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
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- 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 (enExample) | 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 (enExample) |
| EP (1) | EP3024845A1 (enExample) |
| JP (1) | JP6501775B2 (enExample) |
| KR (1) | KR20160031551A (enExample) |
| CN (1) | CN105612172A (enExample) |
| AP (1) | AP2016009021A0 (enExample) |
| AU (1) | AU2014293386B2 (enExample) |
| BR (1) | BR112016001542A2 (enExample) |
| CA (1) | CA2918074A1 (enExample) |
| CL (1) | CL2016000190A1 (enExample) |
| CR (1) | CR20160048A (enExample) |
| CU (1) | CU20160013A7 (enExample) |
| EA (1) | EA201690278A1 (enExample) |
| HK (1) | HK1218298A1 (enExample) |
| IL (1) | IL243682A0 (enExample) |
| MX (1) | MX2016001020A (enExample) |
| PE (1) | PE20160878A1 (enExample) |
| PH (1) | PH12016500104A1 (enExample) |
| SG (1) | SG11201600211XA (enExample) |
| SV (1) | SV2016005145A (enExample) |
| TN (1) | TN2016000031A1 (enExample) |
| TW (1) | TW201536814A (enExample) |
| UY (1) | UY35670A (enExample) |
| WO (1) | WO2015013168A1 (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 |
| AU2016209968B2 (en) * | 2015-01-23 | 2018-11-29 | Novartis Ag | Synthetic apelin fatty acid conjugates with improved half-life |
| US10730911B2 (en) | 2015-04-08 | 2020-08-04 | Universitat Zurich | Backbone-cyclized peptidomimetics with GLP-1R modulating activity |
| WO2017140684A2 (en) | 2016-02-15 | 2017-08-24 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods and pharmaceutical compositions for the treatment of post-operative cognitive dysfunction |
| 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 |
| 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 |
Family Cites Families (119)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE2951135A1 (de) | 1979-12-19 | 1981-06-25 | Hoechst Ag, 6230 Frankfurt | Sulfonylharnstoffe, verfahren zu ihrer herstellung, pharmazeutische praeparate auf basis dieser verbindungen und ihre verwendung |
| US4617307A (en) | 1984-06-20 | 1986-10-14 | Ciba-Geigy Corporation | Substituted imidazo[1,5-A]pyridine derivatives as aromatase inhibitors |
| US4889861A (en) | 1982-12-21 | 1989-12-26 | Ciba-Geigy Corp. | Substituted imidazo[1,5-a]pyridine derivatives and other substituted bicyclic derivatives and their use as aromatase inhibitors |
| DE3347565A1 (de) | 1983-12-30 | 1985-07-11 | Thomae Gmbh Dr K | Neue phenylessigsaeurederivate, diese verbindungen enthaltende arzneimittel und verfahren zu ihrer herstellung |
| JPS6354321A (ja) | 1985-03-27 | 1988-03-08 | Ajinomoto Co Inc | 血糖降下剤 |
| US5120712A (en) | 1986-05-05 | 1992-06-09 | The General Hospital Corporation | Insulinotropic hormone |
| US5118666A (en) | 1986-05-05 | 1992-06-02 | The General Hospital Corporation | Insulinotropic hormone |
| WO1991011457A1 (en) | 1990-01-24 | 1991-08-08 | Buckley Douglas I | Glp-1 analogs useful for diabetes treatment |
| AU654331B2 (en) | 1991-03-30 | 1994-11-03 | Kissei Pharmaceutical Co. Ltd. | Succinic acid compounds |
| US5155100A (en) | 1991-05-01 | 1992-10-13 | Ciba-Geigy Corporation | Phosphono/biaryl substituted dipeptide derivatives |
