JP2016531868A5 - - Google Patents
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- Publication number
- JP2016531868A5 JP2016531868A5 JP2016517332A JP2016517332A JP2016531868A5 JP 2016531868 A5 JP2016531868 A5 JP 2016531868A5 JP 2016517332 A JP2016517332 A JP 2016517332A JP 2016517332 A JP2016517332 A JP 2016517332A JP 2016531868 A5 JP2016531868 A5 JP 2016531868A5
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- JP
- Japan
- Prior art keywords
- group
- alkyl
- substituted
- hydrogen atom
- het
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
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- 125000000217 alkyl group Chemical group 0.000 claims 110
- 125000001153 fluoro group Chemical group F* 0.000 claims 67
- 125000004435 hydrogen atoms Chemical group [H]* 0.000 claims 66
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 46
- 125000001424 substituent group Chemical group 0.000 claims 43
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 30
- 229910052731 fluorine Inorganic materials 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 23
- 125000003386 piperidinyl group Chemical group 0.000 claims 20
- 125000002393 azetidinyl group Chemical group 0.000 claims 19
- 125000004193 piperazinyl group Chemical group 0.000 claims 18
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 18
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 15
- 125000000623 heterocyclic group Chemical group 0.000 claims 14
- 125000002757 morpholinyl group Chemical group 0.000 claims 14
- 125000003566 oxetanyl group Chemical group 0.000 claims 14
- 125000001412 tetrahydropyranyl group Chemical group 0.000 claims 14
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 claims 13
- 150000001875 compounds Chemical class 0.000 claims 12
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 11
- 125000005843 halogen group Chemical group 0.000 claims 11
- 125000003545 alkoxy group Chemical group 0.000 claims 9
- 238000006467 substitution reaction Methods 0.000 claims 7
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 125000004432 carbon atoms Chemical group C* 0.000 claims 6
- 125000000842 isoxazolyl group Chemical group 0.000 claims 5
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- 229910052757 nitrogen Inorganic materials 0.000 claims 4
- 125000004433 nitrogen atoms Chemical group N* 0.000 claims 4
- 125000000335 thiazolyl group Chemical group 0.000 claims 4
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims 3
- -1 Het 6 Chemical group 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000001786 isothiazolyl group Chemical group 0.000 claims 3
- 125000002971 oxazolyl group Chemical group 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000002098 pyridazinyl group Chemical group 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000001544 thienyl group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000011780 sodium chloride Substances 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- WYURNTSHIVDZCO-UHFFFAOYSA-N tetrahydrofuran Chemical compound C1CCOC1 WYURNTSHIVDZCO-UHFFFAOYSA-N 0.000 claims 2
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000002062 proliferating Effects 0.000 claims 1
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP13186139 | 2013-09-26 | ||
EP13186139.5 | 2013-09-26 | ||
EP14176121.3 | 2014-07-08 | ||
EP14176121 | 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 (3)
Publication Number | Publication Date |
---|---|
JP2016531868A JP2016531868A (ja) | 2016-10-13 |
JP2016531868A5 true JP2016531868A5 (US07794700-20100914-C00152.png) | 2017-11-02 |
JP6402179B2 JP6402179B2 (ja) | 2018-10-10 |
Family
ID=51619194
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
JP2016517332A Active JP6402179B2 (ja) | 2013-09-26 | 2014-09-25 | 新規な、NIK阻害剤としての1−(4−ピリミジニル)−1H−ピロロ[3,2−c]ピリジン誘導体 |
Country Status (15)
Families Citing this family (15)
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 |
BR112017008045A2 (pt) | 2014-10-23 | 2017-12-19 | Janssen Pharmaceutica Nv | compostos como inibidores de nik |
CA2960574C (en) | 2014-10-23 | 2023-03-07 | Janssen Pharmaceutica Nv | Pyrazolopyrimidine derivatives as nik inhibitors |
US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
BR112017007715B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de tienopirimidina 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 |
CN108697710B (zh) | 2016-01-22 | 2022-02-18 | 杨森制药有限公司 | 作为nik抑制剂的新颖的经取代的氰基吲哚啉衍生物 |
WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
ES2805976T3 (es) | 2016-06-30 | 2021-02-16 | Janssen Pharmaceutica Nv | Derivados heteroaromáticos en calidad de inhibidores de NIK |
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 |
CN109863142B (zh) * | 2016-08-24 | 2022-06-10 | 豪夫迈·罗氏有限公司 | 2-氮杂双环[3.1.0]己烷-3-酮衍生物及使用方法 |
UY38721A (es) | 2019-05-31 | 2020-11-30 | Janssen Pharmaceutica Nv | INHIBIDORES DE MOLÉCULAS PEQUEÑAS DE QUINASA INDUCTORA DE NF-kB |
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 |
Family Cites Families (17)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
BRPI0510319A (pt) | 2004-04-26 | 2007-10-16 | Pfizer | inibidores da enzima integrase de hiv |
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 |
US20110086834A1 (en) | 2008-06-26 | 2011-04-14 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
AU2009266806A1 (en) * | 2008-07-03 | 2010-01-07 | Exelixis Inc. | CDK modulators |
US20110183975A1 (en) * | 2008-10-07 | 2011-07-28 | Yasuhiro Goto | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
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 |
TW201247650A (en) * | 2011-03-16 | 2012-12-01 | Hoffmann La Roche | 6,5-heterocyclic propargylic alcohol compounds and uses therefor |
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 |
BR112017007715B1 (pt) | 2014-10-23 | 2023-04-11 | Janssen Pharmaceutica N.V. | Derivados de tienopirimidina como inibidores de nik, seu uso no tratamento ou prevenção de câncer e composição farmacêutica que os compreende |
BR112017008045A2 (pt) | 2014-10-23 | 2017-12-19 | Janssen Pharmaceutica Nv | compostos como inibidores de nik |
CA2960574C (en) | 2014-10-23 | 2023-03-07 | Janssen Pharmaceutica Nv | Pyrazolopyrimidine derivatives as nik inhibitors |
US9981962B2 (en) | 2014-10-23 | 2018-05-29 | Janssen Pharmaceutica Nv | Pyrazole derivatives as NIK inhibitors |
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2014
- 2014-09-24 TW TW103132898A patent/TWI704146B/zh not_active IP Right Cessation
- 2014-09-25 US US15/024,603 patent/US10005773B2/en active Active
- 2014-09-25 JP JP2016517332A patent/JP6402179B2/ja active Active
- 2014-09-25 EP EP14772372.0A patent/EP3071566B1/en active Active
- 2014-09-25 ES ES14772372T patent/ES2804595T3/es active Active
- 2014-09-25 EA EA201690645A patent/EA029595B1/ru not_active IP Right Cessation
- 2014-09-25 MX MX2016003861A patent/MX2016003861A/es active IP Right Grant
- 2014-09-25 KR KR1020167007899A patent/KR102317334B1/ko active IP Right Grant
- 2014-09-25 CN CN201480052786.XA patent/CN105579451B/zh active Active
- 2014-09-25 BR BR112016005914A patent/BR112016005914A2/pt not_active Application Discontinuation
- 2014-09-25 AU AU2014327233A patent/AU2014327233B2/en not_active Ceased
- 2014-09-25 WO PCT/EP2014/070484 patent/WO2015044267A1/en active Application Filing
- 2014-09-25 CA CA2922753A patent/CA2922753C/en active Active
-
2016
- 2016-03-22 IL IL244706A patent/IL244706B/en active IP Right Grant
- 2016-11-04 HK HK16112697.3A patent/HK1224295A1/zh not_active IP Right Cessation