| 摘要 |
The compsn. comprises pepstatin (I) together with a cyclobutene-3,4-dione deriv. of formula (II) or its acid-addn. salt, hydrate or solvate, together with a carrier. In the formula R1 and R2 are H or alkyl, or R1 is H and R2 is allyl, proparagyl, cycloalkyl(alkyl) cyanoalkyl, 2-fluoroethyl, 2,2,2-trifluoroethyl, OH, 2,3-dihydroxypropyl, R3R4C6H3(CH2)p or R5-pyridinyl-(CH2)q; p and q are 1-6; R3 and R4 are H, alkyl, OH, alkoxy or halogen; or R3 is H and R4 is CF3; or R3 + R4 form OCH2O; R5 is H, alkyl, alkoxy, OH, NH2 or halogen; m is 0-2; n is 2-5; Z is S, O, or CH2; A is furyl, thienyl, phenyl, or pyridinyl all substd. by R8R9N(CH2)r and by R6- ; R6 is H, alkyl, alkoxy or halogen; r is 1-4; R8 and R9 are H, alkyl, allyl, propargyl, alkoxyalkyl, cycloalkyl or Ph-alkyl; or NR8R9 is pyrrolidino, (di)methyl pyrrolidino, morpholino, thiomorpholino, piperidino, (di)methylpiperidino, hydroxypiperidino, N-methylpiperazino, 1,2,3,6-tetrahydropyridino, 3-pyrrolidono, homopiperidino, hepta- or octa-methyleneimino or 3-azabicyclo (3.2.2)nonane. Cpds. (II) are histamine H2 receptor antagonists and many of them are described in GB2067987 and some cpds. have much greater potency than cimetidine on oral admin. When (II) is administered in compsns. with (I), their potency is increased, so that the effective dosage may be reduced.
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