compostos para inibição da interação de bcl2 com contrapartes de ligação

abstract the present invention relates to compounds of formula i: in which r1, r2, r3 and r4 are as defined in the summary of the invention. compounds of formula i are capable of disrupting the bcl-2 interations with proteins containing a bh3 domain. disrupting this interaction can restore the anti-...

Ausführliche Beschreibung

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Bibliographische Detailangaben
Hauptverfasser: NAEEM YUSUFF, MICHAEL SCOTT VISSER
Format: Patent
Sprache:por
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Zusammenfassung:abstract the present invention relates to compounds of formula i: in which r1, r2, r3 and r4 are as defined in the summary of the invention. compounds of formula i are capable of disrupting the bcl-2 interations with proteins containing a bh3 domain. disrupting this interaction can restore the anti-apoptotic function of bcl-2 in cancer cells and tumor tissue expressing bcl-2. the invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases. tradução do resumo resumo patente de invenção: "compostos para inibição da interação de bcl2 com contrapartes de ligação". a presente invenção refere-se a compostos de fórmula i: onde r1, r2, r3 e r4 são conforme definido no sumário da invenção. os compostos de fórmula i são capazes de romper as interações de blc-2 com proteínas contendo um domínio bh3. rompimento desta interação pode restaurar a função antiapoptótica de blc-2 em células de câncer e tecido de tumor expressando bcl-2. a invencao provê ainda um processo para a preparação de compostos da invenção, preparações farmacêuticas compreendendo tais compostos e métodos de uso de tais compostos no tratamento de doenças cancerosas. The present invention relates to compounds of formula I: in which R1, R2, R3 and R4 are as defined in the Summary of the Invention. Compounds of formula I are capable of disrupting the BCL-2 interations with proteins containing a BH3 domain. Disrupting this interaction can restore the anti-apoptotic function of BCL-2 in cancer cells and tumor tissue expressing BCL-2. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds in the treatment of cancerous diseases.