JP2019531075A5 - - Google Patents
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- JP2019531075A5 JP2019531075A5 JP2019515862A JP2019515862A JP2019531075A5 JP 2019531075 A5 JP2019531075 A5 JP 2019531075A5 JP 2019515862 A JP2019515862 A JP 2019515862A JP 2019515862 A JP2019515862 A JP 2019515862A JP 2019531075 A5 JP2019531075 A5 JP 2019531075A5
- Authority
- JP
- Japan
- Prior art keywords
- tyrosine
- general formula
- xaa16
- serine
- threonine
- 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.)
- Granted
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- OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims 56
- OUYCCCASQSFEME-UHFFFAOYSA-N tyrosine Natural products OC(=O)C(N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-UHFFFAOYSA-N 0.000 claims 56
- 235000002374 tyrosine Nutrition 0.000 claims 56
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 46
- MTCFGRXMJLQNBG-UHFFFAOYSA-N Serine Natural products OCC(N)C(O)=O MTCFGRXMJLQNBG-UHFFFAOYSA-N 0.000 claims 33
- NOESYZHRGYRDHS-UHFFFAOYSA-N insulin Chemical class N1C(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(NC(=O)CN)C(C)CC)CSSCC(C(NC(CO)C(=O)NC(CC(C)C)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CCC(N)=O)C(=O)NC(CC(C)C)C(=O)NC(CCC(O)=O)C(=O)NC(CC(N)=O)C(=O)NC(CC=2C=CC(O)=CC=2)C(=O)NC(CSSCC(NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2C=CC(O)=CC=2)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)C(CCC(O)=O)NC(=O)C(C(C)C)NC(=O)C(CC(C)C)NC(=O)C(CC=2NC=NC=2)NC(=O)C(CO)NC(=O)CNC2=O)C(=O)NCC(=O)NC(CCC(O)=O)C(=O)NC(CCCNC(N)=N)C(=O)NCC(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC=CC=3)C(=O)NC(CC=3C=CC(O)=CC=3)C(=O)NC(C(C)O)C(=O)N3C(CCC3)C(=O)NC(CCCCN)C(=O)NC(C)C(O)=O)C(=O)NC(CC(N)=O)C(O)=O)=O)NC(=O)C(C(C)CC)NC(=O)C(CO)NC(=O)C(C(C)O)NC(=O)C1CSSCC2NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C(CCC(N)=O)NC(=O)C(CC(N)=O)NC(=O)C(NC(=O)C(N)CC=1C=CC=CC=1)C(C)C)CC1=CN=CN1 NOESYZHRGYRDHS-UHFFFAOYSA-N 0.000 claims 33
- 235000004400 serine Nutrition 0.000 claims 33
- AYFVYJQAPQTCCC-UHFFFAOYSA-N Threonine Natural products CC(O)C(N)C(O)=O AYFVYJQAPQTCCC-UHFFFAOYSA-N 0.000 claims 30
- 239000004473 Threonine Substances 0.000 claims 30
- 239000004026 insulin derivative Substances 0.000 claims 30
- 235000008521 threonine Nutrition 0.000 claims 30
- 235000004554 glutamine Nutrition 0.000 claims 24
- ZDXPYRJPNDTMRX-UHFFFAOYSA-N glutamine Natural products OC(=O)C(N)CCC(N)=O ZDXPYRJPNDTMRX-UHFFFAOYSA-N 0.000 claims 24
- 239000004471 Glycine Substances 0.000 claims 23
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 22
- ROHFNLRQFUQHCH-YFKPBYRVSA-N L-leucine Chemical compound CC(C)C[C@H](N)C(O)=O ROHFNLRQFUQHCH-YFKPBYRVSA-N 0.000 claims 22
- ROHFNLRQFUQHCH-UHFFFAOYSA-N Leucine Natural products CC(C)CC(N)C(O)=O ROHFNLRQFUQHCH-UHFFFAOYSA-N 0.000 claims 22
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 22
- 235000013922 glutamic acid Nutrition 0.000 claims 22
- 239000004220 glutamic acid Substances 0.000 claims 22
- 235000005772 leucine Nutrition 0.000 claims 22
- 235000013930 proline Nutrition 0.000 claims 22
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 21
- 235000003704 aspartic acid Nutrition 0.000 claims 21
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 21
- DCXYFEDJOCDNAF-UHFFFAOYSA-N Asparagine Natural products OC(=O)C(N)CC(N)=O DCXYFEDJOCDNAF-UHFFFAOYSA-N 0.000 claims 20
- DCXYFEDJOCDNAF-REOHCLBHSA-N L-asparagine Chemical compound OC(=O)[C@@H](N)CC(N)=O DCXYFEDJOCDNAF-REOHCLBHSA-N 0.000 claims 20
- 235000009582 asparagine Nutrition 0.000 claims 20
- 229960001230 asparagine Drugs 0.000 claims 20
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 19
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 19
- 235000008729 phenylalanine Nutrition 0.000 claims 19
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 17
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims 10
- 235000004279 alanine Nutrition 0.000 claims 10
- 150000001413 amino acids Chemical class 0.000 claims 10
- MTCFGRXMJLQNBG-REOHCLBHSA-N (2S)-2-Amino-3-hydroxypropansäure Chemical compound OC[C@H](N)C(O)=O MTCFGRXMJLQNBG-REOHCLBHSA-N 0.000 claims 9
- 229940024606 amino acid Drugs 0.000 claims 9
- 235000001014 amino acid Nutrition 0.000 claims 9
- 235000014304 histidine Nutrition 0.000 claims 9
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 claims 9
- HNDVDQJCIGZPNO-YFKPBYRVSA-N L-histidine Chemical compound OC(=O)[C@@H](N)CC1=CN=CN1 HNDVDQJCIGZPNO-YFKPBYRVSA-N 0.000 claims 8
- 230000035772 mutation Effects 0.000 claims 6
- 102000004877 Insulin Human genes 0.000 claims 5
- 108090001061 Insulin Proteins 0.000 claims 5
- AYFVYJQAPQTCCC-GBXIJSLDSA-N L-threonine Chemical compound C[C@@H](O)[C@H](N)C(O)=O AYFVYJQAPQTCCC-GBXIJSLDSA-N 0.000 claims 5
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 4
- 239000004472 Lysine Substances 0.000 claims 4
- 235000018977 lysine Nutrition 0.000 claims 4
- ZDXPYRJPNDTMRX-VKHMYHEASA-N L-glutamine Chemical compound OC(=O)[C@@H](N)CCC(N)=O ZDXPYRJPNDTMRX-VKHMYHEASA-N 0.000 claims 3
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 3
- 150000007523 nucleic acids Chemical class 0.000 claims 3
- 102000039446 nucleic acids Human genes 0.000 claims 3
- 108020004707 nucleic acids Proteins 0.000 claims 3
- 239000004480 active ingredient Substances 0.000 claims 2
- 238000005277 cation exchange chromatography Methods 0.000 claims 2
- 239000013604 expression vector Substances 0.000 claims 2
- 238000000746 purification Methods 0.000 claims 2
- 238000003259 recombinant expression Methods 0.000 claims 2
- 102000003670 Carboxypeptidase B Human genes 0.000 claims 1
- 108090000087 Carboxypeptidase B Proteins 0.000 claims 1
- 241000588724 Escherichia coli Species 0.000 claims 1
- ONIBWKKTOPOVIA-BYPYZUCNSA-N L-Proline Chemical compound OC(=O)[C@@H]1CCCN1 ONIBWKKTOPOVIA-BYPYZUCNSA-N 0.000 claims 1
- 102000004142 Trypsin Human genes 0.000 claims 1
- 108090000631 Trypsin Proteins 0.000 claims 1
- 238000005571 anion exchange chromatography Methods 0.000 claims 1
- 239000013592 cell lysate Substances 0.000 claims 1
- 238000012258 culturing Methods 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 238000003306 harvesting Methods 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 238000004366 reverse phase liquid chromatography Methods 0.000 claims 1
- 238000000926 separation method Methods 0.000 claims 1
- 239000012588 trypsin Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR20160122484 | 2016-09-23 | ||
| KR10-2016-0122484 | 2016-09-23 | ||
| PCT/KR2017/010504 WO2018056764A1 (ko) | 2016-09-23 | 2017-09-22 | 인슐린 수용체와의 결합력이 감소된, 인슐린 아날로그 및 이의 용도 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019531075A JP2019531075A (ja) | 2019-10-31 |
