Hydroxy, Bonded Directly To Carbon, Or Ether Containing (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/158)
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Publication number: 20140011882Abstract: Disclosed are 5-nitrobenzoate derivatives of Formula I, and the preparation method therefor, wherein R is referred to hydrogen (H), unsubstituted, mono-substituted, di-substituted or tri-substituted benzoyl moiety. 5-Nitrobenzoate derivatives of Formula I do not affect the platelet aggregation, possesses the inhibitory activity related to the tumor cell-induced platelet aggregation (TCIPA), and further specifically inhibits podoplanin-induced platelet aggregation. Therefore, 5-nitrobenzoates of the invention are applicable in its therapeutic use as the novel therapeutic agent in preventing tumor metastasis.Type: ApplicationFiled: November 28, 2012Publication date: January 9, 2014Applicant: CHANG GUNG UNIVERSITYInventors: CHING-PING TSENG, PEI-WEN HSIEH, YAO-WEN CHANG
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Patent number: 8598386Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.Type: GrantFiled: October 17, 2011Date of Patent: December 3, 2013Assignee: Euticals GmbHInventors: Richard Wisdom, Joerg Jung, Andreas Meudt
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Publication number: 20130245064Abstract: The invention relates to novel acylamino-hydroxy-benzamides of formula (I), wherein R1 is phenyl substituted by phenyl, phenoxy, phenylamino or heteroaryl, all optionally further substituted; bicyclic aryl, monocyclic heteroaryl substituted by optionally substituted phenyl, or bicyclic heteroaryl, R2 is hydrogen or methyl, and R3 and R4 have the meanings indicated in the description. These compounds are useful for the treatment and/or prophylaxis of skeletal muscle atrophy, schizophrenia and Alzheimer's disease, and as cognitive enhancers.Type: ApplicationFiled: October 31, 2011Publication date: September 19, 2013Inventors: Shaheen Ahmed, Stefan Hettwer, Jan Willem Vrijbloed, Carlo Farina, Piero Paravidino
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Publication number: 20130231385Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have anticancer activity. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: ApplicationFiled: May 27, 2011Publication date: September 5, 2013Applicant: The Board of Regents of the University of Texas SystemsInventors: Jung-Mo Ahn, Ganesh Raj
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Publication number: 20130225686Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.Type: ApplicationFiled: April 12, 2013Publication date: August 29, 2013Applicant: Medichem, S.A.Inventor: Medichem, S.A.
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Publication number: 20130211082Abstract: A method of producing 6-amino-cyclopenta[g]quinazolines, in enantiomerically enriched form, is provided. In particular, the method may be applicable to the synthesis of N-{N-{4-[N-((6S)-2-hydroxymethyl-4-oxo-3,4,7,8-tetrahydro-6H-cyclo-penta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino]benzoyl}-L-?-glutamyl}-D-glutamic acid (ONX-0801).Type: ApplicationFiled: July 15, 2011Publication date: August 15, 2013Applicant: ONYX Pharmaceuticals, Inc.Inventors: James Alan Kerschen, Alexander James Bridges, Sean Mark Daizlel, Olivier Dapremont, Hyunjung Kim, Andrew S. Thompson, James Robert Zeller
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Publication number: 20130204042Abstract: 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: ApplicationFiled: January 31, 2011Publication date: August 8, 2013Applicant: RANBAXY LABORATORIES LIMITEDInventors: Hari Mohan Sriram, Mukesh Kumar Madhra, Mukesh Kumar Sharma
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Patent number: 8497397Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: GrantFiled: February 24, 2012Date of Patent: July 30, 2013Assignee: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
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Publication number: 20130190533Abstract: The present invention relates to a process of manufacture of compounds of formula (B) wherein R1, R2 and R3 are as defined for compounds of formula (A), which process comprises hydrogenation of compounds of general formula (A). In particular, the present invention relates to an improved process for the manufacture of Lacosamide (LCM), (R)-2-acetamido-N-benzyl-3-methoxypropion-amide (B1), which is useful as an anticonvulsive drug.Type: ApplicationFiled: September 29, 2011Publication date: July 25, 2013Applicant: UCB PHARMA GMBHInventors: Alain Merschaert, Didier Bouvy, David Vasselin, Nicolas Carly
