Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tryrosine kinase-dependent diseases/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
Type:
Grant
Filed:
February 28, 2001
Date of Patent:
October 15, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Mark T. Bilodeau, Randall W. Hungate, April M. Cunningham, Timothy J. Koester
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:
Application
Filed:
February 1, 2002
Publication date:
October 10, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Mark T. Bilodeau, George D. Hartman, Peter J. Manley
Abstract: Genes encoding herpes simplex virus type 2 (HSV-2) proteins were cloned into eukaryotic expression vectors to express the encoded proteins in mammalian muscle cells in vivo. Animals were immunized by injection of these DNA constructs, termed polynucleotide vaccines or PNV, into their muscles. In a DNA titration, it was found that a single immunization of ≧0.5 &mgr;g of (one) PNV, gave >90% seroconversion by ten weeks post immunization. Immune antisera neutralized both HSV-2 and HSV-1 in cell culture. When animals were challenged with HSV-2, significant (p<0.001) protection from lethal infection was achieved following PNV vaccination. DNA constructs may be full-length, truncated and/or mutated forms and may be delivered along or in combination in order to optimize immunization and protection from HSV infection.
Type:
Application
Filed:
April 16, 2001
Publication date:
October 10, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Marcy E. Armstrong, Robert D. Keys, John A. Lewis, Margaret A. Liu, William L. McClements
Abstract: There is disclosed a pinch valve for allowing access to a sterile reaction vessel using a cannula. The valve remains closed until a cannula is inserted. Upon removal of the cannula, the valve automatically closes maintaining the sterile or otherwise controlled conditions of the reaction vessel.
Abstract: The invention relates to novel oxazolidine derivatives of the formula
in which R1, R2 and R3 have the meanings stated in claim 1, their salts and processes for preparing the compounds according to the invention.
The compounds of the formula I act as 5-HT2A antagonists with a 5-HT reuptake-inhibiting, antidepressant or anxiolytic effect and can be used to produce pharmaceuticals.
Type:
Grant
Filed:
August 25, 1999
Date of Patent:
October 8, 2002
Assignee:
Merck Patent Gesellschaft mit beschrankter Haftung
Inventors:
Henning Böttcher, Helmut Prücher, Hartmut Greiner, Gerd Bartoszyk, Christoph Seyfried
Abstract: A tachykinin receptor antagonist is useful for alleviating or managing symptoms associated with premenstrual syndrome in a woman, in particular, for the treatment or prevention of disturbances of appetite, disturbances of mood, or both, associated with premenstrual syndrome.
Abstract: Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment and control of obesity, diabetes, and sexual dysfunction, including erectile dysfunction and female sexual dysfunction.
Type:
Grant
Filed:
March 20, 2001
Date of Patent:
October 1, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Brenda L. Palucki, Khaled J. Barakat, Liangqin Guo, Yingjie Lai, Ravi P. Nargund, Min K. Park, Patrick G. Pollard, Iyassu K. Sebhat, Zhixiong Ye
Abstract: A micro mixer for liquid, viscous or gaseous phases with two adjacent housing parts (1,2) disposed on a parting plane (3). Capillary tubes (7) forming line connections are inserted into cross holes (6) in the top part of the housing (1) by welding, for instance, and run into the parting plane (3). The other free ends of the capillary tubes (7) are bent apart and respectively bear a screw connection.
Type:
Grant
Filed:
May 26, 2000
Date of Patent:
October 1, 2002
Assignee:
Merck Patent Gesellschaft mit
Inventors:
Andreas Beirau, Michael Schmelz, Frank Schwarz, Jöran Stoldt
Abstract: This invention relates to a novel estrogen receptor and to the polynucleotide sequences encoding this receptor. This invention also relates to methods for identifying ligands which bind to this receptor, to the ligands so identified, and to pharmaceutical compositions comprising such ligands. This invention also relates to pharmaceutical compositions useful for treating or preventing estrogen receptor mediated diseases or conditions, such as abnormal bone resorption, cardiovascular diseases, cancer, or central nervous system disorders.
