Nitrogen In Alcohol Moiety Other Than As Nitro, Nitroso Or Isocyanate Patents (Class 560/250)
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Patent number: 10039726Abstract: Disclosed herein are compounds and compositions thereof which find use in increasing stability of TTR tetramers reducing its tendency to misfold and form aggregates. Also provided herein are methods for using these compounds and compositions for increasing stability of TTR and therby decreasing aggegate formation by TTR. Also disclosed herein are methods to screen for candidate compounds that increase stability of TTR. Also disclosed herein are heterobifunctional compounds that include a TTR binding compound connected to a targeting moiety via a linker, for use in disrupting PP is of a target protein.Type: GrantFiled: April 6, 2016Date of Patent: August 7, 2018Assignee: The Board of Trustees of the Leland Stanford Junior UniversityInventors: Isabella A. Graef, Mamoun M. Alhamadsheh
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Patent number: 9233914Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.Type: GrantFiled: February 25, 2015Date of Patent: January 12, 2016Assignees: CYMABAY THERAPEUTICS, INC., DIATEX, INC.Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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Publication number: 20150094485Abstract: 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, can be produced by treating a compound of formula (II) with a chiral alcohol to yield the diastereomeric esters of formula (IV) and (IV?), which can be further transformed into a compound of formula (I), or an enantiomer, solvate or salt thereof, wherein R1 is C1-C8 alkyl; and R2 and R3, independently of one another, represent H or C1-C6 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound.Type: ApplicationFiled: April 26, 2013Publication date: April 2, 2015Inventors: Antonio Lorente Bonde-Larsen, Francisco Javier Gallo Nieto, Juan José Ferreiro Gil, Pablo Martín Pascual
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Patent number: 8993797Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.Type: GrantFiled: July 10, 2013Date of Patent: March 31, 2015Assignee: Cymabay Therapeutics, Inc.Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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Patent number: 8871977Abstract: Disclosed are a novel asymmetric azine compound (I) and a method for producing an asymmetric azine compound (I) which is characterized in that an aldehyde compound (III) and hydrazine are reacted in an alcohol solvent at a molar ratio (aldehyde compound (III)):(hydrazine) of from 2:1 to 1:2, thereby obtaining a reaction solution including a hydrazone compound (IV), and then an aldehyde compound (V) is added for a reaction into the thus-obtained reaction solution at a molar ratio (aldehyde compound (V)):(hydrazone compound (IV)) of from 2:1 to 1:2. The method can commercially advantageously produce an asymmetric azine compound having a polar group such as a hydroxyl group or a carboxyl group in each molecule. The novel asymmetric azine compound can be obtained by this production method. (In the formulae, R1 and R2 each represents a hydroxyl group or a carboxyl group, X1 to X8 each represents a hydrogen atom, —C(?O)—OR3 or the like; and R3 represents an alkyl group having 1 to 10 carbon atoms or the like.Type: GrantFiled: June 17, 2009Date of Patent: October 28, 2014Assignee: Zeon CorporationInventors: Kei Sakamoto, Yasushi Nakano
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Publication number: 20140283199Abstract: Bio-regulators from a group of quaternary ammonium moieties modify a gene expression in undesirable plants to inhibit growth and robustness and enhance the effectiveness of herbicides. Such bio-regulator may be applied to plants through seed treatments, root drenching, spraying and dusting, or to soil were desirable crops are planted or will be planted. Bio-regulators may be duel-acting; causing beneficial modification to gene expressions in desirable plants while modifying gene expression in undesirable plants, making them more susceptible to herbicides. Bio-regulators are Ester Compounds, BMIA Compounds or related salts of those compounds.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Applicant: KamTecInventor: KamTec
