Patents Represented by Attorney Manfred Polk
  • 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: 5183826
    Abstract: An antiviral agent produced by Hypoxylon fragiforme and having the structure: ##STR1## is described. The product has high activity as an HIV protease enzyme inhibitor and is useful in the treatment of diseases in which control of HIV protease activity is desirable.
    Type: Grant
    Filed: September 25, 1990
    Date of Patent: February 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Gerald F. Bills, Otto D. Hensens, Lawrence Koupal, Russell B. Lingham, John G. Ondeyka, Deborah L. Zink
  • 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: 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: 5134146
    Abstract: The use of compounds for formula (I): ##STR1## or a salt or prodrug thereof; wherein one of X, Y, or Z is an oxygen or sulphur atom and the other two are nitrogen atoms, and the dotted circle represents two double bonds thus forming a 1,3,4-oxadiazole, 1,2,4-oxadiazole, 1,3,4-thiadiazole or 1,2,4-thiadiazole nucleus;R.sup.1 represents a non-aromatic azacyclic or azabicyclic ring system selected from ##STR2## wherein the broken line represents an optional chemical bond; the substituents R.sup.3 and R.sup.4 may be present at any position, including the point of attachment to the oxa- or thia-diazole ring, and independently represent hydrogen, C.sub.1-4 alkyl, halo, C.sub.1-4 alkoxy, hydroxy or carboxy, or R.sup.3 and R.sup.4 together represent carbonyl;the group R.sup.5 represents hydrogen or C.sub.1-4 alkyl; andR.sup.2 represents hydrogen, C.sub.1-8 hydrogen, C.sub.1-8 alkyl optionally substituted by hydroxy or fluoro, C.sub.2-8 alkenyl, OR.sup.7, SR.sup.7, NR.sup.7 R.sup.8, CN, CO.sub.2 R.sup.7, CONR.sup.7 R.
    Type: Grant
    Filed: May 29, 1991
    Date of Patent: July 28, 1992
    Assignee: Merck Sharp and Dohme Ltd.
    Inventors: Graham Showell, Victor Lotti
  • 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: 5066648
    Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.
    Type: Grant
    Filed: September 13, 1990
    Date of Patent: November 19, 1991
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Takeru Higuchi, deceased
  • 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: 5002206
    Abstract: A double tip drug dispensing and metering device having a bellows or conventional squeeze body container between the double tips. The device being adapted to hold at least two substances in solution which are required to be separated until just prior to dispensation.
    Type: Grant
    Filed: October 25, 1989
    Date of Patent: March 26, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John E. Allegretti, Thomas E. Schlaudecker
  • 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: 4973579
    Abstract: Choline ester salts are used as drug absorption enhancing agents for orally and rectally administered drugs.
    Type: Grant
    Filed: February 16, 1989
    Date of Patent: November 27, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix
  • Patent number: 4970206
    Abstract: The invention relates to pyroglutamic acid esters used as dermal penetration enhancers for therapeutic agents having poor skin permeation.
    Type: Grant
    Filed: May 8, 1989
    Date of Patent: November 13, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Takeru Higuchi
  • Patent number: 4963556
    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: April 20, 1989
    Date of Patent: October 16, 1990
    Assignee: Merck & Co., Inc.
    Inventors: Jose Alexander, Joseph A. Fix, A. J. Repta