1,3-thiazoles (including Hydrogenated) Patents (Class 548/146)
  • Publication number: 20110288131
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3 and R4 are as defined in claim 1; or a salt or oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.
    Type: Application
    Filed: January 13, 2010
    Publication date: November 24, 2011
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Myriem El Qacemi, Thomas Pitterna, Jerome Yves Cassayre, Peter Renold
  • Patent number: 8063205
    Abstract: The present invention is a method for producing a 2-oxazoline analogue or a 1,3-oxazine analogue represented by the following general formula (3) by reacting a 1,2-aminoalcohol compound or a 1,2-aminothiol compound with an ?,?-dihaloamine compound. (In the formula, n represents 0 or 1, and R represents an oxygen atom or a sulfur atom. R1, R2 and R3 each represents an atom or a group shown in Group 1 to Group 3, and R0 represents an atom or a group shown in Group 2 or Group 3. Two or more of R1, R2 and R3 may be bonded to each other to form a ring.
    Type: Grant
    Filed: August 30, 2006
    Date of Patent: November 22, 2011
    Assignees: National University Corporation Hokkaido University, Mitsubishi Gas Chemical Company, Inc.
    Inventors: Shoji Hara, Tsuyoshi Fukuhara, Toshio Hidaka
  • Patent number: 8063067
    Abstract: Compounds of the formula (I): in which R, R1, R2 and R3 are as defined in the description, the use thereof for the treatment of dyslipidaemia, atherosclerosis and diabetes, pharmaceutical compositions comprising them, and processes for the preparation of these compounds.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: November 22, 2011
    Assignee: Merck Patent GmbH
    Inventors: Jean Jacques Zeiller, Hervè Dumas, Valérie Guyard-Dangremont, Isabelle Berard, Francis Contard, Daniel Guerrier, Gérard Ferrand, Yves Bonhomme
  • Patent number: 8034954
    Abstract: The present invention provides novel calcium channel antagonists, and methods of treating disease sates using the novel antagonists.
    Type: Grant
    Filed: December 20, 2006
    Date of Patent: October 11, 2011
    Assignee: Icagen, Inc.
    Inventors: Gregory J. Pacofsky, Mark J. Suto, Paul Christopher Fritch
  • Patent number: 8026369
    Abstract: Disclosed herein is a composition containing hetero arylene or arylene showing a p-type semiconductor property in addition to thiophene showing a p-type semiconductor property and thiazole rings showing a n-type semiconductor property at a polymer main chain, an organic semiconductor polymer containing the composition, an organic active layer containing the organic semiconductor polymer, an organic thin film transistor (OTFT) containing the organic active layer, an electronic device containing the OTFT, and a method of preparing the same. The composition of example embodiments, which is used in an organic semiconductor polymer and contains thiazole rings, may exhibit increased solubility to an organic solvent, coplanarity, processibility and an improved thin film property.
    Type: Grant
    Filed: January 9, 2008
    Date of Patent: September 27, 2011
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Bang Lin Lee, Eun Kyung Lee, Joo Young Kim, Kook Min Han
  • Patent number: 8026260
    Abstract: The present invention relates to a novel class of histone deacetylase inhibitors with aryl-pyrazolyl motifs. The compounds of this invention can be used to treat cancer. The compounds of this invention are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The present invention further provides pharmaceutical compositions comprising the compounds of this invention and safe dosing regimens of these pharmaceutical compositions, which are easy to follow, and which result in a therapeutically effective amount of the compounds of this invention in vivo.
    Type: Grant
    Filed: October 30, 2006
    Date of Patent: September 27, 2011
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Joshua Close, Richard W. Heidebrecht, Jr., Solomon Kattar, Thomas A. Miller, David Sloman, Matthew G Stanton, Paul Tempest, David J. Witter
  • Patent number: 8022079
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 18, 2009
    Date of Patent: September 20, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Patent number: 8017608
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: September 13, 2011
    Assignee: Novartis AG
    Inventors: Graham Charles Bloomfield, Ian Bruce, Catherine Leblanc, Mrinalini Sachin Oza, Lewis Whithead, Bernard Cuenoud, Thomas Hugo Keller, Louise Kirman, Clive McCarthy, Gaynor Elizabeth Woodward
  • Patent number: 8008502
    Abstract: The present invention relates to novel thiazoline acids and derivatives thereof useful as chelators of trivalent metals in therapeutic applications. For example, the thiazoline acid derivatives are useful in diagnosing and treating pathological conditions associated with an excess of trivalent metals in humans and animals.
    Type: Grant
    Filed: March 27, 2009
    Date of Patent: August 30, 2011
    Assignee: University of Florida Research Foundation, Inc.
    Inventor: Raymond J. Bergeron
  • Patent number: 8003801
    Abstract: A highly active synthetic epothilone compound whose activity exceeds that of either epothilone EpoA or EpoB when assayed as a cytotoxic agent against a cancer cell line is disclosed as is a pharmaceutical composition containing the synthetic epothilone.
    Type: Grant
    Filed: November 9, 2006
    Date of Patent: August 23, 2011
    Assignee: The Scripps Research Institute
    Inventors: Kyriacos C. Nicolaou, Benjamin Pratt, Stellios Arseniyadis
  • Publication number: 20110202942
    Abstract: An aspect of the present invention relates to an optical information recording medium comprising a recording layer, wherein the recording layer comprises a cationic dye and a polynuclear azo metal complex dye comprising an azo dye and a metal ion, and a method of recording information comprising recording information on the recording layer comprised in the optical recording medium, and conducting the recording by irradiation of a laser beam having a wavelength of equal to or shorter than 440 nm onto the optical information recording medium. Another aspect of the present invention relates to a photo sensitizer.
    Type: Application
    Filed: October 9, 2009
    Publication date: August 18, 2011
    Applicant: FUJIFILM CORPORATION
    Inventors: Taisuke Fujimoto, Kousuke Watanabe, Taro Hashizume
  • Patent number: 7989394
    Abstract: The present invention relates to 1-(azolin-2-yl)-amino-2-aryl-1-hetaryl-ethane compounds (I) and 1-(aminothiocarbonylamino)-2-aryl-1-hetaryl-ethane compounds (II) and their salts which are useful for combating animal pest, in particular insects, arachnids and nematodes. Furthermore, the present invention relates to a method for combating animal pests selected from insects, arachnids and nematodes, and to agricultural compositions for combating animal pests. Furthermore, the present invention relates to veterinary compositions for combating animal pests.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: August 2, 2011
    Assignee: BASF SE
    Inventors: Markus Kordes, Delphine Breuninger, Ronan Le Vezouet, Christopher Koradin, Livio Tedeschi, Michael Puhl, Deborah L. Culbertson
  • Publication number: 20110178142
    Abstract: The present invention provides a pharmaceutical composition comprising 3-{5-[4-Oxo-2-thioxo-3-(3-trifluoromethyl-phenyl)-thiazolidin-5-ylidenemethyl]-furan-2-yl}-benzoic acid or a pharmaceutically acceptable salt thereof and pharmaceutically acceptable excipients for therapeutic or prophylactic treatment of bacterial infections and diseases associated thereof.
    Type: Application
    Filed: October 13, 2009
    Publication date: July 21, 2011
    Applicant: National Institute of Immunology
    Inventors: Avadhesha Surolia, Tushar Beuria Kant, Panda Dulal
  • Patent number: 7977363
    Abstract: Novel biphenyl thiazole carboxamides of Formula (I) where R1, R2, R3, R4, R5 and n have the meanings specified in the description, several methods for the manufacture of these substances and their use for combating undesired microorganisms, as well as novel intermediate products and their manufacture.
    Type: Grant
    Filed: August 13, 2005
    Date of Patent: July 12, 2011
    Assignee: Bayer Cropscience AG
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Jörg Nico Greul, Benoit Hartmann, Herbert Gayer, Thomas Seitz, Ulrike Wachendorff-Neumann, Peter Dahmen, Karl-Heinz Kuck
  • Patent number: 7968560
    Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.
    Type: Grant
    Filed: September 21, 2009
    Date of Patent: June 28, 2011
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
  • Patent number: 7947685
    Abstract: The present invention is concerned with novel pyrazine 2-carboxyamide derivatives of formula (I) wherein R1, R2 and R3 are as defined in the specification. These compounds are useful for the treatment of CNS disorders.
    Type: Grant
    Filed: May 22, 2009
    Date of Patent: May 24, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
  • Patent number: 7947675
    Abstract: Compounds of the formula (I), in which the radicals R1 to R3 and AR are as defined in the description, processes for the preparation thereof, the use thereof in the treatment of cardiovascular diseases, and pharmaceutical compositions comprising them.
    Type: Grant
    Filed: February 16, 2006
    Date of Patent: May 24, 2011
    Assignee: Merck Patent GmbH
    Inventors: Bruno Roux, Isabelle Berard
  • Patent number: 7943788
    Abstract: A compound of the formula: wherein Ring A and Ring B are: (1) Ring A is an optionally substituted unsaturated monocyclic heterocyclic ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring, (2) Ring A is an optionally substituted benzene ring, and Ring B is an optionally substituted unsaturated monocyclic heterocyclic ring or an optionally substituted unsaturated fused heterobicyclic ring, or (3) Ring A is an optionally substituted unsaturated fused heterobicyclic ring, and Ring B are independently an optionally substituted unsaturated monocyclic heterocyclic ring, an optionally substituted unsaturated fused heterobicyclic ring, or an optionally substituted benzene ring; X is a carbon atom or a nitrogen atom; Y is —(CH2)n— (n is 1 or 2); a pharmaceutically acceptable salt thereof, or a prodrug thereof.
    Type: Grant
    Filed: January 31, 2005
    Date of Patent: May 17, 2011
    Assignee: Mitsubishi Tanabe Pharma Corporation
    Inventors: Sumihiro Nomura, Eiji Kawanishi, Kiichiro Ueta
  • Patent number: 7939669
    Abstract: The present invention relates to a light emitting transition metal compound of Chemical Formula 1 and an organic electroluminescence device including the compound. In the Chemical Formula 1, M is selected from Ir, Pt, Rh, Re, and Os, m is 2 or 3, n is 0 or 1, the sum of m and n is 3, provided that the sum of m and n is 2 M is Pt. X is a N or P atom, and Y is S, O, or Se.
    Type: Grant
    Filed: January 8, 2007
    Date of Patent: May 10, 2011
    Assignees: Samsung Electronics Co., Ltd., Industry-University Cooperation Foundation, Hanyang University
    Inventors: Dong-Hack Suh, Jin-Sik Choi, Jin-Soo Lim, Song-Ho Kim, Chi-Hun Kim
  • Publication number: 20110105488
    Abstract: The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.
    Type: Application
    Filed: March 20, 2009
    Publication date: May 5, 2011
    Applicant: Chlorion Pharma, Inc.
    Inventors: Giorgio Attardo, Sasmita Tripathy
  • Publication number: 20110071125
    Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.
    Type: Application
    Filed: May 9, 2008
    Publication date: March 24, 2011
    Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
  • Patent number: 7902237
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular, compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of the disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Grant
    Filed: August 9, 2005
    Date of Patent: March 8, 2011
    Assignee: Exelixis, Inc.
    Inventors: Richard Martin, Brenton Todd Flatt, Jeffrey Dean Kahl
  • Patent number: 7902248
    Abstract: Disclosed herein are pyrazole glucokinase activators of the formula (I): that are useful for the treatment of metabolic diseases and disorders.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: March 8, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Steven Joseph Berthel, Robert Francis Kester, Douglas Eric Murphy, Thomas Jay Prins, Frank Ruebsam, Chinh Viet Tran, Dionisios Vourloumis
  • Patent number: 7897331
    Abstract: Thiazolyl tetrazolium salts with increased solubility in aqueous solutions have alkylammonium alkoxy substituents, preferably trimethyl ammonium propoxy groups substituents, on phenyl rings attached to the tetrazolium ring.
