Substituent Q Is Alkyl Patents (Class 564/98)
  • Publication number: 20140377875
    Abstract: UV-Absorbing and fluorescent pl markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Gyula Vigh, Ming-Chien Li
  • Patent number: 8877969
    Abstract: A photosensitive composition comprising: (A) a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation, a pattern forming method using the photosensitive composition, and a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation.
    Type: Grant
    Filed: April 13, 2010
    Date of Patent: November 4, 2014
    Assignee: FUJIFILM Corporation
    Inventor: Kenji Wada
  • Patent number: 8809584
    Abstract: Novel compounds are continually sought after to treat and prevent diseases and disorders. The invention relates to N-substituted-N-phenylethylsulfonamides useful for being biologically and pharmacologically screened, and to contribute to the exploration and identification of new lead molecules that are capable of modulating the functional activity of a biological target.
    Type: Grant
    Filed: December 21, 2011
    Date of Patent: August 19, 2014
    Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.
    Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
  • Patent number: 8809577
    Abstract: A process to prepare fluorinated sulfobetaine compounds of formula (I) wherein Rf is C2 to C10 fluoroalkyl optionally interrupted by one or more of O, CH2, CHF, or combinations thereof; R1 is C1 to C10 alkylene; R2 is C1 to C6 alkylene or a chemical bond; R3 is H or CH3; R4 is C1 to C6 alkylene containing at least one hydroxyl group; R5 is H or CH3; and R6 is H or CH3; comprising contacting a fluorinated sulfonamide amine of formula (II) with an aliphatic chlorosulfonic acid or salt thereof of formula (III) in the presence of water and at least one alkylene glycol, and optionally at least one alkyl carbonate, said fluorinated sulfobetaine having reduced free chloride content and reduced flammability without the need for additional purification steps.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: August 19, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Stephen James Getty, Peter Michael Murphy, Romain Severac, Alexander Borisovich Shtarov, Hollis Thomas Warren
  • Patent number: 8802895
    Abstract: The invention provides a compound of formula (I), a pharmaceutical composition thereof, a method of preparing a medicament for the treatment of a cancer, and a method of treating cancers. The invention exhibits merits against cancers such as significantly higher potency and effectiveness over a broader range of cancers. In formula (I), Ra is a benzyl group with alkyl and/or alkoxy; Rb is selected from H and alkyl groups; Rf is an alkyl; and R3 is selected from a substituted phenyl, a heterocyclic group, and wherein Rc is selected from a fused ring, fused rings, and any bivalent cyclic group.
    Type: Grant
    Filed: October 18, 2010
    Date of Patent: August 12, 2014
    Assignee: Cleveland State University
    Inventors: Bin Su, Aimin Zhou, Yan Xu
  • Patent number: 8796468
    Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: August 5, 2014
    Assignee: Shionogi & Co., Ltd.
    Inventors: Tomoyuki Ogawa, Koji Masuda
  • Patent number: 8772343
    Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula 10 (I):(I) or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R3, R4 and R5 are as defined in the description. Nav1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
    Type: Grant
    Filed: July 6, 2011
    Date of Patent: July 8, 2014
    Assignee: Pfizer Limited
    Inventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
  • Patent number: 8609897
    Abstract: The present invention is directed to a novel trifluoromethylsulfonamide derivative which inhibits the processing of APP by the putative ?-secretase and thus is useful in the treatment or prevention of Alzheimer's disease. This compound possesses favorable pharmacokinetic properties in higher species (rhesus) and thus can be dosed on an intermittent dosing regiment (e.g., once weekly). When dosed on such a regiment the compound exhibits significant and continuous A? lowering without the manifestation of Notch associated gastrointestinal toxicity for extended periods, e.g., 7 days. Pharmaceutical compositions and methods of use are also included.
