Combinations for the treatment of cancer comprising an MPS-1 kinase inhibitor and a mitotic inhibitor

A mitosis and inhibitor technology, applied in the direction of drug combination, organic active ingredients, heavy metal active ingredients, etc., can solve the problems of accelerating cells, cell death, and anti-mitotic drugs stagnating mitosis.

Inactive Publication Date: 2016-01-27
BAYER PHARMA AG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In contrast, Mps-1 kinase inhibitors induce SAC inactivation, which accelerates the progression of cells through mitosis, leading to severe chromosome missegregation and ultimately cell death
Silencing of Mps-1 renders cells incapable of arresting mitosis in response to antimitotic drugs

Method used

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  • Combinations for the treatment of cancer comprising an MPS-1 kinase inhibitor and a mitotic inhibitor
  • Combinations for the treatment of cancer comprising an MPS-1 kinase inhibitor and a mitotic inhibitor
  • Combinations for the treatment of cancer comprising an MPS-1 kinase inhibitor and a mitotic inhibitor

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Experimental program
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Embodiment Construction

[0029] According to a first aspect, the present invention relates to a combination comprising an Mps-1 kinase inhibitor and one or more mitotic inhibitors.

[0030] The Mps-1 kinase inhibitor is selected from compounds of formula (I):

[0031]

[0032] in:

[0033] R 1 express

[0034]

[0035] where * indicates the point of attachment of said group to the rest of the molecule;

[0036] R 2 express

[0037]

[0038] where * indicates the point of attachment of said group to the rest of the molecule;

[0039] R 3 Represents a group selected from: methyl-, HO-CH 2 -, H 2 N-CH 2 -, -NH 2 ;

[0040] R 4 represents a group selected from: methoxy-, F 3 C-CH 2 -O-;

[0041] and

[0042] R 5 represents a group selected from:

[0043] h 3 C-S(O) 2 -, H 2 N-C(O)-, (CH 3 ) 2 N-C(O)-,

[0044]

[0045] or a hydrate, solvate or salt thereof, or a mixture thereof.

[0046] In a preferred embodiment, R 3 denotes a methyl-group.

[0047] In another preferr...

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Abstract

The present invention relates to a combination comprising an Mps-1 kinase inhibitor and a mitotic inhibitor. The present invention also relates to the use of said combination for the treatment of cancer, in particular of pancreatic cancer, glioblastoma, ovarian cancer, non-small cell lung carcinoma, breast cancer and / or gastric cancer.

Description

[0001] The present invention relates to combinations comprising an inhibitor of Mps-1 kinase and an inhibitor of mitosis. The invention also relates to the use of said combination for the treatment of cancer, especially pancreatic cancer, glioblastoma, ovarian cancer, non-small cell lung cancer, breast cancer and / or gastric cancer. Background of the invention [0002] Mps-1 (monopolar spindle 1) kinase (also known as tyrosine-threonine kinase, TTK) is a dual-specificity Ser / Thr kinase that acts at the mitotic checkpoint (also known as spindle checkpoint, spindle assembly checkpoint), thereby ensuring proper chromosome segregation during mitosis [AbrieuA et al., Cell, 2001, 106, 83-93]. Each dividing cell must ensure that the duplicated chromosomes are divided equally between the two daughter cells. After entering mitosis, the chromosomes join at their centromeres to the microtubules of the spindle. The mitotic checkpoint is a supervisory mechanism that is active as long as u...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/337A61K31/437A61K31/475A61K33/24A61P35/00A61K33/243
CPCA61K31/337A61K31/475A61K31/437A61P35/00A61P43/00A61K33/243A61K2300/00A61K33/24
Inventor A.M.温格纳G.西迈斯特
Owner BAYER PHARMA AG
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