公开(公告)号：US4237141A

公开(公告)日：1980-12-02

申请号：US910024

申请日：1978-05-26

申请人： Akira Shiozawa ,  Shuji Kurashige ,  Hiroaki Hamano ,  Yasuhiko Furuta ,  Masako Ikeda ,  Hiroshi Miyazaki ,  Chiyoko Aoyagi ,  Yasuo Ishii

发明人： Akira Shiozawa ,  Shuji Kurashige ,  Hiroaki Hamano ,  Yasuhiko Furuta ,  Masako Ikeda ,  Hiroshi Miyazaki ,  Chiyoko Aoyagi ,  Yasuo Ishii

IPC分类号： C07D295/108 ,  C07D295/10 ,  A61K31/445

CPC分类号： C07D295/108

摘要： Novel .alpha.-methyl-.beta.-aminopropiophenone derivatives having bronchodilator activity represented by the following general formula: ##STR1## where R represents alkyl having 1-6 carbon atom benzyl or phenyl; R.sub.1 and R.sub.2 individually represent alkyl having 1-6 carbon atom or they form, joining to each other together with the adjacent nitrogen atom with or without intervening an atom other than carbon atom, a saturated heterocyclic ring which may be substituted with lower alkyl; n is an integer of 0, 1 or 2 on the proviso that R represents methyl or ethyl if n is 0, as well as their non-toxic salts are presented. Method of producing the new derivatives and the bronchodilatation method using them are disclosed as well.

摘要翻译： 具有由以下通式表示的支气管扩张剂活性的新型α-甲基-β-氨基苯丙酮衍生物：其中R表示具有1-6个碳原子的烷基苄基或苯基; R1和R2分别代表具有1-6个碳原子的烷基或它们形成，可以与相邻的氮原子相互连接或不连接除碳原子以外的原子，可以被低级烷基取代的饱和杂环; n为0或1或2的整数，条件是R表示甲基或乙基，如果n为0，以及它们的无毒盐。 还公开了制备新衍生物的方法和使用它们的支气管扩张方法。

公开(公告)号：US5789439A

公开(公告)日：1998-08-04

申请号：US861262

申请日：1997-05-21

申请人： Makoto Hosono ,  Akira Fujita ,  Giichi Izumi ,  Tochiro Tatee ,  Takashi Takahira ,  Yasuhiko Furuta ,  Michiko Sakai ,  Osamu Ishizuka ,  Takashi Terada ,  Junpei Itoh

发明人： Makoto Hosono ,  Akira Fujita ,  Giichi Izumi ,  Tochiro Tatee ,  Takashi Takahira ,  Yasuhiko Furuta ,  Michiko Sakai ,  Osamu Ishizuka ,  Takashi Terada ,  Junpei Itoh

IPC分类号： A61K31/35 ,  A61K31/352

CPC分类号： A61K31/352 ,  A61K31/35

摘要： The present invention relates to novel pharmaceutical use of forskolin derivatives represented by the general formula: ##STR1## wherein R.sup.1, R.sup.2 and Ac are as defined later ##STR2## (wherein R.sup.3 and R.sup.4 are each hydrogen or lower alkyl group, or R.sup.3 and R.sup.4 may be combined to represent lower alkylene group which may have oxygen or nitrogen atom in the linking chain, and n is an integer of 1 to 5); R.sup.2 represents hydrocarbon group having 2 to 3 carbon atoms; and Ac represents acetyl group. The above-mentioned forskolin derivative or a physiologically acceptable salt thereof can be used as a platelet aggregation inhibiting or controlling agent, spasmolytic agent, therapeutic agent for skin ulcer, peripheral circulation improving agent for limbs and differentiation inducing and promoting agent.

摘要翻译： 本发明涉及由以下通式表示的毛喉素衍生物的新型药物用途：其中R1，R2和Ac如下文定义（其中R3和R4各自为氢或低级烷基，或R3和R4 可以结合表示在连接链中可以具有氧或氮原子的低级亚烷基，n是1〜5的整数）; R2表示碳原子数2〜3的烃基， Ac表示乙酰基。 上述的毛喉素衍生物或其生理上可接受的盐可以用作血小板聚集抑制剂，解痉药，皮肤溃疡治疗剂，肢体周边循环改善剂和分化诱导促进剂。