JP2014521594A5 - - Google Patents
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- JP2014521594A5 JP2014521594A5 JP2014512117A JP2014512117A JP2014521594A5 JP 2014521594 A5 JP2014521594 A5 JP 2014521594A5 JP 2014512117 A JP2014512117 A JP 2014512117A JP 2014512117 A JP2014512117 A JP 2014512117A JP 2014521594 A5 JP2014521594 A5 JP 2014521594A5
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- Prior art keywords
- xaa
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- lys
- compound
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- Prior art date
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- 150000001875 compounds Chemical class 0.000 claims 21
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 11
- JUFFVKRROAPVBI-PVOYSMBESA-N chembl1210015 Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CC(=O)N[C@H]1[C@@H]([C@@H](O)[C@H](O[C@H]2[C@@H]([C@@H](O)[C@@H](O)[C@@H](CO[C@]3(O[C@@H](C[C@H](O)[C@H](O)CO)[C@H](NC(C)=O)[C@@H](O)C3)C(O)=O)O2)O)[C@@H](CO)O1)NC(C)=O)C(=O)NCC(=O)NCC(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(=O)N[C@@H](CO)C(=O)NCC(=O)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CO)C(N)=O)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCC(O)=O)NC(=O)[C@H](CCSC)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CCCCN)NC(=O)[C@H](CO)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC(O)=O)NC(=O)[C@H](CO)NC(=O)[C@@H](NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@@H](NC(=O)CNC(=O)[C@H](CCC(O)=O)NC(=O)CNC(=O)[C@@H](N)CC=1NC=NC=1)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 JUFFVKRROAPVBI-PVOYSMBESA-N 0.000 claims 5
- 108010011459 Exenatide Proteins 0.000 claims 4
- 150000001413 amino acids Chemical group 0.000 claims 4
- 229960001519 exenatide Drugs 0.000 claims 4
- 235000001014 amino acid Nutrition 0.000 claims 3
- 230000004071 biological effect Effects 0.000 claims 3
- SLYFITHISHUGLZ-LWZDQURMSA-N chembl2105635 Chemical compound N([C@H](C(=O)N[C@@H](CC(C)C)C(=O)NCC(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CO)C(=O)N[C@@H](CCC(N)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC=1N=CNC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC(C)C)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@@H]([C@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H]([C@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)C(C)C)C(=O)[C@@H]1CSSC[C@H](NC(=O)[C@@H](N)CCCCN)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@H](C)O)C(=O)N[C@@H](C)C(=O)N[C@@H]([C@H](C)O)C(=O)N1 SLYFITHISHUGLZ-LWZDQURMSA-N 0.000 claims 3
- 108010007487 davalintide Proteins 0.000 claims 3
- 229950002572 davalintide Drugs 0.000 claims 3
- 201000001320 Atherosclerosis Diseases 0.000 claims 2
- 210000002237 B-cell of pancreatic islet Anatomy 0.000 claims 2
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 2
- 208000024172 Cardiovascular disease Diseases 0.000 claims 2
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 208000030814 Eating disease Diseases 0.000 claims 2
- 208000019454 Feeding and Eating disease Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 2
- 206010020772 Hypertension Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 239000002202 Polyethylene glycol Substances 0.000 claims 2
- 208000006011 Stroke Diseases 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 125000000539 amino acid group Chemical group 0.000 claims 2
- 238000004166 bioassay Methods 0.000 claims 2
- 206010012601 diabetes mellitus Diseases 0.000 claims 2
- 235000014632 disordered eating Nutrition 0.000 claims 2
- 208000004104 gestational diabetes Diseases 0.000 claims 2
- 208000031225 myocardial ischemia Diseases 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000813 peptide hormone Substances 0.000 claims 2
- 229920001223 polyethylene glycol Polymers 0.000 claims 2
- 208000002815 pulmonary hypertension Diseases 0.000 claims 2
