KR20220024405A - Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용 - Google Patents

Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용 Download PDF

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Publication number
KR20220024405A
KR20220024405A KR1020227000044A KR20227000044A KR20220024405A KR 20220024405 A KR20220024405 A KR 20220024405A KR 1020227000044 A KR1020227000044 A KR 1020227000044A KR 20227000044 A KR20227000044 A KR 20227000044A KR 20220024405 A KR20220024405 A KR 20220024405A
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South Korea
Prior art keywords
alkyl
methyl
compound
phenyl
pharmaceutically acceptable
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Ceased
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KR1020227000044A
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English (en)
Korean (ko)
Inventor
마크 에드워드 자크
나오미 에스. 라자파크사
윤-싱 쳉
제시카 마리 그랜드너
대니얼 쥐. 엠. 쇼어
마리안 씨. 브라이언
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에프. 호프만-라 로슈 아게
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Publication of KR20220024405A publication Critical patent/KR20220024405A/ko
Ceased legal-status Critical Current

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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A61K9/0075—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy for inhalation via a dry powder inhaler [DPI], e.g. comprising micronized drug mixed with lactose carrier particles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • 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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/0012—Galenical forms characterised by the site of application
    • A61K9/007—Pulmonary tract; Aromatherapy
    • A61K9/0073—Sprays or powders for inhalation; Aerolised or nebulised preparations generated by other means than thermal energy
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00—Medicinal preparations characterised by special physical form
    • A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
    • A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16—Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • 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
    • 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
    • A61P19/00—Drugs for skeletal disorders
    • A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • 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
    • A61P37/02—Immunomodulators
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • 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
    • A61P9/02—Non-specific cardiovascular stimulants, e.g. drugs for syncope, antihypotensives
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pulmonology (AREA)
  • Diabetes (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Epidemiology (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Pain & Pain Management (AREA)
  • Immunology (AREA)
  • Otolaryngology (AREA)
  • Obesity (AREA)
  • Hospice & Palliative Care (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Emergency Medicine (AREA)
  • Endocrinology (AREA)
  • Hematology (AREA)
  • Psychiatry (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Virology (AREA)
  • Vascular Medicine (AREA)
KR1020227000044A 2019-06-18 2020-06-16 Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용 Ceased KR20220024405A (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
CNPCT/CN2019/091712 2019-06-18
CN2019091712 2019-06-18
US202063035381P 2020-06-05 2020-06-05
US63/035,381 2020-06-05
PCT/US2020/037853 WO2020257145A1 (en) 2019-06-18 2020-06-16 Pyrazolopyrimidine sulfone inhibitors of jak kinases and uses thereof

Publications (1)

Publication Number Publication Date
KR20220024405A true KR20220024405A (ko) 2022-03-03

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
KR1020227000044A Ceased KR20220024405A (ko) 2019-06-18 2020-06-16 Jak 키나제의 피라졸로피리미딘 설폰 억제제 및 그 사용

Country Status (18)

Country Link
US (2) US11453671B2 (https=)
EP (1) EP3986901A1 (https=)
JP (1) JP7657740B2 (https=)
KR (1) KR20220024405A (https=)
CN (1) CN114008051B (https=)
AU (1) AU2020297415A1 (https=)
BR (1) BR112021025618A2 (https=)
CA (1) CA3140024A1 (https=)
CL (1) CL2021003341A1 (https=)
CO (1) CO2022000118A2 (https=)
CR (1) CR20210661A (https=)
IL (1) IL288957A (https=)
MA (1) MA56518A (https=)
MX (1) MX2021015319A (https=)
PE (1) PE20220577A1 (https=)
PH (1) PH12021552998A1 (https=)
TW (1) TW202115068A (https=)
WO (1) WO2020257145A1 (https=)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230147351A (ko) * 2022-04-14 2023-10-23 한국화학연구원 퀴녹살린 카르복스아마이드 유도체 및 이를 유효성분으로 포함하는 교모세포종의 예방 또는 치료용 약학적 조성물

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202115069A (zh) 2019-06-18 2021-04-16 瑞士商赫孚孟拉羅股份公司 Ｊａｋ激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途
KR20250011137A (ko) 2022-05-11 2025-01-21 피아이 인더스트리스 엘티디. 바이사이클릭 화합물 및 해충 방제제로서 이의 용도

Family Cites Families (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU650953B2 (en) 1991-03-21 1994-07-07 Novartis Ag Inhaler
US5543523A (en) 1994-11-15 1996-08-06 Regents Of The University Of Minnesota Method and intermediates for the synthesis of korupensamines
US6034057A (en) 1995-07-06 2000-03-07 Zeneca Limited Peptide inhibitors of fibronectine
US6248713B1 (en) 1995-07-11 2001-06-19 Biogen, Inc. Cell adhesion inhibitors
YU25500A (sh) 1999-05-11 2003-08-29 Pfizer Products Inc. Postupak za sintezu analoga nukleozida
GB0028383D0 (en) 2000-11-21 2001-01-03 Novartis Ag Organic compounds
EP1241176A1 (en) 2001-03-16 2002-09-18 Pfizer Products Inc. Purine derivatives for the treatment of ischemia
DE60214428T2 (de) 2001-12-20 2007-09-20 Bayer Healthcare Ag 1, 4-dihydro-1, 4-diphenylpyridin-derivate
SE0302487D0 (sv) 2003-09-18 2003-09-18 Astrazeneca Ab Novel compounds
GB0502258D0 (en) 2005-02-03 2005-03-09 Argenta Discovery Ltd Compounds and their use
CA2676665A1 (en) * 2007-01-30 2008-08-07 Biogen Idec Ma Inc. Modulators of mitotic kinases
CN101616921A (zh) * 2007-01-30 2009-12-30 比奥根艾迪克Ma公司 1-H-吡唑并(3,4b)嘧啶衍生物及其作为有丝分裂激酶调节剂的用途
CN102131389A (zh) 2008-06-20 2011-07-20 健泰科生物技术公司 三唑并吡啶jak抑制剂化合物和方法
EP2348860B1 (en) 2008-10-31 2015-05-27 Genentech, Inc. Pyrazolopyrimidine jak inhibitor compounds and methods
UA110324C2 (en) 2009-07-02 2015-12-25 Genentech Inc Jak inhibitory compounds based on pyrazolo pyrimidine
US8575336B2 (en) 2011-07-27 2013-11-05 Pfizer Limited Indazoles
AP2015008433A0 (en) 2012-11-09 2015-05-31 Jacobus Pahrmaceutical Company Inc Heteroaryl derivatives and uses thereof
JP2017516850A (ja) 2014-05-23 2017-06-22 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ Ｊａｋ阻害剤である５−クロロ−２−ジフルオロメトキシフェニルピラゾロピリミジン化合物
TW201720828A (zh) * 2015-11-23 2017-06-16 赫孚孟拉羅股份公司 治療性化合物及組合物以及其使用方法
JP6936236B2 (ja) * 2016-02-18 2021-09-15 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ 治療化合物、組成物及びその方法の使用
CR20190310A (es) 2016-12-29 2019-08-21 Hoffmann La Roche Compuestos de pirazolopirimidina y métodos de uso de los mismos
JP2020510061A (ja) 2017-03-14 2020-04-02 エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ ピラゾロクロロフェニル化合物、組成物及びその使用方法
CN110678467B (zh) * 2017-05-22 2023-06-13 豪夫迈·罗氏有限公司 治疗化合物和组合物及其使用方法
MX387969B (es) 2017-05-22 2025-03-19 Hoffmann La Roche Composiciones y compuestos terapéuticos, y métodos para su uso.
EP3740488A1 (en) * 2018-01-15 2020-11-25 F. Hoffmann-La Roche AG Pyrazolopyrimidine compounds as jak inhibitors
AU2020210455B2 (en) * 2019-01-25 2023-02-02 Beijing Scitech-Mq Pharmaceuticals Limited Acylamino bridged heterocyclic compound, and composition and application thereof
TW202115069A (zh) 2019-06-18 2021-04-16 瑞士商赫孚孟拉羅股份公司 Ｊａｋ激酶之經四唑取代之吡唑并嘧啶抑制劑及其用途
EP3986899A1 (en) 2019-06-18 2022-04-27 F. Hoffmann-La Roche AG Pyrazolopyrimidine aryl ether inhibitors of jak kinases and uses thereof

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR20230147351A (ko) * 2022-04-14 2023-10-23 한국화학연구원 퀴녹살린 카르복스아마이드 유도체 및 이를 유효성분으로 포함하는 교모세포종의 예방 또는 치료용 약학적 조성물

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Publication number Publication date
US20200399275A1 (en) 2020-12-24
JP7657740B2 (ja) 2025-04-07
PE20220577A1 (es) 2022-04-20
AU2020297415A1 (en) 2022-01-06
CN114008051A (zh) 2022-02-01
WO2020257145A1 (en) 2020-12-24
PH12021552998A1 (en) 2023-08-14
CO2022000118A2 (es) 2022-01-28
CN114008051B (zh) 2024-08-13
US11453671B2 (en) 2022-09-27
IL288957A (en) 2022-02-01
JP2022537964A (ja) 2022-08-31
TW202115068A (zh) 2021-04-16
US20230016791A1 (en) 2023-01-19
MX2021015319A (es) 2022-04-07
CR20210661A (es) 2022-02-11
MA56518A (fr) 2022-04-27
EP3986901A1 (en) 2022-04-27
CL2021003341A1 (es) 2022-07-22
BR112021025618A2 (pt) 2022-02-01
CA3140024A1 (en) 2020-12-24

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