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 (cg-RX-API-DMAC7.html) | 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 (cg-RX-API-DMAC7.html) |
| EP (1) | EP3143015B1 (cg-RX-API-DMAC7.html) |
| JP (1) | JP6468611B2 (cg-RX-API-DMAC7.html) |
| CN (1) | CN106687457B (cg-RX-API-DMAC7.html) |
| WO (1) | WO2015175632A1 (cg-RX-API-DMAC7.html) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EA201391626A1 (ru) | 2011-05-04 | 2014-03-31 | Ариад Фармасьютикалз, Инк. | Соединения для ингибирования клеточной пролиферации в egfr-стимулированных типах рака |
| 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 |
| GB201311888D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compounds |
| GB201311891D0 (en) | 2013-07-03 | 2013-08-14 | Glaxosmithkline Ip Dev Ltd | Novel compound |
| US20180228907A1 (en) | 2014-04-14 | 2018-08-16 | Arvinas, Inc. | Cereblon ligands and bifunctional compounds comprising the same |
| SG11201610517PA (en) * | 2014-06-19 | 2017-01-27 | Ariad Pharma Inc | Heteroaryl compounds for kinase inhibition |
| AU2015330506B2 (en) * | 2014-10-11 | 2020-01-30 | Jiangsu Hansoh Pharmaceutical Group Co., Ltd. | EGFR inhibitor, and preparation and application thereof |
| CN111170998B (zh) | 2014-11-05 | 2023-04-11 | 益方生物科技(上海)股份有限公司 | 嘧啶或吡啶类化合物、其制备方法和医药用途 |
| EP3312179B1 (en) | 2015-04-29 | 2019-07-10 | Nanjing Sanhome Pharmaceutical Co., Ltd. | Fused-ring or tricyclic aryl pyrimidine compound used as kinase inhibitor |
| JP6863901B2 (ja) * | 2015-05-13 | 2021-04-28 | アリアド ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| 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 |
| WO2017120429A1 (en) | 2016-01-07 | 2017-07-13 | CS Pharmasciences, Inc. | Selective inhibitors of clinically important mutants of the egfr tyrosine kinase |
| 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 |
| AU2017326029B2 (en) * | 2016-09-19 | 2019-11-21 | Nanjing Chuangte Pharmaceutical Technology Co., Ltd | Deuterated 3-(4,5-substituted pyrimidinamine) phenyl derivatives and applications thereof |
| JOP20190073A1 (ar) | 2016-10-31 | 2019-04-07 | Taiho Pharmaceutical Co Ltd | مثبط انتقائي لمستقبل عامل نمو بشروي (egfr) لطافر إدخال exon 20 |
| EP3559002A4 (en) | 2016-12-23 | 2021-02-17 | Arvinas Operations, Inc. | CHEMERICAL MOLECULES TARGETING EGFR PROTEOLYSIS AND RELATED 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 |
| BR112020001278A2 (pt) | 2017-07-28 | 2020-07-21 | Yuhan Corporation | processo aprimorado para preparar derivados de aminopirimidina |
| EP3677266B1 (en) | 2017-09-01 | 2024-01-17 | 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 |
| DK3902548T3 (da) | 2018-12-28 | 2025-07-07 | Taiho Pharmaceutical Co Ltd | L718- og/eller l792-mutant-behandlingsresistent egfr-inhibitor til anvendelse i behandlingen af kræft |
| KR102318875B1 (ko) | 2019-03-19 | 2021-11-01 | 보로노이 주식회사 | 헤테로아릴 유도체, 이를 제조하는 방법, 및 이를 유효성분으로 포함하는 약학적 조성물 |
| US12157730B2 (en) | 2019-03-19 | 2024-12-03 | Voronoi Inc. | Heteroaryl derivative, method for producing same, and pharmaceutical composition comprising same as effective component |
| AU2020262221B2 (en) * | 2019-04-24 | 2025-11-20 | Bayer Aktiengesellschaft | 4H-pyrrolo(3,2-c)pyridin-4-one compounds |
