Patent classifications
C07D403/12
Use of N-functionalized alkoxy pyrazole compounds as nitrification inhibitors
The present invention relates to the use of novel nitrification inhibitors of formula (I), which are N-functionalized alkoxy pyrazole compounds. Moreover, the invention relates to the use of compounds of formula (I) as nitrification inhibitors, i.e. for reducing nitrification, as well as agrochemical mixtures and compositions comprising the nitrification inhibitors of formula (I).
Triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors
Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer. ##STR00001##
Triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors
Provided herein are triazacyclododecansulfonamide (“TCD”)-based protein secretion inhibitors, such as inhibitors of Sec61, methods for their preparation, related pharmaceutical compositions, and methods for using the same. For example, provided herein are compounds of Formula (I) and pharmaceutically acceptable salts and compositions including the same. The compounds disclosed herein may be used, for example, in the treatment of diseases including inflammation and/or cancer. ##STR00001##
Method and apparatus for sorting heterogeneous material
A system is provided for the identification and separation of heterogeneous material, the system comprising: a hyperspectral identification system for capturing spectra of material; a computer receiving and analyzing data from the hyperspectral identification system and selecting desired materials from the heterogeneous materials; and an ejection system, whereby the desired materials are ejected from the system.
Method and apparatus for sorting heterogeneous material
A system is provided for the identification and separation of heterogeneous material, the system comprising: a hyperspectral identification system for capturing spectra of material; a computer receiving and analyzing data from the hyperspectral identification system and selecting desired materials from the heterogeneous materials; and an ejection system, whereby the desired materials are ejected from the system.
Inhibitors of LRRK2 kinase
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.
Inhibitors of LRRK2 kinase
Compounds having activity as inhibitors of LRRK2 kinase are provided. The compounds have Structure (I): ##STR00001##
or a pharmaceutically acceptable salt, stereoisomer or prodrug thereof, wherein A, B, R.sup.1a, R.sup.1b, R.sup.2, and L are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of LRRK2 kinase are also provided.
Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application
A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. ##STR00001##
Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application
A nitrogenous heterocyclic compound, a preparation method, an intermediate, a composition, and an application. The present invention provides a nitrogenous heterocyclic compound as represented by formula I, pharmaceutically acceptable salts thereof, enantiomers thereof, diastereoisomers thereof, tautomers thereof, solvates thereof, metabolites thereof, or prodrugs thereof. The compound has high inhibitory activity against ErbB2 tyrosine kinase, has good inhibitory activity against human breast cancer cells BT-474, human gastric cancer cells NCI-N87 and the like with high expression of ErbB2, and in addition has relatively weak inhibitory activity against EGFR kinase, that is, the compound is an EGFR/ErbB2 double target inhibitor that attenuates EGFR kinase inhibitory activity or a small-molecule inhibitor having selectivity for an ErbB2 target. ##STR00001##
Heterocyclic compounds for inhibiting TYK2 activities
The present invention is directed to Compounds 1-8, and their pharmaceutically acceptable salts or prodrugs thereof. Compounds 1-8 are selective binders to TYK2's JH2 and they exhibit significant inhibitory effects on the physiological function of TYK2 and they have excellent in vivo pharmacokinetic properties. Compounds 1-5 and 7 have several deuterium substitutions on methyl to improve pharmacokinetic (PK) properties.