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。

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。

公开(公告)号：US5302730A

公开(公告)日：1994-04-12

申请号：US71616

申请日：1993-06-04

申请人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita ,  Chikara Komuro ,  Kazuhisa Narita

发明人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita ,  Chikara Komuro ,  Kazuhisa Narita

IPC分类号： C07D311/92

CPC分类号： C07D311/92

摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

摘要翻译： 本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：（*化学结构*）（I）其中R1和R2各自代表酰基，R3代表 具有2至3个碳原子的脂族基团，其包括通过以下通式除去在通式为（* CHEMICAL STRUCTURE *）（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中的第1位的酰基，其中R1 ，R2和R3如上定义，通过溶剂分解。 预期式（I）化合物为药物。

公开(公告)号：US5484954A

公开(公告)日：1996-01-16

申请号：US179826

申请日：1994-01-19

申请人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita

发明人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Narita

IPC分类号： C07D311/92

CPC分类号： C07D311/92

摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

摘要翻译： 本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：其中R1和R2各自代表酰基，R3代表脂族基团 具有2至3个碳原子，其包括在通式（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中除去第1位的酰基，其中R 1，R 2和R 3为 通过溶剂分解来定义。 预期式（I）化合物为药物。

公开(公告)号：US5610315A

公开(公告)日：1997-03-11

申请号：US442403

申请日：1995-05-16

申请人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Ishikawa ,  Chikara Komuro ,  Kazuhisa Narita

发明人： Tochiro Tatee ,  Akira Shiozawa ,  Hirotaka Yamamoto ,  Yuh-ichiro Ichikawa ,  Aya Ishikawa ,  Chikara Komuro ,  Kazuhisa Narita

IPC分类号： C07D311/92

CPC分类号： C07D311/92

摘要： This invention relates to a process for the preparation of a 6,7-diacyl-7-deacetylforskolin derivative represented by the general formula: ##STR1## wherein R.sup.1 and R.sup.2 each stands for an acyl group and R.sup.3 stands for an aliphatic group having 2 to 3 carbon atoms, which comprises eliminating the acyl group at position 1 in a 1,6,7-triacyl-7-deacetylforskolin derivative represented by the general formula: ##STR2## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined above, by solvolysis. The compound of the formula (I) is expected as medicine.

摘要翻译： 本发明涉及一种制备由以下通式表示的6,7-二酰基-7-脱乙酰福斯克林衍生物的方法：其中R1和R2各自代表酰基，R3代表脂族基团 具有2至3个碳原子，其包括在通式（III）表示的1,6,7-三酰基-7-脱乙酰福斯克林衍生物中除去第1位的酰基，其中R 1，R 2和R 3为 通过溶剂分解来定义。 预期式（I）化合物为药物。

公开(公告)号：US5245052A

公开(公告)日：1993-09-14

申请号：US732547

申请日：1991-07-19

申请人： Tochiro Tatee ,  Tatsuo Sugioka

发明人： Tochiro Tatee ,  Tatsuo Sugioka

IPC分类号： C07D311/92 ,  C07F7/18

CPC分类号： C07D311/92

摘要： A process for the manufacture of a 6-acyl-7-deacetylforskolin derivative represented by formula (I) ##STR1## by reacting a 7-acyl-7-deacetylforskolin derivative represented by formula (II) ##STR2## with a strong base in an aprotic solvent.