JOP20190230A1 - طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به - Google Patents

طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به

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Publication number
JOP20190230A1
JOP20190230A1 JOP/2019/0230A JOP20190230A JOP20190230A1 JO P20190230 A1 JOP20190230 A1 JO P20190230A1 JO P20190230 A JOP20190230 A JO P20190230A JO P20190230 A1 JOP20190230 A1 JO P20190230A1
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JO
Jordan
Prior art keywords
processes
intermediate compounds
jak inhibitors
related intermediate
preparing
Prior art date
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JOP/2019/0230A
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English (en)
Inventor
Qiyan Lin
Haisheng Wang
James D Rodgers
Tai-Yuen Yue
Jiacheng Zhou
Brian W Metcalf
David Meloni
Michael Xia
Mei Li
Yongchun Pan
Pingli Liu
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Incyte Corp
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Publication of JOP20190230A1 publication Critical patent/JOP20190230A1/ar

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    • 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
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    • C07D487/04Ortho-condensed systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
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    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
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    • C07D239/24Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
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    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
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    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

يتعلق الاكتشاف الحالي بطرق لتحضير بايريمدينات [2,3-d] بايرولو بايرازوليل مستبدلة الجزيئات غير منطبقة مرآويا خاصة بالصيغة III والمركبات الوسيطة التوليفية الصناعية المتعلقة بها. البايريمدينات [2,3-d] بايرولو بايرازوليل مستبدلة الجزيئات غير المنطبقة مرآويا مفيدة كمثبطات لعائلة مستقبِل كاينيز جانوس لبروتين كاينيز تايروزين لمعالجة الامراض الالتهابية واضطرابات التشعب النخاعي العظمي وغير ذلك من الامراض.
JOP/2019/0230A 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به JOP20190230A1 (ar)

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US14499109P 2009-01-15 2009-01-15

Publications (1)

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JOP20190230A1 true JOP20190230A1 (ar) 2017-06-16

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ID=42026219

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JOP/2019/0231A JOP20190231A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JOP/2019/0230A JOP20190230A1 (ar) 2009-01-15 2009-01-15 طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
JOP/2010/0010A JO3441B1 (ar) 2009-01-15 2010-01-14 طرق لاصلاح مثبطات انزيم jak والمركبات الوسيطة المتعلقة به

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Country Status (29)

Country Link
US (9) US8410265B2 (ar)
EP (2) EP2398774B1 (ar)
JP (6) JP5650662B2 (ar)
KR (7) KR102422043B1 (ar)
CN (4) CN108395433A (ar)
AR (2) AR082747A1 (ar)
AU (4) AU2010204772B2 (ar)
BR (3) BR122020005540B8 (ar)
CA (2) CA2749483C (ar)
CL (3) CL2011001668A1 (ar)
CO (1) CO6400137A2 (ar)
EA (3) EA034207B1 (ar)
EC (1) ECSP11011268A (ar)
ES (1) ES2641761T3 (ar)
IL (7) IL214061A (ar)
JO (3) JOP20190231A1 (ar)
MA (1) MA33038B1 (ar)
MX (5) MX357874B (ar)
MY (3) MY182004A (ar)
NZ (5) NZ706894A (ar)
PE (4) PE20110858A1 (ar)
PH (1) PH12016502060B1 (ar)
PL (1) PL2398774T3 (ar)
PT (1) PT2398774T (ar)
SG (3) SG172468A1 (ar)
TN (1) TN2011000329A1 (ar)
TW (7) TWI644915B (ar)
WO (1) WO2010083283A2 (ar)
ZA (1) ZA201104909B (ar)

