Chalcogen Bonded Directly To Chalcogen Patents (Class 514/347)
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Patent number: 7235664Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: February 8, 2005Date of Patent: June 26, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Joachim Brendel, Thomas Boehme, Stefan Peukert, Heinz-Werner Kleemann
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Patent number: 7208506Abstract: The present invention relates to compounds of formula I wherein R1, R2 and R3 are defined herein, their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above compounds, medicaments containing them and their manufacture, as well as the use of the above compounds in the control or prevention of illnesses such as cancer.Type: GrantFiled: June 29, 2006Date of Patent: April 24, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Edward Boyd, Frederick Brookfield, Jonathan Gridley, Manfred Kubbies, Raymond Lau, Ulrike Reiff, Georg Tiefenthaler, Wolfgang von der Saal, Thomas von Hirschheydt, Timothy Woodcock
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Patent number: 7160905Abstract: The present invention relates to novel hydroxyethylene compounds having Asp2 (?-secretase. BACE1 or Memapsin) inhibitory activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by elevated ?-amyloid levels or ?-amyloid deposits, particularly Alzheimer's disease.Type: GrantFiled: November 29, 2002Date of Patent: January 9, 2007Assignee: SmithKline Beecham p.l.c.Inventors: Andrew Faller, Peter Henry Milner, John Gerard Ward
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Patent number: 7132425Abstract: The present invention provides a compound according to formula I where the substituent designations are provided in the specification. Pharmaceutical compositions comprising a compound according to formula I are also provided.Type: GrantFiled: December 10, 2003Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Patent number: 7067539Abstract: The invention relates to compounds of the formula a prodrug thereof, or a pharmaceutically acceptable salt, solvate or stereoisomer of the compound or of said prodrug; which exhibit anti-inflammatory and immunodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds and methods of using the compounds for the treatment of various diseases and conditions.Type: GrantFiled: August 7, 2002Date of Patent: June 27, 2006Assignee: Schering CorporationInventors: Joseph A. Kozlowski, Neng-Yang Shih, Brian J. Lavey, Razia K. Rizvi, Bandarpalle B. Shankar, James M. Spitler, Ling Tong, Ronald L. Wolin, Michael K. Wong
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Patent number: 7034159Abstract: The present invention concerns the use of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea in the pharmaceutical field. In particular, it proposes the use of a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridyl)sulphonyl]-urea for the preparation of solid pharmaceutical forms, and likewise a method of synthesis to obtain such a pure and stable polymorphic form of 1-isopropyl-3-[(4-m-toluidino-3-pyridiyl)sulphonyl]-urea.Type: GrantFiled: March 27, 2003Date of Patent: April 25, 2006Assignee: Cosma S.p.A.Inventors: Massimiliano Lussana, Mauro Rainoni
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Patent number: 6960688Abstract: The use of compounds of formula (I), and salts thereof; and pharmaceutically acceptable in vivo cleavable prodrugs of said compound of formula (I); and pharmaceutically acceptable salts of said compound or said prodrugs; in formula (I), Ring C is phenyl or a carbon linked heteroaryl ring substituted as defined within; R1 is an ortho substituent as defined within; n is 1 or 2; A-B is a linking group as defined within; R2 and R3 are as defined within; R4 is hydroxy, hydrogen, halo, amino or methyl; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described.Type: GrantFiled: October 23, 2002Date of Patent: November 1, 2005Assignee: AstraZeneca ABInventors: Roger J Butlin, Thorsten Nowak, Jeremy N Burrows, Michael H Block
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Patent number: 6903216Abstract: This invention encompasses anthranilamides with heteroarylsulfonyl side chain, process for their preparation, their use as medicament or diagnostic aid, and pharmaceutical preparations containing them. Compounds of formula I, in which R1 to R7 have the meanings stated in the claims, act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. They are therefore suitable as novel antiarrhythmic ingredients, such as for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutter.Type: GrantFiled: June 12, 2002Date of Patent: June 7, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Joachim Brendel, Thomas Böhme, Stefan Peukert, Heinz-Werner Kleemann
