CN118019746A - 多环稠环衍生物及其用途 - Google Patents
多环稠环衍生物及其用途 Download PDFInfo
- Publication number
- CN118019746A CN118019746A CN202280065503.XA CN202280065503A CN118019746A CN 118019746 A CN118019746 A CN 118019746A CN 202280065503 A CN202280065503 A CN 202280065503A CN 118019746 A CN118019746 A CN 118019746A
- Authority
- CN
- China
- Prior art keywords
- alkyl
- membered
- pharmaceutically acceptable
- acceptable salt
- stereoisomer
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Classifications
-
- 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
- C07D498/12—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 three hetero rings
- C07D498/16—Peri-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
-
- 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
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
- A61K31/554—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one sulfur as ring hetero atoms, e.g. clothiapine, diltiazem
-
- 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
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D207/12—Oxygen or sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D223/04—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with only hydrogen atoms, halogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D223/00—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom
- C07D223/02—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings
- C07D223/06—Heterocyclic compounds containing seven-membered rings having one nitrogen atom as the only ring hetero atom not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
- C07D223/08—Oxygen atoms
- C07D223/10—Oxygen atoms attached in position 2
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
- C07D265/30—1,4-Oxazines; Hydrogenated 1,4-oxazines not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D267/00—Heterocyclic compounds containing rings of more than six members having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D267/02—Seven-membered rings
- C07D267/08—Seven-membered rings having the hetero atoms in positions 1 and 4
- C07D267/10—Seven-membered rings having the hetero atoms in positions 1 and 4 not condensed with other rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- 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
- C07D471/04—Ortho-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
- C07D498/22—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 four or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/22—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains four or more hetero rings
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (9)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2021120863 | 2021-09-27 | ||
| CNPCT/CN2021/120863 | 2021-09-27 | ||
| CN2022081601 | 2022-03-18 | ||
| CNPCT/CN2022/081601 | 2022-03-18 | ||
| CNPCT/CN2022/102280 | 2022-06-29 | ||
| CN2022102280 | 2022-06-29 | ||
| CNPCT/CN2022/120205 | 2022-09-21 | ||
| CN2022120205 | 2022-09-21 | ||
| PCT/CN2022/121202 WO2023046135A1 (en) | 2021-09-27 | 2022-09-26 | Polycyclic fused ring derivatives and use thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN118019746A true CN118019746A (zh) | 2024-05-10 |
Family
ID=85720111
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202280065503.XA Pending CN118019746A (zh) | 2021-09-27 | 2022-09-26 | 多环稠环衍生物及其用途 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20250034166A1 (enExample) |
| EP (1) | EP4408851A4 (enExample) |
| JP (1) | JP2024534610A (enExample) |
| KR (1) | KR20240070619A (enExample) |
| CN (1) | CN118019746A (enExample) |
| WO (1) | WO2023046135A1 (enExample) |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019195609A2 (en) | 2018-04-04 | 2019-10-10 | Arvinas Operations, Inc. | Modulators of proteolysis and associated methods of use |
| UA129778C2 (uk) | 2019-10-28 | 2025-07-30 | Мерк Шарп Енд Доум Елелсі | Низькомолекулярні інгібітори g12c-мутантного kras |
| EP4067343A4 (en) | 2019-11-29 | 2024-01-03 | Taiho Pharmaceutical Co., Ltd. | NEW PHENOLIC COMPOUND OR SALT THEREOF |
| CR20240508A (es) | 2022-05-19 | 2024-12-20 | Genentech Inc | Compuestos aza-tetracíclicos de oxazepina y usos de los mismos |
| AU2023302139A1 (en) * | 2022-07-05 | 2024-12-19 | Pfizer Inc. | Pyrido[4,3-d]pyrimidine compounds |
| CN119790058A (zh) * | 2022-07-09 | 2025-04-08 | 荣山医药股份有限公司 | 用于治疗疾病的稠合环kras抑制剂 |
| IL318647A (en) | 2022-08-05 | 2025-03-01 | Kumquat Biosciences Inc | Heterocyclic compounds and their uses |
| JP2025528126A (ja) * | 2022-08-11 | 2025-08-26 | ベイジン スウィッツアランド ゲゼルシャフト ミット ベシュレンクテル ハフツング | 複素環式化合物、その組成物、及びそれらによる処置方法 |
| WO2024032747A1 (zh) * | 2022-08-12 | 2024-02-15 | 正大天晴药业集团股份有限公司 | 三环类化合物及其医药用途 |
| WO2024041573A1 (en) * | 2022-08-25 | 2024-02-29 | Zai Lab (Shanghai) Co., Ltd. | Fused multi-heterocyclic compounds as kras g12d modulators and uses thereof |
| TW202430179A (zh) | 2022-11-21 | 2024-08-01 | 美商樹線生物科學公司 | 螺環二氫哌喃并嘧啶ＫＲａｓ抑制劑 |
| AU2023388747A1 (en) * | 2022-12-07 | 2025-07-10 | Jacobio Pharmaceuticals Co., Ltd. | Fused cyclic compounds and use thereof |
| US12448399B2 (en) | 2023-01-26 | 2025-10-21 | Arvinas Operations, Inc. | Cereblon-based KRAS degrading PROTACs and uses related thereto |
| WO2024178304A1 (en) * | 2023-02-24 | 2024-08-29 | Alterome Therapeutics, Inc. | Kras modulators |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| PE20252775A1 (es) * | 2023-04-05 | 2025-12-22 | Pfizer | Compuestos de pirido[4,3-d]pirimidina |
| WO2024208305A1 (zh) * | 2023-04-07 | 2024-10-10 | 江苏恒瑞医药股份有限公司 | 稠合四环类化合物、其制备方法及其在医药上的应用 |
| EP4695262A1 (en) * | 2023-04-10 | 2026-02-18 | Pfizer Inc. | Pyrido[4,3-d]pyrimidine compounds |
| AU2024252725A1 (en) * | 2023-04-11 | 2025-11-06 | Gilead Sciences, Inc. | Kras modulating compounds |
| WO2024218686A1 (en) * | 2023-04-20 | 2024-10-24 | Pfizer Inc. | Pyrido[4,3-d]pyrimidine compounds |
| TW202508595A (zh) | 2023-05-04 | 2025-03-01 | 美商銳新醫藥公司 | 用於ｒａｓ相關疾病或病症之組合療法 |
| CN121194980A (zh) * | 2023-05-16 | 2025-12-23 | 和记黄埔医药（上海）有限公司 | 三环类化合物及其用途 |
| EP4735438A2 (en) * | 2023-06-30 | 2026-05-06 | Merck Patent GmbH | Heterobifunctional compounds for the degradation of kras |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025038936A1 (en) | 2023-08-17 | 2025-02-20 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025049619A1 (en) | 2023-08-29 | 2025-03-06 | Quanta Therapeutics, Inc. | Kras modulators and uses thereof |
| US20250109147A1 (en) | 2023-09-08 | 2025-04-03 | Gilead Sciences, Inc. | Kras g12d modulating compounds |
| 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 |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024361909A1 (en) | 2023-10-20 | 2026-03-26 | Merck Sharp & Dohme Llc | Small molecule inhibitors of kras proteins |
| CN117700374A (zh) * | 2023-12-25 | 2024-03-15 | 吉尔多肽生物制药(大连市)有限公司 | 手性高吗啉-3-甲酸的制备方法 |
| WO2025148868A1 (zh) * | 2024-01-08 | 2025-07-17 | 泰励生物科技（上海）有限公司 | 一种抗体偶联药物及其用途 |
| WO2025168072A1 (en) * | 2024-02-08 | 2025-08-14 | Beigene (Suzhou) Co., Ltd. | Heterocyclic compounds, compositions thereof, and methods of treatment therewith |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202547461A (zh) | 2024-05-17 | 2025-12-16 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| WO2025245127A1 (en) | 2024-05-21 | 2025-11-27 | Treeline Biosciences, Inc. | Spirocyclic dihydropyranopyrimidine kras inhibitors |
| WO2025255438A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025265060A1 (en) | 2024-06-21 | 2025-12-26 | Revolution Medicines, Inc. | Therapeutic compositions and methods for managing treatment-related effects |
| WO2026006747A1 (en) | 2024-06-28 | 2026-01-02 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026015790A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015801A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026035945A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a topoisomerase payload |
| WO2026035947A1 (en) | 2024-08-07 | 2026-02-12 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a topoisomerase payload |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026064527A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Kras-targeting covalent-induced drug conjugates comprising a tubulin inhibitor payload |
| WO2026064520A1 (en) | 2024-09-19 | 2026-03-26 | Tesseract Medicines Us, Llc | Covalent-induced drug conjugates targeting kras and comprising a tubulin inhibitor payload |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
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| Publication number | Priority date | Publication date | Assignee | Title |
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| US5962453A (en) * | 1995-08-08 | 1999-10-05 | Nippon Shinyaku Co. Ltd. | Triazine derivative and medicine |
| US20100069346A1 (en) * | 2005-06-23 | 2010-03-18 | Sara Holmqvist | New Azetidine Derivatives as Neurokinin Receptor Antagonists for the Treatment of Gastrointestinal Diseases |
| CN102875556B (zh) * | 2011-07-12 | 2016-03-30 | 天津药明康德新药开发有限公司 | (4s)-1-取代-2,5-二氮杂双环[2,2,1]庚烷衍生物及制备方法 |
| US9181288B2 (en) * | 2014-01-16 | 2015-11-10 | Novira Therapeutics, Inc. | Azepane derivatives and methods of treating hepatitis B infections |
| EP3621968A1 (en) * | 2017-05-11 | 2020-03-18 | Astrazeneca AB | Heteroaryl compounds that inhibit g12c mutant ras proteins |
| TW202012415A (zh) * | 2018-05-08 | 2020-04-01 | 瑞典商阿斯特捷利康公司 | 化學化合物 |
| JP7756069B6 (ja) * | 2019-08-02 | 2025-11-27 | 上海済▲ユウ▼医薬科技股▲フン▼有限公司 | 四環式化合物、その調製と使用の方法 |
| CN112390818B (zh) * | 2019-08-12 | 2023-08-22 | 劲方医药科技(上海)有限公司 | 取代的杂芳环并二氢嘧啶酮衍生物，其制法与医药上的用途 |
| EP4065231A1 (en) * | 2019-11-27 | 2022-10-05 | Revolution Medicines, Inc. | Covalent ras inhibitors and uses thereof |
| CA3210167A1 (en) * | 2021-02-09 | 2022-08-18 | Genentech, Inc. | Tetracyclic oxazepine compounds and uses thereof |
| US20240199644A1 (en) * | 2021-03-07 | 2024-06-20 | Jacobio Pharmaceuticals Co., Ltd. | Fused Ring Derivatives Useful as KRAS G12D Inhibitors |
| CA3211725A1 (en) * | 2021-03-17 | 2022-09-22 | Tao Jiang | Pyrimidine-fused cyclic compound, preparation method therefor and use thereof |
| CN116113632B (zh) * | 2021-03-30 | 2025-08-29 | 浙江海正药业股份有限公司 | 杂环类衍生物、其制备方法及其医药上的用途 |
| EP4361157A4 (en) * | 2021-06-21 | 2024-10-16 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | FUSED TETRACYCLIC COMPOUND, ITS PREPARATION METHOD AND ITS USE IN MEDICINE |
-
2022
- 2022-09-26 US US18/695,384 patent/US20250034166A1/en active Pending
- 2022-09-26 CN CN202280065503.XA patent/CN118019746A/zh active Pending
- 2022-09-26 JP JP2024518761A patent/JP2024534610A/ja active Pending
- 2022-09-26 KR KR1020247013592A patent/KR20240070619A/ko active Pending
- 2022-09-26 EP EP22872179.1A patent/EP4408851A4/en active Pending
- 2022-09-26 WO PCT/CN2022/121202 patent/WO2023046135A1/en not_active Ceased
Also Published As
| Publication number | Publication date |
|---|---|
| JP2024534610A (ja) | 2024-09-20 |
| KR20240070619A (ko) | 2024-05-21 |
| US20250034166A1 (en) | 2025-01-30 |
| EP4408851A4 (en) | 2025-09-17 |
| EP4408851A1 (en) | 2024-08-07 |
| WO2023046135A1 (en) | 2023-03-30 |
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