| RU2086544C1 (ru) | 1991-06-13 | 1997-08-10 | Хоффманн-Ля Рош АГ | Бензолсульфонамидные производные пиримидина или их соли, фармацевтическая композиция для лечения заболеваний, связанных с активностью эндотелина |
| DE59109151D1 (de) | 1991-06-21 | 1999-10-14 | Boehringer Ingelheim Pharma | Verwendung von (s)(+)-2-äthoxy-4-[n-[1-(2-piperidino-phenyl)-3-methyl-1-butyl]aminocarbonylmethyl]-benzoesäure zur herstellung eines langzeitantidiabetikums |
| EP0526171B1 (en) | 1991-07-30 | 1997-03-05 | Ajinomoto Co., Inc. | Crystals of N-(trans-4-isopropylcyclohexylcarbonyl)-D-phenylalanine and methods for preparing them |
| WO1993011782A1 (en) | 1991-12-19 | 1993-06-24 | Southwest Foundation For Biomedical Research | Cetp inhibitor polypeptide, antibodies against the synthetic polypeptide and prophylactic and therapeutic anti-atherosclerosis treatments |
| DE69317883T2 (de) | 1992-11-17 | 1998-11-12 | Icos Corp., Bothell, Wash. | Neue Sieben-Transmembran-Rezeptor V28 |
| IL111785A0 (en) | 1993-12-03 | 1995-01-24 | Ferring Bv | Dp-iv inhibitors and pharmaceutical compositions containing them |
| US5705483A (en) | 1993-12-09 | 1998-01-06 | Eli Lilly And Company | Glucagon-like insulinotropic peptides, compositions and methods |
| US5512549A (en) | 1994-10-18 | 1996-04-30 | Eli Lilly And Company | Glucagon-like insulinotropic peptide analogs, compositions, and methods of use |
| TW313568B (enExample) | 1994-12-20 | 1997-08-21 | Hoffmann La Roche | |
| US6096871A (en) | 1995-04-14 | 2000-08-01 | Genentech, Inc. | Polypeptides altered to contain an epitope from the Fc region of an IgG molecule for increased half-life |
| US6428771B1 (en) | 1995-05-15 | 2002-08-06 | Pharmaceutical Discovery Corporation | Method for drug delivery to the pulmonary system |
| WO1997034631A1 (en) | 1996-03-18 | 1997-09-25 | Board Of Regents, The University Of Texas System | Immunoglobin-like domains with increased half lives |
| DE19616486C5 (de) | 1996-04-25 | 2016-06-30 | Royalty Pharma Collection Trust | Verfahren zur Senkung des Blutglukosespiegels in Säugern |
| US20020052310A1 (en) | 1997-09-15 | 2002-05-02 | Massachusetts Institute Of Technology The Penn State Research Foundation | Particles for inhalation having sustained release properties |
| TW492957B (en) | 1996-11-07 | 2002-07-01 | Novartis Ag | N-substituted 2-cyanopyrrolidnes |
| US6555339B1 (en) | 1997-04-14 | 2003-04-29 | Arena Pharmaceuticals, Inc. | Non-endogenous, constitutively activated human protein-coupled receptors |
| EP1040189B1 (en) | 1997-12-24 | 2008-01-09 | Takeda Pharmaceutical Company Limited | Polypeptides, their production and use |
| US6197786B1 (en) | 1998-09-17 | 2001-03-06 | Pfizer Inc | 4-Carboxyamino-2-substituted-1,2,3,4-tetrahydroquinolines |
| GT199900147A (es) | 1998-09-17 | 1999-09-06 | 1, 2, 3, 4- tetrahidroquinolinas 2-sustituidas 4-amino sustituidas. | |
| AU5759399A (en) | 1998-09-25 | 2000-04-17 | Takeda Chemical Industries Ltd. | Peptide derivative |
| ATE440857T1 (de) | 1998-10-05 | 2009-09-15 | Takeda Pharmaceutical | Verfahren zum eliminieren von n-terminalem methionin |
| US6660843B1 (en) | 1998-10-23 | 2003-12-09 | Amgen Inc. | Modified peptides as therapeutic agents |