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Publication number: 20130184222Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1 comprising administering to a subject in need thereof a compound described here.Type: ApplicationFiled: July 15, 2011Publication date: July 18, 2013Applicant: AGIOS PHARMACEUTICALS, INCInventors: Janeta Popovici-Muller, Francesco G. Salituro, Jeffrey Saunders, Jeremy Travins, Shunqi Yan
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Publication number: 20130184343Abstract: A compound of formula (I): wherein A1, A2, A3, A4, R1, R2, G1, G2, Q1 and Q2 are as defined in claim 1; or salts or N-oxides thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, molluscicidal and nematicidal compositions comprising them and to methods of using them to combat and control insect, acarine, mollusc and nematode pests.Type: ApplicationFiled: March 4, 2013Publication date: July 18, 2013Applicants: Syngenta Crop Protection LLC, Syngenta Participations AGInventor: Syngenta Participations AG
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Publication number: 20130172388Abstract: Cannabionid receptor-2 inverse antagonists include compounds represented by Formula IV, or a pharmaceutically acceptable salt thereof: wherein: R1 and R2 are independently H, alkyl, or alkenyl; R3 is alkyl, alkenyl, aryl, aralkyl, aralkenyl, heterocyclyl, heterocyclylalkyl, heteroaryl, heteroarylalkyl; R4 and R5 are independently a bond, alkylenyl, or alkenylenyl; each R6 and R7 is independently selected from the group consisting of OH, F, Cl, Br, I, (C1-C6)alkyl, alkoxy, amino, COOH, CONH2, SO3H, PO3H2, CN, SH, NO2 and CF3; and p and q are independently 0, 1, 2, 3, 4, or 5. Such compounds may be used to treat osteoporosis or multiple myeloma.Type: ApplicationFiled: December 14, 2012Publication date: July 4, 2013Applicant: University of Pittsburgh -- Of the Commonwealth System of Higher EducationInventor: University of Pittsburgh -- Of the Commonwealth System of Higher Education
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Publication number: 20130165443Abstract: Compounds of the formula I: or a pharmaceutically acceptable salt thereof, wherein, R1 is optionally substituted phenyl or optionally substituted pyridinyl, and R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. Also disclosed are methods of using the compounds for treating diseases associated with P2X3 and/or a P2X2/3 receptor antagonists and methods of making the compounds.Type: ApplicationFiled: August 23, 2012Publication date: June 27, 2013Inventors: Chris Allen Broka, Ronald Charles Hawley
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Publication number: 20130164228Abstract: Described herein are compositions for topical use comprising an antibacterially effective concentration of a gallate or gallamide compound which is a polysubstituted cycloalkyl or heterocycloalkyl wherein the substituents are selected from hydroxy, hydroxymethyl, fluoro, chloro, amino, nitro, or a moiety of formula -X-(CO)-(3,4,5-trihydroxyphenyl), wherein X is selected from O and NH, provided that the substituents comprise at least two moieties of formula -X-(CO)-(3,4,5-trihydroxyphenyl) attached to adjacent carbons in free or in orally or topically acceptable salt form, as well as methods of making and using the same.Type: ApplicationFiled: December 21, 2011Publication date: June 27, 2013Applicant: Colgate-Palmolive CompanyInventors: Stanislav Jaracz, Guofeng Xu, Steven Miller, Leonora Leigh, Guillaume Picquet, Laurence Du-Thumm
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Publication number: 20130150442Abstract: The present invention includes bis- and tris-benzamide compounds that block AR signaling and have activity against prostate cancer. Uses for these compounds, and pharmaceutical compositions containing the same, also are provided.Type: ApplicationFiled: November 21, 2012Publication date: June 13, 2013Applicant: The Board of Regents of the University of Texas SystemInventor: The Board of Regents of the University of Texas S
