Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
  • Publication number: 20120108592
    Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.
    Type: Application
    Filed: October 28, 2011
    Publication date: May 3, 2012
    Inventors: J. Edward Semple, Jean-Francois Rossignol
  • Publication number: 20120093929
    Abstract: The present invention relates to a composition, comprising (i) a matrix made of polymeric nanofibers, and (ii) an opioid agonist within the matrix.
    Type: Application
    Filed: May 5, 2009
    Publication date: April 19, 2012
    Applicant: Euro-Celtique S.A.
    Inventors: Alexander Oksche, Kevin J. Smith, Derek Prater, Malcolm Walden, Will Heath, Bernard Kennedy, Vanessa Addison, Hassan Mohammad
  • Publication number: 20120065206
    Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.
    Type: Application
    Filed: December 1, 2009
    Publication date: March 15, 2012
    Applicant: SYNTA PHARMACEUTICALS CORP.
    Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
  • Publication number: 20120058201
    Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.
    Type: Application
    Filed: April 5, 2010
    Publication date: March 8, 2012
    Applicant: VANDA PHARMACEUTICALS, INC.
    Inventors: Christian Lavedan, Simona Volpi, Louis Licamele
  • Publication number: 20120058186
    Abstract: The present invention relates to a stable orally disintegrating coated tablet containing a drug, wherein the tablet is coated with a coating layer containing a water-soluble substance and a polyvinyl alcohol resin of not less than 5% by weight based on the weight of the coating layer, the water-soluble substance dissolving in an amount of 1 g or more in less than 10 mL of water at 20° C., having a hydroxyl group(s) in its molecule, and having a molecular weight of not more than 200 per a unit hydroxyl group. There is provided a stable orally disintegrating coated tablet which does not cause a crack in the coating layer even when the orally disintegrating tablet has been swollen by moisture absorption under high humidity, while ensuring rapid disintegration properties in an oral cavity. In the case of an orally disintegrating tablet containing a light-unstable drug, degradation of the drug can be suppressed by blending a light shading agent in the coating layer.
    Type: Application
    Filed: March 29, 2010
    Publication date: March 8, 2012
    Applicant: TORAY INDUSTRIES, INC.
    Inventors: Suguru Takaki, Kotoe Ohta, Yasuhide Horiuch
  • Patent number: 8129376
    Abstract: The present invention relates to piperidine derivatives that act as inhibitors of stearoyl-CoA desaturase. The invention also relates to methods of preparing the compounds, compositions containing the compounds, and to methods of treatment using the compounds.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: March 6, 2012
    Inventors: Kumar Sundaresan, P. Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
  • Patent number: 8129414
    Abstract: Disclosed herein are non-competitive NMDA receptor antagonists having chemical structures similar to that of phencyclidine (PCP). These antagonists contain a polycyclic ring structure in place of the cycloalkyl ring of PCP. The antagonists also differ from PCP in that they include an electron withdrawing group, a hydroxyl group, or an amine group at the para position of the phenyl ring. The antagonists disclosed herein are useful for treating or ameliorating a symptom of ailments associated with over excitation of cells (e.g., neurons) that express NMDA receptors. Examples of ailments that can be treated and for which symptoms can be ameliorated include epilepsy, neurodegenerative disease (e.g., Alzheimer's and Parkinson's diseases), drug addiction, neuropathic pain, and neuronal and glutamate-dependent tumors.
    Type: Grant
    Filed: June 19, 2007
    Date of Patent: March 6, 2012
    Inventor: Adeboye Adejare
  • Publication number: 20120046247
    Abstract: This invention relates to compounds of Formula (I), (II), or (III) as shown in the specification, which contain a 1,5-diphenylpenta-1,4-dien-3-one backbone. These compounds can be used to treat cancer, inflammatory disease, or autoimmune disease.
    Type: Application
    Filed: August 16, 2011
    Publication date: February 23, 2012
    Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
  • Patent number: 8119563
    Abstract: N-substituted azacycle derivative compounds represented by formula (I): wherein m, q, r, t and u are independently selected from 0 or 1; and p is 0, 1, 2, or 3; and A, B, D, X, Y, R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 and R11 are fully described herein. The compounds being particularly useful in compositions comprising an insecticidally effective amount of at least one compound of formula I, and an 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: October 4, 2004
    Date of Patent: February 21, 2012
    Assignee: FMC Corporation
    Inventors: George Theodoridis, David Rosen, Shunxiang Zhang, Walter H. Yeager, Robert N. Henrie, II, Syed Z. Ahmed, Hongbin Men, Stephen Donovan
  • Publication number: 20120029021
    Abstract: Nitroxide free radicals attached to antineoplastic agents can synergize their potencies to cancer cells. This invention relates to any antineoplastic agents and their derivatives chemically attached with nitroxide free radicals, such as TEMPO and its radical derivatives. This invention also relates to precursors of such compounds, as well as the products formed from the adducts after administration.
    Type: Application
    Filed: January 17, 2011
    Publication date: February 2, 2012
    Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITY
    Inventors: Yong Ba, Errol V. Mathias
  • Publication number: 20120022076
    Abstract: This invention concerns N-(2-arylamino)aryl sulfonamides, which are inhibitors of MEK and are useful in treatment of cancer and other hyperproliferative diseases.
    Type: Application
    Filed: September 23, 2011
    Publication date: January 26, 2012
    Inventors: Andreas MADERNA, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Dinesh Barawkar, Zhi Hong
  • Patent number: 8093391
    Abstract: This invention relates to an improved and scalable process for the preparation of substantially pure palonosetron and its acid addition salts, in particular hydrochloride (I) which comprises of, (a) converting intermediate (IIa) as such or as its freebase (II) to a crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) via hydrogenation under pressure with an appropriately chosen hydrogenation catalyst in an suitable organic solvent. (b) making the resulting crude mixture of diastereomeric palonosetrons (VIII) or (VIIIa) contaminated with varying amounts of unconverted intermediate (II) or (IIa) substantially free from (II) or (IIa) via halogenation reaction.
    Type: Grant
    Filed: January 5, 2010
    Date of Patent: January 10, 2012
    Assignee: Sterling Biotech Research Center
    Inventors: Sugata Chatterjee, Ajay Singh Rawat, Anil V. Pawar, Jetti Rajanikanth, Penigandla Venkateswarlu
  • Patent number: 8093386
    Abstract: There are described compounds having the general formula (I) below and their pharmaceutically acceptable salts thereof, wherein E, X, m, q, R1, R2, n and ZBG have the meanings reported in the description useful, in therapy, as inhibitors of zinc metalloproteinases.
    Type: Grant
    Filed: July 25, 2007
    Date of Patent: January 10, 2012
    Assignee: Bracco Imaging S.p.A
    Inventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
  • Publication number: 20120004266
    Abstract: The invention provides a method of determining whether or not an individual has a predisposition to migraine including the step of determining whether an isolated nucleic acid obtained from the individual comprises a nucleotide sequence corresponding to at least a fragment of a dopamine ?-hydroxylase (DBH) gene promoter, wherein the presence of a ?1021C?T single nucleotide polymorphism (SNP) in said nucleotide sequence indicates whether or not said individual has an increased predisposition to migraine compared to an individual without the polymorphism. DBH ?1021C/C homozygotes are particularly susceptible to migraine. The ?1021T allele may exert a protective effect. The method is particularly suited to detection of a predisposition to migraine with aura in females. The invention also provides a diagnostic kit for detecting a ?1021C?T SNP associated with migraine. The method and kit may facilitate selection of individuals for migraine therapy which targets the dopaminergic system.
    Type: Application
    Filed: June 18, 2008
    Publication date: January 5, 2012
    Applicant: Griffith University
    Inventors: Lynette Robyn Griffiths, Rod A. Lea, Francesca Fernandez
  • Publication number: 20110319378
    Abstract: The present invention provides MDM2 inhibitor compounds of Formula I, wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
    Type: Application
    Filed: June 3, 2011
    Publication date: December 29, 2011
    Applicant: AMGEN INC.
