JPWO2021222278A5 - - Google Patents
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- JPWO2021222278A5 JPWO2021222278A5 JP2022565600A JP2022565600A JPWO2021222278A5 JP WO2021222278 A5 JPWO2021222278 A5 JP WO2021222278A5 JP 2022565600 A JP2022565600 A JP 2022565600A JP 2022565600 A JP2022565600 A JP 2022565600A JP WO2021222278 A5 JPWO2021222278 A5 JP WO2021222278A5
- Authority
- JP
- Japan
- Prior art keywords
- composition
- subject
- mek inhibitor
- kras
- administered
- 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
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- 229940124647 MEK inhibitor Drugs 0.000 claims description 55
- 239000002829 mitogen activated protein kinase inhibitor Substances 0.000 claims description 55
- 238000000034 method Methods 0.000 claims description 45
- 206010028980 Neoplasm Diseases 0.000 claims description 35
- 201000011510 cancer Diseases 0.000 claims description 31
- 230000009977 dual effect Effects 0.000 claims description 26
- 230000035772 mutation Effects 0.000 claims description 20
- 229940124783 FAK inhibitor Drugs 0.000 claims description 16
- 102200006531 rs121913529 Human genes 0.000 claims description 12
- 102200006539 rs121913529 Human genes 0.000 claims description 12
- 239000003795 chemical substances by application Substances 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 8
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims description 6
- ACWZRVQXLIRSDF-UHFFFAOYSA-N binimetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1F ACWZRVQXLIRSDF-UHFFFAOYSA-N 0.000 claims description 4
- 229950008937 defactinib Drugs 0.000 claims description 4
- FWLMVFUGMHIOAA-UHFFFAOYSA-N n-methyl-4-[[4-[[3-[methyl(methylsulfonyl)amino]pyrazin-2-yl]methylamino]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide Chemical group C1=CC(C(=O)NC)=CC=C1NC1=NC=C(C(F)(F)F)C(NCC=2C(=NC=CN=2)N(C)S(C)(=O)=O)=N1 FWLMVFUGMHIOAA-UHFFFAOYSA-N 0.000 claims description 4
- 208000029729 tumor suppressor gene on chromosome 11 Diseases 0.000 claims description 4
- LMMJFBMMJUMSJS-UHFFFAOYSA-N CH5126766 Chemical group CNS(=O)(=O)NC1=NC=CC(CC=2C(OC3=CC(OC=4N=CC=CN=4)=CC=C3C=2C)=O)=C1F LMMJFBMMJUMSJS-UHFFFAOYSA-N 0.000 claims description 3
- 239000003112 inhibitor Substances 0.000 claims description 3
- GFMMXOIFOQCCGU-UHFFFAOYSA-N 2-(2-chloro-4-iodoanilino)-N-(cyclopropylmethoxy)-3,4-difluorobenzamide Chemical compound C=1C=C(I)C=C(Cl)C=1NC1=C(F)C(F)=CC=C1C(=O)NOCC1CC1 GFMMXOIFOQCCGU-UHFFFAOYSA-N 0.000 claims description 2
- RWEVIPRMPFNTLO-UHFFFAOYSA-N 2-(2-fluoro-4-iodoanilino)-N-(2-hydroxyethoxy)-1,5-dimethyl-6-oxo-3-pyridinecarboxamide Chemical compound CN1C(=O)C(C)=CC(C(=O)NOCCO)=C1NC1=CC=C(I)C=C1F RWEVIPRMPFNTLO-UHFFFAOYSA-N 0.000 claims description 2
- IGUBBWJDMLCRIK-UHFFFAOYSA-N 2-[[2-(2-methoxy-4-morpholin-4-ylanilino)-5-(trifluoromethyl)pyridin-4-yl]amino]-n-methylbenzamide Chemical compound CNC(=O)C1=CC=CC=C1NC1=CC(NC=2C(=CC(=CC=2)N2CCOCC2)OC)=NC=C1C(F)(F)F IGUBBWJDMLCRIK-UHFFFAOYSA-N 0.000 claims description 2
