Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/89)
  • Patent number: 9023850
    Abstract: Disclosed are compounds of Formula 1, N-oxides, and salts thereof, wherein Z is O or S; A1, A2, A3 and A4 are independently N or CR1, provided that only one of A1, A2, A3 and A4 is N; and R1, R2, R3 and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling a parasitic nematode comprising contacting the parasitic nematode or its environment with a biologically effective amount of a compound or a composition of the invention.
    Type: Grant
    Filed: October 5, 2011
    Date of Patent: May 5, 2015
    Assignee: E I du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Francis Pahutski, Jr.
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8962244
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Grant
    Filed: January 8, 2013
    Date of Patent: February 24, 2015
    Assignee: University of Massachusetts
    Inventor: Sean Ryder
  • Publication number: 20150024032
    Abstract: Embodiments of the invention include methods of treating, preventing, and/or reduce the risk or severity of a condition selected from the group consisting of muscle wasting, muscle weakness, cachexia, and a combination thereof in an individual in need thereof. In some embodiments, particular small molecules are employed for treatment, prevention, and/or reduction in the risk of muscle wasting. In at least particular cases, the small molecules are inhibitors of STAT3.
    Type: Application
    Filed: July 18, 2014
    Publication date: January 22, 2015
    Inventors: David J. Tweardy, Moses M. Kasembeli, Marvin X. Xu, Thomas Kristian Eckols
  • Publication number: 20140378681
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: February 26, 2013
    Publication date: December 25, 2014
    Applicant: Siga Technologies Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey, Jack H. Nunberg, Celestine Johnson Thomas
  • Publication number: 20140315946
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 2, 2014
    Publication date: October 23, 2014
    Inventor: Arun K. Ghosh
  • Publication number: 20140315954
    Abstract: Compounds having cytotoxic and/or anti-mitotic activity are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4 and R5 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed. Also disclosed are compositions having the structure: (T)-(L)-(D), wherein (T) is a targeting moiety, (L) is an optional linker, and (D) is a compound having structure (I).
    Type: Application
    Filed: March 14, 2014
    Publication date: October 23, 2014
    Inventors: Geoffrey C. WINTERS, Alexander L. Mandel, BRADLEY J. HEDBERG
  • Patent number: 8859815
    Abstract: A diamine of formula (I) is described in which A is hydrogen or a saturated or unsaturated C1-C20 alkyl group or an aryl group; B is a substituted or unsubstituted C1-C20 alkyl, cycloalkyl, alkaryl, alkaryl or aryl group or an alkylamino group and at least one of X1, X2, Y1, Y2 or Z is a C1-C10 alkyl, cycloalkyl, alkaryl, aralkyl or alkoxy substituting group. The chiral diamine may be used to prepare catalysts suitable for use in transfer hydrogenation reactions.
    Type: Grant
    Filed: December 7, 2011
    Date of Patent: October 14, 2014
    Assignee: Bial-Portela & C.A., S.A.
    Inventors: Beatriz Dominguez, Antonio Zanotti-Gerosa, Gabriela Alexandra Grasa, Jonathan Alan Medlock
  • Publication number: 20140288183
    Abstract: This invention relates to the use of bis- and tris-dihydroxyaryl compounds as well as sulfonamides, heteroaryls, tricycloalkyl and their analogs and pharmaceutically acceptable salts, for modulating tau aggregation and alleviating tauopathies, such as Alzheimer's disease (AD), Pick's disease (PiD), progressive supranuclear palsy (PSP), corticobasal degeneration (CBD) and familial frontotemporal dementia/Parkinsonism linked to chromosome 17 (FTDP-17), amyotrophic lateral sclerosis/Parkinsonism-dementia complex, argyrophilic grain dementia, dementia pugilistic, diffuse neurofibrillary tangles with calcification, progressive subcortical gliosis and tangle only dementia.
    Type: Application
    Filed: June 10, 2014
    Publication date: September 25, 2014
    Inventors: Alan D. Snow, Qubai Hu, Thomas Lake, Judy Cam
  • Publication number: 20140286866
    Abstract: The invention relates to compounds suitable for use in an imaging agent said imaging agent showing an improved pharmacokinetic profile.
