JP2019527230A5 - - Google Patents
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- Publication number
- JP2019527230A5 JP2019527230A5 JP2019504675A JP2019504675A JP2019527230A5 JP 2019527230 A5 JP2019527230 A5 JP 2019527230A5 JP 2019504675 A JP2019504675 A JP 2019504675A JP 2019504675 A JP2019504675 A JP 2019504675A JP 2019527230 A5 JP2019527230 A5 JP 2019527230A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- nhc
- cycloalkyl
- nhs
- aryl
- 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.)
- Pending
Links
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 65
- 125000003118 aryl group Chemical group 0.000 claims 53
- 125000001072 heteroaryl group Chemical group 0.000 claims 32
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 28
- 150000001875 compounds Chemical class 0.000 claims 25
- 150000003839 salts Chemical class 0.000 claims 22
- 125000001246 bromo group Chemical group Br* 0.000 claims 21
- 125000001309 chloro group Chemical group Cl* 0.000 claims 21
- 125000001153 fluoro group Chemical group F* 0.000 claims 21
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 21
- 229910052736 halogen Inorganic materials 0.000 claims 18
- 150000002367 halogens Chemical class 0.000 claims 18
- 125000000217 alkyl group Chemical group 0.000 claims 16
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 claims 13
- 229910052805 deuterium Inorganic materials 0.000 claims 13
- 125000002950 monocyclic group Chemical group 0.000 claims 12
- 229910052799 carbon Inorganic materials 0.000 claims 11
- -1 -OH Chemical group 0.000 claims 10
- 238000000034 method Methods 0.000 claims 10
- 125000000753 cycloalkyl group Chemical group 0.000 claims 8
- 206010028980 Neoplasm Diseases 0.000 claims 7
- 201000011510 cancer Diseases 0.000 claims 7
- 101000997832 Homo sapiens Tyrosine-protein kinase JAK2 Proteins 0.000 claims 6
- 102100033444 Tyrosine-protein kinase JAK2 Human genes 0.000 claims 6
- 229910052739 hydrogen Inorganic materials 0.000 claims 6
- 108090000623 proteins and genes Proteins 0.000 claims 6
- 150000001345 alkine derivatives Chemical class 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 208000023275 Autoimmune disease Diseases 0.000 claims 3
- 206010061218 Inflammation Diseases 0.000 claims 3
- 108020001507 fusion proteins Proteins 0.000 claims 3
- 102000037865 fusion proteins Human genes 0.000 claims 3
- 230000004054 inflammatory process Effects 0.000 claims 3
- 230000035772 mutation Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 208000012902 Nervous system disease Diseases 0.000 claims 2
- 208000025966 Neurological disease Diseases 0.000 claims 2
- 208000002193 Pain Diseases 0.000 claims 2
- 239000012634 fragment Substances 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 208000032839 leukemia Diseases 0.000 claims 2
- 230000001404 mediated effect Effects 0.000 claims 2
- 102000004169 proteins and genes Human genes 0.000 claims 2
- 229910052717 sulfur Inorganic materials 0.000 claims 2
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims 1
