239462-54-5Relevant academic research and scientific papers
Potent and selective TF/FVIIa inhibitors containing a neutral P1 ligand
Miura, Masanori,Seki, Norio,Koike, Takanori,Ishihara, Tsukasa,Niimi, Tatsuya,Hirayama, Fukushi,Shigenaga, Takeshi,Sakai-Moritani, Yumiko,Kawasaki, Tomihisa,Sakamoto, Shuichi,Okada, Minoru,Ohta, Mitsuaki,Tsukamoto, Shin-ichi
, p. 7688 - 7705 (2007/10/03)
Inhibition of tissue factor/factor VIIa complex (TF/FVIIa) is an attractive strategy for antithrombotic therapies. We began with an investigation of a non-amidine TF/FVIIa inhibitor based on a modification of amidine compound 1. Optimization of the substituents on the P1 phenyl portion of the compound 1 led to a neutral or less basic alternative for the 4-amidinophenyl moiety. By further optimization of the substituents on the central phenyl ring, a highly potent and selective TF/FVIIa inhibitor 17d was discovered.
Amidino derivatives and drugs containing the same as the active ingredient
-
Page column 107, (2010/01/30)
The novel amidino derivatives of the formula (I): wherein all the symbols are as in specification defined; have an inhibitory activity of a blood coagulation factor VIIa and are useful for treatment and/or prevention of several angiopathy caused by enhanc
