Abstract: The present invention is directed to a dual compartment, mixing and dispensing device suitable for the containment of two separate pharmaceutical components that mixable, upon breaking of a seal that separates the compartments, to provide an instantly mixed dose of medication. The medication can be administered to a patient through an aperture located at one end of the device. The device is characterized as two compartments connected by a flexible, sealed orifice, wherein the two components are separated. Flexing of the device at the orifice breaks the seal and allows mixing of the components to prepare the dose. Thereafter, an end-portion of the device can be opened for oral administration of the dose.
Abstract: Disclosed are methods for inhibiting bone resorption in mammals while minimizing the occurrence of or potential for adverse gastrointestinal effects. Also disclosed are pharmaceutical compositions and kits for carrying out the therapeutic methods disclosed herein.
Type:
Grant
Filed:
January 8, 2001
Date of Patent:
April 8, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Anastasia G. Daifotis, Arthur C. Santora, II, A. John Yates
Abstract: A device suitable for dispensing a plurality of like articles therefrom, the device characterized as having a plurality of columns for storing and dispensing the articles, each column having a front opening for dispensing the articles and a bottom side for holding the articles, each column having resilient spring means for biasing the articles towards the front opening of the column, the improvement being a tilt ramp attached to the front opening, wherein the ramp is at a decreased angle.
Abstract: The present invention is directed to peptidomimetic macrocyclic 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.
Type:
Grant
Filed:
April 6, 2001
Date of Patent:
March 18, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Diem N. Nguyen, Craig A. Stump, Theresa M. Williams
Abstract: There is disclosed an adsorption powder effective for capturing mercury from a high temperature, high moisture gas stream comprising: about 1-97% carbon; about 1-97% calcium hydroxide; about 1-97% cupric chloride impregnated carbon, and about 1-60% carbon impregnated with KI3. Additionally, a method of removing mercury from high temperature, high moisture gas streams is disclosed.
Type:
Grant
Filed:
February 24, 2000
Date of Patent:
March 18, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Rudy J. Maes, Youssef El-Shoubary, Subash Seth
Abstract: The present invention relates to novel cysteine protease inhibitors of Formula I:
the pharmaceutically acceptable salts and N-oxide derivatives thereof, their use as therapeutic agents and methods of making them.
Type:
Grant
Filed:
January 5, 2001
Date of Patent:
February 25, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Renata Marcella Oballa, Petpiboon Prasit, Joel Stephane Robichaud, Elise Isabel, Eduardo Setti, Dan-Xiong Wang, Rohan V. Mendonca, Shankar Venkatraman
Abstract: The present invention is directed to peptidomimetic macrocyclic 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.
Type:
Grant
Filed:
January 9, 2001
Date of Patent:
February 25, 2003
Assignee:
Merck & Co., Inc.
Inventors:
S. Jane deSolms, Suzanne C. MacTough, Anthony W. Shaw
Abstract: A process for removing mercury and organic compounds from gaseous stream using an adsorption powder, characterized as containing a carbon-based powder and an effective amount of cupric chloride, the process characterized by the steps of:
a) placing a solid phase mercury-containing contaminated soil into a rotary kiln/drum;
b) heating the kiln/drum to form gaseous and solid components of the soil;
c) transferring the gaseous component to an exhaust cleaning unit/afterburner, and transferring the soil component to a cooling unit;
d) heating the gaseous component in the exhaust cleaning unit/afterburner;
e) cooling the gaseous component;
f) adding the adsorption powder to the gaseous component;
g) transferring the powder-containing, gaseous component to a baghouse; and
h) releasing the substantially mercury-free gaseous component to the atmosphere.
Type:
Grant
Filed:
July 10, 2001
Date of Patent:
February 25, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Youssef El-Shoubary, Rudy Maes, Subash C. Seth
Abstract: Pharmaceutical compositions of bisphosphonic acids, and salts thereof, are prepared by direct compression/dry mix 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.
Type:
Grant
Filed:
October 19, 2001
Date of Patent:
February 11, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Simon R. Bechard, Kenneth A. Kramer, Ashok V. Katdare
Abstract: The present invention relates to novel crystalline forms of the integrin &agr;v&bgr;3 antagonist 3-{2-oxo-3-[3-(5,6,7,8-tetrahydro-[1,8]naphthyridin-2-yl)-propyl]imidazolidin-1-yl}-3(S)-(6-methoxy-pyridin-3-yl)-propionic acid.
Abstract: A process for the direct crystallization of a compound of the formula I:
or a pharmaceutically acceptable salt thereof, is disclosed, wherein R1 and R2 represent H, C1-10 alkyl, aryl or heteroaryl, or substituted C1-10 alkyl, aryl or heteroaryl and X+ represents a charge balancing group, comprising extracting a solution containing a crude compound of formula I or Ia:
or a pharmaceutically acceptable salt thereof, wherein each X+ is a charge balancing group, and R1 and R2 are as described above with a C4-10 alcohol, collecting and crystallizing the resulting aqueous phase to produce a crystalline compound of formula I.
Type:
Grant
Filed:
January 19, 2000
Date of Patent:
January 7, 2003
Assignee:
Merck & Co., Inc.
Inventors:
John M. Williams, Karel M. J. Brands, Renato T. Skerlj, Peter Houghton
Abstract: There is disclosed an apparatus and method for evenly dispersing the contents of powder filled bulk bags, in order to create a flat, even, horizontal bulk bag surface for efficient attachment to the suction head of a vacuum lift.
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and treatment of cancer.
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 protein 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 24, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Helen M. Armstrong, Richard Beresis, Joung L. Goulet, Mark A. Holmes, Xingfang Hong, Sander G. Mills, William H. Parsons, Peter J. Sinclair, Mark G. Steiner, Frederick Wong, Dennis M. Zaller
Abstract:
A process of synthesizing a carbapenem compound of formula (6) is disclosed, wherein R represents H or methyl, P and P* independently represent H or protecting groups and each R1 is independently selected from: H, halo, OH, OP wherein P is a protecting group, C1-6 alkyl or C1-6 alkyl substituted with 1-3 of halo, OH, OP, NH2, NHC1-4 alkyl or N(C1-4 alkyl)2, comprising reacting a carbapenem of formula (4′) with a compound of formula (7), wherein R, R1, P and P* are as previously defined and R2 represents acetate, C(O)OR′ or P(O)(OR″)2, wherein R′ and R″ independently represent Clot alkyl, benzyl or aryl, in the presence of a catalyst to produce a compound of formula (6).
Type:
Grant
Filed:
March 5, 2001
Date of Patent:
December 3, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Guy R. Humphrey, Ross A. Miller, Nobuyoshi Yasuda
Abstract: The present invention involves a process for preparing a stable final formulation product of a compound of formula I,
or its pharmaceutically acceptable salt, hydrate or solvate by incorporating a suitable carbon dioxide source to an unstable monosodium adduct of carbapenem antibiotic compound.
Type:
Grant
Filed:
April 27, 2001
Date of Patent:
November 26, 2002
Assignee:
Merck & Co., Inc.
Inventors:
William A. Hunke, Kathleen J. Illig, Anand Kanike, Scott D. Reynolds, Stelios C. Tsinontides, Anthony S. Al-Dehneh, Hiren S. Patel
Abstract: Crystalline 2S-cis-3-[[(4-mercapto-2-pyrrolidinyl)carbonyl]-amino]benzoic acid and salts and solvates thereof are disclosed. A crystalline type is described.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Karel J. M. Brands, Karen M. Conrad, John M. Williams
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:
October 17, 2000
Date of Patent:
November 12, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Scott R. Hambaugh, Randall W. Hungate
Abstract: The present invention relates to novel imidazolidinone 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, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.
Type:
Grant
Filed:
January 19, 2001
Date of Patent:
October 29, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Duggan, Wasyl Halczenko, John H. Hutchinson, Aiwen Li, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Jiabing Wang, Michael A. Patane