Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/335)
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Dye-forming coupler, silver halide photographic light-sensitive material and azomethine dye compound
Publication number: 20030073047Abstract: A dye-forming coupler of formula (I), a silver halide photographic light-sensitive material containing the coupler, and an azomethine dye that can be derived from the dye-forming coupler: 1Type: ApplicationFiled: March 27, 2002Publication date: April 17, 2003Inventors: Kiyoshi Takeuchi, Shigeki Uehira, Mario Aoki, Jun Ogasawara, Yasuhiro Shimada, Seiji Ichijima, Yasuaki Deguchi, Naoto Matsuda, Akira Ikeda, Hisashi Mikoshiba, Masahara Sugai, Taiji Katsumata -
Patent number: 6548523Abstract: The present invention is a process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: that includes preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof:Type: GrantFiled: June 4, 2002Date of Patent: April 15, 2003Assignee: SmithKline Beecham CorporationInventors: Ronnie Maxwell Lawrence, Alan Millar
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Patent number: 6544604Abstract: The present invention provides a liquid crystalline compound having a difluoropropyleneoxy group as a bonding group, which is represented by Formula (1): wherein R1 and R2 each independently represent hydrogen, halogen, a cyano group or an alkyl group having 1 to 20 carbon atoms; rings A1 to A5 each independently represent a 1,4-cyclohexylene group, a 1,4-cyclohexenylene group or a 1,4-phenylene group; Z1 to Z4 each independently represent a single bond, —CH2CH2—, —CH2O—, —OCH2—, —COO—, —OCO—, —CH═CH—, —C≡C—, —CF2O— or —OCF2—; Y1, Y2, Y3 and Y4 each independently represent hydrogen or fluorine; and k, l, m and n each independently represent 0 or 1. This liquid crystalline compound has a large absolute value (|&Dgr;&egr;|) of a dielectric anisotropy and shows a relatively small refractive anisotropy.Type: GrantFiled: August 10, 2001Date of Patent: April 8, 2003Assignees: Chisso Corporation, Chisso Petrochemical CorporationInventors: Shuichi Matsui, Yasuyuki Sasada, Kazutoshi Miyazawa, Hiroyuki Takeuchi, Katsuyuki Kawano, Yasuhiro Kubo, Etsuo Nakagawa, Mayumi Furuya
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Publication number: 20030064992Abstract: 1Type: ApplicationFiled: June 26, 2002Publication date: April 3, 2003Inventors: Karl-Heinz Altmann, Guido Bold, Pascal Furet, Paul William Manley, Jeanette Marjorie Wood, Stefano Ferrari, Francesco Hofmann, Jurgen Mestan, Andreas Huth, Martin Kruger, Dieter Seidelmann, Andreas Menrad, Martin Haberey, Karl-Heinz Thierauch
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Publication number: 20030064332Abstract: A dye-forming coupler of formula (I): 1Type: ApplicationFiled: March 27, 2002Publication date: April 3, 2003Inventors: Kiyoshi Takeuchi, Shigeki Uehira, Mario Aoki
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Patent number: 6541505Abstract: This invention is directed to an (aminoiminomethyl or aminomethyl)benzoheteroaryl compound of formula I which is useful for inhibiting the activity of Factor Xa by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.Type: GrantFiled: June 30, 2000Date of Patent: April 1, 2003Assignee: Aventis Pharmaceuticals Inc.Inventors: William P. Dankulich, Daniel G. McGarry, Christopher Burns, Timothy F. Gallagher, Francis A. Volz
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Patent number: 6537996Abstract: Compounds of formula 1 are effective modulators of p38 MAP kinase. wherein R1 is H, lower alkyl, or OR5, where R5 is aryl, heterocyclyl, acyl, N—R6-4-piperidinyl, N—R6-4-piperidinylmethyl, or N—R6-4-pipelidinylethyl, where aryl and heterocyclyl are substituted with 1-3 R6 substituents selected from the group consisting of H, lower alkyl, lower alkenyl, OH, NO2, NH2, halo, trihalomethyl, —CN, SH, SO, SO2, SO3H, —OR, —COR, —COOR, —CONHR, —OCOR, and —NCOR, where R is lower alkyl; R2 is H or lower alkyl; R3 is aryl substituted with 1-3 R6 substituents; R4 is H, lower alkyl, aryl, aralkyl, —OH, —NH2, —NHR, or —OR, where R is lower alkyl or aryl-lower alkyl; and A is —CH— or —N—; and pharmaceutically acceptable salts thereof.Type: GrantFiled: February 23, 2001Date of Patent: March 25, 2003Assignee: Iconix Pharmaceuticals, Inc.Inventors: David J. Morgans, Jr., Silke Thode, Dongxu Sun
