CN103429595B - Hiv复制的抑制剂 - Google Patents

Hiv复制的抑制剂 Download PDF

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Publication number
CN103429595B
CN103429595B CN201180065030.5A CN201180065030A CN103429595B CN 103429595 B CN103429595 B CN 103429595B CN 201180065030 A CN201180065030 A CN 201180065030A CN 103429595 B CN103429595 B CN 103429595B
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CN
China
Prior art keywords
methyl
compounds
tetrahydro
mmol
stirred
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Legal status (The legal status 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 status listed.)
Expired - Fee Related
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CN201180065030.5A
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English (en)
Chinese (zh)
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CN103429595A (zh
Inventor
A.S.贝尔
I.B.加德纳
D.C.普里德
F.M.瓦肯胡特
K.R.吉布森
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ViiV Healthcare UK Ltd
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ViiV Healthcare UK Ltd
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Priority to CN201510602538.4A priority Critical patent/CN105330675A/zh
Publication of CN103429595A publication Critical patent/CN103429595A/zh
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic 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
    • C07D495/04—Ortho-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
    • A61K31/435—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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/4365—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 ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system having sulfur as a ring hetero atom, e.g. ticlopidine
    • 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
    • A61K31/4353—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 ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—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 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
    • 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
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
    • 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
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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
    • C07D495/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic 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

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  • 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)
CN201180065030.5A 2010-11-15 2011-11-01 Hiv复制的抑制剂 Expired - Fee Related CN103429595B (zh)

Priority Applications (1)

Application Number Priority Date Filing Date Title
CN201510602538.4A CN105330675A (zh) 2010-11-15 2011-11-01 Hiv复制的抑制剂

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
US41361810P 2010-11-15 2010-11-15
US61/413618 2010-11-15
US61/413,618 2010-11-15
US201161485355P 2011-05-12 2011-05-12
US61/485,355 2011-05-12
US61/485355 2011-05-12
PCT/IB2011/054852 WO2012066442A1 (en) 2010-11-15 2011-11-01 Inhibitors of hiv replication

Related Child Applications (1)

Application Number Title Priority Date Filing Date
CN201510602538.4A Division CN105330675A (zh) 2010-11-15 2011-11-01 Hiv复制的抑制剂

Publications (2)

Publication Number Publication Date
CN103429595A CN103429595A (zh) 2013-12-04
CN103429595B true CN103429595B (zh) 2015-10-21

Family

ID=44999830

Family Applications (2)

Application Number Title Priority Date Filing Date
CN201180065030.5A Expired - Fee Related CN103429595B (zh) 2010-11-15 2011-11-01 Hiv复制的抑制剂
CN201510602538.4A Pending CN105330675A (zh) 2010-11-15 2011-11-01 Hiv复制的抑制剂

Family Applications After (1)

Application Number Title Priority Date Filing Date
CN201510602538.4A Pending CN105330675A (zh) 2010-11-15 2011-11-01 Hiv复制的抑制剂

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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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
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US9663536B2 (en) 2013-03-13 2017-05-30 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
US9580431B2 (en) 2013-03-13 2017-02-28 VIIV Healthcare UK (No.5) Limited Inhibitors of human immunodeficiency virus replication
JP2016512507A (ja) 2013-03-13 2016-04-28 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ ヒト免疫不全ウイルス複製の阻害剤
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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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
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WO2005076861A2 (en) * 2004-02-04 2005-08-25 University Of Virginia Patent Foundation Compounds that inhibit hiv particle formation
WO2010130842A1 (en) * 2009-05-15 2010-11-18 Katholieke Universiteit Leuven Thieno [2, 3-b] pyridine derivatives as viral replication inhibitors

Also Published As

Publication number Publication date
TW201300395A (zh) 2013-01-01
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
TWI445709B (zh) 2014-07-21
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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