Enzyme Inactivation By Chemical Treatment Patents (Class 435/184)
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Publication number: 20140031361Abstract: The present invention is directed to compounds of formula I-II and pharmaceutically acceptable tautomers, salts, or stereoisomers thereof which are inhibitors of syk and/or JAK kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition syk and/or JAK kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by syk and/or JAK kinase activity, such as undesired thrombosis and Non Hodgkin's Lymphoma.Type: ApplicationFiled: June 13, 2013Publication date: January 30, 2014Inventors: Shawn M. Bauer, Zhaozhong J. Jia, Yonghong Song, Qing Xu, Mukund Mehrotra, Jack W. Rose, Wolin Huang, Chandrasekar Venkataramani, Anjali Pandey
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Publication number: 20140031354Abstract: The present invention relates to compounds of Formula I: as well as pharmaceutically acceptable salts, hydrates, isomers, or solvates thereof, wherein the variables are described herein. The present invention further relates to pharmaceutical compositions which comprise the compounds of Formula I, and to methods for inhibiting protein kinase and methods of treating diseases, such as cancers, inflammation.Type: ApplicationFiled: July 30, 2012Publication date: January 30, 2014Applicant: Astar Biotech LLCInventors: Chunrong YU, Haihong Huang, Dongfeng Zhang, Peng Li
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Publication number: 20140031358Abstract: The present invention discloses compounds of formula (I), or pharmaceutically acceptable salts or prodrugs thereof, which inhibit the poly(ADP-ribose) polymerases (PARP) and therefore are useful for treating diseases, disorders, and conditions related to PARP. The present invention also discloses pharmaceutical compositions comprising a compound of formula (I), and methods of using such compounds to inhibit PARP enzymes, and to treat diseases, disorders, and conditions related to PARP.Type: ApplicationFiled: March 12, 2012Publication date: January 30, 2014Applicant: Eternity Bioscience Inc.Inventors: Dong Liu, Minsheng Zhang, Kan He, Lianshan Zhang
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Publication number: 20140031344Abstract: The present invention provides compounds that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases, skin disorders, myeloid proliferative disorders, cancer, and other diseases.Type: ApplicationFiled: September 20, 2013Publication date: January 30, 2014Applicant: INCYTE CORPORATIONInventors: Argyrios G. Arvanitis, James D. Rodgers, Andrew P. Combs, Richard B. Sparks, Darius J. Robinson, Jordan S. Fridman, Krishna Vaddi
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Publication number: 20140024583Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: July 15, 2013Publication date: January 23, 2014Inventors: Natalie Dales, Julia Fonarev, Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Zaihui Zhang
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Publication number: 20140024578Abstract: In general, the invention relates to methods of synthesizing AbA derivatives that are useful for treating infection and amenable to further chemical elaboration. These novel methods are scalable for industrial production and employ safer, simpler, and more efficient process conditions. Furthermore, the invention also provides novel compounds and intermediates useful for implementing the methods described herein and/or for the treatment of infection.Type: ApplicationFiled: March 23, 2012Publication date: January 23, 2014Applicant: AureoGen Biosciences ,Inc.Inventors: Peter Wuts, Ake P. Elhammer
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Publication number: 20140024685Abstract: Compositions that are effective in inhibiting gamma-glutamyl transpeptidase are disclosed. Methods of producing and using these compositions are also disclosed.Type: ApplicationFiled: August 23, 2013Publication date: January 23, 2014Applicants: Ohio State Innovation Foundation, The Board of Regents of the University of OklahomaInventors: Marie H. Hanigan, Pui Kai Li
