JP2015506370A5 - - Google Patents
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- JP2015506370A5 JP2015506370A5 JP2014553847A JP2014553847A JP2015506370A5 JP 2015506370 A5 JP2015506370 A5 JP 2015506370A5 JP 2014553847 A JP2014553847 A JP 2014553847A JP 2014553847 A JP2014553847 A JP 2014553847A JP 2015506370 A5 JP2015506370 A5 JP 2015506370A5
- Authority
- JP
- Japan
- Prior art keywords
- seq
- nle
- polypeptide
- amide
- 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
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- 229920001184 polypeptide Polymers 0.000 claims 61
- 108090000765 processed proteins & peptides Proteins 0.000 claims 61
- 102000004196 processed proteins & peptides Human genes 0.000 claims 61
- 150000003839 salts Chemical class 0.000 claims 32
- 150000001408 amides Chemical class 0.000 claims 31
- 150000002148 esters Chemical class 0.000 claims 25
- 235000001014 amino acid Nutrition 0.000 claims 12
- 229940024606 amino acid Drugs 0.000 claims 12
- 150000001413 amino acids Chemical class 0.000 claims 9
- 235000018417 cysteine Nutrition 0.000 claims 9
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 9
- 229940117803 phenethylamine Drugs 0.000 claims 8
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 6
- 125000000400 lauroyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 6
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 5
- -1 glycine amino acids Chemical class 0.000 claims 5
- 125000001419 myristoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 5
- 206010007556 Cardiac failure acute Diseases 0.000 claims 4
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Natural products NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims 4
- 239000004471 Glycine Substances 0.000 claims 3
- HXEACLLIILLPRG-YFKPBYRVSA-N L-pipecolic acid Chemical compound [O-]C(=O)[C@@H]1CCCC[NH2+]1 HXEACLLIILLPRG-YFKPBYRVSA-N 0.000 claims 3
- 201000010099 disease Diseases 0.000 claims 3
- 208000035475 disorder Diseases 0.000 claims 3
- HXEACLLIILLPRG-RXMQYKEDSA-N l-pipecolic acid Natural products OC(=O)[C@H]1CCCCN1 HXEACLLIILLPRG-RXMQYKEDSA-N 0.000 claims 3
- 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 2
- JJMDCOVWQOJGCB-UHFFFAOYSA-N 5-aminopentanoic acid Chemical compound [NH3+]CCCCC([O-])=O JJMDCOVWQOJGCB-UHFFFAOYSA-N 0.000 claims 2
- 108091008803 APLNR Proteins 0.000 claims 2
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims 2
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 206010003658 Atrial Fibrillation Diseases 0.000 claims 2
- 101800000407 Brain natriuretic peptide 32 Proteins 0.000 claims 2
- 206010059027 Brugada syndrome Diseases 0.000 claims 2
- 229940127291 Calcium channel antagonist Drugs 0.000 claims 2
- 206010007558 Cardiac failure chronic Diseases 0.000 claims 2
- 208000031229 Cardiomyopathies Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 206010016807 Fluid retention Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 102000004270 Peptidyl-Dipeptidase A Human genes 0.000 claims 2
- 108090000882 Peptidyl-Dipeptidase A Proteins 0.000 claims 2
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims 2
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims 2
- 206010042496 Sunburn Diseases 0.000 claims 2
- 208000032109 Transient ischaemic attack Diseases 0.000 claims 2
- 208000030886 Traumatic Brain injury Diseases 0.000 claims 2
- 230000008484 agonism Effects 0.000 claims 2
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 2
- 206010003119 arrhythmia Diseases 0.000 claims 2
- 230000006793 arrhythmia Effects 0.000 claims 2
- 239000000480 calcium channel blocker Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 208000004104 gestational diabetes Diseases 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 230000000302 ischemic effect Effects 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 201000011461 pre-eclampsia Diseases 0.000 claims 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 208000037803 restenosis Diseases 0.000 claims 2
- 201000010875 transient cerebral ischemia Diseases 0.000 claims 2
- 230000009529 traumatic brain injury Effects 0.000 claims 2
- 206010047302 ventricular tachycardia Diseases 0.000 claims 2
- DFZVZEMNPGABKO-ZETCQYMHSA-N (2s)-2-amino-3-pyridin-3-ylpropanoic acid Chemical compound OC(=O)[C@@H](N)CC1=CC=CN=C1 DFZVZEMNPGABKO-ZETCQYMHSA-N 0.000 claims 1
- 125000001431 2-aminoisobutyric acid group Chemical group [#6]C([#6])(N*)C(*)=O 0.000 claims 1
