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    Pyrrolyl tetrahydroquinoxalin diones, their production and use in the treatment of diseases
    24.
    发明授权
    Pyrrolyl tetrahydroquinoxalin diones, their production and use in the treatment of diseases 失效
    吡咯基四氢喹喔啉二氢睾酮，其生产和用于治疗疾病

    公开(公告)号：US06407109B1

    公开(公告)日：2002-06-18

    申请号：US09000277

    申请日：1998-01-27

    申请人： Wilfried Lubisch ,  Berthold Behl ,  Hans-Peter Hofmann ,  Hans-Jürgen Teschendorf

    发明人： Wilfried Lubisch ,  Berthold Behl ,  Hans-Peter Hofmann ,  Hans-Jürgen Teschendorf

    IPC分类号： A61K31498

    CPC分类号： C07D401/14 ,  C07D403/04

    摘要： Pyrrolylquinoxalinediones of the formula I and their tautomeric and isomeric forms, and their physiologically tolerated salts, where the variables have the following meanings: R1 hydrogen, cyclohexyl an aliphatic radical which has 1 to 4 carbon atoms and can carry the radical —COOR5, where R5 is hydrogen or C1-C4-alkyl, R2 —COOH, —COO—C1-C4, —COO—(CH2)m—Ph, —CONR6R7 and where m can be an integer from 1 to 6, R6 can be hydrogen, C1-C4-alkyl or OH and R7 can be hydrogen, C1-C4-alkyl, where all the phenyl or pyridyl rings present in R2 can also be substituted by up to 3 of the following radicals: C1-C4-alkyl, halogen, —O—C1-C4-alkyl, —OCF3, —NO2, —CN, —COOR5 or —CONHR5, R3 —CF3, —NO2, —CN, and R4 hydrogen or R3 and R4 can together be a fused-on benzene ring. The compounds are suitable as drugs for human and veterinary medicine.

    摘要翻译： 具有式I的吡咯基喹喔啉及其互变异构体和异构体形式及其生理学耐受盐，其中变量具有以下含义：具有1至4个碳原子并且可以携带-COOR5基团的R1氢，环己烷基脂族基团，其中R5是氢或 C 1 -C 4烷基，R 2，其中m可以是1至6的整数，R 6可以是氢，C 1 -C 4 - 烷基或OH，且R 7可以是氢，C 1 -C 4 - 烷基，其中所有苯基或吡啶环存在于 R2还可以被多达3个以下基团取代：R3R4氢或R3和R4可以一起是稠合的苯环。 该化合物适合作为人兽药用药物。

    2,3(1H,4H)quinoxalinedione
    27.
    发明授权
    2,3(1H,4H)quinoxalinedione 失效
    2,3（1H，4H）喹喔啉二酮

    公开(公告)号：US5714489A

    公开(公告)日：1998-02-03

    申请号：US512282

    申请日：1995-08-08

    申请人： Wilfried Lubisch ,  Berthold Behl ,  Hans Peter Hofmann

    发明人： Wilfried Lubisch ,  Berthold Behl ,  Hans Peter Hofmann

    IPC分类号： 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

    CPC分类号： C07D403/04 ,  C07D241/52 ,  C07D487/14

    摘要： 2,3(1H,4H)-quinoxalinediones of the formula I ##STR1## where R.sup.1 is hydrogen, an aliphatic radical which has up to 12 carbons and can be substituted by one of the following: phenyl, cyclopentyl, cyclohexyl or --CO--R.sup.3, --CO--O--R.sup.3 or --CO--NH--R.sup.3, where R.sup.3 is hydrogen, C.sub.1 -C.sub.4 -alkyl, phenyl, benzyl or 1-phenylethyl, a cycloaliphatic radical with up to 12 carbons or phenyl, where the cyclic groups in R.sup.1 can have up to three of the following substituents: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -haloalkoxy, halogen, nitro, cyano, --CO--O--R.sup.3 and --CO--NH--R.sup.3 ; R.sup.2 is 1-pyrrolyl which can have up to two of the following substituents: C.sub.1 -C.sub.4 -alkyl, phenyl, phenylsulfonyl, nitro, cyano and --CO--O--R.sup.3, --CO--NH--R.sup.3, --CH.sub.2 --O--R.sup.3, --O--R.sup.3 and --CH.dbd.NO--R.sup.3 R radicals are identical or different and are the following: C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, trifluoromethyl, trichloromethyl, trifluoromethoxy, trichloromethoxy, fluorine, chlorine, bromine, iodine, nitro, cyano and --CO--O--R.sup.3 and --CO--NH--R.sup.3 as well as a fused-on benzene ring; n is 0-3, and 2,3(1H,4H)-quinoxalinediones I' ##STR2## where R.sup.1 has the stated meanings, are suitable as drugs in the treatment of neurodegenerative disorders and neurotoxic disturbances of the central nervous system.

    摘要翻译： 式I的2,3（1H，4H） - 喹喔啉，其中R 1是氢，具有至多12个碳原子并且可以被下列之一取代的脂族基团：苯基，环戊基，环己基或-CO -R 3，-CO-O-R 3或-CO-NH-R 3，其中R 3是氢，C 1 -C 4烷基，苯基，苄基或1-苯基乙基，具有至多12个碳的脂环族基团或苯基， R1中的基团可以具有多达三个以下取代基：C 1 -C 4 - 烷基，C 1 -C 4 - 卤代烷基，C 1 -C 4 - 烷氧基，C 1 -C 4 - 卤代烷氧基，卤素，硝基，氰基，-CO-O-R 3和 -CO-NH-R3; R2是可以具有至多两个以下取代基的1-吡咯基：C 1 -C 4烷基，苯基，苯基磺酰基，硝基，氰基和-CO-O-R 3，-CO-NH-R 3，-CH 2 -O-R 3 ，-O-R3和-CH = NO-R3R基团是相同或不同的，如下：C 1 -C 4 - 烷基，C 1 -C 4 - 烷氧基，三氟甲基，三氯甲基，三氟甲氧基，三氯甲氧基，氟，氯，溴，碘 ，硝基，氰基和-CO-O-R 3和-CO-NH-R 3以及稠合的苯环; n为0-3，并且具有所述含义的2,3（1H，4H） - 喹喔啉酮I'，其中R 1具有所述含义，适合作为治疗神经变性疾病和中枢神经系统的神经毒性紊乱的药物。

    3-substituted pyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and their use
    30.
    发明授权
    3-substituted pyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine derivatives, their preparation and their use 有权
    3-取代的吡啶并[4'，3'：4,5]噻吩并[2,3-d]嘧啶衍生物，其制备及其用途

    公开(公告)号：US06222034B1

    公开(公告)日：2001-04-24

    申请号：US09254449

    申请日：1999-03-10

    申请人： Gerd Steiner ,  Wilfried Lubisch ,  Alfred Bach ,  Franz Emling ,  Karsten Wicke ,  Hans-Jürgen Teschendorf ,  Berthold Behl ,  Sharon Cheetham ,  Frank Kerrrigan

    发明人： Gerd Steiner ,  Wilfried Lubisch ,  Alfred Bach ,  Franz Emling ,  Karsten Wicke ,  Hans-Jürgen Teschendorf ,  Berthold Behl ,  Sharon Cheetham ,  Frank Kerrrigan

    IPC分类号： C07D49514

    CPC分类号： C07D495/14

    摘要： A 3-substituted 3,4,5,6,7,8-hexahydropyrido[4′,3′:4,5]thieno[2,3-d]pyrimidine compound of formula I wherein R1 is hydrogen, C1-C4-alkyl, acetyl or benzoyl, optionally substituted phenyl-C1-C4-alkyl, naphthyl-C1-C3-alkyl, phenyl-C2-C3-alkanone or a phenylcarbamoyl-C2-alkyl, R2 is optionally substituted phenyl, pyridyl, pyrimidyl or pyrazinyl, or an optionally substituted bicyclus wherein one of the two fused rings is a phenyl, a pyridyl, a pyrimidyl or a pyrazinyl ring, A is NH or oxygen, B is hydrogen or methyl, C is hydrogen, methyl or hydroxyl, X is nitrogen, Y is CH2, CH2—C2, CH2—C2—CH2 or CH2—CH, Z is nitrogen, C or CH, and the linkage between Y and Z is a single or a double bond, and n is 2, 3 or 4, or a physiologically tolerated salt thereof, and compositions comprising them and their use as antagonists of 5HT1B and 5HT1A and for the treatment of depression and related disorders.

    摘要翻译： 式I的3-取代的3,4,5,6,7,8-六氢吡啶并[4'，3'：4,5]噻吩并[2,3-d]嘧啶化合物，其中R1为氢，C1-C4-烷基， 乙酰基或苯甲酰基，任选取代的苯基-C 1 -C 4 - 烷基，萘基-C 1 -C 3 - 烷基，苯基-C 2 -C 3 - 烷酮或苯基氨基甲酰基-C 2 - 烷基，R 2是任选取代的苯基，吡啶基，嘧啶基或吡嗪基，或 任选取代的双环，其中两个稠合环之一为苯基，吡啶基，嘧啶基或吡嗪基，A为NH或氧，B为氢或甲基，C为氢，甲基或羟基，X为氮，Y 是CH2，CH2-C2，CH2-C2-CH2或CH2-CH，Z是氮，C或CH，Y和Z之间的键是单键或双键，并且是2,3或4，或 生理上耐受的盐，以及包含它们的组合物及其作为5HT1B和5HT1A的拮抗剂的用途以及用于治疗抑郁症和相关疾病的用途。