Chalcogen Bonded Directly To Ring Carbon Of The Diazole Ring Patents (Class 548/366.1)
  • Publication number: 20100210704
    Abstract: To provide pesticides such as insecticides, miticides and nematicides, which are excellent in the safety, pesticidal effects, residual effectiveness, etc., which further have infiltration, and which can be applied by soil treatment. A pesticide comprising a 3-alkoxy-1-phenyl-pyrazole derivative represented by the formula [I] or an agriculturally acceptable salt thereof as an active ingredient: wherein, for example, R1 is a C1-C10 alkyl group or the like, R2 is a hydrogen atom or the like, R3 is a hydrogen atom or the like, and each of R4, R5, R6 and R8 which are independent of one another, is a hydrogen atom or the like, and R7 is a C2-C4 haloalkylthio group or the like.
    Type: Application
    Filed: October 17, 2008
    Publication date: August 19, 2010
    Applicants: KUMIAI CHEMICAL INDUSTRY CO., LTD., IHARA CHEMICAL INDUSTRY CO., LTD.
    Inventors: Satoru Ohata, Katsuya Kato, Keiji Toriyabe, Yoshihiro Ito, Ryuji Hamaguchi, Yuki Nakano
  • Patent number: 7759291
    Abstract: The present invention provides a pyrazole compound of formula (a): a noxious arthropod pests controlling composition containing the compound shown by the formula (a) as an active ingredient; and a method for controlling noxious arthropod pests comprising applying an effective amount of the compound shown by the formula (a).
    Type: Grant
    Filed: January 25, 2005
    Date of Patent: July 20, 2010
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hayato Takyo, Masaya Hashizume, Noriyasu Sakamoto
  • Publication number: 20100152443
    Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.
    Type: Application
    Filed: February 26, 2010
    Publication date: June 17, 2010
    Applicants: SAGAMI CHEMICAL RESEARCH CENTER, KAKEN PHARMACEUTICAL CO., LTD.
    Inventors: Kenji Hirai, Atsushi Uchida, Atsuko Watanabe, Taeko Abe, Takuya Ueda, Hiroshi Sakurai
  • Publication number: 20100113276
    Abstract: The use of N2-phenylamidines of formula (I) as herbicides is described. In this formula (I), R2, R3, R4, R5 and R6 are different radicals and A is a bond or various 1- or polyatomic bridging elements.
    Type: Application
    Filed: March 4, 2008
    Publication date: May 6, 2010
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Birgit Kuhn, Harald Jakobi, Thomas Mueller, Joerg Tiebes, Heinz Kehne, Dirk Schmutzler, Martin Hills, Christopher Rosinger, Klaus Kunz, Mark Wilheim Drewes, Dieter Feucht, Thomas Seitz, Benoit Hartmann, Ralf Dunkel, Joerg Nico Greul, Oliver Guth, Kerstein Ilg, Darren James Mansfeld, Wahed Ahmed Moradi, Peter Dahmen, Ulrike Wachendorf-Neumann, Arnd Voerste, Dale Robert Mitchell, Jean-Pierre Andre Vors, Dale Robert Mitchell, Tom Hough
  • Publication number: 20100112104
    Abstract: The invention relates to a new derivative of aryldimethylpyrazolone of formula (I) which is effective in reducing unsightly cellulite, and compositions containing it.
    Type: Application
    Filed: March 20, 2008
    Publication date: May 6, 2010
    Applicant: A.MENARINI INDUSTRIE FARMACEUTICHE RIUNITE S.R.L.
    Inventor: Alberto Aleotti
  • Patent number: 7700786
    Abstract: The present invention provides a pyrazole derivative of the general formula (1), which has an excellent efficacy as an active component for a herbicide, an intermediate for the production thereof, processes for the production thereof, and a herbicide containing the derivative as an active ingredient.
    Type: Grant
    Filed: February 19, 2002
    Date of Patent: April 20, 2010
    Assignees: Sagami Chemical Research Center, Kaken Pharmaceutical Co., Ltd.
