发明名称 INHIBITORS OF VIIA FACTOR
摘要 FIELD: organic chemistry, medicine. SUBSTANCE: invention relate to group of new compounds of the general formula (I): R1-A-B-D-En-R2 (I) wherein R1 represents R12C(O) being R12 is taken among the group comprising alkenyl, alkenyloxy-group or alkenylamino-group; A represents the group A1- A2-A3 wherein A1 represents NH; A2 represents CHR93 wherein R93 represents 4-amidinophenylmethyl; A 3 represents C(O); B represents the group B1-B2-B3 wherein B1 represents NH; B2 represents CHR97 wherein R97 represents ethyl that is substituted at position 2 with hydroxycarbonyl or alkyloxycarbonyl; B3 represents C(O); D represents the group D1-D2-D3 wherein D1 represents NH; D2 represents CR81R82 wherein R81 and R82 are taken independently among the group consisting of hydrogen atom and unsubstituted or substituted residues of alkyl, aryl, arylalkyl, heteroarylalkyl; D3 represents C(O); En represents (E1-E2-E3)n wherein n = 0 or 1; E1 represents NR70 wherein R70 represents hydrogen atom; E2 represents CR71R72 wherein R71 and R71 are taken independently among the group consisting of hydrogen atom and unsubstituted or substituted residues of alkyl, aryl, arylalkyl, heteroarylalkyl; E3 represents C(O); R2 represents NR21R22 wherein R21 and R22 are taken independently among hydrogen atom and unsubstituted or substituted residues of alkyl, aryl, arylalkyl, heteroarylalkyl and heterocycloalkylalkyl being alkyl comprises from 1 to 13 carbon atoms; alkenyl comprises from 2 to 13 carbon atoms; aryl and heteroaryl comprise from 5 to 13 ring carbon atoms wherein in heteroaryl residue one or some carbon atoms are substituted with heteroatoms taken among the group consisting of nitrogen, oxygen and sulfur atoms; heterocycloalkyl comprises from 3 to 8 ring carbon atoms among that from one to three carbon atoms are substituted with heteroatoms taken among the group consisting of nitrogen, oxygen and sulfur atoms; in any stereoisomeric forms or their mixtures taken in any ratio and their pharmaceutically acceptable salts. Invention relates also to method for preparing compounds of the general formula (I) that involves binding protected amino acids. Invention relates also to pharmaceutical composition eliciting ability to exert anti-thrombotic effect by means of activated VII factor (FVIIa) in blood coagulation factors system. EFFECT: valuable medicinal properties of compounds. 19 cl, 4 tbl, 22 ex
申请公布号 RU2223967(C2) 申请公布日期 2004.02.20
申请号 RU20010110086 申请日期 1999.09.02
申请人 发明人 SAFAR PAVEL;SAFAROVA ALENA;VAJLDGUZ PITER
分类号 A61K38/00;A61K38/06;A61K38/07;A61P7/00;A61P7/02;A61P9/00;A61P9/10;A61P29/00;A61P43/00;C07K1/04;C07K1/06;C07K5/068;C07K5/072;C07K5/09;C07K5/11 主分类号 A61K38/00
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