Benzo Fused At 4,5-positions Of The Diazole Ring Patents (Class 514/394)
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Publication number: 20140039021Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: October 3, 2013Publication date: February 6, 2014Applicant: Gilead Sciences, Inc.Inventors: Elizabeth Bacon, Eda Canales, Aesop Cho, Jeromy Cottell, Mano Desai, Michael Graupe, Hongyan Guo, Randall Halcomb, Darryl Kato, Choung U. Kim, Thorsten A. Kirschberg, Evan Krygowski, Scott Lazerwith, John Link, Hongtao Liu, Qi Liu, Richard Mackman, Michael Mitchell, Jay Parrish, Hyung-Jung Pyun, Joseph Saugier, Scott Schroeder, Jianyu Sun, James Taylor, James Trenkle, Winston Tse, Randall Vivian, William Watkins, Lianhong Xu
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Patent number: 8642602Abstract: The present invention relates to the discovery of an epigenetic relay pathway that controls hepatic stellate cell activation and the wound-healing response in fibrogenesis, including fibrogenesis of the injured liver. Methods of inhibiting fibrogenesis, including liver fibrogenesis and secondary disease states and conditions thereof, and in treating liver damage, including cirrhosis of the liver (which may be caused by viruses or chemicals, including alcohol), are aspects of the present invention. The methods utilize certain nucleoside compounds and/or antibodies which are optionally conjugated. Pharmaceutical compositions represent additional aspects of the invention.Type: GrantFiled: February 2, 2010Date of Patent: February 4, 2014Assignees: University of Georgia Research Foundation, Inc., University of Newcastle Upon TyneInventors: Jelena Mann, Chung K. Chu, Derek A. Mann
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Publication number: 20140030260Abstract: The present invention regards compositions and methods for treating chronic lymphocytic leukemia in the in vivo tissue environment using selenium-containing compositions. In particular aspects, a selenium-comprising compound is administered to an individual wherein the CLL cells are in a stromal cell environment, wherein stromal factors modulate the selenium comprising compound to enhance its activity.Type: ApplicationFiled: November 22, 2011Publication date: January 30, 2014Applicant: BOARD OF REGENTS, THE UNIVERSITY OF TEXAS SYSTEMInventors: Peng Huang, Wan Zhang, Michael J. Keating
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Publication number: 20140030351Abstract: The present disclosure relates in part to pharmaceutical compositions comprising polymeric nanoparticles having certain glass transition temperatures. Other aspects of the invention include methods of making such nanoparticles.Type: ApplicationFiled: September 27, 2013Publication date: January 30, 2014Applicant: BIND Therapeutics, Inc.Inventors: Stephen E. Zale, Greg Troiano, Mir Mukkaram Ali, Jeff Hrkach, James Wright
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Publication number: 20140031317Abstract: The present invention is directed to a novel 2-substituted benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: ApplicationFiled: October 1, 2013Publication date: January 30, 2014Applicant: Janssen Pharmaceutica, NVInventors: Vernon C Alford, JR., James C. Lanter, Raymond A. Ng
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Patent number: 8637676Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: GrantFiled: June 4, 2008Date of Patent: January 28, 2014Assignee: Theravance, Inc.Inventors: Paul Allegretti, Seok-Ki Choi, Paul R. Fatheree, Roland Gendron, Ryan Hudson, Keith Jendza, Robert Murray McKinnell, Darren McMurtrie, Brooke Olson
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Publication number: 20140024691Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.Type: ApplicationFiled: September 19, 2013Publication date: January 23, 2014Applicant: Eagle Pharmaceuticals, Inc.Inventors: Nagesh R. Palepu, Philip Christopher Buxton
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Publication number: 20140024692Abstract: Embodiments of the invention relate to the treatment of neuropathic pain in mammals. Embodiments of the invention include methods for treating neuropathic pain with benzimidazole derivatives with PPARgamma agonist activity, as well as methods for preparing medicaments used in such treatments of mammalian pain.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: Aestus Therapeutics, Inc.Inventors: Lillian W. Chiang, Tage Honore
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Patent number: 8633235Abstract: Compounds of Formula (I) or pharmaceutically acceptable salts thereof; wherein R1, R2, R3, and R4 are as defined in the specification as well as salts and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: September 24, 2004Date of Patent: January 21, 2014Assignee: Neomed InstituteInventors: Ziping Liu, Daniel Pagé, Christopher Walpole, Hua Yang
