C07F9/650994

2-(PYRAZIN-2-YLCARBONYLAMINOMETHYL) BENZIMIDAZOLIUM COMPOUNDS AS EPITHELIAL SODIUM CHANNEL INHIBITORS
20180002314 · 2018-01-04 ·

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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ANTICANCER COMPOUND AND MEDICAL USE THEREOF
20230026163 · 2023-01-26 ·

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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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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Phenazine derivatives as anti-neoplastic agents and anti-infective agents

Novel phenazine derivatives, methods for their preparation and their medical use, in particular as anti-neoplastic agents and anti-infective agents, are provided. Novel methods for the preparation of iodinin and myxin are also provided.

SALT OF EGFR INHIBITOR, CRYSTAL FORM, AND PREPARATION METHOD THEREFOR

Provided are a salt of an EGFR inhibitor, a crystal form thereof and a preparation method therefor, and an application of the salt and the crystal form in the preparation of a treatment for non-small cell lung cancer. The salt has a structure as shown in formula (II).

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Method for producing optically active 2, 3-bisphosphinopyrazine derivative and method for producing optically active phosphine transition metal complex

In the method for producing an optically active 2,3-bisphosphinopyrazine derivative of the present invention, an optically active 2,3-bisphosphinopyrazine derivative represented by the following formula (3) is produced by the step of: preparing solution A containing 2,3-dihalogenopyrazine represented by the following formula (1) ##STR00001##
and a carboxylic acid amide coordinating solvent, lithiating an optically active R- or S-isomer of a hydrogen-phosphine borane compound represented by the following formula (2) ##STR00002##
to give a lithiated phosphine borane compound; adding solution B containing the lithiated phosphine borane compound to the solution A to perform an aromatic nucleophilic substitution reaction; and then performing a deboranation reaction. ##STR00003## (For symbols in the formulas, see the description.)

MULTI-COORDINATE GOLD-PHOSPHINE COMPOUNDS AND METHOD OF USE
20230357292 · 2023-11-09 ·

The presently-disclosed subject matter includes a multi-coordinate gold-phosphine compound or a pharmaceutically acceptable salt thereof.

Phosphine transition metal complex, method for producing same, and anticancer agent

The phosphine transition metal complex of the present invention is represented by formula (1). ##STR00001##
Preferably, R.sup.1 and R.sup.6 are identical groups, R.sup.2 and R.sup.7 are identical groups, R.sup.3 and R.sup.8 are identical groups, R.sup.4 and R.sup.9 are identical groups, R.sup.5 and R.sup.10 are identical groups, and n and y are identical numbers. The phosphine transition metal complex is suitably obtained by reacting a phosphine derivative represented by formula (2) and a phosphine derivative represented by formula (3) with a salt of a transition metal of gold, copper or silver. ##STR00002##
See the description for the meanings of the symbols in each formula.

PHOSPHINE TRANSITION METAL COMPLEX, METHOD FOR PRODUCING SAME, AND ANTICANCER AGENT

The phosphine transition metal complex of the present invention is represented by formula (1).

##STR00001##

Preferably, R.sup.1 and R.sup.6 are identical groups, R.sup.2 and R.sup.7 are identical groups, R.sup.3 and R.sup.8 are identical groups, R.sup.4 and R.sup.9 are identical groups, R.sup.5 and R.sup.10 are identical groups, and n and y are identical numbers. The phosphine transition metal complex is suitably obtained by reacting a phosphine derivative represented by formula (2) and a phosphine derivative represented by formula (3) with a salt of a transition metal of gold, copper or silver.

##STR00002##

See the description for the meanings of the symbols in each formula.

Process for preparing optically active 2,3-bisphosphino-substituted quinoxalines

There is provided a method for producing a 2,3-bisphosphinopyrazine derivative, the method comprising a first step of adding a base to a liquid comprising: 2,3-dihalogenopyrazine represented by the following general formula (1); a hydrogen-phosphine borane compound represented by the following general formula (2); and a deboranating agent, and allowing the resultant to react to thereby obtain the 2,3-bisphosphinopyrazine derivative represented by the following general formula (3). According to the present invention, a method for producing the industrially advantageous 2,3-bisphosphinopyrazine derivative can be provided. ##STR00001##