Chalcogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/424)
-
Publication number: 20110064807Abstract: An extended release pharmaceutical composition of Levetiracetam with once a day dosage regime and the process of preparing it. The extended release tablet of Levetiracetam is with the core comprising of Levetiracetam and water dispersible rate controlling polymer, and the tablet core is optionally functional coated comprising a combination of water non-dispersible and/or water dispersible polymer. It provides extended therapeutically effective plasma levels over a twenty four hour period with diminished incidences of neuropsychiatric adverse events by eliminating the troughs and peaks of drug concentration in a patients blood plasma, which comprises administering orally to a patient in need thereof, an extended release tablet that provides a peak blood plasma level of Levetiracetam in from about eight to about Sixteen hours. The core is prepared by Wet granulation, Dry granulation or Direct compression and optionally the tablet core is coated either in an coating pan or in and Fluidized bed system.Type: ApplicationFiled: November 9, 2010Publication date: March 17, 2011Applicant: UCB Pharma S.A.Inventors: Rajesh Kshirsagar, Mayank Joshi, Yogesh Raichandani
-
Publication number: 20110064808Abstract: The present invention relates to extended release pharmaceutical compositions of Levetiracetam and processes for preparing the same. The extended release tablet of Levetiracetam is with a core comprising of Levetiracetam and water dispersible rate controlling polymer, and the tablet core is optionally functional coated comprising a combination of water non-dispersible and/or water dispersible polymer. It provides extended therapeutically effective plasma levels over a twenty four hour period with diminished incidences of neuropsychiatric adverse events by eliminating the troughs and peaks of drug concentration in a patient's blood plasma. The composition also exhibits no food effect.Type: ApplicationFiled: November 12, 2010Publication date: March 17, 2011Applicant: UCB Pharma S.A.Inventors: Rajesh Kshirsagar, Ashwin Rao, Nilesh Malaviya, Kaustubh Jinturkar
-
Publication number: 20110059909Abstract: The present invention relates generally to the fields of molecular biology. More particularly, it concerns materials and methods for the treatment of nitric oxide and cytokind mediated disorders. In a preferred embodiment, PDMP may be used to inhibit the expression of iNOS and pro-inflammatory cytokines such as TNF? and IL1?.Type: ApplicationFiled: March 30, 2010Publication date: March 10, 2011Inventors: Inderjit Singh, Avtar Singh
-
Publication number: 20110053914Abstract: A pharmaceutical combination comprising: (a) at least one 6-dimethylaminomethyl-1-(3-methoxy-phenyl)-cyclohexane-1,3-diol component and/or at least one 6-dimethylaminomethyl-1-(3-hydroxy-phenyl)-cyclohexane-1,3-diol component, and (b) at least one antiepileptic; a pharmaceutical composition comprising said combination, a medicament comprising such a combination, a kit containing the ingredients of such a combination, and a method of treating pain in which components (a) and (b) are administered simultaneously or sequentially, whereby component (a) may be administered before or after component (b), and in which components (a) and (b) are administered either via the same or a different pathway of administration.Type: ApplicationFiled: August 27, 2010Publication date: March 3, 2011Applicant: Gruenenthal GmbHInventors: Klaus SCHIENE, Petra Bloms-Funke
-
Publication number: 20110053904Abstract: 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: ApplicationFiled: August 19, 2010Publication date: March 3, 2011Inventors: Sabine Kolczewski, Emmanuel Pinard
-
Publication number: 20110052556Abstract: The present invention refers to a pharmaceutical composition comprising racetam and carnitine. Said pharmaceutical composition may further comprise coenzyme Q10 and/or agent associated with mitochondrial and/or metabolic disturbance, such as hypocholesterolemic agent of the statins group, a hypoglycemic agent, or an antiepileptic agent. The invention also includes a method of treatment for mitochondrial disturbances comprising administration of the pharmaceutical composition of the invention.Type: ApplicationFiled: February 27, 2009Publication date: March 3, 2011Applicant: Biolab Sanus Farmaceutical LtdaInventors: José Roberto da Costa Perreira, Marcio Falci, Mauricio Matteis Alario
-
