Enzyme Inactivation By Chemical Treatment Patents (Class 435/184)
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Publication number: 20140206677Abstract: Compounds of formula (I), pharmaceutically acceptable salts thereof, and uses of the compounds of formula (I) for treating bacterial infections are disclosed.Type: ApplicationFiled: January 21, 2014Publication date: July 24, 2014Applicant: AstraZeneca ABInventors: Gregory Steven BASARAB, Madhusudhan Reddy GOWRAVARAM, Sheila Irene HAUCK, Fei ZHOU
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Publication number: 20140206738Abstract: A compound of formula (I) as defined herein is useful in the treatment and prevention of a disorder such as cachexia, stroke, atherosclerosis, coronary artery disease, and diabetes and pharmaceutical compositions of the same. Also, a method of screening for lipase inhibitors using a compound of formula (I) and determining its lipase inhibitory activity. The method includes in vitro assays of compounds using ATGL and/or HSL, and cellular assays wherein inhibition is followed by observing indicators of efficacy. Also, methods for treatment or prevention of a condition involving cachexia, stroke, artherosclerosis, coronary artery disease, diabetes, preferably diabetes type II by administering a pharmaceutical composition comprising an agent which is able to inhibit ATGL. Also contemplated herein, are compositions comprising one or more ATGL-inhibiting agents optionally in combination with one or more lipase inhibitors or inhibitors of inflammatory cytokines.Type: ApplicationFiled: January 23, 2014Publication date: July 24, 2014Applicants: Karl-Franzens-Universität Graz, Technische Universität GrazInventors: Martina SCHWEIGER, Matthias ROMAUCH, Robert ZIMMERMANN, Nicole MAYER, Rolf BREINBAUER
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Patent number: 8785402Abstract: Methods of diagnosing Helicobacter pylori infection or associated conditions are based in part on the correlation of the presence of a ?-L-fucosidase 2 marker with the infection. Methods and compositions for treating or preventing Helicobacter pylori infection or associated conditions are based in part on administering an ?-L-fucosidase 2 inhibitor to an infected subject or a subject at risk of developing the infection.Type: GrantFiled: August 2, 2010Date of Patent: July 22, 2014Assignee: Academia SinicaInventors: Chun-Hung Lin, Ta-Wei Liu
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Publication number: 20140200198Abstract: Compounds, pharmaceutical formulations, and methods of treating anti-inflammatory conditions and/or helminth-associated diseases are disclosed.Type: ApplicationFiled: December 18, 2013Publication date: July 17, 2014Applicant: ANACOR PHARMACEUTICALS, INC.Inventors: Kurt Jarnagin, Tsutomu Akama
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Publication number: 20140200245Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: March 14, 2014Publication date: July 17, 2014Applicant: Janssen Pharmaceutica NVInventors: Carl R. ILLIG, Jinsheng CHEN, Renee Louise DESJARLAIS, Kenneth WILSON
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Publication number: 20140200227Abstract: The present disclosure describes thiazole and pyridine carboxamide derivatives, their compositions and methods of use. The compounds inhibit the activity of the Pim kinases and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Chu-Biao Xue, Yun-Long Li, Hao Geng, Jun Pan, Anlai Wang, Ke Zhang, Wenqing Yao, Fenglei Zhang, Jincong Zhuo
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Publication number: 20140200216Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.Type: ApplicationFiled: January 14, 2014Publication date: July 17, 2014Applicant: INCYTE CORPORATIONInventors: Yun-Long Li, David M. Burns, Hao Feng, Chu-Biao Xue, Anlai Wang, Jun Pan
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Publication number: 20140194406Abstract: The present invention relates to alkynyl substituted pyrimidinyl-pyrrole compounds which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Jak and/or Src family kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: July 18, 2012Publication date: July 10, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Jay Aaron Bertrand, Paola Gnocchi, Ilaria Motto, Marcella Nesi, Achille Panzeri, Paola Vianello
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Publication number: 20140193463Abstract: A method for inhibiting dipeptidyl-peptidase IV is provided and includes administering a peptide to the dipeptidyl-peptidase IV, in which the peptide is isolated from a gelatin hydrolysate produced by enzymatic digestion with alcalase (ALA), bromelain (BRO), and flavourzyme (FLA).Type: ApplicationFiled: January 4, 2013Publication date: July 10, 2014Applicant: CHINA MEDICAL UNIVERSITYInventors: Kuo-Chiang HSU, Kit-Pan HO, Shih-Li HUANG, Chia-Ling JAO
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Publication number: 20140194449Abstract: Provided herein is an optically active pyrozolylaminoquinazaline, and pharmaceutical compositions thereof. Also provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a JAK-mediated condition, disorder, or disease. Further provided herein is a method for treating, preventing, or ameliorating one or more symptoms of a proliferative disease, inflammatory disease, or renal disease.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicant: Ambit Biosciences Corp.Inventors: Mark W. HOLLADAY, Eduardo SETTI
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Publication number: 20140194383Abstract: 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: April 9, 2012Publication date: July 10, 2014Applicants: Cornell University, Coferon, Inc., Purdue Research FoundationInventors: Francis Barany, Maneesh Pingle, Donald E. Bergstrom, Sarah F. Giardina, Lee Daniel Arnold
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Publication number: 20140193339Abstract: A new family of analogues of NADP+ or NADPH, their preparation and their application in therapeutics.Type: ApplicationFiled: June 19, 2012Publication date: July 10, 2014Inventors: Anny Slama-Schwok, Jean-Luc Boucher, Yun Xu-Li, Eric Deprez, Etienne Henry, Chantal Dessy, Olivier Feron, Bogdan Tarus
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Publication number: 20140194469Abstract: Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.Type: ApplicationFiled: December 5, 2013Publication date: July 10, 2014Applicant: Quanticel Pharmaceuticals, Inc.Inventors: Zhe Nie, Jeffrey Alan Stafford, James Marvin Veal, Michael Brennen Wallace
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Publication number: 20140194495Abstract: The present invention concerns groups of compounds derived from tunicates of the Synoicum species, as well as to pharmaceutical compositions comprising these compounds, and uses thereof. Extracts from tunicates show selective toxicity against several different cancer cell lines in the NCI 60 cell line panel. These compounds are useful in the effective treatment of cancers, particularly malignant melanomas, colon cancer, and renal cancer cell lines.Type: ApplicationFiled: March 11, 2014Publication date: July 10, 2014Applicants: THE UAB RESEARCH FOUNDATION, UNIVERSITY OF SOUTH FLORIDAInventors: BILL J. BAKER, THUSHARA DIYABALANAGE, JAMES B. MCCLINTOCK, CHARLES D. AMSLER
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Patent number: 8772240Abstract: Methods of preparing alpha-1-antiproteinase inhibitor and controlling the amount of des-lys alpha-1-antiproteinase inhibitor in the preparation, and compositions comprising the same, as well as methods of treatment using the same are provided.Type: GrantFiled: May 17, 2007Date of Patent: July 8, 2014Assignees: Baxter International Inc., Baxter Healthcare SAInventors: Peter Matthiessen, Alfred Weber, Peter Turecek, Hans-Peter Schwarz
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Patent number: 8772332Abstract: The invention provides a compound of formula (I): or a salt thereof, wherein R1-R4 have any of the values described in the specification, as well as compositions comprising a compound of formula (I). The compounds are useful as antibacterial agents.Type: GrantFiled: September 7, 2011Date of Patent: July 8, 2014Inventor: Richard H. Ebright
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Publication number: 20140187484Abstract: A novel Src inhibitor that targets the Na/K-ATPase/Src receptor complex and antagonizes ouabain-induced protein kinase cascades and uses thereof are disclosed.Type: ApplicationFiled: March 3, 2014Publication date: July 3, 2014Applicant: THE UNIVERSITY OF TOLEDOInventors: Zi-Jian Xie, Zhichuan Li, Joseph I. Shapiro
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Publication number: 20140179593Abstract: Provided herein is a novel binding pocket within NEDD8 co-E3 proteins that binds NEDD8 E2 enzymes. Particularly at its M-Terminus. Methods are provided for screening for compounds that bind to the disclosed E2-binding pocket in NEDD8 co-E3 proteins. Compounds that bind to the E2-binding pocket and optionally inhibit the activity of NEDD8 co-E3 proteins and pharmaceutical compositions comprising the same are further provided. The NEDD8 co-E3 inhibitors find use, as agents preventing the NEDDylation of a target protein, in inhibiting cell growth and methods for treating cancers, inflammatory disorders, and pathogenic infections. The preferred inhibitors are peptides corresponding to a M-terminal fragment of Dnc1, e.g. MTLASKLKRDD, MLKLRQLQKKKQ, and MIKLFSLKQQKK, which are substituted at the M-Terminus with an uncharged group (e.g. acyl).Type: ApplicationFiled: May 16, 2012Publication date: June 26, 2014Applicant: St. Jude Children's Research HospitalInventors: Julie K. Monda, Brenda A. Schulman, Daniel C. Scott
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Publication number: 20140179720Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: Celgene Avilomics Research, Inc.Inventors: Richland Tester, Prasoon Chaturvedi, Zhendong Zhu, Sekhar S. Surapaneni, Lisa Beebe
