申请人:University of Lancaster
公开号:EP0240257A2
公开(公告)日:1987-10-07
Pharmaceutical compositions useful in regulating calcium transport across cellular membranes in man and animals are disclosed. The compositions contain plant growth regulators such as abscisic acid and its derivatives. In particular, the compositions contain a compound of the formula:
or
R₁ - Y - R₂
wherein R₁ is an alkyl of up to seven carbons or a saturated or unsaturated six membered carbon ring, which may be substituted; R₂ is a cyano group, a thio or hydroxy lower alkyl group or a group containing a carbonyl, most commonly a carboxyl group; R₃ is hydrogen or lower alkyl; R₄ is hydrogen, lower alkyl or halide; R₅ is hydrogen or hydroxy; R₆ is hydrogen, carboxy or carboxy lower alkyl, or R₅ and R₆ form a bond between the carbons to which they are attached or with the carbons to which they are attached form a carbon ring; or R₂ and R₆ together with the carbon to which they are bonded form a heterocyclic ring; n is 0 or 1, with the proviso that when n is 0, R₂ is an acyl group; X is -CH₂-, -CH=CH-, -CH₂-CH₂-, -CH₂-NH-, -CH₂-O-, -CH₂-S- or -NH-CO-; and Y is a carbocyclic group bonded to R₁ and R₂ through a single carbon. The compositions are formulated for oral, parenteral or other form of administration in dosages necessary to effect the desired change in calcium flux. Daily doses of 0.01 to 200 mg/kg in one or more doses are contemplated. Dosage units may be formulated with any pharmaceutically acceptable carrier which is compatible with the active ingredient.
本发明公开了可用于调节人和动物细胞膜钙转运的药物组合物。这些组合物含有植物生长调节剂,如脱落酸及其衍生物。特别是,组合物中含有一种式的化合物:
或
R₁ - Y - R₂
其中,R₁ 是最多七个碳原子的烷基或饱和或不饱和的六分子碳环,可以被取代;R₂ 是氰基、硫代或羟基低级烷基或含有羰基的基团,最常见的是羧基;R₃ 是氢或低级烷基;R₄ 是氢、低级烷基或卤化物;R₅ 是氢或羟基;R₆ 是氢、羧基或羧基低级烷基,或 R₅ 和 R₆ 在所连接的碳之间形成键,或与所连接的碳一起形成碳环;或 R₂ 和 R₆ 与所连接的碳一起形成杂环;n 为 0 或 1,但当 n 为 0 时,R₂ 为酰基;X 为-CH₂-、-CH=CH-、-CH₂-CH₂-、-CH₂-NH-、-CH₂-O-、-CH₂-S-或-NH-CO-;Y 是通过一个碳与 R₁ 和 R₂ 键合的碳环基团。组合物配制成口服、肠外或其他形式的给药剂量,以实现所需的钙通量变化。日剂量为 0.01 至 200 毫克/千克,可考虑一次或多次给药。剂量单位可与任何与活性成分相容的药学上可接受的载体配制。