| CO5150173A1 (es) | 1998-12-10 | 2002-04-29 | Novartis Ag | Compuestos n-(glicilo sustituido)-2-cianopirrolidinas inhibidores de peptidasa de dipeptidilo-iv (dpp-iv) los cuales son efectivos en el tratamiento de condiciones mediadas por la inhibicion de dpp-iv |
| US7045532B2 (en) | 1999-04-30 | 2006-05-16 | Millennium Pharmaceuticals, Inc. | ACE-2 modulating compounds and methods of use thereof |
| US6521607B1 (en) | 1999-09-23 | 2003-02-18 | Pharmacia Corporation | (R)-chiral halogenated substituted N-phenoxy N-phenyl aminoalcohol compounds useful for inhibiting cholesteryl ester transfer protein activity |
| AU2001242749A1 (en) | 2000-03-23 | 2001-10-03 | Takeda Chemical Industries Ltd. | Peptide derivative |
| AR032316A1 (es) | 2000-04-12 | 2003-11-05 | Novartis Ag | Uso de una composicion farmaceutica para la fabricacion de medicamentos y una composicion farmaceutica |
| AU2001264937A1 (en) | 2000-05-23 | 2001-12-03 | Genaissance Pharmaceuticals, Inc. | Haplotypes of the agtrl1 gene |
| EP1490483B1 (en) | 2001-04-19 | 2015-06-03 | The Scripps Research Institute | In vivo incorporation of unnatural amino acids |
| CA2652991A1 (en) | 2001-07-16 | 2003-11-13 | Caprotec Bioanalytics Gmbh | Capture compounds, collections thereof and methods for analyzing the proteome and complex compositions |
| WO2003063892A1 (en) | 2002-01-29 | 2003-08-07 | Takeda Chemical Industries, Ltd. | Use of apelin |
| AR040441A1 (es) | 2002-06-07 | 2005-04-06 | Glaxo Group Ltd | Compuesto de tiol, composicion farmaceutica que lo comprende, su uso para la fabricacion de un medicamento, procedimiento para prepararlo y compuesto intermediario de utilidad en dicho procedimiento |
| EP1537114B8 (en) | 2002-08-07 | 2007-10-03 | Novartis AG | Organic compounds as agents for the treatment of aldosterone mediated conditions |
| JP2006508970A (ja) | 2002-11-18 | 2006-03-16 | ノバルティス アクチエンゲゼルシャフト | イミダゾ［１，５ａ］ピリジン誘導体およびアルデステロンにより仲介される疾患の処置方法 |
| WO2004081198A2 (en) | 2003-03-12 | 2004-09-23 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Methods for modulating angiogenesis with apelin compositions |
| US7947280B2 (en) | 2003-05-22 | 2011-05-24 | The Board Of Trustees Of The Leland Stanford Junior University | Apelin and uses thereof |
| EP1656560A2 (en) | 2003-05-22 | 2006-05-17 | Agilent Technologies, Inc. | Diagnostic markers and pharmacological targets in heart failure and related reagents and methods of use thereof |
| EP1520861A1 (en) | 2003-09-11 | 2005-04-06 | Aventis Pharma Deutschland GmbH | Test system for the identification of APJ receptor ligands |
| EP1673395A1 (en) | 2003-10-15 | 2006-06-28 | PDL BioPharma, Inc. | Alteration of fc-fusion protein serum half-lives by mutagenesis of positions 250, 314 and/or 428 of the heavy chain constant region of ig |
| AU2005230915A1 (en) | 2004-03-26 | 2005-10-20 | Eli Lilly And Company | Compounds and methods for treating dyslipidemia |
| UA90269C2 (ru) | 2004-04-02 | 2010-04-26 | Мицубиси Танабе Фарма Корпорейшн | Тетрагидрохинолиновые производные и способ их получения |
| WO2005106493A1 (en) | 2004-04-30 | 2005-11-10 | Bayer Healthcare Ag | Diagnostics and therapeutics for diseases associated with g protein-coupled apelin receptor (apj) |
| CA2568159A1 (en) | 2004-05-28 | 2005-12-15 | Speedel Experimenta Ag | Tetrahydro-imidazo [1,5-a] pyridin derivatives as aldosterone synthase inhibitors |
| JP2008500998A (ja) | 2004-05-28 | 2008-01-17 | シュペーデル・エクスペリメンタ・アーゲー | 複素環式化合物およびアルドステロンシンターゼ阻害薬としてのそれらの使用 |
| DE602005025110D1 (de) | 2004-05-28 | 2011-01-13 | Novartis Ag | Heterocyclische verbindungen und deren verwendung als aldosteronsynthaseinhibitoren |
| EP1768951A4 (en) | 2004-06-17 | 2011-06-15 | Musc Found For Res Dev | NON-NATURAL AMINO ACIDS |
| AR049711A1 (es) | 2004-07-09 | 2006-08-30 | Speedel Experimenta Ag | Compuestos heterociclicos condensados como inhibidores de la aldosterona sintasa; composiciones farmaceuticas que los contienen y su uso en la preparacion de un medicamento para el tratamiento o prevencion de enfermedades relacionadas con el hiperaldosterismo y por una liberacion excesiva de cortiso |
| US20060045880A1 (en) | 2004-08-23 | 2006-03-02 | Krieg Paul A | Methods for modulating angiogenesis and apoptosis with apelin compositions |
| JP2008013436A (ja) | 2004-10-14 | 2008-01-24 | Kanazawa Univ | 血管形成促進剤 |
| WO2006047558A2 (en) | 2004-10-26 | 2006-05-04 | The General Hospital Corporation | Methods for detecting a trial fibrillation and related conditions |
| US8431558B2 (en) | 2004-11-01 | 2013-04-30 | The Regents Of The University Of California | Compositions and methods for modification of biomolecules |
| WO2006076736A2 (en) | 2005-01-14 | 2006-07-20 | Arizona Board Of Regents On Behalf Of The University Of Arizona | Methods for modulating angiogenesis, lymphangiogenesis, and apoptosis with apelin compositions |
| TW200716634A (en) | 2005-05-31 | 2007-05-01 | Speedel Experimenta Ag | Heterocyclic spiro-compounds |
| TW200716636A (en) | 2005-05-31 | 2007-05-01 | Speedel Experimenta Ag | Heterocyclic spiro-compounds |
| TW200716105A (en) | 2005-05-31 | 2007-05-01 | Speedel Experimenta Ag | Imidazole compounds |
| EP2330125A3 (en) | 2005-08-11 | 2012-12-12 | Amylin Pharmaceuticals, Inc. | Hybrid polypeptides with selectable properties |
| GT200600381A (es) | 2005-08-25 | 2007-03-28 | Compuestos organicos | |
| 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 |
| EP1876448A1 (en) | 2005-09-30 | 2008-01-09 | DIGILAB BioVisioN GmbH | Method and analytical reagents for identifying therapeutics using biomarkers responsive to thiazolidinediones. |
| US7736346B2 (en) | 2005-10-18 | 2010-06-15 | Biocardia, Inc. | Bio-interventional therapeutic treatments for cardiovascular diseases |
| TW200804378A (en) | 2005-12-09 | 2008-01-16 | Speedel Experimenta Ag | Organic compounds |
| US20080031871A1 (en) | 2006-02-21 | 2008-02-07 | Allen Margaret L | Memory and learning impairments associated with disruption of Ephrin receptor A6 (EphA6) gene |
| CN101415803B (zh) | 2006-04-04 | 2012-10-24 | 大阳日酸株式会社 | 甲烷分离方法、甲烷分离装置以及甲烷利用系统 |
| TW200808813A (en) | 2006-04-12 | 2008-02-16 | Speedel Experimenta Ag | Imidazo compounds |
| TW200808812A (en) | 2006-04-12 | 2008-02-16 | Speedel Experimenta Ag | Imidazo compounds |
| JPWO2007123233A1 (ja) | 2006-04-25 | 2009-09-10 | 国立大学法人九州大学 | 動脈硬化性疾患関連遺伝子、およびその利用 |
| AR060873A1 (es) | 2006-05-10 | 2008-07-16 | Novartis Ag | Derivados biciclicos como inhibidores de cetp |
