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    Organic compounds
    2.
    发明授权
    Organic compounds 失效
    有机化合物

    公开(公告)号：US4120852A

    公开(公告)日：1978-10-17

    申请号：US575156

    申请日：1975-05-07

    Applicant: Wilfried Bauer ,  Janos Pless

    Inventor： Wilfried Bauer ,  Janos Pless

    IPC: C07K7/08 ,  A61K38/00 ,  C07K14/575 ,  C07K14/655 ,  C07C103/52 ,  A61K37/00

    CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/26

    Abstract: This invention provides new compounds of formula I, ##STR1## wherein X is H-Ala, D-Ala, .beta.-Ala, propionyl or Ac-Ala (wherein Ac is pharmaceutically acceptable acyl),Y is hydrogen or a direct bond between the sulphur atoms in positions 3 and 14, andZ is the radical --COOH, --COOR.sub.1 (wherein R.sub.1 is lower alkyl), ##STR2## (wherein R.sub.2 and R.sub.3 independently are hydrogen or lower alkyl) or --CH.sub.2 OH,with the proviso that X is other than H-Ala, when Z is COOH.useful as agents for the treatment of Diabetes Mellitus, acromegaly and angiopathy.

    Abstract translation: 本发明提供了新的式I化合物，其中X为H-Ala，D-Ala，β-Ala，丙酰或Ac-Ala（其中Ac为药学上可接受的酰基），Y为氢或 位置3和14之间的硫原子之间的直接键，Z是基团-COOH，-COOR1（其中R1是低级烷基），其中R2和R3独立地是氢或低级烷基或-CH2OH，与 条件是X不是H-Ala，当Z是COOH时。

    Calcitonin derivatives
    3.
    发明授权
    Calcitonin derivatives 失效
    降钙素衍生物

    公开(公告)号：US5541159A

    公开(公告)日：1996-07-30

    申请号：US346118

    申请日：1994-11-29

    Applicant: Rainer Albert ,  Wilfried Bauer ,  Fran.cedilla.ois Cardinaux ,  Janos Pless

    Inventor： Rainer Albert ,  Wilfried Bauer ,  Fran.cedilla.ois Cardinaux ,  Janos Pless

    IPC: A61K38/23 ,  A61K38/00 ,  A61K38/04 ,  A61P1/00 ,  A61P3/00 ,  A61P43/00 ,  C07K1/02 ,  C07K1/06 ,  C07K1/113 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575 ,  C07K14/585 ,  A61K8/23

    CPC classification number: C07K9/005 ,  C07K14/585 ,  C07K7/23 ,  C07K9/001 ,  A61K38/00

    Abstract: Peptide derivatives selected from (i) a calcitonin peptide and a LHRH antagonist peptide modified by at least one sugar residue and/or at least one short polyhydroxy compound or derivative, and (ii) a calcitonin peptide modified by at least one formyl and/or at least C.sub.3-5 alkyl attached to an amino group other than a N-terminal amino group, and (iii) a calcitonin peptide modified by a combination of said substituents, with the provisos thati) when the calcitonin peptide comprises at least one sugar residue a), this sugar residue is attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.-amino substituted side chain in the 24 position, andii) when the LHRH antagonist comprises at least one sugar residue a), this sugar residue is an Amadori sugar residue attached by a coupling other than a direct N-glycosidic bond to an .omega.-amino group of an .omega.-amino substituted side chain in the 8 positionin free form or in salt or complex form, have pharmacological activity.

    Abstract translation: 选自（i）由至少一种糖残基和/或至少一种短多羟基化合物或衍生物修饰的降钙素肽和LHRH拮抗剂肽的肽衍生物，和（ii）通过至少一种甲酰基和/或 至少C3-5烷基连接到除了N-末端氨基以外的氨基，和（iii）通过所述取代基的组合修饰的降钙素肽，条件是i）当降钙素肽包含至少一个糖残基 a），该糖残基通过除了直接N-糖苷键之外的偶联与在24位的ω-氨基取代侧链的ω-氨基连接，和ii）当LHRH拮抗剂包含至少一种糖 残基a），该糖残基是通过除直接N-糖苷键之外的偶联与游离形式的8位的ω-氨基取代侧链的ω-氨基或盐或复合物连接的阿马多糖残基 形式，有p 有害活动。