Families Citing this family (125)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005105814A1 (en) * 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
KR101391900B1 (ko) 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘
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.
KR101549876B1 (ko) 2007-06-13 2015-09-03 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
BRPI0820544A2 (pt) * 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
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.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
ES2487542T3 (es) * 2009-05-22 2014-08-21 Incyte Corporation 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 cinasas Janus
NZ596374A (en) * 2009-05-22 2014-01-31 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
US9249145B2 (en) * 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN102596960B (zh) 2009-10-09 2016-01-20 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CA2790070C (en) * 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
SI3050882T1 (en) 2010-03-10 2018-06-29 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives, as inhibitors of JAK1
CN102985424B (zh) 2010-04-14 2015-03-11 阵列生物制药公司 5,7-取代的-咪唑并[1,2-c]嘧啶
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Jak抑制劑的局部製劑
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
US8754114B2 (en) 2010-12-22 2014-06-17 Incyte Corporation Substituted imidazopyridazines and benzimidazoles as inhibitors of FGFR3
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
CN102690281A (zh) * 2011-03-22 2012-09-26 上海药明康德新药开发有限公司 1-甲基4-吡唑频哪醇酯的合成方法
ES2560611T3 (es) 2011-06-20 2016-02-22 Incyte Holdings Corporation Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
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
WO2013157021A1 (en) 2012-04-20 2013-10-24 Advinus Therapeutics Limited Bicyclic compounds, compositions and medicinal applications thereof
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
AU2013287176C1 (en) 2012-06-13 2023-01-19 Incyte Holdings Corporation Substituted tricyclic compounds as FGFR inhibitors
DK3450434T3 (da) 2012-06-15 2021-05-03 Concert Pharmaceuticals Inc Deutererede derivater af ruxolitinib
WO2014011540A1 (en) 2012-07-09 2014-01-16 Emory University Bone morphogenetic protein pathway activation, compositions for ossification, and methods related thereto
US9388185B2 (en) 2012-08-10 2016-07-12 Incyte Holdings Corporation Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors
AU2013302519B2 (en) 2012-08-17 2017-11-02 Concert Pharmaceuticals, Inc. Deuterated baricitinib
WO2014060381A1 (de) 2012-10-18 2014-04-24 Bayer Cropscience Ag Heterocyclische verbindungen als schädlingsbekämpfungsmittel
JP2016503395A (ja) 2012-10-31 2016-02-04 バイエル・クロップサイエンス・アクチェンゲゼルシャフト 病害生物防除剤としての複素環化合物
AR093308A1 (es) 2012-11-01 2015-05-27 Incyte Corp Derivados triciclicos fusionados de tiofeno como inhibidores de jak
UA120834C2 (uk) 2012-11-15 2020-02-25 Інсайт Холдінгс Корпорейшн Лікарські форми руксолітинібу зі сповільненим вивільненням
