Cyclohexyl Ring Containing Patents (Class 564/462)
  • Patent number: 10759743
    Abstract: Pd(II)-catalyzed g-G(sp3)-H arylation or heteroarylation of primary amines is realized by using 2-hydroxynicotinaldehyde as a catalytic transient directing group. Importantly, the catalyst and the directing group loading can be lowered to 2% and 4% respectively, thus demonstrating high efficiency of this newly designed transient directing group. Heterocyclic aryl iodides are also compatible with this reaction. Furthermore, swift synthesis of 1,2,3,4-tetrahydronaphthyridine derivatives is accomplished using this reaction.
    Type: Grant
    Filed: October 19, 2017
    Date of Patent: September 1, 2020
    Assignee: THE SCRIPPS RESEARCH INSTITUTE
    Inventor: Jin-Quan Yu
  • Patent number: 10159674
    Abstract: A compound, or a pharmaceutically acceptable salt or ester thereof, having a structure of: wherein X is a divalent linking moiety; and R1-R10 are each individually H, optionally-substituted alkyl, optionally-substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, halogen, amino, or hydroxy, provided that at least one of R3 or R8 is an optionally-substituted alkyl, a substituted alkoxy, optionally-substituted aryl, optionally-substituted cycloalkyl, optionally-substituted heterocyclic, or halogen.
    Type: Grant
    Filed: April 25, 2016
    Date of Patent: December 25, 2018
    Assignees: University of Pittsburgh—Of the Commonwealth System of Higher Education, The United States of America as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama K. Mallampalli
  • Publication number: 20150114884
    Abstract: Treatment compositions for neutralizing acidic species and reducing hydrochloride and amine salts in a fluid hydrocarbon stream are disclosed. The treatment compositions may comprise at least one amine with a salt precipitation potential index of equal to or less than about 1.0. Methods for neutralizing acidic species and reducing deposits of hydrochloride and amine salts in a hydrocarbon refining process are also disclosed. The methods may comprise providing a fluid hydrocarbon stream and adding a treatment composition to the fluid hydrocarbon stream. The treatment compositions used may have a salt precipitation potential index of equal to or less than about 1.0 and comprise either water-soluble or oil-soluble amines.
    Type: Application
    Filed: October 31, 2013
    Publication date: April 30, 2015
    Applicant: General Electric Company
    Inventors: Alagarsamy Subbiah, Rebika Mayanglambam Devi, Nimeshkumar Kantilal Patel, Muthukumar Nagu, Rhomit Ghosh, Sathees Kesavan, Ashok Shankar Shetty, Manish Joshi
  • Patent number: 8877814
    Abstract: The present invention relates to a titration scheme for the administration of a 1-amino-alkylcyclohexane derivative which allows for quick attainment of an effective dose of a 1-amino-alkylcyclohexane derivative while minimizing side effects. The present invention further relates to a titration package for providing a 1-amino-alkylcyclohexane derivative (e.g., neramexane or a pharmaceutically acceptable salt thereof) in at least two different dosages. The present titration scheme/titration package may be useful in the treatment of various diseases, including tinnitus.
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: November 4, 2014
    Assignee: Merz Pharma GmbH & Co. KGaA
    Inventors: Barbara Ellers-Lenz, Tanja Rosenberg, Erhard Seiller, Hagen Kruger, Michael Althaus
  • Patent number: 8846645
    Abstract: The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic.
    Type: Grant
    Filed: December 13, 2011
    Date of Patent: September 30, 2014
    Assignees: Rheinische Friedrich-Wilhelms Universität Bonn, Universität Konstanz
    Inventors: Günter Mayer, Christina Elsbeth Luense, Valentin Wittmann, Magnus S. Schmidt
  • Patent number: 8835689
    Abstract: The invention relates to compounds that have an affinity to the ?-opioid receptor and the ORL 1-receptor, methods for their production, medications containing these compounds and the use of these compounds for the treatment of pain and other conditions.
    Type: Grant
    Filed: April 24, 2012
    Date of Patent: September 16, 2014
    Assignee: Grünenthal GmbH
    Inventors: Bert Nolte, Wolfgang Schröder, Klaus Linz, Werner Englberger, Hans Schick, Heinz Graubaum, Birgit Roloff, Sigrid Ozegowski, József Bálint, Helmut Sonnenschein
  • Publication number: 20140200345
    Abstract: Provided is a method for producing a 2-alkenylamine compound efficiently and at low cost, using a primary or secondary amine compound and a 2-alkenyl compound as the starting materials therefor. The 2-alkenyleamine compound is produced by 2-alkenylating a primary or secondary amine compound, using a specified 2-alkenylating agent and in the presence of a catalyst comprising a complexing agent and a transition metal precursor stabilized by a monovalent anionic five-membered conjugated diene.
