Additional Hydroxy, Bonded Directly To Carbon, Or Ether Oxygen Attached Directly Or Indirectly To The Acyclic Carbon Or Chain By Acyclic Nonionic Bonding With No Amino Nitrogen Between The Additional Hydroxy Or Ether Oxygen And The Aryl Ring Or Ring System (h Of -oh May Be Replaced By A Substituted Or Unsubstitited Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/360)
  • Publication number: 20150087620
    Abstract: The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the DESCRIPTION, which has a superior peripheral blood lymphocyte decreasing action, and is useful for the treatment or prophylaxis of autoimmune diseases; prophylaxis or suppression of resistance or acute rejection or chronic rejection of transplantation of organ or tissue; treatment or prophylaxis of graft-versus-host (GvH) disease due to bone marrow transplantation; or treatment or prophylaxis of allergic diseases.
    Type: Application
    Filed: April 23, 2013
    Publication date: March 26, 2015
    Applicant: MITSUBISHI TANABE PHARMA CORPORATION
    Inventors: Maiko Hamada, Kaoru Tashiro, Hiroshi Sakashita, Masatoshi Kiuchi, Shuzo Takeda, Kunitomo Adachi
  • Publication number: 20150087720
    Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial 3 to 6 days of treatment the daily dosage is raised so that in total the R-fold (R being the accumulation factor) standard daily dosage is administered and thereafter continued at the standard daily dosage or at a daily dosage lower than the standard daily dosage.
    Type: Application
    Filed: October 16, 2014
    Publication date: March 26, 2015
    Applicant: Novartis AG
    Inventors: John M. Kovarik, Silke Appel-Dingemanse
  • Publication number: 20140323501
    Abstract: Immune-modulators of formula (I) below are prepared: A pharmaceutical composition contains the immune-modulators. The pharmaceutical composition is used as a drug, especially as an immune-modulating drug. The compound can be used in treatment of immune disorders and for immune suppression. Thus, for example, the compound can be used in treating hypo-immunity, rejection after organ transplantation and auto-immune disease.
    Type: Application
    Filed: July 5, 2012
    Publication date: October 30, 2014
    Applicant: INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF MEDICAL SCIENCES
    Inventors: Weijuan Han, Haijing Zhang, Xiaojian Wang, Jing Jin, Gang Li, Yi Zhang, Qiong Xiao, Wanqi Zhou, Xiaoguang Chen, Dali Yin
  • Patent number: 8853452
    Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: October 7, 2014
    Assignee: The Administrators of the Tulane Educational Fund
    Inventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
  • Publication number: 20140271541
    Abstract: Disclosed are pharmaceutical combinations comprising at least one S1P receptor agonist, as well as a method for treating demyelinating diseases, e.g. multiple sclerosis or disorders associated therewith or Guillain-Barré syndrome, comprising co-administration, e.g. concomitantly or in sequence, of a therapeutically effective amount of a) an S1P receptor agonist, and b) at least one co-agent shown to have clinical activity against at least one symptom of a demyelinating disease.
    Type: Application
    Filed: March 18, 2014
    Publication date: September 18, 2014
    Applicant: NOVARTIS AG
    Inventors: Carolyn Ann Foster, Peter C. Hiestand, Paul William Glue
  • Publication number: 20140248236
    Abstract: The disclosure provides methods of use of certain compounds that are useful for treating certain symptoms of endocrine disturbances, and in particular those associated with hot flashes.
    Type: Application
    Filed: November 7, 2012
    Publication date: September 4, 2014
    Inventors: Michael G. Natchus, Richard Arrendale
  • Publication number: 20140235895
    Abstract: The present application provide processes for the preparation of fingolimod and its pharmaceutically acceptable salts, process for the purification of fingolimod hydrochloride and process for the preparation of amorphous fingolimod hydrochloride.
    Type: Application
    Filed: April 27, 2012
    Publication date: August 21, 2014
    Applicant: DR. REDDY'S LABORATORIES LTD.
    Inventors: Srinivas Katkam, Rajeswar Reddy Sagyam, Raghavendar Rao Morthala, Babu Ireni, Krishna Vinigari, Suresh Kumar Ramdoss, Srinivasulu Rangineni, Arjunkumar Tummala, Javed Iqbal, Srinivas Oruganti, Bhaskar Kandagatla
  • Publication number: 20140227358
    Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.
