JPWO2022014639A5 - - Google Patents
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- Publication number
- JPWO2022014639A5 JPWO2022014639A5 JP2022536419A JP2022536419A JPWO2022014639A5 JP WO2022014639 A5 JPWO2022014639 A5 JP WO2022014639A5 JP 2022536419 A JP2022536419 A JP 2022536419A JP 2022536419 A JP2022536419 A JP 2022536419A JP WO2022014639 A5 JPWO2022014639 A5 JP WO2022014639A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl group
- hydrogen atom
- group optionally
- general formula
- substituent
- 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
- 125000001424 substituent group Chemical group 0.000 claims description 98
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims description 71
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims description 71
- 125000001153 fluoro group Chemical group F* 0.000 claims description 50
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 claims description 48
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 claims description 33
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 claims description 33
- 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 description 33
- 239000003814 drug Substances 0.000 claims description 31
- 229940124597 therapeutic agent Drugs 0.000 claims description 31
- -1 pyrimidine compound Chemical class 0.000 claims description 30
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 27
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims description 25
- 125000001309 chloro group Chemical group Cl* 0.000 claims description 25
- 150000001875 compounds Chemical class 0.000 claims description 25
- 229910052731 fluorine Inorganic materials 0.000 claims description 24
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims description 23
- 125000006645 (C3-C4) cycloalkyl group Chemical group 0.000 claims description 23
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims description 23
- 239000011737 fluorine Substances 0.000 claims description 23
- 125000005843 halogen group Chemical group 0.000 claims description 23
- 150000003839 salts Chemical class 0.000 claims description 22
- KJWHUTTYFUQYBW-WAOWUJCRSA-N 4-amino-6-(2-cyclopropylethynyl)-7-[(3R,5S)-5-methyl-1-prop-2-enoylpyrrolidin-3-yl]-N-[(1R)-1-phenylethyl]pyrrolo[2,3-d]pyrimidine-5-carboxamide Chemical compound C(C=C)(=O)N1C[C@@H](C[C@@H]1C)N1C(=C(C2=C1N=CN=C2N)C(=O)N[C@H](C)C1=CC=CC=C1)C#CC1CC1 KJWHUTTYFUQYBW-WAOWUJCRSA-N 0.000 claims description 18
- 201000010099 disease Diseases 0.000 claims description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 206010028980 Neoplasm Diseases 0.000 claims description 10
- 239000004480 active ingredient Substances 0.000 claims description 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 6
- 230000004544 DNA amplification Effects 0.000 claims description 4
- 101150039808 Egfr gene Proteins 0.000 claims description 4
- 201000011510 cancer Diseases 0.000 claims description 4
- 108700021358 erbB-1 Genes Proteins 0.000 claims description 4
- 230000035772 mutation Effects 0.000 claims description 4
- 230000002018 overexpression Effects 0.000 claims description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 4
- 229940121647 egfr inhibitor Drugs 0.000 claims description 3
- UDTMKUKLYSHHHD-QKNQBKEWSA-N 4-amino-6-(3,3-dimethylbut-1-ynyl)-7-[(3R,5S)-5-methyl-1-prop-2-enoylpyrrolidin-3-yl]-N-[(1R)-1-phenylethyl]pyrrolo[2,3-d]pyrimidine-5-carboxamide Chemical compound C(C=C)(=O)N1C[C@@H](C[C@@H]1C)N1C(=C(C2=C1N=CN=C2N)C(=O)N[C@H](C)C1=CC=CC=C1)C#CC(C)(C)C UDTMKUKLYSHHHD-QKNQBKEWSA-N 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 2
- 239000003937 drug carrier Substances 0.000 claims description 2
- 125000005745 ethoxymethyl group Chemical group [H]C([H])([H])C([H])([H])OC([H])([H])* 0.000 claims description 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 2
