Chalcogen Attached Directly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/312)
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Patent number: 8802659Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.Type: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: Biogen Idec MA Inc.Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
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Publication number: 20140221423Abstract: This invention relates to compounds that modulate TRPM7 protein activity and use of the same for treatment or prophylaxis of ischemia, cancer, pain or glaucoma.Type: ApplicationFiled: June 15, 2012Publication date: August 7, 2014Inventors: Xiujun Sun, Michael Tymianski
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Publication number: 20140221364Abstract: The present invention relates to tetrahydroquinoline compounds as muscarinic receptor agonists; compositions comprising the same; methods of inhibiting an activity of a muscarinic receptor with said compounds; methods of treating a disease condition associated with a muscarinic receptor using said compounds; and methods for identifying a subject suitable for treatment using said compounds.Type: ApplicationFiled: February 5, 2014Publication date: August 7, 2014Applicant: ACADIA PHARMACEUTICALS, INC.Inventors: NIELS SKJAERBAEK, KRISTIAN NORUP KOCH, BO LENNART MIKAEL FRIBERG, BO-RAGNAR TOLF
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Publication number: 20140221357Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: September 25, 2012Publication date: August 7, 2014Applicant: Bristol-Myers Squibb CompanyInventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
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Publication number: 20140221425Abstract: Provided in the present invention is a quinolyl-containing hydroxamic acid compound as shown in formula (I), at the same time also disclosed is the preparation method of the compound and the use thereof, and a pharmaceutical composition containing the quinolyl-containing hydroxamic acid compound. Such compounds are inhibitors of protein kinases and/or histone deacetylases, and can be used in the treatment of diseases caused by the abnormal activity of protein kinases and/or histone deacetylases, for example, tumors, etc.Type: ApplicationFiled: September 27, 2011Publication date: August 7, 2014Applicant: BEIJING KONRUNS PHARMACEUTICAL CO., LTD.Inventors: Ziwei Yun, Hongtao Wang
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Publication number: 20140221424Abstract: The present invention relates to the use of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide and pharmaceutical compositions thereof for the treatment of cystic fibrosis, in patients, including kits and/or products thereof.Type: ApplicationFiled: January 30, 2014Publication date: August 7, 2014Inventor: Jiuhong Zha
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Publication number: 20140221298Abstract: The present invention provides an agricultural and horticultural fungicidal composition including a compound A which is at least one selected from a nitrogen-containing heterocyclic compound having a specific structure including a compound represented by the formula (1), and a salt thereof, and a compound B which is at least one selected from the group of specific pesticidally active compounds: in the formula (1), X each independently represents a halogeno group or a C1 to 6 alkyl group; n represents the number of X(s) and is an integer of 0 to 6; and X? represents a halogeno group; and R1, R2 and R3 each independently represent a C1 to 6 alkyl group or a hydroxyl group.Type: ApplicationFiled: September 24, 2012Publication date: August 7, 2014Inventor: Raito Kuwahara
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Publication number: 20140221284Abstract: The invention provides compositions and methods for determining GLP-1 analog and/or DPPIV inhibitor response in a subject. In one embodiment, the composition comprises a solid support comprising probes for measuring a biomarker panel comprising, for example, adiponectin, C-peptide, hsCRP, insulin, proinsulin. The simultaneous use of multiple biomarkers with independent classification power will increase the performance of the biomarker panel in characterizing GLP-1 analog and DPPIV inhibitor response. The invention also provides methods of treating a subject (e.g. one experiencing cardiodiabetes) and determining the efficacy of a therapy through assaying the various biomarkers of a biomarker panel disclosed herein.Type: ApplicationFiled: January 23, 2012Publication date: August 7, 2014Applicant: IR2DX, Inc.Inventor: Andreas Pfuetzner
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Patent number: 8796307Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.Type: GrantFiled: November 11, 2013Date of Patent: August 5, 2014Assignee: Novartis AGInventors: Bernard Cuenoud, Ian Bruce, Robin Alec Fairhurst, David Beattie
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Patent number: 8796001Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: August 5, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Zachary A. Buchan, Michael T. Sullenberger
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Patent number: 8796308Abstract: This invention relates to a compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein R is COOH or CH2OH.Type: GrantFiled: November 19, 2013Date of Patent: August 5, 2014Assignee: Vertex Pharamaceuticals IncorporatedInventors: Xiaoqing Yang, Sara Sabina Hadida Ruah, Peter Diederik Jan Grootenhuis, Fredrick F. Van Goor, Martyn Curtis Botfield, Gregor Zlokarnik
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Publication number: 20140213538Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: January 15, 2014Publication date: July 31, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert, Shendong Yuan
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Publication number: 20140213612Abstract: Methods of treatment of multiple sclerosis (MS) with PPAR? agonists, and in particular with the compound of formula (I) known as INT131:Type: ApplicationFiled: January 23, 2014Publication date: July 31, 2014Applicant: InteKrin Therapeutics, Inc.Inventor: David Weinstein
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Publication number: 20140213613Abstract: A novel crystalline form of a compound is disclosed.Type: ApplicationFiled: August 31, 2012Publication date: July 31, 2014Inventor: Mei-yin Lee
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Patent number: 8791090Abstract: Disclosed is a compound which has a low molecular weight and has an activity of enhancing the production of EPO and/or an activity of enhancing the production of hemoglobin.Type: GrantFiled: March 31, 2010Date of Patent: July 29, 2014Assignee: Kowa Company, Ltd.Inventors: Masanori Ashikawa, Junya Tagashira, Akiyasu Koketsu, Toshiharu Morimoto, Takahiro Kitamura, Syunji Takemura, Gen Watanabe, Tatsuaki Nishiyama, Satoshi Goda, Masaki Yamabi, Takeshi Doi, Hiroyuki Ishiwata
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Publication number: 20140206661Abstract: The present invention provides a compound of Formula (X) or a pharmaceutically acceptable salt thereof; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicant: NOVARTIS AGInventors: Jake AXFORD, Natalie DALES, Moo Je SUNG
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Publication number: 20140206720Abstract: The present invention relates to formulations of 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid in Form I, pharmaceutical packs or kits thereof, and methods of treatment therewith.Type: ApplicationFiled: March 19, 2014Publication date: July 24, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventor: Christopher Young
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Publication number: 20140206676Abstract: In one aspect, the invention relates to substituted 4-(1H-pyrazol-4-yl)benzyl analogs compounds, derivatives thereof, and related compounds, which are useful as positive allosteric modulators of the muscarinic acetylcholine receptor M1 (mAChR M1); synthesis methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating neurological and psychiatric disorders associated with muscarinic acetylcholine receptor dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: January 12, 2013Publication date: July 24, 2014Applicant: Vanderbilt UniversityInventors: Craig W. Lindsley, P. Jeffrey Conn, Michael R. Wood, Bruce J. Melancon, Michael S. Poslusney, James C. Tarr
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Patent number: 8785476Abstract: The present invention relates to solid state forms of N-[2,4-bis(1,1-dimethylethyl)-5-hydroxyphenyl]-1,4-dihydro-4-oxoquinoline-3-carboxamide (Compound 1), pharmaceutical compositions thereof and methods therewith.Type: GrantFiled: November 20, 2012Date of Patent: July 22, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sneha G. Arekar, Steven C. Johnston, Mariusz Krawiec, Ales Medek, Praveen Mudunuri, Mark Jeffrey Sullivan
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Patent number: 8785475Abstract: Lipoic acid derivatives and pharmaceutical formulations containing lipoic acid derivatives are useful in the treatment and prevention of disease characterized by disease cells that are sensitive to lipoic acid derivatives.Type: GrantFiled: April 17, 2008Date of Patent: July 22, 2014Assignee: Cornerstone Pharmaceuticals, Inc.Inventors: Paul Bingham, Tom Kwok, Zuzana Zachar
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Publication number: 20140200215Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: March 12, 2013Publication date: July 17, 2014Inventors: Brad Owen Buckman, John Beamond Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Publication number: 20140200243Abstract: This application provides for a method of treating a subject suffering from Crohn's disease, the method comprising periodically administering to the subject an amount of laquinimod or pharmaceutically acceptable salt thereof effective to treat the subject. This application provides for use of laquinimod in the manufacture of a medicament for treating a subject suffering from Crohn's disease. This application also provides for a pharmaceutical composition comprising laquinimod for use in treating a subject suffering from Crohn's disease.Type: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Applicant: TEVA PHARMACEUTICAL INDUSTRIES, LTD.Inventors: Nora Tarcic, Asi Haviv, Eran Blaugrund, Joel Kaye
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Publication number: 20140200239Abstract: The present invention provides new compounds of formula I, II or III, which have Src homology-2 containing protein tyrosine phosphatase-1 (SHP-1) agonist activity. Also provided are treatment methods using the compounds of formula I, II or III.Type: ApplicationFiled: August 3, 2012Publication date: July 17, 2014Applicant: National Taiwan UniversityInventors: Chung-Wai Shiau, Kuen-Feng Chen
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Publication number: 20140200242Abstract: The present invention is directed to processes for making and compositions containing quinolines such as formula I or pharmaceutically acceptable salts thereof wherein: X1 is H, Br, CI, or X2 is H, Br, CI, or n1 is 1-2; and n2 is 1-2.Type: ApplicationFiled: February 10, 2012Publication date: July 17, 2014Applicant: Exelixis, Inc.Inventor: Jo Ann Wilson
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Patent number: 8778966Abstract: The present invention provides compounds of formula (I), their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7, n, m and X have defined meanings.Type: GrantFiled: September 14, 2012Date of Patent: July 15, 2014Assignee: Janssen Pharmaceutica, NVInventors: Jorge Eduardo Vialard, Patrick René Angibaud, Laurence Anne Mevellec, Christophe Meyer, Eddy Jean Edgard Freyne, Isabelle Noëlle Constance Pilatte, Bruno Roux, Elisabeth Thèrése Jeanne Pasquier, Xavier Marc Bourdrez, Christophe Denis Adelinet, Laurence Françoise Bernadette Marconnet-Decrane, Jacqueline Anne Macritchie, James Edward Stewart Duffy, Andrew Pate Owens, Pierre-Henri Storck, Virginie Sophie Poncelet
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Patent number: 8778965Abstract: It is intended to provide a lotion preparation which exerts an excellent antibacterial effect, is excellent in the stability of active ingredient and does not contain an additive having a safety problem. The lotion preparation contains (a) 1-cyclo-propyl-8-methyl-7-[5-methyl-6-(methylamino)-3-pyridyl]-4-oxo-1,4-dihydro-3-quinolinecarboxylic acid and/or a pharmaceutically acceptable salt thereof, (b) a lower alcohol, (c) a water-soluble polymer and (d) a polyhydric alcohol and the pH of the preparation is in the range of 9 to 12.Type: GrantFiled: July 31, 2006Date of Patent: July 15, 2014Assignee: Maruho Co., Ltd.Inventor: Tsuyoshi Hirota
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Patent number: 8779146Abstract: The invention relates to improvements of the physiochemical and/or the pharmaceutical properties of cilostazol. Disclosed herein are several new compositions and cocrystals of cilostazol, including: a 1:1 cilostazol gentisic acid cocrystal, a 1:1:1 cilostazol gentisic acid H2O cocrystal, a 1:1 cilostazol 4-hydroxybenzoic acid cocrystal, and a 1:1 cilostazol 2,4-dihydroxybenzoic acid cocrystal. The therapeutic methods and uses of these cilostazol cocrystals are described as well as therapeutic compositions containing them.Type: GrantFiled: April 28, 2011Date of Patent: July 15, 2014Assignee: Nuformix LimitedInventors: Alan Chorlton, Christopher Frampton, Daniel Gooding, Joanne Holland
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Patent number: 8772317Abstract: The invention provides a rebamipide-containing aqueous pharmaceutical suspension which can be prepared by a simple process and keep the dispersed fine-particle state of rebamipide stable without having the fine particle agglutinated. The rebamipide-containing aqueous pharmaceutical suspension of the invention is prepared by mixing polyvinyl alcohol and additionally a sodium salt compound with rebamipide.Type: GrantFiled: October 24, 2007Date of Patent: July 8, 2014Assignee: Otsuka Pharmaceutical Co., Ltd.Inventor: Yoshito Masuda
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Patent number: 8772493Abstract: The present invention relates to a compound represented by formula 1 in the present specification or a pharmaceutically acceptable thereof, which inhibits an apoptosis mechanism of auditory hair cells for various ototoxicities leading to deafness, and protects the auditory organ and hearing, a method for preparation thereof, and a composition containing the same.Type: GrantFiled: December 11, 2012Date of Patent: July 8, 2014Assignees: Ajou University Industry-Academic Cooperation Foundation, Korea Research Institute of Chemical TechnologyInventors: Chul Ho Kim, Young Sik Jung
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Publication number: 20140187519Abstract: Provided herein are diagnostic markers and uses thereof for predicting if a subject is at risk of a major adverse event. In particular, one aspect provided herein relates to methods to determine if a subject is at risk of having a major adverse effect by measuring at least 2, or at least 3 of the biomarkers beta 2 microglobulin, c-reactive protein and cystatin C.Type: ApplicationFiled: December 3, 2013Publication date: July 3, 2014Applicant: The Board Of Trustees Of The Leland Stanford Junior UniversityInventors: John P. Cooke, Nicholas J. Leeper, Kevin Nead
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Publication number: 20140186329Abstract: The present invention provides methods of use of polyphenol compounds for treating, preventing, mitigating and delaying ischemia or a condition where ischemia occurs. In one embodiment, the method comprises providing a polyphenol analog; and administering the polyphenol analog to a subject to treat ischemia or a condition where ischemia occurs. Various embodiments of the present invention are useful for the treatment of patients having, or at risk for, any of (1) ischemic stroke, (2) hemorrhagic stroke, (3) cardiovascular disease, (4) ischemia related spinal cord injury, (5) ischemia in diabetic patients, or (6) embolic stroke. For example, use of the polyphenol compounds can maintain glutathione levels in the patient.Type: ApplicationFiled: February 6, 2014Publication date: July 3, 2014Inventors: Paul A. Lapchak, David R. Schubert, Pamela A. Maher, Chandramouli Chiruta
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Publication number: 20140187550Abstract: A compound of formula (I): in free or salt form, wherein R1, R3, Qa, Qb and Q are as defined herein, for the treatment of a disease mediated by the S1P2 or S1P3 receptor, such as inflammatory or obstructive airways disease.Type: ApplicationFiled: December 16, 2013Publication date: July 3, 2014Applicant: Novartis AGInventor: Roger John Taylor
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Publication number: 20140187510Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.Type: ApplicationFiled: July 11, 2013Publication date: July 3, 2014Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATIONInventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
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Publication number: 20140186328Abstract: The present invention provides neuroprotective polyphenol compounds, which can be synthetic analogs of fisetin, baicalein or chlorogenic acid, that maintain neuroprotective, anti-inflammatory, glutathione promoting, and/or antioxidant properties. The neuroprotective polyphenol compounds are useful for promoting, enhancing and/or increasing neuron protection, growth and/or regeneration. The polyphenol compounds further find use for increasing and or maintaining intracellular glutathione (GSH) levels. The polyphenol compounds are also useful for treating, preventing, mitigating and/or delaying neurodegenerative conditions, including diabetes, Parkinson's disease, Huntington's disease, Alzheimer's disease, non-Alzheimer's dementias, multiple sclerosis, traumatic brain injury, spinal cord injury or ALS.Type: ApplicationFiled: February 5, 2014Publication date: July 3, 2014Applicant: Salk Institute for Biological StudiesInventors: David R. Schubert, Pamela A. Maher, Chandramouli Chiruta
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Publication number: 20140187578Abstract: The invention provides pharmaceutical stable semisolid topical compositions comprising between 0.2 to 5% of a des-fluoroquinolone compound, and a suitable carrier to manufacture an ointment or a cream.Type: ApplicationFiled: March 5, 2014Publication date: July 3, 2014Applicant: Ferrer Internacional, S.A.Inventors: Cristina TARRAGO, Benjamin SANTOS, Manuel RAGA, Antonio Guglietta
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Publication number: 20140187577Abstract: Biomarkers are provided that are predictive of a subject's responsiveness to a therapy comprising lenvatinib or a pharmaceutically acceptable salt thereof (e.g., lenvatinib mesylate). The biomarkers, compositions, and methods described herein are useful in selecting appropriate treatment modalities for a subject having cancer (e.g., thyroid cancer, kidney cancer), suspected of having cancer, or at risk of developing cancer.Type: ApplicationFiled: May 31, 2012Publication date: July 3, 2014Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Yasuhiro Funahashi, Tadashi Kadowaki, Junji Matsui, Jason S. Simon, Lucy Xu
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Patent number: 8765723Abstract: This invention relates to novel compounds which are derivatives of the phosphodiesterase inhibitor, cilostazol and pharmaceutically acceptable salts thereof. This invention also provides pyrogen-free compositions comprising one or more compounds of the invention and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are treated by administration of a phosphodiesterase inhibitor, such as cilostazol. The invention also relates to the use of the disclosed compounds and compositions as reagents in analytical studies involving cilostazol.Type: GrantFiled: January 7, 2013Date of Patent: July 1, 2014Assignee: CoNCERT Pharmaceuticals, Inc.Inventors: Rose A. Persichetti, Julie F. Liu, Craig E. Masse, Scott L. Harbeson
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Patent number: 8765752Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is O or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: GrantFiled: March 15, 2013Date of Patent: July 1, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140179675Abstract: The present invention provides a compound represented by the formula (I) wherein X is a hydrogen atom or a fluorine atom; R is a hydrogen atom or alkyl; R1 is (1) cyclopropyl optionally substituted by 1 to 3 halogen atoms or (2) phenyl optionally substituted by 1 to 3 halogen atoms; R2 is alkyl, alkoxy, haloalkoxy, a halogen atom, cyano, etc.; and R3 is 7-oxo-7,8-dihydro-1,8-naphthyridinyl, 3-pyridyl, etc., or a salt thereof. The compound of the present invention has excellent antimicrobial activity against Clostridium difficile and is useful for the prevention or treatment of intestinal infection such as Clostridium difficile-associated diarrhea.Type: ApplicationFiled: February 28, 2014Publication date: June 26, 2014Applicant: OTSUKA PHARMACEUTICAL CO., LTD.Inventors: Mamuti ABUDUSAIMI, Fangguo YE, Jiangqin SUN, Hisashi MIYAMOTO, Jay-Fei CHENG, Daisuke OKA
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Publication number: 20140179679Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.Type: ApplicationFiled: October 21, 2013Publication date: June 26, 2014Applicant: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUEInventors: Piona Dariavach, Pierre Emile Ulysse Martineau, Bruno Villoutreix
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Publication number: 20140179736Abstract: This invention is directed to the treatment of cancer, particularly lung cancer, breast cancer, melanoma, renal cell carcinoma, thyroid cancer that has metastasized to the bone. The invention is also directed to a method for treating bone cancer pain in an individual in need of such treatment comprising administering to the individual an effective amount of a compound of Formula I.Type: ApplicationFiled: May 2, 2012Publication date: June 26, 2014Applicant: Exelixis, Inc.Inventors: Gisela Schwab, Dana T. Aftab
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Publication number: 20140179647Abstract: 1-Phenyl-2-pyridinyl alkyl alcohol compounds are effective as inhibitors of the phosphodiesterase 4 (PDE4) enzyme and may be used to prevent and/or treat certain diseases or conditions.Type: ApplicationFiled: December 17, 2013Publication date: June 26, 2014Applicant: CHIESI FARMACEUTICI S.p.A.Inventors: GABRIELE AMARI, ELISABETTA ARMANI, MAURIZIO DELCANALE
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Publication number: 20140171490Abstract: Disclosed is the use of a mist of a pharmaceutical composition for ophthalmic delivery of a protein or peptide active pharmaceutical ingredient, a related method of treatment and a device useful in implementing the use and method. Disclosed is also the use of a mist for ophthalmic delivery of a pharmaceutical composition including a highly irritating penetration enhancer and an ophthalmically acceptable carrier, a related method of treatment and a device useful in implementing the use and method. Disclosed is also a device for ophthalmic administration configured to direct a mist of a pharmaceutical composition to the eye only when the eye is open. Disclosed is also a self-sterlizing device for ophthalmic administration. Disclosed is also a device and a method for increasing the bioavailability of an ophthalmically administered API in a pharmaceutical composition.Type: ApplicationFiled: August 9, 2013Publication date: June 19, 2014Applicant: PHARMALINGT INC.Inventors: Yossi Gross, Rafi Herzog, Steven B. Koevary
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Publication number: 20140171455Abstract: Methods for deterring microglia-mediated neurotoxicity in a human or non-human animal subjects comprising the step of inhibiting or blocking the intermediate-conductance calcium-activated potassium channel Kv1.3 in microglia, such as in subjects how suffer from neurodegenerative diseases (e.g., Alzheimer's Disease) or ischemic/anoxic/hypoxic conditions. The inhibition or blocking of the KCa1.3 channels may be accomplished by administering a substance that inhibits Kv1.3 in microglia. Examples of Kv1.3 inhibiting substances include certain 5-phenoxyalkoxypsoralens, such as (4-Phenoxybutoxy)psoralen (PAP-1) as well as certain 4-phenoxybutoxy-substituted heterocyclic compounds.Type: ApplicationFiled: June 8, 2012Publication date: June 19, 2014Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Lee-Way Jin, Izumi Meezawa
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Publication number: 20140171431Abstract: The present invention relates to the field of pharmaceutical chemistry, and in particular, to a novel class of azole compounds represented by general formula (I), (II) or (III) and a preparation method thereof, a pharmaceutical composition with the compounds as active components, and a use of the azole compounds and the pharmaceutical composition in the preparation of a medicament for treatment of diseases associated with Lp-PLA2 enzyme activities, wherein each substituent is as defined in the specification.Type: ApplicationFiled: May 15, 2012Publication date: June 19, 2014Inventors: Jianhua Shen, Yiping Wang, Kai Wang
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Patent number: 8754104Abstract: A stable solid pharmaceutical composition consisting essentially of an effective amount of a crystalline salt of formula (II) together with an alkaline-reacting component maintaining the pH preferably above 8, or a salt with a divalent metal cation; and at least one pharmaceutical excipient; said salt of formula (II) being essentially stable during storage at room temperature for a period of at least 3 years. A process for stabilizing the salt of formula (II). A crystalline salt of formula (II) and a process for preparing said salt.Type: GrantFiled: November 6, 2012Date of Patent: June 17, 2014Assignee: Active Biotech ABInventors: Karl Jansson, Tomas Fristedt, Hans Wannman, Anders Bjork
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Patent number: 8754105Abstract: Inhibitors of HCV replication of formula (I) the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms; wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituents; L is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(?O)—, —O—C(?O)—NR4a— or —O—C(?O)—NR4aC1-4 alkanediyl-; R2 is hydrogen, —OR5, —C(?O)OR5, —C(?O)R6, —C(?O)NR4aR4b, —C(?O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2; R3 is hydrogen, and wheType: GrantFiled: May 17, 2011Date of Patent: June 17, 2014Assignees: Medivir AB, Janssen R&D IrelandInventors: Kenneth Alan Simmen, Herman Augustinus De Kock, Pierre Jean-Marie Bernard Rabiosson, Abdellah Tahri, Karl Magnus Nilsson, Bengt Bertil Samuelsson, Asa Annica Kristina Rosenquist, Dmitry Antonov
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Publication number: 20140163068Abstract: Pharmaceutical compositions comprising 3-(6-(1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)cyclopropanecarboxamido)-3-methylpyridin-2-yl)benzoic acid (Compound 1) in Form I and a solid dispersion comprising substantially amorphous N-(5-hydroxy-2,4-ditert-butyl-phenyl)-4-oxo-1H-quinoline-3-carboxamide (Compound 2), methods of treating, lessening the severity of, or symptomatically treating CFTR mediated diseases, such as cystic fibrosis, methods of manufacturing, methods of administering, and kits thereof are disclosed.Type: ApplicationFiled: November 1, 2013Publication date: June 12, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Marinus Jacobus Verwijs, Radhika Karkare, Michael Douglas Moore
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Publication number: 20140163011Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: December 19, 2013Publication date: June 12, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
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Patent number: 8748458Abstract: Compounds of the invention are of the formula (I); wherein: is a double bond and X is C; or is a single bond and X is N, CH or CQR1; and wherein: n is 1 to 10; R is H or QR1; each R? is independently selected from H and QR1; each Q is independently selected from a bond, CO, NH, S, SO, SO2 or O; each R1 is independently selected from C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, substituted or unsubstituted aryl or heteroaryl, acyl, C1-C10 cycloalkyl, halogen, C1-C10 alkylaryl or C1-C10 heterocycloalkyl; L is a nitrogen-containing heteroaryl; and W is a zinc-chelating residue; or a pharmaceutically acceptable salt thereof. The compounds are useful in therapy.Type: GrantFiled: January 26, 2010Date of Patent: June 10, 2014Assignee: Karus Therapeutics LimitedInventors: Stephen Joseph Shuttleworth, Cyrille Davy Tomassi