Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/366.1)
  • Patent number: 6482955
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Grant
    Filed: August 6, 2001
    Date of Patent: November 19, 2002
    Assignee: Pharmacia Corporation
    Inventors: Matthew J. Graneto, Susan J. Hartmann, Suzanne Metz, John J. Talley, Michael L. Vazquez, David Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
  • Patent number: 6472538
    Abstract: A process for preparing compounds of the formula I in which R1 is hydrogen, an aliphatic group having 1-8 carbon atoms, C1-C6-alkoxycarbonyl, C1-C6-alkylthiocarbonyl or a cyclic ring system having 3-14 ring atoms, and R2 is hydrogen, an aliphatic group having 1-8 carbon atoms, or R1 and R2 together with the carbon atom to which they are bound form a cyclic or bicyclic ring system having 3-14 ring atoms, comprises the preparation of compounds of the formula II  in which R3 and R4 are readily detachable groups and R1 and R2 are as defined above, as starting materials or intermediates and the cyclization of these under suitable reaction conditions to give compounds of the formula I.
    Type: Grant
    Filed: April 25, 2001
    Date of Patent: October 29, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Norbert Götz, Roland Götz, Michael Rack
  • Publication number: 20020156115
    Abstract: The present invention provides an insecticidal or acaricidal composition having an excellent pesticidal effect and a high safety, containing, as an active ingredient, a pyrazolyl compound of the following general formula (I): 1
    Type: Application
    Filed: March 25, 2002
    Publication date: October 24, 2002
    Applicant: AGRO-KANESHO CO., LTD.
    Inventors: Masatsugu Oda, Manabu Katsurada, Yasushi Shiga, Toshiki Fukuchi, Taku Kato
  • Patent number: 6462199
    Abstract: There is disclosed a silver halide color photographic light-sensitive material that is improved in such aspects as fastness of dye images, color reproduction, cyan stain, processing cyan color contamination, and the like, by the combination use of a phenidone compound having a specific structure as in the following general formula (VIII) and a pyrrolotriazole cyan coupler. The phenidone compound (VIII) can be produced industrially in low cost, by reacting an &agr;-alkyl or alkenyl acrylate with a compound represented by the following general formula (VII): wherein, R4, R5, R6, R7, R8, and R9, each represent a hydrogen atom, an alkyl group, or the like; R2a represents an alkyl group having 6 to 30 carbon atoms, or the like.
    Type: Grant
    Filed: November 21, 2000
    Date of Patent: October 8, 2002
    Assignee: Fuji Photo Film Co., Ltd.
    Inventors: Hisashi Mikoshiba, Yasuhiro Yoshioka, Shin Soejima, Osamu Takahashi, Naoki Saito, Masakazu Morigaki
  • Patent number: 6455525
    Abstract: The present invention is directed to novel heterocyclic substituted pyrazolones, including pharmaceutical compositions, diagnostic kits, assay standards or reagents containing the same, and methods of using the same as therapeutics. The invention is also directed to intermediates and processes for making these novel compounds.
    Type: Grant
    Filed: October 31, 2000
    Date of Patent: September 24, 2002
    Assignee: Cephalon, Inc.
    Inventors: Jasbir Singh, Rabindranath Tripathy
  • Publication number: 20020133025
    Abstract: Benzamidoxime derivatives of the formula I 1
    Type: Application
    Filed: March 11, 2002
    Publication date: September 19, 2002
    Inventors: Karl Eicken, Joachim Rheinheimer, Frank Wetterich, Eberhard Ammermann, Gisela Lorenz, Siegfried Strathmann
  • Patent number: 6451734
    Abstract: The present invention relates to novel substituted 3-benzylpyrazoles of the formula I
    Type: Grant
    Filed: May 3, 1999
    Date of Patent: September 17, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Cyrill Zagar, Gerhard Hamprecht, Markus Menges, Olaf Menke, Peter Schäfer, Karl-Otto Westphalen, Ulf Misslitz, Helmut Walter, Robert Reinhard, Robert Brian Jones
  • Patent number: 6451790
    Abstract: Compounds of formula I wherein W is optionally substituted alkylene; Y is N or CRa; Ra is hydrogen, halogen or alkyl; R1n represents hydrogen or 1 to 4 substituents; R2 is hydrogen, nitro, cyano, halogen, alkyl, haloalkyl, alkoxy, alkylthio or alkoxycarbonyl; R3 is optionally substituted alkyl, cycloalkyl, aryl or hetaryl; A is N—OR4, CH—OR4, CH—SR4 or CHR5; R4 is alkyl or haloalkyl; R5 is halogen, alkyl or haloalkyl; methods and intermediates for their preparation. The compounds and compositions comprising them are useful for combating animal pests and harmful fungi.
    Type: Grant
    Filed: July 11, 2001
    Date of Patent: September 17, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Markus Gewehr, Hubert Sauter, Bernd Müller, Wassilios Grammenos, Andreas Gypser, Arne Ptock, Oliver Cullmann, Jordi Tormo i Blasco, Eberhard Ammermann, Siegfried Strathmann, Gisela Lorenz, Volker Harries, Roland Götz, Thomas Grote
  • Patent number: 6448263
    Abstract: This invention is directed to methods of treating insulin resistance in a mammal which comprise administering an effective amount of a compound of formula I, where the variables are defined in the specification, or the stereoisomeric mixtures, diastereomerically enriched, diastereomerically pure, enantiomerically enriched or enantiomerically pure isomers, or the pharmaceutically acceptable salts and prodrugs thereof to said mammal. The compounds of formula I are growth hormone secretagogues and as such are useful for increasing the level of endogenous growth hormone. In another aspect this invention provides certain intermediates which are useful in the synthesis of the foregoing compounds and certain processes useful for the synthesis of said intermediates and the compounds of formula I.
    Type: Grant
    Filed: August 26, 1999
    Date of Patent: September 10, 2002
    Assignee: Pfizer Inc.
    Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski
  • Publication number: 20020115868
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Application
    Filed: August 6, 2001
    Publication date: August 22, 2002
    Inventors: Matthew J. Graneto, Susan J. Hartmann, Suzanne Metz, John J. Talley, Michael L. Vazquez, David Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
  • Publication number: 20020111374
    Abstract: Estrogen receptor-modulating pyrazole compounds are described in addition to methods and compositions for treating or preventing estrogen receptor-mediated disorders. The compounds described have been found to have unexpected and surprising activity in modulating estrogen receptor activity. Thus, the compounds of the present invention have utility in preventing or treating estrogen receptor-mediated disorders such as osteoporosis, breast and endometrial cancers, atherosclerosis, and Alzheimer's disease.
    Type: Application
    Filed: September 18, 2001
    Publication date: August 15, 2002
    Applicant: Chiron Corporation
    Inventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Beata Krywult, Rajinder Singh, Liang Wang
  • Patent number: 6432881
    Abstract: 2-Benzoylcyclohexane-1,3-diones of formula I : where: R1 and R2 are each hydrogen, mercapto, nitro, halogen, cyano, thiocyanato, alkyl, haloalkyl, alkoxy, alkenyl, alkynyl, —OR3, —OCOR3, —OSO2R3, —S(O)nR3 (n=0, 1, 2), —SO2OR3, —SO2N(R3)2, —NR3SO2R3 or —NR3COR3; R3 is hydrogen or optionally substituted alkyl, haloalkyl, alkenyl, alkynyl, phenyl or phenylalkyl; Q is optionally substituted cyclohexane-2-yl-1,3-dione; X1 is optionally substituted alkylene, propenylene, alkenylene or alkynylene; R4 is hydrogen or optionally substituted alkyl, alkenyl, alkynyl, phenyl, phenylalkyl; Het is a three- to six-membered, optionally substituted heterocyclic or heteroaromatic group; and agriculturally useful salts thereof, processes and intermediates for preparing compounds of formula I, compositions comprising them, and the use of the compounds of formula I and the compositions comprising them for controlling harmful plants are described.
    Type: Grant
    Filed: February 7, 2000
    Date of Patent: August 13, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Stefan Engel, Joachim Rheinheimer, Ernst Baumann, Wolfgang von Deyn, Regina Luise Hill, Guido Mayer, Ulf Misslitz, Oliver Wagner, Matthias Witschel, Martina Otten, Helmut Walter, Karl-Otto Westphalen
  • Patent number: 6407259
    Abstract: A “one-pot” process is described herein for the production of pyrazole compounds of general formula (II) comprising the steps of reacting a compound of general formula (III) with an acylating agent in the presence of a base and an optional activating agent followed by the addition of a hydrazine compound in situ.
    Type: Grant
    Filed: July 6, 2001
    Date of Patent: June 18, 2002
    Assignee: Pfizer Inc.
    Inventors: Laurence James Harris, Philip Charles Levett
  • Publication number: 20020065289
    Abstract: Amino pyrazole derivatives of the formula: 1
    Type: Application
    Filed: February 22, 2001
    Publication date: May 30, 2002
    Inventors: Cheryl P. Kordik, Scott L. Dax, Chi Luo, Allen B. Reitz, James J. McNally, Timothy W. Lovenberg
  • Publication number: 20020058681
    Abstract: The present invention relates to compounds of the formula 1
    Type: Application
    Filed: March 2, 2001
    Publication date: May 16, 2002
    Inventors: Hengmiao Cheng, Subas Man Sakya, Jason Kenneth Dutra
  • Patent number: 6365552
    Abstract: Substituted 3-phenylpyrazoles of the formula I Salts thereof and use as herbicides.
    Type: Grant
    Filed: February 19, 1999
    Date of Patent: April 2, 2002
    Assignee: BASF Aktiengesellschaft
    Inventors: Christoph-Sweder von dem Bussche-Hünnefeld, Ralf Klintz, Gerhard Hamprecht, Elisabeth Heistracher, Peter Schäfer, Peter Münster, Klaus Ditrich, Hartmann König, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
  • Publication number: 20020028814
    Abstract: The present invention relates to N-substituted cyclic aza compounds, pharmaceutical compositions comprising such compounds, and methods of their use for effecting neuronal activities.
    Type: Application
    Filed: April 17, 2001
    Publication date: March 7, 2002
    Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
  • Patent number: 6342608
    Abstract: This invention relates to a novel process of preparing selected 5-substituted pyrazoles useful as p38 kinase and COX-2 inhibitors.
    Type: Grant
    Filed: January 30, 2001
    Date of Patent: January 29, 2002
    Assignee: G.D. Searle & Company
    Inventors: Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiaodong Xu
  • Publication number: 20020006947
    Abstract: This invention relates to compounds having the Formula I: 1
    Type: Application
    Filed: March 22, 2001
    Publication date: January 17, 2002
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
  • Publication number: 20020006943
    Abstract: Compounds of the formula: 1
    Type: Application
    Filed: April 12, 2001
    Publication date: January 17, 2002
    Inventors: Theodore O. Johnson , Jr., Ye Hua, Hiep T. Luu, Peter S. Dragovich
  • Patent number: 6329530
    Abstract: The invention relates to a method for the production of 1-substituted 5-hydroxypyrazoles of formula (I) wherein R1 is C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkinyl, C3-C6-cycloalkyl or C1-C4-alkoxy, whereby these groups can be substituted by halogen, C1-C4-alkoxy, phenoxy, C1-C6-alkoxycarbonyl, C1-C6-alkylthiocarbonyl or a cyclic ring system with 3-14 ring atoms, by reacting a) an alkylvinylether of general formula (III) wherein R2 is C1-C6-alkyl or C3-C6-cycloalkyl, with phosgene (IVa), “diphosgene” (IVb) or “triphosgene” (IVc) to form acid chlorides of formula (V), b) transforming said acid chlorides by eliminating hydrogen chloride into the corresponding 3-alkoxyacrylic acid chloride of formula (VI) and c) reacting said acid chloride with hydrazines of formula (VII) wherein R1 has the above cited meaning, to form 5-hydroxypyrazoles of formula (I).
    Type: Grant
    Filed: May 3, 2001
    Date of Patent: December 11, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: Volker Maywald, Adrian Steinmetz, Michael Rack, Norbert Götz, Roland Götz, Jochem Henkelmann, Heike Becker, Juan Jose Aiscar Bayeto
  • Publication number: 20010044445
    Abstract: Compounds having the formula 1
    Type: Application
    Filed: April 8, 1999
    Publication date: November 22, 2001
    Inventors: NWE Y. BAMAUNG, ANWER BASHA, STEVAN W. DJURIC, EARL J. GUBBINS, JAY R. LULY, NOAH P. TU, DAVID J. MADAR, USHA WARRIOR, PAUL E. WIEDEMAN, XUN ZHOU, RICHARD J. SCIOTTI, FRANK L. WAGENAAR
  • Patent number: 6312478
    Abstract: The method for temporarily coloring and later decolorizing hair includes applying a colorant to the hair, which contains a monomethine or polymethine dye of formula (Ia/Ib), or a salt thereof, W=L−V′(Ia)&rlarr2;W′−L=V (Ib), wherein W=L−V′ and W′=L−V are tautomers, W and V are each a substituted five-member or six-member heterocyclic ring, each of which is a substituted pyrazolone, substituted pyridone, substituted dioxothiazoline, substituted rhodanine, substituted dioxoimidazolidine or substituted barbituric acid; wherein L represents —[—CH═CH—]m—CR═[═CH—CH═]n═ and R is hydrogen, a phenyl group, a halogen atom, a methyl group or a carboxamido group, and wherein m and n are each 0, 1 or 2, but n+m≦2; then allowing the colorant to act for from 10 to 45 min at 20 to 50° C.
    Type: Grant
    Filed: October 26, 1999
    Date of Patent: November 6, 2001
    Assignee: Wella Aktiengesellschaft
    Inventors: Otto Goettel, Aline Pirrello
  • Patent number: 6310206
    Abstract: The invention relates to a process for preparing N-(5-amino-2-cyano-4-fluoro-phenyl)-sulphonamides in which, in a first step, 2-amino-4,5-difluoro-benzonitrile is reacted with sulphonyl halides in the presence of an acid acceptor and in the presence of a diluent at temperatures between 0° C. and 150° C. and, in a second step, the N-(2-cyano-4,5-difluoro-phenyl)-sulphon-amides and/or N-(2-cyano-4,5-difluoro-phenyl)-sulphonamides obtained in the first step are as pure substances or as mixtures with ammonia in the presence of a diluent reacted at a temperature between 100° C. and 200° C. The invention furthermore relates to novel intermediates of the process.
    Type: Grant
    Filed: January 18, 2000
    Date of Patent: October 30, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Achim Hupperts, Mark Wilhelm Drewes, David Erdman, Reinhard Lantzsch
  • Patent number: 6271391
    Abstract: Hydrazide fixed to a resin represented by the following formula: P—Q—CO—NH—NH2  (I) where P represents a main chain of a resin polymer and Q represents a hydrocarbon side chain optionally having a substituent which may be bonded via a heteroatom, and a hydrazone derived therefrom and fixed to a resin P—Q—CO—NH—N═CH—R1  (II) are provided, and solid phase synthesis of pyrazolone is conducted using the same, thereby enabling synthesis of pyrazolones by the application of the Mannich type reaction based on the solid phase synthesis and efficient construction of libraries for various kinds of them.
    Type: Grant
    Filed: November 8, 2000
    Date of Patent: August 7, 2001
    Assignee: Japan Science and Technology Corporation
    Inventors: Shu Kobayashi, Hidekazu Oyamada
  • Patent number: 6271179
    Abstract: Benzylidenepyrazolones of the formula I, Useful as herbicides.
    Type: Grant
    Filed: May 11, 2000
    Date of Patent: August 7, 2001
    Assignee: BASF Aktiengesellschaft
    Inventors: 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
  • Patent number: 6172225
    Abstract: The invention relates to a novel process for producing thereof hydroxyarenes of the general formula (I) in which n represents the numbers 1, 2, 3 or 4, R represents cyano, carboxyl, formyl, nitro, halogen or represents alkyl, alkoxy, alkylthio, alkylsulphinyl, alkylsulphonyl, alkylcarbonyl or alkoxycarbonyl, each of which is optionally substituted, and Z represents hydrogen, cyano, nitro, halogen, alkyl, halogenoalkyl, or represents monocyclic or bicyclic, saturated or unsaturated heterocyclyl, heterocyclylamino or heterocyclylimino, each of which is optionally substituted, characterized in that halogenoarenes of the general formula (II) in which n, R and Z are each as defined above and X represents halogen are reacted with 3-hydroxy-propionitrile of the formula (III), HO—CH2CH2—CN  (III), if appropriate in the presence of a reaction auxiliary and if appropriate in the presence of a diluent, at temperatures between 0° C. and 100° C.
    Type: Grant
    Filed: November 12, 1998
    Date of Patent: January 9, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Karl-Heinz Linker, Wilhelm Haas, Otto Schallner, Kurt Findeisen, Roland Andree, Mark Wilhelm Drewes