JP2016531110A5 - - Google Patents
Download PDFInfo
- Publication number
- JP2016531110A5 JP2016531110A5 JP2016529806A JP2016529806A JP2016531110A5 JP 2016531110 A5 JP2016531110 A5 JP 2016531110A5 JP 2016529806 A JP2016529806 A JP 2016529806A JP 2016529806 A JP2016529806 A JP 2016529806A JP 2016531110 A5 JP2016531110 A5 JP 2016531110A5
- 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 31
- 229920001184 polypeptide Polymers 0.000 claims 29
- 102000004196 processed proteins & peptides Human genes 0.000 claims 29
- 150000001408 amides Chemical class 0.000 claims 15
- 150000002148 esters Chemical class 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 15
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 7
- 210000004899 c-terminal region Anatomy 0.000 claims 4
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims 4
- 239000003814 drug Substances 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
- 125000002228 disulfide group Chemical group 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
- 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
- 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
- 239000003937 drug carrier Substances 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
- 230000002265 prevention Effects 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 |
|---|---|---|---|
| US201361858290P | 2013-07-25 | 2013-07-25 | |
| US61/858,290 | 2013-07-25 | ||
| PCT/US2014/047375 WO2015013167A1 (en) | 2013-07-25 | 2014-07-21 | Disulfide cyclic polypeptides for the treatment of heart failure |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016531110A JP2016531110A (ja) | 2016-10-06 |
| JP2016531110A5 true JP2016531110A5 (enExample) | 2017-08-31 |
| JP6505692B2 JP6505692B2 (ja) | 2019-04-24 |
Family
ID=51352764
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016529806A Expired - Fee Related JP6505692B2 (ja) | 2013-07-25 | 2014-07-21 | 心不全治療のためのジスルフィド環状ポリペプチド |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US9683018B2 (enExample) |
| EP (1) | EP3024847A1 (enExample) |
| JP (1) | JP6505692B2 (enExample) |
| CN (1) | CN105612174A (enExample) |
| WO (1) | WO2015013167A1 (enExample) |
Families Citing this family (15)
| 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 |
| SG11201600211XA (en) | 2013-07-25 | 2016-02-26 | Novartis Ag | Cyclic polypeptides for the treatment of heart failure |
| TW201518323A (zh) | 2013-07-25 | 2015-05-16 | Novartis Ag | 合成apelin多肽之生物結合物 |
| 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 |
| EP3157942B1 (en) | 2014-06-23 | 2020-06-17 | Novartis AG | Site specific protein modifications |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| AU2016340472B2 (en) | 2015-10-23 | 2019-02-28 | Fujifilm Corporation | Cyclic peptide, affinity chromatography support, labeled antibody, antibody-drug conjugate, and pharmaceutical preparation |
| WO2017069269A1 (ja) * | 2015-10-23 | 2017-04-27 | 富士フイルム株式会社 | 環状ペプチド、アフィニティクロマトグラフィー担体、標識化抗体、抗体薬物複合体、および医薬製剤 |
| EP3205664A1 (en) * | 2016-02-11 | 2017-08-16 | Polypeptide Laboratories Holding (PPL) AB | Method for preparation of liraglutide using bal linker |
| WO2018013053A1 (en) * | 2016-07-15 | 2018-01-18 | Agency For Science, Technology And Research | Methods of diagnosis and treatment of pre-eclampsia |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| WO2019207427A2 (en) * | 2018-04-25 | 2019-10-31 | Janssen Pharmaceutica Nv | Thioether cyclic peptide amylin receptor modulators |
| WO2019229242A1 (en) | 2018-05-31 | 2019-12-05 | Novo Nordisk A/S | Derivatives comprising an apelin analogue and uses thereof |
Family Cites Families (15)
| 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 |
| US20070212703A1 (en) * | 2005-09-27 | 2007-09-13 | 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 |
| BRPI0921815A2 (pt) * | 2008-11-04 | 2018-10-09 | Anchor Therapeutics Inc | compostos receptores de apj |
| CN102428368B (zh) * | 2009-05-05 | 2015-04-22 | B.R.A.H.M.S有限公司 | 患有内皮功能/功能障碍相关疾病的患者的基于血管活性激素的分层 |
| EP3045183B1 (en) * | 2011-03-11 | 2018-07-04 | Genzyme Corporation | Pegylated apelin and uses thereof |
| CU23950B1 (es) * | 2011-03-21 | 2013-10-29 | Ct De Ingeniería Genética Y Biotecnología | Péptidos cíclicos con actividad antineoplásica y antiangiogénica |
| MX2014000316A (es) * | 2011-07-08 | 2014-02-19 | Bayer Ip Gmbh | Proteinas de fusion liberadoras de relaxina y usos de las mismas. |
| US8921307B2 (en) * | 2012-11-20 | 2014-12-30 | Novartis Ag | Synthetic linear 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 |
| AU2013350802B2 (en) | 2012-11-30 | 2016-07-14 | Novartis Ag | Methods for making conjugates from disulfide-containing proteins |
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
| TW201518323A (zh) | 2013-07-25 | 2015-05-16 | Novartis Ag | 合成apelin多肽之生物結合物 |
| US9683018B2 (en) | 2013-07-25 | 2017-06-20 | Novartis Ag | Disulfide cyclic polypeptides for the treatment of heart failure |
| SG11201600211XA (en) * | 2013-07-25 | 2016-02-26 | Novartis Ag | Cyclic polypeptides for the treatment of heart failure |
-
2014
- 2014-07-21 US US14/905,338 patent/US9683018B2/en not_active Expired - Fee Related
- 2014-07-21 WO PCT/US2014/047375 patent/WO2015013167A1/en not_active Ceased
- 2014-07-21 JP JP2016529806A patent/JP6505692B2/ja not_active Expired - Fee Related
- 2014-07-21 CN CN201480052701.8A patent/CN105612174A/zh active Pending
- 2014-07-21 EP EP14750842.8A patent/EP3024847A1/en not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2016531110A5 (enExample) | ||
| JP2016527248A5 (enExample) | ||
| JP2016527249A5 (enExample) | ||
| JP2016532681A5 (enExample) | ||
| JP2015506370A5 (enExample) | ||
| JP2018048157A5 (enExample) | ||
| SI2807183T1 (en) | Synthetic appel mimetics for the treatment of cardiac insufficiency | |
| JP2016501851A5 (enExample) | ||
| ES2257298T3 (es) | Proteccion de peptidos terapeuticos endogenos contra la actividad de la peptidasa a traves de la conjugacion con componentes sanguineos. | |
| PH12016500103A1 (en) | Bioconjugates of synthetic apelin polypeptides | |
| JP2016512213A5 (enExample) | ||
| JP2011511753A5 (enExample) | ||
| JP2012505902A5 (enExample) | ||
| JP2013515057A5 (enExample) | ||
| JP2011524420A5 (enExample) | ||
| JP2013518115A5 (enExample) | ||
| JP2014508510A5 (enExample) | ||
| JP2013515055A5 (enExample) | ||
| JP2007001987A5 (enExample) | ||
| JP2004536077A5 (enExample) | ||
| JP2013504318A5 (enExample) | ||
| JP2020502051A5 (enExample) | ||
| JP2012531219A5 (enExample) | ||
| JP2019510739A5 (enExample) | ||
| JP2010536356A5 (enExample) |