JPWO2019164945A5 - - Google Patents
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- Publication number
- JPWO2019164945A5 JPWO2019164945A5 JP2020566546A JP2020566546A JPWO2019164945A5 JP WO2019164945 A5 JPWO2019164945 A5 JP WO2019164945A5 JP 2020566546 A JP2020566546 A JP 2020566546A JP 2020566546 A JP2020566546 A JP 2020566546A JP WO2019164945 A5 JPWO2019164945 A5 JP WO2019164945A5
- Authority
- JP
- Japan
- Prior art keywords
- carbon atoms
- alkyl
- pharmaceutical preparation
- combination pharmaceutical
- egfr inhibitor
- 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.)
- Pending
Links
- 125000004432 carbon atom Chemical group C* 0.000 claims 48
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 239000000825 pharmaceutical preparation Substances 0.000 claims 21
- 229940121647 egfr inhibitor Drugs 0.000 claims 20
- -1 4,5,6,7-tetrahydropyrazolo [1,5-a] pyridin-3-yl Chemical group 0.000 claims 19
- 125000005842 heteroatom Chemical group 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 13
- 229910052717 sulfur Inorganic materials 0.000 claims 12
- 230000003281 allosteric effect Effects 0.000 claims 10
- 125000003118 aryl group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 125000000623 heterocyclic group Chemical group 0.000 claims 10
- 125000001072 heteroaryl group Chemical group 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000012453 solvate Substances 0.000 claims 8
- 125000003545 alkoxy group Chemical group 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 7
- 125000004438 haloalkoxy group Chemical group 0.000 claims 7
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 6
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 6
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims 6
- 239000003795 chemical substances by application Substances 0.000 claims 4
- 238000000034 method Methods 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 150000001875 compounds Chemical class 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229940126062 Compound A Drugs 0.000 claims 2
- NLDMNSXOCDLTTB-UHFFFAOYSA-N Heterophylliin A Natural products O1C2COC(=O)C3=CC(O)=C(O)C(O)=C3C3=C(O)C(O)=C(O)C=C3C(=O)OC2C(OC(=O)C=2C=C(O)C(O)=C(O)C=2)C(O)C1OC(=O)C1=CC(O)=C(O)C(O)=C1 NLDMNSXOCDLTTB-UHFFFAOYSA-N 0.000 claims 2
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 claims 2
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 239000000539 dimer Substances 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- ZTQSADJAYQOCDD-UHFFFAOYSA-N ginsenoside-Rd2 Natural products C1CC(C2(CCC3C(C)(C)C(OC4C(C(O)C(O)C(CO)O4)O)CCC3(C)C2CC2O)C)(C)C2C1C(C)(CCC=C(C)C)OC(C(C(O)C1O)O)OC1COC1OCC(O)C(O)C1O ZTQSADJAYQOCDD-UHFFFAOYSA-N 0.000 claims 2
- 229910052739 hydrogen Inorganic materials 0.000 claims 2
- 230000005764 inhibitory process Effects 0.000 claims 2
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 102000001253 Protein Kinase Human genes 0.000 claims 1
- 229910052799 carbon Inorganic materials 0.000 claims 1
- 230000002860 competitive effect Effects 0.000 claims 1
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 1
- 238000006471 dimerization reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 1
- 230000002401 inhibitory effect Effects 0.000 claims 1
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 108060006633 protein kinase Proteins 0.000 claims 1
- 238000002626 targeted therapy Methods 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical group C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862632798P | 2018-02-20 | 2018-02-20 | |
| US62/632,798 | 2018-02-20 | ||
| PCT/US2019/018770 WO2019164945A1 (en) | 2018-02-20 | 2019-02-20 | Pharmaceutical combinations of egfr inhibitors and methods of use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2021514398A JP2021514398A (ja) | 2021-06-10 |
| JP2021514398A5 JP2021514398A5 (https=) | 2022-02-25 |
| JPWO2019164945A5 true JPWO2019164945A5 (https=) | 2022-02-25 |
Family
ID=67686991
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020566546A Pending JP2021514398A (ja) | 2018-02-20 | 2019-02-20 | Ｅｇｆｒ阻害剤の組合せ医薬製剤およびその使用法 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20210077469A1 (https=) |
| EP (1) | EP3755330A4 (https=) |
| JP (1) | JP2021514398A (https=) |
| AU (1) | AU2019225803A1 (https=) |
| CA (1) | CA3088972A1 (https=) |
| WO (1) | WO2019164945A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12377080B2 (en) | 2019-06-21 | 2025-08-05 | Dana-Farber Cancer Institute, Inc. | Allosteric EGFR inhibitors and methods of use thereof |
| JP7561777B2 (ja) * | 2019-06-21 | 2024-10-04 | エフ・ホフマン－ラ・ロシュ・アクチェンゲゼルシャフト | 新規ｅｇｆｒ阻害剤 |
| IL326879A (en) | 2019-11-11 | 2026-04-01 | Dana Farber Cancer Inst Inc | EGFR allosteric inhibitors and methods of using them |
| CN111592535B (zh) * | 2020-06-22 | 2021-07-20 | 通化师范学院 | 一种抗egfr突变的抑制剂eai045的制备方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2049518B1 (en) * | 2006-05-31 | 2011-08-31 | Takeda San Diego, Inc. | Indazole and isoindole derivatives as glucokinase activating agents. |
| WO2012129562A2 (en) * | 2011-03-24 | 2012-09-27 | The Scripps Research Institute | Compounds and methods for inducing chondrogenesis |
| CN103702990B (zh) * | 2011-07-27 | 2015-09-09 | 阿斯利康(瑞典)有限公司 | 2-(2,4,5-取代苯胺)嘧啶衍生物作为egfr调谐子用于治疗癌症 |
| CN105315259B (zh) * | 2014-07-29 | 2018-03-09 | 上海艾力斯医药科技有限公司 | 吡啶胺基嘧啶衍生物、其制备方法及应用 |
| CA2987914C (en) * | 2015-06-30 | 2022-09-13 | Dana-Farber Cancer Institute, Inc. | Inhibitors of egfr and methods of use thereof |
| EP3445357B1 (en) * | 2016-04-22 | 2021-05-26 | Dana-Farber Cancer Institute, Inc. | Bifunctional molecules for degradation of egfr and methods of use |
-
2019
- 2019-02-20 US US16/971,021 patent/US20210077469A1/en not_active Abandoned
- 2019-02-20 EP EP19758033.5A patent/EP3755330A4/en not_active Withdrawn
- 2019-02-20 CA CA3088972A patent/CA3088972A1/en active Pending
- 2019-02-20 WO PCT/US2019/018770 patent/WO2019164945A1/en not_active Ceased
- 2019-02-20 AU AU2019225803A patent/AU2019225803A1/en not_active Abandoned
- 2019-02-20 JP JP2020566546A patent/JP2021514398A/ja active Pending
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