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Publication number: 20140018368Abstract: The present invention provides compounds which antagonize hedgehog signaling and inhibit HDAC activity. The compounds can be used in methods of treating proliferative diseases and disorders such as cancer.Type: ApplicationFiled: July 1, 2013Publication date: January 16, 2014Applicants: Genetech, Inc., Curis, Inc.Inventors: Xiong Cai, Changgeng Qian, Haixiao Zhai
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Publication number: 20140018313Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: November 16, 2011Publication date: January 16, 2014Inventors: Elizabeth M. Bacon, Jeromy J. Cottell, Ashley Anne Katana, Darryl Kato, Evan S. Krygowski, John O. Link, James Taylor, Chinh Tran, Teresa Alejandra Trejo Martin, Zheng-Yu Yang, Sheila Zipfel
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Publication number: 20140018373Abstract: 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: ApplicationFiled: December 22, 2011Publication date: January 16, 2014Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: Hayato Takyo, Masaki Takahashi, Takamasa Tanabe, Yoshihiko Nokura, Mai Ito, Atsushi Iwata
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Publication number: 20140018334Abstract: In the present invention, there is provided an oral pharmaceutical composition, comprising bendamustine or a pharmaceutically acceptable, ester, salt or solvate thereof as an active ingredient, and a pharmaceutically acceptable excipient, which is a pharmaceutically acceptable non-ionic surfactant, selected from the group consisting of polyethoxylated castor oil or derivative thereof and a block copolymer of ethylene oxide and propylene oxide.Type: ApplicationFiled: July 1, 2013Publication date: January 16, 2014Applicant: Astellas Deutschland GmbHInventor: Jeffrey Colledge
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Patent number: 8629170Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to, Arenaviridae (Junin, Machupo, Guanarito, Sabia, Lassa, Tacaribe, Pichinde, and LCMV), Filoviridae (Ebola and Marburg viruses), Flaviviridae (yellow fever, Omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).Type: GrantFiled: October 26, 2010Date of Patent: January 14, 2014Assignee: Siga Technologies, Inc.Inventors: Dennis E. Hruby, Tove Bolken, Sean M. Amberg, Dongcheng Dai
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Patent number: 8629285Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.Type: GrantFiled: August 10, 2006Date of Patent: January 14, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Weiwen Ying, Zhenjian Du, Kevin Foley
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Patent number: 8623899Abstract: Inhibitors of HCV replication of formula I including stereochemically isomeric forms, and salts, hydrates, solvates thereof, wherein R and R? have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: GrantFiled: August 6, 2010Date of Patent: January 7, 2014Assignee: Janssen Research & Development IrelandInventors: David McGowan, Samuel Dominique Demin, Stefaan Julien Last, Koen Vandyck, Pierre Jean-Marie Bernard Raboisson
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Patent number: 8623347Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by the Arenavirus family is disclosed.Type: GrantFiled: January 14, 2009Date of Patent: January 7, 2014Assignee: Siga Technologies, Inc.Inventors: Dongcheng Dai, Dennis E. Hruby, Tove C. Bolken, Sean M. Amberg, Travis K. Warren
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Publication number: 20140005194Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to benzimidazole containing compounds and methods for their preparation. These compounds may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with dysregulation of histone deacetylase (HDAC).Type: ApplicationFiled: September 3, 2013Publication date: January 2, 2014Applicant: MEI Pharma, Inc.Inventors: DiZhong CHEN, Hong Yan SONG, Eric T. SUN, Niefang YU, Yong ZOU
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Publication number: 20140004190Abstract: In the present invention there is provided a pharmaceutical composition in a solid dosage form suitable or oral administration, the composition comprising bendamustine or a pharmaceutically acceptable ester, salt or solvate thereof as an active ingredient, and at least one pharmaceutically acceptable excipient, which is a pharmaceutically acceptable saccharide selected from the group consisting of one or more of a monosaccharide, a disaccharide, an oligosaccharide, a cyclic oligosaccharide, a polysaccharide and a saccharide alcohol, wherein the ratio by weight of the active ingredient to the saccharide excipient(s) is in the range of 1:1-5.Type: ApplicationFiled: June 13, 2013Publication date: January 2, 2014Applicant: Astellas Deutschland GmbHInventors: Jeffrey Colledge, Thomas Alfred Profitlich, Ulrich Patzak, Taoufik Ouatas, Margaretha Olthoff
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Publication number: 20140005165Abstract: Disclosed are CCR2 antagonists of Formula (I) or pharmaceutically acceptable thereof, wherein R1, L1 and A are defined herein. Also disclosed are pharmaceutical compositions containing the compounds, methods of treatment using the compounds, and compositions to treat diseases or disorders associated with CCR2 activity.Type: ApplicationFiled: March 14, 2012Publication date: January 2, 2014Inventors: Anilkumar G. Nair, Jose S. Duca, Michael P. Dwyer, Joseph A. Kozlowski, Stuart B. Rosenblum
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Publication number: 20140005221Abstract: The present invention relates to a compound that has URAT1 inhibitory action, and a URAT1 inhibitor, a blood uric acid level-reducing agent and a pharmaceutical composition comprising the compound. More specifically, the present invention relates to a compound represented by Formula (I) below.Type: ApplicationFiled: January 30, 2012Publication date: January 2, 2014Applicant: SATO PHARMACEUTICAL CO., LTD.Inventors: Keita Nagai, Koh Nagasawa, Hirobumi Takahashi, Motoaki Baba, Shinichi Fujioka, Eri Kondoh, Kenichi Tanaka, Yoshiki Itoh
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Patent number: 8618151Abstract: Provided herein are compounds, pharmaceutical compositions, and combination therapies for inhibition of hepatitis C.Type: GrantFiled: December 4, 2012Date of Patent: December 31, 2013Assignee: Presidio Pharmaceuticals, Inc.Inventors: Leping Li, Min Zhong
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Patent number: 8618148Abstract: The present invention relates to a method for the prophylaxis of vascular headaches which do not originate from hypertension, especially migraine, the method comprising administration of telmisartan to a subject in need of such a treatment. The present invention relates also to a method for the prophylaxis of vascular headaches, comprising the co-administration of telmisartan in combination with other drugs suitable for migraine prophylaxis and/or acute treatment of migraine.Type: GrantFiled: June 16, 2006Date of Patent: December 31, 2013Assignee: Boehringer Ingelheim International GmbHInventor: Giora Davidai
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Publication number: 20130345164Abstract: This invention concerns methods of identifying treatments for treating various disorders and related computer products and systems. Also disclosed are methods for treating cellular proliferative disorders and use of compounds identified for such treatment.Type: ApplicationFiled: April 21, 2011Publication date: December 26, 2013Applicant: UNIVERSITY OF MEDICINE AND DENTISTRY OF NEW JERSEYInventors: Alexei Vazquez, Darren Carpizo, Arnold Levine
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Publication number: 20130338205Abstract: The present invention provides pharmaceutical formulations of lyophilized bendamustine suitable for pharmaceutical use. The present invention further provides methods of producing lyophilized bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.Type: ApplicationFiled: August 19, 2013Publication date: December 19, 2013Applicant: Cephalon, Inc.Inventors: Jason Edward Brittain, Joe Craig Franklin
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Patent number: 8609628Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: GrantFiled: January 23, 2012Date of Patent: December 17, 2013Assignee: University of North Carolina at WilmingtonInventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Patent number: 8609707Abstract: Long term storage stable bendamustine-containing compositions are disclosed. The compositions can include bendamustine or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable fluid which can include in some embodiments PEG, PG or mixtures thereof and an antioxidant or chloride ion source. The bendamustine-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 15 months of storage at a temperature of from about 5° C. to about 25° C.Type: GrantFiled: January 28, 2011Date of Patent: December 17, 2013Assignee: Eagle Pharmaceuticals, Inc.Inventors: Nagesh R. Palepu, Philip Christopher Buxton
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Patent number: 8609864Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.Type: GrantFiled: January 7, 2010Date of Patent: December 17, 2013Assignee: Purdue Pharmaceutical Products, L.P.Inventors: Yu Chen, Yi Chen
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Publication number: 20130331362Abstract: An ophthalmic solution is provided. The ophthalmic solution includes an ultraviolet-A absorber and an ultraviolet-B absorber. The ophthalmic solution has a viscosity of between about 1 and 100 cps. The ophthalmic solution can be used to absorb ultraviolet radiation in the eye.Type: ApplicationFiled: June 6, 2012Publication date: December 12, 2013Inventor: Brian J. Smith
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Patent number: 8603520Abstract: An oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a first population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a first rate; a population of a basic substance; and a second population of a pharmaceutical active comprising a pharmaceutical active substance releasable at a second rate. In another embodiment, the oral pharmaceutical composition comprises multiple populations of at least one of beads, pellets, tablets and granules provided in a capsule, the composition comprising: a population of a pharmaceutical active; a population of a basic substance; a population of enteric coated pharmaceutical active; and a population of enteric coated basic substance. The composition can provide multiple site specific delivery of a pharmaceutical active in a rapid, delayed and/or sustained release manner into the plasma.Type: GrantFiled: January 29, 2010Date of Patent: December 10, 2013Assignee: Intellipharmaceutics Corp.Inventors: Isa Odidi, Amina Odidi
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Patent number: 8604217Abstract: A compound, a process for its preparation, a pharmaceutical composition, use of a compound, a method for modulating or regulating serine/threonine and tyrosine kinases and a serine/threonine and tyrosine kinases modulating agent. Novel small-molecule compounds with kinase inhibitory activity, having superior properties as pharmaceutical agents, production method thereof and uses thereof. In particular, new derivatives of tetrahalogenated benzimidazole with serine/threonine and tyrosine kinases inhibitory properties, preferably selected from the group of PIM, HIPK, DYRK, CLK, CDK, FLT, PKG, Haspin, MER, TAO, MNK, TRK kinases which exhibit superior pharmacological actions, and can be useful for the treatment of disease conditions, especially cancers depending on serine/threonine and tyrosine kinases, such as but not limited to leukemias and solid tumors.Type: GrantFiled: December 28, 2011Date of Patent: December 10, 2013Assignee: Selvita S.A.Inventors: Krzysztof Brzózka, Wojciech Czardybon, Aleksandra Sabiniarz, Mariusz Millik, Renata Windak, Adrian Zarebski, Nicolas Beuzen
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Publication number: 20130324496Abstract: Amorphous and crystalline solid forms of the anti-HCV compound (1-{3-[6-(9,9-difluoro-7-{2-[5-(2-methoxycarbonylamino-3-methyl-butyryl)-5-aza-spiro[2.4]hept-6-yl]-3H-imidazol-4-yl}-9H-fluoren-2-yl)-1H-benzoimidazol-2-yl]-2-aza-bicyclo[2.2.1]heptane-2-carbonyl}-2-methyl-propyl)-carbamic acid methyl ester (Compound I) were prepared and characterized in the solid state: Also provided are processes of manufacture and methods of using the amorphous and crystalline forms.Type: ApplicationFiled: March 13, 2013Publication date: December 5, 2013Inventors: Robert William Scott, Fang Wang, Bing Shi, Erik Mogalian
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Publication number: 20130324537Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: ApplicationFiled: November 21, 2012Publication date: December 5, 2013Applicants: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Abbott GmbH & Co. KG, Abbott Laboratories, Andrea Hager-Wernet
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Patent number: 8598078Abstract: Compounds of Formula I wherein the substituents are as defined in Claim 1, and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula I can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: GrantFiled: August 21, 2008Date of Patent: December 3, 2013Assignee: Syngenta Crop Protection, LLCInventors: Olivier Loiseleur, Roger Graham Hall, André Denis Stoller, Gerald Wayne Craig, André Jeanguenat, Andrew Edmunds
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Patent number: 8598181Abstract: Compounds of the present invention and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: July 2, 2010Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Peter D. J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
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Patent number: 8598217Abstract: The invention provides compounds of the formula (I): and salts, tautomers, solvates and N-oxides thereof; wherein Q is CH or N; X is N, N+—O? or CR3; Y is N, N+—O? or CR3a; R1 and R2 are independently selected from hydrogen and various substituents as defined in the claims; or R1 and R2 together with the atoms to which they are attached, link to form an optionally substituted carbocyclic or heterocyclic aromatic or non-aromatic ring of 4 to 7 members; R3 is selected from hydrogen and various substituents; and R3a is selected from hydrogen and various substituents as defined in the claims. Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds. The compounds of formula (I) have activity as inhibitors of CDK kinases and are useful in the treatment of inter alia proliferative diseases such as cancers.Type: GrantFiled: April 30, 2010Date of Patent: December 3, 2013Assignees: Astex Therapeutics Ltd., Novartis AGInventors: Steven Howard, Paul Neil Mortenson, Steven Douglas Hiscock, Alison Jo-Anne Woolford, Andrew James Woodhead, Gianni Chessari, Marc O'Reilly, Miles Stuart Congreve, Claudio Dagostin, Young Shin Cho, Fan Yang, Christine Hiu-Tung Chen, Christopher Thomas Brain, Bharat Lagu, Yaping Wang, Sunkyu Kim, John Giraldes, Michael Joseph Luzzio, Lawrence Blas Perez
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Patent number: 8598168Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: April 5, 2007Date of Patent: December 3, 2013Assignee: MethylGene Inc.Inventors: Oscar Moradei, Isabelle Paquin, Sylvie Frechette, Tammy Mallais, Simon Roy, Roger Machaalani, Arkadii Vaisburg, Jeffrey M Besterman, Pierre Tessier, David Smil, Silvana Leit, Robert Déziel
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Publication number: 20130317027Abstract: The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and other complications associated with these diseases and disorders.Type: ApplicationFiled: December 7, 2012Publication date: November 28, 2013Applicant: Myrexis, Inc.Inventors: J. Adam Willardsen, Jeffrey W. Lockman, Brett R. Murphy, Weston R. Judd, In Chul Kim, Se-Ho Kim, Daniel Feodore Zigar, Kraig M. Yager, Tracey C. Fleischer, Ryan T. Terry-Lorenzo, J. Jay Boniface, Daniel P. Parker, Ian A. McAlexander, Matthew Gregory Bursavich, David M. Dastrup, Christophe Hoarau, David A. Gerrish, Paul R. Sebahar, Dange Vijay Kumar
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Publication number: 20130317047Abstract: The present invention relates to use of an inhibitor of the renin-anglotensin system (RAS) or a pharmaceutically acceptable derivative thereof, such as ramipril or ramiprilat, in the prevention of stroke, diabetes and/or congestive heart failure (CHF).Type: ApplicationFiled: November 9, 2012Publication date: November 28, 2013Applicant: Aventis Pharma Deutschland GmbHInventor: Aventis Pharma Deutschland GmbH
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Publication number: 20130317025Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: ApplicationFiled: June 17, 2013Publication date: November 28, 2013Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
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Publication number: 20130309196Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: March 14, 2013Publication date: November 21, 2013Inventors: John O. Link, Jeromy J. Cottell, Teresa Alejandra Trejo Martin
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Publication number: 20130310427Abstract: Antiviral compounds may be used to inhibit or reduce the activity of Hepatitis C virus (HCV), particularly HCV's NS5A protein. In these contexts, inhibition and reduction of activity of the NS5A protein refers to a lower level of the measured activity relative to a control experiment in which the cells or the subjects are not treated with the test compound. The inhibition or reduction in the measured activity is at least a 10% reduction or inhibition. The compounds and their isomeric forms and pharmaceutically acceptable salts thereof are useful in treating and preventing HCV infection alone or when used in combination with other compounds targeting viral or cellular elements or functions involved in the HCV lifecycle.Type: ApplicationFiled: June 9, 2011Publication date: November 21, 2013Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20130309307Abstract: The present invention relates to a bilayer pharmaceutical tablet comprising a first layer formulated for immediate release of the angiotensin II receptor antagonist telmisartan from a dissolving tablet matrix which contains telmisartan in substantially amorphous form, and a second layer formulated for immediate release of a diuretic like hydrochlorothiazide from a fast disintegrating tablet matrix. A method of producing the bilayer tablet is also disclosed.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: BOEHRINGER INGELHEIM PHARMA GMBH & CO. KGInventors: Thomas FRIEDL, Gottfried SCHEPKY
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Patent number: 8586616Abstract: The present invention is directed to novel benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the androgen receptor.Type: GrantFiled: December 16, 2010Date of Patent: November 19, 2013Assignee: Janssen Pharmaceutica, NVInventors: Raymond Ng, Zhihua Sui, Jihua Guan, James C. Lanter, Vernon C. Alford, Jr.
