Provided is a 2,3-bisphosphinopyrazine derivative represented by the following general formula (1), wherein R.sup.1, R.sup.2, R.sup.3, and R.sup.4 represent an optionally substituted straight-chain or branched alkyl group having 1 to 10 carbon atoms, an optionally substituted cycloalkyl group, an optionally substituted adamantyl group, or an optionally substituted phenyl group, R.sup.5 represents an optionally substituted alkyl group having 1 to 10 carbon atoms or an optionally substituted phenyl group, each R.sup.5 may be the same group or a different group, R.sup.6 represents a monovalent substituent, n denotes an integer of 0 to

##STR00001##

An optically active 2,3-bisphosphinopyrazine derivative represented by the following general formula (1):

##STR00001##

wherein R.sup.1 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, an optionally substituted cycloalkyl group, and an optionally substituted aryl group; R.sup.2 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, and an optionally substituted cycloalkyl group, provided that when R.sup.1 is a tert-butyl group, R.sup.1 and R.sup.2 are not the same; R.sup.3 represents a monovalent substituent; n represents an integer of 0 to 4; and * represents an asymmetric center on a phosphorus atom.

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##

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.)

The present invention relates to defined quinoxalin-2-one compounds or a pharmaceutically acceptable salt or a hydrate or a solvate thereof. The compounds, salts or hydrates have a glucocorticoid receptor agonist activity, and are useful as a medicine, in particular as a prophylactic or therapeutic agent for a glucocorticoid receptor related disease.

The present invention relates to defined quinoxalin-2-one compounds or a pharmaceutically acceptable salt or a hydrate or a solvate thereof. The compounds, salts or hydrates have a glucocorticoid receptor agonist activity, and are useful as a medicine, in particular as a prophylactic or therapeutic agent for a glucocorticoid receptor related disease.

The present invention relates to defined quinoxalin-2-one compounds or a pharmaceutically acceptable salt or a hydrate or a solvate thereof. The compounds, salts or hydrates have a glucocorticoid receptor agonist activity, and are useful as a medicine, in particular as a prophylactic or therapeutic agent for a glucocorticoid receptor related disease.

The present invention is directed to a process for making Tetracyclic Heterocycle Compounds of Formula (I): ##STR00001##
and pharmaceutically acceptable salts thereof, wherein X.sup.1, X.sup.2, R.sup.1, R.sup.2 and R.sup.3 are defined above herein. The present invention is also directed to compounds that may be useful as synthetic intermediates in the process of the invention.

The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is useful as a medicine, in particular as a prophylactic or therapeutic agent for the glucocorticoid receptor related disease.

The present invention relates to a novel [4-(1,3,3-trimethyl-2-oxo-3,4-dihydro-1H-quinoxalin-7-yl)phenoxy]ethyloxy compound or a salt thereof. The compound or a salt thereof of the present invention has a glucocorticoid receptor agonist activity, and is useful as a medicine, in particular as a prophylactic or therapeutic agent for the glucocorticoid receptor related disease.