Substituted benzimidazoles and methods of preparation

Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined herein ...

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 PREPARATION

Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined herein ...

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 preparation

Methods for preparing new substituted benzimidazole compounds having formula (I) useful for treating kinase mediated disorders are provided wherein R1, R2, R3, R4, a, b, and c are defined herein ...

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

Pyrimidine derivative, its use as a drug and composition containing the derivative

Fosfatidylinositol (PI) 3-kinaseinhibitorforbindelser (I), deres farmasøytisk akseptable salter og prodrug derav; sammensetninger av de nye forbindelsene, enten alene, eller i kombinasjon med minst et ytterligere terapeutisk middel, med en farmasøytisk akseptabel bærer; og anvendelser av de nye forbindelsene, enten alene eller i kombinasjon med minst et ytterligere terapeutisk middel, for profylakse eller behandling av proliferative sykdommer kjennetegnet ved abnormal aktivitet til vekstfaktorer, protein serin/treoninkinaser og fosfolipidkinaser. Phosphatidylinositol (PI) 3-kinase inhibitor compounds (I), their pharmaceutically acceptable salts and prodrugs thereof; compositions of the novel compounds, either alone, or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier; and uses of the novel compounds, either alone or in combination with at least one additional therapeutic agent, for the prophylaxis or treatment of proliferative diseases characterized by abnormal activity of growth factors, protein serine / threonine kinases and phospholipid kinases.

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 benzimidazoles as kinase inhibitors

SUBSTITUTED BENZIMIDAZOLES AND METHODS OF PREPARATION

L'invention concerne des procédés de préparation de nouveaux composés benzimidazoles substitués de formule (I) utiles pour le traitement de troubles à médiation par kinase, où R1, R2, R3, R4, a, b, et c sont définis au sein de la formule (I). The invention relates to processes for the preparation of novel substituted benzimidazole compounds of formula (I) useful for the treatment of kinase-mediated disorders, wherein R1, R2, R3, R4, a, b, and c are defined within the formula (I).

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 benzimidazoles and methods of preparation

Pyrimidine derivatives used as PI-3 kinase inhibitors

Fosfatidylinositol (PI) 3-kinaseinhibitorforbindelser (I), deres farmasøytisk akseptable salter og prodrug derav; sammensetninger av de nye forbindelsene, enten alene, eller i kombinasjon med minst et ytterligere terapeutisk middel, med en farmasøytisk akseptabel bærer; og anvendelser av de nye forbindelsene, enten alene eller i kombinasjon med minst et ytterligere terapeutisk middel, for profylakse eller behandling av proliferative sykdommer kjennetegnet ved abnormal aktivitet til vekstfaktorer, protein serin/treoninkinaser og fosfolipidkinaser.

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.