Chalcogen Bonded Directly To Ring Carbon Of The Five-membered Hetero Ring (e.g., Adrenochrome, Etc.) Patents (Class 514/421)
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METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR TREATING INFECTIOUS DISEASES
Publication number: 20120264678Abstract: Disclosed are methods of treating infectious diseases comprising administering to an animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.Type: ApplicationFiled: June 6, 2012Publication date: October 18, 2012Applicant: NEREUS PHARMACEUTICALS, INC.Inventor: Michael Palladino -
Publication number: 20120230972Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: ApplicationFiled: May 22, 2012Publication date: September 13, 2012Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H.R. Feling
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Patent number: 8258176Abstract: The invention discloses a dithiolopyrrolone compound represented by formula I or its pharmaceutically acceptable salts, wherein X1, R1, R2, R3, R4 are defined as in the description. The invention also discloses the preparation of such compounds, and the use of such compounds in preparation of medicaments for increasing peripheral white blood cells and in preparation of ancillary medicaments for inhibiting the decrease of peripheral white blood cells in radiotherapy or chemotherapy.Type: GrantFiled: August 29, 2008Date of Patent: September 4, 2012Assignees: Shanghai Institute of Pharmaceutical Industry, Shanghai Modern Pharmaceutical Co., Ltd.Inventors: Guoping Wang, Quanhai Liu, Haiyan Sun, Wei Wu, Jian Hou, Lin Yao, Chungang Li, Minyu Liu, Fei Li, Xuejun Wu, Shuai Zhao
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Patent number: 8227503Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.Type: GrantFiled: March 21, 2011Date of Patent: July 24, 2012Assignee: Nereus Pharmaceuticals, Inc.Inventors: Venkat Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur, Ta-Hsiang Chao, Saskia Theodora Cornelia Neuteboom
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Publication number: 20120184494Abstract: Disclosed herein are diagnostic and prognostic methods for determining the overall survival, and therapeutic regimes, for multiple myeloma patients. The methods involve the detection of PTHR1 gene expression alone or in combination with other clinical factors. The tests are suitable for diagnosing and monitoring treatment of patients having or suspected of having multiple myeloma. The disclosure also relates to proteasome inhibitors and other activators of PTHR1, for the treatment of multiple myeloma.Type: ApplicationFiled: November 10, 2011Publication date: July 19, 2012Inventors: Maurizio Zangari, Fenghuang Zhan, Guido Tricot
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Patent number: 8222289Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: GrantFiled: December 15, 2009Date of Patent: July 17, 2012Assignee: The Regents of the University of CaliforniaInventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Patent number: 8217072Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: GrantFiled: June 18, 2004Date of Patent: July 10, 2012Assignee: The Regents of the University of CaliforniaInventors: William H. Fenical, Paul R. Jensen, Tracy J. Mincer, Robert H. R. Feling
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Publication number: 20120135990Abstract: The present invention describes compounds, processes for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: May 27, 2010Publication date: May 31, 2012Applicant: TETRALOGIC PHARMACEUTICALS CORP.Inventors: Stephen M. Condon, Yijun Deng, Matthew D. Alexander, Matthew G. Laporte
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Publication number: 20120128724Abstract: Systems and methods for treating inflammatory and proliferative diseases, and wounds, using as a pharmacon a fatty acid metabolism inhibitor, a glycolytic inhibitor, and/or an agent able to alter cellular production of reactive oxygen, or combination thereof, optionally in combination with one or more chemotherapeutic agents. In preferred embodiments, the invention combines an oxirane carboxylic acid, represented by etomoxir, with a 2-deoxyglucose compound, represented by 2-deoxy-D-glucose, and/or an antibody against UCP and/or Fas antigen. The systems and methods of the invention can be used to treat drug-resistant or multi-drug resistant cancers.Type: ApplicationFiled: November 22, 2011Publication date: May 24, 2012Applicant: The Regents of the University of Colorado, a body corporateInventors: M. Karen Newell, Evan Newell, Elizabeth Villalobos-Menuey
