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New 1,4-naphthoquinone derivs. - used for treatment and prophylaxis of Pneumocystis carinii infections and malaria

机译:新的1,4-萘醌衍生物。 -用于治疗和预防卡氏肺孢子虫感染和疟疾

摘要

A compsn. for the treatment and/or prophylaxis of Pneumocystis carinii infections in mammals comprises a 1,4-naphthoquinone deriv. of formula (I) or its salts and a carrier. In (I), (R3 = 1-35C non-aromatic hydrocarbon residue opt. substd.; R4 = OH, halogen, OCOR5, OR6, SR6 or NR7R8; R5 = 1-10C alkyl, 3-10C cycloalkyl, 1-10C alkoxy or a phenyl or naphthyl gp., each such R5 gp. being opt. substd. e.g. by amino, mono- or di-1-4C alkyl-amino, carboxy or OH; R6 = opt. substd. 1-10C alkyl, 3-10C cycloalkyl, phenyl or naphthyl gp. as defined for R5; R7,R8 = H or 1-4C alkyl or the gp. NR7R8 represents a 5-7 membered satd. heterocyclic ring which may opt. contain a further heteroatom selected from N, O or S). Also claimed are naphthoquinone cpds. of formula (II), where R11,R12 = O and the dotted line represents a double bond between the 2 and 3 positions of the quinone ring in which case R13 is OCOR5, OR6, SR6 or NR7R8; or the dotted line represents double bonds at the 1,2 and 3,4 positions of the quinol ring and R11,R12 and R13 each represent OCOR14, where R14 is opt. substd. 1-10C alkyl.
机译:一个compsn。用于治疗和/或预防卡氏肺孢子虫感染的哺乳动物包含1,4-萘醌衍生物。式(I)的化合物或其盐和载体。在(I)中,(R3 = 1-35C非芳族烃残基,优选; R4 = OH,卤素,OCOR5,OR6,SR6或NR7R8; R5 = 1-10C烷基,3-10C环烷基,1-10C烷氧基或苯基或萘基gp。,每个这样的R5 gp.opt。例如被氨基,单-或二-1-4C烷基-氨基,羧基或OH取代; R6 = optsubd.1-10C烷基, R 5所定义的3-10C环烷基,苯基或萘基; R 7,R 8 = H或1-4 C烷基或gp NR 7 R 8表示5-7元饱和的杂环,其可以选择含有选自以下的其他杂原子N,O或S)。还要求保护萘醌cpds。式(II)的化合物,其中R 11,R 12 = O,并且虚线表示醌环的2位和3位之间的双键,在这种情况下,R 13为OCOR 5,OR 6,SR 6或NR 7 R 8。或虚线代表在喹啉环的1,2和3,4位的双键,R11,R12和R13分别代表OCOR14,其中R14是opt。取代1-10C烷基。

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