C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
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Publication number: 20030191168Abstract: Aryl-benzimidazole compounds according to the formula 1Type: ApplicationFiled: June 6, 2002Publication date: October 9, 2003Applicant: GeneSoft, Inc.Inventors: Dustin L. McMinn, Roland W. Burli, Jacob Kaizerman, Eldon E. Baird, Matthew J. Taylor
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Patent number: 6610714Abstract: Compounds of the formula I: where; R1 is O, S; R2 is an optionally substituted nitrogen-containing heterocycle, wherein the nitrogen is located at the 2 position relative to the (thio)urea bond; R3 is H, C1-C3 alkyl, R4-R7 are independently selected from H, C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, haloC1-C6 alkyl, C1-C6 alkanoyl, haloC1-C6 alkanoyl, C1-C6 alkoxy, haloC1-C6 alkoxy, C1-C6 alkyloxy-C1-C6 alkyl, haloC1-C6 alkyloxy-C1-C6 alkyl hydroxy-C1-C6 alkyl, amino-C1-C6 alkyl, carboxy-C1-C6 alkyl, cyano-C1-C6 alkyl, amino, carboxy, carbamoyl, cyano, halo, hydroxy, keto; X is —(CR8R9)n— R8 and R9 are independently H, C1-C3 alkyl, OH or R8 and R9 together are ═O n is 1, 2 or 3 and prodrugs and pharmaceutically acceptable salts thereof, have utility as inhibitors of HIV-1 reverse transcriptase, particularly drug escape mutants.Type: GrantFiled: March 5, 2002Date of Patent: August 26, 2003Assignee: Medivir ABInventors: Christer Sahlberg, Dmitry Antonov, Hans Wallberg, Rolf Noréen
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Patent number: 6583165Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.Type: GrantFiled: February 21, 2001Date of Patent: June 24, 2003Assignee: Tularik Inc.Inventor: Jonathan B. Houze
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Patent number: 6569874Abstract: The present application describes oxygen and sulfur containing heteroaromatics and derivatives thereof of formula I: or pharmaceutically acceptable salt or prodrug forms thereof, wherein J is O or S and D may be C(═NH)NH2, which are useful as inhibitors of factor Xa.Type: GrantFiled: November 17, 2000Date of Patent: May 27, 2003Assignee: Bristol-Myers Squibb CompanyInventors: James Russell Pruitt, John Matthew Fevig, Mimi Lifen Quan, Donald Joseph Phillip Pinto
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Patent number: 6552042Abstract: The present application describes inhibitors of factor Xa of formula I: or pharmaceutically acceptable salt forms thereof, wherein W, W1, W2, and W3 may be N or C and J, Ja, and Jb combine to form a substituted carbocycle or heterocycle.Type: GrantFiled: January 29, 2001Date of Patent: April 22, 2003Assignee: Bristol-Myers Squibb Pharma CompanyInventors: Qi Han, Celia Dominguez, Eugene C. Amparo, Jeongsook M. Park, Mimi L. Quan, Karen A. Rossi
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Publication number: 20030069290Abstract: The invention provides compounds of Formula I: compounds of the Formula I: 1Type: ApplicationFiled: August 14, 2002Publication date: April 10, 2003Inventors: Donn G. Wishka, Jason K. Myers, Bruce N. Rogers, Eric Jon Jacobsen, David W. Piotrowski, Jeffrey W. Corbett, Alice L. Bodnar, Vincent E. Groppi,
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Patent number: 6544961Abstract: The present invention relates to therapeutic combinations of 3S-[3R*(1R*,2S*)-[3 -[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester (141W94), 3′-azido-3′-deoxythymidine (zidovudine) and (2R, cis)-4-amino-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (3TC) (or, alternatively to 3TC, (2R,cis)-4-amino-5-fluoro-1-(2-hydroxymethyl-1,3-oxathiolan-5-yl)-(1H)-pyrimidin-2-one (FTC) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.Type: GrantFiled: December 18, 1998Date of Patent: April 8, 2003Assignee: SmithKline Beecham CorporationInventors: Martha Heider St. Clair, David Walter Barry
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Patent number: 6534531Abstract: The invention provides a method for preventing or treating alopecia induced by chemotherapy or radiotherapy by administering to a mammalian specie in need thereof a therapeutically effective amount of a compound of formula I or II or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 26, 2001Date of Patent: March 18, 2003Assignee: Bristol-Myers Squibb CompanyInventors: S. David Kimball, Kevin R. Webster, David K. Bol
