Patents Assigned to Merck Sharp & Dohme
  • Patent number: 5219849
    Abstract: A class of pyrazine, pyrimidine and pyridazine derivatives, substituted by a non-aromatic azabicyclic ring system and optionally by up to two further substituents, is of use in the preparation of medicaments, especially formulations adapted for topical administration to the eye, suitable for the treatment of glaucoma and/or for reducing intraocular pressure.
    Type: Grant
    Filed: December 17, 1991
    Date of Patent: June 15, 1993
    Assignee: Merck Sharp & Dohme
    Inventors: Victor Lotti, Graham A. Showell
  • Patent number: 5208248
    Abstract: A class of indazole-substituted five-membered heteroaromatic compounds are specific agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: July 16, 1991
    Date of Patent: May 4, 1993
    Assignee: Merck Sharpe & Dohme, Ltd.
    Inventors: Raymond Baker, Mark S. Chambers, Leslie J. Street
  • Patent number: 5194440
    Abstract: A class of substituted cyclic sulphamide derivatives are selective agonists of 5-HT.sub.1 -like receptors and are therefore useful in the treatment of clinical conditions, in particular migraine and associated disorders, for which a selective agonist of these receptors is indicated.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: March 16, 1993
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Jose L. C. Pineiro
  • Patent number: 5177084
    Abstract: Benzenes, substituted by a non-aromatic, non-fused 1-azabicycle and a substituent of low lipophilicity or a hydrocarbon substituent, their salts and prodrugs are useful in medicine, for example, in treating dementia. Some formulations of such benzenes are novel as are some of the compounds per se. They can be synthesized by methods analogous to those known in the art.
    Type: Grant
    Filed: November 19, 1991
    Date of Patent: January 5, 1993
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Graham A. Showell
  • Patent number: 5158192
    Abstract: A sterile packaging assembly (100) for dispensing a liquid in drops comprises a main body (101) of plastic material, having a top portion (103) with an outside thread for receiving a screw cap (104), the top portion ending in an elongate neck, constituting a dispensing portion which is surmounted by a closure head (110) that can be torn off in order to define a dispensing orifice (111) on first utilization of the packaging assembly. The invention is particularly applicable to sterile packaging of pharmaceutical substances such as eye drops.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: October 27, 1992
    Assignee: Laboratoires Merck Sharp & Dohme-Chibret
    Inventor: Gilbert Lataix
  • Patent number: 5158213
    Abstract: A sterile packaging assembly (100) for dispensing a liquid in drops comprises a main body (101) of plastic material, having a top portion (103) with an outside thread for receiving a screw cap (104), and containing a flow rate restriction system (105) for controlling drop formation. The flow rate restriction system is positioned substantially on the axis of the main body and is held in position by a constricted portion (106) of the top portion (103) of the main body. The invention is particularly applicable to sterile packaging of pharmaceutical substances such as eye drops.
    Type: Grant
    Filed: October 24, 1990
    Date of Patent: October 27, 1992
    Assignee: Laboratoires Merck Sharp & Dohme-Chibret
    Inventor: Gilbert Lataix
  • Patent number: 5140034
    Abstract: A class of 5-membered heterocyclic compounds having at least one heteroatom, substituted on the heterocyclic ring by an imidazolyl moiety, are useful in the treatment of psychotic disorders (e.g. schizophrenia and mania); anxiety; alcohol or drug withdrawal or dependence; pain; gastric stasis; gastric dysfunction (such as occurs with dyspepsia, peptic ulcer, reflux oesophagitis and flatulence); migraine, nausea and vomiting; movement disorders; and presenile and senile dementia.
    Type: Grant
    Filed: March 8, 1990
    Date of Patent: August 18, 1992
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Christopher Swain, John Saunders
  • Patent number: 5124460
    Abstract: A process for preparing a substantially pure enantiomer of a compound formula (I) ##STR1## wherein X is O or S; andR.sup.2 represents hydrogen, --CF.sub.3, --OR.sup.7, --SR.sup.7, --NR.sup.7 R.sup.8, --CN, --COOR.sup.7, --CONR.sup.7 R.sup.8, or a saturated or unsaturated, substituted or unsubstituted hydrocarbon group, wherein R.sup.7 and R.sup.8 are independently selected from hydrogen and C.sub.1-2 alkyl provided that --NR.sup.7 R.sup.8 is other than NH.sub.2 ;which process comprises cyclization of a compound of formula (10) or salt thereof: ##STR2## wherein X and R.sup.2 are as defined in formula (I); and R.sup.4 is a labile leaving group and optionally epimerizing the endo-diastereomer so prepared to produce the corresponding exo-diastereomer.
    Type: Grant
    Filed: May 6, 1991
    Date of Patent: June 23, 1992
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Guy R. Humphrey
  • Patent number: 5106853
    Abstract: The compound (3R, 4R)-3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-1-azabicyclo[2.2.1]heptane and its salts behave as a functionally selective muscarinic agonist and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by methods analogous to those known in the art via suitable chiral intermediates and cyclopropyl carboxamide oxime.
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 21, 1992
    Assignee: Merck Sharp & Dohme, Ltd.
    Inventors: Graham A. Showell, Leslie J. Street
  • Patent number: 5104989
    Abstract: A process for preparing substantially pure enantiomers of formula (I) ##STR1## where the * represents a chiral center, x is 0 or 1, in exo-, endo- or a mixture of exo- and endo- forms; and R is hydrogen, alkyl or aralkyl, via diastereomers of formula (IIA) or (IIB); ##STR2##
    Type: Grant
    Filed: May 9, 1990
    Date of Patent: April 14, 1992
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: I. Cottrell, S. H. B. Wright, D. Hands
  • Patent number: 5073557
    Abstract: The compound (R)-3-[2-(6-chloropyrazin)yl]-1-azabicyclo[2.2.2]octane and its salts behave as M.sub.1, M.sub.3 muscarinic agonists and are useful in the treatment of neurological and mental disorders, preferably in a pharmaceutical formulation comprising the active compound in association with a pharmaceutically acceptable carrier. The compound can be prepared by via methods analogous to those known in the art and a chiral acid resolution.
    Type: Grant
    Filed: August 8, 1990
    Date of Patent: December 17, 1991
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Raymond Baker, Leslie J. Street, John Saunders
  • Patent number: 5055597
    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: January 8, 1990
    Date of Patent: October 8, 1991
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: David C. Billington
  • Patent number: 5041456
    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 alkylcarobnyl;V represents nitrogen, ##STR3## 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: July 13, 1990
    Date of Patent: August 20, 1991
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, John Saunders, Christopher Swain
  • Patent number: 4996197
    Abstract: The present invention concerns a pharmaceutical and/or cosmetic composition designed to be applied on the skin or the mucosae, characterized in that it contains Rhamsan gum.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: February 26, 1991
    Assignee: Laboratoires Merck Sharp & Dohme-Chibret
    Inventor: Claude Mazuel
  • Patent number: 4996211
    Abstract: The present invention provides a compound of formula (I): ##STR1## or a pharmaceutically acceptable salt thereof, wherein one of R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represents a hydrocarbon or hydrocarbyloxycarbonyl group and the remaining groups R.sup.1, R.sup.2, R.sup.3 and R.sup.4 independently represent hydrogen, hydrocarbon, hydrocarbyloxycarbonyl, halogen, hydroxy or C.sub.1-6 alkoxy, or R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4 may together represent the residue of a carbocyclic ring; R.sup.5 and R.sup.6 independently represent hydrogen, hydrocarbon, hydroxy or fluoro; R.sup.7 represents hydrogen or C.sub.1-3 alkyl; and R.sup.8 represents methyl or ethyl; which compounds are useful as anticonvulsant agents and in the treatment of neurodegenerative diseases.
    Type: Grant
    Filed: August 12, 1988
    Date of Patent: February 26, 1991
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Raymond Baker, Paul D. Leeson, Susan F. Britcher
  • Patent number: 4992436
    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
  • Patent number: 4977258
    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
  • 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: 4940703
    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
  • Patent number: 4936446
    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.
    Type: Grant
    Filed: February 28, 1989
    Date of Patent: June 26, 1990
    Assignee: Laboratoires Merck, Sharp & Dohme-Chibret
    Inventor: Gilbert Lataix