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Patent number: 6903108Abstract: Fungicidal mixtures comprise as active components a) an amide compound of the formula I A—CO—NR1R2??I in which A is an aryl group or an aromatic or non-aromatic, 5- or 6-membered heterocycle which has from 1 to 3 hetero atoms selected from O, N and S; ?where the aryl group or the heterocycle may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, halogen, CHF2, CF3, alkoxy, haloalkoxy, alkylthio, alkylsulfynyl and alkylsulfonyl; R1 is a hydrogen atom; R2 is a phenyl or cycloalkyl group which may or may not have 1, 2 or 3 substituents which are selected, independently of one another, from alkyl, alkenyl, alkynyl, alkoxy, alkenyloxy, alkynyloxy, cycloalkyl, cycloalkenyl, cycloalkyloxy, cycloalkenyloxy, phenyl and halogen, where the aliphatic and cycloaliphatic radicals may be partially or fully halogenated and/or the cycloaliphatic radicals may be substituted by from 1 to 3 alkyl groups and where the phenyl group may have from 1 to 5 halogen atoms and/orType: GrantFiled: January 14, 2002Date of Patent: June 7, 2005Assignee: BASF AktiengesellschaftInventors: Klaus Schelberger, Maria Scherer, Karl Eicken, Manfred Hampel, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
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Patent number: 6833379Abstract: The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.Type: GrantFiled: March 13, 2002Date of Patent: December 21, 2004Assignee: Pliva Hrvatska d.o.o.Inventors: Darko Filić, Miljenko Dumić, Aleksandar Danilovski, Bo{hacek over (z)}ena Klepić, Ines Fistrić, Marina Ore{hacek over (s)}ić, Jasna Horvat Mikul{hacek over (c)}ić
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Publication number: 20040254223Abstract: The present invention relates to a simple and efficient process for the preparation of amorphous form of torsemide, demonstrated in the X-ray diffraction pattern of FIG. 1.Type: ApplicationFiled: July 30, 2004Publication date: December 16, 2004Inventors: Yatendra Kumar, Om Dutt Tyagi, Nitin Maheshwari
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Publication number: 20040235906Abstract: This invention relates to novel substituted amine derivatives. In other aspects the invention relates to the use of these compounds in a method for therapy and to pharmaceutical compositions comprising the compounds of the invention.Type: ApplicationFiled: January 30, 2004Publication date: November 25, 2004Inventors: Alex Haahr Gouliaev, Dan Peters
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Publication number: 20040229919Abstract: The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.Type: ApplicationFiled: June 21, 2004Publication date: November 18, 2004Applicant: PLIVA HRVATSKA d.o.o.Inventors: Darko Filic, Miljenko Dumic, Aleksandar Danilovski, Bozena Klepic, Ines Fistric, Marina Oresic, Jasna Horvat Mikulcic
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Publication number: 20040171541Abstract: Compounds are provided that complex with the modulating domain of erythropoietin receptor (EPO-R) for use with EPO-R to determine the presence of EPO-R, the ability of other molecules to bind to the modulating domain in competitive assays and to induce a signal by EPO-R into a cell when bound by the subject compounds in a physiological environment. The compounds are characterized by having a six-membered heterocyclic ring comprising at least one nitrogen atom and include substituted triazolopyrimidine, pyridazinone, pyridine and piperidine.Type: ApplicationFiled: July 2, 2003Publication date: September 2, 2004Inventors: Lennart Olsson, Tatjana Naranda
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Publication number: 20040147748Abstract: The present invention provides a compound according to formula I 1Type: ApplicationFiled: December 10, 2003Publication date: July 29, 2004Inventors: Shaoqing Chen, Wendy Lea Corbett, Kevin Richard Guertin, Nancy-Ellen Haynes, Robert Francis Kester, Francis A. Mennona, Steven Gregory Mischke, Yimin Qian, Ramakanth Sarabu, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar
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Publication number: 20040116346Abstract: Compounds are provided that complex with the modulating domain of erythropoietin receptor (EPO-R) for use with EPO-R to determine the presence of EPO-R, the ability of other molecules to bind to the modulating domain in competitive assays and to induce a signal by EPO-R into a cell when bound by the subject compounds in a physiological environment. The compounds are characterized by having a six-membered heterocyclic ring comprising at least one nitrogen atom and include substituted triazolopyrimidine, pyridazinone, pyridine and piperidine.Type: ApplicationFiled: July 3, 2003Publication date: June 17, 2004Inventors: Lennart Olsson, Tatjana Naranda
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Publication number: 20040097559Abstract: Compounds of Formula (I) 1Type: ApplicationFiled: November 6, 2003Publication date: May 20, 2004Inventors: Namal Chithranga Warshakoon, Rodney Dean Bush
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Patent number: 6713497Abstract: The invention provides a method for treating visual field defects in a mammal in need thereof by administering an effective amount of vitamin B6 to the mammal.Type: GrantFiled: March 17, 2003Date of Patent: March 30, 2004Assignee: Brookhaven Science Associates, LLCInventor: Charles R. Ashby, Jr.