- BVAHPPKGOOJSPU-UHFFFAOYSA-N 2-[[5-chloro-2-[(5-methyl-2-propan-2-ylpyrazol-3-yl)amino]pyridin-4-yl]amino]-n-methoxybenzamide Chemical compound CONC(=O)C1=CC=CC=C1NC1=CC(NC=2N(N=C(C)C=2)C(C)C)=NC=C1Cl BVAHPPKGOOJSPU-UHFFFAOYSA-N 0.000 claims description 2
- UYJNQQDJUOUFQJ-UHFFFAOYSA-N 2-[[5-chloro-2-[2-methoxy-4-(4-morpholinyl)anilino]-4-pyrimidinyl]amino]-N-methylbenzamide Chemical compound CNC(=O)C1=CC=CC=C1NC1=NC(NC=2C(=CC(=CC=2)N2CCOCC2)OC)=NC=C1Cl UYJNQQDJUOUFQJ-UHFFFAOYSA-N 0.000 claims description 2
- HLFGQICCFZTXTP-UHFFFAOYSA-N 2-chloro-n-(12-cyanoindolizino[2,3-b]quinoxalin-2-yl)benzamide Chemical compound ClC1=CC=CC=C1C(=O)NC1=CC2=C(C#N)C3=NC4=CC=CC=C4N=C3N2C=C1 HLFGQICCFZTXTP-UHFFFAOYSA-N 0.000 claims description 2
- RCLQNICOARASSR-SECBINFHSA-N 3-[(2r)-2,3-dihydroxypropyl]-6-fluoro-5-(2-fluoro-4-iodoanilino)-8-methylpyrido[2,3-d]pyrimidine-4,7-dione Chemical compound FC=1C(=O)N(C)C=2N=CN(C[C@@H](O)CO)C(=O)C=2C=1NC1=CC=C(I)C=C1F RCLQNICOARASSR-SECBINFHSA-N 0.000 claims description 2
- QUSSZSMDFABHLI-UHFFFAOYSA-N 3-methoxy-n-(1-methylpiperidin-4-yl)-4-[[4-[(3-oxo-1,2-dihydroinden-4-yl)oxy]-5-(trifluoromethyl)pyrimidin-2-yl]amino]benzamide Chemical compound C=1C=C(NC=2N=C(OC=3C=4C(=O)CCC=4C=CC=3)C(=CN=2)C(F)(F)F)C(OC)=CC=1C(=O)NC1CCN(C)CC1 QUSSZSMDFABHLI-UHFFFAOYSA-N 0.000 claims description 2
- 208000010507 Adenocarcinoma of Lung Diseases 0.000 claims description 2
- 206010052747 Adenocarcinoma pancreas Diseases 0.000 claims description 2
- YWPHBSHEGTZPNS-UHFFFAOYSA-N ClC=1C(=NC(=NC=1)NC1=C(C=C(C(=C1)C)C=1CCN(CC=1)C1CCOCC1)OC(C)C)NC1=C(C=CC=C1)S(=O)(=O)C(C)C Chemical compound ClC=1C(=NC(=NC=1)NC1=C(C=C(C(=C1)C)C=1CCN(CC=1)C1CCOCC1)OC(C)C)NC1=C(C=CC=C1)S(=O)(=O)C(C)C YWPHBSHEGTZPNS-UHFFFAOYSA-N 0.000 claims description 2
- 206010052360 Colorectal adenocarcinoma Diseases 0.000 claims description 2
- 208000005431 Endometrioid Carcinoma Diseases 0.000 claims description 2
- RFWVETIZUQEJEF-UHFFFAOYSA-N GDC-0623 Chemical compound OCCONC(=O)C=1C=CC2=CN=CN2C=1NC1=CC=C(I)C=C1F RFWVETIZUQEJEF-UHFFFAOYSA-N 0.000 claims description 2
- VIUAUNHCRHHYNE-JTQLQIEISA-N N-[(2S)-2,3-dihydroxypropyl]-3-(2-fluoro-4-iodoanilino)-4-pyridinecarboxamide Chemical compound OC[C@@H](O)CNC(=O)C1=CC=NC=C1NC1=CC=C(I)C=C1F VIUAUNHCRHHYNE-JTQLQIEISA-N 0.000 claims description 2
- 206010033128 Ovarian cancer Diseases 0.000 claims description 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims description 2
- SUDAHWBOROXANE-SECBINFHSA-N PD 0325901 Chemical compound OC[C@@H](O)CONC(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F SUDAHWBOROXANE-SECBINFHSA-N 0.000 claims description 2
- 208000009956 adenocarcinoma Diseases 0.000 claims description 2
- 229950003054 binimetinib Drugs 0.000 claims description 2
- 229960002271 cobimetinib Drugs 0.000 claims description 2
- RESIMIUSNACMNW-BXRWSSRYSA-N cobimetinib fumarate Chemical compound OC(=O)\C=C\C(O)=O.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F.C1C(O)([C@H]2NCCCC2)CN1C(=O)C1=CC=C(F)C(F)=C1NC1=CC=C(I)C=C1F RESIMIUSNACMNW-BXRWSSRYSA-N 0.000 claims description 2
