Patents Assigned to E. R. Squibb & Sons
  • Bis protected (hydroxymethyl)cyclobutanols
    Patent number: 5185459
    Abstract: Cyclobutanols of the formula ##STR1## wherein P is a hydroxy protecting group are useful intermediates in the preparation of antiviral compounds.
    Type: Grant
    Filed: May 26, 1992
    Date of Patent: February 9, 1993
    Assignee: E. R. Squibb & Sons Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Process for the preparation of an antiviral agent
    Patent number: 5185463
    Abstract: Racemic Feist's acid is treated with (R)-(+)-.alpha.-methylbenzylamine to yield (1R-trans)-3-methylenecyclopropane-1,2-dicarboxylic acid, (R)-.alpha.-methylbenzylamine (1:1) salt. This salt can then be converted to (1R-trans)-3-methylene-1,2-cyclopropanedicarboxylic acid, dimethyl ester which is an intermediate in the preparation of the antiviral agent [1R-(1.alpha.,2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-1,9-dihydro-6H-pur in-6-one. The improved process also enables the recovery of racemic Feist's acid from the resolution.
    Type: Grant
    Filed: October 2, 1991
    Date of Patent: February 9, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Richard H. Mueller, Thomas P. Kissick, Janak Singh
  • Boronic acid adducts of metal dioxime complexes useful in labelling proteins and other amine-containing compounds
    Patent number: 5183653
    Abstract: Boronic acid adducts of metal dioxime complexes are useful as reagents for labeling proteins and other amine-containing compounds.
    Type: Grant
    Filed: April 13, 1990
    Date of Patent: February 2, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karen E. Linder, Adrian D. Nunn, Kondareddiar Ramalingam
  • Pravastatin pharmaceuatical compositions having good stability
    Patent number: 5180589
    Abstract: A pharmaceutical composition is provided which has excellent stability, when dispersed in water has a pH of at least about 9, and includes a medicament which is sensitive to a low pH environment such as pravastatin, one or more fillers such as lactose and/or microcrystalline cellulose, one or more binders, such as microcrystalline cellulose (dry binder) or polyvinylpyrrolidone (wet binder), one or more disintegrating agents such as croscarmellose sodium, one or more lubricants such as magnesium stearate and one or more basifying agents such as magnesium oxide.
    Type: Grant
    Filed: May 20, 1991
    Date of Patent: January 19, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Yatindra M. Joshi, Pierina Chiesa, Nemichand B. Jain
  • Ostomy bag coupling
    Patent number: 5178615
    Abstract: An ostomy bag coupling appliance has body side and bag side couplings each including a seal means. The bag side coupling includes one ring like member carrying the seal means associated with a locking ring which can be rotated relative to the member. The locking ring and the body side coupling have interengaging parts whereby upon relative rotational movement (about the axis of the coupling) these cooperating parts can be engaged and disengaged so locking together, or allowing to be released, as the case may be, the body side and bag side couplings.
    Type: Grant
    Filed: June 13, 1989
    Date of Patent: January 12, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Peter L. Steer, Neil P. Wiltshire
  • 6-.alpha.-hydroxy derivatives of mevinic acids
    Patent number: 5177104
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts thereof have been found to possess activity as cell-selective HMG-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula, ##STR2## R.sup.1 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; and R.sup.2 is hydrogen, alkyl, ammonium, or alkali metal.
    Type: Grant
    Filed: April 3, 1990
    Date of Patent: January 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Sam T. Chao, Eric M. Gordon
  • Method for preparing a phosphonic acid ester
    Patent number: 5177239
    Abstract: A method is provided for preparing a phosphonic acid ester having the structure ##STR1## wherein R.sup.1 is farnesyl or a derivative or analog thereof, and R.sup.2 is lower alkyl, by treating a farnesyl halide R.sup.1 Hal(Hal.dbd.Cl,Br,I) with an alkoxide of the structure ##STR2## wherein M is an alkali metal and R.sup.2c is lower alkyl. The resulting phosphonic acid ester is an intermediate in preparing a squalene synthetase inhibitor which is used for inhibiting cholesterol biosynthesis.
    Type: Grant
    Filed: July 17, 1989
    Date of Patent: January 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Richard H. Mueller
  • Enzymatic resolution process
    Patent number: 5177006
    Abstract: A novel enzymatic resolution process for preparing resolved compounds of the formula ##STR1## with improved yields and high optical purity is disclosed. Compounds of formula I' are useful, for example, as intermediates for the preparation of physiologically active compounds, e.g. captopril, zofenopril and endopeptidase inhibitor.
    Type: Grant
    Filed: July 2, 1991
    Date of Patent: January 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey M. Howell, Ramesh N. Patel, Laszlo J. Szarka
  • Acyl amidine and acyl, guanidine substituted biphenyl derivatives
    Patent number: 5177097
    Abstract: Novel compounds are disclosed having the formula ##STR1## and wherein R.sub.1, R.sub.2 and R.sub.3 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
    Type: Grant
    Filed: July 24, 1991
    Date of Patent: January 5, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Mevinic acid derivatives
    Patent number: 5173487
    Abstract: Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, is exhibited by a compound of the formula ##STR1## m is 0 to 3; R is selected from:(1) alkyl;(2) substituted alkyl;(3) alkoxy;(4) alkenyl;(5) cycloalkyl;(6) phenyl; and(7) substituted aryl; andR.sup.1 and R.sup.2 are as defined in the specification.
    Type: Grant
    Filed: November 13, 1989
    Date of Patent: December 22, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Buoyant controlled release powder formulation
    Patent number: 5169638
    Abstract: A buoyant controlled release pharmaceutical powder formulation is provided which may be filled into capsules and 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. and excipients.
    Type: Grant
    Filed: October 23, 1991
    Date of Patent: December 8, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Andrew Dennis, Peter Timmins, Kevin Lee
  • Catheter attachment device
    Patent number: 5167639
    Abstract: A catheter attachment device comprises a first pad of medical grade adhesive having one surface covered by a removable protective layer, a second surface covered by a plastics film, and, attached to the film, a second pad of medical grade adhesive. A surface of this second pad which faces away from the first pad is covered by a removable protective layer and has a plastics film on its other surface. The two plastics films are attached to each other over a central region substantially smaller in area than the areas of both the first and second pads.
    Type: Grant
    Filed: June 22, 1990
    Date of Patent: December 1, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Keith G. M. Hollands, Graham E. Steer
  • Method for preventing onset of restenosis after angioplasty employing an ace inhibitor
    Patent number: 5166143
    Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering an ACE inhibitor such as fosinopril or ceranapril, prior to, during and/or after angioplasty.
    Type: Grant
    Filed: June 13, 1991
    Date of Patent: November 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Miguel A. Ondetti, A. K. Gunnar Aberg, Patricia Ferrer
  • Process of making isoprenoid phosphinylformic acid squalene synthetase inhibitors
    Patent number: 5166386
    Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H;R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 --wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: November 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Scott A. Biller
  • Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same
    Patent number: 5166364
    Abstract: Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy- 2-methyl)-substituted-decahydronaphthalene esters and have the structure ##STR1## wherein Z is ##STR2## wherein R is alkali metal such as Na, or H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis, and also as antifungal agents.In addition, a method for preparing the above-mevinic acid derivatives is also provided.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: November 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Peptifluorin and neopeptifluorin
    Patent number: 5165931
    Abstract: Two related, novel antibiotic substances, peptifluorin and neopeptifluorin, are prepared by cultivation of strains of Pseudomonas fluorescens, A. T. C. C. No. 53,958 and A. T. C. C. No. 55,129, respectively.
    Type: Grant
    Filed: March 28, 1991
    Date of Patent: November 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward Meyers, Wen-Chih Liu, Gordon W. Robinson
  • Benzodiazolo analogs
    Patent number: 5164509
    Abstract: Novel potassium channel activators of the formula ##STR1## where Y, X, X.sub.1, X.sub.2 (N or O), and R.sub.1 -R.sub.4 are as defined herein, are disclosed.
    Type: Grant
    Filed: November 26, 1990
    Date of Patent: November 17, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Intermediates for purinyl and pyrimidinyl tetrahydrofurans
    Patent number: 5164520
    Abstract: Intermediate for the preparation of antiviral compounds having the formula ##STR1## wherein R.sub.1 is a purine or pyrimidine base or an analog thereof.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: November 17, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, Joseph A. Tino
  • Process for the direct chromatographic analysis of drugs and metabolites in whole blood samples using internal surface reverse phase technology
    Patent number: 5164090
    Abstract: Disclosed herein is a process for separation and analysis of free and bound hydrophobic components in whole blood. In this process, whole blood is passed through an internal surface reverse phase material having particles large enough to allow blood cells to pass through. These particles have hydrophobic pores that are small enough to prevent penetration by proteinaceous substances and large enough to allow penetration by free hydrophobic components. Thus, free hydrophobic components are retained by the internal pore surfaces. A non-denaturing solvent is used to wash the whole blood through the material, and a hydrophobic or organic solvent may be separately used to wash the hydrophobic components from the material. This process may be combined with qualitative, quantitative, and selective detection techniques, such as radiolabelling.
    Type: Grant
    Filed: November 6, 1989
    Date of Patent: November 17, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Walter W. Hirth
  • Combination of a calcium channel blocker and thromboxane A.sub.2 receptor antagonist or synthetase inhibitor and method for treating ischemia employing such combination
    Patent number: H1139
    Abstract: A method is provided for treating ischemia in a mammalian species by administering a combination of a calcium channel blocker such as diltiazem, SQ 31,765 or SQ 32,324 and a thromoboxane A.sub.2 receptor antagonist such as SQ 30,741 or a thromboxane synthetase inhibitor such as dazoxiben.
    Type: Grant
    Filed: July 21, 1988
    Date of Patent: February 2, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Gary J. Grover