Patents Assigned to E. R. Squibb & Sons
  • 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: 4623729
    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: July 22, 1982
    Date of Patent: November 18, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4621092
    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: July 14, 1983
    Date of Patent: November 4, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Sesha I. Natarajan, Eric M. Gordon
  • Patent number: 4618583
    Abstract: A method is provided for preparing L-(+)-.beta.-hydroxyisobutyric acid by fermentation employing microorganisms of the species Pseudomonas aeruginosa and of the genus Protaminobacter such as of the species Protaminobacter alboflavus, and isobutyric acid and/or methacrylic acid and/or derivatives thereof as the substrate.
    Type: Grant
    Filed: November 19, 1984
    Date of Patent: October 21, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Robert S. Robison, Michael G. Doremus
  • Patent number: 4616088
    Abstract: Compounds of the formula ##STR1## wherein A is ##STR2## intervene in the conversion of angiotensinogen to angiotensin II by inhibiting renin and thus are useful as anti-hypertensive agents.
    Type: Grant
    Filed: December 14, 1984
    Date of Patent: October 7, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Denis E. Ryono, Edward W. Petrillo, Jr.
  • Patent number: 4616005
    Abstract: Phosphonyl hydroxyacyl amino acids of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid or ester. These compounds possess angiotensin converting enzyme activity and are thus useful as hypotensive agents.
    Type: Grant
    Filed: December 16, 1985
    Date of Patent: October 7, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4614825
    Abstract: 7-Oxabicycloheptane and 7-oxabicycloheptene prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombolytic disease.
    Type: Grant
    Filed: July 25, 1985
    Date of Patent: September 30, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: David L. Snitman, Martin F. Haslanger, Peter W. Sprague
  • Patent number: 4611005
    Abstract: 5,6-Epoxy-7-oxabicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## wherein m is 1 to 5, R is H, lower alkyl, alkali metal or polyhydroxylamine, and R.sup.1 is lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl or lower alkenyl, including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: May 21, 1985
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jagabandhu Das
  • Patent number: 4611007
    Abstract: 7-Oxabicycloheptane substituted prostaglandin analogs are provided having the structural formula ##STR1## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease and as inhibitors of 5-lipoxygenase enzyme.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jagabandhu Das
  • Patent number: 4610870
    Abstract: A controlled release pharmaceutical formulation which undergoes substantially or approaches zero order release of active drug is provided, preferably in the form of a coated tablet, containing a core portion from which medicament, such as procainamide hydrochloride, is slowly released over a controlled length of time. The core also includes one or more hydrocolloid gelling agents having a viscosity of within the range of from about 10,000 to about 200,000 centipoises in 2% solution at 20.degree. C., such as hydroxypropylmethyl cellulose and/or methyl cellulose, one or more non-swellable binders and/or wax binders (where the medicament and/or hydrocolloid gelling agents are non-compressible), one or more inert fillers or excipients, one or more lubricants, and optionally one or more anti-adherents such as silicon dioxide and water. The above-described core is coated with a pharmaceutical coating composition containing a hydrophobic polymer and a hydrophilic polymer.
    Type: Grant
    Filed: October 5, 1984
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Nemichand B. Jain, Linda P. Gertie, Edward M. Rudnic
  • 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: 4611006
    Abstract: 5,6-Epoxy-7-oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: June 28, 1985
    Date of Patent: September 9, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jagabandhu Das
  • Patent number: 4609671
    Abstract: 5-6-Epoxy-7-oxabicycloheptane substituted amino prostaglandin analogs are provided having the structural formula ##STR1## wherein A is CH.dbd.CH or (CH.sub.2).sub.2, m is 1 to 8, n is 0 to 5, R is H, lower alkyl, alkali metal or hydroxylamine salt, and R.sup.1 is lower alkyl, aryl, aralkyl, cycloalkyl, cycloalkylalkyl, lower alkenyl, lower alkoxy, aralkoxy or ##STR2## including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: June 27, 1985
    Date of Patent: September 2, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Jagabandhu Das
  • Patent number: 4608386
    Abstract: 7-Oxabicycloheptane substituted ether prostaglandin analogs are provided having the structural formula ##STR1## wherein X is O or ##STR2## and including all stereoisomers thereof. The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: April 26, 1985
    Date of Patent: August 26, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Steven E. Hall, Wen-Ching Han
  • Patent number: 4607049
    Abstract: 7-Oxabicycloheptane substituted thio prostaglandin analogs are provided having the structural formula ##STR1## wherein R is hydrogen, lower alkyl, alkali metal, or a polyhydroxylamine salt, R.sup.1 is hydrogen, lower alkyl, arylalkyl, aryl, cycloalkyl or cycloalkylalkyl, R.sup.2 is hydrogen or lower alkyl, A is --CH.dbd.CH-- or --(CH.sub.2).sub.2, n is 1 to 4, n' is 0, 1 or 2, q is 1 to 10 and m is 0 to 8, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease, and as such are useful in inhibiting platelet aggregation.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: August 19, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Steven E. Hall
  • Patent number: 4607048
    Abstract: 7-Oxabicycloheptane substituted aryl amino prostaglandin analogs are provided having the structural formula ##STR1## wherein A is --CH.dbd.CH-- or --(CH.sub.2).sub.2 --; m is 1 to 8; n is 1 to 5; R is H, lower alkyl, alkali metal or a polyhydroxyamino salt; R.sup.1 is H, lower alkyl, hydroxyalkyl or aryl; R.sup.2 is H, lower alkyl, aryl or cycloalkyl, R.sup.3 is substituted aryl wherein the aryl group (which may be phenyl or naphthyl) is substituted with one or two of the following groups: hydroxy, ##STR2## SR.sup.4, --CN, --NO.sub.2, ##STR3## wherein R.sup.4 and R.sup.5 may be the same or different and are H or lower alkyl, and including all stereoisomers thereof.The compounds are cardiovascular agents useful, for example, in the treatment of thrombotic disease.
    Type: Grant
    Filed: May 16, 1985
    Date of Patent: August 19, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Masami Nakane
  • Patent number: 4607053
    Abstract: Arylhydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy.These compound are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: April 4, 1985
    Date of Patent: August 19, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Martin F. Haslanger
  • Patent number: 4604407
    Abstract: Hydroxamates are provided having the structure ##STR1## wherein R.sup.1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkenyl, aralkyl, or ##STR2## wherein n is 1 to 4 and X is hydroxy, alkoxy, amino, C.sub.1 -C.sub.4 -alkylamino or C.sub.1 -C.sub.4 -dialkylamino.R.sup.2 is hydrogen or lower alkyl; andR.sup.3 is C.sub.1 -C.sub.20 alkyl or C.sub.3 -C.sub.20 alkenyl, aryl, aryl-alkyl, cycloalkyl, aryl-alkenyl, lower alkoxy, lower alkenyloxy, aryl-alkoxy or cycloalkyloxy, and m is 0 to 5. These compounds are useful as inhibitors of .DELTA..sup.5 -lipoxygenase and as such are useful as antiallergy agents.
    Type: Grant
    Filed: April 4, 1985
    Date of Patent: August 5, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Martin F. Haslanger, Donald S. Karanewsky
  • Patent number: 4604402
    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: March 30, 1984
    Date of Patent: August 5, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Jollie D. Godfrey, Jr., Eric M. Gordon, Sesha I. Natarajan
  • Patent number: 4602092
    Abstract: A method is provided for preparing phosphinic acid prodrug intermediates which are useful in preparing phosphinic acid angiotensin-converting enzyme inhibitors which method includes the step of coupling a phosphonous acid or its ester of the structure ##STR1## wherein R is H or lower alkyl and R.sup.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl, with an alkylating agent of the structure ##STR2## wherein Hal is Cl, Br or I, n is 0 or 1, R.sup.2 is H or lower alkyl, and Z is H, lower alkyl, --CO.sub.2 R.sup.3 (wherein R.sup.3 is H or lower alkyl), ##STR3## (wherein R.sup.4 is H, lower alkyl, aryl or arylalkyl), --CN, or ##STR4## (wherein R.sup.5 and R.sup.6 may be the same or different and are selected from the group consisting of H, lower alkyl, aryl, aryl-lower alkyl, cycloalkyl or cycloalkylalkyl and at least one of R.sup.5 and R.sup.6 is other than H, or R.sup.5 and R.sup.
    Type: Grant
    Filed: January 22, 1985
    Date of Patent: July 22, 1986
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: John K. Thottathil, Jerome L. Moniot