Alicyclic Acids Having An Element Other Than Oxygen, Carbon, Or Hydrogen Patents (Class 562/507)
  • Patent number: 10081605
    Abstract: Provided herein is a process and intermediates for the preparation of a compound of formula (I): or a pharmaceutically acceptable salt thereof, using cyanamide in the reaction.
    Type: Grant
    Filed: March 11, 2016
    Date of Patent: September 25, 2018
    Assignee: Lumos Pharma, Inc.
    Inventors: William R. Cantrell, Jr., William E. Bauta
  • Publication number: 20150148523
    Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.
    Type: Application
    Filed: January 28, 2014
    Publication date: May 28, 2015
    Applicant: Wisconsin Alumni Research Foundation
    Inventors: Samuel Helmer Gellman, Li Guo, Michael Giuliano
  • Publication number: 20150045274
    Abstract: The present invention relates to the field of perfumery. More particularly, it concerns compounds comprising at least one ?-thio carbonyl or nitrile moiety capable of liberating an active molecule selected from an ?,?-unsaturated ketone, aldehyde or nitrile. The present invention concerns also the use of said compounds in perfumery as well as the perfuming compositions or perfumed articles comprising the invention's compounds. (I) wherein: a) m represents an integer from 1 to 6; b) Pro represents a hydrogen atom or a group susceptible of generating an odoriferous ?,?-unsaturated ketone, aldehyde or nitrile and is represented by the formulae (II) or (II?) in which the wavy line indicates the location of the bond between said Pro and the sulfur atom S; and at least one of the Pro groups is of the formula (II) or (II?).
    Type: Application
    Filed: March 19, 2013
    Publication date: February 12, 2015
    Inventors: Peter Fankhauser, Andreas Herrmann, Umberto Maddalena, Alain Trachsel, Youqing Shen
  • Publication number: 20150024456
    Abstract: Compounds and methods for use in detecting gabapentin in a sample suspected of containing gabapentin are disclosed. Gabapentin derivatives are used to produce gabapentin conjugates. A gabapentin-immunogenic carrier conjugate may be used as an immunogen for the preparation of an anti-gabapentin antibody. A gabapentin-detectable label may be used in a signal producing system in gabapentin assays.
    Type: Application
    Filed: July 30, 2014
    Publication date: January 22, 2015
    Inventors: Johnny Jose Valdez, Byung Sook Moon, Michael Kevin Helms, Alejandro A. Orozco
  • Patent number: 8921571
    Abstract: Several different pyrrolysine analogs are disclosed in this application. Those analogs have distinct chemical and biophysical properties. Some analogs are useful in chemical ligation applications. Methods of making and using are also disclosed.
    Type: Grant
    Filed: October 6, 2010
    Date of Patent: December 30, 2014
    Assignee: The Ohio State University
    Inventors: Michael K. Chan, Tomasz Fekner, Xin Li, Marianne Lee, Manoj Nair, Jennifer Jo Ottensen
  • Publication number: 20140377875
    Abstract: UV-Absorbing and fluorescent pl markers for isoelectric focusing separations and fluorescent labeling, and methods for making and using the markers.
    Type: Application
    Filed: August 27, 2012
    Publication date: December 25, 2014
    Applicant: THE TEXAS A&M UNIVERSITY SYSTEM
    Inventors: Gyula Vigh, Ming-Chien Li
  • Patent number: 8907128
    Abstract: The purpose of the present invention is to provide a novel boron-containing compound utilizable in BNCT and so on and a process for preparing same. According to the process, a boron compounds having an amino acid skeleton containing cyclo-type rings or a pharmaceutically acceptable salt thereof is prepared, said boron compound being represented by general formula (I) [wherein l is an integer of 1 to 6; m is 0, 1, or 2; and n is 0, 1 or 2].
