1,2,3-thiadiazoles (including Hydrogenated) Patents (Class 548/127)
  • Publication number: 20150148373
    Abstract: The invention provides heterocyclic guanidine compounds that inhibit F1F0-ATPase, and methods of using heterocyclic guanidine compounds as therapeutic agents to treat medical disorders, such as an immune disorder, inflammatory condition, or cancer.
    Type: Application
    Filed: June 7, 2013
    Publication date: May 28, 2015
    Inventors: Alexander R. Hurd, Clarke B. Taylor, Peter L. Toogood
  • Publication number: 20150133495
    Abstract: Disclosed herein is a compound of Formula I or a pharmaceutically acceptable salt thereof, in which A, G, R1 and R2 are as defined herein. The compounds and pharmaceutical compositions of the compounds are suitable for the treatment of HCV infection in mammals and are also useful to modulate or inhibit NS3/4 dimerization.
    Type: Application
    Filed: November 13, 2014
    Publication date: May 14, 2015
    Inventor: Daniel Lamarre
  • Publication number: 20150080349
    Abstract: The present invention provides compounds and methods for modulation of the quorum sensing of bacteria. In an embodiment, the compounds of the present invention are able to act as replacements for naturally occurring bacterial quorum sensing ligands in a ligand-protein binding system; that is, they imitate the effect of natural ligands and produce an agonistic effect. In another embodiment, the compounds of the present invention are able to act in a manner which disturbs or inhibits the naturally occurring ligand-protein binding system in quorum sensing bacteria; that is, they produce an antagonistic effect. The compounds of the present invention comprise N-acylated-homoserine lactones (AHLs) comprised of a wide range of acyl groups.
    Type: Application
    Filed: July 10, 2014
    Publication date: March 19, 2015
    Inventors: Helen E. BLACKWELL, Grant D. GESKE, Jennifer C. CAMPBELL
  • Publication number: 20150005320
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: January 1, 2015
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Patent number: 8921364
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Grant
    Filed: December 20, 2012
    Date of Patent: December 30, 2014
    Assignee: Rhizen Pharmaceuticals SA
    Inventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri Swaroop Merikapudi, Swaroop Kumar V. S. Vakkalanka
  • Publication number: 20140378681
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Application
    Filed: February 26, 2013
    Publication date: December 25, 2014
    Applicant: Siga Technologies Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey, Jack H. Nunberg, Celestine Johnson Thomas
  • Patent number: 8895741
    Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: November 25, 2014
    Assignee: Melinta Therapeutics, Inc.
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Patent number: 8846727
    Abstract: A new class of haloalkyl heteroaryl benzamides is described. These compounds show strong activity against hepatitis viruses.
    Type: Grant
    Filed: May 11, 2010
    Date of Patent: September 30, 2014
    Assignee: Romark Laboratories, L.C.
    Inventors: Jean-Francois Rossignol, J. Edward Semple
  • Patent number: 8841332
    Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogs, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Grant
    Filed: July 30, 2009
    Date of Patent: September 23, 2014
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Publication number: 20140256771
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: October 19, 2012
    Publication date: September 11, 2014
    Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
  • Publication number: 20140249163
    Abstract: The present disclosure describes new inhibitors or antagonists of Ras useful for the treatment of conditions resulting from Ras-induced or mediated cellular processes, including cellular proliferation, differentiation, apoptosis, senescence, and survival. These cellular processes may be associated with a non-malignant or malignant disease, disorder, or pathological condition. The present disclosure also describes a method for inhibiting such Ras-induced or mediated cellular processes. The method entails administering a Ras antagonist in an amount effective to inhibit such cellular processes.
    Type: Application
    Filed: October 5, 2012
    Publication date: September 4, 2014
    Applicant: PICES THERAPEUTICS LLC
    Inventors: James H. Wikel, Michael J. Brownstein
  • Publication number: 20140242120
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein Y, L, A, W1, W2, and R?1 are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 8, 2014
    Publication date: August 28, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Shoujun Chen, Lijun Sun, Yu Xie
  • Publication number: 20140221357
    Abstract: The present invention provides compounds of Formula (I) or Formula (III): [INSERT CHEMICAL STRUCTURE HERE] (I) [INSERT CHEMICAL STRUCTURE HERE] (III) as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Application
    Filed: September 25, 2012
    Publication date: August 7, 2014
    Applicant: Bristol-Myers Squibb Company
    Inventors: Lynn Abell, Leonard Adam, Cullen L. Cavallaro, Heather Finlay, Todd J. Friends, Jon J. Hangeland, Ji Jiang, R. Michael Lawrence, John Lloyd, Zulan Pi, George O. Tora, Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang
  • Patent number: 8748431
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: June 10, 2014
    Assignee: Syngenta Participations AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Publication number: 20140135331
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: May 15, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Publication number: 20140128437
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: January 10, 2014
    Publication date: May 8, 2014
    Applicants: President and Fellows of Harvard College, TRUSTEES OF BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITAL, INC., Tufts University
    Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterrev, John A. Proco, JR.
  • Publication number: 20140107134
    Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 17, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
  • Publication number: 20140039009
    Abstract: The invention relates to compounds of structural formulas (I), (VII) and (XI): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein X1, X2, X3, Y, Z, L, R1, R2, R3, R18 and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: October 15, 2013
    Publication date: February 6, 2014
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Lijun Sun, Shoujun Chen, Zhiqiang Xia, Jun Jiang, Yu Xie, Junyi Zhang
  • Publication number: 20140038987
    Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
    Type: Application
    Filed: October 8, 2013
    Publication date: February 6, 2014
    Inventors: Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stirn
  • Patent number: 8642642
    Abstract: The invention relates to compounds of the formula (I) wherein the variables have meanings given in the claims and the description. The invention also relates to the use of a compound of the formula (I) or a pharmaceutically acceptable salt thereof for preparing a medicament for the treatment of a medical disorder susceptible to the treatment with a 5HT6 receptor ligand.
    Type: Grant
    Filed: April 18, 2007
    Date of Patent: February 4, 2014
    Assignees: Abbott Laboratories, AbbVie Deutschland GmbH & Co. KG
    Inventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger, Dan Plata
  • Patent number: 8617827
    Abstract: The present invention relates to novel photoactivable rhodamine or carbopyronine derivatives of the following general formulae G1-G4 (I), G1: A1=O, A2=N, A3=C; G2: A1=S, A2=N, A3=C; G3: A1=O, A2=O, A3=N; G4: A1=S, A2=O, A3=N; comprising UV light absorbing chromophores which after photolysis by irradiation at 254-490 nm (preferably at 375-420 nm) generate fluorescent rhodamine or carbopyronine derivatives and small non-toxic fragments such as N2 or N2O. The invention also relates to methods for preparing such compounds and to the use of these compounds for optical microscopy and imaging techniques.
    Type: Grant
    Filed: September 10, 2009
    Date of Patent: December 31, 2013
    Assignee: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Stefan W. Hell, Vladimir N. Belov, Vadim P. Boyarskiy, Christian A. Wurm, Stefan Jakobs, Claudia Geisler
  • Publication number: 20130324544
    Abstract: Compounds of the formula I Formula (I) wherein the substituents are as defined in claim 1, are useful as active ingredients, which have microbiocidal activity, in particular fungicidal activity.
    Type: Application
    Filed: November 25, 2011
    Publication date: December 5, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta, Fredrik Cederbaum, Guillaume Berthon
  • Publication number: 20130317032
    Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R?1, X, X?, L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
    Type: Application
    Filed: May 16, 2013
    Publication date: November 28, 2013
    Applicant: Synta Pharmaceuticals Corp.
    Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
  • Publication number: 20130310377
    Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.
    Type: Application
    Filed: December 20, 2012
    Publication date: November 21, 2013
    Applicant: Rhizen Phamaceuticals SA
    Inventor: Rhizen Phamaceuticals SA
  • Patent number: 8580799
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.
    Type: Grant
    Filed: December 8, 2009
    Date of Patent: November 12, 2013
    Assignee: Bayer Cropscience AG
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8568756
    Abstract: Methods are provided for identifying molecules that can be used to positively and negatively manipulate quorum-sensing-mediated communication to control bacterial behavior. Small-molecule antagonists that disrupt quorum-sensing-mediated activities are identified. Methods are provided for disrupting detection of acyl-homoserine lactone autoinducer in Gram-negative bacteria by contacting the bacteria with the antagonists. Methods of inhibiting quorum sensing-mediated activity in Gram-negative bacteria are provided wherein the activity is pathogenicity, bioluminescence, siderophore production, type III secretion, or metalloprotease production.
    Type: Grant
    Filed: June 2, 2009
    Date of Patent: October 29, 2013
    Assignee: The Trustees of Princeton University
    Inventors: Bonnie Bassler, Lee Swem
  • Publication number: 20130269064
    Abstract: Novel heteroaromatic compounds of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.
    Type: Application
    Filed: November 18, 2011
    Publication date: October 10, 2013
    Applicant: SYNGENTA PARTICIPATIONS AG
    Inventors: Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
  • Publication number: 20130261158
    Abstract: The present invention relates to fungicide N-(2-phenoxyethyl)carboxamide derivatives of formula (I), their aza, thia and sila analogues, their process of preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions. Formula (1) wherein A, T, W, X, n and Z3 to Z7 represent various substituents.
    Type: Application
    Filed: July 30, 2009
    Publication date: October 3, 2013
    Inventors: Samir Bennabi, Jurgen Benting, Stephane Brunet, Philippe Desbordes, Peter Dahmen, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Rachel Rama, Philippe Rinolfi, Valerie Toquin, Arnd Voerste, Ulrike Wachendorff-Neumann
  • Patent number: 8519188
    Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: August 27, 2013
    Assignee: Marc-Henry Pitty
    Inventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, C├ęcile Bougeret
  • Publication number: 20130203818
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Application
    Filed: April 27, 2011
    Publication date: August 8, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8501946
    Abstract: The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein A is hydrogen, C1-4alkyl, C3-6cycloalkyl, C1-3alkoxy, C1-3alkoxy C1-4alkyl, C1-2fluoroalkyl, halogen, NR6R7, optionally substituted heteroaryl (Het), or optionally substituted phenyl, and R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The compounds or salts are thought to modulate P2X7 receptor function and to be capable of antagonizing the effects of ATP at the P2X7 receptor. The invention also provides the use of the compound or salt in the treatment or prophylaxis of, for example, inflammatory pain, neuropathic pain, visceral pain, rheumatoid arthritis, osteoarthritis or neurodegenerative disorders.
    Type: Grant
    Filed: April 28, 2010
    Date of Patent: August 6, 2013
    Assignee: Glaxo Group Limited
    Inventors: David Kenneth Dean, Jorge Munoz-Muriedas, Mairi Sime, Jon Graham Anthony Steadman, Rachel Elizabeth Anne Thewlis, Giancarlo Trani, Daryl Simon Walter
  • Patent number: 8487113
    Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.
    Type: Grant
    Filed: December 18, 2009
    Date of Patent: July 16, 2013
    Assignee: Farmak, A.S.
    Inventors: Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
  • Patent number: 8455497
    Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.
