BR112022021514A2 - [1,3]diazino[5,4-d]pirimidinas como inibidores de her2 - Google Patents
[1,3]diazino[5,4-d]pirimidinas como inibidores de her2Info
- Publication number
- BR112022021514A2 BR112022021514A2 BR112022021514A BR112022021514A BR112022021514A2 BR 112022021514 A2 BR112022021514 A2 BR 112022021514A2 BR 112022021514 A BR112022021514 A BR 112022021514A BR 112022021514 A BR112022021514 A BR 112022021514A BR 112022021514 A2 BR112022021514 A2 BR 112022021514A2
- Authority
- BR
- Brazil
- Prior art keywords
- diazino
- pyrimidines
- her2 inhibitors
- her2
- inhibitors
- Prior art date
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)
- 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)
Abstract
[1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INIBIDORES DE HER2. A presente invenção refere-se a novas [1,3]diazino[5,4-d]pirimidinas e derivados de Fórmula (I), em que os grupos R1, R2, R3 e R4 têm os significados dados nas reivindicações e no relatório descritivo, seus usos como inibidores de HER2 e seus mutantes, composições farmacêuticas que contêm tais compostos e seus usos como medicamentos, especialmente como agentes para tratamento e/ou prevenção de doenças oncológicas.
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 |
|---|---|
| BR112022021514A2 true BR112022021514A2 (pt) | 2023-01-24 |
Family
ID=70470818
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022021514A BR112022021514A2 (pt) | 2020-04-24 | 2021-04-07 | [1,3]diazino[5,4-d]pirimidinas como inibidores de her2 |
Country Status (19)
| Country | Link |
|---|---|
| US (2) | US11608343B2 (pt) |
| EP (1) | EP4139309A1 (pt) |
| JP (2) | JP7260723B2 (pt) |
| KR (1) | KR20230005263A (pt) |
| CN (3) | CN118307544A (pt) |
| AR (1) | AR121779A1 (pt) |
| AU (1) | AU2021260721A1 (pt) |
| BR (1) | BR112022021514A2 (pt) |
| CA (1) | CA3173602A1 (pt) |
| CL (1) | CL2022002579A1 (pt) |
| CO (1) | CO2022015054A2 (pt) |
| CR (1) | CR20220537A (pt) |
| DO (1) | DOP2022000189A (pt) |
| EC (1) | ECSP22072777A (pt) |
| IL (1) | IL297490A (pt) |
| MX (1) | MX2022013223A (pt) |
| PE (1) | PE20230827A1 (pt) |
| TW (1) | TW202206432A (pt) |
| WO (1) | WO2021213800A1 (pt) |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2022266458A1 (en) * | 2021-06-17 | 2022-12-22 | Black Diamond Therapeutics, Inc. | 6-heterocycloalkyl-quinazoline derivatives and uses thereof |
| WO2023154124A1 (en) * | 2022-02-09 | 2023-08-17 | Enliven Therapeutics, Inc. | Acylated heterocyclic quinazoline derivatives as inhibitors of erbb2 |
| 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 |
| WO2024133289A1 (en) | 2022-12-22 | 2024-06-27 | Boehringer Ingelheim International Gmbh | Solid dispersion of a her2 inhibitor |
| WO2024133325A1 (en) | 2022-12-22 | 2024-06-27 | Boehringer Ingelheim International Gmbh | Dosing schedule of a solid dispersion of a her2 inhibitor |
| WO2024133302A1 (en) | 2022-12-22 | 2024-06-27 | Boehringer Ingelheim International Gmbh | Crystalline forms of a her2 inhibitor |
Family Cites Families (14)
| 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 |
| MXPA04004107A (es) | 2001-12-12 | 2004-07-23 | Pfizer Prod Inc | Moleculas pequenas para el tratamiento del crecimiento celular anormal. |
| MXPA06005024A (es) | 2003-11-06 | 2006-07-06 | Pfizer Prod Inc | Combinaciones de inhibidor de erbb2 selectivo/anticuerpos anti-erbb en el tratamiento del cancer. |
| CA2632194C (en) | 2005-11-15 | 2012-01-03 | Array Biopharma Inc. | N4-phenyl-quinazoline-4-amine derivatives and related compounds as erbb type i receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases |
| EP3143015B1 (en) | 2014-05-13 | 2019-02-20 | ARIAD Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| EA034691B1 (ru) | 2014-06-19 | 2020-03-06 | Ариад Фармасьютикалз, Инк. | Гетероарильные соединения для ингибирования киназ |
| US20210323976A1 (en) | 2015-05-13 | 2021-10-21 | Ariad Pharmaceuticals, Inc. | Heteroaryl compounds for kinase inhibition |
| 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 |
| 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 |
| JP2023512175A (ja) | 2020-02-03 | 2023-03-24 | 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 |
| EP4100409A1 (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 |
-
2021
- 2021-04-06 US US17/223,132 patent/US11608343B2/en active Active
- 2021-04-07 CN CN202410475949.0A patent/CN118307544A/zh active Pending
- 2021-04-07 MX MX2022013223A patent/MX2022013223A/es unknown
- 2021-04-07 CN CN202180030549.3A patent/CN115485277B/zh active Active
- 2021-04-07 WO PCT/EP2021/059015 patent/WO2021213800A1/en active Application Filing
- 2021-04-07 CR CR20220537A patent/CR20220537A/es unknown
- 2021-04-07 CA CA3173602A patent/CA3173602A1/en active Pending
- 2021-04-07 AU AU2021260721A patent/AU2021260721A1/en active Pending
- 2021-04-07 BR BR112022021514A patent/BR112022021514A2/pt unknown
- 2021-04-07 IL IL297490A patent/IL297490A/en unknown
- 2021-04-07 CN CN202410475947.1A patent/CN118307543A/zh active Pending
- 2021-04-07 TW TW110112486A patent/TW202206432A/zh unknown
- 2021-04-07 PE PE2022002443A patent/PE20230827A1/es unknown
- 2021-04-07 JP JP2022563041A patent/JP7260723B2/ja active Active
- 2021-04-07 KR KR1020227040861A patent/KR20230005263A/ko active Search and Examination
- 2021-04-07 EP EP21716218.9A patent/EP4139309A1/en active Pending
- 2021-04-07 AR ARP210100910A patent/AR121779A1/es unknown
-
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
-
2023
- 2023-02-10 US US18/167,168 patent/US20230374021A1/en active Pending
- 2023-04-06 JP JP2023062141A patent/JP2023085489A/ja active Pending
Also Published As
| Publication number | Publication date |
|---|---|
| US20210332054A1 (en) | 2021-10-28 |
| CN115485277B (zh) | 2024-05-14 |
| CR20220537A (es) | 2022-12-06 |
| CN118307544A (zh) | 2024-07-09 |
| CA3173602A1 (en) | 2021-10-28 |
| US11608343B2 (en) | 2023-03-21 |
| JP2023085489A (ja) | 2023-06-20 |
| JP2023512343A (ja) | 2023-03-24 |
| MX2022013223A (es) | 2022-11-14 |
| TW202206432A (zh) | 2022-02-16 |
| DOP2022000189A (es) | 2022-09-30 |
| AU2021260721A1 (en) | 2022-09-15 |
| KR20230005263A (ko) | 2023-01-09 |
| PE20230827A1 (es) | 2023-05-19 |
| WO2021213800A1 (en) | 2021-10-28 |
| CL2022002579A1 (es) | 2023-05-19 |
| ECSP22072777A (es) | 2022-10-31 |
| IL297490A (en) | 2022-12-01 |
| CN118307543A (zh) | 2024-07-09 |
| JP7260723B2 (ja) | 2023-04-18 |
| EP4139309A1 (en) | 2023-03-01 |
| AR121779A1 (es) | 2022-07-06 |
| CO2022015054A2 (es) | 2023-02-16 |
| US20230374021A1 (en) | 2023-11-23 |
| CN115485277A (zh) | 2022-12-16 |
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