Patents Assigned to Merck
  • Substituted piperidine derivatives as selective agonists of 5-HT receptors
    Patent number: 6048878
    Abstract: A compound of formula (I), or a salt or prodrug thereof, is described, wherein G is attached at position 3 or 4 of the piperidine ring and represents halogen or C.sub.1-6 alkoxy; R1 represents C.sub.3-6 alkenyl, C.sub.3-6 alkynyl, aryl(C.sub.1-6)alkyl or heteroaryl (C.sub.1-6)alkyl, any of which groups may be optionally substituted; processes for its preparation and its use in therapy, particularly in the treatment of migraine.
    Type: Grant
    Filed: May 13, 1998
    Date of Patent: April 11, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Jose Luis Castro Pineiro, Ian James Collins, Angus Murray MacLeod, Christopher Richard Moyes, Michael Rowley, Graham Andrew Showell
  • Process for preparing lithium intercalation compounds
    Patent number: 6048643
    Abstract: The invention relates to a process for preparing lithium intercalation compounds by thermal solid state reaction of mixtures of lithium hydroxide or lithium oxide and oxides or oxide precursors of transition metals. A significant step of this process is the treatment of an aqueous suspension of the raw material components lithium hydroxide or lithium oxide and metal oxide or metal oxide precursors with hydrogen peroxide, resulting in the lithium compound going into solution. In the drying of the mixture, the lithium hydroxide is very uniformly absorbed onto the metal oxide. Calcination at temperatures between 450.degree. C. and 700.degree. C. results in complete reaction to form the lithium intercalation compound in less than 5 hours.
    Type: Grant
    Filed: February 10, 1999
    Date of Patent: April 11, 2000
    Assignee: Merck Patent Gesellschaft
    Inventors: Max van Ghemen, Birgit Sauerbrey, Ludwig Pohl
  • Morpholine and thiomorpholine tachykinin receptor antagonists
    Patent number: 6048859
    Abstract: Substituted heterocycles of the general structural formula: ##STR1## are tachykinin receptor antagonists useful in the treatment of inflammatory diseases, pain or migraine, asthma and emesis, and calcium channel blockers useful in the treatment of cardiovascular conditions such as angina, hypertension or ischemia.
    Type: Grant
    Filed: February 16, 1999
    Date of Patent: April 11, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Paul E. Finke, Jeffrey J. Hale, Malcolm Maccoss, Sander G. Mills, Shrenik K. Shah, Mark Stuart Chambers, Timothy Harrison, Tamara Ladduwahetty, Brian John Williams
  • Chemical synthesis of 1,4-oxazin-2-ones
    Patent number: 6046325
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl or arylC.sub.1-4 alkyl group; and R.sup.2 is a hydrogen atom, a halogen atom, or a group selected from C.sub.1-6 alkyl, CF.sub.3 or C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.
    Type: Grant
    Filed: September 8, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Michael Stewart Ashwood, Brian Christopher Bishop, Ian Frank Cottrell
  • Convergent process for the preparation of a growth hormone secretagogue
    Patent number: 6046333
    Abstract: The present invention is directed to a novel convergent process for the preparation of the compound N-[1(R)-[(1,2-dihydro-1-methanesulfonyl-spiro[3H-indole-3,4'-piperdin]-1'- yl)carbonyl]-2-(phenylmethyl-oxy)ethyl]-2-amino-2-methyl-propanamide, and salts thereof, which has the structure: ##STR1## and which has the ability to stimulate the release of natural or endogenous growth hormone. This compound may be used to treat conditions which require the stimulation of growth hormone production or secretion such as in humans with a deficiency of natural growth hormone or in animals used for food or wool production where the stimulation of growth hormone will result in a larger, more productive animal.
    Type: Grant
    Filed: October 21, 1997
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Ilias Dorziotis, Ioannis Houpis, Audrey Molina, Ralph Volante
  • 2,3,5-trisubstituted pyridines as inhibitors of cyclooxygenase-2
    Patent number: 6046217
    Abstract: The invention encompasses the novel compound of Formula I as well as a method of treating cyclooxygenase-2 mediated diseases comprising administration to a patient in need of such treatment of a non-toxic therapeutically effective amount of a compound of Formula I. ##STR1## The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: September 11, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck Frosst Canada & Co.
    Inventors: Richard Friesen, Rejean Fortin, Daniel Dube, Denis Deschenes
  • Spiro-azacyclic derivatives, their preparation and their use as tachykinin antagonists
    Patent number: 6046195
    Abstract: The present invention relates to certain spiro-azacyclic derivatives which are tachykinin antagonists and are useful, for example, in the treatment or prevention of pain, inflammation, migraine, emesis and postherpetic neuralgia.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Karen Elizabeth Haworth, Eileen Mary Seward, Christopher John Swain
  • Antispastic use of triazolo-pyridazine derivatives
    Patent number: 6046196
    Abstract: A class of substituted 7,8-ring fused 1,2,4-triazolo[4,3-b]pyridazine derivatives, as shown in Formula I possessing an optionally substituted cycloalkyl, phenyl or heteroaryl substituent at the 3-position and a substituted alkoxy moiety at the 6-position, are selective ligands for GABA.sub.A receptors, in particular having high affinity for the .alpha.2 and/or .alpha.3 subunit thereof, and are accordingly of benefit in the treatment and/or prevention of muscle spasm or spasticity, e.g. in paraplegic patients.
    Type: Grant
    Filed: December 9, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck Sharp & Dohme Ltd.
    Inventor: Franz Fridolin Hefti
  • Phosphate-mediated cyclization
    Patent number: 6046327
    Abstract: This invention relates to a cyclization process useful in the preparation of a key intermediate in the preparation of an endothelin antagonist of the general formula shown below: ##STR1##
    Type: Grant
    Filed: April 1, 1999
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Richard D. Tillyer, David M. Tschaen, Zhiguo Song, Mangzu Zhao
  • Electro-optical liquid-crystal display
    Patent number: 6045878
    Abstract: The invention relates to an electro-optical liquid-crystal display having a realignment layer for realigning the liquid crystals whose field has a significant component parallel to the liquid-crystal layer and which contains a liquid-crystalline medium of positive dielectric anisotropy, where the medium comprises at least one mesogenic compound and at least one alkenyl compound of formula I*.
    Type: Grant
    Filed: December 4, 1997
    Date of Patent: April 4, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Kazuaki Tarumi, Andreas Beyer, Volker Reiffenrath, Eike Poetsch
  • Method of synergistic treatment for benign prostatic hyperplasia
    Patent number: 6046183
    Abstract: Disclosed is an improved treatment for men with benign prostatic hyperplasia (BPH), involving combination therapy of a 5.alpha.-reductase inhibitor, e.g. a 17.beta.-substituted 4-azasteroid, a 17.beta.-substituted non-azasteroid, 17.beta.-acyl-3-carboxy-androst-3,5-diene, benzoylaminophenoxybutanoic acid derivative, fused benz(thio)amide or cinnamoylamide derivative, aromatic 1,2-diethers or thioethers, aromatic ortho acylaminophenoxy alkanoic acids, ortho thioalkylacylaminophenoxy alkanoic acids, pharmaceutically acceptable salts and esters thereof, and particularly finasteride, in combination with an .alpha..sub.1 -adrenergic receptor blocker, i.e., terazosin. The combination provides therapy at the molecular level for the underlying cause of the disease as well as providing symptomatic relief. Pharmaceutical compositions useful for treatment are also disclosed.
    Type: Grant
    Filed: February 20, 1998
    Date of Patent: April 4, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Glenn J. Gormley, Elizabeth Stoner
  • Nitromethyl ketones, process for preparing them and compositions containing them
    Patent number: 6043281
    Abstract: The present invention relates to the compounds of formula: ##STR1## in which R.sub.1, R.sub.2, R.sub.3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: March 28, 2000
    Assignee: Merck Patent Gesellschaft mit Beschrankter Haftung
    Inventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Philippe Durbin
  • Combination therapy for the prevention and treatment of osteoporosis
    Patent number: 6043026
    Abstract: The combination of an estrogen receptor modulator and a growth hormone secretagogue is useful in the treatment or prevention of diseases involving bone resorption, especially osteoporosis.
    Type: Grant
    Filed: May 1, 1998
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Arthur A. Patchett, Gideon A. Rodan
  • Chiral bisphosphines
    Patent number: 6043387
    Abstract: New chiral biphosphines, e.g., ##STR1## are useful as key components in catalysts for asymmetric reactions, providing desirably high enantiomeric excess (ee).
    Type: Grant
    Filed: February 3, 1999
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Philip Pye, Ralph P. Volante, Kai Rossen
  • Electrooptical liquid crystal system
    Patent number: 6042745
    Abstract: The invention relates to an electroptical system which, between 2 electrode layers, contains a PDLC film comprising a liquid crystal mixture forming micro-droplets in an optically isotropic, transparent polymer matrix. The liquid crystal mixture comprises one or more compounds of the formula I ##STR1## wherein Z.sup.1, Z.sup.2, ##STR2## X.sup.1, X.sup.2, Q, Y, n and R are as defined herein. The liquid crystal mixture additionally contains one or more reactive liquid crystalline compounds in order to obtain improved switching times especially at low temperatures.
    Type: Grant
    Filed: January 16, 1998
    Date of Patent: March 28, 2000
    Assignee: Merck Patent GmbH
    Inventors: David Coates, Owain Llyr Parri, Simon Greenfield, Martin David Tillin, Mark John Goulding, Patrick Nolan
  • Fused piperidine substituted arylsulfonamides as .beta.3-agonists
    Patent number: 6043253
    Abstract: Fused piperidine substituted arylsulfonamides are .beta..sub.3 adrenergic receptor agonists with very little .beta..sub.1 and .beta..sub.2 adrenergic receptor activity and as such the compounds are capable of increasing lipolysis and energy expenditure in cells. The compounds thus have potent activity in the treatment of Type II diabetes and obesity. The compounds can also be used to lower triglyceride levels and cholesterol levels or raise high density lipoprotein levels or to decrease gut motility. In addition, the compounds can be used to reduced neurogenic inflammation or as antidepressant agents. Compositions and methods for the use of the compounds in the treatment of diabetes and obesity and for lowering triglyceride levels and cholesterol levels or raising high density lipoprotein levels or for decreasing gut motility are also disclosed.
    Type: Grant
    Filed: February 25, 1999
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Linda Brockunier, Ann E. Weber, Emma R. Parmee
  • Hexahydro-5-imino-1,4-heteroazepine derivatives as inhibitors of nitric oxide synthases
    Patent number: 6043358
    Abstract: Disclosed herein are compounds of Formula I and pharmaceutically acceptable salts thereof which have been found useful in the treatment of nitric oxide synthase mediated diseases and disorders, including neurodegenerative disorders, disorders of gastrointestinal motility and inflammation.
    Type: Grant
    Filed: September 25, 1996
    Date of Patent: March 28, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Charles G. Caldwell, William K. Hagmann, Malcolm Maccoss, Shrenik K. Shah, Kothandaraman Shankaran, Karla L. Furman
  • Chroman derivatives
    Patent number: 6040308
    Abstract: Chroman derivatives of the formula I ##STR1## wherein R.sup.1 to R.sup.8 have the meanings defined herein, and their salts have an effect on the cardiovascular system.
    Type: Grant
    Filed: October 28, 1994
    Date of Patent: March 21, 2000
    Assignee: Merck Gesellschaft mit beschrankter Haftung
    Inventors: Gunther Hausler, Rolf Gericke, Hanns Wurziger, Manfred Baumgarth, Inge Lues, Jacques De Peyer, Rolf Bergmann
  • Sulfonamide fibrinogen receptor antagonists
    Patent number: 6040317
    Abstract: A series of non-peptide derivatives that are antagonists of the fibrinogen IIb/IIIa receptor and thus are platelet anti-aggregation compounds useful in the prevention and treatment of diseases caused by thrombus formation.
    Type: Grant
    Filed: December 28, 1998
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Duggan, Wasyl Halczenko, Melissa S. Egbertson, George D. Hartman, William L. Laswell
  • Sordarin derivatives
    Patent number: 6040463
    Abstract: Sordarin derivatives are antifungal agents useful in the treatment and/or prevention of human and animal fungal infections, as well as in the control of phytopathogenic fungi in crops.
    Type: Grant
    Filed: September 24, 1997
    Date of Patent: March 21, 2000
    Assignee: Merck & Co., Inc.
    Inventors: James M. Balkovec, Bruno Tse