Patents Assigned to Merck & Co., Inc.
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Publication number: 20100152258Abstract: A compound having the structure (Formula I), wherein Y is —Y1, —Y2, —Y3, —Y4, —Y5; Y1 is C(O) or C(R1R2); Y2 is O, C(O), P(O)(OH) or CH2, provided that when Y1 is C(O), Y2 is not C(O); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the pup consisting of hydrogen, C1-4 alkyl, and —OC(O)C1-4 alkyl; Y3 is O, C(O) or CH2, provided that when Y2 is C(O), then Y3 is not C(O), and further provided that when Y2 is O, then Y3 is not O; Y4 is O or CH2 or is absent, provided that when Y3 is O, then Y4 is not O; Y5 is —(CH2)1-2—(X)0-1—(CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 11, 2007Publication date: June 17, 2010Applicant: Merck & Co. Inc.Inventors: lyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali
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Publication number: 20100152259Abstract: A compound having the structure (Formula I), wherein R an angiotensin receptor antagonist active group, Y is Y1—Y2—Y3—Y4—Y5. Y1 is C(R1R2); R1 is selected from the group consisting of hydrogen and C1-4 alkyl; R2 is selected from the group consisting of hydrogen, C1-4 alkyl, and -0C(0)C1-4 alkyl; Y2 is O or CH2; Y3 is C(O) or CH2; Y4 is O or CH2; Y5 is —(CH2)1-2—(X)0-1—CH2)0-1— or is absent; X is —O— or —CR3R4—; and R3 and R4 are independently selected from the group consisting of hydrogen and C1-C4 alkyl; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: ApplicationFiled: December 11, 2007Publication date: June 17, 2010Applicants: Merck & Co Inc., NICox S.A.Inventors: Iyassu K. Sebhat, Michael Man-chu Lo, Ravi P. Nargund, Amjad Ali, Chris Franklin, Nicoletta Almirante, Laura Storoni, Silvia Stefanini
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Publication number: 20100152278Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-1, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-1, MMP -2, MMP-3, MMP-9 and MMP-12.Type: ApplicationFiled: May 2, 2008Publication date: June 17, 2010Applicant: Merck & Co., IncInventors: Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
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Publication number: 20100145038Abstract: This invention relates to compounds, compositions, and methods useful for modulating gene expression using short interfering nucleic acid (siNA) molecules. In particular, the instant invention features small nucleic acid molecules, such as short interfering nucleic acid (siNA), short interfering RNA (siRNA), double-stranded RNA (dsRNA), micro-RNA (miRNA), and short hairpin RNA (shRNA) molecules and methods used to modulate the expression of genes, such as expressed pseudogenes associated with the maintenance or development of diseases, disorders, traits, and conditions in a subject or organism.Type: ApplicationFiled: November 9, 2009Publication date: June 10, 2010Applicant: Merck & Co., Inc.Inventors: James McSwiggen, Narendra Vaish
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Patent number: 7731962Abstract: The present invention relates to antibodies that differentially recognize multi-dimensional conformations of A?-derived diffusible ligands, also known as ADDLs. The antibodies of the invention can distinguish between Alzheimer's Disease and control human brain extracts and are useful in methods of detecting ADDLs and diagnosing Alzheimer's Disease. The present antibodies also block binding of ADDLs to neurons, assembly of ADDLS, and tau phosphorylation and are there useful in methods for the preventing and treating diseases associated with soluble oligomers of amyloid ? 1-42.Type: GrantFiled: October 17, 2006Date of Patent: June 8, 2010Assignee: Merck & Co., Inc.Inventors: Gene Kinney, William R. Strohl, Zhiqiang An
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Patent number: 7732472Abstract: The present invention relates to dihydroisoxazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: August 15, 2005Date of Patent: June 8, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Mark E. Fraley, Robert M. Garbaccio, George D. Hartman
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Publication number: 20100137406Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-I, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-1, MMP-2, MMP-3, MMP-9 and MMP-12.Type: ApplicationFiled: May 2, 2008Publication date: June 3, 2010Applicant: Merck & Co., IncInventors: Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
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Publication number: 20100137405Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-I, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-I, MMP-2, MMP-3, MMP-9 and MMP-12.Type: ApplicationFiled: May 2, 2008Publication date: June 3, 2010Applicant: Merck & Co., IncInventors: Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
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Patent number: 7723365Abstract: The present invention relates to oxadiazoles that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: August 15, 2005Date of Patent: May 25, 2010Assignees: Merck & Co., Inc., Merck Sharp & Dohme Corp.Inventors: Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio
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Publication number: 20100120895Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression and/or activity, including PDE4B1, PDE4B2, and PDE4B3 gene expression and/or activity. The present invention is also directed to compounds, compositions, and methods relating to traits, diseases and conditions that respond to the modulation of expression and/or activity of genes involved in cyclic nucleotide type 4 phosphodiesterase (PDE4B) gene expression pathways or other cellular processes that mediate the maintenance or development of such traits, diseases and conditions, including but not limited to IL-6, IL-7, IL-8, IL-15, TNF-alpha and matrix metalloproteinases (MMPs), such as MMP-I, MMP-2, MMP-3, MMP-9 and MMP-12.Type: ApplicationFiled: May 2, 2008Publication date: May 13, 2010Applicant: Merck & Co., Inc.Inventors: India Vasant Jadhav, Ivan Richards, Walter Strapps, Chandra Vargeese
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Patent number: 7714021Abstract: The present invention is directed to pyrrolidin-3-yl derivative compounds which are inhibitors of the beta-secretase enzyme and that are useful in the treatment of diseases in which the beta-secretase enzyme is involved, such as Alzheimer's disease. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases in which the beta-secretase enzyme is involved.Type: GrantFiled: June 10, 2005Date of Patent: May 11, 2010Assignee: Merck & Co., Inc.Inventor: Craig A. Coburn
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Publication number: 20100113469Abstract: This invention concerns compositions for the treatment of Lower Urinary Tract Symptoms (LUTS), and especially LUTS which results from benign prostatic hypertrophy. The compositions of the invention comprise a Beta-3 agonist described below, optionally in combination with a 5-alpha reductase inhibitor, or an NK-1 antagonist or an alpha-1 adrenergic antagonist or an anti-muscarinic agent. The invention also includes compositions comprising a beta-3 agonist and two additional active agents selected from a 5-alpha reductase inhibitor, an NK-1 antagonist, an alpha-1 adrenergic antagonist or an anti-muscarinic agent.Type: ApplicationFiled: March 25, 2008Publication date: May 6, 2010Applicant: MERCK & CO., INC.Inventors: Tara Frenkl, Stuart A. Green, Enan Macintyre, Sander G. Mills
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Publication number: 20100113492Abstract: Certain novel substituted aminopyrimidines are ligands of the human cholecystokinin receptor and, in particular, are selective ligands of the human cholecystokinin-1 receptor (CCK-1R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the modulation of CCK-1R, such as obesity, and diabetes.Type: ApplicationFiled: January 22, 2008Publication date: May 6, 2010Applicant: MERCK & CO., INC.Inventors: Scott Edmondson, David E. Kaelin, Randy Sweis
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Publication number: 20100113439Abstract: Novel derivatives of enfumafungin are disclosed herein, along with their pharmaceutically acceptable salts, hydrates and prodrugs. Also disclosed are compositions comprising such compounds, methods of preparing such compounds and methods of using such compounds as antifungal agents and/or inhibitors of (1,3)-?-D-glucan synthase. The disclosed compounds, their pharmaceutically acceptable salts, hydrates and prodrugs, as well as compositions comprising such compounds, salts, hydrates and prodrugs, are useful for treating and/or preventing fungal infections and associated diseases and conditions.Type: ApplicationFiled: August 7, 2009Publication date: May 6, 2010Applicants: Merck & Co., Inc., Scynexis, Inc.Inventors: Mark L. Greenlee, Robert Wilkening, James Apgar, Donald Sperbeck, Kenneth J. Wildonger, Dongfang Meng, Dann L. Parker, JR., Gregory J. Pacofsky, Brian H. Heasley, Ahmed Mamai, Kingsley Nelson
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Patent number: 7704988Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.Type: GrantFiled: October 4, 2006Date of Patent: April 27, 2010Assignee: Merck & Co., Inc.Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
