N-(o=)s(=o) Containing (i.e., Sulfonamides) Patents (Class 514/117)
  • Patent number: 9657032
    Abstract: 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: Grant
    Filed: December 28, 2015
    Date of Patent: May 23, 2017
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Chenggeng Qian, Rudi Bao
  • Patent number: 9408940
    Abstract: 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: Grant
    Filed: April 22, 2013
    Date of Patent: August 9, 2016
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: 8993544
    Abstract: 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: Grant
    Filed: February 9, 2010
    Date of Patent: March 31, 2015
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem, Ltd.
    Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
  • Patent number: 8871438
    Abstract: 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: Grant
    Filed: August 9, 2012
    Date of Patent: October 28, 2014
    Assignee: Korea Research Institute of Standards and Science
    Inventors: Tae Geol Lee, Dae Won Moon, Byong Chul Yoo, In Hoo Kim
  • Patent number: 8614201
    Abstract: 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: Grant
    Filed: June 4, 2010
    Date of Patent: December 24, 2013
    Assignee: Janssen Pharmaceutica NV
    Inventors: Didier Jean-Calude Berthelot, Henricus Jacobus Maria Gijsen, Mirko Zaja, Jason Rech, Alec Lebsack, Bryan Branstetter, Wei Xiao, J. Guy Breitenbucher
  • Patent number: 8569376
    Abstract: 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: Grant
    Filed: March 1, 2013
    Date of Patent: October 29, 2013
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Patent number: 8518913
    Abstract: 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: Grant
    Filed: December 9, 2011
    Date of Patent: August 27, 2013
    Assignee: Allergan, Inc.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Patent number: 8425890
    Abstract: 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: Grant
    Filed: February 23, 2010
    Date of Patent: April 23, 2013
    Inventors: David J. Schneider, Charles A. Schneider
  • Patent number: 8426471
    Abstract: 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: Grant
    Filed: July 13, 2012
    Date of Patent: April 23, 2013
    Assignee: Topokine Therapeutics, Inc.
    Inventors: Murat V. Kalayoglu, Michael S. Singer
  • Patent number: 8389500
    Abstract: 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: Grant
    Filed: October 28, 2009
    Date of Patent: March 5, 2013
    Assignee: Gilead Sciences, Inc.
    Inventors: Matthew Abelman, Elfatih Elzein, Robert Jiang, Rao Kalla, Tetsuya Kobayashi, Xiaofen Li, Thao Perry, Jeff Zablocki
  • Patent number: 8367663
    Abstract: 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: Grant
    Filed: January 8, 2010
    Date of Patent: February 5, 2013
    Assignee: Curis, Inc.
    Inventors: Xiong Cai, Haixiao Zhai, Cheng-Jung Lai, Changgeng Qian
  • Patent number: 8283117
    Abstract: 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: Grant
    Filed: June 25, 2008
    Date of Patent: October 9, 2012
    Assignee: Korea Research Institute of Standards and Science
    Inventors: Tae Geol Lee, Dae Won Moon, Byong Chul Yoo, In Hoo Kim
  • Publication number: 20120190650
    Abstract: Stabilized benzyl phosphonic acid and naphthyl phosphonic acid analog compounds are effective in inhibiting the activity of autotaxin.
    Type: Application
    Filed: January 19, 2012
    Publication date: July 26, 2012
    Applicant: University of Tennessee Research Foundation
    Inventors: Renuka Gupte, Renukadevi Patil, Gabor Tigyi, Duane D. Miller
  • Publication number: 20120157413
    Abstract: 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: Application
    Filed: December 9, 2011
    Publication date: June 21, 2012
    Applicant: ALLERGAN, INC.
    Inventors: Haiqing Yuan, Richard I. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath, Michael E. Garst
  • Publication number: 20120115816
    Abstract: 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: Application
    Filed: March 4, 2010
    Publication date: May 10, 2012
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Julia Lynne Ramsay, David Stock, Gordon Alstair Bell, Claudio Screpanti, Colin Douglas Miln, Henry Ebun Agbaje, Charles A. Jones, III, Ravi Ramachandran
  • Publication number: 20120083471
    Abstract: 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: Application
    Filed: October 14, 2011
    Publication date: April 5, 2012
    Inventors: Craig A. Townsend, Edward Wydysh, Francis Kuhajda, Gabriele Valeria Ronnett
  • Publication number: 20120053139
    Abstract: 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: Application
    Filed: August 24, 2011
    Publication date: March 1, 2012
    Applicant: Ambrilia Biopharma Inc.
