Q Is Acyclic And Benzene Ring In A Substituent E Patents (Class 514/605)
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Patent number: 6620813Abstract: In accordance with the present invention, there are provided novel chemical entities which have multiple utilities, e.g., as prodrugs of NSAIDs; as dual inhibitors of cyclooxygenase (COX) and 5-lipoxygenase (5-LO); as anticancer agents (through promoting apoptosis and/or inhibiting the matrix metalloproteinases (MMPs)), and the like. Invention compounds comprise a non-steroidal anti-inflammatory agent (NSAID), covalently linked to a hydroxamate. Invention compounds are useful for a variety of applications, such as, for example, treating inflammation and inflammation-related conditions; reducing the side effects associated with administration of anti-inflammatory agents; promoting apoptosis; inhibiting matrix metalloproteinases; and the like.Type: GrantFiled: June 21, 2002Date of Patent: September 16, 2003Assignee: Medinox, Inc.Inventors: Tingmin Wang, Ching-San Lai
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Publication number: 20030171350Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: ApplicationFiled: December 12, 2002Publication date: September 11, 2003Inventors: MacKlin Brian Arnold, David Michael Bender, Andrew Hendley Fray, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6610747Abstract: A compound of general formula (I) wherein R1 and R2 are H, C1-C6alkyl or (CH2)d(C3-C6cycloalkyl) wherein d=0, 1, 2 or 3; or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; Z or Y is —SR3 and the other Z or Y is halogen or —R3; wherein R3 is C1-C4 alkyl optionally substituted with fluorine; except that R3 is not CF3; or Z and Y are linked so that, together with the interconnecting atoms, Z and Y form a fused 5 to 7-membered carbocyclic or heterocyclic ring, and wherein when Z and Y form a heterocyclic ring, in addition to carbon atoms, the linkage contains one or two heteroatoms independently selected from oxygen, sulfur and nitrogen; R4 and R5, which may be the same or different, are: A—X, wherein A=—CH═CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7, SO2NR6R7, SO2NHC(═O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10; or a 5- or 6-membered hetType: GrantFiled: August 27, 2001Date of Patent: August 26, 2003Assignee: Pfizer Inc.Inventors: Mavis Diane Adam, Mark David Andrews, Mark Leonard Elliott, Geoffrey Edward Gymer, David Hepworth, Harry Ralph Howard, Jr., Donald Stuart Middleton, Alan Stobie
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Patent number: 6605641Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z), 14(Z)-dienoic acid and 20-, 21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z), 8(Z), 11(Z), 14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z), 15(Z)-dienoic acid.Type: GrantFiled: December 14, 2001Date of Patent: August 12, 2003Assignee: MCW Research FoundationInventors: Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
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Publication number: 20030144310Abstract: This invention provides a compound having the structure: 1Type: ApplicationFiled: September 24, 2002Publication date: July 31, 2003Inventors: Lakmal W. Boteju, Michael J. Konkel, Joel K. Kawakami, John Wetzel
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Patent number: 6596769Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),4(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.Type: GrantFiled: December 14, 2001Date of Patent: July 22, 2003Assignee: MCW Research FoundationInventors: Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
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Patent number: 6589973Abstract: A clear, stable novel pharmaceutical preparation of selective cyclooxygenase II inhibitors (COX 2) inhibitors in the parenteral form for the treatment of pain & inflammatory conditions arising because of cyclooxygenase-2 activity. In particular the pharmaceutical preparation of COX 2 inhibitors comprise of selective active COX 2 inhibitors selected from Celeoxib, Rofecoxib and their analogs dissolved in a selective isosorbide type solvent of following general formula I where R1 and R2 are hydrogen or alkyl chains containing 1-3 carbons or acetate group. Also disclosed is a simple and cost effective process of manufacture of the above novel pharmaceutical preparation.Type: GrantFiled: May 15, 2002Date of Patent: July 8, 2003Assignee: THEMIS Medicare Ltd.Inventors: Dinesh Shantilal Patel, Sachin Dinesh Patel, Shashikant Prabhudas Kurani
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Aryl sulfonamides and analogues thereof and their use in the treatment of neurodegenerative diseases
