JP2020500866A - Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 - Google Patents

Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 Download PDF

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JP2020500866A
JP2020500866A JP2019529156A JP2019529156A JP2020500866A JP 2020500866 A JP2020500866 A JP 2020500866A JP 2019529156 A JP2019529156 A JP 2019529156A JP 2019529156 A JP2019529156 A JP 2019529156A JP 2020500866 A JP2020500866 A JP 2020500866A
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JP2020500866A5 (enExample
Inventor
グラハム，トーマス・エイチ
ウォッデル，シャーマン・ティー
マッコーリー，ジョン・エー
ユー，タオ
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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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
    • C07D498/16—Peri-condensed systems
    • 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
    • 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
    • A61K31/53—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • 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
    • A61K31/5395—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 having two or more nitrogen atoms in the same ring, e.g. oxadiazines
    • 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
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • 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
    • C07D471/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/22—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains four or more hetero rings

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2019529156A 2016-12-02 2017-12-01 Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物 Ceased JP2020500866A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201662429376P 2016-12-02 2016-12-02
US62/429,376 2016-12-02
PCT/US2017/064116 WO2018102634A1 (en) 2016-12-02 2017-12-01 Tricyclic heterocycle compounds useful as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2020500866A true JP2020500866A (ja) 2020-01-16
JP2020500866A5 JP2020500866A5 (enExample) 2021-01-14

Family

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JP2019529156A Ceased JP2020500866A (ja) 2016-12-02 2017-12-01 Ｈｉｖインテグラーゼ阻害剤として有用な三環式複素環化合物

Country Status (11)

Country Link
US (1) US10934312B2 (enExample)
EP (1) EP3548031B1 (enExample)
JP (1) JP2020500866A (enExample)
KR (1) KR20190086017A (enExample)
CN (1) CN110062627A (enExample)
AU (1) AU2017367714B2 (enExample)
BR (1) BR112019011074B1 (enExample)
CA (1) CA3042314A1 (enExample)
MX (1) MX384729B (enExample)
RU (1) RU2749043C2 (enExample)
WO (1) WO2018102634A1 (enExample)

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EP4257137A3 (en) 2018-05-31 2023-11-01 Shionogi & Co., Ltd Polycyclic carbamoylpyridone derivatives for the treatment of hiv
SG11202011386QA (en) 2018-05-31 2020-12-30 Shionogi & Co Polycyclic pyridone derivative
WO2019236396A1 (en) 2018-06-05 2019-12-12 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
WO2020197991A1 (en) 2019-03-22 2020-10-01 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
IL295677A (en) 2020-02-24 2022-10-01 Gilead Sciences Inc Tetracyclic compounds for treating hiv infection
CN112047945B (zh) * 2020-09-10 2021-11-12 浙江大学 螺环吡啶酮衍生物及应用
US12421235B2 (en) 2020-09-30 2025-09-23 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
PT4196479T (pt) 2021-01-19 2024-01-03 Gilead Sciences Inc Compostos de piridotriazinas substituídos e suas utilizações
TWI856796B (zh) 2022-04-06 2024-09-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049675A1 (ja) * 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
WO2014183532A1 (en) * 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2015089847A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors
US20150329539A1 (en) * 2012-12-17 2015-11-19 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors

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EP2181985B1 (en) 2001-08-10 2011-10-26 Shionogi & Co., Ltd. Antiviral Agent
CA2463976C (en) 2001-10-26 2007-02-13 Benedetta Crescenzi N-substituted hydroxypyrimidinone carboxamide inhibitors of hiv integrase
DK1441734T3 (da) 2001-10-26 2007-06-11 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carboxamid-inhibitorer a HIV-integrase
US7279487B2 (en) 2002-01-17 2007-10-09 Merck & Co., Inc. Hydroxynaphthyridinone carboxamides useful as HIV integrase inhibitors
TWI332956B (en) 2002-04-26 2010-11-11 Gilead Sciences Inc Cellular accumulation of phosphonate analogs of hiv protease inhibitor compounds
KR20050087865A (ko) 2002-12-27 2005-08-31 이스티투토 디 리세르쉐 디 비올로지아 몰레콜라레 피. 안젤레티에스.피.에이. ＨＩＶ 인테그라제 억제제로서 유용한테트라하이드로-4Ｈ-피리도[1,2-ａ]피리미딘 및 관련화합물
WO2004062613A2 (en) 2003-01-13 2004-07-29 Bristol-Myers Squibb Company Hiv integrase inhibitors
US7037908B2 (en) 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
TW200510425A (en) 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
AR046938A1 (es) 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
US7273859B2 (en) 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
US7173022B2 (en) 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7157447B2 (en) 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7192948B2 (en) 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7176196B2 (en) 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
CN101146811B (zh) 2005-03-31 2012-01-11 P.安杰莱蒂分子生物学研究所 Hiv整合酶抑制剂
JP4295353B2 (ja) 2005-04-28 2009-07-15 スミスクライン ビーチャム コーポレーション Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
US8039458B2 (en) 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
US7897593B2 (en) 2006-05-30 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7893055B2 (en) 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors
EA019558B1 (ru) 2009-10-13 2014-04-30 Эланко Энимал Хэлс Аиэлэнд Лимитед Макроциклические ингибиторы интегразы
RU2567385C2 (ru) 2010-04-02 2015-11-10 ЯНССЕН Ар ЭНД Ди АЙРЛЭНД Макроциклические ингибиторы интегразы
EP2986291B1 (en) * 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
US9951079B2 (en) * 2013-06-13 2018-04-24 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as HIV integrase inhibitors
JP6579549B2 (ja) * 2014-05-16 2019-09-25 塩野義製薬株式会社 Ｈｉｖ複製阻害作用を有する３環性複素環誘導体
WO2016187788A1 (en) * 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2007049675A1 (ja) * 2005-10-27 2007-05-03 Shionogi & Co., Ltd. Ｈｉｖインテグラーゼ阻害活性を有する多環性カルバモイルピリドン誘導体
US20150329539A1 (en) * 2012-12-17 2015-11-19 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
WO2014183532A1 (en) * 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2015089847A1 (en) * 2013-12-20 2015-06-25 Merck Sharp & Dohme Corp. Spirocyclic heterocycle compounds useful as hiv integrase inhibitors

Also Published As

Publication number Publication date
CA3042314A1 (en) 2018-06-07
AU2017367714B2 (en) 2020-11-12
BR112019011074B1 (pt) 2021-01-19
EP3548031A1 (en) 2019-10-09
EP3548031B1 (en) 2023-07-19
MX2019006449A (es) 2019-09-10
MX384729B (es) 2025-03-14
EP3548031A4 (en) 2020-06-03
KR20190086017A (ko) 2019-07-19
US10934312B2 (en) 2021-03-02
WO2018102634A1 (en) 2018-06-07
BR112019011074A2 (pt) 2019-08-20
US20200017524A1 (en) 2020-01-16
CN110062627A (zh) 2019-07-26
RU2019116590A3 (enExample) 2021-01-26
AU2017367714A1 (en) 2019-05-16
RU2019116590A (ru) 2021-01-11
RU2749043C2 (ru) 2021-06-03

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