| 摘要 |
<p>Sulfamide derivatives represented by general formula (1) or pharmacologically acceptable salts or hydrates thereof, characterized in that they have an excellent antithrombin activity and are useful as drugs for, e.g., the treatment of thrombosis, capable of oral administration, and reduced in side effects, wherein R1 represents hydrogen, lower alkyl, or amino-protective group; R2 represents optionally substituted and fused nitrogenous heterocycle; R3 represents a group represented by A-(CH2)m-, hydrogen, or optionally substituted lower alkyl (where A represents optionally substituted aryl, optionally substituted and fused heterocycle, or optionally substituted lower cycloalkyl, m is an integer of 0 to 6, and the moiety represented by -(CH2)m- may have at least one substituent); R4 represents hydrogen or lower alkyl; and R5 represents a group represented by -C(=NR6)NH2, -NH-C(=NR6)NH2, or -(CH2)n-NHR6 (where R6 represents hydrogen, lower alkyl, hydroxy, acyl, acyloxy, lower alkoxy, lower alkoxycarbonyl, lower alkoxycarbonyloxy, or lower hydroxyalkylcarbonyloxy, n is an integer of 0 to 2, and the moiety represented by -(CH2)n- may have at least one substituent).</p> |
