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    Gonadoliberine analogues, process for preparing them, pharmaceutical composition and use
    12.
    发明公开
    Gonadoliberine analogues, process for preparing them, pharmaceutical composition and use 失效
    Gonadoliberinanaloga，Verfahren zu deren Herstellung，pharmazeutische Zusammensetzung und Anwendung。

    公开(公告)号：EP0220654A2

    公开(公告)日：1987-05-06

    申请号：EP86114532.4

    申请日：1986-10-21

    申请人： RICHTER GEDEON VEGYESZETI GYAR RT.

    发明人： Seprödi, János, Dr. ,  Teplán, István, Dr. ,  Schön, István, Dr. ,  Erchegyi, Judit, Dr. ,  Vadász, Zsolt ,  Kuprina Née Nyéki, Olga ,  Szirtes, Tamás ,  Selmeczi, András, Dr. ,  Kanyicska, Béla

    IPC分类号： C07K7/06 ,  A61K37/02

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S514/80

    摘要： The present invention relates to novel gonadoliberine analogues of formula I Glp-His-Trp-Ser-X-W-Leu-Arg-Pro-Y (I) wherein

    X stands for Phe-, Tyr or 3,5-dibromo-tyrosyl,
    W represents Asu or Asp OR , wherein R stands for alkyl having 1 to 6 carbon atoms or phenyl-or phenyl(alkyl having 1 to 4 carbon atoms), which latter two groups may optionally be substituted by nitro or one or more halogen atoms, and
    Y stands for glycinamide, aza-glycinamide or alkylamino having 1 to 4 carbon atoms, and acid-addition salts thereof, processes for preparing the same pharmaceutical compositions comprising the same, and use of the same in the preparation of a therapeutic agent having effect on the sexual processes.

    摘要翻译： 本发明涉及式I Glp-His-Trp-Ser-XW-Leu-Arg-Pro-Y（I）的新型性腺素类似物，其中X是Phe-，Tyr（3,5-3H）或3,5- 二溴 - 酪氨酰基，W是Asu或Asp OR，其中R是具有1至6个碳原子的烷基或苯基或苯基（具有1至4个碳原子的烷基），后两个基团可任选地被硝基或一个或多个卤素 原子，Y是甘氨酰胺，氮杂 - 甘氨酰胺或具有1至4个碳原子的烷基氨基，及其酸加成盐，其制备方法和包含其的药物组合物。 新化合物对性过程有影响。

    Nonapeptide and decapeptide analogs of LHRH, useful as LHRH agonists, and processes for their preparation
    13.
    发明公开
    Nonapeptide and decapeptide analogs of LHRH, useful as LHRH agonists, and processes for their preparation 失效
    九肽和LHRH作为LHRH激动剂有用的Decapeptidanaloge，以及它们的制备方法。

    公开(公告)号：EP0145258A1

    公开(公告)日：1985-06-19

    申请号：EP84307648.0

    申请日：1984-11-06

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nestor, John Joseph ,  Vickery, Brian Henry

    IPC分类号： C07K7/20 ,  A61K37/38

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

    摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula
    and the pharmaceutically acceptable salts thereof, wherein:

    A is tryptophyl, phenylalanyl, 3-(1-naphthyl)-L-alanyl or 3-(2-napthyl)-L-alanyl;
    B is tyrosyl, phenylalanyl, histidyl or 3-(1-pentafluorophenyl)-L-alanyl;
    C is an amino acyl residue selected from the radicals represented by the following structural formulas: a)
    wherein
    n is 1 to 5;
    R, is alkyl of 1 to 12 carbon atoms, -NRR 3 wherein R is hydrogen or alkyl of 1 to 4 carbon atoms, R 3 is hydrogen, alkyl of 1 to 12 carbon atoms, cycloalkyl, fluoroalkyl, phenyl, benzyl, ―(CH 2 ) n -morpholino or ―(CH 2 ) n N(R 4 ) 2 wherein n is 1 to 5 and R 4 is lower alkyl;
    R 2 is hydrogen or R 3 ; or R, and R 2 comprise a ring represented by the following structural formulas:
    wherein n is 1 to 7; A is hydrogen, alkyl of 1 to 6 carbon atoms or cycloalkyl; and X is halo or A or
    wherein R 5 is alkyl of 1 to 12 carbon atoms, benzyl, phenylethyl, cyclohexyl, cyclopentyl;
    and R 6 . R 7 and R 8 are hydrogen or alkyl of 1 to 4 carbon atoms; and n is the integer 2-5; or
    c) a substituent of the formula
    wherein R 9 is hydrogen, alkyl of 1 to 12 carbon atoms, phenyl or phenylloweralkyl;
    D is leucyl, isoleucyl, nor-leucyl, N-methyl-leucyl or tryptophanyl;
    E is arginyl, glutaminyl, tyrosyl or leucyl; and
    F is glycinamide or -NH-R 1 , wherein
    R 1 is lower alkyl, cycloalkyl, fluoro lower alkyl or -NR-CO-NH-R 2 wherein
    R 2 is hydrogen or lower alkyl.

