Phenanthridines (including Hydrogenated) Patents (Class 514/298)
  • Patent number: 10023538
    Abstract: Compounds, compositions and methods useful for treating infectious diseases are provided. In particular, 3-aryl quinoline compounds, their synthesis, pharmaceutical compositions thereof and methods of treating infectious diseases such as malaria, are disclosed.
    Type: Grant
    Filed: February 23, 2017
    Date of Patent: July 17, 2018
    Assignees: The United States of America as represented by the Department of Veterans Affairs, Oregon Health and Science University
    Inventors: Michael K. Riscoe, Rolf W. Winter, Sovitj Pou, David J. Hinrichs, Jane Xu Kelly, Yuexin Li, Aaron Nilsen
  • Patent number: 9962377
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of areata, endogenous acne, exogenous acne or acne rosacea.
    Type: Grant
    Filed: June 10, 2016
    Date of Patent: May 8, 2018
    Assignee: TAKEDA GMBH
    Inventor: Ulrich Kautz
  • Patent number: 9387205
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.
    Type: Grant
    Filed: August 25, 2015
    Date of Patent: July 12, 2016
    Assignee: TAKEDA GMBH
    Inventor: Ulrich Kautz
  • Patent number: 9150540
    Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: October 6, 2015
    Assignee: Janssen Pharmaceutica NV
    Inventors: Patrick Rene Angibaud, Laurence Anne Mevellec, Bruno Roux, Pierre-Henri Storck, Christophe Meyer, Jorge Eduardo Vialard
  • Publication number: 20150119389
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.
    Type: Application
    Filed: October 7, 2014
    Publication date: April 30, 2015
    Inventor: Ulrich KAUTZ
  • Patent number: 9012451
    Abstract: The present invention relates to 1-aza-bicycloalkyl derivatives of formula I, wherein X is CH2 or a single bond; Y is a group of formula and wherein R has the meanings as defined in the specification, which compounds are alpha 7 nicotinic acetylcholine receptor (nAChR) agonists; to processes for their production, their use as pharmaceuticals and to pharmaceutical compositions comprising them.
    Type: Grant
    Filed: May 2, 2012
    Date of Patent: April 21, 2015
    Assignee: Novartis AG
    Inventors: Dominik Feuerbach, Konstanze Hurth, Timothy John Ritchie
  • Publication number: 20150105375
    Abstract: This invention relates to 2-Aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides of formula 1 and their use as inhibitors of Cathepsin C, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of diseases connected with dipeptidyl peptidase I activity, e.g. respiratory diseases.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Inventors: Ralf ANDERSKEWITZ, Florian BINDER, Matthias GRAUERT, Marc GRUNDL, Peter Wilhelm HAEBEL, Thorsten OOST, Alexander PAUTSCH, Stefan PETERS, Viktor VINTONYAK
  • Publication number: 20150038521
    Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.
    Type: Application
    Filed: October 14, 2014
    Publication date: February 5, 2015
    Inventors: Patrick Rene Angibaud, Laurence Anne Mevellec, Bruno Roux, Pierre-Henri Storck, Christophe Meyer, Jorge Eduardo Vialard
  • Patent number: 8889707
    Abstract: The invention discloses methods for preventing or treating addiction by administering to a subject in need thereof a PARP inhibitor.
    Type: Grant
    Filed: February 7, 2013
    Date of Patent: November 18, 2014
    Inventor: Malka Cohen-Armon
  • Publication number: 20140303201
    Abstract: The subject invention provides for cancer therapy.
    Type: Application
    Filed: April 7, 2014
    Publication date: October 9, 2014
    Inventor: Malka COHEN-ARMON
  • Patent number: 8829189
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Grant
    Filed: October 11, 2013
    Date of Patent: September 9, 2014
    Assignee: Takeda GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Patent number: 8754218
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Grant
    Filed: December 7, 2012
    Date of Patent: June 17, 2014
    Assignee: Takeda GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Patent number: 8729080
    Abstract: The subject invention provides for cancer therapy.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: May 20, 2014
    Inventor: Malka Cohen-Armon
  • Publication number: 20140135296
    Abstract: The invention provides methods of treating autophagy mediated diseases and disorders and related pharmaceutical compositions, diagnostics, screening techniques and kits. In one embodiment, the invention provides a method of determining whether a subject suffers from, or is at risk of developing, and autophagy mediated disease state and/or condition by evaluating LC3 levels.
    Type: Application
    Filed: May 10, 2012
    Publication date: May 15, 2014
    Inventors: Vojo Deretic, Eliseo Castillo, Steven Bradfute, Larry A. Sklar
  • Publication number: 20140073636
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of atopic eczema.
