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 (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2020328598A1 (en) | 2019-08-15 | 2022-03-03 | Black Diamond Therapeutics, Inc. | Alkynyl quinazoline compounds |
| EP4100409B1 (en) * | 2020-02-03 | 2024-08-28 | 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 |
| WO2022221227A1 (en) | 2021-04-13 | 2022-10-20 | Nuvalent, Inc. | Amino-substituted heterocycles for treating cancers with egfr mutations |
| WO2022266458A1 (en) * | 2021-06-17 | 2022-12-22 | Black Diamond Therapeutics, Inc. | 6-heterocycloalkyl-quinazoline derivatives and uses thereof |
| IL309252A (en) | 2021-06-26 | 2024-02-01 | Array Biopharma Inc | Inhibitors of HER2 mutations |
| EP4476211A1 (en) * | 2022-02-09 | 2024-12-18 | Enliven Inc. | Acylated heterocyclic quinazoline derivatives as inhibitors of erbb2 |
| KR20240167844A (ko) | 2022-03-28 | 2024-11-28 | 지앙수 헨그루이 파마슈티컬스 컴퍼니 리미티드 | 질소 함유 헤테로시클릭 화합물, 이의 제조 방법 및 이의 의학적 응용 |
| IL316080A (en) * | 2022-04-05 | 2024-12-01 | Voronoi Inc | Heteroaryl derivative and use thereof |
| 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 |
| 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 |
| TW202438059A (zh) | 2022-12-22 | 2024-10-01 | 德商百靈佳殷格翰國際股份有限公司 | Her2抑制劑之結晶形式 |
| AU2024247020A1 (en) | 2023-03-29 | 2025-10-30 | Boehringer Ingelheim International Gmbh | Dosing schedule of a her2 inhibitor |
| WO2024206858A1 (en) | 2023-03-30 | 2024-10-03 | Revolution Medicines, Inc. | Compositions for inducing ras gtp hydrolysis and uses thereof |
| AU2024265078A1 (en) | 2023-05-04 | 2025-12-11 | Revolution Medicines, Inc. | Combination therapy for a ras related disease or disorder |
| WO2024246114A1 (en) | 2023-05-31 | 2024-12-05 | Boehringer Ingelheim International Gmbh | Survivin as a biomarker for predicting the responsiveness of cancer treatment |
| 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 |
| WO2025026901A1 (en) | 2023-07-28 | 2025-02-06 | Boehringer Ingelheim International Gmbh | Process for the manufacture of a her2 inhibitor |
| 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 |
| US20250205238A1 (en) | 2023-12-20 | 2025-06-26 | Boehringer Ingelheim International Gmbh | Anti-cancer combination therapy |
| US20250228858A1 (en) | 2023-12-20 | 2025-07-17 | 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 |
| 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 |
| WO2026007878A1 (zh) * | 2024-07-01 | 2026-01-08 | 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 |
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 |
| PL373848A1 (en) | 2001-12-12 | 2005-09-19 | Pfizer Products Inc. | Quinazoline derivatives for the treatment of abnormal cell growth |
| CA2544863A1 (en) | 2003-11-06 | 2005-05-19 | Pfizer Products Inc. | Selective erbb2 inhibitor/anti-erbb antibody combinations in the treatment of cancer |
| PT2090575E (pt) | 2005-11-15 | 2011-06-06 | Array Biopharma Inc | Inibidores de erbb |
| US20070107957A1 (en) * | 2005-11-16 | 2007-05-17 | Lonnie Lehrer | Automobile propulsion system |
| WO2015175632A1 (en) | 2014-05-13 | 2015-11-19 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| BR112016029662B1 (pt) | 2014-06-19 | 2023-10-24 | Takeda Pharmaceutical Company Limited | COMPOSTO DE FÓRMULA Bf OU UMA FORMA FARMACEUTICAMENTE ACEITÁVEL DO MESMO, COMPOSIÇÃO FARMACÊUTICA COMPREENDENDO O MESMO E SEU USO |
| EP3294712A4 (en) | 2015-05-13 | 2018-11-07 | ARIAD Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| EP3676267A4 (en) | 2017-08-31 | 2021-04-14 | Dana Farber Cancer Institute, Inc. | EGFR AND / OR HER2 INHIBITORS AND METHODS OF USE |
| US11578074B2 (en) | 2017-09-01 | 2023-02-14 | Shanghai Pharmaceuticals Holding Cd., Ltd. | Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application |
| JP7626774B2 (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 |
| EP4100409B1 (en) | 2020-02-03 | 2024-08-28 | 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 CN CN202410490491.6A patent/CN118388490A/zh active Pending
- 2021-04-07 CA CA3173602A patent/CA3173602A1/en active Pending
- 2021-04-07 SI SI202130269T patent/SI4139309T1/sl unknown
- 2021-04-07 PT PT217162189T patent/PT4139309T/pt unknown
- 2021-04-07 CN CN202410508210.5A patent/CN118388494A/zh active Pending
- 2021-04-07 MA MA59373A patent/MA59373B1/fr unknown
- 2021-04-07 PE PE2022002443A patent/PE20230827A1/es unknown
- 2021-04-07 HU HUE21716218A patent/HUE070805T2/hu unknown
- 2021-04-07 CN CN202410494941.9A patent/CN118388492A/zh active Pending
- 2021-04-07 CN CN202410481753.2A patent/CN118388489A/zh active Pending
- 2021-04-07 BR BR112022021514A patent/BR112022021514A2/pt unknown
- 2021-04-07 CN CN202410479058.2A patent/CN118619956A/zh active Pending
- 2021-04-07 MX MX2022013223A patent/MX2022013223A/es unknown
- 2021-04-07 HR HRP20250426TT patent/HRP20250426T1/hr unknown
- 2021-04-07 CN CN202410475949.0A patent/CN118307544A/zh active Pending
- 2021-04-07 CN CN202180030549.3A patent/CN115485277B/zh active Active
- 2021-04-07 CN CN202410508211.XA patent/CN118388495A/zh active Pending
- 2021-04-07 RS RS20250199A patent/RS66557B1/sr unknown
- 2021-04-07 CN CN202410490516.2A patent/CN118388491A/zh active Pending
- 2021-04-07 AU AU2021260721A patent/AU2021260721A1/en active Pending
- 2021-04-07 WO PCT/EP2021/059015 patent/WO2021213800A1/en not_active Ceased
- 2021-04-07 LT LTEPPCT/EP2021/059015T patent/LT4139309T/lt unknown
- 2021-04-07 KR KR1020257002191A patent/KR20250016507A/ko active Pending
- 2021-04-07 AR ARP210100910A patent/AR121779A1/es unknown
- 2021-04-07 PH PH1/2022/552745A patent/PH12022552745A1/en unknown
- 2021-04-07 TW TW110112486A patent/TW202206432A/zh unknown
- 2021-04-07 CN CN202410479057.8A patent/CN118388487A/zh active Pending
- 2021-04-07 JP JP2022563041A patent/JP7260723B2/ja active Active
- 2021-04-07 CR CR20220537A patent/CR20220537A/es unknown
- 2021-04-07 CN CN202410494942.3A patent/CN118388493A/zh active Pending
- 2021-04-07 SM SM20250164T patent/SMT202500164T1/it unknown
- 2021-04-07 PL PL21716218.9T patent/PL4139309T3/pl unknown
- 2021-04-07 IL IL320477A patent/IL320477A/en unknown
- 2021-04-07 EP EP24221865.9A patent/EP4566611A3/en active Pending
- 2021-04-07 IL IL297490A patent/IL297490B2/en unknown
- 2021-04-07 KR KR1020227040861A patent/KR102759974B1/ko active Active
- 2021-04-07 FI FIEP21716218.9T patent/FI4139309T3/fi active
- 2021-04-07 EP EP21716218.9A patent/EP4139309B9/en active Active
- 2021-04-07 DK DK21716218.9T patent/DK4139309T5/da active
- 2021-04-07 CN CN202410481750.9A patent/CN118388488A/zh active Pending
- 2021-04-07 CN CN202410475947.1A patent/CN118307543A/zh active Pending
- 2021-04-07 ES ES21716218T patent/ES3013860T3/es active Active
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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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