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Publication number: 20140155648Abstract: A new compound, (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid, of formula II (S)-5-(2-acetoxypropanamido)-2,4,6-triiodoisophthalic acid. Said new compound is of use for the production of triiodinated contrast agent, especially lopamidol, with low content of acetyl and hydroxyacetyl analogs. The new compound may be formed from 5-amino-2,4,6-triiodoisophtalic acid by acylating with (S)-1-chloro-1-oxopropan-2-yl acetate. The new compound may then be converted to the respective acid dichloride by reacting with a chlorinating reagent, which is a further object of the present invention, followed by the amidation with 2-amino-1,3-propanediol and acetate hydrolysis.Type: ApplicationFiled: February 2, 2012Publication date: June 5, 2014Applicant: HOVIONE INTER LIMITEDInventors: Jose Manuel Galindro, Ana Cristina Cruz, João José Bandarra, William Heggie
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Patent number: 8668986Abstract: The present invention relates to aromatic aldimines, which are based on primary aromatic polyamines, which are solid at room temperature and liquid at room temperature and which have the lowest possible viscosity, hydrolyze with little odor, and can be used as blocked amines in curable compositions, in particular in compositions having one-component and two-component isocyanate groups. Said compositions have a relatively long open time, but cure surprisingly rapidly, said curing occurring without strong odor formation and without bubbling. In addition, the compositions have outstanding mechanical properties after curing, in particular high strength with high ductility, and good resistance to heat and moisture.Type: GrantFiled: November 13, 2008Date of Patent: March 11, 2014Assignee: Sika Technology AGInventor: Urs Burckhardt
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Publication number: 20140066500Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Applicant: Reviva Pharmaceuticals, Inc.Inventors: Laxminarayan BHAT, Seema BHAT
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Publication number: 20140051757Abstract: It is described the use of L-carnitine and/or one or more alkanoyl L-carnitines, or mixture thereof, or one of their pharmaceutically acceptable salts, for the preparation of a medicament or a nutritional supplement useful for preventing or treating the Leber optic neuropathy.Type: ApplicationFiled: September 9, 2011Publication date: February 20, 2014Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.Inventors: Silvia Cavazza, Martina Cavazza, Francesca Cavazza, Anna Atti, Enrico Cavazza
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Publication number: 20140038822Abstract: Use of substituted spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof for enhancement of stress tolerance in plants. The invention relates to the use of spirocyclic sulfonamidocarboxylic acids, -carboxylic esters, -carboxamides and -carbonitriles or salts thereof of the formula (I) in which the respective substituents have the meanings given in the description, for increasing stress tolerance in plants with respect to abiotic stress, and also for increasing plant growth and/or for increasing plant yield.Type: ApplicationFiled: December 27, 2011Publication date: February 6, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jens Frackenpohl, Lothar Willms, Thomas Müller, Stefan Lehr, Pascal Von Koskull-Döring, Ines Heinemann, Christopher Hugh Rosinger, Isolde Häuser-hahn, Martin Jeffrey Hills
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Patent number: 8618323Abstract: A composition comprising a polymer backbone and at least one side group, wherein the side group comprises a benzene ring-based chromophore comprising a ketone at the 1-position, a substituted or unsubstituted amino group at the 2-position, and an oxygen atom at the 3-position of the benzene ring. The chromophore is a kynurenine-based compound. Methods of making and using the composition are also provided. The composition can be used in an ophthalmic lens or device for protecting the retina by blocking UV rays and filtering violet rays.Type: GrantFiled: January 28, 2011Date of Patent: December 31, 2013Assignee: Benz Research and Development CorporationInventors: Patrick H. Benz, Jose A. Ors
