| 摘要 |
<p>Certain 1-(substituted amino)-2-(amino or substituted amino) cyclobutene-3,4-diones are potent histamine H2-antagonlsts useful in the treatment of peptic ulcers. Compounds of the formula -IMAGE- I wherein R1 and R2 each are independently hydrogen or (lower)alkyl, and, when R1 is hydrogen, R2 also may be allyl, propargyl, cyclo(lower)alkyl(lower)alkyl, cyclo(lower)alkyl, cyano(lower)alkyl, 2-fluoroethyl, 2,2,2-trifluoroethyl, hydroxy, 2,3-dihydroxypropyl, -IMAGE- or -IMAGE-in which p is an integer of from 1 to 6 inclusive, q is an integer of from 1 to 6 inclusive, R3 and R4 each are independently hydrogen, (lower)alkyl, hydroxy, (lower)alkoxy or halogen, and, when R3 is hydrogen, R4 also may be trifluoromethyl, or R3 and R4, taken together, may be methylenedioxy, R is hydrogen, m is an integer of from 0 to 2 inclusive; n is an integer of from 2 to 5 inclusive; Z is sulfur, oxygen or methylene; and A is -IMAGE- -IMAGE- or -IMAGE-in which R6 is hydrogen, (lower)alkyl, (lower)alkoxy or halogen; r is an integer of from 1 to 4 inclusive; and R8 and R9 each are independently hydrogen, (lower)alkyl, allyl, propargyl, (lower)alkoxy(lower)alkyl in which the (lower)alkoxy moiety is at least two carbon atoms removed from the nitrogen atom, cyclo(lower)alkyl, or phenyl(lower)alkyl, provided that R8 and R9 may not both be cyclo(lower)alkyl, or R8 and R9, taken together with the nitrogen atom to which they are attached, may be pyrrolidino, methylpyrrolidino, dimethylpysrolidino, morphollno, thiomorpholino, piperidino, methylpiperidino, dimethylpiperidino, hydroxypiperidino, N-methyl-piperazino, 1,2,3,6-tetrahydropyrldyl, 3-pyrrolino, homopiperidino, heptamethyleneimino, octamethyleneimino or 3-azabicyclo¢3.2.2!-nonane; or a nontoxic, pharmaceutically acceptable salt, hydrate or solvate thereof are described.</p> |
