Novel compounds, pharmaceutical compositions containing same, and methods of use for same

A compound and alkyl technology, applied to new compounds, pharmaceutical compositions containing the compounds and the application fields of the compounds, can solve the problems of sensitivity to inhibition and the like

Inactive Publication Date: 2010-01-27
FASGEN +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it has been found that administration of type I fatty acid synthesis inhibitors to such microbial cells renders them more susceptible to inhibition by inhibitors of downstream fatty acid processing and / or application

Method used

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  • Novel compounds, pharmaceutical compositions containing same, and methods of use for same
  • Novel compounds, pharmaceutical compositions containing same, and methods of use for same
  • Novel compounds, pharmaceutical compositions containing same, and methods of use for same

Examples

Experimental program
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Embodiment

[0112] The invention is illustrated, but not limited, by the following examples.

[0113] A series of compounds according to the present invention were synthesized as described below. The biological activities of certain compounds are described below: Compounds tested: (1) Inhibition of purified human FAS, (2) Inhibition of fatty acid synthesis activity in whole cells, (3) Cytotoxicity against cultured MCF-7 human breast cancer cells , such cells are known to have high levels of FAS and fatty acid synthesis activity, using crystal violet and XTT assays, and (4) antimicrobial activity. Compounds with low levels of cytotoxicity were selected and then tested for weight loss in Bal b / C mice. In addition, representative compounds from the group exhibiting significant body weight loss and low levels of cytotoxicity were tested in Balb / C mice for fatty acid oxidation, and carnitine palmitoyltransferase-1 (CPT-1) activity, as well as by Northern analysis. Effects of hypothalamic NPY...

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PUM

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Abstract

The present invention relates to a new compound, pharmaceutical composition comprising the new compound and using method of the compound, the structure of the compound is disclosed in the description. The compound of the present invention has the functions of weight loss, anti-microbial and anti-cancer applications, inhibition of fatty acid synthase and neuropeptide-Y, and the stimulation of the activity of carnitine palmitoyl transferase-1.

Description

[0001] This application is a divisional application of a Chinese patent application with the application number 03818369.2, the application date being July 1, 2003, and the same invention title. Background technique [0002] fatty acid synthase [0003] Fatty acids have three main roles in cellular physiology. First, they are the building blocks of biological membranes, and second, fatty acid derivatives function as hormones and intracellular messengers. Third, and which is of particular importance to the present invention, fatty acids are fuel molecules that can be stored in adipose tissue in the form of triacylglycerols, also known as neutral fats. [0004] There are four important enzymes involved in the fatty acid synthesis pathway: fatty acid synthase (FAS), acetyl-CoA carboxylase (ACC), malic enzyme, and citrate lyase. The main enzyme: FAS, catalyzes the NADPH-dependent condensation of the precursors malonyl-CoA and acetyl-CoA to produce fatty acids. NADPH is a reduc...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D307/33C07D307/68A61K31/341A61P3/04A61P35/00A61P31/00A61P43/00
CPCC07D307/68C07D307/33C07D307/58A61P25/00A61P3/00A61P3/04A61P31/00A61P35/00A61P43/00C07D307/32
Inventor F·P·库哈蒂亚S·M·麦德豪驰J·N·苏帕里C·A·唐森德J·M·麦克法顿
Owner FASGEN
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