JP2016527248A5 - - Google Patents
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- Publication number
- JP2016527248A5 JP2016527248A5 JP2016529805A JP2016529805A JP2016527248A5 JP 2016527248 A5 JP2016527248 A5 JP 2016527248A5 JP 2016529805 A JP2016529805 A JP 2016529805A JP 2016529805 A JP2016529805 A JP 2016529805A JP 2016527248 A5 JP2016527248 A5 JP 2016527248A5
- Authority
- JP
- Japan
- Prior art keywords
- polypeptide
- side chain
- amide
- ester
- salt
- 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
Links
- 108090000765 processed proteins & peptides Proteins 0.000 claims 28
- 229920001184 polypeptide Polymers 0.000 claims 26
- 102000004196 processed proteins & peptides Human genes 0.000 claims 26
- 150000001408 amides Chemical class 0.000 claims 13
- 150000002148 esters Chemical class 0.000 claims 13
- 150000003839 salts Chemical class 0.000 claims 13
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 6
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000002228 disulfide group Chemical group 0.000 claims 3
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims 2
- 101800000407 Brain natriuretic peptide 32 Proteins 0.000 claims 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 2
- 206010007556 Cardiac failure acute Diseases 0.000 claims 2
- 150000001413 amino acids Chemical class 0.000 claims 2
- 239000000480 calcium channel blocker Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 2
- 239000003087 receptor blocking agent Substances 0.000 claims 2
- 125000001431 2-aminoisobutyric acid group Chemical group [#6]C([#6])(N*)C(*)=O 0.000 claims 1
- 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 1
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical group OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims 1
- 108091008803 APLNR Proteins 0.000 claims 1
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 1
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 1
- 101800002247 Brain natriuretic peptide 45 Proteins 0.000 claims 1
- 206010059027 Brugada syndrome Diseases 0.000 claims 1
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 1
- 208000031229 Cardiomyopathies Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- FFFHZYDWPBMWHY-GSVOUGTGSA-N D-Homocysteine Chemical compound OC(=O)[C@H](N)CCS FFFHZYDWPBMWHY-GSVOUGTGSA-N 0.000 claims 1
- LRQKBLKVPFOOQJ-RXMQYKEDSA-N D-norleucine Chemical group CCCC[C@@H](N)C(O)=O LRQKBLKVPFOOQJ-RXMQYKEDSA-N 0.000 claims 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 1
- 206010016807 Fluid retention Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 102000008100 Human Serum Albumin Human genes 0.000 claims 1
- 108091006905 Human Serum Albumin Proteins 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- FFFHZYDWPBMWHY-UHFFFAOYSA-N L-Homocysteine Natural products OC(=O)C(N)CCS FFFHZYDWPBMWHY-UHFFFAOYSA-N 0.000 claims 1
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical compound OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 claims 1
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 1
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 1
- 208000008589 Obesity Diseases 0.000 claims 1
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 1
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 1
- 102000003743 Relaxin Human genes 0.000 claims 1
- 108090000103 Relaxin Proteins 0.000 claims 1
- 206010042496 Sunburn Diseases 0.000 claims 1
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 1
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 1
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 claims 1
- 230000008484 agonism Effects 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 229940126317 angiotensin II receptor antagonist Drugs 0.000 claims 1
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims 1
- 230000003178 anti-diabetic effect Effects 0.000 claims 1
- 230000003579 anti-obesity Effects 0.000 claims 1
- 239000003146 anticoagulant agent Substances 0.000 claims 1
- 229940127219 anticoagulant drug Drugs 0.000 claims 1
- 239000003472 antidiabetic agent Substances 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 230000006793 arrhythmia Effects 0.000 claims 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 1
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims 1
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 208000002296 eclampsia Diseases 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 208000004104 gestational diabetes Diseases 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 230000000302 ischemic effect Effects 0.000 claims 1
- 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 1
- 229960001267 nesiritide Drugs 0.000 claims 1
