TWI740843B - 用於抑制jak之化合物和方法 - Google Patents

用於抑制jak之化合物和方法 Download PDF

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Publication number
TWI740843B
TWI740843B TW105130891A TW105130891A TWI740843B TW I740843 B TWI740843 B TW I740843B TW 105130891 A TW105130891 A TW 105130891A TW 105130891 A TW105130891 A TW 105130891A TW I740843 B TWI740843 B TW I740843B
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Taiwan
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methyl
indol
methoxy
pyrazol
amino
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TW105130891A
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Chinese (zh)
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TW201730186A (zh
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阿尼卡 貝吉塔 瑪格里塔 亞斯崔德
麥格耐斯 K 尼爾森
奈爾 派翠克 葛民斯特
賽米爾 卡哇第卡
蘇啟彬
德東 吳
文章 楊
理查 道諾德 沃森諾
霍特 強 詹姆士 溫特
傑森 格瑞特 凱透
吐朵 葛雷酥
詹姆士 麥卡貝
里尼特 立思 魯斯頓
麥琳莎 瑪麗 韋斯班德
克勞迪歐 艾德莫多 查奇
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中國大陸商迪哲(江蘇)醫藥有限公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Vascular Medicine (AREA)
  • Rheumatology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
TW105130891A 2015-09-25 2016-09-23 用於抑制jak之化合物和方法 TWI740843B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562232629P 2015-09-25 2015-09-25
US62/232,629 2015-09-25

Publications (2)

Publication Number Publication Date
TW201730186A TW201730186A (zh) 2017-09-01
TWI740843B true TWI740843B (zh) 2021-10-01

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TW105130891A TWI740843B (zh) 2015-09-25 2016-09-23 用於抑制jak之化合物和方法

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US (5) US9714236B2 (https=)
EP (2) EP4219482A1 (https=)
JP (1) JP6767491B2 (https=)
KR (2) KR20250035597A (https=)
CN (4) CN111606893B (https=)
AR (1) AR106138A1 (https=)
AU (1) AU2016328764B2 (https=)
BR (1) BR112018005833B1 (https=)
CA (1) CA2995430C (https=)
DK (1) DK3353168T3 (https=)
ES (1) ES2956642T3 (https=)
MX (1) MX375724B (https=)
PT (1) PT3353168T (https=)
RU (1) RU2760359C2 (https=)
TW (1) TWI740843B (https=)
WO (1) WO2017050938A1 (https=)
ZA (1) ZA201800782B (https=)

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JP6767491B2 (ja) * 2015-09-25 2020-10-14 ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド Jakを阻害するための化合物及び方法
MX383920B (es) 2016-05-26 2025-03-14 Recurium Ip Holdings Llc Compuestos inhibidores de egfr.
ES2938648T3 (es) * 2017-01-17 2023-04-13 Astrazeneca Ab Inhibidores selectivos de JAK1
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
EP3823964A1 (en) * 2018-07-18 2021-05-26 Astrazeneca AB A xinafoate salt of a jak inhibiting compound
CA3113732C (en) * 2018-09-21 2023-07-11 Shanghai Ennovabio Pharmaceuticals Co., Ltd. Aromatic heterocyclic compound with kinase inhibitory activity
KR102195348B1 (ko) * 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
MX2021012749A (es) * 2019-04-19 2021-11-18 Dizal Jiangsu Pharmaceutical Co Ltd Inhibidor selectivo de la jak1 cinasa.
CN110627775B (zh) * 2019-10-24 2026-01-30 特科罗生物科技(成都)有限公司 一种小分子化合物
CN111961037B (zh) * 2020-09-17 2021-09-21 嘉兴特科罗生物科技有限公司 一种作为jak激酶抑制剂的药物化合物
WO2022111499A1 (zh) * 2020-11-26 2022-06-02 深圳铂立健医药有限公司 一种酰胺化合物、药物组合物及其应用
TW202246243A (zh) * 2021-02-26 2022-12-01 美商泰拉生物科學公司 胺基嘧啶化合物及其使用方法
MX2023010642A (es) 2021-03-11 2023-11-28 Janssen Pharmaceutica Nv Lorpucitinib para uso en el tratamiento de trastornos mediados por jak.
CN115260128B (zh) * 2022-09-21 2022-12-09 苏州凯瑞医药科技有限公司 一种新型jak抑制剂关键中间体的制备方法
WO2025230951A1 (en) * 2024-04-29 2025-11-06 Icahn School Of Medicine At Mount Sinai Method of treating adenoid cystic carcinoma

Citations (4)

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WO2010135650A1 (en) * 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
TW201107325A (en) * 2009-07-31 2011-03-01 Japan Tobacco Inc Nitrogen-containing spiro cyclic compounds and pharmaceutical use thereof
WO2012068450A1 (en) * 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012177606A1 (en) * 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

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ES2364340T3 (es) * 2004-03-30 2011-08-31 Vertex Pharmaceuticals Incorporated Azaindoles útiles como inhibidores de jak y otras proteína quinasas.
GB0500492D0 (en) * 2005-01-11 2005-02-16 Cyclacel Ltd Compound
JP2009513615A (ja) 2005-10-28 2009-04-02 アストラゼネカ アクチボラグ 癌の治療においてチロシンキナーゼ阻害剤として使用するための4−(3−アミノピラゾール)ピリミジン誘導体
KR20080110998A (ko) * 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Jak­2 조절자로서 4­아릴­2­아미노­피리미딘 또는 4­아릴­2­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
EA017405B9 (ru) * 2006-12-08 2014-05-30 АйАрЭм ЭлЭлСи Соединения и композиции в качестве ингибиторов протеинкиназы
US9908884B2 (en) * 2009-05-05 2018-03-06 Dana-Farber Cancer Institute, Inc. EGFR inhibitors and methods of treating disorders
EP2611793A1 (en) * 2010-09-01 2013-07-10 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof
US9198911B2 (en) 2010-11-02 2015-12-01 The Trustees Of Columbia University In The City Of New York Methods for treating hair loss disorders
JP2014500254A (ja) * 2010-11-09 2014-01-09 セルゾーム リミティッド Tyk2阻害剤としてのピリジン化合物およびそのアザ類似体
WO2012116247A1 (en) * 2011-02-25 2012-08-30 Synta Pharmaceuticals Corp. Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers
DK2830662T3 (da) 2012-03-29 2019-01-02 Univ Columbia Fremgangsmåder til behandlng af hårtabsforstyrrelser
JP6767491B2 (ja) * 2015-09-25 2020-10-14 ディザル(ジァンスー)ファーマシューティカル・カンパニー・リミテッド Jakを阻害するための化合物及び方法

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010135650A1 (en) * 2009-05-22 2010-11-25 Incyte Corporation N-(HETERO)ARYL-PYRROLIDINE DERIVATIVES OF PYRAZOL-4-YL-PYRROLO[2,3-d]PYRIMIDINES AND PYRROL-3-YL-PYRROLO[2,3-d]PYRIMIDINES AS JANUS KINASE INHIBITORS
TW201107325A (en) * 2009-07-31 2011-03-01 Japan Tobacco Inc Nitrogen-containing spiro cyclic compounds and pharmaceutical use thereof
WO2012068450A1 (en) * 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012177606A1 (en) * 2011-06-20 2012-12-27 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as jak inhibitors

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AR106138A1 (es) 2017-12-13
CA2995430C (en) 2023-07-11
US10654835B2 (en) 2020-05-19
KR20180058719A (ko) 2018-06-01
US10167276B2 (en) 2019-01-01
CN111606893A (zh) 2020-09-01
MX375724B (es) 2025-03-06
KR20250035597A (ko) 2025-03-12
JP6767491B2 (ja) 2020-10-14
CN111848586A (zh) 2020-10-30
RU2760359C2 (ru) 2021-11-24
MX2018003590A (es) 2018-11-29
CN111646980A (zh) 2020-09-11
EP3353168A1 (en) 2018-08-01
KR102774784B1 (ko) 2025-02-27
EP3353168B1 (en) 2023-08-30
ZA201800782B (en) 2018-12-19
AU2016328764B2 (en) 2020-07-09
AU2016328764A1 (en) 2018-02-22
JP2018529770A (ja) 2018-10-11
US20170088543A1 (en) 2017-03-30
RU2018112993A (ru) 2019-10-28
US12319670B2 (en) 2025-06-03
EP4219482A1 (en) 2023-08-02
BR112018005833A2 (pt) 2018-10-16
CN111848586B (zh) 2024-05-03
US9714236B2 (en) 2017-07-25
BR112018005833B1 (pt) 2023-10-10
CN108368091A (zh) 2018-08-03
US20170320857A1 (en) 2017-11-09
CN111646980B (zh) 2021-08-27
DK3353168T3 (da) 2023-10-02
CA2995430A1 (en) 2017-03-30
US20220119372A1 (en) 2022-04-21
RU2018112993A3 (https=) 2020-01-30
HK1259422A1 (zh) 2019-11-29
US20210078981A1 (en) 2021-03-18
PT3353168T (pt) 2023-09-20
US20190092760A1 (en) 2019-03-28
ES2956642T3 (es) 2023-12-26
CN111606893B (zh) 2021-05-04
WO2017050938A1 (en) 2017-03-30
TW201730186A (zh) 2017-09-01
US11247983B2 (en) 2022-02-15
CN108368091B (zh) 2020-08-11

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