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Publication number: 20140018361Abstract: The present invention provides furano- and pyrrolo-pyrimidine and pyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140018343Abstract: The present invention provides arylo-fused thienopyrimidine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Donna L. Romero, Shaughnessy Robinson, Matthew David Wessel, Jeremy Robert Greenwood
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Publication number: 20140018357Abstract: The present invention provides thienopyridine compounds, compositions thereof, and methods of using the same.Type: ApplicationFiled: July 11, 2013Publication date: January 16, 2014Inventors: Geraldine C. Harriman, Ronald T. Wester, Donna L. Romero, Craig E. Masse, Shaughnessy Robinson, Jeremy Robert Greenwood
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Publication number: 20140018318Abstract: The present invention provides inhibitors of a wide variety of serine hydrolase enzymes. The inhibitors of the present invention are N1- and N2-carbamoyl-1,2,3-triazole compounds such as those of Formula (I): in which N1, N2, and N3 are the nitrogen atoms at positions 1, 2, and 3, respectively, of the triazole ring, and R4, R5, R6 and R7 in Formula (I) are as described herein. Methods of inhibiting serine hydrolase enzymes and methods of preparing carbamoyl-1,2,3-triazole compounds also are described.Type: ApplicationFiled: April 5, 2012Publication date: January 16, 2014Applicant: The Scipps Research InstituteInventors: Benjamin Cravatt, Alexander Adibekian, Katsunori Tsuboi, Ku-Lung Hsu
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Patent number: 8629135Abstract: A class of compounds useful in pharmaceutical compositions and methods for treating or preventing cancer is described. The compounds' ability to inhibit RET kinase is quantified, i.e., their respective RET IC50 and EC50 values are described. One such compound, known as cyclobenzaprine and herein as SW-01, has been identified as RET-specific with an IC50 of 300 nM. SW-01 inhibits RET autophosphorylation and blocks the growth and transformation of thyroid cancer cell lines. It has been further tested in pancreatic cancer, breast cancer, and SCLC cell lines. The compounds show utility for inhibition of survival and proliferation of tumor cells.Type: GrantFiled: July 14, 2009Date of Patent: January 14, 2014Assignee: Queen's University at KingstonInventors: Taranjit S. Gujral, Lois M. Mulligan, Vinay K. Singh
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Publication number: 20140011806Abstract: This invention describes substituted pyrazole derivatives of Formula I and methods of making and using the compounds. These compounds have utility in the treatment of conditions or diseases in which modification of the activity of ERK would have a positive therapeutic outcome, for instance various cancers, psoriasis and actinic keratosis.Type: ApplicationFiled: January 3, 2012Publication date: January 9, 2014Applicant: KINENTIA BIOSCIENCES LLCInventors: David Fairfax, Russell Joseph Deorazio
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Publication number: 20140011810Abstract: Provided are compounds and methods for treating or preventing kinase-mediated disorders therewith.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: Gatekeeper Pharmaceuticals, Inc.Inventors: Nathanael S. Gray, Wenjun Zhou
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Publication number: 20140011819Abstract: The present invention relates to selective inhibitors of PI3K delta protein kinases, methods of preparing them, pharmaceutical compositions containing them and methods of treatment and/or prevention of kinase mediated diseases or disorders with them.Type: ApplicationFiled: July 2, 2013Publication date: January 9, 2014Inventors: Swaroop Kumar V.S. VAKKALANKA, Meyyappan Muthuppalaniappan, Dhanapalan Nagarathnam
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Publication number: 20140010784Abstract: The present invention relates to peptidomimetic compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention.Type: ApplicationFiled: May 29, 2013Publication date: January 9, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Luc J. Farmer, Janos Pitlik, Robert B. Perni, John H. van Drie, JR.
