N-(o=)s(=o) Containing (i.e., Sulfonamides) Patents (Class 514/117)
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Patent number: 9657032Abstract: The invention provides a compound of Formula I, Pharmaceutical compositions comprising such compounds and the use of such compounds in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: December 28, 2015Date of Patent: May 23, 2017Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian, Rudi Bao
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Patent number: 9408940Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.Type: GrantFiled: April 22, 2013Date of Patent: August 9, 2016Inventors: David J. Schneider, Charles A. Schneider
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Patent number: 8993544Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.Type: GrantFiled: February 9, 2010Date of Patent: March 31, 2015Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd.Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
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Patent number: 8871438Abstract: The present invention relates to a disease diagnosis method, a marker screening method, and a marker using a time-of-flight secondary ion mass spectrometry (TOF-SIMS), and more particularly, to a large intestine cancer diagnosis method, a large intestine cancer marker screening method, and a large intestine cancer marker using a time-of-flight secondary ion mass spectrometry (TOF-SIMS). Specifically, the present invention provides a method diagnosing a disease using a pattern of secondary ion mass (m/z) peaks of biological samples measured using a time-of-flight secondary ion mass spectrometry (TOF-SIMS) as a marker, a marker screening method being a reference judging an existence or non-existence of a disease, and a marker configured of specific secondary ion mass peaks.Type: GrantFiled: August 9, 2012Date of Patent: October 28, 2014Assignee: Korea Research Institute of Standards and ScienceInventors: Tae Geol Lee, Dae Won Moon, Byong Chul Yoo, In Hoo Kim
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Patent number: 8614201Abstract: Certain heterocyclic amide compounds are described. The compounds may be used in pharmaceutical compositions and methods for treating disease states, disorders, and conditions mediated by TRPA1 activity, such as pain, arthritis, itch, cough, asthma, or inflammatory bowel disease.Type: GrantFiled: June 4, 2010Date of Patent: December 24, 2013Assignee: Janssen Pharmaceutica NVInventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
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Patent number: 8569376Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I) and/or (V): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, R4, R5, R6, R7, R7?, Z, Y, n, y, and x, are as defined herein.Type: GrantFiled: March 1, 2013Date of Patent: October 29, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8518913Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: December 9, 2011Date of Patent: August 27, 2013Assignee: Allergan, Inc.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Patent number: 8426471Abstract: Provided are methods of reducing body fat in a subject, comprising locally (e.g., topically) administering one or more compounds of the Formula (I): or a pharmaceutically acceptable salt, hydrate, solvate, stereoisomer, polymorph, tautomer, isotopically enriched derivative, or prodrug thereof, wherein X is —OR1, —SR2, or —NR3R4, and R1, R2, R3, and R4 are as defined herein.Type: GrantFiled: July 13, 2012Date of Patent: April 23, 2013Assignee: Topokine Therapeutics, Inc.Inventors: Murat V. Kalayoglu, Michael S. Singer
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Patent number: 8425890Abstract: An odor-controlling bodily fluid absorbent member comprises (a) an absorbent material or substrate; and (b) a halo active aromatic sulfonamide compound of Formula (I): wherein R1, R2, R3, R4, R5, X, M, and n are as described herein; and wherein at least one of R1, R2, R3, R4, and R5 is not hydrogen. The absorbent member effectively controls odor arising from various body fluids.Type: GrantFiled: February 23, 2010Date of Patent: April 23, 2013Inventors: David J. Schneider, Charles A. Schneider
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Patent number: 8389500Abstract: The present invention relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula (IA) or (IB): as further described herein. The invention also relates to methods for the preparation of the compounds, and to pharmaceutical compositions containing such compounds.Type: GrantFiled: October 28, 2009Date of Patent: March 5, 2013Assignee: Gilead Sciences, Inc.Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
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Patent number: 8367663Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.Type: GrantFiled: January 8, 2010Date of Patent: February 5, 2013Assignee: Curis, Inc.Inventors: Xiong Cai, Haixiao Zhai, Cheng-Jung Lai, Changgeng Qian
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Patent number: 8283117Abstract: The present invention relates to a disease diagnosis method, a marker screening method, and a marker using a time-of-flight secondary ion mass spectrometry (TOF-SIMS), and more particularly, to a large intestine cancer diagnosis method, a large intestine cancer marker screening method, and a large intestine cancer marker using a time-of-flight secondary ion mass spectrometry (TOF-SIMS). Specifically, the present invention provides a method diagnosing a disease using a pattern of secondary ion mass (m/z) peaks of biological samples measured using a time-of- flight secondary ion mass spectrometry (TOF-SIMS) as a marker, a marker screening method being a reference judging an existence or non-existence of a disease, and a marker configured of specific secondary ion mass peaks.Type: GrantFiled: June 25, 2008Date of Patent: October 9, 2012Assignee: Korea Research Institute of Standards and ScienceInventors: Tae Geol Lee, Dae Won Moon, Byong Chul Yoo, In Hoo Kim
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Publication number: 20120190650Abstract: Stabilized benzyl phosphonic acid and naphthyl phosphonic acid analog compounds are effective in inhibiting the activity of autotaxin.Type: ApplicationFiled: January 19, 2012Publication date: July 26, 2012Applicant: University of Tennessee Research FoundationInventors: Renuka Gupte, Renukadevi Patil, Gabor Tigyi, Duane D. Miller
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Publication number: 20120157413Abstract: The present invention relates to novel phosphorous derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 9, 2011Publication date: June 21, 2012Applicant: ALLERGAN, INC.Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
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Publication number: 20120115816Abstract: The invention includes aqueous compatibilized pesticidal formulations and methods of making them. In typical embodiments, formulations comprise a first electrolytic pesticide and a second electrolytic pesticide, and about 30 to about 300 g/L of at least one alkyl polyglycoside. The invention also includes methods of preparing pesticidal formulations to increase the concentration of the electrolytic pesticides. The invention also includes storage and transport systems containing formulation embodiments. The invention also includes methods inhibiting pests.Type: ApplicationFiled: March 4, 2010Publication date: May 10, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Julia Lynne Ramsay, David Stock, Gordon Alstair Bell, Claudio Screpanti, Colin Douglas Miln, Henry Ebun Agbaje, Charles A. Jones, III, Ravi Ramachandran
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Publication number: 20120083471Abstract: The present invention relates to novel pharmaceutical compositions containing the same, and methods of use for a variety of therapeutically valuable uses including, but not limited to, treating obesity by inhibiting the activity of Glycerol 3-phosphate acyltransferase (GPAT).Type: ApplicationFiled: October 14, 2011Publication date: April 5, 2012Inventors: Craig A. Townsend, Edward Wydysh, Francis Kuhajda, Gabriele Valeria Ronnett
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Publication number: 20120053139Abstract: The present invention provides methods for improving the pharmacokinetics of protease inhibitors and protease inhibitor precursors and pharmaceutical composition comprising protease inhibitors or protease inhibitor precursors of formula I and a cytochrome P450 monooxigenase inhibitor; when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: ApplicationFiled: August 24, 2011Publication date: March 1, 2012Applicant: Ambrilia Biopharma Inc.Inventors: Jinzi Jason Wu, Brent Richard Stranix, Michael Ge, Guy Milot, Marco Petrella, Chandra J. Panchal
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Publication number: 20120035140Abstract: The present invention relates to novel metalloproteinase inhibitors having an aryloxybenzenesulfonamide moiety and a carbamoylphosphonic acid moiety, to pharmaceutical compositions comprising them, and to their uses in the prevention and/or treatment of disease or disorder associated with MMP.Type: ApplicationFiled: February 9, 2010Publication date: February 9, 2012Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
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Publication number: 20120022024Abstract: This disclosure relates to compositions and methods including for the inhibition, prevention, and/or treatment of microbial infections, including infections from such pathogens as Staphylococcus aureus.Type: ApplicationFiled: July 21, 2011Publication date: January 26, 2012Applicant: The Board of Trustees of the University of IllinoisInventors: Eric Oldfield, Yongcheng Song
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Publication number: 20120015909Abstract: The invention provides novel compounds of formulae I and II: that are monoamine oxidase-B inhibitors, which can be useful in treating obesity, diabetes, and/or cardiometabolic disorders (e.g., hypertension, dyslipidemias, high blood pressure, and insulin resistance).Type: ApplicationFiled: March 30, 2011Publication date: January 19, 2012Applicant: JENRIN DISCOVERYInventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
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Publication number: 20110319366Abstract: Compounds of the following formula (I), for example: wherein R1, R2, R3, and R4 are described herein, are useful as inhibitors of plasma carboxypeptidase B. Pharmaceutical compositions containing these compounds, methods of using these compounds as antithrombotic agents and processes for synthesizing these compounds are also described herein.Type: ApplicationFiled: August 29, 2011Publication date: December 29, 2011Inventors: Brad Buckman, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendong Yuan
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Patent number: 8017558Abstract: Novel carboxamides of the formula (I) The present application is further directed toward a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: GrantFiled: December 5, 2006Date of Patent: September 13, 2011Assignee: Bayer Cropscience AGInventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
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Patent number: 8008297Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: GrantFiled: April 4, 2008Date of Patent: August 30, 2011Assignee: Ambrilia Biopharma Inc.Inventors: Brent Richard Stranix, Valerie Perron
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; 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 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20100261677Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.Type: ApplicationFiled: September 4, 2008Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20090181932Abstract: A synthetic compound characterized by having the structure of formula I or II or a pharmaceutically acceptable salt and/or hydrate thereof is provided. Formula I and formula II are defined as follows. wherein R1 is substituted aryl or substituted heteroaryl; R2 and R3 are independently selected from the group consisting of CF3, substituted phenyl, C1-C4 alkyl, substituted C1-C4 alkyl, (CF3)nC1-C4alkyl, (CF3)n(substituted C1-C4 alkyl), provided that when R2 or R3 is CF3, the other is not an unsubstituted alkyl; R4 and R4? are independently selected from the group consisting of M, C1-C4 alkyl, phenyl, and benzyl, wherein M is a metal ion is selected from the group consisting of sodium, lithium, calcium, magnesium and potassium, or R4 and R4? are taken together to form a cyclic structure. Methods of making such compounds and uses thereof are also provided.Type: ApplicationFiled: January 7, 2009Publication date: July 16, 2009Applicant: WyethInventors: David Zenan LI, Dane Springer, Sayed Elmarakby, Appavu Chandrasekaran, Anthony F. Kreft, III
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Publication number: 20090131374Abstract: The present invention provides compounds of Formula (I) and Formula (II) that are useful for modulating the biological activity of the protein tyrosine phosphatase-1b (PTP1B) enzyme. Compounds of this invention can be used to treat diseases and/or conditions in which the PTP1B enzyme is a factor. Such diseases and/or conditions include, but are not limited to, Type 1 diabetes, Type 2 diabetes, inadequate glucose tolerance, insulin resistance, obesity, hyperlipidemia, hypertriglyceridemia, hypercholesterolemia, low HDL levels, atherosclerosis, vascular restenosis, inflammatory bowel disease, pancreatitis, adipose cell tumors, adipose cell carcinoma, liposarcoma, dyslipidemia, cancer, and neurodegenerative diseases.Type: ApplicationFiled: January 30, 2009Publication date: May 21, 2009Applicant: CEPTYR, INC.Inventors: Mark Arnold Thomas Blaskovich, Ted Baughman, Thomas Little, William Patt, Maher Qabar, Lauri Marie Schultz, Feng Hong, Gangadhar Nagula, Jennifer Lynn Gage, James Jeffry Howbert
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Patent number: 7511037Abstract: The invention encompasses a series of bicyclic pyrimidinone compounds of Formula I which inhibit HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 16, 2006Date of Patent: March 31, 2009Assignee: Bristol-Myers Squibb CompanyInventors: B. Narasimhulu Naidu, Jacques Banville, Francis Beaulieu, Timothy P. Connolly, Mark R. Krystal, John D. Matiskella, Carl Ouellet, Serge Plamondon, Roger Remillard, Margaret E. Sorenson, Yasutsugu Ueda, Michael A. Walker
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Publication number: 20090075945Abstract: Novel phosphate-bearing prodrugs of sulfonyl hydrazines have the formula presented below. Methods of treatment of cancer are claimed. The aforementioned prodrugs include enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates and metabolites from all stages. The aforementioned prodrugs are preferentially activated in hypoxic tumors and can be given either alone, or in combination with other anticancer agents or with phototheraphy or radiotherapy. where R is C1-C10 alkyl or haloalkyl; R? and R? are each independently C1-C10 alkyl; and R1 is C1-C10 alkyl, or a pharmaceutically acceptable salt, solvate, polymorph or metabolite thereof.Type: ApplicationFiled: April 2, 2008Publication date: March 19, 2009Applicant: Vion Pharmaceuticals, Inc.Inventors: Xu Lin, Ivan King, Michael F. Belcourt, Terrence W. Doyle
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Patent number: 7494984Abstract: The invention encompasses a series of bicyclic heterocyclic compounds of Formula I which are inhibitors of HIV integrase and prevent viral integration into human DNA. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.Type: GrantFiled: August 29, 2006Date of Patent: February 24, 2009Assignee: Bristol-Myers Squibb CompanyInventors: Jacques Banville, Roger Remillard, Serge Plamondon
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Publication number: 20080269172Abstract: The present invention provides lysine based compounds of the formula; and when the compound of formula I comprises an amino group, pharmaceutically acceptable ammonium salts thereof, wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, alkyl-CO— or cycloalkyl-CO—, wherein X may be, for example, F, Cl, and Br, and wherein R2 and R3 are as defined herein.Type: ApplicationFiled: April 4, 2008Publication date: October 30, 2008Inventors: Brent Richard Stranix, Valerie Perron
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Patent number: 7256200Abstract: Composition and methods of treating pain and reducing, reversing, or preventing tolerance to opiate analgesics are disclosed. The composition and method utilize an opiate analgesic and a calcium calmodulin kinase (CaMKII) inhibitor as active agents to treat pain in mammals, including humans.Type: GrantFiled: January 30, 2004Date of Patent: August 14, 2007Assignee: The Board of Trustees of the University of Illinois, a body corporate and politic of the State of IllinoisInventor: Zaijie Wang
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Patent number: 7030103Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: October 8, 2002Date of Patent: April 18, 2006Assignee: Methylgene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 6949521Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2?-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: May 4, 2001Date of Patent: September 27, 2005Assignees: The University of Georgia Research Foundation, Inc., Emory UniversityInventors: Chung K. Chu, Lakshmi P. Kotra, Konstantine Manouilov, Jinfa Du, Raymond Schinazi
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Patent number: 6921756Abstract: The invention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: April 8, 2003Date of Patent: July 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6884791Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel ?-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic ?-lactamase inhibitors presently available, and which do not require a ?-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.Type: GrantFiled: November 22, 2002Date of Patent: April 26, 2005Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
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Patent number: 6822001Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic agent such as gemcitabine or paclitaxel.Type: GrantFiled: November 2, 2001Date of Patent: November 23, 2004Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Patent number: 6737068Abstract: The present invention relates to a liquid formulation for a feminine wipe. The preferred formulation has an anti-irritant agent, a pH adjuster namely citric acid, and at least one preservative.Type: GrantFiled: October 1, 2001Date of Patent: May 18, 2004Assignee: Playtex Products, Inc.Inventor: Catherine Durden
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Patent number: 6699902Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.Type: GrantFiled: January 28, 2002Date of Patent: March 2, 2004Assignee: Beacon Laboratories, Inc.Inventors: Hsuan-Yin Lan-Hargest, Norbert L. Wiech
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Patent number: 6620800Abstract: A method to assess oxidative stress in vivo includes the steps of measuring an amount of neuroprostanes in a biological sample before the ex vivo development of neuroprostanes in a sample, comparing the measured amount of neuroprostanes with a control and assessing oxidative stress in vivo based on this comparison. There is also provided a marker for oxidated stress by an increase of neuroprostanes in a biological sample compared to a control sample. A diagnostic tool for determining the presence of a neurodegenerative disease provides for determining an increased amount of neuroprostanes in a biological sample compared to that of a control sample.Type: GrantFiled: June 29, 1999Date of Patent: September 16, 2003Assignee: Vanderbilt UniversityInventor: L. Jackson Roberts, II
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Publication number: 20020082243Abstract: Disclosed and claimed is a method for treating tumors using sulfonylamino-substituted N-aryl- or heteroarylcarboxamide derivatives.Type: ApplicationFiled: August 29, 2001Publication date: June 27, 2002Inventor: Irwin Braude
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Patent number: 6355628Abstract: Combination therapies are provided for the treatment of proliferative disorders which use a pentafluorobenzenesulfonamide of formula I and an antineoplastic platinum coordination complex such as cisplatin.Type: GrantFiled: July 27, 2000Date of Patent: March 12, 2002Assignee: Tularik Inc.Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
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Publication number: 20020028791Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1Type: ApplicationFiled: July 18, 2001Publication date: March 7, 2002Inventors: Robert F. Kaltenbach, George L. Trainor
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Publication number: 20020002149Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.Type: ApplicationFiled: March 21, 2001Publication date: January 3, 2002Inventors: Christopher Bayly, Mitsuru Ohkubo
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Patent number: 6313106Abstract: The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.Type: GrantFiled: July 12, 2000Date of Patent: November 6, 2001Assignee: D-Pharm Ltd.Inventor: Alexander Kozak
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Patent number: 6271212Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: March 3, 1998Date of Patent: August 7, 2001Assignees: University of Georgia Research Foundation Inc., Emory UniversityInventors: Chung K. Chu, Lakshimi Kotra, Kostantine K. Manouilov, Jinfa Du, Raymond Schinazi
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Patent number: 6235727Abstract: Compounds of the formula I are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading enzymes is involved.Type: GrantFiled: July 15, 1999Date of Patent: May 22, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Manfred Schudok, Wilfried Schwab, Gerhard Zoller, Eckart Bartnik, Frank Büttner, Klaus-Ulrich Weithmann
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Patent number: 6211167Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infrections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: June 14, 2000Date of Patent: April 3, 2001Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6077837Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.Type: GrantFiled: October 23, 1998Date of Patent: June 20, 2000Assignee: D-Pharm Ltd.Inventor: Alexander Kozak
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Patent number: 6040338Abstract: The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.Type: GrantFiled: November 3, 1997Date of Patent: March 21, 2000Assignee: Yale UniversityInventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh, Shu-Hui Chen