Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Diazine Ring Patents (Class 544/406)
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Publication number: 20130203988Abstract: The invention relates to processes of making bortezomib of formula (1) enantiomers thereof and/or intermediates thereof, comprising at least one step of coupling a carboxylic acid with an amine, wherein the coupling step is performed in a presence of the compound of formula (8), wherein A is C1-C6 alkyl group, preferably wherein A is n-propyl group.Type: ApplicationFiled: October 14, 2010Publication date: August 8, 2013Applicant: Synthon BVInventors: Jakub Castulik, Miroslav Zabadal
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Publication number: 20130197226Abstract: The present invention features pharmaceutical compositions and methods of using the pharmaceutical compositions for treating left ventricular diastolic dysfunction. In particular, the pharmaceutical compositions include an apolipoprotein complex comprising a lipid fraction and a protein fraction.Type: ApplicationFiled: July 19, 2011Publication date: August 1, 2013Inventors: Jean-Claude Tardif, David Busseuil, Éric Rhéaume
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Patent number: 8497374Abstract: A synthetic process for producing bortezomib comprising converting racemic boronic esters, such as the pinacol ?-aminoboronic ester, into mixtures of diastereomers [6] by reaction with a suitably protected L-phenylalanine derivative (see Scheme 3), such as N—BOC-L-phenylalanine. The protecting group of the L-phenylalanine moiety is then removed, such as by reacting the diastereomers [6] with an acid, such as hydrochloric acid, to form a mixture of amine salt diastereomers [7] which is then subjected to conditions under which the desired diastereomer (R,S)-[7] is selectively isolated, such as by crystallization, chromatography or stereoselective hydrolysis. The separated desired diastereomer (R,S)-[7] is then converted into bortezomib or bortezomib anhydride.Type: GrantFiled: May 12, 2011Date of Patent: July 30, 2013Assignee: Scinopharm Taiwan, Ltd.Inventors: Julian Paul Henschke, Aiping Xie, Xin Yan Huang, Yung Fa Chen
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Publication number: 20130172367Abstract: Novel 2-alkylcycloalk(en)ylcarboxamides of the formula (I) in which X, s, R1, L, R2 and A are as defined in the description, a plurality of processes for preparing these compounds and their use for controlling unwanted microorganisms, and also novel intermediates and their preparation.Type: ApplicationFiled: November 27, 2012Publication date: July 4, 2013Applicant: BAYER CROPSCIENCE AGInventor: Bayer CropScience AG
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Publication number: 20130149249Abstract: The present invention provides novel in vivo imaging agents useful for detecting the presence of mycobacteria using in vivo imaging methods. Also provided by the present invention is a precursor compound useful in the synthesis of the in vivo imaging agents of the invention, and a method to obtain the in vivo imaging agent of the invention using said precursor compound. Methods of in vivo imaging and diagnosis in which the in vivo imaging agent of the invention finds use are also provided.Type: ApplicationFiled: August 22, 2011Publication date: June 13, 2013Applicant: GE HEALTHCARE LIMITEDInventors: Vijaya Raj Kuniyil Kulangara, Ravi Hegde
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Publication number: 20130137635Abstract: This invention relates to tryptophan hydroxylase inhibitors, compositions comprising them, and methods of their use for the treatment, management and/or prevention of metastatic bone disease.Type: ApplicationFiled: February 9, 2011Publication date: May 30, 2013Applicant: LEXICON PHARMACEUTICALS, INC.Inventor: Arthur Thomas Sands
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Publication number: 20130109665Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament. In particular, the compound may be used as a preferential agonist of Cannabinoid Receptor 2.Type: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130072679Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A1, A2 and A3 are as described herein, compositions including the compounds and methods of using the compounds. These compounds are useful for therapy or prophylaxis in a mammal, and in particular as aldosterone synthase (CYP11B2 or CYP11B1) inhibitors for the treatment or prophylaxis of chronic kidney disease, congestive heart failure, hypertension, primary aldosteronism and Cushing syndrome.Type: ApplicationFiled: September 13, 2012Publication date: March 21, 2013Inventors: Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Henner Knust, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Alexander V. Mayweg, Peter Mohr, Xuefei Tan, Mingwei Zhou
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Patent number: 8389767Abstract: The invention relates to methods of using certain compounds of formula (I), (II) and (III) in the synthesis of an insecticide intermediate of formula (IV), wherein the substituents are as defined in claim 1, to processes for preparing these compounds, to processes which use these compounds to prepare insecticide intermediates, and to certain novel compounds of formula (II?) and (III?).Type: GrantFiled: September 2, 2008Date of Patent: March 5, 2013Assignee: Syngenta Crop Protection LLCInventors: Andre Denis Stoller, Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Peter Maienfisch, Werner Zambach
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Publication number: 20130040389Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 5, 2012Publication date: February 14, 2013Applicant: Intrexon CoporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20130035487Abstract: The present invention relates to non-steroidal ligands for use in nuclear receptor-based inducible gene expression system, and a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising: the exogenous gene and a response element; wherein the exogenous gene is under the control of the response element and binding of the DNA binding domain to the response element in the presence of the ligand results in activation or suppression of the gene.Type: ApplicationFiled: September 5, 2012Publication date: February 7, 2013Applicant: Intrexon CorporationInventors: Robert Eugene HORMANN, David W. Potter, Orestes Chortyk, Colin M. Tice, Glenn Richard Carlson, Andrew Meyer, Thomas R. Opie
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Publication number: 20130023660Abstract: Disclosed are carboxamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment is a compound having the structure in which R1, R2, R3, R4, D, J, Z, T, p, q, w and x are as described herein. In certain embodiments, a compound disclosed herein activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.Type: ApplicationFiled: September 18, 2012Publication date: January 24, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Hui Hong, Ihab S. Darwish, Xiang Xu, Rajinder Singh
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Publication number: 20120330015Abstract: The present invention relates to a process for the preparation of a compound of the general Formula (I), comprising: a) reacting a compound of the general Formula (II) with a compound of the Formula III R2COOH and a compound of the general Formula IV R3NC under such conditions that compound I is formed, wherein R1 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R2 represents a substituted or unsubstituted alkyl, alkenyl, alkynyl, aromatic or non-aromatic, mono-, di- or tricyclic, or heterocyclic structure, and R3 represents a substituted or unsubstituted alkyl, alkenyl, or alkynyl structure. In further aspect the subject invention relates to the use of the obtained products as intermediates for various peptidomimetics, and preferably as a building block in a convergent synthesis of prolyl dipeptide structures.Type: ApplicationFiled: September 16, 2010Publication date: December 27, 2012Applicant: Vereniging voor Christelijk hoger onderwijs, wetenschappelijk onderzoek en patientenzorgInventors: Eelco Ruijter, Romano Orru, Anass Znabet, Marloes Polak, Nicholas Turner
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Publication number: 20120309833Abstract: The present invention relates to analogs of bexarotene and methods of use thereof.Type: ApplicationFiled: February 17, 2011Publication date: December 6, 2012Inventors: Carl E. Wagner, Peter W. Jurutka, Pamela A. Marshall, Arjan van der Vaart
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Publication number: 20120289520Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesityType: ApplicationFiled: April 25, 2012Publication date: November 15, 2012Applicant: ASTRAZENECA ABInventors: Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
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Patent number: 8299246Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: March 6, 2012Date of Patent: October 30, 2012Assignee: AstraZeneca ABInventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Patent number: 8293899Abstract: The present invention relates to a process for preparing stereoisomerically enriched 3-heteroaryl-3-hydroxycarboxylic esters by reducing 3-heteroaryl-3-oxocarboxylic esters in the presence of ruthenium-containing catalysts.Type: GrantFiled: February 27, 2003Date of Patent: October 23, 2012Assignee: Lanxess Deutschland GmbHInventors: Boris Bosch, Markus Eckert, Hans-Christian Militzer, Claus Dreisbach
