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15 条记录 (耗时 0.037 秒)

    Peptide derivatives
    5.
    发明授权
    Peptide derivatives 失效
    肽衍生物

    公开(公告)号：US4439425A

    公开(公告)日：1984-03-27

    申请号：US385594

    申请日：1982-06-07

    申请人： Lajos Tarcsay ,  Bruno Kamber ,  Jaroslav Stanek ,  Gerhard Baschang ,  Albert Hartmann

    发明人： Lajos Tarcsay ,  Bruno Kamber ,  Jaroslav Stanek ,  Gerhard Baschang ,  Albert Hartmann

    IPC分类号： C07K1/113 ,  A61K38/00 ,  A61P37/04 ,  C07J41/00 ,  C07K5/083 ,  C07K5/103 ,  C07K7/06 ,  C07K14/245 ,  A61K37/00

    CPC分类号： C07K7/06 ,  C07K14/245 ,  C07K5/081 ,  C07K5/1013 ,  A61K38/00

    摘要： The present invention relates to new lipopeptides and in particular to compounds of either of the formulae ##STR1## wherein R.sub.1 and R.sub.2 each represent a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical which has 11-21 C atoms and which is also optionally substituted by oxygen functions, R.sub.3 represents hydrogen or the radical R.sub.1 --CO--O--CH.sub.2 --, where R.sub.1 has the same meaning, R.sub.1 ' is a saturated or unsaturated aliphatic hydrocarbon radical of at least 9 C atoms, which is optionally substituted at one of the C atoms non adjacent to the sulfur atom by a free hydroxyl group or a hydroxyl group esterified with a monobasic carboxylic acid and which is optionally interrupted in the C atoms chain by one or more oxygen atoms, and which hydrocarbon is optionally substituted by a maximum of 2 cycloaliphatic hydrocarbon radicals having 5-8 ring C atoms, or R.sub.1 ' is the radical --CO--R.sub.1 ", wherein R.sub.1 " represents a saturated or unsaturated aliphatic or mixed aliphatic-cycloaliphatic hydrocarbon radical of 11-21 C-atoms and which is optionally interrupted in the C atoms chain by oxygen atoms, and X represents an amino acid with free esterified or amidated carboxyl group, or an amino acid sequence of 2-10 aliphatic amino acids, the terminal carboxyl group of which is free or in the ester or amide form, the amino acids being naturals ones in the case of compounds of formula (1).

    摘要翻译： 本发明涉及新的脂肽，特别是涉及式（I）* = R ** = R或S或R / S中的任一个的化合物（I'）n = 1,2 * = R / S或R或S，其中R 1和R 2各自表示饱和或不饱和的具有11-21个C原子的脂族或混合的脂族 - 脂环族烃基，并且也可任选被氧官能团取代，R 3表示氢或基团R 1 - CO-O-CH 2 - ，其中R 1具有相同的含义，R 1'是至少9个C原子的饱和或不饱和脂族烃基，其任选地在不与硫原子相邻的C原子之一被自由基 羟基或用一元羧酸酯化的羟基，其任选地在C原子链中被一个或多个氧原子中断，并且该烃任选被具有5-8个环C原子的最多2个脂环族烃基取代 ，或者R1'是-CO-R1“基团，其中R1”表示 是11-21个C原子的饱和或不饱和脂族或混合脂族 - 脂环族烃基，其任选在C原子链中被氧原子中断，X表示具有游离酯化或酰胺化羧基的氨基酸，或 2-10脂肪族氨基酸的氨基酸序列，其末端羧基是游离的或呈酯或酰胺形式，氨基酸在式（1）化合物的情况下是天然的。

    Muramyl peptides and processes for their manufacture
    6.
    发明授权
    Muramyl peptides and processes for their manufacture 失效
    胞壁酰多肽及其制造方法

    公开(公告)号：US4548923A

    公开(公告)日：1985-10-22

    申请号：US608911

    申请日：1984-05-09

    申请人： Albert Hartmann ,  Oskar Wacker ,  Gerhard Baschang ,  Lajos Tarcsay

    发明人： Albert Hartmann ,  Oskar Wacker ,  Gerhard Baschang ,  Lajos Tarcsay

    IPC分类号： A61K38/00 ,  A61K38/14 ,  A61K38/17 ,  A61P31/12 ,  A61P35/00 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  A61K37/00 ,  C07D333/32

    CPC分类号： C07K9/005

    摘要： The compounds of the formula I ##STR1## in which each of R.sup.1, R.sup.4 and R.sup.6, independently of the others, represents hydrogen or lower alkanoyl, R.sup.2 represents C.sub.1-4 -alkyl, hydroxymethyl or phenyl, R.sup.3 represents hydrogen or methyl, R.sup.5 represents hydrogen or C.sub.1-3 -alkyl, R.sup.7 represents C.sub.1-3 -alkyl that is unsubstituted or substituted by hydroxy, mercapto or methylthio, R.sup.8 represents hydrogen or lower alkyl, X represents oxygen or the group NH, Y represents C.sub.1-4 -alkylidene, and each of R.sup.9 and R.sup.10, independently of the other, represents C.sub.11-17 -alkyl or C.sub.11-17 -alkenyl, and their salts, have an immunostimulating activeity.