    摘要翻译： 九肽和十肽LHRH的类似物具有下式... ...和其药学上可接受的盐，worin：...一个是色氨酰，苯丙氨酰基，3-（1-萘基）-L-丙氨酰基或3-（2-萘基） -L-丙氨酰基; ... B是酪氨酰基，苯丙氨酰基，组氨酰基或3-（1-五氟苯基）-L-丙氨酰基; ... C是从由以下结构式表示的自由基中的氨基酸酰基残基：... ... worin ... n为1至5; ... R 1是1至12个碳原子的烷基，-NRR3 worin R是氢或1至4个碳原子的烷基，R 3是氢，1〜12个碳原子，环烷基，氟烷基，苯基烷基 基，苄基， - （CH 2）N-吗啉代或 - （CH2）NN（R 4）2，其中n为1至5和R 4是低级烷基; R2是氢或R3 ...; 或者R1和R2包括由以下结构式表示的环：... ... worin n是1至7; A是氢，1至6个碳原子或环烷基烷基; 和X为卤素或A或... ... worin R5是1至12个碳原子，苄基，苯乙基，环己基，环戊基烷基; ...和R6，R7和R8是氢或1至4个碳原子的烷基; 和n是整数2-5; 或... C）下式的取代基... ... worin R9是氢，1〜12个碳原子，苯基或phenylloweralkyl烷基; ... D是亮氨酰，异亮，也不亮氨酰，N-甲基 - 亮氨酰或色氨; ... e是精氨酰，谷氨酰胺，酪氨酰或亮氨酰; 和... E是甘氨酸酰胺或NH-R <1>，... worinř<1>是低级烷基，环烷基，氟代低级烷基，或-NH-CO-NH-R <2> ... worinř<2>是氢或 低级烷基。

    Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists, methods of making them, and their pharmaceutical uses
    19.
    发明公开
    Nonapeptide and decapeptide analogs of LHRH, useful as LHRH antagonists, methods of making them, and their pharmaceutical uses 失效
    LHRH的九肽和十肽的类似物如LHRH拮抗剂，它们的制备和它们的药物用途。

    公开(公告)号：EP0049628A2

    公开(公告)日：1982-04-14

    申请号：EP81304597.8

    申请日：1981-10-05

    申请人： SYNTEX (U.S.A.) INC.

    发明人： Nester, John J. ,  Jones, Gordon H. ,  Vickery, Brian H.

    IPC分类号： C07K7/06 ,  A61K37/02

    CPC分类号： C07K7/23 ,  A61K38/00 ,  Y10S514/80 ,  Y10S930/13

    摘要： Nonapeptide and decapeptide analogs of LHRH which have the formula
    and the pharmaceutically acceptable salts thereof, wherein:

    X is a D-alanyl residue wherein one hydrogen on C-3 is replaced by:

    a) a carbocyclic aryl-containing radical selected from the group consisting of phenyl substituted with three or more straight chain lower alkyl groups, naphthyl, anthryl, fluorenyl, phenanthryl, biphenylyl and benzhydryl; or
    b) a saturated carbocyclic radical selected from the group consisting of cyclohexyl substituted with three or more straight chain lower alkyl groups, perhydronaphthyl, perhydrobiphenylyl, perhydro-2,2-diphenylmethyl, and adamantyl; or
    c) a heterocyclic aryl containing radical selected from the group consisting of radicals represented by the following structural formulas:

    wherein A" and A' are independently selected from the group consisting of hydrogen, lower alkyl, chlorine, and bromine, and G is selected from the group consisting of oxygen, nitrogen, and sulfur;
    A is an aminoacyl residue selected from the group consisting of L-pyroglutamyl, D-pyroglutamyl, N-acyl-L-prolyl, N-acyl-D-prolyl, N-acyl-D-tryptophanyl, N-acyl-D-phenylalanyl, N-acyl-D-p-halophenylalanyl, and N-acyl-X wherein X is as defined previously;
    B is an amino acyl residue selected from the group consisting of D-phenylalanyl, D-p-halophenylalanyl, 2,2-diphenylglycyl, and X wherein X is as defined previously;
    C is an amino acyl residue selected from the group consisting of L-tryptophanyl, D-tryptophanyl, D-phenylalanyl and X wherein X is as defined above;
    E is glycinamide or -NH-R 1 , wherein R 1 is lower alkyl, cycloalkyl, fluoro lower alkyl or


    R 2 is hydrogen or lower alkyl;

    are disclosed. These compounds are LHRH antagonists.