    Type: Grant
    Filed: January 29, 2010
    Date of Patent: December 17, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
  • Patent number: 8410150
    Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: April 2, 2013
    Assignee: University Health Network
    Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
  • Patent number: 8383276
    Abstract: An organic electrolyte solvent includes a compound of the formula: R1—SO2—NR2—OR3 wherein R1 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives and perfluorinated analogues; R2 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives; R3 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives wherein the electrolyte solvent is stable at voltages of greater than 4.0 volts.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: February 26, 2013
    Assignees: Toyota Motor Engineering & Manufacturing North America, Inc., Synthonix Corporation
    Inventors: John Muldoon, Gary Allred, Anthony Dotse
  • Publication number: 20120270934
    Abstract: This invention relates to novel prostacyclin derivatives and acceptable salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by prostacyclin, and in particular those diseases and conditions beneficially treated by dilators of systemic and pulmonary arterial vascular beds or by platelet aggregation inhibitors.
    Type: Application
    Filed: July 2, 2010
    Publication date: October 25, 2012
    Inventors: Craig E. Masse, Scott L. Harbeson, Roger D. Tung
  • Publication number: 20120259128
    Abstract: Disclosed is an adamantanamine derivative which is useful as a significant intermediate of an 11?HSD-1 inhibitor. Disclosed is a compound represented by the formula (II): wherein R10 is a group represented by the formula: —(CR13R14)m-NR12—R11 or the like.
    Type: Application
    Filed: December 20, 2010
    Publication date: October 11, 2012
    Applicant: SHIONOGI & CO., LTD.
    Inventors: Tomoyuki Ogawa, Koji Masuda
  • Patent number: 8148422
    Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, R2, R3, R4, RA, and RB are defined herein.
    Type: Grant
    Filed: December 15, 2009
    Date of Patent: April 3, 2012
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Mark J. Macielag, James J. McNally
  • Patent number: 8115030
    Abstract: Disclosed is a process for the preparation of Compound (III), salt or solvate thereof by reacting Compound (I), salt or solvate thereof with Compound (II) in a toluene solvent in the presence of an additive such as water or an alcohol. Also disclosed is a process for the preparation of Compound (IV) comprising hydrolyzing the obtained Compound (III) if necessary, and then oxidizing. In the formula, R1 is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted aryl lower alkyl, and R2 is optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl lower alkyl.
    Type: Grant
    Filed: March 30, 2006
    Date of Patent: February 14, 2012
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshiaki Masui, Kazuhiro Yoshida
  • Patent number: 7875746
    Abstract: A photosensitive composition comprising: (A) a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation, a pattern forming method using the photosensitive composition, and a compound capable of generating a compound having a specific structure upon irradiation with actinic rays or radiation.
    Type: Grant
    Filed: May 23, 2006
    Date of Patent: January 25, 2011
    Assignee: FUJIFILM Corporation
    Inventor: Kenji Wada
  • Publication number: 20110008680
    Abstract: An organic electrolyte solvent includes a compound of the formula: R1—SO2—NR2—OR3 wherein R1 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives and perfluorinated analogues; R2 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives; R3 is selected from alkanes, alkenes, alkynes, aryls and their substituted derivatives wherein the electrolyte solvent is stable at voltages of greater than 4.0 volts.
    Type: Application
    Filed: June 24, 2010
    Publication date: January 13, 2011
    Applicants: Toyota Motor Engineering & Manufacturing North America, Inc., Synthonix Corporation
    Inventors: John Muldoon, Gary Allred, Anthony Dotse
  • Patent number: 7704988
    Abstract: This invention provides cholesterol absorption inhibitors of Formula I: and the pharmaceutically acceptable salts and esters thereof. The compounds are useful for lowering plasma cholesterol levels, particularly LDL cholesterol, and for treating and preventing atherosclerosis and atherosclerotic disease events.