- 125000004184 methoxymethyl group Chemical group [H]C([H])([H])OC([H])([H])* 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- ZJRNPKQLORKDSN-YQVWRLOYSA-N 4-amino-7-[(3R,5S)-5-methyl-1-prop-2-enoylpyrrolidin-3-yl]-N-[(1R)-1-phenylethyl]-6-prop-1-ynylpyrrolo[2,3-d]pyrimidine-5-carboxamide Chemical compound C(C=C)(=O)N1C[C@@H](C[C@@H]1C)N1C(=C(C2=C1N=CN=C2N)C(=O)N[C@H](C)C1=CC=CC=C1)C#CC ZJRNPKQLORKDSN-YQVWRLOYSA-N 0.000 claims 2
- 238000000034 method Methods 0.000 description 4
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 230000002401 inhibitory effect Effects 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2020121525 | 2020-07-15 | ||
| JP2020121525 | 2020-07-15 | ||
| PCT/JP2021/026461 WO2022014639A1 (ja) | 2020-07-15 | 2021-07-14 | Ｅｇｆｒ阻害剤 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JPWO2022014639A1 JPWO2022014639A1 (enExample) | 2022-01-20 |
| JPWO2022014639A5 true JPWO2022014639A5 (enExample) | 2023-03-27 |
| JP7495983B2 JP7495983B2 (ja) | 2024-06-05 |
Family
ID=79554696
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022536419A Active JP7495983B2 (ja) | 2020-07-15 | 2021-07-14 | Ｅｇｆｒ阻害剤 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20230285397A1 (enExample) |
| EP (1) | EP4197538A4 (enExample) |
| JP (1) | JP7495983B2 (enExample) |
| KR (1) | KR102873219B1 (enExample) |
| CN (1) | CN116368136B (enExample) |
| AU (1) | AU2021309779B2 (enExample) |
| BR (1) | BR112023000770A2 (enExample) |
| CA (1) | CA3189460A1 (enExample) |
| MX (1) | MX2023000693A (enExample) |
| PH (1) | PH12023550119A1 (enExample) |
| TW (1) | TW202216152A (enExample) |
| WO (1) | WO2022014639A1 (enExample) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2022014638A1 (ja) * | 2020-07-15 | 2022-01-20 | 大鵬薬品工業株式会社 | ピリミジン化合物の結晶 |
| AU2021308045B2 (en) * | 2020-07-15 | 2024-06-20 | Taiho Pharmaceutical Co., Ltd. | Pyrimidine compound-containing combination to be used in tumor treatment |
| EP4351737A4 (en) * | 2021-05-24 | 2025-05-14 | Taiho Pharmaceutical Co., Ltd. | Treatment methods for subjects with cancer having an aberration in egfr and/or her2 |
| KR20250164828A (ko) | 2023-03-30 | 2025-11-25 | 레볼루션 메디슨즈, 인크. | Ras gtp 가수분해 유도를 위한 조성물 및 이의 용도 |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2025034702A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Rmc-6291 for use in the treatment of ras protein-related disease or disorder |
| WO2025080946A2 (en) | 2023-10-12 | 2025-04-17 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8426428B2 (en) * | 2008-12-05 | 2013-04-23 | Principia Biopharma, Inc. | EGFR kinase knockdown via electrophilically enhanced inhibitors |
| US9034885B2 (en) * | 2012-01-13 | 2015-05-19 | Acea Biosciences Inc. | EGFR modulators and uses thereof |
| TW201336847A (zh) * | 2012-02-07 | 2013-09-16 | Taiho Pharmaceutical Co Ltd | 喹啉基吡咯并嘧啶化合物或其鹽 |
| DK3345907T3 (da) * | 2015-09-01 | 2020-06-22 | Taiho Pharmaceutical Co Ltd | Pyrazolo[3,4-d]pyrimidinforbindelser eller salte deraf |
| MD3269370T2 (ro) * | 2016-02-23 | 2020-05-31 | Taiho Pharmaceutical Co Ltd | Compus pirimidinic condensat nou sau sare a acestuia |
| MA54702A (fr) * | 2019-01-11 | 2021-11-17 | Taiho Pharmaceutical Co Ltd | Composé pyrimidine ou sel correspondant |
-
2021
- 2021-07-14 CA CA3189460A patent/CA3189460A1/en active Pending
- 2021-07-14 TW TW110125853A patent/TW202216152A/zh unknown
- 2021-07-14 PH PH1/2023/550119A patent/PH12023550119A1/en unknown
- 2021-07-14 WO PCT/JP2021/026461 patent/WO2022014639A1/ja not_active Ceased
- 2021-07-14 EP EP21842292.1A patent/EP4197538A4/en active Pending
- 2021-07-14 CN CN202180061165.8A patent/CN116368136B/zh active Active
- 2021-07-14 MX MX2023000693A patent/MX2023000693A/es unknown
- 2021-07-14 BR BR112023000770A patent/BR112023000770A2/pt unknown
- 2021-07-14 US US18/016,103 patent/US20230285397A1/en active Pending
- 2021-07-14 KR KR1020237001973A patent/KR102873219B1/ko active Active
- 2021-07-14 AU AU2021309779A patent/AU2021309779B2/en active Active
- 2021-07-14 JP JP2022536419A patent/JP7495983B2/ja active Active
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