Boron Containing Doai Patents (Class 514/64)
  • SUBSTITUTED TRIAZOLOPYRIDINES
    Publication number: 20120328611
    Abstract: The present invention relates to triazolopyridine compounds of general formula (I) which are Monopolar Spindle 1 kinase (Mps-1 or TTK) inhibitors: Formula (I), in which R1, R2, R3, R4, and R5 are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis proliferative of diseases, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: November 17, 2010
    Publication date: December 27, 2012
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Volker Schulze, Marcus Koppitz, Dirk Kosemund, Benjamin Bader, Philip Lienau, Hans Briem, Simon Holton, Gerhard Siemeister, Stefan Prechtl, Antje Margret Wengner
  • Phosphine-borane compound and method for producing the same, and method for producing hydrogen-phosphine-borane compound
    Patent number: 8338391
    Abstract: An object of the present invention is to provide an optically active phosphine-borane compound and a method for producing the same which are useful for the production of an optically active phosphine ligand and allow easy production of any antipode. There is provided a phosphine-borane compound represented by the following general formula (P-1). There is also provided a method for producing the phosphine-borane compound, the method comprising subjecting a hydrogen-phosphine-borane compound represented by the following general formula (P-2) to a coupling reaction with an optically active isocyanate compound represented by the following general formula (3).
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: December 25, 2012
    Assignee: Nippon Chemical Industrial Co., Ltd.
    Inventor: Daisuke Mayama
  • Stable Bortezomib Formulations
    Publication number: 20120322763
    Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
    Type: Application
    Filed: August 22, 2012
    Publication date: December 20, 2012
    Applicant: INNOPHARMA, INC.
    Inventors: Kumaresh Soppimath, Satish Pejaver, Kanaiyalal R. Patel, Lakkaraju Dasaradhi, Rama Sodum, Hari Desu, Navneet Puri
  • Stable Bortezomib Formulations
    Publication number: 20120322762
    Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
    Type: Application
    Filed: August 22, 2012
    Publication date: December 20, 2012
    Applicant: INNOPHARMA, INC.
    Inventors: Kumaresh Soppimath, Satish Pejaver, Kanaiyalal R. Patel, Lakkaraju Dasaradhi, Rama Sodum, Hari Desu, Navneet Puri
  • USES OF FORMULATIONS OF THYROID HORMONE ANALOGS AND NANOPARTICULATE FORMS THEREOF TO INCREASE CHEMOSENSIVITY AND RADIOSENSITIVITY IN TUMOR OR CANCER CELLS
    Publication number: 20120315320
    Abstract: Disclosed are methods of increasing the chemosensitivity of normal and/or chemoresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof. Also disclosed are methods of increasing radiosensitivity of normal and/or radioresistant tumor or cancer cells using thyroid hormone analogs and/or nanoparticulate or polymeric forms thereof.
    Type: Application
    Filed: January 6, 2012
    Publication date: December 13, 2012
    Inventors: Paul J. Davis, Shaker A. Mousa
  • Process For The Co-Encapsulation Of Biocidally Active Compounds In Clay Minerals Functionalized By Nitrogen Compounds
    Publication number: 20120316259
    Abstract: This invention relates to a process for the co-encapsulation of biocidally active ingredients in a clay mineral, the process comprising the step of bringing the clay mineral into contact with a biocidally active nitrogen compound that contains at least one hydrocarbon group with 6 to 20 carbon atoms, and at the same time or subsequently with at least one biocidally active compound selected from the group consisting of 2-n-octyl-4-isothiazoline-3-one, 3-iodopropenylbutyl-carbamate and tetrahis(hydroxymethyl)phosphonium sulfate. And the use of such encapsulated product in water based paints, coatings and varnishes.
    Type: Application
    Filed: February 15, 2011
    Publication date: December 13, 2012
    Applicant: CLARIANT S.A. BRAZIL
    Inventors: Antonio Pedro de Oliveira Filho, Wagner Claudio Da Silva, Manlio Gallotti, Alexandra Paschoalin Menezes, Karine Framesqui Righi, Marcia Regina Da Silva Rios
  • Inhibitors of fatty acid amide hydrolase
    Patent number: 8329675
    Abstract: The present invention provide compounds, and pharmaceutical compositions thereof, encompassed by the formulae (I), (II) or (III). The present invention also provides methods for treating an FAAH mediated disease, disorder or condition by administering a therapeutically effective amount of a provided compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof. Additionally, the present invention provides methods for inhibiting FAAH in a patient by administering a therapeutically effective amount of a compound of the formulae (I), (II) or (III), or a pharmaceutical composition thereof, to a patient in need thereof.
    Type: Grant
    Filed: March 16, 2011
    Date of Patent: December 11, 2012
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Julian Adams, Mark L. Behnke, Alfredo C. Castro, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Tao Liu, Daniel A. Snyder, Thomas T. Tibbitts
  • Tumor necrosis factor inhibitors
    Patent number: 8318699
    Abstract: The present invention is directed to compounds that are allosteric inhibitors of tumor necrosis factor receptor I, compositions comprising such compounds, and methods of using such compounds and compositions thereof in the treatment of TNF-? mediated conditions.
    Type: Grant
    Filed: January 31, 2006
    Date of Patent: November 27, 2012
    Assignees: The Trustees Of The University Of Pennsylvania, Cephalon, Inc.
    Inventors: Mark I Greene, Ramachandran Murali, Xin Cheng, Raphael Ottenbrite, Yingxin Xiao
  • BORON-CONTAINING SMALL MOLECULES AS ANTIPROTOZOAL AGENTS
    Publication number: 20120295875
    Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Application
    Filed: October 19, 2010
    Publication date: November 22, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Huchen Zhou, Dazhong Ding, Daoan Sun, Yasheen Zhou, Yong-Kang Zhang, Jacob J. Plattner
  • Combination Therapy With Organic Arsenicals
    Publication number: 20120295861
    Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-I or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-I in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-I and another therapeutic agent.
    Type: Application
    Filed: July 26, 2012
    Publication date: November 22, 2012
    Applicant: ZIOPHARM ONCOLOGY, INC.
    Inventors: Barbara P. WALLNER, Philip B. KOMARNITSKY
  • COFERONS AND METHODS OF MAKING AND USING THEM
    Publication number: 20120295874
    Abstract: The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes one or more pharmacophores which potentially binds to a target molecule with a dissociation constant of less than 300 ?M and a linker element connected to the pharmacophore. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to the pharmacophore.
    Type: Application
    Filed: October 7, 2010
    Publication date: November 22, 2012
    Applicants: CORNELL UNIVERSITY, COFERON, INC., PURDUE RESEARCH FOUNDATION
    Inventors: Francis Barany, Maneesh Pingle, Sarah Filippa Giardina, Donald Bergstrom, Lee Daniel Arnold
  • Compositions and Methods of Use for Livestock Pen Spray
    Publication number: 20120288488
    Abstract: Compositions and methods for preventing or controlling bacteria, viruses and parasitic growths that cause diarrhea, pneumonia and septicemia in animals comprising a biocidal system comprised of a primary biocide and a pH buffer component; a cationic or ionic surfactant having an HLB of from about 5 to about 30; a thickening agent; and an aqueous based carrier.
    Type: Application
    Filed: January 9, 2012
    Publication date: November 15, 2012
    Applicant: NOBLE ION, LLC
    Inventors: Burt R. Sookram, John W. Veenstra
  • Compositions and Methods for Promoting Epithelialization and Wound Closure
    Publication number: 20120289463
    Abstract: Compositions for antagonizing phosphorylation and subsequent degradation of glycogen synthase kinase 3 beta (GSK3?) in epidermal cells are disclosed. GSK3? phosphorylation antagonists include molecules that function to inhibit or reduce the binding activity or enzymatic activity of an upstream signaling molecule leading to GSK3? phosphorylation, or by downregulating the expression of one or more upstream signaling molecules involved in regulating GSK3? phosphorylation. Methods of using the GSK3? phosphorylation antagonists to inhibit or reduce the phosphorylation and degradation of GSK3? in epidermal cells are provided. The methods are useful to promote epithelialization and closure of wounds, such as chronic non-healing wounds.
    Type: Application
    Filed: December 29, 2010
    Publication date: November 15, 2012
    Applicant: New York University
    Inventors: Marjana Tomic-Canic, Harold Brem
  • CANFOSFAMIDE MONOTHERAPY FOR TREATING MULTIPLE MYELOMA
    Publication number: 20120288554
    Abstract: Provided herein are methods for treating multiple myeloma by administering canfosfamide or a pharmaceutically acceptable salt thereof as a monotherapy, and also by administering canfosfamide or a pharmaceutically acceptable salt thereof as part of novel combination therapies further comprising one or more of bortezomib, lenalidomide, vorinostat, carfilzomib, pomalidomide, and elotuzumab.
    Type: Application
    Filed: May 12, 2011
    Publication date: November 15, 2012
    Inventor: Gail L. Brown
  • METHODS OF SENSITIZING CANCER TO THERAPY-INDUCED CYTOTOXICITY
    Publication number: 20120282168
    Abstract: The present application demonstrates that Salinosporamide A can be used to sensitize cancer cells to cancer therapy. Furthermore, the present application demonstrates that Salinosporamide A acts as a therapeutic agent to kill or inhibit cancer cells after sensitization of the cells by an antibody or other chemosensitizing reagents. The cancer cells can be either therapy-sensitive or therapy resistant. The present application further demonstrates that Salinosporamide A induces the expression of Raf kinase inhibitor protein (RKIP) and PTEN, tumor suppressor proteins, and inhibits the expression of YY1, a transcriptional regulator protein overexpressed in cancer cells and also inhibits the growth factor pleiotrophin (PTN).
    Type: Application
    Filed: April 26, 2012
    Publication date: November 8, 2012
    Applicants: Nereus Pharmaceuticals, Inc., The Regents of the University of California
    Inventors: Benjamin BONAVIDA, Michael PALLADINO
  • Boronic acid aryl analogs
    Patent number: 8304579
    Abstract: The present invention relates to novel boronic acid aryl derivatives which are useful as antitumor/anticancer agents. The present compounds, which are inexpensive to synthesize, exhibit unexpectedly good inhibitors of the growth of human breast cancer cells. The present invention also relates to the use of the novel boronic acid aryl derivatives to treat cancer. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of cancer.
    Type: Grant
    Filed: November 5, 2010
    Date of Patent: November 6, 2012
    Assignee: Johns Hopkins University
    Inventor: Saeed R. Khan
  • THERAPEUTIC COMBINATION COMPRISING A CDC7 INHIBITOR AND AN ANTI-NEOPLASTIC AGENT
    Publication number: 20120276093
    Abstract: The present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.
    Type: Application
    Filed: November 17, 2010
    Publication date: November 1, 2012
    Applicant: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Dario Ballinari, Antonella Ciavolella, Enrico Pesenti, Alessia Montagnoli
  • Arginine Derivatives with NP-I Antagonistic Activity
    Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Proteasome inhibitors and processes for their preparation, purification and use
    Publication number: 20120270840
    Abstract: The invention provides boronic esters of Formula I wherein R1, R2, R3, and R4 are as described herein, and methods for the preparation and purification thereof.
    Type: Application
    Filed: June 20, 2012
    Publication date: October 25, 2012
    Applicant: Cephalon Inc.
    Inventor: Renee Caroline Roemmele
  • Therapeutic applications of fatty acid amide hydrolase inhibitors
    Patent number: 8293724
    Abstract: Fatty acid amide hydrolase (FAAH) is an enzyme responsible for the degradation of oleamide (an endogenous sleep-inducing lipid) and anandamide (an endogenous ligand for cannabinoid receptors). Disclosed herein are potent inhibitors of FAAH and methods for their use for treating a variety of disorder, including hypertension and cardiac hypertrophy.
    Type: Grant
    Filed: April 6, 2010
    Date of Patent: October 23, 2012
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: George Kunos, Alexandros Makriyannis
  • BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS
    Publication number: 20120264714
    Abstract: Methods of treating anti-inflammatory conditions through the use of boron-containing small molecules are disclosed.
    Type: Application
    Filed: April 23, 2012
    Publication date: October 18, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: Stephen J. BAKER, Virginia SANDERS, Tsutsomu AKAMA, Carolyn BELLINGER-KAWAHARA, Yvonne FREUND, Kirk R. MAPLES, Jacob J. PLATTNER, Yong-Kang ZHANG, Huchen ZHOU, Vincent S. HERNANDEZ
  • SUBSTITUTED AMINOQUINOXALINES AS TYROSINE THREONINE KINASE INHIBITORS
    Publication number: 20120263708
    Abstract: The present invention relates to substituted aminoquinoxaline compounds of general formula (I) in which (II), R2, R3, R4, R6, R7, n and m are as given in the description and in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds, to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, as well as to intermediate compounds useful in the preparation of said compounds.
    Type: Application
    Filed: August 24, 2010
    Publication date: October 18, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Benjamin Bader, Ulf Bömer, Stuart Ince, Marcus Koppitz, Philip Lienau, Tobias Marquardt, Duy Nguyen, Stefan Prechtl, Gerhard Siemeister, Christof Wegscheid-Gerlach
  • SUBSTITUTED HALOPHENOXYBENZAMIDE DERIVATIVES
    Publication number: 20120263714
    Abstract: The present invention relates to substituted halophenoxybenzamide derivative compounds of general formula (I) in which R1, R2, R3, R3a, R4, R5, R6, Ra, Rb, Rc, and X are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: October 12, 2010
    Publication date: October 18, 2012
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Marion Hitchcock, Ingo Hartung, Florian Pühler, Gerhard Siemeister, Roland Neuhaus
  • PHARMACEUTICAL CO-CRYSTALS OF QUERCETIN
    Publication number: 20120258170
    Abstract: A co-crystal composition comprised of Quercetin and at least one antidiabetic agent acts as a combination drug having unique physical properties and biological activity, which differ from both Quercetin in pure form and the at least one antidiabetic agent in pure form. The co-crystal composition may comprise quercetin and metformin. The co-crystals of quercetin and metformin may be prepared by grinding the compounds, and used in pharmaceutical compositions comprising these co-crystals. Co-crystal compositions of quercetin and Metformin may be used in combination with other anti-diabetic agents, including DPP-IV inhibitors.
    Type: Application
    Filed: March 19, 2012
    Publication date: October 11, 2012
    Applicant: Nutracryst Therapeutics Private Limited
    Inventors: Anil Kumar KRUTHIVENTI, Iqbal Javed, Satyanarayana Reddy Jaggavarapu, RaviKumar Nagalapalli, Ganesh Saraswatula Viswanadha, Solomon Kamalakaran Anand
  • COMBINATION
    Publication number: 20120258933
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof.
    Type: Application
    Filed: February 8, 2012
    Publication date: October 11, 2012
    Inventor: Rakesh KUMAR
  • EZATIOSTAT FOR TREATING MULTIPLE MYELOMA
    Publication number: 20120251496
    Abstract: Ezatiostat is useful for inhibiting multiple myeloma cell proliferation and treating multiple myeloma, alone or when added together with another anti-myeloma drug.
    Type: Application
    Filed: March 20, 2012
    Publication date: October 4, 2012
    Inventor: Michael M. Wick
  • Methods of Treating Cancer with Glut Inhibitors
    Publication number: 20120252749
    Abstract: Methods of treating cancer comprising administering inhibitors of glucose transporters (GLUTs) are provided. Methods of predicting whether a cancer will respond to treatment with a GLUT inhibitor also are provided.
    Type: Application
    Filed: March 30, 2012
    Publication date: October 4, 2012
    Applicant: NORTHWESTERN UNIVERSITY
    Inventors: Malathy Shanmugam, Samuel K. McBrayer, Steven T. Rosen
  • Boron dipyrromethene difluoro (BODIPY) conjugates
    Patent number: 8277775
    Abstract: The present invention relates to FTY720 analogs bearing a boron dipyrromethene difluoro (BODIPY) fluorophore in the alkyl side chain and methods of preparation. The compounds of the present invention can be used in fluorescence spectroscopy and fluorescence microscopy and in chromatography using fluorescence detection.
    Type: Grant
    Filed: August 15, 2008
    Date of Patent: October 2, 2012
    Assignee: The Research Foundation of the City University of New York
    Inventors: Robert Bittman, Zaiguo Li
  • Boroxine composition for removal of skin changes
    Patent number: 8278289
    Abstract: The present invention relates to the field of skin disorders, particularly to the prevention and/or treatment of benignant or malignant changes of the epidermis visible in form of e.g. nevus. A pharmaceutical, dermatological and/or cosmetic composition is disclosed comprising as active constituent the boroxine compound. The present invention further provides the respective uses of the boroxine compound in medicine, particularly in the field of skin disorders, and in dermatological and/or cosmetic applications.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: October 2, 2012
    Inventor: Borivoj Galic
  • DIAZENIUMDIOLATED COMPOUNDS, PHARMACEUTICAL COMPOSITIONS, AND METHOD OF TREATING CANCER
    Publication number: 20120238518
    Abstract: Disclosed is a method of treating cancer in a patient comprising administering to the patient an effective amount of a diazeniumdiolated (N2O2-containing) compound or a pharmaceutically acceptable salt thereof, wherein the cancer cell has an elevated level of reactive oxygen species (ROS) and/or a decreased level of one or more of PRX1, PRX6, and OGG1, compared to a normal cell of the same tissue or tissue type. An example of a diazeniumdiolated compound is Formula (I), wherein X and Q are defined herein. Also disclosed are diazeniumdiolated compounds, pharmaceutical compositions, and methods of use including enhancing the chemotherapeutic treatment of chemotherapeutic agents and high energy radiation.
    Type: Application
    Filed: November 12, 2010
    Publication date: September 20, 2012
    Applicant: The United States of America, as represented by the Secretary, Dept of Health and Human Services
    Inventors: Anna E. Maciag, Larry K. Keefer, Joseph E. Saavedra, Lucy M. Anderson, Harinath Chakrapani
  • Methods for Treating Autoimmune Disorders, and Reagents Related Thereto
    Publication number: 20120232004
    Abstract: The invention generally relates to improved methods for the treatment or prophylaxis in animal subjects (including humans) of autoimmune disorders including Type I diabetes, septic shock, multiple sclerosis, inflammatory bowel disease (IBD) and Crohn's disease.
    Type: Application
    Filed: March 14, 2012
    Publication date: September 13, 2012
    Applicants: The Brigham and Women's Hospital, Trustees Of Tufts College
    Inventors: William W. Bachovchin, Vijay K. Kuchroo
  • NEW SYNTHETIC ROUTE FOR THE PREPARATION OF ALPHA-AMINO BORONIC ACID DERIVATIVES via SUBSTITUTED ALK-1-YNES
    Publication number: 20120231993
    Abstract: The present invention relates in general to the field of organic chemistry and in particular to the preparation of ?-amino boronic acid derivatives.
    Type: Application
    Filed: June 18, 2010
    Publication date: September 13, 2012
    Applicant: LEK PHARMACEUTICALS D.D.
    Inventors: Ivana Gazic Smilovic, Zdenko Casar
  • Stable bortezomib formulations
    Patent number: 8263578
    Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
    Type: Grant
    Filed: March 27, 2012
    Date of Patent: September 11, 2012
    Assignee: InnoPharma, Inc.
    Inventors: Kumaresh Soppimath, Satish Pejaver, Kanaiyalal R. Patel, Lakkaraju Dasaradhi, Rama Sodum, Hari Desu, Navneet Puri
  • HETEROCYCLIC COMPOUNDS FOR THE INHIBITION OF PASK
    Publication number: 20120225846
    Abstract: Disclosed herein are new heterocyclic compounds and compositions 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: Application
    Filed: March 2, 2012
    Publication date: September 6, 2012
    Applicant: BIOENERGENIX
    Inventors: John M. McCall, Donna L. Romero, Michael Clare
  • PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND COMPOSITION FOR PREVENTION AND TREATMENT OF OSTEOPOROSIS CONTAINING SAME
    Publication number: 20120220550
    Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.
    Type: Application
    Filed: September 2, 2010
    Publication date: August 30, 2012
    Applicant: EWHA UNIVERSITY- INDUSTRY COLLABORATION FOUNDATION
    Inventors: Yun Soo Bae, Jee Hyun Lee, Mi Sun Seo, Soo Young Lee, Sun Choi, Kee In Lee, Hye Rin Bin, Do Min Lee
  • Hyperthermic technologies and therapeutic uses thereof
    Patent number: 8252772
    Abstract: The present invention provides nanoscale and microscale compositions useful for a variety of purposes, including the diagnosis and treatment of diseases. In one embodiment, the present invention provides a disease treatment system comprising a thermal induction agent and a radiation source, wherein the thermal induction agent comprises at least one carbon nanotube, at least one carbon microtube, or a mixture thereof.
    Type: Grant
    Filed: May 25, 2007
    Date of Patent: August 28, 2012
    Assignee: Wake Forest University
    Inventors: Suzy Torti, Frank Torti, David Loren Carroll, Steven Akman, Omkaram Nalamasu, Pulickel Ajayan
  • Combination therapy with organic arsenicals
    Patent number: 8252773
    Abstract: The invention provides a combination therapy wherein one or more other therapeutic agents are administered with an organic arsenical, preferably SGLU-1 or a pharmaceutically acceptable salt thereof. The invention also relates to methods for the treatment of cancer, comprising administering SGLU-1 in combination with another therapeutic agent. Another aspect of the invention relates to a kit comprising SGLU-1 and another therapeutic agent.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: August 28, 2012
    Assignee: Ziopharm Oncology, Inc.
    Inventors: Barbara P. Wallner, Philip B. Komarnitsky
  • Methods and Compositions for Treating Cancer Using Proteasome Inhibitors
    Publication number: 20120214757
    Abstract: The present invention relates to therapeutic compositions for treating cancer or preventing the growth of cancer cells, e.g., tumor growth, in a subject. The present invention also relates to methods for treating cancer, e.g., inhibiting tumor growth, in a subject who has become resistant to treatment, by administering to a subject an effective amount of a proteasome inhibitor and an effective amount of a therapeutic agent, e.g., a chemotherapeutic agent. The present invention further relates to methods for purging bone marrow, i.e., removing cancer cells from bone marrow, by exposing the bone marrow cells to a proteasome inhibitor and a therapeutic agent, e.g., a chemotherapeutic agent.
    Type: Application
    Filed: September 23, 2011
    Publication date: August 23, 2012
    Applicant: Dana-Farber Cancer Institute, Inc.
    Inventors: Kenneth C. Anderson, Teru Hideshima, Constantine S. Mitsiades, Nicholas Mitsiades
  • BORON-CONTAINING SMALL MOLECULES AS ANTI-INFLAMMATORY AGENTS
    Publication number: 20120214765
    Abstract: Compounds and methods of treating anti-inflammatory conditions are disclosed.
    Type: Application
    Filed: September 19, 2011
    Publication date: August 23, 2012
    Applicant: Anacor Pharmaceuticals, Inc.
    Inventors: 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 T. Jacobs, Daitao Chen, Michael Richard Kevin Alley
  • Imidazoquinolines as lipid kinase inhibitors
    Publication number: 20120207751
    Abstract: The invention relates to a combination comprising compounds of formula (I) and one or more other antiproliferative compounds, hormones or radiation, pharmaceutical preparations comprising the combination thereof, and the application thereof in a process for the treatment of tumors.
    Type: Application
    Filed: April 23, 2012
    Publication date: August 16, 2012
    Applicant: NOVARTIS AG
    Inventors: Carlos Garcia-Echeverria, Frédéric Stauffer, Pascal Furet
  • SUBSTITUTED INDOLE AND AZAINDOLE OXOACETYL PIPERAZINAMIDE DERIVATIVES
    Publication number: 20120202775
    Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.
    Type: Application
    Filed: August 4, 2011
    Publication date: August 9, 2012
    Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
  • ROS-sensitive iron chelators and methods of using the same
    Patent number: 8236783
    Abstract: The present invention provides compounds of Formula (I): along with compositions containing the same and methods of use thereof in treating oxidative stress.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: August 7, 2012
    Assignee: Duke University
    Inventors: Katherine J. Franz, Louise K. Charkoudian
  • Compositions Comprising Thalidomide and Artemisinin for the Treatment of Cancer
    Publication number: 20120190646
    Abstract: The present invention relates to pharmaceutical compositions for the treatment of cancer and especially for the treatment of hematological malignancies such as multiple myeloma. Specifically, the present invention relates to pharmaceutical composition for the treatment of cancer comprising: thalidomide, or a derivative thereof, or salts or solvates thereof; one or more artemisinin compounds, or salts or solvates thereof; and one or more pharmaceutically acceptable carriers and/or excipients.
    Type: Application
    Filed: July 27, 2010
    Publication date: July 26, 2012
    Inventor: Frans Herwig Jansen
  • USE OF INHIBITORS OF BRUTON'S TYROSINE KINASE (BTK)
    Publication number: 20120183535
    Abstract: Disclosed herein are methods for treating a cancer comprising: a. administering a Btk inhibitor to a subject sufficient to result in an increase or appearance in the blood of a subpopulation of lymphocytes defined by immunophenotyping; b. determining the expression profile of one or more biomarkers from one or more subpopulation of lymphocytes; and c. administering a second agent based on the determined expression profile.
    Type: Application
    Filed: December 29, 2011
    Publication date: July 19, 2012
    Applicant: Pharmacyclics, Inc.
    Inventors: Joseph J. Buggy, Laurence Elias, Gwen Fyfe, Eric Hedrick, David J. Loury, Tarak D. Mody
  • SOFT PROTEASE INHIBITORS, AND PRO-SOFT FORMS THEREOF
    Publication number: 20120178677
    Abstract: 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. Another aspect of the invention provides for the use of the disclosed compounds for treating Type II diabetes, insulin resistance, glucose intolerance, hyperglycemia, hypoglycemia, hyperinsulinemia, obesity, hyperlipidemia, or hyperlipoproteinemia.
    Type: Application
    Filed: March 1, 2010
    Publication date: July 12, 2012
    Applicant: Trustees of Tufts College
    Inventors: William W. Bachovchin, Hung-sen Lai, Wengen Wu
  • Stable Bortezomib Formulations
    Publication number: 20120172808
    Abstract: Multi-dose formulations for bortezomib are presented in which bortezomib has significantly improved stability. Especially preferred formulations include those in which bortezomib is in a liquid form suitable for injection, wherein the solvent system predominantly comprises propylene glycol. In other preferred aspects, bortezomib is present as a Lewis donor-acceptor complex with a hetero-bifunctional Lewis base.
    Type: Application
    Filed: March 27, 2012
    Publication date: July 5, 2012
    Applicant: INNOPHARMA, LLC
    Inventors: Kumaresh Soppimath, Satish Pejaver, Kanaiyalal R. Patel, Lakkaraju Dasaradhi, Rama Sodum, Hari Desu, Navneet Puri
  • SUBSTITUTED BENZIMIDAZOLONE DERIVATIVES, MEDICAMENTS COMPRISING THEM AND THEIR USE
    Publication number: 20120172335
    Abstract: The present invention relates to novel benzimidazolone derivatives of the general formula (I) in which the substituents R1, R2, R3, A1, A2, and B are as defined in claim 1, medicaments comprising these, and the use thereof for the prophylaxis and/or treatment of vasopressin-dependent diseases.
    Type: Application
    Filed: November 22, 2011
    Publication date: July 5, 2012
    Inventors: Torsten Arndt, Thorsten Oost, Wilfried Lubisch, Wilfried Homberger, Liliane Unger, Juliana Ruiz Caro, Wolfgang Wernet, ALfred Hahn
  • SINGLE STEP CREOSOTE/BORATE WOOD TREATMENT
    Publication number: 20120171504
    Abstract: Disclosed is a method of reducing insect and microbial decay in wood. The method comprises the steps of: a) immersing the wood in a treatment solution comprising i) a C1-C6monoalkanolamine ester of boric acid (e.g., monoethanolamine ester of boric acid) and ii) creosote; and b) exposing the immersed wood from step a) to conditions which cause the release of boron from the C1-C6 monoalkanolamine ester of boric acid (monoethanolamine ester of boric acid) and which cause the boron to migrate into the interior of the wood.
    Type: Application
    Filed: January 3, 2011
    Publication date: July 5, 2012
    Inventor: Gordon Murray
  • Arginase Inhibitors and Methods of Use Thereof
    Publication number: 20120171116
    Abstract: The present invention includes arginase enzyme inhibitors, compositions comprising these arginase inhibitors, and methods of treating or diagnosing conditions characterized either by abnormally high arginase activity or abnormally low nitric oxide levels in a mammal, comprising administering compositions of the invention to the mammal.
    Type: Application
    Filed: July 26, 2011
    Publication date: July 5, 2012
    Inventors: Bruce Edward Tomczuk, Gary Lee Olson, Richard Scott Pottorf, Jane Wang, Bhaskara Rao Nallaganchu
  • PYRAZINAMIDE FOR IMMUNOSTIMULATION AND THE TREATMENT OF LEISHMANIASES
    Publication number: 20120157396
    Abstract: Applicants claim the use of a pyrazine compound of formula I: or a salt thereof, for treating or preventing leishmaniases, and diseases and disorders caused by Trypanosoma cruzi or Trypanosoma brucei, and for inducing immunostimulation.
    Type: Application
    Filed: November 21, 2011
    Publication date: June 21, 2012
    Applicants: THE RESEARCH FOUNDATION OF STATE UNIVERSITY OF NEW YORK, UNITED STATES GOVERMENT AS REPRESENTED BY THE DEPARTMENT OF VETERANS AFFAIR, CORNELL UNIVERSITY
    Inventors: John T. WELCH, Susana MENDEZ, Michael H. CYNAMON