    Type: Grant
    Filed: October 4, 2006
    Date of Patent: April 27, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
  • Patent number: 7678941
    Abstract: The present invention provides polyoxyalkylene ammonium imide or methide salts and their use as antistatic agents. Another embodiment provides articles comprising these salts, and processes for making and using these salts.
    Type: Grant
    Filed: July 23, 2007
    Date of Patent: March 16, 2010
    Assignee: 3M Innovative Properties Company
    Inventors: Patricia M. Savu, William M. Lamanna, Thomas P. Klun
  • Publication number: 20100063322
    Abstract: A compound having the general formula (I) or a pharmacologically acceptable salt thereof: X—NH—Y—NH—R1??(I) [wherein X represents R2—SO2— in which R2 represents an optionally substituted lower alkyl group or phenyl group; Y represents a group selected from the group consisting of —R3—NH—R4—, —R5—NH—R6—NH—R7—, —R8—NH—R9—NH—R10—NH—R11— and —R12—NH—R13—NH—R14—NH—R15— in which R3 to R15 each independently represent a C3 to C5 alkylene group; and R1 represents hydrogen or an optionally substituted lower alkyl group, with the proviso that the case where X represents a tosyl group, Y represents —(CH2)3—NH—(CH2)4—NH—(CH2)3— and R1 represents hydrogen is excepted].
    Type: Application
    Filed: November 12, 2007
    Publication date: March 11, 2010
    Inventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
  • Patent number: 7453010
    Abstract: The invention relates to compounds of general formula (I): where R1 represents H or a (C1-C4)alkyl, —CO(C1-C4)alkyl, (C1-C4)alkylphenyl or —CO-phenyl group, said phenyl optionally being substituted; R2 represents H, a halogen atom, an —S(O)z(C1-C4)alkyl group, where z is equal to 0, 1 or 2, an —NHSO2(C1-C4)alkyl group, an —NHSO2-phenyl group or an —NHSO2—(C1-C4)alkylphenyl group, said phenyl optionally being substituted; R3 represents an —X—R4 group—in which X represents a bond, an oxygen atom or a —CH2— group and R4 represents H or a —CR5R6—COOR7 group, where R5, R6 and R7 independently represent H or a (C1-C4)alkyl group—a phenyl group optionally substituted or fused with a dioxolane group, a —CO—NR8R9 group—where R8 represents H, a (C1-C4)alkyl group or a (C1-C4)alkyl(C1-C4)alkoxy group and R9 represents a (C1-C4)alkyl(C1-C4)alkoxy group, a —(CH2)n-A group, where n is equal to 0, 1, 2, 3 or 4 and where A represents an indolyl group, a fluorenyl group or a phenyl group which is substituted, an optiona
    Type: Grant
    Filed: May 26, 2003
    Date of Patent: November 18, 2008
    Assignee: Sanofi Aventis
    Inventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
  • Publication number: 20080262264
    Abstract: Disclosed is a process for the preparation of Compound (III), salt or solvate thereof by reacting Compound (I), salt or solvate thereof with Compound (II) in a toluene solvent in the presence of an additive such as water or an alcohol. Also disclosed is a process for the preparation of Compound (IV) comprising hydrolyzing the obtained Compound (III) if necessary, and then oxidizing. In the formula, R1 is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted aryl lower alkyl, and R2 is optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl lower alkyl.
    Type: Application
    Filed: March 30, 2006
    Publication date: October 23, 2008
    Applicant: Shionogi & Co., Ltd.
    Inventors: Toshiaki Masui, Kazuhiro Yoshida
  • Patent number: 7411002
    Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.
    Type: Grant
    Filed: June 7, 2006
    Date of Patent: August 12, 2008
    Assignees: The University of Kansas, Mediquest Therapeutics, Inc.
    Inventors: Mark R. Burns, Sunil A. David, Scott A. Jenkins
  • Patent number: 7365196
    Abstract: A class of compounds is disclosed, comprising sulphonamido-substituted bridged bicycloalkyl structures. The compounds are inhibitors of gamma-secretase, and hence are useful in the treatment of and/or prevention of Alzheimer's disease.
