Merck + Co., Inc.

Gerard R Kieczykowski

Richard Robert Dauer

Lisa DiMichele

Mauricio Futran

William J Greenlee

Thomas F Walsh

William H Parsons

Prasun K Chakravarty

Kathleen M Rupprecht

Robert K Baker

Scott William Bagley

James R Tata

Hyun O Ok

Ralph A Rivero

David G Melillo

Daljit S Dhanoa

Nancy J Kevin

Richard B Toupence

Kenneth J Fitch

Douglas J Pettibone

Ronald B Jobson

David L Williams

Theodore P Broten

Jay M Matthews

Ruth V Wattley

Phenoxyphenylacetic acids and derivatives of the general structural formula I ##STR1## have endothelin antagonist activity and are useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, endotoxic shock, benign prostatic hyperplasia, inflammatory diseases including Raynaud's disease and asthma.

Phenoxyphenylacetic acid derivatives

Process for producing n-amino-1-hydroxy-alkyl-idene-1,1-bisphosphonic

Aryl and heteroaryl macrolides of the general structural Formula I: ##STR1## have been prepared from suitable precursors by olefination at C-27. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases, the prevention of rejection of foreign organ transplants and/or related afflictions, diseases, and illnesses.

Aryl and heteroaryl macrolides having immunosuppressive activity

A process for continuously producing alkylpyrophosphonate, alkylpyrophosphate and multimers thereof and for producing 4-amino-1-hydroxyalkylidene-1,1-bisphosphonic acids or salts thereof.

Process for producing N-amino-1-hydroxy-alkylidene-1,1-bisphosphonic

Described is a new process for producing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP), a new antihypercalcemic agent. The process involves a 3-step sequence starting with 4-phthalimidobutanoyl chloride which can be practiced as a 'one-pot' reaction sequence, without employing PCl.sub.3 or H.sub.3 PO.sub.3.

Process for preparing an antihypercalcemic agent

Described is a new diphosphonate intermediate useful in a new process for producing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid (ABP), a new antihypercalcemic agent. The process involves a 3-step sequence starting with 4-phthalimidobutanoyl chloride which can be practiced as a 'one-pot' reaction sequence, without employing PCl.sub.3 or H.sub.3 PO.sub.3. The new intermediate has the structure: ##STR1## where n=1-5.

Diphosphonate intermediate for preparing an antihypercalcemic agent

An improved process is described for the preparation of 4-amino-1-hydroxybutylidene-1,1-bisophosphonic acid (ABP) or salts thereof which comprises:

Process for preparing 4-amino-1-hydroxybutylidene-1,1-bisphosphonic acid

A process for the preparation of 4-amino-1-hydroxybutylidene-1, 1-bisphosphonic acid or salts thereof which comprises:

The muscle relaxant (E)-3-(9-chloro-5,6-dihydro-11H-pyrrolo[2,1-b][3]benzazepin-11-ylidene-N,N -dimethyl-1-propanamine is prepared by the geometric stereoselective dehydration of the intermediate carbinol with acidic agents and organic bases and low temperatures.

Process for the geometric stereoselective dehydration of

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Westfield, NJ, United States of America

Gerard R Kieczykowski