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    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols
    2.
    发明授权
    1,2,3,4,5,6-Hexahydro-2,6-methano-3-benzazocin-10-ols 有权
    1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖庚因-10-ols

    公开(公告)号：US06455538B1

    公开(公告)日：2002-09-24

    申请号：US09523473

    申请日：2000-03-10

    申请人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    发明人： Matthias Grauert ,  Adrian Carter ,  Wolf-Dietrich Bechtel ,  Thomas Weiser ,  Rainer Palluk ,  Uwe Pschorn

    IPC分类号： A61K31439

    CPC分类号： C07D221/26

    摘要： Compounds of general formula I wherein X is a single bond, —O—, C-C4-alkylene, or an alkylene bridge having 1 to 8 carbon atoms which may be branched or unbranched and optionally have one or two oxygen atom(s) anywhere in the bridge; R1 is hydrogen, methyl, ethyl, or phenyl; R2 is hydrogen or methyl; R3 is hydrogen, fluorine, chlorine, bromine, hydroxy, methyl, or methoxy; R4 is hydrogen, methyl, or ethyl; R5 is hydrogen, methyl, or ethyl; R6 is hydrogen, methyl, or ethyl; R7 is tert-butyl, cyclohexyl, phenyl optionally substituted by R9 and R10, which may be identical or different, or; R8 is hydrogen or C1-C4-alkyl; Z is oxygen, NH, or sulfur; R9 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; R10 is hydrogen, methyl, fluorine, chlorine, bromine, or methoxy; optionally in the form of the individual optical isomers, mixtures of the individual enantiomers or racemates as well as in the form of the free bases or the corresponding acid addition salts with pharmaceutically acceptable acids.

    摘要翻译： 通式I的化合物，其中X是单键，-O-，C-C4-亚烷基或具有1至8个碳原子的亚烷基桥，其可以是支链或非支链的，并且任选地在一个或多个氧原子中具有一个或两个氧原子 桥梁 R1是氢，甲基，乙基或苯基; R2是氢或甲基; R3是氢，氟，氯，溴，羟基，甲基或甲氧基; R4是氢，甲基或乙基; R5是氢，甲基或乙基; R6是氢，甲基或乙基; R 7是叔丁基，环己基，任选被R 9和R 10取代的苯基，其可以相同或不同，或者R 8是氢或C 1 -C 4 - 烷基; Z是氧，NH或硫; R9是氢，甲基，氟，氯，溴或甲氧基; R 10为氢，甲基，氟，氯，溴或甲氧基; 任选以各种旋光异构体的形式，各个对映异构体或外消旋体的混合物，以及游离碱的形式或与药学上可接受的酸的相应的酸加成盐。

    Pharmaceutical compositions containing triazolones and methods of treating neurodegenerative disease using triazolones
    7.
    发明授权
    Pharmaceutical compositions containing triazolones and methods of treating neurodegenerative disease using triazolones 有权
    含有三唑酮的药物组合物和使用三唑酮治疗神经变性疾病的方法

    公开(公告)号：US06492407B2

    公开(公告)日：2002-12-10

    申请号：US09840281

    申请日：2001-04-23

    申请人： Michael Brenner ,  Wolf-Dietrich Bechtel ,  Rainer Palluk ,  Marion Wienrich ,  Thomas Weiser

    发明人： Michael Brenner ,  Wolf-Dietrich Bechtel ,  Rainer Palluk ,  Marion Wienrich ,  Thomas Weiser

    IPC分类号： A61K3141

    CPC分类号： C07D401/04 ,  C07D249/12

    摘要： A method for treating a neurodegenerative disease or cerebral ischemia arising from conditions selected from the group consisting of Status epilepticus, hypoglycaemia, hypoxia, anoxia, brain trauma, brain oedema, amyotropic lateral sclerosis, Huntington's disease, Alzheimer's disease, hypotonia, cardiac infarction, brain pressure (elevated intracranial pressure), ischaemic and haemorrhagic stroke, global cerebral ischaemia with heart stoppage, diabetic polyneuropathy, tinnitus, perinatal asphyxia, psychosis, schizophrenia, depression, and Parkinson's disease, the method of treatment comprising administering to a host in need of such treatment a therapeutic amount of a compound of formula (I) wherein R1, R2, R3, R4, R5, R6, and R7 are as defined herein, or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions containing a compound of formula (I).

    摘要翻译： 一种用于治疗由选自癫痫持续状态，低血糖，缺氧，缺氧，脑外伤，脑水肿，肌萎缩性侧索硬化，亨廷顿舞蹈病，阿尔茨海默氏病，低张力，心肌梗死，脑中的病症引起的神经变性疾病或脑缺血的方法 压力（颅内压升高），缺血性和出血性中风，心脏停止的全球性脑缺血，糖尿病性多发性神经病，耳鸣，围产期窒息，精神病，精神分裂症，抑郁症和帕金森病，治疗方法包括向需要这种 治疗治疗量的式（I）化合物，其中R 1，R 2，R 3，R 4，R 5，R 6和R 7如本文所定义，或其药学上可接受的盐，以及含有式（I）化合物的药物组合物， 。

    Phenyl-and phenylalkyl-substituted ethanolamines and ethylenediamines
    8.
    发明授权
    Phenyl-and phenylalkyl-substituted ethanolamines and ethylenediamines 有权
    苯基和苯基烷基取代的乙醇胺和乙二胺

    公开(公告)号：US06770636B2

    公开(公告)日：2004-08-03

    申请号：US09912163

    申请日：2001-07-24

    申请人： Klaus Fuchs ,  Werner Stransky ,  Matthias Grauert ,  Adrian Carter ,  Wolfram Gaida ,  Thomas Weiser ,  Helmut Ensinger

    发明人： Klaus Fuchs ,  Werner Stransky ,  Matthias Grauert ,  Adrian Carter ,  Wolfram Gaida ,  Thomas Weiser ,  Helmut Ensinger

    IPC分类号： A61K3133

    CPC分类号： C07D295/125 ,  C07C211/35 ,  C07C217/48 ,  C07C2601/02 ,  C07C2601/14 ,  C07C2601/16 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D295/092

    摘要： Compounds of formula 1, wherein: R1 is hydrogen, hydroxy, CF3, NO2, CN, halogen, C1-C8-alkyl, or C1-C8-alkoxy; R2, R3, and R4 independently of one another are hydrogen, C1-C8-alkyl, hydroxy, NO2, CN, C1-C8-alkoxyl, CF3, or halogen; R5 and R6 independently of one another are hydrogen or a group consisting of C1-C8-alkyl, C2-C8-alkenyl, C3-C8-alkynyl, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkylene, C5-C8-cycloalkenyl, C5-C8-cycloalkenyl-C1-C6-alkylene, C6-C10-aryl, and C6-C10-aryl-C1-C6-alkylene, each optionally substituted by a group consisting of C1-C6-alkyl, C2-C6-alkenyl, halogen, C1-C6-alkyloxy, —NH2, —NH(C1-C4-alkyl), —N(C1-C4-alkyl)2, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, and CF3, or R5 and R6 together with the nitrogen atom are a saturated or unsaturated 5-, 6-, 7-, or 8-membered heterocyclic group optionally containing one or two further heteroatoms consisting of sulfur, oxygen, and nitrogen, and optionally mono-, di-, or trisubstituted by a group consisting of C1-C4-alkyl, hydroxy, ═O, —COOH, —CO—OC1-C4-alkyl, —CONH2, —CONH(C1-C4-alkyl), —CON(C1-C4-alkyl)2, halogen, and benzyl; X is oxygen, —NH—, —N(CHO)—, —N(CO—C1-C6-alkyl), —N(C1-C6-alkyl), or —N(C3-C6-cycloalkyl-C1-C4-alkylene); and A is a group consisting of C1-C6-alkylene, C2-C6-alkenylene, and C3-C6-alkynylene, each optionally substituted by a group consisting of halogen, ═O, and hydroxy, or an optical isomer, enantiomer, tautomer, free base, or pharmacologically acceptable acid addition salt thereof; methods of making such compounds; pharmaceutical compositions thereof, and their use in treating or preventing certain diseases.

    摘要翻译： 式1的化合物，其中：R 1是氢，羟基，CF 3，NO 2，CN，卤素，C 1 -C 8 - 烷基或C 1 -C 8 - 烷氧基; R 2，R 3， 4>彼此独立地是氢，C 1 -C 8 - 烷基，羟基，NO 2，CN，C 1 -C 8 - 烷氧基，CF 3或卤素; R 5和R 6彼此独立地是氢或基团 由C 1 -C 8 - 烷基，C 2 -C 8 - 烯基，C 3 -C 8 - 炔基，C 3 -C 8 - 环烷基，C 3 -C 8 - 环烷基-C 1 -C 6亚烷基，C 5 -C 8 - 环烯基，C 5 -C 8 - 环烯基 - C 1 -C 6 - 亚烷基，C 6 -C 10 - 芳基和C 6 -C 10 - 芳基-C 1 -C 6亚烷基，各自任选被C 1 -C 6 - 烷基，C 2 -C 6 - 烯基，卤素，C 1 -C 6 - 烷氧基，-NH 2，-NH（C 1 -C 4 - 烷基），-N（C 1 -C 4 - 烷基）2，羟基，= O，-COOH，-CO-OC 1 -C 4烷基，-CONH 2，-CONH C 1 -C 4烷基），-CON（C 1 -C 4 - 烷基）2和CF 3或R 5和R 6与氮原子一起为饱和或不饱和的5-，6-，7-或 任选地含有一个或两个由硫，氧和氮组成的另外的杂原子的8-元杂环基，以及任选的单 - ，二 - ，或被由C 1 -C 4 - 烷基，羟基，O，-COOH，-CO-OC 1 -C 4烷基，-CONH 2，-CONH（C 1 -C 4 - 烷基），-CON（C 1 -C 4） - 烷基）2，卤素和苄基; X是氧，-NH-，-N（CHO） - ， - N（CO-C 1 -C 6烷基）， - N（C 1 -C 6 - 烷基） （C 3 -C 6 - 环烷基-C 1 -C 4 - 亚烷基）; 并且A是由C 1 -C 6亚烷基，C 2 -C 6亚烯基和C 3 -C 6亚炔基组成的基团，各自任选地被卤素，= O和羟基取代，或光学异构体，对映体，互变异构体， 游离碱或其药理学上可接受的酸加成盐; 制备此类化合物的方法; 其药物组合物及其在治疗或预防某些疾病中的用途。

    Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions
    10.
    发明授权
    Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines and their use as pharmaceutical compositions 有权
    取代的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪及其作为药物组合物的用途

    公开(公告)号：US06387921B1

    公开(公告)日：2002-05-14

    申请号：US09995382

    申请日：2001-11-27

    申请人： Matthias Grauert ,  Adrian Carter ,  Thomas Weiser ,  Helmut Ensinger ,  Wolfram Gaida ,  Joachim Mierau

    发明人： Matthias Grauert ,  Adrian Carter ,  Thomas Weiser ,  Helmut Ensinger ,  Wolfram Gaida ,  Joachim Mierau

    IPC分类号： A61K314748

    CPC分类号： C07D405/06 ,  C07D221/26

    摘要： Substituted 1,2,3,4,5,6-hexahydro-2,6-methano-3-benzazocines of general formula 1: wherein: R1 and R2, which are identical or different, are each hydrogen, C1-C6-alkyl, C1--C6-alkyloxy, OH, F, Cl, or Br; R3 is hydrogen, F, Cl, Br, methyl, ethyl, OH, or methoxy; R4 and R5, which are identical or different, are each hydrogen, methyl, or ethyl; R6 is hydrogen; X is NH2, NH—(C1-C6-alkyl), N(C1-C6-alkyl)2, the two C1-C6-alkyl groups of which are identical or different, NH—COH, NH—CO(C1-C6-alkyl), or F; A is —(CH2)3—, —CH2—CH2—O—, —CH2—O—CH2—, —(CH2)4—, —CH(C1-C6-alkyl)-O—CH2—, —(CH2)2—O—CH2—, —(CH2)3—O—, —(CH2)5—, —CH2—O—(CH2)3—, —(CH2)2—O—(CH2)2—, —(CH2)3—O—CH2—, —(CH2)4—O—, —CH2—O—CH2—CH2—O—, the racemates thereof, the enantiomers thereof, the diastereomers thereof, and mixtures thereof, and the pharmacologically acceptable acid addition salts thereof, processes for preparing them, and their use as pharmaceutical compositions.

    摘要翻译： 取代的通式1的1,2,3,4,5,6-六氢-2,6-亚甲基-3-苯并吖嗪：其中：R 1和R 2各自相同或不同，为氢，C 1 -C 6 - 烷基 ，C 1 -C 6烷氧基，OH，F，Cl或Br; R 3是氢，F，Cl，Br，甲基，乙基，OH或甲氧基; R 4和R 5各自相同或不同， 甲基或乙基; R6是氢; X是NH2，NH-（C1-C6-烷基），N（C1-C6-烷基）2，它们的两个C1-C6-烷基相同或不同，NH- COH，NH-CO（C1-C6-烷基）或F; A是 - （CH2）3-，-CH2-CH2-O-，-CH2-O-CH2-， - （CH2） （C 1 -C 6 - 烷基）-O-CH 2 - ， - （CH 2）2 -O-CH 2 - ， - （CH 2）3 -O - ， - （CH 2） ， - （CH 2）2 -O-（CH 2）2 - ， - （CH 2）3 -O-CH 2 - ， - （CH 2）4 -O - ， - CH 2 -O-CH 2 -CH 2 -O-， ，其对映异构体，其非对映体及其混合物，及其药学上可接受的酸加成盐，其制备方法及其作为药物组合物的用途。