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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Publication number
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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Taiwan
Prior art keywords
acetonitrile
cyclohexyl
imidazo
compound
trans
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TW107101035A
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English (en)
Chinese (zh)
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TW201829407A (zh
Inventor
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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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—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
    • A61K31/435—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
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • A61P37/08—Antiallergic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs 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)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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
EP17151020 2017-01-11
EP17151020.9 2017-01-11
??17151020.9 2017-01-11

Publications (2)

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

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TW107101035A TWI760419B (zh) 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

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US (1) US10703751B2 (enExample)
EP (1) EP3568396B1 (enExample)
JP (1) JP7009504B2 (enExample)
KR (1) KR102548543B1 (enExample)
CN (1) CN110167938B (enExample)
AU (1) AU2018208516B2 (enExample)
CA (1) CA3045567A1 (enExample)
CY (1) CY1123864T1 (enExample)
DK (1) DK3568396T3 (enExample)
ES (1) ES2846741T3 (enExample)
HR (1) HRP20210095T1 (enExample)
HU (1) HUE052720T2 (enExample)
IL (1) IL267829B (enExample)
LT (1) LT3568396T (enExample)
MX (1) MX389378B (enExample)
MY (1) MY195576A (enExample)
PL (1) PL3568396T3 (enExample)
PT (1) PT3568396T (enExample)
RS (1) RS61317B1 (enExample)
RU (1) RU2019125177A (enExample)
SI (1) SI3568396T1 (enExample)
TW (1) TWI760419B (enExample)
UA (1) UA123972C2 (enExample)
WO (1) WO2018130563A1 (enExample)
ZA (1) ZA201904190B (enExample)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز
MX2022004474A (es) 2016-12-16 2023-08-15 Janssen Pharmaceutica Nv Inhibidores de moléculas pequeñas de la familia de quinasas jak.
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
JP7345220B2 (ja) * 2019-08-30 2023-09-15 ティーエスディー ライフ サイエンス カンパニー リミテッド イミダゾピリジン誘導体及びこれを有効成分として含有する薬学的組成物
US12390451B2 (en) 2021-03-11 2025-08-19 Janssen Pharmaceutica Nv Small molecule inhibitor of the JAK family of kinases
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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WO2009100375A1 (en) * 2008-02-06 2009-08-13 Bristol-Myers Squibb Company Substituted imidazopyridazines useful as kinase inhibitors
SG10201505997TA (en) * 2010-08-05 2015-09-29 Amgen Inc Benzimidazole And Azabenzimidazole Compounds That Inhibit Anaplastic Lymphoma Kinase
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
UY34616A (es) 2012-02-10 2013-09-30 Galapagos Nv Nuevo compuesto útil 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
EP3181564B1 (en) * 2012-11-20 2019-09-18 H. Hoffnabb-La Roche Ag Aminopyrimidine compounds as inhibitors of t790m containing egfr mutants
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
SG11201609016VA (en) 2014-04-30 2016-11-29 Incyte Corp Processes of preparing a jak1 inhibitor and new forms thereto
EA201990523A1 (ru) 2016-10-03 2019-10-31 НОВЫЕ СЕЛЕКТИВНЫЕ ИНГИБИТОРЫ Jak1 И ИХ ПРИМЕНЕНИЕ
JOP20190144A1 (ar) 2016-12-16 2019-06-16 Janssen Pharmaceutica Nv إيميدازو بيرولو بيريدين كمثبطات لعائلة jak الخاصة بإنزيمات الكيناز

Patent Citations (2)

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

Also Published As

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

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