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

Info

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
Authority
TW
Taiwan
Prior art keywords
methyl
indol
methoxy
pyrazol
amino
Prior art date
Application number
TW105130891A
Other languages
English (en)
Chinese (zh)
Other versions
TW201730186A (zh
Inventor
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
Original Assignee
中國大陸商迪哲(江蘇)醫藥有限公司
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by 中國大陸商迪哲(江蘇)醫藥有限公司 filed Critical 中國大陸商迪哲(江蘇)醫藥有限公司
Publication of TW201730186A publication Critical patent/TW201730186A/zh
Application granted granted Critical
Publication of TWI740843B publication Critical patent/TWI740843B/zh

Links

Images

Classifications

    • 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

Landscapes

  • 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)
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

Family

ID=56979589

Family Applications (1)

Application Number Title Priority Date Filing Date
TW105130891A TWI740843B (zh) 2015-09-25 2016-09-23 用於抑制jak之化合物和方法

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)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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 (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

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
US20130225615A1 (en) * 2010-09-01 2013-08-29 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
AU2011328237A1 (en) * 2010-11-09 2013-05-23 Cellzome Limited Pyridine compounds and aza analogues thereof as TYK2 inhibitors
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
KR102774784B1 (ko) * 2015-09-25 2025-02-27 디잘 (지앙수) 파마슈티칼 씨오., 리미티드 Jak를 억제하기 위한 화합물 및 방법

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

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
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
AU2016328764B2 (en) 2020-07-09
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

Similar Documents

Publication Publication Date Title
CN108368091B (zh) 用于抑制jak的化合物和方法
TWI920639B (zh) Shp2之八氫環戊烷并[c]吡咯別構抑制劑
CN115626919A (zh) 哒嗪基噻唑甲酰胺类化合物
HK40035295A (en) Compounds and methods for inhibiting jak
HK40026768A (en) Compounds and methods for inhibiting jak
HK40026768B (en) Compounds and methods for inhibiting jak
HK40035295B (en) Compounds and methods for inhibiting jak
HK40026896B (en) Compounds and methods for inhibiting jak
HK40026896A (en) Compounds and methods for inhibiting jak
HK40096832A (en) Compounds and methods for inhibiting jak
HK1259422B (en) Compounds and methods for inhibiting jak
HK40077526B (en) Compounds active towards nuclear receptors
HK40084227B (en) Pyridazinyl thiazolecarboxamide compound
HK40085586B (en) Pyridazinyl thiazolecarboxamide compound
HK40059656B (zh) 哒嗪基噻唑甲酰胺类化合物