JP2023524489A - コロナウイルス感染症を処置するための共有結合修飾を有するｓａｒｓ－ｃｏｖ－２阻害剤 - Google Patents

コロナウイルス感染症を処置するための共有結合修飾を有するｓａｒｓ－ｃｏｖ－２阻害剤 Download PDF

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JP2023524489A
JP2023524489A JP2022566330A JP2022566330A JP2023524489A JP 2023524489 A JP2023524489 A JP 2023524489A JP 2022566330 A JP2022566330 A JP 2022566330A JP 2022566330 A JP2022566330 A JP 2022566330A JP 2023524489 A JP2023524489 A JP 2023524489A
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alkyl
solvate
pharmaceutically acceptable
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ザボロンコフス，アレクサンドルス
イバネンコフ，ヤン・エイ
ザグリベルニー，ボグダン
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インシリコ メディシン アイピー リミテッド
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    • C07—ORGANIC CHEMISTRY
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    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D213/54—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/56—Amides
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    • 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
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/501—Pyridazines; Hydrogenated pyridazines not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • 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
    • A—HUMAN NECESSITIES
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    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
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    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
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    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/12—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring
    • C07D217/14—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals
    • C07D217/16—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems with radicals, substituted by hetero atoms, attached to carbon atoms of the nitrogen-containing ring other than aralkyl radicals substituted by oxygen atoms
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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/04—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D233/28—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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    • C07D233/32—One oxygen atom
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    • C07D237/02—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings
    • C07D237/06—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D237/08—Heterocyclic compounds containing 1,2-diazine or hydrogenated 1,2-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/26—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/12—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • 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
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring

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  • Veterinary Medicine (AREA)
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  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
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JP2022566330A 2020-04-30 2021-04-29 コロナウイルス感染症を処置するための共有結合修飾を有するｓａｒｓ－ｃｏｖ－２阻害剤 Ceased JP2023524489A (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US202063017878P 2020-04-30 2020-04-30
US63/017,878 2020-04-30
US202063059095P 2020-07-30 2020-07-30
US63/059,095 2020-07-30
US202063112087P 2020-11-10 2020-11-10
US63/112,087 2020-11-10
PCT/CN2021/091093 WO2021219089A1 (en) 2020-04-30 2021-04-29 Sars-cov-2 inhibitors having covalent modifications for treating coronavirus infections

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JP2023524489A true JP2023524489A (ja) 2023-06-12
JP2023524489A5 JP2023524489A5 (enExample) 2024-05-09

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US (1) US20230174488A1 (enExample)
EP (1) EP4143176A4 (enExample)
JP (1) JP2023524489A (enExample)
CN (1) CN115803322B (enExample)
TW (1) TW202200551A (enExample)
WO (1) WO2021219089A1 (enExample)

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WO2021219089A1 (en) * 2020-04-30 2021-11-04 Insilico Medicine Ip Limited Sars-cov-2 inhibitors having covalent modifications for treating coronavirus infections
WO2022119756A1 (en) * 2020-12-04 2022-06-09 Arizona Board Of Regents On Behalf Of The University Of Arizona Compositions and methods for inhibiting m pro protease activity and for preventing and treating sars-cov-2 infection
WO2022221686A1 (en) * 2021-04-15 2022-10-20 Pardes Biosciences, Inc. Inhibitors of cysteine proteases and methods of use thereof
WO2023078238A1 (en) * 2021-11-02 2023-05-11 Insilico Medicine Ip Limited Sars-cov-2 inhibitors for treating coronavirus infections
JP2024542969A (ja) * 2021-11-02 2024-11-19 インシリコ メディシン アイピー リミテッド コロナウイルス感染を処置するためのｓａｒｓ－ｃｏｖ－２阻害剤
CN117143082B (zh) * 2022-03-07 2026-07-03 广州国家实验室 用作3c样蛋白酶抑制剂的氮杂双环[3.1.0]己烷衍生物
US20240158368A1 (en) 2022-10-14 2024-05-16 Abbvie Inc. Pyrrolidine Main Protease Inhibitors as Antiviral Agents
WO2024174966A1 (en) * 2023-02-20 2024-08-29 Insilico Medicine Ip Limited Mpro inhibitors for treating coronavirus infections
WO2024222796A1 (en) * 2023-04-26 2024-10-31 Insilico Medicine Ip Limited Crystalline sars-cov-2 inhibitor and uses thereof
WO2025067202A1 (en) * 2023-09-25 2025-04-03 Insilico Medicine Ip Limited 3cl-protease inhibitors for treating or preventing veterinary coronavirus infections
CN117756760B (zh) * 2024-01-10 2026-07-31 山东邹平大展新材料有限公司 一种2,3-二氢苯并呋喃的合成方法
CN118344285B (zh) * 2024-01-10 2025-06-06 中国药科大学 一类靶向SARS-Cov-2 3CLpro的化合物及其用途

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JP2011523956A (ja) * 2008-06-13 2011-08-25 シトミク システム 癌の治療のために用いることができる化合物
WO2014011973A2 (en) * 2012-07-13 2014-01-16 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-ras-selective lethal compounds and their use

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US9975885B2 (en) * 2016-04-28 2018-05-22 Purdue Research Foundation Broad-spectrum non-covalent coronavirus protease inhibitors
WO2021219089A1 (en) * 2020-04-30 2021-11-04 Insilico Medicine Ip Limited Sars-cov-2 inhibitors having covalent modifications for treating coronavirus infections

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JP2011523956A (ja) * 2008-06-13 2011-08-25 シトミク システム 癌の治療のために用いることができる化合物
WO2014011973A2 (en) * 2012-07-13 2014-01-16 The Trustees Of Columbia University In The City Of New York Quinazolinone-based oncogenic-ras-selective lethal compounds and their use

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