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US 8,815,872 B2Granted
Macrocyclics pyrimidines as aurora kinase inhibitors
AssigneeMerck Patent GmbH
InventorsHenry Yu, Lizbeth Celeste De Selm, Xuliang Jiang, Benny C. Askew, Jr., Srinivasa R. Karra, Andreas Goutopoulos
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Abstract
Macrocyclic derivative compounds that inhibit protein kinase enzymes are disclosed along with pharmaceutical compositions comprising these compounds and methods for synthesizing the same. Such compounds have utility in the treatment of proliferative diseases resulting from unregulated and/or disturbed kinase activity such as cancers, psoriasis, viral and bacterial infections, inflammatory and autoimmune diseases.
Claims5
A compound of the Formula I :
- wherein:
- X is F;
- is aryl;
- is cyclopentane, optionally substituted by carboxamide and dihydroxyethyl;
- - - - represents the presence or absence of a double bond;
- L1 is O;
- L2 is CH2;
- L2′, and L3 each independently, is CHOH;
- n is 1;
- p and q, each independently, is 0 or 1;
- or a pharmaceutically acceptable salt, tautomer, enantiomer or racemic mix thereof.
8 more elements
Dependencies are inferred from the claim text.