Abstract: This invention relates to compounds of Formula I and the stereoisomers and pharmaceutically acceptable salts thereof ##STR1## wherein R is alkyl, alkenyl, alkynyl, or cycloalkylalkyl and m is 1 or 2;R.sup.1 is alkyl of 1 to 4 carbon atoms;R.sup.2 is hydrogen or alkyl of 1 to 5 carbon atoms;R.sup.4 is alkyl of 1 to 6 carbon atoms;n is an integer from 1 to 5; andY is NH or oxygen.The compounds of Formula I are leukotriene B.sub.4 antagonists and are useful as anti-inflammatory agents and in the treatment of LTB.sub.4 mediated diseases.

Abstract: This invention encompasses a compound of the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of 1,1-dimethylethyl, halo, phenyl and substituted phenyl; Alk is straight or branched chain lower alkylene; R.sub.4 is hydrogen or lower alkyl; R.sub.3 is hydrogen or lower alkyl; or a cycloalkyl group of from 3 to 8 carbon atoms. The formulation of this invention are useful as anti-inflammatory and anti-allergy agents.

Abstract: Compounds of formula I ##STR1## are described which are useful to inhibit the formation of serum cholesterol by virtue of their ability to inhibit .beta.-hydroxy-.beta.-methylglutaryl-CoA(HMG CoA), the rate-controlling substance in the synthesis of serum cholesterol.

Abstract: This invention encompasses compounds and methods for inhibiting lipoxygenase and includes a pharmaceutical composition comprising a pharmaceutical carrier and an effective lipoxygenase inhibiting amount of a compound of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different members of the group consisting of tert-alkyl of 4 to 10 carbon atoms; and R.sub.3 isa) ##STR2## wherein R.sub.4 is hydrogen or lower alkyl; b) ##STR3## c) ##STR4## wherein R.sub.6 and R.sub.7 may be the same or different and are alkyl of 1 to 4 carbon atoms; ord) ##STR5## and the pharmaceutically acceptable salts thereof. The compounds and pharmaceutical formulations of the present invention are 5-lipoxygenase inhibitors and, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metabolic pathway are involved.

Abstract: A novel S diastereomer of an N.sup.6 -[(2-hydroxypropyl)aryl] adenosine, which diastereomer exhibits fewer CNS side effects than the racemate, but with no decrease in cardiovascular activity. The invention further provides for compositions incorporating the diastereomer, and methods of its use, as well as pharmaceutically acceptable salts thereof.

Abstract: A novel R diastereomer of an N.sup.6 -[(2-hydroxypropyl)aryl]adenosine, which diastereomer exhibits fewer CNS side effects than the racemate, but with no decrease in cardiovascular activity. The invention further provides for compositions incorporating the diastereomer, and methods of its use as well as pharmaceutically acceptable salts thereof.

Abstract: The present invention relates to a method of inhibiting tumor metastasis in an aminal by administering to an animal in need of such treatment an acrylaminoalkylpryridineamides represented by the formula ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided n+m+p is equal to or less than 10; x is thio or sulfinyl; Alk.sub.1 is straight or branched chain lower alkylene of 1 to 6 carbon atoms, R.sub.3 is hydrogen or lower alkyl, Alk.sub.2 is straight or branched chain alkylene of 1 to 4 carbon atoms; R.sub.4 is selected from the group consisting of hydrogen, halo, hydroxy, lower alkyl and lower alkoxy; or a pharmaceutically acceptable salt thereof, in an amount effective to inhibit tumor metastasis.

Abstract: N-benzylpiperidine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.

Abstract: The compounds of this invention are bicyclic, tricyclic, azabicyclic and azatricyclic amides represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein n, m and p are independently an integer of from 1 to 8 provided that n+m+p is equal to or less than 10; X is thio, sulfinyl or sulfonyl; Alk is straight or branched chain lower alkylene; R.sub.3 is selected from the group consisting of a bicycloalkylamino, tricycloalkylamino, azabicycloalkyl, azatricycloalkyl, azabicycloalkylamino, azatricycloalkylamino or dicycloalkylamino. The compounds are useful as anti-inflammatory and anti-allergy agents.

Abstract: This invention relates to novel substituted imidazopyridine derivatives having the following formula ##STR1## or a pharmaceutically acceptable acid addition salt useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention relates to pharmaceutical compositions of such substituted imidazopyridines.

Abstract: A stabilized pharmaceutical composition which is an admixture of an NSAID selected from diclofenac and piroxicam, a prostaglandin and hydroxypropyl methylcellulose for maintaining the prostaglandin in a therapeutically effective amount without negatively affecting the therapeutic activity of the NSAID.

Abstract: A process for producing an .alpha.-alkoxy acetic acids and salts thereof which comprises reacting an alcohol of the formula R--OH wherein R is alkyl, substituted alkyl, or cycloalkyl, or cycloalkyl alkyl with a base in an aprotic organic solvent to give an alkoxide followed by removal of the organic solvent and reaction of the alkoxide with a salt of a monohaloacetic acid in a polar aprotic solvent such as DMSO to give the corresponding alkoxyacetate salt which then may be recovered or may optionally be converted to the corresponding acid by contacting the alkoxy acetate salt with an acid.

Abstract: A pharmaceutical composition and a method of inhibiting human immunodeficiency virus (HIV) is disclosed which comprises administering to an HIV infected patient a synergistic combination of 3'-azido-3'-deoxythymidine (AZT) and N-butyl deoxynojirimycin (N-butyl DNJ) in an amount which achieves antiviral efficacy.

Abstract: This invention encompasses a process for preparing higher order cuprate complexes which contain a carbanion for the formation of carbon to carbon bonds in reactions such as epoxide addition. The complex is formed by reacting a first cuprate complex with a stannane such that the carbanion to be used to form carbon to carbon bonds is transferred from the stannane to the first cuprate complex to form a different higher order cuprate complex. This process permits the in situ preparation of a higher order cuprate complex having the carbanion desired to be used in a synthetic reaction. Higher order cuprate complexes derived from the reaction of a cuprate complex with 1,2-bis-tri-n-butylstannyl ethylene are particularly useful for the addition to epoxides to form vinyl tin intermediates useful for preparing omega side chains of prostaglandins.

Abstract: A method of inhibiting tumor metastasis in an animal without treating the tumor cells by administering to said animal a metastasis inhibiting effective amount of a heterocyclic amide represented by the formula: ##STR1## wherein: R.sub.1 and R.sub.2 are the same or different members of the group consisting of halo, phenyl, substituted phenyl and a ##STR2## group wherein q, r and t are independently an integer of from 1 to 8 provided that q+r+t is equal to or less than 10; Y is thio or sulfinyl; alk is straight or branched chain lower alkylene, and R.sub.3 is a heterocyclic amine represented by the formula: ##STR3## wherein R.sub.4 is selected from the group consisting of hydrogen, lower alkyl, phenyl, substituted phenyl, benzyl, or substituted benzyl; p is 0 to 2; or a pharmaceutically acceptable salt thereof.

Abstract: The compounds of the present invention comprise substituted phenolic thioethers, sulfoxides, and disulfides that are specific inhibitors of 5-lipoxygenase and which, therefore, are useful in the treatment of local and systemic inflammation, allergy and hypersensitivity reactions and other disorders in which agents formed in the 5-lipoxygenase metablic pathway are involved.

Abstract: A class of phosphono-hydroisoquinoline componds 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 phosphono-hydroisoquinoline compound 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.1 through R.sup.4 is hydrido, each of Z.sup.1 and Z.sup.2 is hydroxyl and wherein the A ring is aromatic.

Abstract: Tricyclic quinolizine amides, which have activity as Class III antiarrhythmic agents, acting by prolonging cardiac action potential repolarization. The invention further provides for compositions incorporating the compounds and methods of their use, as well as providing for pharmaceutically acceptable salts of the compounds.

Abstract: A method of making novel R and S diastereomers of an N.sup.6 -[(2-hydroxypropyl)aryl] adenosine, which diastereomers exhibit fewer CNS side effects than the racemate, but with no decrease in cardiovascular activity.

Abstract: This invention relates to substituted imidazopyridine derivatives having the follow formula ##STR1## or a pharmaceutically acceptable acid addition salt thereof: wherein the variables are described in the specification are useful in the treatment of diseases or disorders mediated by platelet-activating factor. This invention also relates to pharmaceutical compositions of such substituted imidazopyridines.