JP2019535749A5 - - Google Patents
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- Publication number
- JP2019535749A5 JP2019535749A5 JP2019527379A JP2019527379A JP2019535749A5 JP 2019535749 A5 JP2019535749 A5 JP 2019535749A5 JP 2019527379 A JP2019527379 A JP 2019527379A JP 2019527379 A JP2019527379 A JP 2019527379A JP 2019535749 A5 JP2019535749 A5 JP 2019535749A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- substituted
- alkyl
- heteroaryl
- optionally
- 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
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- 125000000623 heterocyclic group Chemical group 0.000 claims 78
- 125000001072 heteroaryl group Chemical group 0.000 claims 76
- 229910052739 hydrogen Inorganic materials 0.000 claims 57
- 239000001257 hydrogen Substances 0.000 claims 57
- 125000003107 substituted aryl group Chemical group 0.000 claims 56
- 150000002431 hydrogen Chemical class 0.000 claims 53
- 125000004452 carbocyclyl group Chemical group 0.000 claims 52
- 125000000547 substituted alkyl group Chemical group 0.000 claims 48
- 125000005017 substituted alkenyl group Chemical group 0.000 claims 47
- 125000004426 substituted alkynyl group Chemical group 0.000 claims 47
- 150000001875 compounds Chemical class 0.000 claims 44
- 150000003839 salts Chemical class 0.000 claims 39
- 125000002252 acyl group Chemical group 0.000 claims 38
- 239000008194 pharmaceutical composition Substances 0.000 claims 38
- 239000012453 solvate Substances 0.000 claims 37
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 25
- 230000002062 proliferating effect Effects 0.000 claims 25
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 24
- 229910052736 halogen Inorganic materials 0.000 claims 23
- 150000002367 halogens Chemical class 0.000 claims 23
- 201000010099 disease Diseases 0.000 claims 21
- 229910052757 nitrogen Inorganic materials 0.000 claims 20
- 229910052717 sulfur Inorganic materials 0.000 claims 17
- 238000000034 method Methods 0.000 claims 14
- 125000004429 atom Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 125000004430 oxygen atom Chemical group O* 0.000 claims 12
- 125000006239 protecting group Chemical group 0.000 claims 12
- 125000004434 sulfur atom Chemical group 0.000 claims 12
- 125000000217 alkyl group Chemical group 0.000 claims 11
- 102100038111 Cyclin-dependent kinase 12 Human genes 0.000 claims 10
- 101710179260 Cyclin-dependent kinase 12 Proteins 0.000 claims 10
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims 10
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims 10
- 125000002837 carbocyclic group Chemical group 0.000 claims 9
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 6
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 239000001301 oxygen Substances 0.000 claims 6
- 239000011593 sulfur Substances 0.000 claims 6
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000002947 alkylene group Chemical group 0.000 claims 4
- 125000003118 aryl group Chemical group 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical group [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 230000000694 effects Effects 0.000 claims 3
- 230000002401 inhibitory effect Effects 0.000 claims 3
