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AR037770A1 - Compuesto inhibidor de la integrasa del vih, composicion farmaceutica que lo comprende y uso del mismo para prepararla - Google Patents

Compuesto inhibidor de la integrasa del vih, composicion farmaceutica que lo comprende y uso del mismo para prepararla

Info

Publication number
AR037770A1
AR037770A1 ARP020104777A ARP020104777A AR037770A1 AR 037770 A1 AR037770 A1 AR 037770A1 AR P020104777 A ARP020104777 A AR P020104777A AR P020104777 A ARP020104777 A AR P020104777A AR 037770 A1 AR037770 A1 AR 037770A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
heteroaryl
independently selected
co2r5
Prior art date
Application number
ARP020104777A
Other languages
English (en)
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 AR037770A1 publication Critical patent/AR037770A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C207/00Compounds containing nitroso groups bound to a carbon skeleton
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C207/00Compounds containing nitroso groups bound to a carbon skeleton
    • C07C207/04Compounds containing nitroso groups bound to a carbon skeleton the carbon skeleton being further substituted by singly-bound oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C239/00Compounds containing nitrogen-to-halogen bonds; Hydroxylamino compounds or ethers or esters thereof
    • C07C239/08Hydroxylamino compounds or their ethers or esters
    • C07C239/20Hydroxylamino compounds or their ethers or esters having oxygen atoms of hydroxylamino groups etherified
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/32Oximes
    • C07C251/34Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals
    • C07C251/48Oximes with oxygen atoms of oxyimino groups bound to hydrogen atoms or to carbon atoms of unsubstituted hydrocarbon radicals with the carbon atom of at least one of the oxyimino groups bound to a carbon atom of a six-membered aromatic ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/63Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C255/64Carboxylic acid nitriles containing cyano groups and nitrogen atoms further bound to other hetero atoms, other than oxygen atoms of nitro or nitroso groups, bound to the same carbon skeleton with the nitrogen atoms further bound to oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C259/00Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups
    • C07C259/04Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids
    • C07C259/06Compounds containing carboxyl groups, an oxygen atom of a carboxyl group being replaced by a nitrogen atom, this nitrogen atom being further bound to an oxygen atom and not being part of nitro or nitroso groups without replacement of the other oxygen atom of the carboxyl group, e.g. hydroxamic acids having carbon atoms of hydroxamic groups bound to hydrogen atoms or to acyclic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/16Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms
    • C07D295/18Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182Radicals derived from carboxylic acids
    • C07D295/185Radicals derived from carboxylic acids from aliphatic carboxylic acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D317/00Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/32Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D317/34Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/02Systems containing only non-condensed rings with a three-membered ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00Systems containing only non-condensed rings
    • C07C2601/12Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14The ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Virology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Epidemiology (AREA)
  • Communicable Diseases (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Engineering & Computer Science (AREA)
  • Oncology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Material From Animals Or Micro-Organisms (AREA)

