Abstract: In the present invention, viruses, plasmids or both are constructed which contain viral DNA and lox sites positioned such that site-specific recombination between lox sites in separate plasmids results in generation of infectious viral DNA at high-efficiency in cotransfected host cells that have been engineered to express the Cre recombinase. Because of the high-efficiency and specificity of the Cre enzyme, suitably engineered plasmids can be readily recombined to produce infectious virus at high-efficiency in cotransfected 293 cells, without, at the same time, producing wild-type adenovirus, with the attendant problems for removal thereof. Use of recombinases besides Cre and recombinase recognition sites besides lox sites, and use of cells other than 293 cells are also disclosed and enabled, as are kits incorporating the site-specific vector system, as well as compositions and methods for using such compositions as vaccines or in gene therapeutic applications.
Type:
Grant
Filed:
March 5, 1999
Date of Patent:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Frank L. Graham, Robin J. Parks, Philip Ng
Abstract: The recovery of iodide from chemical process wastewater is accomplished by loading the wastewater containing iodide onto a strongly basic anion-exchange resin in free-base form; eluting the sorbed iodide from the resin with aqueous strong acid (e.g., hydrochloric acid); loading the iodide-rich cuts onto a weakly basic anion-exchange resin in free-base form; and eluting the sorbed iodide with aqueous base (e.g., sodium hydroxide). The recovered iodide typically has sufficient purity to permit its re-use in the chemical process.
Type:
Grant
Filed:
September 13, 1999
Date of Patent:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Ed Venkat, Ralph J. Magliette, Donald McKinney, Alan S. Michaels
Abstract: The monkey GnRH receptor has been isolated, cloned and sequenced. The monkey GnRH receptor may be used to screen and identify compounds which bind to the GnRH receptor. Such identified compounds may be used in the treatment of sex hormone related conditions such as endometriosis, uterine fibroids, polycystic ovarian disease, hirsutism, precocious puberty, gonadal steroid-dependent neoplasias such as cancers of the prostate, breast and ovary, gonadotrophe pituitary adenomas, sleep apnea, irritable bowel syndrome, premenstrual syndrome and benign prostatic hypertrophy. The receptor proteins and polypeptides, nucleic acids, cells and assays of this invention are useful in drug screening and development, diagnosis and therapeutic applications.
Type:
Grant
Filed:
February 10, 2000
Date of Patent:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jisong Cui, Jane-Ling Lo, George R. Mount
Abstract: Substituted 5-aryl-2,4-thiazolidinediones and oxazolidinediones are potent agonists of PPAR, and are therefore useful in the treatment, control or prevention of diabetes, hyperglycemia, hyperlipidemia (including hypercholesterolemia and hypertriglyceridemia), atherosclerosis, obesity, vascular restenosis, and other PPAR &agr; and/or &ggr; mediated diseases, disorders and conditions.
Type:
Grant
Filed:
June 16, 2000
Date of Patent:
April 30, 2002
Assignee:
Merck & Co. Inc.
Inventors:
Ranjit C. Desai, Soumya P. Sahoo, Jeffrey P. Bergman, Victoria K. Lombardo, Edward J. Metzger, Hiroo Koyama
Abstract: 4-substituted cyclohexanes substituted in the 1-position with quinazoline either directly or through a C1-C4alkyl, C1-C4alkenyl, C1-C4alkynyl, C1-C4alkoxy, amino, aminoC1-C4alkyl, hydroxyC1-C4alkyl, carbonyl, cycloC3-C6alkyl or aminocarbonyl chain are effective as NMDA NR2B antagonists useful for relieving pain.
Type:
Grant
Filed:
May 21, 2001
Date of Patent:
April 30, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Wayne Thompson, David A. Claremon, Peter M. Munson, John A. McCauley
Abstract: The present invention is directed to peptidomimetic compounds which inhibit prenyl-protein transferase 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.
Abstract: Novel compounds of the formula I
in which
X, R1, R2, R3, R4 and R5 have the meaning indicated in Patent Claim 1,
are inhibitors of the coagulation factor Xa and can be employed for the prophylaxis and/or therapy of thromboembolic disorders.
Type:
Grant
Filed:
December 29, 2000
Date of Patent:
April 30, 2002
Assignee:
Merck Patent Gesellschaft mit beschraenkterHaftung
Inventors:
Dieter Dorsch, Horst Juraszyk, Werner Mederski, Joachim Gante, Hanns Wurziger, Hans-Peter Buchstaller, Sabine Bernotat-Danielowski, Guido Melzer
Abstract: Certain six-membered aromatic and heteroaromatic-dioxobutyric acid derivatives are described as inhibitors of HIV integrase and inhibitors of HIV replication. These compounds are useful in 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:
June 1, 1999
Date of Patent:
April 30, 2002
Assignees:
Merck & Co., Inc., Tularik Inc.
Inventors:
Steven D. Young, Melissa Egbertson, Linda S. Payne, John S. Wai, Thorsten E. Fisher, James P. Guare, Jr., Mark W. Embrey, Lekhanh Tran, Linghang Zhuang, Joseph P. Vacca, H. Marie Langford, Jeffrey Melamed, Juan C. Jaen, David L. Clark, Julio C. Medina
Abstract: The invention relates to a liquid crystal display device comprising a liquid crystal cell and at least one compensation film or a combination of polarizer and optical compensators comprising at least one compensation film, said compensation film comprising at least one layer of an isotropic polymer obtainable by polymerization of a mixture of a polymerizable mesogenic material comprising:
a) compound having one or two more polymerizable functional group, in the presences
b) an initiator,
c) optionally a non-polymerizable compound having two or more polymerizable functional groups and
d) optionally a stabilizer,
characterized in that said layer of an anisotropic polymer has a hometropic or tilted hometropic molecular orientation. The invention also relates to methods of manufacturing said compensation films. The invention further relates to mixtures of chiral polymerizable mesogenic material used for manufacturing of said compensation films.
Type:
Grant
Filed:
December 30, 1998
Date of Patent:
April 30, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Abstract: A group of compounds of, the preparation of, and the methods of use of benzoylpyridazine derivatives and the physiologically acceptable salts and solvates thereof, which have valuable pharmacological properties while well tolerated. They selectively inhibit phosphodiesterase IV with an intracellular increase in the CAMP level, and have an inhibitory effect on the formation of tumor necrosis factor.
Type:
Grant
Filed:
May 3, 2001
Date of Patent:
April 23, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Rochus Jonas, Michael Wolf, Franz-Werner Kluxen
Abstract: This invention relates to certain novel compounds and derivatives thereof, their synthesis, and their use as alpha 1a adrenergic receptor antagonists. 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: The present invention comprises piperazine-containing compounds which inhibit prenyl-protein transferases, including farnesyl-protein transferase and geranylgeranyl-protein transferase type I. Such therapeutic compounds are useful in the treatment of cancer.
Type:
Grant
Filed:
March 1, 2000
Date of Patent:
April 23, 2002
Assignee:
Merck & Co., Inc.
Inventors:
George D. Hartman, William C. Lumma, Jr., John T. Sisko, Anthony M. Smith, Thomas J. Tucker, Jeffrey M. Bergman
Abstract: Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure:
or a pharmaceutically acceptable salt thereof, wherein b is N Y1 or O; c is CY2 or N; d is CY2; e is CY1 or N; f is CY1 or N; g is CY1 or N; Y1 is hydrogen, C1-4 alkyl, or halogen; Y2 is hydrogen, C1-4 alkyl, C3-7 cycloalkyl, halogen, NH2, OH or C1-4 alkoxy;
A is
and W, X, Z, R3, R4 and R5 are defined in the specification.
Type:
Grant
Filed:
October 28, 1999
Date of Patent:
April 23, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Philip E. Sanderson, Terry Lyle, Bruce Dorsey, Matthew G. Stanton, Adel M. Naylor-Olsen
Abstract: The inhibition of natural bone formation experienced in the prophylaxis and/or treatment of bone resorption disease with a bisphosphonic acid or a pharmaceutically acceptable salt thereof is overcome by the concommitant administration of an agent that binds to the androgen receptor.
Abstract: Piperazine derivatives of formula (I)
wherein
Z, X, n, Ar and i have the meanings defined herein are usefull in the treatment of pathologies associated with insulin-resistance syndrome.
Abstract: The invention encompasses novel compounds of Formula I as well as a method of treating NMDA mediated diseases comprising administration to a patient in need of such treatment a non-toxic amount of a compound of Formula I effective to block the NMDA NR2B receptor sub-unit.
The invention also encompasses certain pharmaceutical compositions for the treatment of NMDA mediated diseases comprising compounds of Formula I and a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
April 17, 2000
Date of Patent:
April 23, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
Abstract: Nematic liquid-crystal compositions of negative dielectric anisotropy comprising compounds of the formula I
are useful in plasma-addressed liquid-crystal displays.
Type:
Grant
Filed:
September 13, 1999
Date of Patent:
April 23, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung