| 摘要 |
The amino acid derivative has the formula I or a pharmaceutical acceptable salt thereof limited by the provisos listed in the specification wherein: R1 is H, C(O)R11, SiR12R13R14 or optionally substituted alkyl; R12, R13 and R14 are independently H, phenyl or alkyl; R11 is H or alkyl; R2 and R3 is H, alkyl, cyclohexyl or phenyl; Rx is a group of formula IIA, IIb or IIc; k, l, m and n are independently 0 to 4; R4 and R5 are independently H, Si(Me)3, 1- or 2-naphthyl, a polycyclic hydrocarbyl group, CHR41R42 or optionally fluoro substituted alkyl or optionally substituted cycloalkyl, phenyl, methylenedioxyphenyl, benzodioxanyl, benzofuranyl, dihydrobenzofuranyl, benzothiazolyl, benzoxazolyl, benzimidazolyl, coumaranoyl, coumarinyl or dihydrocoumarinyl; R41 and R42 are independently cyclohexyl or phenyl; R6 and R7 are independently H, alkyl, cycloalkyl, optionally substituted phenyl, or together with the carbon to which they are attached form a cycloalkyl group; Y is CH2, (CH2)2, CH=CH or optionally substituted (CH2)3, CH2CH=CH or CH=CHCH2; B is a group of formula IVA, IVB or IVC and X1 and X2 are independently a single bond or CH2. A pharmaceutical composition thereof useful as a thrombin inhibitor or as an anticoagulant.
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