Abstract: The present invention is directed to novel pyridazinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition/cognitive disorders.

Abstract: The present invention is directed to compounds having histamine H3 antagonist activity, as well as methods of their use and preparation.

Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.

Abstract: The present invention is directed to novel pyridizinone derivatives that mediate enzymatic activity. In particular, the compounds may be effective in the treatment of diseases or disease states related to the activity of the histamine H3 receptor, including, for example, neurodegenerative disorders, sleep/wake disorders, attention deficit hyperactivity disorder and cognition.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, amino, perhalomethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio or C.sub.1-6 -alkylamino;A is methyl, halomethyl, cyanomethyl, aminomethyl, vinyl, methylthiomethyl or methoxymethyl;R.sup.1 is selected from optionally substituted N-bonded heterocyclics.The compounds have been found useful for treating central nervous system ailments.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, trifluoromethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, C.sub.1-6 -alkylamino or C.sub.1-6 -dialkylamino;R.sup.1 and R.sup.4 are H or straight or branched C.sub.1-6 -alkyl or trifluoromethyl or R.sup.1 and R.sup.4 together form a cycloalkyl ring;Y is O, S, SO.sub.2, NH or N-alkyl;R.sup.5 is selected from optionally substituted heterocycles.R.sup.6 and R.sup.7 are hydrogen, benzoyl or C.sub.1-6 -alkanoyl.The compounds have been found useful for treating central nervous system and cardiovascular ailments.

Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein X is halogen, perhalomethyl, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio, or C.sub.1-6 -alkylamino; andR.sup.1 is selected from N-bonded heterocycles.The compound with the greatest ability to discriminate between the A1 and A2 adenosine receptors is 2-chloro-N-[4-phenoxy-1-piperidinyl]adenosine. These adenosine derivatives are useful as anti-convulsants.

Abstract: Adenosine compounds having the following structure ##STR1## wherein X is halogen, perhalomethyl, acetamido, cyano, C.sub.1-6 -alkoxy, C.sub.1-6 -alkylthio or C.sub.1-6 -alkylamino; andR.sup.1 is --NR.sup.2 R.sup.3 or YR.sup.4, wherein Y is oxygen or sulfur;R.sup.2 is phenyl, C.sub.1-6 -alkyl or substituted C.sub.1-6 -alkyl; andR.sup.4 is naphthyl, partly saturated naphthyl; optionally phenyl or phenoxy substituted C.sub.1-6 -alkyl wherein the phenyl and phenoxy substituents are also optionally substituted, or optionally phenyl or phenoxy substituted C.sub.3-8 -cycloalkyl and their pharmaceutically acceptable salts are useful in the treatment of myocardial and cerebral ischemias.

Abstract: The invention relates to therapeutically active azaheterocyclic compounds and to pharmaceutical compositions comprising the compounds. The novel compounds are useful in treating a central nervous system ailment related to the GABA uptake.

Abstract: Novel O-alkylated oximes of the general formula I ##STR1## or ##STR2## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.

Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA re-uptake from the synaptic cleft.

Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.

Abstract: Novel O-alkylated oximes of the general formula I ##STR1## wherein R.sup.1 and R.sup.2 are optionally substituted aromatic or heteroaromatic rings, R.sup.3 is hydrogen or lower alkyl, R.sup.4 is a nitrogen containing, substituted ring or an amino group carrying a substituted ring, and n and m independently are 0, 1 or 2, are potent inhibitors of GABA reuptake from the synaptic cleft.