Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
April 18, 2002
Date of Patent:
September 21, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Kenneth L. Arrington, Mark T. Bilodeau, George D. Hartman, William F. Hoffman, Yuntae Kim, Randall W. Hungate
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;v&bgr;3, &agr;v&bgr;5, and/or &agr;v&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:
July 27, 2001
Date of Patent:
August 31, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Ben C. Askew, Paul J. Coleman, Mark E. Duggan, Wasyl Halczenko, George D. Hartman, Cecilia A. Hunt, John H. Hutchinson, Robert S. Meissner, Michael A. Patane, Garry R. Smith, Jiabing Wang
Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restenosis, gynecomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
Type:
Grant
Filed:
April 11, 2002
Date of Patent:
June 15, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Frank P. DiNinno, Jane Y. Wu, Seongkon Kim, Helen Y. Chen
Abstract: The tris(hydroxymethyl)aminomethane (“TRIS”) salt of 3-(pyrimidin-5-yl)-9-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-nonanoic acid is a potent antagonist of the integrin &agr;v&bgr;3 receptor and is useful for the prevention and/or treatment of osteoporosis and vascular restenosis, as well as conditions associated with excessive angiogenesis, such as macular degeneration, diabetic retinopathy, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth. The invention also relates to a process for the preparation of the novel salt as well as pharmaceutical compositions containing the salt and methods of using the salt.
Abstract: An apparatus and process for automatically, repetitively sampling blood from conscious animals. The apparatus can simultaneously extract blood from a number of conscious, catherized animals at programmable time intervals. The apparatus is characterized as a system of computer controlled valves and pumps connected by tubing filled with saline solution to a catherized animal. Blood samples are collected via a cannula from the animal and placed in a fraction collector for analyses.
Type:
Grant
Filed:
March 14, 2001
Date of Patent:
May 18, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Kevin R. Blake, Kang Cheng, Glenn A. Clarke, Gary S. Kath, Gregory W. King, Tsuei-Ju Wu
Abstract: A stopper debris separator useful for removing unwanted debris from stoppers utilized to seal bottles of IV pharmaceutical compositions at the manufacturing process. Debris-containing stopper in the stopper injection hopper are drawn through the stopper duct into the cyclone separator tube by the vacuum wherein the debris on the stoppers is separated therefrom and drawn through the vacuum duct into the vacuum filter.
Abstract: A novel process is provided for the preparation of optionally protected 2,5-di-(3′-aminopropyl)-pyridines which are useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.
Type:
Grant
Filed:
June 5, 2002
Date of Patent:
March 16, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Nobuyoshi Yasuda, Michael Palucki, Yi Xiao, Frederick W. Hartner, Lushi Tan
Abstract: The present invention relates to oral compositions and methods for inhibiting bone resoprtion in a mammal while counteracting the occurrence of potentially adverse gastrointestinal effects. The compositions useful herein comprise the combination of a pharmaceutically effective amount of a nitrogen-containing bisphosphonate or a pharmaceutically-acceptable salt thereof and a pharmaceutically effective amount of an isoprenoid compound.
Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by wet granulation tablet formulation. These pharmaceutical compositions are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease. These compositions are prepared without the addition of binder; instead, the drug itself acts as a binder.
Abstract: The present invention relates to novel alkanoic acid derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammatory arthritis, cancer, and metastatic tumor growth.
Type:
Grant
Filed:
January 23, 2001
Date of Patent:
February 17, 2004
Assignee:
Merck & Co., Inc.
Inventors:
Ben C. Askew, Michael J. Breslin, Mark E. Duggan, John H. Hutchinson, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Michael A. Patane
Abstract: The present invention relates to orally active salts of compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angio-genesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
October 17, 2001
Date of Patent:
December 2, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Shyam B. Karki, Yuntae Kim
Abstract: The invention discloses a novel process for the preparation of enantiomerically enriched mixtures of compounds of structural formula I which are useful intermediates in the synthesis of &agr;v&bgr;3 integrin receptor antagonists
Type:
Grant
Filed:
July 17, 2002
Date of Patent:
November 11, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Nelo R. Rivera, Christopher J. Welch, Yi Xiao, Nobuyoshi Yasuda
Abstract: The present invention relates to compositions and methods of preventing or reducing the risk or incidence of skeletal injuries in horses. The present invention further relates to compositions and methods for alleviating pain associated with skeletal injuries in horses and to treating skeletal injuries in horses.
Abstract: A carbon-based, adsorption powder containing an effective amount of cupric chloride suitable for removing mercury from a high temperature, high moisture gas stream, wherein the effective amount of cupric chloride ranges from about 1 to about 45 wt percent. Additional additives, such as potassium permanganate, calcium hydroxide, potassium iodide and sulfur, may be added to the powder to enhance the removal of mercury from the gas stream.
Type:
Grant
Filed:
July 10, 2001
Date of Patent:
October 28, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Youssef El-Shoubary, Rudy Maes, Subash C. Seth
Abstract: The present invention is directed to piperazine-containing macrocyclic compounds which inhibit prenylyl-protein transferase, such as farnesyl-protein transferase (FTase), and therefore inhibit 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: This invention relates to novel substituted succinic acid metallo-&bgr;-lactamase inhibitors which are useful potentiators of &bgr;-lactam antibiotics. Accordingly, the present invention provides a method of treating bacterial infections in animals or humans which comprises administering, together with a b-lactam antibiotic, a therapeutically effective amount of a compound of formula I:
including pharmaceutically acceptable salts, prodrugs, anhydrides, and solvates thereof.
Type:
Grant
Filed:
October 26, 2000
Date of Patent:
October 7, 2003
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Mark L. Greenlee, Steven H. Olson, Gregory P. Rouen
Abstract: The present invention relates to novel pharmaceutical tablets useful for administering pharmaceutical active ingredients, such as bisphosphonates. These tablets have improved surface properties which can aid esophageal transit, thereby reducing the potential for adverse gesture intestinal effects. The present invention also relates to processes for making said novel pharmaceutical tablets.
Type:
Grant
Filed:
March 15, 2002
Date of Patent:
September 23, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Tzyy-Show H. Chen, Thomas G. Nyairo, Ashok V. Katdare
Abstract: The present invention relates to a process for preparing a compound of gonadotropin releasing hormone antagonists having a Formula I,
in an efficient way, which involves preparation of key intermediates: 2-arylindole core; a chiral aziridine, in particular chiral nosyl aziridine; and an amine salt. The key process involves the coupling reaction of 2-arylindole and nosyl aziridine under boron trifluoride catalysis, which provides the final compound with unprecedented regioselectivity and enantioselectivity.
Type:
Grant
Filed:
April 5, 2002
Date of Patent:
September 16, 2003
Assignee:
Merck & Co., Inc.
Inventors:
John Y. L. Chung, Roger N. Farr, Guy R. Humphrey
Abstract: The present invention is directed to peptidomimetic macrocyclic compounds that 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.