Three Or More Hetero Atoms In The Tricyclo Ring System Patents (Class 514/293)
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Publication number: 20140323516Abstract: Pharmaceutical formulations and methods for the topical and/or transdermal delivery of imiquimod, including creams, ointments and pressure-sensitive adhesive compositions to treat dermatological disorders, namely, viral infections, such as Type I or Type II Herpes simplex infections and genital and perianal warts, actinic deratosis and superficial basal cell carcinoma, and to induce interferon biosynthesis to achieve an antiviral effect, with shorter durations of therapy, than currently approved for imiquimod by the Food & Drug Administration (“FDA”).Type: ApplicationFiled: November 27, 2013Publication date: October 30, 2014Applicant: Medicis Pharmaceutical CorporationInventors: Jefferson J. Gregory, Michael T. Nordsiek
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Patent number: 8871782Abstract: Imidazoquinoline compounds with an alkoxy substituent at the 6, 7, 8, or 9-position, pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of use of these compounds as immunomodulators, for inducing or inhibiting cytokine biosynthesis in animals and in the treatment of diseases including viral, and neoplastic, are disclosed.Type: GrantFiled: October 1, 2004Date of Patent: October 28, 2014Assignee: 3M Innovative Properties CompanyInventors: Kyle J. Lindstrom, Bryon A. Merrill, Chad A. Haraldson, Michael J. Rice, Tushar A. Kshirsagar, Philip D. Heppner, Joshua R. Wurst, Shri Niwas, Sarah C. Johannessen
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Publication number: 20140314815Abstract: The present invention is drawn to adhesive solid gel-forming formulations, methods of drug delivery, and solidified gel layers for dermal delivery of a drug. The formulation can include a drug, a solvent vehicle, and a gelling agent. The solvent vehicle can include a volatile solvent system having one or more volatile solvent, and a non-volatile solvent system having one or more non-volatile solvent, wherein at least one non-volatile solvent is flux-enabling non-volatile solvent(s) capable of facilitating the delivery of the drug at therapeutically effective rates over a sustained period of time. The formulation can have a viscosity suitable for application to a skin surface prior to evaporation of the volatile solvents system. When applied to the skin, the formulation can form a solidified gel layer after at least a portion of the volatile solvent system is evaporated. The solidified gel layer is can be removed by peeling or washing.Type: ApplicationFiled: January 22, 2014Publication date: October 23, 2014Applicant: Nuvo Research Inc.Inventors: Jie Zhang, Kevin S. Warner, Sanjay Sharma
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Publication number: 20140315916Abstract: The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.Type: ApplicationFiled: October 23, 2012Publication date: October 23, 2014Inventors: Latha G. Nair, Stephane L. Bogen, Ronald J. Doll, Yao Ma, Yuan Tian
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Publication number: 20140315943Abstract: A pharmaceutical composition comprising an mTOR/PI3K inhibitor, and an Hsp90 inhibitor according to the following formulae (I) and (Ia) or tautomers, or pharmaceutically acceptable salts thereof, wherein the variables in the structural formulae are defined herein. Also provided are methods for treating a proliferative disorder in a subject in need thereof, using pharmaceutical compositions described herein.Type: ApplicationFiled: May 23, 2012Publication date: October 23, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: David Proia, Suqin He
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Patent number: 8865713Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: September 3, 2013Date of Patent: October 21, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20140294856Abstract: The invention provides compositions comprising a Histone Deacetylase 6 (HDAC6) inhibitor and an AKT inhibitor, pharmaceutical compositions/formulations and kits of parts comprising the same; optionally further comprising one or more anti-cancer agents. The compositions of the invention provide for surprisingly efficacious killing of inter alia, cancer cells. Thus, the invention also provides for the use of the compositions, pharmaceutical compositions and kits of parts in medicine, and further, for use in the prevention or treatment of cancer and/or neuro-degenerative conditions, including Alzheimer's disease, Parkinson's disease, Huntington's disease, Amyotrophic lateral sclerosis (ALS), spinal and bulbar muscular atrophy (SbMA), Rubinstein-Taybi syndrome, Rett syndrome, and Friedreich's ataxia, or autoimmune diseases, including Rheumatoid Arthritis, Myasthenia Gravis, and Multiple Sclerosis.Type: ApplicationFiled: June 21, 2012Publication date: October 2, 2014Inventors: Eric O. Aboagye, Maciej A. Kaliszczak