    Type: Application
    Filed: April 17, 2014
    Publication date: August 14, 2014
    Applicant: NOVARTIS AG
    Inventors: Michael AMBUHL, Jutta BEYER, Begona CARRENO-GOMEZ, Colleen RUEGGER, Stephen VALAZZA
  • Publication number: 20140066657
    Abstract: S1P receptor modulators or agonists are administered following a dosage regimen whereby during the initial days of treatment the daily dosage is lower than the standard daily dosage
    Type: Application
    Filed: September 6, 2013
    Publication date: March 6, 2014
    Applicant: Novartis AG
    Inventors: Robert Schmouder, Thomas Dumortier, Olivier David, Michael Looby
  • Publication number: 20140051766
    Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.
    Type: Application
    Filed: August 12, 2013
    Publication date: February 20, 2014
    Applicant: Novartis AG
    Inventors: Guido Jordine, Michael Mutz
  • Publication number: 20140039216
    Abstract: The present invention relates to an improved process for the preparation of Fesoterodine and pharmaceutically acceptable salts thereof. The present invention particularly relates to a process for the preparation of fesoterodine and pharmaceutically acceptable salts thereof which involves use and preparation of R(+)benzyl tolterodine and fumarate salt of R(+)-[4-benzyloxy-3-(3-diisopropylamino-1-phenylpropyl)-phenyl]-methanol.
    Type: Application
    Filed: November 11, 2011
    Publication date: February 6, 2014
    Applicant: ALEMBIC PHARMACEUTICALS LIMITED
    Inventors: Jayaraman Venkat Raman, Samir Patel, Indrajit Thakor, Mahesh Ladani, Chetan Patil, Ronak Patel, Prashant Raval, Viral Parekh, Hiral Shah
  • Publication number: 20130303490
    Abstract: The invention relates to compounds which are agonists of at least one receptor selected from S1PR1, S1PR2, S1PR3, S1PR4 and S1PR5 receptors, for use in methods for treating HIV infections in humans or animals.
    Type: Application
    Filed: December 12, 2011
    Publication date: November 14, 2013
    Applicant: Centre National De La Recherche Scientifique-CNRS
    Inventors: Vincent Francois, Pierre Corbeau, Charline Duquenne
  • Publication number: 20130289127
    Abstract: Disclosed are compounds of formula I wherein R1, R2, R5 and R6 are as defined in the claims; such compounds have interesting pharmacological properties.
    Type: Application
    Filed: June 13, 2013
    Publication date: October 31, 2013
    Inventors: Ernst Küsters, Lukas Oberer, Gottfried Sedelmeier
  • Patent number: 8569371
    Abstract: Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical composition thereof.
    Type: Grant
    Filed: March 29, 2011
    Date of Patent: October 29, 2013
    Assignee: Pliva Hrvatska D.O.O.
    Inventors: Marina Ratkaj, Gustavo Frenkel
  • Publication number: 20130281739
    Abstract: The present invention provides crystalline polymorphic forms of Fingolimod HCl (I) and processes for preparation thereof. The application provides processes for preparation of crystalline polymorphic forms-?, ? and ? substantially free from process related impurities. The crystalline polymorphic forms of Fingolimod HCl (I) obtained by the processes according to the present invention having an XRDP pattern as per FIGS. 1, 3 and 5, which are useful as active pharmaceutical ingredient in pharmaceutical compositions for the treatment or prevention of autoimmune related disorder including multiple sclerosis.
    Type: Application
    Filed: August 29, 2011
    Publication date: October 24, 2013
    Inventors: Vimal Kumar Shrawat, Veereshappa N/A, Vinod Kumar Singh, Prashant Purohit
  • Publication number: 20130245321
    Abstract: Provided are novel compositions and analogs which are useful in a number of applications, indications and diseases, as well as for monitoring pharmakinetics and patient management. These compounds and analogs are applicable to treating tumors of the central nervous system, e.g., glioblastoma (GBM).
    Type: Application
    Filed: October 11, 2012
    Publication date: September 19, 2013
    Inventors: SARAH SPIEGEL, ROBERT ELLIOT ZIPKIN, JEFFREY KROLL ADAMS
  • Patent number: 8530522
    Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.
    Type: Grant
    Filed: November 10, 2009
    Date of Patent: September 10, 2013
    Assignee: Novartis AG
    Inventors: Guido Jordine, Michael Mutz
  • Publication number: 20130230489
    Abstract: The present invention relates to pharmaceutical compositions comprising a 2-amino-2-[2-(4-C2-20-alkyl-phenypethyl]propane-1,3-diol compound or a pharmaceutically acceptable salt thereof, and to the use thereof for treating, preventing or delaying the progression of multiple sclerosis in a paediatric patient or a patient suffering from a specific condition.
    Type: Application
    Filed: March 18, 2013
    Publication date: September 5, 2013
    Inventors: John M. Kovarik, Robert Schmouder, Marie-Claude Bastien, David Olivier, Goeril Karlsson
  • Publication number: 20120288559
    Abstract: The present invention provides various pharmaceutical compositions comprising an S1P receptor modulator, e.g. an S1P receptor agonist. In one aspect, there is provided a pharmaceutical composition having a coating. In other aspects, rapid disintegrating compositions are provided. In a further aspect, a pharmaceutical composition which is free of sugar alcohols is provided. In another aspect, the invention provides a pharmaceutical composition comprising a coating comprising an S1P receptor modulator.
    Type: Application
    Filed: July 19, 2012
    Publication date: November 15, 2012
    Inventors: Michael Ambühl, Jutta Beyer, Begona Carreno-Gomez, Colleen Ruegger, Stephen Valazza
  • Publication number: 20120264719
    Abstract: S1P receptor modulators are administered following a dosage regimen providing a positive benefit-risk profile.
    Type: Application
    Filed: September 20, 2010
    Publication date: October 18, 2012
    Inventors: Craig Boulton, Pascale Burtin, Olivier David, Ana de Vera, Thomas Dumortier, Irene Hunt, Robert Schmouder
  • Publication number: 20120244071
    Abstract: There are provided new iodo- and bromo-compounds, and their use as diagnostic agents and imaging agents for diseases and disorders wherein S1P receptor expression is altered.
    Type: Application
    Filed: December 8, 2010
    Publication date: September 27, 2012
    Applicant: Novartis AG
    Inventors: Yves Auberson, Emmanuelle Briard, David Orain
  • Publication number: 20120141513
    Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.
    Type: Application
    Filed: December 5, 2011
    Publication date: June 7, 2012
    Inventors: Julie F. Liu, Rose A. Persichetti
  • Patent number: 8063250
    Abstract: Provided are crystalline forms of O-desmethylvenlafaxine fumarate, methods for their preparation, and pharmaceutical compositions thereof.
    Type: Grant
    Filed: November 26, 2008
    Date of Patent: November 22, 2011
    Assignee: Teva Pharmaceutical Industries, Ltd.
    Inventors: Valerie Niddam-Hildesheim, Eli Lancry, Sharona Shachan-tov, Sigalit Levi, Tamar Nidam
  • Publication number: 20110229501
    Abstract: The present invention relates to crystalline forms and hydrates of 2-Amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diol, and to the use thereof, in particular in the treatment or prevention of various autoimmune conditions.
    Type: Application
    Filed: November 10, 2009
    Publication date: September 22, 2011
    Applicant: NOVARTIS AG
    Inventors: Guido Jordine, Michael Mutz
  • Publication number: 20110118357
    Abstract: The present invention provides a convenient and efficient process for the preparation of O-desmethylvenlafaxine (ODV), comprising the reaction of venlafaxine, or a salt thereof, with a thiol reagent such as a dithiol, an aminothiol or an inorganic thiol. The present invention also provides a process for purifying ODV base, said process comprising the steps of mixing crude ODV base with an alcohol to form a suspension and adding acid followed by base to generate ODV base with high purity.
    Type: Application
    Filed: October 18, 2008
    Publication date: May 19, 2011
    Inventors: Vinayak Govind Gore, Vikas Sharad Kulkarni, Madhukar Shaligram Patil
  • Publication number: 20110077396
    Abstract: In one aspect, the present invention provides a protected ligand precursor having structure XX wherein R8 is independently at each occurrence a protected hydroxy group, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, and b is 0-4; R9-R11 are independently at each occurrence hydrogen, a protected C1-C3 hydroxyalkyl group, or a C1-C3 alkyl group, with the proviso that at least one of R8-R11 is a protected hydroxy group or a protected C1-C3 hydroxyalkyl group; and R12 and R13 are independently at each occurrence a protecting group is selected from the group consisting of C1-C30 aliphatic radicals, C3-C30 cycloaliphatic radicals, and C2-C30 aromatic radicals.
    Type: Application
    Filed: May 21, 2010
    Publication date: March 31, 2011
    Applicant: General Electric Company
    Inventors: Brian James Grimmond, Michael James Rishel, Michael Todd Luttrell
  • Publication number: 20110015425
    Abstract: The present invention relates to improved processes for the production of 2-amino-2-[2-(4-C2-20-alkyl-phenyl)ethyl]propane-1,3-diols, and to compounds for use therein.
    Type: Application
    Filed: March 17, 2009
    Publication date: January 20, 2011
    Inventor: Gottfried Sedelmeier
  • Publication number: 20110009648
    Abstract: This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.
    Type: Application
    Filed: January 22, 2007
    Publication date: January 13, 2011
    Applicant: Sandoz AG
    Inventors: Martin Albert, Hubert Sturm, Andreas Berger, Peter Kremminger
  • Publication number: 20100311841
    Abstract: Therapeutic compounds based on synthetic sphingolipid analogs are provided, particularly alkylthiophenyl substituted ceramide analogs, suitable for treating degenerative, infectious, and other diseases.
    Type: Application
    Filed: November 6, 2008
    Publication date: December 9, 2010
    Inventors: Arie Dagan, Shimon Gatt, Shimon Slavin
  • Patent number: 7820694
    Abstract: Compounds of formula in free or salt or solvate form, where Ar is a group of formula Y is carbon or nitrogen and R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, X, n, p, q and r are as defined in the specification, their preparation and their use as pharmaceuticals, particularly for the treatment of obstructive or inflammatory airways diseases.
    Type: Grant
    Filed: October 13, 2009
    Date of Patent: October 26, 2010
    Assignee: Novartis AG
    Inventors: Bernard Cuenoud, Ian Bruce, Robin A Fairhurst, David Beattie
  • Patent number: 7807854
    Abstract: To provide a medicament which efficiently expresses an immunosuppressive agent or an anti-inflammatory agent and reduces expression of side effect. A medicament includes diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure having an activity of reducing lymphocytes circulating peripherally, in combination with an immunosuppressive agent and/or an anti-inflammatory agent.
    Type: Grant
    Filed: December 31, 2009
    Date of Patent: October 5, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Shinji Kudou, Kazuhiko Kuriyama, Tokutarou Yasue
  • Patent number: 7781617
    Abstract: A medicine which effectively functions as an immunosuppressant or anti-inflammatory agent and is effective in diminishing the occurrence of side effects. The medicine comprises a combination of: a diaryl sulfide or diaryl ether compound having a 2-amino-1,3-propanediol structure and having the function of diminishing lymphocytes circulating through the periphery; and an immunosuppressant and/or an anti-inflammatory agent.
    Type: Grant
    Filed: July 15, 2005
    Date of Patent: August 24, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd
    Inventors: Shinji Kudou, Kazuhiko Kuriyama, Tokutarou Yasue
  • Publication number: 20100191015
    Abstract: The present invention relates to process for the preparation of novel crystalline Desmethylvenlafaxine succinate polymorphic Forms-A, B. The present invention also relates to novel processes for the preparation of 0-Desmethylvenlafaxine succinate polymorphic Forms-(I), (II), (III) and amorphous.
    Type: Application
    Filed: July 15, 2008
    Publication date: July 29, 2010
    Applicant: MATRIX LABORATORIES LIMITED
    Inventors: Ramakoteswara Rao Jetti, Purandhar Koilkonda, Jagan Mohana Chary Tummanapally, Mohana Vamsi, Krishna Vadlamudi, Prasanth Kumar Barik, Om Dutt Tyagi
  • Patent number: 7763752
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects: .
    Type: Grant
    Filed: November 21, 2008
    Date of Patent: July 27, 2010
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Publication number: 20100130736
    Abstract: Drug discovery is a complex undertaking facing many challenges, not the least of which is a high attrition rate as many promising candidates prove ineffective or toxic in the clinic owing to a poor understanding of the diseases, and thus the biological systems, they target. Therefore, it is broadly agreed that to increase the productivity of drug discovery one needs a far deeper understanding of the molecular mechanisms of diseases, taking into account the full biological context of the drug target and moving beyond individual genes and proteins. The present methods rely on the use of label-free cellular assays, particularly the DMR index, to systematically display the mode of actions, the toxicity, and the target(s) and pathway(s) of any molecules.
    Type: Application
    Filed: November 23, 2009
    Publication date: May 27, 2010
    Inventors: Ye Fang, Ann M. Ferrie, Joydeep Lahiri, Elizabeth Tran
  • Publication number: 20100076086
    Abstract: The present invention relates to a novel process for the preparation of O-desmethyl venlafaxine (ODV).
    Type: Application
    Filed: January 31, 2008
    Publication date: March 25, 2010
    Applicant: Merck Development Centre Private Limited Plot 1 A/2
    Inventor: Vinayak G. Gore
  • Publication number: 20100068786
    Abstract: A method for inhibiting therapeutic drug resistance within a cell over-expressing a membrane protein is provided. The method comprises synthesizing a dimeric prodrug inhibitor of a monomeric therapeutic agent; administering the dimeric prodrug inhibitor to the membrane protein together with the monomeric therapeutic agent; and occupying at least one substrate binding site of the membrane protein with the synthesized dimeric prodrug to allow the monomeric therapeutic agent to accumulate within the cell. The dimeric prodrug inhibitor contains a crosslinking agent that is adapted to breakdown under reducing conditions within the cytosol of the cell to cause the dimeric prodrug to revert back to a form equivalent to the monomeric therapeutic agent.
    Type: Application
    Filed: September 16, 2009
    Publication date: March 18, 2010
    Inventors: Jean A. Chmielewski, Christine A. Hrycyna, Marcos M. Pires
  • Publication number: 20100063160
    Abstract: The present invention relates to crystalline forms of O-desmethyl venlafaxine (ODV) succinate monohydrate, namely Forms I and II, in pure form and to novel processes for their preparation. The present invention provides a process for the preparation of Form II free of Form I and a process for the preparation of Form I free of Form II. The present invention provides direct methods for the preparation of ODV succinate Form II from ODV free base and for the preparation of ODV succinate Form I from ODV free base.
    Type: Application
    Filed: October 18, 2007
    Publication date: March 11, 2010
    Applicant: Merck Development Centre Private Limited
    Inventors: Vinayak G. Gore, Vikas S. Kulkarni, V.S. Wakchaure, M.G. Hublikar, S.R. Wavhal
  • Publication number: 20090326075
    Abstract: This invention provides pharmaceutically active enantiomers of the venlafaxine metabolite O-Desmethyl venlafaxine, R(?)-4-[2-(Dimethylamino-1-(1-hydroxycyclo-hexyl)ethyl]phenol or R(?)1-[2-(dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclo-hexanol, and S(+)-1-[2-(Dimethylamino)-1-(4-hydroxyphenyl)ethyl]cyclohexanol or S(+)-4-[2-(Dimethylamino)-1-(1-hydroxycyclohexyl)ethyl]phenol, or one or more pharmaceutically acceptable salts or salt hydrates thereof, as well as pharmaceutical compositions utilizing these enantiomers and methods of using the enantiomers to treat, inhibit or control central nervous system disorders.
    Type: Application
    Filed: September 4, 2009
    Publication date: December 31, 2009
    Applicant: Wyeth
    Inventors: John P. Yardley, Andrew A. Asselin
  • Publication number: 20090247472
    Abstract: This invention relates to compounds with the formula (I) given below or one of their pharmaceutically acceptable salts, as a medicine; Formula (I) of pharmaceutical compositions comprising one or more compounds with Formula (I) as active constituent, use of compounds with Formula (I) for the preparation of compositions designed to prevent or treat at least one illness involving an abnormal cellular proliferation, pro-apoptotic compositions and/or anti-proliferative compositions comprising at least one compound with Formula (I)/and the use of compounds with formula (I) as pro-apoptotic and/or anti-proliferative agents.
    Type: Application
    Filed: April 25, 2007
    Publication date: October 1, 2009
    Applicants: FLUOFARMA, UNIVERSITE BORDEAUX 1, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Gaelle Depierre, Jean Dessolin, Michel Laguerre, Claude Commandeur
  • Publication number: 20090240082
    Abstract: A process for preparing venlafaxine in a high yield as well as processes for producing venlafaxine hydrochloride of form I having a very hight polymorphic purity are described.
    Type: Application
    Filed: June 4, 2009
    Publication date: September 24, 2009
    Inventor: Silvo Zupancic
  • Publication number: 20090202572
    Abstract: The instant invention relates to compositions and methods for treating or preventing bone diseases. In certain aspects, the invention provides compositions comprising a ?-adrenergic antagonist or agonist associated to a bone-targeted molecule, as well as methods of modulating bone mass and/or growth in a mammal by administering a composition of the present invention. In other aspects, the invention provides methods of modulating bone mass and/or growth in a mammal by administering a composition comprising a ?2-selective antagonist or agonist.
    Type: Application
    Filed: May 13, 2006
    Publication date: August 13, 2009
    Inventors: Gerard Karsenty, Bruce Devens
  • Publication number: 20090176744
    Abstract: This invention relates to novel compounds that are deuterated derivatives of fingolimod and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising one or more compounds of this invention and a carrier and the use of the disclosed compounds and compositions in methods of treating diseases and conditions that are beneficially treated by administering a lysophospholipid edg1 (S1P1) receptor agonist, such as fingolimod.
    Type: Application
    Filed: October 31, 2008
    Publication date: July 9, 2009
    Applicant: CoNCERT Pharmaceuticals, Inc.
    Inventors: Julie F. Liu, Rose A. Persichetti
  • Publication number: 20090137846
    Abstract: The present invention describes processes for the preparation of O-desmethylvenlafaxine and tridesmethylvenlafaxine, which may be used as an intermediate in preparing O-desmethylvenlafaxine.
    Type: Application
    Filed: October 20, 2008
    Publication date: May 28, 2009
    Inventors: Valerie Niddam-Hildesheim, Tamar Nidam, Ben-Zion Dolitzky, Gustavo Frenkel
  • Publication number: 20090137530
    Abstract: A novel amine compound represented by the following formula (I), which is superior in immunosuppressive action, rejection suppressive action and the like, and shows reduced side effects such as bradycardia and the like, or a pharmaceutically acceptable acid addition salt thereof, or hydrates thereof, or solvate, as well as a pharmaceutical composition containing this compound and a pharmaceutically acceptable carrier. wherein R is a hydrogen atom or P(?O)(OH)2, X is an oxygen atom or a sulfur atom, Y is CH2CH2 or CH?CH, R1 is cyano or alkyl having a carbon number of 1 to 4 and substituted by a halogen atom(s), R2 is alkyl having a carbon number of 1 to 4 and optionally substituted by a hydroxyl group(s) or a halogen atom(s), R3 and R4 may be the same or different and each is a hydrogen atom or alkyl having a carbon number of 1 to 4, and n is 5-8.
    Type: Application
    Filed: December 15, 2006
    Publication date: May 28, 2009
    Applicant: Mitsubishi Tanabe Pharma Corporation
    Inventors: Masatoshi Kiuchi, Kaoru Marukawa, Nobutaka Kobayashi, Kunio Sugahara
  • Patent number: 7524887
    Abstract: The present invention relates to a method for the prophylaxis or treatment of pain using compounds of formula I, in which R, R2, R3, R4 and R5 have the meanings indicated in the specification.
    Type: Grant
    Filed: May 25, 2004
    Date of Patent: April 28, 2009
    Assignee: Sanofi-Aventis Deutschland GmbH
    Inventors: Martin Michaelis, Gerd Geisslinger, Klaus Scholich
  • Patent number: 7482491
    Abstract: An amino alcohol derivative represented by the following general formula (1) (for example, (±)-2-amino-5-[4-(3-benzyloxyphenylthio)-2-chlorophenyl]-2-methylpentane-1-ol) exhibits strong immunosuppressive effect while causing less side effects:
    Type: Grant
    Filed: September 16, 2003
    Date of Patent: January 27, 2009
    Assignee: Kyorin Pharmaceutical Co., Ltd.
    Inventors: Yasushi Kohno, Kiyoaki Tanaka, Kazuhiko Kuriyama
  • Patent number: 7452995
    Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: April 7, 2005
    Date of Patent: November 18, 2008
    Assignee: Theravance, Inc.
    Inventors: Edmund J. Moran, John R. Jacobsen, James Aggen
  • Publication number: 20080234281
    Abstract: The present invention relates to N-substituted benzylic aniline derivatives that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also relates to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.
    Type: Application
    Filed: March 18, 2005
    Publication date: September 25, 2008
    Inventors: Robert M. Garbaccio, Christy M. Olson, Edward S. Tasber, Maricel Torrent
  • Patent number: 7402673
    Abstract: The invention provides novel ?2 adrenergic receptor agonist compounds. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with ?2 adrenergic receptor activity, and processes and intermediates useful for preparing such compounds.
    Type: Grant
    Filed: June 2, 2005
    Date of Patent: July 22, 2008
    Assignee: Theravance, Inc.
    Inventor: Martin S. Linsell