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Combinations of (a) an ATP-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents

A competitive inhibitor and kinase activity technology, applied in antineoplastic drugs, drug combinations, organic active ingredients, etc.

Inactive Publication Date: 2005-12-28
NOVARTIS AG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Phase I study shows that STI571 has strong activity against chronic phase CML, but limited anti-p190 expression bcr / abl Blast crisis activity of acute lymphoblastic leukemia and CML

Method used

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  • Combinations of (a) an ATP-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents
  • Combinations of (a) an ATP-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents
  • Combinations of (a) an ATP-competitive inhibitor of c-acl kinase activity with (b) two or more other antineoplastic agents

Examples

Experimental program
Comparison scheme
Effect test

Embodiment approach

[0070] In the following preferred embodiments of the invention, more general terms may be replaced independently or entirely by the more specific definitions given above, thus resulting in more preferred embodiments of the invention.

[0071] Preferred combinations of the invention comprise (a) N-{5-[4-(4-methyl-piperazin-1-yl-methyl)-benzamido]-2-methylphenyl}-4 -(3-pyridyl)-2-pyrimidine-amine, or a pharmaceutically acceptable salt thereof, and (b) at least two other antineoplastic agents, independently in free form or in pharmaceutically acceptable salt form, preferably the above defined antineoplastic agents.

[0072] More preferred combinations of the present invention comprise (a) N-{5-[4-(4-methyl-piperazin-1-yl-methyl)-benzamido]-2-methylphenyl}- 4-(3-pyridyl)-2-pyrimidine-amine, or a pharmaceutically acceptable salt thereof, and (b) two or three, preferably two, selected from purine nucleoside analogs and topoisomerase II inhibitors Other antineoplastic agents can be...

Embodiment 1

[0128] Example 1: N-{5-[4-(4-methyl-piperazin-1-yl-methyl)-benzamido]-2-methylbenzene Base}-4-(3-pyridyl)-2-pyrimidine-amine monomethanesulfonate (STI571) with fludarabine and cytarabine (ara-C) combination - effect on CEM / 0 cells

[0129] effective dose

[0130] From these data it can be seen that the ED 50 and ED 70 Synergy found between STI571 and fludarabine and ara-C, but in ED 90 No synergistic effect was found.

Embodiment 2

[0131] Example 2: N-{5-[4-(4-methyl-piperazin-1-yl-methyl)-benzamido]-2-methylbenzene Base}-4-(3-pyridyl)-2-pyrimidine-amine monomethanesulfonate (STI571) with fludarabine and cytarabine (ara-C) Combination with fludarabine first - effect on CEM / 0 cells

[0132] effective dose

[0133] Visible: Compared with Example 1, in ED 50 and ED 70 When fludarabine treatment was preceded by STI treatment for 4 hours, a smaller drug synergy was found, and in the ED 90 However, no synergistic effect was found.

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PUM

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Abstract

The invention relates to combinations of (a) an ATP-competitive inhibitor of c-abl kinase activity with (b) two or more other antineoplastic agents for simultaneous, separate or sequential use, in particular for the delay of progression or treatment of a proliferative disease

Description

field of invention [0001] The present invention relates to ATP-competitive inhibitors of (a) c-abl kinase activity and (b) two or more Combinations of other antineoplastic agents; methods of treating warm-blooded animals, particularly humans, with proliferative disorders comprising combining (a) an ATP-competitive inhibitor of c-abl kinase activity and (b) two or Combinations of multiple other antineoplastic agents administered to animals; pharmaceutical compositions comprising such combinations; uses of such combinations in the manufacture of medicaments for treating proliferative diseases or delaying their progression; and commercial packages or product. Background of the invention [0002] Individual compounds as well as selective combinations of purine and pyrimidine analogs are known to increase remission rates, especially in pediatric patients with relapsed leukemia. [0003] For example, Ara-C, a pyrimidine analog, is the 2'-α-hydroxyribose (arabinoside) derivative ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K31/704A61K31/7068A61K31/7076A61K45/06A61P35/00A61P35/02A61P43/00
CPCA61K31/506A61K31/704A61K31/7068A61K31/7076A61K45/06A61P35/00A61P35/02A61P43/00A61K2300/00
Inventor I·A·阿夫拉米斯V·I·阿夫拉米斯
Owner NOVARTIS AG
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