JP2024526762A - Jak阻害剤を調製するためのプロセス及び中間体 - Google Patents

Jak阻害剤を調製するためのプロセス及び中間体 Download PDF

Info

Publication number
JP2024526762A
JP2024526762A JP2024501966A JP2024501966A JP2024526762A JP 2024526762 A JP2024526762 A JP 2024526762A JP 2024501966 A JP2024501966 A JP 2024501966A JP 2024501966 A JP2024501966 A JP 2024501966A JP 2024526762 A JP2024526762 A JP 2024526762A
Authority
JP
Japan
Prior art keywords
compound
formula
salt
reaction
reacting
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.)
Pending
Application number
JP2024501966A
Other languages
English (en)
Japanese (ja)
Other versions
JP2024526762A5 (https=
Inventor
チョウ,ジアチェン
チェン,シリ
ジア,ジョンジアン
リウ,ピンリー
メローニ,デイビッド
パン,ヨンチュン
スー,ナイジン
シア,マイケル
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Incyte Corp
Original Assignee
Incyte Corp
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Incyte Corp filed Critical Incyte Corp
Publication of JP2024526762A publication Critical patent/JP2024526762A/ja
Publication of JP2024526762A5 publication Critical patent/JP2024526762A5/ja
Pending legal-status Critical Current

Links

Images

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
JP2024501966A 2021-07-12 2022-07-11 Jak阻害剤を調製するためのプロセス及び中間体 Pending JP2024526762A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US202163220752P 2021-07-12 2021-07-12
US63/220,752 2021-07-12
PCT/US2022/073599 WO2023288197A1 (en) 2021-07-12 2022-07-11 Process and intermediates for preparing baricitinib

Publications (2)

Publication Number Publication Date
JP2024526762A true JP2024526762A (ja) 2024-07-19
JP2024526762A5 JP2024526762A5 (https=) 2025-07-18

Family

ID=82748410

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2024501966A Pending JP2024526762A (ja) 2021-07-12 2022-07-11 Jak阻害剤を調製するためのプロセス及び中間体

Country Status (6)

Country Link
US (2) US12071439B2 (https=)
EP (1) EP4370504A1 (https=)
JP (1) JP2024526762A (https=)
CN (1) CN118317946A (https=)
CA (1) CA3226714A1 (https=)
WO (1) WO2023288197A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
CN117903032A (zh) * 2022-10-12 2024-04-19 重庆博腾制药科技股份有限公司 一种巴瑞替尼中间体的制备方法及制备巴瑞替尼的方法
CN121135621A (zh) * 2024-06-07 2025-12-16 上海长森药业有限公司 一种jak抑制剂的制备方法及其中间体

