Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/366.1)
  • Patent number: 6858639
    Abstract: 3-Arylphenyl sulfide derivatives represented by general formula (I): ? (wherein R is a C2-C6 alkyl group, a C2-C6 alkenyl group, a C2-C6 alkynyl group or the like, B0 to B2 and B3 are hydrogen atoms, halogen atoms, cyano groups, C1-C4 haloalkyl groups or the like, n is 0, 1 or 2, and Ar is a phenyl ring, a pyridine ring, a thiophene ring, a pyrazole ring or the like), and insecticides and miticides containing the 3-arylphenyl sulfide derivatives as an active ingredient.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: February 22, 2005
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Keiji Toriyabe, Nobuo Takefuji, Minoru Itou, Tetsuya Hirade, Kiyotoshi Nishiyama, Mitsuharu Asahida, Yasunobu Maeda, Nobuhide Wada, Toyokazu Fujisawa, Hiroyuki Yano, Masaaki Komatsu, Osamu Tada
  • Publication number: 20040267014
    Abstract: Substituted aryl ether derived compounds represented by general structure (I) are described. X and Y are independent of each other and are represented by hydrogen, halogen, cyano, nitro, (C1-4)alkyl, (C1-4)haloalkyl, or (C1-4)haloalkoxy; Z is oxygen or sulfur, Q is selected form Q1 to Q6; A is oxygen, sulfur, or imino; R1 is hydrogen, (C1-4)alkyl, (C1-4)haloalkyl, or amino and can be independent of each other in a single molecule; R2 and R3 are independent of each other and may be selected from the group consisting of hydrogen, halogen, cyano nitro, (C1-4)alkyl, (C1-4)haloalkyl, (C2-4)alkenyl, (C2-6)haloalkenyl and amino which may be optionally substituted with (C1-4)alkyl or (C1-4)haloalkyl; Ar is substituted or unsubstituted carbocyclic or heterocyclic aromatic ring being at least a five or six membered ring. This ring can be fused with another substituted or unsubstituted five or six membered carbocyclic or heterocyclic ring. When Q is Q5, unsubstituted or substituted phenyl is excluded.
    Type: Application
    Filed: August 20, 2004
    Publication date: December 30, 2004
    Inventors: Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
  • Publication number: 20040192929
    Abstract: A process for the oxidation of thioethers to sulfoxides or sulfones or for the oxidation of sulfoxides to sulfones by treatment of thioethers or sulfoxides with an oxidizing amount of &egr;-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
    Type: Application
    Filed: March 17, 2004
    Publication date: September 30, 2004
    Applicant: DINAMITE DIPHARMA S.P.A. abbreviated DIPHARMA S.P.A.
    Inventors: Pietro Allegrini, Caterina Napoletano, Gabriele Razzetti, Graziano Castaldi
  • Publication number: 20040192667
    Abstract: One aspect of the invention is concerned with cannabimimetic pyrazole analogs. Another aspect of the invention is concerned with new and improved pyrazole analogs having high affinities and/or selectivities for the CB1 cannabinoid receptor. A further aspect of the invention is concerned with pharmaceutical preparations employing the inventive analogs and methods of administering therapeutically effective amounts of the inventive analogs to provide a physiological effect.
    Type: Application
    Filed: March 1, 2004
    Publication date: September 30, 2004
    Applicant: University of Connecticut
    Inventors: Alexandros Makriyannis, Qian Liu, Rajesh Thotapally
  • Publication number: 20040180891
    Abstract: This invention relates to pyrazole derivatives of 1
    Type: Application
    Filed: March 15, 2004
    Publication date: September 16, 2004
    Inventors: Uday Khire, Chengzhi Zhang, Harold C E Kluender, Ingo Mugge, Zhengqui Hong, Jianxing Shao, Neil Bifulco, Pamela A Trail, Jacques Dumas, Rico C Lavoie, Xaio-Gao Liu, Veena Agarwal, Sharad K Verma, Lei Wang
  • Publication number: 20040142820
    Abstract: The present invention relates to pyrazolylarylalkines and to their use, to a process for preparing pyrazolylarylalkines and also to intermediates.
    Type: Application
    Filed: January 5, 2004
    Publication date: July 22, 2004
    Inventors: Wolfgang Ebenbeck, Florian Rampf, Albrecht Marhold
  • Publication number: 20040127365
    Abstract: The present invention relates to novel arylphenyl-substituted cyclic ketoenols of the formula (I) 1
    Type: Application
    Filed: December 8, 2003
    Publication date: July 1, 2004
    Inventors: Folker Lieb, Reiner Fischer, Alan Graff, Udo Schneider, Thomas Bretshneider, Christoph Erdelen, Wolfram Andersch, Mark Wilhelm Drewes, Markus Dollinger, Ingo Wetcholowsky, Randy Allen Myers
  • Patent number: 6750338
    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: October 10, 2002
    Date of Patent: June 15, 2004
    Assignee: Pharmacia Corporation
    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
  • Patent number: 6750222
    Abstract: The present invention relates to compounds of the formula (I) and/or salts thereof where R1, R2, A, B, X and Y are as defined in claim 1. The compounds according to the invention are suitable for use as herbicides and plant growth regulators.
    Type: Grant
    Filed: December 13, 2002
    Date of Patent: June 15, 2004
    Assignee: Bayer CropScience GmbH
    Inventors: Hendrik Helmke, Michael Gerhard Hoffmann, Klaus Haaf, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
  • Publication number: 20040110816
    Abstract: This invention relates to pyrazole derivatives of formula (I) 1
    Type: Application
    Filed: September 23, 2003
    Publication date: June 10, 2004
    Applicant: Pfizer, Inc.
    Inventors: Oscar Barba, Lyn Howard Jones
  • Publication number: 20040082551
    Abstract: This invention is directed generally to pyrazoles that, inter alia, inhibit p38 kinase, TNF, and/or cyclooxygenase-2 activity.
    Type: Application
    Filed: June 5, 2003
    Publication date: April 29, 2004
    Inventors: Alan G. Benson, Thomas P. Fraher, Michael E. Hepperle, Kevin D. Jerome, Win Naing, Shaun R. Selness, John K. Walker
  • Publication number: 20040077701
    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: June 12, 2003
    Publication date: April 22, 2004
    Applicant: CHIRON CORPORATION
    Inventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Beata Krywult, Rajinder Singh, Liang Wang
  • Publication number: 20040072693
    Abstract: A description is given of derivatives of benzoylpyrazoles of the formula (I) and of their use as herbicides.
    Type: Application
    Filed: August 5, 2003
    Publication date: April 15, 2004
    Inventors: Thomas Seitz, Andreas van Almsick, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
  • Publication number: 20040059128
    Abstract: The invention relates to a method of Aryl preparing 1-alkyl-3-aryl-5-difluoromethoxy-1H-pyrazoles of the formula (I), wherein aryl represents a mono- or polysubstituted phenyl ring, and R1 represents C1-C4 alkyl. The inventive method is characterized by reacting, in a first reaction step, a &bgr;-ketoester of the general formula (II) with hydrazine and by successively reacting the reaction product obtained with chlorodifluoromethane and a compound R1-L, wherein R1 has the meanings indicated above and L represents the leaving group of a nucleophilic displacement reaction.
    Type: Application
    Filed: July 3, 2003
    Publication date: March 25, 2004
    Inventors: Thomas Volk, Michael Puhl, Cyrill Zagar, Rene Lochtman, Norbert Gotz, Gerhard Hamprecht
  • Publication number: 20040058918
    Abstract: The present invention relates to compounds having the general formula 1
    Type: Application
    Filed: September 8, 2003
    Publication date: March 25, 2004
    Inventors: Celia Dominguez, Dawei Zhang
  • Patent number: 6699887
    Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.
    Type: Grant
    Filed: September 20, 2001
    Date of Patent: March 2, 2004
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
  • Publication number: 20040034081
    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: February 19, 2004
    Applicant: Chiron Corporation
    Inventors: Verena D. Huebner, Xiaodong Lin, Ian James, Liya Chen, Manoj Desai, Beata Krywult, Rajinder Singh, Liang Wang
  • Publication number: 20040029886
    Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides
    Type: Application
    Filed: November 7, 2002
    Publication date: February 12, 2004
    Inventors: Jorg Tiebes, Ralf Braun, Joachim Dickhaut, Harald Jakobi, Stephen Lindell, Vincent L. Salgado, Eva Wojtech, Daniela Jans, Jutta Maria Waibel, Waltraud Hempel, Ronald Wilhelm
  • Patent number: 6689805
    Abstract: A pyrazole-3-one derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a pharmaceutical composition containing the derivative or the salt as an active ingredient are provided: wherein: R1 and R2 each independently represent C1-C3 alkyl, aryl, or substituted aryl; R3 represents amino or methyl; R4 and R5 each independently represent hydrogen, C1-C3 alkyl, halogen, methyl substituted with halogen, C1-C3 alkoxy, cyano, or nitro; or a non-toxic salt thereof.
    Type: Grant
    Filed: June 13, 2003
    Date of Patent: February 10, 2004
    Assignee: CJ Corp.
    Inventors: Il Hwan Cho, Ji Young Noh, Sang Wook Park, Hyung Chul Ryu, Jee Woong Lim, Jong Hoon Kim, Myeong Yun Chae, Dal Hyun Kim, Sung Hak Jung, Hyun Jung Park, Young Hoon Kim, In Ki Min
  • 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: 20040002532
    Abstract: A pyrazole-3-one derivative of formula 1 or a non-toxic salt thereof, a preparation method thereof, and a.
    Type: Application
    Filed: June 13, 2003
    Publication date: January 1, 2004
    Inventors: Il Hwan Cho, Ji Young Noh, Sang Wook Park, Hyung Chul Ryu, Jee Woong Lim, Jong Hoon Kim, Myeong Yun Chae, Dal Hyun Kim, Sung Hak Jung, Hyun Jung Park, Young Hoon Kim, In Ki Min
  • Publication number: 20040002523
    Abstract: This invention relates to compounds having the Formula I: 1
    Type: Application
    Filed: June 9, 2003
    Publication date: January 1, 2004
    Applicant: Euro-Celtique S.A.
    Inventors: Derk J. Hogenkamp, Phong Nguyen, Ji Yang
  • Publication number: 20030236253
    Abstract: Thio-alpha-amino acids of general formula (I), wherein R1, R2 and R3 have the meanings given in the description, methods for producing them, and medicaments containing these compounds. The invention also provides methods for treating pain and other diseases using the pharmaceutical compositions comprising the thioamino acids.
    Type: Application
    Filed: March 14, 2003
    Publication date: December 25, 2003
    Applicant: Gruenenthal GmbH
    Inventors: Boris Chizh, Matthias Gerlach, Michael Haurand, Claudia Puetz, Gero Gaube, D. Enders
  • Publication number: 20030228982
    Abstract: The present invention relates to compounds of the formula (I) and/or salts thereof 1
    Type: Application
    Filed: December 13, 2002
    Publication date: December 11, 2003
    Inventors: Hendrik Helmke, Michael Gerhard Hoffmann, Klaus Haaf, Lothar Willms, Thomas Auler, Hermann Bieringer, Hubert Menne
  • Publication number: 20030220339
    Abstract: Heterocyclic arylsulfonamidobenzylic compounds are provided which are useful in treating lipid disorders, metabolic disorders and cell-proliferative diseases.
    Type: Application
    Filed: January 29, 2003
    Publication date: November 27, 2003
    Applicant: Tularik Inc.
    Inventors: Xian Yun Jiao, Frank Kayser, David J. Kopecky, Sharon McKendry, Derek E. Piper, Andrew K. Shiau
  • Publication number: 20030216396
    Abstract: This invention relates to urea compounds containing a pyridine, quinoline, or isoquinoline functionality which is oxidized at the nitrogen heteroatom and which are useful in the treatment of (i) raf mediated diseases, for example, cancer, (ii) p38 mediated diseases such as inflammation and osteoporosis, and (iii) VEGF mediated diseases such as angiogenesis disorders.
    Type: Application
    Filed: February 11, 2003
    Publication date: November 20, 2003
    Applicant: BAYER CORPORATION
    Inventors: Jacques Dumas, William J. Scott, Bernd Riedl
  • Publication number: 20030212116
    Abstract: A heterocyclic imino compound of the formula (1) and an agrochemically acceptable salt thereof; and an agricultural chemical, fungicide and insecticide containing at least one member selected from the group of such compounds as an active ingredient: 1
    Type: Application
    Filed: June 25, 2002
    Publication date: November 13, 2003
    Inventors: Toshio Niki, Takashi Mizukoshi, Hiroaki Takahashi, Jun Satow, Tomoyuki Ogura, Kazuhiro Yamagishi, Hiroyuki Suzuki, Fumio Hayasaka
  • Publication number: 20030207874
    Abstract: Compounds of formula (I), (IIa) or (IIb) wherein R1-R6, Z, Q and n are as defined in claim 1 and their pharmaceutically acceptable salts are ligands at gastrin and/or cholecystokinin receptors. Compositions comprising a compound of formula (I), (IIa) or (IIb) are also described.
    Type: Application
    Filed: April 23, 2003
    Publication date: November 6, 2003
    Inventors: Iain Mair McDonald, Caroline Minli Rachel Low, Katherine Isobel Mary Steel, John Spencer
  • Patent number: 6642265
    Abstract: Invented are non-peptide TPO mimetics. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.
    Type: Grant
    Filed: March 8, 2002
    Date of Patent: November 4, 2003
    Assignee: SmithKline Beecham Corporation
    Inventors: Juan I. Luengo, Kevin J. Duffy
  • Publication number: 20030199394
    Abstract: The present invention describes a method of purifying a pesticide that includes: a) melting a pesticide, wherein the pesticide includes at least one active ingredient and at least one impurity capable of inhibiting crystallization; b) coating the pesticide on a substrate to form a pesticide particle; c) substantially reducing the amount of crystallization inhibiting impurity by an azeotropic method; and d) crystallizing the pesticide. In another embodiment, the present invention includes a method of purifying a pesticide as described above, such that the pesticide has a melting point of not more than about 90° C. Also included in the invention is the product produced by the above process for the pesticide, methyl N-(2-{[1-(4-chlorophenyl)-1H-pyrazol-3-yl]oxymethyl}phenyl)N-methoxy carbamate.
    Type: Application
    Filed: March 26, 2003
    Publication date: October 23, 2003
    Inventors: Charles W. Finch, Kenneth E. Fersch
  • Patent number: 6635641
    Abstract: Amide compounds represented by the formula: wherein: R1 is a moiety represented by the formula  where X is selected from the group consisting of CH2, O, S, and NH; and Y is selected from the group consisting of CH2, O, and S, provided that at least one of X and Y is CH2, or X and Y together with the bond there-between form a cyclopropyl; are described. These compounds and pharmaceutical compositions containing them modulate and/or inhibit the activity of certain protein kinases and are capable of mediating tyrosine kinase signal transduction in order to modulate and/or inhibit unwanted cell proliferation.
    Type: Grant
    Filed: January 19, 2001
    Date of Patent: October 21, 2003
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Steven Lee Bender, Dilip Bhumralkar, Michael Raymond Collins, Stephen James Cripps, Judith Gail Deal, Lei Jia, Mitchell David Nambu, Cynthia Louise Palmer, Zhengwei Peng, Michael David Varney
  • Patent number: 6630487
    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: May 29, 2002
    Date of Patent: October 7, 2003
    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: 20030176466
    Abstract: A method of controlling parasites in or on an animal comprising administering to the animal a parasiticidally effective, substantially non-emetic 1-arylpyrazole.
    Type: Application
    Filed: April 4, 2003
    Publication date: September 18, 2003
    Applicant: Aventis CropScience S.A.
    Inventors: Scot Kevin Huber, David Teh-Wei Chou, Stefan Schnatterer
  • Patent number: 6605631
    Abstract: Compounds of the general formula I where the index and the substituents have the following meanings: n is 0 or 1 to 4; X is O or S; Y is a five-membered heteroaromatic ring; R1 is nitro; cyano; halogen; alkyl; haloalkyl; alkoxy; haloalkoxy; alkylthio; phenyl or phenoxy; R2 is hydrogen; alkyl, alkenyl or alkynyl; or a saturatedy,or unsaturated ring which, in addition to carbon atoms, can also contain hetero atoms as ring members are described.
    Type: Grant
    Filed: September 30, 1999
    Date of Patent: August 12, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Reinhard Kirstgen, Wassilios Grammenos, Herbert Bayer, Reinhard Doetzer, Hartmann Koenig, Klaus Oberdorf, Hubert Sauter, Horst Wingert, Gisela Lorenz, Eberhard Ammermann, Volker Harries
  • 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
  • Patent number: 6600071
    Abstract: A process for preparing compounds of the formula I in which R1 is hydrogen, an aliphatic group having 1-8 carbon atoms, Cl-C6-alkoxycarbonyl, Cl-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. The intermediates of the formula II are novel.
    Type: Grant
    Filed: August 27, 2002
    Date of Patent: July 29, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Norbert Götz, Roland Götz, Michael Rack
  • Publication number: 20030130122
    Abstract: Substituted aryl ether derived compounds represented by the general structure (1) are described.
    Type: Application
    Filed: December 5, 2001
    Publication date: July 10, 2003
    Applicant: ISHIHARA SANGYO KAISHA, LTD.
    Inventors: Sandeep Gupta, Masamitsu Tsukamoto, Mark Read
  • Publication number: 20030125325
    Abstract: The invention relates to novel pyrazolyl benzyl thioethers, to two processes for their preparation and to their use for controlling harmful organisms.
    Type: Application
    Filed: June 28, 2002
    Publication date: July 3, 2003
    Inventors: Ulrich Heinemann, Bernd-Wieland Kruger, Herbert Gayer, Fritz Maurer, Christiane Boie, Ronald Ebbert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik
  • Publication number: 20030109717
    Abstract: A process for preparing compounds of the formula I 1
    Type: Application
    Filed: August 27, 2002
    Publication date: June 12, 2003
    Inventors: Norbert Gotz, Roland Gotz, Michael Rack
  • Publication number: 20030100554
    Abstract: This invention relates to pyrazole derivatives of formula (I) 1
    Type: Application
    Filed: April 5, 2002
    Publication date: May 29, 2003
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Publication number: 20030092740
    Abstract: The present application describes inhibitors of factor Xa with a neutral P1 specificity group of formula I: 1
    Type: Application
    Filed: May 16, 2002
    Publication date: May 15, 2003
    Inventors: Robert A. Galemmo, Celia Dominguez, John M. Fevig, Qi Han, Patrick Y. Lam, Donald J.P. Pinto, James R. Pruitt, Mimi L. Quan
  • Patent number: 6562856
    Abstract: The invention relates to novel pyrazolyl benzyl ethers, to a process for their preparation and to their use for controlling harmful organisms.
    Type: Grant
    Filed: June 14, 2002
    Date of Patent: May 13, 2003
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Herbert Gayer, Peter Gerdes, Bernd-Wieland Krüger, Fritz Maurer, Martin Vaupel, Astrid Mauler-Machnik, Ulrike Wachendorff-Neumann, Gerd Hänssler, Karl-Heinz Kuck, Christoph Erdelen, Peter Lösel
  • Publication number: 20030060494
    Abstract: The present invention relates to use of 1-carbamoylazole derivatives as medicaments and pharmaceutical compositions containing 1-carbamoylazole derivatives as the active ingredient, based on their DPPIV inhibiting effects.
    Type: Application
    Filed: May 15, 2002
    Publication date: March 27, 2003
    Inventors: Nobuyuki Yasuda, Tadashi Nagakura, Kazuto Yamazaki, Seiji Yoshikawa, Toshimi Okada, Hironori Ikuta, Mika Koyanagi
  • Patent number: 6537948
    Abstract: The present invention relates to an uracil compound of the formula [I]: [wherein, Q—R3 represents a R3-substituted group of a 5-membered or 6-membered heterocyclic ring having one or two nitrogen selected from the group consisting of moieties represented in the specification (wherein, this heterocyclic ring may be substituted with at least one kind of substituent, Y represents oxygen, sulfur, imino or C1 to C3 alkylimino, R1 represents C1 to C3 alkyl or C1 to C3 haloalkyl, R2 represents C1 to C3 alkyl, R3 represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, OR7, SR8, N(R9)R10 or the like, X1 represents halogen, cyano, thiocarbamoyl or nitro, X2 represents hydrogen or halogen. {wherein, each of R7, R8 and R10 independently represents carboxy C1 to C6 alkyl, C1 to C6 alkoxycarbonyl C1 to C6 alkyl, C1 to C6 haloalkoxycarbonyl C1 to C6 alkyl, or the like, and R9 represents hydrogen or C1 to C6 alkyl.}.].
    Type: Grant
    Filed: January 31, 2001
    Date of Patent: March 25, 2003
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshitomo Tohyama, Yuzuru Sanemitsu
  • 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
  • Patent number: 6515139
    Abstract: The present invention relates to a process for preparing N-substituted 2-pyrazolin-5-ones of the formula I where R has the meaning given in claim 1, which comprises reacting a compound of the formula II where R, X and Y have the meanings given in claim 1, at elevated temperature with a molar excess of alkali metal hydroxide in an aqueous reaction medium and then adjusting the pH to pH≦6 by adding an acid.
    Type: Grant
    Filed: May 13, 2002
    Date of Patent: February 4, 2003
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans Rupert Merkle, Erich Fretschner, Knut Koob
  • 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: 20030018197
    Abstract: The present invention comprises novel and known pyrazole derivatives having anti-HIV activity, a process for their manufacture, pharmaceutical compositions and the use of such compounds in medicine. In particular, the compounds of formula I are inhibitors of the human immunodeficiency virus reverse transcriptase enzyme which is involved in viral replication. Consequently the compounds of this invention may be advantageously used as therapeutic agents for HIV infection.
    Type: Application
    Filed: September 20, 2001
    Publication date: January 23, 2003
    Inventors: Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
  • Publication number: 20030004193
    Abstract: 1-Heterocycle substituted diarylamines, methods of making and using them, and compositions containing them.
    Type: Application
    Filed: July 23, 2002
    Publication date: January 2, 2003
    Inventors: Stephen Douglas Barrett, Alexander James Bridges, Haile Tecle, Lu-Yan Zhang
  • Publication number: 20030004344
    Abstract: This invention relates generally to inhibitors of trypsin-like serine protease enzymes, especially factor Xa or thrombin, pharmaceutical compositions containing the same, and methods of using the same as anticoagulant agents for treatment and prevention of thromboembolic disorders.
    Type: Application
    Filed: January 2, 2002
    Publication date: January 2, 2003
    Inventors: Patrick Y.S. Lam, Charles G. Clark, Renhau Li, Donald J.P. Pinto