177476-75-4Relevant academic research and scientific papers
Substituted Heteroaryl Spiropyrrolidine MDM2 Antagonists
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, (2012/03/10)
There are provided compounds of the general formula wherein A, B, V, W, R1, R2, R3, R3, and R4, are as described herein and enantiomers and pharmaceutically acceptable salts thereof. The compounds are useful as anticancer agents.
SPIROINDOLINONE PYRROLIDINES
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, (2011/06/23)
There are provided compounds of the formula wherein X, Y and R1 to R8 are described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.
SPIROINDOLINONE PYRROLIDINES
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, (2011/11/12)
There are provided compounds of the formula (I) wherein X, Y and R1 to R8 are as described herein, their enantiomers and pharmaceutically acceptable salts and esters, as well as processes for making these compounds and medicaments containing them.
THIAZOLONES FOR USE AS PI3 KINASE INHIBITORS
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, (2008/06/13)
Invented is a method of inhibiting the activity/function of PI3 kinases using substituted thiazolones. Also invented is a method of treating one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, ne
2,4-DI(AMINOPHENYL) PYRIMIDINES AS PLK INHIBITORS
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Page/Page column 64, (2008/06/13)
The invention relates to compounds of general formula (1), wherein A, W, X, Y, Z, Ra, Rb, Rc, R1, and R3 are defined as indicated in claim 1. Said compounds are used for the treatment of diseases characterized by excessive or anomalous cell proliferation. Also disclosed is the use of the inventive compounds for producing a medicament having said properties.
NOVEL CHEMICAL COMPOUNDS
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Page/Page column 39, (2010/02/13)
This invention relates to newly identified compounds for inhibiting hYAK3 proteins and methods for treating diseases associated with the imbalance or inappropriate activity of hYAK3 proteins.
Development of serine protease inhibitors displaying a multicentered short (<2.3 ?) hydrogen bond binding mode: Inhibitors of urokinase-type plasminogen activator and factor Xa
Verner,Katz,Spencer,Allen,Hataye,Hruzewicz,Hui,Kolesnikov,Li,Luong,Martelli,Radika,Rai,She,Shrader,Sprengeler,Trapp,Wang,Young,Mackman
, p. 2753 - 2771 (2007/10/03)
Novel scaffolds that bind to serine proteases through a unique network of short hydrogen bonds to the catalytic Ser195 have been developed. The resulting potent serine protease inhibitors were designed from lead molecule 2-(2-hydroxyphenyl)1H-benzoimidazo
Design and SAR of novel potassium channel openers targeted for urge urinary incontinence. 1. N-cyanoguanidine bioisosteres possessing in vive bladder selectivity
Butera, John A.,Antane, Madelene M.,Antane, Schuyler A.,Argentieri, Thomas M.,Freeden, Chris,Graceffa, Russell F.,Hirth, Bradford H.,Jenkins, Douglas,Lennox, Joseph R.,Matelan, Edward,Norton, N. Wesley,Quagliato, Dominick,Sheldon, Jeffrey H.,Spinelli, Walter,Warga, Dawn,Wojdan, Alexandra,Woods, Morgan
, p. 1187 - 1202 (2007/10/03)
A structurally novel series of adenosine 5'-triphosphate-sensitive potassium (K(ATP)) channel openers is described. As part of our efforts directed toward identifying novel, bladder-selective potassium channel openers (KCOs) targeted for urge urinary incontinence (UUI), we found that bioisosteric replacement of the N-cyanoguanidine moiety of pinacidil (1, Figure 1) with a diaminocyclobutenedione template afforded squaric acid analogue 2, the prototype of a novel series of K(ATP) channel openers with unique selectivity for bladder smooth muscle in vive. Further modification of the heterocyclic ring to give substituted aryl derivatives (3) afforded potent KCOs that possessed the desired detrusor selectivity when administered orally. The effects of these potassium channel agonists on bladder contractile function was studied in vitro using isolated rat detrusor strips. Potent relaxants were evaluated in vive in a rat model of bladder instability. Lead compounds were evaluated concomitantly in normotensive rats for their effects on mean arterial blood pressure (MAP) and heart rate as a measure of in vive bladder selectivity. (R)-4-[3,4-Dioxo-2-(1,2,2-trimethyl- propylamino)-cyclobut-1-enyαmino]-3-ethyl-benzonitrile (79) met our potency and selectivity criteria and represents an attractive development candidate for the treatment of UUI. Electrophysiological studies using isolated rat bladder detrusor myocytes have demonstrated that compound 79 produces significant hyperpolarization which is glyburide-reversed, thus consistent with the activation of K(ATP). The design, synthesis, structure-activity relationships (SAR), and pharmacological activity associated with this series of novel KCOs will be discussed.
Substituted N-heteroaryl and N-aryl-1,2-diaminocyclobutene-3,4-diones
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, (2008/06/13)
The compounds of the formula: STR1 wherein: R1 and R2 are, independently, hydrogen, straight or branched chain alkyl or mono- or bi-cyclic alkyl; A is a substituted phenyl group containing one cyano substituent and one substituent se
