JP2016501851A5 - - Google Patents
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- JP2016501851A5 JP2016501851A5 JP2015543111A JP2015543111A JP2016501851A5 JP 2016501851 A5 JP2016501851 A5 JP 2016501851A5 JP 2015543111 A JP2015543111 A JP 2015543111A JP 2015543111 A JP2015543111 A JP 2015543111A JP 2016501851 A5 JP2016501851 A5 JP 2016501851A5
- Authority
- JP
- Japan
- Prior art keywords
- polypeptide
- amide
- salt
- ester
- amino acid
- 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.)
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- 108090000765 processed proteins & peptides Proteins 0.000 claims description 69
- 229920001184 polypeptide Polymers 0.000 claims description 66
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 66
- 150000001408 amides Chemical class 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 42
- 150000002148 esters Chemical class 0.000 claims description 40
- 150000008574 D-amino acids Chemical group 0.000 claims description 26
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 206010007556 Cardiac failure acute Diseases 0.000 claims description 6
- SNDPXSYFESPGGJ-SCSAIBSYSA-N D-2-aminopentanoic acid Chemical compound CCC[C@@H](N)C(O)=O SNDPXSYFESPGGJ-SCSAIBSYSA-N 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 5
- UUUHXMGGBIUAPW-UHFFFAOYSA-N 1-[1-[2-[[5-amino-2-[[1-[5-(diaminomethylideneamino)-2-[[1-[3-(1h-indol-3-yl)-2-[(5-oxopyrrolidine-2-carbonyl)amino]propanoyl]pyrrolidine-2-carbonyl]amino]pentanoyl]pyrrolidine-2-carbonyl]amino]-5-oxopentanoyl]amino]-3-methylpentanoyl]pyrrolidine-2-carbon Chemical compound C1CCC(C(=O)N2C(CCC2)C(O)=O)N1C(=O)C(C(C)CC)NC(=O)C(CCC(N)=O)NC(=O)C1CCCN1C(=O)C(CCCN=C(N)N)NC(=O)C1CCCN1C(=O)C(CC=1C2=CC=CC=C2NC=1)NC(=O)C1CCC(=O)N1 UUUHXMGGBIUAPW-UHFFFAOYSA-N 0.000 claims description 4
- SNDPXSYFESPGGJ-UHFFFAOYSA-N 2-aminopentanoic acid Chemical compound CCCC(N)C(O)=O SNDPXSYFESPGGJ-UHFFFAOYSA-N 0.000 claims description 4
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims description 4
- 101800000407 Brain natriuretic peptide 32 Proteins 0.000 claims description 4
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 4
- ROHFNLRQFUQHCH-RXMQYKEDSA-N D-leucine Chemical compound CC(C)C[C@@H](N)C(O)=O ROHFNLRQFUQHCH-RXMQYKEDSA-N 0.000 claims description 4
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims description 4
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims description 4
- 239000000480 calcium channel blocker Substances 0.000 claims description 4
- 239000003795 chemical substances by application Substances 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 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 4
- 239000003112 inhibitor Substances 0.000 claims description 4
- 238000000034 method Methods 0.000 claims description 4
- 108091008803 APLNR Proteins 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 3
- 206010059027 Brugada syndrome Diseases 0.000 claims description 3
- 206010007558 Cardiac failure chronic Diseases 0.000 claims description 3
- 208000031229 Cardiomyopathies Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- 206010016807 Fluid retention Diseases 0.000 claims description 3
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims description 3
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims description 3
- 206010042496 Sunburn Diseases 0.000 claims description 3
- 208000032109 Transient ischaemic attack Diseases 0.000 claims description 3
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 3
- 230000008484 agonism Effects 0.000 claims description 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 208000004104 gestational diabetes Diseases 0.000 claims description 3
- 230000000302 ischemic effect Effects 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 201000011461 pre-eclampsia Diseases 0.000 claims description 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 201000010875 transient cerebral ischemia Diseases 0.000 claims description 3
- 230000009529 traumatic brain injury Effects 0.000 claims description 3
- 206010047302 ventricular tachycardia Diseases 0.000 claims description 3
- NRCSJHVDTAAISV-QMMMGPOBSA-N (2s)-2-amino-3-(3,4-dichlorophenyl)propanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=C(Cl)C(Cl)=C1 NRCSJHVDTAAISV-QMMMGPOBSA-N 0.000 claims description 2
- 125000001431 2-aminoisobutyric acid group Chemical group [#6]C([#6])(N*)C(*)=O 0.000 claims description 2
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical group OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims description 2
- MVEOHWRUBFWKJY-UHFFFAOYSA-N 7-hydroxynaphthalene-2-sulfonic acid Chemical compound C1=CC(S(O)(=O)=O)=CC2=CC(O)=CC=C21 MVEOHWRUBFWKJY-UHFFFAOYSA-N 0.000 claims description 2
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims description 2
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims description 2
- 101800002247 Brain natriuretic peptide 45 Proteins 0.000 claims description 2
- BWKMGYQJPOAASG-SECBINFHSA-N D-1,2,3,4-Tetrahydroisoquinoline-3-carboxylic acid Chemical compound C1=CC=C2CN[C@@H](C(=O)O)CC2=C1 BWKMGYQJPOAASG-SECBINFHSA-N 0.000 claims description 2
- XUJNEKJLAYXESH-UWTATZPHSA-N D-Cysteine Chemical compound SC[C@@H](N)C(O)=O XUJNEKJLAYXESH-UWTATZPHSA-N 0.000 claims description 2
- LRQKBLKVPFOOQJ-RXMQYKEDSA-N D-norleucine Chemical group CCCC[C@@H](N)C(O)=O LRQKBLKVPFOOQJ-RXMQYKEDSA-N 0.000 claims description 2
- 102000002045 Endothelin Human genes 0.000 claims description 2
- 108050009340 Endothelin Proteins 0.000 claims description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 2
- OUYCCCASQSFEME-QMMMGPOBSA-N L-Tyrosine Natural products OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 claims description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 2
- HXEACLLIILLPRG-YFKPBYRVSA-N L-pipecolic acid Chemical compound [O-]C(=O)[C@@H]1CCCC[NH2+]1 HXEACLLIILLPRG-YFKPBYRVSA-N 0.000 claims description 2
- 125000003798 L-tyrosyl group Chemical group [H]N([H])[C@]([H])(C(=O)[*])C([H])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims description 2
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims description 2
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims description 2
- 102000003743 Relaxin Human genes 0.000 claims description 2
- 108090000103 Relaxin Proteins 0.000 claims description 2
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 claims description 2
- 235000004279 alanine Nutrition 0.000 claims description 2
- FUOOLUPWFVMBKG-UHFFFAOYSA-N alpha-amino-isobutyric acid Natural products CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims description 2
- QWCKQJZIFLGMSD-UHFFFAOYSA-N alpha-aminobutyric acid Chemical compound CCC(N)C(O)=O QWCKQJZIFLGMSD-UHFFFAOYSA-N 0.000 claims description 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 2
- 239000005557 antagonist Substances 0.000 claims description 2
- 230000003178 anti-diabetic effect Effects 0.000 claims description 2
- 230000003579 anti-obesity Effects 0.000 claims description 2
- 239000003146 anticoagulant agent Substances 0.000 claims description 2
- 229940127219 anticoagulant drug Drugs 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims description 2
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims description 2
- 210000004899 c-terminal region Anatomy 0.000 claims description 2
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims description 2
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 230000001882 diuretic effect Effects 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 2
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 claims description 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 2
- HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 claims description 2
- HPNRHPKXQZSDFX-OAQDCNSJSA-N nesiritide Chemical compound C([C@H]1C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@H](C(N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CSSC[C@@H](C(=O)N1)NC(=O)CNC(=O)[C@H](CO)NC(=O)CNC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](CCSC)NC(=O)[C@H](CCCCN)NC(=O)[C@H]1N(CCC1)C(=O)[C@@H](N)CO)C(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1N=CNC=1)C(O)=O)=O)[C@@H](C)CC)C1=CC=CC=C1 HPNRHPKXQZSDFX-OAQDCNSJSA-N 0.000 claims description 2
- 229960001267 nesiritide Drugs 0.000 claims description 2
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 239000003087 receptor blocking agent Substances 0.000 claims description 2
- 239000002461 renin inhibitor Substances 0.000 claims description 2
- 229940086526 renin-inhibitors Drugs 0.000 claims description 2
- 229960004441 tyrosine Drugs 0.000 claims description 2
- ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 claims description 2
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000000753 cycloalkyl group Chemical group 0.000 claims 4
- 102000008100 Human Serum Albumin Human genes 0.000 claims 3
- 108091006905 Human Serum Albumin Proteins 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 2
- WCZSMQWMSBJQMP-UHFFFAOYSA-N 1-(4-phenoxyphenyl)piperidine Chemical compound C1CCCCN1C(C=C1)=CC=C1OC1=CC=CC=C1 WCZSMQWMSBJQMP-UHFFFAOYSA-N 0.000 description 1
- 230000009787 cardiac fibrosis Effects 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- -1 salt ester Chemical class 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261728395P | 2012-11-20 | 2012-11-20 | |
| US61/728,395 | 2012-11-20 | ||
| US201361781397P | 2013-03-14 | 2013-03-14 | |
| US61/781,397 | 2013-03-14 | ||
| US201361858251P | 2013-07-25 | 2013-07-25 | |
| US61/858,251 | 2013-07-25 | ||
| PCT/US2013/070742 WO2014081702A2 (en) | 2012-11-20 | 2013-11-19 | Synthetic linear apelin mimetics for the treatment of heart failure |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018122192A Division JP2018172410A (ja) | 2012-11-20 | 2018-06-27 | 心不全治療用の合成鎖状アペリン模倣物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016501851A JP2016501851A (ja) | 2016-01-21 |
| JP2016501851A5 true JP2016501851A5 (enExample) | 2016-12-28 |
| JP6444882B2 JP6444882B2 (ja) | 2018-12-26 |
Family
ID=49876968
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015543111A Expired - Fee Related JP6444882B2 (ja) | 2012-11-20 | 2013-11-19 | 心不全治療用の合成鎖状アペリン模倣物 |
| JP2018122192A Pending JP2018172410A (ja) | 2012-11-20 | 2018-06-27 | 心不全治療用の合成鎖状アペリン模倣物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018122192A Pending JP2018172410A (ja) | 2012-11-20 | 2018-06-27 | 心不全治療用の合成鎖状アペリン模倣物 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US10005829B2 (enExample) |
| EP (1) | EP2922559B1 (enExample) |
| JP (2) | JP6444882B2 (enExample) |
| CN (1) | CN105007928B (enExample) |
| AR (1) | AR093559A1 (enExample) |
| ES (1) | ES2705323T3 (enExample) |
| TW (1) | TW201425339A (enExample) |
| UY (1) | UY35144A (enExample) |
| WO (1) | WO2014081702A2 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
| US9683018B2 (en) | 2013-07-25 | 2017-06-20 | Novartis Ag | Disulfide cyclic polypeptides for the treatment of heart failure |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| EP3157942B1 (en) | 2014-06-23 | 2020-06-17 | Novartis AG | Site specific protein modifications |
| JP6758294B2 (ja) * | 2014-12-23 | 2020-09-23 | アンスティチュ ナショナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシュ メディカル | アペリン受容体により媒介される疾患の処置における代謝的に安定なアペリン類似体 |
| WO2017140684A2 (en) | 2016-02-15 | 2017-08-24 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of post-operative cognitive dysfunction |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| WO2019008438A1 (en) | 2017-07-03 | 2019-01-10 | The Governors Of The University Of Alberta | APELIN PEPTIDES AND USES THEREOF |
| CN109771634A (zh) * | 2017-07-11 | 2019-05-21 | 南华大学 | 含有apelin 12环肽的药物组合物及用途 |
| US10905738B2 (en) * | 2018-07-05 | 2021-02-02 | Biozeus Desenvolvimento De Produtos Biofarmacêuticos | Synthetic peptides, prodrugs, pharmaceutical compositions and uses |
| WO2021030687A1 (en) * | 2019-08-15 | 2021-02-18 | Cohbar, Inc. | Therapeutic peptides |
| CN114099642A (zh) * | 2021-11-12 | 2022-03-01 | 南通大学 | 基因Apln在制备治疗与细胞成血管有关疾病药物中的应用 |
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-
2013
- 2013-11-18 UY UY0001035144A patent/UY35144A/es unknown
- 2013-11-19 ES ES13811648T patent/ES2705323T3/es active Active
- 2013-11-19 CN CN201380070626.3A patent/CN105007928B/zh not_active Expired - Fee Related
- 2013-11-19 TW TW102142121A patent/TW201425339A/zh unknown
- 2013-11-19 US US14/440,198 patent/US10005829B2/en not_active Expired - Fee Related
- 2013-11-19 WO PCT/US2013/070742 patent/WO2014081702A2/en not_active Ceased
- 2013-11-19 JP JP2015543111A patent/JP6444882B2/ja not_active Expired - Fee Related
- 2013-11-19 EP EP13811648.8A patent/EP2922559B1/en not_active Not-in-force
- 2013-11-20 AR ARP130104278A patent/AR093559A1/es unknown
-
2018
- 2018-06-27 JP JP2018122192A patent/JP2018172410A/ja active Pending
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