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    2,3 (1H,4H)-quinoxalinediones
    77.
    发明专利
    2,3 (1H,4H)-quinoxalinediones 未知

    公开(公告)号：AU3988793A

    公开(公告)日：1993-12-02

    申请号：AU3988793

    申请日：1993-05-28

    Applicant: BASF AG

    Inventor： LUBISCH WILFRED ,  BEHL BERTHOLD ,  HOFMANN HANS PETER

    IPC: A61K31/495 ,  A61K31/498 ,  A61P25/00 ,  A61P25/08 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/26 ,  C07D241/44 ,  C07D241/52 ,  C07D401/04 ,  C07D403/04 ,  C07D487/12 ,  C07D487/14 ,  C07D403/10

    Abstract: Quinoxaline-2,3-(1H,4H)diones of the general formula I in which the variables have the following meaning: R is hydrogen; an aliphatic radical having up to 12 C atoms, which can carry one of the following substituents: phenyl, cyclopentyl, cyclohexyl or a group -CO-R , -CO-O-R or -CO-NH-R , where R denotes hydrogen, C1-C4-alkyl, phenyl, benzyl or 1-phenylethyl; a cycloaliphatic radical having up to 12 C atoms, or a phenyl group, where the cyclic groups contained in R can carry up to three of the following substituents: C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, halogen, nitro, cyano, -CO-O-R and -CO-NH-R ; R is a pyrrol-1-yl group which can carry up to two of the following substituents: C1-C4-alkyl, phenyl, phenylsulphonyl, nitro, cyano and one of the groups -CO-O-R , -CO-NH-R , -CH2-O-R , -O-R and -CH=NO-R ; R is identical or different radicals from the following: C1-C4-alkyl, C1-C4-alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and one of the groups -CO-O-R and -CO-NH-R and a fused benzene ring; n is 0 to 3. Quinoxaline-2,3-(1H,4H)diones I' in which R has the meaning mentioned. The compounds I and I' are suitable as medicines for human and veterinary medicine.

    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION
    79.
    发明专利
    3-SUBSTITUTED PYRIDO[4', 3': 4,5]THIENO[2,3-D]PYRIMIDINE DERIVATIVES, THEIR PREPARATION AND APPLICATION 未知

    公开(公告)号：BG63602B1

    公开(公告)日：2002-06-28

    申请号：BG10312299

    申请日：1999-01-27

    Applicant: BASF AG

    Inventor： STEINER GERD ,  LUBISCH WILFRIED ,  BACH ALFRED ,  EMLING FRANZ ,  WICKE KARSTEN ,  TESCHENDORF HANS-JUERGEN ,  BEHL BERTHOLD ,  KERRIGAN FRANK ,  CHEETHAM SHARON

    IPC: A61K31/435 ,  A61K31/519 ,  A61P25/24 ,  A61P43/00 ,  C07D211/00 ,  C07D239/00 ,  C07D333/00 ,  C07D495/14

    Abstract: The 3-substituted 3,4,5,6,7.8-hexahydro-pyrido[4', 3': 4,5]-thieno [2,3-d] pyrimidine derivatives can be used as medicamentous forms for diseases where there is redud serotonin concentration and where, within the therapy, the activity of the presnaptic receptors 5-HT1B-, 5-HT1A-, 5-HT1D-, should be blocked without seriously affecting any other receptors. Depression is an example for such morbid state. The compounds have formula in which R1 is hydrogen, C1-C4-alkyl group, acetyl, benzoyl, phenylalkyl-C1-C4-residue where the aromatic residue is optionally substituted with halogen, C1-C4-alkyl, trifluoromethyl, hydroxy-, C1-C4-alkoxy-, amino-, cyano- or nitrogroups or is naphtalene-C1-C4-alkyl residue, phenylalkanon-C2-C4-residue or phenylcarbamoylalkyl-C2-residue where the phenyl group can be substituted by halogen; R2 optionally is mono-, di- or trisubstituted with halogen atoms, C1-C4-alkyl, trifluoromethyl, trifluormethoxy, hydroxy, C1-C4-alkoxy, amino-, monomethylamino-, diethylamino-, cyano- or nitrogroup, phenyl, pyridyl, pyrimidinyl or pyrasinyl reside which can optionally be ringed by one benzene ring which optionally can be mono- or disubstituted with halogen atom, C1-C4-alkyl, hydroxy, trifluormethyl, C1-C4-alkoxy, amino-, cyano- or nitrogroup, and optionally can contain one nitrogen atom or be ringed by 5- or 6-member ring which can contain one to two oxygen atoms, or can be substituted by phenyl-C1-C2-alkyl, or alkoxygroup, respectively, where the phenyl residue can be substituted with halogen, methyl, trifluormethyl or methoxygroup. A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxy, X is nitrogen atom, Y is the group CH2, CH2- CH2, CH2-CH2-CH2 or CH2-CH, Z is nitrogen atom, carbon or CH where the bond between Y and Z can be double, n has the value of 2, 3 or 4. The invention also relates to physiologically acceptable salts of the above compounds. 6 claims

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