MODIFIED GLP-1 PEPTIDES WITH INCREASED BIOLOGICAL POTENCY
    2.
    发明公开
    MODIFIED GLP-1 PEPTIDES WITH INCREASED BIOLOGICAL POTENCY 审中-公开
    改进的GLP-1增加的生物有效性肽

    公开(公告)号:EP1543030A2

    公开(公告)日:2005-06-22

    申请号:EP03753161.3

    申请日:2003-09-25

    IPC分类号: C07K14/605

    CPC分类号: C07K14/605 A61K38/26

    摘要: The present invention relates to a GLP-1 peptide having the following formula, or a pharmaceutically acceptable salt thereof: X-His-Ala-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Val-Ser-Ser-Tyr-Leu-Glu-Gly-Gln-Ala-Ala-Lys-Glu-Phe-IIe-Ala-Trp-Leu-val-Lys-Gly-Arg-Y (SEQ ID NO.1), wherein X is a rigidifying hydrophobic moiety and wherein Y is selected from the group consisting of OH, NH2 and Gly-OH. Moreover, the present invention relates to pharmaceutical compositions comprising a therapeutically effective amount of a peptide of the present invention, or a pharmaceutically acceptable salt thereof, in association with at least one constituent selected from a pharmaceutically acceptable carrier, diluent, and excipient.

    HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF
    3.
    发明公开
    HALOGENATED RHODAMINE DERIVATIVES AND APPLICATIONS THEREOF 审中-公开
    卤代罗丹明及其用途

    公开(公告)号:EP1276734A1

    公开(公告)日:2003-01-22

    申请号:EP02708105.8

    申请日:2002-03-27

    IPC分类号: C07D311/82 A61K31/352

    CPC分类号: C07D311/82

    摘要: Novel compounds of the formula (I) wherein: one of R1, R2, R3, R4, and (R10)n represents an halogen atom and each of the remaining R1, R2, R3, R4, and each of the remaining R10 group is independently selected in the group constituted by hydrogen, halogen atoms, an amino, acylamino, dialkylamino, cycloalkylamino, azacycloalkyl, alkylcycloalkylamino, aroylamino, diarylamino, arylalkylamino, aralkylamino, alkylaralkylamino, arylaralkylamino, hydroxy, alkoxy, aryloxy, aralkyloxy, mercapto, alkylthio, arylthio, aralkylthio, carboxyl, alkoxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl, carbamoyl, alkylcarbamoyl, dialkylcarbamoyl, cyano, hydroxysulfonyl, amidosulfonyl, dialkylamidosulfonyl, arylalkylamidosulfonyl, formyl, acyl, aroyl, alkyl, alkylene, alkenyl, aryl, aralkyl, vinyl, alkynyl group and by the corresponding substituted groups; - m = 0 - 1; n = 1-4, A is nil, O, or NH; R9 represents an alkylene group; -Z is H, amino, dialkylamino, or trialkylamino salt; X- is an anion; R5, R6, R7 and R8 are independently H or C1-C6 alkyl or R1 in combination with R5 or R6, or R2 in combination with R5 or R6, or R3 in combination with R7 or R8, or R4in combination with R7 or R8 represents an alkylene, alone or in association with a pharmaceutically acceptable carrier. These compounds, which are usefull as intermediate and as bactericides, as antiviral agent and in the treatment of immunologic disoders.

    GROWTH HORMONE RELEASING FACTOR (GRF) ANALOGS AND USES THEREOF
    5.
    发明公开
    GROWTH HORMONE RELEASING FACTOR (GRF) ANALOGS AND USES THEREOF 审中-公开
    生长激素释放因子(GRF)类似物及其用途

    公开(公告)号:EP2699591A1

    公开(公告)日:2014-02-26

    申请号:EP12774217.9

    申请日:2012-04-17

    IPC分类号: C07K14/60 A61K38/25

    CPC分类号: C07K14/60 A61K38/00

    摘要: Growth Hormone-releasing Factor (GRF) analogs wherein lysine-21, leucine-22 and leucine-23 are deleted are described herein. These analogs retain GRF activity. The uses of said analogs for example as a GRF receptor agonist,
    e.g. to induce growth hormone secretion in a subject or biological system are also described.

    摘要翻译: 本文描述了缺失赖氨酸-21,亮氨酸-22和亮氨酸-23的生长激素释放因子(GRF)类似物。 这些类似物保留GRF活性。 所述类似物作为例如GRF受体激动剂例如 还描述了在受试者或生物系统中诱导生长激素分泌。

    GRF ANALOGS WITH INCREASED BIOLOGICAL POTENCY
    8.
    发明公开
    GRF ANALOGS WITH INCREASED BIOLOGICAL POTENCY 有权
    GRF具有增加的生物效价类似物

    公开(公告)号:EP1109909A2

    公开(公告)日:2001-06-27

    申请号:EP99941349.5

    申请日:1999-09-07

    摘要: The present invention relates to chimeric fatty body-GRF analogs with increased biological potency, their application as anabolic agents and in the diagnosis and treatment of growth hormone deficiencies. The chimeric fatty body-GRF analogs include a hydrophobic moiety (tail), and can be prepared, either by anchoring at least one hydrophobic tail to the GRF, in the chemical synthesis of GRF. The GRF analogs of the present invention are biodegradable, non-immunogenic and exhibit an improved anabolic potency with a reduced dosage and prolonged activity.