Cyclobutyl substituted derivatives of prostaglandin analogs
申请人:Miles Laboratories, Inc.
公开号:US04220795A1
公开(公告)日:1980-09-02
Novel C15 cyclobutyl analogs or derivatives of prostaglandins of the E-, A- and F-classes are useful modifiers of smooth muscle activity. The compounds have valuable pharmacological properties such as platelet antiaggregating agents, gastric antisecretory agents and brochodilating agents.
Cyclobutanecarboxylic acid derivatives and liquid crystalline
申请人:Kanto Kagaku Kabushiki Kaisha
公开号:US05545747A1
公开(公告)日:1996-08-13
An optically inactive cyclobutanecarboxylic acid derivative of the general formula ##STR1## wherein R.sup.1 is a hydrogen atom or a straight or branched chain alkyl group having 1-14 carbon atoms, R.sup.2 is a straight or branched chain alkyl group having 1-14 carbon atoms, X.sup.1 and X.sup.2 independently represent hydrogen or fluorine atoms, as well as a liquid crystalline composition containing at least one such derivative.
CYCLOBUTANECARBOXYLIC ACID DERIVATIVE AND LIQUID CRYSTAL COMPOSITION CONTAINING THE SAME
申请人:KANTO KAGAKU KABUSHIKI KAISHA
公开号:EP0496896A1
公开(公告)日:1992-08-05
An optically inactive cyclobutanecarboxylic acid derivative represented by general formula (I) and a liquid crystal composition containing at least one such derivative wherein R¹ represents hydrogen or C₁ to C₁₄ linear or branched alkyl; R² represents C₁ to C₁₄ linear or branched alkyl; and X¹ and X² represent each hydrogen or fluorine.
The great demand for improved long-acting injectable steroid contraceptives, particularly in developing countries, and the relative lack of interest from the pharmaceutical industry to develop such products stimulated WHO to launch a synthetic and screening programme to find improved, safe and acceptable injectable preparations. More than 210 esters of norethisterone (17 alpha-ethynyl-17 beta-hydroxyestr-4-en-3-one) and levonorgestrel (D-(-)-13 beta-ethyl-17 alpha-ethynyl-17 beta-hydroxygon-4-en-3-one) have been prepared in university-based research laboratories situated mainly in developing countries, and then screened by NICHHD in animal models. The following three compounds, levonorgestrel butanoate, cyclopropylcarboxylate and cyclobutylcarboxylate, proved to be particularly long-acting when administered as microcrystalline suspensions. The overall strategy of this research and development programme is described.