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Patent number: 6534492Abstract: Novel uracil substituted phenyl sulfamoyl carboxamides I and salts thereof, where A=oxygen or sulfur; X1=H, halogen, C1-C4-alkyl; X2=H, CN, CS—NH2, halogen, C1-C4-alkyl, C1-C4-haloalkyl; X3=H, CN, C1-C6-alkyl, C1-C6-alkoxyalkyl, C3-C7-cycloalkyl, C3-C6-alkenyl, C3-C6-alkynyl, optionally substituted benzyl; R1, R2=H, halogen, optionally substituted hydroxy, C1-C10-alkyl, C2-C10-alkenyl, C3-C10-alkynyl, C3-C7-cycloalkyl, phenyl, benzyl or C5-C7-cycloalkenyl, or R1+R2 together with the atom to which they are attached form 3- to 7-membered heterocyclic ring; Q is selected from Q1 to Q40 as defined in the description. Use: As herbicides; for the desiccation/defoliation of plants.Type: GrantFiled: May 4, 2001Date of Patent: March 18, 2003Assignee: BASF AktiengesellschaftInventors: Marianne Carlsen, Michael Anthony Guaciaro, James Jan Takasugi
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Publication number: 20030050247Abstract: Compositions and methods for inhibiting and controlling the growth of microbes are disclosed. The composition comprises at least one chemically-modified peptide with antimicrobial activity and at least one carrier. The method comprises of administering an amount, effective for the prevention, inhibition and termination of microbial growth for industrial, pharmaceutical, household and personal care use.Type: ApplicationFiled: June 15, 2001Publication date: March 13, 2003Inventors: Carla H. Kuhner, James A. Romesser
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Publication number: 20030040625Abstract: This invention provides a class of therapeutic compounds and methods for the treatment of mammals with physiological disorders, such as for example a frequently occurring type of essential hypertension, which are critically associated with the decreased binding of magnesium to the plasma membranes of their cells. These methods consist of administering to a mammal in need of such treatment a compound selected from a series of disubstituted trans, trans 1,3-butadienes, 1,3-disubstituted perhydrobutadienes, 1,2-disubstituted trans ethylenes and 1,2 disubstituted ethanes and disubstitutedpropanes, each of which embodies, in common, the unique structural feature essential for the biological activity of these compounds. This invention also provides for pharmaceutical formulations that employ these novel compounds.Type: ApplicationFiled: August 29, 2002Publication date: February 27, 2003Inventor: Ibert Clifton Wells
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Patent number: 6525059Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula IA wherein R1, R 2, R3 and R4 are as described in the specification.Type: GrantFiled: February 24, 2000Date of Patent: February 25, 2003Assignee: G. D. Searle & CompanyInventors: Ashok Anantanarayan, Michael Clare, Paul W. Collins, Joyce Zuowu Crich, Rajesh Devraj, Daniel L. Flynn, Lifeng Geng, Matthew J. Graneto, Cathleen E. Hanau, Gunnar J. Hanson, Susan J. Hartmann, Michael Hepperle, He Huang, Francis J. Koszyk, Shuyuan Liao, Suzanne Metz, Richard A. Partis, Thao D. Perry, Shashidhar N. Rao, Shaun Raj Selness, Michael S. South, Michael A. Stealey, John Jeffrey Talley, Michael L. Vazquez, Richard M. Weier, Xiangdong Xu, Ish K. Khanna, Yi Yu
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Patent number: 6525001Abstract: Compounds of formula (I), and their N-oxides and agriculturally suitable salts, are disclosed which are useful for controlling undesired vegetation, wherein J is (J-1), (J-2), (J-3), (J-4), (J-5), (J-6) or (J-7); and J, W, X, Y, Z, A, R1-R8 are as defined in the disclosure. Also disclosed are compositions containing the compounds of formula (I) and a method for controlling undesired vegetation which involves contacting the vegetation or its environment with an effective amount of a compound of formula (I).Type: GrantFiled: June 2, 2000Date of Patent: February 25, 2003Assignee: Mid-American Commercialization CorporationInventors: Gerard Michael Koether, Thomas Paul Selby, Thomas Martin Stevenson
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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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Patent number: 6521626Abstract: Compounds of formula (1): wherein R1 is a hydrogen atom or an optionally substituted cycloaliphatic, polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; Alk1 is an optionally substituted aliphatic or heteroaliphatic chain; L1 is a linker atom or group; r and s is each zero or an integer 1; R2 and R3, which may be the same or different, is each a hydrogen or halogen atom or a straight or branched alkyl, haloalkyl, alkoxy, haloalkoxy, hydroxyl or nitro group; Alk2 is a straight or branched alkylene chain; m is zero or an integer 1; R4 is a hydrogen atom or a methyl group; R5 is a hydrogen atom or a straight or branched alkyl group; R6 is a group —(CH2)tR7 in which t is zero or the integer 1 and R7 is an optionally substituted polycycloaliphatic, heterocycloaliphatic, polyheterocycloaliphatic, aromatic or heteroaromatic group; R is a carboxylic acid (—CO2H) or a derivative thereof; and the salts, solvates and hydrates theType: GrantFiled: March 23, 1999Date of Patent: February 18, 2003Assignee: Celltech R&D LimitedInventors: Sarah Catherine Archibald, John Clifford Head, Graham John Warrellow, John Robert Porter
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Patent number: 6521610Abstract: 4-Haloalkyl-3-heterocyclylpyridines and 4-haloalkyl-5-heterocyclyl-pyrimidines, processes for their preparation, compositions comprising them, and their use as pesticides The present invention relates to 4-haloalkyl-3-heterocyclylpyridines and 4-haloalkyl-5-heterocyclylpyrimidines of the formula (I), to processes for their preparation, to compositions comprising them, and to the use of these compounds for controlling animal pests, in particular insects, spider mites, ectoparasites and helminths. In the formula (I), Q is a 5-membered heterocyclic group which is optionally substituted by halogen or organic radicals, Y is halo-C1-C6-alkyl, X is CH or N and m is 0 or 1.Type: GrantFiled: March 14, 2001Date of Patent: February 18, 2003Assignee: Hoechst Schering AgrEvo GmbHInventors: Jörg Tiebes, Thomas Taapken, Burkhard Rook, Manfred Kern, Ulrich Sanft
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Patent number: 6518285Abstract: Piperidinyloxy, pyrrolidinyloxyl and azetidinyloxy compounds of the formula: wherein R1 is a piperidinyl, pyrrolidinyl or azetidinyl moiety as described herein and in which the substituents have the meaning indicated in the description. These compounds are useful as antibacterial agents.Type: GrantFiled: December 5, 2000Date of Patent: February 11, 2003Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Michele A. Weidner-Wells, Christine Boggs, Dennis Hlasta, Erin Nelson
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Patent number: 6518425Abstract: Processes for the preparation of 1,3-oxathiolane nucleosides are provided that include efficient methods for the preparation of the 1,3-oxathiolane ring and subsequent condensation of the 1,3-oxathiolane with a pyrimidine or purine base. Using the processes described herein, the compounds can be provided as isolated enantiomers.Type: GrantFiled: May 15, 2000Date of Patent: February 11, 2003Assignees: Emory University, Triangle Pharmaceuticals, Inc.Inventors: George R. Painter, Dennis C. Liotta, Merrick R. Almond, Darryl G. Cleary, Josè D. Soria, Marcos Sznaidman
