Oral preparations containing forskolin derivatives and...

A - Human Necessities – 61 – K

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A61K 31/35 (2006.01) A61K 9/20 (2006.01) A61K 47/02 (2006.01) C07D 311/92 (2006.01)

Patent

CA 2329736

Oral preparations excellent in storage stability and containing salts of forskolin derivatives represented by general formula (1), such as colforsin dapropate hydrochloride [6-(3-dimethylaminopropionyl)forskolin], and alkali metal halides wherein R1 represents hydrogen; R4 represents vinyl; and one of R2 and R3 represents -CO(CH2)mNR5R6 (wherein R5 and R6 represent each lower alkyl, etc. and m is an integer of from 1 to 5), while another represents hydrogen or -CO(CH2)nX [wherein X represents hydrogen or -NR7R8 (wherein R7 and R8 represent each lower alkyl, etc.), and n is an integer of from 1 to 5].

On décrit des préparations orales présentant une excellente stabilité de conservation et contenant des sels de dérivés de forskoline de la formule générale (1), tels que le chlorhydrate de colforsine dapropate[6-(3-diméthylaminopropionyl)forskoline], et des halogénures métallisés. Dans ladite formule, R?1¿ est hydrogène, R?4¿ est vinyle, et R?2¿ ou R?3¿ est CO(CH¿2?)¿m?NR?5¿R?6¿ (R?5¿ et R?6¿ étant chacun alkyle inférieur, etc. et m un entier compris entre 1 et 5) tandis que l'autre est hydrogène ou CO(CH¿2?)¿n?X (X est hydrogène ou -NR?7¿R?8¿ (R?7¿ et R?8¿ étant chacun alkyle inférieur, etc.) et n un entier compris entre 1 et 5).

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