JP2017518282A5 - - Google Patents
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- Publication number
- JP2017518282A5 JP2017518282A5 JP2016567502A JP2016567502A JP2017518282A5 JP 2017518282 A5 JP2017518282 A5 JP 2017518282A5 JP 2016567502 A JP2016567502 A JP 2016567502A JP 2016567502 A JP2016567502 A JP 2016567502A JP 2017518282 A5 JP2017518282 A5 JP 2017518282A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- pharmaceutically acceptable
- compound
- halo
- acceptable form
- 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 28
- 150000001875 compounds Chemical class 0.000 claims 22
- 125000001475 halogen functional group Chemical group 0.000 claims 18
- 125000001072 heteroaryl group Chemical group 0.000 claims 17
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000000623 heterocyclic group Chemical group 0.000 claims 12
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 12
- 125000003342 alkenyl group Chemical group 0.000 claims 11
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 11
- 125000003118 aryl group Chemical group 0.000 claims 10
- 125000000304 alkynyl group Chemical group 0.000 claims 9
- 125000000753 cycloalkyl group Chemical group 0.000 claims 9
- 150000002148 esters Chemical class 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- XEEYBQQBJWHFJM-UHFFFAOYSA-N Iron Chemical compound [Fe] XEEYBQQBJWHFJM-UHFFFAOYSA-N 0.000 claims 7
- 125000002252 acyl group Chemical group 0.000 claims 7
- 150000001408 amides Chemical class 0.000 claims 7
- 125000004104 aryloxy group Chemical group 0.000 claims 7
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 7
- 229910052757 nitrogen Inorganic materials 0.000 claims 6
- 125000005864 sulfonamidyl group Chemical group 0.000 claims 5
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 5
- 125000004453 alkoxycarbonyl group Chemical group 0.000 claims 4
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 4
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 4
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 claims 3
- BVKZGUZCCUSVTD-UHFFFAOYSA-L Carbonate Chemical compound [O-]C([O-])=O BVKZGUZCCUSVTD-UHFFFAOYSA-L 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 229910019142 PO4 Inorganic materials 0.000 claims 3
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 3
- -1 amino, carbonyl Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 239000004202 carbamide Substances 0.000 claims 3
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims 3
- 239000010452 phosphate Substances 0.000 claims 3
- ACVYVLVWPXVTIT-UHFFFAOYSA-M phosphinate Chemical compound [O-][PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-M 0.000 claims 3
- UEZVMMHDMIWARA-UHFFFAOYSA-M phosphonate Chemical compound [O-]P(=O)=O UEZVMMHDMIWARA-UHFFFAOYSA-M 0.000 claims 3
- BDHFUVZGWQCTTF-UHFFFAOYSA-M sulfonate Chemical compound [O-]S(=O)=O BDHFUVZGWQCTTF-UHFFFAOYSA-M 0.000 claims 3
- 125000004962 sulfoxyl group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 2
- 125000005110 aryl thio group Chemical group 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical compound O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 claims 2
