Patent classifications
C07D487/14
FUSED TRICYCLIC COMPOUND AND MEDICINAL USE THEREOF
The present invention provides a compound having a PDHK inhibitory activity and useful for the treatment or prophylaxis of diabetes (type 1 diabetes, type 2 diabetes etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract etc.), cardiac failure (acute cardiac failure, chronic cardiac failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral artery disease, intermittent claudication, chronic obstructive pulmonary disease s, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension, Alzheimer disease, vascular dementia, glaucoma, diabetic retinopathy, retinopathy of prematurity, retinal vein occlusion, ischemic optic neuropathy or chronic kidney disease. The present invention relates to a compound of the formula [I-a], or a pharmaceutically acceptable salt thereof:
##STR00001##
wherein each symbol is as defined in the DESCRIPTION.
FUSED TRICYCLIC COMPOUND AND MEDICINAL USE THEREOF
The present invention provides a compound having a PDHK inhibitory activity and useful for the treatment or prophylaxis of diabetes (type 1 diabetes, type 2 diabetes etc.), insulin resistance syndrome, metabolic syndrome, hyperglycemia, hyperlactacidemia, diabetic complications (diabetic neuropathy, diabetic retinopathy, diabetic nephropathy, cataract etc.), cardiac failure (acute cardiac failure, chronic cardiac failure), cardiomyopathy, myocardial ischemia, myocardial infarction, angina pectoris, dyslipidemia, atherosclerosis, peripheral artery disease, intermittent claudication, chronic obstructive pulmonary disease s, brain ischemia, cerebral apoplexy, mitochondrial disease, mitochondrial encephalomyopathy, cancer, pulmonary hypertension, Alzheimer disease, vascular dementia, glaucoma, diabetic retinopathy, retinopathy of prematurity, retinal vein occlusion, ischemic optic neuropathy or chronic kidney disease. The present invention relates to a compound of the formula [I-a], or a pharmaceutically acceptable salt thereof:
##STR00001##
wherein each symbol is as defined in the DESCRIPTION.
ORGANIC COMPOUND, P-TYPE DOPED MATERIAL AND APPLICATION THEREOF
Provided are an organic compound, a P-type doped material and an application thereof. The organic compound has a structure represented by Formula I, and through a molecular structure design, the organic compound has a lowest unoccupied molecular orbital energy level which is close to an anode work function and a highest occupied molecular orbital energy level of a hole transport layer, effectively promoting the generation of holes. The organic compound has a suitable molecular weight, low volatility and high stability, sufficiently satisfying an evaporation preparation process of OLED devices; moreover, the synthesis method is simple and low cost, achieving large-scale application. As an organic electroluminescent material, the organic compound can be used as the P-type doped material, especially suitable for a charge injection layer of organic electroluminescent devices, which can adjust charge balance of devices, effectively improve efficiency and lifetime of devices and reduce drive voltage and energy consumption.
ORGANIC COMPOUND, P-TYPE DOPED MATERIAL AND APPLICATION THEREOF
Provided are an organic compound, a P-type doped material and an application thereof. The organic compound has a structure represented by Formula I, and through a molecular structure design, the organic compound has a lowest unoccupied molecular orbital energy level which is close to an anode work function and a highest occupied molecular orbital energy level of a hole transport layer, effectively promoting the generation of holes. The organic compound has a suitable molecular weight, low volatility and high stability, sufficiently satisfying an evaporation preparation process of OLED devices; moreover, the synthesis method is simple and low cost, achieving large-scale application. As an organic electroluminescent material, the organic compound can be used as the P-type doped material, especially suitable for a charge injection layer of organic electroluminescent devices, which can adjust charge balance of devices, effectively improve efficiency and lifetime of devices and reduce drive voltage and energy consumption.
FUSED AZA-HETEROCYCLIC AMIDE COMPOUND AND USE THEREOF
A compound of formula (I) or a tautomer, a stereoisomer, a solvate, a nitrogen oxide, a prodrug, an isotope derivative or a pharmaceutically acceptable salt thereof exhibit kinase inhibitory activity against a variety of kinases (such as TRK, ALK and ROS1) and mutants thereof, in particular TRK and a mutant form thereof. An in vitro cell inhibitory activity test and an in vivo anti-tumor model test show that the compounds have a strong inhibitory effect on a variety of cells containing TRK mutations and tumors, have a good safety, and have a good clinical value as drugs.
##STR00001##
FUSED AZA-HETEROCYCLIC AMIDE COMPOUND AND USE THEREOF
A compound of formula (I) or a tautomer, a stereoisomer, a solvate, a nitrogen oxide, a prodrug, an isotope derivative or a pharmaceutically acceptable salt thereof exhibit kinase inhibitory activity against a variety of kinases (such as TRK, ALK and ROS1) and mutants thereof, in particular TRK and a mutant form thereof. An in vitro cell inhibitory activity test and an in vivo anti-tumor model test show that the compounds have a strong inhibitory effect on a variety of cells containing TRK mutations and tumors, have a good safety, and have a good clinical value as drugs.
##STR00001##
SELECTIVE CDK4/6 INHIBITOR CANCER THERAPEUTICS
This disclosure describes embodiments of selective and potent CDK 4/6 inhibitors that show advantageous inhibition of cancer growth, even at low concentrations. As described herein, compounds of the present approach comprise substituted pyridinylpiper-azine-pyrrolopyrimidine compounds having a fatty acid moiety. The compounds described herein may be used as pharmaceutical compounds for anti-cancer therapies, and are useful for the treatment, prevention and/or amelioration of cancer. Formula (a)
##STR00001##
SELECTIVE CDK4/6 INHIBITOR CANCER THERAPEUTICS
This disclosure describes embodiments of selective and potent CDK 4/6 inhibitors that show advantageous inhibition of cancer growth, even at low concentrations. As described herein, compounds of the present approach comprise substituted pyridinylpiper-azine-pyrrolopyrimidine compounds having a fatty acid moiety. The compounds described herein may be used as pharmaceutical compounds for anti-cancer therapies, and are useful for the treatment, prevention and/or amelioration of cancer. Formula (a)
##STR00001##
SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS BRUTON'S TYROSINE KINASE MODULATORS
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
##STR00001##
SUBSTITUTED PYRAZOLO[1,5-a]PYRIMIDINES AS BRUTON'S TYROSINE KINASE MODULATORS
The invention is fused heterocyclic compounds of formula (I), and salts thereof, compositions thereof, and methods of use therefor. In particular, disclosed herein are certain fused heterocyclic compounds that can be useful for inhibiting protein kinase, including Bruton's tyrosine kinase (Btk), and for treating disorders mediated thereby.
##STR00001##