- ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The inventi
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- Design, synthesis, and structure-activity relationship of a novel series of GluN2C-selective potentiators
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NMDA receptors are tetrameric complexes composed of GluN1 and GluN2A-D subunits that mediate a slow Ca2+-permeable component of excitatory synaptic transmission. NMDA receptors have been implicated in a wide range of neurological diseases and thus represent an important therapeutic target. We herein describe a novel series of pyrrolidinones that selectively potentiate only NMDA receptors that contain the GluN2C subunit. The most active analogues tested were over 100-fold selective for recombinant GluN2C-containing receptors over GluN2A/B/D-containing NMDA receptors as well as AMPA and kainate receptors. This series represents the first class of allosteric potentiators that are selective for diheteromeric GluN2C-containing NMDA receptors.
- Zimmerman, Sommer S.,Khatri, Alpa,Garnier-Amblard, Ethel C.,Mullasseril, Praseeda,Kurtkaya, Natalie L.,Gyoneva, Stefka,Hansen, Kasper B.,Traynelis, Stephen F.,Liotta, Dennis C.
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p. 2334 - 2356
(2014/04/17)
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- NMDA RECEPTOR MODULATORS AND USES RELATED THERETO
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This disclosure relates to NMDA modulators and used related thereto such as for treatment of central nervous system disorders. In certain embodiments, compounds disclosed herein are NR2C subunit-selective NMDA potentiators. In certain embodiments, the disclosure contemplates compounds and pharmaceutical compositions. In certain embodiments, the disclosure contemplates compounds disclosed herein as prodrugs, optionally substituted with one or more substituents, derivatives, or salts thereof. In certain embodiments, the disclosure relates to methods of treating or preventing nervous system disorders comprising administering an effective amount of a composition comprising compound disclosed herein to a subject in need thereof.
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Page/Page column 26; 27; 32
(2014/03/21)
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- NOVEL DIHYDROPYRIDIN-2(1H)-ONE COMPOUNDS AS S-NITROSOGLUTATHIONE REDUCTASE INHIBITORS AND NEUROKININ-3 RECEPTOR ANTAGONISTS
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The present invention is directed to novel dihydropyridin-2(1H)-one compounds useful as S-nitrosoglutathione reductase (GSNOR) inhibitors and/or Neurokinin-3 (NK3) receptor antagonists, pharmaceutical compositions comprising such compounds, and methods of making and using the same.
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- Compounds and Compositions as Tpo Mimetics
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The invention provides a novel class of compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with abnormal or deregulated TPO activity, particularly disea
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Page/Page column 7-8
(2008/12/07)
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- Oxidant scavengers
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The present invention relates, in general, to a method of modulating physiological and pathological processes and, in particular, to a method of modulating intra- and extracellular levels of oxidants and thereby processes in which such oxidants are a participant. The invention also relates to compounds and compositions suitable for use in such methods.
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- Thermolysis and CoII-tetraphenylporphyrin-catalysed decomposition of substituted cycloheptatriene endoperoxides: A new synthetic approach to substituted dihydrooxepines
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Photooxygenation of the carbonyl group-substituted cycloheptatrienes 14-17 affords the corresponding [2+4] cycloaddition products derived from cycloheptatriene and its valence isomer norcaradiene as well as rearranged aromatic compounds. Thermolysis of the cycloheptatriene endoperoxides 19, 22, 23, 26, 27 and 31 at 174°C gives the corresponding bis-epoxides, no rearranged products being observed. However, treatment of 19, 26 and 31 with cobalt tetraphenylporphyrin provides the ring-opened products 47, 49 and 51 which are easily converted into the substituted 4,5-dihydrooxepine derivatives 48, 50 and 52. The outcome of Co-TPP-catalysed rearrangement is discussed in terms of different conformers.
- Senguel, M. Emin,Balci, Metin
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p. 2071 - 2077
(2007/10/03)
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- Selective and one-pot formation of phenols by anodic oxidation
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Direct monohydroxylation of benzene and substituted benzenes was successfully performed by anodic oxidation to form the corresponding phenol derivatives in good yields. The anodic oxidation was generally carried out in a mixed solvent of trifluoroacetic acid and dichloromethane containing triethylamine using a divided cell equipped with a platinum plate as the anode, a carbon rod as the cathode. Benzene derivatives having electron withdrawing groups were suitable for the present electrochemical oxidation. It was clarified that aryltrifluoroacetates were formed as the initial products from the reaction of the radical cations, generated by one electron transfer from the substrates, with trifluoroacetic acid, followed by hydrolysis during work-up to give the corresponding phenols.
- Fujimoto, Kazuo,Tokuda, Yuichiro,Maekawa, Hirofumi,Matsubara, Yoshiharu,Mizuno, Takumi,Nishiguchi, Ikuzo
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p. 3889 - 3896
(2007/10/03)
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