207279-37-6Relevant articles and documents
Macroporous chiral ruthenium porphyrin polymers: A new solid-phase material used as a device for catalytic asymmetric carbene transfer
Ferrand, Yann,Le Maux, Paul,Simonneaux, Gerard
, p. 3829 - 3836 (2005)
A chiral ruthenium porphyrin complex, functionalized with four vinyl groups, has been polymerized with styrene, divinylbenzene (or ethylene glycol dimethacrylate) to obtain supported ruthenium complexes. The asymmetric addition of ethyl diazoacetate (or d
Discovery of MK-0952, a selective PDE4 inhibitor for the treatment of long-term memory loss and mild cognitive impairment
Gallant, Michel,Aspiotis, Renee,Day, Stephen,Dias, Rebecca,Dubé, Daniel,Dubé, Laurence,Friesen, Richard W.,Girard, Mario,Guay, Daniel,Hamel, Pierre,Huang, Zheng,Lacombe, Patrick,Laliberté, Sebastien,Lévesque, Jean-Franois,Liu, Susana,MacDonald, Dwight,Mancini, Joseph,Nicholson, Donald W.,Styhler, Angela,Townson, Karen,Waters, Kerry,Young, Robert N.,Girard, Yves
scheme or table, p. 6387 - 6393 (2010/12/18)
The structure-activity relationship of a novel series of 8-biarylnaphthyridinones acting as type 4 phosphodiesterase (PDE4) inhibitors for the treatment of long-term memory loss and mild cognitive impairment is described herein. The manuscript describes a new paradigm for the development of PDE4 inhibitor targeting CNS indications. This effort led to the discovery of the clinical candidate MK-0952, an intrinsically potent inhibitor (IC 50 = 0.6 nM) displaying limited whole blood activity (IC50 = 555 nM). Supporting in vivo results in two preclinical efficacy tests and one test assessing adverse effects are also reported. The comparative profiles of MK-0952 and two other Merck compounds are described to validate the proposed hypothesis.
COMPOUNDS WHICH POTENTIATE GLUTAMATE RECEPTOR AND USES THEREOF IN MEDICINE
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Page/Page column 42, (2008/06/13)
This invention relates to potentiation of the glutamate receptor by novel compounds of formula (I): The invention also relates to the use of the derivatives in treating diseases and conditions mediated by potentiation of the glutamate receptor, compositio