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Inhibitors of akt activity

A technology selected from, alkyl, applied in the direction of organic active ingredients, pill delivery, medical preparations containing active ingredients, etc., can solve problems such as impact

Active Publication Date: 2010-02-10
NOVARTIS AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, PI3K inhibition not only potentially indiscriminately affects all three Akt isozymes but also other PdtIns(3,4,5)-P3-dependent PH domain-containing signaling molecules such as the Tec family of tyrosine kinases

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 96

[0565] The compound of Example 96 was generally tested according to the AKT enzyme assay described above, and exhibited pIC50 values ​​in at least one assay: equal to 9.0 for full-length AKT1; equal to 8.0 for full-length AKT2; and equal to 8.8 for full-length AKT3.

Embodiment 137

[0566] The compound of Example 137 was generally tested according to the AKT enzyme assay described above, and exhibited pIC50 values ​​in at least one assay: equal to 9.0 for full-length AKT1; equal to 7.8 for full-length AKT2; and equal to 8.4 for full-length AKT3.

Embodiment 224

[0567] The compound of Example 224 was generally tested according to the AKT enzyme assay described above, and exhibited pIC50 values ​​in at least one assay: equal to 8.7 for full-length AKT1; and equal to 7.8 for full-length AKT2.

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PUM

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Abstract

Invented are novel heterocyclic carboxamide compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.

Description

field of invention [0001] The present invention relates to novel heterocyclic carboxamide compounds, the use of these compounds as inhibitors of protein kinase B (hereinafter referred to as PKB / Akt, PKB or Akt) activity and in the treatment of cancer and arthritis. Background of the invention [0002] The present invention relates to heterocyclic carboxamide compounds which are inhibitors of the activity of one or more serine / threonine kinase Akt (also known as protein kinase B) isoforms (isoforms), the compounds of the invention are suitably all three Inhibitors of the activity of an isoform of the serine / threonine kinase Akt. The invention also relates to pharmaceutical compositions comprising said compounds and methods of using the compounds of the invention in the treatment of cancer and arthritis (Liu et al. Current Opin. Pharmacology 3 : 317-22 (2003)). [0003] Apoptosis (programmed cell death) plays an important role in embryonic development and the pathogenesis o...

Claims

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Application Information

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IPC IPC(8): A61K31/12
CPCA61K31/12C07D409/04C07D403/04C07D405/12C07D409/12C07D405/04C07D409/14A61K31/4155A61K31/4178A61K31/4192A61K31/4196A61P19/00A61P19/02A61P35/00A61P35/02A61P35/04A61P43/00A61K45/06A61K9/0019A61K9/0053A61K9/20A61K9/48A61K31/4439
Inventor 马克·A·西费尔德米根·B·劳斯德克·A·西尔丁西蒙·皮斯丹尼斯·S·亚马希塔肯尼思·C·麦克纳尔蒂
Owner NOVARTIS AG
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