Abstract: This invention relates to bicyclic aryl compounds having selective LTB.sub.4 antagonist properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, and to methods for the treatment of disorders which result from LTB.sub.4 activity and pharmaceutical compositions including such compounds.

Abstract: The present invention relates to new lupane dervivatives of the general formula: ##STR1## to their salts, to their preparation and to the pharmaceutical compositions which contain them.

Abstract: This invention relates to a class of novel aliphatic amino bis-aryl compounds containing at least four carbon atoms and an amino group either substituted thereon or incorporated therein and is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: This invention relates to a class of novel polycyclic compounds containing a cycloalkyl ring having substituted thereon a primary amine and which is further linked or bridged to two mono- and/or bicyclic rings and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: This invention relates to a class of novel phosphonate derivatives of lipophilic amines which exhibit squalene synthase inhibition properties. More specifically the compounds are bis aryl cycloalkylamino and azacycloalkyl phosphonates. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: Oxazole derivatives of the formula ##STR1## wherein R and R' are each hydrogen or alkyl containing 1 or 2 carbon atoms, R.sub.1 and R.sub.2 are the same or different and represent hydrogen, halogen or straight- or branched-chain (C.sub.1-4) alkyloxy radicals, and n is 3-6; their salts their isomers and mixtures and their preparation method, are method are described. These derivatives display anti-inflammatory activity.

Abstract: This invention relates to a class of novel amino bi- and tri-carbocyclic alkane compounds having bis-aryl substitution which exhibit squalene synthase inhibition properties. The bi- and tri-carbocyclic alkane ring contains an amino group and the ring is further linked or bridged to two mono- and/or bicyclic rings. Compounds of this invention reduce levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.

Abstract: Oxathiane derivatives of formula ##STR1## in which R represents alkyl and A represents optionally substituted phenyl or a heteroaromatic group containing 1 or 2 nitrogen atoms optionally substituted by alkyl, alkoxy or halogen, and salts thereof possess pharmacological activity and are also useful in inhibiting head hair loss.

Abstract: This invention relates to polycyclic compounds containing two mono- and/or bicyclic rings and a basic tertiary amino group capable of forming an ammonium ion at biological pH and which reduces levels of serum cholesterol in the body without significantly reducing mevalonic metabolite synthesis. This invention relates also to pharmacological compositions and method of treatment for lowering serum cholesterol levels using the compounds of this invention.The compounds of this invention are described by the formula ##STR1## where Ar I is phenylene or naphthylene, Ar II is phenyl or naphthyl and A is 1-azabicyclo[2.2.2]octan-3-yl.

Abstract: This invention relates to compounds having selective LTB.sub.4 antagonist properties, compositions comprising said compounds and methods for the treatment of disorders involving LTB.sub.4 agonist-mediated activity utilizing said compositions wherein the compounds are described by the general formula ##STR1## and pharmaceutically acceptable salts thereof.

Abstract: Thioformamide derivatives of formula (I): ##STR1## wherein R represents alkyl; A represents optionally substituted pyrid-4-yl; Y represents ethylene or methylene or a direct bond and X represents an optionally substituted phenyl, pyridyl, furyl or thienyl group or optionally substituted alkyl, alkenyl or cycloalkyl, and salts thereof possessing useful pharmacological properties.

Abstract: This invention relates to a method of lowering abnormally high serum cholesterol levels in the body without significantly reducing mevalonic metabolite synthesis and to novel pharmacological compositions containing as an active ingredient bisphosphonic acid and ester compounds containing a mono-, bi- or tricyclic ring linked with a bisphosphonate moiety through a basic amino alkylene group. This invention also provides novel bisphosphonate compounds and the processes for their preparation.

Abstract: Novel compounds which are 2,6-methano-2H-1-benzoxocincarboxamides having 5-HT.sub.3 -antagonist properties including unique CNS, antiemetic and gastric prokinetic activities and which are void of any significant D.sub.2 receptor binding affinity, therapeutic compositions and methods of treatment of disorders which result from 5-HT.sub.3 activity using said compounds. Processes for their preparation and the preparation of their intermediates are also disclosed.

Abstract: The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by an intramolecular Heck stereospecific synthesis substantially free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.

Abstract: A hydrazine derivative of formula (I), ##STR1## wherein A represents an optionally substituted phenyl, naphthyl or heteroaromatic group containing one or two nitrogen atoms, and R.sup.1 represents hydrogen, optionally substituted alkyl, or optionally substituted benzyl, phenethyl, or 1-naphthylmethyl, or pyrid-3-ylmethyl group, and salts thereof, possess useful pharmaceutical properties.

Abstract: Monocyclic aryl compounds having selective LTB.sub.4 antagonists properties and comprising an amido substituent, a substituent group having a terminal carboxylic acid or derivative thereof and a lipophilic substituent, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the monocyclic aryl compounds are disclosed.

Abstract: This invention relates to the stereospecific process for the preparation, separation and purification of hexahydrodibenzofurans which are used in the preparation of the 5HT.sub.3 compounds. More specifically, the present invention relates to a process for the preparation of substantially optically pure cishexahydrodibenzofuran compounds including at least two chiral fused ring centers which comprises the acidic catalyzed stereospecific ring closure by the intra-molecular inversion of a gamma, i.e. 2', carbon atom of a 2-[(2'-leaving group)cycloalkyl]phenol.

Abstract: Monocyclic and bicyclic aryl ring compounds having selective LTB.sub.4 properties and comprising two ring substituents, the first substituent comprising a lipophilic group and a terminal carboxylic acid or derivative group, and the second substituent comprising an amido group, therapeutic compositions and methods of treatment of disorders which result from LTB.sub.4 activity using the mono- and bicyclic aryl compounds are disclosed.

Abstract: In a method in which an ionizable pharmaceutical material, such as theophylline, having a pharmaceutically-active anionic group is bonded to an anion exchange resin having cationic groups bonded to displacable anionic groups by bringing said material and said resin into contact with each other under conditions such that the pharmaceutically-active anionic group of said material is bonded to the cationic group of said resin and replaces the anionic group thereof, the improvement comprising effecting said contact in an environment which is substantially free of carbon dioxide and/or bicarbonate ion, a pharmacologically active composition comprising said pharmaceutically active anion and said resin, including a composition in which at least about 40% of the binding capacity of the resin comprises said pharmaceutically active anion, and a sustained release pharmaceutical composition, including enteric coated particles of the composition, and stabilizing said composition by maintaining it in an environment substan

Abstract: The present invention is directed to the synthesis of 2-chloro-cis-[5a(S)-9a(S)-(5a,6,7,8,9,9a-hexahydro)]dibenzofuran-4-carboxy lic acid by a stereospecific catalytic heteroannulation synthesis free of undesirable 8-chloro-2,6-methano-2H-3,4,5,6-tetrahydro-1-benzoxocin-10-carboxylic.