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PE20071080A1 - Compuestos de pirimidinona biciclicos como inhibidores de la integrasa de hiv - Google Patents

Compuestos de pirimidinona biciclicos como inhibidores de la integrasa de hiv

Info

Publication number
PE20071080A1
PE20071080A1 PE2006001455A PE2006001455A PE20071080A1 PE 20071080 A1 PE20071080 A1 PE 20071080A1 PE 2006001455 A PE2006001455 A PE 2006001455A PE 2006001455 A PE2006001455 A PE 2006001455A PE 20071080 A1 PE20071080 A1 PE 20071080A1
Authority
PE
Peru
Prior art keywords
alkyl
bicycle
inhibitors
hiv integrase
compounds
Prior art date
Application number
PE2006001455A
Other languages
English (en)
Inventor
B Narasimhulu Naidu
Yasutsugu Ueda
John D Matiskella
Michael A Walker
Jacques Banville
Francis Beaulieu
Carl Ouellet
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 PE20071080A1 publication Critical patent/PE20071080A1/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
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
    • 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
    • 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
    • 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
    • C07D498/10—Spiro-condensed systems
    • 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
    • C07D498/12—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 three hetero rings
    • C07D498/20—Spiro-condensed systems

Landscapes

  • 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)
  • Communicable Diseases (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Virology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

SE REFIERE A COMPUESTOS PIRIMIDINONA BICICLICOS DE FORMULA (I) EN DONDE R1 ES (Ar1)ALQUILO, (Ar1)(CON(R8)(R9)ALQUILO, (Ar1)(CO2R14)ALQUILO, ENTRE OTROS; R2 ES H, ALQUILO, ENTRE OTROS; Ar1 ES (a), (b), DONDE R3 ES H, HALO, CON(R8)(R9), SO2R7, Ar2, ENTRE OTROS; Ar2 ES TETRAZOLILO, TRIAZOLILO, OXADIAZOLILO, ENTRE OTROS, OPCIONALMENTE SUSTITUIDOS; X-Y-Z ES C(R14)2C(R14)2OC(CR14)2, C(R14)2C(R14)2OC(CR14)2C(CR14)2, ENTRE OTROS; R14 ES H, ALQUILO O DOS R14 TOMADOS CONJUNTAMENTE FORMAN CH2(CH2)2-5, CH2CH2OCH2CH2, ENTRE OTROS. SON PREFERIDOS: N-((4-FLUOROFENIL)METIL)-3-HIDROXI-10,10-DIMETIL-4-OXO-6,7,9,10-TETRAHIDRO-4H-PIRIMIDO[1,2-d][1,4]OXAZEPIN-2-CARBOXAMIDA, N-((4-FLUORO-2-(1H-1,2,4-TRIAZOL-1-IL)FENIL)METIL)-3-HIDROXI-10,10-DIMETIL-4-OXO-6,7,9,10-TETRAHIDRO-4H-PIRIMIDO[1,2-d][1,4]OXAZEPIN-2-CARBOXAMIDA, ENTRE OTROS. TAMBIEN SE REFIERE A UNA COMPOSICION FARMACEUTICA Y UN PROCEDIMIENTO DE PREPARACION. ESTOS COMPUESTOS SON INHIBIDORES DE LA INTEGRASA DEL HIV Y SON UTILES PARA EL TRATAMIENTO DE PACIENTES INFECTADOS POR HIV O SIDA
PE2006001455A 2005-11-17 2006-11-15 Compuestos de pirimidinona biciclicos como inhibidores de la integrasa de hiv PE20071080A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US73778105P 2005-11-17 2005-11-17
US11/590,637 US8039458B2 (en) 2005-11-17 2006-10-31 HIV integrase inhibitors

Publications (1)

Publication Number Publication Date
PE20071080A1 true PE20071080A1 (es) 2007-11-19

Family

ID=38041727

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2006001455A PE20071080A1 (es) 2005-11-17 2006-11-15 Compuestos de pirimidinona biciclicos como inhibidores de la integrasa de hiv

Country Status (20)

Country Link
US (1) US8039458B2 (es)
EP (1) EP1948666B1 (es)
JP (1) JP2009515981A (es)
KR (1) KR20080069254A (es)
CN (1) CN101360752B (es)
AR (1) AR057896A1 (es)
AT (1) ATE461202T1 (es)
AU (1) AU2006316582B2 (es)
CY (1) CY1110665T1 (es)
DE (1) DE602006013025D1 (es)
DK (1) DK1948666T3 (es)
ES (1) ES2341132T3 (es)
HR (1) HRP20100247T1 (es)
NO (1) NO20081935L (es)
PE (1) PE20071080A1 (es)
PL (1) PL1948666T3 (es)
PT (1) PT1948666E (es)
SI (1) SI1948666T1 (es)
TW (1) TW200738728A (es)
WO (1) WO2007061714A1 (es)

Families Citing this family (31)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7763630B2 (en) * 2007-06-06 2010-07-27 Bristol-Myers Squibb Company HIV integrase inhibitors
MX2010007952A (es) 2008-02-07 2010-08-04 Bayer Cropscience Ag Arilpirrolinas insecticidas.
US8129398B2 (en) * 2008-03-19 2012-03-06 Bristol-Myers Squibb Company HIV integrase inhibitors
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
JP2012527414A (ja) 2009-05-19 2012-11-08 バイエル・クロップサイエンス・アーゲー 殺虫性アリールピロリン
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
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
EP2686312B1 (en) 2011-03-14 2016-08-31 Boehringer Ingelheim International GmbH N-cyclopropyl-n-piperidinylbenzamides as gpr119 modulators
WO2012168315A1 (en) 2011-06-09 2012-12-13 Boehringer Ingelheim International Gmbh Substituted piperidines as gpr119 modulators for the treatment of metabolic disorders
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
WO2014019967A1 (en) 2012-08-02 2014-02-06 Boehringer Ingelheim International Gmbh N-cyclopropyl-n-piperidinyl-amides, pharmaceutical compositions containing them and uses thereof
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
CN105307651A (zh) * 2013-04-22 2016-02-03 艾伯维公司 噻唑类化合物及其用途
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.
ES2708344T3 (es) * 2015-01-16 2019-04-09 Bayer Cropscience Ag Procedimiento para la preparación de hidrocloruro de 4-cianoperidina
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
WO2018010163A1 (zh) * 2016-07-15 2018-01-18 泸州东方农化有限公司 一种1,2,4-三唑-3-硫酮化合物的合成方法及其中间体
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
WO2020221294A1 (zh) * 2019-04-30 2020-11-05 上海拓界生物医药科技有限公司 桥环-3,4-二氢-吡啶并[1,2-a]吡嗪-1,8-二酮化合物及其药物用途
CN114426540B (zh) * 2020-10-29 2024-04-26 上海拓界生物医药科技有限公司 吡啶并[1,2-a]吡嗪-1,8-二酮类前药衍生物、其制备方法及其应用
CN113372335B (zh) * 2021-07-05 2023-02-24 山东大学 一种含有1,2,4-三唑硫醚的苯丙氨酸衍生物及其制备方法与应用

Family Cites Families (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
AU2006228278C1 (en) * 2005-03-31 2011-06-23 Msd Italia S.R.L. HIV integrase inhibitors
JP4982482B2 (ja) 2005-05-10 2012-07-25 メルク・シャープ・エンド・ドーム・コーポレイション Ｈｉｖインテグラ−ゼ阻害剤

Also Published As

Publication number Publication date
EP1948666A1 (en) 2008-07-30
ES2341132T3 (es) 2010-06-15
NO20081935L (no) 2008-06-24
KR20080069254A (ko) 2008-07-25
HRP20100247T1 (hr) 2010-06-30
ATE461202T1 (de) 2010-04-15
JP2009515981A (ja) 2009-04-16
DE602006013025D1 (de) 2010-04-29
TW200738728A (en) 2007-10-16
CN101360752B (zh) 2012-09-05
EP1948666B1 (en) 2010-03-17
AU2006316582A1 (en) 2007-05-31
PT1948666E (pt) 2010-05-17
US8039458B2 (en) 2011-10-18
AR057896A1 (es) 2007-12-26
WO2007061714A1 (en) 2007-05-31
PL1948666T3 (pl) 2010-08-31
DK1948666T3 (da) 2010-05-25
SI1948666T1 (sl) 2010-06-30
CN101360752A (zh) 2009-02-04
AU2006316582B2 (en) 2012-01-19
CY1110665T1 (el) 2015-06-10
US20070111984A1 (en) 2007-05-17

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