- 235000020824 obesity Nutrition 0.000 claims 1
- 201000011461 pre-eclampsia Diseases 0.000 claims 1
- 208000002815 pulmonary hypertension Diseases 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- 208000037803 restenosis Diseases 0.000 claims 1
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 1
- 230000009529 traumatic brain injury Effects 0.000 claims 1
- 206010047302 ventricular tachycardia Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361858280P | 2013-07-25 | 2013-07-25 | |
| US61/858,280 | 2013-07-25 | ||
| PCT/US2014/047372 WO2015013165A1 (en) | 2013-07-25 | 2014-07-21 | Cyclic apelin derivatives for the treatment of heart failure |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016527248A JP2016527248A (ja) | 2016-09-08 |
| JP2016527248A5 true JP2016527248A5 (enExample) | 2017-08-31 |
| JP6505691B2 JP6505691B2 (ja) | 2019-04-24 |
Family
ID=51301346
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016529805A Expired - Fee Related JP6505691B2 (ja) | 2013-07-25 | 2014-07-21 | 心不全治療用の環状アペリン誘導体 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9908919B2 (enExample) |
| EP (1) | EP3024846A1 (enExample) |
| JP (1) | JP6505691B2 (enExample) |
| CN (1) | CN105612173A (enExample) |
| WO (1) | WO2015013165A1 (enExample) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8673848B2 (en) | 2012-01-27 | 2014-03-18 | Novartis Ag | Synthetic apelin mimetics for the treatment of heart failure |
| UY35144A (es) * | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| EP3024845A1 (en) | 2013-07-25 | 2016-06-01 | Novartis AG | Cyclic polypeptides for the treatment of heart failure |
| EP3024847A1 (en) | 2013-07-25 | 2016-06-01 | Novartis AG | Disulfide cyclic polypeptides for the treatment of heart failure |
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
| CN105705167A (zh) | 2013-07-25 | 2016-06-22 | 诺华股份有限公司 | 合成的apelin多肽的生物缀合物 |
| ES2818109T3 (es) | 2014-06-23 | 2021-04-09 | Novartis Ag | Modificaciones de proteínas específicas para un sitio |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| US10849992B1 (en) * | 2015-04-07 | 2020-12-01 | Alector Llc | Methods of screening for sortilin binding antagonists |
| ES2930077T3 (es) * | 2016-02-15 | 2022-12-07 | Inst Nat Sante Rech Med | Apelina para su uso en el tratamiento de la disfunción cognitiva posoperatoria |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| CN112007027B (zh) * | 2020-09-14 | 2022-07-15 | 长春金赛药业有限责任公司 | 含酯基芳香丙酰胺类化合物及其代谢产物在制备治疗心衰药物中的应用 |
Family Cites Families (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8673848B2 (en) * | 2012-01-27 | 2014-03-18 | Novartis Ag | Synthetic apelin mimetics for the treatment of heart failure |
| US20070191272A1 (en) * | 2005-09-27 | 2007-08-16 | Stemmer Willem P | Proteinaceous pharmaceuticals and uses thereof |
| WO2009155556A2 (en) * | 2008-06-20 | 2009-12-23 | The Board Of Regents Of The University Of Texas System | Crkl targeting peptides |
| KR20110091702A (ko) * | 2008-11-04 | 2011-08-12 | 앵커 테라퓨틱스, 인코포레이티드 | Apj 수용체 화합물 |
| US9229013B2 (en) * | 2009-05-05 | 2016-01-05 | B.R.A.H.M.S Gmbh | Vasoactive hormone-based stratification of patients suffering from diseases related to endothelial function/dysfunction |
| HRP20160547T1 (hr) * | 2011-03-11 | 2016-06-17 | Genzyme Corporation | Pegilirani apelin i njegova upotreba |
| CU23950B1 (es) * | 2011-03-21 | 2013-10-29 | Ct De Ingeniería Genética Y Biotecnología | Péptidos cíclicos con actividad antineoplásica y antiangiogénica |
| BR112014000474A2 (pt) * | 2011-07-08 | 2017-02-21 | Bayer Ip Gmbh | proteínas de fusão libertadoras de relaxina e suas utilizações |
| UY35144A (es) | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| ES2732574T3 (es) * | 2012-11-30 | 2019-11-25 | Novartis Ag | Métodos para preparar conjugados a partir de proteínas que contienen disulfuro |
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
| CN105705167A (zh) * | 2013-07-25 | 2016-06-22 | 诺华股份有限公司 | 合成的apelin多肽的生物缀合物 |
| EP3024845A1 (en) | 2013-07-25 | 2016-06-01 | Novartis AG | Cyclic polypeptides for the treatment of heart failure |
| EP3024847A1 (en) | 2013-07-25 | 2016-06-01 | Novartis AG | Disulfide cyclic polypeptides for the treatment of heart failure |
-
2014
- 2014-07-21 WO PCT/US2014/047372 patent/WO2015013165A1/en not_active Ceased
- 2014-07-21 JP JP2016529805A patent/JP6505691B2/ja not_active Expired - Fee Related
- 2014-07-21 CN CN201480052673.XA patent/CN105612173A/zh active Pending
- 2014-07-21 EP EP14750267.8A patent/EP3024846A1/en not_active Withdrawn
- 2014-07-21 US US14/905,333 patent/US9908919B2/en not_active Expired - Fee Related
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