    摘要翻译： R 1，R 4和R 6各自独立地表示氢或低级烷酰基，R 2表示C 1-4 - 烷基，羟甲基或苯基，R 3表示 氢或甲基，R 5表示氢或C 1-3 - 烷基，R 7表示未被取代或被羟基，巯基或甲硫基取代的C 3-烷基，R 8表示氢或低级烷基，X表示氧或NH基，Y表示 C 1-4 - 亚烷基，R 9和R 10各自独立地表示C 11-17 - 烷基或C 11-17-链烯基及其盐具有免疫刺激活性。

    Phosphoryl compounds, pharmaceutical preparations containing such compounds, and their use
    9.
    发明授权
    Phosphoryl compounds, pharmaceutical preparations containing such compounds, and their use 失效
    磷酰化合物，含有这些化合物的药物制剂及其用途

    公开(公告)号：US4423038A

    公开(公告)日：1983-12-27

    申请号：US340680

    申请日：1982-01-19

    申请人： Gerhard Baschang ,  Albert Hartmann ,  Oskar Wacker ,  Lajos Tarcsay

    发明人： Gerhard Baschang ,  Albert Hartmann ,  Oskar Wacker ,  Lajos Tarcsay

    IPC分类号： A61K39/39 ,  A61P31/04 ,  A61P37/00 ,  C07K1/113 ,  C07K9/00 ,  C07K14/52 ,  C07K14/53 ,  C07K14/535 ,  A61K37/02 ,  C07C103/52

    CPC分类号： C07K9/005

    摘要： There are described hexopyranose compounds of the formula I and salts thereof having immunomodulatory action, which can be used, for example, in the form of pharmaceutical preparations, and also together with antibiotics, and processes for their manufacture. ##STR1## The variables are as described in the disclosure. The invention relates to the above-mentioned compounds as immunomodulators, especially as immunostimulants, their use as pharmacologically active substances, especially their use as immunomodulators, particularly as immunostimulants, and their use for the manufacture of pharmaceutical preparations, and to pharmaceutical preparations containing these compounds.

    摘要翻译： 描述了式I的六价吡喃糖化合物及其具有免疫调节作用的盐，其可以例如以药物制剂的形式使用，并且还与抗生素一起使用，以及其制备方法。 （I）变量如本公开所述。 本发明涉及作为免疫调节剂的上述化合物，特别是作为免疫刺激剂，其作为药理活性物质的用途，特别是其作为免疫调节剂，特别是作为免疫刺激剂的用途，以及其用于制备药物制剂的用途以及含有这些化合物的药物制剂 。

    Novel phosphorylmuramyl peptides and processes for the manufacture thereof
    10.
    发明授权
    Novel phosphorylmuramyl peptides and processes for the manufacture thereof 失效

    公开(公告)号：US4409209A

    公开(公告)日：1983-10-11

    申请号：US327381

    申请日：1981-12-04

    申请人： Gerhard Baschang ,  Lajos Tarcsay ,  Albert Hartmann ,  Jaroslav Stanek

    发明人： Gerhard Baschang ,  Lajos Tarcsay ,  Albert Hartmann ,  Jaroslav Stanek

    IPC分类号： C07K9/00 ,  A61K37/00

    CPC分类号： C07K9/005

    摘要： Phosphorylmuramyl peptides of the formula ##STR1## are immuno-potentiating. In the formula, R.sub.1 represents optionally substituted alkyl or aryl, R.sub.2, R.sub.4, R.sub.6 and R.sub.7 represent, for example, hydrogen, R.sub.3 represents hydrogen or lower alkyl, R.sub.5 represents, for example, hydrogen, lower alkyl, hydroxy-lower alkyl, amino-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, aryl or aralkyl, or nitrogen-containing heterocyclyl or heterocyclyl-lower alkyl, and one of the radicals A.sub.1 and A.sub.2 represents a radical of the formula (II) ##STR2## In the formula (II), T represents NH or O, Y represents an optionally substituted alkylene group, which may also be interrupted by one or two oxycarbonyl and/or iminocarbonyl groups, and W represents an aliphatic radical or a cycloalkyl or cycloalkenyl radical having more than 6 carbon atoms. The other of the radicals A.sub.1 and A.sub.2 represents free or etherified hydroxy, amino, lower alkylamino or aminocarbonyl-lower alkylamino.