Hydroxy, Bonded Directly To Carbon, Or Ether In Substituent Q (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/165)
  • Publication number: 20150141437
    Abstract: The use of compounds of formula wherein R2, R3, R4, R5, R6 and R7 have several meanings, for the treatment of disorders mediated by protozoan organisms, novel compounds of the above formula and intermediates for the preparation of such compounds, pharmaceutical compositions comprising such novel compounds, a method of treating disorders mediated by protozoan organisms comprising administering such compounds, optionally together with a second drug substance, to a subject in need thereof and the use of such compounds, whenever comprising a photoaffinity label, for the identification of the molecular target(s) of arylamino alcohol antimalarials.
    Type: Application
    Filed: June 10, 2013
    Publication date: May 21, 2015
    Inventors: Hubert Gstach, Peter Chiba, Matthias Mastalir
  • Publication number: 20150133407
    Abstract: The invention relates to the compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, solvates, enantiomers, stereoisomers and hydrates thereof. The pharmaceutical compositions comprising an effective amount of compounds of formula I, and methods for the treatment of respiratory disorders may be formulated for oral, buccal, rectal, topical, transdermal, transmucosal, intravenous, parenteral administration, syrup, or injection. Such compositions may be used to treatment of viscid or excessive mucus, cough, inflammation, redness in sore throat, infection in the throat, sore throat, abnormal mucus secretion, impaired mucus transport, allergic rhinitis, asthma, COPD, respiratory muscular disorders and pain in acute sore throat.
    Type: Application
    Filed: May 14, 2013
    Publication date: May 14, 2015
    Inventor: Mahesh Kandula
  • Patent number: 8987262
    Abstract: The present technology relates the use of a beta blocker for the manufacture of a medicament for the treatment of hemangiomas, for example of infantile hemangiomas. The beta blocker may be a non-selective beta-blocker, for example propranolol. The present technology provides an alternative to the known compounds, e.g. corticosteroïds, interferon or vincristine, generally used for the treatment of hemangiomas.
    Type: Grant
    Filed: November 16, 2012
    Date of Patent: March 24, 2015
    Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de Bordeaux
    Inventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
  • Publication number: 20150057451
    Abstract: The present invention provides organic molecules and methods thereof for reactions between organoboron reagents and double bonds, such as imines or carbonyls, to stereoselectively provide chiral products including amines and alcohols, entities useful for the preparation of biologically active molecules.
    Type: Application
    Filed: March 1, 2013
    Publication date: February 26, 2015
    Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
  • Publication number: 20150025274
    Abstract: This invention relates to processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).
    Type: Application
    Filed: August 29, 2012
    Publication date: January 22, 2015
    Applicant: SIGNA S.A. DE C.V.
    Inventors: Pablo Miguel Bernal-Vazquez, José Miguel Lazcano-Seres, Yaneth Mariá-Antonieta Contreras-Martinez, Jorge Alberto Juárez-Lagunas, Donato Sánchez-Mereles, Juan Rolando Vázquez-Miranda, Armando Zambrano-Huerta
  • Publication number: 20140350284
    Abstract: Provided herein are compositions including diastereomers in substantially diastereomerically pure form and enantiomers in substantially enantiomerically pure form, and processes for preparing them and converting them to metyrosine.
    Type: Application
    Filed: August 8, 2014
    Publication date: November 27, 2014
    Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
  • Publication number: 20140350019
    Abstract: The present invention relates to aniline derivatives of formula (I), to their preparation and to their therapeutic application, for example in treating glaucoma: Formula (I), R1a represents H, an halogen, a (C1-C6)alkyl or a CN; R1b represents H, an halogen or a (C1-C6)alkyl; R1c represents H or a (C1-C6)alkyl; R2 represents H, an halogen, an OH, an O—(C1-C6)alkyl or (C1-C6)alkyl; R3 represents H, an halogen, a (C1-C6)alkyl, an OH, an O—(C1-C6)alkyl, a CONH2 or CN; R4 represents H, an halogen or a (C1-C6)alkyl; R5 represents H or F: R7 represents H or F; R8 represents H or F; R9 represents H or (C1-C6)alkyl, or one of its enantiomers.
