Substituted bis-(4-aminophenyl)-sulfones, their preparation...

C - Chemistry – Metallurgy – 07 – C

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C07C 317/36 (2006.01) A61K 31/135 (2006.01) C07C 205/26 (2006.01) C07C 205/34 (2006.01)

Patent

CA 1315287

27169-103 ABSTRACT Bis-(4-aminophenyl)-sulfones The invention relates to new bis(4-aminophenyl)- sulfones of formula I Image (I) (wherein R1 represents a hydrogen atom, an alkyl group with 1 to 7 carbon atoms or a cycloalkyl group with 3 to 7 carbon atoms; R2 represents a hydrogen atom or an alkyl group with 1 to 3 carbon atoms; R3 represents a nitrile, alkylaminocarbonyl, dialkylamino- carbonyl, N-cycloalkyl-alkylaminocarbonyl, alkylamino, dialkylamino, dialkylaminocarbonylalkoxy, alkylamino- sulfonyl, dialkylaminosulfonyl, hydroxyalkyl, alkyl- carbonyl, aminoalkyl or alkoxyalkyl group, or, if R1 and R2 represent hydrogen atoms, R3 may also represent a hydroxy, hydroxycarbonylalkoxy or dialkylaminoalkoxy group, or, if R1 represents an alkyl or cycloalkyl group and R2 represents a hydrogen atom or an alkyl group, R3may also represent a halogen atom or a trifluoromethyl, nitro, amino, aminosulfonyl, aminocarbonyl, alkyl, carboxy or alkoxycarbonyl group; and R4 represents a hydrogen atom or, if R1 and R2 both represent hydrogen atoms and R3 in the 2 position represents a halogen atom or a hydroxy group, R4 may also represent a halogen atom or a hydroxy or alkoxy group; and wherein in groups R3 and R4 any alkyl moiety contains from 1 to 3 carbon atoms and any cycloalkyl moiety contains from 3 to 7 carbon atoms) and the acid addition salts thereof. The compounds have valuable pharmacological properties, particularly an inhibiting effect on bacteria, mycobacteria and plasmodia.

481752

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