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AR035218A1 - Inhibidores vla-4 - Google Patents

Inhibidores vla-4

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Publication number
AR035218A1
AR035218A1 ARP010106105A ARP010106105A AR035218A1 AR 035218 A1 AR035218 A1 AR 035218A1 AR P010106105 A ARP010106105 A AR P010106105A AR P010106105 A ARP010106105 A AR P010106105A AR 035218 A1 AR035218 A1 AR 035218A1
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AR
Argentina
Prior art keywords
group
substituted
unsubstituted
atom
hydrogen atom
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ARP010106105A
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English (en)
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Daiichi Seiyaku Co
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Publication of AR035218A1 publication Critical patent/AR035218A1/es

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    • C07D263/54Benzoxazoles; Hydrogenated benzoxazoles
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    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
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Abstract

Un compuesto representado por la siguiente fórmula (1) [donde, W representa WA-A1-WB- (en el cual WA representa un grupo arilo sustituido o no sustituido o un grupo heterocíclico monovalente sustituido o no sustituido, A1 representa -NR1-, un enlace simple, -C(O)-, -C(O)NR1-, un grupo vinileno sustituido o no sustituido, un grupo etinileno, -CR1aR1b-O-, -CR1a=CR1b-C(O)NR1- o CR1a=CR1b-C(O)-(en el cual R1 representa un átomo de hidrógeno o un grupo alquilo inferior, y R1a y R1b, cada uno representa de manera independiente un átomo de hidrógeno o un grupo alquilo inferior), WB representa un grupo arileno sustituido o no sustituido o un grupo heterocíclico divalente sustituido); R representa un enlace simple, -NH-, -OCH2-, un grupo alquenileno o -(CH2)n-(en el cual, n representa 1 o 2); X representa -C(O)-, -CH2 - o -S(O)2-, y M representa la siguiente fórmula (3), (4) o (5): en la cual (3a) representa un grupo heterocíclico divalente de 4, 5 o 6 miembros (en el cual el átomo de nitrógeno está unido a X y Q representa un átomo de carbono, azufre oxígeno o nitrógeno), R11, R12 y R13 cada uno representa de manera independiente un átomo de hidrógeno, un grupo hidroxilo, un grupo amino, un átomo de halógeno, un grupo ciano, un grupo carboxilo, un grupo alcoxicarbonilo, un grupo carbamoilo, un grupo mono- o dialquilaminocarbonilo sustituido o no sustituido, un grupo alquilo sustituido o no sustituido, un grupo arilo sustituido o no sustituido, un grupo heteroarilo sustituido o no sustituido, un grupo alcoxi sustituido o no sustituido, un grupo mono- o dialquilamino sustituido o no sustituido, un grupo cicloalquilamino sustituido o no sustituido, un grupo alquilsulfonilamino sustituido o no sustituido, un grupo arilsulfonilamino sustituido o no sustituido, un grupo ariloxi, sustituido o no sustituido, un grupo heteroariloxi sustituido o no sustituido, y un grupo benciloxi sustituido o no sustituido, un grupo alquiltio sustituido o no sustituido, un grupo cicloalquiltio sustituido o no sustituido, un grupo ariltio sustituido o no sustituido, un grupo alquilsulfonilo sustituido o no sustituido, un grupo cicloalquilsulfonilo sustituido o no sustituido, o un grupo arilsulfonilo sustituido o no sustituido, o R11, R13 o R12 y R13 se pueden acoplar para formar, junto con el átomo que constituye el grupo heterocíclico al que R12 a R13 están unidos, un hidrocarburo cíclico o heterociclo de 3 a 7 miembros (el hidrocarburo cíclico y el heterociclo pueden tener de 1 a 3 sustituyentes seleccionados de un grupo hidroxilo, átomos de halógeno, un grupo amino, grupos alquilo, grupos alcoxi, grupos arilo, grupos ariloxi, grupos alquilamino, un grupo benciloxi y grupos heteroarilo). R14 representa un átomo de hidrógeno o un alquilo inferior sustituido o no sustituido, Y representa un enlace simple, -C(O)-, -C(O)NH-, o un grupo hidrocarburo alifático divalente lineal o ramificado de C1-12 que puede tener un anillo espiro de C3-6 o puede tener por los menos un -O-, -S-, -S(O)2-, -C(O)- o -NY1- (en la cual Y1 representa un átomo de hidrógeno o un grupo alquilo inferior) en el grupo funcional hidrocarburo en reemplazo del átomo de carbono, Z representa un grupo arileno sustituido o no sustituido, un grupo heteroarileno sustituido o no sustituido o un grupo cicloalquileno sustituido o no sustituido, A2 representa un enlace simple, un grupo alquenileno, un grupo alquinileno, -(CH2)t - o -O(CH2)v-, (en el que t representa 1, 2 o 3 y v representa 0, 1, 2, o 3), y R10 representa un grupo hidroxilo o un grupo alcoxi inferior) de fórmula (4), en el cual fórmula (4a) representa un grupo heterocíclico divalente de 4, 5, 6 o 7 miembros (en el cual el átomo de nitrógeno está unido a X y Q1 representa un átomo de carbono, azufre, oxígeno o nitrógeno), R15 y R16 cada uno representa de manera independiente un átomo de hidrógeno, un grupo hidroxilo, un átomo de halógeno, un grupo amino, un grupo alquilo sustituido o no sustituido o un grupo alcoxi, R16a representa un átomo de hidrógeno o un grupo alquilo sustituido o no sustituido; Y3 representa -O-, -S-, -S(O)2-, -(CH2)fO-, o -NY4- (en la cual f representa 1, 2 o 3 e Y4 representa un átomo de hidrógeno o un grupo alquilo inferior), Z1 representa un grupo arileno sustituido o no sustituido, un grupo heteroarileno sustituido o no sustituido o un grupo cicloalquileno sustituido o no sustituido, A3 representa un enlace simple, un grupo alquenileno, un grupo alquinileno, -(CH2)e- (en el que, e representa 1, 2, o 3), y R17 representa un grupo hidroxilo o un grupo alcoxi inferior), (fórmula 5) (en la cual R18 representa -NR20-(en la cual R20 representa un átomo de hidrógeno, un grupo alquilo sustituido o no sustituido, un grupo cicloalquilo sustituido o no sustituido, un grupo arilo sustituido o no sustituido, un grupo bencilo sustituido o no sustituido, un grupo alquenilo inferior sustituido o no sustituido o un grupo alquinilo sustituido o no sustituido), Z2 representa un grupo hidrocarbonado alifático divalente lineal o ramificado de C1-12 que puede tener un anillo espiro de C3-6, puede tener por lo menos un grupo cicloalquileno de C3-6 en el grupo hidrocarbonado en reemplazo del átomo de carbono o puede tener por lo menos un -O-, -S-, -S(O)2-, -C(O)- o -NR21-(en la cual R21 representa un átomo de hidrógeno o un grupo alquilo inferior sustituido o no sustituido en el grupo funcional hidrocarburo en reemplazo del átomo de carbono, Q2 representa un enlace simple, un grupo arileno sustituido o no sustituido, un grupo heteroarileno sustituido o no sustituido o un grupo cicloalquileno sustituido o no sustituido, L representa un enlace simple, o un grupo alquileno inferior sustituido o no sustituido o un grupo alquinileno inferior sustituido o no sustituido, o R19 representa un grupo hidroxi o un grupo alcoxi inferior)]; o una sal del mismo. Un producto farmacéutico que comprende un compuesto de fórmula (1) o sal del mismo, útil como preventivo o remedio de una enfermedad causada por adhesión celular que se selecciona entre enfermedades inflamatorias, autoinmunes, metástasis, asma bronquial, rinostenosis, diabetes, artritis, psoriasis, esclerosis múltiple, enfermedades intestinales inflamatorias y rechazo al trasplante. Una composición farmacéutica que comprende un vehículo farmacéuticamente aceptable y un compuesto de fórmula (1) o su sal.
ARP010106105A 2000-12-28 2001-12-28 Inhibidores vla-4 AR035218A1 (es)

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JP2000402890 2000-12-28
JP2001149923 2001-05-18

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AR035218A1 true AR035218A1 (es) 2004-05-05

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US (1) US7157487B2 (es)
EP (1) EP1346982B1 (es)
JP (1) JP4212358B2 (es)
KR (1) KR100884877B1 (es)
CN (1) CN100471838C (es)
AR (1) AR035218A1 (es)
AT (1) ATE524441T1 (es)
AU (1) AU2002219555B2 (es)
BR (1) BR0116608A (es)
CA (1) CA2430978C (es)
IL (1) IL156064A0 (es)
MX (1) MXPA03005838A (es)
NO (1) NO326014B1 (es)
RU (1) RU2290403C2 (es)
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WO (1) WO2002053534A1 (es)

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