- 201000003914 endometrial carcinoma Diseases 0.000 claims description 2
- 208000028730 endometrioid adenocarcinoma Diseases 0.000 claims description 2
- 201000005249 lung adenocarcinoma Diseases 0.000 claims description 2
- RDSACQWTXKSHJT-NSHDSACASA-N n-[3,4-difluoro-2-(2-fluoro-4-iodoanilino)-6-methoxyphenyl]-1-[(2s)-2,3-dihydroxypropyl]cyclopropane-1-sulfonamide Chemical compound C1CC1(C[C@H](O)CO)S(=O)(=O)NC=1C(OC)=CC(F)=C(F)C=1NC1=CC=C(I)C=C1F RDSACQWTXKSHJT-NSHDSACASA-N 0.000 claims description 2
- 201000002094 pancreatic adenocarcinoma Diseases 0.000 claims description 2
- RYYNGWLOYLRZLK-RBUKOAKNSA-N pf03814735 Chemical compound C1([C@H]2CC[C@@H](C1=CC=1)N2C(=O)CNC(=O)C)=CC=1NC(N=1)=NC=C(C(F)(F)F)C=1NC1CCC1 RYYNGWLOYLRZLK-RBUKOAKNSA-N 0.000 claims description 2
- 229950002592 pimasertib Drugs 0.000 claims description 2
- 229950008933 refametinib Drugs 0.000 claims description 2
- 229950010746 selumetinib Drugs 0.000 claims description 2
- CYOHGALHFOKKQC-UHFFFAOYSA-N selumetinib Chemical compound OCCONC(=O)C=1C=C2N(C)C=NC2=C(F)C=1NC1=CC=C(Br)C=C1Cl CYOHGALHFOKKQC-UHFFFAOYSA-N 0.000 claims description 2
- 229960004066 trametinib Drugs 0.000 claims description 2
- LIRYPHYGHXZJBZ-UHFFFAOYSA-N trametinib Chemical group CC(=O)NC1=CC=CC(N2C(N(C3CC3)C(=O)C3=C(NC=4C(=CC(I)=CC=4)F)N(C)C(=O)C(C)=C32)=O)=C1 LIRYPHYGHXZJBZ-UHFFFAOYSA-N 0.000 claims description 2
- 102100025093 Zinc fingers and homeoboxes protein 2 Human genes 0.000 claims 26
- 206010069755 K-ras gene mutation Diseases 0.000 claims 2
- 229940126685 KRAS G12R Drugs 0.000 claims 1
- 102200006537 rs121913529 Human genes 0.000 claims 1
- 102200006538 rs121913530 Human genes 0.000 claims 1
- 102200006540 rs121913530 Human genes 0.000 claims 1
- 102200006541 rs121913530 Human genes 0.000 claims 1
- ULMMVBPTWVRPSI-UHFFFAOYSA-N 2-fluoro-5-methoxy-4-[[4-[(2-methyl-3-oxo-1h-isoindol-4-yl)oxy]-5-(trifluoromethyl)pyrimidin-2-yl]amino]-n-(1-methylpiperidin-4-yl)benzamide Chemical compound FC=1C=C(NC=2N=C(OC=3C=4C(=O)N(C)CC=4C=CC=3)C(=CN=2)C(F)(F)F)C(OC)=CC=1C(=O)NC1CCN(C)CC1 ULMMVBPTWVRPSI-UHFFFAOYSA-N 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202063015883P | 2020-04-27 | 2020-04-27 | |
| US63/015,883 | 2020-04-27 | ||
| PCT/US2021/029435 WO2021222278A1 (en) | 2020-04-27 | 2021-04-27 | Methods of treating abnormal cell growth |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2023523323A JP2023523323A (ja) | 2023-06-02 |
| JPWO2021222278A5 true JPWO2021222278A5 (https=) | 2024-05-10 |
| JP2023523323A5 JP2023523323A5 (https=) | 2024-05-10 |
Family
ID=78332185
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022565600A Pending JP2023523323A (ja) | 2020-04-27 | 2021-04-27 | 異常な細胞成長を処置する方法 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20230201198A1 (https=) |
| EP (1) | EP4142882A4 (https=) |
| JP (1) | JP2023523323A (https=) |
| KR (1) | KR20230011277A (https=) |
| CN (1) | CN115916346A (https=) |
| AU (1) | AU2021263742A1 (https=) |
| BR (1) | BR112022021657A2 (https=) |
| CA (1) | CA3175481A1 (https=) |
| IL (1) | IL297650A (https=) |
| MX (1) | MX2022013430A (https=) |
| WO (1) | WO2021222278A1 (https=) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP7582694B2 (ja) | 2020-01-10 | 2024-11-13 | イミューニヤリング コーポレーション | Ｍｅｋ阻害剤及びその治療的使用 |
| TW202329967A (zh) * | 2022-01-21 | 2023-08-01 | 大陸商應世生物科技（南京）有限公司 | 治療腫瘤的藥物組合及用途 |
| EP4469086A4 (en) * | 2022-01-25 | 2026-01-21 | Verastem Inc | POLYTHERAPY FOR THE TREATMENT OF ABNORMAL CELL GROWTH |
| EP4488272A4 (en) * | 2022-02-28 | 2026-02-25 | Wigen Biomedicine Tech Shanghai Co Ltd | COMPOUND USED AS A FAK INHIBITOR AND ITS USE |
| CN118973580A (zh) * | 2022-04-08 | 2024-11-15 | 米拉蒂治疗股份有限公司 | 包含sos1抑制剂和mek抑制剂的组合疗法 |
| JP2025518795A (ja) * | 2022-06-03 | 2025-06-19 | ベラステム・インコーポレーテッド | 異常な細胞成長を処置するための併用療法 |
| US11873296B2 (en) | 2022-06-07 | 2024-01-16 | Verastem, Inc. | Solid forms of a dual RAF/MEK inhibitor |
| TW202517624A (zh) * | 2023-07-03 | 2025-05-01 | 美商醫療免疫工程公司 | Mek免疫腫瘤抑制劑醫藥組合物 |
| WO2025079712A1 (ja) * | 2023-10-12 | 2025-04-17 | 中外製薬株式会社 | ドライバー変異を有するがん患者における分子標的薬併用療法 |
| WO2025261499A1 (zh) * | 2024-06-20 | 2025-12-26 | 上海科州药物股份有限公司 | 蛋白激酶Mek抑制剂苯并噻唑的颗粒药物组合物 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| IN2012DN01403A (https=) * | 2009-08-24 | 2015-06-05 | Genentech Inc | |
| CA2779843A1 (en) * | 2009-11-13 | 2011-05-19 | Infinity Pharmaceuticals, Inc. | Compositions, kits, and methods for identification, assessment, prevention, and therapy of cancer |
| US20130217710A1 (en) * | 2010-11-05 | 2013-08-22 | Glaxosmithkline Intellectual Property (No.2) Limited | Methods for treating cancer |
| US20130004481A1 (en) * | 2011-01-12 | 2013-01-03 | Boehringer Ingelheim International Gmbh | Anticancer therapy |
| BR112017023821A2 (pt) * | 2015-05-06 | 2018-07-31 | Leidos Biomedical Res Inc | moduladores de k-ras |
| AU2018329925B2 (en) * | 2017-09-08 | 2025-05-29 | F. Hoffmann-La Roche Ag | Diagnostic and therapeutic methods for cancer |
| US11666574B2 (en) * | 2019-11-27 | 2023-06-06 | Turning Point Therapeutics, Inc. | Combination therapy involving diaryl macrocyclic compounds |
-
2021
- 2021-04-27 IL IL297650A patent/IL297650A/en unknown
- 2021-04-27 CN CN202180028579.0A patent/CN115916346A/zh active Pending
- 2021-04-27 MX MX2022013430A patent/MX2022013430A/es unknown
- 2021-04-27 CA CA3175481A patent/CA3175481A1/en active Pending
- 2021-04-27 KR KR1020227037020A patent/KR20230011277A/ko active Pending
- 2021-04-27 JP JP2022565600A patent/JP2023523323A/ja active Pending
- 2021-04-27 AU AU2021263742A patent/AU2021263742A1/en active Pending
- 2021-04-27 US US17/921,509 patent/US20230201198A1/en active Pending
- 2021-04-27 WO PCT/US2021/029435 patent/WO2021222278A1/en not_active Ceased
- 2021-04-27 EP EP21797285.0A patent/EP4142882A4/en active Pending
- 2021-04-27 BR BR112022021657A patent/BR112022021657A2/pt unknown
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