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    O-[3-(4-Substituted-piperazin-1-yl)-2-hydroxypropyl]-hydroxylamines
    1.
    发明授权
    O-[3-(4-Substituted-piperazin-1-yl)-2-hydroxypropyl]-hydroxylamines 失效

    公开(公告)号：US4404384A

    公开(公告)日：1983-09-13

    申请号：US267722

    申请日：1981-05-28

    申请人： Ulrich Gebert ,  Werner Thorwart ,  Jaromir Komarek ,  Carl Cartheuser

    发明人： Ulrich Gebert ,  Werner Thorwart ,  Jaromir Komarek ,  Carl Cartheuser

    IPC分类号： A61K31/395 ,  A61K31/13 ,  A61K31/24 ,  A61P9/12 ,  C07C215/30 ,  C07C239/12 ,  C07C239/20 ,  C07C255/53 ,  C07C255/54 ,  C07C319/14 ,  C07C323/12 ,  C07D207/06 ,  C07D211/00 ,  C07D211/14 ,  C07D233/60 ,  C07D233/74 ,  C07D235/06 ,  C07D295/06 ,  C07D295/08 ,  C07D295/088 ,  C07D295/12 ,  C07D473/08 ,  C07D521/00 ,  A61K31/50

    CPC分类号： C07D235/06 ,  C07C255/00 ,  C07D207/06 ,  C07D211/14 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/088 ,  C07D473/08 ,  Y02P20/55

    摘要： A compound of general formula ##STR1## wherein X represents a radical selected from the group consisting of one of the formulae ##STR2## in which R.sup.1 represents a radical selected from the group(a) a hydrogen atom,(b) an amino group, when X represents an --OR.sup.1 moiety,(c) an alkyl group having from 1 to 6 carbon atoms(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents of the group halogen atoms, alkyl, alkoxy, halogenalkyl groups each having up to 4 carbon atoms, cycloalkyl groups having 3 to 6 carbon atoms, nitro and cyano groups; andR.sup.2 and R.sup.3, which may be the same or different, each represents a radical selected from the group(a) a hydrogen atom,(b) an alkyl group having from 1 to 6 carbon atoms, an unsubstituted cycloalkyl group having from 3 to 7 carbon atoms, such cycloalkyl group substituted by at most 3 substituents of the group hydroxy groups and alkoxycarbonyl groups having 1 to 4 carbon atoms,(c) an aralkyl group, a diaralkyl group each having 1 to 4 carbon atoms in the alkyl moiety and being unsubstituted or substituted in at least one of the radicals in the alkyl moiety by hydroxy groups, and in the aryl moieties by at most 3 substituents selected from the group consisting of alkoxy groups having from 1 to 4 carbon atoms and halogen atoms,(d) an at most binuclear aryl group being unsubstituted or substituted by at most 3 substituents selected from the group consisting of alkyl, alkoxy, halogenoalkyl groups each having up to 4 carbon atoms and halogen atoms,(e) a hydroxy group when the other of R.sup.2 and R.sup.3 is hydrogen,(f) R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, represent a 5- to 7-membered ring selected from the group consisting of an unsubstituted ring, a ring being substituted by an alkyl group having from 1 to 4 carbon atoms, and a ring being interrupted by a heteroatom selected from the group consisting of oxygen, sulphur and further nitrogen atom, and(g) R.sup.2 and R.sup.3 together with the nitrogen atom to which they are attached, represent a ring from the group a 5-membered heteroaromatic ring containing up to 4 nitrogen atoms and such a ring being anelled to a benzene- or uracil-ring, and physiologically acceptable acid addition salts thereof, a process for their preparation and a pharmaceutical composition containing them.

    Xanthine derivatives
    2.
    发明授权
    Xanthine derivatives 失效
    黄嘌呤衍生物

    公开(公告)号：US4289776A

    公开(公告)日：1981-09-15

    申请号：US32536

    申请日：1979-04-23

    申请人： Werner Mohler ,  Manfred Jayme ,  Jaromir Komarek

    发明人： Werner Mohler ,  Manfred Jayme ,  Jaromir Komarek

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P7/02 ,  A61P9/08 ,  C07D473/06

    CPC分类号： C07D473/06

    摘要： Compounds of general formula ##STR1## wherein one of the groups R.sub.1 and R.sub.3 is a straight-chain or branched oxoalkyl group consisting from 5 to 8 carbon atoms and the oxygen atom is attached to a non-terminal carbon atom and is separated from the nearest ring nitrogen atom by at least 3 carbon atoms in (.omega.-1)-oxoalkyl groups and by at least 4 carbon atoms in oxoalkyl groups in which the oxygen atom is separated from the terminal carbon atom by more than one carbon atom, R.sub.2 and the other one of groups R.sub.1 and R.sub.3 are straight chain or branched alkyl groups containing from 1 to 12 carbon atoms but wherein that group R.sub.1 or R.sub.3 which is other than an oxoalkyl group may also be hydrogen, one nitrogen-bound substituent being hydrogen or alkyl containing more than 1 carbon atom, and physiologically acceptable acid addition salts thereof, a process for their preparation and pharmaceutical compositions containing said compounds.

    摘要翻译： 通式（Ⅰ）的化合物，其中R 1和R 3中的一个是由5-8个碳原子组成的直链或支链的氧代烷基，氧原子与非末端碳原子连接并被分离 （ω-1） - 氧代烷基中最接近的环氮原子至少3个碳原子和氧原子与碳原子一起多于一个碳原子的氧代烷基中的至少4个碳原子， R2和R 1和R 3中的另一个是含有1至12个碳原子的直链或支链烷基，但是除了氧代烷基之外的基团R 1或R 3也可以是氢，一个氮键合取代基是氢 或含有多于1个碳原子的烷基，及其生理上可接受的酸加成盐，其制备方法和含有所述化合物的药物组合物。