JP2020517600A5 - - Google Patents
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- Publication number
- JP2020517600A5 JP2020517600A5 JP2019556175A JP2019556175A JP2020517600A5 JP 2020517600 A5 JP2020517600 A5 JP 2020517600A5 JP 2019556175 A JP2019556175 A JP 2019556175A JP 2019556175 A JP2019556175 A JP 2019556175A JP 2020517600 A5 JP2020517600 A5 JP 2020517600A5
- Authority
- JP
- Japan
- Prior art keywords
- substituted
- unsubstituted
- heterocycloalkyl
- pharmaceutically acceptable
- acceptable salt
- 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
- 125000001072 heteroaryl group Chemical group 0.000 claims 33
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 33
- 150000001875 compounds Chemical class 0.000 claims 31
- 125000000217 alkyl group Chemical group 0.000 claims 29
- 125000000753 cycloalkyl group Chemical group 0.000 claims 27
- 150000003839 salts Chemical class 0.000 claims 25
- 229910052739 hydrogen Inorganic materials 0.000 claims 23
- 239000001257 hydrogen Substances 0.000 claims 23
- 125000003118 aryl group Chemical group 0.000 claims 20
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 18
- 125000002947 alkylene group Chemical group 0.000 claims 17
- 125000001424 substituent group Chemical group 0.000 claims 16
- 125000004404 heteroalkyl group Chemical group 0.000 claims 14
- 229910052757 nitrogen Inorganic materials 0.000 claims 12
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 12
- 125000002993 cycloalkylene group Chemical group 0.000 claims 10
- 229910052736 halogen Inorganic materials 0.000 claims 10
- 150000002367 halogens Chemical class 0.000 claims 10
- 239000008194 pharmaceutical composition Substances 0.000 claims 9
- 125000000732 arylene group Chemical group 0.000 claims 6
- 125000004474 heteroalkylene group Chemical group 0.000 claims 6
- 125000005549 heteroarylene group Chemical group 0.000 claims 6
- 150000002431 hydrogen Chemical class 0.000 claims 5
- 101710113436 GTPase KRas Proteins 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 208000035475 disorder Diseases 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003785 benzimidazolyl group Chemical group N1=C(NC2=C1C=CC=C2)* 0.000 claims 3
- 125000000499 benzofuranyl group Chemical group O1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000004196 benzothienyl group Chemical group S1C(=CC2=C1C=CC=C2)* 0.000 claims 3
- 125000004541 benzoxazolyl group Chemical group O1C(=NC2=C1C=CC=C2)* 0.000 claims 3
- 125000006588 heterocycloalkylene group Chemical group 0.000 claims 3
- 125000002883 imidazolyl group Chemical group 0.000 claims 3
- 125000003453 indazolyl group Chemical group N1N=C(C2=C1C=CC=C2)* 0.000 claims 3
- 125000003387 indolinyl group Chemical group N1(CCC2=CC=CC=C12)* 0.000 claims 3
- 125000003373 pyrazinyl group Chemical group 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000000168 pyrrolyl group Chemical group 0.000 claims 3
- 125000003831 tetrazolyl group Chemical group 0.000 claims 3
