Patent classifications
C07D413/12
Naphthalene isoxazoline compounds for controlling invertebrate pests
Disclosed are compounds of Formula 1, ##STR00001##
wherein J is ##STR00002##
and R.sup.1a, R.sup.1b, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8, R.sup.14, R.sup.15, R.sup.16, Q and X are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.
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##
AROMATIC SULPHONAMIDES DERIVATIVES THAT INHIBITS PDI A3, THEIR SYNTHESIS AND USE
The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A1 that display antiplatelet, antithrombotic and anticancer activities.
AROMATIC SULPHONAMIDES DERIVATIVES THAT INHIBITS PDI A3, THEIR SYNTHESIS AND USE
The invention relates to a new group of aromatic sulphonamides derivatives of formula (I) and their synthesis and use for modulation of the activity of protein disulfide isomerase (PDI). More particularly, the invention provides small molecule inhibitors of PDI A1 that display antiplatelet, antithrombotic and anticancer activities.
MATRIPTASE 2 INHIBITORS AND USES THEREOF
The present invention provides compounds for inhibiting matriptase 2, or a mutant thereof, and compositions and methods of use thereof.
SMALL MOLECULE MODULATORS OF SIGMA-1 AND SIGMA-2 RECEPTORS AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.
SMALL MOLECULE MODULATORS OF SIGMA-1 AND SIGMA-2 RECEPTORS AND USES THEREOF
This invention is in the field of medicinal chemistry. In particular, the invention relates to anew class of small-molecules having a tetrahydroindazole structure which function as modulators (e.g., activators or inhibitors) of sigma-1 and/or sigma-2 receptors, and their use as therapeutics for the treatment of cancer and other diseases (e.g., neurological conditions) characterized with sigma-1 and/or sigma-2 receptor activity.
N-(1,3,4-OXADIAZOL-2-YL)ARYLCARBOXAMIDES OR SALTS THEREOF, PREPARATION METHODS, HERBICIDAL COMPOSITIONS AND USES THEREOF
The invention belongs to the technical field of agricultural chemicals, and particularly relates to an N-(1,3,4-oxadiazol-2-yl)arylcarboxamide compound or a salt thereof, a preparation method, a herbicidal composition and a use thereof. The compound is as shown in the following Formula I:
##STR00001## wherein X represents O, S, SO, SO.sub.2 or NR.sub.1; Y represents halogen, cyano, cyanoalkyl, carboxyl, nitro, etc.; or —X—Y represents unsubstituted or substituted five- or six-membered heterocyclyl or heteroaryl; Z represents hydrogen, halogen, cyano, OR.sub.4, -alkyl-OR.sub.4, —O-alkyl-N(R.sub.5).sub.2, etc., M represents hydrogen, OR.sub.6, SR.sub.6, COR.sub.6, COOR.sub.6, CON(R.sub.7).sub.2, etc. The compound has advantages of a low dosage for use, excellent herbicidal activity, and higher crop safety, especially good selectivity for key crops such as rice.