PE20230827A1 - [1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2 - Google Patents
[1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2Info
- Publication number
- PE20230827A1 PE20230827A1 PE2022002443A PE2022002443A PE20230827A1 PE 20230827 A1 PE20230827 A1 PE 20230827A1 PE 2022002443 A PE2022002443 A PE 2022002443A PE 2022002443 A PE2022002443 A PE 2022002443A PE 20230827 A1 PE20230827 A1 PE 20230827A1
- Authority
- PE
- Peru
- Prior art keywords
- diazino
- pyrimidines
- atom
- her2
- halogen
- Prior art date
Links
- 229940125497 HER2 kinase inhibitor Drugs 0.000 title 1
- 150000003230 pyrimidines Chemical class 0.000 title 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 3
- 101001012157 Homo sapiens Receptor tyrosine-protein kinase erbB-2 Proteins 0.000 abstract 2
- 102100030086 Receptor tyrosine-protein kinase erbB-2 Human genes 0.000 abstract 2
- 229910052799 carbon Inorganic materials 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 229910052736 halogen Inorganic materials 0.000 abstract 2
- 150000002367 halogens Chemical class 0.000 abstract 2
- 125000000623 heterocyclic group Chemical group 0.000 abstract 2
- 125000004433 nitrogen atom Chemical group N* 0.000 abstract 2
- 229940124639 Selective inhibitor Drugs 0.000 abstract 1
- 239000003795 chemical substances by application Substances 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 102000052116 epidermal growth factor receptor activity proteins Human genes 0.000 abstract 1
- 108700015053 epidermal growth factor receptor activity proteins Proteins 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 abstract 1
- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 abstract 1
- 230000000771 oncological effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- JOZPEVMCAKXSEY-UHFFFAOYSA-N pyrimido[5,4-d]pyrimidine Chemical class N1=CN=CC2=NC=NC=C21 JOZPEVMCAKXSEY-UHFFFAOYSA-N 0.000 abstract 1
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)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Molecular Biology (AREA)
- Engineering & Computer Science (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Biochemistry (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 (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP20171221 | 2020-04-24 | ||
| PCT/EP2021/059015 WO2021213800A1 (en) | 2020-04-24 | 2021-04-07 | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20230827A1 true PE20230827A1 (es) | 2023-05-19 |
Family
ID=70470818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022002443A PE20230827A1 (es) | 2020-04-24 | 2021-04-07 | [1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2 |
Country Status (32)
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20220047810A (ko) | 2019-08-15 | 2022-04-19 | 블랙 다이아몬드 테라퓨틱스, 인코포레이티드 | 알키닐 퀴나졸린 화합물 |
| JP7626773B2 (ja) * | 2020-02-03 | 2025-02-04 | 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 | ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン |
| 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 |
| BR112023021111A2 (pt) | 2021-04-13 | 2023-12-19 | Nuvalent Inc | Composto, composição farmacêutica, método de tratamento de câncer, método para inibir seletivamente her2, método de regulação de um nível de her2, método para aumentar um nível de her2, método de diminuição da fosforilação de her2 |
| WO2022266458A1 (en) * | 2021-06-17 | 2022-12-22 | Black Diamond Therapeutics, Inc. | 6-heterocycloalkyl-quinazoline derivatives and uses thereof |
| PE20250118A1 (es) | 2021-06-26 | 2025-01-16 | Array Biopharma Inc | Inhibidores de mutacion de her2 |
| WO2023154124A1 (en) * | 2022-02-09 | 2023-08-17 | Enliven Therapeutics, Inc. | Acylated heterocyclic quinazoline derivatives as inhibitors of erbb2 |
| CN118715216A (zh) | 2022-03-28 | 2024-09-27 | 江苏恒瑞医药股份有限公司 | 含氮杂环类化合物、其制备方法及其在医药上的应用 |
| JP2025510926A (ja) * | 2022-04-05 | 2025-04-15 | ボロノイ インコーポレイテッド | ヘテロアリール誘導体およびその使用 |
| 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 |
| US20240132521A1 (en) | 2022-08-22 | 2024-04-25 | Iambic Therapeutics, Inc. | Compounds and methods for modulating her2 |
| AU2023410324A1 (en) | 2022-12-22 | 2025-05-15 | Boehringer Ingelheim International Gmbh | Crystalline forms of a her2 inhibitor |
| WO2024133289A1 (en) | 2022-12-22 | 2024-06-27 | Boehringer Ingelheim International Gmbh | Solid dispersion of a her2 inhibitor |
| CN120456906A (zh) | 2022-12-22 | 2025-08-08 | 勃林格殷格翰国际有限公司 | Her2抑制剂的固体分散体的给药安排方案 |
| WO2024200637A2 (en) | 2023-03-29 | 2024-10-03 | Boehringer Ingelheim International Gmbh | Dosing schedule of a her2 inhibitor |
| TW202504611A (zh) | 2023-03-30 | 2025-02-01 | 美商銳新醫藥公司 | 用於誘導ｒａｓ ｇｔｐ水解之組合物及其用途 |
| WO2024229406A1 (en) | 2023-05-04 | 2024-11-07 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| TW202510886A (zh) | 2023-05-31 | 2025-03-16 | 德商百靈佳殷格翰國際股份有限公司 | 作為用於預測癌症治療反應性之生物標記之存活素 |
| 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 |
| TW202521538A (zh) | 2023-07-28 | 2025-06-01 | 德商百靈佳殷格翰國際股份有限公司 | 製備her2抑制劑之方法 |
| US20250049810A1 (en) | 2023-08-07 | 2025-02-13 | Revolution Medicines, Inc. | Methods of treating a ras protein-related disease or disorder |
| WO2025051693A1 (en) * | 2023-09-06 | 2025-03-13 | Boehringer Ingelheim International Gmbh | Cancer treatment with a her2 inhibitor and a cyp3a and/or p-gp modulator |
| US20250154171A1 (en) | 2023-10-12 | 2025-05-15 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025132549A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Cancer combination therapy using zongertinib and a kras g12c inhibitor |
| WO2025132522A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
| WO2025171296A1 (en) | 2024-02-09 | 2025-08-14 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025210042A1 (en) * | 2024-04-03 | 2025-10-09 | Boehringer Ingelheim International Gmbh | Combination of zongertinib with a sos1 inhibitor for use in the treatment of cancer |
| WO2025240847A1 (en) | 2024-05-17 | 2025-11-20 | Revolution Medicines, Inc. | Ras inhibitors |
| WO2025255438A1 (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 |
Family Cites Families (15)
| 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 |
| AU2002339687A1 (en) | 2001-12-12 | 2003-06-23 | Pfizer Products Inc. | Quinazoline derivatives for the treatement of abnormal cell growth |
| JP2007510708A (ja) | 2003-11-06 | 2007-04-26 | ファイザー・プロダクツ・インク | 癌の治療における選択的ｅｒｂＢ２阻害剤／抗ｅｒｂＢ抗体の組合せ |
| DE602006009968D1 (de) | 2005-11-15 | 2009-12-03 | Array Biopharma Inc | N4-phenyl-chinazolin-4-aminderivate und verwandte verbindungen als inhibitoren der erbb-typ-i-rezeptortyrosinkinase zur behandlung hyperproliferativer krankheiten |
| US20070107957A1 (en) * | 2005-11-16 | 2007-05-17 | Lonnie Lehrer | Automobile propulsion system |
| JP6468611B2 (ja) | 2014-05-13 | 2019-02-13 | アリアド ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| AP2017009690A0 (en) | 2014-06-19 | 2017-01-31 | Ariad Pharma Inc | Heteroaryl compounds for kinase inhibition |
| JP6863901B2 (ja) | 2015-05-13 | 2021-04-28 | アリアド ファーマシューティカルズ， インコーポレイテッド | キナーゼ阻害のためのヘテロアリール化合物 |
| CN115322193A (zh) | 2017-08-31 | 2022-11-11 | 达纳-法伯癌症研究所股份有限公司 | Egfr和/或her2抑制剂和使用方法 |
| JP7333313B2 (ja) | 2017-09-01 | 2023-08-24 | シャンハイ ファーマシューティカルズ ホールディング カンパニー，リミティド | 窒素含有複素環化合物、製造方法、中間体、組成物および使用 |
| JP7626773B2 (ja) | 2020-02-03 | 2025-02-04 | 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 | ＨＥＲ２阻害薬としての［１，３］ジアジノ［５，４－ｄ］ピリミジン |
| EP4100412A1 (en) | 2020-02-03 | 2022-12-14 | 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 |
| 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 SI SI202130269T patent/SI4139309T1/sl unknown
- 2021-04-07 AU AU2021260721A patent/AU2021260721A1/en active Pending
- 2021-04-07 IL IL297490A patent/IL297490B2/en unknown
- 2021-04-07 PE PE2022002443A patent/PE20230827A1/es unknown
- 2021-04-07 IL IL320477A patent/IL320477A/en unknown
- 2021-04-07 SM SM20250164T patent/SMT202500164T1/it unknown
- 2021-04-07 MA MA59373A patent/MA59373B1/fr unknown
- 2021-04-07 BR BR112022021514A patent/BR112022021514A2/pt unknown
- 2021-04-07 DK DK21716218.9T patent/DK4139309T5/da active
- 2021-04-07 HU HUE21716218A patent/HUE070805T2/hu unknown
- 2021-04-07 CA CA3173602A patent/CA3173602A1/en active Pending
- 2021-04-07 KR KR1020257002191A patent/KR20250016507A/ko active Pending
- 2021-04-07 WO PCT/EP2021/059015 patent/WO2021213800A1/en not_active Ceased
- 2021-04-07 CN CN202410479057.8A patent/CN118388487A/zh active Pending
- 2021-04-07 ES ES21716218T patent/ES3013860T3/es active Active
- 2021-04-07 KR KR1020227040861A patent/KR102759974B1/ko active Active
- 2021-04-07 AR ARP210100910A patent/AR121779A1/es unknown
- 2021-04-07 LT LTEPPCT/EP2021/059015T patent/LT4139309T/lt unknown
- 2021-04-07 EP EP24221865.9A patent/EP4566611A3/en active Pending
- 2021-04-07 CN CN202410481753.2A patent/CN118388489A/zh active Pending
- 2021-04-07 FI FIEP21716218.9T patent/FI4139309T3/fi active
- 2021-04-07 JP JP2022563041A patent/JP7260723B2/ja active Active
- 2021-04-07 CN CN202410508210.5A patent/CN118388494A/zh 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 TW TW110112486A patent/TW202206432A/zh unknown
- 2021-04-07 PT PT217162189T patent/PT4139309T/pt unknown
- 2021-04-07 CN CN202410479058.2A patent/CN118619956A/zh active Pending
- 2021-04-07 RS RS20250199A patent/RS66557B1/sr unknown
- 2021-04-07 CN CN202410481750.9A patent/CN118388488A/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 HR HRP20250426TT patent/HRP20250426T1/hr unknown
- 2021-04-07 EP EP21716218.9A patent/EP4139309B9/en active Active
- 2021-04-07 CN CN202410508211.XA patent/CN118388495A/zh active Pending
- 2021-04-07 CN CN202410475947.1A patent/CN118307543A/zh active Pending
- 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 CN CN202410490516.2A patent/CN118388491A/zh active Pending
- 2021-04-07 MX MX2022013223A patent/MX2022013223A/es unknown
- 2021-04-07 CN CN202410475949.0A patent/CN118307544A/zh active Pending
- 2021-04-07 CR CR20220537A patent/CR20220537A/es 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
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