    Type: Grant
    Filed: February 12, 2009
    Date of Patent: June 4, 2013
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Michael R. Hale, Roger Tung, Stephen Price, Robin David Wilkes, Wayne Carl Schairer, Ashley Nicholas Jarvis, Andrew Spaltenstein, Eric Steven Furfine, Vicente Samano, Istvan Kaldor, John Franklin Miller, Michael Stephen Brieger, Ronald George Sherrill
  • Patent number: 8445525
    Abstract: The present invention relates to new substituted carboxylic acid amides of general formula wherein A, B and R1 to R5 are defined as in claim 1, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
    Type: Grant
    Filed: December 2, 2010
    Date of Patent: May 21, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Henning Priepke, Kai Gerlach, Roland Pfau, Norbert Hauel, Iris Kauffmann-Hefner, Georg Dahmann, Herbert Nar, Sandra Handschuh, Wolfgang Wienen, Annette Schuler-Metz
  • Publication number: 20130116287
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein X represents various substituents, T represents various heterocyclyl group and Het represents a pyridyl or thiazolyl group.
    Type: Application
    Filed: April 22, 2011
    Publication date: May 9, 2013
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8410145
    Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of Formula (I), to insecticidal, acaricidal, molluscicidal or nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc or nematode pests.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: April 2, 2013
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Peter Renold
  • Patent number: 8410149
    Abstract: Compounds, methods and pharmaceutical compositions for treating viral infections, by administering certain novel semicarbazides, sulfonyl carbazides, ureas and related compounds in therapeutically effective amounts are disclosed. Methods for preparing the compounds and methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment and prophylaxis of viral infections such as caused by hemorrhagic fever viruses is disclosed, i.e., including but not limited to Arenaviridae (Junin, Machupo, Guanavito, Sabia and Lassa), Filoviridae (ebola and Marburg viruses), Flaviviridae (yellow fever, omsk hemorrhagic fever and Kyasanur Forest disease viruses), and Bunyaviridae (Rift Valley fever).
    Type: Grant
    Filed: October 28, 2010
    Date of Patent: April 2, 2013
    Assignee: Siga Technologies Inc.
    Inventors: Dongcheng Dai, Tove Bolken, Sean M. Amberg, Dennis E. Hruby, Thomas R. Bailey
  • Publication number: 20130066076
    Abstract: The present invention relates to processes for the preparation of biaryl oxazolidinones. These compounds are useful as anti-infective, anti-proliferative, anti-inflammatory, and prokinetic agents.
    Type: Application
    Filed: September 14, 2012
    Publication date: March 14, 2013
    Inventors: Yusheng Wu, Shili Chen, Yi Chen, Roger Hanselmann, Rongliang Lou, Jiacheng Zhou
  • Publication number: 20130045995
    Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein Het represents a pyridyl or thiazolyl group, T represents a substituted or non-substituted heterocyclyl group, and X represents various substituents.
    Type: Application
    Filed: April 22, 2011
    Publication date: February 21, 2013
    Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Ulrike Wachendorff-Neumann
  • Patent number: 8372991
    Abstract: Described herein are compounds of Formula (I): wherein A, J, Z, X, R1 and R4 are defined herein, and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.
    Type: Grant
    Filed: March 17, 2011
    Date of Patent: February 12, 2013
    Assignee: Calcimedica, Inc.
    Inventors: Gonul Velicelebi, Kenneth A. Stauderman, Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Publication number: 20130012547
    Abstract: The present invention relates to novel triazole derivatives of formula (I) having insecticidal activity, to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Application
    Filed: March 11, 2011
    Publication date: January 10, 2013
    Applicant: SYNGENTA CROP PROTECTION LLC
    Inventors: Pierre Joseph Marcel Jung, Peter Danko, Christopher Richard Ayles Godfrey, Peter Renold, Ottmar Franz Hueter
  • Patent number: 8334316
    Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.
    Type: Grant
    Filed: February 9, 2009
    Date of Patent: December 18, 2012
    Assignee: ACEA Biosciences, Inc.
    Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
  • Publication number: 20120309795
    Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
    Type: Application
    Filed: August 20, 2012
    Publication date: December 6, 2012
    Inventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev, John A. Porco, JR.
  • Patent number: 8314132
    Abstract: Invention is related to novel compounds -5-aryl-4-(5-substituted 2,4-dihydroxyphenyl)-1,2,3-thiadiazoles with general formula (I). The compounds can be used in biomedicine as active ingredients in pharmaceutical formulations, because they inhibit Hsp90 chaperone which participate in cancer progression. This invention is also related to new intermediate compounds which are used for the synthesis of thiadiazoles of general formula (I).
    Type: Grant
    Filed: June 18, 2008
    Date of Patent: November 20, 2012
    Assignee: Biotechnologijos Institutas
    Inventors: Daumantas Matulis, Inga Cikotiene, Egidijus Kazlauskas, Jurgita Matuliene
  • Publication number: 20120269864
    Abstract: The present invention is a compound of formula (I) or formula (II) which are suitable as NP-1 antagonists.
    Type: Application
    Filed: June 11, 2012
    Publication date: October 25, 2012
    Inventors: Haiyan Jia, Ian ZACHARY, Michelle TICKNER, Lili CHENG, Chris CHAPMAN, Katie ELLARD, Basil HARTZOULAKIS, Ashley JARVIS, Rosemary LYNCH, Jamie NALLY, David SELWOOD, Mark STEWART
  • Patent number: 8288403
    Abstract: The invention relates to methods for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis, Dutch-type (HCHWA-D), multi-infarct dementia, dementia pugilistica and Down syndrome which comprise administering a therapeutically effective amount of a compound of formula I wherein R1, R2, R3, V, W, Y, and Z are as defined herein or a pharmaceutically active acid addition salt of such compounds. The invention also relates to a subgenus of such compounds and pharmaceutical compositions containing them, as well as methods for their manufacture.
    Type: Grant
    Filed: November 4, 2009
    Date of Patent: October 16, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Karlheinz Baumann, Erwin Goetschi, Synese Jolidon, Anja Limberg, Thomas Luebbers
  • Patent number: 8283383
    Abstract: 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: Grant
    Filed: June 22, 2010
    Date of Patent: October 9, 2012
    Assignee: Roche Palo Alto LLC
    Inventors: Chris Allen Broka, Ronald Charles Hawley
  • Publication number: 20120202216
    Abstract: The present invention relates to novel photoactivable rhodamine or carbopyronine derivatives of the following general formulae G1-G4 (I), G1: A1=O, A2=N, A3=C; G2: A1=S, A2=N, A3=C; G3: A1=O, A2=O, A3=N; G4: A1=S, A2=O, A3=N; comprising UV light absorbing chromophores which after photolysis by irradiation at 254-490 nm (preferably at 375-420 nm) generate fluorescent rhodamine or carbopyronine derivatives and small non-toxic fragments such as N2 or N2O. The invention also relates to methods for preparing such compounds and to the use of these compounds for optical microscopy and imaging techniques.
    Type: Application
    Filed: September 10, 2009
    Publication date: August 9, 2012
    Applicant: Max-Planck-Gesellschaft zur Foerderung der Wissenschaften e.V.
    Inventors: Stefan W. Hell, Vladimir N. Belov, Vadim P. Boyarskiy, Christian A. Wurm, Stefan Jakobs, Claudia Geisler
  • Publication number: 20120202750
    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: Application
    Filed: January 23, 2012
    Publication date: August 9, 2012
    Applicant: Genentech, Inc.
    Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
  • Patent number: 8236828
    Abstract: A compound of formula (I) wherein A1, A2, A3, A4, G1, G2, R1, R2, R3, R4, Q1, Y1, Y2, Y3 and Y4 are as defined in claim 1; or a salt or TV-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests.
    Type: Grant
    Filed: October 13, 2008
    Date of Patent: August 7, 2012
    Assignee: Syngenta Crop Protection LLC
    Inventors: Pierre Joseph Marcel Jung, Peter Renold, Christopher Richard Ayles Godfrey, William Lutz, Peter Maienfisch, Werner Zambach