JP2016532681A5 - - Google Patents
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- JP2016532681A5 JP2016532681A5 JP2016529807A JP2016529807A JP2016532681A5 JP 2016532681 A5 JP2016532681 A5 JP 2016532681A5 JP 2016529807 A JP2016529807 A JP 2016529807A JP 2016529807 A JP2016529807 A JP 2016529807A JP 2016532681 A5 JP2016532681 A5 JP 2016532681A5
- Authority
- JP
- Japan
- Prior art keywords
- polypeptide
- amide
- salt
- absent
- 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
Links
- 108090000765 processed proteins & peptides Proteins 0.000 claims description 102
- 229920001184 polypeptide Polymers 0.000 claims description 96
- 102000004196 processed proteins & peptides Human genes 0.000 claims description 96
- 150000001408 amides Chemical class 0.000 claims description 46
- 150000003839 salts Chemical class 0.000 claims description 46
- 150000002148 esters Chemical class 0.000 claims description 40
- 229910052731 fluorine Inorganic materials 0.000 claims description 25
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims description 14
- SNDPXSYFESPGGJ-SCSAIBSYSA-N D-2-aminopentanoic acid Chemical compound CCC[C@@H](N)C(O)=O SNDPXSYFESPGGJ-SCSAIBSYSA-N 0.000 claims description 12
- 210000004899 c-terminal region Anatomy 0.000 claims description 9
- 150000001413 amino acids Chemical class 0.000 claims description 8
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 8
- 125000000250 methylamino group Chemical group [H]N(*)C([H])([H])[H] 0.000 claims description 8
- 206010007556 Cardiac failure acute Diseases 0.000 claims description 6
- 102000008100 Human Serum Albumin Human genes 0.000 claims description 5
- 108091006905 Human Serum Albumin Proteins 0.000 claims description 5
- 239000003795 chemical substances by application Substances 0.000 claims description 5
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 claims description 4
- 101800000407 Brain natriuretic peptide 32 Proteins 0.000 claims description 4
- 229940127291 Calcium channel antagonist Drugs 0.000 claims description 4
- 239000000480 calcium channel blocker Substances 0.000 claims description 4
- 201000010099 disease Diseases 0.000 claims description 4
- 208000035475 disorder Diseases 0.000 claims description 4
- 125000002228 disulfide group Chemical group 0.000 claims description 4
- 239000003814 drug Substances 0.000 claims description 4
- 239000002308 endothelin receptor antagonist Substances 0.000 claims description 4
- 239000003087 receptor blocking agent Substances 0.000 claims description 4
- 108091008803 APLNR Proteins 0.000 claims description 3
- 201000001320 Atherosclerosis Diseases 0.000 claims description 3
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 3
- 206010059027 Brugada syndrome Diseases 0.000 claims description 3
- 206010007558 Cardiac failure chronic Diseases 0.000 claims description 3
- 208000031229 Cardiomyopathies Diseases 0.000 claims description 3
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 3
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims description 3
- 206010016807 Fluid retention Diseases 0.000 claims description 3
- 206010020772 Hypertension Diseases 0.000 claims description 3
- 208000008589 Obesity Diseases 0.000 claims description 3
- 208000005764 Peripheral Arterial Disease Diseases 0.000 claims description 3
- 208000030831 Peripheral arterial occlusive disease Diseases 0.000 claims description 3
- 206010042496 Sunburn Diseases 0.000 claims description 3
- 208000032109 Transient ischaemic attack Diseases 0.000 claims description 3
- 208000030886 Traumatic Brain injury Diseases 0.000 claims description 3
- 230000008484 agonism Effects 0.000 claims description 3
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 3
- 206010003119 arrhythmia Diseases 0.000 claims description 3
