266690-86-2Relevant academic research and scientific papers
FACTOR XIIa INHIBITORS
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Page/Page column 20; 25-26, (2018/06/06)
The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
FACTOR XIIa INHIBITORS
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Page/Page column 24, (2018/06/06)
The present invention provides a compound of Formula (I) and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIIa inhibitors.
Serine protease inhibitor
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Page/Page column 21-22, (2010/02/11)
A serine protease inhibitor having the formula (I), in which J is H, R1, R1—O—C(O)—, R1—C(O—, R1—SO2—, R3OOC—(CHR2)p—, (R2a,R2b)N—CO—(CHR2)p— or Het-CO—(CHR2)p—;W is an amino-acid of the formula —NH—CHR1—C(O)—, —NR4—CH((CH2)qC(O)OR1)—C(O)—, —NR4—CH((CH2)qC(O)N(R2a,R2b))—C(O)—, —NR4—CH((CH2)qC(O)Het)-C(O)—, D-1-Tiq, D-3-Tiq, D-Atc, Aic, D-1-Piq, D-3 Piq, glutanyl or a (C1-C6) alkylester thereof;E is —NR2—CH2— or the fragment ?which is unsubstituted or substituted with (1-6C)alkyl, (1-6C)alkoxy or benzyloxy;R1 is selected form (1-12C)alkyl, (2-12C)alkenyl, (2-12C)alkynyl, (3-12C)cycloalkyl and (3-12C)cycloalkyl(1-6C)alkylene, which groups are unsubstituted or substituted with (3-12C)cycloalkyl, (1-6C)alkoxy, oxo, OH, CF3 or halogen, and from (6-14C)aryl, (7-15C)aralkyl, (8-16C)aralkenyl and (14-20C)(bisary)alkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-12C)cycloalkyl, (1-6C)alkoxy, OH, CF3 or halogen;R2, R2a and R2b are each independently selected from H, (1-C)alkyl, (3-8C)alkenyl, (3-8C)alkynyl, (3-8C)cycloalkyl and (3-6C)cycloalkyl(1-4C)alkylene, which are unsubstituted or substituted with (3-6C)cycloalkyl, (1-6C)alkoxy, CF3 or halogen, and from (6-14C)aryl and (7-15C)aralkyl, wherein the aryl groups are unsubstituted or substituted with (1-6C)alkyl, (3-6C)cycloalkyl, (1-6C)alkoxy, CF3 or halogen;R3 is the same as R2 or is Het-(1-6C)alkyl;R4 is H or (1-3C)alkyl;X and Y are CH or N, with the proviso that they are not both N;Het is a 4-, 5- or 6-membered heterocycle containing one or more heteroatoms selected from O, N and S;m is 1 or 2;p is 1, 2 or 3;q is 1, 2 or 3;t is 2, 3 or 4;or a pharmaceutically acceptable addition salt or solvate thereof.
