JP2020504747A5 - - Google Patents
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- Publication number
- JP2020504747A5 JP2020504747A5 JP2019534709A JP2019534709A JP2020504747A5 JP 2020504747 A5 JP2020504747 A5 JP 2020504747A5 JP 2019534709 A JP2019534709 A JP 2019534709A JP 2019534709 A JP2019534709 A JP 2019534709A JP 2020504747 A5 JP2020504747 A5 JP 2020504747A5
- Authority
- JP
- Japan
- Prior art keywords
- fluoro
- methyl
- pyridin
- imidazole
- heterocyclyl
- 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
- RAXXELZNTBOGNW-UHFFFAOYSA-N imidazole Natural products C1=CNC=N1 RAXXELZNTBOGNW-UHFFFAOYSA-N 0.000 claims 55
- 150000001875 compounds Chemical class 0.000 claims 41
- -1 NH 2 Inorganic materials 0.000 claims 36
- 125000000623 heterocyclic group Chemical group 0.000 claims 24
- 125000000217 alkyl group Chemical group 0.000 claims 21
- LJXQPZWIHJMPQQ-UHFFFAOYSA-N pyrimidin-2-amine Chemical compound NC1=NC=CC=N1 LJXQPZWIHJMPQQ-UHFFFAOYSA-N 0.000 claims 10
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 9
- 229910052736 halogen Inorganic materials 0.000 claims 8
- 150000002367 halogens Chemical class 0.000 claims 8
- 125000003118 aryl group Chemical group 0.000 claims 7
- 125000001072 heteroaryl group Chemical group 0.000 claims 7
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 125000003545 alkoxy group Chemical group 0.000 claims 6
- 125000005842 heteroatom Chemical group 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 4
- OJHWPOJTJKJBLA-UHFFFAOYSA-N 2,3,3a,4-tetrahydro-1h-benzimidazole Chemical compound C1C=CC=C2NCNC21 OJHWPOJTJKJBLA-UHFFFAOYSA-N 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- PXBRQCKWGAHEHS-UHFFFAOYSA-N dichlorodifluoromethane Chemical compound FC(F)(Cl)Cl PXBRQCKWGAHEHS-UHFFFAOYSA-N 0.000 claims 3
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 2
- HYZJCKYKOHLVJF-UHFFFAOYSA-N 1H-benzimidazole Chemical compound C1=CC=C2NC=NC2=C1 HYZJCKYKOHLVJF-UHFFFAOYSA-N 0.000 claims 2
- JQTMGOLZSBTZMS-UHFFFAOYSA-N 4-methylpiperazine-1-carbaldehyde Chemical compound CN1CCN(C=O)CC1 JQTMGOLZSBTZMS-UHFFFAOYSA-N 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 150000002460 imidazoles Chemical class 0.000 claims 2
- 239000003112 inhibitor Substances 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims 2
- 125000006413 ring segment Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- GWZRZYQFXWGKIQ-UHFFFAOYSA-N 2-(2-amino-6-methylpyrimidin-4-yl)sulfanyl-n-methylacetamide Chemical compound CNC(=O)CSC1=CC(C)=NC(N)=N1 GWZRZYQFXWGKIQ-UHFFFAOYSA-N 0.000 claims 1
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 1
- UHYVUSGJRCYGIS-UHFFFAOYSA-N 5-fluoro-4-(6-fluoro-1-methyl-1,2,3,4-tetrahydropyrido[1,2-a]benzimidazol-8-yl)-N-[5-[(4-methylpiperazin-1-yl)methyl]pyrimidin-2-yl]pyrimidin-2-amine Chemical compound FC=1C(=NC(=NC=1)NC1=NC=C(C=N1)CN1CCN(CC1)C)C1=CC2=C(N=C3N2C(CCC3)C)C(=C1)F UHYVUSGJRCYGIS-UHFFFAOYSA-N 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
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 108010025464 Cyclin-Dependent Kinase 4 Proteins 0.000 claims 1
