Nitrogen Attached To The Acid Group Directly Or Indirectly By Acyclic Nonionic Bonding (e.g., N-hydroxy Ureas, Dihydroxamic Acids, Etc.) Patents (Class 562/623)
  • Publication number: 20150018424
    Abstract: The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities.
    Type: Application
    Filed: October 6, 2014
    Publication date: January 15, 2015
    Inventors: Vinayak G. Gore, Madhukar S. Patil, Rahul A. Bhalerao, Hemant M. Mande, Sandeep G. Mekde
  • Publication number: 20150018331
    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 such compounds.
    Type: Application
    Filed: March 24, 2014
    Publication date: January 15, 2015
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Publication number: 20150018566
    Abstract: The invention provides combretastatin A-4 like compounds that are modified to have enhanced tubulin binding activity and in some embodiments the ability to promote accumulation in the vasculature undergoing angiogenesis (homing activity). The compounds are based on the combretastatin A-4 skeletal structure having a tubulin-binding pharmacophore comprising two fused rings (A and B rings) in which the B ring is substituted with (a) an aromatic ring structure (C ring) and (b) a second substituent/functional group that comes off the B ring. The aromatic ring structure is typically a six membered ring phenolic or aniline structure, or may also be a fused ring structure such as a substituted or unsubstituted naphthalene.
    Type: Application
    Filed: August 27, 2012
    Publication date: January 15, 2015
    Inventors: John Jarlath Walsh, Richard Shah, Emmet Martin McCormack, Gillian Joy Hudson, Martina White, Gary Daniel Stack, Brian William Moran, Adrian Coogan, Elaine Carmel Breen
  • Patent number: 8901337
    Abstract: Compounds comprising a metal complex having the structure [X—Y—Z-Mn+]p+.B are disclosed in which X is a histone deacetylase inhibitor, Mn+ is a DNA-binding heavy metal ion, Y is an aliphatic or aromatic spacer or is absent, and Z is a mono- or bi-dentate or chelating donor linker, or a bridging linker, P+ designates the charge on the complex ion, which may be positive, negative or absent and B is a counterion or is absent. The linker Z is labile and its metal complex X—Y—Z-Mn+ is capable of being hydrolysed in-vivo. The compounds find application in the treatment of cancer.
    Type: Grant
    Filed: July 13, 2010
    Date of Patent: December 2, 2014
    Assignee: Royal College of Surgeons in Ireland
    Inventors: Celine Josephine Marmion, Darren Griffith
  • Publication number: 20140288119
    Abstract: This invention provides a compound having the structure: wherein R1 is H, halogen, —NR5R6, —NR5—C(?O)—R6, —NH—C(?O)—OR7, —OR7, —NO2, —CN, —SR7, —SO2R7, —CO2R7, CF3, —SOR7, —POR7, —C(?S)R7, —C(?O)—NR5R6, —CH2—C(?O)—NR5R6, —C(?NR5)R6, —P(?O)(OR5)(OR6), —P(OR5)(OR6), —C(?S)R7, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, aryl, heteroaryl, or heterocyclyl, wherein R5, R6, and R7 and are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; m is an integer from 0 to 2; R2 and R3 are each, independently, H, halogen, —NH2, —CX3, —C(?O)OR8, C(?O)R8, —C(?O)NR9R10, C1-10 alkyl, C2-10 alkenyl, C2-10 alkynyl, heteroalkyl, aryl, heteroaryl, or heterocyclyl; wherein X is Cl, Br, or F; R8, R9 and R10 are each, independently, H, C1-5 alkyl, C2-5 alkenyl, C2-5 alkynyl, heteroalkyl, cycloalkyl, heterocycloalkyl, aryl, or heteroaryl; Q is —Ar1—Z— or —Z—Ar1—Z—, wherein Ar1 is aryl or heteroaryl; and each occurrence of Z is independently present or
    Type: Application
    Filed: October 3, 2012
    Publication date: September 25, 2014
    Applicants: The Trustees of Columbia University in the City of New York, SLOAN-KETTERING INSTITUTE FOR CANCER RESEARCH
    Inventors: Ronald Breslow, Paul A. Marks
  • Patent number: 8841291
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Grant
    Filed: September 30, 2013
    Date of Patent: September 23, 2014
    Assignee: Novartis AG
    Inventors: Leslie Wighton McQuire, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
  • Patent number: 8779175
    Abstract: A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.