    Type: Application
    Filed: April 30, 2013
    Publication date: March 13, 2014
    Applicant: TAKEDA GMBH
    Inventor: Ulrich KAUTZ
  • Publication number: 20140039001
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Application
    Filed: October 11, 2013
    Publication date: February 6, 2014
    Applicant: TAKEDA GMBH
    Inventors: Ulrich KAUTZ, Matthias WEBEL, Christian SCHEUFLER, Rolf-Peter HUMMEL
  • Publication number: 20130296228
    Abstract: Novel compositions and methods of reducing microbial resistance to antimicrobial agents and treating infections are disclosed. In particular, compositions and methods of inhibiting efflux pump activity, treating infection and methods of enhancing antimicrobial activity of antimicrobial agents are provided.
    Type: Application
    Filed: April 22, 2013
    Publication date: November 7, 2013
    Inventors: Mahesh Vithalbhai PATEL, Sachin Subhash Bhagwat, Mohammad Alam Jafri
  • Publication number: 20130237528
    Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
    Type: Application
    Filed: April 25, 2013
    Publication date: September 12, 2013
    Applicant: Janssen Pharmaceutica, NV
    Inventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20130203801
    Abstract: The invention discloses methods for preventing or treating addiction by administering to a subject in need thereof a PARP inhibitor.
    Type: Application
    Filed: February 7, 2013
    Publication date: August 8, 2013
    Inventor: Malka COHEN-ARMON
  • Patent number: 8455653
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.
    Type: Grant
    Filed: October 26, 2012
    Date of Patent: June 4, 2013
    Assignee: Takeda GmbH
    Inventor: Ulrich Kautz
  • Publication number: 20130096152
    Abstract: Disclosed herein are salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical compositions.
    Type: Application
    Filed: December 7, 2012
    Publication date: April 18, 2013
    Applicant: NYCOMED GMBH
    Inventor: NYCOMED GMBH
  • Publication number: 20130045974
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.
    Type: Application
    Filed: October 26, 2012
    Publication date: February 21, 2013
    Applicant: NYCOMED GMBH
    Inventor: NYCOMED GMBH
  • Patent number: 8362028
    Abstract: Pseudobase benzo[c]phenanthridines and the pharmaceutically acceptable salts thereof of Formula I are provided herein. The variables R, R1, R2, R3, and R4 are defined herein. Certain pseudobase benzo[c]phenanthridines provided herein act as prodrugs, targeting the parent benzo[c]phenanthridinium alkaloid to hydrophilic or hydrophobic regions in the body. Pharmaceutical compositions comprising a pseudobase benzo[c]phenanthridine and a carrier, excipient, or diluent are provided herein. Methods of treating or preventing microbial, fungal and or viral infections and methods of treating diseases and disorders responsive to protein kinase C modulation, topoisomerase I, and/or topoisomerase II modulation are also provided.
    Type: Grant
    Filed: April 6, 2009
    Date of Patent: January 29, 2013
    Assignee: Yale University
    Inventors: Kenneth Shaw, Mingbao Zhang, Amy F. T. Arnsten
  • Patent number: 8354535
    Abstract: The invention relates to salts of 6-heteroaryl substituted hexahydrophenanthridine PDE4 inhibiting compounds, which can be used in the pharmaceutical industry for the production of pharmaceutical composition for use, e.g., in treatment of airway disorders.
    Type: Grant
    Filed: March 26, 2010
    Date of Patent: January 15, 2013
    Assignee: Nycomed GmbH
    Inventors: Ulrich Kautz, Matthias Webel, Christian Scheufler, Rolf-Peter Hummel
  • Patent number: 8329685
    Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.
    Type: Grant
    Filed: January 16, 2003
    Date of Patent: December 11, 2012
    Assignee: North West University
    Inventor: Petrus Johannes Meyer
  • Patent number: 8329906
    Abstract: The compounds of a certain formula (1), in which R1, R2, R3, R31, R4, R5, R6 and R7 have the meanings as given in the description, are novel effective PDE4 inhibitors.
    Type: Grant
    Filed: July 27, 2009
    Date of Patent: December 11, 2012
    Assignee: Nycomed GmbH
    Inventor: Ulrich Kautz
  • Publication number: 20120258181
    Abstract: The present invention relates to combinations between artemisinin-based potent anti-malarial agents, selected from the group consisting of ART, DHA and ARM, and a further chemotherapeutic drug selected from the group consisting of a camptothecin derivative, or a PARP-1 inhibitor, or an intercalating DNA agent, or an alkylating agent. Such combinations, showed medium to strong synergism in various models of cancer, in particular in NSCL.
