R-c(=x)-n-x-c Containing (e.g., Hydroxamic Acid Ester, Etc.) (r Is C Or H And X Is Chalcogen) Patents (Class 514/507)
  • Patent number: 10494389
    Abstract: The subject matter disclosed herein relates to compositions and methods of making and using the compositions. In a further aspect, the subject matter disclosed herein relates to inhibitors of STAT3 dimerization. Methods of making these compositions as well as compositions comprising these compositions are also disclosed. Also disclosed are methods of treating or preventing certain cancers by administering to an individual in need thereof and effective amount of the compounds disclosed herein. Still further, disclosed herein are methods of inhibiting STAT3 by contacting a cell with a compound or composition as disclosed herein.
    Type: Grant
    Filed: November 20, 2017
    Date of Patent: December 3, 2019
    Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.
    Inventors: Said M. Sebti, Nicholas James Lawrence, Harshani Rithma Lawrence
  • Patent number: 9974762
    Abstract: The invention provides amides that inhibit cellular necrosis and/or human receptor interacting protein 1 kinase (RIP1), including corresponding sulfonamides, and pharmaceutically acceptable salts, hydrides and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition, and detecting a resultant improvement in the person's health or condition.
    Type: Grant
    Filed: June 26, 2017
    Date of Patent: May 22, 2018
    Assignee: National Institute of Biological Sciences, Beijing
    Inventors: Zhiyuan Zhang, Xiaodong Wang, Xiaoguang Lei, Yaning Su, Sudan He, Hanying Ruan, Liming Sun
  • Patent number: 9018411
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Grant
    Filed: December 7, 2010
    Date of Patent: April 28, 2015
    Assignees: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20140303246
    Abstract: Use of an adamantaneamine derivative for the treatment of actinic keratosis.
    Type: Application
    Filed: September 7, 2012
    Publication date: October 9, 2014
    Applicant: MERZ Pharma GmbH & Co. KGaA
    Inventors: Kevin Kiehm, Rainer Pooth, Harry Frank Abts
  • Publication number: 20140243196
    Abstract: The present invention relates to substituted carbamoylmethoxy and carbamoylmethylthio benzamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the carbamoylmethoxy- and carbamoylmethylthio-benzamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: August 28, 2014
    Applicant: BASF SE
    Inventors: Prashant Deshmukh, Markus Kordes, Wolfgang Von Deyn, Karsten Koerber, Florian Kaiser, Joachim Dickhaut, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Publication number: 20140243195
    Abstract: The present invention relates to N-thio-anthranilamide compounds and the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising the same. The invention also relates to the use of the N-thio-anthranilamide compounds or of the compositions comprising such compounds for combating invertebrate pests. Furthermore, the invention relates to methods of applying such compounds.
    Type: Application
    Filed: August 10, 2012
    Publication date: August 28, 2014
    Applicant: BASF SE
    Inventors: Markus Kordes, Prashant Deshmukh, Wolfgang Von Deyn, Karsten Koerber, Joachim Dickhaut, Henricus Maria Martinus Bastiaans, Florian Kaiser, Arun Narine, Nina Gertrud Bandur, Gemma Veitch, Deborah L. Culbertson, Paul Neese, Koshi Gunjima
  • Patent number: 8802659
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Grant
    Filed: August 5, 2010
    Date of Patent: August 12, 2014
    Assignee: Biogen Idec MA Inc.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • 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
  • Patent number: 8785419
    Abstract: Method of identifying compounds that modulate intermolecular interactions between a target protein and a modifier are disclosed. Pharmaceutical composition comprising compounds that inhibit intermolecular interactions between a target protein and a modifier are disclosed. Methods of treating individual suffering from inflammatory conditions, undesirable immune responses, immunological conditions and bacterial infections are disclosed.
