AR043271A1 - Compuestos de dihidropironas con heterociclos unidos y su uso en composicines farmaceuticas que poseen actividad inhibidora de hiv proteasa - Google Patents

Compuestos de dihidropironas con heterociclos unidos y su uso en composicines farmaceuticas que poseen actividad inhibidora de hiv proteasa

Info

Publication number
AR043271A1
AR043271A1 ARP990104528A ARP990104528A AR043271A1 AR 043271 A1 AR043271 A1 AR 043271A1 AR P990104528 A ARP990104528 A AR P990104528A AR P990104528 A ARP990104528 A AR P990104528A AR 043271 A1 AR043271 A1 AR 043271A1
Authority
AR
Argentina
Prior art keywords
nnr
branched
alkyl
straight
pnr
Prior art date
Application number
ARP990104528A
Other languages
English (en)
Inventor
Frederick E Boyer
John Michael Domagala
Edmund Lee Ellsworth
Susan Hagen
Michael James Lovdahl
Elizabeth A Lunney
Larry James Markoski
Vara Prasad Venkata Nagendra Josyula
Bradley Dean Tait
Christopher Andrew Gajda
Original Assignee
Warner Lambert 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 Warner Lambert Co filed Critical Warner Lambert Co
Publication of AR043271A1 publication Critical patent/AR043271A1/es

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • 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
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/32—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Virology (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Communicable Diseases (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Molecular Biology (AREA)
  • Public Health (AREA)
  • Oncology (AREA)
  • AIDS & HIV (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Compounds Containing Sulfur Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
  • Furan Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Indole Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

El uso de estos compuestos para la preparación de composiciones farmacéuticas, con actividad inhibitoria de HIV proteasa utilizable en combinación con AZT y otro agente retroviral en el tratamiento del SIDA. Reivindicación 1: Un compuesto de dihidropironas con heterociclos unidos, caracterizado por tener la fórmula (1), o una sal farmacológicamente aceptable de él, donde R1 es H, un alquilo recto o ramificado C1-6 o un carbociclo C3-6; R2 es H, un alquilo recto o ramificado C1-5; R3 es H, (CR'2)nOR, (CR'2)nN(R)2, (CR'2)nNR'COR, (CR'2)nCO2R, (CR'2)nOCOR, (CR'2)nCON(R)2, (CR'2)nOCON(R)2, (CR'2)nR, (CR'2)nNR'CON(R)2, (CR'2)nNR'CO2R, (CR'2)nOSO2N(R)2, (CR'2)nNR'SO2OR, (CR'2)nNR'SO2N(R)2, (CR'2)nOSO2R, (CR'2)nNR'SO2R, (CR'2)nSOpR, (CR'2)nNR'CSN(R)2, (CR'2)nNR'C(NR')N(R)2, (CR'2)nSO2N(R)2, (CR'2)nC(NR')N(R)2, (CR'2)nCOR, O(CR'2)mOR, NR(CR'2)mOR, F, Cl, Br, CF3, CF3, CN, u =O; R4, R5 y R6 son independientemente H, un alquilo recto o ramificado C1-6, un cicloalquilo C3-6, (CR'2)nOR, (CR'2)nN(R)2, F, Cl, Br. CN, CF3, (CR'2)pNR'COR, (CR'2)pSOpR, (CR'2)pR, (CR'2)pOCOR, O(CR'2)mOR, NR(CR'2)mOR, (CR'2)pNR'CON(R)2, (CR'2)pOCON(R)2, (CR'2)pNR'CO2R, (CR'2)pCOR, (CR'2)pCO2R, (CR'2)pCON(R)2, (CR'2)pNR'SO2R, (CR'2)pSO2N(R)2, (CR'2)2NR' SO2OR, (CR'2)pOSO2N(R)2, (CR'2)pNR'SO2N(R)2, (CR'2)pC(NR')N(R)2, (CR'2)pNR'C(NR')N(R)2, (CR'2)pHet; dos cualquiera de R1-R3 o R4-R6 pueden formar juntos un anillo de 5 a 6 átomos totales que pueden contener de 0 a 3 heteroátomos; n es un número entero de 0 a 3; m es un número entro de 2 a 4; p es un número entero de 0 a 2; R7 es un alquilo recto o ramificado C1-6 o un carbociclo C3-6; R es independientemente H, un alquilo recto o ramificado C1-4, (CH)2nPh, o un heterociclo (CH2)n de 5 a 6 átomos que contienen de 1 a 2 heteroátomos y donde el (R)2 en N(R)2 puede formar un heterociclo que contiene el nitrógeno, todos optativamente sustituidos por F, Cl, Br, OR', CN, CO2R', N(R')2, NR'COR', CF3, u =O; R' es independientemente H, un alquilo recto o ramificado C1-4, o fenilo; R'' es independientemente H, un alquilo recto o ramificado C1-4, F, Cl, Br, OR', o N(R')2; Ar1 y Ar2 son independientemente fenilo o Het con la salvedad de que al menos un Ar es Het; Het es un heterociclo de 5 a 6 átomos que tienen de 1 a 4 heteroátomos o un heterociclo fusionado de 9 a 10 átomos que tienen de 1 a 3 heteroátomos.
ARP990104528A 1998-09-11 1999-09-09 Compuestos de dihidropironas con heterociclos unidos y su uso en composicines farmaceuticas que poseen actividad inhibidora de hiv proteasa AR043271A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US9994698P 1998-09-11 1998-09-11