Abstract: The inventive micromixer for mixing liquid, viscous or gaseous phases has a housing bottom part (2) and a housing top part (3) which lie closely against each other via connecting surfaces (6, 7). Two delivery channels (1a, 1b) and an outlet channel (5) open out into the dividing surface between the two connecting surface (6, 7). Channel grooves (9, 10) which cross each other several times are formed in one connecting surfaces (6) and provide a mixing section for the phases being mixed.
Type:
Grant
Filed:
April 24, 2000
Date of Patent:
October 1, 2002
Assignee:
Merck Patent Gesellschaft mit
Inventors:
Ulrich Koop, Michael Schmelz, Andreas Beirau
Abstract: The present invention relates to compounds of the formula (I):
wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and n are defined herein. The compounds are of particular use in the treatment or prevention of depression, anxiety, pain, inflammation, migraine, emesis and postherpetic neuralgia.
Type:
Grant
Filed:
September 10, 2001
Date of Patent:
October 1, 2002
Assignee:
Merck Sharp & Dohme Ltd.
Inventors:
Simon Neil Owen, Eileen Mary Seward, Christopher John Swain, Brian John Williams
Abstract: The present invention is directed toward radiolabeled farnesyl-protein transferase inhibitor compounds which are useful to label FPTase in assays, whether cell-based, tissue-based or in whole animal. The tracers can also be used in competitive binding assays to obtain information on the interaction of unlabeled FTIs with FPTase.
Type:
Grant
Filed:
June 12, 2000
Date of Patent:
October 1, 2002
Assignee:
Merck & Co., Inc.
Inventors:
H. Donald Burns, Terence G. Hamill, Raymond E. Gibson
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 is related to a drug delivery device, that is pH insensitive, for the sustained in situ production and release of a dispersion, in an environment of use, which comprises
Type:
Application
Filed:
March 12, 2002
Publication date:
September 26, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Michael W. McGlynn, Mandana Asgharnejad
Abstract: Certain novel substituted piperidine compounds are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction. Also provided are methods of treating sexual dysfunction with a compound that is a selective agonist of MC-4R over any other human melanocortin receptor.
Type:
Application
Filed:
November 21, 2001
Publication date:
September 26, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Raman K. Bakshi, Khaled J. Barakat, Ravi P. Nargund, Brenda L. Palucki, Arthur A. Patchett, Iyassu Sebhat, Zhixiong Ye, Leonardus H.T. Van Der Ploeg
Abstract: The present invention provides mice that have had their PTP-1B genes disrupted by targeted homologous recombination. The mice have no detectable PTP-1B protein, yet appear to be physiologically normal. However, in the fed state on a normal diet, the mice have half the level of circulating insulin as their wild-type littermates. In glucose and insulin tolerance tests, the mice show an increased insulin sensitivity. When fed a high fat, high carbohydrate diet, the mice show a resistance to weight gain as compared to their wild-type littermates.
Type:
Application
Filed:
July 30, 2001
Publication date:
September 26, 2002
Applicant:
Merck & Co., Inc.
Inventors:
Brian Kennedy, Paul Payette, Michael Gresser, Chidambaram Ramachandran, Michel Tremblay, Mounib Elchebly
Abstract: The present invention is directed to pyrrolidine compounds of the formula I:
(wherein R1, R2, R3, R4c, R4d, and R4f are defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptors CCR-3 and/or CCR-5.
Type:
Grant
Filed:
February 27, 2001
Date of Patent:
September 24, 2002
Assignee:
Merck & Co., Inc.
Inventors:
Jennifer Chee, Jill N. Johanson, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht
Abstract: A combination of a muscarinic agonist and an inverse agonist of the GABAA &agr;5 receptor subtype useful in treating neurodegenerative conditions such as Alzheimer's Disease is disclosed.