Two Diazole Rings Are Bonded Directly To Each Other, To The Same Acyclic Carbon Atom Or To The Same Acyclic Carbon Chain Patents (Class 548/365.4)
  • Publication number: 20150105252
    Abstract: Disclosed is a method for controlling the growth of undesired vegetation comprising contacting the vegetation or its environment with a herbicidally effective amount of a compound of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, R1, Q and J are as defined in the disclosure. Also disclosed is a method wherein the compound of Formula 1 (i.e. in a herbicidally effective amount) is comprised in a herbicidal composition further comprising at least one component selected from the group consisting of surfactants, solid diluents and liquid diluents. Also disclosed are compound of Formula 1 (including all stereoisomers), including N-oxides and salts thereof, their use as herbicides wherein A, R1, Q and J are as defined in the disclosure.
    Type: Application
    Filed: October 15, 2014
    Publication date: April 16, 2015
    Inventor: THOMAS MARTIN STEVENSON
  • Publication number: 20150072396
    Abstract: Low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations for modifying biomolecules is provided. Compositions, methods, and kits relating to low-copper click chemistry, 1.3-dipolar cycloadditions, and Staudinger ligations are also provided.
    Type: Application
    Filed: March 1, 2012
    Publication date: March 12, 2015
    Applicant: LIFE TECHNOLOGIES CORPORATION
    Inventors: Kyle Gee, Upinder Singh, Scott Grecian, Scott Clarke
  • Patent number: 8946236
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: February 3, 2015
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Patent number: 8916555
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: December 23, 2014
    Assignee: Axikin Pharmaceuticals, Inc.
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20140343030
    Abstract: The present invention provides compounds of Formula I: or pharmaceutically acceptable salts thereof, as well as their compositions and methods of use, that inhibit the activity of Janus kinase (JAK) and are useful in the treatment of diseases related to the activity of JAK including, for example, inflammatory disorders, autoimmune disorders, cancer, and other diseases.
    Type: Application
    Filed: May 16, 2014
    Publication date: November 20, 2014
    Applicant: Incyte Corporation
    Inventors: Yun-Long Li, Jincong Zhuo, Ding-Quan Qian, Song Mei, Ganfeng Cao, Yongchun Pan, Qun Li, Zhongjiang Jia
  • Publication number: 20140329684
    Abstract: The invention relates to the use of 4-substituted 1-phenylpyrazole-3-carboxylic acid derivatives of the general formula (I), or salts thereof, where the radicals in the general formula (I) correspond to the definitions given in the description, for enhancing stress tolerance in plants to abiotic stress, for strengthening plant growth and/or for increasing plant yield, and to selected processes for preparing the compounds mentioned above.
    Type: Application
    Filed: September 20, 2012
    Publication date: November 6, 2014
    Inventors: Thomas Müller, Lothar Willms, Stefan Lehr, Monika H. Schmitt, Ines Heinemann, Jan Dittgen, Christopher Hugh Rosinger, Martin Jeffrey Hills, Pascal Von Kosküll-Döring, Isolde Häuser-Hahn
  • Publication number: 20140288105
    Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds described herein are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 25, 2014
    Applicant: EPIZYME, INC.
    Inventors: RICHARD CHESWORTH, LORNA HELEN MITCHELL, GIDEON SHAPIRO, OSCAR MIGUEL MORADEI
  • Publication number: 20130338162
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: July 29, 2013
    Publication date: December 19, 2013
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
  • Publication number: 20130324560
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Bernd Alig, Ruediger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Goergens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Publication number: 20130303492
    Abstract: Provided herein are 3,5-diaminopyrazoles, for example, compounds of Formula IA, that are useful for modulating regulated-in-COPD kinase activity, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a RC kinase-mediated disorder, disease, or condition.
