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 (enExample) | 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 (enExample) |
| EP (1) | EP3143015B1 (enExample) |
| JP (1) | JP6468611B2 (enExample) |
| CN (1) | CN106687457B (enExample) |
| WO (1) | WO2015175632A1 (enExample) |
Families Citing this family (52)
| 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 |
| AU2013204563B2 (en) | 2012-05-05 | 2016-05-19 | Takeda Pharmaceutical Company Limited | 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 |
| EP3157916B1 (en) * | 2014-06-19 | 2018-12-12 | ARIAD Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| US10259820B2 (en) * | 2014-10-11 | 2019-04-16 | Shanghai Hansoh Biomedical Co., Ltd. | EGFR inhibitor, preparation method and use thereof |
| 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 |
| WO2016173438A1 (zh) * | 2015-04-29 | 2016-11-03 | 南京明德新药研发股份有限公司 | 稠环或三环芳基嘧啶化合物用作激酶抑制剂 |
| US20210323976A1 (en) * | 2015-05-13 | 2021-10-21 | 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 |
| KR20180105161A (ko) | 2016-01-07 | 2018-09-27 | 씨에스 파마테크 리미티드 | Egfr 티로신 키나제의 임상적으로 중요한 돌연변이체의 선택적 억제제 |
| 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 |
| ES2863925T3 (es) * | 2016-09-19 | 2021-10-13 | Nanjing Chuangte Pharmaceutical Tech Co Ltd | Derivados de 3-(pirimidinamina 4,5-sustituida)fenilo deuterados y aplicaciones de los mismos |
| JOP20190073A1 (ar) | 2016-10-31 | 2019-04-07 | Taiho Pharmaceutical Co Ltd | مثبط انتقائي لمستقبل عامل نمو بشروي (egfr) لطافر إدخال exon 20 |
| WO2018119441A1 (en) | 2016-12-23 | 2018-06-28 | Arvinas, Inc. | Egfr proteolysis targeting chimeric molecules and associated methods of use |
| 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 |
| MY198379A (en) | 2017-07-28 | 2023-08-28 | Yuhan Corp | Improved Process for Preparing Aminopyrimidine Derivatives |
| US11701359B2 (en) | 2017-09-01 | 2023-07-18 | Taiho Pharmaceutical Co., Ltd. | Exon 18 and/or exon 21 mutant EGFR selective inhibitor |
| 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 |
| BR112021012687A2 (pt) | 2018-12-28 | 2021-09-28 | Taiho Pharmaceutical Co., Ltd. | Inibidor de egfr resistente a tratamento de mutante l718 e/ou l792 |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| CA3134261A1 (en) | 2019-03-19 | 2020-09-24 | Voronoi Inc. | 6-(isooxazolidin-2-yl)-n-phenylpyrimidin-4-amine derivatives as inhibitors of epidermal growth factor receptors |
| BR112021019998B1 (pt) * | 2019-04-24 | 2024-01-16 | The Broad Institute, Inc. | 4h-pirrolo[3,2-c]piridin-4-ona, seus usos, composição farmacêutica, e kit de partes |
| US12433597B2 (en) * | 2019-06-04 | 2025-10-07 | Trisalus Life Sciences, Inc. | Atraumatic occlusive system with compartment for measurement of vascular pressure change |
| CA3150927A1 (en) | 2019-09-13 | 2021-03-18 | Holistick Medical | Medical implant, delivery device, method of producing a medical implant, and method of delivering a medical implant |
| 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 |
| US20210161897A1 (en) | 2019-11-12 | 2021-06-03 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US12466825B2 (en) * | 2019-11-14 | 2025-11-11 | Amgen Inc. | Synthesis of KRAS G12C inhibitor compound |
| AU2021211871A1 (en) | 2020-01-20 | 2022-09-08 | Astrazeneca Ab | Epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| US20230126204A1 (en) | 2020-02-03 | 2023-04-27 | Boehringer Ingelheim International Gmbh | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS |
| CN115052881B (zh) * | 2020-02-03 | 2024-07-09 | 勃林格殷格翰国际有限公司 | 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 |
| 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 |
| EP4217070A1 (en) | 2020-09-23 | 2023-08-02 | Scorpion Therapeutics, Inc. | Pyrrolo[3,2-c]pyridin-4-one derivatives useful in the treatment of cancer |
| WO2022072645A2 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Methods for treating cancer |
| 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 |
| JP2023548657A (ja) | 2020-10-09 | 2023-11-20 | スコーピオン セラピューティクス インコーポレイテッド | がんの処置に使用するための、ｅｇｆｒおよび／またはｈｅｒ２のヘテロ環阻害剤 |
| 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 |
| EP4323356A1 (en) | 2021-04-13 | 2024-02-21 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| 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 |
| IL315848A (en) | 2022-03-31 | 2024-11-01 | Astrazeneca Ab | Epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors in combination with an AKT inhibitor for cancer treatment |
| 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 |
| KR20250029133A (ko) | 2022-06-27 | 2025-03-04 | 아스트라제네카 아베 | 암 치료를 위한 표피성장인자 수용체 티로신 키나제 억제제를 포함하는 조합물 |
| CN119654152A (zh) | 2022-07-08 | 2025-03-18 | 阿斯利康(瑞典)有限公司 | 与hgf-受体抑制剂组合用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂 |
| CN120359211A (zh) * | 2022-12-08 | 2025-07-22 | 盐野义制药株式会社 | 具有血清素受体结合活性的含氮杂环和碳环衍生物 |
| 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 |
| WO2024254266A1 (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 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0311274D0 (en) * | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
| SI1948180T1 (sl) * | 2005-11-11 | 2013-06-28 | Boehringer Ingelheim International Gmbh | Kombinacijsko zdravljenje raka, ki obsega EGFR/HER2 inhibitorje |
| ES2417148T3 (es) * | 2007-06-08 | 2013-08-06 | Genentech, Inc. | Marcadores de expresión génica de la resistencia tumoral al tratamiento con inhibidor de HER2 |
| EP2361248B1 (en) * | 2008-06-27 | 2018-09-19 | Celgene CAR LLC | Heteroaryl compounds 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 |
| JP5918693B2 (ja) * | 2009-05-05 | 2016-05-18 | 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 | Ｅｇｆｒ阻害剤及び疾患の治療方法 |
| US8563567B2 (en) * | 2009-12-30 | 2013-10-22 | Arqule, Inc. | Substituted heterocyclic compounds |
| PT3009431T (pt) * | 2011-07-27 | 2017-12-26 | Astrazeneca Ab | Compostos de 2-(2,4,5-anilino-substituídos)pirimidina como moduladores úteis do egfr para o tratamento do cancro |
-
2015
- 2015-05-13 JP JP2016567502A patent/JP6468611B2/ja not_active Expired - Fee Related
- 2015-05-13 CN CN201580037958.0A patent/CN106687457B/zh not_active Expired - Fee Related
- 2015-05-13 WO PCT/US2015/030522 patent/WO2015175632A1/en not_active Ceased
- 2015-05-13 EP EP15792086.9A patent/EP3143015B1/en active Active
- 2015-05-13 US US15/310,349 patent/US20170166598A1/en not_active Abandoned
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