Additional Chalcogen Attached Directly Or Indirectly To The Diazine Ring By Nonionic Bonding Patents (Class 544/318)
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Patent number: 7939527Abstract: Thiazolopyridin-2-yloxy-phenyl and thiazolopyrazin-2-yloxy-phenyl amine compounds are described, which are useful as LTA4 hydrolase (LTA4H) modulators. Such compounds may be used in pharmaceutical compositions and methods for modulation of LTA4H and for the treatment of disease states, disorders, and conditions mediated by LTA4 hydrolase activity.Type: GrantFiled: April 9, 2009Date of Patent: May 10, 2011Assignee: Janssen Pharmaceutica NVInventors: Genesis M. Bacani, Diego Broggini, Eugene Y. Cheung, Christa C. Chrovian, Xiaohu Deng, Laurent Gomez, Cheryl A. Grice, Aaron M. Kearney, Adrienne M. Landry-Bayle, Alice Lee-Dutra, Jimmy T. Liang, Susanne Lochner, Neelakandha S. Mani, Alejandro Santillán, Jr., Kathleen Sappey, Kia Sepassi, Virginia M. Tanis, Alvah T. Wickboldt, John J. M. Wiener, Hartmut Zinser
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Publication number: 20110092526Abstract: A compound of formula (I): and pharmaceutically-acceptable salts thereof, wherein the variable groups are defined within; their use in the inhibition of 11?HSD1, processes for making them and pharmaceutical compositions comprising them are also described herein.Type: ApplicationFiled: October 19, 2010Publication date: April 21, 2011Applicant: ASTRAZENECA ABInventors: Stuart Norman Lile Bennett, Frederick Woolf Goldberg, Andrew Leach, Paul Robert Owen Whittamore, Pernilla Sörme
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Patent number: 7906511Abstract: The present invention has its object to study synthesis of novel cyclic compounds having a pyrimidinylalkylthio group and to find pharmacological actions of the compounds. According to the present invention, a compound represented by the formula (1) or a salt thereof is provided. In the formula, the ring X represents: R1 and R2 independently represent a hydrogen atom, an alkyl group, an aryl group, an aromatic heterocyclic group or the like; R3 represents a hydrogen atom, a halogen atom, a hydroxy group, an alkoxy group, an aryloxy group, an alkyl group, an aryl group, an amino group, an alkylamino group or the like; A1 represents a sulfur atom or the like; and A2 represents an alkylene group.Type: GrantFiled: March 31, 2006Date of Patent: March 15, 2011Assignee: Santen Pharmaceutical Co., Ltd.Inventors: Hisashi Tajima, Takahiro Honda, Kenji Kawashima, Kazuyoshi Okamoto, Minoru Yamamoto
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Patent number: 7893073Abstract: The invention relates to novel 3,4-dihydropyrimidin-2(1H)-one derivatives having the formula processes for their preparation, and their use in compositions, and in the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: GrantFiled: February 15, 2005Date of Patent: February 22, 2011Assignee: Bayer Schering Pharma AktiengesellschaftInventors: Heike Gielen-Haertwig, Barbara Albrecht, Jörg Keldenich, Volkhart Li, Josef Pernerstorfer, Karl-Heinz Schlemmer, Leila Telan
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Publication number: 20110034435Abstract: A compound of formula (A); wherein ring A is an aromatic ring or a heteroaromatic ring; R1 is independently halogen, cyano, etc., each of X1, X2 and X3 is CR2 or nitrogen, R2 is independently hydrogens, etc., n is 0, 1, 2, 3 or 4; -D-Y is —O—CH2COOH, etc, and G is a substituted amino, a substituted heterocyclic group, etc, or a pharmaceutical acceptable salt thereof, has activities of opening BK channels.Type: ApplicationFiled: April 8, 2009Publication date: February 10, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Yasuyuki Tsuzuki, Miki Hirai