    Type: Application
    Filed: August 29, 2012
    Publication date: July 17, 2014
    Applicants: NATIONAL UNIV. CORP. NAGOYA UNIVERSITY, SHOWA DENKO K.K.
    Inventors: Yoshitaka Ishibashi, Naoya Fukumoto, Masato Kitamura
  • Patent number: 8759581
    Abstract: Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, an intermediate in the synthesis of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof, comprising step (iii): (iii) reacting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane with chloroacetonitrile in the presence of an acid, wherein 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane is employed in step (iii) as obtained in the reaction of a methylmagnesium halide with 3,3,5,5-tetramethylcyclohexanone without having been subjected to a purification step.
    Type: Grant
    Filed: June 28, 2010
    Date of Patent: June 24, 2014
    Assignee: Merz Pharma GmbH & Co. KGaA
    Inventors: Herbert Koller, Michael Pyerin
  • Publication number: 20140130714
    Abstract: Provided are aminoalcohol compounds for use as additives for paints and coatings. The compounds are of the formula (I): wherein x, R, R1, R2, R3, R4, R5, R6, and RA are as defined herein.
    Type: Application
    Filed: July 23, 2012
    Publication date: May 15, 2014
    Applicants: ANGUS CHEMICAL COMPANY, DOW GLOBAL TECHNOLOGIES LLC
    Inventors: Asghar Peera, Raymond J. Swedo, G. David Green, Esin G. Busche, John W. Quinn, Shreyas Bhide, Mahesh Sawant
  • Publication number: 20140107328
    Abstract: Chemoselective isolation of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds is accomplished via formation of polymeric siloxyl ethers. Chemoselective release of aliphatic hydroxyl group-containing and aromatic hydroxyl group-containing compounds from polymeric siloxyl reagents is described.
    Type: Application
    Filed: December 11, 2013
    Publication date: April 17, 2014
    Inventors: Erin E. CARLSON, Darci TRADER
  • Patent number: 8692021
    Abstract: Method of preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane or a pharmaceutically acceptable salt thereof (Neramexane), comprising step (iv): (iv) hydrolyzing a mixture comprising an acid, 1-formamido-1,3,3,5,5-pentamethylcyclohexane and hydrogen cyanide to yield 1-amino-1,3,3,5,5-pentamethylcyclohexane.
    Type: Grant
    Filed: September 24, 2010
    Date of Patent: April 8, 2014
    Assignee: Merz Pharma GmbH & Co. KGaA
    Inventors: Markus-Rene Gold, Valerjans Kauss, Aigars Jirgensons
  • Patent number: 8686189
    Abstract: The invention is directed to a process for producing intermediates of a compound which exhibits an activated blood coagulation factor Xa inhibitory action and which is a useful preventive and a therapeutic agent for thrombotic diseases. The intermediate production process is represented by the following reaction scheme.
    Type: Grant
    Filed: September 15, 2006
    Date of Patent: April 1, 2014
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Koji Sato, Kotaro Kawanami, Tsutomu Yagi
  • Publication number: 20140066409
    Abstract: The present invention relates to compounds according to general formula (I), pharmaceutical compositions comprising compounds according to general formula (I) and the use of the compounds for the treatment of a bacterial infection, particularly for use as an antibiotic.
    Type: Application
    Filed: December 13, 2011
    Publication date: March 6, 2014
    Applicants: UNIVERSITÄT KONSTANZ, RHEINISCHE FRIEDRICH-WILHELMS UNIVERSITÄT BONN
    Inventors: Günter Mayer, Christina Elsbeth Luense, Valentin Wittmann, Magnus S. Schmidt
  • Publication number: 20140041062
    Abstract: The present disclosure relates to an ASD genetically engineered model carrying a deletion of Shank2 gene and having reduced NMDA receptor function. According to the present disclosure, genetically engineered mice that show the clinical features of ASD due to the deletion of the Shank2 gene can be obtained, and the genetically engineered mice can be effectively used to screen candidate therapeutic agents.
    Type: Application
    Filed: August 2, 2013
    Publication date: February 6, 2014
    Applicants: Industry-Academic Cooperation Foundation, Yonsei University, Korea Advanced Institute of Science and Technology, Seoul National University R&DB Foundation
    Inventors: Min Goo Lee, Bong Kiun Kaang, Eunjoon Kim
  • Publication number: 20130310245
    Abstract: The present invention is directed to a process for the production of high density polyethylene by polymerisation of ethylene in the presence of a supported chromium oxide based catalyst which is modified with an organic compound comprising oxygen and a nitrogen atom which is selected from the group consisting of saturated heterocyclic organic compounds with a five or six membered ring, amino esters and amino alcohols. Such organic compounds allow manufacturing of HDPE with increases molecular weight distribution and increased molecular weight.
    Type: Application
    Filed: October 4, 2011
    Publication date: November 21, 2013
    Applicant: SAUDI BASIC INDUSTRIES CORPORATION
    Inventors: Vugar O. Aliyev, Ali Saad Headan, Jaiprakash Brijal Sainani
  • Patent number: 8586794
    Abstract: The present invention relates to 5-isopropyl-3-aminomethyl-2-methyl-1-aminocyclohexane (carvonediamine) and to a process for preparation thereof by a) reacting carvone with hydrogen cyanide, b) then reacting the carvonenitrile obtained in stage a) with ammonia in the presence of an imine formation catalyst and c) then reacting the carvonenitrile imine-containing reaction mixture obtained in stage b) with hydrogen and ammonia over hydrogenation catalysts. The present invention further relates to the use of carvonediamine as a hardener for epoxy resins, as an intermediate in the preparation of diisocyanates, as a starter in the preparation of polyetherols and/or as a monomer for polyamide preparation.
    Type: Grant
    Filed: July 13, 2009
    Date of Patent: November 19, 2013
    Assignee: BASF SE
    Inventors: Martin Ernst, Alfred Oftring, Kathrin Wissel-Stoll, Oemer Uensal, Stephan Freyer, Ansgar Gereon Altenhoff, Wolfgang Staffel
  • Patent number: 8545783
    Abstract: There is provided an acid gas absorbent having excellent performance of absorbing acid gas such as carbon dioxide, and an acid gas removal device and an acid gas removal method using the acid gas absorbent. An acid gas absorbent of an embodiment contains at least one type of tertiary amine compound represented by the following general formula (1). (In the above formula (1), the cycle A represents a cyclic structure whose carbon number is not less than 3 nor more than 8. R1, R2 and R3 each represent an alkyl group whose carbon number is 1 to 4, and R4 represents a hydroxyalkyl group. R1 and R2 are groups coupled to carbon atoms adjacent to a carbon atom forming the cycle A and coupled to a nitrogen atom.
    Type: Grant
    Filed: May 18, 2012
    Date of Patent: October 1, 2013
    Assignee: Kabushiki Kaisha Toshiba
    Inventors: Shinji Murai, Yukishige Maezawa, Yasuhiro Kato, Takehiko Muramatsu, Masatoshi Hodotsuka
  • Patent number: 8513442
    Abstract: Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods of performing asymmetric catalytic reactions are also described that include (a) combining a first reactant, a second reactant, and a catalytic amount of a chiral hydrogen-bond donor in a solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form an enantiomeric excess of a reaction product. Reaction mixtures corresponding to these methods are also described.
    Type: Grant
    Filed: June 11, 2007
    Date of Patent: August 20, 2013
    Assignee: The University of Chicago
    Inventors: Viresh H. Rawal, Yong Huang, Aditya K. Unni, Avinash N. Thadani
  • Patent number: 8476043
    Abstract: Inhibitors of the soluble epoxide hydrolase (sEH) are provided that incorporate multiple pharmacophores and are useful in the treatment of diseases.
    Type: Grant
    Filed: December 4, 2009
    Date of Patent: July 2, 2013
    Assignee: The Regents of the University of California
    Inventors: Bruce D. Hammock, In-Hae Kim, Christophe Morisseau, Takaho Watanabe, John W. Newman
  • Publication number: 20130165682
    Abstract: The present invention relates to a method for the synthesis of an ? amino acetal, comprising (i) oxidizing a tertiary amine in the presence of a copper catalyst, at least one oxidant and a solvent, or (ii) reacting a secondary amine and an aliphatic aldehyde in the presence of a copper catalyst, at least one oxidant and a solvent.
