Fluorescent Human EP3 Receptor Antagonists

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Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent,Selective, and Orally Active EP3 Receptor Antagonists

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Novel 3-Aryl Indoles as Progesterone Receptor Antagonists for Uterine Fibroids

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Patent Evaluation: Novel 3-Indolyl Thioacetate Derivatives as NMDA Receptor Antagonists

Summary

Novelty: New 3-indolylthioacetate derivatives are disclosed as NMDA antagonists. The compounds are claimed to be useful in treating convulsions, ischaemia, hypoxic or hypoglycaemic conditions and neurodegenerative diseases. They also have an anxiolytic effect.

Biology: Anticonvulsant properties are assessed in vivo by inhibition of quinolinic acid-induced seizures in mice, where the control group has a statistically higher seizure rate than mice administered intracerebroventricularly with the test compound. Anti-epileptic activity is assessed by inhibition of audiogenic convulsion (one hundred and ten decibels for thirty seconds) in mice with similiar results. The anxiolytic effect is measured by blocking the ultrasonic vocalization in rat pups in vivo when removed from the litter, again the two groups show statistical differences.

Chemistry: Synthesis, by conventional methods, of the starting material, the 3,5-dichlorophenylhydrazone of ethyl pyruvate, and of eleven compounds is presented. Characterization is by Mp, IR and NMR. The preferred compound is 2-carboxyethyl-4,6-dichloroindole. A large number of compounds are claimed.     

Patent Evaluation: Novel Quinoline Leukotriene Receptor Antagonists

Summary

Novelty: Unsaturated hydroxyalkylquinoline acids, which are said to be leukotriene antagonists and inhibitors of leukotriene biosynthesis, are disclosed. Quinoline acids may be useful for treating conditions such as angina, cerebral spasm and hepatitis.

Biology: Leukotriene antagonism was evaluated in LTD₄ receptor binding studies undertaken on g.p. lung membranes (in vitro) and in vivo in guinea pigs. A PMN leukocyte LTB₄ assay was also performed. In vivo leukotriene antagonism and leukotriene biosynthesis inhibition were assessed using asthmatic rats and pulmonary mechanics tests. However, no data are provided.

Chemistry: The syntheses of the compounds are described in fifteen reaction schemes. Preparatory details are included for thirty-nine compounds. A further one hundred and sixty-seven examples are given. All compounds were prepared by conventional methods.

Structure: