Discovery of Imidazo[1,5-c]imidazol-3-ones: Weakly Basic, Orally Active Factor Xa Inhibitors
Y Imaeda, T Kuroita, H Sakamoto… - Journal of medicinal …, 2008 - ACS Publications
The coagulation enzyme factor Xa (FXa) has been recognized as a promising target for the
development of new antithrombotic agents. We previously found compound 1 to be an orally …
development of new antithrombotic agents. We previously found compound 1 to be an orally …
The design of phenylglycine containing benzamidine carboxamides as potent and selective inhibitors of factor Xa
SD Jones, JW Liebeschuetz, PJ Morgan… - Bioorganic & medicinal …, 2001 - Elsevier
Factor Xa, a critical serine protease in the blood coagulation cascade, has become a target
for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we …
for inhibition as a strategy for the invention of novel anti-thrombotic agents. Here we …
Coagulation factor Xa inhibition: biological background and rationale
J Leadley - Current topics in medicinal chemistry, 2001 - ingentaconnect.com
Ischemic heart disease and cerebrovascular disease are the leading causes of death in the
world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due …
world. Surprisingly, these diseases are treated by relatively antiquated drugs. However, due …
Novel FXa inhibitor identification through integration of ligand-and structure-based approaches
CF Lagos, GF Segovia, N Nuñez-Navarro, MA Faúndez… - Molecules, 2017 - mdpi.com
Factor Xa (FXa), a vitamin K-dependent serine protease plays a pivotal role in the
coagulation cascade, one of the most interesting targets for the development of new …
coagulation cascade, one of the most interesting targets for the development of new …
Design, synthesis and biological activity of novel non-amidine factor Xa inhibitors. Part 1: P1 structure–activity relationships of the substituted 1-(2-Naphthyl)-1H …
ZJ Jia, Y Wu, W Huang, E Goldman, P Zhang… - Bioorganic & medicinal …, 2002 - Elsevier
Based on DuPont Pharmaceuticals' monobenzamidine lead structure SN429, we have
designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of …
designed the biphenyl 1-(2-naphthyl)-1H-pyrazole-5-carboxylamides as a novel series of …
Structure and property based design of factor Xa inhibitors: Pyrrolidin-2-ones with biaryl P4 motifs
RJ Young, AD Borthwick, D Brown… - Bioorganic & medicinal …, 2008 - Elsevier
Structure and property based drug design was exploited in the synthesis of
sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups …
sulfonamidopyrrolidin-2-one-based factor Xa (fXa) inhibitors, incorporating biaryl P4 groups …
Design, synthesis, and biological activity of novel factor Xa inhibitors: 4-aryloxy substituents of 2, 6-diphenoxypyridines
HP Ng, BO Buckman, KA Eagen, WJ Guilford… - Bioorganic & medicinal …, 2002 - Elsevier
A novel series of triaryloxypyridines have been designed to inhibit factor Xa, a serine
protease strategically located in the coagulation cascade. Inhibitor 5e has a KI against factor …
protease strategically located in the coagulation cascade. Inhibitor 5e has a KI against factor …
Biarylmethoxy isonipecotanilides as potent and selective inhibitors of blood coagulation factor Xa
G Lopopolo, F Fiorella, M de Candia, O Nicolotti… - European Journal of …, 2011 - Elsevier
New chloro-substituted biarylmethoxyphenyl piperidine-4-carboxamides were synthesized
and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and …
and assayed in vitro as inhibitors of the blood coagulation enzymes factor Xa (fXa) and …
Preparation of meta-amidino-N, N-disubstituted anilines as potent inhibitors of coagulation factor Xa
JM Fevig, J Cacciola, RS Alexander, RM Knabb… - Bioorganic & medicinal …, 1998 - Elsevier
The serine protease factor Xa is a critical enzyme in the blood coagulation cascade.
Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the …
Recently, the inhibition of factor Xa has begun to emerge as an attractive strategy for the …
Sulfonamidopyrrolidinone factor Xa inhibitors: potency and selectivity enhancements via P-1 and P-4 optimization
YM Choi-Sledeski, DG McGarry… - Journal of medicinal …, 1999 - ACS Publications
Sulfonamidopyrrolidinones were previously disclosed as a selective class of factor Xa (fXa)
inhibitors, culminating in the identification of RPR120844 as a potent member with efficacy …
inhibitors, culminating in the identification of RPR120844 as a potent member with efficacy …