Patents Assigned to E. R. Squibb & Sons
  • Phosphorus-containing squalene synthetase inhibitors
    Patent number: 5212164
    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 m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; 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;and when m is o, X is other than S; and if m is o and X is 0, then n is 1, 2, 3 or 4; including all stereoisomers thereof.
    Type: Grant
    Filed: March 29, 1990
    Date of Patent: May 18, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Michael J. Sofia
  • Method for rehabilitating the vasorelaxant action of the coronary arteries impaired through atherosclerosis or hypercholesterolemia employing an ACE inhibitor
    Patent number: 5212165
    Abstract: A method is provided for rehabilitating or restoring the vasorelaxant action of the endothelium impaired by atherosclerosis and/or hypercholesterolemia, thereby preventing arteriospasm in the coronary arteries using an angiotensin converting enzyme inhibitor such as captopril, fosinopril, ceranapril, enalapril or lisinopril, which may be administered by oral or parenteral dosage forms.
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: May 18, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: A. K. Gunnar Aberg, Miguel A. Ondetti
  • Indole and benzimidazole-substituted dihydropyrimidine derivatives
    Patent number: 5212177
    Abstract: Novel compounds having the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and X are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore, for example, an antihypertensive agents.
    Type: Grant
    Filed: December 16, 1991
    Date of Patent: May 18, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Michael A. Poss, Karnail S. Atwal
  • Method for preparing a phosphonic acid ester
    Patent number: 5210262
    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=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: September 14, 1992
    Date of Patent: May 11, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Janak Singh, Richard H. Mueller
  • Indole- and benzimidazole-substituted imidazole derivatives
    Patent number: 5208235
    Abstract: Novel compounds having the formula ##STR1## where X R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are as defined herein. These compounds inhibit the action of angiotensin II and are useful, therefore for example, as antihypertensive agents.
    Type: Grant
    Filed: March 10, 1992
    Date of Patent: May 4, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Substituted imidazole phosphonic and phosphinic acid derivatives
    Patent number: 5208234
    Abstract: Novel compounds having the formula ##STR1## wherein 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: March 10, 1992
    Date of Patent: May 4, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • Hydroxymethyl (methylenecyclopentyl) purines and pyrimidines
    Patent number: 5206244
    Abstract: Antiviral activity is exhibited by compounds having the formula ##STR1## and its pharmaceutically acceptable salts.
    Type: Grant
    Filed: September 20, 1991
    Date of Patent: April 27, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, William A. Slusarchyk
  • Tetrahydroethanonaphthaleneamine derivatives
    Patent number: 5202486
    Abstract: Tetrahydronaphthaleneamine derivatives having the formula ##STR1## wherein R, R', R.sub.1 and R.sub.2 are as defined herein, are novel calcium channel blockers.
    Type: Grant
    Filed: July 31, 1990
    Date of Patent: April 13, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joel C. Barrish, Steven H. Spergel
  • 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
  • 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
  • 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
  • Ostomy device with improved coupling system
    Patent number: 5195996
    Abstract: In the first embodiment, the faceplate coupling ring is of conventional design and includes an axially extending rib with a radially outwardly extending rim and a radially inwardly extending deflectable sealing strip. The pouch coupling ring includes inner and outer spaced walls, forming a channel for receiving the rib. First and second protrusions extend inwardly from points on the interior surface of the walls proximate the ends thereof. The first protrusion cooperates with the rim and the second protrusion cooperates with the tip of the sealing strip, to securely retain the rib within the channel. The walls of the channel have reduced thickness and are easily deflectable as the rib is inserted into the channel, such that coupling of the rings is facilitated but decoupling requires the conventional amount of force due to the second protrusion.
    Type: Grant
    Filed: January 9, 1991
    Date of Patent: March 23, 1993
    Assignee: E. R. Squibb & Sons
    Inventors: John V. Edwards, Walter F. Leise, Jr., John B. Cline
  • 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
  • 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
  • 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