TWI627173B - 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 - Google Patents

作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 Download PDF

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Publication number
TWI627173B
TWI627173B TW103132895A TW103132895A TWI627173B TW I627173 B TWI627173 B TW I627173B TW 103132895 A TW103132895 A TW 103132895A TW 103132895 A TW103132895 A TW 103132895A TW I627173 B TWI627173 B TW I627173B
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alkyl
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substituted
hydrogen
het
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TW103132895A
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TW201602103A (zh
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喬治 海德
派特里其亞 帝塞立
愛德華 克勒可
亞努茲 克拉谷威士奇
加勒 麥克勞德
沙姆爾 曼恩
法比安 路塞爾
史帝分 普賴斯
約翰 蒙大拿
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比利時商健生藥品公司
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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
    • 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
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B59/00Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
    • C07B59/002Heterocyclic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/05Isotopically modified compounds, e.g. labelled

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Epidemiology (AREA)
TW103132895A 2013-09-26 2014-09-24 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物 TWI627173B (zh)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
??13186148.6 2013-09-26
EP13186148 2013-09-26
??14176125.4 2014-07-08
EP14176125 2014-07-08

Publications (2)

Publication Number Publication Date
TW201602103A TW201602103A (zh) 2016-01-16
TWI627173B true TWI627173B (zh) 2018-06-21

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TW103132895A TWI627173B (zh) 2013-09-26 2014-09-24 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物

Country Status (14)

Country Link
US (1) US9981963B2 (enExample)
EP (1) EP3049412B1 (enExample)
JP (1) JP6404332B2 (enExample)
KR (1) KR102317335B1 (enExample)
CN (1) CN105579452B (enExample)
AU (1) AU2014327235B2 (enExample)
BR (1) BR112016006232B1 (enExample)
CA (1) CA2922633C (enExample)
EA (1) EA028101B1 (enExample)
ES (1) ES2643070T3 (enExample)
IL (1) IL244702B (enExample)
MX (1) MX365739B (enExample)
TW (1) TWI627173B (enExample)
WO (1) WO2015044269A1 (enExample)

Families Citing this family (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI663166B (zh) 2013-04-24 2019-06-21 健生藥品公司 新化合物
TWI704146B (zh) 2013-09-26 2020-09-11 比利時商健生藥品公司 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物
TWI627173B (zh) 2013-09-26 2018-06-21 比利時商健生藥品公司 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物
US10323045B2 (en) 2014-10-23 2019-06-18 Janssen Pharmaceutica Nv Thienopyrimidine derivatives as NIK inhibitors
KR102499862B1 (ko) * 2014-10-23 2023-02-13 얀센 파마슈티카 엔.브이. Nik 억제제로서의 신규 피라졸 유도체
ES2718557T3 (es) 2014-10-23 2019-07-02 Janssen Pharmaceutica Nv Nuevos compuestos como inhibidores de nik
EP3209663B1 (en) 2014-10-23 2018-12-12 Janssen Pharmaceutica N.V. New pyrazolopyrimidine derivatives as nik inhibitors
EP3383390A4 (en) * 2015-12-02 2019-11-20 Astraea Therapeutics, LLC PIPERIDINYL-nociceptin RECEPTOR COMPOUNDS
US10112924B2 (en) 2015-12-02 2018-10-30 Astraea Therapeutics, Inc. Piperdinyl nociceptin receptor compounds
KR102720461B1 (ko) 2016-01-22 2024-10-21 잔센파마슈티카엔.브이. Nik 억제제로서의 신규 6원 헤테로방향족 치환된 시아노인돌린 유도체
SI3405196T1 (sl) 2016-01-22 2020-03-31 Janssen Pharmaceutica Nv Novi substituirani derivati cianoindolina kot inhibitorji NIK
CA3027416A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Heteroaromatic derivatives as nik inhibitors
ES2837157T3 (es) 2016-06-30 2021-06-29 Janssen Pharmaceutica Nv Derivados de cianoindolina como inhibidores de NIK
WO2020162638A1 (ja) * 2019-02-08 2020-08-13 学校法人近畿大学 悪性腫瘍疾患の改善用組成物
RS66105B1 (sr) 2019-05-31 2024-11-29 Janssen Pharmaceutica Nv Inhibitori malih molekula nf-kb koji indukuju kinazu
CN110156766A (zh) * 2019-06-04 2019-08-23 南京工业大学 一种银催化的氘代五元芳香杂环化合物的制备方法
JPWO2022138735A1 (enExample) 2020-12-22 2022-06-30
TW202402269A (zh) * 2022-05-26 2024-01-16 大陸商迪哲(江蘇)醫藥股份有限公司 ROCK(Rho相關激酶)抑制劑及其用途
EP4566599A1 (en) 2022-08-02 2025-06-11 Kinki University Pharmaceutical composition for ameliorating allergic diseases

