JP2019524646A5 - - Google Patents
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- Publication number
- JP2019524646A5 JP2019524646A5 JP2018562323A JP2018562323A JP2019524646A5 JP 2019524646 A5 JP2019524646 A5 JP 2019524646A5 JP 2018562323 A JP2018562323 A JP 2018562323A JP 2018562323 A JP2018562323 A JP 2018562323A JP 2019524646 A5 JP2019524646 A5 JP 2019524646A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- ring
- het
- 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 description 481
- 125000001424 substituent group Chemical group 0.000 claims description 133
- 125000005843 halogen group Chemical group 0.000 claims description 82
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 78
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 77
- 229910052799 carbon Inorganic materials 0.000 claims description 64
- 125000004432 carbon atom Chemical group C* 0.000 claims description 58
- 150000001875 compounds Chemical class 0.000 claims description 54
- 229910052739 hydrogen Inorganic materials 0.000 claims description 52
- 239000001257 hydrogen Substances 0.000 claims description 52
- 229910052717 sulfur Inorganic materials 0.000 claims description 52
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 49
- 125000005842 heteroatom Chemical group 0.000 claims description 44
- 229910052760 oxygen Inorganic materials 0.000 claims description 42
- 125000000623 heterocyclic group Chemical group 0.000 claims description 41
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 32
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 20
- 229910052757 nitrogen Inorganic materials 0.000 claims description 20
- 125000006705 (C5-C7) cycloalkyl group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 11
- 125000003342 alkenyl group Chemical group 0.000 claims description 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 10
- -1 2-oxo-1,2-dihydropyridin-3-yl Chemical group 0.000 claims description 8
- 125000004429 atom Chemical group 0.000 claims description 8
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000003118 aryl group Chemical group 0.000 claims description 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000004043 oxo group Chemical group O=* 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims description 4
- 239000012453 solvate Substances 0.000 claims description 4
- 125000003003 spiro group Chemical group 0.000 claims description 4
- 206010028980 Neoplasm Diseases 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 239000003085 diluting agent Substances 0.000 claims description 2
- 201000010099 disease Diseases 0.000 claims description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 2
- 239000003814 drug Substances 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000001153 fluoro group Chemical group F* 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000002950 monocyclic group Chemical group 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 9
- 230000002265 prevention Effects 0.000 claims 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
Applications Claiming Priority (7)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16177147.2 | 2016-06-30 | ||
| EP16177142 | 2016-06-30 | ||
| EP16177142.3 | 2016-06-30 | ||
| EP16177131 | 2016-06-30 | ||
| EP16177147 | 2016-06-30 | ||
| EP16177131.6 | 2016-06-30 | ||
| PCT/EP2017/066125 WO2018002219A1 (en) | 2016-06-30 | 2017-06-29 | Cyanoindoline derivatives as nik inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019524646A JP2019524646A (ja) | 2019-09-05 |
| JP2019524646A5 true JP2019524646A5 (enExample) | 2020-08-06 |
| JP6936814B2 JP6936814B2 (ja) | 2021-09-22 |
Family
ID=59227756
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018562323A Active JP6936814B2 (ja) | 2016-06-30 | 2017-06-29 | Ｎｉｋ阻害剤としてのシアノインドリン誘導体 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US20190119299A1 (enExample) |
| EP (1) | EP3478673B1 (enExample) |
| JP (1) | JP6936814B2 (enExample) |
| KR (1) | KR102587619B1 (enExample) |
| CN (1) | CN109689645B (enExample) |
| AU (1) | AU2017289317B2 (enExample) |
| ES (1) | ES2837157T3 (enExample) |
| WO (1) | WO2018002219A1 (enExample) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| WO2017125530A1 (en) | 2016-01-22 | 2017-07-27 | Janssen Pharmaceutica Nv | New substituted cyanoindoline derivatives as nik inhibitors |
| 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 |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| LT3976597T (lt) | 2019-05-31 | 2024-10-10 | Janssen Pharmaceutica Nv | Nf-κb indukuojančios kinazės mažos molekulės inhibitoriai |
| KR20220044495A (ko) * | 2019-07-04 | 2022-04-08 | 치루 레고르 테라퓨틱스 인코포레이티드 | Hpk1 억제제 및 그의 용도 |
| WO2022214008A1 (zh) * | 2021-04-08 | 2022-10-13 | 杭州阿诺生物医药科技有限公司 | 高活性hpk1激酶抑制剂 |
| CN114380806B (zh) * | 2022-03-24 | 2022-06-10 | 中国药科大学 | 2-氨基-4-吲哚基嘧啶类化合物及其制备方法与应用 |
Family Cites Families (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE396978T1 (de) * | 1999-10-07 | 2008-06-15 | Amgen Inc | Triazin-kinase-hemmer |
| MXPA02007957A (es) | 2000-02-17 | 2002-11-29 | Amgen Inc | Inhibidores de cinasas. |
| AU2001250783A1 (en) | 2000-02-29 | 2001-09-12 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor 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 |
| KR20070084067A (ko) * | 2004-10-13 | 2007-08-24 | 와이어쓰 | Ｎ-벤젠설포닐 치환 아닐리노-피리미딘 동족체 |
| JP2011525915A (ja) * | 2008-06-26 | 2011-09-29 | アムジエン・インコーポレーテツド | キナーゼ阻害薬としてのアルキニルアルコール類 |
| SG10201510696RA (en) | 2008-06-27 | 2016-01-28 | Celgene Avilomics Res Inc | Heteroaryl compounds and uses thereof |
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | 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 |
| CA2806341C (en) | 2010-07-29 | 2020-03-24 | Rigel Pharmaceuticals, Inc. | Ampk-activating heterocyclic compounds and methods for using the same |
| EP2696683A4 (en) | 2011-04-12 | 2014-08-13 | Alzheimer S Inst Of America Inc | COMPOSITIONS AND THERAPEUTIC APPLICATIONS OF IKK-MEDIATED KINASE EPSILON AND TANK BINDING KINASE-1 HEMMER |
| TWI663166B (zh) | 2013-04-24 | 2019-06-21 | 健生藥品公司 | 新化合物 |
| WO2015030847A1 (en) | 2013-08-30 | 2015-03-05 | Ptc Therapeutics, Inc. | Substituted pyrimidine bmi-1 inhibitors |
| 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 |
| LT3126352T (lt) | 2014-04-04 | 2019-01-10 | Syros Pharmaceuticals, Inc. | Nuo ciklino priklausomos kinazės 7 (cdk7) inhibitoriai |
| CN106536478A (zh) | 2014-05-22 | 2017-03-22 | 悉尼大学 | ω‑3类似物 |
| WO2016022645A1 (en) | 2014-08-06 | 2016-02-11 | Merck Sharp & Dohme Corp. | Heterocyclic cgrp receptor antagonists |
| JP6499282B2 (ja) | 2014-09-26 | 2019-04-10 | ギリアード サイエンシーズ， インコーポレイテッド | Ｔａｎｋ結合キナーゼ阻害剤化合物として有用なアミノトリアジン誘導体 |
| 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 |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| WO2017125530A1 (en) | 2016-01-22 | 2017-07-27 | Janssen Pharmaceutica Nv | New substituted cyanoindoline derivatives as nik inhibitors |
| BR112018068703B1 (pt) | 2016-03-16 | 2024-02-06 | Kura Oncology, Inc. | Inibidores substituídos de menin-mll e métodos de uso |
| ES2837157T3 (es) | 2016-06-30 | 2021-06-29 | Janssen Pharmaceutica Nv | Derivados de cianoindolina como inhibidores de NIK |
| 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 |
-
2017
- 2017-06-29 ES ES17733469T patent/ES2837157T3/es active Active
- 2017-06-29 AU AU2017289317A patent/AU2017289317B2/en not_active Ceased
- 2017-06-29 WO PCT/EP2017/066125 patent/WO2018002219A1/en not_active Ceased
- 2017-06-29 US US16/309,080 patent/US20190119299A1/en not_active Abandoned
- 2017-06-29 EP EP17733469.5A patent/EP3478673B1/en active Active
- 2017-06-29 KR KR1020197002912A patent/KR102587619B1/ko active Active
- 2017-06-29 CN CN201780053613.3A patent/CN109689645B/zh active Active
- 2017-06-29 JP JP2018562323A patent/JP6936814B2/ja active Active
-
2020
- 2020-02-06 US US16/783,810 patent/US11186589B2/en active Active
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