CN101711237B - 氮杂肽衍生物 - Google Patents
氮杂肽衍生物 Download PDFInfo
- Publication number
- CN101711237B CN101711237B CN2008800216013A CN200880021601A CN101711237B CN 101711237 B CN101711237 B CN 101711237B CN 2008800216013 A CN2008800216013 A CN 2008800216013A CN 200880021601 A CN200880021601 A CN 200880021601A CN 101711237 B CN101711237 B CN 101711237B
- Authority
- CN
- China
- Prior art keywords
- compound
- pharmaceutically acceptable
- compounds
- atazanavir
- composition
- 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.)
- Expired - Fee Related
Links
- 0 *C(c(cc1)ccc1-c1ccccn1)N(C[C@@]([C@](Cc1ccccc1)NC([C@](C(*)(*)*)NC(O*)=O)=O)O)NC([C@](*)NC(O*)=O)=O Chemical compound *C(c(cc1)ccc1-c1ccccn1)N(C[C@@]([C@](Cc1ccccc1)NC([C@](C(*)(*)*)NC(O*)=O)=O)O)NC([C@](*)NC(O*)=O)=O 0.000 description 11
- RJFFVAGYPXHKIN-UHFFFAOYSA-N CC(CN1CCN(C)CC1)=O Chemical compound CC(CN1CCN(C)CC1)=O RJFFVAGYPXHKIN-UHFFFAOYSA-N 0.000 description 1
- LWAQMFOMLLTHKZ-UHFFFAOYSA-N CC(CN1CCNCC1)=O Chemical compound CC(CN1CCNCC1)=O LWAQMFOMLLTHKZ-UHFFFAOYSA-N 0.000 description 1
- LOBSVGRXQAHJDT-UHFFFAOYSA-N CC(CN1CCOCC1)=O Chemical compound CC(CN1CCOCC1)=O LOBSVGRXQAHJDT-UHFFFAOYSA-N 0.000 description 1
Images
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
- C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4418—Non condensed pyridines; Hydrogenated derivatives thereof having a carbocyclic group directly attached to the heterocyclic ring, e.g. cyproheptadine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
- A61P31/12—Antivirals
- A61P31/14—Antivirals for RNA viruses
- A61P31/18—Antivirals for RNA viruses for HIV
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/553—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
- C07F9/576—Six-membered rings
- C07F9/58—Pyridine rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Molecular Biology (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Public Health (AREA)
- Oncology (AREA)
- Virology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Communicable Diseases (AREA)
- Biochemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- AIDS & HIV (AREA)
- Tropical Medicine & Parasitology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Peptides Or Proteins (AREA)
- Pyridine Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US93420107P | 2007-06-12 | 2007-06-12 | |
| US60/934,201 | 2007-06-12 | ||
| US6762708P | 2008-02-29 | 2008-02-29 | |
| US61/067,627 | 2008-02-29 | ||
| PCT/US2008/007331 WO2008156632A1 (en) | 2007-06-12 | 2008-06-12 | Azapeptide derivatives |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011102869075A Division CN102424668A (zh) | 2007-06-12 | 2008-06-12 | 氮杂肽衍生物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN101711237A CN101711237A (zh) | 2010-05-19 |
| CN101711237B true CN101711237B (zh) | 2013-08-07 |
Family
ID=39730784
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011102869075A Pending CN102424668A (zh) | 2007-06-12 | 2008-06-12 | 氮杂肽衍生物 |
| CN2008800216013A Expired - Fee Related CN101711237B (zh) | 2007-06-12 | 2008-06-12 | 氮杂肽衍生物 |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2011102869075A Pending CN102424668A (zh) | 2007-06-12 | 2008-06-12 | 氮杂肽衍生物 |
Country Status (25)
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW200835693A (en) * | 2007-02-23 | 2008-09-01 | Auspex Pharmaceuticals Inc | Preparation and utility of non-nucleoside reverse transcriptase inhibitors |
