JP2017526620A5 - - Google Patents
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- JP2017526620A5 JP2017526620A5 JP2016572433A JP2016572433A JP2017526620A5 JP 2017526620 A5 JP2017526620 A5 JP 2017526620A5 JP 2016572433 A JP2016572433 A JP 2016572433A JP 2016572433 A JP2016572433 A JP 2016572433A JP 2017526620 A5 JP2017526620 A5 JP 2017526620A5
- Authority
- JP
- Japan
- Prior art keywords
- isolated polypeptide
- heart failure
- amino acid
- composition
- item
- 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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- 108090000765 processed proteins & peptides Proteins 0.000 claims description 115
- 229920001184 polypeptide Polymers 0.000 claims description 113
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 113
- 206010019280 Heart failures Diseases 0.000 claims description 33
- ODKSFYDXXFIFQN-UHFFFAOYSA-N Arginine Chemical compound OC(=O)C(N)CCCNC(N)=N ODKSFYDXXFIFQN-UHFFFAOYSA-N 0.000 claims description 26
- 230000002526 effect on cardiovascular system Effects 0.000 claims description 26
- 150000001413 amino acids Chemical group 0.000 claims description 24
- 235000001014 amino acid Nutrition 0.000 claims description 22
- -1 tridecanoyl Chemical group 0.000 claims description 22
- 102000018746 Apelin Human genes 0.000 claims description 20
- 108010052412 Apelin Proteins 0.000 claims description 20
- 125000002252 acyl group Chemical group 0.000 claims description 18
- 125000001931 aliphatic group Chemical group 0.000 claims description 16
- 239000002202 Polyethylene glycol Substances 0.000 claims description 14
- 229920001223 polyethylene glycol Polymers 0.000 claims description 14
- 230000001684 chronic effect Effects 0.000 claims description 12
- 239000003814 drug Substances 0.000 claims description 12
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 12
- 229920000642 polymer Polymers 0.000 claims description 12
- BWVPHIKGXQBZPV-QKFDDRBGSA-N apelin Chemical compound NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N1CCC[C@H]1C(=O)N[C@@H](CC(C)C)C(=O)N1[C@H](C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(O)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=2NC=NC=2)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CCC(N)=O)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(N)=O)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C3=CC=CC=C3NC=2)C(=O)N[C@@H](CCC(N)=O)C(=O)NCC(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC=2C=CC=CC=2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CC=2NC=NC=2)C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CCSC)C(=O)N2[C@@H](CCC2)C(=O)N[C@@H](CC=2C=CC=CC=2)C(O)=O)CCC1 BWVPHIKGXQBZPV-QKFDDRBGSA-N 0.000 claims description 11
- 230000000747 cardiac effect Effects 0.000 claims description 10
- 125000000628 margaroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 10
- 101100411708 Danio rerio rarga gene Proteins 0.000 claims description 8
- 244000191761 Sida cordifolia Species 0.000 claims description 8
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical compound NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims description 8
