JP2017502003A5 - - Google Patents

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Publication number
JP2017502003A5
JP2017502003A5 JP2016538037A JP2016538037A JP2017502003A5 JP 2017502003 A5 JP2017502003 A5 JP 2017502003A5 JP 2016538037 A JP2016538037 A JP 2016538037A JP 2016538037 A JP2016538037 A JP 2016538037A JP 2017502003 A5 JP2017502003 A5 JP 2017502003A5
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JP
Japan
Prior art keywords
phe
pro
tyr
aib
nal
Prior art date
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Pending
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JP2016538037A
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English (en)
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JP2017502003A (ja
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Priority claimed from PCT/EP2014/077240 external-priority patent/WO2015086686A2/en
Publication of JP2017502003A publication Critical patent/JP2017502003A/ja
Publication of JP2017502003A5 publication Critical patent/JP2017502003A5/ja
Pending legal-status Critical Current

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Claims (1)

  1. 下記のアミノ酸配列を含む合成GLP−1ペプチド。
    1−His−X1−Glu−Gly−X2−X3−Thr−Ser−Asp−Val−Ser−Ser−X4−Leu−Glu−Gly−Gln−Ala−Ala−X5−Glu−X6−Ile−Ala−X7−X8−X9−X10−X11−X12−R2(配列番号:63)(但し、
    1は、Hy、AcまたはpGluであり;
    2は、−NH2または−OHであり;
    X1は、Ala、Aib、ProまたはGlyであり;
    X2は、Thr、ProまたはSerであり;
    X3は、Aib、Bip、β,β−Dip、F5−Phe、Phe、PhG、Nle、ホモPhe、ホモTyr、N−MePhe、α−MePhe、α−Me−2F−Phe、Tyr、Trp、Tyr−OMe、4I−Phe、2F−Phe、3F−Phe、4F−Phe、1−Nal、2−Nal、Proまたはジ−β,β−Me−Pheであり;
    X4は、Aib、Ala、Asp、Arg、Bip、Cha、β,β−Dip、Gln、F5−Phe、PhG、Nle、ホモPhe、ホモTyr、α−MePhe、α−Me−2F−Phe、Phe、Thr、Trp、Tyr−OMe、4I−Phe、2F−Phe、3F−Phe、4F−Phe、Tyr、1−Nal、2−Nal、Pro、またはジ−β,β−Me−Pheであり;
    X5は、Aib、Lys、D−pro、Proもしくはα−MeLysであり;
    X6は、Aib、Asp、Arg、Bip、Cha、Leu、Lys、2Cl−Phe、3Cl−Phe、4Cl−Phe、PhG、ホモPhe、2Me−Phe、3Me−Phe、4Me−Phe、2CF3−Phe、3CF3−Phe、4CF3−Phe、β−Phe、β−MePhe、D−phe、4I−Phe、3I−Phe、2F−Phe、β,β−Dip、β−Ala、Nle、Leu、F5−Phe、ホモTyr、α−MePhe、α−Me−2F−Phe、Ser、Tyr、Trp、Tyr−OMe、3F−Phe、4F−Phe、Pro、1−Nal、2−Nalまたはジ−β,β−Me−Pheであり;
    X7は、Aib、Arg、Bip、Cha、β,β−Dip、F5−Phe、PhG、Phe、Tyr、ホモPhe、ホモTyr、α−MePhe、α−Me−2F−Phe,2Me−Phe、3Me−Phe、4Me−Phe、Nle、Tyr−OMe、4I−Phe、1−Nal、2−Nal、2F−Phe、3F−Phe、4F−Phe、Pro、N−MeTrp、α−MeTrpまたはジ−β,β−Me−Pheであり;
    X8は、Aib、Ala、Arg、Asp、Glu、Nle、Pro、Ser、N−MeLeu、α−MeLeuまたはValであり;
    X9は、Aib、Glu、Lys、α−MeValまたはProであり;
    X10は、Aib、Glu、α−MeLysまたはProであり;
    X11は、Aib、Glu、ProまたはSerであり;かつ
    X12は、Aib、Gly、Glu、Proまたはα−MeArgである。)