    Polypeptide derivatives
    6.
    发明授权
    Polypeptide derivatives 失效
    多肽衍生物

    公开(公告)号：US5686410A

    公开(公告)日：1997-11-11

    申请号：US276280

    申请日：1994-07-18

    Applicant: Rainer Albert ,  Wilfried Bauer ,  Janos Pless

    Inventor： Rainer Albert ,  Wilfried Bauer ,  Janos Pless

    IPC: A61K47/48 ,  A61K51/08 ,  A61K38/18 ,  C07K14/485

    CPC classification number: A61K47/48276 ,  A61K47/48238 ,  A61K51/088 ,  A61K2121/00 ,  A61K2123/00

    Abstract: A biologically active peptide selected from growth factors, peptide hormones, interferons and cytokines and analogues and derivatives thereof, and bearing at least one chelating group linked to an amino group of said peptide, the chelating group being capable of complexing a detectable element and such amino group having no significant binding affinity to target receptors, are complexed with a detectable element and are useful as a pharmaceutical, e.g. a radiopharmaceutical for in vivo imaging of target tissues or for therapy.

    Abstract translation: 选自生长因子，肽激素，干扰素和细胞因子及其类似物和衍生物的生物活性肽，并且具有与所述肽的氨基连接的至少一个螯合基团，所述螯合基团能够络合可检测元件，并且所述氨基 与靶受体没有显着结合亲和力的基团与可检测元件复合并且可用作药物，例如， 用于靶组织的体内成像或用于治疗的放射性药物。

    Somatostatine derivatives
    7.
    发明授权
    Somatostatine derivatives 失效
    生长激素衍生物

    公开(公告)号：US4728638A

    公开(公告)日：1988-03-01

    申请号：US816663

    申请日：1986-01-07

    Applicant: Wilfried Bauer ,  Janos Pless ,  Rene Huguenin

    Inventor： Wilfried Bauer ,  Janos Pless ,  Rene Huguenin

    IPC: A61K38/00 ,  C07K14/655 ,  A61K37/24 ,  C07K7/26

    CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/16

    Abstract: Somatostatine derivatives of the general formula ##STR1## wherein either (a)A is ##STR2## W is -CO-N(A.sub.4) or -N(A.sub.5)-CO- and Y.sub.1 and Y.sub.2 are H or together a bondor (b)A is H, alkyl, phenylalkyl or RCO andY.sub.1 and Y.sub.2 are acyl groups as defined in claim 1,A', B, C, D, E, F, A.sub.1, A.sub.2, A.sub.3, A.sub.4, A.sub.5, R and Z having the meanings recited in claim 1, have pharmacological, in particular GH-, gastric- and pancreatic secretion inhibiting activity.

    Abstract translation: 其中（a）A是-CO-N（A4）或-N（A5）-CO-，Y1和Y2是H或一起键或（b）的通式的生长激素衍生物 ）A是H，烷基，苯基烷基或RCO，Y 1和Y 2是如权利要求1中定义的酰基，A'，B，C，D，E，F，A1，A2，A3，A4，A5，R和Z具有 权利要求1所述的含义具有药理学，特别是GH-，胃和胰腺分泌抑制活性。

    Organic compounds
    8.
    发明授权
    Organic compounds 失效
    有机化合物

    公开(公告)号：US4261888A

    公开(公告)日：1981-04-14

    申请号：US097630

    申请日：1979-11-27

    Applicant: Wilfried Bauer ,  Francois Cardinaux ,  Rene Huguenin ,  Janos Pless ,  Edmond Sandrin

    Inventor： Wilfried Bauer ,  Francois Cardinaux ,  Rene Huguenin ,  Janos Pless ,  Edmond Sandrin

    IPC: C07K5/107 ,  C07C103/52

    CPC classification number: C07K5/1016 ,  Y10S514/809

    Abstract: The invention provides polypeptides of formula I,A-B-Gly-D-E Iwherein A is Tyr or substituted Tyr,B is -Gly- or -(D)Ala-,D is, for example, Phe or MePhe andE is, for example, -Met-X, -Leu-X, -Nle-X, -Nva-X, -Ile-X, methioninesulhoxide-X, methioninesulphone-X wherein X is --NR'R" or --OR'" and each of R', R" and R'" independently signifies hydrogen or alkyl of 1 to 5 carbon atoms,which compounds possess pharmacological activity, for example, analgesic activity.

