AR033686A1 - Nuevos derivados de n-(arilsulfonil)beta-aminoacidos que comprenden un grupo aminometilo substituido, su preparacion, y las composiciones farmaceuticas que los contienen - Google Patents

Nuevos derivados de n-(arilsulfonil)beta-aminoacidos que comprenden un grupo aminometilo substituido, su preparacion, y las composiciones farmaceuticas que los contienen

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Publication number
AR033686A1
AR033686A1 ARP020101096A ARP020101096A AR033686A1 AR 033686 A1 AR033686 A1 AR 033686A1 AR P020101096 A ARP020101096 A AR P020101096A AR P020101096 A ARP020101096 A AR P020101096A AR 033686 A1 AR033686 A1 AR 033686A1
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Argentina
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group
unsubstituted
substituted
several times
alkyl
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ARP020101096A
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English (en)
Inventor
Bernard Ferrari
Jean Gougat
Yvette Muneaux
Pierre Perreaut
Lionel Sarran
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Sanofi Aventis
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Publication of AR033686A1 publication Critical patent/AR033686A1/es

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    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
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Abstract

Compuestos de fórmula (1) en la cual: R1 representa un grupo fenilvinilo; fenilo no sustituido o sustituido una o varias veces por R6, idénticos o diferentes; naftilo no sustituido o sustituido una o varias veces por R6, idénticos o diferentes; tetrahidronaftilo; nafto[2,3-d][1,3]dioxol-6-ilo; un radical heterocíclico elegido entre quinolilo, isoquinolilo, 1-benzofuran-2-ilo, 2,1,3-benzoxadiazol-4-ilo, 2,1,3-benzotiadiazol-4-ilo, 1,3-benzotiazol-2-ilo, 1-benzotiofen-2-ilo, 1H-pirazol-4-ilo, tien-2-ilo, 5-isoxazoltien-2-ilo, benzotien-2-ilo, tieno [3,2-c]piridin-2-ilo; dichos radicales heterocíclicos están no sustituidos o sustituidos una o varias veces por R6 idénticos o diferentes; R2 representa hidrógeno o un grupo alquilo(C1-4) y R3 representa un grupo fenilo no sustituido o sustituido una o varias veces por R7, idénticos o diferentes; un radical heterocíclico elegido entre benzo[1,3]dioxol-5-ilo, 2,1,3-benzotiadiazol-5-ilo, 2,1,3-benzoxiadiazol-5-ilo, benzotiofen-5-ilo, 2,3-dihidro-benzo[1,4]dioxin-6-ilo, benzofuranilo, dihidrobenzofuranilo, 1,3-tiazol-2-ilo, furano tienilo, dicho radical heterocíclico está no sustituido o sustituido una o varias veces por un átomo de halógeno o un grupo alquilo (C1-4); o bien R2 representa un grupo fenilo no sustituido o sustituido una o varias veces por R6, idénticos o diferentes; un radical heterocíclico elegido entre benzo[1,3]dioxol-5-ilo, piridilo, indanilo, y R3 representa hidrógeno; R4 representa un grupo -CONR8R9; un grupo -CSNR8R9; un grupo -COR13; un grupo fenilo no sustituido o sustituido una o varias veces por R10; un radical heterocíclico elegido entre piridilo, imidazolilo, furilo, benzimidazolilo, benzotiazol-2-ilo, benzo[1,3]dioxol-5-ilo, dichos radicales están no sustituidos o sustituidos por uno o varios grupos metilo o átomos de halógeno; R5 representa un grupo -CH2NR11R12 o -CH2N(O)NR11R12; R6 representa un átomo de halógeno; un grupo alquilo(C1-4); trifluorometilo; alcoxi(C1-4); 2-fluroetoxi; trifluorometoxi, metilendioxi, difluorometilendioxi, R7 representa un átomo de halógeno; un grupo alquilo(C1-4); fluorometilo; alcoxi(C1-4); benciloxi; trifluorometoxi; R8 y R9 representan cada uno independientemente hidrógeno; un grupo alquilo(C1-4); cicloalquilo (C3-7); cicloalquilo(C3-7)alquilo(C1-4); w-dialquilamino(C1-4)alquilo(C2-4); o bien R8 y R9 junto con el átomo de nitrógeno al cual están unidos constituyen un radical heterocíclico elegido entre pirrolidinilo, morfolin-4-ilo, tiomorfolin-4-ilo, azepin-1-ilo, piperidinilo no sustituido o sustituido por uno o varios átomos de halógeno o uno o varios grupos alquilo(C1-4) o alcoxi(C1-4) o trifluorometilo, 3,4-dihidropiperidin-1-ilo, ciclohexilespiro-4-piperidin-1-ilo, piperazinilo no sustituido o sustituido por uno o varios grupos alquilo(C1-4); R10 representa un átomo de halógeno; un grupo alquilo(C1-4); hidroxi; alcoxi(C1-6); R10 puede además representar un grupo -CH2NR11R12 cuando R5 representa un grupo -CH2NR11R12, entonces, dichos grupos son idénticos; R11 y R12 representan cada uno independientemente, hidrógeno; un grupo alquilo(C1-6); alquenilo(C2-4); cicloalquilo(C3-7); cicloalquilo(C3-7)alquilo(C1-4); w-hidroxialquileno(C2-4); w-metoxialquileno(C2-4); w-trifluorometilalquileno(C2-4); w-halogenoalquileno(C2-4), o bien R11 y R12 junto con el átomo de nitrógeno al cual están unidos constituyen un radical heterocíclico, mono o bicíclico, elegido entre azetidinilo, pirrolidinilo, morfolin-4-ilo, tiomorfolin-4-ilo, piperidin-1-ilo, piperazin-1-ilo, 1,2,3,6-tetrahidropirid-1-ilo, 2,3,4,5-tetrahidropiridinio, decahidroquinolilo, decahidroisoquinolilo, tetrahidroisoquino-ilo, octahidro-1H-isoindolilo, cicloalquilespiropiperidinilo (C4-6), 3-azabiciclo[3.1.0]hexilo, 7-azabiciclo[2.2.1]heptan-7-ilo, no sustituido o sustituidos una o varias veces por un átomo de halógeno, un grupo alquilo(C1-4), hidroxi, alcoxi(C1-4), trifluorometilo, difluorometileno, fenilo; R13 representa un grupo fenilo, tiazol-2-ilo o piridilo; así como sus sales con ácidos minerales u orgánicos y/o solvatos o sus hidratos. Estos compuestos presentan una afinidad con los receptores de la bradikinina con una selectividad para los receptores B1; pueden ser utilizados para la preparación de medicamentos destinados al tratamiento o a la prevención de las patologías de la inflamación y de las enfermedades inflamatorias persistentes o crónicas. Su preparación y composiciones farmacéuticas que comprenden los compuestos de la fórmula (1).
ARP020101096A 2001-03-28 2002-03-26 Nuevos derivados de n-(arilsulfonil)beta-aminoacidos que comprenden un grupo aminometilo substituido, su preparacion, y las composiciones farmaceuticas que los contienen AR033686A1 (es)

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