KR900003100A - Naphthoquinone - Google Patents

Abstract

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Description

Naphthoquinone

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Claims (12)

A method of using naphthoquinone for the manufacture of a medicament for the treatment and / or prophylaxis of pediatric pneumocystis carinii infections. The method according to claim 1, wherein the naphthoquinone is a compound of the following general formula (II) and their physiologically acceptable salts and other physiologically active derivatives. Wherein R ³ is a C _1-35 non-aromatic hydrocarbon optionally substituted with one or more substituents selected from halo, C _1-6 alkoxy, hydroxy, phenyl, phenyl-C _1-6 alkoxy and phenyl-C _1-6 alkyl And each phenyl group is C _1-6 alkoxy, C _1-6 alkyl, C _1-6 alkoxy-C _1-6 alkyl, hydroxy, halogen, halo-C _1-6 alkyl, amino and mono- or di- Optionally substituted with one or more groups selected from C _1-4 alkyl-amino, R ⁴ is a group of hydroxy, halogen, OCOR ⁵ , wherein R ⁵ is a C _1-10 alkyl, C _3-10 cycloalkyl group, C _{1 A -10} alkoxy group, or a phenyl or naphthyl group, each R ⁵ group is optionally substituted with amino, mono- or di-C _1-4 alkylamino, carboxy or hydroxy, groups of OR ⁶ or SR ⁶ R ⁶ is optionally substituted with a C _1-10 alkyl, C _3-10 cycloalkyl, phenyl or naphthyl group as defined by R ⁵ or a group of NR ⁷ R ⁸ , wherein R ⁷ and R ⁸ are each Each hydrogen or C _1-4 alkyl, or NR ⁷ R ⁸ group is a 5-7 membered saturated heterocyclic ring optionally containing a heteroatom selected from nitrogen, oxygen or sulfur). The naphthoquinone is 2- (4-tbutylcyclohexyl) -3-hydroxy-1,4-naphthoquinone, 2- (4-t-butylcyclohexylmethyl). -3-hydroxy-1,4-naphthoquinone, 2- [4- (4-chlorophenyl) cyclohexyl] -3-chloro-1,4-naphthoquinone, and their physiologically acceptable salts and physiological actions Method of use selected from derivatives. 2- [4- (4-chlorophenyl) cyclohexyl] -3-hydroxy-1,4-naphthoquinone, and their physiological tolerance for the manufacture of drugs for the treatment and / or prophylaxis of pediatric pneumococcal infections in mammals Method of using salt or physiologically induced derivatives. The method of claim 4, wherein the compound is in the form of a trans isomer or in the form of a mixture of cis and trans isomers containing at least 95% of the trans isomers. The naphthoquinone according to any one of claims 1 to 5 for use in the treatment and / or prevention of pediatric pneumococcal infection in mammals. A method for the treatment and / or prophylaxis of pediatric pneumococcal infections comprising administering to a mammal infected with pediatric pneumococci an effective amount of naphthoquinone according to any one of claims 1 to 5. A compound of the following general formula (VI); Wherein R ¹¹ and R ¹² are each = 0, and the dotted line represents a double bond between the 2 and 3 positions of the quinone ring, in which case R ¹³ is a -OCOR ⁵ group OR ⁶ or SR ⁶ group, or NR ⁷ R ⁸ groups, R ⁵ , R ⁶ , R ⁷ and r ⁸ are as described above, or the dotted line represents double bonds at 1,2, 3,4 positions of the quinone ring and R ¹¹ , R ¹² and R ¹³ are Each represents an -OCOR ¹⁴ group, wherein R ¹⁴ is an optionally substituted C _1-10 alkyl group. Naphthoquinone according to any one of claims 1 to 5 together with a pharmaceutical acceptable carrier comprising a pharmaceutically acceptable carrier thereof. Claims 1 to 5 of the naphthoquinone according to any one of the drugs together with the pharmaceutically acceptable carrier comprising a pharmaceutically acceptable carrier. A pharmaceutical formulation comprising a pharmaceutically acceptable carrier thereof with a compound of the following general formula (VI). Wherein R ¹¹ and R ¹² are each = 0, and the dotted line represents a double bond between the 2 and 3 positions of the quinone ring, in which case R ¹³ is a -OCOR ⁵ group OR ⁶ or SR ⁶ group, or NR ⁷ R ⁸ groups, R ⁵ , R ⁶ , R ⁷ and R ⁸ are as described above, or the dotted line represents double bonds at 1,2, 3,4 positions of the quinone ring and R ¹¹ , R ¹² and R ¹³ are Each represents an -OCOR ¹⁴ group, wherein R ¹⁴ is an optionally substituted C _1-10 alkyl group. (a) a compound of general formula (Ⅴ) or by reacting the compound which is added a group R ¹¹ and R ¹² in accordance with the R ¹³ group, a need required of a compound of (Ⅶ) or, (b) represented by the following general formula (Ⅷ) A method for producing a compound of formula (VI), consisting of reacting with a main compound to which a 4- (4-chlorophenyl) cyclohexyl group is added. Wherein R ¹¹ and R ¹² are each = 0, and the dotted line represents a double bond between the 2 and 3 positions of the quinone ring, in which case R ¹³ is a -OCOR ⁵ group OR ⁶ or SR ⁶ group, or NR ⁷ R ⁸ groups, R ⁵ , R ⁶ , R ⁷ and R ⁸ are as described above, or the dotted line represents double bonds at 1,2, 3,4 positions of the quinone ring and R ¹¹ , R ¹² and R ¹³ are Each represents an -OCOR ¹⁴ group, wherein R ¹⁴ is an optionally substituted C _1-10 alkyl group, and X is halogen. ※ Note: The disclosure is based on the initial application.