C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
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Patent number: 8883793Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.Type: GrantFiled: December 29, 2011Date of Patent: November 11, 2014Assignee: Development Center for BiotechnologyInventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
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Publication number: 20140309207Abstract: The present invention provides a novel compound represented by a general formula (1) as shown below, which has a glucokinase-activating action in the liver and pancreatic ?-cells and which is useful as an agent for preventing and/or treating diseases caused by hyperglycemia, such as diabetes. A spiroindoline compound represented by the general formula (1), or a salt thereof, or a solvate of the compound or the salt: [wherein ring A represents a nitrogen-containing 5-10 membered heteroaryl group; R1 and R2, which are the same or different, each represent a hydrogen atom, a halogen atom, a halo C1-6 alkyl group, a C6-10 aryl group, a cyano group, a C1-6 alkyl group optionally having a substituent, a C2-6 alkenyl group optionally having a substituent, etc.; R3 represents a hydrogen atom, a C1-6 alkyl group optionally having a substituent, etc.; and R4 represents a hydrogen atom, a halogen atom, a C1-6 alkyl group optionally having a substituent, etc.Type: ApplicationFiled: October 18, 2012Publication date: October 16, 2014Inventors: Takahisa Ogamino, Yukiyoshi Yamazaki, Shin Tanikawa, Ayumu Okuda, Tomoaki Fukuda, Okihisa Tokuda, Yoshiharu Miyake, Shinsuke Itoh, Hiroyuki Ishiwata
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Patent number: 8853415Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: November 14, 2013Date of Patent: October 7, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
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Publication number: 20140296134Abstract: Embodiments include methods for generating a metabolite profile of a stool sample and methods of assessing the status of a subject using the metabolic profile derived from a stool sample.Type: ApplicationFiled: November 8, 2012Publication date: October 2, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Tor Savidge, Sara Dann
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Patent number: 8846730Abstract: The present application relates to cannabinoid receptor ligands of formula (I) wherein X1, A1, Rx, R2, R3, R4, and z are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: GrantFiled: September 4, 2009Date of Patent: September 30, 2014Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Jennifer M. Frost, Teodozyj Kolasa, Tongmei Li, Bo Liu, Arturo Perez-Medrano, Meena Patel, Xueqing Wang, Sridhar Peddi
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Patent number: 8846947Abstract: Provided herein are sirtuin-modulating compounds of formula (II). 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 relating 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: GrantFiled: July 2, 2009Date of Patent: September 30, 2014Assignee: GlaxoSmithKline LLCInventors: Chi B. Vu, Jeremy S. Disch, Pui Yee Ng, Charles A. Blum, Robert B. Perni
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Patent number: 8846731Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogs, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: GrantFiled: October 6, 2011Date of Patent: September 30, 2014Assignee: FerroKin Biosciences, Inc.Inventors: Amy E. Tapper, Hugh Y. Rienhoff, Jr., Stephan D. Parent, Patricia Andres, Jason A. Hanko, Huamin Zhang
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Patent number: 8846667Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.Type: GrantFiled: September 13, 2012Date of Patent: September 30, 2014Assignee: The General Hospital CorporationInventors: Vineet Gupta, M. Amin Arnaout
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Patent number: 8841334Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a, Rx, and n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: November 19, 2008Date of Patent: September 23, 2014Assignee: AbbVie Inc.Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson, Xueqing Wang
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Publication number: 20140275047Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: DOW AGROSCIENCES LLCInventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Jeff Petkus, Andrew L. Ward, Thomas C. Sparks
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Publication number: 20140275189Abstract: The present invention relates to compounds and methods for the treatment of bacterial infections. The compounds and methods involve the disruption of the QseC signaling pathway which modulates the virulence of some bacteria. This methodology for treatment of bacterial infections reduces evolutionary pressure to develop resistance because the bacteria are not killed in the process.Type: ApplicationFiled: March 10, 2014Publication date: September 18, 2014Applicant: The Board of Regents of the University of Texas SystemInventors: Vanessa Sperandio, John R. Falck
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Publication number: 20140274688Abstract: This disclosure relates to the field of molecules having pesticidal utility against pests in Phyla Nematoda, Arthropoda, and/or Mollusca, processes to produce such molecules and intermediates used in such processes, compositions containing such molecules, and processes of using such molecules against such pests. These molecules may be used, for example, as nematicides, acaricides, insecticides, miticides, and/or molluscicides. This document discloses molecules having the following formula (“Formula One”).Type: ApplicationFiled: March 13, 2014Publication date: September 18, 2014Applicant: DOW AGROSCIENCES LLCInventors: Lindsey G. Fischer, Erich W. Baum, Gary D. Crouse, Carl DeAmicis, Beth Lorsbach, Jeff Petkus, Thomas C. Sparks, Gregory T. Whiteker
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Patent number: 8835644Abstract: The invention provides novel antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit antibacterial and antiparasitic action against a wide range of human pathogens. The new classes of compounds show extended action against Gram positive bacteria including MRSA drug resistant pathogens. In the Gram-positive organisms, they specifically target and functionally inhibit microbial attachment to surfaces and biofilm formation. In Gram-negative bacteria, including enteroaggregative E. coli strains, these compounds function as pilicides by inhibiting the assembly of pilin subunits into adhesive filaments. Several of these compounds show potent antimicrobial action against Gram positive bacteria, perhaps involving novel targets. Many of the benzothiophene derivatives exhibit antimicrobial activity in the low micrograms per ml range and in blocking biofilm formation in the nanomolar range; ranges considered are well within the range of utility as therapeutics.Type: GrantFiled: March 16, 2010Date of Patent: September 16, 2014Assignee: University of Virginia Patent FoundationInventors: Paul S. Hoffman, Richard L. Guerrant, Timothy L. Macdonald, Thomas Eric Ballard, Jr.
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Patent number: 8822496Abstract: The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) an interferon alfa and (c) ribavirin and particular regimens for administering this combination. Compound (1) is a selective and potent inhibitor of the HCV NS3 serine protease. The present invention also relates to methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient.Type: GrantFiled: October 27, 2010Date of Patent: September 2, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Carla Haefner, Gerhard Steinmann, Jerry O. Stern, Chan-Loi Yong
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Patent number: 8815910Abstract: Compounds having activity as phosphate transport inhibitors, more specifically, inhibitors of intestinal apical membrane Na/phosphate co-transport, are disclosed. The compounds have the following structure (I): including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein X, Y and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: January 4, 2013Date of Patent: August 26, 2014Assignee: Ardelyx, Inc.Inventors: Jason G. Lewis, Jeffrey W. Jacobs, Nicholas Reich, Michael R. Leadbetter, Noah Bell, Han-Ting Chang, Tao Chen, Marc Navre, Dominique Charmot, Christopher Carreras, Eric Labonte
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Patent number: 8809329Abstract: The present invention provides a method for diagnosing schizophrenia, and a schizophrenia diagnostic reagent or device for use in the method. The present invention further provides a therapeutic or ameliorating agent for schizophrenia, which is effective for the treatment or amelioration of schizophrenia. The therapeutic or ameliorating agent for schizophrenia contains a carbonyl scavenger or a carbonyl-modified protein formation inhibitor as an active ingredient. The method for diagnosing schizophrenia according to the present invention includes measuring at least one parameter in a subject, the parameter being selected from the group consisting of: (1) a genetic abnormality of glyoxalase I gene; (2) the expression level or activity of glyoxalase I in a biological sample; (3) the amount of a carbonyl compound or a carbonyl-modified protein that is a protein modified with the carbonyl compound; and (4) the amount of pyridoxal in a biological sample.Type: GrantFiled: July 31, 2008Date of Patent: August 19, 2014Assignees: Tokyo Metropolitan Institute of Medical Science, Renascience Co., Ltd.Inventors: Masanari Itokawa, Toshio Miyata, Makoto Arai
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Publication number: 20140228365Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neturodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: February 7, 2014Publication date: August 14, 2014Applicant: Merck Serono S.A.Inventors: Anna QUATTROPANI, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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Patent number: 8802861Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: GrantFiled: January 11, 2005Date of Patent: August 12, 2014Assignee: Merck Serono SAInventors: Anna Quattropani, Thomas Rueckle, Matthias Schwarz, Jerome Dorbais, Wolfgang Sauer, Christophe Cleva, Gwenaelle Desforges
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Publication number: 20140206691Abstract: Novel cyclic compounds and salts thereof, pharmaceutical compositions containing such compounds, and methods of using such compounds in the treatment of protein tyrosine kinase-associated disorders such as immunologic and oncologic disorders.Type: ApplicationFiled: March 27, 2014Publication date: July 24, 2014Inventors: Jagabandhu Das, Ramesh Padmanabha, Ping Chen, Derek Norris, Arthur M.P. Doweyko, Joel C. Barrish, John Wityak
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Publication number: 20140206726Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of 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. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: August 21, 2012Publication date: July 24, 2014Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Ulrike Wachendorff-Neumann
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Publication number: 20140194424Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.Type: ApplicationFiled: December 12, 2013Publication date: July 10, 2014Inventors: Hao Zhou, Guiying Li, Dario Doller, Gil Ma
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Publication number: 20140170160Abstract: The invention relates generally to methods and compositions for treating conditions associated with angiogenesis, and, more specifically, the invention relates to methods and compositions for treating conditions associated with angiogenesis using vascular adhesion protein-1 (VAP-1) inhibitors. The invention also relates to methods and compositions for treating conditions associated with lymphangiogenesis using VAP-1 inhibitors.Type: ApplicationFiled: November 1, 2013Publication date: June 19, 2014Applicant: MASSACHUSETTS EYE & EAR INFIRMARYInventor: Ali Hafezi-Moghadam
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Patent number: 8754053Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 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, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: GrantFiled: February 17, 2011Date of Patent: June 17, 2014Assignee: Syngenta Crop Protection LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Patent number: 8741939Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: March 22, 2013Date of Patent: June 3, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
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Publication number: 20140148398Abstract: Compounds useful for the treatment of giardiasis are described.Type: ApplicationFiled: October 12, 2011Publication date: May 29, 2014Applicants: The United States of America, as represented by the Secretary, Dept. of Health and Human Service, UNIVERSITY OF MARYLAND, COLLEGE PARKInventors: Wei Zheng, Catherine Chen, Juan Jose Marugan, Noel Southall, Christopher P. Austin, Andrey Galkin, Liudmila Kulakova, Osnat Herzberg
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Publication number: 20140148457Abstract: Compounds of the formula I in which R, R1, X and Y have the meanings indicated in Claim 1, are inhibitors of TBK1 and IKK? and can be employed, inter alia, for the treatment of cancer and inflammatory diseases.Type: ApplicationFiled: April 12, 2012Publication date: May 29, 2014Applicant: MERCK PATENT GMBHInventors: Srinivasa R. Karra, Wolfgang Staehle, Eike Staub, Margarita Wucherer-Plietker
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Publication number: 20140135331Abstract: 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: ApplicationFiled: May 16, 2013Publication date: May 15, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Nha Huu Vo, Shoujun Chen, Qinglin Che, Yu Xie
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Publication number: 20140128397Abstract: The present invention provides methods for inhibiting growth and proliferation of HIF pathway proficient cells by administering GLUT1 inhibitors of the invention to HIF pathway proficient cells.Type: ApplicationFiled: January 20, 2012Publication date: May 8, 2014Inventors: John Irwin, Patrick Sutphin, Denise Chan, Sandra Turcotte, Amato Giaccia, Edwin Lai, Olga Razorenova, Michael Patrick Hay, Muriel Bonnet, Connie Sun, Raymond Tabibiazar
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Patent number: 8716320Abstract: The present invention provides novel heterocyclic urea compounds having useful antibacterial activity, pharmaceutical compositions comprising one or more of these compounds, methods of making the same, and methods of using the same.Type: GrantFiled: July 23, 2007Date of Patent: May 6, 2014Assignee: Replidyne, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun
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Publication number: 20140121250Abstract: Alkylamidothiazoles of general formula (I), wherein R 1=—C1-C24 alkyl (linear and branched), —C1-C24 alkenyl (linear and branched), —C1-C8 cycloalkyl, —C1-C8 cycloalkyl-alkylhydroxy, —C1-C24 alkylhydroxy (linear and branched), —C1-C24 alkylamine (linear and branched), —C1-C24 alkylaryl (linear and branched), —C1-C24 alkylaryl-alkyl-hydroxy (linear and branched), —C1-C24 alkyl-heteroaryl (linear and branched), —C1-C24-alkyl-O—C1-C24-alkyl (linear and branched), —C1-C24 alkyl morpholino, —C1-C24 alkyl piperidino, —C1-C24 alkyl piperazino, —C1-C24 alkyl-piperazino-N-alkyl, as well as cosmetic or dermatological preparations having an effective content of one or more alkylamidothiazoles, as well as the use thereof for the cosmetic or dermatological treatment and/or prophylaxis of undesired skin pigmentation.Type: ApplicationFiled: September 18, 2012Publication date: May 1, 2014Applicant: Beiersdorf AGInventors: Ludger Kolbe, Cathrin Scherner, Sabrina Ahlheit, Michael Woehrmann, Tobias Mann, Wolfram Gerwat, Torsten Schlaeger
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Publication number: 20140120147Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.Type: ApplicationFiled: January 6, 2014Publication date: May 1, 2014Applicant: NOVARTIS AGInventors: Steve NANCHEN, Noelle GAUVRY, Thomas GOEBEL
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Patent number: 8710052Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: GrantFiled: October 18, 2012Date of Patent: April 29, 2014Assignee: Hydra Biosciences, Inc.Inventor: Jayhong A. Chong
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Publication number: 20140113012Abstract: The present invention provides compounds and compositions for the amelioration of arthritis and joint injuries by inducing mesenchymal stem cells into chondrocytes.Type: ApplicationFiled: March 26, 2012Publication date: April 24, 2014Applicant: THE SCRIPPS RESEARCH INSTITUTEInventors: Peter Schultz, Laure Bouchez
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Publication number: 20140113897Abstract: The present invention embraces compounds that modulate the activity of Epstein-Barr Nuclear Antigen 1 (BBNA1) protein and use thereof in methods for treating latent Epstein-Barr virus infection. R7 is a substituted or unsubstituted phenyl, pyridyl, or pyrimidinyl group. A pharmaceutical composition comprising a compound of the invention in admixture with a pharmaceutically acceptable carrier is also provide as are methods for modulating the activity of Epstein-Barr Nuclear Antigen 1 (EBNA1) protein and treating a latent EpsteinBarr virus infection with a composition of the present invention.Type: ApplicationFiled: May 22, 2012Publication date: April 24, 2014Applicant: THE WISTAR INSTITUTEInventors: Paul M. Lieberman, Troy Messick
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Publication number: 20140112888Abstract: The present disclosure relates to methods for treating viral hepatitis, compounds useful in the treatment of viral hepatitis, and pharmaceutical compositions comprising such compounds. In one embodiment, pharmaceutical compositions comprising nitazoxanide, tizoxanide, or derivatives and/or mixtures thereof are provided, as well as methods of treating hepatitis C using such compositions.Type: ApplicationFiled: December 20, 2013Publication date: April 24, 2014Applicant: Romark Laboratories, L.C.Inventor: Jean-Francois Rossignol
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Patent number: 8703961Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: GrantFiled: November 9, 2010Date of Patent: April 22, 2014Assignee: Merck Patent GmbHInventors: Timo Heinrich, Hannes Koolman
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Publication number: 20140107161Abstract: The present invention provides compounds of formula (I) wherein R1, R2, R2, R3, R4, G1, n, A1, A2, A3, A4, Y1, Y2, and Y3 are as defined in the claims. The invention also relates to processes and intermediates for preparing these compounds, to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising these compounds and to methods of using these compounds to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: May 12, 2012Publication date: April 17, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi, Torsten Luksch, Peter Renold
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Publication number: 20140100211Abstract: Pyrrolidine derivatives of the formula and their use as medicaments for the treatment of obesity and type 2 diabetes.Type: ApplicationFiled: October 1, 2013Publication date: April 10, 2014Applicant: Boehringer Ingelheim International GmbHInventors: Martin FLECK, Niklas HEINE, Bernd NOSSE, Gerald Juergen ROTH
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Publication number: 20140080828Abstract: This disclosure relates to antiviral compounds disclosed herein and uses related thereto. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising 2-((benzo[d]imidazol-2-yl)thio)-N-phenylpropanamide derivatives, N-phenyl-2-((1-phenyl-benzo[d]imidazol-2-yl)thio)propanamide derivatives, or 2-((benzo[d]imidazol-2-yl)thio)-N-(2-chloro-4-methylphenyl)propanamide derivatives. The derivatives may be substituted with one or more substituents. Typically, the pharmaceutical composition comprises a compound of Formula (I), or salt, prodrug, or ester thereof wherein X, Y, and R1 to R7 are described herein.Type: ApplicationFiled: March 28, 2012Publication date: March 20, 2014Applicants: CHILDREN'S HEATLHCARE OF ATLANTA, INC., EMORY UNIVERSITYInventors: Richard K. Plemper, James P. Snyder, Aiming Sun, John M. Ndungu, Jeong-Joong Yoon
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Publication number: 20140080825Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: August 21, 2013Publication date: March 20, 2014Applicant: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Patent number: 8674111Abstract: The invention relates to oxazole and thiazole derivatives of formula (I), wherein A, E, X, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: GrantFiled: June 11, 2010Date of Patent: March 18, 2014Assignee: Actelion Pharmaceuticals Ltd.Inventors: Daniel Bur, Olivier Corminboeuf, Sylvaine Cren, Corinna Grisostomi, Xavier Leroy, Sylvia Richard-Bildstein
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Publication number: 20140065215Abstract: Solid dosage formulations of nitazoxanide or a nitazoxanide analogue are provided that comprise a controlled release portion and an immediate release portion. The pharmaceutical composition is typically in the form of a bilayer solid oral dosage form comprising (a) a first layer comprising a first quantity of nitazoxanide or analogue thereof in a controlled release formulation; and (b) a second layer comprising a second quantity of nitazoxanide or analogue thereof in an immediate release formulation. Method of using the formulations in the treatment of hepatitis C are also provided.Type: ApplicationFiled: July 30, 2013Publication date: March 6, 2014Applicant: Romark Laboratories L.C.Inventors: Jean-Francois Rossignol, Marc Ayers
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Publication number: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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Publication number: 20140051575Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of 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. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: March 30, 2012Publication date: February 20, 2014Inventors: Juergen Benting, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Daniela Portz, Anne-Sophie Rebstock, Ulrike Wachendorff-Neumann
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Patent number: 8653116Abstract: The invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on warm-blooded animals.Type: GrantFiled: January 14, 2013Date of Patent: February 18, 2014Assignee: Novartis AGInventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
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Patent number: 8653127Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I The structures of rings A and B and substituents Ra, Rb and Rc are described in the specification. Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis, treatment and inhibition of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: January 14, 2010Date of Patent: February 18, 2014Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Publication number: 20140045859Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: October 2, 2013Publication date: February 13, 2014Applicant: Takeda California, Inc.Inventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Mingnam Tang, Haixia Wang, Jeffrey A. Stafford
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Patent number: 8642576Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: GrantFiled: August 29, 2012Date of Patent: February 4, 2014Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20140031395Abstract: The present invention relates to compounds useful in the positive modulation of the alpha 7 nicotinic acetylcholine receptor (?7nAChR). The invention also relates to the use of these compounds in the treatment or prevention of a broad range of diseases in which the positive modulation of ?7nAChR is advantageous, including neurodegenerative and neuropsychiatric diseases and also inflammatory diseases.Type: ApplicationFiled: February 2, 2012Publication date: January 30, 2014Applicant: Bionomics LimitedInventors: Andrew Harvey, Audrey Fluck, Bruno Giethlen, Dharam Paul, Laurent Schaeffer
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Publication number: 20140030224Abstract: The present invention relates to methods and pharmaceutical compositions for inhibiting influenza virus replication. More particularly, the present invention relates to a compound selected from the group consisting of Gemcitabine, Obatoclax Mesylate, Docetaxel, HA-14, Alsterpaullone, GSK3B inhibitor VIII, GSK3B inhibitor XV, Indirubin 3?- monoxime, L glutathione reduced, Fluocinolone acetonide, Tirofiban, Topotecan hydrochloride, Clofarabine, Vinblastine, Menadione Crystalline and derivatives or analogues thereof for use in the treatment of an influenza infection in a subject in need thereof.Type: ApplicationFiled: April 10, 2012Publication date: January 30, 2014Applicant: UNIVERSITÉ CLAUDE BERNARD - LYON 1Inventors: Vincent Lotteau, Benoit De Chassey, Patrice Andre, Laurene Meyniel-Schicklin, Anne Aublin-Gex