Patent classifications
C07D407/14
SMALL MOLECULES THAT BIND CYCLIN-DEPENDENT KINASE INHIBITOR 1B (P27KIP1)
Various compounds and pharmaceutically acceptable salts thereof are provided capable of binding cyclin-dependent kinase inhibitor 1B. The compounds can have a structure according to Formula I or Formula II as detailed herein. The compounds can include SJ747, SJ749, SJ755, SJ757. Pharmaceutical formulations containing the compounds or pharmaceutically acceptable salts are also provided along with methods of use thereof. The formulations and methods can be useful for treating cancer. In some aspects, the cancer is associated with a mislocalization of the intrinsically disordered protein p27. In some aspects, the cancer is resistant to an anticancer therapy. The pharmaceutical formulation can therefore include a second active agent and/or can be given in combination with a second active agent such as a cancer therapeutic. In various aspects, methods of promoting reentry into the cell division cycle in a subject in need thereof using compounds and formulations described herein are also provided.
SMALL MOLECULES THAT BIND CYCLIN-DEPENDENT KINASE INHIBITOR 1B (P27KIP1)
Various compounds and pharmaceutically acceptable salts thereof are provided capable of binding cyclin-dependent kinase inhibitor 1B. The compounds can have a structure according to Formula I or Formula II as detailed herein. The compounds can include SJ747, SJ749, SJ755, SJ757. Pharmaceutical formulations containing the compounds or pharmaceutically acceptable salts are also provided along with methods of use thereof. The formulations and methods can be useful for treating cancer. In some aspects, the cancer is associated with a mislocalization of the intrinsically disordered protein p27. In some aspects, the cancer is resistant to an anticancer therapy. The pharmaceutical formulation can therefore include a second active agent and/or can be given in combination with a second active agent such as a cancer therapeutic. In various aspects, methods of promoting reentry into the cell division cycle in a subject in need thereof using compounds and formulations described herein are also provided.
N-CONTAINING CHROMEN-4-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
The present invention provides the compounds having the general formula: (I) wherein R.sup.1 to R.sup.8, and X are as described herein, compositions including the compounds and methods of using the compounds.
##STR00001##
N-CONTAINING CHROMEN-4-ONE DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION
The present invention provides the compounds having the general formula: (I) wherein R.sup.1 to R.sup.8, and X are as described herein, compositions including the compounds and methods of using the compounds.
##STR00001##
HETEROCYCLIC DERIVATIVE AND ORGANIC ELECTROLUMINESCENT DEVICE THEREOF
Provided are a heterocyclic derivative and an organic electroluminescent device thereof, which relates to the field of organic photoelectric materials. The heterocyclic derivative of Formula I has high electron mobility and great hole blocking performance, and thus the organic electroluminescent device prepared by using the heterocyclic derivative as the electron transport region material, especially the hole blocking material, has low drive voltage and high luminous efficiency. The organic electroluminescent device can also include a hole transport region, and the hole transport region, especially the emissive auxiliary layer, contains the triarylamine compound of Formula II. Since the electron transport region and the hole transport region of the device can effectively balance carriers, which reduces the quenching of excitons and improves the recombination probability of carriers, the device shows low drive voltage and high luminous efficiency.
Quaternary lactam compound and pharmaceutical use thereof
A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders. ##STR00001##
Quaternary lactam compound and pharmaceutical use thereof
A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders. ##STR00001##
Matrix metalloproteinase (MMP) inhibitors and methods of use thereof
Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
Matrix metalloproteinase (MMP) inhibitors and methods of use thereof
Hydantoin based compounds useful as inhibitors of matrix metalloproteinases (MMPs), particularly macrophage elastase (MMP-12) are described. Also described are related compositions and methods of using the compounds to inhibit MMP-12 and treat diseases mediated by MMP-12, such as asthma, chronic obstructive pulmonary disease (COPD), emphysema, acute lung injury, idiopathic pulmonary fibrosis (IPF), sarcoidosis, systemic sclerosis, liver fibrosis, nonalcoholic steatohepatitis (NASH), arthritis, cancer, heart disease, inflammatory bowel disease (IBD), acute kidney injury (AKI), chronic kidney disease (CKD), Alport syndrome, and nephritis.
MATERIALS FOR ELECTRONIC DEVICES
The present application concerns compounds for use in electronic devices, processes for preparing the compounds, and electronic devices comprising the compounds.