TWI760419B - 作為酪胺酸蛋白激酶抑制劑之新穎的胺基-咪唑并吡啶衍生物及其醫藥用途 - Google Patents

作為酪胺酸蛋白激酶抑制劑之新穎的胺基-咪唑并吡啶衍生物及其醫藥用途 Download PDF

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TWI760419B
TWI760419B TW107101035A TW107101035A TWI760419B TW I760419 B TWI760419 B TW I760419B TW 107101035 A TW107101035 A TW 107101035A TW 107101035 A TW107101035 A TW 107101035A TW I760419 B TWI760419 B TW I760419B
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acetonitrile
cyclohexyl
imidazo
compound
trans
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TW107101035A
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Chinese (zh)
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TW201829407A (zh
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珍斯 豪蘭德 拉森
摩根斯 拉森
拉斯 齊恩 拉斯穆森
安卓利亞 里茲恩
汀 杜斯
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丹麥商理奧藥品公司
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • 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
    • 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
    • A61P37/08Antiallergic agents
    • 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

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  • 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)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Immunology (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
TW107101035A 2017-01-11 2018-01-11 作為酪胺酸蛋白激酶抑制劑之新穎的胺基-咪唑并吡啶衍生物及其醫藥用途 TWI760419B (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
??17151020.9 2017-01-11
EP17151020.9 2017-01-11
EP17151020 2017-01-11

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TW201829407A TW201829407A (zh) 2018-08-16
TWI760419B true TWI760419B (zh) 2022-04-11

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US (1) US10703751B2 (enExample)
EP (1) EP3568396B1 (enExample)
JP (1) JP7009504B2 (enExample)
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CN (1) CN110167938B (enExample)
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RS (1) RS61317B1 (enExample)
RU (1) RU2019125177A (enExample)
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UA (1) UA123972C2 (enExample)
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JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
ES2922379T3 (es) 2016-12-16 2022-09-14 Janssen Pharmaceutica Nv Compuestos de imidazo[4,5,D]pirrolo[2,3,B]piridina como inhibidores de Janus quinasas
TW202016110A (zh) 2018-06-15 2020-05-01 比利時商健生藥品公司 Jak激酶家族之小分子抑制劑
WO2020007698A1 (en) * 2018-07-06 2020-01-09 Leo Pharma A/S Novel amino-imidazopyrimidine derivatives as janus kinase inhibitors and pharmaceutical use thereof
WO2021040502A1 (ko) * 2019-08-30 2021-03-04 주식회사 티에스디라이프사이언스 이미다조피리딘 유도체 및 이를 유효성분으로 함유하는 약학적 조성물
AU2022233254A1 (en) 2021-03-11 2023-10-26 Janssen Pharmaceutica Nv Lorpucitinib for use in the treatment of jak mediated disorders
CN119569971B (zh) * 2025-02-07 2025-05-27 吉林大学 一种用于蛋白质磷酸化和棕榈酰化修饰同时筛选的Janus材料的制备方法

Citations (2)

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WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
EP2518071A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors

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CN101981033B (zh) * 2008-02-06 2015-02-04 百时美施贵宝公司 用作激酶抑制剂的取代的咪唑并哒嗪化合物
CN103168032A (zh) * 2010-08-05 2013-06-19 安美基公司 抑制间变性淋巴瘤激酶的苯并咪唑和氮杂苯并咪唑化合物
EP2527344A1 (en) 2011-05-25 2012-11-28 Almirall, S.A. Pyridin-2(1H)-one derivatives useful as medicaments for the treatment of myeloproliferative disorders, transplant rejection, immune-mediated and inflammatory diseases
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
WO2013007765A1 (en) 2011-07-13 2013-01-17 F. Hoffmann-La Roche Ag Fused tricyclic compounds for use as inhibitors of janus kinases
UY34615A (es) 2012-02-10 2013-09-30 Galapagos Nv Nuevos compuestos útiles para el tratamiento de enfermedades degenerativas e inflamatorias.
CA2888816A1 (en) 2012-11-01 2014-05-08 Incyte Corporation Tricyclic fused thiophene derivatives as jak inhibitors
CN104955824B (zh) * 2012-11-20 2017-09-22 豪夫迈·罗氏有限公司 作为含t790m的egfr突变体的抑制剂的氨基嘧啶化合物
CN104098563A (zh) 2013-04-02 2014-10-15 山东亨利医药科技有限责任公司 Jnk抑制剂化合物
CR20160553A (es) 2014-04-30 2017-04-25 Incyte Corp Procesos para preparar un inhibidor de jak1 y nuevas formas de este
MX390005B (es) 2016-10-03 2025-03-20 Hangzhou Highlightll Pharmaceutical Co Ltd Inhibidores selectivos de jak1 novedosos y usos de los mismos.
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز

Patent Citations (2)

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WO2011086053A1 (en) * 2010-01-12 2011-07-21 F. Hoffmann-La Roche Ag Tricyclic heterocyclic compounds, compositions and methods of use thereof
EP2518071A1 (en) * 2011-04-29 2012-10-31 Almirall, S.A. Imidazopyridine derivatives as PI3K inhibitors

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US10703751B2 (en) 2020-07-07
US20190367512A1 (en) 2019-12-05
ES2846741T3 (es) 2021-07-29
RU2019125177A (ru) 2021-02-15
ZA201904190B (en) 2020-10-28
KR102548543B1 (ko) 2023-06-29
TW201829407A (zh) 2018-08-16
PL3568396T3 (pl) 2021-05-31
JP7009504B2 (ja) 2022-01-25
HRP20210095T1 (hr) 2021-03-05
MX2019008331A (es) 2020-01-14
JP2020504186A (ja) 2020-02-06
RU2019125177A3 (enExample) 2021-05-11
CN110167938A (zh) 2019-08-23
PT3568396T (pt) 2021-02-09
AU2018208516B2 (en) 2021-07-08
NZ754922A (en) 2025-11-28
RS61317B1 (sr) 2021-02-26
CA3045567A1 (en) 2018-07-19
MX389378B (es) 2025-03-20
EP3568396A1 (en) 2019-11-20
CN110167938B (zh) 2024-06-14
SI3568396T1 (sl) 2021-04-30
IL267829A (en) 2019-09-26
BR112019014191A2 (pt) 2020-02-11
DK3568396T3 (da) 2021-01-18
IL267829B (en) 2022-02-01
EP3568396B1 (en) 2020-11-11
WO2018130563A1 (en) 2018-07-19
MY195576A (en) 2023-02-02
HUE052720T2 (hu) 2021-05-28
CY1123864T1 (el) 2022-05-27
AU2018208516A1 (en) 2019-07-11
UA123972C2 (uk) 2021-06-30
KR20190103231A (ko) 2019-09-04
LT3568396T (lt) 2021-02-10

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