Family Cites Families (64)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB812366A (en) 1955-08-18 1959-04-22 Wellcome Found Improvements in and relating to derivatives of pyrimidine and the preparation thereof
US5102904A (en) 1989-12-08 1992-04-07 American Cyanamid Company N-oxygenated arylpyrrole insecticidal, acaricidal and nematicidal agents and use thereas
WO2004021979A2 (en) 2002-09-06 2004-03-18 Smithkline Beecham Corporation PYRROLO[2, 3-d]PYRIMIDINE-4-YL AND PURIN-6-YL UREA COMPOUNDS
JP4842929B2 (ja) 2004-05-27 2011-12-21 ファイザー・プロダクツ・インク 癌治療に有用なピロロピリミジン誘導体
AR054416A1 (es) 2004-12-22 2007-06-27 Incyte Corp Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas.
EP1913000B1 (en) 2005-07-29 2012-01-11 Pfizer Products Inc. Pyrrolo[2,3-d]pyrimidine derivatives; their intermediates and synthesis
SG10202003901UA (en) 2005-12-13 2020-05-28 Incyte Holdings Corp Heteroaryl substituted pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidines as janus kinase inhibitors
KR101450535B1 (ko) 2006-02-02 2014-10-14 밀레니엄 파머슈티컬스 인코퍼레이티드 E1 활성화 효소의 억제제
CL2008001709A1 (es) 2007-06-13 2008-11-03 Incyte Corp Compuestos derivados de pirrolo [2,3-b]pirimidina, moduladores de quinasas jak; composicion farmaceutica; y uso en el tratamiento de enfermedades tales como cancer, psoriasis, artritis reumatoide, entre otras.
KR20150036210A (ko) 2007-06-13 2015-04-07 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
WO2009016460A2 (en) 2007-08-01 2009-02-05 Pfizer Inc. Pyrazole compounds and their use as raf inhibitors
UA104849C2 (uk) 2007-11-16 2014-03-25 Інсайт Корпорейшн 4-піразоліл-n-арилпіримідин-2-аміни і 4-піразоліл-n-гетероарилпіримідин-2-аміни як інгібітори кіназ janus
HUE029767T2 (en) * 2008-03-11 2017-04-28 Incyte Holdings Corp JAK inhibitor azetidine and cyclobutane derivatives
CL2009001884A1 (es) 2008-10-02 2010-05-14 Incyte Holdings Corp Uso de 3-ciclopentil-3-[4-(7h-pirrolo[2,3-d]pirimidin-4-il)-1h-pirazol-1-il)propanonitrilo, inhibidor de janus quinasa, y uso de una composición que lo comprende para el tratamiento del ojo seco.
TWI720517B (zh) 2009-01-15 2021-03-01 美商英塞特公司 製造jak抑制劑之方法及相關中間化合物
JP2012523405A (ja) 2009-04-10 2012-10-04 ファイザー・インク 4,5−ジヒドロ−1h−ピラゾール化合物およびその薬学的使用
SI2432472T1 (sl) 2009-05-22 2019-11-29 Incyte Holdings Corp 3-(4-(7H-pirolo(2,3-d)pirimidin-4-il)-1H-pirazol-1-il)oktan- ali heptan-nitril kot inhibitorji JAK
AR076794A1 (es) 2009-05-22 2011-07-06 Incyte Corp Derivados de n-(hetero)aril-pirrolidina de pirazol-4-il-pirrolo [2,3-d]pirimidinas y pirrol-3-il-pirrolo [2,3-d ]pirimidinas como inhibidores de la quinasa janus y composiciones farmaceuticas que los contienen
TW201113285A (en) 2009-09-01 2011-04-16 Incyte Corp Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
EA021478B1 (ru) 2009-10-09 2015-06-30 Инсайт Корпорейшн ГИДРОКСИЛЬНЫЕ, КЕТО И ГЛЮКУРОНИДНЫЕ ПРОИЗВОДНЫЕ 3-(4-(7Н-ПИРРОЛО[2,3-d]ПИРИМИДИН-4-ИЛ)-1Н-ПИРАЗОЛ-1-ИЛ)-3-ЦИКЛОПЕНТИЛПРОПАННИТРИЛА
CN106220623A (zh) 2009-11-06 2016-12-14 普莱希科公司 用于激酶调节的化合物和方法及其适应症
ES2627911T3 (es) 2009-11-18 2017-08-01 Plexxikon, Inc. Derivados de N-[2-fluoro-3-(4-amino-7H-pirrolo[2,3-d]pirimidin-5-carbonil)-fenil]-4-bencenosulfonamida como moduladores de la proteína quinasa Raf para el tratamiento del cáncer
JP5858434B2 (ja) 2010-02-18 2016-02-10 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Janusキナーゼ阻害薬としてのシクロブタンおよびメチルシクロブタン誘導体
EP3354652B1 (en) 2010-03-10 2020-05-06 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives as jak1 inhibitors
TWI510487B (zh) 2010-04-21 2015-12-01 Plexxikon Inc 用於激酶調節的化合物和方法及其適應症
PE20130216A1 (es) 2010-05-21 2013-02-27 Incyte Corp Formulacion topica para un inhibidor de jak
US9034884B2 (en) 2010-11-19 2015-05-19 Incyte Corporation Heterocyclic-substituted pyrrolopyridines and pyrrolopyrimidines as JAK inhibitors
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
