CN113214278B - 新型Jak1选择性抑制剂及其用途 - Google Patents

新型Jak1选择性抑制剂及其用途 Download PDF

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Publication number
CN113214278B
CN113214278B CN202110514751.5A CN202110514751A CN113214278B CN 113214278 B CN113214278 B CN 113214278B CN 202110514751 A CN202110514751 A CN 202110514751A CN 113214278 B CN113214278 B CN 113214278B
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compound
formula
imidazo
pyridin
pharmaceutically acceptable
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CN113214278A (zh
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梁从新
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Hangzhou Gaoguang Pharmaceutical Co ltd
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Hangzhou Gaoguang Pharmaceutical Co ltd
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/14—Ortho-condensed systems
    • C07D491/147—Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/415—1,2-Diazoles
    • A61K31/4155—1,2-Diazoles non condensed and containing further heterocyclic 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • 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
    • 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
    • A61P37/06—Immunosuppressants, e.g. drugs for graft rejection
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04—Ortho-condensed systems
    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring the oxygen-containing ring being five-membered

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Rheumatology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Transplantation (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
CN202110514751.5A 2016-10-03 2017-09-30 新型Jak1选择性抑制剂及其用途 Active CN113214278B (zh)

Applications Claiming Priority (4)

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US201662403660P 2016-10-03 2016-10-03
US62/403,660 2016-10-03
PCT/US2017/054668 WO2018067422A1 (en) 2016-10-03 2017-09-30 Novel jak1 selective inhibitors and uses thereof
CN201780004442.5A CN108366994B (zh) 2016-10-03 2017-09-30 新型Jak1选择性抑制剂及其用途

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CN113214278B true CN113214278B (zh) 2022-10-28

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Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113214278B (zh) 2016-10-03 2022-10-28 杭州高光制药有限公司 新型Jak1选择性抑制剂及其用途
AU2018208516B2 (en) 2017-01-11 2021-07-08 Aqilion Ab Novel amino-imidazopyridine derivatives as Janus kinase inhibitors and pharmaceutical use thereof
JP7431845B2 (ja) 2018-10-31 2024-02-15 インサイト・コーポレイション 血液疾患の治療のための併用療法
MX2021010545A (es) 2019-03-05 2021-11-17 Incyte Corp Inhibidores de la vía de cinasa janus 1 (jak1) para el tratamiento de la disfunción crónica del aloinjerto pulmonar.
EP3941474A2 (en) * 2019-03-19 2022-01-26 Incyte Corporation Biomarkers for vitiligo
EP3981398A4 (en) * 2019-06-06 2023-03-15 Hangzhou Highlightll Pharmaceutical Co., Ltd. METHOD FOR SYNTHESIS OF A FUROIMIDAZOPYRIDINE COMPOUND, POLYMORPHOUS SUBSTANCE AND POLYMORPHOUS SUBSTANCE OF A SALT
BR112021024533A2 (pt) * 2019-06-06 2022-01-18 Highlightll Pharmaceutical Hainan Co Ltd Método de síntese de composto de furoimidazopiridina, forma cristalina de composto de furoimidazopiridina, e forma cristalina de sal do mesmo
US20230192617A1 (en) 2020-05-19 2023-06-22 Bayer Cropscience Aktiengesellschaft Azabicyclic(thio)amides as fungicidal compounds
US20230234945A1 (en) 2020-06-10 2023-07-27 Bayer Aktiengesellschaft Azabicyclyl-substituted heterocycles as fungicides
US20240307396A1 (en) * 2021-06-07 2024-09-19 The Regents Of The University Of California Compositions and methods for treating celiac disease
CN116490180B (zh) * 2021-09-13 2024-03-22 杭州高光制药有限公司 治疗cns病症的方法
CN114213424B (zh) 2021-12-30 2023-05-26 杭州高光制药有限公司 一种呋喃[3，2-b]并吡啶衍生物的合成方法
WO2025224600A1 (en) * 2024-04-21 2025-10-30 Biohaven Therapeutics Ltd. Treatment of alpha-synucleinopathies and neuroprotection
WO2025248468A1 (en) 2024-05-28 2025-12-04 Biohaven Therapeutics Ltd. Use of tyk2/jak1 inhibitors to treat amyloid-related imaging abnormalities (aria)

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101277963A (zh) * 2005-08-04 2008-10-01 西特里斯药业公司 作为sirtuin调节剂的噁唑并吡啶衍生物
WO2012022045A1 (en) * 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
CN102741253A (zh) * 2009-09-29 2012-10-17 艾科睿控股公司 PI3K(δ)选择性抑制剂
CN103442568A (zh) * 2010-10-08 2013-12-11 Abbvie公司 呋喃并[3,2-d]嘧啶化合物
CN104918945A (zh) * 2012-11-01 2015-09-16 因赛特公司 作为jak抑制剂的三环稠合噻吩衍生物

Family Cites Families (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4369172A (en) 1981-12-18 1983-01-18 Forest Laboratories Inc. Prolonged release therapeutic compositions based on hydroxypropylmethylcellulose
DE3583799D1 (de) 1985-01-11 1991-09-19 Abbott Lab Ltd Feste zubereitung mit langsamer freisetzung.
JP2773959B2 (ja) 1990-07-10 1998-07-09 信越化学工業株式会社 大腸内放出性固形製剤
UA73092C2 (uk) 1998-07-17 2005-06-15 Брістол-Майерс Сквібб Компані Таблетка з ентеросолюбільним покриттям і спосіб її приготування
WO2000006128A1 (fr) 1998-07-28 2000-02-10 Tanabe Seiyaku Co., Ltd. Preparation capable de liberer un medicament au niveau d'un site cible dans l'intestin
JP2000119271A (ja) * 1998-08-12 2000-04-25 Hokuriku Seiyaku Co Ltd １ｈ―イミダゾピリジン誘導体
US6461631B1 (en) 1999-11-16 2002-10-08 Atrix Laboratories, Inc. Biodegradable polymer composition
US6800663B2 (en) 2002-10-18 2004-10-05 Alkermes Controlled Therapeutics Inc. Ii, Crosslinked hydrogel copolymers
JP2007526324A (ja) 2004-03-02 2007-09-13 スミスクライン・ビーチャム・コーポレイション Ａｋｔ活性のある阻害剤
WO2013007768A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof as jak inhibitors
CN105001226B (zh) 2011-08-12 2017-09-08 日产化学工业株式会社 三环杂环化合物和jak抑制剂
WO2015061665A1 (en) 2013-10-24 2015-04-30 Abbvie Inc. Jak1 selective inhibitor and uses thereof
MA39987A (fr) 2014-04-30 2017-03-08 Incyte Corp Procédés de préparation d'un inhibiteur de jak1 et nouvelles formes associées
WO2015184305A1 (en) 2014-05-30 2015-12-03 Incyte Corporation TREATMENT OF CHRONIC NEUTROPHILIC LEUKEMIA (CNL) AND ATYPICAL CHRONIC MYELOID LEUKEMIA (aCML) BY INHIBITORS OF JAK1
CN113214278B (zh) 2016-10-03 2022-10-28 杭州高光制药有限公司 新型Jak1选择性抑制剂及其用途

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN101277963A (zh) * 2005-08-04 2008-10-01 西特里斯药业公司 作为sirtuin调节剂的噁唑并吡啶衍生物
CN102741253A (zh) * 2009-09-29 2012-10-17 艾科睿控股公司 PI3K(δ)选择性抑制剂
WO2012022045A1 (en) * 2010-08-20 2012-02-23 Hutchison Medipharma Limited Pyrrolopyrimidine compounds and uses thereof
CN103442568A (zh) * 2010-10-08 2013-12-11 Abbvie公司 呋喃并[3,2-d]嘧啶化合物
CN104918945A (zh) * 2012-11-01 2015-09-16 因赛特公司 作为jak抑制剂的三环稠合噻吩衍生物

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DK3509591T3 (da) 2021-12-20
HUE058120T2 (hu) 2022-07-28
RS62695B1 (sr) 2022-01-31
AU2017339417A1 (en) 2019-03-28
IL265358A (en) 2019-05-30
US10738060B2 (en) 2020-08-11
CN113214278A (zh) 2021-08-06
IL291265B2 (en) 2023-05-01
AU2017339417B2 (en) 2021-11-18
EP3509591B1 (en) 2021-11-17
IL291265B1 (en) 2023-01-01
CA3039178A1 (en) 2018-04-12
MX2019003649A (es) 2019-08-14
EP3509591A1 (en) 2019-07-17
MX390005B (es) 2025-03-20
IL291267B1 (en) 2023-01-01
US20190256523A1 (en) 2019-08-22
JP7089141B2 (ja) 2022-06-22
PT3509591T (pt) 2021-12-27
CN108366994B (zh) 2021-10-01
CN108366994A (zh) 2018-08-03
ES2901216T3 (es) 2022-03-21
IL291267B2 (en) 2023-05-01
AU2022201061B2 (en) 2023-03-16
KR102399848B1 (ko) 2022-05-19
JP2019537559A (ja) 2019-12-26
IL265358B (en) 2022-04-01
PL3509591T3 (pl) 2022-01-31
BR112019005969A2 (pt) 2019-06-18
AU2022201058A1 (en) 2022-03-10
USRE49834E1 (en) 2024-02-13
EP3509591A4 (en) 2020-03-25
AU2017339417C1 (en) 2022-06-02
IL291265A (en) 2022-05-01
HK1253040A1 (zh) 2019-06-06
AU2022201061A1 (en) 2022-03-10
KR20190057069A (ko) 2019-05-27
NZ751284A (en) 2022-09-30
IL291267A (en) 2022-05-01
HRP20211965T1 (hr) 2022-03-18
EA201990523A1 (ru) 2019-10-31
WO2018067422A1 (en) 2018-04-12
AU2022201058B2 (en) 2023-03-16

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