Patent classifications
C07F9/6509
2-(PYRAZIN-2-YLCARBONYLAMINOMETHYL) BENZIMIDAZOLIUM COMPOUNDS AS EPITHELIAL SODIUM CHANNEL INHIBITORS
The present invention relates to compounds of formula (I) or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, X, and Z.sup.− have one of the meanings as defined in the specification, to the use of compounds of formula (I) as medicaments, to pharmaceutical compositions comprising at least one compound of formula (I), as well as to medicament combinations containing one or more compounds of formula (I). The compounds are ENaC inhibitors useful for the treatment of respiratory diseases and allergic diseases of the airways.
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METHOD FOR PRODUCING SOLID ELECTROLYTE
According to a method for producing a solid electrolyte that contains a lithium atom, a sulfur atom, a phosphorus atom and a halogen atom, including mixing a complexing agent and a solid electrolyte raw material, a solid electrolyte having a high ionic conductivity is provided using a liquid-phase method.
ANTICANCER COMPOUND AND MEDICAL USE THEREOF
A compound of formula (I), or pharmaceutically acceptable salts, solvates, isotopic variants, or isomers thereof, and anticancer medical use are provided.
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Substituted bicyclic compounds
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V): ##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
PYRIDAZINOL COMPOUND, DERIVATIVE THEREOF, PREPARATION METHOD THEREFOR, HERBICIDAL COMPOSITION AND USE THEREOF
The present invention belongs to the technical field of pesticides, and in particular relates to a pyridazinol compound, a derivative thereof, a preparation method therefor, a herbicidal composition and the use thereof. The pyridazinol compound is as represented by general formula I,
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wherein X represents
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and the ring is an unsubstituted or substituted aryl or unsubstituted or substituted heterocyclyl containing a carbon atom at the 1-position; Y represents haloalkyl; and Z represents halogen, cyano, hydroxy, etc. The derivative refers to an agriculturally acceptable derivative of the hydroxyl group at the 4-position of the pyridazine ring in the general formula I, including a salt, an ester, an oxime, a hydroxylamine and an ether derivative, etc. The compound, the derivative thereof and the composition thereof have good herbicidal activity and crop safety.
Reagents Useful for Synthesizing Rhodamine-Labeled Oligonucleotides
The present disclosure provides reagents that can be used to label synthetic oligonucleotides with rhodamine dyes or dye networks that contain rhodamine dyes.
INDOLE DERIVATIVE-CONTAINING INHIBITOR, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
The present invention relates to an indole derivative-containing inhibitor, a preparation method therefor and an application thereof, and in particular, to a compound as represented by general formula (Ia), a preparation method therefor, a pharmaceutical composition comprising the compound, and the use thereof in treating related diseases such as cancer, inflammation, chronic liver disease, diabetes, cardiovascular disease, and AIDS as a kinase inhibitor, especially as a receptor tyrosine kinase inhibitor (TKI), more specifically, as an EGFR or HER2 inhibitor. The compound exhibits good inhibitory activity in EGFR and HER2 20 exon mutations.
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SUBSTITUTED BICYCLIC COMPOUNDS
Disclosed are compounds of Formulas (I), (II), (III), (IV), and (V):
##STR00001##
and/or a salt thereof, wherein R.sub.1 is —OH or —OP(O)(OH).sub.2, and X.sub.1, X.sub.2, X.sub.3, R.sub.2, R.sub.2a, R.sub.a, R.sub.b, and R.sub.c are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P.sub.1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
A CLASS OF PHOSPHINE NITROGEN LIGAND WITH MULTIPLE CHIRAL CENTERS AND ITS SYNTHESIS METHOD AND APPLICATION
The present invention discloses a phosphine nitrogen ligand with multiple chiral centers and its synthesis method and application. The ligand has the axial chirality of a biaryl skeleton and the central chirality of a chiral amine. The chiral ligand is synthesized from commercially available raw materials through a simple five-step reaction, and the resulting diastereomer can be separated by simple column chromatography or recrystallization. The chiral phosphine nitrogen ligand synthesized by the present invention can catalyze the asymmetric three-component coupling reaction of terminal alkynes, aldehydes and amines, and realize the efficient preparation of chiral propargyl amines with high optical activity.
CONDENSED CYCLIC COMPOUND AND AN ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME
A condensed cyclic compound represented by Formula 1 and an organic light-emitting device including the same.
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