| 摘要 |
FIELD: biochemistry, more particularly NO syntase-induced enzyme inhibitors. SUBSTANCE: present invention describes amidine derivatives of formula: HN=C(R<SP>1</SP>)-NH-Q-C(NH<SB>2</SB>)-CO<SB>2</SB>H, salts, pharmaceutically acceptable ethers and amides thereof wherein R is C<SB>1</SB>-C<SB>6</SB>- alkyl, C<SB>2</SB>-C<SB>6</SB>-alkenyl, C<SB>2</SB>-C<SB>6</SB>-alkynyl, C<SB>3</SB>-C<SB>6</SB>-cycloalkyl, C<SB>3</SB>-C<SB>6</SB>- cycloalkyl-C<SB>1</SB>-C<SB>6</SB>-alkyl; Q is C<SB>3</SB>-C<SB>6</SB>-alkylene, C<SB>3</SB>-C<SB>6</SB>-alkenylene or C<SB>3</SB>-C<SB>6</SB> alkynylene group which is optionally substituted by one or more C<SB>1</SB>-C<SB>3</SB>-alkyl; or group of formula: (CH<SB>2</SB>)<SB>p</SB>X(CH<SB>2</SB>)<SB>q</SB> wherein p is 2 or 3; q is 1 or 2; X is S(O)<SB>x</SB> (wherein X is 0, 1 or 2), -O-, -NR<SP>2</SP>, wherein R is H, C<SB>1</SB>-C<SB>6</SB>-alkyl; or Q is (CH<SB>2</SB>)<SB>n</SB>A(CH<SB>2</SB>)<SB>s</SB> 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 CH<SB>2</SB>CH<SB>2</SB>CH<SB>2</SB> or CH<SB>2</SB>CH<SB>2</SB>CH<SB>2</SB>CH<SB>2</SB> if R is methyl, and is not CH<SB>2</SB>CH<SB>2</SB>CH<SB>2</SB> if R is ethyl. EFFECT: improved properties of the title compounds. 4 cl, 17 ex, 1 tbl
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