Benzo Fused At 4,5-positions Of The Diazole Ring Patents (Class 514/394)
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Publication number: 20150094304Abstract: 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: ApplicationFiled: December 11, 2014Publication date: April 2, 2015Inventors: SARA SABINA HADIDA RUAH, PETER DIEDERIK JAN GROOTENHUIS, FREDRICK F. VAN GOOR, JINGLAN ZHOU, BRIAN RICHARD BEAR, MARK THOMAS MILLER, JASON MC CARTNEY, MEHDI MICHEL DJAMEL NUMA
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Publication number: 20150093391Abstract: A method of treating cancer or metastasis is provided involving administering at least one oncostatin M (OSM) antagonist to a subject, wherein the subject has been diagnosed with cancer. Administration of an OSM antagonist such as a small molecule pharmaceutical is provided as well as an anti-OSM antibody, an anti-OSM aptamer, and an OSM mRNA antagonist. The OSM antagonists were found to inhibit or prevent tumor cell detachment, proliferation and metastasis in several cancer types.Type: ApplicationFiled: September 5, 2014Publication date: April 2, 2015Applicant: BOISE STATE UNIVERSITYInventors: Cheryl Jorcyk, Dong Xu
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Patent number: 8993612Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: GrantFiled: October 6, 2010Date of Patent: March 31, 2015Assignee: Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Kanthikiran V S Varanasi, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
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Publication number: 20150087617Abstract: The invention provides indole and indoline derivatives and slats thereof, compositions comprising them and uses thereof for the treatment of diseases and disorders.Type: ApplicationFiled: April 2, 2013Publication date: March 26, 2015Inventors: Abraham Nudelman, Marta Weinstock-Rosin
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Publication number: 20150086551Abstract: The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.Type: ApplicationFiled: January 31, 2013Publication date: March 26, 2015Inventors: Yu Chen, Yi Chen
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Publication number: 20150087681Abstract: The present invention provides a lyophilized bendamustine hydrochloride (HCL) pharmaceutical composition. The present invention further provides methods of producing the lyophilized bendamustine HCL composition from a composition including bendamustine HCL, mannitol, formic acid, and water. The pharmaceutical formulation can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.Type: ApplicationFiled: September 25, 2014Publication date: March 26, 2015Inventors: Pranav Patel, Mahendra R. Patel
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Publication number: 20150087618Abstract: Compounds effective in inhibiting replication of Hepatitis C virus (“HCV”) are described. This invention also relates to processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.Type: ApplicationFiled: December 2, 2014Publication date: March 26, 2015Applicant: AbbVie Inc.Inventors: Mary E. Bellizzi, David A. Betebenner, Jean C. Califano, William A. Carroll, Daniel D. Caspi, David A. DeGoey, Pamela L. Donner, Charles A. Flentge, Yi Gao, Charles W. Hutchins, Douglas K. Hutchinson, Tammie K. Jinkerson, Warren M. Kati, Ryan G. Keddy, Allan C. Krueger, Wenke Li, Dachun Liu, Clarence J. Maring, Mark A. Matulenko, Christopher E. Motter, Lissa T. Nelson, Sachin V. Patel, John K. Pratt, John T. Randolph, Todd W. Rockway, Kathy Sarris, Michael D. Tufano, Seble H. Wagaw, Rolf Wagner, Kevin R. Woller
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Patent number: 8987214Abstract: The present invention features solid compositions comprising a selected HCV inhibitor in an amorphous form. In one embodiment, the selected HCV inhibitor is formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.Type: GrantFiled: October 6, 2014Date of Patent: March 24, 2015Assignee: AbbVie Inc.Inventors: Yi Gao, Geoff Zhang
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Publication number: 20150079170Abstract: The present invention relates to novel tablet dosage forms and methods of preparing these forms, which can be used for different classes of pharmaceutical active ingredients posing stability issues in a single unit system. The dosage form includes a first layer, which includes a tablet of one or more active pharmaceutical ingredients, which is inlayed in the first layer along with other pharmaceutically acceptable excipients, and a second layer that includes one or more active pharmaceutical ingredients optionally with other pharmaceutically acceptable excipients.Type: ApplicationFiled: September 13, 2013Publication date: March 19, 2015Inventors: Girish Kumar JAIN, Ramakant GUNDU, Rahul DABRE
