Patents Represented by Attorney Lawrence S. Levinson
  • Patent number: 4740508
    Abstract: Compounds of the formula ##STR1## are disclosed. These compounds are useful as hypotensive agents due to their angiotensin converting enzyme inhibition activity and depending upon the definition of X may also be useful as analgesics due to their enkephalinase inhibition activity.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: April 26, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Harold N. Weller, III, Eric M. Gordon
  • Patent number: 4740332
    Abstract: A process is provided for preparing phosphonous acids of the structure wherein R.sub.1 is lower alkyl or arylalkyl ##STR1## which are useful in preparing phosphinic and phosphonic acid ACE inhibitors, which process includes the steps of treating an olefin of the structure R.sub.1 --CH.dbd.CH.sub.2 wherein R.sub.2 is lower alkyl or arylalkyl with a phosphorus-containing reagent such as sodium hypophosphite or hypophosphorous acid in the presence of an organic alcohol solvent such as ethanol or methanol, and a radical initiator such as azobisisobutyronitrile, under acidic conditions, preferably at the reflux temperature of the organic solvent, to form the phosphonous acid without forming the alkyl ester.
    Type: Grant
    Filed: January 20, 1987
    Date of Patent: April 26, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4738978
    Abstract: Bisthioamide-7-oxabicycloheptane prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 lower alkyl or ##STR2## q is 1 to 12; and R.sup.1 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S-aryl-S-, arylalkyl-S-, ##STR3## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: November 10, 1986
    Date of Patent: April 19, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Masami Nakane, Joyce Reid
  • Patent number: 4735901
    Abstract: Candida albicans has been transformed by the insertion of a plasmid comprising a fragment of DNA from Candida albicans containing the intact ADE 2 gene.
    Type: Grant
    Filed: January 14, 1985
    Date of Patent: April 5, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Myra B. Kurtz, Donald R. Kirsch
  • Patent number: 4735795
    Abstract: New X-ray contrast agents are provided which are alkylammonium complexes of diatrizoic acid having the structure ##STR1## X-ray contrast medium containing the above X-ray contrast agent and a carrier therefor such as a liposome carrier, and a method for the X-ray visualization of body cavities and organs are also provided.
    Type: Grant
    Filed: September 7, 1984
    Date of Patent: April 5, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Malcolm L. Robinson, Frank Ridgway, Peter Timmins
  • Patent number: 4735962
    Abstract: 7-Thiabicycloheptane substituted diamide and congener prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 1 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH, ##STR2## wherein R.sup.3 and R.sup.4 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.3 and R.sup.4 being other than hydroxy and lower alkoxy; p is 1 to 4; Z is ##STR3## q is 1 to 12; R.sup.1 is H or lower alkyl; and R.sup.3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, ##STR4## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: October 6, 1986
    Date of Patent: April 5, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Masami Nakane
  • Patent number: 4736066
    Abstract: Intermediates of the formula ##STR1## are disclosed. These compounds are useful in preparing substituted peptide compounds which possess hypotensive and analgesic activity.
    Type: Grant
    Filed: May 25, 1984
    Date of Patent: April 5, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4734496
    Abstract: .beta.-Lactams having a sulfonic acid salt substituent in the 1-position, an acylamino substituent in the 3-position and an --NR.sub.2 R.sub.3 substituent in the 4-position wherein R.sub.2 and R.sub.3 are the same or different and each is ##STR1## or R.sub.2 and R.sub.3 together with the nitrogen atom to which they are attached are ##STR2## R.sub.4 is alkyl, aryl or arylalkyl; and R.sub.5 and R.sub.6 are the same or different and each is hydrogen, halogen, alkyl, alkoxy, alkylthio, alkoxycarbonyl, carboxyl or a carboxyl salt; have antibacterial activity.
    Type: Grant
    Filed: May 29, 1981
    Date of Patent: March 29, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Uwe D. Treuner, Theodor Denzel, Hermann Breuer
  • Patent number: 4734424
    Abstract: Bicycloheptane substituted amide prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 0 to 4; A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; Q is --CH.dbd.CH--, --CH.sub.2 --, ##STR2## or a single bond; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH, ##STR3## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; p is 1 to 4; R.sup.1 is H or lower alkyl; q is 1 to 12; R.sup.2 is H or lower alkyl; and R.sup.3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, lower alkyl-S-, aryl-S-, arylalkyl-S-, ##STR4## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.
    Type: Grant
    Filed: September 24, 1986
    Date of Patent: March 29, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Joyce Reid
  • Patent number: 4734425
    Abstract: 7-Oxabicycloheptane substituted hydroxamic acid prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --CH.sub.2 -CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt, --CH.sub.2 OH, ##STR2## wherein R.sup.4 and R.sup.5 are the same or different and are H, lower alkyl, hydroxy, lower alkoxy or aryl, at least one of R.sup.4 and R.sup.5 being other than hydroxy and lower alkoxy; q is 1 to 12, R.sup.1 is H or OH; R.sup.2 is OH or H, provided that one of R.sup.1 and R.sup.2 is OH and the other is H; and R.sup.3 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, ##STR3## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: October 17, 1986
    Date of Patent: March 29, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Masami Nakane, Joyce Reid
  • Patent number: 4734508
    Abstract: A process is provided for preparing 4-hydroxy-4-phenyl-proline derivatives of the structure ##STR1## wherein R.sub.1 is a nitrogen protecting group such as benzoyl, benzyloxycarbonyl, t-butoxycarbonyl, benzyl, benzhydryl, trityl, acetyl, trifluoromethylacetyl, sulfonamides, and the like and wherein X is OR.sub.2 and R.sub.2 is hydrogen or an acid protecting group such as lower alkyl, aryl-lower alkyl or a metal ion, such as Na or K, or X is NR.sub.3 R.sub.4 wherein R.sub.3 and R.sub.4 may be the same or different and are hydrogen, lower alkyl, aryl or arylalkyl, or R.sub.3 and R.sub.4 together with the nitrogen to which they are attached form a 5-, 6- or 7-membered ring. The process includes the steps of forming triphenylcerium [(C.sub.6 H.sub.5).sub.3 Ce], for example, by reacting cerium trichloride (CeCl.sub.3) with phenyllithium, and reacting the triphenylcerium with the keto acid ##STR2## in the presence of an inert organic solvent such as tetrahydrofuran.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: March 29, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4734426
    Abstract: 5,6-Epoxy-7-oxabicycloheptane substituted diamide prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --; n is 1 to 5; R is CO.sub.2 H, CO.sub.2 alkyl, CO.sub.2 alkali metal, CO.sub.2 polyhydroxyamine salt or ##STR2## q is 1 to 12; and R.sup.1 is H, lower alkyl, lower alkenyl, lower alkynyl, aryl, arylalkyl, lower alkoxy, aryloxy, arylalkyloxy, amino, alkylamino arylamino, arylalkylamino, ##STR3## (wherein n' is 0, 1 or 2), alkylaminoalkyl, arylaminoalkyl, arylalkylaminoalkyl, alkoxyalkyl, aryloxyalkyl or arylalkoxyalkyl.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: September 24, 1986
    Date of Patent: March 29, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jagabandhu Das
  • Patent number: 4728652
    Abstract: 1,4-Dihydropyrimidines of the formula ##STR1## wherein X is sulfur or oxygen and R.sub.4 is aryl or heterocyclo and disclosed. These compounds are useful as cardiovacular agents, particularly anti-hypertensive agents, due to their vasodilator activity.
    Type: Grant
    Filed: April 21, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Karnail Atwal
  • Patent number: 4728642
    Abstract: This invention is directed to an occlusive dressing useful for treating skin lesions and a granular material capable of interacting with wound exudate. Wounds emitting a large amount of fluid can be treated by first packing with the granular material and then covering the wound with the occlusive dressing.
    Type: Grant
    Filed: April 29, 1985
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John M. Pawelchak, Frank M. Freeman
  • Patent number: 4728670
    Abstract: Biphenyl hydroxamic acids are provided having the structure ##STR1## wherein m is 1 to 7, X is S, O or NH, R is H, lower alkyl, aryl, aralkyl or cycloalkyl and R.sup.1 is H, lower alkyl, aryl, aralkyl, cycloalkyl, alkanoyl or aroyl.These compounds are inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: June 4, 1986
    Date of Patent: March 1, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Martin F. Haslanger, Ravi K. Varma, Eric M. Gordon
  • Patent number: 4725440
    Abstract: An antifungal pastille formulation, preferably containing nystatin as the antifungal agent, is provided which is soft and smooth in texture and when dissolved slowly in the mouth does not cause irritation of and will not adhere to oral mucosa and yet distributes nystatin in sufficiently high saliva concentrations, throughout the oral cavity, for long enough periods of time so as to be particularly effective in the treatment of candidiasis in the oral cavity and esophagus. A method for treating candidiasis in the oral cavity and esophagus employing the antifungal pastille and a method for preparing a nystatin pastille formulation are also provided.
    Type: Grant
    Filed: May 24, 1984
    Date of Patent: February 16, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frank Ridgway, Michael D. Ward
  • Patent number: 4723951
    Abstract: An ostomy bag has a filter attached to it by a series of plural sequentially peelable adhesive annuli.
    Type: Grant
    Filed: June 19, 1986
    Date of Patent: February 9, 1988
    Assignee: Craig Medical Products Ltd.
    Inventor: Peter L. Steer
  • Patent number: 4722810
    Abstract: Mercaptoalkanoyl and acylmercaptoalkanoyl compounds of the formula ##STR1## wherein n is an integer from one to fifteen possess enkephalinase inhibition activity and are useful as analgesic agents.
    Type: Grant
    Filed: August 13, 1986
    Date of Patent: February 2, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Norma G. Delaney, Eric M. Gordon, Miguel A. Ondetti
  • Patent number: 4723002
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having an acylamino substituent in the 3-position and having an activating group in the 1-position of the formula ##STR1##
    Type: Grant
    Filed: April 28, 1986
    Date of Patent: February 2, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, Glenn A. Jacobs, William H. Koster, Robert Zahler
  • Patent number: 4721725
    Abstract: Aryl-cyclopenta- and arylcyclohexa[b]pyrrole derivatives are provided having the structure ##STR1## wherein n is 1 or 2; X is --OR.sup.1 or --NR.sup.2 R.sup.3 wherein R.sup.1 is H, lower alkyl, cycloalkyl, aryl, aralkyl or cycloalkylalkyl, and R.sup.2 and R.sup.3 may be the same or different and are H, lower alkyl, cycloalkyl, aryl, aralkyl or cycloalkylalkyl;Y is --OR.sup.4 or --NR.sup.5 R.sup.6 wherein R.sup.4 is H or lower alkyl, and R.sup.5 and R.sup.6 are the same or different and are H or lower alkyl; andZ is aryl.These compounds are useful in inhibiting the 5-lipoxygenation of arachadonic acid in RBL-1 cells and preventing leukotriene formation in macrophages and as such are useful as antiallergy agents and in treating inflammation and psoriasis.
    Type: Grant
    Filed: January 27, 1986
    Date of Patent: January 26, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Donald S. Karanewsky