JP2018048157A5 - - Google Patents
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- JP2018048157A5 JP2018048157A5 JP2017195815A JP2017195815A JP2018048157A5 JP 2018048157 A5 JP2018048157 A5 JP 2018048157A5 JP 2017195815 A JP2017195815 A JP 2017195815A JP 2017195815 A JP2017195815 A JP 2017195815A JP 2018048157 A5 JP2018048157 A5 JP 2018048157A5
- Authority
- JP
- Japan
- Prior art keywords
- seq
- nle
- polypeptide
- amide
- ester
- 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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- 150000001413 amino acids Chemical class 0.000 claims 6
- 229920001184 polypeptide Polymers 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 102000004196 processed proteins & peptides Human genes 0.000 claims 6
- 150000001408 amides Chemical class 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 150000002148 esters Chemical class 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 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
- 239000000480 calcium channel blocker Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000035475 disorder Diseases 0.000 claims 2
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 2
- 239000003087 receptor blocking agent Substances 0.000 claims 2
- 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
- 108010009911 Cytochrome P-450 CYP11B2 Proteins 0.000 claims 1
- 102100024329 Cytochrome P450 11B2, mitochondrial Human genes 0.000 claims 1
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims 1
- 206010016654 Fibrosis Diseases 0.000 claims 1
- 206010016807 Fluid retention Diseases 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- HXEACLLIILLPRG-YFKPBYRVSA-N L-pipecolic acid Chemical compound [O-]C(=O)[C@@H]1CCCC[NH2+]1 HXEACLLIILLPRG-YFKPBYRVSA-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
- 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
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004761 fibrosis Effects 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
- HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 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
- 229940117803 phenethylamine Drugs 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
- 230000001225 therapeutic effect Effects 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 (6)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261591557P | 2012-01-27 | 2012-01-27 | |
| US61/591,557 | 2012-01-27 | ||
| US201261717760P | 2012-10-24 | 2012-10-24 | |
| US61/717,760 | 2012-10-24 | ||
| US201261731697P | 2012-11-30 | 2012-11-30 | |
| US61/731,697 | 2012-11-30 |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014553847A Division JP6313222B2 (ja) | 2012-01-27 | 2013-01-25 | 心不全治療用の合成アペリン模倣物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2018048157A JP2018048157A (ja) | 2018-03-29 |
| JP2018048157A5 true JP2018048157A5 (https=) | 2018-05-31 |
| JP6595553B2 JP6595553B2 (ja) | 2019-10-23 |
Family
ID=47997598
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014553847A Expired - Fee Related JP6313222B2 (ja) | 2012-01-27 | 2013-01-25 | 心不全治療用の合成アペリン模倣物 |
| JP2017195815A Expired - Fee Related JP6595553B2 (ja) | 2012-01-27 | 2017-10-06 | 心不全治療用の合成アペリン模倣物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014553847A Expired - Fee Related JP6313222B2 (ja) | 2012-01-27 | 2013-01-25 | 心不全治療用の合成アペリン模倣物 |
Country Status (42)
Families Citing this family (42)
| 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 |
| 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 |
| US20160067347A1 (en) * | 2012-12-20 | 2016-03-10 | Amgen Inc. | Apj receptor agonists and uses thereof |
| US9353163B2 (en) | 2013-03-14 | 2016-05-31 | Regeneron Pharmaceuticals, Inc. | Apelin fusion proteins and uses thereof |
| HK1218252A1 (zh) | 2013-07-25 | 2017-02-10 | Novartis Ag | 合成apelin多肽之生物结合物 |
| 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 |
| KR20160031551A (ko) | 2013-07-25 | 2016-03-22 | 노파르티스 아게 | 심부전의 치료를 위한 시클릭 폴리펩티드 |
| UA119247C2 (uk) | 2013-09-06 | 2019-05-27 | РОЙВЕНТ САЙЕНСИЗ ҐмбГ | Спіроциклічні сполуки як інгібітори триптофангідроксилази |
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| EA201691075A1 (ru) | 2013-11-26 | 2016-09-30 | Новартис Аг | Способы оксимной конъюгации с кетон-модифицированными полипептидами |
| WO2015089137A1 (en) | 2013-12-11 | 2015-06-18 | Karos Pharmaceuticals, Inc. | Acylguanidines as tryptophan hydroxylase inhibitors |
| DK3122764T3 (en) * | 2014-03-25 | 2019-04-15 | Lanthiopep Bv | CYCLIC APELINE ANALOGS |
| GB201407532D0 (en) | 2014-04-29 | 2014-06-11 | Univ Ulster | Apelin analogues |
| ES2792598T3 (es) * | 2014-05-23 | 2020-11-11 | Novartis Ag | Métodos para preparar conjugados a partir de proteínas que contienen disulfuro |
| 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 |
| WO2016109501A1 (en) | 2014-12-30 | 2016-07-07 | Karos Pharmaceuticals, Inc. | Amide compounds as tryptophan hydroxylase inhibitors |
| MA41580A (fr) * | 2015-01-23 | 2017-11-29 | Novartis Ag | Conjugués d'acides gras de l'apeline synthétique présentant une demi-vie améliorée |
| US9611201B2 (en) | 2015-03-05 | 2017-04-04 | Karos Pharmaceuticals, Inc. | Processes for preparing (R)-1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanol and 1-(5-chloro-[1,1′-biphenyl]-2-yl)-2,2,2-trifluoroethanone |
| US10426818B2 (en) * | 2015-03-24 | 2019-10-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Method and pharmaceutical composition for use in the treatment of diabetes |
| HUE050317T2 (hu) | 2015-05-20 | 2020-11-30 | Amgen Inc | APJ receptor triazol agonistái |
| 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 |
| US9988369B2 (en) | 2016-05-03 | 2018-06-05 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the APJ receptor |
| CN110072531A (zh) | 2016-10-19 | 2019-07-30 | 阿维夫公司 | 用于治疗心血管相关疾病的爱帕琳的新型聚乙二醇化的脂质体制剂 |
| WO2018093579A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Triazole phenyl compounds as agonists of the apj receptor |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| WO2018093576A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the apj receptor |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| WO2018093577A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the apj receptor |
| US10736883B2 (en) | 2016-11-16 | 2020-08-11 | Amgen Inc. | Triazole furan compounds as agonists of the APJ receptor |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| EP3681900A4 (en) | 2017-09-11 | 2021-09-08 | Protagonist Therapeutics, Inc. | OPIOID AGONIST PEPTIDES AND THEIR USES |
| MA50509A (fr) | 2017-11-03 | 2021-06-02 | Amgen Inc | Agonistes de triazole fusionnés du récepteur apj |
| US11807624B2 (en) | 2018-05-01 | 2023-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the APJ receptor |
| US12269847B2 (en) | 2018-08-16 | 2025-04-08 | Donaldson Company, Inc. | Genetically encoded polypeptide for affinity capture and purification of biologics |
| CA3119912A1 (en) | 2018-11-14 | 2020-05-22 | Altavant Sciences Gmbh | A crystalline spirocyclic compound inhibitor of tryptophan hydroxylase 1 (tph1) for treating diseases or disorders associated with peripheral serotonin |
| 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 |
| 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 |
| WO2026007692A1 (zh) * | 2024-07-05 | 2026-01-08 | 浙江大学 | Apelin-13多肽突变体 |
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| KR20160031551A (ko) | 2013-07-25 | 2016-03-22 | 노파르티스 아게 | 심부전의 치료를 위한 시클릭 폴리펩티드 |
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-
2013
- 2013-01-23 US US13/747,621 patent/US8673848B2/en not_active Expired - Fee Related
- 2013-01-24 JO JOP/2013/0027A patent/JO3380B1/ar active
- 2013-01-24 UY UY0001034593A patent/UY34593A/es not_active Application Discontinuation
- 2013-01-25 AP AP2014007846A patent/AP2014007846A0/xx unknown
- 2013-01-25 EA EA201491433A patent/EA027853B1/ru not_active IP Right Cessation
- 2013-01-25 EP EP13711953.3A patent/EP2807183B1/en active Active
- 2013-01-25 AU AU2013213265A patent/AU2013213265C1/en not_active Ceased
- 2013-01-25 CA CA2862240A patent/CA2862240A1/en active Pending
- 2013-01-25 CN CN201380016261.6A patent/CN104220452B/zh not_active Expired - Fee Related
- 2013-01-25 MX MX2014009085A patent/MX351569B/es active IP Right Grant
- 2013-01-25 LT LTEP13711953.3T patent/LT2807183T/lt unknown
- 2013-01-25 SG SG11201404369PA patent/SG11201404369PA/en unknown
- 2013-01-25 WO PCT/IB2013/050666 patent/WO2013111110A2/en not_active Ceased
- 2013-01-25 PL PL13711953T patent/PL2807183T3/pl unknown
- 2013-01-25 KR KR1020147023505A patent/KR102068370B1/ko not_active Expired - Fee Related
- 2013-01-25 BR BR112014018306A patent/BR112014018306A8/pt not_active IP Right Cessation
- 2013-01-25 ES ES13711953.3T patent/ES2670832T3/es active Active
- 2013-01-25 DK DK13711953.3T patent/DK2807183T3/en active
- 2013-01-25 TW TW102103025A patent/TWI576356B/zh not_active IP Right Cessation
- 2013-01-25 JP JP2014553847A patent/JP6313222B2/ja not_active Expired - Fee Related
- 2013-01-25 NZ NZ627772A patent/NZ627772A/en not_active IP Right Cessation
- 2013-01-25 HR HRP20180806TT patent/HRP20180806T1/hr unknown
- 2013-01-25 SI SI201330999T patent/SI2807183T1/en unknown
- 2013-01-25 RS RS20180546A patent/RS57200B1/sr unknown
- 2013-01-25 HU HUE13711953A patent/HUE039137T2/hu unknown
- 2013-01-25 KR KR1020197037887A patent/KR20200003229A/ko not_active Ceased
- 2013-01-25 UA UAA201408328A patent/UA116196C2/uk unknown
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2014
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2015
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