- 230000006793 arrhythmia Effects 0.000 claims description 3
- 206010012601 diabetes mellitus Diseases 0.000 claims description 3
- 208000004104 gestational diabetes Diseases 0.000 claims description 3
- 230000000302 ischemic effect Effects 0.000 claims description 3
- 235000020824 obesity Nutrition 0.000 claims description 3
- 201000011461 pre-eclampsia Diseases 0.000 claims description 3
- 208000002815 pulmonary hypertension Diseases 0.000 claims description 3
- 208000037803 restenosis Diseases 0.000 claims description 3
- 201000010875 transient cerebral ischemia Diseases 0.000 claims description 3
- 230000009529 traumatic brain injury Effects 0.000 claims description 3
- 206010047302 ventricular tachycardia Diseases 0.000 claims description 3
- ODHCTXKNWHHXJC-VKHMYHEASA-N 5-oxo-L-proline Chemical group OC(=O)[C@@H]1CCC(=O)N1 ODHCTXKNWHHXJC-VKHMYHEASA-N 0.000 claims description 2
- 102000005666 Apolipoprotein A-I Human genes 0.000 claims description 2
- 108010059886 Apolipoprotein A-I Proteins 0.000 claims description 2
- FFFHZYDWPBMWHY-GSVOUGTGSA-N D-Homocysteine Chemical compound OC(=O)[C@H](N)CCS FFFHZYDWPBMWHY-GSVOUGTGSA-N 0.000 claims description 2
- QWCKQJZIFLGMSD-GSVOUGTGSA-N D-alpha-aminobutyric acid Chemical group CC[C@@H](N)C(O)=O QWCKQJZIFLGMSD-GSVOUGTGSA-N 0.000 claims description 2
- LRQKBLKVPFOOQJ-RXMQYKEDSA-N D-norleucine Chemical group CCCC[C@@H](N)C(O)=O LRQKBLKVPFOOQJ-RXMQYKEDSA-N 0.000 claims description 2
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 claims description 2
- FFFHZYDWPBMWHY-UHFFFAOYSA-N L-Homocysteine Natural products OC(=O)C(N)CCS FFFHZYDWPBMWHY-UHFFFAOYSA-N 0.000 claims description 2
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical compound OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 claims description 2
- 102000003979 Mineralocorticoid Receptors Human genes 0.000 claims description 2
- 108090000375 Mineralocorticoid Receptors Proteins 0.000 claims description 2
- 102000003743 Relaxin Human genes 0.000 claims description 2
- 108090000103 Relaxin Proteins 0.000 claims description 2
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 2
- ODHCTXKNWHHXJC-UHFFFAOYSA-N acide pyroglutamique Natural products OC(=O)C1CCC(=O)N1 ODHCTXKNWHHXJC-UHFFFAOYSA-N 0.000 claims description 2
- 239000002333 angiotensin II receptor antagonist Substances 0.000 claims description 2
- 229940126317 angiotensin II receptor antagonist Drugs 0.000 claims description 2
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 2
- 230000003178 anti-diabetic effect Effects 0.000 claims description 2
- 230000003579 anti-obesity Effects 0.000 claims description 2
- 239000003146 anticoagulant agent Substances 0.000 claims description 2
- 229940127219 anticoagulant drug Drugs 0.000 claims description 2
- 239000003472 antidiabetic agent Substances 0.000 claims description 2
- 102000012740 beta Adrenergic Receptors Human genes 0.000 claims description 2
- 108010079452 beta Adrenergic Receptors Proteins 0.000 claims description 2
- 239000003354 cholesterol ester transfer protein inhibitor Substances 0.000 claims description 2
- 229940125881 cholesteryl ester transfer protein inhibitor Drugs 0.000 claims description 2
- 125000004122 cyclic group Chemical group 0.000 claims description 2
- 239000002934 diuretic Substances 0.000 claims description 2
- 230000001882 diuretic effect Effects 0.000 claims description 2
- 229940079593 drug Drugs 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 239000012634 fragment Substances 0.000 claims description 2
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 claims description 2
- 239000003112 inhibitor Substances 0.000 claims description 2
- 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 description 2