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Patent number: 6713498Abstract: Provided, among things, is a method of decreasing intraocular pressure in an animal, including a human, comprising administering an intraocular pressure decreasing amount of a compound of the formula I:Type: GrantFiled: May 30, 2002Date of Patent: March 30, 2004Assignee: Alteon IncorporatedInventor: Martin Gall
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Patent number: 6693137Abstract: 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: February 17, 2004Assignee: Eli Lilly and CompanyInventors: Macklin Brian Arnold, David Michael Bender, Buddy Eugene Cantrell, Winton Dennis Jones, Paul Leslie Ornstein, Richard Lee Simon, Edward C. R. Smith, Eric George Tromiczak, Hamideh Zarrinmayeh, Dennis Michael Zimmerman
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Patent number: 6686388Abstract: The present invention makes available methods and reagents for inhibiting aberrant growth states resulting from hedgehog gain-of-function, ptc loss-of-function or smoothened gain-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule in an amount sufficient to control the aberrant growth state e.g., to agonize a normal ptc pathway or antagonize smoothened or hedgehog activity. The present invention further makes available methods and reagents for ameliorating to consequences of hedgehog loss-of-function, ptc gain-of-function, or smoothened loss-of-function comprising contacting a cell with a compound, such as a polypeptide or small molecule, in an amount sufficient to ameliorate the In certain embodiments, the subject compounds, e.g., a cAMP analog, adenylate cyclase agonist, or cAMP phosphodiesterase inhibitor, regulate cAMP levels, which in turn modulates activity of the hedgehog pathway.Type: GrantFiled: May 29, 2001Date of Patent: February 3, 2004Assignee: Curis, Inc.Inventors: Henryk Dudek, Benxiu Ji
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Patent number: 6667342Abstract: Compounds of formula (I), pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, wherein: Ring X is phenyl or a six membered heteroaryl ring containing one or two ring nitrogens where said nitrogens are optionally oxidised to form the N-oxide; R1 and R2 are substituents as defined within; R3 and R4 are defined within and are alkyl or halo alkyl or together form a halocycloalkyl ring; R5 is a substituent as defined within; Y—Z is a linking group as defined within; are useful in the production of a elevation of PDH activity in a warm-blooded animal such as a human being. Pharmaceutical compositions, methods and processes for preparation of compounds of formula (I) are described.Type: GrantFiled: August 22, 2000Date of Patent: December 23, 2003Assignee: Astrazeneca ABInventors: David S Clarke, Jeremy N Burrows, Paul Ro Whittamore, Roger J Butlin, Thorsten Nowak
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Patent number: 6653331Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO2-pyridinylsulfonyl groups, or p-NO2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.Type: GrantFiled: March 17, 1999Date of Patent: November 25, 2003Assignee: Pharmacia & Upjohn CompanyInventors: Zhiyang Zhao, Alfredo G. Tomasselli, Kenneth A. Koeplinger, Tillie Peterson
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Patent number: 6653332Abstract: The present invention provides pharmaceutical compositions and methods for the treatment of diabetes mellitus using combination therapy. The compositions relate to a compound of Formula I and an antidiabetic agent such as sulfonylureas, biguanides, glitazones, &agr;-glucosidase inhibitors, potassium channel antagonists, aldose reductase inhibitors, glucagon antagonists, activators of RXR, insulin therapy or other anti-obesity agent. The methods include the administration of the combination of compound of Formula I with antidiabetic agent where the two components are delivered in a simultaneous manner, where the compound of Formula I is administered first, followed by the antidiabetic agent, as well as wherein the antidiabetic agent is delivered first followed by the compound of Formula I.Type: GrantFiled: May 2, 2001Date of Patent: November 25, 2003Assignee: Tularik Inc.Inventors: Juan C. Jaen, Jin-Long Chen