    Type: Grant
    Filed: July 29, 2011
    Date of Patent: July 22, 2014
    Assignee: The Trustees Of The University Of Pennsylvania
    Inventors: Ramachandran Murali, Mark I. Greene
  • Patent number: 8785443
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Grant
    Filed: October 14, 2011
    Date of Patent: July 22, 2014
    Assignee: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20140200260
    Abstract: The invention provides methods for determining whether a subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene comprising contacting isolated fibroblasts from the subject with a molecule or pool of molecules directed to the BRAF oncogene; and culturing the sample in the presence of the agent and determining whether BRAF oncogene expression by the cell is decreased and/or whether cells in the sample return to a less transformed phenotype, exhibit decreased cell proliferation and/or exhibit increased contact inhibition, any of which is indicative that the subject is suffering from a rheumatoid arthritis associated with the BRAF oncogene.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Inventor: Richard H. Weisbart
  • Publication number: 20140171441
    Abstract: Pharmaceutical compositions of a low-solubility drug and lower alkanoate-, phthalate- and trimellitate esters of hydroxypropyl methyl cellulose and lower alkanoate- and succinate esters of cellulose and methyl cellulose are disclosed that provide enhanced concentrations of the drug in a use environment.
    Type: Application
    Filed: December 17, 2013
    Publication date: June 19, 2014
    Applicant: BEND RESEARCH, INC.
    Inventors: Walter C. Babcock, Dwayne T. Friesen, Warren K. Miller, Daniel T. Smithey
  • Publication number: 20140155399
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: December 4, 2013
    Publication date: June 5, 2014
    Applicant: DANA-FARBER CANCER INSTITUTE, INC.
    Inventors: Levi Garraway, Caroline Emery
  • Publication number: 20140142178
    Abstract: Novel compounds of Formula I are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R1 is selected from a group consisting of hydroxy, alkoxy, amine, alkyl, haloalkyl, NHSO2R, or NHCOR wherein R is selected from alkyl or cycloalkyl, NHR? wherein R? is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy; and n1 and n2 are independently selected from 0, 1, and 2. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally, when R3 and R4 or R5 and R6 do not form a cyclic ring, then they may be independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is a linear aliphatic chain optionally containing from 4 to 16 carbon atoms. The chain may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 22, 2014
    Applicant: Kareus Therapeutics, SA
    Inventors: Ish Khanna, Sivaram Pillarisetti
  • Publication number: 20140121267
    Abstract: Novel compounds of Formula A1 are provided: its stereoisomers and/or pharmaceutically acceptable salts for the treatment of diabetes and diabetes-associated dyslipidemia, wherein R7 is independently selected from a group consisting of hydroxy, alkoxy, alkyl, amine, NHR? wherein R? is alkyl or cycloalkyl optionally substituted by hydroxy or alkoxy, NHSO2R or NHCOR, wherein R is selected from alkyl or cycloalkyl. At least one of R3 and R4 and/or R5 and R6 form a cyclic ring of 3-8 carbon atoms optionally containing alkyl groups, hetero atoms, or functional groups such as O, N, SO2. Additionally R3 and R4 or R5 and R6, when they do not form a cyclic ring, are independently selected from hydrogen, alkyl, branched alkyl, and cycloalkyl. L1 is independently a linear aliphatic chain optionally containing from 6 to 16 carbon-atoms and L1 may optionally be substituted one or more times by alkyl, branched alkyl, cycloalkyl, or aryl.
    Type: Application
    Filed: January 6, 2014
    Publication date: May 1, 2014
    Applicant: Kareus Therapeutics, SA
    Inventors: Ish Khanna, Sivaram Pillarisetti
  • Patent number: 8623853
    Abstract: The present invention is directed, inter alia, to methods of treating NUT midline carcinoma (NMC) by administering compounds that promote increased histone acetylation. The invention also includes assay methods for determining the responsiveness of NMC to specific histone deacetylases and other compounds.
    Type: Grant
    Filed: July 21, 2009
    Date of Patent: January 7, 2014
    Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.
    Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
  • 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: 20130243707
    Abstract: Topical compositions are disclosed that are useful for delivering a therapeutic level of an NSAID to a target within a subject having a local inflammatory disorder. A composition of the present invention comprises a Drug and a solvent system, wherein the solvent system comprises at least two solvent alcohols and wherein the solvent system is present in an amount sufficient to solubilize the Drug, the solvent system is a low alkanol system, and the composition is a single phase composition. Exemplary solvent systems are those for which one of the at least two solvent alcohols is polyethylene glycol, glycerin, butylene glycol, diproylene glycol, propylene glycol, ethanol, isopropanol, or a derivative thereof. Optionally the local inflammatory disorder is pseudofolliculitis barbae, dermatitis, psoriasis, wounds, or sunburn.
    Type: Application
    Filed: March 28, 2013
    Publication date: September 19, 2013
    Inventors: Monique Renata GREEN, Kenton FEDDE
  • Publication number: 20130244944
    Abstract: Provided herein are self-assembling compounds that can form ion channels in lipid bilayers or cell membranes and ion-channel-forming compositions comprising the self-assembling compounds. Also provided are methods of making and using the ion channels formed from a plurality of molecules of the self-assembling compounds. Further, provided are methods of treating or preventing conditions and diseases that are related to the dysfunction of ion channels, including chloride channels.
    Type: Application
    Filed: December 31, 2012
    Publication date: September 19, 2013
    Applicants: VERSITECH LIMITED, THE UNIVERSITY OF HONG KONG
    Inventors: Dan Yang, Xiang Li, Huiyan Zha
  • Patent number: 8507554
    Abstract: In the quorum sensing antagonist blocking the communication in bacteria, the method for preventing biofilm formation using this quorum sensing antagonist and the method for reducing the bacterial contamination, the quorum sensing antagonist contains the homoserine lactone moiety and sulfanylethanoyl group, and has a similar chemical structure to that of the autoinducer which is produced by bacteria as a signal, whereby the quorum sensing antagonist can inhibit the formation of biofilm and reduce the bacterial contamination as well.
    Type: Grant
    Filed: May 3, 2007
    Date of Patent: August 13, 2013
    Assignee: Seoul National University Industry Foundation
    Inventors: Je-Yong Yoon, Cheol-Jin Kim, Jae-Eun Kim, Hyung-Yeon Park
  • Patent number: 8476315
    Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Grant
    Filed: March 10, 2010
    Date of Patent: July 2, 2013
    Assignee: Onepharm Research & Development GmbH
    Inventors: Paul Kosma, Ulrich Jordis, Dirk Classen-Houben, Bernhard Kueenburg, Christian Stanetty, Laszlo Czollner
  • Publication number: 20130096127
    Abstract: The present invention provides a compound of formula I?; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R5, B1, X and n are defined herein. The invention also relates 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: Application
    Filed: November 29, 2012
    Publication date: April 18, 2013
    Applicant: NOVARTIS AG
    Inventor: NOVARTIS AG
  • Patent number: 8389570
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also 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: Grant
    Filed: August 12, 2011
    Date of Patent: March 5, 2013
    Assignee: Pharmacyclics, Inc.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Publication number: 20130004509
    Abstract: The present invention relates to methods, compositions and kits concerning resistance to treatment with an anti-cancer agent, specifically an inhibitor of BRAF. In particular embodiments, the invention concerns mutations in a BRAF sequence that confer resistance to a BRAF inhibitor. Identification of such mutations in a BRAF sequence allows the identification and design of second-generation BRAF inhibitors. Methods and kits for detecting the presence of a mutant BRAF sequence in a sample are also provided.
    Type: Application
    Filed: February 22, 2011
    Publication date: January 3, 2013
    Inventor: Levi Garraway
  • 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
  • Publication number: 20120190649
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: August 5, 2010
    Publication date: July 26, 2012
    Applicant: BIOGEN IDEC MA INC.
    Inventors: Jermaine Thomas, Xiaogao Liu, Edward Yin-Shiang Lin, Guo Zhu Zheng, Bin Ma, Richard D. Caldwell, Kevin M. Guckian, Gnanasambandam Kumaravel, Arthur G. Taveras
  • Patent number: 8227636
    Abstract: The present invention is directed to prodrugs of hydroxamic acid based histone deacetylase (HDAC) inhibitors, e.g., suberoylanilide hydroxamic acid (SAHA). The prodrugs are acylated derivatives having increased aqueous solubility and cellular permeability as compared with the free hydroxamic acid, and are useful for inhibiting HDACs, and for selectively inducing terminal differentiation, cell growth arrest and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the prodrugs of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The prodrugs of the invention are also useful in the prevention and treatment of thioredoxin (TRX)-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.