| ES2394952T3 (es) | 2007-06-12 | 2013-02-07 | Concert Pharmaceuticals Inc. | Derivados de axapéptido como inhibidores de la proteasa VIH |
| US9163067B2 (en) * | 2008-10-06 | 2015-10-20 | Yissum Research Development Company Of The Hebrew University Of Jerusalem Ltd | HIV-1 integrase derived stimulatory peptides interfering with integrase—Rev protein binding |
| WO2010132663A1 (en) * | 2009-05-13 | 2010-11-18 | Concert Pharmaceticals, Inc. | Pegylated azapeptide derivatives as hiv protease inhibitors |
| WO2010135424A1 (en) * | 2009-05-19 | 2010-11-25 | Glaxosmithkline Llc | Chemical compounds |
| CA2784530C (en) | 2009-12-21 | 2018-05-22 | Janssen R&D Ireland | Degradable removable implant for the sustained release of an active compound |
| WO2011080562A1 (en) | 2009-12-29 | 2011-07-07 | Hetero Research Foundation | Novel aza-peptides containing 2,2-disubstituted cyclobutyl and/or substituted alkoxy benzyl derivatives as antivirals |
| HUE030883T2 (en) | 2011-06-20 | 2017-06-28 | H Lundbeck As | Deuterated 1-piperazino-3-phenylindanes for the treatment of schizophrenia |
| CN106543073A (zh) * | 2015-09-17 | 2017-03-29 | 宁波杰尔盛化工有限公司 | 2-[4-(2-吡啶基)苄基]-肼羧酸叔丁酯的制备方法 |
| MX374931B (es) * | 2015-12-02 | 2025-03-06 | Merck Sharp & Dohme Llc | Composiciones farmaceuticas que contienen doravirina, tenofovir disoproxil fumarato y lamivudina. |
| KR102558066B1 (ko) | 2016-03-28 | 2023-07-25 | 인사이트 코포레이션 | Tam 억제제로서 피롤로트리아진 화합물 |
| JOP20180009A1 (ar) | 2017-02-06 | 2019-01-30 | Gilead Sciences Inc | مركبات مثبط فيروس hiv |
| WO2019025250A1 (en) | 2017-08-04 | 2019-02-07 | Basf Se | SUBSTITUTED TRIFLUOROMETHYLOXADIAZOLES FOR COMBATING PHYTOPATHOGENIC FUNGI |
| IL273579B2 (en) | 2017-09-27 | 2025-10-01 | Incyte Corp | Salts of pyrrolizidine derivatives used as Tm inhibitors. |
| HRP20250676T1 (hr) | 2018-06-29 | 2025-08-01 | Incyte Corporation | Formulacije inhibitora axl/mer |
| TWI829205B (zh) | 2018-07-30 | 2024-01-11 | 美商基利科學股份有限公司 | 抗hiv化合物 |
| CN115697343A (zh) | 2020-03-06 | 2023-02-03 | 因赛特公司 | 包含axl/mer和pd-1/pd-l1抑制剂的组合疗法 |
| EP4135740A4 (en) * | 2020-04-16 | 2024-05-22 | The Medical College of Wisconsin, Inc. | AEROSOLATED FORMULATIONS OF HIV PROTEASE INHIBITORS FOR THE TREATMENT OF RESPIRATORY TRACT REFLUX |
| CN114426568B (zh) * | 2022-01-11 | 2023-04-25 | 嘉兴安谛康生物科技有限公司 | 2-氧代-3-吡咯烷基丙腈类化合物及其药物组合物和用途 |
| WO2024249517A1 (en) | 2023-05-31 | 2024-12-05 | Gilead Sciences, Inc. | Anti-hiv compounds |
| CN116987024A (zh) * | 2023-08-01 | 2023-11-03 | 浙江荣耀生物科技股份有限公司 | 一种阿扎那韦中间体的制备方法 |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006014282A2 (en) * | 2004-07-06 | 2006-02-09 | Abbott Laboratories | Prodrugs of hiv protease inhibitors |
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| EP0206497B1 (en) | 1985-05-15 | 1994-07-20 | The Wellcome Foundation Limited | Therapeutic nucleosides and their preparation |
| GB8815265D0 (en) | 1988-06-27 | 1988-08-03 | Wellcome Found | Therapeutic nucleosides |
| US5696270A (en) | 1989-05-23 | 1997-12-09 | Abbott Laboratories | Intermediate for making retroviral protease inhibiting compounds |
| US5304121A (en) | 1990-12-28 | 1994-04-19 | Boston Scientific Corporation | Drug delivery system making use of a hydrogel polymer coating |
| GB9009861D0 (en) | 1990-05-02 | 1990-06-27 | Glaxo Group Ltd | Chemical compounds |
| ES2189721T3 (es) | 1992-12-29 | 2003-07-16 | Abbott Lab | Inhibidores de proteasa retroviral. |
| US5886026A (en) | 1993-07-19 | 1999-03-23 | Angiotech Pharmaceuticals Inc. | Anti-angiogenic compositions and methods of use |
| US6221335B1 (en) | 1994-03-25 | 2001-04-24 | Isotechnika, Inc. | Method of using deuterated calcium channel blockers |
| AU707748B2 (en) | 1994-03-25 | 1999-07-22 | Isotechnika Inc. | Enhancement of the efficacy of drugs by deuteration |
| US6099562A (en) | 1996-06-13 | 2000-08-08 | Schneider (Usa) Inc. | Drug coating with topcoat |
| TW409125B (en) * | 1996-04-22 | 2000-10-21 | Novartis Ag | Antivirally active heterocyclic azahexane derivatives |
| US5849911A (en) | 1996-04-22 | 1998-12-15 | Novartis Finance Corporation | Antivirally active heterocyclic azahexane derivatives |
| WO1997046514A1 (en) | 1996-05-31 | 1997-12-11 | Novartis Ag | Process for the preparation of hydrazine derivatives useful as intermediates for the preparation of peptide analogues |
| US6087383A (en) * | 1998-01-20 | 2000-07-11 | Bristol-Myers Squibb Company | Bisulfate salt of HIV protease inhibitor |
| US6440710B1 (en) | 1998-12-10 | 2002-08-27 | The Scripps Research Institute | Antibody-catalyzed deuteration, tritiation, dedeuteration or detritiation of carbonyl compounds |
| GB9914821D0 (en) | 1999-06-24 | 1999-08-25 | Glaxo Group Ltd | Compounds |
| GB9925962D0 (en) | 1999-11-02 | 1999-12-29 | Novartis Ag | Organic compounds |
| EP1104760B1 (en) | 1999-12-03 | 2003-03-12 | Pfizer Products Inc. | Sulfamoylheteroaryl pyrazole compounds as anti-inflammatory/analgesic agents |
| PL366998A1 (en) | 2001-05-03 | 2005-02-07 | F.Hoffmann-La Roche Ag | Pharmaceutical dosage form of amorphous nelfinavir mesylate |
| US6737042B2 (en) | 2001-05-24 | 2004-05-18 | Alexza Molecular Delivery Corporation | Delivery of drug esters through an inhalation route |
| JP2005501880A (ja) | 2001-08-31 | 2005-01-20 | ブリストル−マイヤーズ スクイブ カンパニー | Hiv療法におけるアタザナビルの使用 |
| TW200413273A (en) | 2002-11-15 | 2004-08-01 | Wako Pure Chem Ind Ltd | Heavy hydrogenation method of heterocyclic rings |
| CN101829327A (zh) | 2003-02-21 | 2010-09-15 | 加罗配方公司 | 包含喹啉抗疟化合物和蛋白酶抑制剂的组合的药物组合物及其应用 |
| US20050131017A1 (en) | 2003-12-11 | 2005-06-16 | Degoey David A. | HIV protease inhibiting compounds |
| US20050148523A1 (en) | 2003-12-15 | 2005-07-07 | Colonno Richard J. | Method of treating HIV infection in atazanavir-resistant patients using a combination of atazanavir and another protease inhibitor |
| US7829720B2 (en) * | 2004-05-04 | 2010-11-09 | Bristol-Myers Squibb Company | Process for preparing atazanavir bisulfate and novel forms |
| WO2006039237A1 (en) | 2004-09-29 | 2006-04-13 | Cordis Corporation | Pharmaceutical dosage forms of stable amorphous rapamycin like compounds |
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| CN101309917B (zh) | 2005-10-06 | 2013-09-11 | 奥斯拜客斯制药有限公司 | 具有增强治疗性质的胃h+,k+-atp酶氘代抑制剂 |
| US7750168B2 (en) | 2006-02-10 | 2010-07-06 | Sigma-Aldrich Co. | Stabilized deuteroborane-tetrahydrofuran complex |
| JO2630B1 (en) | 2006-04-13 | 2012-06-17 | نوفارتيس ايه جي | Organic compounds |
| WO2008030382A1 (en) | 2006-09-05 | 2008-03-13 | Schering Corporation | Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis |
| ES2394952T3 (es) | 2007-06-12 | 2013-02-07 | Concert Pharmaceuticals Inc. | Derivados de axapéptido como inhibidores de la proteasa VIH |
| US20090076097A1 (en) | 2007-09-14 | 2009-03-19 | Protia, Llc | Deuterium-enriched atazanavir |
| WO2010132663A1 (en) | 2009-05-13 | 2010-11-18 | Concert Pharmaceticals, Inc. | Pegylated azapeptide derivatives as hiv protease inhibitors |
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2008