    Type: Grant
    Filed: August 2, 2011
    Date of Patent: December 9, 2014
    Assignee: Stella Pharma Corporation
    Inventors: Mitsunori Kirihata, Yoshihide Hattori, Kohki Uehara, Hiroshi Takenaka
  • Patent number: 8846946
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Grant
    Filed: January 31, 2013
    Date of Patent: September 30, 2014
    Assignee: Bayer CropScience AG
    Inventors: Reiner Fischer, Stefan Lehr, Jan Dittgen, Dieter Feucht, Ulrich Görgens, Isolde Häuser-Hahn, Christopher Hugh Rosinger, Arnd Voerste, Eva-Maria Franken, Olga Malsam
  • Publication number: 20140213795
    Abstract: The invention relates to novel compounds of the formula (I) in which W, X, Y, Z, A, B and G have the meanings given above, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also provides selective herbicidal compositions comprising, firstly, geminally alkoxy/alkylspirocyclically substituted tetramic acid derivatives and, secondly, a crop plant compatibility-improving compound. The invention furthermore relates to the boosting of the action of crop protection compositions comprising compounds of the formula (I) through the addition of ammonium salts or phosphonium salts and optionally penetrants.
    Type: Application
    Filed: January 31, 2013
    Publication date: July 31, 2014
    Applicant: BAYER INTELLECTUAL PROPERTY GMBH
    Inventors: Reiner FISCHER, Stefan LEHR, Jan DITTGEN, Dieter FEUCHT, Ulrich GÖRGENS, Isolde HÄUSER-HAHN, Christopher Hugh ROSINGER, Arnd VOERSTE, Eva-Maria FRANKEN, Olga MALSAM
  • Publication number: 20140171507
    Abstract: The invention relates to compounds, to compositions comprising the same and uses thereof for the prevention or treatment of pain, e.g neuropathic pain while having neutral or beneficial effect on metabolic parameters.
    Type: Application
    Filed: September 6, 2013
    Publication date: June 19, 2014
    Inventors: Xianqi KONG, Nigel LEVENS, Serge LAMOTHE, Mohammed ATFANI, Stephane CIBLAT, Lucie JETTE
  • Publication number: 20140094615
    Abstract: Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
    Type: Application
    Filed: April 26, 2012
    Publication date: April 3, 2014
    Applicant: The Board of Trustees of the University of Illinois
    Inventors: Martin D. Burke, Junqi Li, Eric P. Gillis
  • Patent number: 8664356
    Abstract: The invention provides compounds and methods, for example, to carry out organocatalytic Michael additions of aldehydes to cyclically constrained nitroethylene compounds catalyzed by a proline derivative to provide cyclically constrained ?-substituted-?-nitro-aldehydes. The reaction can be rendered enantioselective when a chiral pyrrolidine catalyst is used, allowing for Michael adducts in nearly optically pure form (e.g., 96 to >99% e.e.). The Michael adducts can bear a single substituent or dual substituents adjacent to the carbonyl. The Michael adducts can be efficiently converted to cyclically constrained protected ?-amino acid residues, which are essential for systematic conformational studies of ?-peptide foldamers. New methods are also provided to prepare other ?-amino acids and peptides. These new building blocks can be used to prepare foldamers, such as ?/?-peptide foldamers, that adopt specific helical conformations in solution and in the solid state.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: March 4, 2014
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Samuel Helmer Gellman, Li Guo, Michael Giuliano
  • Patent number: 8652360
    Abstract: The present invention aims to provide a method of use for surface-modifying a semiconductor nanocrystal comprising at least the steps consisting in having a semiconductor nanocrystal, the organic coating layer of which is provided, at the outer surface of the nanocrystal, with at least one reactive group G1 that reacts according to a cycloaddition reaction of click chemistry type; and bringing said nanocrystal together with an adjoining material provided at the surface with at least one G2 group complementary to the G1 group with respect to said click chemistry reaction, under conditions favorable to the interaction of said G1 and G2 groups, characterized in that said G1 and G2 groups are respectively an azide and a strained cycloalkynyl radical, or vice versa.