    Type: Application
    Filed: June 4, 2014
    Publication date: September 25, 2014
    Applicant: GE HEALTHCARE AS
    Inventors: ALAN CUTHBERTSON, MAGNE SOLBAKKEN
  • Patent number: 8829052
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: September 23, 2011
    Date of Patent: September 9, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Zhi Hong
  • Patent number: 8829198
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Grant
    Filed: October 3, 2008
    Date of Patent: September 9, 2014
    Assignee: Proteotech Inc
    Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan D. Snow, Lesley Larsen
  • Publication number: 20140243362
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators of formula (I), processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR? wherein R1 to R7 are as defined in claim 35.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 28, 2014
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le
  • Patent number: 8808742
    Abstract: This invention relates to compositions, methods for preparing the compositions and methods for treating or preventing diseases, comprising administering the compositions.
    Type: Grant
    Filed: April 14, 2009
    Date of Patent: August 19, 2014
    Assignee: Ardea Biosciences, Inc.
    Inventors: Barry D. Quart, Colin Edward Rowlings
  • Publication number: 20140221231
    Abstract: A method is described that uses ROR gamma t, or ROR alpha to diagnose rosacea and/or to screen inhibitors of Th17 differentiation, notably in inhibiting ROR gamma t or ROR alpha. Also described is a method of using these screened inhibitors in rosacea treatment.
    Type: Application
    Filed: June 25, 2012
    Publication date: August 7, 2014
    Applicant: Galderma Research & Development
    Inventor: Martin Steinhoff
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Publication number: 20140206875
    Abstract: Disclosed are a novel compound or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1). The disclosed compound and the pharmaceutical composition including the same for inhibiting human 11-?-hydroxy steroid dehydrogenase type 1 (11?-HSD1) are excellent in activity and solubility, and is more efficient in formulation and transfer.
    Type: Application
    Filed: August 6, 2012
    Publication date: July 24, 2014
    Applicant: HYUNDAI PHARM CO., LTD.
    Inventors: Inhee Lee, Doohyeok Pyeon, Myounghyeon Shin, Jeongun Hwang, Changmin Park, Sehoan Kim, Heeil Chae, Soonyoung Moon, Soyoun Kim, Jaekeol Rhee
  • Patent number: 8784879
    Abstract: In an aspect of the invention, a composition for making a patch for the transdermal delivery of tamsulosin is provided. The composition comprises (a) at least about 1 wt % tamsulosin or a pharmaceutically acceptable salt of tamsulosin, (b) at least about 40 wt % polyisobutylene adhesive or hydrophobic synthetic rubber adhesive, (c) about 1-20 wt % of an aprotic solvent in which tamsulosin dissolves readily, (d) about 1-20 wt % of an unsaturated fatty acid or an alpha-hydroxy acid or a mixture of unsaturated fatty acids or alpha-hydroxy acids or of both unsaturated fatty acids and alpha-hydroxy acids, (e) a lipophilic permeation enhancer, and (f) a matrix modifier.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: July 22, 2014
    Assignee: Corium International, Inc.
    Inventors: Parminder Singh, Eun Soo Lee, Amit K. Jain
  • Patent number: 8741960
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Grant
    Filed: January 25, 2007
    Date of Patent: June 3, 2014
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Publication number: 20140107160
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: October 9, 2013
    Publication date: April 17, 2014
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul E. Fleming, Geraldine C.B. Harriman, Zhan Shi, B. Shaowu Chen
  • Publication number: 20130244262
    Abstract: The present invention provides a cardiomyocyte- and/or cardiac progenitor cell-proliferating agent comprising at least one compound selected from the group consisting of: a GSK3? inhibitor, ERK dephosphorylation inhibitor, Raf activator, CaMK2 inhibitor and p38 inhibitor; and a method for proliferating cardiomyocytes and/or cardiac progenitor cells using the agent.
    Type: Application
    Filed: November 17, 2011
    Publication date: September 19, 2013
    Applicant: KYOTO UNIVERSITY
    Inventors: Jun Yamashita, Hideki Uosaki
  • Publication number: 20130231332
    Abstract: The present invention relates to compositions and methods for the treatment of infection by enveloped viruses, such as Ebola and Lassa fever viruses.
    Type: Application
    Filed: September 1, 2011
    Publication date: September 5, 2013
    Inventors: James Cunningham, Kyungae Lee, Tao Ren, Kartik Chandran
  • Publication number: 20130172388
    Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.
    Type: Application
    Filed: December 14, 2012
    Publication date: July 4, 2013
    Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher Education
    Inventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
  • Publication number: 20130172295
    Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed
    Type: Application
    Filed: February 27, 2013
    Publication date: July 4, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8431745
    Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed.