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Publication number: 20030028023Abstract: The invention relates to a method of preparing lithium complex salts and their intermediaries and to the use of these in electrolytes.Type: ApplicationFiled: July 10, 2002Publication date: February 6, 2003Inventors: Andrei Leonov, Armin de Meijere, Michael Schmidt
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Publication number: 20030013881Abstract: The present invention is directed toward substituted hydroxyethylene compounds of formulas (XII) (XIII), and (XIV) 1Type: ApplicationFiled: September 21, 2001Publication date: January 16, 2003Inventors: Roy Hom, Shumeye Mamo, Jay Tung, Andrea Gailunas, Varghese John, Lawrence Fang
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Patent number: 6506755Abstract: 5-Arylidene-4-oxo-2-thioxo-3-thiazolidinecarboxylic acids of formula I in which the symbols R1, R2, A, A1 and A2 have the significance given in the description as medicaments for the treatment of cancer diseases.Type: GrantFiled: January 23, 2001Date of Patent: January 14, 2003Assignee: Hoffmann-La Roche Inc.Inventors: Walter-Gunar Friebe, Hans-Willi Krell, Sabine Woelle, Hans-Peter Wolff
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Publication number: 20030008882Abstract: The present invention relates to compounds and pharmaceutical compositions which are proteomimetic and to methods for inhibiting the interaction of an alpha-helical protein with another protein or binding site. Methods for treating diseases or conditions which are modulated through interactions between alpha helical proteins and their binding sites are other aspects of the invention.Type: ApplicationFiled: May 8, 2002Publication date: January 9, 2003Inventors: Andrew D. Hamilton, Justin Ernst, Brendan P. Orner
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Publication number: 20030008884Abstract: The invention relates to compounds of formula (I), and also to salts thereof, which have fungicidal activities: 1Type: ApplicationFiled: August 6, 2001Publication date: January 9, 2003Applicant: Aventis CropScience S.A.Inventors: Vincent Gerusz, Darren James Mansfield, Jose Perez, David Tickle, Jean-Pierre Vors, Derek Baldwin, Thomas Lawley Hough, Dale Robert Mitchell
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Patent number: 6503912Abstract: The present application relates to novel guanidine derivatives of the formula (I) in which R1 represents a five- or six-membered heterocyclic group; R2 represents hydrogen or alkyl, R3 represents the groupings —OR4, —OCOR5, —OCOOR6, —OCONR7R8 and —OSO2R9, where R4, R5 and R6 independently of one another represent alkyl, alkoxyalkyl, halogenoalkyl, alkenyl, alkinyl, alkylaminoalkyl, dialkylaminoalkyl, optionally substituted cycloalkyl and in each case optionally substituted phenyl or benzyl, R7 and R8 independently of one another represent hydrogen, alkyl, alkenyl and in each case optionally substituted phenyl or benzyl and R9 represents alkyl or optionally substituted phenyl, A represents the groupings —CH2CH2—, (CH2)3 and —CH═CH— and z represents cyano or nitro, with the proviso that, if Z represents NO2 and A represents —CH2CH2—, the radical R2 represents hydrogen; and the compound of the formula (I) in whichType: GrantFiled: June 28, 2000Date of Patent: January 7, 2003Assignee: Bayer AktiengesellschaftInventors: Klaus Wagner, Christoph Erdelen, Wolfram Andersch, Ulrike Wachendorff-Neumann, Andreas Turberg, Norbert Mencke
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Patent number: 6500950Abstract: Benzylidenepyrazolones of the formula I, where the substituents and the index n have the following meanings: R1 is unsubstituted or substituted C1-C6-alkyl; R2 is unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, halogen, nitro, cyano; R3 is hydrogen, halogen, nitro, cyano, a group NR5R6, OCOR5, NR5COR6, CO2R5, —COSR5, —CONR5R6, C1-C4-alkoxyiminoalkyl, C1-C6-alkylcarbonyl, unsubstituted or substituted C1-C6-alkyl, unsubstituted or substituted C1-C6-alkoxy, unsubstituted or substituted C1-C6-alkylthio, unsubstituted or substituted C2-C6-alkenyl, unsubstituted or substituted