1,3-oxazoles (including Hydrogenated) Patents (Class 548/215)
  • Patent number: 7326696
    Abstract: Aminomethyl substituted tetracycline compounds, pharmaceutical compositions, and methods of use thereof are discussed.
    Type: Grant
    Filed: December 15, 2003
    Date of Patent: February 5, 2008
    Assignee: Paratek Pharmaceuticals, Inc.
    Inventors: Mark L. Nelson, Kwasi Ohemeng, Roger Frechette, Paul Abato, Victor Amoo, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Laura Honeyman, Mohamed Y. Ismail, Oak Kim, Rachid Mechiche, N. Laxma Reddy, Atul K. Verma, Peter Viski, Tadeusz Warchol, Ivan Yanachkov
  • Patent number: 7320978
    Abstract: This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.
    Type: Grant
    Filed: August 1, 2006
    Date of Patent: January 22, 2008
    Assignee: Sanofi-Aventis
    Inventors: Francis Barth, Joelle Arnaud-Taillades, Christian Congy, Murielle Rinaldi-Carmona
  • Patent number: 7316851
    Abstract: An electroluminescent element is disclosed, comprising an electroluminescent material and a fluorescent substance emitting light having an emission maximum at the wavelength different from that of light emitted from the electroluminescent material upon absorption of the light emitted from the electroluminescent material. A color conversion filter is also disclosed, comprising a fluorescent substance emitting light having an emission maximum at the wavelengths of 400 to 700 nm upon absorption of the light emitted from the electroluminescent material.
    Type: Grant
    Filed: September 4, 2003
    Date of Patent: January 8, 2008
    Assignee: Konica Corporation
    Inventors: Hiroshi Kita, Yoshiyuki Suzuri, Taketoshi Yamada, Kazuaki Nakamura, Noriko Ueda, Yasushi Okubo
  • Publication number: 20080004451
    Abstract: Disclosed is a process for the manufacture of pseudo proline dipeptides of the formula wherein R1 is a side chain of an alpha amino acid, R2 is an amino protecting group and R3 and R4 are independently either hydrogen or C1-4-alkyl, and R5 is hydrogen or methyl starting from an amino acid derivative of the formula wherein R1 and R2 are as defined above. Pseudo proline dipeptides can be used as reversible protecting groups for Ser, Thr and Cys and thus are versatile tools in peptide chemistry.
    Type: Application
    Filed: June 14, 2007
    Publication date: January 3, 2008
    Inventors: Thomas Ammann, Stephan Goetzoe, Bernd Thern, Sandra Welz, Klaus-Juergen Wolter
  • Publication number: 20070281981
    Abstract: Disclosed herein is a compound having a structure or a pharmaceutically acceptable salt, or a prodrug thereof. Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
    Type: Application
    Filed: May 11, 2007
    Publication date: December 6, 2007
    Inventors: DAVID W. OLD, Danny T. Dinh
  • Patent number: 7301028
    Abstract: The present invention relates to dihydropyrazole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Grant
    Filed: June 12, 2003
    Date of Patent: November 27, 2007
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth L. Arrington, Mark E. Fraley
  • Patent number: 7300472
    Abstract: The invention relates to agents for coloring fibers containing keratin, in particular, human hair, which comprise selected cationic, CH-acidic heterocycles according to formula I in which A, R1, R2 and X? are as defined in the application, in combination with reactive carbonyl compounds, to the use of this combination in agents for coloring fibers containing keratin, for freshening up the color or nuancing fibers containing keratin which have already been colored, and to a method of coloring fibers containing keratin, in particular, human hair.
    Type: Grant
    Filed: June 19, 2006
    Date of Patent: November 27, 2007
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Wibke Gross, Horst Höffkes, Doris Oberkobusch, Sandra Mausberg
  • Patent number: 7297797
    Abstract: The invention relates to novel ?1-pyrrolines of the formula (I) in which R1, R2, R3, R4, A1, A2, R5, R6, R7, R8, R9 and Q are as defined in the disclosure, to a process for preparing these compounds and to their use for controlling pests.