| EP1886695A1 (en) | 2006-06-27 | 2008-02-13 | Speedel Experimenta AG | Pharmaceutical combination of an aldosterone synthase inhibitor and a glucocorticoid receptor antagonist or a cortisol synthesis inhibitor or a corticotropin releasing factor antagonist |
| WO2008009435A1 (en) | 2006-07-20 | 2008-01-24 | Novartis Ag | Amino-piperidine derivatives as cetp inhibitors |
| JP2010501573A (ja) | 2006-08-25 | 2010-01-21 | ノバルティス アクチエンゲゼルシャフト | アルドステロン合成酵素および／または１１−β−ヒドロキシラーゼおよび／またはアロマターゼが介在する疾患の処置のための縮合イミダゾール誘導体 |
| CA2673119A1 (en) | 2006-12-18 | 2008-06-26 | Novartis Ag | 4-imidazolyl-1,2,3,4-tetrahydroquinoline derivatives and their use as aldosterone/11-beta-hydroxylase inhibitors |
| MX2009006631A (es) | 2006-12-18 | 2009-06-30 | Novartis Ag | Imidazoles como inhibidores de sintasa de aldosterona. |
| US20100041722A1 (en) | 2006-12-18 | 2010-02-18 | Qi-Ying Hu | Organic compounds |
| ES2354008T3 (es) | 2007-03-29 | 2011-03-09 | Novartis Ag | Compuestos espiroheterocíclicos. |
| TWI448284B (zh) | 2007-04-24 | 2014-08-11 | Theravance Inc | 雙效抗高血壓劑 |
| EP2200975A1 (en) | 2007-09-07 | 2010-06-30 | Theravance, Inc. | Dual-acting antihypertensive agents |
| WO2009033819A2 (en) | 2007-09-11 | 2009-03-19 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| WO2009040019A2 (en) | 2007-09-11 | 2009-04-02 | Mondobiotech Laboratories Ag | Use of a peptide as a therapeutic agent |
| DK2207775T3 (da) | 2007-11-05 | 2012-06-18 | Novartis Ag | 4-Benzylamino-1-carboxyacylpiperidinderivater som CETP-inhibitorer, som er anvendelige til behandling af sygdomme som hyperlipidæmi eller arteriosclerose |
| JP5421282B2 (ja) | 2007-12-03 | 2014-02-19 | ノバルティス アーゲー | 高脂血症または動脈硬化症のような疾患の処置に有用なｃｅｔｐ阻害剤としての１，２−二置換−４−ベンジルアミノ−ピロリジン誘導体 |
| US20110123534A1 (en) | 2007-12-12 | 2011-05-26 | Erasmus University Medical Center Rotterdam | Novel compounds for modulating neovascularisation and methods of treatment using these compounds |
| WO2009075566A1 (en) | 2007-12-12 | 2009-06-18 | Erasmus University Medical Center Rotterdam | Biomarkers for cardiovascular disease |
| US7989484B2 (en) | 2008-04-29 | 2011-08-02 | Theravance, Inc. | Dual-acting antihypertensive agents |
| WO2009155556A2 (en) * | 2008-06-20 | 2009-12-23 | The Board Of Regents Of The University Of Texas System | Crkl targeting peptides |
| AR072297A1 (es) | 2008-06-27 | 2010-08-18 | Novartis Ag | Derivados de indol-2-il-piridin-3-ilo, composicion farmaceutica que los comprende y su uso en medicamentos para el tratamiento de enfermedades mediadas por la sintasa aldosterona. |
| CA2742043C (en) | 2008-10-24 | 2014-11-25 | Irm Llc | Biosynthetically generated pyrroline-carboxy-lysine and site specific protein modifications via chemical derivatization of pyrroline-carboxy-lysine and pyrrolysine residues |
| BRPI0921815A2 (pt) | 2008-11-04 | 2018-10-09 | Anchor Therapeutics Inc | compostos receptores de apj |
| WO2010115874A1 (en) | 2009-04-07 | 2010-10-14 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for the treatment and the diagnosis ofpulmonary arterial hypertension |
| SG175925A1 (en) | 2009-05-15 | 2011-12-29 | Novartis Ag | Aryl pyridine as aldosterone synthase inhibitors |
| BRPI1011657A2 (pt) | 2009-05-28 | 2019-04-16 | Novartis Ag | derivados aminopropiônicos substituídos como inibidores de neprilisina |