    Type: Grant
    Filed: May 26, 2010
    Date of Patent: July 15, 2014
    Assignee: Synthonics, Inc.
    Inventors: Thomas Piccariello, John D. Price, Robert A. Oberlender, Michaela E. Mulhare, Mary C. Spencer, Scott B. Palmer
  • Publication number: 20140142189
    Abstract: Provided are methionine analogs which may be useful for inhibiting protein synthesis, inhibiting microbial growth and/or treating infectious diseases. In some instances, the analogs exhibit bactericidal, antibacterial, anti-infective, antimicrobial, sporicidal, disinfectant, antifungal and/or antiviral properties. Also provided are methods of treatment and methods of preparation, as well as kits and unit dosages.
    Type: Application
    Filed: October 7, 2013
    Publication date: May 22, 2014
    Applicant: BIOXINESS PHARMACEUTICALS, INC.
    Inventors: Mansour BASSIRI, Afsaneh RAHIMI-LARIJANI
  • Patent number: 8664182
    Abstract: Methods of inhibiting cancer cell growth using HDAC10 inhibitors are provided. Methods of treating cancer in a subject using HDAC10 inhibitors are also provided. In certain embodiments, at least one second inhibitor selected from an autophagy inhibitor, an AMPK inhibitor, and methyl pyruvate is also used in the methods. Dose packs comprising HDAC10 inhibitors and at least one second inhibitor are provided. Methods of identifying HDAC10 inhibitors are also provided.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: March 4, 2014
    Assignee: Duke University
    Inventors: Tso-pang Yao, Hitoshi Sasajima, Yoshiharu Kawaguchi, Kai Cui, Chun-Hsiang Lai
  • Publication number: 20140045943
    Abstract: Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 13, 2014
    Applicant: Naurex, Inc.
    Inventor: Naurex, Inc.
  • Publication number: 20140031399
    Abstract: The present invention provides a compound of formula (I): said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Application
    Filed: September 30, 2013
    Publication date: January 30, 2014
    Inventors: Leslie Wighton MCQUIRE, Olivier ROGEL, Michael SHULTZ, Ruben Alberto TOMMASI, Sven WEILER
  • Patent number: 8633228
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(?G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Grant
    Filed: June 29, 2009
    Date of Patent: January 21, 2014
    Assignee: Mitsui Chemicals Agro, Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • Patent number: 8450525
    Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).
    Type: Grant
    Filed: October 21, 2008
    Date of Patent: May 28, 2013
    Assignee: Orchid Chemicals & Pharmaceuticals Limited
    Inventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Karnambaram Anandhan, Sriram Rajagopal, Rajendran Praveen, Prabhu Daivasigamani
  • Publication number: 20130072677
    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.
    Type: Application
    Filed: April 20, 2011
    Publication date: March 21, 2013
    Applicants: 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
  • Publication number: 20130018103
    Abstract: In recognition of the need to develop novel therapeutic agents and efficient methods for the synthesis thereof, the present invention provides novel bifunctional, trifunctional, or multifunctional 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 an inventive compound to a subject in need thereof. The present invention also provides methods for preparing compounds of the invention.
    Type: Application
    Filed: July 16, 2012
    Publication date: January 17, 2013
    Applicants: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard College
    Inventors: James Elliot Bradner, Ralph Mazitschek, Weiping Tang, Stuart S. Schreiber
  • Publication number: 20120190693
    Abstract: The present invention relates to novel “reverse amide” compounds comprising a zinc chelator group, and the use of such compounds in the inhibition of HDAC6 and in the treatment of various diseases, disorders or conditions related to HDAC6.
    Type: Application
    Filed: April 2, 2012
    Publication date: July 26, 2012
    Inventors: John H. van Duzer, Ralph Mazitschek, Walter Ogier, James E. Bradner, Guoxiang Huang, Dejian Xie, Nan Yu
  • Publication number: 20120190874
    Abstract: Compounds comprising a metal complex having the structure [X—Y—Z-Mn+]p+.B are disclosed in which X is a histone deacetylase inhibitor, Mn+ is a DNA-binding heavy metal ion, Y is an aliphatic or aromatic spacer or is absent, and Z is a mono- or bi-dentate or chelating donor linker, or a bridging linker, P+ designates the charge on the complex ion, which may be positive, negative or absent and B is a counterion or is absent. The linker Z is labile and its metal complex X—Y—Z-Mn+ is capable of being hydrolysed in-vivo. The compounds find application in the treatment of cancer.
    Type: Application
    Filed: July 13, 2010
    Publication date: July 26, 2012
    Applicant: ROYAL COLLEGE OF SURGEONS IN IRELAND
    Inventors: Celine Josephine Marmion, Darren Griffith
  • Publication number: 20120157462
    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: Application
    Filed: January 30, 2008
    Publication date: June 21, 2012
    Inventors: Alan T. Johnson, Guan-Sheng Jiao
  • 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: 20120004309
    Abstract: Disclosed are amino alkyl/aryl hydroxamic acid compounds and pharmaceutical compositions containing such compounds. The disclosed compositions are useful as therapeutics for degenerative diseases in mammal.
    Type: Application
    Filed: May 31, 2011
    Publication date: January 5, 2012
    Inventors: Amin Khan, Paul Wood, Joseph Moskal
  • Publication number: 20110312007
    Abstract: Provided are compositions and methods for intracellular detection of enzyme activity. One example of a composition is a histone deacetylase substrate comprising a compound of the following formula (I): One example of a method is a method for detecting histone deacetylase activity comprising introducing a compound according to formula (I) to a plurality of cells and monitoring the cells with magnetic resonance spectroscopy.
    Type: Application
    Filed: August 1, 2011
    Publication date: December 22, 2011
    Inventors: Sabrina M. Ronen, Juri G. Gelovani, William G. Bornmann, Jihai Pang, Ashutosh Pal, William P. Tong, David S. Maxwell, Madhuri Sankaranarayanapillai
  • Publication number: 20110311654
    Abstract: The present invention comprises methods and pharmaceutical compositions for intranasal delivery of effective amounts of DFO directly to the CNS, in particular the brain treatments that inhibit GSK3b in patients with psychiatric disorders including, but not limited to, bipolar disorder, depression, ADHD and schizophrenia. In addition a treatment composition is disclosed which comprises DFO and in certain embodiments combines DFO with one or more of the psychotropic drug types, i.e., antipsychotics, mood stabilizers and antidepressants. Moreover, a treatment for treating impairment of neural plasticity through inhibition of GSK3b is provided as well as prevention of apoptosis of cells through inhibition of GSK3b.
    Type: Application
    Filed: June 16, 2011
    Publication date: December 22, 2011
    Applicant: HealthPartners Research Foundation
    Inventors: Leah Ranae Bresin Hanson, William H. Frey, II
  • Publication number: 20110269838
    Abstract: The present invention relates to crystalline forms of the active pharmaceutical ingredient vorinostat, processes for their preparation and their use in pharmaceutical compositions.
    Type: Application
    Filed: November 25, 2009
    Publication date: November 3, 2011
    Inventors: Vinayak Gore, Madhukar Patil, Rahul Bhalerao, Hemant Mande
  • Publication number: 20110263712
    Abstract: The present invention relates to an improved process for the preparation of the active pharmaceutical ingredient vorinostat. In particular it relates to a process for preparing vorinostat substantially free from impurities, involving suberic acid, aniline and hydroxylamine as starting materials.
    Type: Application
    Filed: October 14, 2009
    Publication date: October 27, 2011
    Applicant: Generics (UK) Limited
    Inventors: Vinayak G. Gore, Madhukar S. Patil, Rahul A. Bhalerao, Hemant M. Mande, Sandeep G. Mekde
  • Publication number: 20110237832
    Abstract: Embodiments herein relate to histone deacetylaces (HDACs) and HDAC inhibitors, such as trichostatin A (TSA) and TSA analogues. Embodiments provide simple methods of synthesizing TSA and TSA analogues. These methods provide routes of synthesis of TSA and TSA analogues that enable the production of the HDAC inhibitors at lower cost and in greater quantities than previously were available.
    Type: Application
    Filed: February 16, 2011
    Publication date: September 29, 2011
    Applicant: University of Notre Dame du Lac
    Inventors: Paul Helquist, Douglas Schauer, Casey C. Cosner, Vijaya B.R. Iska, Anamitra Chatterjee, Olaf Wiest
  • Patent number: 7989660
    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: August 10, 2007
    Date of Patent: August 2, 2011
    Assignees: Novartis Vaccines and Diagnostics, Inc., University of Washington
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20110172174
    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: Application
    Filed: October 31, 2007
    Publication date: July 14, 2011
    Inventors: Niels H. Andersen, Jason Bowman, Alice Erwin, Eric Harwood, Toni Kline, Khisimuzi Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
  • Publication number: 20110136878
    Abstract: A pest control agent containing a compound represented by the following Formula (1), wherein A represents a carbon atom, a nitrogen atom, or the like, K represents a non-metal atom group necessary for forming a cyclic linking group derived from a 5- or 6-membered aromatic ring, in combination with A and two carbon atoms to which A bonds, X represents a hydrogen atom, a halogen atom, or the like, n represents an integer of from 0 to 4, T represents —C(=G1)-Q1 (wherein G1 and G2 represent an oxygen atom or the like, Q1 represents a phenyl group which may have a substituent, a heterocyclic group which may have a substituent, or the like), or the like, Q2 represents a phenyl group or the like, G3 represents an oxygen atom or the like, and R1 and R2 each independently represent a hydrogen atom, a C1-C6 alkyl group, or a group represented by -L-D, or the like (provided that at least either R1 or R2 represents a group represented by -L-D); as an active ingredient exhibits an excellent effect.
    Type: Application
    Filed: June 29, 2009
    Publication date: June 9, 2011
    Applicant: Mitsui Chemicals Agro., Inc.
    Inventors: Yumi Kobayashi, Hiroyuki Katsuta, Michikazu Nomura, Hidetaka Tsukada, Atsushi Hirabayashi, Hidenori Daido, Yusuke Takahashi, Shinichi Banba
  • 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
  • Publication number: 20110112076
    Abstract: The present invention provides a compound of formula (I) said compound is inhibitor of MMP-12 and/or MMP-13, and thus can be employed for the treatment of a disorder or disease characterized by abnormal activity of MMP-12 and/or MMP-13. Accordingly, the compound of formula (I) can be used in treatment of disorders or diseases mediated by MMP-12 and/or MMP-13. Finally, the present invention also provides pharmaceutical composition that include the compound of formula (I).
    Type: Application
    Filed: July 13, 2009
    Publication date: May 12, 2011
    Inventors: Leslie Wighton McQuire, Olivier Rogel, Michael Shultz, Ruben Alberto Tommasi, Sven Weiler
  • Publication number: 20110105572
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is a C5-20heteroaryl or C5-20carboaryl group and is optionally substituted; Q1 is a C2-7alkylene group having a backbone of at least 2 carbon atoms, and is optionally substituted; J is —N(R1)C(?O)— or —C(?O)N(R1)—; R1 is hydrogen, C1-7alkyl, C3-20heterocyclyl, or C5-20aryl; and, Q2 is C1-7alkylene, C5-20arylene, C5-20arylene-C1-7alkylene, or C1-7alkylene-C5-20arylene having a backbone of at least 3 carbon atoms, and is optionally substituted; and pharmaceutically acceptable salts thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to treat proliferative conditions, such as cancer and psoriasis.
    Type: Application
    Filed: January 4, 2011
    Publication date: May 5, 2011
    Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma M. Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E.S. Duffy
  • Patent number: 7884242
    Abstract: New N-heterocyclylphthaldiamides of structure (I) in which n, A, Q1, Q2, R1 and X have the meanings given in the description, several methods for the preparation of these substances and their use for the control of pests, as well as new intermediates and methods for their preparation.
    Type: Grant
    Filed: November 5, 2005
    Date of Patent: February 8, 2011
    Assignee: Bayer CropScience AG
    Inventors: Rüdiger Fischer, Christian Funke, Olga Malsam, Tetsuya Murata, Katsuaki Wada, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Christian Arnold
  • Publication number: 20100324025
    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: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    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
  • Publication number: 20100273847
    Abstract: The present invention relates to desferoxamine conjugates, derivatives and analogues thereof. In particular, the present invention relates to desferoxamine conjugates, analogues and derivatives thereof, and methods for reducing levels of metals, especially iron, in a mammal. Uses of the compounds according to the invention are also provided. Compounds of the present invention may also be used to treat iron dyshomeostasis disorders, cancer, malaria and fungal infections. The compounds of the invention may be formulated into a pharmaceutical composition or packaged into kits.
    Type: Application
    Filed: October 31, 2008
    Publication date: October 28, 2010
    Inventors: Rachel Codd, Liam Grant Schipanski
  • Publication number: 20100249197
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the formula (1) wherein: A is an aryl group; Q1 is an aryl leader group having a backbone of at least 2 carbon atoms; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; and, Q2 is an acid leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g.
    Type: Application
    Filed: June 3, 2009
    Publication date: September 30, 2010
    Inventors: Clare J. Watkins, Maria Rosario Romero-Martin, Kathryn G. Moore, James Ritchie, Paul W. Finn, Ivars Kalvinsh, Einars Loza, Igor Starchenkov, Klara Dikovska, Rasma Bokaldere, Vija Gailite, Maxim Vorona, Victor Andrianov, Daina Lolya, Valentina Semenikhina, Andris Amolins, C. John Harris, James E.S. Duffy
  • Publication number: 20100247454
    Abstract: The present invention describes therapeutic compositions comprising one or more minerals, including trivalent iron, divalent manganese and salts thereof, suitable in facilitating synthesis and deposition of connective tissue matrix, particularly rich of elastin and collagen, and mitogenic potential in human dermal fibroblasts. It also describes the phenomenon in which stimulation of elastogenesis by arterial SMC associates with a net decrease in proliferation of these cell types. The present invention also describes methods of treatment of human skin fibroblasts and arterial smooth muscle cells. The therapeutic compositions of the present invention comprise one or more of trivalent iron or divalent manganese or salts thereof and may be combined with an elastic tissue digest.
    Type: Application
    Filed: January 12, 2010
    Publication date: September 30, 2010
    Inventors: Thomas Mitts, Felipe Jimenez, Aleksander Hinek, Severa Bunda
  • Publication number: 20100240601
    Abstract: A coordination complex having a physiologically acceptable pKa includes a metal and a biologically active agent. The pKa of the coordination complex is less than the pKa of the biologically active agent. A pharmaceutical solution for treating a patient includes a coordination complex and water, wherein the coordination complex is at least partially soluble in the water at physiological pH and in a therapeutically efficacious concentration. A method for treating a patient includes administering a pharmaceutical solution including a coordination complex and water to a patient in need of a biologically active agent.