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Patent number: 8759359Abstract: The present invention provides fused derivatives of Formula I: 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: GrantFiled: December 17, 2010Date of Patent: June 24, 2014Assignee: Incyte CorporationInventors: Andrew P. Combs, Yun-Long Li, Eddy W. Yue, Richard B. Sparks
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Publication number: 20140171454Abstract: The present invention relates to compounds useful as inhibitors of protein 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: December 10, 2013Publication date: June 19, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Mark Ledeboer, Albert Pierce, Guy Bemis, Luc Farmer, Tiansheng Wang, David Messersmith, John Duffy, Francesco Salituro, Jian Wang
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Publication number: 20140171409Abstract: The present invention provides azetidinyl phenyl, pyridyl, or pyrazinyl carboxamide derivatives, as well as their compositions and methods of use, that modulate the activity of Janus kinase (JAKs) 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: February 21, 2014Publication date: June 19, 2014Applicant: Incyte CorporationInventors: Wenqing Yao, David M. Burns, Jincong Zhuo
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Publication number: 20140171405Abstract: The present invention relates to fused pyrazole derivatives, and pharmaceutical compositions including 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: December 18, 2013Publication date: June 19, 2014Applicant: Incyte CorporationInventors: Jincong Zhuo, Meizhong Xu, Ding-Quan Qian
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Patent number: 8754033Abstract: Disclosed herein are transglutaminase peptide inhibitors which have inhibitory activity against transglutaminase, and a pharmaceutical composition comprising one of them as an active ingredient. The inhibitors or the composition is useful in the prevention and treatment of various diseases caused by aberrant transglutaminase activation, including inflammatory diseases and cancers. Also, methods for treating various inflammatory diseases and cancers and for preparing mutant peptides capable of inhibiting transglutaminase are also disclosed.Type: GrantFiled: October 11, 2006Date of Patent: June 17, 2014Assignee: National Cancer CenterInventors: Soo youl Kim, In hoo Kim, Sung soo Park
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Publication number: 20140162939Abstract: The invention provides compounds of formula (I): and salts thereof, wherein X and Y have any of the values defined herein. The compounds inhibit bacterial RNA polymerase, inhibit bacterial growth, and have applications in, analysis of RNA polymerase structure and function, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, antibacterial therapy, and drug discovery.Type: ApplicationFiled: December 12, 2013Publication date: June 12, 2014Inventors: Richard H. Ebright, Yon W. Ebright, Yu Feng, David Degen
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Publication number: 20140163042Abstract: Compounds of formula (I) are inhibitors of histone deacetylase activity, and are useful in the treatment of, for example, cancers, wherein R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; Y is a bond, —C(?O), —S(?O)2—, —C(?O)O—, —C(O)NR3—, —C(?S)—NR3, —C(?NH)NR3 or —S(?O)2NR3— wherein R3 is hydrogen or optionally substituted C1-C6 alkyl; L1 is a divalent radical of formula -(Alk1)m(Q)n(Alk2)p- wherein m, n and p are independently 0 or 1, Q is (i) an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic radical having 5-13 ring members, or (ii), in the case where both m and p are 0, a divalent radical of formula —X2-Q1- or -Q1-X2— wherein X2 is —O—, S— or NRA— wherein RA is hydrogen or optionally substituted C1-C3 alkyl, and Q1 is an optionally substituted divalent mono- or bicyclic carbocyclic or heterocyclic rType: ApplicationFiled: February 13, 2014Publication date: June 12, 2014Applicant: Chroma Therapeutics Ltd.Inventors: Alan Hornsby Davidson, Sanjay Ratilal Patel, Francesca Ann Mazzei, Stephen John Davies, Alan Hastings Drummond, David Festus Charles Moffat, Kenneth William John Baker, Alastair David Graham Donald
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Publication number: 20140161785Abstract: Verticillin A is found to be a potent inhibitor of histone methyltransferases, selective for G9a, GLP, SUV39H1, SUV39H2, MLL1, and NSD2. Methods of using Verticillin A are provided. The Verticillin A can be synthetically produced or it can be isolated from natural sources. Methods if inhibiting one or more histone methyltransferases are provided. In addition, methods are provided for treating diseases or disorders related to overexpression of one or more histone methyltransferases. Exemplary diseases and disorders to be treated include cancer, asthma, HIV, and progeria.Type: ApplicationFiled: December 6, 2013Publication date: June 12, 2014Inventors: Feiyan Liu, Ping Wu, Kebin Liu
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Publication number: 20140163022Abstract: 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 that include 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 3, 2013Publication date: June 12, 2014Inventors: Rao Kolluri, Esteban Masuda, Kin Tso, Salvador Alvarez, Thilo Heckrodt, Sacha Holland, Ryan Kelley, Matthew Duncton, Rajinder Singh, Darren McMurtrie
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Publication number: 20140163079Abstract: The present invention provides compounds of Formulae (I)-(V), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. In one aspect, compounds of the present invention are useful as glycosyltransferase inhibitors, in particular, O-linked N-acetylglucosamine (O-GlcNAc) transferase (OGT) inhibitors. In another aspect, compounds of the present invention are useful as kinase inhibitors, in particular, PLK1 inhibitors, GSK3P inhibitors, or MAPKAPK2 inhibitors. The present invention further provides methods of using the inventive compounds, e.g., as biological probes to study the inhibition of OGT and/or kinase activity and as therapeutics, e.g., for the treatment of OGT-associated and/or kinase-associated conditions.Type: ApplicationFiled: July 6, 2012Publication date: June 12, 2014Applicant: President and Fellows of Harvard CollegeInventors: Suzanne Walker Kahne, Jiaoyang Jiang, Michael Block Lazarus
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Publication number: 20140161771Abstract: Disclosed are compositions and methods comprising one or more recombinant influenza viruses. Recombinant influenza viruses with mutated polymerases and/or rearranged genomes are disclosed. Constructs comprising different influenza nucleic acid sequences are also provided. Methods of inducing protecting immunity with the recombinant influenza viruses are disclosed. Also disclosed are methods of plasmid-free production of influenza virus comprising amplicons comprising one or more of influenza genes.Type: ApplicationFiled: May 28, 2013Publication date: June 12, 2014Inventors: Daniel R. Perez, Hongjun Chen, Yibin Cai, Lindomar Jose Pena, Matthew Angel
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Publication number: 20140163045Abstract: Small molecule xanthine oxidase inhibitors are provided, as well as methods for their use in treating gout or hyperuricemia.Type: ApplicationFiled: March 8, 2013Publication date: June 12, 2014Applicant: BAYLOR COLLEGE OF MEDICINEInventors: Changyi Chen, Jian-Ming Lu, Qizhi Yao
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Publication number: 20140162940Abstract: The invention provides bipartite inhibitors of bacterial RNA polymerase that contain: (i) a first moiety that binds to the salinamide binding site of a bacterial RNA polymerase; (ii) a second moiety comprising a nucleoside analog; and (iii) a linker connecting said first and second moieties.Type: ApplicationFiled: December 12, 2013Publication date: June 12, 2014Inventors: Richard H. Ebright, Yu Feng, Yu Zhang
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Publication number: 20140155421Abstract: The present invention relates to substituted pyrimidinyl-pyrrole compounds of formula (I) which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity, in particular Janus kinases. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.Type: ApplicationFiled: April 5, 2012Publication date: June 5, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maria Gabriella Brasca, Tiziano Bandiera, Jay Aaron Bertrand, Paola Gnocchi, Danilo Mirizzi, Marcella Nesi, Achille Panzeri
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Publication number: 20140154264Abstract: In alternative embodiments, the invention provides compositions and methods for identifying individuals that would be responsive to a treatment comprising (including) blocking activation of integrin polypeptide alphav-beta3 (or ?v-?3), or blocking the interaction of a ligand with integrin polypeptide alphav-beta3 (or ?v-?3). The invention provides compositions and methods for determining the effectiveness of such a treatment and can contribute to a prognosis for the patient.Type: ApplicationFiled: June 1, 2012Publication date: June 5, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: David Cheresh, Aleksandra Franovic, Laetitia Seguin
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Publication number: 20140154772Abstract: 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 are disclosed. Preferably, the methods employ active agents that selectively inhibit PI3K?, while not significantly inhibiting activity of other PI3K isoforms. Compounds are provided that inhibit PI3K? activity, including compounds that selectively inhibit PI3K? activity. Methods of using PI3K? inhibitory compounds to inhibit cancer cell growth or proliferation are also provided. Accordingly, the invention provides methods of using PI3K? inhibitory compounds to inhibit PI3K?-mediated processes in vitro and in vivo.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Applicant: ICOS CORPORATIONInventors: Chanchal SADHU, Ken DICK, Jennifer TREIBERG, C. Gregory SOWELL, Edward A. KESICKI, Amy OLIVER
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Publication number: 20140155339Abstract: Compositions comprising hydroxytyrosol-containing formulations and treatment regiments comprising hydroxytyrosol and/or oleuropein and chemotherapeutic agents are disclosed. Compositions and/or regiments may optionally include the administration of vitamins, minerals, and anti-oxidants. Methods for using these compositions and treatment regimens for treating subjects for diseases, such as a malignancy, and for inducing or enhancing angiogenesis, treating or preventing oxidative stress, for treating or preventing high glucose-induced dysfunction, treating or preventing chemotherapy-induced dysfunction, and for improving cell viability are provided. Various methods for use of the hydroxytyrosol compositions for inhibition of lysine specific demethylase 1 (LSD1) in various cancers are also provided.Type: ApplicationFiled: November 27, 2013Publication date: June 5, 2014Inventors: Darlene E. McCord, Thomas Karagiannis
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Publication number: 20140147905Abstract: A boronic or borinic acid compound is used to inhibit the activity of a sulfenic acid-containing protein. Thus, a biologically-active sulfenic acid-containing protein is contacted with an activity-inhibiting effective amount of a boronic or borinic acid compound of Formula I or a salt, hydrate or solvate thereof, whose components are disclosed within, and that contact is maintained for a time sufficient to inhibit the biological activity of the protein.Type: ApplicationFiled: August 27, 2013Publication date: May 29, 2014Inventors: Stephen Benkovic, Chunyu Liu, John W. Tomsho
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Patent number: 8735083Abstract: The present invention deals with reagents and compositions capable of effectively inhibiting peroxidase activity. According to the invention, peroxidase enzymatic activity is blocked with an acidic aqueous solution of a protein denaturing agent. preferred protein denaturing agents are detergents and chaotropic substances.Type: GrantFiled: June 6, 2007Date of Patent: May 27, 2014Assignee: Roche Diagnostics Operations, Inc.Inventors: Manfred Watzele, Bernd Buchberger, Claudia Kirr
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Publication number: 20140142040Abstract: Methods for inhibiting activated protein C (APC) comprising contacting the APC with a Kunitz polypeptide in an amount effective in inhibiting the activity of APC, wherein the Kunitz polypeptide comprises six cysteine residues at positions corresponding to positions 7, 16, 32, 40, 53, and 57 in SEQ ID NO:1, a motif X1GX2CBX? at positions corresponding to positions 13-18 in SEQ ID NO:1, wherein each of X1 and X2, independently, is any amino acid residue, B is a basic amino acid residue, and X? is G, A, or V; and at least one heparin-binding motif, which can present at the C-terminus of the Kunitz polypeptide.Type: ApplicationFiled: November 15, 2013Publication date: May 22, 2014Inventors: Inn-Ho Tsai, An-Chun Cheng
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Publication number: 20140141099Abstract: The present invention relates to drug discovery methods, particularly methods for assaying compounds for activity as Aurora kinase inhibitors. This invention also relates to a pharmacophore describing compounds that are able to promote a conformational change in the protein AuroraB and whose binding constant for the two-step process is given as Ki*. Finally, this invention also relates to compounds having the features of the pharmacophore.Type: ApplicationFiled: January 27, 2014Publication date: May 22, 2014Inventors: Julian Golec, John Pollard, James Westcott, Hayley Binch, Michael Mortimore, Daniel Robinson
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Publication number: 20140142120Abstract: The present invention relates to pharmaceutical compositions comprising a compound and a pharmaceutically acceptable carrier. The present invention is also directed to a method of treating cancer in a subject. Also disclosed are methods of inhibiting SCF-Skp2 activity and a method of identifying inhibitors of SCF-Skp2 activity.Type: ApplicationFiled: October 16, 2013Publication date: May 22, 2014Applicant: NEW YORK UNIVERSITYInventors: Timothy Cardozo, Michele Pagano, Lily Wu, Leslie I. Gold
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Publication number: 20140134736Abstract: The present disclosure relates to methods of controlling the sulfide (S2˜) content in systems, such as oil and gas reservoirs and pipelines, by the use of chlorine oxyanions and microorganisms with (per)chlorate-reducing activity.Type: ApplicationFiled: May 31, 2012Publication date: May 15, 2014Applicant: The Regents of the University of CaliforniaInventor: John D. Coates
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Publication number: 20140135347Abstract: Disclosed herein are compounds that form covalent bonds with Bruton's tyrosine kinase (Btk). Also described are irreversible inhibitors of Btk. Methods for the preparation of the compounds are disclosed. Also disclosed are pharmaceutical compositions that include the compounds. Methods of using the Btk inhibitors are disclosed, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions.Type: ApplicationFiled: January 10, 2014Publication date: May 15, 2014Applicant: Pharmacyclics, Inc.Inventors: Lee HONIGBERG, Erik VERNER, Zhengying PAN
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Publication number: 20140134133Abstract: The present invention provides heteroaromatic derivatives and pharmaceutical acceptable salts and formulations thereof useful in modulating the protein kinase activity, especially phosphatidylinositol 3-kinases (PI3 kinases) and mTOR, and in modulating inter- and/or intra-cellular signaling activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.Type: ApplicationFiled: November 10, 2013Publication date: May 15, 2014Applicants: Calitor Sciences, LLCInventor: Ning Xi
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Publication number: 20140128460Abstract: Inhibitors of EYA tyrosine phosphatase are provided herein, as well as pharmaceutical compositions and methods relating thereto.Type: ApplicationFiled: March 6, 2013Publication date: May 8, 2014Applicant: CHILDREN'S HOSPITAL MEDICAL CENTERInventor: Children's Hospital Medical Center
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Publication number: 20140127284Abstract: In alternative embodiments, the invention provides compositions and methods comprising use of microRNAs and microRNA inhibitors to modulate blood vessel growth (angiogenesis), e.g., act as anti-angiogenic agents, and modulate cell and tumor microenvironment patterning, cancer cell and tumor growth and malignant disease (metastasis). In alternative embodiments, the invention provides compositions and methods that can sensitize blood vessels, e.g., tumor blood vessels, to radiation and agents and chemotherapies that cause DNA damage.Type: ApplicationFiled: October 18, 2013Publication date: May 8, 2014Applicant: The Regents of The University of CaliforniaInventors: David CHERESH, Sudarshan ANAND, Sunil ADVANI
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Publication number: 20140128344Abstract: The invention provides compounds and methods for inhibiting proteases. One aspect of the invention features pro-soft inhibitors which react with an activating protease to release an active inhibitor moiety in proximity to a target protease. In certain instances, compounds inhibit proteasomes and/or post-proline cleaving enzymes (PPCE), such as dipeptidyl peptidase IV. The compounds of the invention provide a better therapeutic index, owing in part to reduced toxicity and/or improved specificity for the targeted protease.Type: ApplicationFiled: September 30, 2013Publication date: May 8, 2014Applicant: Trustees of Tufts CollegeInventors: William W. Bachovchin, Hung-Sen Lai, Wengen Wu
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Publication number: 20140128392Abstract: Disclosed herein are new heterocyclic compounds of Formula IIa: and compositions thereof, and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: ApplicationFiled: March 19, 2010Publication date: May 8, 2014Applicant: BIOENERGENIXInventors: John M. McCall, Donna L. Romero
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Patent number: 8716344Abstract: The present invention relates to compounds of the following formula wherein R3 is a fluorescent tag. Another aspect of the invention provides an assay for determining the inhibitory effect of a test compound on an HDAC protein comprising: incubating the HDAC protein with a substrate of the above formula in the presence of a test compound; and determining the activity of the HDAC protein.Type: GrantFiled: August 11, 2010Date of Patent: May 6, 2014Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Ralph Mazitschek, James Elliot Bradner
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Patent number: 8716295Abstract: A method for treating cancer in a subject, comprising administering to a subject having cancer a therapeutically effective amount of (i) a fluoroquinolone derivative that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity or (ii) a sulfonamide moiety-containing compound that inhibits tyrosyl-DNA-phosphodiesterase 1 (Tdp1) activity, thereby treating the cancer in the subject. In certain embodiments, the fluoroquinolone derivative or sulfonamide moiety-containing compound is co-administered with a topoisomerase I (TopI) inhibitor.Type: GrantFiled: October 27, 2011Date of Patent: May 6, 2014Inventors: Yves Pommier, Christophe Marchand, Periyasamy Selvam, Thomas Dexheimer, Kasthuraiah Maddali