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 2
- SZUVGFMDDVSKSI-WIFOCOSTSA-N (1s,2s,3s,5r)-1-(carboxymethyl)-3,5-bis[(4-phenoxyphenyl)methyl-propylcarbamoyl]cyclopentane-1,2-dicarboxylic acid Chemical compound O=C([C@@H]1[C@@H]([C@](CC(O)=O)([C@H](C(=O)N(CCC)CC=2C=CC(OC=3C=CC=CC=3)=CC=2)C1)C(O)=O)C(O)=O)N(CCC)CC(C=C1)=CC=C1OC1=CC=CC=C1 SZUVGFMDDVSKSI-WIFOCOSTSA-N 0.000 claims 1
- 108010041872 Islet Amyloid Polypeptide Proteins 0.000 claims 1
- 102000036770 Islet Amyloid Polypeptide Human genes 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000001691 aryl alkyl amino group Chemical group 0.000 claims 1
- 125000002102 aryl alkyloxo group Chemical group 0.000 claims 1
- 125000001769 aryl amino group Chemical group 0.000 claims 1
- 125000004104 aryloxy group Chemical group 0.000 claims 1
- 229940126543 compound 14 Drugs 0.000 claims 1
- 229940126214 compound 3 Drugs 0.000 claims 1
- 125000006310 cycloalkyl amino group Chemical group 0.000 claims 1
- 235000018417 cysteine Nutrition 0.000 claims 1
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 1
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 1
- 125000004663 dialkyl amino group Chemical group 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 230000009977 dual effect Effects 0.000 claims 1
- 239000005556 hormone Substances 0.000 claims 1
- 229940088597 hormone Drugs 0.000 claims 1
- 229910052739 hydrogen Inorganic materials 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 230000002107 myocardial effect Effects 0.000 claims 1
- 210000004165 myocardium Anatomy 0.000 claims 1
- 230000010412 perfusion Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 229960003611 pramlintide Drugs 0.000 claims 1
- 108010029667 pramlintide Proteins 0.000 claims 1
- NRKVKVQDUCJPIZ-MKAGXXMWSA-N pramlintide acetate Chemical compound C([C@@H](C(=O)NCC(=O)N1CCC[C@H]1C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC(C)C)C(=O)N1[C@@H](CCC1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H](C(C)C)C(=O)NCC(=O)N[C@@H](CO)C(=O)N[C@@H](CC(N)=O)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CC=1C=CC(O)=CC=1)C(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CO)NC(=O)[C@H](CO)NC(=O)[C@H](CC=1NC=NC=1)NC(=O)[C@@H](NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CC=1C=CC=CC=1)NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](C)NC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CS)NC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@@H](NC(=O)[C@H](CC(N)=O)NC(=O)[C@H](CS)NC(=O)[C@@H](N)CCCCN)[C@@H](C)O)[C@@H](C)O)[C@@H](C)O)C(C)C)C1=CC=CC=C1 NRKVKVQDUCJPIZ-MKAGXXMWSA-N 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000010410 reperfusion Effects 0.000 claims 1
- 125000006850 spacer group Chemical group 0.000 claims 1
- 229920003169 water-soluble polymer Polymers 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161489951P | 2011-05-25 | 2011-05-25 | |
| US61/489,951 | 2011-05-25 | ||
| PCT/US2012/039440 WO2012162547A2 (en) | 2011-05-25 | 2012-05-24 | Long duration dual hormone conjugates |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2014521594A JP2014521594A (ja) | 2014-08-28 |
| JP2014521594A5 true JP2014521594A5 (https=) | 2015-04-23 |
Family
ID=47218099
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014512117A Pending JP2014521594A (ja) | 2011-05-25 | 2012-05-24 | 長持続期間デュアルホルモンコンジュゲート |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20140221282A1 (https=) |
| EP (1) | EP2714069A4 (https=) |
| JP (1) | JP2014521594A (https=) |
| WO (1) | WO2012162547A2 (https=) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| UA116217C2 (uk) | 2012-10-09 | 2018-02-26 | Санофі | Пептидна сполука як подвійний агоніст рецепторів glp1-1 та глюкагону |
| HK1211232A1 (en) | 2012-12-21 | 2016-05-20 | Sanofi | Exendin-4 derivatives as dual glp1/gip or trigonal glp1/gip/glucagon agonists |
