Patents Assigned to E. R. Squibb & Sons, Inc.
  • Method for preparing isoprenoid cyclopropane 1,1-dicarboxylates
    Patent number: 5157146
    Abstract: A process is provided for preparing isoprenoid cyclopropane 1,1-dicarboxylates which are useful in preparing squalene synthetase inhibitors which inhibit cholesterol biosynthesis, and also useful in preparing pyrethrin insecticides.
    Type: Grant
    Filed: October 24, 1991
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Cornelia Forster
  • Derivatives of pravastatin and method of making the same
    Patent number: 5155229
    Abstract: Derivatives of pravastatin are provided which are useful in inhibiting cholesterol biosynthesis and in preparing radiolabeled compounds useful in the radioimmunoassay (RIA) of pravastatin and derivatives thereof. The pravastatin derivatives have the structure ##STR1## wherein R is hydroxy, lower alkylamine, arylamine, arylalkylamine or heterocyclic alkylamine such as histamine, tyramine, O-benzyltyramine, methyl tyrosinate as well as iodinated derivatives thereof.
    Type: Grant
    Filed: July 1, 1991
    Date of Patent: October 13, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard A. DiPietro, Jan-I Tu, Noor Z. Turabi
  • Phosphonate, phosphinate derivatives useful as antihypertensive agents
    Patent number: 5153347
    Abstract: Novel angiotensin II receptor antagonists of the formula ##STR1## wherein X, X.sub.1, X.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein, are disclosed. These compounds are useful, for example, in the treatment of hypertension, congestive heart failure and cardiac hypertrophy.
    Type: Grant
    Filed: January 31, 1991
    Date of Patent: October 6, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John E. Lloyd
  • 7-Oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    Patent number: 5153327
    Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasospastic disease have the structural formula ##STR1## wherein m is 1, 2 or 3; n is 1, 2, 3 or 4; Z is --(CH.sub.2).sub.2 --, --CH.dbd.CH-- or ##STR2## wherein Y is O, a single bond or vinyl, with the proviso that when n is O, if Z is ##STR3## then Y cannot be O, and when Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3 m CONHR.sup.3a or --CH.sub.2 -5-tetrazolyl, X is O, S or NH; and where R.sup.1, R.sup.2, R.sup.3 and R.sup.3a are as defined herein.
    Type: Grant
    Filed: October 10, 1991
    Date of Patent: October 6, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Raj N. Misra, Philip M. Sher, Philip D. Stein, Steven E. Hall, David Floyd, Joel C. Barrish
  • N-heterocyclic alcohol derivatives
    Patent number: 5151513
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is an N-heterocyclic group as defined herein, are disclosed. These compounds are inhibitors of renin and therefore useful as cardiovascular agents.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: September 29, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Denis E. Ryono
  • Method for purification of monoclonal antibodies
    Patent number: 5151504
    Abstract: An improved method for the purification of monoclonal antibodies using Protein G, whereby the monoclonal antibodies are eluted from the Protein G at alkaline pH.
    Type: Grant
    Filed: March 26, 1990
    Date of Patent: September 29, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Edward M. Croze
  • Method for solubilizing membrane receptor proteins
    Patent number: 5151502
    Abstract: A process for solubilizing membrane receptor proteins which includes exposing an outer membrane having the desired protein to an oxidizing agent, treating the membrane with a detergent and treating with an inhibitory material lowering agent. This method maintains the activity of the membrane proteins after solubilization.
    Type: Grant
    Filed: April 30, 1991
    Date of Patent: September 29, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Maria L. Webb, Hossain Monshizadegan
  • Pyrimidinyl tetrahydrofurans
    Patent number: 5145960
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein R.sub.1 is a pyrimidine base or an analog thereof and R.sub.2 and R.sub.3 are independently hydrogen, --PO.sub.3 H.sub.2 or ##STR2## wherein X.sub.7 is hydrogen, alkyl, substituted alkyl or aryl.
    Type: Grant
    Filed: August 7, 1991
    Date of Patent: September 8, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, Joseph A. Tino
  • [3S(Z)]-3-[[(2-amino-4- thiazolyl)[[2-(hydroxyamino)-2-oxoethoxy]imino]acetyl]amino]-2,2-dimethyl -4-oxo-1-azetidinyl sulfate
    Patent number: 5143913
    Abstract: The compound [3S(Z)]-3-[[(2-amino-4-thiazolyl)[[2-(hydroxyamino)-2-oxoethoxy]imino]acet yl]amino]-2,2-dimethyl-4-oxo-1-azetidinyl sulfate has gram-positive and gram-negative activity and good oral absorption.
    Type: Grant
    Filed: May 10, 1991
    Date of Patent: September 1, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, Joseph E. Sundeen
  • Method for preparing isoprenoid cyclopropane 1,1-dicarboxylates and derivatives thereof and novel intermediates
    Patent number: 5144080
    Abstract: A process is provided for preparing isoprenoid cyclopropane 1,1-dicarboxylates and derivatives thereof including the corresponding monocarboxylate, monocarboxylic acid and alcohol derivatives thereof, all of which are useful in preparing squalene synthetase inhibitors which inhibit cholesterol biosynthesis, and also useful in preparing pyrethrin insecticides.
    Type: Grant
    Filed: August 30, 1991
    Date of Patent: September 1, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Cornelia Forster
  • Dihydropyrimidine macrocyclic lactones useful as calcium antagonists and agonists
    Patent number: 5143915
    Abstract: A compound of the formula ##STR1## (symbols defined in the specification), its 3,4-dihydropyrimidine tautomer form and pharmaceutically acceptable salts thereof have calcium entry blocking activity. A process of preparation, pharmaceutical composition and method of using the compound to reduce blood pressure are also provided.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: September 1, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: George C. Rovnyak, Spencer D. Kimball
  • Monoclonal antibodies which bind thromboxane A2 receptor antagonists and diagnostic methods based thereon
    Patent number: 5141865
    Abstract: Monoclonal antibodies which bind thromboxane A2 receptor antagonists, hybrid cell lines which produce these monoclonal antibodies, and immunoassay methods for detecting thromboxane A2 receptor antagonists using these monoclonal antibodies.
    Type: Grant
    Filed: November 17, 1989
    Date of Patent: August 25, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward M. Croze, Jan-I Tu
  • Pyranyl cyanoguanidine derivatives
    Patent number: 5140031
    Abstract: Novel compounds having the formula ##STR1## wherein ##STR2## are disclosed. These compounds have potassium channel activating activity and are useful, for example, as cardiovascular agents, especially as antiischemic agents.
    Type: Grant
    Filed: February 27, 1991
    Date of Patent: August 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, Gary J. Grover, Kyoung S. Kim
  • Method for preventing onset of restenosis after angioplasty employing pravastatin
    Patent number: 5140012
    Abstract: A method is provided for preventing or reducing the risk of restenosis following angioplasty by administering pravastatin alone or in combination with an ACE inhibitor such as captopril or ceranapril, prior to, during and/or after angioplasty.
    Type: Grant
    Filed: May 31, 1990
    Date of Patent: August 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Mark E. McGovern, Miguel A. Ondetti, Henry Y. Pan
  • Tablet composition and method for problem pharmaceutical materials using citric acid
    Patent number: 5137730
    Abstract: In accordance with the present invention an improved tablet composition for drugs or active ingredients prone to poor tabletting properties is disclosed. The improved composition comprises a premixture, consisting essentially of between about 85 and 99.9 percent by weight of the active ingredient and between about 0.1 and 15 percent by weight of citric acid, and one or more other formulation ingredients added to premixture. The present invention also involves the process for making such compositions and products therefrom.
    Type: Grant
    Filed: May 28, 1991
    Date of Patent: August 11, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Andrew B. Dennis, Peter Timmins, Himadri Sen
  • Heterocyclic ketone prostaglandin analogs
    Patent number: 5135939
    Abstract: Prostaglandin analogs useful in treating thrombotic and vasospastic disease having the structural formula ##STR1## wherein: m is 1, 2, or 3;n is 0, 1, 2 or 3;R.sup.1 is hydrogen, alkyl, alkenyl, alkynyl, aralkyl, aryl cycloalkyl, cycloalkylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl, heteroaryl or heteroarylalkyl, each of R.sup.1 being unsubstituted or optionally substituted with alkyl, aryl, cycloalkyl, or cycloalkylalkyl;R.sup.2 is CO.sub.2 R CONHSO.sub.2 R.sup.3, CONHR.sup.4 ;R is hydrogen, alkyl, or alkali metal;X is O or NH;Y is --O--, a single bond or vinylene, except that Y cannot be --O--when n is O;Z is --CH.dbd.CH--, --(CH.sub.2).sub.2 --, or ##STR2## and the remaining symbols are as defined in the specification.
    Type: Grant
    Filed: January 28, 1991
    Date of Patent: August 4, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Raj N. Misra
  • Cyclobutane derivatives
    Patent number: 5130462
    Abstract: Cyclobutane derivatives of the formulas ##STR1## wherein P is a hydroxy protecting group and X is a leaving group are useful intermediates in the preparation of antiviral compounds.
    Type: Grant
    Filed: February 19, 1991
    Date of Patent: July 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler
  • Method for treating type II diabetes employing a cholesterol lowering drug
    Patent number: 5130333
    Abstract: A method is provided for preventing or reducing the risk of or treating Type II diabetes by administering a cholesterol lowering drug, such as pravastatin, alone or in combination with an ACE inhibitor, such as captopril, zofenopril, ceranapril, fosinopril, enalapril or lisinopril.
    Type: Grant
    Filed: October 19, 1990
    Date of Patent: July 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Henry Y. Pan, Michael Bergman
  • Enzymatic resolution process hydrolyzing thio-ester
    Patent number: 5128263
    Abstract: A novel enzymatic resolution process for preparing resolved compounds of the formula ##STR1## with improved yields and high optical purity is disclosed. The thioester bond of the compound is hydrolyzed and the hydrolyzed compound is separated from the unhydrolyzed. Compounds of formula I' are useful, for example, as intermediates for the preparation of physiologically active compounds, e.g. captopril and zofenopril.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: July 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey M. Howell, Ramesh N. Patel, Laszlo J. Szarka
  • Bis (hydroxymethyl) cyclobutyl triazolopyrimidines
    Patent number: 5126345
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts wherein R.sub.1 is ##STR2## R.sub.6 is hydrogen, alkyl, substituted alkyl, or aryl; and R.sub.7 and R.sub.
    Type: Grant
    Filed: February 8, 1991
    Date of Patent: June 30, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: William A. Slusarchyk, Robert Zahler