AU2021260721B2 - [1,3]diazino[5,4-d]pyrimidines as HER2 inhibitors - Google Patents
[1,3]diazino[5,4-d]pyrimidines as HER2 inhibitorsInfo
- Publication number
- AU2021260721B2 AU2021260721B2 AU2021260721A AU2021260721A AU2021260721B2 AU 2021260721 B2 AU2021260721 B2 AU 2021260721B2 AU 2021260721 A AU2021260721 A AU 2021260721A AU 2021260721 A AU2021260721 A AU 2021260721A AU 2021260721 B2 AU2021260721 B2 AU 2021260721B2
- Authority
- AU
- Australia
- Prior art keywords
- cancer
- compound
- her2
- pharmaceutically 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.)
- Active
Links
Classifications
-
- 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
- C07D487/04—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
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/26—Carbohydrates, e.g. sugar alcohols, amino sugars, nucleic acids, mono-, di- or oligo-saccharides; Derivatives thereof, e.g. polysorbates, sorbitan fatty acid esters or glycyrrhizin
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/36—Polysaccharides; Derivatives thereof, e.g. gums, starch, alginate, dextrin, hyaluronic acid, chitosan, inulin, agar or pectin
-
- 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
- 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)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20171221 | 2020-04-24 | ||
| EP20171221.3 | 2020-04-24 | ||
| PCT/EP2021/059015 WO2021213800A1 (en) | 2020-04-24 | 2021-04-07 | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2026220268 Division | 2021-04-07 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| AU2021260721A1 AU2021260721A1 (en) | 2022-09-15 |
| AU2021260721B2 true AU2021260721B2 (en) | 2026-05-28 |
Family
ID=70470818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU2021260721A Active AU2021260721B2 (en) | 2020-04-24 | 2021-04-07 | [1,3]diazino[5,4-d]pyrimidines as HER2 inhibitors |
Country Status (33)
Families Citing this family (51)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2020328598B2 (en) | 2019-08-15 | 2026-07-02 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| US20230126204A1 (en) * | 2020-02-03 | 2023-04-27 | Boehringer Ingelheim International Gmbh | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS |
| US11608343B2 (en) | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| TW202214641A (zh) | 2020-06-30 | 2022-04-16 | 美商艾瑞生藥股份有限公司 | Ｈｅｒ２突變抑制劑 |
| TW202309022A (zh) | 2021-04-13 | 2023-03-01 | 美商努法倫特公司 | 用於治療具egfr突變之癌症之胺基取代雜環 |
| WO2022266458A1 (en) * | 2021-06-17 | 2022-12-22 | Black Diamond Therapeutics, Inc. | 6-heterocycloalkyl-quinazoline derivatives and uses thereof |
| EP4359082A1 (en) | 2021-06-26 | 2024-05-01 | Array BioPharma Inc. | Her2 mutation inhibitors |
| EP4476211A4 (en) * | 2022-02-09 | 2026-02-25 | Enliven Inc | ACYLIC HETEROCYCLIC QUINAZOLINE DERIVATIVES USED AS ERBB2 INHIBITORS |
| US20250206760A1 (en) | 2022-03-28 | 2025-06-26 | Jiangsu Hengrui Pharmaceuticals Co., Ltd. | Nitrogen-containing heterocyclic compound, preparation method therefor, and pharmaceutical application thereof |
| WO2023195773A1 (ko) * | 2022-04-05 | 2023-10-12 | 보로노이 주식회사 | 헤테로아릴 유도체 및 이의 용도 |
| CN117384162A (zh) * | 2022-05-17 | 2024-01-12 | 浙江文达医药科技有限公司 | 选择性her2抑制剂 |
| WO2024027695A1 (zh) * | 2022-08-04 | 2024-02-08 | 微境生物医药科技(上海)有限公司 | 作为her2抑制剂的化合物 |
| CA3263309A1 (en) | 2022-08-22 | 2024-02-29 | Iambic Therapeutics, Inc. | HER2 COMPOUNDS AND MODULATION METHODS |
| AU2023410324A1 (en) | 2022-12-22 | 2025-05-15 | Boehringer Ingelheim International Gmbh | Crystalline forms of a her2 inhibitor |
| EP4637771A1 (en) * | 2022-12-22 | 2025-10-29 | Boehringer Ingelheim International GmbH | Solid dispersion of a her2 inhibitor |
| US20260207606A1 (en) | 2022-12-22 | 2026-07-23 | Boehringer Ingelheim International Gmbh | Dosing schedule of a solid dispersion of a her2 inhibitor |
| WO2024200637A2 (en) | 2023-03-29 | 2024-10-03 | Boehringer Ingelheim International Gmbh | Dosing schedule of a her2 inhibitor |
| CN121487738A (zh) | 2023-03-30 | 2026-02-06 | 锐新医药公司 | 诱导ras gtp水解的组合物和其用途 |
| KR20260019479A (ko) | 2023-05-04 | 2026-02-10 | 레볼루션 메디슨즈, 인크. | Ras 관련 질환 또는 장애를 위한 병용 요법 |
| JP2026520494A (ja) | 2023-05-31 | 2026-06-23 | 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 | がん処置の応答性を予測するためのバイオマーカーとしてのサバイビン |
| CN116903615A (zh) * | 2023-06-21 | 2023-10-20 | 江苏丽源医药有限公司 | 一种妥卡替尼及其中间体的制备方法 |
| CN121568696A (zh) | 2023-07-28 | 2026-02-24 | 勃林格殷格翰国际有限公司 | 制备her2抑制剂的方法 |
| CN121889155A (zh) | 2023-08-07 | 2026-04-17 | 锐新医药公司 | 用于治疗ras蛋白相关疾病或病症的rmc-6291 |
| EP4773966A1 (en) * | 2023-09-06 | 2026-07-15 | Boehringer Ingelheim International GmbH | Cancer treatment with a her2 inhibitor and a cyp3a and/or p-gp modulator |
| AU2024360465A1 (en) | 2023-10-12 | 2026-04-09 | Revolution Medicines, Inc. | Macrocyclic ras inhibitors |
| US20250228858A1 (en) | 2023-12-20 | 2025-07-17 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
| IL330174A (en) | 2023-12-20 | 2026-08-01 | Boehringer Ingelheim Int Gmbh | Combination cancer treatment using zongratinib and KRAS G12C inhibitor |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| TW202606709A (zh) * | 2024-04-03 | 2026-02-16 | 德商百靈佳殷格翰國際股份有限公司 | 抗癌組合療法 |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| US20250375445A1 (en) | 2024-06-07 | 2025-12-11 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025257149A1 (en) | 2024-06-11 | 2025-12-18 | Boehringer Ingelheim International Gmbh | Crystalline forms of zongertinib a her2 tyrosine kinase inhibitor |
| 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 |
| CN121270563A (zh) * | 2024-07-01 | 2026-01-06 | 北京鞍石生物科技股份有限公司 | 稠环化合物及其制备方法和应用 |
| 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 |
| WO2026027757A1 (en) | 2024-08-02 | 2026-02-05 | Boehringer Ingelheim International Gmbh | Treatment of cancer with metastases in the central nervous system |
| 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 |
| WO2026077844A1 (en) | 2024-10-07 | 2026-04-16 | Boehringer Ingelheim International Gmbh | Solid dispersions having stabilized emulsion particles |
| WO2026090116A2 (en) | 2024-10-21 | 2026-04-30 | Revolution Medicines, Inc. | Ras inhibitors |
| US20260108528A1 (en) | 2024-10-22 | 2026-04-23 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2026090245A1 (en) | 2024-10-22 | 2026-04-30 | Revolution Medicines, Inc. | Use of ras inhibitors for treating cancer |