    Type: Grant
    Filed: June 16, 2010
    Date of Patent: March 1, 2011
    Assignee: Bayer HealthCare LLC
    Inventors: James P. Albarella, Steven W. Felman, John J. Landi, Karen L. Marfurt
  • Publication number: 20110046000
    Abstract: The presently disclosed subject matter provides dyes having an improved photostability, biosensors comprising such dyes, and methods of use thereof, including methods for detecting target molecules in a sample under test and for live-cell imaging. The dyes can include a binding member, including a biomolecule or fragments thereof, which can interact with target molecules of interest and can be specific to a given conformational state or covalent modification, e.g., phosphorylation, of the target molecule. The presently disclosed dyes can be used for detecting changes in the binding, conformational change, or posttranslational modification of the target molecule.
    Type: Application
    Filed: June 20, 2008
    Publication date: February 24, 2011
    Inventors: Klaus Hahn, Alexei Toutchkine
  • Patent number: 7888379
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 15, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Patent number: 7879888
    Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.
    Type: Grant
    Filed: May 24, 2006
    Date of Patent: February 1, 2011
    Assignee: Merck Serono SA
    Inventors: Anna Quattropani, David Covini, Vincent Pomel, Jerome Dorbais, Thomas Rueckle
  • Publication number: 20110020566
    Abstract: A charge transporting, liquid crystal photoalignment material comprising a charge transporting moiety connected through covalent chemical bonds to a surface derivatising moiety, and a photoalignment moiety connected through covalent chemical bonds to a surface derivatising moiety.
    Type: Application
    Filed: February 16, 2009
    Publication date: January 27, 2011
    Inventor: Gene Carl Koch
  • Patent number: 7875640
    Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Grant
    Filed: March 19, 2008
    Date of Patent: January 25, 2011
    Assignee: Abbott Laboratories
    Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Sridhar Peddi, William A. Carroll, Michael J. Dart
  • Patent number: 7872027
    Abstract: Compounds and compositions for interfering with the association of Myc and Max are described herein. These compounds and compositions are useful in methods inhibiting growth or proliferation of a cell. Methods of inhibiting growth or proliferation of a cell are provided, comprising contacting the cell with an amount of a compound that interferes with Myc and Max association effective to inhibit growth or proliferation of the cell.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: January 18, 2011
    Assignees: University of Pittsburgh - Of the Commonwealth System of Higher Education, Georgetown University
    Inventors: Steven J. Metallo, Edward V. Prochownik
  • Patent number: 7872146
    Abstract: Process for the preparation of a carboxamide derivative of formula (I) or a salt thereof Intermediates for preparing this compound are also provided.
    Type: Grant
    Filed: May 6, 2006
    Date of Patent: January 18, 2011
    Assignee: Bayer CropScience AG
    Inventors: Thierry Eynard, Cécile Franc
  • Publication number: 20110009261
    Abstract: A compound of the formula (I) where, for example, W, X and Y are each CH; R1 and R6 together with the adjacent nitrogen forms a 3 to 10-membered saturated ring, wherein the ring may contain, in addition to the nitrogen and carbon ring members, 1, 2 or 3 heteroatoms and/or heteroatom groups as ring members, independently of one another, selected from the group consisting of sulfur, CO, SO, SO2 and N—R7 and/or the ring may carry 1, 2 or 3 radicals, independently of one another, each selected, for example, from the group consisting of halogen, cyano, nitro, amino, and C1-C6-alkyl. R2 is, for example, halogen, C1-C6-alkyl, C1-C6-haloalkyl, C1-C6-alkoxy, C1-C6-haloalkoxy or C1-C6-alkoxy-C1-C6-alkoxy, and R7 is for example, R10C(?O), C1-C6 alkyl or C1-C6-haloalkyl; and/or salts thereof; and their use as pesticidal agents.