    Type: Application
    Filed: September 7, 2012
    Publication date: November 27, 2014
    Applicant: FOVEA PHARMACEUTICALS
    Inventors: John Feutrill, Caroline Leriche, David Middlemiss
  • Publication number: 20140336262
    Abstract: Disclosed herein are naphthamide and quinoline carboxamide compounds containing two bicyclic moieties, pharmaceutical compositions comprising those compounds and methods of using the compositions in the treatment of cancers mediated by cyclic-AMP (cAMP) response element binding protein (CREB). The disclosed compositions have utility in the treatment of lung, prostate and breast cancers in a human subject.
    Type: Application
    Filed: November 2, 2012
    Publication date: November 13, 2014
    Applicant: OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Xiangshu Xiao, Bingbing Li, Fuchun Xie
  • Patent number: 8853453
    Abstract: The present invention relates to processes for reducing impurities in lacosamide during the preparation of lacosamide. The invention provides processes for minimizing or removing impurities such as (2R)-2-(acetylamino)-3-(benzylamino)-3-oxopropyl acetate of Formula II or (2R)-2-propanoylamino-N-benzyl-3-methoxypropionamide of Formula III in lacosamide.
    Type: Grant
    Filed: January 31, 2011
    Date of Patent: October 7, 2014
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Hari Mohan Sriram, Mukesh Kumar Madhra, Mukesh Kumar Sharma
  • Patent number: 8846763
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C1-C5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: September 30, 2014
    Assignee: Newron Pharmaceuticals, S.p.A.
    Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Publication number: 20140288040
    Abstract: The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyc
    Type: Application
    Filed: October 31, 2012
    Publication date: September 25, 2014
    Applicant: ASTEX THERAPEUTICS LIMITED
    Inventors: Andrew James Woodhead, Gianni Chessari, Gilbert Ebai Besong, Maria Grazia Carr, Steven Douglas Hiscock, Michael Alistair O'Brien, David Charles Rees, Susanne Maria Saalau-Bethell, Hendrika Maria Gerarda Willems, Neil Thomas Thompson
  • Publication number: 20140271527
    Abstract: The present disclosure provides polymer conjugates comprising a polymer and an agent, the agent linked to the polymer via a linking group containing a cleavable moiety.
    Type: Application
    Filed: November 1, 2012
    Publication date: September 18, 2014
    Applicant: Serina Therapeutics, Inc.
    Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
  • Publication number: 20140274699
    Abstract: Described herein are methods and compositions for enhancing pathogen immunity in plants and improving plant growth.
    Type: Application
    Filed: March 11, 2014
    Publication date: September 18, 2014
    Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Thomas Eulgem, Melinda Rodriguez-Salus, Colleen M. Knoth
  • Publication number: 20140235738
    Abstract: A latent curing agent obtained by the reaction of a coumarin compound of the general formula (1), where X and Y can be independently H, an alkyl group, a heteroalkyl group, an aromatic group, a heteroaromatic group or an acetyl group and Z can be H, OH, an alkyl group, a heteroalkyl group, an aromatic group, a heteroaromatic group with an amine of the general formula (2), where “a” is 1 or 2, A can be an alkylene group, a heteroalkylene group, an aromatic group, a heteroaromatic group, and B can be an alkyl group (if a=1), an alkylene group (if a=2), a heteroalkyl group (if a=1), a heteroalkylene group (if a=2), an aromatic group, a heteroaromatic group, a hydroxyl group (if a=1), a secondary amino group (if a=2), O or S (if a=2), whereby B has the valency “a”, or where B alone or where A and B together form a ring system selected from an aliphatic ring system, a heteroaliphatic ring system, or an aromatic ring system, can be used for curable compositions with a polyepoxide which has at least 2 1,2-ep
    Type: Application
    Filed: May 1, 2014
    Publication date: August 21, 2014
    Applicant: Henkel AG & Co. KGaA
    Inventors: Masashi Horikiri, Atsushi Sudo, Takeshi Endo
  • Publication number: 20140155357
    Abstract: The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for tetracycline compounds such as blocking tetracycline efflux and modulation of gene expression.
