- Method of diminishing the adverse effects of interleukin-2
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A method and composition for preserving or enhancing the beneficial effects of interlude-2 (IL-2) while simultaneously mitigating the adverse effects of IL-2 on a subject is disclosed. The method involves administering an amount of a leukotriene B4 (LTB4) antagonist, preferably a LTB4 receptor antagonistic, to a subject exhibiting adverse pharmacological effects due to exogenous IL-2, where the amount administered to the subject is sufficient to decrease the IL-2 induces adverse effects. Also disclosed is an article of manufacturing comprising a composition of the leukotriene B4 antagonist in combination with labeling instructions for treatment. Also disclosed is a method for preparing a pharmaceutical composition. Generally the LTB4 antagonist will reduce the IL-2-induced adverse effects while preserving or enhancing the anti tumor, antiviral, or immunostimulatory effects of IL-2, thereby improving the therapeutic index of IL-2.
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- Method of diminishing the adverse effects of interleukin-2
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A method and composition for preserving or enhancing the beneficial effects of interleukin-2 (IL-2) while simultaneously mitigating the adverse effects of IL-2 on a subject is disclosed. The method involves administering an amount of a leukotriene B4 (LTB4) antagonist, preferably a LTB4 receptor antagonistic, to a subject exhibiting adverse pharmacological effects due to exogenous IL-2, where the amount administered to the subject is sufficient to decrease the IL-2 induces adverse effects. Also disclosed is an article of manufacturing comprising a composition of the leukotriene B4 antagonist in combination with labeling instructions for treatment. Also disclosed is a method for preparing a pharmaceutical composition. Generally the LTB4 antagonist will reduce the IL-2-induced adverse effects while preserving or enhancing the antitumor, antiviral, or immunostimulatory effects of IL-2, thereby improving the therapeutic index of IL-2.
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- Leukotriene B4 antagonists
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This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof STR1 wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl; R1 is alkyl; R2 represents alkyl from 1 to 5 carbon a
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- ALKOXY-SUBSTITUTED DIHYDROBENZOPYRAN-2-SULFONIMIDES
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This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof STR1 wherein R is alkyl, alkenyl, alkynyl, or (CH 2) m R 3 where R. sup.3 is cycloalkyl and m is 1 or 2;R 1 is alkyl; R 2 is alkyl, aryl or aryl substituted with halogen or alkyl; R 4 is alkyl;n is an integer from 1 to 5;p is an integer from 0 to 6; Y is NH, oxygen or sulfur; andZ is hydrogen, alkyl, alkoxy, NR 6 R 5 wherein R 6 and R 5 are independently hydrogen or alkyl, or SR 7 wherein R 7 is hydrogen, benzyl or alkyl.The compounds of Formula I are leukotriene B 4 antagonists and are useful as anti-inflammatory agents and in the treatment of leukotriene B 4 mediated conditions.
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- LEUKOTRIENE B4 ANTAGONISTS
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This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof STR1 wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl;R 1 is alkyl; R 2 is hydrogen, alkyl;R 6 is alkyl;
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- Alkoxy-substituted dihydrobenzopyran-2-carboxylic acids and derivatives thereof, compositions and use
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This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof STR1 wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl and m is 1 or 2; R1 is alkyl of 1 to 4 carbon atoms; R2/sup
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- Alkoxy-substituted dihydrobenzopyran-2-carboxylic acids and derivatives thereof
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This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof STR1 wherein R is alkyl, alkenyl, alkynyl, or (CH2)m R3 where R3 is cycloalkyl and m is 1 or 2
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- Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives.
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This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. wherein R1 represents alkyl having 2-6 carbon atoms; R2 represents methyl or ethyl; R3 represents alkyl having 1 to 5 carbon atoms; W represents (CH?)x where x is 2 to 7, alkylene having 2 to 7 carbon atoms, alkenylene having 3 to 7 carbon atoms, alkynylene having 3 to 7 carbon atoms, or cyclopentyl; R? represents hydrogen, alkyl having 2-5 carbon atoms, alkenyl having 2 to 5 carbon atoms, or alkynyl having 2 to 5 carbon atoms; Q represents oxygen or CH?; B represents CH?, C=O or CH-OH; R? represents hydrogen, alkyl having 1 to 6 carbon atoms, or R? and R? together optionally represent a carbon to carbon bond; or R? represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH?)y-CO?R? wherein y is 0 to 4 and R? is hydrogen or alkyl having 1 to 6 carbon atoms; and A represents-Z-CO?R? or-Z-COR?R1? wherein R? represents hydrogen or alkyl having 1 to 6 carbon atoms, R?, R1?, represent hydrogen, alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms or NR?R1? form a heterocyclic ring, and wherein Z is absent or represents straight or branched chain alkylene or alkenylene having up to 6 carbon atoms.These compounds are selective antagonists of leukotriene B?(LTB?) with little or no antagonism of leukotriene D? (LTD?) and are useful anti-inflammatory agents for treating inflammatory bowel disease, rheumatoid arthritis, gout and psoriasis.
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- Alkoxy-substituted dihydrobenzopyran-2-carboxylate derivatives
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This invention encompasses compounds of Formula 1 and the pharmaceutically acceptable salts thereof. STR1 wherein R1 represents alkyl having 2-6 carbon atoms; R2 represents methyl or ethyl; R3 represents alkyl having 1 to 5 carbon atoms; W represents (CH2)x where x is 2 to 7, alkylene having 2 to 7 carbon atoms, alkenylene having 3 to 7 carbon atoms, alkynylene having 3 to 7 carbon atoms, or cyclopentyl; R4 represents hydrogen, alkyl having 2-5 carbon atoms, alkenyl having 2 to 5 carbon atoms, or alkynyl having 2 to 5 carbon atoms; Q represents oxygen or CH2 ; B represents CH2, C=O or CH--OH; R5 represents hydrogen, alkyl having 1 to 6 carbon atoms, or R5 and R6 together optionally represent a carbon to carbon bond; or R5 represents alkanoyl having 2 to 4 carbon atoms, carboxy, alkoxycarbonyl, or (CH2)y--CO2 R8 wherein y is 0 to 4 and R8 is hydrogen or alkyl having 1 to 6 carbon atoms; and A represents --Z--CO2 R7 or --Z--COR9 R10 wherein R7 represents hydrogen or alkyl having 1 to 6 carbon atoms, R9, R10, represent hydrogen, alkyl having 1 to 6 carbon atoms, or cycloalkyl having 3 to 6 carbon atoms or NR9 R10 form a heterocyclic ring, and wherein Z is absent or represents straight or branched chain alkylene or alkenylene having up to 6 carbon atoms. These compounds are selective antagonists of leukotriene B4 (LTB4) with little or no antagonism of leukotriene D4 (LTD4) and are useful anti-inflammatory agents for treating inflammatory bowel disease, rheumatoid arthritis, gout and psoriasis.
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