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    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF
    1.
    发明申请
    GIP RECEPTOR AGONIST PEPTIDE COMPOUNDS AND USES THEREOF 审中-公开

    公开(公告)号：WO2020067557A2

    公开(公告)日：2020-04-02

    申请号：PCT/JP2019/038441

    申请日：2019-09-24

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED

    Inventor： IMOTO, Hiroshi ,  ADACHI, Mari ,  KANEMATSU, Yoko ,  ASAMI, Taiji ,  NIIDA, Ayumu ,  NISHIZAWA, Naoki ,  COLE, Derek, Cecil ,  FLINSPACH, Mack ,  SCORAH, Nick ,  BHAT, Abhijit, Suresh

    Abstract: The present disclosure provides GIP receptor agonist peptide compounds having an activating action on GIP receptors and use of the GIP receptor agonist peptide as a medicament for the treatment and/or prevention of diabetes, obesity, emesis, or a symptom or condition associated with diabetes, obesity, or emesis. Specifically, a GIP receptor agonist peptide containing a sequence represented by the formula (I) or a salt thereof, and a medicament comprising the same are provided. Formula I: P 1 - A 1 - A2- A3 - A4- A5 - A6- A7 - A8-A9-A 10- A 11 - A 12- A 13- A 14- A 15-A 16-A 17-A18-A19-A20-A21 -A22-A23-A24-A25- A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-A37-A38-A39-A40-A41-P2 (SEQ ID NO: 4), or a salt thereof, wherein each symbol is as defined herein, with the proviso that the GIP receptor agonist peptide does not have an amino acid sequence as provided in SEQ ID NOs: 4-569 disclosed in PCT/JP2018/013540.

    PEPTIDE DERIVATIVE
    2.
    发明申请
    PEPTIDE DERIVATIVE 审中-公开
    肽衍生物

    公开(公告)号：WO2012050227A1

    公开(公告)日：2012-04-19

    申请号：PCT/JP2011/073982

    申请日：2011-10-12

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ASAMI, Taiji ,  NISHIZAWA, Naoki ,  KANEMATSU, Yoko

    Inventor： ASAMI, Taiji ,  NISHIZAWA, Naoki ,  KANEMATSU, Yoko

    IPC: C07K14/575

    CPC classification number: C07K14/575 ,  A61K38/00

    Abstract: The present invention relates to a peptide derivative selected from the group consisting of PEG20k(AL)- β-Ala-Tyr-Nal(1)-Leu-Phe-Arg-Pro-Arg-Asn-NH 2 , PEG20k(AL)-β-Ala-Tyr-Nal(2)-Leu-Phe-Arg-Pro-Arg-Asn-NH 2 , PEG20k(AL)-NpipAc-Tyr-Nal(2)-Leu-Phe-Arg-Pro-Arg-Asn-NH 2 , PEG20k(AL)-NpipAc-Tyr-Nal(2)-Leu-Phe-Arg-Ala-Arg-Asn-NH 2 , PEG20k(AL)-PEG(2)-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH 2 , PEG20k(AL)-Pic(4)-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH 2 , PEG20k(AL)-Acp-Tyr-Nal(2)-Leu-Phe-Arg-NMeAla-Arg-Asn-NH 2 ,and PEG20k(AL)- -Ala-Tyr-Nal(2)-Leu-Pya(4)-Arg-Pro-Arg-Asn-NH 2 ; or a salt thereof.

    Abstract translation: 本发明涉及选自PEG20k（AL）-β-Ala-Tyr-Nal（1）-Leu-Phe-Arg-Pro-Arg-Asn-NH2，PEG20k（AL）-β （2）-Leu-Phe-Arg-Pro-Arg-Asn-NH 2，PEG20k（AL）-NpipAc-Tyr-Nal（2）-Leu-Phe-Arg-Pro-Arg-Asn- NH2，PEG20k（AL）-NpipAc-Tyr-Nal（2）-Leu-Phe-Arg-Ala-Arg-Asn-NH2，PEG20k（AL）-PEG（2）-Tyr-Nal（2）-Leu-Phe -Arg-NMeAla-Arg-Asn-NH2，PEG20k（AL）-Pic（4）-Tyr-Nal（2）-Leu-Phe-Arg-NMeAla-Arg-Asn-NH2，PEG20k（AL）-Acp-Tyr -Nal（2）-Leu-Phe-Arg-NMeAla-Arg-Asn-NH 2和PEG20k（AL）-Ala-Tyr-Nal（2）-Leu-Pya（4）-Arg-Pro-Arg-Asn -NH2; 或其盐。

    METASTIN DERIVATIVES AND USE THEREOF
    3.
    发明申请
    METASTIN DERIVATIVES AND USE THEREOF 审中-公开
    分子衍生物及其用途

    公开(公告)号：WO2008050897A1

    公开(公告)日：2008-05-02

    申请号：PCT/JP2007/071169

    申请日：2007-10-24

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ASAMI, Taiji ,  NISHIZAWA, Naoki

    Inventor： ASAMI, Taiji ,  NISHIZAWA, Naoki

    IPC: C07K14/47 ,  A61K38/16

    CPC classification number: C07K14/4703 ,  A61K38/00

    Abstract: The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotropic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids, the metastin derivatives of the present invention achieve more improved blood stability, solubility, etc., reduced gelation tendency, improved pharmacokinetics, as well as exhibit an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity. The metastin derivatives of the present invention also have a gonadotropic hormone secretion suppressing activity, sex hormone secretion suppressing activity, etc.

