Patents Represented by Attorney Donald J. Barrack
  • Patent number: 4636560
    Abstract: Analgesic and hypotensive activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy, or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl, or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.
    Type: Grant
    Filed: November 16, 1984
    Date of Patent: January 13, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Eric M. Gordon, Norma G. Delaney
  • Patent number: 4633017
    Abstract: Processes for preparing the useful intermediates having the formula ##STR1## are disclosed herein, utilizing novel chemical compounds having the formula ##STR2##
    Type: Grant
    Filed: October 24, 1985
    Date of Patent: December 30, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard H. Mueller, Jakob-Matthias Drossard, Peter H. Ermann
  • Patent number: 4632985
    Abstract: Antibacterial activity is exhibited by 2-azetidinones activated in the 1-position with an --SO.sub.
    Type: Grant
    Filed: June 3, 1985
    Date of Patent: December 30, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: David Kronenthal
  • Patent number: 4625038
    Abstract: Disclosed herein are novel chemical intermediates having the formula ##STR1## wherein R.sub.1 is alkyl, cycloalkyl, aryl or arylalkyl.
    Type: Grant
    Filed: December 23, 1985
    Date of Patent: November 25, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4625022
    Abstract: The process of this invention provides for the conversion of amino acid amides having the formula ##STR1## to 3-amino-2-oxo-1-azetidinesulfonic acid salts having the formula ##STR2## wherein one of R.sub.2 and R.sub.3 is hydrogen and the other is hydrogen, alkyl, cycloalkyl, phenyl or substituted phenyl and M.sup..sym. is hydrogen or a cation.
    Type: Grant
    Filed: November 15, 1985
    Date of Patent: November 25, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David M. Floyd, Alan W. Fritz, Christopher M. Cimarusti
  • Patent number: 4610824
    Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: October 9, 1984
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Uwe D. Truner
  • Patent number: 4601904
    Abstract: Cultivation of a strain of the microorganism Pseudomonas cepacia which has been deposited in the American Type Culture Collection as A.T.C.C. No. 39277, yields novel antibiotic substances xylocandin A and xylocandin B having activity against yeasts and fungi.
    Type: Grant
    Filed: June 25, 1984
    Date of Patent: July 22, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward Meyers, Wen-Chih Liu, Richard B. Sykes
  • Patent number: 4600786
    Abstract: Cultivation of a strain of the microorganism Pseudomonas fluorescens A.T.C.C. No. 39502 yields a novel antibiotic substance 2,3-dihydroxy-N-[2-[(4-nitrophenyl)methyl]-4-oxo-3-oxetanyl]benzamide.
    Type: Grant
    Filed: November 23, 1983
    Date of Patent: July 15, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard B. Sykes, Adrienne Tymiak
  • Patent number: 4597951
    Abstract: Hydroxylapatite, a compound having the formulaM.sub.10 (PO.sub.4).sub.6 (OH).sub.2,wherein M is calcium, strontium, barium, lead, iron, sodium, potassium, zinc, cadmium, magnesium, aluminum or a rare earth metal, as a support medium for strontium-82 in a strontium-82/rubidium-82 parent-daughter radionuclide generator.
    Type: Grant
    Filed: August 16, 1984
    Date of Patent: July 1, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gerald P. Gennaro, Paul S. Haney
  • Patent number: 4594188
    Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.
    Type: Grant
    Filed: May 20, 1985
    Date of Patent: June 10, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Norma G. Delaney, Eric M. Gordon
  • Patent number: 4588828
    Abstract: Antimicrobial activity is exhibited by compounds having the formula ##STR1## wherein R.sub.1 is hydrogen or aryl;R.sub.2 is hydroxymethyl, carboxyaldehyde, propenalyl, 3-hydroxy-1-propenyl, or 3-hydroxy-1,2-epoxypropyl; andn is 2 and m is 1 or n is 3 and m is 0; with the proviso that if R.sub.1 is hydrogen, n is 2 and m is 1.
    Type: Grant
    Filed: August 23, 1984
    Date of Patent: May 13, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Gregory S. Bisacchi, William H. Koster
  • Patent number: 4588819
    Abstract: 4-Substituted proline derivatives having the formula ##STR1## can be prepared by reacting the compound having the formula ##STR2## with a compound having the formula ##STR3## to obtain a compound having the formula ##STR4## (a novel intermediate), alkylating that compound to obtain a compound having the formula ##STR5## (a novel intermediate), converting that compound to a compound having the formula ##STR6## (a novel intermediate), and oxidizing that compound to yield the desired proline having the formula ##STR7## wherein R.sub.1 is alkyl, cycloalkyl, aryl or arylalkyl, R.sub.1 ' is alkyl, cycloalkenyl, aryl or arylalkyl, R.sub.2 is alkyl, aryl, arylalkyl or cycloalkyl and R.sub.3 is hydrogen, alkyl, aryl, arylalkyl or cycloalkyl.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: May 13, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John K. Thottathil
  • Patent number: 4588588
    Abstract: A novel antifungal antibiotic which has been designated EM5487 is prepared by cultivating Lysobacter gummosus A.T.C.C. No. 39472 under submerged aerobic conditions in an aqueous nutrient medium containing an assimilable carbohydrate and nitrogen source.
    Type: Grant
    Filed: December 5, 1983
    Date of Patent: May 13, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward Meyers, Raymond Cooper
  • Patent number: 4587047
    Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.
    Type: Grant
    Filed: April 1, 1982
    Date of Patent: May 6, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
  • Patent number: 4587051
    Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: May 6, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: William H. Koster
  • Patent number: 4584131
    Abstract: Vasodilating activity is exhibited by compounds having the formula ##STR1## n is 2 or 3; X is oxygen or sulfur;R.sub.1 and R.sub.2 are each independently hydrogen alkyl, cycloalkyl, or allyl, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl;R.sub.3 is alkyl, alkoxy, halogen, trifluoromethyl, or nitro;R.sub.4 is hydrogen, halogen, trifluoromethyl, or nitro; andR.sub.5 and R.sub.6 are each independently alkyl or cycloalkyl or R.sub.5 and R.sub.6 together with the nitrogen atom to which they are attached are pyrrolidinyl, piperidinyl, or morpholinyl.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: April 22, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Floyd, John Krapcho
  • Patent number: 4581170
    Abstract: Processes for preparing the useful intermediates having the formula ##STR1## are disclosed herein, utilizing novel chemical compounds having the formula ##STR2##
    Type: Grant
    Filed: August 3, 1984
    Date of Patent: April 8, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Richard H. Mueller, Jakob-Matthias Drossard, Peter H. Ermann
  • Patent number: 4578474
    Abstract: Imido, amido and amino derivatives of mercaptoacyl prolines and pipecolic acids are useful for the treatment of hypertension.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: March 25, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John Krapcho, Peter C. Wade
  • Patent number: 4576749
    Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).
    Type: Grant
    Filed: April 13, 1984
    Date of Patent: March 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
  • Patent number: 4574153
    Abstract: Antibacterial activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein, R.sub.1 is an acyl group derived from a carboxylic acid;R.sub.2 is hydrogen, methoxy, or formamido ##STR2## and one of R.sub.3 and R'.sub.3 is hydrogen and the other is ##STR3## and R.sub.4 is hydrogen alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl.
    Type: Grant
    Filed: March 1, 1985
    Date of Patent: March 4, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David Kronenthal, Paula L. Kuester, William H. Koster