    Type: Application
    Filed: July 6, 2011
    Publication date: June 27, 2013
    Applicant: NANYANG TECHNOLOGICAL UNIVERSITY
    Inventors: Teck Peng Loh, Jiesheng Tian
  • Publication number: 20130123541
    Abstract: Method of preparing 3,3,5,5-tetramethylcyclohexanone comprising step (i): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone in the presence of methylmagnesium chloride. The thus prepared 3,3,5,5-tetramethylcyclohexanone may be employed in a method of preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 16, 2013
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventors: Herbert Koller, Michael Pyerin, Federico Sbrogio
  • Patent number: 8436210
    Abstract: The present invention provides an amide compound having antibacterial activity, and a bacterial infection control agent for agricultural and horticultural use that contains the amide compound. The novel amide compound of the present invention is represented by General Formula (1): wherein R is a —CH(R1)(R2) or a —CO(R2) group, R1 is a hydrogen atom or a hydroxyl group, and R2 is a C1-12 alkyl group.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: May 7, 2013
    Assignees: The University of Tokyo, Otsuka Chemical Co., Ltd.
    Inventors: Hiroaki Suga, Jun Igarashi
  • Patent number: 8344180
    Abstract: Disclosed are compound having NPY Y5 receptor antagonistic activity of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is optionally substituted lower alkyl, R2 and R8 are each independently hydrogen or lower alkyl, X is optionally substituted cycloalkylene, or —NR2—X— may be a group of the formula: wherein a group of the formula: is piperidinediyl, piperazinediyl, pyridindiyl, pyrazinediyl, pyrrolidinediyl or pyrrolediyl, U is a bond, lower alkylene or lower alkenylene, Y is —OCONR7—, —CONR7— or —CSNR7—, R7 is hydrogen or lower alkyl, Z is optionally substituted carbocyclyl, or optionally substituted heterocyclyl, W is —S(?O)n-, n is 2, provided that Z is not carbocyclyl substituted with non-halogeno lower alkoxy, and provided that 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [2-[(5-chloro-1H-indole-2-carbonyl)-amino]-5 -(N?,N?-dimethyl-hydrazinocarbonyl)-cyclohexyl]-amide and 5-Methyl-4,5,6,7-tetrahydro-thiazolo[5,4-c]pyridine-2-carboxylic acid [
    Type: Grant
    Filed: August 28, 2007
    Date of Patent: January 1, 2013
    Assignee: Shionogi & Co., Ltd.
    Inventor: Naoki Kouyama
  • Publication number: 20120308451
    Abstract: There is provided an acid gas absorbent having excellent performance of absorbing acid gas such as carbon dioxide, and an acid gas removal device and an acid gas removal method using the acid gas absorbent. An acid gas absorbent of an embodiment contains at least one type of tertiary amine compound represented by the following general formula (1). (In the above formula (1), the cycle A represents acyclic structure whose carbon number is not less than 3 nor more than 8. R1, R2 and R3 each represent an alkyl group whose carbon number is 1 to 4, and R4 represents a hydroxyalkyl group. R1 and R2 are groups coupled to carbon atoms adjacent to a carbon atom forming the cycle A and coupled to a nitrogen atom.
    Type: Application
    Filed: May 18, 2012
    Publication date: December 6, 2012
    Inventors: Shinji MURAI, Yukishige Maezawa, Yasuhiro Kato, Takehiko Muramatsu, Masatoshi Hodotsuka
  • Publication number: 20120251449
    Abstract: The present invention claims fluoro- & iodo-containing aldehydes as ALDH substrates for use as diagnostic imaging agents or as therapeutic agents. The aldehydes are both directly and indirectly attached to an aromatic or a straight chain ring. ALDH activity was monitored either by the formation of acid-product or consumption of aldehyde substrates.
    Type: Application
    Filed: December 22, 2010
    Publication date: October 4, 2012
    Inventors: Vijaya Raj Kuniyil Kulangara, Alan Cuthbertson, Peter Iveson, Chitralekha Rangaswamy, Veena Rao, Rajiv Bhalla
  • Publication number: 20120178942
    Abstract: Processes useful for the preparation of a Compound of Formula I: Formula (I). Intermediates useful for the preparation of the compound of Formula I, and processes useful for preparing said intermediates are disclosed.
