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Combination

A technology of compounds and solvates, applied in the field of treating cancer in mammals, can solve the problem of low frequency

Inactive Publication Date: 2012-09-12
GLAXO SMITHKLINE LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ultimately, the pathway can be genetically activated downstream of PI3K by DNA amplification or mutation of AKT; however, these genetic events occur with low frequency in human cancers

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0102] Preparation of MEK inhibitors

[0103] MEK inhibitors suitable for use in the combinations according to the invention, in particular

[0104] N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4 ,6,7-Tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide dimethyl sulfoxide

[0105]

[0106] It can be prepared according to International Patent Publication WO2005 / 121142.

[0107] PI3K inhibitors suitable for use in the combinations of the invention, in particular

[0108] 2,4-Difluoro-N-{2-(methoxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridyl}benzenesulfonamide

[0109]

[0110] It can be prepared according to International Patent Publication No. WO08 / 144463 (Example 345).

[0111] Compound A described in the experimental part refers to N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2, dimethylsulfoxide solvate of 4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide.

[0112] In v...

Embodiment 1

[0222] Example 1 - Capsule Composition

[0223] Oral dosage forms for administering the combinations of the invention are prepared by filling standard two-part hard gelatin capsules with the ingredients in the proportions shown in Table I below.

[0224] Table I

[0225]

[0226]

Embodiment 2

[0227] Example 2 - Capsule Composition

[0228] Oral dosage forms for administering one of the compounds of the invention are prepared by filling standard two-part hard gelatin capsules with the ingredients in the proportions shown in Table II below.

[0229] Table II

[0230]

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PUM

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Abstract

The present invention relates to a method of treating cancer in a mammal and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a novel combination comprising the MEK inhibitor: N -{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2,4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d / ]pyrimidin-1 (2H)-yl]phenyl}acetamide, or a pharmaceutically acceptable salt or solvate thereof, and the PI3 kinase inhibitor: 2,4-difluoro-N-{2-(methyloxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridinyl}benzenesulfonamide, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions comprising the same, and methods of using such combinations in the treatment of cancer.

Description

technical field [0001] The present invention relates to methods of treating cancer in mammals, and to combinations useful in such treatment. Specifically, the method involves the inclusion of the MEK inhibitor: N-{3-[3-cyclopropyl-5-[(2-fluoro-4-iodophenyl)amino]-6,8-dimethyl-2, 4,7-trioxo-3,4,6,7-tetrahydropyrido[4,3-d]pyrimidin-1(2H)-yl]phenyl}acetamide, or its pharmaceutically acceptable salt or solvent compounds, and PI3K inhibitors: 2,4-difluoro-N-{2-(methoxy)-5-[4-(4-pyridazinyl)-6-quinolinyl]-3-pyridyl} Novel combinations of benzenesulfonamides or pharmaceutically acceptable salts thereof, pharmaceutical compositions containing the combinations, and methods of using the combinations in the treatment of cancer. Background of the invention [0002] Effective treatment of hyperproliferative diseases, including cancer, has long been a goal of the field of oncology. In general, cancers arise from aberrations in the normal processes that control cell division, differenti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/505
CPCC07D401/14C07D471/04A61P35/00A61P43/00A61K31/519A61K31/505A61K31/501
Inventor K.R.奥格K.E.巴克曼T.M.吉尔默小詹姆斯.G.格雷杰J.D.格雷肖克S.拉奎尔L.刘S.R.莫里斯
Owner GLAXO SMITHKLINE LLC
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