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US 6,465,484 B1Granted
Angiogenesis inhibitors
AssigneeMerck & Co., Inc.
InventorsMark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
Life of this patent
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Abstract
The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
Claims14
A compound in accordance with formula Ia:
- or a pharmaceutically acceptable salt, hydrate or prodrug thereof,
- wherein
- X is N;
- R1 is C6-10 aryl, C3-10 heterocyclyl, or C5-10 heteroaryl, said aryl, heteroaryl and heterocyclyl being optionally substituted with from one to three members selected from Ra;
- R2 is H, or C1-6 alkyl;
- R3 is H, or C1-10 alkyl;
- R4 C6-10 aryl, said aryl, being optionally substituted with from one to three members selected from Ra;
- R5 is H, or C1-10 alkyl, said alkyl being optionally substituted with from one to three members selected from Ra;
- Ra is H, C1-10 alkyl, halogen, NO2, R, NHC1-6 alkylR9, OR, NR7R8, CN, C6-10 aryl, C5-10 heteroaryl or C3-10 heterocyclyl;
- R is H, C1-6 alkyl or C1-6 alkylR9;
- R9 is C6-10 aryl, C3-10 heterocyclyl, or C5-10 heteroaryl said aryl, heteroaryl and heterocyclyl being optionally substituted with from one to three members selected from Ra;
- and
- R7&R8 are independently H, C1-10 alkyl, C3-6 cycloalkyl, COR, C6-10 aryl, C3-10 heterocyclyl, or C5-10 heteroaryl, said alkyl, aryl, heteroaryl and heterocyclyl being optionally substituted with from one to three members selected from Ra or NR7R8 can be taken together to form a heterocyclic 5-10 membered saturated or unsaturated ring containing, in addition to the nitrogen atom, one to two additional heteroatoms selected from the group consisting of N, O and S.
10 more elements
Dependencies are inferred from the claim text.