| 摘要 |
<p>Thienopyridine derivs. of formula (I) and their salts are new. In (I) R1 is (i) H or 1-4C alkyl, (ii) Cl or Br in the 2, 3 or 7 position or (iii) F, CN or COOB in the 2 or 3 position; B is 1-4C alkyl; R is (i) H or 1-4C alkyl, (ii) Cl or Br in the 2, 3 or 7 position or (iii) F in the 2 or 3 position; R3 is H or -COR4; R4 is 1-17C alkyl, phenyl (opt. monosubstd. by NO2, disubstd. by 1-4C alkyl, F, Cl or Br, or trisubstd. by 1-4C alkoxy) or -D-COOH; D is ethylene or trimethylene. R is 8-10C phenylalkyl (opt. monosubstd. in the ring by 1-4C alkyl, F, Cl or Br, or opt. mono- or disubstd. in the ring by 1-4C alkoxy), the phenyl ring being sepd. from the N atom to which R is bonded by >=2C; when R3 is -COR4, R can also be 3-7C alkyl, 3-7C cycloalkyl (opt. monosubstd. by 1-4C alkyl), 5-9C alpha-dialkylpropvnyl, 5-9C alpha-dialkylallyl or 8-11C phenoxyalkyl where the O atom is sepd. from the N atom to which R is bonded by >=2C; provided that when R1 is CN or COOB, then R2 is not Cl, Br and F in the 2- or 3-position. (I) are beta-adrenergic blockers, useful for the treatment or prophylaxis of coronary diseases, esp. angina pectoris. (I) also have antiarrhythmic and metabolic activity. They reduce psychic stress-induced mobilisation of glucose and fatty acids in the blood.</p> |