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 3
- 238000006467 substitution reaction Methods 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 206010041067 Small cell lung cancer Diseases 0.000 claims 2
- 208000003721 Triple Negative Breast Neoplasms Diseases 0.000 claims 2
- 230000001028 anti-proliverative effect Effects 0.000 claims 2
- 239000012472 biological sample Substances 0.000 claims 2
- 239000003795 chemical substances by application Substances 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 230000002018 overexpression Effects 0.000 claims 2
- 208000000587 small cell lung carcinoma Diseases 0.000 claims 2
- 208000022679 triple-negative breast carcinoma Diseases 0.000 claims 2
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims 2
- 208000010839 B-cell chronic lymphocytic leukemia Diseases 0.000 claims 1
- 206010060999 Benign neoplasm Diseases 0.000 claims 1
- 206010005949 Bone cancer Diseases 0.000 claims 1
- 208000018084 Bone neoplasm Diseases 0.000 claims 1
- 208000003174 Brain Neoplasms Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000006168 Ewing Sarcoma Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 230000001594 aberrant effect Effects 0.000 claims 1
- 230000002159 abnormal effect Effects 0.000 claims 1
- 125000006193 alkinyl group Chemical group 0.000 claims 1
- 230000033115 angiogenesis Effects 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000004663 cell proliferation Effects 0.000 claims 1
- 230000006806 disease prevention Effects 0.000 claims 1
- 238000001727 in vivo Methods 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 230000006654 negative regulation of apoptotic process Effects 0.000 claims 1
- 201000008968 osteosarcoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229940127557 pharmaceutical product Drugs 0.000 claims 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662425519P | 2016-11-22 | 2016-11-22 | |
| US62/425,519 | 2016-11-22 | ||
| PCT/US2017/063132 WO2018098361A1 (en) | 2016-11-22 | 2017-11-22 | Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019535749A JP2019535749A (ja) | 2019-12-12 |
| JP2019535749A5 true JP2019535749A5 (https=) | 2021-01-14 |
| JP7258748B2 JP7258748B2 (ja) | 2023-04-17 |
Family
ID=60703092
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019527379A Active JP7258748B2 (ja) | 2016-11-22 | 2017-11-22 | サイクリン依存性キナーゼ１２（ｃｄｋ１２）の阻害剤およびその使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (2) | US11306070B2 (https=) |
| EP (1) | EP3544971B1 (https=) |
| JP (1) | JP7258748B2 (https=) |
| AU (1) | AU2017363307B2 (https=) |
| CA (1) | CA3041563C (https=) |
| WO (1) | WO2018098361A1 (https=) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9180127B2 (en) | 2009-12-29 | 2015-11-10 | Dana-Farber Cancer Institute, Inc. | Type II Raf kinase inhibitors |
| AU2015371251B2 (en) | 2014-12-23 | 2020-06-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| HK1246645A1 (zh) | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| WO2018098361A1 (en) | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| SG11202013175SA (en) * | 2018-06-29 | 2021-01-28 | Kinnate Biopharma Inc | Inhibitors of cyclin-dependent kinases |
| CN109111376B (zh) * | 2018-09-18 | 2021-09-14 | 四川医立特生物医药有限公司 | 一种2,5-双脱氧链霉胺衍生物及其应用 |