    Type: Grant
    Filed: February 21, 2012
    Date of Patent: April 30, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard P. Polniaszek, Richard Hung Chiu Yu
  • Patent number: 8377639
    Abstract: The invention relates to compositions and methods for inhibiting RNA binding proteins (e.g., MEX-3, MEX-5 and POS-1), as well as methods for treating and preventing disorders associated with parasitic infections and inflammatory disorders.
    Type: Grant
    Filed: June 25, 2010
    Date of Patent: February 19, 2013
    Assignee: University of Massachusetts
    Inventor: Sean Ryder
  • Publication number: 20120282180
    Abstract: The present invention relates to the field of therapeutic and diagnostic agents and more specifically to compounds of formula (I) that are inhibitors of matrix-metalloproteinases (MMPs) and are useful in the treatment of diseases related thereto such as cardiovascular diseases, inflammatory diseases and malignant diseases. One embodiment of the invention is a compound of formula (I) labeled with a 18-fluorine atom having matrix metalloproteinase inhibitory activity suitable for diagnostic imaging. Also disclosed in the present invention is a pharmaceutical composition comprising the inhibitors of matrix-metalloproteinases (MMPs) of the invention or the corresponding labeled compounds useful as diagnostic imaging agents of the invention in a form suitable for mammalian administration.
    Type: Application
    Filed: June 8, 2011
    Publication date: November 8, 2012
    Inventors: Hartmuth C. Kolb, Guenter Haufe, Malte Behrends, Klaus Kopka, Stefan Wagner, Verena Hugenberg, Hans-Joerg Breyholz, Sven Hermann, Michael Schaefers
  • Publication number: 20120258935
    Abstract: A process for the synthesis of bisfuran intermediates useful for preparing antiviral HIV protease inhibitor compounds is hereby disclosed
    Type: Application
    Filed: February 21, 2012
    Publication date: October 11, 2012
    Applicant: Gilead Sciences, Inc.
    Inventors: Kenneth R. Crawford, Eric D. Dowdy, Arnold Gutierrez, Richard P. Polniaszek, Richard Hung Chiu Yu
  • Patent number: 8268885
    Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.
    Type: Grant
    Filed: September 10, 2004
    Date of Patent: September 18, 2012
    Assignee: Janssen R&D Ireland
    Inventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
  • Publication number: 20120196884
    Abstract: The present invention relates to sulphonamide derivatives, whith a urea moiety. The invention also relates to the use of the derivatives as inhibitors of collagen receptor integrins, especially ?2?1 integrin inhibitors e.g. in connection with diseases and medical conditions that involve the action of cells and platelets expressing collagen receptors, their use as a medicament, e.g. for the treatment of thrombosis, inflammation, cancer and vascular diseases, pharmaceutical compositions containing them and a process for preparing them. The sulphonamide derivatives have the general formula (I) or (I?).
    Type: Application
    Filed: June 14, 2010
    Publication date: August 2, 2012
    Applicant: BIOTIE THERAPIES CORPORATION
    Inventors: Jarkko Tapani Koivunen, Jani Korhonen, Anne Marjamäki, Liisa Nissinen, Marjo Pihlavisto, Olli Taneli Pentikäinen
  • Patent number: 8232420
    Abstract: The present invention provides an organic metal compound, a ligand, an asymmetric catalyst, and a process for preparing optically-active alcohols using the asymmetric catalyst.
    Type: Grant
    Filed: April 12, 2010
    Date of Patent: July 31, 2012
    Assignee: Kanto Kagaku Kabushiki Kaisha
    Inventors: Masahito Watanabe, Junichi Hori
  • Publication number: 20120065204
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt, ester or stereoisomer thereof, wherein R1 to R3 and X have the significances given herein. The present invention is also directed to processes for making said compounds and uses of said compounds, in particular their use as medicaments, more particularly their use as medicaments in the treatment of cancer.
    Type: Application
    Filed: September 7, 2011
    Publication date: March 15, 2012
    Inventors: Lei Guo, Guozhi Tang, Zhanguo Wang, Jason Christopher Wong, Weixing Zhang
  • Patent number: 8101799
    Abstract: This invention concerns N—(2-arylamino) aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Grant
    Filed: July 30, 2007
    Date of Patent: January 24, 2012
    Assignee: Ardea Biosciences
    Inventors: Andreas Maderna, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoui, Zhi Hong
  • Publication number: 20110313000
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Publication number: 20110294793
    Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.
    Type: Application
    Filed: June 8, 2009
    Publication date: December 1, 2011
    Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
  • Publication number: 20110294775
    Abstract: Novel compounds which are useful for treating acute pain, visceral pain, neuropathic pain, inflammatory/pain receptor-mediated pain, tumour pain and headache diseases.
    Type: Application
    Filed: August 12, 2008
    Publication date: December 1, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
  • Publication number: 20110178123
    Abstract: Novel compounds and compositions for treating patients in need of relief from HIV, AIDS, and AIDS-related diseases are described. Methods for treating HIV, AIDS, and AIDS-related diseases using the compounds described herein are also described.
    Type: Application
    Filed: July 1, 2009
    Publication date: July 21, 2011
    Applicant: PURDUE RESEARCH FOUNDATION
    Inventor: Arun K. Ghosh
  • Publication number: 20110178092
    Abstract: Described are novel protease inhibitors and methods for using said protease inhibitors in the treatment of human immunodeficiency virus (HIV) infection.
    Type: Application
    Filed: December 19, 2007
    Publication date: July 21, 2011
    Inventors: Akbar Ali, Michael D. Altman, Saima G. Anjum, Hong Cao, Sripriya Chellappan, Miguel X. Fernandes, Michael K. Gilson, Visvaldas Kairys, Nancy King, Ellen Nalivaika, Moses Prabu, Tariq M. Rana, Kiran Kumar Sai, Celia A. Schiffer, Bruce Tidor
  • Publication number: 20110166342
    Abstract: A 7-membered heterocyclic compound having the formula (I), or its salt, or a solvate thereof with a chymase inhibitory action and useful for the prevention or treatment of various diseases, in which chymase is involved: a method for producing the same, and a pharmaceutical composition useful for the prevention or treatment of diseases, in which chymase is involved, including the compound of having the formula (I), or its pharmaceutically acceptable salt, or a solvate thereof are provided.
    Type: Application
    Filed: January 4, 2011
    Publication date: July 7, 2011
    Applicant: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Tsuyoshi Muto, Taisaku Tanaka, Hiroshi Maruoka, Seiichi Imajo, Yoshiaki Tomimori
  • Publication number: 20110077231
    Abstract: Novel compounds, with the following being exemplary:
    Type: Application
    Filed: August 12, 2008
    Publication date: March 31, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Walter Rainer
  • Publication number: 20110028509
    Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.
    Type: Application
    Filed: April 8, 2009
    Publication date: February 3, 2011
    Applicant: MERCK SERONO SA
    Inventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
  • Publication number: 20100331380
    Abstract: Dihydroxyaryl compounds and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of ?-amyloid diseases, such as observed in Alzheimer's disease, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.
    Type: Application
    Filed: June 29, 2009
    Publication date: December 30, 2010
    Inventors: Luke A. Esposito, F. Michael Hudson, Thomas Lake, Joel Cummings, Manfred Weigele, Alan Snow, Lesley Larsen
  • Publication number: 20100298439
    Abstract: Described herein are derivatives of arylsulfonamido-substituted hydroxamic acid of formula (I) having good solubility in water and inhibitory activity of matrix metalloproteinases, useful for the preparation of pharmaceutical compositions for the treatment of diseases associated to a pathologic activity and/or an over-expression of metalloproteinases, and of cosmetic preparations having anti-ageing properties in particular for hair and skin.
    Type: Application
    Filed: August 4, 2010
    Publication date: November 25, 2010
    Inventors: Ivano BERTINI, Marco FRAGAI, Mauro LO CONTE, Claudio LUCHINAT, Cristina NATIVI, Chiara VENTURI
  • Publication number: 20100280074
    Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.
    Type: Application
    Filed: December 3, 2009
    Publication date: November 4, 2010
    Applicant: Millennium Pharmaceuticals, Inc.
    Inventors: Paul Fleming, Geraldine C.B. Harriman, Zhan Shi, Shaowu Chen
  • Patent number: 7824918
    Abstract: Novel fluorescent dyes are disclosed for use in analyte detection. In particular, mono- and bis-substituted HPTS dyes and methods of making them are provided.
    Type: Grant
    Filed: August 6, 2008
    Date of Patent: November 2, 2010
    Assignee: Glumetrics, Inc.
