The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): ##STR00001##
(wherein X represents a halogen atom, R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group containing 1 to 7 carbon atoms, R.sup.3 represents —CHO, and R.sup.4 represents —CH.sub.2—CH═C(CH.sub.3)—R.sup.0 (wherein R.sup.0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)),
an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor which is applicable to various diseases. When used as an active ingredient, a compound represented by formula (I): ##STR00001##
(wherein X represents a halogen atom, R.sup.1 represents a hydrogen atom, R.sup.2 represents an alkyl group containing 1 to 7 carbon atoms, R.sup.3 represents —CHO, and R.sup.4 represents —CH.sub.2—CH═C(CH.sub.3)—R.sup.0 (wherein R.sup.0 represents an alkyl group containing 1 to 12 carbon atoms which may have a substituent on the terminal carbon and/or on a non-terminal carbon, etc.)),
an optical isomer thereof or a pharmaceutically acceptable salt thereof has a high inhibitory effect on dihydroorotic acid dehydrogenase and can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anticancer agent, a therapeutic agent for graft rejection, an antiviral agent, an anti-H. pylori agent, a therapeutic agent for diabetes or the like.

A process for the preparation of a compound of formula (I) and of a acid salt (T) wherein R.sup.1 is selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R.sup.2 and R.sup.3, are, independently of each other, selected from the group consisting of alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, R.sup.4, R.sup.5, R.sup.6 and R.sup.7, are independently of each other, selected from the group consisting of H, alkyl, aryl, cycloalkyl, heteroalkyl, heteroaryl and heterocycloalkyl, and wherein the acid salt is a 2,3-Ditoluoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid salt, 2,3-Dianisoyl tartaric acid salt, 2,3-Dibenzoyl tartaric acid mono(dimethylamide) salt or a mixture of two or more thereof, wherein the tartaric acid salt (T) of the compound of formula (I) contains at least 90% by weight of the tartaric salt of the compound of formula (Ia) based on the total weight of the acid salt of the compound of formula (I).

##STR00001##

The present invention provides a water-soluble fluorescent compound of resveratrone 6-O-β-glucoside [(E)-4-(8-hydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)naphthalen-2-yl)but-3-en-2-one] and its derivatives of Formula I which have at least one water-soluble substituent, and a method for preparing the same by a photochemical reaction of resveratrol 3-O-β-glucoside and its derivatives of having Formula 3 which are not fluorescent. Said new water-soluble fluorescent compounds has single-photon absorptive characteristics and/or two-photon absorptive characteristics as well as no or little toxicity, and can be usefully utilized in fields that requires water-soluble fluorescent characteristics (diagnosis, fluorescent probe, in vivo imaging, display, etc.).

The present invention provides a water-soluble fluorescent compound of resveratrone 6-O-β-glucoside [(E)-4-(8-hydroxy-6-(((2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)naphthalen-2-yl)but-3-en-2-one] and its derivatives of Formula I which have at least one water-soluble substituent, and a method for preparing the same by a photochemical reaction of resveratrol 3-O-β-glucoside and its derivatives of having Formula 3 which are not fluorescent. Said new water-soluble fluorescent compounds has single-photon absorptive characteristics and/or two-photon absorptive characteristics as well as no or little toxicity, and can be usefully utilized in fields that requires water-soluble fluorescent characteristics (diagnosis, fluorescent probe, in vivo imaging, display, etc.).

The present invention discloses a process for preparation of white curcumin from purified curcuminoids. The curcuminoids are obtained by solvent extraction and crystallization of dried turmeric powder. The autoclave is charged with ethyl acetate and the 95% purity curcuminoids mixture is added to and stirred for uniformity at room temperature. 5% (w/w) of 10% palladium carbon is added to the reaction mixture and allowed for hydrogenation in the presence of hydrogen gas at 2 lbps pressure and stirred continuously for 15 hours. Once the reaction is completed, the reaction mixture is filtered and washed with ethyl acetate. The ethyl acetate is distilled off and crude mass is stirred with water to obtain a solid precipitate. Finally, the solid obtained is filtered and dried to pale brown crystals of white curcumin. White curcumin is encapsulated with beta-cyclodextrin, which exhibited increased bioavailability. White curcumin also exhibited anti-oxidant and chemopreventive activities.

The present invention discloses a process for preparation of white curcumin from purified curcuminoids. The curcuminoids are obtained by solvent extraction and crystallization of dried turmeric powder. The autoclave is charged with ethyl acetate and the 95% purity curcuminoids mixture is added to and stirred for uniformity at room temperature. 5% (w/w) of 10% palladium carbon is added to the reaction mixture and allowed for hydrogenation in the presence of hydrogen gas at 2 lbps pressure and stirred continuously for 15 hours. Once the reaction is completed, the reaction mixture is filtered and washed with ethyl acetate. The ethyl acetate is distilled off and crude mass is stirred with water to obtain a solid precipitate. Finally, the solid obtained is filtered and dried to pale brown crystals of white curcumin. White curcumin is encapsulated with beta-cyclodextrin, which exhibited increased bioavailability. White curcumin also exhibited anti-oxidant and chemopreventive activities.

The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.

The invention provides compounds and methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits.

The present invention relates to novel small molecules of Formulas I, II, III, Ilia, Illb, and IV and pharmaceutically acceptable salts thereof, as well as the preparation and the use thereof.