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AR049498A1 - Inhibidores de integrasa del virus de inmunodeficiencia humana: compuestos de pirimidinona ciclica - Google Patents

Inhibidores de integrasa del virus de inmunodeficiencia humana: compuestos de pirimidinona ciclica

Info

Publication number
AR049498A1
AR049498A1 ARP050101931A ARP050101931A AR049498A1 AR 049498 A1 AR049498 A1 AR 049498A1 AR P050101931 A ARP050101931 A AR P050101931A AR P050101931 A ARP050101931 A AR P050101931A AR 049498 A1 AR049498 A1 AR 049498A1
Authority
AR
Argentina
Prior art keywords
alkyl
ch2ch2
ch2n
ch2ch2ch2
halo
Prior art date
Application number
ARP050101931A
Other languages
English (en)
Inventor
B Narasimhulu Naidu
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 AR049498A1 publication Critical patent/AR049498A1/es

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • 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
    • C07D487/10Spiro-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
    • A61K31/495Heterocyclic 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
    • A61K31/527Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim spiro-condensed
    • 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
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/10Spiro-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • 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
    • C07D498/10Spiro-condensed systems

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  • 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)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (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)

Abstract

Una serie de compuestos de pirimidinona que inhiben la integrasa del VIH y con lo cual impiden la integracion viral en el ADN humano. Esta accion hace a los compuestos utiles para el tratamiento de la infeccion por el VIH y el SIDA. También productos intermediarios que son utiles para la elaboracion de los compuestos de pirimidona. Adicionalmente, están incluidas las composiciones farmacéuticas y los métodos para el tratamiento de aquellos infectados con el VIH. Reivindicacion 1: Un compuesto caracterizado porque tiene la formula (1) en donde: R1 es (Ar1)alquilo C1-6; R2 es H, alquilo C1-6 u OR6; R3 es H, halo, hidroxi, ciano, alquilo C1-6, cicloalquilo C3-7, haloalquilo C1-6, alcoxi C1-6, alquiltio C1-6, haloalcoxi C1-6, CON(R6)(R6), SOR7, SO2R7, SO2N(R6)(R6) o Ar2; R4 es H, halo, hidroxi, ciano, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6 o haloalcoxi C1-6; R5 es H, halo, hidroxi, ciano, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6 o haloalcoxi C1-6; R6 es H o alquilo C1-6; R7 es alquilo C1-6; R8 y R9, tomados conjuntamente, son CH2CH2, CH2CH2CH2, CH2CH2CH2CH2, CH2CH2CH2CH2CH2, CH2CH2CH2CH2CH2CH2, OCH2CH2, CH2OCH2, OCH2CH2CH2, CH2OCH2CH2, OCH2CH2CH2CH2, CH2OCH2CH2CH2, CH2CH2OCH2CH2, OCH2CH2CH2CH2CH2, CH2OH2CH2CH2CH2, CH2CH2OH2CH2CH2, N(R6)CH2CH2, CH2N(R6)CH2, N(R6)CH2CH2CH2, CH2N(R6)CH2CH2, N(R6)CH2CH2CH2CH2, CH2N(R6)CH2CH2CH2, CH2CH2N(R6)CH2CH2, N(R6)CH2CH2CH2CH2CH2, CH2N(R6)CH2CH2CH2CH2 o CH2CH2N(R6)CH2CH2CH2; o Ar1 es un resto de formula (2); Ar2 es tetrazolilo, triazolilo, imidazolilo, pirazolilo, pirrolilo o dioxotiazinilo y es sustituido por 0-2 sustituyentes seleccionados del grupo que consiste de amino, oxo, halo, ciano y alquilo C1-6, y X-Y-Z es C(R8)(R9)CH2CH2, C(R8)(R9)CH2CH2CH2, C(R8)(R9)CH2CH2CH2CH2, C(R8)(R9)OCH2, C(R8)(R9)OCH2CH2 o C(R8)(R9)OCH2CH2CH2; o una sal o solvato farmacéuticamente aceptable del mismo.
ARP050101931A 2004-05-12 2005-05-11 Inhibidores de integrasa del virus de inmunodeficiencia humana: compuestos de pirimidinona ciclica AR049498A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US57034804P 2004-05-12 2004-05-12

Publications (1)

Publication Number Publication Date
AR049498A1 true AR049498A1 (es) 2006-08-09

Family

ID=34967012

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050101931A AR049498A1 (es) 2004-05-12 2005-05-11 Inhibidores de integrasa del virus de inmunodeficiencia humana: compuestos de pirimidinona ciclica

Country Status (26)

Country Link
US (2) US7273859B2 (es)
EP (1) EP1745052B9 (es)
JP (1) JP2007537251A (es)
KR (1) KR20070014173A (es)
CN (1) CN1984917A (es)
AR (1) AR049498A1 (es)
AT (1) ATE405570T1 (es)
AU (1) AU2005245789A1 (es)
BR (1) BRPI0511078A (es)
CA (1) CA2566755A1 (es)
DE (1) DE602005009172D1 (es)
DK (1) DK1745052T3 (es)
ES (1) ES2310823T3 (es)
HR (1) HRP20080531T3 (es)
IL (1) IL179161A0 (es)
MX (1) MXPA06013023A (es)
NO (1) NO20065443L (es)
NZ (1) NZ550698A (es)
PE (1) PE20060238A1 (es)
PL (1) PL1745052T3 (es)
PT (1) PT1745052E (es)
RU (1) RU2006143683A (es)
SI (1) SI1745052T1 (es)
TW (1) TW200540173A (es)
WO (1) WO2005113562A1 (es)
ZA (1) ZA200609181B (es)

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Also Published As

Publication number Publication date
IL179161A0 (en) 2007-03-08
US20060106007A1 (en) 2006-05-18
PL1745052T3 (pl) 2009-01-30
ZA200609181B (en) 2008-06-25
EP1745052A1 (en) 2007-01-24
TW200540173A (en) 2005-12-16
NO20065443L (no) 2006-11-27
ATE405570T1 (de) 2008-09-15
CN1984917A (zh) 2007-06-20
DK1745052T3 (da) 2009-01-05
DE602005009172D1 (de) 2008-10-02
AU2005245789A1 (en) 2005-12-01
US7273859B2 (en) 2007-09-25
ES2310823T3 (es) 2009-01-16
WO2005113562A1 (en) 2005-12-01
JP2007537251A (ja) 2007-12-20
US20050256109A1 (en) 2005-11-17
US7419969B2 (en) 2008-09-02
PT1745052E (pt) 2008-11-14
EP1745052B9 (en) 2009-10-28
MXPA06013023A (es) 2006-12-20
HRP20080531T3 (en) 2009-03-31
BRPI0511078A (pt) 2007-12-26
NZ550698A (en) 2009-05-31
RU2006143683A (ru) 2008-06-20
EP1745052B1 (en) 2008-08-20
PE20060238A1 (es) 2006-03-31
KR20070014173A (ko) 2007-01-31
CA2566755A1 (en) 2005-12-01
SI1745052T1 (sl) 2009-04-30

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