FIELD: biochemistry, more particularly NO syntase-induced enzyme inhibitors. SUBSTANCE: present invention describes amidine derivatives of formula: HN=C(R1)-NH-Q-C(NH2)-CO2H, salts, pharmaceutically acceptable ethers and amides thereof wherein R1 is C1-C6- alkyl, C2-C6-alkenyl, C2-C6-alkynyl, C3-C6-cycloalkyl, C3-C6- cycloalkyl-C1-C6-alkyl; Q is C3-C6-alkylene, C3-C6-alkenylene or C3-C6 alkynylene group which is optionally substituted by one or more C1-C3-alkyl; or group of formula: (CH2)pX(CH2)q wherein p is 2 or 3; q is 1 or 2; X is S(O)x (wherein X is 0, 1 or 2), -O-, -NR2, wherein R2 is H, C1-C6-alkyl; or Q is (CH2)nA(CH2)s wherein, r is 0, 1 or 2; s is 0,1 or 2; A is aromatic or 3-6 membered heterocyclic ring having sulfur atom provided that Q is not CH2CH2CH2 or CH2CH2CH2CH2 if R1 is methyl, and is not CH2CH2CH2 if R1 is ethyl. EFFECT: improved properties of the title compounds. 4 cl, 17 ex, 1 tbl
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Authors
Dates
1999-05-10—Published
1992-12-23—Filed