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This update includes basic patents and patent applications published between July 1992 and June 1994 which may have utility for the treatment of three major groups of sleep disorders, namely, simple insomnia, sleep disorders secondary to anxiety or mood disorders, and sleep disorders stemming from circadian rhythm disruptions. Accordingly, the patents are grouped by their presumed mode of action as non-psychotropic agents, psychotropic agents, and chronobtotic agents. For the purposes of this review, only those patents and applications which specifically describe or claim sleep enhancing or sedative-hypnotic properties are included. Coverage is limited to novel small-molecule, non-peptidergic agents.

Zirconocene( iso -butyl) chloride, 1 , which can be generated in situ from commercially available, inexpensive, and air-stable zirconocene dichloride, can function as a zirconocene(methyl) chloride equivalent.

Zirconocene( iso -butyl) chloride, 1 , which can be generated in situ from commercially available, inexpensive, and air-stable zirconocene dichloride, can function as a zirconocene(methyl) chloride equivalent.

A series of fluoren-9-yl ethyl amides ( 2 ) were synthesized and evaluated for human melatonin MT 1 and MT 2 receptor binding. N -[2-(2,7-dimethoxyfluoren-9-yl)ethyl]propanamide ( 2b ) was selected and evaluated in functional assays measuring intrinsic activity at the human MT 1 and MT 2 receptors and demonstrated full agonism at both receptors. The chronobiotic properties of 2b were demonstrated in both acute and chronic rat models where 2b produced an acute phase advance of 32 min at 1 mg/kg and chronically entrained free-running rats with a mean effective dose of 0.23 mg/kg. Compound 2b is significantly less efficacious than melatonin in constricting human coronary artery.

Schwartz's reagent product: Schwartz's Reagent Keywords: carbometallation; reduction, miscellaneous; assay methods, for Schwartz's Reagent; dichloromethane (methylene chloride); tetrahydrofuran; chlorobis(η5-cyclopentadienyl)hydridozirconium = Schwartz's Reagent; Schwartz's Reagent, in presence of methylene chloride; filtration, with cannula fitted with glass fiber filter; flasks, schlenk filtration apparatus

Obtention de methoxy-, iodo- et (methoxyiodo) alcanophenones, de benzisothiazoles-1,2, et de bicyclo [4.2.0] octatrienes-1,3,5

A series of novel azazirconacyclopentenes have been prepared by the thermolysis of diphenylzirconocene in the presence of one equivalent of a wide variety of nitriles. An X-ray crystal structure shows these metallacycles to be dimeric in the solid state.

A series of novel azazirconacyclopentenes have been prepared by the thermolysis of diphenylzirconocene in the presence of one equivalent of a wide variety of nitriles. An X-ray crystal structure shows these metallacycles to be dimeric in the solid state.

A convenient method for the preparation of 65–85 g quantities of Cp2Zr(H)Cl, Schwartz's reagent has been developed. The reagent prepared by this method is of high purity and has several advantages over the reagent prepared by previously reported methods.

Syntheses a partir du complexe chloro de Zr-methyl zirconocene via la reaction de CO avec des alkyl-3 aryl-5 trimethylsilyl-1 di-η 5 -cyclopentadienyl-2,2 aza-1zircona-2cyclopentenes-3