Patents Represented by Attorney Manfred Polk
  • Patent number: 4963525
    Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
    Type: Grant
    Filed: May 16, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix, A. J. Repta
  • Patent number: 4952587
    Abstract: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted circle represents one or two double bonds in any position in the 5-membered ring;X, Y and Z independently represent oxygen, sulphur, nitrogen or carbon, provided that at least one of X, Y and Z represents oxygen, sulphur or nitrogen;A represents a group of formula II: ##STR2## in which R.sup.1 represents hydrogen, hydroxy, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkoxy, hydroxy(C.sub.1-6)alkyl, halogen, amino, cyano, --CONR.sup.6 R.sup.7 or --SO.sub.2 NR.sup.6 R.sup.7, in which R.sup.6 and R.sup.7 independently represent hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.2-6 alkynyl;R.sup.2 represents hydrogen, halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy or C.sub.1-6 alkylcarbonyl;V represents nitrogen, ##STR3## and W represents oxygen, sulphur or ##STR4## in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.
    Type: Grant
    Filed: February 3, 1989
    Date of Patent: August 28, 1990
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, John Saunders, Christopher Swain
  • Patent number: 4925867
    Abstract: Compounds of formula (I) and pharmaceutically acceptable acid addition salts thereof: ##STR1## wherein R represents a hydrocarbon group, X represents oxygen or sulphur, and R and --NH.sub.2 are cis; are of use in the treatment and/or prevention of neurodegenerative disorders, and are also useful as anticonvulsant agents and muscle relaxants.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: May 15, 1990
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Paul D. Leeson, Tamara Ludduwahetty, Brian J. Williams
  • Patent number: 4919938
    Abstract: Oral dosage forms for neutral, zwitterions or slats of acidic or basic drugs with approximate zero order release kinetics comprise a core matrix of the drug, and a gelling polymer, the matrix being coated with a water permeable but insoluble polymer.
    Type: Grant
    Filed: October 4, 1989
    Date of Patent: April 24, 1990
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Claire J. Lovegrove, David A. Rawlins, Anthony J. Phillips, David A. Tainsh
  • Patent number: 4916230
    Abstract: This invention relates to a new one-step process for preparation of novel N-(acyloxyalkoxy)carbonyl derivatives useful as bioreversible prodrug moieties for drugs having a primary or secondary amine function thereon.
    Type: Grant
    Filed: July 2, 1984
    Date of Patent: April 10, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Patent number: 4906761
    Abstract: This invention provides the 4-mono-anion of myo-inositol orthoformate, and describes a process for preparing this anion as well as the use of this anion in the preparation of a variety of mono- and poly-phosphate derivatives of myo-inositol.
    Type: Grant
    Filed: June 28, 1988
    Date of Patent: March 6, 1990
    Assignee: Merck Sharpe & Dohme Ltd.
    Inventor: David C. Billington
  • Patent number: 4894169
    Abstract: This invention relates to a method of inhibiting deposition or precipitation of iron salts in aqueous systems which comprises adding a urea salt to said systems.
    Type: Grant
    Filed: October 13, 1988
    Date of Patent: January 16, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Mona Delitsky
  • Patent number: 4873263
    Abstract: The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: October 10, 1989
    Assignee: Merck & Co., Inc.
    Inventor: A. J. Repta
  • Patent number: 4872873
    Abstract: This invention relates to an improved controlled release bolus device wherein the improvement comprises attaching at the orifice a screen or insert which prevents blockage of the orifice by exogeneous materials, but does not vary the flow of medicament from the device.
    Type: Grant
    Filed: December 14, 1987
    Date of Patent: October 10, 1989
    Assignee: Merck & Co., Inc.
    Inventor: Joel R. Zingerman
  • Patent number: 4847250
    Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.
    Type: Grant
    Filed: July 18, 1988
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Takeru Higuchi
  • Patent number: 4847298
    Abstract: Acylcarnitine used as a nasal, buccal, sublingual and vaginal drug absorption enhancing vehicle for poorly absorbed drugs.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: July 11, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix, A. J. Repta
  • Patent number: 4835138
    Abstract: Choline esters are used as drug absorption enhancing agents for drugs which are poorly absorbed from the nasal, oral, and vaginal cavities.
    Type: Grant
    Filed: May 18, 1987
    Date of Patent: May 30, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, A. J. Repta, Joseph A. Fix
  • Patent number: 4822773
    Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
    Type: Grant
    Filed: December 20, 1987
    Date of Patent: April 18, 1989
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix
  • Patent number: 4780319
    Abstract: The invention relates to the use of carboxylic acids incorporated as a catalyst in poly(orthoester)s and other acid labile polymers such that upon exposure to aqueous environments the acid catalyzes the erosion of the polymer matrix. The rate of release of a drug substance incorporated into or surrounded by the poly(orthoester) or other acid labile polymer can be controlled in that the drug is released as the polymer is eroded in response to the catalytic action of the acid incorporated therein.
    Type: Grant
    Filed: April 3, 1987
    Date of Patent: October 25, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Gaylen M. Zentner, Kenneth J. Himmelstein, Stefano A. Pogany, Cheryl Ringeisen
  • Patent number: 4771073
    Abstract: The invention relates to compositions and methods of enhancing rectal absorption of L-dopa via the formation of an ester prodrug and optionally with a decarboxylase inhibitor.
    Type: Grant
    Filed: April 17, 1987
    Date of Patent: September 13, 1988
    Assignee: Merck & Co., Inc.
    Inventor: A. J. Repta
  • Patent number: 4767627
    Abstract: A drug delivery device retained in the stomach comprising a planar figure made from an erodible polymer that may release a drug associated therewith over a controlled, predictable and extended period of time.
    Type: Grant
    Filed: May 1, 1987
    Date of Patent: August 30, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Larry J. Caldwell, Colin R. Gardner, Robyn C. Cargill
  • Patent number: 4765973
    Abstract: The instant invention is directed to a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units.The instant invention is also directed to a controlled release device which comprises:(A) a polymer with at least one labile backbone bond per repeat unit and at least one pendant acid functionality per thousand repeat units; and(B) a beneficial substance incorporated within or surrounded by the matrix of said polymer.
    Type: Grant
    Filed: October 6, 1986
    Date of Patent: August 23, 1988
    Assignee: Merck & Co., Inc.
    Inventor: Jorge Heller
  • Patent number: 4762851
    Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.
    Type: Grant
    Filed: November 29, 1985
    Date of Patent: August 9, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Takeru Higuchi
  • Patent number: 4760057
    Abstract: This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regeneration of the parent amine drug of the carbamate prodrug moiety. The case also contains pharmaceutical composition, method of treatment and process claims.
    Type: Grant
    Filed: April 22, 1985
    Date of Patent: July 26, 1988
    Assignee: Merck & Co., Inc.
    Inventor: Jose Alexander
  • Patent number: 4758436
    Abstract: A drug delivery device retained in the stomach comprising a ring figure made from polymer(s) that may release a drug associated therewith over a controlled, predictable and extended period of time.
    Type: Grant
    Filed: May 7, 1987
    Date of Patent: July 19, 1988
    Assignee: Merck & Co., Inc.
    Inventors: Larry J. Caldwell, Colin R. Gardner, Robyn C. Cargill, Takeru Higuchi