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US 11,440,904 B2Granted
Substituted pyrimidines, pharmaceutical compositions and therapeutic methods thereof
OwnerZhihong Cheninventor
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Abstract
The invention provide novel pyrimidine derivatives and analogs having inhibitory activities towards certain tyrosine kinases, e.g., Bruton's tyrosine kinase (Btk) and/or Focal adhesion kinase (FAK), extracellular signal-regulated kinase (ERK), pharmaceutical compositions thereof, and methods of treatment, reduction or prevention of certain diseases or conditions mediated by such by tyrosine kinases, e.g., cancers, tumors, fibrosis, inflammatory diseases, autoimmune diseases, diabetes, or immunologically mediated diseases.
Claims8
A compound having the structural formula of (I):
- wherein,
- X is NH(CH2)n, O or S, wherein n is 0 or 1;
- A is a 5- to 7- membered, aliphatic or aromatic, cyclic or heterocyclic moiety;
- R1 is selected from halogen, C1-C6 alkyl, C1-C6 alkoxy, CN, OH, amino, carboxylic amide, sulfonamide and R1x, wherein R1x is selected from:
- each of R2 and R3 is independently selected from the group consisting of:
- H, halogen, C1-C6 alkyl, C1-C6 alkoxy, or R2 and R3 jointly form a 5- to 7-membered, aliphatic or aromatic, cyclic or heterocyclic moiety;
- R4 and R5 jointly form a 12-membered aliphatic heterocyclic moiety,
- or a pharmaceutically acceptable form thereof.
5 more elements
A compound selected from the group consisting of:
Dependencies are inferred from the claim text.