2-pyridinamine compositions and related methods
OwnerElfrida R. Grant, Frank K. Brown +4inventors
InventorsElfrida R. Grant, Frank K. Brown, Robert Allan Zivin, Michael McMillian, Zhong Zhong, Daniel Benjamin
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Abstract
This invention provides neuroprotective pharmaceutical compositions comprising 2-pyridinamines. This invention also provides methods of using these compositions to prevent ischemic cell death, particularly neuronal cell death, and reduce the likelihood of neuronal cell death in a subject due to a traumatic event. Finally, this invention provides an apparatus for administering to a subject the instant pharmaceutical compositions.
Claims45
A pharmaceutical composition comprising a pharmaceutically acceptable carrier and a compound having the formula
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- or a pharmaceutically acceptable salt thereof, wherein
- (a) R1 is H or a substituent bound at either the 5 or 6 ring position and selected from the group consisting of alkyl, alkenyl, alkynyl, thienyl, furanyl, pyrrolyl, phenyl, pyrimidinyl, substituted pyrimidinyl, pyridinyl, substituted pyridinyl, phenyl alkenyl, substituted phenyl alkenyl, benzo[b]thien-2-yl, 2-benzofuranyl and substituted phenyl,
- said substituted phenyl having the formula
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- wherein (i) R6 is selected from the group consisting of H, OH, halogen, alkylamino, dialkylamino, hydroxy-substituted dialkyl amino, lower alkyl, acidic lower alkyl, alkoxy, halogen-substituted lower alkoxy, phenyl and morpholinyl, and (ii) R7 represents between one and four substituents which may be the same or different and are selected from the group consisting of H, halogen, amino, alkyl, lower alkyl, halogen-substituted lower alkyl, alkylamino, dialkylamino, acidic lower alkoxy, alkoxy, halogen-substituted lower alkoxy, alkoxy and phenylalkoxy, with the proviso that R6 and R7 may be fused to form 2-naphthyl or 1,3, benzodioxolyl;
- (b) Each R2 is independently H or lower alkyl;
- (c) Each R3 is independently selected from the group consisting of H, lower alkyl, amino, alkylamino, dialkylamino and lower alkoxy;
- (d) R4 is H, alkoxy or morpholinyl, with the proviso that R4 may be fused with R3 to form 2,3-dihydro-1,4-benzodioxinyl or 9-alkyl 9H carbazolyl;
- and
- (e) R5 is H or lower alky.
5 The pharmaceutical composition of claim 1, wherein R1 is at the 6 ring position, and each R2 is H.
The pharmaceutical composition of claim 5, wherein each R3 and R4 are lower alkoxy.
Dependencies are inferred from the claim text.