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Publication number: 20120107269Abstract: Disclosed is a compound of formula (I), wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined in the present application.Type: ApplicationFiled: May 14, 2010Publication date: May 3, 2012Applicant: Tianjin Hemay Biotech Co., LtdInventors: Hesheng Zhang, Guanghuai Zeng, Yifei Gao
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Patent number: 8168803Abstract: Disclosed are methods of treating cancer, inflammatory conditions, and/or infectious disease in an animal comprising: administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.Type: GrantFiled: June 10, 2008Date of Patent: May 1, 2012Assignee: Nereus Pharmaceuticals, Inc.Inventors: Michael Palladino, Saskia Theodora Cornelia Neuteboom
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Publication number: 20120083495Abstract: Compounds useful for the treatment of spinal muscular atrophy or other uses, as well as methods of using such compounds to increase SMN expression, increase EAAT2 expression, or increase the expression of a nucleic acid that encodes a translational stop codon introduced by mutation or frameshift.Type: ApplicationFiled: December 5, 2011Publication date: April 5, 2012Applicants: SCIENCE APPLICATIONS INTERNATIONAL INC. (SAIC), ALBANY MOLECULAR RESEARCH, INC., DEPARTMENT OF HEALTH AND HUMAN SERVICESInventors: Jill Heemskerk, Keith D. Barnes, John M. McCall, Graham Johnson, David Fairfax, Matthew Robert Johnson
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Publication number: 20120041045Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryan-themaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.Type: ApplicationFiled: March 16, 2010Publication date: February 16, 2012Applicant: H.L. HALL & SONS LIMITEDInventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
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Patent number: 8101644Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: GrantFiled: March 28, 2008Date of Patent: January 24, 2012Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
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Patent number: 8084487Abstract: The present invention relates to a process for the production of carbamic acid (2-chloroethyl)(3-oxocyclohexyl)-alkyl ester enantiomers and of 1-carbalkoxy-4-ketoperhydroindole enantiomers.Type: GrantFiled: August 10, 2009Date of Patent: December 27, 2011Assignee: Novartis AGInventors: Ernst Kuesters, Murat Acemoglu, Philipp Lustenberger, Gottfried Sedelmeier, Beat Schmitz, Gerhard Penn
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Publication number: 20110224274Abstract: A compound of formula (I) or a compound of formula (II) or pharmaceutically acceptable salts thereof, wherein R1-R7 and X are as defined in the description, and the use of these compounds in therapy, in particular in treating cancer or as an inhibitor of the interaction of the MDM2 protein with p53.Type: ApplicationFiled: June 25, 2009Publication date: September 15, 2011Inventors: Bernard Thomas Golding, Christiane Riedinger, Roger John Griffin, Ian Robert Hardcasctle, Eric Valeur, Anna Frances Watson, Martin Noble
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Publication number: 20110212969Abstract: This invention provides compounds of formula (I): wherein ring A, X1, X2, X3, R2, R4b, R10, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention, and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: ApplicationFiled: February 25, 2011Publication date: September 1, 2011Applicant: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, Sean J. Harrison, He Xu
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Patent number: 8008340Abstract: A method for inhibiting casein kinase I? activity, comprising administering to said patient a therapeutically effective amount of a compound of formula I. its stereoisomer, enantiomer, racemate, tautomer or pharmaceutically acceptable salt thereof.Type: GrantFiled: February 15, 2007Date of Patent: August 30, 2011Assignee: Aventis Pharmaceuticals Inc.Inventor: William Arthur Metz, Jr.
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Publication number: 20110195986Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable forms thereof according to Formula I wherein R1, R4, R5, R3, R3a, W, D, R2a, R2b and R2c are defined herein. Additionally, the present application provides pharmaceutical compositions containing at least one compound according to Formula I and optionally at least one additional therapeutic agent. Finally, the present application provides methods for treating a patient suffering from an MCHR-1 modulated disease or disorder such as, for example, obesity, diabetes, depression, anxiety or intestinal inflammation, by administration of a therapeutically effective dose of a compound according to Formula I.Type: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Guohua Zhao, William N. Washburn, James J. Mignone
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Publication number: 20110195934Abstract: The present application provides compounds, including all stereoisomers, solvates, prodrugs and pharmaceutically acceptable faints thereof according to wherein all of the variables are defined herein.Type: ApplicationFiled: October 8, 2009Publication date: August 11, 2011Inventors: Pratik Devasthale, Wliiam N. Washburn, Wei Wang, Andres Hernandez, Saleem Ahmad, Guohua Zhao
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Publication number: 20110172285Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.Type: ApplicationFiled: March 21, 2011Publication date: July 14, 2011Applicant: NEREUS PHARMACEUTICALS, INC.Inventors: Venkat Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur, Ta-Hsiang Chao, Saskia Theodora Cornelia Neuteboom
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Publication number: 20110152210Abstract: Synthetic polyphenolic compounds of formula (I), their modes of synthesis, and pharmaceutical compositions thereof are provided herein. Use of the compounds and compositions described herein for inhibiting proteasomal activity and for treating cancer is also provided.Type: ApplicationFiled: December 15, 2010Publication date: June 23, 2011Applicants: THE ROYAL INSTITUTION FOR THE ADVANCEMENT OF LEARNING/McGILL UNIVERSITY, THE HONG KONG POLYTECHNIC UNIVERSITY, WAYNE STATE UNIVERSITYInventors: Tak-Hang CHAN, Q. Ping DOU
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Publication number: 20110117015Abstract: The invention relates to aryl-sulphonamido compounds endowed with affinity against metallo proteases MMP, having formula (I) below wherein R, R1, R2, R3, G and n have the meanings reported in the specification, properly labelled with diagnostic imaging moieties or even radiotherapeutic moieties. The invention also refers to the process for their preparation, to pharmaceutical compositions comprising them and to their use as diagnostic imaging agents or radiotherapeutic agents.Type: ApplicationFiled: July 21, 2009Publication date: May 19, 2011Applicant: BRACCO IMAGING S.P.A.Inventors: Armando Rossello, Elisa Nuti, Stanislava Ivanova Avramova, Fulvio Uggeri, Alessandro Maiocchi
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Patent number: 7928138Abstract: The invention is the discovery of an actinomycete genus, given the name Salinospora gen. nov., that displays an obligate requirement of seawater (Na+) for growth and unique 16S rRNA signature nucleotides. The invention is also the use of the genus for the production and discovery of active biomolecules such as pharmaceutical agents, agrichemicals, immunomodifiers, enzymes and enzyme inhibitors.Type: GrantFiled: December 28, 2007Date of Patent: April 19, 2011Assignee: Regents of the University of CaliforniaInventors: Robert H. R. Feling, William Fenical, Paul R. Jensen, Tracy J. Mincer
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Patent number: 7923466Abstract: Methods for the treatment of a patient suffering from a disease or disorder ameliorated by inhibition of casein kinase I? activity comprising the administration of a compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) useful in the claimed methods of treatment are also disclosed.Type: GrantFiled: November 12, 2008Date of Patent: April 12, 2011Assignee: Aventis Pharmaceuticals Inc.Inventors: William Arthur Metz, Jr., Fa-Xiang Ding
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Publication number: 20110082172Abstract: Pyrrolidinone carboxamide compounds are provided that are useful for inhibiting the binding of ligands to the ChemR23 receptor.Type: ApplicationFiled: September 21, 2010Publication date: April 7, 2011Applicant: ChemoCentryx, Inc.Inventors: Trevor T. Charvat, Hiufung Chu, Antoni Krasinski, Christopher W. Lange, Manmohan Reddy Leleti, Jay P. Powers, Sreenivas Punna, Timothy J. Sullivan, Solomon Ungashe
