公开(公告)号：US20140357633A1

公开(公告)日：2014-12-04

申请号：US14366855

申请日：2012-12-12

Applicant: NOVARTIS AG

Inventor： Daniel Ford ,  John Robert Porter ,  Michael Scott Visser ,  Naeem Yusuff

IPC: C07D513/04 ,  A61K31/4725 ,  C07D401/14 ,  C07D471/04 ,  C07D413/14 ,  A61K31/4745 ,  A61K31/513 ,  C07D405/14 ,  C07D487/04 ,  A61K31/519 ,  C07D409/14 ,  C07D417/14 ,  A61K31/501 ,  A61K31/5377 ,  C07D401/10

CPC classification number: C07D513/04 ,  A61K31/4725 ,  A61K31/4745 ,  A61K31/501 ,  A61K31/513 ,  A61K31/519 ,  A61K31/5377 ,  C07D401/10 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D513/02

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.

公开(公告)号：US20140350014A1

公开(公告)日：2014-11-27

申请号：US14366860

申请日：2012-12-12

Applicant: NOVARTIS AG

Inventor： Daniel Ford ,  John Robert Porter ,  Michael Scott Visser ,  Naeem Yusuff

IPC: C07D413/14 ,  C07D401/14 ,  A61K31/4725 ,  C07D401/10 ,  A61K31/5377 ,  A61K31/496

CPC classification number: C07D413/14 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/5377 ,  C07D401/10 ,  C07D401/14

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.

公开(公告)号：US20140343093A1

公开(公告)日：2014-11-20

申请号：US14366857

申请日：2012-12-12

Applicant: Novartis AG

Inventor： Daniel Ford ,  John Robert Porter ,  Michael Scott Visser ,  Naeem Yusuff

IPC: C07D401/10

CPC classification number: C07D401/10

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.

公开(公告)号：US09126979B2

公开(公告)日：2015-09-08

申请号：US14366857

申请日：2012-12-12

Applicant: Novartis AG

Inventor： Daniel Ford ,  John Robert Porter ,  Michael Scott Visser ,  Naeem Yusuff

IPC: C07D401/10 ,  A61K31/4725

CPC classification number: C07D401/10

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.

Abstract translation: 本发明涉及式I化合物：其中R 1，R 2，R 3和R 4如发明概述中所定义。 式I的化合物能够破坏含有BH3结构域的蛋白质的BCL-2相互作用。 破坏这种相互作用可以恢复BCL-2在癌细胞和表达BCL-2的肿瘤组织中的抗凋亡功能。 本发明还提供了制备本发明化合物的方法，包含这些化合物的药物制剂和使用这些化合物治疗癌性疾病的方法。