    Inventors: Jinzi Jason Wu, Brent Richard Stranix, Michael Ge, Guy Milot, Marco Petrella, Chandra J. Panchal
  • Publication number: 20120035140
    Abstract: 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: Application
    Filed: February 9, 2010
    Publication date: February 9, 2012
    Applicant: YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM, LTD.
    Inventors: Eli Breuer, Reuven Reich, Julia Frant, Amnon Hoffman, Veerendhar Ainelly
  • Publication number: 20120022024
    Abstract: 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: Application
    Filed: July 21, 2011
    Publication date: January 26, 2012
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Eric Oldfield, Yongcheng Song
  • Publication number: 20120015909
    Abstract: 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: Application
    Filed: March 30, 2011
    Publication date: January 19, 2012
    Applicant: JENRIN DISCOVERY
    Inventors: John Francis McElroy, Robert J. Chorvat, Parthasarathi Rajagopalan
  • Publication number: 20110319366
    Abstract: 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: Application
    Filed: August 29, 2011
    Publication date: December 29, 2011
    Inventors: Brad Buckman, Kumar Emayan, Imadul Islam, Karen May, Judi Bryant, Raju Mohan, Christopher West, Shendong Yuan
  • Patent number: 8017558
    Abstract: 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: Grant
    Filed: December 5, 2006
    Date of Patent: September 13, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Herbert Gayer, Bernd-Wieland Krüger, Arnd Voerste, Ulrike Wachendorff-Neumann, Peter Dahmen
  • Patent number: 8008297
    Abstract: 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: Grant
    Filed: April 4, 2008
    Date of Patent: August 30, 2011
    Assignee: Ambrilia Biopharma Inc.
    Inventors: Brent Richard Stranix, Valerie Perron
  • Publication number: 20110136735
    Abstract: 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: Application
    Filed: November 30, 2010
    Publication date: June 9, 2011
    Inventors: 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
  • Publication number: 20100261677
    Abstract: 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: Application
    Filed: September 4, 2008
    Publication date: October 14, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Publication number: 20090181932
    Abstract: 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: Application
    Filed: January 7, 2009
    Publication date: July 16, 2009
    Applicant: Wyeth
    Inventors: David Zenan LI, Dane Springer, Sayed Elmarakby, Appavu Chandrasekaran, Anthony F. Kreft, III
  • Publication number: 20090131374
    Abstract: 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: Application
    Filed: January 30, 2009
    Publication date: May 21, 2009
    Applicant: 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
  • Patent number: 7511037
    Abstract: 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: Grant
    Filed: August 16, 2006
    Date of Patent: March 31, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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
  • Publication number: 20090075945
    Abstract: 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: Application
    Filed: April 2, 2008
    Publication date: March 19, 2009
    Applicant: Vion Pharmaceuticals, Inc.
    Inventors: Xu Lin, Ivan King, Michael F. Belcourt, Terrence W. Doyle
  • Patent number: 7494984
    Abstract: 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: Grant
    Filed: August 29, 2006
    Date of Patent: February 24, 2009
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jacques Banville, Roger Remillard, Serge Plamondon
  • Publication number: 20080269172
    Abstract: 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: Application
    Filed: April 4, 2008
    Publication date: October 30, 2008
    Inventors: Brent Richard Stranix, Valerie Perron
  • Patent number: 7256200
    Abstract: 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: Grant
    Filed: January 30, 2004
    Date of Patent: August 14, 2007
    Assignee: The Board of Trustees of the University of Illinois, a body corporate and politic of the State of Illinois
    Inventor: Zaijie Wang
  • Patent number: 7030103
    Abstract: 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: Grant
    Filed: October 8, 2002
    Date of Patent: April 18, 2006
    Assignee: Methylgene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 6949521
    Abstract: 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: Grant
    Filed: May 4, 2001
    Date of Patent: September 27, 2005
    Assignees: The University of Georgia Research Foundation, Inc., Emory University
    Inventors: Chung K. Chu, Lakshmi P. Kotra, Konstantine Manouilov, Jinfa Du, Raymond Schinazi
  • Patent number: 6921756
    Abstract: 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: Grant
    Filed: April 8, 2003
    Date of Patent: July 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6884791
    Abstract: 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: Grant
    Filed: November 22, 2002
    Date of Patent: April 26, 2005
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Jubrail Rahil, Arkadii Vaisburg
  • Patent number: 6822001
    Abstract: 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: Grant
    Filed: November 2, 2001
    Date of Patent: November 23, 2004
    Assignee: Tularik Inc.
    Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
  • Patent number: 6737068
    Abstract: 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: Grant
    Filed: October 1, 2001
    Date of Patent: May 18, 2004
    Assignee: Playtex Products, Inc.
    Inventor: Catherine Durden
  • Patent number: 6699902
    Abstract: 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: Grant
    Filed: January 28, 2002
    Date of Patent: March 2, 2004
    Assignee: Beacon Laboratories, Inc.
    Inventors: Hsuan-Yin Lan-Hargest, Norbert L. Wiech
  • Patent number: 6620800
    Abstract: 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: Grant
    Filed: June 29, 1999
    Date of Patent: September 16, 2003
    Assignee: Vanderbilt University
    Inventor: L. Jackson Roberts, II
  • Publication number: 20020082243
    Abstract: Disclosed and claimed is a method for treating tumors using sulfonylamino-substituted N-aryl- or heteroarylcarboxamide derivatives.
    Type: Application
    Filed: August 29, 2001
    Publication date: June 27, 2002
    Inventor: Irwin Braude
  • Patent number: 6355628
    Abstract: 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: Grant
    Filed: July 27, 2000
    Date of Patent: March 12, 2002
    Assignee: Tularik Inc.
    Inventors: Susan Schwendner, Pieter Timmermans, Jacqueline Walling
  • Publication number: 20020028791
    Abstract: This invention relates generally to phosphate esters of bis-amino acid sulfonamides containing substituted benzyl amines of formula I: 1
    Type: Application
    Filed: July 18, 2001
    Publication date: March 7, 2002
    Inventors: Robert F. Kaltenbach, George L. Trainor
  • Publication number: 20020002149
    Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme.
    Type: Application
    Filed: March 21, 2001
    Publication date: January 3, 2002
    Inventors: Christopher Bayly, Mitsuru Ohkubo
  • Patent number: 6313106
    Abstract: 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: Grant
    Filed: July 12, 2000
    Date of Patent: November 6, 2001
    Assignee: D-Pharm Ltd.
    Inventor: Alexander Kozak
  • Patent number: 6271212
    Abstract: 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: Grant
    Filed: March 3, 1998
    Date of Patent: August 7, 2001
    Assignees: University of Georgia Research Foundation Inc., Emory University
    Inventors: Chung K. Chu, Lakshimi Kotra, Kostantine K. Manouilov, Jinfa Du, Raymond Schinazi
  • Patent number: 6235727
    Abstract: 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: Grant
    Filed: July 15, 1999
    Date of Patent: May 22, 2001
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Manfred Schudok, Wilfried Schwab, Gerhard Zoller, Eckart Bartnik, Frank Büttner, Klaus-Ulrich Weithmann
  • Patent number: 6211167
    Abstract: 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: Grant
    Filed: June 14, 2000
    Date of Patent: April 3, 2001
    Assignee: Tularik Inc.
    Inventor: Jonathan B. Houze
  • Patent number: 6077837
    Abstract: 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: Grant
    Filed: October 23, 1998
    Date of Patent: June 20, 2000
    Assignee: D-Pharm Ltd.
    Inventor: Alexander Kozak
  • Patent number: 6040338
    Abstract: 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: Grant
    Filed: November 3, 1997
    Date of Patent: March 21, 2000
    Assignee: Yale University
    Inventors: Alan C. Sartorelli, Krishnamurthy Shyam, Philip G. Penketh, Shu-Hui Chen