HUP0002303A2 - Benzofurazán-származékok és alkalmazásuk AMPA receptor aktivitást fokozó hatású gyógyszerkészítmények előállítására - Google Patents
Benzofurazán-származékok és alkalmazásuk AMPA receptor aktivitást fokozó hatású gyógyszerkészítmények előállításáraInfo
- Publication number
- HUP0002303A2 HUP0002303A2 HU0002303A HUP0002303A HUP0002303A2 HU P0002303 A2 HUP0002303 A2 HU P0002303A2 HU 0002303 A HU0002303 A HU 0002303A HU P0002303 A HUP0002303 A HU P0002303A HU P0002303 A2 HUP0002303 A2 HU P0002303A2
- Authority
- HU
- Hungary
- Prior art keywords
- independently
- carboxylic acid
- crr
- group
- groups
- Prior art date
Links
- 102000003678 AMPA Receptors Human genes 0.000 title abstract 2
- 108090000078 AMPA Receptors Proteins 0.000 title abstract 2
- AWBOSXFRPFZLOP-UHFFFAOYSA-N 2,1,3-benzoxadiazole Chemical class C1=CC=CC2=NON=C21 AWBOSXFRPFZLOP-UHFFFAOYSA-N 0.000 title 1
- 239000008194 pharmaceutical composition Substances 0.000 title 1
- -1 nitro- Chemical class 0.000 abstract 8
- 150000001299 aldehydes Chemical class 0.000 abstract 2
- 125000003545 alkoxy group Chemical group 0.000 abstract 2
- 125000000217 alkyl group Chemical group 0.000 abstract 2
- 125000004414 alkyl thio group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 abstract 2
- 150000001733 carboxylic acid esters Chemical class 0.000 abstract 2
- 125000005843 halogen group Chemical group 0.000 abstract 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- 241000124008 Mammalia Species 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 150000001721 carbon Chemical group 0.000 abstract 1
- 229910052799 carbon Inorganic materials 0.000 abstract 1
- 230000003920 cognitive function Effects 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 230000002708 enhancing effect Effects 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 230000006386 memory function Effects 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
- 230000000698 schizophrenic effect Effects 0.000 abstract 1
- 229910052717 sulfur Chemical group 0.000 abstract 1
- 125000004434 sulfur atom Chemical group 0.000 abstract 1
- 230000003313 weakening effect Effects 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D285/00—Heterocyclic compounds containing rings having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by groups C07D275/00 - C07D283/00
- C07D285/01—Five-membered rings
- C07D285/02—Thiadiazoles; Hydrogenated thiadiazoles
- C07D285/14—Thiadiazoles; Hydrogenated thiadiazoles condensed with carbocyclic rings or ring systems
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P5/00—Drugs for disorders of the endocrine system
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
- C07D271/12—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms condensed with carbocyclic rings or ring systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Endocrinology (AREA)
- Pain & Pain Management (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Hydrogenated Pyridines (AREA)
- Breeding Of Plants And Reproduction By Means Of Culturing (AREA)
- Luminescent Compositions (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Furan Compounds (AREA)
Abstract
