Substituent Q Is Alkyl Patents (Class 564/98)
-
Publication number: 20140377875Abstract: UV-Absorbing and fluorescent pl markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: THE TEXAS A&M UNIVERSITY SYSTEMInventors: Gyula Vigh, Ming-Chien Li
-
Patent number: 8877969Abstract: 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: GrantFiled: April 13, 2010Date of Patent: November 4, 2014Assignee: FUJIFILM CorporationInventor: Kenji Wada
-
Patent number: 8809577Abstract: 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: GrantFiled: July 20, 2012Date of Patent: August 19, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Stephen James Getty, Peter Michael Murphy, Romain Severac, Alexander Borisovich Shtarov, Hollis Thomas Warren
-
Patent number: 8809584Abstract: 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: GrantFiled: December 21, 2011Date of Patent: August 19, 2014Assignee: Institut Univ. de Ciencia i Tecnologia, S.A.Inventors: Josep Castells Boliart, David Enrique Miguel Centeno, Marta Pascual Gilabert
-
Patent number: 8802895Abstract: 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: GrantFiled: October 18, 2010Date of Patent: August 12, 2014Assignee: Cleveland State UniversityInventors: Bin Su, Aimin Zhou, Yan Xu
-
Patent number: 8796468Abstract: 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: GrantFiled: December 20, 2010Date of Patent: August 5, 2014Assignee: Shionogi & Co., Ltd.Inventors: Tomoyuki Ogawa, Koji Masuda
-
Patent number: 8772343Abstract: 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: GrantFiled: July 6, 2011Date of Patent: July 8, 2014Assignee: Pfizer LimitedInventors: Andrew Simon Bell, Alan Daniel Brown, Russell Andrew Lewthwaite, Manuel Perez-Pacheco, David James Rawson, Robert Ian Storer, Nigel Alan Swain
-
Patent number: 8609897Abstract: 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: GrantFiled: January 29, 2010Date of Patent: December 17, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Matthew Daniels, Jed Hubbs, Thomas Miller
-
Patent number: 8410150Abstract: 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: GrantFiled: March 6, 2008Date of Patent: April 2, 2013Assignee: University Health NetworkInventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
-
Patent number: 8383276Abstract: 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: GrantFiled: June 24, 2010Date of Patent: February 26, 2013Assignees: Toyota Motor Engineering & Manufacturing North America, Inc., Synthonix CorporationInventors: John Muldoon, Gary Allred, Anthony Dotse
-
Publication number: 20120270934Abstract: 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: ApplicationFiled: July 2, 2010Publication date: October 25, 2012Inventors: Craig E. Masse, Scott L. Harbeson, Roger D. Tung
-
Publication number: 20120259128Abstract: 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: ApplicationFiled: December 20, 2010Publication date: October 11, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Tomoyuki Ogawa, Koji Masuda
-
Patent number: 8148422Abstract: 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: GrantFiled: December 15, 2009Date of Patent: April 3, 2012Assignee: Janssen Pharmaceutica, NVInventors: Mark J. Macielag, James J. McNally
-
Patent number: 8115030Abstract: 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: GrantFiled: March 30, 2006Date of Patent: February 14, 2012Assignee: Shionogi & Co., Ltd.Inventors: Toshiaki Masui, Kazuhiro Yoshida
-
Patent number: 7875746Abstract: 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: GrantFiled: May 23, 2006Date of Patent: January 25, 2011Assignee: FUJIFILM CorporationInventor: Kenji Wada
-
Publication number: 20110008680Abstract: 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: ApplicationFiled: June 24, 2010Publication date: January 13, 2011Applicants: Toyota Motor Engineering & Manufacturing North America, Inc., Synthonix CorporationInventors: John Muldoon, Gary Allred, Anthony Dotse
-
Patent number: 7704988Abstract: 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: GrantFiled: October 4, 2006Date of Patent: April 27, 2010Assignee: Merck & Co., Inc.Inventors: Robert J. DeVita, Gregori J. Morriello, Peter Lin
-
