Abstract: There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.

Abstract: Novel derivatives of benzodioxa alkylene ethers are provided which are useful as melatonergic agents.

Abstract: The present invention provides novel amino acid derivatives having the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: The present invention provides novel 4-aryl-3-aminoquinolin-2-one derivatives having the general formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein, or a non-toxic pharmaceutically acceptable salt thereof which are modulators of the large conductance calcium-activated K.sup.+ channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

Abstract: The present invention provides novel benzoate derivatives having the general formula ##STR1## wherein R is as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: Novel polycyclic ethyl alkylamides of formula I are active as melatonergic agents. ##STR1## wherein Z=CH (when a double bond is present) or (CH.sub.2).sub.n, wherein n is 1-4;X=O, CH.sub.2, or CH (when a double bond is present);R=C.sub.1-6 alkyl, C.sub.3-6 cycloalkyl, or C.sub.1-3 haloalkyl, C.sub.2-6 alkenyl, C.sub.2-4 alkoxyalkyl, C.sub.1-4 trifluoromethylalkyl, C.sub.1-6 aminoalkyl; andY=H, C.sub.1-6 alkoxy or halogen.

Abstract: The present invention provides novel phosphate derivatives having the general formula wherein A, R.sup.1 and R.sup.2 are as defined herein, or a nontoxic pharmaceutically acceptable salt or solvate thereof and are useful in the treatment of disorders which are responsive to the opening of potassium channels.

Abstract: There is provided novel substituted 4-aryl-3-hydroxyquinolin-2-one derivatives of the formula ##STR1## wherein R is hydrogen or methyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, bromo, chloro or trifluoromethyl, and when R.sup.1, R.sup.3 and R.sup.4 are hydrogen, R.sup.2 is nitro;R.sup.5 is hydrogen or methyl; andR.sup.6 is bromo or chloro;or a nontoxic pharmaceutically acceptable salt thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

Abstract: The present invention is concerned with a chemical acetylation process for the preparation of 3'-acetylated cephalosporin from desacetyl-cephalosporin. The novel process is carried out with an acetyl donor and an activator or catalyst.

Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.

Abstract: There is provided novel substituted 4-aryl-3-hydroxyquinolin-2-one derivatives of the formula ##STR1## wherein R is hydrogen or methyl;R.sup.1, R.sup.2, R.sup.3 and R.sup.4 each are independently hydrogen, bromo, chloro or trifluoromethyl, and when R.sup.1, R.sup.3 and R.sup.4 are hydrogen, R.sup.2 is nitro;R.sup.5 is hydrogen or methyl; andR.sup.6 is bromo or chloro;or a nontoxic pharmaceutically acceptable salt thereof, which are openers of the large-conductance calcium-activated potassium channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.

Abstract: The present invention provides a series of non-peptidergic antagonists of NPY comprising piperidine derivatives of 4-phenyl-1,4-dihydropyrimidinones of the Formula I ##STR1## wherein R, R.sup.1 and R.sup.2 are defined herein. As antagonists of NPY-induced feeding behavior, these compounds are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.

Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.

Abstract: Novel compounds of Formula 1 are useful to treat disorders responsive to openers of the large conductance calcium-activated potassium channels: ##STR1## wherein "Het" is one of a select group of heterocyclic moieties; Z is independently for each occurrence selected from O or S; R.sup.a, R.sup.b and R.sup.c each are independently selected from hydrogen, halogen, OH, CF.sub.3, ##STR2## provided R.sup.c is not hydrogen; and when R.sup.a and R.sup.b are hydrogen, R.sup.c may be a heterocyclic moiety selected from the group consisting of imidazol-1-yl, morpholinomethyl, N-methylimidazol- 2-yl, and pyridinyl; R.sup.d and R.sup.e each are independently selected from hydrogen, halogen, CF.sub.3, NO.sub.2 or imidazol-1-yl; m, n and p each are independently selected from an integer of O or 1; and R.sup.f and R.sup.g each are independently hydrogen; C.sub.1-4 alkyl; or R.sup.f and R.sup.

Abstract: Novel derivatives of benzofuran and dihydrobenzofuran are provided which are useful as melatonergic agents.

Abstract: There is provided novel biphenylamido derivatives of the formula ##STR1## wherein Z is ##STR2## and Y is H or Z is H and Y is ##STR3## n is 0 or 1; R is C.sub.1-6 alkyl;R.sup.1 is C.sub.1-3 alkyl, C.sub.3-6 cycloalkyl, C.sub.1-4 alkoxymethyl, or NHR.sup.2 ; andR.sup.2 is C.sub.1-3 alkyl or cyclopropylwhich are melatonergic agents and are useful in the treatment of circadian rhythm-related disorders and other conditions affected by melatonin activity.

Abstract: The present invention relates to novel intermediates of the formula ##STR1## wherein the wavy bond () represents the racemate, the (R)-enantiomer or the (S)-enantiomer; and R is hydrogen, a carboxyl-protecting group or a cation of an addition salt; or solvate thereof; and to the use thereof in a process for the preparation of certain 3-fluoro oxindole derivatives.

Abstract: Certain indanyl piperazines are useful as melatonergic agents and can treat various CNS disorders. They are use useful in treating sleep disorders and other conditions related to circadian rhythms.

Abstract: Certain N-acyl 2-aryl cyclopropylmethylamine derivatives are useful as melatonergic agents.

Abstract: There is provided a novel series of malonate derivatives of glycolipid compounds of the formula ##STR1## wherein R is an acyl residue of a fatty acid:R.sup.1 is --(CH.dbd.CH).sub.m --(CH.sub.2).sub.n --CH.sub.3 ;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 each are independently hydrogen, unsubstituted or substituted (lower)alkanoyl, arylalkyl or arylcarbonyl wherein said substituent is selected from the group consisting of halogen, C.sub.1-4 alkyl, trifluoromethyl, hydroxy and C.sub.1-4 alkoxy provided that one of R.sup.2, R.sup.3, R.sup.4 and R.sup.6 substituents is --(CH.sub.2).sub.p --CH(CO.sub.2 R.sup.7).sub.2 ;m is an integer of 0 or 1;n is an integer of from 5 to 14 inclusive;p is an integer of from 2 to 6 inclusive; andR.sup.