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 101150009057 JAK2 gene Proteins 0.000 claims 1
- 208000031422 Lymphocytic Chronic B-Cell Leukemia Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 101150090128 PCM1 gene Proteins 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 1
- 239000000654 additive Substances 0.000 claims 1
- 230000000996 additive effect Effects 0.000 claims 1
- 208000032852 chronic lymphocytic leukemia Diseases 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000000338 in vitro Methods 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 102000037979 non-receptor tyrosine kinases Human genes 0.000 claims 1
- 108091008046 non-receptor tyrosine kinases Proteins 0.000 claims 1
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662367886P | 2016-07-28 | 2016-07-28 | |
| US62/367,886 | 2016-07-28 | ||
| PCT/US2017/044214 WO2018022911A1 (en) | 2016-07-28 | 2017-07-27 | Macrocycle kinase inhibitors |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2019527230A JP2019527230A (ja) | 2019-09-26 |
| JP2019527230A5 true JP2019527230A5 (enExample) | 2020-09-03 |
Family
ID=61016718
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019504675A Pending JP2019527230A (ja) | 2016-07-28 | 2017-07-27 | 大環状キナーゼ阻害剤 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US10689400B2 (enExample) |
| EP (1) | EP3490564A4 (enExample) |
| JP (1) | JP2019527230A (enExample) |
| KR (1) | KR20190034225A (enExample) |
| CN (1) | CN109715165A (enExample) |
| AU (1) | AU2017302019A1 (enExample) |
| BR (1) | BR112019001607A2 (enExample) |
| CA (1) | CA3031100A1 (enExample) |
| IL (1) | IL264395A (enExample) |
| MX (1) | MX2019001125A (enExample) |
| RU (1) | RU2019105587A (enExample) |
| SG (1) | SG11201900163PA (enExample) |
| TW (1) | TW201815799A (enExample) |
| WO (1) | WO2018022911A1 (enExample) |
| ZA (1) | ZA201901034B (enExample) |
Families Citing this family (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PL3097107T3 (pl) | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| KR102772574B1 (ko) | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 大環式化合物およびその使用 |
| CN109516999B (zh) * | 2017-11-01 | 2021-08-17 | 郑州泰基鸿诺医药股份有限公司 | 用作蛋白质激酶调节剂的化合物及其应用 |
| SI3728271T1 (sl) | 2017-12-19 | 2023-01-31 | Turning Point Therapeutics, Inc. | Makrociklične spojine za zdravljenje bolezni |
| MX2020010116A (es) | 2018-03-28 | 2020-11-06 | Fochon Biosciences Ltd | Compuestos macrociclicos como inhibidores de quinasas del receptor de tropomiosina (trk). |
| WO2019206069A1 (zh) | 2018-04-25 | 2019-10-31 | 北京普祺医药科技有限公司 | 一种二芳基巨环化合物、药物组合物以及其用途 |
| CA3224985A1 (en) | 2018-07-31 | 2020-02-06 | Loxo Oncology, Inc. | Spray-dried dispersions, formulations, and polymorphs of (s)-5-amino-3-(4-((5-fluoro-2-methoxybenzamido)methyl)phenyl)-1-(1,1,1-trifluoropropan-2-yl)-1h-pyrazole-4-carboxamide |
| JP7631193B2 (ja) | 2018-10-22 | 2025-02-18 | アルミス インコーポレイテッド | Ｔｙｋ２阻害剤およびその使用 |
| SG11202110523XA (en) * | 2019-03-26 | 2021-10-28 | Ventyx Biosciences Inc | Tyk2 pseudokinase ligands |