    Type: Application
    Filed: March 14, 2013
    Publication date: November 14, 2013
    Inventors: Erik Dean Raaum, Garrett Thomas Potter, Tai Wei Ly
  • Publication number: 20130296567
    Abstract: A bisazole-based compound is represented by formula (I): wherein X represents C—R3 or nitrogen, R1 and R2 independently represent a haloalkyl group, R3 represents H or F. A transition metal complex is represented by formula (II): ML1L2L3??(II) wherein M is a transition metal, L1 represents in which X represents C—R31 or nitrogen, R11 and R21 independently represent a haloalkyl group, and R31 represents H or F; and L2 and L3 independently represent a dipyridine-based ligand.
    Type: Application
    Filed: November 2, 2012
    Publication date: November 7, 2013
    Inventors: Yun CHI, Hsiu-Hsuan YEH, Shu-Te HO, Shih-Han CHANG
  • Patent number: 8536214
    Abstract: The present invention relates to a heterocyclic derivative according to formula (I); wherein the variables are defined as in the specification, or to a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to a pharmaceutical composition comprising said heterocyclic derivatives and to their use in therapy, for instance in the treatment or prevention of psychiatric diseases where an enhancement of synaptic responses mediated by AMPA receptors is required, including schizophrenia, depression and Alzheimer's disease.
    Type: Grant
    Filed: June 3, 2009
    Date of Patent: September 17, 2013
    Inventors: Jonathan Gillespie, Craig Jamieson, John Kinaird Fergusen MaClean, Elizabeth Margaret Moir, Zoran Rankovic
  • Patent number: 8536092
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: September 17, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Bernd Alig, Rüdiger Fischer, Christian Funke, Rudolf F. Ernst Gesing, Achim Hense, Olga Malsam, Mark Wilhelm Drewes, Ulrich Görgens, Tetsuya Murata, Katsuaki Wada, Christian Arnold, Erich Sanwald
  • Publication number: 20130177529
    Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
    Type: Application
    Filed: November 15, 2012
    Publication date: July 11, 2013
    Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
  • Publication number: 20130137865
    Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.
    Type: Application
    Filed: August 11, 2011
    Publication date: May 30, 2013
    Applicant: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
  • Patent number: 8372379
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: February 12, 2013
    Assignee: Mallinckrodt LLC
    Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
  • Publication number: 20120094830
    Abstract: The present invention relates to new insecticides of the formula (I) in which R1, R2, R3, R4, R5, R6, A, Q and n can have the definitions stated in the description, to a number of processes for preparing them and to their use as active compounds, more particularly to their use as pest control compositions.
    Type: Application
    Filed: December 14, 2011
    Publication date: April 19, 2012
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Bernd ALIG, Rüdiger FISCHER, Christian FUNKE, Ernst Rudolf F. GESING, Achim HENSE, Olga MALSAM, Mark Wilhelm DREWES, Ulrich GÖRGENS, Tetsuya MURATA, Katsuaki WADA, Christian ARNOLD, Erich SANWALD
  • Publication number: 20120088783
    Abstract: The invention relates to novel chroman derivatives, stereoisomers and pharmaceutically acceptable salts of Formula I wherein the substituents are as defined in the specification. They are useful in the treatment of disorders mediated by lipoxygenase, such as immune diseases, respiratory diseases and cardiovascular diseases, as well as in the treatment of neurodegenerative disorders and/or mitochondria) disorders. They are also useful in the manufacture of pharmaceutical formulations for the treatment of such conditions.
    Type: Application
    Filed: September 26, 2011
    Publication date: April 12, 2012
    Applicant: Ampere Life Sciences, Inc.
    Inventors: Bing WANG, Gail Walkinshaw, Donald R. James
  • Publication number: 20120029192
    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: Application
    Filed: October 7, 2011
    Publication date: February 2, 2012
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Publication number: 20120029204
    Abstract: The present invention discloses a process of preparing compound of formula (I): wherein A, M, and Z are as defined herein. An example of a compound of formula (I) is 3-amino-1-methyl-1H-1?H-4,4?-bispyrazole.
    Type: Application
    Filed: June 4, 2008
    Publication date: February 2, 2012
    Applicant: Schering Corporation
    Inventors: Carmen S. Alvarez, Michael P. Dwyer, Timothy J. Guzi, Kartik M. Keertikar, Marc A. Labroli, Kamil Paruch, Cory Seth Poker
  • Patent number: 8063044
    Abstract: This invention relates to pyrazole derivatives of formula (I) or pharmaceutically acceptable salts, solvates or derivative thereofs, 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: August 25, 2008
    Date of Patent: November 22, 2011
    Assignee: Pfizer Inc.
    Inventors: Lyn Howard Jones, Charles Eric Mowbray, David Anthony Price, Matthew Duncan Selby, Paul Anthony Stupple
  • Patent number: 8053458
    Abstract: The present invention is directed to dipyrazole compounds of formula I and their pharmaceutically acceptable salts, stereoisomers, tautomers, or solvates thereof. Novel compounds include those of formula I. The compounds of this invention modulate AMPA and NMDA receptor function, and therefore are useful as pharmaceutical agents, especially for the treatment of neuropsychiatric disorders.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: November 8, 2011
    Assignee: Aventis Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Douglas MacDonald, Rosy Sher
  • Publication number: 20110257014
    Abstract: The invention provides compounds of the formula (I) and salts thereof which are described herein. The compounds (I) or salts thereof are suitable for use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants, and can be prepared by the described processes.
    Type: Application
    Filed: December 14, 2010
    Publication date: October 20, 2011
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Harald Jakobi, Arianna Martelletti, Jan Dittgen, Dieter Feucht, Isolde H?user-Hahn, Christopher Hugh Rosinger
  • Publication number: 20110245262
    Abstract: Disclosed are compounds and methods of using compounds of the invention for treating a subject with a proliferative disorder, such as cancer, and methods for treating disorders responsive to Hsp70 induction and/or natural killer induction. Also, disclosed are pharmaceutical compositions comprising compounds of the invention and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: August 20, 2007
    Publication date: October 6, 2011
    Inventors: Lijun Sun, Keizo Koya, Shoujun Chen, Zachary Demko, Zhi-Qiang Xia
  • Publication number: 20110245157
    Abstract: This invention provides for dimeric1-arylpyrazole compounds, of formulas (I), (II), and (III): or salts thereof, and the use of these compounds against ectoparasites such as insects, arthropods and acarina. The resulting compounds may be used in veterinary formulations such as, for example, spot-on and pour-on formulations, which may be used for treatment, controlling and preventing of parasitic infections in warm-blooded animals and birds.
    Type: Application
    Filed: November 18, 2009
    Publication date: October 6, 2011
    Inventor: Charles Q. Meng
  • Publication number: 20110129455
    Abstract: Invented are novel pyrrole compounds, the use of such compounds as inhibitors of protein kinase B activity and in the treatment of cancer and arthritis.
    Type: Application
    Filed: June 24, 2009
    Publication date: June 2, 2011
    Inventors: Hong Lin, Meagan B. Rouse, Mark A. Seefeld, Dennis S. Yamashita, Ren Xie
  • Publication number: 20110098236
    Abstract: Methods of inhibiting cytochrome P450 enzymes are provided that can be used for improving the treatment of diseases by preventing degradation of drugs or other molecules by cytochrome P450. Pharmaceutical compositions are provided that can act as boosters to improve the pharmacokinetics, enhance the bioavailability, and enhance the therapeutic effect of drugs that undergo in vivo degradation by cytochrome P450 enzymes.
    Type: Application
    Filed: February 23, 2009
    Publication date: April 28, 2011
    Applicant: Sequoia Pharmaceuticals, Inc.
    Inventors: Michael Eissenstat, Dehui Duan
  • Patent number: 7888515
    Abstract: The present invention relates to an improved process for preparing N,N?-carbonyldiazoles by reacting azoles with phosgene.
    Type: Grant
    Filed: December 7, 2004
    Date of Patent: February 15, 2011
    Assignee: Saltigo GmbH
    Inventors: Andreas Job, Bernd Griehsel, Johannes Scherer
  • Publication number: 20100280036
    Abstract: The present invention relates to the use of compounds of the general Formula (I): wherein in Formula (I), R is H, alkyl, cycloalkyl, aryl or heteroaryl; R1 is H, alkyl, cycloalkyl, aryl or heteroaryl; R2 is H, alkyl, cycloalkyl, aryl or heteroaryl; A1 and A2 each independently represent an optionally substituted C1-C20-alkyl group which may contain one or more group(s) Z, or a monocyclic or polycyclic optionally substituted aromatic or non-aromatic ring system which may contain one or more group(s) X, and in case of a polycyclic ring system, said system contains at least one aromatic ring; Z is selected from the group consisting of S, O, N, NR4, CO, CO2, CS, SO or SO2 X is selected from the group consisting of S, O, N, NR4, SO or SO2;
    Type: Application
    Filed: December 28, 2007
    Publication date: November 4, 2010
    Inventors: Aldo Ammendola, Katharina Aulinger-Fuchs, Astrid Gotschlich, Bernd Kramer, Martin Lang, Wael Saeb, Udo Sinks, Andreas Wuzik
  • Publication number: 20100227846
    Abstract: The present invention provides a novel pyrazole derivative and an androgen receptor antagonist containing the derivative. The present invention provides a compound represented by the formula (I?) wherein R1 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R2 is a phenyl group having cyano (the phenyl group may further have substituent(s) other than cyano); R3 is a hydrogen atom, a group via a carbon atom, a group via a nitrogen atom, a group via an oxygen atom, or a group via a sulfur atom; R4 is a cyclic group optionally having substituent(s); and X is methylene optionally having substituent(s), or CO, or a salt thereof.
    Type: Application
    Filed: August 27, 2008
    Publication date: September 9, 2010
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Mitsuhiro Ito, Tomohiko Suzaki, Satoshi Tamamoto
  • Publication number: 20100160324
    Abstract: The invention provides a compound of the formula (I): for use in medicine: or salts or tautomers or N-oxides or solvates thereof; wherein R1 is an optionally substituted heterocyclic group having from 3 to 12 ring members provided that the cyclic group joined to the pyrazole contains at least one heteroatom selected from N, O or S; A is a bond or —Y—(B)n—; B is C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; n is 0 or 1; Y is a bond or an alkylene chain of 1,2 or 3 carbon atoms in length; R2 is hydrogen; halogen; C1-4 alkoxy (e.g. methoxy); or a C1-4 hydrocarbyl group optionally substituted by halogen (e.g. fluorine), hydroxyl or C1-4 alkoxy (e.g. methoxy); R3 is selected from optionally substituted carbocyclic and heterocyclic groups having from 3 to 12 ring members or an optionally substituted C1-8 hydrocarbyl group; with the proviso that R1 is not formula (II): where X, R3? and R4? are defined in the claims.
    Type: Application
    Filed: December 30, 2005
    Publication date: June 24, 2010
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Valerio Berdini, Michael Alistair O'Brien, Maria Grazia Carr, Nicholas Gareth Morse Davies, Adrian Liam Gill, Eva Figueroa Navarro, Steven Howard, Gary Trewartha, Andrew James Woodhead, Alison Jo-Anne Woolford, Paul Graham Wyatt
  • Patent number: 7728029
    Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, type II diabetes mellitus and metabolic syndrome.
    Type: Grant
    Filed: March 14, 2007
    Date of Patent: June 1, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kevin William Anderson, Nader Fotouhi, Paul Gillespie, Robert Alan Goodnow, Jr., Kevin Richard Guertin, Nancy-Ellen Haynes, Michael Paul Myers, Sherrie Lynn Pietranico-Cole, Lida Qi, Pamela Loreen Rossman, Nathan Robert Scott, Kshitij Chhabilbhai Thakkar, Jefferson Wright Tilley, Qiang Zhang
  • Publication number: 20100105729
    Abstract: Disclosed herein are potent and selective aryl-substituted heterocyclic compounds, useful as inhibitors of phosphodiesterase 4 (PDE4), compositions comprising the same, and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of PDE4 activity are also provided, as well as methods for the treatment of inflammatory diseases and other diseases in which PDE4 or one of its isoforms may play a role.
    Type: Application
    Filed: September 20, 2007
    Publication date: April 29, 2010
    Applicant: KALYPSYS, INC.
    Inventors: Steven P. Govek, Guy Oshiro, Stewart A. Noble, James W. Malecha, Andrew K. Shiau
  • Publication number: 20100074842
    Abstract: Chelators of the formulae (I), (II) and (III) and tricarbonyl complexes of radioisotopes of Tc and Re bound to them, for use in myocardial imaging.
    Type: Application
    Filed: November 23, 2007
    Publication date: March 25, 2010
    Inventors: Isabel Rego Santos, Antonio Manuel Rocha Paulo
  • Publication number: 20090143454
    Abstract: The present invention relates to novel pyrazoline derivatives of the formula (I) in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these substances, and to their use for controlling pests, and further relates to novel intermediates and processes for their preparation.
    Type: Application
    Filed: July 8, 2002
    Publication date: June 4, 2009
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Fritz Maurer, Rainer Fuchs, Christoph Erdelen, Angelika Lubos-Erdelen, Udo Reckmann, Andreas Turberg
  • Patent number: 7528162
    Abstract: The present invention relates to a group of novel 4,5-dihydro-1H-pyrazole derivatives which are potent cannabinoid (CB1) receptor antagonists with utility for the treatment of diseases connected with disorders of the cannabinoid system. The compounds have the general formula (I) wherein the symbols have the meanings given in the specification. The invention also relates to methods for the preparation of these compounds, and to pharmaceutical compositions containing one or more of these compounds as an active component.
    Type: Grant
    Filed: September 17, 2002
    Date of Patent: May 5, 2009
    Assignee: Solvay Pharmaceuticals, B.V.
    Inventors: Cornelis G. Kruse, Josephus H. M. Lange, Jacobus Tipker, Arnoldus H. J. Herremans, Herman H. Van Stuivenberg
  • Publication number: 20090099209
    Abstract: Compounds of formula (I), or pharmaceutically acceptable derivatives thereof, wherein: R1 represents H, C1-6alkyl, 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; and R9 and R10 independently represent H, C1-6alkyl, C1-6alkyloxy, CN, CF3 or halo; may be useful for treati
    Type: Application
    Filed: December 12, 2008
    Publication date: April 16, 2009
    Inventors: Paul Anthony Bradley, Kevin Neil Dack, Ian Roger Marsh
  • Patent number: 7459415
    Abstract: Embodiments relate to lubricants disposed over magnetic storage media, such as rotatable thin film magnetic discs. One embodiment comprises a lubricant compound of a fluoropolyether chain having one or more carbonyl-imide pairs. For example, the carbonyl-imide pair may be located at one end, both ends, and/or in the middle of the fluoropolyether chain.
    Type: Grant
    Filed: October 13, 2004
    Date of Patent: December 2, 2008
    Assignee: Seagate Technology LLC
    Inventors: Jianwei Liu, Michael Joseph Stirniman, Jing Gui
  • Patent number: 7345080
    Abstract: This invention relates to novel substituted 4-pyrazolylpyrazolines of formula (I) in which R1, R2, R3 and R4 are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling pests, and to novel intermediates and processes for their preparation.
    Type: Grant
    Filed: February 23, 2003
    Date of Patent: March 18, 2008
    Assignee: Bayer CropScience AG
    Inventors: Fritz Maurer, Rainer Fuchs, Angelika Lubos-Erdelen, legal representative, Jörg Konze, Andreas Turberg, Christoph Erdelen
  • Publication number: 20070232648
    Abstract: Novel non-steroidal compounds are provided which are glucocorticoid receptor modulators which are useful in treating diseases requiring glucocorticoid receptor agonist or antagonist therapy such as obesity, diabetes, inflammatory and immune disorders, and have the structure where A, B, and R1-R3 are defined herein.
    Type: Application
    Filed: March 30, 2007
    Publication date: October 4, 2007
    Inventors: Russell Dahl, Sara Sabine Hadida-Ruah, Leslie A. Robinson
  • Patent number: 7232896
    Abstract: A colorant for ocular lenses represented by the formula (I) defined herein or a colorant for ocular lenses represented by the formula (II) defined herein.
    Type: Grant
    Filed: November 10, 2005
    Date of Patent: June 19, 2007
    Assignee: Nidek Co., Ltd.
    Inventors: Sadao Miki, Masaki Kuwahara, Yoshihiro Nakahata, Tsutomu Sunada
  • Patent number: 7102012
    Abstract: A process is provided for preparing N,N?-carbonyldiazoles by reacting azoles with phosgene in halogenated aliphatic hydrocarbon solvents, the entirety of the azole for reaction being introduced in the solvent, followed by the addition of phosgene.
    Type: Grant
    Filed: May 11, 2005
    Date of Patent: September 5, 2006
    Assignee: LANXESS Deutschland GmbH
    Inventors: Andreas Job, Bernd Griehsel
  • Patent number: 7060718
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: March 11, 2003
    Date of Patent: June 13, 2006
    Assignee: Amgen Inc.
    Inventor: Jonathan B. Houze
  • Patent number: 7041669
    Abstract: Disclosed are 1,4-disubstituted benzo-fused urea compounds of formula (I): wherein Ar, X, A, L, and Q of formula(I) are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.
    Type: Grant
    Filed: February 19, 2003
    Date of Patent: May 9, 2006
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Pier Francesco Cirillo, Abdelhakim Hammach, John Robinson Regan
  • Patent number: 6949580
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: October 16, 2003
    Date of Patent: September 27, 2005
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Hale, James Janetka, Francois Maltais
  • Patent number: 6784195
    Abstract: Described herein are compounds that are useful as protein kinase inhibitors having the formula: where R1, R2, T and Ht are described in the specification. The compounds are useful for treating disease states in mammals that are alleviated by a protein kinase inhibitor, particularly diseases such as cancer, inflammatory disorders, restenosis, and cardiovascular disease.
    Type: Grant
    Filed: October 5, 2001
    Date of Patent: August 31, 2004
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael Hale, James Janetka, Francois Maltais, Jingrong Cao
  • Patent number: 6716257
    Abstract: The new diaminopyrazole compounds are bridged 4,5-diaminopyrazole compounds or salts thereof.
    Type: Grant
    Filed: December 14, 2001
    Date of Patent: April 6, 2004
    Assignee: Wella Aktiengesellschaft
    Inventors: Otto Goettel, Aline Pirrello, André Hayoz, Emmanuel Morand
  • Publication number: 20040034234
    Abstract: A process for the preparation of a compound of formula (I) 1
    Type: Application
    Filed: July 3, 2003
    Publication date: February 19, 2004
    Inventors: Jean-Louis Clavel, Isabelle Pelta, Sylvie Le Bars, Philippe Charreau
  • Patent number: 6583165
    Abstract: The invention provides compounds, compositions and methods relating to novel arylsulfonanilide derivatives and their use as pharmacologically active agents. The compositions find particular use as pharmacological agents in the treatment of disease states, particularly cancer, psoriasis, vascular restenosis, infections, atherosclerosis and hypercholesterolemia, or as lead compounds for the development of such agents.
    Type: Grant
    Filed: February 21, 2001
    Date of Patent: June 24, 2003
    Assignee: Tularik Inc.
    Inventor: Jonathan B. Houze
  • Publication number: 20030018051
    Abstract: The present invention relates to certain pyrazole derivatives of Formula (I): 1
    Type: Application
    Filed: February 1, 2002
    Publication date: January 23, 2003
    Inventors: David Michael Goldstein, Sharada Shenvi Labadie, David Mark Rotstein, Eric Brian Sjorgren, Francisco Xavier Talamas