    Type: Application
    Filed: June 14, 2013
    Publication date: June 5, 2014
    Inventors: Paul Abato, Haregewein Assefa, Joel Berniac, Beena Bhatia, Todd Bowser, Jackson Chen, Mark Grier, Laura Honeyman, Mohamed Y. Ismail, Mark L. Nelson, Kwasi Ohemeng, Jingwen Pan
  • Publication number: 20140128614
    Abstract: To provide pesticidal allylAryl heterocycle derivatives that are useful as a pesticidal compound. Pesticidal allylAryl heterocycle derivatives that are expressed by the Formula (I), and pesticides and an agent for controlling animal parasites which include the allylAryl heterocycle derivatives as an effective component.
    Type: Application
    Filed: April 24, 2012
    Publication date: May 8, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Mamoru Hatazawa, Tetsuya Murata, Peter Bruechner, Daiei Yamazaki, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Tadashi Ishikawa
  • Publication number: 20140088074
    Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.
    Type: Application
    Filed: May 29, 2012
    Publication date: March 27, 2014
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventor: Paolo Pevarello
  • Publication number: 20140051758
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides, and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to a reduction reaction with a reducing agent selected from sodium borohydride and potassium borohydride in an appropriate amount of an organic solvent selected from C1-C5 lower alkanols, allowing the formation and presence during a substantial position of the reduction reaction course of a suspension of the Schiff base into the saturated solution of the Schiff base into the same organic solvent.
    Type: Application
    Filed: August 7, 2013
    Publication date: February 20, 2014
    Applicant: Newron Pharmaceuticals S.p.A.
    Inventors: Elena BARBANTI, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Publication number: 20140018549
    Abstract: Compounds of Formula I are useful for the treatment of anxiety disorders such as generalized anxiety disorder (GAD), panic attack, post traumatic stress disorder (PTSD), obsessive compulsive disorder (OCD) and social phobias, wherein: A is chosen from: aryl or heteroaryl, A being optionally substituted with up to 5 independently-selected groups R8; R1 is chosen from: alkyl or haloalkyl; R2 is chosen from: H, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7; R3, R4 and R5 are independently chosen from: H or alkyl; R6 and R7 are independently chosen from: H or alkyl; and R8 is chosen from: OH, CN, halo, alkyl, alkoxy, haloalkyl, haloalkoxy, C(O)R6, C(O)OR6, SO2R6 or C(O)NR6R7.
    Type: Application
    Filed: April 25, 2013
    Publication date: January 16, 2014
    Applicant: NPS Pharmaceuticals, Inc.
    Inventor: NPS Pharmaceuticals, Inc.
  • Publication number: 20130303568
    Abstract: The invention is directed to substituted 2-aminoacetamides represented by formula (II): and to pharmaceutically acceptable salts and prodrugs thereof, wherein the substituents are defined herein. The invention is also directed to the use of substituted 2-aminoacetamides in methods for the treatment of neuronal damage following global and focal ischemia, and for the treatment, prevention or amelioration of pain, anxiety, or manic depression, as anticonvulsants, as antimanic depressants, as local anesthetics, as antiarrhythmics and for the treatment or prevention of diabetic neuropathy.
    Type: Application
    Filed: April 22, 2013
    Publication date: November 14, 2013
    Inventors: Nancy C. LAN, Yan Wang, Sui Xiong Cai
  • Publication number: 20130289122
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly useful for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital and gastrointestinal diseases.
    Type: Application
    Filed: March 11, 2013
    Publication date: October 31, 2013
    Inventor: Newron Pharmaceuticals S.P.A.
  • Publication number: 20130289275
    Abstract: The present disclosure describes a novel, cost-effective process for preparation of a 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino-[2,1-a]isoquinoline derivatives. Specifically, it discloses a process for the preparation of the anthelmintic drug praziquantel through the use of a novel intermediate, 2-[(2,2-dimethoxyethyl)benzyl amino]-N-phenethylacetamide. This present disclosure also describes a novel crystalline form of 4-oxo-1,2,3,6,7,11b-hexahydro-4H-pyrazino[2,1-a]isoquinoline.
    Type: Application
    Filed: June 12, 2013
    Publication date: October 31, 2013
    Inventors: Lingappa BALAYA, Mahalinga MANJATHURU, Yogeesh DERAMBALA, Pejakala Kakrannaya VASUDEVA, Thangavel ARULMOLI
  • Publication number: 20130244995
    Abstract: Compounds of general formula (I), their use as calcium receptor-active compounds for the prophylaxis, treatment or amelioration of physiological disorders or diseases associated with disturbances of CaSR activity, such as hyperparathyroidism, pharmaceutical compositions comprising said compounds, and methods of treating diseases with said compounds.
    Type: Application
    Filed: November 21, 2011
    Publication date: September 19, 2013
    Applicant: LEO PHARMA A/S
    Inventors: Per Vedsø, Lars Kristian Albert Blæhr
  • Patent number: 8530701
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]-propanamides and their salts with pharmaceutically acceptable acids with a high degree of purity, i.e. with a content of dibenzyl derivatives impurities lower than 0.03% by weight. The process is carried out by submitting a Schiff base intermediate to a reduction reaction with a reducing agent in an amount of organic solvent to allow the formation (and presence during a substantial portion of the reduction reaction) of a suspension of the Schiff base.
    Type: Grant
    Filed: December 1, 2008
    Date of Patent: September 10, 2013
    Assignee: Newron Pharmaceuticals, S.p.A.
    Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
  • Patent number: 8519000
    Abstract: Substituted 2-[2-(phenyl)ethylamino]alkaneamide derivatives, pharmaceutically acceptable salts thereof, and pharmaceutical compositions containing them are useful as sodium and/or calcium channel modulators for preventing, alleviating and curing pathologies wherein the above mechanisms play a pathological role. The compounds may be particularly used for the prevention, alleviation, and curing of, for example, neurological, cognitive, psychiatric, inflammatory, urogenital, and gastrointestinal diseases.
    Type: Grant
    Filed: May 14, 2008
    Date of Patent: August 27, 2013
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
  • Patent number: 8518995
    Abstract: A method for a prevention and/or treatment of irritable bowel syndrome or amelioration of a symptom thereof in a subject, comprises administering to said subject an effective amount of a compound of formula I:
    Type: Grant
    Filed: April 4, 2011
    Date of Patent: August 27, 2013
    Assignee: MediciNova, Inc.
    Inventors: Kazuko Matsuda, Yuichi Iwaki, Kale Ruby
  • Publication number: 20130121919
    Abstract: The invention provides for a method for screening compounds that bind to and modulate a histone acetyltransferase protein. The invention further provides methods for treating neurodegenerative disorders, conditions associated with accumulated amyloid-beta peptide deposits, Tau protein levels, and/or accumulations of alpha-synuclein as well as cancer by administering a HAT-activating compound to a subject.
    Type: Application
    Filed: June 11, 2012
    Publication date: May 16, 2013
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
  • Patent number: 8378142
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Grant
    Filed: June 7, 2011
    Date of Patent: February 19, 2013
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
  • Patent number: 8278485
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
    Type: Grant
    Filed: November 3, 2011
    Date of Patent: October 2, 2012
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
  • Publication number: 20120238653
    Abstract: A latent curing agent obtained by the reaction of a coumarin compound with an amine.
    Type: Application
    Filed: April 9, 2012
    Publication date: September 20, 2012
    Applicant: Henkel AG & Co. KGaa
    Inventors: Masashi Horikiri, Atsushi Sudo, Takeshi Endo
  • Publication number: 20120214852
    Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are alkoxyl derivative compounds 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: November 8, 2011
    Publication date: August 23, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
  • Publication number: 20120190012
    Abstract: The invention provides compositions and methods useful in DNA sequencing. In exemplary embodiments, a detectable label such as a luminescent macrocycle is used.
    Type: Application
    Filed: April 6, 2011
    Publication date: July 26, 2012
    Applicant: LUMIPHORE, INC.
    Inventors: Nathaniel G. BUTLIN, Ga-Lai LAW, Christopher ANDOLINA
  • Publication number: 20120157712
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
    Type: Application
    Filed: November 3, 2011
    Publication date: June 21, 2012
    Applicant: NEWRON PHARMACEUTICALS S.P.A.
    Inventors: ELENA BARBANTI, CARLA CACCIA, PATRICIA SALVATI, FRANCESCO VELARDI, TIZIANO RUFFILLI, LUIGI BOGOGNA
  • Patent number: 8143448
    Abstract: The present invention relates to a process for the preparation of (2S,3S)-3-amino-N-cyclopropyl-2-hydroxyalkanamides as well as novel compounds prepared or used in the process.
    Type: Grant
    Filed: June 12, 2009
    Date of Patent: March 27, 2012
    Assignee: ViroBay, Inc.
    Inventor: Jeffrey Dener
  • Publication number: 20120071654
    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: Application
    Filed: June 28, 2011
    Publication date: March 22, 2012
    Applicant: THERAVANCE, INC.
    Inventors: Robert M. McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke R. Saito
  • Publication number: 20120053346
    Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Application
    Filed: August 30, 2011
    Publication date: March 1, 2012
    Inventor: Hubert Maehr
  • Publication number: 20120046293
    Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.
    Type: Application
    Filed: October 10, 2011
    Publication date: February 23, 2012
    Applicant: Merck Frosst Canada Ltd.
    Inventors: CHRISTOPHER I. BAYLY, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20120041038
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120041039
    Abstract: Provided are amine derivative compounds, pharmaceutical compositions thereof, and methods of treating ophthalmic diseases and disorders, such as age-related macular degeneration and Stargardt's Disease, using said compounds and compositions.
    Type: Application
    Filed: October 21, 2011
    Publication date: February 16, 2012
    Applicant: Acucela Inc.
    Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
  • Publication number: 20120027844
    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: Application
    Filed: February 9, 2010
    Publication date: February 2, 2012
    Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITY
    Inventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
  • Publication number: 20120022086
    Abstract: Novel compounds, compositions, and methods related to the activation of the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing a catecholamine backbone and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods, compositions, and compounds for the treatment of disorders including neurological disorders, neuropsychiatric disorders, and metabolic disorders are provided. For example, a first method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes administering to the subject a therapeutically effective amount of the described compounds. A further method of promoting neuroprotection in a subject also is provided, which includes administering to the subject a therapeutically effective amount of the described compounds.
    Type: Application
    Filed: March 17, 2010
    Publication date: January 26, 2012
    Applicant: EMORY UNIVERSITY
    Inventor: Keqiang Ye
  • Patent number: 8093426
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Grant
    Filed: December 3, 2008
    Date of Patent: January 10, 2012
    Assignee: Ranbaxy Laboratories Limited
    Inventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
  • Publication number: 20120004462
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Application
    Filed: June 7, 2011
    Publication date: January 5, 2012
    Applicant: RANBAXY LABORATORIES LIMITED
    Inventors: Mukesh Kumar MADHRA, Pankaj Kumar Singh, Chandra Has Khanduri
  • Publication number: 20120004452
    Abstract: The present invention is concerned with novel compounds and their use for the preparation of lacosamide. The present invention also contemplates processes for the preparation of lacosamide employing the novel compound of general Formula II, Formula IIa or Formula IIb as intermediate. Wherein R1 is —OH or —OMe; R2 is —OH or —NH—CH2—C6H5.
    Type: Application
    Filed: June 7, 2011
    Publication date: January 5, 2012
    Inventors: Mukesh Kumar MADHRA, Pankaj Kumar Singh, Chandra Has Khanduri
  • Publication number: 20110312875
    Abstract: The present invention provides a compound of formula I, II, III and IV as defined herein and pharmaceutically acceptable derivatives thereof. The present invention further provides use of the compounds of the present invention in the treatment of bacterial infection and in the treatment of HIV infection. Also provided are pharmaceutical compositions comprising the compounds of the present invention.
    Type: Application
    Filed: August 2, 2011
    Publication date: December 22, 2011
    Applicant: UNIVERSITY OF WOLLONGONG
    Inventors: Timothy Patrick Boyle, John Barnard Bremner, Zinka Brkic, Jonathan Alan Victor Coates, Neal Kevin Dalton, John Deadman, Paul Anthony Keller, Jody Morgan, Stephen Geoffrey Pyne, David Ian Rhodes, Mark James Robertson
  • Patent number: 8076514
    Abstract: The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (xx); X is selected from CH, CF and N, R5 is selected from H, C1-C6 alkyl, C1-C6 fluoroalkyl, and —OR12, R9 is selected from H and —C(O)NR1OR1 1, R12 is selected from H, C1-C6 alkyl and C3-C6 cycloalkyl for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes.
    Type: Grant
    Filed: July 14, 2006
    Date of Patent: December 13, 2011
    Assignee: Eli Lilly and Company
    Inventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley
  • Patent number: 8076515
    Abstract: A process for obtaining therapeutically active 2-[4-(3- and 2-(fluorobenzyloxy)benzylamino]propanamides and their salts with pharmaceutically acceptable acids with high purity degree, in particular, with a content of dibenzyl derivatives impurities lower than 0.03%, preferably lower than 0.01% by weight. The process is carried out by submitting the Schiff bases intermediates 2-[4-(3- and 2-fluorobenzyloxy)benzylideneamino]propanamides to catalytic hydrogenation in the presence of a heterogeneous catalyst in a protic organic solvent.
    Type: Grant
    Filed: December 18, 2008
    Date of Patent: December 13, 2011
    Assignee: Newron Pharmaceuticals S.p.A.
    Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
  • Publication number: 20110301179
    Abstract: A compound (particularly useful for inhibiting cancer) according to formula I: or a pharmaceutically acceptable salt thereof, wherein: x is 0 or 1; R1-R6 are each independently H, —CN, —NO2, —NO, —OH, halogen, hydroxyalkyl, carboxyl, substituted carboxyl, aminocarbonyl, alkoxy, carbonyl or substituted carbonyl; R7 is H, alkyl, alkyl amino, aminoacyl, hydroxyacyl, heteroaryl, heterocycloalkyl, alkyl heteroaryl or alkyl heterocycloalkyl; R8 is H or alkyl; A is O or N; and Ar is an aryl, substituted aryl, heteroaryl, or substituted heteroaryl, provided that if R7 is H then Ar is aryl substituted with alkyl amino.
    Type: Application
    Filed: October 21, 2009
    Publication date: December 8, 2011
    Inventors: Xiangshu Xiao, Bingbing Li
  • Patent number: 8063105
    Abstract: The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.
    Type: Grant
    Filed: July 20, 2006
    Date of Patent: November 22, 2011
    Assignee: Merck Canada Inc.
    Inventors: Christopher I. Bayly, Austin C. Chen, Daniel Dube, Laurence Dube, Michel Gallant, Patrick Lacombe, Dwight MacDonald, Daniel McKay, David A. Powell, Erich L. Grimm
  • Publication number: 20110263604
    Abstract: The invention relates to phenylcyclopropylamine acetamide derivatives and their use in treating diseases.
    Type: Application
    Filed: April 18, 2011
    Publication date: October 27, 2011
    Applicant: Oryzon Genomics, S.A.
    Inventors: Nathalie Guibourt, Alberto Ortega Munoz, Julio Castro-Palomino Laria