Chalcogen Attached Directly To The 1,2-diazole Ring By Nonionic Bonding Patents (Class 546/276.1)
  • Publication number: 20110033417
    Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.
    Type: Application
    Filed: August 27, 2008
    Publication date: February 10, 2011
    Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
  • Publication number: 20110009622
    Abstract: [Problem] To provide compounds useful as preventives or remedies for circular system disorders, nervous system disorders, metabolic disorders, reproduction system disorders, digestive system disorders, neoplasm, infectious diseases, etc., or as herbicides. [Means for Solution] A long-chain fatty acyl elongase inhibitor comprising, as the active ingredient thereof, a compound or a pharmaceutically-active salt thereof of a formula (I): [wherein W represents a hydrogen atom, a C1-6 alkyl, etc.; X represents an aryl, a heteroaryl, etc.; n indicates 0 or 1; Z represents a hydrogen atom, a C1-6 alkyl, etc.; A1, A2, A3 and A4 each independently represent CH or N].
    Type: Application
    Filed: April 17, 2009
    Publication date: January 13, 2011
    Inventors: Makoto Jitsuoka, Tsuyoshi Nagase, Nagaaki Sato, Daisuke Tsukahara
  • Publication number: 20110003851
    Abstract: The present embodiments relate to compounds with physiological effects, such as the activation of hematopoietic growth factor receptors. The present embodiments also relate to use of the compounds to treat a variety of conditions, diseases and ailments such as hematopoietic conditions and disorders.
    Type: Application
    Filed: May 6, 2010
    Publication date: January 6, 2011
    Applicant: Ligand Pharmaceuticals, Inc.
    Inventors: Lin Zhi, Andrew R. Hudson, Cornelis A. Van Oeveren, Steven L. Roach, Jason C. Pickens, Yixing Shen, Catalina Cuervo, Lino J. Valdez, Jillian Basinger, Virgina H. Grant
  • Publication number: 20100305085
    Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.
    Type: Application
    Filed: October 12, 2007
    Publication date: December 2, 2010
    Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFT
    Inventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
  • Publication number: 20100298141
    Abstract: Disclosed are compounds of Formula 1, including N-oxides, and salts thereof, wherein W is O or NR7, n is 0 or 1, and R1, R2, R3, R4, R5, R6, R7 and m are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention. Also disclosed are mixtures and compositions comprising a herbicidally effective amount of a compound of Formula 1 and an effective amount of another herbicide or herbicide safener.
    Type: Application
    Filed: February 8, 2008
    Publication date: November 25, 2010
    Applicant: E. I. DU PONT DE NEMOURS AND COMPANY
    Inventors: Thomas Paul Selby, Brenton Todd Smith, Thomas Martin Stevenson
  • Patent number: 7834186
    Abstract: A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II) wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl.
    Type: Grant
    Filed: September 19, 2008
    Date of Patent: November 16, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Publication number: 20100280251
    Abstract: Disclosed is a method for preparing a compound of Formula 1 comprising contacting a compound of Formula 2 with a metal cyanide reagent, a copper(I) salt reagent, an iodide salt reagent and at least one compound of Formula 3 wherein R1 is NHR3 or OR4; R2 is CH3 or Cl; R3 is H, C1-C4 alkyl, cyclopropyl, cyclopropylcyclopropyl, cyclopropylmethyl or methylcyclopropyl; R4 is H or C1-C4 alkyl; Y is Br or Cl; X is NR13 or O; n is 0 or 1; and R5, R6, R7, R8, R9, R10, R11, R12 and R13 are as defined in the disclosure. Also disclosed is a method for preparing a compound of Formula 2 wherein Y is Br and R1 is NHR3 comprising introducing a gas containing bromine into a liquid containing a compound of Formula 4, and further disclosed is a method for preparing a compound of Formula 5 wherein R14, R15, R16 and Z are as defined in the disclosure using a compound of Formula 1 characterized by preparing the compound of Formula 1 by the method disclosed above.
    Type: Application
    Filed: December 18, 2007
    Publication date: November 4, 2010
    Applicant: E.I. Du Pont De Nemours and Company
    Inventors: Joerg Bruening, Gary David Annis, Martin James Currie, Donald J. Dumas, Rafael Shapiro
  • Publication number: 20100273830
    Abstract: An insecticidal compound of formula (I) in which G1, G2, and G3 together with the two carbon atoms to which G1 and G3 are attached, form a non-aromatic 4- or 5-membered ring system; wherein G1 is sulfur, SO, SO2, oxygen, a direct bond, NRa or CR5aR5b; G2 is sulfur, SO, SO2, oxygen, a direct bond, NRb or CR5cR5d; G3 is sulfur, SO, SO2, oxygen, a direct bond, NRc or CR5eR5f; with the provisos that a) not more than 1 group G can be a direct bond, b) not more than 2 G groups can be oxygen, sulfur, SO or SO2 and c) when 2 G groups are oxygen, SO, SO2 and/or sulfur the two groups are separated by a carbon atom; each of Z1 and Z2, which may be the same or different, represents oxygen or sulfur; D is phenyl or a 5- or 6-membered heteroaromatic ring and R1a, R1b, R5a, R5b, R5c, R5d, R5e, R5f, Ra, Rb Rc, R2, R3 and R20 are specified organic groups and agronomically acceptable salts/isomers/enantiomers/tautomers/N-oxides of those compounds.
    Type: Application
    Filed: July 14, 2008
    Publication date: October 28, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Roger Graham Hall, Olivier Loiseleur, Jagadish Pabba, Sitaram Pal, Andre Jeanguenat, Andrew Edmunds, Andre Stoller
  • Publication number: 20100256192
    Abstract: In one aspect, the invention relates to compounds which are useful as as inhibitors of glycine type 1 transporter (GlyT1) activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders associated with glycine type 1 transporter (GlyT1) activity using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Application
    Filed: December 29, 2009
    Publication date: October 7, 2010
    Inventors: Craig W. Lindsley, P. Jeffrey Conn, Richard Williams, Carrie K. Jones, Douglas J. Sheffler
  • Publication number: 20100222592
    Abstract: A pyridone derivative represented by Formula [1] or an agriculturally acceptable salt thereof: wherein R1 is a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group, or the like; R2 and R3 are each independently a hydrogen atom, a nitro group, a cyano group, or the like; and A is a group represented by Formula A-1, Formula A-2, Formula A-3, Formula A-4, or Formula A-5: The compounds represented by general formula [1] control various weeds growing in upland fields, orchards, paddy fields, and non-crop lands while showing high safety to useful plants and crops.
    Type: Application
    Filed: January 31, 2007
    Publication date: September 2, 2010
    Applicants: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Fumiaki Takabe, Shunichirou Fukumoto, Ryu Kajiki, Sohei Asakura, Ryohei Ueno, Masami Kobayashi, Satoru Takahashi, Norihisa Yonekura, Ryo Hanai, Takashi Mitsunari
  • Patent number: 7759381
    Abstract: Provided are 1-aryl-5-alkyl pyrazole compounds, of formula (I): wherein: R1 is hydrogen, cyano, halogen, R8, formyl, —C(O)R8, —C(O)OR8, —C(O)NR9R10, or —C(S)NH2; R2 is R8 or —S(O)mR11; R3 is methyl, ethyl or C1-C4 haloalkyl; R4, R5 and R7 are independently hydrogen, halogen, alkyl, haloalkyl, cyano or nitro; R6 is halogen, alkyl, haloalkyl, alkoxy, haloalkyloxy, cyano, nitro, —C(O)R12, —S(O)nR12 or SF5; Z is a nitrogen atom or C—R13; R8 is alkyl, haloalkyl, cycloalkyl or halocycloalkyl; R9 is hydrogen, alkyl, haloalkyl or alkoxy; R10 is hydrogen, alkyl, haloalkyl or alkoxy; R11 is alkyl, haloalkyl, alkenyl, haloalkenyl, alkynyl, haloalkynyl or cycloalkyl; R12 is alkyl or haloalkyl; R13 is hydrogen, halogen, cyano, nitro, alkyl, haloalkyl, alkoxy or haloalkoxy; m is 0, 1 or 2; and n is 0, 1 or 2; or a salt thereof, the method of making compounds of formula (I) and the use of these compounds against ectoparasites, endoparasites and pests.
