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    11.
    发明专利
    未知

    公开(公告)号：DK118288B

    公开(公告)日：1970-08-03

    申请号：DK478568

    申请日：1968-10-03

    Applicant: BAYER AG

    Inventor： FRITSCHE D ,  NAST R ,  METZGER K ,  LEY K ,  EHOLZER U

    IPC: C07D241/52 ,  A61K27/00 ,  C07D51/78

    Abstract: 1,188,249. 2 - Halomethyl - quinoxaline -1,4- di - N - oxide - 3 - carboxylic acid amide derivatives. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47012/68. Heading C2C. Novel 2 - halomethyl quinoxaline - 1,4 - di- N - oxide - 3 - carboxylic acid amide derivatives of the general formula wherein R 1 is a hydrogen or chlorine atom or a C 1-4 alkyl or C 1-4 alkoxy group; R 2 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical; R 3 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical or, when R 2 is a hydrogen atom, a cyclohexyl group; or R 2 and R 3 , together with the nitrogen atom to which they are attached, form a 5- or 6-membered saturated heterocyclic ring which may contain a further nitrogen atom or an oxygen atom and the further nitrogen atom may be attached to a C 1-4 alkyl radical which may be substituted by a hydroxy, methoxy or acetoxy radical; and Hal is a chlorine or bromine atom, are prepared (a) by reaction of a 2-methyl-quinoxaline-1,4- di-N-oxide derivative of the general formula with a halogenating agent in an organic solvent at a temperature of 20-120‹ C. or (b) by oxidation of a 2-halomethyl-quinoxaline derivative of the general formula with hydrogen peroxide or an organic per-acid. N - 2 - di - Methyl - quinoxaline - 1,4 - di - N - oxide - 3 - carboxylic acid amide is prepared by reaction of methylamine with diketene, followed by addition to the resulting reaction mixture of benzofuroxan and ammonia. Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, a 2-halomethyl - quinoxaline - 1,4 - di - N - oxide- 3-carboxylic acid amide derivative of the first general formula above, in admixture with a solid or liquid diluent or carrier, and may be administered orally, rectally or parenterally.

    POSTOPEK ZA PRIPRAVO AMIDO-KINOKSALIN-DI-N-OKSIDOV-(1,4) 2-METIL-3-KARBOKSILNE KISLINE S SPLOSNO FORMULO III
    13.
    发明专利
    POSTOPEK ZA PRIPRAVO AMIDO-KINOKSALIN-DI-N-OKSIDOV-(1,4) 2-METIL-3-KARBOKSILNE KISLINE S SPLOSNO FORMULO III 未知

    公开(公告)号：YU229668A

    公开(公告)日：1975-06-30

    申请号：YU229668

    申请日：1968-10-02

    Applicant: BAYER AG

    Inventor： LEY K ,  EHOLZER U ,  FRITSCHE D ,  NAST R ,  METZGER K

    IPC: C07D241/52 ,  C07D51/78

    Abstract: 1,235,869. Quinoxaline-1,4-dioxides. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47013/68. Heading C2C. Novel quinoxaline-1,4-dioxides of the Formula I in which R 1 is H, C 1-4 alkyl, C 1-4 alkoxy, or Cl, R 2 is straight or branched chain alkyl radical which may be substituted by OH, C 1-5 alkoxy, carbalkoxy, or dialkylamino (which term includes saturated N-containing heterocyclic radicals, R 3 is H, straight or branched chain alkyl radical which may be substituted by OH 2 C 1-5 alkoxy, carbalkoxy, mono- or di-alkylamino or when R 3 is H, R 2 may be cyclohexyl or R 2 and R 3 together with the amide nitrogen atom may form part of a 5- or 6-membered ring are prepared by reacting the appropriate benzofuroxane with an acetoacetic acid amide of the formula in the presence of ammonia or a primary amine in an organic solvent at a temperature of 20‹ to 100‹ C. or by oxidizing with hydrogen peroxide a quinoxaline derivative of the Formula XXIII above in which X is a radical readily convertible into a COOH or CON(R 2 )R 3 , group in the presence of glacial acetic acid or acetic anhydride, or an organic per-acid or mixture thereof and converting the thus obtained 1,4-dioxide to a compound of Formula I above. Pharmaceutical compositions having antibacterial activity and suitable for oral or parenteral administration, contain the above novel compounds in admixture with a solid or liquid diluents or carriers.

    17.
    发明专利
    未知

    公开(公告)号：DK119878B

    公开(公告)日：1971-03-08

    申请号：DK478168

    申请日：1968-10-03

    Applicant: BAYER AG

    Inventor： LEY K ,  EHOLZER U ,  NAST R ,  METZGER K ,  FRITSCHE D

    IPC: C07D241/52 ,  A61K27/00 ,  C07D51/78

    Abstract: 1,235,869. Quinoxaline-1,4-dioxides. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47013/68. Heading C2C. Novel quinoxaline-1,4-dioxides of the Formula I in which R 1 is H, C 1-4 alkyl, C 1-4 alkoxy, or Cl, R 2 is straight or branched chain alkyl radical which may be substituted by OH, C 1-5 alkoxy, carbalkoxy, or dialkylamino (which term includes saturated N-containing heterocyclic radicals, R 3 is H, straight or branched chain alkyl radical which may be substituted by OH 2 C 1-5 alkoxy, carbalkoxy, mono- or di-alkylamino or when R 3 is H, R 2 may be cyclohexyl or R 2 and R 3 together with the amide nitrogen atom may form part of a 5- or 6-membered ring are prepared by reacting the appropriate benzofuroxane with an acetoacetic acid amide of the formula in the presence of ammonia or a primary amine in an organic solvent at a temperature of 20‹ to 100‹ C. or by oxidizing with hydrogen peroxide a quinoxaline derivative of the Formula XXIII above in which X is a radical readily convertible into a COOH or CON(R 2 )R 3 , group in the presence of glacial acetic acid or acetic anhydride, or an organic per-acid or mixture thereof and converting the thus obtained 1,4-dioxide to a compound of Formula I above. Pharmaceutical compositions having antibacterial activity and suitable for oral or parenteral administration, contain the above novel compounds in admixture with a solid or liquid diluents or carriers.

    POSTOPEK ZA PRIPRAVO AMIDO-KINOKSALIN-DI-N-OKSIDOV-(1,4) 2-HALOGENMETIL-3-KARBOKSILNE KISLINE
    20.
    发明专利
    POSTOPEK ZA PRIPRAVO AMIDO-KINOKSALIN-DI-N-OKSIDOV-(1,4) 2-HALOGENMETIL-3-KARBOKSILNE KISLINE 未知

    公开(公告)号：YU229568A

    公开(公告)日：1975-06-30

    申请号：YU229568

    申请日：1968-10-02

    Applicant: BAYER AG

    Inventor： NAST R ,  METZGER K ,  LEY K ,  EHOLZER U

    IPC: C07D241/52 ,  A61K

    Abstract: 1,188,249. 2 - Halomethyl - quinoxaline -1,4- di - N - oxide - 3 - carboxylic acid amide derivatives. FARBENFABRIKEN BAYER A.G. 3 Oct., 1968 [4 Oct., 1967], No. 47012/68. Heading C2C. Novel 2 - halomethyl quinoxaline - 1,4 - di- N - oxide - 3 - carboxylic acid amide derivatives of the general formula wherein R 1 is a hydrogen or chlorine atom or a C 1-4 alkyl or C 1-4 alkoxy group; R 2 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical; R 3 is a hydrogen atom or an alkyl group optionally substituted by a hydroxy, C 1-4 alkoxy, C 1-5 carbalkoxy, acyloxy or mono- or di-C 1-4 alkylamino radical or, when R 2 is a hydrogen atom, a cyclohexyl group; or R 2 and R 3 , together with the nitrogen atom to which they are attached, form a 5- or 6-membered saturated heterocyclic ring which may contain a further nitrogen atom or an oxygen atom and the further nitrogen atom may be attached to a C 1-4 alkyl radical which may be substituted by a hydroxy, methoxy or acetoxy radical; and Hal is a chlorine or bromine atom, are prepared (a) by reaction of a 2-methyl-quinoxaline-1,4- di-N-oxide derivative of the general formula with a halogenating agent in an organic solvent at a temperature of 20-120‹ C. or (b) by oxidation of a 2-halomethyl-quinoxaline derivative of the general formula with hydrogen peroxide or an organic per-acid. N - 2 - di - Methyl - quinoxaline - 1,4 - di - N - oxide - 3 - carboxylic acid amide is prepared by reaction of methylamine with diketene, followed by addition to the resulting reaction mixture of benzofuroxan and ammonia. Pharmaceutical compositions having antibacterial activity comprise, as active ingredient, a 2-halomethyl - quinoxaline - 1,4 - di - N - oxide- 3-carboxylic acid amide derivative of the first general formula above, in admixture with a solid or liquid diluent or carrier, and may be administered orally, rectally or parenterally.

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