| JP7660063B2 (ja) | 2018-12-28 | 2025-04-10 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用 |
| AU2020263390B2 (en) * | 2019-04-23 | 2026-01-08 | Dana-Farber Cancer Institute, Inc. | Degraders of cyclin-dependent kinase 12 (CDK12) and uses thereof |
| US20220288067A1 (en) * | 2019-04-24 | 2022-09-15 | The Trustees Of The University Of Pennsylvania | Treatment of cancer with cdk inhibitors |
| CN114901284A (zh) * | 2019-10-29 | 2022-08-12 | 希洛斯医药品股份有限公司 | 用细胞周期蛋白依赖性激酶7(cdk7)抑制剂治疗生物标志物鉴定的患者的癌症的方法 |
| CN111269217B (zh) * | 2020-04-07 | 2021-01-08 | 苏州信诺维医药科技有限公司 | 一种嘧啶胺类化合物、其制备方法及应用 |
| CN111393415B (zh) * | 2020-04-30 | 2020-11-20 | 苏州信诺维医药科技有限公司 | 一种杂芳腈类化合物及其应用 |
| CN114133394B (zh) * | 2020-08-12 | 2023-12-08 | 赛诺哈勃药业（成都）有限公司 | 一种选择性针对细胞周期依赖性激酶12活性的化合物、制备方法及医药用途 |
| US20230303512A1 (en) * | 2020-08-26 | 2023-09-28 | Massachusetts Institute Of Technology | Modulators of myb-mediated transcription and uses thereof |
| US12018016B2 (en) | 2021-08-18 | 2024-06-25 | Amgen Inc. | Aryl sulfonyl (hydroxy) piperidines as CCR6 inhibitors |
| WO2023023534A2 (en) | 2021-08-18 | 2023-02-23 | Chemocentryx, Inc. | Aryl sulfonyl compounds as ccr6 inhibitors |
| WO2023091726A1 (en) * | 2021-11-18 | 2023-05-25 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin‑dependent kinase 12 (cdk12) |
| TW202329937A (zh) * | 2021-12-03 | 2023-08-01 | 美商英塞特公司 | 雙環胺ｃｋ１２抑制劑 |
| WO2023107705A1 (en) | 2021-12-10 | 2023-06-15 | Incyte Corporation | Bicyclic amines as cdk12 inhibitors |
| CN114452391B (zh) * | 2022-01-28 | 2023-08-25 | 深圳市泰尔康生物医药科技有限公司 | Cdk16作为靶标在制备用于治疗三阴性乳腺癌的药物中的应用 |
| KR102821060B1 (ko) | 2023-03-09 | 2025-06-16 | 미네암리타 테라퓨틱스, 엘엘씨 | 위암의 치료를 위한 약물 조합 |
Family Cites Families (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6143764A (en) | 1995-11-07 | 2000-11-07 | Kirin Beer Kabushiki Kaisha | Quinoline and quinazoline derivatives inhibiting platelet-derived growth factor receptor autophosphorylation and pharmaceutical compositions containing the same |
| SK288365B6 (sk) | 1999-02-10 | 2016-07-01 | Astrazeneca Ab | Medziprodukty pre chinazolínové deriváty ako inhibítory angiogenézy |
| JP2003503351A (ja) | 1999-06-30 | 2003-01-28 | メルク エンド カムパニー インコーポレーテッド | Ｓｒｃキナーゼ阻害化合物 |
| WO2006038001A1 (en) * | 2004-10-06 | 2006-04-13 | Celltech R & D Limited | Aminopyrimidine derivatives as jnk inhibitors |
| JP2008517064A (ja) * | 2004-10-19 | 2008-05-22 | アークル インコーポレイテッド | Ｐ３８ｍａｐキナーゼのイミダゾオキサゾールおよびイミダゾチアゾール阻害剤の合成 |
| AU2005323797B2 (en) | 2005-01-10 | 2009-07-09 | Pfizer Inc. | Pyrrolopyrazoles, potent kinase inhibitors |
| EP2013218A2 (en) * | 2006-04-17 | 2009-01-14 | Arqule, Inc. | Raf inhibitors and their uses |
| WO2007129195A2 (en) | 2006-05-04 | 2007-11-15 | Pfizer Products Inc. | 4-pyrimidine-5-amino-pyrazole compounds |
| US20090054392A1 (en) | 2007-08-20 | 2009-02-26 | Wyeth | Naphthylpyrimidine, naphthylpyrazine and naphthylpyridazine analogs and their use as agonists of the wnt-beta-catenin cellular messaging system |
| AU2009227013B2 (en) | 2008-03-21 | 2013-01-10 | Novartis Ag | Novel heterocyclic compounds and uses therof |
| CN102317293A (zh) | 2008-12-05 | 2012-01-11 | 艾科尔公司 | Raf抑制剂及其用途 |
| US20120165309A1 (en) | 2009-02-12 | 2012-06-28 | Astellas Pharma Inc. | Hetero ring derivative |
