Enzyme Inactivation By Chemical Treatment Patents (Class 435/184)
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Publication number: 20130280763Abstract: The present invention relates to the use of Archease proteins as RNA ligase enhancer, methods of ligating RNA molecules, kits for these methods and uses and transgenic cells.Type: ApplicationFiled: April 23, 2013Publication date: October 24, 2013Applicant: IMBA - INSTITUT FUR MOLEKULARE BIOTECHNOLOGIE GMBHInventors: Johannes POPOW, Javier MARTINEZ, Anne NIELSEN, Alexander SCHLEIFFER
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Publication number: 20130280286Abstract: The medicament for the prevention or the relief of poisoning by large clostridial cytotoxins (LCTs), in particular Clostridium difficile toxins A and B (TcdA and TcdB), is characterized by containing as active ingredient at least one effector, namely an inhibitor or activator of the autocatalytic protease activity of LCTs (large clostridial cytotoxins).Type: ApplicationFiled: May 30, 2012Publication date: October 24, 2013Applicant: JOHANNES GUTENBERG-UNIVERSITAET MAINZInventors: Christoph VON EICHEL-STREIBER, Jessica REINEKE, Stefan TENZER, Hansjörg SCHILD, Maja RUPNIK
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Publication number: 20130274218Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: ApplicationFiled: April 11, 2013Publication date: October 17, 2013Applicant: Biota Scientific Management Pty LtdInventors: Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding, Silas Bond, Rosliana Halim
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Publication number: 20130274259Abstract: Compounds, compositions and methods useful for treatment of Flt3-mediated diseases or conditions are provided herewith. Also provided herewith are methods for modulating the receptor protein tyrosine like kinase 3(Flt3).Type: ApplicationFiled: March 11, 2013Publication date: October 17, 2013Inventors: Chao Zhang, Gideon Bollag, Gaston Habets, Jiazhong Zhang, Prabha N. Ibrahim, Guoxian Wu
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Publication number: 20130274179Abstract: The present invention relates to viral polymerase inhibitors of formula (I) or salts, N-oxides, solvates, hydrates, racemates, enantiomers or isomers thereof, processes for their preparation and their use in the treatment of Flaviviridae viral infections such as Hepatitis C virus (HCV) infections.Type: ApplicationFiled: April 11, 2013Publication date: October 17, 2013Applicant: Biota Scientific Management Pty LtdInventors: Silas Bond, Rosliana Halim, Tyrone Pieter Jeynes, Alistair George Draffan, Michael Harding
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Patent number: 8557552Abstract: Compounds and related methods for selective inhibition of neuronal nitric oxide synthase over inducible and endothelial isoforms, such compounds as can provide reduced cationic character and enhanced bioavailability.Type: GrantFiled: April 6, 2012Date of Patent: October 15, 2013Assignee: Northwestern UniversityInventors: Richard B. Silverman, Haitao Ji, He Huang
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Publication number: 20130267498Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: February 13, 2013Publication date: October 10, 2013Inventors: Ronald Knegtel, Jean-Damien Charrier, Steven Durrant, Guy Brenchley, Michael Mortimore
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Publication number: 20130266636Abstract: In alternative embodiments, the invention provides methods for regulating or modulating RAF kinases. In alternative embodiments, the invention provides methods for ameliorating, preventing and/or treating diseases, infections and/or conditions having unwanted, pathological or aberrant cell proliferation, or that are responsive to inhibition or arrest of cell growth, by administration of an allosteric RAF inhibitor and/or any agent which prevents localization of RAF to mitotic spindles or mid-bodies.Type: ApplicationFiled: August 12, 2011Publication date: October 10, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: David Cheresh, Eric Murphy, Ainhoa Mielgo
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Publication number: 20130267530Abstract: The present invention provides a solid form and compositions thereof, which are useful as an inhibitor of EGFR kinases and which exhibit desirable characteristics for the same.Type: ApplicationFiled: March 13, 2013Publication date: October 10, 2013Inventor: Mei Lai
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Publication number: 20130261101Abstract: The present invention provides bicyclic azaheterocyclobenzylamines of Formula I: wherein the variables are defined herein, that modulate the activity of phosphoinositide 3-kinases (PI3Ks) and are useful in the treatment of diseases related to the activity of PI3Ks including, for example, inflammatory disorders, immune-based disorders, cancer, and other diseases.Type: ApplicationFiled: April 1, 2013Publication date: October 3, 2013Inventors: Andrew P. Combs, Richard B. Sparks, Thomas P. Maduskuie, Jr.