    Type: Application
    Filed: March 2, 2009
    Publication date: January 13, 2011
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Peter Maienfisch, Ottmar Hueter, Peter Renold, Werner Zambach, Thomas Pitterna
  • Publication number: 20110009428
    Abstract: The compounds of the subject invention have a structure according to formula I: wherein X is S or SO2; R1 is (1C-6C)alkyl, (3C-6C)alkenyl, or (3C-6C)alkynyl, each optionally substituted with (3C-6C)cycloalkyl, OH, OC(O)(1C-4C)alkyl, (1C-4C)alkoxy, halogen, cyano, formyl, C(O)(1C-4C)alkyl, CO2H, CO2(1C-4C)alkyl, C(O)NR5R6, S(O)(1C-4C)alkyl or S(O)2(1C-4C)alkyl; R2 is hydrogen, (1C-4C)alkyl or C(O)(1C-4C)alkyl; R3 is a phenyl group optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, (1C-4C)fluoroalkoxy, halogen, cyano or nitro; or R3 is a 5- or 6-membered aromatic heterocyclic ring structure optionally substituted with (1C-4C)alkyl, (1C-4C)fluoroalkyl, (1C-4C)alkoxy, halogen or cyano; R4 is a phenyl group or an aromatic 6-membered heterocycle, substituted at the ortho position with 1-hydroxy(1C-4C)alkyl, (1C-4C)alkoxy, C(O)(1C-4C)alkyl, CO2(1C-4C)alkyl, C(O)NH2, cyano, nitro, or CH?NOR7, and optionally further substituted with (1C-2C)alkyl, (1C-2C)fluoroalkyl or halogen; or R4
    Type: Application
    Filed: September 22, 2010
    Publication date: January 13, 2011
    Applicant: N.V. Organon
    Inventors: Jaap Van Der Louw, Neeltje Miranda Teerhuis, Johannes Petrus Maria Lommerse, Herman Thijs Stock, Pedro Harold Han Hermkens
  • Patent number: 7868030
    Abstract: Compounds of formula as well as pharmaceutically acceptable salts and esters thereof, wherein R1 to R3 have the significance given in the application and which can be used in the form of pharmaceutical compositions.
    Type: Grant
    Filed: May 30, 2007
    Date of Patent: January 11, 2011
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Marcel Gubler, Wolfgang Haap, Paul Hebeisen, Eric A. Kitas, Bernd Kuhn, Rudolf E. Minder, Brigitte Schott, Hans P. Wessel
  • Patent number: 7863304
    Abstract: Embodiments of this invention include novel analogs of Glycyl-Prolyl-Glutamate (GPE) and compositions containing such analogs of GPE. Of these, certain analogs have modified proline residues. Other embodiments of this invention include uses of analogs of GPE to protect neural cells from degeneration and/or death in response to injury or disease. Disorders treatable with compounds and compositions of this invention include hypoxia/ischemia, toxic injury, and chronic neurodegenerative disorders including Parkinson's disease.
    Type: Grant
    Filed: November 20, 2007
    Date of Patent: January 4, 2011
    Assignee: Neuren Pharmaceuticals Limited
    Inventors: Margaret Anne Brimble, Paul William Richard Harris, Frank Sieg
  • Patent number: 7863263
    Abstract: An EP2 agonist which may have an EP3 agonistic effect has an effect of regenerating and/or protecting nerves, and is therefore useful as a therapeutic agent for a disease of the peripheral nervous system, such as a lower or upper motor neuron disease, a nerve root disease, plexopathy, thoracic outlet compression syndrome, peripheral neuropathy, neurofibromatosis and neuromuscular transmission disease. An EP2 agonist which has an EP3 agonistic effect is a safe and effective agent for the regeneration and/or protection of nerves which has little influence on the circulatory system.
    Type: Grant
    Filed: June 2, 2006
    Date of Patent: January 4, 2011
    Assignee: Ono Pharmaceutical Co., Ltd.