- 229960001267 nesiritide Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 230000002265 prevention Effects 0.000 claims description 2
- 239000002461 renin inhibitor Substances 0.000 claims description 2
- 229940086526 renin-inhibitors Drugs 0.000 claims description 2
- 229910052717 sulfur Inorganic materials 0.000 claims description 2
- 239000011593 sulfur Substances 0.000 claims description 2
- 125000005647 linker group Chemical group 0.000 description 7
- 125000002947 alkylene group Chemical group 0.000 description 6
- 235000001014 amino acid Nutrition 0.000 description 5
- 125000000753 cycloalkyl group Chemical group 0.000 description 4
- 238000000034 method Methods 0.000 description 3
- 235000004279 alanine Nutrition 0.000 description 2
- 125000003118 aryl group Chemical group 0.000 description 2
- 235000014113 dietary fatty acids Nutrition 0.000 description 2
- 229930195729 fatty acid Natural products 0.000 description 2
- 239000000194 fatty acid Substances 0.000 description 2
- 150000004665 fatty acids Chemical class 0.000 description 2
- 125000004080 3-carboxypropanoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C(O[H])=O 0.000 description 1
- -1 4-phenylbutanoyl Chemical group 0.000 description 1
- 102000018071 Immunoglobulin Fc Fragments Human genes 0.000 description 1
- 108010091135 Immunoglobulin Fc Fragments Proteins 0.000 description 1
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical compound C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 description 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 description 1
- 239000004472 Lysine Substances 0.000 description 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 description 1
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 description 1
- 125000003295 alanine group Chemical group N[C@@H](C)C(=O)* 0.000 description 1
- 125000000217 alkyl group Chemical group 0.000 description 1
- 125000003236 benzoyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C(*)=O 0.000 description 1
- 125000002619 bicyclic group Chemical group 0.000 description 1
- 230000009787 cardiac fibrosis Effects 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 125000001153 fluoro group Chemical group F* 0.000 description 1
- HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 1
- 125000003588 lysine group Chemical group [H]N([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])(N([H])[H])C(*)=O 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 230000035772 mutation Effects 0.000 description 1
- 125000002801 octanoyl group Chemical group C(CCCCCCC)(=O)* 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201361858263P | 2013-07-25 | 2013-07-25 | |
| US61/858,263 | 2013-07-25 | ||
| US201462015854P | 2014-06-23 | 2014-06-23 | |
| US62/015,854 | 2014-06-23 | ||
| PCT/US2014/047377 WO2015013168A1 (en) | 2013-07-25 | 2014-07-21 | Cyclic polypeptides for the treatment of heart failure |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2016532681A JP2016532681A (ja) | 2016-10-20 |
| JP2016532681A5 true JP2016532681A5 (https=) | 2017-08-31 |
| JP6501775B2 JP6501775B2 (ja) | 2019-04-17 |
Family
ID=51263584
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016529807A Expired - Fee Related JP6501775B2 (ja) | 2013-07-25 | 2014-07-21 | 心不全治療用の環状ポリペプチド |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US9266925B2 (https=) |
| EP (1) | EP3024845A1 (https=) |
| JP (1) | JP6501775B2 (https=) |
| KR (1) | KR20160031551A (https=) |
| CN (1) | CN105612172A (https=) |
| AP (1) | AP2016009021A0 (https=) |
| AU (1) | AU2014293386B2 (https=) |
| BR (1) | BR112016001542A2 (https=) |
| CA (1) | CA2918074A1 (https=) |
| CL (1) | CL2016000190A1 (https=) |
| CR (1) | CR20160048A (https=) |
| CU (1) | CU20160013A7 (https=) |
| EA (1) | EA201690278A1 (https=) |
| HK (1) | HK1218298A1 (https=) |