Abstract

Una composición farmacéutica útil para el tratamiento de infecciones por VIH, que comprende una cantidad terapéutica del compuesto de la fórmula (1) y un portador farmacéuticamente aceptable, la cual puede comprender además una cantidad terapéuticamente efectiva de uno o más de otros agentes para el tratamiento del VIH. Uso de un compuesto de la fórmula (1) o una sal o solvato farmacéuticamente aceptable del mismo, para preparar una composición farmacéutica para inhibir la integrasa de VIH o para aplicar en el tratamiento de una infección por VIH. Reivindicación 1: Un compuesto de la fórmula (1), en donde: R1 es arilo, alquilo C1-6-arilo, alquilo C1-6-S(O)n-arilo, alquilo C1-5-O-arilo; o y en donde R1 está sin sustituir o sustituido independientemente con 1-3 R3; cada R3 se selecciona independientemente de H, halo, CN, alquilo C1-6, cicloalquilo C3-6, -OR4, alquilo C1-10-O-R4, -CO2R5, alquilo C1-10-CO2R5, N(R6)(R7), alquilo C1-10-N(R6)(R7), CON(R6)(R7), alquilo C1-10-CON(R6)(R7), -S(O)nR8, alquilo C1-10-S-(O)nR8, -S(O)n(R9)(R10), alquilo C1-10-S(O)nN(R9)(R10), arilo, -O-arilo, heteroarilo, -O-heteroarilo, alquilo C1-6-arilo, alquilo C1-6-heteroarilo, radical-C(O)-heterocíclico, radical alquilo C1-10-C(O)-heterocíclico, o haloalquilo C1-6; R2 es H, alquilo C1-10, cicloalquilo C3-6, haloalquilo C1-10, arilo, heteroarilo, alquilo C1-6-arilo, alquilo C1-5-O-arilo, alquilo C1-6-heteroarilo, alquilo C1-5-O-heteroarilo, alquilo C1-10-OR4, alquilo C1-10-CO2R5, alquilo C1-10-N(R6)(R7), alquilo C1-10-CON(R6)(R7), alquilo C1-10-S(O)nR8, alquilo C1-10-S(O)nN(R9)(R10), o radical alquilo C1-10-C(O)-heterocíclico; cada R4 se selecciona independientemente de H, alquilo C1-6, cicloalquilo C3-6, alquilo C1-9-CO2R5, alquilo C1-9-N(R6)(R7), alquilo C1-9-CON(R6)(R7), alquilo C1-9-S(O)nR8, o alquilo C1-9-S(O)nN(R9)(R10); cada R5 se selecciona independientemente de H, alquilo C1-6, cicloalquilo C3-6, o alquilo C1-6-arilo; cada R6 se selecciona independientemente de H, alquilo C1-6, arilo, heteroarilo, alquilo C1-6-arilo, alquilo C1-6-heteroarilo, -C(O)-alquiloC1-6, -C(O)-arilo, -C(O)-alquilo C1-6-arilo, -C(O)-heteroarilo, -C(O)-alquilo C1-6-heteroarilo, -C(NH)NH2, -S(O)n-R8, o alquilo C1-6-CO2R5; cada R7 se selecciona independientemente de H, alquilo C1-6, arilo o heteroarilo; cada R8 se selecciona independientemente de alquilo C1-6, arilo o heteroarilo; cada R9 se selecciona independientemente de H, alquilo C1-6, alquilo C1-6-arilo, alquilo C1-6-heteroarilo, -C(O)-alquilo C1-6, -C(O)-arilo, -C(O)-alquilo C1-6-arilo, -C(O)-alquilo C1-6-heteroarilo, arilo, o heteroarilo; cada R10 se selecciona independientemente de H, alquilo C1-6, alquilo C1-6-arilo, alquilo C1-6-heteroarilo, arilo o heteroarilo; R11 es H, arilo, heteroarilo, alquilo C1-6-heteroarilo, cicloalquilo C3-6, alquilo C1-6, alquilo C1-6-arilo, alquilo C1-6-CO2R5, o alquilo C1-6-N(R6)(R7); R12 es H, alquilo C1-6, arilo o heteroarilo; R13 es H, alquilo C1-6, arilo, o heteroarilo; B1 se selecciona del grupo de fórmulas (2) y n es 0, 1 ó 2; o una sal o solvato farmacéuticamente aceptable del mismo.
ARP020104777A 2001-12-12 2002-12-10 Compuesto inhibidor de la integrasa del vih, composicion farmaceutica que lo comprende y uso del mismo para prepararla AR037770A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US33967401P 2001-12-12 2001-12-12

Publications (1)

Publication Number Publication Date
AR037770A1 true AR037770A1 (es) 2004-12-01

Family

ID=23330105

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP020104777A AR037770A1 (es) 2001-12-12 2002-12-10 Compuesto inhibidor de la integrasa del vih, composicion farmaceutica que lo comprende y uso del mismo para prepararla

Country Status (24)

Country Link
US (1) US6777440B2 (es)
EP (1) EP1467695A2 (es)
JP (1) JP2005515206A (es)
KR (1) KR20040065251A (es)
CN (1) CN1617849A (es)
AR (1) AR037770A1 (es)
AU (1) AU2002366604A1 (es)
BR (1) BR0214842A (es)
CA (1) CA2469592C (es)
CO (1) CO5590909A2 (es)
HR (1) HRP20040534A2 (es)
HU (1) HUP0402675A2 (es)
IL (1) IL162325A0 (es)
IS (1) IS7305A (es)
MX (1) MXPA04005623A (es)
NO (1) NO20042916L (es)
NZ (1) NZ533413A (es)
PE (1) PE20030763A1 (es)
PL (1) PL370664A1 (es)
RU (1) RU2284315C2 (es)
TW (1) TWI252757B (es)
UY (1) UY27577A1 (es)
WO (1) WO2003049690A2 (es)
ZA (1) ZA200404628B (es)

