JP2019521097A5 - - Google Patents
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- JP2019521097A5 JP2019521097A5 JP2018562331A JP2018562331A JP2019521097A5 JP 2019521097 A5 JP2019521097 A5 JP 2019521097A5 JP 2018562331 A JP2018562331 A JP 2018562331A JP 2018562331 A JP2018562331 A JP 2018562331A JP 2019521097 A5 JP2019521097 A5 JP 2019521097A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- het
- substituted
- cycloalkyl
- group
- 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 467
- 125000001424 substituent group Chemical group 0.000 claims description 132
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims description 94
- 125000004433 nitrogen atom Chemical group N* 0.000 claims description 92
- 125000005843 halogen group Chemical group 0.000 claims description 88
- 229910052717 sulfur Inorganic materials 0.000 claims description 60
- 229910052799 carbon Inorganic materials 0.000 claims description 57
- 125000004432 carbon atom Chemical group C* 0.000 claims description 52
- 229910052739 hydrogen Inorganic materials 0.000 claims description 48
- 239000001257 hydrogen Substances 0.000 claims description 48
- 150000001875 compounds Chemical class 0.000 claims description 47
- 125000005842 heteroatom Chemical group 0.000 claims description 42
- 229910052760 oxygen Inorganic materials 0.000 claims description 36
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims description 33
- 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 24
- 125000000623 heterocyclic group Chemical group 0.000 claims description 18
- 229910052757 nitrogen Inorganic materials 0.000 claims description 14
- -1 3,6-dihydro-2H-pyran-4-yl Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 12
- 150000002431 hydrogen Chemical class 0.000 claims description 12
- 125000004429 atom Chemical group 0.000 claims description 8
- 239000008194 pharmaceutical composition Substances 0.000 claims description 7
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 4
- 125000001153 fluoro group Chemical group F* 0.000 claims description 4
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 4
- 125000002950 monocyclic group Chemical group 0.000 claims description 4
- 125000004430 oxygen atom Chemical group O* 0.000 claims description 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 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
- 125000003342 alkenyl group Chemical group 0.000 claims description 3
- 201000011510 cancer Diseases 0.000 claims description 3
- 239000003814 drug Substances 0.000 claims description 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 2
- 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
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 2
- 125000000587 piperidin-1-yl group Chemical group [H]C1([H])N(*)C([H])([H])C([H])([H])C([H])([H])C1([H])[H] 0.000 claims description 2
- 230000002062 proliferating effect Effects 0.000 claims description 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims description 2
- 229920006395 saturated elastomer Polymers 0.000 claims description 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 8
- 230000002265 prevention Effects 0.000 claims 1
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 description 1
- 239000004480 active ingredient Substances 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 125000004043 oxo group Chemical group O=* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP16177104.3 | 2016-06-30 | ||
| EP16177104 | 2016-06-30 | ||
| PCT/EP2017/066120 WO2018002217A1 (en) | 2016-06-30 | 2017-06-29 | Heteroaromatic derivatives as nik inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019521097A JP2019521097A (ja) | 2019-07-25 |
| JP2019521097A5 true JP2019521097A5 (enExample) | 2020-08-06 |
| JP6936815B2 JP6936815B2 (ja) | 2021-09-22 |
Family
ID=56296645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018562331A Active JP6936815B2 (ja) | 2016-06-30 | 2017-06-29 | Ｎｉｋ阻害剤としてのヘテロ芳香族誘導体 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US11136311B2 (enExample) |
| EP (1) | EP3478675B1 (enExample) |
| JP (1) | JP6936815B2 (enExample) |
| KR (1) | KR102517352B1 (enExample) |
| CN (1) | CN109641882B (enExample) |
| AU (1) | AU2017289315B2 (enExample) |
| CA (1) | CA3027416A1 (enExample) |
| ES (1) | ES2805976T3 (enExample) |
| WO (1) | WO2018002217A1 (enExample) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TWI739783B (zh) | 2016-01-22 | 2021-09-21 | 比利時商健生藥品公司 | 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| CA3027416A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
| KR102797697B1 (ko) | 2018-05-25 | 2025-04-22 | 에이2에이 파마수티칼스, 잉크. | 신종 항암제 후보로서, 매우 강력한 tacc3 억제제 |
| KR101954370B1 (ko) | 2018-07-25 | 2019-03-05 | 한미약품 주식회사 | 피리미딘 화합물 및 이를 포함하는 암의 예방 또는 치료용 약학 조성물 |
| AU2019203034B1 (en) * | 2018-07-25 | 2019-09-26 | Hanmi Pharm. Co., Ltd. | Pyrimidine compounds and pharmaceutical compositions for preventing or treating cancers including the same |
| MX2021010115A (es) | 2019-02-22 | 2021-09-21 | Hanmi Pharm Ind Co Ltd | Composicion farmaceutica que comprende un inhibidor de flt3 y un agente hipometilante para tratar la leucemia mieloide aguda. |
| PH12021553011A1 (en) | 2019-05-31 | 2022-11-07 | Janssen Pharmaceutica Nv | SMALL MOLECULE INHIBITORS OF NF-kB INDUCING KINASE |
| CN113993859B (zh) * | 2019-06-25 | 2024-07-02 | 益方生物科技(上海)股份有限公司 | 杂环化合物、其制备方法及其使用方法 |
| EP3991733A4 (en) | 2019-06-27 | 2023-07-05 | Hanmi Pharm. Co., Ltd. | PHARMACEUTICAL COMPOSITION FOR THE TREATMENT OF ACUTE MYELOID LEUKEMIA CONTAINING FLT3 INHIBITOR AND CHEMOTHERAPY AGENTS |
| JP2024518711A (ja) * | 2021-04-12 | 2024-05-02 | エーツーエー ファーマシューティカルズ インコーポレーテッド | 癌を処置するための組成物及び方法 |
| TW202400575A (zh) | 2022-03-24 | 2024-01-01 | 美商Ａ２Ａ製藥公司 | 治療癌症的組合物和方法 |
Family Cites Families (27)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MXPA02003436A (es) | 1999-10-07 | 2002-08-20 | Amgen Inc | Inhibidores de triazina cinasa. |
| AU2001237041B9 (en) | 2000-02-17 | 2005-07-28 | Amgen Inc. | Kinase inhibitors |
| WO2001064642A2 (en) | 2000-02-29 | 2001-09-07 | Cor Therapeutics, Inc. | Benzamides and related inhibitors of factor xa |
| US6949544B2 (en) | 2001-03-29 | 2005-09-27 | Vertex Pharmaceuticals Incorporated | Inhibitors of c-Jun N-terminal kinases (JNK) and other protein kinases |
| US7087614B2 (en) | 2001-06-19 | 2006-08-08 | Bristol-Myers Squibb Co. | Pyrimidine inhibitors of phosphodiesterase (PDE) 7 |
| 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 |
| WO2009158011A1 (en) * | 2008-06-26 | 2009-12-30 | Amgen Inc. | Alkynyl alcohols as kinase inhibitors |
| TWI546290B (zh) | 2008-06-27 | 2016-08-21 | 賽基艾維洛米斯研究股份有限公司 | 雜芳基化合物及其用途 |
| WO2010042337A1 (en) * | 2008-10-07 | 2010-04-15 | Merck Sharp & Dohme Corp. | Novel 6-azaindole aminopyrimidine derivatives having nik inhibitory activity |
| BR112012003637A2 (pt) | 2009-08-17 | 2017-04-25 | Memorial Sloan Kettering Cancer Center | "compostos de ligação de proteína de choque térmico, composições, e métodos para preparar e usar os mesmos" |
| 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 |
| JP2014510794A (ja) | 2011-04-12 | 2014-05-01 | アルツハイマーズ・インスティテュート・オブ・アメリカ・インコーポレイテッド | ＩＫＫ関連キナーゼεおよびＴＡＮＫ結合キナーゼ１の阻害剤の組成物および治療的使用 |
| 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 |
| HRP20190039T1 (hr) | 2014-04-04 | 2019-03-08 | Syros Pharmaceuticals, Inc. | Inhibitori ciklin-ovisne kinaze 7 (cdk7) |
| KR20170030474A (ko) | 2014-05-22 | 2017-03-17 | 더 유니버시티 오브 시드니 | 오메가―３ 유사체 |
| WO2016022645A1 (en) | 2014-08-06 | 2016-02-11 | Merck Sharp & Dohme Corp. | Heterocyclic cgrp receptor antagonists |
| NZ729618A (en) | 2014-09-26 | 2018-07-27 | 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 |
| TWI739783B (zh) | 2016-01-22 | 2021-09-21 | 比利時商健生藥品公司 | 作為nik抑制劑的新穎的經取代氰基吲哚啉衍生物 |
| US11001569B2 (en) | 2016-01-22 | 2021-05-11 | Janssen Pharmaceutica Nv | 6-membered heteroaromatic substituted cyanoindoline derivatives as NIK inhibitors |
| SG11201807982UA (en) | 2016-03-16 | 2018-10-30 | Kura Oncology Inc | Substituted inhibitors of menin-mll and methods of use |
| WO2018002219A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Cyanoindoline derivatives as nik inhibitors |
| CA3027416A1 (en) | 2016-06-30 | 2018-01-04 | Janssen Pharmaceutica Nv | Heteroaromatic derivatives as nik inhibitors |
-
2017
- 2017-06-29 CA CA3027416A patent/CA3027416A1/en active Pending
- 2017-06-29 JP JP2018562331A patent/JP6936815B2/ja active Active
- 2017-06-29 WO PCT/EP2017/066120 patent/WO2018002217A1/en not_active Ceased
- 2017-06-29 KR KR1020197002588A patent/KR102517352B1/ko active Active
- 2017-06-29 AU AU2017289315A patent/AU2017289315B2/en not_active Ceased
- 2017-06-29 US US16/309,059 patent/US11136311B2/en active Active
- 2017-06-29 ES ES17739902T patent/ES2805976T3/es active Active
- 2017-06-29 EP EP17739902.9A patent/EP3478675B1/en active Active
- 2017-06-29 CN CN201780053583.6A patent/CN109641882B/zh active Active
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