| CN113727984B (zh) * | 2019-05-21 | 2024-03-15 | 浙江海正药业股份有限公司 | 大环类衍生物、及其制备方法和用途 |
| CN113773335B (zh) * | 2019-06-21 | 2024-12-03 | 成都海博为药业有限公司 | 一种作为蛋白质激酶抑制剂的化合物及其制备方法和用途 |
| WO2021027503A1 (zh) * | 2019-08-12 | 2021-02-18 | 罗欣药业(上海)有限公司 | 三环类化合物、其制备方法、中间体及应用 |
| US20220372135A1 (en) | 2019-09-27 | 2022-11-24 | Disc Medicine, Inc. | Methods for treating myelofibrosis and related conditions |
| IL295938A (en) * | 2020-03-02 | 2022-10-01 | Turning Point Therapeutics Inc | Therapeutic uses of macrocyclic compounds |
| IL297437A (en) | 2020-05-13 | 2022-12-01 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| WO2021244609A1 (zh) * | 2020-06-04 | 2021-12-09 | 成都倍特药业股份有限公司 | 具有大环结构的化合物及其用途 |
| US20240132517A1 (en) * | 2021-02-10 | 2024-04-25 | Goharmony Therapeutics (Shenzhen) Co., Ltd. | Macrocyclic compound, pharmaceutical composition, and use thereof |
| CN113354548A (zh) * | 2021-04-12 | 2021-09-07 | 常熟耐素生物材料科技有限公司 | 一种基于六亚甲基四胺的植物多烯酚醛胺环氧固化剂及其制备方法 |
| CN116063326B (zh) * | 2021-11-02 | 2025-08-05 | 赛诺哈勃药业（成都）有限公司 | 作为蛋白激酶调节剂的含氨基大环化合物 |
| WO2023208244A1 (zh) * | 2022-04-29 | 2023-11-02 | 南京明德新药研发有限公司 | 大环类化合物及其应用 |
| WO2025010294A2 (en) * | 2023-07-03 | 2025-01-09 | Blossomhill Therapeutics, Inc. | Macrocyclic compounds and use as tyk2 inhibitors |
Family Cites Families (29)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DK0690843T3 (da) | 1993-03-25 | 2000-11-13 | Upjohn Co | Fornyl- eller cyanosubstituerede indolderivater med dopaninerg aktivitet |
| RS49779B (sr) | 1998-01-12 | 2008-06-05 | Glaxo Group Limited, | Biciklična heteroaromatična jedinjenja kao inhibitori protein tirozin kinaze |
| US7517882B2 (en) * | 2006-09-18 | 2009-04-14 | Polaris Group | Protein kinase inhibitors |
| US8815872B2 (en) * | 2008-09-08 | 2014-08-26 | Merck Patent Gmbh | Macrocyclics pyrimidines as aurora kinase inhibitors |
| ES2464461T3 (es) | 2008-09-22 | 2014-06-02 | Array Biopharma, Inc. | Compuestos de imidazo[1,2B]piridazina sustituidos como inhibidores de la TRK cinasa |
| SG196855A1 (en) | 2008-10-22 | 2014-02-13 | Array Biopharma Inc | Substituted pyrazolo[1,5-a]pyrimidine compounds as trk kinase inhibitors |
| JP5769199B2 (ja) | 2008-10-31 | 2015-08-26 | ジェネンテック， インコーポレイテッド | ピラゾロピリミジンｊａｋ阻害剤化合物と方法 |
| AU2011256380C1 (en) | 2010-05-20 | 2016-09-08 | Array Biopharma Inc. | Macrocyclic compounds as Trk kinase inhibitors |
| US8757434B2 (en) * | 2010-07-01 | 2014-06-24 | The Coca-Cola Company | Merchandiser |
| UY33597A (es) | 2010-09-09 | 2012-04-30 | Irm Llc | Compuestos y composiciones como inhibidores de la trk |
| EP2508607A1 (en) | 2011-04-07 | 2012-10-10 | Helmholtz-Zentrum für Infektionsforschung GmbH | Medicament for liver regeneration and for treatment of liver failure |
| US9284334B2 (en) * | 2011-05-19 | 2016-03-15 | Fundación Centro Nacional De Investigaciones Oncologicas Carlos Iii | Macrocyclic compounds as protein kinase inhibitors |
| WO2013001310A1 (en) | 2011-06-30 | 2013-01-03 | Centro Nacional De Investigaciones Oncológicas (Cnio) | Macrocyclic compounds and their use as cdk8 inhibitors |
| RU2014110399A (ru) | 2011-08-19 | 2015-09-27 | Мерк Шарп И Доум Корп. | Кристаллические формы вгс протеазного ингибитора |
| ES2583477T3 (es) * | 2011-09-30 | 2016-09-21 | Ipsen Pharma S.A.S. | Inhibidores macrocíclicos de cinasa de LRRK2 |
| KR20140078710A (ko) | 2011-09-30 | 2014-06-25 | 온코디자인 에스.에이. | 거대고리 flt3 키나제 억제제 |
| WO2013132376A1 (en) | 2012-03-06 | 2013-09-12 | Pfizer Inc. | Macrocyclic derivatives for the treatment of proliferative diseases |
| RU2014140735A (ru) | 2012-03-09 | 2016-04-27 | Лексикон Фармасьютикалз, Инк. | ПРОИЗВОДНЫЕ ПИРАЗОЛО[1, 5-a]ПИРИМИДИНА, КОМПОЗИЦИИ, СОДЕРЖАЩИЕ УКАЗАННЫЕ СОЕДИНЕНИЯ, И СПОСОБЫ ИХ ПРИМЕНЕНИЯ |
| KR102085121B1 (ko) | 2012-03-09 | 2020-03-05 | 렉시컨 파마슈티컬스 인코퍼레이티드 | 이미다조[1,2-b]피리다진계 화합물, 그를 포함하는 조성물 및 그의 용도 |
| GB201205669D0 (en) | 2012-03-30 | 2012-05-16 | Agency Science Tech & Res | Bicyclic heterocyclic derivatives as mnk2 and mnk2 modulators and uses thereof |
| CN105228625A (zh) * | 2013-03-15 | 2016-01-06 | 昂科迪塞恩股份有限公司 | 大环rip2激酶抑制剂 |
| CN104513253A (zh) * | 2013-10-01 | 2015-04-15 | 南京波尔泰药业科技有限公司 | 用于治疗增殖性疾病的大环化合物 |
| PL3097107T3 (pl) | 2014-01-24 | 2020-01-31 | Turning Point Therapeutics, Inc. | Diarylowe związki makrocykliczne jako modulatory kinaz białkowych |
| AU2016287568B2 (en) | 2015-07-02 | 2020-08-20 | Turning Point Therapeutics, Inc. | Chiral diaryl macrocycles as modulators of protein kinases |
| HRP20240780T1 (hr) | 2015-07-06 | 2024-09-13 | Turning Point Therapeutics, Inc. | Polimorf diaril makrocikla |
| KR102772574B1 (ko) | 2015-07-21 | 2025-02-24 | 터닝 포인트 테라퓨틱스, 인크. | 키랄 디아릴 매크로사이클 및 이것의 용도 |
| RU2019105587A (ru) | 2016-07-28 | 2020-08-28 | Тёрнинг Поинт Терапьютикс, Инк. | Макроциклические ингибиторы киназ |
| TWI808958B (zh) | 2017-01-25 | 2023-07-21 | 美商特普醫葯公司 | 涉及二芳基巨環化合物之組合療法 |
| JP7224334B2 (ja) | 2017-07-28 | 2023-02-17 | ターニング・ポイント・セラピューティクス・インコーポレイテッド | 大環式化合物およびその使用 |
-
2017
- 2017-07-27 RU RU2019105587A patent/RU2019105587A/ru not_active Application Discontinuation
- 2017-07-27 KR KR1020197003927A patent/KR20190034225A/ko not_active Ceased
- 2017-07-27 EP EP17835284.5A patent/EP3490564A4/en not_active Withdrawn
- 2017-07-27 TW TW106125249A patent/TW201815799A/zh unknown
- 2017-07-27 CN CN201780056515.5A patent/CN109715165A/zh active Pending
- 2017-07-27 WO PCT/US2017/044214 patent/WO2018022911A1/en not_active Ceased
- 2017-07-27 BR BR112019001607-4A patent/BR112019001607A2/pt not_active Application Discontinuation
- 2017-07-27 MX MX2019001125A patent/MX2019001125A/es unknown
- 2017-07-27 CA CA3031100A patent/CA3031100A1/en active Pending
- 2017-07-27 JP JP2019504675A patent/JP2019527230A/ja active Pending
- 2017-07-27 SG SG11201900163PA patent/SG11201900163PA/en unknown
- 2017-07-27 US US16/320,589 patent/US10689400B2/en active Active
- 2017-07-27 AU AU2017302019A patent/AU2017302019A1/en not_active Abandoned
-
2019
- 2019-01-22 IL IL264395A patent/IL264395A/en unknown
- 2019-02-18 ZA ZA2019/01034A patent/ZA201901034B/en unknown
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