- 125000001425 triazolyl group Chemical group 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000005334 azaindolyl group Chemical group N1N=C(C2=CC=CC=C12)* 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 206010051066 Gastrointestinal stromal tumour Diseases 0.000 claims 1
- 101000584612 Homo sapiens GTPase KRas Proteins 0.000 claims 1
- 208000006286 Legius syndrome Diseases 0.000 claims 1
- 206010024305 Leukaemia monocytic Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000003019 Neurofibromatosis 1 Diseases 0.000 claims 1
- 208000024834 Neurofibromatosis type 1 Diseases 0.000 claims 1
- 206010029748 Noonan syndrome Diseases 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 208000031839 Peripheral nerve sheath tumour malignant Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010041329 Somatostatinoma Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 230000000694 effects Effects 0.000 claims 1
- 201000011243 gastrointestinal stromal tumor Diseases 0.000 claims 1
- 102000053557 human K-Ras4B Human genes 0.000 claims 1
- 108700002490 human K-Ras4B Proteins 0.000 claims 1
- 102000049555 human KRAS Human genes 0.000 claims 1
- 230000000366 juvenile effect Effects 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
- 201000009020 malignant peripheral nerve sheath tumor Diseases 0.000 claims 1
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims 1
- 201000006894 monocytic leukemia Diseases 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 208000029974 neurofibrosarcoma Diseases 0.000 claims 1
- 208000022982 optic pathway glioma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000028591 pheochromocytoma Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 201000009410 rhabdomyosarcoma Diseases 0.000 claims 1
- 208000011580 syndromic disease Diseases 0.000 claims 1
- 0 CC(CC1)CC*1C(C)=O Chemical compound CC(CC1)CC*1C(C)=O 0.000 description 2
- CQASEQRRQRRTLY-UHFFFAOYSA-N C[n]1nc(C(NCc2c[n](CC3[U]C3)nn2)=O)c2c1cccc2 Chemical compound C[n]1nc(C(NCc2c[n](CC3[U]C3)nn2)=O)c2c1cccc2 CQASEQRRQRRTLY-UHFFFAOYSA-N 0.000 description 1
- NTEZNSBVTJXZID-SNVBAGLBSA-N Cc(cc1)ccc1S(c1c[n](C[C@H]2OC2)nn1)(=O)=O Chemical compound Cc(cc1)ccc1S(c1c[n](C[C@H]2OC2)nn1)(=O)=O NTEZNSBVTJXZID-SNVBAGLBSA-N 0.000 description 1
- CUNPROXJYKWQJP-NSHDSACASA-N O=C(c1c[nH]c2c1cccc2)NCc1c[n](C[C@@H]2OC2)nn1 Chemical compound O=C(c1c[nH]c2c1cccc2)NCc1c[n](C[C@@H]2OC2)nn1 CUNPROXJYKWQJP-NSHDSACASA-N 0.000 description 1
- CUNPROXJYKWQJP-LLVKDONJSA-N O=C(c1c[nH]c2ccccc12)NCc1c[n](C[C@H]2OC2)nn1 Chemical compound O=C(c1c[nH]c2ccccc12)NCc1c[n](C[C@H]2OC2)nn1 CUNPROXJYKWQJP-LLVKDONJSA-N 0.000 description 1
- FCQHSKPNEQRLKN-JTQLQIEISA-N O=C(c1n[nH]c2c1cccc2)NCc1c[n](C[C@@H]2OC2)nn1 Chemical compound O=C(c1n[nH]c2c1cccc2)NCc1c[n](C[C@@H]2OC2)nn1 FCQHSKPNEQRLKN-JTQLQIEISA-N 0.000 description 1
- FCQHSKPNEQRLKN-SNVBAGLBSA-N O=C(c1n[nH]c2c1cccc2)NCc1c[n](C[C@H]2OC2)nn1 Chemical compound O=C(c1n[nH]c2c1cccc2)NCc1c[n](C[C@H]2OC2)nn1 FCQHSKPNEQRLKN-SNVBAGLBSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762487756P | 2017-04-20 | 2017-04-20 | |
| US62/487,756 | 2017-04-20 | ||
| PCT/US2018/028593 WO2018195439A2 (en) | 2017-04-20 | 2018-04-20 | K-ras modulators |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020517600A JP2020517600A (ja) | 2020-06-18 |
| JP2020517600A5 true JP2020517600A5 (enExample) | 2021-06-10 |
Family
ID=62117061
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019556175A Pending JP2020517600A (ja) | 2017-04-20 | 2018-04-20 | Ｋ−Ｒａｓモジュレーター |
Country Status (16)
| Country | Link |
|---|---|
| US (1) | US11358940B2 (enExample) |
| EP (1) | EP3612526A2 (enExample) |
| JP (1) | JP2020517600A (enExample) |
| KR (1) | KR20200011426A (enExample) |
| CN (1) | CN110785414A (enExample) |
| AU (1) | AU2018255413A1 (enExample) |
| BR (1) | BR112019021899A2 (enExample) |
| CA (1) | CA3059943A1 (enExample) |
| CL (1) | CL2019002968A1 (enExample) |
| EA (1) | EA201992497A1 (enExample) |
| EC (1) | ECSP19075354A (enExample) |
| MA (1) | MA50014A (enExample) |
| MX (1) | MX2019012532A (enExample) |
| SG (1) | SG11201909570PA (enExample) |
| TW (1) | TW201900638A (enExample) |
| WO (1) | WO2018195439A2 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10857140B2 (en) | 2015-05-06 | 2020-12-08 | The Regents Of The University Of California | K-Ras modulators |
| EP3458445B1 (en) | 2016-05-18 | 2021-02-17 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| ES3008911T3 (en) | 2017-07-11 | 2025-03-25 | Vertex Pharma | Carboxamides as modulators of sodium channels |
| EP3710439B1 (en) | 2017-11-15 | 2023-02-15 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| US10647715B2 (en) | 2017-11-15 | 2020-05-12 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| EP3790551A4 (en) | 2018-05-07 | 2022-03-09 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| EP3849536A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3849538A4 (en) | 2018-09-10 | 2022-06-29 | Mirati Therapeutics, Inc. | Combination therapies |
| ES3004338T3 (en) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Combination therapies |
| WO2020118066A1 (en) | 2018-12-05 | 2020-06-11 | Mirati Therapeutics, Inc. | Combination therapies |
| EP3908283A4 (en) | 2019-01-10 | 2022-10-12 | Mirati Therapeutics, Inc. | KRAS G12C INHIBITORS |
| WO2020146612A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Esters and carbamates as modulators of sodium channels |
| WO2020146682A1 (en) | 2019-01-10 | 2020-07-16 | Vertex Pharmaceuticals Incorporated | Carboxamides as modulators of sodium channels |
| WO2020172324A1 (en) * | 2019-02-19 | 2020-08-27 | The Regents Of The University Of California | Nurr1 receptor modulators |
| JP7622043B2 (ja) | 2019-08-29 | 2025-01-27 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｄ阻害剤 |
| US12122787B2 (en) | 2019-09-20 | 2024-10-22 | Shanghai Jemincare Pharmaceuticals Co., Ltd | Fused pyridone compound, and preparation method therefor and use thereof |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| CN112574174B (zh) * | 2019-09-27 | 2021-12-07 | 恩瑞生物医药科技（上海）有限公司 | 蛋白降解靶向嵌合体类化合物及其制备方法和医药用途 |
| CR20220316A (es) | 2019-12-06 | 2022-10-07 | Vertex Pharma | Tetrahidrofuranos sustituidos como moduladores de canales de sodio |
| IL294048A (en) | 2019-12-20 | 2022-08-01 | Mirati Therapeutics Inc | sos1 inhibitors |
