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    Peptides and processes for the manufacture thereof
    1.
    发明授权
    Peptides and processes for the manufacture thereof 失效
    肽及其制造方法

    公开(公告)号：US4316890A

    公开(公告)日：1982-02-23

    申请号：US129066

    申请日：1980-03-10

    申请人： Bruno Kamber ,  Hans Rink ,  Peter Sieber

    发明人： Bruno Kamber ,  Hans Rink ,  Peter Sieber

    IPC分类号： C07K14/575 ,  A61K38/00 ,  A61K38/04 ,  A61P5/00 ,  A61P5/02 ,  C07K1/113 ,  C07K14/655 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y10S930/16

    摘要： The somatostatin-analogous peptides according to the invention of the general formula ##STR1## in which Bmp represents the desaminocysteine radicalX represents Asn or His,trp represents D-Trp that may be substituted in the benzene ring by a halogen atom, andY represents the radical of a secondary .alpha.-amino acid having a maximum of 8 carbon atomsand the corresponding peptide amides and also acid addition salts and complexes thereof are distinguished by strong insulin-antagonistic and glucagon-antagonistic effects and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially also as antidiabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates and by the formation of the cystine disulphide bridge by means of oxidation.

    摘要翻译： 根据本发明的通式（IMAGE）的生长抑素类似物肽，其中Bmp表示脱氨基半胱氨酸基团X表示Asn或His，trp表示可在苯环中被卤素原子取代的D-Trp，Y表示 具有最多8个碳原子的次级α-氨基酸的基团和相应的肽酰胺及其酸加成盐和复合物的特征在于强的胰岛素拮抗作用和胰高血糖素拮抗作用，并且因此是治疗上可接受的，优选在 形式的药物制剂，类似于生长抑素的适应症，特别是抗糖尿病药。 该化合物通过肽合成的常规方法制备，特别是通过相应的受保护的中间体的释放和通过氧化形成胱氨酸二硫桥。

    Novel cyclopeptides
    2.
    发明授权
    Novel cyclopeptides 失效
    新型环肽

    公开(公告)号：US4238481A

    公开(公告)日：1980-12-09

    申请号：US942565

    申请日：1978-09-15

    申请人： Hans Rink ,  Bruno Kamber ,  Peter Sieber

    发明人： Hans Rink ,  Bruno Kamber ,  Peter Sieber

    IPC分类号： A61K38/00 ,  A61K38/04 ,  A61K38/22 ,  A61P5/00 ,  A61P5/02 ,  A61P43/00 ,  C07K1/113 ,  C07K5/097 ,  C07K7/06 ,  C07K7/56 ,  C07K14/575 ,  C07K14/655 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K5/0821 ,  C07K14/6555 ,  A61K38/00 ,  Y02P20/55 ,  Y10S514/806 ,  Y10S930/16

    摘要： Sulphur-free cyclopeptides with somatostatin-analogous aminoacid partial sequences, of the formula ##STR1## in which R is Asn, Ala or de-R, trp is D-Trp or L-Trp, which can be substituted in the benzene ring by halogen atoms or nitro groups, W is a free or etherified hydroxyl group or halogen atom present as a substituent on the benzene ring of the L-phenylalanine radical, or is hydrogen, X is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-X and Y is the radical of an .omega.-amino-lower alkane-(mono or di)-carboxylic acid or de-Y, and also acid addition salts and complexes thereof have biological properties similar to those of somatostatin and can be used, especially in the form of pharmaceutical preparations, for the treatment of excessive secretion of somatotropin, insulin and/or glucagon. The compounds according to the invention are obtained by cyclising a corresponding linear peptide compound in which the .epsilon.-amino group of the lysine radical and, if desired, also the hydroxyl group of the threonine radical are protected and detaching the protective groups which are present.

    摘要翻译： 具有生长抑素 - 类似氨基酸部分序列的无硫环肽，其中R为Asn，Ala或de-R，trp为式（I），其为可在苯中取代的D-Trp或L-Trp 卤素原子或硝基，W是在L-苯丙氨酸基团的苯环上作为取代基存在的游离的或醚化的羟基或卤素原子，或是氢，X是ω-氨基 - 低级烷烃的基团 - （单或二） - 羧酸或脱-X，Y是ω-氨基 - 低级烷烃 - （单或二） - 羧酸或脱Y的基团，并且其酸加成盐和络合物具有生物 特性与生长抑素相似，可用于治疗生长激素，胰岛素和/或胰高血糖素过度分泌的药物制剂形式。 根据本发明的化合物是通过环化相应的线性肽化合物而获得的，其中赖氨酸基团的ε-氨基和如果需要也保护苏氨酸基团的羟基并分离存在的保护基团。

    Process for the manufacture of peptides containing cystine
    3.
    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

    申请人： Bruno Kamber ,  Peter Sieber ,  Bernhard Riniker ,  Albert Hartmann ,  Werner Rittel

    发明人： Bruno Kamber ,  Peter Sieber ,  Bernhard Riniker ,  Albert Hartmann ,  Werner Rittel

    IPC分类号： A61K38/00 ,  C07C231/00 ,  C07K1/00 ,  C07K1/06 ,  C07K1/113 ,  C07K1/12 ,  C07K14/575 ,  C07K14/62 ,  C07C103/52 ,  A61K37/26 ,  C07G7/00

    CPC分类号： C07K1/00 ,  C07K1/067 ,  C07K14/62 ,  A61K38/00 ,  Y02P20/55

    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
    4.
    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

    申请人： Werner Rittel ,  Max Brugger ,  Bruno Kamber ,  Bernhard Riniker ,  Peter Sieber ,  Hendrik Marie Greven

    发明人： Werner Rittel ,  Max Brugger ,  Bruno Kamber ,  Bernhard Riniker ,  Peter Sieber ,  Hendrik Marie Greven

    IPC分类号： A61K38/00 ,  C07K14/585 ,  A61K37/00 ,  C07C103/52 ,  C07G7/00

    CPC分类号： C07K14/585 ,  A61K38/00 ,  Y10S514/807

    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 。

    Peptides and process for their manufacture
    6.
    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

    申请人： Werner Rittel ,  Max Brugger ,  Bruno Kamber ,  Bernhard Riniker ,  Peter Sieber ,  Hendrik M. Greven

    发明人： Werner Rittel ,  Max Brugger ,  Bruno Kamber ,  Bernhard Riniker ,  Peter Sieber ,  Hendrik M. Greven

    IPC分类号： A61K38/00 ,  C07K14/585 ,  C07C103/52

    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。

    Peptide derivatives
    7.
    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。

    Cyclopeptides and pharmaceutical preparations thereof and also processes for their manufacture
    8.
    发明授权
    Cyclopeptides and pharmaceutical preparations thereof and also processes for their manufacture 失效
    环肽及其药物制剂及其制备方法

    公开(公告)号：US4328214A

    公开(公告)日：1982-05-04

    申请号：US162712

    申请日：1980-06-25

    申请人： Hans Rink ,  Peter Sieber ,  Bruno Kamber

    发明人： Hans Rink ,  Peter Sieber ,  Bruno Kamber

    IPC分类号： A61K38/00 ,  C07K14/655 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K14/6555 ,  A61K38/00 ,  Y02P20/55 ,  Y10S514/806 ,  Y10S930/16

    摘要： The somatostatin-analogous cyclic octapeptides according to the invention of the general formula ##STR1## in which trp represents L-Trp or D-Trp, in which the benzene ring may be substituted by a halogen atom, andGaba(Ar) represents the residue of a .gamma.-aminobutyric acid substituted by a cyclic hydrocarbyl radical,and their acid addition salts and complexes are distinguished by a strong inhibition of the insulin and glucagon secretion of the pancreas and are therefore therapeutically acceptable, preferably in the form of pharmaceutical preparations, in similar indications to those of somatostatin, especially as anti-diabetics. The compounds are manufactured by conventional processes of peptide synthesis, especially by liberation from corresponding protected intermediates after intramolecular cyclization of a corresponding linear octapeptide.

