Reverse-turn mimetics and methods relating thereto
AssigneeMolecumetics, Ltd.
InventorsJan Urban, Hiroshi Nakanishi, Min S. Lee
Life of this patent
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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: 1 wherein A, B, X, R1, and R5 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 as well as inhibitors of central nervous disorders. Libraries containing the compounds of this invention are also disclosed, as well as methods for screening the same to identify biologically active members.
Claims31
A compound having the structure:
- 185
- or pharmaceutically acceptable salt or stereoisomer thereof,
- wherein
- A is —(CR2R2a)m— where m is 1, 2 or 3;
- B is —(CR3R3a)n— where n is 1, 2, 3 or 4;
- X is —N(R4)—, —O—, or —S—;
- R2 and R3 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;
- R5 is an amino acid side chain moiety or amino acid side chain derivative;
- R2a and R3a 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;
- R1 and R4 are the same or different and represent the remainder of the molecule;
- and
- wherein R1 and R2 taken together optionally form a fused heterocycle or substituted heterocycle.
Dependencies are inferred from the claim text.