    Inventors: Michael David BARTBERGER, Ana GONZALEZ BUENROSTRO, Hilary Plake BECK, Xiaoqi CHEN, Richard Victor CONNORS, Jeffrey DEIGNAN, Jason DUQUETTE, John EKSTEROWICZ, Benjamin FISHER, Brian Matthew FOX, Jiasheng FU, Zice FU, Felix GONZALEZ LOPEZ DE TURISO, Michael GRIBBLE, JR., Darin James GUSTIN, Julie Anne HEATH, Xin HUANG, Xianyun JIAO, Michael G. JOHNSON, Frank KAYSER, David John KOPECKY, Sujen LAI, Yihong LI, Zhihong LI, Jiwen LIU, Jonathan Dante LOW, Brian Stuart LUCAS, Zhihua MA, Lawrence McGEE, Joel McINTOSH, Dustin McMINN, Julio Cesar MEDINA, Jeffrey Thomas MIHALIC, Steven Howard Olson, Yosup REW, Philip Marley ROVETO, Daqing SUN, Xiaodong WANG, Yingcai WANG, Xuelei YAN, Ming YU, Jiang ZHU
  • Patent number: 8084465
    Abstract: The present invention provides N-substituted-2(1H) pyridones or the pharmaceutical acceptable salts thereof, and the pharmaceutical preparations containing the compounds. The compounds of the present invention can be used to treat various fibrotic diseases effectively, e.g., hepatic fibrosis.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: December 27, 2011
    Assignee: Shanghai Genomics, Inc.
    Inventor: Xianghui Yi
  • Patent number: 8080541
    Abstract: The present invention relates to the use of a compound of formula I wherein R1, R2, R3, R4, X and n are as defined herein or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomers and/or optical isomers for the treatment of psychoses, pain, dysfunction in memory and learning, attention deficit, schizophrenia, dementia disorders or Alzheimer's disease.
    Type: Grant
    Filed: August 19, 2010
    Date of Patent: December 20, 2011
    Assignee: Hoffman-La Roche Inc.
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110294800
    Abstract: The present invention provides, inter alia, a compound of formula I: wherein the substituent designations are indicated in the Specification. The present invention also provides pharmaceutical compositions comprising a compound of formula I, and methods of treatment or prevention of diabetes or hyperglycemia in a patient, and of normalizing blood glucose levels in a subject, by administering an effective amount of a compound of formula I.
    Type: Application
    Filed: August 7, 2009
    Publication date: December 1, 2011
    Applicant: The Trustees Of Columbia University in the City of New York
    Inventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
  • Publication number: 20110281855
    Abstract: The present invention provides a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol. The present invention further provides a method of treating pain and pain related conditions by administering to a patient in need thereof, a dosage form comprising at least one form of tapentadol, with or without a second analgesic, and at least one opioid antagonist, wherein tapentadol is present in an optimal or suboptimal amount and the said antagonist is present in an amount effective to improve the efficacy and or reduce the side effects of tapentadol.
    Type: Application
    Filed: April 21, 2011
    Publication date: November 17, 2011
    Applicant: GRUENENTHAL GMBH
    Inventor: RAMESH SESHA
  • Publication number: 20110281851
    Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.
    Type: Application
    Filed: July 29, 2011
    Publication date: November 17, 2011
    Applicant: THERAVANCE, INC.
    Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
  • Publication number: 20110275673
    Abstract: The invention relates to compounds of Formula (I). Compounds of the present invention are inhibitors of sphingosine kinase 3, and are useful in the treatment of various disorders and conditions, such as inflammatory disorders.
    Type: Application
    Filed: September 17, 2009
    Publication date: November 10, 2011
    Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
  • Patent number: 8053448
    Abstract: This invention provides methods of using compounds of formula Ib below to treat pulmonary disorders. wherein: R4 is hydrogen or (1-4C)alkyl; q is 0, 1, or 2; R5 is independently selected from halo, (1-4C)alkyl, and (1-4C)alkoxy, wherein each alkyl and alkoxy group is optionally substituted with from 1 to 3 fluoro substituents; R7 is hydrogen or (1-4C)alkyl; or a pharmaceuticallly acceptable salt thereof.
    Type: Grant
    Filed: February 10, 2011
    Date of Patent: November 8, 2011
    Assignee: Theravance, Inc.
    Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
  • Publication number: 20110269785
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Application
    Filed: January 7, 2011
    Publication date: November 3, 2011
    Applicant: Purdue Neuroscience Company
    Inventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
  • Publication number: 20110263628
    Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.
    Type: Application
    Filed: June 8, 2011
    Publication date: October 27, 2011
    Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.
    Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
  • Patent number: 8044069
    Abstract: The present application relates to calcium channel inhibitors containing compounds of formula (I) wherein Ar1, Ar2, L1, L2, n, R1, R4, X and Y 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: Grant
    Filed: October 1, 2009
    Date of Patent: October 25, 2011
    Assignees: Abbott Laboratories, Abbott GmbH & Co. KG
    Inventors: Pramila A. Bhatia, George A. Doherty, Irene Drizin, Helmut Mack, Richard J. Perner, Andrew O. Stewart, Qingwei Zhang
  • Publication number: 20110257229
    Abstract: Behavioral pharmacological data with the compound of formula (I), a novel and selective 5HT2A/2C receptor inverse agonist, demonstrate in vivo efficacy in models of psychosis and dyskinesias. This includes activity in reversing MK-801 induced locomotor behaviors, suggesting that this compound may be an efficacious anti-psychotic, and activity in an MPTP primate model of dyskinesias, suggesting efficacy as an anti-dyskinesia agent. These data support the hypothesis that 5HT2A/2C receptor inverse agonism may confer antipsychotic and anti-dyskinetic efficacy in humans, and indicate a use of the compound of formula (I) and related agents as novel therapeutics for Parkinson's Disease, related human neurodegenerative diseases, and psychosis.
    Type: Application
    Filed: June 27, 2011
    Publication date: October 20, 2011
    Inventors: David M. WEINER, Robert E. DAVIS, Mark R. BRANN, Carl-Magnus A. ANDERSSON, Allan K. ULDAM
  • Publication number: 20110250268
    Abstract: The present invention is related to novel oral compositions comprising an irreversible gastric H+/K+-ATPase proton pump inhibitor (PPI) as a gastric acid secretion inhibitor and one or more small carboxylic acid molecules as parietal cell activators in the gastric lumen. Unexpectedly, the compositions of the present invention are capable of enhancing the anti-acid activity of PPI in the stomach. The present invention further relates to a method of using such compositions to reduce gastric acid secretion in a mammal.
    Type: Application
    Filed: April 19, 2011
    Publication date: October 13, 2011
    Inventors: Aleksey Kostadinov, David Ayelet, Sabina Glozman, Tal Atarot
  • Publication number: 20110250256
    Abstract: A dissolvable nano web porous film has a network structure and a large specific surface area. The network structure is formed by stacking nano fibers that have a thickness of 10˜50,000 nm. The nano fibers are formed of a composition comprising nano fiber forming polymer, a gelling agent, a plasticizer, an optional active component and an optional additive. A method of preparing a dissolvable nano web film comprises producing a polymer melt or solution formed of a composition that comprises a nano fiber forming polymer, a gelling agent, a plasticizer, an optional active component and additives, spinning the melt or solution to form a nano web porous film having nano webs stacked in a network structure, drying the nano web porous film, and stabilizing the nano web porous film. The porous film has a 5˜5000 times higher specific surface area and a 2˜20 times faster dissolving time than a conventional film. The dissolvable nano web porous film has excellent dissolvability and solubility.
    Type: Application
    Filed: September 7, 2007
    Publication date: October 13, 2011
    Applicant: GENIC CO, LTD.
    Inventors: Yoo Hyun-Oh, Son Tae-Won
  • Publication number: 20110251164
    Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.
    Type: Application
    Filed: July 1, 2010
    Publication date: October 13, 2011
    Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
  • Publication number: 20110244051
    Abstract: Disclosed herein are pharmaceutical compositions comprising a plurality of first beads each comprising: a core; a first layer comprising pilocarpine or a pharmaceutically acceptable salt thereof; and a second layer comprising a first polymer. Also disclosed are pharmaceutical compositions comprising a plurality of second beads each comprising: a core; and a first layer comprising tolterodine or a pharmaceutically acceptable salt thereof. Further disclosed are pharmaceutical formulations comprising: a) a plurality of the first beads; b) a plurality of the second beads; or c) a plurality of the first beads and a plurality of the second beads.
    Type: Application
    Filed: April 1, 2011
    Publication date: October 6, 2011
    Applicant: THERAVIDA, INC.
    Inventors: Mehdi PABORJI, Roger S. FLUGEL
  • Publication number: 20110237563
    Abstract: The present invention related to the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with critical buccal condition, leading to difficulties in swallowing oral medicine forms and thus difficulties in treating said illnesses. Particularly, the present invention discloses the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for treating illnesses of patient with dysphagia and/or odynophagia and/or aspiration risk. Another aspect of the present invention is the administration of bioactive agents via oral fast dispersing/dissolving drug delivery systems for the treatment of dysphagia and/or odynophagia and/or aspiration risk.
    Type: Application
    Filed: March 23, 2010
    Publication date: September 29, 2011
    Inventor: Dominique Costantini
  • Publication number: 20110237511
    Abstract: This invention relates to potent selective agonists of the EP4 subtype of prostaglandin E2 receptors, their use or a formulation thereof in the treatment of glaucoma and other conditions, which are related to elevated intraocular pressure in the eye of a patient. This invention further relates to the use of the compounds of this invention for mediating the bone modeling and remodeling processes of the osteoblasts and osteoclasts.
    Type: Application
    Filed: June 3, 2011
    Publication date: September 29, 2011
    Applicant: Merck Frosst Canada
    Inventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
  • Patent number: 8026258
    Abstract: The invention relates to a compound of formula (I): Wherein m, n, X, Y, R1, R2, R3 and R4 are as defined herein. The invention also relates to the use of same in therapeutics.
    Type: Grant
    Filed: January 21, 2010
    Date of Patent: September 27, 2011
    Assignee: Sanofi-Aventis
    Inventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
  • Publication number: 20110230504
    Abstract: The present invention relates to compositions and methods for promoting and enhancing the analgesic, anesthetic and anticonvulsant properties of epoxygenated fatty acids, in particular, epoxy-eicosatrienoic acids (“EETs”) and inhibitors of soluble epoxide hydrolase (“sEH”) in the presence of elevated levels of cyclic adenosine monophosphate (“cAMP”) by combining or co-administering the epoxygenated fatty acid, EET and/or inhibitor of sEH with an agent that increases intracellular levels of cAMP, e.g., a phosphodiesterase inhibitor.
    Type: Application
    Filed: September 11, 2009
    Publication date: September 22, 2011
    Applicant: The Regents Of The University Of California Office Of Technology
    Inventors: Bruce D. Hammock, Ahmet Bora Inceoglu, Steven L. Jinks
  • Patent number: 8022087
    Abstract: The present invention provides N-substituted-2(1H) pyridones or the pharmaceutical acceptable salts thereof, and the pharmaceutical preparations containing the compounds. The compounds of the present invention can be used to treat various fibrotic diseases effectively, e.g., hepatic fibrosis.
    Type: Grant
    Filed: September 17, 2010
    Date of Patent: September 20, 2011
    Assignee: Shangai Genomics, Inc.
    Inventor: Xianghui Yi
  • Patent number: 8012955
    Abstract: The present invention provides N-substituted-heterocycloalkyloxybenzamide compounds, as well as pharmaceutical compositions and methods of use. One embodiment of the invention is a compound having the structure in which R1, R2, R3, R4, T, n, w and x are as described herein. In certain embodiments of the invention, a compound of the present invention activates the AMPK pathway, and can be used to treat metabolism-related disorders and conditions.
    Type: Grant
    Filed: December 21, 2007
    Date of Patent: September 6, 2011
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
  • Patent number: 8012993
    Abstract: The present invention relates to stable S-nitrosothiols derivatives of formula (I) having vasodilating effect and which inhibit the aggregation of the platelets and which therefore are useful for the preparation of medicaments for treatment of NO related diseases. The invention also relates to a process for the synthesis of the compounds of formula (I).