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Patent number: 8283383Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: GrantFiled: June 22, 2010Date of Patent: October 9, 2012Assignee: Roche Palo Alto LLCInventors: Chris Allen Broka, Ronald Charles Hawley
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Patent number: 8283349Abstract: A compound of general formula (I): A process for preparing this compound. A fungicidal composition comprising a compound of general formula (I). A method for treating plants by applying a compound of general formula (I) or a composition comprising it.Type: GrantFiled: February 21, 2008Date of Patent: October 9, 2012Assignee: Bayer Cropscience AGInventors: Pierre-Yves Coqueron, Rüdiger Fischer, Oliver Gaertzen, Marie-Claire Grosjean-Cournoyer, Benoît Hartmann, Klaus Kunz, Darren Mansfield, Amos Mattes, Oswald Ort, Philippe Desbordes
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Publication number: 20120252809Abstract: The present invention relates to compounds of the formula I, wherein A, D, E, L, G, R10, R30, R40, R50 and R60 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. They are inhibitors of the protease cathepsin A, and are useful for the treatment of diseases such as atherosclerosis, heart failure, renal diseases, liver diseases or inflammatory diseases, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: January 24, 2012Publication date: October 4, 2012Applicant: SANOFIInventors: Sven RUF, Thorsten SADOWSKI, Klaus WIRTH, Herman SCHREUDER, Christian BUNING
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Patent number: 8269045Abstract: Substituted pyrazinecarboxylic acid anilide derivatives represented by the general formula (I) or salts thereof; intermediates of them; pesticides (such as insecticides and acaricides) for agricultural and horticultural use, containing the compounds as the active ingredient; and usage thereof: wherein R1 is H, C1-6 alkyl, halo C1-6 alkyl, or the like; R2 is halogeno, C1-6 alkyl, or the like; G is C2-10 alkyl or the like; Z is oxygen or sulfur; X's are each independently H, halogeno, or the like; Y's are each independently H, halogeno, cyano, or the like; and m and n are each an integer of 1 to 3.Type: GrantFiled: July 29, 2010Date of Patent: September 18, 2012Assignee: Nihon Nohyaku Co., Ltd.Inventors: Takashi Furuya, Kozo Machiya, Akiyuki Suwa, Shinsuke Fujioka
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Publication number: 20120225891Abstract: A compound represented by Formula (1): The compound can be used as insecticides.Type: ApplicationFiled: March 22, 2012Publication date: September 6, 2012Applicant: MITSUI CHEMICALS, INC.Inventors: Kei Yoshida, Takeo Wakita, Hiroyuki Katsuta, Akiyoshi Kai, Yutaka Chiba, Kiyoshi Takahashi, Hiroko Kato, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido, Junji Maki, Shinichi Banba
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Patent number: 8247552Abstract: Compounds represented by the following structure (II) are disclosed: as are methods for making such compounds. Compositions and methods for treating various disease conditions including cancer and non-cancer diseases associated with vascular proliferation are also disclosed.Type: GrantFiled: April 4, 2011Date of Patent: August 21, 2012Assignee: Nereus Pharmaceuticals, Inc.Inventors: Michael Palladino, George Kenneth Lloyd, Yoshio Hayashi
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Publication number: 20120201763Abstract: The present invention relates to the discovery that certain non-naturally occurring, non-peptide amide compounds and amide derivatives, such as oxalamides, ureas, and acrylamides, are useful flavor or taste modifiers, such as a flavoring or flavoring agents and flavor or taste enhancer, more particularly, savory (the “umami” taste of monosodium glutamate) or sweet taste modifiers, —savory or sweet flavoring agents and savory or sweet flavor enhancers, for food, beverages, and other comestible or orally administered medicinal products or compositions.Type: ApplicationFiled: December 23, 2011Publication date: August 9, 2012Applicant: SENOMYX, INC.Inventors: Catherine Tachdjian, Andrew P. Patron, Sara L. Adamski-Werner, Farid Bakir, Qing Chen, Vincent Darmohusodo, Stephen Terrence Hobson, Xiaodong Li, Ming Qi, Daniel H. Rogers, Marketa Rinnova, Guy Servant, Xiao-Qing Tang, Mark Zoller, Daivd Wallace, Amy Xing, Klaus Gubernator
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Publication number: 20120190686Abstract: The present invention provides bicyclo[3.2.1]octyl amide derivatives of formula (I): wherein L, R1 and R2 are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods using the same.Type: ApplicationFiled: December 22, 2011Publication date: July 26, 2012Applicant: H. LUNDBECK A/SInventors: Guiying Li, Hao Zhou, Jesse Weiss, Dario Doller, James Ford Burns
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Patent number: 8217048Abstract: The present invention relates to compounds that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: June 28, 2010Date of Patent: July 10, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Robert B. Perni, John J. Court, Shawn D. Britt, Janos Pitlik, John H. van Drie
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Patent number: 8211896Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.Type: GrantFiled: October 1, 2010Date of Patent: July 3, 2012Assignee: Chemocentryx, Inc.Inventors: Solomon Ungashe, Zheng Wei, J. J. Wright, Andrew Pennell
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Publication number: 20120157476Abstract: The present invention relates to compounds of the formula wherein A1 to A3 and R1 to R9 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: December 8, 2011Publication date: June 21, 2012Inventors: Paul Hebeisen, Stephan Roever
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Publication number: 20120135975Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, Alzheimer's disease, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia.Type: ApplicationFiled: May 14, 2007Publication date: May 31, 2012Applicant: MERCK & CO., INC.Inventors: Vincent J. Colandrea, William K. Hagmann, Jeffrey J. Hale, Irene E. Whitney
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Patent number: 8188093Abstract: The present invention relates to a method of raising HDL cholesterol comprising administering to a patient in need thereof a compound of the formula wherein A, G, R1 to R8 and R17 are as defined in the description.Type: GrantFiled: June 29, 2010Date of Patent: May 29, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Mirjana Andjelkovic, Agnes Benardeau, Evelyne Chaput, Paul Hebeisen, Matthias Nettekoven, Ulrike Obst Sander, Constantinos G. Panousis, Stephan Roever
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Patent number: 8188092Abstract: DGAT-1 inhibitor compounds of formula (I), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, r is 0 or 1 and X1 is linear (1-3C)alkyl; q is 0 or 1 and X2 is fluoro, chloro or (1-3C)alkyl; Y1 is selected from fluoro, chloro, bromo, cyano, (1-3C)alkyl and (1-2C)alkoxy; n is 0, 1 or 2 and Y2 is fluoro, chloro or (1-3C)alkyl; p is 0, 1 or 2 and Y3 is (1-3C)alkyl or forms a (3-5C)cycloalkyl ring; Z is carboxy or —CONHSO2Me or —CONRbRc wherein Rb and Rc are independently selected, for example, from hydrogen and (1-4C)alkyl or Rb and Rc are linked so as to form a morpholine ring or a (4-6C)heterocyclic ring and when Z is —CONRbRc the Rb and Rc groups may be optionally substituted by carboxy.Type: GrantFiled: June 18, 2010Date of Patent: May 29, 2012Assignee: AstraZeneca ABInventors: Alan Martin Birch, Roger John Butlin, Leonie Campbell, Clive Green, Andrew Leach, Michael James Waring, Paul Michael Murray, Per Olof Ryberg
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Publication number: 20120115726Abstract: The present invention relates to 6,6-dioxo-6-thia-1,4-diaza-naphthalene derivatives of formula (I) where R1, R2, R3a, R3b, R4 and R5 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for making compounds of formula (I), to herbicidal compositions comprising compounds of formula (I) and to methods of using compounds of formula (I) to control plant growth.Type: ApplicationFiled: May 6, 2010Publication date: May 10, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Nigel James Willetts, Nicholas Phillip Mulholland, Paul Anthony Worthington, Alaric James Avery
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Publication number: 20120108611Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: ApplicationFiled: December 29, 2011Publication date: May 3, 2012Inventors: Jean-Michel Altenburger, Valérie Fossey, Gilbert Lassalie, Frédéric Petit, Jean Claude Vernieres, Philip Janiak
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Publication number: 20120108602Abstract: DGAT-1 inhibitor compounds of formula (1), pharmaceutically-acceptable salts and pro-drugs thereof are described, together with pharmaceutical compositions, processes for making them and their use in treating, for example, obesity wherein, for example, Ring A is optionally substituted 2,6-pyrazindiyl; X is ?0; Ring B is optionally substituted 1,4-phenylene; Y1 is a direct bond or —O—; Y2 is —(CH2)r— wherein r is 2 or 3; n is 0 or n is 1 when Y1 is a direct bond between Ring B and Ring C and when Ring B is 1,4-phenylene and Ring C is (4-6C)cycloalkane; Ring C is optionally substituted (4-6C)cycloalkane, (7-10C)bicycloalkane, (8-12C)tricycloalkane, phenylene or pryidindiyl; L is a direct bond or —O—; p is 0, 1 or 2 and when p is 1 or 2 RA1 and RA2 are each independently hydrogen or (1-4C)alkyl; Z is carboxy or a mimic or bioisostere thereof.Type: ApplicationFiled: May 5, 2011Publication date: May 3, 2012Applicant: AstraZeneca ABInventors: Udo Andreas BAUER, Jonas Gunnar BARLIND, Petra JOHANNESSON, Jan Magnus JOHANSSON, Alexander Tobias NOESKE, Annika Ulrika PETERSSON, Alan Martin BIRCH, Roger John BUTLIN, Clive GREEN, Andrew LEACH, Ragnar HOVLAND
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Patent number: 8168654Abstract: Compounds of formula I in salt or zwitterionic form wherein, wherein R1, R2, R3, and R4 have the meanings as indicated in the specification, are useful for treating conditions that are mediated by the muscarinic M3 receptor. Pharmaceutical compositions that contain the compounds and a process for preparing the compounds are also described.Type: GrantFiled: October 20, 2009Date of Patent: May 1, 2012Assignee: Novartis AGInventors: Stephen P Collingwood, Brian Cox, Urs Baettig, Gurdip Bhalay, Nicholas J Devereux
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Patent number: 8163905Abstract: The present invention relates to pyrazinone derivatives of formula (I): wherein R1, R2, R3, R4, R5, R6 and R7 are as herein defined; processes for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: June 26, 2008Date of Patent: April 24, 2012Assignee: AstraZeneca ABInventors: Stephen Brough, Richard Evans, Timothy Jon Luker, Piotr Raubo
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Publication number: 20120094971Abstract: This invention relates to compounds of Formula (I) wherein Cy1, L1, Y, R1, L2, and Ar2 are defined herein, for the treatment of cancers, inflammatory disorders, and neurological conditions.Type: ApplicationFiled: September 3, 2009Publication date: April 19, 2012Applicant: REPLIGEN CORPORATIONInventors: James R. Rusche, Norton P. Peet, Allen T. Hopper
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Publication number: 20120088740Abstract: The invention relates to compositions and co-crystals each comprising VX-950 and a co-crystal former selected from the group consisting of salicylic acid, 4-amino salicylic acid, and oxalic acid. Also within the scope of this invention are methods of making and using the same.Type: ApplicationFiled: October 10, 2011Publication date: April 12, 2012Applicant: Vertex Pharmaceuticals IncorporatedInventors: Patrick R. Connelly, Sherry Collier, Michael Tauber
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120065064Abstract: Compounds of the formula (I) wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: December 12, 2009Publication date: March 15, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: John Benjamin Taylor, Jeffrey Steven Wailes, Stephane André Marie Jeanmart, Mangala Govenkar
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Patent number: 8119635Abstract: Compounds of formula I pharmaceutical compositions of these compounds, and use of said compositions to control synaptic transmission in mammals.Type: GrantFiled: August 19, 2009Date of Patent: February 21, 2012Assignee: Abbott LaboratoriesInventors: Michael R. Schrimpf, Karin R. Tietje, Richard B. Toupence, Jianguo Ji, Anwer Basha, William H. Bunnelle, Jerome F. Daanen, Jennifer M. Frost, Kevin B. Sippy
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Patent number: 8110579Abstract: The present invention relates to derivatives of 5,6-bisaryl-2-pyridine-carboxamide, their preparation and their application in therapeutics as antagonists of urotensin II receptors.Type: GrantFiled: February 11, 2009Date of Patent: February 7, 2012Assignee: Sanofi-AventisInventors: Jean-Michel Altenburger, Valerie Fossey, Philip Janiak, Gilbert Lassalle, Frederic Petit, Jean Claude Vernieres
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Publication number: 20120015961Abstract: The present invention provides, for example, a compound of the following formula (I): wherein R1 is substituted amino and the like, R2 is halogen and the like, R3 is substituted or unsubstituted lower alkyl and the like, RA and RB are each independently hydrogen, substituted or unsubstituted lower alkyl and the like, RC and RD are each independently hydrogen, substituted or unsubstituted lower alkyl, or RC and RD together with the carbon atom to which they are attached may form a substituted or unsubstituted carbocycle, and ring A is a carbocycle or a heterocycle, its pharmaceutically acceptable salt, or a solvate thereof as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-?proteins.Type: ApplicationFiled: March 29, 2010Publication date: January 19, 2012Applicant: SHIONOGI & CO., LTD.Inventors: Yuusuke Tamura, Shinji Suzuki, Sae Matsumoto, Akihiro Hori, Yuuji Kooriyama
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Publication number: 20120010219Abstract: The invention features salvinorin compositions that are selective for kappa opioid receptors; methods of treating mania by using a selective kappa receptor agonist; and methods of treating mood disorders, such as depressive disorders and manic disorders, using salvinorin compositions.Type: ApplicationFiled: December 14, 2009Publication date: January 12, 2012Applicant: The McLean Hospital CorporationInventors: Cecile Beguin, Justin Stephen Potuzak, Thomas Anthony Munro, Katherine K. Duncan, William A. Carlezon, Bruce M. Cohen, Lee-yuan Liu Chen
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Publication number: 20110319398Abstract: The disclosure relates to compounds and methods of inhibiting type three secretion system effector molecules, to methods of detecting compounds that inhibit Yops translocation, and to methods of treating or preventing infections by administering compounds described herein to a subject in need thereof.Type: ApplicationFiled: June 1, 2011Publication date: December 29, 2011Applicant: TUFTS UNIVERSITYInventor: Joan Mecsas
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Publication number: 20110319411Abstract: Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.Type: ApplicationFiled: December 8, 2009Publication date: December 29, 2011Applicant: Sirtis Pharmaceuticals, Inc.Inventors: Chi B. Vu, Lauren Mcpherson, Pui Yee Ng, Charles Blum
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Publication number: 20110301178Abstract: This present disclosure is related to the field of pyrazine carboxamides and their derivatives and the use of these compounds as fungicides.Type: ApplicationFiled: May 31, 2011Publication date: December 8, 2011Applicant: DOW AGROSCIENCES LLCInventors: Kristy Bryan, George E. Davis, Paul R. Graupner, Beth Lorsbach, W. John Owen, Francis E. Tisdell
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Patent number: 8071606Abstract: The present invention provides compounds of Formula (I) that act as glucokinase activators; pharmaceutical compositions thereof; and methods of treating diseases, disorders, or conditions mediated by glucokinase. The variables R1, R2, R3 and R4 are as described herein.Type: GrantFiled: January 20, 2010Date of Patent: December 6, 2011Assignee: Pfizer Inc.Inventors: John William Benbow, Jeffrey Allen Pfefferkorn
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Patent number: 8067638Abstract: The present invention is to provide a compound represented by the general formula (1) exhibiting a high insecticidal effect and an insecticide comprising the compound as an active ingredient. The compound represented by the general formula (1) and an insecticide comprising the compound as an active ingredient, wherein, in the formula, A1, A2, A3 and A4 each represent a carbon atom or the like; R1 and R2 each represent a hydrogen atom or the like; G1 and G2 represent an oxygen atom or the like; Xs each represent a hydrogen atom, a halogen atom or the like; n represents an integer of 0 to 4; Q1 represents a substituted phenyl group, a substituted heterocyclic group or the like; Q2 represents a substituted phenyl group, a substituted heterocyclic group or the like.Type: GrantFiled: June 20, 2006Date of Patent: November 29, 2011Assignee: Mitsui Chemicals, Inc.Inventors: Akiyoshi Kai, Takeo Wakita, Hiroyuki Katsuta, Kei Yoshida, Hidetaka Tsukada, Yusuke Takahashi, Nobuyuki Kawahara, Michikazu Nomura, Hidenori Daido
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Patent number: 8039623Abstract: The present invention relates to compounds of formula I: or a pharmaceutically acceptable salt or mixtures thereof that inhibit serine protease activity, particularly the activity of hepatitis C virus NS3-NS4A protease. As such, they act by interfering with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The invention further relates to compositions comprising these compounds either for ex vivo use or for administration to a patient suffering from HCV infection and to processes for preparing the compounds. The invention also relates to methods of treating an HCV infection in a patient by administering a composition comprising a compound of this invention. The invention further relates to processes for preparing these compounds.Type: GrantFiled: March 9, 2007Date of Patent: October 18, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, Robert B. Perni, Janos Pitlik