    Type: Grant
    Filed: September 8, 2009
    Date of Patent: February 18, 2014
    Assignee: Commissariat a l'Energie Atomique
    Inventors: Isabelle Texier-Nogues, Aude Bernardin
  • Patent number: 8628684
    Abstract: A process is proposed for the preparation of a powder comprising one or more derivatives of glycine-N,N-diacetic acid and/or one or more derivatives of glutamine-N,N-diacetic acid with a degree of crystallinity of ?30%, starting from an aqueous solution comprising the one or more derivatives of glycine-N,N-diacetic acid and/or the one or more derivatives of glutamine-N,N-diacetic acid in a concentration range from 20 to 60% by weight, based on the total weight of the aqueous solution, where the aqueous solution is concentrated in a first process step in an evaporator with rotating internals, which are arranged at a distance relative to the inside wall of the evaporator of ?1% of the diameter of the evaporator, to give a crystal slurry with a solids concentration in the range from 60 to 85% by weight, based on the total weight of the crystal slurry, and where in a second process step the crystal slurry is left to ripen in a paste bunker and then in a thin-film contact dryer, and where the residence time in t
    Type: Grant
    Filed: May 19, 2010
    Date of Patent: January 14, 2014
    Assignee: BASF SE
    Inventors: Frank Mrzena, Hans-Juergen Kinder, Michael Schoenherr, Gerhard Cox, Thomas Schmidt, Volker Huett
  • Publication number: 20130344527
    Abstract: The present invention provides modified cycloalkyne compounds; and method of use of such compounds in modifying biomolecules. The present invention features a cycloaddition reaction that can be carried out under physiological conditions. In general, the invention involves reacting a modified cycloalkyne with an azide moiety on a target biomolecule, generating a covalently modified biomolecule. The selectivity of the reaction and its compatibility with aqueous environments provide for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).
    Type: Application
    Filed: April 23, 2013
    Publication date: December 26, 2013
    Applicant: The Regents of the University of California
    Inventor: The Regents of the University of California
  • Publication number: 20130310545
    Abstract: Described is a compound capable of reducing or inhibiting (a) the biological activity of branched-chain-aminotranferase-1 (BCAT1) or (b) the expression of the gene encoding BCAT1 for use in a method of treating a neoplasia. A preferred compound is 1-(aminomethyl) cyclohexaneacetic acid (gabapentin).
    Type: Application
    Filed: January 27, 2012
    Publication date: November 21, 2013
    Applicant: Deutsches Krebsforschungszentrum
    Inventors: Bernhard Radlwimmer, Martje Toenjes, Sebastian Barbus, Peter Lichter
  • Publication number: 20130281726
    Abstract: To provide a method for recovering a precious metal from a solution containing precious metal ions, an extracting agent or adsorbent used therefor, and a back-extracting agent or desorbent. An extracting agent or adsorbent in which precious metal ions are extracted or adsorbed, is brought into contact with a back-extracting agent or desorbent containing a sulfur-containing amino acid derivative represented by the following formula (I): wherein R1 is a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group, or a C6-14 aromatic hydrocarbon group, R2's are each independently a hydrogen atom, a methyl group, an ethyl group, a vinyl group, a C3-8 linear, branched or cyclic hydrocarbon group or a C6-14 aromatic hydrocarbon group, and n is 0 or 1, to obtain a solution containing the precious metal ions, which is subjected to a reduction treatment to obtain a precious metal.
    Type: Application
    Filed: December 28, 2011
    Publication date: October 24, 2013
    Applicant: TOSOH CORPORATION
    Inventors: Yukinori Suso, Takashi Sakaki
  • Patent number: 8524940
    Abstract: It is possible to produce oseltamivir safely and stably in large quantities by using as a starting material tartaric acid, mannitol or arabinose, via dihydroxyhexenoic acid ester of the formula (4c): (wherein R1, R2 and R6 are same or different and are each alkyl, aryl, substituted aryl, aralkyl, substituted aralkyl or aromatic heterocyclic group, and R1 and R2 are not methyl simultaneously).
    Type: Grant
    Filed: December 6, 2011
    Date of Patent: September 3, 2013
    Assignee: National University Corporation Okayama University
    Inventors: Teruhiko Ishikawa, Seiki Saito, Takayuki Kudoh, Kotaro Suto, Hironori Nishiuchi, Makoto Okada, Masatoshi Taniguchi
  • Publication number: 20130225828
    Abstract: The present invention provides novel amino acid compounds useful in detecting and evaluating brain and body tumors. These compounds have the advantageous properties of rapid uptake and prolonged retention in tumors and can be labeled with halogen isotopes such as fluorine-18, iodine-123, iodine-124, iodine-125, iodine-131, bromine-75, bromine-76, bromine-77, bromine-82, astatine-210, astatine-211, and other astatine isotopes. These compounds can also be labeled with technetium and rhenium isotopes using known chelation complexes. The compounds disclosed herein bind tumor tissues in vivo with high specificity and selectivity when administered to a subject. Preferred compounds show a target to non-target ratio of at least 2:1, are stable in vivo and substantially localized to target within 1 hour after administration. Preferred compounds include 1-amino-2-[18F]fluorocyclobutyl-1-carboxylic acid (2-[18F]FACBC) and 1-amino-2-[18]fluoromethylcyclobutyl-1-carboxylic acid (2-[18F]FMACBC).
