Abstract: Quinoxaline compounds of the general formula ##STR1## wherein R.sup.1 is COX', POX'X" or alkyl substituted with COX' or POX'X", and X' and X" independently are hydroxy or alkoxy, and R.sup.6, R.sup.7, R.sup.8 and R.sup.9 independently are hydrogen, alkyl, halogen, NH.sub.2, NO.sub.2, CN, CF.sub.3, SO.sub.2 NY'Y" or COZ' wherein Z' is NY'Y" or alkyl and Y' and Y" independently are hydrogen or alkyl, triazolyl, imidazolyl, imidazolyl substituted with phenyl or alkyl, or R.sup.6 and R.sup.7, or R.sup.8 and R.sup.9, together form a further fused ring, are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: The present invention relates to [1,2,4]triazolo[4,3-a quinoxaline derivatives of formula I ##STR1## wherein one of R.sup.1 and R.sup.2 is a 5- or 6-membered nitrogen-containing heterocyclic ring which is optionally substituted with one, two or three substituents, wherein each substituent is independently phenyl or C.sub.1-6 -alkyl, or one of R.sup.1 and R.sup.2 is a fused ring system comprising a 5- or 6-membered nitrogen-containing heterocyclic ring and a benzene, pyridine, pyrimidine or pyrazine ring, wherein the fused ring system is optionally substituted with phenyl or C.sub.1-6 -alkyl; and the other of R.sup.1 and R.sup.2 is hydrogen, C.sub.1-6 -alkyl, C.sub.1-6 -alkoxy, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, COC.sub.1-6 -alkyl or SO.sub.2 NR'R", wherein R' and R" are independently hydrogen or C.sub.1-6 -alkyl; and X is O or S; and pharmaceutically acceptable salts thereof.

Abstract: Quinoxaline compounds represented by formulas I or II, ##STR1## wherein R.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 -alkyl, halogen, NO.sub.2, NH.sub.2, CN, CF.sub.3, SO.sub.2 NR.sup.4 R.sup.5 wherein R.sup.4 and R.sup.5 are independently hydrogen or C.sub.1-6 -alkyl, or COR.sup.6 wherein R.sup.6 is C.sub.1-6 -alkyl; and R.sup.3 is hydrogen, C.sub.1-6 -alkyl or CF.sub.3, compositions thereof and methods of preparing the compounds are described.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Novel [1]benzothieno[2,3-b]pyrazine-2,3(1H,4H)-diones or tautomeric forms thereof of the general formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, halogen, alkyl, alkoxy or trifluoromethyl.The compounds are useful for treating a central nervous system ailment associated with the NMDA receptor-associated glycine site.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy; andR.sup.5 and R.sup.6 together form a fused phenyl, cyclohexyl or pyridyl ring, which is optionally substituted with halogen or CN; and R.sup.7 and R.sup.8 independently are hydrogen, hydroxy, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.5 and R.sup.6 independently are hydroxy, hydrogen, NO.sub.2, halogen, CN, CF.sub.3, C.sub.1-4 -alkoxy, acetyl, SO.sub.2 NHCOCO.sub.2 Et, SO.sub.2 NR'R' or SO.sub.2 R', wherein R' is hydrogen or C.sub.1-4 -alkyl; and R.sup.7 and R.sup.8 together form a fused phenyl, cyclohexyl or pyridyl ring which is optionally substituted with halogen or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ;--X--Y--Z-- is selected from .dbd.N-Se--N.dbd., .dbd.N--O--N.cuberoot., .dbd.N--S--N.dbd.;wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy;R.sup.5 and R.sup.6 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl; orR.sup.7 and R.sup.8 together form a further fused ring, which is substituted with hydrogen, halogen or CN, and R.sup.5 and r.sup.6 independently are hydrogen, NO.sub.2, halogen, CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ; --X--Y--Z-- is selected from --N.dbd.CR.sup.3 --CR.sup.3 .dbd.N--, --NH--CR.sup.3 .dbd.CR.sup.3 --CR.sup.3 .dbd.N--, wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ;--X--Y--Z-- is selected from --S--CR.sup.3 .dbd.N--, --N.dbd.CR.sup.3 --S--wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is hydroxy, alkoxy, aryloxy, aralkyloxy, cycloalkylalkoxy, cycloalkoxy, or acyloxy; andR.sup.5, R.sup.6, R.sup.7 and R.sup.8 independently are hydrogen, NO.sub.2, halogen CN, SO.sub.2 NR'R', SO.sub.2 R', CF.sub.3, or OR', wherein R' is hydrogen or C.sub.1-4 -alkyl;The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ;--X--Y--Z-- is selected from --NR.sup.3 --N=CR.sup.3 -- and --CR.sup.3 =N--NR.sup.3 --,wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substututed by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, Cl or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 - alkyl; orR.sup.7 and R.sup.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ; --X--Y--Z-- is selected from --N.dbd.N--N.sup.3 --,--NR.sup.3 --N.dbd.N--,.dbd.N--NR.sup.3 --N.dbd., wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is C.sub.1-12 -alkyl, which may optionally be substituted by hydroxy, formyl, carboxy, carboxylic esters, amides or amines, C.sub.3-8 -cycloalkyl, aryl, aralkyl; and wherein R.sup.6 is, hydrogen, halogen, CN, CF.sub.3, NO.sub.2, or OR', wherein R' is C.sub.1-4 -alkyl and R.sup.5, R.sup.7 and R.sup.8 is hydrogen, provided R.sup.6 is not CF.sub.3, OCH.sub.3, NO.sub.2, C.sup.1 or Br when R.sup.1 is CH.sub.3 ; orR.sup.6 and R.sup.7 independently are NO.sub.2, halogen, CN, CF.sub.3, or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.5 and R.sup.8 are each hydrogen; orR.sup.5 and R.sup.6 together form a further fused aromatic ring, which may be substituted with halogen, NO.sub.2, CN, CF.sub.3 or OR', wherein R' is C.sub.1-4 -alkyl, and R.sup.7 and R.sup.8 independently are hydrogen, halogen, CN, CF.sub.3, NO.sub.2 or OR', wherein R' is C.sub.1-4 -alkyl; orR.sup.7 and R.sup.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR2## R.sup.1, R.sup.2 and R.sup.3 are independently H, halogen, CN, NH.sub.2, NO.sub.2, SO.sub.3 H, SO.sub.2 NH.sub.2, or CONH.sub.2The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein --A-- together with the two carbon atoms denoted as 1 and 2 is selected from ##STR2## R.sup.1, R.sup.2 and R.sup.3 are independently H, halogen, CN, NH.sub.2, NO.sub.2, SO.sub.3 H, SO.sub.2 NH.sub.2, or CONH.sub.2The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.

Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.1 is halogen, CN, CF.sub.3, ethynyl, or N.sub.3 andR.sup.2 is SO.sub.2 C.sub.1-3 -alkyl, CF.sub.3, NO.sub.2, ethynyl, or CN.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters, particularly the quisqualate receptors, and especially as neuroleptics.