JPWO2020236940A5 - - Google Patents
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- Publication number
- JPWO2020236940A5 JPWO2020236940A5 JP2021568865A JP2021568865A JPWO2020236940A5 JP WO2020236940 A5 JPWO2020236940 A5 JP WO2020236940A5 JP 2021568865 A JP2021568865 A JP 2021568865A JP 2021568865 A JP2021568865 A JP 2021568865A JP WO2020236940 A5 JPWO2020236940 A5 JP WO2020236940A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- compound
- acceptable salt
- independently
- heterocyclyl
- 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
- 150000001875 compounds Chemical class 0.000 claims description 157
- 125000005842 heteroatom Chemical group 0.000 claims description 84
- 229910052760 oxygen Inorganic materials 0.000 claims description 80
- 150000003839 salts Chemical class 0.000 claims description 74
- 125000000217 alkyl group Chemical group 0.000 claims description 73
- 229910052739 hydrogen Inorganic materials 0.000 claims description 64
- 229910052799 carbon Inorganic materials 0.000 claims description 60
- 125000000623 heterocyclic group Chemical group 0.000 claims description 58
- 229910052731 fluorine Inorganic materials 0.000 claims description 48
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims description 44
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 43
- 125000001072 heteroaryl group Chemical group 0.000 claims description 37
- 125000003118 aryl group Chemical group 0.000 claims description 35
- 229910052736 halogen Inorganic materials 0.000 claims description 34
- 150000002367 halogens Chemical class 0.000 claims description 34
- 229910052801 chlorine Inorganic materials 0.000 claims description 29
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 24
- RWRDLPDLKQPQOW-UHFFFAOYSA-N Pyrrolidine Chemical compound C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims description 21
- 125000001188 haloalkyl group Chemical group 0.000 claims description 21
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 21
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims description 21
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 21
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 18
- 125000003545 alkoxy group Chemical group 0.000 claims description 15
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 13
- 239000003814 drug Substances 0.000 claims description 4
- 229940079593 drug Drugs 0.000 claims description 4
- 125000000325 methylidene group Chemical group [H]C([H])=* 0.000 claims description 3
- 239000008194 pharmaceutical composition Substances 0.000 claims description 3
- 206010028980 Neoplasm Diseases 0.000 claims description 2
- 201000011510 cancer Diseases 0.000 claims description 2
- 239000003085 diluting agent Substances 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 5
- 125000004429 atom Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 description 51
- 229910052717 sulfur Inorganic materials 0.000 description 17
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 8
- 229920006395 saturated elastomer Polymers 0.000 description 7
- 229910052794 bromium Inorganic materials 0.000 description 6
- 125000004432 carbon atom Chemical group C* 0.000 description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 4
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound 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 description 3
- 125000004438 haloalkoxy group Chemical group 0.000 description 2
- 125000004433 nitrogen atom Chemical group N* 0.000 description 2
- 125000004568 thiomorpholinyl group Chemical group 0.000 description 2
- 125000005940 1,4-dioxanyl group Chemical group 0.000 description 1
- HKDFRDIIELOLTJ-UHFFFAOYSA-N 1,4-dithianyl Chemical group [CH]1CSCCS1 HKDFRDIIELOLTJ-UHFFFAOYSA-N 0.000 description 1
- 229940126639 Compound 33 Drugs 0.000 description 1
- 125000002950 monocyclic group Chemical group 0.000 description 1
- 125000002757 morpholinyl group Chemical group 0.000 description 1
- 125000004193 piperazinyl group Chemical group 0.000 description 1
- 125000003386 piperidinyl group Chemical group 0.000 description 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 description 1
- -1 sulfolanyl Chemical group 0.000 description 1
- 125000003718 tetrahydrofuranyl group Chemical group 0.000 description 1
- 125000001412 tetrahydropyranyl group Chemical group 0.000 description 1
- 125000003507 tetrahydrothiofenyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962850289P | 2019-05-20 | 2019-05-20 | |
| US62/850,289 | 2019-05-20 | ||
| PCT/US2020/033816 WO2020236940A1 (en) | 2019-05-20 | 2020-05-20 | Kras g12c inhibitors and uses thereof |
Publications (4)
| Publication Number | Publication Date |
|---|---|
| JP2022533398A JP2022533398A (ja) | 2022-07-22 |
| JPWO2020236940A5 true JPWO2020236940A5 (https=) | 2023-05-29 |
| JP2022533398A5 JP2022533398A5 (https=) | 2023-05-29 |
| JP7502337B2 JP7502337B2 (ja) | 2024-06-18 |
Family
ID=73458223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021568865A Active JP7502337B2 (ja) | 2019-05-20 | 2020-05-20 | Ｋｒａｓ ｇ１２ｃインヒビター及びその使用 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20220227738A1 (https=) |
| EP (1) | EP3972978A4 (https=) |
| JP (1) | JP7502337B2 (https=) |
| KR (1) | KR20220038289A (https=) |
| CN (1) | CN114096544B (https=) |
| AU (1) | AU2020279253A1 (https=) |
| BR (1) | BR112021023359A2 (https=) |
| CA (1) | CA3141604A1 (https=) |
| IL (1) | IL288200A (https=) |
| MX (1) | MX2021014177A (https=) |
| SG (1) | SG11202112790SA (https=) |
| WO (1) | WO2020236940A1 (https=) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11932633B2 (en) | 2018-05-07 | 2024-03-19 | Mirati Therapeutics, Inc. | KRas G12C inhibitors |
| SMT202500028T1 (it) | 2018-09-10 | 2025-03-12 | Mirati Therapeutics Inc | Terapie combinate |
| CA3112043A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| WO2020055761A1 (en) | 2018-09-10 | 2020-03-19 | Mirati Therapeutics, Inc. | Combination therapies |
| JP2022500385A (ja) | 2018-09-10 | 2022-01-04 | ミラティ セラピューティクス， インコーポレイテッド | 組み合わせ療法 |
| WO2020085504A1 (ja) | 2018-10-26 | 2020-04-30 | 大鵬薬品工業株式会社 | 光照射ザンドマイヤー反応を用いたクロロアゾールカルボキシレート誘導体の製造方法 |
| CN113164418A (zh) | 2018-12-05 | 2021-07-23 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| WO2020146613A1 (en) | 2019-01-10 | 2020-07-16 | Mirati Therapeutics, Inc. | Kras g12c inhibitors |
| WO2021041671A1 (en) | 2019-08-29 | 2021-03-04 | Mirati Therapeutics, Inc. | Kras g12d inhibitors |
| CN114761012B (zh) | 2019-09-24 | 2025-03-21 | 米拉蒂治疗股份有限公司 | 组合疗法 |
| CN114867726B (zh) | 2019-10-28 | 2023-11-28 | 默沙东有限责任公司 | Kras g12c突变体的小分子抑制剂 |
| WO2021093758A1 (zh) * | 2019-11-15 | 2021-05-20 | 四川海思科制药有限公司 | 一种嘧啶并环衍生物及其在医药上的应用 |
| US12479834B2 (en) | 2019-11-29 | 2025-11-25 | Taiho Pharmaceutical Co., Ltd. | Phenol compound or salt thereof |
| PH12022551513A1 (en) | 2019-12-20 | 2023-04-24 | Mirati Therapeutics Inc | Sos1 inhibitors |
| TWI770760B (zh) * | 2020-01-08 | 2022-07-11 | 大陸商蘇州亞盛藥業有限公司 | 螺環四氫喹唑啉 |
| WO2021245055A1 (en) | 2020-06-02 | 2021-12-09 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| WO2022040469A1 (en) * | 2020-08-19 | 2022-02-24 | The Trustees Of The Stevens Institute Of Technology | Spiro compounds as kras inhibitors |
| WO2022056307A1 (en) | 2020-09-11 | 2022-03-17 | Mirati Therapeutics, Inc. | Crystalline forms of a kras g12c inhibitor |
| AU2021347232A1 (en) | 2020-09-23 | 2023-04-27 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| WO2022132200A1 (en) | 2020-12-15 | 2022-06-23 | Mirati Therapeutics, Inc. | Azaquinazoline pan-kras inhibitors |
| EP4262803A4 (en) | 2020-12-16 | 2025-03-12 | Mirati Therapeutics, Inc. | Tetrahydropyridopyrimidine pan-kras inhibitors |
| WO2022133345A1 (en) | 2020-12-18 | 2022-06-23 | Erasca, Inc. | Tricyclic pyridones and pyrimidones |
| CN114685502A (zh) * | 2020-12-25 | 2022-07-01 | 由理生物医药（上海）有限公司 | 作为kras-g12c抑制剂的螺环类化合物 |
| CN114805311B (zh) * | 2021-01-21 | 2024-10-29 | 苏州亚盛药业有限公司 | 螺环茚 |
| WO2022240971A2 (en) * | 2021-05-11 | 2022-11-17 | 1200 Pharma Llc | Kras g12d inhibitors and uses thereof |
| US20240293558A1 (en) | 2021-06-16 | 2024-09-05 | Erasca, Inc. | Kras inhibitor conjugates |
| CA3224341A1 (en) | 2021-09-01 | 2023-03-09 | Novartis Ag | Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of cancers |
| CN119156383A (zh) * | 2021-11-09 | 2024-12-17 | 1200药业有限责任公司 | 选择性kras g12c抑制剂及其用途 |
| JP2024543982A (ja) * | 2021-12-01 | 2024-11-26 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | がんの処置のための縮環２－アミノ－３－シアノチオフェン及び誘導体 |
| WO2023099624A1 (en) | 2021-12-01 | 2023-06-08 | Boehringer Ingelheim International Gmbh | Annulated 2-amino-3-cyano thiophenes and derivatives for the treatment of cancer |
| AU2023218370B2 (en) * | 2022-02-09 | 2024-11-28 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| IL317601A (en) | 2022-05-25 | 2025-02-01 | Quanta Therapeutics Inc | Pyrimidine-based modulators and their uses |
| WO2024112654A1 (en) | 2022-11-21 | 2024-05-30 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2024192424A1 (en) | 2023-03-15 | 2024-09-19 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| AU2024323424A1 (en) | 2023-08-17 | 2026-03-05 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| TW202528315A (zh) | 2023-09-21 | 2025-07-16 | 美商樹線生物科學公司 | 螺環二氫哌喃并吡啶ＫＲａｓ抑制劑 |
| WO2025085748A1 (en) | 2023-10-20 | 2025-04-24 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| WO2025237091A1 (zh) * | 2024-05-17 | 2025-11-20 | 中山优理生物医药有限公司 | 螺环类化合物的制备方法及其中间体 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6011029A (en) * | 1996-02-26 | 2000-01-04 | Bristol-Myers Squibb Company | Inhibitors of farnesyl protein transferase |
| US6875751B2 (en) | 2000-06-15 | 2005-04-05 | Idenix Pharmaceuticals, Inc. | 3′-prodrugs of 2′-deoxy-β-L-nucleosides |
| US7964580B2 (en) | 2007-03-30 | 2011-06-21 | Pharmasset, Inc. | Nucleoside phosphoramidate prodrugs |
| EP2209775A1 (en) * | 2007-10-09 | 2010-07-28 | UCB Pharma, S.A. | Heterobicyclic compounds as histamine h4-receptor antagonists |
| AU2014331794C1 (en) | 2013-10-10 | 2019-09-12 | Araxes Pharma Llc | Inhibitors of KRAS G12C |
| JO3556B1 (ar) * | 2014-09-18 | 2020-07-05 | Araxes Pharma Llc | علاجات مدمجة لمعالجة السرطان |
| JP2018513853A (ja) * | 2015-04-10 | 2018-05-31 | アラクセス ファーマ エルエルシー | 置換キナゾリン化合物およびその使用方法 |
| JP7039489B2 (ja) | 2016-05-18 | 2022-03-22 | ミラティ セラピューティクス， インコーポレイテッド | Ｋｒａｓ ｇ１２ｃ阻害剤 |
| JOP20190186A1 (ar) * | 2017-02-02 | 2019-08-01 | Astellas Pharma Inc | مركب كينازولين |
| US20190134056A1 (en) * | 2017-03-10 | 2019-05-09 | The Trustees Of The Stevens Institute Of Technolog | K-ras mutations and antagonists |
| AU2018271990A1 (en) | 2017-05-25 | 2019-12-12 | Araxes Pharma Llc | Covalent inhibitors of KRAS |
| JP2020521741A (ja) * | 2017-05-25 | 2020-07-27 | アラクセス ファーマ エルエルシー | がんの処置のための化合物およびその使用の方法 |
| JP7514005B2 (ja) * | 2017-06-21 | 2024-07-10 | シャイ・セラピューティクス・エルエルシー | がん、炎症性疾患、ラソパシー、及び線維性疾患の治療のためのｒａｓスーパーファミリーと相互作用する化合物 |
| TW201942116A (zh) * | 2018-02-09 | 2019-11-01 | 美商輝瑞股份有限公司 | 作為抗癌劑之四氫喹唑啉衍生物 |
| ES2938987T3 (es) * | 2018-06-01 | 2023-04-18 | Amgen Inc | Inhibidores de KRAS G12c y métodos de uso de los mismos |
| US20190375749A1 (en) * | 2018-06-11 | 2019-12-12 | Amgen Inc. | Kras g12c inhibitors and methods of using the same |
| WO2020035031A1 (en) * | 2018-08-16 | 2020-02-20 | Genentech, Inc. | Fused ring compounds |
| TWI770760B (zh) * | 2020-01-08 | 2022-07-11 | 大陸商蘇州亞盛藥業有限公司 | 螺環四氫喹唑啉 |
| WO2022040469A1 (en) * | 2020-08-19 | 2022-02-24 | The Trustees Of The Stevens Institute Of Technology | Spiro compounds as kras inhibitors |
-
2020
- 2020-05-20 CN CN202080052231.0A patent/CN114096544B/zh active Active
- 2020-05-20 JP JP2021568865A patent/JP7502337B2/ja active Active
- 2020-05-20 CA CA3141604A patent/CA3141604A1/en active Pending
- 2020-05-20 WO PCT/US2020/033816 patent/WO2020236940A1/en not_active Ceased
- 2020-05-20 AU AU2020279253A patent/AU2020279253A1/en not_active Abandoned
- 2020-05-20 MX MX2021014177A patent/MX2021014177A/es unknown
- 2020-05-20 EP EP20810811.8A patent/EP3972978A4/en active Pending
- 2020-05-20 BR BR112021023359A patent/BR112021023359A2/pt unknown
- 2020-05-20 KR KR1020217041514A patent/KR20220038289A/ko not_active Ceased
- 2020-05-20 SG SG11202112790SA patent/SG11202112790SA/en unknown
- 2020-05-20 US US17/612,972 patent/US20220227738A1/en active Pending
-
2021
- 2021-11-17 IL IL288200A patent/IL288200A/en unknown
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