    Type: Application
    Filed: July 27, 2010
    Publication date: July 12, 2012
    Inventors: John Traverse, William M. Leong, Steven P. Miller, Jennifer Albaneze-Walker, Thomas J. Hunter, Lijun Wang, Hongbiao Liao, Ashok Arasappan, Scott T. Trzaska, Randi M. Smith, Azzeddine Lekhal, Stephane L. Bogen, Jianshe Kong, Frank Bennett, F. George Njoroge, Marc Poirier, Shen-Chun Kuo, Yonggang Chen, Kenneth S. Matthews, Patrice Demonchaux, Amadeo Ferreira
  • Patent number: 8212078
    Abstract: This invention provides aromatic diimines where the diimines have imino groups with at least two carbon atoms, and either are in the form of one benzene ring having two imino groups on the ring, which imino groups are meta or para relative to each other, and in which each position ortho to an imino group bears a hydrocarbyl group, or are in the form of two benzene rings connected by an alkylene bridge and having one imino group on each ring, and in which each position ortho to an imino group bears a hydrocarbyl group.
    Type: Grant
    Filed: December 30, 2005
    Date of Patent: July 3, 2012
    Assignee: Albemarle Corporation
    Inventors: John Y. Lee, Paul L. Wiggins, Judit Orgad, Mahmood Sabahi, Vernon O. Brandt, David W. Owens
  • Patent number: 8211945
    Abstract: Methods for stabilizing ?-galactosidase, stabilizing ?-glucocerebrosidase, treating a glycolipid metabolic disorder caused by mutation of ?-galactosidase gene, treating a glycolipid metabolic disorder caused by mutation of ?-glucocerebrosidase gene, regenerating the activity of ?-galactosidase, regenerating the activity of ?-glucosidase, treating GM1 gangliosidosis, Morquio-B or Krabbe's disease, and treating Gaucher's disease, include administering a carba-sugar amine derivative represented by the following formula (1) or (2):
    Type: Grant
    Filed: June 24, 2009
    Date of Patent: July 3, 2012
    Assignee: Seikagaku Corporation
    Inventors: Seiichiro Ogawa, Yoshiyuki Suzuki, Eiji Nanba, Junichiro Matsuda, Kousaku Ohno
  • Publication number: 20120165521
    Abstract: A method for producing a polyamino-polyalcohol. The method comprises steps of: (a) combining an aminoalcohol of formula (I) with a nitro-diol of formula (II) to produce a nitro amino diol; and (b) contacting the nitro amino diol with a reducing agent capable of reducing aliphatic nitro groups.
    Type: Application
    Filed: December 12, 2011
    Publication date: June 28, 2012
    Inventors: Ian A. Tomlinson, Asghar A. Peera
  • Publication number: 20120161071
    Abstract: An acid gas absorbent of which recovery amount of acid gas such as carbon dioxide is high, and an acid gas removal device and an acid gas removal method using the acid gas absorbent are provided. The acid gas absorbent of the embodiment comprising at least one type of tertiary amine compound represented by the following general formula (1). (In the above-stated formula (1), either one of the R1, R2 represents a substituted or non-substituted alkyl group of which carbon number is 2 to 5, and the other one represents a substituted or non-substituted alkyl group of which carbon number is 1 to 5. The R3 represents a methyl group or an ethyl group, and the R4 represents a hydroxyalkyl group. The R1, R2 may either be the same or different, and they may be coupled to form a cyclic structure.
    Type: Application
    Filed: December 20, 2011
    Publication date: June 28, 2012
    Inventors: Shinji MURAI, Yukishige Maezawa, Yasuhiro Kato, Takehiko Muramatsu, Satoshi Saito, Hiroko Watando, Naomi Shida, Reiko Yoshimura, Takashi Kuboki
  • Publication number: 20120130130
    Abstract: The method of producing a salt of 1-amino-1,3,3,5,5-pentamethylcyclohexane comprising steps (i) to (v): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone; (ii) converting 3,3,5,5-tetramethylcyclohexanone obtained in step (i) to 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane; (iii) converting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane obtained in step (ii) to 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane; (iv) converting 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane obtained in step (iii) to 1-amino-1,3,3,5,5-pentamethylcyclohexane; wherein at least one of 3,3,5,5-tetramethylcyclohexanone, 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane, 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, is not subjected to a purification step.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 24, 2012
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventors: Herbert Koller, Mchael Pyerin, Federico Sbrogio
  • Publication number: 20120130127
    Abstract: Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, an intermediate in the synthesis of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof, comprising step (iii): (iii) reacting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane with chloroacetonitrile in the presence of an acid, wherein 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane is employed in step (iii) as obtained in the reaction of a methylmagnesium halide with 3,3,5,5-tetramethylcyclohexanone without having been subjected to a purification step.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 24, 2012
    Applicant: MER PHARMA GmbH & CO. KGaA
    Inventors: Herbert Koller, Michael Pyerin
  • Publication number: 20120130131
    Abstract: The invention relates to a method of producing 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof comprising the step of heating a mixture comprising 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, thiourea and water.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 24, 2012
    Inventors: Herbert Koller, Michael Pyerin
  • Publication number: 20120123166
    Abstract: Method of preparing 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane comprising step (ii): (ii) converting 3,3,5,5-tetramethylcyclohexanone to 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane by using methylmagnesium chloride. 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane may be used for preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 17, 2012
    Applicant: MERZ PHARMA GmbH & CO. KGaA
    Inventors: Herbert Koller, Michael Pyerin, Federico Sbrogio
  • Patent number: 8178583
    Abstract: The invention is concerned with compounds of formula I: wherein R, R2, and Q are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are useful as inhibitors of cholesteryl ester transfer protein (CETP).
    Type: Grant
    Filed: December 7, 2009
    Date of Patent: May 15, 2012
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Torsten Hoffmann, Holger Kuehne, Eric J. Niesor, Philippe Pflieger
  • Publication number: 20120116125
    Abstract: Method of preparing 1-amino-1,3,3,5,5-pentamethylcyclohexane or pharmaceutically acceptable salt thereof, comprising at least two steps selected from the following steps (i) to (iv): (i) converting isophorone to 3,3,5,5-tetramethylcyclohexanone in the presence of methylmagnesium chloride; (ii) converting 3,3,5,5-tetramethylcyclohexanone to 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane in the presence of methylmagnesium chloride; (iii) converting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane to 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane in the presence of chloroacetonitrile in acidic solution; (iv)converting 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane to 1-amino-1,3,3,5,5-pentamethylcyclohexane in the presence of thiourea in water.
    Type: Application
    Filed: June 28, 2010
    Publication date: May 10, 2012
    Applicant: MERZ PHARMA GMBH & CO. KGAA
    Inventors: Herbert Koller, Michael Pyerin, Federico Sbrogio
  • Publication number: 20120014923
    Abstract: A hypoglycemic effect enhancer for enhancing the activity of an ?-glucosidase inhibitor, the enhancer comprising at least one kind of bacteria selected from the group consisting of bifidobacteria, lactic acid bacteria, saccharifying bacteria, and butyric acid bacteria.
    Type: Application
    Filed: March 25, 2010
    Publication date: January 19, 2012
    Inventors: Yasuhiro Isa, Masaki Shimakawa, Hiroshi Ohno, Hideki Yamamura
  • Patent number: 8076518
    Abstract: This invention provides chain extender compositions. These compositions comprise (i) an aliphatic secondary diamine, and (ii) a component selected from the group consisting of: (a) a cycloaliphatic primary diamine; (b) an aliphatic secondary diamine; (c) an aliphatic secondary diamine and an aliphatic primary diamine; (d) an aliphatic diimine; and (e) a combination of any two or more of (a) through (d), with the proviso that when (ii) is (a), (i) is a noncyclic aliphatic secondary diamine. Processes for producing polyurethanes, polyureas, and polyurea-urethanes are also provided.
    Type: Grant
    Filed: September 25, 2006
    Date of Patent: December 13, 2011
    Assignee: Albemarle Corporation
    Inventors: Paul L. Wiggins, John Y. Lee, Judit Orgad, David W. Owens
  • Patent number: 8058475
    Abstract: Novel cyclohexylmethyl compounds corresponding to formula I wherein R1, R2, R3, R4 and R5, have the meanings given in the description. Pharmaceutical formulations containing these compounds, as well as a processes for preparing these compounds and related methods of treatment are also provided.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: November 15, 2011
    Assignee: Gruenenthal GmbH
    Inventors: Stefan Oberboersch, Beatrix Merla, Bernd Sundermann, Werner Englberger, Hagen-Heinrich Hennies, Achim Kless, Petra Bloms-Funke, Babette-Yvonne Koegel, Heinze Graubaum
  • Publication number: 20110052732
    Abstract: A mineral absorption accelerator, and an anemia improving agent, food and drink or food and drink material containing the mineral absorption accelerator are provided, the mineral absorption accelerator including: an ?-glucosidase inhibitory component.
