Nitrogen In Alcohol Moiety Other Than As Nitro, Nitroso Or Isocyanate Patents (Class 560/250)
  • Patent number: 10039726
    Abstract: 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: Grant
    Filed: April 6, 2016
    Date of Patent: August 7, 2018
    Assignee: The Board of Trustees of the Leland Stanford Junior University
    Inventors: Isabella A. Graef, Mamoun M. Alhamadsheh
  • Patent number: 9233914
    Abstract: 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: Grant
    Filed: February 25, 2015
    Date of Patent: January 12, 2016
    Assignees: CYMABAY THERAPEUTICS, INC., DIATEX, INC.
    Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
  • Publication number: 20150094485
    Abstract: 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: Application
    Filed: April 26, 2013
    Publication date: April 2, 2015
    Inventors: Antonio Lorente Bonde-Larsen, Francisco Javier Gallo Nieto, Juan José Ferreiro Gil, Pablo Martín Pascual
  • Patent number: 8993797
    Abstract: 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: Grant
    Filed: July 10, 2013
    Date of Patent: March 31, 2015
    Assignee: Cymabay Therapeutics, Inc.
    Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
  • Patent number: 8871977
    Abstract: 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: Grant
    Filed: June 17, 2009
    Date of Patent: October 28, 2014
    Assignee: Zeon Corporation
    Inventors: Kei Sakamoto, Yasushi Nakano
  • Publication number: 20140283199
    Abstract: 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: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: KamTec
    Inventor: KamTec
  • Publication number: 20140155648
    Abstract: 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: Application
    Filed: February 2, 2012
    Publication date: June 5, 2014
    Applicant: HOVIONE INTER LIMITED
    Inventors: Jose Manuel Galindro, Ana Cristina Cruz, João José Bandarra, William Heggie
  • Patent number: 8668986
    Abstract: 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: Grant
    Filed: November 13, 2008
    Date of Patent: March 11, 2014
    Assignee: Sika Technology AG
    Inventor: Urs Burckhardt
  • Publication number: 20140066500
    Abstract: 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: Application
    Filed: November 6, 2013
    Publication date: March 6, 2014
    Applicant: Reviva Pharmaceuticals, Inc.
    Inventors: Laxminarayan BHAT, Seema BHAT
  • Publication number: 20140051757
    Abstract: 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: Application
    Filed: September 9, 2011
    Publication date: February 20, 2014
    Applicant: SIGMA-TAU Industrie Farmaceutiche Riunite S.p.A.
    Inventors: Silvia Cavazza, Martina Cavazza, Francesca Cavazza, Anna Atti, Enrico Cavazza
  • Publication number: 20140038822
    Abstract: 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: Application
    Filed: December 27, 2011
    Publication date: February 6, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Jens Frackenpohl, Lothar Willms, Thomas Müller, Stefan Lehr, Pascal Von Koskull-Döring, Ines Heinemann, Christopher Hugh Rosinger, Isolde Häuser-hahn, Martin Jeffrey Hills
  • Patent number: 8618323
    Abstract: 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: Grant
    Filed: January 28, 2011
    Date of Patent: December 31, 2013
    Assignee: Benz Research and Development Corporation
    Inventors: Patrick H. Benz, Jose A. Ors
  • Patent number: 8604112
    Abstract: 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: Grant
    Filed: August 13, 2009
    Date of Patent: December 10, 2013
    Assignee: The Lubrizol Corporation
    Inventors: Patrick J. Sunderland, Dean Thetford, Thomas Forder
  • Publication number: 20130261133
    Abstract: 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: Application
    Filed: March 14, 2013
    Publication date: October 3, 2013
    Applicant: The University of Montana
    Inventors: John Howard Hoody, David Brian Bolstad
  • Patent number: 8507719
    Abstract: 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: Grant
    Filed: May 11, 2012
    Date of Patent: August 13, 2013
    Assignees: Metabolex, Inc.
    Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
  • Patent number: 8476315
    Abstract: 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: Grant
    Filed: March 10, 2010
    Date of Patent: July 2, 2013
    Assignee: Onepharm Research & Development GmbH
    Inventors: Paul Kosma, Ulrich Jordis, Dirk Classen-Houben, Bernhard Kueenburg, Christian Stanetty, Laszlo Czollner
  • Publication number: 20130035317
    Abstract: 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: Application
    Filed: February 15, 2011
    Publication date: February 7, 2013
    Inventors: Christopher John Perry, Iain Douglas Nicholl
  • Patent number: 8344176
    Abstract: 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: Grant
    Filed: May 26, 2007
    Date of Patent: January 1, 2013
    Assignee: Schwarz Pharma Ltd.
