Benzyl Amines Having Hydroxy Or Ether Oxygen Bonded Directly To The Benzene Ring (h Of -oh May Be Replaced By A Substituted Or Unsubstituted Ammonium Ion Or A Group Ia Or Iia Light Metal) Patents (Class 564/389)
  • Publication number: 20150148301
    Abstract: The present invention relates to inhibitors of the activity of Complex (III) of the mitochondrial electron transport chain and use thereof in treatment and/or prevention of cancers presenting tumour-initiating cells. The present invention further relates to pharmaceutical compositions containing said inhibitors alone or in combination with other pharmaceutically active agents, and their use as medicaments or as agrochemicals where their properties as inhibitors of the mitochondrial respiration is of benefit.
    Type: Application
    Filed: May 23, 2013
    Publication date: May 28, 2015
    Inventors: Virginie Clement-Schatlo, Thomas Fessard, Damien Barbaras, Joana Matos, Erick Carreira
  • Publication number: 20150094294
    Abstract: The present disclosure provides compounds, specifically pyrimidin-4,6-dicarboxylic acid amide derivatives, or pharmaceutically acceptable salts thereof and pharmaceutical compositions containing said compounds. Also provided are methods for treating a mammal having malaria, or killing or inhibiting the growth of a Plasmodium species, comprising administering to said mammal or contacting said Plasmodium species with, an effective amount of a pyrimidin-4,6-dicarboxylic acid amide derivative.
    Type: Application
    Filed: February 28, 2013
    Publication date: April 2, 2015
    Inventors: Richard W. Scott, Robert W. Kavash, Wenxi Pan, Katie Freeman, Michael J. Costanzo, Doron Greenbaum, Yongjiang Xu, Trevor Young
  • Patent number: 8889163
    Abstract: Facially amphiphilic polyphenylene and heteroarylene polymers and articles made therform having biocidal surfaces are disclosed. The polymers can inhibit the growth of microorganisms in contact with the surface or in areas adjacent to said biocidal surface. There is also disclosed a methods to attach facially amphiphilic polmers to a solid support. Utility as a contact disinfectant is disclosed.
    Type: Grant
    Filed: March 7, 2002
    Date of Patent: November 18, 2014
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Gregory N. Tew, Michael L. Klein
  • Publication number: 20140316163
    Abstract: Disclosed are compounds represented by structural formula (I): methods of producing compounds represented by structural formula (I). and their use in inhibiting oxidation in an oxidizable material.
    Type: Application
    Filed: April 17, 2014
    Publication date: October 23, 2014
    Applicant: Polnox Corporation
    Inventors: Rajesh Kumar, Suizhou Yang, Vijayendra Kumar, Ashok L. Cholli
  • Publication number: 20140303232
    Abstract: This invention provides for a compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1-R4, L and X are defined herein. The compounds of formula (I) and pharmaceutically acceptable salts thereof are cationic lipids useful in the delivery of biologically active agents to cells and tissues.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: NOVARTIS AG
    Inventors: Jeremy Lee BARYZA, Rohan Eric John BECKWITH, Keith BOWMAN, Crystal BYERS, Tanzina FAZAL, Gabriel Grant GAMBER, Cameron Chuck-munn LEE, Ritesh Bhanudasji TICHKULE, Chandra VARGEESE, Shuangxi WANG, Laura Ellen West, Thomas ZABAWA, Junping ZHAO
  • Publication number: 20140256853
    Abstract: The present invention provides Mannich base derivatives of N,N?-dimethyl secondary diamine polymers including Mannich base derivatives of methylamine-terminated poly-(N-methylazetidine) and Mannich base derivatives of methylamine-terminated poly-(N-methylazacycloheptane). Amine curing agent compositions and amine-epoxy compositions containing Mannich base derivatives of N,N?-dimethyl secondary diamine polymers are also disclosed.
    Type: Application
    Filed: April 30, 2014
    Publication date: September 11, 2014
    Applicant: AIR PRODUCTS AND CHEMICALS, INC.
    Inventors: Frederick Herbert Walker, Michael Ian Cook, Gamini Ananda Vedage, Robert Marjo Theodoor Rasing
  • Patent number: 8716530
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: February 3, 2012
    Date of Patent: May 6, 2014
    Assignee: The Trustess of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Publication number: 20140039181
    Abstract: The invention relates to a method for producing a N-substituted amine compound by catalyzed alkylation. The method uses amine and alcohol or two kinds of amines as the reaction materials, employs composite metal oxides catalyst at a reaction temperature of 80-180° C. to catalyze the reaction for 6-36 hours, so as to produce the N-substituted amine compound. The reaction condition of the method of the invention is relatively moderate, using a catalyst made of cheap non-noble metals, which is non-caustic and easy to be separated and reused. The reaction does not need any medium and has relatively high conversion rate and selectivity.
    Type: Application
    Filed: December 28, 2012
    Publication date: February 6, 2014
    Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
    Inventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
  • Patent number: 8637713
    Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.
    Type: Grant
    Filed: December 5, 2012
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: Christian Mathes, Michael Foulkes, Martin Kesselgruber
  • Publication number: 20130310529
    Abstract: Use of homogeneous catalytic systems which include as a pre-catalyst a complex of a group 4 metal and a Salan ligand in the polymerization of alpha-olefins, is disclosed. The Salan ligand is characterized by a sequential diamino-containing skeleton unit which is non-symmetric, and the pre-catalysts can also be such that are devoid of a symmetry element. The disclosed polymerization results in alpha-olefin polymers such as polypropylene which are characterized by high levels of tacticity. Also disclosed are novel Salan ligands and novel complexes thereof with group 4 metals.
    Type: Application
    Filed: January 19, 2012
    Publication date: November 21, 2013
    Applicant: RAMOT AT TEL-AVIV UNIVERSITY LTD.
    Inventors: Moshe Kol, Konstantin Press
  • Publication number: 20130289076
    Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I) as described and defined herein, and their use in therapy, including, e.g., the treatment or prevention of cancer.
    Type: Application
    Filed: October 7, 2011
    Publication date: October 31, 2013
    Inventors: Julio Castro-Palomino Laria, Matthew Colin Thor Fyfe, Marc Murtinell Pedemonte, Alberto Ortega Muñoz, Núrla Valls Vidal
  • Publication number: 20130217910
    Abstract: The present invention relates to a process for the preparation of substituted N-(benzyl)cyclopropanamines of the general formula (II) starting from N-[(aryl)methylene]cyclopropanamine derivatives. The present invention further provides the N-[(arypmethylene]cyclopropanamine derivatives used as starting compounds in this process according to the invention, and their use for the preparation of substituted N (benzyl)cyclopropanamines.
    Type: Application
    Filed: November 4, 2011
    Publication date: August 22, 2013
    Inventors: Norbert Lui, Wahed Ahmed Moradi, Thomas Norbert Muller
  • Publication number: 20130101684
    Abstract: The present invention provides edible compositions comprising a compound of the present invention, food products comprising such edible compositions and methods of preparing such food products. The present invention also provides methods of reducing the amount of NaCl in a food product, methods of reducing the sodium intake in a diet, and methods of reducing bitter taste in a food product.
    Type: Application
    Filed: April 15, 2011
    Publication date: April 25, 2013
    Applicant: Chromocell Corporation
    Inventors: Jane V. Leland, Louise Slade, David Hayashi, William P. Jones, Peter H. Brown, Joseph Gunnet, Daniel Lavery, Jessica Langer, Kambiz Shekdar
  • Publication number: 20130096129
    Abstract: The present invention provides compounds of Formulae (A), (B), (C), and (D), pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof, pharmaceutical compositions thereof, and kits thereof. The present invention further provides methods of using the compounds to treat or prevent neurological disorders. In one aspect, the methods include administering to a subject in need of treatment for a neurological disorder a therapeutically effective amount of DAC-001, DAC-002, DAC-003, DAC-009, or DAC-012, or a compound of Formula (A), (B), (C), or (D).
    Type: Application
    Filed: July 20, 2012
    Publication date: April 18, 2013
    Inventors: Li-Huei Tsai, Ling Pan, Stephen J. Haggarty, Debasis Patnaik
  • Publication number: 20130096337
    Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.
    Type: Application
    Filed: December 5, 2012
    Publication date: April 18, 2013
    Applicant: Novartis AG
    Inventor: Novartis AG
  • Patent number: 8415508
    Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.
    Type: Grant
    Filed: December 17, 2009
    Date of Patent: April 9, 2013
    Assignee: Novartis AG
    Inventors: Christian Mathes, Michael Foulkes, Martin Kesselgruber
  • Publication number: 20120308640
    Abstract: The invention concerns compounds of the formula: X—(Y)t wherein: X is Formula (X), each Y is the same or different and is Formula (Y) —O—[CH2—CH(OH)—CH2—O—]m—H; or —C(OR5)3; R1, R2, R3, R6, R7, R8, R9, R10 are each, independently, —(CH2CH2O)m—R4, —[CH2CH(OH)CH2O]nH, OR11, —O(CH2)PR13, or —(CH2)R12; each R4 is independently OR5 or OH; R5, R11 and R12 are each, independently, H or C1-C30 alkyl; R13 is —NH3+Cl? or —NHBoc; t is an integer from 2 to 6; m, n, and p are each, independently, an integer from 1 to 12; and each q, r, and s is 0 or 1 and the sum of q+r+s is at least 2.
    Type: Application
    Filed: August 5, 2010
    Publication date: December 6, 2012
    Applicant: The Trustees of The University of Pennsylvania
    Inventors: Virgil Percec, Andrew D. Hughes, Pawaret Leowanawat, Daniela A. Wilson, Christopher J. Wilson
  • Patent number: 8324429
    Abstract: The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N—[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.
    Type: Grant
    Filed: January 10, 2008
    Date of Patent: December 4, 2012
    Assignees: Shanghai Institute of Pharmaceutical Industry, Zhejian Hisun Pharmaceutical Co., Ltd.
    Inventors: Fuli Zhang, Meng Hu, Meihua Xie, Anping Lai, Rentong Sun, Daoxin Chen, Rusheng Bao, Hua Bai
  • Publication number: 20120283249
    Abstract: The subject matter of the present invention is novel families of compounds which are aromatic amine, imine, aminoadamantane and benzodiazepine derivatives, medicaments comprising same and the use thereof as inhibitors of the toxic effects of toxins with intracellular activity, such as, for example, ricin, and of viruses that use the internalization pathway for infecting cells.
    Type: Application
    Filed: June 17, 2009
    Publication date: November 8, 2012
    Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
  • Patent number: 8293948
    Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.
    Type: Grant
    Filed: January 9, 2012
    Date of Patent: October 23, 2012
    Assignee: Jitsubo Co., Ltd.
    Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
  • Patent number: 8222456
    Abstract: The present invention discloses methods of use of facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, including, but not limited to, pharmaceutical uses of the polymers and oligomers as antimicrobial agents and as antidotes for hemorrhagic complications associated with heparin therapy. The present invention also discloses novel facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers, compositions of the novel polymers and oligomers, including pharmaceutical compositions, and methods of designing and synthesizing the facially amphiphilic polyaryl and polyarylalkynyl polymers and oligomers.
    Type: Grant
    Filed: January 21, 2005
    Date of Patent: July 17, 2012
    Assignee: The Trustees of the University of Pennsylvania
    Inventors: William F. DeGrado, Dahui Liu, Gregory N. Tew, Michael L. Klein
  • Publication number: 20120022281
    Abstract: Disclosed herein are novel intermediates and process for large scale production of (S)-3-[(1-dimethylamino)ethyl]phenyl-N-ethyl-N-methyl-carbamate (rivastigmine) or its pharmaceutically acceptable salts employing the novel intermediates. Further provided are methods for producing the novel intermediates thereof.
    Type: Application
    Filed: August 25, 2009
    Publication date: January 26, 2012
    Applicant: Jubilant Life Sciences Limited
    Inventors: Shailendra Kumar Dubey, Vikas Bansal, Kamaljeet Pannu, Sushil Kumar Dubey
  • Publication number: 20120010403
    Abstract: A production method of a compound containing a primary, secondary, or tertiary aminomethyl aromatic ring of the present invention includes: using a fluoroboron compound or a dimer thereof, or solvates thereof, which are represented by a formula (I): Ra(Rb)N—CH2—BF3M??(I) as an aminomethylating agent for an aromatic ring; and reacting the aminomethylating agent with an aromatic ring-containing compound, which can react with the aminomethylating agent, under the presence of a metal catalyst such as a palladium compound so as to perform the direct aminomethylation of the aromatic ring.
    Type: Application
    Filed: September 21, 2011
    Publication date: January 12, 2012
    Inventor: Keigo TANAKA
  • Patent number: 8093435
    Abstract: A reagent for organic synthesis with which a chemical reaction can be conducted in a liquid phase and unnecessary compound(s) can be easily separated at low cost from the liquid phase after completion of the reaction. The reagent for organic synthesis reversibly changes from a liquid-phase state to a solid-phase state with changes in solution composition and/or solution temperature, and is for use in organic synthesis reactions. This reagent for organic syntheses facilitates process development. With the reagent, research on and development of, e.g., medicines through, e.g., compound library synthesis, etc. can be accelerated. It can hence contribute to technical innovations in the biochemical industry and chemical industry.
    Type: Grant
    Filed: February 19, 2007
    Date of Patent: January 10, 2012
    Assignee: JITSUBO Co., Ltd.
    Inventors: Kazuhiro Chiba, Shokaku Kim, Yusuke Kono
  • Publication number: 20110301159
    Abstract: The disclosure relates to novel compounds that are capable of modulating Jak2 kinase activities, compounds that have therapeutic use in treating or preventing a subject suffering from or susceptible to a Jak2 mediated disease or disorder, and methods of use and compositions thereof.
    Type: Application
    Filed: December 9, 2009
    Publication date: December 8, 2011
    Applicants: UNIVERSITY OF SOUTH FLORIDA, UNIVERSITY OF FLORIDA RESEARCH FOUNDATION, INC.
    Inventors: Peter P. Sayeski, Gyorgy M. Keseru, Kirpal Bisht
  • Publication number: 20110184174
    Abstract: The present invention provides a compound of formula (IV) wherein R is Cl, Br, NO2, OH or OR?, and R? is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (?)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
    Type: Application
    Filed: June 2, 2009
    Publication date: July 28, 2011
    Applicant: CIPLA LIMITED
    Inventors: Dharmaraj Ramachandra Rao, Rajendra Narayanrao Kankan, Maruti Ghagare, Sandip Vasant Chikhalikar
  • Publication number: 20110160433
    Abstract: The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.
    Type: Application
    Filed: December 22, 2010
    Publication date: June 30, 2011
    Applicant: AJINOMOTO CO., INC.
    Inventor: Daisuke TAKAHASHI
  • Publication number: 20110040125
    Abstract: Disclosed are compounds represented by structural formula (I): methods of producing compounds represented by structural formula (I), and their use in inhibiting oxidation in an oxidizable material.
    Type: Application
    Filed: August 11, 2010
    Publication date: February 17, 2011
    Applicant: Polnox Corporation
    Inventors: Rajesh Kumar, Suizhou Yang, Vijayendra Kumar, Ashok L. Cholli
  • Publication number: 20100331234
    Abstract: Aminoalcohol lipidoids are prepared by reacting an amine with an epoxide-terminated compound are described. Methods of preparing aminoalcohol lipidoids from commercially available starting materials are also provided. Aminoalcohol lipidoids may be prepared from racemic or stereochemically pure epoxides. Aminoalcohol lipidoids or salts forms thereof are preferably biodegradable and biocompatible and may be used in a variety of drug delivery systems. Given the amino moiety of these aminoalcohol lipidoid compounds, they are particularly suited for the delivery of polynucleotides. Complexes, micelles, liposomes or particles containing the inventive lipidoids and polynucleotide have been prepared. The inventive lipidoids may also be used in preparing microparticles for drug delivery. They are particularly useful in delivering labile agents given their ability to buffer the pH of their surroundings.
    Type: Application
    Filed: March 3, 2010
    Publication date: December 30, 2010
    Applicant: Massachusetts Institute of Technology
    Inventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
  • Publication number: 20100311790
    Abstract: The object of the present invention is to provide a compound having excellent controlling effect on plant diseases. An amide compound represented by the following formula (I) has excellent controlling effect on plant diseases: wherein R1 is a hydrogen atom or a fluorine atom, and R2 is a C3-C8 linear alkenyl group or a C3-C8 linear alkynyl group.
    Type: Application
    Filed: November 21, 2008
    Publication date: December 9, 2010
    Applicant: SUMITOMO CHIEMCAL COMPANY LIMITED
    Inventors: Hiroshi Sakaguchi, Mayumi Kubota
  • Publication number: 20100286437
    Abstract: The present invention provides N-methylethylcarbamino-3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenyl ester represented by formula (II) and its preparation method. The present invention also provides (S)-1-(3-methoxyphenyl)-N-methyl-N—[(S)-1-phenylethyl]ethylamine and 3-[(S)-1-(methyl-[(S)-1-phenylethyl]amino)ethyl]phenol as intermediates of the compound represented by formula (II), and the use of the compound represented by formula (II) for preparing rivastigmine used for treating Alzheimer disease.
    Type: Application
    Filed: January 10, 2008
    Publication date: November 11, 2010
    Inventors: Fuli Zhang, Meng Hu, Meihua Xie, Anping Lai, Rentong Sun, Daoxin Chen, Rusheng Bao, Hua Bai
  • Publication number: 20100227884
    Abstract: The object of the present invention is to provide a compound having excellent controlling effect on plant diseases. An amide compound represented by the following formula (I) has excellent controlling effect on plant diseases: (in the formula, R denotes a C1-C5 straight-chain alkyl group).
    Type: Application
    Filed: October 7, 2008
    Publication date: September 9, 2010
    Applicant: Sumitomo Chemical Company, Limited
    Inventors: Mayumi Kubota, Takashi Komori
  • Publication number: 20100168229
    Abstract: A catalytic process for the preparation of optically active compounds and their conversion thereafter to desired drug substances. In particular, the process relates to the preparation of (S)-3-(1-Dimethylamino-ethyl)-phenol using asymmetric catalytic reduction and transfer hydrogenation, thereby providing an improved route to forming drug substances such as rivastigimine and rivastigimine hydrogen tartrate.
    Type: Application
    Filed: December 17, 2009
    Publication date: July 1, 2010
    Inventors: Christian Mathes, Michael Foulkes, Martin Kesselgruber
  • Publication number: 20100129471
    Abstract: The invention relates to a compound of the formula (I) in which: R1, R2 and R3 are independently a methoxy group optionally substituted by one or more fluorine atoms; R4 is a hydrogen atom; R5 and R6 are identical and each represent a hydrogen or fluorine atom; A is a cycle selected from the group including aryl and heteroaryl groups, wherein said groups can be substituted.
    Type: Application
    Filed: April 4, 2008
    Publication date: May 27, 2010
    Inventors: Mouâd Alami, Jean-Daniel Brion, Olivier Provot, Jean-François Peyrat, Samir Messaoudi, Abdallah Hamze, Anne Giraud, Jérôme Bignon, Joanna Bakala, Jian-Miao Liu
  • Publication number: 20100130784
    Abstract: Substituted 1,1,1-trifluoro-3-[(benzyl)-(pyrimidin-2-yl)-amino]-propan-2-ol compounds, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
    Type: Application
    Filed: February 13, 2006
    Publication date: May 27, 2010
    Inventors: George Chang, Michael Patrick Pence
  • Publication number: 20090275611
    Abstract: Compounds are provided which bind to and are agonist, antagonists or inverse agonists of the CB2 receptor, the compounds having the general formula (I) wherein R1, R2, R3, X and Ar have the meanings given in the specification, and the preparation and use thereof. The compounds are valuable CB2 receptor modulators, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.
    Type: Application
    Filed: April 2, 2007
    Publication date: November 5, 2009
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
  • Patent number: 7445645
    Abstract: The present disclosure relates to novel N-alkylhydroxylated secondary para-phenylenediamine compounds, to a composition for dyeing keratin fibers, for instance human keratin fibers such as the hair, comprising, in a medium that is suitable for dyeing, at least one ortho- and/or meta-substituted N-alkylhydroxylated secondary para-phenylenediamine, to a process for dyeing keratin fibers comprising applying this composition, and also a dyeing “kit.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: November 4, 2008
    Assignee: L'Oreal S.A.
    Inventors: Stéphane Sabelle, Philippe Breton, Alex Junino
  • Patent number: 7435268
    Abstract: The present disclosure relates to novel N-alkylhydroxylated secondary para-phenylenediamines and a process for making these compounds. The present disclosure further relates to a composition for dyeing keratin fibers, including human keratin fibers such as hair, containing, in a medium that is suitable for dyeing, at least one such N-alkylhydroxylated secondary para-phenylenediamine, a process for dyeing keratin fibers using the composition, and a device or kit for dyeing keratin fibers that contains the composition.
    Type: Grant
    Filed: February 28, 2005
    Date of Patent: October 14, 2008
    Assignee: L'Oreal S.A.
    Inventors: Stéphane Sabelle, Eric Metais
  • Publication number: 20080200535
    Abstract: There is provided a compound exhibiting an activity of suppressing immune response with reduced adverse drug reactions, which compound is useful in the chemotherapy for preventing or treating, for example, a wide range of various autoimmune diseases including systemic erythematodes, chronic rheumatoid arthritis, Type I diabetes, inflammatory bowel disease, biliary cirrhosis, uveitis, multiple sclerosis or other disorders, or chronic inflammatory diseases, or cancers, lymphoma or leukemia, or resistance to organ or tissue transplantation or rejection against transplantation. Novel amine compounds having an S1P1/Edg1 receptor agonist effect, possible stereoisomers or racemic bodies of the compounds, or pharmacologically acceptable salts, hydrates or solvates of the compound, the stereoisomers or the racemic bodies, or prodrugs of the compounds, the stereoisomers, the racemic bodies, the salts, the hydrates or the solvates, are provided.
    Type: Application
    Filed: August 24, 2007
    Publication date: August 21, 2008
    Applicant: Asahi Kasei Pharma Corporation
    Inventors: Yutaka Ohmori, Masakazu Komatsu
  • Patent number: 6861561
    Abstract: The invention relates to substituted aromatic polycyclic tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases.
    Type: Grant
    Filed: September 26, 2002
    Date of Patent: March 1, 2005
    Assignee: G. D. Searle & Co.
    Inventors: James A. Sikorski, Richard C. Durley, Mark A. Massa, Jane L. Wang, Deborah A. Mischke, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6855711
    Abstract: Use of a compound of formula (I), wherein R1 is H or hydrocarbyl; R2 is a hydrophobic radical; R3 is 3-(C2-C6)acyl-4-hydroxyphenyl, 3-hydroxyimino (C2-C6)-alkyl-4-hydroxyphenyl, or COOZ, wherein Z is H, (C1-C6) alkyl, aryl, aryl or ar(C1-C6) alkyl; and n is 1-20; and of a compound of formula (II), wherein R4 is (C1-C6) alkyl, cyano (C1-C6) alkyl, (C1-C6) alkoxy (C1-C6) alkyl or —CH2NR7R8, wherein R7 and R8, the same or different, is each H or (C1-C6) alkyl, or together with the N atom form a saturated or unsaturated 5-7 membered ring optionally containing a further heteroatom selected from N, O or S, the further N atom being optionally substituted, and either R5 is H and R6 is (C2-C6) acyl or hydroxyimino (C2-C6) alkyl, or R5 and R6 together with the phenyl ring form a quinoline, a 1,2,3,4-tetrahydroquinoline or a perhydroquinoline ring, for the preparation of pharmaceutical compositions for the treatment of Parkinson's disease or stroke.
    Type: Grant
    Filed: June 7, 2000
    Date of Patent: February 15, 2005
    Assignees: Yeda Research and Development Co. Ltd., Technion Research and Development Foundation Ltd.
    Inventors: Rivka Warshawsky, Moussa B. H. Youdim, Dorit Ben-Shachar, Abraham Warshawsky
  • Patent number: 6828443
    Abstract: A hybrid dye is provided that is useful for coloring keratin fibers and skin. The hybrid dye has the structure X-S-Y, where X is derived from a substantive dye, Y is derived from an oxidation dye precursor or a melanin precursor, and S is a direct bond or spacer group. The present invention also provides a composition for coloring keratin fibers that contains the hybrid dye.
    Type: Grant
    Filed: June 13, 2002
    Date of Patent: December 7, 2004
    Assignee: Henkel Kommanditgesellschaft auf Aktien
    Inventors: Detlef Hollenberg, Horst Hoeffkes, Frank Naumann, David Rose, Leszek J. Wolfram, Joachim-Kurt Foitzik
  • Publication number: 20040192969
    Abstract: Diol-functionalized antioxidants and the process for the preparation thereof are disclosed and have the general formula (I): 1
    Type: Application
    Filed: March 25, 2003
    Publication date: September 30, 2004
    Applicant: COUNCIL OF SCIENTIFIC AND INDUSTRIAL RESEARCH
    Inventors: Shailendra Singh Solanky, Shrojal Mohitkumar Desai, Raj Pal Singh
  • Patent number: 6787570
    Abstract: The invention relates to substituted N-Alkyl/Alkenyl/Cycloalkyl/Heterocycyl N-Aryl/Heteroaryl tertiary-Heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery disease. Preferred tertiary-heteroalkylamine compounds are substituted N-cycloalkyl N-benzyl aminoalcohols.
    Type: Grant
    Filed: December 16, 2002
    Date of Patent: September 7, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Deborah A. Mischke, Emily J. Reinhard, Barry L. Parnas, Melvin L. Rueppel
  • Patent number: 6770785
    Abstract: The present invention relates to a novel antiozonant as well as antioxidant based on functionalized hindered phenol and the process for the preparation thereof of formula 1 wherein R1 is tert-butyl and R2 and R3 are C1 to C8 linear or branched alkyl. The present invention also relates to a process for the preparation thereof comprising dissolving a compound of formula 3 wherein R1 is tert-butyl, with liquid bromine in a non polar organic solvent at temperature range 80 to 95° C. for a period of 4 to 7 hours, evaporating the solvent under reduced pressure to obtain a compound of formula 2 wherein R1 is a tertiary butyl group and X is Br, reacting the compound of formula 2 with a compound of formula 4 wherein R2 and R3 are C1 to C8 linear or branched alkyl, dissolved in an organic solvent in presence of a suitable mild base at a temperature ranging from 80 to 95° C.
    Type: Grant
    Filed: March 25, 2003
    Date of Patent: August 3, 2004
    Assignee: Council of Scientific and Industrial Research
    Inventors: Shrojal Mohitkumar Desai, Shailendra Singh Solanky, Raj Pal Singh
  • Patent number: 6765023
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N,N-disubstituted reverse aminoalcohols.
    Type: Grant
    Filed: May 23, 2002
    Date of Patent: July 20, 2004
    Assignee: Pfizer, Inc.
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: 6759554
    Abstract: The present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide or amine moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In additional embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between a nitrogen atom of an acyl hydrazine and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of a nitrogen-containing heteroaromatic, e.g., indole, pyrazole, and indazole, and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate.
    Type: Grant
    Filed: April 24, 2002
    Date of Patent: July 6, 2004
    Assignee: Massachusetts Institute of Technology
    Inventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
  • Publication number: 20040110767
    Abstract: The present invention provides estrogen receptor (ER) ligands of structural formula (I) 1
    Type: Application
    Filed: September 17, 2003
    Publication date: June 10, 2004
    Applicant: Pfizer Inc
    Inventors: Kimberly O. Cameron, Richard Chesworth
  • Patent number: 6723753
    Abstract: The invention relates to substituted polycyclic aryl and heteroaryl tertiary-heteroalkylamine compounds useful as inhibitors of cholesteryl ester transfer protein (CETP; plasma lipid transfer protein-I) and compounds, compositions and methods for treating atherosclerosis and other coronary artery diseases. Preferred tertiary-heteroalkylamine compounds are substituted N-benzyl-N-phenyl aminoalcohols.
    Type: Grant
    Filed: February 7, 2002
    Date of Patent: April 20, 2004
    Assignee: Pharmacia Corporation
    Inventors: James A. Sikorski, Richard C. Durley, Deborah A. Mischke, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Margaret L. Grapperhaus, Brian S. Hickory, Mark A. Massa, Monica B. Norton, William F. Vernier, Barry L. Parnas, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
  • Patent number: RE39530
    Abstract: 3-amino-3-arylpropan-1-ol compounds corresponding to the formula I in which R1 to R5, A and X have the meanings according to claim 1, and their preparation and use as medicaments.
    Type: Grant
    Filed: September 11, 2003
    Date of Patent: March 27, 2007
    Assignee: Gruenenthal GmbH
    Inventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann