Abstract: Novel 12-halogenated forskolin derivatives, intermediates and processes for the preparation thereof, and methods for reducing intraocular pressure utilizing compounds or compositions thereof are disclosed.
Abstract: There are disclosed compounds having the formula ##STR1## wherein n is 1-4; R.sub.1 is hydrogen, alkyl, aryl, arylloweralkyl, naphthyl, furyl, thienyl, pyridinyl or pyrrolyl; X is hydrogen, loweralkyl, cycloalkyl, loweralkoxy, halogen, hydroxy nitro, trifluoromethyl, formyl, loweralkylcarbonyl, arylcarbonyl, --SH, loweralkylthio, --NHCOR.sub.2 or --NR.sub.3 R.sub.4 where R.sub.2 is hydrogen or loweralkyl, and R.sub.3 and R.sub.4 are independently hydrogen, loweralkyl or cycloalkyl; stereo, optical and geometrical isomers thereof, and pharmaceutically acceptable acid addition salts thereof, which are useful for enhancing memory and pharmaceutical compositions comprising an effective memory enhancing amount of such a compound.
Abstract: This invention relates to 1-(pyridinylamino)-2-pyrrolidinones of the formula ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are independently hydrogen, loweralkyl, aryl, arylloweralkyl or heteroarylloweralkyl selected from the group consisting of pyridinylmethyl, pyridinylethyl, thienylmethyl, thienylethyl or R.sub.2 and R.sub.3 together form a cycloalkane ring of 4 to 6 carbons or a spiro-fused aryl or heteroaryl substituted cycloalkane; X is hydrogen, halogen, hydroxy, loweralkyl, loweralkoxy, nitro, amino or trifluoromethyl; m is an integer of 1 to 3, the pharmaceutically acceptable acid addition salts thereof and where appropriate the geometrical, optical and stereoisomers and racemic mixtures thereof. The compounds of this invention display utility as analgesics, for enhancing memory and for the treatment of Alzheimer's disease.
Abstract: 4-Pentafluorophenoxypiperidines and methods for alleviating pain and treating depression, convulsions, and hypertension utilizing compounds or compositions thereof are disclosed.
Abstract: This invention relates to 1,4 dihydropyridines having the following formula ##STR1## wherein R is loweralkyl or Arloweralkyl; R.sub.1, R.sub.2 and R.sub.3 may be the same or different and are hydrogen, loweralkyl or halogen; X is hydrogen, NH.sub.2, ##STR2## and R.sub.4 is hydrogen or loweralkyl. The compounds of this invention display utility in the treatment of Alzheimer's disease and related cognitive disorders characterized by centrally deficient cholinergic function.
Abstract: This invention relates to 6,11-dihydro-11-oxo-dibenz[b, e]oxepin derivatives of the formula ##STR1## where Y is hydrogen, alkyl, alkoxy, halogen and trifluoromethyl, n is 0, 1, 2 or 3; R.sub.9 is hydrogen and alkyl; R is ##STR2## where Hal is a halogen; ##STR3## where R.sub.10 is hydrogen, alkyl and benzyl of the formula ##STR4## where Z is hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, nitro, and amino; where n is 0, 1, 2 or 3; p is 1 or 2; q is 0, 1 or 2; R.sub.1 to R.sub.7 are the same or different and are hydrogen and alkyl; and R.sub.8 is hydrogen, alkyl and phenyl; and R.sub.9 is hydrogen and alkyl, and where appropriate pharmaceutically acceptable acid or base addition salts thereof.
Abstract: This invention relates to 4-aryloxy-1,2,3,4-tetrahydroisoquinolines of the formula ##STR1## where Y is hydrogen and alkoxy; X is hydrogen, cyano, benzoyl, trifluoromethyl, phenyl, halogen, alkyl alkoxy and nitro; R is hydrogen and alkyl; R.sub.1 is hydrogen, alkyl, aralkyl, ##STR2## and CO.sub.2 R.sub.4 where R.sub.1 is aryl and alkyl; R.sub.2 and R.sub.3 are the same or differnt and are hydrogen and alkyl or R.sub.2 and R.sub.3 are fused together to form a pyrrolidino or a piperidino ring substituent; and m is an integer of 1 or 2; n is an integer of 2 or 3; and a pharmaceutically acceptable acid addition salt thereof.
Abstract: This invention relates to substituted 8-phenylisoxazolo[4,3-e][1,4]diazepin-5-ones of the formula ##STR1## wherein R is lower alkyl; R.sub.1 is hydrogen, amino alkyl, propargyl and lower alkyl; X is oxygen and sulfur; and Y is halogen, trifluoromethyl, lower alkyl, lower alkoxy and hydrogen. The compounds of this invention display useful anxiolytic and anticonvulsant activities.
Abstract: Spiro[2H-1,4-benzodioxepin-3(5H)4'-piperidine and -3'-pyrrolidine] compounds of the formula ##STR1## where the substituents are as defined herein, are useful in the treatment of hypertension in mammals. Such compounds, their use as antihypertensive agents, pharmaceutical compositions containing the compounds, intermediates and processes for preparing the compounds are provided.
Abstract: Spiro[2H-1,4-benzodioxepin-3(5H)4'-piperidine and -3-pyrrolidine] compounds of the formula ##STR1## where the substituents are as defined herein, are useful in the treatment of hypertension in mammals. Such compounds, their use as antihypertensive agents, pharmaceutical compositions containing the compounds, intermediates and processes for preparing the compounds are provided.
Abstract: There are described spiro[indolo[1,7-ab][1,5]benzodiazepine-2,4'-piperidines]of the formula ##STR1## wherein p is 1 or 0, R.sub.1 is hydrogen or methyl and R is hydrogen or --CO(CH.sub.2).sub.n NR.sub.2 R.sub.3, R.sub.2 and R.sub.3 being each hydrogen or methyl but at least one of the two being methyl, and n being 1 or 2, which are useful as analgesic agents; intermediate compounds therefor; and methods for synthesizing the foregoing compounds.
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Abstract: There are described antihypertensive spiro[benzofuran-azalkanes] of the formula ##STR1## where X is hydrogen or halogen (F, Cl, Br, or I); m and n are each 0, 1 or 2 but m plus n is 1 or 2; and R is ##STR2## k being 2 or 3 and Y being hydrogen or halogen, which are useful as antihypertensive agents and methods for synthesizing the same.
Abstract: A neuroleptic agent is disclosed. The agent is 3-{3-[4-(4-fluorobenzoyl)piperidyl]propyl}-2-methylindole or an acid addition salt thereof prepared from a pharmaceutically acceptable acid.
Abstract: Novel 4-aryloxy- and 4-arylthio-3-phenylpiperidines and related compounds, physiologically acceptable salts thereof and intermediates therefor possessing analgesic, antidepressant properties, and a process for the preparation of such compounds, derivatives and intermediates are described.
Abstract: Novel 4-phenyl-1,3-benzodiazepines, novel intermediates thereof, and methods of preparing same are described. These benzodiazepines are useful as antidepressants, analgetics and anticonvulsants.
Abstract: 1-[2-(4,5-dihydro-4,4-dialkyl-2-oxazolyl)phenyl]-4-(dialkylamino)cyclohexan ol as an intermedate for Spiro cyclohexane-1,1'(3'H)-isobenzofuran)s, which in turn are useful as antidepressants, tranquilizers, analgesics, and anticonvulsants.