EA033057B1 - Производные 5-(n-бензил-тетрагидроизохинолин-6-ил)пиридин-3-ил-уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека - Google Patents

Производные 5-(n-бензил-тетрагидроизохинолин-6-ил)пиридин-3-ил-уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека

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Publication number
EA033057B1
EA033057B1 EA201890361A EA201890361A EA033057B1 EA 033057 B1 EA033057 B1 EA 033057B1 EA 201890361 A EA201890361 A EA 201890361A EA 201890361 A EA201890361 A EA 201890361A EA 033057 B1 EA033057 B1 EA 033057B1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
alkoxy
ris
compounds
tetrahydroisoquinolin
Prior art date
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EA201890361A
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English (en)
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EA201890361A1 (ru
Inventor
Кайл Дж. Истман
Джон Ф. Кадоу
Кайли И. Парселла
Б. Нарасимхулу Наиду
Тао Ван
Чживэй Инь
Чжонсин Чзан
Original Assignee
ВАЙВ ХЕЛТКЕР ЮКей (№ 5) ЛИМИТЕД
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Application filed by ВАЙВ ХЕЛТКЕР ЮКей (№ 5) ЛИМИТЕД filed Critical ВАЙВ ХЕЛТКЕР ЮКей (№ 5) ЛИМИТЕД
Publication of EA201890361A1 publication Critical patent/EA201890361A1/ru
Publication of EA033057B1 publication Critical patent/EA033057B1/ru

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • 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
    • 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
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/04Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K2300/00Mixtures 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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Epidemiology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Molecular Biology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • AIDS & HIV (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Раскрыты соединения формулы I, включая фармацевтически приемлемые соли, фармацевтические композиции, содержащие соединения, способы получения соединений и их применение в ингибировании интегразы ВИЧ и лечении инфицированных ВИЧ или СПИД. В соединениях формулы I Rвыбран из водорода, алкила или циклоалкила; Rвыбран из тетрагидроизохинолинила и замещен одним заместителем Rи дополнительно 0-3 галогеновыми или алкильными заместителями; Rвыбран из азетидинила, пирролидинила, пиперидинила, пиперазинила, морфолинила, гомопиперидинила, гомопиперазинила или гомоморфолинила и замещен 0-3 заместителями, выбранными из циано, галогена, алкила, галогеналкила, алкокси и галогеналкокси; Rвыбран из алкила или галогеналкила; Rпредставляет собой алкил; Rвыбран из Ar, (Ar)алкила, (хроманил)алкила, цианоциклоалкила или (дигидробензодиоксинил)алкила; Arпредставляет собой фенил, замещенный 0-5 заместителями, выбранными из циано, галогена, алкила, циклоалкила, галогеналкила, гидрокси, алкокси, галогеналкокси, (гидрокси)алкокси, (алкокси)алкокси, фенокси, бензилокси, карбокси, фенила и цианоциклоалкила.
EA201890361A 2015-08-11 2016-08-10 Производные 5-(n-бензил-тетрагидроизохинолин-6-ил)пиридин-3-ил-уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека EA033057B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201562203791P 2015-08-11 2015-08-11
PCT/IB2016/054832 WO2017025917A1 (en) 2015-08-11 2016-08-10 5-(n-benzyl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

Publications (2)

Publication Number Publication Date
EA201890361A1 EA201890361A1 (ru) 2018-11-30
EA033057B1 true EA033057B1 (ru) 2019-08-30

Family

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EA201890361A EA033057B1 (ru) 2015-08-11 2016-08-10 Производные 5-(n-бензил-тетрагидроизохинолин-6-ил)пиридин-3-ил-уксусной кислоты в качестве ингибиторов репликации вируса иммунодефицита человека

Country Status (23)

Country Link
US (2) US10189816B2 (ru)
EP (1) EP3334716A1 (ru)
JP (1) JP6782766B2 (ru)
KR (1) KR20180032649A (ru)
CN (1) CN108137534A (ru)
AR (1) AR105653A1 (ru)
AU (1) AU2016306089B2 (ru)
CA (1) CA2994791A1 (ru)
CL (1) CL2018000363A1 (ru)
CO (1) CO2018001359A2 (ru)
CR (1) CR20180091A (ru)
DO (1) DOP2018000035A (ru)
EA (1) EA033057B1 (ru)
HK (1) HK1249503A1 (ru)
IL (1) IL257240B (ru)
MA (1) MA42614A (ru)
MX (1) MX2018001722A (ru)
PE (1) PE20181002A1 (ru)
PH (1) PH12018500294A1 (ru)
TW (1) TWI657086B (ru)
UA (1) UA120464C2 (ru)
WO (1) WO2017025917A1 (ru)
ZA (1) ZA201800689B (ru)

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* Cited by examiner, † Cited by third party
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JP2018522913A (ja) * 2015-08-12 2018-08-16 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤としての5−(n−[6,5]−縮合二環式アリールテトラヒドロイソキノリン−6−イル)ピリジン−3−イル酢酸誘導体
TW201718537A (zh) * 2015-08-12 2017-06-01 Viiv醫療保健英國(No.5)有限公司 做為人類免疫缺陷病毒複製抑制劑之吡啶-3-基乙酸衍生物
JP2019515003A (ja) * 2016-05-11 2019-06-06 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−3−イル酢酸誘導体
EP3455214A1 (en) * 2016-05-11 2019-03-20 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
US20200325127A1 (en) * 2016-05-11 2020-10-15 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
TW201835068A (zh) * 2017-01-03 2018-10-01 英商Viiv醫療保健英國(No.5)有限公司 作為人類免疫缺乏病毒複製之抑制劑之吡啶-3-基乙酸衍生物
JP2020503352A (ja) * 2017-01-03 2020-01-30 ヴィーブ ヘルスケア ユーケー(ナンバー5)リミテッド ヒト免疫不全ウイルス複製の阻害剤としてのピリジン−3−イル酢酸誘導体

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Publication number Publication date
CR20180091A (es) 2018-06-13
HK1249503A1 (zh) 2018-11-02
AU2016306089A1 (en) 2018-03-01
JP2018522927A (ja) 2018-08-16
ZA201800689B (en) 2021-08-25
EP3334716A1 (en) 2018-06-20
UA120464C2 (uk) 2019-12-10
PE20181002A1 (es) 2018-06-26
US10189816B2 (en) 2019-01-29
CN108137534A (zh) 2018-06-08
AR105653A1 (es) 2017-10-25
AU2016306089B2 (en) 2018-08-09
DOP2018000035A (es) 2018-03-30
US20190092754A1 (en) 2019-03-28
CO2018001359A2 (es) 2018-05-10
KR20180032649A (ko) 2018-03-30
MA42614A (fr) 2021-05-26
CL2018000363A1 (es) 2018-07-06
IL257240A (en) 2018-03-29
IL257240B (en) 2020-02-27
EA201890361A1 (ru) 2018-11-30
TW201718549A (zh) 2017-06-01
JP6782766B2 (ja) 2020-11-11
PH12018500294A1 (en) 2018-08-13
MX2018001722A (es) 2018-05-16
TWI657086B (zh) 2019-04-21
WO2017025917A1 (en) 2017-02-16
CA2994791A1 (en) 2017-02-16
US20180230129A1 (en) 2018-08-16

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