AR057455A1 - Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica - Google Patents

Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica

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Publication number
AR057455A1
AR057455A1 ARP060102994A ARP060102994A AR057455A1 AR 057455 A1 AR057455 A1 AR 057455A1 AR P060102994 A ARP060102994 A AR P060102994A AR P060102994 A ARP060102994 A AR P060102994A AR 057455 A1 AR057455 A1 AR 057455A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
nr3r4
optionally
fluoroalkyl
Prior art date
Application number
ARP060102994A
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English (en)
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Merck & Co Inc
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Publication date
Application filed by Merck & Co Inc filed Critical Merck & Co Inc
Publication of AR057455A1 publication Critical patent/AR057455A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/30—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45—Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups at least one of the singly-bound nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfonamides
    • C07C311/46—Y being a hydrogen or a carbon atom
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/54—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and etherified hydroxy groups bound to the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00—Carboxylic acid nitriles
    • C07C255/49—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton
    • C07C255/60—Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton containing cyano groups and singly-bound nitrogen atoms, not being further bound to other hetero atoms, bound to the carbon skeleton at least one of the singly-bound nitrogen atoms being acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00—Amides of sulfuric acids, i.e. compounds having singly-bound oxygen atoms of sulfate groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C307/04—Diamides of sulfuric acids
    • C07C307/06—Diamides of sulfuric acids having nitrogen atoms of the sulfamide groups bound to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00—Sulfones; Sulfoxides
    • C07C317/26—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C07C317/34—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring
    • C07C317/38—Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton with sulfone or sulfoxide groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton having sulfone or sulfoxide groups and amino groups bound to carbon atoms of six-membered aromatic rings being part of the same non-condensed ring or of a condensed ring system containing that ring with the nitrogen atom of at least one amino group being part of any of the groups, X being a hetero atom, Y being any atom, e.g. N-acylaminosulfones
    • C07C317/40—Y being a hydrogen or a carbon atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/08—Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/62—Oxygen or sulfur atoms
    • C07D213/63—One oxygen atom
    • C07D213/65—One oxygen atom attached in position 3 or 5
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom 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
    • C07D213/72—Nitrogen atoms
    • C07D213/75—Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04—Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06—Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D249/00—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/06—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/56—Benzoxazoles; Hydrogenated benzoxazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/10—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
    • C07D271/107—1,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles with two aryl or substituted aryl radicals attached in positions 2 and 5
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/64—Benzothiazoles with only hydrocarbon or substituted hydrocarbon radicals attached in position 2
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/46—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom
    • C07D333/48—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings substituted on the ring sulfur atom by oxygen atoms
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
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    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/12—Systems containing only non-condensed rings with a six-membered ring
    • C07C2601/14—The ring being saturated

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  • 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)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Engineering & Computer Science (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Molecular Biology (AREA)
  • AIDS & HIV (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Indole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Estos compuestos son inhibidores de transcriptasa reversa de VIH. Los compuestos y sus sales farmacéuticamente aceptables son utiles en la inhibicion de transcriptasa reversa de VIH, la profilaxis y tratamiento de la infeccion mediante VIH y en la profilaxis, retraso en la aparicion, y tratamiento de SIDA. Los compuestos y sus sales se pueden emplear como ingredientes en composiciones farmacéuticas, opcionalmente en combinacion con otros antivirales, inmunomoduladores, antibioticos o vacunas. Reivindicacion 1: Un compuesto de formula (1), o una sal farmacéuticamente aceptable del mismo, en la que: R1 y R2 se seleccionan independientemente del grupo constituido por: a) H, b) alquilo C1-6, c) cicloalquilo C3-6, d) fluoroalquilo C1-3, e) NO2, f) halogeno, g) OR3, h) O(CH2)sOR3, i) CO2R3, j) (CO)NR3R4, k) O(CO)NR3R4, 1) N(R3)(CO)NR3R4. m) N(R3)(CO)R4, n) N(R3)(CO)OR3, o) SO2NR3R4. p) N(R3)SO2R4, q) S(O)mR3, r) CN, s) NR3R4, t) N(R3)(CO)NR3R4, y u) O(CO)R3; A es arilo, cicloalquilo C3-7, o heterociclilo; V es -C(R5R6)-; X se selecciona del grupo constituido por -O-, -NH-, y -C(R5R6)-; Y se selecciona del grupo constituido por de -O-, -C(R5R6)-, y -S(O)m-; R5 y R6 se seleccionan independientemente del grupo constituido por hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y OR3; R10 es un heterociclilo seleccionado del grupo constituido por las formulas (2) a (28), donde R12 y R13 se seleccionan independientemente del grupo constituido por hidrogeno, halogeno, oxo, NO2, CN, OR3, O(CH2)tCF3, CO2R3, CONR3R4, O(CH2)tNR3R4, O(CH2)vCOR3, S(O)mR3, SO2NR3R4, alquilo C1-6, fluoroalquilo C1-3, cicloalquilo C3-6, y NR3R4; R3 y R4 se seleccionan independientemente del grupo constituido por hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y cicloalquilo C3-6; o, alternativamente y opcionalmente, cuando R3 y R4 están en un grupo NR3R4, entonces: A) uno de R3 y R4 se selecciona del grupo que consta de hidrogeno, alquilo C1-6, fluoroalquilo C1-3, y cicloalquilo C3-6, y el otro R3 y R4 es alquilo Cl-6 sustituido con O-alquiloC1-6, C(O)RA, CO2RA, C(O)N(RA)RB; o (B) R3 y R4 conjuntamente con átomo de nitrogeno al cual se unen formando: i) una anillo monocíclico saturado o insaturado de 4-7 miembros que contienen opcionalmente 1 o 2 heteroátomos además del nitrogeno unidos a R3 y R4 seleccionados de N, O, y S, donde la S se oxida opcionalmente a S(O) o S(O)2, o ii) un sistema anillo bicíclico de 7 a 12-miembros en el que cada anillo en ii) es independiente de, está fusionado a, o unido mediante puente con el otro anillo y cada anillo estará saturado o insaturado, y en el que sistema de anillo bicíclico contiene opcionalmente de 1 a 3 heteroátomos además del nitrogeno unido a R3 y R4 seleccionados de N, O, y S, donde la S se oxida opcionalmente a S(O) o S(O)2, y en el que el anillo monocíclico del sistema anillo bicíclico está sustituido opcionalmente con de 1 a 3 sustituyentes cada uno de los cuales es independientemente: alquilo C1-6; haloalquilo C1-6, alquilo C1-6 sustituido con OH, O-alquilC1-6, O-haloalquilC1-6, CN, NO2, N(RA)RB, C(O)N(RA)RB, C(O)RA, CO2RA, SRA, S(O)RA SO2RA, o SO2N(RA)RB; O-alquilC1-6; O-haloalquilC1-6; OH; oxo; halogeno; CN; N02; N(RA)RB; C(O)N(RA)RB; C(O)RA; C(O)- haloalquilC1-6; C(O)ORA; OC(O)N(RA)RB; SRA; S(O)RA; S(O)2RA; S(O)2N(RA)RB; N(RA)CORB; o N(RA)SO2RB y en el que cada RA es independientemente H o alquilo C1-6, y cada RB es independientemente H o alquilo 1-6; HetA es heteroarilo seleccionado del grupo constituido por piridinilo, pirimidinilo, y pirazinilo; s es 1-5; t es 2-3; v es 1-2; y m, en cada caso en el cual aparece, se selecciona independientemente de 0-2; y siempre que cuando X es -C(R5R6)-, entonces ni R1 ni R2 es OR3.
ARP060102994A 2005-07-22 2006-07-12 Inhibidores de la transcriptasa reversa de vih y composicion farmaceutica AR057455A1 (es)

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US70179705P 2005-07-22 2005-07-22
US72791605P 2005-10-18 2005-10-18
US79070506P 2006-04-10 2006-04-10

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AR057455A1 true AR057455A1 (es) 2007-12-05

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US (1) US7807684B2 (es)
EP (2) EP1912935A2 (es)
JP (1) JP5075821B2 (es)
KR (1) KR20080039379A (es)
AR (1) AR057455A1 (es)
AT (1) ATE459624T1 (es)
AU (1) AU2006276231B2 (es)
CA (1) CA2615019C (es)
CR (1) CR9694A (es)
DE (1) DE602006012683D1 (es)
IL (1) IL188615A0 (es)
MA (1) MA29745B1 (es)
MX (1) MX2008000959A (es)
NO (1) NO20080913L (es)
PE (1) PE20070243A1 (es)
TW (1) TW200738702A (es)
WO (2) WO2007015812A2 (es)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CL2007002105A1 (es) * 2006-07-21 2008-02-22 Hoffmann La Roche Compuestos derivados de 2-[3-(3-cianofenoxi)(fenoxi o fenilsulfanil)]-n-fenil acetamida, inhibidores de la transcriptasa inversa del vih; procedimiento de preparacion; composicion farmaceutica que comprende a dichos compuestos; y su uso para tratar u
EP2057125B1 (en) * 2006-08-16 2011-03-30 F. Hoffmann-La Roche AG Non-nucleoside reverse transcriptase inhibitors
TW200831085A (en) * 2006-12-13 2008-08-01 Merck & Co Inc Non-nucleoside reverse transcriptase inhibitors
WO2009008906A2 (en) * 2007-02-06 2009-01-15 The Trustees Of The University Of Pennsylvania Therapeutic compounds for blocking dna synthesis of pox viruses
CN101679414A (zh) * 2007-04-09 2010-03-24 弗·哈夫曼-拉罗切有限公司 非核苷逆转录酶抑制剂
CA2687747C (en) * 2007-05-30 2015-11-17 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
CL2008001631A1 (es) * 2007-06-06 2009-01-02 Smithkline Beecham Corp Compuestos derivados de heterociclos sustituidos, con la presencia de un grupo fenoxi, inhibidores de transcriptasa inversa; composicion farmaceutica; y uso en el tratamiento de infecciones virales por vih.
MX2009013865A (es) * 2007-06-22 2010-01-27 Hoffmann La Roche Urea y derivados carbamato como inhibidores no nucleosidicos de la transcriptasa inversa.
MX2010001636A (es) * 2007-08-14 2010-03-15 Hoffmann La Roche Derivados de pirazolo[3,4-d]-pirimidina como agentes antiproliferativos.
KR20100088142A (ko) * 2007-11-20 2010-08-06 머크 샤프 앤드 돔 코포레이션 비-뉴클레오사이드 역전사효소 억제제
EP2225239B1 (en) * 2007-12-21 2014-10-22 F. Hoffmann-La Roche AG Heterocyclic antiviral compounds
WO2009117278A2 (en) * 2008-03-20 2009-09-24 Merck & Co., Inc. Processes for preparing (amino-pyrazolopyridinyl)methoxy substituted biaryl ethers
EP2408753A4 (en) * 2009-03-20 2012-11-07 Univ Brandeis COMPOUNDS AND METHOD FOR THE TREATMENT OF MICROBIAL STOMACH DARM INFECTIONS IN MAMMALS
US20120232062A1 (en) * 2009-10-20 2012-09-13 Eiger Biopharmaceuticals, Inc. Azaindazoles to treat flaviviridae virus infection
EP2516437B1 (en) 2009-12-21 2014-01-29 Novartis AG Disubstituted heteroaryl-fused pyridines
PL2924034T3 (pl) 2010-03-30 2017-07-31 Merck Canada Inc. Kompozycja farmaceutyczna zawierająca nienukleozydowy inhibitor odwrotnej transkryptazy
CN103517990A (zh) 2010-10-07 2014-01-15 通用医疗公司 癌症生物标志物
US20120142627A1 (en) * 2010-12-06 2012-06-07 Emory University Monophosphate prodrugs of dapd and analogs thereof
