Plural Chalcogens Bonded Directly To Ring Carbons Of The Thiazole Ring Patents (Class 548/183)
  • Patent number: 9126959
    Abstract: The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).
    Type: Grant
    Filed: October 30, 2014
    Date of Patent: September 8, 2015
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: Gerard R. Colca, Steven P. Tanis, Scott D. Larsen
  • Publication number: 20150139915
    Abstract: Methods and compositions are described for reducing airway reactivity and the susceptibility to asthmatic bronchoconstriction that involve increasing sphingolipid content in airways and lungs of a mammalian subject.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 21, 2015
    Inventors: Stefan Worgall, Tilla S. Worgall
  • Publication number: 20150133514
    Abstract: Protein disulfide isomerase inhibitors according to formula I are described, wherein R1 is an aryl or cycloalkyl group, R2 is selected from the group consisting of CN, SO2CH3, NO2, CO2R3, CONHR3, NMe2, and CF3, R3 is selected from H or lower alkyl, R4 is H, halogen, CN, or COOH, and X and Y are C—H or heteroatoms selected from the group consisting of N, O, and S. The protein disulfide isomerase inhibitors can be used for the treatment of cancer in a subject.
    Type: Application
    Filed: November 10, 2014
    Publication date: May 14, 2015
    Inventors: Frederic J. Reu, Jim Phillips, Sergei Vatolin, Dale Grabowski
  • Publication number: 20150133431
    Abstract: This invention relates to geranylgeranyl acetone (GGA) derivatives, pharmaceutical compositions comprising GGA derivatives and the use of GGA derivatives.
    Type: Application
    Filed: July 10, 2014
    Publication date: May 14, 2015
    Applicant: COYOTE PHARMACEUTICALS, INC.
    Inventor: Gary C. Look
  • Patent number: 9023876
    Abstract: The application describes small molecules capable of modulating activity of beta2 family of integrins, such as integrin CD11b/CD18 (also known as Mac-1, CR3 and ?M?2). Such compounds may be used in certain embodiments for treating a disease or condition, such as inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, wound-healing, organ transplantation and cardiovascular disease, among others.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: May 5, 2015
    Assignee: Adhaere Pharmaceuticals, Inc.
    Inventor: Vineet Gupta
  • Patent number: 8969581
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: March 3, 2015
    Assignee: DeuteRx, LLC
    Inventor: Sheila DeWitt
  • Publication number: 20150057319
    Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.
    Type: Application
    Filed: November 4, 2014
    Publication date: February 26, 2015
    Inventors: Isabel KALOFONOS, Patrick G. STAHLY, William Martin-Doyle, Dimitris KALOFONOS, Travis L. Houston, Jeffrey S. STULTS
  • Publication number: 20150051406
    Abstract: The present invention relates to novel salts of thiazolidinediones and other pharmaceutical agents that are useful for treating and/or preventing metabolic diseases (e.g., diabetes, or neurodegenerative diseases (e.g., Alzheimer's Disease).
    Type: Application
    Filed: October 30, 2014
    Publication date: February 19, 2015
    Inventors: Gerard R. Colca, Steven P. Tanis, Scott D. Larsen
  • Publication number: 20150051255
    Abstract: Thiazolidinedione compounds and pharmaceutically acceptable salts thereof are described. The compounds can be used in methods of treating cancer in a subject by administering to the subject a therapeutically effective amount of the compound. The compounds can also be used in methods of inhibiting glucose uptake in a cell by contacting the cell with the compound.
    Type: Application
    Filed: March 28, 2013
    Publication date: February 19, 2015
    Applicant: The Ohio State University Research Foundation
    Inventors: Ching-Shih Chen, Dasheng Wang, Samuel K. Kulp
  • Publication number: 20150045396
    Abstract: The present invention provides a prophylactic or therapeutic agent for giant cell tumors occurring in a bone and soft tissue or for chondrosarcoma, which comprises a non-steroidal anti-inflammatory agent or thiazolidine derivative as an active ingredient, and the like
    Type: Application
    Filed: March 18, 2013
    Publication date: February 12, 2015
    Applicant: NIPPON CHEMIPHAR CO., LTD.
    Inventors: Akihiko Takeuchi, Hiroyuki Tsuchiya
  • Patent number: 8933240
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Grant
    Filed: August 9, 2011
    Date of Patent: January 13, 2015
    Assignee: Metabolic Solutions Development Company, LLC
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, Gerald D. Artman, III, James R. Zeller
  • Publication number: 20150005353
    Abstract: 3-(2-amino-ethyl)-5-[3-(4-substituted-phenyl)-alkylidene)-thiazolidine-2,4-dione and 1-(2-amino-ethyl)-3-alkylidene-1,3-dihydro-indol-2-one and derivatives thereof are provided for use as selective SphK2 inhibitors and for use in the treatment of human diseases, such as cancer.
    Type: Application
    Filed: February 7, 2013
    Publication date: January 1, 2015
    Applicant: Virginia Commonwealth University
    Inventors: Shijun Zhang, Sarah Spiegel
  • Publication number: 20140364465
    Abstract: The present invention relates to thiazolidinedione derivatives, to the processes for preparing same and to the therapeutic use thereof for preventing or treating cancer, and more specifically breast cancer. These compounds are of formula (I) and exhibit, at a concentration of 100 ?M, a hepatocyte viability preferably greater than 60%, preferably greater than 80% and more preferentially greater than 85%.
    Type: Application
    Filed: January 25, 2013
    Publication date: December 11, 2014
    Applicants: UNIVERSITE DE LORRAINE, CENTRE NATIONAL DE LA RECHERCH SCIENTIFIQUE - CNRS
    Inventors: Michel Boisbrun, Yves Chapleur, Andrea Bordessa, Stephane Flament, Isabelle Grillier-Vuissoz, Sandra Kuntz
  • Patent number: 8906948
    Abstract: The invention relates to a novel choline cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel choline cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel choline cocrystal and the therapeutic use of the novel choline cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, treating and/or preventing homocystinuria reducing levels of homocysteine in blood serum, inhibiting aldose reductase, and affording cardioprotection in non-diabetic patients.
    Type: Grant
    Filed: September 3, 2009
    Date of Patent: December 9, 2014
    Assignee: Bionevia, LLC
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Travis L. Houston
  • Patent number: 8883834
    Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.
    Type: Grant
    Filed: June 6, 2014
    Date of Patent: November 11, 2014
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20140329674
    Abstract: The present specification discloses honeybee repellents exhibiting repellent properties similar to 2-heptanone, compositions comprising such repellents, uses to repel a honeybee from a mammal, location, plant, structure treated of such repellents, and methods of treating a mammal, location, plant, structure by applying such repellents.
    Type: Application
    Filed: May 3, 2014
    Publication date: November 6, 2014
    Applicant: INSCENT, INC.
    Inventors: Daniel F. Woods, Spiros Dimitratos, Robin W. Justice
  • Patent number: 8865909
    Abstract: Novel agents exhibiting anti-biofilm formation activity while being non-cytotoxic are provided, as well as methods of using the same, either per se or conjugated to a polymer, for preventing and/or reducing the formation of microbial biofilms and/or for disrupting microbial biofilms. The novel agents described herein include thiazolidine-2,4-diones (TZDs), pyrrolidine-2,5-diones (PYDs), imidazolidine-2,4-diones or oxazolidine-2,4-diones, substituted by an alkyl having 7-20 carbon atoms in its backbone chain.
    Type: Grant
    Filed: November 19, 2009
    Date of Patent: October 21, 2014
    Assignees: Yissum Research Development Company of the Hebrew University of Jerusalem Ltd., Hadasit Medical Research Services and Development Ltd.
    Inventors: Morris Srebnik, Itzhack Polacheck, Doron Steinberg, Adel Jabbour, Edward Sionov
  • Publication number: 20140296270
    Abstract: Small molecule inhibitors of Stat3 and their derivatives are disclosed. Also described are methods to inhibit cell growth by use of Stat3 inhibitors, and the use of Stat3 inhibitors for the prevention and/or treatment of cancer. Further, inhibitors of Stat3 that also do not inhibit Stat1 are described as well as their derivatives. Methods of screening additional compounds for Stat3 inhibition activity and/or non-inhibition of Stat1 activity are also described herein.
    Type: Application
    Filed: April 15, 2014
    Publication date: October 2, 2014
    Applicant: Baylor College of Medicine
    Inventors: David J. Tweardy, Xuejun Xu, Moses M. Kasembeli
  • Publication number: 20140288106
    Abstract: The present invention relates to compounds of formula 1 that are useful for the preventive or therapeutic treatment of diseases caused by abnormal activation of CXCR3 chemokines. The invention relates furthermore to a process for the preparation of said compounds, to pharmaceutical compositions containing said compounds and to novel intermediates used in the preparation of said compounds.
    Type: Application
    Filed: June 3, 2014
    Publication date: September 25, 2014
    Applicant: Sanofi
    Inventors: Imre BATA, Peter BUZDER-LANTOS, Attila VASAS, Veronika BARTANE BODOR, Gyorgy FERENCZY, Zsuzsanna TOMOSKOZI, Gabor SZELECZKY, Sandor BATORI, Martin SMRCINA, Marcel PATEK, Aleksandra WEICHSEL, David Squire Thorpe
  • Publication number: 20140275180
    Abstract: The invention provides 5-deuterium-enriched 2,4-thiazolidinediones (e.g., 5-[4-[2-(5-ethyl-2-pyridyl)-2-oxoethoxy]benzyl]-5-deutero-thiazolidine-2,4-dione), deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: DEUTERX, LLC
    Inventor: Sheila DeWitt
  • Publication number: 20140243534
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: May 5, 2014
    Publication date: August 28, 2014
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20140221438
    Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.
    Type: Application
    Filed: April 11, 2014
    Publication date: August 7, 2014
    Applicant: Bionevia Pharmaceuticals, Inc.
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Travis L. Houston
  • Patent number: 8795984
    Abstract: A method is described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of an inhibitor of Pmt-mediated O-linked glycosylation and/or in the presence of one or more ?-1,2-mannosidases.
    Type: Grant
    Filed: June 22, 2012
    Date of Patent: August 5, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Piotr Bobrowicz, W. James Cook, Warren Kett
  • Patent number: 8790855
    Abstract: The present invention provides a charge control agent containing, as an active substance(s), one or two or more thiazolidinedione derivatives represented by the following formula (1), where R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc.; R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a chlorine atom, a linear or branched alkyl group having 1 to 8 carbon atoms which may have a substituent, etc., and may be joined to each other to form a ring; and V, W, X, Y and Z represent a carbon atom or a nitrogen atom, and 0 to 3 of any of V, W, X, Y and Z are nitrogen atoms which do not have the substituents of R3 to R7.
    Type: Grant
    Filed: September 1, 2011
    Date of Patent: July 29, 2014
    Assignee: Hodogaya Chemical Co., Ltd
    Inventors: Ikuo Kimura, Motonori Tsuji, Masami Ito, Masaya Tojo, Kanae Hiraishi
  • Patent number: 8778981
    Abstract: Provided are methods for increasing fat locally in a body of a subject in need thereof comprising percutaneously administering to the subcutaneous fat of the subject a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, optionally delivered as a composition comprising a pharmaceutically acceptable carrier, as described herein. In certain embodiments, the pharmaceutically acceptable carrier comprises a percutaneous carrier, as described herein. Further provided are compositions comprising a thiazolidinedione or an orexigenic compound, or a pharmaceutically acceptable salt or prodrug thereof, for use according to the invention.
    Type: Grant
    Filed: November 21, 2013
    Date of Patent: July 15, 2014
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Publication number: 20140194412
    Abstract: The present invention provides an anticancer drug having a Ras function inhibitory action. The present invention provides a Ras function inhibitor comprising a compound represented by the formula (I?): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: May 9, 2012
    Publication date: July 10, 2014
    Applicants: KNC LABORATORIES CO., LTD., NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
    Inventors: Tohru Kataoka, Fumi Shima, Masahiro Neya, Daisuke Sasahara
  • Patent number: 8765409
    Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: July 1, 2014
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ranjit Desai, Lihu Yang
  • Publication number: 20140179743
    Abstract: A compound, having the formula A-1: Wherein R1 and R2 are defined herein. Methods of using the compound and compositions containing the compound are provided.
    Type: Application
    Filed: December 20, 2013
    Publication date: June 26, 2014
    Applicant: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Paul S. Shapiro, Alexander D. MacKerell, JR., Steven Fletcher
  • Patent number: 8759536
    Abstract: Disclosed are novel rhodanine derivatives which are inhibitory of HIV activity. Also provided are a method for preparing the novel rhodanine derivatives, and a pharmaceutical composition for the prevention or treatment of AIDS containing the rhodanine derivatives as active ingredients. Having high inhibitory activity against HIV, the rhodanine derivatives can be effectively used in the prophylaxis or therapy of AIDS.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: June 24, 2014
    Assignee: Avixgen Inc.
    Inventors: Ji Chang You, Gyoon Hee Han, Chul Ho Lee, Doo Na Song, Koo Hwan Chung
  • Publication number: 20140142308
    Abstract: Receptor type oligothiopene compounds, methods of preparing the compounds, and use of the compounds in photoelectric materials.
    Type: Application
    Filed: March 27, 2012
    Publication date: May 22, 2014
    Applicant: NANKAI UNIVERSITY
    Inventors: Yongsheng Chen, Xiangjian Wan, Yongsheng Liu, Zhi Li, Jiaoyan Zhou, Fei Wang, Guangrui He, Guankui Long
  • Publication number: 20140113884
    Abstract: Compounds and compositions comprising epoxyeicosatrienoic acid (EET) analogs that act as EET agonists and are useful as medications in the treatment of drug-induced nephrotoxicity, hypertension and other related conditions. Methods of making and using the compounds and compositions are further described.
    Type: Application
    Filed: April 4, 2012
    Publication date: April 24, 2014
    Inventors: John David Imig, William B. Campell, John Russell Falck
  • Patent number: 8697735
    Abstract: The invention relates to novel crystalline salts of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid and a novel betaine cocrystal of 5-[(1Z,2E)-2-methyl-3-phenylpropenylidene]-4-oxo-2-thioxo-3-thiazolidineacetic acid. The preparation and characterization of the novel crystalline salts and cocrystal according to various embodiments of the invention is described. The invention also relates to pharmaceutical compositions containing the novel crystalline salts and cocrystal and the therapeutic use of the novel crystalline salts and cocrystal to treat and/or prevent various conditions, including treating and/or preventing diabetic complications, inhibiting aldose reductase, and affording cardioprotection in patients who may be non-diabetic.
    Type: Grant
    Filed: January 25, 2011
    Date of Patent: April 15, 2014
    Assignee: Bionevia Pharmaceuticals, Inc.
    Inventors: Isabel Kalofonos, G. Patrick Stahly, William Martin-Doyle, Dimitris Kalofonos, Jeffrey S. Stults, Travis L. Houston
  • Patent number: 8686009
    Abstract: The invention provides a method of sustained delivery of a lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug by administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile conjugates of parent drugs that are derivatized through carbonyl linked prodrug moieties. The prodrug compounds of the invention can be used to treat any condition for which the lactam, imide, amide, sulfonamide, carbamate or urea containing parent drug is useful as a treatment.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: April 1, 2014
    Assignee: Alkermes Pharma Ireland Limited
    Inventors: Laura Cook Blumberg, Julius F. Remenar, Örn Almarsson, Tarek A. Zeidan
  • Patent number: 8653279
    Abstract: The present embodiments relate to a dye for a dye-sensitized solar cell and a dye-sensitized solar cell prepared from the same. The dye includes a fluorenyl-containing compound. The dye according to the present embodiments is applied to a light absorption layer to improve photovoltaic efficiency and increase an open-circuit voltage.
    Type: Grant
    Filed: April 16, 2007
    Date of Patent: February 18, 2014
    Assignee: Samsung SDI Co., Ltd.
    Inventors: Jae-Kwan Lee, Ji-Won Lee, Jae-Jung Ko, Sang-Hoon Kim, Soo-Jin Moon, Moon-Sung Kang, Moon-Seok Kwon
  • Patent number: 8653115
    Abstract: The invention relates a kind of antiviral agents, more concretely, relates to a kind of heterocyclic non-nucleoside compounds with the following structures, their preparation and pharmaceutical compositions including the compounds. The said compounds can be used as antiviral agents and as medicaments for treating diseases such as hepatitis B, influenza, herpes, HIV and so on.
    Type: Grant
    Filed: June 13, 2007
    Date of Patent: February 18, 2014
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Fajun Nan, Jianping Zuo, Haijun Chen, Guifeng Wang, Min Gu, Fenghua Zhu, Wei Tang
  • Publication number: 20140038962
    Abstract: Methods of treating, preventing, and/or ameliorating a Flavivirus infection in a subject are disclosed. The methods comprise administering to the subject a therapeutically effective amount of a Flavivirus inhibitor, e.g., a Flavivirus serine protease inhibitor. These methods are useful in treating, preventing, and/or ameliorating Flavivirus infections such as, for example, West Nile Virus, Dengue Virus, and Japanese Encephalitis Virus.
    Type: Application
    Filed: September 20, 2013
    Publication date: February 6, 2014
    Applicant: GEORGETOWN UNIVERSITY
    Inventors: Radhakrishnan Padmanabhan, Nagarajan Pattabiraman, Niklaus Mueller, Kuppuswamy Nagarajan
  • Publication number: 20140038970
    Abstract: This invention provides for certain bridged and fused compounds of the formula G-L-A??I or a pharmaceutically acceptable salt, ester of solvate thereof wherein: A is and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.
    Type: Application
    Filed: October 2, 2013
    Publication date: February 6, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: HUBERT B. JOSIEN, John W. Clader, William J. Greenlee, Michael J. Mayer, Jason L. Davis, Shuangyi Wan
  • Patent number: 8637556
    Abstract: Provided herein are compounds and compositions for interfering with the association of Myc and Max. These compounds and compositions are useful in methods for inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell comprise contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.
    Type: Grant
    Filed: January 15, 2010
    Date of Patent: January 28, 2014
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, Georgetown University
    Inventors: Steven J. Metallo, Edward V. Prochownik, Ariele Viacava Follis
  • Publication number: 20140017722
    Abstract: The present invention provides a hematopoietic stem cell identification probe.
    Type: Application
    Filed: July 10, 2013
    Publication date: January 16, 2014
    Inventors: Kohei Watanabe, Tsuyoshi Nomoto, Mie Okano, Taichi Shintou, Takeshi Miyazaki, Yasuhiko Tabata, Hiroshi Kohara
  • Publication number: 20140012002
    Abstract: The present invention relates to compounds of general formula I wherein R100 and R200 are each independently hydrogen, C1-C10-alkyl which in case of C2-alkyl may be interrupted by one and in case of C3-C10-alkyl by one or two nonadjacent oxygen atoms, C5-C7-cycloalkyl, aryl, aryl-C1-C10-alkyl or aryloxy-C1-C10-alkyl, D is an m-valent (m=1, 2 or 3) donor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, A is an acceptor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, and the donor moiety D and the acceptor moiety A are ?-conjugated to one another. Furthermore, the present invention relates to the use of compounds of formula I for producing dye-sensitized solar cells and to dye-sensitized solar cells comprising compounds of formula I.
    Type: Application
    Filed: July 1, 2013
    Publication date: January 9, 2014
    Inventors: Ingmar BRUDER, Robert Send, Simona Urnikaite, Tadas Malinauskas, Maryte Daskeviciene, Vytautas Getautis
  • Publication number: 20130345267
    Abstract: 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: Application
    Filed: May 30, 2013
    Publication date: December 26, 2013
    Inventors: Ronen Marmorstein, Xin Liu, Philip A. Cole, Ling Wang, Erin M. Bowers, David J. Meyers, Chandrani Mukherjee
  • Publication number: 20130316398
    Abstract: Compounds and methods are described for producing protein compositions having reduced amounts of O-linked glycosylation. The method includes producing the protein in cells cultured in the presence of certain benzylidene thiazolidinediones inhibitors of Pmt-mediated O-linked glycosylation.
    Type: Application
    Filed: August 17, 2012
    Publication date: November 28, 2013
    Applicant: Merck Sharpe & Dohme Corp.
    Inventors: RANJIT DESAI, Lihu Yang
  • Publication number: 20130308219
    Abstract: The present invention relates to a polymerizable composition comprising at least one ethylenically unsaturated, polymerizable compound and at least one oxime sulfonate compound of the formula (I) QAaBbCc where a is 0, 1, 2, 3, 4 or 6, b is 0, 1, 2, 3, 4 or 6, and c is 0, 1, 2, 3, 4 or 6, where the sum of a+b+c is 1, 2, 3, 4 or 6 where (A) is a group (B) is a group (C) is a group where # denotes the point of attachment to Q; X is S or NR14 and Q, R1, R2, R3 and R14 are as defined in claim 1 and in the description. The present invention also relates to the use of the this composition, to novel oxime sulfonates and the use of the oxime sulfonates as thermal curing promoter.
    Type: Application
    Filed: January 27, 2012
    Publication date: November 21, 2013
    Applicant: BASF SE
    Inventors: Kazuhiko Kunimoto, Kaori Sameshima, Yuki Matsuoka, Hisatoshi Kura
  • Publication number: 20130296386
    Abstract: Small molecule inhibitors of bacterial ribonuclease (e.g., RnpA) and methods for their synthesis and use are described herein. The methods of using the compounds include treating and preventing microbial infections and inhibiting bacterial ribonuclease.
    Type: Application
    Filed: January 26, 2012
    Publication date: November 7, 2013
    Applicants: UNIVERSITY OF ROCHESTER, TEMPLE UNIVERSITY--OF THE COMMONWEALTH SYSTEM OF HIGHER LEARNING, BOARD OF REGENTS OF THE UNIVERSITY OF NEBRASKA
    Inventors: Paul M. Dunman, Patrick D. Olson, Wayne Childers
  • Publication number: 20130280169
    Abstract: To provide a central nervous system tissue-labeling composition labeling the central nervous tissue system. Also, another object of the present invention is to provide a method for non-invasively labeling the central nervous tissue system. Further, another object of the present invention is to provide a screening method using the above central nervous system tissue-labeling composition. A central nervous system tissue-labeling composition containing, as an active ingredient, at least one of compounds represented by the general formula (1) or (7).
    Type: Application
    Filed: June 19, 2013
    Publication date: October 24, 2013
    Inventors: Kohei Watanabe, Taichi Shintou, Tsuyoshi Nomoto, Takeshi Miyazaki, Mie Okano, Toshio Tanaka, Yuhei Nishimura, Yasuhito Shimada
  • Patent number: 8552038
    Abstract: A crystalline form of a hydrate of a dihydrochloride 5-(4-{[6-(4-amino-3,5-dimethylphenoxy)-1-methyl-1-H-benzimidazol-2-yl]methoxy}benzyl)-1,3-thiazolidine-2,4-dione represented by the following formula: wherein the crystalline form shows main peaks at interplanar spacings of 10.42, 5.85, 5.52, 3.84, 3.46 and 2.95 angstroms in X-ray powder diffraction obtained with Cu K? line radiation (wavelength ?=1.54 angstroms).
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: October 8, 2013
    Assignee: Daiichi Sankyo Company, Limited
    Inventor: Hiroshi Miyamoto
  • Publication number: 20130253021
    Abstract: 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: Application
    Filed: March 22, 2013
    Publication date: September 26, 2013
    Applicants: The Johns Hopkins University, Southern Methodist University
    Inventors: Edward R. Biehl, Sukanta Kamila, Ted M. Dawson
  • Publication number: 20130231604
    Abstract: Halo-organic heterocyclic compounds are described, in which at least two halogen atoms are bound to a nitrogen-containing heterocyclic terminal moiety of the compound, with at least one of such halogen atoms being iodine or bromine. Also described are polymethine dyes based on these heterocyclic compounds, and dendrimeric compounds and conjugates of such polymethine dyes. The polymethine dyes are characterized by enhanced properties, e.g., brightness, photostability, sensitivity and/or selective affinity that make them useful to target cancer cells, pathogenic microorganisms, and/or other biological materials, in applications such as photodynamic therapy, photodynamic antimicrobial chemotherapy (PACT), cancer treatment, selective removal or attachment of biological materials, antimicrobial coating materials, and other diagnostic, theranostic, spectrum shifting, deposition/growth, and analytic applications.
    Type: Application
    Filed: March 3, 2012
    Publication date: September 5, 2013
    Applicant: NANOQUANTUM SCIENCES, INC.
    Inventors: Gary W. Jones, Anatoliy L. Tatarets, Leonid D. Patsenker
  • Publication number: 20130211095
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: August 15, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Timothy Parker, Robert C. Gadwood, Steven P. Tanis, Scott D. Larsen, James R. Zeller
  • Publication number: 20130204008
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, Gerald D. Artman, III, James R. Zeller