| BR102013017626A2 (pt) * | 2013-06-14 | 2015-02-10 | Univ Rio De Janeiro | Bioconjugados não aglomerantes de amilinomiméticos com polietilenoglicol, uso de bioconjugados não aglomerantes de amilinomiméticos com polietilenoglicol, composições farmacêuticas de baixa toxicidade, adjuvante para a prevenção ou tratamento das doenças, medicamento, método de tratamento ou prevenção de doenças. |
| AR097701A1 (es) * | 2013-09-19 | 2016-04-13 | Zealand Pharma As | Análogos de amilina |
| EP3080152A1 (en) | 2013-12-13 | 2016-10-19 | Sanofi | Non-acylated exendin-4 peptide analogues |
| WO2015086728A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Exendin-4 peptide analogues as dual glp-1/gip receptor agonists |
| TW201609799A (zh) | 2013-12-13 | 2016-03-16 | 賽諾菲公司 | 雙重ｇｌｐ－１／ｇｉｐ受體促效劑 |
| WO2015086733A1 (en) | 2013-12-13 | 2015-06-18 | Sanofi | Dual glp-1/glucagon receptor agonists |
| TW201625668A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 作為胜肽性雙重ｇｌｐ－１／昇糖素受體激動劑之艾塞那肽－４衍生物 |
| TW201625669A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自艾塞那肽－４（Ｅｘｅｎｄｉｎ－４）之肽類雙重ＧＬＰ－１／升糖素受體促效劑 |
| TW201625670A (zh) | 2014-04-07 | 2016-07-16 | 賽諾菲公司 | 衍生自ｅｘｅｎｄｉｎ－４之雙重ｇｌｐ－１／升糖素受體促效劑 |
| US9932381B2 (en) | 2014-06-18 | 2018-04-03 | Sanofi | Exendin-4 derivatives as selective glucagon receptor agonists |
| AR105319A1 (es) | 2015-06-05 | 2017-09-27 | Sanofi Sa | Profármacos que comprenden un conjugado agonista dual de glp-1 / glucagón conector ácido hialurónico |
| AR105284A1 (es) | 2015-07-10 | 2017-09-20 | Sanofi Sa | Derivados de exendina-4 como agonistas peptídicos duales específicos de los receptores de glp-1 / glucagón |
| WO2018215506A1 (en) * | 2017-05-23 | 2018-11-29 | Université De Genève | Beta-2-glycoprotein 1 derived peptide and use thereof for treating antiphospholipid syndrome |
| AR116632A1 (es) * | 2018-10-11 | 2021-05-26 | Intarcia Therapeutics Inc | Polipéptidos análogos de la amilina humana y sus métodos de uso |
| WO2020097556A1 (en) * | 2018-11-09 | 2020-05-14 | Nektar Therapeutics | Long-acting interleukin-15 receptor agonist in combination with another pharmacologically active agent |
| EP3930757A1 (en) | 2019-03-01 | 2022-01-05 | President And Fellows Of Harvard College | Methods and compositions for protein delivery |
| WO2022034062A1 (en) * | 2020-08-12 | 2022-02-17 | Txp Pharma Ag | Exendin-4 peptide analogues |
| TWI850611B (zh) | 2020-12-18 | 2024-08-01 | 丹麥商諾佛 儂迪克股份有限公司 | Glp-1及澱粉素受體之共促效劑 |
| EP4429704A4 (en) | 2021-11-10 | 2025-11-05 | I2O Therapeutics Inc | IONIC LIQUID COMPOSITIONS |
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| US4911920A (en) | 1986-07-30 | 1990-03-27 | Alcon Laboratories, Inc. | Sustained release, comfort formulation for glaucoma therapy |
| FR2588189B1 (fr) | 1985-10-03 | 1988-12-02 | Merck Sharp & Dohme | Composition pharmaceutique de type a transition de phase liquide-gel |
| ATE141502T1 (de) | 1991-01-15 | 1996-09-15 | Alcon Lab Inc | Verwendung von karrageenan in topischen ophthalmologischen zusammensetzungen |
| HU222249B1 (hu) | 1991-03-08 | 2003-05-28 | Amylin Pharmaceuticals Inc. | Eljárás amilin agonista peptidszármazékok és ezeket tartalmazó gyógyszerkészítmények előállítására |
| US5212162A (en) | 1991-03-27 | 1993-05-18 | Alcon Laboratories, Inc. | Use of combinations gelling polysaccharides and finely divided drug carrier substrates in topical ophthalmic compositions |
| US5424286A (en) | 1993-05-24 | 1995-06-13 | Eng; John | Exendin-3 and exendin-4 polypeptides, and pharmaceutical compositions comprising same |
| US6309853B1 (en) | 1994-08-17 | 2001-10-30 | The Rockfeller University | Modulators of body weight, corresponding nucleic acids and proteins, and diagnostic and therapeutic uses thereof |
| WO1998005351A1 (en) | 1996-08-08 | 1998-02-12 | Amylin Pharmaceuticals, Inc. | Methods for regulating gastrointestinal motility |
