Methods for solid phase combinatorial synthesis of integrin inhibitors
AssigneeWyeth
InventorsAriamala Gopalsamy, Hui Y. Yang
Life of this patent
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Abstract
Compounds of the formula are useful in the treatment of various disorders including, but not limited to, cancer (tumor metathesis, tumorgenesis/tumor growth), angiogenesis (as in cancer, diabetic retinopathy, rheumatoid arthritis), restenosis (following balloon angioplasty or stent implantation), inflammation (as in rheumatoid arthritis, psoriasis), bone diseases (osteopenia induced by bone metastases, immobilization and glucocortocoid treatment, periodontal disease, hyperparathyroidism and rheumatoid arthritis), and as antiviral agents. Novel method of making compounds of formula I are also provided.
Claims12
A compound having the formula
- R1 and R2 independently are alkyl of 1-8 carbon atoms, alkenyl of 2-8 carbon atoms, alkynyl of 2-8 carbon atoms, cycloalkyl of 3-12 carbon atoms, aryl, aralkyl of 6 to 10 carbon atoms, heterocycloalkyl of 5-10 members consisting of carbon atoms and from 1 to 3 heteroatoms selected from N, S and O;
- R3 is H, alkyl of 1-6 carbon atoms, aralkoxy of 1-6 carbon atoms;
- X is NHCOO, NHCO, NHCONH, NHSO2;
- Y is CH2, NH;
- Z is CH, N, S;
- m is 0-4;
- and
- n is 0-3;
- or pharmaceutical salts thereof.
A combinatorial library comprising a plurality of different compounds, each compound covalently linked to a solid support P, according to the formula:
- R1 and R2 independently are alkyl of 1-8 carbon atoms, alkenyl of 2-8 carbon atoms, alkynyl of 2-8 carbon atoms, cycloalkyl of 3-12 carbon atoms, aryl, aralkyl of 6 to 10 carbon atoms, heterocycloalkyl of 5-10 members consisting of carbon atoms and from 1 to 3 heteroatoms selected from N, S and O;
- R3 is H, alkyl of 1-6 carbon atoms, aralkoxy of 1-6 carbon atoms;
- X is NHCOO, NHCO, NHCONH, NHSO2;
- Y is CH2, NH;
- Z is CH, N, S;
- m is 0-4;
- and n is 0-3;
- or pharmaceutical salts thereof.
Dependencies are inferred from the claim text.