91192-27-7Relevant academic research and scientific papers
NITROGEN CONTAINING HETEROAROMATICS AS FACTOR Xa INHIBITORS
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Page/Page column 70, (2009/10/01)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula (I) or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
Nitrogen containing heteroaromatics as factor Xa inhibitors
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, (2008/06/13)
The present application describes nitrogen containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is N or NH and D may be C(=NH)NH2, which are useful as inhibitors of factor Xa.
3-AMIDINOANILINE DERIVATIVES, ACTIVATED BLOOD COAGULATION FACTOR X INHIBITORS, AND INTERMEDIATES FOR PRODUCING BOTH
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, (2008/06/13)
The present invention relates to a 3-amidinoaniline derivative represented by the general formula: wherein R represents a hydrogen atom, a lower alkyl group, a lower alkenyl group etc.; R1 represents a hydrogen atom, a hydroxy group, a lower alkyl group etc.; Y represents a single bond or an oxygen atom; and R2 represents a lower alkyl group or a group represented by the general formula: wherein n represents 1 or 2; and T represents a hydrogen atom or a group represented by the general formula:-C(=NH)-W wherein W represents a lower alkyl group; or a pharmaceutically acceptable salt thereof, which has a potent and selective activated blood coagulation factor X inhibitory activity, and an intermediate for producing both.
Use of conformationally restricted benzamidines as arginine surrogates in the design of platelet GPIIb-IIIa receptor antagonists
Sall, Daniel J.,Arfsten, Ann E.,Bastian, Jolie A.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Morin Jr., John M.,Rose, Jack W.,Scarborough, Robert M.,Smyth, Mark S.,Um, Suzane L.,Utterback, Barbara G.,Vasileff, Robert T.,Wikel, James H.,Wyss, Virginia L.,Jakubowski, Joseph A.
, p. 2843 - 2857 (2007/10/03)
The use of 5,6-bicyclic amidines as arginine surrogates in the design of a novel class of potent platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists is described. The additional conformational restriction offered by the bicyclic nucleus results in 20-400-fold increases in potency compared to the freely flexible, acyclic benzamidine counterpart. The design, synthesis, structure-activity relationships (SAR), and in vitro activity of this novel class of GPIIb-IIIa antagonists are presented.
Platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa) antagonists derived from amidinoindoles
Sall, Daniel J.,Arfsten, Ann E.,Berry, Dennis R.,Denney, Michael L.,Harms, Cathy S.,McCowan, Jefferson R.,Ray, Judith K.,Scarborough, Robert M.,Um, Suzane L.,Utterback, Barbara G.,Jakubowski, Joseph A.
, p. 81 - 86 (2007/10/03)
A series of substituted amidinoindoles have been prepared as mimics of the RGD sequence and were studied as antagonists of the platelet glycoprotein IIb-IIIa receptor (GPIIb-IIIa). The agents were potent and selective antagonists of GPIIb-IIIa. Compared to their acyclic counterparts, the amidinoindole series bound with 10- to 20-fold greater affinity, indicating the advantages of added conformational restriction and/or hydrophobicity in the basic region of RGD mimics.
