Oxadiazoles (including Hydrogenated) Patents (Class 514/364)
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Publication number: 20150011594Abstract: Provided are methods for screening a subject for cancer. The methods involve obtaining a blood sample from the subject and determining a level of Bridging Integrator 1 (BIND isoforms comprising exon 12a in the sample. Optionally, the method involves determining a level of 12a+/13? BIN isoform (comprising exon 12a but lacking exon 13) in the sample. An elevated level of 12a+ (e.g., 12a+/13?) BIN1 isoforms in the blood sample indicates the subject has cancer. Also provided are methods for determining efficacy of a cancer therapy in a subject and methods of treating cancer. Isolated antibodies that selectively bind human 12a+ BIN1 are also provided as well as kits for determining 12a+/13? BIN1 isoforms.Type: ApplicationFiled: September 28, 2012Publication date: January 8, 2015Inventors: Darryl Steven Shaw, Neil Gavin Shaw
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Publication number: 20150005232Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, and R6 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 obesity and related diseases, disorders, and conditions associated with MetAP2.Type: ApplicationFiled: February 28, 2013Publication date: January 1, 2015Applicant: Takeda Pharmaceutical Company LimitedInventors: Zacharia Cheruvallath, Philip Erickson, Jun Feng, Mallareddy Komandla, John David Lawson, Christopher McBride, Joanne Miura, Sean Murphy, Mingnam Tang, Huong-Thu Ton-Nu
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Patent number: 8921359Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.Type: GrantFiled: April 22, 2013Date of Patent: December 30, 2014Assignee: Vitae Pharmaceuticals, Inc.Inventors: Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
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Publication number: 20140377292Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: ApplicationFiled: September 5, 2014Publication date: December 25, 2014Applicant: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20140378445Abstract: Disclosed are methods for treating Vascular Leak Syndrome. Further disclosed are methods for treating vascular leakage due to inflammatory diseases, inter alia, sepsis, lupus, inflammatory bowel disease. Yet further disclosed are methods for treating renal cell carcinoma and melanoma. Still further disclosed are methods for reducing metastasis of malignant cells and/or preventing the proliferation of carcinoma cells via spreading due to vascular leakage.Type: ApplicationFiled: December 21, 2012Publication date: December 25, 2014Inventors: Robert Shalwitz, Kevin G. Peters
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Publication number: 20140378493Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: ApplicationFiled: September 8, 2014Publication date: December 25, 2014Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Publication number: 20140378459Abstract: [Problem] Provided is a compound which is useful as an agent for preventing and/or treating renal diseases. [Means for Solution] The present inventors have conducted extensive studies on compounds having a trypsin inhibitory action, and as a result, they have found that a guanidinobenzoic acid compound has a trypsin inhibitory action, thereby completing the present invention. The guanidinobenzoic acid compound of the present invention can be used as an agent for preventing and/or treating renal disease as an agent which will substitute low-protein diet therapy, and an agent for preventing and/or treating trypsin-related diseases, for example, pancreatitis, gastroesophageal reflux disease, hepatic encephalopathy, influenza, and the like.Type: ApplicationFiled: September 14, 2012Publication date: December 25, 2014Applicant: ASTELLAS PHARMA INC.Inventors: Jiro Fujiyasu, Kazuhiko Ohne, Susumu Yamaki, Tomoyoshi Imaizumi, Takeshi Hondo, Keisuke Matsuura, Tomohki Satou, Satoshi Sasamura
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Patent number: 8916594Abstract: This invention provides new compounds having NPY Y5 antagonistic activity. The present inventors found that a compound of the formula (I): wherein R1 is substituted or unsubstituted alkyl or the like; p, q and r are each independently 0 or 1; ring A is oxadiazole; and R2 is substituted or unsubstituted alkyl or the like, has NPY Y5 antagonistic activity.Type: GrantFiled: April 25, 2012Date of Patent: December 23, 2014Assignee: Shionogi & Co., Ltd.Inventors: Kyohei Hayashi, Yuusuke Tamura, Naoki Omori
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Patent number: 8916592Abstract: Compounds of formula I wherein X is O or S(?O)n; n is 0, 1 or 2; R1 is optionally substituted alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, cycloalkyl, halocycloalkyl, cycloalkenyl, halocycloalkenyl, phenyl, hetaryl, phenylalkyl, hetaryl alkyl, optionally fused to phenyl, hetaryl or heterocyclyl; A is —NRb2, —C(=G)GRb, —C(=G)NRb2, —C(?NORb)Rb, C(=G)[N?SRb2], —C(=G)NRb—NRb2, C2-C6-alkandiyl, C2-C6-alkenediyl, C1-C3-alkyl-G-C1-C3-alkyl, wherein Rb is as defined in the description, or optionally substituted phenyl, hetaryl, heterocyclyl, optionally fused to phenyl or heterocyclyl; B is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 3 carbon chain atoms; D is an optionally substituted saturated or partially unsaturated hydrocarbon chain with 1 to 5 carbon chain atoms or C3-C6-cycloalkyl; G is oxygen or sulfur; or the enantiomers or diastereomers or salts or N-oxides thereof, processes for preparing the compounds I, pesticidal compositions and synergistic mType: GrantFiled: December 13, 2006Date of Patent: December 23, 2014Assignee: Merial LimitedInventors: Matthias Pohlman, Michael Hofmann, Henricus Maria Martinus Bastiaans, Michael Rack, Deborah L. Culbertson, Hassan Oloumi-Sadeghi, Takeo Hokama, Christopher Palmer, Jürgen Langewald
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Publication number: 20140371231Abstract: The present disclosure describes compounds and pharmaceutically acceptable salts thereof and compositions and formulations comprising the same that are useful in methods of treating dyskinesia or related disorders, and methods for treating dyskinesia or related disorders.Type: ApplicationFiled: August 29, 2014Publication date: December 18, 2014Inventors: John Ciallella, John Gruner, Andrew G. Reaume, Michael S. Saporito
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Publication number: 20140371276Abstract: The invention relates to compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (TRPM8), and having formula (I). Said compounds are useful in the treatment of diseases associated with activity of TRPM8 such as pain, inflammation, ischaemia, neurodegeneration, stroke, psychiatric disorders, itch, irritable bowel diseases, cold induced and/or exhacerbated respiratory disorders and urological disorders.Type: ApplicationFiled: December 19, 2012Publication date: December 18, 2014Inventors: Alessio Moriconi, Gianluca Bianchini, Sandro Colagioia, Laura Brandolini, Andrea Aramini, Chiara Liberati, Silvia Bovolenta
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Publication number: 20140371279Abstract: The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J or form K. The substantially pure crystalline forms of azilsartan of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof.Type: ApplicationFiled: September 27, 2012Publication date: December 18, 2014Applicants: SUNSHINE LAKE PHARMA CO., LTD., RUYUAN PHARM CO., LTD.Inventors: Xin Lei, Jinan Peng, Tianming Wang, Zhiqing Lv, Wan Li
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Publication number: 20140364464Abstract: The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan medoxomil potassium, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L. The substantially pure crystalline forms of azilsartan medoxomil potassium of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan medoxomil potassium generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan medoxomil potassium, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof.Type: ApplicationFiled: January 14, 2013Publication date: December 11, 2014Applicants: SUNSHINE LAKE PHARMA CO., LTD., RUYUAN HEC PHARM CO., LTD.Inventors: Xin Lei, Zhiqing Lv, Tianming Wang
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Patent number: 8906899Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: June 28, 2013Date of Patent: December 9, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang
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Patent number: 8906945Abstract: Organic compounds showing the ability to inhibit effector toxin secretion or translocation mediated by bacterial type III secretion systems are disclosed. The disclosed type III secretion system inhibitor compounds are useful for combating infections by Gram-negative bacteria such as Salmonella spp., Shigella flexneri, Pseudomonas spp., Yersinia spp., enteropathogenic and enteroinvasive Escherichia coli, and Chlamydia spp. having such type III secretion systems.Type: GrantFiled: April 6, 2010Date of Patent: December 9, 2014Assignee: Microbiotix, Inc.Inventors: Donald T. Moir, Daniel Aiello, Norton P. Peet, John D. Williams
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Publication number: 20140357675Abstract: Compounds are provided having an excellent hypoglycemic effect and ? cell- or pancreas-protecting effects, or pharmaceutically acceptable salts thereof, and a pharmaceutical composition having an excellent therapeutic effect and/or prophylactic effect on type 1 diabetes, type 2 diabetes, and the like, which cause hyperglycemia due to abnormal glucose metabolism. A compound represented by general formula (I), or a pharmaceutically acceptable salt thereof, is disclosed.Type: ApplicationFiled: January 17, 2013Publication date: December 4, 2014Applicant: DAIICHI SANKYO COMPANY, LIMITEDInventors: Shigeo Yamanoi, Hidenori Namiki, Yuichi Ochiai, Madoka Hoshino, Koji Matsumoto
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Patent number: 8901119Abstract: The present invention relates to a compound of Formula (I): or a pharmaceutically acceptable salt thereof, corresponding pharmaceutical compositions, compound preparation and treatment methods directed to bacterial infections and inhibition of bacterial peptide deformylase (PDF) activity.Type: GrantFiled: March 9, 2012Date of Patent: December 2, 2014Assignee: GlaxoSmithKline Intellectual Property (No. 2) LimitedInventors: Kelly M. Aubart, Andrew B. Benowitz, Yuhong Fang, James Hoffman, Joseph M. Karpinski, Andrew Nicholson Knox, Xiangmin Liao, Donghui Qin, Dongchuan Shi, Jared T. Spletstoser
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Patent number: 8901156Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, Z, L and n are as defined herein, and methods of making and using the same.Type: GrantFiled: January 13, 2011Date of Patent: December 2, 2014Assignee: Tempero Pharmaceuticals, Inc.Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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Publication number: 20140349987Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides pyrrolo carboxamide compounds of Formula (1) and the enantiomers, diastereomers, N-oxides, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: December 3, 2012Publication date: November 27, 2014Inventors: Christoph Steeneck, Olaf Kinzel, Christian Gege, Gerald Kleymann, Thomas Hoffmann
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Publication number: 20140349848Abstract: The present invention provides fungicidal 4-substituted-3-{phenyl[(heterocyclylmethoxy)imino]methyl}-1,2,4-oxadiazol-5(4H)-one derivatives of formula (I) wherein A represents a pyridyl or thiazole group and X1, Y1 to Y5 represent independently different substituents.Type: ApplicationFiled: September 10, 2012Publication date: November 27, 2014Inventors: Christoph Braun, Haruko Sawada, Helene Lachaise, Stephane Brunet, Philippe Rinolfi, Christophe Dubost, Pierre-Yves Coqueron, Simon Maechling, Anne-Sophie Rebstock, Ulrike Wachendorff-Neumann
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Publication number: 20140350026Abstract: The present invention provides an anti-Coxsackie virus oxadiazole compound as represented by formula (I), or the pharmaceutically acceptable salt thereof, a preparation method, a pharmaceutical composition, and use thereof, wherein R is CH3 or CF3; R? and R? are respectively H, alkyl or halogen; A is O or S; n is a number from 1 to 6; X is O, S or NH; Y is alkyl, unsubstituted cycloalkyl, mono-substituted cycloalkyl, disubstituted cycloalkyl, poly-substituted cycloalkyl, unsubstituted aryl, mono-substituted aryl, disubstituted aryl, poly-substituted aryl, unsubstituted 5-6 membered heterocyclyl, mono-substituted 5-6 membered heterocyclyl, disubstituted 5-6 membered heterocyclyl, or poly-substituted 5-6 membered heterocyclyl. Compared to prior art, the oxadiazole compound of the present invention has excellent anti-Coxsackie virus activity, lower toxicity and high safety.Type: ApplicationFiled: November 9, 2012Publication date: November 27, 2014Inventors: Xianjin Luo, Weidong Ye
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Patent number: 8895306Abstract: The present invention relates to methods to use non-steroidal ligands in nuclear receptor-based inducible gene expression system to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: GrantFiled: November 5, 2007Date of Patent: November 25, 2014Assignee: Intrexon CorporationInventors: Robert Eugene Hormann, Orestes Chortyk, Dat Phat Le
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Patent number: 8895535Abstract: Compounds of the formula I in which R1, R2, R3 and R4 have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumors.Type: GrantFiled: September 14, 2011Date of Patent: November 25, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Frank Zenke, Michel Calderini, Djordje Musil
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Publication number: 20140341850Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Applicant: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Publication number: 20140343066Abstract: The present invention relates to compounds of formula (I) or pharmaceutical acceptable salts, wherein A, R1, R2, R3 and m, are defined in the description. The present invention relates also to methods of making said compounds, and compositions containing said compounds which are useful for inhibiting kinases such as Glycogen Synthase kinase 3 (GSK-3), Rho kinase (ROCK), Janus Kinases (JAK), Cdc7, AKT, PAK4, PLK, CK2, KDR, MK2, JNK1, aurora, pim 1 and nek 2.Type: ApplicationFiled: December 20, 2013Publication date: November 20, 2014Inventors: Irini Akritopoulou-Zanze, Brian D. Wakefield, Helmut Mack, Sean C. Turner, Alan F. Gasiecki, Vijaya J. Gracias, Kathy A. Sarris, Douglas M. Kalvin, Melissa J. Michmerhuizen, Qi Shuai, Jyoti R. Patel, Margaretha H.M. Bakker, Nicole Teusch, Eric F. Johnson, Peter J. Kovar, Stevan W. Djuric, Andrew J. Long, Anil Vasudevan, Dawn M. George, Lu Wang, Biqin Li, Nigel S. Moore, Adrian D. Hobson, Keith W. Woods, Julie M. Miyashiro, Steven L. Swann, Jr., Thomas D. Penning
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Publication number: 20140343017Abstract: Provided is a highly safe and effective compound represented by the following general formula (1) or a salt thereof which acts on tubulin and has an anticancer effect, wherein Ar represents an aryl group or a heteroaryl group; Z1, Z2, Z3, and Z4 each independently represent CH, a nitrogen atom, an oxygen atom, or a sulfur atom; R1 represents a hydrogen atom, a halogen atom, an alkyl group, or the like; R2 and R3 are the same or different and each represent a hydrogen atom, a halogen atom, a carboxyl group, or the like; n units of R4 are the same or different and each represent a hydrogen atom, an alkyl group, or the like; and n represents a number of 0 to 4.Type: ApplicationFiled: January 24, 2013Publication date: November 20, 2014Applicant: Kabushiki Kaisha Yakult HonshaInventors: Takashi Ikeda, Masahiro Ono, Satoshi Ueno, Ryuta Yamazaki, Takashi Yaegashi, Takeshi Matsuzaki
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Publication number: 20140343009Abstract: Methods for treating methylmalonic acidemia in which at least one allele of a gene associated with MMA (e.g., the MUT, MMAA, or MMAB gene) contains a mutation (e.g., nonsense mutation) that results in a premature stop codon in RNA encoded by an allele of the gene associated with MMA involving the administration of a compound that promotes readthrough of RNA (e.g., messenger RNA) containing a premature stop codon encoded by an allele of the gene associated with MMA are described. The compound can be administered as a single-agent therapy or in combination with one or more additional therapies to a human in need of such treatment.Type: ApplicationFiled: July 31, 2014Publication date: November 20, 2014Applicant: PTC Therapeutics Inc.Inventor: Jay Allan Barth