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Patent number: 7915300Abstract: A compound of the formula II wherein one of R1 and R2 is halo and the other is H or halo; R3 is C1-C4 straight or branched chain, optionally fluorinated, alkyl; R4 is H; or R3 together with R4 and the adjoining backbone carbon defines: a spiro-C5-C7 cycloalkyl, optionally substituted with 1 to 3 substituents selected from halo, hydroxyl, C1-C4 alkyl or C1-C4 haloalkyl; or optionally bridged with a methylene group; or a C4-C6 saturated heterocycle having a hetero atom selected from O, NRa, S, S(?O)2; where Ra is H, C1-C4 alkyl or CH3C(?O); R5 is independently selected from H or methyl; E is —C(?O)—, —S(?O)m—, —NR5S(?O)m—, —NR5C(?O)—, —OC(?O)—, R6 is a stable, optionally substituted, monocyclic or bicyclic, carbocycle or heterocycle; m is independently 0,1 or 2; are inhibitors of cathepsin K and useful in the treatment or prophylaxis of osteoporosis.Type: GrantFiled: January 6, 2005Date of Patent: March 29, 2011Assignee: Medivir ABInventors: Magnus Nilsson, Xiao-Xiong Zhou, Lourdes Oden, Bjorn Classon, Rolf Noren, Urszula Grabowska, Philip Jackson, Philip Fallon, Andrew Carr, Mark Liley, Matt Tozer, Tony Johnson, Victor Diaz, Laia Crespo, Jussi Kangasmetsa, Thierry Bonnaud
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Publication number: 20110071071Abstract: The present invention relates to a method for diagnosing chronic graft rejection of a grafted organ in a subject from a biological sample of said subject, comprising: (a) determining in vitro an expression level value for PSMB10 in said subject biological sample, (b) comparing said value to at least one reference expression level value for PSMB10 in at least one reference sample, and (c) diagnosing if said subject is or not undergoing chronic rejection of said grafted organ. The invention also concerns a diagnostic kit or microarray for performing the method of the invention. The invention further concerns the medical use of proteasome inhibitors for treating chronic rejection.Type: ApplicationFiled: February 10, 2009Publication date: March 24, 2011Inventors: Sophie Brouard, Magali Giral, Jean-Paul Soulillou, Vojislav Jovanovic, Joanna Ashton-Chess
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Patent number: 7910616Abstract: Disclosed herein are compounds of Formula (I) that include a sulfonate ester, ester or ether group. Compounds of Formula (I) can be included in pharmaceutical compositions, and can be used to treating and/or ameliorating a disease or condition, such as cancer, a microbial disease and/or inflammation.Type: GrantFiled: May 12, 2009Date of Patent: March 22, 2011Assignee: Nereus Pharmaceuticals, Inc.Inventors: Venkat Rami Reddy Macherla, Barbara Christine Potts, Rama Rao Manam, Katherine A. McArthur, Ta-Hsiang Chao, Saskia Theodora Cornelia Neuteboom
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Publication number: 20110021543Abstract: Novel N-aryl substituted heteroindole compounds, processes for their manufacture, veterinary compositions containing such compounds, and methods of controlling ectoparasites are provided. The compounds are believed effective in the control of ectoparasites on warm-blooded productive livestock and domestic animals.Type: ApplicationFiled: April 29, 2008Publication date: January 27, 2011Inventors: Noelle Gauvry, Jorg Fruchtel, Thomas Goebel, Sandra Schorderet Weber, Jacques Bouvier
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Publication number: 20110020272Abstract: Disclosed are methods of using proteasome inhibitors (PI) in combinations with other pharmaceutically active agents for treating viral hepatitis infections, for example, for treating therapy-resistant and -refractory viral hepatitis infections. Also disclosed are pharmaceutical compositions and kits of pharmaceutical compositions which can be used for treating viral hepatitis infections, for example, for treating therapy-resistant and refractory viral hepatitis infections.Type: ApplicationFiled: July 26, 2010Publication date: January 27, 2011Inventor: Ulrich SCHUBERT
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Publication number: 20110015248Abstract: The present invention relates to substituted heterocycles, processes for their preparation, and their use in medicaments, especially for the treatment of inflammatory disease, i.e. asthma, or cancer.Type: ApplicationFiled: January 8, 2009Publication date: January 20, 2011Applicant: INTERMED DISCOVERY GMBHInventors: Marc STADLER, Stephan Seip, Hartwig Müller, Anke Mayer-Bartschmid, Michael-Alexander Brüning, Jordi Benet-Buchholz, Hiroko Togame, Reiko Dodo, Peter Reinemer, Kevin Bacon, Kinji Fuchikami, Satoko Matsukawa, Klaus Urbahns
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Publication number: 20110009456Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: December 21, 2009Publication date: January 13, 2011Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Patent number: 7868008Abstract: The present invention is directed to compounds of formula I: wherein R1, R2, R3, R4, R5, R6, R7, R8, R9 and n are as defined for formula I in the description. The invention also relates to processes for the preparation of the compounds and to new intermediates employed in the preparation, pharmaceutical compositions containing the compounds, and to the use of the compounds in therapy.Type: GrantFiled: February 15, 2006Date of Patent: January 11, 2011Assignee: AstraZeneca ABInventors: Bradford Van Wagenen, Radhakrishnan Ukkiramapandian, Joshua Clayton, Ian Egle, James Empfield, Methvin Isaac, Fupeng Ma, Abdelmalik Slassi, Gary Steelman, Rebecca Urbanek, Sally Walsh
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Patent number: 7824698Abstract: Lyophilized formulations comprising Salinosporamide A or analogs thereof are provided. In some aspects, lyophilized formulations comprising Salinosporamide A or analogs thereof and bulking agents are provided. Also provided are methods of lyophilizing Salinosporamide A or analogs thereof. In some aspects, a solvent or co-solvent system is utilized. Also provided are methods of administering Salinosporamide A or analogs thereof to patients.Type: GrantFiled: February 4, 2008Date of Patent: November 2, 2010Assignee: Nereus Pharmaceuticals, Inc.Inventors: Barbara Potts, Ramsharan Singh, Jan-Jon Chu, Bao Viet Mai, Natasha Reddinger, Cheryl (Billstrom) Sifferlen
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Publication number: 20100255116Abstract: A fungicidal composition is provided. A fungicidal composition comprising synergistically effective amounts of (a) a carboxylic acid amide derivative of the formula (I) or its salt: wherein B is a heterocyclic group which may be substituted; each of R1 and R2 which are independent of each other, is alkyl; X is halogen, alkyl or alkoxy; and n is an integer of from 0 to 5, and (b) at least one fungicidal compound selected from the group consisting of an azole compound, an anilinopyrimidine compound, a triazolopyrimidine compound, a strobilurin compound, an N-halogenothioalkyl compound, a pyridinamine compound, a bicarbonate, an inorganic sulfur compound, a dithiocarbamate compound, an organic chlorine compound, a dicarboxyimide compound, an amine compound, a phenylpyrrole compound, a benzophenone compound, a dinitrobenzene compound, a piperidine compound, a morpholine compound, etc.Type: ApplicationFiled: October 20, 2008Publication date: October 7, 2010Applicant: ISHIHARA SANGYO KAISHA, LTD.Inventors: Shigeru Mitani, Shintaro Tsukuda
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Publication number: 20100240581Abstract: Methods of modulating chronic low-grade inflammation are provided. More particularly, methods of treating diabetes, such as for example, type-2 diabetes mellitus, in a mammal by administering an effective amount of a selective proteasome inhibitor are provided. Also provided are unit dosage forms of such inhibitors.Type: ApplicationFiled: November 13, 2007Publication date: September 23, 2010Applicant: The Trustees of Columbia University in the City of New YorkInventors: Drew Tortoriello, Stuart P Weisberg
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Publication number: 20100227892Abstract: Methods of using di, tri, and tetracyclic acylhydrazide derivatives and analogs, as well as pharmaceutical compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.Type: ApplicationFiled: April 1, 2010Publication date: September 9, 2010Applicant: Siga Technologies Inc.Inventors: Robert Jordan, Thomas R. Bailey, Susan R. Rippin
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Patent number: 7781429Abstract: A vehicle for topical delivery which contains a liquid eutectic mixture of hydrophobic compounds.Type: GrantFiled: May 18, 2006Date of Patent: August 24, 2010Assignee: Alpharx Inc.Inventors: Joseph Schwarz, Michael Weisspapir
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Publication number: 20100179189Abstract: Compounds represented by Formula (I) or Formula (II) against cell releasing TNF?, their pharmaceutically acceptable salts or hydrates and preparation methods and uses thereof, in which A and B represent CH2, CO, SO, or SO2; D represents S, NH, or NC1-6 alkyl; R1 represents H, or one or two same or different radical(s) selected from the group consisting of F, Cl, Br, C1-4 alkyl, OH, OC1-4 alkyl, NO2, NHC(O)C1-4 alkyl, NH2, NH(C1-4 alkyl), or N(C1-4 alkyl)2.Type: ApplicationFiled: October 16, 2007Publication date: July 15, 2010Inventor: Hesheng Zhang
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METHODS OF USING [3.2.0] HETEROCYCLIC COMPOUNDS AND ANALOGS THEREOF FOR TREATING INFECTIOUS DISEASES
Publication number: 20100168046Abstract: Disclosed are methods of treating infectious diseases comprising administering to the animal, a therapeutically effective amount of a heterocyclic compound. The animal is a mammal, preferably a human or a rodent.Type: ApplicationFiled: March 9, 2010Publication date: July 1, 2010Applicant: NEREUS PHARMACEUTICALS, INC.Inventor: Michael Palladino -
Patent number: 7737174Abstract: The invention relates to small molecules which function as inhibitors of the interaction between p53 and MDM2. The invention also relates to the use of these compounds for inhibiting cell growth, inducing cell death, inducing cell cycle arrest and/or sensitizing cells to additional agent(s).Type: GrantFiled: August 30, 2007Date of Patent: June 15, 2010Assignee: The Regents of the University of MichiganInventors: Shaomeng Wang, Dongguang Qin, Jiangyong Chen, Shanghai Yu
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Publication number: 20100144826Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: ApplicationFiled: December 15, 2009Publication date: June 10, 2010Inventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Patent number: 7732480Abstract: There are disclosed bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.Type: GrantFiled: October 31, 2007Date of Patent: June 8, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Lawrence Hamann, Haixia Wang
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Patent number: 7696241Abstract: The present invention relates to bicyclic compounds according to formula I, pharmaceutical compositions containing such compounds and methods of using such compounds in the treatment of androgen receptor-associated conditions, such as age-related diseases, for example sarcopenia, wherein R1, R2, R5, X and n are defined herein.Type: GrantFiled: March 2, 2005Date of Patent: April 13, 2010Assignee: Bristol-Myers Squibb CompanyInventors: James J. Li, Lawrence Hamann, Haixia Wang
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Patent number: 7691896Abstract: Disclosed herein are analogs of Salinosporamide A, having the Formula I as follows: Like Salinosporamide A, the compounds of the present invention will inhibit the proteasome, an intracellular enzyme complex that destroys proteins the cell no longer needs. Without the proteasome, proteins would build up and clog cellular machinery. Fast-growing cancer cells make especially heavy use of the proteasome, so thwarting its action is a compelling drug strategy.Type: GrantFiled: February 8, 2008Date of Patent: April 6, 2010Assignee: President and Fellows of Harvard CollegeInventors: Andrew G. Myers, Binyuan Sun, Stona R Jackson
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Patent number: 7642272Abstract: There are disclosed compounds of the formula I a pharmaceutically acceptable salt or solvate of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.Type: GrantFiled: March 18, 2004Date of Patent: January 5, 2010Assignee: Schering CorporationInventors: Bandarpalle B. Shankar, Razia K. Rizvi, Joseph A. Kozlowski, Neng-Yang Shih
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Publication number: 20090318529Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: ApplicationFiled: June 18, 2004Publication date: December 24, 2009Inventors: William H. Fenical, Paul R. Jensen, Tracy J. Mincer, Robert H.R. Feling
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Patent number: 7635712Abstract: The present invention is based on the discovery that certain fermentation products of the marine actinomycete strains CNB392 and CNB476 are effective inhibitors of hyperproliferative mammalian cells. The CNB392 and CNB476 strains lie within the family Micromonosporaceae, and the generic epithet Salinospora has been proposed for this obligate marine group. The reaction products produced by this strain are classified as salinosporamides, and are particularly advantageous in treating neoplastic disorders due to their low molecular weight, low IC50 values, high pharmaceutical potency, and selectivity for cancer cells over fungi.Type: GrantFiled: February 12, 2007Date of Patent: December 22, 2009Assignee: The Regents of the University of CaliforniaInventors: William Fenical, Paul Jensen, Tracy Mincer, Robert H. R. Feling
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Patent number: 7629376Abstract: The present invention discloses and claims compounds of formula (I) and formula (II) as inhibitors of human casein kinase I?, and methods of using the compounds of formula (I) and formula (II) for treating central nervous system diseases and disorders including mood disorders and sleep disorders. The R-group substituents are defined herein and pharmaceutical compositions comprising compounds of formula (I) or formula (II) are also disclosed and claimed.Type: GrantFiled: February 13, 2007Date of Patent: December 8, 2009Assignee: Aventis Pharmaceuticals Inc.Inventors: William Arthur Metz, Jr., Fa-Xiang Ding