Chalcogen Bonded Directly To Ring Carbon Of The Piperidine Ring Patents (Class 514/327)
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Patent number: 8211916Abstract: N- and O-substituted 4[2-diaromaticmethoxy and methylamino)alkyl] piperidines exhibit high CNS activity with respect to the dopamine transporter (DAT) and serotonin transporter (SERT). Preferred compounds exhibit highly differential behavior as between the DAT and SERT and between the DAT and the norepinephrine transporter (NET). The compounds have utility in treating CNS disorders, including but not limited to cocaine addiction, depression, and Parkinson's disease.Type: GrantFiled: January 22, 2008Date of Patent: July 3, 2012Assignee: Wayne State UniversityInventor: Aloke K. Dutta
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Patent number: 8198304Abstract: 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: GrantFiled: September 9, 2011Date of Patent: June 12, 2012Assignee: Theravance, Inc.Inventors: YuHua Ji, Craig Husfeld, YongQi Mu, Rick Lee, Li Li
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Publication number: 20120142659Abstract: The invention relates to compounds according to Formula I: or a pharmaceutically acceptable salt thereof, wherein m, n, R1, R2, R3, R4, R5, x and y are as defined herein. Compounds according to Formula I are pharmacologically effective as potassium channel inhibitors, in particular inhibitors of the acetylcholine operated inward rectifying potassium channel current (i.e. IKACh blockers), and are believed to be useful in the treatment of cardiac arrhythmias, in particular supraventricular tacharrhythmias, such as atrial fibrillation and atrial flutter.Type: ApplicationFiled: November 29, 2011Publication date: June 7, 2012Applicant: ASTRAZENECA ABInventors: Jonas Bostrõm, Hans Emtenäs, Kenneth Granberg, Mickael Mogemark, Antonio Llinas
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Publication number: 20120141471Abstract: The present invention includes compositions that are useful in preventing or treating metastasis in a subject diagnosed with cancer. The present invention also includes methods of preventing or treating metastasis in a subject diagnosed with cancer, wherein the method comprises administering to the subject in need thereof an effective amount of a pharmaceutical formulation comprising at least one pharmaceutically acceptable carrier and at least one CX3CR1 or fractalkine antagonist.Type: ApplicationFiled: December 6, 2011Publication date: June 7, 2012Inventors: Joseph M. Salvino, Olimpia Meucci, Alessandro Fatatsis, Whitney L. Jamieson
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Publication number: 20120129888Abstract: Novel compounds are continually sought after to treat and prevent disorders. The invention relates to N-(2-oxo-1-phenylpiperidin-3-yl)sulfonamides useful for contributing to the search and identification of new lead compounds which can modulate the functional activity of a biological target.Type: ApplicationFiled: December 22, 2011Publication date: May 24, 2012Inventors: JOSEP CASTELLS BOLIART, David Enrique Miguel Centeno, Marta Pascual Gilabert
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Publication number: 20120122792Abstract: S-t-butyl protected cysteine di-peptide analogs and related compounds and methods of using these compounds for the treatment of diseases and/or conditions, including but not limited to diseases and/or conditions of Central Nervous System (CNS).Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: PROMENTIS PHARMACEUTICALS, INC.Inventors: Edward M. Johnson, II, Daniel G. Lawton
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Publication number: 20120122850Abstract: 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: ApplicationFiled: January 11, 2012Publication date: May 17, 2012Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20120115910Abstract: This application describes compositions of receptor inhibitors, including typical antipsychotic agents, for example haloperidol, and methods of use for treating clinical signs or symptoms of Parkinson's disease. Furthermore, this application describes compositions and methods to induce supersensitivity in dopamine D2 and other receptors involved in Parkinson's disease as a means of alleviating the clinical signs or symptoms of Parkinson's disease.Type: ApplicationFiled: July 30, 2010Publication date: May 10, 2012Applicant: Clera Inc.Inventor: Philip Seeman
