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filingDate 1992-02-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5d91f09c86847b02e6efb7dff687ac53
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publicationDate 1993-08-12-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber DE-4203201-A1
titleOfInvention NEW AMIDINE DERIVATIVES, THEIR PREPARATION AND USE
abstract Amidino-benzene, pyridine, thiophene or naphthalene derivs. of formula (I), as racemates or in enantiomerically pure or enriched form, opt. as diastereomer pairs or as cis- or trans-isomer, and their salts are new. In formula (I), R1, R2 are e.g., CF3, halogen, R5, OR5, COR6, SR6, SOR6, SO2R6, etc.; or R1+R2 on adjacent C is CH=CH-CH=CH, OCH2CH2, OCH2O, OCH2CH2O, etc.; R3 is e.g. halogen, OH, CF3, R5, OR6, COR6, SR6, SOR6, SO2R6; provided that R3 can only be H when at least one of R1 and R2 is other than H; R4 is halogen, R5 or OR5; R5 is H, 1-12C alkyl or phenyl (opt. substd. by halogen, 1-4C alkyl, 1-4C alkyl, 1-4C alkoxy or 2-5C acyl); R6 is 1-12C alkyl or phenyl (opt. substd. by halogen, 1-4C alkyl, 1-4C alkoxy or 2-5C acyl); A is X1-A1-X2, X2-A2-X3, X4-A2-X2, (CH2)x-NHCO-(CH2)y-X2 or CH=CH-A2X2; x is 1 or 2; y is 1-3; B is CH=CH, CH=N, S or o-phenylene; A1 is 2-4C alkylene, cis- or trans-CH=CHCH2, CH2CCCH2, -CH2-cyclohexylene-CH2 or -CH2-phenylene-CH2-; A2 is 1-5C alkylene; X1 is O, NH, S, SO, SO2, CO or CH2; X2 is O, NH or S; X3 is NHCO, CONH or SO2NH; and X4 is NHCO, CONH, NHSO2 or SO2NH. USE - (I) are leukotriene B4 (LTB4) antagonists and are used for prodn. of medicaments for treatment of diseases involving inflammatory and/or allergic reactions, esp. asthma, ulcerative colitis and psoriasis. (I) are administered topically, orally, transdermally, intranasally, parenterally or by inhalation, opt. in combination with other drugs, e.g., antiallergics, secretolytics, beta(2)-mimetics, steroids, antihistamines or PAF antagonists. Typical dose is 10-250 (pref. 20-200)mg orally or 2-20mg by inhalation. Typically EC50 for inhibition of LTB4-induced neutrophil aggregation is 0.5-0.05 micro-M.
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