Patents Assigned to E. R. Squibb & Sons, Inc.
  • 2-thio or oxo-4-aryl or heterocyclo-1,5(2H)-pyrimidinedicarboxylic acid diesters and 3-acyl-5-pyrimidinecarboxylic acids and esters
    Patent number: 5202330
    Abstract: Pyrimidine compounds of the formula ##STR1## wherein X is sulfur or oxygen, Y is R.sub.11 or --O--R.sub.1, and R.sub.4 is aryl or heterocyclo are disclosed. These compounds are useful as cardiovascular agents, particularly anti-hypertensive agents, due to their calcium entry blocking vasodilator activity.
    Type: Grant
    Filed: January 5, 1987
    Date of Patent: April 13, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, George C. Rovnyak, Spencer D. Kimball
  • Phosphorus-containing HMG-CoA reductase inhibitors
    Patent number: 5202327
    Abstract: Novel phosphorus-containing compounds which inhibit the activity of HMG-CoA reductase, including a 5-pyrimidinyl-containing moiety. Pharmaceutical compositions and methods of use for the treatment or prevention of hypercholesterolemia, atheroschlerosis, hyperlipoproteinaemia and hyperlipidemia are provided.
    Type: Grant
    Filed: July 10, 1991
    Date of Patent: April 13, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jeffrey A. Robl
  • Method of diagnosing senile dementia of the Alzheimer type
    Patent number: 5200324
    Abstract: A method is provided for the screening of senile dementia of the Alzheimer type (Alzheimer's disease) by testing for an anomalous molecular form of acetylcholinesterase in cerebrospinal fluid of a patient.
    Type: Grant
    Filed: August 1, 1991
    Date of Patent: April 6, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Dasakumar S. Navaratnam, John D. Priddle, Brendon I. McDonald, A. David Smith, Kim A. Jobst
  • Optically active cyclobutane nucleoside and intermediates, therefor
    Patent number: 5198583
    Abstract: The optically active antiviral compound [1R-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)-cyclobutyl]-1,9-dihydro-6H-pu rin-6-one and novel intermediates useful in its preparation are described.
    Type: Grant
    Filed: October 3, 1991
    Date of Patent: March 30, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt
  • Dihydroxyheptanoic acids containing an oxabicycloheptane nucleus useful as antihypercholesterolemic agents
    Patent number: 5194634
    Abstract: Dihydroxyheptanoic acids containing an oxabicyloheptane 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: July 30, 1992
    Date of Patent: March 16, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Process and intermediates for beta-lactams having aminothiazole(iminooxyacetic acid)acetic acid sidechains
    Patent number: 5194604
    Abstract: Disclosed herein are processes for preparing a compound of the formula ##STR1## in which a novel compound of the formula ##STR2## is reacted with a beta lactam of the formula ##STR3## by treatment with a base, wherein the symbols are as defined in the specification.
    Type: Grant
    Filed: June 29, 1990
    Date of Patent: March 16, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Theodor Denzel, Christopher M. Cimarusti, Janak Singh, Richard H. Mueller
  • Method for preventing onset of or treating Type II diabetes employing a cholesterol lowering drug alone or in combination with an ace inhibitor
    Patent number: 5190970
    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 combintion with an ACE inhibitor, such as captopril, zofenopril, ceranapril, fosinopril, enalapril or lisinopril.
    Type: Grant
    Filed: December 20, 1991
    Date of Patent: March 2, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Henry Y. Pan, Michael Bergman
  • Imidazole and benzimidazole derivatives
    Patent number: 5191086
    Abstract: Novel angiotensin-II receptor antagonists are disclosed having the general formula ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, W and X are as defined herein.
    Type: Grant
    Filed: March 19, 1991
    Date of Patent: March 2, 1993
    Assignee: E.R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Benzoxazole and related heterocyclic substituted imidazole and benzimidazole derivatives
    Patent number: 5190942
    Abstract: Novel compounds are disclosed having the formula ##STR1## wherein X, Y, R.sub.1, R.sub.2, R.sub.3, R.sub.4, and R.sub.5 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, as antihypertensive agents.
    Type: Grant
    Filed: April 22, 1991
    Date of Patent: March 2, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates
    Patent number: 5189180
    Abstract: Seco-mevinic acid derivatives are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## R is H, alkali metal or lower alkyl, R.sup.1 is H, lower alkyl, aryl, lower alkoxy, cycloalkyl, heteroaryl, aralkyl, heteroaralkyl or heterocyclic; R.sup.2 is lower alkyl, cycloalkyl or aralkyl, and X is O or NR.sup.5 wherein R.sup.5 is H or lower alkyl, and are HMG CoA reductase inhibitors and thus are useful as antihypercholesterolemic agents and in treating atherosclerosis.New intermediates for preparing the above seco-mevinic acid derivatives are also provided.
    Type: Grant
    Filed: May 1, 1991
    Date of Patent: February 23, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Acylaminoalkanoyl urethanes or thiourethanes
    Patent number: 5187290
    Abstract: Compounds of the formula ##STR1## wherein Z is oxygen or sulfur are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inbitition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: September 29, 1986
    Date of Patent: February 16, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Eric M. Gordon
  • 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
  • Farnesyl-protein transferase assay for identifying compounds that block neoplastic transformation
    Patent number: 5185248
    Abstract: Assays for farnesyl-protein transferase (FT) which can be used to identify substances that block the farnesylation of ras oncogene products are described. Because farnesylation is required for ras oncogene activity, inhibitory compounds identified in the assays of the invention can block neoplastic transformation mediated by the ras oncogene. The assays of the invention are targeted for a step subsequent to the synthesis of farnesyl pyrophosphate (FPP), the donor of the farnesyl residue, and an intermediate in cholesterol synthesis and other important cellular pathways. Therefore, compounds which inhibit ras mediated transformation, yet do not cause major disruptions of important cell pathways that require FPP as an intermediate may be identified using the assays of the invention.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: February 9, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Mariano Barbacid, Veeraswamy Manne
  • 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
  • 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
  • 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