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Patent number: 8604112Abstract: The invention relates to a composition containing a particulate solid, a plastic material (such as a thermoplastic polymer) and a compound capable of having dispersant properties. The compound may be obtained/obtainable by reacting a fatty acid with either (i) a hydroxy-C4-5-alkylene carboxylic acid, or (ii) a lactone. The invention further relates to novel compounds, and the use of the compound as a dispersant.Type: GrantFiled: August 13, 2009Date of Patent: December 10, 2013Assignee: The Lubrizol CorporationInventors: Patrick J. Sunderland, Dean Thetford, Thomas Forder
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Publication number: 20130261133Abstract: The compounds of the invention exhibit antiprotozoal, antimicrobial, and anticancer properties that are useful for the treatment or prevention of infections or cancer in a patient (e.g., a human). For example, the compounds and methods described herein can be used for the treatment or prevention of protozoal infections such as leishmaniasis, malaria, and trypanosoma infections, bacterial infections such as S. aureus and C. albicans, and cancers such as breast, colon, lung, or prostate cancer. The invention further provides methods of synthesizing such compounds as well as kits useful for administering the compounds.Type: ApplicationFiled: March 14, 2013Publication date: October 3, 2013Applicant: The University of MontanaInventors: John Howard Hoody, David Brian Bolstad
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Patent number: 8507719Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.Type: GrantFiled: May 11, 2012Date of Patent: August 13, 2013Assignees: Metabolex, Inc.Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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Patent number: 8476315Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.Type: GrantFiled: March 10, 2010Date of Patent: July 2, 2013Assignee: Onepharm Research & Development GmbHInventors: Paul Kosma, Ulrich Jordis, Dirk Classen-Houben, Bernhard Kueenburg, Christian Stanetty, Laszlo Czollner
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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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Patent number: 8344176Abstract: The present disclosure relates to a process for the preparation of 2-(3 -diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol or its phenolic monoesters or salts thereof, characterized by the steps of a) reacting a compound of formula (II) with a mixture of a Grignard initiator and Mg in a solvent; b) optionally reducing the temperature of the Grignard reagent to a lower temperature than in step a), and reacting the resulting Grignard reagent with an excess of a carbonate in a solvent, to obtain a compound of formula (III) wherein A is a C1-C6 alkyl, and the further reacting the compound of formula (III) in a known manner to obtain the desired end product.Type: GrantFiled: May 26, 2007Date of Patent: January 1, 2013Assignee: Schwarz Pharma Ltd.Inventors: Roisin Browne, Michael Kilkelly
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Publication number: 20120258063Abstract: An object is to provide an external preparation for skin preferably usable to prevent or ameliorate pigmentation. The object is achieved by providing a preventing or ameliorating agent for pigmentation, consisting of a compound represented by the following general formula (1), an isomer thereof, and/or a pharmacologically acceptable salt thereof, and an external preparation for skin containing the same as a component: [wherein R1 represents an unsubstituted aromatic group or an aromatic group having any substituent; R2 represents a hydrogen atom, a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4, or an acyl group having a linear or branched alkyl chain having a number of carbon atom or atoms of 1 to 4; and R3 represents a hydrogen atom or a linear chain or branched chain alkyl group having a number of carbon atom or atoms of 1 to 4.Type: ApplicationFiled: December 16, 2010Publication date: October 11, 2012Applicant: Pola Chemical Industries Inc.Inventors: Yuko Saitoh, Chihiro Kondo, Takashi Yamasaki
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Publication number: 20120220797Abstract: The invention relates to a process for obtaining 3,3-diphenylpropylamines of general formula (I), particularly Fesoterodine, as well as their enantiomers, solvates and salts, comprising a chemoselective reduction of the acid group against the ester group in compounds of general formula (V), wherein R1 is C1-C8 alkyl; and R3 and R4, independently of one another, represent H or C1-C8 alkyl, or together form a ring of 3 to 7 members with the nitrogen to which they are bound. The invention also relates to the compounds of formula (V), as well as their enantiomers, solvates and salts.Type: ApplicationFiled: July 26, 2010Publication date: August 30, 2012Inventors: Antonio Lorente Bonde-Larsen, Pablo Martín Pascual, Mario Laderas Muñoz, Luis Gerardo Gutiérrez Fuentes
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Publication number: 20120220784Abstract: The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding ?-acyloxy sulfides.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: ScinoPharm Singapore PTE, Ltd.Inventors: JyhHsiung Liao, LungHuang Kuo
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Publication number: 20120172426Abstract: The present invention provides novel cycloalkylmethylamine derivatives, and methods of preparing cycloalkylmethylamine derivatives. The present invention also provides methods of using cycloalkylmethylamine derivatives and compositions of cycloalkylmethylamine derivatives. The pharmaceutical compositions of the compounds of the present invention can be advantageously used for treating and/or preventing obesity and obesity related co-morbid indications and depression and depression related co-morbid indications.Type: ApplicationFiled: July 1, 2011Publication date: July 5, 2012Applicant: REVIVA PHARMACEUTICALS, INC.Inventors: Laxminarayan Bhat, Kouacou Adiey
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Patent number: 8202679Abstract: An oxime ester compound of formula (I) useful as a photopolymerization initiator. A photopolymerization initiator having the oxime ester compound as an active ingredient is activated through efficient absorption of light of long wavelength, e.g., 405 nm or 365 nm, to exhibit high sensitivity. In formula (I), R1 and R2 are each R11, OR11, COR11, SR11, CONR12R13, or CN; R11, R12, and R13 are each hydrogen, a C1-C20 alkyl group, C6-C30 aryl group, a C7-C30 arylalkyl group, or a C2-C20 heterocyclic group; R3 and R4 are each R11, OR11, SR11, COR11, CONR12R13, NR12COR11, OCOR11, COOR11, SCOR11, OCSR11, COSR11, CSOR11, CN, halogen, or a hydroxyl group; a and b is each 0 to 4; X is oxygen, sulfur, selenium, CR31R32, CO, NR33, or PR34; and R31, R32, R33, and R34 each have the same meaning as R1.Type: GrantFiled: December 25, 2007Date of Patent: June 19, 2012Assignee: Adeka CorporationInventors: Daisuke Sawamoto, Nobuhide Tominaga
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Patent number: 8203019Abstract: The present invention provides crystalline solid and amorphous forms of (?)-halofenate. The crystalline solid forms may be used in various pharmaceutical compositions, and are particularly effective for the prevention and/or treatment of conditions associated with blood lipid deposition in a mammal, particularly those diseases related to Type 2 diabetes and hyperlipidemia. The invention also relates to a method for preventing or treating Type 2 diabetes and hyperlipidemia in a mammal comprising the step of administering a therapeutically effective amount of crystalline solid and amorphous forms of (?)-halofenate.Type: GrantFiled: April 20, 2006Date of Patent: June 19, 2012Assignees: Metabolex, Inc., DiaTex, Inc.Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
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Publication number: 20120149900Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.Type: ApplicationFiled: January 8, 2010Publication date: June 14, 2012Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
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Publication number: 20120101087Abstract: The present invention relates to, in part, novel bisphenol compounds useful for the recognition, attachment and growth of unwanted biologics on natural and manmade surfaces. Another aspect of the invention relates to combinatorial libraries for producing the same. Another aspect of the invention relates to pharmaceutical formulations comprising the same.Type: ApplicationFiled: December 12, 2008Publication date: April 26, 2012Inventors: Randall S. Alberte, Robert D. Smith
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Publication number: 20120022154Abstract: The present invention encompasses novel triterpene compounds of general formula I, wherein R3a, R3b, R11a, R11b, R31 and R32 are defined as in claim 1, which are suitable for the prevention and/or treatment of diseases mediated by 11 ?-HSD and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: March 10, 2010Publication date: January 26, 2012Applicant: ONEPHARM RESEARCH & DEVELOPMENT GMBHInventors: Dirk Classenhouben, Bernhard Kueenburg, Paul Kosma, Ulrich Jordis, Christian Stanetty, Laszlo Czollner
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Patent number: 8049031Abstract: New solid forms of fesoterodine fumarate are described. In particular, amorphous fesoterodine fumarate, characterized by a powder X-ray diffraction spectrum as shown in FIG. 1 and by an IR spectrum as shown in FIG. 2 is described. Also fesoterodine fumarate in crystalline form I, characterized by a powder X-ray diffraction spectrum as shown in FIG. 3, by a DSC profile as shown in FIG. 4, by an IR spectrum as shown in FIG. 5, by a solid state 13C-NMR spectrum as shown in FIG. 6 and by a Raman spectrum as shown in FIGS. 7, 8 and 9 is described.Type: GrantFiled: December 10, 2009Date of Patent: November 1, 2011Assignee: Chemi S.p.A.Inventors: Umberto Ciambecchini, Maurizio Zenoni, Stefano Turchetta
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Publication number: 20110245110Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.Type: ApplicationFiled: May 9, 2011Publication date: October 6, 2011Applicant: AFFYMETRIX, INC.Inventors: Glenn H. McGall, Andrea Cupoletti
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Patent number: 8003699Abstract: Disclosed is an amide compound represented by the following formula (1). (1) (In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR6R7R8 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with at least one halogen atom or the like, R6 and R7 independently represent a C1-C4 alkyl group, and R8 represents a halogen atom, a hydroxyl group or the like.) The amide compound has excellent plant disease controlling activity.Type: GrantFiled: April 25, 2008Date of Patent: August 23, 2011Assignee: Sumitomo Chemical Company, LimitedInventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
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Publication number: 20110195979Abstract: A compound of formula (I) as well as pharmaceutically acceptable salt thereof, wherein R1 to R4 and Ar are as defined in description and in claims, can be used as a medicament.Type: ApplicationFiled: February 7, 2011Publication date: August 11, 2011Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
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Publication number: 20110155626Abstract: The present invention relates to an improved process for the preparation of Rasagiline or pharmaceutically acceptable salts thereof. The present invention also relates to Rasagiline salts, polymorphs thereof and process for preparation thereof.Type: ApplicationFiled: November 24, 2010Publication date: June 30, 2011Applicant: USV LimitedInventors: Dhananjay Govind Sathe, Subhash Vishwanath Damle, Kamlesh Digambar Sawant, Parag Sukumar Gatne, Tushar Anil Naik
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Publication number: 20110160370Abstract: The invention relates to a composition containing a particulate solid, a plastic material (such as a thermoplastic polymer) and a compound capable of having dispersant properties. The compound may be obtained/obtainable by reacting a fatty acid with either (i) a hydroxy-C4-5-alkylene carboxylic acid, or (ii) a lactone. The invention further relates to novel compounds, and the use of the compound as a dispersant.Type: ApplicationFiled: August 13, 2009Publication date: June 30, 2011Applicant: LUBRIZOL ADVANCED MATERIALS, INC.Inventors: Patrick J. Sunderland, Dean Thetford, Thomas Forder
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Publication number: 20110152227Abstract: This invention relates to novel derivatives of tolterodine, 5-hydroxymethyl tolterodine, fesoterodine and pharmaceutically acceptable salts thereof. This invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions that are beneficially treated by muscarinic receptor antagonists.Type: ApplicationFiled: April 9, 2009Publication date: June 23, 2011Applicant: CONCERT PHARMACEUTICALS INC.Inventor: Julie F. Liu
