Patents Issued in December 30, 2010
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Publication number: 20100331266Abstract: Methods for analyzing, selecting, characterizing or classifying compositions of a co-polymer, e.g., glatiramer acetate are described. The methods entail analysis of pyro-glutamate in the composition, and, in some methods, comparing the amount of pyro-glutamate present in a composition to a reference standard.Type: ApplicationFiled: September 15, 2010Publication date: December 30, 2010Applicant: Momenta Pharmaceuticals, Inc. a Massachusetts corporationInventors: Yanjie Jiang, Peter James Ahern, James Eric Anderson, Corinne Bauer, Xiangping Zhu, Zachary Shriver
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Publication number: 20100331267Abstract: The present invention relates to methods for treating ?-synucleinopathies, methods for modulating of assembly, folding, accumulation, oligomerization, rate of aggregation, oligomerization and clearance of proteins of fragments comprising ?-synuclein aggregates in a subject, by administering a medicament comprising a therapeutically effective amount of a cyclohexanehexyl derivative. More specifically, the invention provides medicaments comprising at least one cyclohexanehexyl derivative of formula (III) or (IV) useful in improving neuron, glia and oligodendrocyte function, for slowing the degeneration and death of neurons, glial cells and oligodendrocytes in the brain and treating synucleinopathies such as Parkinson's disease. These medicaments are formulated for oral and parenteral administration. Formulae (III), (IV).Type: ApplicationFiled: April 11, 2008Publication date: December 30, 2010Inventor: JoAnne McLaurin
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Publication number: 20100331268Abstract: Described herein are nitrated lipids and methods of making and using the nitrated lipids.Type: ApplicationFiled: June 9, 2010Publication date: December 30, 2010Applicants: THE UAB RESEARCH FOUNDATION, State of Oregon Acting By and Through the Board of Education on behalf of the University of OregonInventors: Bruce A. Freeman, Francisco Schopfer, Valerie O'Donnell, Paul Baker, Yuqing E. Chen, Bruce Branchaud
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Publication number: 20100331269Abstract: A compound of formula (I): wherein R1 is selected from the group consisting of H, ?-L-Rhamnopyranose, ?-D-Mannopyranose, ?-D-Xylopyranose, ?-D-Glucopyranose, and ?-D-Arabinopyranose; R2 is selected from CH3, COOH, CH2OH, COOCH3 and CH2O-?-D-Arabinopyranose; with the proviso that the compound of formula (I) is not a compound of formula (I) wherein R1 is ?-D-Glucopyranose and R2 is COOH; wherein R1 is ?-L-Rhamnopyranose and R2 is CH3; wherein R1 is ?-D-Glucopyranose and R2 is CH2OH; wherein R1 is ?-D-Xylopyranose and R2 is CH2OH; wherein R1 is ?-L-Rhamnopyranose and R2 is COOCH3, wherein R1 is H and R2 is CH3; wherein R1 is H and R2 is CH2OH; wherein R1 is H and R2 is COOH; or wherein R1 is H and R2 is COOCH3, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: June 17, 2010Publication date: December 30, 2010Inventors: Andre Pichette, Jean Legault, Charles Gauthier
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Publication number: 20100331270Abstract: It is an object of the invention to discover a substance that effectively increases the production of adrenomedullin, as well as to provide an adrenomedullin production-enhancing agent utilizing this substance. The adrenomedullin production-enhancing agent is characterized by inclusion of a ginsenoside, a sanshool, and/or a shogaol as active ingredients.Type: ApplicationFiled: February 19, 2008Publication date: December 30, 2010Applicants: Natl. Uni. Corp. ASAHIKAWA MEDICAL COLLEGE, TSUMURA & CO.Inventors: Toru Kono, Atsushi Kaneko, Yuji Omiya
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Publication number: 20100331271Abstract: This invention provides a method for treating or preventing human atrial arrhythmia (fibrillation) using the leading flavone compound acacetin, and its derivatives and analogues that inhibit the ultra-rapidly-activating delayed rectifier potassium current (IKur or IKsus), transient outward potassium (Ito), and acetylcholine-activated potassium current (IK.ACh).Type: ApplicationFiled: September 7, 2010Publication date: December 30, 2010Inventors: Gui-Rong LI, Chu-Pak Lau, Guo-Wei Qin, Hong-Bing Wang