| US12433597B2 (en) * | 2019-06-04 | 2025-10-07 | Trisalus Life Sciences, Inc. | Atraumatic occlusive system with compartment for measurement of vascular pressure change |
| CN114502110A (zh) | 2019-09-13 | 2022-05-13 | 霍利斯蒂克医疗公司 | 医疗植入物、递送装置、制作医疗植入物的方法以及递送医疗植入物的方法 |
| 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 |
| KR20220101125A (ko) * | 2019-11-14 | 2022-07-19 | 암젠 인크 | Kras g12c 억제제 화합물의 개선된 합성 |
| CN114980883A (zh) | 2020-01-20 | 2022-08-30 | 阿斯利康(瑞典)有限公司 | 用于治疗癌症的表皮生长因子受体酪氨酸激酶抑制剂 |
| WO2021156180A1 (en) | 2020-02-03 | 2021-08-12 | Boehringer Ingelheim International Gmbh | [1,3]diazino[5,4-d]pyrimidines as her2 inhibitors |
| CN115052878B (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 |
| WO2022066734A1 (en) | 2020-09-23 | 2022-03-31 | 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 |
| WO2022072634A1 (en) | 2020-09-30 | 2022-04-07 | Scorpion Therapeutics, Inc. | Bicyclic compounds for use in the treatment cancer |
| AU2021358596A1 (en) | 2020-10-09 | 2023-05-25 | Antares Therapeutics, Inc. | Heterocyclic inhibitors of egfr and/or her2, for use in the treatment of cancer |
| 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 |
| CA3213079A1 (en) | 2021-04-13 | 2022-10-20 | Kristin Lynne ANDREWS | 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 |
| AU2023246862A1 (en) | 2022-03-31 | 2024-10-31 | Astrazeneca Ab | Epidermal growth factor receptor (egfr) tyrosine kinase inhibitors in combination with an akt inhibitor for the treatment of cancer |
| 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 |
| EP4543920A1 (en) | 2022-06-27 | 2025-04-30 | Astrazeneca AB | Combinations involving epidermal growth factor receptor tyrosine kinase inhibitors for the treatment of cancer |
| CA3261476A1 (en) | 2022-07-08 | 2024-01-11 | Astrazeneca Ab | Epidermal Growth Factor Receptor Tyrosine Kinase Inhibitors in Combination with HGF Receptor Inhibitors for the Treatment of Cancer |
| EP4631938A1 (en) * | 2022-12-08 | 2025-10-15 | Shionogi & Co., Ltd | Nitrogen-containing heterocycle with serotonin receptor-binding activity and carbocyclic derivative |
| 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 |
| EP2340837B1 (en) * | 2005-11-11 | 2017-03-15 | Boehringer Ingelheim International GmbH | Combination treatment of cancer comprising egfr/her2 inhibitors |
| PL2171090T3 (pl) * | 2007-06-08 | 2013-09-30 | Genentech Inc | Markery ekspresji genów odporności guza na leczenie hamujące HER2 |
| CA3031835C (en) * | 2008-06-27 | 2021-09-07 | 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 |
| KR101705158B1 (ko) * | 2009-05-05 | 2017-02-09 | 다나-파버 캔서 인스티튜트 인크. | Ｅｇｆｒ 억제제 및 질환 치료방법 |
| WO2011082266A2 (en) * | 2009-12-30 | 2011-07-07 | Arqule, Inc. | Substituted heterocyclic compounds |
| CN105198862B (zh) * | 2011-07-27 | 2018-01-23 | 阿斯利康(瑞典)有限公司 | 取代的n‑(4‑氟‑2‑甲氧基‑5‑硝基苯基)嘧啶‑2‑胺化合物及其盐 |
-
2015
- 2015-05-13 EP EP15792086.9A patent/EP3143015B1/en active Active
- 2015-05-13 US US15/310,349 patent/US20170166598A1/en not_active Abandoned
- 2015-05-13 CN CN201580037958.0A patent/CN106687457B/zh not_active Expired - Fee Related
- 2015-05-13 JP JP2016567502A patent/JP6468611B2/ja not_active Expired - Fee Related
- 2015-05-13 WO PCT/US2015/030522 patent/WO2015175632A1/en not_active Ceased
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