JP2016531110A5 - - Google Patents
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- 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 (https=) | 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 (https=) |
| EP (1) | EP3024847A1 (https=) |
| JP (1) | JP6505692B2 (https=) |
| CN (1) | CN105612174A (https=) |
| WO (1) | WO2015013167A1 (https=) |
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 |
| CN105612174A (zh) | 2013-07-25 | 2016-05-25 | 诺华股份有限公司 | 用于治疗心力衰竭的二硫化物环状多肽 |
| HK1218252A1 (zh) | 2013-07-25 | 2017-02-10 | Novartis Ag | 合成apelin多肽之生物结合物 |
| KR20160031551A (ko) | 2013-07-25 | 2016-03-22 | 노파르티스 아게 | 심부전의 치료를 위한 시클릭 폴리펩티드 |
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
| SG11201609706VA (en) | 2014-06-23 | 2017-01-27 | 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 |
| EP3366693B1 (en) * | 2015-10-23 | 2023-08-16 | 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 |
| CA3097812A1 (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 |
| JP2009509535A (ja) * | 2005-09-27 | 2009-03-12 | アムニクス， インコーポレイテッド | タンパク様薬剤およびその使用 |
| CA2728763A1 (en) * | 2008-06-20 | 2009-12-23 | The Board Of Regents Of The University Of Texas System | Crkl targeting peptides |
| WO2010053545A2 (en) * | 2008-11-04 | 2010-05-14 | Anchor Therapeutics, Inc. | Apj receptor compounds |
| JP5753159B2 (ja) * | 2009-05-05 | 2015-07-22 | ベー．エル．アー．ハー．エム．エス ゲゼルシャフト ミット ベシュレンクテル ハフツング | 内皮性機能／機能不全に関連した疾患に罹患している患者の血管作動性ホルモンに基づいた層化 |
| SI3045183T1 (sl) * | 2011-03-11 | 2018-11-30 | Genzyme Corporation | Pegiliran Apelin in njegove uporabe |
| CU23950B1 (es) * | 2011-03-21 | 2013-10-29 | Ct De Ingeniería Genética Y Biotecnología | Péptidos cíclicos con actividad antineoplásica y antiangiogénica |
| KR20140039257A (ko) * | 2011-07-08 | 2014-04-01 | 바이엘 인텔렉쳐 프로퍼티 게엠베하 | 릴랙신을 방출하는 융합 단백질 및 이의 용도 |
| 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 |
| ES2732574T3 (es) * | 2012-11-30 | 2019-11-25 | Novartis Ag | Métodos para preparar conjugados a partir de proteínas que contienen disulfuro |
| HK1218252A1 (zh) | 2013-07-25 | 2017-02-10 | Novartis Ag | 合成apelin多肽之生物结合物 |
| KR20160031551A (ko) | 2013-07-25 | 2016-03-22 | 노파르티스 아게 | 심부전의 치료를 위한 시클릭 폴리펩티드 |
| CN105612174A (zh) | 2013-07-25 | 2016-05-25 | 诺华股份有限公司 | 用于治疗心力衰竭的二硫化物环状多肽 |
| WO2015013165A1 (en) | 2013-07-25 | 2015-01-29 | Novartis Ag | Cyclic apelin derivatives for the treatment of heart failure |
-
2014
- 2014-07-21 CN CN201480052701.8A patent/CN105612174A/zh active Pending
- 2014-07-21 JP JP2016529806A patent/JP6505692B2/ja not_active Expired - Fee Related
- 2014-07-21 EP EP14750842.8A patent/EP3024847A1/en not_active Withdrawn
- 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
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