    Type: Application
    Filed: December 6, 2010
    Publication date: October 11, 2012
    Applicant: SIGMA-TAU INDUSTRIE FARMACEUTICHE RIUNITE S.P.A.
    Inventors: Claudio Pisano, Loredana Vesci
  • Publication number: 20120178725
    Abstract: A method of treating or preventing an immune disorder, such as graft versus host disease, in a subject. The method includes the administering a SHIP1 inhibitor, such as 3?-aminocholestane, to a subject in need of treatment. Thus, SHIP1 inhibitors taught herein represent a novel class of small molecules that have the potential to enhance allogeneic transplantation, boost innate immunity and improve the treatment of hematologic malignancies.
    Type: Application
    Filed: April 13, 2011
    Publication date: July 12, 2012
    Applicant: H. Lee Moffitt Cancer and Research Institute, Inc.
    Inventor: William G. Kerr
  • Publication number: 20120129817
    Abstract: The subject matter of this application is directed to combinations of (2R,4aR,10bR)-6-(2,6-Dimethoxy-pyridin-3-yl)-9-ethoxy-8-methoxy-1,2,3,4,4a,10b-hexahydrophenanthridin-2-ol with other active compounds for the treatment of diabetes mellitus type 2 and/or type 1.
    Type: Application
    Filed: February 1, 2012
    Publication date: May 24, 2012
    Applicant: NYCOMED GMBH
    Inventors: Thomas KLEIN, Anja BLASER, Bettina RUDOLPH, Ulrich KAUTZ, Jens SELIGE, Wolfgang KROMER
  • Publication number: 20120129849
    Abstract: The present invention provides deuterated compounds having certain biological activities that include, but are not limited to, inhibiting cell proliferation, modulating protein kinase activity and modulating polymerase activity. The deuterated compounds of the invention can modulate casein kinase (CK) activity and/or poly(ADP-ribose)polymerase (PARP) activity. The invention also relates in part to methods for using such deuterated compounds as therapeutic agents.
    Type: Application
    Filed: September 23, 2011
    Publication date: May 24, 2012
    Applicant: CYLENE PHARMACEUTICALS, INC.
    Inventors: Mustapha HADDACH, David M. Ryckman
  • Publication number: 20120122917
    Abstract: This invention discloses cannabinoid derivatives and pharmaceutical uses thereof.
    Type: Application
    Filed: January 23, 2012
    Publication date: May 17, 2012
    Inventor: Craig Rick Travis
  • Publication number: 20120122916
    Abstract: The invention concerns screening molecules with anti-prion activity. More particularly, it concerns kits for screening molecules with anti-prion activity characterized in that they comprise in combination a [PSI+], phenotype yeast, an antibiogram and an agent for purifying prions at sub-efficient doses, said yeast including the ade1-14 allele of the ADE1 gene and an inactivated ERG6 gene, the screening methods, and a family of molecules with anti-prion activity isolated by the inventive screen. The invention is applicable to anti-prion agents for producing medicines in particular for treating neurodegenerative diseases involving protein aggregates.
    Type: Application
    Filed: December 16, 2011
    Publication date: May 17, 2012
    Applicants: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITE DE POITIERS, UNIVERSITE VICTOR SEGALEN BORDEAUX 2
    Inventors: Marc BLONDEL, Christophe Cullin, Jean Michel Vierfond, Stephane Bach, Nicolas Talarek, Yvette Mettey
  • Patent number: 8129402
    Abstract: The invention concerns screening molecules with anti-prion activity. More particularly, it concerns kits for screening molecules with anti-prion activity characterized in that they comprise in combination a [PSI+], phenotype yeast, an antibiogram and an agent for purifying prions at sub-efficient doses, said yeast including the adel-14 allele of the ADE1 gene and an inactivated ERG6 gene, the screening methods, and a family of molecules with anti-prion activity isolated by the inventive screen. The invention is applicable to anti-prion agents for producing medicines in particular for treating neurodegenerative diseases involving protein aggregates.
