US 2007/0185196 A1Published application

Inhibitionof bid-induced cell-death using small organic moleculeus

AssigneeThe Burnham Institute

InventorsJohn Reed, Maurizio Pellecchia

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Abstract

Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.

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Claims27

Dependent claims

A compound having the formula (A):

wherein each of R1 and R2 is independently selected from a group consisting of:
Y is a moiety selected from a group consisting of:
X is a moiety selected from a group consisting of:
R3 is at least one substitutent in ortho-, meta-, or para-position of the benzene ring, wherein “(R3)1-5” symbolizes that the number of R3 substitutents is between 1 and 5, inclusively, wherein R3 is selected from a group consisting of:
n is an integer having the value between 1 and 5;
and
Ph in any of R1, R2, and R3 is independently selected from an unsubstituted phenyl ring and a substituted phenyl ring having between one and five substitutents in ortho-, meta-, or para-position of the benzene ring, wherein the substitutents in the ring are selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.

5 more elements

Dependencies are inferred from the claim text.

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Abstract

Various phenylamine derivatives are described as well as the use of compounds to inhibit BID protein for controlling apoptotic cascade.

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Drawings

Claims27

Dependent claims

A compound having the formula (A):

wherein each of R1 and R2 is independently selected from a group consisting of:
Y is a moiety selected from a group consisting of:
X is a moiety selected from a group consisting of:
R3 is at least one substitutent in ortho-, meta-, or para-position of the benzene ring, wherein “(R3)1-5” symbolizes that the number of R3 substitutents is between 1 and 5, inclusively, wherein R3 is selected from a group consisting of:
n is an integer having the value between 1 and 5;
and
Ph in any of R1, R2, and R3 is independently selected from an unsubstituted phenyl ring and a substituted phenyl ring having between one and five substitutents in ortho-, meta-, or para-position of the benzene ring, wherein the substitutents in the ring are selected from the group consisting of:
or a pharmaceutically acceptable salt thereof.

5 more elements

Dependencies are inferred from the claim text.

Description8,287 words

Summary955 words

#1. Field of the Invention

#The present invention relates generally to the use of compounds to treat a variety of disorders, diseases and pathologic conditions and more specifically to the use of phenylamine derivatives to treat various disorders.

#2. Background Information

Brief description of the drawings12 figures

#FIG. 1 is a scheme illustrating the process of cell death induced by BID.

#FIG. 2 demonstrates spectral intra- and inter-ligand based identification of some compounds that bind BID.

#FIG. 3 provides microphotographs demonstrating binding to BID by chemical shift mapping.

Detailed description7,142 words

#The following terms, definitions and abbreviations apply:

#The general terms “alkyl,” “alkoxy,” “alkenyl,” and “alkynyl” refer to both straight-chain and branched groups; references to individual radicals include specifically either straight-chain or branched groups, but not both. For instance, a reference to “propyl” includes only the straight-chain radical while a reference to “isopropyl” includes only the branched group.

#The term “alkyl” refers to a monovalent straight or branched chain hydrocarbon group. Examples of alkyl structures that can be used include (C1-C6)alkyls such as be methyl, ethyl, propyl, isopropyl, butyl, isobutyl, sec-butyl, tert-butyl, pentyl, 3-pentyl, or hexyl.

Abstract

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Claims27

Abstract

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Claims27

Description8,287 words

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Classification9 codes

Life of this patent

Description8,287 words