| JP2019531075A5 true JP2019531075A5 (https=) | 2020-10-22 |
| JP7158378B2 JP7158378B2 (ja) | 2022-10-21 |
Family
ID=61690584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019515862A Active JP7158378B2 (ja) | 2016-09-23 | 2017-09-22 | インスリン受容体との結合力が減少された、インスリンアナログ及びその用途 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US11396534B2 (https=) |
| EP (1) | EP3517544B1 (https=) |
| JP (1) | JP7158378B2 (https=) |
| KR (1) | KR102698929B1 (https=) |
| CN (1) | CN110546161B (https=) |
| AR (1) | AR109552A1 (https=) |
| AU (1) | AU2017332408B2 (https=) |
| BR (1) | BR112019005637A2 (https=) |
| CA (1) | CA3037844A1 (https=) |
| RU (1) | RU2764197C1 (https=) |
| TW (1) | TWI774694B (https=) |
| WO (1) | WO2018056764A1 (https=) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2018107117A1 (en) | 2016-12-09 | 2018-06-14 | Akston Biosciences Corporation | Insulin-fc fusions and methods of use |
| KR102629006B1 (ko) * | 2017-03-23 | 2024-01-25 | 한미약품 주식회사 | 인슐린 수용체와의 결합력이 감소된 인슐린 아날로그의 결합체 및 이의 용도 |
| KR20210029210A (ko) | 2018-06-29 | 2021-03-15 | 악스톤 바이오사이언시스 코퍼레이션 | 초장기 작용 인슐린-fc 융합 단백질 및 사용 방법 |
| US11267862B2 (en) | 2018-06-29 | 2022-03-08 | Akston Biosciences Corporation | Ultra-long acting insulin-Fc fusion proteins and methods of use |
| KR20210102347A (ko) | 2018-12-11 | 2021-08-19 | 사노피 | 인슐린 수용체 결합 친화성이 감소된 인슐린 유사체 |
| KR20250142943A (ko) | 2019-12-19 | 2025-09-30 | 악스톤 바이오사이언시스 코퍼레이션 | 초-장기 작용 인슐린-fc 융합 단백질 및 사용 방법 |
| US11186623B2 (en) | 2019-12-24 | 2021-11-30 | Akston Bioscience Corporation | Ultra-long acting insulin-Fc fusion proteins and methods of use |
| US11192930B2 (en) | 2020-04-10 | 2021-12-07 | Askton Bioscences Corporation | Ultra-long acting insulin-Fc fusion protein and methods of use |
| LT3972987T (lt) | 2020-04-10 | 2023-09-25 | Akston Biosciences Corporation | Antigenui specifinė imunoterapija, skirta sulietiems covid-19 baltymams ir naudojimo būdai |
| US11198719B2 (en) | 2020-04-29 | 2021-12-14 | Akston Biosciences Corporation | Ultra-long acting insulin-Fc fusion protein and methods of use |
| EP4373861A4 (en) | 2021-07-23 | 2025-08-20 | Akston Biosciences Corp | INSULIN-FC FUSION PROTEINS AND METHODS OF USE FOR TREATING CANCER |
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| KR102629006B1 (ko) | 2017-03-23 | 2024-01-25 | 한미약품 주식회사 | 인슐린 수용체와의 결합력이 감소된 인슐린 아날로그의 결합체 및 이의 용도 |
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2017
- 2017-09-22 JP JP2019515862A patent/JP7158378B2/ja active Active
- 2017-09-22 CA CA3037844A patent/CA3037844A1/en active Pending
- 2017-09-22 TW TW106132612A patent/TWI774694B/zh active
- 2017-09-22 US US16/335,490 patent/US11396534B2/en active Active
- 2017-09-22 CN CN201780071757.1A patent/CN110546161B/zh active Active
- 2017-09-22 KR KR1020170122759A patent/KR102698929B1/ko active Active
- 2017-09-22 AU AU2017332408A patent/AU2017332408B2/en active Active
- 2017-09-22 RU RU2019109608A patent/RU2764197C1/ru active
- 2017-09-22 WO PCT/KR2017/010504 patent/WO2018056764A1/ko not_active Ceased
- 2017-09-22 BR BR112019005637A patent/BR112019005637A2/pt unknown
- 2017-09-22 EP EP17853478.0A patent/EP3517544B1/en active Active
- 2017-09-25 AR ARP170102640A patent/AR109552A1/es unknown
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