C2-C6-alkynyl, unsubstituted or substituted phenyl, unsubstituted or substituted phenoxy, an unsubstituted or substituted 5- or 6-membered saturated or unsaturated heterocycle which may contain up to 4 nitrogen atoms and/or up to 2 oxygen or sulfur atoms as ring members; R4 is C1-C6-alkyl, C1-C4-haloalkyl; R3 and R4 form an optionally substituted saturated or unsaturatedType: GrantFiled: January 22, 2001Date of Patent: December 31, 2002Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Matthias Witschel, Stefan Engel, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Martina Otten, Karl-Otto Westphalen, Helmut Walter
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Patent number: 6500832Abstract: &agr;- and &bgr;-amino acid hydroxyethylamino sulfonamide compounds are effective as retroviral protease inhibitors, and in particular as inhibitors of HIV protease.Type: GrantFiled: March 14, 2000Date of Patent: December 31, 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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Publication number: 20020198207Abstract: Compounds of the formula 1Type: ApplicationFiled: May 22, 2002Publication date: December 26, 2002Inventors: John Charles Kath, Matthew Frank Brown, Christopher Stanley Poss
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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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Publication number: 20020193562Abstract: Hydroxamic acids are provided which are ACE and/or NEP inhibitors and have the structure 1Type: ApplicationFiled: February 9, 2001Publication date: December 19, 2002Inventor: Jeffrey A. Robl
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Patent number: 6495688Abstract: Disclosed are compounds of formula wherein Ar represents an aryl or heteroaryl group; and R1, R2, R3, R4 and R5 represent organic or inorganic substituents, which compounds are highly selective partial agonists or antagonists at human CRF1 receptors and, thus, are useful in the diagnosis and treatment of treating stress related disorders such as post trumatic stress disorder (PTSD) as well as depression, headache and anxiety.Type: GrantFiled: June 21, 2001Date of Patent: December 17, 2002Assignee: Neurogen CorporationInventors: Jun Yuan, Alan Hutchison
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Patent number: 6491989Abstract: Fluorinated naphthalene derivatives of the formula (I) R1(—A1—M1)a(—A2—M2)b—B—(—M3—A3)c—(M4—A4)d—R2 (I) where B is having the meaning and R1(—A1—M1)a(—A2—M2) and (—M3—A3)(M4—A4)R2 are mesogenic radicals, are suitable as components of liquid-crystal mixtures, in particular ferroelectric liquid-crystal mixtures.Type: GrantFiled: July 10, 2000Date of Patent: December 10, 2002Assignee: Aventis Reseach & Technologies GmbH & Co. KGInventors: Javier Manero, Wolfgang Schmidt, Barbara Hornung
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Patent number: 6492356Abstract: The present invention relates to acylguanidine derivatives of formula (I) in which R1, R2, R4, R5, R6, A, m and n have the meanings indicated in the patent claims, their physiologically tolerable salts and their prodrugs. The compounds of formula (I) are valuable pharmaceutical active ingredients. They are vitronectin receptor antagonists and inhibitors of bone resorption by osteoclasts and are suitable, for example, for the therapy or prophylaxis of diseases which are caused at least partially by an undesired extend of bone resorption, for example of osteoporosis. The invention furthermore relates to processes for the preparation of compounds of formula (I), their use, in particular as pharmaceutical active ingredients, and pharmaceutical preparations comprising them.Type: GrantFiled: November 2, 2000Date of Patent: December 10, 2002Assignees: Aventis Pharma Deutschland GmbH, Genentech, Inc.Inventors: Anuschirwan Peyman, Jochen Knolle, Gerhard Breipohl, Karl-Heinz Scheunemann, Denis Carniato, Jean-Francois Gourvest, Thomas Gadek, Robert McDowell, Sarah Catherine Bodary, Robert Andrew Cuthbertson, Napoleane Ferrara