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Publication number: 20140010842Abstract: The subject matter disclosed herein pertains to the modulation of a bacterial invasion switch and the subsequent use of the bacterium to vaccinate an organism. In one embodiment, the bacterial invasion switch is modulated by changing the proteolysis of ExoR protein. In another embodiment, a mutated bacterium produces a mutant ExoR protein that resists proteolysis.Type: ApplicationFiled: May 28, 2013Publication date: January 9, 2014Inventors: Haiping Cheng, Shari Walcott, Haiyang Lu, Li Luo, Menghua Yang
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Publication number: 20140010799Abstract: The present invention relates to compositions and methods for the diagnosis and treatment of obesity and related metabolic disorders. The invention provides isolated nucleic acids molecules, designated DGAT2 family member nucleic acid molecules, which encode diacylglycerol acyltransferase family members. The invention also provides recombinant expression vectors containing DGAT2 family member nucleic acid molecules, host cells into which the expression vectors have been introduced, and nonhuman transgenic animals in which a DGAT2 family member gene has been introduced or disrupted. The invention still further provides isolated DGAT2 family member proteins, fusion proteins, antigenic peptides and anti-DGAT2 family member antibodies. Methods of use of the provided DGAT2 family member compositions for screening, diagnostic and therapeutic methods in connection with obesity disorders are also disclosed.Type: ApplicationFiled: February 14, 2013Publication date: January 9, 2014Applicant: Millenium Pharmaceuticals, Inc.Inventor: Millenium Pharmaceuticals, Inc.
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Publication number: 20140011768Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.Type: ApplicationFiled: June 11, 2013Publication date: January 9, 2014Inventors: Tsutomu Akama, Yong-Kang Zhang, Charles Z. Ding, Jacob J. Plattner, Kirk R. Maples, Yvonne Freund, Virginia Sanders, Yi Xia, Stephen J. Baker, James A. Nieman, Xiaosong Lu, Marcelo Sales, Rashmi Sharma, Rajeshwar Singh, Robert Jacobs, Daitao Chen, Michael Richard Kevin Alley
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Publication number: 20140011254Abstract: A method for reducing nuclease activity in a subtilisin solution obtained from a fermentation broth comprising a) adjusting the pH of the subtilisin solution to a pH in the range of from pH 8.5 to pH 10.5; b) adding a polyol; c) adjusting the temperature of the subtilisin solution to a temperature in the range of from 50° C. to 80° C.; whereby the nuclease activity is reduced to less than 5% of the initial value and the subtilisin activity is maintained at more than 80% of the initial value.Type: ApplicationFiled: September 11, 2013Publication date: January 9, 2014Applicant: NOVOZYMES A/SInventors: Kim Uhre Hansen, Peter Rahbek Oestergaard
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Publication number: 20140011770Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: ApplicationFiled: September 10, 2013Publication date: January 9, 2014Applicant: Rigel Pharmaceuticals, Inc.Inventors: Yan Chen, Vanessa Taylor, Hui Li, Rajinder Singh
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Publication number: 20140005180Abstract: The present invention relates to phenyl amino pyrimidine compounds which are inhibitors of protein kinases including JAK kinases. In particular the compounds are selective for JAK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.Type: ApplicationFiled: June 7, 2013Publication date: January 2, 2014Inventors: Christopher John BURNS, Andrew Craig DONOHUE, John Thomas FEUTRILL, Thao Lien Thi NGUYEN, Andrew Frederick WILKS, Jun ZENG
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Publication number: 20140004590Abstract: The invention provides methods to inhibit the replication of a flavivirus, methods of inhibiting the guanosine triphosphate (GTP)-binding and guanylyltransferase activity of a flavivirus RNA capping enzyme, and methods of treating a subject infected with a flavivirus. The methods can include contacting a flavivirus with an effective amount of a thioxothiazolidine compound described herein, or a derivative thereof, such as a compound of Formula (I).Type: ApplicationFiled: May 31, 2013Publication date: January 2, 2014Inventors: Brian J. GEISS, Susan M. KEENAN, Hillary Jo BEEK
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Publication number: 20140005225Abstract: A method of reducing or inhibiting kinase activity of C-KIT in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to C-KIT using a compound of the present invention: or a solvate, hydrate, tautomer or pharmaceutically acceptable salt thereof. The present invention is further directed to methods for treating conditions such as cancers and other cell proliferative disorders.Type: ApplicationFiled: September 6, 2013Publication date: January 2, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Sanath K. Meegalla, M. Jonathan Rudolph, Mark J. Wall, Kenneth J. Wilson, Renee Louise Desjarlais, Carl M. Manthey, Christopher J. Molloy
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Publication number: 20140005166Abstract: The present invention provides piperidinylcyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I, as defined herein, as well as their compositions and methods of use, that modulate the activity of Janus kinases (JAKs) and are useful in the treatment of diseases related to the activity of JAKs including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.Type: ApplicationFiled: May 17, 2013Publication date: January 2, 2014Applicant: Incyte CorporationInventors: JAMES D. RODGERS, Stacey Shepard, Wenyu Zhu, Lixin Shao, Joseph Glenn
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Publication number: 20140005119Abstract: A method of inhibiting the activity, signaling, and/or function of a p110? mutant protein in a cancer cell expressing the p110? mutant protein includes administering to the cancer cell an amount of a therapeutic agent effective to inhibit binding of the p110? mutant protein to IRS1 in the cell.Type: ApplicationFiled: June 28, 2013Publication date: January 2, 2014Inventors: Zhengne Wang, Yujun Hao, Chao Wang, Weiping Zheng
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Publication number: 20130345224Abstract: The present invention relates to imidazo[1,2-b][1,2,4]triazines that are inhibitors of c-Met and are useful in the treatment of c-Met associated diseases including cancer.Type: ApplicationFiled: June 12, 2013Publication date: December 26, 2013Applicant: INCYTE CORPORATIONInventors: Jincong Zhuo, Chunhong He, Wenqing Yao
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Publication number: 20130345214Abstract: The disclosure provides bisindole suitable for inhibiting lipoxygenases or A?-formation, and treating associated diseases, such as Alzheimer's disease. The bisindoles are indolo[2,3-b]carbazole derivatives, and may be administered to a patient as part of a pharmaceutical formulation.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: SRI International, Inc.Inventor: Ling Jong
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Publication number: 20130344031Abstract: Compounds represented by formula (Ia) or (Ib) and wherein R and R1 are as defined in the description, and pharmaceutically acceptable salts thereof, are disclosed; the said compounds are useful in the treatment of cell cycle proliferative disorders, e.g. cancer, associated with an altered cell cycle dependent kinase activity.Type: ApplicationFiled: August 27, 2013Publication date: December 26, 2013Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Raffaella Amici, Daniele Fancelli, Marcella Nesi, Paolo Orsini, Fabrizio Orzi, Patrick Roussel, Anna Vulpetti, Paolo Pevarello
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Publication number: 20130344563Abstract: A class of anionic oligomers and polymers that function for inhibition of nucleases, particularly RNase. Specific inhibitors include mixtures of oligomers of vinyl sulfate. Methods for inhibition or inactivation of one or more nucleases in vitro which comprises the step of contacting the one or more nucleases in a biological medium with one or more of the anionic oligomeric or polymeric inhibitors of this invention. Kits for carrying out a biological procedure, biological reaction and/or a biological assay containing one or more inhibitors of this invention. The use of oligomers and/or polymers of this invention as additives in buffers or reagents. The inhibitors of the invention can also be attached to surfaces to provide for removal of nucleases from media, solutions or other liquids in contact with the solid.Type: ApplicationFiled: June 10, 2013Publication date: December 26, 2013Applicant: WISCONSIN ALUMNI RESEARCH FOUNDATIONInventors: Ronald T. RAINES, Bryan D. Smith, Matthew B. Soellner, David M. Lynn
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Publication number: 20130345192Abstract: The present invention provides compounds useful as inhibitors of Tec family kinases, compositions thereof, and methods of using the same.Type: ApplicationFiled: October 28, 2011Publication date: December 26, 2013Applicants: SUNESIS PHARMACEUTICALS, INC., BIOGEN IDEC MA INC.Inventors: Brian T. Hopkins, Daniel Scott, Patrick Conlon, Tracy J. Jenkins, Noel Powell, Bing Guan, Julio H. Cuervo, Deping Wang, Art Taveras
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Publication number: 20130345242Abstract: This invention relates to compounds that inhibit E1 activating enzymes, pharmaceutical compositions comprising the compounds, and methods of using the compounds. The compounds are useful for treating disorders, particularly cell proliferation disorders, including cancers, inflammatory and neurodegenerative disorders; and inflammation associated with infection and cachexia.Type: ApplicationFiled: June 6, 2013Publication date: December 26, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventors: Christopher F. Claiborne, Stephen Critchley, Courtney A. Cullis, Steven P. Langston, Hirotake Mizutani, Edward J. Olhava, Stephane Peluso, Irache Visiers, Stepan Vyskocil, Gabriel S. Weatherhead
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Publication number: 20130345215Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof, wherein Q, R1 and R2 are as defined herein. The compounds of formula I are useful in the treatment of cancer.Type: ApplicationFiled: June 6, 2013Publication date: December 26, 2013Inventors: Jianwen Feng, Nancy-Ellen Haynes, Johannes Cornelius Hermann, Kyungjin Kim, Jin-Jun Liu, Nathan Robert Scott, Lin Yi, Mark Edward Zak, Guiling Zhao
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Publication number: 20130345227Abstract: The present invention relates to novel pyrido[2,3-b]pyrazine derivatives of formula (I) and to the use of such compounds in which the inhibition, regulation and/or modulation of signal transduction by ATP consuming proteins like kinases plays a role, particularly to inhibitors of TGF-beta receptor kinases, and to the use of such compounds for the treatment of kinase-induced diseases, in particular for the treatment of tumors.Type: ApplicationFiled: February 13, 2012Publication date: December 26, 2013Applicant: MERCK PATENT GMBHInventors: Dieter Dorsch, Alfred Jonczyk, Guenter Hoelzemann, Christiane Amendt, Frank Zenke
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Publication number: 20130345197Abstract: The present invention relates to inhibitors of protein kinases. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: June 3, 2013Publication date: December 26, 2013Applicant: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Luc Farmer, Randy Bethiel, Edmund Harrington, Jeremy Green, John Court, Jon Come, David Lauffer, Alex Aronov, Hayley Binch, Dean Boyall, Jean-Damien Charrier, Simon Everitt, Damien Fraysse, Michael Mortimore, Francoise Pierard, Daniel Robinson, Jian Wang, Joanne Pinder, Tiansheng Wang, Albert Pierce
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Publication number: 20130345267Abstract: The present invention relates to a method for identifying compounds that modulate the activity of p300/CBP. Compounds of the invention are identified by designing or screening for a compound which binds to at least one amino acid residue of the newly identified lysine-CoA inhibitor binding site, L1 loop, electronegative pocket, or electronegative groove of the HAT domain of p300/CBP and testing the compound for its ability to modulate the activity of p300/CBP. Compositions and methods for preventing or treating diseases or disorders associated with p300/CBP are also provided as is a method for producing a semi-synthetic HAT domain.Type: ApplicationFiled: May 30, 2013Publication date: December 26, 2013Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
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Publication number: 20130345216Abstract: Chemical entities that modulate PI3 kinase activity, pharmaceutical compositions containing the chemical entities, and methods of using these chemical entities for treating diseases and conditions associated with PI3 kinase activity are described herein.Type: ApplicationFiled: August 20, 2013Publication date: December 26, 2013Applicant: INTELLIKINE LLCInventors: Pingda Ren, Yi Liu, Troy Edward Wilson, Liansheng Li, Katrina Chan, Christian Rommel
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Publication number: 20130336883Abstract: The invention provides compounds that bind to deoxycytidine kinase (dCK) and compositions including pharmaceutically acceptable compositions containing the compounds. The compounds are useful in treating diseases and disorders where dCK activity is implicated such as cancer and immune disorders. The compounds also find use in clinical methodologies including positron emission tomography (PET) imaging.Type: ApplicationFiled: March 8, 2012Publication date: December 19, 2013Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Caius G. Radu, Hsiang-I Liao, Nagichettiar Satyamurthy, Johannes Czernin, Jennifer M. Murphy, David A. Nathanson
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Publication number: 20130338196Abstract: Compounds are disclosed that are effective in inhibition of fatty acid amide hydrolase, an enzyme responsible for catabolism of endogenous cannabinoids such as anandamide. The compounds are useful as analgesic compounds and as sleep-inducing compounds, that can be orally administered, and that can have a relatively long duration of effect. Methods of preparation of the compounds are also provided. The compounds are conformationally constrained analogs of heterocyclylketones such as oxazolylketones.Type: ApplicationFiled: February 3, 2012Publication date: December 19, 2013Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20130338140Abstract: Compounds having the formula I wherein Z, Z1 Z2 Z, R3a, R3b and Rb and as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.Type: ApplicationFiled: February 28, 2012Publication date: December 19, 2013Applicants: Genetech, Inc., Array BioPharma Inc.Inventors: James F. Blake, Huifen Chen, Mark Joseph Chcarelli, Jason Demeese, Rustam Garrey, John J. Gaudino, Robert J. Kaus, Gabrielle R. Kolakowski, Allison L. Marlow, Peter J. Mohr, Li Ren, Jacob Schwartz, Christopher S. Siedem, Allen A. Thomas, Eli Wallace, Steven Mark Wenglowsky
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Publication number: 20130338134Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.Type: ApplicationFiled: June 12, 2013Publication date: December 19, 2013Inventors: Liangxing Wu, Colin Zhang, Chunhong He, Yaping Sun, Liang Lu, Ding-Quan Qian, Meizhong Xu, Jincong Zhuo, Wenqing Yao
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Publication number: 20130338153Abstract: Provided herein are PAK inhibitors and methods of utilizing PAK inhibitors for the treatment of CNS disorders.Type: ApplicationFiled: June 10, 2011Publication date: December 19, 2013Applicant: AFRAXIS, INC.Inventors: David Campbell, Sergio G. Duron, Benedikt Vollrath, Warren Wade
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Patent number: 8609638Abstract: The invention provides compounds, compositions, and methods for studying the Rohmer pathway and for treating bacterial infections or parasitic infections. The parasitic infection can be a protozoan infection, such as malaria. The compounds and compositions can also be used as antibiotics, for example, to kill bacteria or parasites, or to inhibit bacterial or parasite growth. The invention further provides inhibitors of isoprenoid biosynthesis enzymes, and methods of inhibiting the activity of isoprenoid biosynthesis enzymes. The compounds can be, for example, alkynes or allenes that bind to a unique Fe of an Fe4S4 cluster of an isoprenoid biosynthesis enzyme.Type: GrantFiled: October 8, 2010Date of Patent: December 17, 2013Assignee: The Board of Trustees of the University of IllinoisInventors: Eric Oldfield, Ke Wang, Weixue Wang, Yonghui Zhang
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Publication number: 20130330734Abstract: A hot start enzyme composition is described that includes a hot start nuclease, a nucleic acid polymerase, and a substantially double-stranded oligonucleotide that inhibits the catalytic activity of the nucleic acid polymerase at temperatures lower than the melting temperature of the oligonucleotide.Type: ApplicationFiled: June 11, 2013Publication date: December 12, 2013Inventors: Win D. CHEUNG, Jason A. OPDYKE
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Publication number: 20130331375Abstract: There are provided compounds of the formula (I) wherein Q, R1 and R2 are defined herein. The compounds have activity as anticancer agents.Type: ApplicationFiled: June 6, 2013Publication date: December 12, 2013Inventors: Nancy-Ellen Haynes, Johannes Hermann, Kyungjin Kim, Nathan Robert Scott, Lin Yi, Mark Zak
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Publication number: 20130330371Abstract: In one aspect, the invention relates to an immunogenic composition that includes a mutant Clostridium difficile toxin A and/or a mutant Clostridium difficile toxin B. Each mutant toxin includes a glucosyltransferase domain having at least one mutation and a cysteine protease domain having at least one mutation, relative to the corresponding wild-type C. difficile toxin. The mutant toxins may further include at least one amino acid that is chemically crosslinked. In another aspect, the invention relates to antibodies or binding fragments thereof that binds to said immunogenic compositions. In further aspects, the invention relates to isolated nucleotide sequences that encode any of the foregoing, and methods of use of any of the foregoing compositions.Type: ApplicationFiled: August 19, 2013Publication date: December 12, 2013Applicant: WYETH LLCInventors: Annaliesa Sybil Anderson, Maninder K. Sidhu, Robert G. K. Donald, Kathrin Ute Jansen, Narender Kumar Kalyan, Justin Keith Moran, Mark E. Ruppen, Michael James Flint
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Publication number: 20130331432Abstract: A novel pathway in cancer cell metabolism is identified. Targeting of any gene, protein, or enzyme that modulates activity or flux through this pathway, including, but not limited to IDH1, isocitrate dehydrogenase 2 (IDH2), aconitase 1 (ACO1), aconitase 2 (ACO2), glutaminase (GLS), glutamate dehydrogenase (GDH) and transaminase, provides effective means of inhibiting tumor growth.Type: ApplicationFiled: July 8, 2011Publication date: December 12, 2013Applicants: The General Hospital Corporation d/b/a Massachusetts General Hospital, Massachusetts Institute Of TechnologyInventors: Gregory Stephanopoulos, Christian M. Metallo, Joanne K. Kelleher, Othon Iliopoulos, Paulo Alexandre da Costa Gameiro Guerreiro
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Publication number: 20130331392Abstract: The invention provides cycloalkyl guanidine compounds that inhibit F1F0-ATPase, and methods of using cyclalkyl guanidine compounds as therapeutic agents in therapy, such as treating an immune disorder, inflammatory condition, or cancer.Type: ApplicationFiled: December 8, 2011Publication date: December 12, 2013Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood, Chad A. Van Huis
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Publication number: 20130331398Abstract: The instant invention is based, at least in part, on a newly-identified proteasome-independent signaling function of ubiquitinated PSD-95. Mdm2 inhibitors, Mdm4 inhibitors, PSD-95 inhibitors, and/or enantiomers and/or derivatives thereof de-crease endocytosis via preventing PSD-95 ubiquitination, and thereby increase AMPAR, NMDAR, D1 dopamine receptor surface expression in response to a given stimulus (e.g., NMDA, A?). Accordingly, the invention provides methods for modulating AM-PARS, NMDARs, or D1 dopamine receptors in a neuronal cell by contacting the neuronal cell with an Mdm2 and/or Mdm4 inhibitor or PSD-95 inhibitor and/or enantiomers and/or derivatives thereof. Mdm2 and/or Mdm4 inhibitors decrease the enzymatic activity of the respective proteins, and/or interactions with their respective substrates. Mdm2 and Mdm4 inhibitors and/or PSD-95 inhibitors of the invention are contemplated for use in the treatment of neurological disorders, neurodevelopmental disorders, and psychiatric disorders.Type: ApplicationFiled: November 14, 2011Publication date: December 12, 2013Applicant: UNIVERSITY OF MASSACHUSETTSInventors: Maria Morabito, Michael Bianchetta
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Publication number: 20130331374Abstract: 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: April 4, 2013Publication date: December 12, 2013Inventor: Rigel Pharmaceuticals, Inc.