    Type: Application
    Filed: April 3, 2009
    Publication date: March 3, 2011
    Applicant: FUJIFILM Corporation
    Inventor: Fumitaka Ueda
  • Patent number: 7875750
    Abstract: The present invention relates to a process for preparing 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles (I) wherein the asterisk (*) represents an asymmetric carbon and R1 is C1-C6 alkyl; their enantiomers or mixtures thereof, their solvates, hydrates or pharmaceutically acceptable salts, comprising: (a) reacting a compound (II) with a secondary amine, optionally in the presence of an acid and a solvent 1, to form an enamine; (b) optionally removing said acid and said solvent 1, and then reacting said enamine with sulfur in the presence of a solvent 2; and (c) reacting the previously obtained compound with cyanamide to obtain the compound (I). Pramipexole, a compound with dopamine D-2 agonist activity, is among the compounds (I) and is useful for the treatment of Parkinson's disease and schizophrenia.
    Type: Grant
    Filed: November 16, 2009
    Date of Patent: January 25, 2011
    Assignee: Ragactives, S.L.
    Inventors: Gustavo Pascual Coca, Jorge Martin Juarez
  • Patent number: 7790773
    Abstract: A carba-sugar amine derivative represented by the following formula (1) or (2) is used as the active ingredient of a ?-galactosidase inhibitor or a glycolipid metabolic disorder treating agent. Wherein each of R1 and R2 independently represents H, an alkyl group, an acyl group, an aryl group or an aralkyl group, with the proviso that both are not H at the same time, and each of R3, R4, R5 and R6 independently represents a hydroxyl group or hydroxyl group having a substituent. Also, R7 represents an alkyl group, and each of R8, R9, R10 and R11 independently represents a hydroxyl group or a hydroxyl group having a substituent.
    Type: Grant
    Filed: March 8, 2004
    Date of Patent: September 7, 2010
    Assignee: Seikagaku Corporation
    Inventors: Seiichiro Ogawa, Yoshiyuki Suzuki, Eiji Nanba, Junichiro Matsuda, Kousaku Ohno
  • Patent number: 7790769
    Abstract: Disclosed are merocyanine derivatives of formula (1), wherein R1 and R2 independently from each other are branched C4-C22alkyl; or branched C4-C12 alkenyl; R3 and R4 independently from each other are cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; wherein at least one of R3 and R4 is cyano; R5 and R6 independently from each other are hydrogen; C1-C6alkyl; C5-C8cycloalkyl which may be substituted by one or more than one C1-C4alkyl; and R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl. The compounds are useful as UV absorbers for protecting human hair and skin against the damaging effect of UV radiation.
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: September 7, 2010
    Assignee: Ciba Corporation
    Inventors: Barbara Wagner, Astrid Walther, Bernd Herzog
  • Patent number: 7767858
    Abstract: This invention provides aromatic diimines which have imino hydrocarbylidene groups with at least two carbon atoms, and aromatic secondary diamines which have amino hydrocarbyl groups with at least two carbon atoms. Both the aromatic diimines and the aromatic secondary diamines either are in the form of one phenyl ring, or are in the form of two phenyl rings connected by an alkylene bridge; each position ortho to an imino group or an amino group bears a hydrocarbyl group. When in the form of one phenyl ring, there are two imino groups on the ring or two amino groups on the ring; the imino groups or amino groups are meta or para relative to each other. When in the form of two phenyl rings connected by an alkylene bridge, there is either one imino group or one amino group on each phenyl ring. Also provided are processes for forming diimines and secondary diamines.
    Type: Grant
    Filed: September 14, 2007
    Date of Patent: August 3, 2010
    Assignee: Albemarle Corporation
    Inventors: Paul L. Wiggins, Judit Orgad, John Y. Lee, Mahmood Sabahi
  • Publication number: 20100184999
    Abstract: Methods of performing cycloadditions are described that include (a) combining a first reactant and a second reactant in a hydrogen bonding solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form a cycloadduct. Methods of performing asymmetric catalytic reactions are also described that include (a) combining a first reactant, a second reactant, and a catalytic amount of a chiral hydrogen-bond donor in a solvent to form a reaction mixture; and (b) reacting the first reactant and the second reactant to form an enantiomeric excess of a reaction product. Reaction mixtures corresponding to these methods are also described.
    Type: Application
    Filed: June 11, 2007
    Publication date: July 22, 2010
    Inventors: Viresh H. Rawal, Yong Huang, Aditya K. Unni, Avinash N. Thadani
  • Publication number: 20100185012
    Abstract: A method of producing optically active trans-2-aminocyclohexanol includes allowing racemic trans-2-aminocyclohexanol to react with optically active 2-methoxyphenylacetic acid to produce an optically active 2-methoxyphenylacetic acid salt of optically active trans-2-aminocyclohexanol and separating the salt. An optically active 2-methoxyphenylacetic acid salt of optically active trans-2-aminocyclohexanol is also provided. The method makes it possible to produce optically active trans-2-aminocyclohexanol with ease and a high yield from an industrially-advantageous, inexpensive raw material.
    Type: Application
    Filed: June 18, 2008
    Publication date: July 22, 2010
    Applicant: TORAY FINE CHEMICALS CO., LTD
    Inventors: Ryuji Ogawa, Toshihiro Fujino, Kenichi Sakai
  • Publication number: 20100063324
    Abstract: The present invention relates to a process for preparing 2-amino-6-alkyl-amino-4,5,6,7-tetrahydrobenzothiazoles (I) wherein the asterisk (*) represents an asymmetric carbon and R1 is C1-C6 alkyl; their enantiomers or mixtures thereof, their solvates, hydrates or pharmaceutically acceptable salts, comprising: (a) reacting a compound (II) with a secondary amine, optionally in the presence of an acid and a solvent 1, to form an enamine; (b) optionally removing said acid and said solvent 1, and then reacting said enamine with sulfur in the presence of a solvent 2; and (c) reacting the previously obtained compound with cyanamide to obtain the compound (I). Pramipexole, a compound with dopamine D-2 agonist activity, is among the compounds (I) and is useful for the treatment of Parkinson's disease and schizophrenia.
    Type: Application
    Filed: November 16, 2009
    Publication date: March 11, 2010
    Applicant: RAGACTIVES, S.L.
    Inventors: Gustavo Pascual Coca, Jorge Martín Juárez
  • Patent number: 7642381
    Abstract: The process of the present invention can be briefly summarized as depicted in the following scheme: R1 is C1-Calkyl, R2 is C1-C6alkyl and Hal is a halogen atom.
    Type: Grant
    Filed: January 18, 2007
    Date of Patent: January 5, 2010
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Jinhua J. Song, Jinghua Xu
  • Publication number: 20090203910
    Abstract: Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
    Type: Application
    Filed: December 11, 2008
    Publication date: August 13, 2009
    Inventors: Jason Chi-Chung Choy, Saul Jaime-Figueroa, Joseph M. Muchowski, Paul J. Wagner
  • Publication number: 20090169495
    Abstract: Disclosed are merocyanine derivatives of formula (1), wherein R1 and R2 independently from each other are branched C4-C22alkyl; or branched C4-C12 alkenyl; R3 and R4 independently from each other are cyano; COR7, COOR7; CONR7R8; SO2(C6-C12)aryl; C2-C12alk-1-enyl; C3-C12cycloalk-1-enyl; C2-C12alk-1-inyl; C2-C12heteroalkyl; C3-C5heterocycloalkyl; C6-C10aryl; or C1-C9heteroaryl; wherein at least one of R3 and R4 is cyano; R5 and R6 independently from each other are hydrogen; C1-C6alkyl; C5-C8cycloalkyl which may be substituted by one or more than one C1-C4alkyl; and R7 and R8 independently from each other are hydrogen; C1-C22alkyl; C2-C12alkenyl; C2-C12alkinyl; C3-C12cycloalkyl; C3-C12cycloalkenyl; —(CH2)tCOOH; C7-C12aralkyl; C1-C12heteroalkyl; C2-C11heteroaralkyl; C6-C10aryl; C1-C9heteroaryl. The compounds are useful as UV absorbers for protecting human hair and skin against the damaging effect of UV radiation.
    Type: Application
    Filed: December 11, 2006
    Publication date: July 2, 2009
    Inventors: Barbara Wagner, Astrid Walther, Bernd Herzog