    摘要翻译： 根据本发明的通式（I）的生长抑素类似环状八肽，其中trp表示其中苯环可被卤素原子取代的L-Trp或D-Trp，Gaba（Ar） 表示由环状烃基取代的γ-氨基丁酸的残基，并且它们的酸加成盐和复合物的特征在于对胰腺的胰岛素和胰高血糖素分泌的强烈抑制，因此是治疗上可接受的，优选以药物形式 制剂，类似于生长抑素的适应症，特别是抗糖尿病药。 通过肽合成的常规方法制备化合物，特别是通过相应的线性八肽在分子内环化后从相应的受保护的中间体释放。

    Dihydro pyridine compounds, compositions and use
    10.
    发明授权
    Dihydro pyridine compounds, compositions and use 失效
    二氢吡啶化合物，组成和用途

    公开(公告)号：US4616002A

    公开(公告)日：1986-10-07

    申请号：US816461

    申请日：1986-01-06

    申请人： Bruno Kamber ,  Thomas Leutert ,  Hans Kuhnis ,  Kurt Eichenberger

    发明人： Bruno Kamber ,  Thomas Leutert ,  Hans Kuhnis ,  Kurt Eichenberger

    IPC分类号： C07D211/90 ,  C07D401/06 ,  C07D405/12 ,  C07D417/12 ,  C07K5/065 ,  A61K31/535 ,  A61K37/02 ,  C07D413/12 ,  C07K5/06

    CPC分类号： C07D401/06 ,  C07D211/90 ,  C07D405/12 ,  C07D417/12 ,  C07K5/06078

    摘要： Compounds of the formula I ##STR1## in which n represents 1, 2 or 3, Ar represents a carbocyclic or heterocyclic aryl radical, Ac represents the acyl radical of an acid, Z represents a radical --OR.sub.7 or --NR.sub.8 R.sub.9, R.sub.1 represents hydrogen, unsubstituted or substituted lower alkyl, a carbocyclic or heterocyclic aryl radical or free, etherified or esterified hydroxy, R.sub.2 and R.sub.3, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl, formyl or functionally modified formyl, carboxy or functionally modified carboxy, a carbocyclic or heterocyclic aryl radical or unsubstituted or mono- or di-substituted amino, R.sub.4 represents hydrogen or lower alkyl, R.sub.5 and R.sub.6, independently of one another, each represents hydrogen, unsubstituted or substituted lower alkyl or a carbocyclic or heterocyclic aryl radical, R.sub.7, R.sub.8 and R.sub.9, independently of one another, each represents hydrogen, unsubstituted or substituted alkyl or a carbocyclic or heterocyclic aryl radical; in which R.sub.1 and R.sub.2 together or R.sub.1 and R.sub.3 together may represent unsubstituted or substituted lower alkylene in which a carbon atom is optionally replaced by a hetero atom, in which R.sub.4 and R.sub.5 together, and likewise R.sub.5 and R.sub.6 together and/or R.sub.8 and R.sub.9 together, independently of one another, may represent unsubstituted or substituted lower alkylene in which a carbon atom may have been replaced by a hetero atom, optical isomers of compounds of the formula I, mixtures of these optical isomers and salts of such compounds that have a salt-forming grouping, are distinguished by cardiovascular, especially blood pressure-reducing, properties. They are manufactured in a manner known per se.

    摘要翻译： 式I的化合物（I）其中n表示1,2或3，Ar表示碳环或杂环芳基，Ac表示酸的酰基，Z表示基团-OR7或-NR8R9，R1 代表氢，未取代或取代的低级烷基，碳环或杂环芳基或游离的醚化或酯化的羟基，R 2和R 3彼此独立地表示氢，未取代或取代的低级烷基，甲酰基或官能改性的甲酰基，羧基或 官能改性的羧基，碳环或杂环芳基或未取代的或单取代或二取代的氨基，R 4表示氢或低级烷基，R 5和R 6彼此独立地表示氢，未取代或取代的低级烷基或碳环或 杂环芳基，R 7，R 8和R 9彼此独立地表示氢，未取代或取代的烷基或碳环或杂环芳基; 其中R 1和R 2一起或R 1和R 3一起可以表示未取代或取代的低级亚烷基，其中碳原子任选被杂原子取代，其中R 4和R 5一起以及R 5和R 6一起和/或R 8和R 9 一起彼此独立地表示未取代或取代的低级亚烷基，其中碳原子可以被杂原子取代，式I化合物的光学异构体，这些光学异构体的混合物和这些化合物的盐，其具有 盐形成分组由心血管特别是降血压特性区分。 它们以本身已知的方式制造。