Fused pyrimidine-based hydroxamate derivatives
AssigneeAgency for Science, Technology and Research
InventorsHaishan Wang, Dizhong Chen, Chang Kai Soh
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Abstract
The present invention relates to fused pyrimidine-based hydroxamate compounds of formula (I), comprising a hydroxamate group, that are inhibitors of histone deacetylase (HDAC) and kinases. More particularly, the present invention relates to hydroxamate substituted purine or 5H-pyrrolo[3,2-d]pyrimidine derivatives, methods for their preparation, pharmaceutical compositions containing these compounds and uses of these compounds in the treatment of disorders/conditions/diseases involving, relating to or associated with enzymes having histone deacetylase, non-histone deacetylase and kinase activities/functions and/or via unspecified/multi-targeted mechanisms.
Claims13
A compound of Formula (I);
- wherein X, Y and Z are independently selected from N, CHR3 or CR3, wherein at least one of X, Y or Z is N;
- is a single or double bond, as valency allows;
- R1 is selected from the group consisting of optionally substituted amino, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl and optionally substituted heteroaryl;
- R2 is selected from the group consisting of halogen, optionally substituted amino, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted aryl and optionally substituted heteroaryl;
- R3 is selected from the group consisting of hydrogen, optionally substituted alkyl, optionally substituted amino, and optionally substituted heterocycloalkyl;
- R4 is optionally substituted alkyl;
- at least one of R1, R2, R3 or R4 is further independently substituted by an hydroxamate group -L1-R5-L2-R6-L3-CON(Ra)ORb, wherein;
- Ra and Rb are hydrogen;
- L1, L2 and L3 are independently selected from the group consisting of a bond, optionally substituted alkyl, optionally substituted alkenyl and optionally substituted alkynyl;
- R5 and R6 are independently selected from the group consisting of a bond, O, NRc, S(O)n, optionally substituted amide, optionally substituted heterocycloalkyl, optionally substituted aryl and optionally substituted heteroaryl;
- wherein;
- Rc is independently selected from the group consisting of hydrogen or, optionally substituted alkyl;
- and
- n is an integer from 0 to 2;
- or a pharmaceutically acceptable form thereof.
Dependencies are inferred from the claim text.