The Alicyclic Ring And Amino Nitrogen Are Bonded Directly To The Same Acyclic Carbon, Which Carbon Additionally Has Only Hydrogen Or Acyclic Hydrocarbyl Substituents Bonded Directly Thereto Patents (Class 564/455)
  • Patent number: 9752030
    Abstract: The purpose of the present invention is to provide a polyimide resin which exhibits higher heat resistance than that of a conventional polyimide resin by controlling the geometric configuration of the constituent units. Provided is a polyamic acid which comprises repeating units represented by general formula (1), wherein the 1,4-bismethylenecyclohexane skeleton units consist of both trans- and cis-form units, and the contents of the trans- and cis-form units are 60 to 100% and 0 to 40% respectively (with the sum total of the trans- and cis-form units being 100%).
    Type: Grant
    Filed: February 26, 2010
    Date of Patent: September 5, 2017
    Assignee: MITSUI CHEMICALS, INC.
    Inventors: Kenichi Fukukawa, Masaki Okazaki, Yoshihiro Sakata, Ichiro Fujio, Wataru Yamashita
  • Publication number: 20150119461
    Abstract: The present application provides novel tetrahydro-isohumulone (THIAA) derivatives and substantially enantiomerically pure compositions and pharmaceutical formulations thereof. The application further provides methods of using the disclosed compounds and compositions to activate PPAR?, inhibit inflammation, and treat conditions associated with inflammation and conditions responsive to PPAR? modulation such as diabetes.
    Type: Application
    Filed: January 9, 2015
    Publication date: April 30, 2015
    Inventors: Veera KONDA, Jan URBAN, Anuradha DESAI, Clinton J. DAHLBERG, Brian J. CARROLL
  • Publication number: 20150057361
    Abstract: Disclosed herein are novel motuporamine compounds that act as anti-metastatic agents with low toxicity and high anti-migration activity. The non-toxic, anti-metastatic agents may be given to patients with potential or actual metastatic cancers, such as pancreatic cancers, alone in combination with known and/or new therapies to help block the growth and spread of tumor(s).
    Type: Application
    Filed: March 13, 2013
    Publication date: February 26, 2015
    Applicant: University of Central Florida Research Foundation, Inc.
    Inventors: Otto Phanstiel, IV, Aaron Muth
  • Publication number: 20140296575
    Abstract: The present invention relates to a multi-branched Mannich base corrosion inhibitor and the method for preparing thereof. The method comprises (1) adding 3˜7 moles ketone and 3˜7 moles aldehyde to reaction kettle, adjusting pH to 2˜6 with acid, controlling temperature to 20˜50° C. and stirring for 20˜30 mins; (2) adding 1 mole organic polyamine to the reaction kettle under stirring, or adding the pH-adjusted ketone, aldehyde and organic solvent to organic polyamine, controlling temperature to 60˜90° C. and reacting for 1˜3 hrs, and after completion of the reaction, heating the system to 110° C. under nitrogen to remove water; the organic polyamine is organic compound comprising three or more primary amine groups and/or secondary amine groups.
    Type: Application
    Filed: April 27, 2012
    Publication date: October 2, 2014
    Applicant: PetroChina Company Limited
    Inventors: Ling Ma, Lei Li, Xiangjun Kong, Malike Dilibai, Xinping Zhen, Chunge Niu, Shengjun Bai
  • Publication number: 20140094616
    Abstract: Compound (1) or a salt that is useful as an intermediate for the production of a medicine, an agrochemical or the like can be produced by a process including the following steps: (A) reacting an aldehyde (2) with nitromethane to produce a nitroaldehyde; (B) reacting the nitroaldehyde with an alcohol to produce a nitroacetal; (C) reducing the nitroacetal to produce an aminoacetal; (D) protecting an amino group in the aminoacetal to produce a protected aminoacetal; (E) treating the protected aminoacetal with an acid and subsequently with a base and then reacting the resultant product with a cyanating agent to produce a nitrile; (F) hydrolyzing the nitrile to produce a protected amino acid; and (G) substituting a group R5 in the protected amino acid by a hydrogen atom and protecting a carboxyl group therein.
