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    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them
    1.
    发明授权
    N-substituted isoquinoline derivatives and pharmaceutical compositions containing them 失效
    N-取代的异喹啉衍生物和含有它们的药物组合物

    公开(公告)号：US4668688A

    公开(公告)日：1987-05-26

    申请号：US664770

    申请日：1984-10-25

    申请人： Gabor Bernath ,  Jeno Kobor ,  Ferenc Fulop ,  Pal Perjesi ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    发明人： Gabor Bernath ,  Jeno Kobor ,  Ferenc Fulop ,  Pal Perjesi ,  Elemer Ezer ,  Gyorgy Hajos ,  Eva Palosi ,  Laszlo Denes ,  Laszlo Szporny

    IPC分类号： A61K31/47 ,  A61K31/472 ,  A61P1/04 ,  A61P25/04 ,  A61P29/00 ,  A61P37/06 ,  C07D217/16

    CPC分类号： C07D217/16

    摘要： The invention relates to new N-substituted bis(hydroxymethyl)-methyl-isoquinoline derivatives of the formula (I), ##STR1## wherein R.sup.1 and R.sup.2 represent hydroxyl or alkoxy having from 1 to 6 carbon atoms,the dotted line is an optional double bond in the 1,2-position,R.sup.3 is alkyl having from 1 to 6 carbon atoms or aralkyl containing from 1 to 4 carbon atoms in the alkyl moiety, or--if there is a single bond in the 1,2-position--represents a group of the formula ##STR2## in which X is oxygen ifR.sup.4 is alkyl having from 1 to 5 carbon atoms, alkoxy having from 1 to 4 carbon atoms, hydroxyl, phenyl or substituted phenyl; orX is oxygen or sulfur ifR.sup.4 is an --NH.sub.2, --NH--C.sub.1-4 -alkyl, --NH--C.sub.3-6 -cycloalkyl, --NH-phenyl or --NH--C.sub.1-4 -alkyl-phenyl group; andR.sup.5 and R.sup.6 independently stand for hydrogen, alkyl having from 1 to 4 carbon atoms or phenyl, with the proviso that at least one of them is other than phenyl,and salts thereof. Processes for the preparation of these compounds and pharmaceutical compositions are also within the scope of the invention.

    摘要翻译： 本发明涉及式（I）的新的N-取代双（羟甲基） - 甲基 - 异喹啉衍生物，其中R1和R2代表羟基或具有1-6个碳原子的烷氧基，虚线是 在1,2-位上的任选的双键，R3是具有1至6个碳原子的烷基或在烷基部分含有1至4个碳原子的芳烷基，或 - 如果1,2-二烷基中存在单键， 位置 - 表示如果R 4是具有1至5个碳原子的烷基，具有1至4个碳原子的烷氧基，羟基，苯基或取代的苯基，其中X是氧的式“IMAGE”的基团; 如果R 4是-NH 2，-NH-C 1-4 - 烷基，-NH-C 3-6 - 环烷基，-NH-苯基或-NH-C 1-4 - 烷基 - 苯基，则X是氧或硫; 并且R 5和R 6独立地代表氢，具有1至4个碳原子的烷基或苯基，条件是它们中的至少一个不是苯基，及其盐。 用于制备这些化合物和药物组合物的方法也在本发明的范围内。

    2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines
    7.
    发明授权
    2,3-Polymethylene-4-oxo-4H-pyrido[1,2-a]pyrimidines 失效
    2,3-二亚甲基-4-氧代-4H-吡啶并[1,2-a]嘧啶

    公开(公告)号：US4220771A

    公开(公告)日：1980-09-02

    申请号：US935071

    申请日：1978-08-18

    申请人： Istvan Hermecz ,  Ferenc Fulop ,  Zoltan Meszaros ,  Gabor Bernath ,  Jozsef Knoll

    发明人： Istvan Hermecz ,  Ferenc Fulop ,  Zoltan Meszaros ,  Gabor Bernath ,  Jozsef Knoll

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61K31/55 ,  A61P7/02 ,  A61P9/10 ,  A61P11/00 ,  A61P25/04 ,  A61P29/00 ,  A61P31/04 ,  A61P43/00 ,  C07D471/04 ,  C07D487/04 ,  C07D487/14

