Peptides and process for their manufacture
    1.
    发明授权
    Peptides and process for their manufacture 失效
    肽及其制造方法

    公开(公告)号:US4159981A

    公开(公告)日:1979-07-03

    申请号:US842122

    申请日:1977-10-04

    CPC分类号: C07K14/585 A61K38/00

    摘要: The new hypocalcaemically active peptides of formula I ##STR1## and corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.

    摘要翻译: 式I的新的低活性活性肽GlyThrTyrThrGlnAspPheAsnLysPhe HisThrPheProGlnThrAlaGleVal GlyAlaProOH和其中一个或多个天冬酰胺和谷氨酸基团被天冬氨酸或谷氨酸基团和/或天冬氨酸基团代替的相应化合物被替换为 天冬酰胺基团,它们的二聚体,特别是其中2个相同的肽序列(1-32和1'-32')通过半胱氨酸自由基1,7'和7,1'以反平行布置连接的那些,借助于 二硫键和衍生物可用作低钙血症药物,并且通过分离保护至少一个氨基或一个羧基的基团或将相应的硫化物氧化成二硫化物或将其合并在一起而制备。

    Process for the manufacture of peptides containing cystine
    4.
    发明授权
    Process for the manufacture of peptides containing cystine 失效
    制造含有胱氨酸的肽的方法

    公开(公告)号:US3994871A

    公开(公告)日:1976-11-30

    申请号:US471617

    申请日:1974-05-20

    摘要: Process for the manufacture of peptides which contain more than one disulphide bond characterized in that in one or two aminoacid sequences containing cysteine, in which disulphide bonds are to be produced, two cysteine radicals which are to be linked are protected by a mercapto-protective group R.sub.1 of the aralkyl type, two further cysteine radicals are protected by an acylaminomethyl group R.sub.2, the protective groups R.sub.1 are removed by treatment with iodine in the presence of a polyhalogenated lower aliphatic hydroxy compound or oxo compound, or a corresponding lower alkanoic acid lower alkyl ester, at the same time forming the disulphide bond between these cysteine radicals, which are protected by R.sub.1, and at any desired point after removal of the polyhalogenated compound the second disulphide bridge is formed in the usual manner.

    摘要翻译: 用于制造含有多于一个二硫键的肽的方法,其特征在于在含有半胱氨酸的一个或两个氨基酸序列中,其中将产生二硫键,待连接的两个半胱氨酸基团被巯基保护基团保护 芳烷基类型的R1,两个另外的半胱氨酸基团被酰氨基甲基R2保护,保护基R1在多卤化低级脂族羟基化合物或氧代化合物或相应的低级链烷酸低级烷基存在下用碘处理除去 酯,同时形成由R1保护的这些半胱氨酸基团之间的二硫键,并且在去除多卤代化合物之后的任何所需点,以通常的方式形成第二二硫桥。

    N-acyl and desamino human calcitonin and analogs thereof
    5.
    发明授权
    N-acyl and desamino human calcitonin and analogs thereof 失效
    N-酰基和去氨基人降钙素及其类似物

    公开(公告)号:US3934008A

    公开(公告)日:1976-01-20

    申请号:US271873

    申请日:1972-07-14

    摘要: The new hypocalcaemically active peptides of formula Ih-cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Thr-Gln-Asp-Phe-Asn-Lys-Phe-His-Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-val-Gly-Ala-Pro-OHand corresponding compounds in which one or more of the asparagine and glutamic acid radicals are replaced by the aspartic acid or glutamic acid radical and/or the aspartic acid radical is replaced by the asparagine radical, their dimers, especially those in which 2 identical peptide sequences (1-32 and 1'-32') are joined in an anti-parallel arrangement via the cysteine radicals 1,7' and 7,1' by means of a disulfide bond, and derivatives are useful as hypocalcaemic agents and are prepared by splitting off groups protecting at least one amino or one carboxyl group or oxidizing the corresponding sulfides to the disulfides or condensing together adequate peptides.

