- 3-SUBSTITUTED 1,2,3-TRIAZIN-4-ONE'S AND 3-SUBSTITUTED 1,3-PYRIMIDINONE'S FOR ENHANCING GLUTAMATERGIC SYNAPTIC RESPONSES
-
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.
- -
-
Page/Page column 48-50
(2009/04/25)
-
- Chirospecific synthesis of amino acids, amino aldehydes and amino alcohols from D-glucosamine hydrochloride. A multigram synthesis of N-BOC-L-serinal
-
N-tert.-butyloxycarbonyl-L-serinal 4 was readily prepared from D-glucosamine hydrochloride 1 in three steps. The versatile synthetic intermediate 4 is chemically and configurationally stable for prolonged time and reacts with various stabilized phosphorus
- Giannis,Henk
-
p. 1253 - 1256
(2007/10/02)
-
- Intramolecular Pictet-Spengler Reaction of N-Alkoxytryptamines. 3. Stereoselective Synthesis of (-)-Debromoeudistomin L and (-)-O-Methyldebromoeudistomin E and Their Stereoisomers
-
The N-hydroxytrypamines 10 and 11 were converted into the N-alkoxy derivatives 32-34 (overall yield 57-72percent) by successive protection with chloroformate providing 27 and 28, reaction with functionalized chloromethyl sulfides, and deprotection with a "naked" fluoride.Intramolecular cyclization succeeded with 33 and 34 by reduction of the methyl ester with DIBAL and treatment with TFA to give diastereomeric pairs with a slight selectivity for the trans isomer (53-81percent, cis/trans ca. 35/65).Removal of the BOC group gave debromoeudistomin L ((-)-1e), its three stereoisomers (42a,b and (+)-1e), O-methyldebromoeudistomin E ((-)-1f), and its stereomer 43.
- Hermkens, Pedro H. H.,Maarseveen, Jan H. v.,Ottenheijm, Harry C. J.,Kruse, Chris G.,Scheeren, Hans W.
-
p. 3998 - 4006
(2007/10/02)
-
- SYNTHESIS OF THE SERINE EQUIVALENT, (2R) AND (2S)-AMINO-3-BUTENOL DERIVATIVES. SYNTHETIC APPROACHES TO THE METAL CHELATING POLY-AMINO ACID, "ASPERGILLOMARASMINE A"
-
Chiral synthons, equivalent to the C3 amino acid serine, were synthesized in both (2R) and (2S) form from D or L-methionine respectively; Utilization of this synthon in the construction of metal chelating poly-amino acid aspergillomarasmine A skeleton is presented.
- Ohfune, Yasufumi,Kurokawa, Natsuko
-
p. 1071 - 1074
(2007/10/02)
-