Patents Assigned to E. R. Squibb & Sons, Inc.
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs
    Patent number: 5162352
    Abstract: 7-Oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs are provided which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists and have the structural formula ##STR1## wherein m is 1, 2 or 3, n is 1, 2, 3 or 4 and p is 2 to 18. These compounds are also useful in identifying thromboxane receptors in various tissue.
    Type: Grant
    Filed: August 22, 1991
    Date of Patent: November 10, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Martin L. Ogletree
  • Selective processes for fosinopril polymorphs
    Patent number: 5162543
    Abstract: Described herein is a process for selectively preparing and interconverting polymorph salts of fosinopril, an antihypertensive agent that inhibits angiotensin converting enzyme. Each polymorph is prepared by mixing an alkali metal carrier, fosinopril, water and a keto and/or hydroxylic solvent and isolating the polymorph formed from the reaction mixture. The less exothermic polymorph A is formed when the water makes up more than about 0.2% of the water and solvents; at about 0.2% or less, the more exothermic polymorph B is formed.
    Type: Grant
    Filed: February 16, 1990
    Date of Patent: November 10, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John A. Grosso
  • Captopril formulation providing increased duration of activity
    Patent number: 5158777
    Abstract: A formulation comprising captopril within an enteric or delayed release coated pH stable core combined with additional captopril that is available for immediate release following administration.
    Type: Grant
    Filed: August 16, 1991
    Date of Patent: October 27, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Abramowitz, Yatinda M. Joshi, Nemichand B. Jain
  • 10'-Desmethoxystreptonigrin
    Patent number: 5158960
    Abstract: 10'-Desmethoxystreptonigrin, obtainable by cultivation of a strain of Streptomyces albus, A.T.C.C. No. 55161, and salts, esters and amides thereof. The novel compounds have antitumor and antibiotic activity.
    Type: Grant
    Filed: May 24, 1991
    Date of Patent: October 27, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward Meyers, Terrence W. Doyle, Veeraswamy Manne, Wen-Chih Liu
  • 7-oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    Patent number: 5158967
    Abstract: 7-Oxabicycloheptyl substituted heterocyclic amide prostaglandin analogs are provided which are thromboxane A.sub.2 (TXA.sub.2) receptor antagonists or combined thromboxane A.sub.2 receptor antagonist/thromboxane synthetase inhibitors and have the structural formula ##STR1## wherein R is SO.sub.3 H, P(O)OR.sup.3 OH or P(O)R.sup.4 OH, X is O or NH, and Z, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined herein.
    Type: Grant
    Filed: June 12, 1991
    Date of Patent: October 27, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Dihydroxyheptanoic acids containing an oxabicycloheptane nucleus useful as antihypercholesterolemic agents
    Patent number: 5157134
    Abstract: Dihydroxyheptonic acids containing an oxabicycloheptane nucleus are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## and X, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
    Type: Grant
    Filed: March 12, 1992
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Bisphosphonate squalene synthetase inhibitors and method
    Patent number: 5157027
    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## and analogs thereof, wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, a metal ion or a prodrug ester;R.sup.5 is H, halogen or lower alkyl;Zq is substituted alkenyl, substituted alkynyl, mixed alkenyl-alkynyl or substituted phenylalkyl or, phenylalkenyl or phenylalkynyl, or alkyl, including all stereoisomers thereof.New methods for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, David R. Magnin
  • Method for lowering serum cholesterol employing a phosphorus containing ACE inhibitor alone or in combination with a cholesterol lowering drug
    Patent number: 5157025
    Abstract: A method is provided for lowering serum cholesterol and thereby inhibiting fatty streak lesions of atherosclerosis by administering to a patient a phosphorus-containing ACE inhibitor, such as fosinopril or ceronapril, alone or in combination with a cholesterol lowering drug, such as pravastatin.
    Type: Grant
    Filed: April 1, 1991
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: A. K. Gunnar Aberg, Mark Kowala, Patricia Ferrer