Nippon Kayaku Kabushiki Kaisha

Hoechst Japan Limited

Nippon Kayaku Co., Ltd

Tochiro Tatee

Akira Shiozawa

Kazuhisa Narita

Yuh-ichiro Ichikawa

Hirotaka Yamamoto

Takashi Takahira

Takashi Terada

Tatsuo Sugioka

Giichi Izumi

Kouwa Yamashita

Makoto Hosono

Yasuhiko Furuta

Chikara Komuro

Akira Fujita

Michiko Sakai

Aya Narita

Masao Sakurai

Aya Ishikawa

Junpei Itoh

Osamu Ishizuka

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.

Pharmaceutical use of forskolin derivatives

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.

Process for the preparation of 6,7-diacyl-7-deacetylforskolin derivatives

Process for the preparation of 6,7-diacyl-7-deacteylforskolin derivatives

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.

Process for producing 6-acyl-7-deacetylforskolin derivatives

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,

Forskolin compounds

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Tokyo, Japan

Tochiro Tatee