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Publication number: 20100331272Abstract: An agent for preventing or ameliorating skin aging, which exhibits a more excellent effect on the suppression of formation, or the amelioration, of wrinkles on the skin or sagging skin. An agent for preventing or ameliorating skin aging, containing triterpenoid saponins represented by the following formula (1) as an active ingredient, wherein at least one of R1 and R2 is a tigloyl group and the other represents a tigloyl group or an angeloyl group; R3 represents a methyl group or a hydroxymethyl group; and R4 represents Glc, Xyl or Gal.Type: ApplicationFiled: February 26, 2009Publication date: December 30, 2010Applicant: KAO CorporationInventors: Akiyo Kameyama, Tsutomu Fujimura
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Publication number: 20100331273Abstract: The present invention relates to a complex that can be injected into the body to hone in on target cells to deliver molecules. In one embodiment, the invention provides a drug delivery system that includes components that self-assemble into one targeted conjugate. In another embodiment, the invention includes a targeted carrier protein and a nucleic acid sequence non-covalently linked to one or more drugs.Type: ApplicationFiled: July 3, 2008Publication date: December 30, 2010Applicant: CEDARS-SINAI MEDICAL CENTERInventor: Lali K. Medina-Kauwe
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Publication number: 20100331274Abstract: This invention relates to certain chirally-correct mitoprotectant phosphorylated heterocyclic agents [formula (I)], which are useful for the treatment of dermatological disorders that include challenged skin from cancer, diabetes, radiation treatments, chemotherapy, and sun-burn; mitochondrial dysfunction; age spots; acne, loss of cellular antioxidants; skin changes associated with aging including collagen loss, loss of skin pliability, loss of skin suppleness, skin wrinkles and fine lines, oxidation, damage from radiation, damage from free radicals, and damage from UV; dry skin; xerosis; ichthyosis; dandruff; brownish spots; keratoses; melasma; lentigines; liver spots; skin pigmentation including pigmented spots, dark circles under the eyes, darkened skin, and blemishes; oily skin; warts; eczema; pruritic skin; psoriasis; inflammatory dermatoses; topical inflammation; disturbed keratinization; scalp dryness; skin depigmentation, and combinations thereof;Type: ApplicationFiled: August 6, 2010Publication date: December 30, 2010Applicant: ISLAND KINETICS INC.Inventors: SHYAM K. GUPTA, LINDA WALKER
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Publication number: 20100331275Abstract: The invention provides a method for supporting operational activities in daily living by providing a combination of (a) long-chain polyunsaturated fatty acids, particularly DHA and/or EPA, and (b) nucleosides or nucleotides, particularly uridine or its equivalent. The operational activities comprise eating; walking; toileting; bathing; grooming; dressing; u se of communication equipment; making conversations; keeping appointments; use of household appliances; cleaning dishes; preparation of meal or drink; writing; reading; independent housekeeping; transportation and shopping.Type: ApplicationFiled: June 20, 2008Publication date: December 30, 2010Inventors: Martine Groenendijk, Mattheus Cornelis De Wilde, Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis
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Publication number: 20100331276Abstract: The invention relates to a composition for topical application as well as the use of such a composition. The invention is characterised in that it comprises at least one first and one second mono- or oligosaccharide, each of said first and second mono- or oligosaccharides being capable of limiting the adhesion of microorganisms on the skin of warm-blooded animals with coats.Type: ApplicationFiled: September 13, 2010Publication date: December 30, 2010Applicant: VIRBAC SAInventor: Hugues Gatto
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Publication number: 20100331277Abstract: The present invention relates to inhibiting or preventing infection and protecting against patency complications after a blood catheter has been inserted in a patient comprising administering to the device a pharmaceutically effective amount of a composition comprising: (A) at least one taurinamide derivative, (B) at least one compound selected from the group consisting of biologically acceptable acids and biologically acceptable salts thereof; and (C) heparin at a low concentration.Type: ApplicationFiled: March 12, 2010Publication date: December 30, 2010Inventor: Frank R. Prosl
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Publication number: 20100331278Abstract: Described are an oral ingestion form comprising cationic hydroxyethylcellulose, and methods of using the same in prevention and treatment of metabolic disorders.Type: ApplicationFiled: May 6, 2010Publication date: December 30, 2010Inventors: W. H. Kerr Anderson, Shao-Ching Hung, William T. Stott, Maciej Turowski, Wallace H. Yokoyama, Scott A. Young
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Publication number: 20100331279Abstract: Methods to prevent the rejection of immunogenic tissues in an animal by administering a non-immunogenic, poorly catabolized molecule in an amount sufficient to inhibit an immune response are described herein. Also described are compositions that are useful for inhibiting immune responses in animals that are recipients of cellular transplants. For example, these methods and compositions can be used to prevent the rejection of xenografted and allografted tissues in an animal.Type: ApplicationFiled: August 31, 2010Publication date: December 30, 2010Inventors: Gregory I. Frost, Per Borgstrom
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Publication number: 20100331280Abstract: There is provided a method of modifying vasoactivity by regulating a soluble A? pro-inflammatory pathway. Also provided is a method of modifying inflammatory reactions in microglia and neurons by regulating a soluble A? pro-inflammatory pathway. A method of treating patients with vascular disease by modifying an intracellular soluble A? pro-inflammatory pathway is also provided. A pharmaceutical composition consisting essentially of an effective amount of a soluble A? pro-inflammatory pathway regulator in a pharmaceutically effective carrier is also provided.Type: ApplicationFiled: October 20, 2009Publication date: December 30, 2010Inventors: Daniel C. Paris, Terrence C. Town, Michael J. Mullan
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Publication number: 20100331281Abstract: We have discovered that phospholipids diundecanoyl (C11:0-C11:0) and dilauroyl (C12:0-C12:0) phosphatidylcholine (PC) act as agonists of the LRH-1 receptor. We have also shown that administration of these lipids to diabetic mice reduces blood glucose levels. On the basis of these discoveries, the present invention features compositions that include these lipids and structurally related lipids. Also featured are methods of treating metabolic disorders and inflammatory bowel disease, lowering blood glucose levels, and increasing LRH-1 receptor activity in a subject by administration of these lipids.Type: ApplicationFiled: November 17, 2008Publication date: December 30, 2010Applicant: Baylor College of MedicineInventors: David D. Moore, Jae Man Lee
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Publication number: 20100331282Abstract: The present invention provides an antifungal agent that has excellent antifungal action, and is also superior in terms of its properties, and particularly its solubility in water and safety in an aqueous solution, and its in vivo pharmacokinetics and safety. According to the present invention, there is provided a compound represented by the following formula (I), or a salt thereof: wherein R1 represents a hydrogen atom, a halogen atom, an amino group, a C1-6 alkyl group, a C1-6 alkoxy group, or a C1-6 alkoxy C1-6 alkyl group; R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group, or a di-C1-6 alkylamino group; R3 represents a hydrogen atom, a halogen atom, or a C1-6 alkyl group; and R4 represents a hydrogen atom, a halogen atom, or a C1-6 alkyl group.Type: ApplicationFiled: June 22, 2010Publication date: December 30, 2010Inventor: Masayuki MATSUKURA
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100331284Abstract: The present invention provides compositions and methods for prevention and prophylaxis of neurological diseases accompanied by neuronal death. The invention includes synthesis of 5-benzylamino salicylic acid (BAS) and its derivatives. BAS and its derivatives protect cortical neurons from toxic insults by N-methyl-D-aspartate, Zn2+, and reactive oxygen species. Thus, the present invention provides compositions and methods for treating stroke, traumatic brain and spinal cord injury, epilepsy, and neurodegenerative diseases that are accompanied by severe neuronal loss via excitotoxicity, Zn2+ neurotoxicity, and free radical neurotoxicity.Type: ApplicationFiled: May 24, 2010Publication date: December 30, 2010Applicant: NEUROTECH PHARMACEUTICALS CO., LTD.Inventors: Byoung Joo GWAG, Young Ae Lee, Bo Rum Ryu, Sung Hwa Yoon, Ho Sang Moon
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Publication number: 20100331285Abstract: A polymorph of aspirin is provided by the present invention. Methods of making and using the same are also provided.Type: ApplicationFiled: August 23, 2010Publication date: December 30, 2010Applicants: TRANSFORM PHARMACEUTICALS, INC., UNIVERSITY OF SOUTH FLORIDAInventors: Orn Almarsson, Jennifer McMahon, Vishweshwar Peddy, Matthew Peterson, Michael J. Zaworotko
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Publication number: 20100331286Abstract: The field of the present invention relates to novel and improved therapies for treatment of complications associated with impaired renal function. More specifically, the present invention relates to evaluating the effects of a novel renal multivitamin on Vitamin D levels, EPO dose, inflammatory (e.g., C-reactive protein) and other biomarkers in an end stage renal disease (ESRD) population on hemodialysis (HD).Type: ApplicationFiled: August 25, 2010Publication date: December 30, 2010Inventor: Ray Chow
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Publication number: 20100331287Abstract: 6-(Aminoalkyl)indazoles of formula (I) and the salts thereof have renin-inhibiting properties and can be used as antihypertensive, and renal, cardiac and vascular protecting medicinally active ingredients.Type: ApplicationFiled: March 30, 2007Publication date: December 30, 2010Inventors: John J. Baldwin, David A. Claremon, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wenguang Zeng
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Publication number: 20100331288Abstract: The present invention relates to a crystalline, enantiomerically pure hydrate of R-6-hydroxy-8-{1-hydroxy-2-[2-(4-methoxy-phenyl)-1,1-dimethyl-ethylamino]-ethyl}-4H-benzo[1,4]oxazin-3-one-hydrochloride of formula (1) and its activity as a long-acting betamimetic, on its own or combined with one or more other active substances for treating respiratory complaints.Type: ApplicationFiled: October 21, 2008Publication date: December 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Michael Aven, Peter Sieger
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Publication number: 20100331289Abstract: A pharmaceutical product or formulation, which comprises azelastine or a pharmaceutically acceptable salt, solvate or physiologically functional derivative thereof, and a steroid, or a pharmaceutical acceptable salt, solvate or physiologically functional derivative thereof, preferably the product or formulation being in a form suitable for nasal or ocular administration.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Applicant: CIPLA LIMITEDInventors: Amar Lulla, Geena Malhotra
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Publication number: 20100331290Abstract: Nanoparticulate formulations for delivery of taxane conjugate prodrug formed from a taxane coupled to a hydrophobic moiety through a glycolate linker are described.Type: ApplicationFiled: November 26, 2008Publication date: December 30, 2010Inventors: Steven M. Ansell, Sharon Johnstone, Paul Tardi, Lawrence Mayer
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Publication number: 20100331291Abstract: A process is described for the preparation of drospirenone, a synthetic steroid with progestogenic, antimineralocorticoid and antiandrogenic activity, useful for preparing pharmaceutical compositions with contraceptive action by the oxidation of 17?-(3-hydroxypropyl)-6?,7?,15?, 16?-dimethylene-5?-androstane-3?,5,17?-triol.Type: ApplicationFiled: August 4, 2010Publication date: December 30, 2010Inventors: Francesca COSTANTINO, Roberto LENNA, Silvia PIURI
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Publication number: 20100331292Abstract: The present invention relates to substituted steroid compounds having the formula Wherein R1 is H or halogen; R2 is H, (1C-4C)alkyl, (1C-4C)acyl, glucuronyl or sulfamoyl; R3 is H or halogen; R4 is H, (1C-4C)alkyl, (2C-4C)alkenyl or (2C-4C)alkynyl; R5 is methyl or ethyl; R6 is H or methyl; R7 is H or methyl; R8 is H or acyl for use in the treatment and prevention of endometriosis, for contraception, for hormonal therapy in perimenopausal and post-menopausal women, for the treatment of osteoporosis and for the treatment uterine fibroids and other menstrual-related disorders, such as dysfunctional uterine bleeding.Type: ApplicationFiled: June 8, 2010Publication date: December 30, 2010Applicant: N.V. OrganonInventors: Fredericus Antonius Dijcks, Hubert Jan Jozef Loozen, Samira Addo, Antonius Gerardus Hendrikus Ederveen
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Publication number: 20100331293Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjogren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute LymphobType: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Timothy D. Cushing, Paul John Dransfield, Felix Gonzalez Lopez De Turiso, Michael G. Johnson, Todd Kohn, Vatee Pattaropong, Jillian L. Simard
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Publication number: 20100331294Abstract: Compounds of the formula wherein R1 and R2 are as disclosed herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor full or partial agonists. Also disclosed are pharmaceutical compositions, methods for using such compounds and compositions, and processes for preparing the compounds.Type: ApplicationFiled: June 30, 2010Publication date: December 30, 2010Applicant: ABBOTT LABORATORIESInventors: Lawrence A. Black, Gregory A. Gfesser, Marlon D. Cowart
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Publication number: 20100331295Abstract: Compounds of the invention, such as compounds of Formulae Ia, Ib, Ic, or Id and pharmaceutically acceptable salts, isomers, and prodrugs thereof, which are useful as modulators of the activity of liver X receptors, where R1, R2, R21, R3, and G are defined herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.Type: ApplicationFiled: June 26, 2006Publication date: December 30, 2010Applicant: EXELIXIS, INC.Inventors: Brett B Busch, Brenton T. Flatt, Xiao Hui Gu, Shao Po Lu, Richard Martin, Raju Mohan, Michael Charles Nyman, Edwin Schweiger, William C. Stevens, JR., Tie Lin Wang, Yinong Xie
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Publication number: 20100331296Abstract: The invention relates to new bicyclic heterocyclic derivative compounds of formula (I): wherein R1, A, X1, X2, X3, X4, X5 and R2 are as defined herein, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.Type: ApplicationFiled: October 10, 2008Publication date: December 30, 2010Applicant: Astex Therapeutics LimitedInventors: Gordon Saxty, Valerio Berdini, Christopher William Murray, Charlotte Mary Griffiths-Jones, Emma Vickerstaffe, Gilbert Ebai Besong, Maria Grazia Carr
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Publication number: 20100331297Abstract: Compounds and compositions are provided for treatment or amelioration of one or more disorders characterized by defects in protein trafficking. A method of treating a disorder characterized by impaired protein trafficking includes administering to a subject or contacting a cell with a compound of Formula I: [formula here] or pharmaceutically acceptable salts or derivatives thereof.Type: ApplicationFiled: November 7, 2008Publication date: December 30, 2010Applicant: FOLDRX PHARMACEUTICALS, INC.Inventors: Christine Ellen Bulawa, Michael DeVit, Daniel Elbaum
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Publication number: 20100331298Abstract: Chemokine receptor antagonists, in particular, compounds of Formula (I) that act as antagonists of the chemokine CCR2 receptor, including pharmaceutical compositions and uses thereof to treat or prevent diseases associated with monocyte accumulation, lymphocyte accumulation or leukocyte accumulation are described herein.Type: ApplicationFiled: December 10, 2008Publication date: December 30, 2010Applicant: CytoPathfinder, Inc.Inventors: Efrat Ben-Zeev, Dongli Chen, Merav Fichman, Shomir Ghosh, Steffi Koerner, Jian Lin, Yael Marantz, Rosa E. Melendez, Pradyumna Mohanty, Sharon Shacham, Zhaoda Zhang
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Publication number: 20100331299Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: April 22, 2010Publication date: December 30, 2010Inventors: Haiyan Bian, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20100331300Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) as follows: wherein Y, Z, R1, and s are defined herein.Type: ApplicationFiled: April 22, 2010Publication date: December 30, 2010Inventors: Haiyan BIAN, Kristen Chevalier, Jose Clemente, Pete Connolly, Chris Flores, Shu-Chen Lin, Li Liu, John Mabus, Mark Macielag, Mark McDonnell, Philip Pitis, Yue-Mei Zhang, Sui-Po Zhang, Bin Zhu
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Publication number: 20100331301Abstract: Compounds of formula [I]: wherein each symbol is as defined in the description, or a pharmaceutically acceptable salts or solvates thereof.Type: ApplicationFiled: May 14, 2010Publication date: December 30, 2010Applicant: JAPAN TOBACCO INC.Inventors: Kazutaka Ikegashira, Taku Ikenogami, Naoki Ogawa, Tatsuya Matsumoto, Takahiro Oka, Takuya Matsuo, Takayuki Yamasaki
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Publication number: 20100331302Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: ApplicationFiled: July 8, 2010Publication date: December 30, 2010Applicant: Chemocentryx, Inc.Inventors: Trevor T. Charvat, Cheng Hu, Anita Melikian, Aaron Novack, Andrew M.K. Pennell, Edward J. Sullivan, William D. Thomas, Solomon Ungashe, Penglie Zhang, Jay Powers, Sreenivas Punna
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Publication number: 20100331303Abstract: The present disclosure relates to HIF-1? prolyl hydroxylase inhibitors, compositions which comprise the HIF-1? prolyl hydroxylase inhibitors described herein and to methods for controlling, inter alia, Peripheral Vascular Disease (PVD), Coronary Artery Disease (CAD), heart failure, ischemia, and anemia.Type: ApplicationFiled: August 20, 2010Publication date: December 30, 2010Inventors: Richard Masaru Kawamoto, Shengde Wu, Namal C. Warshakoon, Artem G. Evdokimov, Kenneth D. Greis, Angelique Sun Boyer
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Publication number: 20100331304Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: October 30, 2008Publication date: December 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Publication number: 20100331305Abstract: Disclosed are compounds of Formula I, including steroisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, that are useful in modulating PIKK related kinase signaling, e.g., mTOR, and for the treatment of diseases (e.g., cancer) that are mediated at least in part by the dysregulation of the PIKK signaling pathway (e.g., mTOR).Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Genentech, Inc.Inventors: Philippe Bergeron, Frederick Cohen, Anthony Estrada, Michael F.T. Koehler, Cuong Ly, Joseph P. Lyssikatos, Zhonghua Pei, Wendy Lee, Xianrui Zhao
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Publication number: 20100331306Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity.Type: ApplicationFiled: June 25, 2010Publication date: December 30, 2010Applicant: AMGEN INC.Inventors: Minna Bui, Yi Chen, Timothy D. Cushing, Jason A. Duquette, BenjamÃn Fisher, Felix Gonzalez Lopez De Turiso, Xiaolin Hao, Xiao He, Michael G. Johnson, Brian Lucas
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Publication number: 20100331307Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.Type: ApplicationFiled: June 29, 2010Publication date: December 30, 2010Inventors: Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
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Publication number: 20100331308Abstract: The invention relates to compounds of Formula (I) wherein U, V, W, R1, R1b, A and G are as defined in the description, to pharmaceutically acceptable salts of such compounds and to the use of these compounds in the manufacture of a medicament for the prevention or treatment of a bacterial infection.Type: ApplicationFiled: February 20, 2009Publication date: December 30, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Christian Hubschwerlen, Georg Rueedi, John-Philippe Surivet, Cornelia Zumbrunn-Acklin
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Publication number: 20100331309Abstract: Compounds of a formula entitled, trans-4-[[(5S)-5-[[[3,5-bis(trifluoromethyl)phenyl]methyl](2-methyl-2H-tetrazol-5-yl)amino]-2,3,4,5-tetrahydro-7,9-dimethyl-1H-1-benzazepin-1-yl]methyl]-cyclohexanecarboxylic acid, as a free acid or a pharmaceutically acceptable salt thereof; and hydrates and other solvates in crystalline form; pharmaceutical formulations; and methods of use are disclosed.Type: ApplicationFiled: June 28, 2010Publication date: December 30, 2010Applicant: ELI LILLY AND COMPANYInventors: Xinchao Chen, Scott Alan Frank, David Michael Remick, Steven Wayne Pedersen
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Publication number: 20100331310Abstract: Compounds represented by formula (I) and pharmaceutically acceptable salts thereof have excellent sodium channel inhibitory action and are useful as therapeutic agents and analgesics for various kinds of neuralgia, neuropathy, epilepsy, insomnia, premature ejaculation and the like. wherein Q represents ethylene, etc., R1, R2 and R3 represent hydrogen, etc., X1 represents C1-6 alkylene, etc., X2 represents C1-6 alkylene, etc., A1 represents a 5- to 6-membered heterocyclic group, etc., and A2 represents C6-14 aryl, etc.Type: ApplicationFiled: February 9, 2009Publication date: December 30, 2010Inventors: Fumihiro Ozaki, Motohiro Soejima, Tasuku Ishida, Yoshihiko Norimine, Nobuyuki Kurusu, Eriko Doi, Toshihiko Kaneko, Daiju Hasegawa, Kiyoaki Kobayashi, Noboru Yamamoto
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Publication number: 20100331311Abstract: The present invention relates to the use of galantamine for neuroprotection of retinal ganglion cells.Type: ApplicationFiled: September 10, 2010Publication date: December 30, 2010Inventor: Adriana Di Polo
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Publication number: 20100331312Abstract: Amide derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the histamine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders, such as cognitive disorders, epilepsy, brain trauma, depression, obesity, disorders of sleep and wakefulness such as excessive daytime sleepiness, narcolepsy, shift-work sleep disorder, drowsiness as a side effect from a medication, maintenance of vigilance to aid in the completion of tasks and the like, cataplexy, hypersomnia, somnolence syndrome, jet lag, sleep apnea and the like, attention deficit hyperactivity disorder (ADHD), schizophrenia, allergies, allergic responses in the upper airway, allergic rhinitis, nasal congestion, dementia, Alzheimer's disease, pain and the like.Type: ApplicationFiled: February 18, 2009Publication date: December 30, 2010Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Vincent J. Santora, Brian J. Hofilena, Michelle Pulley, Graeme Semple, Yun Shan, Brian M. Smith
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Publication number: 20100331313Abstract: The present invention relates to novel Thiazole Derivatives, compositions comprising the Thiazole Derivatives, and methods for using the Thiazole Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral infection, a fungal infection, or a disorder related to the activity of a protein kinase.Type: ApplicationFiled: October 27, 2008Publication date: December 30, 2010Inventors: Panduranga Adulla P. Reddy, Tzu T. Wong, Lianyun Zhao, Shuyi Tang, Marc A. Labroli, Timothy J. Guzi, M. Arshad Siddiqui
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Publication number: 20100331314Abstract: The invention provides compounds of general formula (I) that inhibit selected kinases (Pim and/or CK2 kinases) and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, and certain infections and immunological disorders.Type: ApplicationFiled: May 20, 2010Publication date: December 30, 2010Inventors: Mustapha HADDACH, Joe TRAN
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Publication number: 20100331315Abstract: The invention provides compounds that inhibit PIM kinases and/or CK2, and compositions containing such compounds. These compounds and compositions are useful for treating proliferative disorders such as cancer, as well as other kinase-associated conditions including inflammation, pain, vascular disorders, pathogenic infections and certain immunological disorders.Type: ApplicationFiled: June 18, 2010Publication date: December 30, 2010Inventors: Mustapha HADDACH, David M. RYCKMAN