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AR012340A1 - 3,4-DIHYDRO-2 (1H) -QUINAZOLINONES 4,4-DISSTITUTED USEFUL AS INHIBITORS OF THE REVERSE TRANSCRIPTASE OF HIV, COMPOSITION AND KITFARMACEUTICOS THAT CONTAIN THEM - Google Patents

3,4-DIHYDRO-2 (1H) -QUINAZOLINONES 4,4-DISSTITUTED USEFUL AS INHIBITORS OF THE REVERSE TRANSCRIPTASE OF HIV, COMPOSITION AND KITFARMACEUTICOS THAT CONTAIN THEM

Info

Publication number
AR012340A1
AR012340A1 ARP980101558A ARP980101558A AR012340A1 AR 012340 A1 AR012340 A1 AR 012340A1 AR P980101558 A ARP980101558 A AR P980101558A AR P980101558 A ARP980101558 A AR P980101558A AR 012340 A1 AR012340 A1 AR 012340A1
Authority
AR
Argentina
Prior art keywords
substituted
dihydro
useful
nr5r5a
reverse transcriptase
Prior art date
Application number
ARP980101558A
Other languages
Spanish (es)
Original Assignee
Du Pont
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 Du Pont filed Critical Du Pont
Publication of AR012340A1 publication Critical patent/AR012340A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/06Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/80Oxygen atoms

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Virology (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Communicable Diseases (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La presente invencion hace conocer 3,4-dihidro-2(1H)-quinazolinonas 4,4- disustituidas de la formula (I), o las formas estereoisoméricas, mezclasestereoisoméricas o sales apras para uso farmacéutico de las mismas, que son de utilidad como inhibidores de la transcriptasa inversa del HIV y concomposiciones farmacéuticas y kits de diagnostico que contienen a las mismas, donde: R1 es alquilo-C1-3 sustituido con 1-7 halogenos; R2 se selecciona dealquilo-C1-5 sustituido con 1-2 R4, alquenilo-C2-5 sustituido con 1-2 R4 y alquinilo-C2-5 sustituido con 1 R4; R3, en cada aparicion, se seleccionaindependientemente de alquilo-C1-4, OH, alcoxi-C1-4, F, Cl, Br, I, NR5R5a, NO2, CN, C(O)R6, NHC(O)R7 y NHC(O)NR5R5a, como alternativa, si hay dosR3 yestán unidos a átomos de carbono adyacentes, entonces se pueden combinar para formar -OCH2O-; R4 se selecciona de cicloalquilo-C3-5 sustituido con 0-2 R3,fenilo sustituido con 0-5 R3 y un sistema heterocíclico de 5-6 miembros que contienede 1-3 heteroátomos seleccionados entre O, N y S, sustituido con 0-2R3; R5 y R5a se seleccionan independientemente de H y alquilo C1-3; R6 se selecciona de H, OH, alquilo C1-4, alcoxi-C1-4, y NR5R5a; R7 se selecciona dealquilo C1-3 y alcoxi-C1-3; R8 se selecciona de H, cicloalquilo-C3-5 y alquilo C1-3 y n se selecciona de 0, 1, 2, 3 y 4.The present invention discloses 3,4-dihydro-2 (1H) -4,4-disubstitutedquinazolinones of formula (I), or the stereoisomeric forms, stereoisomeric mixtures or salts for pharmaceutical use thereof, which are useful as HIV reverse transcriptase inhibitors and pharmaceutical compositions and diagnostic kits containing the same, where: R1 is C1-3alkyl substituted with 1-7 halogens; R2 is selected from C1-5alkyl substituted with 1-2R4, C2-5alkenyl substituted by 1-2R4 and C2-5alkynyl substituted by 1R4; R3, at each occurrence, is independently selected from C1-4alkyl, OH, C1-4alkoxy, F, Cl, Br, I, NR5R5a, NO2, CN, C (O) R6, NHC (O) R7 and NHC (O) NR5R5a, alternatively, if there are twoR3s and they are attached to adjacent carbon atoms, then they can combine to form -OCH2O-; R4 is selected from C3-5-cycloalkyl substituted with 0-2 R3, phenyl substituted with 0-5 R3 and a 5-6 membered heterocyclic system containing 1-3 heteroatoms selected from O, N and S, substituted with 0- 2R3; R5 and R5a are independently selected from H and C1-3 alkyl; R6 is selected from H, OH, C1-4alkyl, C1-4alkoxy, and NR5R5a; R7 is selected from C1-3alkyl and C1-3alkoxy; R8 is selected from H, C3-5 cycloalkyl, and C1-3 alkyl and n is selected from 0, 1, 2, 3, and 4.

ARP980101558A 1997-04-09 1998-04-06 3,4-DIHYDRO-2 (1H) -QUINAZOLINONES 4,4-DISSTITUTED USEFUL AS INHIBITORS OF THE REVERSE TRANSCRIPTASE OF HIV, COMPOSITION AND KITFARMACEUTICOS THAT CONTAIN THEM AR012340A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US83854097A 1997-04-09 1997-04-09
US7132298P 1998-01-14 1998-01-14

Publications (1)

Publication Number Publication Date
AR012340A1 true AR012340A1 (en) 2000-10-18

Family

ID=26752095

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP980101558A AR012340A1 (en) 1997-04-09 1998-04-06 3,4-DIHYDRO-2 (1H) -QUINAZOLINONES 4,4-DISSTITUTED USEFUL AS INHIBITORS OF THE REVERSE TRANSCRIPTASE OF HIV, COMPOSITION AND KITFARMACEUTICOS THAT CONTAIN THEM

Country Status (19)

Country Link
EP (1) EP0973753A2 (en)
JP (1) JP2002504095A (en)
KR (1) KR20010006146A (en)
CN (1) CN1252063A (en)
AR (1) AR012340A1 (en)
AU (1) AU734928B2 (en)
BR (1) BR9808513A (en)
CA (1) CA2284996A1 (en)
EA (1) EA001991B1 (en)
EE (1) EE9900452A (en)
HR (1) HRP980143A2 (en)
HU (1) HUP0001446A3 (en)
IL (1) IL132188A0 (en)
NO (1) NO314936B1 (en)
NZ (1) NZ500592A (en)
PL (1) PL336305A1 (en)
SK (1) SK137899A3 (en)
TW (1) TW587078B (en)
WO (1) WO1998045276A2 (en)

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US6596729B2 (en) 2000-07-20 2003-07-22 Bristol-Myers Squibb Company Tricyclic-2-pyridone compounds useful as HIV reverse transcriptase inhibitors
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Also Published As

Publication number Publication date
AU6796098A (en) 1998-10-30
NZ500592A (en) 2001-09-28
EE9900452A (en) 2000-04-17
HUP0001446A3 (en) 2001-11-28
PL336305A1 (en) 2000-06-19
BR9808513A (en) 2000-05-23
CN1252063A (en) 2000-05-03
KR20010006146A (en) 2001-01-26
HUP0001446A2 (en) 2001-05-28
NO994904L (en) 1999-12-01
NO314936B1 (en) 2003-06-16
EA001991B1 (en) 2001-10-22
WO1998045276A2 (en) 1998-10-15
CA2284996A1 (en) 1998-10-15
NO994904D0 (en) 1999-10-08
SK137899A3 (en) 2000-05-16
EP0973753A2 (en) 2000-01-26
JP2002504095A (en) 2002-02-05
IL132188A0 (en) 2001-03-19
AU734928B2 (en) 2001-06-28
EA199900907A1 (en) 2000-04-24
TW587078B (en) 2004-05-11
WO1998045276A3 (en) 1999-01-14
HRP980143A2 (en) 1999-02-28

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