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Publication number: 20110028478Abstract: The present invention provides isoxazoline FAAH inhibitors of the formula (I): or pharmaceutically acceptable forms thereof, wherein each of G, Ra, Rb, Rc, and Rd are as defined herein. The present invention also provides pharmaceutical compositions comprising a compound of formula (I), or a pharmaceutically acceptable form thereof, and a pharmaceutically acceptable excipient. The present invention also provides methods for treating an FAAH-mediated condition comprising administering a therapeutically effective amount of a compound of formula (I), or pharmaceutically acceptable form thereof, to a subject in need thereof.Type: ApplicationFiled: May 18, 2010Publication date: February 3, 2011Applicant: Infinity Pharmaceuticals, Inc.Inventors: Mark L. Behnke, Alfredo C. Castro, Lawrence K. Chan, Catherine A. Evans, Louis Grenier, Michael J. Grogan, Yves Leblanc, Tao Liu, Stephane Peluso, Daniel A. Snyder, Thomas T. Tibbitts
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Patent number: 7872012Abstract: Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia.Type: GrantFiled: December 23, 2005Date of Patent: January 18, 2011Assignee: Zhejiang Hisun Pharma Co., Ltd.Inventor: Hui Yao
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Publication number: 20110003798Abstract: The invention provides a novel class of 2,7-naphthyridin derivatives; pharmaceutical compositions comprising such compounds and methods of using such compounds to treat o prevent diseases or disorders associated with abnormal or deregulated kinase activity, particularly Syk, ZAP70, KDR, FMS, FLT*, c-Kit, RET, TrkA, TrkB, TrkC-GR-1R, Alk, c-FMS or combinations thereof.Type: ApplicationFiled: January 27, 2009Publication date: January 6, 2011Applicant: IRM LLCInventors: Barun Okram, Tetsuo Uno, Qiang Ding, Yahua Liu, Yunho Jin, Qihui Jin, Xu Wu, Jianwei Che, S. Frank Yan, Xueshi Hao
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Patent number: 7863445Abstract: Carboxylic acid derivatives where R-R6, X, Y and Z have the meanings stated in the description, and the preparation thereof, are described. The novel compounds are suitable for controlling diseases.Type: GrantFiled: August 17, 2009Date of Patent: January 4, 2011Assignee: Abbott GmbH & Co. KGInventors: Hartmut Riechers, Dagmar Klinge, Wilhelm Amberg, Andreas Kling, Stefan Muller, Ernst Baumann, Joachim Rheinheimer, Uwe Josef Vogelbacher, Wolfgang Wernet, Liliane Unger, Manfred Raschack
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Publication number: 20100317854Abstract: The invention relates to compounds of formulae (II), (IV), and (VI) as shown below, wherein the several variable groups are as defined in the specification and claims. Processes for making these materials, and methods for using them in the synthesis of compounds for treatment of cardiovascular disorders and fibrotic disorders are also disclosed.Type: ApplicationFiled: August 23, 2010Publication date: December 16, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Cristina Alonso-Alija, Markus Heil, Dietmar Flubacher, Paul Naab, Josef Pernerstorfer, Johannes-Peter Stasch, Frank Wunder, Klaus Dembowsky, Elizabeth Perzborn, Elke Stahl
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Publication number: 20100298140Abstract: Compounds of formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: September 1, 2008Publication date: November 25, 2010Applicant: SYNGENTA LIMITEDInventors: Stephane Andre Marie Jeanmart, John Benjamin Taylor, Melloney Tyte, Christopher John Mathews, Steve Smith
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Patent number: 7816528Abstract: A 2-(N-methyl-N-methanesulfonylamino)pyrimidine compound of the formula (3): [R is a hydrocarbyl group], is prepared by the steps of: (I) reacting an isobutyrylacetate ester with 4-fluorobenzaldehyde and urea in the presence of a protonic compound and a metal salt; (II) oxidizing the reaction product of the step (I); (III) reacting the oxidation product of the step (II) with an organic sulfonyl halide or an organic sulfonyl anhydride; and (IV) reacting the reaction product of the step (III) with N-methyl-N-methanesulfonamide.Type: GrantFiled: November 1, 2007Date of Patent: October 19, 2010Assignee: AstraZeneca UK LimitedInventors: Akio Matsushita, Mizuho Oda, Yasuhiro Kawachi, Jun-ichi Chika