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Patent number: 7700591Abstract: Cyclopentyl compounds linked to a benzoxazinyl group through an amido moiety utilizing the ring nitrogen of the benzoxazine, and further substituted with a heterocyclic moiety, such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.Type: GrantFiled: May 13, 2005Date of Patent: April 20, 2010Assignee: Merck & Co., Inc.Inventors: Stephen D. Goble, Sander G. Mills, Lihu Yang, Alexander Pasternak, Celine Bonnefous, Theodore M Kamenecka, Jean-Michel Vernier, John H. Hutchinson, Essa Hu, Steven Govek
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Patent number: 7700103Abstract: Synthetic DNA molecules encoding the HPV 52 L1 protein are provided. Specifically, the present invention provides polynucleotides encoding HPV 52 L1 protein, wherein said polynucleotides are codon-optimized for high level expression in a yeast cell. In alternative embodiments of the invention, the nucleotide sequence of the synthetic molecule is altered to eliminate transcription termination signals that are recognized by yeast. The synthetic molecules may be used to produce HPV 52 virus-like particles (VLPs), and to produce vaccines and pharmaceutical compositions comprising the HPV 52 VLPs. The vaccines of the present invention provide effective immunoprophylaxis against papillomavirus infection through neutralizing antibody and cell-mediated immunity and may also be useful for treatment of existing HPV infections.Type: GrantFiled: March 18, 2005Date of Patent: April 20, 2010Assignee: Merck & Co., Inc.Inventors: Janine T. Bryan, Michelle K. Brownlow, Loren D. Schultz, Kathrin U. Jansen
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Patent number: 7700099Abstract: The present invention relates to a non-immunostimulatory antibody which lacks antibody-dependent cell-mediated cytotoxicity, Fc gamma receptor binding and complement-mediated cytotoxicity. In some embodiments, the antibody contains a modified immunoglobulin G2 (IgG2) Fc region with at least one substitution in the B/C loop, FcRn binding domain, and the F/G loop. The antibody of the invention is useful in the preparation of therapeutic antibodies and pharmaceutical compositions and kits containing the same.Type: GrantFiled: October 17, 2006Date of Patent: April 20, 2010Assignee: Merck & Co., Inc.Inventor: William R. Strohl
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Patent number: 7687541Abstract: The invention encompasses the novel compounds of Formula (I) and Formula (II), which are prodrugs that convert in vivo to diaryl-2-(5H)-furanones useful in the treatment of cyclooxygenase-2 mediated diseases. These prodrugs are far more soluble in aqueous media than the active agents into which they convert, in vivo. As such compounds of Formula (I) and (II) are advantageous for, among other things intravenous administration. The invention also encompasses certain pharmaceutical compositions and methods for treatment of cyclooxygenase-2 mediated diseases comprising the use of compounds of Formula (I) and Formula (II).Type: GrantFiled: October 18, 2004Date of Patent: March 30, 2010Assignee: Merck & Co., Inc.Inventors: Jeannie M. Arruda, Benito Munoz, Brian A. Stearns
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Publication number: 20100074888Abstract: It is an object to provide a gene-modified non-human animal having inactivated MGAT2 gene and a gene-modified non-human animal cell, which are useful for the search of the function of MGAT2 in vivo. It is another object to provide a method for screening of a compound capable of inhibiting the activity of MGAT2 and a compound capable of inhibiting the activity of MGAT2. It is further another object to provide a method for detecting a disease induced by abnormal lipid metabolism based on the expression level or activity of MGAT2. A method for screening of a compound by using a gene-modified non-human mammal having the artificially inhibited expression of MGAT2 gene and a cell thereof enable to prevent or treat a disease induced by abnormal lipid metabolism. Also a screening of a compound capable of inhibiting or enhancing the function of MGAT2 enables to prevent or treat a disease induced by abnormal lipid metabolism.Type: ApplicationFiled: November 30, 2007Publication date: March 25, 2010Applicant: MERCK & CO., INC.Inventors: Katsumi Aragane, Ktsuya Ohbuchi, Yoshitaka Tamai, Naomoto Harada, Naomi Murai, Yoshiki Ito, Jun Kusunoki, Yukina Tokushima, Takaharu Maruyama