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Bridged Ring compounds As Hepatitis C Virus (HCV) Inhibitors And Pharmaceutical Applications Thereof
Publication number: 20150079028Abstract: Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.Type: ApplicationFiled: August 5, 2013Publication date: March 19, 2015Applicant: SUNSHINE LAKE PHARMA CO., LTDInventors: Yingjun Zhang, Jaincun Zhang, Hongming Xie, Qingyun Ren, Yumei Tan, Huichao Luo -
Publication number: 20150080444Abstract: Methods of treating bendamustine responsive conditions in patients having fluid and/or sodium intake restrictions are disclosed. The methods include identifying patients having such restrictions and in need of bendamustine, and then administering thereto a bendamustine-containing composition in a volume of about 100 ml or less intravenously over a period of about 30 minutes or less. The smaller volumes and reduced sodium load as compared to currently known methods of treatment minimize cardiac and/or renal stress in patients having diseases such as congestive heart failure or renal disease.Type: ApplicationFiled: November 26, 2014Publication date: March 19, 2015Inventors: Srikanth Sundaram, Scott L. Tarriff
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Patent number: 8980920Abstract: The present invention relates to novel Linked Tricyclic Aryl Compounds, compositions comprising at least one Linked Tricyclic Compound, and methods of using Linked Tricyclic Aryl Compounds for treating or preventing HCV infection in a patient. in one aspect, the present invention provides Compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein: Non-limiting examples of the Compounds of Formula (II) include compound 56.Type: GrantFiled: May 28, 2010Date of Patent: March 17, 2015Assignee: Merck Sharp & Dohme Corp.Inventors: Qingbei Zeng, Kevin X. Chen, Anilkumar Gopinadhan Nair, Stuart B. Rosenblum, Joseph A. Kozlowski, F. George Njoroge
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Patent number: 8975416Abstract: Disclosed are compounds of formula (I), which are of use in the treatment of bacterial diseases and infections, to compositions containing those compounds and to methods of treating bacterial diseases and infections using the compounds. In particular, the compounds are useful for the treatment of infection with, and diseases caused by, Clostridium difficile.Type: GrantFiled: December 1, 2009Date of Patent: March 10, 2015Assignee: Summit Corporation PLCInventors: Paul James Davis, Olivier De Moor, Colin Richard Dorgan, Peter David Johnson, Alan Geoffrey Roach, Richard Storer, Richard John Vickers, Francis Xavier Wilson, Graham Michael Wynne
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Publication number: 20150065549Abstract: Provided herein are pharmaceutical formulations of dry-powder bendamustine suitable for pharmaceutical use. Also provided are methods of producing dry-powder bendamustine. The pharmaceutical formulations can be used for any disease that is sensitive to treatment with bendamustine, such as neoplastic diseases.Type: ApplicationFiled: August 22, 2014Publication date: March 5, 2015Inventor: Vasilios Voudouris
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Patent number: 8969588Abstract: 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: GrantFiled: March 13, 2013Date of Patent: March 3, 2015Assignee: Gilead Pharmasset LLCInventors: Robert William Scott, Fang Wang, Bing Shi, Erik Mogalian
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Patent number: 8969313Abstract: The invention relates to a method of preventing, inhibiting, arresting or reversing tumorigenesis in a cell as well as a method of inducing apoptosis in a tumor cell. The method includes increasing the amount and/or the activity of a DACT protein, or a functional fragment thereof, in the cell. Also provided is a pharmaceutical composition that comprises a compound of general formula (I), wherein A is CH or N, R1, R4 and R5 are independent from each other H, an aliphatic group, an alicyclic group, an aromatic group, an arylaliphatic group, and an arylalicyclic group comprising 0-3 heteroatoms. The heteroatoms may be N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen such as F, Cl, Br or L. R3 is H, F, Cl or an aliphatic or arylaliphatic group that includes 1-8 main chain carbon atoms and 0-3 heteroatoms. The pharmaceutical composition also comprises a histone deacetylase inhibitor.Type: GrantFiled: November 3, 2008Date of Patent: March 3, 2015Assignee: Agency for Science, Technology and ResearchInventor: Qiang Yu
