RU2749043C2 - Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич - Google Patents

Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич Download PDF

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RU2749043C2
RU2749043C2 RU2019116590A RU2019116590A RU2749043C2 RU 2749043 C2 RU2749043 C2 RU 2749043C2 RU 2019116590 A RU2019116590 A RU 2019116590A RU 2019116590 A RU2019116590 A RU 2019116590A RU 2749043 C2 RU2749043 C2 RU 2749043C2
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int
mmol
enantiomer
compound
mixture
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RU2019116590A
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RU2019116590A3 (enExample
RU2019116590A (ru
Inventor
Томас Х. ГРЭХЭМ
Тао Юй
Шерман Т. УОДДЕЛЛ
Джон А. МАККОЛИ
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Мерк Шарп И Доум Корп.
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12Heterocyclic 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
    • C07D498/16Peri-condensed 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
    • A61K31/53Heterocyclic 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
    • 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
    • A61K31/5395Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • 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
    • 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
    • C07D471/12Heterocyclic 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
    • C07D471/16Peri-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic 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
    • C07D491/22Heterocyclic 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)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (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)
RU2019116590A 2016-12-02 2017-12-01 Трициклические гетероциклические соединения, полезные в качестве ингибиторов интегразы вич RU2749043C2 (ru)

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 (3)

Publication Number Publication Date
RU2019116590A RU2019116590A (ru) 2021-01-11
RU2019116590A3 RU2019116590A3 (enExample) 2021-01-26
RU2749043C2 true RU2749043C2 (ru) 2021-06-03

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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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CA3102063A1 (en) 2018-05-31 2019-12-05 Shionogi & Co., Ltd. Polycyclic carbamoylpyridone derivative
ES2989103T3 (es) 2018-06-05 2024-11-25 Merck Sharp & Dohme Llc Compuestos de heterociclo tricíclico útiles como inhibidores de la integrasa del VIH
IL286328B1 (en) 2019-03-22 2026-04-01 Gilead Sciences Inc Tricyclic bridging compounds of carbamoylpyridone and their pharmaceutical use
US12577241B2 (en) 2019-11-28 2026-03-17 Shionogi & Co., Ltd. Polycyclic pyridopyrazine derivative
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CN112047945B (zh) * 2020-09-10 2021-11-12 浙江大学 螺环吡啶酮衍生物及应用
CA3192145A1 (en) 2020-09-30 2022-04-07 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
JP7591155B2 (ja) 2021-01-19 2024-11-27 ギリアード サイエンシーズ, インコーポレイテッド 置換ピリドトリアジン化合物及びその使用
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

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Also Published As

Publication number Publication date
CN110062627A (zh) 2019-07-26
MX2019006449A (es) 2019-09-10
RU2019116590A3 (enExample) 2021-01-26
WO2018102634A1 (en) 2018-06-07
EP3548031B1 (en) 2023-07-19
US20200017524A1 (en) 2020-01-16
AU2017367714A1 (en) 2019-05-16
BR112019011074A2 (pt) 2019-08-20
EP3548031A4 (en) 2020-06-03
CA3042314A1 (en) 2018-06-07
BR112019011074B1 (pt) 2021-01-19
MX384729B (es) 2025-03-14
EP3548031A1 (en) 2019-10-09
RU2019116590A (ru) 2021-01-11
KR20190086017A (ko) 2019-07-19
US10934312B2 (en) 2021-03-02
JP2020500866A (ja) 2020-01-16
AU2017367714B2 (en) 2020-11-12

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