- 125000002813 thiocarbonyl group Chemical group *C(*)=S 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010009944 Colon cancer Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- OAKJQQAXSVQMHS-UHFFFAOYSA-N Hydrazine Chemical compound NN OAKJQQAXSVQMHS-UHFFFAOYSA-N 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 125000004183 alkoxy alkyl group Chemical group 0.000 claims 1
- 125000003368 amide group Chemical group 0.000 claims 1
- 125000004103 aminoalkyl group Chemical group 0.000 claims 1
- 125000004429 atom Chemical group 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 125000004432 carbon atom Chemical group C* 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 125000004415 heterocyclylalkyl group Chemical group 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
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 1
- MPQXHAGKBWFSNV-UHFFFAOYSA-N oxidophosphanium Chemical class [PH3]=O MPQXHAGKBWFSNV-UHFFFAOYSA-N 0.000 claims 1
- 125000004043 oxo group Chemical group O=* 0.000 claims 1
- AUONHKJOIZSQGR-UHFFFAOYSA-N oxophosphane Chemical compound P=O AUONHKJOIZSQGR-UHFFFAOYSA-N 0.000 claims 1
- 229910052760 oxygen Inorganic materials 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000000446 sulfanediyl group Chemical group *S* 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- MDDUHVRJJAFRAU-YZNNVMRBSA-N tert-butyl-[(1r,3s,5z)-3-[tert-butyl(dimethyl)silyl]oxy-5-(2-diphenylphosphorylethylidene)-4-methylidenecyclohexyl]oxy-dimethylsilane Chemical compound C1[C@@H](O[Si](C)(C)C(C)(C)C)C[C@H](O[Si](C)(C)C(C)(C)C)C(=C)\C1=C/CP(=O)(C=1C=CC=CC=1)C1=CC=CC=C1 MDDUHVRJJAFRAU-YZNNVMRBSA-N 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
- 239000003981 vehicle Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461992742P | 2014-05-13 | 2014-05-13 | |
| US61/992,742 | 2014-05-13 | ||
| PCT/US2015/030522 WO2015175632A1 (en) | 2014-05-13 | 2015-05-13 | Heteroaryl compounds for kinase inhibition |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017518282A JP2017518282A (ja) | 2017-07-06 |
| JP2017518282A5 true JP2017518282A5 (https=) | 2018-06-21 |
| JP6468611B2 JP6468611B2 (ja) | 2019-02-13 |
Family
ID=54480594
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016567502A Expired - Fee Related JP6468611B2 (ja) | 2014-05-13 | 2015-05-13 | キナーゼ阻害のためのヘテロアリール化合物 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20170166598A1 (https=) |
| EP (1) | EP3143015B1 (https=) |
| JP (1) | JP6468611B2 (https=) |
| CN (1) | CN106687457B (https=) |
| WO (1) | WO2015175632A1 (https=) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2704572B1 (en) | 2011-05-04 | 2015-12-30 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| WO2013169401A1 (en) | 2012-05-05 | 2013-11-14 | Ariad Pharmaceuticals, Inc. | Compounds for inhibiting cell proliferation in egfr-driven cancers |
| US9611283B1 (en) | 2013-04-10 | 2017-04-04 | Ariad Pharmaceuticals, Inc. | Methods for inhibiting cell proliferation in ALK-driven cancers |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| EP3778584A1 (en) * | 2014-06-19 | 2021-02-17 | ARIAD Pharmaceuticals, Inc. | Production process of 2-chloro-4-heteroaryl-pyrimidine derivatives |
| WO2016054987A1 (zh) * | 2014-10-11 | 2016-04-14 | 上海翰森生物医药科技有限公司 | Egfr抑制剂及其制备和应用 |
| CN105085489B (zh) | 2014-11-05 | 2019-03-01 | 益方生物科技（上海）有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| CA2984586C (en) | 2015-04-29 | 2021-02-16 | Guangdong Zhongsheng Pharmaceutical Co., Ltd. | Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor |
| EP3294712A4 (en) * | 2015-05-13 | 2018-11-07 | ARIAD Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| CN106810553B (zh) * | 2015-11-30 | 2020-03-17 | 江苏正大丰海制药有限公司 | 3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 |
| TWI726968B (zh) | 2016-01-07 | 2021-05-11 | 開曼群島商Ｃｓ醫藥技術公司 | Egfr酪胺酸激酶之臨床重要突變體之選擇性抑制劑 |
| CN107344934B (zh) * | 2016-05-04 | 2019-08-23 | 江苏正大丰海制药有限公司 | 药物活性物质的固体形式 |
| WO2018050108A1 (zh) * | 2016-09-19 | 2018-03-22 | 江苏正大丰海制药有限公司 | 氘代3-(4,5-取代氨基嘧啶)苯基衍生物及其应用 |
| WO2018079310A1 (ja) | 2016-10-31 | 2018-05-03 | 大鵬薬品工業株式会社 | エクソン２０挿入変異型ｅｇｆｒ選択的阻害剤 |
| JP2020505327A (ja) | 2016-12-23 | 2020-02-20 | アルビナス・オペレーションズ・インコーポレイテッドＡｒｖｉｎａｓ Ｏｐｅｒａｔｉｏｎｓ， Ｉｎｃ． | Ｅｇｆｒタンパク質分解標的化キメラ分子およびその関連する使用方法 |
| AR111469A1 (es) | 2017-04-21 | 2019-07-17 | Yuhan Corp | Sal de un compuesto del derivado de aminopiridina, una forma cristalina de la misma, y un proceso para preparar la misma |
| SG11201913517UA (en) | 2017-07-28 | 2020-02-27 | Yuhan Corp | Improved process for preparing aminopyrimidine derivatives |
| PL3677266T3 (pl) | 2017-09-01 | 2024-07-01 | Taiho Pharmaceutical Co., Ltd. | Selektywny inhibitor egfr z mutacją w eksonie 18 i/lub eksonie 21 |
| EP3613738A1 (en) * | 2018-08-23 | 2020-02-26 | Lead Discovery Center GmbH | 4-substituted pyrrolo[2,3-b]pyridine as erbb modulators useful for treating cancer |
| ES3033635T3 (en) * | 2018-12-28 | 2025-08-06 | Taiho Pharmaceutical Co Ltd | L718 and/or l792 mutant treatment-resistant egfr inhibitor for use in the treatment of cancer |
| PT3943491T (pt) | 2019-03-19 | 2025-07-28 | Voronoi Inc | Derivado de heteroarilo, método para a produção do mesmo e composição farmacêutica que compreende o mesmo como componente eficaz |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| DK3959211T3 (da) * | 2019-04-24 | 2026-04-27 | Bayer Ag | 4h-pyrrol[3,2-c]pyridin-4-on-forbindelser |
| US12433597B2 (en) * | 2019-06-04 | 2025-10-07 | Trisalus Life Sciences, Inc. | Atraumatic occlusive system with compartment for measurement of vascular pressure change |
| MX2022003004A (es) | 2019-09-13 | 2022-04-07 | Holistick Medical | Implante medico, dispositivo de colocacion, metodo de produccion de un implante medico y metodo de colocacion de un implante medico. |
| CN110746307B (zh) * | 2019-11-01 | 2021-07-06 | 韶远科技（上海)有限公司 | 一种1-硝基-2-乙基-4-氟苯的制备方法 |
| WO2021094379A1 (en) | 2019-11-12 | 2021-05-20 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| JP2023501528A (ja) | 2019-11-14 | 2023-01-18 | アムジエン・インコーポレーテツド | Ｋｒａｓ ｇ１２ｃ阻害剤化合物の改善された合成 |
| WO2021148396A1 (en) | 2020-01-20 | 2021-07-29 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| JP7626774B2 (ja) * | 2020-02-03 | 2025-02-04 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン |
| EP4100409B1 (en) | 2020-02-03 | 2024-08-28 | Boehringer Ingelheim International GmbH | [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors |
| US11608343B2 (en) | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| US20210369709A1 (en) | 2020-05-27 | 2021-12-02 | Astrazeneca Ab | EGFR TKIs FOR USE IN THE TREATMENT OF NON-SMALL CELL LUNG CANCER |
| KR20230094197A (ko) | 2020-09-23 | 2023-06-27 | 스코르피온 테라퓨틱스, 인코퍼레이티드 | 암 치료에 유용한 피롤로[3,2-c]피리딘-4-온 유도체들 |
