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    Piperidine derivatives and pharmaceutical compositions containing them
    93.
    发明授权
    Piperidine derivatives and pharmaceutical compositions containing them 失效
    哌啶衍生物和含有它们的药物组合物

    公开(公告)号：US4551465A

    公开(公告)日：1985-11-05

    申请号：US565902

    申请日：1983-12-27

    申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

    发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szabolcs Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Istvan Hajdu

    IPC分类号： C07D295/08 ,  A61K31/445 ,  A61P1/16 ,  A61P39/02 ,  A61P43/00 ,  C07D211/14 ,  C07D295/092 ,  C12N9/99

    CPC分类号： C07D295/088

    摘要： The invention relates to new piperidine derivatives of the formula (I) ##STR1## wherein R.sub.1 is halogen, trihalomethyl, alkyl having from one to 4 carbon atoms or alkoxy having from one to 4 carbon atoms; andR.sub.2 is hydrogen or alkyl having from one to 4 carbon atoms, and acid addition and quaternary ammonium salts thereof. According to another aspect of the invention there are provided processes for the preparation of these compounds. The compounds of the formula (I) are pharmacologically active. In particular, they inhibit the microsomal monooxigenase enzyme system of the liver. Pharmaceutical compositions containing them as active ingredient are also within the scope of the invention.

    摘要翻译： 本发明涉及式（I）的新的哌啶衍生物：其中R 1是卤素，三卤代甲基，具有1至4个碳原子的烷基或具有1至4个碳原子的烷氧基; 并且R 2为氢或具有1至4个碳原子的烷基，及其酸加成盐和季铵盐。 根据本发明的另一方面，提供了这些化合物的制备方法。 式（I）的化合物具有药理活性。 特别地，它们抑制肝脏的微粒体单致原子酶系统。 含有它们作为活性成分的药物组合物也在本发明的范围内。

    N-methyl substituted piperazino nitrobenzophenones and a process for the preparation thereof
    98.
    发明授权
    N-methyl substituted piperazino nitrobenzophenones and a process for the preparation thereof 失效
    N-甲基取代的哌嗪子基硝基二苯甲酮及其制备方法

    公开(公告)号：US3975390A

    公开(公告)日：1976-08-17

    申请号：US603854

    申请日：1975-08-12

    申请人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaholes Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

    发明人： Edit Toth ,  Jozsef Torley ,  Eva Palosi ,  Szaholes Szeberenyi ,  Laszlo Szporny ,  Sandor Gorog ,  Csilla Meszaros

    IPC分类号： C07D295/10 ,  C07D295/06

    CPC分类号： C07D295/10 ,  Y10S514/916

    摘要： New compounds of the general formula (I), ##SPC1##whereinR.sub.1 and R.sub.2 each stand for a saturated or unsaturated, straight-chained or branched alkyl group, an aralkyl group, a saturated or unsaturated cycloalkyl group or an aryl group, orR.sub.1 and R.sub.2 together with the adjacent nitrogen atom may form an optionally substituted heterocyclic group optionally containing a further oxygen or nitrogen hetero atom,But if R.sub.1 stands for methyl, R.sub.2 may only stand for a group other than methyl,Are prepared by reacting a compound of the general formula (II), ##SPC2##wherein X stands for halogen, with a secondary amine of the general formula (III),r.sub.1 --nh--r.sub.2 (iii)wherein R.sub.1 and R.sub.2 each have the same meanings as defined above.The new compounds of the general formula (I), as well as their pharmaceutical acceptable acid addition salts or quaternary ammonium salts are active primarily in the induction of liver microsomal enzyme, but they also possess antipyretic activity.

    摘要翻译： 通式（I）的新化合物，其中R 1和R 2各自表示饱和或不饱和的直链或支链烷基，芳烷基，饱和或不饱和环烷基或芳基，或R 1和R 2一起 相邻的氮原子可以形成任选地含有另外的氧或氮杂原子的任选取代的杂环基团，但是，R 1代表甲基，R 2可以仅代表甲基以外的基团，ARE通过反应通用化合物 （II），其中X代表卤素，具有通式（III）的仲胺，R1-NH-R2（III）其中R1和R2各自具有与上述相同的含义。

    Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof
    100.
    发明授权
    Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof 失效
    具有拮抗作用的血管紧张素-II类似物，其含有8位的酯基及其制备方法

    公开(公告)号：US4388304A

    公开(公告)日：1983-06-14

    申请号：US225048

    申请日：1981-01-14

    申请人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    发明人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07K7/06 ,  A61K38/00 ,  A61K38/08 ,  A61K38/55 ,  A61P9/12 ,  C07K7/14 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/14 ,  A61K38/00 ,  Y02P20/55 ,  Y10S530/80

    摘要： New octapeptides of the general formula (I),X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I)whereinX stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid,Y is the residue of an aliphatic amino acid, andA is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II),B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andA, X and Y are as defined above,are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex.The new compounds according to the invention possess angiotensin-II antagonizing effects, and can be used in the therapy to diagnose or treat hypertensive states.

    摘要翻译： 通式（I）的新八肽，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X代表N-甲基氨基酸的酰基或脂族 α-羟基或α-氨基氧基羧酸，Y是脂族氨基酸的残基，A是C 1-5烷基，使得通式（II）的保护的八肽衍生物的保护基， BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OA（II）其中B是通过酸解或催化氢化除去的基团，C是临时保护的基团 Arg部分的胍基，D为Tyr部分上芳香族羟基的临时保护基，E为His部分上咪唑基的临时保护基团，A，X和Y为 如上所定义的，可以逐步地或单步地去除。 如果需要，将通式（I）的化合物转化为其酸加成盐或药学上可接受的络合物。 根据本发明的新化合物具有血管紧张素-II拮抗作用，可用于诊断或治疗高血压状态的治疗。