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Patent number: 6646005Abstract: Methods for treating hair loss using a composition including a compound having the following structure and pharmaceutically acceptable salts, hydrates, and biohydrolyzable amides, esters, and imides thereof are provided. R1 is —(CH2)n(CHNR7R8)mC(O)R9, wherein n is an integer from 1 to 3, and m is an integer from 0 to 1. R3 and R5each, independently, is chlorine, bromine, iodine and —CH3. R7 and R8 each, independently, is hydrogen or C1 to C4 alkyl. R9 is hydroxy, C1 to C4 alkoxy and —NR7R8. R31 is a hydrogen, chlorine, bromine, iodine, C1 to C4 alkyl, C4 to C6 cycloalklyl, C1 to C4 haloalkyl, C4 to C6 halocycloalkyl, or CH(R10)Ar. Ar is 5-hydroxypyrid-2-yl, 6-hydroxypyrid-3-yl, 6-hydroxypyridazin-3-yl, 6-methioxypyridazin-3-yl N-oxide or 6-hydroxypyridazin-3-yl N-oxide. R10 is hydrogen or C1 to C4 alkyl. R41 is hydroxy or C1 to C4 alkoxy.Type: GrantFiled: February 21, 2002Date of Patent: November 11, 2003Assignee: The University of Texas Southwestern Medical CenterInventors: Lixin Lilly Zhang, Robert Scott Youngquist
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Patent number: 6620827Abstract: Modulators of PPAR&ggr; activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.Type: GrantFiled: December 19, 2000Date of Patent: September 16, 2003Assignee: Tularik Inc.Inventors: Fabienne De la Brouse-Elwood, Jin-Long Chen, Timothy D. Cushing, John A. Flygare, Jonathan B. Houze, Juan C. Jaen, Lawrence R. McGee, Shi-Chang Miao, Steven Marc Rubenstein, Patrick C. Kearney
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Publication number: 20030158151Abstract: The novel active compound combinations of methoximinoacetamide derivatives of the general formula (I), 1Type: ApplicationFiled: October 16, 2002Publication date: August 21, 2003Inventors: Ulrike Wachendorff-Neumann, Thomas Seitz, Herbert Gayer, Ulrich Heinemann, Bernd-Wieland Kruger, Wolfgang Kramer, Lutz Assmann
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Patent number: 6608060Abstract: The present invention relates to inhibitors of p38, a mammalian protein kinase involved cell proliferation, cell death and response to extracellular stimuli. The invention also relates to methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing those compositions in the treatment and prevention of various disorders.Type: GrantFiled: June 14, 1999Date of Patent: August 19, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Guy W. Bemis, Francesco Gerald Salituro, John Patrick Duffy, John E. Cochran, Edmund Martin Harrington, Mark A. Murko, Keith P. Wilson, Michael Su, Vincent P. Galullo
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Publication number: 20030153608Abstract: Stable pharmaceutical preparations, comprising torasemide in noncrystalline form.Type: ApplicationFiled: December 6, 2002Publication date: August 14, 2003Inventors: Markus Maegerlein, Thomas Hantke, Jorg Breitenbach, Jorg Rosenberg
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Patent number: 6583161Abstract: The invention provides compounds, compositions and methods relating to novel aromatic derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: December 12, 2000Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Julio C. Medina
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Publication number: 20030109555Abstract: The present invention relates to Glutathione S-transferase (GST)/Reduced Glutathione (GSH) as a means for the in-vivo release of a drug that has been conjugated to specific electrophilic moieties via a sulfonamide bond. The drug may be an anticancer agent (or one with other therapeutic properties) carrying a free —NH— which has been derivatized by the attachment of an electrophile containing a moiety, such as p-CN— or p-NO 2-pyridinylsulfonyl groups, or p-NO 2- or 2,4 dinitrophenylsulfonyl groups, or suitable derivatives thereof, to make a prodrug. Optionally, the sulfonamide moiety may have attached to it a targeting molecule. The present invention also provides Glutathione S-transferase (GST)/Reduced Gluthathione (GSH) as a means for the release of a protected amino derivative that has been conjugated to specific electrophilic moieties via a sulfonamide bond.Type: ApplicationFiled: March 17, 1999Publication date: June 12, 2003Inventors: ZHIYANG ZHAO, ALFREDO G. TOMASSELLI, KENNETH A. KOEPLINGER, TILLIE PETERSON
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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 -
Patent number: 6562842Abstract: The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.Type: GrantFiled: May 30, 2002Date of Patent: May 13, 2003Assignee: SmithKline Beecham CorporationInventor: Dennis Shinji Yamashita
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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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Patent number: 6555540Abstract: This invention is directed to methods, pharmaceutical compositions and kits comprising an aldose reductase inhibitor (ARI), a prodrug thereof or a pharmaceutically acceptable salt of said ARI or said prodrug and a selective COX-2 inhibitor, a prodrug thereof or a pharmaceutically acceptable salt of said selective COX-2 inhibitor or said prodrug. This invention further relates to methods of using those pharmaceutical compositions for the treatment of diabetic complications such as diabetic neuropathy, diabetic nephropathy, diabetic retinopathy and diabetic cardiomyopathy.Type: GrantFiled: June 23, 2000Date of Patent: April 29, 2003Assignee: Pfizer IncInventor: Banavara L. Mylari
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Patent number: 6545027Abstract: A method of modulating NF-kB transcription factor comprising administering to a human in need thereof an effective amount of a compound having the formula wherein R1 and R3 are independently hydrogen, wherein Ar is optionally substituted phenyl; R2 is selected from the group consisting of pyrrolidine, hexamethyleneamino, and piperidino; or a pharmaceutically acceptable salt of solvate thereof.Type: GrantFiled: June 7, 1995Date of Patent: April 8, 2003Assignee: Eli Lilly and CompanyInventors: David T. Berg, David S. Calnek, Brian W. Grinnell
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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: 6514984Abstract: A method is disclosed for the prevention and treatment of Alzheimer's disease by administering to a human in need thereof an effective amount of a substituted tricyclic sPLA2 inhibitor.Type: GrantFiled: April 12, 2000Date of Patent: February 4, 2003Assignee: Eli Lilly and CompanyInventor: August Masaru Watanabe
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Patent number: 6509379Abstract: Phenylacetic acid derivatives of the formula I where the variables are as disclosed herein, their salts, processes and intermediates for their preparation, and their use for controlling harmful fungi and animal pests.Type: GrantFiled: April 23, 1998Date of Patent: January 21, 2003Assignee: BASF AktiengesellschaftInventors: Herbert Bayer, Hubert Sauter, Klaus Oberdorf, Wassilios Grammenos, Thomas Grote, Reinhard Kirstgen, Bernd Müller, Ruth Müller, Franz Röhl, Eberhard Ammermann, Volker Harries, Gisela Lorenz, Siegfried Strathmann, Norbert Götz, Albrecht Harreus
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Patent number: 6498172Abstract: This invention relates to 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: August 20, 1999Date of Patent: December 24, 2002Assignee: Pfizer Inc.Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
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Patent number: 6498254Abstract: Certain pyridine and quinoline derivatives' which inhibit replication of the retroviruses HIV-1, HIV-2 and human cytomegalovirus (HCMV) are provided. Pharmaceutical compositions useful in methods of treating or inhibiting certain retrovirus infections are described.Type: GrantFiled: October 29, 2001Date of Patent: December 24, 2002Assignee: Uniroyal Chemical Company, Inc.Inventors: Arthur D. Brewer, Stephen E. Cantor, Mark A. Dekeyser, Arthur M. P. Doweyko, John W. Harris, John A. Lacadie, James B. Pierce, Howard L. Plant, William A. Harrison
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Patent number: 6482837Abstract: Compositions comprising antimuscarinic compounds that have been modified to render them substantially irreversible, such as by quaternization of the heterocyclic ring nitrogen, have improved properties when administered intravesically for treatment of bladder diseases, particularly urinary incontinence. Pharmaceutical compositions and methods of treatment using these improved compounds or improved routes of administration re disclosed.Type: GrantFiled: April 23, 1999Date of Patent: November 19, 2002Assignee: University of RochesterInventor: Ronald W. Wood
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Patent number: 6465496Abstract: The present invention is directed to the novel forms of torsemide, designated Form V, amorphous torsemide, Dupont Form 2 solvent adduct, Dupont Form 2 ethanol adduct and Dupont Form 2 isopropanol adduct. Methods for their preparation are also disclosed. The present invention also relates to processes for making torsemide modification I. Pharmaceutical compositions containing the new forms of torsemide and methods of using them are also disclosed.Type: GrantFiled: August 11, 2000Date of Patent: October 15, 2002Assignee: Teva Pharmaceutical Industries, Ltd.Inventors: Judith Aronhime, David Leonov, Marko Kordova, Anchel Schwartz, Ben-Zion Dolitzky
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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
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Patent number: 6448286Abstract: The current invention discloses useful pharmaceutical compositions containing amidino derivative useful as nitric oxide synthase inhibitors.Type: GrantFiled: July 28, 1998Date of Patent: September 10, 2002Assignee: G.D. Searle & Co.Inventors: Donald W. Hansen, Jr., Mark G. Currie, E. Ann Hallinan, Kam F. Fok, Timothy J. Hagen, Arija A. Bergmanis, Steven W. Kramer, Len F. Lee, Suzanne Metz, William M. Moore, Karen B. Peterson, Barnett S. Pitzele, Dale P. Spangler, R. Keith Webber, Mihaly V. Toth, Mahima Trivedi, Foe S. Tjoeng
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Patent number: 6399637Abstract: The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.Type: GrantFiled: November 5, 1999Date of Patent: June 4, 2002Assignee: PLIVA, farmaceutska, kemijska, prehrambena i kozmeticka industrija, dionicko drustvoInventors: Darko Filić, Miljenko Dumić, Aleksandar Danilovski, Bo{haeck over (z)}ena Klepić, Ines Fistrić, Marina Ore{haeck over (s)}ić, Jasna Horvat Mikul{haeck over (c)}ić
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Patent number: 6395718Abstract: The present disclosure relates to a method of inhibiting angiogenesis comprising administering a N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) inhibitor to a patient in need thereof, and a pharmaceutical composition comprising an anti-angiogenic effective amount of a NAALADase inhibitor and a pharmaceutically acceptable carrier.Type: GrantFiled: July 6, 1998Date of Patent: May 28, 2002Assignee: Guilford Pharmaceuticals Inc.Inventors: Barbara S. Slusher, Rena Lapidus
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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: 6384052Abstract: Trisubstituted pyrroles are useful in the control of coccidiosis in poultry.Type: GrantFiled: November 10, 2000Date of Patent: May 7, 2002Assignee: Merck & Co., Inc.Inventors: Tesfaye Bitfu, Danqing D. Feng
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Patent number: 6369273Abstract: The use of a compound of the formula (I): wherein: ring C is phenyl or carbon-linked heteroaryl selected from pyridyl, pyrazinyl, pyrimidinyl and pyridazinyl; and wherein said phenyl or heteroaryl is substituted as defined herein; A—B is selected from NHCO, OCH2, SCH2, NHCH2, trans-vinylene, and ethynylene; R1 is linked to ring C at a carbon ortho to the position of A—B attachment and is defined herein; n is 1 or 2; R2 and R3 are alkyl, haloalkyl or together from cycloalkyl or halocycloalkyl as defined herein; in the manufacture of a medicament for use in the elevation of PDH activity in warm-blooded animals such as humans is described. Salts and esters of compounds of formula (I) are also described.Type: GrantFiled: August 2, 2000Date of Patent: April 9, 2002Assignee: AstraZeneca ABInventor: Roger J Butlin