| TW202210633A (zh) | 2020-06-05 | 2022-03-16 | 法商昂席歐公司 | 用於治療癌症之dbait分子與kras抑制劑的組合 |
| TW202214574A (zh) * | 2020-06-08 | 2022-04-16 | 加拿大商愛彼特生物製藥公司 | 經取代之(呔-1-基甲基)脲類、經取代之n-(呔-1-基甲基)醯胺類及其類似物 |
| JP2023530351A (ja) | 2020-06-18 | 2023-07-14 | レヴォリューション・メディスンズ，インコーポレイテッド | Ｒａｓ阻害剤への獲得耐性を遅延させる、防止する、及び、治療する方法 |
| KR20230081726A (ko) | 2020-09-03 | 2023-06-07 | 레볼루션 메디슨즈, 인크. | Shp2 돌연변이가 있는 악성 종양을 치료하기 위한 sos1 억제제의 용도 |
| KR20230137286A (ko) | 2020-09-11 | 2023-10-04 | 미라티 테라퓨틱스, 인크. | Kras g12c 억제제의 결정 형태 |
| EP4262807A4 (en) | 2020-12-15 | 2025-04-23 | Mirati Therapeutics, Inc. | Azachinazoline pan-KRAS inhibitors |
| US11999753B2 (en) | 2020-12-16 | 2024-06-04 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-KRas inhibitors |
| UY39569A (es) | 2020-12-17 | 2022-07-29 | Astrazeneca Ab | N-(2-(4-cianotiazolidin-3-il)-2-oxoetil)- quinolin-4-carboxamidas |
| AU2022215844A1 (en) | 2021-02-02 | 2023-09-14 | Liminal Biosciences Limited | Gpr84 antagonists and uses thereof |
| US20240210412A1 (en) * | 2021-04-13 | 2024-06-27 | University Of Virginia Patent Foundation | Sulfonyl-triazole compounds useful as ligands and inhibitors of prostaglandin reductase 2 |
| JP2024522292A (ja) | 2021-06-04 | 2024-06-13 | バーテックス ファーマシューティカルズ インコーポレイテッド | ナトリウムチャネルのモジュレーターとしてのｎ－（ヒドロキシアルキル（ヘテロ）アリール）テトラヒドロフランカルボキサミド |
| AR127064A1 (es) | 2021-09-15 | 2023-12-13 | Hua Medicine Shanghai Ltd | Prodroga de derivados de pirrolidona como activador de glucoquinasa |
| WO2023060362A1 (en) * | 2021-10-15 | 2023-04-20 | Genetolead Inc. | Ras inhibitors, compositions and methods of use thereof |
| EP4452416A1 (en) * | 2021-12-22 | 2024-10-30 | The Regents Of The University Of California | Covalently binding inhibitors of g12s, g12d and/or g12e mutants of k-ras gtpase |
| CN115028678B (zh) * | 2022-07-08 | 2024-09-06 | 杭州医学院 | 基于vhl配体诱导bcr-abl蛋白降解的双功能分子及其制备方法和应用 |
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-
2018
- 2018-04-20 AU AU2018255413A patent/AU2018255413A1/en not_active Abandoned
- 2018-04-20 MA MA050014A patent/MA50014A/fr unknown
- 2018-04-20 US US16/605,643 patent/US11358940B2/en active Active
- 2018-04-20 MX MX2019012532A patent/MX2019012532A/es unknown
- 2018-04-20 EP EP18723215.2A patent/EP3612526A2/en not_active Withdrawn
- 2018-04-20 CA CA3059943A patent/CA3059943A1/en active Pending
- 2018-04-20 BR BR112019021899-8A patent/BR112019021899A2/pt not_active Application Discontinuation
- 2018-04-20 SG SG11201909570P patent/SG11201909570PA/en unknown
- 2018-04-20 KR KR1020197034310A patent/KR20200011426A/ko not_active Withdrawn
- 2018-04-20 WO PCT/US2018/028593 patent/WO2018195439A2/en not_active Ceased
- 2018-04-20 EA EA201992497A patent/EA201992497A1/ru unknown
- 2018-04-20 JP JP2019556175A patent/JP2020517600A/ja active Pending
- 2018-04-20 CN CN201880037317.9A patent/CN110785414A/zh active Pending
- 2018-04-20 TW TW107113553A patent/TW201900638A/zh unknown
-
2019
- 2019-10-17 CL CL2019002968A patent/CL2019002968A1/es unknown
- 2019-10-18 EC ECSENADI201975354A patent/ECSP19075354A/es unknown
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