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Publication number: 20140296219Abstract: The present invention is directed to methods, kits, and uses of inhibitors of LCMV mediated NF-?B activation to treat viral infections and inflammatory conditions.Type: ApplicationFiled: November 14, 2013Publication date: October 2, 2014Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Robert W. Finberg, Evelyn A. Kurt-Jones, Shenghua Zhou
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Publication number: 20140296272Abstract: The present invention relates to a series of compounds having antiviral activity, more specifically HIV (Human Immunodeficiency Virus) replication inhibiting properties. The invention also relates to methods for the preparation of such compounds, as well as to novel intermediates useful in one or more steps of such syntheses. The invention also relates to pharmaceutical compositions comprising an effective amount of such compounds as active ingredients. This invention further relates to the use of such compounds as medicines or in the manufacture of a medicament useful for the treatment of animals suffering from viral infections, in particular HIV infection. This invention further relates to methods for the treatment of viral infections in animals by the administration of a therapeutic amount of such compounds, optionally combined with one or more other drugs having anti-viral activity.Type: ApplicationFiled: June 17, 2014Publication date: October 2, 2014Inventors: Dorothée Bardiot, Patrick Chaltin, Frauke Christ, Zeger Debyser, Marc De Maeyer, Arnaud Marchand, Damien Marchand, Arnout Voet
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Patent number: 8846023Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.Type: GrantFiled: September 9, 2013Date of Patent: September 30, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Carol Bachand, Makonen Belema, Daniel H. Deon, Andrew C. Good, Jason Goodrich, Clint A. James, Rico Lavoie, Omar D. Lopez, Alain Martel, Nicholas A. Meanwell, Van N. Nguyen, Jeffrey Lee Romine, Edward H. Ruediger, Lawrence B. Snyder, Denis R. St. Laurent, Fukang Yang, David R. Langley, Gan Wang, Lawrence G. Hamann
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Patent number: 8846710Abstract: A method of preferentially inducing IFN-? biosynthesis in an animal comprising administering certain imidazo[4,5-c] ring compounds with a hydroxymethyl or hydroxyethyl substituent at the 2-position or pharmaceutical compositions containing the compounds, intermediates, methods of making, and methods of using these compounds a immunomodulators for treatment of diseases including viral and neoplastic diseases comprising preferentially inducing IFN-? biosynthesis in an animal are disclosed.Type: GrantFiled: February 22, 2006Date of Patent: September 30, 2014Assignee: 3M Innovative Properties CompanyInventors: Tushar A. Kshirsagar, Bryon A. Merrill, Scott E. Langer, Kyle J. Lindstrom, Sarah C. Slania, Gregory J. Marszalek, Joshua R. Wurst, Karl J. Manske, Shri Niwas, Gregory D. Lundquist, Jr., Philip D. Heppner, George W. Griesgraber, Michael E. Danielson
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Publication number: 20140288062Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: June 6, 2014Publication date: September 25, 2014Inventors: John Emmerson Campbell, Philip Jones, Michael Charles Hewitt
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Publication number: 20140286899Abstract: A class of compounds that inhibit Hepatitis C Virus (HCV) is disclosed, along with compositions containing the compound, and methods of using the composition for treating individuals infected with HCV.Type: ApplicationFiled: November 18, 2013Publication date: September 25, 2014Applicant: Presidio Pharmaceuticals, Inc.Inventors: Min Zhong, Leping Li
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Publication number: 20140288018Abstract: The present invention relates to methods for predicting the response to treatment with an agonist of TLR7, or an agonist of TLR8 or an anti-cancer agent for treating cancer, in particular non-small cell lung cancer comprising the step of detecting the expression of TLR7 or TLR8 in cancer cells of said patient.Type: ApplicationFiled: March 27, 2014Publication date: September 25, 2014Applicant: INSERM (Institut National de la Sante et de la Recherche Medicale )Inventors: Julien Cherfils, Herve Fridman, Isabelle Cremer
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Publication number: 20140256722Abstract: The present invention is directed to benzoimidazole compounds of the formula: and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: ApplicationFiled: May 20, 2014Publication date: September 11, 2014Applicant: Janssen Pharmaceutica NVInventors: Frances Meredith HOCUTT, Barry Eastman Leonard, JR., Hillary M. Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D. Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Patent number: 8829024Abstract: The present invention provides compositions of an anti-inflammatory glucocorticosteroid and a glucocorticoid receptor (GR) modulator useful for inhibiting glucocorticoid receptor induced transactivation without substantially inhibiting glucocorticoid receptor induced transrepression. Also provided are methods of treating a disorder or condition and reducing the side effects of glucocorticosteroid treatment, using the compositions of the present invention.Type: GrantFiled: January 6, 2012Date of Patent: September 9, 2014Assignee: Corcept Therapeutics, Inc.Inventors: Joe Belanoff, Peter Lockey
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Publication number: 20140249143Abstract: Provided are certain compounds and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and their use for treating viral infections.Type: ApplicationFiled: October 19, 2012Publication date: September 4, 2014Applicant: GlaxoSmithKline LLCInventors: Anna Lindsey Banka, Janos Botyanszki, Eric Gregory Burroughs, John George Catalano, Wendy Huang Chern, Hamilton D. Dickson, Margaret J. Gartland, Robert Hamatake, Hans Hofland, Jesse Daniel Keicher, Christopher Brooks Moore, John Bradford Shotwell, Matthew David Tallant, Jean-Philippe Therrien, Shihyun You
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Patent number: 8822448Abstract: The present inventors have investigated a compound which has a PDE9-inhibiting action and is useful as an active ingredient for an agent for treating and/or preventing storage dysfunction, voiding dysfunction, bladder/urethral diseases, and the like, and thus, have found that a pyrazoloquinoline compound has a PDE9-inhibiting action, thereby completing the present invention.Type: GrantFiled: March 7, 2013Date of Patent: September 2, 2014Assignee: Astellas Pharma Inc.Inventors: Hiroyuki Kaizawa, Hirofumi Yamamoto, Kazunori Kamijo, Mari Sugita, Ryushi Seo, Satoshi Yamamoto, Atsushi Ukai
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Publication number: 20140243396Abstract: Imidazoquinolines, as set forth in formula (I), are useful for inhibiting growth or proliferation of mucoepidermoid carcinoma cells. The therapeutic and prophylactic treatments provided by this invention are practiced by administering to a patient in need thereof an amount of a compound of formula (I) that is effective to inhibit growth or proliferation of the mucoepidermoid carcinoma cells.Type: ApplicationFiled: September 27, 2012Publication date: August 28, 2014Inventors: James D. Griffin, Lizi Wu, Jie Chen
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Publication number: 20140243321Abstract: Described herein are monomers capable of forming a biologically useful multimer when in contact with one, two, three or more other monomers in an aqueous media. In one aspect, such monomers may be capable of binding to another monomer in an aqueous media (e.g. in vivo) to form a multimer, (e.g. a dimer). Contemplated monomers may include a ligand moiety, a linker element, and a connector element that joins the ligand moiety and the linker element. In an aqueous media, such contemplated monomers may join together via each linker element and may thus be capable of modulating one or more biomolecules substantially simultaneously, e.g., modulate two or more binding domains on a protein or on different proteins.Type: ApplicationFiled: February 28, 2014Publication date: August 28, 2014Applicant: Coferon, Inc.Inventors: Lee Daniel Arnold, Kenneth W. Foreman, Douglas S. Werner
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Publication number: 20140235616Abstract: The invention relates to compounds corresponding to formula (I), in which R1, R2 and R3 are as defined in Claim 1, and also to the process for preparing them and to their therapeutic use.Type: ApplicationFiled: September 24, 2012Publication date: August 21, 2014Applicant: SANOFIInventors: Alexandre Benazet, Olivier Duclos, Nathalie Guillo, Gilbert Lassalle, Karim Macary, Valerie Vin