CN103797010B (zh) 2011-06-20 2016-02-24 因塞特控股公司 作为jak抑制剂的氮杂环丁烷基苯基、吡啶基或吡嗪基甲酰胺衍生物
AU2012295802B2 (en) 2011-08-12 2017-03-30 Nissan Chemical Industries, Ltd. Tricyclic heterocyclic compounds and JAK inhibitors
TW201313721A (zh) 2011-08-18 2013-04-01 Incyte Corp 作為jak抑制劑之環己基氮雜環丁烷衍生物
UA111854C2 (uk) 2011-09-07 2016-06-24 Інсайт Холдінгс Корпорейшн Способи і проміжні сполуки для отримання інгібіторів jak
TW201406761A (zh) 2012-05-18 2014-02-16 Incyte Corp 做爲jak抑制劑之哌啶基環丁基取代之吡咯并吡啶及吡咯并嘧啶衍生物
PH12020551186B1 (en) 2012-11-15 2024-03-20 Incyte Holdings Corp Sustained-release dosage forms of ruxolitinib
RS62867B1 (sr) 2013-03-06 2022-02-28 Incyte Holdings Corp Postupci i intermedijeri za dobijanje inhibitora jak
HUE033587T2 (hu) 2013-05-17 2017-12-28 Incyte Corp Bipirazol-származékok mint JAK inhibitorok
SMT202000315T1 (it) 2013-08-07 2020-07-08 Incyte Corp Forme di dosaggio a rilascio prolungato per un inibitore di jak1
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
EP3183252B1 (en) 2014-08-21 2021-05-12 ratiopharm GmbH Oxalate salt of ruxolitinib
EP3183253B1 (en) 2014-08-21 2018-06-27 ratiopharm GmbH Salt of (r)-3-(4-(7h-pyrrolo [2,3-d]pyrimidin-4-yl)-lh-pyrazol-l-yl)-3-cyclopentylpropanenitrile with benzenesulfonic acid
WO2016035014A1 (en) 2014-09-01 2016-03-10 Sun Pharmaceutical Industries Limited Processes for the preparation of ruxolitinib phosphate
WO2016063294A2 (en) 2014-10-20 2016-04-28 Msn Laboratories Private Limited Process for the preparation of (r)-3-(4-(7h-pyrrolo[2,3-d], pyrimidin-4-yl)-1 h-pyrazol-1-yl)-3-cyclopentylpropanenitrile phosphate and its polymorphs thereof
MX2017010844A (es) 2015-02-24 2017-12-07 Pfizer Derivados de nucleosidos sustituidos utiles como agentes anticancerosos.
CA2928286A1 (en) 2015-04-28 2016-10-28 Signa S.A. De C.V. Solid form of ruxolitinib phosphate
CN106397443A (zh) 2015-07-17 2017-02-15 浙江九洲药业股份有限公司 一种吡咯嘧啶类衍生物中间体的制备方法
CZ2015575A3 (cs) 2015-08-26 2017-03-08 Zentiva, K.S. Soli 5-fluoro-3-fenyl-2-[(1S)-1-(9H-purin-6-ylamino)propyl]quinazolin-4-onu a jejich příprava
EP3394080B1 (en) 2015-12-23 2023-06-07 The University Of British Columbia Lipid-linked prodrugs
US10562904B2 (en) 2015-12-31 2020-02-18 Chia Tai Tianqing Pharmaceutical Group Co., Ltd. Synthesis process of ruxolitinib
CZ201629A3 (cs) 2016-01-22 2017-08-02 Zentiva, K.S. Krystalické modifikace solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a způsoby jejich přípravy
CN107513069A (zh) 2016-06-16 2017-12-26 正大天晴药业集团股份有限公司 手性吡咯并嘧啶化合物的制备方法
IN201641026603A (https=) 2016-08-04 2018-02-09
CN107722012B (zh) 2016-08-11 2020-05-29 斯福瑞(南通)制药有限公司 制备4-氯-7H-吡咯并[2,3-d]嘧啶的方法
CN107759601B (zh) 2016-08-23 2020-09-11 苏州旺山旺水生物医药有限公司 一种jak抑制剂及其盐的制备方法
CN107759623B (zh) 2016-08-23 2020-08-14 苏州旺山旺水生物医药有限公司 Jak抑制剂的中间体及其制备方法
US20190263796A1 (en) 2016-09-23 2019-08-29 Cellipse Lim kinase inhibitors, pharmaceutical composition and method of use in limk-mediated diseases
CN109651424B (zh) 2017-10-11 2021-01-22 新发药业有限公司 一种7-保护基-4-(1-氢-吡唑-4-基)吡咯[2,3-d]嘧啶的合成方法
US10766900B2 (en) 2017-12-29 2020-09-08 Formosa Laboratories, Inc. Baricitinib intermediate, method for forming Baricitinib intermediate, and method for preparing Baricitinib or pharmaceutically acceptable salt thereof
SG11202007164UA (en) 2018-01-30 2020-08-28 Incyte Corp Processes for preparing (1 -(3-fluoro-2-(trifluoromethyl)isonicotinyl)piperidine-4-one)
CN112041303A (zh) 2018-05-21 2020-12-04 Pi工业有限公司 制备取代的杂环化合物的方法
AU2020219797B2 (en) 2019-02-06 2025-10-16 Sun Pharmaceutical Industries, Inc. Process for preparing enantiomerically enriched jak inhibitors
CN110724145A (zh) 2019-11-01 2020-01-24 廖文杰 一种医药中间体4-氯吡咯并嘧啶的合成方法
PE20231743A1 (es) 2020-08-18 2023-10-31 Incyte Corp Proceso e intermediarios para preparar un inhibidor de jak
IL300557A (en) 2020-08-18 2023-04-01 Incyte Corp Process and intermediates for preparing a JAK1 inhibitor
CN113480546A (zh) 2021-07-30 2021-10-08 江苏君若药业有限公司 巴瑞克替尼及其衍生物的制备

