SUBSTITUTED BENZAMIDINE DERIVATIVES

medicine. SUBSTANCE: described are substituted benzamidine derivatives of general formula I: wherein A is O-CmH2m-X1 or group of formula IV: ; m is 2-6; X1 is group formula: ; X3 is O-CnH2n-; X2 is -CnH2n-O-;; n is 1 or 2; R1 is OH, COR7 or COOR7;; R2 is (C1-C6) alkyl, -CR5R6 aryl or hydrogen (is A...

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Hauptverfasser: EHRNST-OTTO RENT, FRANTS BIRKE, RAL'F ANDERSKEVITTS, KURT SHROMM, ARMIN FJUGNER, KRISTOFER MID, KHUBERT KHOJER
Format: Patent
Sprache:eng
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Zusammenfassung:medicine. SUBSTANCE: described are substituted benzamidine derivatives of general formula I: wherein A is O-CmH2m-X1 or group of formula IV: ; m is 2-6; X1 is group formula: ; X3 is O-CnH2n-; X2 is -CnH2n-O-;; n is 1 or 2; R1 is OH, COR7 or COOR7;; R2 is (C1-C6) alkyl, -CR5R6 aryl or hydrogen (is A is residue of formula IV or X1 is residue of formula III, (C1-C6) alkoxy (if A is -OCmH2m-X1- and X1 is group of formula III; R3 is hydrogen, (C1-C6) alkyl, (C1-C6) alkoxy (provided that X2 is -CR5R6 aryl or if X1 is group of formula III; R4 is H or (C1-C6) alkyl; R5 and R6 are (C1-C4) alkyl; R7 is alkyl, (C5-C7) cycloalkyl, aryl, heteroaryl with nitrogen atom as heteroatom. Said derivatives have antogonistic effect on receptors of B4 lenkotriene; provided that if A is -OCmH2m-X1-; m is 2,3 or 4, X1 is group of formula III; R2 is H or (C1-C6) alkyl, R3 is H,(C1-C6) alkyl, (C1-C6) alkoxy; R4 is hydrogen or (C1-C6) alkyl, then R1 is other than OH. EFFECT: improved properties of the title compounds. 10 cl, 8 ex