    Type: Application
    Filed: May 26, 2010
    Publication date: September 23, 2010
    Inventors: Thomas Piccariello, John D. Price, Robert A. Oberlender, Michaela E. Mulhare, Mary C. Spencer, Scott B Palmer
  • Publication number: 20100190766
    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 such compounds.
    Type: Application
    Filed: December 10, 2009
    Publication date: July 29, 2010
    Applicant: Achaogen, Inc.
    Inventors: Heinz E. Moser, Qing Lu, Phillip A. Patten, Dan Wang, Ramesh Kasar, Stephen Kaldor, Brian D. Patterson
  • Publication number: 20100145034
    Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.
    Type: Application
    Filed: August 14, 2009
    Publication date: June 10, 2010
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Alina Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
  • Publication number: 20090297417
    Abstract: Disclosed are methods and apparatus enabling the efficient utilization of urea for purposes such as selective catalytic reduction (SCR) of NOx, which enable feeding urea to a chamber designed to efficiently and completely gasify the urea to enable ammonia feed. Preferably, aqueous urea is fed to a gasification chamber, which is also fed with heated gases. An injector means, capable of distributing the aqueous urea as fine droplets, is positioned centrally of a gas distribution plate in the chamber. An arrangement of spaced holes in the gas distribution plate provides higher gas velocity in the vicinity of the injector means than near the walls of the chamber. Uniform gas distribution without equipment fouling is achieved.
    Type: Application
    Filed: May 27, 2009
    Publication date: December 3, 2009
    Applicant: FUEL TECH, INC.
    Inventors: William H. Sun, John M. Boyle, Ronald A. Lau
  • Patent number: 7504436
    Abstract: The present invention relates to novel bioisosteres of the antibiotic actinonin of the general formula (I). The novel compounds are of particular interest as inhibitors of metalloproteinases.
    Type: Grant
    Filed: May 7, 2004
    Date of Patent: March 17, 2009
    Assignee: Novartis AG
    Inventors: Michael Thormann, Michael Almstetter
  • Patent number: 7498358
    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: December 13, 2002
    Date of Patent: March 3, 2009
    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: 7407988
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (1) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
    Type: Grant
    Filed: September 7, 2006
    Date of Patent: August 5, 2008
    Assignee: Topotarget UK Limited
    Inventors: Ivars Kalvinsh, Einars Loza, Vija Gailite
  • Publication number: 20080176916
    Abstract: The invention relates to ?-amino-N-hydroxy-acetamide derivatives of formula I, wherein R is di-lower alkyl amino, 1,2,3-triazol-1-yl, 1,2,3-triazol-2-yl or 1,2,4-triazol-4-yl, m represents an integer from 1 up to and including 10, and n represents an integer from 0 up to and including 10, and salts thereof: to processes for their preparation, pharmaceutical compositions comprising said hydroxamic acid derivatives, the use of such hydroxamic acid derivatives as medicaments, and a method of treating conditions or diseases mediated by matrix-degrading metalloproteinases (MMP's) using said derivatives alone or in combination with one or more other therapeutic agents.
    Type: Application
    Filed: October 5, 2007
    Publication date: July 24, 2008
    Inventors: Kenji Hayakawa, Genji Iwasaki, Shinichi Koizumi, Ichiro Umemura
  • Patent number: 7399884
    Abstract: Histone deacetylase inhibitors and uses thereof are provided that have the general formula wherein R1, R2, R3 and R4 are each independently selected from the group consisting of hydrogen, a substituted or unsubstituted straight chained C1-12 alkyl, C2-12 aminoalkyl or C2-12 oxaalkyl, and a substituted and unsubstituted 3, 4, 5, 6, 7 or 8 membered ring, with the proviso that R3 and R4 are not both hydrogen; R5 is selected from the group consisting of a carbonyl, a substituted or unsubstituted C1-3 alkyl, a substituted or unsubstituted —C1-3 alkyl-C(O), a substituted or unsubstituted —C(O)—C1-3 alkyl, and a substituted or unsubstituted —C(O)C(O)C1-3 alkyl; M is a substituent capable of complexing with a protein metal ion; and L is a substituent comprising a chain of 3-12 atoms connecting the M substituent to the carbon atom alpha to the L substituent.
    Type: Grant
    Filed: November 7, 2006
    Date of Patent: July 15, 2008
    Assignee: Takeda San Diego, Inc.
    Inventors: Jerome C. Bressi, Sheldon X. Cao, Jeffrey A. Stafford, Phong H. Vu
  • Publication number: 20080070954
    Abstract: The present invention relates to hydroxamate compounds which are inhibitors of histone deacetylase. More particularly, the present invention relates to acylurea/sulfonylurea containing compounds and methods for their preparation. These compounds 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 activities.
    Type: Application
    Filed: October 26, 2004
    Publication date: March 20, 2008
    Applicant: S*BIO PTE LTD.
    Inventors: Ze-Yi Lim, Haishan Wang, Yan Zhou
  • Patent number: 7323448
    Abstract: Compounds of formula (I) or a pharmaceutically or veterinarily acceptable salts thereof wherein R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10-(ALK)m-, and A represents (i) a group of formula (IA): wherein the compounds inhibit the activity of bacterial PDF enzyme.
    Type: Grant
    Filed: August 2, 2006
    Date of Patent: January 29, 2008
    Assignee: British Biotech Pharmaceuticals Ltd.
    Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
  • Patent number: 7282496
    Abstract: Compounds of the formula are useful in treating disease conditions mediated by TNF-?, such as rheumatoid arthritis, osteoarthritis, sepsis, AIDS, ulcerative colitis, multiple sclerosis, Crohn's disease, degenerative cartilage loss, graft rejection, cachexia, inflammation, fever, insulin resistance, septic shock, congestive heart failure, inflammatory disease of the central nervous system, inflammatory bowel disease and HIV.
    Type: Grant
    Filed: November 1, 2002
    Date of Patent: October 16, 2007
    Assignee: Wyeth Holdings Corporation
    Inventors: Vincent Premaratna Sandanayaka, Efren Guillermo Delos Santos
  • Patent number: 7241921
    Abstract: Compounds of formula (I) are antibacterial agents: wherein: Z is —N(OH)CH(?O) or —C(?O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula —N(OH)CH(?O), a hydroxy, halo or amino group; R2, R3 and R4 independently represents hydrogen or a group R10—(D)n—(ALK)m— wherein R10, D, n, m and ALK are as defined in the claims; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which R4 and R5 are attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen
    Type: Grant
    Filed: November 27, 2002
    Date of Patent: July 10, 2007
    Assignee: De Novo Pharmaceuticals Limited
    Inventors: Paul Gane, Barry Porter, Henriette Willems, Raymond Paul Beckett, Kenneth Keavey
  • Patent number: 7183298
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: (I) A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is a sulfonamide linkage selected from: —S(?O)2NR1— and —NR1S(?O)2—; R1 is a sulfonamido substituent; and, Q2 is an acid leader group; with the proviso that if J is —S(?O)2NR1—, then Q1 is an aryl leader group; and pharmaceutically acceptable salts, solvates, amides, esters, ethers, chemically protected forms, and prodrugs thereof. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit HDAC, and, e.g., to inhibit proliferative conditions, such as cancer and psoriasis.
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: February 27, 2007
    Assignee: Topotarget UK Limited
    Inventors: Clare J Watkins, Maria Rosario Romero-Martin, Kathryn G Moore, James Ritchie, Paul W Finn, Ivars Kalvinsh, Einars Loza, Klara Dikovska, Vija Gailite, Maxim Vorona, Irina Piskunova, Igor Starchenkov, Victor Andrianov, C. John Harris, James E. S. Duffy