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Publication number: 20110144379Abstract: Disclosed are a novel asymmetric azine compound (I) and a method for producing an asymmetric azine compound (I) which is characterized in that an aldehyde compound (III) and hydrazine are reacted in an alcohol solvent at a molar ratio (aldehyde compound (III)):(hydrazine) of from 2:1 to 1:2, thereby obtaining a reaction solution including a hydrazone compound (IV), and then an aldehyde compound (V) is added for a reaction into the thus-obtained reaction solution at a molar ratio (aldehyde compound (V)):(hydrazone compound (IV)) of from 2:1 to 1:2. The method can commercially advantageously produce an asymmetric azine compound having a polar group such as a hydroxyl group or a carboxyl group in each molecule. The novel asymmetric azine compound can be obtained by this production method. (In the formulae, R1 and R2 each represents a hydroxyl group or a carboxyl group, X1 to X8 each represents a hydrogen atom, —C(?O)—OR3 or the like; and R3 represents an alkyl group having 1 to 10 carbon atoms or the like.Type: ApplicationFiled: June 17, 2009Publication date: June 16, 2011Applicant: ZEON CORPORATIONInventors: Kei Sakamoto, Yasushi Nakano
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Publication number: 20110136827Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.Type: ApplicationFiled: December 7, 2010Publication date: June 9, 2011Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20100324064Abstract: The present invention relates to novel analogs of choline and methods of use or treatment of neurodegenerative disorders and/or conditions such as Parkinson's disease, Huntington disease, Alzheimer's disease and related disorders such as amyotrophic lateral sclerosis, spinal muscular atrophy, Friedrich's ataxia, Pick's disease, Bassen-Kornzweig syndrome, Refsom's disease, retinal degeneration, Cruetzfelt-Jacob syndrome or prion disease (mad cow disease), dementia with Lewy bodies, schizophrenia, paraneoplastic cerebellar degeneration and neurodegenerative conditions caused by stroke. The present compounds are effective to treat any neurological condition where acetylcholine transmission neurons and their target cells are affected.Type: ApplicationFiled: July 22, 2010Publication date: December 23, 2010Applicants: Medical College of Georgia Research Institute, Universtiy of Georgia Research FoundationInventors: Jerry J. BUCCAFUSCO, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
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Patent number: 7851505Abstract: The current invention provides novel thiotungstate derivatives, methods of making novel thiotungstate derivatives, pharmaceutical compositions of novel thiotungstate derivatives, methods of using novel thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders and obesity and methods of using pharmaceutical compositions of thiotungstate derivatives to treat diseases associated with aberrant vascularization, copper metabolism disorders, neurodegenerative disorders, obesity or NF-?B dysregulation.Type: GrantFiled: May 27, 2004Date of Patent: December 14, 2010Assignee: Attenuon, LLCInventors: Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Melissa L. P. Price, Andrew Mazar
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Publication number: 20100297241Abstract: The present invention provides a novel amorphous form of fesoterodine fumarate, process for preparation, pharmaceutical compositions, and method of treating thereof.Type: ApplicationFiled: October 1, 2008Publication date: November 25, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Kishore Charugundla, Udhaya Kumar Chandramohan, Nitin Sharadchandra Pradhan, Jon Valgeirsson, Praveen Kumar Neela
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Patent number: 7829304Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.Type: GrantFiled: February 11, 2008Date of Patent: November 9, 2010Assignee: Northwestern UniversityInventors: Daniel H. Appella, Michael C. Myers