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Publication number: 20150056300Abstract: The present disclosure generally relates to therapeutic nanoparticles. Exemplary nanoparticles disclosed herein may include about 0.1 to about 40 weight percent of a therapeutic agent and about 10 to about 90 weight percent a diblock poly(lactic) acid-poly(ethylene)glycol copolymer or a diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer, wherein the diblock poly(lactic) acid-poly(ethylene)glycol copolymer comprises poly(lactic) acid having a number average molecule weight of about 30 kDa to about 90 kDa or the diblock poly(lactic)-co-poly(glycolic) acid-poly(ethylene)glycol copolymer comprises poly(lactic)-co-poly(glycolic) acid having a number average molecule weight of about 30 kDa to about 90 kDa.Type: ApplicationFiled: October 24, 2011Publication date: February 26, 2015Applicant: BIND Therapeutics, Inc.Inventors: David Dewitt, Maria Figueiredo, Hong Wang, Greg Troiano, Young-Ho Song
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Publication number: 20150057272Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: August 1, 2014Publication date: February 26, 2015Inventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Publication number: 20150050210Abstract: The present invention is related to the field of pharmaceutical compositions for the treatment of various disease states, particularly neoplastic diseases and autoimmune diseases. It especially relates to the oral application of bendamustine and its derivatives. The invention further relates to a process for preparing a pharmaceutical composition which comprises bendamustine and its derivatives prepared by hot melt extrusion using pharmaceutically acceptable excipients. The invention also relates to such pharmaceutical compositions and hot melt extrudates.Type: ApplicationFiled: March 25, 2013Publication date: February 19, 2015Inventors: Akif Emre Tuereli, Bernd Baumstuemmler, Richard Ammer
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Publication number: 20150051258Abstract: Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use.Type: ApplicationFiled: November 3, 2014Publication date: February 19, 2015Inventors: Martin Ian Cooper, Laurent D. Courvoisier, Mark Eddleston, Robert E. McKean
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Publication number: 20150044169Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of identifying a candidate agent for the treatment of hepatitis C virus (HCV) infection, and the like.Type: ApplicationFiled: September 23, 2014Publication date: February 12, 2015Inventors: Shirit Einav, Jeffrey S. Glenn, Robert McDowell, Wenjin Yang, Hadas Dvory-Sobol
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Publication number: 20150038509Abstract: The invention relates to heterocyclic compounds consisting of a core nitrogen atom surrounded by three pendant groups, wherein two of the three pendant groups are preferably benzimidazolyl methyl and tetrahydroquinolyl, and the third pendant group contains N and optionally contains additional rings. The compounds bind to chemokine receptors, including CXCR4 and CCR5, and demonstrate protective effects against infection of target cells by a human immunodeficiency virus (HIV).Type: ApplicationFiled: June 12, 2014Publication date: February 5, 2015Inventors: Gary J. Bridger, Renato T. Skerlj, Al Kaller, Curtis Harwig, David Earl Bogucki, Trevor R. Wilson, Jason B. Crawford, Ernest J. McEachern, Bem Atsma, Siqiao Nan, Yuanxi Zhou, Dominique Schols, Christopher Dennis Smith, Maria Rosario DiFluri
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Publication number: 20150038501Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: October 20, 2014Publication date: February 5, 2015Inventors: Leping LI, Min ZHONG
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Publication number: 20150038488Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I wherein X1, X2, X3, R2, R3, R4, R5, and Y are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.Type: ApplicationFiled: July 31, 2014Publication date: February 5, 2015Inventors: Kevin S. Currie, Zhimin Du, Julie Farand, Juan A. Guerrero, Ashley A. Katana, Darryl Kato, Scott E. Lazerwith, Jiayao Li, John O. Link, Nicholas Mai, Gregory Notte, Hyung-Jung Pyun, Michael Sangi, Aaron C. Schmitt, Adam J. Schrier, Kirk L. Stevens, Chandrasekar Venkataramani, William J. Watkins, Zheng-Yu Yang, Jeff Zablocki, Sheila Zipfel
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Patent number: 8945510Abstract: Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.Type: GrantFiled: May 24, 2012Date of Patent: February 3, 2015Assignee: Probiodrug AGInventors: Ulrich Heiser, Daniel Ramsbeck, Hans-Ulrich Demuth
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Publication number: 20150031670Abstract: Compounds of the formula (I), in which R1, R3, R5, R6, R7, R, X and Y have the meanings indicated in Claim 1, are inhibitors of methionine aminopeptidase and can be employed for the treatment of tumours.Type: ApplicationFiled: March 21, 2013Publication date: January 29, 2015Applicant: MERCK PATENT GmbHInventors: Timo Heinrich, Frank Zenke, Mireille Krier, Manja Friese-Hamim, Jeyaprakashnarayanan Seenisamy
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Publication number: 20150025024Abstract: The present invention features solid compositions comprising a selected HCV inhibitor in an amorphous form. In one embodiment, the selected HCV inhibitor is formulated in an amorphous solid dispersion which comprises a pharmaceutically acceptable hydrophilic polymer and preferably a pharmaceutically acceptable surfactant.Type: ApplicationFiled: October 6, 2014Publication date: January 22, 2015Applicant: ABBVIE INC.Inventors: Yi Gao, Geoff Zhang
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Publication number: 20150023916Abstract: 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 such as Lassa fever, Argentine hemorrhagic fever, Bolivian hemorrhagic fever, and Venezuelan hemorrhagic fever.Type: ApplicationFiled: February 14, 2013Publication date: January 22, 2015Applicant: SIGA TECHNOLOGIES INC.Inventors: Dongcheng Dai, James R. Burgeson, Sean M. Amberg, Dennis E. Hruby
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Publication number: 20150011591Abstract: The present invention is directed to a compound of Formula I or a pharmaceutically acceptable salt thereof; wherein R, R1, R2, R3, R4, m, and n are as defined herein, to pharmaceutical compositions comprising said compound, and to methods of treating diseases or conditions mediated by elevated persistent sodium current, such as an ocular disorder, multiple sclerosis, seizure disorder, and chronic pain.Type: ApplicationFiled: September 24, 2014Publication date: January 8, 2015Inventors: George R. Ehring, Ellen Chao, Herman Ng, Hau Ton, Jia Chian Li, Joseph S. Adorante, Michael E. Garst, Howard B. Rind, Mark R. Hansen, Alfred Arthur Avey, JR., Lloyd Jay Dolby, Shervin Esfandiari, Vivian R. MacKenzie, Jeremiah Andrew Marsden, David Charles Muchmore
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Publication number: 20150011548Abstract: A compound of formula (I), wherein R3, R4, G, B, M, and Z are as defined in the claims, and pharmaceutically acceptable salts thereof are disclosed. The compounds of formula (I) possess utility as FGFR inhibitors and are useful in the treatment of a condition, where FGFR kinase inhibition is desired, such as cancer.Type: ApplicationFiled: October 9, 2012Publication date: January 8, 2015Inventors: Tero Linnanen, Gerd Wohlfahrt, Srinivas Nanduri, Ravi Ujjinamatada, Srinivasan Rajagopalan, Subhendu Mukherjee
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Publication number: 20150011512Abstract: The invention relates to novel compounds for use in the treatment or prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express cytochrome P450 1B1 (CYP1B1) and allelic variants thereof. The invention also provides pharmaceutical compositions comprising one or more such compounds for use in medical therapy, for example in the treatment of prophylaxis of cancers or other proliferative conditions, as well as methods for treating cancers or other conditions in human or non-human animal patients. The invention also provides methods for identifying novel compounds for use in the treatment of prophylaxis of cancers and other proliferative conditions that are for example characterized by cells that express CYP1 B1 and allelic variants thereof. The invention also provides a method for determining the efficacy of a compound of the invention in treating cancer.Type: ApplicationFiled: September 12, 2014Publication date: January 8, 2015Inventors: Steven Albert Everett, Saraj Ulhaq