US9266892B2 (en) 2012-12-19 2016-02-23 Incyte Holdings Corporation Fused pyrazoles as FGFR inhibitors
CA3091179C (en) 2013-03-06 2023-01-17 Incyte Holdings Corporation Processes and intermediates for making a jak inhibitor
UA120087C2 (uk) 2013-04-19 2019-10-10 Інсайт Холдинґс Корпорейшн Біциклічні гетероцикли як інгібітори fgfr
UA117830C2 (uk) 2013-05-17 2018-10-10 Інсайт Корпорейшн Похідні біпіразолу як інгібітори jak
CN105579032A (zh) 2013-08-07 2016-05-11 因赛特公司 Jak1抑制剂的持续释放剂型
CN103601749B (zh) * 2013-11-26 2016-04-27 大连联化化学有限公司 一种1-烷基吡唑-4-硼酸频哪醇酯的合成方法
CN104860950A (zh) * 2014-02-24 2015-08-26 重庆医药工业研究院有限责任公司 一种制备4-氯吡咯[2,3-d]并嘧啶的方法
US10064866B2 (en) 2014-04-08 2018-09-04 Incyte Corporation Treatment of B-cell malignancies by a combination JAK and PI3K inhibitors
CA2947418A1 (en) 2014-04-30 2015-11-05 Incyte Corporation Processes of preparing a jak1 inhibitor and new forms thereto
US9498467B2 (en) 2014-05-30 2016-11-22 Incyte Corporation Treatment of chronic neutrophilic leukemia (CNL) and atypical chronic myeloid leukemia (aCML) by inhibitors of JAK1
CN105218548A (zh) * 2014-06-09 2016-01-06 上海海和药物研究开发有限公司 一种新型杂环化合物及其制备方法和作为激酶抑制剂的用途
TW201618773A (zh) 2014-08-11 2016-06-01 艾森塔製藥公司 Btk抑制劑、pi3k抑制劑、jak-2抑制劑、及/或cdk4/6抑制劑的治療組合物
PT3179992T (pt) 2014-08-11 2022-07-12 Acerta Pharma Bv Combinações terapêuticas de um inibidor de btk, um inibidor de pd-1 e/ou um inibidor de pd-l1
SI3179991T1 (sl) 2014-08-11 2022-04-29 Acerta Pharma B.V. Terapevtske kombinacije zaviralca BTK in zaviralca BCL-2
WO2016035014A1 (en) * 2014-09-01 2016-03-10 Sun Pharmaceutical Industries Limited Processes for the preparation of ruxolitinib phosphate
US10851105B2 (en) 2014-10-22 2020-12-01 Incyte Corporation Bicyclic heterocycles as FGFR4 inhibitors
CZ2014773A3 (cs) 2014-11-10 2016-05-18 Zentiva, K.S. Soli (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu
CN104496904B (zh) * 2014-11-28 2017-01-11 上海北卡医药技术有限公司 一种鲁索利替尼中间体的合成方法
US9873706B2 (en) 2014-12-05 2018-01-23 Sun Pharmaceutical Industries Limited Process for the preparation of baricitinib and an intermediate thereof
WO2016134294A1 (en) 2015-02-20 2016-08-25 Incyte Corporation Bicyclic heterocycles as fgfr4 inhibitors
ES2751669T3 (es) 2015-02-20 2020-04-01 Incyte Corp Heterociclos bicíclicos como inhibidores FGFR
MA41551A (fr) 2015-02-20 2017-12-26 Incyte Corp Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4
CZ2015496A3 (cs) 2015-07-14 2017-01-25 Zentiva, K.S. Krystalické formy solí (3R)-3-cyklopentyl-3-[4-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrazol-1-yl]propannitrilu a jejich příprava
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
HU230805B1 (hu) * 2015-12-23 2018-06-28 Egis Gyógyszergyár Zrt Eljárás és köztitermék baricitinib előállítására
CN108699063B (zh) * 2015-12-31 2020-06-26 正大天晴药业集团股份有限公司 一种芦可替尼的合成工艺
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
ES2877200T3 (es) * 2016-01-26 2021-11-16 Hangzhou Bangshun Pharmaceutical Co Ltd Derivado azacíclico de cinco miembros de pirrolopirimidina y aplicación del mismo
CN107226814A (zh) * 2016-03-23 2017-10-03 罗欣生物科技(上海)有限公司 一种巴瑞克替尼中间体的制备方法
MX2018013347A (es) 2016-05-04 2019-09-02 Concert Pharmaceuticals Inc Tratamiento de trastornos de pérdida de cabello con inhibidores de cinasas asociadas a janus (jak) deuterados.
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
CN106188116B (zh) * 2016-07-14 2018-02-06 沧州普瑞东方科技有限公司 一种合成吡唑‑4‑硼酸频那醇酯的方法
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
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
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
AR111960A1 (es) 2017-05-26 2019-09-04 Incyte Corp Formas cristalinas de un inhibidor de fgfr y procesos para su preparación
CN107501154B (zh) * 2017-09-13 2020-02-11 浙江普洛康裕制药有限公司 (s)-1-(2-氯乙酰基)吡咯烷-2-甲腈的合成方法
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
WO2019113487A1 (en) 2017-12-08 2019-06-13 Incyte Corporation Low dose combination therapy for treatment of myeloproliferative neoplasms
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
MA51771B1 (fr) 2018-01-30 2022-03-31 Incyte Corp Procédés de préparation de (1-(3-fluoro-2-(trifluorométhyl)isonicotinyl)pipéridine-4-one)
US11103510B2 (en) 2018-02-16 2021-08-31 Incyte Corporation JAK1 pathway inhibitors for the treatment of cytokine-related disorders
EP3775284A1 (en) 2018-03-30 2021-02-17 Incyte Corporation Biomarkers for inflammatory skin disease
SG11202009441PA (en) 2018-03-30 2020-10-29 Incyte Corp Treatment of hidradenitis suppurativa using jak inhibitors
WO2019200030A1 (en) 2018-04-13 2019-10-17 Incyte Corporation Biomarkers for graft-versus-host disease
CA3099116A1 (en) 2018-05-04 2019-11-07 Incyte Corporation Salts of an fgfr inhibitor
JP2021523121A (ja) 2018-05-04 2021-09-02 インサイト・コーポレイションIncyte Corporation Fgfr阻害剤の固体形態及びその調製プロセス
EP3829543A1 (en) 2018-07-31 2021-06-09 Loxo Oncology, Inc. Spray-dried dispersions and formulations of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoro propan-2-yl)-1h-pyrazole-4-carboxamide
WO2020072870A1 (en) 2018-10-05 2020-04-09 Johnson Matthey Public Limited Company Co-crystal forms of baricitinib
SG11202104321PA (en) 2018-10-31 2021-05-28 Incyte Corp Combination therapy for treatment of hematological diseases
US20220081438A1 (en) 2018-12-19 2022-03-17 Array Biopharma Inc. Substituted pyrazolo[1,5-a]pyridine compounds as inhibitors of fgfr tyrosine kinases
US20220041579A1 (en) 2018-12-19 2022-02-10 Array Biopharma Inc. Substituted quinoxaline compounds as inhibitors of fgfr tyrosine kinases
US20220306636A1 (en) * 2019-02-06 2022-09-29 Concert Pharmaceuticals, Inc. Process for preparing enantiomerically enriched jak inhibitors
US11628162B2 (en) 2019-03-08 2023-04-18 Incyte Corporation Methods of treating cancer with an FGFR inhibitor
JP2022526713A (ja) 2019-03-21 2022-05-26 オンクセオ がんの処置のための、キナーゼ阻害剤と組み合わせたDbait分子
CN110028509B (zh) * 2019-05-27 2020-10-09 上海勋和医药科技有限公司 作为选择性jak2抑制剂的吡咯并嘧啶类化合物、其合成方法及用途
WO2021007269A1 (en) 2019-07-09 2021-01-14 Incyte Corporation Bicyclic heterocycles as fgfr inhibitors
CN110538183B (zh) * 2019-10-09 2021-05-04 吉林大学 一种预防和治疗小儿湿疹的组合物及其制备方法
CR20220169A (es) 2019-10-14 2022-10-27 Incyte Corp Heterociclos bicíclicos como inhibidores de fgfr
US11566028B2 (en) 2019-10-16 2023-01-31 Incyte Corporation Bicyclic heterocycles as FGFR inhibitors
CN114761006A (zh) 2019-11-08 2022-07-15 Inserm(法国国家健康医学研究院) 对激酶抑制剂产生耐药性的癌症的治疗方法
JP2023502742A (ja) 2019-11-22 2023-01-25 インサイト コーポレーション Alk2阻害剤及びjak2阻害剤を含む併用療法
BR112022010664A2 (pt) 2019-12-04 2022-08-16 Incyte Corp Derivados de um inibidor de fgfr
CA3163875A1 (en) 2019-12-04 2021-06-10 Incyte Corporation Tricyclic heterocycles as fgfr inhibitors
WO2021148581A1 (en) 2020-01-22 2021-07-29 Onxeo Novel dbait molecule and its use
WO2021236139A1 (en) 2020-05-21 2021-11-25 Concert Pharmaceuticals, Inc. Novel deuterated jak inhibitor and uses thereof
KR20230027086A (ko) 2020-06-02 2023-02-27 인사이트 코포레이션 Jak1 저해제의 제조 공정
US11833155B2 (en) 2020-06-03 2023-12-05 Incyte Corporation Combination therapy for treatment of myeloproliferative neoplasms
CN111790439B (zh) * 2020-07-29 2022-12-27 成都能特科技发展有限公司 一种手性二级胺二苯基膦芳甲酰胺双功能催化剂及其制备方法与应用
CN116348467A (zh) * 2020-08-12 2023-06-27 康塞特医药品有限公司 用于制备对映异构体富集的jak抑制剂的方法
JP2023539126A (ja) 2020-08-18 2023-09-13 インサイト・コーポレイション Jak阻害剤を調製するための方法及び中間体
EP4200278A1 (en) 2020-08-18 2023-06-28 Incyte Corporation Process and intermediates for preparing a jak1 inhibitor
AU2021372512A1 (en) 2020-10-28 2023-06-22 Sun Pharmaceutical Industries, Inc. Regimens for the treatment of hair loss disorders with deuterated jak inhibitors
CN112625030A (zh) * 2020-12-25 2021-04-09 杭州澳赛诺生物科技有限公司 一种一锅法合成n-保护3-溴代吡唑的合成方法
CN114907353A (zh) * 2021-02-09 2022-08-16 明慧医药(杭州)有限公司 一种前药化合物及其制备方法和用途
CN112876503B (zh) * 2021-03-18 2022-04-29 中国科学院兰州化学物理研究所 用于癌症硼中子俘获治疗药物的硼酸盐化合物及其制备
CN113264936B (zh) * 2021-05-25 2022-08-09 常州制药厂有限公司 一种jak抑制剂关键中间体及其制备方法
CN113292569A (zh) * 2021-05-25 2021-08-24 常州制药厂有限公司 一种jak抑制剂的制备方法
AR126102A1 (es) 2021-06-09 2023-09-13 Incyte Corp Heterociclos tricíclicos como inhibidores de fgfr
CA3226714A1 (en) * 2021-07-12 2023-01-19 Incyte Corporation Process and intermediates for preparing baricitinib
KR20240027732A (ko) * 2021-07-20 2024-03-04 코발 바이오파마 (상하이) 컴퍼니 리미티드 외용 항염증 결합 화합물 약물 및 그 제조 방법과 응용
WO2023018904A1 (en) 2021-08-11 2023-02-16 Concert Pharmaceuticals, Inc. Treatment of hair loss disorders with deuterated jak inhibitors
CA3228509A1 (en) 2021-08-12 2023-02-16 Sun Pharmaceutical Industries, Inc. Treatment of jak-inhibition-responsive disorders with prodrugs of jak inhibitors
WO2023042224A1 (en) * 2021-09-18 2023-03-23 Natco Pharma Limited An improved process for the preparation of ruxolitinib phosphate
CN114044777B (zh) * 2022-01-10 2022-04-19 南京佰麦生物技术有限公司 一种磷酸芦可替尼的制备方法
WO2023215520A1 (en) 2022-05-04 2023-11-09 Sun Pharmaceutical Industries, Inc. Dosage regimens for treatment with deuterated jak inhibitors
WO2023223253A1 (en) * 2022-05-19 2023-11-23 Glenmark Life Sciences Limited Process for preparation of ruxolitinib
CN114805368B (zh) * 2022-05-25 2023-12-01 山东诺明康药物研究院有限公司 一种芦克替尼的制备方法
CN115028638A (zh) * 2022-06-09 2022-09-09 安徽大学 一种鲁索替尼中间体的制备方法
CN117384163A (zh) * 2022-07-05 2024-01-12 盛世泰科生物医药技术(苏州)股份有限公司 一种含偕二氟基的化合物及其制备方法和用途

Family Cites Families (65)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US2985589A (en) 1957-05-22 1961-05-23 Universal Oil Prod Co Continuous sorption process employing fixed bed of sorbent and moving inlets and outlets
JPS5519438A (en) 1978-07-26 1980-02-12 Mitsubishi Electric Corp Brazing method
US4402832A (en) 1982-08-12 1983-09-06 Uop Inc. High efficiency continuous separation process
US4498991A (en) 1984-06-18 1985-02-12 Uop Inc. Serial flow continuous separation process
JP2513001B2 (ja) * 1988-11-01 1996-07-03 山川薬品工業株式会社 光学活性テトラヒドロフラン−2−カルボン酸のラセミ化方法
DE4038356A1 (de) * 1990-12-01 1992-06-04 Bayer Ag Verfahren zur racemisierung von optisch aktiven l-aryl-alkylaminen
JPH04308556A (ja) * 1991-04-05 1992-10-30 Hokuriku Seiyaku Co Ltd 光学活性なベンジルアルコール誘導体のラセミ化方法
JPH06122686A (ja) * 1992-10-12 1994-05-06 Fujisawa Pharmaceut Co Ltd ラセミ体の光学分割法
JPH07247286A (ja) * 1994-01-18 1995-09-26 Sankyo Co Ltd 含窒素環状化合物の光学分割方法
US5630943A (en) 1995-11-30 1997-05-20 Merck Patent Gesellschaft Mit Beschrankter Haftung Discontinuous countercurrent chromatographic process and apparatus
GB9602516D0 (en) 1996-02-08 1996-04-10 Chiroscience Ltd Racemisation
US6063284A (en) 1997-05-15 2000-05-16 Em Industries, Inc. Single column closed-loop recycling with periodic intra-profile injection
PA8474101A1 (es) 1998-06-19 2000-09-29 Pfizer Prod Inc Compuestos de pirrolo [2,3-d] pirimidina
US6413419B1 (en) 1998-10-29 2002-07-02 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic
US6375839B1 (en) 1998-10-29 2002-04-23 Institut Francais Du Petrole Process and device for separation with variable-length chromatographic zones
FR2785196B1 (fr) 1998-10-29 2000-12-15 Inst Francais Du Petrole Procede et dispositif de separation avec des zones chromatographiques a longueur variable
PT1235830E (pt) 1999-12-10 2004-04-30 Pfizer Prod Inc Compostos de pirrolo¬2,3-d|pirimidina como inibidores das proteina cinases
JP3753971B2 (ja) * 2000-11-17 2006-03-08 武田薬品工業株式会社 新規イミダゾール誘導体、その製造法および用途
KR20050004214A (ko) 2002-05-31 2005-01-12 에자이 가부시키가이샤 피라졸 화합물 및 이것을 포함하여 이루어지는 의약 조성물
ATE323702T1 (de) 2002-08-06 2006-05-15 Astrazeneca Ab Kondensierte pyridine und pyrimidine mit tie2 (tek) aktivität
JP2004143053A (ja) * 2002-10-22 2004-05-20 Senju Pharmaceut Co Ltd β−アミノヒドロキサム酸誘導体およびその用途
EP1988397B8 (en) * 2002-12-19 2012-02-15 The Scripps Research Institute Compositions and uses for stabilising transthyretin and inhibiting transthyretin misfolding
JP2005304368A (ja) * 2004-04-21 2005-11-04 Toyo Kasei Kogyo Co Ltd 光学活性な4−(n−保護アミノ)−1−アルケン−3−オールの製造方法、およびそれを用いた3−ベンザミド−2−ヒドロキシカルボン酸またはその塩の製造方法
WO2005105814A1 (en) 2004-04-28 2005-11-10 Incyte Corporation Tetracyclic inhibitors of janus kinases
NZ553267A (en) * 2004-07-27 2010-09-30 Sgx Pharmaceuticals Inc Pyrrolo-pyridine kinase modulators
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.
RU2434871C2 (ru) 2005-02-03 2011-11-27 Вертекс Фармасьютикалз Инкорпорейтед Пирролопиримидины, применимые в качестве ингибиторов протеинкиназы
EP2270014A1 (en) 2005-09-22 2011-01-05 Incyte Corporation Azepine inhibitors of janus kinases
EP1937664B1 (en) 2005-10-14 2011-06-15 Sumitomo Chemical Company, Limited Hydrazide compound and pesticidal use of the same
US20130137681A1 (en) 2005-12-13 2013-05-30 Incyte Corporation HETEROARYL SUBSTITUTED PYRROLO[2,3-b]PYRIDINES AND PYRROLO[2,3-b]PYRIMIDINES AS JANUS KINASE INHIBITORS
KR101391900B1 (ko) 2005-12-13 2014-05-02 인사이트 코포레이션 야누스 키나아제 억제제로서의 헤테로아릴 치환된 피롤로[2,3-b]피리딘 및 피롤로[2,3-b]피리미딘
KR100815432B1 (ko) * 2005-12-29 2008-03-20 엘아이지엔설팅주식회사 사업 재난 관리 시스템, 방법, 및 상기 방법을 실행시키기위한 컴퓨터 판독 가능한 프로그램을 기록한 매체
RU2008143361A (ru) * 2006-04-05 2010-05-10 Вертекс Фармасьютикалз Инкорпорейтед (Us) Деазапурины в качестве ингибиторов янус-киназ
