Chalcogen Attached Indirectly To The Hetero Ring By Nonionic Bonding Patents (Class 549/75)
  • Patent number: 10682323
    Abstract: Provided is a novel therapeutic agent for glaucoma, which has sGC-activating action. A therapeutic agent for glaucoma or an ocular hypotensive agent, which contains, as an effective component, a compound represented by Formula (I-a) or Formula (I-b) and having a Log D value of more than 1.5 and less than 2.5, or a pharmaceutically acceptable salt thereof. [In formulae (I-a) and (I-b), each symbol is as defined in the description.
    Type: Grant
    Filed: July 21, 2017
    Date of Patent: June 16, 2020
    Assignee: TOA EIYO LTD.
    Inventors: Toshihiro Sawabe, Fumito Maruyama, Akiyuki Takaya, Takeshi Hasegawa
  • Patent number: 10611749
    Abstract: The present invention relates to a novel process for the preparation of Rotigotine of formula (I) and intermediates thereof.
    Type: Grant
    Filed: February 14, 2019
    Date of Patent: April 7, 2020
    Assignee: Solara Active Pharma Sciences Limited
    Inventors: Victor Paul Raj Irudayaraj, Senthilkumar Subramani, Vedhachalam Govindaraj, Jeyakanthan Jayavelu, Boopathy Jayaraman, Uttam Kumar Ray, Tangirala Vittal
  • Patent number: 9034914
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol(rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Grant
    Filed: March 31, 2014
    Date of Patent: May 19, 2015
    Assignee: UCB PHARMA GMBH
    Inventors: Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
  • Publication number: 20150112086
    Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
    Type: Application
    Filed: December 23, 2014
    Publication date: April 23, 2015
    Inventors: Dominique Michel, Rudolf Fuchs
  • Patent number: 9012660
    Abstract: The present disclosure relates to 5,6,7,8-tetrahydro-6-[N,N-bis[(2-thienyl)ethyl]]amino-1-naphthol, a method for preparing the same, and use of 5,6,7,8-tetrahydro-6-[N,N-bis[(2-thienyl)ethyl]]amino-1-naphthol as a reference compound for determining an impurity in rotigotine or a preparation thereof.
    Type: Grant
    Filed: August 6, 2012
    Date of Patent: April 21, 2015
    Assignee: Shandong Luye Pharmaceutical Co., Ltd.
    Inventors: Mina Yang, Yanyan Zhao, Fengmei Zhou, Quingguo Meng, Tao Wang
  • Publication number: 20150105429
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2014
    Publication date: April 16, 2015
    Applicant: GENENTECH, INC.
    Inventors: Benjamin Fauber, Olivier Rene
  • Publication number: 20150080451
    Abstract: Potent low molecular weight, highly selective, competitive non-peptidic serine protease inhibitors and their use in treating serine protease-associated diseases are disclosed.
    Type: Application
    Filed: September 12, 2012
    Publication date: March 19, 2015
    Applicant: THE JOHNS HOPKINS UNIVERSITY
    Inventors: Ernesto Freire, Patrick C. Ross, Rogelio Siles
  • Patent number: 8981122
    Abstract: The present invention provides a method for producing an N-monoalkyl-3-hydroxy-3-arylpropylamine compound represented by Formula (2): wherein Ar represents an optionally substituted aryl or an optionally substituted heteroaryl, R represents an optionally substituted C1-5 alkyl, and * represents an asymmetric carbon atom; the method comprising:reacting, in the presence of an asymmetric reduction catalyst, hydrogen gas with an N-benzyl-N-monoalkyl-3-oxo-3-arylpropenylamine compound represented by Formula (1): wherein Ar and R are as defined above. The present invention allows an optically active N-monoalkyl-3-hydroxy-3-arylpropylamine compound to be produced easily and inexpensively under industrially advantageous conditions.
    Type: Grant
    Filed: March 23, 2011
    Date of Patent: March 17, 2015
    Assignee: Sumitomo Seika Chemicals Co., Ltd.
    Inventors: Kenji Kogami, Shuzo Satake
  • Publication number: 20150065725
    Abstract: In OLEDs, improved efficiency is obtained by compounds which can form inter alia electron injection layers of the formula (I) wherein R1 is a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with one or more C1-C4 alkyl, alkoxy or cyano; R2 and R3 together form a 1-5 ring aryl (including polycyclic), aralkyl or heteroaryl group which is optionally substituted with C1-C4 alkyl, alkoxy or cyano; R4 is hydrogen, C1-C4 alkyl or aryl; and Ar is monocyclic, bicyclic or tricyclic aryl or heteroaryl which is optionally substituted with one or more C1-C4-alkyl or alkoxy groups, or an oligomer thereof.
    Type: Application
    Filed: October 9, 2014
    Publication date: March 5, 2015
    Inventors: Poopathy KATHIRGAMANATHAN, Yun Fu CHAN
  • Publication number: 20150065538
    Abstract: Compounds of formula (I) wherein R1, R2, R3, and Y are defined in the description are TRPA1 antagonists. Compositions comprising such compounds and methods for treating conditions and disorders using such compounds and compositions are also disclosed.
    Type: Application
    Filed: November 4, 2014
    Publication date: March 5, 2015
    Inventors: Richard J. Perner, Michael E. Kort, Stanley DiDomenico, Jun Chen, Anil Vasudevan
  • Patent number: 8962865
    Abstract: A process is disclosed for the preparation of a compound of formula and/or an addition salt of a proton acid, wherein R1 and R2 independently represent alkyl, cycloalkyl, aryl or aralkyl, each aryl or aralkyl being optionally further substituted with alkyl, alkoxy and/or halogen.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: February 24, 2015
    Assignee: Lonza AG
    Inventors: Dominique Michel, Rudolf Fuchs
  • Publication number: 20150018341
    Abstract: The invention provides novel ethylene derivatives represented by Formula I, which may be used as selective estrogen receptor modulators (SERMs) and useful in the prophylaxis and/or treatment of estrogen-dependent conditions or conditions.
    Type: Application
    Filed: December 28, 2012
    Publication date: January 15, 2015
    Applicant: CENTAURUS BIOPHARMA CO., LTD.
    Inventors: Dengming Xiao, Li Zhu, Yuandong Hu, Rong Yu, Wei Hu, Na Zhao, Yong Peng, Hong Luo, Yongxin Han
  • Publication number: 20140377365
    Abstract: Provided herein are methods and compositions for producing formulations systemic delivery of dopamine agonists via the oral inhalation route. Specifically, provided herein are methods and compositions for a formulation of rotigotine that is suitable for administration via oral inhalation. Such methods and compositions are useful in the treatment or amelioration of one or more Parkinson's disease symptom(s).
    Type: Application
    Filed: June 18, 2014
    Publication date: December 25, 2014
    Inventors: Libo WU, Wiwik WATANABE
  • Patent number: 8906946
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Grant
    Filed: January 27, 2012
    Date of Patent: December 9, 2014
    Assignee: Dompe' S.p.A.
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140357874
    Abstract: The present invention relates to a method for preparing (S)-3-N-methylamino-1-(2-thienyl)-1-propanol and salts thereof.
    Type: Application
    Filed: August 19, 2014
    Publication date: December 4, 2014
    Inventors: Michael KREIS, Antje STEINHAUS, Guido GIFFELS, Oliver KREBS
  • Publication number: 20140323518
    Abstract: Compounds of formula (I) or a pharmaceutically acceptable ester, amide, carbamate or salt thereof, including a salt of such an ester, amide or carbamate in which R1 to R9 have meanings as defined in the Specification, are useful as estrogen receptor ligands.
    Type: Application
    Filed: August 2, 2012
    Publication date: October 30, 2014
    Inventors: Aiping Cheng, Neeraj Garg, Lars Krüger, Joakim Löfstedt, Eva Koch, Konrad Koehler, Lars Hagberg, Daniel Nöteberg
  • Publication number: 20140315898
    Abstract: The present invention relates to novel N-arylamide-substituted trifluoroethyl sulfide derivatives of the formula (I) in which X1, X2, X3, X4, R1, R2, R3, n have the meanings given in the description—to their use as acaricides and insecticides for controlling animal pests and to processes and intermediates for their preparation
    Type: Application
    Filed: December 12, 2012
    Publication date: October 23, 2014
    Applicant: BAYER CROPSCIENCE AG
    Inventors: Adeline Koehler, Bernd Alig, Angela Becker, Arnd Voerste, Ulrich Goergens, Reiner Fischer, Wahed Ahmed Moradi, Silvia Cerezo-Galvez, Julia Johanna Hahn, Kerstin Ilg, Hans-Georg Schwarz, Takuya Gomibuchi, Masahito Ito, Daiei Yamazaki, Katsuhiko Shibuya, Eiichi Shimojo
  • Patent number: 8835654
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-related disease.
    Type: Grant
    Filed: September 20, 2011
    Date of Patent: September 16, 2014
    Assignee: BHI Limited Partnership
    Inventors: Xianqi Kong, Xinfu Wu, Abderrahim Bouzide, Isabelle Valade, David Migneault, Francine Gervais, Daniel Delorme, Benoit Bachand, Mohamed Atfani, Sophie Levesque, Bita Samim
  • Publication number: 20140243386
    Abstract: The present invention relates to new salts of 6-(propyl-(2-thiophen-2-ylethyl)amino)tetralin-1-ol (rotigotine), their use as a medicament, for example for the treatment of CNS disorders like Parkinson Disease, RLS, fibromyalgia and/or depression, in particular through electromotive administration. The present invention relates to pharmaceutical formulations suitable for iontophoresis that provide enhanced iontophoretic delivery of rotigotine to at least one target tissue. The formulations are further characterized by good to excellent solubility of the salts in aqueous solutions.
    Type: Application
    Filed: March 31, 2014
    Publication date: August 28, 2014
    Applicant: UCB Pharma GmbH
    Inventors: Johanna Aaltje Bouwstra, Oliver Ackaert, Jacob Eikelenboom, Hans-Michael Wolff
  • Publication number: 20140196523
    Abstract: The present disclosure relates to 5,6,7,8-tetrahydro-6-[N,N-bis[(2-thienypethyl]]amino-1-naphthol, a method for preparing the same, and use of 5,6,7,8-tetrahydro-6-[N,N-bis[(2-thienypethyl]]amino-1-naphthol as a reference compound for determining an impurity in rotigotine or a preparation thereof.
    Type: Application
    Filed: August 6, 2012
    Publication date: July 17, 2014
    Applicant: SHANDONG LUYE PHARMACEUTICAL CO., LTD.
    Inventors: Mina Yang, Yanyan Zhao, Fengmei Zhou, Quingguo Meng, Tao Wang
  • Patent number: 8772330
    Abstract: The present disclosure concerns a compound, or a pharmaceutically acceptable salt thereof, having a formula: where at least one of R1-R4 is a heterocycle, at least one of R1-R4 is an aryl group coupled to the ring by a linker atom, functional group, or other moiety, or where none of R1-R4 is an amide, and any and all combinations thereof. Remaining R1-R4 substituents independently are aliphatic, substituted aliphatic, amine, substituted amine, aryl, substituted aryl, cyclic, substituted cyclic, halide, heteroaryl, substituted heteroaryl, heterocyclic, substituted heterocyclic, hydrogen or hydroxyl. A method for treating a subject also is provided comprising administering a disclosed compound or compounds, or a prodrug that is converted into the disclosed compound or compounds, or a composition comprising the compound, compounds, or prodrugs thereof, to a subject. A method for making disclosed compounds also is provided.
    Type: Grant
    Filed: January 20, 2012
    Date of Patent: July 8, 2014
    Assignee: State of Oregon acting by and through the State Board of Higher Education on behalf of Oregon State University
    Inventors: James David White, David T. Wong, David B. Chan, Jongtae Yang, Rajan Juniku
  • Publication number: 20140135320
    Abstract: The present invention relates to antimalarial compounds and their use against protozoa of the genus Plasmodium, including drug-resistant Plasmodia strains. This invention further relates to compositions containing such compounds and a process for making the compounds.
    Type: Application
    Filed: November 8, 2013
    Publication date: May 15, 2014
    Applicant: Jacobus Pharmaceutical Company, Inc.
    Inventors: Gavin David Heffernan, David Penman Jacobus, Kurt William Saionz, Guy Alan Schiehser, Hong-Ming Shieh, Wenyi Zhao
  • Publication number: 20140121380
    Abstract: A method for industrially preparing a nitrogen substituted 6-amino-5,6,7,8-tetrahydronaphthol is disclosed. The method comprises includes reacting a nitrogen substituted amino-5,6,7,8-tetrahydronaphthol compound of formula (II) with a 2-substituted ethyl sulfonate compound of formula (III) under an alkaline condition and in the presence of a sulfite.
    Type: Application
    Filed: June 21, 2012
    Publication date: May 1, 2014
    Applicant: SHAN DONG LUYE PHARMACEUTICAL CO., LTD.
    Inventors: Qingguo Meng, Mina Yang, Tao Wang, Qilin Wang, Jun Li, Zheng Ruan
  • Patent number: 8658400
    Abstract: The present invention relates to novel phenylethanol dehydrogenase mutants, to a method for the manufacture thereof; to coded nucleic acid sequences therefor, to expression cassettes, to vectors and recombinant microorganisms that contain said sequences; to a method for the biocatalytic synthesis of substituted, optically active alcohols and to the use of said mutants; and particularly to a method for manufacturing duloxetine alcohol or duloxetine, comprising a synthesis step catalyzed biocatalytic by said mutants.
    Type: Grant
    Filed: December 16, 2009
    Date of Patent: February 25, 2014
    Assignee: BASF SE
    Inventors: Nina Schneider, Hans Wolfgang Höffken
  • Publication number: 20140039183
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Application
    Filed: July 15, 2013
    Publication date: February 6, 2014
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Publication number: 20140031564
    Abstract: The present invention relates to a method for preparing (S)-3-N-methylamino-1-(2-thienyl)-1-propanol and salts thereof.
    Type: Application
    Filed: August 26, 2011
    Publication date: January 30, 2014
    Applicant: SALTIGO GmbH
    Inventors: Michael Kreis, Antje Steinhaus, Guido Giffels, Oliver Krebs
  • Publication number: 20140031398
    Abstract: Compounds acting as selective antagonists of Transient Receptor Potential cation channel subfamily M member 8 (hereinafter referred to as TRPM8), having formula: Wherein R is selected from: H, Br, CN, NO2, SO2NH2, SO2NHR? and SO2NR?2, where R? is selected from linear or branched C1-C4 alkyl; X is selected from: F, Cl, C1-C3 alkyl, NH2 and OH Y is selected from: O, CH2, NH and SO2 R1 and R2, independently one from the other, are selected from H, F and linear or branched C1-C4 alkyl; R3 and R4, independently one from the other, are selected from H and linear or branched C1-C4 alkyl; Z is selected from: NR6 and R6R7N+, where R6 and R7 independently one from the other, are selected from: H and linear or branched C1-C4 alkyl R5 is a residue selected from: H and linear or branched C1-C4 alkyl Het is a heteroaryl group selected from a substituted or not substituted pyrrolyl, a substituted or not substituted N-methylpyrrolyl, a substituted or not substituted thiophenyl, a substituted or
    Type: Application
    Filed: January 27, 2012
    Publication date: January 30, 2014
    Inventors: Alessio Moriconi, Gianluca Bianchini, Andrea Aramini, Laura Brandolini, Chiara Liberati, Silvia Bovolenta, Andrea Beccari, Simone Lorenzi
  • Publication number: 20140024650
    Abstract: Provided is a compound having an AMPA receptor function enhancing action, and useful as a prophylactic or therapeutic drug for depression, Alzheimer's disease, schizophrenia, attention deficit hyperactivity disorder (ADHD) and the like. A compound represented by the formula (I): wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Application
    Filed: April 5, 2012
    Publication date: January 23, 2014
    Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Shoji Fukumoto, Osamu Ujikawa, Shinji Morimoto, Yasutomi Asano, Satoshi Mikami, Norihito Tokunaga, Masakuni Kori, Toshihiro Imaeda, Koichiro Fukuda, Shinji Nakamura, Kouichi Iwanaga
  • Publication number: 20140005414
    Abstract: The present invention provides a process for preparing duloxetine hydrochloride with higher yield and lower cost.
    Type: Application
    Filed: August 29, 2013
    Publication date: January 2, 2014
    Applicant: SCI Pharmtech, Inc.
    Inventors: Bo-Fong Chen, Feng-Ju Lu, Jinun-Ban Yeh, Wei-Chyun Wong, Feng-hsu Li, Yen-Wei Li, Yeh-Chi Su
  • Publication number: 20130345283
    Abstract: A process for the preparation of Rotigotine (1) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid-sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7, 8-tetrahydro-6-(S)-N-propylamino-1-methoxy-naphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.
    Type: Application
    Filed: July 23, 2013
    Publication date: December 26, 2013
    Applicant: FIDIA FARMACEUTICI S.P.A.
    Inventors: Aldo Banfi, Gianluca Belogi, Claudio Fuganti, Roberta Pizzocaro
  • Patent number: 8614337
    Abstract: The chiral compound S-5-substituted-N-2?-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).
    Type: Grant
    Filed: September 7, 2010
    Date of Patent: December 24, 2013
    Assignee: 2Y-Chem Ltd.
    Inventors: Xungui He, Jianping Guo, Yanling Wang, Wensheng Tang, Xingzhong Zhang, Xuezhang Wang, Yuan Wang
  • Patent number: 8614336
    Abstract: The present invention provides a process for preparing a N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound. The present invention also provides a process for preparing (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine with higher yield and low treatment cost, which includes the preparation of the N-methyl-N-hydroxyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine compound.
    Type: Grant
    Filed: March 5, 2010
    Date of Patent: December 24, 2013
    Assignee: SCI Pharmtech, Inc.
    Inventors: Bo-Fong Chen, Jinun-Ban Yeh, Wei-Chyun Wong
  • Publication number: 20130324585
    Abstract: The present invention provides ionic liquids of rotigotine, pharmaceutical compositions comprising said ionic liquids and methods of preparing such ionic liquids. The invention further provides methods of using the compositions described herein to overcome problems arising from polymorphism, solubility and delivery, to control release rates, to add functionality, to enhance efficacy, and to improve ease of use and manufacture.
    Type: Application
    Filed: November 29, 2011
    Publication date: December 5, 2013
    Inventor: Christian Janssen
  • Patent number: 8592477
    Abstract: The present invention relates to a novel polymorphic form of Rotigotine characterized by at least one of the following X-ray powder diffraction peaks: 12.04, 13.68, 17.72 and 19.01±0.2 (°2?), measured with a Cu—K? irradiation (1.54060), and a process for production thereof, which is useful for the manufacture of a stable medicament for treating or alleviating symptoms of Parkinson's Disease and other dopamine-related disorders.
    Type: Grant
    Filed: November 25, 2008
    Date of Patent: November 26, 2013
    Assignee: UCB Pharma GmbH
    Inventors: Hans-Michael Wolff, Luc Quere, Jens Riedner
  • Publication number: 20130306917
    Abstract: The invention relates to a photovoltaic coating containing a mixture of organic N-type (acceptor) and P-type (donor) semiconductor compounds, which makes it possible, when selecting the donor/acceptor pair, to modulate the semiconductor properties of the photovoltaic coating so as to enable the use thereof within a photovoltaic device, wherein one of the organic semiconductors includes a quinone core.
    Type: Application
    Filed: October 21, 2011
    Publication date: November 21, 2013
    Applicant: RHODIA OPERATIONS
    Inventors: Floryan Decampo, Gerard Mignani, Bertrand Pavageau
  • Publication number: 20130273800
    Abstract: The present disclosure provides novel oligo phenylene ethynylene (OPE) compounds, methods for synthesizing these compounds, and materials and substances incorporating these compounds. The various OPEs show antibacterial, antiviral and anti-fungal activity.
    Type: Application
    Filed: July 13, 2011
    Publication date: October 17, 2013
    Applicant: Office of Technology Licensing
    Inventors: David G. Whitten, Kirk S. Schanze, Eunkyung Ji, Thomas S. Corbitt, Zhijun Zhou, Dimitri Dascier, Ying Wang, Linnea K. Ista, Anand Parthsaray
  • Publication number: 20130236434
    Abstract: A method of enhancing binding of cells to an integrin-binding ligand comprises treating integrin-expressing cells in vitro with an agonist of integrin, wherein the integrin is selected from the group consisting of ?4?1, ?5?1, ?4?7, ?v?3 and ?L?2, and contacting the treated cells with an integrin-binding ligand; integrin agonist compounds having the general formula I; methods of treating integrin-expressing cells with such agonists to enhance binding; and therapeutic methods comprising administering agonist-treated cells or agonist compounds to a mammal.
    Type: Application
    Filed: November 16, 2011
    Publication date: September 12, 2013
    Applicant: TEXAS HEART INSTITUTE
    Inventors: Ronald J. Biediger, William C. Gundlach, IV, Robert V. Market, Michael M. Savage, Peter Vanderslice
  • Publication number: 20130225619
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.
    Type: Application
    Filed: January 18, 2013
    Publication date: August 29, 2013
    Applicant: Acucela Inc.
    Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
  • Patent number: 8519160
    Abstract: A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid-sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II). The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-1-methoxynaphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.
    Type: Grant
    Filed: September 24, 2009
    Date of Patent: August 27, 2013
    Assignee: Fidia Farmaceutici S.p.A.
    Inventors: Aldo Banfi, Gialunca Belogi, Claudio Fuganti, Roberta Pizzocaro
  • Patent number: 8513162
    Abstract: There is provided a halogen-containing organosulfur compound having a controlling effect on arthropod pests represented by the formula (I): wherein m represents 0, 1 or 2; n represents 0, 1 or 2; A represents an optionally substituted 3- to 8-membered saturated heterocyclic group; Q represents a fluorine atom or a C1-C5 haloalkyl group having at least one fluorine atom; R1, R1a and R3 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.; R2, R2a and R4 independently represent an optionally halogenated C1-C4 chain hydrocarbon group, etc.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: August 20, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventor: Hiromasa Mitsudera
  • Patent number: 8507538
    Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds is provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
    Type: Grant
    Filed: November 15, 2010
    Date of Patent: August 13, 2013
    Assignee: Receptos, Inc.
    Inventors: Marcus F. Boehm, Esther Martinborough, Enugurthi Brahmachary, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam Richard Yeager
  • Patent number: 8501802
    Abstract: The present invention relates to co-crystals of duloxetine and co-crystal formers selected from COX-INHIBITORs, processes for preparation of the same and their uses as medicaments or in pharmaceutical formulations, more particularly for the treatment of pain.
    Type: Grant
    Filed: May 20, 2009
    Date of Patent: August 6, 2013
    Assignee: Laboratorios del Dr. Esteve, S.A.
    Inventors: Helmut Heinrich Buschmann, Lluis Solá Carandell, Jordi Benet Buchholz, Jordi Carles Ceròn Bertran, Jesüs Ramirez Artero
  • Publication number: 20130197013
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.
    Type: Application
    Filed: July 27, 2011
    Publication date: August 1, 2013
    Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
  • Publication number: 20130190356
    Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.
    Type: Application
    Filed: December 18, 2012
    Publication date: July 25, 2013
    Applicant: GENENTECH, INC.
    Inventor: Genetech, Inc.
  • Publication number: 20130157982
    Abstract: The present invention relates to novel amine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
    Type: Application
    Filed: February 11, 2013
    Publication date: June 20, 2013
    Applicant: ALLERGAN, INC.
    Inventor: ALLERGAN, INC.
  • Publication number: 20130102794
    Abstract: The present invention provides an alternative synthesis of N-substituted aminotetralines comprising resolution of N-substituted aminotetralins of formula (II), wherein R1, R2 and R3 are as defined for compound of formula (I).
    Type: Application
    Filed: June 24, 2011
    Publication date: April 25, 2013
    Applicant: UCB PHARMA GMBH
    Inventors: Celal Ates, Arnaud Schule, Magali Palacio, Paul Deutsch, David Vasselin, Nicolas Carly, Ganesh Phadtare, Swapnil Yerande, Jean-Pierre Delatinne, Maria Luisa Escudero Hernandez, Veronique Pinilla
  • Publication number: 20130096321
    Abstract: An isolated and pure crystalline rotigotine base of polymorph Form I, and processes for producing the crystalline rotigotine base are disclosed. Also disclosed is a transdermal patch for the delivery of rotigotine base using the disclosed isolated and pure form of rotigotine base, which can be used in treatment of Parkinson's Disease and other disorders ameliorated or treated by rotigotine, including restless leg syndrome.
    Type: Application
    Filed: December 3, 2012
    Publication date: April 18, 2013
    Applicant: CHEMAGIS LTD.
    Inventor: CHEMAGIS Ltd.
  • Patent number: 8420832
    Abstract: The present invention provides an (S)-methylhydroxylaminopropanol compound and the (S)-methylhydroxylaminopropanol compound of the present invention is used as an intermediate for preparation of (S)-(?)-3-methylamino-1-(2-thienyl)propan-1-ol, which is an intermediate for preparation of (S)-(+)-N-methyl-3-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate. The present invention also provides a process for preparing (S)-(+3-methylamino-1-(2-thienyl)propan-1-ol with higher yield and lower cost, wherein the (S)-methylhydroxylaminopropanol compound is used as an intermediate.
    Type: Grant
    Filed: March 30, 2012
    Date of Patent: April 16, 2013
    Assignee: Sci Pharmtech, Inc.
    Inventors: Bo-Fong Chen, Jinun-Ban Yeh, Weichyun Wong
  • Publication number: 20130053579
    Abstract: A process for the preparation on N-methyl-aryloxy-propanamine derivatives of the formula I and salts thereof. The invention also relates to the preparation and use novel intermediate of the formula XII. The invention also relates to the process of further conversion of novel intermediate into N-methyl-aryloxy propanamine derivatives and salts thereof. Wherein Q and P independently represents substituted or unsubstituted aryl group such as phenyl, naphthyl, pyridine, furanyl, pyranyl thienyl, and the like optionally substituted aryl by a halogen, a straight chain or branched alkyl group containing 1 to 6 carbon atoms, —O-alkyl group containing straight chain or branched C1-C6 alkyl group, an alkoxy group containing a straight chain or branched alkyl group having 1 to 6 carbon atoms, which comprises demethylation of N,N-dimethyl analogues of compound of formula IA.
    Type: Application
    Filed: November 30, 2010
    Publication date: February 28, 2013
    Applicant: ARCH PHARMALABS LIMITED
    Inventors: Nishikant Digamber Ghadge, Bapu Atmaram Chaudhari, Ganesh Gurpur Pai, Arun Kanti Mandal
  • Publication number: 20130046100
    Abstract: The chiral compound S-5-substituted-N-2?-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2?-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5).
    Type: Application
    Filed: September 7, 2010
    Publication date: February 21, 2013
    Applicant: 2Y-Chem, Ltd.
    Inventors: Xungui He, Jianping Guo, Yanling Wang, Wensheng Tang, Xingzhong Zhang, Xuezhang Wang, Yuan Wang