    Type: Grant
    Filed: July 3, 2007
    Date of Patent: July 20, 2010
    Assignee: Aventis Agriculture
    Inventors: Hyoung Ik Lee, Loïc Patrick Le Hir de Fallois, Philip Reid Timmons, William Glenn Cawthorne, Jr., Adalberto Perez de Leon
  • Publication number: 20100179161
    Abstract: Compounds of the formula (I) and pharmaceutically acceptable salts or in vivo hydrolysable esters thereof, useful in the treatment of Mycobacterium tuberculosis (M.tb).
    Type: Application
    Filed: August 16, 2006
    Publication date: July 15, 2010
    Applicant: ASTRAZENECA AB
    Inventors: Balachandra Shankar Bandodkar, Stefan Schmitt
  • 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
  • Patent number: 7723363
    Abstract: A compound of general formula (I). A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: May 25, 2010
    Assignee: Bayer Cropscience SA
    Inventors: Darren James Mansfield, Heiko Rieck, Pierre-Yves Coqueron, Philippe Desbordes, Marie-Claire Grosjean-Cournoyer, Pierre Genix, Alain Villier
  • Publication number: 20100063063
    Abstract: The present invention provides Formula (1A) compounds that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. X, Y, Z, R1, R2, R3, and R4 are as described herein.
    Type: Application
    Filed: September 9, 2009
    Publication date: March 11, 2010
    Inventors: John William Benbow, Jihong Lou, Jeffrey Allen Pfefferkorn, Meihua Mike Tu
  • Patent number: 7666882
    Abstract: This invention provides compounds of Formula I, N-oxides and suitable salts thereof wherein Y and V are each independently N or CR4a; W is N, CH or CR6; and R1 through R6, and n are as defined in the disclosure. This invention also pertains to a composition for controlling an invertebrate pest comprising a biologically effective amount of a compound of Formula I, an N-oxide thereof or an agronomic or nonagronomic suitable salt of the compound and at least one additional component selected from the group consisting of a surfactant, a solid diluent and a liquid diluent, and optionally further comprising an effective amount of at least one additional biologically active compound or agent. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I, an N-oxide thereof or an agronomic or nonagronomic suitable salt of the compound or with the composition described herein.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: February 23, 2010
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: George Philip Lahm
  • Patent number: 7659288
    Abstract: The invention relates to 5-aminoalkylaminopyrazole derivatives of formula (I) or salts thereof: wherein the various symbols are as defined in the description, to processes for their preparation, to compositions thereof, and to their use for the control of pests (including arthropods and helminths).
    Type: Grant
    Filed: September 22, 2006
    Date of Patent: February 9, 2010
    Assignee: Merial Limited
    Inventors: Stefan Schnatterer, David Teh-Wei Chou, Werner Knauf, Daniela Jans, Karl Seeger
  • Publication number: 20100022503
    Abstract: The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof. The formula (I) compounds inhibit tyrosine kinase activity thereby making them useful as anticancer agents.
    Type: Application
    Filed: January 4, 2008
    Publication date: January 28, 2010
    Inventors: Marco Dodier, Claude A. Quesnelle, Anne Marinier
  • Patent number: 7638514
    Abstract: There are described compounds of formula (I) wherein X1 and X2 are each independently of the other fluorine, chlorine or bromine; A1 and A2 are, for example, a bond or a C1-C6alkylene bridge; A3 is a C1-C6alkylene bridge; R1 and R2 are, for example, halogen, OH, SH, CN, nitro, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkyl-carbonyl, C2-C6alkenyl, C2-C6haloalkenyl or C3-C6alkynyl; R,3 is, for example, H, halogen, OH, SH, CN, nitro, C1-C6alkyl or C1-C6haloalkyl; R4 and R5 are, for example, H, halogen, cyano, nitro, C1-C6alkyl or C1-C3haloalkyl; m is 1 or 2; Y is, for example, O, S, SO or SO2; Q is, for example, O, S, SO or SO2; W is, for example, a bond, O, S, SO, S02, —C(?O)—O— or —O—C(?O)—; T is, for example, a bond, O, S, SO, SO2, —C(?O)—O— or —O—C(?O)—; and E is aryl unsubstituted or substituted from one to five times or heterocyclyl unsubstituted or, depending upon the possibilities of substitution on the ring, substituted from one to four times; and, where applicable, their possible E/Z isomers, E/Z isomeric mixt
    Type: Grant
    Filed: August 25, 2004
    Date of Patent: December 29, 2009
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: Werner Zambach, Stephan Trah, Roger Graham Hall, William Lutz
  • Publication number: 20090253751
    Abstract: Compounds effective for preventing, treatment or improving diseases against which activation of the thrombopoietin receptor is effective are provided. A compound represented by the formula (I) (wherein R1, R2, R3, L1, L2, X and Y are defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: November 7, 2006
    Publication date: October 8, 2009
    Applicant: Nissan Chemical Industries, Ltd.
    Inventors: Katsuaki Miyaji, Yukihiro Shigeta, Satoshi Nakano, Hirofumi Ota, Norihisa Ishiwata
  • Publication number: 20090227592
    Abstract: The invention relates to the use of a compound of Formula (I) or a salt, solvate or prodrug thereof, wherein R1, R2, R3, n and m are as described in the specification, in the preparation of a medicament for the treatment or prevention of a disease condition mediated through glucokinase (GLK), such as type 2 diabetes. The invention also relates to a novel group of compounds of Formula (I) and to methods for preparing compounds of Formula (I).
    Type: Application
    Filed: February 2, 2009
    Publication date: September 10, 2009
    Applicant: AstraZeneca AB
    Inventors: Scott BOYD, Peter William Rodney CAULKETT, Rodney Brian HARGREAVES, Suzanne Saxon BOWKER, Roger JAMES, Clifford David JONES, Darren McKERRECHER, Michael Howard BLOCK, Craig JOHNSTONE
  • Patent number: 7576107
    Abstract: The invention relates to the use for the control of pests, of a compound which is a 5-substituted-alkylaminopyrazole derivative of formula (I) or a salt thereof: wherein the various symbols are as defined in the description, to novel 5-substituted-alkylaminopyrazole derivatives and pesticidal compositions thereof, and to processes for their preparation.
    Type: Grant
    Filed: February 27, 2003
    Date of Patent: August 18, 2009
    Assignee: Merial Limited
    Inventors: David Teh-Wei Chou, Henricus Maria Marinus Bastiaans, Anke Kuhlmann, Maria-Theresia Thönessen, Stefan Schnatterer, Uwe Döller, Jamin Huang, Karl Seeger, Andrew Scribner, Adalberto A. Perez De Leon
  • Publication number: 20090131676
    Abstract: A compound represented by the formula (I) (wherein R1, R2, R3 and R4 are as defined in the description), a tautomer, prodrug or pharmaceutically acceptable salt of the compound or a solvate thereof.
    Type: Application
    Filed: July 19, 2006
    Publication date: May 21, 2009
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Katsuaki Miyaji, Yutaka Hirokawa, Masato Horikawa, Norihisa Ishiwata
  • 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: 7514561
    Abstract: Substituted-acylaminopyrazole derivatives of formula (I): or salts thereof, wherein the various symbols are as defined in the description, processes for their preparation, compositions thereof and methods for their use for the control of pests, such as arthropods (e.g. insects and arachnids) and helminths (including nematodes).
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: April 7, 2009
    Assignee: Merial Limited
    Inventors: Stefan Schnatterer, David William Hawkins, Daniela Jans, Michael Maier, Anke Kuhlmann, Erich Friedrich Sanwald, Maria-Theresia Thönessen, Karl Seeger
  • Publication number: 20090074373
    Abstract: The present invention provides optical filters comprising a squarylium compound represented by General Formula (I): [wherein R1 and R2 may be the same or different and each represents a hydrogen atom, an alkyl group optionally having substituent(s) or the like, R3 represents a hydrogen atom or an alkyl group optionally having substituent(s), and Y represents a group represented by General Formula (A): (wherein R4 represents a hydrogen atom, an alkyl group optionally having substituent(s) or the like, R5 represents a hydrogen atom, a halogen atom or the like, and R6, R7, R8 and R9 may be the same or different and each represents a hydrogen atom, a halogen atom, an alkyl group optionally having substituent(s) or the like)] and the like.
    Type: Application
    Filed: November 18, 2005
    Publication date: March 19, 2009
    Applicant: KYOWA HAKKO CHEMICAL CO., LTD.
