JP6028105B2 - 多環式カルバモイルピリドン化合物およびその薬学的用途 - Google Patents

多環式カルバモイルピリドン化合物およびその薬学的用途 Download PDF

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JP6028105B2
JP6028105B2 JP2015549669A JP2015549669A JP6028105B2 JP 6028105 B2 JP6028105 B2 JP 6028105B2 JP 2015549669 A JP2015549669 A JP 2015549669A JP 2015549669 A JP2015549669 A JP 2015549669A JP 6028105 B2 JP6028105 B2 JP 6028105B2
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lcms
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reaction mixture
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JP2016508134A5 (en16
JP2016508134A (ja
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ハオルン ジン，
ハオルン ジン，
スコット イー． レザーウィズ，
スコット イー． レザーウィズ，
マーティン， テレサ アレハンドラ トレホ
マーティン， テレサ アレハンドラ トレホ
エリザベス エム． ベーコン，
エリザベス エム． ベーコン，
ジェロミー ジェイ． コッテル，
ジェロミー ジェイ． コッテル，
ゼンホン アール． カイ，
ゼンホン アール． カイ，
ヒュン−ジュン ピュン，
ヒュン−ジュン ピュン，
フィリップ アントニー モーガネリ，
フィリップ アントニー モーガネリ，
ミンゼ ジ，
ミンゼ ジ，
ジェイムズ ジー． テイラー，
ジェイムズ ジー． テイラー，
シャオウー チェン，
シャオウー チェン，
マイケル アール． ミッシュ，
マイケル アール． ミッシュ，
マノジ シー． デサイ，
マノジ シー． デサイ，
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ギリアード サイエンシス インコーポレーテッド
ギリアード サイエンシス インコーポレーテッド
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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 three hetero rings
    • C07D471/14—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
    • A61K31/498—Pyrazines or piperazines ortho- and peri-condensed with carbocyclic ring systems, e.g. quinoxaline, phenazine
    • 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
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring 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
    • A61K31/529—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim forming part of bridged ring 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
    • A61K31/535—Heterocyclic 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
    • A61K31/5365—Heterocyclic 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
    • 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
    • A61K31/535—Heterocyclic 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
    • A61K31/537—Heterocyclic 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
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/551—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having two nitrogen atoms, e.g. dilazep
    • 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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/12—Heterocyclic 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 three hetero rings
    • C07D471/18—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic 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
    • C07D471/22—Heterocyclic 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 systems contains four or more hetero rings
    • 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
    • C07D487/12—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 three hetero rings
    • C07D487/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/18—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
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  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2015549669A 2012-12-21 2013-12-19 多環式カルバモイルピリドン化合物およびその薬学的用途 Active JP6028105B2 (ja)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US201261745375P 2012-12-21 2012-12-21
US61/745,375 2012-12-21
US201361788397P 2013-03-15 2013-03-15
US61/788,397 2013-03-15
US201361845803P 2013-07-12 2013-07-12
US61/845,803 2013-07-12
PCT/US2013/076367 WO2014100323A1 (en) 2012-12-21 2013-12-19 Polycyclic-carbamoylpyridone compounds and their pharmaceutical use

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JP2016508134A5 JP2016508134A5 (en16) 2016-08-12
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JP2015549669A Active JP6028105B2 (ja) 2012-12-21 2013-12-19 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2016122743A Active JP6411409B2 (ja) 2012-12-21 2016-06-21 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2018179844A Active JP6571256B2 (ja) 2012-12-21 2018-09-26 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2019145317A Active JP6933690B2 (ja) 2012-12-21 2019-08-07 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2021134172A Active JP7301918B2 (ja) 2012-12-21 2021-08-19 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2023101636A Pending JP2023134483A (ja) 2012-12-21 2023-06-21 多環式カルバモイルピリドン化合物およびその薬学的用途

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JP2018179844A Active JP6571256B2 (ja) 2012-12-21 2018-09-26 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2019145317A Active JP6933690B2 (ja) 2012-12-21 2019-08-07 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2021134172A Active JP7301918B2 (ja) 2012-12-21 2021-08-19 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2023101636A Pending JP2023134483A (ja) 2012-12-21 2023-06-21 多環式カルバモイルピリドン化合物およびその薬学的用途

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US (6) US9216996B2 (en16)
EP (4) EP2822954B1 (en16)
JP (6) JP6028105B2 (en16)
KR (8) KR102040007B1 (en16)
CN (4) CN111303152B (en16)
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Cited By (3)

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JP2016179996A (ja) * 2012-12-21 2016-10-13 ギリアード サイエンシス インコーポレーテッド 多環式カルバモイルピリドン化合物およびその薬学的用途
JP2017518356A (ja) * 2014-06-20 2017-07-06 ギリアード サイエンシス インコーポレーテッド ナトリウム（２ｒ，５ｓ，１３ａｒ）−７，９−ジオキソ−１０−（（２，４，６−トリフルオロベンジル）カルバモイル）−２，３，４，５，７，９，１３，１３ａ−オクタヒドロ−２，５−メタノピリド［１’，２’：４，５］ピラジノ［２，１−ｂ］［１，３］オキサゼピン−８−オレート
JP2017518357A (ja) * 2014-06-20 2017-07-06 ギリアード サイエンシス インコーポレーテッド （２Ｒ，５Ｓ，１３ＡＲ）−８−ヒドロキシ−７，９−ジオキソ−Ｎ−（２，４，６−トリフルオロベンジル）−２，３，４，５，７，９，１３，１３Ａ−オクタヒドロ−２，５−メタノピリド［１’，２’：４，５］ピラジノ［２，１−ｂ］［１，３］オキサゼピン−１０−カルボキサミドの結晶形

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TWI568722B (zh) 2012-06-15 2017-02-01 葛蘭馬克製藥公司 作爲ｍＰＧＥＳ－１抑制劑之三唑酮化合物
UA111305C2 (uk) 2012-12-21 2016-04-11 Пфайзер Інк. Конденсовані лактами арилу та гетероарилу
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ES2859102T3 (es) 2013-07-12 2021-10-01 Gilead Sciences Inc Compuestos de carbamoilpiridona policíclica y su uso para el tratamiento de infecciones por VIH
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ZA201503540B (en) * 2014-05-20 2016-10-26 Cipla Ltd Process for preparing polycyclic carbamoyl pyridone derivatives
PL3157915T3 (pl) 2014-06-17 2019-07-31 Pfizer Inc. Podstawione związki dihydroizochinolinonowe
TWI744723B (zh) * 2014-06-20 2021-11-01 美商基利科學股份有限公司 多環型胺甲醯基吡啶酮化合物之合成
WO2016010897A1 (en) 2014-07-14 2016-01-21 Incyte Corporation Bicyclic heteroaromatic carboxamide compounds useful as pim kinase inhibitors
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JP2022095640A (ja) * 2014-06-20 2022-06-28 ギリアード サイエンシス インコーポレーテッド ナトリウム（２ｒ，５ｓ，１３ａｒ）－７，９－ジオキソ－１０－（（２，４，６－トリフルオロベンジル）カルバモイル）－２，３，４，５，７，９，１３，１３ａ－オクタヒドロ－２，５－メタノピリド［１’，２’：４，５］ピラジノ［２，１－ｂ］［１，３］オキサゼピン－８－オレート
JP2018199687A (ja) * 2014-06-20 2018-12-20 ギリアード サイエンシス インコーポレーテッド （２Ｒ，５Ｓ，１３ＡＲ）−８−ヒドロキシ−７，９−ジオキソ−Ｎ−（２，４，６−トリフルオロベンジル）−２，３，４，５，７，９，１３，１３Ａ−オクタヒドロ−２，５−メタノピリド［１’，２’：４，５］ピラジノ［２，１−ｂ］［１，３］オキサゼピン−１０−カルボキサミドの結晶形
KR101899803B1 (ko) 2014-06-20 2018-09-20 길리애드 사이언시즈, 인코포레이티드 소듐 (2r,5s,13ar)-7,9-디옥소-10-((2,4,6-트리플루오로벤질)카르바모일)-2,3,4,5,7,9,13,13a-옥타히드로-2,5-메타노피리도[1',2':4,5]피라지노[2,1-b][1,3]옥사제핀-8-올레이트
JP2017518357A (ja) * 2014-06-20 2017-07-06 ギリアード サイエンシス インコーポレーテッド （２Ｒ，５Ｓ，１３ＡＲ）−８−ヒドロキシ−７，９−ジオキソ−Ｎ−（２，４，６−トリフルオロベンジル）−２，３，４，５，７，９，１３，１３Ａ−オクタヒドロ−２，５−メタノピリド［１’，２’：４，５］ピラジノ［２，１−ｂ］［１，３］オキサゼピン−１０−カルボキサミドの結晶形

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