    Inventors: Kenji Hirai, Atsushi Uchida, Atsuko Watanabe, Taeko Abe, Takuya Ueda, Hiroshi Sakurai
  • Publication number: 20100087428
    Abstract: The present invention provides a compound of formula (I) or its salts or pharmaceutically acceptable derivatives thereof wherein; X1 is selected from a group consisting of CH2, C(?O), C(?NH), NC(?O), R1 is selected from the group consisting of optionally substituted arylalkyl, and optionally substituted heteroarylalkyl R2 is selected from the group consisting of optionally substituted alkyl, optionally substituted aryl or heteroaryl or NR24R25 R3 is selected from the group consisting of hydrogen, halogen, hydroxyl, alkoxy, aryloxy, optionally substituted alkyl, optionally substituted amino, optionally substituted amino sulfonyl or nitrile; R4 is selected from the group consisting of optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted heterocycloalkyl, optionally substituted acyl, optionally substituted sulfonyl, optionally substituted sulfamoyl, optionally substituted aryl, optionally substituted arylalkyl, and optionally substituted heteroaryl R5 may be hydrogen, an o
    Type: Application
    Filed: August 31, 2009
    Publication date: April 8, 2010
    Applicant: Xention Limited
    Inventors: Mushtaq Mulla, Derek Edward John, Richard John Hamlyn, Sasha Louise Garrett, Basil Hartzoulakis, David Madge, John Ford
  • Publication number: 20100055116
    Abstract: The present invention relates to compositions and methods for targeting c-Rel. In particular, the present invention provides compositions and methods for treating cancers, inflammatory diseases, autoimmune diseases, and transplant rejection by inhibiting c-Rel activity and for regulating c-Rel for research and drug screening applications.
    Type: Application
    Filed: April 13, 2007
    Publication date: March 4, 2010
    Inventors: Hsiou-chi Liou, Wenzhi Tian, Shuhua Cheng, Constance Y. Hsia, Alex Owyang, Jason J. Hsu
  • Patent number: 7659300
    Abstract: The present invention is directed to compounds of Formula I: I (where A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
    Type: Grant
    Filed: September 6, 2005
    Date of Patent: February 9, 2010
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Ian M. Bell, Craig A. Stump
  • Patent number: 7652049
    Abstract: Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: January 26, 2010
    Assignee: Merck & Co., Inc.
    Inventors: Amjad Ali, Joann M. Napolitano, Qiaolin Deng, Zhijian Lu, Peter J. Sinclair, Gayle E. Taylor, Christopher F. Thompson, Nazia Quraishi, Cameron J. Smith, Julianne A. Hunt, Adrian A. Dowst, Yi-Heng Chen, Hong Li
  • Patent number: 7652057
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R4 have the significance given in claim 1 can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: August 29, 2006
    Date of Patent: January 26, 2010
    Assignee: Hoffman-La Roche Inc.
    Inventors: Kurt Amrein, Daniel Hunziker, Bernd Kuhn, Alexander V Mayweg, Werner Neidhart
  • Patent number: 7642360
    Abstract: Disclosed herein are a composition for dyeing keratinous fibers, for example, human keratinous fibers such as hair, comprising at least one oxidation base chosen from diamino-N,N-dihydropyrazolone derivative and a method using the composition. Further disclosed herein are amino-N,N-dihydropyrazolone derivatives and the addition salts thereof and diamino-N,N-dihydropyrazolone derivatives and the addition salts thereof, as well as the methods for preparing these compounds.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: January 5, 2010
    Assignee: L'Oreal S.A.
    Inventors: Laurent Vidal, Aziz Fadli
  • Patent number: 7635664
    Abstract: The invention relates to benzoylpyrazoles of the general formula (I), in which Q, R1, R2, R3, R4, R5, Y and Z are as defined in the disclosure, to processes and intermediates for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: May 8, 2002
    Date of Patent: December 22, 2009
    Assignee: Bayer CropScience AG
    Inventors: Hans-Georg Schwarz, Klaus-Helmut Müller, Stefan Herrmann, Dorothee Hoischen, Kristian Kather, Stefan Lehr, Otto Schallner, Mark Wilhelm Drewes, Peter Dahmen, Dieter Feucht, Rolf Pontzen
  • Patent number: 7635684
    Abstract: The present invention provides pyrazole derivatives represented by the general formula: wherein R1 represents H, an optionally substituted C1-6 alkyl group etc.; one of Q and T represents a group represented by the general formula: or a group represented by the general formula: while the other represents an optionally substituted C1-6 alkyl group etc.; R2 represents H, a halogen atom, OH, an optionally substituted C1-6 alkyl group etc.; X represents a single bond, O or S; Y represents an optionally substituted C1-6 alkylene group etc.; Z represents —RB, —CORC etc. in which RB represents an optionally substituted C1-6 alkyl group etc.; and RC represents an optionally substituted C1-6 alkyl group etc.; R4 represents H, an optionally substituted C1-6 alkyl group etc.; and R3, R5 and R6 represent H, a halogen atom etc.
