WO2021027943A1 - Dérivé de pyrimidinopyridazinone et son utilisation médicale - Google Patents

Dérivé de pyrimidinopyridazinone et son utilisation médicale Download PDF

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Publication number
WO2021027943A1
WO2021027943A1 PCT/CN2020/109333 CN2020109333W WO2021027943A1 WO 2021027943 A1 WO2021027943 A1 WO 2021027943A1 CN 2020109333 W CN2020109333 W CN 2020109333W WO 2021027943 A1 WO2021027943 A1 WO 2021027943A1
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WIPO (PCT)
Prior art keywords
alkyl
room temperature
crude product
reaction
membered
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Application number
PCT/CN2020/109333
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English (en)
Chinese (zh)
Inventor
魏国平
阳华
付宁
邴铁军
高倩
郭东满
闻培洋
赵谈封
杨玲
王含建
杨霞
Original Assignee
正大天晴药业集团南京顺欣制药有限公司
正大天晴药业集团股份有限公司
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Application filed by 正大天晴药业集团南京顺欣制药有限公司, 正大天晴药业集团股份有限公司 filed Critical 正大天晴药业集团南京顺欣制药有限公司
Priority to CN202080052504.1A priority Critical patent/CN114174298B/zh
Publication of WO2021027943A1 publication Critical patent/WO2021027943A1/fr

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    • 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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne un dérivé de pyrimidinopyridazinone et son utilisation médicale. Le dérivé a une structure représentée par la formule générale (I). La présente invention concerne également un procédé de préparation du composé de formule générale (I), une composition pharmaceutique de celui-ci, et son utilisation en tant qu'inhibiteur de KRas G12C dans le traitement du cancer.
PCT/CN2020/109333 2019-08-14 2020-08-14 Dérivé de pyrimidinopyridazinone et son utilisation médicale WO2021027943A1 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN202080052504.1A CN114174298B (zh) 2019-08-14 2020-08-14 哒嗪酮并嘧啶类衍生物及其医药用途

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
CN201910749791.0 2019-08-14
CN201910749791 2019-08-14
CN201910928635.0 2019-09-28
CN201910928635 2019-09-28
CN202010060070.1 2020-01-19
CN202010060070 2020-01-19

Publications (1)

Publication Number Publication Date
WO2021027943A1 true WO2021027943A1 (fr) 2021-02-18

Family

ID=74570315

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/CN2020/109333 WO2021027943A1 (fr) 2019-08-14 2020-08-14 Dérivé de pyrimidinopyridazinone et son utilisation médicale

Country Status (2)

Country Link
CN (1) CN114174298B (fr)
WO (1) WO2021027943A1 (fr)

Cited By (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN114262250A (zh) * 2021-12-24 2022-04-01 乐威医药（江苏）股份有限公司 芳香环苄基邻位双烷基的合成方法
WO2022184178A1 (fr) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Inhibiteurs de kras g12d
US11453683B1 (en) 2019-08-29 2022-09-27 Mirati Therapeutics, Inc. KRas G12D inhibitors
WO2022266206A1 (fr) 2021-06-16 2022-12-22 Erasca, Inc. Conjugués d'inhibiteurs de kras
US11548888B2 (en) 2019-01-10 2023-01-10 Mirati Therapeutics, Inc. KRas G12C inhibitors
WO2023031781A1 (fr) 2021-09-01 2023-03-09 Novartis Ag Combinaisons pharmaceutiques comprenant un inhibiteur de tead et leurs utilisations pour le traitement de cancers
US11697657B2 (en) 2019-10-28 2023-07-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
US11702418B2 (en) 2019-12-20 2023-07-18 Mirati Therapeutics, Inc. SOS1 inhibitors
US11845761B2 (en) 2020-12-18 2023-12-19 Erasca, Inc. Tricyclic pyridones and pyrimidones
US11890285B2 (en) 2019-09-24 2024-02-06 Mirati Therapeutics, Inc. Combination therapies
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
WO2024081674A1 (fr) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Polythérapies pour le traitement du cancer

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009006959A1 (fr) * 2007-07-12 2009-01-15 Merck Patent Gmbh Dérivés de pyridazinone
CN102311448A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 噻吩并嘧啶酮类dpp-iv抑制剂
WO2013028818A1 (fr) * 2011-08-23 2013-02-28 Endo Pharmaceuticals Inc. Composés de pyrimido-pyridazinone et leurs procédés d'utilisation

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2003525845A (ja) * 1997-10-28 2003-09-02 ヴィヴァス・インコーポレイテッド 勃起機能不全の処置のためのホスホジエステラーゼインヒビターの局所投与
US9242969B2 (en) * 2013-03-14 2016-01-26 Novartis Ag Biaryl amide compounds as kinase inhibitors
US20160067241A1 (en) * 2013-06-13 2016-03-10 Dennis M. Brown Compositions and methods to improve the therapeutic benefit of suboptimally administered chemical compounds including substituted naphthalimides such as amonafide for the treatment of immunological, metabolic, infectious, and benign or neoplastic hyperproliferative disease conditions
CN112830928A (zh) * 2019-11-22 2021-05-25 四川海思科制药有限公司 一种嘧啶并环衍生物及其在医药上的应用

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2009006959A1 (fr) * 2007-07-12 2009-01-15 Merck Patent Gmbh Dérivés de pyridazinone
CN102311448A (zh) * 2010-07-07 2012-01-11 中国科学院广州生物医药与健康研究院 噻吩并嘧啶酮类dpp-iv抑制剂
WO2013028818A1 (fr) * 2011-08-23 2013-02-28 Endo Pharmaceuticals Inc. Composés de pyrimido-pyridazinone et leurs procédés d'utilisation

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DAVANA GONÇALVES, MICHAEL SILVA, THIAGO SOUZA, ANDREY JACOMINI, DAVI BACK, ERNANI BASSO, SIDNEI MOURA, FERNANDA ROSA: "Synthesis of a New Polyfunctionalised Pyrimidine-4-carboxylate and Its Application for the Construction of a Series of Pyrimidine Derivatives", SYNTHESIS, GEORG THIEME VERLAG, STUTTGART, DE., vol. 48, no. 18, 31 August 2016 (2016-08-31), STUTTGART, DE., pages 3042 - 3049, XP055697404, ISSN: 0039-7881, DOI: 10.1055/s-0035-1561860 *

Cited By (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US11932633B2 (en) 2018-05-07 2024-03-19 Mirati Therapeutics, Inc. KRas G12C inhibitors
US11548888B2 (en) 2019-01-10 2023-01-10 Mirati Therapeutics, Inc. KRas G12C inhibitors
US11964989B2 (en) 2019-08-29 2024-04-23 Mirati Therapeutics, Inc. KRas G12D inhibitors
US11453683B1 (en) 2019-08-29 2022-09-27 Mirati Therapeutics, Inc. KRas G12D inhibitors
US11890285B2 (en) 2019-09-24 2024-02-06 Mirati Therapeutics, Inc. Combination therapies
US11697657B2 (en) 2019-10-28 2023-07-11 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
US11702418B2 (en) 2019-12-20 2023-07-18 Mirati Therapeutics, Inc. SOS1 inhibitors
US11845761B2 (en) 2020-12-18 2023-12-19 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022184178A1 (fr) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Inhibiteurs de kras g12d
WO2022266206A1 (fr) 2021-06-16 2022-12-22 Erasca, Inc. Conjugués d'inhibiteurs de kras
WO2023031781A1 (fr) 2021-09-01 2023-03-09 Novartis Ag Combinaisons pharmaceutiques comprenant un inhibiteur de tead et leurs utilisations pour le traitement de cancers
CN114262250A (zh) * 2021-12-24 2022-04-01 乐威医药（江苏）股份有限公司 芳香环苄基邻位双烷基的合成方法
WO2024081674A1 (fr) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Polythérapies pour le traitement du cancer

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Publication number Publication date
CN114174298B (zh) 2023-08-01
CN114174298A (zh) 2022-03-11

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