JPWO2022125962A5 - - Google Patents
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- JPWO2022125962A5 JPWO2022125962A5 JP2023560239A JP2023560239A JPWO2022125962A5 JP WO2022125962 A5 JPWO2022125962 A5 JP WO2022125962A5 JP 2023560239 A JP2023560239 A JP 2023560239A JP 2023560239 A JP2023560239 A JP 2023560239A JP WO2022125962 A5 JPWO2022125962 A5 JP WO2022125962A5
- Authority
- JP
- Japan
- Prior art keywords
- egfr
- composition
- cancer
- formula
- pharma
- 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
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims 8
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims 8
- 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 8
- 150000001875 compounds Chemical class 0.000 claims 7
- 150000003839 salts Chemical class 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 229940121647 egfr inhibitor Drugs 0.000 claims 3
- 238000000034 method Methods 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 101150039808 Egfr gene Proteins 0.000 claims 2
- 108700021358 erbB-1 Genes Proteins 0.000 claims 2
- 230000037431 insertion Effects 0.000 claims 2
- 238000003780 insertion Methods 0.000 claims 2
- 201000008129 pancreatic ductal adenocarcinoma Diseases 0.000 claims 2
- NGFFVZQXSRKHBM-FKBYEOEOSA-N 5-[[(1r,1as,6br)-1-[6-(trifluoromethyl)-1h-benzimidazol-2-yl]-1a,6b-dihydro-1h-cyclopropa[b][1]benzofuran-5-yl]oxy]-3,4-dihydro-1h-1,8-naphthyridin-2-one Chemical compound N1C(=O)CCC2=C1N=CC=C2OC(C=C1[C@@H]23)=CC=C1O[C@@H]3[C@H]2C1=NC2=CC=C(C(F)(F)F)C=C2N1 NGFFVZQXSRKHBM-FKBYEOEOSA-N 0.000 claims 1
- 208000031261 Acute myeloid leukaemia Diseases 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 1
- 230000004544 DNA amplification Effects 0.000 claims 1
- 230000003350 DNA copy number gain Effects 0.000 claims 1
- 102000009024 Epidermal Growth Factor Human genes 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 239000005411 L01XE02 - Gefitinib Substances 0.000 claims 1
- 239000005551 L01XE03 - Erlotinib Substances 0.000 claims 1
- 239000002136 L01XE07 - Lapatinib Substances 0.000 claims 1
- 239000002118 L01XE12 - Vandetanib Substances 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 102000043136 MAP kinase family Human genes 0.000 claims 1
- 108091054455 MAP kinase family Proteins 0.000 claims 1
- 208000033776 Myeloid Acute Leukemia Diseases 0.000 claims 1
- 208000037538 Myelomonocytic Juvenile Leukemia Diseases 0.000 claims 1
- RRMJMHOQSALEJJ-UHFFFAOYSA-N N-[5-[[4-[4-[(dimethylamino)methyl]-3-phenylpyrazol-1-yl]pyrimidin-2-yl]amino]-4-methoxy-2-morpholin-4-ylphenyl]prop-2-enamide Chemical compound CN(C)CC=1C(=NN(C=1)C1=NC(=NC=C1)NC=1C(=CC(=C(C=1)NC(C=C)=O)N1CCOCC1)OC)C1=CC=CC=C1 RRMJMHOQSALEJJ-UHFFFAOYSA-N 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 229960001686 afatinib Drugs 0.000 claims 1
- ULXXDDBFHOBEHA-CWDCEQMOSA-N afatinib Chemical compound N1=CN=C2C=C(O[C@@H]3COCC3)C(NC(=O)/C=C/CN(C)C)=CC2=C1NC1=CC=C(F)C(Cl)=C1 ULXXDDBFHOBEHA-CWDCEQMOSA-N 0.000 claims 1
- 229940008421 amivantamab Drugs 0.000 claims 1
- 229960005395 cetuximab Drugs 0.000 claims 1
- 210000000349 chromosome Anatomy 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 229950002205 dacomitinib Drugs 0.000 claims 1
- LVXJQMNHJWSHET-AATRIKPKSA-N dacomitinib Chemical compound C=12C=C(NC(=O)\C=C\CN3CCCCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 LVXJQMNHJWSHET-AATRIKPKSA-N 0.000 claims 1