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Publication number: 20140234428Abstract: The invention, a transdermal delivery method, relates to penetration-enhancing pharmaceutical compositions comprising a novel, stable mixture of cetylated esters, cetyl or stearyl alcohols, polar solvents and surfactants, which, under appropriate conditions, combine into amphiphilic nanoparticles within a stabilized liquid dispersion for use in delivery of medicinal agents through the skin. The term cetosomes is used to describe these particles in order to differentiate them from other nanoparticles, such as niosomes, cerasomes, polymeric micelles, dendrimers, liposomes, lipoids, solid lipid nanoparticles and other particles. The self-assembling cetosomes, with both ionic and nonionic points of attraction, incorporate and concentrate a variety of different bioactive agents of interest and demonstrate stable properties with similarities to colloidal molecular structures. The compositions enhance topical transdermal fluxes of bioactives without permanently disrupting natural skin barrier function.Type: ApplicationFiled: February 15, 2013Publication date: August 21, 2014Applicant: Cymbiotics, Inc.Inventors: Raj R. Barathur, Jack Bain Bookout
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Patent number: 8802712Abstract: The invention relates to compounds of the formulae (I), (II) and (III), and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitisation of cancer cells to anticancer agents and/or ionising radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumours, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent.Type: GrantFiled: June 24, 2011Date of Patent: August 12, 2014Assignee: Merck Patent GmbHInventors: Thomas Fuchss, Werner Mederski, Frank Zenke
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Publication number: 20140221338Abstract: The present invention provides compounds of Formula (Ia): or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: August 6, 2012Publication date: August 7, 2014Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J. P. Pinto, James R. Corte, Paul J. Gilligan, Tianan Fang, Leon M. Smith, II, Yufeng Wang, Wu Yang, William R. Ewing
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Patent number: 8796303Abstract: The present invention relates to compounds of formula (I), racemates, isomers and/or salts thereof useful in the treatment of viral infections, in particular respiratory syncytial virus (RSV) infections. The present invention also relates to processes for preparing the compounds.Type: GrantFiled: November 22, 2011Date of Patent: August 5, 2014Assignee: Biota Scientific Management Pty Ltd.Inventors: Penelope Anne Mayes, Jeffrey Peter Mitchell, Alistair George Draffan, Gary Robert William Pitt, Kelly Helen Anderson, Chin Yu Lim
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Publication number: 20140213610Abstract: Compounds of Formula (I) inhibit the PARP enzyme and are useful for treating a disease or a disorder associated with PARP. Also disclosed are pharmaceutical compositions comprising compounds of Formula (I), methods of treatment comprising compounds of Formula (I), and methods of inhibiting the PARP enzyme comprising compounds of Formula (I).Type: ApplicationFiled: August 27, 2013Publication date: July 31, 2014Applicant: AbbVie Inc.Inventors: Thomas D. Penning, Gui-Dong Zhu, Virajkumar B. Gandhi, Jianchun Gong, Vincent L. Giranda
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Publication number: 20140212442Abstract: The invention provides compounds of formula I: wherein R1-R3, Ra, and Rb have any of the values defined herein, and salts thereof. The compounds have immunomodulatory properties.Type: ApplicationFiled: August 30, 2012Publication date: July 31, 2014Applicant: REGENTS OF THE UNIVERSITY OF MINNESOTAInventors: David M. Ferguson, John Ohlfest, Courtney Aldrich
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Patent number: 8791131Abstract: The present invention is directed to compounds of Formula (I), and to salts thereof, their synthesis, and their use as PI3-K? inhibitors and/or PI3-K?/mTOR dual inhibitors.Type: GrantFiled: September 18, 2009Date of Patent: July 29, 2014Assignee: Pfizer Inc.Inventors: Hengmiao Cheng, Ted William Johnson, Jacqui Elizabeth Hoffman, Lisa Chen Guo, Zhengyu Liu
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Patent number: 8791133Abstract: The disclosure relates to compounds of formula I: wherein the groups R1, R2, R3, R4, R5 and X are as defined in the disclosure, having antithrombotic activity, which in particular inhibits the protease-activated receptor 1 (PAR1). The disclosure further relates to methods for producing the same and to the use thereof as a pharmaceutical product.Type: GrantFiled: October 16, 2012Date of Patent: July 29, 2014Assignee: SanofiInventors: Karl Schoenafinager, Henning Steinhagen, Bodo Scheiper, Uwe Heinelt, Volkmar Wehner, Matthias Herrmann, Jacques Mauger, Pavel Safar
