1,3,4-thiadiazoles (including Hydrogenated) Patents (Class 514/363)
  • Dietary supplement and a method to enhance sleep and lucid dreaming
    Patent number: 8092840
    Abstract: A nutritional supplement for enhancing sleep and lucid dreaming in humans. It contains a combination of ingredients in proportions calculated to enhance lucid dreaming. The primary ingredients are Calea ternifolia, L-5-Hydroxytryptophan (L-5-HTP), and Vinpocetine. In addition, the nutritional supplement may include the secondary ingredient Melatonin and the tertiary ingredients Wild Lettuce Extract, Mugwort Extract, Dimethylaminoethanol Powder (DMAE), Passionflower Extract and Green Tea Extract. Further, various Vitamins may be added such as certain B vitamins, D and C, as well as Zinc, Magnesium and Calcium. The selection and amounts of the ingredients of the nutritional supplement promotes sleep and lucid dreaming in people who have taken the nutritional supplement prior to going to sleep.
    Type: Grant
    Filed: October 30, 2007
    Date of Patent: January 10, 2012
    Inventor: Jeff Luciano
  • Antifungal Treatment
    Publication number: 20110319455
    Abstract: A method of treating or preventing fungal infection, which includes identifying a plant or animal having a fungal infection and administering an effective amount of an anti-fungal composition to the plant or animal to reduce the fungal infection. In a preferred form of the present invention, the antifungal composition is compound 13 or 33 and is combined with an azole compound, such as fluconazole.
    Type: Application
    Filed: April 19, 2011
    Publication date: December 29, 2011
    Inventors: Bruce Steven Klein, Brad Mark Tebbets
  • 1,2,4-OXADIAZOLE DERIVATIVES AND THEIR THERAPEUTIC USE
    Publication number: 20110311485
    Abstract: The present disclosure relates to 1, 2, 4 oxadiazole derivatives of formula (I) as well as pharmaceutical compositions comprising them, and their use in therapy as agonists of the S1P1 receptors.
    Type: Application
    Filed: December 15, 2009
    Publication date: December 22, 2011
    Applicant: ALMIRALL S.A.
    Inventors: Victor Giulio Matassa, Nuria Aguilar Izquierdo, Marta Mir Cepeda, Marta Carrascal Riera, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Julio Cesar Castro Palomino Laria, Montserrat Erra Sola
  • Therapeutic Uses of Compounds Which Selectively Modulate The CB2 Receptor
    Publication number: 20110312932
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: August 25, 2011
    Publication date: December 22, 2011
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
  • MODULATORS OF ATP-BINDING CASSETTE TRANSPORTERS
    Publication number: 20110306637
    Abstract: 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: Application
    Filed: May 20, 2011
    Publication date: December 15, 2011
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
  • INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
    Publication number: 20110306599
    Abstract: Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
    Type: Application
    Filed: November 24, 2010
    Publication date: December 15, 2011
    Applicant: JAPAN TOBACCO INC.
    Inventors: Teruhiko INOUE, Tetsudo KAYA, Shinichi KIKUCHI, Koji MATSUMURA, Ritsuki MASUO, Motoya SUZUKI, Michihide MAEKAWA
  • Pyrrole Derivatives As Pharmaceutical Agents
    Publication number: 20110301128
    Abstract: Compounds, compositions and methods for modulating the activity of receptors are provided. In particular compounds and compositions are provided for modulating the activity of receptors and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder directly or indirectly related to the activity of the receptors.
    Type: Application
    Filed: August 22, 2011
    Publication date: December 8, 2011
    Applicant: EXELIXIS, INC.
    Inventors: Lynne Canne Bannen, Jeff Chen, Lisa Esther Dalrymple, Brenton T. Flatt, Timothy Patrick Forsyth, Xiao-Hui Gu, Morrison B. Mac, Larry W. Mann, Grace Mann, Richard Martin, Raju Mohan, Brett Murphy, Michael Charles Nyman, William C. Stevens, Tie-Lin Wang, Yong Wang, Jason H. Wu
  • ARYL CARBONYL DERIVATIVES AS THERAPEUTIC AGENTS
    Publication number: 20110301158
    Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.
