Patents by Inventor Donald S. Karanewsky

Donald S. Karanewsky has filed for patents to protect the following inventions. This listing includes patent applications that are pending as well as patents that have already been granted by the United States Patent and Trademark Office (USPTO).

  • Patent number: 5157134
    Abstract: Dihydroxyheptonic acids containing an oxabicycloheptane nucleus are provided which have the structure ##STR1## including all stereoisomers thereof, wherein Z is ##STR2## and X, R.sub.1, R.sub.2 and R.sub.3 are as defined herein.
    Type: Grant
    Filed: March 12, 1992
    Date of Patent: October 20, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 5124453
    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: January 28, 1991
    Date of Patent: June 23, 1992
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • 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
  • 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
  • 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
  • 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
  • Patent number: 5017716
    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, lower alkoxy or lower alkyl; R.sup.x is H or alkyl;X is --O-- or --NH--;n is 1 or 2Z 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: December 1, 1989
    Date of Patent: May 21, 1991
    Assignee: E.R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Scott A. Biller, Eric M. Gordon
  • Patent number: 4910198
    Abstract: The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
    Type: Grant
    Filed: May 26, 1989
    Date of Patent: March 20, 1990
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, Donald S. Karanewsky
  • Patent number: 4904646
    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, lower alkoxy or lower alkyl; R.sup.x is H or alkyl;X is --O-- or --NH--;n is 1 or 2Z 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 27, 1990
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Scott A. Biller, Eric M. Gordon
  • Patent number: 4873356
    Abstract: A method is provided for preparing phosphinic acid compounds, which are useful in preparing certain angiotensin converting enzyme inhibitors, which have the formula ##STR1## wherein R.sub.1 is lower alkyl, aryl, arylalkyl, cycloalkyl or cycloalkylalkyl;R.sub.2 is hydrogen, lower alkyl or arylalkyl;X is hydrogen, lower alkyl or phenyl;Y is hydrogen, lower alkyl, phenyl or alkoxy, or together X and Y are --(CH.sub.2).sub.2 --, --(CH.sub.2).sub.3 --, --CH.dbd.CH--, or ##STR2## and n is 0 or 1including salts thereof and stereoisomers thereof, which method includes the steps of reacting a phosphinic acid ester of the structure ##STR3## wherein R.sub.
    Type: Grant
    Filed: September 30, 1987
    Date of Patent: October 10, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Edward W. Petrillo, Jr., Donald S. Karanewsky, John K. Thottathil, James E. Heikes, John A. Grosso
  • Patent number: 4855426
    Abstract: The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
    Type: Grant
    Filed: April 14, 1988
    Date of Patent: August 8, 1989
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, Donald S. Karanewsky
  • Patent number: 4849414
    Abstract: Compounds of the formula ##STR1## wherein X is various amino or imino acids and esters are disclosed. These compounds are useful as anti-hypertensive 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: May 20, 1987
    Date of Patent: July 18, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Melanie J. Loots, Donald S. Karanewsky
  • Patent number: 4804770
    Abstract: A process is provided for preparing the keto-phosphonate ##STR1## in enantiomerically homogeneous form, by reacting the anhydride ##STR2## with S-.alpha.-methylbenzylamine to effect diastereoselective opening of the anhydride to give a mixture of amides ##STR3## separating the amides, for example, by frictional crystallization, and converting the desired amide IVA (which is obtained in high yield from the anhydride) to enantiomerically homogeneous ketophosphonate in high yield and on a large scale.The so-formed ketophosphonate is useful in the synthesis of compactin as well as 7-substituted-(3,5-dihydroxy)-hept-6-enoic and -heptanoic acid HMG-CoA reductase inhibitors.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: February 14, 1989
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 4761413
    Abstract: The synthesis of epoxybenzazepin compounds is described. The novel compounds have anti-ulcer activity.
    Type: Grant
    Filed: December 22, 1986
    Date of Patent: August 2, 1988
    Assignee: Ortho Pharmaceutical Corporation
    Inventors: Michael P. Wachter, Donald S. Karanewsky
  • Patent number: 4745196
    Abstract: This invention is directed to orally active antihypertensive agents of the formula ##STR1## wherein R.sub.1 is certain alkyl or aralkyl groups.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: May 17, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • 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
  • Patent number: 4716155
    Abstract: Phosphorus containing compounds of the formula ##STR1## wherein X is a substituted or unsubstituted imino or amino acid and A is ##STR2## These compounds possess angiotensin converting enzyme activity and are thus useful as hypertensive agents.
    Type: Grant
    Filed: January 25, 1985
    Date of Patent: December 29, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4711884
    Abstract: This invention is directed to compounds of the formula ##STR1## wherein X is a thiazine or thiazepine of the formula ##STR2## These compounds possess angiotensin converting enzyme inhibition activity and are thus useful as hypotensive agents.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: December 8, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: Donald S. Karanewsky
  • Patent number: 4703043
    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 27, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4686298
    Abstract: Compounds of the formula ##STR1## are useful in the preparation of .alpha.-acyloxy phosphonate compounds. The final products are useful as anti-hypertensive agents due to their angiotensin converting enzyme inhibition activity.
    Type: Grant
    Filed: February 4, 1987
    Date of Patent: August 11, 1987
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Tamara Dejneka