Abstract: Shelf stable tablets containing fosinopril sodium are prepared by employing either sodium stearyl fumarate or hydrogenated vegetable oil as the lubricant. The tablets can contain conventional excipients such as fillers, binders, and disintegrants as well as an optional diuretic.
Type:
Grant
Filed:
June 26, 1990
Date of Patent:
April 9, 1991
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Robert L. Jerzewski, Thomas M. Wong, Lewis J. Gryziewicz, Nemichand B. Jain, Ajit B. Thakur
Abstract: In accordance with the present invention a novel composite compression and support dressing is disclosed. This dressing comprises an extensible bandage having a stretchable hydrocolloid adhesive composition laminated thereto.
Abstract: Novel compounds of the formula ##STR1## and tautomers thereof are disclosed. These compounds possess potassium channel blocking activity and, as such, are useful as antiarrhythmic agents.
Abstract: A method of manufacturing a bag for containing liquid, the bag provided with an outlet tube. The method entails seam welding the outlet tube between two superposed bag walls, placing the bag and tube combination between the blocks of a mold, each block having confronting recesses of a particular shape and then injecting molding plastic material to fill these recesses. The injected material forms a collar which completely surrounds the tube and adjacent bag material. The bag film material on either side of the tube is melted to itself and to the tube wall and the collar is thereby securely attached in an encircling configuration thereby to preclude leakage. The tube may be a part of tap or other outlet fitting such as a push pull tap.
Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R.sup.1, R.sup.2 and R.sup.3 are independently selected from:(1) alkyl,(2) substituted alkyl in which one or more substituents are selected from(a) halogen,(b) hydroxyl,(c) alkoxy,(d) alkoxycarbonyl,(e) acyloxy,(f) cycloalkyl,(g) phenyl,(h) substituted phenyl in which one or more substituents are X or Y,(i) alkyl-S(O).sub.n,(j) cycloalkyl-S(O).sub.n,(k) phenyl-S(O).sub.n,(l) substituted phenyl-S(O).sub.n in which one or more substituents are X or Y, and(m) oxo,(3) alkoxy,(4) alkenyl,(5) cycloalkyl,(6) substituted cycloalkyl in which one or more substituents are selected from(a) alkyl,(b) substituted alkyl in which one or more substituents are selected from(i) halogen,(ii) hydroxy,(iii) alkoxy,(iv) alkoxycarbonyl(v) acyloxy(vi) phenyl(vii) substituted phenyl in which one or more substituents are X and Y,(viii) alkyl-S(O).sub.n,(ix) cycloalkyl-S(O).sub.
Abstract: An optically active amine compound and a method for preparing same are provided which compound has the structure ##STR1## in the form of its R-(+) enantiomer or S-(-) enantiomer, wherein R and R.sup.1 are independently H, lower alkyl or halogen, R.sup.2 is H or lower alkyl and R.sup.3 is lower alkyl, the optically active amine is useful in the optical resolution of DL-3-acylthio-2-methylpropanoic acid wherein acyl is acetyl or benzoyl. The optically active D-(+)-3-acylthio-2-methylpropanoic acids are used as intermediated for preparing antihypertensive agents, such as captopril.
Type:
Grant
Filed:
January 15, 1988
Date of Patent:
March 19, 1991
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Patrick A. MacManus, Peter Walsh, Adrian J. Kilbane
Abstract: A bagside coupling for an ostomy bag is intended to cooperate with a filter cartridge. Inserting the filter cartridge in a suitable recess results in establishing connection between the interior of the bag and the exterior. Escaping gases are constrained to pass through filter material in the filter cartridge.
Type:
Grant
Filed:
December 11, 1989
Date of Patent:
January 22, 1991
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Peter L. Steer, Neil P. Wiltshire, David J. Auld
Abstract: A method is provided for preparing D(-)-.beta.-hydroxyisobutyric acid by fermentation employing the method and/or ethyl esters of isobutyric acid, the methyl and/or ethyl esters of methacrylic acid, isobutyl isobutyrate and/or isobutyl methacrylate as the substrate and a microorganism of the genus Candida and other fungi. In an alternative method, the isolated cells of the various microorganisms are employed with one or mixtures of the above substrates.
Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is an N-heterocyclic group as defined herein and Y can be --NH--, --O-- or --CH.sub.2 --, are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
Abstract: An improved process for making compounds having the formula ##STR1## includes subjecting an intermediate of the formula ##STR2## to hydrogenolysis in the presence of a ketonic solvent so as to simultaneously remove both Z-protecting groups from compound II while selectively reprotecting the --A.sub.1 --NH.sub.
Type:
Grant
Filed:
September 26, 1989
Date of Patent:
December 25, 1990
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Jollie D. Godfrey, Jr., Richard H. Mueller, Robert Zahler
Abstract: A new process for preparing [1S-[1.alpha.,2.alpha.(Z),-3.alpha.,4.alpha.]]-7-[3-[[[ (1-oxoheptyl)amino]acetyl]amino]-methyl]-7-oxabicyclo[2,2,1]hept-2-yl]-5-h eptenoic acid. New intermediates are also described. [1S-(1.alpha.,2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amino ]acetyl]amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid is useful in the treatment of thrombotic disease.
Abstract: 7-Oxabicycloheptane imidazole prostaglandin analogs are provided which are useful in treating thrombotic and vasospastic disease and have the structural formula ##STR1## wherein m is 0, 1, 2, 3 or 4; n is 1, 2 or 3; and p is 1, 2 or 3; Z is --CH.dbd.CH--, --CH.sub.2 CH.sub.2 -- or ##STR2## wherein Y is 1 or a single bond; R is CO.sub.2 H, CO.sub.2 lower alkyl, CO.sub.2 alkali metal, CONHSO.sub.2 R.sub.2 (wherein R.sub.2 is lower alkyl or aryl) or --CH.sub.2 -5-tetrazolyl; A is CHOH, C.dbd.O, ##STR3## (wherein R.sub.3 is H or lower alkyl), or a single bond; R.sub.1 is lower alkyl, aryl, cycloalkyl or H, R.sub.1 can be H only when A is a single bond.
Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, which is (S)-1-[6-amino-2-[[hydroxy-(4-phenylbutyl)phosphenyl]oxy]-1-oxohexyl]-L-pr oline, fosinopril or zofenopril, alone or in combination with an antidepressant drug such as lithium, over a prolonged period of treatment.
Abstract: In accordance with the present invention a novel oral composition and method of using same for the treatment of ulcers and other gastrointestinal disorders is disclosed. The composition comprises an agent capable of forming an ulcer-adherent protective complex in an acid environment combined with one or more alkaline materials in a total amount sufficient to substantially prevent the formation of such a complex in the mouth and adherence of such a complex to the buccal mucosa.
Type:
Grant
Filed:
January 30, 1989
Date of Patent:
December 4, 1990
Assignee:
E. R. Squibb & Sons, Inc.
Inventors:
Richard J. Harwood, Edward V. Henry, Joseph S. Sonk, Luke T. H. Foo, Jay L. Rheingold, Robert C. deGroof
Abstract: p-Aminophenols are provided having the structure ##STR1## wherein m is 0, 1 or 2; n is 0, 1, 2 or 3; R.sup.1 and R.sup.2 may be the same or different and are H, hydroxy or alkoxy; R.sup.3 is H, lower alkyl, alkanoyl or aroyl and R.sup.4 is H, lower alkyl or alkanoyl, and including acid-addition salts thereof.These compounds are useful as inhibitors of leukotriene production and as such are useful as antiallergy, anti-inflammatory and anti-psoriatic agents.
Abstract: A method is provided for improving post-ischemic myocardial function such as contractile dysfunction or reperfusion injury by administering a thromboxane receptor antagonist which is a 7-oxabicycloheptane substituted diamide prostaglandin analog in combination with a thrombolytic agent before, during or immediately after an ischemic attack.
Abstract: Novel thromboxane receptor antagonists are disclosed, having the formula ##STR1## wherein: A is aryl, optionally substituted withhalogen,lower alkoxy,carboalkoxy,lower alkyl,alkylamino, orphenyl;X is --CH.sub.2 or --NH;R.sub.1 is COOH, COO-alkali metal (such as Na, K, or Li), COO-lower alkyl, CONHSO.sub.2 R.sub.2, or 5-tetrazolyl;R.sub.2 is lower alkyl or aryl;m is 0, 1, or 2; andp is 2, 3, 4 or 5.Also disclosed are novel intermediates of formula I compounds.
Abstract: An ostomy coupling has a first channel shaped element for attachment to an ostomy bag and a second element for attachment to a pad of medical grade adhesive. Each of these elements surrounds a stomal orifice. The second element is made into parts. The first attaches to the pad and the second is slidable axially relative to the first part. Moreover, the second part has a flange under which fingers can be placed when joining the elements to substantially prevent the application of pressure to the peristomal area.
Abstract: A process has now been discovered by which an intermediate in preparation of antibiotics ##STR1## may be directly derived from the substrate ##STR2## by treatment with aqueous solutions of MHCO.sub.3 and MOH, wherein: R.sup.1, R.sup.2 and R.sup.3 are each independently alkyl, alkenyl, alkynyl, substituted alkyl, substituted alkenyl, substituted alkynyl, aryl, or substituted aryl;M is alkali metal (such as Na, Li, or K); andX is halogen.
Abstract: 3,5-Dihydroxypentanoic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-thiazolidine derivatives and have the structure ##STR1## wherein Z is ##STR2## R.sup.6 is an alkali metal, lower alkyl or H; R.sup.1 and R.sup.2 are the same or different and are H, lower alkyl or aryl;X is S, O, ##STR3## or a single bond; R.sup.7 is lower alkyl; R.sup.3 is lower alkyl or aryl; R.sup.4 and R.sup.5 are the same or different and are H or lower alkyl; and represents a single bond or a double bond, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, novel intermediates for use in preparing the above mevinic acid derivatives are also provided.