The Rockefeller University

Other

Henry Hirsch and Stanley Rothschild, Trustees

Jack Fishman

Mary Jeanne Kreek

Shinichi Mayairi

Method for controlling gastrointestinal dysmotility in humans by administration of opioid antagonists.

Method for controlling gastrointestinal dysmotility

A method of treating patients in chronic pain or suffering from chronic cough over a prolonged period to provide systemic analgesia or central antitussive effect while simultaneously avoiding the onset of intestinal hypomotility. The method includes the oral administration to the patient of dosage units comprising in combination opioid analgesics or antitussives and selected opioid antagonists which are substantially devoid of systemic antagonist activity when administered orally.

Method of treating patients suffering from chronic pain or chronic cough

Invention relates to 3-methylene substituted androst-4-ene-17-oxygenated compounds substituted with various substituents at the 10.beta.-position which are useful as inhibitors of estrogen biosynthesis.

Estrogen synthesis inhibitors

Novel compounds constituting esters of benzoic acids, selected from the group consisting of p-vinyl benzoic acid and p-ethynyl benzoic acid, with an aminoethanol selected from the group consisting of diethylaminoethanol and N-substituted aminoethanols. The esters have the formula ##STR1## where X is selected from the group consisting of ##STR2## or HC.tbd.C and each of R.sub.1 and R.sub.2 is selected from the group consisting of H, lower alkyls containing up to 6 carbon atoms and cycloalkyls. The novel compounds also include inorganic and organic acid salts of said esters. The novel compounds have a unique medicinal function as local subcutaneously-applied anesthetics which have a long-acting effect when administered without vasoconstrictors that heretofore have been used to prevent rapid dissipation of subcutaneously-applied local anesthetics. The invention also embraces compositions containing the compounds and the method of using the novel compounds and compositions as local long-acting subcutaneously-applied anesthetics.

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New York, NY, United States of America

Jack Fishman