Patent number: 6573278Abstract: The present invention relates to new aryl ether sulphonamides and analogues, processes for their preparation and their use for the treatment of neurodegenerative disorders, in particular for the prophylaxis and treatment of neurodegenerative disorders, in particular for the treatment of cerebral apoplexy and craniocerebral trauma.Type: GrantFiled: June 11, 2001Date of Patent: June 3, 2003Assignee: Bayer AktiengesellschaftInventors: Joachim Mittendorf, Jürgen Dressel, Michael Matzke, Jörg Keldenich, Klaus-Helmut Mohrs, Siegfried Raddatz, Jürgen Franz, Peter Spreyer, Verena Vöhringer, Joachim Schuhmacher, Michael-Harold Rock, Ervin Horváth, Arno Friedl, Frank Mauler, Jean Marie Viktor de Vry, Reinhard Jork -
Publication number: 20030100591Abstract: A method of treating or preventing a pathological condition of the uterus in an individual the method comprising administering to the individual any one or more of an inhibitor of cyclooxygenase-2 (COX-2), an inhibitor of prostaglandin E synthase (PGES), or an EP2 or EP4 receptor antagonist. Typically, the pathological condition is uterine cancer, fibroids or endometriosis.Type: ApplicationFiled: October 8, 2002Publication date: May 29, 2003Inventor: Henry Nicolas Jabbour
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Publication number: 20030096807Abstract: A method and solution for perioperatively inhibiting a variety of pain and inflammation processes during arthroscopic procedures. The solution preferably includes a vasoconstrictor that exhibits alpha-adrenergic activity and one or more additional pain and inflammation inhibitory agents at dilute concentration in a physiologic carrier, such as saline or lactated Ringer's solution. The solution is applied by continuous irrigation of a wound during a surgical procedure for peripheral vasoconstriction and inhibition of pain and/or inflammation while avoiding undesirable side effects associated with systemic application of larger doses of the agents.Type: ApplicationFiled: May 1, 2002Publication date: May 22, 2003Applicant: Omeros CorporationInventors: Gregory A. Demopulos, Pamela Pierce Palmer, Jeffery M. Herz
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Publication number: 20030092770Abstract: The present invention provides a method for treating depression, comprising administering to a patient an effective amount of a first component which is a suitable antidepressant, in combination with an effective amount of a second component which is a suitable AMPA receptor potentiator.Type: ApplicationFiled: October 23, 2002Publication date: May 15, 2003Inventor: Phil Skolnick
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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
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Nitromethyl ketone compounds having aldose reduction inhibiting properties and methods for their use
Patent number: 6559185Abstract: The present invention relates to the compounds of formula: in which R1, R2, R3, E, A, X, Z, p and n are as defined herein. These compounds are aldose reductase inhibitors.Type: GrantFiled: November 12, 1999Date of Patent: May 6, 2003Assignee: Merck Patent GmbHInventors: Claude Lardy, Jaques Barbanton, Herve Dumas, Francois Collonges, Philippe Durbin -
Publication number: 20030069312Abstract: The present invention relates to the compounds of formula: 1Type: ApplicationFiled: November 12, 1999Publication date: April 10, 2003Inventors: CLAUDE LARDY, JAQUES BARBANTON, HERVE DUMAS, FRANCOIS COLLONGES, PHILLIPE DURBIN
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Patent number: 6545053Abstract: Compounds having a &bgr;-3 adrenaline receptor agonist and are useful as drugs for the treatment and prevention of diabetes, obesity, hyperlipemia, etc., represented by a general formula (I) and salts thereof, and a process for producing these, and their intermediates, wherein R represents hydrogen or methyl; R1 represents hydrogen, halogen, hydroxy, benzyloxy, amino, or hydroxymethyl; R2 represents hydrogen, hydroxymethyl, NHR3, SO2NR4R4′, or nitro; R6 represents hydrogen or lower alkyl; and X represents methylene, R9 represents hydrogen, one of R7 and R8 represent hydrogen, and the other thereof represents hydrogen, amino, acetylamino, or hydroxy.Type: GrantFiled: November 16, 2000Date of Patent: April 8, 2003Assignee: Asahi Kasei Kogyo Kabushiki KaishaInventors: Shiro Miyoshi, Kohei Ogawa
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Publication number: 20030065034Abstract: Disclosed are intermediates of the formula (A) and methods of making same. The intermediate compounds are useful in the synthesis of heteroaryl/aryl urea compounds.Type: ApplicationFiled: October 4, 2002Publication date: April 3, 2003Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Suresh R. Kapadia, Jinhua J. Song, Nathan K. Yee
