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US 6,552,079 B2Granted
Integrin antagonists
AssigneeEli Lilly and Company
InventorsRobert M. Scarborough, Mark Smyth, Ting Su, Matthew J. Fisher, Joseph A. Jakubowski, John J. Masters, Jeffry Bernard Franciskovich
Life of this patent
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Abstract
Novel compounds, their salts and compositions related thereto having activity against mammalian integrins are disclosed. The compounds are useful in vitro or in vivo for preventing or treating thrombotic or restenotic disorders.
Claims23
A compound having the formula:
- wherein:
- Y is selected from the group consisting of —COOH and —COOR4;
- where R4 is selected from the group consisting of C1-10alkyl, C1-8alkylaryl, and aryl-C1-8alkyl;
- A is selected from the group consisting of C0-8alkyl-NR5—CO—C0-8alkyl, C0-8alkyl-CO—NR5—C0-8alkyl, C0-8alkyl-NR5 —CO—C1-8alkyl-NR5 —CO—C0-8alkyl, C0-8alkyl-CO—NR5—C1-8alkyl-NR5—CO—C0-8alkyl, C0-8alkyl-CO—NR5—C0-8alkyl-CO—NR5—C0-8alkyl, C0-8alkyl-CO—C1-8alkyl—CO—NR5—C0-8alkyl, C0-8alkyl-NR5—C0-8alkyl-CO—NR5—C0-8alkyl, C0-8alkyl-O—C0-8alkyl-CO—NR5—C0-8alkyl, and C0-8alkyl-O—C2-8alkyl-O—C0-8alkyl-CO—NR5—C0-8alkyl;
- where R5 are independently selected from the group consisting of H and C1-6alkyl;
- Z is selected from the group consisting of —NH—C(NR9R10)═NR11 and —C(NR9R10)═NR;
- where R9, R10 and R11 are independently selected from the group consisting of H and C1-6alkyl;
- R1 is H;
- R2 is selected from the group consisting of —SOm-aryl and —SOm—C1-10alkyl, where m=2;
- and
- R3 is H;
- and all pharmaceutically-acceptable stereoisomers, salts, hydrates, solvates and prodrug derivatives thereof.
9 more elements
A compound selected from the group consisting of:
A compound selected from the group consisting of:
- or a pharmaceutically acceptable stereoisomer, salt, solvate, hydrate, or prodrug derivative thereof.
Dependencies are inferred from the claim text.