JP2019500387A - Ｈｉｖインテグラーゼ阻害剤としての縮合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の縮合三環式複素環化合物 Download PDF

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Publication number
JP2019500387A
JP2019500387A JP2018534101A JP2018534101A JP2019500387A JP 2019500387 A JP2019500387 A JP 2019500387A JP 2018534101 A JP2018534101 A JP 2018534101A JP 2018534101 A JP2018534101 A JP 2018534101A JP 2019500387 A JP2019500387 A JP 2019500387A
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compound
alkyl
hiv
mmol
int
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Pending
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JP2018534101A
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Japanese (ja)
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JP2019500387A5 (enExample
Inventor
イー，タオ
ウォッデル，シャーマン・ティー
グラハム，トーマス・エイチ
チャン，ヨンリアン
マッコーリー，ジョン・エー
ステムフォールド，アンドリュー・ダブリュー
ツァイ，ジアチアン
チー，ジーチー
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Merck Sharp and Dohme LLC
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Merck Sharp and Dohme LLC
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Publication of JP2019500387A publication Critical patent/JP2019500387A/ja
Publication of JP2019500387A5 publication Critical patent/JP2019500387A5/ja
Pending legal-status Critical Current

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    • 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
    • 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
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
    • 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
    • A61K31/50—Pyridazines; Hydrogenated pyridazines
    • A61K31/5025—Pyridazines; Hydrogenated pyridazines 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
    • 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
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • 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
    • A61K31/52—Purines, e.g. adenine
    • 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
    • A61K31/63—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide
    • A61K31/635—Compounds containing para-N-benzenesulfonyl-N-groups, e.g. sulfanilamide, p-nitrobenzenesulfonyl hydrazide having a heterocyclic ring, e.g. sulfadiazine
    • 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
    • A61K31/66—Phosphorus compounds
    • A61K31/683—Diesters of a phosphorus acid with two hydroxy compounds, e.g. phosphatidylinositols
    • 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
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
JP2018534101A 2015-12-31 2016-12-22 Ｈｉｖインテグラーゼ阻害剤としての縮合三環式複素環化合物 Pending JP2019500387A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
CNPCT/CN2015/100106 2015-12-31
PCT/CN2015/100106 WO2017113288A1 (en) 2015-12-31 2015-12-31 Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
PCT/US2016/068173 WO2017116928A1 (en) 2015-12-31 2016-12-22 Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Publications (2)

Publication Number Publication Date
JP2019500387A true JP2019500387A (ja) 2019-01-10
JP2019500387A5 JP2019500387A5 (enExample) 2020-01-23

Family

ID=57799839

Family Applications (1)

Application Number Title Priority Date Filing Date
JP2018534101A Pending JP2019500387A (ja) 2015-12-31 2016-12-22 Ｈｉｖインテグラーゼ阻害剤としての縮合三環式複素環化合物

Country Status (15)

Country Link
US (4) US20170190701A1 (enExample)
EP (1) EP3397639B1 (enExample)
JP (1) JP2019500387A (enExample)
KR (1) KR20180095833A (enExample)
CN (1) CN108473494A (enExample)
AR (1) AR107170A1 (enExample)
AU (1) AU2016381072B2 (enExample)
BR (1) BR112018013251A2 (enExample)
CA (1) CA3008018A1 (enExample)
JO (1) JO3811B1 (enExample)
MA (1) MA43528A (enExample)
MX (1) MX2018008095A (enExample)
RU (1) RU2740187C2 (enExample)
TW (1) TW201726683A (enExample)
WO (2) WO2017113288A1 (enExample)

Cited By (1)

* Cited by examiner, † Cited by third party
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JP2023514635A (ja) * 2020-02-24 2023-04-06 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖ感染症を治療するための四環式化合物及びその使用

Families Citing this family (15)

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US10081647B2 (en) * 2015-03-26 2018-09-25 Merck Sharp & Dohme Corp. Phosphate substituted quinolizine derivatives useful as HIV integrase inhibitors
JOP20190130A1 (ar) * 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
RU2749043C2 (ru) 2016-12-02 2021-06-03 Мерк Шарп И Доум Корп. Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич
KR20210005139A (ko) * 2018-04-27 2021-01-13 머크 샤프 앤드 돔 코포레이션 Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물
IL313474A (en) 2018-05-31 2024-08-01 Shionogi & Co Polycyclic carbamoylpyridone derivative
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WO2019236396A1 (en) * 2018-06-05 2019-12-12 Merck Sharp & Dohme Corp. Tricyclic heterocycle compounds useful as hiv integrase inhibitors
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HUE059677T2 (hu) 2019-03-22 2022-12-28 Gilead Sciences Inc Áthidalt triciklusos karbamoilpiridon-vegyületek és ezek gyógyszerészeti alkalmazása
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
WO2021107066A1 (ja) 2019-11-28 2021-06-03 塩野義製薬株式会社 インテグラーゼ阻害剤及び抗ｈｉｖ薬を組み合わせることを特徴とするｈｉｖ感染症の予防及び治療用医薬
JP7691494B2 (ja) 2020-09-30 2025-06-11 ギリアード サイエンシーズ， インコーポレイテッド 架橋三環式カルバモイルピリドン化合物及びその使用
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CA3208396A1 (en) * 2021-02-16 2022-08-25 Timothy John Hartingh Tetracyclic heterocycle compounds useful as hiv integrase inhibitors
TWI843506B (zh) 2022-04-06 2024-05-21 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

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Patent Citations (2)

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WO2014172188A2 (en) * 2013-04-16 2014-10-23 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
WO2014183532A1 (en) * 2013-05-17 2014-11-20 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2023514635A (ja) * 2020-02-24 2023-04-06 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖ感染症を治療するための四環式化合物及びその使用
JP7453399B2 (ja) 2020-02-24 2024-03-19 ギリアード サイエンシーズ， インコーポレイテッド Ｈｉｖ感染症を治療するための四環式化合物及びその使用

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RU2740187C2 (ru) 2021-01-12
AU2016381072B2 (en) 2020-11-26
RU2018127728A (ru) 2020-02-03
US20190322666A1 (en) 2019-10-24
JO3811B1 (ar) 2021-01-31
MX2018008095A (es) 2018-08-23
EP3397639B1 (en) 2022-02-23
EP3397639A1 (en) 2018-11-07
AR107170A1 (es) 2018-03-28
US20180099967A1 (en) 2018-04-12
CA3008018A1 (en) 2017-07-06
WO2017113288A1 (en) 2017-07-06
RU2018127728A3 (enExample) 2020-02-14
KR20180095833A (ko) 2018-08-28
BR112018013251A2 (pt) 2018-12-04
MA43528A (fr) 2018-11-07
WO2017116928A1 (en) 2017-07-06
AU2016381072A1 (en) 2018-05-31
US20170190701A1 (en) 2017-07-06
US20210040096A1 (en) 2021-02-11
TW201726683A (zh) 2017-08-01
CN108473494A (zh) 2018-08-31

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