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Patent number: 6492363Abstract: Phenylamino benzoic acid, benzamides, and benzyl alcohol derivatives of the formula where R1, R2, R3, R4, R5, and R6 are hydrogen or substituent groups such as alkyl, and where R7 is hydrogen or an organic radical, and Z is COOR7, tetrazolyl, CONR6R7, or CH2OR7, are potent inhibitors of MEK and, as such, are effective in treating cancer and other proliferative diseases such as inflammation, psoriasis and restenosis, as well as stroke, heart failure, and immunodeficiency disorders.Type: GrantFiled: August 16, 2001Date of Patent: December 10, 2002Assignee: Warner-Lambert CompanyInventors: Stephen Douglas Barrett, Alexander James Bridges, Donna Reynolds Cody, Annette Marian Doherty, David Thomas Dudley, Alan Robert Saltiel, Mel Conrad Schroeder, Haile Tecle
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Patent number: 6485797Abstract: A ferroelectric liquid crystal mixture, especially useful for operation in the &tgr;Vmin−mode, comprises a 5-Arylindane derivative of the formula (I), wherein Y is CH, CF or N and R1(—A1—M1)a(—A2—M2)b—, (M3—A3—)cR2 are mesogenic groups.Type: GrantFiled: August 31, 2000Date of Patent: November 26, 2002Assignee: Aventis Research & Technologies GmbH & Co. KGInventors: Wolfgang Schmidt, Javier Manero, Barbara Hornung, Rainer Wingen, Ayako Ogawa
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Patent number: 6485799Abstract: A aniline derivative represented by general formula (1) wherein R and R′ represent independently each other alkyl with 1 to 10 carbon, alkoxyalkyl with 1 to 10 carbon, or hydrogen; x represents cyano, halogen, haloalkyl, haloalkyloxy, or 2-cyanoethynyl; Y represents fluorine or hydrogen; na and nc represent independently each other 0 or 1; Za, Zb, and Zc represent independently each other a single bond, 1,2-ethylene, carbonyloxy, or oxymethylene; ring A1 represents 1,4-phenylene in which hydrogen may be substituted by fluorine; ring A2 and ring A3 represent independently each other 1,4-cyclohexylene, 1,4-phenylene in which hydrogen may be substituted by fluorine, or 1,3-pyrimidine-2,5-diyl.Type: GrantFiled: July 24, 2000Date of Patent: November 26, 2002Assignee: Chisso CorporationInventors: Atsuko Fujita, Norio Tamura, Hiroyuki Tekeuchi, Fusayuki Takeshita, Nobumasa Nakamura, Etsuo Nakagawa
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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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Patent number: 6479550Abstract: &agr;-Sulfenimino acid derivatives of formula I including the optical isomers thereof and mixtures of such isomers, wherein A is cycloalkyl, cycloalkenyl, aryl or heteroaryl, each optionally substituted, B is a direct bond or optionally substituted alkylene, E is hydrogen or optionally substituted aryl, R is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkylalkyl, aryl or arylalkyl, each optionally substituted, and T is NH or oxygen, have been found to be useful for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi. The invention relates the novel compounds and also to the preparation thereof and to the use of the compounds for plant protection, and to compositions suitable for applying the novel compounds in agricultural techniques.Type: GrantFiled: July 16, 2001Date of Patent: November 12, 2002Assignee: Syngenta Crop Protection, Inc.Inventors: André Jeanguenat, Martin Zeller, Hugo Ziegler
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Patent number: 6479514Abstract: Compounds of formula (I) in which the substituents and symbols have the meanings indicated in the description, are suitable for the control of Helicobacter bacteria.Type: GrantFiled: November 17, 2000Date of Patent: November 12, 2002Assignee: Altana Pharma AGInventors: Peter Zimmerman, Gerhard Grundler