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Patent number: 8889668Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, have the meanings given in claim 1. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: GrantFiled: December 12, 2012Date of Patent: November 18, 2014Assignee: Merck Serono SAInventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
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Publication number: 20140336224Abstract: Compounds of the Formula (I) as well as pharmaceutically acceptable salts thereof, that may be useful for treating aldosterone-mediated diseases are disclosed. Processes for preparing compounds of the Formula (I), use of the compounds for the therapy and prophylaxis of the abovementioned diseases and for preparing pharmaceuticals for this purpose, and pharmaceutical compositions which comprise compounds of the Formula (I) are disclosed.Type: ApplicationFiled: October 18, 2012Publication date: November 13, 2014Inventors: Ping Lan, Kun Liu, Anthony Ogawa, Hong Shen, Christine Yang, Yuguang Wang, Richard Beresis, Changhe Qi
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Publication number: 20140336194Abstract: The present invention provides the use of a neutral endopeptidase inhibitor, in the manufacture of a medicament for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The invention also relates to the use of a compound of Formula I: wherein R1, R2, R3, R5, X, A3, B1, s and n are defined herein, for the treatment, amelioration and/or prevention of contrast-induced nephropathy. The present invention further provides a combination of pharmacologically active agents for use in the treatment, amelioration and/or prevention of contrast-induced nephropathy.Type: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Applicant: NOVARTIS AGInventor: Shi Yin FOO
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Patent number: 8883827Abstract: The present invention relates to new compounds of formula I, to processes for their preparation, to pharmaceutical formulations containing such compounds and to their use in therapy. Such compounds find particular use in the treatment and/or prevention of conditions or diseases which are affected by over-activation of signaling in the Wnt pathway. For example, these may be used in preventing and/or retarding proliferation of tumor cells, for example carcinomas such as colon carcinomas.Type: GrantFiled: June 7, 2010Date of Patent: November 11, 2014Assignee: Oslo University Hospital HFInventors: Daniel Holsworth, Jo Waaler, Ondrej Machon, Stefan Krauss
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Publication number: 20140329796Abstract: The present invention aims to provide a novel compound having a TRPA1 antagonist activity, and a medicament containing the compound. Moreover, the present invention aims to provide a TRPA1 antagonist and a medicament useful for the prophylaxis or treatment of diseases involving TRPA1. A medicament containing a compound represented by the formula (I): wherein each symbol is as defined in the DESCRIPTION, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: July 16, 2014Publication date: November 6, 2014Applicant: Ajinomoto Co., Inc.Inventors: Tamotsu SUZUKI, Kaori Kobayashi, Sayaka Asari, Seiji Shiraishi, Tatsuya Okuzumi
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Patent number: 8877751Abstract: Compounds of the formula I, in which R1, R2, R3, R3?, R4, R4?, E, E?, E? and E?? have the meanings indicated in Claim 1, are inhibitors of tyrosine kinases, in particular Met kinase, and can be employed, inter alia, for the treatment of tumors.Type: GrantFiled: December 8, 2009Date of Patent: November 4, 2014Assignee: Merck Patent GmbHInventors: Frank Stieber, Oliver Schadt, Dieter Dorsch, Andree Blaukat
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Publication number: 20140322136Abstract: The present invention provides methods to reduce or inhibit weight gain by administering inhibitors of the SirT1 protein to a subject. Methods to identify such inhibitors are also disclosed.Type: ApplicationFiled: May 6, 2014Publication date: October 30, 2014Inventors: Yansong GU, Hongzhe LI
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Patent number: 8871738Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.Type: GrantFiled: October 25, 2012Date of Patent: October 28, 2014Assignee: Merck Sharp & Dohme Corp.Inventors: Pengcheng Patrick Shao, Wanying Sun, Revathi Reddy Katipally, Petr Vachal, Feng Ye, Jian Liu, Deyou Sha
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Publication number: 20140315962Abstract: The present invention is directed to 1,2,5-oxadiazole derivatives, and compositions of the same, which are inhibitors of indoleamine 2,3-dioxygenase and are useful in the treatment of cancer and other disorders, and to the processes and intermediates for making such 1,2,5-oxadiazole derivatives.Type: ApplicationFiled: July 2, 2014Publication date: October 23, 2014Applicant: INCYTE CORPORATIONInventors: Andrew P. Combs, Eddy W. Yue, Richard B. Sparks, Wenyu Zhu, Jiacheng Zhou, Qiyan Lin, Lingkai Weng, Tai-Yuen Yue, Pingli Liu
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Publication number: 20140309238Abstract: The present invention relates to compounds of Formula (I), wherein R1 is chosen among the following radicals: (II); (III); (IV), (V), (VI) (VII) and n=1 or 2 and m=1 or 2 with the proviso that m=2 when R1 is (VIII). The present invention also relates to the use thereof as drugs, more particularly in the treatment of mycobacterial infections and more particularly in the treatment of tuberculosis.Type: ApplicationFiled: October 24, 2012Publication date: October 16, 2014Applicants: Universite de Droit et de la Sante de Lille 2, INSERM (Institut National de la Sante et de la Recherche Medicale), Institut Pasteur de LilleInventors: Benoit Deprez, Nicolas Willand, Marion Flipo, Matthieu Desroses, Alain Baulard, Florence Leroux
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Publication number: 20140309265Abstract: The invention relates generally to macrocyclic compounds and their therapeutic use. More particularly, the invention relates to macrocyclic compounds that modulate the activity of inhibitors of apoptosis (IAPs) and/or are useful in the treatment of medical conditions, such as cancer.Type: ApplicationFiled: November 9, 2012Publication date: October 16, 2014Inventors: Benjamin Adam Seigal, Nicholas Terrett, Percy H. Carter, Robert M. Borzilleri, Yong Zhang, Michael M. Miller
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Publication number: 20140308243Abstract: The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, esters, or prodrugs thereof: Q-G-A-L-B—Z—W??(I), which inhibit RNA-containing virus, particularly the hepatitis C virus (HCV). Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: April 16, 2014Publication date: October 16, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yao-Ling Qiu, Hui Cao, Xiaowen Peng, Zhigang Chen, Yat Sun Or
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Patent number: 8859598Abstract: The present invention relates to 1,2,4-oxadiazoles azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: September 30, 2013Date of Patent: October 14, 2014Assignee: Allergan, Inc.Inventors: Janet A. Takeuchi, Ling Li, Wha-Bin Im, Ken Chow
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Patent number: 8859597Abstract: This invention generally provides compounds, pharmaceutical compositions, and methods for their use, which include methods that result in increased expression in an Atoh1 gene (e.g., Hath1) in a biological cell. More specifically, the invention relates to the treatment of diseases and/or disorders that would benefit from increased Atoh1 expression, e.g., a hearing impairment or imbalance disorder associated with a loss of auditory hair cells, or a disorder associated with abnormal cellular proliferation.Type: GrantFiled: April 24, 2012Date of Patent: October 14, 2014Assignees: Massachusetts Eye & Ear Infirmary, Brigham & Women's Hospital, Inc.Inventors: Albert Edge, Sang-Jun Jeon, Kathleen Seyb, Marcie Glicksman, Lixin Qiao, Gregory D. Cuny
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Publication number: 20140301978Abstract: Novel 1,2,4-oxadiazole benzoic acid compounds, methods of using and pharmaceutical compositions comprising an 1,2,4-oxadiazole benzoic acid derivative are disclosed. The methods include methods of treating or preventing a disease ameliorated by modulation of premature translation termination or nonsense-mediated mRNA decay, or ameliorating one or more symptoms associated therewith.Type: ApplicationFiled: June 18, 2014Publication date: October 9, 2014Applicant: PTC Therapeutics Inc.Inventors: Gary Mitchell Karp, Seongwoo Hwang, Guangming Chen, Neil Gregory Almstead, Young-Choon Moon
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Publication number: 20140303171Abstract: Compounds of Formula I are disclosed: wherein A, R1, R2, R3, R4A, R4B, R5, R6 and R7 are defined herein. The compounds encompassed by Formula I include compounds which are HIV protease inhibitors. The compounds and their pharmaceutically acceptable salts are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: October 26, 2012Publication date: October 9, 2014Inventors: Michael John Boyd, Jean-Francois Chiasson, Sheldon Crane, André Giroux
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Patent number: 8853219Abstract: Disclosed are muscarinic agonist compounds including oxadiazole derivatives, compositions and preparations thereof. Also disclosed are methods of synthesizing such oxadiazole compounds. Further disclosed are methods for treating a subject with said muscarinic agonists or a pharmaceutically suitable form thereof to enhance cognitive function.Type: GrantFiled: January 11, 2011Date of Patent: October 7, 2014Assignee: NeuroSolis, Inc.Inventors: Michael L. Hendrickson, Jeffrey C. Ockuly, Trevor M. Twose, Melinda L. Verdone, Brent D. Abraham, Richard R. Copp, James G. Farnham, Seth A. Hanson
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Publication number: 20140296308Abstract: The present invention relates to compounds with a benzoxadiazolyl amine structure which are capable of inhibiting the activation or the biological activity of p38 mitogen-activated protein kinase (MAPK) and the use thereof in the treatment of a disease that can be alleviated by means of inhibiting the activation or the biological activity of said p38 MAPK, for example, an inflammatory disease or a disease presenting with pain.Type: ApplicationFiled: October 31, 2012Publication date: October 2, 2014Inventors: Federico Mayor Ménendez, Cristina Murga Montesinos, Pedro Manuel Campos Muelas, Jacoba Johana Heijnen, Anna Maria Agnes Antonius Kavelaars, Antonio Morreale de León, Rubén Gil Redondo
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Publication number: 20140296177Abstract: A new class of biotin protein ligase (BPL) inhibitors that have antibacterial activity against multiple Staphylococcus aureus isolates, including clinically important methicillin-resistant S. aureus (MRSA) are disclosed that are non-toxic.Type: ApplicationFiled: September 21, 2012Publication date: October 2, 2014Inventors: Andrew Abel, Steven Polyak, Grant Booker, John Wallace, Tatiana Soares Da Costa, Angie Jarrad, William Tieu, Kelly Lee Keeling, Daniel Sejer Pederson, Nicole Pendini, Matthew Wilce, Min Yin Yap
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Publication number: 20140296239Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicant: SANOFIInventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
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Publication number: 20140296307Abstract: The present invention relates compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell. The compounds exhibit increased inhibitory activity against c-Myc relative to the known c-Myc inhibitor small-molecule benzofurazan N-([1,1?-biphenyl]-2-yl)-7-nitrobenzo[c][1,2,5]oxadiazol-4-amine (10074-G5).Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Applicant: University of Maryland, BaltimoreInventor: STEVEN FLETCHER
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Publication number: 20140296296Abstract: The present invention relates to compounds of the formula I, wherein X, R, R1, R2, D, E1, E2, E3, E4, G1, G2, G3 and G4 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: March 27, 2014Publication date: October 2, 2014Inventors: Sven Ruf, Thorsten Sadowski, Klaus Wirth, Herman Schreuder, Christian Buning, Christopher Kallus, Hartmut Strobel, Hermut Wehlan
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Patent number: 8846728Abstract: The present invention relates to novel oxadiazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.Type: GrantFiled: June 26, 2013Date of Patent: September 30, 2014Assignee: Allergan, Inc.Inventors: Wenkui K. Fang, Evelyn G. Corpuz, Wha-Bin Im, Ken Chow, Liming Wang