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)
-
Patent number: 11111208Abstract: The present application provides methods for the synthesis of intermediates in the synthesis of Safinamide or a pharmaceutically acceptable salt thereof herein Safinamide Mesylate, that is substantially free of impurities.Type: GrantFiled: June 12, 2020Date of Patent: September 7, 2021Assignee: RK PHARMA SOLUTIONS LLCInventors: Ravishanker Kovi, Jayaraman Kannappan, Rajesh A Patel, Daxeshkumar Prakashbhai Patel
-
Patent number: 11053190Abstract: The present disclosure relates to an ?-aminoamide derivative compound and a pharmaceutical composition containing the same. According to various embodiments of the present disclosure, provided is a therapeutic agent which can overcome the disadvantages of existing drugs used as a MAO-B inhibitor and, specifically, reversibly inhibits MAO-B through a non-covalent bond so as to alleviate or eliminate the side effects of the existing drugs which exhibit a therapeutic effect by irreversibly acting via a covalent bond with MAO-B. Particularly, a new compound having superior stability and efficacy compared to the existing reversible MAO-B inhibitors may be provided.Type: GrantFiled: April 24, 2020Date of Patent: July 6, 2021Assignee: NeuroBiogen Co., Ltd.Inventors: Ki Duk Park, ChangJoon Justin Lee, Dong Jin Kim, Ae Nim Pae, Hyun Ah Choo, Sun Joon Min, Yong Koo Kang, Yun Kyung Kim, Hyo Jung Song, Ji Won Choi, Min Ho Nam, Jun Young Heo, Seul Ki Yeon, Bo Ko Jang, Eun Ji Ju, Seon Mi Jo, Jong-Hyun Park
-
Patent number: 10640457Abstract: 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: GrantFiled: June 11, 2012Date of Patent: May 5, 2020Assignee: The Trustees of Columbia University in the City of New YorkInventors: Yan Feng, Mauro Fa, Ottavio Arancio, Shixian Deng, Donald W. Landry, Yitshak Francis
-
Publication number: 20150141437Abstract: 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: ApplicationFiled: June 10, 2013Publication date: May 21, 2015Inventors: Hubert Gstach, Peter Chiba, Matthias Mastalir
-
Publication number: 20150133407Abstract: 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: ApplicationFiled: May 14, 2013Publication date: May 14, 2015Inventor: Mahesh Kandula
-
Patent number: 8987262Abstract: 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: GrantFiled: November 16, 2012Date of Patent: March 24, 2015Assignees: Universite de Bordeaux, Centre Hospitalier Universitaire de BordeauxInventors: Christine Leaute-Labreze, Eric Dumas De La Roque, Alain Taieb, Jean-Benoit Thambo
-
Publication number: 20150057451Abstract: 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: ApplicationFiled: March 1, 2013Publication date: February 26, 2015Inventors: Amir H. Hoveyda, Daniel L. Silverio, Tatiana Pilyugina, Sebastian Torker, Daniel Robbins
-
Publication number: 20150025274Abstract: This invention relates to processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide (I) and intermediates thereof. Formula (I).Type: ApplicationFiled: August 29, 2012Publication date: January 22, 2015Applicant: 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: 20140350019Abstract: 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: ApplicationFiled: September 7, 2012Publication date: November 27, 2014Applicant: FOVEA PHARMACEUTICALSInventors: John Feutrill, Caroline Leriche, David Middlemiss
-
Publication number: 20140350284Abstract: 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: ApplicationFiled: August 8, 2014Publication date: November 27, 2014Inventors: Kevin John HALLORAN, Alex COMELY, Zhengming CHEN, Shyam KRISHNAN
-
Publication number: 20140336262Abstract: 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: ApplicationFiled: November 2, 2012Publication date: November 13, 2014Applicant: OREGON HEALTH & SCIENCE UNIVERSITYInventors: Xiangshu Xiao, Bingbing Li, Fuchun Xie
-
Patent number: 8853453Abstract: 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: GrantFiled: January 31, 2011Date of Patent: October 7, 2014Assignee: Ranbaxy Laboratories LimitedInventors: Hari Mohan Sriram, Mukesh Kumar Madhra, Mukesh Kumar Sharma
-
Patent number: 8846763Abstract: 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: GrantFiled: August 7, 2013Date of Patent: September 30, 2014Assignee: Newron Pharmaceuticals, S.p.A.Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
-
Publication number: 20140288040Abstract: 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 bicycType: ApplicationFiled: October 31, 2012Publication date: September 25, 2014Applicant: ASTEX THERAPEUTICS LIMITEDInventors: 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: 20140271527Abstract: 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: ApplicationFiled: November 1, 2012Publication date: September 18, 2014Applicant: Serina Therapeutics, Inc.Inventors: Randall Moreadith, Kunsang Yoon, Zhihao Fang, Rebecca Weimer, Bekir Dizman, Tacey Viegas, Michael David Bentley
-
Publication number: 20140274699Abstract: Described herein are methods and compositions for enhancing pathogen immunity in plants and improving plant growth.Type: ApplicationFiled: March 11, 2014Publication date: September 18, 2014Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Thomas Eulgem, Melinda Rodriguez-Salus, Colleen M. Knoth
-
Publication number: 20140235738Abstract: 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-epType: ApplicationFiled: May 1, 2014Publication date: August 21, 2014Applicant: Henkel AG & Co. KGaAInventors: Masashi Horikiri, Atsushi Sudo, Takeshi Endo
-
Publication number: 20140155357Abstract: 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: ApplicationFiled: June 14, 2013Publication date: June 5, 2014Inventors: 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: 20140128614Abstract: 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: ApplicationFiled: April 24, 2012Publication date: May 8, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Mamoru Hatazawa, Tetsuya Murata, Peter Bruechner, Daiei Yamazaki, Eiichi Shimojo, Teruyuki Ichihara, Katsuhiko Shibuya, Tadashi Ishikawa
-
Publication number: 20140088074Abstract: 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: ApplicationFiled: May 29, 2012Publication date: March 27, 2014Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventor: Paolo Pevarello
-
Publication number: 20140051758Abstract: 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: ApplicationFiled: August 7, 2013Publication date: February 20, 2014Applicant: Newron Pharmaceuticals S.p.A.Inventors: Elena BARBANTI, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
-
Publication number: 20140018549Abstract: 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: ApplicationFiled: April 25, 2013Publication date: January 16, 2014Applicant: NPS Pharmaceuticals, Inc.Inventor: NPS Pharmaceuticals, Inc.
-
Publication number: 20130303568Abstract: 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: ApplicationFiled: April 22, 2013Publication date: November 14, 2013Inventors: Nancy C. LAN, Yan Wang, Sui Xiong Cai
-
Publication number: 20130289122Abstract: 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: ApplicationFiled: March 11, 2013Publication date: October 31, 2013Inventor: Newron Pharmaceuticals S.P.A.
-
Publication number: 20130289275Abstract: 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: ApplicationFiled: June 12, 2013Publication date: October 31, 2013Inventors: Lingappa BALAYA, Mahalinga MANJATHURU, Yogeesh DERAMBALA, Pejakala Kakrannaya VASUDEVA, Thangavel ARULMOLI
-
Publication number: 20130244995Abstract: 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: ApplicationFiled: November 21, 2011Publication date: September 19, 2013Applicant: LEO PHARMA A/SInventors: Per Vedsø, Lars Kristian Albert Blæhr
-
Patent number: 8530701Abstract: 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: GrantFiled: December 1, 2008Date of Patent: September 10, 2013Assignee: Newron Pharmaceuticals, S.p.A.Inventors: Elena Barbanti, Laura Faravelli, Patricia Salvati, Renato Canevotti, Francesco Ponzini
-
Patent number: 8519000Abstract: 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: GrantFiled: May 14, 2008Date of Patent: August 27, 2013Assignee: Newron Pharmaceuticals S.p.A.Inventors: Piero Melloni, Alessandra Restivo, Emanuela Izzo, Simona Francisconi, Elena Colombo, Cibele Sabido-David
-
Patent number: 8518995Abstract: 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: GrantFiled: April 4, 2011Date of Patent: August 27, 2013Assignee: MediciNova, Inc.Inventors: Kazuko Matsuda, Yuichi Iwaki, Kale Ruby
-
Publication number: 20130121919Abstract: 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: ApplicationFiled: June 11, 2012Publication date: May 16, 2013Applicant: The Trustees of Columbia University in the City of New YorkInventors: Yan FENG, Mauro Fa, Ottavio Arancio, Shi Xian Deng, Donald W. Landry, Yitshak Francis
-
Patent number: 8378142Abstract: 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: GrantFiled: June 7, 2011Date of Patent: February 19, 2013Assignee: Ranbaxy Laboratories LimitedInventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
-
Patent number: 8278485Abstract: 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: GrantFiled: November 3, 2011Date of Patent: October 2, 2012Assignee: Newron Pharmaceuticals S.p.A.Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
-
Publication number: 20120238653Abstract: A latent curing agent obtained by the reaction of a coumarin compound with an amine.Type: ApplicationFiled: April 9, 2012Publication date: September 20, 2012Applicant: Henkel AG & Co. KGaaInventors: Masashi Horikiri, Atsushi Sudo, Takeshi Endo
-
Publication number: 20120214852Abstract: 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: ApplicationFiled: November 8, 2011Publication date: August 23, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Thomas Little, Anna Gall, Feng Hong
-
Publication number: 20120190012Abstract: The invention provides compositions and methods useful in DNA sequencing. In exemplary embodiments, a detectable label such as a luminescent macrocycle is used.Type: ApplicationFiled: April 6, 2011Publication date: July 26, 2012Applicant: LUMIPHORE, INC.Inventors: Nathaniel G. BUTLIN, Ga-Lai LAW, Christopher ANDOLINA
-
Publication number: 20120157712Abstract: 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: ApplicationFiled: November 3, 2011Publication date: June 21, 2012Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventors: ELENA BARBANTI, CARLA CACCIA, PATRICIA SALVATI, FRANCESCO VELARDI, TIZIANO RUFFILLI, LUIGI BOGOGNA
-
Patent number: 8143448Abstract: 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: GrantFiled: June 12, 2009Date of Patent: March 27, 2012Assignee: ViroBay, Inc.Inventor: Jeffrey Dener
-
Publication number: 20120071654Abstract: 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: ApplicationFiled: June 28, 2011Publication date: March 22, 2012Applicant: THERAVANCE, INC.Inventors: Robert M. McKinnell, John R. Jacobsen, Sean G. Trapp, Daisuke R. Saito
-
Publication number: 20120053346Abstract: 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: ApplicationFiled: August 30, 2011Publication date: March 1, 2012Inventor: Hubert Maehr
-
Publication number: 20120046293Abstract: The present invention relates to renin inhibitor compounds having the structure and their use in treating cardiovascular events and renal insufficiency.Type: ApplicationFiled: October 10, 2011Publication date: February 23, 2012Applicant: 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: 20120041038Abstract: 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: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
-
Publication number: 20120041039Abstract: 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: ApplicationFiled: October 21, 2011Publication date: February 16, 2012Applicant: Acucela Inc.Inventors: Ian L. Scott, Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Thomas L. Little, JR., Ryo Kubota
-
Publication number: 20120027844Abstract: 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: ApplicationFiled: February 9, 2010Publication date: February 2, 2012Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITYInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
-
Publication number: 20120022086Abstract: 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: ApplicationFiled: March 17, 2010Publication date: January 26, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
-
Patent number: 8093426Abstract: 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: GrantFiled: December 3, 2008Date of Patent: January 10, 2012Assignee: Ranbaxy Laboratories LimitedInventors: Mukesh Kumar Madhra, Pankaj Kumar Singh, Chandra Has Khanduri
-
Publication number: 20120004452Abstract: 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: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Inventors: Mukesh Kumar MADHRA, Pankaj Kumar Singh, Chandra Has Khanduri
-
Publication number: 20120004462Abstract: 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: ApplicationFiled: June 7, 2011Publication date: January 5, 2012Applicant: RANBAXY LABORATORIES LIMITEDInventors: Mukesh Kumar MADHRA, Pankaj Kumar Singh, Chandra Has Khanduri
-
Publication number: 20110312875Abstract: 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: ApplicationFiled: August 2, 2011Publication date: December 22, 2011Applicant: UNIVERSITY OF WOLLONGONGInventors: 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: 8076515Abstract: 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: GrantFiled: December 18, 2008Date of Patent: December 13, 2011Assignee: Newron Pharmaceuticals S.p.A.Inventors: Elena Barbanti, Carla Caccia, Patricia Salvati, Francesco Velardi, Tiziano Ruffilli, Luigi Bogogna
-
Patent number: 8076514Abstract: 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: GrantFiled: July 14, 2006Date of Patent: December 13, 2011Assignee: Eli Lilly and CompanyInventors: Larry Chris Blaszczak, Shon Roland Pulley, Michael Alan Robertson, Scott Martin Sheehan, Qing Shi, Brian Morgan Watson, Michael Robert Wiley