JP2016538037A 2013-12-13 2014-12-10 プロテアーゼ耐性ペプチド Pending JP2017502003A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361915662P 2013-12-13 2013-12-13
US61/915,662 2013-12-13
PCT/EP2014/077240 WO2015086686A2 (en) 2013-12-13 2014-12-10 Protease resistant peptides

Publications (2)

Publication Number Publication Date
JP2017502003A JP2017502003A (ja) 2017-01-19
JP2017502003A5 true JP2017502003A5 (ja) 2017-12-28

Family

ID=52021207

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2016538037A Pending JP2017502003A (ja) 2013-12-13 2014-12-10 プロテアーゼ耐性ペプチド

Country Status (11)

Country Link
US (1) US20160318987A1 (ja)
EP (2) EP3415526A1 (ja)
JP (1) JP2017502003A (ja)
KR (1) KR20160098406A (ja)
CN (1) CN105849123A (ja)
AU (1) AU2014363547A1 (ja)
BR (1) BR112016013157A2 (ja)
CA (1) CA2933405A1 (ja)
MX (1) MX2016007407A (ja)
SG (1) SG10201805039UA (ja)
WO (1) WO2015086686A2 (ja)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI726889B (zh) 2015-06-10 2021-05-11 英商梅迪繆思有限公司 蛋白酶抗性之脂化肽
CN108473547A (zh) * 2015-10-28 2018-08-31 塔夫茨大学 具有改良的蛋白质分解安定性的新颖多肽,以及制备与使用该新颖多肽的方法
KR20190017017A (ko) 2016-06-09 2019-02-19 메디뮨 리미티드 프로테아제-내성 모노-지질화된 펩타이드
US10278957B2 (en) 2017-09-11 2019-05-07 Protagonist Therapeutics, Inc. Opioid agonist peptides and uses thereof
EP4364751A3 (en) 2018-04-05 2024-06-26 Sun Pharmaceutical Industries Limited Novel glp-1 analogues
TW202346323A (zh) * 2022-02-07 2023-12-01 英商梅迪繆思有限公司 具有改善的生物穩定性的glp—1及升糖素雙重激動肽

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000034331A2 (en) * 1998-12-07 2000-06-15 Societe De Conseils De Recherches Et D'applications Scientifiques Sas Analogues of glp-1
CN101379075B (zh) * 2006-02-08 2013-05-15 隆萨股份公司 类胰高血糖素肽的合成
US20100022457A1 (en) * 2006-05-26 2010-01-28 Bristol-Myers Squibb Company Sustained release glp-1 receptor modulators
US20090318353A1 (en) * 2006-08-25 2009-12-24 Novo Nordisk A/S Acylated Exendin-4 Compounds
MX2010006287A (es) * 2007-12-11 2010-10-26 Cadila Healthcare Ltd Peptidomimeticos con actividades antagonistas de glucagon y agonistas del peptido 1 similar al glucagon.
ES2354488T3 (es) * 2008-04-18 2011-03-15 F. Hoffmann-La Roche Ag Alfa-n-metilación de aminoácidos.
EP2491054A2 (en) * 2009-10-22 2012-08-29 Cadila Healthcare Limited Short chain peptidomimetics based orally active glp-1 agonist and glucagon receptor antagonist
US20130143800A1 (en) * 2011-11-07 2013-06-06 Research Development Foundation Combination therapies to treat diabetes
AR092873A1 (es) * 2012-09-26 2015-05-06 Cadila Healthcare Ltd Peptidos como agonistas triples de los receptores de gip, glp-1 y glugagon
EP3459598A1 (en) * 2012-12-06 2019-03-27 Stealth Peptides International, Inc. Combinations of peptide therapeutics and methods for using same

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