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Patent number: 8927720Abstract: A compound satisfying formula I, a prodrug, N-oxide, addition salt, quaternary amine, metal complex, or a stereochemically isomeric form thereof; compositions contain these compounds as active ingredient and processes for preparing these compounds and compositions.Type: GrantFiled: December 16, 2011Date of Patent: January 6, 2015Assignee: Janssen R&D IrelandInventors: Ludwig Paul Cooymans, Samuël Dominique Demin, Lili Hu, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri, Sandrine Marie Helene Vendeville
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Patent number: 8927029Abstract: Disclosure is provided for methods of preventing, removing or inhibiting microbial biofilm formation or microbial infection in a plant or plant part thereof, including applying thereto a treatment effective amount of an active compound as described herein, or an agriculturally acceptable salt thereof. Methods of enhancing a microbicide (e.g., including a copper, antibiotic, bacteriophage, etc.) and/or plant defense activator are also provided, including applying an active compound as described herein. Compositions comprising an active compound as described herein in an agriculturally acceptable carrier are also provided, and in some embodiments the compositions further include a microbicide (e.g., including copper, antibiotic, bacteriophage, etc.) and/or plant defense activator.Type: GrantFiled: November 25, 2013Date of Patent: January 6, 2015Assignee: North Carolina State UniversityInventors: Christian Melander, John Cavanagh, David Ritchie, Robert W. Huigens, III, T. Eric Ballard, Justin J. Richards, Thomas W. Lindsey, Jonathan S. Lindsey
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Publication number: 20150005355Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with temozolomide (TMZ).Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Inventors: Cherrie K. Donawho, Vincent L. Giranda
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Publication number: 20150005354Abstract: The present invention describes benzimidazole derivatives of Formula (I) which constitute potent PARP inhibitors in combination with radiotherapy or in combination with other chemotherapeutic agents.Type: ApplicationFiled: September 12, 2014Publication date: January 1, 2015Inventors: Vincent L. Giranda, Cherrie K. Donawho
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Publication number: 20150005345Abstract: The present invention features benzhydrol-pyrazole derivatives and related compounds having kinase inhibitory activity. The compounds of the invention, alone or in combination with other pharmaceutically active agents, can be used for treating or preventing various medical conditions, such as cancers, inflammatory disorders, or autoimmune disorders.Type: ApplicationFiled: January 9, 2013Publication date: January 1, 2015Inventors: Anthony D. Keefe, Richard W. Wagner, Matthew Clark, Ying Zhang, Diana Gikunju, John Cuozzo, Heather Thomson
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Publication number: 20140378407Abstract: The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range ?5±1° C. to ?5±3° C.; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.Type: ApplicationFiled: March 29, 2012Publication date: December 25, 2014Applicant: Fresenius Kabi Oncology LimitedInventors: Dhiraj Khattar, Rajesh Khanna, Sanjay Motwani, Minakshi Garg, Vikas Chandel, Mukti Yadav, Vijay Kumar Kyama, Vikas Bhandari
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Publication number: 20140378453Abstract: The present invention relates to novel inhibitors of Factors VIIa, IXa, Xa, XIa, in particular Factor VIIa, pharmaceutical compositions comprising these inhibitors, and methods for using these inhibitors for treating or preventing thromboembolic disorders, cancer or rheumatoid arthritis. Processes for preparing these inhibitors are also disclosed.Type: ApplicationFiled: June 27, 2014Publication date: December 25, 2014Inventors: Aleksandr KOLESNIKOV, Roopa RAI, William Dvorak SHRADER, Steven M. TORKELSON, Kieron E. WESSON, Wendy B. YOUNG
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Publication number: 20140378518Abstract: New formulations of bendamustine hydrochloride having HPLC purity higher than 99% obtained through the lyophilization of aqueous solutions without organic solvents, are described.Type: ApplicationFiled: June 17, 2014Publication date: December 25, 2014Inventors: Stefano Turchetta, Maurizio Zenoni, Paolo Brandi
