Novel compounds represented by formula (I) are useful for preventing or treating diseases caused by protozoans. Use is made of one or more members selected from among compounds represented by formula (I), optical isomers thereof and pharmaceutically acceptable salts of the same. In formula (I): X represents a hydrogen atom or a halogen atom; R1 represents a hydrogen atom; R2 represents a hydrogen atom or a C1-7 alkyl group; R3 represents -CHO, -C(=O)R5, -COOR5 [wherein R5 represents a C1-7 alkyl group], -CH2OH or -COOH; and R4 represents a C1-16 alkyl group having various substituent(s) on a terminal carbon atom and/or a non-terminal carbon atom, a C2-16 alkenyl group having various substituent(s) on a terminal carbon atom and/or a non-terminal carbon atom, or a C2-16 alkynyl group having various substituent(s) on a terminal carbon atom and/or a non-terminal carbon atom.

Novel dihydroxybenzene derivatives and antiprotozoal agent comprising same as active ingredient

The present invention provides a novel dihydroorotic acid dehydrogenase inhibitor that is applicable to various diseases. As an active ingredient, a compound represented by formula (I) (wherein X represents a halogen atom; R1 represents a hydrogen atom; R2 represents an alkyl group having 1 to 7 carbon atoms; R3 represents -CHO; and R4 represents -CH2-CH=C(CH3)-R0 (wherein R0 represents an alkyl group having 1 to 12 carbon atoms which may have a substituent on a terminal carbon atom and/or a non-terminal carbon atom, or the like)), an optical isomer of the compound, and a pharmaceutically acceptable salt of the compound or the optical isomer. The compound, the optical isomer and the pharmaceutically acceptable salt have an excellent inhibitory activity on dihydroorotic acid dehydrogenase and therefore can be used as an immunosuppressive agent, a therapeutic agent for rheumatism, an anti-cancer agent, a therapeutic agent for rejection response, an anti-viral agent, an anti-H. pylori agent, a therapeutic agent for diabetes and the like.

Dihydroorotic acid dehydrogenase inhibitor

PROBLEM TO BE SOLVED: To provide a novel compound for preventing or treating diseases caused by protozoans.SOLUTION: A compound represented by formula (I), optical isomers of the compound, and one or more kinds of pharmaceutically acceptable salts of the compound are used. In formula (I), X represents a hydrogen atom or a halogen atom; Rrepresents a hydrogen atom; Rrepresents a hydrogen atom or a 1-7C alkyl group; Rrepresents -CHO, -C(=O)R, -COOR(where Rrepresents a 1-7C alkyl group), -CHOH or -COOH; and Rrepresents a 1-16C alkyl group having various substituents on a terminal carbon atom and/or a non-terminal carbon atom, a 2-16C alkenyl group having various substituents on a terminal carbon atom and/or a non-terminal carbon atom, or a 2-16C alkynyl group having various substituents on a terminal carbon atom and/or a non-terminal carbon atom.

Novel dihydroxybenzene derivative and antiprotozoal agent comprising the same as active ingredient

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): (wherein
 X represents a halogen atom, R 1 represents a hydrogen atom, R 2 represents an alkyl group containing 1 to 7 carbon atoms, R 3 represents —CHO, and R 4 represents —CH 2 —CH═C(CH 3 )—R 0 (wherein R 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.

Dihydroorotic and acid dehydrogenase inhibitor

PURPOSE: To obtain new substance BE-24811 useful as an antitumor agent, etc., having an inhibitory effect on proliferation. CONSTITUTION: A compound of the formula has the following properties. Properties: semi-opaque needle-like crystal. Molecular formula: C 18 H 21 O 4 Cl. Mass spectrum (high resolution E1-MS, m/z): 336. 1133 [M + ]. Ultraviolet light absorption spectrum: λ max [MeOH, nm(e)] 230 (22900), 293 (10900), 3,44 (5300). Infrared light absorption spectrum: ν max (KBr, cm -1 : 3167, 2927, 1672, 1628, 1608, 1421, 1248, 1113. Solubility: readily soluble in dimethyl sulfoxide, soluble in chloroform, ethyl acetate and methanol, insoluble in water. Distinction of acid, neutral or basic substance: acidic substance. Color reaction: positive in iodine reaction, potassium permanganate reaction and 2,4dinitrophenylhydrazine reaction. The compound of the formula is obtained by culturing a fungus belonging to the genus Talaromyces, capable of producing the compound of the formula, such as Talaromyces retardatus F24811 (FERM P-14,103). COPYRIGHT: (C)1995,JPO

Hidemi Matsumoto

Papers

Antitumor substance be-24811 and its production