AU2016328764B2 - Compounds and methods for inhibiting JAK - Google Patents

Compounds and methods for inhibiting JAK Download PDF

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Publication number
AU2016328764B2
AU2016328764B2 AU2016328764A AU2016328764A AU2016328764B2 AU 2016328764 B2 AU2016328764 B2 AU 2016328764B2 AU 2016328764 A AU2016328764 A AU 2016328764A AU 2016328764 A AU2016328764 A AU 2016328764A AU 2016328764 B2 AU2016328764 B2 AU 2016328764B2
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Prior art keywords
methyl
indol
pyrazol
methoxy
amino
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AU2016328764A
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AU2016328764A1 (en
Inventor
Annika Birgitta Margareta Astrand
Claudio Edmundo Chuaqui
Tudor GRECU
Neil Patrick Grimster
Sameer KAWATKAR
Jason Grant Kettle
James Mccabe
Magnus K. Nilsson
Linette Lys Ruston
Qibin Su
Melissa Marie Vasbinder
Jon James Winter-Holt
Richard Donald Woessner
Dedong Wu
Wenzhan YANG
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Dizal Jiangsu Pharmaceutical Co Ltd
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Dizal 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (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)
  • Heart & Thoracic Surgery (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Hematology (AREA)
  • Diabetes (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Dermatology (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)
AU2016328764A 2015-09-25 2016-09-22 Compounds and methods for inhibiting JAK Active AU2016328764B2 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201562232629P 2015-09-25 2015-09-25
US62/232,629 2015-09-25
PCT/EP2016/072616 WO2017050938A1 (en) 2015-09-25 2016-09-22 Compounds and methods for inhibiting jak

Publications (2)

Publication Number Publication Date
AU2016328764A1 AU2016328764A1 (en) 2018-02-22
AU2016328764B2 true AU2016328764B2 (en) 2020-07-09

Family

ID=56979589

Family Applications (1)

Application Number Title Priority Date Filing Date
AU2016328764A Active AU2016328764B2 (en) 2015-09-25 2016-09-22 Compounds and methods for inhibiting JAK

Country Status (17)

Country Link
US (5) US9714236B2 (enExample)
EP (2) EP3353168B1 (enExample)
JP (1) JP6767491B2 (enExample)
KR (2) KR102774784B1 (enExample)
CN (4) CN111606893B (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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KR102774784B1 (ko) * 2015-09-25 2025-02-27 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 Jak를 억제하기 위한 화합물 및 방법
CN109311858B (zh) 2016-05-26 2021-12-03 里科瑞尔姆Ip控股有限责任公司 Egfr抑制剂化合物
PE20191108A1 (es) 2017-01-17 2019-08-26 Astrazeneca Ab Inhibidores selectivos de jak1
KR20190043437A (ko) 2017-10-18 2019-04-26 씨제이헬스케어 주식회사 단백질 키나제 억제제로서의 헤테로고리 화합물
US11149029B2 (en) * 2018-07-18 2021-10-19 Astrazeneca Ab Salts of IJAK inhibitors and methods of using the same
EP3854793A4 (en) * 2018-09-21 2022-06-01 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
AU2020258619C1 (en) * 2019-04-19 2026-01-29 Dizal (Jiangsu) Pharmaceutical Co., Ltd. JAK1 selective kinase inhibitor
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
EP4297873A1 (en) * 2021-02-26 2024-01-03 Tyra Biosciences, Inc. Aminopyrimidine compounds and methods of their use
US12390451B2 (en) 2021-03-11 2025-08-19 Janssen Pharmaceutica Nv Small molecule inhibitor of the JAK family of kinases
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 (1)

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WO2012030910A1 (en) * 2010-09-01 2012-03-08 Ambit Biosciences Corporation 2-cycloquinazoline derivatives and methods of use thereof