Az (I) általános képletű vegyületek - a képletben R1 jelentése oxigénatom vagy kénatom; R2 és R3 jelentése egymástól függetlenül -N=, -CR= vagy -CX=; M jelentése =N- vagy =CR4-; R4 és R8 jelentése egymástól függetlenül R, vagy együtt egyetlenkötőmaradékot képeznek és a gyűrű 2'-helyzete között; ez a kötőmaradéklehet egyes kötés, -CRR'-, -CR=CR'-, -C(O)-, -O-, -S(O)y-, -NR- vagy -N=; és R5 és R7 jelentése egymástól függetlenül -(CRR')n-, -C(O)-, -CR=CR'-,-CR=CX-, -CRX-, -CXX'-, -S- vagy -O-; és R6 jelentése -(CRR')m-, -C(O)-, -CR=CR'-, -CRX-, -CXX'-, -S- vagy -O-;ahol X és X' jelentése egymástól függetlenül -Br, -Cl, -F, -CN, -NO2, -OR,-SR, -NRR', -C(O)R, -CO2R vagy -CONRR', ahol két R vagy R' csoport egyX csoporton belül vagy két szomszédos különálló X csoportban együttgyűrűt alkothat; R és R' jelentése egymástól függetlenül (i) hidrogénatom, (ii) 1-6szénatomos egyenes vagy elágazó szénláncú alkilcsoport, amelyszubsztituálatlan, vagy egy vagy több halogénatom, nitro-, alkoxi-,hidroxi-, alkil-tio-, amino-, keto-, aldehid-, karbonsav-, karbonsav-észter- vagy karbonsav-amid-csoport közül választott funkcionalitássallehet szubsztituálva, ahol két ilyen alkilcsoport ugyanazon aszénatomon vagy szomszédos szénatomokon együtt gyűrűt is alkothat,vagy (iii) arilcsoport, amely szubsztituálatlan vagy egy vagy többhalogénatom, nitro-, alkoxi-, hidroxi-, aril-oxi-, alkil-tio-, amino-,keto-, aldehid-, karbonsav-, karbonsav-észter- vagy karbonsav-amid-csoport közül választott funkcionalitással lehet szubsztituálva; m és p értéke egymástól függetlenül 0 vagy 1; és n és y értéke egymástól függetlenül 0, 1 vagy 2 - emlősökben AMPA-receptort fokozó aktivitással rendelkeznek, fenti tulajdonságaikkövetkeztében memória vagy megismerési funkciók gyengülésénekjavítására, illetve skizofrénia vagy skizofrén viselkedés kezelésérealkalmazhatók. Ó
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US08/800,108 US6110935A (en) | 1997-02-13 | 1997-02-13 | Benzofurazan compounds for enhancing glutamatergic synaptic responses |
| PCT/US1998/002713 WO1998035950A1 (en) | 1997-02-13 | 1998-02-13 | Benzofurazan compounds which enhance ampa receptor activity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| HUP0002303A2 true HUP0002303A2 (hu) | 2001-04-28 |
| HUP0002303A3 HUP0002303A3 (en) | 2002-09-30 |
Family
ID=25177504
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| HU0002303A HUP0002303A3 (en) | 1997-02-13 | 1998-02-13 | Benzofurazan derivatives and their use for the preparation of pharmaceutical compositions which enhance ampa receptor activity |
Country Status (24)
| Country | Link |
|---|---|
| US (3) | US6110935A (hu) |
| EP (2) | EP1428534B1 (hu) |
| JP (1) | JP4446023B2 (hu) |
| KR (1) | KR100544295B1 (hu) |
| CN (1) | CN1085206C (hu) |
| AT (2) | ATE326221T1 (hu) |
| AU (1) | AU737802C (hu) |
| BR (1) | BR9807333B1 (hu) |
| CA (1) | CA2279319C (hu) |
| CZ (1) | CZ299765B6 (hu) |
| DE (2) | DE69823803T2 (hu) |
| DK (2) | DK0960105T3 (hu) |
| ES (2) | ES2264078T3 (hu) |
| GB (1) | GB2325225B (hu) |
| HU (1) | HUP0002303A3 (hu) |
| ID (1) | ID22342A (hu) |
| IL (1) | IL131200A (hu) |
| NO (1) | NO318935B1 (hu) |
| NZ (1) | NZ336980A (hu) |
| PL (1) | PL199135B1 (hu) |
| PT (2) | PT960105E (hu) |
| RU (1) | RU2189984C2 (hu) |
| TR (1) | TR199901941T2 (hu) |
| WO (1) | WO1998035950A1 (hu) |
Families Citing this family (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN188837B (hu) | 1998-05-22 | 2002-11-09 | Torrent Pharmaceuticals Ltd | |
| WO2003053439A1 (en) * | 2001-12-20 | 2003-07-03 | Alangudi Sankaranarayanan | Use of benzofuroxan derivatives as antiplatelet agents |
| NZ540468A (en) * | 2003-01-13 | 2008-03-28 | Univ California | Method of treating cognitive decline due to sleep deprivation and stress using an AMPA receptor potentiator |
| ES2300775T3 (es) * | 2003-05-23 | 2008-06-16 | Basilea Pharmaceutica Ag | Furazanobencimidazoles. |
| JP2007519733A (ja) * | 2004-01-26 | 2007-07-19 | コーテックス ファーマシューティカルズ インコーポレーティッド | アンパカインにより誘導されるシナプス応答促通のコリンエステラーゼ阻害剤による増強方法 |
| JP2010501597A (ja) | 2006-08-31 | 2010-01-21 | ザ ガバナーズ オブ ザ ユニバーシティー オブ アルバータ | 正のアロステリックａｍｐａ受容体モジュレーターを用いて呼吸抑制を阻害する方法 |
| RS52108B (en) * | 2007-01-03 | 2012-08-31 | Les Laboratoires Servier | 3-SUBSTITUTED [1,2,3] -BENZOTRIAZINONE UNIT TO INCREASE GLUTAMATERGIC SYNAPTIC ANSWERS |
| EA200900937A1 (ru) * | 2007-01-03 | 2009-12-30 | Кортекс Фармасеутикалс, Инк. | Соединения 3-замещенного-[1,2,3]бензотриазинона для усиления глутаматергических синаптических ответов |
| EP2154970B1 (en) * | 2007-05-17 | 2017-10-25 | RespireRx Pharmaceuticals Inc. | Di-substituted amides for enhancing glutamatergic synaptic responses |
| US8263591B2 (en) * | 2007-08-10 | 2012-09-11 | Cortex Pharmaceuticals, Inc. | Bicyclic amides for enhancing glutamatergic synaptic responses |
| US8119632B2 (en) | 2007-08-10 | 2012-02-21 | Cortex Pharmaceuticals, Inc. | Bicyclic amide derivatives for enhancing glutamatergic synaptic responses |
| US8071914B2 (en) * | 2007-12-26 | 2011-12-06 | Noboru Oshima | Heating apparatus |
| US20110218190A1 (en) * | 2008-11-10 | 2011-09-08 | The Regents Of The University Of California | Therapeutic uses of ampa receptor modulators for treatment of motor dysfunction |
| AU2010208646A1 (en) * | 2009-02-02 | 2011-09-01 | Cortex Pharmaceuticals, Inc. | Bicyclic amide derivatives for enhancing glutamatergic synaptic responses |
| WO2011109398A2 (en) | 2010-03-02 | 2011-09-09 | President And Fellows Of Harvard College | Methods and compositions for treatment of angelman syndrome and autism spectrum disorders |
| US20110257186A1 (en) * | 2010-04-15 | 2011-10-20 | Staubli Ursula V | Compositions and methods for treating visual disorders |
| EP2801377B1 (en) | 2011-03-04 | 2019-08-07 | The Regents of The University of California | Hydrogel comprising cells for local release of growth factors to mediate motor recovery after stroke |
| CN102633731B (zh) * | 2012-03-13 | 2014-04-30 | 四川大学华西医院 | 6-喹喔啉甲酸酰胺化合物、制备方法和应用 |
| KR101421032B1 (ko) * | 2012-12-28 | 2014-07-22 | 주식회사 레고켐 바이오사이언스 | (2-메틸-1-(3-메틸벤질)-1Ｈ-벤조[d]이미다졸-5일)(피페리딘-5-일)메탄온의 제조방법 |
| AU2014277952A1 (en) | 2013-06-13 | 2016-01-28 | Veroscience Llc | Compositions and methods for treating metabolic disorders |
| CN107286114B (zh) * | 2016-04-13 | 2020-08-18 | 中国人民解放军军事医学科学院毒物药物研究所 | Ampa受体增效剂的脑靶向前药及其医药用途 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3981864A (en) * | 1973-09-08 | 1976-09-21 | Eisai Co., Ltd. | 1,3-Benzodioxol derivatives |
| FR2499991A1 (fr) * | 1981-02-19 | 1982-08-20 | Sandoz Sa | Nouveaux 2,1,3-benzothiadiazoles et 2,1,3-benzoxadiazoles, leur preparation et leur application comme medicaments |
| US4420485A (en) * | 1982-09-29 | 1983-12-13 | Hoechst-Roussel Pharmaceuticals Inc. | 1'-[3-(1,2-Benzisoxazol-3-yl) proply]spiro[benzofuran-2(3H),3' or 4'-piperidines or 3'-pyrrolidines] |
| IL96507A0 (en) * | 1989-12-08 | 1991-08-16 | Merck & Co Inc | Nitrogen-containing spirocycles and pharmaceutical compositions containing them |
| US5112824A (en) * | 1989-12-08 | 1992-05-12 | Merck & Co., Inc. | Benzofuran compounds as class III antiarrhythmic agents |
| US5032604A (en) * | 1989-12-08 | 1991-07-16 | Merck & Co., Inc. | Class III antiarrhythmic agents |
| DK0651746T3 (da) * | 1992-07-24 | 2002-07-29 | Univ California | Lægemidler, der forbedrer synaptiske responser medieret af AMPA-receptorer |
| EP0709384B1 (de) * | 1994-10-31 | 1998-12-23 | MERCK PATENT GmbH | Benzylpiperidinderivate mit hoher Affinität zu Bindungsstellen von Aminosäure-Rezeptoren |
| US5650409A (en) * | 1995-06-02 | 1997-07-22 | Cortex Pharmaceuticals, Inc. | Benzoyl piperidines/pyrrolidines for enhancing synaptic response |
| US5736543A (en) * | 1996-04-03 | 1998-04-07 | The Regents Of The University Of California | Benzoxazines for enhancing synaptic response |
| US5985871A (en) | 1997-12-24 | 1999-11-16 | Cortex Pharmaceuticals, Inc. | Benzoxazine compounds for enhancing synaptic response |
-
1997
- 1997-02-13 US US08/800,108 patent/US6110935A/en not_active Expired - Lifetime
-
1998
- 1998-02-13 NZ NZ336980A patent/NZ336980A/xx not_active IP Right Cessation
- 1998-02-13 DE DE69823803T patent/DE69823803T2/de not_active Expired - Lifetime
- 1998-02-13 EP EP04075259A patent/EP1428534B1/en not_active Expired - Lifetime
- 1998-02-13 CA CA002279319A patent/CA2279319C/en not_active Expired - Fee Related
- 1998-02-13 PT PT98906358T patent/PT960105E/pt unknown
- 1998-02-13 GB GB9809221A patent/GB2325225B/en not_active Expired - Fee Related
- 1998-02-13 ID IDW990855A patent/ID22342A/id unknown
- 1998-02-13 AT AT04075259T patent/ATE326221T1/de active
- 1998-02-13 HU HU0002303A patent/HUP0002303A3/hu unknown
- 1998-02-13 KR KR1019997007369A patent/KR100544295B1/ko not_active IP Right Cessation
- 1998-02-13 ES ES04075259T patent/ES2264078T3/es not_active Expired - Lifetime
- 1998-02-13 TR TR1999/01941T patent/TR199901941T2/xx unknown
- 1998-02-13 BR BRPI9807333-8A patent/BR9807333B1/pt not_active IP Right Cessation
- 1998-02-13 CN CN98802541A patent/CN1085206C/zh not_active Expired - Fee Related
- 1998-02-13 PL PL335058A patent/PL199135B1/pl not_active IP Right Cessation
- 1998-02-13 DK DK98906358T patent/DK0960105T3/da active
- 1998-02-13 US US09/355,139 patent/US6313115B1/en not_active Expired - Fee Related
- 1998-02-13 EP EP98906358A patent/EP0960105B1/en not_active Expired - Lifetime
- 1998-02-13 DK DK04075259T patent/DK1428534T3/da active
- 1998-02-13 RU RU99119488/04A patent/RU2189984C2/ru not_active IP Right Cessation
- 1998-02-13 ES ES98906358T patent/ES2221152T3/es not_active Expired - Lifetime
- 1998-02-13 JP JP53589698A patent/JP4446023B2/ja not_active Expired - Fee Related
- 1998-02-13 AU AU61599/98A patent/AU737802C/en not_active Ceased
- 1998-02-13 PT PT04075259T patent/PT1428534E/pt unknown
- 1998-02-13 CZ CZ0279599A patent/CZ299765B6/cs not_active IP Right Cessation
- 1998-02-13 WO PCT/US1998/002713 patent/WO1998035950A1/en not_active Application Discontinuation
- 1998-02-13 DE DE69834590T patent/DE69834590T2/de not_active Expired - Lifetime
- 1998-02-13 IL IL13120098A patent/IL131200A/xx not_active IP Right Cessation
- 1998-02-13 AT AT98906358T patent/ATE266649T1/de active
-
1999
- 1999-08-04 NO NO19993768A patent/NO318935B1/no not_active IP Right Cessation
-
2001
- 2001-04-27 US US09/845,128 patent/US6730677B2/en not_active Expired - Fee Related
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