Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/314)
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Patent number: 9040550Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: July 16, 2014Date of Patent: May 26, 2015Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20150132352Abstract: The present invention relates to chemical compounds, methods for their discovery, and their therapeutic and research use. In particular, the present invention provides compounds as therapeutic agents against bacterial infections (e.g., biofilms).Type: ApplicationFiled: May 2, 2013Publication date: May 14, 2015Inventors: Hongmin Sun, Bryan Yestrepsky, David Ginsburg, Scott D. Larsen
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Publication number: 20150105351Abstract: The present invention is directed to novel nanomolar and picomolar inhibitors of HIV reverse transcriptase, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV-1 and HIV-2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 8, 2014Publication date: April 16, 2015Inventors: William L. Jorgensen, Karen S. Anderson
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Publication number: 20150086911Abstract: An actinic ray-sensitive or radiation-sensitive resin composition includes; a compound (A) which generates an acid by irradiation with actinic rays or radiation, wherein the acid is linked with a group represented by the following general formula (M) through covalent bonding. In the formula, Y1 and Y2 each independently represent a hydrogen atom, an alkyl group, a cycloalkyl group, an alkenyl group, an alkynyl group, an aryl group, or an acyl group. Z represents a hydrogen atom or a substituent.Type: ApplicationFiled: December 4, 2014Publication date: March 26, 2015Applicant: FUJIFILM CorporationInventors: Takuya TSURUTA, Tomotaka TSUCHIMURA, Tadeteru YATSUO
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Publication number: 20150065532Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: November 7, 2014Publication date: March 5, 2015Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
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Patent number: 8957251Abstract: This disclosure describes the molecular cloning of a pactamycin biosynthetic gene cluster from Streptomyces pactum ATCC 27456, characterization of individual genes in the gene cluster and the proteins encoded thereby as well as uses thereof. The pactamycin gene cluster is located within an 86.35 kilobases genetic locus and includes 53 open reading frames, 26 of which are considered to be the core cluster directly involved in the biosynthesis of pactamycin. The present disclosure also relates to the use of the pactamycin biosynthetic genes located within the identified gene cluster for drug design and development purposes, including the development of pactamycin analogs that are more efficacious and less toxic. Also provided are drugs and antibiotics so produced, as well as methods of their use.Type: GrantFiled: April 18, 2008Date of Patent: February 17, 2015Assignee: State of Oregon Acting by and Through the State Board of Higher Education on Behalf of Oregon State UniversityInventors: Taifo Mahmud, Takuya Ito, Patricia M. Flatt, Niran Roongsawang, Norifumi Shirasaka
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Patent number: 8865898Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.Type: GrantFiled: November 30, 2011Date of Patent: October 21, 2014Assignee: Japan Science and Technology AgencyInventor: Yoshihito Ueno
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Patent number: 8853397Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: February 5, 2013Date of Patent: October 7, 2014Assignee: Rigel Pharmacuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20140288017Abstract: The present invention is directed to novel catechol diether compounds, pharmaceutical compositions therefrom and methods for inhibiting reverse transcriptase and treating HIV infections, especially included drug resistant strains of HIV 1 and 2 and/or secondary disease states and/or conditions which occur as a consequence of HIV infection.Type: ApplicationFiled: October 12, 2012Publication date: September 25, 2014Inventors: William L. Jorgensen, Karen S. Anderson
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Publication number: 20140288049Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: ApplicationFiled: June 9, 2014Publication date: September 25, 2014Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
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Publication number: 20140248378Abstract: The present invention provides compounds of formula (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, Y and Z are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: ApplicationFiled: July 5, 2012Publication date: September 4, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Xiao-Ling Fan Cockcroft, William Farnaby, Natasha Kinsella, Kevin Merchant, David Miller
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Patent number: 8822685Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: August 7, 2013Date of Patent: September 2, 2014Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Patent number: 8816074Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.Type: GrantFiled: May 13, 2011Date of Patent: August 26, 2014Assignee: University of Georgia Foundation, Inc.Inventors: Chung K. Chu, Jianing Wang
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Publication number: 20140221637Abstract: A nucleoside analog and a salt thereof represented by any of the general formulae (1) to (10) below: wherein R1, R2, and R3 are the same or different groups, and each of the R1, R2 and R3 is selected from a hydrogen atom, a protecting group for a functional group in nucleic acid synthesis, a phosphate group, a phosphate group protected by a protecting group in nucleic acid synthesis, and an activated phosphate group for solid phase synthesis; and Ar is one of an aromatic hydrocarbon group and a polyaromatic hydrocarbon group.Type: ApplicationFiled: November 30, 2011Publication date: August 7, 2014Inventor: Yoshihito Ueno
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Patent number: 8759539Abstract: Described herein are substituted bicyclic amines. In particular, described herein are substituted bicyclic amines that are effective as antagonists of SSTR5 and useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, metabolic syndrome, depression, and anxiety.Type: GrantFiled: November 11, 2009Date of Patent: June 24, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Jiafang He, John Bawiec, Weiguo Liu, Gui-Bai Liang, Lihu Yang
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Publication number: 20140107339Abstract: Catalysts and methods for the carbonylation of epoxides to substituted 3-hydroxy-?-lactones and ?-lactones are disclosed.Type: ApplicationFiled: September 4, 2013Publication date: April 17, 2014Applicant: Cornell UniversityInventors: Geoffrey W. Coates, John W. Kramer
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Publication number: 20140088125Abstract: Salts of 3-carboxy-N-ethyl-N,N-dimethylpropan-1-aminium, method of preparation thereof and use in the treatment of cardiovascular disease.Type: ApplicationFiled: April 27, 2012Publication date: March 27, 2014Applicant: JSC GrindeksInventors: Ivars Kalvins, Edgars Liepins, Einars Loza, Maija Dambrova, Limars Stonans, Daina Lola, Janis Kuka, Osvalds Pugovics, Reinis Vilskersts, Solveiga Grinberga
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Patent number: 8658776Abstract: Methods for preparation of 2?,3?-dideoxynucleotides support structures, such as 2?,3?-dideoxyguanosine, 2?,3?-dideoxyadenosine, and 3?-deoxythymidine support structures are disclosed. Various methods of using such structures are also provided, such as their use for automated DNA synthesis and pyrophosphorolysis activated polymerization.Type: GrantFiled: May 26, 2011Date of Patent: February 25, 2014Assignee: Life Technologies CorporationInventors: Zhaochun Ma, Khairuzzaman Bashar Mullah, Robert G. Eason
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Publication number: 20140031545Abstract: Processes for making an organozinc reagents are disclosed comprising reacting (A) organomagnesium or organozinc complexes with (B) at least one coordination compound comprising one or more carboxylate groups and/or alcoholate groups and/or tertiary amine groups, optionally in combination with zinc ions and/or lithium ions and/or halide ions, wherein the halide ions are selected from chloride, bromide and iodide, the organozinc complex comprises an aryl group, a heteroaryl group or a benzyl group when the coordinating compound is a chelating polyamine, and the reaction is conducted in the presence of zinc complexed with at least one coordinating compound when reactant (A) comprises at least one organomagnesium complex. The resulting organozinc reagents may optionally be isolated from solvents to obtain a solid reagent. The reagents may be used for making organic compounds via Negishi cross-coupling reactions or via aldehyde and/or ketone oxidative addition reactions.Type: ApplicationFiled: December 21, 2011Publication date: January 30, 2014Applicant: LUDWIG-MAXIMILIAN-UNIVERSITAT MUNCHENInventors: Paul Knochel, Sebastian Bernhardt, Georg Manolikakes
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Publication number: 20130337052Abstract: Administering a therapeutically effective dose of lithium ions mitigates the side effects of a psychoactive substance such as a cannabinoid. The therapeutically effective dose of lithium ions includes greater than 4 milligrams of lithium and less than 170 milligrams of lithium, or includes between 8 and 32 milligrams of lithium ions per milligram of the psychoactive substance. The therapeutically effective dose of lithium ions is administered using lithium carbonate, lithium citrate, lithium chloride, lithium orotate, lithium aspartate, or analogs thereof using a delivery vehicle selected from pills, tablets, capsules, gelcaps, liquids, syrups, injectable liquids, powders, or foods and administered prior to, with, or after administration of the psychoactive substance. The psychoactive substance includes one or more of anandamide, 2-arachidonoyl glycerol, 2-arachidonoyl glycerol ether, tetrahydrocannabinol, cannabinol, cannabidiol, or analogs thereof and may be administered using the delivery vehicle.Type: ApplicationFiled: September 24, 2012Publication date: December 19, 2013Inventors: Patricia Linert, Kenneth J. Ouimet
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Patent number: 8604194Abstract: Novel pharmaceutically acceptable salts of desvenlafaxine with physiologically ubiquitous ions selected from sugar acids and vitamins, processes for their preparation, pharmaceutical compositions containing them and uses therefor are described.Type: GrantFiled: January 29, 2009Date of Patent: December 10, 2013Assignee: Lek Pharmaceuticals D.D.Inventors: Furlan Borut, Anton Copar
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Patent number: 8604192Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclo-hexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: GrantFiled: September 23, 2009Date of Patent: December 10, 2013Assignee: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Eric E. Swayze
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Patent number: 8604193Abstract: Disclosed is a method for preparing HIV reverse transcriptase inhibitors which inhibit replication of HIV in HIV infected cells, and novel intermediate compounds used therein.Type: GrantFiled: January 26, 2010Date of Patent: December 10, 2013Assignee: Korea Research Institute of Chemical TechnologyInventors: Stacey Heumann, Christopher M. Levins, Steven Pfeiffer, Donald Tang
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Patent number: 8552184Abstract: The present invention relates to compounds and pharmaceutically acceptable salts thereof, and compositions comprising the same, that are useful in modulating lyn kinase activity, treating obesity, type II diabetes, metabolic syndrome, and in reducing blood glucose level, weight gain, or fat depot level, or treating a disease or condition associated with the same.Type: GrantFiled: July 1, 2009Date of Patent: October 8, 2013Assignee: Melior Pharmaceuticals I, Inc.Inventors: Andrew G. Reaume, Michael S. Saporito, Alexander R. Ochman, Christopher K. Lipinski
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Publication number: 20130224149Abstract: This disclosure is directed to: (a) processes for preparing compounds and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compounds and salts; (c) pharmaceutical compositions comprising the compounds or salts; and (d) methods of use of such compositions.Type: ApplicationFiled: August 21, 2012Publication date: August 29, 2013Applicant: ABBVIE INC.Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Publication number: 20130225815Abstract: A method of forming a fluorinated molecular entity includes reacting in a reaction mixture an aromatic halide, copper, a fluoroalkyl group, and a ligand. The aromatic halide includes an aromatic group and a halogen substituent bonded to the aromatic group. The ligand includes at least one group-V donor selected from phosphorus and an amine. The overall molar ratio of copper to aromatic halide in the reaction mixture is from 0.2 to 3. The method further includes forming a fluoroalkylarene including the aromatic group and the fluoroalkyl group bonded to the aromatic group. A composition, which may be used in the method, consists essentially of copper, the fluoroalkyl group, and the ligand, where the molar ratio of copper to the fluoroalkyl group is approximately 1.Type: ApplicationFiled: February 19, 2013Publication date: August 29, 2013Applicant: The Board of Trustees of the University of IllinoisInventors: John F. Hartwig, Hiroyuki Morimoto, Patrick Fier
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Publication number: 20130217876Abstract: The disclosure is directed to: (a) phosphacycle ligands; (b) catalyst compositions comprising phosphacycle ligands; and (c) methods of using such phosphacycle ligands and catalyst compositions in bond forming reactions.Type: ApplicationFiled: August 21, 2012Publication date: August 22, 2013Applicant: ABBVIE INC.Inventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Patent number: 8492390Abstract: The invention relates to a novel strategy for the synthesis of Locked Nucleic Acid derivatives, such as ?-L-oxy-LNA, amino-LNA, ?-L-amino-LNA, thio-LNA, ?-L-thio-LNA, seleno-LNA and methylene LNA, which provides scalable high yielding reactions utilising intermediates that also can produce other LNA analogues such as oxy-LNA. Also, the compounds of the formula X are important intermediates that may be reacted with varieties of nucleophiles leading to a wide variety of LNA analogues.Type: GrantFiled: December 23, 2011Date of Patent: July 23, 2013Assignee: Santaris Pharma A/SInventors: Mads Detlef Sorensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Patent number: 8461167Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: GrantFiled: May 8, 2007Date of Patent: June 11, 2013Assignee: ARIAD Pharmaceuticals, Inc.Inventors: Yihan Wang, Xiaotian Zhu, Rajeswari Sundaramoorthi, Wei-Sheng Huang, Dong Zou, R. Mathew Thomas, Jiwei Qi, Jan Antoinette C. Romero, David C. Dalgarno, William C. Shakespeare, Tomi K. Sawyer, Chester A. Metcalf, III
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Publication number: 20130123230Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.Type: ApplicationFiled: November 7, 2012Publication date: May 16, 2013Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
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Patent number: 8410266Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: November 3, 2011Date of Patent: April 2, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li
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Publication number: 20130078256Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: Korea Research Institute of Chemical TechnologyInventor: Korea Research Institute of Chemical Technology
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Publication number: 20130023539Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating and/or preventing metabolic diseases.Type: ApplicationFiled: June 18, 2012Publication date: January 24, 2013Applicant: Euroscreen S.A.Inventors: Hamid R. Hoveyda, Didier Schils, Ludivine Zoute, Julien Parcq
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Patent number: 8343986Abstract: The present invention relates to compounds of Formula (I): pharmaceutically acceptable salts thereof, corresponding preparation processes, pharmaceutical formulations and methods for use as inhibitors of matrix metalloproteinase enzymes (MMPs).Type: GrantFiled: September 1, 2009Date of Patent: January 1, 2013Assignee: Glaxo Group LimitedInventors: Simon Gaines, Ian Peter Holmes, Stephen Lewis Martin, Stephen Paul Watson
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Publication number: 20120309705Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.Type: ApplicationFiled: December 14, 2010Publication date: December 6, 2012Applicant: NOVADEX PHARMACEUTICALS ABInventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
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Patent number: 8232275Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: GrantFiled: July 15, 2011Date of Patent: July 31, 2012Assignees: Wayne State University, The Regents of the University of MichiganInventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Patent number: 8222411Abstract: Methods of making compounds of the formula (I) wherein the variables are as defined herein. Also, methods of making compounds that may be used to inhibit dipeptidyl peptidase.Type: GrantFiled: September 15, 2006Date of Patent: July 17, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Jun Feng, Stephen L. Gwaltney, Jeffrey A. Stafford, Zhiyuan Zhang, Paul R. Brodfuahrer, Bruce Elder, Paul Isbester, Richard S. Fornicola, Philip B. Kisanga, Bingidimi I. Mobele, Grant J. Palmer, Maxwell M. Reeve, Jonathon S. Salsbury, Luckner Ulysse, Sripathy Venkatraman
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Publication number: 20120157431Abstract: A compound of formula (I), or a pharmaceutically acceptable salt, solvate or in vivo hydrolysable ester thereof and pharmaceutical compositions comprising these, all for use in the treatment of chemokine mediated diseases and disorders.Type: ApplicationFiled: December 23, 2011Publication date: June 21, 2012Inventors: David Ranulf Cheshire, Rhona Jane Cox, Premji Meghani, Neal Michael Smith, Jeffrey Paul Stonehouse, Cherylin Francis Preston
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Publication number: 20120122810Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: January 23, 2012Publication date: May 17, 2012Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Publication number: 20120088911Abstract: where R—R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: ApplicationFiled: October 6, 2011Publication date: April 12, 2012Applicant: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack, Andrea Hager-Wernet
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Publication number: 20120082646Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: ApplicationFiled: March 25, 2010Publication date: April 5, 2012Applicant: ABBOTT LABORATORIESInventors: David A. Betebenner, John K. Pratt, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Douglas K. Hutchinson, Warren M. Kati, Allan C. Krueger, Kenton L. Longenecker, Clarence J. Maring, John T. Randolph, Todd W. Rockway, Michael D. Tufano, Rolf Wagner, Dachun Liu
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Patent number: 8148525Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: GrantFiled: April 16, 2010Date of Patent: April 3, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sasha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
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Publication number: 20120029193Abstract: A monomer of formula (1) is provided wherein R1 is hydrogen or a monovalent C1-C6 hydrocarbon group, and R2 is a group having polymerization functionality. Using the monomer, crosslinking units can be incorporated into a polymer chain. A chemically amplified negative resist composition comprising a base polymer having crosslinking units incorporated therein has a high sensitivity and forms a resist pattern with minimized LER.Type: ApplicationFiled: July 26, 2011Publication date: February 2, 2012Applicant: SHIN-ETSU CHEMICAL CO., LTD.Inventors: Daisuke Domon, Satoshi Watanabe
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Publication number: 20120014913Abstract: This disclosure is directed to: (a) processes for preparing a compound and salts thereof that, inter alia, are useful for inhibiting hepatitis C virus (HCV); (b) intermediates useful for the preparation of the compound and salts; (c) pharmaceutical compositions comprising the compound or salts; and (d) methods of use of such compositions.Type: ApplicationFiled: July 15, 2011Publication date: January 19, 2012Applicant: ABBOTT LABORATORIESInventors: Shashank Shekhar, Thaddeus S. Franczyk, David M. Barnes, Travis B. Dunn, Anthony R. Haight, Vincent S. Chan
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Publication number: 20110319439Abstract: MCHR1 antagonists are provided having the following Formula I: wherein all of the variables are defined herein. Such compounds are useful for the treatment of MCHR1 mediated diseases, such as obesity, diabetes, IBD, depression, and anxiety.Type: ApplicationFiled: March 9, 2010Publication date: December 29, 2011Inventor: Saleem Ahmad
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Publication number: 20110319418Abstract: Disclosed are compounds, compositions and methods for treating pain, including inflammatory, visceral, and acute pain. Such compounds are represented by Formula (I) as follows: wherein A1, L1, D, L2, and Q are defined herein.Type: ApplicationFiled: June 27, 2011Publication date: December 29, 2011Inventors: Christopher M. Flores, Paul R. Wade
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Patent number: 8084458Abstract: Methods are described for the synthesis of Locked Nucleic Acid (LNA) derivatives using certain nitrogen-containing nucleophiles.Type: GrantFiled: August 3, 2009Date of Patent: December 27, 2011Assignee: Santaris Pharma A/SInventors: Mads Detlef Sørensen, Jesper Wengel, Troels Koch, Signe M. Christensen, Christoph Rosenbohm, Daniel Sejer Pedersen
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Patent number: 8076302Abstract: A novel pyrimidine nucleoside derivative represented by the following formula (1) and a salt thereof, as well as a pharmaceutical composition comprising the same as an active ingredient have excellent antiviral properties and are useful as antiviral therapeutic agents: [wherein R represents a nitrogen-containing heterocyclic ring which may have any one of a C1-C3 alkyl group or a C1-C3 alkoxy group as a substituent, or a C1-C6 alkyl group which has one primary amino group as a substituent].Type: GrantFiled: February 15, 2007Date of Patent: December 13, 2011Assignee: aRigen Pharmaceuticals, Inc.Inventors: Haruhiko Machida, Masaichi Yamamoto
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Publication number: 20110275652Abstract: Compounds which are active against viruses have the following formulas: wherein B is a purine or pyrimidine heterocyclic ring or base. In a preferred embodiment, the purine include 6-aminopurine (adenine), 6-hydroxypurine (hypoxanthine), 2-amino-6-hydroxypurine (guanine), 2,6-diamino-purine, 2-amino-6-azidopurine, 2-amino-6-halo substituted purines such as 2-amino-6-chloropurine, 2-amino-6-fluoropurine, 2-amino-6-alkoxypurines such as 2-amino-6-methoxypurine, 2-amino-6-cyclopropylaminopurine, 2-amino-6-alkylamino or 2-amino-6-dialkylamino substituted purines, 2-amino-6-thiopurine, 2-amino-6-alkylthio substituted purines, 3-deazapurines, 7-deazapurines and 8-azapurines. The pyrimidine incorporates cytosine, uracil and thymine, 5-halo substituted cytosines and uracils, 5-alkyl substituted cytosines and uracils including derivatives with a saturated or unsaturated alkyl group and 6-azapyrimidines.Type: ApplicationFiled: July 15, 2011Publication date: November 10, 2011Inventors: Jiri Zemlicka, Shaoman Zhou, John C. Drach
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Patent number: RE43029Abstract: This invention relates to a process for the synthesis and method of use of an effective amount of a creatine heterocyclic acid salt for the regulation athletic function in humans.Type: GrantFiled: January 8, 2007Date of Patent: December 13, 2011Assignee: Bio-Engineered Supplements & Nutrition, Inc.Inventors: Sal Abraham, Shengli Jiang