SULFONYLAMINOCARBOXYLIC ACID, PROCESS OF THEIR PREPARATION, MEDICAMENT IN WHICH THEY ARE COMPRISED AND THEIR USE
Sulphonamide derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 alkyl, 3-6C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrro...
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Zusammenfassung: | Sulphonamide derivatives of formula (I) and their stereoisomers and salts are new. R1 = Ar or Het; Ar = phenyl (optionally substituted by 1 or 2 alkyl, 3-6C cycloalkyl, OH, alkyl-COO-, alkyl-O-, alkyl-O-(1-4C alkylene)-O-, halo, CF3, CN, NO2, COOH, alkyl-O-CO-, OCH2O, NR4R5CO and NR4R5); Het = pyrrolyl, pyrazolyl, imidazolyl, triazolyl, thienyl, thiazolyl, oxazolyl, isoxazolyl, pyridinyl, pyrimidinyl, indolyl, benzothiophenyl, benzimidazolyl, benzoxazolyl or benzothiazolyl (all optionally substituted as for phenyl in Ar); R2, R4, R5 = H, alkyl, carboxyalkyl, Ar-(CH2)n- (in which Ar is further optionally substituted by 2-4C alkanoylamino) or picolyl; or NR4R5 = 4-7 membered ring (optionally with one C replaced by O, S or NH and optionally having two adjacent C forming part of a benzene residue); n = 0-2; R3 = H, 1-10C alkyl (optionally substituted by OH), 2-10C alkenyl, alkyl substituted by R2O-, R2S(O)m-, R2S(O)n=NH)- or a group of formula (i)); Ar-(CH2)m - (optionally substituted by OH in the (CH2)m chain and in which Ar is further optionally substituted by -O-(CH2)m-Ar and -CO(CH2)mAr); Het-(CH2)m- (optionally substituted by OH in the (CH2)m chain and in which Het is further optionally substituted by CHO, SO2Ar and -O(CH2)m-Ph); -(CH2)m-P(O)(OH)-(1-3C alkyl) or R6CO-alkyl-; or R2+R3 = (CH2)r (in which the obtained ring optionally has one ring C replaced by O, S or NR7 and is optionally substituted by alkyl, Ph, (CH2)mPh and/or OH); W = O, S or N; m = 0-6; r = 1-4; R6 = H, alkyl, Ar, Het or Het-(CH2)m-NH- (both further optionally ring-substituted by carboxy-(1-4C) alkyl), OH, OR2, NR4R5, NHNR4R5 or NHCHR3COOH; R7 = H, alkyl, Ar, CH2Ar or R2N-C(=NH)-; A = bond, O, CH=CH or C IDENTICAL C; B = (CH2)m, O(CH2)p or CH=CH; p = 1-5; X = CH=CH, O or S; and unless specified otherwise alkyl moieties have 1-6C. Also claimed are intermediates of formula (VI) (see "Preparation). |
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