申请人:Leo Pharmaceutical Products Ltd. A/S
公开号:US04870063A1
公开(公告)日:1989-09-26
Novel compounds of the formula I ##STR1## in which R.sub.1 -R.sub.11 can be the same or different and stand for hydrogen, a straight or branced aliphatic or alicyclic C.sub.1 -C.sub.10 hydrocarbon radical, an aryl or an aryl-C.sub.1 -C.sub.4 -alkyl radical; n is zero or one, and m is zero, one or two; or R.sub.2 and R.sub.4 when taken together form a saturated aliphatic 5-, 6- or 7-membered ring which may be substituted with one or more C.sub.1 -C.sub.4 alkyl radicals; and pharmaceutically acceptable salts and easily hydroyzable esters thereof, methods for producing said new compounds, pharmaceutical compositions containing the new compounds, dosage units of the compositions, and methods of treating patients using said compositions and dosage units. The present compounds are valuable in the human and veterinary practice by reducing bone resorption and surprisingly also stimulating bone alkaline phosphatase. A substantial increase in bone mass is actually observed during treatment with the present compounds.
化合物的新结构式I的新化合物 ##STR1## 在该结构中,R.sub.1-R.sub.11可以相同也可以不同,代表氢、直链或支链烷基或脂环烷基C.sub.1-C.sub.10、芳基或芳基-C.sub.1-C.sub.4-烷基基团;n为零或一,m为零、一或二;或当R.sub.2和R.sub.4在一起形成饱和的脂肪族5-、6-或7-成员环时,该环可能被一个或多个C.sub.1-C.sub.4烷基基团取代;以及其药学上可接受的盐和易水解酯,制备该新化合物的方法,含有该新化合物的制药组合物,该组合物的剂量单位,以及使用该组合物和剂量单位治疗患者的方法。这些化合物通过减少骨吸收并令人惊讶地刺激骨碱性磷酸酶,在人类和兽医实践中具有价值。实际上,在使用这些化合物进行治疗期间,骨量显著增加。