JP2022551691A - ヒト免疫不全ウイルスの複製阻害剤 - Google Patents

ヒト免疫不全ウイルスの複製阻害剤 Download PDF

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Publication number
JP2022551691A
JP2022551691A JP2022521353A JP2022521353A JP2022551691A JP 2022551691 A JP2022551691 A JP 2022551691A JP 2022521353 A JP2022521353 A JP 2022521353A JP 2022521353 A JP2022521353 A JP 2022521353A JP 2022551691 A JP2022551691 A JP 2022551691A
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Prior art keywords
chloro
indazol
mmol
ethyl
difluorophenyl
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Ceased
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JP2022521353A
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Japanese (ja)
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JPWO2021070054A5 (https=
JP2022551691A5 (https=
Inventor
マイケル、エス.ボウシャー
カイル、イー.パーセラ
クリスティアナ、イワグウ
エリック、ピー、ギリス
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ViiV Healthcare UK No 5 Ltd
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ViiV Healthcare UK No 5 Ltd
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Publication of JP2022551691A publication Critical patent/JP2022551691A/ja
Publication of JPWO2021070054A5 publication Critical patent/JPWO2021070054A5/ja
Publication of JP2022551691A5 publication Critical patent/JP2022551691A5/ja
Ceased legal-status Critical Current

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/5365Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/537Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines spiro-condensed or forming part of bridged ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2022521353A 2019-10-08 2020-10-06 ヒト免疫不全ウイルスの複製阻害剤 Ceased JP2022551691A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201962912215P 2019-10-08 2019-10-08
US62/912,215 2019-10-08
PCT/IB2020/059377 WO2021070054A1 (en) 2019-10-08 2020-10-06 Inhibitors of human immunodeficiency virus replication

Publications (3)

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JP2022551691A true JP2022551691A (ja) 2022-12-13
JPWO2021070054A5 JPWO2021070054A5 (https=) 2023-10-17
JP2022551691A5 JP2022551691A5 (https=) 2023-10-17

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JP2022521353A Ceased JP2022551691A (ja) 2019-10-08 2020-10-06 ヒト免疫不全ウイルスの複製阻害剤

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US (1) US20220370451A1 (https=)
EP (1) EP4041729B1 (https=)
JP (1) JP2022551691A (https=)
ES (1) ES2962774T3 (https=)
WO (1) WO2021070054A1 (https=)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW202128648A (zh) * 2019-10-04 2021-08-01 英商Viiv醫療保健英國(No 5)有限公司 人類免疫不全病毒複製之抑制劑
US20250042926A1 (en) 2023-05-31 2025-02-06 Gilead Sciences, Inc. Therapeutic compounds for hiv
AR132951A1 (es) 2023-06-15 2025-08-13 Viiv Healthcare Uk No 5 Ltd Métodos e intermedios para preparar compuestos
US12594276B2 (en) 2024-02-05 2026-04-07 Viiv Healthcare Uk (No. 5) Limited Inhibitors of human immunodeficiency virus replication

Citations (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2021521131A (ja) * 2018-04-11 2021-08-26 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤としての4−オキソ−3,4−ジヒドロキナゾリン化合物
JP2022500425A (ja) * 2018-09-14 2022-01-04 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505637A (ja) * 2018-10-24 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505597A (ja) * 2018-10-25 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505841A (ja) * 2018-10-24 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022506399A (ja) * 2018-11-05 2022-01-17 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022551254A (ja) * 2019-10-01 2022-12-08 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルスの複製阻害剤
JP2022552156A (ja) * 2019-10-04 2022-12-15 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルスの複製阻害剤
JP2023505543A (ja) * 2019-12-09 2023-02-09 ヴィーブ、ヘルスケア、カンパニー カボテグラビルを含んでなる医薬組成物
JP2023521460A (ja) * 2020-04-15 2023-05-24 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルス複製の阻害剤

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CN102464654B (zh) 2010-11-12 2016-01-13 上海泓博智源医药技术有限公司 抗病毒化合物
EP2729448B1 (en) 2011-07-06 2015-09-09 Gilead Sciences, Inc. Compounds for the treatment of hiv
CN102863512B (zh) 2011-07-07 2016-04-20 上海泓博智源医药技术有限公司 抗病毒化合物
TW201443037A (zh) 2013-01-09 2014-11-16 Gilead Sciences Inc 治療用化合物
CA2896244C (en) 2013-01-09 2017-07-04 Gilead Sciences, Inc. 5-membered heteroaryls and their use as antiviral agents
CA2897268C (en) 2013-01-09 2018-12-04 Gilead Sciences, Inc. Therapeutic compounds for the treatment of viral infections
TWI694071B (zh) 2013-03-01 2020-05-21 美商基利科學股份有限公司 治療反轉錄病毒科(Retroviridae)病毒感染之治療性化合物
WO2015130966A1 (en) 2014-02-28 2015-09-03 Gilead Sciences, Inc. Antiviral agents
WO2015130964A1 (en) 2014-02-28 2015-09-03 Gilead Sciences, Inc. Therapeutic compounds
PT3186239T (pt) 2014-08-29 2019-01-10 Gilead Sciences Inc Agentes antirretrovirais
CN107151223B (zh) 2016-03-10 2020-03-31 中国医学科学院药物研究所 一类n-烷基吲哚类化合物在制备抗流感病毒药物中的用途
KR20230011471A (ko) 2016-08-19 2023-01-20 길리애드 사이언시즈, 인코포레이티드 Hiv 바이러스 감염의 예방적 또는 치유적 치료에 유용한 치료 화합물
TW201906834A (zh) 2017-05-02 2019-02-16 英商Viiv醫療保健英國(No.5)有限公司 人類免疫不全病毒複製之抑制劑
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JP2021521131A (ja) * 2018-04-11 2021-08-26 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤としての4−オキソ−3,4−ジヒドロキナゾリン化合物
JP2022500425A (ja) * 2018-09-14 2022-01-04 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505637A (ja) * 2018-10-24 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505841A (ja) * 2018-10-24 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022505597A (ja) * 2018-10-25 2022-01-14 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022506399A (ja) * 2018-11-05 2022-01-17 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤
JP2022551254A (ja) * 2019-10-01 2022-12-08 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルスの複製阻害剤
JP2022552156A (ja) * 2019-10-04 2022-12-15 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルスの複製阻害剤
JP2023505543A (ja) * 2019-12-09 2023-02-09 ヴィーブ、ヘルスケア、カンパニー カボテグラビルを含んでなる医薬組成物
JP2023521460A (ja) * 2020-04-15 2023-05-24 ビーブ、ヘルスケア、ユーケー、(ナンバー5)、リミテッド ヒト免疫不全ウイルス複製の阻害剤

Also Published As

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WO2021070054A1 (en) 2021-04-15
EP4041729C0 (en) 2023-09-27
EP4041729B1 (en) 2023-09-27
EP4041729A1 (en) 2022-08-17
US20220370451A1 (en) 2022-11-24
ES2962774T3 (es) 2024-03-21

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