CN114096544B - Kras g12c抑制剂及其用途 - Google Patents
Kras g12c抑制剂及其用途Info
- Publication number
- CN114096544B CN114096544B CN202080052231.0A CN202080052231A CN114096544B CN 114096544 B CN114096544 B CN 114096544B CN 202080052231 A CN202080052231 A CN 202080052231A CN 114096544 B CN114096544 B CN 114096544B
- Authority
- CN
- China
- Prior art keywords
- mmol
- compound
- mixture
- alkyl
- spiro
- 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.)
- Active
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/527—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
- C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D495/10—Spiro-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/10—Spiro-condensed systems
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962850289P | 2019-05-20 | 2019-05-20 | |
| US62/850289 | 2019-05-20 | ||
| PCT/US2020/033816 WO2020236940A1 (en) | 2019-05-20 | 2020-05-20 | Kras g12c inhibitors and uses thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114096544A CN114096544A (zh) | 2022-02-25 |
| CN114096544B true CN114096544B (zh) | 2025-08-12 |
Family
ID=73458223
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080052231.0A Active CN114096544B (zh) | 2019-05-20 | 2020-05-20 | Kras g12c抑制剂及其用途 |
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 |
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| 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
Also Published As
| Publication number | Publication date |
|---|---|
| EP3972978A1 (en) | 2022-03-30 |
| JP2022533398A (ja) | 2022-07-22 |
| KR20220038289A (ko) | 2022-03-28 |
| JP7502337B2 (ja) | 2024-06-18 |
| BR112021023359A2 (pt) | 2022-02-01 |
| AU2020279253A1 (en) | 2021-12-16 |
| WO2020236940A1 (en) | 2020-11-26 |
| CN114096544A (zh) | 2022-02-25 |
| EP3972978A4 (en) | 2023-04-26 |
| CA3141604A1 (en) | 2020-11-26 |
| MX2021014177A (es) | 2022-04-25 |
| IL288200A (en) | 2022-01-01 |
| US20220227738A1 (en) | 2022-07-21 |
| SG11202112790SA (en) | 2021-12-30 |
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