Publication number: 20110046174Abstract: The present invention concerns methods useful in treating a subject having diarrhea-predominant IBS (IBS-D) by administering N-methyl-N-[(1S)-1-phenyl-2-((3S)-3-hydroxypyrrolidin-1-yl)ethyl]-2,2-diphenylacetamide and/or a pharmaceutically acceptable salt thereof to the subject.Type: ApplicationFiled: November 5, 2010Publication date: February 24, 2011Applicant: Tioga Pharmaceuticals, Inc.Inventor: Allen MANGEL
-
Publication number: 20110039853Abstract: Novel substituted benzamide based inhibitors, their use in therapy, pharmaceutical compositions comprising the compounds, the use of said compounds in the manufacture of medicaments, and therapeutic methods comprising the administration of said compounds are described. The present compounds modulate the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and are accordingly useful in the treatment of diseases in which such a modulation is beneficial, such as the metabolic syndrome.Type: ApplicationFiled: February 19, 2008Publication date: February 17, 2011Inventor: Soren Ebdrup
-
Publication number: 20110033538Abstract: The present invention relates to a pharmaceutical formulation of solid dosage forms comprising a therapeutically effective amount of a pyrrolidone anticonvulsant agent, and in particular Levetiracetam or a pharmaceutical acceptable salt or derivative thereof, in combination with an effective diluent, such as Dibasic Calcium Phosphate, and additional pharmaceutical excipients, and a process for the preparation thereof by wet granulation.Type: ApplicationFiled: October 16, 2007Publication date: February 10, 2011Applicant: PHARMATHEN S.A.Inventors: Evangelos Karavas, Efthimios Koutris, Dimitrios Bikiaris, Vicky Samara, Ioanna Koutri, Eleni Stathaki
-
Publication number: 20110027359Abstract: The present invention relates to a pharmaceutical composition comprising levetiracetam as active ingredient, the invention relates specifically to a prolonged release formulation.Type: ApplicationFiled: March 10, 2010Publication date: February 3, 2011Applicant: UCB, S.A.Inventors: Caroline Goffin, Monique Berwaer, Michaël Boonen, Michel Deleers, Domenico Fanara
-
Publication number: 20110028476Abstract: A proton pump inhibitor containing a compound represented by the formula (I) wherein X and Y are the same or different and each is a bond or a spacer having 1 to 20 carbon atoms in the main chain, R1 is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, R2, R3 and R4 are the same or different and each is a hydrogen atom, an optionally substituted hydrocarbon group, an optionally substituted thienyl group, an optionally substituted benzo[b]thienyl group, an optionally substituted furyl group, an optionally substituted pyridyl group, an optionally substituted pyrazolyl group, an optionally substituted pyrimidinyl group, an acyl group, a halogen atom, a cyano group or a nitro group, R5 and R6 are the same or different and each is a hydrogen atom or an optionally substituted hydrocarbon group, which has a superior proton pump action and shows an antiulcer activity and the like after conversion to a proton pump inhibitor in the body, or a salt thereof.Type: ApplicationFiled: September 1, 2010Publication date: February 3, 2011Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
-
Publication number: 20110023876Abstract: Compositions, methods and systems are provided for pulmonary delivery of long-acting muscarinic antagonists and long-acting ?2 adrenergic receptor agonists via a metered dose inhaler. In particular embodiments, the compositions include a suspension medium, active agent particles, and suspending particles, in which the active agent particles and suspending particles form a co-suspension within the suspension medium.Type: ApplicationFiled: May 28, 2010Publication date: February 3, 2011Applicant: PEARL THERAPEUTICS, INC.Inventors: Reinhard Vehring, Michael Steven Hartman, Adrian Edward Smith, Vidya B. Joshi, Sarvajna Kumar Dwivedi
-
Publication number: 20110028510Abstract: The present invention provides compositions, methods, and kits for treating or preventing a viral infection (e.g., an infection caused by an influenza virus).Type: ApplicationFiled: February 18, 2010Publication date: February 3, 2011Applicants: COMBINATORX (SINGAPORE) PTE. LTD., EXCRX (Singapore) PTE. LTD. (F.K.A. CombinatoRx (Singapore) PTE. LTD.Inventors: Ralf Altmeyer, Geeta Sharma, Danilal Champalal Sharma, Vishal Vikas Pendharkar
-
Publication number: 20110021508Abstract: The present invention relates to compositions comprising a combination of PKC activators and PKC inhibitors and methods to modulate ?-secretase activity; improve or enhance cognitive ability; and or reduce neurodegeneration in individuals suffering from diseases that impair cognitive ability, particularly Alzheimer's Disease. The invention also relates to methods for improving or enhancing cognitive ability. The present invention also provides methods for increasing the generation of non-amyloidogenic soluble APP (sAPP) comprising the activation of protein kinase C (PKC) in the brain and inhibiting PKC in peripheral tissues. Macrocyclic lactones (i.e. bryostatin class and neristatin class) are preferred PKC activators and Vitamin E is a preferred PKC inhibitor for use in the inventive composition.Type: ApplicationFiled: September 16, 2010Publication date: January 27, 2011Applicant: BLANCHETTE ROCKEFELLER NEUROSCIENCES INSTITUTEInventor: Daniel Alkon
-
Publication number: 20110020445Abstract: Extended release pharmaceutical compositions of levetiracetam or pharmaceutically acceptable salts thereof in the form of a tablet comprising glyceryl behenate and a polymethacrylate polymer with at least one pharmaceutically acceptable excipient.Type: ApplicationFiled: July 19, 2010Publication date: January 27, 2011Applicant: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETIInventors: Hasan Ali Turp, Gulay Yelken, Asiye Sezgia, Ali Turkyilmaz, Levent Oner
-
Publication number: 20110021505Abstract: The present invention relates to the use of sulfonyl-substituted 2-sulfonylaminobenzoic acid N-phenylamides of the formula I, wherein A and R1 to R6 have the meanings indicated in the claims, for treating pain and for manufacturing a medicament for the treatment of pain.Type: ApplicationFiled: March 30, 2010Publication date: January 27, 2011Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBHInventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
-
Publication number: 20110003792Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(1?-methylcyclohexylcarbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2—; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alklylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyType: ApplicationFiled: September 7, 2010Publication date: January 6, 2011Applicant: CAMBRIDGE ENTERPRISE LIMITEDInventors: David J. Grainger, David John Fox
-
Patent number: 7863317Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the prevention of asthma, multiple sclerosis, artherosclerosis, and rheumatoid arthritis.Type: GrantFiled: February 15, 2007Date of Patent: January 4, 2011Assignee: Bristol-Myers Squibb CompanyInventor: Percy H. Carter
-
Publication number: 20100324025Abstract: Antibacterial compounds of formula I are provided: As well as stereoisomers, pharmaceutically acceptable salts, esters, and prodrugs thereof; pharmaceutical compositions comprising such compounds; methods of treating bacterial infections by the administration of such compounds; and processes for the preparation of the compounds.Type: ApplicationFiled: September 21, 2009Publication date: December 23, 2010Applicant: University of WashingtonInventors: Niels H. Andersen, Jason Bowman, Alice L. Erwin, Eric A. Harwood, Toni Kline, Khisimuzi E. Mdluli, Simon Ng, Keith B. Pfister, Ribhi Shawar, Allan S. Wagman, Asha Yabannavar
-
Publication number: 20100324009Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 23, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
-
Publication number: 20100317644Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
-
Publication number: 20100311711Abstract: Compounds and pharmaceutical compositions are contemplated that inhibit N-acyl-ethanolamine-hydrolyzing acid amidase (NAAA) to so increase the concentration of the substrate of NAAA, palmitoylethanolamide (PEA). NAAA inhibition is contemplated to be effective to alleviate conditions associated with a reduced concentration of PEA. Among other uses, various NAAA inhibitors are especially contemplated as therapeutic agents in the treatment of inflammatory diseases.Type: ApplicationFiled: October 10, 2008Publication date: December 9, 2010Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
-
Publication number: 20100310652Abstract: An extended release pharmaceutical composition comprising levetiracetam. A coated extended release pharmaceutical composition comprising levetiracetam wherein the core is coated with a rate controlling composition.Type: ApplicationFiled: December 22, 2008Publication date: December 9, 2010Applicant: Alembic LimitedInventors: Rajesh Kshirsagar, Ashwin Rao, Atul Kathiriya
-
Publication number: 20100311794Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventor: Chandrasekar Venkataramani
-
Publication number: 20100310500Abstract: The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.Type: ApplicationFiled: June 7, 2010Publication date: December 9, 2010Applicant: Gilead Sciences, Inc.Inventors: Michael Graupe, Chandrasekar Venkataramani
-
Patent number: 7842730Abstract: Medicine, in particular medications for treating blood losses, hypoxic and ishemic states, for improving a blood oxygen supply and for preserving isolated perfused organs and tissues. The inventive medical emulsion of perfluororganic compounds includes rapidly excretable perfluororganic compounds such as perfluordecalin, perfluoractilbromide, a perfluoroganic additive embodied in the form of a mixture of perfluorinated tertiary amines and phospholipids in the form of a water-salt dispersion. The perfluordecalin and perfluoractilbromide are contained in the composition of the rapidly excretable perfluororganic compounds at a ratio ranging from 10:1 to 1:10. The mixture of perfluorinated tertiary amines is embodied in the form of the mixture of perfluorotpripropylamine and the co-products thereof: cis- and trans-isomers perfluor-1-propyl 3,4-dimethylpirrolidone and perfluor-1-propyl-4-methhylpiperidine.Type: GrantFiled: February 7, 2005Date of Patent: November 30, 2010Inventors: Irina Nikolaievna Kuznetsova, Evgeny Ilich Maievsky
-
Patent number: 7842820Abstract: Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective HDAC inhibitors.Type: GrantFiled: March 10, 2005Date of Patent: November 30, 2010Assignee: 4SC AGInventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
-
Publication number: 20100292296Abstract: Novel ligand compounds having the general formula (I): and pharmaceutical/cosmetic compositions comprised thereof are useful in human and veterinary medicine or, alternatively, in cosmetics.Type: ApplicationFiled: July 23, 2010Publication date: November 18, 2010Applicant: Galderma Research & DevelopmentInventors: Thibaud BIADATTI, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
-
Publication number: 20100286204Abstract: There is provided a compound having Formula I wherein each of R1, R2, R3, R4, R5, R6, R7, R8 and R9 are independently selected from (a) H, (b) R13, —OC(R13)3, —OCH(R13)2, —OCH2R13, C(R13)3, —CH(R13)2, or —CH2R13 wherein R13 is a halogen; (c) —CN; (d) optionally substituted alkyl, (e) optionally substituted heteroalkyl; (f) optionally substituted aryl; (g) optionally substituted heteroaryl; (h) optionally substituted arylalkyl; (i) optionally substituted heteroarylalkyl; (j) hydroxy; (k) alkoxy; (l) aryloxy; (m) —SO2-alkyl; and (n) —N(R14)C(O)R15, wherein R14 and R15 are independently selected from H and hydrocarbyl, wherein the optional substituents of (d) (e) (f) (h) and (i) are selected from the group consisting of: C1-6 alkyl, halo, cyano, nitro, haloalkyl, hydroxy, C1-6 alkoxy, carboxy, carboxyalkyl, carboxamide, mercapto, amino, alkylamino, dialkylamino, sulfonyl, sulfonamido, aryl and heteroaryl; wherein n and p are independently selected from 0 and 1; X is an optional group selected from O, S, S=0Type: ApplicationFiled: November 19, 2008Publication date: November 11, 2010Applicant: Sterix LimitedInventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
-
Publication number: 20100286207Abstract: The present invention is related to new 2-oxo-cyclic compound, the process for preparing them and a pharmaceutical composition comprising the same. The present invention provides a pharmaceutical composition for preventing and treating the inflammatory disease comprising the pain or inflammation caused by rheumatic disease, for example, rheumatoid arthritis, spondyloarthopathies, gout, osteoarthritis, systemic lupus erythematosus and juvenile arthritis, and inflammatory syndrome for example, from myositis, gingivitis, synovitis, ankylosing spondylitis, burstitis, burns and scar, inflammatory Crohn's disease, Types I diabetes. therefore, it can be used as the therapeutics for treating and preventing inflammatory diseases.Type: ApplicationFiled: July 20, 2010Publication date: November 11, 2010Applicant: Korea Research Institute of Bioscience and BiotechnologyInventors: Yung Hee KHO, Gyoon Hee HAN, Ho Jae LEE, Bum Woo PARK, Hyo Kon CHUN, Hwan Mook KIM, Song Kyu PARK, Sang Bae HAN, Dong Kyu RYU, Tae Gyu CHUN, Jin Ha LEE, Chang Woo LEE, Ki Hoon LEE, Hee Yoon LEE
-
Patent number: 7829571Abstract: The present application describes modulators of MCP-1 of formula (I): or pharmaceutically acceptable salt forms thereof, useful for the treatment of rheumatoid arthritis, multiple sclerosis, atherosclerosis and asthma.Type: GrantFiled: January 15, 2009Date of Patent: November 9, 2010Assignee: Bristol-Myers Squibb CompanyInventors: Percy H. Carter, Robert J. Cherney, Douglas G. Batt, John V. Duncia, Daniel S. Gardner, Soo S. Ko, Anurag S. Srivastava, Michael G. Yang
-
Publication number: 20100279997Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.Type: ApplicationFiled: October 28, 2009Publication date: November 4, 2010Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
-
Publication number: 20100276329Abstract: Individually packaged topical formulations comprising about 0.25 to about 6% w/w of glycopyrrolate for the treatment of hyperhidrosis, wherein said wipe is contained within a pouch resistant to leakage. The formulations may further comprise ethanol, a buffering agent and water. In addition, the formulations may further comprise a polymer system comprising a hydrophobic polymer in combination with a hydrophilic polymer.Type: ApplicationFiled: October 17, 2008Publication date: November 4, 2010Inventors: Michael Johnston, Robert James Houlden
-
Publication number: 20100273739Abstract: The present invention relates to aminotetraline derivatives of the formula (I) or a physiologically tolerated salt thereof. The invention relates to pharmaceutical compositions comprising such aminotetraline derivatives, and the use of such aminotetraline derivatives for therapeutic purposes. The aminotetraline derivatives are GlyT1 inhibitors.Type: ApplicationFiled: February 16, 2010Publication date: October 28, 2010Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
-
Publication number: 20100273724Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.Type: ApplicationFiled: July 7, 2010Publication date: October 28, 2010Applicant: CARDIOME PHARMA CORP.Inventors: Elizabeth L. S. Cheu, Lewis Siu Leung Choi, Doug Ta Hung Chou, Allen W. Davidoff, Alan M. Ezrin, Grace Jung, Bertrand M.C. Plouvier, Aregahegn S. Yifru
-
Patent number: 7820712Abstract: Methods, formulations, dosing regimes, and routes of administration for the treatment or prevention of arrhythmias, including the treatment or prevention of atrial fibrillation. In these methods, the disease or condition is treated or prevented by administering one or more ion channel modulating compounds to a subject, where the ion channel modulating compound or compounds produce specific plasma levels in the subject. The ion channel modulating compounds may be cycloalkylamine ether compounds, particularly cyclohexylamine ether compounds.Type: GrantFiled: November 29, 2007Date of Patent: October 26, 2010Assignee: Cardiome Pharma Corp.Inventors: Gregory N. Beatch, Alan M. Ezrin
-
Publication number: 20100266696Abstract: A process of preparing a particulate and substantially crystalline drug substance. The process involves suspending a substantially crystalline drug substance in an anti-solvent to give a suspension, homogenising the suspension at elevated pressure to give drug particles that have a mean particle size of less than about 10 ?m, and drying the drug particles to remove any residual anti-solvent.Type: ApplicationFiled: December 11, 2008Publication date: October 21, 2010Inventors: Gerhard Muhrer, Thomas Kieckbusch, Ranjit Thakur, Norbert Rasenack, Dilraj Singh, Kurt Schaffluetzel
-
Patent number: 7816396Abstract: The invention relates to a method of treating sialorrhea in a human patient, which comprises orally administering glycopyrrolate in a liquid solution to the human patient under fasted conditions.Type: GrantFiled: December 28, 2009Date of Patent: October 19, 2010Assignee: Shionogi Pharma, Inc.Inventors: Alan Roberts, Balaji Venkataraman
-
Patent number: 7816389Abstract: 14-O—[(((C1-6)Alkoxy-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O—[(((C1-6)Mono- or dialkylamino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Hydroxy-(C1-6)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Formyl-(C0-5)-alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Guanidino-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Ureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Thioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins, 14-O-[((Isothioureido-imino-(C1-6)alkyl)-phenylsulfanyl)-acetyl]-mutilins and their use as pharmaceuticals.Type: GrantFiled: January 11, 2007Date of Patent: October 19, 2010Assignee: Nabriva Therapeutics Forschungs GmbHInventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
-
Patent number: 7816395Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof, or a solvate thereof, or a combination thereof, wherein R1, R2, and X are as defined herein. Compounds of the present invention are useful as progesterone receptor modulators.Type: GrantFiled: August 7, 2007Date of Patent: October 19, 2010Assignee: GlaxoSmithKline LLCInventors: David G. Washburn, Tram H. Hoang
-
Publication number: 20100261761Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Inventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
-
Publication number: 20100261721Abstract: Compounds of a certain formula (I), in which R1, R2, R3, R4, R5, R6 and R7 have the meanings indicated in the description, are novel effective HDAC inhibitors.Type: ApplicationFiled: June 24, 2010Publication date: October 14, 2010Inventors: Thomas MAIER, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
-
Publication number: 20100256072Abstract: The invention provides for methods of treating a mammal who has a BCR/ABL-mediated leukemia, including chronic myelogenous leukemia (CML), particularly the blast crisis stage of CML, Philadelphia-positive acute lymphoblastic leukemia (Ph?-ALL), and refractory leukemias. The invention also provides for compounds for the treatment of these leukemias and methods of identifying anti-leukemic agents.Type: ApplicationFiled: March 24, 2006Publication date: October 7, 2010Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATIONInventors: Danilo Perrotti, Paolo Neviani, Ramasamy Santhanam, John C. Byrd, Guido Marcucci, Natarajan Muthusamy, Ching-Shih Chen
-
Publication number: 20100256216Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 30, 2008Publication date: October 7, 2010Inventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
-
Publication number: 20100247658Abstract: A process for reducing the tendency of a drug substance to aggregate and/or agglomerate during storage. The process involves micronising the drug substance to give a mean particle size of less than about 10 ?m, and exposing the micronised drug substance to a dry environment at an elevated temperature between 40° C. and 120° C. for at least six hours.Type: ApplicationFiled: December 11, 2008Publication date: September 30, 2010Inventors: Gerhard Muhrer, Norbert Rasenack, Michael Juhnke
-
Publication number: 20100249086Abstract: Cannabinoid receptor ligands of formula (I) wherein Ring A and R1 are as defined in the specification. Compositions including such compounds, and methods of treating conditions and disorders using such compounds and compositions are also described.Type: ApplicationFiled: March 26, 2010Publication date: September 30, 2010Applicant: ABBOTT LABORATORIESInventors: Xueqing Wang, Michael J. Dart, Bo Liu
-
Publication number: 20100249101Abstract: The present invention relates to compounds of formula I, The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong anti-thrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardio-vascular disorders like thromboembolic diseases or restenoses. They are inhibitors of the blood clotting enzymes, especially factor VIIa and can in general be applied in conditions in which an undesired activity of factor VIIa is present or for the cure or prevention of which an inhibition of factor VIIa is intended. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them.Type: ApplicationFiled: January 7, 2010Publication date: September 30, 2010Applicant: SANOFI-AVENTISInventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
-
Patent number: 7803794Abstract: The invention provides compounds, pharmaceutical compositions and uses of compounds and salts thereof of general formula (I), for the preparation of a medicament for treatment of an inflammatory disorder, but excluding (S)-3-(r-methylcyclohexyl-carbonylamino)-caprolactam: wherein z is 1, 2, 3 or 4; A is —CO— or —SO2-; Q is linear or branched alkyl, alkenyl, alkynyl, alkoxy, oxyalkyl, aminoalkyl, alkylamino, alkylaminoalkyl, haloalkyl, aryl or substituted aryl; T1 and T2 together constitute a cycloalkyl, cycloalkenyl or polycycloalkyl radical composed of n additional carbon atoms, where n is between 2 and 7; and each hydrogen atom bonded to the carbon atoms in the ring generated by T1 and T2 may be independently be substituted by a group R1, where R1 is independently selected from an alkyl, haloalkyl, alkoxy, haloalkoxy, alkenyl, alkynyl or alkylamino radical of 1 to 20 carbon atoms; or each R1 is independently selected from fluoro, chloro, bromo, iodo, hydroxy, oxyalkyl, amino, aminoalkyl or aminodialkyl radiType: GrantFiled: June 14, 2006Date of Patent: September 28, 2010Assignee: Cambridge Enterprise LimitedInventors: David J. Grainger, David John Fox
-
Patent number: 7803786Abstract: The present invention comprises pharmaceutical compositions comprising a co-crystal of an API and a co-crystal former, and methods of making and using the same.Type: GrantFiled: June 16, 2005Date of Patent: September 28, 2010Assignees: Transform Pharmaceuticals, Inc., University of South FloridaInventors: Jennifer McMahon, Matthew Peterson, Michael J. Zaworotko, Tanise Shattock, Magali Bourghol Hickey
-
Publication number: 20100240728Abstract: The present invention relates to new co-crystals of pyrrolidinones having the formula (I) wherein R1 is a C1-C6 alkyl group. R2 is a C1-C6 alkyl group which is optionally substituted by 1 to 3 halogens or R2 is a C2-C6 alkenyl group.Type: ApplicationFiled: June 6, 2007Publication date: September 23, 2010Applicant: UCB PHARMA, S.A.Inventor: Luc Quere