CN113135910A - 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 - Google Patents
嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 Download PDFInfo
- Publication number
- CN113135910A CN113135910A CN202010056202.3A CN202010056202A CN113135910A CN 113135910 A CN113135910 A CN 113135910A CN 202010056202 A CN202010056202 A CN 202010056202A CN 113135910 A CN113135910 A CN 113135910A
- Authority
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- Prior art keywords
- methyl
- alkyl
- optionally substituted
- ring
- cycloalkyl
- Prior art date
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Classifications
-
- 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
-
- 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
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
- A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/02—Antineoplastic agents specific for leukemia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
-
- 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
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Epidemiology (AREA)
- Hematology (AREA)
- Oncology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Priority Applications (10)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010056202.3A CN113135910A (zh) | 2020-01-19 | 2020-01-19 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| AU2021208025A AU2021208025A1 (en) | 2020-01-19 | 2021-01-13 | Pyrimidine-4(3H)-ketone heterocyclic compound, preparation method therefor and use thereof in medicine and pharmacology |
| MX2022008881A MX2022008881A (es) | 2020-01-19 | 2021-01-13 | Compuesto heterociclico de pirimidin-4(3h)-ona, metodo de preparacion del mismo y su uso farmaceutico. |
| PCT/CN2021/071375 WO2021143701A1 (zh) | 2020-01-19 | 2021-01-13 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| KR1020227028172A KR20220130168A (ko) | 2020-01-19 | 2021-01-13 | 피리미딘-4(3h)-케톤 헤테로시클릭 화합물, 그의 제조 방법, 및 의약 및 약리학에서의 그의 용도 |
| US17/793,571 US20230219946A1 (en) | 2020-01-19 | 2021-01-13 | Pyrimidin-4(3h)-one heterocyclic compound, preparation method thereof, and pharmaceutical use thereof |
| CN202180009655.3A CN114981268B (zh) | 2020-01-19 | 2021-01-13 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| JP2022543700A JP7716110B2 (ja) | 2020-01-19 | 2021-01-13 | ピリミジン－４（３ｈ）－オンヘテロ環式化合物、その調製方法、およびその医薬的使用 |
| CA3168452A CA3168452A1 (en) | 2020-01-19 | 2021-01-13 | Pyrimidin-4(3tf)-one heterocyclic compound, preparation method thereof, and pharmaceutical use thereof |
| EP21741216.2A EP4092024A4 (en) | 2020-01-19 | 2021-01-13 | PYRIMIDINE-4(3H)-KETON HETEROCYCLIC COMPOUND, PROCESS FOR PRODUCTION THEREOF AND USE THEREOF IN MEDICINE AND PHARMACOLOGY |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN202010056202.3A CN113135910A (zh) | 2020-01-19 | 2020-01-19 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN113135910A true CN113135910A (zh) | 2021-07-20 |
Family
ID=76808550
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202010056202.3A Pending CN113135910A (zh) | 2020-01-19 | 2020-01-19 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
| CN202180009655.3A Active CN114981268B (zh) | 2020-01-19 | 2021-01-13 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202180009655.3A Active CN114981268B (zh) | 2020-01-19 | 2021-01-13 | 嘧啶-4(3h)-酮类杂环化合物、其制备方法及其在医药学上的应用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US20230219946A1 (https=) |
| EP (1) | EP4092024A4 (https=) |
| JP (1) | JP7716110B2 (https=) |
| KR (1) | KR20220130168A (https=) |
| CN (2) | CN113135910A (https=) |
| AU (1) | AU2021208025A1 (https=) |
| CA (1) | CA3168452A1 (https=) |
| MX (1) | MX2022008881A (https=) |
| WO (1) | WO2021143701A1 (https=) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20250195521A1 (en) | 2020-09-03 | 2025-06-19 | Revolution Medicines, Inc. | Use of sos1 inhibitors to treat malignancies with shp2 mutations |
| CA3194067A1 (en) | 2020-09-15 | 2022-03-24 | Revolution Medicines, Inc. | Ras inhibitors |
| CN116848121A (zh) * | 2020-12-18 | 2023-10-03 | 建新公司 | 制备shp2抑制剂的方法 |
| TW202241907A (zh) * | 2020-12-18 | 2022-11-01 | 美商瑞佛路森醫藥公司 | 製備shp2抑制劑之方法 |
| TW202309052A (zh) | 2021-05-05 | 2023-03-01 | 美商銳新醫藥公司 | Ｒａｓ抑制劑 |
