Hydroxamic Acids, Chalcogen Analogs Or Salts Thereof (i.e., Compounds Having The -c(=x)-n(r)-xh Group Or The -c(xh)=nxr Group, Wherein R May Be Hydrogen Or Substitution For Hydrogen, The X's In Each Group May Be The Same Or Diverse Chalcogens, And H Of -xh In Each Group May Be Replaced By A Group Ia Or Iia Light Metal, Or By Substituted Or Unsubstituted Ammonium) Patents (Class 562/621)
  • Patent number: 9499477
    Abstract: Provided is a novel compound which is useful as a pharmaceutical composition by inhibiting an LpxC activity, thereby exhibiting potent antimicrobial activity against gram-negative bacteria including Pseudomonas aeruginosa and its drug resistant bacteria. Provided is a hydroxamic acid derivative represented by the following general formula [1] or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 21, 2015
    Date of Patent: November 22, 2016
    Assignees: TOYAMA CHEMICAL CO., LTD., TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Hajime Takashima, Risa Tsuruta, Tetsuya Yabuuchi, Yusuke Oka, Hiroki Urabe, Yoichiro Suga, Masato Takahashi, Fumito Uneuchi, Hironori Kotsubo, Muneo Shoji, Yasuko Kawaguchi
  • Patent number: 9034922
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Grant
    Filed: September 16, 2011
    Date of Patent: May 19, 2015
    Assignees: THE UNIVERSITY OF TOKYO, KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Patent number: 8921424
    Abstract: The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.
    Type: Grant
    Filed: October 27, 2008
    Date of Patent: December 30, 2014
    Assignees: Zhejiang Hisun Pharmaceutical Co. Ltd., Central South University
    Inventors: Niefang Yu, Xiaoyu Liu, Xiaodong Hu
  • Publication number: 20140364398
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives, their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: August 27, 2014
    Publication date: December 11, 2014
    Applicant: PFIZER INC.
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Publication number: 20140315965
    Abstract: The present disclosure relates to novel compounds having vitamin D receptor agonist and histone deacetylase inhibitory efficacy as well as methods for reducing or inhibiting the proliferation of cancer cells or for treating cancer.
    Type: Application
    Filed: December 20, 2012
    Publication date: October 23, 2014
    Inventors: James L. Gleason, John H. White, Dainis Kaldre, Joshua Fischer
  • Patent number: 8816107
    Abstract: Stable complexes are described, formed by mono- and di-functional compounds bound to nanoparticles composed of various types of transition metal oxides and of metals useful in the production processes of different types of new materials (such as for example some types of hydrophile plastics, fibers); processes for the production of the complexes are also described.
    Type: Grant
    Filed: January 3, 2007
    Date of Patent: August 26, 2014
    Assignee: Colorobbia Italia S.p.A.
    Inventors: Giovanni Baldi, Alfredo Ricci, Mauro Comes Franchini, Daniele Bonacchi, Marco Bitossi
  • Patent number: 8796330
    Abstract: The invention relates to the inhibition of histone deacetylase. The invention provides compounds, prodrugs thereof, and methods for inhibiting histone deacetylase enzymatic activity. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.
    Type: Grant
    Filed: December 18, 2007
    Date of Patent: August 5, 2014
    Assignee: Methylgene Inc.
    Inventors: Robert Déziel, Alain Ajamian
  • Publication number: 20140206651
    Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
    Type: Application
    Filed: March 24, 2014
    Publication date: July 24, 2014
    Applicant: Pfizer Inc.
    Inventors: Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
  • Publication number: 20140107166
    Abstract: The present invention provides novel compounds for inhibiting histone deacetylases, and pharmaceutically acceptable salts and derivatives thereof. The present invention further provides methods for treating disorders regulated by histone deacetylase activity (e.g., proliferative diseases, cancer, inflammatory diseases, protozoal infections, hair loss, etc.) comprising administering a therapeutically effective amount of a compound of the invention to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Application
    Filed: February 13, 2012
    Publication date: April 17, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Ralph Mazitschek, James E. Bradner, Melissa Grachan Harman
  • Publication number: 20140081017
    Abstract: The present invention relates to compositions and methods to selectively treat fungal infection. More particularly, the invention relates to compounds, compositions thereof, and methods for selectively enhancing fungal sensitivity to antifungal compounds.
    Type: Application
    Filed: March 14, 2013
    Publication date: March 20, 2014
    Applicant: METHYLGENE INC.
    Inventor: METHYLGENE INC.
  • Patent number: 8642635
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: February 4, 2014
    Assignee: Novartis AG
    Inventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi
  • Publication number: 20130338251
    Abstract: Surface-modified zirconia nanoparticles include zirconia nanoparticles and surface-modifying ligands attached to the zirconia nanoparticles. The ligand includes a hydroxamate functionality, and either a reactive group or an oligomeric group. Reactive groups include chain transfer groups or photoinitiator groups. Oligomeric groups include poly(meth)acrylate or poly(meth)acrylamide groups. Articles can be prepared that include the surface-modified zirconia nanoparticles in an organic matrix.
    Type: Application
    Filed: December 13, 2011
    Publication date: December 19, 2013
    Applicant: 3M INNOVATIVE PROPERTIES COMPANY
    Inventors: Guy D. Joly, Nathan E. Schultz, Babu N. Gaddam
  • Patent number: 8609864
    Abstract: The disclosure includes hydroxamic compounds of Formula I: (I) wherein P, Z, and m are defined herein. Also disclosed is a method for treating a neoplastic disease or an immune disease with these compounds.
    Type: Grant
    Filed: January 7, 2010
    Date of Patent: December 17, 2013
    Assignee: Purdue Pharmaceutical Products, L.P.
    Inventors: Yu Chen, Yi Chen
  • Publication number: 20130177900
    Abstract: A composition for maintaining a function of platelets, the composition comprising, as an active ingredient, a compound represented by the following general formula (I) or a salt thereof, or a solvate thereof: wherein X represents a phenylene group; Y represents any one of a hydrogen atom and —(CH2)mR1; wherein m represents an integer of any one of 0 to 4; and R1 is any one of —NR5COR2, —NR5SO2R2, and —NR3R4; wherein R2 represents any one of a C1 to C6 alkyl group, an aryl group, a C1 to C6 alkoxy group, and the like; R3 and R4 represent a C1 to C6 alkyl group or the like; and R5 represents any one of a hydrogen atom, a C1 to C6 alkyl group, and the like; and Z represents any one of a hydrogen atom and a C1 to C6 alkyl group.
    Type: Application
    Filed: September 16, 2011
    Publication date: July 11, 2013
    Applicants: KAKEN PHARMACEUTICAL CO., LTD., THE UNIVERSITY OF TOKYO
    Inventors: Koji Eto, Ryoko Ohnishi, Hiromitsu Nakauchi, Takahiko Murata
  • Patent number: 8383855
    Abstract: In recognition of the need to develop novel therapeutic agents, the present invention provides novel histone deacetylase inhibitors. These compounds include an ester bond making them sensitive to deactivation by esterases. Therefore, these compounds are particularly useful in the treatment of skin disorders. When the compounds reaches the bloodstream, an esterase or an enzyme with esterase activity cleaves the compound into biologically inactive fragments or fragments with greatly reduced activity Ideally these degradation products exhibit a short serum and/or systemic half-life and are eliminated rapidly. These compounds and pharmaceutical compositions thereof are particularly useful in treating cutaneous T-cell lymphoma, neurofibromatosis, psoriasis, hair loss, skin pigmentation, and dermatitis, for example. The present invention also provides methods for preparing compounds of the invention and intermediates thereto.
    Type: Grant
    Filed: February 14, 2007
    Date of Patent: February 26, 2013
    Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.
    Inventors: James Elliot Bradner, Ralph Mazitschek
  • Patent number: 8377978
    Abstract: The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: April 18, 2012
    Date of Patent: February 19, 2013
    Assignee: Novartis AG
    Inventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi
  • Patent number: 8372885
    Abstract: The present application describes organic compounds of a general formula: and salts, and isomers thereof, wherein R, R2 and R3 are defined in the specification. The compounds are useful for treating a gram-negative bacterial infection.
    Type: Grant
    Filed: September 11, 2009
    Date of Patent: February 12, 2013
    Assignee: Novartis AG
    Inventors: Markus Rolf Dobler, Francois Lenoir, David Thomas Parker, Yunshan Peng, Grazia Piizzi, Sompong Wattanasin
  • Patent number: 8329946
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: December 11, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Patent number: 8329751
    Abstract: The invention relates to aryl-sulphonamido compounds endowed with inhibitory activity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, R4, R5, n and m have the meanings reported in the specification; the invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as therapeutic agents, particularly in the treatment of degenerative disorders.
    Type: Grant
    Filed: March 14, 2008
    Date of Patent: December 11, 2012
    Assignee: Bracco Imaging S.p.A.
    Inventors: Aldo Balsamo, Armando Rossello, Elisa Nuti, Elisabetta Orlandini, Tiziano Tuccinardi
  • Patent number: 8329945
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Grant
    Filed: August 30, 2011
    Date of Patent: December 11, 2012
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Patent number: 8242175
    Abstract: New histone deacetylase inhibitors according to the general formula (I) wherein: Q is a bond, CH2, CH—NR3R4, NR5 or oxygen, X is CH or nitrogen, Y is a bond, CH2, oxygen or NR6, Z is CH or nitrogen, R1, R2 are, independently, hydrogen, halogen, C1-C6 alkyl or C1-C6 haloalkyl, R11, R12 are, independently, hydrogen or C1-C6 alkyl, and R3, R4, R5 and R6 are as further defined in the specification.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: August 14, 2012
    Assignee: DAC S.R.L.
    Inventors: Antonello Mai, Saverio Minucci, Florian Thaler, Gilles Pain, Andrea Colombo, Stefania Gagliardi, Pier Giuseppe Pelicci, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Patent number: 8242174
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of aniline and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: August 14, 2012
    Assignee: PanThera Biopharma LLC
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • Publication number: 20120202777
    Abstract: The present invention is directed to a new class of hydroxamic acid derivatives of Formula I, wherein the variables G, T, D, L, A, X, R1 and R2 are as described hereinabove, and their use as LpxC inhibitors, and more specifically their use to treat bacterial infections.
    Type: Application
    Filed: October 4, 2010
    Publication date: August 9, 2012
    Inventors: Matthew Frank Brown, Anthony Marfat, Michael Joseph Melnick, Usa Reilly
  • Patent number: 8236985
    Abstract: There is provided a compound of formula (I) wherein R1a, R2a, R3, X1 to X6, a, b and c have meanings given in the description, which compounds are useful as, or are useful as prodrugs of, inhibitors of HDAC enzyme activity, and thus, in particular, in the treatment of conditions where inhibition of HDAC enzyme activity is required.
    Type: Grant
    Filed: October 24, 2007
    Date of Patent: August 7, 2012
    Assignee: Imperial Innovations Ltd.
    Inventors: Eric Ofori Aboagye, David Michael Vigushin, Wendy Vigushin, legal representative
  • Publication number: 20120196740
    Abstract: Bi-functional cobalt-containing catalysts useful for making stereo specific compounds and compositions, along with methods of making, and uses thereof in the syntheses of optically pure ?-lactones from aldehydes and ketene are described. Precursors, intermediates, compositions, and particular features of the use if the compositions, such as high enantiomeric selectivity, high yield and low mole percent of catalyst useful are provided.
    Type: Application
    Filed: June 7, 2010
    Publication date: August 2, 2012
    Applicant: UNIVERSITY OF TOLEDO
    Inventor: Yun-Ming Lin
  • Patent number: 8222286
    Abstract: The present invention provides a compound of formula I: or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R6, A1, A2, X1, s and m are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: July 17, 2012
    Assignee: Novartis AG
    Inventors: Yuki Iwaki, Toshio Kawanami, Gary Michael Ksander, Muneto Mogi
  • Patent number: 8153843
    Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: April 10, 2012
    Assignees: University of Washington, Novartis Vaccines and Diagnostics, Inc.
    Inventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Patent number: 8143423
    Abstract: A process for preparing hydroxamic acids is provided. The process comprises reacting an aldehyde with a nitroso compound in the presence of a N-heterocyclic carbene (NHC) catalyst.
    Type: Grant
    Filed: March 20, 2008
    Date of Patent: March 27, 2012
    Assignee: Agency for Science, Technology and Research
    Inventors: Yugen Zhang, Jackie Y. Ying, Jayasree Seayad, Fong Tian Wong, Pranab K. Patra
  • Patent number: 8119692
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of 4-phenyl-4-hydroxy-butyric acid and capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Grant
    Filed: March 28, 2008
    Date of Patent: February 21, 2012
    Assignee: PanThera Biopharma LLC
    Inventors: Alan T. Johnson, Seongjin Kim
  • Publication number: 20120035257
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
    Type: Application
    Filed: March 7, 2011
    Publication date: February 9, 2012
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L. Wiech
  • Patent number: 8093386
    Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: January 10, 2012
    Assignee: Bracco Imaging S.p.A
    Inventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
  • Publication number: 20110319493
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 29, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Publication number: 20110313045
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Application
    Filed: August 30, 2011
    Publication date: December 22, 2011
    Applicant: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Publication number: 20110301028
    Abstract: A method of stimulating germination in plant seeds and/or releasing plant tissue or plant organs from dormancy, comprising applying to a seed, plant, plant organ or plant tissue a compound of formula (I): where: R1 is alkyl or H; R2, R3, R4 and R5 are independently selectable from H, halide, —NO2, —SO2R?, —OH, —Oalkyl where R? is alkyl or aminoalkyl; and/or R1 and R5 are joined as —O(CH2)m—, where m is 1, 2, 3 or 4; R6 is a substituted or non-substituted alkyl, and/or substituted or non-substituted aryl; and n is an integer of 1 to 4.
    Type: Application
    Filed: November 17, 2009
    Publication date: December 8, 2011
    Applicant: SYNGENTA CROP PROTECTION, LLC
    Inventors: Andrew Thompson, Timothy Bugg
  • Publication number: 20110280803
    Abstract: The present invention provides a method for the synthesis of radioiodinated compounds which is advantageous over prior art methods. Using a hydrazine or an aminoxy in place of a primary amine for indirect radioiodination facilitates a much quicker reaction thus reducing reaction time and increasing the yield. In addition, where there are primary amines in the molecule to be radioiodinated, such as the N-terminus of a peptide or lysine residues, reaction at the hydrazine or aminoxy is greatly favoured.
    Type: Application
    Filed: January 29, 2010
    Publication date: November 17, 2011
    Applicant: GE HEALTHCARE UK LIMITED
    Inventors: Michelle Avory, Jane Brown, Peter Brian Iveson
  • Patent number: 8058273
    Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
    Type: Grant
    Filed: June 1, 2010
    Date of Patent: November 15, 2011
    Assignee: DAC S.R.L.
    Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Patent number: 8022249
    Abstract: Compounds useful for the treatment of various metabolic disorders, such as insulin resistance syndrome, diabetes, hyperlipidemia, fatty liver disease, cachexia, obesity, atherosclerosis and arteriosclerosis are disclosed.
    Type: Grant
    Filed: March 31, 2006
    Date of Patent: September 20, 2011
    Assignee: Wellstat Therapeutics Corporation
    Inventors: Shalini Sharma, Reid W. von Borstel
  • Publication number: 20110218221
    Abstract: The present invention relates to compounds represented by formula (I) or composition comprising at least one of such compounds, which are inhibitors of histone deacetylase. The detailed description of these compounds is disclosed in the Description. These compounds and the composition comprising the same may be useful as medicaments for the treatment of proliferative disorders as well as other diseases involving, relating to or associated with enzymes having histone deacetylase (HDAC) activities.
    Type: Application
    Filed: October 27, 2008
    Publication date: September 8, 2011
    Applicants: Zhejiang Hisun Pharmaceutical Co., Ltd., Central South University
    Inventors: Niefang Yu, Xiaoyu Liu, Xiaodong Hu
  • Publication number: 20110218154
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Application
    Filed: February 17, 2011
    Publication date: September 8, 2011
    Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGE
    Inventors: STUART L. SCHREIBER, JACK TAUNTON, CHRISTIAN A. HASSIG, TIMOTHY F. JAMISON
  • Patent number: 7994357
    Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: August 9, 2011
    Assignee: Naturewise Biotech & Medicals Corporation
    Inventors: Chung-Yang Huang, Chia-Nan Chen, Wei-Jan Huang, Chia-Wei Lin, Jing-Shi Huang, Li-Ling Chi, Ai-Ling Chen, Chi-Yun Lee, Yu-Chen Huang
  • Patent number: 7994362
    Abstract: The present invention concerns the discovery that proteins encoded by a family of genes, termed here HDx-related genes, which are involved in the control of chromatin structure and, thus in transcription and translation. The present invention makes available compositions and methods that can be utilized, for example to control cell proliferation and differentiation in vitro and in vivo.
    Type: Grant
    Filed: August 22, 2008
    Date of Patent: August 9, 2011
    Assignee: President and Fellows of Harvard College
    Inventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
  • Patent number: 7951972
    Abstract: The present invention provides compounds useful for inhibiting the ADAM-10 protein. Such compounds are useful in the in vitro study of the role of ADAM-10 (and its inhibition) in biological processes. The present invention also comprises pharmaceutical compositions comprising one or more ADAM-10 inhibitors according to the invention in combination with a pharmaceutically acceptable carrier. Such compositions are useful for the treatment of cancer, arthritis, and diseases related to angiogenesis. Correspondingly, the invention also comprises methods of treating forms of cancer, arthritis, and diseases related to angiogenesis in which ADAM-10 plays a critical role. The invention also provides methods for making bis-aryl ether sulfonyl chlorides and ADAM-10 modulators therefrom.
    Type: Grant
    Filed: February 2, 2009
    Date of Patent: May 31, 2011
    Assignee: Exelixis, Inc.
    Inventors: S. David Brown, Lynne Canne-Bannen, Erick Wang Co, Vasu Jammalamadaka, Rickard George Khoury, Moon Hwan Kim, Donna T. Le, Amy Lew Tsuhako, Morrison B. Mac, Shumeye Mamo, John M. Nuss, Michael P. Prisbylla, Wei Xu
  • Patent number: 7932326
    Abstract: Novel di- and tripodal compounds useful as chelators, intermediates for their production and a method for treating an aqueous solution to remove trivalent metal ions are presented.
    Type: Grant
    Filed: April 16, 2008
    Date of Patent: April 26, 2011
    Assignee: The University of Kentucky Research Foundation
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
  • Patent number: 7902259
    Abstract: Histone deacetylase is a metallo-enzyme with zinc at the active site. Compounds having a zinc-binding moiety, such as, for example, a hydroxamic acid group or a carboxylic acid group, can inhibit histone deacetylase. Histone deacetylase can repress gene expression, including expression of genes related to tumor suppression. Accordingly, inhibition of histone deacetylase can provide an alternate route for treating cancer, hematological disorders, e.g., hemoglobinopathies, and genetic related metabolic disorders, e.g., cystic fibrosis and adrenoleukodystrophy.
    Type: Grant
    Filed: February 17, 2005
    Date of Patent: March 8, 2011
    Assignee: Errant Gene Therapeutics, LLC
    Inventors: Hsuan-Yin Lan-Hargest, Robert J. Kaufman, Norbert L Wiech
  • Patent number: 7879911
    Abstract: Compounds having the formula wherein the symbols have the meaning described in the specification are hydroxamic acid derivatives of phenoxy-acetic acids and analogs capable of inhibiting the lethal effects of infection by anthrax bacteria and are useful in the treatment of poisoning by anthrax.
    Type: Grant
    Filed: January 30, 2008
    Date of Patent: February 1, 2011
    Inventors: Alan T. Johnson, Guan-Sheng Jiao, Seongjin Kim
  • Publication number: 20100286279
    Abstract: The present invention pertains to the general field of chemical synthesis, and more particularly to methods for the synthesis of certain hydroxamic acid compounds, and in particular, (E)-N-hydroxy-3-(3-phenylsulfamoyl-phenyl)-acrylamide, also known as PXD101 and Belinostat®, comprising, for example, the steps of: (SAF) sulfonamide formation; (PURC) optional purification; (AAA) alkenyl-acid addition, comprising: either (i): the steps of, in order: (ACAEA) alkenyl-carboxylic acid ester addition; (PURE) optional purification; and (CAD) carboxylic acid deprotection; or (ii): the step of: (ACAA) alkenyl-carboxylic acid addition; (PURF) optional purification; (HAF) hydroxamic acid formation; and (PURG) optional purification.
    Type: Application
    Filed: September 23, 2008
    Publication date: November 11, 2010
    Applicant: TOPOTARGET UK LIMITED
    Inventors: Helge A. Reisch, Peter Leeming, Prasad S. Raje
  • Publication number: 20100278896
    Abstract: A solid, implantable dosage form comprising a therapeutically active agent in solid form, optionally with one or more pharmaceutically acceptable excipients, wherein the one or more excipients, when present, do not lead to a significant delay or prolongation of the release of active agent, as compared to an equivalent dosage form containing no excipients when tested in vitro.
    Type: Application
    Filed: November 17, 2008
    Publication date: November 4, 2010
    Applicant: UCL BUSINESS PLC
    Inventors: Peng T. Khaw, Stephen Brocchini
  • Publication number: 20100256401
    Abstract: The invention relates to a compound represented by the following formula (I): and pharmaceutically acceptable salts, stereoisomers, enantiomers, prodrugs and solvates thereof. The compounds are useful as an agent for enhancing the neurite outgrowth and preventing or treating of diseases associated with HDAC in particular, tumor or cell proliferative diseases. In particular, the compounds of the invention can be used as an agent for anti-cancer, anti-diabetic, and anti-neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Spinocerebellar Ataxias (SCA), and human spinal muscular atrophy (SMA).
    Type: Application
    Filed: April 3, 2009
    Publication date: October 7, 2010
    Applicant: NatureWise Biotech & Medicals Corporation
    Inventors: Chung-Yang Huang, Chia-Nan Chen, Wei-Jan Huang, Chia-Wei Lin, Jing-Shi Huang, Li-Ling Chi, Ai-Ling Chen, Chi-Yun Lee, Yu-Chen Huang
  • Patent number: 7803800
    Abstract: New inhibitors of histone deacetylases having antitumor activity, and the process of preparation thereof are herein described. These compounds belong to the structural formula (I) where R1 is a linear or branched chain containing at least two conjugated double bonds, A is an optionally substituted phenyl or pyridyl ring, Ar is an aryl or heteroaryl group, and R3 is hydrogen or alkoxyalkyl. The application also describes the use of said compounds in the treatment of diseases associated to the deregulation of histone deacetylases activity, such as tumors, as well as the relevant pharmaceutical compositions for administration to patients requiring said treatment.
    Type: Grant
    Filed: September 30, 2005
    Date of Patent: September 28, 2010
    Assignee: DAC S.R.L.
    Inventors: Saverio Minucci, Pier Giuseppe Pelicci, Antonello Mai, Marco Ballarini, Gaetano Gargiulo, Silvio Massa
  • Patent number: 7763751
    Abstract: This invention is related to hydroxylamino derivatives of the general formula (I) wherein n is 0, 1 or 2; R1 and R2, independently of each other, are H, OH or OCH3; R3 is H or CH3; R4 is H, C1-C3 straight or branched alkyl or, together with R3, forms a five to seven-membered carbocyclic ring; and R5 and R6, independently of each other, are H or C1-C5 straight or branched alkyl and the pharmaceutically acceptable salts or prodrug thereof, for the preparation of medicaments useful for the prevention, treatment and diagnosis of CNS degenerative disorders related to protein misfolding and/or misaggregation. The invention also relates to novel compounds included in formula (I), to a method for preparing said compounds and to pharmaceutical compositions containing them.
    Type: Grant
    Filed: December 10, 2004
    Date of Patent: July 27, 2010
    Assignees: Newron Pharmaceuticals S.p.A., Vicuron Pharmaceuticals Inc.
    Inventors: Carla Caccia, Laura Girola, Petra Karin Kaltofen, Daniele Losi, Patricia Salvati, Enrico Selva, Florian Thaler