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US7169932B2 (en) 2001-06-11 2007-01-30 Pfizer Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses, material for their synthesis
US7094909B2 (en) 2001-06-11 2006-08-22 Agouron Pharmaceuticals, Inc. HIV protease inhibitors, compositions containing the same, their pharmaceutical uses and materials for their synthesis
HN2002000136A (es) 2001-06-11 2003-07-31 Basf Ag Inhibidores de la proteasa del virus hiv, compuestos que contienen a los mismos, sus usos farmaceuticos y los materiales para su sintesis
PA8586801A1 (es) 2002-10-31 2005-02-04 Pfizer Inhibidores de hiv-integrasa, composiciones farmaceuticas y metodos para su uso
BRPI0407052A (pt) 2003-01-27 2006-01-17 Pfizer Inibidores da hiv-integrase, composições farmacêuticas, e métodos para sua utilização
US6890942B2 (en) * 2003-05-16 2005-05-10 Bristol-Myers Squibb Company Acyl sulfonamides as inhibitors of HIV integrase
US20050215544A1 (en) * 2004-03-24 2005-09-29 Pin-Fang Lin Methods of treating HIV infection
US7776863B2 (en) * 2004-03-24 2010-08-17 Bristol-Myers Squibb Company Methods of treating HIV infection
EP1751157B1 (en) 2004-04-26 2007-10-03 Pfizer Inc. Inhibitors of the hiv integrase enzyme
CA2564356A1 (en) 2004-04-26 2005-11-03 Pfizer Inc. Pyrrolopyridine derivatives and their use as hiv-integrase inhibitors
US7507838B2 (en) * 2004-09-01 2009-03-24 Bristol-Myers Squibb Company Process for the preparation of Z-5-carboxymethylene-1,3-dioxolan-4-ones
US20060058286A1 (en) * 2004-09-16 2006-03-16 Mark Krystal Methods of treating HIV infection
WO2007086584A1 (ja) * 2006-01-30 2007-08-02 Meiji Seika Kaisha, Ltd. 新規FabKおよびFabI/K阻害剤
WO2008004100A2 (en) 2006-07-05 2008-01-10 Pfizer Products Inc. Therapeutic compounds
SI2364293T1 (sl) * 2008-12-05 2013-05-31 Syngenta Participations Ag Novi pirazol-4-N-alkoksikarboksamidi kot mikrobiocidi
SG10201408512RA (en) 2009-12-23 2015-02-27 Univ Leuven Kath Novel antiviral compounds
US8283366B2 (en) 2010-01-22 2012-10-09 Ambrilia Biopharma, Inc. Derivatives of pyridoxine for inhibiting HIV integrase
WO2012066442A1 (en) 2010-11-15 2012-05-24 Pfizer Limited Inhibitors of hiv replication
BR112013011737A2 (pt) 2010-11-15 2016-08-09 Univ Leuven Kath composto, uso de um composto composição farmacêutica, e, método de tratamento ou prevenção de uma infecção por hiv
IN2014DN09934A (es) * 2012-04-26 2015-08-14 Bayer Cropscience Ag

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Publication number Priority date Publication date Assignee Title
EP1082121A4 (en) * 1998-06-03 2003-02-05 Merck & Co Inc HIV integrase
US6380249B1 (en) * 1998-06-03 2002-04-30 Merck & Co., Inc. HIV integrase inhibitors
AR029304A1 (es) * 1998-06-26 2003-06-25 Daiichi Seiyaku Co DERIVADOS DE PROPIONILO SUSTITUIDOS, PRODUCTO FARMACEUTICO, USO PARA LA FABRICACION DE UNA COMPOSICION FARMACEUTICA PARA LA PREVENCION Y/O TRATAMIENTO DE HIPERCOLESTEROLEMIA, HIPERLIPEMIA O ARTERIOESCLEROSIS, COMPOSICIoN FARMACÉUTICA Y COMPUESTOS INTERMEDIARIOS

Also Published As

Publication number Publication date
RU2284315C2 (ru) 2006-09-27
PL370664A1 (en) 2005-05-30
WO2003049690A3 (en) 2004-01-22
WO2003049690A2 (en) 2003-06-19
BR0214842A (pt) 2005-01-11
EP1467695A2 (en) 2004-10-20
NO20042916L (no) 2004-09-10
HUP0402675A2 (hu) 2005-03-29
CO5590909A2 (es) 2005-12-30
RU2004119963A (ru) 2006-01-10
UY27577A1 (es) 2003-07-31
NZ533413A (en) 2006-09-29
JP2005515206A (ja) 2005-05-26
MXPA04005623A (es) 2004-12-06
AU2002366604A1 (en) 2003-06-23
CA2469592A1 (en) 2003-06-19
PE20030763A1 (es) 2003-09-13
US20030176495A1 (en) 2003-09-18
TWI252757B (en) 2006-04-11
KR20040065251A (ko) 2004-07-21
IS7305A (is) 2004-06-10
US6777440B2 (en) 2004-08-17
TW200301105A (en) 2003-07-01
ZA200404628B (en) 2005-09-01
IL162325A0 (en) 2005-11-20
HRP20040534A2 (en) 2005-04-30
CA2469592C (en) 2005-08-23
CN1617849A (zh) 2005-05-18

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