Abstract: The present invention provides a spiro-azabicyclic compound or a salt or prodrug thereof, said compound comprising a saturated or unsaturated 5-membered heterocyclic ring containing two heteroatoms selected from oxygen, nitrogen and sulphur, no more than one of said heteroatoms being nitrogen; said heterocyclic ring having a spiro attachment to an optionally substituted azabicyclo[2.2.1]heptane or azabicyclo[3.2.1]octane ring system; which compounds are useful for the treatment of neurological and mental disorders.
Type:
Grant
Filed:
June 29, 1989
Date of Patent:
February 12, 1991
Assignee:
Merck Sharp & Dohme, Ltd.
Inventors:
Raymond Baker, Leslie J. Street, John Saunders
Abstract: Compounds of formula III: ##STR1## wherein R.sup.1 is a 5- or 6-membered aromatic heterocyclic group; and R.sup.4 and R.sup.5 each idependently signify hydrogen, halogen, trifluoromethyl, cyano, nitro, amino or lower alkyl; are useful intermediates in a novel process for the preparation of a class of pharmacologically active compounds of formula I: ##STR2## wherein R.sup.1, R.sup.4 and R.sup.5 are as defined above; and R.sup.3 represents hydrogen or lower alkyl.
Type:
Grant
Filed:
September 29, 1989
Date of Patent:
December 11, 1990
Assignee:
Merck, Sharp & Dohme Ltd.
Inventors:
Peter G. Houghton, Stanley H. B. Wright
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: The present invention provides a compound of formula I or a salt or prodrug thereof: ##STR1## wherein the dotted line represents an optional chemical bond in one of the two possible positions;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, benzyloxy, hydroxy (C.sub.1-6)alkyl, halogen, amino, cyano, nitro, --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, halogen, 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, --CH or --C--; andW represents oxygen, sulphur or --NR.sup.8, in which R.sup.8 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.
Type:
Grant
Filed:
April 4, 1989
Date of Patent:
July 10, 1990
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Raymond Baker, Clare O. Kneen, John Saunders, Christopher Swain
Abstract: A packaging and dispensing system provides for separate packaging of two ingredients of which at least one is a liquid and for extemporaneous mixing of the two ingredients at the time of first use. The system comprises a first bottle (2) containing the liquid or solid first ingredient and the neck of which is stoppered by a plug (5, 8). It further comprises a second bottle (9) containing the liquid second ingredient and assembled to the first bottle (2) at its neck. There is also an internal coupling member (11) carried by the second bottle (9) and the end of which is coupled to the plug (8). This coupling is obtained automatically when the two bottles are assembled together. A cap (13)screwed onto the second bottle (9) is coupled to the coupling member (11) so that at the time of first use unscrewing the cap (13) initially displaces the plug (8) and establishes automatically the communication between the two bottles without compromising any sterile conditions that may apply.
Abstract: The present invention provides a compound of formula I: ##STR1## or a salt thereof, wherein: the dotted lines represent optional double bonds;R.sup.1 represents hydrogen, hydroxy, alkenyl, alkyl, aminoalkyl or hydroxyalkyl;R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 independently represet hydrogen, hydroxy, fluoro, alkenyl, aryl, alkyl, or alkyl substituted with aryl, amino, hydroxy, carboxy or fluoro; andR.sup.7, R.sup.8, R.sup.9 and R.sup.10 independently represent hydrogen, hydrocarbon or a heterocyclic group provided that R.sup.7, R.sup.8, R.sup.9 and R.sup.10 are not simultaneously hydrogen; orR.sup.7 and R.sup.8 and/or R.sup.9 and R.sup.10 may complete a saturated or unsaturated C.sub.4-9 hydrocarbon or heterocyclic ring; which compounds are useful as anticonvulsant agents and in the treatment and/or prevention of neurodegenerative disorders.
Type:
Grant
Filed:
November 22, 1988
Date of Patent:
May 22, 1990
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Raymond Baker, William R. Carling, Kim James, Paul D. Leeson
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: Specific N-methyl-D-aspartate receptor antagonists are useful in the prevention and treatment of neurodegeneration in various pathological states.
Type:
Grant
Filed:
December 24, 1986
Date of Patent:
December 19, 1989
Assignee:
Merck Sharp & Dohme Limited
Inventors:
Geoffrey N. Woodruff, Erik H. F. Wong, John A. Kemp
Abstract: Heterocyclic aminoethanols of the formulaHet--CHOH--CH.sub.2 --NH--aralkylwhere het is a 6-10 membered N heterocycle are disclosed. The compounds are useful as pharmaceuticals.
Abstract: A granulation method involving polysaccharide gelling agents, e.g., alginic acid, and a metal salt, e.g., magnesium salt is developed for the stabilization of heat and/or moisture sensitive drugs or food supplements such as Efrotomycin, avermectins, milbemycins, mocimycin and other drugs. It has been found that the granules so obtained can be incorporated into various formulations without substantial decomposition.
Type:
Grant
Filed:
February 1, 1983
Date of Patent:
July 1, 1986
Assignee:
Merck Sharp & Dohme
Inventors:
Howard C. Maxfield, Anthony J. Phillips, Richard J. Yarwood
Abstract: The invention relates to an assembly for preparing and dispensing a solution and to the stopper for such an assembly, said assembly comprising a first bottle containing a first liquid component, with an elongated head; a second bottle containing a second component, liquid or solid; a stopper for this second bottle presenting a recess whose shape is homologous of the head of the first bottle, and in which said head is for example screwed. The bottom of the recess is constituted by a membrane of deformable material comprising an axial orifice which is hermetically closed, in the absence of deformation of the membrane, by the natural radial constriction of the material of the membrane. By screwing the first bottle in the stopper, the membrane is axially deformed and the orifice is radially distended, thus allowing the two bottles to be placed in communication in reversible manner. The invention also relates to a process for making the stopper.
Abstract: The invention relates to a device for preparing and dispensing a solution. A bottle containing a substance to be disolved is closed by a disc-shaped base having a rigid rod thereon and a deformable head. A tube of solvent is closed by an apertured slidable piston. Mixing is effected by placing the piston against the rigid rod and applying axial pressure which dispenses the solvent from the tube, through a capillary channel in the rod and into the bottle. Slots in the rod are revealed during this operation to allow the air to escape from the bottle. The deformable head also serves to pressurize the bottle to permit dispensing therefrom.
Abstract: Novel 4-substituted-3-hydroxy-3-pyrroline-2,5-diones are disclosed which inhibit glycolic acid oxidase and thus are useful in the treatment and prevention of calcium oxalate renal lithiasis.
Abstract: The present invention relates to a container which is notably intended to hold pills, and it comprises on the one hand an external, rigid envelope 10 and on the other hand an internal envelope 11 enclosing the pills, this internal envelope being elastically deformable and capable of an increase in volume which is sufficient for absorbing the surplus pressure resulting from the packing of the pills when the lid is applied, without crushing the pills.In a first embodiment, the internal envelope 11 is cylindrical and it has a convex, deformable base 12.In a second embodiment, the internal envelope is a sleeve provided with at least one slit allowing its radial expansion.
Abstract: Novel N-(substituted) derivatives of 2-aza-2'-hydroxy-5,6-benzotricyclo[6.3.0.sup.1,8.0.sup.4,11 ] undecane of the formula: ##STR1## are centrally acting analgesics effective in the relief of pain.
Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted by C.sub.3-6 alkyl; or a pharmaceutically acceptable salt thereof;useful in treating urinary tract, especially renal calcium oxalate lithiasis.
Abstract: 4-Hydroxy-5-substituted-3(2H)-isothiazolone-1,1-dioxide derivatives of the formula: ##STR1## where X and Y are independently selected from the group consisting of hydrogen, halogen, and C.sub.1-6 alkyl; provided that positions 2 and 6 of the substituted phenyl moiety may not be substituted; and n is 0 or 1;or a pharmaceutically acceptable salt thereof; useful in treating urinary tract, especially renal calcium oxalate lithiasis.
Abstract: This invention relates to ophthalmic preparations which include 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)-3-indenylacetic acid or ophthalmologically acceptable salts thereof as the active entity for reducing or controlling inflammation of the eye.
Abstract: An enteric coating medium for solid medicinal dosage units is prepared by precipitation of a pH sensitive polymer from an alcoholic solution of such a polymer and a plasticizing agent to produce a suspension of fine particles of a mixture of polymer and plasticizing agent.