KR102317334B1 - NIK 억제제로서의 신규 1-(4-피리미디닐)-1H-피롤로[3,2-c]피리딘 유도체들 - Google Patents

NIK 억제제로서의 신규 1-(4-피리미디닐)-1H-피롤로[3,2-c]피리딘 유도체들 Download PDF

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KR102317334B1
KR102317334B1 KR1020167007899A KR20167007899A KR102317334B1 KR 102317334 B1 KR102317334 B1 KR 102317334B1 KR 1020167007899 A KR1020167007899 A KR 1020167007899A KR 20167007899 A KR20167007899 A KR 20167007899A KR 102317334 B1 KR102317334 B1 KR 102317334B1
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KR20160058814A (ko
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조지 하인드
패트리지아 티셀리
데이비드 에드워드 클락
야뉴스 죠제프 쿠라고프스키
칼럼 맥클레오드
사무엘 에드워드 만
테리 아론 판챨
스티븐 콜린 프라이스
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얀센 파마슈티카 엔.브이.
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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
    • 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
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond

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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)
  • Epidemiology (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)
KR1020167007899A 2013-09-26 2014-09-25 NIK 억제제로서의 신규 1-(4-피리미디닐)-1H-피롤로[3,2-c]피리딘 유도체들 Expired - Fee Related KR102317334B1 (ko)

Applications Claiming Priority (5)

Application Number Priority Date Filing Date Title
EP13186139 2013-09-26
EP13186139.5 2013-09-26
EP14176121 2014-07-08
EP14176121.3 2014-07-08
PCT/EP2014/070484 WO2015044267A1 (en) 2013-09-26 2014-09-25 NEW 1-(4-PYRIMIDINYL)-1H-PYRROLO[3,2-c]PYRIDINE DERIVATIVES AS NIK INHIBITORS

Publications (2)

Publication Number Publication Date
KR20160058814A KR20160058814A (ko) 2016-05-25
KR102317334B1 true KR102317334B1 (ko) 2021-10-26

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KR1020167007899A Expired - Fee Related KR102317334B1 (ko) 2013-09-26 2014-09-25 NIK 억제제로서의 신규 1-(4-피리미디닐)-1H-피롤로[3,2-c]피리딘 유도체들

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US (1) US10005773B2 (https=)
EP (1) EP3071566B1 (https=)
JP (1) JP6402179B2 (https=)
KR (1) KR102317334B1 (https=)
CN (1) CN105579451B (https=)
AU (1) AU2014327233B2 (https=)
BR (1) BR112016005914A2 (https=)
CA (1) CA2922753C (https=)
EA (1) EA029595B1 (https=)
ES (1) ES2804595T3 (https=)
IL (1) IL244706B (https=)
MX (1) MX373186B (https=)
TW (1) TWI704146B (https=)
WO (1) WO2015044267A1 (https=)

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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
AU2015334917B2 (en) 2014-10-23 2019-08-29 Janssen Pharmaceutica Nv New compounds as NIK inhibitors
JP6616412B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ.ベー. Nik阻害剤としての新規のピラゾロピリミジン誘導体
MX371151B (es) 2014-10-23 2020-01-20 Janssen Pharmaceutica Nv NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK).
BR112017008039B1 (pt) 2014-10-23 2023-04-11 Janssen Pharmaceutica N.V. Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende
EP3405464B1 (en) * 2016-01-22 2019-12-04 Janssen Pharmaceutica NV New 6-membered heteroaromatic substituted cyanoindoline derivatives as nik inhibitors
ES2775449T3 (es) 2016-01-22 2020-07-27 Janssen Pharmaceutica Nv Nuevos derivados de cianoindolina sustituida como inhibidores de nik
ES2837157T3 (es) 2016-06-30 2021-06-29 Janssen Pharmaceutica Nv Derivados de cianoindolina como inhibidores de NIK
WO2018002217A1 (en) 2016-06-30 2018-01-04 Janssen Pharmaceutica Nv Heteroaromatic derivatives as nik inhibitors
WO2018037059A1 (en) * 2016-08-24 2018-03-01 F. Hoffmann-La Roche Ag 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use
WO2018037058A1 (en) 2016-08-24 2018-03-01 F. Hoffmann-La Roche Ag 2-azabicyclo[3.1.0]hexan-3-one derivatives and methods of use
CN114222737B (zh) 2019-05-31 2024-07-26 詹森药业有限公司 NF-κB诱导激酶的小分子抑制剂
CN113816957B (zh) * 2021-10-29 2023-04-07 浙江工业大学 4-(7-氮杂吲哚)-2-氨基嘧啶类化合物及其应用

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WO2007058850A2 (en) 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
US20120214762A1 (en) 2011-03-16 2012-08-23 Genentech, Inc. 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
WO2005103003A2 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
DE102008005493A1 (de) 2008-01-22 2009-07-23 Merck Patent Gmbh 4-(Pyrrolo[2,3-c] pyridine-3-yl)-pyrimidin-2-yl-amin-derivate
CN102143746A (zh) 2008-07-03 2011-08-03 埃克塞利希斯股份有限公司 Cdk 调节剂
WO2010042337A1 (en) 2008-10-07 2010-04-15 Merck Sharp & Dohme Corp. Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity
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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
BR112017008039B1 (pt) 2014-10-23 2023-04-11 Janssen Pharmaceutica N.V. Derivados de pirazol como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende
AU2015334917B2 (en) 2014-10-23 2019-08-29 Janssen Pharmaceutica Nv New compounds as NIK inhibitors
MX371151B (es) 2014-10-23 2020-01-20 Janssen Pharmaceutica Nv NUEVOS DERIVADOS DE TIENOPIRIMIDINA EN CALIDAD DE INHIBIDORES DE LA CINASA INDUCTORA DE NF-kB (NIK).
JP6616412B2 (ja) 2014-10-23 2019-12-04 ヤンセン ファーマシューティカ エヌ.ベー. Nik阻害剤としての新規のピラゾロピリミジン誘導体

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WO2007058850A2 (en) 2005-11-10 2007-05-24 Smithkline Beecham Corporation Inhibitors of akt activity
WO2009158011A1 (en) 2008-06-26 2009-12-30 Amgen Inc. Alkynyl alcohols as kinase inhibitors
US20120214762A1 (en) 2011-03-16 2012-08-23 Genentech, Inc. 6,5-heterocyclic propargylic alcohol compounds and uses therefor

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Publication number Publication date
IL244706B (en) 2021-02-28
ES2804595T3 (es) 2021-02-08
WO2015044267A1 (en) 2015-04-02
JP2016531868A (ja) 2016-10-13
KR20160058814A (ko) 2016-05-25
TWI704146B (zh) 2020-09-11
CN105579451A (zh) 2016-05-11
MX373186B (es) 2020-05-12
EA201690645A1 (ru) 2016-08-31
IL244706A0 (en) 2016-04-21
CN105579451B (zh) 2017-10-27
JP6402179B2 (ja) 2018-10-10
EA029595B1 (ru) 2018-04-30
EP3071566B1 (en) 2020-04-15
MX2016003861A (es) 2016-07-26
CA2922753A1 (en) 2015-04-02
BR112016005914A2 (pt) 2017-08-01
EP3071566A1 (en) 2016-09-28
US20160257679A1 (en) 2016-09-08
CA2922753C (en) 2021-08-17
HK1224295A1 (zh) 2017-08-18
US10005773B2 (en) 2018-06-26
TW201602104A (zh) 2016-01-16
AU2014327233B2 (en) 2018-03-01
AU2014327233A1 (en) 2016-03-10

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