- 108010025468 Cyclin-Dependent Kinase 6 Proteins 0.000 claims 1
- 102100036252 Cyclin-dependent kinase 4 Human genes 0.000 claims 1
- 102100026804 Cyclin-dependent kinase 6 Human genes 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000025205 Mantle-Cell Lymphoma Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 0.000 claims 1
- SDUUDIZDGDPGHT-UHFFFAOYSA-N N-[5-(4-cyclopropylpiperazin-1-yl)pyridin-2-yl]-5-fluoro-4-(9-fluoro-4-methyl-3,4-dihydro-1H-[1,4]oxazino[4,3-a]benzimidazol-7-yl)pyrimidin-2-amine Chemical compound C1(CC1)N1CCN(CC1)C=1C=CC(=NC=1)NC1=NC=C(C(=N1)C1=CC2=C(N=C3COCC(N32)C)C(=C1)F)F SDUUDIZDGDPGHT-UHFFFAOYSA-N 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010042971 T-cell lymphoma Diseases 0.000 claims 1
- 208000027585 T-cell non-Hodgkin lymphoma Diseases 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- HSUGRBWQSSZJOP-RTWAWAEBSA-N diltiazem Chemical group C1=CC(OC)=CC=C1[C@H]1[C@@H](OC(C)=O)C(=O)N(CCN(C)C)C2=CC=CC=C2S1 HSUGRBWQSSZJOP-RTWAWAEBSA-N 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 208000005017 glioblastoma Diseases 0.000 claims 1
- 239000001257 hydrogen Substances 0.000 claims 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 claims 1
- 206010024627 liposarcoma Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000001301 oxygen Substances 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 229940002612 prodrug Drugs 0.000 claims 1
- 239000000651 prodrug Substances 0.000 claims 1
- LETVJWLLIMJADE-UHFFFAOYSA-N pyridazin-3-amine Chemical compound NC1=CC=CN=N1 LETVJWLLIMJADE-UHFFFAOYSA-N 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2016111457 | 2016-12-22 | ||
| CNPCT/CN2016/111457 | 2016-12-22 | ||
| CN2017080661 | 2017-04-14 | ||
| CNPCT/CN2017/080661 | 2017-04-14 | ||
| PCT/CN2017/117950 WO2018113771A1 (en) | 2016-12-22 | 2017-12-22 | Benzimidazole derivatives, preparation methods and uses theirof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020504747A JP2020504747A (ja) | 2020-02-13 |
| JP2020504747A5 true JP2020504747A5 (https=) | 2021-01-14 |
| JP7105781B2 JP7105781B2 (ja) | 2022-07-25 |
Family
ID=62624617
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019534709A Active JP7105781B2 (ja) | 2016-12-22 | 2017-12-22 | ベンズイミダゾール誘導体、調製方法およびそれらの使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US11053238B2 (https=) |
| EP (1) | EP3559000B1 (https=) |
| JP (1) | JP7105781B2 (https=) |
| KR (1) | KR102543603B1 (https=) |
| CN (1) | CN110234652B (https=) |
| AU (1) | AU2017379041B2 (https=) |
| CA (1) | CA3047876C (https=) |
| DK (1) | DK3559000T3 (https=) |
| ES (1) | ES2917377T3 (https=) |
| TW (1) | TWI732083B (https=) |
| WO (1) | WO2018113771A1 (https=) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106608879A (zh) * | 2015-10-27 | 2017-05-03 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| TW201920141A (zh) | 2017-08-15 | 2019-06-01 | 中國大陸商北京軒義醫藥科技有限公司 | Cdk4/6抑制劑及其用途 |
| JP2021514359A (ja) | 2018-02-15 | 2021-06-10 | ニューベイション・バイオ・インコーポレイテッドＮｕｖａｔｉｏｎ Ｂｉｏ Ｉｎｃ． | キナーゼ阻害剤としての複素環式化合物 |
| CN113861191B (zh) | 2018-06-21 | 2023-09-19 | 贝达药业股份有限公司 | 抑制cdk4/6活性化合物的晶型及其应用 |
| MA55909A (fr) * | 2019-05-05 | 2022-03-16 | Qilu Regor Therapeutics Inc | Inhibiteurs de cdk |
| CN111138455B (zh) * | 2020-01-16 | 2022-03-04 | 郑州大学 | 一种手性四氢呋喃并恶嗪稠合苯并咪唑衍生物及其制备方法和用途 |
| CN115427414A (zh) * | 2020-04-28 | 2022-12-02 | 贝达药业股份有限公司 | 稠环化合物及其在医药上的应用 |
| KR102269420B1 (ko) | 2020-09-18 | 2021-06-24 | 전용석 | 긴급대피용 마스크장치 |
| WO2022113003A1 (en) | 2020-11-27 | 2022-06-02 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| WO2022149057A1 (en) | 2021-01-05 | 2022-07-14 | Rhizen Pharmaceuticals Ag | Cdk inhibitors |
| MX2023008896A (es) * | 2021-02-03 | 2023-08-09 | Tuojie Biotech Shanghai Co Ltd | Inhibidor triciclico fusionado de la cinasa dependiente de ciclina, y metodo de preparacion del mismo y uso farmaceutico del mismo. |
| CN112979567B (zh) * | 2021-03-05 | 2023-07-18 | 中国医科大学 | Cdk12小分子抑制剂的化合物及其应用 |
| CN117222411B (zh) * | 2021-03-24 | 2026-03-27 | 贝达药业股份有限公司 | 药物组合、包含其的试剂盒及其用途 |
| WO2023131179A1 (zh) * | 2022-01-05 | 2023-07-13 | 贝达药业股份有限公司 | 苯并咪唑衍生物或其盐在治疗白血病中的用途 |
| CN119522226A (zh) * | 2022-08-01 | 2025-02-25 | 江苏恒瑞医药股份有限公司 | 一种稠三环类衍生物的晶型及制备方法 |
| WO2025016439A1 (zh) * | 2023-07-19 | 2025-01-23 | 浙江同源康医药股份有限公司 | 用作cdk2/4蛋白激酶抑制剂的化合物及其应用 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PA8852901A1 (es) | 2008-12-22 | 2010-07-27 | Lilly Co Eli | Inhibidores de proteina cinasa |
| WO2012002527A1 (ja) | 2010-07-02 | 2012-01-05 | あすか製薬株式会社 | 複素環化合物及びｐ２７Ｋｉｐ１分解阻害剤 |
| UA111756C2 (uk) | 2011-11-03 | 2016-06-10 | Ф. Хоффманн-Ля Рош Аг | Сполуки гетероарилпіридону та азапіридону як інгібітори тирозинкінази брутона |
| CA2954298A1 (en) | 2014-07-24 | 2016-01-28 | Beta Pharma, Inc. | 2-h-indazole derivatives as cyclin-dependent kinase (cdk) inhibitors and therapeutic uses thereof |
| AR104291A1 (es) | 2015-04-17 | 2017-07-12 | Abbvie Inc | Moduladores tricíclicos de la señalización por tnf |
| TWI696617B (zh) | 2015-04-28 | 2020-06-21 | 大陸商上海復尚慧創醫藥研究有限公司 | 特定蛋白質激酶抑制劑 |
| CN105153119B (zh) | 2015-09-11 | 2019-01-01 | 广州必贝特医药技术有限公司 | 吡啶嘧啶胺类化合物或吡啶吡啶胺类化合物及其应用 |
| CN106608879A (zh) | 2015-10-27 | 2017-05-03 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
-
2017
- 2017-12-22 WO PCT/CN2017/117950 patent/WO2018113771A1/en not_active Ceased
- 2017-12-22 US US16/471,415 patent/US11053238B2/en active Active
- 2017-12-22 EP EP17882916.4A patent/EP3559000B1/en active Active
- 2017-12-22 DK DK17882916.4T patent/DK3559000T3/da active
- 2017-12-22 TW TW106145306A patent/TWI732083B/zh active
- 2017-12-22 CA CA3047876A patent/CA3047876C/en active Active
- 2017-12-22 KR KR1020197020604A patent/KR102543603B1/ko active Active
- 2017-12-22 CN CN201780078241.XA patent/CN110234652B/zh active Active
- 2017-12-22 ES ES17882916T patent/ES2917377T3/es active Active
- 2017-12-22 JP JP2019534709A patent/JP7105781B2/ja active Active
- 2017-12-22 AU AU2017379041A patent/AU2017379041B2/en active Active
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