Abstract: Pyrimidinone, oxazolidinone, and (alkyl)aryl derivatives, their synthesis, and their use as alpha 1a adrenergic receptor antagonists are disclosed. 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 are achieved.
Abstract: Herpes Zoster, or varicella related post herpetic neuralgia is alleviated by immunizing people at risk of developing herpes zoster with varicella zoster virus (VZV) antigen.
Type:
Grant
Filed:
August 11, 1999
Date of Patent:
April 10, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Gary B. Calandra, Philip J. Provost, Myron J. Levin, C. Jo White
Abstract: A class of substituted aminocyclohexane derivatives are selective agonists of 5-HT1-like receptors, being potent agonists of the human 5-HT1D&agr; receptor subtype while possessing at least a 10-fold selective affinity for the 5-HT1D&agr; receptor subtype relative to the 5-HT1D&bgr; subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, while eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.
Type:
Grant
Filed:
January 4, 1999
Date of Patent:
April 3, 2001
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Angus Murray MacLeod, Graham Andrew Showell, Leslie Joseph Street
Abstract: The present invention is a method for diagnosing a patient at risk to thrombocytopenia induced by administration of a GP IIb/IIIa receptor antagonist, which comprises combining
i) a plasma sample of the patient;
ii) detectable monoclonal antibody which recognizes induced binding sites formed on the GP IIb/IIIa receptor following association of a fibrinogen receptor antagonist with the GP IIb/IIIa receptor; and
iii) GP IIb/IIIa receptor:GP IIb/III receptor antagonist complex,
and determining association of the detectable monoclonal antibody with the complex in the presence of the plasma.
Type:
Grant
Filed:
October 13, 1998
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Bohumil Bednar, Daniel M. Bollag, Robert J. Gould
Abstract: The invention relates to novel lithium fluorophosphates of the general formula
Li+[PFa(CHbFc(CF3)d)e]−, (I)
wherein
a is 1, 2, 3, 4 or 5,
b is 0 or 1,
c is 0, 1, 2 or 3,
d is 0, 1, 2 or 3 and
e is 1, 2, 3 or 4,
with the condition that the sum of a+e is equal to 6, the sum of b+c+d is equal to 3 and b and c are not simultaneously 0, with the proviso that the ligands (CHbFc(CF3)d) may be different,
a process for producing said compounds, their use in electrolytes, and also lithium batteries produced using said electrolytes.
Type:
Grant
Filed:
March 8, 2000
Date of Patent:
April 3, 2001
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Type:
Grant
Filed:
October 26, 1998
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
Abstract: The invention encompasses compounds of Formula I as well as a method of treating COX-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 COX-2 mediated diseases comprising compounds of Formula I.
Type:
Grant
Filed:
April 28, 2000
Date of Patent:
April 3, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Cheuk Kun Lau, Chun-Sing Li, Cameron Black, Michel Therien, Jacques Yves Gauthier
Abstract: Transgenic non-human mammals which express in their brains a nucleic acid construct comprising a DNA sequence encoding a human amyloid precursor protein FAD variant where at amino acid position 717 valine is substituted by isoleucine. These transgenic non-human mammals can be assays systems for determining compounds which are effective in modulating production of human amyloid precursor protein in brain and in isolated neuronal cells. Specifically exemplified are transgenic mice whose genome comprises a DNA sequence encoding a human amyloid precursor protein FAD variant where at amino acid position 717 valine is substituted by isoleucine operably linked to a Thy-1 promoter. The mice are shown to produce the APP-FAD variant in their brains by mRNA and protein assays.
Type:
Grant
Filed:
April 28, 1997
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Gurparlash Singh, Howard Y. Chen, Robert P. Heavens, Dalip J. S. Sirinathsinghji, David W. Smith, Myrna E. Trumbauer, Leonardus H. T. Van Der Ploeg, Aurawan Vongs, Hui Zheng
Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as vitronectin receptor antagonists. The vitronectin receptor antagonist compounds of the present invention are &agr;v&bgr;3 antagonists, &agr;v&bgr;5 antagonists or dual &agr;v&bgr;3/&agr;v&bgr;5 antagonists useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation and tumor growth.
Type:
Grant
Filed:
June 14, 1999
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, George D. Hartman, William F. Hoffman, Robert S. Meissner, James J. Perkins, Ben C. Askew, Paul J. Coleman, John J. Hutchinson, Adel M. Naylor-Olsen
Abstract: The present invention is directed to certain naphtho-fused lactams of the general structural formula:
wherein and R1, R1a, R1b, R2a, R2b, R3a, R4, R5, R6, A, L, X, n, p and w 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.
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;&ngr;&bgr;3, &agr;&ngr;&bgr;5, and/or &agr;&ngr;&bgr;6 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, wound healing, viral disease, tumor growth, and metastasis.
Type:
Grant
Filed:
December 15, 1998
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, James J. Perkins, Robert S. Meissner
Abstract: Supertwist liquid crystal displays having very short switching times are obtained if the nematic liquid crystal mixture contains at least one component chosen from group A consisting of compounds of the formulae AI to AVI:
wherein R1 and R2 in each case independently of one another are each R and R is alkyl having 1-12 C atoms, wherein one or two non-adjacent CH2 groups can also be replaced by —O—, —CH═CH—, —CO—, —O—CO— or —CO—O—, and up to four other components.
Type:
Grant
Filed:
December 8, 1998
Date of Patent:
April 3, 2001
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Georg Weber, Herbert Plach, Takamasa Oyama, Hiroki Yoshitake, Bernhard Scheuble, Reinhard Hittich, Hans Adolf Kurmeier, Eike Poetsch, Klaus Peter Stahl
Abstract: Compositions are provided for improving the stability of live virus vaccines containing, e.g., live varicella zoster, measles, mumps, and rubella viruses. Such improved stabilizers are aqueous solutions containing recombinant human serum albumin (rHA) as a component at from 1-100 g/l. Live virus vaccines as well as methods of preparing live virus vaccines containing the stabilizers are also provided.
Abstract: Compounds and methods for treating prostaglandin mediated diseases, and certain pharmaceutical compositions thereof are disclosed. The compounds are represented by formula II:
Ar1—W—Ar2—X—Q II
The compounds of the invention are structurally different from NSAIDs and opiates, and are antagonists of the pain and inflammatory effects of E-type prostaglandins.
Type:
Grant
Filed:
October 4, 1999
Date of Patent:
April 3, 2001
Assignee:
Merck Frosst Canada & Co.
Inventors:
Michel Belley, Marc Labelle, Nicholas Lachance, Michel Gallant, Nathalie Chauret, Laird A. Trimble, Chun Li
Abstract: The invention relates to cholesteric polymer flakes obtainable from a chiral polymerizable mesogenic material, to methods of manufacturing such cholesteric flakes, to the use of certain chiral and achiral polymerizable compounds with one or more terminal polymerizable groups for the manufacturing of such flakes and to the use of such cholesteric flakes as effect pigments in spraying or printing inks or paints or colored plastics for different applications, especially for automotive use, cosmetic products and security applications.
Type:
Grant
Filed:
August 14, 1998
Date of Patent:
March 27, 2001
Assignee:
Merck Patent GmbH
Inventors:
David Coates, Mark Goulding, Alison May
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:
July 24, 1998
Date of Patent:
March 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Daniel R. Sidler, Michel Chartrain, Norihiro Ikemoto, Gerald F. Bills, Christopher Roberge, Colleen S. Taylor
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
Pharmaceutical compositions and methods of use are also included.
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
July 21, 1999
Date of Patent:
March 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
Abstract: The invention relates to biocement pastes based on tricalcium phosphate and materials which are suitable for preventing or reducing the tendencies of the settable pastes to disintegrate and for improving their cohesion properties, with the result that improved processing of said pastes in the preparation of synthetic bone cements is ensured.
Type:
Grant
Filed:
April 16, 1999
Date of Patent:
March 27, 2001
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: We have modified PE40 toxin by removing at least two of its four cysteine amino acid residues and have formed hybrid molecules containing modified PE40 linked to a cell recognition protein that can be an antibody, a growth factor, a hormone, a lymphokine, or another polypeptide cell recognition protein for which a specific cellular receptor exists whereby the modified PE40 toxin is directed to cell types having receptors for the cell recognition protein linked to the modified PE40.
Type:
Grant
Filed:
February 10, 1997
Date of Patent:
March 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Allen I. Oliff, Gwynneth M. Edwards, Deborah D. Jones