Chalcogen Attached Indirectly To The Five-membered Hetero Ring By Acyclic Nonionic Bonding Patents (Class 548/570)
  • Patent number: 9671415
    Abstract: The current invention provides an improved immunoassay for the detection and determination of pyrrolidinophenone based designer drugs in hair and biological fluids (urine, blood, and oral fluid). The generic immunoassay is underpinned by novel, sub-family-specific antibodies, which display surprising sensitivity. The invention further describes substrates comprising an antibody that is specific to compounds of the pyrrolidinophenone family. Also described are the novel immunogens from which the antibodies are derived and kits incorporating the antibodies of the current invention.
    Type: Grant
    Filed: October 2, 2015
    Date of Patent: June 6, 2017
    Assignee: Randox Laboratories Limited
    Inventors: Ivan McConnell, Peter Fitzgerald, Philip Lowry, Elouard Benchikh
  • Patent number: 9096565
    Abstract: This invention relates to compounds for the inhibition of histone deacetylase. More particularly, the invention provides for compounds of the Formula (I) and N-oxides, hydrates, solvates, pharmaceutically acceptable salts, prodrugs and complexes thereof, and racemic and scalemic mixtures, diastereomers and enantiomers thereof, wherein groups L, M, X and Y are as defined herein.
    Type: Grant
    Filed: April 9, 2008
    Date of Patent: August 4, 2015
    Assignee: MethylGene Inc.
    Inventors: Pierre Tessier, Silvana Leit, David Smil, Robert Deziel, Alain Ajamian, Yves Andre Chantigny, Celia Dominguez
  • Publication number: 20150126577
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: January 12, 2015
    Publication date: May 7, 2015
    Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
    Inventors: Eric Stangeland, Daisuke Roland Saito, Priscilla Van Dyke, Lori Jean Patterson
  • Publication number: 20150099720
    Abstract: Provided herein are compounds having a structure selected from among Formula (I), Formula (II), Formula (III), Formula (IV), Formula (V) and Formula (VI) that are androgen receptor modulators and/or androgen receptor binding agents. Also disclosed are methods of making and using such compounds, including, but not limited to, using such compounds for treating various conditions.
    Type: Application
    Filed: October 20, 2014
    Publication date: April 9, 2015
    Inventors: Lin Zhi, Robert I. Higuchi, E. Adam Kallel, Cornelis Arjan Van Oeveren, Jyun-Hung Chen, Daniel A. Ruppar, Bijan Pedram, Thomas Lot Stevens Lau, Todd A. Miller
  • Patent number: 9000191
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: November 26, 2013
    Date of Patent: April 7, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20150087832
    Abstract: The present invention is directed to processes for preparing beta 3 agonists of Formula (I) and Formula (II) and their intermediates. The beta 3 agonists are useful in the treatment of certain disorders, including overactive bladder, urinary incontinence, and urinary urgency.
    Type: Application
    Filed: October 22, 2012
    Publication date: March 26, 2015
    Applicant: MERCK SHARP & DOHME, CORP.
    Inventors: John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R. Scott Hoerrner, Stephen Keen, Dave Liebermann, Zhuqing Liu, Joseph Lynch, Kevine M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
  • Publication number: 20150080369
    Abstract: The present invention is directed to novel retinoid-related orphan receptor gamma (ROR?) modulators, processes for their preparation, pharmaceutical compositions containing these modulators, and their use in the treatment of inflammatory, metabolic and autoimmune diseases mediated by ROR?.
    Type: Application
    Filed: April 25, 2013
    Publication date: March 19, 2015
    Inventors: Veronique Birault, Amanda Jennifer Campbell, Stephen Harrison, Joelle Le, Lena Shukla
  • Patent number: 8969403
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Grant
    Filed: January 7, 2014
    Date of Patent: March 3, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Patent number: 8933249
    Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: June 27, 2012
    Date of Patent: January 13, 2015
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20140309275
    Abstract: The disclosure relates to compounds, pharmaceutical compositions, and methods of treating or preventing disease. In certain embodiments, the disclosure relates to methods of treating an infection or cancer comprising administering a pharmaceutical composition disclosed herein to a subject in need thereof. In a typical embodiment, one administers a pharmaceutical composition comprising sphingosine or a sphingosine analog to a subject at risk for, exhibiting symptoms of or diagnosed with a malaria infection.
    Type: Application
    Filed: September 27, 2012
    Publication date: October 16, 2014
    Inventors: Dennis C. Liotta, Jason Holt, JR., Michael G. Natchus, Mark T. Baillie, Eric J. Miller, Mary R. Galinski
  • Patent number: 8853423
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: June 15, 2011
    Date of Patent: October 7, 2014
    Assignee: Seragon Pharmaceuticals, Inc.
    Inventors: Steven P. Govek, Nicholas D. Smith
  • Patent number: 8853255
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: April 25, 2013
    Date of Patent: October 7, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Eric L. Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam D. Hughes, Lori Jean Patterson
  • Publication number: 20140243536
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: November 26, 2013
    Publication date: August 28, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20140242645
    Abstract: The present invention is directed to a process for preparing a compound of formula I-11 through multiple-step reactions.
    Type: Application
    Filed: October 22, 2012
    Publication date: August 28, 2014
    Inventors: John Y.L. Chung, Kevin Campos, Edward Cleator, Robert F. Dunn, Andrew Gibson, R Scott Hoerrner, Stephen Keen, Dave Lieberman, Zhuqing Liu, Joseph Lynch, Kevin M. Maloney, Feng Xu, Nobuyoshi Yasuda, Naoki Yoshikawa, Yong-Li Zhong
  • Patent number: 8802856
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 22, 2013
    Date of Patent: August 12, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Patent number: 8791151
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: December 19, 2012
    Date of Patent: July 29, 2014
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventor: Daisuke Roland Saito
  • Patent number: 8791076
    Abstract: The invention relates to compounds of Formula I: and pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, and R3 are defined as set forth in the specification. The compounds are agonists of neurotrophin (such as nerve growth factor) receptors.
    Type: Grant
    Filed: August 31, 2011
    Date of Patent: July 29, 2014
    Inventors: Pablo Villoslada, Angel Messeguer
  • Patent number: 8747690
    Abstract: A quaternary ammonium salt of the formula (1), a composition containing the quaternary ammonium salt and an organic solvent, and an electrochemical device using the salt wherein R1 and R2 are both methyl and X? is BF4? or N(CF3SO2)2?.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: June 10, 2014
    Assignees: Otsuka Chemical Co., Ltd., Stella Chemifa Corporation
    Inventors: Tetsuo Nishida, Yasutaka Tashiro, Megumi Tornisaki, Masashi Yamamoto, Kazutaka Hirano, Akihiro Nabeshima, Hiroaki Tokuda, Kenji Sato, Takashi Higono
  • Patent number: 8729119
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: May 20, 2014
    Assignee: Theravance, Inc.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Publication number: 20140121385
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Application
    Filed: January 7, 2014
    Publication date: May 1, 2014
    Applicant: THERAVANCE, INC.
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Patent number: 8658691
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Grant
    Filed: September 28, 2012
    Date of Patent: February 25, 2014
    Assignee: Theravance, Inc.
    Inventors: Pierre-Jean Colson, Timothy Fass, Venkat R. Thalladi
  • Publication number: 20140005222
    Abstract: The present invention provides a compound of the Formula II: wherein A is: R1 is CH3, CF3, or F; R2 is H, CH3, or F; R3 is CH3, OCH3, OH, F; R4 is OH or CH2OH; and X is CH or N; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 20, 2013
    Publication date: January 2, 2014
    Inventors: Maria-Jesus BLANCO-PILLADO, Matthew Joseph FISHER, Steven Lee KUKLISH, Tatiana Natali VETMAN
  • Patent number: 8604038
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: December 10, 2013
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gergori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Patent number: 8604245
    Abstract: The present invention relates to a novel class of tri-aryl compounds, compositions comprising the same and processes for the preparation thereof.
    Type: Grant
    Filed: June 3, 2008
    Date of Patent: December 10, 2013
    Assignee: Ben-Gurion University of the Negev Research and Development Authority
    Inventors: Esther Priel, Aviv Gazit, Shimon Slavin, Sara Yitzchak
  • Patent number: 8597706
    Abstract: The present invention relates to a method for synthetizing a compound of the following formula (I): wherein R is a methyl or ethyl group, n is 1 or 2, and X is a CH2 or CD2 group, from a compound of the following formula (II): wherein R and n are as defined above, and also relates to a method for assaying the compounds of the formula (I) using a corresponding deuterated derivative as an internal reference, as well as to the use of ketal derivatives of compounds of the formula (I) as a stable precursor, in particular in a flavoring composition.
    Type: Grant
    Filed: June 24, 2010
    Date of Patent: December 3, 2013
    Assignees: Centre National de la Recherche Scientifique (CNRS), Universite Montpellier 2 Sciences et Techniques
    Inventors: Alain Morere, Chantal Menut, Yusuf Ziya Gunata, Abdelhamid Agrebi
  • Patent number: 8592453
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: November 26, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Patent number: 8552051
    Abstract: The use of mesembrenone and medicaments and dietary supplements containing mesembrenone. The applicant has surprisingly found that mesembrenone exhibits potent PDE-4 inhibition properties and, in addition to being useful in treating conditions that respond to treatment with a PDE-4 inhibitor, has dual activity on account of its serotonin-uptake inhibition properties. Mesembrenone is extracted and isolated, for example as a pure compound, from plant material of the plant family Mesembryanthemaceae. Preferably a plant or plants from the genus Sceletium, more preferably, Sceletium tortuosum(L) N.E.Br is used.
    Type: Grant
    Filed: March 16, 2010
    Date of Patent: October 8, 2013
    Assignee: H. L. Hall & Sons Limited
    Inventors: Alan Harvey, Nigel Gericke, Alvaro Viljoen
  • Patent number: 8507537
    Abstract: The present invention relates to novel trifluoromethoxyphenyl-substituted tetramic acid derivatives of the formula (I), in which J, X, Y, A, B, D and G have the meanings given above, to a number of processes for their preparation, and to their use as pesticides and/or herbicides. The invention further provides selective herbicidal compositions which comprise, firstly, trifluoromethoxyphenyl-substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention further relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the additions of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: October 13, 2007
    Date of Patent: August 13, 2013
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Christian Arnold, Thomas Auler, Jan Dittgen, Dieter Feucht, Eva-Maria Franken, Waltraud Hempel, Martin Jeffrey Hills, Heinz Kehne, Peter Losel, Olga Malsam, Christopher Hugh Rosinger, Erich Sanwald, Ulrich Gorgens, Stefan Antons, Wolfgang Ebenbeck, Axel Pleschke, Marielouise Schneider, Ralf Wischnat
  • Publication number: 20130203815
    Abstract: The present invention provides compounds represented by general formula (I): wherein, R1, R2, R3, L and T are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, and prodrugs thereof. The invention also relates to processes for the manufacture of compounds of formula (I) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful in the treatment of a condition or disorder mediated by one or more cytokines selected from Tumor Necrosis Factor-alpha (TNF-?) and interleukins such as IL-1, IL-6, and IL-8. The present invention further provides a method of treatment of inflammatory disorders by administering a therapeutically effective amount of the said compound of formula (I) or its pharmaceutical composition, to a mammal in need thereof.
    Type: Application
    Filed: March 25, 2011
    Publication date: August 8, 2013
    Applicant: PIRAMAL ENTERPRISES LIMITED
    Inventors: Babasaheb Pandurang Bandgar, Jalindar Vasant Totre
  • Publication number: 20130178509
    Abstract: In one aspect, the invention relates to compounds of formula I: where a and R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: June 27, 2012
    Publication date: July 11, 2013
    Applicant: THERAVANCE, INC.
    Inventors: Eric Stangeland, Priscilla Van Dyke, Timothy J. Church, Lori Jean Patterson, Daisuke Roland Saito
  • Patent number: 8476336
    Abstract: The invention relates to an ophthalmologic composition including a dye of the general formula I in which R1=substituted or unsubstituted hydrocarbon radical, R2=substituted or unsubstituted hydrocarbon radical with at least one polymerizable double bond, R3?H or substituted or unsubstituted hydrocarbon radical, R4?H, electron-withdrawing substituent or substituted or unsubstituted hydrocarbon radical and X?O, S, NH or NR5, wherein R5 is a substituted and/or unsubstituted hydrocarbon radical. Moreover, the invention relates to another ophthalmologic composition and an ophthalmologic lens.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: July 2, 2013
    Assignee: Acri.Tec GmbH
    Inventor: Juergen Nachbaur
  • Patent number: 8471040
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: October 10, 2011
    Date of Patent: June 25, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric L. Stangeland, Lori Jean Patterson, Daisuke Roland Saito
  • Patent number: 8455665
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: August 17, 2012
    Date of Patent: June 4, 2013
    Assignee: Theravance, Inc.
    Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
  • Patent number: 8436192
    Abstract: Ester derivatives of 2-amino-2-phenyl-alkanol of general formula (I) in which: R1 forms with R3 and the nitrogen and carbon atoms to which they are respectively attached, a heterocycle with 4 to 7 members, optionally substituted in the ? position of the nitrogen atom by one or two Ra and Rb radicals being able to be independently of one another hydrogen or linear or branched alkyl (1 to 4C), and R2 is H or a —CO—O—CHR4—OCOR5 radical for which R4 is H or linear or branched alkyl (1 to 4C), and R5 is alkyl optionally substituted by benzyloxycarbonylamino, acylamino or by the remainder of an amino acid, or represents a heterocycle, or R2 is linear or branched alkyl (1 to 4C), alkyl (2 to 4C) substituted by OH, alkoxy, alkylthio, NH2, alkylamino, dialkylamino optionally forming with the nitrogen atom to which they are attached, a heterocycle with 5 or 6 members, it being understood that the substituted alkyl radical is linear or branched and comprises at least 2C between >N—R2 and the substituent, unless speci
    Type: Grant
    Filed: July 28, 2010
    Date of Patent: May 7, 2013
    Assignee: Oraxcell
    Inventors: Jean Pachot, Christophe Dini
  • Publication number: 20130085172
    Abstract: The invention provides crystalline hydrochloride salts of (S)-3-[(S)-2-methanesulfonyl-1-(4-trifluoromethylphenoxy)ethyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salts, processes and intermediates for preparing the crystalline salts, and methods of using the crystalline salts to treat diseases.
    Type: Application
    Filed: September 28, 2012
    Publication date: April 4, 2013
    Inventors: Pierre-Jean COLSON, Timothy FASS, Venkat R. THALLADI
  • Publication number: 20130053572
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that is susceptible to hydrolytic instability that may translate into reduced liver residence times and reduced hepatocellular toxicity. The present invention employs acetals and ketals to provide a low pH sensitive chemical handle for degradation.
    Type: Application
    Filed: January 19, 2011
    Publication date: February 28, 2013
    Inventors: Steven L. Colletti, Zhengwu James Deng, Matthew G. Stanton, Weimin Wang, Ivory Hills
  • Patent number: 8383669
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: March 20, 2012
    Date of Patent: February 26, 2013
    Assignee: Theravance, Inc.
    Inventor: Daisuke Roland Saito
  • Patent number: 8378121
    Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: February 19, 2013
    Assignee: Theravance, Inc.
    Inventors: YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
  • Patent number: 8366956
    Abstract: A quaternary ammonium salt of the formula (1), a composition containing the quaternary ammonium salt and an organic solvent, and an electrochemical device using the salt wherein R1 and R2 are both methyl and X? is BF4? or N(CF3SO2)2?.
    Type: Grant
    Filed: November 9, 2010
    Date of Patent: February 5, 2013
    Assignees: Otsuka Chemical Co., Ltd., Stella Chemifa Corporation
    Inventors: Tetsuo Nishida, Yasutaka Tashiro, Megumi Tomisaki, Masashi Yamamoto, Kazutaka Hirano, Akihiro Nabeshima, Hiroaki Tokuda, Kenji Sato, Takashi Higono
  • Publication number: 20120309985
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: August 17, 2012
    Publication date: December 6, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric STANGELAND, Jane SCHMIDT, Daisuke Roland SAITO, Adam HUGHES, Lori Jean PATTERSON
  • Patent number: 8273786
    Abstract: In one aspect, the invention relates to compounds of formula I: where R1-6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin and norepinephrine reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Grant
    Filed: July 14, 2010
    Date of Patent: September 25, 2012
    Assignee: Theravance, Inc.
    Inventors: Eric Stangeland, Jane Schmidt, Daisuke Roland Saito, Adam Hughes, Lori Jean Patterson
  • Publication number: 20120225886
    Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.
    Type: Application
    Filed: August 24, 2010
    Publication date: September 6, 2012
    Applicant: Merck Sharp & Dohme, Corp.
    Inventors: Scott D. Edmondson, Lehua Chang, Nam Fung Kar, Gregori J. Morriello, Christopher R. Moyes, Dong-Ming Shen, Cheng Zhu, Neville J. Anthony, Philip Jones, Graham F. Smith, Mark E. Scott, Christopher F. Thompson, Joon Jung, Carolyn Cammarano, Dawn Marie Hoffman
  • Publication number: 20120225485
    Abstract: The present invention discloses methods for producing synthetic surfaces that mimic collagen coated surfaces for cell culture comprising: providing a monomer source comprising one or more organic compounds which are capable of polymerization, wherein at least one organic compound is prolinol; creating a plasma of said monomer source; and contacting at least a portion of a surface with the plasma to provide a plasma polymer coated surface. Advantageously, such methods provide an animal-free, synthetic, chemically defined surface that mimics a collagen coated surface for cell culture. Advantageously, such methods not only reduce the cost and/or issues associated with animal-derived collagen but are also amenable to large scale manufacturing.
    Type: Application
    Filed: May 15, 2012
    Publication date: September 6, 2012
    Applicant: BECTON, DICKINSON AND COMPANY
    Inventors: Xiaoxi Kevin Chen, Kristina Parry, Anita Mistry, Deepa Saxena
  • Patent number: 8227623
    Abstract: The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.
    Type: Grant
    Filed: May 24, 2010
    Date of Patent: July 24, 2012
    Assignee: MSD Oss B.V.
    Inventors: Gerardus Johannes Kemperman, Timothy Lee Stuk, Jacobus Johannes Maria Van Der Linden
  • Publication number: 20120100274
    Abstract: The present invention relates to a method for synthetizing a compound of the following formula (I): wherein R is a methyl or ethyl group, n is 1 or 2, and X is a CH2 or CD2 group, from a compound of the following formula (II): wherein R and n are as defined above, and also relates to a method for assaying the compounds of the formula (I) using a corresponding deuterated derivative as an internal reference, as well as to the use of ketal derivatives of compounds of the formula (I) as a stable precursor, in particular in a flavoring composition.
    Type: Application
    Filed: June 24, 2010
    Publication date: April 26, 2012
    Inventors: Alain Morere, Chantal Menut, Yusuf Ziya Gunata, Abdelhamid Agrebi
  • Patent number: 8163794
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: June 30, 2011
    Date of Patent: April 24, 2012
    Assignee: Theravance, Inc.
    Inventors: Daisuke Roland Saito, Miroslav Rapta
  • Publication number: 20120088799
    Abstract: In one aspect, the invention relates to compounds of formula I: where X, Y, R1, R2, R3, R4, R4, and n are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds of formula I are serotonin reuptake inhibitors. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
    Type: Application
    Filed: October 10, 2011
    Publication date: April 12, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Eric L. STANGELAND, Lori Jean PATTERSON, Daisuke Roland SAITO
  • Publication number: 20120022271
    Abstract: [Object] A novel method for producing an optically active pyrrolidine compound, which is useful as a production intermediate of a pharmaceutical, and a production intermediate thereof, is provided. [Means for Solution] According to the production method of the present invention, a chloro compound that is a key intermediate can be produced efficiently industrially by subjecting a mixture of regioisomers obtained by reacting an optically active epoxy compound substituted with aryl, which is easily available, with an amine compound, to chlorination. Furthermore, an optically active pyrrolidine compound can be produced industrially efficiently with the key intermediate.
    Type: Application
    Filed: April 13, 2010
    Publication date: January 26, 2012
    Applicant: ASTELLAS PHARMA INC.
    Inventors: Atsushi Ohigashi, Takashi Kikuchi
  • Publication number: 20120010265
    Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Application
    Filed: June 30, 2011
    Publication date: January 12, 2012
    Inventors: Daisuke Roland SAITO, Miroslav RAPTA
  • Publication number: 20120004220
    Abstract: Provided herein are compounds of formulae I to II that bind to androgen receptors and/or modulate activity of androgen receptors; and to methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Application
    Filed: December 12, 2008
    Publication date: January 5, 2012
    Inventor: Lin Zhi