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Patent number: 6514963Abstract: The present invention comprises methods and compositions for use in inhibiting egg production by parasitic trematode worms comprising administering to an individual in need thereof an effective amount of an agent which transiently inhibits the influx of calcium through a cell membrane calcium channel. Inhibition of egg production in the worms ameliorates many of the symptoms and pathology related to infection by trematode related diseases, including Schistosomiasis. The methods can also effect disease transmission by reducing the number of eggs released into the environment available to continue the worm life cycle.Type: GrantFiled: July 18, 2001Date of Patent: February 4, 2003Assignee: The Regents of the University of CaliforniaInventors: Mark Walter, Armand Kuris
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Patent number: 6511988Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 10, 2001Date of Patent: January 28, 2003Assignee: Isotechnika Inc.Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6509363Abstract: 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: March 16, 2001Date of Patent: January 21, 2003Assignee: Vertex Pharmaceuticals IncorporatedInventors: Francesco Salituro, Guy Bemis, John Cochran
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Patent number: 6495551Abstract: The invention concerns compounds of formula (I), wherein, for example, R1 is of the formula —NHC(═O)Ra wherein Ra is (1-4C)alkyl; R2 and R3 are independently hydrogen or fluoro; R5 and R6 are, for example, hydrogen; R4 is —X—Y—Het.; wherein, for example, X is a direct bond and Y is —(CH2)m— or —CONH—(CH2)m—; or X is —(CH2)n— and Y is —S(O)p—(CH2)m—; or X is —CH2O—or —CH2NH— and Y is —CO—(CH2)m—; wherein n is 1, 2 or 3; m is 0, 1, 2 or 3 and p is 0, 1 or 2; wherein Het. is a heterocyclic ring, unsaturated or saturated, optionally substituted by, for example, (1-4C)alkyl, halo, cyano, nitro or amino; pharmaceutically acceptable salts and in vivo hydrolysable ester thereof; processes for their preparation; pharmaceutical compositions containing them and their use as antibacterial agents.Type: GrantFiled: May 25, 2000Date of Patent: December 17, 2002Inventors: Michael John Betts, Michael Lingard Swain
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Patent number: 6486136Abstract: The present invention relates to therapeutic combinations of [3R*(1R*,2S*)]-[3[[(4-aminophenyl)sulphonyl](2-methylpropyl)-amino]-2-hydroxy-1-phenylmethyl)propyl]carbamic acid, tetrahydro-3-furanyl ester (141W94), 3′-azido-3′-deoxythymidine (zidovudine) and (1S,4R)-cis-4-[2-amino-6(cyclopropylamino)-9H-purin-9-yl]-2-cyclopentene-1-methanol (1592U89) which have anti-HIV activity. The present invention is also concerned with pharmaceutical compositions containing said combinations and their use in the treatment of HIV infections including infections with HIV mutants bearing resistance to nucleoside and/or non-nucleoside inhibitors.Type: GrantFiled: December 18, 1998Date of Patent: November 26, 2002Assignee: SmithKline Beecham CorporationInventors: Martha Heider St. Clair, David Walter Barry
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Patent number: 6486184Abstract: Substituted benzene acetamide compounds which are glucokinase activators and pharmaceutically acceptable salts thereof.Type: GrantFiled: July 13, 2001Date of Patent: November 26, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Robert Francis Kester, Ramakanth Sarabu
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Publication number: 20020165236Abstract: Treatment of Protozoan Infections with new diphenylurea derivatives.Type: ApplicationFiled: December 12, 2001Publication date: November 7, 2002Inventors: Andrea Aschenbrenner, Katharina Aulinger Fuchs, Matthias Dormeyer, Gabriel Garcia, Bernd Kramer, Stefano Pegoraro, Jurgen Kraus, Rolf Krauss, Hans Leban, Wael Saeb, Kristina Wolf
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Publication number: 20020165259Abstract: Compounds of the formula 1Type: ApplicationFiled: March 29, 2002Publication date: November 7, 2002Inventors: David B. Rawlins, S. David Kimball, Kyoung S. Kim, Raj N. Misra, Kevin R. Webster
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Publication number: 20020160986Abstract: Compounds having Formulas 5 and 6 wherein the symbols have the meaning defined in the specification are inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids.Type: ApplicationFiled: March 14, 2002Publication date: October 31, 2002Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020132794Abstract: The present invention is directed to compounds, compositions and methods of inhibiting and treating HIV and related viruses, and methods for cocrystallizing reverse transcriptase in vitro, inhibition of the replication of HIV and related viruses thereof.Type: ApplicationFiled: February 13, 2002Publication date: September 19, 2002Applicant: MEDIVIR ABInventors: Peter Thomas Lind, Rolf Noreen, John Michael Morin, Robert John Ternansky
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Patent number: 6441005Abstract: Oxazolidinones and methods for their synthesis are provided. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. Oxazolidinones as disclosed herein can be readily synthesized and used in a variety of applications including use as antimicrobial agents. In one embodiment, a variety of thioamidomethyloxazolidinones and methods for their synthesis and use are provided.Type: GrantFiled: July 26, 2000Date of Patent: August 27, 2002Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Robert C. Gadwood
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Patent number: 6413997Abstract: 3-(Substituted phenyl)-5-(substituted heterocyclyl)-1,2,4-triazole compounds are useful as insecticides and acaricides. New synthetic procedures and intermediates for preparing the compounds, pesticide compositions containing the compounds, and methods of controlling insects and mites using the compounds are also provided.Type: GrantFiled: October 22, 1999Date of Patent: July 2, 2002Assignee: Dow AgroSciences LLCInventors: Francis E. Tisdell, Peter L. Johnson, James T. Pechacek, Robert G. Suhr, Donald H. DeVries, Carl P. Denny, Mary L. Ash
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Patent number: 6410542Abstract: The current invention discloses aminotetrazole derivatives useful as nitric oxide synthase inhibitors.Type: GrantFiled: October 13, 2000Date of Patent: June 25, 2002Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Donald W. Hansen, Jr., Sofya Tsymbalov
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Patent number: 6407124Abstract: Compounds of the formula and pharmaceutically acceptable salts thereof are provided.Type: GrantFiled: June 10, 1999Date of Patent: June 18, 2002Assignee: Bristol-Myers Squibb CompanyInventors: David B. Rawlins, S. David Kimball, Kyoung S. Kim, Raj N. Misra, Kevin R. Webster
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Patent number: 6388088Abstract: Tetrazolyl-phenyl acetamides are active as glucokinase activators, and are able to increase insulin secretion, which makes them useful for treating type II diabetes.Type: GrantFiled: October 11, 2001Date of Patent: May 14, 2002Assignee: Hoffman-La Roche Inc.Inventor: Achyutharao Sidduri
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Patent number: 6380230Abstract: The present invention relates to cholecystokinin (CCK)-agonist substituted thiazoles of formula: in which R1 is a substituted phenyl group, R2 is a group chosen from CH2—R7, (CH2)2—R7, S—CH2—R7, CH2—S—R7 and (C5-C8)alkyl with R7 being a (C5-C7)cycloalkyl group, and R3 is a group with R8 being a group (CH2)nR15 or and R15 being COOH or COO(C1-C4)alkyl. The invention also relates to a process for the preparation of the pharmaceutical compositions containing them and to their uses for the preparation of medicines.Type: GrantFiled: June 2, 2000Date of Patent: April 30, 2002Assignee: Sanofi-SynthelaboInventors: Roger Brodin, Robert Boigegrain, Eric Bignon, Jean Charles Molimard, Dominique Olliero
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Publication number: 20020049164Abstract: The present invention relates to prodrug compounds of inhibitors of dipeptidyl peptidase IV (DP IV), which prodrug compounds have the general formula A-B-C, whereinType: ApplicationFiled: December 22, 2000Publication date: April 25, 2002Inventors: Hans-Ulrich Demuth, Dagmar Schlenzig, Torsten Hoffmann, Susanne Manhart
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Patent number: 6372769Abstract: The present invention provides 5-carboxanilido-2,4-bis-trifluoromethylthiazoles and their compositions. The compounds and compositions are effective for controlling fungal diseases on plants. They are particularly effective for controlling rice blast.Type: GrantFiled: December 5, 2000Date of Patent: April 16, 2002Assignee: Dow AgroSciences LLCInventor: Frisby Davis Smith
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Patent number: 6358945Abstract: Disclosed are novel aromatic compounds which are useful for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. Also disclosed are pharmaceutical compositions containing and processes of making such compounds.Type: GrantFiled: February 16, 2000Date of Patent: March 19, 2002Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Steffen Breitfelder, Pier F. Cirillo, Thomas A. Gilmore, Eugene R. Hickey, John R. Proudfoot, John R. Regan, Alan D. Swinamer, Hidenori Takahashi
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Patent number: 6355661Abstract: The preparation and use of a protected organic aldehyde is described wherein bioavailability of the orally administered therapeutic aldehyde is improved. The protected aldehyde is prepared by reacting the aldehyde with a protecting group, for example, condensing the aldehyde chemically with a thiazolidine-4-carboxylic acid. The improved bioavailability of such orally administered drugs increases the feasibility of delivering sufficient amounts of vanillin or other therapeutic organic aldehydes in vivo to prevent sickling in sickle cell anemia. Combination therapy is also described wherein a protected organic aldehyde is administered to a subject in treatment of sickle cell anemia in conjunction with one or more other drugs, such as pain killers, used in treatment of the symptoms of sickle cell anemia or sickle cell disease.Type: GrantFiled: March 1, 2001Date of Patent: March 12, 2002Assignee: Medinox, Inc.Inventors: Ching-San Lai, Vassil P. Vassilev, Long-Shiuh Chen
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Publication number: 20020006899Abstract: The invention comprises the use of activity-reducing effectors of dipeptidyl peptidase (DP IV) and DP IV-analogous enzyme activity in the blood of a mammal to lower the blood sugar level and the blood pressure in mammalian organisms.Type: ApplicationFiled: August 17, 2001Publication date: January 17, 2002Inventors: Andrew J. Pospisilik, Hans-Ulrich Demuth, Konrad Glund, Matthias Hoffmann, Christopher H.S. Mcintosh, Ray A. Pederson
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Patent number: 6337338Abstract: Methods for treating diseases associated with the activity of the insulin growth factor-1 receptor (IGF-1R), such as cancer, are provided. Methods for inhibiting cell growth and proliferation, especially of tumor cells, and promoting apoptosis are also provided. Each of these methods employs the use of a heteroaryl-aryl urea compound as an antagonist for IGF-1R.Type: GrantFiled: December 15, 1999Date of Patent: January 8, 2002Assignee: Telik, Inc.Inventors: Michael R. Kozlowski, Robert T. Lum, Steven R. Schow, Hugo O. Villar, Micheal M. Wick
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Patent number: 6331555Abstract: The present invention concerns compounds which can inhibit platelet derived growth factor receptor (PDGF-R) activity, preferably such compounds also inhibit the activity other members of the PDGF-R super family and are selective for members of the PDGF-R super family. The PDGF-R super family includes PDGF-R and PDGF-R related kinases Flt, and KDR. The featured compounds are active on cell cultures to reduce the activity of the PDGF-R and preferably one or more PDGF-R related kinases. An example of a featured compound, A10 (see FIG. 1a), and its ability to inhibit growth of tumor cells in vivo is described below. Using the present application as guide other compounds able to inhibit PDGF-R and preferably Flt and/or KDR can be obtained. Such compounds are preferably used to treat patients suffering from cell proliferative disorders characterized by inappropriate PDGF-R activity.Type: GrantFiled: July 27, 1999Date of Patent: December 18, 2001Assignees: University of California, Yissum Research Development Company of the Hebrew University of Jerusalem, Biosignal LTD, Sugen, Inc., Max-Planck-Gesellschaft zur Forderung der Wissenschaften E.V.Inventors: Klaus P. Hirth, Elaina Mann, Laura K. Shawyer, Axel Ullrich, Istvan Szekely, Tamas Bajor, Janis Haimichael, Laszlo Orfi, Alex Levitzki, Aviv Gazit, Peng Cho Tang, Reiner Lammers
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Patent number: 6329372Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; Het is an optionally substituted heteroaromatic group; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of alpha4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: January 26, 1999Date of Patent: December 11, 2001Assignee: Celltech Therapeutics LimitedInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Patent number: 6320054Abstract: Compounds of the formula: as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance ascribed herein, inhibit binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. These compounds can be used in the form of pharmaceutical preparations for the control or prevention of neoplasms, tumor metastasing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure, as well as infection caused by viruses, bacteria or fungi.Type: GrantFiled: March 15, 2000Date of Patent: November 20, 2001Assignee: Hoffman-La Roche Inc.Inventors: Leo Alig, Albrecht Edenhofer, Kurt Hilpert, Thomas Weller
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Patent number: 6316503Abstract: The invention provides compounds, compositions and methods for modulating the effects of LXR in a cell. The compounds and compositions are useful both as diagnostic indicators of LXR function and as pharmacologically active agents. The compounds and compositions find particular use in the treatment of disease states associated with cholesterol metabolism, particularly atherosclerosis and hypercholesterolemia.Type: GrantFiled: March 14, 2000Date of Patent: November 13, 2001Assignee: Tularik Inc.Inventors: Leping Li, Julio C. Medina, Kevin Lustig, Bei Shan, Hirohiko Hasegawa, Serena T. Cutler, Jiwen Liu, Liusheng Zhu
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Patent number: 6306857Abstract: Disclosed are compounds of formula I: or the pharmaceutically acceptable salts thereof wherein X is a carbonyl, sulfonyl, methylene, or methylene substituted with optionally substituted phenyl; Z is nitrogen or CH; Ar1 and Ar2 independently represent aryl groups; and Y is hydrogen; or Y and R1 or R2 together represent CH2; CH2CH2; CH20; CH2S forming a five or six membered ring and such ring may be optionally substituted with loweralkyl or phenyl; or pharmaceutically acceptable salts thereof, useful in the treatment of neoplastic diseases, and bacterial or fungal infections, and for preventing or decreaseing the production of abnormally phosphorylated paired helical filament (PHF) epitopes associated with Alzheimer's Disease and, therefore for treating Alzheimer's Disease.Type: GrantFiled: August 10, 1999Date of Patent: October 23, 2001Assignee: Molecular Geriatrics CorporationInventors: John Francis DeBernardis, Daniel Joseph Kerkman, Raymond Paul Zinkowski
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Patent number: 6306871Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: September 19, 2000Date of Patent: October 23, 2001Inventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6297266Abstract: Compounds of formula (I) as well as pharmaceutically usable salts and esters thereof, wherein R1, R2 and R3 have the significance described in the specification, inhibit the binding of adhesive proteins to the surface of different types of cell and accordingly influence cell-cell and cell-matrix interactions. They can be used in the form of pharmaceutical preparations in the control or prevention of neoplasms, tumor metastasizing, tumor growth, osteoporosis, Paget's disease, diabetic retinopathy, macular degeneration, restenosis following vascular intervention, psoriasis, arthritis, fibrosis, kidney failure as well as infections caused by viruses, bacteria or fungi.Type: GrantFiled: October 19, 1999Date of Patent: October 2, 2001Assignee: Hoffmann-La Roche Inc.Inventors: Leo Alig, Kurt Hilpert, Thomas Weller
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Patent number: 6294674Abstract: The present invention relates to compounds of Formula I that inhibit matrix metalloproteinases and to a method of inhibiting matrix metalloproteinases using the compounds. wherein Q is an un-natural amino acid. More particurlarly, the present invention relates to a method of treating diseases in which matrix metalloproteinases are involved such as multiple sclerosis, atherosclerotic plaque rupture, restenosis, aortic aneurism, heart failure, periodontal disease, corneal ulceration, burns, decubital ulcers, chronic ulcers or wounds, cancer metastasis, tumor angiogenesis, arthiritis, or other autoimmune or inflammatory diseases dependent upon tissue invasion by leukocytes.Type: GrantFiled: March 2, 1999Date of Patent: September 25, 2001Assignee: Warner-Lambert CompanyInventors: Joseph Armand Picard, Drago Robert Sliskovic
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Patent number: 6288061Abstract: The present invention relates to the imidazole derivative of the following formula (I) wherein R1 is hydrogen, optionally substituted alkyl and the like, R2 is hydrogen, optionally substituted alkyl and the like, R3is optionally substituted heteroaryl, R4 is optionally substituted cycloalkyl, optionally substituted phenyl and the like, provided that when R1 is hydrogen, and R2 and R4 are the same or different and each is phenyl or phenyl substituted by halogen atom, lower alkyl or lower alkoxy, R3 is benzothiazolyl or thiazolyl substituted by phenyl, the imidazole derivative of the following formula (XII) wherein R6 is optionally substituted phenyl or optionally substituted heteroaryl and R7 is substituted phenyl, and pharmaceutically acceptable salts thereof.Type: GrantFiled: June 21, 2000Date of Patent: September 11, 2001Assignee: Welfide CorporationInventors: Hiroyuki Sueoka, Jouji Yasuoka, Akira Nishiyama, Masatoshi Kiuchi, Katsuya Yamamoto, Kunio Sugahara, Syuji Ehara, Kei Sakata
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Patent number: 6281234Abstract: This invention provides compounds of Formula I having the structure wherein R1, R2 are both hydrogen or form a bond, or are each, independently, alkyl of 1-6 carbon atoms or aryl of 6-12 carbon atoms; m=0-10; n=1-3; and p=0-10; with the proviso that m+p is less than or equal to 15; or a pharmaceutically acceptable salt thereof, which are useful in treating metabolic disorders related to insulin resistance or hyperglycemia.Type: GrantFiled: May 10, 1999Date of Patent: August 28, 2001Assignee: American Home Products CorporationInventor: Kenneth L. Kees
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Publication number: 20010006975Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: ApplicationFiled: January 8, 2001Publication date: July 5, 2001Applicant: BAYER CORPORATION and ONYX PHARMACEUTICALS West Haven, CT and Richmond, CA, respectivelyInventors: Jill E. Wood, Hanno Wild, Daniel H. Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: 6251927Abstract: The preparation and use of a protected organic aldehyde is described wherein bioavailability of the orally administered therapeutic aldehyde is improved. The protected aldehyde is prepared by reacting the aldehyde with a protecting group, for example, condensing the aldehyde chemically with a thiazolidine-4-carboxylic acid. The improved bioavailability of such orally administered drugs increases the feasibility of delivering sufficient amounts of vanillin or other therapeutic organic aldehydes in vivo to prevent sickling in sickle cell anemia. Combination therapy is also described wherein a protected organic aldehyde is administered to a subject in treatment of sickle cell anemia in conjunction with one or more other drugs, such as pain killers, used in treatment of the symptoms of sickle cell anemia or sickle cell disease.Type: GrantFiled: April 20, 1999Date of Patent: June 26, 2001Assignee: Medinox, Inc.Inventors: Ching-San Lai, Vassil P. Vassilev, Long-Shiuh Chen
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Patent number: 6239152Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.Type: GrantFiled: January 22, 1999Date of Patent: May 29, 2001Assignee: Pharmacia & Upjohn CompanyInventors: Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
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Patent number: 6225323Abstract: A series of activated iodo-benzamide derivatives are described as antineoplastic and antiviral drug compounds. The compounds generally possess a chelating group, a thiol trapping group and an activating group. The presumptive mechanism of action in preventing cancer cell and virus replication is through inhibition of the binding of transcription factors to zinc finger binding domains. The compounds are effective in inhibiting growth of a variety of human and animal tumor and leukemia cell lines at low concentrations.Type: GrantFiled: August 11, 1998Date of Patent: May 1, 2001Assignee: Joseph KoziakInventors: Randall W. Yatscoff, Robert T. Foster, Selvaraj Naicker
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Patent number: 6214862Abstract: Compounds related to lactacystin and lactacystin &bgr;-lactone, pharmaceutical compositions containing the compounds, and methods of use.Type: GrantFiled: September 11, 1997Date of Patent: April 10, 2001Assignee: President and Fellows of Harvard CollegeInventors: Gabriel Fenteany, Timothy F. Jamison, Stuart L. Schreiber, Robert F. Standaert
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Patent number: 6211373Abstract: This invention relates to novel compounds of Formula (I), and a novel use of these compounds in treating chemokine mediated diseases, wherein the chemokine binds to an IL-8 a or b receptor.Type: GrantFiled: July 8, 1998Date of Patent: April 3, 2001Assignee: SmithKline Beecham CorporationInventors: Katherine Louisa Widdowson, Daniel Frank Veber, Anthony Joseph Jurewicz, Robert Philip Hertzberg, Melvin Clarence Rutledge, Jr.
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Patent number: 6191150Abstract: A family of compounds having the general structural formula where W is a reverse hydroxamic acid group, and R1, R2, R3, R4, R5 and R6 are as described in the specification, or a pharmaceutically acceptable salt, solvate, biohydrolyzable ester, biohydrolyzable amide, affinity reagent, or prodrug thereof.Type: GrantFiled: August 25, 1999Date of Patent: February 20, 2001Assignee: Glaxo Wellcome Inc.Inventors: Robert Carl Andrews, Marc Werner Andersen, Dulce Garrido Bubacz, Joseph Howing Chan, David John Cowan, Michael David Gaul, Daryl Lynn McDougald, David Lee Musso, Michael Howard Rabinowitz, Jennifer Badiang Stanford, Robert William Wiethe
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Patent number: 6191160Abstract: Compounds of the general structural formula I are selective NPY Y5 receptor antagonists. The compounds and compositions of the present invention are useful in the treatment of obesity and complications associated therewith.Type: GrantFiled: November 8, 1999Date of Patent: February 20, 2001Assignees: Merck & Co., Inc., Banyu Pharmaceutical Co., Ltd.Inventors: Ying-Duo Gao, Douglas J. MacNeil, Lihu Yang, Nancy R. Morin, Takehiro Fukami, Akio Kanatani, Takahiro Fukuroda, Yasuyuki Ishii, Masaki Ihara
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Patent number: 6187799Abstract: Methods of treating tumors mediated by raf kinase, with substituted urea compounds, and such compounds per se.Type: GrantFiled: May 22, 1998Date of Patent: February 13, 2001Assignees: Onyx Pharmaceuticals, Bayer CorporationInventors: Jill E Wood, Hanno Wild, Daniel H Rogers, John Lyons, Michael Katz, Yolanda Caringal, Robert Dally, Wendy Lee, Roger A. Smith, Cheri Blum
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Patent number: RE37094Abstract: Compounds of formula in which R1 represents H, an alkyl or a substituted alkyl, R2 represents H or alkyl and R3 represents an optionally substituted cycloalkyl or an optionally substituted aromatic group, which can be a phenyl or a heterocyclic group comprising one or more hetero-atoms chosen from O, S and N, or R2 and R3 considered together represent the group which is optionally substituted on the phenyl ring, and Z represents a heterocycle comprising one or more heteroatoms chosen from O, S and N, fused with an aromatic ring which can comprise a hetero-atom and can be substituted, the said heterocycle being optionally substituted on N, when it comprises such an atom, by an alkyl or a substituted alkyl group, and the salts of these compounds with acids or bases. Use of these compounds as medicaments. No figure.Type: GrantFiled: September 11, 1995Date of Patent: March 13, 2001Assignee: SanofiInventors: Daniel Fréhel, Danielle Gully, Gérard Valette, Jean-Pierre Bras