Bicyclic compounds as kinase modulators, methods and uses thereof
AssigneeAgency for Science, Technology and Research
InventorVikrant Arun Adsool
Life of this patent
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Abstract
The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds.
Claims20
A method for treating cancer in a patient in need thereof, the method comprising administering to the patient a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof:
- wherein
- R1 and R2 are independently selected from optionally substituted alkyl, optionally substituted alkenyl, and optionally substituted alkynyl;
- X is selected from optionally substituted cycloalkylene, optionally substituted heterocyclylene, optionally substituted arylene, and optionally substituted heteroarylene;
- Y is optionally substituted cycloalkylene;
- and
- Z is selected from optionally substituted —N-heterocyclyl, optionally substituted —NH(heterocyclyl), optionally substituted —NH(cycloalkyl), optionally substituted —NH(aryl), and optionally substituted —NH(heteroaryl);
- wherein at least one of X, Y or Z is an optionally substituted bridged moiety;
- wherein the cancer is selected from thyroid cancer, kidney cancer, colorectal cancer, gastrointestinal cancer, skin cancer, lung cancer, and bladder cancer.
A pharmaceutical composition comprising a compound of formula (I) or a salt, solvate or prodrug thereof:
- wherein
- R1 and R2 are independently selected from optionally substituted alkyl, optionally substituted alkenyl, and optionally substituted alkynyl;
- X is selected from optionally substituted cycloalkylene, optionally substituted heterocyclylene, optionally substituted arylene, and optionally substituted heteroarylene;
- Y is optionally substituted cycloalkylene;
- and
- Z is selected from optionally substituted —N-heterocyclyl, optionally substituted —NH(heterocyclyl), optionally substituted —NH(cycloalkyl), optionally substituted —NH(aryl), and optionally substituted —NH(heteroaryl);
- wherein at least one of X, Y or Z is an optionally substituted bridged moiety;
- together with one or more pharmaceutically acceptable ingredients selected from carriers, binders, surface-active agents, dispersing agents, diluents, disintegrants, sweeteners, thickeners, flavoring agents, coating agents, preservatives, lubricants, time delay agents, anti-oxidants, buffers, bactericides, solutes, and suspending agents.
A method of synthesizing a compound of formula (I) or a pharmaceutically acceptable salt, solvate or prodrug thereof:
- herein
- R1 and R2 are independently selected from optionally substituted alkyl, optionally substituted alkenyl, and optionally substituted alkynyl;
- X is selected from optionally substituted cycloalkylene, optionally substituted heterocyclylene, optionally substituted arylene, and optionally substituted heteroarylene;
- Y is optionally substituted cycloalkylene;
- and
- Z is selected from optionally substituted —N-heterocyclyl, optionally substituted —NH(heterocyclyl), optionally substituted —NH(cycloalkyl), optionally substituted —NH(aryl), and optionally substituted —NH(heteroaryl);
- wherein at least one of X, Y or Z is an optionally substituted bridged moiety;
- the method comprising:
- a) coupling a compound of formula (III)
- with an amine ZH to form the compound of formula (I).
Dependencies are inferred from the claim text.