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
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creator EHRNST-OTTO RENT
FRANTS BIRKE
RAL'F ANDERSKEVITTS
KURT SHROMM
ARMIN FJUGNER
KRISTOFER MID
KHUBERT KHOJER
description 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
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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. 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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. 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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</abstract><edition>7</edition><oa>free_for_read</oa></addata></record>
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
title SUBSTITUTED BENZAMIDINE DERIVATIVES
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