C07D209/24

ASH1L INHIBITORS AND METHODS OF TREATMENT THEREWITH

Provided herein are small molecules that bind to ASH1L and inhibit ASH1L activity, and methods of use thereof for the treatment of disease, including acute leukemia, solid cancers and other diseases dependent on activity of ASH1L.

PSMA targeted fluorescent agents for image guided surgery

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

PSMA targeted fluorescent agents for image guided surgery

Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

TAK1 kinase inhibitors, compositions, and uses related thereto

The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I, pharmaceutical compositions having a compound of formula I, and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula I to a subject in need thereof.

TAK1 kinase inhibitors, compositions, and uses related thereto

The disclosure relates to TAK1 inhibitors, compositions, and uses related thereto. In certain embodiments, the disclosure relates to compounds of formula I, pharmaceutical compositions having a compound of formula I, and methods of treating or preventing cancer by administering an effective amount of a pharmaceutical composition having a compound of formula I to a subject in need thereof.

METHOD FOR OXYGENATIVE COUPLING OF ALKYNES USING ACID CATALYST

The present disclosure relates to a method for preparing various physiologically active pharmaceutical ingredients, such as a 1,1-diaryl compound and a 1,1-diheteroaryl compound (specifically, a 1,1-diaryl carbonyl compound), in an economical and convenient manner under mild conditions without using an expensive transition metal catalyst by activating an alkyne compound (e.g., an ynamide) using a Brnsted acid as a catalyst to induce a reaction of the activated alkyne compound and a NO bond oxidant to form an adduct intermediate and then inducing a coupling reaction of the adduct intermediate with various nucleophilic organic compounds (e.g., a nucleophilic arene compound).

METHOD FOR OXYGENATIVE COUPLING OF ALKYNES USING ACID CATALYST

The present disclosure relates to a method for preparing various physiologically active pharmaceutical ingredients, such as a 1,1-diaryl compound and a 1,1-diheteroaryl compound (specifically, a 1,1-diaryl carbonyl compound), in an economical and convenient manner under mild conditions without using an expensive transition metal catalyst by activating an alkyne compound (e.g., an ynamide) using a Brnsted acid as a catalyst to induce a reaction of the activated alkyne compound and a NO bond oxidant to form an adduct intermediate and then inducing a coupling reaction of the adduct intermediate with various nucleophilic organic compounds (e.g., a nucleophilic arene compound).

PROCESS FOR PREPARING A CRYSTALLINE FORM OF FLUVASTATIN SODIUM SALT

The present invention refers to an improved process for the preparation of a crystalline form of Fluvastatin sodium salt. Moreover, it is also related to a novel Fluvastatin sodium salt crystalline form and a process for the preparation thereof.

SUBSTITUTED INDOLE MCL-1 INHIBITORS

The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.

SUBSTITUTED INDOLE MCL-1 INHIBITORS

The present application, among other things, provides compounds that are capable of inhibiting the activity of anti-apoptotic Bcl-2 family proteins, for example, myeloid cell leukemia-1 (Mcl-1) protein. The present invention also provides pharmaceutical compositions as well as methods for using provided compounds for treatment of diseases and conditions (e.g., cancer) characterized by the over-expression or dysregulation of Mcl-1 protein. In some embodiments, a provided compound has the structure of formula I. In some embodiments, a provided compound has the structure of formula II.