Abstract: Compounds having the formula ##STR1## and salts thereof, wherein R.sub.1 is a readily hydrolyzable acyl protecting group;R.sub.2 is hydrogen or alkyl;R.sub.3 is hydrogen, alkyl or arylalkyl;n is 1 or 2; andp is 1 or 2inhibit the action of angiotensin converting enzyme.
Abstract: Photolysis of azetidin-2-one derivatives having the formula ##STR1## wherein R.sub.1 is acyl, R.sub.2 is hydrogen or .alpha.-methoxy, R.sub.3 is hydrogen, alkyl, 2,2,2-trichloroethyl, trimethylsilyl, diphenylmethyl, benzyl, 4-methoxybenzyl, or 4-nitrobenzyl, and R.sub.4 is an aromatic heterocyclic group, yields 3-methylene cephalosporins.
Abstract: A myocardial imaging agent is provided having the structure ##STR1## wherein Q, R.sub.1, R.sub.2, R.sub.3 and R.sub.4 and A are as defined herein. A method for scanning the heart, liver or kidneys employing the above agent is also provided.
Abstract: Compounds of the formula ##STR1## wherein X is an imino acid or ester and R.sub.1 is hydrogen, ##STR2## are useful hypotensive agents due to their angiotensin converting enzyme inhibition activity.
Abstract: Bis-amidine indene ketones are provided having the structure ##STR1## wherein R is hydrogen, lower alkyl or aryl; and R.sup.1 is hydrogen, lower alkyl, halogen, carboxy, trifluoromethyl, lower alkoxy, hydroxy or acyl, and acid-addition salts thereof. In addition, pharmaceutical compositions containing the above compounds and a method of using same to treat inflammatory conditions in mammalian species are also provided.
Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity.
Abstract: A method is provided for preparing intermediates for use in prostacyclin syntheses which method includes the steps of aceylating ketopinic acid or its acid halide to form the corresponding ketopinoyl diene ester intermediate, subjecting the diene ester to a Diels-Alder reaction by reacting same with cyclopentendione, subjecting the resulting chiral ester intermediate to a fluorination and reduction to form the corresponding chiral ester diol intermediate, subjecting the diol to solvolysis to form the chiral triol intermediate, hydroxylating the chiral triol to form a pentol intermediate, subjecting the pentol to a ring cleavage to form the difluoro dihydroxy prostacyclin intermediate: ##STR1## and subjecting same to a Wittig reaction to form the difluoro dihydroxy prostacyclin intermediate: ##STR2## All of the above-mentioned intermediates are novel compounds and thus are also provided.
Type:
Grant
Filed:
September 24, 1981
Date of Patent:
December 7, 1982
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jerome L. Moniot, Rita T. Fox, Peter W. Sprague, Martin F. Haslanger
Abstract: 3-Ketoandrostenes having in the 17-position the substituents R.sub.1 --S-- and R.sub.2 --S-- wherein R.sub.1 and R.sub.2 are the same or different and each is alkyl, cycloalkyl or aryl, have antiinflammatory activity.
Abstract: The invention relates to chroman derivatives of the general formula ##STR1## wherein R.sub.1 is hydrogen, lower alkyl, substituted phenyl, phenyl, phenyl-lower alkyl, substituted phenyl-lower alkyl or lower alkyl-amino-lower alkyl;R.sub.2 is ##STR2## R.sub.3, R.sub.4, R.sub.5 and R.sub.6 each is independently selected from hydrogen, hydroxy, amino, -o-acyl, -o-lower alkyl; ##STR3## halogen, lower alkyl, or halo substituted lower alkyl; and salts and hydrates thereof.These compounds are useful as anti-inflammatory agents; for inhibition of blood platelet aggregation, as antiallergy and as antihypertensive agents.
Abstract: New dioxatricyclic prostacyclin analogs are provided which have the general formula ##STR1## wherein R is hydrogen or lower alkyl, Q is a single bond or --CH.sub.2 --, m is 1 to 9 and n is 3 or 4, and all stereoisomers thereof, and are useful as cardiovascular agents.
Abstract: This invention is directed to compounds of the formula ##STR1## and various intermediates therefore. The final products possess useful hypotensive activity.
Abstract: Compounds are provided having the structure ##STR1## wherein R.sup.1 and R.sup.2 may be the same or different and are hydrogen, lower alkyl, lower alkenyl, or hydroxylower alkyl, or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached also form a heterocyclic radical which may contain another heteroatom, namely nitrogen, oxygen or sulfur; R.sup.3 and R.sup.4 may be the same or different and are hydrogen or lower alkyl. These compounds are useful in the treatment of arrhythmia.In addition, novel intermediates are provided having the structure ##STR2## wherein R is hydrogen, benzyl or ##STR3## These intermediates are also useful in treating acute myocardial infarction.
Abstract: An article of manufacture comprising a pharmaceutical radioactive capsule formed essentially of a non-toxic, water soluble material adapted to being ingested and rapidly disintegrating on contact with fluids of the gastro-intestinal tract, and having a filler material supporting a pharmaceutically useful radioactive compound absorbable from the gastro-intestinal tract said filler material being supported by said capsule. And a method of filling a pharmaceutical radioactive capsule comprising providing filler material supporting a pharmaceutically useful radioactive compound and transporting said filler material carrying a pharmaceutically useful radioactive compound into the chamber of said capsule.
Type:
Grant
Filed:
April 14, 1980
Date of Patent:
September 14, 1982
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Nabil A. Morcos, Thomas A. Haney, Paul W. Wedeking
Abstract: A steroid formulation is provided which is preferably in the form of a lotion or cream and contains a steroid, such as halcinonide, a polyol vehicle therefor, such as polyethylene glycol, and dipotassium ethylenediaminetetraacetic acid which is soluble in the polyol vehicle and inhibits metal catalyzed degradation of the steroid.
Abstract: Radiolabeled steroid derivatives having the formula ##STR1## wherein St is a des-hydroxy steroid moiety of (i) a hydroxy steroid intended for radioimmunoassay or (ii) a hydroxy containing derivative of a steroid intended for radio-immunoassay, said derivative having a strong affinity for the antibodies of the steroid intended for radioimmunoassay; R is hydrogen or alkyl of 1 to 3 carbon atoms; n is 0, 1, 2, 3 or 4 and the asterisk (*) indicates tagging with a radioisotope, are useful as tracers in radioimmunoassays.
Type:
Grant
Filed:
March 10, 1980
Date of Patent:
August 17, 1982
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jack Bernstein, Ravi K. Varma, B. Richard Vogt, Frank L. Weisenborn
Abstract: A container having a container tube with a central tube chamber and apertures at both ends with a resilient plug over each aperture, a weir extending into the central tube chamber.The container is useful for drawing blood and labeling it with Tc-99.The container is sterile and sealed at less than atmospheric pressure inside.
Abstract: Disclosed herein is a pharmaceutically active gelled composition of dimethyl sulfoxide for utilization in the treatment of musculoskeletal disorders.
Abstract: The labeling of red blood cells with technetium-99m using a stannous reducing agent is facilitated by the addition of an oxidizing agent along with the radioactive pertechnetate ion.