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)
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Patent number: 10494389Abstract: 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: GrantFiled: November 20, 2017Date of Patent: December 3, 2019Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Said M. Sebti, Nicholas James Lawrence, Harshani Rithma Lawrence
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Patent number: 9974762Abstract: 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: GrantFiled: June 26, 2017Date of Patent: May 22, 2018Assignee: National Institute of Biological Sciences, BeijingInventors: Zhiyuan Zhang, Xiaodong Wang, Xiaoguang Lei, Yaning Su, Sudan He, Hanying Ruan, Liming Sun
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Patent number: 9018411Abstract: 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: GrantFiled: December 7, 2010Date of Patent: April 28, 2015Assignees: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins UniversityInventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20140303246Abstract: Use of an adamantaneamine derivative for the treatment of actinic keratosis.Type: ApplicationFiled: September 7, 2012Publication date: October 9, 2014Applicant: MERZ Pharma GmbH & Co. KGaAInventors: Kevin Kiehm, Rainer Pooth, Harry Frank Abts
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Publication number: 20140243195Abstract: 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: ApplicationFiled: August 10, 2012Publication date: August 28, 2014Applicant: BASF SEInventors: 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
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Publication number: 20140243196Abstract: 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: ApplicationFiled: August 17, 2012Publication date: August 28, 2014Applicant: BASF SEInventors: 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
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Patent number: 8802659Abstract: 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: GrantFiled: August 5, 2010Date of Patent: August 12, 2014Assignee: 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
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Patent number: 8796330Abstract: 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: GrantFiled: December 18, 2007Date of Patent: August 5, 2014Assignee: Methylgene Inc.Inventors: Robert Déziel, Alain Ajamian
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Patent number: 8785419Abstract: 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: GrantFiled: July 29, 2011Date of Patent: July 22, 2014Assignee: The Trustees Of The University Of PennsylvaniaInventors: Ramachandran Murali, Mark I. Greene
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Patent number: 8785443Abstract: 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: GrantFiled: October 14, 2011Date of Patent: July 22, 2014Assignee: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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Publication number: 20140200260Abstract: 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: ApplicationFiled: March 18, 2014Publication date: July 17, 2014Inventor: Richard H. Weisbart
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Publication number: 20140171441Abstract: 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: ApplicationFiled: December 17, 2013Publication date: June 19, 2014Applicant: BEND RESEARCH, INC.Inventors: Walter C. Babcock, Dwayne T. Friesen, Warren K. Miller, Daniel T. Smithey
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Publication number: 20140155399Abstract: 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: ApplicationFiled: December 4, 2013Publication date: June 5, 2014Applicant: DANA-FARBER CANCER INSTITUTE, INC.Inventors: Levi Garraway, Caroline Emery
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Publication number: 20140142178Abstract: 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: ApplicationFiled: January 6, 2014Publication date: May 22, 2014Applicant: Kareus Therapeutics, SAInventors: Ish Khanna, Sivaram Pillarisetti
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Publication number: 20140121267Abstract: 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: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: Kareus Therapeutics, SAInventors: Ish Khanna, Sivaram Pillarisetti
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Patent number: 8623853Abstract: 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: GrantFiled: July 21, 2009Date of Patent: January 7, 2014Assignees: The Brigham and Women's Hospital, Inc., Dana-Farber Cancer Institute, Inc.Inventors: Christopher French, Jon Aster, Matthias Hofer, James Bradner
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Patent number: 8609864Abstract: 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: GrantFiled: January 7, 2010Date of Patent: December 17, 2013Assignee: Purdue Pharmaceutical Products, L.P.Inventors: Yu Chen, Yi Chen
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Publication number: 20130243707Abstract: 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: ApplicationFiled: March 28, 2013Publication date: September 19, 2013Inventors: Monique Renata GREEN, Kenton FEDDE
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Publication number: 20130244944Abstract: 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: ApplicationFiled: December 31, 2012Publication date: September 19, 2013Applicants: VERSITECH LIMITED, THE UNIVERSITY OF HONG KONGInventors: Dan Yang, Xiang Li, Huiyan Zha
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Patent number: 8507554Abstract: 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: GrantFiled: May 3, 2007Date of Patent: August 13, 2013Assignee: Seoul National University Industry FoundationInventors: Je-Yong Yoon, Cheol-Jin Kim, Jae-Eun Kim, Hyung-Yeon Park
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Patent number: 8476315Abstract: 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: GrantFiled: March 10, 2010Date of Patent: July 2, 2013Assignee: Onepharm Research & Development GmbHInventors: Paul Kosma, Ulrich Jordis, Dirk Classen-Houben, Bernhard Kueenburg, Christian Stanetty, Laszlo Czollner
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Publication number: 20130096127Abstract: 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: ApplicationFiled: November 29, 2012Publication date: April 18, 2013Applicant: NOVARTIS AGInventor: NOVARTIS AG
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Patent number: 8389570Abstract: 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: GrantFiled: August 12, 2011Date of Patent: March 5, 2013Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Publication number: 20130004509Abstract: 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: ApplicationFiled: February 22, 2011Publication date: January 3, 2013Inventor: Levi Garraway
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Patent number: 8329945Abstract: 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: GrantFiled: August 30, 2011Date of Patent: December 11, 2012Assignee: President and Fellows of Harvard CollegeInventors: Stuart L. Schreiber, Jack Taunton, Christian A. Hassig, Timothy F. Jamison
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Publication number: 20120190649Abstract: 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: ApplicationFiled: August 5, 2010Publication date: July 26, 2012Applicant: 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
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Patent number: 8227636Abstract: 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: GrantFiled: April 5, 2005Date of Patent: July 24, 2012Assignee: Merck HDAC Research, LLCInventors: Thomas A. Miller, David J. Witter, Sandro Belvedere
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Publication number: 20120095003Abstract: 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: ApplicationFiled: October 14, 2011Publication date: April 19, 2012Applicant: XenoPort, Inc.Inventors: Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
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Publication number: 20120030779Abstract: 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: ApplicationFiled: January 18, 2008Publication date: February 2, 2012Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDTIONInventors: Ivor J. Benjamin, Namakkal S. Rajasekaran, Thomas P. Kennedy
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Publication number: 20120022154Abstract: 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: ApplicationFiled: March 10, 2010Publication date: January 26, 2012Applicant: ONEPHARM RESEARCH & DEVELOPMENT GMBHInventors: Dirk Classenhouben, Bernhard Kueenburg, Paul Kosma, Ulrich Jordis, Christian Stanetty, Laszlo Czollner
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Publication number: 20110206638Abstract: 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: ApplicationFiled: January 19, 2011Publication date: August 25, 2011Inventor: Jinah Choi
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Publication number: 20110136827Abstract: 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: ApplicationFiled: December 7, 2010Publication date: June 9, 2011Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Patent number: 7951972Abstract: 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: GrantFiled: February 2, 2009Date of Patent: May 31, 2011Assignee: 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
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Patent number: 7947743Abstract: 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: GrantFiled: June 1, 2005Date of Patent: May 24, 2011Assignee: Les Laboratories ServierInventors: Christian De Bodinat, Elisabeth Mocaer
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Publication number: 20100292169Abstract: 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: ApplicationFiled: February 5, 2010Publication date: November 18, 2010Inventors: Tso-Pang Yao, Jeffrey J. Kovacs, Charlotte Hubbert, Yi-shan Lee, Ya-sheng Gao, June-Tai Wu
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Publication number: 20100234455Abstract: Hormone refractory metastatic disease can be treated with an oxyamide-containing compound through the inhibition of HDAC1 or HDAC2.Type: ApplicationFiled: October 6, 2009Publication date: September 16, 2010Inventors: Norbert L. Wiech, Hsuan-Yin Lan-Hargest
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Publication number: 20100197676Abstract: 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: ApplicationFiled: April 1, 2010Publication date: August 5, 2010Applicant: Chugai Seiyaku Kabushiki KaishaInventors: Yoshiaki Isshiki, Yasunori Kohchi, Eisaku Mizuguchi, Hitoshi Iikura, Yasuaki Matsubara, Shinji Tsujii, Nobuo Shimma, Masanori Miwa, Satoshi Aida, Masami Kohchi, Takeshi Murata, Kosuke Aso
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Patent number: 7745465Abstract: 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: GrantFiled: July 10, 2003Date of Patent: June 29, 2010Assignee: CytRx CorporationInventors: 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
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Patent number: 7557140Abstract: 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: GrantFiled: February 13, 2008Date of Patent: July 7, 2009Assignee: Topotarget UK LimitedInventors: Ivars Kalvinsh, Einars Loza, Vija Gailite
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Publication number: 20090143386Abstract: 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: ApplicationFiled: February 2, 2009Publication date: June 4, 2009Inventors: 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
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Patent number: 7537759Abstract: The invention provides methods and compositions relating to Kuz involvement in angiogenesis.Type: GrantFiled: March 21, 2005Date of Patent: May 26, 2009Assignee: The Regents of the University of CaliforniaInventors: Duojia Pan, Gerald M. Rubin, Hongbing Zhang
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Patent number: 7498358Abstract: 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: GrantFiled: December 13, 2002Date of Patent: March 3, 2009Assignee: 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
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Patent number: 7491844Abstract: Described herein are compounds having a formula and therapeutic methods, compositions, and medicaments, related thereto.Type: GrantFiled: April 20, 2007Date of Patent: February 17, 2009Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Patent number: 7476755Abstract: Therapeutic substituted cyclopentane compounds, and compositions, medicaments, and therapeutic methods related thereto are disclosed herein.Type: GrantFiled: April 27, 2007Date of Patent: January 13, 2009Assignee: Allergan, Inc.Inventors: Yariv Donde, Jeremiah H. Nguyen
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Patent number: 7420089Abstract: 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: GrantFiled: August 6, 2007Date of Patent: September 2, 2008Assignee: Pharmacyclics, Inc.Inventors: Erik J. Verner, Martin Sendzik, Chitra Baskaran, Joseph J. Buggy, James Robinson
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Patent number: 7411001Abstract: 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: GrantFiled: April 7, 2005Date of Patent: August 12, 2008Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Cathlin Marie Biwersi, Michael Huai Gu Chen, Michael David Kaufman, Haile Tecle, Joseph Scott Warmus
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Patent number: 7294639Abstract: 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: GrantFiled: August 18, 2006Date of Patent: November 13, 2007Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova
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Patent number: 7232929Abstract: 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: GrantFiled: February 15, 2004Date of Patent: June 19, 2007Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Eyal Sobol, Dan Kaufmann
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Patent number: 7169808Abstract: 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: GrantFiled: June 15, 2001Date of Patent: January 30, 2007Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Nicola Fanto′, Maria Ornella Tinti
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Patent number: 7122564Abstract: 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: GrantFiled: January 26, 2005Date of Patent: October 17, 2006Assignee: Galderma Research & DevelopmentInventors: Jean-Michel Bernardon, Laurence Clary, Eric Terranova