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Patent number: 8455688Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.Type: GrantFiled: March 21, 2012Date of Patent: June 4, 2013Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Publication number: 20130123537Abstract: The present invention relates to an improved process for the preparation of Lacosamide of Formula (I), comprising: O-methylating a compound of Formula (V) or a compound of Formula (XX) or a compound of Formula XXII; in the presence of a methylating agent and a base to produce Lacosamide of Formula (I).Type: ApplicationFiled: May 16, 2011Publication date: May 16, 2013Inventors: K a s s Narayan Garimella, Subba Reddy Danda, Shankar Reddy Budidet, Srinivasachary Katuroju, Gowrisankar Rao Kaki, Srinivasa Rao Yatcherla, Islam Aminul, Sivakumaran Meenakshisunderam
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Publication number: 20130123522Abstract: The present invention discloses novel process for the preparation of (2R)-2-acetamido-N-benzyl-3-methoxypropanamide of Formula I involving novel intermediates of Formula-XIX and Formula-XX.Type: ApplicationFiled: July 26, 2011Publication date: May 16, 2013Inventors: Mangesh Narayan Rajadhyaksha, Ranjeet Nair, Nilesh Balkrishna Shrigadi, Aditi Milind Panandikar
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Patent number: 8440861Abstract: The invention relates to solid forms of the anti-epileptic agent lacosamide (I). The invention also relates to mixtures of solid forms of lacosamide. The invention further relates to mixtures of lacosamide enantiomers crystallized in a conglomerate Form and the use thereof in providing enantiomerically enriched lacosamide, preferably lacosamide enriched with the (R)-enantiomer of lacosamide.Type: GrantFiled: August 5, 2010Date of Patent: May 14, 2013Assignee: Medichem, S.A.Inventors: Ernesto Duran Lopez, Monica Benito Velez, Jordi Bosch i Lladó
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Patent number: 8440716Abstract: The present invention provides novel compounds of formula (I) and pharmaceutical compositions thereof. The inventive compounds are useful as deacetylase inhibitors (e.g., histone deacetylase inhibitors) and may be useful in the treatment of proliferative diseases such as cancer. In particular, the inventive compounds are HDAC6 inhibitors. The invention also provide synthetic methods for preparing the inventive compounds.Type: GrantFiled: July 22, 2009Date of Patent: May 14, 2013Assignees: President and Fellows of Harvard College, Dana-Farber Cancer Institute, Inc.Inventors: Weiping Tang, James Elliot Bradner, Stuart L. Schreiber
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Publication number: 20130109880Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.Type: ApplicationFiled: November 12, 2012Publication date: May 2, 2013Applicant: Obschestvo S Ogranichennoi Otvetstvennostiyu PharmenterprisesInventor: Obschestvo S Ogranichennoi Otvetstvennostiyu
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Publication number: 20130102811Abstract: The present invention relates to a novel and improved process for the preparation of lacosamide, wherein the process is a sequential one-pot process.Type: ApplicationFiled: July 1, 2011Publication date: April 25, 2013Applicant: SUN PHARMACEUTICAL INDUSTRIES LTDInventors: Maheshbhai Mehulkumar Patel, Vishal Diliprao Mohite, Sudhakar Khambampati, Rao Trinadha Chitturi, Rajamannar Thennati
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Publication number: 20130071328Abstract: This invention discloses a series of novel propynoic acid carbamoyl methyl-amides (PACMAs), methods for synthesizing the PACMAs and pharmaceutical compositions containing the PACMAs. These novel compounds and compositions show cytotoxicity in cancer cells and are useful as lead compounds for anti-cancer drugs or pharmaceutical agents. This invention also discloses treatment methods that uses the PACMAs and pharmaceutical compositions as well as methods for promoting the release and nuclear localization of the transcription factor Nrf2.Type: ApplicationFiled: March 22, 2012Publication date: March 21, 2013Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Nouri NEAMATI, Nicos A. PETASIS, Roppei YAMADA
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Publication number: 20130041180Abstract: Processes for preparing and purifying (R)-2-acetamido-N-benzyl-3-methoxy-propionamide of formula-1 and intermediates thereof are provided.Type: ApplicationFiled: February 9, 2011Publication date: February 14, 2013Inventors: Manne Satyanarayana Reddy, Sajja Eswaraiah, Aluru Srinivas, Revu Satyanarayana
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Publication number: 20130035317Abstract: The invention relates to the use of di-aspirin (bis(2-carboxyphenyl)succinate) and its derivatives in the treatment of colon and colorectal cancer. It also relates to novel derivatives of di-aspirin and to a method of synthesis of the di-aspirin and its derivatives.Type: ApplicationFiled: February 15, 2011Publication date: February 7, 2013Inventors: Christopher John Perry, Iain Douglas Nicholl
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Publication number: 20130035508Abstract: Present invention relates to an improved and commercial process for the preparation of lacosamide ((R)-2-acetami-do-N-benzyl-3-methoxypropanamide) of formula (I). Present process utilizes high purity crystalline solids of formulae (XXXII) and (XIII) as key intermediates. Lacosamide is indicated for the adjunctive treatment of partial onset seizures in patients aged at least 17 years.Type: ApplicationFiled: February 4, 2011Publication date: February 7, 2013Applicant: Natco Pharma LimitedInventors: Pulla Reddy Muddasani, Veerababu Madalapu, Venkaiah Chowdary Nannapaneni
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Publication number: 20130030216Abstract: A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.Type: ApplicationFiled: December 22, 2010Publication date: January 31, 2013Applicant: EUTICALS S.P.A.Inventors: Alberto Bologna, Patrizia Castoldi, Domenico Vergani, Giorgio Bertolini
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Patent number: 8329745Abstract: Ghrelin O-acyltransferase (GOAT) is inhibited with designed small molecules of the general formula: Methods comprise contacting the GOAT with an inhibitor and detecting a resultant inhibition.Type: GrantFiled: September 6, 2011Date of Patent: December 11, 2012Assignee: Board of Regents, The University of Texas SystemInventors: Patrcik G. Harran, Michael S. Brown, Joseph L. Goldstein, Jing Yang, Tong-Jin Zhao
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Publication number: 20120308481Abstract: Radio-opaque biodegradable compositions are formed by modifying terminal groups of synthetic and natural biodegradable polymers such as polylactones with iodinated moieties. The biodegradable property of the compositions renders them suitable for use in medical field such as drug delivery, imaging. Compounds disclosed in this invention exist as neat liquid. Certain compositions disclosed in this invention form hydrophobic iodine rich domains when dissolved in water, such domains provide better contrasting properties as well as ability to dissolve hydrophobic bioactive drugs. Certain iodinated moieties disclosed in the invention are capable of cross linking natural proteins in situ in presence of suitable catalysts and co-catalysts.Type: ApplicationFiled: August 16, 2012Publication date: December 6, 2012Applicant: PATHAK HOLDINGS LLCInventors: Chandrashekhar P. Pathak, Sanjay M. Thigle
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Publication number: 20120309812Abstract: The present invention relates to certain bisamide derivatives of formula (I), to processes and intermediates for preparing them, to insecticidal, acaricidal, nematicidal or molluscicidal compositions comprising them and to methods of using them to combat and control insect, acarine, nematode or mollusc pests compounds.Type: ApplicationFiled: February 1, 2011Publication date: December 6, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Pierre Joseph Marcel Jung, Christopher Richard Ayles Godfrey, Ottmar Franz Hueter, Peter Renold
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Publication number: 20120295907Abstract: The present invention relates to bis-amide derivatives of formula (I), to processes and intermediates for preparing them, to methods of using them to control insect, acarine, nematode and mollusc pests, and to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising them.Type: ApplicationFiled: April 14, 2010Publication date: November 22, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Maienfisch, Christopher Richard Ayles Godfrey, Pierre Joseph Marcel Jung, Ottmar Franz Hueter, Peter Renold
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Patent number: 8309766Abstract: The present invention relates to novel phenyl-N-acyl derivatives of biogenic amines and amino acids of general formula (I) as cyclooxynease inhibitors, possessing analgetic and anti-inflammatory properties and devoid of side effects in particular ulcerogeneity and pro-spasmodic actions, as well as capability to potentiate effect of other analgetics, and possessing in addition antihypoxic, antidepressant and anti-Parkinsonistic action; as well as to the processes for the preparation novel and known phenyl-N-acyl derivatives of biogenic amines, to a pharmaceutical composition and to an agent comprising compounds of general formula (I) as well as to use thereof and a method of treating.Type: GrantFiled: March 24, 2006Date of Patent: November 13, 2012Assignee: Obschestvo S. Organichennoi Otvetstvennostiyu PharmenterprisesInventors: Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova, Galina Alexandrovna Zheltukhina, Violetta Leonidovna Kovaleva