    Type: Application
    Filed: August 15, 2011
    Publication date: December 8, 2011
    Applicant: Novo Nordisk A/S
    Inventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce-Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
  • Small molecule inhibitors of kynurenine-3-monooxygenase
    Patent number: 8071631
    Abstract: The present invention relates to compounds of Formula I below and their tautomers or pharmaceutically acceptable salts, compositions and methods of uses thereof:
    Type: Grant
    Filed: August 16, 2007
    Date of Patent: December 6, 2011
    Assignees: The J. David Gladstone Institutes, A Testamentary Trust Established Under The Will Of J. David Gladstone, University Of Maryland, Baltimore
    Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
  • Anthelmintic composition
    Patent number: 8067382
    Abstract: The invention relates to a novel formulation having the advantage of including triclabendazole in solution. In addition a further anthelmintic may be included. The formulation is made by mixing the abamectin and benzyl alcohol and mixing this with triclabendazole and butyl dioxitol. The mix is then heated to dissolve the active, and allowed to cool at which stage the solution is diluted to volume with PEG 4000. The present invention overcomes the solubility difficulties of triclabendazole and presents the triclabendazole in a solution.
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: November 29, 2011
    Assignee: Merial Limited
    Inventor: Colin Manson Harvey
  • Modulators of glucocorticoid receptor, AP-1, and/or NF-?B activity and use thereof
    Patent number: 8067447
    Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, and/or AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I), its enantiomers, diastereomers, or a pharmaceutically-acceptable salt, or hydrate, thereof, wherein (Ia) is heterocycle or heteroaryl; J, Ja, E, F, G, Ma, M, Q, Za and Z are as defined herein. Also provided are pharmaceutical compositions and methods of treating inflammatory- or immune-associated diseases and obesity and diabetes employing said compounds.
    Type: Grant
    Filed: October 31, 2007
    Date of Patent: November 29, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventors: James E. Sheppeck, John L. Gilmore, T. G. Murali Dhar, Hai-Yun Xiao
  • METHOD OF TREATING CANCER BY INHIBITION OF PROTEIN KINASE-LIKE ENDOPLASMIC RETICULUM PROTEIN KINASE
    Publication number: 20110288083
    Abstract: The present invention relates to a method of identifying compounds useful in inhibiting protein kinase-like endoplasmic reticulum protein kinase (PERK). The method comprises providing a first model comprising PERK active domains, where the said active domains are selected from the group consisting of the peptide spanning from amino acid residue Asp144 to amino acid residue Ser191 of SEQ ID NO: 1 and a peptide comprising the amino acid residue at position 7 of SEQ ID NO: 1, providing one or more candidate compounds, evaluating contact between the candidate compounds and the first model to determine which of the one or more candidate compounds have an ability to bind to and/or fit in the first model, and identifying the compounds which, based on said evaluating, have the ability to bind to and/or fit in the first model as compounds potentially useful for inhibiting PERK.
    Type: Application
    Filed: May 19, 2011
    Publication date: November 24, 2011
    Applicant: NEW YORK UNIVERSITY
    Inventors: Timothy CARDOZO, Hong WANG, David Ron
  • SULFONYL CONTAINING COMPOUNDS AS CYSTEINE PROTEASE INHIBITORS
    Publication number: 20110281879
    Abstract: The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
    Type: Application
    Filed: January 12, 2011
    Publication date: November 17, 2011
    Applicant: ViroBay, Inc.
    Inventor: Craig Mossman
  • NOVEL SUBSTITUTED OCTAHYDROCYCLOPENTA[C]PYRROL-4-AMINES AS CALCIUM CHANNEL BLOCKERS
    Publication number: 20110281870
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein L1, L2, R1, R2, and R3 are as defined in the specification. The present application also relates to compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.
    Type: Application
    Filed: May 24, 2011
    Publication date: November 17, 2011
    Applicant: ABBOTT LABORATORIES
    Inventors: Xenia B. Searle, Ming C. Yeung, Stanley DiDomenico, Andrew O. Stewart, Daria Darczak, Michael Schrimpf, Michael J. Rozema
  • Compounds as cannabinoid receptor ligands
    Patent number: 8058293
    Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.
    Type: Grant
    Filed: March 11, 2009
    Date of Patent: November 15, 2011
    Assignee: Abbott Laboratories
    Inventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
  • OPHTHALMIC COMPOSITION
    Publication number: 20110275617
    Abstract: The present invention provides an ophthalmic composition comprising a hyperbranched polymer. The ophthalmic compositions may also comprise carbonic anhydrase inhibitors, wherein the hyperbranched polymer increases the aqueous solubility of the carbonic anhydrase inhibitor, and increases corneal permeation of the active agent. The ophthalmic compositions may also comprise non-ionic surfactants, such as polysorbate, hydroxypropyl methyl cellulose or hydroxyethyl cellulose, and beta-blockers, such as carteolol, levobunolol, betaxolol, metipranolol, timolol or propranolol.
    Type: Application
    Filed: May 5, 2010
    Publication date: November 10, 2011
    Inventors: Jun INOUE, Tapan Shah
  • COMPOUNDS
    Publication number: 20110269738
    Abstract: The present invention relates to novel compounds having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.
    Type: Application
    Filed: April 28, 2011
    Publication date: November 3, 2011
    Applicant: Glaxo Group Limited
    Inventors: Guanghui Deng, Xichen Lin, Feng Ren, Baowei Zhao
  • Compounds which selectively modulate the CB2 receptor
    Patent number: 8048899
    Abstract: are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 22, 2009
    Date of Patent: November 1, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, Markus Ostermeier, Doris Riether, Achim Sauer, David Smith Thomson, Lifen Wu, Renee M. Zindell, Patricia Amouzegh, Nigel James Blumire, Stephen Peter East, Monika Ermann, Someina Khor, Innocent Mushi
  • SCREEN FOR INHIBITORS OF FILOVIRUS AND USES THEREFOR
    Publication number: 20110263554
    Abstract: The invention provides methods to identify agents useful to prevent, inhibit or treat viral infections, e.g. filovirus infections, as well as compositions having one or more agents to prevent, inhibit or treat viral infection.
    Type: Application
    Filed: November 6, 2009
    Publication date: October 27, 2011
    Applicant: WARF - Wisconsin Alumni Research Foundation
    Inventors: Yoshihiro Kawaoka, Shinji Watanabe, Yasuko Hatta
  • IL-8 receptor antagonists
    Patent number: 8044075
    Abstract: This invention relates to novel compounds, compositions and combinations thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).
    Type: Grant
    Filed: December 5, 2007
    Date of Patent: October 25, 2011
    Assignee: GlaxoSmithKline
    Inventors: Gregory L. Adams, James A. Brackley, III, Jakob Busch-Petersen, Jianghe Deng, Wei Fu, Huijie Li, Jack J. Taggart, Feng Wang, Yonghui Wang, Katherine Louisa Widdowson, Hongyi Yu
  • Water-soluble prodrugs of chloramphenicol, thiamphenicol, and analogs thereof
    Patent number: 8044230
    Abstract: The present invention discloses certain novel prodrugs of chloramphenicol or thiamphenicol, or of an analog of either, including prodrugs of pharmaceutically acceptable salts of chloramphenicol or thiamphenicol or of their analogs, including nitrogen-containing esters of both alcohol groups of such compounds. In certain embodiments these novel prodrugs are sufficiently water-soluble to serve the functions needed of a prodrug of chloramphenicol or thiamphenicol or of an analog of either. In one embodiment, a certain subclass of the compounds also possesses the hydrolytic stability needed to maintain the prodrug in solution in the subject's system until appropriate conditions exist when the prodrug can hydrolyze, releasing the active compound in question.
    Type: Grant
    Filed: December 11, 2007
    Date of Patent: October 25, 2011
    Assignee: Intervet Inc.
    Inventor: Tomasz W. Glinka
  • Selective androgen receptor modulators
    Publication number: 20110224267
    Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, and or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, and intermediates useful in the preparation of same.
    Type: Application
    Filed: August 17, 2010
    Publication date: September 15, 2011
    Applicant: Radius Health,Inc.
    Inventor: Chris P. Miller
  • TREATMENT OF OBSTRUCTIVE SLEEP APNEA SYNDROME WITH A COMBINATION OF A CARBONIC ANHYDRASE INHIBITOR AND AN ADDITIONAL ACTIVE AGENT
    Publication number: 20110224196
    Abstract: This invention relates generally to methods and pharmaceutical formulations useful in treating patients suffering from obstructive sleep apnea syndrome (OSAS). Treatment of OSAS is effected by administering a carbonic anhydrase inhibitor to the patient in combination with at least one additional active agent. Examples of additional active agents include modafinil, eszopiclone, zolpidem, zaleplon, and phentermine.
    Type: Application
    Filed: January 7, 2011
    Publication date: September 15, 2011
    Applicant: Vivus, Inc.
    Inventors: Leland F. Wilson, Peter Tam, Thomas Najarian, Charles H. Bowden
  • 5-Phenylthiazole derivatives and their use as p13 kinase inhibitors
    Patent number: 8017608
    Abstract: Compounds of formula I in free or salt form, wherein R1, R2, R3, R4 and R5 have the meanings as indicated in the specification, are useful for treating diseases mediated by phosphatidylinositol 3-kinase. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.
    Type: Grant
    Filed: March 5, 2004
    Date of Patent: September 13, 2011
    Assignee: Novartis AG
    Inventors: Graham Charles Bloomfield, Ian Bruce, Catherine Leblanc, Mrinalini Sachin Oza, Lewis Whithead, Bernard Cuenoud, Thomas Hugo Keller, Louise Kirman, Clive McCarthy, Gaynor Elizabeth Woodward
  • HUMAN PROTEIN TYROSINE PHOSPHATASE INHIBITORS AND METHODS OF USE
    Publication number: 20110212951
    Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.
    Type: Application
    Filed: August 4, 2010
    Publication date: September 1, 2011
    Inventors: Jeffery Lyle Gray, Kande K.D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
  • 3,4-dihalogenoisothiazole derivative, and agricultural or horticultural plant disease-controlling agent
    Patent number: 8003675
    Abstract: A 3,4-dihalogenoisothiazole derivative represented by the general formula [I] (wherein R1 is a halogen atom; A is an oxygen atom or a sulfur atom; and R is a C1-C6 alkyl group, a C2-C5 alkenyl group, a C2-C5 alkynyl group, a C3-C6 cycloalkyl group, a phenyl group or a 5- to 10-membered heterocyclic group containing at least one of oxygen atom, sulfur atom and nitrogen atom), or a salt thereof.
    Type: Grant
    Filed: July 6, 2007
    Date of Patent: August 23, 2011
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Toshihiro Nagata, Atsushi Kogure, Isao Kaneko, Norihisa Yonekura, Ryo Hanai
  • PROTEASOME INHIBITORS FOR SELECTIVELY INDUCING APOPTOSIS IN CANCER CELLS
    Publication number: 20110201609
    Abstract: The subject invention concerns compounds having activity as inhibitors of proteasomes and methods of using the subject compounds.
    Type: Application
    Filed: June 30, 2009
    Publication date: August 18, 2011
    Applicants: H. Lee Moffitt Cancer Center & Research Institute, University of South Florida
    Inventors: Harshani Lawrence, Yiyu Ge, Said M. Sebti, Wayne Guida
  • Inhibitors of c-Met and uses thereof
    Patent number: 7998987
    Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.
    Type: Grant
    Filed: April 8, 2010
    Date of Patent: August 16, 2011
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: David Lauffer, Alex Aronov, Pan Li, David Deininger, Kira McGinty, Dean Stamos, Jon Come, Michelle Stewart
  • Antagonists of Prostaglandin D2 Receptors
    Publication number: 20110190227
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein that are antagonists Of PGD2 receptors. Also described herein are methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: August 4, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns, Jeffrey Roger Roppe
  • Imidazolothiadiazoles for Use as Protein Kinase Inhibitors
    Publication number: 20110190289
    Abstract: There is provided compounds of formula (I), wherein Z, M, R1, X, R2, R3 and B have meanings given in the description, and pharmaceutically-acceptable esters, amides, solvates or salts thereof, which compounds are useful in the treatment of diseases in which inhibition of a protein kinase (e.g. a PIM family kinase or PI3-K) is desired and/or required, and particularly in the treatment of cancer.
    Type: Application
    Filed: September 29, 2008
    Publication date: August 4, 2011
    Applicant: Centro Nacional De Investigaciones Oncologicas (CNIO)
    Inventors: Paolo Pevarello, Ana Maria Garcia Collazo, Ana Belen Garcia Garcia
  • SELECTIVE HETEROCYCLIC SPHINGOSINE 1 PHOSPHATE RECEPTOR MODULATORS
    Publication number: 20110183953
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Application
    Filed: November 15, 2010
    Publication date: July 28, 2011
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • METHODS AND COMPOSITIONS OF TRAIL-DEATH RECEPTOR AGONISTS/ACTIVATORS
    Publication number: 20110172234
    Abstract: This invention describes a series of methods and compositions for prevention and treatment of diseases such as cancer. One aspect of the invention describes small molecule-based drugs that can be used to bind to death receptors TRAIL-R1/DR4 and/or TRAIL-R2/DR5 and induce apoptosis in cancer cells, while sparing normal cells. The invention also describes TRAIL Death Receptor Agonists/Activators (DRAs) and their uses, such as the induction of apoptosis through caspase-8 and caspase-3 activation. The present invention also describes the methods of treating cancers, such as breast, prostate, colon, pancreatic, ovarian, lung, and brain cancers, leukemia, lymphoma, multiple myeloma, and mesothelioma, using DRAs either as single-agent treatments, or in combination with other therapies.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 14, 2011
    Applicants: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM, UNIVERSITY OF MARYLAND, BALTIMORE A CONSTITUENT INSTITUTION OF THE UNIVERSITY
    Inventors: Rakesh Srivastava, Sharmila Shankar, Alexander D. MacKerell, JR.
  • Insecticidal N-(heteroarylalkyl)alkanediamine derivatives
    Patent number: 7977332
    Abstract: Certain noel N-(heteroarylalkyl)alkanediamine derivatives have provided unexpected insecticidal and acaricidal activity. These compounds are represented by formula I: wherein Ar, a, r, R, Ra, Rb, Rc, Rd, b, c, Re, Rf, Rg, Rh, R5, d, e, U, V, X, WR6 and R7 are fully described herein. In addition, compositions comprising an insecticidally effective amount of at least one compound of formula I, and optionally, an effective amount of at least one of a second compound, with at least one insecticidally compatible carrier are also disclosed; along with methods of controlling insects comprising applying said compositions to a locus where insects are present or are expected to be present.
    Type: Grant
    Filed: December 2, 2004
    Date of Patent: July 12, 2011
    Assignee: FMC Corporation
    Inventors: David M. Roush, John F. Chiarello, Jianming Yu, Benjamin J. Dugan, George Theodoridis, Manorama M. Patel, Walter H. Yeager, Steven W. Szczepanski
  • 5,5-FUSED ARYLENE OR HETEROARYLENE HEPATITIS C VIRUS INHIBITORS
    Publication number: 20110150827
    Abstract: Provided herein are 5,5-fused heteroarylene hepatitis C virus inhibitor compounds, for example, of Formula I, IA, or IB, pharmaceutical compositions comprising the compounds, and processes of preparation thereof. Also provided are methods of their use for the treatment of an HCV infection in a host in need thereof.
    Type: Application
    Filed: December 17, 2010
    Publication date: June 23, 2011
    Applicant: Idenix Pharmaceuticals, Inc.
    Inventors: Cyril B. Dousson, David Dukhan, Christophe Claude Parsy, Claire Pierra, Francois-Rene Alexandre, Guillaume Brandt, Daniel Da Costa, Houcine Rahali, Jean-Laurent Paparin, Michel Derock, Thierry Convard, Dominique Surleraux
  • INHIBITORS OF THE PLASMODIAL SURFACE ANION CHANNEL AS ANTIMALARIALS
    Publication number: 20110144086
    Abstract: Disclosed are inhibitors of the plasmodial surface anion channel (PSAC) inhibitors and the use thereof in treating or preventing malaria in an animal such as a human, comprising administering an effective amount of an inhibitor or a combination of inhibitors. An example of such an inhibitor is a compound of formula I, Formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R7 are as described herein.
    Type: Application
    Filed: July 15, 2009
    Publication date: June 16, 2011
    Applicant: The United States of America, as represented by the Secretary, Dept of Health and Human Service
    Inventors: Sanjay A. Desai, Ajay D. Pillai
  • SMALL MOLECULE INHIBITORS OF THE PLECKSTRIN HOMOLOGY DOMAIN AND METHODS FOR USING SAME
    Publication number: 20110144066
    Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
    Type: Application
    Filed: April 14, 2009
    Publication date: June 16, 2011
    Applicants: The Board of Regents of the University of Texas System, Arizona Board of Regents on Behalf of the University of Arizona
    Inventors: Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Vijay Gokhale, Garth Powis, Shuxing Zhang
  • Antagonists of Prostaglandin D2 Receptors
    Publication number: 20110144160
    Abstract: Described herein are compounds that are antagonists of PGD2 receptors. Also described are pharmaceutical compositions that include the compounds described herein, and methods of using such antagonists of PGD2 receptors, alone or in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
    Type: Application
    Filed: July 2, 2009
    Publication date: June 16, 2011
    Applicant: Amira Pharmaceuticals, Inc.
    Inventors: John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Brian Andrew Stearns
  • Bicyclic compositions and methods for modulating a kinase cascade
    Publication number: 20110136807
    Abstract: The invention relates to compounds and methods for modulating one or more components of a kinase cascade.
    Type: Application
    Filed: June 29, 2007
    Publication date: June 9, 2011
    Applicant: Kinex Pharmaceuticals, LLC
    Inventor: David G. Hangauer, JR.
  • Mitotic kinesin inhibitors and methods of use thereof
    Patent number: 7956073
    Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
    Type: Grant
    Filed: March 6, 2008
    Date of Patent: June 7, 2011
    Assignee: Array BioPharma Inc.
    Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Joseph P. Lyssikatos, Thomas D. Aicher, Ellen R Laird, John Robinson, Shelley Allen
  • PYRROLINONE COMPOUNDS AS INHIBITORS OF BACTERIAL PEPTIDYL TRNA HYDROLASE AND USES THEREOF
    Publication number: 20110130397
    Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.
    Type: Application
    Filed: September 21, 2007
    Publication date: June 2, 2011
    Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
  • IMIDAZOTHIADIAZOLE DERIVATIVES
    Publication number: 20110130396
    Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.
    Type: Application
    Filed: July 1, 2009
    Publication date: June 2, 2011
    Inventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
  • COMPOUNDS FOR INHIBITING KSP KINESIN ACTIVITY
    Publication number: 20110123435
    Abstract: The present invention relates to compounds of Formula (I), below, (wherein X, R1, R2, R3, p, E, ring A, and ring B are as defined herein). The present invention also relates to compositions (including pharmaceutically acceptable compositions) comprising these compounds, alone and in combination with one or more additional therapeutic agents, and to methods for their use in inhibiting KSP kinesin activity, and for treating cellular proliferative diseases or disorders associated with KSP kinesin activity.
    Type: Application
    Filed: October 16, 2008
    Publication date: May 26, 2011
    Inventors: M. Arshad Siddiqui, Chaoyang Dai, Umar Faruk Mansoor, Liping Yang, Lalalnthi Dilrukshi Vitharana, Angie R. Angeles
  • Compounds, compositions and methods
    Publication number: 20110112154
    Abstract: Certain substituted sulfonamide derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.
    Type: Application
    Filed: January 18, 2011
    Publication date: May 12, 2011
    Inventors: Bradley Paul MORGAN, Fady Malik, Erica Anne Kraynack, Alexander Ramon Muci, Xiangping Qian, David J. Morgans, JR.
  • Inhibitors Of 11beta-Hydroxysteroid Dehydrogenase Type 1
    Publication number: 20110105504
    Abstract: This invention relates to novel compounds of the Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11?-HSD1 in mammals.
    Type: Application
    Filed: March 18, 2009
    Publication date: May 5, 2011
    Inventors: David A. Claremon, Linghang Zhuang, Yuanjle Ye, Suresh B. Singh, Colin M. Tice, Gerard McGeehan
  • CYCLOPENTATHIOPHENE MODULATORS OF THE GLUCOCORTICOID RECEPTOR, AP-1, AND/OR NF-kB ACTIVITY AND USE THEREOF
    Publication number: 20110105495
    Abstract: A compound of Formula (I) and enantiomers, diastereomers and pharmaceutically-acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as defined herein. Also disclosed are pharmaceutical compositions and combinations containing compounds of Formula I and methods of treating diseases or disorders including metabolic and inflammatory or immune associated diseases or disorders.
    Type: Application
    Filed: June 24, 2009
    Publication date: May 5, 2011
    Inventor: Bingwei Vera Yang
  • FUSED RING COMPOUNDS AND USE THEREOF
    Publication number: 20110098297
    Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like. The present invention provides a glucokinase activator containing a compound represented by the formula (I): wherein each symbol is defined in the specification, or a salt thereof or a prodrug thereof.
    Type: Application
    Filed: April 9, 2009
    Publication date: April 28, 2011
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tsuneo Yasuma, Nobuyuki Takakura
  • IMIDAZOLE MODULATORS OF MUSCARINIC ACETYLCHOLINE RECEPTOR M3
    Publication number: 20110091459
    Abstract: The present invention relates to new imidazole modulators of M3 muscarinic acetylcholine receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: December 11, 2009
    Publication date: April 21, 2011
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Manouchehr M. Shahbaz
  • USE OF PDE7 INHIBITORS FOR THE TREATMENT OF MOVEMENT DISORDERS
    Publication number: 20110091388
    Abstract: A method of treating a movement abnormality associated with the pathology of a neurological movement disorder, such as Parkinson's disease or Restless Leg(s) Syndrome by administering a therapeutically effective amount of a PDE7 inhibitory agent. An aspect of the invention provides for the administration of a PDE& inhibitory agent in conjunction with a dopamine agonist or precursor, such as levodopa. In another aspect of the invention, the PDE7 inhibitory agent may be selective for PDE7 relative to other molecular targets (i) known to be involved with the pathology of Parkinson's disease or (ii) at which other drug(s) that are therapeutically effective to treat Parkinson's disease act.
    Type: Application
    Filed: December 21, 2010
    Publication date: April 21, 2011
    Applicant: OMEROS CORPORATION
    Inventors: John E. Bergmann, Neil S. Cutshall, Gregory A. Demopulos, Vincent A. Florio, George A. Gaitanaris, Patrick Gray, John Hohmann, Rene Onrust, Hongkui Zeng
  • Compounds which modulate the CB2 receptor
    Patent number: 7928123
    Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Grant
    Filed: September 13, 2007
    Date of Patent: April 19, 2011
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
  • PHARMACEUTICAL COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER
    Publication number: 20110086861
    Abstract: Provided is a pharmaceutical composition including as an active component a compound of formula (I): wherein X and (R1)n are as defined, and a physiological acceptable carrier. Also provided is a method for treating cancer including administering to an individual in need of such treatment an effective amount of the presently described pharmaceutical composition.
    Type: Application
    Filed: August 10, 2008
    Publication date: April 14, 2011
    Applicant: URIFER LTD
    Inventors: Uri Nir, Sally Shpungin, Etai Yaffe, Moshe Cohen