    Type: Grant
    Filed: August 21, 2003
    Date of Patent: December 22, 2009
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Nobuhiko Fushimi, Kazuo Shimizu, Shigeru Yonekubo, Hirotaka Teranishi, Masaki Tomae, Masayuki Isaji
  • Patent number: 7608635
    Abstract: Compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I) and methods of inhibiting Hsp90 in a cell, treating or preventing a proliferation disorder in a mammal and treating cancer in a mammal comprising administering a compound of formula (I) to a patient or a cell. Variable R5 is an optionally substituted heteroaryl; an optionally substituted 6 to 14-membered aryl; a bicyclic 9-member heterocycle optionally substituted at any substitutable nitrogen or carbon atoms; or a substituent R18, defined herein. Ring A is an aryl or a heteroaryl optionally further substituted with one or more substituents in addition to R3. Substituent R3 is defined herein.
    Type: Grant
    Filed: August 10, 2006
    Date of Patent: October 27, 2009
    Assignee: Synta Pharmaceuticals Corp.
    Inventors: Weiwen Ying, Shijie Zhang, Zhenjian Du, Kevin Foley
  • Patent number: 7569519
    Abstract: What is described are derivatives of benzoyl derivatives of the formula (I) and their use as herbicides. In this formula (I), R1, R2 and R3 are different radicals, X is a bridge atom selected from the group consisting of oxygen and sulfur and Het is a saturated heterocyclic group which comprises oxygen and carbon atoms.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: August 4, 2009
    Assignee: Bayer CropScience AG
    Inventors: Andreas Van Almsick, Lothar Willms, Hermann Bieringer, Hubert Menne, Thomas Auler
  • Patent number: 7507833
    Abstract: A compound having a structure and therapeutic methods, compositions, and medicaments related thereto are disclosed herein.
    Type: Grant
    Filed: August 8, 2007
    Date of Patent: March 24, 2009
    Assignee: Allergan, Inc.
    Inventors: David W. Old, Danny T. Dinh
  • Patent number: 7488831
    Abstract: A pyrazole compound represented by general formula (1) is reacted with a sulfur compound represented by general formula (2) in the presence of a base and formaldehyde, to thereby produce a 5-hydroxy-4-thiomethylpyrazole compound represented by general formula (3). The 5-hydroxy-4-thiomethylpyrazole compound may easily be produced in a good yield, by using such a process. Further, this process may easily provide the 5-hydroxy-4-thiomethylpyrazole compound under a mild condition in a single step, without using a special apparatus, an expensive catalyst, or a transition metal, etc. In addition, this process may be conducted substantially without producing a harmful waste which can be derived from a catalyst, etc., and therefore this process is friendly to the environment and industrially valuable.
    Type: Grant
    Filed: March 31, 2005
    Date of Patent: February 10, 2009
    Assignee: Ihara Chemical Industry Co., Ltd.
    Inventor: Yukio Uchida
  • Patent number: 7482375
    Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6-alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R2 represents H, C1-6alkyl (optionally substituted by R3), phenyl (optionally substituted by CN), or Het; R3 represents OH, CN, Het, —R4—C1-6alkyl, or CONR5R6; R4 represents —CO2—, or —O—; R5 and R6 independently represent H, C1-6alkyl (optionally substituted by OR7) or C3-8cycloalkyl; R7 represents H or C1-6alkyl; Het represents a five or six membered aromatic heterocyclic group containing (i) from one to four nitrogen heteroatom(s) or (ii) one or two nitrogen heteroatom(s) and one oxygen or one sulphur heteroatom or (iii)one or two oxygen or sulphur heteroatom(s), said heterocyclic group being optionally substituted by one or more groups selected from CN and C1-6alkyl; R8 represents C1-6alkyl, C1-6alkyloxy, C3-8cycloalkyl, or halo; R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treating e
    Type: Grant
    Filed: April 18, 2006
    Date of Patent: January 27, 2009
    Assignee: Pfizer Inc.
    Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
  • Publication number: 20090018345
    Abstract: Disclosed are pyrazole-1-carboxylate derivatives of the general formula (1), (wherein symbols are as defined in the specification), a process for the production thereof and processes for producing herbicidally active 3-aryloxypyrazole-1-carboxamide derivatives from the above compound and an intermediate therefor. According to this invention, there can be industrially advantageously produced 3-aryloxypyrazole-1-carboxamide derivatives that does not cause chemical damage on crops but exhibits excellent herbicidal activity against weeds that impair the growth of such crops.
    Type: Application
    Filed: May 22, 2006
    Publication date: January 15, 2009
    Applicants: KAKEN PHARMACEUTICAL CO., LTD., SAGAMI CHEMICAL RESEARCH CENTER
    Inventors: Atsushi Uchida, Wakako Yokota, Kenji Hirai, Tomoyuki Yano
  • Publication number: 20080275070
    Abstract: The invention relates to aryl ether compounds and its preparation method and use thereof. The aryl ether compounds of the invention having general formula (I): The groups are as defined as specification. The aryl ether compounds of present invention have wide spectrum fungicidal activity, and may be used to control diseases in all sorts of plants caused by oomycete, basidiomycete, ascomycete pathogens and deuteromycete. The some of the compounds have very good insecticidal and acaricidal activity, and may be used to control insects and mites.
    Type: Application
    Filed: May 15, 2006
    Publication date: November 6, 2008
    Applicant: SHENYANG RESEARCH INSTITUTE OF CHEMICAL INDUSTRY
    Inventors: Changling Liu, Miao Li, Zhinian Li, Liwen Geng, Hong Zhang, Defeng Zhou, Dongliang Cui, Yanmei Luo
  • Publication number: 20080269220
    Abstract: A compound represented by the formula (1): wherein each symbol is as defined in the specification, and a salt thereof and a prodrug thereof unexpectedly have superior GPR40 receptor agonist activity, superior in the properties as a pharmaceutical product such as stability and the like, and can be a safe and useful pharmaceutical agent as a drug for the prophylaxis or treatment of GPR40 receptor related pathology or diseases such as diabetes and the like.
    Type: Application
    Filed: March 14, 2005
    Publication date: October 30, 2008
    Inventors: Tsuneo Yasuma, Nobuyuki Negoro, Shinobu Sasaki
  • Patent number: 7439242
    Abstract: Modulators of PPAR? activity are provided which are useful in pharmaceutical compositions and methods for the treatment of conditions such as type II diabetes and obesity.
    Type: Grant
    Filed: April 15, 2002
    Date of Patent: October 21, 2008
    Assignee: Amgen Inc.
    Inventors: Jonathan B. Houze, Lawrence R. McGee, Steven Marc Rubenstein
  • Patent number: 7439366
    Abstract: The present invention relates to a phenacylamine derivative of the formula (I) or a salt thereof: wherein A is alkyl, cycloalkyl, phenyl which may be substituted by Y, pyridyl which may be substituted by Y, or pyrazolyl which may be substituted by Y, R1 and R2 are each alkyl, or R1 and R2 may together form a 3- to 6-membered saturated carbocycle, R3 is hydrogen, alkyl, alkoxyalkyl, alkylthioalkyl or COR4, X is halogen, alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl, alkoxy, haloalkoxy, alkenyloxy, haloalkenyloxy, alkynyloxy, haloalkynyloxy, alkylthio, haloalkylthio, alkenylthio, haloalkenylthio, alkynylthio, haloalkynylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, dialkylaminosulfonyl, nitro, cyano, phenyl which may be substituted by Y, phenoxy which may be substituted by Y, benzyloxy which may be substituted by Y, or pyridyloxy which may be substituted by Y, and n is an integer of from 0 to 5.
