ECSP13013025A - Inhibidores de la tirosina-quinasa de bruton - Google Patents
Inhibidores de la tirosina-quinasa de brutonInfo
- Publication number
- ECSP13013025A ECSP13013025A ECSP13013025A ECSP13013025A EC SP13013025 A ECSP13013025 A EC SP13013025A EC SP13013025 A ECSP13013025 A EC SP13013025A EC SP13013025 A ECSP13013025 A EC SP13013025A
- Authority
- EC
- Ecuador
- Prior art keywords
- compounds
- btk
- quinase
- bruton
- tyrosine
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 230000000694 effects Effects 0.000 abstract 2
- 208000023275 Autoimmune disease Diseases 0.000 abstract 1
- 230000001594 aberrant effect Effects 0.000 abstract 1
- 210000003719 b-lymphocyte Anatomy 0.000 abstract 1
- 239000003085 diluting agent Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000027866 inflammatory disease Diseases 0.000 abstract 1
- 230000002757 inflammatory effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000000546 pharmaceutical excipient Substances 0.000 abstract 1
- 230000035755 proliferation Effects 0.000 abstract 1
- 206010039073 rheumatoid arthritis Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/10—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- 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
- A61K31/50—Pyridazines; Hydrogenated pyridazines
- A61K31/502—Pyridazines; Hydrogenated pyridazines ortho- or peri-condensed with carbocyclic ring systems, e.g. cinnoline, phthalazine
-
- A—HUMAN NECESSITIES
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- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- 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
- C07D413/10—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 aromatic rings
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Immunology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Physical Education & Sports Medicine (AREA)
- Pulmonology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Dermatology (AREA)
- Urology & Nephrology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Rheumatology (AREA)
- Oncology (AREA)
- Psychiatry (AREA)
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- Pain & Pain Management (AREA)
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Abstract
En esta solicitud se describen compuestos que se ajustan a la fórmula genérica I:en la que todas las variables tienen los significados aquí descritos, e inhiben la Btk. Los compuestos aquí descritos son útiles para modular la actividad de la Btk y tratar enfermedades asociadas con una actividad excesiva de la Btk. Los compuestos son útiles además para tratar enfermedades inflamatorias y autoinmunes asociadas con una proliferación aberrante de las células B, por ejemplo la artritis reumatoide. Se describen también composiciones que contienen los compuestos de la fórmula I y por lo menos un vehículo, diluyenteo excipiente.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161486809P | 2011-05-17 | 2011-05-17 | |
| US201261635470P | 2012-04-19 | 2012-04-19 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| ECSP13013025A true ECSP13013025A (es) | 2014-01-31 |
Family
ID=46124327
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ECSP13013025 ECSP13013025A (es) | 2011-05-17 | 2013-11-15 | Inhibidores de la tirosina-quinasa de bruton |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US8729078B2 (es) |
| EP (1) | EP2709997B1 (es) |
| JP (1) | JP5859640B2 (es) |
| KR (1) | KR101585753B1 (es) |
| CN (1) | CN103582637B (es) |
| AR (1) | AR086403A1 (es) |
| AU (1) | AU2012257802A1 (es) |
| BR (1) | BR112013029620A2 (es) |
| CA (1) | CA2834077A1 (es) |
| CO (1) | CO6852067A2 (es) |
| EC (1) | ECSP13013025A (es) |
| ES (1) | ES2590491T3 (es) |
| IL (1) | IL229197A0 (es) |
| MA (1) | MA35112B1 (es) |
| MX (1) | MX345170B (es) |
| PH (1) | PH12013502379A1 (es) |
| SG (1) | SG194728A1 (es) |
| TW (1) | TW201300374A (es) |
| WO (1) | WO2012156334A1 (es) |
| ZA (1) | ZA201308397B (es) |
Families Citing this family (40)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR082590A1 (es) * | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
| KR20140096100A (ko) | 2011-11-03 | 2014-08-04 | 에프. 호프만-라 로슈 아게 | 이환 피페라진 화합물 |
| RU2622391C2 (ru) | 2011-11-03 | 2017-06-15 | Ф. Хоффманн-Ля Рош Аг | Соединения 8-фторфталазин-1(2н)-она в качестве ингибиторов тирозинкиназы брутона |
| UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| BR112014010439A2 (pt) | 2011-11-03 | 2017-04-18 | F Hoffmann - La Roche Ag | compostos, composição farmacêutica, processo de produção, método de tratamento de uma doença ou distúrbio, métodos, kit e uso de uma composição farmacêutica |
| CA2879570A1 (en) | 2012-07-24 | 2014-01-30 | Pharmacyclics, Inc. | Mutations associated with resistance to inhibitors of bruton's tyrosine kinase (btk) |
| JP6348492B2 (ja) | 2012-08-10 | 2018-06-27 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ブルトン型チロシンキナーゼ(btk)阻害剤としてのヘテロ芳香族化合物 |
| MX2015006162A (es) * | 2012-11-16 | 2015-08-14 | Hoffmann La Roche | Inhibidores de la tirosina-cinasa de bruton. |
| CN104968346B (zh) * | 2012-11-30 | 2017-06-27 | 弗·哈夫曼-拉罗切有限公司 | 酪氨酸蛋白激酶抑制剂 |
| SG11201506764WA (en) | 2013-04-25 | 2015-09-29 | Beigene Ltd | Fused heterocyclic compounds as protein kinase inhibitors |
| CN104211703B (zh) * | 2013-05-30 | 2018-04-03 | 南京勇山生物科技有限公司 | 一类作为布鲁顿激酶抑制剂的稠杂环化合物 |
| CN105473573B (zh) | 2013-06-25 | 2018-03-16 | 百时美施贵宝公司 | 用作激酶抑制剂的咔唑甲酰胺化合物 |
| UY35625A (es) | 2013-06-25 | 2014-12-31 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa |
| WO2015000949A1 (en) | 2013-07-03 | 2015-01-08 | F. Hoffmann-La Roche Ag | Heteroaryl pyridone and aza-pyridone amide compounds |
| JP6623353B2 (ja) | 2013-09-13 | 2019-12-25 | ベイジーン スウィッツァーランド ゲーエムベーハー | 抗pd−1抗体並びにその治療及び診断のための使用 |
| EP3077384B1 (en) | 2013-12-05 | 2017-09-06 | F. Hoffmann-La Roche AG | Heteroaryl pyridone and aza-pyridone compounds with electrophilic functionality |
| CA2929747C (en) | 2013-12-13 | 2018-01-23 | F. Hoffmann-La Roche Ag | Inhibitors of bruton's tyrosine kinase |
| KR20160127754A (ko) | 2014-03-12 | 2016-11-04 | 노파르티스 아게 | Btk 억제제 및 akt 억제제를 포함하는 조합물 |
| KR102003754B1 (ko) | 2014-07-03 | 2019-07-25 | 베이진 엘티디 | Pd-l1 항체와 이를 이용한 치료 및 진단 |
| CN106922146B (zh) * | 2014-10-02 | 2020-05-26 | 豪夫迈·罗氏有限公司 | 用于治疗由布鲁顿酪氨酸激酶(btk)介导的疾病的吡唑甲酰胺化合物 |
| TN2017000158A1 (en) | 2014-10-24 | 2018-10-19 | Bristol Myers Squibb Co | Carbazole derivatives |
| PT3461821T (pt) | 2014-10-24 | 2020-08-05 | Bristol Myers Squibb Co | Compostos de indol carboxamida úteis como inibidores de quinase |
| CA2965516A1 (en) | 2014-10-24 | 2016-04-28 | Bristol-Myers Squibb Company | Tricyclic atropisomer compounds |
| EP3402789B1 (en) | 2016-01-13 | 2020-03-18 | Boehringer Ingelheim International Gmbh | Isoquinolones as btk inhibitors |
| JPWO2017169503A1 (ja) * | 2016-04-01 | 2019-02-14 | 国立大学法人千葉大学 | 含窒素芳香族アミドの製造方法、ピロール・イミダゾールポリアミドの製造方法、及び化合物 |
| NZ749997A (en) | 2016-07-05 | 2022-11-25 | Beigene Ltd | Combination of a pd-l antagonist and a raf inhibitor for treating cancer |
| KR102604975B1 (ko) | 2016-08-16 | 2023-11-24 | 베이진 스위찰랜드 게엠베하 | (s)-7-(1-아크릴로일피페리딘-4-일)-2-(4-페녹시페닐)-4,5,6,7-테트라-하이드로피라졸로 [1,5-a] 피리미딘-3-카르복스아미드의 제조 및 그 용도 |
| EP3500299B1 (en) | 2016-08-19 | 2023-12-13 | BeiGene Switzerland GmbH | Combination of zanubrutinib with an anti-cd20 or an anti-pd-1 antibody for use in treating cancer |
| JP2019529419A (ja) | 2016-09-19 | 2019-10-17 | エムイーアイ ファーマ,インク. | 併用療法 |
| WO2018137681A1 (en) | 2017-01-25 | 2018-08-02 | Beigene, Ltd. | Crystalline forms of (s) -7- (1- (but-2-ynoyl) piperidin-4-yl) -2- (4-phenoxyphenyl) -4, 5, 6, 7-tetrahy dropyrazolo [1, 5-a] pyrimidine-3-carboxamide, preparation, and uses thereof |
| WO2018149284A1 (zh) * | 2017-02-16 | 2018-08-23 | 四川科伦博泰生物医药股份有限公司 | 激酶抑制剂及其制备方法和用途 |
| KR102757960B1 (ko) | 2017-06-26 | 2025-01-22 | 베이진 엘티디 | 간세포암(hepatocellular carcinoma: HCC)에 대한 면역 치료 |
| CN110997677A (zh) | 2017-08-12 | 2020-04-10 | 百济神州有限公司 | 具有改进的双重选择性的Btk抑制剂 |
| WO2019108795A1 (en) | 2017-11-29 | 2019-06-06 | Beigene Switzerland Gmbh | Treatment of indolent or aggressive b-cell lymphomas using a combination comprising btk inhibitors |
| US20220249491A1 (en) | 2019-06-10 | 2022-08-11 | Beigene Switzerland Gmbh | Oral solid tablet comprising bruton's tyrosine kinase inhibitor and preparation method therefor |
| US20240100172A1 (en) | 2020-12-21 | 2024-03-28 | Hangzhou Jijing Pharmaceutical Technology Limited | Methods and compounds for targeted autophagy |
| US11926634B2 (en) * | 2022-02-01 | 2024-03-12 | Eli Lilly And Company | Processes for the preparation of selective estrogen receptor degraders |
| CN119156388A (zh) * | 2022-04-15 | 2024-12-17 | 海南先声再明医药股份有限公司 | 膜缔合酪氨酸和苏氨酸激酶抑制剂 |
| US11786531B1 (en) | 2022-06-08 | 2023-10-17 | Beigene Switzerland Gmbh | Methods of treating B-cell proliferative disorder |
| CN120379999A (zh) | 2022-11-30 | 2025-07-25 | 深圳众格生物科技有限公司 | 新型irak4抑制剂以及抑制并降解irak4蛋白的化合物及其制备方法和应用 |
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| US20050032869A1 (en) | 2003-07-08 | 2005-02-10 | Pharmacia Italia S.P.A. | Pyrazolyl-indole derivatives active as kinase inhibitors, process for their preparation and pharmaceutical compositions comprising them |
| WO2009098144A1 (en) | 2008-02-05 | 2009-08-13 | F. Hoffmann-La Roche Ag | Novel pyridinones and pyridazinones |
| WO2010006970A1 (en) * | 2008-07-18 | 2010-01-21 | F. Hoffmann-La Roche Ag | Novel phenylimidazopyrazines |
| BRPI0922565A2 (pt) * | 2008-12-19 | 2015-12-15 | Bristol Myers Squibb Co | compostos de carbazol carboxamida úteis como inibidores de cinase |
| US8299077B2 (en) | 2009-03-02 | 2012-10-30 | Roche Palo Alto Llc | Inhibitors of Bruton's tyrosine kinase |
| AR082590A1 (es) | 2010-08-12 | 2012-12-19 | Hoffmann La Roche | Inhibidores de la tirosina-quinasa de bruton |
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- 2012-05-14 WO PCT/EP2012/058845 patent/WO2012156334A1/en not_active Ceased
- 2012-05-14 CN CN201280023444.6A patent/CN103582637B/zh not_active Expired - Fee Related
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- 2012-05-14 SG SG2013080924A patent/SG194728A1/en unknown
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- 2012-05-14 JP JP2014510756A patent/JP5859640B2/ja not_active Expired - Fee Related
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- 2012-05-16 US US13/472,541 patent/US8729078B2/en not_active Expired - Fee Related
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- 2013-11-15 EC ECSP13013025 patent/ECSP13013025A/es unknown
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| CO6852067A2 (es) | 2014-01-30 |
| MX345170B (es) | 2017-01-19 |
| ES2590491T3 (es) | 2016-11-22 |
| HK1194381A1 (en) | 2014-10-17 |
| CN103582637B (zh) | 2015-08-12 |
| AU2012257802A1 (en) | 2013-10-31 |
| KR101585753B1 (ko) | 2016-01-14 |
| CA2834077A1 (en) | 2012-11-22 |
| EP2709997A1 (en) | 2014-03-26 |
| ZA201308397B (en) | 2014-07-30 |
| MA35112B1 (fr) | 2014-05-02 |
| CN103582637A (zh) | 2014-02-12 |
| TW201300374A (zh) | 2013-01-01 |
| KR20140025519A (ko) | 2014-03-04 |
| PH12013502379A1 (en) | 2014-01-13 |
| WO2012156334A1 (en) | 2012-11-22 |
| IL229197A0 (en) | 2014-01-30 |
| BR112013029620A2 (pt) | 2016-09-06 |
| US8729078B2 (en) | 2014-05-20 |
| US20120295885A1 (en) | 2012-11-22 |
| SG194728A1 (en) | 2013-12-30 |
| MX2013013267A (es) | 2014-06-23 |
| AR086403A1 (es) | 2013-12-11 |
| JP5859640B2 (ja) | 2016-02-10 |
| EP2709997B1 (en) | 2016-06-29 |
| JP2014520079A (ja) | 2014-08-21 |
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