Chalcogen Attached Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/335)
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Patent number: 6451843Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols, their preparation and the use of such ketoenols as pesticides and/or herbicides. The novel arylphenyl-substituted cyclic ketoenols are of the formula (I) in which CKE refers to the cyclic ketoenol and W, X, Y and Z are as defined in the specification.Type: GrantFiled: January 2, 2001Date of Patent: September 17, 2002Assignee: Bayer AktiengesellschaftInventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretschneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Dieter Feucht, Rolf Pontzen, Randy Allen Myers
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Patent number: 6444817Abstract: Compounds of the formula where A, B, D, R1 and R2 have the meanings stated in the description, are described. The compounds are suitable for controlling diseases. The novel compounds are prepared via compounds of the formula H2N—CH2—G—M.Type: GrantFiled: October 8, 1999Date of Patent: September 3, 2002Assignee: Abbott LaboratoriesInventors: Hans-Joachim Böhm, Hans Wolfgang Höffken, Wilfried Hornberger, Stefan Koser, Helmut Mack, Thomas Pfeiffer, Werner Seitz, Thomas Zierke
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Patent number: 6444679Abstract: The present invention relates to compounds of the formula I, wherein Z1, X, Y, ( )n, R1, R2 and R3 are defined as in the specification, pharmaceutical compositions containing such compounds; and the use of such compounds to treat neurological and gastrointestinal disorders.Type: GrantFiled: February 14, 2000Date of Patent: September 3, 2002Assignee: Pfizer IncInventors: Spiros Liras, Stanton F. McHardy
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Patent number: 6444279Abstract: Acetylene derivatives of the formula I in which R, A1, A2, Z1, Z2, Z3, L1, L2, L3, Y, m and n are as defined herein are suitable as components of liquid-crystalline media.Type: GrantFiled: January 24, 2000Date of Patent: September 3, 2002Assignee: Merck Patent GmbHInventors: Volker Reiffenrath, Harald Hirschmann
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Patent number: 6436925Abstract: Benzamides of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: R1—C1-C6-alkyl, branched or unbranched, where one of the C atoms in this chain may be substituted by a phenyl ring, cyclohexyl ring, indolyl ring and an SCH3 group, and the phenyl ring in turn is substituted by by [sic] a maximum of two R4 radicals, where R4 [lacuna] hydrogen, C1-C4-alkyl, branched or unbranched, —O—C1-C4-alkyl, OH, Cl, F, Br, I, CF3, NO2, NH2, CN, COOH, COO—C1-C4-alkyl, NHCO—C1-C4-alkyl, and R2 can be NR5CO—R6 and NHR5SO2—R6, and R3 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl, CN, COOH, CONH2, COO—C1-C4-alkyl, SO2—C1-C4-alkyl, —SO2Ph, SO2NH—C1-C4-alkyl, iodine, SO2NH2 and NH2, and A can be aromType: GrantFiled: October 3, 2000Date of Patent: August 20, 2002Assignee: Abbott LaboratoriesInventors: Wilfried Lubisch, Achim Möller, Hans-Jörg Treiber, Monika Knopp
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Patent number: 6432963Abstract: Pyrimidine-5-carboxamide derivatives represented by a general formula (I) or salts thereof [wherein each symbol has the following meaning; X: O, S, NR1, CO, NR1CO, CONR1, C═N—OR1 or a bond, Y: a lower alkylene group which may be substituted by OR1 or —NHR1, or a bond, Z: O, NR2 or a bond, A: H, or a lower alkyl which may have a substituent, a —CO-lower alkyl which may have a substituent, an aryl which may have a substituent, a heteroaryl which may have a substituent, a cycloalkyl which may have a substituent or a nitrogen-containing saturated heterocyclic group which may have a substituent, B: an aryl which may have a substituent or a heteroaryl group which may have a substituent, R1, R2: H, a lower alkyl or a —CO-lower alkyl group].Type: GrantFiled: June 15, 2000Date of Patent: August 13, 2002Assignee: Yamanouchi Pharmaceutical Co., Ltd.Inventors: Hiroyuki Hisamichi, Ryo Naito, Souichirou Kawazoe, Akira Toyoshima, Kazuhito Tanabe, Eiichi Nakai, Atsushi Ichikawa, Akiko Orita, Makoto Takeuchi
