Nitrogen Attached Directly To The Diazole Ring By Nonionic Bonding Patents (Class 548/367.4)
  • Publication number: 20040030140
    Abstract: A process for preparing pesticides or pesticidal intermediates, particularly 5-amino-1 aryl-3-cyanopyrazoles, having the formula 1
    Type: Application
    Filed: July 18, 2003
    Publication date: February 12, 2004
    Applicant: Aventis CropScience S.A.
    Inventor: Jean-Erick Ancel
  • Publication number: 20040024208
    Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.
    Type: Application
    Filed: March 3, 2003
    Publication date: February 5, 2004
    Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek J. Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
  • Patent number: 6686318
    Abstract: The invention relates to new substituted aromatic amino compounds of the general formula (I) in which R1, R2, R3, R4 and Z have the meanings given in the description, to a process for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 22, 2003
    Date of Patent: February 3, 2004
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andree, Mark Wilhelm Drewes, Kurt Findeisen, Joachim Kluth, Karl-Heinz Linker, Klaus-Helmut Müller, Otto Schallner, Markus Dollinger
  • Publication number: 20040019085
    Abstract: Compounds having the formula (I), 1
    Type: Application
    Filed: June 17, 2003
    Publication date: January 29, 2004
    Inventors: William A. Slusarchyk, Scott A. Bolton, Timothy Herpin, Gregory S. Bisacchi, Zulan Pi, E. Scott Priestley
  • Publication number: 20040006085
    Abstract: This invention is directed to a class of compounds (Formula I) including hydroxyalkanoyl amino pyrazoles, hydroxyalkanoyl amino thiadiazoles, hydroxyalkanoyl amino acid esters, hydroxyalkanoyl amino acid amides, hydroxyalkanoyl amino alcohols, hydroxyalkanoyl amino ketoes, hydroxyalkanoyl amino hydantoins, hydroxyalkanoyl anilines, and hydroxyalkanoyl derivatives of privileged structures. The invention is also directed to a pharmaceutical formation comprising such compound in a pharmaceutically acceptable salt form or prodrug thereof. The invention is further directed to a method for inhibiting &bgr;-amyloid peptide release and/or synthesis, a method for inhibiting &ggr;-secretase activity and a method for treating neurological disorders associated with &bgr;-amyloid peptide production. The method comprises administering to a host a pharmaceutical formulation comprising an effective amount of a compound of Formula I. The compounds of Formula I are useful in the prevention and treatment of Alzheimer's disease.
    Type: Application
    Filed: January 31, 2003
    Publication date: January 8, 2004
    Inventors: Jay S. Tung, Ashley C. Guinn, Gene Thorsett, Mike A. Pleiss
  • Patent number: 6638956
    Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) These compounds are found to be generally safe systemic insecticides for control of arthropod, nematode, helminth or protozoan pests including compositions and derivatives thereof.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: October 28, 2003
    Assignee: Rhone-Poulenc, Inc.
    Inventors: Tai-Teh Wu, Alain Chene, David Treadway Manning, Peter Wyatt Newsome, Nicholas Charles Ray, Jennifer Lantz Phillips, Patrick Doyle Lowder
  • Patent number: 6620943
    Abstract: A process for the preparation of a compound of formula (I) comprising oxidizing a compound of formula (II) with trifluoroperacetic acid in the presence of a corrosion inhibiting compound such as boric acid. Also, a process for preparing a compound of formula (II) by adding sulfur dioxide to a mixture of the corresponding disulfide, a formate salt, trifluoromethyl bromide and a polar solvent; and a process for preparing the disulfide comprising adding S2Cl2 to a solution, in an organic solvent, of the corresponding 4-unsubstituted pyrazole.
    Type: Grant
    Filed: August 15, 2002
    Date of Patent: September 16, 2003
    Assignee: Bayer Cropscience SA
    Inventors: Jean-Louis Clavel, Isabelle Pelta, Sylvie Le Bars, Philippe Charreau
  • Publication number: 20030166940
    Abstract: A process for the preparation of a compound of the formula (I): 1
    Type: Application
    Filed: April 30, 2003
    Publication date: September 4, 2003
    Inventors: Jean-Francois Rousseau, Albert Buforn
  • Publication number: 20030149051
    Abstract: The present invention provides compounds of formula I: 1
    Type: Application
    Filed: February 12, 2002
    Publication date: August 7, 2003
    Inventors: Jeremy Green, Guy Bemis, Anne-Laure Grillot, Mark Ledeboer, Francesco G. Salituro, Edmund Harrington, Huai Gao, Christopher Baker, Jingrong Cao, Michael Hale
  • Publication number: 20030144529
    Abstract: A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders.
    Type: Application
    Filed: October 9, 2002
    Publication date: July 31, 2003
    Inventors: Gunnar J. Hanson, Shuyuan Liao
  • Publication number: 20030135057
    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: October 10, 2002
    Publication date: July 17, 2003
    Inventors: Matthew J. Graneto, Michael L. Vazquez, Susan J. Hartmann, Suzanne Metz, John J. Talley, David L. Brown, Richard M. Weier, Michael A. Stealey, Xiangdong Xu
  • Publication number: 20030109687
    Abstract: Compounds of the formula
    Type: Application
    Filed: August 5, 2002
    Publication date: June 12, 2003
    Inventors: Tae K. Song, Min Teng, Roshantha A. Chandraratna
  • Patent number: 6518296
    Abstract: The invention relates to novel substituted 3-thiocarbamoylpyrazoles of general formula (I), wherein m, n, R1, R2, R3 and Ar have the meanings cited in the description. The invention further relates to methods for the production and use thereof as pesticides.
    Type: Grant
    Filed: November 28, 2000
    Date of Patent: February 11, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Alig, Albrecht Marhold, Jörn Stölting, Wolfgang Gau, Christoph Erdelen, Andreas Turberg, Norbert Mencke, Olaf Hansen
  • Publication number: 20030022929
    Abstract: Disclosed are novel compounds of the formula Ia and methods of using soluble epoxide hydrolase (sEH) inhibitors of the formulas I and Ia for diseases related to cardiovascular disease.
    Type: Application
    Filed: June 14, 2002
    Publication date: January 30, 2003
    Applicant: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Richard H. Ingraham, John R. Proudfoot
  • Publication number: 20030018058
    Abstract: The present invention describes compounds of formula I 1
    Type: Application
    Filed: August 15, 2002
    Publication date: January 23, 2003
    Inventors: Mark E. Salvati, S. David Kimball
  • Publication number: 20030013747
    Abstract: Antiatherosclerotic agents are provided which are represented by Formulas I or II: 1
    Type: Application
    Filed: August 6, 2002
    Publication date: January 16, 2003
    Applicant: Wyeth
    Inventors: Robert J. Steffan, Amedeo A. Failli
  • Patent number: 6500850
    Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) These compounds are found to be generally safe systemic insecticides for control of arthropod, nematode, helminth or protozoan pests including compositions and derivatives thereof.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: December 31, 2002
    Assignee: Rhone-Poulenc Inc.
    Inventors: Tai-Teh Wu, Alain Chene, David Treadway Manning, Peter Wyatt Newsome, Nicholas Charles Ray, Jennifer Lantz Phillips, Patrick Doyle Lowder
  • Publication number: 20020147198
    Abstract: Selected compounds are effective for prophylaxis and treatment of diseases, such as angiogenesis mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving, cancer and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
    Type: Application
    Filed: January 10, 2002
    Publication date: October 10, 2002
    Inventors: Guoqing Chen, Guolin Cai, Celia Dominguez, Julie Germain, Joseph L. Kim, Tae-Seong Kim, Leon M. Smith, Andrew Tasker, Chester Chenguang Yuan, Shon Booker, Michael Croghan, Lucian DiPietro, Daniel Elbaum, Qi Huang, Ning Xi, Shimin Xu, Vinod F. Patel
  • 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: 6432997
    Abstract: The invention relates to new 1-arylpyrazole hydroxylamines and hydrazines of the formula wherein the structural variables are as defined in the specification. The subject compounds are especially useful as pesticides, for controlling arthropods, especially insects, by systemic action.
    Type: Grant
    Filed: September 24, 1999
    Date of Patent: August 13, 2002
    Assignee: Rhone-Poulenc, Inc.
    Inventor: Tai-Teh Wu
  • Publication number: 20020103185
    Abstract: The invention provides compounds of formula 1 1
    Type: Application
    Filed: August 28, 2001
    Publication date: August 1, 2002
    Inventors: Mark A. Sanner, Chris J. Helal, Christopher B. Cooper, Travis T. Wager
  • Publication number: 20020082283
    Abstract: A method for the inhibition of high affinity glycine transporters, compounds that inhibit these transporters; pharmaceutically active compositions comprising such compounds; and the use of such compounds either as above, or in formulations for the control or prevention of disease states in which glycine is involved are disclosed.
    Type: Application
    Filed: September 13, 2001
    Publication date: June 27, 2002
    Applicant: Gliatech, Inc.
    Inventors: Syed M. Ali, Kurt R. Brunden, Jack B. Jiang
  • Publication number: 20020082289
    Abstract: A compound having the formula: 1
    Type: Application
    Filed: December 31, 2001
    Publication date: June 27, 2002
    Inventor: Scot Kevin Huber
  • 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
  • Patent number: 6403628
    Abstract: The invention relates to 1-phenylpyrazole derivatives of formula (I): wherein R1, R2, R3, R4 and X are as defined in the description, and to their use as insecticides.
    Type: Grant
    Filed: May 26, 2000
    Date of Patent: June 11, 2002
    Assignee: Rhone-Poulenc Agro
    Inventors: Jennifer Phillips, Michael Pilato, Tai-Teh Wu
  • 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
  • Publication number: 20020052395
    Abstract: A compound of general formula (I), or pharmaceutically acceptable salts, solvates or polymorphs thereof; wherein; R1 and R2, which may be the same or different, are hydrogen, C1-C6alkyl, (CH2)m(C3-C6cycloalkyl) wherein m =0, 1, 2 or 3, or R1 and R2 together with the nitrogen to which they are attached form an azetidine ring; each R3 is independently CF3, OCF3, C1-4alkylthio or C1-C4alkoxy; n is 1, 2 or 3; and R4 and R5, which may be the same or different, are: A-X, wherein A =—CH=CH— or —(CH2)p— where p is 0, 1 or 2; X is hydrogen, F, Cl, Br, I, CONR6R7,SO2NR6R7, SO2NHC(=O)R6, OH, C1-4alkoxy, NR8SO2R9, NO2, NR6R11, CN, CO2R10, CHO, SR10, S(O)R9 or SO2R10 R6, R7, R and R10 which may be the same or different, are hydrogen or C1-6alkyl optionally substituted independently by one or more R12; R9 is C1-6 alkyl optionally substituted independently by one or more R12; R11 is hydrogen, C1-6 alkyl optionally substituted independently by one or more R12, C(O)R6, CO2R9
    Type: Application
    Filed: March 16, 2001
    Publication date: May 2, 2002
    Inventors: Mark David Andrews, David Hepworth, Donald Stuart Middleton, Alan Stobie
  • Patent number: 6372774
    Abstract: N-Phenylpyrazole derivatives of the formula: wherein R1 represents optionally halogenated alkyl; R2 represents halogen, cyano, nitro, cycloalkyl, alkenyl, thiocyanato, optionally alkyl substituted sulphamoyl, optionally alkyl substituted carbamoyl, alkoxycarbonyl, alkanoyl or optionally halogenated alkyl; and R3 represents a hydrogen atom or a group N″R′″ or a variety of other groupings. These compounds possess arthropodicidal, plant nematocidal, anthelmintic and anti-protozoal properties; their preparation, compositions containing them and their use are described.
    Type: Grant
    Filed: July 16, 1999
    Date of Patent: April 16, 2002
    Assignee: Rhone-Poulenc Agriculture Ltd.
    Inventors: Leslie Roy Hatton, Ian George Buntain, David William Hawkins, Edgar William Parnell, Christopher John Pearson, David Alan Roberts
  • Patent number: 6350771
    Abstract: The invention relates to novel 1-arylpyrazole oxime derivatives, of general formula (I) or (I bis) These compounds are found to be generally safe systemic insecticides for control of arthropod, nematode, helminth or protozoan pests including compositions and derivatives thereof.
    Type: Grant
    Filed: December 12, 1997
    Date of Patent: February 26, 2002
    Assignee: Rhone-Poulenc, Inc.
    Inventors: Tai-Teh Wu, Alain Chene, David Treadway Manning, Peter Wyatt Newsome, Nicholas Charles Ray, Jennifer Lantz Phillips, Patrick Doyle Lowder
  • Patent number: 6346542
    Abstract: A composition comprising (S)-5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulfinylpyrazole and (R)-5-amino-3-cyano-1-(2,6-dichloro-4-trifluoromethylphenyl)-4-trifluoromethylsulfinylpyrazole, enantiomerically enriched in the (S)-enantiomer.
    Type: Grant
    Filed: April 14, 2000
    Date of Patent: February 12, 2002
    Assignee: Aventis CropScience S.A.
    Inventor: Scot Kevin Huber
  • Publication number: 20020016468
    Abstract: The invention relates to 1-arylpyrazole-3-thiocarboxamide derivatives of formula (I): 1
    Type: Application
    Filed: June 24, 1999
    Publication date: February 7, 2002
    Applicant: Rhone-Poulenc Agrochimie
    Inventors: DAVID TREADWAY MANNING, MICHAEL PILATO, TAI-TEH WU, DAVID WILLIAM HAWKINS
  • Patent number: 6335357
    Abstract: A 1-aryl-3-cyano-5-(het)arylalkylaminopyrazole derivative represented by the general formula (1): process of making, intermediate thereof and pesticide therewith.
    Type: Grant
    Filed: October 7, 1999
    Date of Patent: January 1, 2002
    Assignee: Mitsubishi Chemical Corporation
    Inventors: Shuko Okui, Nobuo Kyomura, Toshiki Fukuchi, Ken Tanaka
  • Patent number: 6329418
    Abstract: The invention provides compounds which are potent inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the present invention relates to compounds having a structure according to the following Formula (I): wherein R1, R2, X, Z, m, and n are defined below. to This invention also includes optical isomers, diastereomers and enantiomers of the formula above, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. The compounds of the present invention are useful for the treatment of diseases and conditions which are characterized by unwanted metalloprotease activity. Accordingly, the invention further provides pharmaceutical compositions comprising these compounds. The invention still further provides methods of treatment for metalloprotease-related maladies using these compounds or the pharmaceutical compositions containing them.
    Type: Grant
    Filed: March 23, 1999
    Date of Patent: December 11, 2001
    Assignee: The Procter & Gamble Company
    Inventors: Menyan Cheng, Michael George Natchus, Biswanath De, Neil Gregory Almstead, Yetunde Olabisi Taiwo, Stanislaw Pikul
  • Patent number: 6319941
    Abstract: This invention concerns the treatment of smooth muscle spasticity or excess muscle contraction such as urge urinary incontinence with a compound of the formula wherein: R1 and R2 are independently straight chain alkyl of 1 to 6 carbon atoms, branched alkyl of 3 to 6 carbons atoms, or cycloalkyl of 3 to 6 carbons atoms where R1 and R2 may be substituted by F, Cl, Br, I, OH, NH2, cyano, C1-C6 alkoxy, C1-C6alkylthio, COOH or COOC1-C6 alkyl; R3 is an aryl or heteroaryl as defined herein, optionally substituted with 0 to 4 groups selected independently from C1-C6 alkyl, C1-C6 alkoxy, cyano, F, Cl, Br, C1-C6 alkylthio, CO2R1, CONH2, OH, NH2, and NO2; n is 0 or 1; R4 is a straight chain alkyl group of 1 to 10 carbons atoms, a branched alkyl of 3 to 10 carbons, or a cycloalkyl of 3 to 10 carbons; and all crystalline forms and the pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: September 6, 2000
    Date of Patent: November 20, 2001
    Assignee: American Home Products Corporation
    Inventors: Adam Matthew Gilbert, Zhen-jia Chen
  • Patent number: 6265430
    Abstract: The invention relates to new 3-thiocarbarnoylpyrazole derivatives of the formula (I) in which Ar represents in each case optionally substituted phenyl or pyridyl, R1 represents H2N—CS— and R2 and R3 are as defined in the description, to a plurality of processes for their preparation and to their use as pesticides.
    Type: Grant
    Filed: May 6, 1999
    Date of Patent: July 24, 2001
    Assignee: Bayer Aktiengesellschaft
    Inventors: Bernd Alig, Achim Bertsch, Dietmar Bielefeldt, Norbert Lui, Albrecht Marhold, Christoph Erdelen, Wolfram Andersch, Andreas Turberg, Norbert Mencke
  • Publication number: 20010007876
    Abstract: The invention relates to new 3-thiocarbamoylpyrazole derivatives of the formula (I) 1
    Type: Application
    Filed: May 6, 1999
    Publication date: July 12, 2001
    Inventors: BERND ALIG, ACHIM BERTSCH, DIETMAR BIELEFELDT, NORBERT LUI, ALBRECHT MARHOLD, CHRISTOPH ERDELEN, WOLFRAM ANDERSCH, ANDREAS TURBERG, NORBERT MENCKE
  • Patent number: 6242475
    Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.
    Type: Grant
    Filed: June 29, 2000
    Date of Patent: June 5, 2001
    Assignee: Rhone-Poulenc Inc.
    Inventors: Jamin Huang, Scot Kevin Huber
  • Patent number: RE37936
    Abstract: A compound of formula (I): compositions containing them and methods of use to control pests.
    Type: Grant
    Filed: July 13, 2001
    Date of Patent: December 10, 2002
    Assignee: Aventis CropScience USA Inc.
    Inventors: Jamin Huang, Scot Kevin Huber