    Type: Grant
    Filed: September 8, 2003
    Date of Patent: November 20, 2007
    Assignee: Bayer CropScience AG
    Inventors: Johannes Rudolf Jansen, Udo Kraatz, Hubertus Stakemeier, Thomas Seitz, Fritz Maurer, Martin Füsslein, Bernd Alig, Christian Funke, Werner Hallenbach, Jörg Konze, Udo Beckmann, Ulrich Görgens
  • Patent number: 7291633
    Abstract: Compounds of the formula I in which R1, R2, R3 and R4 are as defined in claim 1, are ligands of the nicotinic acetylcholine receptor and/or serotonergic ligands and are suitable for the prophylaxis or treatment of psychoses, schizophrenia, depression, anxiety states, dementia, in particular Alzheimer's disease and Lewy bodies dementia, neurodegenerative disorders, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, Tourette's syndrome, learning and memory restrictions, bulimia anorexia nervosa or other eating disorders, compulsvie behaviour, premenstrual syndrome, age-induced memory impairment, amelioration of withdrawal symptoms in nicotine dependence, strokes or brain damage by toxic compounds, and for the treatment of disorders which are characterised by an excess of circulating serotonin or by serotonergic hyperactivity
    Type: Grant
    Filed: April 5, 2002
    Date of Patent: November 6, 2007
    Assignee: Merck Patent GmbH
    Inventors: Kai Schiemann, Henning Böttcher, Joachim Leibrock
  • Patent number: 7285568
    Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration 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, into cosmetic compositions.
    Type: Grant
    Filed: May 24, 2005
    Date of Patent: October 23, 2007
    Assignee: Galderma Research & Development
    Inventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
  • Publication number: 20070238765
    Abstract: The present invention provides a compound of the formula: or pharmaceutically acceptable salts, solvates or prodrugs thereof, wherein Y, Ar, R1 and R2 are defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
    Type: Application
    Filed: April 11, 2007
    Publication date: October 11, 2007
    Inventors: Xiao-Fa Lin, David Garrett Loughhead, Jason Manka, Counde O'Yang, Michael Soth, Dennis M. Yasuda
  • Patent number: 7265140
    Abstract: The present invention relates to acyloxymethylcarbamate oxazolidinones. The compounds of the present invention have potent activity with excellent oral bioavailability against Gram-positive and Gram-negative bacteria.
    Type: Grant
    Filed: September 9, 2004
    Date of Patent: September 4, 2007
    Assignee: Pfizer Inc
    Inventors: Vara Prasad Venkata Nagendra Josyula, Robert C. Gadwood, Lisa Marie Thomasco, Ji-Young Kim, Allison Laura Choy, Frederick Earl Boyer
  • Patent number: 7265138
    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: February 9, 2004
    Date of Patent: September 4, 2007
    Assignee: Amgen Inc.
    Inventors: Elizabeth M. Doherty, Christopher H. Fotsch, Nianhe Han, Randall W. Hungate, Qingyian Liu, Mark H. Norman, Ning Xi, Shimin Xu
  • Patent number: 7262156
    Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.
    Type: Grant
    Filed: January 17, 2007
    Date of Patent: August 28, 2007
    Assignee: Procter & Gamble Company
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle, Lon Montgomery Gray
  • Publication number: 20070191313
    Abstract: The invention provides compounds represented by the formula I, each of which compounds may have sphingosine-1-phosphate receptor agonist and or antagonist biological activity: and wherein the variables Y, R4, n, A, X, Z, R1, o, R3, R2 and p are as defined in the specification.
    Type: Application
    Filed: February 15, 2007
    Publication date: August 16, 2007
    Inventors: Richard L. Beard, John E. Donello, Haiqing Yuan, Diana F. Colon, Tien Duong, Xiaoxia Liu, Yihui Hu
  • Patent number: 7256206
    Abstract: The present invention relates to bicyclic derivatives, process for their production, their uses and pharmaceutical compositions containing them. The invention provides a novel class of compounds useful in the treatment or prevention of diseases or disorders mediated by lymphocyte interactions, particularly diseases associated with EDG/S1P receptor mediated signal transduction.
    Type: Grant
    Filed: February 11, 2004
    Date of Patent: August 14, 2007
    Assignee: IRM LLC
    Inventors: Shifeng Pan, Nathanael S. Gray, Yuan Mi, Wenqi Gao, Yi Fan, Sophie Lefebvre
  • Patent number: 7247649
    Abstract: The present invention relates to novel oxazoles of formula (I) their pharmaceutically acceptable salts, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, medicaments containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: August 3, 2004
    Date of Patent: July 24, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Ulrike Reiff, Matthias Rueth, Edgar Voss
  • Patent number: 7244851
    Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.
    Type: Grant
    Filed: July 5, 2005
    Date of Patent: July 17, 2007
    Assignee: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 7244752
    Abstract: The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9—; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is —C(?O)—, —O—C(?O)—, —NR8—C(?O)—, —O—C1-6alkanediyl-C(?O)—, —NR8—C1-6alkanediyl-C(?O)—, —S(?O)2—, —O—S(?O)2—, —NR8—S(?O)2; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC(?O), carboxyl, aminoC(?O), mono- or di(C1-4alkyl)aminoC(?O), C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; A is C1-6alkanediyl, —C(?O)—, —C(?S)—, —S(?O)2—, C1-6alkanediyl-C(?O)—, C1-6alkanediyl-C(?S)— or C1-6alkanediyl-S(?O)2—; R5 is H, OH, C1-6alkyl, Het1C1-6alkyl, Het2C1-6alkyl, optionally substituted aminoC1-6alkyl; R6 is C1-6alkylO, Het1, Het1O, Het2, Het2O, aryl, arylO, C1-6
    Type: Grant
    Filed: April 9, 2002
    Date of Patent: July 17, 2007
    Assignee: Tibotec Pharmaceuticals Ltd.
    Inventors: Dominique Louis Nestor Ghislain Surleraux, Sandrine Marie Helene Vendeville, Wim Gaston Verschueren, Marie-Pierre T. M. M. G. De Bethune, Herman Augustinus De Kock, Abdellah Tahri, Montserrat Erra Solà
  • Patent number: 7241900
    Abstract: A method of synthesizing aromatic ketone compositions of formula I comprising the step of introducing a double bond into the 5 membered ring of the 4,5-dihydro-1,3-azoles moiety of formula II is disclosed. A method of synthesizing aromatic ketone compositions of formula I comprising the step of ring synthesis of the tetrahydro-1,3-azoles of formula XI is also disclosed.
    Type: Grant
    Filed: November 23, 2005
    Date of Patent: July 10, 2007
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Pawel K. Grzywacz, Rafal R. Sicinski
  • Patent number: 7232792
    Abstract: Benzoyl derivatives of the formula I where the variables have the following meanings: R1, R2 are hydrogen, nitro, halogen, cyano, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio, haloalkylthio, alkylsulfinyl, haloalkylsulfinyl, alkylsulfonyl or C1–C6-haloalkylsulfonyl; R3 is hydrogen, halogen or alkyl; R4, R5 are hydrogen, halogen, cyano, nitro, alkyl, alkoxy, alkylthio, dialkylamino, phenyl or carbonyl, it being possible for the 6 last-mentioned radicals to be substituted; X is O, S, NR9, CO or CR10R11; Y is O, S, NR12, CO or CR13R14; R15 is pyrazole which is unsubstituted or substituted, linked in the 4-position and has attached to it in the 5-position a hydroxyl or sulfonyloxy radical; and the agriculturally useful salts thereof; processes and intermediates for the preparation of the 3-heterocyclyl-substituted benzoyl derivatives, compositions comprising them; and the use of these derivatives or compositions comprising them for controlling undesirable plants.
    Type: Grant
    Filed: December 27, 2000
    Date of Patent: June 19, 2007
    Assignee: BASF Aktiengesellschaft
    Inventors: Wolfgang von Deyn, Regina Luise Hill, Uwe Kardorff, Ernst Baumann, Stefan Engel, Guido Mayer, Matthias Witschel, Michael Rack, Norbert Götz, Joachim Gebhardt, Ulf Miβlitz, Helmut Walter, Karl-Otto Westphalen, Martina Otten, Joachim Rheinheimer
  • Patent number: 7229988
    Abstract: The present invention provides novel dialkylhydroxybenzoic acid derivatives containing metal chelating groups and the use of the novel compounds as therapeutics for treating and/or preventing various medical dysfunctions and diseases arising from reactive oxygen species and/or excess Zn ions, in particular stroke, Parkinson's disease, Alzheimer's disease. The compounds of the invention have not only low toxicity but also similar or superior LPO inhibition activity to references. They also effectively inhibit the cerebral neuronal cell death by ROS and/or zinc ion, and show neuroprotective effects against ischemic neuronal degeneration.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: June 12, 2007
    Assignee: Samsung Electronics Co., Ltd.
