| 摘要 |
<p>The invention comprises compounds of the formula <FORM:1007334/C2/1> wherein R1 is hydrogen, halogen, triflouromethyl, hydroxy, C1- 3 alkyl, C1- 3 alkoxy or C1- 3 alkylmercapto; A is <FORM:1007334/C2/2> which is bound to the nucleus either directly or through an intermediate -NH- or -CH2-group, in which R2 and R3 are hydrogen, C1- 7 alkyl, C1- 7 alkenyl, C1- 7 cycloalkyl, phenyl or C7- 10 phenylalkyl in which a methylene group, other than a -methylene, may be replaced in the alkyl or alkenyl groups by -O-or -S- or in which R2 and R3 together represent ethylene or propylene in which individual hydrogen atoms can be replaced by alkyl groups containing in total not more than 6 carbon atoms which can also together form a ring, and in which R4 is hydrogen or C1- 6 alkyl; B has one of the meanings of A or of R1; n is 2, 3 or 4; and X is -R-, -R-Y-R, -R-NH-Y-R, -R-NH-Y-NH-R, <FORM:1007334/C2/3> or <FORM:1007334/C2/4> wherein R is -CO- or -CS-, Y has one of the meanings of Y1, Y2 and Y3 as well as of -Y1-Y3-, -Y1-Y3-Y1- and -Y3-Y1-Y3 wherein Y1 is a mono or binuclear aromatic group which may be substituted by R5 and R6; Y2 is a 5-membered heterocyclic ring with one oxygen, sulphur or nitrogen atom as the hetero atom, or a 6-membered heterocyclic ring, if desired condensed with benzene, with one or two nitrogen atoms as hetero atoms, and Y3 is -CH=CH-; Z is -N=N-, -NH-R-NH-, -NH-R-Y-R-NH-, -NH-R-NH-Y-NH-R-NH- or -NH-R-(CH2)p-R-NH-, p being an integer from 1 to 8 and m being 1 or 2; and R5 and R6 are hydrogen, halogen, trifluoromethyl, hydroxy, mercapto, amino, nitro, carboxyl or carboxylic amide, or alkyl, alkoxy, alkylmercapto or acylamino with not more than 3 carbon atoms linked directly with one another; but excludes compounds in which X is -CO- and at the same time R2, R3 and R4 are hydrogen or C1- 4 alkyl; and acid-addition salts thereof; and their preparation (1) by reacting the amine <FORM:1007334/C2/5> with a polybasic acid <FORM:1007334/C2/6> or a reactive derivative thereof; or (2) reacting one of the amines <FORM:1007334/C2/7> or a mixture of 2 or more such amines with an acid HO-R-Y-R-OH or HO-R-(CH2p-R-OH or a reactive derivative thereof; or (3) reacting an amine of one of the formulae II, IV or V, or a mixture of 2 or more such amines with a carbonic acid or a reactive derivative thereof, e.g. phosgene, or a corresponding thio compound, e.g. thiophosgene, or carbon disulphide; or by reacting one of these amines with a compound of a similar formula in which the amino group is replaced by an isocyanate or isothiocyanate group; or by reacting by an isocyanate or isothiocyanate groups; or by reacting one of these amines or a mixture thereof with a compound R=N-Y-N=R; or reacting an amine IV or V or a mixture thereof with a compound R=N-(CH2p-N=R; or reacting one or a mixture of several amines of the formula II with a compound <FORM:1007334/C2/8> or (4) reacting an isocyanate or isothiocyanate of one of the formulaae <FORM:1007334/C2/9> or a mixture thereof with a diamine NH2-Y-NH2, or reacting a compound IVA or VA or a mixture thereof with the diamine NH2-(CH2)p-NH2, or reacting one or a mixture of several compounds IIA with a diamine or tetra-amine <FORM:1007334/C2/100> or (s) reacting a compound of the formula <FORM:1007334/C2/111> (wherein A1 is <FORM:1007334/C2/122> and B1 has one of the meanings of A1 or R1) with the amine NHR3R4, or reacting a compound of the formula IA wherein A1 is <FORM:1007334/C2/133> with the diamine H2N-R2-R3-NH2. Examples are given. 4 - Amino - 41 - (2 - imidazolin - 2 - yl)-benzanilide is prepared by condensation of 2-(p - aminophenyl) - imidazoline and p - aminobenzoic acid. 4 - Cyano - 31 - [(p - cyanophenyl) - carbanoyl] - carbanilide is prepared by reaction of m-aminobenzoyl - p1 - cyananiline with p-cyanophenyl isocyanate, and is reacted with hydrogen sulphide to give 4-thioamido - 31 - [(p - thioamidophenyl) - carbamoyl]-carbanilide. The compounds of the invention, which are stated to have use as tuberculostats, in cancer treatment and for treatment of trypanozoa infections, may be made up itno pharmaceutical compositions with suitable carriers. Solutions, suspensions, powders and ointments are referred to.</p> |