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Patent number: 6426348Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are useful in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (I BD).Type: GrantFiled: May 23, 2001Date of Patent: July 30, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
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Patent number: 6423728Abstract: It has been discovered that compounds of the formula: and the pharmaceutically acceptable salts and esters thereof wherein X and Y are as defined below, inhibit the binding of VCAM-1 to VLA-4 and are usefull in treating inflammation associated with chronic inflammatory diseases such as rheumatoid arthritis (RA), multiple sclerosis, (MS), asthma, and inflammatory bowel disease (IBD).Type: GrantFiled: May 23, 2001Date of Patent: July 23, 2002Assignee: Hoffman-La Roche Inc.Inventors: Kenneth Gregory Hull, Achytharao Sidduri, Jefferson Wright Tilley
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Patent number: 6410728Abstract: Compounds of the formula or therapeutically acceptable salts or prodrugs thereof, are useful for treating bacterial infections, psoriasis, arthritis, and toxicity due to chemotherapy. Preparation of the compounds, compositions containing the compounds, and treatment of diseases using the compounds are disclosed.Type: GrantFiled: June 19, 2001Date of Patent: June 25, 2002Assignee: Abbott LaboratoriesInventors: Richard J. Sciotti, Stevan W. Djuric, Marina Pliushchev
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Publication number: 20020068701Abstract: This invention relates to positively charged non-natural amino acids, methods of making thereof, and utilization thereof in peptides. In one embodiment, the invention relates to non-natural amino acids that closely replicate the natural amino acids lysine and arginine.Type: ApplicationFiled: January 10, 2002Publication date: June 6, 2002Applicant: Medical University of South CarolinaInventor: Thomas A. Dix
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Publication number: 20020068826Abstract: Disclosed are novel 2-(5-halopyridyl) and 2-(5-halopyrimidinyl) magnesium halides, processes of making and their use in the efficient synthesis in their respective 5-halo-2-substituted pyridines and pyrimidines.Type: ApplicationFiled: December 6, 2001Publication date: June 6, 2002Inventors: Jinhua J. Song, Nathan K. Yee, Suresh R. Kapadia
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Patent number: 6399620Abstract: There are described cycloalkyl derivatives of the formula (I) R1—Y—A—B—D—E—F—G (I) in which R1, Y, A, B, D, E, F and G have the meaning indicated herein, their preparation and their use as medicaments. The compounds according to the invention can be used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: June 29, 2000Date of Patent: June 4, 2002Assignee: Aventis Pharma S.A.Inventors: Volkmar Wehner, Jochen Knolle, Hans Ulrich Stilz, Jean-Francois Gourvest, Denis Carniato, Thomas Richard Gadek, Robert McDowell, Robert Maurice Pitti, Sarah Catherine Bodary
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Patent number: 6399774Abstract: Compounds having Formula 1 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: GrantFiled: April 9, 2001Date of Patent: June 4, 2002Assignee: Allergen Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Dehua Huang, Roshantha A. Chandraratna
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Patent number: 6395731Abstract: The invention relates to heterocyclic derivatives of formula (I) and (Ia), or pharmaceutically-acceptable salts thereof, which possess antithrombotic and anticoagulant properties and are accordingly useful in methods of treatment of humans or animals. The invention also relates to processes for the preparation of the heterocyclic derivatives, to pharmaceutical compositions containing them and to their use in the manufacture of medicaments for use in the production of an antithrombotic or anticoagulant effect.Type: GrantFiled: December 20, 2000Date of Patent: May 28, 2002Assignee: Astrazeneca ABInventors: Nowak Thorsten, John Preston, John W Rayner, Michael J Smithers, Andrew Stocker
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Patent number: 6391880Abstract: This invention concerns heterocyclic derivatives of formula (I) which are useful in inhibiting oxido-squalene cyclase, processes for their preparation and pharmaceutical compositions containing them. The present invention is also concerned with heterocyclic derivatives capable of inhibiting cholesterol biosynthesis and hence in lowering cholesterol levels in blood plasma. The present invention also relates to methods of using such heterocyclic derivatives in diseases and medical conditions such as hypercholesterolemia and atherosclerosis.Type: GrantFiled: August 13, 1999Date of Patent: May 21, 2002Assignee: Zeneca LimitedInventors: Alan John Foubister, George Robert Brown, Nicholas John Newcombe
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Patent number: 6387892Abstract: Novel compounds having the Formulas 1 through 8, wherein the symbols have the meaning defined in the specification, and certain previously known compounds have been discovered to act as inhibitors of the cytochrome P450RAI (retinoic acid inducible) enzyme, and are used for treating diseases responsive to treatment by retinoids. The compound can also be used in co-treatment with retinoids.Type: GrantFiled: June 7, 2001Date of Patent: May 14, 2002Assignee: Allergan Sales, Inc.Inventors: Jayasree Vasudevan, Alan T. Johnson, Liming Wang, Dehua Huang, Roshantha A. Chandraratna
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Publication number: 20020055509Abstract: Disclosed are a series of phenylalanine derivatives, to compositions containing them, to processes for their preparation, and to their use in medicine.Type: ApplicationFiled: July 20, 2001Publication date: May 9, 2002Inventors: Andrei W. Konradi, Michael A. Pleiss, Eugene D. Thorsett, Susan Ashwell, Gregory S. Welmaker, Anthony Kreft, Dimitrios Sarantakis, Darren B. Dressen, Francine S. Grant, Christopher Semko, Ying-Zi Xu
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Patent number: 6380258Abstract: A sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl divalent aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 24, 1999Date of Patent: April 30, 2002Assignee: G. D. Searle, L.L.C.Inventors: Louis J. Bedell, Joseph J. McDonald, Thomas E. Barta, Daniel P. Becker, Shashidhar N. Rao, John N. Freskos, Brent V. Mischke, Daniel P. Getman, Gary A. DeCrescenzo
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Patent number: 6376489Abstract: Novel 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 disease and other diseases involving elevated levels of cytokines, as well as central nervous system (CNS) disorders, also is disclosed.Type: GrantFiled: December 7, 2000Date of Patent: April 23, 2002Assignee: ICOS CorporationInventors: Timothy J. Martins, Kerry W. Fowler, Joshua Odingo, Laurence E. Burgess, Stephen T. Schlachter
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Publication number: 20020045629Abstract: The present invention is directed to chemical compositions of substituted thioacetamides, processes for the preparation thereof and uses of the compositions in the treatment of diseases.Type: ApplicationFiled: May 15, 2001Publication date: April 18, 2002Inventors: Edward R. Bacon, Sankar Chatterjee, Derek Dunn, John P. Mallamo, Jeffry L. Vaught
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Patent number: 6372758Abstract: A sulfamato hydroxamic acid compound that, inter alia, inhibits matrix metalloprotease (mmp) activity is disclosed as are a process for preparing the same, intermediate compounds useful in those syntheses, and a treatment process that comprises administering a contemplated sulfamato hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity.Type: GrantFiled: June 19, 2001Date of Patent: April 16, 2002Assignee: G. D. Searle & CompanyInventors: Gary A DeCrescenzo, Joseph G Rico, Terri Boehm, Jeffery N Carroll, Darren J Kassab, Deborah A Mischke, Shashidhar Rao
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Patent number: 6365587Abstract: The present application describes novel substituted aryl hydroxamic acids of formula I: or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.Type: GrantFiled: May 13, 1999Date of Patent: April 2, 2002Inventors: Matthew E. Voss, Carl P. Decicco, Ruth R. Wexler
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Patent number: 6362192Abstract: Compounds of the formula I and salts thereof, in which the substituents and the index n have the following meanings: Q is —C(═CHCH3)—COOCH3, —C(═CHOCH3)—COOCH3, —C(═NOCH3)—COOCH3 or —C(═NOCH3)—CONH(CH3); R1 is hydrogen, halogen, C1-C4-alkyl, C1-C2-haloalkyl, C1-C4-alkoxy or C1-C2-haloalkoxy; R2 is halogen, C1-C4-alkyl, C1-C2-haloalkyl, C1-C4-alkoxy; n is 0, 1 or 2, where the substituents R2 may be different if n=2; R3 is phenyl, pyridyl or pyrimidyl, compositions comprising them and the use of the compounds I and the compositions for controlling harmful fungi and animal pests are described.Type: GrantFiled: July 6, 2000Date of Patent: March 26, 2002Assignee: BASF AktiengesellschaftInventors: Arne Ptock, Hubert Sauter, Reinhard Kirstgen, Wassilios Grammenos, Thomas Grote, Andreas Gypser, Herbert Bayer, Markus Gewehr, Oliver Cullmann, Bernd Müller, Roland Götz, Franz Röhl, Eberhard Ammermann, Gisela Lorenz, Volker Harries, Siegfried Strathmann
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Patent number: 6362204Abstract: Phenylalanine derivatives of formula (1) are described: wherein R is a carboxylic acid or a derivative thereof; L1 is a linker atom or group; and R5 is a group —L2(CH2)tR6 in which L2 is a —N(R7)CO— or —N(R7)CS— group. The compounds are able to inhibit the binding &agr;4 integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: May 20, 1999Date of Patent: March 26, 2002Assignee: Celltech Therapeutics, LtdInventors: John Clifford Head, Sarah Catherine Archibald, Graham John Warrellow, John Robert Porter
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Patent number: 6358980Abstract: Compounds of the formula: useful in the treatment of arthritis, tumor metastasis, tissue ulceration, abnormal wound healing, periodontal disease, bone disease, diabetes (insulin resistance) and HIV infection.Type: GrantFiled: January 27, 2000Date of Patent: March 19, 2002Assignee: American Cyanamid CompanyInventors: Jeremy I. Levin, Aranapakam M. Venkatesan, James M. Chen, Arie Zask, Vincent P. Sandanayaka, Mila T. Du, Jannie L. Baker
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Publication number: 20020032328Abstract: Heterocyclic acylsulfimides, processes for their preparation, compositions comprising them and their use as pesticidesType: ApplicationFiled: March 20, 2001Publication date: March 14, 2002Inventors: Yuriy Grigorievich Shermolovich, Pavel Petrovich Kornuta, Uwe Doller, Oswald Ort, Wolfgang Schaper, Daniela Jans, Ulrich Sanft, Maria-Theresia Thonessen, Marion Beckmann, Jutta Maria Waibel, Sergiy Pazenok
