| 摘要 |
FIELD: medicine. ^ SUBSTANCE: invention refers to imidazole derivatives of formula (1a): and/or to stereoisomeric forms of compound of formula (1a) and/or to physiologically acceptable salt of compound of formula (1a), and U means 1) hydrogen atom; X means the remaining formula (II): -(A1)m-A2 (II), where m means an integer 1; A1 means 1) -(CH2)n- where n means an integer 1; A2 means 1) aminopyridyl; Y means 1) the remaining formula (III): A3-(A4)o-(A5)p (III), and A3 means (C3-C8)-cycloalkyl or (C2-C6)-alkinylene wherein cycloalkyl or alkinylene is unsubstituted or independently one-, two- or three-substituted with R1, A4 is absent, A5 is absent; b) A3 means -(C3-C8)-cycloalkyl wherein cycloalkyl is unsubstituted or independently one-, two- or three-substituted with R1, A4 means -N(R2)- and A5 means a)1) -C(O)-R3; a)2) -C(O)-N(R4)-R5; a)3) -(SO2)-R6; O stands for an integer 1, and p stands for an integer 1; A3 means cyclic amine with 3-8 atoms in cycle where cyclic amine is unsubstituted, A4 is absent; and A5 has value specified in cl. b), and A5 is connected with N-atom A3, o means an integer zero and p means an integer zero or 1; or d) A3 means -(CH2)q-phenyl wherein phenyl is unsubstituted or independently one-, two- or three-substituted with R1, A4 is absent; and A5 has value specified in cl. b), p means an integer 1 and q means integer zero or 1;) A3 means -(CH2)rHet wherein Het stands for benzothiophene or piperidine which is unsubstituted or independently one-, two- or three-substituted by =0 or R1, A4 is absent; and A5 has value specified cl. b), p means an integer 1 and r means an integer 1 or 2; f) A3 means -(CH2)q-phenyl wherein phenyl is unsubstituted, A4 means -O- A5 means phenyl wherein phenyl is unsubstituted or independently one-, two- or three-substituted by R1, o and p mean an integer 1, and q means an integer zero, 1; g) -CH(-phenyl)-phenyl; and R1 means phenyl, and phenyl is unsubstituted or independently one-, two- or three-substituted by -(C1-C6)alkyl, b) triazolyl,) c) - (C1-C6)-alkyl, d) - (C0-C4)-alkyl - (C3-C8) a-cycloalkyl, e) -O-CF3 or g) halogen; and R2 means: a) hydrogen atom; and R3 and R6 are identical or different and independently mean: a) -(C1-C6)-alkyl wherein alkyl is unsubstituted or independently one-, two- or three-substituted by R1, b) -phenyl wherein phenyl is unsubstituted or independently one-, two- or three-substituted by R1, while R4 and R5 are identical or different and independently mean: a) -(C1-C6)-alkyl or -(C2-C10)-alkenyl wherein alkyl or alkenyl is unsubstituted, b) -phenyl wherein phenyl is unsubstituted, c) hydrogen atom; Y means 2) the remaining formula (IV): , and R8 means a) -phenyl where phenyl is unsubstituted; Z means 1) hydrogen atom, 2) -(C1-C6)-alkyl, 3) -(C1-C6)-alkyl, 4) -(C0-C4)-alkyl-(C3-C6)-cycloalkyl, 5) -(C1-C10)-alkyl-O-C(O)-O-R1. Besides the invention concerns the method for making the compound of formula (1a) and the based medicinal agent for inhibition of TAFIa enzyme. ^ EFFECT: production of new compounds and the based medicinal agent to be used in medicine to prevent and treat the conditions accompanied with thromboses, embolism, hypercoagulation or fibrotic changes. ^ 8 cl, 1 tbl, 47 ex |
