C07D495/14

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is (LQ).sub.mY; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.

##STR00001##

TRICYCLIC HETEROCYCLIC COMPOUNDS AS PHOSPHOINOSITIDE 3-KINASE INHIBITORS

Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N—(C.sub.1-C.sub.10 alkyl) or S; each X is independently CH or N; R.sup.1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R.sup.2 is (LQ).sub.mY; and each R.sup.3 is independently H, C.sub.1-C.sub.10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110δ, and therefore have utility in therapy.

##STR00001##

METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

METHODS TO INDUCE TARGETED PROTEIN DEGRADATION THROUGH BIFUNCTIONAL MOLECULES

The present application provides bifunctional compounds which act as protein degradation inducing moieties. The present application also relates to methods for the targeted degradation of endogenous proteins through the use of the bifunctional compounds that link a cereblon-binding moiety to a ligand that is capable of binding to the targeted protein which can be utilized in the treatment of proliferative disorders. The present application also provides methods for making compounds of the application and intermediates thereof.

Preparation of condensed triazepine derivatives and their use as BET inhibitors

The invention relates to compounds of the formula: ##STR00001##
and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of inflammatory diseases, fibtrotic diseases and neoplastic diseases.

Preparation of condensed triazepine derivatives and their use as BET inhibitors

The invention relates to compounds of the formula: ##STR00001##
and pharmaceutically acceptable salts thereof. These compounds are useful in the treatment of inflammatory diseases, fibtrotic diseases and neoplastic diseases.

ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME
20230234963 · 2023-07-27 ·

The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.

ARYL RECEPTOR MODULATORS AND METHODS OF MAKING AND USING THE SAME
20230234963 · 2023-07-27 ·

The present invention is generally directed towards compounds capable of binding the aryl hydrocarbon receptor and modulating its activity, methods of treating inflammatory conditions such as Crohn's disease using such compounds, and pharmaceutical compositions comprising such compounds. Also provided are methods of increasing levels of IL-22 in a subject and/or decreasing levels of IFN-γ in a subject.

CDK Inhibitors And Their Use As Pharmaceuticals
20230234964 · 2023-07-27 ·

The disclosure is directed to compounds of Formula I

##STR00001##

pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

CDK Inhibitors And Their Use As Pharmaceuticals
20230234964 · 2023-07-27 ·

The disclosure is directed to compounds of Formula I

##STR00001##

pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.