Abstract: This invention relates to prostaglandin-bisphosphonate conjugates. These conjugates are effective for treating or preventing bone diseases such as osteoporosis. These conjugates simultaneously deliver a prostaglandin agent for increasing bone formation and a bisphosphonate agent for inhibiting bone resorption.
Type:
Grant
Filed:
November 15, 1999
Date of Patent:
September 19, 2000
Assignee:
Merck Frosst Canada & Co.
Inventors:
Yongxin Han, Robert N. Young, Laurent Gil, Rejean Ruel
Abstract: The present invention is directed to certain compounds of the general structural formula: ##STR1## wherein R.sub.1, R.sub.1a, R.sub.2a, R.sub.3, R.sub.3a, R.sub.4, R.sub.5, R.sub.6, A, W, and n are as defined herein. These compounds promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such compounds as the active ingredient thereof are also disclosed.
Type:
Grant
Filed:
March 27, 1997
Date of Patent:
September 19, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Meng Hsin Chen, Gregori J. Morriello, Ravi Nargund, Arthur A. Patchett, Lihu Yang
Abstract: Compounds of this invention have the formula:X--(CH.sub.2).sub.n --C(O)NH--A--C(COOR.sup.5)R.sup.3 R.sup.4or a pharmaceutically acceptable salt thereof, e.g. ##STR1## which are useful for inhibiting fibrinogen binding to blood platelets, thereby inhibiting platelet aggregation.
Abstract: The invention relates to a bone replacement material which comprises one or more polypeptides having the biological action of fibroblast growth factors in a porous matrix. The healing-in properties correspond to those of autologous bone transplantation.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
September 12, 2000
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Inventors:
Berthold Nies, Elvira Dingeldein, Helmut Wahlig
Abstract: The present invention relates to the treatment or prevention of depression and/or anxiety by the administration of a combination of CNS-penetrant NK-1 receptor antagonists and an antidepressant or anti-anxiety agent.
Type:
Grant
Filed:
December 19, 1997
Date of Patent:
September 12, 2000
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Emma Joanne Carlson, Nadia Melanie Rupniak
Abstract: The invention relates to a thermochromic polymerizable mesogenic composition essentially consisting of:a) a component MA comprising at least one achiral polymerizable mesogenic compound comprising at least one polymerizable functional group,b) a component MB comprising at least one chiral polymerizable mesogenic compound comprising at least one polymerizable functional group,c) a photoinitiator, andd) optionally a dye component,to anisotropic polymers and polymer films with a chiral mesophase obtainable from said thermochromic polymerizable mesogenic composition and to the use of said thermochromic polymerizable mesogenic composition, anisotropic polymers and polymer films for optical information storage, photomasks, decorative pigments, cosmetics, security applications, active and passive optical elements such as polarizers or optical retarders, color filters, scattering displays, adhesives or synthetic resins with anisotropic mechanical properties.
Type:
Grant
Filed:
July 12, 1999
Date of Patent:
September 12, 2000
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Abstract: This invention relates to somatostatin agonist compounds which are potent with high selectivity toward the receptor subtype 2. The compounds provide an improved therapeutic index in the treatment of diabetes, cancer, acromegaly and retenosis. Many of the compounds are also orally active. Thus, it is an object of this invention to describe such compounds. It is a further object to describe the specific preferred stereoisomers of the somatostastin agonists. A still further object is to describe processes for the preparation of such compounds. Another object is to describe methods and compositions which use the compounds as the active ingredient thereof. Further objects will become apparent from reading the following description.
Type:
Grant
Filed:
October 28, 1998
Date of Patent:
September 12, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Liangquin Guo, Ralph T. Mosley, Alexander Pasternak, Arthur A. Patchett, Lihu Yang
Abstract: Disclosed is a binding assay for proteases and phosphatases, which contain cysteine in their binding sites or as a necessary structural component for enzymatic binding. The sulfhydryl group of cysteine is the nucleophilic group in the enzyme's mechanistic proteolytic and hydrolytic properties. The assay can be used to determine the ability of new, unknown ligands and mixtures of compounds to competitively bind with the enzyme versus a known binding agent for the enzyme, e.g., a known enzyme inhibitor. By the use of a mutant form of the natural or native wild-type enzyme, in which serine, or another amino acid, e.g., alanine, replaces cysteine, the problem of interference from extraneous oxidizing and alkylating agents in the assay procedure is overcome. The interference arises because of oxidation or alkylation of the sulfhydryl, --SH (or --S.sup.-), in the cysteine, which then adversely affects the binding ability of the enzyme.
Type:
Grant
Filed:
November 4, 1997
Date of Patent:
September 5, 2000
Assignee:
Merck Frosst Canada & Co.
Inventors:
Sylvie Desmarais, Michael Gresser, Richard Friesen, Brian Kennedy, Don Nicholson, Kathryn Skorey, Chidambaran Ramachandran, Anthony Ford-Hutchinson
Abstract: The present invention provides methods for the treatment or prevention of major depressive disorder with anxiety without concomitant therapy with other anti-depressant or anti-anxiety agents which comprises oral administration of an orally active, long acting, CNS-penetrant NK-1 receptor antagonist and pharmaceutical compositions comprising such a NK-1 receptor antagonist.
Type:
Grant
Filed:
June 11, 1998
Date of Patent:
September 5, 2000
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Raymond Baker, Neil Roy Curtis, Jason Matthew Elliott, Timothy Harrison, Gregory John Hollingworth, Philip Stephen Jackson, Janusz Jozef Kulagowski, Nadia Melanie Rupniak, Eileen Mary Seward, Christopher John Swain, Brian John Williams
Abstract: A tablet dispensing cap that allows an individual who is elderly, infirm, handicapped or visually impaired to dispense a single, non-liquid form through a single-handed operation.
Abstract: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-ben zoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
Type:
Grant
Filed:
January 4, 1999
Date of Patent:
September 5, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Lisa F. Frey, Edward J. J. Grabowski, Richard D. Tillyer
Abstract: A method is provided for making synthetic capped RNAs. These compounds serve as substrates for the virally encoded endonuclease associated with influenza virus. We are able to assay for this unique and specific viral activity of cleavage of a capped RNA in vitro. Therefore, screening of inhibitors of this activity is possible. In addition, short non-extendible (due to their length or because of the modification of the 3'-end of the oligo, i.e. 3'-dA) RNAs are potent inhibitors of the cleavage of capped RNAs by influenza endonuclease. Finally, these compounds may be used to investigate viral and cellular mechanisms of transcription/translation or mRNA maturation.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
August 29, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Fritz Benseler, James L. Cole, David B. Olsen, Lawrence C. Kuo
Abstract: Natural products such as certain chaetochromins are described. These compounds are useful in the inhibition of HIV integrase, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
Type:
Grant
Filed:
February 4, 1998
Date of Patent:
August 29, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Russell B. Lingham, Ali Shafiee, Keith C. Silverman, Ana M. Teran, Sheo Bux Singh, Deborah L. Zink
Abstract: Histone deacetylase inhibition provides a target for identifying potential antiprotozoal compounds. Histone deacetylase inhibitors are useful as therapeutic agents against protozoal infections.
Type:
Grant
Filed:
September 20, 1996
Date of Patent:
August 29, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Paula M. Dulski, Robert W. Myers, Anne M. Gumett, Sandra J. Rattray, Dennis M. Schmatz
Abstract: The present invention relates to porous implant materials which are loaded with an excipient/active compound combination, the excipient components used being oligomeric esters of polyhydric alcohols and .alpha.-hydroxy acids.
Type:
Grant
Filed:
June 22, 1998
Date of Patent:
August 29, 2000
Assignee:
Merck Patent Gesellschaft mit Beschrankter Haftung
Abstract: In accordance with the present invention, there are provided nucleic acids encoding human NMDA receptor protein subunits and the proteins encoded thereby. The NMDA receptor subunits of the invention comprise components of NMDA receptors that have cation-selective channels and bind glutamate and NMDA. In one aspect of the invention, the nucleic acids encode NMDAR1 and NMDAR2 subunits of human NMDA receptors. In a preferred embodiment, the invention nucleic acids encode NMDAR1, NMDAR2A, NMDAR2B, NMDAR2C and NMDAR2D subunits of human NMDA receptors. In addition to being useful for the production of NMDA receptor subunit proteins, these nucleic acids are also useful as probes, thus enabling those skilled in the art, without undue experimentation, to identify and isolate related human receptor subunits.
Abstract: Thienopyrimidines of the formula I ##STR1## and the physiologically acceptable salts thereof in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and n have the meanings given in Claim 1inhibit phosphodiesterase V and can be employed for the treatment of diseases of the cardiovascular system and for the therapy of impaired potency.
Type:
Grant
Filed:
February 9, 1999
Date of Patent:
August 29, 2000
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Jonas Rochus, Pierre Schelling, Franz-Werner Kluxen, Maria Christadler
Abstract: Anisotropic compounds of the formula (1) specified in claim 1 are suitable, owing to their low .DELTA..epsilon./.epsilon..perp. values for liquid crystal displays which have high information densities of for examples up to 10.sup.6 image dots and accordingly need to be highly multiplexible; compared with known compounds they offer improved application properties and are relatively simple to synthesize.
Type:
Grant
Filed:
April 1, 1993
Date of Patent:
September 5, 2000
Assignee:
Merck Patent GmbH
Inventors:
Hans P. Schad, Stephen M. Kelly, Eike Poetsch, Reinhard Hittich, Georg Weber