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Publication number: 20130261052Abstract: Proteases such as memapsin-1 are import enzymes, playing roles in a variety of diseases including diabetes. The inventors have developed inhibitors of memapsin 1 and methods of use therefore in the treatment of disease.Type: ApplicationFiled: March 11, 2013Publication date: October 3, 2013Applicant: Oklahoma Medical Research FoundationInventors: Jordan Tang, Xiangping Huang, Deborah Downs
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Publication number: 20130261113Abstract: This invention relates to novel 2,3-dihydroimidazo[1,2-c]quinazoline compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for phosphotidylinositol-3-kinase (PI3K) inhibition and treating diseases associated with phosphotidylinositol-3-kinase (PI3K) activity, in particular treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: June 3, 2013Publication date: October 3, 2013Inventors: Martin HENTEMANN, Jill WOOD, William SCOTT, Martin MICHELS, Ann-Marie CAMPBELL, Ann BULLION, Ronald ROWLEY, Aniko REDMAN
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Publication number: 20130261134Abstract: This invention relates to novel mesylate salt forms of the following Compound (1), and methods for the preparation thereof, pharmaceutical compositions thereof, and their use in methods for the treatment of Hepatitis C Viral (HCV) infection:Type: ApplicationFiled: March 15, 2013Publication date: October 3, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Zhibin LI, Bing-Shiou YANG, Kazuhiko YIP
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Publication number: 20130261114Abstract: The present invention relates to compounds useful as inhibitors of choline kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions.Type: ApplicationFiled: September 21, 2012Publication date: October 3, 2013Inventors: Simon Everitt, Ronald Knegtel, Michael Mortimore, Alistair Rutherford
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Publication number: 20130261102Abstract: Heterocyclic entities that modulate PI3 kinase activity, pharmaceutical compositions containing the heterocyclic entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: May 24, 2011Publication date: October 3, 2013Inventors: Pingda Ren, Yi Liu, Liansheng Li, Katrina Chan, Troy Edward Wilson, Simon Fraser Campbell
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Publication number: 20130252934Abstract: Compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative, pain and inflammatory diseases. Methods of using compounds of Formula I or a stereoisomer, tautomer, prodrug or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.Type: ApplicationFiled: March 1, 2013Publication date: September 26, 2013Applicants: Genentech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Mark Joseph Chicarelli, Rustam Ferdinand Garrey, John Gaudino, Jonas Grina, David A. Moreno, Peter J. Mohr, Li Ren, Jacob Schwarz, Huifen Chen, Kirk Robarge, Aihe Zhou
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Publication number: 20130253021Abstract: The present invention provides methods of making and using 5-(2-(indol-3-yl)-2-oxoethylidene)-3-phenyl-2-thioxothiazolidin-4-one derivatives having HIV-1 or JSP-1 inhibitory activity.Type: ApplicationFiled: March 22, 2013Publication date: September 26, 2013Applicants: The Johns Hopkins University, Southern Methodist UniversityInventors: Edward R. Biehl, Sukanta Kamila, Ted M. Dawson
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Publication number: 20130251732Abstract: Methods for inhibiting the motility or proliferation of premalignant and malignant cells are provided. Methods for treating a malignancy of the head and neck and for treating a malignancy of the lung are also provided.Type: ApplicationFiled: November 30, 2011Publication date: September 26, 2013Applicant: Institute For Cancer Research d/b/a The Research Institute of Fox Chase Cancer Center ("Fox ChaseInventors: Margie L. Clapper, Ekaterina G. Shatalova, Sibele Meireles
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Publication number: 20130253042Abstract: Oligonucleotide conjugates, where an oligonucleotide is covalently attached to an aromatic system, are provided. In particular embodiments the oligonucleotide is complementary to the RNA component of human telomerase and is covalently attached to a nucleobase via an optional linker. The conjugates inhibit telomerase enzyme activity.Type: ApplicationFiled: May 10, 2013Publication date: September 26, 2013Applicant: Geron CorporationInventors: Sergei M. Gryaznov, Krisztina Pongracz, Richard L. Tolman, Gregg B. Morin
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Publication number: 20130252966Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders such as neuropsychiatric disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130252920Abstract: Disclosed herein are pharmaceutical compositions that can include a thionucleotide analog for use in combination therapy with other agents. Also disclosed herein are methods of treating diseases and/or conditions with a pharmaceutical composition that can include a thionucleotide analog in combination therapy with other agents.Type: ApplicationFiled: March 12, 2013Publication date: September 26, 2013Applicants: VERTEX PHARMACEUTICALS INC., ALIOS BIOPHARMA, INC.Inventors: Lawrence M. Blatt, Leonid Beigelman, Hua Tan, Julian Alexander Symons, David Bernard Smith, Min Jiang, Tara Lynn Kieffer, Cornelis Arie Rijnbrand
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Publication number: 20130253005Abstract: Provided are small molecule inhibitors of ubiquitin specific protease 1 (USP1) activity and methods for their use in treating and characterizing cancers. The small molecule USP1 inhibitors of the invention are particularly useful in the treatment of cancers that are resistant to DNA cross-linking agents.Type: ApplicationFiled: April 29, 2011Publication date: September 26, 2013Applicants: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Alan D. D'Andrea, Gregory D. Cuny, Ross L. Stein, Marcie Glicksman, April Case, Jun Xian, David Wilson, Min Huang
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Publication number: 20130252967Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 26, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130243790Abstract: The present invention, in various embodiments, relates to methods of inhibiting NNMT production or activity in a cell, and methods of treating or preventing obesity or a related metabolic condition in a subject in need thereof, comprising administering a nicotinamide N-methyltransferase (NNMT) antagonist. The invention further provides methods of identifying NNMT antagonists useful for treating obesity and related metabolic disorders.Type: ApplicationFiled: November 18, 2011Publication date: September 19, 2013Inventors: Barbara B. Kahn, Qin Yang, Daniel Kraus
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Publication number: 20130244253Abstract: An object is to provide a compound capable of inhibiting activation of TGF-? receptors due to HCV, and a screening method for the compound. It has been found that a HCV-derived NS3 protease binds to type I TGF-? receptor, and this binding results in activation of TGF-? receptors. Moreover, binding sites between the NS3 protease and type I TGF-? receptor were identified, and it has been found that antibodies recognizing these binding sites inhibit activation of TGF-? receptors due to NS3 protease. Furthermore, it has been also found that screening for a compound capable of inhibiting activation of TGF-? receptors can be performed by using the inhibition of the binding between NS3 protease and type I TGF-? receptor or the like as an index.Type: ApplicationFiled: August 30, 2011Publication date: September 19, 2013Applicant: RIKENInventors: Soichi Kojima, Mitsuko Hara, Takehisa Matsumoto, Daisuke Takaya
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Publication number: 20130245032Abstract: According to the embodiments described herein, a tricyclic SUMOylation inhibitor compound is provided. In some embodiments, a method for inhibiting a SUMOylation enzyme in a cell is provided. Such a method may include administering a SUMOylation inhibitor compound to the cell. In some aspects, the SUMOylation enzyme is SUMO E1 or SUMO E2. In some aspects, the method may be used to inhibit a cancer cell in vitro (e.g., grown in culture) or in vivo (e.g., as part of a tumor in a subject). In other embodiments, a method for treating a cancer, degenerative diseases and viral infection is provided. Such a method may include administering an effective amount of a pharmaceutical composition to a subject having the cancer. The pharmaceutical composition may include a SUMOylation inhibitor compound. In some embodiments, the method for treating a disease may further comprise administering one or more DNA-damaging therapy in combination with administration of the pharmaceutical composition.Type: ApplicationFiled: May 9, 2013Publication date: September 19, 2013Applicants: Sanford-Burnham Medical Research Institute at Lake Nona, City of HopeInventors: Yuan Chen, Yi-Jia Li, Daniela Divlianska, Ekaterina Bobkova, Greg Roth, Jun PU, Pasha Khan
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Publication number: 20130245026Abstract: Provided herein are methods for treating or preventing head and neck squamous cell carcinoma, comprising administering an effective amount of a TOR kinase inhibitor to a patient having head and neck squamous cell carcinoma.Type: ApplicationFiled: March 14, 2013Publication date: September 19, 2013Applicant: SIGNAL PHARMACEUTICALS, LLCInventors: Shuichan Xu, Kristen Mae Hege, Heather Raymon, Lilly Loraine Wong
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Publication number: 20130245012Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: September 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130237555Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.Type: ApplicationFiled: February 26, 2013Publication date: September 12, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Vivekananda M. Vrudhula, Senliang Pan, Ramkumar Rajamani, John E. Macor, Joanne J. Bronson, Carolyn Diane Dzierba, Susheel Jethanand Nara, Maheswaran Sivasamban Karatholuvhu
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Publication number: 20130237516Abstract: The present invention relates to compounds useful as inhibitors of protein kinases, particularly of JAK family kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: ApplicationFiled: April 25, 2013Publication date: September 12, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc Farmer, Gabriel Martinez-Botella, Albert Pierce, Francesco Salituro, Jian Wang, Wannamaker W. Wannamaker, Tiansheng Wang
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Publication number: 20130237595Abstract: The invention provides compounds of Formula (I) and pharmaceutically acceptable salts thereof, wherein Ya, Yb, R1, R2, and G are as described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as inhibitors of bacterial RNA polymerase and as antibacterial agents.Type: ApplicationFiled: September 16, 2011Publication date: September 12, 2013Inventors: Richard H. Ebright, Yon W. Ebright
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Patent number: 8529882Abstract: The present invention relates to peptidomimetic compounds useful as protease inhibitors, particularly as serine protease inhibitors and more particularly as hepatitis C NS3 protease inhibitors; intermediates thereto; their preparation including novel stereoselective processes to intermediates. The invention is also directed to pharmaceutical compositions and to methods for using the compounds for inhibiting HCV protease or treating a patient suffering from an HCV infection or physiological condition related to the infection. Also provided are pharmaceutical combinations comprising, in addition to one or more HCV serine protease inhibitors, one or more interferons exhibiting anti-HCV activity and/or one or more compounds having anti HCV activity and a pharmaceutically acceptable carrier, and methods for treating or preventing a HCV infection in a patient using the compositions. The present invention is also directed to a kit or pharmaceutical pack for treating or preventing HCV infection in a patient.Type: GrantFiled: July 3, 2012Date of Patent: September 10, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert Edward Babine, Shu Hui Chen, Ivan Collado, Cristina Garcia-Paredes, John Irvin Glass, Ling Jin, Jason Eric Lamar, Raymond Samuel Parker, III, Nancy June Snyder, Xicheng David Sun, Deqi Guo, Yvonne Yee Mai Yip, Q. May Wang, Frantz Victor, Mark Joseph Tebbe, Robert B. Perni, Luc Farmer
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Publication number: 20130231348Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 9, 2011Publication date: September 5, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Publication number: 20130231356Abstract: Compounds that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3K?) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3K? plays a role in leukocyte function, using the compounds also are disclosed.Type: ApplicationFiled: February 12, 2013Publication date: September 5, 2013Applicant: ICOS CORPORATIONInventors: Edward A. KESICKI, Kerry W. FOWLER, Danwen HUANG, Hua Chee OOI, Amy OLIVER, Kamal Deep PURI, Fuqiang RUAN, Jennifer TREIBERG
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Publication number: 20130231340Abstract: The invention provides a method of inhibiting a TYK2 kinase, which method comprises bringing into contact with the TYK2 kinase an effective TYK2 kinase-inhibiting amount of a compound having the formula (0): or a salt or stereoisomer thereof. The invention also provides a novel subset of compounds within formula (0) as well as pharmaceutical compositions containing them and their use in medicine.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: SAREUM LIMITEDInventor: John Charles READER
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Publication number: 20130225527Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.Type: ApplicationFiled: March 15, 2013Publication date: August 29, 2013Applicant: ARIAD PHARMACEUTICALS, INC.Inventor: ARIAD PHARMACEUTICALS, INC.
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Publication number: 20130225620Abstract: Compounds having the formula I wherein A, Z, R1a, R1b, R2, R3, R4, R5, R6, R7, R9, R10, Ra, Rb and n are as defined herein are inhibitors of PAK1. Also disclosed are compositions and methods for treating cancer and hyperproliferative disorders.Type: ApplicationFiled: August 24, 2012Publication date: August 29, 2013Applicant: Genentech, Inc.Inventors: Ignacio Aliagas-Martin, James Crawford, Wendy Lee, Simon Mathieu, Joachim Rudolph
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Publication number: 20130224827Abstract: The activity of endothelial nitric oxide synthase (eNOS) was modulated by contact with an effective amount of a mitogen-activated protein (MAP) kinase, resulting in phosphorylation of S602, T46, and/or S58. Kinetics and stoichiometry are disclosed. The contact strongly reduced nitric oxide (NO) synthesis, and also inhibited the cytochrome c reductase activity of eNOS reductase domains. Three sites of phosphorylation were determined that matched the serine-proline (SP) and threonine-proline (TP) motifs of typical MAP kinase phosphorylation sites.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Inventors: John C. Salerno, Carol A. Chrestensen
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Publication number: 20130225579Abstract: Disclosed is a compound of formula I, a stereoisomer thereof, a cis-trans-isomer thereof, a tautomer thereof, or a mixture thereof, or a pharmaceutically acceptable salt thereof, a solvate thereof or a prodrug thereof, wherein R1, R2, R3 and R4 are each as defined in the present application.Type: ApplicationFiled: June 8, 2011Publication date: August 29, 2013Applicant: Tianjin Hemay Bio-Tech Co., Ltd.Inventors: Hesheng Zhang, Yingwei Chen, Qingchao He
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Publication number: 20130217613Abstract: Disclosed are compositions and methods for modulating Dpy-30 binding activity. The compositions may include peptides or peptidomimetics thereof that are related to RSP3 or Ash2L and that bind to Dpy-30.Type: ApplicationFiled: August 8, 2012Publication date: August 22, 2013Applicant: MARQUETTE UNIVERSITYInventors: Pinfen Yang, Priyanka Sivadas
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Publication number: 20130217617Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain pyruvamide compounds of the following formula (for convenience, collectively referred to herein as “PVA compounds”), which, inter alia, inhibit a dust mite Group 1 peptidase allergen (e.g., Der p 1, Der f 1, Eur m 1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit a dust mite Group 1 peptidase allergen, and in the treatment of diseases and disorders that are mediated by a dust mite Group 1 peptidase allergen; that are ameliorated by the inhibition of a dust mite Group 1 peptidase allergen; asthma; rhinitis; allergic conjunctivitis; atopic dermatitis; an allergic condition which is triggered by dust mites; an allergic condition which is triggered by a dust mite Group 1 peptidase allergen; and canine atopy.Type: ApplicationFiled: March 28, 2013Publication date: August 22, 2013Applicants: The University of Manchester, St George's Hospital Medical SchoolInventors: Clive Robinson, Jihui Zhang, David Ronald Garrod, Trevor Robert Perrior, Gary Karl Newton, Kerry Jenkins, Rebekah Elisabeth Key, Meriel Ruth Major, Mark Richard Stewart
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Publication number: 20130219533Abstract: In some aspects, the invention provides compositions and methods for inhibiting viral infection. In some aspects, the invention provides compositions and methods useful for identifying antiviral compounds.Type: ApplicationFiled: June 17, 2011Publication date: August 22, 2013Applicant: WHITEHEAD INSTITUTE FOR BIOMEDICAL RESEARCHInventors: Thijn R. Brummelkamp, Jan E. Carette
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Publication number: 20130210831Abstract: The present disclosure provides pyrrolopyrimidine compounds and methods of use therefor. For example, the disclosure provides certain pyrrolopyrimidine compounds capable of inhibiting JAK kinases. The disclosure further provides the pharmaceutical compositions containing these pyrrolopyrimidine compounds, and use of these pyrrolopyrimidine compounds in the treatment of disorders or diseases, such as inflammatory diseases and cancer.Type: ApplicationFiled: August 18, 2011Publication date: August 15, 2013Inventors: Wei-Guo Su, Wei Deng, Jinshui Li, Jianguo Ji
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Publication number: 20130210711Abstract: The invention relates to a compound of the general structure (I), where R is a hydrogen atom (II) or an unsubstituted, monosubstituted or polysubstituted C1-C20-alkyl, wherein the alkyl is straight, branched, cyclic and/or partially unsaturated, or an unsubstituted, monosubstituted or polysubstituted phenyl group.Type: ApplicationFiled: April 30, 2010Publication date: August 15, 2013Applicant: GEOMAR Helmholtz-Zentrum fur Ozeanforschung KielInventors: Johannes Imhoff, Inga Knopf-Kajahn, Gerhard Lang, Jutta Wiese, Arne Peters
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Publication number: 20130210845Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.Type: ApplicationFiled: July 22, 2011Publication date: August 15, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Daniel J. Finley, Randall W. King, Byung-Hoon Lee, Min J. Lee, Timothy C. Gahman
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Publication number: 20130210883Abstract: The invention provides a compound of formula (I) as defined herein that is useful in the treatment and prevention of a disorder such as cachexia, stroke, atherosclerosis, coronary artery disease, or diabetes and disorders and conditions associated therewith. The invention also provides a method of screening for lipase inhibitors using a compound of formula (I) and determining its lipase inhibitory activity. activity.Type: ApplicationFiled: March 15, 2013Publication date: August 15, 2013Inventors: Johannes Grillari, Rolf Breinbauer, Martina Schweiger, Matthias Romauch, Robert Zimmermann, Nicole Mayer, Elisabeth Schraml, Klaus Fortschegger, Regina Grillari
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Publication number: 20130210810Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 18, 2012Publication date: August 15, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: Rigel Pharmaceuticals, Inc.
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Publication number: 20130209487Abstract: The invention includes compositions and methods for regulating p110 delta in an avian species. The invention includes inhibiting p110 delta, a component of p110 delta signaling pathway, or any combination thereof in an avian species as an anti-viral therapeutic approach for treating virus infection.Type: ApplicationFiled: June 30, 2011Publication date: August 15, 2013Applicant: Philadelphia Health & Education Corporation d/b/a Drexel University College of MedicineInventor: Peter D. Katsikis
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Publication number: 20130203706Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of inhibiting or reducing the activity of HCV polymerase in a subject or in a biological in vitro sample comprises administering to the subject or to the sample a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 21, 2012Publication date: August 8, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130203755Abstract: Provided are compounds having an inhibitory effect on kinases including Mixed Lineage Kinases. Also provided are pharmaceutical compositions, methods of preparing the compounds, synthetic intermediates, and methods of using the compounds, independently or in combination with other therapeutic agents, for treating diseases and conditions that are affected by Mixed Lineage Kinase inhibition. Also provided are methods of treatment of neuropsychiatric disorders that comprise the inhibition of Mixed Lineage Kinases.Type: ApplicationFiled: May 24, 2011Publication date: August 8, 2013Applicant: UNIVERSITY OF ROCHESTERInventors: Harris A. Gelbard, Stephen Dewhurst, Val S. Goodfellow, Torsten Wiemann, Satheesh Babu Ravula, Colin J. Loweth