Citations (3)

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WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
WO2010042337A1 (en) * 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
WO2012123522A1 (en) * 2011-03-16 2012-09-20 F. Hoffmann-La Roche Ag 6,5-heterocyclic propargylic alcohol compounds and uses therefor

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JP3990061B2 (ja) * 1998-01-05 2007-10-10 エーザイ・アール・アンド・ディー・マネジメント株式会社 プリン誘導体および糖尿病の予防・治療剤としてのアデノシンa2受容体拮抗剤
DE19948417A1 (de) * 1999-10-07 2001-04-19 Morphochem Ag Imidazol-Derivate und ihre Verwendung als Arzneimittel
CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
AR056786A1 (es) * 2005-11-10 2007-10-24 Smithkline Beecham Corp Compuesto de 1h- imidazo ( 4,5-c) piridin-2-ilo, composicion farmaceutica que lo comprende, procedimiento para preparar dicha composicion, su uso para preparar unmedicamento, uso de una combinacion que omprende al compuesto y al menos un agente antineoplasico para preparar un medicamento y dicha com
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
WO2010003133A2 (en) 2008-07-03 2010-01-07 Exelixis Inc. Cdk modulators
CN101723936B (zh) 2008-10-27 2014-01-15 上海睿星基因技术有限公司 激酶抑制剂及其在药学中的用途
WO2011050245A1 (en) 2009-10-23 2011-04-28 Yangbo Feng Bicyclic heteroaryls as kinase inhibitors
TWI663166B (zh) * 2013-04-24 2019-06-21 健生藥品公司 新化合物
TWI627173B (zh) 2013-09-26 2018-06-21 比利時商健生藥品公司 作為NIK抑制劑的新穎3-(1H-吡唑-4-基)-1H-吡咯并[2,3-c]吡啶衍生物
TWI704146B (zh) * 2013-09-26 2020-09-11 比利時商健生藥品公司 用作NIK抑制劑之新的1-(4-嘧啶基)-1H-吡唑並[3,2-c]吡啶衍生物
EP3209663B1 (en) 2014-10-23 2018-12-12 Janssen Pharmaceutica N.V. New pyrazolopyrimidine derivatives as nik inhibitors
US10323045B2 (en) 2014-10-23 2019-06-18 Janssen Pharmaceutica Nv Thienopyrimidine derivatives as NIK inhibitors
KR102499862B1 (ko) 2014-10-23 2023-02-13 얀센 파마슈티카 엔.브이. Nik 억제제로서의 신규 피라졸 유도체
ES2718557T3 (es) 2014-10-23 2019-07-02 Janssen Pharmaceutica Nv Nuevos compuestos como inhibidores de nik

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009158011A1 (en) * 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
WO2010042337A1 (en) * 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
WO2012123522A1 (en) * 2011-03-16 2012-09-20 F. Hoffmann-La Roche Ag 6,5-heterocyclic propargylic alcohol compounds and uses therefor

Also Published As

Publication number Publication date
IL244702A0 (en) 2016-04-21
EA028101B1 (ru) 2017-10-31
BR112016006232B1 (pt) 2022-11-29
US9981963B2 (en) 2018-05-29
EP3049412A1 (en) 2016-08-03
KR20160060054A (ko) 2016-05-27
BR112016006232A2 (pt) 2017-08-01
JP2016531858A (ja) 2016-10-13
CA2922633A1 (en) 2015-04-02
AU2014327235B2 (en) 2018-02-08
ES2643070T3 (es) 2017-11-21
MX365739B (es) 2019-06-12
CA2922633C (en) 2022-07-26
AU2014327235A1 (en) 2016-03-17
JP6404332B2 (ja) 2018-10-10
CN105579452A (zh) 2016-05-11
EA201690657A1 (ru) 2016-08-31
CN105579452B (zh) 2018-01-23
KR102317335B1 (ko) 2021-10-26
TW201602103A (zh) 2016-01-16
US20160229851A1 (en) 2016-08-11
EP3049412B1 (en) 2017-07-12
MX2016003863A (es) 2016-08-04
WO2015044269A1 (en) 2015-04-02
IL244702B (en) 2019-07-31

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