- 230000037430 deletion Effects 0.000 claims 1
- 238000012217 deletion Methods 0.000 claims 1
- 229960001433 erlotinib Drugs 0.000 claims 1
- AAKJLRGGTJKAMG-UHFFFAOYSA-N erlotinib Chemical compound C=12C=C(OCCOC)C(OCCOC)=CC2=NC=NC=1NC1=CC=CC(C#C)=C1 AAKJLRGGTJKAMG-UHFFFAOYSA-N 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 229960002584 gefitinib Drugs 0.000 claims 1
- XGALLCVXEZPNRQ-UHFFFAOYSA-N gefitinib Chemical compound C=12C=C(OCCCN3CCOCC3)C(OC)=CC2=NC=NC=1NC1=CC=C(F)C(Cl)=C1 XGALLCVXEZPNRQ-UHFFFAOYSA-N 0.000 claims 1
- 201000010536 head and neck cancer Diseases 0.000 claims 1
- 208000014829 head and neck neoplasm Diseases 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 201000005992 juvenile myelomonocytic leukemia Diseases 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 229960004891 lapatinib Drugs 0.000 claims 1
- BCFGMOOMADDAQU-UHFFFAOYSA-N lapatinib Chemical compound O1C(CNCCS(=O)(=O)C)=CC=C1C1=CC=C(N=CN=C2NC=3C=C(Cl)C(OCC=4C=C(F)C=CC=4)=CC=3)C2=C1 BCFGMOOMADDAQU-UHFFFAOYSA-N 0.000 claims 1
- 229950009640 lazertinib Drugs 0.000 claims 1
- 229950009767 lifirafenib Drugs 0.000 claims 1
- 201000007270 liver cancer Diseases 0.000 claims 1
- 208000014018 liver neoplasm 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
- 229940015637 mobocertinib Drugs 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 229950000908 nazartinib Drugs 0.000 claims 1
- IOMMMLWIABWRKL-WUTDNEBXSA-N nazartinib Chemical compound C1N(C(=O)/C=C/CN(C)C)CCCC[C@H]1N1C2=C(Cl)C=CC=C2N=C1NC(=O)C1=CC=NC(C)=C1 IOMMMLWIABWRKL-WUTDNEBXSA-N 0.000 claims 1
- 229960000513 necitumumab Drugs 0.000 claims 1
- 229950008835 neratinib Drugs 0.000 claims 1
- ZNHPZUKZSNBOSQ-BQYQJAHWSA-N neratinib Chemical compound C=12C=C(NC\C=C\CN(C)C)C(OCC)=CC2=NC=C(C#N)C=1NC(C=C1Cl)=CC=C1OCC1=CC=CC=N1 ZNHPZUKZSNBOSQ-BQYQJAHWSA-N 0.000 claims 1
- 229950010203 nimotuzumab Drugs 0.000 claims 1
- 229960003278 osimertinib Drugs 0.000 claims 1
- DUYJMQONPNNFPI-UHFFFAOYSA-N osimertinib Chemical group COC1=CC(N(C)CCN(C)C)=C(NC(=O)C=C)C=C1NC1=NC=CC(C=2C3=CC=CC=C3N(C)C=2)=N1 DUYJMQONPNNFPI-UHFFFAOYSA-N 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 229960001972 panitumumab Drugs 0.000 claims 1
- 230000037361 pathway Effects 0.000 claims 1
- AZSRSNUQCUDCGG-UHFFFAOYSA-N propan-2-yl 2-[4-[2-(dimethylamino)ethyl-methylamino]-2-methoxy-5-(prop-2-enoylamino)anilino]-4-(1-methylindol-3-yl)pyrimidine-5-carboxylate Chemical compound C(C=C)(=O)NC=1C(=CC(=C(C=1)NC1=NC=C(C(=N1)C1=CN(C2=CC=CC=C12)C)C(=O)OC(C)C)OC)N(C)CCN(C)C AZSRSNUQCUDCGG-UHFFFAOYSA-N 0.000 claims 1
- 102200048928 rs121434568 Human genes 0.000 claims 1
- 102200048955 rs121434569 Human genes 0.000 claims 1
- 102200048795 rs121913428 Human genes 0.000 claims 1
- 102200048929 rs121913444 Human genes 0.000 claims 1
- 102220198020 rs139236063 Human genes 0.000 claims 1
- 102220198019 rs149840192 Human genes 0.000 claims 1
- 102220198150 rs149840192 Human genes 0.000 claims 1
- 102200048796 rs28929495 Human genes 0.000 claims 1
- 102200048979 rs28929495 Human genes 0.000 claims 1
- 102200008493 rs28933385 Human genes 0.000 claims 1
- 102220198149 rs769696078 Human genes 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 229960000241 vandetanib Drugs 0.000 claims 1
- UHTHHESEBZOYNR-UHFFFAOYSA-N vandetanib Chemical compound COC1=CC(C(/N=CN2)=N/C=3C(=CC(Br)=CC=3)F)=C2C=C1OCC1CCN(C)CC1 UHTHHESEBZOYNR-UHFFFAOYSA-N 0.000 claims 1
