Usv Pharmaceutical Corporation

Rorer Pharmaceutical Corporation

Rhone-poulenc Rorer Pharmaceuticals Inc.

Raymond D Youssefyeh

Henry F Campbell

Howard Jones

John T Suh

Jerry W Skiles

Jeffrey C Pelletier

Donald E Kuhla

Matthew R Powers

Utpal R Chakraborty

John E Airey

William L Studt

Christopher J Burns

Scott I Klein

Edward S Neiss

Jeffrey D Wilson

Rohit M Desai

John W Ullrich

Walter Rodriguez

Daniel L Cheney

Frederick A Golec

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.

Azacyclic bisphosphonates as anticholesterolemic agents

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.

2,6-methano-2H-1-benzoxocincarboxylic acids, esters and amides

This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinctic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

Pharmaceutically useful dibenzofurancarboxamides of specific

This invention is directed to certain dibenzofurancarboxamides and dibenzofurancarboxamide acids and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. Further, this invention relates to a process for the synthesis of stereoisomeric compounds having such CNS, anti-emetic and gastric prokinetic activity.

Process for the preparation of optically pure amides

This invention relates to a series of bicyclic benzomonoazacyclic carboxamide compounds of the general formula: ##STR1## Where Z is tertiary amine, which are useful for the method of treating patients suffering from gastrointestinal disorders, and of pharmaceutical composition including an effective 5HT3 - antagonists amount of said compounds therein.

Substituted saturated and unsaturated indole quinoline and benzazepine

This invention is directed to certain dibenzofurancarboxamides and their use as 5HT.sub.3 antagonists having unique CNS, anti-emetic and gastric prokinetic activity void of any significant D.sub.2 receptor binding properties. This invention also describes novel processes necessary for their preparation.

Hexahydrodibenzofuran carboxylic acid derivatives

This invention relates to benzoxazine and benzoxazepine carboxamide compounds which exhibit 5-HT.sub.3 antagonist properties including CNS, anti-emetic and gastric prokinetic activity and which are void of any significant D.sub.2 receptor binding affinity. This invention also relates to pharmaceutical compositions and methods for the treatment of gastrointestinal and mental disorders using said compounds.

Benzoxazine and benzoxazepine carboxamide 5-HT.sub.3 antagonists

This invention relates to heteroazabenzo-bicyclic substituted carboxamide compounds of the formula: ##STR1## where W is O, S or NR.sub.5 and

Heteroazabenzobicyclic carboxamide 5-HT.sub.3 antagonists

Certain specific substituted benzobicyclic carboxamides and their valuable use as 5-HT3 antagonists having CNS and gastric prokenetic activity void of any significant D.sub.2 receptor binding activity are disclosed.

Benzobicyclic carboxamide 5-HT3 antagonists

Certain specific substituted azabicyclic carboxiamides and their valuable use as 5-HT3 antagonists having CNS and gastric prokenetic activity void of any D.sub.2 receptor binding properties are disclosed.

Dibenzofurancarboxamides and their pharmaceutical compositions and

Provided are antihypertensive compounds of the formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl, and may be the same or different,

Antihypertensive amide compounds

This invention relates to new chemical compounds having valuable pharmaceutical activity. It particularly relates to stereoisomeric compounds possessing hypotensive activity, i.e., angiotensin converting enzyme inhibitory (ACEI) activity and having the structure ##STR1## wherein R and R.sub.9 are independently hydroxy, lower alkoxy, lower alkenoxy, di(lower alkyl)amino-lower alkoxy, hydroxy-lower alkoxy, acylamino-lower alkoxy, acryloxy-lower alkoxy, aryloxy, aryloxyl-lower alkoxy, amino, lower alkylamino, di-lower alkylamino, hydroxyamino, or aryl-lower alkylamino;

N-substituted-amido-amino acids

Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy or lower alkoxy,

This invention relates to new lipoxygenase inhibitors possessing anti-inflammatory and anti-allergic properties. The present new compounds are of the formula: ##STR1## and salts thereof; wherein

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Tarrytown, NY, United States of America

Raymond D Youssefyeh