| 摘要 |
THE PRESENT INVENTION RELATES TO THERAPEUTIC BIARYL DERIVATIVES OF FORMULA (1), AND PHARMACEUTICALLY ACCEPTABLE DERIVATIVES THEREOFFORMULA 1WHEREIN R1 IS A PHENYL, NAPHTHYL, PYRIDYL, THIAZOLYL, PHENOXYMETYYL, OR PYRIMIDYL GROUP, OPTIONALLY SUBSTITUTED BY ONE OR MORE SUBSTITUENTS SELCETED FORM THE GROUP CONSISTING OF HALOGEN, HYDROXY, C1-6ALKOXY, C1-6ALKYL, NITRO, CYANO, HYDROXYMETHYL, TRIFLUOROMETHYL, -NR6R6, AND -NHSO2R6, WHERE EACH R6 IS INDEPENDENTLY HYDROGEN OR C1-4ALKYL;R2 IS HYDROGEN OR C1-6ALKYL;X IS OXYGEN, SULFUR, -NH, OR NC 1-4ALKYL;R3 IS CYANO, TETRAZOL-5-YL, OR-R7 IS HYDROGEN OR C1-6AKLYL;R4 AND R5 ARE INDEPENDENTLY HYDROGEN, C1-6 ALKYL,-CO2H, -CO2C1-6 ALKYL, CYANO, TETRAZOL-5-YL, HALOGEN, TRIFLUOROMETHYL, OR C1-6ALKOXY, OR, WHEN R4 AND R5 ARE BONDED TO ADJACENT CARBON ATOMS, R4 AND R5 MAY, TOGETHER WITH THE CARBON ATOMS WHICH THEY ARE BONDED, FORM A FUSED 5 OR 6 MEMBERED RING OPTIONALLY CONTAINING ONE OR TWO NITROGEN, OXYGEN, OR SULFUR ATOMS; AND Y IS N OR CH, TO PROCESSES FOR THEIR PREPARATION AND THEIR USE IN THE TREATMENT OF DISEASES SUSCEPTIBLE TO AMELEORATION BY TREATMENT WITH A BETA-3 ADRENOCEPTOR AGONIST.
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