| 摘要 |
COMPOUNDS OF THE FORMULA, (FORMULA I)WHEREIN R1 SIGNIFIES HETEROCYCLYL;R2 SIGNIFIES YDROGEN, LOWER-ALKYL, LOWER-ALKOXY, LOWER-ALKYLTHIO, LOWER-ALKOXY-LOWER-ALKYL, LOWER-ALKYLSULPHONYL-LOWER-ALKOXY, PHENYL, LOWER ALKYLPHENYL, LOWER-ALKOXY-PHENYL, LOWER-ALKYLENE-DIOXYPHENYL, PHENYL-LOWER ALKYL, LOWER ALKYL-PHENYL-LOWER ALKYL, LOWER ALKOXY-PHENYL-LOWER ALKYL, LOWER ALKYLENEDIOXYPHENYL-LOWER ALKYL, HETEROCYCLYL, OR HETEROCYCLYL-LOWER ALKYL;R3 SIGNIFIES LOWER-ALKYL, LOWER-ALKOXY, FORMYL, HALO-LOWER-ALKYL, HYDROXY-LOWER-ALKYL, AMINO-LOWER-ALKYL OR A RESIDUE -CH2O-A- LOWER-ALKYL, -(CH2)M -O-(CRARB)NOH, -(CH2)M-O-(CRARB)NOR9, -(CH2)M-O-(CRARB)NNH2 OR -(CH2)M -O-(CRARB)N-B-R9;R4-R8 SIGNIFY HYDROGEN, LOWER-ALKOXY OR HALOGEN;R9 SIGNIFIES HETEROCYCLYL; PHENYL OR PHENYL SUBSTITUTED BY LOWER-ALKYL, LOWER-ALKOXY AND/OR HALOGEN, OR LOWER-ALKYL;RA AND RB SIGNIFY HYDROGEN OR LOWER-ALKYL;A SIGNIFIES A KETALIZED 1, 2-DIHYDROXY-ETHYLENE GROUP;B SIGNIFIES -OC(O)O-, -O(C(O)NH-, -NH(C(0)NH-OR -NHC(O)O-:N SIGNIFIES 2, 3 OR 4; AND M SIGNIFIES 0 OR 1ARE INHIBITORS FOR ENDOTHELIN RECEPTORS. THEY CAN BE USED FOR THE TREATMENT OF DISORDERS WHICH ARE ASSOCIATED WITH ENDOTHELIN ACTIVITIES, ESPECIALLY CIRCULATORY DISORDERS SUCH AS HYPERTENSION, ISCHAEMIA, VASOSPASMS AND ANGINA PECTORIS.
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