5631-83-4Relevant academic research and scientific papers
PYRIDINE DERIVATIVES AS VEGFR-2 RECEPTOR AND PROTEIN TYROSINE KINASE INHIBITORS
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Page/Page column 40, (2010/04/06)
The invention relates to compounds of general formula (I) wherein W, D, E, G, J, L, R1, R2, R3, R4, R5 and Y are as defined herein, and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use -alone or in combination with one or more other pharmaceutically active compounds- in therapy, for treating diseases associated with deregulated angiogenesis, such as cancer and skin and eye diseases.
Structure-activity relationships of pregabalin and analogues that target the α2-δ protein
Belliotti, Thomas R.,Capiris, Thomas,Ekhato, I. Victor,Kinsora, Jack J.,Field, Mark J.,Heffner, Thomas G.,Meltzer, Leonard T.,Schwarz, Jacob B.,Taylor, Charles P.,Thorpe, Andrew J.,Vartanian, Mark G.,Wise, Lawrence D.,Zhi-Su, Ti,Weber, Mark L.,Wustrow, David J.
, p. 2294 - 2307 (2007/10/03)
Pregabalin exhibits robust activity in preclinical assays indicative of potential antiepileptic, anxiolytic, and antihyperalgesic clinical efficacy. It binds with high affinity to the α2-δ subunit of voltage-gated calcium channels and is a substrate of the system L neutral amino acid transporter. A series of pregabalin analogues were prepared and evaluated for their α2-δ binding affinity as demonstrated by their ability to inhibit binding of [3H]gabapentin to pig brain membranes and for their potency to inhibit the uptake of [3H]leucine into CHO cells, a measure of their ability to compete with the endogenous substrate at the system L transporter. Compounds were also assessed in vivo for their ability to promote anxiolytic, analgesic, and anticonvulsant actions. These studies suggest that distinct structure activity relationships exist for α2-δ binding and system L transport inhibition. However, both interactions appear to play an important role in the in vivo profile of these compounds.
OPIOID RECEPTOR ANTAGONISTS
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Page 44, (2010/02/08)
A compound of the formula I: (I) wherein the variables are as described herein, or a pharmaceutically acceptable salt, solvate, enantiomer, racemate, diastereomer or mixture thereof, formulations and methods of use thereof are disclosed.
Pyrazolo-[1,5-a]-1,3,5-triazine corticotropin-releasing factor (CRF) receptor ligands
Gilligan, Paul J.,Folmer, Beverly K.,Hartz, Richard A.,Koch, Stephanie,Nanda, Kausik K.,Andreuski, Stephen,Fitzgerald, Lawrence,Miller, Keith,Marshall, William J.
, p. 4093 - 4102 (2007/10/03)
The syntheses and rat CRF receptor binding affinities of 'retro-pyrazolotriazine' corticotropin-releasing factor (CRF) ligands 4 are reported. Some have high affinity for rat CRF receptors (Ki≤10 nM). The data provide additional support for the hypothesis that it is possible to interchange isosteric cores with similar electronic properties in the design of high-affinity CRF receptor ligands, provided the peripheral pharmacophore elements are maintained in the same three-dimensional array.
Pyrazolo[1,5-A]triazine corticotropin releasing factor antagonists
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, (2008/06/13)
The present invention describes novel pyrazolo[1,5-a]triazines of formula: wherein R3is an alkyl, alkenyl, alkynyl, or cycloalkyl group, or pharmaceutically acceptable salt forms thereof, which are useful as CRF antagonists.
Pyrazolopyrimidines as CRF antagonists
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, (2008/06/13)
The present invention relates to pyrazolopyrimidines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification wherein all of the compounds are useful as CRF antagonists and are thus useful in the treatment of neurological disorders as well as a multitude of other CRF associated diseases or conditions.
Pyrazolotriazines as CRF antagonists
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, (2008/06/13)
The present invention relates to pyrazolotriazines according to formula (I) and stereoisomers, isomers and salts thereof wherein R1-R5 are selected from certain alkyl, aryl and heteroaryl species as defined in the specification where
Metal Ion Photoinitiated Addition of Acetonitrile and Methanol to Olefins
Bruno, Joseph W.,Marks, Tobin J.,Lewis, Frederick D.
, p. 5580 - 5585 (2007/10/02)
Irradiation of norbornene and silver or thallium trifluoromethanesulfonate in acetonitrile solutions results in the efficient formation of exo-2-(cyanomethyl)bicycloheptane.Investigation of the scope of this reaction established that (a) copper(I or II) salts are not effective, (b) propionitrile and methanol give analogous norbornene-solvent adducts, and (c) acetonitrile addition is observed for several cyclic and acyclic olefins.Investigation of the mechanism of solvent addition indicates that the reaction is initiated by photoinduced electron transfer to silver(I) from coordinated norbornene.Reaction of the resulting norbonene cation radical with acetonitrile yields norbornyl cation and cyanomethyl radical.Free-radical chain addition of the cyanomethyl radical to norbornene then leads to product formation.In ethereal solvents, metal ion catalyzed photodimerization of norbornene has previously been reported for copper(I) salts.This reaction can also be effected by copper(II) and silver(I) salts, but not by Tl(I) salts.
