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

    • 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

Landscapes

  • 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)
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 (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=)

Families Citing this family (15)

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

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
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
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
AU2011328237A1 (en) * 2010-11-09 2013-05-23 Cellzome Limited Pyridine compounds and aza analogues thereof as TYK2 inhibitors
US20140045908A1 (en) * 2011-02-25 2014-02-13 Synta Pharmaceuticals Corp. Hsp90 inhibitory compounds in treating jak/stat signaling-mediated cancers
EP3459565A1 (en) 2012-03-29 2019-03-27 The Trustees of Columbia University in the City of New York Methods for treating hair loss disorders
BR112018005833B1 (pt) * 2015-09-25 2023-10-10 Dizal (Jiangsu) Pharmaceutical Co., Limited Composto, sal farmaceuticamente aceitável, composição farmacêutica e uso do composto

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
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
CN111848586B (zh) 2024-05-03
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
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

Similar Documents

Publication Publication Date Title
TWI740843B (zh) 用於抑制jak之化合物和方法
CN115626919A (zh) 哒嗪基噻唑甲酰胺类化合物
HK40035295A (en) Compounds and methods for inhibiting jak
HK40026768B (en) Compounds and methods for inhibiting jak
HK40026768A (en) Compounds and methods for inhibiting jak
HK40035295B (zh) 用於抑制jak的化合物和方法
HK40026896A (en) Compounds and methods for inhibiting jak
HK40026896B (en) Compounds and methods for inhibiting jak
HK40096832A (en) Compounds and methods for inhibiting jak
HK1259422B (zh) 用於抑制jak的化合物和方法
HK40077526B (zh) 对核受体具有活性的化合物
HK40084227B (zh) 哒嗪基噻唑甲醯胺类化合物
HK40085586B (zh) 哒嗪基噻唑甲酰胺类化合物
HK40059656B (zh) 哒嗪基噻唑甲酰胺类化合物