| IL (1) | IL243682A0 (https=) |
| MX (1) | MX2016001020A (https=) |
| PE (1) | PE20160878A1 (https=) |
| PH (1) | PH12016500104A1 (https=) |
| SG (1) | SG11201600211XA (https=) |
| SV (1) | SV2016005145A (https=) |
| TN (1) | TN2016000031A1 (https=) |
| TW (1) | TW201536814A (https=) |
| UY (1) | UY35670A (https=) |
| WO (1) | WO2015013168A1 (https=) |
Families Citing this family (16)
| 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 |
| 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 |
| US10588980B2 (en) | 2014-06-23 | 2020-03-17 | Novartis Ag | Fatty acids and their use in conjugation to biomolecules |
| SG11201609706VA (en) | 2014-06-23 | 2017-01-27 | Novartis Ag | Site specific protein modifications |
| MA41580A (fr) | 2015-01-23 | 2017-11-29 | Novartis Ag | Conjugués d'acides gras de l'apeline synthétique présentant une demi-vie améliorée |
| WO2016162127A1 (en) * | 2015-04-08 | 2016-10-13 | Polyphor Ag | Backbone-cyclized peptidomimetics |
| 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 |
| US10738338B2 (en) | 2016-10-18 | 2020-08-11 | The Research Foundation for the State University | Method and composition for biocatalytic protein-oligonucleotide conjugation and protein-oligonucleotide conjugate |
| JOP20190245A1 (ar) | 2017-04-20 | 2019-10-15 | Novartis Ag | أنظمة توصيل إطلاق مستدام تتضمن روابط بلا أثر لنقطة الربط |
| CN213866028U (zh) * | 2020-08-19 | 2021-08-03 | 江苏金斯瑞生物科技有限公司 | 一种多肽合成装置 |
| IL313485A (en) * | 2021-12-16 | 2024-08-01 | Socpra Sciences Sant? Et Humaines S E C | Apelinergic macrocycles and uses thereof |
| CN118252913B (zh) * | 2024-02-07 | 2024-09-17 | 中国医学科学院阜外医院 | 多肽偶联物及其在射血分数保留的心衰中的应用 |
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-
2014
- 2014-07-21 KR KR1020167004512A patent/KR20160031551A/ko not_active Withdrawn
- 2014-07-21 BR BR112016001542A patent/BR112016001542A2/pt not_active Application Discontinuation
- 2014-07-21 CN CN201480052591.5A patent/CN105612172A/zh active Pending
- 2014-07-21 CA CA2918074A patent/CA2918074A1/en not_active Withdrawn
- 2014-07-21 AP AP2016009021A patent/AP2016009021A0/en unknown
- 2014-07-21 AU AU2014293386A patent/AU2014293386B2/en not_active Revoked
- 2014-07-21 WO PCT/US2014/047377 patent/WO2015013168A1/en not_active Ceased
- 2014-07-21 PE PE2016000106A patent/PE20160878A1/es not_active Application Discontinuation
- 2014-07-21 EA EA201690278A patent/EA201690278A1/ru unknown
- 2014-07-21 UY UY35670A patent/UY35670A/es not_active Application Discontinuation
- 2014-07-21 TN TN2016000031A patent/TN2016000031A1/en unknown
- 2014-07-21 EP EP14747284.9A patent/EP3024845A1/en not_active Withdrawn
- 2014-07-21 HK HK16106224.7A patent/HK1218298A1/zh unknown
- 2014-07-21 MX MX2016001020A patent/MX2016001020A/es unknown
- 2014-07-21 US US14/336,262 patent/US9266925B2/en not_active Expired - Fee Related
- 2014-07-21 TW TW103124998A patent/TW201536814A/zh unknown
- 2014-07-21 SG SG11201600211XA patent/SG11201600211XA/en unknown
- 2014-07-21 JP JP2016529807A patent/JP6501775B2/ja not_active Expired - Fee Related
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2015
- 2015-12-09 US US14/963,391 patent/US9683019B2/en not_active Expired - Fee Related
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2016
- 2016-01-15 PH PH12016500104A patent/PH12016500104A1/en unknown
- 2016-01-19 IL IL243682A patent/IL243682A0/en unknown
- 2016-01-25 CL CL2016000190A patent/CL2016000190A1/es unknown
- 2016-01-25 CU CUP2016000013A patent/CU20160013A7/es unknown
- 2016-01-25 SV SV2016005145A patent/SV2016005145A/es unknown
- 2016-01-25 CR CR20160048A patent/CR20160048A/es unknown
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2017
- 2017-04-25 US US15/497,135 patent/US20170233443A1/en not_active Abandoned
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