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
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AR
Argentina
Prior art keywords
alkyl
group
nr3r4
optionally
fluoroalkyl
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ARP060102994A
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English (en)
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Merck & Co Inc
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Publication of AR057455A1 publication Critical patent/AR057455A1/es

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    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides 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
    • C07C311/30Sulfonamides, the carbon skeleton of the acid part being further substituted by singly-bound nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/45Sulfonamides, 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
    • C07C311/46Y being a hydrogen or a carbon atom
    • 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
    • A61K31/435Heterocyclic 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
    • A61K31/4353Heterocyclic 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
    • A61K31/437Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • 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
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    • 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
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
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    • C07C255/00Carboxylic acid nitriles
    • C07C255/49Carboxylic acid nitriles having cyano groups bound to carbon atoms of six-membered aromatic rings of a carbon skeleton
    • C07C255/58Carboxylic 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
    • C07C255/60Carboxylic 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
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C307/00Amides 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
    • C07C307/04Diamides of sulfuric acids
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    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • C07C317/26Sulfones; Sulfoxides having sulfone or sulfoxide groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C317/32Sulfones; 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
    • C07C317/34Sulfones; 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
    • C07C317/38Sulfones; 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
    • C07C317/40Y being a hydrogen or a carbon atom
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/08Indoles; Hydrogenated indoles with only hydrogen atoms or radicals containing only hydrogen and carbon atoms, directly attached to carbon atoms of the hetero ring
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    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/62Oxygen or sulfur atoms
    • C07D213/63One oxygen atom
    • C07D213/65One oxygen atom attached in position 3 or 5
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    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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
    • C07D213/72Nitrogen atoms
    • C07D213/75Amino or imino radicals, acylated by carboxylic or carbonic acids, or by sulfur or nitrogen analogues thereof, e.g. carbamates
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56Benzopyrazoles; Hydrogenated benzopyrazoles
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
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    • C07D249/00Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms
    • C07D249/02Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D249/041,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
    • C07D249/061,2,3-Triazoles; Hydrogenated 1,2,3-triazoles with aryl radicals directly attached to ring atoms
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
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    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/061,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
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    • C07DHETEROCYCLIC COMPOUNDS
    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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    • C07D271/00Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
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    • C07D271/101,3,4-Oxadiazoles; Hydrogenated 1,3,4-oxadiazoles
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    • C07D333/46Heterocyclic 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
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    • 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
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  • Veterinary Medicine (AREA)
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  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
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  • AIDS & HIV (AREA)
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  • Epidemiology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Indole Compounds (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)

Families Citing this family (24)

* 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
WO2008019968A1 (en) * 2006-08-16 2008-02-21 F. Hoffmann-La Roche Ag Non-nucleoside reverse transcriptase inhibitors
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