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PE20060242A1 - Heterociclicos biciclicos como inhibidores de la integrasa del vih - Google Patents

Heterociclicos biciclicos como inhibidores de la integrasa del vih

Info

Publication number
PE20060242A1
PE20060242A1 PE2005000602A PE2005000602A PE20060242A1 PE 20060242 A1 PE20060242 A1 PE 20060242A1 PE 2005000602 A PE2005000602 A PE 2005000602A PE 2005000602 A PE2005000602 A PE 2005000602A PE 20060242 A1 PE20060242 A1 PE 20060242A1
Authority
PE
Peru
Prior art keywords
methyl
fluoro
phenyl
oxazin
carboxamide
Prior art date
Application number
PE2005000602A
Other languages
English (en)
Inventor
B Narasimhulu Naidu
Carl Ouellet
Jacques Banville
Francis Beaulieu
Timothy P Connolly
Mark R Krystal
John D Matiskella
Michael A Walker
Yasutsugu Ueda
Margaret E Sorenson
Roger Remillard
Serge Plamondon
Original Assignee
Bristol Myers Squibb Co
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 Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20060242A1 publication Critical patent/PE20060242A1/es

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-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
    • A61K31/535Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/5381,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems

Landscapes

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

Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I, DONDE R1 ES (4-FLUOROFENIL)METIL, [4-FLUORO-2-(METILAMINO-CARBONIL)FENIL]METIL, 3-[3,4-DICLOROFENIL]PROPIL, ENTRE OTROS; R2 ES H, ALQUILO (C1-C6), OH, O-(ALQUILO C1-C6); R3 ES H, HALO, CIANO, ENTRE OTROS; X, Y, Z JUNTO AL ANILLO AL QUE ESTA UNIDO ES DE PREFERENCIA PIRIMIDO[2,1-c][1,4]OXAZIN, PIRIMIDO[2,1-c][1,4]OXAZEPIN. SON COMPUESTOS PREFERIDOS: N-[[4-FLUORO-2-[(METILAMINO)CARBONIL]FENIL]METIL]-4,6,7,9-TETRAHIDRO-3-HIDROXI-9,9-DIMETIL-4-OXO-PIRIMIDO[2,1-C][1,4]OXAZIN-2-CARBOXAMIDA; 9,9-DIETIL-N-[[4-FLUORO-2-(1H-1,2,4-TRIAZOL-1-IL)FENIL)METIL]-4,6,7,9-TETRAHIDRO-3-HIDROXI-4-OXO-PIRIMIDO[2,1-C][1,4]OXAZIN-2-CARBOXAMIDA, N-[[4-FLUORO-2-(1H-1,2,4-TRIAZOL-1-IL]FENIL]METIL]-4,7,8,10-TETRAHIDRO-3-HIDROXI-10,10-DIMETIL-4-OXO-6H-PIRIMIDO[2,1-C][1,4]OXAZEPIN-2-CARBOXAMIDA. REFERIDA TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS INHIBEN LA INTEGRASA DEL VIH, UTILES EN EL TRATAMIENTO DE INFECCION POR VIH
PE2005000602A 2004-05-28 2005-05-30 Heterociclicos biciclicos como inhibidores de la integrasa del vih PE20060242A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US57551304P 2004-05-28 2004-05-28
US60337104P 2004-08-20 2004-08-20
US11/126,891 US7176196B2 (en) 2004-05-28 2005-05-11 Bicyclic heterocycles as HIV integrase inhibitors

Publications (1)

Publication Number Publication Date
PE20060242A1 true PE20060242A1 (es) 2006-03-31

Family

ID=35456854

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2005000602A PE20060242A1 (es) 2004-05-28 2005-05-30 Heterociclicos biciclicos como inhibidores de la integrasa del vih

Country Status (26)

Country Link
US (2) US7176196B2 (es)
EP (1) EP1749011B1 (es)
JP (1) JP4874959B2 (es)
KR (1) KR101097623B1 (es)
AR (1) AR049124A1 (es)
AT (1) ATE412656T1 (es)
AU (1) AU2005250356C1 (es)
BR (1) BRPI0511623A (es)
CA (1) CA2568356C (es)
CY (1) CY1110266T1 (es)
DE (1) DE602005010690D1 (es)
DK (1) DK1749011T3 (es)
ES (1) ES2315875T3 (es)
HR (1) HRP20090005T3 (es)
IL (1) IL179455A (es)
MX (1) MXPA06013835A (es)
NO (1) NO20065879L (es)
NZ (1) NZ551282A (es)
PE (1) PE20060242A1 (es)
PL (1) PL1749011T3 (es)
PT (1) PT1749011E (es)
RS (1) RS50700B (es)
RU (1) RU2381228C2 (es)
SI (1) SI1749011T1 (es)
TW (1) TWI366567B (es)
WO (1) WO2005118593A1 (es)

Families Citing this family (39)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7115601B2 (en) 2004-05-18 2006-10-03 Bristol-Myers Squibb Company HIV integrase inhibitors
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
WO2007039218A1 (en) * 2005-10-04 2007-04-12 Istituto Di Ricerche Di Biologia Molecolare P Angeletti Spa Hiv integrase inhibitors
US7902182B2 (en) * 2005-11-16 2011-03-08 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
US20070129379A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Hiv integrase inhibitors
WO2007064502A1 (en) * 2005-12-01 2007-06-07 Bristol-Myers Squibb Company Forms of n-[(4-fluorophenyl)methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide
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
US20100092427A1 (en) * 2006-07-19 2010-04-15 The University Of Georgia Research Foundation Pyridinone Diketo Acids: Inhibitors of HIV Replication in Combination Therapy
US7763630B2 (en) * 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
US8129398B2 (en) * 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
EP2280980B1 (en) * 2008-03-27 2016-03-23 Bristol-Myers Squibb Company Crystalline form of n-[[4-fluoro-2-(5-methyl-1h-1,2,4-triazol-1-yl)phenyl]methyl]-4,6,7,9-tetrahydro-3-hydroxy-9,9-dimethyl-4-oxo-pyrimido[2,1-c][1,4]oxazine-2-carboxamide, sodium salt monohydrate
CN102239172A (zh) * 2008-10-06 2011-11-09 默沙东公司 Hiv整合酶抑制剂
US8143244B2 (en) * 2009-02-26 2012-03-27 Bristol-Myers Squibb Company Cyclopropyl fused indolobenzazepine HCV NS5B inhibitors
ES2446720T3 (es) 2009-10-13 2014-03-10 Elanco Animal Health Ireland Limited Inhibidores de la integrasa macrocíclica
US8383639B2 (en) * 2009-10-15 2013-02-26 Bristol-Myers Squibb Company HIV integrase inhibitors
PH12012501095A1 (en) 2009-12-07 2015-04-22 Univ Georgia Pyridinone hydroxycyclopentyl carboxamides: hiv integrase inhibitors with therapeutic applications
SMT201800290T1 (it) 2010-01-27 2018-07-17 Viiv Healthcare Co Terapia antivirale
US8716293B2 (en) 2010-04-02 2014-05-06 Janssen R&D Ireland Macrocyclic integrase inhibitors
ES2603032T3 (es) 2010-07-15 2017-02-23 Bayer Intellectual Property Gmbh Compuestos de 3-piridil-heteroarilcarboxamida como pesticidas
US8791108B2 (en) 2011-08-18 2014-07-29 Bristol-Myers Squibb Company Inhibitors of human immunodeficiency virus replication
EP2785184B1 (en) 2011-11-30 2020-06-10 Emory University Compositions comprising jak inhibitors and haart drugs for use in the prevention or treatment of hiv
JP2015508417A (ja) * 2012-01-26 2015-03-19 クロ コンサルティング リミテッド 神経変性障害を治療するためのジアジリジン
WO2014099586A1 (en) 2012-12-17 2014-06-26 Merck Sharp & Dohme Corp. 4-pyridinonetriazine derivatives as hiv integrase inhibitors
EP2986291B1 (en) 2013-04-16 2020-05-27 Merck Sharp & Dohme Corp. 4-pyridone derivative compounds and uses thereof as hiv integrase inhibitors
EP2997033B1 (en) 2013-05-17 2017-11-15 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
WO2014200880A1 (en) 2013-06-13 2014-12-18 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
TN2016000090A1 (en) 2013-09-27 2017-07-05 Merck Sharp & Dohme Substituted quinolizine derivatives useful as hiv integrase inhibitors.
WO2016187788A1 (en) 2015-05-25 2016-12-01 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds useful for treating hiv infection
US10548910B2 (en) 2015-11-17 2020-02-04 Merck Sharp & Dohme Corp. Amido-substituted pyridotriazine derivatives useful as HIV integrase inhibitors
WO2017106071A1 (en) 2015-12-15 2017-06-22 Merck Sharp & Dohme Corp. Spirocyclic quinolizine derivatives useful as hiv integrase inhibitors
WO2017113288A1 (en) 2015-12-31 2017-07-06 Merck Sharp & Dohme Corp. Fused tricyclic heterocyclic compounds as hiv integrase inhibitors
EP3548031B1 (en) 2016-12-02 2023-07-19 Merck Sharp & Dohme LLC Tricyclic heterocycle compounds useful as hiv integrase inhibitors
JOP20190130A1 (ar) 2016-12-02 2019-06-02 Merck Sharp & Dohme مركبات حلقية غير متجانسة رباعية الحلقات مفيدة كمثبطات إنزيم مدمج لفيروس نقص المناعة البشرية (hiv)
EP3573984A4 (en) 2017-01-26 2020-07-29 Merck Sharp & Dohme Corp. USEFUL SUBSTITUTE QUINOLIZINE DERIVATIVES AS HIV INTEGRASE INHIBITORS
WO2021050555A1 (en) * 2019-09-10 2021-03-18 X-Chem, Inc. Compositions and uses thereof
CN113912622B (zh) * 2020-07-10 2023-12-01 上海纽思克生物科技有限公司 三环嘧啶酮类化合物、其制备方法、其组合物和用途

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5693641A (en) * 1996-08-16 1997-12-02 Berlex Laboratories Inc. Bicyclic pyrimidine derivatives and their use as anti-coagulants
ATE355064T1 (de) 2001-10-26 2006-03-15 Angeletti P Ist Richerche Bio Dihydroxypyrimidin-carbonsäueramid-hemmer der hiv-integrase
CN102229605B (zh) 2001-10-26 2015-01-14 Msd意大利有限公司 关于hiv整合酶的n-取代的羟基嘧啶酮甲酰胺抑制剂
EP1539762A2 (en) * 2002-06-26 2005-06-15 Bristol-Myers Squibb Company Bicyclic pyrimidinones as coagulation cascade 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.
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
BRPI0518741A2 (pt) 2004-12-03 2008-12-02 Merck & Co Inc uso de uma combinaÇço de uma droga diretamente metabolizada por ugt1a1 ou um seu sal farmaceuticamente aceitÁvel e atazanavir ou um seu sal farmaceuticamente aceitÁvel, e, combinaÇço farmacÊutica para administraÇço oral a um mamÍfero
AU2006228278C1 (en) 2005-03-31 2011-06-23 Msd Italia S.R.L. HIV integrase inhibitors

Also Published As

Publication number Publication date
RU2006146970A (ru) 2008-07-10
JP2008501018A (ja) 2008-01-17
KR20070039502A (ko) 2007-04-12
HK1107343A1 (en) 2008-04-03
WO2005118593A1 (en) 2005-12-15
DK1749011T3 (da) 2009-02-16
IL179455A0 (en) 2007-05-15
US20050267105A1 (en) 2005-12-01
EP1749011B1 (en) 2008-10-29
KR101097623B1 (ko) 2011-12-22
CY1110266T1 (el) 2015-01-14
NO20065879L (no) 2007-02-20
ATE412656T1 (de) 2008-11-15
AR049124A1 (es) 2006-06-28
MXPA06013835A (es) 2007-02-02
SI1749011T1 (sl) 2009-08-31
AU2005250356C1 (en) 2011-10-06
HRP20090005T3 (hr) 2009-02-28
US20060276466A1 (en) 2006-12-07
EP1749011A1 (en) 2007-02-07
DE602005010690D1 (de) 2008-12-11
RU2381228C2 (ru) 2010-02-10
TWI366567B (en) 2012-06-21
BRPI0511623A (pt) 2008-03-11
ES2315875T3 (es) 2009-04-01
IL179455A (en) 2011-10-31
RS50700B (sr) 2010-06-30
NZ551282A (en) 2009-05-31
JP4874959B2 (ja) 2012-02-15
PT1749011E (pt) 2008-11-27
TW200600503A (en) 2006-01-01
US7176196B2 (en) 2007-02-13
PL1749011T3 (pl) 2009-04-30
CA2568356C (en) 2012-07-03
CA2568356A1 (en) 2005-12-15
US7511037B2 (en) 2009-03-31
AU2005250356B2 (en) 2011-03-17
AU2005250356A1 (en) 2005-12-15

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