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2. 发明授权

US4954642A Forskolin compounds 失效
标题翻译：福斯康林化合物
公开(公告)号：US4954642A
公开(公告)日：1990-09-04
申请号：US361763
申请日：1989-05-30
申请人： Tochiro Tatee , Takashi Takahira , Kouwa Yamashita , Masao Sakurai , Akira Shiozawa , Kazuhisa Narita
发明人： Tochiro Tatee , Takashi Takahira , Kouwa Yamashita , Masao Sakurai , Akira Shiozawa , Kazuhisa Narita
IPC分类号： A61K31/35 , C07D311/92 , C07D405/12
CPC分类号： C07D311/92
摘要： This invention relates to forskolin derivatives, their physiologically acceptable salts, and a process for producing these compounds. The forskolin derivative is represented by the general formula ##STR1## wherein; I. when R.sup.1 is hydrogen and R.sup.4 is vinyl, ethyl, or cyclopropyl,(1) either of R.sup.2 and R.sup.3 denotes a residue represented by the formula ##STR2## wherein each of R.sup.5 and R.sup.6 denotes hydrogen or lower alkyl or R.sup.5 and R.sup.6 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom and m is an integer of 1 to 5, and the other one of R.sup.2 and R.sup.3 denotes hydrogen or a residue represented by the formula CO(CH.sub.2).sub.n X, X being hydrogen or ##STR3## wherein, each of R.sup.7 and R.sup.8 denotes hydrogen or lower alkyl or R.sup.7 and R.sup.8 combine with each other to form a lower alkylene chain which may or may not contain an oxygen or nitrogen atom, and n being an integer of 1 to 5, or(2) R.sup.2 denotes hydrogen or --COCH.sub.2 CH.sub.2 CO.sub.2 H and R.sup.3 denotes hydrogen, --COCH.sub.3, --COCH.sub.2 CH.sub.2 CH.sub.2 CO.sub.2 H, or --COCH(OH)CH.sub.2 OH with the proviso that R.sup.3 is one of the last two residues when R.sup.2 is hydrogen, andII. whenR.sup.1 is a residue represented by a formula of CO(CH.sub.2).sub.p CO.sub.2 H and ##STR4## wherein, each of R.sup.9 and R.sup.10 denotes hydrogen or lower alkyl, p is an integer of 0 to 5, and q is an integer of 1 to 5,R.sup.2 denotes hydrogen , R.sup.3 denotes acetyl, and R.sup.4 denotes vinyl.
摘要翻译：本发明涉及毛喉素衍生物及其生理学上可接受的盐，以及这些化合物的制备方法。毛喉素衍生物由通式表示，其中：当R1是氢并且R4是乙烯基，乙基或环丙基时，（1）R2和R3中的任一个表示由下式表示的残基：其中R 5和R 6各自表示氢或低级烷基或R 5和R 6结合彼此形成可以含有或不含有氧或氮原子并且m为1〜5的整数的低级亚烷基链，R2和R3中的另一个表示氢或由式CO（CH2）表示的残基）n X，X为氢或者其中，R 7和R 8各自表示氢或低级烷基，或者R 7和R 8彼此结合形成可含有或不含有氧或氮原子的低级亚烷基链，n 为1〜5的整数，或（2）R2表示氢或-COCH2 CH2CO2H，R3表示氢，-COCH3，-COCH2CH2CH2CO2H或-COCH（OH）CH2OH，条件是R3为最后两个残基之一， R2是氢，II。当R 1是由CO（CH 2）p CO 2 H和的式表示的残基时，R 9和R 10各自表示氢或低级烷基，p是0至5的整数，q是1至5的整数，R2表示氢，R3表示乙酰基，R4表示乙烯基。

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