Pharmaceutical use of forskolin derivatives

• US 5,789,439 A
• Filed: 05/21/1997
• Issued: 08/04/1998
• Est. Priority Date: 03/23/1990
• Status: Expired due to Fees

• Current Assignee: Nippon Kayaku Company Limited
• Original Assignee: Nippon Kayaku Company Limited
• Inventors: Hosono, Makoto, Terada, Takashi, Fujita, Akira, Sakai, Michiko, Ishizuka, Osamu, Itoh, Junpei, Tatee, Tochiro, Furuta, Yasuhiko, Takahira, Takashi, Izumi, Giichi
• Primary Examiner(s): MACMILLAN, KEITH D
• Application Number:
  US08/861,262
• Time in Patent Office: 440 Days
• Field of Search: 514/455
• US Class Current: 514/455
• CPC Class Codes: A61K 31/35 having six-membered rings with one oxygen as the only ring hetero atom
• CPC Class Codes: A61K 31/352 condensed with carbocyclic rings, e.g. methantheline cannabinoids A61K31/658

Abstract

The present invention relates to novel pharmaceutical use of forskolin derivatives represented by the general formula: ##STR1## wherein R¹, R² and Ac are as defined later ##STR2## (wherein R³ and R⁴ are each hydrogen or lower alkyl group, or R³ and R⁴ 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); R² 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.

Claims

1. A therapeutic method for the treatment of a skin ulcer which comprises administering to a mammal having a skin ulcer, a medicament containing as the active principle a forskolin derivative represented by the formula:

##STR7## (wherein R¹ is a group represented by the formula ##STR8## (wherein R³ and R⁴ are each hydrogen or lower alkyl group, or R³ and R⁴ may be combined to represent a lower alkylene group which may have an oxygen or nitrogen atom in the linking chain, and n is an integer of 1 to

     5);

R² represents a hydrocarbon group having 2 to 3 carbon atoms; and

Ac represents an acetyl group) or a physiologically acceptable salt thereof.

2. The method according to claim 1, wherein R¹ in the formula is dimethylaminopropionyl group and R² is vinyl group.

3. The method according to claim 1, wherein the skin ulcer is decubitus.

4. The method according to claim 1, wherein the medicament is applied directly to the region of skin ulcer.