Patent number: 7678941Abstract: 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: GrantFiled: July 23, 2007Date of Patent: March 16, 2010Assignee: 3M Innovative Properties CompanyInventors: Patricia M. Savu, William M. Lamanna, Thomas P. Klun
-
Publication number: 20100063322Abstract: 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: ApplicationFiled: November 12, 2007Publication date: March 11, 2010Inventors: Muneharu Miyake, Tadashi Kusama, Takashi Masuko
-
Patent number: 7453010Abstract: 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 optionaType: GrantFiled: May 26, 2003Date of Patent: November 18, 2008Assignee: Sanofi AventisInventors: Philippe R. Bovy, Roberto Cecchi, Tiziano Croci, Olivier Venier
-
Publication number: 20080262264Abstract: 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: ApplicationFiled: March 30, 2006Publication date: October 23, 2008Applicant: Shionogi & Co., Ltd.Inventors: Toshiaki Masui, Kazuhiro Yoshida
-
Patent number: 7411002Abstract: Certain lipophilic polycationic sulfonamides are provided and are useful for treating various diseases or conditions and particularly sepsis.Type: GrantFiled: June 7, 2006Date of Patent: August 12, 2008Assignees: The University of Kansas, Mediquest Therapeutics, Inc.Inventors: Mark R. Burns, Sunil A. David, Scott A. Jenkins
-
Patent number: 7365196Abstract: 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: GrantFiled: March 15, 2001Date of Patent: April 29, 2008Assignees: 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: 7232817Abstract: ?- and ?-amino acid hydroxyethylamino sulfonyl urea derivative compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 27, 2005Date of Patent: June 19, 2007Assignees: G.D. Searle & Co., Monsanto CompanyInventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P. Getman, Gary A. DeCrescenzo, Eric T. Sun
-
Patent number: 7220914Abstract: Zwitterionic compounds, photovoltaic cell charge carrier layers containing such compounds, photovoltaic cells including such charge carrier layers, and related methods are disclosed.Type: GrantFiled: November 30, 2004Date of Patent: May 22, 2007Assignee: Konarka Technologies, Inc.Inventors: Kethinni G. Chittibabu, Savvas Hadjikyriacou, David Waller
-
Patent number: 7169952Abstract: 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: GrantFiled: June 1, 2001Date of Patent: January 30, 2007Assignee: FMC CorporationInventors: Leland A. Smeltz, Thomas C. Sedergran, Harold C. Jarrow
-
Patent number: 6984757Abstract: 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: GrantFiled: March 23, 2004Date of Patent: January 10, 2006Assignee: Lonza AGInventor: Ulrich Veith
-
Patent number: 6963010Abstract: 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: GrantFiled: January 8, 2002Date of Patent: November 8, 2005Assignee: MediQuest Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski
-
Patent number: 6958416Abstract: 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: GrantFiled: March 5, 2002Date of Patent: October 25, 2005Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventors: Meir Bialer, Boris Yagen, Nina Isoherranen
-
Patent number: 6911595Abstract: 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: GrantFiled: June 14, 2002Date of Patent: June 28, 2005Assignee: Fuji Photo Film Co., Ltd.Inventors: Masaru Yoshikawa, Chang-yi Qian
-
Patent number: 6908947Abstract: 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: GrantFiled: October 25, 2001Date of Patent: June 21, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
-
Patent number: 6900353Abstract: 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: GrantFiled: September 28, 2001Date of Patent: May 31, 2005Assignee: Eli Lilly and CompanyInventors: Buddy Eugene Cantrell, Winton Dennis Jones, Jr., Timothy Alan Shepherd, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Patent number: 6743929Abstract: Sulfonamide-containing hydroxyethylamine compounds are effecive as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: September 6, 2000Date of Patent: June 1, 2004Assignee: G. D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel Getman, Gary A. DeCrescenzo, John N. Freskos
-
Patent number: 6706755Abstract: 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: GrantFiled: August 26, 2002Date of Patent: March 16, 2004Assignee: Allergan, Inc.Inventors: David W. Old, Robert M. Burk
-
Patent number: 6620858Abstract: 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: GrantFiled: August 1, 2001Date of Patent: September 16, 2003Assignee: Eastman Chemical CompanyInventors: Michael John Cyr, Max Allen Weaver, Gerry Foust Rhodes, Jason Clay Pearson, Phillip Michael Cook, Jos Simon De Wit, Larry Keith Johnson
-
Patent number: 6596863Abstract: 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 formulaType: GrantFiled: April 29, 2002Date of Patent: July 22, 2003Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Patent number: 6583318Abstract: 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: GrantFiled: May 15, 2002Date of Patent: June 24, 2003Assignee: Advanced Syntech, LLCInventors: Eugene Campian, Boliang Lou, Adnan M. M. Mjalli
-
Patent number: 6562782Abstract: 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, arylalkType: GrantFiled: May 10, 2000Date of Patent: May 13, 2003Assignee: University of RochesterInventors: Benjamin L. Miller, Robert D. Hubbard
-
Patent number: 6559137Abstract: 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: GrantFiled: June 23, 2000Date of Patent: May 6, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Roger Dennis Tung, Michael Robin Hale, Christopher Todd Baker, Eric Steven Furfine, Istvan Kaldor, Wieslaw Mieczylaw Kazmierski, Andrew Spaltenstein
-
Patent number: 6451792Abstract: 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: GrantFiled: March 20, 2001Date of Patent: September 17, 2002Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Fuminori Kato, Keizo Miyata, Hirohiko Kimura, Kazuhiro Yamamoto, Hiroyuki Ikegami, Hiromi Takeo
-
Patent number: 6410749Abstract: 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 thType: GrantFiled: July 17, 2001Date of Patent: June 25, 2002Assignee: Nippon Soda Co., Ltd.Inventors: Eiji Katayama, Daisuke Sato, Hirohito Ooka, Tsutomu Inoue
-
Patent number: 6387954Abstract: 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: GrantFiled: January 23, 2001Date of Patent: May 14, 2002Assignee: Eli Lilly and CompanyInventors: Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
-
Patent number: 6319428Abstract: 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: GrantFiled: December 3, 1998Date of Patent: November 20, 2001Assignees: Hydro-Quebec, Centre National de la Recherche ScientifiqueInventors: Christophe Michot, Michel Armand, Michel Gauthier, Yves Choquette
-
Patent number: 6284795Abstract: 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: GrantFiled: August 18, 1999Date of Patent: September 4, 2001Assignee: Warner-Lambert CompanyInventors: Helen Tsenwhei Lee, Randy Ranjee Ramharack, Bruce David Roth, Karen Elaine Sexton
-
Patent number: 6271262Abstract: A compound of formula (I) useful as metalloproteinase inhibitors.Type: GrantFiled: January 11, 2000Date of Patent: August 7, 2001Assignee: British Biotech Pharmaceuticals LimitedInventors: Raymond Paul Beckett, Fionna Mitchell Martin, Andrew Miller, Richard Simon Todd, Mark Whittaker
-
Patent number: 6200967Abstract: 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: GrantFiled: December 17, 1998Date of Patent: March 13, 2001Assignee: Eli Lilly and CompanyInventors: Valentine J Klimkowski, Aaron L Schacht, Michael R Wiley
-
Patent number: 6159989Abstract: 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: GrantFiled: December 15, 1999Date of Patent: December 12, 2000Assignee: Merck & Co., Inc.Inventors: Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
-
Patent number: 6054613Abstract: 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: GrantFiled: May 24, 1999Date of Patent: April 25, 2000Assignee: Zeneca LimitedInventors: Brian David Gott, James Peter Muxworthy, Stephen Martin Brown
-
Patent number: 6022872Abstract: .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: GrantFiled: September 6, 1996Date of Patent: February 8, 2000Assignee: 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: RE43327Abstract: 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: GrantFiled: January 8, 2002Date of Patent: April 24, 2012Assignee: Aminex Therapeutics, Inc.Inventors: Mark R. Burns, Gerard F. Graminski, Nand Baindur