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    Pharmaceutical agents for the treatment of cerebral amyloidosis
    3.
    发明公开
    Pharmaceutical agents for the treatment of cerebral amyloidosis 失效
    Pharmazutische Wirkstoffe zur Behandlung von Hirnamyloidose

    公开(公告)号：EP1930308A1

    公开(公告)日：2008-06-11

    申请号：EP07021294.9

    申请日：1998-05-19

    申请人： NYMOX CORPORATION

    发明人： Averback, Paul ,  Ghanbari, Hossein ,  Beheshti, Iraj ,  Morse, David

    IPC分类号： C07C43/164 ,  A61K31/08 ,  C07C43/174 ,  C07C217/10 ,  C07D211/90 ,  C07D295/02 ,  C07D295/08 ,  C07D473/04 ,  A61K31/495 ,  A61K31/44 ,  A61K31/52

    CPC分类号： C07D295/03 ,  C07C43/164 ,  C07C43/1745 ,  C07C211/28 ,  C07C217/10 ,  C07D211/90 ,  C07D295/088 ,  C07D473/04

    摘要： The invention relates to a compound of the following general formula (III):

    wherein:
    R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
    R 3 is selected from the group consisting of amino, C1-C5 substituted amino and CH 2 ;
    n and m are independently an integer of from 0-5;

    or a pharmaceutically acceptable salt of such compound;
    a compound of the following general formula (IV):

    wherein:
    R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and ca rboxyl;
    R 3 and R 4 each are independent and selected from the group consisting of hydrogen and C1-C5 alkyl;
    n is an integer of from 1 to 5;

    or a pharmaceutically acceptable salt of such compound;
    a compound of the following general formula (V):

    wherein:
    R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
    R 3 is selected from hydrogen and C1-C5 alkyl;
    R 4 is selected from hydrogen and C1-C5 alkyl;
    n is an integer of from 1 to 5 inclusive;
    or a pharmaceutically acceptable salt of such compound; and
    a compound of the following general formula (VI):

    wherein:
    R 1 and R 2 each are one or more independent substituents selected from the group consisting of hydrogen, C1-C5 alkyl, C2-C5 alkenyl, C3-C5 cycloalkyl, C1-C5 alkoxy, C2-C5 alkynyl, halogen, C1-C5 haloalkyl, alkylamino, phenyl, nitro and carboxyl;
    R3 and R4 each are independent and selected from hydrogen and C1-C5 alkyl;
    n is an integer of from 1 to 5 inclusive;
    or a pharmaceutically acceptable salt of such compound.
    Also compositions comprising the compounds III-VI as well as uses of said compounds.

    摘要翻译： 本发明涉及以下通式（III）的化合物：其中：R 1和R 2各自为选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5中的一个或多个独立取代基 环烷基，C 1 -C 5烷氧基，C 2 -C 5炔基，卤素，C 1 -C 5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3选自氨基，C 1 -C 5取代的氨基和CH 2; n和m独立地为0-5的整数; 或该化合物的药学上可接受的盐; 下列通式（IV）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基， C5烷氧基，C2-C5炔基，卤素，C1-C5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3和R 4各自独立地选自氢和C 1 -C 5烷基; n为1〜5的整数， 或该化合物的药学上可接受的盐; 下列通式（V）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基， C5烷氧基，C2-C5炔基，卤素，C1-C5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3选自氢和C 1 -C 5烷基; R 4选自氢和C 1 -C 5烷基; n为1〜5的整数， 或该化合物的药学上可接受的盐; 和下列通式（VI）的化合物：其中：R 1和R 2各自为一个或多个选自氢，C 1 -C 5烷基，C 2 -C 5烯基，C 3 -C 5环烷基，C 1 -C 5环烷基 C 5烷氧基，C 2 -C 5炔基，卤素，C 1 -C 5卤代烷基，烷基氨基，苯基，硝基和羧基; R 3和R 4各自独立地选自氢和C 1 -C 5烷基; n为1〜5的整数， 或该化合物的药学上可接受的盐。 还包含化合物III-VI的组合物以及所述化合物的用途。

    Benzhydryl derivatives having calmodulin inhibitor properties
    6.
    发明公开
    Benzhydryl derivatives having calmodulin inhibitor properties 失效
    二氯甲烷衍生物。

    公开(公告)号：EP0467435A2

    公开(公告)日：1992-01-22

    申请号：EP91201572.4

    申请日：1991-06-20

    申请人： Akzo Nobel N.V.

    发明人： Uilenstede, Patricia Caldirola ,  Mannhold, Raimund ,  Timmerman, Hendrik

    IPC分类号： C07C217/10 ,  C07C323/25

    CPC分类号： C07C211/28 ,  C07C211/27 ,  C07C217/10 ,  C07C323/25

    摘要： The invention relates to a benzhydryl derivative having the formula
    wherein each of the groups Ri, R 2 , and R 3 represents one to four substituents independently selected from the group consisting of hydrogen, lower alkyl, halogen, and CF 3 , and at least one of the groups Ri, R 2 , and R 3 is halogen or CF 3 ;

    R 4 represents hydrogen or methyl;
    n is 2, 3, or 4;
    m is 1, 2, or 3; and
    X represents O or S;
    or its pharmaceutically acceptable salts.

    The benzhydryl derivative of the invention can be used to treat patients who are suffering from diseases which are influenced by calmodulin.

    摘要翻译： 本发明涉及具有式CHEM的二苯甲基衍生物，其中R1，R2和R3各自表示1-4个独立地选自氢，低级烷基，卤素和CF 3的取代基，和至少一个 基团R 1，R 2和R 3是卤素或CF 3; R4代表氢或甲基; n为2,3或4; m为1,2或3; X表示O或S; 或其药学上可接受的盐。 本发明的二苯甲基衍生物可用于治疗患有受钙调素影响的疾病的患者。

    Phenethanolamine compounds
    7.
    发明公开
    Phenethanolamine compounds 失效
    苯酚胺化合物

    公开(公告)号：EP0422889A3

    公开(公告)日：1991-08-28

    申请号：EP90311043.5

    申请日：1990-10-09

    申请人： GLAXO GROUP LIMITED

    发明人： Evans, Brian

    IPC分类号： C07C217/10

    CPC分类号： C07C217/10

    摘要： The present invention provides the compound (R)-(-)-4-hydroxy-α¹-[[[6-(4-­phenylbutoxy)hexyl]amino]methyl]-1,3-benzenedimethanol or physiologically acceptable salts thereof, processes for its preparation, pharmaceutical formulations containing it, and its use in medicine.

    METHOD OF PREPARING INTERMEDIATE OF SALMETEROL
    8.
    发明公开
    METHOD OF PREPARING INTERMEDIATE OF SALMETEROL 审中-公开
    制备中间体SALMETEROL的方法

    公开(公告)号：EP3201171A1

    公开(公告)日：2017-08-09

    申请号：EP15847357.9

    申请日：2015-09-30

    申请人： Amphastar Nanjing Pharmaceuticals Inc.

    发明人： QIU, Yinhua ,  WU, Zhengyuan ,  CHEN, Song ,  ZHANG, Haoning

    IPC分类号： C07C213/08 ,  C07C213/10 ,  C07C217/10 ,  C07C217/28 ,  C07C217/40

    CPC分类号： C07D319/08 ,  C07C213/00

    摘要： A method of preparing an intermediate of salmeterol (Compound 1, 2-amino-1-(2,2-dimethyl-4H-1,3-benzodioxin-6-yl)ethanol) includes: reacting compound 2 with 2-methoxypropene in a first organic solvent to produce a reaction solution including compound 3, compound 2 including a 2-bromo precursor of Compound 1; reacting compound 3 with a nitrogen source to produce compound 4; reacting compound 4 with sodium borohydride in a second organic solvent to produce compound 5; and debenzylating compound 5 by ammonium formate/palladium-carbon catalytic transfer hydrogenation in a third organic solvent to produce Compound 1. A method of preparing salmeterol includes preparing Compound 1, and reacting Compound 1 to prepare salmeterol.

    摘要翻译： 制备沙美特罗中间体（化合物1,2-氨基-1-（2,2-二甲基-4H-1,3-苯并二恶英-6-基）乙醇）的方法包括：使化合物2与2-甲氧基丙烯在 第一有机溶剂中以产生包含化合物3，化合物2（包括化合物1的2-溴前体）的反应溶液; 使化合物3与氮源反应以产生化合物4; 使化合物4与硼氢化钠在第二有机溶剂中反应以产生化合物5; 并在第三有机溶剂中通过甲酸铵/钯 - 碳催化转移氢化将化合物5去苄基化以产生化合物1.制备沙美特罗的方法包括制备化合物1，并使化合物1反应以制备沙美特罗。