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Azoles as malonyl-COA decarboxylase inhibitors useful as metabolic modulators

A carboxyl group and substituent technology, applied in metabolic diseases, medical preparations containing active ingredients, blood diseases, etc.

Inactive Publication Date: 2008-04-23
CHUGAI PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The design of MCD inhibitors for the treatment of cardiovascular disease, diabetes, cancer or obesity has not been reported in the prior art literature

Method used

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  • Azoles as malonyl-COA decarboxylase inhibitors useful as metabolic modulators
  • Azoles as malonyl-COA decarboxylase inhibitors useful as metabolic modulators
  • Azoles as malonyl-COA decarboxylase inhibitors useful as metabolic modulators

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preparation example Construction

[0144] Preparation of compounds of the present invention

[0145] The starting materials used in the preparation of the compounds of the present invention are known and can be obtained by known methods or are commercially available. Methods for preparing precursors and functional groups of the claimed compounds are known to those of ordinary skill and generally described in the literature. Those of ordinary skill can prepare these compounds according to the literature or published publications.

[0146]It is understood that the operations can be readily performed by one of ordinary skill in the art of organic chemistry without further indications, ie, are within the purview and practice of such persons. These manipulations include reduction of carbonyl compounds to the corresponding alcohols, reduction of alkylated amines, oxidation, acylation, aromatic substitution (electrophilic and nucleophilic reactions), etherification, esterification and saponification, among others. T...

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PUM

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Abstract

The present invention relates to methods of treatment of certain metabolic diseases, and to novel compounds and their prodrugs, and / or pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds useful in treating such diseases. In particular, this invention relates to the use of novel compounds and compositions for treatment of cardiovascular diseases, diabetes, cancers, acidosis, and obesity through the inhibition of malonyl-CoA decarboxylase (MCD). These compounds have the formulae (I) and (II), wherein Y, C, R1, R2, R6, and R7 are defined herein.

Description

[0001] This application claims the benefit of Provisional Application No. 60 / 270034, filed February 20, 2001, the entire disclosure of which is incorporated herein by reference. field of invention [0002] The present invention relates to methods for treating certain metabolic diseases, novel compounds and their prodrugs and / or pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing these compounds for treating the above diseases. In particular, the present invention relates to the use of novel compounds and compositions for preventing, treating or treating cardiovascular diseases, diabetes, cancer and obesity by inhibiting malonyl-CoA decarboxylase (MCD). Background technique [0003] In vivo, malonyl-CoA is an important metabolic intermediate produced by acetyl-CoA carboxylase (ACC). Malonyl-CoA is a substrate for fatty acid synthase (FAS) in liver, adipocytes, and other tissues. ACC and malonyl-CoA were found to be present in skeletal and ca...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D277/70C07D513/04A61K31/425A61P9/10A61P3/10C07D277/72A61K31/423A61K31/426A61K31/427A61K31/428A61K31/4353A61K31/4439A61K31/454A61K31/496A61K31/519A61K31/5377A61K31/541A61P3/00A61P3/04A61P3/06A61P3/08A61P7/00A61P9/00A61P9/04A61P35/00A61P43/00C07D277/20C07D277/36C07D277/56C07D277/82C07D409/12C07D417/12
CPCA61K31/454A61K31/496A61K31/425A61K31/5377A61K31/428A61K31/541A61K31/423A61K31/426A61P3/00A61P3/04A61P35/00A61P3/06A61P3/08A61P43/00A61P7/00A61P9/00A61P9/04A61P9/10A61P3/10C07D513/04
Inventor 托马斯·阿尔赫尼厄斯程杰飞马克·威尔逊罗西·塞拉菲莫夫
Owner CHUGAI PHARMA CO LTD
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