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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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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Publication of CN103429595B publication Critical patent/CN103429595B/zh
Expired - Fee Related legal-status Critical Current
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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)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (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)
  • 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
US61/413,618 2010-11-15
US61/413618 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

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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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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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US9102614B2 (en) 2010-07-02 2015-08-11 Gilead Sciences, Inc. Naphth-2-ylacetic acid derivatives to treat AIDS
EP2640729B1 (en) * 2010-11-15 2016-12-21 VIIV Healthcare UK Limited Inhibitors of hiv replication
NZ610315A (en) 2010-11-15 2015-08-28 Univ Leuven Kath Antiviral condensed heterocyclic compounds
PE20141066A1 (es) 2011-04-21 2014-09-05 Gilead Sciences Inc Compuestos de benzotiazol
WO2013062028A1 (ja) 2011-10-25 2013-05-02 塩野義製薬株式会社 Hiv複製阻害剤
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
WO2013103738A1 (en) 2012-01-04 2013-07-11 Gilead Sciences, Inc. Napthalene acetic acid derivatives against hiv infection
PH12014500842A1 (en) 2012-04-20 2014-06-09 Gilead Sciences Inc Benzothiazol-6-yl acetic acid derivatives and their use for treating an hiv infection
US8906929B2 (en) 2012-08-16 2014-12-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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WO2014164467A1 (en) 2013-03-13 2014-10-09 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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ES2623777T3 (es) 2013-03-13 2017-07-12 VIIV Healthcare UK (No.5) Limited Inhibidores de la replicación del virus de la inmunodeficiencia humana
EP2970297A1 (en) 2013-03-14 2016-01-20 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
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UY35625A (es) 2013-06-25 2014-12-31 Bristol Myers Squibb Company Una Corporación Del Estado De Delaware Compuestos de tetrahidrocarbazol y carbazol carboxamida sustituidos como inhibidores de quinasa
CN105473573B (zh) 2013-06-25 2018-03-16 百时美施贵宝公司 用作激酶抑制剂的咔唑甲酰胺化合物
EP2821082A1 (en) 2013-07-05 2015-01-07 Laboratoire Biodim Method of producing an inactivated lentivirus, especially HIV, vaccine, kit and method of use
US9944656B2 (en) 2014-02-12 2018-04-17 VIIV Healthcare UK (No.5) Limited Benzothiazole 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
EP3116879A1 (en) 2014-02-18 2017-01-18 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
ES2687322T3 (es) 2014-02-19 2018-10-24 VIIV Healthcare UK (No.5) Limited Inhibidores de la replicación del virus de inmunodeficiencia humana
US9975906B2 (en) 2014-05-16 2018-05-22 Shionogi & Co., Ltd. Tricyclic heterocycle derivatives having HIV replication inhibitory effect
US10023534B2 (en) 2014-10-24 2018-07-17 Bristol-Myers Squibb Company Carbazole and tetrahydrocarbazole compounds useful as inhibitors of BTK
PE20190710A1 (es) 2014-10-24 2019-05-17 Bristol Myers Squibb Co Compuestos de indol carboxamida utiles como inhibidores de cinasas
RS59707B1 (sr) 2014-10-24 2020-01-31 Bristol Myers Squibb Co Derivati karbazola
US10806734B2 (en) 2015-05-08 2020-10-20 Katholieke Universiteit Leuven Functional cure of retroviral infection
CA2987384A1 (en) 2015-05-29 2016-12-08 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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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
ZA201303433B (en) 2014-12-23
TWI445709B (zh) 2014-07-21
MX343274B (es) 2016-10-31
JP2013542247A (ja) 2013-11-21
CL2013001338A1 (es) 2014-03-28
RU2564445C2 (ru) 2015-10-10
JP2016164163A (ja) 2016-09-08
AR083870A1 (es) 2013-03-27
JP5902704B2 (ja) 2016-04-13
US20120136023A1 (en) 2012-05-31
RU2013121788A (ru) 2014-12-27
EP2640729B1 (en) 2016-12-21
US9447116B2 (en) 2016-09-20
BR112013011991A2 (pt) 2016-08-30
WO2012066442A1 (en) 2012-05-24
AU2011330850A1 (en) 2013-06-27
MX2013005486A (es) 2013-12-12
US8809363B2 (en) 2014-08-19
AU2016202565A1 (en) 2016-05-19
CN103429595A (zh) 2013-12-04
UY33729A (es) 2012-06-29
CN105330675A (zh) 2016-02-17
EP2640729A1 (en) 2013-09-25
US20160355528A1 (en) 2016-12-08
AU2011330850B2 (en) 2016-01-28

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