    Type: Grant
    Filed: March 1, 2007
    Date of Patent: September 6, 2011
    Assignee: Lacer, S.A.
    Inventors: José Repollés Moliner, Francisco Pubill Coy, Marisabel Mourelle Mancini, Juan Carlos del Castillo Nieto, Lydia Cabeza Llorente, Juan Martínez Bonín, Ana Modolell Saladrigas
  • Publication number: 20110207714
    Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 29, 2009
    Publication date: August 25, 2011
    Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran, Victoria D. Wong, Jill A. Jablonowski, Wenying Chai
  • Publication number: 20110207709
    Abstract: Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.
    Type: Application
    Filed: October 29, 2009
    Publication date: August 25, 2011
    Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran
  • Publication number: 20110201583
    Abstract: The invention provides compounds of formula I: or a pharmaceutically acceptable salt thereof, wherein R1-3, R5-7, a, X, Y, Y?, Y?, and Z are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Application
    Filed: April 28, 2011
    Publication date: August 18, 2011
    Applicant: THERAVANCE, INC.
    Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
  • Patent number: 7994198
    Abstract: Compounds of formula (I); wherein R represents various substituent groups, are useful as inhibitors of glucosylceramide synthase.
    Type: Grant
    Filed: July 17, 2003
    Date of Patent: August 9, 2011
    Assignee: Actelion Pharmaceuticals Ltd.
    Inventors: Mezher Hussein Ali, Michael Glen Orchard
  • Publication number: 20110190350
    Abstract: The present invention provides methods of treating cognitive deficits associated with mental retardation. The methods comprise combining cognitive training protocols and a general administration of phosphodiesterase 4 inhibitors.
    Type: Application
    Filed: January 10, 2011
    Publication date: August 4, 2011
    Inventors: Timothy P. Tully, Filippo Cavalieri, Rusiko Bourtchouladze
  • Patent number: 7989630
    Abstract: P-glycoprotein transporter (P-gp) acts as a pump at the blood-brain barrier to exclude a wide range of xenobiotics (e.g., toxins, drugs, etc.) from the brain and is also expressed in a tumor in response to exposure to established or prospective chemotherapeutics (a phenomenon known as multidrug resistance). This invention concerns the preparation and use of radiotracers for imaging P-gp function in vitro and in vivo. Radiotracers of the present invention are avid substrates for P-gp and have structures based on N-Desmethyl-loperamide.
    Type: Grant
    Filed: April 30, 2008
    Date of Patent: August 2, 2011
    Assignee: National Institutes of Health Represented by the Secretary of the Department of Health and Human Services, National Institutes of Health
    Inventors: Victor W. Pike, Robert B. Innis, Sami S. Zoghbi, Neva Lazarova
  • Publication number: 20110178068
    Abstract: The invention provides a method of sustained delivery of a tertiary amine-containing parent drug comprising administering to a patient an effective amount of a prodrug compound of the invention wherein upon administration to the patient, release of the parent drug from the prodrug is sustained release. Prodrug compounds suitable for use in the methods of the invention are labile quaternary ammonium salts of tertiary amine-containing parent drugs (or tertiary imine-containing parent drugs) that are derivatized through aldehyde-linked prodrug moieties that reduce the solubility of the prodrug compound at a reference pH as compared to the parent drug. The physical, chemical and solubility properties of these derivatives can be further modulated by the choice of counterion X?. In one embodiment, the present invention provides a prodrug compound of Formula I: where R1-R5 are defined in the written description of the invention.
    Type: Application
    Filed: December 23, 2010
    Publication date: July 21, 2011
    Applicant: Alkermes, Inc.
    Inventors: Orn Almarsson, Laura Cook Blumberg, Julius F. Remenar
  • Publication number: 20110178077
    Abstract: The present invention relates to small molecule compounds and their use in the treatment of bacterial infections, in particular Tuberculosis.
    Type: Application
    Filed: June 17, 2009
    Publication date: July 21, 2011
    Inventors: Priscille Brodin, Thierry Christophe, Zaesung No, Jaeseung Kim, Auguste Genovesio, Denis Philippe Cedric Fenistein, Heekyoung Jeon, Fanny Anne Ewann, Sunhee Kang, Saeyeon Lee, Min Jung Seo, Eunjung Park, Monica Contreras Dominguez, Ji Youn Nam, Eun Hye Kim
  • Publication number: 20110178066
    Abstract: Chemical agents, such as derivatives of hydroxypiperidine moieties, and similar heterocyclic ring structures, including salts thereof, that act as anti-cancer and anti-tumor agents, especially where such agents modulate the activity of enzymes and structural polypeptides present in cells, such as cancer cells, or where the agents modulate levels of gene expression in cellular systems, including cancer cells, are disclosed, along with methods for preparing such agents, as well as pharmaceutical compositions containing such agents as active ingredients and methods of using these as therapeutic agents.
    Type: Application
    Filed: July 21, 2010
    Publication date: July 21, 2011
    Inventors: Norman E. Ohler, Jeffrey W. Watthey, Qin Zong, Paul E. Young, Kathryn J. Strand, Stanislaw Pikul
  • Publication number: 20110172230
    Abstract: [Object] To provide a compound which can be used for the treatment of a disease associated with fatty acid amide hydrolase (FAAH), particularly urinary frequency, urinary incontinence and/or overactive bladder. [Means for solution] It is confirmed that a urea compound chemical-structurally characterized by having a piperidine or piperazine ring or a salt thereof has an excellent FAAH-inhibitory activity, and thus the present invention is completed. The urea compound or its pharmaceutically acceptable salt of the present invention can increase the effective bladder capacity and ameliorate the state of urinary frequency, and is therefore useful as an agent for treating urinary frequency, urinary incontinence and/or overactive bladder.
    Type: Application
    Filed: August 22, 2007
    Publication date: July 14, 2011
    Inventors: Takahiro Ishii, Takashi Sugane, Akio Kakefuda, Tatsuhisa Takahashi, Tokatoshi Kanayama, Kentaro Sato, Ikumi Kuriwaki, Chika Kitada, Jotaro Suzuki
  • Publication number: 20110160223
    Abstract: Provided are pharmaceutical compositions and methods of treatment or prophylaxis of certain neuropsychiatric conditions, in particular mood disorders. The compounds are of the general Formula I-V as described herein.
    Type: Application
    Filed: November 2, 2010
    Publication date: June 30, 2011
    Inventors: Raymond J. Dingledine, Stephen F. Traynelis
  • Publication number: 20110159058
    Abstract: The film preparation of the present invention includes: a drug-containing intermediate layer containing loperamide hydrochloride, a terpene and a film-forming agent; and coating layers containing a film-forming agent and a plasticizer (but not a terpene) and laminated on both sides of the drug-containing intermediate layer. As a bitter taste derived from loperamide hydrochloride is thereby masked, uncomfortable sensation when taking the film preparation can be reduced. Furthermore, as this film preparation is rapidly dissolved (i.e., has a rapidly dissolving property) only with moisture in the oral cavity, it begins to work quickly and is very convenient when it is carried and taken.
    Type: Application
    Filed: August 25, 2009
    Publication date: June 30, 2011
    Applicants: KYUKYU PHARMACEUTICAL CO., LTD., KOWA CO., LTD.
    Inventors: Tsutomu Awamura, Hisanobu Nishikawa, Toshio Inagi
  • Patent number: 7968124
    Abstract: Methods of attenuating the toxic or medically undesirable effects of drugs and toxins in a human by administering to a human an injectable formulation comprised of a dispersion of particles comprised of reversed cubic or reversed hexagonal lyotropic liquid crystalline material. The particles absorb or adsorb or otherwise sequester and attenuate the effect of drugs and toxins, and may be used as a rescue or reversal agent, or as a prophylaxis. The invention is especially applicable in reversing adverse effects of local anesthetics inadvertently delivered systemically, and attenuating the therapeutic effects of general anesthetics in the course of treatment.
    Type: Grant
    Filed: December 6, 2007
    Date of Patent: June 28, 2011
    Assignee: Lyotropic Therapeutics, Inc.
    Inventors: David M. Anderson, Vincent M. Conklin, Benjamin G. Cameransi