C07D473/32

PURINONE COMPOUNDS AND THEIR USE IN TREATING CANCER

The specification generally relates to compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, where R, A.sup.1, A.sup.2 and A.sup.3 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

##STR00001##

PURINONE COMPOUNDS AND THEIR USE IN TREATING CANCER

The specification generally relates to compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, where R, A.sup.1, A.sup.2 and A.sup.3 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

##STR00001##

Carbocyclic nucleoside reverse transcriptase inhibitors

The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I ##STR00001##
and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

Carbocyclic nucleoside reverse transcriptase inhibitors

The present invention is directed carbocyclic nucleoside reverse transcriptase inhibitors compounds of Formula I ##STR00001##
and their use in the inhibition of HIV reverse transcriptase, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS and/or ARC.

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
20210163423 · 2021-06-03 ·

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

CERTAIN CHEMICAL ENTITIES, COMPOSITIONS, AND METHODS
20210163423 · 2021-06-03 ·

Chemical entities that are kinase inhibitors, pharmaceutical compositions and methods of treatment of cancer are described.

SUBSTITUTED AMINOPURINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are Aminopurine Compounds having the following structures:

##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

SUBSTITUTED AMINOPURINE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH

Provided herein are Aminopurine Compounds having the following structures:

##STR00001## wherein R.sup.1, R.sup.2, and R.sup.3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound, and methods for treating or preventing a cancer, for example, melanoma.

METHOD FOR SYNTHESIZING DIVERSELY SUBSTITUTED PURINES

The present invention relates to a method for synthesizing diversely substituted purines starting from a pyrimidine. Formula (I). The method comprises the formation of an amidine group on the pyrimidine by implementing a Vilsmeier type reagent, the functionalization of the pyrimidine with an amine and the cyclization to form the purine nucleus. Optional steps can also be performed in order to further functionalize the molecule. The invention also relates to new purines and new intermediate product.

##STR00001##

HETEROCYCLIC COMPOUNDS AND USES AS ANTICANCER AGENTS
20210100802 · 2021-04-08 · ·

The present disclosure provides pharmaceutical compounds, compositions and methods, especially as they are related to compositions and methods for the treatment of tumors and related diseases related to the dysregulation of kinase (such as EGFR (including HER), Alk, PDGFR, but not limited to) pathways.