| TW201102387A (en) | 2009-06-08 | 2011-01-16 | Medicinova Inc | Substituted pyrazolo[1,5-a]pyridine compounds having multi-target activity |
| MX2013005445A (es) | 2010-11-19 | 2013-07-29 | Hoffmann La Roche | Pirazolopiridinas y el uso de pirazolopiridinas como inhibidores de tirosina cinasa 2 (tyk2). |
| CA2856291C (en) | 2011-11-17 | 2020-08-11 | Dana-Farber Cancer Institute, Inc. | Inhibitors of c-jun-n-terminal kinase (jnk) |
| EP2909194A1 (en) | 2012-10-18 | 2015-08-26 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| TWI621618B (zh) | 2013-03-13 | 2018-04-21 | 比利時商健生藥品公司 | 經取代２－氮雜雙環類及其作為食慾素受體調控劑之用途 |
| TW201444821A (zh) | 2013-03-13 | 2014-12-01 | Janssen Pharmaceutica Nv | 經取代之哌啶化合物及其作為食慾素受體調節劑之用途 |
| EP3057955B1 (en) | 2013-10-18 | 2018-04-11 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of prolferative diseases |
| AU2014337067B2 (en) * | 2013-10-18 | 2019-01-24 | Syros Pharmaceuticals, Inc. | Heteroaromatic compounds useful for the treatment of proliferative diseases |
| US10047070B2 (en) | 2013-10-18 | 2018-08-14 | Dana-Farber Cancer Institute, Inc. | Polycyclic inhibitors of cyclin-dependent kinase 7 (CDK7) |
| CN106458990B (zh) | 2014-04-04 | 2019-06-07 | 希洛斯医药品股份有限公司 | 细胞周期蛋白依赖性激酶7(cdk7)的抑制剂 |
| WO2016058544A1 (en) | 2014-10-16 | 2016-04-21 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (cdk7) |
| HK1246645A1 (zh) * | 2015-03-27 | 2018-09-14 | 达纳-法伯癌症研究所股份有限公司 | 细胞周期蛋白依赖性激酶的抑制剂 |
| US10702527B2 (en) | 2015-06-12 | 2020-07-07 | Dana-Farber Cancer Institute, Inc. | Combination therapy of transcription inhibitors and kinase inhibitors |
| EP3347018B1 (en) | 2015-09-09 | 2021-09-01 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinases |
| WO2018098361A1 (en) | 2016-11-22 | 2018-05-31 | Dana-Farber Cancer Institute, Inc. | Inhibitors of cyclin-dependent kinase 12 (cdk12) and uses thereof |
| US10969394B2 (en) | 2016-11-28 | 2021-04-06 | Dana-Farber Cancer Institute, Inc. | Reagents and methods for analysis of proteins and metabolites targeted by covalent probes |
| US12187701B2 (en) | 2018-06-25 | 2025-01-07 | Dana-Farber Cancer Institute, Inc. | Taire family kinase inhibitors and uses thereof |
| AU2019395255B2 (en) * | 2018-12-14 | 2025-02-27 | Dana-Farber Cancer Institute, Inc. | Pyrazolopyridine inhibitors of c-Jun-N-terminal kinases and uses thereof |
| JP7660063B2 (ja) | 2018-12-28 | 2025-04-10 | ダナ－ファーバー キャンサー インスティテュート， インコーポレイテッド | サイクリン依存性キナーゼ７のインヒビターおよびそれらの使用 |
| US20230114207A1 (en) * | 2019-12-24 | 2023-04-13 | Dana-Farber Cancer Institute, Inc. | The combination of cyclin dependent kinase 7 inhibitor and immunotherapy for treatment of cancer |
-
2017
- 2017-11-22 WO PCT/US2017/063132 patent/WO2018098361A1/en not_active Ceased
- 2017-11-22 CA CA3041563A patent/CA3041563C/en active Active
- 2017-11-22 US US16/462,892 patent/US11306070B2/en active Active
- 2017-11-22 EP EP17817467.8A patent/EP3544971B1/en active Active
- 2017-11-22 JP JP2019527379A patent/JP7258748B2/ja active Active
- 2017-11-22 AU AU2017363307A patent/AU2017363307B2/en active Active
-
2022
- 2022-03-07 US US17/688,822 patent/US11932625B2/en active Active
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