| WO2026106912A1 (en) | 2024-11-12 | 2026-05-21 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026112260A1 (en) | 2024-11-21 | 2026-05-28 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026122764A2 (en) | 2024-12-06 | 2026-06-11 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026128688A2 (en) | 2024-12-13 | 2026-06-18 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2026161839A1 (en) | 2025-01-27 | 2026-07-30 | Revolution Medicines, Inc. | Ras inhibitors |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007059257A2 (en) * | 2005-11-15 | 2007-05-24 | Array Biopharma Inc. | N4-phenyl-quinaz0line-4 -amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases |
| WO2019042409A1 (zh) * | 2017-09-01 | 2019-03-07 | 上海医药集团股份有限公司 | 一种含氮杂环化合物、制备方法、中间体、组合物和应用 |
Family Cites Families (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW414798B (en) * | 1994-09-07 | 2000-12-11 | Thomae Gmbh Dr K | Pyrimido (5,4-d) pyrimidines, medicaments comprising these compounds, their use and processes for their preparation |
| DE19608588A1 (de) | 1996-03-06 | 1997-09-11 | Thomae Gmbh Dr K | Pyrimido [5,4-d]pyrimidine, diese Verbindungen enthaltende Arzneimittel, deren Verwendung und Verfahren zu ihrer Herstellung |
| IL161908A0 (en) | 2001-12-12 | 2005-11-20 | Pfizer Prod Inc | Quinazoline derivatives for the treatment of abnormal cell growth |
| WO2005044302A1 (en) | 2003-11-06 | 2005-05-19 | Pfizer Products Inc. | Selective erbb2 inhibitor/anti-erbb antibody combinations in the treatment of cancer |
| US20070107957A1 (en) * | 2005-11-16 | 2007-05-17 | Lonnie Lehrer | Automobile propulsion system |
| US20170166598A1 (en) | 2014-05-13 | 2017-06-15 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| CA2949793C (en) | 2014-06-19 | 2024-02-27 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| US20210323976A1 (en) | 2015-05-13 | 2021-10-21 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| AU2018325442B2 (en) | 2017-08-31 | 2023-04-13 | Dana-Farber Cancer Institute, Inc. | Inhibitors of EGFR and/or HER2 and methods of use |
| US20230126204A1 (en) | 2020-02-03 | 2023-04-27 | Boehringer Ingelheim International Gmbh | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS |
| CN115052881B (zh) | 2020-02-03 | 2024-07-09 | 勃林格殷格翰国际有限公司 | 作为HER2抑制剂的[1,3]二嗪并[5,4-d]嘧啶 |
| US11608343B2 (en) | 2020-04-24 | 2023-03-21 | Boehringer Ingelheim International Gmbh | Substituted pyrimido[5,4-d]pyrimidines as HER2 inhibitors |
| WO2021231400A1 (en) * | 2020-05-12 | 2021-11-18 | Accutar Biotechnology, Inc. | Bis-aryl ethers containing n-acyl azetidine as egfr/her2 inhibitors |
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2021
- 2021-04-06 US US17/223,132 patent/US11608343B2/en active Active
- 2021-04-07 PT PT217162189T patent/PT4139309T/pt unknown
- 2021-04-07 CN CN202410481750.9A patent/CN118388488A/zh active Pending
- 2021-04-07 LT LTEPPCT/EP2021/059015T patent/LT4139309T/lt unknown
- 2021-04-07 WO PCT/EP2021/059015 patent/WO2021213800A1/en not_active Ceased
- 2021-04-07 TW TW110112486A patent/TWI913256B/zh active
- 2021-04-07 UA UAA202204335A patent/UA130588C2/uk unknown
- 2021-04-07 AR ARP210100910A patent/AR121779A1/es unknown
- 2021-04-07 CN CN202410479057.8A patent/CN118388487A/zh active Pending
- 2021-04-07 FI FIEP21716218.9T patent/FI4139309T3/fi active
- 2021-04-07 CN CN202410475947.1A patent/CN118307543A/zh active Pending
- 2021-04-07 HU HUE21716218A patent/HUE070805T2/hu unknown
- 2021-04-07 MA MA59373A patent/MA59373B1/fr unknown
- 2021-04-07 CN CN202410481753.2A patent/CN118388489A/zh active Pending
- 2021-04-07 HR HRP20250426TT patent/HRP20250426T1/hr unknown
- 2021-04-07 RS RS20250199A patent/RS66557B1/sr unknown
- 2021-04-07 EP EP24221865.9A patent/EP4566611A3/en active Pending
- 2021-04-07 PL PL21716218.9T patent/PL4139309T3/pl unknown
- 2021-04-07 CN CN202180030549.3A patent/CN115485277B/zh active Active
- 2021-04-07 PH PH1/2022/552745A patent/PH12022552745A1/en unknown
- 2021-04-07 CN CN202410490491.6A patent/CN118388490A/zh active Pending
- 2021-04-07 IL IL320477A patent/IL320477A/en unknown
- 2021-04-07 JP JP2022563041A patent/JP7260723B2/ja active Active
- 2021-04-07 AU AU2021260721A patent/AU2021260721B2/en active Active
- 2021-04-07 CN CN202410475949.0A patent/CN118307544A/zh active Pending
- 2021-04-07 DK DK21716218.9T patent/DK4139309T5/da active
- 2021-04-07 EP EP21716218.9A patent/EP4139309B9/en active Active
- 2021-04-07 CN CN202410479058.2A patent/CN118619956A/zh active Pending
- 2021-04-07 KR KR1020227040861A patent/KR102759974B1/ko active Active
- 2021-04-07 CA CA3173602A patent/CA3173602A1/en active Pending
- 2021-04-07 IL IL297490A patent/IL297490B2/en unknown
- 2021-04-07 CN CN202410508211.XA patent/CN118388495A/zh active Pending
- 2021-04-07 CN CN202410490516.2A patent/CN118388491A/zh active Pending
- 2021-04-07 SI SI202130269T patent/SI4139309T1/sl unknown
- 2021-04-07 CN CN202410508210.5A patent/CN118388494A/zh active Pending
- 2021-04-07 CN CN202410494941.9A patent/CN118388492A/zh active Pending
- 2021-04-07 CN CN202410494942.3A patent/CN118388493A/zh active Pending
- 2021-04-07 CR CR20220537A patent/CR20220537A/es unknown
- 2021-04-07 ES ES21716218T patent/ES3013860T3/es active Active
- 2021-04-07 SM SM20250164T patent/SMT202500164T1/it unknown
- 2021-04-07 PE PE2022002443A patent/PE20230827A1/es unknown
- 2021-04-07 MX MX2022013223A patent/MX2022013223A/es unknown
- 2021-04-07 KR KR1020257002191A patent/KR20250016507A/ko active Pending
- 2021-10-28 JO JOJO/P/2022/0271A patent/JOP20220271A1/ar unknown
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2022
- 2022-09-14 DO DO2022000189A patent/DOP2022000189A/es unknown
- 2022-09-21 EC ECSENADI202272777A patent/ECSP22072777A/es unknown
- 2022-09-23 CL CL2022002579A patent/CL2022002579A1/es unknown
- 2022-10-21 CO CONC2022/0015054A patent/CO2022015054A2/es unknown
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2023
- 2023-02-10 US US18/167,168 patent/US20230374021A1/en not_active Abandoned
- 2023-04-06 JP JP2023062141A patent/JP2023085489A/ja active Pending
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2024
- 2024-06-25 US US18/753,429 patent/US20250122204A1/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007059257A2 (en) * | 2005-11-15 | 2007-05-24 | Array Biopharma Inc. | N4-phenyl-quinaz0line-4 -amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases |
| WO2019042409A1 (zh) * | 2017-09-01 | 2019-03-07 | 上海医药集团股份有限公司 | 一种含氮杂环化合物、制备方法、中间体、组合物和应用 |