    Inventors: Junzo Yamano, Katsumi Ukai, Motoharu Kinugasa
  • Publication number: 20090048256
    Abstract: The present invention relates to a pyrazole compound having potent CB1-antagonizing activity, having the following formula [I]: wherein R1 and R2 are the same or different and an optionally substituted aryl group etc., R3 is an alkyl group etc., E is one of the following groups of the formula (i) to (iv): Q1 is a single bond, an alkylene group or a group of the formula: —N(R7)—, R7 is a hydrogen atom or an alkyl group, Q2 is a single bond, an oxygen atom or an alkylene group, R4 is a cycloalkyl group, a group of the formula: —N(R5)(R6) etc., one of R5 and R6 is a hydrogen atom or an alkyl group and the other is an alkyl group, a group of the formula: —N(R8)(R9) etc., D is an oxygen atom etc., RA1 is an amino group etc., RA2 is an optionally substituted aliphatic heterocyclic group, R is an alkyl group optionally substituted by one to three halogen atom(s) etc., one of R8 and R9 is a hydrogen atom or an alkyl group and the other is an alkyl group etc.
    Type: Application
    Filed: October 20, 2006
    Publication date: February 19, 2009
    Inventors: Yasunori Moritani, Ritsuo Imashiro, Atsushi Sato
  • Patent number: 7488824
    Abstract: The present invention relates to a process for the preparation of compounds of formula (I) wherein the substituents are as defined in claim 1, by reaction of a compound of formula (II) wherein R3 is C1-C8alkyl or C3-C6cycloalkyl and R4 and R05 are as defined for formula (I), with a compound of formula (III) wherein R, R1, R2 and X1, are as defined for formula (I) in claim 1, in an inert solvent in the presence of a proton source.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: February 10, 2009
    Assignee: Syngenta Crop Protection, Inc.
    Inventors: David Anthony Jackson, Martin Charles Bowden
  • Patent number: 7452873
    Abstract: The present invention relates to compounds of formula I that are useful as GSK-3 inhibitors. The invention also relates to methods of using compounds of formula I or pharmaceutical compositions comprising compounds of formula I to inhibit GSK-3 activity. The invention further provides methods of utilizing these compounds and pharmaceutical compositions in the treatment and prevention of various disorders, such as diabetes and Alzheimer's disease. The invention also relates to methods for inhibiting Aurora-2 activity and for treating or preventing Aurora-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I. The invention also relates to methods for inhibiting cyclin-dependent kinase-2 activity and for treating or preventing inhibiting cyclin-dependent kinase-2-mediated diseases using compounds of formula I or pharmaceutical compositions comprising compounds of formula I.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: November 18, 2008
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Jeremy Green, Michael J. Arnost, Albert Pierce
  • Patent number: 7452874
    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: January 8, 2007
    Date of Patent: November 18, 2008
    Assignee: SmithKline Beecham Corp.
    Inventors: Kevin J. Duffy, Juan I. Luengo, Antony N. Shaw, Kenneth Wiggall
  • 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: 20080269293
    Abstract: This invention relates to novel compounds of formula (I) or stereoisomers or pharmaceutically acceptable salts thereof wherein Y, R1 through R9, and X1 through X7 are as defined in the specification, pharmaceutical compositions containing said compounds useful as P2Y1 antagonists, and to methods of treating thromboembolic disorders.
    Type: Application
    Filed: August 22, 2007
    Publication date: October 30, 2008
    Inventors: Liguo Chi, Chulho Choi, Andrew G. Geyer, Robert M. Kennedy, Jeffery A. Pfefferkorn, Roy T. Winters
  • Publication number: 20080263787
    Abstract: The present application relates to cationic pyrazolone dyes of the general formula (I), and to coloring agents for keratin fibers comprising these dyes.
    Type: Application
    Filed: May 18, 2005
    Publication date: October 30, 2008
    Inventors: Markus Speckbacher, Hans-Juergen Braun
  • Patent number: 7442702
    Abstract: This invention relates to prostaglandin agonists, methods of using such prostaglandin agonists, pharmaceutical compositions containing such prostaglandin agonists and kits containing such prostaglandin agonists. The prostaglandin agonists are useful for the treatment of bone disorders including osteoporosis.
    Type: Grant
    Filed: September 25, 2002
    Date of Patent: October 28, 2008
    Assignee: Pfizer Inc.
    Inventors: Kimberly O. Cameron, Bruce A. Lefker, Robert L. Rosati
  • Patent number: 7442799
    Abstract: A method is disclosed for preparing a 2-substituted-5-oxo-3-pyrazolidinecarboxylate compound of Formula I. The method comprises contacting a succinic acid derivative of the formula R1OC(O)C(H)(X)C(R2a)(R2b)C(O)Y (i.e. Formula II)wherein X and Y are leaving groups and L, R1, R2a and R2b are as defined in the disclosure, with a substituted hydrazine of the formula LNHNH2 (i.e. Formula III) in the presence of a suitable acid scavenger and solvent. Also disclosed is the preparation of compounds of Formula IV wherein X1, R6, R7, R8a, R8b, R9, and n are as defined in the disclosure. Also disclosed is a composition comprising on a weight basis about 20 to 99% of the compound of Formula II wherein R1, R2a, R2b, R3, R4 and R5 are as defined in the disclosure; X is Cl, Br or I; and Y is F, Cl, Br or I; provided that when R2a and R2b are each H, and X and Y are each Cl then R1 is other than benzyl and when R2a and R2b are each phenyl, and X and Y are each Cl, then R1 is other than methyl or ethyl.
    Type: Grant
    Filed: March 25, 2004
    Date of Patent: October 28, 2008
    Assignee: E.I. du Pont de Nemours and Company
    Inventor: Gary David Annis
  • Publication number: 20080167322
    Abstract: Substituted pyrazole compounds such compounds represented by formula I: which are used to modulate the CCR-2 chemokine receptor to prevent or treat inflammatory and immunoregulatory disorders and diseases, allergic diseases, atopic conditions including allergic rhinitis, dermatitis, conjunctivitis, and asthma, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis; and pharmaceutical compositions comprising these compounds and the use of these compounds and compositions.
    Type: Application
    Filed: February 14, 2006
    Publication date: July 10, 2008
    Inventors: Anthony B. Pinkerton, Rowena Cube, John Hutchinson, Dehua Huang, Jean-Michel Vernier, Dong-Ming Shen
  • Patent number: 7390907
    Abstract: Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritus, vitiligo, general gastrointestinal disorders, gastric ulceration, d
    Type: Grant
    Filed: September 30, 2004
    Date of Patent: June 24, 2008
    Assignee: Amgen Inc.
    Inventors: Ning Chen, Thomas Nixey, Mark H. Norman
  • 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
  • Publication number: 20080064682
    Abstract: A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitr
    Type: Application
    Filed: July 1, 2005
    Publication date: March 13, 2008
    Applicant: DAIICHI PHARMACEUTICAL CO., LTD.
    Inventors: Naoaki Kanaya, Takashi Ishiyama, Ryo Muto, Toshiyuki Watanabe, Yuichi Ochiai
  • Patent number: 7335649
    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: November 9, 2006
    Date of Patent: February 26, 2008
    Assignee: SmithKline Beecham Corporation
    Inventors: Kevin J. Duffy, Connie Erickson-Miller, Julian Jenkins, Juan I. Luengo, Sophie Visonneau
  • Patent number: 7253290
    Abstract: The invention relates to a group of novel thieno-pyrrole compounds of Formula (I): wherein: R1, R2, R5, R6, R6a, R7, R8, A, B and M are as defined in the specification, which are useful as gonadotrophin releasing hormone antagonists. The invention also relates to pharmaceutical formulations of said compounds, methods of treatment using said compounds and to processes for the preparation of said compounds.
    Type: Grant
    Filed: August 19, 2003
    Date of Patent: August 7, 2007
    Assignee: AstraZeneca AB
    Inventors: Thomas Geoffrey Bird, Mickael Louis Pierre Maudet
  • Patent number: 7232836
    Abstract: This invention provides compounds of Formula 1, their N-oxides and agriculturally suitable salts wherein R1, R2, R3, R4a, R4b and R5 are as defined in the disclosure. Also disclosed are methods for controlling invertebrate pests comprising contacting the invertebrate pests or their environment with a biologically effective amount of a compound of Formula 1 or a composition comprising a compound of Formula 1.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: June 19, 2007
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: George Philip Lahm, Thomas Paul Selby, Thomas Martin Stevenson
  • Patent number: 7223777
    Abstract: The invention discloses a new clause of a five membered heterocylic ring compounds of general formula I and its pharmaceutically or cosmetically acceptable salts, wherein R1, R2, R3, R4, R5, A, B, X and Y are as defined in the specification. The invention also discloses a process for preparation of these compound and their therapeutic and cosmetic applications particularly in the management of aging related and diabetic vascular complications. The compounds in question act by triple action of an AGE (Advanced Glycation Endproducts) breaker, AGE inhibitor and free radical scavenger which make them most suitable in different therapeutic and cosmetic applications. The invention also discloses pharmaceuticals and cosmetic compositions comprising these compounds and method of treatment of diseases caused by accumulation of AGE and/or free radicals in the body cells.
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: May 29, 2007
    Assignee: Torrent Pharmaceuticals Ltd.
    Inventor: Alangudi Sankaranarayanan
  • Patent number: 7214678
    Abstract: According to the invention there is provided a compound the formula I; wherein A, X, B, R1, R2, R3 and R4 are as defined in the specification.
    Type: Grant
    Filed: June 1, 2006
    Date of Patent: May 8, 2007
    Assignee: Allergan, Inc.
    Inventors: Robert M. Burk, Sophie Beauchemin
  • Patent number: 7199246
    Abstract: A process for the preparation of a compound of general formula (I), wherein R1 is CN or CSNH2; R2 is hydrogen or chloride; and R3 is halogen or haloalkyl or haloalkoxy or SF5 which process comprises reacting a compound of formula (II), where R1, R2 and R3 are as defined above; with a proton source.
    Type: Grant
    Filed: June 7, 2001
    Date of Patent: April 3, 2007
    Assignee: Merial Limited
    Inventor: Jean-François Rousseau
  • Patent number: 7199138
    Abstract: This invention provides compounds of Formula I, N-oxides and salts thereof wherein A, B, R1 through R5, R7 through R9, X and Y are as defined in the disclosure. Also disclosed are methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound of Formula I. Also disclosed are compositions for controlling an invertebrate pest comprising the compounds of Formula I.
    Type: Grant
    Filed: August 13, 2002
    Date of Patent: April 3, 2007
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Bruce Lawrence Finkelstein, George Philip Lahm, Stephen Frederick McCann, Thomas Paul Selby, Ying Song, Thomas Martin Stevenson
  • 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: 7179823
    Abstract: A compound of formula (I) F wherein R1 represents a hydrocarbon group which may be substituted or a heterocyclic group which may be substituted; x represents a bond, an oxygen atom, a sulfur atom, or a group of the formula: —CO—, —CS—, —CR4(OR5)— or —NR6— wherein each of R4 and R6 represents a hydrogen atom or a hydrocarbon group which may be stubstituted, R5 represents a hydrogen atom or a protective group for a hydroxyl group; m represents an integer of 0 to 3; Y represents an oxygen atom, a sulfur atom, or a group of the formula: —SO—, —SO2—, —NR7—, —CONR7— or —NR7CO— wherein R7 represents a hydrogen atom or a hydrocarbon group which may be substituted; ring A represents an aromatic ring which may further have 1 to 3 substituents; n represents an integer of 1 to 8; ring B represents a nitrogen-containing 5-membered hetero ring which may further be substituted by an alkyl group.
    Type: Grant
    Filed: November 9, 2000
    Date of Patent: February 20, 2007
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Yu Momose, Tsuyoshi Maekawa, Hiroyuki Odaka, Hiroyuki Kimura
  • Patent number: 7179824
    Abstract: This invention pertains to a compound of Formula I, its N-oxide or an agriculturally suitable salt of the compound (Formula I) wherein R1, R2, R3, R4, and R5 are as defined in the disclosure.
    Type: Grant
    Filed: September 6, 2002
    Date of Patent: February 20, 2007
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: William Thomas Zimmerman
  • Patent number: 7132435
    Abstract: This invention relates to nicotinamide derivatives of general formula (I): in which R1, X, Y, Z and R2 have the meanings defined herein, and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of such derivatives.
    Type: Grant
    Filed: July 20, 2004
    Date of Patent: November 7, 2006
    Assignee: Pfizer Inc.
    Inventors: Mya Coral Helen Smith, Christine Anne Louise Watson