TWI445709B - Hiv複製之抑制劑 - Google Patents

Hiv複製之抑制劑 Download PDF

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Publication number
TWI445709B
TWI445709B TW100141049A TW100141049A TWI445709B TW I445709 B TWI445709 B TW I445709B TW 100141049 A TW100141049 A TW 100141049A TW 100141049 A TW100141049 A TW 100141049A TW I445709 B TWI445709 B TW I445709B
Authority
TW
Taiwan
Prior art keywords
methyl
mmol
tetrahydro
compound
pyridin
Prior art date
Application number
TW100141049A
Other languages
English (en)
Chinese (zh)
Other versions
TW201300395A (zh
Inventor
Andrew Simon Bell
Iain Brian Gardner
Karl Richard Gibson
David Cameron Pryde
Florian Wakenhut
Original Assignee
Viiv Healthcare Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
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Publication date
Application filed by Viiv Healthcare Ltd filed Critical Viiv Healthcare Ltd
Publication of TW201300395A publication Critical patent/TW201300395A/zh
Application granted granted Critical
Publication of TWI445709B publication Critical patent/TWI445709B/zh

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4353Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437Heterocyclic 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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P31/14Antivirals for RNA viruses
    • A61P31/18Antivirals for RNA viruses for HIV
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D495/14Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D519/00Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW100141049A 2010-11-15 2011-11-10 Hiv複製之抑制劑 TWI445709B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US41361810P 2010-11-15 2010-11-15
US201161485355P 2011-05-12 2011-05-12

Publications (2)

Publication Number Publication Date
TW201300395A TW201300395A (zh) 2013-01-01
TWI445709B true TWI445709B (zh) 2014-07-21

Family

ID=44999830

Family Applications (1)

Application Number Title Priority Date Filing Date
TW100141049A TWI445709B (zh) 2010-11-15 2011-11-10 Hiv複製之抑制劑

Country Status (15)

Country Link
US (3) US8809363B2 (enExample)
EP (1) EP2640729B1 (enExample)
JP (2) JP5902704B2 (enExample)
CN (2) CN103429595B (enExample)
AR (1) AR083870A1 (enExample)
AU (2) AU2011330850B2 (enExample)
BR (1) BR112013011991A2 (enExample)
CA (1) CA2817896A1 (enExample)
CL (1) CL2013001338A1 (enExample)
MX (1) MX343274B (enExample)
RU (1) RU2564445C2 (enExample)
TW (1) TWI445709B (enExample)
UY (1) UY33729A (enExample)
WO (1) WO2012066442A1 (enExample)
ZA (1) ZA201303433B (enExample)

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AP2013006706A0 (en) 2010-07-02 2013-02-28 Gilead Sciences Inc Napht-2-ylacetic acid derivatives to treat AIDS
BR112013011737A2 (pt) 2010-11-15 2016-08-09 Univ Leuven Kath composto, uso de um composto composição farmacêutica, e, método de tratamento ou prevenção de uma infecção por hiv
CN103429595B (zh) * 2010-11-15 2015-10-21 Viiv保健英国有限公司 Hiv复制的抑制剂
UA111841C2 (uk) 2011-04-21 2016-06-24 Гіліад Сайєнсіз, Інк. Сполуки бензотіазолу та їх фармацевтичне застосування
WO2013062028A1 (ja) 2011-10-25 2013-05-02 塩野義製薬株式会社 Hiv複製阻害剤
WO2013103738A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. Napthalene acetic acid derivatives against hiv infection
US9376392B2 (en) 2012-01-04 2016-06-28 Gilead Sciences, Inc. 2-(tert-butoxy)-2-(7-methylquinolin-6-yl) acetic acid derivatives for treating AIDS
US9096586B2 (en) 2012-04-20 2015-08-04 Gilead Sciences, Inc. Therapeutic compounds
US8906929B2 (en) 2012-08-16 2014-12-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
TW201441197A (zh) 2013-01-31 2014-11-01 Shionogi & Co Hiv複製抑制劑
US9663536B2 (en) 2013-03-13 2017-05-30 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
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JP6268656B2 (ja) 2013-03-14 2018-01-31 ビーブ・ヘルスケア・ユーケイ・(ナンバー5)・リミテッドViiV Healthcare UK (No.5) Limited ヒト免疫不全ウイルス複製の阻害剤
EP2970274B1 (en) 2013-03-14 2017-03-01 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
MX2015016771A (es) 2013-06-25 2016-03-31 Squibb Bristol Myers Co Compuestos de carbazol carboxamida utiles como inhibidores de cinasa.
TWI648272B (zh) 2013-06-25 2019-01-21 美商必治妥美雅史谷比公司 經取代之四氫咔唑及咔唑甲醯胺化合物
EP2821082A1 (en) 2013-07-05 2015-01-07 Laboratoire Biodim Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use
ES2654242T3 (es) 2014-02-12 2018-02-12 Viiv Healthcare (No.5) Limited Macrociclos de benzotiazol como inhibidores de la réplica del virus de la inmunodeficiencia humana
US9409922B2 (en) 2014-02-18 2016-08-09 Bristol-Myers Squibb Company Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
WO2015126743A1 (en) 2014-02-18 2015-08-27 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US9932353B2 (en) 2014-02-18 2018-04-03 Viiv Healthcare Uk (No. 5) Limited Imidazopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US9273067B2 (en) 2014-02-19 2016-03-01 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
EP3107913B1 (en) 2014-02-19 2018-07-04 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
WO2015174511A1 (ja) 2014-05-16 2015-11-19 塩野義製薬株式会社 Hiv複製阻害作用を有する3環性複素環誘導体
AR102426A1 (es) 2014-10-24 2017-03-01 Bristol Myers Squibb Co Compuestos de indolcarboxamida como inhibidores de btk
PE20171239A1 (es) 2014-10-24 2017-08-24 Bristol Myers Squibb Co Derivados de carbazol
EA031614B1 (ru) 2014-10-24 2019-01-31 Бристол-Майерс Сквибб Компани Трициклические атропоизомерные соединения
EP3294277B1 (en) 2015-05-08 2021-01-20 Katholieke Universiteit Leuven Functional cure of retroviral infection
EP3305789A4 (en) 2015-05-29 2018-11-21 Shionogi & Co., Ltd. Nitrogen-containing tricyclic derivative having hiv replication inhibitory activity
CN111018912A (zh) * 2019-11-22 2020-04-17 苏州二叶制药有限公司 一种抗病毒药物关键中间体的合成和纯化方法

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CN103429595B (zh) * 2010-11-15 2015-10-21 Viiv保健英国有限公司 Hiv复制的抑制剂
BR112013011737A2 (pt) 2010-11-15 2016-08-09 Univ Leuven Kath composto, uso de um composto composição farmacêutica, e, método de tratamento ou prevenção de uma infecção por hiv
US9029391B2 (en) 2011-01-24 2015-05-12 Viiv Healthcare Uk Limited Isoquinoline compounds and methods for treating HIV
EP2731436B1 (en) 2011-07-15 2017-03-08 VIIV Healthcare UK Limited 2-(pyrrolo[2,3-b]pyridine-5-yl)-2-(t-butoxy)-acetic acid derivatives as hiv replication inhibitors for the treatment of aids

Also Published As

Publication number Publication date
TW201300395A (zh) 2013-01-01
CN103429595B (zh) 2015-10-21
US20140315927A1 (en) 2014-10-23
CA2817896A1 (en) 2012-05-24
JP5902704B2 (ja) 2016-04-13
US20120136023A1 (en) 2012-05-31
CN105330675A (zh) 2016-02-17
EP2640729B1 (en) 2016-12-21
CN103429595A (zh) 2013-12-04
AR083870A1 (es) 2013-03-27
RU2564445C2 (ru) 2015-10-10
EP2640729A1 (en) 2013-09-25
WO2012066442A1 (en) 2012-05-24
MX2013005486A (es) 2013-12-12
CL2013001338A1 (es) 2014-03-28
US8809363B2 (en) 2014-08-19
BR112013011991A2 (pt) 2016-08-30
AU2011330850A1 (en) 2013-06-27
US20160355528A1 (en) 2016-12-08
AU2011330850B2 (en) 2016-01-28
JP2013542247A (ja) 2013-11-21
US9447116B2 (en) 2016-09-20
UY33729A (es) 2012-06-29
ZA201303433B (en) 2014-12-23
MX343274B (es) 2016-10-31
AU2016202565A1 (en) 2016-05-19
JP2016164163A (ja) 2016-09-08
RU2013121788A (ru) 2014-12-27

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