    Inventors: Kazuyuki Ohmoto, Akihiro Kinoshita, Hidekazu Matsuya
  • Publication number: 20100331378
    Abstract: The invention relates to aminotriazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.
    Type: Application
    Filed: December 17, 2008
    Publication date: December 30, 2010
    Applicant: Actelion
    Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
  • Publication number: 20100324001
    Abstract: Methods of inhibiting the cytokine or biological activity of Macrophage Migration Inhibitory Factor (MIF) comprising contacting MIF with a compound of formula (I) are provided. The invention also relates to methods of treating diseases or conditions where MIF cytokine or biological activity is implicated comprising administration of compounds of formula (I), either alone or as a part of combination therapy. Novel compounds of formula (I) are also provided for.
    Type: Application
    Filed: June 30, 2010
    Publication date: December 23, 2010
    Applicant: Cortical Pty LTD
    Inventors: Eric Francis Morand, Magdy Naguib Iskander, Colin Edward Skene
  • Patent number: 7854920
    Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.
    Type: Grant
    Filed: July 26, 2007
    Date of Patent: December 21, 2010
    Assignee: University of Pittsburgh
    Inventors: William E. Klunk, Chester A. Mathis, Jr., Yanming Wang
  • Patent number: 7846953
    Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalac
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: December 7, 2010
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Michael Gaul, Alexander Kim, Lily Lee Searle, Raymond Patch, Dionisois Rentzeperis, Guozhang Xu, Xizhen Zhu
  • Publication number: 20100298558
    Abstract: There is provided a novel pest control agent, particularly an insecticide or miticide. A substituted dihydroazole compound of General Formula (1) or a salt thereof: where A1, A2, A3 and A4 are independently C—Y or N, A5 is —CH2—, etc., G1 is a benzene ring, etc., G2 is G2-1, G2-6, G2-9, etc., X is a halogen atom, C1-2haloalkyl, etc., Z is methyl, —NH2, etc., R1 is —C(O)R1a, etc., R1a is C1-4alkyl, etc., R2 is H, C1-4alkyl, etc., R3 is C1-2haloalkyl, etc., R4 is H, cyano, methyl, etc., m is an integer of 1, 2, 3, etc., n is an integer of 0 or 1; and a pest control agent comprising the compound or the salt thereof.
    Type: Application
    Filed: December 5, 2008
    Publication date: November 25, 2010
    Applicant: NISSAN CHEMICAL INDUSTRIES, LTD.
    Inventors: Takeshi Mita, Eitatsu Ikeda, Hiroaki Takahashi, Mitsuaki Komoda
  • Publication number: 20100292239
    Abstract: Compounds of the formula (I), in which the substituents are as defined in claim 1 are suitable for use as microbiocides.
    Type: Application
    Filed: July 24, 2008
    Publication date: November 18, 2010
    Applicant: SYNGENTA CROP PROTECTION, INC.
    Inventors: Daniel Stierli, Antoine Daina, Harald Walter, Hans Tobler, Ramya Rajan
  • Patent number: 7829563
    Abstract: The present invention relates to compounds of formula I wherein Ar1, Ar2, Ar3, n, and R1 to R8 are as defined herein and to pharmaceutically suitable acid addition salts, optically pure enantiomers, racemates or diastereomeric mixtures thereof. These compounds are orexin receptor antagonists and may be useful in the treatment of disorders, in which orexin pathways are involved, like sleep disorders.
    Type: Grant
    Filed: February 27, 2008
    Date of Patent: November 9, 2010
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Henner Knust, Parichehr Malherbe, Matthias Nettekoven, Emmanuel Pinard, Olivier Roche, Mark Rogers-Evans
  • Patent number: 7829722
    Abstract: The present invention relates to compositions of matter that are ionic liquids, the compositions comprising any of eleven cations combined with any of three fluorinated sulfonated anions. Compositions of the invention should be useful as solvents and, perhaps, as catalysts for many reactions, including aromatic electrophilic substitution, nitration, acylation, esterification, etherification, oligomerization, transesterification, isomerization and hydration.
    Type: Grant
    Filed: May 27, 2009
    Date of Patent: November 9, 2010
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Mark Andrew Harmer, Christopher P. Junk, Jemma Vickery
  • Publication number: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Patent number: 7824661
    Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.
    Type: Grant
    Filed: February 14, 2005
    Date of Patent: November 2, 2010
    Assignee: Molecular Insight Pharmaceuticals, Inc.
    Inventors: John W. Babich, Kevin B. Maresca, James F. Kronauge, Jr.
  • Publication number: 20100267676
    Abstract: Gamma-amino-butyric acid derivatives that are GABAB receptor ligands, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives and pharmaceutical compositions thereof for treating diseases are disclosed.
    Type: Application
    Filed: April 16, 2010
    Publication date: October 21, 2010
    Inventors: Feng Xu, Mark A. Gallop, Ge Peng, Thu Phan, Usha Dilip, David J. Wustrow
  • Patent number: 7816558
    Abstract: Provided is a triarylcarboxylic acid derivative, or an isomer, a prodrug, a hydrate, a solvate, a polymorph, or a pharmaceutically acceptable salt thereof, represented by the following general formula (I): wherein A is an optionally substituted aryl or heteroaryl, and B is an optionally substituted monocyclic heteroaryl; and a pharmaceutical composition comprising the same and a pharmaceutically acceptable carrier. The triarylcarboxylic acid derivative (I) exhibits potent xanthine oxidase inhibiting action and is therefore useful as a therapeutic agent for preventing or treating hyperuricemia, gout, inflammatory bowel disease, diabetic nephropathy and diabetic retinopathy.
    Type: Grant
    Filed: October 6, 2006
    Date of Patent: October 19, 2010
    Assignee: Astellas Pharma Inc.
    Inventors: Junji Sato, Kazuyuki Hattori, Hirokazu Kubota, Ryosuke Munakata, Toru Asano, Junko Maeda, Masakatsu Kawakami, Akio Kamikawa
  • Patent number: 7812041
    Abstract: The present invention relates to compounds of the general formula (I) and salts and physiologically functional derivatives thereof, wherein R1 is independently hydrogen; alkyl, cycloalkyl, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl, substituted aryl, heteroaryl, substituted heteroaryl, arylalkyl or substituted arylalkyl; R2 is independently —NR3R4, R3 is independently alkyl, cycloalkyl, alkoxy, alkylamine, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl, R4 is independently alkyl, cycloalkyl, alkoxy, alkylamine, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R5 is independently H, COR6, CO2R6, SOR6, SO3R6, alkyl, cycloalkyl, alkoxy, —NH2, alkylamine, —NR7COR6, halogen, —OH, —SH, alkylthio, hydroxyalkyl, haloalkyl, haloalkyloxy, aryl or heteroaryl; R6 is independently H, alkyl, cycloalkyl, —NH2, alkylamine, aryl or heteroaryl; R7 is independently H, alkyl, cycloalkyl, alkoxy, —OH, —SH, alkylthio, hydroxyalkyl, aryl, or heteroaryl; p is 0, or 1;
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: October 12, 2010
    Assignee: 4SC AG
    Inventors: Johann Leban, Harald Schmitt, Kristina Wolf, Stefano Pegoraro, Andreas Wuzik
  • Publication number: 20100256114
    Abstract: The present invention relates to inhibitors of 11-? hydroxyl steroid dehydrogenase type 1, antagonists of the mineralocorticoid receptor (MR), and pharmaceutical compositions thereof. The compounds of the invention can be useful in the treatment of various diseases associated with expression or activity of 11-? hydroxyl steroid dehydrogenase type 1 and/or diseases associated with aldosterone excess.
    Type: Application
    Filed: June 17, 2010
    Publication date: October 7, 2010
    Applicant: INCYTE CORPORATION
    Inventors: Wenqing Yao, Jincong Zhuo, Meizhong Xu, Brian W. Metcalf, Chunhong He, Ding-Quan Qian, Colin Zhang