    Type: Grant
    Filed: March 15, 2001
    Date of Patent: April 29, 2008
    Assignees: Merck Sharp & Dohme Ltd., Merck Frosst Canada & Co.
    Inventors: Patrice Charles Belanger, Ian James Collins, Joanne Claire Hannam, Timothy Harrison, Stephen John Lewis, Andrew Madin, Edward Giles McIver, Alan John Nadin, Joseph George Neduvelil, Mark Steven Shearman, Adrian Leonard Smith, Timothy Jason Sparey, Graeme Irvine Stevenson, Martin Richard Teall
  • Patent number: 7232817
    Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 27, 2005
    Date of Patent: June 19, 2007
    Assignees: G.D. Searle & Co., Monsanto Company
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: 7220914
    Abstract: Zwitterionic compounds, photovoltaic cell charge carrier layers containing such compounds, photovoltaic cells including such charge carrier layers, and related methods are disclosed.
    Type: Grant
    Filed: November 30, 2004
    Date of Patent: May 22, 2007
    Assignee: Konarka Technologies, Inc.
    Inventors: Kethinni G. Chittibabu, Savvas Hadjikyriacou, David Waller
  • Patent number: 7169952
    Abstract: A process for the preparation of a sulfonamide of formula (II), comprising reacting at elevated temperature an aniline of formula (I), with a sulfonating agent A of the formula R1—SO2-Z in the presence of a catalytic amount of either: (i) an amide B-1, other than N,N-dimethylformamide, or (ii) a high boiling tertiary amine B-2. Also provided in accordance with the present invention are processes for preparing sulfonamides of formula (II) by reacting an aniline of formula (I) with sulfanating agent A of the formula R1—SO2-Z in the presence of N,N-dimethylformamide, at a temperature in the range of about 120° C. to about 160° C. for about three to about seven hours.
    Type: Grant
    Filed: June 1, 2001
    Date of Patent: January 30, 2007
    Assignee: FMC Corporation
    Inventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
  • Patent number: 6984757
    Abstract: A process for the preparation of a 4-(4-flourophenyl)-6-alkyl-2-N-alkansulfonyl-N-alkylamino)pyrimidine-5-carboxylic acid ester of formula (Ib), in which R1, R2, R3 and R4 are identical or different and are each a C1-6-alkyl. A 2-[-1-amino-1-(4-flourophenyl)methylene]-4-alkyl-3-oxo-alkanoic acid ester of formula (IIIb), in which R3 and R4 have the above-mentioned meanings, is reacted with an N-cyano-N-alkylalkanesulfonamide, optionally isolated or prepares in situ, of formula (IVb), in which R1 and R2 have the above-mentioned meanings, to give the final product of formula (Ib).
    Type: Grant
    Filed: March 23, 2004
    Date of Patent: January 10, 2006
    Assignee: Lonza AG
    Inventor: Ulrich Veith
  • Patent number: 6963010
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: November 8, 2005
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski
  • Patent number: 6958416
    Abstract: The invention relates to derivatives of valproyltaurinamide of formula (I) in which R1 and R2 are independently hydrogen, a C1-C6-alkyl group, an arylalkyl group or an aryl group. The derivatives are especially useful for the treatment of epilepsy, affective illness, cognitive disorders, neurodegenerative disease, neuropathic pain syndrome, migraine, stroke, brain ischemia, or head trauma injury.
    Type: Grant
    Filed: March 5, 2002
    Date of Patent: October 25, 2005
    Assignee: Yissum Research Development Company of the Hebrew University of Jerusalem
    Inventors: Meir Bialer, Boris Yagen, Nina Isoherranen
  • Patent number: 6911595
    Abstract: A charge transfer material comprising a basic compound having negative charge and represented by the following general formula (I): (A1-L)n1-A2·M??(I), wherein A1 represents a group having negative charge; A2 represents a basic group; M represents a cation for neutralizing the negative charge of (A1-L)n1-A2; L represents a divalent linking group or a single bond; and n1 represents an integer of 1 to 3. A photoelectric conversion device and a photo-electrochemical cell comprising the charge transfer material. A new nonvolatile pyridine compound, which is a low-viscosity liquid at room temperature, is preferably used for A2.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: June 28, 2005
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Masaru Yoshikawa, Chang-yi Qian
  • Patent number: 6908947
    Abstract: The present invention relates to compounds of formula I, in which X1, X2, X3, X4, Y1, Y2, Y3, Y4, R(3), R(4) and R(5) have the meanings mentioned in the specification, their preparation and their use, in particular in pharmaceuticals. The compounds effect the potassium channel or the IKs channel opened by cyclic adenosine monophosphate (cAMP) and are outstandingly suitable as pharmaceutical active compounds, for example for the prophylaxis and therapy of cardiovascular disorders, in particular arrhythmias, for the treatment of ulcers of the gastrointestinal region or for the treatment of diarrheal disorders.
    Type: Grant
    Filed: October 25, 2001
    Date of Patent: June 21, 2005
    Assignee: Aventis Pharma Deutschland GmbH
    Inventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
  • Patent number: 6900353
    Abstract: The present invention provides compounds of formula (I): useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: May 31, 2005
    Assignee: Eli Lilly and Company
    Inventors: Buddy Eugene Cantrell, Winton Dennis Jones, Jr., Timothy Alan Shepherd, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Patent number: 6743929
    Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: June 1, 2004
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
  • Patent number: 6706755
    Abstract: The present invention provides a method of treating ocular hypertension or glaucoma which comprises administering to an animal having ocular hypertension or glaucoma therapeutically effective amount of a compound represented by the general formula I; wherein a hatched line represents the &agr; configuration, a triangle represents the &bgr; configuration, a straight line, e.g.
    Type: Grant
    Filed: August 26, 2002
    Date of Patent: March 16, 2004
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Robert M. Burk
  • Patent number: 6620858
    Abstract: Disclosed are thermally-stable, colored, photopolymerizable compounds containing a vinyl group which are capable of being copolymerized with reactive vinyl monomers to produce colored compositions such as polyacrylates, polymethacrylates, polystyrene, etc. The compounds exhibit good thermal stability, fastness (stability) to UV-light, good solubility in the reactive monomers and good color strength.
    Type: Grant
    Filed: August 1, 2001
    Date of Patent: September 16, 2003
    Assignee: Eastman Chemical Company
    Inventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook, Jos Simon De Wit, Larry Keith Johnson
  • Patent number: 6596863
    Abstract: Process for producing a nitroetheneamine derivative or its stereoisomer, its tautomer or a salt thereof comprising reacting a compound of the formula with a compound of the formula R6—CH2NO2 to obtain a compound of the formula and reacting the resulting compound with a compound of the formula
    Type: Grant
    Filed: April 29, 2002
    Date of Patent: July 22, 2003
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6583318
    Abstract: A method of synthesizing &agr;-sulfonamido amide, carboxylic acid or hydroxamic acid derivatives comprising providing a set of polymer-bound reactant(s) (sulfonamide, aldehyde or ketone, isocyanide or acid) to react with three sets of the other three reactants to form an array of polymer-bound &agr;-sulfonamido amide-type intermediates and use of such intermediates for the preparation of combinatorial libraries.
