CA2994472A1 - Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals - Google Patents
Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals Download PDFInfo
- Publication number
- CA2994472A1 CA2994472A1 CA2994472A CA2994472A CA2994472A1 CA 2994472 A1 CA2994472 A1 CA 2994472A1 CA 2994472 A CA2994472 A CA 2994472A CA 2994472 A CA2994472 A CA 2994472A CA 2994472 A1 CA2994472 A1 CA 2994472A1
- Authority
- CA
- Canada
- Prior art keywords
- compound
- alkyl
- cancer
- mmol
- group
- 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.)
- Abandoned
Links
Classifications
-
- 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
- C07D401/02—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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- A61K31/47—Quinolines; Isoquinolines
- A61K31/472—Non-condensed isoquinolines, e.g. papaverine
- A61K31/4725—Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P17/00—Drugs for dermatological disorders
- A61P17/06—Antipsoriatics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/02—Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
-
- 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
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P37/00—Drugs for immunological or allergic disorders
- A61P37/02—Immunomodulators
- A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
-
- 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
-
- 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
- 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
- C07D405/14—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 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- 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
- C07D417/14—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 three or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Immunology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Dermatology (AREA)
- Epidemiology (AREA)
- Transplantation (AREA)
- Physical Education & Sports Medicine (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201562203623P | 2015-08-11 | 2015-08-11 | |
| US62/203,623 | 2015-08-11 | ||
| US201662356579P | 2016-06-30 | 2016-06-30 | |
| US62/356,579 | 2016-06-30 | ||
| PCT/CA2016/050943 WO2017024408A1 (en) | 2015-08-11 | 2016-08-11 | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2994472A1 true CA2994472A1 (en) | 2017-02-16 |
Family
ID=57982883
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA2994472A Abandoned CA2994472A1 (en) | 2015-08-11 | 2016-08-11 | Aryl-substituted dihydroquinolinones, their preparation and their use as pharmaceuticals |
Country Status (11)
| Country | Link |
|---|---|
| US (2) | US10501438B2 (https=) |
| EP (1) | EP3334717B1 (https=) |
| JP (1) | JP2018527340A (https=) |
| KR (1) | KR20180039117A (https=) |
| CN (1) | CN108290856A (https=) |
| AU (1) | AU2016305513A1 (https=) |
| CA (1) | CA2994472A1 (https=) |
| HK (1) | HK1256753A1 (https=) |
| IL (1) | IL257347A (https=) |
| MX (1) | MX2018001751A (https=) |
| WO (1) | WO2017024408A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2020093162A1 (en) * | 2018-11-07 | 2020-05-14 | Neomed Institute | Treatment of bet inhibitor-resistant cancers and other diseases responsive to dual bet and cbp/ep300 inhibition therapy |
| BR112021017831A2 (pt) * | 2019-03-11 | 2021-11-30 | Collaborative Medicinal Dev Llc | Derivados heteroaromáticos e aromáticos heterobicíclicos para o tratamento de distúrbios relacionados com ferroptose |
| CN112239456B (zh) * | 2020-06-09 | 2021-09-07 | 浙江理工大学 | 一种取代2，3-二氢喹诺酮化合物的制备方法 |
| CN114276333B (zh) * | 2020-09-28 | 2023-05-09 | 中国科学院上海药物研究所 | 二氢喹喔啉类溴结构域二价抑制剂 |
| CN118005653B (zh) * | 2023-04-23 | 2024-12-10 | 信义核新(北京)生物科技有限公司 | 喹诺酮类似物及其用途 |
Family Cites Families (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4550166A (en) | 1984-05-21 | 1985-10-29 | American Cyanamid Company | (Pyridinyl)-1,2,4-triazolo[4,3-a]pyridines |
| US4785005A (en) * | 1986-06-25 | 1988-11-15 | Rorer Pharmaceutical Corporation | 6-(6-alkylpyridone)-carbostyril compounds and their cardiotonic uses |
| US5093330A (en) | 1987-06-15 | 1992-03-03 | Ciba-Geigy Corporation | Staurosporine derivatives substituted at methylamino nitrogen |
| DE4237656A1 (de) | 1992-06-13 | 1993-12-16 | Merck Patent Gmbh | Benzimidazolderivate |
| US6465484B1 (en) | 1997-09-26 | 2002-10-15 | Merck & Co., Inc. | Angiogenesis inhibitors |
| US6162804A (en) | 1997-09-26 | 2000-12-19 | Merck & Co., Inc. | Tyrosine kinase inhibitors |
| CA2341409A1 (en) | 1998-08-31 | 2000-03-09 | Merck And Co., Inc. | Novel angiogenesis inhibitors |
| MY139563A (en) | 2002-09-04 | 2009-10-30 | Bristol Myers Squibb Co | Heterocyclic aromatic compounds useful as growth hormone secretagogues |
| BRPI0417674A (pt) | 2003-12-18 | 2007-03-20 | Pfizer Prod Inc | método para tratar a inflamação aguda em animais, com inibidores de quinase map p38 |
| ES2328047T3 (es) | 2004-03-19 | 2009-11-06 | Warner-Lambert Company Llc | Derivados de imidazopiridina e imidazopirimidina como agentes antibacterianos. |
| PE20080403A1 (es) | 2006-07-14 | 2008-04-25 | Amgen Inc | Derivados heterociclicos fusionados y metodos de uso |
| HRP20150642T1 (hr) | 2006-12-22 | 2015-08-14 | Astex Therapeutics Limited | BICIKLIÄŚKE HETEROCIKLIÄŚKE TVARI KAO INHIBITORI FGFR-a |
| US8119658B2 (en) | 2007-10-01 | 2012-02-21 | Bristol-Myers Squibb Company | Triazolopyridine 11-beta hydroxysteroid dehydrogenase type I inhibitors |
| AR068877A1 (es) | 2007-10-17 | 2009-12-09 | Novartis Ag | Derivados heterociclicos de imidazol |
| MY153913A (en) | 2009-05-12 | 2015-04-15 | Janssen Pharmaceuticals Inc | 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
| GB0919423D0 (en) | 2009-11-05 | 2009-12-23 | Glaxosmithkline Llc | Novel compounds |
| WO2011060235A1 (en) | 2009-11-16 | 2011-05-19 | Schering Corporation | Imidazole derivatives and methods of use thereof |
| UA112425C2 (uk) | 2010-12-13 | 2016-09-12 | Еррей Біофарма Інк. | ЗАМІЩЕНІ N-(1H-ІНДАЗОЛ-4-ІЛ)ІМІДАЗО[1,2-a]ПІРИДИН-3-КАРБОКСАМІДНІ СПОЛУКИ ЯК ІНГІБІТОРИ РЕЦЕПТОРНОЇ ТИРОЗИНКІНАЗИ ІІІ ТИПУ |
| GB201114103D0 (en) | 2011-08-17 | 2011-09-28 | Glaxosmithkline Llc | Novel compounds |
| MX2014002542A (es) | 2011-08-29 | 2014-07-09 | Infinity Pharmaceuticals Inc | Compuestos heterociclicos y usos de los mismos. |
| BR112014030940B1 (pt) | 2012-06-11 | 2022-09-06 | UCB Biopharma SRL | Benzimidazóis que modulam tnf-alfa e composição farmacêutica compreendendo os mesmos |
| AU2012382373A1 (en) | 2012-06-12 | 2014-12-11 | Abbvie Inc. | Pyridinone and pyridazinone derivatives |
| JP6430383B2 (ja) | 2012-09-28 | 2018-11-28 | ヴァンダービルト ユニバーシティーＶａｎｄｅｒｂｉｌｔ Ｕｎｉｖｅｒｓｉｔｙ | 選択的ｂｍｐ阻害剤としての縮合複素環化合物 |
| US20140094456A1 (en) | 2012-10-02 | 2014-04-03 | Intermune, Inc. | Anti-fibrotic pyridinones |
| AR092742A1 (es) | 2012-10-02 | 2015-04-29 | Intermune Inc | Piridinonas antifibroticas |
| CN105229002A (zh) * | 2012-12-20 | 2016-01-06 | 拜耳医药股份有限公司 | 抑制bet蛋白的二氢吡啶并吡嗪酮 |
| JP2016507496A (ja) | 2012-12-21 | 2016-03-10 | ゼニス・エピジェネティクス・コーポレイションＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｃｏｒｐ． | ブロモドメイン阻害剤としての新規複素環式化合物 |
| WO2014128655A1 (en) | 2013-02-25 | 2014-08-28 | Aurigene Discovery Technologies Limited | Substituted imidazo[4,5-c]quinoline derivatives as bromodomain inhibitors |
| EA201591746A1 (ru) | 2013-03-14 | 2016-08-31 | КОНВЕРДЖЕН ЭлЭлСи | Способы и композиции для ингибирования бромодомен-содержащих белков |
| DK2970265T3 (en) | 2013-03-15 | 2018-10-01 | Plexxikon Inc | HETEROCYCLIC COMPOUNDS AND APPLICATIONS THEREOF |
| CA2904364A1 (en) | 2013-03-15 | 2014-09-25 | Epigenetix, Inc. | Oxazolo[5,4-c]quinolin-2-one compounds as bromodomain inhibitors |
| US8975417B2 (en) | 2013-05-27 | 2015-03-10 | Novartis Ag | Pyrazolopyrrolidine derivatives and their use in the treatment of disease |
| JP6461118B2 (ja) | 2013-06-21 | 2019-01-30 | ゼニス・エピジェネティクス・リミテッドＺｅｎｉｔｈ Ｅｐｉｇｅｎｅｔｉｃｓ Ｌｔｄ． | ブロモドメイン阻害剤としての新規の置換された二環式化合物 |
