EA201890361A1 - 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
EA201890361A1
EA201890361A1 EA201890361A EA201890361A EA201890361A1 EA 201890361 A1 EA201890361 A1 EA 201890361A1 EA 201890361 A EA201890361 A EA 201890361A EA 201890361 A EA201890361 A EA 201890361A EA 201890361 A1 EA201890361 A1 EA 201890361A1
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EA
Eurasian Patent Office
Prior art keywords
alkyl
alkoxy
compounds
tetrahydroisochinolin
haloalkyl
Prior art date
Application number
EA201890361A
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English (en)
Other versions
EA033057B1 (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

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 1 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; и 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 true EA201890361A1 (ru) 2018-11-30
EA033057B1 EA033057B1 (ru) 2019-08-30

Family

ID=56851651

Family Applications (1)

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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
Publication number Priority date Publication date Assignee Title
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
US10577353B2 (en) * 2015-08-12 2020-03-03 VIIV Healthcare UK (No.5) Limited 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
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
WO2017195112A1 (en) * 2016-05-11 2017-11-16 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
WO2017195113A1 (en) * 2016-05-11 2017-11-16 VIIV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
EP3565810A1 (en) * 2017-01-03 2019-11-13 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication
EP3565809A1 (en) * 2017-01-03 2019-11-13 ViiV Healthcare UK (No.5) Limited Pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

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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
US10577353B2 (en) * 2015-08-12 2020-03-03 VIIV Healthcare UK (No.5) Limited 5-(n-[6,5]-fused bicyclic aryl tetrahydroisoquinolin-6-yl) pyridin-3-yl acetic acid derivatives as inhibitors of human immunodeficiency virus replication

Also Published As

Publication number Publication date
AU2016306089A1 (en) 2018-03-01
CA2994791A1 (en) 2017-02-16
AU2016306089B2 (en) 2018-08-09
US20180230129A1 (en) 2018-08-16
HK1249503A1 (zh) 2018-11-02
ZA201800689B (en) 2021-08-25
EP3334716A1 (en) 2018-06-20
MA42614A (fr) 2021-05-26
CL2018000363A1 (es) 2018-07-06
PE20181002A1 (es) 2018-06-26
TW201718549A (zh) 2017-06-01
MX2018001722A (es) 2018-05-16
US10189816B2 (en) 2019-01-29
CO2018001359A2 (es) 2018-05-10
IL257240B (en) 2020-02-27
IL257240A (en) 2018-03-29
AR105653A1 (es) 2017-10-25
PH12018500294A1 (en) 2018-08-13
JP2018522927A (ja) 2018-08-16
WO2017025917A1 (en) 2017-02-16
TWI657086B (zh) 2019-04-21
US20190092754A1 (en) 2019-03-28
UA120464C2 (uk) 2019-12-10
DOP2018000035A (es) 2018-03-30
KR20180032649A (ko) 2018-03-30
CN108137534A (zh) 2018-06-08
EA033057B1 (ru) 2019-08-30
JP6782766B2 (ja) 2020-11-11
CR20180091A (es) 2018-06-13

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