- PAR4 AGONIST PEPTIDES
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The present invention provides PAR4 agonist peptides. These peptides are useful for developing robust PAR4 receptor assays.
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Page/Page column
(2013/11/06)
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- IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR 4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
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The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R5, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
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Paragraph 00161
(2013/11/18)
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- Non-ATP competitive glycogen synthase kinase 3β (GSK-3β) inhibitors: Study of structural requirements for thiadiazolidinone derivatives
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The 2,4-disubstituted thiadiazolidinones (TDZD) were described as the first non-ATP competitive GSK-3β inhibitors. New modifications in this heterocyclic ring are here reported to study the influence on the biological activity. The basic skeleton of 1,2,4-thiadiazole and also one of the carbonyl groups are kept, while different modifications are introduced in positions 3 and 5, respectively. The GSK-3β activity of the new thiadiazole derivatives here synthesized showed IC50 values for some of the compounds in the micromolar range. Additionally, ATP competition studies have been carried out, showing that as well as the first generation of TDZD, these new compounds act in a non-competitive manner. With this study, additional requirements for the biological activity of the TDZD family have been delineated.
- Castro, Ana,Encinas, Arantxa,Gil, Carmen,Braese, Stefan,Porcal, Williams,Perez, Concepcion,Moreno, Francisco J.,Martinez, Ana
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p. 495 - 510
(2008/04/05)
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- α-Heteroarylation of esters, lactones, amides, and lactams by nucleophilic aromatic substitution
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A mild and efficient α-heteroarylation of simple esters and amides was developed via nucleophilic aromatic substitution. The choice of NaHMDS in toluene gave the best results. A tandem α-heteroarylation and hydroxylation protocol using air as the oxidant
- Shen, Hong C.,Ding, Fa-Xiang,Colletti, Steven L.
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p. 1447 - 1450
(2007/10/03)
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