    Type: Application
    Filed: April 5, 2013
    Publication date: August 29, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: EMORY UNIVERSITY
  • Patent number: 8513457
    Abstract: A fluorine-containing unsaturated carboxylic acid represented by formula (1), wherein R1 represents a polymerizable double-bond containing group, R3 represents a fluorine atom or fluorine-containing alkyl group, and W represents a bivalent linking group. This compound can provide a fluorine-containing polymer compound that has a weight-average molecular weight of 1,000-1,000,000 and contains a repeating unit represented by formula (2), wherein R3 and W are defined as above, each of R4, R5 and R6 independently represents a hydrogen atom, fluorine atom or monovalent organic group, at least two of R4, R5 and R6 may be combined to form a ring. This polymer compound can provide a chemically amplified resist composition that is transparent to KrF or ArF excimer laser light and has a high resolution and is capable of forming a pattern having a rectangular section with no swelling.
    Type: Grant
    Filed: May 17, 2012
    Date of Patent: August 20, 2013
    Assignee: Central Glass Company, Limited
    Inventors: Yoshimi Isono, Jonathan Joachim Jodry, Satoru Narizuka, Kazuhiro Yamanaka
  • Publication number: 20130123618
    Abstract: This invention provides amino acid derivatives useful in detecting and evaluating brain and body tumors, including (1S,2S) anti-2-[18F]FACPC and (1R,2R) anti-2-[18F]FACPC.
    Type: Application
    Filed: January 2, 2013
    Publication date: May 16, 2013
    Applicant: EMORY UNIVERSITY
    Inventor: EMORY UNIVERSITY
  • Patent number: 8431739
    Abstract: This invention discloses a process for converting gabapentin acid salt to free gabapentin, where the salt is dissolved in an organic solvent in which both gabapentin acid salt and free gabapentin are soluble. The solution is treated with a powdered alkaline base to liberate free gabapentin which will remain in solution. The insoluble alkali salt of the acid is removed by filtration. From the filtrate free gabapentin is obtained either by adding anti-solvent or by extraction with water.
    Type: Grant
    Filed: December 14, 2010
    Date of Patent: April 30, 2013
    Assignee: Divi's Laboratories, Ltd.
    Inventors: Murali Krishna Prasad Divi, Gundu Rao Padakandla, Mysore Aswatha Narayana Rao, Shaik Nowshuddin, Maddipati Prasad
  • Patent number: 8431738
    Abstract: Disclosed is the method for producing an optically active BSH amino acid, which comprises a step of reacting an optically active a-amino acid derivative having a halogen in a side chain with a cyanoethyl BSH compound represented by formula (1). An optically active BSH amino acid obtained by the method is also disclosed.
    Type: Grant
    Filed: July 23, 2009
    Date of Patent: April 30, 2013
    Assignee: Stella Pharma Corporation
    Inventors: Mitsunori Kirihata, Tomoyuki Asano, Kohki Uehara, Yoshihide Hattori, Shintaro Kusaka
  • Patent number: 8357820
    Abstract: The present invention relates to a method for producing N-protected amino acid. Specifically, the present invention provides a method in which a protecting group is introduced to the amino group of an amino acid in a reaction under alkaline condition, and the N-protected amino acid thus generated is then separated from the reaction solution as crystals, without undergoing an extraction step or a concentration step. The present inventors have completed the invention based on the finding that desirable crystals of N-protected amino acids may be obtained without extraction, concentration or recrystallization steps between the initial generation of the N-protected amino acid molecules and the subsequent separation of the crystals, by first adding an water-soluble organic solvent and optionally water to the reaction solution (alkaline) containing the N-protected amino acid, and then neutralizing the solution by an acid.
    Type: Grant
    Filed: September 16, 2010
    Date of Patent: January 22, 2013
    Assignee: Sekisui Medical Co., Ltd.
    Inventors: Tomoaki Saigoku, Takaharu Iwaki, Masato Sakuyama
  • Publication number: 20120328514
    Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.
    Type: Application
    Filed: July 8, 2010
    Publication date: December 27, 2012
    Applicant: Lantheus Medical Imaging, Inc.
    Inventors: Richard R. Cesati, Thomas D. Harris, Simon P. Robinson, Richard J. Looby, Edward H. Cheesman, Padmaja Yalamanchili, David S. Casebier
  • Publication number: 20120329661
    Abstract: The present invention relates to a plurality of isotopically labeled compounds (“tag isotopomers”) and individual labeled compounds, which are useful for labeling samples of analytes, such as biological compounds. The present invention further relates to methods of labeling and quantifying analytes using these tag isotopomers.
    Type: Application
    Filed: May 15, 2012
    Publication date: December 27, 2012
    Inventor: ZengKui Guo
  • Publication number: 20120309944
    Abstract: The invention relates to growth hormone compounds with a protracted profile. The effect is obtained by linking an albumin binding residue via a hydrophilic spacer to growth hormone variants. Further described are methods of preparing and using such compounds. These growth hormone compounds are based on there altered profile considered particular useful in therapy.
    Type: Application
    Filed: January 24, 2011
    Publication date: December 6, 2012
    Applicant: Novo Nordisk Health Care AG
    Inventors: Carsten Behrens, Nils Langeland Johansen, Henrik Sune Andersen, Leif Noerskov-Lauritsen, Jens Buchardt
  • Publication number: 20120296093
    Abstract: This application discloses a novel process for the preparation of himbacine analogs useful as thrombin receptor antagonists. The process is based in part on the use of a base-promoted dynamic epimerization of a chiral nitro center.
    Type: Application
    Filed: July 31, 2012
    Publication date: November 22, 2012
    Inventors: George Wu, Anantha R. SUDHAKAR, Tao WANG, Ji XIE, Frank Xing CHEN, Marc POIRIER, Mingsheng HUANG, Vijay SABESAN, Daw-long KWOK, Jian CUI, Xiaojing YANG, Tiruvettipuram K. THIRUVENGADAM, Jing LIAO, Ilia A. Zavialov, Hoa N. NGUYEN, Ngiap Kie LIM
  • Patent number: 8304553
    Abstract: A process is provided for the synthesis of 4,5-diamino cyclohexene carboxylate ester (1): or a pharmaceutically acceptable salt thereof. R1-R3 are a silyl-, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. R4, R11 and R12 are H, a silyl-group, an aliphatic, alicyclic, aromatic, arylaliphatic, or an arylalicyclic group. 3,4-Dihydropyran compound (9): with R5 and R6 being suitable protecting groups, is reacted to form aldehyde (4): which is oxidized and converted to N-substituted carbamate (3): with R7 being a suitable protecting group. (3) is, via oxazolinidone (13): converted to azido carboxylate ester (2): and then to 4,5-diamino cyclohexene carboxylate ester (1).
    Type: Grant
    Filed: December 10, 2008
    Date of Patent: November 6, 2012
    Assignee: Nanyang Technological University
    Inventors: Xuewei Liu, Jimei Ma
  • Publication number: 20120264790
    Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.
    Type: Application
    Filed: May 1, 2012
    Publication date: October 18, 2012
    Applicant: SANOFI
    Inventors: Josef PERNERSTORFER, Heinz-Werner KLEEMANN, Matthias SCHAEFER, Alena SAFAROVA, Marcel PATEK
  • Patent number: 8258185
    Abstract: Use of neboglamine, (S)-4-amino-N(4,4-dimethyl-cyclohexyl)glutamic acid (CR 2249) (CAS Registry Number 163000-63-3), the racemic mixture thereof or a pharmaceutically acceptable salt thereof, for the preparation of a medicament for use in the treatment of toxicodependency induced by drugs such as CNS sedatives such as opiates, barbiturates, benzodiazepines, alcohol, stimulants such as amphetamines and cocaine, and hallucinogens such as LSD, mescalin, cannabis (marijuana) or fencyclidine.