DE102006016426A1 (de) * 2006-04-07 2007-10-11 Merck Patent Gmbh Neuartige Cyclobutyl-Verbindungen als Kinase-Inhibitoren
NL2000613C2 (nl) 2006-05-11 2007-11-20 Pfizer Prod Inc Triazoolpyrazinederivaten.
WO2008013622A2 (en) 2006-07-27 2008-01-31 E. I. Du Pont De Nemours And Company Fungicidal azocyclic amides
MY188335A (en) * 2006-11-22 2021-11-30 Incyte Holdings Corp Imidazotriazines and imidazopyrimidines as kinase inhibitors
AR064416A1 (es) 2006-12-21 2009-04-01 Cancer Rec Tech Ltd Derivados de purina, piridina y pirimidina condensadas con heterociclos, moduladores de pka y/o pkb, composiciones farmaceuticas que los contienen, y usos para el tratamiento de enfermedades hiperproliferativas.
JP5492565B2 (ja) 2006-12-22 2014-05-14 インサイト・コーポレイション Janusキナーゼ阻害剤としての置換複素環
KR20080062876A (ko) 2006-12-29 2008-07-03 주식회사 대웅제약 신규한 항진균성 트리아졸 유도체
GB0704932D0 (en) * 2007-03-14 2007-04-25 Astex Therapeutics Ltd Pharmaceutical compounds
AU2008237019A1 (en) * 2007-04-10 2008-10-16 Sgx Pharmaceuticals, Inc. Fused ring heterocycle kinase modulators
KR101549876B1 (ko) 2007-06-13 2015-09-03 인사이트 코포레이션 야누스 키나제 억제제(R)―3―(4―(7H―피롤로[2,3-d]피리미딘―4―일)―1H―피라졸―1―일)―3―사이클로펜틸프로판니트릴의 염
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.
TWI444379B (zh) * 2007-06-29 2014-07-11 Sunesis Pharmaceuticals Inc 有用於作為Raf激酶抑制劑之化合物
BRPI0820544A2 (pt) 2007-11-16 2015-06-16 Incyte Corp 4-pirazolil-n-arilpirimidin-2-aminas e pirazolil-n-heteroarilpirimidin-2-aminas como inibidores de janus cinase
EP2288610B8 (en) 2008-03-11 2016-10-12 Incyte Holdings Corporation Azetidine and cyclobutane derivatives as jak inhibitors
ES2429120T3 (es) * 2008-03-19 2013-11-13 Bial-Portela & Ca, S.A. Hidrogenación catalítica asimétrica
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.
JOP20190231A1 (ar) 2009-01-15 2017-06-16 Incyte Corp طرق لاصلاح مثبطات انزيم jak و المركبات الوسيطة المتعلقة به
IT1393787B1 (it) 2009-03-30 2012-05-08 Cps Color Equipment Spa Dispositivo di erogazione di prodotti fluidi e relativo procedimento di erogazione
ES2487542T3 (es) 2009-05-22 2014-08-21 Incyte Corporation 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 cinasas Janus
NZ596374A (en) 2009-05-22 2014-01-31 Incyte Corp 3-[4-(7h-pyrrolo[2,3-d]pyrimidin-4-yl)-1h-pyrazol-1-yl]octane- or heptane-nitrile as jak inhibitors
US9249145B2 (en) 2009-09-01 2016-02-02 Incyte Holdings Corporation Heterocyclic derivatives of pyrazol-4-yl-pyrrolo[2,3-d]pyrimidines as janus kinase inhibitors
CN102596960B (zh) 2009-10-09 2016-01-20 因西特控股公司 3-(4-(7H-吡咯并[2,3-d]嘧啶-4-基)-1H-吡唑-1-基)-3-环戊基丙腈的羟基衍生物、酮基衍生物和葡糖苷酸衍生物
CA2790070C (en) 2010-02-18 2018-03-06 Incyte Corporation Cyclobutane and methylcyclobutane derivatives as janus kinase inhibitors
SI3050882T1 (en) 2010-03-10 2018-06-29 Incyte Holdings Corporation Piperidin-4-yl azetidine derivatives, as inhibitors of JAK1
TWI499421B (zh) 2010-05-21 2015-09-11 Incyte Corp Jak抑制劑的局部製劑
PE20140146A1 (es) 2010-11-19 2014-02-06 Incyte Corp Derivados de pirrolopiridina y pirrolopirimidina sustituidos con ciclobutilo como inhibidores de jak
JP5917544B2 (ja) 2010-11-19 2016-05-18 インサイト・ホールディングス・コーポレイションIncyte Holdings Corporation Jak阻害剤としての複素環置換ピロロピリジンおよびピロロピリミジン
CN103732226B (zh) 2011-02-18 2016-01-06 诺瓦提斯药物公司 mTOR/JAK抑制剂组合疗法
ES2560611T3 (es) 2011-06-20 2016-02-22 Incyte Holdings Corporation Derivados de fenil de azetidinilo, carboxamida de piridilo o pirazinilo como inhibidores de JAK
EP2741747A1 (en) 2011-08-10 2014-06-18 Novartis Pharma AG JAK P13K/mTOR COMBINATION THERAPY
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

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