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Publication number: 20140371316Abstract: The present invention provides a process for the synthesis of substituted phenoxymethylpropiomc acid and related compounds. The compounds are useful for inhibiting the formation of AGEs (Advanced Glycation End Products).Type: ApplicationFiled: November 23, 2012Publication date: December 18, 2014Inventors: Jill S. FABRICANT, Iraj LALEZARI
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Patent number: 8912186Abstract: The invention provides specific small molecule compounds that allosterically regulate the activity or modulate protein-protein interactions of AGC protein kinases and the Aurora family of protein kinases, methods for their production, pharmaceutical compositions comprising same, and their use for preparing medicaments for the treatment and prevention of diseases related to abnormal activities of AGC protein kinases or of protein kinases of the Aurora family.Type: GrantFiled: October 16, 2009Date of Patent: December 16, 2014Assignee: Universitaet des SaarlandesInventors: Matthias Engel, Wolfgang Fröhner, Adriane Stroba, Ricardo M. Biondi
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Patent number: 8912199Abstract: 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: October 21, 2013Date of Patent: December 16, 2014Assignee: 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: 8912184Abstract: The invention relates to methods of treating diseases, particularly cancers, that respond favorably to the inhibition of Nicotinamide phosphoribosyltransferase (Nampt); it also relates to therapeutic methods that utilize Nampt inhibitors in combination with NAD biosynthesis precursors to intentionally kill cancer cells while limiting or minimizing toxicity to normal host cells; and it relates to methods of identifying cancers that will be most responsive to treatment with Nampt inhibitors, particularly when administered in combination with nicotinic acid.Type: GrantFiled: September 16, 2011Date of Patent: December 16, 2014Assignee: Alzheimer's Institute of America, Inc.Inventors: Tracey C. Fleischer, Daniel M. Cimbora, Jeffrey S. Flick, Andrew D. Gassman, Vijay R. Baichwal, Damon I. Papac
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Patent number: 8912336Abstract: In one aspect, the invention relates to sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: GrantFiled: November 8, 2010Date of Patent: December 16, 2014Assignee: Vanderbilt UniversityInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20140364444Abstract: 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: August 21, 2014Publication date: December 11, 2014Inventors: Hayato TAKYO, Masaki TAKAHASHI, Takamasa TANABE, Yoshihiko NOKURA, Mai ITO, Atsushi IWATA
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Publication number: 20140364473Abstract: A pharmaceutical solution with a pH value of 10 or higher contains an angiotensin II receptor antagonist, where one or more sugar alcohols are present up to a total concentration of 40 wt. % to 70 wt. %.Type: ApplicationFiled: August 27, 2014Publication date: December 11, 2014Applicant: BOEHRINGER INGELHEIM VETMEDICA GMBHInventors: Detlef Mohr, Stefan Lehner
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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: 8901313Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.Type: GrantFiled: March 15, 2012Date of Patent: December 2, 2014Assignee: Genentech, Inc.Inventors: Steven Staben, Jianwen Feng, Pui Leng Loke, Christian A. G. N. Montalbetti
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Patent number: 8895598Abstract: Briefly described, embodiments of this disclosure include compositions, pharmaceutical compositions, methods of treating a host infected with a virus from the Flaviviridae family of viruses, methods of identifying a candidate agent for the treatment of hepatitis C virus (HCV) infection, and the like.Type: GrantFiled: September 18, 2008Date of Patent: November 25, 2014Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Shirit Einav, Jeffrey S. Glenn, Robert McDowell, Wenjin Yang, Hadas Dvory-Sobol
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Publication number: 20140341989Abstract: Dosing regimens, methods of treatment, controlled release formulations, and combination therapies that include bendamustine, or a pharmaceutically acceptable salt thereof and an HDAC inhibitor, or a pharmaceutically acceptable salt thereof, are described.Type: ApplicationFiled: September 13, 2011Publication date: November 20, 2014Applicants: PHARMACYCLICS, INC.Inventors: David J. Loury, Joseph J. Buggy, Tarak D. Mody, Erik J. Verner, Norbert Purro, Sriram Balasubramanian, Ioana Kloos, Stephane Depil