroxy, —COOH, —CONH2, —R6, —OR6, —COOR6, —COR6 or —CONHR6, where R6 is lower alkyl optionally substituted with halogen or hydroxy;
- and
- R1 and R4 represent the remainder of the molecule, with the proviso that when R1 is —C(═O)OMe and R4 is benzyl, R2 is not isopropyl when R3 is methyl and R2 is not methyl when R3 is isopropyl
- and a pharmaceutically acceptable carrier.
Dependencies are inferred from the claim text.