- 2008-06-12 ES ES11155667T patent/ES2394952T3/es active Active
- 2008-06-12 CN CN2011102869075A patent/CN102424668A/zh active Pending
- 2008-06-12 BR BRPI0813911-3A patent/BRPI0813911A2/pt not_active IP Right Cessation
- 2008-06-12 AT AT09075359T patent/ATE536343T1/de active
- 2008-06-12 CA CA2692028A patent/CA2692028C/en not_active Expired - Fee Related
- 2008-06-12 EP EP11155667A patent/EP2322509B1/en active Active
- 2008-06-12 JP JP2010512186A patent/JP2010529196A/ja active Pending
- 2008-06-12 ES ES08252023T patent/ES2356334T3/es active Active
- 2008-06-12 TW TW097122018A patent/TW200908970A/zh unknown
- 2008-06-12 MX MX2009013565A patent/MX2009013565A/es active IP Right Grant
- 2008-06-12 US US12/157,712 patent/US20090036357A1/en not_active Abandoned
- 2008-06-12 RS RSP-2010/0034A patent/RS51226B/sr unknown
- 2008-06-12 ES ES09075359T patent/ES2395137T3/es active Active
- 2008-06-12 PT PT08252023T patent/PT2003120E/pt unknown
- 2008-06-12 SI SI200830012T patent/SI2003120T1/sl unknown
- 2008-06-12 CN CN2008800216013A patent/CN101711237B/zh not_active Expired - Fee Related
- 2008-06-12 BR BRPI0823520-1A patent/BRPI0823520A2/pt not_active IP Right Cessation
- 2008-06-12 AR ARP080102501A patent/AR066972A1/es unknown
- 2008-06-12 DE DE602008000255T patent/DE602008000255D1/de active Active
- 2008-06-12 EP EP08252023A patent/EP2003120B9/en active Active
- 2008-06-12 EP EP09075359A patent/EP2116532B1/en active Active
- 2008-06-12 DK DK08252023.0T patent/DK2003120T3/da active
- 2008-06-12 KR KR1020127003399A patent/KR20120029480A/ko not_active Withdrawn
- 2008-06-12 AT AT08252023T patent/ATE447554T1/de active
- 2008-06-12 AU AU2008267048A patent/AU2008267048C1/en not_active Ceased
- 2008-06-12 RU RU2010100821/04A patent/RU2448958C2/ru not_active IP Right Cessation
- 2008-06-12 PL PL08252023T patent/PL2003120T3/pl unknown
- 2008-06-12 KR KR1020107000675A patent/KR101185899B1/ko not_active Expired - Fee Related
- 2008-06-12 WO PCT/US2008/007331 patent/WO2008156632A1/en not_active Ceased
-
2009
- 2009-12-11 CO CO09141805A patent/CO6241121A2/es not_active Application Discontinuation
- 2009-12-18 ZA ZA2009/09079A patent/ZA200909079B/en unknown
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2010
- 2010-02-03 CY CY20101100099T patent/CY1109766T1/el unknown
- 2010-02-03 HR HR20100065T patent/HRP20100065T1/hr unknown
- 2010-04-06 US US12/755,184 patent/US8158805B2/en not_active Expired - Fee Related
-
2012
- 2012-01-19 RU RU2012101881/04A patent/RU2012101881A/ru not_active Application Discontinuation
- 2012-03-02 US US13/411,089 patent/US8258309B2/en not_active Expired - Fee Related
- 2012-08-27 US US13/595,511 patent/US20130041156A1/en not_active Abandoned
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006014282A2 (en) * | 2004-07-06 | 2006-02-09 | Abbott Laboratories | Prodrugs of hiv protease inhibitors |
Non-Patent Citations (3)
| Title |
|---|
| Cihlar et al.Suppression of HIV-1 protease inhibitor resistance by posphonate-mediated solvent anchoring.《Journal of molecular biology》.2006,第363卷(第3期),635-647. * |
| Xu zhongmin et al.Process research and development for an efficient synthesis of the HIV protease inhibitor BMS-232632.《Organic procesws research & development》.2002,第6卷(第3期),323-328. * |
| Zhang Huiping et al.A facile and efficient syntheis of d3-labelled reyatazTM.《Journal of labelled compounds and radiopharmaceuticals》.2005,第48卷(第14期),1041-1047. * |
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