Rhone-poulenc Rorer Pharmaceuticals Inc.

Rorer Pharmaceutical Corporation

Aventis Pharmaceuticals Products Inc.

Aventis Pharmaceuticals Inc.

Scott I Klein

Bruce F Molino

Mark Czekaj

Henry F Campbell

Donald E Kuhla

Kevin Richard Guertin

Alfred P Spada

Raymond Youssefyeh

Heinz W Pauls

Bruce Francis Molino

Jeffrey C Pelletier

Raymond D Youssefyeh

Daniel Gerard McGarry

Matthew R Powers

Michael R Becker

Yong Gong

John E Airey

Jeffrey M Dener

This invention is directed to N-acylpyrrolidin-2-ylalkylbenzamidine derivatives which useful for inhibiting the activity of Factor Xa, by contacting said derivatives with a composition containing Factor Xa. The present invention is also directed to compositions containing said derivatives, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

N-acylpyrrolidin-2-ylalkylbenzamidine derivatives as inhibitors of factor Xa

The present invention relates to peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and dissembulated intravascular coagulation.

Antithrombotic azacycloalkylalkanoyl peptides and pseudopeptides

This invention relates to compounds of formula

Substituted N-&lsqb;(aminoiminomethyl or aminomethyl)phenyl&rsqb;propyl amides

This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.

Piperididinyl and N-amidinopiperidinyl derivatives

The present invention relates to azacycloalkylalkanoyl peptides and pseudopeptides which inhibit platelet aggregation and thrombus formation thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease, and disseminated intravascular coagulation, to methods for the prevention or treatment of thrombosis in a mammal in need of such therapy comprising the administration of a therapeutically effective amount of such compounds, and to pharmaceutical compositions comprising such compounds.

Substituted intermediate compounds for the preparation of

The compounds according to the invention are substituted N-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides of formula I herein which exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are Factor Xa inhibitors. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, methods for their preparation and their use, which are for treating a patient suffering from, or subject to, conditions which can be ameliorated by the administration of an inhibitor of Factor Xa.

Substituted n-[(aminoiminomethyl or aminomethyl)phenyl]propyl amides

The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-�N-�N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl!-(L)-aspartyl!-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.

This invention relates to novel peptide and pseudopeptide derivatives and analogs of aspartic acid which are useful as inhibitors of platelet aggregation and thrombus formation in mammalian blood, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.

Antithrombotic peptides and pseudopeptides

Disclosed are novel peptide and pseudopeptide derivatives and pharmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.

Anti-thrombotic peptide and pseudopeptide derivatives

This invention relates to novel diaminoalkanoic acid derivatives that inhibit platelet aggregation and thrombus formation in mammalian blood thereby being useful in the prevention and treatment of thrombosis associated with disease states such as myocardial infarction, stroke, peripheral arterial disease and disseminated intravascular coagulation, to pharmaceutical compositions including such compounds, and to their use in inhibiting thrombus formation and platelet aggregation in mammals.

Antithrombotic diaminoalkanoic acid derivatives

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

Disclosed are novel peptide and pseudopeptide derivatives and phrmaceutical compositions thereof that inhibit platelet aggregation and thrombus formation in mammalian blood.

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Norristown, PA, United States of America

Scott I Klein