CN111848586B - 用于抑制jak的化合物和方法 - Google Patents

用于抑制jak的化合物和方法 Download PDF

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Publication number
CN111848586B
CN111848586B CN202010626114.2A CN202010626114A CN111848586B CN 111848586 B CN111848586 B CN 111848586B CN 202010626114 A CN202010626114 A CN 202010626114A CN 111848586 B CN111848586 B CN 111848586B
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methyl
methoxy
indol
pyrazol
methylpiperazin
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Chinese (zh)
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CN111848586A (zh
Inventor
A·B·M·阿斯特兰
N·P·格林斯特
S·卡沃特卡尔
J·G·凯特勒
M·K·尼尔逊
L·L·拉斯顿
Q·苏
M·M·瓦斯宾德
J·J·温特-霍尔特
D·吴
W·杨
T·格雷库
J·麦卡贝
R·D·韦斯纳
C·E·丘阿基
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Dizhe Jiangsu Pharmaceutical Co ltd
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Dizhe Jiangsu Pharmaceutical Co ltd
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    • 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
    • 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/13—Crystalline forms, e.g. polymorphs

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (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)
  • Epidemiology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Hematology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Dermatology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Diabetes (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
CN202010626114.2A 2015-09-25 2016-09-22 用于抑制jak的化合物和方法 Active CN111848586B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202010626114.2A CN111848586B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
US201562232629P 2015-09-25 2015-09-25
US62/232,629 2015-09-25
CN201680055491.7A CN108368091B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法
CN202010626114.2A CN111848586B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法
PCT/EP2016/072616 WO2017050938A1 (en) 2015-09-25 2016-09-22 Compounds and methods for inhibiting jak

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CN111848586B true CN111848586B (zh) 2024-05-03

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CN202010629290.1A Active CN111606893B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法
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CN201680055491.7A Active CN108368091B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法

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US (5) US9714236B2 (enExample)
EP (2) EP3353168B1 (enExample)
JP (1) JP6767491B2 (enExample)
KR (2) KR20250035597A (enExample)
CN (4) CN111848586B (enExample)
AR (1) AR106138A1 (enExample)
AU (1) AU2016328764B2 (enExample)
BR (1) BR112018005833B1 (enExample)
CA (1) CA2995430C (enExample)
DK (1) DK3353168T3 (enExample)
ES (1) ES2956642T3 (enExample)
MX (1) MX375724B (enExample)
PT (1) PT3353168T (enExample)
RU (1) RU2760359C2 (enExample)
TW (1) TWI740843B (enExample)
WO (1) WO2017050938A1 (enExample)
ZA (1) ZA201800782B (enExample)

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CN111848586B (zh) * 2015-09-25 2024-05-03 迪哲(江苏)医药股份有限公司 用于抑制jak的化合物和方法
SG11201809751XA (en) 2016-05-26 2018-12-28 Zeno Royalties & Milestones Llc Egfr inhibitor compounds
HRP20230069T1 (hr) 2017-01-17 2023-03-17 Astrazeneca Ab Selektivni inhibitori 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
CN112823159B (zh) * 2018-09-21 2024-03-01 上海轶诺药业有限公司 一类具有激酶抑制活性的芳香杂环类化合物
KR102195348B1 (ko) 2018-11-15 2020-12-24 에이치케이이노엔 주식회사 단백질 키나제 억제제로서의 신규 화합물 및 이를 포함하는 약제학적 조성물
CA3134174A1 (en) * 2019-04-19 2020-10-22 Dizal (Jiangsu) Pharmaceutical Co., Ltd. Jak1 selective kinase inhibitor
CN110627775A (zh) * 2019-10-24 2019-12-31 嘉兴特科罗生物科技有限公司 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
JP2024509795A (ja) * 2021-02-26 2024-03-05 タイラ・バイオサイエンシーズ・インコーポレイテッド アミノピリミジン化合物及びその使用方法
AU2022233254A1 (en) * 2021-03-11 2023-10-26 Janssen Pharmaceutica Nv Lorpucitinib for use in the treatment of jak mediated disorders
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

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WO2012030910A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof
CN102458581A (zh) * 2009-05-22 2012-05-16 因塞特公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2,3-d]嘧啶和吡咯-3-基-吡咯并[2,3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物