    摘要翻译: 式I H-Cys-Gly-Asn-Leu-Ser-Thr-Cys-Met-Leu-Gly-Thr-Tyr-Thr-Gln-Asp-Phe-Asn-Lys-Phe-His-的新的低血清活性肽 Thr-Phe-Pro-Gln-Thr-Ala-Ile-Gly-val-Gly-Ala-Pro-OH和其中一个或多个天冬酰胺和谷氨酸基被天冬氨酸或谷氨酸基团代替的相应化合物 特别是其中2个相同的肽序列(1-32和1'-32')通过半胱氨酸自由基1以反平行排列连接的那些,天冬酰胺基团和/或天冬氨酸基团被天冬酰胺基团替代, 7'和7,1',并且衍生物可用作低钙血症药物,并且通过分离保护至少一个氨基或一个羧基的基团或将相应的硫化物氧化成二硫化物或将其合并在一起而制备足够的肽 。

    Protected amino acids and process for the preparation thereof
    6.
    发明授权
    Protected amino acids and process for the preparation thereof 失效
    受保护的氨基酸及其制备方法

    公开(公告)号:US5324833A

    公开(公告)日:1994-06-28

    申请号:US509102

    申请日:1990-04-13

    摘要: Compounds of the formula I, ##STR1## in which 'R.sub.1 is an amino protective group, and n stands for 1 or 2, R.sub.1 denotes hydrogen or an amino protective group, R.sub.2 denotes hydrogen or a carboxyl protective group and R.sub.3 denotes triphenylmethyl, 4-monomethoxy-trityl or 4,4'-dimethoxy-trityl, and reactive carboxylic acid derivatives of such compounds of the formula I in which R.sub.2 stands for hydrogen, are described.These compounds can be used as starting materials for the preparation of peptides. They are more suitable for this than are analogous compounds of the formula I in which R.sub.3 denotes hydrogen or one of the carbamoyl protective groups hitherto customary.

    摘要翻译: 式Ⅰ化合物,其中R1为氨基保护基,n为1或2,R1为氢或氨基保护基,R2为氢或羧基保护基,R3为 三苯基甲基,4-单甲氧基 - 三苯甲基或4,4'-二甲氧基三苯甲基,以及其中R2代表氢的式Ⅰ化合物的反应性羧酸衍生物。 这些化合物可以用作制备肽的起始材料。 它们比类似的式I化合物更适合于其中,R3表示氢或迄今为止常用的氨基甲酰基保护基之一。

    Substituted tetrapeptides
    10.
    发明授权
    Substituted tetrapeptides 失效
    取代四肽

    公开(公告)号:US4595677A

    公开(公告)日:1986-06-17

    申请号:US554735

    申请日:1983-11-23

    摘要: Tetrapeptides of the formula I, ##STR1## in which R.sup.1 represents hydrogen or acyl, R.sup.2 represents alkyl or aralkyl, R.sup.3 represents free or functionally modified hydroxy, R.sup.4 represents free or substituted amino or free or etherified hydroxy, and -Pro-, -Phe- and -His- respectively represent the bivalent radicals of the amino acids proline, phenylalanine and histidine or the (D)-isomers thereof, salts of such compounds having salt-forming groups, and processes for their manufacture.The compounds inhibit the action of the enzyme renin and can be used as antihypertensives and for the treatment of cardiac insufficiency.

    摘要翻译: 式I的四肽,其中R 1表示氢或酰基,R 2表示烷基或芳烷基,R 3表示游离或官能改性的羟基,R 4表示游离或取代的氨基或游离的或醚化的羟基,和-Pro- ,-Phe-和-His-分别表示氨基酸脯氨酸,苯丙氨酸和组氨酸或其(D)异构体的二价基团,这些具有成盐基团的化合物的盐及其制备方法。 该化合物抑制酶肾素的作用,可用作抗高血压药物和治疗心功能不全。