ECSP11010959A - Inhibidores de la integrasa del vih - Google Patents

Inhibidores de la integrasa del vih

Info

Publication number
ECSP11010959A
ECSP11010959A EC2011010959A ECSP11010959A ECSP11010959A EC SP11010959 A ECSP11010959 A EC SP11010959A EC 2011010959 A EC2011010959 A EC 2011010959A EC SP11010959 A ECSP11010959 A EC SP11010959A EC SP11010959 A ECSP11010959 A EC SP11010959A
Authority
EC
Ecuador
Prior art keywords
compounds
inhibitors
hiv
prophylaxis
aids
Prior art date
Application number
EC2011010959A
Other languages
English (en)
Inventor
Dai-Shi Su
John S Wai
David C Dubost
Richard C Isaacs
Mark Embrey
Thorsten E Fisher
Wayne J Thompson
Peter D Williams
Shankar Venkatraman
Richard G Ball
Eric J Choi
Tao Pei
Sarah L Trice
Original Assignee
Merck Sharp & Dohme
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 Merck Sharp & Dohme filed Critical Merck Sharp & Dohme
Publication of ECSP11010959A publication Critical patent/ECSP11010959A/es

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (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

Compuestos de Fórmula I son inhibidores de la integrasa del VIH e inhibidores de replicación del VIH:(I).donde X1, X2, Y, R1A, R1B, R2 y R3 se definen en este documento. Los compuestos son útiles para la profilaxis o tratamiento de una infección por el VIH y la profilaxis, tratamiento o retardo en la aparición o progresión del SIDA. Los compuestos se emplean frente a una infección del VIH y SIDA como compuestos en sí mismos (o como hidratos o solvatos de los mismos) o en forma de sales farmacéuticamente aceptables. Los compuestos y sus sales se pueden emplear como ingredientes en composiciones farmacéuticas, opcionalmente en combinación con otros antivirales, inmunomoduladores, antibióticos o vacunas.
EC2011010959A 2008-10-06 2011-04-06 Inhibidores de la integrasa del vih ECSP11010959A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US19527108P 2008-10-06 2008-10-06

Publications (1)

Publication Number Publication Date
ECSP11010959A true ECSP11010959A (es) 2011-05-31

Family

ID=41682332

Family Applications (1)

Application Number Title Priority Date Filing Date
EC2011010959A ECSP11010959A (es) 2008-10-06 2011-04-06 Inhibidores de la integrasa del vih

Country Status (22)

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

Families Citing this family (11)

* 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
LT3938047T (lt) 2019-03-22 2022-10-10 Gilead Sciences, Inc. Tilteliniai tricikliniai karbamoilpiridono junginiai ir jų naudojimas farmacijoje
BR112022015771A2 (pt) 2020-02-24 2022-10-11 Gilead Sciences Inc Compostos tetracíclicos para tratar a infecção por hiv
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
TW202222798A (zh) 2020-09-30 2022-06-16 美商基利科學股份有限公司 橋接三環胺甲醯基吡啶酮化合物及其用途
PT4196479T (pt) 2021-01-19 2024-01-03 Gilead Sciences Inc Compostos de piridotriazinas substituídos e suas utilizações
TWI856796B (zh) 2022-04-06 2024-09-21 美商基利科學股份有限公司 橋聯三環胺甲醯基吡啶酮化合物及其用途

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP4338192B2 (ja) 2001-08-10 2009-10-07 塩野義製薬株式会社 抗ウイルス剤
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
HU230248B1 (hu) 2001-10-26 2015-11-30 Msd Italia S.R.L. N-szubsztituált hidroxipirimidinon-karboxamid HIV-integráz inhibitorok
CA2472372C (en) 2002-01-17 2010-08-17 Melissa Egbertson Hydroxynaphthyridinone carboxamides useful as hiv integrase inhibitors
MXPA05007010A (es) * 2002-12-27 2005-08-18 Angeletti P Ist Richerche Bio Tetrahidro-4h-pirido[1,2-a]pirimidinas y compuestos relacionados utiles como inhibidores de la integrasa del virus de inmunodeficiencia humana.
WO2004062613A2 (en) 2003-01-13 2004-07-29 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
PT1732926E (pt) 2004-04-06 2009-04-03 Novartis Vaccines & Diagnostic Inibidores de cinesinas mitóticas
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
JP5116660B2 (ja) * 2005-03-31 2013-01-09 イステイチユート・デイ・リチエルケ・デイ・ビオロジア・モレコラーレ・ピ・アンジエレツテイ・エツセ・エルレ・エルレ Ｈｉｖインテグラーゼ阻害剤
US7494984B2 (en) 2005-08-31 2009-02-24 Bristol-Myers Squibb Company Substituted imidazo[1,2-a]pyrimidines as HIV viral DNA integrase inhibitors
WO2007058646A1 (en) 2005-11-15 2007-05-24 Bristol-Myers Squibb Company Hiv integrase inhibitors: cyclic pyrimidinone compounds
US7897592B2 (en) 2005-11-15 2011-03-01 Bristol-Myers Squibb Company HIV integrase inhibitors
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
WO2007143446A1 (en) 2006-05-30 2007-12-13 Bristol-Myers Squibb Company Spiro-condensed heterotricyclic compounds as 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
EP2349276A2 (en) 2011-08-03
CN102239172A (zh) 2011-11-09
PE20110344A1 (es) 2011-06-22
JP4880097B1 (ja) 2012-02-22
US20130338141A1 (en) 2013-12-19
EP2349276B1 (en) 2019-11-27
CA2738814C (en) 2014-01-28
IL212019A0 (en) 2011-06-30
JP5600311B2 (ja) 2014-10-01
CA2738814A1 (en) 2010-04-15
US20100087419A1 (en) 2010-04-08
NI201100069A (es) 2012-08-08
BRPI0920605A2 (pt) 2015-12-22
DOP2011000093A (es) 2011-07-15
JP2012504648A (ja) 2012-02-23
TW201020251A (en) 2010-06-01
AU2009302663A1 (en) 2010-04-15
EA201170537A1 (ru) 2011-12-30
ZA201102620B (en) 2011-12-28
MA32764B1 (fr) 2011-11-01
CR20110184A (es) 2011-06-08
WO2010042392A2 (en) 2010-04-15
BRPI0920605A8 (pt) 2016-04-26
MX2011003637A (es) 2011-04-27
US8513234B2 (en) 2013-08-20
KR20110066224A (ko) 2011-06-16
JP2012036207A (ja) 2012-02-23
WO2010042391A3 (en) 2010-06-03
AU2009302663B2 (en) 2012-11-08
WO2010042391A2 (en) 2010-04-15
CO6382127A2 (es) 2012-02-15
AR073769A1 (es) 2010-12-01
WO2010042392A3 (en) 2010-06-03

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