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Publication number: 20130303535Abstract: The invention provides a compound for the treatment or prophylaxis of pathology involving SNS, specifically diseases such as neuropathic pain, nociceptive pain, dysuria, multiple sclerosis and the like.Type: ApplicationFiled: May 15, 2013Publication date: November 14, 2013Inventors: Katsunori TSUBOI, Yusuke YAMAI, Hitoshi WATANABE, Hironori KINOSHITA
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Publication number: 20130303580Abstract: Oil-in-water fungicidal formulations are prepared having pigment dispersed therein, the pigment being stable within the oil-in-water emulsion as a result of the addition of suitable silicone surfactants and suitable emulsifiers. The formulations can be prepared either as a 2-pack formulation or as a single formulation. In the case of the single formulation polyethylene glycol is also added. In either case, the formulations show a synergistic effect through the addition of the pigment, the resulting formulations having an increased efficacy. Further, the formulations show a synergistic effect when mixed with conventional chemical fungicides, both being added in reduced amounts compared to recommended rates.Type: ApplicationFiled: March 15, 2013Publication date: November 14, 2013Inventor: Suncor Energy Inc.
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Publication number: 20130303567Abstract: Compounds and pharmaceutical compositions are provided that inhibit the activity of poly ADP-ribose synthetase (PARP). Such compounds are useful in the treatment of various diseases, conditions and injuries such as stroke, myocardial infarction, ischemia-perfusion injury in various organs, traumatic brain injury, atherosclerosis, inflammatory diseases and cancer.Type: ApplicationFiled: July 14, 2013Publication date: November 14, 2013Inventors: Bijoy Panicker, Dong Sung Lim, David E. Smith
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Publication number: 20130303512Abstract: This disclosure is directed, in part, to a method of determining whether a subject having cancer is at risk for developing metastasis of the cancer. In one embodiment, the method comprises (a) obtaining a biological sample from the subject having cancer; (b) determining CCR5 expression level and/or expression level of at least one of CCR5 ligands in the biological sample; and (c) if the expression level of CCR5 and/or of at least one of CCR5 ligands determined in step (b) is increased compared to CCR5 expression level and/or expression level of at least one of CCR5 ligands in a control sample, then the subject is identified as likely at risk for developing metastasis of the cancer.Type: ApplicationFiled: May 14, 2013Publication date: November 14, 2013Inventor: Richard G. PESTELL
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Publication number: 20130296377Abstract: The present invention provides a compound of formula I: 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: March 14, 2013Publication date: November 7, 2013Inventors: Christopher Michael ADAMS, Charles BABU, Michael Paul CAPPARELLI, Jian DING, Takeru EHARA, Keith JENDZA, Nan JI, Rajeshri Ganesh KARKI, Toshio KAWANAMI, Xue LIANG, Nello MAINOLFI, James J. POWERS, Michael H. SERRANO-WU, Chun ZHANG
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Publication number: 20130296391Abstract: The present invention provides a composition having an excellent controlling activity on a plant disease. The composition comprising a compound represented by Formula (1) and one or more fungicidal compound(s) selected from Group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: October 5, 2011Publication date: November 7, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka