Analgesic and anti-inflammatory compositions comprising xanthines and methods of using same
First Claim
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1. A method of eliciting an onset hastened and enhanced analgesic and anti-inflammatory response in a mammalian organism in need of such treatment, comprising administering to such organism:
- (i) an analgesically and anti-inflammatorily effective amount of benoxaprofen, flurbiprofen, fenbufen, ketoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen, bucloxic acid, or pharmaceutically acceptable salts thereof, and(ii) an amount of xanthine derivative sufficient to hasten the onset of and enhance the analgesic and anti-inflammatory response of component (i), said xanthine derivative having the formula;
##STR61## or a pharmaceutically acceptable non-toxic salt thereof wherein R1 -R3, inclusive, independently represent hydrogen, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 haloalkyl, C3 -C6 cycloalkyl, hydroxy (C1 -C6)alkyl, halogen, hydroxy(C1 -C4)alkylamino(C1 -C4)alkyl, C1 -C4 (dialkyl)amino(C1 -C4)alkyl, C1 -C4 alkylcarbonyl(C1 -C4)alkyl, C1 -C6 alkylamino, C1 -C6 (dialkyl)amino, indolyl, phenyl or allyl;
R4 is hydrogen, C1 -C6 alkyl, halo(C1 -C6)alkyl, C1 -C6 alkylamino, C1 -C6 alkylthio, nitro, carboxy C1 -C6 (dialkyl)amino, C3 -C6 cycloalkyl, phenyl, naphthyl, ar(C1 -C4)alkyl, or a group of the formula ##STR62## where R5 is halo, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 alkylthio, nitro or C1 -C6 alkylamino, and n is 1, 2 or 3with the proviso that R1, R2 and R3 cannot all be C1 alkyl when R4 is hydrogen.
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Abstract
Novel analgesic and anti-inflammatory compositions of matter for use in eliciting an analgesic or anti-inflammatory response, said compositions comprising xanthine together with a selected non-narcotic analgesic/nonsteroidal anti-inflammatory drug or a selected narcotic analgesic, or both, are disclosed. When used in combination with the selected drugs, such xanthine enhances the analgesic or anti-inflammatory response and also hastens its onset.
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Citations
75 Claims
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1. A method of eliciting an onset hastened and enhanced analgesic and anti-inflammatory response in a mammalian organism in need of such treatment, comprising administering to such organism:
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(i) an analgesically and anti-inflammatorily effective amount of benoxaprofen, flurbiprofen, fenbufen, ketoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen, bucloxic acid, or pharmaceutically acceptable salts thereof, and (ii) an amount of xanthine derivative sufficient to hasten the onset of and enhance the analgesic and anti-inflammatory response of component (i), said xanthine derivative having the formula;
##STR61## or a pharmaceutically acceptable non-toxic salt thereof wherein R1 -R3, inclusive, independently represent hydrogen, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 haloalkyl, C3 -C6 cycloalkyl, hydroxy (C1 -C6)alkyl, halogen, hydroxy(C1 -C4)alkylamino(C1 -C4)alkyl, C1 -C4 (dialkyl)amino(C1 -C4)alkyl, C1 -C4 alkylcarbonyl(C1 -C4)alkyl, C1 -C6 alkylamino, C1 -C6 (dialkyl)amino, indolyl, phenyl or allyl;R4 is hydrogen, C1 -C6 alkyl, halo(C1 -C6)alkyl, C1 -C6 alkylamino, C1 -C6 alkylthio, nitro, carboxy C1 -C6 (dialkyl)amino, C3 -C6 cycloalkyl, phenyl, naphthyl, ar(C1 -C4)alkyl, or a group of the formula ##STR62## where R5 is halo, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 alkylthio, nitro or C1 -C6 alkylamino, and n is 1, 2 or 3 with the proviso that R1, R2 and R3 cannot all be C1 alkyl when R4 is hydrogen. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
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17. A pharmaceutical composition of matter adapted to elicit an onset hastened and enhanced analgesic and anti-inflammatory response in a mammalian organism in need of such treatment, said composition comprising:
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(i) an analgesically and anti-inflammatorily effective amount of benoxaprofen, flurbiprofen, fenbufen, ketoprofen, pirprofen, carprofen, oxaprozin, pranoprofen, miroprofen, tioxaprofen, suprofen, alminoprofen, tiaprofenic acid, fluprofen, bucloxic acid, or pharmaceutically acceptable salts thereof, and (ii) an amount of xanthine derivative sufficient to hasten the onset of and enhance the analgesic and anti-inflammatory response of component (i), said xanthine derivative having the formula;
##STR63## or a pharmaceutically acceptable non-toxic salt thereof wherein R1 -R3, inclusive, independently represent hydrogen, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 haloalkyl, C3 -C6 cycloalkyl, hydroxy(C1 -C6)alkyl, halogen, hydroxy(C1 -C4)alkylamino(C1 -C4)alkyl, C1 -C4 (dialkyl)amino(C1 -C4)alkyl, C1 -C4 alkylcarbonyl(C1 -C4)alkyl, C1 -C6 alkylamino, C1 -C6 (dialkyl)amino, indolyl, phenyl or allyl;R4 is hydrogen, C1 -C6 alkyl, halo(C1 -C6)alkyl, C1 -C6 alkylamino, C1 -C6 alkylthio, nitro, carboxy C1 -C6 (dialkyl)amino, C3 -C6 cycloalkyl, phenyl, naphthyl, ar(C1 -C4)alkyl, or a group of the formula ##STR64## where R5 is halo, C1 -C6 alkyl, C1 -C6 alkoxy, C1 -C6 alkylthio, nitro or C1 -C6 alkylamino and n is 1, 2 or 3, with the proviso that R1, R2 and R3 cannot all be C1 alkyl when R4 is hydrogen. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, 30, 31, 32, 33, 34, 35, 36, 37, 38, 39, 40, 41, 42, 43, 44, 45, 46, 47, 48, 49, 50, 51, 52, 53, 54, 55, 56, 57, 58, 59, 60, 61, 62, 63, 64, 65, 66, 67, 68, 69, 70, 71, 72, 73, 74, 75)
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Specification
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Current AssigneeAnalgesic Associates
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Original AssigneeAnalgesic Associates
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InventorsLaska, Eugene M., Sunshine, Abraham, Siegel, Carole E.
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Primary Examiner(s)Friedman, Stanley J.
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Application NumberUS06/560,460Time in Patent Office778 DaysField of Search424/317, 424/253US Class Current514/263.31CPC Class CodesA61K 2300/00 Mixtures or combinations of...A61K 31/19 Carboxylic acids, e.g. valp...A61K 31/40 having five-membered rings ...A61K 31/52 Purines, e.g. adenineA61K 31/54 having six-membered rings w...A61K 31/60 Salicylic acid; Derivatives...A61K 45/06 Mixtures of active ingredie...
