JP2019504067A5 - - Google Patents
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- Publication number
- JP2019504067A5 JP2019504067A5 JP2018535876A JP2018535876A JP2019504067A5 JP 2019504067 A5 JP2019504067 A5 JP 2019504067A5 JP 2018535876 A JP2018535876 A JP 2018535876A JP 2018535876 A JP2018535876 A JP 2018535876A JP 2019504067 A5 JP2019504067 A5 JP 2019504067A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- substituted
- group
- cycloalkyl
- 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.)
- Granted
Links
- 125000000217 alkyl group Chemical group 0.000 claims 185
- 125000001424 substituent group Chemical group 0.000 claims 58
- 125000005843 halogen group Chemical group 0.000 claims 35
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 35
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 33
- 229910052739 hydrogen Inorganic materials 0.000 claims 31
- 239000001257 hydrogen Substances 0.000 claims 31
- 125000004432 carbon atom Chemical group C* 0.000 claims 22
- 150000001875 compounds Chemical class 0.000 claims 20
- 229910052717 sulfur Inorganic materials 0.000 claims 20
- 229910052799 carbon Inorganic materials 0.000 claims 19
- 125000005842 heteroatom Chemical group 0.000 claims 17
- 229910052760 oxygen Inorganic materials 0.000 claims 17
- 125000004093 cyano group Chemical group *C#N 0.000 claims 15
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 15
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 13
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- -1 3,6-dihydro-2H-pyran-4-yl Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 239000012453 solvate Substances 0.000 claims 6
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 5
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 125000003003 spiro group Chemical group 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 3
- 150000002431 hydrogen Chemical class 0.000 claims 3
- 210000003719 b-lymphocyte Anatomy 0.000 claims 2
- 230000036210 malignancy Effects 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000002950 monocyclic group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 230000002265 prevention Effects 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 208000002250 Hematologic Neoplasms Diseases 0.000 claims 1
- 208000017604 Hodgkin disease Diseases 0.000 claims 1
- 208000021519 Hodgkin lymphoma Diseases 0.000 claims 1
- 208000010747 Hodgkins lymphoma Diseases 0.000 claims 1
- 208000031671 Large B-Cell Diffuse Lymphoma Diseases 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 125000005037 alkyl phenyl group Chemical group 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010012818 diffuse large B-cell lymphoma Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 125000000896 monocarboxylic acid group Chemical group 0.000 claims 1
- 230000002062 proliferating effect Effects 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16152416.0 | 2016-01-22 | ||
| EP16152416 | 2016-01-22 | ||
| EP16159651 | 2016-03-10 | ||
| EP16159651.5 | 2016-03-10 | ||
| PCT/EP2017/051150 WO2017125530A1 (en) | 2016-01-22 | 2017-01-20 | New substituted cyanoindoline derivatives as nik inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019504067A JP2019504067A (ja) | 2019-02-14 |
| JP2019504067A5 true JP2019504067A5 (OSRAM) | 2020-03-05 |
| JP6910359B2 JP6910359B2 (ja) | 2021-07-28 |
