144656-11-1Relevant articles and documents
SUBSTITUTED PYRROLES AND METHODS OF USE
-
Page/Page column 36, (2010/01/07)
The invention relates to substituted pyrrole compounds of Formula (I) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chkl) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.
Cyclic urea derivatives, pharmaceutical compositions containing these compounds and processes for preparing them
-
, (2008/06/13)
The invention relates to cyclic urea derivatives of general formula STR1 wherein Ra, Rb, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.
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.
Cyclic urea derivatives, pharmaceutical compositions containing these compounds and methods of using the same
-
, (2008/06/13)
The invention relates to cyclic urea derivatives of general formula STR1 wherein Ra, Rb, X and Y are as defined herein, pharmaceutical compositions containing the derivatives and processes for preparing them.