Ring Sulfur In The Bicyclo Ring System Patents (Class 514/301)
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Publication number: 20140329836Abstract: This invention provides compounds of formula (I): wherein R1, R2, G, n, p and q have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: December 5, 2013Publication date: November 6, 2014Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Publication number: 20140329675Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 3, 2014Publication date: November 6, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140329781Abstract: The present invention relates to a once-a-day therapeutically synergistic pharmaceutical dosage form for treatment of cardiovascular disorders, wherein the dosage form comprises a fixed dose combination of metoprolol in extended release form and one or more antiplatelet agent along with one or more rate controlling excipients.Type: ApplicationFiled: November 1, 2012Publication date: November 6, 2014Applicant: WOCKHARDT LIMITEDInventors: Mandar Kodgule, Amit Gupta, Premchand Nakhat, Girish Kumar Jain
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Publication number: 20140329674Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.Type: ApplicationFiled: May 3, 2014Publication date: November 6, 2014Applicant: INSCENT, INC.Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
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Publication number: 20140329851Abstract: The present application describes deuterium-enriched prasugrel, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: February 7, 2014Publication date: November 6, 2014Applicant: DEUTERX, LLCInventor: Anthony W. Czarnik
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Patent number: 8877683Abstract: The present invention provides substituted pyridine compounds of the formula I or N-oxides or agriculturally suitable salts thereof, wherein the variables in the formula I are defined as in the description. Substituted pyridines of formula I are useful as herbicides.Type: GrantFiled: December 19, 2011Date of Patent: November 4, 2014Assignee: BASF SEInventors: Matthias Witschel, William Karl Moberg, Liliana Parra Rapado, Gilbert Besong, Michael Rack, Andree Van Der Kloet, Thomas Seitz, Ruediger Reingruber, Helmut Kraus, Johannes Hutzler, Trevor William Newton, Jens Lerchl, Klaus Kreuz, Klaus Grossmann, Richard Roger Evans
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Publication number: 20140323482Abstract: The present invention provides a compound of Formula I (The formula should be inserted here) as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: December 17, 2012Publication date: October 30, 2014Inventors: Yao Ma, Manami Shizuka, Timothy J. Guzi, Yuan Liu, Yuan Tian, Brian R. Lahue, Craig R. Gibeau, Gerald W. Shipps, JR., Yaolin Wang, Stephane L. Bogen, Latha G. Nair, Weidong Pan, Mark A. McCoy, Matthew E. Voss, Margarita Kirova-Snover, W. Bent Clayton
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Publication number: 20140314676Abstract: The current application is directed to methods of treating or ameliorating myocardial ischemia, an acute coronary event, and a myocardial reperfusion injury comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient in need thereof. The application is also directed to reducing the risk for myocardial reperfusion injury as well as promoting the beneficial remodeling of cardiac tissue in a patient, comprising administering a therapeutically effective amount of deferiprone or a pharmaceutically acceptable salt thereof to a patient before, during or after reperfusion therapy. The application also includes methods of selecting a patient for treatment of reperfusion injury and subsequently treating the selected patient.Type: ApplicationFiled: November 16, 2012Publication date: October 23, 2014Inventors: Michael Spino, John Chalmers Connelly, John Charles Wood, Graham Arnold Wright, Nilesh Ramesh Ghugre
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Publication number: 20140315801Abstract: This invention relates to methods for treating cell proliferative diseases and conditions and ophthalmic diseases, disorders and conditions using compounds that inhibit protein tyrosine kinase activity. In particular the invention relates to the methods of treatment which utilize compounds that inhibit the protein tyrosine kinase activity of growth factor receptors, resulting in the inhibition of receptor signaling, for example, the inhibition of VEGF receptor signaling.Type: ApplicationFiled: June 18, 2014Publication date: October 23, 2014Inventors: Stéphane Raeppel, Franck Raeppel, Stephen William Claridge, Lijie Zhan, Frederic Gaudette, Michael Mannion, Norifumi Sato, Yohei Yuki, Masashi Kishida, Arkadii Vaisburg
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Patent number: 8865736Abstract: Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ?C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.Type: GrantFiled: November 28, 2011Date of Patent: October 21, 2014Assignee: Biota Scientific Pty LtdInventors: David Ryall Brown, Ian Collins, Lloyd George Czaplewski, David John Haydon
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Publication number: 20140303119Abstract: The present invention teaches a method and new use for anticoagulant compounds for the treatment of central retinal vein occlusion (CRVO) and branch retinal vein occlusion (BRVO) and other conditions. CRVO and BRVO represent debilitating conditions for which there is currently no effective therapy. The present invention teaches a new therapy, including new uses for existing pharmacological agents, comprising enoxaparin sodium, warfarin, clopidrogel, and others, in the treatment of these and other conditions.Type: ApplicationFiled: March 12, 2013Publication date: October 9, 2014Applicant: DiLorenzo Biomedical, LLCInventor: Daniel John DiLorenzo
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Publication number: 20140303149Abstract: Compounds of the formula I or II: wherein X, m, Ar, R1 and R2 are as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.Type: ApplicationFiled: April 2, 2014Publication date: October 9, 2014Applicant: Hoffmann-La Roche Inc.Inventors: Nidhi Arora, Shaoqing Chen, Johannes Cornelius Hermann, Andreas Kuglstatter, Sharada Shenvi Labadie, Clara Jeou Jen Lin, Matthew C. Lucas, Amy Geraldine Moore, Eva Papp, Francisco Xavier Talamas, Jutta Wanner, Yansheng Zhai
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Patent number: 8853238Abstract: A fused heterocyclic compound the formula (1): wherein A1 represents —NR8—, and the like; A2 represents a nitrogen atom, and the like; A3 represents a nitrogen atom, and the like; R1 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R2, R3, R4, and R5 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more halogen atoms, and the like; R6 and R7 are same or different and represent independently a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group X, and the like; R8 represents a C1-C6 chain hydrocarbon group optionally having one or more atoms or groups selected from Group W, and the like; n represents 0, 1 or 2. The compound has an excellent activity of controlling pests.Type: GrantFiled: December 22, 2011Date of Patent: October 7, 2014Assignee: Sumitomo Chemical Company, LimitedInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Publication number: 20140296285Abstract: A method of inhibiting microorganism growth comprising administering an effective amount of a composition including a compound selected from the group consisting of to the microorganism.Type: ApplicationFiled: June 16, 2014Publication date: October 2, 2014Inventors: Gengliang YANG, Zhengyue MA, Wei TIAN, Baoling FANG, Ge WANG, Linbo LI, Chunliu YANG, Ligai BAI
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Publication number: 20140294805Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 2, 2014Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Peter Dragovich, Francis Gosselin, Bingsong Han, Jian Lin, Dominic J. Reynolds, Bruce Roth, Chase C. Smith, Zhongguo Wang, Po-Wai Yuen, Xiaozhang Zheng
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Publication number: 20140296169Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: June 18, 2014Publication date: October 2, 2014Inventors: Hauke SZILLAT, Thomas LEEUW, Martin LORENZ
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Publication number: 20140296272Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
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Publication number: 20140296284Abstract: Citrate salts of N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea and crystalline forms thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.Type: ApplicationFiled: December 16, 2013Publication date: October 2, 2014Inventors: Geoff G. Zhang, Douglas H. Hoffman, Jonathan M. Miller
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Patent number: 8841462Abstract: The invention relates to bicyclic heterocycles of formulae I and II with anti-cancer and/or anti-inflammatory activity and more specifically with MEK kinase inhibitory activity. The invention provides compositions and methods useful for inhibiting abnormal cell growth, treating a hyperproliferative disorder, or treating an inflammatory disease in a mammal. The invention also relates to methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: July 1, 2009Date of Patent: September 23, 2014Inventors: Robert A. Heald, Philip Jackson, Joseph P. Lyssikatos, Stephen Price, Pascal Pierre Alexandre Savy
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Patent number: 8840923Abstract: Slow-release excipients which comprise an association of at least one glycogen and at least one alginate with an alkaline-earth metal salt are useful for the preparation of slow-release pharmaceutical formulations.Type: GrantFiled: December 23, 2008Date of Patent: September 23, 2014Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.Inventors: Vincenzo Russo, Elisa Liberati, Nicola Cazzolla, Leonardo Marchitto, Lorella Ragni
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Publication number: 20140274975Abstract: The invention provides methods and compositions for diagnosing prior ischemic stroke or transient ischemic attack (TIA) and approximate the time said stroke occurred, comprising measurement of IgG and IgM antibodies to NR2A and/or NR2B NMDA receptor or fragment thereof in a biological sample, and comparing those measurements to reference population standards and to each other. The invention also includes optionally measuring other biomarkers for autoimmune disease for the reduction in false positives and better risk stratification for future stroke events. The method is particularly useful for identifying individuals that are at risk for future stroke or TIA, and for diagnosing previous history of ischemic stroke or TIA. This measurement and comparison enables determination of the risk of future stroke which is by definition higher in those patients who have suffered a previous stroke.Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: Health Diagnostic Laboratory, Inc.Inventors: Rebecca E. CAFFREY, Mohmed ASHMAIG
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Publication number: 20140271816Abstract: The composition of the invention, liposomal glutathione in combination with clopidogrel has utility for improving the efficacy of clopidogrel in preventing the aggregation of platelet that can lead to clotting. The prevention of platelet aggregation has widespread utilization in many cardiovascular conditions such as coronary artery narrowing and more consistent “antiplatelet” activity is found with the invention, the combination of clopidogrel and liposomal reduced glutathione.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventor: Frederick Timothy Guilford
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Publication number: 20140275070Abstract: The present invention relates generally to thienopyrimidine and thienopyridine class compounds and methods of use thereof. In particular embodiments, the present invention provides compositions comprising thienopyrimidine class compounds and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins (e.g., for the treatment of leukemia, solid cancers and other diseases dependent on activity of MLL1 and MLL2 or menin).Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Jolanta Grembecka, Tomasz Cierpicki, Dmitry Borkin, Jay L. Hess, Duxin Sun, Xiaoqin Li
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Patent number: 8835407Abstract: The present invention is directed to pharmaceutical compositions comprising prasugrel and a cyclodextrin derivative, and methods of making and using the same.Type: GrantFiled: July 5, 2012Date of Patent: September 16, 2014Assignee: CyDex Pharmaceuticals, Inc.Inventors: Gerold L. Mosher, Stephen G. Machatha, Daniel J. Cushing
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Publication number: 20140256680Abstract: A pharmaceutical combination comprising a BRAF inhibitor, and an Hsp90 inhibitor according to the following formulae (I): or a tautomer, or a pharmaceutically acceptable salt thereof, wherein the variables are defined therein. Also provided is a method for treating a proliferative disorder in a subject in need thereof, using the pharmaceutical combination described herein.Type: ApplicationFiled: November 14, 2012Publication date: September 11, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Jaime Acquaviva
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Publication number: 20140256711Abstract: Disclosed are an anti-angiogenic compound, represented by Chemical Formula I, or a pharmaceutically acceptable salt thereof, a preparation method thereof, and a pharmaceutically acceptable composition including the same. Because the compound of Chemical Formula I potently suppresses the angiogenesis, the compound of Chemical Formula I is applicable to the prevention and treatment of diseases caused by aberrant activity of vascular endothelial growth factor, and available as an anti-angiogenic agent.Type: ApplicationFiled: July 27, 2012Publication date: September 11, 2014Applicant: Boryung Pharmaceutical Co., Ltd.Inventors: Ji Han Kim, Je Hak Kim, Joon Kwang Lee, Hahn-Sun Jung, Nam Seok Han, Yong Park, Seung-Hoon Kang, Hee Jin Jeong, Kyung-Tae Lee, Hye Eun Choi, Yong Ha Chi, Joo Han Lee, Soo Heui Paik
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Publication number: 20140248240Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: September 4, 2014Inventors: Kenneth W. Bair, Timm Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Judith D. Kuntz, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng
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Patent number: 8816086Abstract: A process for the preparation of compounds of formula (I) or a salt thereof wherein X1, X2, X3, X4, Rx, u, R2, R1g, z, and A1 are as defined in the specification is disclosed.Type: GrantFiled: December 15, 2010Date of Patent: August 26, 2014Assignee: AbbVie Inc.Inventors: Yu-Ming Pu, Alan Christesen, Steven Cullen, Yi-Yin Ku
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Publication number: 20140235668Abstract: 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: March 13, 2014Publication date: August 21, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Peter D.J. Grootenhuis, Sara Hadida Ruah, Jinglan Zhou
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Patent number: 8809366Abstract: A compound with the structure of the formula (I) or a pharmaceutically acceptable salt, a preparation method and use thereof are disclosed in the present invention, wherein R is cyano group. The compound provided by the present invention has an antiplatelet aggregation activity and can be used in preparing a medicament for preventing or treating cardiac and cerebral vascular diseases such as coronary artery syndromes, myocardial infarction and myocardial ischemia which are caused by platelet aggregation.Type: GrantFiled: November 12, 2012Date of Patent: August 19, 2014Assignee: Tianjin Institute of Pharmaceutical ResearchInventors: Dengke Liu, Ying Liu, Nan Yue, Furong Chen, Chubing Tan, Yunsong Zhou, Peng Liu, Yigui Zhao, Deguang Zhi, Mo Liu, Bingni Liu, Changjiang Huang, Lida Tang
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Patent number: 8809534Abstract: The present invention is directed to novel compounds of Formula I. The compounds of the present invention are potent tyrosine kinase modulators, and are suitable for the treatment and prevention of diseases and conditions related to abnormal activities of tyrosine kinase receptors.Type: GrantFiled: September 3, 2010Date of Patent: August 19, 2014Assignee: Allergan, Inc.Inventors: Xialing Guo, Zhen Zhu
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Publication number: 20140228394Abstract: The present invention provides compounds of Formula (I) and (II), or a pharmaceutically acceptable salts thereof, where R53, R54, p, q, and n are as defined herein. The compounds of the present invention have been found to be useful as 17?-hydroxylase/C17,20-lyase inhibitors.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Novartis AGInventors: Mark Gary BOCK, Christoph GAUL, Venkateshwar Rao GUMMADI, Saumitra SENGUPTA
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Publication number: 20140227360Abstract: The present disclosure provides ready-to-use, oil/water emulsion compositions with mean droplet size (intensity-average, m) of 100-500 nm, wherein the oil phase comprises clopidogrel free base dispersed in pharmaceutical acceptable oil(s). The emulsion uses clopidogrel free base or premix of clopidogrel free base in oil(s) as the starting materials and may also contain one or more excipients such as surfactant and or co-surfactant, osmotic agent, pH adjustment agent, antioxidant, preservative, sweetener, and/or suspending agent, etc. The emulsion formulations and method of manufacturing significantly improves the stability of clopidogrel over other aqueous based formulations (such as cyclodextrin-based formulations and emulsion made using clopidogrel salt as the starting materials) with respect to chiral degradation, hydrolytic, and thermal degradation.Type: ApplicationFiled: February 6, 2014Publication date: August 14, 2014Inventor: Jingjun Huang
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Publication number: 20140228395Abstract: The present invention relates to novel N-(imidazolidin-2-ylidene)-heterocyclo penta[b]pyridine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: April 21, 2014Publication date: August 14, 2014Applicant: Allergan, Inc.Inventors: SANTOSH C. SINHA, LIMING WANG, KEN CHOW, MOHAMMED I. DIBAS, MICHAEL E. GARST
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Patent number: 8802854Abstract: Salts of prasugrel were prepared including, for example, crystalline forms of prasugrel hydrobromide. These salts are useful, for example, in medicaments that inhibit the aggregation of platelets.Type: GrantFiled: April 7, 2011Date of Patent: August 12, 2014Assignee: Teva Pharmaceutical Industries Ltd.Inventors: Mihaela Tuksar, Tomislav Biljan, Miroslav Zegarac
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Publication number: 20140221422Abstract: The present invention relates to novel compounds capable of modulating the stability and/or activity of hypoxia inducible factor (HIF).Type: ApplicationFiled: April 9, 2014Publication date: August 7, 2014Applicant: FIBROGEN, INC.Inventors: Eric D. Turtle, Lee A. Flippin, Michael P. Arend, Heng Cheng
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Publication number: 20140221349Abstract: Compounds of general formula I wherein the group R1 is defined as in claim 1, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.Type: ApplicationFiled: February 3, 2014Publication date: August 7, 2014Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventor: Matthias ECKHARDT
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Patent number: 8796262Abstract: This invention relates to new fused heterocyclic derivatives having affinity to S1P receptors, a pharmaceutical composition containing said compounds, as well as the use of said compounds for the preparation of a medicament for treating, alleviating or preventing diseases and conditions in which any S1P receptor is involved or in which modulation of the endogenous S1P signaling system via any S1P receptor is involved.Type: GrantFiled: July 8, 2011Date of Patent: August 5, 2014Assignees: AbbVie B.V., AbbVie Inc.Inventors: Pieter Smid, Wouter I. Iwema Bakker, Hein K. A. C. Coolen, Leonardus A. J. M. Sliedregt, Maria J. P. van Dongen, Jacobus A. J. den Hartog, Adrian Hobson
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Patent number: 8796271Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: GrantFiled: August 11, 2011Date of Patent: August 5, 2014Assignee: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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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: 20140212355Abstract: It is provided herein methods, devices, and compositions for trans-arterial local delivery of therapeutic agent for the treatment of liver cancers.Type: ApplicationFiled: January 28, 2013Publication date: July 31, 2014Applicant: Abbott Cardiovascular Systems Inc.Inventors: Mikael TROLLSAS, Syed Hossainy, John Stankus, Paul Consigny
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Publication number: 20140213554Abstract: Compounds active on c-kit protein kinases or mutant c-kit protein kinases having any mutations are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of the c-kit protein kinases and/or mutant c-kit protein kinases.Type: ApplicationFiled: December 20, 2013Publication date: July 31, 2014Inventors: Guoxian Wu, Katrina Chan, Todd Ewing, Prabha N. Ibrahim, Jack Lin, Marika Nespi, Wayne Spevak, Ying Zhang
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Publication number: 20140206679Abstract: The present invention relates to a heterocyclic pyridone compound represented by General Formula (I), where the heterocyclic pyridone compound is used as a tyrosine kinase inhibitor, and particularly a c-Met inhibitor. The present invention also relates to intermediates for preparing heterocyclic pyridone compound and a preparation method. The present invention further relates to a pharmaceutical composition containing the heterocyclic pyridone compound as an active ingredient, and a use of the pharmaceutical composition in treatment of diseases associated with tyrosine kinase c-Met, especially cancer associated with c-Met, as a medicament.Type: ApplicationFiled: May 28, 2012Publication date: July 24, 2014Applicant: SHANGHAI HUILUN LIFE SCIENCE & TECHNOLOGY CO., LTDInventors: Jianjun Cheng, Jihong Qin, Bin Ye
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Publication number: 20140206716Abstract: The present invention provides methods for predicting or determining a subject's response to an antiplatelet agent, and methods for determining a subject's suitability to a treatment regime or intervention for a disease associated with platelet aggregation, using analysis of genetic polymorphisms. The present invention also relates to the use of genetic polymorphisms in assessing a subject's response to an antiplatelet agent.Type: ApplicationFiled: January 8, 2014Publication date: July 24, 2014Applicant: Theranostics LaboratoryInventors: Patrick A. Gladding, Marja-Liisa Dahl, Mark W. Webster
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Publication number: 20140206680Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein G, p, R1, R2, R3a, R4, and R5 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating disorders, diseases, and conditions involving the immune system and inflammation, including rheumatoid arthritis, cancer, and other disorders, diseases, and conditions for which inhibition of SYK is indicated.Type: ApplicationFiled: June 20, 2012Publication date: July 24, 2014Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Mark E. Adams, Rongliang Chen, Mitsunori Kono, Betty Lam, Matthew Lardy, Srinivasa Reddy Natala, Steven James Wilkens, Zhe Nie
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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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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: 20140200240Abstract: Diagnostic methods for determining whether an individual will benefit from a particular anti-thrombotic therapeutic agent are disclosed. The methods involve obtaining a biological sample that comprises platelets, from a patient who has been pre-administered a particular therapeutic agent, which is an antagonist of a receptor associated with the biochemical pathways involved in platelet aggregation, and exposing the platelets to an agonist of the receptor. If the antagonist is ineffective, the platelets will eject microparticles, will have a different size distribution than platelets not exposed to the agonist, and will experience a change in their surface charge. In one embodiment, the diagnostic methods involve using single particle optical sizing techniques to determine the presence of such ejected microparticles, or a change in platelet size due to its activation by the agonist.Type: ApplicationFiled: July 20, 2012Publication date: July 17, 2014Inventor: Don Gabriel
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Publication number: 20140194462Abstract: The present application is related to compounds represented by Formula I, which are novel allosteric modulators of ?7nAChR. The application also discloses the treatment of disorders that are responsive to modulation of acetylcholine action on ?7nAChR in a mammal by administering an effective amount of a compound of Formula I.Type: ApplicationFiled: October 8, 2013Publication date: July 10, 2014Applicant: Anvyl LLCInventor: Richard Kanner
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Patent number: 8772488Abstract: The present application discloses crystals of 2-acetoxy-5-(?-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine hydrobromate, crystal compositions and pharmaceutical compositions comprising them and their use. The crystals of prasugrel hydrobromate of the present application possess excellent stability and solubility.Type: GrantFiled: March 31, 2010Date of Patent: July 8, 2014Assignees: Shanghai Institute of Pharmaceutical Industry, Chia Tai Tianqing Pharmaceutical Group Co., LtdInventors: Zhedong Yuan, Xingdong Cheng, Yulei Yang, Ling Tong, Xiong Yu, Laifang Zhang, Wenliang Zhou