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Patent number: 6472403Abstract: The present invention relates to novel imidazolidinone derivatives thereof, their synthesis, and their use as &agr;v integrin receptor antagonists. More particularly, the compounds of the present invention are antagonists of the integrin receptors &agr;v&bgr;3 and/or &agr;v&bgr;5 and are useful for inhibiting bone resorption, treating and preventing osteoporosis, and inhibiting vascular restenosis, diabetic retinopathy, macular degeneration, angiogenesis, atherosclerosis, inflammation, inflammatory arthritis, viral disease, cancer, and metastatic tumor growth.Type: GrantFiled: January 19, 2001Date of Patent: October 29, 2002Assignee: Merck & Co., Inc.Inventors: Mark E. Duggan, Wasyl Halczenko, John H. Hutchinson, Aiwen Li, Robert S. Meissner, James J. Perkins, Thomas G. Steele, Jiabing Wang, Michael A. Patane
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Patent number: 6469029Abstract: The present invention is directed to non-peptidic factor Xa inhibitors which are useful for the treatment of arterial and venous thrombotic occlusive disorders, inflammation, cancer, and neurodegenerative diseases. The factor Xa inhibitors provide compounds having Formula I: or pharmaceutically acceptable salts thereof; wherein Q is phenyl, benzyl, pyridyl, thienyl, indolyl, quinolinyl, benzothienyl, biphenylyl, or imidazolyl; any of which can include one or more optional substituents independently selected from halo, trifluoromethyl, hydroxy, amino, nitro, cyano, C1-3 alkoxy, C1-3 alkyl, methylenedioxy, carboxamido, acetamido, or amidino; X is methylene, carbonyl, or sulfonyl; Z is methylene, ethylene, or propylene; M is methylene or ethylene; and R1 R2 and R3 are independently hydrogen or C1-3 alkyl.Type: GrantFiled: September 13, 2000Date of Patent: October 22, 2002Assignee: 3-Dimensional Pharmaceuticals, Inc.Inventors: Scott C. Miller, Juan José Marugán Sánchez, Kristin D. Haslow, Jonathan Hall
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Patent number: 6465471Abstract: Compounds of formula (1) are described: in which Het is a heteroaromatic group, Alk1 is an optionally substituted aliphatic or heteroaliphatic chain and R is a carboxylic acid or a derivative thereof. The compounds are able to inhibit the binding of &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: July 1, 1999Date of Patent: October 15, 2002Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, John Clifford Head, John Robert Porter, Sarah Catherine Archibald
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Patent number: 6462047Abstract: Compounds of general structural formula (I) wherein A represents a 5- or 6-membered heteroaryl group containing at least one heteroatom selected from the group consisting of oxygen, nitrogen, and sulfur, and use of the compounds, and salts and solvates thereof, as therapeutic agents, are disclosed.Type: GrantFiled: May 16, 2001Date of Patent: October 8, 2002Assignee: ICOS CorporationInventors: Agnes Bombrun, Françoise Gellibert
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Publication number: 20020143023Abstract: Dihydropyrimidine derivatives of the following formula or analogs thereof have selective N-type calcium channel antagonistic activity, and they are used as therapeutic agents for various diseases participating in the N-type calcium channels.Type: ApplicationFiled: December 26, 2001Publication date: October 3, 2002Applicant: AJINOMOTO CO. INCInventors: Seiji Ohno, Akiko Okajima, Seiji Niwa, Morikazu Kito, Akira Takahara, Yukitsugu Ono, Yuki Kajigaya, Tomoko Takeda, Hajime Koganei
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Patent number: 6458787Abstract: Novel pyrrolidine compounds that are potent and selective inhibitors of PDE4, as well as methods of making the same, are disclosed. Use of the compounds in the treatment of inflammatory diseases and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: May 2, 2001Date of Patent: October 1, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Edward A. Kesicki, Amy Oliver, Laurence E. Burgess, John J. Gaudino, Zachary S. Jones, Bradley J. Newhouse, Stephen T. Schlacter
