Abstract: A controlled release pharmaceutical formulation which undergoes substantially zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which the angiotensin converting enzyme inhibitor (S)-1-[3-(benzoylthio)-2-methyl-1-oxopropyl]-L-proline is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 8000 to about 100,00 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a conventional pharmaceutical coating composition. A method of using such controlled release formulations in treating hypertension is also provided.
Abstract: Cultivation of a strain of the microorganism Pseudomonas cepacia SC 11,783, A.T.C.C. No. 39356 yields a novel antibiotic substance which is made up of two compounds, i.e., 5-[3-[3-(hepta-1,2-dien-4,6-diynyl)oxiran-2-yl]-3-hydroxy-1-propanyl]dihyd ro-2(3H)-furanone and 5-[[3-[3-(hepta-1,2-dien-4,6-diynyl)-2-oxiranyl]-2-oxiranyl]hydroxymethyl] dihydro-2(3H)-furanone.
Abstract: 7-Oxabicycloheptane prostaglandin intermediates are provided having the general structure ##STR1## wherein one of R.sup.1 and R.sup.2 is ##STR2## and the other is hydrogen. A method for preparing the above intermediates is also provided. The final products are used in the treatment of thrombolytic disease.
Abstract: A method is provided for making substituted prolines of the structure ##STR1## wherein X is lower alkyl or aryl, R is H, lower alkyl or an alkali metal and Z is an N-protecting group, which method includes the step of reacting a compound of the structure ##STR2## wherein Z and R are as defined above and Q is Br. tosyloxy or mesylate, with an organic copper lithium compound of the structureXYCuLiwherein X is as defined above and Y is lower alkyl, aryl or CN.Where X is phenyl, the corresponding 4-cyclohexyl compound may be produced by conventional hydrogenation techniques.The compounds produced are useful as intermediates in the preparation of phosphinic acid derivatives useful in the treatment of hypertension.
Type:
Grant
Filed:
September 19, 1983
Date of Patent:
February 26, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
John K. Thottathil, Jerome L. Moniot, David Floyd, Steven Brandt
Abstract: Antibacterial activity is exhibited by .beta.-lactams having the formula ##STR1## wherein R is hydrogen or methoxy;R.sub.1 is an acyl group derived from a carboxylic acid;R.sub.2 and R.sub.3 are each independently hydrogen, alkyl, or aryl or R.sub.2 and R.sub.3 when taken together with the nitrogen atom to which they are attached are ##STR2## wherein n is 4 or 5 and R.sub.4 is hydrogen, alkyl or amino; and M.sup..sym. is hydrogen or a cation.
Abstract: Apparatus is provided for use in detecting defects, such as pin holes, cracks and/or uneven gelatin distribution, in capsule shells. The apparatus is comprised of a light box which includes one or a plurality of light bulbs disposed within the box, one or more opaque panels which are disposed in front of each light bulb, and a plurality of transparent pegs carried by the panels and protruding outwardly away from the light bulbs, each peg being adapted to carry a capsule body or cap which fits snugly over the peg. Light shining through the capsule shells disposed on the pegs indicates defects such as pin holes, cracks and/or uneven distribution of gelatin in the capsules.
Abstract: Cephalosporins of the formula ##STR1## wherein R is hydrogen, sodium, potassium or certain ester groups; R.sub.1 is in the .alpha.-configuration and is hydrogen or methoxy; R.sub.2 is hydrogen, ##STR2## X is hydrogen, ##STR3## R.sub.4 is hydrogen or lower alkyl; R.sub.5 is hydrogen, lower alkyl, ##STR4## --(CH.sub.2).sub.n --N--(lower alkyl).sub.2 ; R.sub.6 is hydrogen, sodium, or potassium; n is an integer from 1 to 4; are disclosed. These compounds are useful as anti-bacterial agents.
Type:
Grant
Filed:
March 12, 1984
Date of Patent:
February 26, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Hermann Breuer, Uwe D. Treuner, Theodor Denzel
Abstract: Amino thiol substituted dipeptides of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
Abstract: 7-Oxabicycloheptane prostaglandin intermediates are provided having the general structure ##STR1## wherein one of R.sup.1 and R.sup.2 is ##STR2## and the other is hydrogen. A method for preparing the above intermediates is also provided.
Abstract: Antibacterial activity is exhibited by .beta.-lactams having an --SO.sub.2 --NH--C--R substituent in the 1-position and an acylamino substituent in the 3-position wherein R is alkyl, phenyl, substituted phenyl, phenylalkyl, (substituted phenyl)alkyl, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, or (substituted phenyl)alkoxy.
Type:
Grant
Filed:
August 6, 1981
Date of Patent:
February 12, 1985
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Hermann Breuer, Theodor Denzel, Uwe D. Treuner
Abstract: Optically active 7-oxabicyclopheptane prostaglandin intermediates are provided having the general structure ##STR1## wherein one of R.sup.1 and R.sup.2 is ##STR2## and the other is hydrogen. A method for preparing the above intermediates is also provided.
Abstract: Topical antiinflammatory activity is exhibited by steroids having the formula ##STR1## and the 1,2-dehydro derivative thereof whereinR.sub.1 is alkyl, cycloalkyl, aryl, alkanoyloxyalkyl or arylcarbonyloxyalkyl;R.sub.2 is alkoxy, aryloxy, arylalkoxy, alkylthio, arylthio, or dialkylamino;R.sub.3 is carbonyl, .beta.-hydroxymethylene or .beta.-acetyloxymethylene;R.sub.4 is hydrogen or halogen;R.sub.5 is hydrogen, methyl, hydroxy, alkanoyl, alkanoyloxy, or halogen; andn is 0, 1 or 2.
Abstract: An ointment-like composition for the topical administration of a corticosteroid is disclosed.For the topical administration of corticosteroids an ointment-like composition comprising not less than 40% by weight of isostearyl alcohol can be used.
Abstract: An ostomy pouch having a filter element affixed to the outer pouch wall. The outer pouch wall has an aperture and the filter element includes a polymeric film cover and an insert of gas deodorizing material. The film cover also has an aperture and opposite ends of the insert overlie the two apertures.
Abstract: Antiinflammatory activity is exhibited by steroids having the structural formula ##STR1## or a 1,2-dihydro derivative thereof, wherein R is alkyl;R.sub.1 is hydrogen, alkyl, alkenyl, alkynyl, or aryl;R.sub.2 is carbonyl or .beta.-hydroxymethylene;R.sub.3 is hydrogen or halogen; andR.sub.4 is hydrogen, methyl or fluorine.
Abstract: 3-Isocyanato-2-oxo-1-azetidinesulfonic acid salts are novel intermediates which are useful in processes for the preparation of 3-amino-2-oxo-1-azetidinesulfonic acid salts and 3-acylamino-2-oxo-1-azetidinesulfonic acid salts.
Abstract: A controller for a two-directional air pump, of the type used in performing medical experiments is described. The controller includes a level sensing apparatus which is used to initiate an electric signal which controls a pneumatic solenoid which toggles the two-directional pump. Using the apparatus, the Doluisio technique may be performed automatically.
Type:
Grant
Filed:
March 16, 1982
Date of Patent:
November 13, 1984
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Wing-Sun Chow, Richard W. Walton, Donna A. D'Stefan