    Type: Grant
    Filed: February 9, 2001
    Date of Patent: October 21, 2008
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Yuji Nakamura, Masayuki Morita, Kenji Izakura
  • Patent number: 7414040
    Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. 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: June 6, 2003
    Date of Patent: August 19, 2008
    Assignee: SmithKline Beecham Corporation
    Inventor: Dirk A. Heerding
  • Publication number: 20080194405
    Abstract: The present invention relates to novel 5-hydroxypyrazolines of the formula I in which the substituents are as defined below: B is phenyl, naphthyl or 5- or 6-membered hetaryl which contains one to four heteroatoms from the group consisting of O, N and S; A is C?O, C?S or SO2; R1 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl or haloalkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, phenyl, 5- or 6-membered heterocyclyl or hetaryl which contains one to four heteroatoms from the group consisting of O, N and S; R2 is alkyl, haloalkyl, alkenyl, haloalkyl, alkynyl, haloalkynyl, cycloalkyl, cycloalkenyl, cycloalkynyl, phenyl, 5- or 6-membered hetaryl or heterocyclyl which contains one to four heteroatoms from the group consisting of O, N and S; R3 is hydrogen, nitro, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, haloalkenyl, alkynyl, haloalkynyl or NR?2, where R? independently of one another are hydrogen or alkyl; R4 is hydrogen, halogen, nitro, cyano, NR?2, alkyl, haloalkyl, COOR? or 5- or 6-memb
    Type: Application
    Filed: May 24, 2006
    Publication date: August 14, 2008
    Applicant: BASF Atkiengesellschaft
    Inventors: Markus Gewehr, Jochen Dietz, Thomas Grote, Andreas Gypser, Matthias Niedenbruck
  • Publication number: 20080182861
    Abstract: Compounds of formula (I), or a pharmaceutically acceptable salt, prodrug, salt of a prodrug, or a combination thereof, Pharmaceutical compositions of formula (I) and related methods for treating or preventing metabolic diseases or conditions.
    Type: Application
    Filed: November 29, 2007
    Publication date: July 31, 2008
    Inventors: Andrew J. Souers, Ju Gao, Todd Matthew Hansen, Rajesh R. Iyengar, Philip R. Kym, Bo. X. Liu, Zhonghua Pei, Vince Yeh, Gang Zhao
  • Patent number: 7396939
    Abstract: What is described are 3-cyclopropyl-4-(3-amino-2-methylbenzoyl)pyrazoles of the formula (I) and their use as herbicides. In this formula (I), R1, R2, R3, R4 and R5 are various radicals.
    Type: Grant
    Filed: December 8, 2005
    Date of Patent: July 8, 2008
    Assignee: Bayer CropScience GmbH
    Inventors: Monika Schmitt, Lothar Willms, Ines Heinemann, Andreas Van Almsick, Thomas Auler, Martin Hills, Heinz Kehne, Dieter Feucht
  • Publication number: 20080090880
    Abstract: Novel phenylpyrazole derivatives of the formula (I), in which R1-R6, X and Y have the meanings indicated in Claim 1, are HSP90 inhibitors and can be used for the preparation of a medicament for the treatment of diseases in which the inhibition, regulation and/or modulation of HSP90 plays a role
    Type: Application
    Filed: September 14, 2005
    Publication date: April 17, 2008
    Inventors: Hans-Michael Eggenweiler, Michael Wolf
  • Patent number: 7323574
    Abstract: A process for the preparation of compound (III) which comprises the reaction between a compound of general formula (V) and dicyano acetylene (IV), said reaction carried out in the presence of water wherein R is selected from CF3, or C1 to C6 alkyl M is an alkaline or alkaline-earth metal or silver.
    Type: Grant
    Filed: September 28, 2006
    Date of Patent: January 29, 2008
    Assignee: BASF Agro B.V. Arnhem
    Inventors: Jean-Erick Ancel, Joelle Vidal
  • Patent number: 7320995
    Abstract: The present invention provides kinase inhibitors of Formula I: wherein W represents inter alia imidazol, oxazol, pyrazol, thiazol as triazol, which are substituted by phenyl or thienyl.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: January 22, 2008
    Assignee: Eli Lilly and Company
    Inventors: Rosanne Bonjouklian, Jose Eugenio De Diego Gomez, Alfonso De Dios, Chafiq Hamdouchi Hamdouchi, Tiecho Li, Beatriz Lopez De Uralde Garmendia, Michal Vieth, Jeremy Schulenberg York, Robert Dean Dally, Miriam Filadelfa Del Prado Catalina, Carlos Jaramillo Aguado, Luisa Maria Martin-Cabrejas, Carlos Montero Salgado, Sheila Pleite Selgas, Concepcion Sanchez-Martinez, Timothy Alan Shepherd, James Howard Wikel
  • Patent number: 7285569
    Abstract: The present invention relates to compounds of formula I their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: September 23, 2005
    Date of Patent: October 23, 2007
    Assignee: Hoff Hoffmann-La Roche Inc.
    Inventors: Georges Guy, Bernhard Goller, Hans-Willi Krell, Klaus-Peter Kuenkele, Anja Limberg, Petra Rueger, Matthias Rueth
  • Patent number: 7256298
    Abstract: The present invention provides pyrazole derivatives useful as production intermediates for isoxazoline derivatives having an excellent herbicidal effect and selectivity between crops and weeds as well as processes for producing the same.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: August 14, 2007
    Assignees: Ihara Chemical Industry Co., Ltd., Kumiai Chemical Industry Co., Ltd.
    Inventors: Masao Nakatani, Minoru Ito, Masahiro Miyazaki
  • Patent number: 7253169
    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: Grant
    Filed: April 17, 2001
    Date of Patent: August 7, 2007
    Assignee: Gliamed, Inc.
    Inventors: Yong-Qian Wu, Wei Huang, Gregory S. Hamilton
  • Patent number: 7230025
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereof, wherein R1 to R4 are defined in the description, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodeficiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: September 23, 2003
    Date of Patent: June 12, 2007
    Assignee: Pfizer, Inc.
    Inventors: Oscar Barba, Lyn Howard Jones
  • Patent number: 7183306
    Abstract: A compound of the formula (I): wherein R1 is hydrogen or lower alkyl; R2 is lower alkyl, etc.; R3 is lower alkoxy, etc.; R4 is hydroxy, etc.; X is O, S, etc.; Y is CH or N; Z is lower alkylene or lower alkenylene; and m is 0 or 1; or salts thereof, which are useful as a medicament.
    Type: Grant
    Filed: November 14, 2003
    Date of Patent: February 27, 2007
    Assignee: Astellas Pharma Inc.
    Inventors: Fumiyuki Shirai, Hidenori Azami, Natsuko Kayakiri, Kazuo Okumura, Katsuya Nakamura
  • Patent number: 7183296
    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: January 27, 2004
    Date of Patent: February 27, 2007
    Assignee: Roche Palo Alto LLC
    Inventors: Brian William Dymock, Philip Stephen Jones, John Herbert Merrett, Martin John Parratt
  • Patent number: 7115575
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: July 28, 2005
    Date of Patent: October 3, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Patent number: 7109228
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivatives thereof, and to processes for the preparation thereof, intermediates used in their preparation of, compositions containing them and the uses of such derivatives. The compounds of the present invention bind to the enzyme reverse transcriptase and are modulators, especially inhibitors thereof. As such, the compounds of the present invention are useful in the treatment of a variety of disorders including those in which the inhibition of reverse transcriptase is implicated. Disorders of interest include those caused by Human Immunodificiency Virus (HIV) and genetically related retroviruses, such as Acquired Immune Deficiency Syndrome (AIDS).
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: September 19, 2006
    Assignee: Agouron Pharmaceuticals, Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 7056892
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: July 27, 2005
    Date of Patent: June 6, 2006
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Patent number: 7037880
    Abstract: Ethylene derivatives of formula (I): where Q is an unsubstituted or substituted phenyl or heterocyclic group, especially a 4-thiazolyl, 1- or 3-pyrazolyl, 1,3-oxazol-4-yl, phenyl or pyridyl group; E is a substituent such as a cyano group; A is a substituent such as a 4-pyrazolyl or thiazolyl group; and B is a substituent such as an alkylcarbonyl group. Agricultural chemicals and agents for preventing the attachment of aquatic organisms containing one or more such ethylene derivatives.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: May 2, 2006
    Assignee: Nissan Chemical Industries, Ltd.
    Inventors: Tomoyuki Ogura, Hiroshi Murakami, Akira Numata, Rika Miyachi, Toshiro Miyake, Norihiko Mimori, Shinji Takii
  • Patent number: 7002023
    Abstract: The present invention relates to a process for preparing 1-substituted 5-chloro-4-methylpyrazoles of the general formula I with the meaning for R stated in claim 1, in which a 4-methylpyrazole of the formula II is reacted with chlorine, the resulting mixture of monochlorinated and dichlorinated product is fractionated by distillation, and subsequently the dichlorinated compound is dehalogenated to compound II and returned to the reaction with chlorine.
    Type: Grant
    Filed: September 28, 2001
    Date of Patent: February 21, 2006
    Assignee: BASF Aktiengesellschaft
    Inventors: Hans Rupert Merkle, Erich Fretschner
  • Patent number: 6998490
    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 ?-phthalimidoperhexanoic acid is particularly useful for the preparation of compounds of industrial interest, in particular pharmaceuticals for human or veterinary use.
    Type: Grant
    Filed: March 17, 2004
    Date of Patent: February 14, 2006
    Assignees: Dinamite Dipharma S.p.A., Abbreviated Dipharma S.p.A.
    Inventors: Pietro Allegrini, Caterina Napoletano, Gabriele Razzetti, Graziano Castaldi
  • Patent number: 6992099
    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: Grant
    Filed: April 4, 2003
    Date of Patent: January 31, 2006
    Assignee: Aventis Cropscience S.A.
    Inventors: Scot Kevin Huber, David Teh-Wei Chou, Stefan Schnatterer, Henricus Maria Martinus Bastiaans
  • Patent number: 6972283
    Abstract: The present invention relates to glucopyranosyloxypyrazole derivatives represented by the general formula: wherein R1 represents a hydrogen atom or a lower alkyl group; one of Q1 and T1 represents a group represented by the general formula: while the other represents a lower alkyl group or a halo(lower alkyl) group; and R2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a lower alkylthio group, a halo(lower alkyl) group or a halogen atom, or pharmaceutically acceptable salts thereof, which have an inhibitory activity in human SGLT2 and are useful as agents for the prevention or treatment of diabetes, diabetic complications or obesity, and to pharmaceutical compositions comprising the same and intermediates thereof.
    Type: Grant
    Filed: January 20, 2004
    Date of Patent: December 6, 2005
    Assignee: Kissei Pharmaceutical Co., Ltd.
    Inventors: Hideki Fujikura, Toshihiro Nishimura, Kenji Katsuno, Masahiro Hiratochi, Akira Iyobe, Minoru Fujioka, Masayuki Isaji
  • Patent number: 6949551
    Abstract: Dihalopropene compounds, process for their preparation, compositions comprising them and their use as pesticides What is described are dihalopropene compounds of the formula (I) in which R1 and R2 are halogen, Y is —O—, —S— or —NH—, X is —O—, —S(O)r— or —NR5— (where r=0, 1, 2 and R5 is hydrogen or C1-C8-alkyl), X? is a direct C—C bond, —O—, —S(O)r— or —NR5— (where R5 is as defined above), R3 is hydrogen, halogen, nitro, cyano, C1-C8-alkyl, C1-C8-haloalkyl, C1-C8-alkoxy, C1-C8-haloalkoxy, C3-C10-cycloalkyl or has one of the meanings defined for A, A has the meaning given in the description (inter alia aryl, heterocyclyl), B is a divalent bridge having the meanings given in the description (inter alia alkylene) and R4 is a monovalent C6-C14-aryl radical or nitrogen-containing heteroaryl radical having at least one ring heteroatom which has the meanings given in the description. These compounds can be used for preparing pesticides.
    Type: Grant
    Filed: November 7, 2002
    Date of Patent: September 27, 2005
    Assignee: Bayer Cropscience S.A.
    Inventors: Jörg 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: 6916839
    Abstract: The present invention relates to pyrazolylarylalkines and to their use, to a process for preparing pyrazolylarylalkines and also to intermediates.
    Type: Grant
    Filed: January 5, 2004
    Date of Patent: July 12, 2005
    Assignee: Bayer Chemicals Aktiengesellschaft
    Inventors: Wolfgang Ebenbeck, Florian Rampf, Albrecht Marhold
  • Patent number: 6897322
    Abstract: The invention relates to a method of 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 ?-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: Grant
    Filed: January 15, 2002
    Date of Patent: May 24, 2005
    Assignee: BASF Aktiengesellschaft
    Inventors: Thorsten Volk, Michael Puhl, Cyrill Zagar, Rene Lochtman, Norbert Götz, Gerhard Hamprecht
  • Patent number: 6881848
    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: July 3, 2003
    Date of Patent: April 19, 2005
    Assignee: BASF Agro B.V. Arnhem (NL), Wädenswil-Branch
    Inventors: Jean-Louis Clavel, Isabelle Pelta, Sylvie Le Bars, Philippe Charreau
  • Patent number: 6867202
    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 th compounds of formula I. This invention is further directed to methods comprising administering to a human or other animal a combination of a functional somatostatin antagonist such as an alpha-2 adrenergic agonist and a compound of formula I.
    Type: Grant
    Filed: July 22, 2003
    Date of Patent: March 15, 2005
    Assignee: Pfizer Inc.
    Inventors: Philip Albert Carpino, Charles Kwok-Fung Chiu, Lydia Codetta Pan, Bruce Allen Lefker, Judith Lee Treadway, Michael Paul Zawistoski