Cyclobutyl In Acid Moiety Patents (Class 560/123)
  • Patent number: 11352312
    Abstract: The present invention provides a process for preparing a diester compound of the following general formula (1), having a dimethylcyclobutane ring, wherein R1 and R2 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, the process comprising reacting a dimethylcyclobutanone compound of the following general formula (2), wherein R1 is as defined above, with a phosphonic ester compound of the following general formula (3), wherein R2 and R3 represent, independently of each other, a monovalent hydrocarbon group having 1 to 10 carbon atoms, to produce the diester compound (1), having a dimethylcyclobutane ring.
    Type: Grant
    Filed: July 16, 2020
    Date of Patent: June 7, 2022
    Assignee: Shin-Etsu Chemical Co., Ltd.
    Inventors: Naoki Ishibashi, Yusuke Nagae, Takeshi Kinsho
  • Patent number: 9359288
    Abstract: The present invention provides a method for the production of [18F]-FACBC which has advantages over know such methods. Also provided by the present invention is a system to carry out the method of the invention and a cassette suitable for carrying out the method of the invention on an automated radiosynthesis apparatus.
    Type: Grant
    Filed: August 7, 2013
    Date of Patent: June 7, 2016
    Assignee: GE Healthcare Limited
    Inventors: Anders Svadberg, Olav Ryan, Roger Smeets
  • Patent number: 9278916
    Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabeled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET agent and particularly to the work-up process of this precursor removing generated salts from the intermediate composition.
    Type: Grant
    Filed: November 28, 2011
    Date of Patent: March 8, 2016
    Assignee: GE Healthcare Limited
    Inventors: Tom Christian Berg, Anne Nilsen
  • Publication number: 20150025250
    Abstract: Compounds of the formula I wherein R2a and R2b are independently H, halo, C1-C4alkyl, C1-C4haloalkyl or C1-C4alkoxy, or R2a and R2b together with the carbon atom to which they are attached form a C3-C6cycloalkyl; R3 is a C5-C10 alkyl, optionally substituted with 1-3 substituents independently selected from halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; or R3 is a C2-C4alkyl chain with at least 2 chloro or 3 fluoro substituents; or R3 is C3-C7cycloalkylmethyl, optionally substituted with 1-3 substituents independently selected from C1-C4alkyl, halo, C1-C4haloalkyl, C1-C4alkoxy, C1-C4haloalkoxy; R4 is C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, C1-C6alkylamino, C1-C6dialkylamino or; R4 is Het or Carbocyclyl, either of which is optionally substituted with 1-3 substituents R4 is Het, carbocyclyl, C1-C6alkyl, C1-C6haloalkyl, C1-C6alkoxy or C1-C6haloalkoxy; n is 1, 2 or 3; for the use in the prophylaxis or treatment of a disorder characterised by inappropriate expression or activation of cat
    Type: Application
    Filed: October 2, 2014
    Publication date: January 22, 2015
    Inventors: Susana AYESA, Urszula GRABOWSKA, Ellen HEWITT, Daniel JONSSON, Bjorn KLASSON, Pia KAHNBERG, Stina LUNDGREN, Jan TEJBRANT, Daniel WIKTELIUS
  • Patent number: 8871967
    Abstract: The present invention relates to some perfuming ingredients which are esters of formula (I) wherein R1 and R2 represent each a hydrogen atom or a methyl or ethyl group; and R3 represents a C5-C8 group of formula satured or unsatured linear, branched or cyclic group.
    Type: Grant
    Filed: October 15, 2010
    Date of Patent: October 28, 2014
    Assignee: Firmenich SA
    Inventors: Peter Fankhauser, Umberto Maddalena
  • Publication number: 20140288230
    Abstract: The present invention provides methylene beta-ketoester monomers, methods for producing the same, and compositions and products formed therefrom. In the method for producing the methylene beta-ketoesters of the invention, a beta-ketoester is reacted with a source of formaldehyde in a modified Knoevenagel reaction optionally in the presence of an acidic or basic catalyst, and optionally in the presence of an acidic or non-acidic solvent, to form reaction complex. The reaction complex may be an oligomeric complex. The reaction complex is subjected to further processing, which may be vaporization by contact with an energy transfer means in order to isolate the beta-ketoester monomer. The present invention further compositions and products formed from methylene beta-ketoester monomers of the invention, including monomer-based products (e.g., inks, adhesives, coatings, sealants or reactive molding) and polymer-based products (e.g., fibers, films, sheets, medical polymers, composite polymers and surfactants).
    Type: Application
    Filed: October 18, 2012
    Publication date: September 25, 2014
    Inventors: Bernard M. Malofsky, Adam G. Malofsky, Tanmoy Dey
  • Publication number: 20140213817
    Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
    Type: Application
    Filed: April 7, 2014
    Publication date: July 31, 2014
    Applicant: Nihon-Medi-Physics Co., Ltd.
    Inventors: Osamu ITO, Akio Hayashi, Fumie Kurosaki, Masahito Toyama, Toshiyuki Shinmura, Arinori Harano
  • Patent number: 8758724
    Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
    Type: Grant
    Filed: November 28, 2006
    Date of Patent: June 24, 2014
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Osamu Ito, Akio Hayashi, Fumie Kurosaki, Masahito Toyama, Toshiyuki Shinmura, Arinori Harano
  • Patent number: 8728978
    Abstract: Suggested are biocide compositions, comprising (a) esters based on ketocarboxylic acids, (b) biocides, and optionally (c) oil components or co-solvents and/or (d) emulsifiers. The compositions exhibit an improved stability even if stored at temperatures between 5° and 40° C. over a longer period.
    Type: Grant
    Filed: August 24, 2010
    Date of Patent: May 20, 2014
    Assignee: Cognis IP Management GmbH
    Inventors: Joaquin Bigorra Llosas, Stéphanie Merlet, Ramon Valls, Stefan Busch
  • Publication number: 20130345468
    Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F]FACBC) PET agent, ensuring that the reaction efficiently goes to completion.
    Type: Application
    Filed: March 7, 2012
    Publication date: December 26, 2013
    Inventors: Steven Michael Fairway, Marit Rolandsgard
  • Publication number: 20130331446
    Abstract: The invention relates to compounds of general formula I, (I), wherein R is wherein R is aryl substituted by R3; or R is (C3-Ci3)-cycloalkyl, (C3-Ci3)-cycloalkenyl or (C7-Ci3)-cycloalkynyl optionally substituted by R4; and pharmaceutically acceptable salts, hydrates, or solvates thereof, for use—alone or in combination with one or more other pharmaceutically active compounds—in therapy, for preventing, treating or ameliorating diseases or conditions responsive to stimulation of neutrophil oxidative burst, responsive to stimulation of keratinocyte IL-8 release or responsive to induction of necrosis.
    Type: Application
    Filed: December 22, 2011
    Publication date: December 12, 2013
    Applicant: LEO LABORATORIES LIMITED
    Inventors: Gunnar Grue-Sørensen, Xifu Liang, Thomas Högberg, Kristoffer Månsson, Per Vedsø
  • Publication number: 20130267730
    Abstract: The invention relates to a process for preparation of radiopharmaceutical precursors, and in particular protected amino acid derivatives which are used as precursors for production of radiolabelled amino acids for use in vivo imaging procedures such as positron emission tomography (PET). Particularly, the invention relates to a process for preparation of a precursor useful in the preparation of the [18F]-1-amino-3-fluorocyclobutanecarboxylic acid ([18F] FACBC) PET tracer.
    Type: Application
    Filed: December 19, 2011
    Publication date: October 10, 2013
    Applicant: GE HEALTHCARE LIMITED
    Inventors: Anne Nilsen, Sondre Nilsen
  • Patent number: 8541613
    Abstract: There is provided a process for producing an amide compound having an excellent harmful arthropod-controlling activity and represented by the formula (3): wherein R1, R2 and R3 independently represent a C1-C6 alkyl group optionally substituted with at least one halogen atom etc., R4, R5, R6 and R7 independently represent a halogen atom etc.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: September 24, 2013
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Yoshihiko Nokura, Hiroshi Ikegami, Markus Jachmann
  • Publication number: 20130165658
    Abstract: This invention is directed to a process for the preparation of high yield alkyl or aryl iodide from its corresponding carboxylic acid using N-iodo amides.
    Type: Application
    Filed: June 9, 2011
    Publication date: June 27, 2013
    Inventors: Gennady Nisnevich, Mark Gandelman, Kseniya Kulbitski
  • Publication number: 20130065969
    Abstract: A compound of formula (I) wherein R1 and R2 are independently selected from hydrogen, methyl, ethyl, propyl and isopropyl; or R1 and R2 together form a saturated or monounsaturated 5- or 6-membered hydrocarbon ring, as represented by the arcuate dotted line; R3 is selected from methyl and ethyl; R4 is selected from methyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, isobutyl, cyclobutyl and cyclopentyl; R5 is selected from hydrogen and methyl, and the dotted line between positions 3? and 4? represents an optional double bond. The compounds have a musk odour and are useful in fine and functional fragrances.
    Type: Application
    Filed: September 10, 2010
    Publication date: March 14, 2013
    Inventors: Philip Kraft, Urs Mueller
  • Patent number: 8288581
    Abstract: Process for the preparation of compounds of formula (IV): wherein R1-R6 are as defined in the specification. Application in the synthesis of ivabradine, addition salts thereof with a pharmaceutically acceptable acid and hydrates thereof.
    Type: Grant
    Filed: December 30, 2011
    Date of Patent: October 16, 2012
    Assignees: Les Laboratoires Servier, Centre National de la Recherche Scientifique
    Inventors: Jean-Louis Peglion, Olivier Baudoin, Nicolas Audic, Manon Chaumontet, Riccardo Piccardi
  • Patent number: 8269035
    Abstract: A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1): (wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.
    Type: Grant
    Filed: December 16, 2008
    Date of Patent: September 18, 2012
    Assignee: Nihon Medi-Physics Co., Ltd.
    Inventors: Fumie Kurosaki, Masahito Toyama, Akio Hayashi
  • Publication number: 20120195844
    Abstract: The present invention relates to some perfuming ingredients which are esters of formula (I) wherein R1 and R2 represent each a hydrogen atom or a methyl or ethyl group; and R3 represents a C5-C8 group of formula satured or unsatured linear, branched or cyclic group.
    Type: Application
    Filed: October 15, 2010
    Publication date: August 2, 2012
    Applicant: Firmenich SA
    Inventors: Peter Fankhauser, Umberto Maddalena
  • Patent number: 8232360
    Abstract: The invention relates to stereoregular ROMP polymers, the monomers used to make them, and the processes used to convert the monomers to the polymers.
    Type: Grant
    Filed: July 17, 2007
    Date of Patent: July 31, 2012
    Assignee: Research Foundation of State University of N.Y.
    Inventors: Nicole S. Sampson, Kathlyn A. Parker
  • Publication number: 20120184630
    Abstract: A compound of formula (I) wherein R1 and R2 are independently selected from hydrogen, methyl, ethyl, propyl and isopropyl; or R1 and R2 together form a saturated or monounsaturated 5- or 6-membered hydrocarbon ring, as represented by the arcuate dotted line; R3 is selected from methyl and ethyl; R4 is selected from methyl, ethyl, propyl, isopropyl, cyclopropyl, butyl, isobutyl, cyclobutyl and cyclopentyl; R5 is selected from hydrogen and methyl, and the dotted line between positions 3? and 4? represents an optional double bond. The compounds have a musk odour and are useful in fine and functional fragrances.
    Type: Application
    Filed: September 10, 2010
    Publication date: July 19, 2012
    Inventors: Philip Kraft, Urs Mueller
  • Publication number: 20110251363
    Abstract: The invention relates to stereoregular ROMP polymers, the monomers used to make them, and the processes used to convert the monomers to the polymers.
    Type: Application
    Filed: July 17, 2007
    Publication date: October 13, 2011
    Inventors: Nicole S. Sampson, Kathlyn A. Parker
  • Publication number: 20110218204
    Abstract: The present invention relates to certain novel salts of Betulinic acid derivatives, to process for preparing such compounds, to use the compounds in treating diseases or disorders mediated by HIV infection, to methods for their therapeutic use and to pharmaceutical compositions containing them.
    Type: Application
    Filed: January 10, 2011
    Publication date: September 8, 2011
    Applicant: HETERO RESEARCH FOUNDATION, HETERO DRUGS LIMITED
    Inventors: Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY
  • Publication number: 20110015196
    Abstract: The invention relates to novel lupeol-type triterpene derivatives and related compounds, and pharmaceutical compositions useful for therapeutic treatment of viral diseases and particularly HIV mediated diseases.
    Type: Application
    Filed: July 2, 2010
    Publication date: January 20, 2011
    Applicant: HETERO RESEARCH FOUNDATION
    Inventors: Bandi PARTHASARADHI REDDY, Vedula MANOHAR SHARMA, Kura RATHNAKAR REDDY, Musku MADHANMOHAN REDDY, Nelli YELLA REDDY, Lanka VL SUBRAHMANYAM
  • Publication number: 20100261931
    Abstract: A process for production of a radioactive fluorine-labeled organic compound is provided which can improve the yield of radioactive fluorination. Provided is a process in which a compound represented by the following formula (1): (wherein R1 is a straight or branched alkyl chain with 1-10 carbon atoms or an aromatic substituent, R2 is a straight or branched haloalkylsulfonic acid substituent with 1-10 carbon atoms, a straight or branched alkylsulfonic acid substituent with 1-10 carbon atoms, a fluorosulfonic acid substituent or an aromatic sulfonic acid substituent, and R3 is a protective group) is heated under stirring in an inert organic solvent in a presence of a phase transfer catalyst, 18F ions and potassium ions, so as to effect labeling with a radioactive fluorine, wherein the heating temperature is 40-90° C., and the concentration of the phase transfer catalyst in the inert organic solvent is 70 mmol/L or more. Preferably, the molar ratio of the phase transfer catalyst is 0.
    Type: Application
    Filed: December 16, 2008
    Publication date: October 14, 2010
    Applicant: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Fumie Kurosaki, Masahito Toyama, Akio Hayashi
  • Publication number: 20100249229
    Abstract: It is intended to provide a bicyclic ?-amino acid derivative having excellent activity as an ?2? ligand. The present invention provides a compound represented by the general formula (I): wherein R1, R2, R2?, R4, R5, R6, R7, R8, and R8? are a hydrogen atom or the like; and R3 is a hydrogen atom, a halogen atom, a C1-C6 alkyl group, or the like.
    Type: Application
    Filed: February 26, 2010
    Publication date: September 30, 2010
    Inventors: KOUSEI SHIMADA, ASUKA KAWAMURA, NAOHISA ARAKAWA, YUKI DOMON
  • Patent number: 7790916
    Abstract: The present invention relates to certain carbocyclic and oxacarbocyclic fumaric acid oligomers and the use thereof for preparing a pharmaceutical preparation as well of pharmaceutical preparations containing these compounds.
    Type: Grant
    Filed: April 3, 2003
    Date of Patent: September 7, 2010
    Assignee: Biogen Idec International GmbH
    Inventors: Rajendra Kumar Joshi, Hans-Peter Strebel
  • Publication number: 20100120907
    Abstract: Provided are topical formulations comprising an Amyris alcohol and/or ester derivatives of Amyris alcohol which may be used for the treatment of diseases including herpes virus infection (e.g., HSV-1, HSV-2), epidermoid carcinoma, cold sores, and human papillomavirus. Amyris alcohols contemplated for use with the present invention include valerianol, beta-eudesmol, epi-gamma-eudesmol, elemol, alpha-eudesmol, and ester derivatives thereof.
    Type: Application
    Filed: April 18, 2008
    Publication date: May 13, 2010
    Inventors: Chandra Ulagaraj Singh, Rao Jagaveerabhadra Nulu
  • Publication number: 20100113821
    Abstract: Disclosed is a process for preparing 3-(amino)-3-cyclobutylmethyl-2-hydroxy-propionamide hydrochloride, an intermediate useful in the preparation of the HCV protease inhibitor (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide.
    Type: Application
    Filed: December 17, 2007
    Publication date: May 6, 2010
    Applicant: Schering-Plough Corporation
    Inventors: Jeonghan Park, Eugene J. Vater, Shuan Dong, Tetsuo Iwama, Ramani R. Raghavan, Hong-Chang Lee, George S.k. Wong
  • Publication number: 20100016626
    Abstract: A process is provided for producing a labeled precursor which is useful for production of a radioactive fluorine-labeled amino acid compound. In the reaction step for introducing a leaving group to a mixture of syn-form and anti-form of FACBC, a base is allowed to present in the reaction system to produce a syn-leaving group adduct, which is unreactive with the base and is highly stable, and an anti-leaving group adduct which can react with the base to form a water-soluble compound. By employing a purification method utilizing such a difference in solubility, the syn-leaving group adduct can be separated selectively. The base may be a linear- or branched-chain primary to tertiary alkylamine having 1 to 10 carbon atoms, a nitrogen-containing heterocyclic compound with 2 to 20 carbon atoms, and a nitrogen-containing hetero aromatic compound with 2 to 20 carbon atoms.
    Type: Application
    Filed: December 17, 2007
    Publication date: January 21, 2010
    Applicant: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Masahito Toyama, Akio Hayashi
  • Patent number: 7550622
    Abstract: The invention relates to the field of pharmaceutics and more specifically to cycloalkylamidoacid compositions useful in the preparation of cycloalkyaminoacids and oxazolidinediones, and processes for making cycloamidoacids X and R are defined herein.
    Type: Grant
    Filed: August 12, 2004
    Date of Patent: June 23, 2009
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Isabelle Gallou, Nizar Haddad, Chris Senanayake, Xudong Wei, Jinghua Xu
  • Patent number: 7524885
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, I, m and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: February 23, 2005
    Date of Patent: April 28, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C Vederas, Jason R. Dyck
  • Publication number: 20090012318
    Abstract: A process which comprises reacting a 1,2,3,4-cyclobutanetetracarboxylic-1,2:3,4-dianhydride [1] with an alcohol [2] in the presence of an acid catalyst to obtain a compound [3], isomerizing the compound [3] with a base catalyst into a compound [4], reacting the compound [4] with an organic acid to obtain a compound [5], and reacting the compound [5] with a dehydrating agent to obtain a 1,2,3,4-cyclobutanetetracarboxylic-1,3:2,4-dianhydride: wherein R1 and R2 are each independently hydrogen, halogeno, alkyl of 1 to 10 carbon atoms, halogenated alkyl of 1 to 10 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, phenyl, or cyano; and R3 is alkyl of 1 to 10 carbon atoms.
    Type: Application
    Filed: October 18, 2005
    Publication date: January 8, 2009
    Inventors: Hideo Suzuki, Takayuki Tamura
  • Patent number: 7473706
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, i and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: March 6, 2006
    Date of Patent: January 6, 2009
    Assignee: The Governors of the University of Alberta
    Inventors: Gary D. Lopaschuk, John C. Vederas, Jason R. Dyck
  • Publication number: 20080281121
    Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.
    Type: Application
    Filed: November 28, 2006
    Publication date: November 13, 2008
    Applicant: NIHON MEDI-PHYSICS CO., LTD.
    Inventors: Osamu Ito, Akio Hayashi, Fumie Kurosaki, Masahito Toyama, Toshiyuki Shinmura, Arinori Harano
  • Publication number: 20080249166
    Abstract: The present invention relates to novel cycloalkyl-hydroxyl compounds, compositions comprising hydroxyl compounds, and methods useful for treating and preventing a variety of diseases and conditions such as, but not limited to aging, Alzheimer's Disease, cancer, cardiovascular disease, diabetic nephropathy, diabetic retinopathy, a disorder of glucose metabolism, dyslipidemia, dyslipoproteinemia, hypertension, impotence, inflammation, insulin resistance, lipid elimination in bile, obesity, oxysterol elimination in bile, pancreatitis, Parkinson's disease, a peroxisome proliferator activated receptor-associated disorder, phospholipid elimination in bile, renal disease, septicemia, Syndrome X, thrombotic disorder. Compounds and methods of the invention can also be used to modulate C reactive protein or enhance bile production in a patient.
    Type: Application
    Filed: June 9, 2008
    Publication date: October 9, 2008
    Applicant: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Daniela Carmen Oniciu
  • Patent number: 7402693
    Abstract: The invention provides a cyclobutanetetracarboxylate compound of general formula (I) and a preparation method thereof: in which R and R1 are as defined in the specification.
    Type: Grant
    Filed: August 2, 2007
    Date of Patent: July 22, 2008
    Assignee: Daxin Material Corporation
    Inventors: Ming-Chih Lai, Chia-Wen Chang, Chi-Wi Ong
  • Patent number: 7390779
    Abstract: Odourant compounds selected from compounds having the structure: wherein, R1 and R2 may be independently hydrogen or methyl, and n is an integer 1, 2 or 3 provided that n+ the carbon atoms in R1 and R2 is less than 5, their preparation and their use in fine fragrances and perfume components, wherein the compounds provide a musk characteristic.
    Type: Grant
    Filed: May 30, 2002
    Date of Patent: June 24, 2008
    Assignee: Givaudan SA
    Inventors: Philip Kraft, Riccardo Cadalbert
  • Patent number: 7122678
    Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
    Type: Grant
    Filed: March 11, 2005
    Date of Patent: October 17, 2006
    Assignee: Warner-Lambert Company
    Inventors: Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
  • Patent number: 7084173
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia wherein W is C1–C6 alkyl, halogen, or aryl; Cyc is C3 or C4 cycloalkyl; p is 0–3 for Cyc being C4 cycloalkyl and p=0–2 for Cyc being C3 cycloalkyl; Y is O, S, or NR, where R?H, alkyl or aryl; X is O, S, NR, or CR3R4; Z is H, alkyl, cycloalkyl, aryl or (cyclo)alkylcarbonyl; R1 is H, alkyl, aryl or O; R2 is H, alkyl or aryl; R3 and R4 are, independently, H, alkyl or aryl; and n is an integer from 1 to 10; or a pharmaceutically acceptable salt, ester or prodrug thereof.
    Type: Grant
    Filed: April 1, 2002
    Date of Patent: August 1, 2006
    Assignee: The Governors of the Univerity of Alberta
    Inventors: Gary D. Lopaschuk, John Christopher Vederas, Jason R. Dyck
  • Patent number: 7074828
    Abstract: The invention provides novel compounds of the Formula (I) that stimulate rates of glucose oxidation in myocardial cells: wherein W, Cyc, p, Y, X, Z, R, R1, R2, R3, R4, i and n are as defined for Formula (I) herein. The invention also relates to pharmaceutical compositions comprising compounds capable of stimulation of glucose oxidation, methods for increasing glucose oxidation rates in myocardial cells, and methods of treatment of myocardial ischemia.
    Type: Grant
    Filed: December 5, 2002
    Date of Patent: July 11, 2006
    Assignee: The Governors of the University of Alberta
    Inventors: Gary David Lopaschuk, John Christopher Vederas, Jason Roland Dyck
  • Patent number: 6965049
    Abstract: Provided is a zwitterionic lipid compound represented by formula (I) given below: In formula (I), m and n are independently integers of 1 to 4, p is an integer of 7 to 21, one R is NH3+, and each other R is H.
    Type: Grant
    Filed: February 23, 2004
    Date of Patent: November 15, 2005
    Assignee: Oxygenix Co., Ltd.
    Inventors: Eishun Tsuchida, Shinji Takeoka, Keitaro Sou, Katsura Mori
  • Patent number: 6909014
    Abstract: The present invention relates to novel ether compounds, compositions comprising ether compounds, and methods useful for treating and preventing cardiovascular diseases, dyslipidemias, dysproteinemias, and glucose metabolism disorders comprising administering a composition comprising an ether compound. The compounds, compositions, and methods of the invention are also useful for treating and preventing Alzheimer's Disease, Syndrome X, peroxisome proliferator activated receptor-related disorders, septicemia, thrombotic disorders, obesity, pancreatitis, hypertension, renal disease, cancer, inflammation, and impotence. In certain embodiments, the compounds, compositions, and methods of the invention are useful in combination therapy with other therapeutics, such as hypocholesterolemic and hypoglycemic agents.
    Type: Grant
    Filed: September 5, 2003
    Date of Patent: June 21, 2005
    Assignee: Esperion Therapeutics, Inc.
    Inventors: Jean-Louis Henri Dasseux, Carmen Daniela Oniciu
  • Patent number: 6878723
    Abstract: The invention concerns compounds inhibiting LTA4 hydrolase of formula (I). The invention also concerns their therapeutic, in particular anti-inflammatory, applications.
    Type: Grant
    Filed: April 6, 2000
    Date of Patent: April 12, 2005
    Assignees: Institut National de la Sante et de la rescherche Medicale (INSERM), Bioprojet
    Inventors: Denis Danvy, Thierry Monteil, Jean-Christophe Plaquevent, Pierre Duhamel, Lucette Duhamel, Nadine Noel, Claude Gros, Olivier Chamard, Jean-Charles Schwartz, Jeanne-Marie Lecomte, Serge Piettre
  • Patent number: 6858650
    Abstract: The present invention concerns highly pure, crystalline, stable compounds of novel derivatives of 3,3-diphenylpropylamines in the form of their salts, a method for the manufacture and highly pure, stable intermediate products. The method is in particular characterized by regio- and chemoselectivity and high yield. Salts of phenolic monoesters of 3,3-diphenylpropylamines are provided, that are particularly well-suited for use in pharmaceutical formulations. Preferred compounds are R-(+)-2-(3-diisopropylamino-1-phenyl-propyl)-4-hydroxymethylphenylisobutyrate ester hydrogen fumarate and R-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenylisobutyrate ester hydrochloride hydrate. Furthermore, stable, crystalline intermediate products that are essential for obtaining the abovementioned salts are provided. A preferred intermediate product is R-(?)-3-(3-diisopropylamino-phenyl-propyl)-4-hydroxy-benzoic acid methyl ester.
    Type: Grant
    Filed: November 15, 2000
    Date of Patent: February 22, 2005
    Assignee: Schwarz Pharma AG
    Inventor: Claus Meese
  • Publication number: 20040234568
    Abstract: Odourant compounds selected from cycloalkanecarboxylic acid esters of 2-[1-(3,3-dimethylcyclohexyl)ethoxy]-2-methylpropan-1-ol, their preparation and their use as ingredients in fine-fragrances and functional perfumery compositions.
    Type: Application
    Filed: June 14, 2004
    Publication date: November 25, 2004
    Inventors: Philip Kraft, Riccardo Cadalbert
  • Patent number: 6753443
    Abstract: The present invention relates to a process for preparing a chiral ester according to the formula (100): by reacting (i) a racemic alcohol, (ii) a selected ruthenium complex to activate racemization of the racemic alcohol, (iii) a lipase to selectively acylate one enantiomer of the racemic alcohol, and (iv) an acyl donor compound to supply an acyl group to the lipase.
    Type: Grant
    Filed: March 2, 2001
    Date of Patent: June 22, 2004
    Assignees: Samsung Fine Chemicals Co., Ltd., Pohang University of Science and Technology
    Inventors: Jai Wook Park, Mahn-Joo Kim, Jeong Hwan Koh, Hyun Min Jung
  • Patent number: 6750363
    Abstract: An efficient and selective process, capable of scale-up, to make itaconate derivatives of formula (IV), and/or succinate derivatives of formula (V) and/or (VI) by asymmetric hydrogenation of the itaconate derivatives. wherein R, R1 and R2 are as defined herein.
    Type: Grant
    Filed: July 18, 2002
    Date of Patent: June 15, 2004
    Assignee: Pfizer, Inc.
    Inventors: Andrew Michael Derrick, Nicholas Murray Thomson
  • Patent number: 6734320
    Abstract: Novel non-symmetric, partially fluorinated compositions and method of manufacture which are useful as lubricants or as additives to lubricant formulations involving the molecular structure: R1f—F′—R2—F″—R3h where R1f represents a wholly or partially fluorinated organic residue end group, F′ and F″ represent functional linkages which may be alike or different, R2 represents the backbone and R3h represents a non-fluorinated organic residue end group. Such compositions are produced by reacting a mixture of alcohols, mercaptans or amines containing at least one partially fluorinated compound and at least one non-fluorinated compound in the mixture, thus producing the R1f and the R3h residues, with a difunctional organic compound (e.g., diacid, dinitrile, disulfonyl halide, diisocyanate, diisothiocyanate, diphosphoryl halide or dithiophosphoryl halide).
    Type: Grant
    Filed: April 30, 2002
    Date of Patent: May 11, 2004
    Assignee: E. I. du Pont de Nemours and Company
    Inventor: Richard P. Beatty
  • Publication number: 20030220397
    Abstract: The invention is a novel series of cyclic amino acids which are useful in the treatment of epilepsy, faintness attacks, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, gastrointestinal disorders such as irritable bowel syndrome (IBS), and inflammation, especially arthritis. A pharmaceutical composition containing a compound of the invention as well as methods of preparing the compounds and novel intermediates useful in the preparation of the final compounds are included.
    Type: Application
    Filed: May 30, 2003
    Publication date: November 27, 2003
    Inventors: Justin Stephen Bryans, David Christopher Horwell, Andrew John Thorpe, David Juergen Wustrow, Po-Wai Yuen
  • Patent number: 6423865
    Abstract: The invention relates to compounds with the general formula Y1—A1—M1—A2—Y2 wherein Y1 and Y2 are different from each other and Y1 is an acrylate or methacrylate residue and Y2 is a vinyl ether, epoxy, or azide residue, A1 and A2 are identical or different residues with the general formula CnH2n in which n is a whole number from 0 to 20 and one or more methylene groups can be replaced by oxygen atoms, and M1 has the general formula —R1—X1—R2—X2—R3—X3—R4— wherein R1, R2, R3, and R4 are identical or different doubly bonded residues from the group —O—, —COO—, —CONH—, —CO—, —S—, —C≡C—, —CH═CH—, —CH═N—, —CH2—, —N═N—, and —N═N(O)—, and R2—X2—R3 can also be a C—C bond, and X1, X2, and X3 are identical or different residues from the group 1,4-phenylene, 1,4-cyclohexylen
    Type: Grant
    Filed: March 1, 2000
    Date of Patent: July 23, 2002
    Assignee: DaimlerChrysler AG
    Inventors: Peter Strohriegl, Katja Strelzyk, Andreas Stohr, Petra Grundig, Michael Gailberger, Fritz Dannenhauer, Anne Barth