A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
167/205
A61K 31/20 (2006.01)
Patent
CA 1041012
Abstract of the Disclosure A method is disclosed for inhibiting and alleviating gastrointestinal side effects often encountered during thera?y with antiinflammatory agents such as indomethacin, phenyl- butazone, oxyphenylbutazone, ibuprofen, mefenamic acid, ?lufenamic acid, naproxen, and the like. The method comprises the administration to a mammal receiving such therapy of a prostaglandin derivative of formula I, Image I in which (a) W is C = O, X and Y each are single bonds, Z is either C = O, CHOH or C(CH3)OH, R1 and R2 each are hydrogen, R3 is (CH2)3CH3, R4 is hydrogen or lower alkyl and R5 is hydrogen; (b) W is CHOH, X and Y each are single bonds, Z is either CHOH or C(CH3)OH, R1 and R2 each are hydrogen, R3 is (CH2)3CH3, R4 is hydrogen or lower alkyl and R5 is hydrogen; (c) W is C = O, X is a single bond, Y is a trans double bond, Z is CH2, CHOH or C(CH3)OH, R1 and R2 each are hydrogen and R3 is (CH2)3CH3, R4 is hydrogen or lower alkyl and R5 is hydrogen; (d) W is C = O, X is a single bond, Y is a trans double bond, Z is CHOH, R1 and R2 each are hydrogen, R3 is -1- cyclohexyl, R4 is hydrogen or lower alkyl and R5 is hydrogen; (e) W is C = O, X is a cis double bond, Y is a trans double bond, Z is CHOH, or C(CH3)OH, R1 is hydrogen and R2 is hydrogen or methyl, R3 is (CH2)3CH3, R4 is hydrogen or lower alkyl and R5 is hydrogen; (f) W is C = O, X is a cis double bond, Y is a trans double bond, Z is CHOH, R1 and R2 each are methyl, R3 is (CH2)3CH3, R4 is hydrogen or lower alkyl and R5 is hydrogen; (g) W is C = O, X is a cis double bond, Y is trans double bond, Z is CHOH, R1 and R2 each are hydrogen or methyl, R3 is (CH2)3, R4 is hydrogen or lower alkyl and R5 is hydroxyl; or (h) W is C = O, X is a cis double bond, Y is a trans double bond, Z is C(CH3)OH, R1 and R2 each are hydrogen, R3 is (CH2)3, R4 is hydrogen or lower alkyl and R5 is hydroxyl. Also disclosed are useful pharmaceutical compositions for treating inflammatory conditions comprising a combination of a gastrointestinal side effect-inhibiting dose of the above prostaglandin derivative of formula I and a therapeutic dose of an antiinflammatory agent. -2-
204494
Lippmann Wilbur
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