    Type: Grant
    Filed: July 27, 2011
    Date of Patent: September 4, 2012
    Assignee: Rottapharm S.p.A.
    Inventors: Francesco Makovec, Gianfranco Caselli, Lucio Claudio Rovati, Antonio Giordani
  • Publication number: 20120165559
    Abstract: The present invention relates to compounds of general formula (I): having a physiological effect, and to the preparation thereof and to the use of same.
    Type: Application
    Filed: April 15, 2010
    Publication date: June 28, 2012
    Inventors: Jean Mane, Jean-Claude Clinet
  • Publication number: 20120142722
    Abstract: Novel compounds and pharmaceutical compositions are provided. In one aspect of the invention the compounds may be utilized in medical practice, for example, in treatment of cancer and immune disorders. In another aspect of the invention there is provided a conjugate, comprising a cytotoxic agent and a modulating moiety, the modulating moiety serving to target apoptotic cells.
    Type: Application
    Filed: June 23, 2010
    Publication date: June 7, 2012
    Inventors: Ilan Ziv, Anat Shirvan, Hagit Grimberg
  • Patent number: 8143443
    Abstract: A process for preparing gabapentin of formula 1, which comprises Formula (I) converting 1-allyl-cyclohexanecarboxaldehyde into 1-allyl-cyclohexanecarbonitrile; ozonizing 1-allyl-cyclohexanecarbonitrile to obtain 1-cyano-cyclohexaneacetaldehyde; acetalizing 1-cyano-cyclohexaneacetaldehyde with a suitable acetalizing agent to give the corresponding acetal and converting the latter into gabapentin.
    Type: Grant
    Filed: June 29, 2007
    Date of Patent: March 27, 2012
    Assignee: ZaCh System S.p.A.
    Inventors: Franco Ghelfi, Livius Cotarca, Fabrizio Roncaglia, Roberto Giovanetti, Andrea Nicoli
  • Publication number: 20120071664
    Abstract: Disclosed are ?-amino acids that are unsubstituted in the ? position; that are substituted in the ? position with an aryl group; that are substituted in the ? position with an aryl group; that bear two substituents in the ? position; and/or that are substituted in the ? and ? positions with groups which, together with the carbon atoms at the ? and ? positions, form a ring. Also disclosed are methods for making the above-mentioned ?-amino acids and other ?-amino acids which involve providing an ?,?-unsaturated imide; converting the ?,?-unsaturated imide to a 2-substituted-isoxazolidin-5-one; and converting the 2-substituted-isoxazolidin-5-one to a ?-amino acid.
    Type: Application
    Filed: September 20, 2011
    Publication date: March 22, 2012
    Applicant: NDSU Research Foundation
    Inventors: Mukund P. SIBI, Craig P. Jasperse, Prabagaran Narayanasamy, Sandeep R. Ghorpade
  • Publication number: 20120065426
    Abstract: The present invention aims to provide a practical process for preparing amine compounds through a generalized highly-diastereoselective reductive amination reaction.
    Type: Application
    Filed: September 14, 2011
    Publication date: March 15, 2012
    Applicant: Kanto Kagaku Kabushiki Kaisha
    Inventors: Masahito Watanabe, Kouichi Tanaka, Takashi Miki, Kunihiko Murata
  • Publication number: 20120053237
    Abstract: The invention relates to (among other things) oligomer-amino acid conjugates and related compounds. A conjugate of the invention, when administered by any of a number of administration routes, exhibits advantages over un-conjugated amino acid compounds.
    Type: Application
    Filed: February 24, 2010
    Publication date: March 1, 2012
    Applicant: NEKTAR THERAPEUTICS
    Inventors: Xuyuan Gu, Jennifer Riggs-Sauthier
  • Patent number: 8105807
    Abstract: The present invention relates to carbamoylglycine derivatives, a process for the preparation of carbamoylglycine derivatives and the use of carbamoylglycine derivatives in the preparation of enantiomerically enriched ?-amino acids. Furthermore, the present invention relates to the preparation of pharmaceutically active products such as perindopril and ramipril using the novel carbamoylglycine derivatives.
    Type: Grant
    Filed: October 2, 2008
    Date of Patent: January 31, 2012
    Assignee: DSM IP Assets B.V.
    Inventors: Georgios Sarakinos, Ben De Lange
  • Publication number: 20120010428
    Abstract: Disclosed is a process for the preparation of Compound (III), salt or solvate thereof by reacting Compound (I), salt or solvate thereof with Compound (II) in a toluene solvent in the presence of an additive such as water or an alcohol. Also disclosed is a process for the preparation of Compound (IV) comprising hydrolyzing the obtained Compound (III) if necessary, and then oxidizing. In the formula, R1 is hydrogen, optionally substituted lower alkyl, optionally substituted aryl or optionally substituted aryl lower alkyl, and R2 is optionally substituted lower alkyl, optionally substituted cycloalkyl or optionally substituted aryl lower alkyl.
    Type: Application
    Filed: September 19, 2011
    Publication date: January 12, 2012
    Applicant: Shionogi & Co., Ltd.
    Inventors: Toshiaki MASUI, Kazuhiro YOSHIDA
  • Publication number: 20120010254
    Abstract: The present invention provides in part a compound of Formula (I) or a pharmaceutically-acceptable salt or stereoisomer thereof: where R1 is selected from the group consisting of a substituted triazole group, a guanidine group, a urea group, a thiourea group, an amidine group, and N3; and R2 is selected from the group consisting of H, Me, Et and an amino acid, and methods and uses thereof.
    Type: Application
    Filed: December 30, 2009
    Publication date: January 12, 2012
    Applicant: Simon Fraser University
    Inventors: Brian Mario Pinto, Sankar Mohan
  • Publication number: 20120010557
    Abstract: The present invention relates to a drug delivery system for use in the treatment of vascular and vessel-related pathologies, comprising a drug delivery platform that comprises at least one compound capable of exerting an effect on the formation and/or maintenance of a thrombus in the vessel to be treated. The platform is preferably formed by liposomes that are sterically stabilized by grafting of poly(ethylene glycol) onto the liposome surface. The liposomes may further comprise photosensitizers and targeting molecules. The liposomes may be thermosensitive. The compound is suitably tranexamic acid. The drug delivery system is preferably used for the treatment of port wine stains.
    Type: Application
    Filed: January 26, 2010
    Publication date: January 12, 2012
    Inventor: Michal Heger
  • Publication number: 20110306787
    Abstract: This invention discloses a process for converting gabapentin acid salt to free gabapentin, where the salt is dissolved in an organic solvent in which both gabapentin acid salt and free gabapentin are soluble. The solution is treated with a powdered alkaline base to liberate free gabapentin which will remain in solution. The insoluble alkali salt of the acid is removed by filtration. From the filtrate free gabapentin is obtained either by adding anti-solvent or by extraction with water.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 15, 2011
    Applicant: DIVI'S LABORATORIES LIMITED
    Inventors: Murali Krishna Prasad Divi, Gundu Rao Padakandla, Mysore Aswatha Narayana Rao, Shaik Nowshuddin, Maddipati Prasad
  • Patent number: 8067630
    Abstract: A method for forming cascade polymers specifically utilizing the amine monomer of the formula The monomer is made by initially reacting nitromethane and CH2?CHCO2—TBu by nucleophilic addition to form the triester nitrotrialkanoate of the formula and then reducing the nitrosubstituent to afford the said amine monomer.
    Type: Grant
    Filed: September 15, 2009
    Date of Patent: November 29, 2011
    Assignee: University of South Florida
    Inventors: George R. Newkome, Charles N. Moorefield, Rajani K. Behera
  • Publication number: 20110288328
    Abstract: A method for preparing a trans-{4-[(alkylamino)methyl]cyclohexyl}acetic acid, which is useful as a raw material compound for manufacture of medicaments and the like, comprising the step of reducing amide group of a compound represented by the following general formula (6) (R1 represents hydrogen atom or a C1-6 alkyl group, and R2 represents a C1-6 alkyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl)(C1-6 alkyl) group, a C6-10 aryl group, or a C7-12 aralkyl group).
    Type: Application
    Filed: November 27, 2009
    Publication date: November 24, 2011
    Applicant: KOWA COMPANY, LTD.
    Inventors: Taichi Kusakabe, Koichi Yamazaki, Tadaaki Ohgiya, Kimiyuki Shibuya
  • Patent number: 8048917
    Abstract: The present invention provides prodrugs of GABA analogs, pharmaceutical compositions of prodrugs of GABA analogs and methods for making prodrugs of GABA analogs. The present invention also provides methods for using prodrugs of GABA analogs and methods for using pharmaceutical compositions of prodrugs of GABA analogs for treating or preventing common diseases and/or disorders.
    Type: Grant
    Filed: April 6, 2005
    Date of Patent: November 1, 2011
    Assignee: XenoPort, Inc.
    Inventors: Mark A. Gallop, Kenneth C. Cundy, Cindy X. Zhou, Fenmei Yao, Jia-Ning Xiang
  • Publication number: 20110257401
    Abstract: It has been demanded to provide a process for industrially producing an intermediate for a compound that exhibits an inhibitory effect on activated blood coagulation factor X and is useful as a preventive and/or therapeutic agent for thrombotic diseases. The present invention provides a process for producing the (R)-?-phenylethylamine salt of (S)-3-cyclohexene-1-carboxylic acid, comprising reacting 3-cyclohexene-1-carboxylic acid and (R)-?-phenylethylamine using a mixed solvent of water and acetone or a mixed solvent of water and ethyl acetate as a solvent.
    Type: Application
    Filed: June 10, 2011
    Publication date: October 20, 2011
    Applicant: Daiichi Sankyo Company, Limited
    Inventors: Koji Sato, Kazuo KUBOTA
  • Patent number: 8022250
    Abstract: 1-Phenylalkanecarboxylic acid derivatives, the processes for the preparation thereof and the use thereof in the treatment and/or prevention of neurodegenerative diseases such as Alzheimer's disease.
    Type: Grant
    Filed: December 24, 2009
    Date of Patent: September 20, 2011
    Assignee: Chiesi Farmaceutici S.p.A.
    Inventors: Luca Raveglia, Ilaria Peretto, Stefano Radaelli, Bruno Pietro Imbimbo, Andrea Rizzi, Gino Villetti
  • Patent number: 7989658
    Abstract: The present invention relates to a process for the purification of gabapentin. The process relates to the addition of hydrochloric acid to an aqueous solution or suspension of gabapentin, before, during or after the concentration step of that solution, and the subsequent slurry of the gabapentin by the addition of an alcoholic solvent. The so obtained gabapentin has an high purity degree and, in particular, is characterized by a low content of lactam.
    Type: Grant
    Filed: December 15, 2005
    Date of Patent: August 2, 2011
    Assignee: ZaCh System S.p.A.
    Inventors: Roberto Giovanetti, Andrea Nicoli, Livius Cotarca
  • Patent number: 7981930
    Abstract: Kits comprising an M2 inhibitor selected from amantadine and rimantadine; ribavirin, and a neuraminidase inhibitor (NAi) in an amount that is antivirally effective in the combination, an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin and a neuraminidase inhibitor are provided for the treatment of influenza. Some embodiments of the kits comprise an oral dosage form containing 75-250 mg of the M2 inhibitor, an oral dosage form comprising 100-400 mg of ribavirin, and a neuraminidase inhibitor.
    Type: Grant
    Filed: February 29, 2008
    Date of Patent: July 19, 2011
    Assignee: Adamas Pharmaceuticals, Inc.
    Inventors: Jack Nguyen, Gregory T. Went, Paul Spence, Timothy J. Fultz, David Chernoff, Terry L. Burkoth, Rowan Chapman, Mickey S. Urdea
  • Patent number: 7973079
    Abstract: Compounds that reduce serum retinol levels are used to treat ophthalmic conditions associated with the overproduction of waste products that accumulate during the course of the visual cycle. We describe methods, compounds, and compositions to treat, for example, the macular degenerations and dystrophies or to alleviate symptoms associated with such ophthalmic conditions.
    Type: Grant
    Filed: September 15, 2008
    Date of Patent: July 5, 2011
    Assignee: Revision Therapeutics, Inc.
    Inventors: Nathan L. Mata, Kim B. Phan, Tam V. Bui, Mustapha Haddach