EA201170537A1 - Ингибиторы вич-интегразы - Google Patents

Ингибиторы вич-интегразы

Info

Publication number
EA201170537A1
EA201170537A1 EA201170537A EA201170537A EA201170537A1 EA 201170537 A1 EA201170537 A1 EA 201170537A1 EA 201170537 A EA201170537 A EA 201170537A EA 201170537 A EA201170537 A EA 201170537A EA 201170537 A1 EA201170537 A1 EA 201170537A1
Authority
EA
Eurasian Patent Office
Prior art keywords
compounds
integrase inhibitors
hiv integrase
hiv
prophylaxis
Prior art date
Application number
EA201170537A
Other languages
English (en)
Inventor
Ричард С.А. Айзакс
Уэйн Дж. Томпсон
Питер Д. Уилльямс
Дай-Ши Су
Шанкар Венкатраман
Марк В. Эмбри
Торстен Э. Фишер
Джон С. Уэй
Дэвид С. Дьюбост
Ричард Дж. Болл
Эрик Дж. Чои
Тао Пэй
Сара Л. Трайс
Original Assignee
Мерк Шарп Энд Домэ Корп.
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.)
Filing date
Publication date
Application filed by Мерк Шарп Энд Домэ Корп. filed Critical Мерк Шарп Энд Домэ Корп.
Publication of EA201170537A1 publication Critical patent/EA201170537A1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/04—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
    • A61K31/495—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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/10—Anthelmintics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/14—Ectoparasiticides, e.g. scabicides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
    • H—ELECTRICITY
    • H01—ELECTRIC ELEMENTS
    • H01L—SEMICONDUCTOR DEVICES NOT COVERED BY CLASS H10
    • H01L2924/00—Indexing scheme for arrangements or methods for connecting or disconnecting semiconductor or solid-state bodies as covered by H01L24/00
    • H01L2924/0001—Technical content checked by a classifier
    • H01L2924/0002—Not covered by any one of groups H01L24/00, H01L24/00 and H01L2224/00

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)

Abstract

Соединения формулы (I) являются ингибиторами ВИЧ-интегразы и ингибиторами ВИЧ-репликации, где X, X, Y, R, R, Rи Rимеют значения, как описано в данном контексте. Соединения пригодны для профилактики или лечения ВИЧ-инфекции и профилактики, лечения или замедления начальной стадии или прогрессирования СПИДа. Соединения применяют против ВИЧ-инфекции и СПИДа в виде самих по себе соединений (или в виде их гидратов или сольватов) или в форме фармацевтически приемлемых солей. Соединения и их соли можно применять в качестве ингредиентов в фармацевтических композициях, необязательно в комбинации с другими противовирусными агентами, иммуномодуляторами, антибиотиками или вакцинами.
EA201170537A 2008-10-06 2009-10-02 Ингибиторы вич-интегразы EA201170537A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US19527108P 2008-10-06 2008-10-06
PCT/US2009/059306 WO2010042391A2 (en) 2008-10-06 2009-10-02 Hiv integrase inhibitors

Publications (1)

Publication Number Publication Date
EA201170537A1 true EA201170537A1 (ru) 2011-12-30

Family

ID=41682332

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201170537A EA201170537A1 (ru) 2008-10-06 2009-10-02 Ингибиторы вич-интегразы

Country Status (22)

Country Link
US (2) US8513234B2 (ru)
EP (1) EP2349276B1 (ru)
JP (2) JP4880097B1 (ru)
KR (1) KR20110066224A (ru)
CN (1) CN102239172A (ru)
AR (1) AR073769A1 (ru)
AU (1) AU2009302663B2 (ru)
BR (1) BRPI0920605A8 (ru)
CA (1) CA2738814C (ru)
CO (1) CO6382127A2 (ru)
CR (1) CR20110184A (ru)
DO (1) DOP2011000093A (ru)
EA (1) EA201170537A1 (ru)
EC (1) ECSP11010959A (ru)
IL (1) IL212019A0 (ru)
MA (1) MA32764B1 (ru)
MX (1) MX2011003637A (ru)
NI (1) NI201100069A (ru)
PE (1) PE20110344A1 (ru)
TW (1) TW201020251A (ru)
WO (2) WO2010042391A2 (ru)
ZA (1) ZA201102620B (ru)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
WO2014008636A1 (en) * 2012-07-11 2014-01-16 Merck Sharp & Dohme Corp. Macrocyclic compounds as hiv integrase inhibitors
CN102936188B (zh) * 2012-11-19 2015-07-15 湖北吉和昌化工科技有限公司 一种丙炔醇缩水甘油醚的合成方法
WO2014172188A2 (en) 2013-04-16 2014-10-23 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
CN107722106A (zh) * 2016-08-11 2018-02-23 重庆大学 Hiv抑制剂
CN111684715B (zh) 2018-02-08 2023-05-02 株式会社索思未来 放大电路、加法电路、接收电路以及集成电路
US11084832B2 (en) 2019-03-22 2021-08-10 Gilead Sciences, Inc. Bridged tricyclic carbamoylpyridone compounds and their pharmaceutical use
CR20220418A (es) 2020-02-24 2022-10-10 Gilead Sciences Inc Compuestos tetracíclicos para el tratamiento de infecciones por vih
CN111454214B (zh) * 2020-05-27 2023-04-07 龙曦宁（上海）医药科技有限公司 一种2-甲氧基1-嘧啶乙胺盐酸盐的合成方法
HUE064467T2 (hu) 2021-01-19 2024-03-28 Gilead Sciences Inc Szubsztituált piridotriazin-származékok és alkalmazásuk

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN100491349C (zh) * 2001-08-10 2009-05-27 盐野义制药株式会社 抗病毒药
ATE355064T1 (de) * 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
PL212914B1 (pl) * 2001-10-26 2012-12-31 Angeletti P Ist Richerche Bio N-podstawione hydroksypirymidynonokarboksyamidy jako inhibitory integrazy HIV
ES2291642T3 (es) * 2002-01-17 2008-03-01 MERCK & CO., INC. Hidroxinaftiridinoncarboxamidas utiles como inhibidores de la integrasa de vih.
WO2004058757A1 (en) * 2002-12-27 2004-07-15 Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa Tetrahydro-4h-pyrido[1,2-a]pyrimidines and related compounds useful as hiv integrase inhibitors
US7135467B2 (en) * 2003-01-13 2006-11-14 Bristol-Myers Squibb Company HIV integrase inhibitors
US7037908B2 (en) * 2003-04-24 2006-05-02 Bristol-Myers Squibb Company HIV integrase inhibitors
TW200510425A (en) * 2003-08-13 2005-03-16 Japan Tobacco Inc Nitrogen-containing fused ring compound and use thereof as HIV integrase inhibitor
AR046938A1 (es) 2003-12-12 2006-01-04 Merck & Co Inc Procedimiento para preparar hexahidropirimido[1,2-a]azepin-2-carboxilatos y compuetos similares
TW200526635A (en) 2003-12-22 2005-08-16 Shionogi & Co Hydroxypyrimidinone derivative having HIV integrase inhibitory activity
BRPI0509653A (pt) * 2004-04-06 2007-10-09 Chiron Corp inibidores cinesina mitótica
US7273859B2 (en) * 2004-05-12 2007-09-25 Bristol-Myers Squibb Company HIV integrase inhibitors: cyclic pyrimidinone compounds
US7115601B2 (en) * 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
US7192948B2 (en) * 2004-05-28 2007-03-20 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7157447B2 (en) * 2004-05-28 2007-01-02 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7173022B2 (en) * 2004-05-28 2007-02-06 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
US7176196B2 (en) * 2004-05-28 2007-02-13 Bristol-Myers Squibb Company Bicyclic heterocycles as HIV integrase inhibitors
WO2006060225A2 (en) * 2004-11-23 2006-06-08 Merck & Co., Inc. Process for asymmetric synthesis of hexahydropyrimido[1,2-a] azepine-2-carboxamides and related compounds
AU2006228278C1 (en) * 2005-03-31 2011-06-23 Msd Italia S.R.L. HIV integrase inhibitors
US7494984B2 (en) * 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
US7897592B2 (en) * 2005-11-15 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007058646A1 (en) 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors: cyclic pyrimidinone compounds
US7902182B2 (en) * 2005-11-16 2011-03-08 Bristol-Myers Squibb Company HIV integrase inhibitors
US8039458B2 (en) * 2005-11-17 2011-10-18 Bristol-Myers Squibb Company HIV integrase inhibitors
WO2007064316A1 (en) 2005-11-30 2007-06-07 Bristol-Myers Squibb Company Bicyclic heterocycles as hiv integrase inhibitors
US7897593B2 (en) * 2006-05-30 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
US7893055B2 (en) * 2006-06-28 2011-02-22 Bristol-Myers Squibb Company HIV integrase inhibitors

Also Published As

Publication number Publication date
WO2010042392A2 (en) 2010-04-15
CA2738814A1 (en) 2010-04-15
CR20110184A (es) 2011-06-08
CA2738814C (en) 2014-01-28
AR073769A1 (es) 2010-12-01
US20100087419A1 (en) 2010-04-08
MX2011003637A (es) 2011-04-27
CO6382127A2 (es) 2012-02-15
AU2009302663B2 (en) 2012-11-08
WO2010042391A2 (en) 2010-04-15
KR20110066224A (ko) 2011-06-16
JP5600311B2 (ja) 2014-10-01
US8513234B2 (en) 2013-08-20
WO2010042392A3 (en) 2010-06-03
TW201020251A (en) 2010-06-01
DOP2011000093A (es) 2011-07-15
JP2012036207A (ja) 2012-02-23
WO2010042391A3 (en) 2010-06-03
BRPI0920605A8 (pt) 2016-04-26
NI201100069A (es) 2012-08-08
JP4880097B1 (ja) 2012-02-22
ECSP11010959A (es) 2011-05-31
ZA201102620B (en) 2011-12-28
CN102239172A (zh) 2011-11-09
BRPI0920605A2 (pt) 2015-12-22
IL212019A0 (en) 2011-06-30
US20130338141A1 (en) 2013-12-19
JP2012504648A (ja) 2012-02-23
AU2009302663A1 (en) 2010-04-15
EP2349276A2 (en) 2011-08-03
MA32764B1 (fr) 2011-11-01
EP2349276B1 (en) 2019-11-27
PE20110344A1 (es) 2011-06-22

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