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063124665P | 2020-12-11 | 2020-12-11 | |
| US63/124,665 | 2020-12-11 | ||
| US202163214718P | 2021-06-24 | 2021-06-24 | |
| US63/214,718 | 2021-06-24 | ||
| US202163253012P | 2021-10-06 | 2021-10-06 | |
| US63/253,012 | 2021-10-06 | ||
| US202163277561P | 2021-11-09 | 2021-11-09 | |
| US63/277,561 | 2021-11-09 | ||
| PCT/US2021/062912 WO2022125962A1 (en) | 2020-12-11 | 2021-12-10 | Combination therapies for the treatment of cancer |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023553532A JP2023553532A (ja) | 2023-12-21 |
| JP2023553532A5 JP2023553532A5 (https=) | 2024-12-17 |
| JPWO2022125962A5 true JPWO2022125962A5 (https=) | 2024-12-17 |
Family
ID=81974006
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023560239A Pending JP2023553532A (ja) | 2020-12-11 | 2021-12-10 | 癌の処置のための併用療法 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US20240050441A1 (https=) |
| EP (1) | EP4259147A4 (https=) |
| JP (1) | JP2023553532A (https=) |
| KR (1) | KR20230154793A (https=) |
| AU (1) | AU2021396395A1 (https=) |
| CA (1) | CA3201657A1 (https=) |
| WO (1) | WO2022125962A1 (https=) |
Families Citing this family (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| WO2022125971A1 (en) * | 2020-12-11 | 2022-06-16 | Erasca, Inc. | Combination therapies for the treatment of cancer |
| US20240293422A1 (en) * | 2021-06-24 | 2024-09-05 | Erasca, Inc. | Shp2 and cdk4/6 inhibitors combination therapies for the treatment of cancer |
| WO2023059771A1 (en) * | 2021-10-06 | 2023-04-13 | Erasca, Inc. | Uses of tri-substituted heteroaryl derivatives as src homology-2 phosphatase inhibitors |
| WO2025226830A1 (en) * | 2024-04-23 | 2025-10-30 | Erasca, Inc. | Shp2 and egfr inhibitors for the treatment of chordoma |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| RU2601892C2 (ru) * | 2008-03-06 | 2016-11-10 | Дженентек, Инк. | Комбинированная терапия антагонистами с-мет и egfr |
| US8828391B2 (en) * | 2011-05-17 | 2014-09-09 | Boehringer Ingelheim International Gmbh | Method for EGFR directed combination treatment of non-small cell lung cancer |
| US20150273057A1 (en) * | 2012-10-25 | 2015-10-01 | Glaxosmithkline Llc | Combination |
| US20140308274A1 (en) * | 2013-03-15 | 2014-10-16 | Mirna Therapeutics, Inc. | Combination cancer treatments utilizing synthetic oligonucleotides and egfr-tki inhibitors |
| JP7542538B2 (ja) * | 2018-09-18 | 2024-08-30 | ニカング セラピューティクス, インコーポレイテッド | Srcホモロジー-2ホスファターゼ阻害剤としての縮合三環式環誘導体 |
| KR20210144844A (ko) * | 2019-03-29 | 2021-11-30 | 아스트라제네카 아베 | 비-소세포 폐암의 치료에 사용하기 위한 오시머티닙 |
| EP4076667A1 (en) * | 2019-12-20 | 2022-10-26 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| US20210292330A1 (en) * | 2020-02-28 | 2021-09-23 | Erasca, Inc. | Pyrrolidine-fused heterocycles |
-
2021
- 2021-12-10 JP JP2023560239A patent/JP2023553532A/ja active Pending
- 2021-12-10 CA CA3201657A patent/CA3201657A1/en active Pending
- 2021-12-10 WO PCT/US2021/062912 patent/WO2022125962A1/en not_active Ceased
- 2021-12-10 AU AU2021396395A patent/AU2021396395A1/en not_active Abandoned
- 2021-12-10 US US18/256,089 patent/US20240050441A1/en active Pending
- 2021-12-10 EP EP21904509.3A patent/EP4259147A4/en not_active Withdrawn
- 2021-12-10 KR KR1020237023446A patent/KR20230154793A/ko not_active Abandoned
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