| EP0996459B1 (en) | 1997-01-07 | 2005-09-21 | Amylin Pharmaceuticals, Inc. | Use of exendins and agonists thereof for the reduction of food intake |
| CA2299425A1 (en) | 1997-08-08 | 1999-02-18 | Amylin Pharmaceuticals, Inc. | Novel exendin agonist compounds |
| US7223725B1 (en) | 1997-11-14 | 2007-05-29 | Amylin Pharmaceuticals, Inc. | Exendin agonist compounds |
| ATE383867T1 (de) | 1997-11-14 | 2008-02-15 | Amylin Pharmaceuticals Inc | Neuartige exendin agonisten |
| WO1999025727A2 (en) | 1997-11-14 | 1999-05-27 | Amylin Pharmaceuticals, Inc. | Novel exendin agonist compounds |
| ATE366115T1 (de) | 1998-02-13 | 2007-07-15 | Amylin Pharmaceuticals Inc | Inotropische und diuretische effekte von exendin und glp-1 |
| DE69939275D1 (de) * | 1998-12-31 | 2008-09-18 | Gen Hospital Corp | Peptide, bestehend aus zwei funktionellen PTH-Domänen, die durch ein Linkermolekül verknüpft sind, und Derivate davon |
| NZ512663A (en) | 1999-01-14 | 2004-05-28 | Amylin Pharmaceuticals Inc | Novel exendin agonist formulations and methods of administration thereof |
| DK1143989T3 (da) | 1999-01-14 | 2007-04-16 | Amylin Pharmaceuticals Inc | Exendiner til glucagonundertrykkelse |
| US6528486B1 (en) | 1999-07-12 | 2003-03-04 | Zealand Pharma A/S | Peptide agonists of GLP-1 activity |
| AU2003268621B2 (en) | 2002-10-02 | 2009-01-15 | Zealand Pharma A/S | Stabilized exendin-4 compounds |
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| EP1718665B1 (en) | 2004-02-11 | 2013-04-10 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
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| EP2330124B1 (en) * | 2005-08-11 | 2015-02-25 | Amylin Pharmaceuticals, LLC | Hybrid polypeptides with selectable properties |
| CN101296942A (zh) * | 2005-08-11 | 2008-10-29 | 安米林药品公司 | 具有可选择特性的杂合多肽 |
| EP1762250A1 (en) | 2005-09-12 | 2007-03-14 | Fresenius Kabi Deutschland GmbH | Conjugates of hydroxyalkyl starch and an active substance, prepared by chemical ligation via thiazolidine |
| EP1976873A2 (en) | 2006-01-11 | 2008-10-08 | Brystol-Myers Squibb Company | Human glucagon-like-peptide-1 modulators and their use in the treatment of diabetes and related conditions |
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| US20100022457A1 (en) | 2006-05-26 | 2010-01-28 | Bristol-Myers Squibb Company | Sustained release glp-1 receptor modulators |
| AU2007267833B2 (en) | 2006-05-26 | 2012-07-26 | Amylin Pharmaceuticals, Llc | Composition and methods for treatment of congestive heart failure |
| US8497240B2 (en) * | 2006-08-17 | 2013-07-30 | Amylin Pharmaceuticals, Llc | DPP-IV resistant GIP hybrid polypeptides with selectable properties |
| JP2008169195A (ja) | 2007-01-05 | 2008-07-24 | Hanmi Pharmaceutical Co Ltd | キャリア物質を用いたインスリン分泌ペプチド薬物結合体 |
| JP2009019027A (ja) | 2007-07-16 | 2009-01-29 | Hanmi Pharmaceutical Co Ltd | アミノ末端のアミノ酸が変異したインスリン分泌ペプチド誘導体 |
| WO2009059278A1 (en) * | 2007-11-02 | 2009-05-07 | Centocor, Inc. | Semi-synthetic glp-1 peptide-fc fusion constructs, methods and uses |
| KR20100098628A (ko) * | 2007-11-14 | 2010-09-08 | 아밀린 파마슈티칼스, 인크. | 비만 및 비만 관련 질환 및 장애의 치료 방법 |
| JO2870B1 (en) * | 2008-11-13 | 2015-03-15 | ميرك شارب اند دوهم كورب | Amino Tetra Hydro Pirans as Inhibitors of Peptide Dipeptide IV for the Treatment or Prevention of Diabetes |
| WO2010120476A2 (en) | 2009-04-01 | 2010-10-21 | Amylin Pharmaceuticals, Inc. | N-terminus conformationally constrained glp-1 receptor agonist compounds |
| EA023925B1 (ru) * | 2010-04-27 | 2016-07-29 | Зилэнд Фарма А/С | Пептидные конъюгаты агонистов рецептора glp-1 и их применение |
-
2012
- 2012-05-24 JP JP2014512117A patent/JP2014521594A/ja active Pending
- 2012-05-24 WO PCT/US2012/039440 patent/WO2012162547A2/en not_active Ceased
- 2012-05-24 US US14/119,581 patent/US20140221282A1/en not_active Abandoned
- 2012-05-24 EP EP12789841.9A patent/EP2714069A4/en not_active Withdrawn
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