Chalcogen Bonded Directly To The Five-membered Hetero Ring By Nonionic Bonding Patents (Class 514/424)
  • Publication number: 20110064807
    Abstract: 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: Application
    Filed: November 9, 2010
    Publication date: March 17, 2011
    Applicant: UCB Pharma S.A.
    Inventors: Rajesh Kshirsagar, Mayank Joshi, Yogesh Raichandani
  • Publication number: 20110064808
    Abstract: 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: Application
    Filed: November 12, 2010
    Publication date: March 17, 2011
    Applicant: UCB Pharma S.A.
    Inventors: Rajesh Kshirsagar, Ashwin Rao, Nilesh Malaviya, Kaustubh Jinturkar
  • Publication number: 20110059909
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: March 10, 2011
    Inventors: Inderjit Singh, Avtar Singh
  • Publication number: 20110053914
    Abstract: 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: Application
    Filed: August 27, 2010
    Publication date: March 3, 2011
    Applicant: Gruenenthal GmbH
    Inventors: Klaus SCHIENE, Petra Bloms-Funke
  • Publication number: 20110053904
    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: Application
    Filed: August 19, 2010
    Publication date: March 3, 2011
    Inventors: Sabine Kolczewski, Emmanuel Pinard
  • Publication number: 20110052556
    Abstract: 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: Application
    Filed: February 27, 2009
    Publication date: March 3, 2011
    Applicant: Biolab Sanus Farmaceutical Ltda
    Inventors: José Roberto da Costa Perreira, Marcio Falci, Mauricio Matteis Alario
  • Publication number: 20110046174
    Abstract: 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: Application
    Filed: November 5, 2010
    Publication date: February 24, 2011
    Applicant: Tioga Pharmaceuticals, Inc.
    Inventor: Allen MANGEL
  • Publication number: 20110039853
    Abstract: 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: Application
    Filed: February 19, 2008
    Publication date: February 17, 2011
    Inventor: Soren Ebdrup
  • Publication number: 20110033538
    Abstract: 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: Application
    Filed: October 16, 2007
    Publication date: February 10, 2011
    Applicant: PHARMATHEN S.A.
    Inventors: Evangelos Karavas, Efthimios Koutris, Dimitrios Bikiaris, Vicky Samara, Ioanna Koutri, Eleni Stathaki
  • Publication number: 20110027359
    Abstract: The present invention relates to a pharmaceutical composition comprising levetiracetam as active ingredient, the invention relates specifically to a prolonged release formulation.
    Type: Application
    Filed: March 10, 2010
    Publication date: February 3, 2011
    Applicant: UCB, S.A.
    Inventors: Caroline Goffin, Monique Berwaer, Michaël Boonen, Michel Deleers, Domenico Fanara
  • Publication number: 20110028476
    Abstract: 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: Application
    Filed: September 1, 2010
    Publication date: February 3, 2011
    Inventors: Masahiro Kajino, Atsushi Hasuoka, Naoki Tarui, Terufumi Takagi
  • Publication number: 20110023876
    Abstract: 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: Application
    Filed: May 28, 2010
    Publication date: February 3, 2011
    Applicant: PEARL THERAPEUTICS, INC.
    Inventors: Reinhard Vehring, Michael Steven Hartman, Adrian Edward Smith, Vidya B. Joshi, Sarvajna Kumar Dwivedi
  • Publication number: 20110028510
    Abstract: 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: Application
    Filed: February 18, 2010
    Publication date: February 3, 2011
    Applicants: 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: 20110021508
    Abstract: 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: Application
    Filed: September 16, 2010
    Publication date: January 27, 2011
    Applicant: BLANCHETTE ROCKEFELLER NEUROSCIENCES INSTITUTE
    Inventor: Daniel Alkon
  • Publication number: 20110020445
    Abstract: 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: Application
    Filed: July 19, 2010
    Publication date: January 27, 2011
    Applicant: SANOVEL ILAC SANAYI VE TICARET ANONIM SIRKETI
    Inventors: Hasan Ali Turp, Gulay Yelken, Asiye Sezgia, Ali Turkyilmaz, Levent Oner
  • Publication number: 20110021505
    Abstract: 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: Application
    Filed: March 30, 2010
    Publication date: January 27, 2011
    Applicant: SANOFI-AVENTIS DEUTSCHLAND GMBH
    Inventors: Karl RUDOLPHI, Martin MICHAELIS, Hans GUEHRING
  • Publication number: 20110003792
    Abstract: 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 aminodialky
    Type: Application
    Filed: September 7, 2010
    Publication date: January 6, 2011
    Applicant: CAMBRIDGE ENTERPRISE LIMITED
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7863317
    Abstract: 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: Grant
    Filed: February 15, 2007
    Date of Patent: January 4, 2011
    Assignee: Bristol-Myers Squibb Company
    Inventor: Percy H. Carter
  • Publication number: 20100324025
    Abstract: 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: Application
    Filed: September 21, 2009
    Publication date: December 23, 2010
    Applicant: University of Washington
    Inventors: 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: 20100324009
    Abstract: 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: Application
    Filed: August 24, 2010
    Publication date: December 23, 2010
    Applicant: Gruenenthal GmbH
    Inventors: 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: 20100317644
    Abstract: 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: Application
    Filed: August 24, 2010
    Publication date: December 16, 2010
    Applicant: Gruenenthal GmbH
    Inventors: 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: 20100311711
    Abstract: 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: Application
    Filed: October 10, 2008
    Publication date: December 9, 2010
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Daniele Piomelli, Giorgio Tarzia, Marco Mor, Andrea Duranti, Andrea Tontini
  • Publication number: 20100310652
    Abstract: 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: Application
    Filed: December 22, 2008
    Publication date: December 9, 2010
    Applicant: Alembic Limited
    Inventors: Rajesh Kshirsagar, Ashwin Rao, Atul Kathiriya
  • Publication number: 20100311794
    Abstract: 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: Application
    Filed: June 7, 2010
    Publication date: December 9, 2010
    Applicant: Gilead Sciences, Inc.
    Inventor: Chandrasekar Venkataramani
  • Publication number: 20100310500
    Abstract: 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: Application
    Filed: June 7, 2010
    Publication date: December 9, 2010
    Applicant: Gilead Sciences, Inc.
    Inventors: Michael Graupe, Chandrasekar Venkataramani
  • Patent number: 7842730
    Abstract: 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: Grant
    Filed: February 7, 2005
    Date of Patent: November 30, 2010
    Inventors: Irina Nikolaievna Kuznetsova, Evgeny Ilich Maievsky
  • Patent number: 7842820
    Abstract: Compounds of the formula I in which the substitutents have the definitions provided in the specification, are novel, effective HDAC inhibitors.
    Type: Grant
    Filed: March 10, 2005
    Date of Patent: November 30, 2010
    Assignee: 4SC AG
    Inventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
  • Publication number: 20100292296
    Abstract: 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: Application
    Filed: July 23, 2010
    Publication date: November 18, 2010
    Applicant: Galderma Research & Development
    Inventors: Thibaud BIADATTI, Laurence Dumais, Catherine Soulet, Sandrine Talano, Sebastien Daver
  • Publication number: 20100286204
    Abstract: 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=0
    Type: Application
    Filed: November 19, 2008
    Publication date: November 11, 2010
    Applicant: Sterix Limited
    Inventors: Nigel Vicker, Helen Victoria Bailey, Wesley Heaton, Joanna Mary Day, Atul Purohit, Barry Victor Lloyd Potter
  • Publication number: 20100286207
    Abstract: 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: Application
    Filed: July 20, 2010
    Publication date: November 11, 2010
    Applicant: Korea Research Institute of Bioscience and Biotechnology
    Inventors: 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: 7829571
    Abstract: 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: Grant
    Filed: January 15, 2009
    Date of Patent: November 9, 2010
    Assignee: Bristol-Myers Squibb Company
    Inventors: 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: 20100279997
    Abstract: 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: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100276329
    Abstract: 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: Application
    Filed: October 17, 2008
    Publication date: November 4, 2010
    Inventors: Michael Johnston, Robert James Houlden
  • Publication number: 20100273739
    Abstract: 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: Application
    Filed: February 16, 2010
    Publication date: October 28, 2010
    Inventors: Wilhelm Amberg, Micheal Ochse, Udo Lange, Andreas King, Berthold Behl, Wilfried Hamberger, Maric Mezier, Charles W. Hutchins
  • Publication number: 20100273724
    Abstract: This invention is directed to PEGlyated derivatives, drug conjugates and isotopic derivatives of certain ion channel modulating compounds.
    Type: Application
    Filed: July 7, 2010
    Publication date: October 28, 2010
    Applicant: 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: 7820712
    Abstract: 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: Grant
    Filed: November 29, 2007
    Date of Patent: October 26, 2010
    Assignee: Cardiome Pharma Corp.
    Inventors: Gregory N. Beatch, Alan M. Ezrin
  • Publication number: 20100266696
    Abstract: 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: Application
    Filed: December 11, 2008
    Publication date: October 21, 2010
    Inventors: Gerhard Muhrer, Thomas Kieckbusch, Ranjit Thakur, Norbert Rasenack, Dilraj Singh, Kurt Schaffluetzel
  • Patent number: 7816396
    Abstract: 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: Grant
    Filed: December 28, 2009
    Date of Patent: October 19, 2010
    Assignee: Shionogi Pharma, Inc.
    Inventors: Alan Roberts, Balaji Venkataraman
  • Patent number: 7816389
    Abstract: 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: Grant
    Filed: January 11, 2007
    Date of Patent: October 19, 2010
    Assignee: Nabriva Therapeutics Forschungs GmbH
    Inventors: Klaus Thirring, Gerd Ascher, Susanne Paukner, Werner Heilmayer, Rodger Novak
  • Patent number: 7816395
    Abstract: 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: Grant
    Filed: August 7, 2007
    Date of Patent: October 19, 2010
    Assignee: GlaxoSmithKline LLC
    Inventors: David G. Washburn, Tram H. Hoang
  • Publication number: 20100261761
    Abstract: 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: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Inventors: Thomas Maier, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
  • Publication number: 20100261721
    Abstract: 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: Application
    Filed: June 24, 2010
    Publication date: October 14, 2010
    Inventors: Thomas MAIER, Thomas Beckers, Thomas Baer, Petra Gimmnich, Frank Dullweber, Matthias Vennemann
  • Publication number: 20100256072
    Abstract: 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: Application
    Filed: March 24, 2006
    Publication date: October 7, 2010
    Applicant: THE OHIO STATE UNIVERSITY RESEARCH FOUNDATION
    Inventors: Danilo Perrotti, Paolo Neviani, Ramasamy Santhanam, John C. Byrd, Guido Marcucci, Natarajan Muthusamy, Ching-Shih Chen
  • Publication number: 20100256216
    Abstract: 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: Application
    Filed: May 30, 2008
    Publication date: October 7, 2010
    Inventors: 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: 20100247658
    Abstract: 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: Application
    Filed: December 11, 2008
    Publication date: September 30, 2010
    Inventors: Gerhard Muhrer, Norbert Rasenack, Michael Juhnke
  • Publication number: 20100249086
    Abstract: 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: Application
    Filed: March 26, 2010
    Publication date: September 30, 2010
    Applicant: ABBOTT LABORATORIES
    Inventors: Xueqing Wang, Michael J. Dart, Bo Liu
  • Publication number: 20100249101
    Abstract: 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: Application
    Filed: January 7, 2010
    Publication date: September 30, 2010
    Applicant: SANOFI-AVENTIS
    Inventors: Henning STEINHAGEN, Hauke SZILLAT, Markus FOLLMANN, Reinhard KIRSCH, Volkmar WEHNER, Hans MATTER, Martin LORENZ, Kent W. Neuenschwander, Anthony C. SCOTESE
  • Patent number: 7803794
    Abstract: 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 radi
    Type: Grant
    Filed: June 14, 2006
    Date of Patent: September 28, 2010
    Assignee: Cambridge Enterprise Limited
    Inventors: David J. Grainger, David John Fox
  • Patent number: 7803786
    Abstract: 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: Grant
    Filed: June 16, 2005
    Date of Patent: September 28, 2010
    Assignees: Transform Pharmaceuticals, Inc., University of South Florida
    Inventors: Jennifer McMahon, Matthew Peterson, Michael J. Zaworotko, Tanise Shattock, Magali Bourghol Hickey
  • Publication number: 20100240728
    Abstract: 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: Application
    Filed: June 6, 2007
    Publication date: September 23, 2010
    Applicant: UCB PHARMA, S.A.
    Inventor: Luc Quere