Patents Assigned to Merck
  • Patent number: 6329393
    Abstract: A crystalline pharmaceutically acceptable benzenesulfonate salt of Compound A of formula: and solvates thereof are disclosed. Compound A and its benzenesulfonate salts are alpha 1a adrenergic receptor antagonists useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts are also disclosed.
    Type: Grant
    Filed: December 13, 1999
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joseph S. Amato, Zhen Li, James A. McCauley
  • Patent number: 6329376
    Abstract: The present invention is directed to peptidomimetic piperazine-containing macrocyclic compounds which inhibit a prenyl-protein transferase (FTase) and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
    Type: Grant
    Filed: October 26, 1999
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventor: Jeffrey M. Bergman
  • Patent number: 6329380
    Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
    Type: Grant
    Filed: June 26, 2000
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Joung L. Goulet, Mark A. Holmes, Julianne A. Hunt, Sander G. Mills, William H. Parsons, Peter J. Sinclair, Dennis M. Zaller
  • Patent number: 6329401
    Abstract: A tachykinin antagonist is useful, alone or in conjunction with other agents, for altering circadian rhythmicity and alleviating circadian rhythm disorders and for enhancing and improving the quality of sleep.
    Type: Grant
    Filed: December 16, 1999
    Date of Patent: December 11, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Carl M. Mendel, Joanne Waldstreicher
  • Patent number: 6329421
    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. The invention also encompasses certain pharmaceutical compositions for treatment of cyclooxygenase-2 mediated diseases comprising compounds of Formula I.
    Type: Grant
    Filed: February 25, 1997
    Date of Patent: December 11, 2001
    Assignee: Merck Frosst Canada & Co.
    Inventors: Petpiboon Prasit, Daniel Guay, Zhaoyin Wang, Serge Leger, Michel Therien
  • Publication number: 20010049376
    Abstract: 17&bgr;-N-monosubstituted-carbamoyl-4-aza-5&agr;-androst-1-en-3-ones of the formula 1
    Type: Application
    Filed: June 6, 2001
    Publication date: December 6, 2001
    Applicant: MERCK & CO., Inc.
    Inventors: Glenn J. Gormley, Elizabeth Stoner
  • Publication number: 20010049439
    Abstract: There is disclosed 3-(5-methylisoxazol-3-yl)-6-(1-methyl-1,2,3-triazol-4-yl)methyloxy-1,2,4-triazolo[3,4-a]phthalazine in the form of a dihydrate, a dehydrate of the dihydrate and a pentahydrate, pharmaceutical compositions comprising the forms, the use of the forms for enhancing cognition, processes for producing the forms, their incorporation in pharmaceutical compositions comprising pamoate ions and the use of such ions for solubilizing neutral molecules.
    Type: Application
    Filed: November 30, 2000
    Publication date: December 6, 2001
    Applicant: Merck & Co., Inc.
    Inventors: Michael J. Kaufman, James A. McCauley, Daniel J. Rush, David M. Tschaen, Richard J. Varsolona, Guo-Jie Ho
  • Patent number: 6326066
    Abstract: 1,4-disubstituted 2,6-difluorobenzene compound of formula I wherein R is an alkyl or alkenyl radical, A1 and A2 are independently (a) a trans-1,4-cyclohexylene radical in which a CH2 group may be replaced by -O- and/or -S, (b) a 1,4-phenylene radical in which a CH group may be replaced by N, (c) 1,4-cyclohexenylene, 1,4-bicyclo(2,2,2)octylene, piperidine-1,4-diyl, naphthalene-2,6-diyl, decahydronaphthalene-2,6-diyl or 1,2,3,4-tetrahydronaphthalene-2,6-diyl, Z1 and Z2 are —CO—O—, —O—CO—, —CH2O—,—OCH2—, —CH2CH2—, —CH═CH—,—C≡C—or a single bond m and n are 0, 1, 2 or 3, (m+n) is 1, 2 or 3, X is R or F, Cl, CF3, —OCF3, or —OCHF2, —OCF5, —CN or —NCS with the provisos that at least one of the radicals A1 and A2 present in the molecule is  and at least one of Z1 or Z2 is —COO—, are suitable as components of liquid-
    Type: Grant
    Filed: February 28, 2000
    Date of Patent: December 4, 2001
    Assignee: Merck Patent Gesellschaft mit Reschankter Haftung
    Inventors: Eike Poetsch, Volker Meyer, Volker Reiffenrath, Andreas Wachtler, Ulrich Finkenzeller, Hans Adolf Kurmeier, Reinhard Hittich, Bernhard Rieger, David Coates, Simon Greenfield, Robert William Clemitson
  • Patent number: 6327010
    Abstract: An electrooptical system contains: (a) a twisted nematic liquid-crystal layer, with an input side and an output side, which is positioned between a first substrate and a second substrate, each of whose inside surface is provided with an electrode coating and an alignment layer thereon, the director of said liquid crystal layer having a parallel edge alignment and a twist angle of 0°≦&bgr;≦1000, (b) at least one compensation layer for compensating the optical path difference of the liquid-crystal layer d·&Dgr;n, and (c) at least one device for linear polarization of light in such an arrangement that light, before entering and after exiting the liquid-crystal layer, passes through a polarization device, I.
    Type: Grant
    Filed: December 19, 1996
    Date of Patent: December 4, 2001
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Bernhard Scheuble, Günter Baur, Waltraud Fehrenbach, Barbara Staudacher
  • Patent number: 6326403
    Abstract: Compounds of the formula I wherein X, Y, Z, R1 and R2 are as defined in claim 1, and their salts and solvates, can be used as integrin inhibitors in particular for the prophylaxis and treatment of circulatory disorders, for thrombosis, cardiac infarction, coronary heart diseases, arteriosclerosis, for pathological processes which are maintained or propagated by angiogenesis and in tumour therapy.
    Type: Grant
    Filed: January 12, 2001
    Date of Patent: December 4, 2001
    Assignee: Merck Patent Gesellschaft mit
    Inventors: Günter Hölzemann, Simon Goodman, Horst Kessler, Christoph Gibson, Jörg Simon Schmitt
  • Patent number: 6326372
    Abstract: Lactam and cyclic urea derivatives and their pharmaceutically acceptable salts are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are typically selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: September 27, 2000
    Date of Patent: December 4, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Ben E. Evans, Kevin F. Gilbert
  • Publication number: 20010046977
    Abstract: Alendronate, an aminobisphosphonate, can prevent osteoporosis in early post menopausal women.
    Type: Application
    Filed: February 27, 2001
    Publication date: November 29, 2001
    Applicant: MERCK & CO., Inc.
    Inventor: Ashley J. Yates
  • Publication number: 20010046628
    Abstract: The invention relates to lithium mixed oxide particles coated with one or more layers of alkali metals and metal oxides for improving the properties of electrochemical cells.
    Type: Application
    Filed: March 26, 2001
    Publication date: November 29, 2001
    Applicant: Merck Patent GmbH
    Inventors: Ruediger Oesten, Bangyin Li, Nobuaki Nakamura, Katsuhisa Nitta
  • Patent number: 6323198
    Abstract: A method of treatment for enhancing cognition in the treatment of Alzheimer's disease, for example, employs a specific GABAA Alpha5 receptor ligand.
    Type: Grant
    Filed: July 20, 2000
    Date of Patent: November 27, 2001
    Assignee: Merck Sharp & Dohme Limited
    Inventor: Gerard Raphael Dawson
  • Patent number: 6319932
    Abstract: Novel oxazolidinone compounds and pharmaceutically acceptable salts thereof are disclosed. The synthesis of these compounds and their use as alpha 1a adrenergic receptor antagonists is also described. One application of these compounds is in the treatment of benign prostatic hyperplasia. These compounds are selective in their ability to relax smooth muscle tissue enriched in the alpha 1a receptor subtype without at the same time inducing hypotension. One such tissue is found surrounding the urethral lining. Therefore, one utility of the instant compounds is to provide acute relief to males suffering from benign prostatic hyperplasia, by permitting less hindered urine flow. Another utility of the instant compounds is provided by combination with a human 5-alpha reductase inhibitory compound, such that both acute and chronic relief from the effects of benign prostatic hyperplasia can be achieved.
    Type: Grant
    Filed: November 10, 1999
    Date of Patent: November 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Jennie B. Nerenberg, Mark G. Bock, Harold G. Selnick, Linda Payne
  • Patent number: 6320052
    Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a sodium salt thereof wherein HET is 7-chloroquinolin-2-yl or 6,7-difluoroquinolin-2-yl, which comprises: reacting the dilithium dianion of 1-(mercapto-methyl)cyclopropaneacetic acid with a compound of formula (II) wherein HET is as defined above and L is arylsulfonyl or alkylsulfonyl. The invention further provides the dicyclohexylamine salt of a compound of formula (I).
    Type: Grant
    Filed: March 22, 1999
    Date of Patent: November 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Mahadevan Bhupathy, Daniel R. Sidler, James M. McNamara, Ralph P. Volante, James Bergan
  • Patent number: 6320049
    Abstract: This invention relates to crystalline pharmaceutically acceptable salts of an alpha 1a adrenergic receptor antagonist, Compound A, which are useful in the treatment of benign prostatic hyperplasia. Pharmaceutical compositions employing the crystalline salts, and processes for making and using the crystalline salts and pharmaceutical compositions of Compound A are also disclosed. This invention further relates to a process for obtaining enantiomerically pure intermediate useful for the synthesis of end product alpha 1a adrenergic receptor antagonists. The end product compounds are useful for the treatment of benign prostatic hyperplasia and for relaxing lower urinary tract tissue. The invention also relates to a process for preparing a class of dihydropyrimidinone compounds of which Compound A is a member, wherein the process involves deprotonating a dihydropyrimidinone compound and then coupling the deprotonated derivative with a primary amine.
    Type: Grant
    Filed: May 2, 2000
    Date of Patent: November 20, 2001
    Assignee: Merck & Co., Inc.
    Inventors: Daniel R. Sidler, Robert D. Larsen, Wenjie Li
  • Patent number: 6319953
    Abstract: The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of a specific class of NK-1 receptor antagonists and fluoxetine.
    Type: Grant
    Filed: December 8, 1999
    Date of Patent: November 20, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Emma Joanne Carlson, Nadia Melanie Rupniak
  • Patent number: 6319924
    Abstract: 1,2,4-triazolo[4,3-b]pyridazine derivatives, represented by wherein Z represents an optionally substituted tetrahydropyridinyl substituent, are selective ligands for GABAA receptors, in particular having high affinity for the &agr;2 and/or &agr;3 subunit thereof, are useful in the treatment of anxiety and convulsions.
    Type: Grant
    Filed: June 28, 2000
    Date of Patent: November 20, 2001
    Assignee: Merck Sharp & Dohme Ltd.
    Inventors: Timothy Harrison, Timothy Jason Sparey
  • Patent number: 6319963
    Abstract: The invention relates to a process as described in claim of preparing a reflective film comprising a layer of a polymerized mesogenic material with helically twisted structure, wherein the helix axis is perpendicular to the film plane, and containing regions with varying helical pitch, to a reflective film obtainable by such a process, to the use of such a reflective film as reflective broadband or notch polarizer or as a multicolored film or image in liquid crystal displays, as color filter, in effect pigments, for decorative or security applications, and to a liquid crystal display comprising a liquid crystal cell and a reflective polarizer as described in the foregoing and the following, and optionally further comprising one or more compensaters or polarizers.
    Type: Grant
    Filed: August 26, 1999
    Date of Patent: November 20, 2001
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: David Coates, Mark Andrew Verrall