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WO2005095400A1 (en) 2004-03-30 2005-10-13 Vertex Pharmaceuticals Incorporated Azaindoles useful as inhibitors of jak and other protein kinases
GB0500492D0 (en) 2005-01-11 2005-02-16 Cyclacel Ltd Compound
WO2007049041A1 (en) 2005-10-28 2007-05-03 Astrazeneca Ab 4- (3-aminopyrazole) pyrimidine derivatives for use as tyrosine kinase inhibitors in the treatment of cancer
EP1979329A2 (en) * 2006-01-30 2008-10-15 Exelixis, Inc. 4-aryl-2-amino-pyrimidines or 4-aryl-2-aminoalkyl-pyrimidines as jak-2 modulators and methods of use
BRPI0720264B1 (pt) * 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
JP5918693B2 (ja) * 2009-05-05 2016-05-18 ダナ ファーバー キャンサー インスティテュート インコーポレイテッド Ｅｇｆｒ阻害剤及び疾患の治療方法
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
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US20140045908A1 (en) * 2011-02-25 2014-02-13 Synta Pharmaceuticals Corp. Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers
US8691807B2 (en) * 2011-06-20 2014-04-08 Incyte Corporation Azetidinyl phenyl, pyridyl or pyrazinyl carboxamide derivatives as JAK inhibitors
KR102135601B1 (ko) 2012-03-29 2020-07-20 더 트러스티스 오브 콜롬비아 유니버시티 인 더 시티 오브 뉴욕 탈모 질환의 치료 방법
CN111848586B (zh) * 2015-09-25 2024-05-03 迪哲(江苏)医药股份有限公司 用于抑制jak的化合物和方法

Patent Citations (2)

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CN102458581A (zh) * 2009-05-22 2012-05-16 因塞特公司 作为JANUS激酶抑制剂的吡唑-4-基-吡咯并[2,3-d]嘧啶和吡咯-3-基-吡咯并[2,3-d]嘧啶的N-(杂)芳基-吡咯烷衍生物
WO2012030910A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof

Also Published As

Publication number Publication date
EP3353168B1 (en) 2023-08-30
PT3353168T (pt) 2023-09-20
MX375724B (es) 2025-03-06
KR102774784B1 (ko) 2025-02-27
CN111848586A (zh) 2020-10-30
TWI740843B (zh) 2021-10-01
CN108368091A (zh) 2018-08-03
AR106138A1 (es) 2017-12-13
JP2018529770A (ja) 2018-10-11
TW201730186A (zh) 2017-09-01
BR112018005833A2 (pt) 2018-10-16
US20190092760A1 (en) 2019-03-28
DK3353168T3 (da) 2023-10-02
CN108368091B (zh) 2020-08-11
KR20250035597A (ko) 2025-03-12
RU2018112993A3 (enExample) 2020-01-30
EP4219482A1 (en) 2023-08-02
RU2018112993A (ru) 2019-10-28
ZA201800782B (en) 2018-12-19
HK1259422A1 (zh) 2019-11-29
US20170320857A1 (en) 2017-11-09
US11247983B2 (en) 2022-02-15
CA2995430A1 (en) 2017-03-30
US20170088543A1 (en) 2017-03-30
US10167276B2 (en) 2019-01-01
JP6767491B2 (ja) 2020-10-14
US20210078981A1 (en) 2021-03-18
CN111606893B (zh) 2021-05-04
BR112018005833B1 (pt) 2023-10-10
US10654835B2 (en) 2020-05-19
EP3353168A1 (en) 2018-08-01
CA2995430C (en) 2023-07-11
CN111646980B (zh) 2021-08-27
ES2956642T3 (es) 2023-12-26
US9714236B2 (en) 2017-07-25
US20220119372A1 (en) 2022-04-21
MX2018003590A (es) 2018-11-29
CN111606893A (zh) 2020-09-01
KR20180058719A (ko) 2018-06-01
AU2016328764B2 (en) 2020-07-09
RU2760359C2 (ru) 2021-11-24
WO2017050938A1 (en) 2017-03-30
AU2016328764A1 (en) 2018-02-22
US12319670B2 (en) 2025-06-03
CN111646980A (zh) 2020-09-11

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