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Patent number: 6458803Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-phenyl-N-heteroaralkyl aminoalcohols.Type: GrantFiled: November 23, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6458794Abstract: Compounds useful as potassium channel inhibitors and especially useful for the treatment of cardiac arrhythmias and cell proliferative disorders are described.Type: GrantFiled: December 21, 2000Date of Patent: October 1, 2002Assignee: Icagen, Inc.Inventors: Michael Gross, Serge Beaudoin, Aimee D. Reed
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Patent number: 6458433Abstract: Disclosed are liquid crystalline compounds which (i) are characterized in that the compounds have a wide temperature range in which the compounds exhibit a liquid crystal phase, are low in viscosity, and have a negative and large &Dgr;&egr;, (ii) are readily mixed with other various liquid crystal materials even at low temperatures, and (iii) are useful as component of liquid crystal compositions suitable both for TFT type display mode and IPS mode; and liquid crystal composition comprising the liquid crystalline compound; the compounds are expressed by the general formula (1) wherein R1 represents an alkyl group having 1 to 15 carbon atoms; ring A1, ring A2, and ring A3 independently represent trans-1,4-cyclohexylene group, trans-1,4-silacyclohexylene group, pyrimidine-2,5-diyl group, pyridine-2,5-diyl group, 1,3-dioxane-2,5-diyl group, tetrahydropyran-2,5-diyl group, 1,3-dithian-2,5-diyl group, or tetrahydrothiopyran-2,5-diyl group, or 1,4-phenylene group in which one or more hydrogen atomType: GrantFiled: June 16, 1999Date of Patent: October 1, 2002Assignee: Chisso CorporationInventors: Takashi Kato, Shuichi Matsui, Kazutoshi Miyazawa, Fusayuki Takeshita, Etsuo Nakagawa
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Patent number: 6455539Abstract: Squaric acid derivatives of formula (1) are described: wherein R1 is a group Ar1Ar2Alk- in which Ar1 is an optionally substituted aromatic or heteroaromatic group; Ar2 is an optionally substituted phenylene or nitrogen-containing six-membered heteroarylene group; and Alk is a chain —CH2—CH(R)—, —CH═C(R)—, in which R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; R2 is a hydrogen atom or a C1-6 alkyl group; L1 is a covalent bond or a linker atom or group; n is zero or the integer 1; Alk1 is an optionally substituted aliphatic chain; R3 is a hydrogen atom or an optionally substituted heteroaliphatic, cycloaliphatic, heterocycloaliphatic, polycycloaliphatic, heteropolycycloaliphatic, aromatic or heteroaromatic group: and the salts, solvates, hydrates and N-oxides thereof.Type: GrantFiled: December 21, 2000Date of Patent: September 24, 2002Assignee: Celltech R&D LimitedInventors: Barry John Langham, Rikki Peter Alexander, John Clifford Head, Janeen Marsha Linsley, John Robert Porter, Sarah Catherine Archibald, Graham John Warrellow
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Publication number: 20020132810Abstract: A compound of the formula 1Type: ApplicationFiled: January 31, 2001Publication date: September 19, 2002Inventors: Matthew F. Brown, Christopher S. Poss
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Patent number: 6451824Abstract: Compounds of formula (I) are suitable for the production of pharmaceuticals for the prophylaxis and therapy of disorders in the course of which an increased activity of matrix-degrading metalloproteinases is involved.Type: GrantFiled: May 8, 1998Date of Patent: September 17, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Werner Thorwart, Wilfried Schwab, Manfred Schudok, Burkhard Haase
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Patent number: 6451830Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted non-fused heterocyclo amines.Type: GrantFiled: November 14, 2001Date of Patent: September 17, 2002Assignee: G.D. Searle & Co.Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel