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19 条记录 (耗时 0.037 秒)

    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity
    6.
    发明授权
    Dealkylated derivatives of pyrrolo[2,1-b]benzothiazepines with atypical antipsychotic activity 失效
    具有非典型抗精神病活性的吡咯并[2,1-b]苯并硫氮杂的脱烷基衍生物

    公开(公告)号：US07713956B2

    公开(公告)日：2010-05-11

    申请号：US11579806

    申请日：2005-04-28

    申请人： Paolo Carminati ,  Maria Assunta Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    发明人： Paolo Carminati ,  Maria Assunta Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    IPC分类号： A61P25/18 ,  A61K31/407 ,  C07D513/04

    CPC分类号： C07D513/04

    摘要： Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C═CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH═NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

    摘要翻译： 吡咯并[2,1-b]苯并硫氮杂与式（I）的衍生物，其中A是CH-CH 2 C = CH; R是氢，卤素，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基，C 5 -C 6环烷基; R1是1-哌嗪基，1-高哌嗪基和1-哌啶基; R 2是氢，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基，CHO，CH = NH，CH 2 OH。 式（I）化合物具有特征性非典型抗精神病活性，因此可用作药物，特别是用于治疗和预防精神分裂症，偏执状态，躁狂抑郁状态，情感障碍，社会回归， 人格回归和幻觉。 所述化合物还表现出有利的药代动力学性质。

    Dealkylated Derivatives of Pyrrolo[2,1-B]Benzothiazepines with Atypical Antipsy-Chotic Activity
    7.
    发明申请
    Dealkylated Derivatives of Pyrrolo[2,1-B]Benzothiazepines with Atypical Antipsy-Chotic Activity 失效
    吡咯并[2,1-B]苯并硫氮杂脱烷基衍生物与非典型抗胆碱活性

    公开(公告)号：US20070270402A1

    公开(公告)日：2007-11-22

    申请号：US11579806

    申请日：2005-04-28

    申请人： Paolo Carminati ,  Maria Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    发明人： Paolo Carminati ,  Maria Di Cesare ,  Orlando Ghirardi ,  Patrizia Minetti ,  Maria Ornella Tinti

    IPC分类号： A61K31/554 ,  A61P25/18 ,  C07D281/02

    CPC分类号： C07D513/04

    摘要： Derivatives of pyrrolo[2,1-b]benzothiazepines with formula (I) where A is CH—CH2C═CH; R is hydrogen, halogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, C5-C6 cycloalkyl; R1 is 1-peperazinyl, 1-homopiperazinyl and 1-piperidinyl; R2 is hydrogen, C1-C4 alkoxy, C1-C4 alkylthio, C1-C4 alkyl, CHO, CH═NOH,CH2OH. The formula (I) compounds are endowed with characteristic atypical anti-psychotic activity, and are therefore useful as medicaments, in particular for the treatment and prevention of schizophrenia, paranoid states, manic-depressive states, disorders of the affective sphere, social regression, personality regression, and hallucinations. Said compounds also present advantageous pharmacokinetic properties.

    摘要翻译： 具有式（I）的吡咯并[2,1-b]苯并硫氮杂的衍生物，其中A是CH-CH 2 C-CH; R是氢，卤素，C 1 -C 4烷氧基，C 1 -C 4烷硫基，C 1 -C 4烷基， C 1 -C 4烷基，C 5 -C 6环烷基，C 1 -C 4烷基，C 5 -C 6环烷基， R 1是1-哌嗪基，1-高哌嗪基和1-哌啶基; R 2是氢，C 1 -C 4烷氧基，C 1 -C 4烷基， C 1 -C 4烷基，C 1 -C 4烷基，CHO，CH-NOH，CH 2 OH。 式（I）化合物具有特征性非典型抗精神病活性，因此可用作药物，特别是用于治疗和预防精神分裂症，偏执状态，躁狂抑郁状态，情感障碍，社会回归， 人格回归和幻觉。 所述化合物还表现出有利的药代动力学性质。

    Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same
    10.
    发明授权
    Oligopeptide derivatives of ipoxantine endowed with immunomodulating activity and pharmaceutical compositions containing same 失效
    具有免疫调节活性的异辛胺的寡肽衍生物和含有它们的药物组合物

    公开(公告)号：US5298621A

    公开(公告)日：1994-03-29

    申请号：US723418

    申请日：1991-06-28

    申请人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

    发明人： Mauro Marzi ,  Patrizia Minetti ,  Piero Foresta ,  Maria O. Tinti

    IPC分类号： A61K38/00 ,  A61P37/00 ,  C07K5/06 ,  C07K5/072 ,  C07K5/08 ,  C07K5/087 ,  C07K5/09 ,  C07K5/093 ,  C07K5/097 ,  C07K5/10 ,  C07K5/103 ,  C07K5/11 ,  C07K7/06

    CPC分类号： C07K7/06 ,  C07K5/06026 ,  C07K5/06043 ,  C07K5/06113 ,  C07K5/0812 ,  C07K5/0815 ,  C07K5/0819 ,  C07K5/0823 ,  C07K5/101 ,  C07K5/1019 ,  A61K38/00

    摘要： Ipoxantine derivatives of general formula (I): ##STR1## both as racemate and chiral forms and the salts thereof with pharmacologically acceptable cations, wherein n is an integer comprised between 2 and 6, and A is the residue of a dipeptide, tripeptide, tetrapeptide and pentapeptide selected, respectively, from the groups consisting of:(a) glycyl-aspartate, alanyl-glycine, glycyl-glycine, aspartyl-arginine, leucyl-arginine;(b) arginyl-lysyl-aspartate, aspartyl-lysyl-arginine, lysyl-prolyl-arginine, prolyl-prolyl-arginine, lysyl-histidyl-glycinamide, prolyl-phenilalanyl-arginine, phenylalanyl-prolyl-arginine;(c) arginyl-lysyl-aspartyl-valine (SEQ ID NO: 1), valyl-aspartyl-lysyl-arginine (SEQ ID NO: 2), threonylvalyl-leucyl-histidyne (SEQ ID NO: 3); and(d) arginyl-lysyl-aspartyl-valyl-tyrosine (SEQ ID NO: 4);are endowed with immunomodulating activity and can be formulated in orally or parenterally administrable pharmaceutical compositions.

    摘要翻译： 作为外消旋物和手性形式的通式（I）的碘醇衍生物：（*化学结构*）及其与药理学上可接受的阳离子的盐，其中n是2和6之间的整数，A是二肽的残基， 分别选自：（a）甘氨酰 - 天冬氨酸，丙氨酰 - 甘氨酸，甘氨酰 - 甘氨酸，天冬氨酰 - 精氨酸，亮氨酰 - 精氨酸;三肽，四肽和五肽; （b）精氨酰 - 赖氨酰 - 天冬氨酸，天冬氨酰赖氨酰 - 精氨酸，赖氨酰 - 脯氨酰 - 精氨酸，脯氨酰 - 脯氨酰 - 精氨酸，赖氨酰 - 组氨酰 - 甘氨酰胺，脯氨酰 - 苯丙氨酰 - 精氨酸，苯丙氨酰脯氨酰 - 精氨酸; （c）精氨酰 - 赖氨酰 - 天冬氨酰缬氨酸（SEQ ID NO：1），缬氨酰天冬氨酰赖氨酰 - 精氨酸（SEQ ID NO：2），苏氨酰缬氨酰 - 亮氨酰 - 组氨酸（SEQ ID NO：3）; 和（d）精氨酰 - 赖氨酰 - 天冬氨酰 - 缬氨酰 - 酪氨酸（SEQ ID NO：4）; 具有免疫调节活性，并可配制成口服或非肠道给药的药物组合物。