JO3470B1 (ar) 2012-10-08 2020-07-05 Merck Sharp & Dohme مشتقات 5- فينوكسي-3h-بيريميدين-4-أون واستخدامها كمثبطات ناسخ عكسي ل hiv
US9233921B2 (en) 2013-03-08 2016-01-12 The Trustees Of The University Of Pennsylvania Potent poxvirus inhibitor
EP3077376B1 (en) 2013-12-04 2019-10-16 Merck Sharp & Dohme Corp. Process for making reverse transcriptase inhibitors
JP2015158727A (ja) * 2014-02-21 2015-09-03 東芝テック株式会社 閲覧端末、及び閲覧端末のプログラム
EP3785714A1 (en) 2014-04-01 2021-03-03 Merck Sharp & Dohme Corp. Prodrugs of hiv reverse transcriptase inhibitors
EP3760208B1 (en) 2014-06-25 2024-05-29 The General Hospital Corporation Targeting human satellite ii (hsatii)
US20210213041A1 (en) 2018-02-06 2021-07-15 The General Hospital Corporation Repeat rna as biomarkers of tumor immune response

Family Cites Families (48)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3600437A (en) 1969-05-28 1971-08-17 Lilly Co Eli Substituted phenylalkanoic acids and derivatives thereof
DE2805981A1 (de) * 1978-02-13 1979-08-16 Bayer Ag Phenoxypropionsaeure-derivate, verfahren zu ihrer herstellung und ihre verwendung als herbizide
DE2850902A1 (de) 1978-11-24 1980-06-12 Hoechst Ag Neue phenoxy-phenoxi-propionsaeureamide und ihre verwendung als herbizide
JPS562965A (en) * 1979-06-20 1981-01-13 Mitsui Toatsu Chem Inc Diphenyl ether derivative and herbicide comprising it
US4443248A (en) * 1982-04-12 1984-04-17 Velsicol Chemical Corporation Phenoxyphenoxypropionic acids and derivatives, and their use as herbicides
US4404018A (en) * 1982-06-23 1983-09-13 Velsicol Chemical Corporation Furfuryl amides of phenoxyphenoxyalkanoic acids and herbicidal use
US4599105A (en) * 1983-06-20 1986-07-08 The Dow Chemical Company 2-[16-(3-fluoro-5-trifluoromethyl-pyridinyl-2-oxy)-3-nitro-phenoxy]-propionic acid derivatives, herbicidal compositions containing same and herbicidal method of use
US4845264A (en) * 1987-03-05 1989-07-04 Teijin Limited Phenoxycarboxylic acid and herbicide comprising it as active ingredient
US5164407A (en) 1989-07-03 1992-11-17 Merck & Co., Inc. Substituted imidazo-fused 5-membered ring heterocycles and their use as angiotensin ii antagonsists
DE4133674A1 (de) * 1991-10-11 1993-04-15 Bayer Ag Fluorierte phenoxyphenoxycarbonsaeurederivate
WO1994012181A1 (en) * 1992-12-01 1994-06-09 Merck & Co., Inc. Fibrinogen receptor antagonists
GB9304920D0 (en) 1993-03-10 1993-04-28 Celltech Ltd Chemical compounds
JP3810020B2 (ja) 1993-04-22 2006-08-16 武田薬品工業株式会社 腎疾患の予防または治療剤
US5744492A (en) 1993-09-17 1998-04-28 United States Of America Method for inhibiting angiogenesis
US5665737B1 (en) 1994-10-12 1999-02-16 Euro Celtique Sa Substituted benzoxazoles
US6057346A (en) 1994-12-12 2000-05-02 The United States Of America As Represented By The Department Of Health And Human Services Inhibition of retroviral LTR promoters by calcium response modifiers
TW332201B (en) 1995-04-06 1998-05-21 Janssen Pharmaceutica Nv 1,3-Dihydro-1-(phenylalkyl)-2H-imidazol-2-one derivatives
US5710171A (en) 1995-05-24 1998-01-20 Merck & Co., Inc. Bisphenyl inhibitors of farnesyl-protein transferase
JP2002514162A (ja) 1996-07-08 2002-05-14 デュポン ファーマシューティカルズ カンパニー Xa因子阻害薬およびトロンビン阻害薬としてのアミジノインドール類、アミジノアゾール類、およびそれらの類似体
ES2176877T3 (es) * 1997-09-26 2002-12-01 Kowa Co Derivados de tetrazol como antagonistas de ltd4 y h1.
US6348032B1 (en) 1998-11-23 2002-02-19 Cell Pathways, Inc. Method of inhibiting neoplastic cells with benzimidazole derivatives
GB9910577D0 (en) * 1999-05-08 1999-07-07 Zeneca Ltd Chemical compounds
GB9920872D0 (en) 1999-09-04 1999-11-10 Glaxo Group Ltd Benzophenones as inhibitors of reverse transcriptase
US6800651B2 (en) * 2000-02-03 2004-10-05 Eli Lilly And Company Potentiators of glutamate receptors
WO2002074726A2 (en) * 2001-01-22 2002-09-26 Memory Pharmaceuticals Corporation Aniline derivatives useful as phosphodiesterase 4 inhibitors
CN1494528A (zh) 2001-03-02 2004-05-05 ʷ��˿�������ȳ�ķ���޹�˾ 作为逆转录酶抑制剂的二苯酮
EE05400B1 (et) 2001-04-10 2011-04-15 Pfizer Inc. Prasoolderivaadid, neid v?i nende farmatseutiliselt vastuv?etavaid sooli, solvaate v?i derivaate sisaldavad farmatseutilised kompositsioonid, nende kasutamine ning meetodid nende valmistamiseks
NZ531153A (en) * 2001-08-09 2005-10-28 Ono Pharmaceutical Co Carboxylic acid derivative compounds and drugs comprising these compounds as the active ingredient
ATE463478T1 (de) 2001-09-27 2010-04-15 Kyorin Seiyaku Kk Diaryletherderivat, dessen additionssalz und immunosuppressivum
JPWO2003048134A1 (ja) 2001-12-05 2005-04-14 日本たばこ産業株式会社 トリアゾール化合物及びその医薬用途
ATE402700T1 (de) * 2002-08-27 2008-08-15 Merck Patent Gmbh Glycinamid-derivate als raf-kinase-hemmer
KR20050119652A (ko) 2003-03-24 2005-12-21 에프. 호프만-라 로슈 아게 역전사 효소 저해제로서의 벤질-피리다진온
TW200505441A (en) 2003-03-24 2005-02-16 Hoffmann La Roche Non-nucleoside reverse transcriptase inhibitorsⅠ
US20060211724A1 (en) * 2003-04-28 2006-09-21 Verschueren Gaston W Hiv integrase inhibitors
WO2005012221A1 (ja) 2003-08-04 2005-02-10 Ono Pharmaceutical Co., Ltd. ジフェニルエーテル化合物、その製造方法および用途
KR20060115396A (ko) * 2003-10-28 2006-11-08 버텍스 파마슈티칼스 인코포레이티드 이온 채널 조절인자로서 유용한 벤즈이미다졸
US20050095215A1 (en) 2003-11-03 2005-05-05 Popp Karl F. Antimicrobial shampoo compositions
JP2007523938A (ja) 2004-02-27 2007-08-23 エフ.ホフマン−ラ ロシュ アーゲー ピラゾールの縮合誘導体
KR100844864B1 (ko) 2004-02-27 2008-07-09 에프. 호프만-라 로슈 아게 헤테로아릴-융합 피라졸로 유도체
US7417063B2 (en) 2004-04-13 2008-08-26 Bristol-Myers Squibb Company Bicyclic heterocycles useful as serine protease inhibitors
US7166738B2 (en) 2004-04-23 2007-01-23 Roche Palo Alto Llc Non-nucleoside reverse transcriptase inhibitors
US7625949B2 (en) 2004-04-23 2009-12-01 Roche Palo Alto Llc Methods for treating retroviral infections
WO2005105766A2 (en) * 2004-04-28 2005-11-10 Icos Corporation Arylphenylamino-and arylphenylether-sulfide derivatives, useful for the treatment of inflammatory and immune diseases, and pharmaceutical compositions containing them
CA2574308C (en) 2004-07-27 2014-03-25 F. Hoffmann-La Roche Ag Benzyltriazolone compounds as non-nucleoside reverse transcriptase inhibitors
EP1831157A2 (en) * 2004-12-22 2007-09-12 Pfizer Limited Nonnucleoside inhibitors of hiv-1 reverse transcriptase
EP1856053A1 (en) 2005-01-14 2007-11-21 Millennium Pharmaceuticals, Inc. Cinnamide and hydrocinnamide derivatives with raf-kinase inhibitory activity
ATE507212T1 (de) * 2005-01-18 2011-05-15 Hoffmann La Roche Morpholine als 5ht2c-agonisten
EP2057125B1 (en) 2006-08-16 2011-03-30 F. Hoffmann-La Roche AG Non-nucleoside reverse transcriptase inhibitors

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