| SI3010503T1 (sl) | 2013-06-21 | 2020-07-31 | Zenith Epigenetics Ltd. | Novi biciklični inhibitorji bromodomene |
| ES2635003T3 (es) | 2013-07-09 | 2017-10-02 | Bayer Pharma Aktiengesellschaft | Dihidroquinoxalinonas y dihidropiridopirazinonas modificadas inhibidoras de proteína BET |
| US20150051208A1 (en) | 2013-08-14 | 2015-02-19 | Boehringer Ingelheim International Gmbh | Pyridinones |
| WO2015049629A1 (en) | 2013-10-01 | 2015-04-09 | Piramal Enterprises Limited | Imidazoquinoline compounds as bromodomain inhibitors |
| WO2015081189A1 (en) | 2013-11-26 | 2015-06-04 | Incyte Corporation | Bicyclic heterocycles as bet protein inhibitors |
| US9399640B2 (en) | 2013-11-26 | 2016-07-26 | Incyte Corporation | Substituted pyrrolo[2,3-c]pyridines and pyrazolo[3,4-c]pyridines as BET protein inhibitors |
| GB201321729D0 (en) | 2013-12-09 | 2014-01-22 | Ucb Pharma Sa | Therapeutic agents |
| EP3089970B1 (en) | 2013-12-09 | 2018-10-17 | AbbVie Inc. | Dihydropyridinone and dihydropyridazinone derivatives useful as bromodomain inhibitors |
| HUE041546T2 (hu) | 2014-01-09 | 2019-05-28 | Orion Corp | Biciklusos heterociklusos származékvegyületek mint bromo doméninhibitorok |
| MX382781B (es) * | 2014-04-02 | 2025-03-13 | Intermune Inc | Piridinonas anti-fibroticas. |
| PL3134403T3 (pl) | 2014-04-23 | 2020-07-13 | Incyte Corporation | 1H-pirolo[2,3-c]pirydyn-7(6H)-ony i pirazolo[3,4-c]pirydyn-7(6H)-ony jako inhibitory białek BET |
| WO2016077656A2 (en) | 2014-11-13 | 2016-05-19 | Convergene Llc | Methods and compositions for inhibition of bromodomain and extraterminal proteins |
| US10710992B2 (en) | 2014-12-01 | 2020-07-14 | Zenith Epigenetics Ltd. | Substituted pyridinones as bromodomain inhibitors |
| WO2016097870A1 (en) | 2014-12-17 | 2016-06-23 | Zenith Epigenetics Corp. | Substituted bicyclic compounds as bromodomain inhibitors |
| CA2966450A1 (en) | 2014-12-17 | 2016-06-23 | Olesya KHARENKO | Inhibitors of bromodomains |
| GB201503720D0 (en) | 2015-03-05 | 2015-04-22 | Glaxosmithkline Ip No 2 Ltd | Chemical compound |
| GB201504689D0 (en) | 2015-03-19 | 2015-05-06 | Glaxosmithkline Ip Dev Ltd | Chemical compounds |
| AR104259A1 (es) | 2015-04-15 | 2017-07-05 | Celgene Quanticel Res Inc | Inhibidores de bromodominio |
| GB201506658D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| GB201506660D0 (en) | 2015-04-20 | 2015-06-03 | Cellcentric Ltd | Pharmaceutical compounds |
| US10501459B2 (en) | 2015-10-21 | 2019-12-10 | Neomed Institute | Substituted imidazo[1,2-a]pyridines as bromodomain inhibitors |
-
2016
- 2016-08-11 JP JP2018506998A patent/JP2018527340A/ja active Pending
- 2016-08-11 AU AU2016305513A patent/AU2016305513A1/en not_active Abandoned
- 2016-08-11 HK HK18115833.9A patent/HK1256753A1/zh unknown
- 2016-08-11 WO PCT/CA2016/050943 patent/WO2017024408A1/en not_active Ceased
- 2016-08-11 KR KR1020187006580A patent/KR20180039117A/ko not_active Withdrawn
- 2016-08-11 EP EP16834368.9A patent/EP3334717B1/en active Active
- 2016-08-11 CA CA2994472A patent/CA2994472A1/en not_active Abandoned
- 2016-08-11 US US15/751,800 patent/US10501438B2/en active Active
- 2016-08-11 MX MX2018001751A patent/MX2018001751A/es unknown
- 2016-08-11 CN CN201680058648.1A patent/CN108290856A/zh active Pending
-
2018
- 2018-02-04 IL IL257347A patent/IL257347A/en unknown
-
2019
- 2019-10-28 US US16/665,198 patent/US20200299262A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2017024408A1 (en) | 2017-02-16 |
| EP3334717A4 (en) | 2019-02-13 |
| KR20180039117A (ko) | 2018-04-17 |
| AU2016305513A1 (en) | 2018-03-08 |
| CN108290856A (zh) | 2018-07-17 |
| US20200299262A1 (en) | 2020-09-24 |
| JP2018527340A (ja) | 2018-09-20 |
| EP3334717B1 (en) | 2020-07-01 |
| HK1256753A1 (zh) | 2019-10-04 |
| IL257347A (en) | 2018-03-29 |
| US10501438B2 (en) | 2019-12-10 |
| US20180230130A1 (en) | 2018-08-16 |
| MX2018001751A (es) | 2018-08-01 |
| EP3334717A1 (en) | 2018-06-20 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |
Effective date: 20221101 |