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US 7,598,253 B2Granted
Reverse-turn mimetics and methods relating thereto
AssigneeMyriad Genetics, Inc.
InventorsMichael Kahn, Masakatsu Eguchi, Hwa-Ok Kim, Marcin Stasiak
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Abstract
Conformationally constrained compounds which mimic the secondary structure of reverse-turn regions of biologically active peptides and proteins are disclosed. Such reverse-turn mimetics have utility in the treatment of cell adhesion-indicated diseases, such as multiple sclerosis, atherosclerosis, asthma and inflammatory bowel disease.
Claims23
A method for treating a cell adhesion-mediated disease comprising administering to a warm-blooded animal in need thereof a composition comprising a therapeutically effective amount of a compound having the structure:
- wherein
- Y is selected from —CH(R5)—A—N(R1)—, —A—N(R1)—CH(R′)—, —A—N(R1)—C(═O)—, —A—C(═O)—N(R1)—, —A—CH(R1)—O— and —A—CH(R1)—N(R′)—;
- A is —(CHR′)n—, where n=0, 1 or 2;
- B is —(CHR″)m—, where m=1, 2 or 3;
- R′, R″, R2, R3 and R5 are the same or different and independently selected from an amino acid side chain moiety or an amino acid side chain derivative;
- and
- R1 and R4 are the same or different and independently selected from an amino acid, and amino acid side chain moiety, an amino acid side chain derivative, a peptide, a peptide derivative, or a protein;
- and
- wherein any two adjacent CH groups or adjacent NH and CH groups on the fused bicyclic ring may optionally form a double bond;
- in combination with a pharmaceutically acceptable carrier or diluent.
7 more elements
Dependencies are inferred from the claim text.