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
- Authority
- JP
- Japan
- Prior art keywords
- phe
- pro
- tyr
- aib
- nal
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
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- 125000000174 L-prolyl group Chemical group [H]N1C([H])([H])C([H])([H])C([H])([H])[C@@]1([H])C(*)=O 0.000 claims 12
- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 6
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 5
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 5
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 3
- MTCFGRXMJLQNBG-REOHCLBHSA-N L-serine Chemical group OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 3
- 125000000510 L-tryptophano group Chemical group [H]C1=C([H])C([H])=C2N([H])C([H])=C(C([H])([H])[C@@]([H])(C(O[H])=O)N([H])[*])C2=C1[H] 0.000 claims 3
- MWZPENIJLUWBSY-VIFPVBQESA-N methyl L-tyrosinate Chemical compound COC(=O)[C@@H](N)CC1=CC=C(O)C=C1 MWZPENIJLUWBSY-VIFPVBQESA-N 0.000 claims 3
- 125000000998 L-alanino group Chemical group [H]N([*])[C@](C([H])([H])[H])([H])C(=O)O[H] 0.000 claims 2
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims 2
- 125000001037 p-tolyl group Chemical group [H]C1=C([H])C(=C([H])C([H])=C1*)C([H])([H])[H] 0.000 claims 2
- DTHNMHAUYICORS-KTKZVXAJSA-N 107444-51-9 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](C)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(N)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](C)NC(=O)[C@H](C)NC(=O)[C@H](CCC(N)=O)NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC(O)=CC=1)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](C)NC(=O)[C@@H](N)CC=1N=CNC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 DTHNMHAUYICORS-KTKZVXAJSA-N 0.000 claims 1
- -1 Aib Chemical group 0.000 claims 1
- COLNVLDHVKWLRT-MRVPVSSYSA-N D-phenylalanine Chemical compound OC(=O)[C@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-MRVPVSSYSA-N 0.000 claims 1
- 125000000237 D-prolino group Chemical group [H]OC(=O)[C@]1([H])N(*)C([H])([H])C([H])([H])C1([H])[H] 0.000 claims 1
- 102100003818 GCG Human genes 0.000 claims 1
- 101710042131 GCG Proteins 0.000 claims 1
- 101700071595 GRZ1 Proteins 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 1
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 1
- 125000000205 L-threonino group Chemical group [H]OC(=O)[C@@]([H])(N([H])[*])[C@](C([H])([H])[H])([H])O[H] 0.000 claims 1
- NYQBYASWHVRESG-MIMYLULJSA-N Phe-Thr Chemical compound C[C@@H](O)[C@@H](C(O)=O)NC(=O)[C@@H](N)CC1=CC=CC=C1 NYQBYASWHVRESG-MIMYLULJSA-N 0.000 claims 1
- 101700078733 ZGLP1 Proteins 0.000 claims 1
- 125000003275 alpha amino acid group Chemical group 0.000 claims 1
- 125000003854 p-chlorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1Cl 0.000 claims 1
- UCMIRNVEIXFBKS-UHFFFAOYSA-N β-Alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims 1
Claims (1)
- 下記のアミノ酸配列を含む合成GLP−1ペプチド。
R1−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、
R1は、Hy、AcまたはpGluであり;
R2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。)
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)
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)
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 |
-
2014
- 2014-12-10 KR KR1020167018887A patent/KR20160098406A/ko not_active Application Discontinuation
- 2014-12-10 CN CN201480067307.1A patent/CN105849123A/zh active Pending
- 2014-12-10 SG SG10201805039UA patent/SG10201805039UA/en unknown
- 2014-12-10 WO PCT/EP2014/077240 patent/WO2015086686A2/en active Application Filing
- 2014-12-10 EP EP18182275.0A patent/EP3415526A1/en not_active Withdrawn
- 2014-12-10 BR BR112016013157A patent/BR112016013157A2/pt not_active Application Discontinuation
- 2014-12-10 JP JP2016538037A patent/JP2017502003A/ja active Pending
- 2014-12-10 AU AU2014363547A patent/AU2014363547A1/en not_active Abandoned
- 2014-12-10 EP EP14809857.7A patent/EP3080153A2/en not_active Withdrawn
- 2014-12-10 MX MX2016007407A patent/MX2016007407A/es unknown
- 2014-12-10 CA CA2933405A patent/CA2933405A1/en not_active Abandoned
- 2014-12-10 US US15/103,607 patent/US20160318987A1/en not_active Abandoned
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