Publications (1)

Publication Number Publication Date
AR043271A1 true AR043271A1 (es) 2005-07-27

Family

ID=22277357

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP990104528A AR043271A1 (es) 1998-09-11 1999-09-09 Compuestos de dihidropironas con heterociclos unidos y su uso en composicines farmaceuticas que poseen actividad inhibidora de hiv proteasa

Country Status (13)

Country Link
US (3) US6528510B1 (es)
EP (1) EP1112269A2 (es)
JP (1) JP2002524560A (es)
KR (1) KR20010085780A (es)
AR (1) AR043271A1 (es)
AU (2) AU773567B2 (es)
BR (1) BR9913598A (es)
CA (1) CA2339275A1 (es)
NZ (1) NZ510013A (es)
PE (1) PE20001052A1 (es)
UY (1) UY25708A1 (es)
WO (1) WO2000015634A2 (es)
ZA (1) ZA200100806B (es)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR9913598A (pt) * 1998-09-11 2001-05-29 Warner Lambert Co Inibidores de protease de hiv
WO2003091230A1 (en) * 2002-04-26 2003-11-06 Orchid Chemicals & Pharmaceuticals Limited Process for the preparation of 4-methyl-thiazole-5-carbaldehyde intermediate
DOP2003000641A (es) * 2002-05-10 2003-11-15 Pfizer Inhibidores de las arn polimerasa dependiente de arn del virus de las hepatitis c y composiciones y tratamiento que los usan
US7148226B2 (en) * 2003-02-21 2006-12-12 Agouron Pharmaceuticals, Inc. Inhibitors of hepatitis C virus RNA-dependent RNA polymerase, and compositions and treatments using the same
GEP20115305B (en) * 2004-08-18 2011-10-10 Pfizer Inhibitors of hepatitis c virus rna-dependent rna polymerase, compositions containing them and using the same for treatment
PA8792501A1 (es) * 2007-08-09 2009-04-23 Sanofi Aventis Nuevos derivados de 6-triazolopiridacina-sulfanil benzotiazol y bencimidazol,su procedimiento de preparación,su aplicación como medicamentos,composiciones farmacéuticas y nueva utilización principalmente como inhibidores de met.
US20100292232A1 (en) * 2007-11-09 2010-11-18 Daniel Elleder Non-nucleoside reverse transcriptase inhibitors
CN101903367B (zh) 2007-12-20 2015-08-05 法马马有限公司 抗肿瘤化合物
FR2933982A1 (fr) * 2008-07-18 2010-01-22 Sanofi Aventis Nouveaux derives imidazo°1,2-a!pyrimidine, leur procede de preparation, leur application a titre de medicaments, compositions pharmaceutiques et nouvelle utilisation notamment comme inhibiteurs de met

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3786063A (en) * 1971-05-24 1974-01-15 Universal Oil Prod Co Thiazolethiosulfonates
ES2176263T3 (es) * 1993-11-19 2002-12-01 Parke Davis & Co 5,6-dihidropironas derivadas como inhibidores de proteasa y agentes antivirus.
US5840751A (en) * 1993-11-19 1998-11-24 Warner-Lambert Company 5,6-dihydropyrone derivatives as protease inhibitors and antiviral agents
NZ275961A (en) * 1993-11-19 2001-11-30 Parke Davis & Co 5,6-dihydropyrone derivatives and pharmaceutical compositions as anti-viral agents in the treatment of HIV infection
US5834506A (en) * 1996-11-01 1998-11-10 Warner-Lambert Company Dihydropyrones with improved antiviral activity
BR9913598A (pt) * 1998-09-11 2001-05-29 Warner Lambert Co Inibidores de protease de hiv

Also Published As

Publication number Publication date
BR9913598A (pt) 2001-05-29
NZ510013A (en) 2003-11-28
KR20010085780A (ko) 2001-09-07
EP1112269A2 (en) 2001-07-04
US20040106606A1 (en) 2004-06-03
UY25708A1 (es) 1999-11-17
ZA200100806B (en) 2002-01-29
US20050075390A1 (en) 2005-04-07
WO2000015634A3 (en) 2000-11-16
AU5780299A (en) 2000-04-03
AU2004205322A1 (en) 2004-09-23
CA2339275A1 (en) 2000-03-23
US6528510B1 (en) 2003-03-04
PE20001052A1 (es) 2000-10-18
US6852711B2 (en) 2005-02-08
JP2002524560A (ja) 2002-08-06
AU773567B2 (en) 2004-05-27
WO2000015634A2 (en) 2000-03-23

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