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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China
Prior art keywords
methyl
compounds
tetrahydro
mmol
stirred
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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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    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (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
US61/485355 2011-05-12
US61/485,355 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)

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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)

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Country Status (15)

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

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EP2588455B1 (en) 2010-07-02 2018-04-04 Gilead Sciences, Inc. 2-quinolinyl-acetic acid derivatives as hiv antiviral compounds
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KR20140003438A (ko) 2010-11-15 2014-01-09 카톨리에케 유니버시테이트 루벤 항바이러스성 축합 헤테로사이클릭 화합물
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
US9284323B2 (en) 2012-01-04 2016-03-15 Gilead Sciences, Inc. Naphthalene 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
UY34750A (es) 2012-04-20 2013-11-29 Gilead Sciences Inc ?compuestos para el tratamiento del hiv, composiciones,métodos de preparación, intermediarios y métodos terapéuticos?.
US8906929B2 (en) 2012-08-16 2014-12-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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WO2014164409A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
ES2619708T3 (es) 2013-03-13 2017-06-26 VIIV Healthcare UK (No.5) Limited Inhibidores de la replicación del virus de inmunodeficiencia humana
WO2014164467A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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JP2016512558A (ja) 2013-03-14 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
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
AU2014302550A1 (en) 2013-06-25 2016-02-11 Bristol-Myers Squibb Company Carbazole carboxamide compounds useful as kinase inhibitors
EP2821082A1 (en) 2013-07-05 2015-01-07 Laboratoire Biodim Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use
EP3105236B1 (en) 2014-02-12 2017-10-18 ViiV Healthcare UK (No.5) Limited Benzothiazole macrocycles as inhibitors of human immunodeficiency virus replication
WO2015126758A1 (en) 2014-02-18 2015-08-27 Bristol-Myers Squibb Company Imidazopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US9834566B2 (en) 2014-02-18 2017-12-05 VIIV Healthcare UK (No.5) Limited Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US9409922B2 (en) 2014-02-18 2016-08-09 Bristol-Myers Squibb Company Imidazopyridine macrocycles as inhibitors of human immunodeficiency virus replication
PT3107913T (pt) 2014-02-19 2018-09-28 Viiv Healthcare Uk No 5 Ltd Inibidores da replicação do vírus da imunodeficiência humana
US9273067B2 (en) 2014-02-19 2016-03-01 Bristol-Myers Squibb Company Pyrazolopyrimidine macrocycles as inhibitors of human immunodeficiency virus replication
US9975906B2 (en) 2014-05-16 2018-05-22 Shionogi & Co., Ltd. Tricyclic heterocycle derivatives having HIV replication inhibitory effect
MX2017005060A (es) 2014-10-24 2017-07-05 Bristol Myers Squibb Co Compuestos atropisomeros triciclicos.
RS59707B1 (sr) 2014-10-24 2020-01-31 Bristol Myers Squibb Co Derivati karbazola
PE20190710A1 (es) 2014-10-24 2019-05-17 Bristol Myers Squibb Co Compuestos de indol carboxamida utiles como inhibidores de cinasas
EP3294277B1 (en) 2015-05-08 2021-01-20 Katholieke Universiteit Leuven Functional cure of retroviral infection
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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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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
JP2013542247A (ja) 2013-11-21
JP5902704B2 (ja) 2016-04-13
MX2013005486A (es) 2013-12-12
UY33729A (es) 2012-06-29
CL2013001338A1 (es) 2014-03-28
CN103429595A (zh) 2013-12-04
BR112013011991A2 (pt) 2016-08-30
US9447116B2 (en) 2016-09-20
US20140315927A1 (en) 2014-10-23
CN105330675A (zh) 2016-02-17
RU2564445C2 (ru) 2015-10-10
AU2011330850B2 (en) 2016-01-28
ZA201303433B (en) 2014-12-23
TWI445709B (zh) 2014-07-21
AU2011330850A1 (en) 2013-06-27
TW201300395A (zh) 2013-01-01
WO2012066442A1 (en) 2012-05-24
US20120136023A1 (en) 2012-05-31
EP2640729B1 (en) 2016-12-21
AR083870A1 (es) 2013-03-27
RU2013121788A (ru) 2014-12-27
JP2016164163A (ja) 2016-09-08
CA2817896A1 (en) 2012-05-24
US8809363B2 (en) 2014-08-19
EP2640729A1 (en) 2013-09-25
US20160355528A1 (en) 2016-12-08
MX343274B (es) 2016-10-31
AU2016202565A1 (en) 2016-05-19

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