Patents Assigned to E. R. Squibb & Sons
  • Phosphonate substituted amino acids useful as antihypertensives
    Patent number: 5102875
    Abstract: Hypotensive activity is exhibited by new phosphonate substituted amino or imino acids of the formula ##STR1## isomeric mixtures thereof and pharmaceutically acceptable salts thereof, wherein:X is an imino or amino acid of the formula ##STR2##
    Type: Grant
    Filed: June 25, 1990
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Dihydropyrimidine lactone derivatives
    Patent number: 5103006
    Abstract: Novel compounds of the formula ##STR1## wherein X is sulfur or oxygen, R.sub.2 is aryl or heterocyclo and R.sub.1 is as defined herein, are disclosed. Compounds of formula I possess calcium channel activating activity.
    Type: Grant
    Filed: August 21, 1990
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: George C. Rovnyak, Spencer D. Kimball
  • Process for preparing 3-alkenylidene-1,1-bisphosphonates
    Patent number: 5103036
    Abstract: A process is provided for preparing a 3-alkenylidene-1,1-bisphosphonate which is an intermediate for preparing an inhibitor of the enzyme squalene synthetase which is useful as an inhibitor of cholesterol biosynthesis, or which bisphosphonate itself is useful as an inhibitor of cholesterol biosynthesis. The process involves the palladium catalyzed coupling of an allylic ester with a tetraester of a methylenebisphosphonate to form a 3-alkenylidene-1,1-bisphosphonate containing an alkene moiety located .gamma., .delta. to the phosphonates.
    Type: Grant
    Filed: May 13, 1991
    Date of Patent: April 7, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David R. Magnin, Richard B. Sulsky
  • 7-oxabicycloheptyl substituted heterocyclic amide or ester prostaglandin analogs useful in the treatment of thrombotic and vasospastic disease
    Patent number: 5100889
    Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs useful in treating thrombotic and vasopastic 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 0, if Z is ##STR3## then Y cannot be O, and Z is --CH.dbd.CH--, n is 1, 2, 3 or 4; and when Y=vinyl, n=0; R is CO.sub.2 H, CO.sub.2 lower alkyl, CH.sub.2 OH, CO.sub.2 alkali metal, CONHSOR.sup.3, 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: June 18, 1990
    Date of Patent: March 31, 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
  • Mevinic acid derivatives useful as antihypercholesterolemic agents and method for preparing same
    Patent number: 5099035
    Abstract: Mevinic acid derivatives are provided which are 6-hydroxy-8-(2,2-dimethyl-1-oxybutoxy-2-methyl)-substituted-decahydronapht halene 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: March 1, 1991
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jeffrey O. Saunders, Eric M. Gordon
  • Method for preventing or inhibiting loss of cognitive function employing a combination of an ace inhibitor and a drug that acts at serotonin receptors
    Patent number: 5098889
    Abstract: A method is provided for imhibiting loss of cognitive functon, including memory, which may or may not be associated with Alzheimer's disease, by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts as serotonin receptors such as zacopride, over a prolonged period of treatment.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Brenda Costall, Zola P. Horovitz
  • Diol sulfonamide and sulfinyl renin inhibitors
    Patent number: 5098924
    Abstract: Compounds of the formula ##STR1## wherein Z is SO or SO.sub.2 possess renin inhibition activity and are useful in treating hypertension and other diseases where the reduction of the levels of circulating angiotensin II are beneficial.
    Type: Grant
    Filed: September 15, 1989
    Date of Patent: March 24, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Michael A. Poss
  • 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
  • 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
  • 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
  • Pouch with mounting member for removable adhesive filter
    Patent number: 5085652
    Abstract: An annular mounting member is bonded to the pouch wall to define a vent opening. The mounting member is made of material which is compatable with the pouch film and has a smooth exterior surface adapted to facilitate removable mounting of an adhesive coated element in alignment with the opening. The element may be a deodorizing filter assembly including a filter disk surrounded by an annular border member coated with pressure sensitive adhesive or a gas impermeable cover member designed to close the vent.
    Type: Grant
    Filed: June 16, 1989
    Date of Patent: February 4, 1992
    Assignee: E. R. Squibb & Sons
    Inventors: Kenneth A. Johnsen, Frank Freeman
  • 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
  • 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
  • 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