    Type: Grant
    Filed: October 20, 2003
    Date of Patent: March 6, 2012
    Assignees: Centre National de la Recherche Scientifique, Universite Victor Segalen Bordeaux 2, Universite de Poitiers
    Inventors: Marc Blondel, Christophe Cullin, Jean Michel Vierfond, Stephane Bach, Nicolas Talarek, Yvette Mettey
  • Publication number: 20120046274
    Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
    Type: Application
    Filed: October 28, 2011
    Publication date: February 23, 2012
    Inventors: Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20120034293
    Abstract: The present invention overcomes the problems associated with existing drug delivery systems by delivering cannabinoids transdermally. Preferably, the cannabinoids are delivered via an occlusive body (i.e., a patch) to alleviate harmful side effects and avoid gastrointestinal (first-pass) metabolism of the drug by the patient.
    Type: Application
    Filed: October 12, 2011
    Publication date: February 9, 2012
    Applicant: AllTranz Inc.
    Inventors: Audra L. Stinchcomb, Buchi N. Nalluri
  • Publication number: 20120022026
    Abstract: The present invention relates to a method of treating or preventing hyperproliferative disease in a body tissue of a subject, comprising the steps of administering to a subject in need thereof a therapeutically effective amount of an agent that induces double strand breaks in the DNA of the hyperproliferative cells of said body tissue; and subjecting the hyperproliferative cells of said body tissue prior to, simultaneously with or subsequent to step a) to hyperthermia to thereby induce in said cells the degradation, inhibition and/or inactivation of BRCA2.
    Type: Application
    Filed: January 13, 2010
    Publication date: January 26, 2012
    Applicants: ERASMUS UNIVERSITY MEDICAL CENTER ROTTERDAM, ACADEMISCH MEDISCH CENTRU BIJ DE UNIVERSITEIT VAN AMSTERDAM
    Inventors: Przemyslaw Krawczyk, Jacob A. Aten, Roland Kanaar, Jeroen Essers
  • Publication number: 20110312918
    Abstract: The present invention provides a novel mechanistic pathway and methods related to this pathway for the identification of compounds for the treatment of diseases involving cell proliferation, invasion and/or metastasis such as cancer. In particular, the instant invention relates to the phosphatase activity of Eya and the Eya-Six complex as a target for identifying novel therapeutic agents for the treatment of proliferative, invasive and/or metastatic disorders, and compositions identified using the methods disclosed herein.
    Type: Application
    Filed: December 8, 2009
    Publication date: December 22, 2011
    Applicant: Children's Hospital Medical Center
    Inventor: Rashmi Hegde
  • Patent number: 8071612
    Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
    Type: Grant
    Filed: November 19, 2010
    Date of Patent: December 6, 2011
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Dominique Jean-Pierre Mabire, Jérôme Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20110268679
    Abstract: Described herein are compositions and methods for preventing and/or treating skin diseases including, but not limited to, psoriasis and atopic dermatitis as well as providing anti-aging benefits which results in reduced appearance of wrinkles and aged skin, improved skin color, treatment of photodamaged skin, improvement in skin's radiance and clarity and finish, and an overall healthy and youthful appearance of the skin, involving aberrant angiogenesis and hyperplasia employing one or more benzo[c]chromen-6-one derivatives.
    Type: Application
    Filed: July 11, 2011
    Publication date: November 3, 2011
    Inventor: David SHERRIS
  • Publication number: 20110268654
    Abstract: The present application provides compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reaction for rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.
    Type: Application
    Filed: November 2, 2009
    Publication date: November 3, 2011
    Applicant: THE GENERAL HOSPITAL CORPORATION
    Inventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder
  • Publication number: 20110269705
    Abstract: The present invention provides a quinolone compound that inhibits the chronic progression of Parkinson's disease or protects dopamine neurons from disease etiology, thereby suppressing the progression of neurological dysfunction, so as to prolong the period of time until L-dopa is administered while also improving neuronal function; the quinolone compound of the invention is represented by Formula (1): wherein: R1 represents hydrogen or the like; R2 represents hydrogen or the like; R3 represents substituted or unsubstituted phenyl or the like; R4 represents halogen or the like; R5 represents hydrogen or the like; R6 represents hydrogen or the like; and R7 represents hydrogen or the like.
    Type: Application
    Filed: December 4, 2009
    Publication date: November 3, 2011
    Applicant: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Otsubo, Takahito Yamauchi, Yuji Ochi
  • Publication number: 20110263622
    Abstract: The present invention provides compounds of formula (I), their use as inhibitors of tubulin polymerization and their use as PARP inhibitors as well as pharmaceutical compositions comprising said compounds of formula (I) wherein R1, R2, R3, R4, R5, R6, R7 and Y have defined meanings.
