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)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Hematology (AREA)
  • Dermatology (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
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
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
CN201680055491.7A CN108368091B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法

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CN111848586A CN111848586A (zh) 2020-10-30
CN111848586B true CN111848586B (zh) 2024-05-03

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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
CN202010629290.1A Active CN111606893B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法
CN202010629286.5A Active CN111646980B (zh) 2015-09-25 2016-09-22 用于抑制jak的化合物和方法

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CN202010629286.5A Active CN111646980B (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 (https=)
EP (2) EP4219482A1 (https=)
JP (1) JP6767491B2 (https=)
KR (2) KR20250035597A (https=)
CN (4) CN111848586B (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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BR112018005833B1 (pt) * 2015-09-25 2023-10-10 Dizal (Jiangsu) Pharmaceutical Co., Limited Composto, sal farmaceuticamente aceitável, composição farmacêutica e uso do composto
AU2017269335B2 (en) 2016-05-26 2021-07-01 Recurium Ip Holdings, Llc EGFR inhibitor compounds
KR102585048B1 (ko) 2017-01-17 2023-10-05 아스트라제네카 아베 Jak1 선택적 억제제
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
SG11202100240RA (en) * 2018-07-18 2021-02-25 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
TWI910107B (zh) * 2019-04-19 2026-01-01 大陸商迪哲（江蘇）醫藥股份有限公司 Ｊａｋ１選擇性激酶抑制劑
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
JP7613778B2 (ja) * 2020-11-26 2025-01-15 科輝智薬（深▲セン▼）新薬研究中心有限公司 アミド化合物、医薬組成物およびその使用
BR112023016986A2 (pt) * 2021-02-26 2023-11-07 Tyra Biosciences Inc Compostos de aminopirimidina e métodos de seu uso
BR112023018286A2 (pt) * 2021-03-11 2023-10-31 Janssen Pharmaceutica Nv Lorpucitinib para uso no tratamento de distúrbios 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

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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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TWI372624B (en) * 2004-03-30 2012-09-21 Vertex Pharma 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
KR20080110998A (ko) * 2006-01-30 2008-12-22 엑셀리시스, 인코포레이티드 Ｊａｋ­２ 조절자로서 ４­아릴­２­아미노­피리미딘 또는 4­아릴­２­아미노알킬­피리미딘 및 이들을 포함하는 약제학적 조성물
BRPI0720264B1 (pt) * 2006-12-08 2022-03-03 Novartis Ag Compostos e composições como inibidores de proteína cinase
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
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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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
CN111606893A (zh) 2020-09-01
AU2016328764B2 (en) 2020-07-09
US12319670B2 (en) 2025-06-03
DK3353168T3 (da) 2023-10-02
RU2018112993A (ru) 2019-10-28
CA2995430C (en) 2023-07-11
HK1259422A1 (zh) 2019-11-29
US20170320857A1 (en) 2017-11-09
PT3353168T (pt) 2023-09-20
RU2018112993A3 (https=) 2020-01-30
US10654835B2 (en) 2020-05-19
EP4219482A1 (en) 2023-08-02
US20190092760A1 (en) 2019-03-28
CA2995430A1 (en) 2017-03-30
WO2017050938A1 (en) 2017-03-30
US20210078981A1 (en) 2021-03-18
MX2018003590A (es) 2018-11-29
ES2956642T3 (es) 2023-12-26
KR20250035597A (ko) 2025-03-12
ZA201800782B (en) 2018-12-19
CN111646980A (zh) 2020-09-11
US20220119372A1 (en) 2022-04-21
TW201730186A (zh) 2017-09-01
JP6767491B2 (ja) 2020-10-14
CN111848586A (zh) 2020-10-30
BR112018005833B1 (pt) 2023-10-10
US20170088543A1 (en) 2017-03-30
BR112018005833A2 (pt) 2018-10-16
EP3353168B1 (en) 2023-08-30
AU2016328764A1 (en) 2018-02-22
EP3353168A1 (en) 2018-08-01
TWI740843B (zh) 2021-10-01
AR106138A1 (es) 2017-12-13
MX375724B (es) 2025-03-06
CN111606893B (zh) 2021-05-04
CN108368091A (zh) 2018-08-03
CN108368091B (zh) 2020-08-11
KR20180058719A (ko) 2018-06-01
CN111646980B (zh) 2021-08-27
JP2018529770A (ja) 2018-10-11
US9714236B2 (en) 2017-07-25
US11247983B2 (en) 2022-02-15
KR102774784B1 (ko) 2025-02-27
US10167276B2 (en) 2019-01-01
RU2760359C2 (ru) 2021-11-24

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