    Abstract translation: 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性，促性腺激素分泌刺激活性，性激素分泌刺激活性等）的稳定的转氨酶衍生物。 通过用特定氨基酸取代组氨酸的氨基酸，本发明的转氨酶衍生物获得更好的血液稳定性，溶解性等，降低的凝胶化趋势，改善的药代动力学，以及表现出优异的癌转移抑制活性或 癌症生长抑制活性。 本发明的转氨酶衍生物也具有促性腺激素分泌抑制活性，性激素分泌抑制活性等。

    METASTIN DERIVATIVES AND USE THEREOF
    5.
    发明申请
    METASTIN DERIVATIVES AND USE THEREOF 审中-公开
    分子衍生物及其用途

    公开(公告)号：WO2007072997A1

    公开(公告)日：2007-06-28

    申请号：PCT/JP2006/326176

    申请日：2006-12-21

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  ASAMI, Taiji ,  NISHIZAWA, Naoki

    Inventor： ASAMI, Taiji ,  NISHIZAWA, Naoki

    IPC: C07K14/47 ,  A61K38/16

    CPC classification number: C07K14/4748 ,  A61K38/00 ,  C07K14/4703

    Abstract: The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc.

    Abstract translation: 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性，促性腺激素分泌刺激活性，性激素分泌刺激活性等）的稳定的转氨酶衍生物。 通过在本发明的转氨酶衍生物中代替具有特定氨基酸的组氨酸的氨基酸，血液稳定性，溶解度等进一步提高，凝胶化倾向降低，药代动力学改善，以及优异的癌转移抑制活性或 展现了癌症生长抑制活性。 此外，本发明的转氨酶衍生物具有抑制促性腺激素分泌，抑制性激素分泌等作用。

    METASTIN DERIVATIVES AND USE THEREOF
    6.
    发明申请
    METASTIN DERIVATIVES AND USE THEREOF 审中-公开
    分子衍生物及其用途

    公开(公告)号：WO2006001499A2

    公开(公告)日：2006-01-05

    申请号：PCT/JP2005/012021

    申请日：2005-06-23

    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED ,  KITADA, Chieko ,  ASAMI, Taiji ,  NISHIZAWA, Naoki

    Inventor： KITADA, Chieko ,  ASAMI, Taiji ,  NISHIZAWA, Naoki

    IPC: C07K14/47

    CPC classification number: C07K14/4703 ,  A61K38/00

    Abstract: The invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, etc.). By modifying the constituent amino acids of metastin with specific modifying groups, metastin derivatives having more improved blood stability, etc. than native metastin and showing excellent cancer metastasis suppressing activity or cancer growth suppressing activity have been found. Furthermore, it has been found that these metastin derivatives exhibit effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc., which are wholly different from the effects heretofore known.

    Abstract translation: 本发明提供具有优异生物活性（癌转移抑制活性，癌生长抑制活性等）的稳定的转铁蛋白衍生物。 已经发现通过用特异性修饰基修饰转氨酶的构成氨基酸，具有比天然转移蛋白更多的改善的血液稳定性的转氨酶衍生物，并且显示出优异的癌症转移抑制活性或癌症生长抑制活性。 此外，已经发现这些转氨酶衍生物表现出抑制促性腺激素分泌，抑制性激素分泌等的作用，其完全不同于迄今已知的效果。

    METASTIN DERIVATIVES AND USE THEREOF
    9.
    发明公开
    METASTIN DERIVATIVES AND USE THEREOF 有权
    METASTINDERIVATE及其用途

    公开(公告)号：EP1963362A1

    公开(公告)日：2008-09-03

    申请号：EP06843555.1

    申请日：2006-12-21

    Applicant: Takeda Pharmaceutical Company Limited

    Inventor： ASAMI, Taiji ,  NISHIZAWA, Naoki

    IPC: C07K14/47 ,  A61K38/16

    CPC classification number: C07K14/4748 ,  A61K38/00 ,  C07K14/4703

    Abstract: The present invention provides stable metastin derivatives having excellent biological activities (a cancer metastasis suppressing activity, a cancer growth suppressing activity, a gonadotrophic hormone secretion stimulating activity, sex hormone secretion stimulating activity, etc.). By substituting the constituent amino acids of metastin with specific amino acids in the metastin derivative of the present invention, blood stability, solubility, etc. are more improved, gelation tendency is reduced, pharmacokinetics are also improved, and an excellent cancer metastasis suppressing activity or a cancer growth suppressing activity is exhibited. Furthermore, the metastin derivative of the present invention has the effects of suppressing gonadotropic hormone secretion, suppressing sex hormone secretion, etc.

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