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: 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
  • 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
  • Patent number: 7728039
    Abstract: Biphenyl and phenyl-naphthyl compounds bearing a hydroxamic group, which are endowed with antitumor, and anti-angiogenic activity These compounds are therefore particularly useful for the treatment of drug-resistant tumors.
    Type: Grant
    Filed: May 31, 2006
    Date of Patent: June 1, 2010
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Claudio Pisano, Giuseppe Giannini, Loredana Vesci, Franco Zunino, Sabrina Dallavalle, Lucio Merlini, Sergio Penco
  • Publication number: 20100105921
    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: Application
    Filed: March 20, 2008
    Publication date: April 29, 2010
    Inventor: Yugen Zhang
  • Patent number: 7683185
    Abstract: The present invention provides histone deacetylase inhibitors of general formula (I), process for the preparation of such compounds and uses of the compounds in medicine.
    Type: Grant
    Filed: November 18, 2003
    Date of Patent: March 23, 2010
    Assignee: Queen Mary & Westfield College
    Inventors: Simon Joel, Charles Marson, Pascal Savy
  • Publication number: 20090261043
    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: Application
    Filed: April 16, 2008
    Publication date: October 22, 2009
    Inventors: Robert A. Yokel, Wesley R. Harris, Christopher D. Spilling, Chang-Guo Zhan
  • Patent number: 7534918
    Abstract: This invention relates to hydroxamic acid derivatives having a sulfonamide linkage, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
    Type: Grant
    Filed: July 8, 2005
    Date of Patent: May 19, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sandro Belvedere, Joey Lee Methot, Thomas A. Miller, David J. Witter, Jiaming Yan
  • Patent number: 7528260
    Abstract: A method is disclosed for preparing compounds of Formula 1 by combining compounds of Formulae 2 and 3 and a sulfonyl chloride. Also disclosed are compounds of Formula 3, which are useful as starting materials for this method.
    Type: Grant
    Filed: December 6, 2005
    Date of Patent: May 5, 2009
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Rafael Shapiro, Eric de Guyon Taylor, William T. Zimmerman
  • Publication number: 20090105168
    Abstract: The present invention provides methods of ameliorating or reducing the extent of ischemic injury, reperfusion injury, and myocardial infarction, by administering an inhibitor of histone deacetylase enzyme (HDAC) or an inhibitor of DNA methyltransferase enzyme (DNMT).
    Type: Application
    Filed: November 30, 2005
    Publication date: April 23, 2009
    Inventors: Peter J. Gruber, Jonathan A. Epstein, Ibrahim Abdullah
  • Patent number: 7507858
    Abstract: This invention relates to iminodiacetic acid and diamine hydroxamic acid derivatives, that are inhibitors of histone deacetylase (HDAC), and are useful in the prevention and/or treatment of cellular proliferative diseases, for example cancer, autoimmune, allergic and inflammatory diseases, diseases of the central nervous system (CNS) such as neurodegenerative diseases, and in the prevention and/or treatment of restenosis.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: March 24, 2009
    Assignee: Merck & Co., Inc.
    Inventors: Sandro Belvedere, Thomas A. Miller, David J. Witter
  • Patent number: 7504537
    Abstract: A hydroxamic acid derivative represented by the following general formula (1) having selective MMP inhibitory activity, wherein R1 and R2 each represents hydrogen atom, lower alkyl group, lower haloalkyl etc., X represents methylene group or NR3 (R3 represents hydrogen atom, lower alkyl group, etc.), and R4 represents C1˜4 lower alkyl group.
    Type: Grant
    Filed: December 26, 2002
    Date of Patent: March 17, 2009
    Assignee: Dainippon Sumitomo Pharma Co., Ltd.
    Inventor: Yoshihiro Horiuchi
  • 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: 7495022
    Abstract: Disclosed are agents that inhibit histone deacetylase. More specifically, the present invention relates to novel hydroxamic acid derivatives or pharmaceutically acceptable salts thereof for anticancer agents or other therapeutic agents based on their histone deacetylase inhibitory activity.
    Type: Grant
    Filed: April 10, 2003
    Date of Patent: February 24, 2009
    Assignee: SK Chemicals Co., Ltd.
    Inventors: Dae-Kee Kim, Ju Young Lee, Nam Kyu Lee, Jae-Sun Kim, Junwon Lee, Suk Ho Lee, Jin Young Choi, Je Ho Ryu, Nam Ho Kim, Guang-Jin Im, Tae Kon Kim, Jung-Woo Seo, Young-Jue Bang
  • Patent number: 7485750
    Abstract: The present invention provides hydroxamic acid derivatives represented by the formula, having antioxidation, collagen biosynthesis promotion and skin pore contraction effects, and a method for preparation thereof. Further, the present invention provides skin-care external compositions for preventing skin aging, containing said hydroxamic acid derivatives represented by the formula as an active ingredient.
    Type: Grant
    Filed: March 21, 2006
    Date of Patent: February 3, 2009
    Assignee: Amorepacific Corporation
    Inventors: Ho Sik Rho, Heung Soo Baek, Jeong A. Lee, Chang Man Park, Duck Hoo Kim, Ih Soop Chang, Ok Sub Lee
  • Patent number: 7465719
    Abstract: This invention pertains to certain carbamic acid compounds of the formula (I), which inhibit HDAC (histone deacetylase) activity: wherein: J is a linking functional group and is independently:—O —C(?O)— or —C(?O)—O — or —C(?O)—; Cy is a cyclyl group and is independently: C3-20carbocyclyl, C3-20heterocyclyl, or C5-20aryl; and is optionally substituted; Q1 is a cyclyl leader group, and is independently a divalent bidentate group obtained by removing two hydrogen atoms from a ring carbon atom of a saturated monocyclic hydrocarbon having from 4 to 7 ring atoms, or by removing two hydrogen atoms from a ring carbon atom of saturated monocyclic heterocyclic compound having from 4 to 7 ring atoms including 1 nitrogen ring atom or 1 oxygen ring atom; and is optionally substituted; Q2 is an acid leader group, and is independently: C1-8alkylene; and is optionally substituted; or: Q2 is an acid leader group, and is independently: C5-20arylene; C5-20arylene-C1-7alkylene; C1-7alkylene-C5-20arylene; or C1-7alkylene-C5-20ary
    Type: Grant
    Filed: January 19, 2004
    Date of Patent: December 16, 2008
    Assignee: Topotarget UK Limited
    Inventors: Paul W. Finn, Ivars Kalvinsh, Einars Loza, Aleksandrs Gutcaits, Irena Olutnika, Ludmila Serpionova, Vija Gailite, Rasma Bokaldere
  • Publication number: 20080139547
    Abstract: The present invention is directed to certain hydroxamate derivatives that are inhibitors of histone deacetylase and are therefore useful in the treatment of diseases associated with histone deacetylase activity. Pharmaceutical compositions and processes for preparing these compounds are also disclosed.
    Type: Application
    Filed: February 7, 2008
    Publication date: June 12, 2008
    Applicant: PHARMACYCLICS, INC.
    Inventor: Martin SENDZIK
  • 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: 7319163
    Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac arrhythmias, thyrotoxicosis and subclinical hyperthyrodism.
    Type: Grant
    Filed: June 24, 2005
    Date of Patent: January 15, 2008
    Assignee: Karo Bio AB
    Inventors: Johan Malm, Chris Litten, Theresa Apelqvist, Asa Hedfors, Peter Brandt, Karin Edvinsson, Sandra Gordon
  • Patent number: 7319096
    Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: January 15, 2008
    Assignee: Karo Bio AB
    Inventors: Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
  • Patent number: 7282522
    Abstract: The present invention provides hydroxamic acid derivatives which have anti-aging efficacy and a method for preparation thereof. It is further provided skin-care external compositions for preventing skin aging, containing the hydroxamic acid derivatives represented by the formula (I) as an active ingredient.
    Type: Grant
    Filed: August 26, 2004
    Date of Patent: October 16, 2007
    Assignee: Amorepacific Corporation
    Inventors: Ho-Sik Rho, Heung-Soo Baek, Su-Jong Kim, Su-Nam Kim, Byung-Geun Chae, Byoung-Seok Lee, Bae-Hwan Kim, Gyu-Ho Choi, Eui-Dong Son, Hae-Kwang Lee, Hye-Won Lee, Jun-Cheol Cho, Duck-Hee Kim, Ih-Seop Chang, Ok-Sub Lee
  • 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: 7235689
    Abstract: Compounds of formula (I), inhibit TNF? production and may therefore be useful in the treatment of inflammation, of auto-immune diseases, and of pathological conditions which involve excessive production of that cytokine.
    Type: Grant
    Filed: January 7, 2004
    Date of Patent: June 26, 2007
    Assignee: Italfarmaco SpA
    Inventors: Massimo Pinori, Paolo Mascagni, Rocco Mazzaferro, Barbara Vergani
  • Patent number: 7183319
    Abstract: Novel mono- and dihydroxy phenylethylamine derivatives useful in treating melanoma are provided having the formulae (Ia, Ib or Ic). In the above formulae, Ra is hydrogen or —COORb, Rb is hydrogen or C1-6 alkyl; Re and Re independently represent hydrogen and hydroxy, Rf is hydrogen, C1–4? alkyl or halogen, X is —CHOH—, —CH2-oxygen or sulphur, m is zero or 1, W is oxygen or sulphur, and —ODrug, —NHDrug and —N(Drug)2 each represent a residue of a therapeutically active agent. The above compounds are prodrugs which are inactive until metabolised by enzymes expressed by host melanoma cells.
    Type: Grant
    Filed: July 25, 2001
    Date of Patent: February 27, 2007
    Inventors: Patrick Anthony Riley, Andrew Photiou, Tariq Hussain Khan, Helen Mary Isted Osborn, Hugh Malkin
  • Patent number: 7169808
    Abstract: Formula (I) compounds are described, where the groups are defined in the description, as well as processes for their preparation and their use as medicaments, particularly as selective phosphodiesterase IV inhibitors.
    Type: Grant
    Filed: June 15, 2001
    Date of Patent: January 30, 2007
    Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Nicola Fanto′, Maria Ornella Tinti
  • Patent number: 7148198
    Abstract: A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB) and wherein R1 is hydrogen, R2 is n-butyl, benzyl or cyclopentylmethyl, R3 is hydrogen, R4 is tert-butyl, iso-butyl, benzyl or methyl, R5 is hydrogen or methyl and R6 is methyl.
    Type: Grant
    Filed: July 29, 2004
    Date of Patent: December 12, 2006
    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: 7091378
    Abstract: The present invention provides a novel method for the formation of hydroxamic acids comprising reacting under suitable conditions an ester with hydroxylamine in the presence of cyanide anion.
    Type: Grant
    Filed: July 6, 2004
    Date of Patent: August 15, 2006
    Assignee: Janssen Pharmaceutica, N.V.
    Inventors: Chih Yung Ho, Eric David Strobel
  • Patent number: 7067551
    Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.
    Type: Grant
    Filed: November 9, 2004
    Date of Patent: June 27, 2006
    Assignee: Novartis AG
    Inventors: Stacy W Remiszewski, Kenneth W Bair, Richard W Versace, Lawrence B Perez, Michael A Green, Lidia C Sambucetti, Sushil Sharma
  • Patent number: 7019003
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: March 1, 2002
    Date of Patent: March 28, 2006
    Assignee: Smithkline Beecham Corporation
    Inventors: Jia-Ning Xiang, Siegfried B. Christensen, IV, Jinhwa Lee, Daniel J. Mercer
  • Patent number: 7007805
    Abstract: The invention relates to a hydroxamate composition for collection of minerals by froth flotation, the composition including an aqueous mixture of hydroxamate wherein the pH of the composition is at least 11 and a method of collecting mineral values from an aqueous ore slurry by froth flotation.
    Type: Grant
    Filed: January 26, 2004
    Date of Patent: March 7, 2006
    Assignee: Ausmelt Limited
    Inventor: Terence Charles Hughes
  • Patent number: 6967220
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: April 4, 2002
    Date of Patent: November 22, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: Ajita Bhat, Siegfried B. Christensen, IV, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
  • Patent number: 6960685
    Abstract: This invention pertains to certain active carbamic acid compounds which inhibit HDAC activity and which have the following formula: wherein: A is an aryl group; Q1 is a covalent bond or an aryl leader group; J is an amide linkage selected from: —NR1C(?O)— and —C(?O)NR1—; R1 is an amido substituent; X is an ether heteroatom, and is —O— or —S—; and, R2 and R3 are each independently an ether 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 27, 2001
    Date of Patent: November 1, 2005
    Assignee: TopoTarget UK Limited
    Inventors: Clare J Watkins, Maria Rosario Romero-Martin, Paul W Finn, Ivars Kalvinsh, Einars Loza, Daina Lolya, Igor Starchenkov, Rasma M Bokaldere, Valentina Semenikhina, C. John Harris, James E. S. Duffy
  • Patent number: 6888027
    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 27, 2001
    Date of Patent: May 3, 2005
    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
  • Patent number: 6852882
    Abstract: Novel PDF inhibitors and novel methods for their use are provided.
    Type: Grant
    Filed: June 4, 2002
    Date of Patent: February 8, 2005
    Assignee: SmithKline Beecham Corporation
    Inventors: Siegfried B. Christensen, IV, Maxwell D. Cummings, Joseph M. Karpinski
  • Publication number: 20040267015
    Abstract: PDF inhibitors and novel methods for their use are provided.
    Type: Application
    Filed: September 29, 2003
    Publication date: December 30, 2004
    Inventors: Ajita Bhat, Siegfried B. Christensen, James S. Frazee, Martha S. Head, Jack D. Leber, Mei Li
  • Publication number: 20040248943
    Abstract: This invention is in the field of antiinflammatory pharmaceutical agents and specifically relates to compounds, compositions and methods for treating disorders mediated by cyclooxygenase-2 or 5-lipoxygenase, such as inflammation.
    Type: Application
    Filed: July 8, 2002
    Publication date: December 9, 2004
    Applicant: Pharmacia Corporation
    Inventors: John J. Talley, James A. Sikorski, Matthew J. Graneto, Bryan H. Norman, Balekudru Devadas, Hwang-Fun Lu
  • Publication number: 20040242928
    Abstract: Reverse hydroxamic acid derivatives having specific structure represented by a general formula (Ia): 1
    Type: Application
    Filed: March 4, 2004
    Publication date: December 2, 2004
    Inventors: Masanao Shimano, Noriyuki Kamei, Tomohiro Tanaka, Tatsuhiro Harada, Makoto Haino, Akihiko Okuyama, Yoshio Arakawa, Yoshiko Murakami
  • Publication number: 20040235911
    Abstract: Hydroxyamidines and related compounds are provided which are suitable as antibacterial agents.
    Type: Application
    Filed: June 25, 2004
    Publication date: November 25, 2004
    Applicant: Tularik Inc.
    Inventors: Leping Li, Xiaoqi Chen, Pingchen Fan, Jeffrey Thomas Mihalic, Serena Cutler
  • Publication number: 20040220147
    Abstract: This invention relates to novel compounds which are thyroid receptor ligands, preferably antagonists, and to methods for using such compounds in the treatment of cardiac and metabolic disorders, such as cardiac arrhythmias, thyrotoxicosis, subclinical hyperthyrodism and liver diseases.
    Type: Application
    Filed: June 10, 2004
    Publication date: November 4, 2004
    Inventors: Johan Malm, Peter Brandt, Karin Edvinsson, Thomas Ericsson, Sandra Gordon
  • Patent number: 6787522
    Abstract: Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n—(ALK)m— wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, an
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: September 7, 2004
    Assignee: British Biotech Pharmaceuticals
    Inventors: Michael George Hunter, Raymond Paul Beckett, John Martin Clements, Mark Whittaker, Stephen John Davies, Lisa Marie Pratt, Zoe Marie Spavold, Steven Launchbury
  • Publication number: 20040171641
    Abstract: Arylpiperazines of formula (I) useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.
    Type: Application
    Filed: February 26, 2004
    Publication date: September 2, 2004
    Applicant: AstraZeneca AB
    Inventors: Bernard C. Barlaam, Nicholas J. Newcombe, Howard Tucker, David Waterson
  • Publication number: 20040167182
    Abstract: This invention is directed generally to hydroxamic acid and amide compounds (including salts of such compounds), and, more particularly, to aryl- and heteroaryl-arylsulfonylmethyl hydroxamic acids and amides that, inter alia, inhibit protease activity, particularly matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity.
    Type: Application
    Filed: June 25, 2003
    Publication date: August 26, 2004
    Inventors: Daniel P. Becker, Yiyuan Chen, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Donald W. Hansen, Robert M. Heintz, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Sergio Mantegani, Mark A. Massa, Joseph J. McDonald, Deborah A. Mischke, Mark A. Nagy, Ettore Perrone, Joseph G. Rico, Michelle A. Schmidt, Dale P. Spangler, John J. Talley, Mahima Trivedi, Thomas A. Wynn
  • Patent number: 6770644
    Abstract: Hydroxamic acid derivatives of the formula (I) (wherein all the symbols have the same meaning as defined in the specification.), non-toxic salt thereof or prodrugs thereof. The compounds of the formula (I) inhibit producing IL-6, so it may be used for the prevention and/or treatment of various inflammatory diseases, sepsis, multiple myeloma, plasma cell leukemia, osteoporosis, cachexia, psoriasis, nephritis, renal cell carcinoma, Kaposi's sarcoma, rheumatoid arthritis, hypergammaglobulinemia, Castleman's disease, atrial myxoma, diabetes mellitus, autoimmune diseases, hepatitis, colitis, graft versus host disease, infectious diseases and endometriosis.
    Type: Grant
    Filed: March 22, 2002
    Date of Patent: August 3, 2004
    Assignee: Ono Pharmaceuticals Co., Ltd.
    Inventors: Mitoshi Konno, Katsuhito Sakaki, Masao Naka, Mikio Konishi, Tadamitsu Kishimoto
  • Publication number: 20040127717
    Abstract: Compounds having therapeutic utility are of formula (I)
    Type: Application
    Filed: December 15, 2003
    Publication date: July 1, 2004
    Inventors: John Gary Montana, Andrew Douglas Baxter, David Alan Owen, Robert John Watson
  • Publication number: 20040122101
    Abstract: The present invention provides methods of selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, and/or inhibiting histone deacetylase (HDAC) by administration of pharmaceutical compositions comprising potent HDAC inhibitors. The oral bioavailability of the active compounds in the pharmaceutical compositions of the present invention is surprisingly high. Moreover, the pharmaceutical compositions unexpectedly give rise to high, therapeutically effective blood levels of the active compounds over an extended period of time. The present invention further provides a safe, daily dosing regimen of these pharmaceutical compositions, which is easy to follow, and which results in a therapeutically effective amount of the HDAC inhibitors in vivo. The present invention also provides a novel Form I polymorph of SAHA, characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well a unique crystalline structure.
    Type: Application
    Filed: June 19, 2003
    Publication date: June 24, 2004
    Inventors: Thomas A. Miller, Victoria M. Richon
  • Publication number: 20040110805
    Abstract: This invention is directed to aromatic sulfone hydroxamates (also known as “aromatic sulfone hydroxamic acids”) and salts thereof that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. This invention also is directed to a prevention or treatment method that comprises administering such a compound or salt in an MMP-inhibiting and/or aggrecanase-inhibiting effective amount to an animal, particularly a mammal having (or disposed to having) a pathological condition associated with MMP and/or aggrecanase activity.
    Type: Application
    Filed: September 5, 2003
    Publication date: June 10, 2004
    Inventors: John N. Freskos, Yvette M. Fobian, Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, Jeffery N. Carroll, Gary A. DeCrescenzo, Susan L. Hockerman, Darren J. Kassab, Steve A. Kolodziej, Joseph McDonald, Deborah A. Mischke, Monica B. Norton, Joseph G. Rico, John J. Talley, Clara I. Villamil, Lijuan Jane Wang
  • Patent number: 6739454
    Abstract: Collector compositions of a mixture of a C6 to C22 fatty hydroxamic acid and an oil for use in a method the removal of impurities from mineral ores by the froth flotation method. The collectors are prepared by reacting an ester of a C6 to C22 fatty acid with a hydroxylamine salt and a base in the presence of an oil and water to produce an alkyl hydroxamate salt; acidifying the alkyl hydroxamate salt, forming an organic layer and an aqueous layer, wherein the organic layer contains a C6 to C22 fatty hydroxamic acid substantially free of starting esters and hydrolysis and transesterification products of the ester; and separating the organic layer from the aqueous layer to provide a collector composition of the C6 to C22 fatty hydroxamic acid and the oil.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: May 25, 2004
    Assignee: Cytec Technology Corp.
    Inventors: Alan S. Rothenberg, Lino Giovanni Magliocco
  • Publication number: 20040077726
    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: Application
    Filed: August 20, 2003
    Publication date: April 22, 2004
    Inventors: Clare 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
  • Patent number: 6716878
    Abstract: Compounds of formula (I) are antibacterial agents: wherein Z represents a radical of formula —N(OH)CH(═O) or of formula —C(═O)NH(OH), and R1-R4 are as defined in the specification. A method for the treatment of bacterial or protozoal infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially or antiprotozoally effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt, hydrate or solvate thereof.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: April 6, 2004
    Assignee: Vernalis (Oxford) Limited
    Inventors: Richard Simon Todd, Daniel Christopher Brookings, Helen Katherine Smith, Alison Jane Thompson, Raymond Paul Beckett
  • Patent number: 6716844
    Abstract: An aromatic sulfonyl aipha-hydroxy hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed, as is a treatment process that comprises administering a contemplated aromatic sulfonyl alpha-hydroxy hydroxamic acid compound in an MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.
    Type: Grant
    Filed: December 3, 2001
    Date of Patent: April 6, 2004
    Assignee: Pharmacia Corporation
    Inventors: John N. Freskos, Terri L. Boehm, Brent V. Mischke, Robert M. Heintz, Joseph J. McDonald, Gary A. DeCrescenzo, Susan C. Howard
  • Publication number: 20040063698
    Abstract: The present invention provides compounds of Formula (I): 1
    Type: Application
    Filed: July 31, 2003
    Publication date: April 1, 2004
    Inventor: Thomas P. Maduskuie