PE20230827A1 - [1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2 - Google Patents

[1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2

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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
Application number
PE2022002443A
Other languages
English (en)
Inventor
Birgit Wilding
Dietrich Boese
Harald Engelhardt
Julian Fuchs
Ralph Neumueller
Mark Petronczki
Dirk Scharn
Matthias Treu
Original Assignee
Boehringer Ingelheim Int
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Boehringer Ingelheim Int filed Critical Boehringer Ingelheim Int
Publication of PE20230827A1 publication Critical patent/PE20230827A1/es

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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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (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)

Abstract

La presente invencion se refiere a compuestos derivados de [1,3]diazino[5,4-d]pirimidinas de formula (I); en donde R1 se selecciona de H, -CH3, -CCH, -OCH3 y halogeno; R2 es H o halogeno; R4 se selecciona del grupo que consiste en R4.a y R4.b; en donde Q es heterociclilo de 4-6 miembros que contiene 1 atomo de N, en donde un atomo de carbono del anillo se sustituye opcionalmente con metilo; Z es heterociclilo de 4-6 miembros que contiene 1 atomo de N, en donde un atomo de carbono del anillo se sustituye opcionalmente con metilo; y R5 es -H o -CH; y al menos uno de R1 y R2 15 no es hidrogeno. Dichos compuestos son inhibidores de HER2, particularmente inhibidores selectivos del exon 20 de HER2 y muestran un perfil de eficacia mejorado que no afecta al EGFR de tipo silvestre. Tambien se refiere a un proceso de preparacion y a una composicion farmaceutica que los comprende; siendo utiles como agentes para el tratamiento y/o la prevencion de enfermedades oncologicas
PE2022002443A 2020-04-24 2021-04-07 [1,3]DIAZINO[5,4-d]PIRIMIDINAS COMO INHIBIDORES DE HER2 PE20230827A1 (es)

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 (19)

Country Link
US (2) US11608343B2 (es)
EP (1) EP4139309A1 (es)
JP (2) JP7260723B2 (es)
KR (1) KR20230005263A (es)
CN (1) CN115485277B (es)
AR (1) AR121779A1 (es)
AU (1) AU2021260721A1 (es)
BR (1) BR112022021514A2 (es)
CA (1) CA3173602A1 (es)
CL (1) CL2022002579A1 (es)
CO (1) CO2022015054A2 (es)
CR (1) CR20220537A (es)
DO (1) DOP2022000189A (es)
EC (1) ECSP22072777A (es)
IL (1) IL297490A (es)
MX (1) MX2022013223A (es)
PE (1) PE20230827A1 (es)
TW (1) TW202206432A (es)
WO (1) WO2021213800A1 (es)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
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
KR20230143959A (ko) * 2022-04-05 2023-10-13 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

Family Cites Families (14)

* Cited by examiner, † Cited by third party
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
BR0214499A (pt) 2001-12-12 2005-05-10 Pfizer Prod Inc Derivados de quinazolina para o tratamento do crescimento anormal das células
BRPI0416190A (pt) 2003-11-06 2007-01-23 Pfizer Prod Inc combinações selectivas de inibidor erbb2/anticorpo anti erbb no tratamento do cancro
EP1971601B1 (en) 2005-11-15 2009-10-21 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
DK3157916T3 (en) 2014-06-19 2019-03-18 Ariad Pharma Inc HETEROARYL COMPOUNDS FOR CHINESE 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
JP2021501123A (ja) 2017-08-31 2021-01-14 デイナ ファーバー キャンサー インスティチュート，インコーポレイテッド Ｅｇｆｒおよび／またはｈｅｒ２の阻害剤ならびに使用方法
US11578074B2 (en) 2017-09-01 2023-02-14 Shanghai Pharmaceuticals Holding Cd., Ltd. Nitrogenous heterocyclic compound, preparation method, intermediate, composition, and application
JP2023512174A (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
US20230131720A1 (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
WO2021231400A1 (en) * 2020-05-12 2021-11-18 Accutar Biotechnology, Inc. Bis-aryl ethers containing n-acyl azetidine as egfr/her2 inhibitors

Also Published As

Publication number Publication date
CL2022002579A1 (es) 2023-05-19
CR20220537A (es) 2022-12-06
KR20230005263A (ko) 2023-01-09
AU2021260721A1 (en) 2022-09-15
CO2022015054A2 (es) 2023-02-16
DOP2022000189A (es) 2022-09-30
EP4139309A1 (en) 2023-03-01
CN115485277A (zh) 2022-12-16
US20210332054A1 (en) 2021-10-28
BR112022021514A2 (pt) 2023-01-24
AR121779A1 (es) 2022-07-06
IL297490A (en) 2022-12-01
TW202206432A (zh) 2022-02-16
CA3173602A1 (en) 2021-10-28
JP7260723B2 (ja) 2023-04-18
CN115485277B (zh) 2024-05-14
WO2021213800A1 (en) 2021-10-28
US20230374021A1 (en) 2023-11-23
US11608343B2 (en) 2023-03-21
ECSP22072777A (es) 2022-10-31
JP2023085489A (ja) 2023-06-20
JP2023512343A (ja) 2023-03-24
MX2022013223A (es) 2022-11-14

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