    Inventor: Jeff T. Suri
  • Publication number: 20100261924
    Abstract: The present invention provides an organic metal compound, a ligand, an asymmetric catalyst, and a process for preparing optically-active alcohols using the asymmetric catalyst.
    Type: Application
    Filed: April 12, 2010
    Publication date: October 14, 2010
    Applicant: Kanto Kagaku Kabushiki Kaisha
    Inventors: Masahito Watanabe, Junichi Hori
  • Patent number: 7772430
    Abstract: Described herein are derivatives of arylsulfonamido-substituted hydroxamic acid of formula (I) having good solubility in water and inhibitory activity of matrix metalloproteinases, useful for the preparation of pharmaceutical compositions for the treatment of diseases associated to a pathologic activity and/or an over-expression of metalloproteinases, and of cosmetic preparations having anti-ageing properties in particular for hair and skin.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: August 10, 2010
    Assignee: Protera S.R.L.
    Inventors: Ivano Bertini, Marco Fragai, Mauro Lo Conte, Claudio Luchinat, Cristina Nativi, Chiara Venturi
  • Publication number: 20100105894
    Abstract: The present invention provides a compound having aggrecanase inhibitory activity and MMP-13 inhibitory activity, and useful as a therapeutic agent for osteoarthritis, rheumatoid arthritis and the like, more specifically, a cyclopropane compound of formula (1): wherein R1 is —(CH2)m—X—(CH2)n-A1 etc., wherein m and n are the same or different and each is 0 to 6, X is a single bond, etc. and A1 is a substituted C3-14 hydrocarbon ring group, etc.; R2 and R3 are the same or different and each is a hydrogen atom, —(CH2)p—X1—(CH2)q-A2, etc., wherein p and q are the same or different and each is 0 to 6, X1 is a single bond, etc. and A2 is an optionally substituted C3-14 hydrocarbon ring group, etc.; R4 is —CO2R9, etc., wherein R9 is a hydrogen atom, etc.; and R20 and R21 are the same or different and each is a hydrogen atom, —(CH2)m12—X12—(CH2)m12—R30, etc., wherein m12 and m12 are the same or different and each is 0 to 6, X12 is a single bond, etc. and R30 is a hydrogen atom, etc.
    Type: Application
    Filed: June 9, 2009
    Publication date: April 29, 2010
    Inventors: Takashi Inaba, Julia Haas, Makoto Shiozaki, Nicole M. Littmann, Katsutaka Yasue, Steven W. Andrews, Atushi Sakai, Andrew M. Fryer, Takafuml Matsuo, Ellen R. Laird, Akira Suma, Yuichi Shinozaki, Yoshikazu Hori, Hiroto Imai, Tamotsu Negoro
  • Patent number: 7598418
    Abstract: A medicament for enhancing an effect of a cancer therapy based on a mode of action of DNA injury, which comprises as an active ingredient a compound represented by the following general formula (I) or a salt thereof: wherein one of R1 and R2 represents hydrogen atom and the other represents the formula —X-A wherein A represents hydrogen atom or an acyl group, X represents oxgen atom or NH; one of R3 and R4 represents hydrogen atom and the other represents the following formula: wherein Y represents a sulfonyl group or a carbonyl group, R5 represents a cyclic group, Z represents a single bond or a C1 to C4 alkylene group, R6 represents hydrogen atom or a C1 to C6 alkyl group.
    Type: Grant
    Filed: April 18, 2003
    Date of Patent: October 6, 2009
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventors: Susumu Muto, Akiko Itai
  • Patent number: RE45314
    Abstract: The invention relates to N-hydroxysulfonamide derivatives that donate nitroxyl (HNO) under physiological conditions and are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure and ischemia/reperfusion injury. Novel N-hydroxysulfonamide derivatives release NHO at a controlled rate under physiological conditions, and the rate of HNO release is modulated by varying the nature and location of functional groups on the N-hydroxysulfonamide derivatives.
    Type: Grant
    Filed: October 3, 2013
    Date of Patent: December 30, 2014
    Assignees: The Johns Hopkins University, Cardioxyl Pharmaceuticals, Inc.
    Inventors: John P. Toscano, Frederick Arthur Brookfield, Andrew D. Cohen, Stephen Martin Courtney, Lisa Marie Frost, Vincent Jacob Kalish