Hanwha Corporation

Hanwha Chemical Corporation

Seung Un Kim

Young Ki Paik

Jung Ho Kim

Eui Deok Kim

Joon Seo Park

You Suk Lee

Tae Neung Jhong

The present invention provides a cholesterol biosynthesis inhibitor which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, a compound of formula (1) below and the use of an extract or the compound of formula (1) for treating hypercholesterolaemia or hyperlipidaemia. The inhibitor comprises an extract obtained by extracting,with a solvent, or an organic layers obtained by partitioning an extract from,with an organic solvent. The extract contains 7,8,13,13&agr;-tetrahydrocoridaline or its derivative, as the active ingredients, which specifically inhibits the enzyme which is involved in the distal pathway of the cholesterol biosynthesis.

Cholesterol biosynthesis inhibitors

The present invention provides a cholesterol biosynthesis inhibitor which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, a compound of formula (1) below and the use of an extract or the compound of formula (1) for treating hypercholesterolaemia or hyperlipidaemia. The inhibitor comprises an extract obtained by extracting Corydalis Turtschaninowii Besser with a solvent, or an organic layers obtained by partitioning an extract from Corydalis Turtschaninowii Besser with an organic solvent. The extract contains 7,8,13,13&agr;-tetrahydrocoridaline or its derivative, as the active ingredients, which specifically inhibits the enzyme which is involved in the distal pathway of the cholesterol biosynthesis.

13,13A-Didehydroberbine derivatives

The antifungal formulation comprising the novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The formulation of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylamino, acetylamino, C.sub.1 -C.sub.8 trialkyl ammonium, guanidinyl, methylthio, ethylthio, trifluoromethoxy, hydroxy, phenoxy, vinyl, carboxyl and C.sub.1 -C.sub.2 alkoxycarbonyl group.

Antifungal formulation comprising protoberberine derivatives and salts

The present invention provides a pharmaceutical composition comprising 5,6-dihydrodibenzo[a,g]quinolizinium derivative and the salts thereof of formula (I) which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, and the use of the compound of formula (I) for treating hypercholesterolaemia or hyperlipidaemia. ##STR1##

Pharmaceutical composition comprising 5,6-dihydrodibenzo[A,G]

The present invention provides a 5,6-dihydrodibenzo[a,g]quinolizinium derivative and the salts thereof of formula (I) which specifically inhibits the sterol 14-reductase which is involved in the distal pathway of cholesterol biosynthesis, and the use of the compound of formula (I) for treating hypercholesterolaemia or hyperlipidaemia. ##STR1## wherein, R.sup.1 and R.sup.2 which may be the same or different from each other, represent a hydroxy group or an alkoxy group having 1 to 4 carbons or R.sup.1 and R.sup.2 together represent a methylenedioxy group;

Dibenzo[a,g]quinolizinium derivatives and the salts thereof

The novel compounds of the following chemical formulae (I) and (II) exhibit in vitro antifungal activity against fungi including cutaneous filamentous fungus, such as Epidermophyton, Microsporum, Trichophyton, Sporothrix schenckii, Aspergillus or Candida. The compounds of the present invention exhibit in vitro antifungal activity at the concentration of 1-100 .mu.g/ml. ##STR1## wherein R.sup.1, R.sup.2, and R.sup.4 may be the same or different, and represent C.sub.1 -C.sub.5 alkoxy, R.sup.3 represents hydrogen or C.sub.1 -C.sub.10 alkyl, A.sup.- represents inorganic acid ion, organic acid ion or halide, R.sup.5 represents hydrogen, pyridylmethyl, substituted pyridylmethyl or a group having the following chemical formula(XI) ##STR2## wherein Z.sup.1, Z.sup.2, Z.sup.3, Z.sup.4 and Z.sup.5 may be the same or different and represent hydrogen, halogen, C.sub.1 -C.sub.5 alkyl, trifluoromethyl, phenyl, substituted phenyl, nitro, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 alkylamino, acetylamino, C.sub.1 -C.sub.8 trialkyl ammonium, guanidinyl, methylthio, ethylthio, trifluoromethoxy, hydroxy, phenoxy, vinyl, carboxyl and C.sub.1 -C.sub.2 alkoxycarbonyl group.

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Daejeon, South Korea

Seung Un Kim