Substituted benzimidazoles and methods of their use

New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

Substituted benzimidazoles and methods of their use

New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

Substituted benzimidazoles and methods of their use

New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

SUBSTITUTED BENZIMIDAZOLES AND METHODS OF THEIR USE

New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

SUBSTITUTED BENZ-AZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Substituted benzimidazoles and methods of their use

New substituted benzimidazole compounds, compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.

Substituted benz-azoles and methods of their use as inhibitors of Raf kinase

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Substituted benz-azoles and methods of their use as inhibitors of Raf kinase

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Substituted benzazoles and methods of their use as inhibitors of raf kinase

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

SUBSTITUTED BENZAZOLES AND METHODS OF THEIR USE AS INHIBITORS OF RAF KINASE

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

BENZIMIDAZOLES DERIVED COMPOUNDS SUBSTITUTED AS TYROSINE KINASE INHIBITORS

SE REFIERE A COMPUESTOS DE FORMULA (I) DONDE R1 ES OH, HALO, ALQUILO(C1-C6), ALCOXI(C1-C6), ENTRE OTROS; R2 ES ALQUILO(C1-C6) O HALO(ALQUILO(C1-C6)); R3 ES HALO, ALQUILO(C1-C6) O ALCOXI(C1-C6); R4 ES OH, ALQUILO(C1-C6), HALO, CARBOXILO, ENTRE OTROS; a ES DE 1 A 5; b ES DE 0 A 3; c ES 1 O 2; R1, R2, R3 Y R4 ESTAN OPCIONALMENTE SUSTITUIDOS CON OH, HALO, ALQUILO(C1-C6), ALCOXI(C1-C6), ENTRE OTROS. SON COMPUESTOS PREFERIDOS: {1-METIL-5-[2-(5-TRI-FLUORO-METIL-1H-IMIDAZOL-2-IL)-PIRIDIN-4-IL-OXI]-1H-BENZO-IMIDAZOL-2-IL}-(4-TRI-FLUORO-METILFENIL)-AMINA, (2-FLUORO-5-PIRIDIN-3-IL-FENIL)-{1-METIL-5-[2-(5-TRI-FLUORO-METIL-1H-IMIDAZOL-2-IL)-PIRIDIN-4-IL-OXI]-1H-BENZO-IMIDAZOL-2-IL}-AMINA, (2-FLUORO-5-PIRIDIN-4-IL-FENIL)-{1-METIL-5-[2-(5-TRI-FLUORO-METIL-1H-IMIDAZOL-2-IL)-PIRIDIN-4-IL-OXI]-1H-BENZO-IMIDAZOL-2-IL}-AMINA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE SERINA/ TREONINA QUINASA O TIROSINA QUINASA DE RECEPTORES SIENDO UTILES EN EL TRATAMIENTO DE CANCER DE MAMA, CANCER DE PROSTATA, MELANOMA, CANCER PANCREATICO

Substituted benz-azoles and methods of their use as inhibitors of RAF kinase

New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

SUBSTITUTED BENZAZOLE AND THEIR USE AS RAF KINASE HEMMER

BENCIMIDAZOLS REPLACED AS CINASA INHIBITORS

Se proporcionan nuevos compuestos de bencimidazol sustituidos de la fórmula (I), composiciones, y métodos para la inhibición de la actividad de cinasa asociada con tumorigénesis en un sujeto humano o animal. En ciertas modalidades, los compuestos y las composiciones son efectivos para inhibir la actividad de cuando menos una cinasa de serina/treonina o una cinasa de tirosina receptora. Los nuevos compuestos y composiciones se pueden utilizar solos o bien en combinación con cuando menos un agente adicional para el tratamiento de un trastorno mediado por cinasa de serina/treonina o por cinasa de tirosina receptora, tal como cáncer. New substituted benzimidazole compounds of the formula (I), compositions, and methods for inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective in inhibiting the activity of at least one serine / threonine kinase or a receptor tyrosine kinase. The new compounds and compositions can be used alone or in combination with at least one additional agent for the treatment of a serine / threonine kinase mediated disorder or receptor tyrosine kinase, such as cancer.

Substituted benzazoles and use thereof as inhibitors of raf kinase

New substituted benz-azole compounds of formula (I), compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Substituted benzimidazoles as kinase inhibitors

BENZAZOLES SUBSTITUTED AND ITS APPLICATION AS QUINASA RAF INHIBITORS

1.- Un compuesto de Fórmula (I):donde, X1 y X2 son seleccionados independientemente de = N-, -NR4, -O-, o -S-, estableciendo que X1 es -NR4, -O- o -S, por consiguiente X2 es = N-, o si X2 es -NR4-, -O- o -S-, entonces X2 es = N-, y ambos X1 y X2 no son = N-; Y es O ó S;Y es O ó S;A1 es alquil sustituido o no sustituido, cicloalquil, heterocicloalquil, aril, aril policíclico, arilalquil policíclico, heteroaril, biaril, heteroarilaril, heteroarilheteroaril, cicloalquilalquil, heterocicloalquilalquil, arilalquil, heteroarilalquil, biarilalquil, o heteroarilarilalquil;A2 es heteroaril sustituido o no sustituido;R1 es O ó H, y R2 es NR5R6 o hidroxil; o R1 es tomado junto a R2 para formar una heterocicloalquil sustituido o no sustituido o un grupo heteroaril; donde, la línea punteada representa un enlace singular o doble;R3 es hidrógeno, halógeno, bajoalquil, o bajoalcoxi;R4 es hidrógeno, hidroxil, alquilamino, dialquilamino o alquil;R5 y R6 son seleccionados independientemente de hidrógeno, y alquil sustituidos o no sustituidos, alcoxialquil, aminoalquil, amidoalquil, acil, cicloalquil, heterocicloalquil, aril, heteroaril, alquiloxialquilheterociclo, y heteroarilalquil; o R5 y R6 son tomados en conjunto para formar una heterociclo sustituido o no sustituido o heteroaril; ylas sales farmacéuticarnente aceptadas, esteres y prodrogas.

Substituted Benzylimidazoles as Motion Suspensions

Παρέχονται νέες υποκαθιστούμενες ενώσεις βενζιμιδαζόλης του τύπου (I), συνθέσεις και μέθοδοι αναστολής της δραστηριότητας κινάσης που συνδέεται με την ογκογένεση στον άνθρωπο ή τα ζώα. Σε ορισμένες εφαρμογές, οι ενώσεις και οι συνθέσεις είναι αποτελεσματικές για την αναστολή της δραστηριότητας τουλάχιστον μίας κινάσης ορίνης / θρεονίνης ή κινάσης τυροζίνης υποδοχέα. Οι νέες ενώσεις και οι συνθέσεις μπορούν να χρησιμοποιηθούν είτε μόνες τους είτε σε συνδυασμό με τουλάχιστον έναν συμπληρωματικό παράγοντα για τη θεραπεία μιας διαταραχής στην οποία εμπλέκεται η κινάση ορίνης / θρεονίνης ή η κινάση τυροζίνης υποδοχέα, όπως ο καρκίνος. New substituted benzimidazole compounds of formula (I), compositions and methods of inhibiting oncogenesis-related kinase activity in humans or animals are provided. In some embodiments, the compounds and compositions are effective for inhibiting the activity of at least one hormone / threonine kinase or receptor tyrosine kinase. The novel compounds and compositions may be used either alone or in combination with at least one adjuvant to treat a disorder involving the urine / threonine kinase or receptor tyrosine kinase, such as cancer.

Substituted benzazoles and use thereof as raf kinase inhibitors

New substituted benz-azole compounds of formula (I), compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.

Substituted benzimidazoles as kinase inhibitors

New substituted benzimidazole compounds of formula (I), compositions, and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase or receptor tyrosine kinase mediated disorder, such as cancer.

BENCIMIDAZOLS REPLACED AS CINASA INHIBITORS.

Se proporcionan nuevos compuestos de bencimidazol sustituidos de la Fórmula (I), composiciones, y métodos para la inhibición de la actividad de cinasa asociada con tumorigénesis en un sujeto humano o animal. En ciertas modalidades, los compuestos y las composiciones son efectivos para inhibir la actividad de cuando menos una cinasa de serina/treonina o una cinasa de tirosina receptora. Los nuevos compuestos y composiciones se pueden utilizar solos o bien en combinación con cuando menos un agente adicional para el tratamiento de un trastorno mediado por cinasa de serina/treonina o por cinasa de tirosina receptora, tal como el cáncer.

Substituierte benzimidazole als kinaseinhibitoren

Substituerte benzimidazoler som kinaseinhibitorer

Nye substituerte benzimidazolforbindelser av formel (I), sammensetninger og fremgangsmåter for inhibering av kinaseaktivitet assosiert med tumorigenese i et humant individ eller dyreindivid er tilveiebrakt. I enkelte utførelsesformer er forbindelsene og sammensetningene effektive til å inhibere aktiviteten av minst en serinAreoninkinase eller reseptortyrosinkinase. De nye forbindelsene og sammensetningene kan bli benyttet enten alene eller i kombinasjon med minst et ytterligere middel for behandlingen av en serin/treoninkinase eller reseptortyrosinkinasemediert lidelse, slik som cancer.