Family
ID=57868252
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018535876A Active JP6910359B2 (ja) | 2016-01-22 | 2017-01-20 | Ｎｉｋ阻害剤としての新たな置換されたシアノインドリン誘導体 |
Country Status (20)
| Country | Link |
|---|---|
| US (1) | US11180487B2 (OSRAM) |
| EP (1) | EP3405196B1 (OSRAM) |
| JP (1) | JP6910359B2 (OSRAM) |
| KR (1) | KR102784966B1 (OSRAM) |
| CN (1) | CN108697710B (OSRAM) |
| AU (1) | AU2017209935B2 (OSRAM) |
| BR (1) | BR112018014675B1 (OSRAM) |
| CA (1) | CA3011880A1 (OSRAM) |
| DK (1) | DK3405196T3 (OSRAM) |
| ES (1) | ES2775449T3 (OSRAM) |
| HR (1) | HRP20200133T1 (OSRAM) |
| HU (1) | HUE047684T2 (OSRAM) |
| IL (1) | IL260500B (OSRAM) |
| LT (1) | LT3405196T (OSRAM) |
| MX (1) | MX2018008974A (OSRAM) |
| PH (1) | PH12018501567A1 (OSRAM) |
| SI (1) | SI3405196T1 (OSRAM) |
| TW (1) | TWI739783B (OSRAM) |
| WO (1) | WO2017125530A1 (OSRAM) |
| ZA (1) | ZA201804688B (OSRAM) |
Families Citing this family (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2017125530A1 (en) | 2016-01-22 | 2017-07-27 | Janssen Pharmaceutica Nv | New substituted cyanoindoline derivatives as nik inhibitors |
| CN109311846B (zh) | 2016-01-22 | 2021-03-19 | 杨森制药有限公司 | 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物 |
| CN109641882B (zh) | 2016-06-30 | 2022-10-28 | 杨森制药有限公司 | 作为nik抑制剂的杂芳族衍生物 |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| EP3492462B1 (en) * | 2016-07-26 | 2023-08-30 | Shenzhen TargetRx, Inc. | Amino pyrimidine compound for inhibiting protein tyrosine kinase activity |
| EA202090888A1 (ru) | 2017-09-30 | 2021-01-27 | Шанхай Хайхэ Фармасьютикал Ко., Лтд. | Соединение, обладающее активностью по ингибированию erk киназы, и его применение |
| TW202045008A (zh) | 2019-02-01 | 2020-12-16 | 印度商皮埃企業有限公司 | 4-取代的異噁唑/異噁唑啉(雜)芳基脒化合物、及其製備與用途 |
| WO2020200209A1 (zh) * | 2019-04-02 | 2020-10-08 | 成都海创药业有限公司 | 芳香胺类化合物及其在制备ar和brd4双重抑制剂和调控剂中的用途 |
| FI3976597T3 (fi) | 2019-05-31 | 2024-09-25 | Janssen Pharmaceutica Nv | Nf-kb:tä indusoivan kinaasin pienimolekyylisiä estäjiä |
| PT4146348T (pt) | 2020-05-08 | 2024-10-04 | Halia Therapeutics Inc | Inibidores da quinase nek7 |
| WO2023026794A1 (ja) | 2021-08-23 | 2023-03-02 | 国立大学法人大阪大学 | 成熟肝細胞の分化転換抑制用組成物 |
| US20240158394A1 (en) | 2022-09-14 | 2024-05-16 | Halia Therapeutics, Inc. | Nek7 inhibitors |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2386218A1 (en) | 1999-10-07 | 2001-04-12 | Amgen Inc. | Triazine kinase inhibitors |
| US20030004174A9 (en) | 2000-02-17 | 2003-01-02 | Armistead David M. | Kinase inhibitors |
| DK1259485T3 (da) | 2000-02-29 | 2006-04-10 | Millennium Pharm Inc | Benzamider og beslægtede inhibitorer for faktor Xa |
| EP1373257B9 (en) * | 2001-03-29 | 2008-10-15 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-jun n-terminal kinases (jnk) and other protein kinases |
| HUP0402352A2 (hu) | 2001-06-19 | 2005-02-28 | Bristol-Myers Squibb Co. | Foszfodiészteráz (PDE) 7 inhibitorként alkalmazható pirimidinszármazékok és ezeket tartalmazó gyógyszerkészítmények |
| WO2003030909A1 (en) * | 2001-09-25 | 2003-04-17 | Bayer Pharmaceuticals Corporation | 2- and 4-aminopyrimidines n-substtituded by a bicyclic ring for use as kinase inhibitors in the treatment of cancer |
| US20110086834A1 (en) | 2008-06-26 | 2011-04-14 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| TWI458721B (zh) | 2008-06-27 | 2014-11-01 | Celgene Avilomics Res Inc | 雜芳基化合物及其用途 |