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Publication number: 20100249262Abstract: An oxime ester compound of formula (I) useful as a photopolymerization initiator. A photopolymerization initiator having the oxime ester compound as an active ingredient is activated through efficient absorption of light of long wavelength, e.g., 405 nm or 365 nm, to exhibit high sensitivity. In formula (I), R1 and R2 are each R11, OR11, COR11, SR11, CONR12R13, or CN; R11, R12, and R13 are each hydrogen, a C1-C20 alkyl group, C6-C30 aryl group, a C7-C30 arylalkyl group, or a C2-C20 heterocyclic group; R3 and R4 are each R11, OR11, SR11, COR11, CONR12R13, NR12COR11, OCOR11, COOR11, SCOR11, OCSR11, COSR11, CSOR11, CN, halogen, or a hydroxyl group; a and b is each 0 to 4; X is oxygen, sulfur, selenium, CR31R32, CO, NR33, or PR34; and R31, R32, R33, and R34 each have the same meaning as R1.Type: ApplicationFiled: December 25, 2007Publication date: September 30, 2010Applicant: ADEKA CORPORATIONInventors: Daisuke Sawamoto, Nobuhide Tominaga
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Publication number: 20100217034Abstract: Disclosed herein is an improved, commercially viable and industrially advantageous process for the preparation of Fesoterodine or a pharmaceutically acceptable salt thereof in high yield and purity. Disclosed also herein is an improved and industrially advantageous optical resolution method of racemic (±)-N,N-Diisopropyl-3-(2-benzyloxy-5-bromophenyl)-3-phenylpropylamine and use thereof for the preparation of Fesoterodine.Type: ApplicationFiled: September 22, 2008Publication date: August 26, 2010Applicant: ACTAVIS GROUP PTC EHFInventors: Kishore Charugundla, Udhaya Kumar, Rajendra Suryabhan Patil, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
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Patent number: 7763747Abstract: Bis- and tris-dihydroxyaryl compounds and their methylenedioxy analogs and pharmaceutically acceptable esters, their synthesis, pharmaceutical compositions containing them, and their use in the treatment of amyloid diseases, especially A? amyloidosis, such as observed in Alzheimer's disease, IAPP amyloidosis, such as observed in type 2 diabetes, and synucleinopathies, such as observed in Parkinson's disease, and the manufacture of medicaments for such treatment.Type: GrantFiled: November 4, 2008Date of Patent: July 27, 2010Assignee: Proteotech, Inc.Inventors: Alan D. Snow, Beth P. Nguyen, Gerardo M. Castillo, Virginia J. Sanders, Thomas P. Lake, Lesley Larsen, Rex T. Weavers, Stephen D. Lorimer, David S. Larsen, David L. Coffen, Charlotte Coffen, legal representative
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Publication number: 20100168459Abstract: The present invention provides a process for the production of a compound of formula (I) or a salt thereof, wherein R is hydrogen, a straight, branched or cyclic C1-C6 alkyl group or an aryl group which may optionally be substituted. This process comprises: (a) reacting a compound of formula (II), with a compound of formula (III), wherein R is as defined above and X is a leaving group, in the presence of N,N-di-isopropylethylamine.Type: ApplicationFiled: June 5, 2007Publication date: July 1, 2010Applicant: SCHWARZ PHARMA LTD.Inventors: Seth C. Ennis, Roland Drews, Claus Meese
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Publication number: 20100152483Abstract: New solid forms of fesoterodine fumarate are described. In particular, amorphous fesoterodine fumarate, characterised by a powder X-ray diffraction spectrum as shown in FIG. 1 and by an IR spectrum as shown in FIG. 2 is described. Also fesoterodine fumarate in crystalline form I, characterised by a powder X-ray diffraction spectrum as shown in FIG. 3, by a DSC profile as shown in FIG. 4, by an IR spectrum as shown in FIG. 5, by a solid state 13C-NMR spectrum as shown in FIG. 6 and by a Raman spectrum as shown in FIGS. 7, 8 and 9 is described.Type: ApplicationFiled: December 10, 2009Publication date: June 17, 2010Applicant: CHEMI S.P.A.Inventors: Umberto Ciambecchini, Maurizio Zenoni, Stefano Turchetta
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Publication number: 20100113770Abstract: A medicament having inhibitory activity against NF-?B activation which comprises as an active ingredient a substance selected from the group consisting of a compound represented by the following general formula (I) and a pharmacologically acceptable salt thereof, and a hydrate thereof and a solvate thereof: wherein X represents a connecting group whose number of atoms in a main chain is 2 to 5 (said connecting group may be substituted), “A” represents an acyl group which may be substituted, (provided that unsubstituted acetyl group and unsubstituted acryloyl group are excluded,) or a C1 to C6 alkyl group which may be substituted, or A may bind to connecting group X to form a cyclic structure which may be substituted, “E” represents an aryl group which may be substituted or a heteroaryl group which may be substituted, ring Z represents an arene which may have one or more substituents in addition to the group represented by formula —O-A wherein A has the same meaning as that defined above and the group rType: ApplicationFiled: October 14, 2009Publication date: May 6, 2010Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.Inventors: Susumu MUTO, Akiko ITAI
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Publication number: 20100105647Abstract: Disclosed is an amide compound represented by the following formula (1). (1) (In the formula, X1 represents a fluorine atom or a methoxy group; X2 represents a hydrogen atom, a halogen atom, a C1-C4 alkyl group or the like; Z represents an oxygen atom or a sulfur atom; and A represents an A1-CR6R7R8 group, an A2-Cy1 group or an A3-Cy2 group, wherein A1 represents a CH2 group or the like, A2 represents a single bond, a CH2 group or the like, Cy1 represents a C3-C6 cycloalkyl group substituted with a C1-C6 alkoxy group or the like, Cy2 represents a C3-C6 cycloalkyl group which may be substituted with at least one halogen atom or the like, R6 and R7 independently represent a C1-C4 alkyl group, and R8 represents a halogen atom, a hydroxyl group or the like.) The amide compound has excellent plant disease controlling activity.Type: ApplicationFiled: April 25, 2008Publication date: April 29, 2010Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
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Publication number: 20100076068Abstract: A compound of formula (1) Including pharmaceutically acceptable salts thereof, wherein: R1 is aryl or heteroaryl optionally substituted with R8; R2 is H or alkyl or CH2 (when forming part of a ring with R3, R4 or R5); R3 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R4 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R5 is H, alkyl, CH2OH or CH2OR6 and can be part of a ring with R2; R6 is H, alkyl, COH, COOR9, CON(R9)2, COR9, COR10, COR11, P(O)nR9, P(O)nR10S(O)nR10 or S(O)nR9 and can be part of a ring with R2, R3, R4 or R5; R7 is H, alkyl, COOR9, COOR11, COR9 or CON(R9)2, and can be part of a ring with R2, R3, R4, R5 or R6; R8 is alkyl, CF3, OR9, OCOR9, CONH2, CN, F, Cl, Br, I, N(R9)2, NO2, NHCHO, NHCONH2, NHSO2R9, CON(R9)2, S(O)nR9, CH2OH Or OCON(R9)2; R9 is H, alkyl or cycloalkyl; R10 is aryl or heteroaryl (optionally substituted with R8) or a four to seven membered ring (which is optionally substituted with R8 and can contain one or more additional heteroatoms selected fromType: ApplicationFiled: December 12, 2007Publication date: March 25, 2010Inventors: Andrea Walmsley, Elena Lasterra
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Patent number: 7667069Abstract: Ibopamine malcate salt (1:1), method for preparing it and pharmaceutical composition containing it.Type: GrantFiled: January 13, 2005Date of Patent: February 23, 2010Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.S.p.A.Inventors: Mario Pinza, Caterina Maugeri, Nicola Cazzolla
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Publication number: 20090318551Abstract: This invention relates to novel AKBA analogs of the formula I given below: Where in R1, R2, R3, R4 and R5 in each of the said analogs are: 1. R1?OCHO, R2?H, R3?COOH, R4 & R5?O 2. R1?OCOCH2Cl, R2?H, R3?COOH, R4 & R5?O 3. R1=5?-O-methylgalloyloxy, R2?H, R3?COOH, R4 & R5?O 4. R1?OCOCH2CH2COOH, R2?H, R3?COOH, R4 & R5?O 5. R1=8?,9?-Dihydro-4?-hydroxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 6. R1=4?-Hydroxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 7. R1=3?,4?-Dimethoxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 8. R1=3?,4?-Dihydroxy-5?-methoxycinnamoyloxy, R2?H, R3?COOH, R4 & R5?O 9. R1?OCOCH2NH(tert-BOC), R2?H, R3?COOCH3, R4 & R5?O 10. R1?OCOCH2NH2HCl, R2?H, R3?COOH, R4 & R5?O 11. R1?OCOCH(CH3)NH2HCl, R2?H, R3?COOH, R4 & R5?O 12. R1?H, R2?OH, R3?COOCH3, R4 & R5?O 13. R1?H, R2?Br, R3?COOCH3, R4 & R5?O 14. R1?CN, R2?H, R3?COOCH3, R4 & R5?O 15. R1?SH, R2?H, R3?COOCH3, R4 & R5?O 16. R1 & R2?N(OH), R3?COOCH3, R4 & R5?O 17.Type: ApplicationFiled: August 28, 2009Publication date: December 24, 2009Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti