Patents Assigned to E. R. Squibb & Sons
  • Preparation of boronic acid derivatives
    Patent number: 5039795
    Abstract: An improved process for preparation of compounds of the formula ##STR1## as disclosed. These compounds are useful as intermediates in the preparation of boronic acid adducts of technetium 99m dioxime complexes of the formula.sup.99m Tc X(Y).sub.3 Zwhich are useful as imaging agents.
    Type: Grant
    Filed: June 21, 1989
    Date of Patent: August 13, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Richard H. Mueller
  • 6,7-dihydroxyquinoxalines as intermediates to beta-lactam antibiotics
    Patent number: 5037983
    Abstract: Compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof and possessing antibacterial activiy, and intermediates to compounds of formula I having the formula ##STR2##
    Type: Grant
    Filed: December 1, 1989
    Date of Patent: August 6, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Peter H. Ermann
  • Method for inhibiting loss of cognitive functions employing a calcium channel blocker alone or in combination with an ACE inhibitor
    Patent number: 5037821
    Abstract: A method is provided for inhibiting loss of cognitive function, including memory, which may or may not be associated with Alzheimer's disease, in a mammalian species by administering a benzazepine-type or a pyrimidine-type calcium channel blocker such as diltiazem, SQ 31,765, SQ 32,324, SQ 33,351, SQ 33,537 or SQ 32,547 alone or in combination with an ACE inhibitor, such as captopril or SQ 29,852, over a prolonged period of treatment.
    Type: Grant
    Filed: March 27, 1989
    Date of Patent: August 6, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Zola P. Horovitz
  • Method for preventing or treating depression employing a combination of an ace inhibitor and a drug that acts at serotonin receptors
    Patent number: 5032578
    Abstract: A method is provided for inhibiting onset of or treating depression by administering an ACE inhibitor, such as captopril, fosinopril, zofenopril or ceranapril in combination with a drug that acts at serotonin receptors such as zacopride, over a prolonged period of treatment.
    Type: Grant
    Filed: September 17, 1990
    Date of Patent: July 16, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Zola P. Horovitz
  • Monobactam hydrazides containing catechol sulfonic acid groups
    Patent number: 5030724
    Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof. 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.Y.sub.1 and Y.sub.2 are either hydrogen or OR.sub.11 but are not the same.R.sub.11 is hydrogen, alkanoyl of from one to ten carbon atoms, substituted alkanoyl of from two to ten carbon atoms, phenylcarbonyl, (substituted phenyl) carbonyl, heteroarylcarbonyl, phenylalkanoyl, (substituted phenyl) alkanoyl, or heteroarylalkanoyl.
    Type: Grant
    Filed: January 22, 1990
    Date of Patent: July 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Joseph E. Sundeen, Robert Zahler, Stefan Jendrzejewski
  • Combination and method for treating obsessive-compulsive disorder, and motor and phonic tics in Tourettes' syndrome using such combination
    Patent number: 5030648
    Abstract: A new combination of drugs is provided which is formed of an angiotensin converting enzyme inhibitor such as ceranapril or captopril, and a dopaminergic receptor blocker which is preferably pimozide and a method for treating obsessive-compulsive disorder and also motor and phonic tics in Tourettes' syndrome using such combinations.
    Type: Grant
    Filed: January 12, 1990
    Date of Patent: July 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Abraham Sudilovsky
  • Pharmaceutical compositions having good stability
    Patent number: 5030447
    Abstract: A pharmaceutical compositions 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 mirocrystalline 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: March 31, 1988
    Date of Patent: July 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Yatindra M. Joshi, Pierina Chiesa, Nemichand B. Jain
  • Clamping systems for two piece ostomy device
    Patent number: 5026360
    Abstract: To minimize trauma after surgery, a clamp is employed to sealingly engage specially configured coupling rings mounted on the adhesive faceplate and the collection pouch, respectively. Each of the coupling rings includes a radially extending annular projection. The circular clamp is designed to surround the coupling rings and receive the projections within an annular recess. The projections and recess have oppositely oriented camming surfaces which cooperates to draw the coupling rings toward each other as the clamp is tightened. The clamp is locked by a toggle clasp connected by a living hinge, a pin and socket arrangement, a serrated clasp or a change purse type clasp. An adaptor can be employed so that the clamp can be used with a pouch with a conventionally configured coupling ring.
    Type: Grant
    Filed: September 18, 1990
    Date of Patent: June 25, 1991
    Assignee: E. R. Squibb & Sons
    Inventors: Kenneth A. Johnsen, Walter F. Leise, Jr.
  • Process for direct isolation of captopril
    Patent number: 5026873
    Abstract: A process is disclosed for direct isolation of captopril from a substrate of the formula ##STR1## wherein R is lower alkyl or lower alkoxy. In this process, the substrate is first treated with an aqueous alkali metal hydroxide capable of forming a water-soluble salt of the substrate, wherein the alkali metal hydroxide has a concentration of 4M or greater. The substrate is then neutralized, preferably with a mineral acid. By this process, captopril may be directly crystallized from an aqueous solution, avoiding the prior art use of organic solvents and zinc treatment to reduce levels of sulfide and disulfide impurities, respectively. In an alternative embodiment, neutralization is carried out by use of a hydrogen-supplying ion exchange resin.
    Type: Grant
    Filed: November 6, 1989
    Date of Patent: June 25, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Neal G. Anderson, David A. Lust, Barbara J. Bennett, Alan F. Feldman, Robert E. Polomski
  • Isoprenoid phosphinylformic acid squalene synthetase inhibitors
    Patent number: 5025003
    Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthetis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- orR.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, 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.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.
    Type: Grant
    Filed: September 18, 1989
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Scott A. Biller
  • Phosphorus-containing HMG-CoA reductase inhibitor compounds
    Patent number: 5025000
    Abstract: Compounds which are useful as inhibitors of cholesterol biosynthesis and thus as hypocholesterolemic agents are provided which have the structure ##STR1## including salts thereof, wherein R is OH, or lower alkoxy;R.sup.x is H or alkyl;X is --(CH.sub.2).sub.a -- (where a is 1, 2 or 3), --CH.dbd.CH--, or --C.tbd.C--.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: March 2, 1990
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Seco-mevinic acid derivatives useful as antihypercholesterolemic agents and new intermediates
    Patent number: 5025017
    Abstract: Seco-mevinic acid derivatives are provided which has 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: September 28, 1989
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Dactylocycline A and dactylocycline B
    Patent number: 5024839
    Abstract: Cultivation of a strain of the microorganism Dactylosporangium sp. A.T.C.C. No. 53693, yields the antibiotic substance EM5586 which contains the novel useful components dactylocycline A and dactylocycline B.
    Type: Grant
    Filed: December 24, 1987
    Date of Patent: June 18, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Carol A. Aklonis, Helen A. Ax, Donald R. Kirsch, Joseph O'Sullivan, Adrienne Tymiak, J. Scott Wells
  • Method for inhibiting loss of cognitive functions employing an ace inhibitor
    Patent number: 5015633
    Abstract: A method is provided for inhibiting loss of cognitive function, including memory, which may or may not be associated with Alzhemier's disease, in a mammalian species by administering an ACE inhibitor, which is a phosphonate substituted amino or imino acid or salt, such as SQ 29,852 over a prolonged period of treatment.
    Type: Grant
    Filed: February 9, 1989
    Date of Patent: May 14, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Abraham Sudilovsky
  • Ester substituted aminoalkanoylureido amino and imino acid and ester compounds
    Patent number: 5013861
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as intermediates in the preparation of pharmaceutically active products.
    Type: Grant
    Filed: October 6, 1986
    Date of Patent: May 7, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Aryl cyanoguanidines: potassium channel activators and method of making same
    Patent number: 5011837
    Abstract: Novel compounds of the formula ##STR1## and tautomers thereof, wherein at least one of R.sub.2, R.sub.3 and R.sub.4 is a strong electron withdrawing group, are disclosed. These compounds possess potassium channel activating activity and, as such, are useful as antihypertensive agents. Advantageously, the compounds of the present invention have shown less cardiac effects than known potassium channel activators.Also disclosed is a process for preparing these and other compounds.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: April 30, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Karnail Atwal, John R. McCullough, Gary J. Grover
  • Starch containing film ostomy pouches
    Patent number: 5009648
    Abstract: Biodegradable composite films comprising a starch containing blended polymeric film and a barrier material coated or laminated to the blended film. The use of such composite films in ostomy pouches and other medical products is described. Also described is an ostomy pouch construction in which an adhesive label is affixed to the pouch so as to reduce the escape of odor from the stomal aperture.
    Type: Grant
    Filed: March 22, 1989
    Date of Patent: April 23, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Marvin S. Aronoff, Denis E. Keyes, Robert C. Hahn, Sr.
  • Diastereoselective preparation of phosphinate esters
    Patent number: 5008399
    Abstract: An increase in the disastereoselectivity resulting from the reaction of a phosphinic acid ester of the formula ##STR1## with the halo ester of the formula ##STR2## is achieved by carrying out the reaction in the presence of 4-methylmorpholine, diazabicyclooctane, quinuclidine, 1-methylpyrolidine, or cinchonidine. After removal of the R.sub.3 protecting group and fractional crystallization, the resulting desired diastereomeric pair can be resolved, and the desired isomer can be coupled to 4-substituted L-proline to give compounds possessing angiotensin converting enzyme inhibition activity. In particular, the process is useful in producing the antihypertensive agent fosinopril sodium in increased yields.
    Type: Grant
    Filed: January 19, 1990
    Date of Patent: April 16, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Thomas C. Sedergran
  • Method of reducing pre- and post-ischemic myocardial arrhythmias and fibrillation
    Patent number: 5008284
    Abstract: Zofenopril, fosinopril, (S)-1-[6-amino-2-[[hydroxy(4-phenylbutyl)phosphinyl]oxy]-1-oxohexyl]-L-pro line or a pharmaceutically acceptable salt thereof alone or in combination with a thrombolytic, antiarrhythmic, or antifibrillatory agent is employed to reduce pre- and post-ischemic myocardial arrhythmias and fibrillations as well as reducing arrhythmias associated with congestive heart failure.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: April 16, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gary J. Grover, James L. Bergey
  • Arylthioalkylphenyl carboxylic acids, derivatives thereof, compositions containing same and method of use
    Patent number: 5006542
    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## where 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 vasopastic diseases.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: April 9, 1991
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Philip D. Stein