Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors

Inactive Publication Date: 2006-10-12
AVANIR PHARMA
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0006] As MIF has been identified in a variety of tissues and has been associated with numerous pathological events, there exists a need for pharmaceutical compositions comprising MIF inhibitors, as well as methods relating to t

Problems solved by technology

Hence, when its activities / gene expression are overinduced by the administration of excess exogenous glucocorticoids (for example when clinical indicated to suppress inflammation, immunity and the like), there is significant toxicity because MIF itself exacerbates the inflammatory / immune response.

Method used

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  • Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors
  • Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors
  • Thienopyridinone derivatives as macrophage migration inhibitory factor inhibitors

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Embodiment Construction

[0054] The following description and examples illustrate a preferred embodiment of the present invention in detail. Those of skill in the art will recognize that there are numerous variations and modifications of this invention that are encompassed by its scope. Accordingly, the description of a preferred embodiment should not be deemed to limit the scope of the present invention.

[0055] As an aid to understanding the preferred embodiments, certain definitions are provided herein.

[0056] The terms “macrophage migration inhibitory activity”“MIF activity” as used herein is a broad term, and is to be given its ordinary and customary meaning to a person of ordinary skill in the art (and is not to be limited to a special or customized meaning), and refers without limitation to an activity or effect mediated at least in part by macrophage migration inhibitory factor. Accordingly, MIF activity includes, but is not limited to, inhibition of macrophage migration, tautomerase activity (e.g., ...

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Abstract

Inhibitors of macrophage migration inhibitory factor having a thienopyridinone backbone are provided which have utility in the treatment of a variety of disorders, including the treatment of pathological conditions associated with macrophage migration inhibitory factor activity. The inhibitors of macrophage migration inhibitory factor have the following structures: including forms such as stereoisomers, free forms, pharmaceutically acceptable salts or esters thereof, solvates, or combinations of such forms, wherein n, R1, R2, R3, X, and Y are as defined herein. Compositions comprising an inhibitor of macrophage migration inhibitory factor in combination with a pharmaceutically acceptable carrier are also provided, as well as methods for use of the same.

Description

RELATED APPLICATIONS [0001] This application claims the benefit of U.S. Provisional Application No. 60 / 665,236, filed Mar. 24, 2005, and U.S. Provisional Application No. 60 / 733,657, filed Nov. 4, 2005. All above-referenced prior applications are incorporated by reference herein in their entirety and are hereby made a portion of this specification.FIELD OF THE INVENTION [0002] The present invention relates to organic compounds, e.g., thienopyridinone derivatives, that are macrophage migration inhibitory factor (MIF) inhibitors. BACKGROUND OF THE INVENTION [0003] The lymphokine, macrophage migration inhibitory factor (MIF), has been identified as a mediator of the function of macrophages in host defense and its expression correlates with delayed hypersensitivity, immunoregulation, inflammation, and cellular immunity. Although MIF was first characterized as being able to block macrophage migration, MIF also appears to effect macrophage adherence; induce macrophage to express interleuki...

Claims

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Application Information

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IPC IPC(8): A61K31/496C07D498/02
CPCC07D498/02C07D495/04A61P1/04A61P3/10A61P9/10A61P11/00A61P11/06A61P17/00A61P19/02A61P29/00A61P31/04A61P35/00A61P43/00
InventorSIRCAR, JAGADISHK.C., SUNILDAVIS, TIMOTHYYING, WENBIN
OwnerAVANIR PHARMA