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Publication number: 20140206678Abstract: The present invention provides methods for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR. The invention also provides methods for treating or preventing viral infections using modulators of host cell enzymes relating to mTOR and modulators of the unfolded protein response.Type: ApplicationFiled: January 27, 2012Publication date: July 24, 2014Applicants: KADMON CORPORATION, LLC, THE TRUSTEES OF PRINCETON UNIVERSITYInventors: Thomas Shenk, Ji-In Kim
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Patent number: 8779154Abstract: The invention relates to certain fused ring compounds, or pharmaceutically acceptable salts, solvates, clathrates, or prodrugs thereof, that are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.Type: GrantFiled: September 25, 2007Date of Patent: July 15, 2014Inventors: Qinglin Che, Nha Huu Vo, Shoujun Chen
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Patent number: 8778963Abstract: Imidazo-quinoline, -pyridine, and -naphthyridine ring systems substituted at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.Type: GrantFiled: November 24, 2004Date of Patent: July 15, 2014Assignee: 3M Innovative Properties CompanyInventors: Larry R. Krepski, Joseph F. Dellaria, Jr., Gregory J. Marszalek
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Publication number: 20140194414Abstract: This disclosure relates to new tetracyclic compounds that may be used to modulate a histamine receptor in an individual. The compounds in one embodiment are tetracyclic[4,3-b]indoles. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.Type: ApplicationFiled: March 8, 2013Publication date: July 10, 2014Applicant: MEDIVATION TECHNOLOGIES, INC.Inventor: MEDIVATION TECHNOLOGIES, INC.
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Patent number: 8771682Abstract: The present invention relates generally to methods and compositions for reducing Interleukin-4 or Interleukin-13 signaling, in particular to treat asthma and atopic dermatitis. The inventors have found that Rac/PAK mediated endocytosis of the ligand bound type I (IL-4R with the chains IL-4Ra and IL-2-Rg) and/or type II receptor (IL-13R with the chains IL-4Ra and IL-13Ra1) is needed for the IL-4 and/or IL-13 mediated activation of downstream signalling events including phosphorylation of Stat family transcrition factors. These discoveries enable new methods of screening compounds that modulate Interleukin-4 and Interleukin-13 signalling, as well as new methods for treating conditions characterized by increased Interleukin-4 and Interleukin-13 levels. These conditions include inflammatory conditions, asthma bronchiale, atopic dermatitis, allergies, atopic syndromes, allergic rhinitis, and th2-induced conditions.Type: GrantFiled: April 26, 2012Date of Patent: July 8, 2014Assignee: Technische Universtität DresdenInventors: Christian Bökel, Thomas Weidemann
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Publication number: 20140187575Abstract: Pharmaceutical formulations and methods for the topical or transdermal delivery of 1isobutyl-1H-imidazo[4,5-c]-quinolin-4-amine, or 1-(2-methylpropyl)-1H-imidazo[4,5 c]quinolin-4-amine, i.e., imiquimod, to treat genital/perianal warts with shorter durations of therapy than currently prescribed for the commercially available for Aldara® 5% imiquimod cream, as now approved by the U.S. Food & Drug Administration (“FDA”), are disclosed and described. More specifically, lower dosage strength imiquimod formulations to deliver an efficacious dose of imiquimod for treating genital/perianal warts with an acceptable safety profile and dosing regimens that are shorter and more convenient for patient use than the dosing regimen currently approved by the U.S. Food & Drug Administration (“FDA”) for Aldara® 5% imiquimod cream to treat genital/perianal warts are also disclosed and described.Type: ApplicationFiled: November 27, 2013Publication date: July 3, 2014Applicant: Medicis Pharmaceutical CorporationInventors: Michael T. Nordsiek, Jefferson J. Gregory
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Publication number: 20140179682Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.Type: ApplicationFiled: June 8, 2012Publication date: June 26, 2014Applicant: SUNOVION PHARMACEUTICALS INC.Inventors: Michele L. R. Heffernan, Larry Wendell Hardy, Frank Xinhe Wu, Lakshmi D. Saraswat, Kerry L. Spear