    Type: Application
    Filed: March 26, 2009
    Publication date: October 27, 2011
    Applicants: JANSSEN-CILAG, JANSSEN PHARMACEUTICA NV
    Inventors: Patrick René Angibaud, Laurence Anne Mevellec, Bruno Roux, Pierre-Henri Storck, Christophe Meyer, Jorge Eduardo Vialard
  • Publication number: 20110257221
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.
    Type: Application
    Filed: May 19, 2011
    Publication date: October 20, 2011
    Applicant: NYCOMED GMBH
    Inventor: Ulrich KAUTZ
  • Publication number: 20110257169
    Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors.
    Type: Application
    Filed: May 19, 2011
    Publication date: October 20, 2011
    Applicant: NYCOMED GmbH
    Inventor: Ulrich KAUTZ
  • Patent number: 8034827
    Abstract: The present invention relates to new phenanthridine derivatives of formula (I), wherein the variables are as defined in the specification, to processes for producing the same, to pharmacological compositions containing the same and to their use in therapy or prevention of painful and inflammatory processes.
    Type: Grant
    Filed: December 19, 2006
    Date of Patent: October 11, 2011
    Assignee: Richter Gegeon Nyrt.
    Inventors: Gyula Beke, Eva Bozo, Gabor Czira, Janos Eles, Sandor Farkas, Katalin Hornok, Eva Schmidt, Eva Szentirmay, Istvan Vago, Monika Vastag
  • Publication number: 20110229408
    Abstract: The present disclosure relates to a sodium iodide symporter (NIS)-repressor binding sites (NRBS) consensus sequence consisting of a DNA molecule having the sequence 5?-T/C(G/A)GCCT(T/C)A(G/A)TTTCCCCA(T/C)CTGT-3?(the “consensus NRBS”). The disclosure further relates to methods of restoring iodide transport in dedifferentiated thyroid cancer cells by interfering with formation or function of the NIS repressor.
    Type: Application
    Filed: March 16, 2010
    Publication date: September 22, 2011
    Inventors: Kenneth AIN, Wei Li
  • Publication number: 20110218210
    Abstract: Provided herein are compounds, compositions and methods for treating disorders mediated by abnormal cellular proliferation and processes for identifying such compounds.
    Type: Application
    Filed: November 3, 2008
    Publication date: September 8, 2011
    Applicant: Taiga Biotechnologies
    Inventors: Yosef Refaeli, Brian Curtis Turner
  • Publication number: 20110144074
    Abstract: This invention provides caspase inhibitors of formula I: wherein Z is oxygen or sulfur; R1 is hydrogen, —CHN2, R, CH2OR, CH2SR, or —CH2Y; between R3 and R4 represents a single or double bond; Y is an electronegative leaving group; R2 is CO2H, CH2CO2H, or esters, amides or isosteres thereof; R3 is a group capable of fitting into the S2 subsite of a caspase enzyme; R4 is a hydrogen or C1-6 alkyl or R3 and R4 taken together form a ring; Ring A and Ring B are each heterocyclic rings, and R and R5 are as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1? secretion.
    Type: Application
    Filed: January 24, 2011
    Publication date: June 16, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Michael Mortimore, Andrew Miller, John Studley, Jean-Damien Charrier
  • Publication number: 20110124673
    Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
    Type: Application
    Filed: November 19, 2010
    Publication date: May 26, 2011
    Inventors: Dominique Jean-Pierre Mabire, Jerôme Emile Georges Guillemont, Jacobus Alphonsus Josephus Van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
  • Publication number: 20110117202
    Abstract: Methods and systems for producing a change in a medium. A first method and system (1) place in a vicinity of the medium at least one upconverter including a gas for plasma ignition, with the upconverter being configured, upon exposure to initiation energy, to generate light for emission into the medium, and (2) apply the initiation energy from an energy source including the first wavelength ?1 to the medium, wherein the emitted light directly or indirectly produces the change in the medium. A second method and system (1) place in a vicinity of the medium an agent receptive to microwave radiation or radiofrequency radiation, and (2) apply as an initiation energy the microwave radiation or radiofrequency radiation by which the agent directly or indirectly generates emitted light in the infrared, visible, or ultraviolet range to produce at least one of physical and biological changes in the medium.
    Type: Application
    Filed: November 10, 2010
    Publication date: May 19, 2011
    Applicants: Immunolight, LLC, Duke University
    Inventors: Frederic A. Bourke, JR., Zakaryae Fathi, Ian Nicholas Stanton, Michael J. Therien, Paul Rath Stauffer, Paolo MacCarini, Katherine Sarah Hansen, Diane Renee Fels, Cory Robert Wyatt, Mark Wesley Dewhirst