    CPC分类号： C07D471/04 ,  C07D487/04

    摘要： Pharmaceutical intermediates, morphine potentiators and other compounds have the formula ##STR1## wherein R is hydrogen, halogen, C.sub.1-4 alkyl, hydroxy, nitro, amino, carboxy or a carboxylic acid derivate radical, R.sup.1 is hydrogen or a C.sub.1-4 alkyl, R.sup.2 is hydrogen or C.sub.1-4 alkyl, R.sup.3 is hydrogen, R.sup.4 is hydrogen or C.sub.1-4 alkyl, R.sup.5 is hydrogen R.sup.6 is hydrogen or R.sup.3 and R.sup.4 and/or R.sup.5 and R.sup.6 form a chemical bond, X is oxygen or imino, m is 1, 2, 3 or 4, n is 0, 1, 2 or 3, and if n is 1, then the dotted lines can stand for bonds, with the proviso that if m=1 and n=1 and if in the 2,3-, 6,7-, 8,9- and 1,10-positions double bonds are present, and R.sup.1 and R.sup.2 are hydrogen, then R is other than 9-hydroxy or 9-methyl; if m=2 and n=1 and R.sup.2 is hydrogen, then at least one of R and R.sup.1 is other than hydrogen; and if m=2 and n=2 and R.sup.2 is hydrogen and the molecule is a 2,3,4,6,7,8,9,10-octahydro derivative, then at least one of R and R.sup.1 is other than hydrogen or an acid-addition or quaternary salt thereof.

    摘要翻译： 药物中间体，吗啡增效剂和其它化合物具有式“IMAGE”，其中R是氢，卤素，C 1-4烷基，羟基，硝基，氨基，羧基或羧酸衍生物基团，R 1是氢或C 1-4烷基， R2是氢或C1-4烷基，R3是氢，R4是氢或C1-4烷基，R5是氢R6是氢或R3和R4和/或R5和R6形成化学键，X是氧或亚氨基，m 是1,2,3或4，n是0,1,2或3，如果n是1，则虚线可以代表键，条件是如果m = 1且n = 1，如果在 存在2,3,6,7,8,9和1,10-位双键，R1和R2是氢，则R不是9-羟基或9-甲基; 如果m = 2且n = 1且R2是氢，则R和R1中的至少一个不是氢; 并且如果m = 2且n = 2且R 2是氢并且该分子是2,3,4,6,7,8,9,10-八氢衍生物，则R和R 1中的至少一个不是氢或 其加酸或季盐。

    Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds
    10.
    发明申请
    Chiral Cyclic Beta-Amino Acids and their Derivatives, Pharmaceutical Compositions Containing Them and the Use of Such Compounds 有权
    手性环状β-氨基酸及其衍生物，含有这些化合物及其使用的药物组合物

    公开(公告)号：US20100081717A1

    公开(公告)日：2010-04-01

    申请号：US12513369

    申请日：2007-11-14

    申请人： Ferenc Fulop ,  Zsolt Szakonyi

    发明人： Ferenc Fulop ,  Zsolt Szakonyi

    IPC分类号： A61K31/195 ,  C07C229/00

    CPC分类号： C07C335/18 ,  C07B2200/07 ,  C07C215/42 ,  C07C229/50 ,  C07C271/24 ,  C07C275/30 ,  C07C275/34 ,  C07C335/14 ,  C07C2602/42 ,  C07C2603/18 ,  C07D205/12

    摘要： The invention relates to chiral cyclic β-amino acids of Formula (I) and their salts formed with pharmaceutically acceptable acids or bases, wherein the main meanings of the substituents are as follows: R stands for C1-4 Alk; X stands for —COOH, —CONH2, —CONH(C1-4 Alk), —CON(C1-4 Alk)2, —COO(C1-4 Alk), —COPhe-O-(C1-4 Alk) or —CH2OH; Y stands for —NH2, —NHBoc, —NHFmoc, —NH(C1-4 Alk), —N(C1-4 Alk)2, —NHCH2Ph, or Ar—NH—C(=X0)—N(R0)— wherein Ar stands for a phenyl group substituted by C1-4 alkoxy or halogen, X0 stands for O or S, and R0 stands for hydrogen or benzyl; and X+Y stands for —CONH— vagy —CON(Boc)-; with the proviso that when X stands for —COOH, then Y may be only different from —NH2. The invention also relates to pharmaceutical compositions having multidrug-resistance reversing effect that contain one or more compound(s) of Formula (I) or a salt thereof and inert pharmaceutical carriers and/or auxiliary agents. The invention also relates to carboxylic acids of Formula (XX) and their salts.

    摘要翻译： 本发明涉及式（I）的手性环状 - 氨基酸及其与药学上可接受的酸或碱形成的盐，其中取代基的主要含义如下：R代表C1-4烷基; X代表-COOH，-CONH 2，-CONH（C 1-4 Alk），-CON（C 1-4 Alk）2，-COO（C 1-4 Alk），-C OPhe-O-（C 1-4 Alk）或 - CH2OH; Y代表-NH2，-NHBoc，-NHFmoc，-NH（C1-4 Alk），-N（C1-4 Alk）2，-NHCH2Ph或Ar-NH-C（= X0）-N（R0） - 其中Ar表示被C 1-4烷氧基或卤素取代的苯基，X 0表示O或S，R 0表示氢或苄基; 而X + Y代表-CON​​H- vagy -CON（Boc） - ; 条件是当X代表-COOH时，则Y可以仅与-NH 2不同。 本发明还涉及含有一种或多种式（I）化合物或其盐和惰性药物载体和/或辅助剂的具有多重耐药性逆转作用的药物组合物。 本发明还涉及式（XX）的羧酸及其盐。