Also Published As

Publication number Publication date
US20230059389A1 (en) 2023-02-23
WO2023288197A1 (en) 2023-01-19
US12071439B2 (en) 2024-08-27
US20240368171A1 (en) 2024-11-07
CA3226714A1 (en) 2023-01-19
EP4370504A1 (en) 2024-05-22
CN118317946A (zh) 2024-07-09

Similar Documents

Publication Publication Date Title
JP7778135B2 (ja) Jak1阻害剤を調製するためのプロセス及び中間体
JP7802770B2 (ja) Jak阻害剤を調製するための方法及び中間体
JP6640297B2 (ja) Jak阻害剤の製造方法及びその中間体
JP2024526762A (ja) Jak阻害剤を調製するためのプロセス及び中間体
CN116761792A (zh) 用于制备jak抑制剂的方法和中间体
EP2444393A1 (en) Methods for producing cyclic benzamidine derivatives
CN115989226B (zh) 制备jak抑制剂的方法和中间体
TWI913303B (zh) 製備jak抑制劑之方法及中間體
EA049332B1 (ru) Способ и промежуточные соединения для получения ингибитора jak1
BR122025013614A2 (pt) Processo para preparar um inibidor de jak, seus intermediários e formas cristalinas
BR122025024131A2 (pt) Processo para preparar um inibidor de jak, seus intermediários e formas cristalinas

Legal Events

Date Code Title Description
A521 Request for written amendment filed

Free format text: JAPANESE INTERMEDIATE CODE: A523

Effective date: 20250710

A621 Written request for application examination

Free format text: JAPANESE INTERMEDIATE CODE: A621

Effective date: 20250710