| US20110183975A1 (en) * | 2008-10-07 | 2011-07-28 | Yasuhiro Goto | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| CA2771190C (en) | 2009-08-17 | 2020-01-21 | Memorial Sloan-Kettering Cancer Center | Heat shock protein binding compounds, compositions, and methods for making and using same |
| WO2011153553A2 (en) | 2010-06-04 | 2011-12-08 | The Regents Of The University Of California | Methods and compositions for kinase inhibition |
| AU2011283684B2 (en) | 2010-07-29 | 2015-08-27 | Rigel Pharmaceuticals, Inc. | AMPK-activating heterocyclic compounds and methods for using the same |
| CA2832919A1 (en) | 2011-04-12 | 2012-10-18 | Ryan C. Holcomb | Compounds, compositions, and therapeutic uses thereof |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| TWI692477B (zh) | 2013-08-30 | 2020-05-01 | 美商Ｐｔｃ治療公司 | 經取代嘧啶ｂｍｉ-１抑制劑 |
| 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 |
| CA2944669A1 (en) | 2014-04-04 | 2015-10-08 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| JP2017520526A (ja) | 2014-05-22 | 2017-07-27 | ザ・ユニバーシティ・オブ・シドニー | オメガ−３類似体 |
| WO2016022645A1 (en) | 2014-08-06 | 2016-02-11 | Merck Sharp & Dohme Corp. | Heterocyclic cgrp receptor antagonists |
| EP3517536B1 (en) | 2014-09-26 | 2021-05-05 | Gilead Sciences, Inc. | Aminotriazine derivatives useful as tank-binding kinase inhibitor compounds |
| CN106928216A (zh) * | 2015-12-31 | 2017-07-07 | 中国科学院上海药物研究所 | 具有erk激酶抑制活性的化合物、其制备方法和用途 |
| WO2017125530A1 (en) | 2016-01-22 | 2017-07-27 | Janssen Pharmaceutica Nv | New substituted cyanoindoline derivatives as nik inhibitors |
| CN109311846B (zh) | 2016-01-22 | 2021-03-19 | 杨森制药有限公司 | 作为nik抑制剂的新的6元杂芳族取代的氰基吲哚衍生物 |
| BR112018068703B1 (pt) | 2016-03-16 | 2024-02-06 | Kura Oncology, Inc. | Inibidores substituídos de menin-mll e métodos de uso |
| CN109641882B (zh) | 2016-06-30 | 2022-10-28 | 杨森制药有限公司 | 作为nik抑制剂的杂芳族衍生物 |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
-
2017
- 2017-01-20 WO PCT/EP2017/051150 patent/WO2017125530A1/en not_active Ceased
- 2017-01-20 LT LTEP17701110.3T patent/LT3405196T/lt unknown
- 2017-01-20 HR HRP20200133TT patent/HRP20200133T1/hr unknown
- 2017-01-20 US US16/071,192 patent/US11180487B2/en active Active
- 2017-01-20 TW TW105143703A patent/TWI739783B/zh not_active IP Right Cessation
- 2017-01-20 CA CA3011880A patent/CA3011880A1/en active Pending
- 2017-01-20 MX MX2018008974A patent/MX2018008974A/es unknown
- 2017-01-20 JP JP2018535876A patent/JP6910359B2/ja active Active
- 2017-01-20 DK DK17701110.3T patent/DK3405196T3/da active
- 2017-01-20 BR BR112018014675-7A patent/BR112018014675B1/pt active IP Right Grant
- 2017-01-20 ES ES17701110T patent/ES2775449T3/es active Active
- 2017-01-20 CN CN201780007786.1A patent/CN108697710B/zh active Active
- 2017-01-20 EP EP17701110.3A patent/EP3405196B1/en active Active
- 2017-01-20 HU HUE17701110A patent/HUE047684T2/hu unknown
- 2017-01-20 SI SI201730183T patent/SI3405196T1/sl unknown
- 2017-01-20 KR KR1020187024257A patent/KR102784966B1/ko active Active
- 2017-01-20 AU AU2017209935A patent/AU2017209935B2/en active Active
-
2018
- 2018-07-09 IL IL260500A patent/IL260500B/en active IP Right Grant
- 2018-07-13 ZA ZA2018/04688A patent/ZA201804688B/en unknown
- 2018-07-23 PH PH12018501567A patent/PH12018501567A1/en unknown
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