CN114174298A - 哒嗪酮并嘧啶类衍生物及其医药用途 - Google Patents

哒嗪酮并嘧啶类衍生物及其医药用途 Download PDF

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Publication number
CN114174298A
CN114174298A CN202080052504.1A CN202080052504A CN114174298A CN 114174298 A CN114174298 A CN 114174298A CN 202080052504 A CN202080052504 A CN 202080052504A CN 114174298 A CN114174298 A CN 114174298A
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reaction
room temperature
crude product
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CN114174298B (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
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Nanjing Shunxin Pharmaceutical Co Ltd
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Chia Tai Tianqing Pharmaceutical Group Co Ltd
Nanjing Shunxin Pharmaceutical Co Ltd
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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)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

哒嗪酮并嘧啶类衍生物及其医药用途，其结构如通式(I)所示，还涉及所述通式(I)化合物的制备方法、其药物组合物以及其作为KRas G12C抑制剂在治疗癌症中的用途。

Description

PCT国内申请，说明书已公开。

Claims (18)

  1. PCT国内申请，权利要求书已公开。
CN202080052504.1A 2019-08-14 2020-08-14 哒嗪酮并嘧啶类衍生物及其医药用途 Active CN114174298B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
CN201910749791 2019-08-14
CN2019107497910 2019-08-14
CN201910928635 2019-09-28
CN2019109286350 2019-09-28
CN2020100600701 2020-01-19
CN202010060070 2020-01-19
PCT/CN2020/109333 WO2021027943A1 (zh) 2019-08-14 2020-08-14 哒嗪酮并嘧啶类衍生物及其医药用途

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CN114174298A true CN114174298A (zh) 2022-03-11
CN114174298B CN114174298B (zh) 2023-08-01

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WO (1) WO2021027943A1 (zh)

Families Citing this family (12)

* 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
JP2022517222A (ja) 2019-01-10 2022-03-07 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｃ阻害剤
JP2022546043A (ja) 2019-08-29 2022-11-02 ミラティ セラピューティクス， インコーポレイテッド Ｋｒａｓ ｇ１２ｄ阻害剤
CA3152025A1 (en) 2019-09-24 2021-04-01 David BRIERE Combination therapies
AU2020372881A1 (en) 2019-10-28 2022-06-09 Merck Sharp & Dohme Llc Small molecule inhibitors of KRAS G12C mutant
EP4076418A4 (en) 2019-12-20 2024-01-24 Mirati Therapeutics Inc SOS1 INHIBITORS
US20230107642A1 (en) 2020-12-18 2023-04-06 Erasca, Inc. Tricyclic pyridones and pyrimidones
WO2022184178A1 (en) * 2021-03-05 2022-09-09 Jacobio Pharmaceuticals Co., Ltd. Kras g12d inhibitors
WO2022266206A1 (en) 2021-06-16 2022-12-22 Erasca, Inc. Kras inhibitor conjugates
WO2023031781A1 (en) 2021-09-01 2023-03-09 Novartis Ag Pharmaceutical combinations comprising a tead inhibitor and uses thereof for the treatment of 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 (en) 2022-10-11 2024-04-18 Aadi Bioscience, Inc. Combination therapies for the treatment of cancer

Citations (6)

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Publication number Priority date Publication date Assignee Title
WO1999021558A2 (en) * 1997-10-28 1999-05-06 Vivus, Inc. Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
US20100197690A1 (en) * 2007-07-12 2010-08-05 Merck Patent Gesellschaft Pyrimidinyl Pyridazinone Derivatives
US20130053346A1 (en) * 2011-08-23 2013-02-28 Endo Pharmaceuticals Inc Pyrimido-pyridazinone compounds and methods of use thereof
CN105143209A (zh) * 2013-03-14 2015-12-09 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物
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

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102311448B (zh) * 2010-07-07 2014-02-19 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

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999021558A2 (en) * 1997-10-28 1999-05-06 Vivus, Inc. Local administration of phosphodiesterase inhibitors for the treatment of erectile dysfunction
US20100197690A1 (en) * 2007-07-12 2010-08-05 Merck Patent Gesellschaft Pyrimidinyl Pyridazinone Derivatives
US20130053346A1 (en) * 2011-08-23 2013-02-28 Endo Pharmaceuticals Inc Pyrimido-pyridazinone compounds and methods of use thereof
CN105143209A (zh) * 2013-03-14 2015-12-09 诺华股份有限公司 作为激酶抑制剂的联芳基酰胺化合物
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

Non-Patent Citations (1)

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Title
吕强等: "1-甲基-3-芳基-6-三氟甲基哒嗪-4-酮类化合物的合成与生物活性", 《有机化学》 *

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CN114174298B (zh) 2023-08-01

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