Abstract: A process is provided for preparing the keto-phosphonate ##STR1## in enantiomerically homogeneous form, by reacting the anhydride ##STR2## with S-.alpha.-methylbenzylamine to effect diastereoselective opening of the anhydride to give a mixture of amides ##STR3## separating the amides, for example, by frictional crystallization, and converting the desired amide IVA (which is obtained in high yield from the anhydride) to enantiomerically homogeneous ketophosphonate in high yield and on a large scale.The so-formed ketophosphonate is useful in the synthesis of compactin as well as 7-substituted-(3,5-dihydroxy)-hept-6-enoic and -heptanoic acid HMG-CoA reductase inhibitors.
Abstract: A dispensing device for a radionuclide generator includes an eluant container, a receptacle for receiving the container, the receptacle being in sliding engagement with a support, a hollow needle which pierces the elastic stopper of the container so that the tip of the needle penetrates into the container, and a fixing device for holding the needle at a distance from its tip. The volume dispensed from the container is controlled by shifting the receptacle up or down within the support along the longitudinal axis of the needle.
Abstract: Acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
Type:
Grant
Filed:
November 13, 1987
Date of Patent:
January 17, 1989
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Norma G. Delaney, Eric M. Gordon, Miguel A. Ondetti
Abstract: A device for wound management permits the application of an apertured pad to the wound and involves the provision of a protective compartment, optionally drained, whose interior is open to the wound and which is normally sealed closed but which can be opened if desired.
Abstract: In accordance with the present invention an improved adhesive structure for adhesion of an article to a fluid-emitting wound and the surrounding normal skin is disclosed. The adhesive structure comprises a first contact region comprised of a fluid-interactive adhesive material which provides adhesion to the wound and surrounding normal skin; a second contact region comprised of the same or a different adhesive material, which provides adhesion betweeen the first region, or another region integral with the first region, and the article; and, an absorbent region comprised of an absorbent fibrous, fabric or foam material intermediate the first and second regions whereby enhanced cohesion between the first and second regions and between the second region and the article, under conditions of heavy fluid emission, is provided.
Type:
Grant
Filed:
November 17, 1986
Date of Patent:
December 27, 1988
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Frank Freeman, Michael J. Amery, Clyde L. Sharik
Abstract: A controlled release pharmaceutical formulation is provided which releases a pharmaceutical of a basic character at a controlled rate regardless of the pH of the environment, which formulation includes a basic pharmaceutical, up to about 45% by weight of a pH dependent polymer which is a salt of alginic acid, such as sodium alginate, up to about 35% by weight of a pH-independent hydrocarbon gelling agent having a viscosity of up to about 100,000 centipoises in 2% solution at 20.degree. C., binder and excipients.
Abstract: Hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is hydrogen or alkyl;R.sub.2 and R.sub.3 are each independently phenyl, substituted phenyl, cycloalkyl, or R.sub.2 is hydrogen and R.sub.3 is heteroaryl;R.sub.4 and R.sub.5 are the same or different and each is hydrogen, hydroxy, alkoxy, alkanoyl or alkyl;R.sub.6 is hydrogen or alkyl; andn is 1, 2, 3 or 4; with the proviso that if R.sub.2 and R.sub.3 are each phenyl, at least one of R.sub.1, R.sub.4, R.sub.5 and R.sub.6 is other than hydrogen.
Type:
Grant
Filed:
April 24, 1985
Date of Patent:
November 29, 1988
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
David M. Floyd, Spencer D. Kimball, Steven Brandt
Abstract: Geminally-substituted cyclic ether carboxylic acids or derivatives thereof are provided which have the structure ##STR1## wherein Z is aryl, which may be optionally substituted with one or more of the following groups: halo, lower alkyl, lower alkoxy, hydroxy, lower alkylamino, phenyl or carbo-lower alkoxy ##STR2## R is COOH, COO alkali metal, coo lower alkyl, ##STR3## R.sup.1 is lower alkyl or aryl; n is 1 or 2;p is 2 to 5; andq is 1 to 4.These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic disease.
Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl;R.sup.2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl;m is 2 to 8; andZ is ##STR2## wherein R.sup.3 is OH, COOH ##STR3## These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
Abstract: Antibacterial activity is exhibited by 3-acylamino-2-oxoazetidines having in the 1-position an activating group of the formula ##STR1## wherein R is ##STR2## and R.sub.
Abstract: The device comprises a substantially cylindrical support member which carries or in part defines an inflatable cuff. The cuff extends for only a portion of the length of said support member. Means are provided for inflating the cuff with air and transmitting changes in pressure within the cuff to a display device such as a pressure gauge.
Abstract: Antibacterial activity is exhibited by .beta.-lactams having a sulfonic acid salt substituent in the 1-position and an amino or acylamino substituent in the 3-position.
Type:
Grant
Filed:
January 19, 1981
Date of Patent:
October 4, 1988
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Richard B. Sykes, William L. Parker, Christopher M. Cimarusti, William H. Koster, William A. Slusarchyk
Abstract: A composite skin barrier including a first adhesive component which fits around the stoma, a coupling element, and a second adhesive component which is flexible, light, and has a degree of porosity. The second adhesive component contacts the skin at a distance from the stoma.
Type:
Grant
Filed:
June 24, 1987
Date of Patent:
October 4, 1988
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Rudolfo D. Cilento, Edward C. Smith, Jr., Frank M. Freeman
Abstract: An occlusive wound dressing comprising a flexible closed cell polyurethane foam containing from about 5% to about 50% by weight of the foam of one or more water dispersible, water swellable, and/or water absorbing agents. A pressure sensitive microporous adhesive is applied or laminated to one surface of the foam as a continuous layer. A polymeric film or skin is laminated or formed on the opposite surface of the foam.
Abstract: An occlusive wound dressing comprising a flexible closed cell polyurethane foam containing from about 5% to about 50% by weight of the foam of one or more water dispersible, water swellable, and/or water absorbing agents. A pressure sensitive adhesive is applied or laminated to one surface of the foam in a discontinuous pattern. A polymeric film or skin is laminated or formed on the opposite surface of the foam.
Abstract: A new class of benzazepine derivatives having the general formula ##STR1## including pharmaceutically acceptable salts, are disclosed. These compounds are useful as cardiovascular agents, particularly as vasodilators.
Abstract: Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
Type:
Grant
Filed:
November 13, 1987
Date of Patent:
September 27, 1988
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Norma G. Delaney, Eric M. Gordon, Miguel A. Ondetti
Abstract: The container has an elongated port section formed of a flexible cylindrical wall. A first tube member is lodged within the wall at a location spaced from the end thereof. A second tube member is forceably inserted within the first tube member, engaging a section of the wall therebetween. The engaged wall section may include a double wall thickness. One of the tube members is composed of substantially non-elastic material and the other is composed of relatively elastic material. The elastic member will deform so as to tightly seal the wall section. A detent may be present on one of the tube members to cooperate with a detent receiving recess on the other to enhance the strength of the seal. Any conventional drain valve or tubing can be connected to the protruding end of the second tube member.
Type:
Grant
Filed:
February 24, 1987
Date of Patent:
September 20, 1988
Assignee:
E. R. Squibb & Sons
Inventors:
Ole R. Jensen, Walter F. Leise, Frank M. Freeman
Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituted and having an activating group in the 1-position of the formula ##STR1## wherein A.sub.1 is a single bond, ##STR2## and A.sub.