    Type: Grant
    Filed: April 5, 2005
    Date of Patent: July 24, 2012
    Assignee: Merck HDAC Research, LLC
    Inventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
  • Publication number: 20120095003
    Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
    Type: Application
    Filed: October 14, 2011
    Publication date: April 19, 2012
    Applicant: XenoPort, Inc.
    Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
  • Publication number: 20120030779
    Abstract: Disclosed herein is a non-human animal model of protein aggregation cardiomyopathy. Also disclosed are compo-sitions and methods of treating or preventing a condition in a subject caused or exacerbated by reductive stress. Also disclosed are compositions and methods of predicting, detecting, or monitoring reductive stress in a subject.
    Type: Application
    Filed: January 18, 2008
    Publication date: February 2, 2012
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDTION
    Inventors: Ivor J. Benjamin, Namakkal S. Rajasekaran, Thomas P. Kennedy
  • Publication number: 20120022154
    Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.
    Type: Application
    Filed: March 10, 2010
    Publication date: January 26, 2012
    Applicant: ONEPHARM RESEARCH & DEVELOPMENT GMBH
    Inventors: Dirk Classenhouben, Bernhard Kueenburg, Paul Kosma, Ulrich Jordis, Christian Stanetty, Laszlo Czollner
  • Publication number: 20110206638
    Abstract: The disclosure provides compositions and methods for reducing the mutation rate of a virus, such as an RNA virus or a DNA virus, in a cell infected with the virus by, in one aspect, contacting the cell with an effective amount of an iron chelator or an antioxidant. Also provided are compositions and methods for enhancing the efficacy of an agent or a therapy directed at a virus.
    Type: Application
    Filed: January 19, 2011
    Publication date: August 25, 2011
    Inventor: Jinah Choi
  • Publication number: 20110136827
    Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.
    Type: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • 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: 7947743
    Abstract: The present invention relates to the use of agomelatine, or N-[2-(7-methoxy-1-naphthyl)ethyl]acetamide, on its own or in association, in obtaining medicaments intended for the treatment of bipolar disorders, especially bipolar disorders of types I and II, and more especially bipolar disorders of type I.
    Type: Grant
    Filed: June 1, 2005
    Date of Patent: May 24, 2011
    Assignee: Les Laboratories Servier
    Inventors: Christian De Bodinat, Elisabeth Mocaer
  • Publication number: 20100292169
    Abstract: The present invention provides methods and compositions for inhibiting Hsp90 activity in a cell, comprising contacting the cell with an inhibitor of histone deacetylase 6 (HDAC6)
    Type: Application
    Filed: February 5, 2010
    Publication date: November 18, 2010
    Inventors: Tso-Pang Yao, Jeffrey J. Kovacs, Charlotte Hubbert, Yi-shan Lee, Ya-sheng Gao, June-Tai Wu
  • Publication number: 20100234455
    Abstract: Hormone refractory metastatic disease can be treated with an oxyamide-containing compound through the inhibition of HDAC1 or HDAC2.
    Type: Application
    Filed: October 6, 2009
    Publication date: September 16, 2010
    Inventors: Norbert L. Wiech, Hsuan-Yin Lan-Hargest
  • Publication number: 20100197676
    Abstract: An objective of the present invention is to provide compounds that exhibit strong MEK-inhibiting activity and are stable in vivo and soluble in water, which can be used as preventive or therapeutic agents for proliferative diseases. The compounds of the present invention and pharmaceutically acceptable salts thereof are represented by the following formula (1): [where R1, R2, R3, R4, and X are the same as defined in the present patent application].
    Type: Application
    Filed: April 1, 2010
    Publication date: August 5, 2010
    Applicant: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
  • Patent number: 7745465
    Abstract: A method of increasing expression of a molecular chaperon by a cell and/or enhancing the activity of a molecular chaperon in cells is provided. The method comprises treating a cell that is exposed to a physiological stress which induces expression of a molecular chaperon by the cell with an effective amount of a certain hydroxylamine derivative to increase the stress. Alternatively, an hydroxylamine derivative can be administrated to a cell before it is exposed to a physiological stress which induces expression of a molecular chaperon by the cell. Preferably, the cell to which an hydroxylamine derivative is administered is an eukaryotic cell. The hydroxylamine derivative corresponds to the formulae (I) or (II). The invention also provides novel hydroxylamine derivatives falling within the scope of the formulae (I) and (II) as well as pharmaceutical and/or cosmetical compositions comprising the said compounds.
    Type: Grant
    Filed: July 10, 2003
    Date of Patent: June 29, 2010
    Assignee: CytRx Corporation
    Inventors: László Vígh, Péter Literáti Nagy, Jenö Szilbereky, László Ürögdi, Andrea Jednákovits, László Jaszlits, Katalin Bíró, Ede Márványos, Mihály Barabás, Erzsébet Hegedüs, László Korányi, Mária Kürthy, Gábor Balogh, Ibolya Horváth, Zsolt Török, Éva Udvardy, György Dormán, Dénes Medzihradszky, Bea Mézes, Eszter Kovács, Ernö Duda, Beatrix Farkas, Attila Glatz
  • Patent number: 7557140
    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: February 13, 2008
    Date of Patent: July 7, 2009
    Assignee: Topotarget UK Limited
    Inventors: Ivars Kalvinsh, Einars Loza, Vija Gailite
  • Publication number: 20090143386
    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: Application
    Filed: February 2, 2009
    Publication date: June 4, 2009
    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: 7537759
    Abstract: The invention provides methods and compositions relating to Kuz involvement in angiogenesis.
    Type: Grant
    Filed: March 21, 2005
    Date of Patent: May 26, 2009
    Assignee: The Regents of the University of California
    Inventors: Duojia Pan, Gerald M. Rubin, Hongbing Zhang
  • 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: 7491844
    Abstract: Described herein are compounds having a formula and therapeutic methods, compositions, and medicaments, related thereto.
    Type: Grant
    Filed: April 20, 2007
    Date of Patent: February 17, 2009
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 7476755
    Abstract: Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.
    Type: Grant
    Filed: April 27, 2007
    Date of Patent: January 13, 2009
    Assignee: Allergan, Inc.
    Inventors: Yariv Donde, Jeremiah H. Nguyen
  • Patent number: 7420089
    Abstract: The present invention is directed to certain hydroxamate derivatives that are useful in the treatment of hepatitis C. These compounds are also 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: Grant
    Filed: August 6, 2007
    Date of Patent: September 2, 2008
    Assignee: Pharmacyclics, Inc.
    Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
  • Patent number: 7411001
    Abstract: The present invention relates to oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof. The present invention also relates to crystalline forms of oxygenated esters of 4-iodophenylamino benzhydroxamic acid derivatives, pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: August 12, 2008
    Assignee: Warner-Lambert Company
    Inventors: Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
  • Patent number: 7294639
    Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.
    Type: Grant
    Filed: August 18, 2006
    Date of Patent: November 13, 2007
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova
  • Patent number: 7232929
    Abstract: The invention relates to new 2,2,3,3-tetramethylcyclopropane carboxamide derivative compounds, pharmaceutical compositions thereof and uses thereof for treating psychotic disorders, neurodegenerative diseases, epilepsy and pain.
    Type: Grant
    Filed: February 15, 2004
    Date of Patent: June 19, 2007
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Meir Bialer, Boris Yagen, Eyal Sobol, Dan Kaufmann
  • 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: 7122564
    Abstract: Novel pharmaceutical/cosmetic compositions contain at least one biaromatic ligand activator of a PPAR? receptor, such biaromatic ligand having the structural formula (I): and are well suited, inter alia, for regulating and/or restoring skin lipid metabolism, for treating a wide variety of dermatological afflictions, and for preventing and/or treating the signs of aging and/or dry skin.
    Type: Grant
    Filed: January 26, 2005
    Date of Patent: October 17, 2006
    Assignee: Galderma Research & Development
    Inventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova