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
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
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
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.
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.
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.
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.
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.
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
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.
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
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.
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.
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