    Type: Application
    Filed: May 17, 2012
    Publication date: April 3, 2014
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Tetsuya Ikemoto, Leopold Mpaka Lutete, Toshiaki Aikawa
  • Publication number: 20130310555
    Abstract: Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
    Type: Application
    Filed: May 17, 2013
    Publication date: November 21, 2013
    Applicant: Illinois Institute of Technology
    Inventor: Hyun-Soon Chong
  • Publication number: 20130303805
    Abstract: The present invention relates to a process for producing an amino compound by subjecting a polyamine and an alkenyl compound to addition reaction in the presence of an alkali metal hydride compound which is capable of supplying the amino compound in a stable manner without occurrence of odor.
    Type: Application
    Filed: January 16, 2012
    Publication date: November 14, 2013
    Applicant: Mitsubishi Gas Chemical Company, Inc.
    Inventors: Hisayuki Kuwahara, Tomotaka Wada
  • Patent number: 8492591
    Abstract: Highly selective 5-HT(2C) receptor agonists receptors are disclosed. The 5-HT(2C) receptor agonists are used in the treatments of disease and conditions wherein modulation of 5-HT(2C) receptors provides a benefit, such as obesity and psychiatric disorders.
    Type: Grant
    Filed: February 3, 2011
    Date of Patent: July 23, 2013
    Assignees: The Board of Trustees of the University of Illinois, The University of North Carolina at Chapel Hikll
    Inventors: Alan Kozikowski, Bryan Roth, Andreas Svennebring, Sung Jin Cho
  • Publication number: 20130137575
    Abstract: Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.
    Type: Application
    Filed: November 29, 2012
    Publication date: May 30, 2013
    Applicant: NORTH CAROLINA STATE UNIVERSITY
    Inventor: North Carolina State University
  • 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: 20120289746
    Abstract: The invention relates to a process for working up a stream (3) comprising from 5 to 90% by weight of isocyanate by hydrolysis of the isocyanate by means of water in a reactor (1), in which the isocyanate-comprising stream (3) is introduced to the reactor (1) via a first inlet and the water is introduced via a second inlet, the isocyanate is reacted with the water in the reactor to form the corresponding: diamine, a diamine-comprising product mixture is taken off from the reactor (1) via a product outlet, wherein part of the product mixture is recirculated to the reactor and the isocyanate-comprising stream (3) is introduced into the recirculated product stream (7), with the isocyanate-comprising stream (3) being introduced continuously without interruption and the molar ratio of H-acid compounds of the hydrolyzate to isocyanate groups of the stream introduced being kept in the range from 10 to 200.
    Type: Application
    Filed: May 9, 2012
    Publication date: November 15, 2012
    Applicant: BASF SE
    Inventors: Ulrich Penzel, Siegfried Richter, Ulrich Juedes, Matthias Neumann, Hermann Lachmann
  • Patent number: 8309610
    Abstract: This invention relates to solid crystalline forms of (1RS,3RS,6RS)-6-Dimethylaminomethyl-1-(3-methoxy-phenyl)cyclohexane-1,3-diol hydrochloride (1), methods of producing 1, methods of use of 1, use of 1 as analgesics and pharmaceutical compositions comprising 1.
    Type: Grant
    Filed: February 21, 2006
    Date of Patent: November 13, 2012
    Assignee: Gruenenthal GmbH
    Inventors: Michael Gruss, Helmut Buschmann, Andreas Fischer, Wolfgang Hell, Dagmar Lischke
  • Patent number: 8268894
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: November 11, 2010
    Date of Patent: September 18, 2012
    Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
  • Patent number: 8202910
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.
    Type: Grant
    Filed: October 22, 2008
    Date of Patent: June 19, 2012
    Assignee: Sequella, Inc.
    Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
  • Publication number: 20120136173
    Abstract: The instant invention provides a process for improving catalytic activity of catalyst systems for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines. The process for improving catalytic activity of catalyst systems for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines comprises the steps of: (1) feeding ammonia, optionally hydrogen, and optionally one or more solvents over one or more heterogeneous metal based catalyst systems having a reduced catalytic activity for a period of greater than 1 hour at a temperature in the range of from 50° C. to 500° C.; wherein said one or more heterogeneous metal based catalyst systems have a yield of less than 90 percent based on the molar conversion of cyanoaldehydes to diamines; and (2) thereby improving the catalytic activity of said one or more heterogeneous metal based catalyst systems.
    Type: Application
    Filed: July 30, 2010
    Publication date: May 31, 2012
    Applicant: Dow Global Technologies LLC
    Inventors: Daniel A. Hickman, Shawn D. Feist, Erich J. Molitor, David C. Molzahn, Stacie Santhany, Abraham D. Schuitman
  • Publication number: 20120116099
    Abstract: The present invention relates to a method of continuously conveying a liquid which is used as starting material in a chemical reaction by means of a displacement pump having physically separate forward-transport valves and a liquid-filled bidirectional flow line between displacement pump and forward-transport valves, wherein an auxiliary liquid which is a product or a starting material of the chemical reaction and has a melting point which is below the melting point or below the saturation temperature of the liquid to be conveyed is present in the bidirectional flow line. The present invention additionally provides for the use of a product formed by hydrogenation of an aromatic compound as auxiliary liquid for conveying an aromatic compound and also the use of an alcohol or an ester derived from alcohol and carboxylic acid as auxiliary liquid for conveying carboxylic acids or carboxylic acid derivatives.
    Type: Application
    Filed: July 6, 2010
    Publication date: May 10, 2012
    Applicant: BASF SE
    Inventors: Joachim Pfeffinger, Willi Gilcher, Juergen Morell
  • Publication number: 20120116124
    Abstract: The instant invention provides a process for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines, and aliphatic diamines produced via such method. The process for reductive amination of aliphatic cyanoaldehydes to aliphatic diamines comprises the steps of: (1) providing a mixture of one or more cycloaliphatic cyanoaldehydes, optionally water, and optionally one or more solvents, wherein said one or more cycloaliphatic cyanoaldehydes are selected from the group consisting of 1,3-cyanocyclohexane carboxaldehyde, 1,4-cyanocyclohexane carboxaldehyde, mixtures thereof, and combinations thereof; (2) contacting said mixture with a metal carbonate based solid bed or a weak base anion exchange resin bed at a temperature in the range of 15 to 40° C.
    Type: Application
    Filed: July 30, 2010
    Publication date: May 10, 2012
    Applicant: Dow Global Technologies LLC
    Inventors: Erich J. Molitor, Erich J. Molitor, Daniel A. Hickman, Shawn D. Feist, David C. Molzahn, Stacie Santhany, Abraham d. Schuitman
  • Publication number: 20120116122
    Abstract: The instant invention is a process for the conversion of aliphatic cyclic amines to aliphatic diamines. The process for conversion of aliphatic cyclic amines to aliphatic diamines comprises the steps of: (1) selecting one or more cyclic amines; (2) contacting said one or more cyclic amines with ammonia and hydrogen, optionally water, and optionally one or more solvents in the presence of one or more heterogeneous metal based catalyst systems at a temperature in the range of from 120° C. to about 250° C.
    Type: Application
    Filed: July 30, 2010
    Publication date: May 10, 2012
    Applicant: Dow Global Technologies LLC
    Inventors: Shawn D. Feist, Daniel A. Hickman, Erich J. Molitor, David C. Molzahn, Stacie Santhany, Abraham D. Schuitman
  • Publication number: 20120058144
    Abstract: The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells. In particular, the invention provides lipids having the following structures XIV or XVII.
    Type: Application
    Filed: November 10, 2009
    Publication date: March 8, 2012
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Marco A. Ciufolini
  • Publication number: 20120035269
    Abstract: Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.
    Type: Application
    Filed: September 29, 2011
    Publication date: February 9, 2012
    Inventor: Edward C. Sisler
  • Publication number: 20110218323
    Abstract: The present invention relates to a process for preparing a cyclic diamine, comprising the reaction of at least one cyclic alkene with a gas mixture (G) comprising dinitrogen the subsequent conversion of monoxide to give at least one cyclic ketone and then converting the at least one cyclic ketone to a cyclic diamine. The invention also relates to the use of a cyclic diamine with primary and secondary amine functions thus obtained to prepare polyamides and polyurethanes.
    Type: Application
    Filed: November 6, 2009
    Publication date: September 8, 2011
    Applicant: Basf SE
    Inventors: Kirsten Dahmen, Martin Ernst, Michael Limbach, Johann-Peter Melder, Beatrice Rössler-Feigel, Joaquim Henrique Teles
  • Publication number: 20110124919
    Abstract: The present invention relates to 3-aminomethyl-1-cyclohexylamine and to a process for preparation thereof by a) reacting cyclohexenone with hydrogen cyanide in the presence of a basic catalyst, b) reacting the cyclohexanonenitrile obtained in stage a) with ammonia in the presence of an imine formation catalyst, and c) reacting the 3-cyanocyclohexylimine-containing reaction mixture obtained in stage b) with hydrogen and ammonia over hydrogenation catalysts. The present invention further relates to the use of 3-aminomethyl-1-cyclohexylamine 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: Application
    Filed: July 13, 2009
    Publication date: May 26, 2011
    Applicant: BASF SE
    Inventors: Martin Ernst, Kirsten Dahmen, Alfred Oftring
  • Publication number: 20110124918
    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: Application
    Filed: July 13, 2009
    Publication date: May 26, 2011
    Applicant: BASF SE
    Inventors: Martin Ernst, Alfred Oftring, Kathrin Wissel-Stoll, Oemer Uensal, Stephan Freyer, Ansgar Gereon Altenhoff, Wolfgang Staffel
  • Publication number: 20110009439
    Abstract: Compounds of formula (Ia): wherein R1, R2, R3, R4a, R4b, R5, and R6 are defined herein, as well as other indene derivatives are disclosed herein. Pharmaceutical compositions containing the compounds and methods of using the compounds are also disclosed.
    Type: Application
    Filed: February 23, 2010
    Publication date: January 13, 2011
    Applicant: AQUINOX PHARMACEUTICALS INC.
    Inventors: Jeffery R. Raymond, Kang Han, Yuanlin Zhou, Yuehua He, Bradley Noren, James Gee Ken Yee
  • Patent number: 7842729
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: June 3, 2005
    Date of Patent: November 30, 2010
    Assignees: The United States of America as represented by the Department of Health and Human Services, Sequella, Inc.
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Publication number: 20100273745
    Abstract: Polyamine, polyamine/guanidino, and polyamine/biguanide compounds are disclosed. The compounds are useful as anti-cancer and anti-parasitic treatments. The compounds are also useful as inhibitors of the enzyme lysine-specific demethylase-1.
    Type: Application
    Filed: April 20, 2010
    Publication date: October 28, 2010
    Applicants: THE JOHNS HOPKINS UNIVERSITY, WAYNE STATE UNIVERSITY
    Inventors: Patrick M. Woster, Tracey Boncher, Robert Casero
  • Patent number: 7763754
    Abstract: A process for producing (1R,3R,6R)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol or (1S,3S,6S)-6-dimethylaminomethyl-1-(3-methoxyphenyl)-cyclohexane-1,3-diol or mixtures thereof.
    Type: Grant
    Filed: February 27, 2009
    Date of Patent: July 27, 2010
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Heinrich Buschmann, Wolfgang Hell, Joerg Holenz, Oswald Zimmer, Irene Vaulont, Dieter Haag, Emad El Sayed, Robert Hett, Alfed Olbrich, Lars Pumpenmeier
  • Publication number: 20100174090
    Abstract: The present application relates to novel methods for the preparation of primary, secondary and tertiary carbinamine compounds, particularly the preparation of compounds of formulae I, IV and VI, from a carbonyl compound of formula II in the presence of ammonia or an ammonium equivalent of the formula NH4+X?, by way of allylation, crotylation, arylation, reductive amination and catalytic hydrogenation.
    Type: Application
    Filed: March 28, 2008
    Publication date: July 8, 2010
    Inventors: Avinash N. Thadani, Bhartesh Dhudshia
  • Publication number: 20100151386
    Abstract: Disclosed is a photobase generator comprising a compound having a nitrogen atom and a conjugated multiple bond.
    Type: Application
    Filed: December 12, 2007
    Publication date: June 17, 2010
    Inventors: Katsuya Shimizu, Fumio Matsushita
  • Patent number: 7728165
    Abstract: In one embodiment, the present application relates to a process of making a compound of formula I. and to certain intermediate compounds that are made within the process of making the compound of formula I.
    Type: Grant
    Filed: June 15, 2009
    Date of Patent: June 1, 2010
    Assignee: Schering Plough Corporation
    Inventors: Jeonghan Park, Anantha R Sudhakar, George S. K. Wong, Minzhang Chen, Juergen Weber, Xiaojing Yang, Daw-long Kwok, Ingyu Jeon, Ramani R Raghavan, Maria Tamarez, Weidong Tong, Eugene J. Vater
  • Publication number: 20090124504
    Abstract: Methods of applying cyclopropene amine derivatives and compositions thereof to inhibit ethylene receptors in plants and plant material are disclosed. Methods include applying to the plant an effective ethylene response-inhibiting amount of at least one cyclopropene amine compound or composition thereof. Cyclopropene amine compounds, enantiomers, stereoisomers or salts thereof are also provided.
    Type: Application
    Filed: June 13, 2008
    Publication date: May 14, 2009
    Inventor: Edward C. Sisler
  • Patent number: 7470816
    Abstract: A process for the resolution of isomeric tramadol mixtures comprising: providing a purification stock comprising both cis and trans tramadol; contacting the purification stock with an acid under conditions effective to form an acid salt of the cis and trans tramadol in the purification stock; and separating the cis tramadol acid salt from the trans tramadol to obtain a purified cis tramadol acid salt; and optionally converting the cis tramadol acid salt to cis tramadol or to a pharmaceutically active salt thereof.
    Type: Grant
    Filed: November 13, 2006
    Date of Patent: December 30, 2008
    Assignee: IPAC Laboratories Limited
    Inventors: Ashok Kumar, Suneel Yeshwant Dike, Satish Rajanikant Soudagar, Chirag Hasmukh Shah, Sandeep Madhavrao Burudkar, Prashant Gautam, Byju Nellithanath Thankachen, Ashvini Saxena, Manavalan Saravanan, Gunjan Pramod Pathak, Virendra Pal, Rahul Karde, Jaysingh Gehlot
  • Patent number: 7456222
    Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: November 25, 2008
    Assignees: Sequella, Inc., The United States of America as represented by the Secretary, Department of Health and Human Services
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III, Elena Bogatcheva, Leo Einck
  • Patent number: 7453011
    Abstract: Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
    Type: Grant
    Filed: June 4, 2007
    Date of Patent: November 18, 2008
    Assignee: Progen Pharmaceuticals, Inc.
    Inventors: Linda Clifford, legal representative, Aldonia L. Valasinas, Andrei V. Blokhin, Aparajita Sarkar, Hirak S. Basu, Venodhar K. Reddy, Laurence J. Marton, Yu Wang, Benjamin Frydman
  • Patent number: 7432399
    Abstract: A polyol monomer comprising the formula: R1 and R3 are —H, aliphatic, aromatic, or ether; R2 is aliphatic, aromatic, ester, ether, or acrylic, and R1 contains a hydroxyl group, R3 contains a hydroxyl group, R2 contains —O—CH2—CH(OH)—, or any combination thereof. The polyol monomer may be made by reacting an epoxy and an amine. Either the epoxy contains more than one epoxide groups, the amine contains a hydroxyl group, or both. A thermoset made by reacting the polyol monomer with a polyisocyanate.
    Type: Grant
    Filed: November 2, 2004
    Date of Patent: October 7, 2008
    Assignee: The United States of America as represented by the Secretary of the Navy
    Inventors: Jozef Verborgt, Arthur Anthony Webb
  • Patent number: 7279502
    Abstract: Peptide conjugates in which cytocidal and cytostatic agents, such as polyamine analogs or naphthoquinones, are conjugated to a polypeptide recognized and cleaved by enzymes such as prostate-specific antigen (PSA) and cathepsin B are provided, as well as compositions comprising these conjugates. Methods of using these conjugates in the treatment of prostate diseases are also provided.
    Type: Grant
    Filed: October 20, 2004
    Date of Patent: October 9, 2007
    Assignee: Cellgate, Inc.
    Inventors: Linda Clifford, legal representative, Laurence J. Marton, Benjamin Frydman, deceased
  • Patent number: 7235695
    Abstract: Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
    Type: Grant
    Filed: August 16, 2005
    Date of Patent: June 26, 2007
    Inventors: Benjamin Frydman, Aldonia L. Valasinas, Andrei V. Blokhin, Aparajita Sarkar, Hirak S. Basu, Venodhar K. Reddy, Laurence J. Marton, Yu Wang
  • Patent number: 7060857
    Abstract: In a process for preparing 3-aminomethyl-3,5,5-trimethylcyclohexylamine (isophoronediamine, IPDA) having a cis/trans isomer ratio of at least 70/30 from 3-cyano-3,5,5-trimethylcyclohexanone (isophoronenitrile, IPN), NH3 and H2, the hydrogenation is carried out at from 50 to 200° C. and a pressure of from 50 to 300 bar in the presence of a hydrogenation catalyst having an alkali metal content of ?0.03% by weight, calculated as alkali metal oxide referring to the total weight of the catalyst. The alkali metal content is made up of the contents of Li, Na, K, Rb and Cs; in particular, the alkali metal content is the Na content. A process for producing hydrogenation catalysts having an alkali metal content (in particular a sodium content) of ?0.03% by weight, calculated as alkali metal oxide/sodium oxide referring to the total weight of the catalyst, and the hydrogenation catalysts themselves are also provided by the invention.
    Type: Grant
    Filed: August 28, 2002
    Date of Patent: June 13, 2006
    Assignee: BASF Aktiengesellschaft
    Inventors: Frank Funke, Thomas Hill, Johann-Peter Melder, Ekkehard Schwab, Walter Himmel, Erhard Henkes, Hermann Petersen, Reinhard Körner
  • Patent number: 7022739
    Abstract: Substituted 1-aminobutane-3-ol compounds, methods for producing them, pharmaceutical compounds containing them, and the use of substituted 1-aminobutane-3-ol compounds for producing pharmaceutical compounds.
    Type: Grant
    Filed: March 28, 2003
    Date of Patent: April 4, 2006
    Assignee: Gruenenthal GmbH
    Inventors: Helmut Buschmann, Corinna Maul, Bernd Sundermann, Utz-Peter Jagusch, Michael Haurand, Boris Chizh
  • Patent number: 6984758
    Abstract: A crude liquid containing 1,3-bis(aminomethyl)cyclohexane and a high-boiling component having a boiling point higher than that of 1,3-bis(aminomethyl)cyclohexane is distilled. By controlling the distillation conditions, the high-boiling component is prevented from entering into a distilled 1,3-bis(aminomethyl)cyclohexane and the content of a low-boiling component in the distilled 1,3-bis(aminomethyl)cyclohexane is minimized.
    Type: Grant
    Filed: March 16, 2005
    Date of Patent: January 10, 2006
    Assignee: Mitsubishi Gas Chemical Co., Inc.
    Inventors: Kazuhiko Amakawa, Kuniaki Muneyasu, Hiroshi Watanabe
  • Patent number: 6982351
    Abstract: Conformationally restricted polyamine compounds useful in treatment of cancer and other diseases marked by abnormal cell proliferation are disclosed. Improved methods of synthesizing such compounds are also disclosed. In one method of the invention, a carbene-bearing or carbene equivalent-bearing compound is reacted with the double bond of an alkene compound to form a cyclopropyl ring as the first step in the synthesis.
    Type: Grant
    Filed: December 6, 2002
    Date of Patent: January 3, 2006
    Assignee: CellGate, Inc.
    Inventors: Benjamin Frydman, Aldonia L. Valasinas, Andrei V. Blokhin, Aparajita Sarkar, Hirak S. Basu, Venodhar K. Reddy, Laurence J. Marton, Yu Wang
  • Patent number: 6828462
    Abstract: Unsaturated 1-Amino-alkylcyclohexane compounds which are systemically-active as NMDA, 5HT3, and nicotinic receptor antagonists, pharmaceutical compositions comprising the same, method of preparation thereof, and method of treating CNS disorders which involve disturbances of glutamatergic, serotoninergic, and nicotinic transmission, treating immunomodulatory disorders, and antimalaria, antitrypanosomal, anti-Borna virus, anti-HSV and anti-Hepatitis C virus activity.
    Type: Grant
    Filed: November 6, 2002
    Date of Patent: December 7, 2004
    Assignee: Merz Pharma GmbH & Co. KGAA
    Inventors: Markus Henrich, Wojciech Danysz, Christopher Graham Raphael Parsons, Ivars Kalvinsh, Valerjans Kauss, Aigars Jirgensons, Markus Gold
  • Patent number: 6509472
    Abstract: Prochiral ketones are enantioselectively reduced to chiral secondary alcohols with a compound having the formula I: where, the two R2 groups are identical and are each a substituted or unsubstituted, aryl, alkyl, cycloalkyl or aralkyl group; and R3 is a hydrogen atom or a substituted or unsubstituted, alkyl, aryl, aralkyl or alkoxy group; wherein the substituents on the R2 and R3 groups are substantially non-reactive.
    Type: Grant
    Filed: August 30, 2001
    Date of Patent: January 21, 2003
    Assignee: Schering Corporation
    Inventor: Richard W. Draper
  • Patent number: 6479661
    Abstract: The invention relates to a method for disubstituting carboxylic acid amides on a geminal carbonyl-C-atom using a Grignard reagent in the presence of an organotitanate.
    Type: Grant
    Filed: March 23, 2001
    Date of Patent: November 12, 2002
    Assignee: Merck Patent Gesellschaft
    Inventors: Herwig Buchholz, Urs Welz-Biermann, Armin Meijere, Vladimir Chaplinski
  • Patent number: 6448445
    Abstract: The invention relates to a method for disubstituting carboxylic acid amides on the geminal carbonyl-C-atom using at least one grignard reagent in the presence of a metal alcoholate compound used as a catalyst and in the presence of another organometallic compound used as a co-catalyst.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: September 10, 2002
    Assignee: Merck Patent Gesellschaft mit beschraenkter Haftung
    Inventors: Herwig Buchholz, Urs Welz-biermann, Armin Meijere
  • Patent number: 6365708
    Abstract: This invention relates to novel polyamines which are the reaction product of A) at least one nonaromatic diamine containing from 2 to 40 carbon atoms, wherein the amine groups are primary amine groups; and B) at least one epihalohydrin of the formula  where R is hydrogen or methyl and X is chlorine or bromine; and the coatings resulting from the reaction between the above reaction product and nonaromatic epoxy resins.
    Type: Grant
    Filed: December 20, 1999
    Date of Patent: April 2, 2002
    Assignee: Cognis Corporation
    Inventors: Shailesh Shah, Anbazhagan Natesh, Joseph Mulvey, Ronald C. LaFreeda, Gaetano D. DeAngelis, Ronald T. Cash, Jr.
  • Patent number: 6329523
    Abstract: Novel compounds having the formula: wherein the constituent variables are defined herein. The compounds are constructed to include a central aromatic, aliphatic, or heterocyclic ring system. Attached to the central ring system are two linear groups having nitrogenous moieties that are derivatized with chemical functional groups. The ring system can include further nitrogenous moieties, either as ring atoms or on pendant groups attached to the ring, that may also be derivatized with chemical functional groups. The totality of the chemical functional groups imparts certain conformational and other properties to the these compounds. In accordance with certain embodiments of the invention, libraries of such compounds are prepared utilizing permutations and combinations of the chemical functional groups and the nitrogenous moieties to build complexity into the libraries.
    Type: Grant
    Filed: March 10, 1999
    Date of Patent: December 11, 2001
    Assignee: ISIS Pharmaceuticals, Inc.
    Inventors: Phillip Dan Cook, Haoyun An
  • Patent number: 6194615
    Abstract: The present invention relates to the composition, process of preparation, and use of novel derivatives prepared from 1,5-bis-(4′-carbomethoxyphenyl)-1,4-pentadien-3-one. These novel compositions can act as crosslinkers with polyfunctional monomeric, oligomeric, and/or polymeric anhydrides, esters, carboxylic acids, isocyantes, epoxies, carbonates, acetoacetates, and alkoxylated melamines.
    Type: Grant
    Filed: June 17, 1999
    Date of Patent: February 27, 2001
    Assignee: Eastman Chemical Company
    Inventors: Philip Conrad Heidt, Matthew Lynn Elliott
  • Patent number: 6166234
    Abstract: Novel tripodal cyclopentadiene derivatives have the formula (I) ##STR1## where E are identical or different and are --N(R)(R), --P(R)(R), --As(R)(R), --Sb(R)(R), --OR, --SR, --SeR, --TeR, where R are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical, or E is a leaving group X andR.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical,Z is a cyclopentadienyl radical or a substituted cyclopentadienyl structural unit andT is hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.30 -organosilicon radical or a group E--Y--, where E is --N(R)(R), --P(R)(R), --As(R)(R), --Sb(R)(R), --OR, --SR, --SeR, --TeR or a leaving group X, where R are identical or different and are each hydrogen, a C.sub.1 -C.sub.20 -carboorganic radical or a C.sub.1 -C.sub.
    Type: Grant
    Filed: January 13, 1998
    Date of Patent: December 26, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Gottfried Huttner, Joachim Vogelgesang, Ute Winterhalter, Bjorn Antelmann
  • Patent number: 6100430
    Abstract: An alicyclic polyamine of the formula (1) ##STR1## wherein Y.sub.1 represents a saturated aliphatic hydrocarbon group and R.sub.1 through R.sub.4 are the same or different and each represents hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group, or an aralkyl group. The alicyclic polyamine can be obtained by subjecting a 3-formylcycloalkanone or 3-formylcycloalkenone to reductive amination reaction.
    Type: Grant
    Filed: September 10, 1998
    Date of Patent: August 8, 2000
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Kenichi Yamamoto, Kazuyuki Matsuoka, Hiroshi Yagihara