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 125000001419 myristoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 125000003696 stearoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 8
- 102400000252 Apelin-13 Human genes 0.000 claims description 6
- 206010007556 Cardiac failure acute Diseases 0.000 claims description 6
- 206010020772 Hypertension Diseases 0.000 claims description 6
- XXCCRHIAIBQDPX-PEWBXTNBSA-N apelin-13 Chemical compound C([C@@H](C(=O)N[C@@H](CCCCN)C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H](CCSC)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(O)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H]1N(CCC1)C(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](N)CCC(N)=O)C1=CN=CN1 XXCCRHIAIBQDPX-PEWBXTNBSA-N 0.000 claims description 6
- 108010040480 apelin-13 peptide Proteins 0.000 claims description 6
- 125000004063 butyryl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000003074 decanoyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C(*)=O 0.000 claims description 6
- 125000003104 hexanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims description 6
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 claims description 6
- 206010007559 Cardiac failure congestive Diseases 0.000 claims description 5
- 208000003037 Diastolic Heart Failure Diseases 0.000 claims description 5
- 208000008253 Systolic Heart Failure Diseases 0.000 claims description 5
- 230000003205 diastolic effect Effects 0.000 claims description 5
- 208000038002 heart failure with reduced ejection fraction Diseases 0.000 claims description 5
- 150000008574 D-amino acids Chemical class 0.000 claims description 4
- 108060003951 Immunoglobulin Proteins 0.000 claims description 4
- 150000001576 beta-amino acids Chemical class 0.000 claims description 4
- DIOQZVSQGTUSAI-UHFFFAOYSA-N decane Chemical compound CCCCCCCCCC DIOQZVSQGTUSAI-UHFFFAOYSA-N 0.000 claims description 4
- SNRUBQQJIBEYMU-UHFFFAOYSA-N dodecane Chemical compound CCCCCCCCCCCC SNRUBQQJIBEYMU-UHFFFAOYSA-N 0.000 claims description 4
- 102000018358 immunoglobulin Human genes 0.000 claims description 4
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 4
- 229920006395 saturated elastomer Polymers 0.000 claims description 4
- 125000006850 spacer group Chemical group 0.000 claims description 4
- 208000038003 heart failure with preserved ejection fraction Diseases 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- NPWMTBZSRRLQNJ-VKHMYHEASA-N (3s)-3-aminopiperidine-2,6-dione Chemical compound N[C@H]1CCC(=O)NC1=O NPWMTBZSRRLQNJ-VKHMYHEASA-N 0.000 claims description 2
- YQZVQKYXWPIKIX-UHFFFAOYSA-N 2-[2-[2-[[2-[2-(2-aminoethoxy)ethoxy]acetyl]amino]ethoxy]ethoxy]acetic acid Chemical compound NCCOCCOCC(=O)NCCOCCOCC(O)=O YQZVQKYXWPIKIX-UHFFFAOYSA-N 0.000 claims description 2
- JPZXHKDZASGCLU-GFCCVEGCSA-N 3-(2-Naphthyl)-D-Alanine Chemical compound C1=CC=CC2=CC(C[C@@H](N)C(O)=O)=CC=C21 JPZXHKDZASGCLU-GFCCVEGCSA-N 0.000 claims description 2
- DKIDEFUBRARXTE-UHFFFAOYSA-N 3-mercaptopropanoic acid Chemical compound OC(=O)CCS DKIDEFUBRARXTE-UHFFFAOYSA-N 0.000 claims description 2
- FWMNVWWHGCHHJJ-SKKKGAJSSA-N 4-amino-1-[(2r)-6-amino-2-[[(2r)-2-[[(2r)-2-[[(2r)-2-amino-3-phenylpropanoyl]amino]-3-phenylpropanoyl]amino]-4-methylpentanoyl]amino]hexanoyl]piperidine-4-carboxylic acid Chemical compound C([C@H](C(=O)N[C@H](CC(C)C)C(=O)N[C@H](CCCCN)C(=O)N1CCC(N)(CC1)C(O)=O)NC(=O)[C@H](N)CC=1C=CC=CC=1)C1=CC=CC=C1 FWMNVWWHGCHHJJ-SKKKGAJSSA-N 0.000 claims description 2
- AHLPHDHHMVZTML-SCSAIBSYSA-N D-Ornithine Chemical compound NCCC[C@@H](N)C(O)=O AHLPHDHHMVZTML-SCSAIBSYSA-N 0.000 claims description 2
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 2
- AKCRVYNORCOYQT-YFKPBYRVSA-N N-methyl-L-valine Chemical compound CN[C@@H](C(C)C)C(O)=O AKCRVYNORCOYQT-YFKPBYRVSA-N 0.000 claims description 2
- 239000004698 Polyethylene Substances 0.000 claims description 2
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims description 2
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims description 2
- 235000008206 alpha-amino acids Nutrition 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000012634 fragment Substances 0.000 claims description 2
- 235000013922 glutamic acid Nutrition 0.000 claims description 2
- 239000004220 glutamic acid Substances 0.000 claims description 2
- YSFZWUJOBANROZ-UHFFFAOYSA-N heptylmalonic acid Chemical compound CCCCCCCC(C(O)=O)C(O)=O YSFZWUJOBANROZ-UHFFFAOYSA-N 0.000 claims description 2
- FXHCFPUEIDRTMR-UHFFFAOYSA-N hydron;1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid;chloride Chemical compound Cl.C1=CC=C2CNC(C(=O)O)CC2=C1 FXHCFPUEIDRTMR-UHFFFAOYSA-N 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 238000006467 substitution reaction Methods 0.000 claims description 2
- 125000002730 succinyl group Chemical group C(CCC(=O)*)(=O)* 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 18
- VLKZOEOYAKHREP-UHFFFAOYSA-N n-Hexane Chemical compound CCCCCC VLKZOEOYAKHREP-UHFFFAOYSA-N 0.000 claims 3
- 230000007170 pathology Effects 0.000 claims 2
- 239000001273 butane Substances 0.000 claims 1
- 230000008602 contraction Effects 0.000 claims 1
- IJDNQMDRQITEOD-UHFFFAOYSA-N n-butane Chemical compound CCCC IJDNQMDRQITEOD-UHFFFAOYSA-N 0.000 claims 1
- OFBQJSOFQDEBGM-UHFFFAOYSA-N n-pentane Natural products CCCCC OFBQJSOFQDEBGM-UHFFFAOYSA-N 0.000 claims 1
- 238000000034 method Methods 0.000 description 18
- 208000024172 Cardiovascular disease Diseases 0.000 description 2
- 206010007558 Cardiac failure chronic Diseases 0.000 description 1
- CDQSJQSWAWPGKG-UHFFFAOYSA-N butane-1,1-diol Chemical compound CCCC(O)O CDQSJQSWAWPGKG-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462010322P | 2014-06-10 | 2014-06-10 | |
| US62/010,322 | 2014-06-10 | ||
| PCT/US2015/035205 WO2015191781A2 (en) | 2014-06-10 | 2015-06-10 | Apelin polypeptides |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019187458A Division JP2020023539A (ja) | 2014-06-10 | 2019-10-11 | アペリンポリペプチド |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017526620A JP2017526620A (ja) | 2017-09-14 |
| JP2017526620A5 true JP2017526620A5 (enExample) | 2018-07-05 |
| JP6803236B2 JP6803236B2 (ja) | 2020-12-23 |
Family
ID=54608924
Family Applications (4)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016572433A Active JP6803236B2 (ja) | 2014-06-10 | 2015-06-10 | アペリンポリペプチド |
| JP2019187458A Pending JP2020023539A (ja) | 2014-06-10 | 2019-10-11 | アペリンポリペプチド |
| JP2021200644A Withdrawn JP2022028961A (ja) | 2014-06-10 | 2021-12-10 | アペリンポリペプチド |
| JP2023210068A Pending JP2024026356A (ja) | 2014-06-10 | 2023-12-13 | アペリンポリペプチド |
Family Applications After (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019187458A Pending JP2020023539A (ja) | 2014-06-10 | 2019-10-11 | アペリンポリペプチド |
| JP2021200644A Withdrawn JP2022028961A (ja) | 2014-06-10 | 2021-12-10 | アペリンポリペプチド |
| JP2023210068A Pending JP2024026356A (ja) | 2014-06-10 | 2023-12-13 | アペリンポリペプチド |
Country Status (8)
| Country | Link |
|---|---|
| US (3) | US10941182B2 (enExample) |
| EP (3) | EP3674314B8 (enExample) |
| JP (4) | JP6803236B2 (enExample) |
| AU (1) | AU2015274574B2 (enExample) |
| CA (1) | CA2951391C (enExample) |
| ES (1) | ES2950789T3 (enExample) |
| MX (1) | MX370689B (enExample) |
| WO (1) | WO2015191781A2 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2016209968B2 (en) | 2015-01-23 | 2018-11-29 | Novartis Ag | Synthetic apelin fatty acid conjugates with improved half-life |
| MX2019008449A (es) | 2017-02-08 | 2019-09-09 | Bristol Myers Squibb Co | Polipetidos de relaxina modificada que comprenden un mejorador farmacocinetico y sus usos. |
| WO2019008438A1 (en) | 2017-07-03 | 2019-01-10 | The Governors Of The University Of Alberta | APELIN PEPTIDES AND USES THEREOF |
| WO2019023295A1 (en) * | 2017-07-27 | 2019-01-31 | Saint Louis University | Fatty acid modified human epidermal growth factor |
| EP4092038A1 (en) | 2017-09-11 | 2022-11-23 | Protagonist Therapeutics, Inc. | Opioid agonist peptides and uses thereof |
| WO2019229242A1 (en) * | 2018-05-31 | 2019-12-05 | Novo Nordisk A/S | Derivatives comprising an apelin analogue and uses thereof |
| TWI848951B (zh) | 2018-06-01 | 2024-07-21 | 瑞士商諾華公司 | 針對ｂｃｍａ之結合分子及其用途 |
| JP2022513626A (ja) | 2018-11-26 | 2022-02-09 | ノバルティス アーゲー | Ｌｐｌ－ｇｐｉｈｂｐ１融合ポリペプチド |
| US12037378B2 (en) | 2019-05-21 | 2024-07-16 | Novartis Ag | Variant CD58 domains and uses thereof |
| BR112021023048A2 (pt) | 2019-05-21 | 2022-04-19 | Novartis Ag | Moléculas de ligação a cd19 e usos das mesmas |
| BR112021026815A2 (pt) * | 2019-07-01 | 2022-06-07 | Valitor Inc | Ligantes hidrofílicos para conjugados de peptídeo multivalentes |
| WO2021030687A1 (en) * | 2019-08-15 | 2021-02-18 | Cohbar, Inc. | Therapeutic peptides |
| CN110669105B (zh) * | 2019-10-31 | 2021-06-11 | 华中科技大学 | 长效多肽构建及其抗急性肾损伤和糖尿病并发肾病的应用 |
| JP7039636B2 (ja) * | 2020-02-19 | 2022-03-22 | ソフトバンク株式会社 | システム、管理装置、監視端末、及びプログラム |
| GB202016149D0 (en) * | 2020-10-12 | 2020-11-25 | Heptares Therapeutics Ltd | Cyclic apelin receptor agonists |
| GB202016152D0 (en) * | 2020-10-12 | 2020-11-25 | Heptares Therapeutics Ltd | Linear Apelin Receptor Agonist |
| AU2021373366A1 (en) | 2020-11-06 | 2023-06-01 | Novartis Ag | Cd19 binding molecules and uses thereof |
| JP2025001049A (ja) * | 2021-09-01 | 2025-01-08 | 積水メディカル株式会社 | アルギニン誘導体 |
| CN116554267A (zh) * | 2022-01-30 | 2023-08-08 | 江苏众红生物工程创药研究院有限公司 | 聚乙二醇修饰的激肽或其变体和药物应用 |
| TW202446782A (zh) * | 2023-04-11 | 2024-12-01 | 美商威特拉公司 | 愛帕琳受體促效劑及其用途 |
| CN119101143A (zh) * | 2023-05-31 | 2024-12-10 | 浙江大学 | 一种G蛋白偏向的apelin-13多肽突变体及应用 |
| WO2025092748A1 (zh) * | 2023-11-01 | 2025-05-08 | 拜西欧斯（北京）生物技术有限公司 | 多肽衍生物、其药物组合物及其用途 |
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