| EP2435402B1 (en) | 2009-05-28 | 2016-04-13 | Novartis AG | Substituted aminobutyric derivatives as neprilysin inhibitors |
| US20120277144A1 (en) | 2009-11-04 | 2012-11-01 | Henricus Johannes Duckers | Novel compounds for modulating neovascularisation and methods of treatment using these compounds |
| JO2967B1 (en) | 2009-11-20 | 2016-03-15 | نوفارتس ايه جي | Acetic acid derivatives of carbamoyl methyl amino are substituted as new NEP inhibitors |
| US9782454B2 (en) | 2010-04-22 | 2017-10-10 | Longevity Biotech, Inc. | Highly active polypeptides and methods of making and using the same |
| TW201138808A (en) | 2010-05-03 | 2011-11-16 | Bristol Myers Squibb Co | Serum albumin binding molecules |
| RU2457216C1 (ru) | 2010-12-21 | 2012-07-27 | Федеральное государственное учреждение "Российский кардиологический научно-производственный комплекс" Министерства здравоохранения и социального развития Российской Федерации (ФГУ "РКНПК" Минздравсоцразвития России) | Додекапептиды, обладающие кардиопротекторными свойствами |
| 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. |
| AU2013208109A1 (en) | 2012-01-09 | 2014-08-14 | Anchor Therapeutics, Inc. | APJ receptor compounds |
| US8921307B2 (en) | 2012-11-20 | 2014-12-30 | Novartis Ag | Synthetic linear apelin mimetics for the treatment of heart failure |
| AU2013350802B2 (en) * | 2012-11-30 | 2016-07-14 | Novartis Ag | Methods for making conjugates from disulfide-containing proteins |
| 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 |
| 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 |
| SG11201600211XA (en) | 2013-07-25 | 2016-02-26 | Novartis Ag | Cyclic polypeptides 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 |
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2014
- 2014-07-21 SG SG11201600211XA patent/SG11201600211XA/en unknown
- 2014-07-21 KR KR1020167004512A patent/KR20160031551A/ko not_active Withdrawn
- 2014-07-21 TW TW103124998A patent/TW201536814A/zh unknown
- 2014-07-21 JP JP2016529807A patent/JP6501775B2/ja not_active Expired - Fee Related
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- 2014-07-21 HK HK16106224.7A patent/HK1218298A1/zh unknown
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- 2014-07-21 BR BR112016001542A patent/BR112016001542A2/pt not_active Application Discontinuation
- 2014-07-21 US US14/336,262 patent/US9266925B2/en not_active Expired - Fee Related
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- 2014-07-21 AU AU2014293386A patent/AU2014293386B2/en not_active Revoked
- 2014-07-21 EP EP14747284.9A patent/EP3024845A1/en not_active Withdrawn
- 2014-07-21 PE PE2016000106A patent/PE20160878A1/es not_active Application Discontinuation
- 2014-07-21 UY UY35670A patent/UY35670A/es not_active Application Discontinuation
- 2014-07-21 WO PCT/US2014/047377 patent/WO2015013168A1/en not_active Ceased
- 2014-07-21 CN CN201480052591.5A patent/CN105612172A/zh active Pending
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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
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- 2016-01-25 CU CUP2016000013A patent/CU20160013A7/es unknown
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2017
- 2017-04-25 US US15/497,135 patent/US20170233443A1/en not_active Abandoned