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Aminobenzimidazole derivatives

A benzo, hydroxybenzamide technology, applied in the directions of drug combination, organic chemistry, organic active ingredients, etc., can solve the problems of difficult to treat cancer, undesired side effects, etc.

Active Publication Date: 2018-12-21
TRANSLATIONAL DRUG DEV LLC
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Cancer is the second leading cause of death in the United States, and while new breakthroughs have led to lower mortality rates, many cancers remain difficult to treat
In addition, many cancers often develop resistance to current chemotherapy over time
Typical treatments such as chemotherapy, radiation therapy and surgery can also cause a wide range of undesired side effects

Method used

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  • Aminobenzimidazole derivatives
  • Aminobenzimidazole derivatives
  • Aminobenzimidazole derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0088] Example 1. Exemplary Compounds of Formula (I) or Formula (II)

[0089] 4-((1-(cyclohexylmethyl)-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#1

[0090]

[0091] 4-((1-cyclohexyl-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID # 2

[0092]

[0093] 4-((1-cycloheptyl-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#3

[0094]

[0095] 4-((1-((1-fluorocyclohexyl)methyl)-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#4

[0096]

[0097] 4-((1-(cyclopentylmethyl)-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#5

[0098]

[0099] 4-((1-(2-cyclopentylethyl)-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#6

[0100]

[0101] 4-((1-((4,4-difluorocyclohexyl)methyl)-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide ID#7

[0102]

[0103] 4-((1-((4,4-difluorocyclohexyl)methyl)-5-fluoro-1H-benzo[d]imidazol-2-yl)amino)-N-hydroxybenzamide. ID#8

[0104]

[0105] N-Hydroxy-4-((1-((tetrahydro-2H-pyran-4-y...

Embodiment 2

[0109] Example 2. Cell viability assay using MM1.S cells

[0110] Cell viability was used to assess cytotoxicity and the effect of compounds on cell proliferation in the presence of various concentrations of the above compounds at different time points. IC of disclosed compounds in MM1.S cell line 50 (or percent activity) data are summarized in Table 1.

[0111] Cell viability assay - by Promega (Madison, WI) The cell viability assay measures cell viability. The luminescent cell viability assay is a homogenous method used to determine the number of surviving cells in culture based on the quantification of the ATP present, which indicates the presence of metabolically active cells. After processing, the Add to treated wells and incubate at 37°C. Luminescence was measured using a Molecular Devices Spectramax microplate reader.

[0112] Single Reagent Studies - Cells were grown to 70% confluency, trypsinized, counted, and plated in 96-well flat-bottom plates at a final...

Embodiment 3

[0122] Example 3. Cell Viability Assay Using Various Cell Lines

[0123] Compound ID #1 (compound of formula (I)) and compound ID #3 (compound of formula (II)) were tested for inhibition of cancer cell proliferation. Cell viability was used to assess cytotoxicity and the effect of compounds on cell proliferation in the presence of various concentrations of Compound ID#1 and Compound ID#3 at different time points. The 50% inhibitory concentration (IC) of the compound 50 ) data are summarized in Table 2. The data clearly show the surprising and unexpected increased anticancer activity associated with Compound ID#1 compared to Compound ID#3.

[0124] Cell viability assay - by Promega (Madison, Wis.) The cell viability assay measures cell viability. The luminescent cell viability assay is a homogenous method used to determine the number of surviving cells in culture based on the quantification of the ATP present, which indicates the presence of metabolically active cells. ...

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PUM

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Abstract

The present invention is directed to aminobenzimidazole derivative compounds and compositions comprising thereof. The present invention also relates to uses of these compounds to treat or prevent several conditions including neoplasia, dysplasia, metaplasia, and cancer.

Description

[0001] Cross References to Related Applications [0002] This application claims priority to U.S. Provisional Patent Application No. 62 / 302,781, filed March 2, 2016, the contents of which are hereby incorporated by reference in their entirety. Background technique [0003] Cancer is the second leading cause of death in the United States, and while new breakthroughs have led to lower mortality rates, many cancers remain difficult to treat. In addition, many cancers often develop resistance to current chemotherapy over time. Typical treatments such as chemotherapy, radiation therapy and surgery also cause a wide range of undesired side effects. Clearly, there is a great need in the field for new compounds and methods that slow the proliferation of cancer cells and which may be useful in the treatment of cancer. Contents of the invention [0004] The present invention provides a compound which can effectively treat cancer. [0005] An object of the present invention is to pr...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D235/30C07D401/04C07D403/04
CPCC07D405/06C07D235/30A61P35/00A61K31/454A61K31/573C07D401/04C07D403/04A61K2300/00
Inventor T·王S·盖特利
Owner TRANSLATIONAL DRUG DEV LLC
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