| WO2022072632A1 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| TW202229282A (zh) | 2020-09-30 | 2022-08-01 | 美商史考皮恩治療有限公司 | 治療癌症之方法 |
| WO2022072645A2 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| KR20230107419A (ko) | 2020-10-09 | 2023-07-14 | 스코르피온 테라퓨틱스, 인코퍼레이티드 | 암 치료 방법 |
| WO2022094271A1 (en) | 2020-10-30 | 2022-05-05 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| WO2022098992A1 (en) | 2020-11-05 | 2022-05-12 | Scorpion Therapeutics, Inc. | Use of macrocyclic compounds in methods of treating cancer |
| WO2022197913A1 (en) | 2021-03-18 | 2022-09-22 | Scorpion Therapeutics, Inc. | Bicyclic derivatives which can be used to treat cancer |
| TW202309022A (zh) | 2021-04-13 | 2023-03-01 | 美商努法倫特公司 | 用於治療具egfr突變之癌症之胺基取代雜環 |
| TW202317106A (zh) * | 2021-08-27 | 2023-05-01 | 南韓商柳韓洋行 | 作為egfr抑制劑之取代胺基吡啶化合物 |
| WO2023173083A1 (en) | 2022-03-11 | 2023-09-14 | Scorpion Therapeutics, Inc. | Tetrahydroindole derivatives as egfr and/or her2 inhibtors useful for the treatment of cancer |
| JP2025510910A (ja) | 2022-03-31 | 2025-04-15 | アストラゼネカ・アクチエボラーグ | 癌の処置のための、ａｋｔ阻害剤との組み合わせにおける上皮成長因子受容体（ｅｇｆｒ）チロシンキナーゼ阻害剤 |
| CN114957224B (zh) * | 2022-05-17 | 2024-03-19 | 浙大城市学院 | 一种肿瘤低氧靶向的egfr抑制剂及其应用 |
| CA3259492A1 (en) | 2022-06-27 | 2024-01-04 | Astrazeneca Ab | COMBINATIONS INVOLVING EPIDERMAL GROWTH FACTOR RECEPTOR TYROSINE KINASE INHIBITORS FOR THE TREATMENT OF CANCER |
| KR20250044679A (ko) | 2022-07-08 | 2025-04-01 | 아스트라제네카 아베 | 암 치료를 위한 hgf-수용체 억제제와 병용의 상피 성장 인자 수용체 티로신 키나아제 억제제 |
| WO2024122617A1 (ja) * | 2022-12-08 | 2024-06-13 | 塩野義製薬株式会社 | セロトニン受容体結合活性を有する含窒素複素環および炭素環誘導体 |
| WO2024254298A1 (en) | 2023-06-08 | 2024-12-12 | Scorpion Therapeutics, Inc. | A 1,5-dihydro-4h-pyrrolo[3,2-c] pyridin-4-one for use in the treatment of cancer |
| CN121712773A (zh) | 2023-06-08 | 2026-03-20 | 安塔列斯疗法股份有限公司 | 1,5-二氢-4h-吡咯并[3,2-c]吡啶-4-酮用于癌症治疗 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0311274D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| PT1948180E (pt) * | 2005-11-11 | 2013-05-10 | Boehringer Ingelheim Int | Tratamento de combinação de cancro compreendendo inibidores de egfr/her2 |
| PL2171090T3 (pl) * | 2007-06-08 | 2013-09-30 | Genentech Inc | Markery ekspresji genów odporności guza na leczenie hamujące HER2 |
| NZ603525A (en) * | 2008-06-27 | 2015-02-27 | Celgene Avilomics Res Inc | Pyrimidine based compound and uses thereof |
| CN101723936B (zh) * | 2008-10-27 | 2014-01-15 | 上海睿星基因技术有限公司 | 激酶抑制剂及其在药学中的用途 |
| US9908884B2 (en) * | 2009-05-05 | 2018-03-06 | Dana-Farber Cancer Institute, Inc. | EGFR inhibitors and methods of treating disorders |
| WO2011082266A2 (en) * | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted heterocyclic compounds |
| EP4119551A1 (en) * | 2011-07-27 | 2023-01-18 | Astrazeneca AB | 2-(2,4,5-substituted-anilino)pyrimidine compounds |
-
2015
- 2015-05-13 JP JP2016567502A patent/JP6468611B2/ja not_active Expired - Fee Related
- 2015-05-13 EP EP15792086.9A patent/EP3143015B1/en active Active
- 2015-05-13 WO PCT/US2015/030522 patent/WO2015175632A1/en not_active Ceased
- 2015-05-13 CN CN201580037958.0A patent/CN106687457B/zh not_active Expired - Fee Related
- 2015-05-13 US US15/310,349 patent/US20170166598A1/en not_active Abandoned
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