    Inventors: Eu-Gene Oh, Sung-Bo Ko, Kyung-Hwa Kim, In-Kyu Chang, Dennis W. Choi, Laura L. Dugan, Jae-Young Koh, In-Jae Shin, Moo-Ho Won
  • Patent number: 7220783
    Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, —CH2—, —NR14— or —S(O)p- and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: November 12, 2003
    Date of Patent: May 22, 2007
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7211674
    Abstract: A process for the recovery of oxazole comprising contacting a mixture comprising oxazole and acetonitrile with an acid to form an acid salt of oxazole; separating acid salt of the oxazole from the mixture; and neutralizing the acid salt of oxazole separated from the mixture to release oxazole.
    Type: Grant
    Filed: December 17, 2003
    Date of Patent: May 1, 2007
    Assignee: Ineos USA LLC
    Inventors: Mark C. Cesa, Eric J. Moore, Mark R. Bruce, Sanjay P. Godbole, Michael K. Hagans, David R. Bender
  • Patent number: 7208169
    Abstract: The invention relates to novel biphenylcarboxamides of the formula (I) in which R1, R2, m, n, R3, Y and A are as defined in the disclosure, to a plurality of processes for preparing these substances and their use for controlling unwanted microorganisms, and to novel intermediates and their preparation.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: April 24, 2007
    Assignee: Bayer CropScience LP
    Inventors: Ralf Dunkel, Hans-Ludwig Elbe, Heiko Rieck, Robert Markert, Ulrike Wachendorff-Neumann, Astrid Mauler-Machnik, Karl-Heinz Kuck, Martin Kugler, Thomas Jaetsch
  • Patent number: 7205326
    Abstract: Compounds of formula (I) are useful in the therapy and/or prevention of illnesses with known over-expression of receptor tyrosine kinases of the HER-family like HER-2 and EGFR (HER-1). Accordingly, these compounds are useful for the treatment of diseases such as cancer in humans or animals.
    Type: Grant
    Filed: April 28, 2004
    Date of Patent: April 17, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Ulrike Reiff, Matthias Rueth, Edgar Voss
  • Patent number: 7202368
    Abstract: A process for preparing an optionally substituted 4-benzimidazol-2-ylmethylamino)benzamidine, the process comprising: (a) condensing an optionally suitably substituted diaminobenzene with 2-[4-(1,2,4-oxadiazol-5-on-3-yl)phenylamino]acetic acid; (b) hydrogenating the product obtained from step (a); and (c) optionally carboxylating the amidino group of the product obtained from step (b).
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: April 10, 2007
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Georg Zerban, Arndt Hausherr, Kerstin Schlarb, Heinz-Peter Schmitt, Bjoern Weyell, Gunter Koch, Rainer Hamm
  • Patent number: 7201892
    Abstract: Novel tumor specific phototherapeutic and photodiagnostic agents are disclosed. The compounds consist of a carbocyanine dye for visualization, photosensitizer for photodynamic treatment, and tumor receptor-avid peptide for site-specific delivery of the probe and phototoxic agent to diseased tissues. A combination of these elements takes full advantage of the unique and efficient properties of each component for an effective patient care management.
    Type: Grant
    Filed: May 17, 2004
    Date of Patent: April 10, 2007
    Assignee: Mallinckrodt Inc.
    Inventors: Samuel Achilefu, Richard B. Dorshow, Raghavan Rajagopalan, Joseph E. Bugaj
  • Patent number: 7202247
    Abstract: The invention relates to compounds, pharmaceutical compositions and methods of using compounds of the general formula or its pharmaceutically acceptable salt or ester, wherein the substituents are defined in the application.
    Type: Grant
    Filed: December 19, 2002
    Date of Patent: April 10, 2007
    Assignee: AtheroGenics, Inc.
    Inventors: James A. Sikorski, Charles Q. Meng, M. David Weingarten
  • Patent number: 7189751
    Abstract: The present invention provides medicinal compositions characterized by comprising as the active ingredient either a compound represented by a formula [I] or a pharmaceutically acceptable composite thereof; [wherein X represents oxygen or sulfur; R1 represents e.g., C1-4 alkyl, phenyl optionally substituted, etc.; Q1 represents spacer consisted of 0 to 3 carbon atoms; R2 represents, e.g., phenyl optionally substituted; R3 represents, e.g., hydrogen, C1-4 alkyl, or a group represented by the following formulae; —CONH—R6; R4 and R5 represent e.g., nitro, cyano, C1-4 alkylcarbonyl, respectively]; in particular, medicine which is useful as therapeutic and/or protective drugs for inflammatory diseases and/or allergic diseases by improving sick conditions accompanied with the stimulated phospholipase A(2) activity.
    Type: Grant
    Filed: June 25, 2002
    Date of Patent: March 13, 2007
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Masae Takagi, Tadayuki Nishibe, Keiichi Ishimitsu
  • Patent number: 7186843
    Abstract: This invention provides a quinolone derivative having potent antibacterial activity against various bacteria including drug-resistant strains which is a compound of the following formula wherein R1 is an optionally substituted aromatic group, a salt of the same or a hydrate of both.
    Type: Grant
    Filed: April 29, 2004
    Date of Patent: March 6, 2007
    Assignee: Daiichi Pharmaceutical Co. Ltd.
    Inventors: Makoto Takemura, Hisashi Takahashi, Katsuhiro Kawakami, Toshiyuki Takeda, Rie Miyauchi
  • Patent number: 7183252
    Abstract: The invention is directed to novel indole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
    Type: Grant
    Filed: March 31, 2003
    Date of Patent: February 27, 2007
    Assignee: Ortho-McNeil Pharmaceutical, Inc.
    Inventors: Han-Cheng Zhang, William J. Hoekstra, Bruce E. Maryanoff, David F. McComsey
  • Patent number: 7173047
    Abstract: Compounds of formula (I) and pharmaceutically acceptable derivatives thereof bind with high affinity to the EP4 receptor and are of use in the treatment or prevention of conditions such as a pain, inflammatory, immunological, bone, neurodegenerative or renal disorder.
    Type: Grant
    Filed: December 20, 2001
    Date of Patent: February 6, 2007
    Assignee: Glaxo Group Limited
    Inventors: Gerard Martin Paul Giblin, Stephen Vernon Frye, Susan Roomans
  • Patent number: 7169797
    Abstract: The present invention is directed to compounds of formula (I), or a pharmaceutically suitable salt or prodrug thereof, which are useful for the selective inhibition of protein tyrosine phosphatase-1B (PTP1B), and are useful for the treatment of disorders caused by overexpressed or altered protein tyrosine phosphatase 1B.
    Type: Grant
    Filed: February 4, 2004
    Date of Patent: January 30, 2007
    Assignee: Abbott Laboratories
    Inventors: Zhili Xin, Gang Liu, Zhonghua Pei, Bruce G. Szczepankiewicz, Michael D. Serby, Hongyu Zhao
  • Patent number: 7166715
    Abstract: The invention provides an asymmetric cyanine dye compound having the structure including substituted forms thereof, wherein, at least one of R1 and R2 is linking group, X is O, S, or Se, and n ranges from 0 to 2. The invention further provides reporter-quencher dye pairs comprising the asymmetric cyanine dyes, dye-labelled polynucleotides incorporating the asymmetric cyanine dyes, and hybridization detection methods utilizing the dye-labelled polynucleotides.
    Type: Grant
    Filed: May 5, 2004
    Date of Patent: January 23, 2007
    Assignee: Applera Corporation
    Inventors: Linda G. Lee, Ronald J. Graham, Khairuzzaman B. Mullah, Francis T. Haxo
  • Patent number: 7163953
    Abstract: Objects of the present invention are the compounds of formula (I) their pharmaceutically acceptable salts or esters, enantiomeric forms, diastereoisomers and racemates, the preparation of the above-mentioned compounds, pharmaceutical compositions containing them and their manufacture, as well as the use of the above-mentioned compounds in the control or prevention of illnesses such as cancer.
    Type: Grant
    Filed: May 18, 2005
    Date of Patent: January 16, 2007
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Birgit Bossenmaier, Walter-Gunar Friebe, Thomas Friess, Christian Geletneky, Guy Georges, Irene Kolm, Edgar Voss
  • Patent number: 7148246
    Abstract: Cycloalkyl derivatives having bioisosteric carboxylic acid groups, processes for their preparation and their use as pharmaceuticals The invention relates to cycloalkyl derivatives having bioisosteric carboxylic acid groups and to their physiologically acceptable salts and physiologically functional derivatives. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistence is involved.
    Type: Grant
    Filed: February 27, 2004
    Date of Patent: December 12, 2006
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Dirk Gretzke, Heiner Glombik, Eugen Falk, Jochen Goerlitzer, Stefanie Keil, Hans-Ludwig Schaefer, Christian Stapper, Wolfgang Wendler
  • Patent number: 7145004
    Abstract: The present invention relates to a process for the preparation of monohydroperfluoroalkanes, bis(perfluoroalkyl)phosphinates and perfluoroalkylphosphonates which comprises at least the treatment of at least one perfluoroalkylphosphorane with at least one base in a suitable reaction medium.
    Type: Grant
    Filed: March 17, 2003
    Date of Patent: December 5, 2006
    Assignee: Merck Patent Gesellschaft
    Inventors: Nikolai Ignatyev, Michael Weiden, Urs Welz-Biermann, Udo Heider, Peter Sartori, Andriy Kucheryna, Helge Willner
  • Patent number: 7132439
    Abstract: The present invention provides a genus of bis-benzimidazole compounds, methods and pharmaceutical compositions that are useful as modulators of potassium ion channels. The compounds of the invention are of use in both therapeutic and diagnostic methods.
    Type: Grant
    Filed: May 13, 2003
    Date of Patent: November 7, 2006
    Assignee: Icagen, Inc.
    Inventors: Xiaodong Wang, Alan B. Fulp, Albert M. van Rhee, Kerry L. Spear
  • Patent number: 7129254
    Abstract: Conjugates of epothilones and epothilone derivatives (as effectors) with suitable biomolecules (as recognition units) are described. Their production is carried out by the effectors being reacted with suitable linkers, and the compounds that are produced are conjugated to the recognition units. The pharmaceutical use of the conjugates for treating proliferative or angiogenesis-associated processes is described.
    Type: Grant
    Filed: July 31, 2003
    Date of Patent: October 31, 2006
    Assignee: Schering Aktiengesellschaft
    Inventors: Markus Berger, Gerhard Siemeister, Ulrich Klar, Jorg Willuda, Andreas Menrad, Klaus Bosslet
  • Patent number: 7126005
    Abstract: The present invention is directed to a new process of preparing highly pure Florfenicol. The invention is further directed to new oxazolidine derivatives useful in making Florfenicol and processes of making these derivatives. Examples of such intermediates include (4R,5R)-3-acetyl-2,2-dimethyl-4-hydroxymethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine; and (4S,5R)-3-acetyl-2,2-dimethyl-4-fluoromethyl-5-[4-(methylsulfonyl)phenyl]-1,3-oxazolidine.
    Type: Grant
    Filed: December 16, 2003
    Date of Patent: October 24, 2006
    Assignee: Aurobindo Pharma Limited
    Inventors: Vijay Kumar Handa, Arun Kumar Gupta, Meenakshisunderam Sivakumaran
  • Patent number: 7119113
    Abstract: The invention relates to carboxamide derivatives as defined in the specification and claims, to a process for their preparation, to pharmaceutical compositions comprising them and to their use as mGluR1 enhancers in the treatment and prevention of neurological disorders and diseases, such as Alzheimer's disease and dementia.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: October 10, 2006
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Joerg Huwyler, Frederic Knoflach, Eric Vieira, Juergen Wichmann
  • Patent number: 7112599
    Abstract: The present invention relates to compounds of the Formula wherein R3, R5, R6, R7, and Z, and other variables enumerated under one or more of R3, R5, R6, R7, and Z, are as defined. Compounds of the Formula I have activity inhibiting production of A?-peptide. This invention also relates to pharmaceutical compositions and methods of treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the Formula I.
    Type: Grant
    Filed: August 5, 2004
    Date of Patent: September 26, 2006
    Assignee: Pfizer Inc.
    Inventor: Yuhpyng L. Chen
  • Patent number: 7109153
    Abstract: The present invention relates to photo-labile pro-fragrance conjugates comprising: a) a photo-labile unit which upon exposure to electromagnetic radiation is capable of releasing a pro-fragrance unit; and b) a pro-fragrance unit, which when so released is either i) a pro-fragrance compound capable of releasing a fragrance raw material; or ii) a fragrance raw material. The present invention relates to systems for delivering fragrances to a situs, and to laundry detergent compositions, fine fragrances, personal care and hair care compositions comprising said systems.
    Type: Grant
    Filed: June 9, 2005
    Date of Patent: September 19, 2006
    Assignee: Procter & Gamble Company
    Inventors: Robert Richard Dykstra, Gregory Scot Miracle, Lon Montgomery Gray
  • Patent number: 7101915
    Abstract: The present invention provides a selective suppressor of the IgE production comprising a compound which suppresses the IgE production in a process from a differentiation of a mature B cell into an antibody-producing cell to the production of an antibody and which does not suppress or weakly suppresses the production of IgG, IgM and/or IgA which are produced at the same time, a compound of the formula (I): wherein R1–R13 are hydrogen, halogen, lower alkyl, lower alkoxy or the like, X is —O—, CH2—, —NR14— or —S(O)p— and Y is lower alkyl, lower alkenyl or the like, a process for producing the same and a pharmaceutical composition comprising the same.
    Type: Grant
    Filed: July 30, 1997
    Date of Patent: September 5, 2006
    Assignee: Shionogi & Co., Ltd.
    Inventors: Kenji Kawada, Mitsuaki Ohtani, Ryuji Suzuki, Akinori Arimura
  • Patent number: 7091360
    Abstract: The present invention is directed to a novel process for preparing heteroaryl and unsaturated heterocycloalkylmagnesium reagents that are useful in the synthesis of a variety of pharmaceuticals, in particular certain cysteine protease inhibitors.
    Type: Grant
    Filed: April 16, 2003
    Date of Patent: August 15, 2006
    Assignee: Aventis Pharma S.A.
    Inventors: Jiayao Li, John O. Link, Colette Colladant
  • Patent number: 7091204
    Abstract: The present invention relates to sulfonamides, pharmaceutical compositions containing them, and their use as antagonists of urotensin II.
    Type: Grant
    Filed: May 7, 2002
    Date of Patent: August 15, 2006
    Assignee: SmithKline Beecham Corporation
    Inventors: Dashyant Dhanak, Timothy F. Gallagher, Steven D. Knight
  • Patent number: 7091350
    Abstract: The invention relates to diaminopyrazole derivatives having the following structure (I), wherein R1 represents an alkyl or alkenyl radical bearing at least one substituent selected from among OR, NRR?, SR, SOR, SO2R, COOR, CONRR?, PO(OH)2, SO3X, NHCONRR, a non-cationic heterocycle, an aryl, a halogen. R2 and R3 are different from H and represent, independently of each other, an alkyl or alkenyl group; R2 and R3, together with the nitrogen atom to which they are attached, can form a heterocycle possibly comprising at least one other heteroatom selected from among N, O and S; R2 and R3 or the heterocycle that they form with the nitrogen to which they are attached can be substituted by at least one substituent defined above.
    Type: Grant
    Filed: February 14, 2002
    Date of Patent: August 15, 2006
    Assignee: L'Oreal
    Inventors: Thilo Fessmann, Eric Terranova
  • Patent number: 7087599
    Abstract: The present invention relates to compounds and derivatives thereof, their synthesis, and their use as estrogen receptor modulators. The compounds of the instant invention are ligands for estrogen receptors and as such may be useful for treatment or prevention of a variety of conditions related to estrogen functioning including: bone loss, bone fractures, osteoporosis, cartilage degeneration, endometriosis, uterine fibroid disease, hot flashes, increased levels of LDL cholesterol, cardiovascular disease, impairment of cognitive functioning, cerebral degenerative disorders, restinosis, gynacomastia, vascular smooth muscle cell proliferation, obesity, incontinence, and cancer, in particular of the breast, uterus and prostate.
    Type: Grant
    Filed: February 14, 2001
    Date of Patent: August 8, 2006
    Assignee: Merck & Co., Inc.
    Inventors: Dann LeRoy Parker, Jr., Ronald W. Ratcliffe, Robert R. Wilkening, Kenneth J. Wildonger
  • Patent number: RE39663
    Abstract: The invention provides compositions electron-deficient nitrogen heterocycle-substituted fluorescein dyes and methods in which the dyes are conjugated to substrates and used as detection labels in molecular biology experiments. The electron-deficient nitrogen heterocycles include pyridine, quinoline, pyrazine, and the like. Substrates include polynucleotides, nucleosides, nucleotides, peptides, proteins, carbohydrates, and ligands.
    Type: Grant
    Filed: April 6, 2004
    Date of Patent: May 29, 2007
    Assignee: Applera Corporation
    Inventors: Krishna G. Upadhva, Steven M. Menchen, Weiguo Zhen