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Publication number: 20120283466Abstract: A new compound is provided, which is used for preparing lacosamide. A novel method for preparing lacosamide is also provided. During the reaction, iodomethane and silver oxide that are cost expensive are not used, nor a Pd-c catalyst is used, so the production cost is low, the raw materials and accessory materials are cheap and easily available, and the process is simple, so that industrial production is easy to realize; and moreover, the yield is high, and good economic efficiency can be achieved.Type: ApplicationFiled: June 29, 2012Publication date: November 8, 2012Applicant: ZHEJIANG JIUZHOU PHARMACEUTICAL CO., LTD.Inventors: Xianyi ZHANG, Shaoqing GE, Daqing CHE
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Publication number: 20120272462Abstract: The present invention relates to a compound of formula (I), where X, Y, T and Z are each as defined in claim 1, to its preparation and to its use.Type: ApplicationFiled: January 17, 2012Publication date: November 1, 2012Applicant: DyStar Colours Deutschland GmbHInventors: Roxana Barbieru, Carsten Harfmann, Werner Russ
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Patent number: 8268885Abstract: The present invention relates to small molecules as entry inhibitors of the HIV virus, processes for their preparation as well as pharmaceutical compositions, their use as medicines, and diagnostic kits comprising them. The present invention also concerns combinations of the present entry inhibitors with other anti-retroviral agents. It further relates to their use in assays as reference compounds or as reagents. The compounds of the present invention are useful for preventing or treating infection by HIV and for treating AIDS.Type: GrantFiled: September 10, 2004Date of Patent: September 18, 2012Assignee: Janssen R&D IrelandInventors: Koenraad Lodewijk August Van Acker, Piet Tom Bert Paul Wigerinck, Lieve Emma Jan Michiels, Abdellah Tahri
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Publication number: 20120232015Abstract: A first aspect of the invention is a compound (sometimes also referred to herein as an “active agent” or “active compound”) of Formula Ia, or more particularly Formula Ib, or a pharmaceutically acceptable salt or prodrug thereof. Compositions thereof and methods of using the same (e.g. for the treatment of a neurological disease) are also described.Type: ApplicationFiled: September 17, 2010Publication date: September 13, 2012Inventors: Harold L. Kohn, Christophe Salomé, Elise Salomé-Grosjean
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Publication number: 20120225912Abstract: The invention relates to colchicine derivatives, methods and uses thereof for treatment of cancer.Type: ApplicationFiled: July 30, 2010Publication date: September 6, 2012Inventors: Jack Tuszynski, Jonathan Y. Mane, John Torin Huzil, Boguslaw Tomanek, Dorota Bartusik
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Publication number: 20120220593Abstract: A pharmaceutical composition comprising a compound having Formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein, R1 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; R2 is, for example, a C6-C10 aryl group which may be substituted with one group or more than one group selected from substituent group ?; and X is, for example, a hydroxyl group or a C1-C6 alkoxy group].Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: Daiichi Sankyo Company, LimitedInventors: Kazumasa Aoki, Koji Suda, Toshio Kaneko, Tomio Kimura
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Publication number: 20120209022Abstract: The invention relates to improved processes for the preparation of lacosamide. The invention also relates to a novel intermediate useful in the preparation of lacosamide. The invention also relates to process for the purification of lacosamide.Type: ApplicationFiled: September 23, 2010Publication date: August 16, 2012Applicant: CADILA HEALTHCARE LIMITEDInventors: Bipin Pandey, Kalpesh Shah
