Abstract: A class of imidazo?1,2-a!pyridinylalkyl compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## wherein each of R.sup.22, R.sup.23 and R.sup.24 is independently selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.

Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein R.sup.9 is selected from hydrido, methyl, ethyl, n-propyl, isopropyl, n-butyl, isobutyl, sec-butyl, tert-butyl, cyclopropyl, cyclobutyl, cyclopentyl, cyclohexyl and cycloheptyl; wherein each of Y.sub.m and Y.sub.

Abstract: A class of imidazo[1,2-a]pyridinylalkyl phosphonic acid compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a compound of this class alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of the formula: ##STR1## and the carboxylic and phosphonic alkyl esters and salts thereof; wherein the substituents are defined herein.

Abstract: The present invention relates to new compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof and the enantiomers thereof, wherein R.sup.1 is H, lower alkyl, alkenyl, aralkyl, or C(O)R.sup.2 wherein R.sup.2 is lower alkyl, alkenyl, alkoxy, or aralkyl; n is an integer of from 2-4; m is an integer of from 0-4; A is S(O).sub.x wherein x is an integer of from 0-2; and Ar is phenyl or thienyl. These compounds are useful as analgesics.

Abstract: This invention relates to [(1H-benzimidazol-2-ylsulfinyl)methyl]-2-pyridinamines that are useful in the treatment and prevention of ulcers.

Abstract: This invention relates to 2-[(imidazo[1,2-a]pyridin-3-ylmethyl)sulfinyl]-1H-benzimidazoles that are useful in the treatment and prevention of ulcers.

Abstract: This invention relates to 2-[(imidazo[1,2-a]pyridinylmethyl)-sulfinyl]-1H-benzimidazoles that are useful in the treatment and prevention of ulcers.

Abstract: This invention relates to 5-(substituted phenyl)-5-[(substituted amino)alkyl]-1,3-diazabicyclo[4.4.0]decan-4-ones and 5-(substituted phenyl)-5-[(substituted amino)-alkyl]-1,3-diazabicyclo[4.4.0]dec-2-en-4-ones that are useful as antiarrhythmic agents.

Abstract: Compounds of formula I and salts thereof which are orally pharmacologically active as inhibitors of gastric secretion are disclosed.

Abstract: N-aralkenyl-N'-cyano-N"-(heterocyclylthioalkyl)-guanidines and salts thereof which are pharmacologically active as inhibitors of gastric secretion and their preparation from isothioureas are disclosed.

Abstract: This invention encompasses novel 1-(3,3-diaryl-3-oxadiazolalkyl)-4-phenyl-4-piperidinomethanols and related compounds. These compounds are useful anti-diarrheal agents which possess little or no analgesic activity.

Abstract: The present invention encompasses compounds of the formula ##STR1## AND THE PHARMACEUTICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF WHEREIN R represents hydrogen, alkanoyl having 1 to 7 carbon atoms, or lower alkyl having 1 to 7 carbon atoms; X and Y represent alkylene having 1 to 3 carbon atoms and Ar, Ar', and Ar" represent phenyl, halosubstituted phenyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1 to 4 carbon atoms; and Ar'" represents phenyl, pyridyl, lower alkyl substituted phenyl wherein the lower alkyl contains 1 to 4 carbon atoms or halosubstituted phenyl. Compounds of the present invention are prepared by reaction of triarylalkanoyl halide with appropriately substituted piperidine followed by subsequent reduction of the resulting amide. Compounds of the present invention are potent antidiarrheal compounds with unexpected separation of antidiarrheal and central nervous system properties.

Abstract: The present invention, comprehends a method for treating diarrhea comprising administering to an animal in need of anti-diarrheal treatment an effective anti-diarrheal amount of a compound of the formula ##STR1## and acid addition salts thereof wherein Y is alkylene containing 1-4 carbon atoms; R.sub.2 and R.sub.3 together with N is a heterocyclic ring system comprising azamonocyclic ring of the formula ##STR2## wherein Z is phenylhydroxymethylmethylene, phenylhydroxymethylene, phenylcarboxymethylene, phenylcarbalkoxymethylene or azabicycloalkyl or phenyl or hydroxyl substituted azabicycloalkyl containing 6-9 carbon atoms and containing at least 5 atoms in each ring of the azabicycloalkyl or 4-azatricyclo[4.3.1.1.sup.3,8 ]undec-4-yl; Ar.sub.1 and Ar.sub.2 are phenyl, halo-substituted phenyl, (lower alkyl) substituted phenyl, pyridyl, thienyl or furyl, and Ar.sub.

Abstract: The present invention encompasses compounds of the formula ##STR1## and pharmaceutically acceptable acid addition salts thereof wherein the Alk is straight or branched chain alkylene containing 2-4 carbon atoms; M is alkylene having 1-4 carbon atoms; Ar and Ar' are phenyl, alkyl substituted phenyl wherein the alkyl contains from 1-4 carbon atoms or halo substituted phenyl; Ar" is phenyl, alkyl substituted phenyl wherein the alkyl contains 1-4 carbon atoms, halo substituted phenyl or pyridyl; X is hydrogen, halogen, trifluoromethyl or alkyl having from 1-4 carbon atoms; R is hydrogen alkyl having from 1-7 carbon atoms or an alkanoyl having from 2-5 carbon atoms. These compounds are potent antidiarrheal agents characterized by little, if any, central nervous system activity.