| KR20240017811A (ko) | 2021-05-05 | 2024-02-08 | 레볼루션 메디슨즈, 인크. | 암의 치료를 위한 ras 억제제 |
| JP2024516450A (ja) | 2021-05-05 | 2024-04-15 | レボリューション メディシンズ インコーポレイテッド | 共有結合性ｒａｓ阻害剤及びその使用 |
| AR127308A1 (es) | 2021-10-08 | 2024-01-10 | Revolution Medicines Inc | Inhibidores ras |
| JP2025510572A (ja) | 2022-03-08 | 2025-04-15 | レボリューション メディシンズ インコーポレイテッド | 免疫不応性肺癌を治療するための方法 |
| CN118871443A (zh) * | 2022-03-28 | 2024-10-29 | 建新公司 | 用于制备shp2抑制剂的方法 |
| WO2023240263A1 (en) | 2022-06-10 | 2023-12-14 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| AU2024241633A1 (en) | 2023-03-30 | 2025-11-06 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| CR20250420A (es) | 2023-04-07 | 2025-11-20 | Revolution Medicines Inc | Inhibidores macrocíclicos de ras |
| AR132338A1 (es) | 2023-04-07 | 2025-06-18 | Revolution Medicines Inc | Inhibidores de ras |
| CN121100123A (zh) | 2023-04-14 | 2025-12-09 | 锐新医药公司 | Ras抑制剂的结晶形式 |
| CN121464140A (zh) | 2023-04-14 | 2026-02-03 | 锐新医药公司 | Ras抑制剂的结晶形式、含有其的组合物及其使用方法 |
| 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 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| CN117720550A (zh) * | 2023-12-14 | 2024-03-19 | 深圳市华先医药科技有限公司 | (s)-3-甲基-4-氧代-2-氧杂-8-氮杂螺[4.5]癸烷-8-甲酸叔丁酯合成方法 |
| 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 |
| 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 |
| WO2026015796A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Methods of treating a ras related disease or disorder |
| WO2026015790A1 (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 |
| WO2026015825A1 (en) | 2024-07-12 | 2026-01-15 | Revolution Medicines, Inc. | Use of ras inhibitor for treating pancreatic cancer |
| WO2026050446A1 (en) | 2024-08-29 | 2026-03-05 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026072904A2 (en) | 2024-09-26 | 2026-04-02 | Revolution Medicines, Inc. | Compositions and methods for treating lung cancer |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3517B1 (ar) | 2014-01-17 | 2020-07-05 | Novartis Ag | ان-ازاسبيرو الكان حلقي كبديل مركبات اريل-ان مغايرة وتركيبات لتثبيط نشاط shp2 |
| WO2016203405A1 (en) | 2015-06-19 | 2016-12-22 | Novartis Ag | Compounds and compositions for inhibiting the activity of shp2 |
| MX388576B (es) | 2016-06-07 | 2025-03-20 | Jacobio Pharmaceuticals Co Ltd | Derivados heterociclicos novedosos utiles como inhibidores de shp2. |
| EP4302834A3 (en) | 2016-07-12 | 2024-07-17 | Revolution Medicines, Inc. | 2,5-disubstituted 3-methyl pyrazines and 2,5,6-trisubstituted 3-methyl pyrazines as allosteric shp2 inhibitors |
| WO2018057884A1 (en) | 2016-09-22 | 2018-03-29 | Relay Therapeutics, Inc. | Shp2 phosphatase inhibitors and methods of use thereof |
| CA3048340A1 (en) * | 2017-01-10 | 2018-07-19 | Novartis Ag | Pharmaceutical combination comprising an alk inhibitor and a shp2 inhibitor |
| WO2021043077A1 (zh) * | 2019-09-06 | 2021-03-11 | 四川科伦博泰生物医药股份有限公司 | 一种取代吡嗪化合物、其制备方法和用途 |
-
2020
- 2020-01-19 CN CN202010056202.3A patent/CN113135910A/zh active Pending
-
2021
- 2021-01-13 WO PCT/CN2021/071375 patent/WO2021143701A1/zh not_active Ceased
- 2021-01-13 JP JP2022543700A patent/JP7716110B2/ja active Active
- 2021-01-13 AU AU2021208025A patent/AU2021208025A1/en active Pending
- 2021-01-13 MX MX2022008881A patent/MX2022008881A/es unknown
- 2021-01-13 CA CA3168452A patent/CA3168452A1/en active Pending
- 2021-01-13 CN CN202180009655.3A patent/CN114981268B/zh active Active
- 2021-01-13 US US17/793,571 patent/US20230219946A1/en active Pending
- 2021-01-13 KR KR1020227028172A patent/KR20220130168A/ko active Pending
- 2021-01-13 EP EP21741216.2A patent/EP4092024A4/en active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| CN114981268A (zh) | 2022-08-30 |
| EP4092024A4 (en) | 2024-03-13 |
| AU2021208025A1 (en) | 2022-09-01 |
| US20230219946A1 (en) | 2023-07-13 |
| KR20220130168A (ko) | 2022-09-26 |
| JP2023511337A (ja) | 2023-03-17 |
| EP4092024A1 (en) | 2022-11-23 |
| CA3168452A1 (en) | 2021-07-22 |
| WO2021143701A1 (zh) | 2021-07-22 |
| JP7716110B2 (ja) | 2025-07-31 |
| MX2022008881A (es) | 2022-08-11 |
| CN114981268B (zh) | 2025-01-28 |
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Application publication date: 20210720 |