Patents Assigned to E. R. Squibb & Sons, Inc.
  • Process of preparing captopril
    Patent number: 5097043
    Abstract: An optically active amine compound and a method for preparing same are provided which compound has the structure ##STR1## in the form of its R-(+) enantiomer or S-(-) enantiomer, wherein R and R.sup.1 are independently H, lower alkyl or halogen, R.sup.2 is H or lower alkyl and R.sup.3 is lower alkyl, the optically active amine is useful in the optical resolution of DL-3-acylthio-2-methylpropanoic acid wherein acyl is acetyl or benzoyl. The optically active D-(+)-3-acylthio-2-methylpropanoic acids are used as intermediates for preparing antihypertensive agents, such as captopril.
    Type: Grant
    Filed: November 5, 1990
    Date of Patent: March 17, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Patrick A. MacManus, Peter Walsh, Adrian J. Kilbane
  • Method for preparing isoprenoid cyclopropane 1,1-dicarboxylates and derivatives thereof and novel intermediates
    Patent number: 5095136
    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 27, 1990
    Date of Patent: March 10, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Cornelia Forster
  • Method for treating addiction to a drug of abuse employing an ACE inhibitor
    Patent number: 5093129
    Abstract: A method is provided for treating addiction to a drug of abuse such as nicotine, cocaine or diazepam, by inhibiting appetitie or desire for such drug by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or SQ 29,852, alone or in combination with a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.
    Type: Grant
    Filed: January 30, 1989
    Date of Patent: March 3, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Zola P. Horovitz, Abraham Sudilovsky
  • Phosphorus-containing HMG-CoA reductase inhibitors, new intermediates and method
    Patent number: 5091378
    Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesteroleumic agents are provided which have the structure ##STR1## wherein R is OH, or salts thereof or lower alkoxy; R.sup.x is H or alkyl;X is --CH.sub.2 --, --CH.sub.2 --CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C--, --CH.sub.2 CH.sub.2 CH.sub.2 -- or --CH.sub.2 O-- (where O is linked to Z);Z is a hydrophobic anchor, such as ##STR2## wherein the dotted lines represent optional double bonds. New intermediates used in preparing the above compounds, pharmaceutical compositions containing such compounds and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: April 18, 1988
    Date of Patent: February 25, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Michael C. Badia, Scott A. Biller, Eric M. Gordon, Michael J. Sofia
  • Method for preventing or treating anxiety employing a calcium channel blocker
    Patent number: 5089502
    Abstract: A method is provided for inhibiting onset of or treating anxiety by administering a calcium channel blocker such as diltiazem or nifedipine, over a prolonged period of treatment.
    Type: Grant
    Filed: August 9, 1990
    Date of Patent: February 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Abraham Sudilovsky, Zola P. Horovitz
  • Fluorinated derivatives of mevinic acids
    Patent number: 5089523
    Abstract: Compounds of the formula ##STR1## and pharmaceutically acceptable salts and tautomeric mixtures thereof possess activity as HMg-CoA reductase inhibitors, thus making them useful as antihypercholesterolemic agents. In the above formula,Z is ##STR2## R.sup.1 and R.sup.2 are each independently fluoro or hydrogen, except that at least one of R.sup.1 and R.sup.2 is fluoro;R.sup.3 is hydrogen, alkyl, cycloalkyl, aryl or arylalkyl; andR.sup.4 is hydrogen, alkyl, ammonium, alkylammonium, or alkali metal.
    Type: Grant
    Filed: May 11, 1990
    Date of Patent: February 18, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ravi K. Varma, Sam T. Chao
  • Microbiological hydrolysis for the preparation of (exo,exo)-7-oxabicyclo(2.2.1) heptane-2,3, monoacyl ester dimethanol
    Patent number: 5084387
    Abstract: Disclosed herein is a process for preparing a novel monoester of the formula ##STR1## in which the associated novel diester ##STR2## is hydrolyzed in the presence of one or more water-soluble enzymes or microorganisms capable of selectively hydrolyzing the --O--C(O)--R.sup.1 group, wherein the treatment is carried out in a biphasic solvent system comprising an aqueous phase having the enzymes or microorganisms and an organic phase immiscible in water having the diester. Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino]m ethyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using this enzymatic/microbial process.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: January 28, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ramesh N. Patel, Laszlo J. Szarka, John K. Thottathil, David Kronenthal
  • Process for preparing (3R-(3a.alpha.,4.beta.,7.beta..beta.,7a.alpha.))-octahydro-4,7 epoxyisobenzofuranol from associated aldehydes
    Patent number: 5084581
    Abstract: Disclosed herein is a novel process in which novel aldehydes ##STR1## and the trans isomer thereof are hydrolyzed by treatment with an alkali metal carbonate, bicarbonate or hydroxide and water to form the cis enantiomer ##STR2## Also disclosed is a process for preparing [1S-[1.alpha., 2.alpha.(Z), 3.alpha., 4.alpha.]]-7-[3[[[[(1-oxoheptyl)amino]acetyl]-amino ]methyl-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid using the above process.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: January 28, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Kronenthal, John K. Thottathil
  • Gram-positive and gram-negative antibacterial compounds from the microorganism, Janthinobacterium lividum
    Patent number: 5081225
    Abstract: A novel antibiotic substance, janthinocin, is prepared by cultivation of a strain of the microorganism Janthinobacterium lividum, ATCC No. 53,857.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: January 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph O'Sullivan, John E. McCullough, Janice H. Del Mar
  • Process for preparing [1S-[1.alpha.,2.alpha.(Z),3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-ami no]acetyl]amino]methyl]-7-oxabicyclo-[2.2.1]hept-2-yl]-5-heptenoic acid
    Patent number: 5081266
    Abstract: A new process for preparing [1S-[1.alpha.,2.alpha.(Z),-3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amin o]acetyl]amino]methyl]-7-oxabicyclo [2.2.1]-hept-2-yl]-5-heptenoic acid. New intermediates are also described. [1S-(1.alpha.,2.alpha.(9Z),3.alpha.,4.alpha.]]-7-[3-[[[[(1-oxoheptyl)-amin o]acetyl]amino]methyl]-7-oxabicyclo[2.2.1]hept-2-yl]-5-heptenoic acid is useful in the treatment of thrombotic disease.
    Type: Grant
    Filed: September 26, 1990
    Date of Patent: January 14, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Monobactam hydrazides containing catechol sulfonic acid groups
    Patent number: 5077432
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.3 and R.sub.4 are the same or different and each is hydrogen or alkyl or R.sub.3 and R.sub.4 taken together with the nitrogen atoms to which they are attached form a 1,2-diazacyclobutane, 1,2-diazacyclopentane, 1,2-diazacyclohexane, or 1,2-diazacycloheptane ring and Y, and Y.sub.2 are either hydrogen or hydroxy but are not the same; are useful chemical intermediates for the preparation of .beta.-lactam antibiotics.
    Type: Grant
    Filed: February 7, 1991
    Date of Patent: December 31, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Robert Zahler, Stefan Jendrzejewski
  • Occlusive attaching device for ostomy appliance
    Patent number: 5074852
    Abstract: Occlusive attaching means comprising a first relatively thick adhesive component to be secured to the skin around the stoma and a relatively thin flexible second adhesive component to be secured to the skin at a distance from the stoma. Both adhesive components include an occlusive adhesive layer formulated as a blend containing one or more water soluble or swellable hydrocolloids dispersed in polyisobutylene along with other optional ingredients. The attaching means can be utilized as part of a one or two-piece ostomy system.
    Type: Grant
    Filed: August 16, 1989
    Date of Patent: December 24, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frank S. Castellana, Thomas A. Iliadis, Walter F. Leise, Keith T. Ferguson
  • Ostomy bag including a multiple layer filter
    Patent number: 5074851
    Abstract: A bag or pouch for receiving discharge from the human body is made of two superposed sheets of synthetic plastics material joined around their edges and has a filter attached to an upper part of an interior surface of one of the walls, there being a hole or slit in the wall to allow gases exiting the filter to pass to the exterior of the bag or pouch, and an intervening wall is included to separate the filter region from the remainder of the interior of the bag or pouch, said wall being characterized by having a series of scattered holes therein, there being from 100 to 300 holes per square inch (155000 to 465000 holes per square meter) and each hole having a maximum dimension of from 130 to 340 microns.
    Type: Grant
    Filed: July 3, 1990
    Date of Patent: December 24, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Ronald A. Plass, Gerald T. Whiting, Peter L. Steer
  • Process for preparing highly substituted phenyls
    Patent number: 5072023
    Abstract: A process is described in which a lactone ##STR1## is reacted with an alkylester X.sup.1 --CH.sub.
    Type: Grant
    Filed: February 15, 1990
    Date of Patent: December 10, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jeffrey A. Robl
  • Boronic acid adducts of technetium-.sup.99m dioxime-imine complexes
    Patent number: 5069900
    Abstract: Boronic acid adducts of technetium-.sup.99m imine-dioxime complexes are useful for imaging the myocardium, hepatobiliary system, brain and blood pool in humans and other mammalian species.
    Type: Grant
    Filed: August 28, 1989
    Date of Patent: December 3, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karen E. Linder
  • Arylthioalkylphenyl carboxylic acids, derivatives thereof, compositions containing same method of use
    Patent number: 5070099
    Abstract: Arylthioalkylphenylcarboxylic acids are provided which have the structure ##STR1## wherein Ar represents an aryl group including phenyl or naphthyl which may or may not include one or more substituents, X is COOR where R is hydrogen, alkali metal, or lower alkyl, or X is 5-tetrazolyl or ##STR2## wherein R.sup.1 is lower alkyl or aryl, p is 1 to 5, and m is 1 to 4. These compounds are cardiovascular agents which exhibit thromboxane antagonist activity and thus are useful in the treatment of thrombotic and vasospastic diseases.
    Type: Grant
    Filed: February 4, 1991
    Date of Patent: December 3, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein
  • Pyranyl quinoline calcium channel blockers
    Patent number: 5070088
    Abstract: Novel calcium channel blockers having the formula ##STR1## wherein X is oxygen or sulfur and wherein R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6 are as defined herein, are disclosed. These compounds are useful, for example, as anti-ischemic agents.
    Type: Grant
    Filed: December 19, 1989
    Date of Patent: December 3, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Certain (2-carboxy or 2-propenoic or 2-carbonyl)-3-halo-4,5-dioxy pyridine intermediates and the corresponding 1,4-dihydro-4-pyridones)
    Patent number: 5068331
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, exhibit antibacterial activity wherein R is ##STR2##
    Type: Grant
    Filed: July 13, 1990
    Date of Patent: November 26, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Treuner
  • Method of preventing or reducing adverse reactions to protamine using a thromboxane A.sub.2 receptor antagonist
    Patent number: 5066480
    Abstract: A method is provided for preventing reducing or reversing adverse reactions, such as pulmonary hypertension produced when protamine interacts with heparin, by administering a thromboxane A.sub.2 receptor antagonist.
    Type: Grant
    Filed: April 11, 1988
    Date of Patent: November 19, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Martin L. Ogletree, William A. Schumacher, Gary J. Grover, Lawrence T. Friedhoff
  • Process for preparing an optically active cyclobutane nucleoside
    Patent number: 5064961
    Abstract: A process for the preparation of the optically active compound [IR-(1.alpha., 2.beta., 3.alpha.)]-2-amino-9-[2,3-bis(hydroxymethyl)cyclobutyl]-6H-purin-6-one, represented by the formula: ##STR1## and novel intermediates are described.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: November 12, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Toomas Mitt