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CO5271669A1 - Carboxamidas de pirimidina utiles como inhibidores de isozimas pde4 - Google Patents

Carboxamidas de pirimidina utiles como inhibidores de isozimas pde4

Info

Publication number
CO5271669A1
CO5271669A1 CO01007018A CO01007018A CO5271669A1 CO 5271669 A1 CO5271669 A1 CO 5271669A1 CO 01007018 A CO01007018 A CO 01007018A CO 01007018 A CO01007018 A CO 01007018A CO 5271669 A1 CO5271669 A1 CO 5271669A1
Authority
CO
Colombia
Prior art keywords
triazolyl
bicyclo
nr12r13
octanyl
benzopyranyl
Prior art date
Application number
CO01007018A
Other languages
English (en)
Inventor
Robert James Chambers
Thomas Victor Magee
Original Assignee
Pfizer Prod Inc
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 Pfizer Prod Inc filed Critical Pfizer Prod Inc
Publication of CO5271669A1 publication Critical patent/CO5271669A1/es

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    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/34—One oxygen atom
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  • Ophthalmology & Optometry (AREA)

Abstract

Se describen compuestos de la fórmula siguiente: <EMI FILE="01007018_1" ID="1" IMF=JPEG >en la que j es 0 ó 1; k es 0 ó 1; m es 0 ó 1; n es 0 ó 1; W es -O-; -S(=O)t-, en el que t es 0, 1 ó 2; o -N(R3)-; en el que R3 es -H; -alquilo (C1-C3); -OR12; fenilo; o bencillo; RC y RD tienen el mismo significado que RA y RB salvo porque al menos uno de Rc y RD debe ser -H, ZA es (a) un grupo heterocíclico (C3-C9) saturado o insaturado, fusionado o abierto, cíclico o bicíclico, seleccionado entre furanilo, tienilo, pirrolilo, pirrolidinilo, oxazolilo, isoxazolilo, tiazolilo, isotiazolilo, morfolinilo, pirazolilo, oxadiazolilo, tiadiazolilo, imidazolilo, pirazinilo, pirimidinilo, piridazinilo, piperidinilo, piperazinilo, triazolilo, tetrazolilo, 2,3-benzofuranilo, 2,3-dihidrobenzofuranilo, 1,3-dihidroisobenzofuranilo, benzo[b]tienilo, indolilo, indolinilo, isoindolinilo, 2H-1-benzopiranilo, 4H-1-benzopiranilo, 1H-2-benzopiranilo, cromanilo, isocromanilo, quinoleilo, isoquinoleilo, 1,2,3,4-tetrahidroquinoleilo, 1,2,3,4-tetrahidroisoquinoIeilo, quinuclidinilo, azabiciclo[3.3.0]octanilo,1,3-benzodioxolilo, 3H-2,1-benzoxatiolilo, benzoxazolilo, 1,2-benzoisoxazolilo, 2,1-benzoisoxazolilo, 1,2-benzoditiolilo, 1,3-benzoditiolilo, benzotiazolilo, 1,2-benzoisotiazolilo, benzoimidazolilo, indazolilo, 1,4-benzodioxanilo, 4H-3,1-benzoxazinilo, 2H-1,4-benzoxazinilo, 1,4-benzotiazinilo, 1,2-benzotiazinilo, quinazolinilo, quinoxalinilo, ftalazinilo, cinnolinilo, 1,2,3-benzotiadiazolilo, 2H-1,2,4-benzotiadiazinilo, 2H-1,2,4-benzoxadiazinilo, benzoxatriazinilo, 1,2,3-benzotriazinilo, 1,2,4-benzotriazinilo y benzotetrazinilo; o ZA es (b) un resto cicloalquilo (C3-C7) monocíclico; un resto cicloalquenilo (C5-C7) monocíclico que es un miembro seleccionado del grupo que consiste en ciclopentenilo, ciclohexenilo y cicloheptenilo; o un resto cicloalquilo (C7-C10) o cicloalquenilo (C7-C10) bicíclico que es un miembro seleccionado del grupo que consiste en norbornanilo, norbornenilo, biciclo[2.2.2]octanilo, biciclo[3.2.1] octanilo, - 2 -biciclo[3.3.0]octanilo, biciclo[2.2.2]oct-5-enilo, biciclo-[2.2.2]oct-7-enilo, biciclo[3.3.1] nonanilo, ciclodecanilo y adamantanilo; en el que dichos restos cicloalquilo monocíclicos y bicíclicos están sustituidos con 0-3 R16; o ZA es (c) fenilo o piridilo sustituido con de 0 a 3 sustituyentes R4; en el que R4 es -F, -Cl, -CN, -OR12, -S(=O)pR12, -C(=O)OR12, -OC(=O)R12, -NO2, -C(=O)NR12R13, -OC(=O)NR12R13, -NR12R13, -NR14C(=O)R12, -NR14C(=O)OR12, -NR14S(=O)pR12, -S(=O)PNR12R13, -alquilo (C1-C4), fenilo, bencilo, o un resto heterociclo; y E es -H, -F, -Cl, -CN, -OR12, alquilo (C1-C4), hidroxialquilo (C1-C4), -CF3, -NO2, -NR12R13, -NR12S(=O)2R13, o -S(=O)2NR12R13.Se describe también un método para tratar a un sujeto que padece una enfermedad, trastorno o estado mediado por la isozima PDE4, mediante el que se regula la activación y la desgranulación de eosinófilos, que comprende administrar una cantidad terapéuticamente eficaz de un compuesto como el anteriormente descrito. Se describe además la utilidad de una composición farmacéutica para tratar enfermedades y estados inflamatorios, respiratorios y alérgicos, especialmente el asma; la enfermedad pulmonar obstructiva crónica (COPD), incluyendo la bronquitis crónica, el enfisema y la bronquiectasia; la rinitis crónica; y la sinusitis crónica.
CO01007018A 2000-01-31 2001-01-31 Carboxamidas de pirimidina utiles como inhibidores de isozimas pde4 CO5271669A1 (es)

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