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Patent number: 6355806Abstract: Compounds of the formula wherein the symbols have the meaning described in the specification, have retinoid-like biological activity.Type: GrantFiled: September 16, 1999Date of Patent: March 12, 2002Assignee: Allergen Sales, Inc.Inventors: Alan T. Johnson, Min Teng, Vidyasagar Vuligonda, Richard L. Beard, Samuel J. Gillett, Tien T. Duong, Roshantha A. Chandraratna
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Patent number: 6350754Abstract: The present invention relates to novel 3-(cycloalkano-heteroarylidenyl)-2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which are expected to modulate the activity of protein tyrosine kinases and therefore to be useful in the prevention and treatment of protein tyrosine kinase related cellular disorders such as cancer.Type: GrantFiled: January 12, 2000Date of Patent: February 26, 2002Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Publication number: 20020015804Abstract: There can be provided a liquid crystalline compound expressed by the general formula (1): 1Type: ApplicationFiled: July 22, 1999Publication date: February 7, 2002Inventors: YASUHIRO HASEBA, SHUICHI MATSUI, KAZUTOSHI MIYAZAWA, NORIHISA HACHIYA, ETSUO NAKAGAWA
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Publication number: 20020015805Abstract: The invention relates to a fluoro-substituted alkenyl compound represented by formula (1) 1Type: ApplicationFiled: May 22, 2001Publication date: February 7, 2002Inventors: Yasuhiro Haseba, Shuichi Matsui, Hiroyuki Takeuchi, Yasuhiro Kubo, Etsuo Nakagawa
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Patent number: 6344467Abstract: The invention relates to novel N-substituted indole-3-glyoxylamides, to processes for their preparation and to their pharmaceutical use. The compounds have antiasthmatic, antiallergic and immunosuppressant/immunomodulating actions.Type: GrantFiled: September 30, 1999Date of Patent: February 5, 2002Assignee: ASTA Medica AGInventors: Guillaume Lebaut, Cécilia Menciu, Bernhard Kutscher, Peter Emig, Stefan Szelenyi, Kay Brune
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Patent number: 6342602Abstract: Compounds of the formula wherein the symbols have the meaning defined in the specification have retinoid-like biological activity.Type: GrantFiled: August 4, 2000Date of Patent: January 29, 2002Assignee: Allergan Sales, Inc.Inventors: Min Teng, Tien T. Duong, Roshantha A. Chandraratna
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Publication number: 20020009748Abstract: Mixtures of chemical compounds are provided having antibacterial and other utility. The mixtures are formed, preferably in solution phase, from the reaction of a purine or pyrimiding heterocyclic scaffold with a set of related chemical substituients, optionally through employment of a tether moiety. Libraries formed in accordance with the invention have utility per se and are articles of commerce. They can be used to screen for pesticides, drugs and other biologically active compounds.Type: ApplicationFiled: May 13, 1998Publication date: January 24, 2002Inventor: PHILLIP DAN COOK
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Patent number: 6333080Abstract: A liquid crystalline alkenyltolan derivative expressed by the general formula CtH2t−1—G—(CH2)m—A1—B1—(A2—B2)n—(A3—B3)p—A4—X wherein A1, A2, A3, and A4 independently represent a 1,4-cyclohexylene, 1,4-phenylene in which one or two hydrogen atoms may be replaced by a fluorine atom(s), dioxane-2,5-diyl, or pyrimidine-2,5-diyl group; B1, B2, and B3 independently represent a covalent bond, an 1,2-ethylene, 1,2-ethenylene, 1,2-ethynylene, oxymethylene, methylenoxy, carbonyloxy, or 1,4-butylene group provided that at least one of B1, B2, and B3 represents an 1,2-ethynylene group; G represents a covalent bond or an oxygen atom; CtH2t−1 represents an alkenyl group having t carbon atoms; n and p are each 0 or 1; and X represents an alkyl group having 1 to 10 carbon atoms.Type: GrantFiled: May 6, 1999Date of Patent: December 25, 2001Assignee: Chisso CorporationInventors: Norio Tamura, Atsuko Fujita, Shuichi Matsui, Kazutoshi Miyazawa, Norihisa Hachiya, Etsuo Nakagawa
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Patent number: 6333082Abstract: Liquid crystalline compounds useful in super twisted nematic liquid crystal displays are described and have the formula: wherein n is 1-5; m is 0-5; p is 0, 1 or 2; q is 0, 1 or 2 p+q is less than or equal to 3; A1, A2, A3 are independently chosen from 1,4-disubstituted benzene, 2,5-disubstituted pyrimidine, 1,5-disubstituted pyridine, 2,6-disubstituted naphthalene which may be laterally substituted with F, Cl, Br or CN, trans-1,4-disubstituted cyclohexane, 2,5-disubstituted dioxane, 2,5-disubstituted thiophene, 2,5-disubstituted furan, 2,5-disubstituted thiodiazole Z1 may be COO, OOC, OCH2, O; Z2, Z3 are independently chosen from a direct bond, COO, OOC, C2H4, CH2O, OCH2, C4H8, C3H6O, (E)—CH═CHC2H4, (E)—CH═CHCH2O, —C≡C—; R1 is alkyl, and may contain up to 20 carbon atoms and may be branched or a straight chain; provided that at least one of, A1, A2, A3 is selected from 1,4-disubstituted thiophene.Type: GrantFiled: June 30, 2000Date of Patent: December 25, 2001Assignee: QinetiQ LtdInventors: Warren L Duffy, John W Goodby, Stephen M Kelly
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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: 6329027Abstract: Provided are liquid crystalline compounds having excellent physical properties and being excellent in miscibility with other liquid crystal materials; liquid crystal compositions comprising the crystalline compound; and liquid crystal display device fabricated by using the liquid crystal composition; the liquid crystalline compounds being specific chlorobenzene derivatives expressed by the general formula (1) Ra—A1—Z1—A2&Parenopenst;Z2—A3&Parenclosest;m&Parenopenst;Z3—A4&Parenclosest;nRb (1) wherein Ra, Rb, A1 to A4, Z1 to Z3, m, and n are herein defined.Type: GrantFiled: May 28, 1999Date of Patent: December 11, 2001Assignee: Chisso CorporationInventors: Tomoyuki Kondo, Shuichi Matsui, Kazutoshi Miyazawa, Hiroyuki Takeuchi, Fusayuki Takeshita, Etsuo Nakagawa
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Patent number: 6329523Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.Type: GrantFiled: March 10, 1999Date of Patent: December 11, 2001Assignee: ISIS Pharmaceuticals, Inc.Inventors: Phillip Dan Cook, Haoyun An
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Patent number: 6326065Abstract: Liquid crystalline compounds having a comparatively high voltage holding ratio, high &Dgr;n and high &Dgr;&egr;, and excellent miscibility with known liquid crystalline compounds at low temperatures.Type: GrantFiled: December 1, 1998Date of Patent: December 4, 2001Assignee: Chisso CorporationInventors: Yasuhiro Haseba, Shuichi Matsui, Kazutoshi Miyazawa, Hiroyuki Takeuchi, Yoshitaka Tomi, Fusayuki Takeshita, Etsuo Nakagawa
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Patent number: 6319925Abstract: Oxime ethers of formula (I) in which a) X is an N atom and Y is an oxygen atom or NH, or b) X is CH and Y is an oxygen atom, in which furthermore R1 is C1-C4alkyl; R2 is hydrogen, C1-C4alkyl or cyclopropyl; and in which R3 and R4 are as defined herein, are fungicidal, acaricidal and insecticidal active ingredients for agriculture. They can be employed as formulated crop protection compositions.Type: GrantFiled: December 22, 1997Date of Patent: November 20, 2001Assignee: Bayer AktiengesellschaftInventor: Hugo Ziegler
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Patent number: 6319922Abstract: Propanoic acid derivatives of formula (1) are described: Ar—X1—Ar1—Z—R (1) in which Ar is a nitrogen base containing group; X1 is linker atom or group; Ar1 is an optionally substituted 5- or 6-membered nitrogen-containing aromatic or non-aromatic monocycle; Z is a group —CH(R13)CH2— [in which R13 is an optionally substituted aliphatic, cycloaliphatic, heteroaliphatic, heterocycloaliphatic, aromatic or heteroaromatic group], —C(R12a)(R13)—CH(R12b)— [in which R12a and R12b together with the carbon atoms to which they are attached form a C3-7cycloalkyl group] or C(R13)═CH—; R is a carboxylic acid (—CO2H) or a derivative or biostere thereof; and the salts, solvates, hydrates and N-oxides thereof. The compounds are able to inhibit the binding of &agr;V integrins to their ligands and are of use in the prophylaxis and treatment of immune or inflammatory disorders.Type: GrantFiled: November 23, 1999Date of Patent: November 20, 2001Assignee: Celltech Therapeutics LimitedInventors: Rikki Peter Alexander, Barry John Langham, James Thomas Reuberson, Emma Louise Trown, Graham John Warrellow
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Patent number: 6316459Abstract: O-Benzyloxime ethers of the formula I where X is substituted or unsubstituted CH2, NOalkyl Y is O, S, NR5 R1, R2, R5 are H, alkyl Z1, Z2 are H, halogen, methyl, methoxy, cyano R3, R4 are hydrogen, cyano, substituted or unsubstituted alkyl, alkenyl, cycloalkyl, cycloalkenyl, alkynyl, alkoxy, haloalkoxy, alkylthio, benzylthio, alkylcarbonyl, substituted or unsubstituted phenylcarbonyl, substituted or unsubstituted benzylcarbonyl, alkoxycarbonyl, substituted or unsubstituted phenoxycarbonyl, substituted or unsubstituted benzyloxycarbonyl, N(R6)2, where R6 is H, alkyl, substituted or unsubstituted phenyl, —CO—N(R7)2, where R7 is H, substituted or unsubstituted alkyl, substituted or unsubstituted aryl, substituted or unsubstituted aryloxy, substituted or unsubstituted arylthio, substituted or unsubstituted hetaryl, substituted or unsubstituted hetaryloxy, substituted or unsubstituted hetarylthio, substituted or unsubstituted heterocyclyl, substituted or unsubstituted heterocyType: GrantFiled: October 25, 1994Date of Patent: November 13, 2001Inventors: Siegbert Brand, Uwe Kardorff, Reinhard Kirstgen, Bernd Mueller, Klaus Oberdorf, Hubert Sauter, Gisela Lorenz, Eberhard Ammermann, Christoph Kuenast, Albrecht Harreus
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Patent number: 6316389Abstract: Compounds of the formula I in which: where: X is CH or N; Y is O; S, S═O or NR5; Z is OR2, SR2, N(R3)R4; or Y and Z together form 5- to 7-membered ring which contains, 2 or 3 hetero atoms O and/or N and which is unsubstituted or substituted by C1-C4alkyl, halo-C1-C4alkyl, halogen, ═O or cyclopropyl; V is a direct bond or C1-C6alkylene, which is unsubstituted or substituted by C1-C3alkyl, C2-C3alkylidene or C3-C6cycloalkylidene; U is O, S, NR7, SO or SO2; W is substituted or unsubstituted aryl or substituted or unsubstituted heteroaryl; R1 is cyclopropyl, C1C6alkyl or halo-C1-C6alkyl; R2 and R3 independently of one another are C1-C6alkyl or halo-C1-C6alkyl; R4 and R5 independently of one another are hydrogen, C1-C6alkyl or C1-C6alkoxy; R7 is hydrogen, C1-C6alkyl, benzyl, C1-C6alkylcarbonyl, halo-C1-C6alkylcarbonyl, halo-C2-C6alkenylcarbonyl; R21 and R22 independently of one another are hydrogen, halogen, C1-C8alkyl or C1-C8alkoxy or C1-C8alkylthio; R23, R24, R25, R26 iType: GrantFiled: June 16, 1997Date of Patent: November 13, 2001Assignee: Bayer AktiengesellschaftInventors: Henry Szczepanski, Martin Zeller, Ottmar Franz Hüter
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Patent number: 6313097Abstract: Compounds of the formula (I) wherein A, R, R1, R2, X1, X2, X3, and Y are as defined herein, and the tautomers and the pharmaceutically acceptable salts thereof, including pharmaceutical compositions containing these compounds, and their use in the selective antagonization of calcitonin gene-related peptide (CGRP) and in the treatment or prophylaxis of migraine or cluster headaches, non-insulin-dependent diabetes mellitus, inflammation, allergic rhinitis, asthma, morphine tolerance, menopausal hot flashes, and diseases characterized by excessive vasodilatation and consequent reduction in blood-flow.Type: GrantFiled: March 10, 2000Date of Patent: November 6, 2001Assignee: Boehringer Ingelheim Pharma KGInventors: Wolfgang Eberlein, Klaus Rudolf, Wolfhard Engel, Henri Doods, Gerhard Hallermayer
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Patent number: 6313339Abstract: Certain cyclopropyl oxime ethers substituted by aryl and heterocyclic moieties possess broad spectrum fungicidal and insecticidal properties. These compounds are disclosed along with compositions containing these compounds and methods for controlling fungi and insects by the use of a fungitoxic or insecticidal amount of these compounds.Type: GrantFiled: February 17, 2000Date of Patent: November 6, 2001Inventors: Ronald Ross, Jr., Duyan Vuong Nguyen, Steve Howard Shaber
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Patent number: 6313120Abstract: The invention relates to compounds of formula in which R1 to R9, R16 and R17 are as defined in Claim 1. These compounds are pharmacologically active.Type: GrantFiled: June 13, 2000Date of Patent: November 6, 2001Assignee: Sanofi-SynthelaboInventors: Bernard Ferrari, Jean Gougat, Claude Muneaux, Yvette Muneaux, Pierre Perreaut, Claudine Planchenault
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Publication number: 20010036942Abstract: This invention relates to neurotrophic low molecular weight, small molecule N-oxides of heterocyclic esters amides, thioesters, and ketones having an affinity for FKBP-type immunophilins, and their use as inhibitors of the enzyme activity associated with immunophilin proteins, particularly peptidyl-prolyl isomerase, or rotamase, enzyme activity.Type: ApplicationFiled: April 26, 2001Publication date: November 1, 2001Inventors: Gregory S. Hamilton, Joseph P. Steiner, Eric S. Burak
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Publication number: 20010037023Abstract: The small nonpeptides of the instant invention are tachykinin antagonists. The compounds are highly selective and functional NK3 antagonists expected to be useful in the treatment of pain, depression, anxiety, panic, schizophrenia, neuralgia, addiction disorders, inflammatory diseases, gastrointestinal disorders, vascular disorders, and neuropathological disorders.Type: ApplicationFiled: June 4, 2001Publication date: November 1, 2001Inventors: Michael Huai Gu Chen, Fu-Zon Chung, Helen Tsenwhei Lee
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Patent number: 6306876Abstract: 4-[aryl(8-azabicyclo[3.2.1]octan-3yl)]aminobenzoic acid derivatives are delta-opioid receptor modulators. As delta-opioid receptor agonists, such compounds are useful as analgesics. Depending on their antagonist effect, such compounds may also be useful immunosuppressants, antiinflammatory agents, agents for the treatment of neurological and psychiatric conditions, medicaments for drug and alcohol abuse, agents for treating gastritis and diarrhea, cardiovascular agents and agents for the treatment of respiratory diseases.Type: GrantFiled: December 4, 2000Date of Patent: October 23, 2001Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: John R. Carson, Robert E. Boyd, Lou Anne Neilson
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Patent number: 6303818Abstract: The present invention relates to certain oxime ether compounds, compositions containing these compounds, and methods for controlling fungi by the use of a fungitoxic amount of the compounds or compositions.Type: GrantFiled: August 8, 2000Date of Patent: October 16, 2001Assignee: Dow AgroSciences LLCInventors: Lixin Zhang, Steven Howard Shaber