    Type: Grant
    Filed: May 15, 2002
    Date of Patent: June 24, 2003
    Assignee: Advanced Syntech, LLC
    Inventors: Eugene Campian, Boliang Lou, Adnan M. M. Mjalli
  • Patent number: 6562782
    Abstract: The present invention related to an oligocycloalkanoid compound comprising formula (I) wherein m, n, and o are independently an integer from 0 to 2; A1 through A10 are independently a direct link, alkylene, alkylene-O—, carbonyl, oxygen, or sulfur; X and Y are independently hydrogen, hydroxy, alkyl, or in combination an electrophilic group; and R1 through R10 are independently hydrogen, hydroxy, alkyl, alkenyl, alkynyl, substituted or unsubstituted aryl, N-, S-, or O-heterocycles, fused or multi-ring aryl with or without hetero ring members, arylalkyl, arylalkenyl, arylalkynyl, alkylphenyl, alkenylphenyl, alkynylphenyl, alkoxy, alkenyloxy, alkynyloxy, substituted or unsubstituted aryloxy, substituted or unsubstituted arylalkoxy, alkylacyl, alkenylacyl, alkynylacyl, arylacyl, aroyl, alkylaroyl, aminoaroyl, aminoalkylacyl, aminoalkyl, aminoalkenyl, aminoalkynyl, amino, alkylamino, alkenylamino, alkynylamino, arylamino, dialkylamino, dialkenylamino, dialkynylamino, arylalkylamino, arylalk
    Type: Grant
    Filed: May 10, 2000
    Date of Patent: May 13, 2003
    Assignee: University of Rochester
    Inventors: Benjamin L. Miller, Robert D. Hubbard
  • Patent number: 6559137
    Abstract: The present invention relates to prodrugs of a class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of prodrugs of HIV aspartyl protease inhibitors characterized by favorable aqueous solubility, high oral bioavailability and facile in vivo generation of the active ingredient. This invention also relates to pharmaceutical compositions comprising these prodrugs. The prodrugs and pharmaceutical compositions of this invention are particularly well suited for decreasing the pill burden and increasing patient compliance. This invention also relates to methods of treating mammals with these prodrugs and pharmaceutical compositions.
    Type: Grant
    Filed: June 23, 2000
    Date of Patent: May 6, 2003
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
  • Patent number: 6451792
    Abstract: A medical composition containing, as an active constituent, a nitroetheneamine derivative represented by the formula (I): wherein the substituents are as defined in the disclosure, its stereoisomers, its tautomers or a salt thereof.
    Type: Grant
    Filed: March 20, 2001
    Date of Patent: September 17, 2002
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
  • Patent number: 6410749
    Abstract: Process for preparing optically active &bgr;-amino alcohols represented by a general formula (2): Ra—C*H(OH)—C*H(Rb)—Rc wherein Ra and Rc are each independently hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, Rb is one member selected from among groups represented by the following general formulae; (3) R1CO(R2)N—, and (4) R1CO(R1′CO)N—, and C* is an asymmetric carbon atom, characterized by reacting a racemic &agr;-aminocarbonyl compound represented by the general formula (1): Ra—CO—CH(Rb)—Rc, with hydrogen in the presence of an optically active transition metal compound represented by a general formula (7): MaXY(Px)m(Nx)n wherein Ma represents a metal atom belonging to VIII-group of the periodic law, X and Y represent each independently hydrogen, halogeno, Px represents a phosphine ligand, Nx represents an amine ligand, at least one of Px and Nx is optically active, and m and n each independently represent 0 or an integer of 1 th
    Type: Grant
    Filed: July 17, 2001
    Date of Patent: June 25, 2002
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Eiji Katayama, Daisuke Sato, Hirohito Ooka, Tsutomu Inoue
  • Patent number: 6387954
    Abstract: The present invention provides certain alkenyl sulphonamide derivatives useful for potentiating glutamate receptor function in a mammal and therefore, useful for treating a wide variety of conditions, such as psychiatric and neurological disorders.
    Type: Grant
    Filed: January 23, 2001
    Date of Patent: May 14, 2002
    Assignee: Eli Lilly and Company
    Inventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
  • Patent number: 6319428
    Abstract: The invention concerns ionic compounds in which the anionic load has been delocalized. A compound disclosed by the invention is comprised of an amide or one of its salts, including an anionic portion combined with at least one cationic portion M+m in sufficient numbers to ensure overall electronic neutrality; the compound is further comprised of M as a hydroxonium, a nitrosonium NO+, an ammonium —NH4+, a metallic cation with the valence m, an organic cation with the valence m, or an organometallic cation with the valence m. The anionic portion matches the formula RF—SOx—N−Z, wherein RF is a perfluorinated group, x is 1 or 2, and Z is an electroattractive substituent. The compounds can be used notably for ionic conducting materials, electronic conducting materials, colorants, and the catalysis of various chemical reactions.
    Type: Grant
    Filed: December 3, 1998
    Date of Patent: November 20, 2001
    Assignees: Hydro-Quebec, Centre National de la Recherche Scientifique
    Inventors: Christophe Michot, Michel Armand, Michel Gauthier, Yves Choquette
  • Patent number: 6284795
    Abstract: The present invention provides compounds having the Formula I The present invention also provides methods of treating or preventing atherosclerosis, coronary heart disease, and restenosis using the compounds of Formula I, and pharmaceutical compositions comprising the compounds of Formula I.
    Type: Grant
    Filed: August 18, 1999
    Date of Patent: September 4, 2001
    Assignee: Warner-Lambert Company
    Inventors: Helen Tsenwhei Lee, Randy Ranjee Ramharack, Bruce David Roth, Karen Elaine Sexton
  • Patent number: 6271262
    Abstract: A compound of formula (I) useful as metalloproteinase inhibitors.
    Type: Grant
    Filed: January 11, 2000
    Date of Patent: August 7, 2001
    Assignee: British Biotech Pharmaceuticals Limited
    Inventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
  • Patent number: 6200967
    Abstract: This invention relates to a compound of the Formula I X—C(O)—Y—G—R  I (wherein X, Y, G and R have the values defined in the description), or a pharmaceutically acceptable salt thereof, processes and intermediates for the preparation of such a compound or salt, pharmaceutical compositions comprising such a compound or salt and methods of their use as thrombin inhibitors, coagulation inhibitors and agents for the treatment of thromboembolic disorders.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: March 13, 2001
    Assignee: Eli Lilly and Company
    Inventors: Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
  • Patent number: 6159989
    Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
    Type: Grant
    Filed: December 15, 1999
    Date of Patent: December 12, 2000
    Assignee: Merck & Co., Inc.
    Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
  • Patent number: 6054613
    Abstract: A process for the preparation of a sulfonamide of formula:RSO.sub.2 NR.sup.1 R.sup.2wherein R represents C.sub.1 -C.sub.10 alkyl; andR.sup.1 and R.sup.2 independently represent hydrogen, C.sub.1 -C.sub.10 alkyl or C.sub.6 -C.sub.10 aryl; which comprises reacting the corresponding alkane- or arenesulfonyl halide of formula:RSO.sub.2 Halwherein Hal represents halogen; with the corresponding compound of formula:NHR.sup.1 R.sup.2in an aqueous solvent and extracting the sulfonamide from the resulting mixture into a polar organic solvent.
    Type: Grant
    Filed: May 24, 1999
    Date of Patent: April 25, 2000
    Assignee: Zeneca Limited
    Inventors: Brian David Gott, James Peter Muxworthy, Stephen Martin Brown
  • Patent number: 6022872
    Abstract: .alpha.- and .beta.-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: February 8, 2000
    Assignee: G. D. Searle & Co.
    Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
  • Patent number: RE43327
    Abstract: The disclosed invention provides new polyamine analogs and derivatives containing a hydrophobic region and a polyamine region as well as methods and compositions for their use.
    Type: Grant
    Filed: January 8, 2002
    Date of Patent: April 24, 2012
    Assignee: Aminex Therapeutics, Inc.
    Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur