Alicyclic Ring Or Ring System And Amino Nitrogen Are Attached Indirectly By An Acyclic Carbon Or Chain Patents (Class 564/453)
  • Patent number: 11919834
    Abstract: The invention pertains to a multi-step process for making polyfunctional aromatic compounds comprising two phenyl rings bearing reactive groups susceptible of polycondensation reaction to provide polycondensed polymers, said method using economic raw materials, and possessing high selectivity and overall yield.
    Type: Grant
    Filed: May 5, 2020
    Date of Patent: March 5, 2024
    Assignee: SOLVAY SPECIALTY POLYMERS ITALY S.P.A.
    Inventors: Rahul Shingte, Debaki Ghosh, Letanzio Bragante, Manuel Gregori, Stefano Millefanti, Emanuela Antenucci, Joel Pollino
  • Patent number: 11673853
    Abstract: Described herein are compounds that disrupt the interaction between Fbxo48 and phosphorylated-AMPK.
    Type: Grant
    Filed: May 6, 2021
    Date of Patent: June 13, 2023
    Assignees: UNIVERSITY OF PITTSBURGH—OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION, The United States as represented by the Department of Veterans Affairs
    Inventors: Beibei Chen, Rama K. Mallampalli, Yuan Liu
  • Patent number: 10343976
    Abstract: N-hydroxyalkylated polyamines, methods of making N-hydroxyalkylated polyamines, and drilling fluids containing N-hydroxyalkylated polyamines are provided, in which the N-hydroxyalkylated polyamine includes Formula (I): where R1 and R2 are independently a —C or —CH group; R3 is an aliphatic hydrocarbyl; R4 and R5 are independently acyclic hydrocarbyls, or R1, R2, R4, and R5 are covalently connected to form a cyclic hydrocarbyl; and R6, R7, R8, and R9 are independently acyclic hydrocarbyls or acyclic heterohydrocarbyls.
    Type: Grant
    Filed: August 23, 2018
    Date of Patent: July 9, 2019
    Assignee: Saudi Arabian Oil Company
    Inventors: Matthew Hilfiger, B. Raghava Reddy
  • Patent number: 10131622
    Abstract: N-hydroxyalkylated polyamines, methods of making N-hydroxyalkylated polyamines, and drilling fluids containing N-hydroxyalkylated polyamines are provided, in which the N-hydroxyalkylated polyamine includes Formula (I): where R1 and R2 are independently a —C or —CH group; R3 is an aliphatic hydrocarbyl; R4 and R5 are independently acyclic hydrocarbyls, or R1, R2, R4, and R5 are covalently connected to form a cyclic hydrocarbyl; and R6, R7, R8, and R9 are independently acyclic hydrocarbyls or acyclic heterohydrocarbyls.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: November 20, 2018
    Assignee: Saudi Arabian Upstream Technology Company
    Inventors: Matthew Hilfiger, B. Raghava Reddy
  • Patent number: 9193939
    Abstract: The present invention relates generally to cleaning compositions and, more specifically, to cleaning compositions containing a polyetheramine, a soil release polymer, and a carboxymethylcellulose, which is suitable for removal of stains from soiled materials.
    Type: Grant
    Filed: March 27, 2014
    Date of Patent: November 24, 2015
    Assignee: The Procter & Gamble Company
    Inventors: Frank Hulskotter, Stefano Scialla, Brian Joseph Loughnane, Alan Thomas Brooker, Colin Ure, Sophia Rosa Ebert, Bjoern Ludolph, Christof Wigbers, Steffen Maas, Dieter Boeckh, Christian Eidamshaus
  • Patent number: 8993768
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Grant
    Filed: May 10, 2012
    Date of Patent: March 31, 2015
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: John A. Beutler, Stuart F. J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Patent number: 8877976
    Abstract: The invention relates to an improved process for preparing 3-aminomethyl-3,5,5-trimethylcyclohexylamine, referred to hereinafter as isophoronediamine or IPDA for short, by means of catalytic hydrogenation and/or catalytic reductive amination (also referred to as aminating hydrogenation) of 3-cyano-3,5,5-trimethylcyclohexanone, also called isophoronenitrile or IPN for short hereinafter.
    Type: Grant
    Filed: November 17, 2011
    Date of Patent: November 4, 2014
    Assignee: Evonik Degussa GmbH
    Inventors: Christian Lettmann, Guido Streukens, Matthias Orschel, Gerda Grund
  • Publication number: 20140249181
    Abstract: Disclosed are compounds that inhibit RNase H activity of retroviruses, for example, a compound of formula (I) wherein R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Pharmaceutical compositions comprising such compounds, as well as methods of use, and treatment or prevention of infection by human immunodeficiency virus (HIV).
    Type: Application
    Filed: May 10, 2012
    Publication date: September 4, 2014
    Applicant: The united States of America, as represented by the Secretary, Department of Health and Human Serv
    Inventors: John A. Beutler, Stuart F.J. LeGrice, Craig Thomas, Jian-Kang Jiang, Suhman Chung, Jennifer Wilson
  • Publication number: 20140235872
    Abstract: The instant invention provides for novel cationic lipids that can be used in combination with other lipid components such as cholesterol and PEG-lipids to form lipid nanoparticles with oligonucleotides. It is an object of the instant invention to provide a cationic lipid scaffold that demonstrates enhanced efficacy along with lower liver toxicity as a result of lower lipid levels in the liver. The present invention employs low molecular weight cationic lipids with one short lipid chain to enhance the efficiency and tolerability of in vivo delivery of siRNA.
    Type: Application
    Filed: April 29, 2014
    Publication date: August 21, 2014
    Applicant: SIRNA THERAPEUTICS, INC.
    Inventors: Brian W. BUDZIK, Steven L. COLLETTI, Jennifer R. DAVIS, Ivory D. HILLS, Darla Danile SEIFRIED, Matthew G. STANTON
  • 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: 8480800
    Abstract: Provided are aminoalcohol compounds for use as neutralizing agents for paints and coatings. The compounds are of the formula (I): or salt thereof, wherein R1, R2, R3, R4, R5, and n are as defined herein. Also provided are precursors of the aminoalcohol compounds and processes for making and using them.
    Type: Grant
    Filed: December 1, 2010
    Date of Patent: July 9, 2013
    Inventors: Ian A. Tomlinson, Asghar A. Peera, George David Green
  • Patent number: 8362164
    Abstract: The embodiments of the invention relate to a multifunctional lithiated amine-containing compound comprising at least two molecules of lithiated amine in a molecule of the compound. In one embodiment, the compound has a formula where x is an integer of 1 or more, Q is (a) an element selected from the group consisting of O, S, N, P and Si or (b) an alkylene group having from 1 to 20 methylene groups, and R1 and R2 are the same or different and are selected from the group consisting of alkyls, cycloalkyls and aralkyls containing from 1 to 20 carbon atoms. In another embodiment, the compound comprises cyclic lithio amines and has a formula: where x is 1 or more, R3, R4 and R5 are the same or different and represent alkylene groups containing from 3 to 20 carbon atoms.
    Type: Grant
    Filed: October 12, 2011
    Date of Patent: January 29, 2013
    Assignee: Bridgestone Corporation
    Inventor: Yan Yan-Yong
  • 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: 8269046
    Abstract: Cyclic bisamides may be used to formulate inks for jet ink printing. The cyclic bisamide may be prepared from a cyclic diamine and acylic monocarboxylic acids. Conversely, the cyclic bisamide may be prepared from a cyclic diacid and acylic monoamines. The performance properties of the product may be enhanced by adding some additional difunctional reactant(s), e.g., diacid or diamine. A blend of bisamides may provide better performance properties than either of the component bisamides alone, where the blend includes at least one cyclic bisamide. The bisamides, in combination with an image-forming material, and optionally in combination with other materials, is taken to a molten form and the applied to a substrate to provide a printed substrate.
    Type: Grant
    Filed: August 2, 2005
    Date of Patent: September 18, 2012
    Assignee: Arizona Chemical Company, LLC
    Inventor: Mark S. Pavlin
  • Publication number: 20120232171
    Abstract: The invention relates to the use of alkoxylated cyclic diamines, the reactive groups of which are alkoxylated by means of at least one C2 to C4 alkylene oxide, and the average degree of alkoxylation of which is between 1 and 200 alkylene oxide units per reactive group, in amounts of 0.0001 to 5 wt % relative to the oil content of the emulsion to be broken, to break water-in-oil emulsions.
    Type: Application
    Filed: September 3, 2010
    Publication date: September 13, 2012
    Applicant: CLARIANT FINANCE (BVI) LIMITED
    Inventors: Carsten Cohrs, Stefan Dilsky, Dirk Leinweber, Michael Feustel
  • 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
  • Patent number: 8173844
    Abstract: A process for preparing O-alkylated amino alcohols of the formula (I) by reacting N-unsubstituted or N-monosubstituted amino alkoxide salts with alkyl halides, the amino alkoxide salts being formed by means of alkoxides
    Type: Grant
    Filed: December 11, 2006
    Date of Patent: May 8, 2012
    Assignee: BASF SE
    Inventors: Wolfgang Siegel, Gerd Haderlein, Tobias Stab
  • Publication number: 20120004380
    Abstract: Crosslink agents used to copolymerize at least one hydrophilic monomer with at least one lens monomer typically used to prepare polymeric materials for ophthalmic lenses. The crosslink agents have a relatively high selectivity for the hydrophilic monomer and limited reactivity with the crosslink agent used to polymerize the lens monomer. Accordingly, the invention is also directed to a hydrophilic crosslinked polymer that comprises at least two monomeric units and at least two different crosslink units. The use of the dual crosslink system provides an improved means to control the final chemical, physical and structural characteristics of the resulting polymer.
    Type: Application
    Filed: September 12, 2011
    Publication date: January 5, 2012
    Inventors: Ivan M. Nunez, Joseph A. McGee, David E. Seelye
  • 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: 20110224457
    Abstract: A method for producing an organolithium compound includes the step of reacting an aromatic compound or a halogenated unsaturated aliphatic compound and a lithiating agent in the presence of a coordinating compound containing three or more elements having a coordinating ability in a molecule, at least one thereof being a nitrogen element, or a coordinating compound containing three or more oxygen elements having a coordinating ability in a molecule, at least one of the groups containing the oxygen elements having a coordinating ability being a tertiary alkoxy group, at a temperature of ?40° C. to 40° C.
    Type: Application
    Filed: December 25, 2009
    Publication date: September 15, 2011
    Inventor: Hiroki Inoue
  • Publication number: 20110146536
    Abstract: Provided are aminoalcohol compounds for use as neutralizing agents for paints and coatings. The compounds are of the formula (I): or salt thereof, wherein R1, R2, R3, R4, R5, and n are as defined herein. Also provided are precursors of the aminoalcohol compounds and processes for making and using them.
    Type: Application
    Filed: December 1, 2010
    Publication date: June 23, 2011
    Inventors: Ian A. Tomlinson, Asghar A. Peera, George D. Green
  • 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: 20100279997
    Abstract: A compound, composition and method are disclosed that can provide analgesia. A contemplated compound has a structure that corresponds to Formula A, wherein A, B, X, R1, R2, R7 and R8, and the dashed lines are defined within.
    Type: Application
    Filed: October 28, 2009
    Publication date: November 4, 2010
    Inventors: Lindsay Burns Barbier, Hoau-Yan Wang, Nan-Horng Lin, Andrei Blasko
  • Publication number: 20100152238
    Abstract: Novel cannabinoid-derived quinone derivatives (quinonoid derivatives) having a substituted hydroxyl group, pharmaceutical compositions comprising same and uses thereof as anti-proliferative agents, are provided.
    Type: Application
    Filed: March 5, 2008
    Publication date: June 17, 2010
    Applicant: Yissum Research Development Company of The Hebrew University of Jerusalem
    Inventors: Raphael Mechoulam, Natalya Kogan
  • Publication number: 20100029983
    Abstract: A process for preparing gabapentin of formula 1, which comprises Formula (I) converting 1-allyl-cyclohexanecarboxaldehyde into 1-allyl-cyclohexanecarbonitrile; ozonizing 1-allyl-cyclohexanecarbonitrile to obtain 1-cyano-cyclohexaneacetaldehyde; acetalizing 1-cyano-cyclohexaneacetaldehyde with a suitable acetalizing agent to give the corresponding acetal and converting the latter into gabapentin.
    Type: Application
    Filed: June 29, 2007
    Publication date: February 4, 2010
    Inventors: Franco Ghelfi, Livius Cotarca, Fabrizio Roncaglia, Roberto Giovanetti, Andrea Nicoli
  • Publication number: 20080306304
    Abstract: A process for preparing O-alkylated amino alcohols of the formula (I) by reacting N-unsubstituted or N-monosubstituted amino alkoxide salts with alkyl halides, the amino alkoxide salts being formed by means of alkoxides
    Type: Application
    Filed: December 11, 2006
    Publication date: December 11, 2008
    Inventors: Wolfgang Siegel, Gerd Haderlein, Tobias Stab
  • 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: 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
  • Publication number: 20080167500
    Abstract: The present invention relates to a process for the preparation of a diastereomerically enriched compound, wherein a first compound according to formula (I), is contacted with a second compound according to formula (II), to form a third compound according to formula (III), whereby the compound according to formula (III) is subsequently reduced and thereby converted into a compound according to formula (IV), in which formulas: R1=a cycloalkyl group whereby R1 # R2, R2=a substituted or unsubstituted: (cyclo)alkyl group, (cyclo)alkenyl group, aryl group, cyclic or acyclic heteroalkyl group or heteroaryl group, R3=an alkyl group, R4=a substituted or unsubstituted: phenyl- or naphthyl-group, *=a chiral center. The invention furthermore relates to a diastereomerically enriched compound according to formula (IV) and its use in the preparation of pharmaceutical and agrochemically active compounds.
    Type: Application
    Filed: July 20, 2005
    Publication date: July 10, 2008
    Applicant: DSM IP ASSETS B.V.
    Inventors: Quirinus Bernardus Broxterman, Ben De Lange, Henrius Leonardus Marie Elsenberg, Matthias Weber
  • Patent number: 7388112
    Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. Examples are those having the structures: wherein a, b and c are integers from 0 to 12, X equals NH or CHNH2, R1 and R2 each is a hydrogen or a C1 to C20 aliphatic; aliphatic amine; an alicyclic; aromatic; heterocycle; and halogenated forms thereof; and wherein, a, b and c are integers from 0 to 12; R1, R2, R3, and R4 each is a hydrogen or a C1 to C20; aliphatic amine; an alicyclic; aromatic; a heterocycle; and halogenated forms thereof.
    Type: Grant
    Filed: July 1, 2005
    Date of Patent: June 17, 2008
    Assignee: MediQuest Therapeutics, Inc.
    Inventors: Mark R. Burns, Maralee McVean, Kevin Kennedy, Arthur Yeung, Bruce H. Devens
  • Patent number: 7276631
    Abstract: The present disclosure relates to chemical compounds and their use in human therapy. A specific embodiment of the disclosure relates to compounds of Formula (I); or an isomer, a pharmaceutically acceptable salt or solvate thereof or a pharmaceutically acceptable formulation comprising said compounds are useful for the useful for the treatment or prevention of conditions mediated by tachykinins and/or selective inhibition of serotonin reuptake transporter protein. The compounds act as dual NK-1 antagonists and selective serotonin reuptake inhibitors.
    Type: Grant
    Filed: July 18, 2005
    Date of Patent: October 2, 2007
    Assignee: Bristol-Myers Squibb Company
    Inventors: Yong-Jin Wu, Huan He
  • 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: 7211589
    Abstract: The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them. Wherein Z represents a bivalent organic group and the like of from 2 to 3 carbon atom(s) which may have a substituent; and R3 represents a carboxyl group and the like.
    Type: Grant
    Filed: April 25, 2002
    Date of Patent: May 1, 2007
    Assignee: Eisai R&D Management Co., Ltd.
    Inventors: Akinori Akaike, Hachiro Sugimoto, Yukio Nishizawa, Masahiro Yonaga, Naoki Asakawa, Naoki Asai, Nariyasu Mano, Taro Terauchi, Takashi Doko
  • Patent number: 7196226
    Abstract: The present invention relates to fluorination reagents comprising 1-fluoro-1-aminoolefins and also processes for preparing fluorination reagents comprising 1-fluoro-1-aminoolefins.
    Type: Grant
    Filed: December 16, 2004
    Date of Patent: March 27, 2007
    Assignee: Lanxess Deutschland GmbH
    Inventors: Wolfgang Ebenbeck, Albrecht Marhold
  • Patent number: 7164034
    Abstract: This invention relates to a method of treating a disorder selected from OCD, agoraphobia, agoraphobia without history of panic disorder, specific phobia, social phobia, PTSD, restless legs syndrome, premenstrual dysphoric disorder, hot flashes, and fibromyalgia by administering a compound of the formula 1 or a pharmaceutically acceptable salt thereof, wherein: R1 is hydrogen, straight or branched alkyl of from 1 to 6 carbon atoms or phenyl; and R2 is straight or branched alkyl of from 4 to 8 carbon atoms, straight or branched alkenyl of from 2 to 8 carbon atoms, cycloalkyl of from 3 to 7 carbon atoms, alkoxy of from 1 to 6 carbon atoms, -alkylcycloalkyl, -alkylalkoxy, -alkyl OH, -alkylphenyl, -alkylphenoxy, or -substituted phenyl. The invention also relates to a method of treating the above disorders by administering the compound (3S,5R)-3-Aminomethyl-5-methyl-octanoic acid.
    Type: Grant
    Filed: December 12, 2003
    Date of Patent: January 16, 2007
    Assignee: Pfizer Inc.
    Inventors: David James Dooley, Charles Price Taylor, Jr., Andrew John Thorpe, David Juergen Wustrow
  • 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: 6924394
    Abstract: Disclosed herein is a process for the manufacture of 2-(aminomethyl)-1-cyclopentylamine by low-pressure hydrogenation of 1-amino-2-cyano-1-cyclopentene using a combination catalyst system of nickel with palladium on carbon, or a single palladium-doped Raney-type catalyst.
    Type: Grant
    Filed: June 5, 2003
    Date of Patent: August 2, 2005
    Assignee: Invista North America S.r.l.
    Inventors: Ronald L. Amey, Ronald H. Mattson, Jr.
  • Patent number: 6919483
    Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF?) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF? and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF? and/or one or more other involved cytokines, alone or in combination with other agents.
    Type: Grant
    Filed: May 23, 2003
    Date of Patent: July 19, 2005
    Assignee: Mediquest Therapeutics, Inc.
    Inventors: Mark R. Burns, Maralee McVean, Kevin J. Kennedy, Arthur Yeung, Bruce H. Devens
  • Publication number: 20040266822
    Abstract: The present invention provides amine derivatives represented by formula I, its isomers, racemes or optical isomers, pharmaceutical salts thereof, its amides or esters, pharmaceutical compositions containing said compounds and the preparation methods thereof. The invention also relates to the use of the above mentioned compounds in the preparation of drugs for the prophylaxis or treatment of cardiovascular diseases, diabetes, bronchial and urinary smooth muscle spasm as well as ischemic and anoxic nerve injury. The above compounds can be used to treat hypertension, angina diaphragmatic, myocardial infarction, congestive heart failure, arrhythmia, diabetes, spasmodic bronchial diseases, spasmodic bladder or ureter diseases, and depression.
    Type: Application
    Filed: August 12, 2004
    Publication date: December 30, 2004
    Inventors: Hai Wang, Liuhong Yun, Huasong Feng, Fulin Li, Xingehun Tang, Huamei He, Rifang Yang, Wenyu Cui, Qixiu Gao, Gang Hu, Rusheng Zhao, Wei Liu, Chaoliang Long, Lin Wang, Xinqiang Lu, Lijun Liu, Yuan Yan
  • 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
  • Publication number: 20040235960
    Abstract: The synthesis and use of a novel class of tumor necrosis factor (TNF&agr;) inhibitors and immunomodulators are provided. These compounds have pharmacological applications as well as uses in assays relating to TNF&agr; and other involved cytokines. As pharmaceuticals, these compounds are used to treat inflammatory, infectious, autoimmune or other proliferative diseases and conditions related to the unwanted presence or activity of TNF&agr; and/or one or more other involved cytokines, alone or in combination with other agents.
    Type: Application
    Filed: May 23, 2003
    Publication date: November 25, 2004
    Inventors: Mark R. Burns, Maralee McVean, Kevin J. Kennedy, Arthur Yeung, Bruce H. Devens
  • Publication number: 20040230067
    Abstract: This invention provides antigen substance inductors which produce highly selective and/or specific vaccine precursor, vaccine, antibody (including idiotype antibody), neutralizing antibody, antitoxin.
    Type: Application
    Filed: February 26, 2004
    Publication date: November 18, 2004
    Inventors: Shozo Koyama, Satoshi Tanaka
  • Patent number: 6794545
    Abstract: Novel conformationally restricted polyamine analogs are provided, as well as compositions comprising these novel polyamine analogs. Methods of using the novel polyamine analogs in treatment of diseases such as cancer are also provided. Also provided is a method of delivering these analogs specifically to tumor cells by covalently attaching polyamine analogs to, porphyrin compounds, along with novel polyamine-porphyrin covalent conjugates.
    Type: Grant
    Filed: April 27, 2000
    Date of Patent: September 21, 2004
    Assignee: SLIL Biomedical Corporation
    Inventors: Benjamin Frydman, Laurence J. Marton, Venodhar K. Reddy, Aldonia Valasinas, Andrei V. Blokhin, Hirak S. Basu
  • Publication number: 20040180930
    Abstract: The present invention provides a novel compound exhibiting an excellent suppressing effect to cell injury caused by radicals and neurotoxicity induced by excitatory nuerotransmitters such as glutamate. Specifically, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
    Type: Application
    Filed: October 9, 2003
    Publication date: September 16, 2004
    Inventors: Akinori Akaike, Hachiro Sugimoto, Yukio Nishizawa, Masahiro Yonaga, Naoki Asakawa, Naoki Asai, Nariyasu Mano, Taro Terauchi, Takashi Doko
  • Publication number: 20040180967
    Abstract: N,N′-bis(3-aminopropyl)cyclohexane-1,4-diamine, of formula (I), is a new compound that is prepared by hydrogenation with Raney nickel catalyst of N,N′-bis(2-cyanoethyl)-cyclohexane-1,4-diamine, the latter being prepared by reaction between 1,4-cyclohexanediamine and acrylonitrile. The oral administration to genetically alcoholic rats (from the strain UChB of the University of Chile) of the tetrametanesulfonate monohydrate of (I) causes a significant reduction in the alcohol consumption. The activity lasts for some time after the treatment period. Besides, there is a virtually null disulfiram-like adverse effect, what constitutes an advantage over the unpleasant use of some anti-alcoholism agents, such as calcium cyanamide or disulfiram itself. Therefore, the compounds of the invention are useful for the preparation of medicaments for the therapeutic and/or prophylactic treatment of alcoholism in mammals, including human beings.
    Type: Application
    Filed: January 5, 2004
    Publication date: September 16, 2004
    Inventors: Norberto Bilbeny Lojo, Hernan Garcia Madrid, Maria Belen Font Arellano
  • Publication number: 20040106684
    Abstract: An object of the present invention is to provide a modified cyclic aliphatic polyamine having a low viscosity and a small content of unreacted polyamine which can provide, when it is used as a curing agent for epoxy resin, an epoxy resin composition having an improved workability without adding solvent or diluent and an excellent property of epoxy resin cure product. The above modified cyclic aliphatic polyamine is obtained by addition reaction of a cyclic aliphatic polyamine such as isophoronediamine and norbornanediamine and an alkenyl compound such as styrene. The modified cyclic aliphatic polyamine thus obtained is added in epoxy resin to be used as a curing agent for epoxy resin.
    Type: Application
    Filed: September 25, 2003
    Publication date: June 3, 2004
    Inventors: Takeshi Koyama, Tetsushi Ichikawa, Hisayuki Kuwahara, Masatoshi Echigo
  • Publication number: 20040039046
    Abstract: The present invention relates to novel scyphostatin analogues, which distinguish themselves by acting as SMase inhibitors so that they are of therapeutic use for a number of diseases such as a HIV infection, neurodegenerative diseases, inflammatory diseases, apoplexy, ischemia, myocardial infarction or in the case of atherosclerosis.
    Type: Application
    Filed: August 22, 2002
    Publication date: February 26, 2004
    Inventor: Hans-Peter Deigner
  • Publication number: 20030236225
    Abstract: Methods and compositions for treating disease caused by microorganisms, 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: Application
    Filed: May 17, 2002
    Publication date: December 25, 2003
    Inventors: Marina Nikolaevna Protopopova, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry
  • Patent number: 6642398
    Abstract: The instant invention is a series of novel mono- and disubstituted 3-propyl gamma aminobutyric acids of Formula I The compounds are useful as therapeutic agents in the treatment of epilepsy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, neuropathological disorders, arthritis, sleep disorders, IBS, and gastric damage. Methods of preparing the compounds and useful intermediates are also part of the invention.
    Type: Grant
    Filed: December 20, 2002
    Date of Patent: November 4, 2003
    Assignee: Warner-Lambert Company
    Inventors: Thomas Richard Belliotti, Justin Stephen Bryans, Ihoezo Victor Ekhato, Augustine Tobi Osuma, Robert Michael Schelkun, Jacob Bradley Schwarz, Andrew John Thorpe, Lawrence David Wise, David Juergen Wustrow, Po-Wai Yuen
  • Publication number: 20030195182
    Abstract: A triterpene derivative useful for the treatment of hepatic disorders is disclosed.
    Type: Application
    Filed: February 24, 2003
    Publication date: October 16, 2003
    Inventors: Kazue Sasaki, Nobuto Minowa, Shoji Nishiyama, Hiroyuki Kuzuhara