Patents Assigned to Merck Sharp & Dohme
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Patent number: 8071771Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
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Patent number: 8071772Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2, J and K are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Harold G. Selnick, Craig A. Stump, Cory R. Theberge, C. Blair Zartman
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Patent number: 8071770Abstract: Compounds of formula I: (wherein variables A1, A2, A3, A4, A5, A6, A7, B, E1, E2, E3, E4, E5, G1, G2 and R6 are as described herein) which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: November 14, 2006Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Ian M. Bell, Craig A. Stump, Cory R. Theberge, Michael R. Wood, C. Blair Zartman
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Patent number: 8071306Abstract: In one aspect, the present invention provides methods for amplifying a microRNA molecule to produce DNA molecules. The methods each include the steps of: (a) using primer extension to make a DNA molecule that is complementary to a target microRNA molecule; and (b) using a universal forward primer and a reverse primer to amplify the DNA molecule to produce amplified DNA molecules. In some embodiments of the method, at least one of the forward primer and the reverse primer comprise at least one locked nucleic acid molecule.Type: GrantFiled: July 18, 2007Date of Patent: December 6, 2011Assignee: Merck Sharp & Dohme Corp.Inventor: Christopher K. Raymond
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Patent number: 8071568Abstract: The present invention provides nucleoside aryl phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside aryl phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside aryl phosphoramidates of the present invention.Type: GrantFiled: December 28, 2007Date of Patent: December 6, 2011Assignees: Merck Sharp & Dohme Corp., Instituto di Ricerche di Biologia Molecolare P. Angeletti S.p.A.Inventors: Frank Narjes, Cristina Gardelli, Monica Donghi, Barbara Attenni, Philippe L. Durette
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Patent number: 8067575Abstract: This invention relates to compounds, compositions, and methods useful for modulating cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression using short interfering nucleic acid (siNA) molecules. This invention also relates to compounds, compositions, and methods useful for modulating the expression and activity of other genes involved in pathways of cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) gene expression and/or activity by RNA interference (RNAi) using small nucleic acid 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 cyclin (e.g., cyclin D1) and/or cyclin dependent kinase (CDK) genes.Type: GrantFiled: August 28, 2008Date of Patent: November 29, 2011Assignee: Merck, Sharp & Dohme Corp.Inventors: James McSwiggen, Leonid Beigelman
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Patent number: 8067607Abstract: The present invention relates to pyridin-3-yl pyridin-3-amine compounds and derivatives thereof having the structure formula (I) useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: January 29, 2007Date of Patent: November 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Jacob M. Hoffman, M. Brad Nolt
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Patent number: 8067339Abstract: Methods for display of recombinant whole immunoglobulins or immunoglobulin libraries on the surface of eukaryote host cells, including yeast and filamentous fungi, are described. The methods are useful for screening libraries of recombinant immunoglobulins in eukaryote host cells to identify immunoglobulins that are specific for an antigen of interest.Type: GrantFiled: June 23, 2009Date of Patent: November 29, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Bianka Prinz, Natarajan Sethuraman, Dongxing Zha, Stefan Wildt, Piotr Bobrowicz
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Patent number: 8063090Abstract: The present invention relates to diphenylmethyl imidazole mineralocorticoid receptor modulators compounds having the structure and their use in treating cardiovascular events.Type: GrantFiled: March 19, 2008Date of Patent: November 22, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Philip E. Brandish, James C. Hershey, Mark E. Fraley, Justin T. Steen
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Patent number: 8053455Abstract: A compound having the structure wherein R is an angiotensin receptor antagonist active group, Y is selected from the group consisting of and —C(R1H)OC(O)X((CR12R13)—(CHR10)m—(CH2)n—Zp—(CH2)q—(CHR11)r—(CR16R17))—R5;??2) Z is —O— or —(CR14R15)—; m, n, p, q, and r are independently selected from the group consisting of 0 and 1; X is —O— or —(CR18R19)—; R1 is selected from the group consisting of hydrogen, C1-4 alkyl, aryl and C1-4 alkylaryl; R5 is —O—N?N(O)—R3R4; or a pharmaceutically acceptable salt or hydrate thereof, which is useful for treating hypertension.Type: GrantFiled: April 25, 2011Date of Patent: November 8, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Amjad Ali, Michael Man-Chu Lo, Christopher Franklin, Brent Whitehead
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Patent number: 8039484Abstract: Diaryl ethers in which one of the aryl groups is a phenyl fused to a cycloalkyl or heterocyclic ring, to which is attached an acetic acid group, are agonists of G-protein coupled receptor 40 (GPR40) and are useful as therapeutic compounds, particularly in the treatment of Type 2 diabetes mellitus, and of conditions that often accompany this disease, including insulin resistance, obesity and lipid disorders.Type: GrantFiled: October 26, 2007Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Min Ge, Songnian Lin, Shawn P. Walsh, Lihu Yang, Changyou Zhou
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Patent number: 8039460Abstract: Compounds of Formula (I): and Formula (II): (where variables R2, R4, A, B, D, W, X, Y and Z are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: GrantFiled: October 12, 2005Date of Patent: October 18, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher S. Burgey, Daniel V. Paone, Anthony W. Shaw, Diem N. Nguyen, Zhengwu J. Deng, Theresa M. Williams, Joseph P. Vacca, Craig M. Potteiger, Harold G. Selnick
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Publication number: 20110251207Abstract: In its many embodiments, the present invention provides a novel class of biaryi spiroaminooxazoline analogues as modulators of ?2C adrenergic receptor agonists, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more conditions associated with the ?2C adrenergic receptors using such compounds or pharmaceutical compositions.Type: ApplicationFiled: October 6, 2009Publication date: October 13, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Kevin D. McCormick, Li Dong, Christopher W. Boyce, Manuel de Lera Ruiz, Salem Fevrier, Jie Wu, Junying Zheng, Younong Yu, Jianhua Chao, Walter S. Won, Ashwin U. Rao, Rongze Kuang, Pauline C. Ting, Xianhai Huang, Ning Shao, Adandan Palani, Michael Y. Berlin, Robert G. Aslanian
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Patent number: 8034772Abstract: The vascular endothelial cell growth factor (VEGF) inhibitors of the present invention are naturally occurring or recombinantly engineered soluble forms with or without a C-terminal transmembrane region of the receptor for VEGF, a very selective growth factor for endothelial cells. The soluble forms of the receptors will bind the growth factor with high affinity but do not result in signal transduction. These soluble forms of the receptor bind VEGF and inhibit its function.Type: GrantFiled: February 6, 2009Date of Patent: October 11, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Richard L. Kendall, Kenneth A. Thomas, Jr.
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Publication number: 20110240511Abstract: The present invention relates to packaging and containers for oxygen-sensitive pharmaceutical products, or oxygen- and moisture-sensitive pharmaceutical products. More particularly, the invention relates to pharmaceutical packages comprising a blister pack with airflow channels and outlets, an oxygen scavenger, and, optionally, a desiccant, all of which are sealed inside an outer container having oxygen and moisture barrier properties.Type: ApplicationFiled: December 2, 2009Publication date: October 6, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Matthew P. Bolton, Rey T. Chern, Arthur L. Jaeger, Matthew Moyer, Anthony P. Panarello
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Patent number: 8030359Abstract: A pharmaceutical composition comprises (a) a CETP inhibiting compound, or a pharmaceutically acceptable salt thereof; (b) a concentration-enhancing polymer, and (c) optionally one or more surfactants; wherein the compound has the structure shown as Formula I below. The composition raises HDL-cholesterol and lowers LDL-cholesterol.Type: GrantFiled: February 9, 2007Date of Patent: October 4, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Sarah Geers, Michael Lowinger, Craig A. McKelvey, Robert F. Meyer, Dina Zhang
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Patent number: 8030332Abstract: The present invention relates to dipyridin-3-ylmethoxy compounds and derivatives thereof having the structure I useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: January 29, 2007Date of Patent: October 4, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: B. Wesley Trotter, Richard C. A. Isaacs, Zhicai Wu, Jacob M. Hoffman, Mark T. Bilodeau, Ahren Iver Green
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Patent number: 8026260Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.Type: GrantFiled: October 30, 2006Date of Patent: September 27, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
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Patent number: 8026082Abstract: The present invention provides a synthetic gene control region which comprises a gene regulatory sequence comprising a binding site for a gene regulatory protein of a yeast strain, and a promoter from filamentous fungal strain located downstream of the gene regulatory sequence; wherein the promoter can be recognized by the general transcription factors and RNA polymerase of the yeast strain; wherein the gene regulatory sequence is capable of regulating transcription initiated by the filamentous fungal promoter in the yeast strain.Type: GrantFiled: June 9, 2006Date of Patent: September 27, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Janine Bryan, Michelle K. Brownlow, Loren D. Schultz, Maria C. Losada, Kathrin Ute Jansen, Myra Kurtz, Stuart Kurtz, legal representative
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Publication number: 20110230526Abstract: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.Type: ApplicationFiled: January 28, 2011Publication date: September 22, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Nicholas D. Cosford, Thomas J. Seiders, Joseph E. Payne, Jeffrey R. Roppe, Dehua Huang, Nicholas D. Smith, Steve F. Poon, Chris King, Brian W. Eastman, Bowei Wang, Jeannie M. Arruda, Jean-Michel Vernier, Xiumin Zhao