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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
BRPI0618011A2 (pt) 2005-10-28 2011-08-16 Astrazeneca Ab composto ou um sal farmaceuticamente aceitável do mesmo, processo para a preparação do mesmo, composição farmacêutica, uso de um composto ou um sal farmaceuticamente aceitável do mesmo, e, métodos para produzir um efeito anti-proliferativo e um efeito pró-apoptósico em um animal de sangue quente, para tratar doença e para produzir um efeito inibidor de jak em um animal de sangue quente
EA200870217A1 (ru) * 2006-01-30 2009-02-27 Экселиксис, Инк. 4-арил-2-аминопиримидины или 4-арил-2-аминоалкилпиримидины в качестве модуляторов jak-2 и содержащие их фармацевтические композиции
JP5208123B2 (ja) * 2006-12-08 2013-06-12 アイアールエム・リミテッド・ライアビリティ・カンパニー タンパク質キナーゼ阻害剤としての化合物および組成物
KR101705158B1 (ko) * 2009-05-05 2017-02-09 다나-파버 캔서 인스티튜트 인크. Ｅｇｆｒ 억제제 및 질환 치료방법
NZ596479A (en) 2009-05-22 2014-01-31 Incyte Corp 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
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
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
AU2011328237A1 (en) * 2010-11-09 2013-05-23 Cellzome Limited Pyridine compounds and aza analogues thereof as TYK2 inhibitors
CA2818542A1 (en) * 2010-11-19 2012-05-24 Incyte Corporation Cyclobutyl substituted pyrrolopyridine and pyrrolopyrimidine derivatives as jak inhibitors
WO2012116247A1 (en) 2011-02-25 2012-08-30 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
DK2830662T3 (da) 2012-03-29 2019-01-02 Univ Columbia Fremgangsmåder til behandlng af hårtabsforstyrrelser
KR102774784B1 (ko) * 2015-09-25 2025-02-27 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 Jak를 억제하기 위한 화합물 및 방법

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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
CN111848586B (zh) 2024-05-03
US20170088543A1 (en) 2017-03-30
MX2018003590A (es) 2018-11-29
CN111606893A (zh) 2020-09-01
RU2760359C2 (ru) 2021-11-24
EP3353168A1 (en) 2018-08-01
CN111606893B (zh) 2021-05-04
EP3353168B1 (en) 2023-08-30
TWI740843B (zh) 2021-10-01
US10654835B2 (en) 2020-05-19
RU2018112993A (ru) 2019-10-28
US12319670B2 (en) 2025-06-03
RU2018112993A3 (enExample) 2020-01-30
US20210078981A1 (en) 2021-03-18
JP6767491B2 (ja) 2020-10-14
US20190092760A1 (en) 2019-03-28
BR112018005833B1 (pt) 2023-10-10
AR106138A1 (es) 2017-12-13
DK3353168T3 (da) 2023-10-02
CA2995430A1 (en) 2017-03-30
CA2995430C (en) 2023-07-11
HK1259422A1 (zh) 2019-11-29
US20220119372A1 (en) 2022-04-21
AU2016328764A1 (en) 2018-02-22
PT3353168T (pt) 2023-09-20
CN108368091B (zh) 2020-08-11
KR20250035597A (ko) 2025-03-12
KR20180058719A (ko) 2018-06-01
JP2018529770A (ja) 2018-10-11
MX375724B (es) 2025-03-06
US20170320857A1 (en) 2017-11-09
ZA201800782B (en) 2018-12-19
US11247983B2 (en) 2022-02-15
KR102774784B1 (ko) 2025-02-27
BR112018005833A2 (pt) 2018-10-16
CN108368091A (zh) 2018-08-03
US10167276B2 (en) 2019-01-01
CN111646980A (zh) 2020-09-11
US9714236B2 (en) 2017-07-25
CN111646980B (zh) 2021-08-27
WO2017050938A1 (en) 2017-03-30
CN111848586A (zh) 2020-10-30
TW201730186A (zh) 2017-09-01
EP4219482A1 (en) 2023-08-02
ES2956642T3 (es) 2023-12-26

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