Abstract: Compounds of the formula ##STR1## AND THE NON-TOXIC PHARMACOLOGICALLY ACCEPTABLE ACID ADDITION SALTS THEREOF; WHEREIN Ar, Ar' and Ar" are each phenyl, halophenyl, or alkylphenyl wherein alkyl contains from 1 to 4 carbon atoms; Ar'" is phenyl, halophenyl, alkylphenyl wherein alkyl contains from 1 to 4 carbon atoms, or pyridyl; R is hydrogen, alkyl having from 1 to 6 carbon atoms, or alkanoyl having from 1 to 6 carbon atoms; and R.sup.1 is hydrogen or alkyl having from 1 to 6 carbon atoms. These compounds are antidiarrheal agents characterized by very weak central nervous system activity.

Abstract: The present invention encompasses compounds of the formula ##STR1## wherein the Alk is straight or branched chain alkylene containing 2-4 carbon atoms; Ar and Ar' are phenyl, Alkyl substituted phenyl wherein the alkyl contains from 1-4 carbon atoms or halo substituted phenyl; Ar" is phenyl, alkyl substituted phenyl wherein the alkyl contains 1-4 carbon atoms, halo substituted phenyl or pyridyl; X is hydrogen, halogen, trifluoromethyl or alkyl having from 1-4 carbon atoms; R is hydrogen, alkyl having from 1-7 carbon atoms, alkenyl having 3-7 carbon atoms, Ar" as herein before defined, or a cation selected from the group consisting of sodium, potassium, ammonium or calcium/2. Compounds of the present invention are potent antidiarrheal agents with little, if any, central nervous system activity.

Abstract: The present invention comprehends a method for treating diarrhea comprising administering to an animal in need of anti-diarrheal treatment an effective antidiarrheal amount of a compound of the formula ##STR1## and acid addition salts thereof wherein Y is alkylene containing 1-4 carbon atoms; R.sub.2 and R.sub.3 together with N is a heterocyclic ring system comprising azamonocyclic ring of the forumula ##STR2## wherein Z is phenylhydroxymethylmethylene, phenylhydroxymethylene, phenylcarboxymethylene, phenylcarbalkoxymethylene or azabicycloalkyl or phenyl or hydroxyl substituted azabicycloalkyl containing 6-9 carbon atoms and containing at least 5 atoms in each ring of azabicycloalkyl or 4-azatricyclo[4.3.1.1.sup.3,8 ]undec-4-yl; Ar.sub.1 and Ar.sub.2 are phenyl, halo-substituted phenyl, (lower alkyl) substituted phenyl, pyridyl, thienyl or furyl, and Ar.sub.

Abstract: Preparation and the valuable antispasmodic, antiarrhythmic, antidiarrheal, and antiviral properties of 2-{3-[4-azatricyclo(4.3.1.1.sup.3,8)undecan-4-yl]-1,1-diphenylpropyl}-5-me thyl-1,3,4-oxadiazole and congeners are disclosed.

Abstract: The present invention relates to compounds of the following formula ##STR1## wherein Y is straight or branched chain alkylene containing 1-4 carbon atoms; X is hydrogen, halo such as fluoro, chloro, bromo or iodo, or lower alkyl containing 1-7 carbon atoms; Ar is phenyl, pyridyl, mono-substituted phenyl, wherein the substituent is halo such as fluoro, chloro, or bromo, or lower alkyl having 1-7 carbon atoms; and R.sub.2 and R.sub.3 are lower alkyl having 1-7 carbon atoms, or R.sub.2 and R.sub.3 together with N is an azamonocyclic ring selected from the group comprising 1-pyrrolidinyl, piperidino, 4-phenyl-4-hydroxypiperidino, 4-phenyl-4-hydroxymethylene, 4-phenyl-4-carboxypiperidino, 4-phenyl-4-carbloweralkoxypiperidino, or 4-phenyl-4-acetoxypiperidino substituted piperidino and morpholino, or an azabicycloalkanyl containing 6 to 9 carbon atoms and having at least 5 atoms in each ring of the azabicycloalkane. These compounds are useful intermediates for preparing potent antidiarrheal compounds.

Abstract: The present invention relates to compounds of the following formula ##STR1## wherein Y is straight or branched chain alkylene containing 1-4 carbon atoms; R.sub.1 is lower alkyl containing 1-7 carbon atoms; X is hydrogen, halo such as fluoro, chloro, bromo or iodo, or lower alkyl containing 1-7 carbon atoms; Ar is phenyl, 2-pyridyl, mono-substituted phenyl, wherein the substituent is halo such as fluoro, chloro, or bromo, or lower alkyl containing 1-7 carbon atoms; and R.sub.2 and R.sub.3 are lower alkyl containing 1-7 carbon atoms, or R.sub.2 and R.sub.3 together with N is an azamonocyclic ring selected from the group comprising pyrrolidinyl, piperidino, 4-phenyl-4-hydroxypiperidino, 4-phenyl-4-carboxypiperidino, 4-phenyl-4-carbalkoxypiperidino, or 4-phenyl-4-acetoxypiperidino substituted piperidino and morpholino, or an azabicyclo-alkane containing 6 to 9 carbon atoms and containing at least 5 atoms in each ring of the azabicycloalkane.