CN108366994B - 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
CN108366994B
CN108366994B CN201780004442.5A CN201780004442A CN108366994B CN 108366994 B CN108366994 B CN 108366994B CN 201780004442 A CN201780004442 A CN 201780004442A CN 108366994 B CN108366994 B CN 108366994B
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compound
disease
equiv
imidazo
pyridin
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CN108366994A (zh
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梁从新
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Guangzhou Gao Ling Pharmaceutical Co ltd
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Hangzhou Gaoguang Pharmaceutical Co ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/12Heterocyclic 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
    • C07D491/14Ortho-condensed systems
    • C07D491/147Ortho-condensed systems the condensed system containing one ring with oxygen as ring hetero atom and two rings with nitrogen as ring hetero atom
    • 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
    • A61K31/41Heterocyclic 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
    • A61K31/4151,2-Diazoles
    • A61K31/41551,2-Diazoles non condensed and containing further heterocyclic 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • 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
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • 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
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D211/00Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/02Heterocyclic 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
    • C07D491/04Ortho-condensed systems
    • C07D491/044Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C07D491/048Ortho-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)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (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)
CN201780004442.5A 2016-10-03 2017-09-30 新型Jak1选择性抑制剂及其用途 Active CN108366994B (zh)

Priority Applications (1)

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CN202110514751.5A CN113214278B (zh) 2016-10-03 2017-09-30 新型Jak1选择性抑制剂及其用途

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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

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EP (1) EP3509591B1 (enExample)
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CN (2) CN108366994B (enExample)
AU (3) AU2017339417C1 (enExample)
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EA (1) EA201990523A1 (enExample)
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HR (1) HRP20211965T1 (enExample)
HU (1) HUE058120T2 (enExample)
IL (3) IL265358B (enExample)
MX (1) MX390005B (enExample)
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PL (1) PL3509591T3 (enExample)
PT (1) PT3509591T (enExample)
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WO (1) WO2018067422A1 (enExample)

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HUE058120T2 (hu) 2016-10-03 2022-07-28 Highlightll Pharmaceutical Hainan Co Ltd Új JAK1-szelektív inhibitorok és alkalmazásuk
PL3568396T3 (pl) * 2017-01-11 2021-05-31 Leo Pharma A/S Nowe pochodne aminoimidazopirydyny jako inhibitory kinaz janusowych i ich zastosowanie farmaceutyczne
CN113490484B (zh) 2018-10-31 2024-08-23 因赛特公司 治疗血液疾病的组合疗法
JP2022524997A (ja) 2019-03-05 2022-05-11 インサイト・コーポレイション 慢性肺同種移植片機能不全の治療のためのjak1経路阻害剤
US11624751B2 (en) 2019-03-19 2023-04-11 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
KR102785014B1 (ko) * 2019-06-06 2025-03-20 항저우 하이라이트엘엘 파마슈티컬 씨오., 엘티디. 푸로이미다조피리딘 화합물의 합성 방법, 푸로이미다조피리딘 화합물의 결정 형태, 및 그의 염의 결정 형태
BR112022023550A2 (pt) 2020-05-19 2023-01-03 Bayer Cropscience Ag (tio)amidas azabicíclicas como compostos fungicidas
WO2021249995A1 (en) 2020-06-10 2021-12-16 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
IL313097A (en) * 2021-09-13 2024-07-01 Hangzhou Highlightll Pharmaceutical Co Ltd Methods of treating cns disorders
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)

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AU2022201058A1 (en) 2022-03-10
IL291267A (en) 2022-05-01
NZ751284A (en) 2022-09-30
EP3509591B1 (en) 2021-11-17
AU2022201061A1 (en) 2022-03-10
WO2018067422A1 (en) 2018-04-12
PT3509591T (pt) 2021-12-27
EP3509591A1 (en) 2019-07-17
BR112019005969A2 (pt) 2019-06-18
PL3509591T3 (pl) 2022-01-31
IL291267B2 (en) 2023-05-01
DK3509591T3 (da) 2021-12-20
AU2022201061B2 (en) 2023-03-16
MX2019003649A (es) 2019-08-14
CA3039178A1 (en) 2018-04-12
AU2017339417C1 (en) 2022-06-02
RS62695B1 (sr) 2022-01-31
KR20190057069A (ko) 2019-05-27
HK1253040A1 (zh) 2019-06-06
ES2901216T3 (es) 2022-03-21
EA201990523A1 (ru) 2019-10-31
CN113214278B (zh) 2022-10-28
HRP20211965T1 (hr) 2022-03-18
AU2017339417A1 (en) 2019-03-28
US10738060B2 (en) 2020-08-11
IL265358B (en) 2022-04-01
CN108366994A (zh) 2018-08-03
USRE49834E1 (en) 2024-02-13
AU2017339417B2 (en) 2021-11-18
IL291265B2 (en) 2023-05-01
AU2022201058B2 (en) 2023-03-16
IL291267B1 (en) 2023-01-01
HUE058120T2 (hu) 2022-07-28
CN113214278A (zh) 2021-08-06
US20190256523A1 (en) 2019-08-22
KR102399848B1 (ko) 2022-05-19
EP3509591A4 (en) 2020-03-25
JP7089141B2 (ja) 2022-06-22
IL291265A (en) 2022-05-01
MX390005B (es) 2025-03-20
IL291265B1 (en) 2023-01-01
JP2019537559A (ja) 2019-12-26
IL265358A (en) 2019-05-30

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