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Publication number: 20120114767Abstract: An assay for a GCH1 allele and associated genotype for the screening, prediction, diagnosis, prognosis, treatment and treatment response of psychiatric, neuropsychiatric, and neurological disorders, such as schizophrenia, schizoaffective disorder and bipolar disorder, and for defining treatments of such disorders. The presence of a variant in the GCH1 gene, alone or in conjunction with a measurement of low or altered biopterin, or altered BH4 system measures, is used to screen or diagnose subjects at risk for developing a psychiatric, neuropsychiatric, or neurological disorder. The genetic assay, with or without a biopterin or BH4 system assay, may also be used to determine treatment regimens. For subjects with an impaired BH4 system, treatments to increase or normalize biopterin, BH4, or the BH4 system can also be used, such as BH4 supplementation, lithium treatment, phenylalanine treatment, or other treatments and therapies.Type: ApplicationFiled: December 12, 2011Publication date: May 10, 2012Applicant: THE RESEARCH FOUNDATION FOR MENTAL HYGIENEInventors: James D. Clelland, Catherine L. Clelland
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Publication number: 20120108545Abstract: Monomeric and dimeric trioxane fluoroaryl amides, 5-carbon-linked, C-10 non-acetal trioxane dimer esters; trioxane silylamides; and trioxane dimer orthoesters and methods of their use for treating subjects infected with malaria or other parasitic infectious diseases including, but not limited to, toxoplasmic infection; subjects afflicted with psychiatric conditions associated with toxoplasmic infection; and subjects afflicted with cancer.Type: ApplicationFiled: May 19, 2010Publication date: May 3, 2012Applicant: THE JOHNS HOPKINS UNIVERSITYInventors: Gary H. Posner, Lauren E. Woodard, David R. Levine, Deuk Kyu Moon, Bryan T. Mott
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Publication number: 20120108570Abstract: The present invention relates generally to pharmacological methods for the prevention of amelioration of sleep-related breathing disorders via administration of agents or combinations of agents that possess serotonin-related pharmacological activity.Type: ApplicationFiled: January 6, 2012Publication date: May 3, 2012Applicant: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOISInventors: Miodrag Radulovacki, David W. Carley
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PHARMACEUTICAL COMPOSITIONS AND METHODS OF USE OF SALICYLANILIDES FOR TREATMENT OF HEPATITIS VIRUSES
Publication number: 20120108592Abstract: A new class of salicylanilides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol -
Publication number: 20120093929Abstract: The present invention relates to a composition, comprising (i) a matrix made of polymeric nanofibers, and (ii) an opioid agonist within the matrix.Type: ApplicationFiled: May 5, 2009Publication date: April 19, 2012Applicant: Euro-Celtique S.A.Inventors: Alexander Oksche, Kevin J. Smith, Derek Prater, Malcolm Walden, Will Heath, Bernard Kennedy, Vanessa Addison, Hassan Mohammad
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Publication number: 20120065206Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: ApplicationFiled: December 1, 2009Publication date: March 15, 2012Applicant: SYNTA PHARMACEUTICALS CORP.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Publication number: 20120058186Abstract: 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: ApplicationFiled: March 29, 2010Publication date: March 8, 2012Applicant: TORAY INDUSTRIES, INC.Inventors: Suguru Takaki, Kotoe Ohta, Yasuhide Horiuch
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Publication number: 20120058201Abstract: 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: ApplicationFiled: April 5, 2010Publication date: March 8, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Christian Lavedan, Simona Volpi, Louis Licamele
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Patent number: 8129414Abstract: 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: GrantFiled: June 19, 2007Date of Patent: March 6, 2012Inventor: Adeboye Adejare
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Patent number: 8129376Abstract: 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: GrantFiled: March 20, 2009Date of Patent: March 6, 2012Inventors: Kumar Sundaresan, P. Bala Koteswara Rao, Bharathiraja Ainan, Hariharasubramanian Ayyamperumal, Girish A R, Srinivas Tatiparthy, Ganesh Prabhu, Hosahalli Subramanya, Alexander Bischoff
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Publication number: 20120046247Abstract: 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: ApplicationFiled: August 16, 2011Publication date: February 23, 2012Inventors: Charles C-Y Shih, Toshio Kitamura, Qian Shi, Toshiyuki Kawashima, Hui-Kang Wang
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Patent number: 8119563Abstract: 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: GrantFiled: October 4, 2004Date of Patent: February 21, 2012Assignee: FMC CorporationInventors: George Theodoridis, David Rosen, Shunxiang Zhang, Walter H. Yeager, Robert N. Henrie, II, Syed Z. Ahmed, Hongbin Men, Stephen Donovan
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Publication number: 20120029021Abstract: 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: ApplicationFiled: January 17, 2011Publication date: February 2, 2012Applicant: THE TRUSTEES OF CALIFORNIA STATE UNIVERSITYInventors: Yong Ba, Errol V. Mathias
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Publication number: 20120022076Abstract: 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: ApplicationFiled: September 23, 2011Publication date: January 26, 2012Inventors: Andreas MADERNA, Jean-Michel Vernier, Dinesh Barawkar, Varaprasad Chamakura, Hassan El Abdellaoul, Dinesh Barawkar, Zhi Hong
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Patent number: 8093386Abstract: 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: GrantFiled: July 25, 2007Date of Patent: January 10, 2012Assignee: Bracco Imaging S.p.AInventors: Armando Rossello, Elisabetta Orlandini, Aldo Balsamo, Laura Panelli, Elisa Nuti
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Patent number: 8093391Abstract: 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: GrantFiled: January 5, 2010Date of Patent: January 10, 2012Assignee: Sterling Biotech Research CenterInventors: Sugata Chatterjee, Ajay Singh Rawat, Anil V. Pawar, Jetti Rajanikanth, Penigandla Venkateswarlu
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Publication number: 20120004266Abstract: 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: ApplicationFiled: June 18, 2008Publication date: January 5, 2012Applicant: Griffith UniversityInventors: Lynette Robyn Griffiths, Rod A. Lea, Francesca Fernandez
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Publication number: 20110319378Abstract: 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: ApplicationFiled: June 3, 2011Publication date: December 29, 2011Applicant: 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
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Patent number: 8084465Abstract: 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: GrantFiled: September 17, 2010Date of Patent: December 27, 2011Assignee: Shanghai Genomics, Inc.Inventor: Xianghui Yi
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Patent number: 8080541Abstract: 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: GrantFiled: August 19, 2010Date of Patent: December 20, 2011Assignee: Hoffman-La Roche Inc.Inventors: Sabine Kolczewski, Emmanuel Pinard
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Publication number: 20110294800Abstract: 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: ApplicationFiled: August 7, 2009Publication date: December 1, 2011Applicant: The Trustees Of Columbia University in the City of New YorkInventors: Yuli Xie, Shixian Deng, Donald W. Landry, Paul Harris, Antonella Maffei
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Publication number: 20110281855Abstract: 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: ApplicationFiled: April 21, 2011Publication date: November 17, 2011Applicant: GRUENENTHAL GMBHInventor: RAMESH SESHA
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Publication number: 20110281851Abstract: 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: ApplicationFiled: July 29, 2011Publication date: November 17, 2011Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20110275673Abstract: 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: ApplicationFiled: September 17, 2009Publication date: November 10, 2011Inventors: Yibin Xiang, Bradford Hirth, John L. Kane, Junkai Liao, Kevin Noson, Christopher Yee
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Patent number: 8053448Abstract: 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: GrantFiled: February 10, 2011Date of Patent: November 8, 2011Assignee: Theravance, Inc.Inventors: Mathai Mammen, YuHua Ji, YongQi Mu, Craig Husfeld, Li Li
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Publication number: 20110269785Abstract: 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: ApplicationFiled: January 7, 2011Publication date: November 3, 2011Applicant: Purdue Neuroscience CompanyInventors: Nancy C. Lan, Yan Wang, Sui Xiong Cai
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Publication number: 20110263628Abstract: 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: ApplicationFiled: June 8, 2011Publication date: October 27, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Patent number: 8044069Abstract: 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: GrantFiled: October 1, 2009Date of Patent: October 25, 2011Assignees: Abbott Laboratories, Abbott GmbH & Co. KGInventors: Pramila A. Bhatia, George A. Doherty, Irene Drizin, Helmut Mack, Richard J. Perner, Andrew O. Stewart, Qingwei Zhang
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Publication number: 20110257229Abstract: 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: ApplicationFiled: June 27, 2011Publication date: October 20, 2011Inventors: David M. WEINER, Robert E. DAVIS, Mark R. BRANN, Carl-Magnus A. ANDERSSON, Allan K. ULDAM
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Publication number: 20110250268Abstract: 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: ApplicationFiled: April 19, 2011Publication date: October 13, 2011Inventors: Aleksey Kostadinov, David Ayelet, Sabina Glozman, Tal Atarot
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Publication number: 20110251164Abstract: The invention relates to compounds of formula processes and intermediates for their preparation, their use as muscarinic antagonists and pharmaceutical composition containing them.Type: ApplicationFiled: July 1, 2010Publication date: October 13, 2011Inventors: Paul Alan Glossop, Simon John Mantell, Anthony Wood, Christine Anne Louise Watson
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Publication number: 20110250256Abstract: 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: ApplicationFiled: September 7, 2007Publication date: October 13, 2011Applicant: GENIC CO, LTD.Inventors: Yoo Hyun-Oh, Son Tae-Won
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Publication number: 20110244051Abstract: 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: ApplicationFiled: April 1, 2011Publication date: October 6, 2011Applicant: THERAVIDA, INC.Inventors: Mehdi PABORJI, Roger S. FLUGEL
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Publication number: 20110237511Abstract: 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: ApplicationFiled: June 3, 2011Publication date: September 29, 2011Applicant: Merck Frosst CanadaInventors: Xavier Billot, John Colucci, Yongxin Han, Marie-Claire Wilson, Robert N. Young
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Publication number: 20110237563Abstract: 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: ApplicationFiled: March 23, 2010Publication date: September 29, 2011Inventor: Dominique Costantini
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Patent number: 8026258Abstract: 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: GrantFiled: January 21, 2010Date of Patent: September 27, 2011Assignee: Sanofi-AventisInventors: Ahmed Abouabdellah, Antonio Almario Garcia, Jacques Froissant, Christian Hoornaert
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Publication number: 20110230504Abstract: 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: ApplicationFiled: September 11, 2009Publication date: September 22, 2011Applicant: The Regents Of The University Of California Office Of TechnologyInventors: Bruce D. Hammock, Ahmet Bora Inceoglu, Steven L. Jinks
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Patent number: 8022087Abstract: 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: GrantFiled: September 17, 2010Date of Patent: September 20, 2011Assignee: Shangai Genomics, Inc.Inventor: Xianghui Yi
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Patent number: 8012993Abstract: 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: GrantFiled: March 1, 2007Date of Patent: September 6, 2011Assignee: 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
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Patent number: 8012955Abstract: 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: GrantFiled: December 21, 2007Date of Patent: September 6, 2011Assignee: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Jiaxin Yu, Hui Hong, Sambaiah Thota, Xiang Xu, Ihab S. Darwish
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Publication number: 20110207709Abstract: Certain biphenyl compounds are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran
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Publication number: 20110207714Abstract: The biphenyic compounds of formula (I) are serotonin modulators useful in the treatment of serotonin-mediated diseases.Type: ApplicationFiled: October 29, 2009Publication date: August 25, 2011Inventors: Nicholas I. Carruthers, Brock T. Shireman, Vi T. Tran, Victoria D. Wong, Jill A. Jablonowski, Wenying Chai