- PECYZEOJVXMISF-REOHCLBHSA-N 3-amino-L-alanine Chemical compound [NH3+]C[C@H](N)C([O-])=O PECYZEOJVXMISF-REOHCLBHSA-N 0.000 claims 1
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 claims 1
- ZUQOBHTUMCEQBG-UHFFFAOYSA-N 4-amino-5-hydroxynaphthalene-1,7-disulfonic acid Chemical compound OS(=O)(=O)C1=CC(O)=C2C(N)=CC=C(S(O)(=O)=O)C2=C1 ZUQOBHTUMCEQBG-UHFFFAOYSA-N 0.000 claims 1
- KHABBYNLBYZCKP-UHFFFAOYSA-N 4-aminopiperidin-1-ium-4-carboxylate Chemical compound OC(=O)C1(N)CCNCC1 KHABBYNLBYZCKP-UHFFFAOYSA-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
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims 1
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims 1
- 101800002247 Brain natriuretic peptide 45 Proteins 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
- 102000002045 Endothelin Human genes 0.000 claims 1
- 108050009340 Endothelin Proteins 0.000 claims 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims 1
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 1
- FFFHZYDWPBMWHY-UHFFFAOYSA-N L-Homocysteine Natural products OC(=O)C(N)CCS FFFHZYDWPBMWHY-UHFFFAOYSA-N 0.000 claims 1
- AHLPHDHHMVZTML-BYPYZUCNSA-N L-Ornithine Chemical compound NCCC[C@H](N)C(O)=O AHLPHDHHMVZTML-BYPYZUCNSA-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
- JTTHKOPSMAVJFE-VIFPVBQESA-N L-homophenylalanine Chemical compound OC(=O)[C@@H](N)CCC1=CC=CC=C1 JTTHKOPSMAVJFE-VIFPVBQESA-N 0.000 claims 1
- UCUNFLYVYCGDHP-BYPYZUCNSA-N L-methionine sulfone Chemical compound CS(=O)(=O)CC[C@H](N)C(O)=O UCUNFLYVYCGDHP-BYPYZUCNSA-N 0.000 claims 1
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims 1
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims 1
- 102000007399 Nuclear hormone receptor Human genes 0.000 claims 1
- AHLPHDHHMVZTML-UHFFFAOYSA-N Orn-delta-NH2 Natural products NCCCC(N)C(O)=O AHLPHDHHMVZTML-UHFFFAOYSA-N 0.000 claims 1
- UTJLXEIPEHZYQJ-UHFFFAOYSA-N Ornithine Natural products OC(=O)C(C)CCCN UTJLXEIPEHZYQJ-UHFFFAOYSA-N 0.000 claims 1
- 102000003743 Relaxin Human genes 0.000 claims 1
- 108090000103 Relaxin Proteins 0.000 claims 1
- XAKBSHICSHRJCL-UHFFFAOYSA-N [CH2]C(=O)C1=CC=CC=C1 Chemical group [CH2]C(=O)C1=CC=CC=C1 XAKBSHICSHRJCL-UHFFFAOYSA-N 0.000 claims 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 1
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 claims 1
- FUOOLUPWFVMBKG-UHFFFAOYSA-N alpha-amino-isobutyric acid Natural products CC(C)(N)C(O)=O FUOOLUPWFVMBKG-UHFFFAOYSA-N 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims 1
- 239000005557 antagonist Substances 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
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 claims 1
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims 1
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims 1
- JCZLABDVDPYLRZ-AWEZNQCLSA-N biphenylalanine Chemical compound C1=CC(C[C@H](N)C(O)=O)=CC=C1C1=CC=CC=C1 JCZLABDVDPYLRZ-AWEZNQCLSA-N 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 230000009787 cardiac fibrosis Effects 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
- 235000014113 dietary fatty acids Nutrition 0.000 claims 1
- 239000002934 diuretic Substances 0.000 claims 1
- 230000001882 diuretic effect Effects 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000002308 endothelin receptor antagonist Substances 0.000 claims 1
- 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 1
- 229930195729 fatty acid Natural products 0.000 claims 1
- 239000000194 fatty acid Substances 0.000 claims 1
- 150000004665 fatty acids Chemical class 0.000 claims 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims 1
- 239000000203 mixture Substances 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
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 claims 1
- 229960003104 ornithine Drugs 0.000 claims 1
- 229940096701 plain lipid modifying drug hmg coa reductase inhibitors Drugs 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000003087 receptor blocking agent Substances 0.000 claims 1
- 239000002461 renin inhibitor Substances 0.000 claims 1
- 229940086526 renin-inhibitors Drugs 0.000 claims 1
- WPLOVIFNBMNBPD-ATHMIXSHSA-N subtilin Chemical group CC1SCC(NC2=O)C(=O)NC(CC(N)=O)C(=O)NC(C(=O)NC(CCCCN)C(=O)NC(C(C)CC)C(=O)NC(=C)C(=O)NC(CCCCN)C(O)=O)CSC(C)C2NC(=O)C(CC(C)C)NC(=O)C1NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(NC(=O)C1NC(=O)C(=C/C)/NC(=O)C(CCC(N)=O)NC(=O)C(CC(C)C)NC(=O)C(C)NC(=O)CNC(=O)C(NC(=O)C(NC(=O)C2NC(=O)CNC(=O)C3CCCN3C(=O)C(NC(=O)C3NC(=O)C(CC(C)C)NC(=O)C(=C)NC(=O)C(CCC(O)=O)NC(=O)C(NC(=O)C(CCCCN)NC(=O)C(N)CC=4C5=CC=CC=C5NC=4)CSC3)C(C)SC2)C(C)C)C(C)SC1)CC1=CC=CC=C1 WPLOVIFNBMNBPD-ATHMIXSHSA-N 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- ORQXBVXKBGUSBA-QMMMGPOBSA-N β-cyclohexyl-alanine Chemical compound OC(=O)[C@@H](N)CC1CCCCC1 ORQXBVXKBGUSBA-QMMMGPOBSA-N 0.000 claims 1
Applications Claiming Priority (7)
| 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 | ||
| PCT/IB2013/050666 WO2013111110A2 (en) | 2012-01-27 | 2013-01-25 | Synthetic apelin mimetics for the treatment of heart failure |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2017195815A Division JP6595553B2 (ja) | 2012-01-27 | 2017-10-06 | 心不全治療用の合成アペリン模倣物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015506370A JP2015506370A (ja) | 2015-03-02 |
| JP2015506370A5 true JP2015506370A5 (enExample) | 2016-03-17 |
| JP6313222B2 JP6313222B2 (ja) | 2018-04-18 |
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 After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| 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 |
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 |
| UY35144A (es) * | 2012-11-20 | 2014-06-30 | Novartis Ag | Miméticos lineales sintéticos de apelina para el tratamiento de insuficiencia cardiaca |
| US8921307B2 (en) * | 2012-11-20 | 2014-12-30 | Novartis Ag | Synthetic linear apelin mimetics for the treatment of heart failure |
| EP2925368B1 (en) | 2012-11-30 | 2019-03-27 | Novartis AG | Methods for making conjugates from disulfide-containing proteins |
| JP6426107B2 (ja) * | 2012-12-20 | 2018-11-21 | アムジエン・インコーポレーテツド | Ａｐｊ受容体アゴニストおよびその使用 |
| WO2014152955A1 (en) | 2013-03-14 | 2014-09-25 | Regeneron Pharmaceuticals, Inc. | Apelin fusion proteins and uses thereof |
| CN105612173A (zh) * | 2013-07-25 | 2016-05-25 | 诺华股份有限公司 | 用于治疗心力衰竭的环状apelin衍生物 |
| US9266925B2 (en) * | 2013-07-25 | 2016-02-23 | Novartis Ag | Cyclic polypeptides for the treatment of heart failure |
| BR112016001376A2 (pt) | 2013-07-25 | 2017-10-24 | Novartis Ag | bioconjugados de polipeptídeos de apelin sintéticos |
| WO2015013167A1 (en) * | 2013-07-25 | 2015-01-29 | Novartis Ag | Disulfide cyclic polypeptides for the treatment of heart failure |
| UA119247C2 (uk) | 2013-09-06 | 2019-05-27 | РОЙВЕНТ САЙЕНСИЗ ҐмбГ | Спіроциклічні сполуки як інгібітори триптофангідроксилази |
| WO2015077491A1 (en) * | 2013-11-20 | 2015-05-28 | Regeneron Pharmaceuticals, Inc. | Aplnr modulators and uses thereof |
| JP6609563B2 (ja) * | 2013-11-26 | 2019-11-20 | ノバルティス アーゲー | ケトンで修飾されたポリペプチドをオキシム複合化する方法 |
| WO2015089137A1 (en) | 2013-12-11 | 2015-06-18 | Karos Pharmaceuticals, Inc. | Acylguanidines as tryptophan hydroxylase inhibitors |
| WO2015147641A1 (en) * | 2014-03-25 | 2015-10-01 | Lanthiopep B.V. | Cyclic apelin analogs |
| GB201407532D0 (en) * | 2014-04-29 | 2014-06-11 | Univ Ulster | Apelin analogues |
| EP3145552B1 (en) | 2014-05-23 | 2020-03-04 | Novartis AG | Methods for making conjugates from disulfide-containing proteins |
| 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 |
| CA2972871A1 (en) * | 2015-01-23 | 2016-07-28 | Novartis Ag | Synthetic apelin fatty acid conjugates with improved half-life |
| 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 |
| WO2016151018A1 (en) * | 2015-03-24 | 2016-09-29 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Method and pharmaceutical composition for use in the treatment of diabetes |
| AU2016263564B2 (en) | 2015-05-20 | 2019-12-05 | Amgen Inc. | Triazole agonists of the APJ receptor |
| US11484577B2 (en) | 2016-02-15 | 2022-11-01 | Inserm (Institut National De La Sante Et De La Recherche Medicale) | Methods and pharmaceutical compositions for the treatment of post-operative cognitive dysfunction |
| US9988369B2 (en) | 2016-05-03 | 2018-06-05 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the APJ receptor |
| EP3528820B1 (en) | 2016-10-19 | 2023-10-04 | Avive, Inc. | Novel pegylated liposomal formulations of apelin for treatment of cardiovascular-related diseases |
| WO2018093577A1 (en) | 2016-11-16 | 2018-05-24 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the apj receptor |
| US10689367B2 (en) | 2016-11-16 | 2020-06-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the APJ receptor |
| US11191762B2 (en) | 2016-11-16 | 2021-12-07 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the APJ Receptor |
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