    Abstract translation: 本发明提供了式I的多肽，其中A为Tyr或取代的Tyr，B为-Gly-或 - （D）Ala-，D为例如Phe或MePhe，E为例如AB-Gly-DE I ，-Met-X，-Leu-X，-Nle-X，-Nva-X，-Ile-X，甲硫氨酸 - X，甲硫氨酸 - X，其中X为-NR'R“或-OR” 的R'，R“和R”“独立地表示氢或1〜5个碳原子的烷基，该化合物具有药理活性，例如止痛活性。

    Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use
    9.
    发明授权
    Polypeptides, processes for their production, pharmaceutical compositions comprising said polypeptides and their use 失效
    多肽，其制备方法，包含所述多肽的药物组合物及其用途

    公开(公告)号：US4496543A

    公开(公告)日：1985-01-29

    申请号：US524374

    申请日：1983-08-18

    Applicant: Wilfried Bauer ,  Janos Pless

    Inventor： Wilfried Bauer ,  Janos Pless

    IPC: A61K38/00 ,  A61K38/04 ,  A61K38/27 ,  A61P1/00 ,  A61P1/04 ,  A61P3/08 ,  A61P3/10 ,  A61P5/00 ,  A61P9/00 ,  C07K7/06 ,  C07K14/655 ,  A61K37/00 ,  C07C103/52

    CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S930/16 ,  Y10S930/26

    Abstract: Straight-chain or mono-cyclicpolypeptides comprising a heptapeptide moiety, said moiety having in the 1-position (N-terminal) an .alpha.-N-phenylalkylated, optionally ring-substituted phenylalanine residue, in the 2-position a cysteine residue, in the 3-position an optionally ring-substituted phenylalanine residue, in the 4-position an optionally benzene-ring-substituted tryptophan residue, in the 5-position an optionally .epsilon.-N-alkylated lysine residue and in the 7-position (C-terminal) a cysteine or cysteinol residue the S-atoms of the cysteine residue at the 2-position and the cysteine or cysteinol residue at the 7-position being linked together in the case of the mono-cyclic polypeptides to form an -S-S-bridge, whereby the residues at the 1-, 2-, 4-, 6-, and 7-positions of said heptapeptide moiety may each be in the (L)- or (D)-configuration and the residues at the 4-, 5- and 6-positions of said heptapeptide moiety may each be optionally .alpha.-N-alkylated, said polypeptides being in free or protected form, as well as salt forms and complexes thereof. Subject compounds are useful as pharmaceuticals, e.g. as GH-secretion inhibitors.

    Abstract translation: 包括七肽部分的直链或单环多肽，所述部分在2-位半胱氨酸残基中具有1-位（N-末端）α-N-烷基苯基烷基化，任选环取代的苯丙氨酸残基，在 3-位任选环取代的苯丙氨酸残基，在4-位任选的苯环取代的色氨酸残基，在5-位任选的ε-N-烷基化赖氨酸残基和7-位（C-末端 ）半胱氨酸或半胱氨酸残基，在2-位的半胱氨酸残基的S原子和7-位的半胱氨酸或半胱氨酸残基在单环多肽的情况下连接在一起以形成-SS桥， 其中所述七肽部分的1-，2-，4-，6-和7-位上的残基可以各自为（L） - 或（D） - 构型，并且4-，5- 所述七肽部分的6-位可各自任选为α-烷基化的，所述多肽为 游离或保护形式，以及其盐形式和复合物。 主题化合物可用作药物，例如 作为GH分泌抑制剂。

    N-Acyl-polypeptides and processes for the production thereof
    10.
    发明授权
    N-Acyl-polypeptides and processes for the production thereof 失效
    N-酰基多肽及其生产方法

    公开(公告)号：US4435385A

    公开(公告)日：1984-03-06

    申请号：US353900

    申请日：1982-03-02

    Applicant: Wilfried Bauer ,  Janos Pless

    Inventor： Wilfried Bauer ,  Janos Pless

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

    CPC classification number: C07K14/6555 ,  A61K38/00 ,  Y10S514/806 ,  Y10S930/26

    Abstract: N-Acyl-polypeptides comprising the basic sequence ##STR1## wherein "Acyl" is the acyl residue of an organic or inorganic acid; A is H or alkyl; >N--CH(Z)--CO-- and E are the residues of natural .alpha.-amino acids or corresponding (D)-amino acids; C is --Trp-- or --(D)Trp--; F is a terminal grouping; and Y.sub.1 and Y.sub.2 are each H or together are a direct bond; as well as their salt forms and complexes.

    Abstract translation: 包含碱基序列“IMAGE”的N-酰基多肽，其中“酰基”是有机或无机酸的酰基残基; A是H或烷基; > N-CH（Z）-CO-和E是天然α-氨基酸或相应的（D） - 氨基酸的残基; C是-Trp-或 - （D）Trp-; F是终端分组; Y1和Y2各自为H或一起为直接键; 以及它们的盐形式和复合物。

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