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Patent number: 7812159Abstract: The present invention relates to processes for preparing aromatic ether compounds that are modulators of glucose metabolism and therefore useful in the treatment of metabolic disorders such as diabetes and obesity.Type: GrantFiled: January 9, 2006Date of Patent: October 12, 2010Assignee: Arena Pharamaceuticals, Inc.Inventors: Tawfik Gharbaoui, John R. Fritch, Ashwin M. Krishnan, Beverly Wolgast Throop, Naomi S. Kato
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Publication number: 20100249077Abstract: The present invention relates to novel pyridylmethyl-sulfonamide compounds of formula (I) where: n is 0 to 4; m is 0 to 4; R1 is halogen, CN, NO2, OH, SH, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy, C1-C4-haloalkoxy, etc.; and/or two radicals R1 together form a fused ring; R2 is H, C1-C4-alkyl, C1-C4-haloalkyl, C2-C4-alkenyl, C2-C4-alkynyl, C3-C8-cycloalkyl, C1-C4-alkyl-C3-C8-cycloalkyl or benzyl; R3 is halogen, CN, NO2, C1-C4-alkyl, C1-C4-haloalkyl, C1-C4-alkoxy or C1-C4-haloalkoxy; Y is —O—, C1-C4-alkanediyl, —O—CH2—, —CH2—O—, —C(NORn)—, —S—, —S(?O)—, —S(?O)2— or —N(Rn)—; and the N-oxides, and salts thereof and their use for combating phytopathogenic harmful fungi, and also to compositions and seed comprising at least one such compound.Type: ApplicationFiled: November 21, 2008Publication date: September 30, 2010Applicant: BASF SEInventors: Wassilios Grammenos, Jan Klaas Lohmann, Thomas Grote, Jochen Dietz, Bernd Mueller, Michael Puhl, Jens Renner, Sarah Ulmschneider, Marianna Vrettou, Joachim Rheinheimer
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Publication number: 20100249124Abstract: The present invention relates to compounds of formula I wherein R1a to R1c, R2, R3 and R5 are as defined in the description and claims and R4 signifies a bicyclic heteroaryl group or a cyanophenyl group, as well as pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100204163Abstract: The invention relates to derivatives and metabolites of ambrisentan, including compounds of general Formula (I) or salts, hydrates, solvates, racemates, or optical isomers thereof, wherein R1 is —H or —OCH3; R2 is —H, lower alkyl (e.g. C1-C4 alkyl) or glycosidyl; and R3 and R4 are independently —CH3, —C(O)H or —CH2OR6, wherein R6 is —H or a hydrocarbyl group having 1 to 20 carbon atoms. In some embodiments, compounds of Formula (I) exhibit selective affinity for ETA receptors and serve as endothelin receptor antagonists. In some embodiments, the compounds correspond to metabolites of ambrisentan produced by the enzymatic action of cytochrome P450 or uridine diphosphate glucuronosyl transferase enzymes, for example as elucidated in pre-clinical or clinical studies.Type: ApplicationFiled: July 31, 2008Publication date: August 12, 2010Applicant: Gilead Colorado, Inc.Inventors: Lawrence S. Melvin, JR., Martina Ullrich, Hans-Guenther Hege, Jürgen Weymann
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Publication number: 20100197680Abstract: The present application relates to novel lactam-substituted dicarboxylic acid derivatives, processes for their preparation, their use for the treatment and/or prophylaxis of diseases, and their use for producing medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: March 15, 2008Publication date: August 5, 2010Inventors: Michael Hahn, Eva-Maria Becker, Andreas Knorr, Dirk Schneider, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Frank Wunder, Dieter Lang
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Publication number: 20100197917Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.Type: ApplicationFiled: March 18, 2010Publication date: August 5, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
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Patent number: 7767811Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.Type: GrantFiled: June 5, 2006Date of Patent: August 3, 2010Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang
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Publication number: 20100190779Abstract: Compounds of formula I: wherein X, R2, R3, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: July 31, 2008Publication date: July 29, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Paul J. Edwards, Martin Poirier, Jean Rancourt, Timothy A. Stammers
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Publication number: 20100174076Abstract: Novel compounds composition capable of inhibiting TNF? and having antiimmunionflammatory and autoimmune properties useful in a pharmaceutical composition, such as for a drug containing this as an active ingredient; and a therapeutic method with the use of these novel compounds.Type: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: CHUGAI SEIYAKU KABUSHIKI KAISHAInventors: Jie Fei Cheng, Thomas Arrhenius, David Wallace, Mi Chen, Sovouthy Tith, Hirotaka Kashiwagi, Yoshiyuki Ono, Yoshiaki Watanabe
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Publication number: 20100144771Abstract: The invention provides compounds of formula (I): wherein R1 and R2 are as defined in the specification; processes for their preparation; pharmaceutical compositions containing them; a process for preparing the pharmaceutical compositions; and their use in therapy.Type: ApplicationFiled: December 2, 2009Publication date: June 10, 2010Inventors: Balint Gabos, Lena Ripa, Kristina Stenvall
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Publication number: 20100130739Abstract: Provided is a compound that has the ability to promote axonal outgrowth in combination with the ability to promote angiogenesis and can therefore be used to reduce central nerve injuries such as head injury and spinal cord injury, cerebral infarction, ischemic heart diseases such as myocardial infarction and organic angina, peripheral arterial occlusive diseases such as critical limb ischemia, or after-effects of these diseases. Specifically, the compound is represented by the following formula (I): in which Nx group is preferably a 6-membered aromatic ring containing two nitrogen atoms; R0, R1 and R2 are each independently a hydrogen atom, an alkyl group, an amino group or the like; E is an oxygen atom or an —NR8 group (wherein R8 is an alkyl group or the like); n is an integer of 0 to 5; X and Y are each a connecting bond, a cycloalkyl group, —CO— or the like; and Q is a hydrogen atom or a phenyl group.Type: ApplicationFiled: April 25, 2008Publication date: May 27, 2010Applicant: ASUBIO PHARMA CO., LTD.Inventors: Naohiro Takemoto, Kenji Murata, Norihito Murayama, Chikaomi Yamada
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Publication number: 20100121059Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: ApplicationFiled: July 6, 2009Publication date: May 13, 2010Applicant: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Patent number: 7709494Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n, V, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.Type: GrantFiled: November 10, 2008Date of Patent: May 4, 2010Assignee: Sanofi-AventisInventors: Elisabeth Defossa, Jochen Goerlitzer, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Stefan Bartoschek
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Publication number: 20100105900Abstract: A CPT inhibitor compound is represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof: or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject having cancer comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2008Publication date: April 29, 2010Inventors: Heinz W. Pauls, Peter Brent Sampson, Bryan T. Forrest, Radoslaw Laufer, Yong Liu, Miklos Feher, Yi Yao, Guohua Pan
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Patent number: 7705008Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: GrantFiled: August 14, 2008Date of Patent: April 27, 2010Assignee: Allergan, Inc.Inventors: David W. Old, Danny T. Dinh
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Patent number: 7687500Abstract: Oxetane-containing nucleosides, particularly non-reducing psiconucleoside oxetanes are described herein. Therapeutic application of these oxetane compounds toward the treatment of nucleoside analog related disorders such as disorders involving cellular proliferation and infection are also described.Type: GrantFiled: January 24, 2008Date of Patent: March 30, 2010Assignee: The University of ConnecticutInventors: Amy R. Howell, Rosa C. Taboada, Stewart K. Richardson
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Patent number: 7687511Abstract: The present invention is directed in part towards methods of modulating the function of calcium channels with pyrimidine-based compounds. In addition, the invention describes methods of preventing and treating calcium channel-related abnormal conditions in organisms with a compound identified by the invention. Furthermore, the invention pertains to pyrimidine-based compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: November 12, 2007Date of Patent: March 30, 2010Inventors: Phani Kumar Pullela, Paramashivappa Rangappa, Srinivasa Rao Alapati, Pillarisetti V. Subbarao
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Patent number: 7659272Abstract: The invention relates to compounds represented by Structural Formula I, which can bind to CCR9 receptors and block the binding of a ligand (e.g., TECK) to the receptors. The invention also relates to a method of inhibiting a function of CCR9, and to the use compounds represented by Structural Formula I in research, therapeutic, prophylactic and diagnostic methods.Type: GrantFiled: October 16, 2007Date of Patent: February 9, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Paul Fleming, Geraldine C. B. Harriman, Zhan Shi, Chen Shaowu
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Patent number: 7655649Abstract: The present invention is directed to compounds which contain substituted pyridazines and pyrimidines moieties which inhibit the activity of Akt, a serine/threonine protein kinase. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for treating cancer comprising administration of the compounds of the invention.Type: GrantFiled: April 5, 2005Date of Patent: February 2, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Mark T. Bilodeau, Peter C. Chua, Nicholas D. P. Cosford, Jacob M. Hoffman, Johnny Yasuo Nagasawa
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Publication number: 20100022537Abstract: This invention relates to novel heterocyclic derivatives, processes for their preparation, and their use in medicaments, especially for the treatment of chronic obstructive pulmonary diseases, acute coronary syndrome, acute myocardial infarction and heart failure development.Type: ApplicationFiled: July 27, 2009Publication date: January 28, 2010Applicant: Bayer Healthcare AGInventors: Heike Gielen-Haertwig, Volkhart Min-Jian Li, Ulrich Rosentreter, Karl-Heinz Schlemmer, Swen Allerheiligen, Leila Telan, Lars Bärfacker, Jörg Keldenieh, Mary F. Fitzgerald, Kevin Nash, Barbara Albrecht, Dirk Meurer
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Patent number: 7652010Abstract: Azabicyclo pyridazinyl compounds including azabicyclooctyl-pyridazinyl-oxy compounds, which are found to be cholinergic ligands at the nicotinic acetylcholine receptors and modulators of the monoamine receptors and transporters. Due to their pharmacological profile, the compounds may be used for the treatment of various diseases or disorders, including those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: October 14, 2005Date of Patent: January 26, 2010Assignee: Neurosearch A/SInventors: Dan Peters, Daniel B. Timmermann, Gunnar M. Olsen, Elsebet Østergaard Nielsen, Tino Dyhring Jørgensen
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Publication number: 20090318481Abstract: This application relates to a substituted hydroxyphenyl ketone compound of formula I, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof and its use in treating migraine. This application also relates to processes for preparing a compound of formula I, and intermediate compounds useful therein.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Thomas Daniel AICHER, Guillermo S. CORTEZ, Todd Michael GROENDYKE, Albert KHILEVICH, James Allen KNOBELSDORF, Fredrik Pehr MARMSATER, Jeffrey Michael SCHKERYANTZ, Tony Pisal TANG
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Patent number: 7557138Abstract: Compositions of matter comprising 5-phenoxyalkoxypsoralen compounds and their method of synthesis and use. The compounds are useable to treat diseases or disorders in human or animal subjects, including autoimmune diseases. The compounds inhibit potassium channels, including the Kv1.3 channel and at least some of the therapeutic effects of such compounds may be due at least in part to potassium channel inhibition. In some embodiments, the compounds are more selective for certain potassium channels (e.g., Kv1.3 channels) than other potassium channels (e.g., Kv1.5 channels).Type: GrantFiled: October 4, 2004Date of Patent: July 7, 2009Assignee: The Regents of the University of CaliforniaInventors: Heike Wulff, Ananthakrishnan Sankaranarayanan, Wolfram Haensel, Alexander Schmitz, Kristina Schmidt-Lassen
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Publication number: 20090149486Abstract: This invention relates to a compound of formula I, wherein R1, R2, m, n, V, W, X and Y are as defined herein, or a physiologically tolerated salt thereof, its pharmaceutical composition and use for lowering blood glucose, treating diabetes, or increasing insulin release.Type: ApplicationFiled: November 10, 2008Publication date: June 11, 2009Applicant: SANOFI-AVENTISInventors: Elisabeth Defossa, Jochen Goerlitzer, Thomas Klabunde, Viktoria Dietrich, Siegfried Stengelin, Guido Haschke, Andreas Herling, Stefan Bartoschek
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Patent number: 7538072Abstract: A stem/leaf desiccant for crop plants which comprises as an active ingredient, a compound of formula (I): wherein X represent CH or nitrogen; Z represents halogen; A represents oxygen, sulfur, or NH; R1 represents hydroxyl, C1-C7 alkoxy, C3-C7 alkenyloxy, C3-C7 alkynyloxy, C5-C7 cycloalkoxy, {(C1-C7 alkoxy)carbonyl} C1-C3 alkoxy, (C1-C7 alkylamino)oxy, {di(C1-C7 alkyl)amino}oxy, (C3-C7 alkylideneamino)oxy, C1-C7 alkylamino, di(C1-C7 alkyl)amino, C3-C7 alkenylamino, C3-C7 alkynylamino, C5-C7 cycloalkylamino, {(C1-C7 alkoxy)carbonyl} C1-C3 alkylamino, or (C1-C7 alkoxy)amino; R2 is hydrogen or methyl; and R3 is hydrogen, halogen, C1-C3 alkyl, or C1-C3 alkoxy; a method for desiccating a crop plant and a method for harvesting a crop by using the stem/leaf desiccant.Type: GrantFiled: June 16, 2006Date of Patent: May 26, 2009Assignee: Sumitomo Chemical Company, LimitedInventor: Nobuaki Mito
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Patent number: 7534885Abstract: A process is disclosed for the stereo-selective preparation of emtricitabine, which allows the desired product to be obtained in good yield and without the use of chromatographic techniques. The process for the production of emtricitabine of the formula (Ia) is characterized by the formation and isolation of intermediate compounds of formula (XIa) in salified form. Emtricitabine is a known antiviral drug.Type: GrantFiled: March 19, 2004Date of Patent: May 19, 2009Assignee: Archimica S.r.l.Inventors: Giorgio Bertolini, Maurizio Deleo, Marco Frigerio, Massimo Losa, Maurizio Velati
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Patent number: 7511149Abstract: Insecticidal sulfoximines are produced efficiently and in high yield by the oxidation of the corresponding sulfilimine with ruthenium tetraoxide or an alkali metal permanganate.Type: GrantFiled: February 9, 2007Date of Patent: March 31, 2009Assignee: Dow AgroSciences LLCInventors: Kim E. Arndt, Douglas C. Bland, David E. Podhorez, James R. McConnell
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Publication number: 20090069309Abstract: Compounds comprising or a pharmaceutically acceptable salt or a prodrug thereof is disclosed herein. A, X, J, E, and Z are as described herein. These compounds are useful for treating diseases.Type: ApplicationFiled: August 14, 2008Publication date: March 12, 2009Applicant: ALLERGAN, INC.Inventors: David W. Old, Danny T. Dinh
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Publication number: 20090069353Abstract: The present application describes deuterium-enriched ambrisentan, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: ApplicationFiled: August 21, 2008Publication date: March 12, 2009Applicant: Protia, LLCInventor: Anthony W. Czarnik
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Patent number: 7498327Abstract: The present invention provides a compound of formula I and the use thereof for the therapeutic treatment of disorders relating to or affected by the 5-HT6 receptor.Type: GrantFiled: June 22, 2005Date of Patent: March 3, 2009Assignee: WyethInventors: Youchu Wang, Chia-Cheng Shaw, Ronald Charles Bernotas, Chung-Chiee Paul Wang, Ping Cai, Zhi Wang
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Patent number: 7479558Abstract: The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.Type: GrantFiled: March 24, 2006Date of Patent: January 20, 2009Assignee: Glaxo Group LimitedInventors: James F. Callahan, Jeffrey C. Boehm, Zehong Wan, Hongxing Yan, Xichen Lin
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Publication number: 20080318959Abstract: The present invention describes novel methods of identifying compounds which inhibit HIV particle formation and Rev-dependent HIV production. The present invention also provides methods and compounds for inhibiting HIV particle formation and or treating patients infected with HIV.Type: ApplicationFiled: February 1, 2005Publication date: December 25, 2008Inventors: David Rekosh, Marie-Louise Hammarskjold
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Publication number: 20080293684Abstract: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: July 26, 2005Publication date: November 27, 2008Inventors: Anthony B Pinkerton, Jean-Michel Vernier, Rowena V. Cube, John H. Hutchinson, Dehua Huang, Celine Bonnefous, Steven P. Govak, Theodore Kamenecka
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Publication number: 20080280930Abstract: Disclosed are pyrimidinone compounds having formula (I), a preparation and use thereof. The compounds are inhibitors of HMG-CoA reductase, and therefore have antivirus activities and are useful for preventing and treating cardiovascular and cerebrovascular disorders, senile dementia, diabetes mellitus, osteoporosis and tumors, and enhancing immune functions in a subject, and especially useful for treating diseases associated with hyperlipaemia.Type: ApplicationFiled: December 23, 2005Publication date: November 13, 2008Applicants: ZHEJIANG HISUN PHARMA. CO., LTDInventor: Hui Yao
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Patent number: 7414011Abstract: Disclosed are compounds of the formula (I) or salts thereof in which R1, R2, R3, R4, I, R5, Q, R4, W, X, Y, V and Z, are as defined in the specification, which are suitable for use as herbicides or plant growth regulators. Also disclosed are processes for preparing the compounds of formula (I) or salts thereof.Type: GrantFiled: September 12, 2005Date of Patent: August 19, 2008Assignee: Hoechst Schering Agrevo GmbHInventors: Hansjörg Dietrich, Christian Waldraff, Lothar Willms, Hermann Bieringer, Christopher Rosinger, Felix Thürwächter, Thomas Auler
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Publication number: 20080194586Abstract: Fused aromatic compounds of Formula (I) are PPAR gamma agonists or partial agonists and are useful in the treatment or control of type II diabetes, including hyperglycemia, dylipidermia, hyperlipidemia, hypercholesterolemia, hypertriglyceridemia, and obesity that are often associated with type 2 diabetes.Type: ApplicationFiled: March 3, 2006Publication date: August 14, 2008Inventors: Harold B. Wood, Peter T. Meinke, Guo Q. Shi, Yong Zhang
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Publication number: 20080167307Abstract: According to the present invention, a compound represented by the following formula (I) having a superior PPAR? agonist action and concurrently showing a hypolipidemic action can be provided, and further, a compound useful as a synthetic intermediate for the compound can be provided.Type: ApplicationFiled: November 4, 2005Publication date: July 10, 2008Applicant: Mitsubishi Phama CorporationInventors: Takashi Tozawa, Osamu Tsuruta, Hiroshi Kitajima, Yoshiyuki Aoki, Naoko Ando, Hiroki Tamakawa
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Patent number: 7393845Abstract: A heteroaryl derivative having the formula (I).Type: GrantFiled: June 5, 2007Date of Patent: July 1, 2008Assignee: H. Lundbeck A/SInventors: Mario Rottländer, Ejner Knud Moltzen, Ivan Mikkelsen, Thomas Ruhland, Kim Andersen, Christian Krog-Jensen