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Publication number: 20140178366Abstract: The present invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of hypoxia in cancerous cells in the subject. In one embodiment, the invention provides methods for the preselection of a subject for therapeutic treatment with an agent based on modulated levels of lactate dehydrogenase (LDH) in a cell, e.g., a cancerous cell. The invention also provides methods for treating cancer in a subject by administering an effective amount of an agent to the subject, wherein the subject has been selected based on a modulated level of hypoxia. The invention further provides kits to practice the methods of the invention.Type: ApplicationFiled: December 17, 2013Publication date: June 26, 2014Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Ronald K. Blackman, Vojo Vukovic
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Publication number: 20140179671Abstract: The present invention provides a novel class of fused ring azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: September 12, 2013Publication date: June 26, 2014Applicant: Corcept Therapeutics, Inc.Inventors: Robin D. Clark, Nicholas C. Ray, Paul M. Blaney, Christopher A. Hurley, Karen Williams
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Patent number: 8759345Abstract: The present invention is directed to benzoimidazole compounds of the formula (1) and enantiomers, diastereomers, racemates, and pharmaceutically acceptable salts thereof. Compounds of the present invention are useful in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions modulated by prolyl hydroxylase activity.Type: GrantFiled: April 28, 2009Date of Patent: June 24, 2014Assignee: Janssen Pharmaceutica NVInventors: Frances Meredith Hocutt, Barry Eastman Leonard, Jr., Hillary M Peltier, Victor K. Phuong, Michael H. Rabinowitz, Mark D Rosen, Kyle T. Tarantino, Hariharan Venkatesan, Lucy Xiumin Zhao
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Publication number: 20140171407Abstract: The invention relates to 1,7-diazacarbazole compounds of Formula (I), (I-a) and (I-b) which are useful as kinase inhibitors, more specifically useful as checkpoint kinase 1 (chk1) inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: ApplicationFiled: February 17, 2014Publication date: June 19, 2014Applicant: Genentech, Inc.Inventors: Hazel Joan Dyke, Lewis Gazzard, Karen Williams, Huifen Chen, Samuel Kintz, Joy Drobnick, Joseph P. Lyssikatos, Simon Goodacre, Calum Macleod, Charles Ellwood
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Publication number: 20140170112Abstract: In alternative embodiments the invention provides compositions, e.g., pharmaceutical compositions and preparations, formulations, kits and other products of manufacture, e.g., exemplary drug combinations packaged together or separately in blister packs, lidded blisters or blister cards, or wrapped in paper, plastic or cellophane wrappers (e.g., a shrink wrap), comprising a combination regimen of at least two active ingredients designed to diminish systemic inflammation by targeting (inhibiting) two different, but convergent, signaling pathways, i.e., the sympathetic nervous system and the lipid-derived autacoid system; and methods for making and using these compositions. In alternative embodiments, the compositions of the invention (e.g., the combination of drugs) are used to ameliorate, diminish, treat, block or prevent an inflammatory response secondary to an infection, e.g., a viral infection and/or a reactivation.Type: ApplicationFiled: March 8, 2012Publication date: June 19, 2014Applicant: VICUS THERAPEUTICS, LLCInventors: John Maki, Newell Bascomb, Timothy J. Turner, Fredric Young
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Publication number: 20140171462Abstract: Novel quinoline compounds pharmaceutical compositions containing such compounds and their use in therapy.Type: ApplicationFiled: August 15, 2012Publication date: June 19, 2014Applicant: GlaxcoSmithKline LLCInventors: Emmanuel Hubert Demont, Katherine Louise Jones, Robert J. Watson
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Publication number: 20140155384Abstract: Hydrogenated pyrido[4,3-b]indoles, pyrido[3,4-b]indoles and azepino[4,5-b]indoles are described. The compounds may bind to and are antagonists of the adrenergic receptor a2A. The compounds may also bind to and are an antagonist of the adrenergic receptor ?2B; or the compounds are not antagonists of the adrenergic receptor ?2? and the compounds are administered in conjunction with a second agent that reduces, or is expected to reduce, blood pressure in an individual. The compounds may find use in therapy, e.g., to regulate blood glucose level, increase insulin secretion and treat diseases or conditions that are, or are expected to be, responsive to an increase in insulin production. Use of the compounds to treat type 2 diabetes is particularly described.Type: ApplicationFiled: February 17, 2012Publication date: June 5, 2014Applicant: Medivation Technologies, Inc.Inventors: Andrew Asher Protter, Sarvajit Chakravarty
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Patent number: 8735422Abstract: A cationic pharmaceutically active ingredient containing composition is provided. The composition includes a cationic pharmaceutically active ingredient, a hydrophobic polymer/hydrophilic polymer adduct comprising a poly(vinylpyrrolidone/alkylene) polymer and a polymer comprising carboxylic acid groups, hydroxyl groups, or a mixture of carboxylic acid groups and hydroxyl groups, a compatibilizing amount of a long chain organic acid having a carbon chain of at least 8 carbon atoms, and at least about 50 wt. % water.Type: GrantFiled: February 5, 2010Date of Patent: May 27, 2014Assignee: Skinvisible Pharmaceuticals, Inc.Inventors: James A. Roszell, Jie Zhang
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Publication number: 20140140932Abstract: The present disclosure provides functionalized magnetic nanoparticles (MNPs) comprising a functional group that binds to ?-amyloid deposits and/or neurofibrillary tangles. The present disclosure provides compositions comprising the functionalized MNPs, and methods of using the functionalized MNPs in imaging ?-amyloid deposits and neurofibrillary tangles.Type: ApplicationFiled: April 4, 2012Publication date: May 22, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventor: Masoud Akhtari
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Publication number: 20140121231Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof wherein X, M, Y, R1 and R2 are as defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 19, 2013Publication date: May 1, 2014Inventors: David Robert Bolin, Javier de Vicente Fidalgo, Johannes Hermann, Parcharee Tivitmahaisoon, Lin Yi, Mark Zak
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Publication number: 20140121198Abstract: The present invention provides tricyclic fused thiophene derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: October 31, 2013Publication date: May 1, 2014Applicant: Incyte CorporationInventors: Yun-Long Li, Wenyu Zhu, Song Mei, Joseph Glenn
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Patent number: 8710046Abstract: Novel 5-HT3 receptor modulators are disclosed. These compounds are used in the treatment of various disorders, including chemotherapy-induced nausea and vomiting, post-operative nausea and vomiting, and irritable bowel syndrome. Methods of making these compounds are also described in the present invention.Type: GrantFiled: June 30, 2010Date of Patent: April 29, 2014Assignee: Albany Molecular Research, Inc.Inventors: Peter R. Guzzo, David D. Manning, William Earley
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Publication number: 20140107141Abstract: The present invention provides compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting kinase (e.g., GSK3 (e.g., GSK3? or GSK3?) or CK1) activity. The present invention further provides methods of using the compounds described herein for treating kinase-mediated disorders, such as neurological diseases, psychriatic disorders, metabolic disorders, and cancer.Type: ApplicationFiled: October 11, 2013Publication date: April 17, 2014Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, The Broad Institute, Inc.Inventors: Florence Fevrier Wagner, Jennifer Q. Pan, Sivaraman Dandapani, Andrew Germain, Edward Holson, Benito Munoz, Partha P. Nag, Michel Weiwer, Michael C. Lewis, Stephen J. Haggarty, Joshua A. Bishop
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Publication number: 20140093505Abstract: The present invention relates to a pyridonaphthyridine compound as represented by general formula (I), which has a dual PI3K and mTOR inhibition effect, and its pharmaceutically acceptable salt, stereoisomer and deuteride thereof, wherein R1, R2, R3, R4, R5, R6, R7 and X are as defined in the specification; the present invention also relates to a method for preparing said compound, a pharmaceutical composition and a pharmaceutical formulation containing said compound, and uses of said compound in treating and/or preventing a proliferative disease and in the manufacture of a medicament for treating and/or preventing a proliferative disease.Type: ApplicationFiled: June 4, 2012Publication date: April 3, 2014Applicant: Xuanzhu Pharma Co., Ltd.Inventors: Frank Wu, Yan Zhang