Arylhydroxamates useful as antiallergy agents
First Claim
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1. A compound having the structure ##STR72## wherein R1 is lower alkyl, aryl, lower alkenyl aralkyl, or ##STR73## wherein n is 2 to 4 and X is hydroxy, alkoxy, amino, C1 -C4 -alkylamino or C1 -C4 -dialkylamino;
- R2 is hydrogen or lower alkyl; and
R3 is C1 -C20 alkyl, C3 -C20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy, aryloxy or cycloalkyloxy, including pharmaceutically acceptable monobasic and dibasic salts whereof, and wherein the term alkyl by itself or as part of another group is unsubstituted or substituted with a substituent which is a halo, trifluoromethyl, alkoxy, aryl, alkyl-aryl, haloaryl, cycloalkyl, alkylcycloalkyl, hydroxy, alkylamino, alkanoylamino, arylcarbonylamino, nitro, cyano, thiol or an alkylthio substituent,the term aryl by itself or as part of another group is unsubstituted or substituted with 1 or 2 halogens, 1 or 2 lower alkyl groups, 1 or 2 lower alkoxy groups, an aryl group, 1 or 2 hydroxyls, 1 or 2 alkylamino groups, 1 or 2 alkanoylamino groups, 1 or 2 arylcarbonylamino groups, 1 or 2 amino groups, 1 or 2 nitro groups, 1 or 2 cyano groups, 1 or 2 thiol groups and/or 1 or 2 alkythio groups; and
the term cycloalkyl by itself or as Part of another group is unsubstituted or substituted with 1 or 2 halogens 1 or 2 lower alkyl groups, 1 or 2 alkoxy groups, an aryl group, 1 or 2 hydroxyls, 1 or 2 alkylamino groups, 1 or 2 alkanoylamino, 1 or 2 arylcarbonylamino groups, 1 or 2 amino groups, 1 or 2 nitro groups, 1 or 2 cyano groups, 1 or 2 thiol groups and/or 1 or 2 alkylthio groups.
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Abstract
Arylhydroxamates are provided having the structure ##STR1## wherein R1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C1 -C4 -alkylamino or C1 -C4 -dialkylamino.
R2 is hydrogen or lower alkyl; and
R3 is C1 -C20 alkyl or C3 -C20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy.
These compound are useful as inhibitors of Δ5 -lipoxygenase and as such are useful as antiallergy agents.
29 Citations
33 Claims
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1. A compound having the structure ##STR72## wherein R1 is lower alkyl, aryl, lower alkenyl aralkyl, or ##STR73## wherein n is 2 to 4 and X is hydroxy, alkoxy, amino, C1 -C4 -alkylamino or C1 -C4 -dialkylamino;
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R2 is hydrogen or lower alkyl; and R3 is C1 -C20 alkyl, C3 -C20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy, aryloxy or cycloalkyloxy, including pharmaceutically acceptable monobasic and dibasic salts whereof, and wherein the term alkyl by itself or as part of another group is unsubstituted or substituted with a substituent which is a halo, trifluoromethyl, alkoxy, aryl, alkyl-aryl, haloaryl, cycloalkyl, alkylcycloalkyl, hydroxy, alkylamino, alkanoylamino, arylcarbonylamino, nitro, cyano, thiol or an alkylthio substituent, the term aryl by itself or as part of another group is unsubstituted or substituted with 1 or 2 halogens, 1 or 2 lower alkyl groups, 1 or 2 lower alkoxy groups, an aryl group, 1 or 2 hydroxyls, 1 or 2 alkylamino groups, 1 or 2 alkanoylamino groups, 1 or 2 arylcarbonylamino groups, 1 or 2 amino groups, 1 or 2 nitro groups, 1 or 2 cyano groups, 1 or 2 thiol groups and/or 1 or 2 alkythio groups; and the term cycloalkyl by itself or as Part of another group is unsubstituted or substituted with 1 or 2 halogens 1 or 2 lower alkyl groups, 1 or 2 alkoxy groups, an aryl group, 1 or 2 hydroxyls, 1 or 2 alkylamino groups, 1 or 2 alkanoylamino, 1 or 2 arylcarbonylamino groups, 1 or 2 amino groups, 1 or 2 nitro groups, 1 or 2 cyano groups, 1 or 2 thiol groups and/or 1 or 2 alkylthio groups. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33)
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11. The compound as defined in claim I having the name, (Z)-4-[[4-(1-decenyl)benzoyl]methoxyamino]butanoic acid or its dicyclohexylamine salt(1:
- 1) including all stereoisomers thereof.
Specification
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Current AssigneeE R Squibb & Sons Incorporated
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Original AssigneeE R Squibb & Sons Incorporated
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InventorsKaranewsky, Donald S., Haslanger, Martin F.
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Primary Examiner(s)EVANS, JOSEPH
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Application NumberUS06/719,935Time in Patent Office502 DaysField of Search260/500.5 H, 260/501.1, 260/501.11, 260/453 RW, 514/575, 514/555, 560/20, 560/312, 562/452US Class Current514/575CPC Class CodesC07C 63/04 Monocyclic monocarboxylic a...C07C 65/24 polycyclicC07C 65/26 containing rings other than...C07C 65/28 having unsaturation outside...