    Inventors: Roisin Browne, Michael Kilkelly
  • Publication number: 20120258063
    Abstract: 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: Application
    Filed: December 16, 2010
    Publication date: October 11, 2012
    Applicant: Pola Chemical Industries Inc.
    Inventors: Yuko Saitoh, Chihiro Kondo, Takashi Yamasaki
  • Publication number: 20120220797
    Abstract: 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: Application
    Filed: July 26, 2010
    Publication date: August 30, 2012
    Inventors: Antonio Lorente Bonde-Larsen, Pablo Martín Pascual, Mario Laderas Muñoz, Luis Gerardo Gutiérrez Fuentes
  • Publication number: 20120220784
    Abstract: The present invention provides an efficient and scalable process to prepare the compound of formula 4 by reduction of the corresponding ?-acyloxy sulfides.
    Type: Application
    Filed: February 24, 2012
    Publication date: August 30, 2012
    Applicant: ScinoPharm Singapore PTE, Ltd.
    Inventors: JyhHsiung Liao, LungHuang Kuo
  • Publication number: 20120172426
    Abstract: 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: Application
    Filed: July 1, 2011
    Publication date: July 5, 2012
    Applicant: REVIVA PHARMACEUTICALS, INC.
    Inventors: Laxminarayan Bhat, Kouacou Adiey
  • Patent number: 8203019
    Abstract: 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: Grant
    Filed: April 20, 2006
    Date of Patent: June 19, 2012
    Assignees: Metabolex, Inc., DiaTex, Inc.
    Inventors: Edward D. Daugs, Eric J. Hagen, Jason A. Hanko, David H. Louks
  • Patent number: 8202679
    Abstract: 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: Grant
    Filed: December 25, 2007
    Date of Patent: June 19, 2012
    Assignee: Adeka Corporation
    Inventors: Daisuke Sawamoto, Nobuhide Tominaga
  • Publication number: 20120149900
    Abstract: Fluorinated compounds and methods of making fluorinated compounds are described herein.
    Type: Application
    Filed: January 8, 2010
    Publication date: June 14, 2012
    Inventors: Tobias Ritter, Laura Brass, Curtis Keith, Alan Watson, David J. Greenblatt
  • Publication number: 20120101087
    Abstract: 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: Application
    Filed: December 12, 2008
    Publication date: April 26, 2012
    Inventors: Randall S. Alberte, Robert D. Smith
  • Publication number: 20120022154
    Abstract: 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: Application
    Filed: March 10, 2010
    Publication date: January 26, 2012
    Applicant: ONEPHARM RESEARCH & DEVELOPMENT GMBH
    Inventors: Dirk Classenhouben, Bernhard Kueenburg, Paul Kosma, Ulrich Jordis, Christian Stanetty, Laszlo Czollner
  • Patent number: 8049031
    Abstract: 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: Grant
    Filed: December 10, 2009
    Date of Patent: November 1, 2011
    Assignee: Chemi S.p.A.
    Inventors: Umberto Ciambecchini, Maurizio Zenoni, Stefano Turchetta
  • Publication number: 20110245110
    Abstract: 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: Application
    Filed: May 9, 2011
    Publication date: October 6, 2011
    Applicant: AFFYMETRIX, INC.
    Inventors: Glenn H. McGall, Andrea Cupoletti
  • Patent number: 8003699
    Abstract: 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: Grant
    Filed: April 25, 2008
    Date of Patent: August 23, 2011
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
  • Publication number: 20110195979
    Abstract: 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: Application
    Filed: February 7, 2011
    Publication date: August 11, 2011
    Inventors: Li Chen, Xianfeng Lin, Zongxing Qiu, Guozhi Tang, Lisha Wang, Jim Zhen Wu, Wengang Yang
  • Publication number: 20110160370
    Abstract: 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: Application
    Filed: August 13, 2009
    Publication date: June 30, 2011
    Applicant: LUBRIZOL ADVANCED MATERIALS, INC.
    Inventors: Patrick J. Sunderland, Dean Thetford, Thomas Forder
  • Publication number: 20110155626
    Abstract: 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: Application
    Filed: November 24, 2010
    Publication date: June 30, 2011
    Applicant: USV Limited
    Inventors: Dhananjay Govind Sathe, Subhash Vishwanath Damle, Kamlesh Digambar Sawant, Parag Sukumar Gatne, Tushar Anil Naik
  • Publication number: 20110152227
    Abstract: 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: Application
    Filed: April 9, 2009
    Publication date: June 23, 2011
    Applicant: CONCERT PHARMACEUTICALS INC.
    Inventor: Julie F. Liu
  • Publication number: 20110144379
    Abstract: 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: Application
    Filed: June 17, 2009
    Publication date: June 16, 2011
    Applicant: ZEON CORPORATION
    Inventors: Kei Sakamoto, Yasushi Nakano
  • Publication number: 20110136827
    Abstract: 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: Application
    Filed: December 7, 2010
    Publication date: June 9, 2011
    Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
  • Publication number: 20100324064
    Abstract: 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: Application
    Filed: July 22, 2010
    Publication date: December 23, 2010
    Applicants: Medical College of Georgia Research Institute, Universtiy of Georgia Research Foundation
    Inventors: Jerry J. BUCCAFUSCO, Alvin V. Terry, J. Warren Beach, Rammamohanna R. Jonnala
  • Patent number: 7851505
    Abstract: 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: Grant
    Filed: May 27, 2004
    Date of Patent: December 14, 2010
    Assignee: Attenuon, LLC
    Inventors: Robert J. Ternansky, Patricia L. Gladstone, Amy L. Allan, Melissa L. P. Price, Andrew Mazar
  • Publication number: 20100297241
    Abstract: The present invention provides a novel amorphous form of fesoterodine fumarate, process for preparation, pharmaceutical compositions, and method of treating thereof.
    Type: Application
    Filed: October 1, 2008
    Publication date: November 25, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Kishore Charugundla, Udhaya Kumar Chandramohan, Nitin Sharadchandra Pradhan, Jon Valgeirsson, Praveen Kumar Neela
  • Patent number: 7829304
    Abstract: Ketoamine compounds and related methods for reactivation of tumor suppressor protein p53.
    Type: Grant
    Filed: February 11, 2008
    Date of Patent: November 9, 2010
    Assignee: Northwestern University
    Inventors: Daniel H. Appella, Michael C. Myers
  • Publication number: 20100249262
    Abstract: 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: Application
    Filed: December 25, 2007
    Publication date: September 30, 2010
    Applicant: ADEKA CORPORATION
    Inventors: Daisuke Sawamoto, Nobuhide Tominaga
  • Publication number: 20100217034
    Abstract: 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: Application
    Filed: September 22, 2008
    Publication date: August 26, 2010
    Applicant: ACTAVIS GROUP PTC EHF
    Inventors: Kishore Charugundla, Udhaya Kumar, Rajendra Suryabhan Patil, Praveen Kumar Neela, Nitin Sharadchandra Pradhan, Jon Valgeirsson
  • Patent number: 7763747
    Abstract: 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: Grant
    Filed: November 4, 2008
    Date of Patent: July 27, 2010
    Assignee: 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
  • Publication number: 20100168459
    Abstract: 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: Application
    Filed: June 5, 2007
    Publication date: July 1, 2010
    Applicant: SCHWARZ PHARMA LTD.
    Inventors: Seth C. Ennis, Roland Drews, Claus Meese
  • Publication number: 20100152483
    Abstract: 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: Application
    Filed: December 10, 2009
    Publication date: June 17, 2010
    Applicant: CHEMI S.P.A.
    Inventors: Umberto Ciambecchini, Maurizio Zenoni, Stefano Turchetta
  • Publication number: 20100113770
    Abstract: 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 r
    Type: Application
    Filed: October 14, 2009
    Publication date: May 6, 2010
    Applicant: INSTITUTE OF MEDICINAL MOLECULAR DESIGN, INC.
    Inventors: Susumu MUTO, Akiko ITAI
  • Publication number: 20100105647
    Abstract: 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: Application
    Filed: April 25, 2008
    Publication date: April 29, 2010
    Inventors: Takashi Komori, Mayumi Kubota, Yuichi Matsuzaki
  • Publication number: 20100076068
    Abstract: 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 from
    Type: Application
    Filed: December 12, 2007
    Publication date: March 25, 2010
    Inventors: Andrea Walmsley, Elena Lasterra
  • Patent number: 7667069
    Abstract: Ibopamine malcate salt (1:1), method for preparing it and pharmaceutical composition containing it.
    Type: Grant
    Filed: January 13, 2005
    Date of Patent: February 23, 2010
    Assignee: Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F.S.p.A.
    Inventors: Mario Pinza, Caterina Maugeri, Nicola Cazzolla
  • Publication number: 20090318551
    Abstract: 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: Application
    Filed: August 28, 2009
    Publication date: December 24, 2009
    Inventors: Ganga Raju Gokaraju, Rama Raju Gokaraju, Venkata Subbaraju Gottumukkala, Trimurtulu Golakoti