- 3-SUBSTITUTED 1,2,3-TRIAZIN-4-ONE'S AND 3-SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
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This invention relates to compounds, pharmaceutical compositions and methods for use in the prevention and treatment of cerebral insufficiency, including enhancement of receptor functioning in synapses in brain networks responsible for basic and higher order behaviors. These brain networks, which are involved in regulation of breathing, and cognitive abilities related to memory impairment, such as is observed in a variety of dementias, in imbalances in neuronal activity between different brain regions, as is suggested in disorders such as Parkinson''s disease, schizophrenia, respiratory depression, sleep apneas, attention deficit hyperactivity disorder and affective or mood disorders, and in disorders wherein a deficiency in neurotrophic factors is implicated, as well as in disorders of respiration such as overdose of an alcohol, an opiate, an opioid, a barbiturate, an anesthetic, or a nerve toxin, or where the respiratory depression results form a medical condition such as central sleep apnea, stroke- induced central sleep apnea, obstructive sleep apnea, congenital hypoventilation syndrome, obesity hypoventilation syndrome, sudden infant death syndrome, Rett syndrome, spinal cord injury, traumatic brain injury, Cheney-Stokes respiration, Ondines curse, Prader-Willi''s syndrome and drowning. In a particular aspect, the invention relates to compounds useful for treatment of such conditions, and methods of using these compounds for such treatment.
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Page/Page column 67
(2009/04/25)
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- Cycloaddition of Isocyanides with 1-Aryl-2-nitro-1-propenes, Methyl 2-Nitro-3-arylpropenoates, and Methyl 2-Nitro-2,4-pentadienoates. Synthesis of 1-Hydroxyindoles and 1-Hydroxypyrroles
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The cycloadditions of isocyanides with various aryl nitroalkenes have been investigated.When the aryl groups were XC6H4, naphthyl, and 2-pyridinyl, the reactions gave the 1-hydroxyindoles, 1-hydroxybenzoindoles, and 1-hydroxy-7-azaindole.When the ar
- Foucaud, Andre,Razorilalana-Rabearivony, Claudia,Loukakou, Emile,Person, Herve
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p. 3639 - 3644
(2007/10/02)
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- Heterocyclic analogs of amphetamine: Thioureas, dithiocarbamates, and negatively substituted amides
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A series of heterocyclic analogs of amphetamine was synthesized. The heterocycles employed included the 2-furyl, 2-thienyl, 3-methyl-2 thienyl, 3-pyridyl, and 6-methyl-2-pyridyl rings. The aliphatic amine group was converted to the N-methylthiourea, dithiocarbamate, methanesulfonyl, trifluoromethanesulfonyl, and trifluoroacetyl functions since similar conversions of the β-phenethylamine structure had shown blood pressure-lowering effects and some loss of behavioral effects. P-Chlorophenyl and 1-naphthyl analogs were also converted to these derivatives. Behavioral and other biological effects, including antiarthritic, passive cutaneous anaphylactic, and antimicrobial, were observed. The 3-methyl-2-thienyl analog of amphetamine significantly increased papillary muscle contractile force without producing arrhythmias.
- Foye,Tovivich
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p. 591 - 595
(2007/10/04)
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