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Patent number: 6538016Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6538159Abstract: The invention relates to &agr;-sulfin- and &agr;-sulfonamino acid amides of the general formula I including the optical isomers thereof and mixtures of such isomers, wherein n is a number zero or one; R1 is C1-C12alkyl, C1-C12alkyl substituted with C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1-C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or C3-C6alkenyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl; or a group NR12R13 wherein R12 and R13 are each independently of the other hydrogen or C1-C6-alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently hydrogen; C1-C8alkyl; C1-C8alkyl substituted with hydroxy, mercapto, C1-C4alkoxy or C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered hydrocarbon ring; R4, R5, R6 and R7 are each independently hydrogen or C1-C4alkType: GrantFiled: June 1, 2001Date of Patent: March 25, 2003Assignee: Syngenta Participations AGInventors: Martin Zeller, André Jeanguenat, Clemens Lamberth
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Patent number: 6525099Abstract: The present invention provides certain N-substituted sulfonamide 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: February 25, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Winton Dennis Jones, Paul Leslie Ornstein, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20030036563Abstract: The present invention relates to nimesulide topical formulations comprising a carboxyvinylpolymer neutralized as a gel-forming agent or a polyacrylamide-isoparaffin and a solvent selected from the group consisting of ethanol, isopropanol and diethylene glycol monoethyl ether, and to the process for the preparation thereof. Said formulations have advantages such as higher stability of the system and bioavailability of the active ingredient.Type: ApplicationFiled: September 26, 2002Publication date: February 20, 2003Applicant: HELSINN HEALTHCARE S.A.Inventors: Stefano Bader, Enrique Hausermann, Tiziana Monti
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Patent number: 6515026Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to process for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 18, 2002Date of Patent: February 4, 2003Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20030022934Abstract: The invention relates to novel phenoxyphenyl alkanesulphonates, processes for their preparation, their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment of states of pain and neurodegenerative disordersType: ApplicationFiled: September 26, 2001Publication date: January 30, 2003Inventors: Markus Heil, Heinrich Meier, Paul Naab, Arnd Voerste, Jean-Marie-Viktor De Vry, Dirk Denzer, Frank Mauler, Klemens Lustig, Jan-Bernd Lenfers
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Patent number: 6509499Abstract: The invention concerns novel compound of general formula (1) in which: P, T1, T2, X and n are as defined in claim 1, their tautomeric forms, and their additive salts with pharmaceutically acceptable bases. The invention also concerns methods for preparing these compounds and their applications as medicines. These compounds inhibit the aldose reductase enzyme and can be used in the treatment or prevention of peripheral and autonomous neurological diabetic complications, renal and ocular disorders such as cataract and retinopathy.Type: GrantFiled: March 17, 2000Date of Patent: January 21, 2003Assignee: Merck PatentGesellschaft mitInventors: François Collonges, Hervé Dumas, Claude Lardy, Philippe Durbin
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Publication number: 20030013717Abstract: The invention provides a COX-2 inhibitor or a pharmaceutically acceptable derivative thereof for use in the treatment of constipation.Type: ApplicationFiled: July 25, 2002Publication date: January 16, 2003Inventors: Allen Wyane Mangel, Alan Naylor
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Patent number: 6506733Abstract: Compounds of the formula: are provided, and are useful as cysteine protease inhibitors, particularly in the treatment of diseases such as osteoporosis or autoimmune disorders in which cathepsins K or S contribute to the pathology or symptomatolgy of the disease.Type: GrantFiled: March 15, 2000Date of Patent: January 14, 2003Assignee: Axys Pharmaceuticals, Inc.Inventors: Ann M. Buysse, Rohan V. Mendonca, James T. Palmer, Zong-Qiang Tian, Shankar Venkatraman
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Patent number: 6500865Abstract: The present invention provides certain sulfonamide 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: December 31, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, Thomas John Bleisch, Paul Leslie Ornstein, Edward C. R. Smith, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20020193422Abstract: The presently disclosed invention relates to compounds of general formula I: 1Type: ApplicationFiled: April 26, 2002Publication date: December 19, 2002Inventors: Joachim Brendel, Bernard Pirard
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Patent number: 6495358Abstract: Compounds of the general formula I are provided: and pharmaceutically acceptable salts thereof, wherein, Z is a chemical species or Ri capable of binding at a primary specificity site of a protease; Y is a chemical species reactive to a specific class of protease; each of R2, R3, R5 and R7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls; R4 and R6 are independently selected from the group consisting of: (a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and Ri; (b) —C(O)OH and derivatives thereof, said derivatives selected from the group consisting of —C(O)OQ, —C(O)NRYRZ, —C(O)[NHCHRi(q)C(O)]qOQ, and —C(O)[NHCHRi(q)C(O)]qNRYRZ; and (c) —CHRiNH2 and derivatives thereof, said derivatives selected from the group consisting of —CHRiNHW, —CHRiNHC(O)OQ, —CHRiNHC(O)R, —CHRiNHC(O)NRYRZ, —CHRiNHC(O)[NHCHRi(qType: GrantFiled: April 19, 2000Date of Patent: December 17, 2002Assignee: Wichita State UniversityInventor: William C. Groutas
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Patent number: 6492412Abstract: Prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.Type: GrantFiled: June 29, 2001Date of Patent: December 10, 2002Assignee: Pfizer, Inc.Inventors: Kimberly O. Cameron, Hua Z. Ke, Bruce A. Lefker, Robert L. Rosati, David D. Thompson
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Patent number: 6482859Abstract: The invention relates to novel pesticidally active compounds of the general formula I as well as possible isomers and mixtures of isomers thereof, wherein n is a number zero or one; and R1 is C1-C12alkyl that is unsubstituted or may be substituted by C1-C4alkoxy, C1-C4alkylthio, C1-C4alkylsulfonyl, C3-C8cycloalkyl, cyano, C1C6alkoxycarbonyl, C3-C6alkenyloxycarbonyl or by C3-C6alkynyloxycarbonyl; C3-C8cycloalkyl; C2-C12alkenyl; C2-C12alkynyl; C1-C12haloalkyl: or a group NR11R12 wherein R11 and R12 are each independently of the other hydrogen or C1-C8alkyl, or together are tetra- or penta-methylene; R2 and R3 are each independently of the other hydrogen; C1-C8alkyl; C1-C8alkyl substituted by hydroxy, C1-C4alkoxy, mercapto or by C1-C4alkylthio; C3-C8alkenyl; C3-C8alkynyl; C3-C8cycloalkyl; C3-C8cycloalkyl-C1-C4alkyl; or the two groups R2 and R3 together with the carbon atom to which they are bonded form a three- to eight-membered ring; R4, R5, R6 and R7 are identical or different and are eaType: GrantFiled: February 4, 2000Date of Patent: November 19, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: Martin Zeller, André Jeanguenat
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Publication number: 20020169213Abstract: A method of treating urinary incontinence in a patient in need thereof, the method comprising administering to the patient an effective amount of 2-amino-1-(4-hydroxy-2-methanesulfonamidophenyl)ethanol or a pharmacologically acceptable salt thereof, and pharmaceutical compositions.Type: ApplicationFiled: January 30, 2002Publication date: November 14, 2002Inventors: Pascale Pouzet, Franz Esser, Hisato Kitagawa, Naoki Ishiguro, Ikunobu Muramatsu
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Patent number: 6469040Abstract: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula I. wherein A, R2 and R3 are as described in the specification.Type: GrantFiled: May 21, 2001Date of Patent: October 22, 2002Assignee: G.D. Searle & Co.Inventors: Karen Seibert, Jaime Masferrer, Gary B Gordon
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Patent number: 6458845Abstract: Macrophage scavenger receptor antagonists are provided. Methods of treating cardiovascular disease comprising administration of the present compounds are also provided. The present compounds inhibit lipid accumulation within macrophage-derived foam cells.Type: GrantFiled: December 12, 2001Date of Patent: October 1, 2002Assignee: SmithKline Beecham CorporationInventors: Joseph Weinstock, Robert G. Franz, Dimitri E. Gaitanopoulos
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Patent number: 6455502Abstract: The present invention relates to novel N-cyanomethyl amides which are cysteine protease inhibitors, the pharmaceutically acceptable salts and N-oxides thereof, their uses as therapeutic agents and the methods of their making.Type: GrantFiled: March 15, 2000Date of Patent: September 24, 2002Assignee: AXYS Pharmaceuticals, Inc.Inventors: Clifford M. Bryant, Barry A. Bunin, Erica A. Kraynack, John W. Patterson
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Patent number: 6455581Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: May 25, 1995Date of Patent: September 24, 2002Assignee: G.D. Searle & Co.Inventors: Michael L. Vazquez, Richard A. Mueller, John J. Talley, Daniel P Getman, Gary A. DeCrescenzo, John N. Freskos, Robert M. Heintz, Deborah E. Bertenshaw
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Patent number: 6451302Abstract: A Parenteral Water-miscible non-intensely coloured injectable composition of Non-steroidal anti-inflammatory drugs is disclosed. The invention utilizes solubilization techniques to achieve sufficiently high concentrations of Nimesulide suitable to deliver therapeutic doses in conveniently small volumes using water and without any salt form or complexing agent of Nimesulide. In the composition of the invention all the ingredients of the base are hydrophillic. The hydrophillic base serves the advantage of better miscibility with body fluids, faster drug disposition and better compatibility with the tissue environment.Type: GrantFiled: August 17, 2000Date of Patent: September 17, 2002Assignee: Panacea Biotec LimitedInventors: Amarjit Singh, Rajesh Jain
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Publication number: 20020107282Abstract: The invention relates to a composition containing at least one aminophenol derivative and at least one isoflavonoid. These combinations of active agents show synergism in the depigmentation and/or bleaching of the skin.Type: ApplicationFiled: November 13, 2001Publication date: August 8, 2002Applicant: L'OREALInventors: Veronique Chevalier, Dang-Man Pham
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Patent number: 6414020Abstract: Amidino and benzamidino compounds, including compounds of the formula: wherein R1-R4, R6-R9, Y, Z, n and m are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof, that inhibit a number of proteolytic enzymes are described. Also described are methods for preparing the compounds of Formula I.Type: GrantFiled: May 9, 2001Date of Patent: July 2, 2002Assignee: 3- Dimensional Pharmaceuticals, Inc.Inventors: Tianbao Lu, Bruce E. Tomczuk, Carl R. Illig, Richard M. Soll
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Patent number: 6403630Abstract: Cancers associated with overexpression of HER-2/neu are treated with a selective inhibitor of cyclooxygenase-2 as the sole treating agent or said inhibitor in combination regimen with HERCEPTIN® and/or standard therapy. Uses include adjuvant therapy for HER-2/neu positive breast cancer and treatment of HER-2/neu positive breast cancer that has metastasized.Type: GrantFiled: June 22, 2001Date of Patent: June 11, 2002Assignee: Cornell Research Foundation, Inc.Inventors: Andrew J. Dannenberg, Kotha Subbaramaiah
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Patent number: 6395781Abstract: 20-HETE agonists and antagonists are disclosed along with therapeutic applications. In a preferable form of the invention, the 20-HETE agonists are selected from the group consisting of 21-hydroxyheneicosa-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid, 20-hydroxyeicosa-5(Z),14(Z)-dienoic acid and 20-,21-dimethyl 20-HETE. Preferable 20-HETE antagonists include 5(S)-HETE, 15(S)-HETE, 19(S)-HETE, 19-hydroxynonadeca-5(Z),8(Z),11(Z),14(Z)-tetraenoic acid and 20-hydroxyeicosa 6(Z),15(Z)-dienoic acid.Type: GrantFiled: February 23, 1999Date of Patent: May 28, 2002Assignee: MCW Research FoundationInventors: Richard J. Roman, John R. Falck, Magdalena Alonso-Galicia, Elizabeth R. Jacobs, David R. Harder
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Patent number: 6391918Abstract: Novel &agr;-amino acid amides of formula (I) as well as possible isomers and mixtures of isomers thereof, wherein the substituents are defined as follows: n is the number zero or one; R1 is optionally substituted alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl; or a group NRaRb wherein Ra and Rb are each independently of the other hydrogen, alkyl or form together an alkylene bridge; R2 is hydrogen or alkyl; R3 is optionally substituted aryl or heteroaryl; A is alkylene; and B is optionally substituted aryl; with the exception of the following compounds 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methylphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-chlorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-nitrolphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-methoxyphenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-(4-fluorophenyl)-sulfonylamino-acetamide, 2-phenyl-N-(1-phenyl-ethyl)-2-phenyl-sulfonylamino-acetamide and 2-phenyl-N-(1-pType: GrantFiled: August 25, 2000Date of Patent: May 21, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller
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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
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Patent number: 6380199Abstract: A method of treating ADHD comprising administering a 5-HT6 receptor antagonist according to formula (A) hereinbelow: wherein: P is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; A is a single bond, a C1-6alkylene or a C1-6alkenylene group; R1 is halogen, C1-6alkyl optionally substituted by one or more halogen atoms, C3-6cycloalkyl, C1-6alkoxy, OCF3, hydroxy, hydroxyC1-6alkyl, hydroxyC1-6alkoxy, C1-6alkoxyC1-6alkoxy, C1-6alkanoyl, nitro, amino, C1-6alkylamino or diC1-6alkylamino, cyano or R1 is phenyl, naphthyl, a bicyclic heterocyclic ring or is a 5 to 7-membered heterocyclic ring each containing 1 to 4 heteroatoms selected from oxygen, nitrogen or sulphur; n is 0, 1, 2, 3, 4, 5 or 6, R2 is hydrogen, C1-6 alkyl or aryl C1-6 alkyl; R3 is a group R5 or together with R5 forms a group (CH2)2O or (CH2)3O or R3 is linked to R2 to form a group (CH2)2 or (CH2)3; R4 is &mdashType: GrantFiled: April 17, 2001Date of Patent: April 30, 2002Assignee: SmithKline Beechan p.l.c.Inventors: Charles Alan Reavill, Carol Routledge
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Publication number: 20020035156Abstract: This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing cardiovascular disorders.Type: ApplicationFiled: September 6, 2001Publication date: March 21, 2002Inventors: Barbara Roniker, Richard J. LaChapelle, Daniel T. Connolly, Karen Seibert, Philip Needleman
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Patent number: 6358981Abstract: The present invention relates to the potentiation of glutamate receptor function using certain sulphonamide derivatives. It also relates to novel sulphonamide derivatives, to processes for their preparation and to pharmaceutical compositions containing them.Type: GrantFiled: January 23, 2001Date of Patent: March 19, 2002Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Andrew Hendley Fray, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Publication number: 20020032236Abstract: The present invention relates to a method of treatment of dermatological diseases characterized by accumulation of polymorphonuclear leukocytes by use of Nimesulide or of a physiologically equivalent form thereof.Type: ApplicationFiled: June 19, 2001Publication date: March 14, 2002Inventors: Giuliana Villa, Fabio Macchi, Maurizio Bevilacqua
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Publication number: 20020016369Abstract: The invention relates to a method of treatment of psoriatic arthritis comprising the administration to patients in need of such treatment of an effective amount of Nimesulide or of a physiologically equivalent form thereof.Type: ApplicationFiled: June 13, 2001Publication date: February 7, 2002Inventors: Giuliana Villa, Fabio Macchi, Piercarlo Scarzi-Puttini
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Patent number: 6342531Abstract: A pharmaceutical composition for the prophylaxis and therapy of brain tissue impairment, which contains, as an active ingredient, a compound of the following formula (I) wherein R1 represents an alkyl group having 1-4 carbon atoms or an aryl group having 6-10 carbon atoms which is optionally substituted; R2 and R3 may be the same or different and each represents hydrogen or an alkyl group having 1-4 carbon atoms or R2 and R3 may jointly form a ring having 3-7 carbon atoms; and R4 represents a lower alkyl group which is optionally substituted by aryl, cycloalkyl, or aromatic heterocyclic residue, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: September 19, 2000Date of Patent: January 29, 2002Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Mitsuyoshi Azuma, Yukuo Yoshida, Yuji Sakamoto, Jun Inoue
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Patent number: 6333349Abstract: 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: June 29, 1999Date of Patent: December 25, 2001Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Hans Jochen Lang, Uwe Gerlach
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Patent number: RE38103Abstract: The Compound of Formula I and pharmaceutically acceptable sales thereof in the treatment of cyclooxygenase-2 mediated diseases are disclosed.Type: GrantFiled: April 6, 2001Date of Patent: April 29, 2003Assignee: Merck Frosst Canada & Co.Inventors: Daniel Guay, Chun-Sing Li