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Patent number: 8227643Abstract: This invention relates to bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable salts and their use in the modulation of Sirtuin 1 (Sirt1) and there use in neuroprotection for subject suffering from neurodegenerative diseases such as Alzheimer's disease, Huntington's disease, Amyotrophic lateral sclerosis, frontotemporal dementia, Parkinson's disease, including Parkinson's plus diseases such as multiple system atrophy, progressive supranuclear palsy, corticobasal degeneration and dementia with Lewy bodies, and in the manufacture of medicaments for such Sirt1 modulation and neuroprotection.Type: GrantFiled: January 12, 2010Date of Patent: July 24, 2012Assignee: ProteoTech, Inc.Inventors: Alan D. Snow, Qubai Hu, Judy A. Cam
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Publication number: 20120183468Abstract: Provided herein are water-soluble, functionalized fullerenes, and processes for producing water-soluble, functionalized fullerenes. The process includes sulfonating a fullerene in an acidic solution comprising sulfuric acid to produce a sulfonated fullerene, isolating the sulfonated fullerene from the acidic solution without neutralizing the acidic solution, reacting the sulfonated fullerene with hydrogen peroxide to form a reaction product, and isolating a polyhydroxylated fullerene from the reaction product produced from reacting the sulfonated fullerene with the hydrogen peroxide. The process of producing water-soluble fullerenes further includes functionalizing a polyhydroxylated fullerene with one or more pendant functional groups by reacting the polyhydroxylated fullerene with one or more functional group precursors.Type: ApplicationFiled: January 17, 2012Publication date: July 19, 2012Applicant: MARELLE, LLCInventors: Mark Farrell, Michelle Guaragno
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Publication number: 20120178783Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N; wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15, wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Inventors: John S. Kovach, Francis Johnson
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Publication number: 20120178747Abstract: The mechanism by which the high bone mass (HBM) mutation (G171V) of the Wnt coreceptor LRP5 regulates the canonical Wnt signaling was investigated. The mutation was previously shown to reduce Dkk protein-1-mediated antagonism, suggesting that the first YWTD repeat domain where G171 is located may be responsible for Dkk protein-mediated antagonism. However, we found that the third YWTD repeat, but not the first repeat domain, is required for DKK1-mediated antagonism. Instead, we found that the G171V mutation disrupted the interaction of LRP5 with Mesd, a chaperon protein for LRP5/6 that is required for the coreceptors' transport to cell surfaces, resulting in less LRP5 molecules on the cell surface. Although the reduction in the level of cell surface LRP5 molecules led to a reduction in Wnt signaling in a paracrine paradigm, the mutation did not appear to affect the activity of coexpressed Wnt in an autocrine paradigm.Type: ApplicationFiled: November 14, 2006Publication date: July 12, 2012Inventors: Dianqing (Dan) Wu, Dakai Liu, James J. Donegan
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Patent number: 8217076Abstract: Analogs of largazole are described herein. Methods of treating cancer and blood disorders using largazole and largazole analogs and pharmaceutical compositions comprising the same are additionally described herein. Methods for preparing largazole analogs are likewise described.Type: GrantFiled: July 16, 2009Date of Patent: July 10, 2012Assignees: Colorado State University Research Foundation, Dana-Farber Cancer InstituteInventors: Robert M. Williams, James E. Bradner, Albert Bowers, Tenaya Newkirk
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Publication number: 20120149737Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-amido-aryl compounds of the following formula (for convenience, collectively referred to herein as “AAA compounds”), which, inter alia, are (selective) retinoic acid receptor ? (RAR?) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RAR?, and in the treatment of diseases and conditions that are mediated by RAR?, that are ameliorated by the activation of RAR?, etc., including cognitive disorders, memory impairment, memory deficit, senile dementia, Alzheimer's disease, early stage Alzheimer's disease, intermediate stage Alzheimer's disease, late stage Alzheimer's disease, cognitive impairment, and mild cognitive impairment.Type: ApplicationFiled: September 1, 2010Publication date: June 14, 2012Applicant: KING'S COLLEGE LONDONInventors: Jonathan Patrick Thomas Corcoran, Sarkis Barret Kalindjian, Alan David Borthwick, David Reginald Adams, Jane Theresa Brown, David Michel Adrien Taddei, Jason John Shiers
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Publication number: 20120121536Abstract: Glucose deprivation is an attractive strategy in cancer research and treatment. Cancer cells upregulate glucose uptake and metabolism for maintaining accelerated growth and proliferation rates. Specifically blocking these processes is likely to provide new insights to the role of glucose transport and metabolism in tumorigenesis, as well as in apoptosis. As solid tumors outgrow the surrounding vasculature, they encounter microenvironments with a limited supply of nutrients leading to a glucose deprived environment in some regions of the tumor. Cancer cells living in the glucose deprived environment undergo changes to prevent glucose deprivation-induced apoptosis. Knowing how cancer cells evade apoptosis induction is also likely to yield valuable information and knowledge of how to overcome the resistance to apoptosis induction in cancer cells.Type: ApplicationFiled: March 24, 2011Publication date: May 17, 2012Applicant: OHIO UNIVERSITYInventors: Xiaozhuo Chen, Stephen Bergmeier
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Patent number: 8178577Abstract: The present invention relates to certain tricyclic derivatives which are capable of inhibiting histone deacetylases. The compounds of this invention are therefore useful in treating diseases associated with abnormal histone deacetylase activities. Pharmaceutical compositions comprising these compounds, methods of treating diseases utilizing pharmaceutical compositions comprising these compounds, and methods of preparing these compounds are also disclosed.Type: GrantFiled: May 8, 2009Date of Patent: May 15, 2012Assignee: Shenzhen Chipscreen Biosciences Ltd.Inventors: Xian-Ping Lu, Zhi-Bin Li, Zhi-Qiang Ning
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Publication number: 20120095251Abstract: The present invention relates to a method for producing (R)-2-acetamido-N-benzyl-3-methoxypropionamide (lacosamide), by methylation of (R)-2-acetamino-2-N-benzyl-3-hydroxy-propionamide (V), in which the methylation is carried out at a temperature below 20° C.Type: ApplicationFiled: October 17, 2011Publication date: April 19, 2012Inventors: Richard WISDOM, Joerg JUNG, Andreas MEUDT
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Patent number: 8158827Abstract: Disclosed are cationic lipid compounds and compositions of lipid aggregates for delivery of macromolecules and other compounds into cells. The compounds can be used alone or in combination with other compounds to prepare liposomes and other lipid aggregates suitable for transfection or delivery of compounds to target cells, either in vitro or in vivo. The compounds are preferably polycationic and preferably form highly stable complexes with various anionic macromolecules, particularly polyanions such as nucleic acids. These compounds have the property, when dispersed in water, of forming lipid aggregates which associate strongly, via their cationic portion, with polyanions. Also disclosed are intermediates for preparing the compound and compositions of the invention and methods of using the compounds to introduce other compounds into cells.Type: GrantFiled: January 14, 2009Date of Patent: April 17, 2012Assignee: Life Technologies CorporationInventors: Yongliang Chu, Malek Masoud, Gulilat Gebeyehu
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Patent number: 8143445Abstract: This invention provides the compound having the structure wherein n is 1-10; X is C—R11 or N, wherein R11 is H, OH, SH, F, Cl, SO2R7, NO2, trifluoromethyl, methoxy, or CO—R7, wherein R7 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl; Z is R2 is H or NR3R4, wherein R3 and R4 are each independently H, C1-C6 alkyl, or C3-C8 cycloalkyl; R5 is OH or SH; and R6, R12, R13, and R14 are each independently H, OH, SH, F, Cl, SO2R15, NO2, trifluoromethyl, methoxy, or CO—R15 wherein R15 is alkyl, alkenyl, alkynyl, C3-C8 cycloalkyl, or aryl, or a salt of the compound, which is useful in the treatment of tumors.Type: GrantFiled: October 1, 2008Date of Patent: March 27, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson