RU2740187C2 - Слитые трициклические гетероциклические соединения в качестве ингибиторов интегразы вич - Google Patents

Слитые трициклические гетероциклические соединения в качестве ингибиторов интегразы вич Download PDF

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RU2740187C2
RU2740187C2 RU2018127728A RU2018127728A RU2740187C2 RU 2740187 C2 RU2740187 C2 RU 2740187C2 RU 2018127728 A RU2018127728 A RU 2018127728A RU 2018127728 A RU2018127728 A RU 2018127728A RU 2740187 C2 RU2740187 C2 RU 2740187C2
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compound
int
mmol
group
alkyl
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RU2018127728A
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RU2018127728A3 (enExample
RU2018127728A (ru
Inventor
Тао ЙУ
Шерман Т. ВАДДЕЛЛ
Томас Х. ГРЭХАМ
Юнлянь Чжан
Джон А. МАККАУЛИ
Эндрю В. СТЭМФОРД
Цзяцян Цай
Чжици ЦИ
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Мерк Шарп энд Доум Корп.
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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Virology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (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)
RU2018127728A 2015-12-31 2016-12-22 Слитые трициклические гетероциклические соединения в качестве ингибиторов интегразы вич RU2740187C2 (ru)

Applications Claiming Priority (3)

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

Publications (3)

Publication Number Publication Date
RU2018127728A RU2018127728A (ru) 2020-02-03
RU2018127728A3 RU2018127728A3 (enExample) 2020-02-14
RU2740187C2 true RU2740187C2 (ru) 2021-01-12

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RU2018127728A RU2740187C2 (ru) 2015-12-31 2016-12-22 Слитые трициклические гетероциклические соединения в качестве ингибиторов интегразы вич

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)

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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
KR20190086017A (ko) 2016-12-02 2019-07-19 머크 샤프 앤드 돔 코포레이션 Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물
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)
KR20210005139A (ko) * 2018-04-27 2021-01-13 머크 샤프 앤드 돔 코포레이션 Hiv 인테그라제 억제제로서 유용한 트리시클릭 헤테로사이클 화합물
EP3805220B1 (en) 2018-05-31 2024-07-31 Shionogi & Co., Ltd Polycyclic carbamoylpyridone derivatives for the treatment of hiv
EA202092923A1 (ru) 2018-05-31 2021-04-09 Сионоги Энд Ко., Лтд. Полициклическое производное пиридона
US11884683B2 (en) 2018-06-05 2024-01-30 Merck Sharp & Dohme Llc Tricyclic heterocycle compounds useful as HIV integrase inhibitors
MX2021004679A (es) * 2018-10-22 2021-07-15 Univ Nebraska Profarmacos antivirales y nanoformulaciones de las mismas.
CR20240238A (es) 2019-03-22 2024-08-12 Gilead Sciences Inc Compuestos de carbamoyl piridona tricíclicos con puente y su uso farmacéutico (divisional 2021-0486)
US20200398978A1 (en) 2019-06-20 2020-12-24 Bell Helicopter Textron Inc. Low-drag rotor blade extension
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WO2022072520A1 (en) 2020-09-30 2022-04-07 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and uses thereof
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MX2023009445A (es) * 2021-02-16 2023-08-25 Merck Sharp & Dohme Llc Compuestos de heterociclos tetraciclicos utiles como inhibidores de la integrasa del vih.
TW202446773A (zh) 2022-04-06 2024-12-01 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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JP2019500387A (ja) 2019-01-10
RU2018127728A3 (enExample) 2020-02-14
AU2016381072B2 (en) 2020-11-26
US20180099967A1 (en) 2018-04-12
WO2017113288A1 (en) 2017-07-06
US20190322666A1 (en) 2019-10-24
AU2016381072A1 (en) 2018-05-31
BR112018013251A2 (pt) 2018-12-04
JO3811B1 (ar) 2021-01-31
RU2018127728A (ru) 2020-02-03
MA43528A (fr) 2018-11-07
CN108473494A (zh) 2018-08-31
KR20180095833A (ko) 2018-08-28
US20170190701A1 (en) 2017-07-06
CA3008018A1 (en) 2017-07-06
EP3397639A1 (en) 2018-11-07
AR107170A1 (es) 2018-03-28
TW201726683A (zh) 2017-08-01
US20210040096A1 (en) 2021-02-11
EP3397639B1 (en) 2022-02-23
WO2017116928A1 (en) 2017-07-06
MX2018008095A (es) 2018-08-23

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