Benzyl Amines Wherein The Benzene Ring Has No Other Substituents Patents (Class 564/391)
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Patent number: 10703833Abstract: Described herein is a polymer comprising: interpolymerized units of (i) a fluorinated terminal alkene monomer and (ii) a tertiary amine-containing fluorinated monomer comprising at least one of a vinyl amine, a substituted vinyl amine, an allyl amine, a substituted allyl amine, and combinations thereof; wherein the polymer can be amorphous or semi-crystalline with a melting point no greater than 325° C. Dispersions thereof and methods of making and using the same are also described.Type: GrantFiled: December 13, 2016Date of Patent: July 7, 2020Assignee: 3M Innovative Properties CompanyInventors: Michael J. Bulinski, Michael G. Costello, Denis Duchesne, Klaus Hintzer, William M. Lamanna, Kai H. Lochhaas, Michael J. Parent, Sean M. Smith
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Publication number: 20150119589Abstract: This invention relates to methods for making oxetan-3-ylmethanamines having the formula (I) wherein R1? and R2? are as defined herein. The methods of the invention provide the compounds of formula (I) in high yields and under conditions amenable for large-scale commercial production.Type: ApplicationFiled: May 1, 2013Publication date: April 30, 2015Inventors: Magnus Carl Arne Eriksson, Suresh R. Kapadia, Jonathan Timothy Reeves, Xingzhong Zeng
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Publication number: 20150119581Abstract: A method of preparing a porous graphene oxide material. The method includes the steps of: (1) preparing graphene oxide sheets from graphite at 40 to 170° C.; (2) providing a graphene oxide suspension containing the graphene oxide sheets; (3) heating the graphene oxide suspension with a base at 25 to 300° C. for 0.1 to 48 hours to obtain base-treated graphene oxide sheets; and (4) heating a mixture of the base-treated graphene oxide sheets and an acid at 25 to 300° C. for 0.1 to 48 hours to yield the porous graphene oxide material. Also disclosed are novel porous graphene oxide materials and methods of using these materials as catalysts.Type: ApplicationFiled: June 18, 2013Publication date: April 30, 2015Inventors: Kian Ping Loh, Chen Liang Su
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Publication number: 20150105559Abstract: Disclosed is a method for producing a compound having an amino group and/or a hydroxyl group from a substrate compound having an atomic group containing CO or CS by eliminating such atomic group. The substrate compound, having an atomic group containing CO or CS (for example, an amide, a carbamate, or the like), is allowed to react with a compound expressed by formula (I) below, at a temperature of 120° C. or lower, preferably in the presence of an ammonium salt, to eliminate such atomic group containing CO or CS. In formula (I) A may not be present, and in a case where A is present, A represents an alkyl group having 1 to 6 carbon atoms. H2N-A—NH2 (I) - - -.Type: ApplicationFiled: March 4, 2013Publication date: April 16, 2015Applicant: Kyushu University, National University CorporationInventors: Takashi Ohshima, Hiroyuki Morimoto, Yuhei Shimizu
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Publication number: 20140235729Abstract: Herbal compositions and techniques for suppressing appetite and managing weight are described. These compositions and techniques are based at least in part on beneficial results showing that benzylamine can suppress appetite. In at least one embodiment, a composition that includes an effective amount of benzylamine and an effective amount of at least one benzylamine enhancer may be utilized for appetite suppression.Type: ApplicationFiled: February 17, 2014Publication date: August 21, 2014Applicant: ZIJA INTERNATIONAL, INC.Inventor: Joshua James Plant
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Patent number: 8791201Abstract: The present invention relates to a compound characterized by the following formula: wherein each R1 is independently methyl or ethyl; and n 1 to 10. The compound is useful in preparing hydrophobically modified alkylene oxide urethane polymers, which are useful as rheology modifiers for coatings formulations.Type: GrantFiled: April 18, 2013Date of Patent: July 29, 2014Assignee: Rohm and Haas CompanyInventors: John J. Rabasco, Barrett R. Bobsein
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Patent number: 8742175Abstract: The present invention discloses novel aromatic ketone compounds with functional substitution groups at para- or meta positions which can be used as photo-initiators or effective components of photo-initiator mixtures for the photopolymerizations of ethylenically unsaturated systems. The preparation of these compounds is also disclosed.Type: GrantFiled: November 4, 2011Date of Patent: June 3, 2014Assignee: Shenzhen UV-Chemtech Co., Ltd.Inventors: Yongbo Zhang, Yanchao Wang, Yapeng Wang, Huaihai Song, Zhigang Wang
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Patent number: 8658789Abstract: A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetic acid salt; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetic acid salt obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetic acid salt of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture.Type: GrantFiled: January 8, 2010Date of Patent: February 25, 2014Assignee: Lianhe Chemical Technology Co., Ltd.Inventors: Ping Wang, Qiangbiao Pan, Yangzhou Li, Daoliang Zheng
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Publication number: 20140039181Abstract: 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: ApplicationFiled: December 28, 2012Publication date: February 6, 2014Applicant: Lanzhou Institute of Chemical Physics, Chinese Academy of SciencesInventor: Lanzhou Institute of Chemical Physics, Chinese Academy of Sciences
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Patent number: 8569544Abstract: The present invention provides a simple method for preparation of benzphetamine and its acid addition salt comprising reaction of methamphetamine hydrochloride of formula (III) with benzyl chloride and treating the isolated benzphetamine of formula (II) with an acid dissolved in an organic solvent to provide benzphetamine acid addition salt, more specifically, benzphetamine hydrochloride of formula (I).Type: GrantFiled: August 18, 2010Date of Patent: October 29, 2013Assignee: Emcure Pharmaceuticals LimitedInventors: Mukund Keshav Gurjar, Narendra Kumar Tripathy, Kiran Avinash Bapat, Vemavarapu P. K. V. Rao, Satyajeet Binay Biswas, Samit Satish Mehta
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Publication number: 20130281617Abstract: The present invention relates to a compound characterized by the following formula: where R1, R2, Y, m, and p are described herein. The compound of the present invention is useful as a precursor to hydrophobically modified alkylene oxide urethane polymers, which are useful as rheology modifiers for coatings formulations.Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Inventors: John J. Rabasco, Barrett R. Bobsein
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Publication number: 20130281639Abstract: The present invention relates to a compound characterized by the following formula: wherein each R1 is independently methyl or ethyl; and n 1 to 10. The compound is useful in preparing hydrophobically modified alkylene oxide urethane polymers, which are useful as rheology modifiers for coatings formulations.Type: ApplicationFiled: April 18, 2013Publication date: October 24, 2013Inventors: John J. Rabasco, Barrett R. Bobsein
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Publication number: 20130217877Abstract: The present invention discloses novel aromatic ketone compounds with functional substiution groups at para- or meta positions which can be used as photo-initiators or effective components of photo-initiator mixtures for the photopolymerizations of ethylenically unsaturated systems. The preparation of these compounds is also disclosed.Type: ApplicationFiled: November 4, 2011Publication date: August 22, 2013Applicant: SHENZHEN UV-CHEMTECH CO., LTDInventors: Yongbo Zhang, Yanchao Wang, Yapeng Wang, Huaihai Song, Zhigang Wang
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Publication number: 20130202994Abstract: To provide an amine compound, represented by General Formula (I) below: [In General Formula (I), R1 and R2 represent a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aromatic hydrocarbon group, which may be identical or different; m and n are an integer of 1 or 0; Ar1 represents a substituted or unsubstituted aromatic hydrocarbon group; Ar2 and Ar3 represent a substituted or unsubstituted alkyl group, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted aromatic hydrocarbon group; and Ar1 and Ar2 or Ar2 and Ar3 may bind to each other to form a substituted or unsubstituted heterocyclic group including a nitrogen atom.Type: ApplicationFiled: January 29, 2013Publication date: August 8, 2013Inventors: Tomoyuki SHIMADA, Masayoshi NOMURA, Ryota ARAI
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Publication number: 20120283249Abstract: 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: ApplicationFiled: June 17, 2009Publication date: November 8, 2012Inventors: Roman Lopez, Séverine Hebbe, Daniel Gillet, Julien Barbier
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Patent number: 8212080Abstract: A method of producing xylylenediamine by the hydrogenation of dicyanobenzene obtained by the ammoxidation of xylene in a high yield while prolonging the catalyst life. In the method, a molten dicyanobenzene from which compounds having a boiling point lower than that of dicyanobenzene have been removed but compounds having a boiling point higher than that of dicyanobenzene are not removed is dissolved in a solvent containing liquid ammonia. By this dissolution, at least part of dicyanobenzene polymers precipitates as insolubles. The precipitates are removed by a solid-liquid separation. By subjecting the resulting solution containing the dicyanobenzene polymers in a reduced amount to hydrogenation, xylylenediamine is produced in a high yield and the life time of hydrogenation catalyst is prolonged.Type: GrantFiled: December 8, 2009Date of Patent: July 3, 2012Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Tatsuyuki Kumano, Kenji Nakaya, Shinichi Nagao
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Publication number: 20120027844Abstract: Compounds and their syntheses are disclosed herein. Compositions and pharmaceutical compositions comprising a compound are also described, and include compositions also comprising liposomes. Methods for the treatment of cancer in animals comprising administering a compound or a composition comprising a compound are also described.Type: ApplicationFiled: February 9, 2010Publication date: February 2, 2012Applicants: XAVIER UNIVERSITY OF LOUISIANA, TULANE UNIVERSITYInventors: Barbara S. Beckman, Maryam Foroozesh, Jiawang Liu
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Publication number: 20110275805Abstract: A method for preparing the linezolid (compound 1), which comprises the steps of: (1) carrying out the debenzyl reaction of compound 4 in solvent, to obtain the compound 5 or its acetate; (2) carrying out the acetylation reaction in the amino of the compound 5 or its acetate obtained in step (1) in solvent to obtain the compound 1. The intermediates to prepare the compound 1 and the acetate of compound 5. The present preparation method is easy to obtain the chiral materials and the chiral materials are cheap, the process and the post treatment are simple, the intermediate products and the end product are easy to be purified, the total yield is high, their purities are also high, this preparation method is easy to be used in the industry manufacture.Type: ApplicationFiled: January 8, 2010Publication date: November 10, 2011Applicant: LIANHE CHEMICAL TECHNOLOGY CO., LTD.Inventors: Ping Wang, Qiangbiao Pan, Yangzhou Li, Daoliang Zheng
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Publication number: 20110184071Abstract: The present invention relates to an improved process for the preparation of rasagiline (1) and its pharmaceutically acceptable salts. In particular it relates to a process for preparing rasagiline (1) and its salts substantially free from impurities.Type: ApplicationFiled: June 2, 2009Publication date: July 28, 2011Inventors: Vinayak Gore, Bindu Manojkumar, Sandeep Sonawane, Dattatrey Kokane, Sinderpal Tank
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Publication number: 20110112282Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof, in which each compound is adapted to occupy the binding site of human IDO, which comprises a large hydrophobic pocket A and a second, proximal hydrophobic pocket B, the compound comprising at least one of the following elements: (i) a large hydrophobic fragment to substantially fill pocket A in the binding site of human IDO; (ii) an atom that can coordinate to the heme iron of human IDO, (iii) a positively charged group that can form a salt-bridge with the heme 7-propionate of the human IDO; (iv) a negatively charged group that can form a salt-bridge with Arg231 of the human IDO; (v) a hydrophobic group that can form van der Waals interactions with pocket B; and (vi) one or more substituents that can hydrogen bond to Ser167 and to Gly262, and as IDO inhibitors and their therapeutic use, eg in the treatment of cancer.Type: ApplicationFiled: April 15, 2009Publication date: May 12, 2011Inventors: Ute Roehrig, Loay Awad, Olivier Michelin, Benoit Van Den Eynde, Luc Pilotte, Vincent Stroobant, Pierre Larrieu
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Publication number: 20100331234Abstract: 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: ApplicationFiled: March 3, 2010Publication date: December 30, 2010Applicant: Massachusetts Institute of TechnologyInventors: Kerry Peter Mahon, Kevin Thomas Love, Christopher Gerard Levins, Kathryn Ann Whitehead, Robert S. Langer, Daniel G. Anderson
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Publication number: 20100234596Abstract: [Problem] The present invention aims to provide a novel organometallic compound that can be used as a general-use highly active catalyst with superior selectivity for functional groups. [Means for Solving Problem] The present invention relates to an organometallic compound having a novel specific structure of general formula (1): and to a general-use highly active catalyst used in reductive amination reaction with superior selectivity for functional groups that comprises said organometallic compound, and to a process for preparing amine compounds by reductive amination reaction using said catalyst.Type: ApplicationFiled: March 12, 2010Publication date: September 16, 2010Applicant: Kanto Kagaku Kabushiki KaishaInventors: Masahito Watanabe, Junichi Hori, Kunihiko Murata
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Publication number: 20100104629Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.Type: ApplicationFiled: September 10, 2009Publication date: April 29, 2010Applicant: ABBOTT LABORATORIESInventors: Prasad A. Dande, Todd M. Hansen, Robert D. Hubbard, Aparna V. Sarthy, Yu Shen, Lu Tian, Carol K. Wada, Xiaobin Zhao
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Publication number: 20090263407Abstract: Cationic lipids, cationic lipid based drug delivery systems, ways to make them and methods of treating diseases using them are disclosed.Type: ApplicationFiled: April 16, 2009Publication date: October 22, 2009Applicant: ABBOTT LABORATORIESInventors: Prasad A. Dande, Todd M. Hansen, Robert D. Hubbard, Carol K. Wada, Lu Tian, Xiaobin Zhao
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Publication number: 20080267813Abstract: Corrosion inhibitor and method of protecting metallic materials in strongly alkaline medium by means of a corrosion inhibitor, characterized in that it contains an amine containing at least one CH group bound to the nitrogen.Type: ApplicationFiled: June 23, 2008Publication date: October 30, 2008Inventors: Lutz Heuer, Stylianos Savakis, Helmut Diekmann, Eberhard Zirngiebl
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Publication number: 20080262268Abstract: There is disclosed a method for the crystallization of benzphetamine hydrochloride from an organic medium by the steps of removing water from the system to a very low level and then reducing the temperature of the organic medium to provide crystallization of the acid salt. In the event that crystallization does not occur upon lowering the temperature of the medium, it has been discovered that gentle heating of the organic medium results in crystallization of the acid salt. It has also been discovered that higher temperature crystallization has been provided by removal of methamphetamine from the composition. The crystalline benzphetamine hydrochloride can then be isolated by typical liquid/solid separation means such as filtration or centrifugation.Type: ApplicationFiled: November 2, 2005Publication date: October 23, 2008Inventors: Dennis J. Kalota, Keith G. Tomazi
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Patent number: 7432399Abstract: 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: GrantFiled: November 2, 2004Date of Patent: October 7, 2008Assignee: The United States of America as represented by the Secretary of the NavyInventors: Jozef Verborgt, Arthur Anthony Webb
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Publication number: 20080207913Abstract: The present invention provides bifunctional polymers, methods of preparing the same, and intermediates thereto. These compounds are useful in a variety of applications including the PEGylation of biologically active molecules. The invention also provides methods of using said compounds and compositions thereof.Type: ApplicationFiled: April 27, 2007Publication date: August 28, 2008Applicant: Intezyne TechnologiesInventors: Kurt Breitenkamp, Kevin N. Sill, Habib Skaff
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Publication number: 20070255057Abstract: A method of nitrating a compound selected from the group consisting of is provided.Type: ApplicationFiled: February 27, 2007Publication date: November 1, 2007Inventors: Miall Cedilote, Thomas Patrick Cleary, Pingsheng Zhang
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Patent number: 6951958Abstract: Described is method for preparing tertiary amines comprising sequential, exhaustive alkylation of a hydroxylamine derivative and cleavage of the O—N bond using the following steps: a) reacting the hydroxylamine derivative with an alkylating agent or with a carbonyl compound to form an oxime intermediate. b) reacting the oxime intermediate with a reducing agent to produce an alkylated derivative c) reacting the alkylated derivative with an alkylating agent or a carbonyl compound in the presence of a reducing agent to produce a dialkylated derivative d) reacting the dialkylated derivative with an alkylating agent to produce a quaternized derivative e) reacting the quaternized derivative with a reagent causing cleavage of the O—N bond to produce a tertiary amine.Type: GrantFiled: August 3, 2000Date of Patent: October 4, 2005Assignee: Acadia Pharmaceuticals Inc.Inventors: Carl-Magnus A. Andersson, Magnus Gustafsson, Kent R. I. Olsson
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Patent number: 6849767Abstract: A method of hydroborating an alkene or alkyne, or reducing an organic functionality, oxidizing primary and secondary alcohols using a fluorous borane-sulfide is disclosed. The method includes regeneration and recycling the fluorous borane-sulfide.Type: GrantFiled: July 24, 2003Date of Patent: February 1, 2005Assignee: The Board of Trustees of the University of IllinoisInventors: David C. Crich, Santhosh Neelamkavil
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Patent number: 6765023Abstract: 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: GrantFiled: May 23, 2002Date of Patent: July 20, 2004Assignee: 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
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Patent number: 6759554Abstract: 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: GrantFiled: April 24, 2002Date of Patent: July 6, 2004Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Artis Klapars, Jon C. Antilla, Gabriel E. Job, Martina Wolter, Fuk Y. Kwong, Gero Nordmann, Edward J. Hennessy
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Patent number: 6723753Abstract: 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: GrantFiled: February 7, 2002Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6723752Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1 )-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N-benzyl-N-phenyl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: April 20, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6713135Abstract: The present invention provides novel polyimides, poly(amic acids) and poly(amide esters) thereof, and optical alignment layers derived therefrom, for inducing alignment of liquid crystals and liquid crystal displays. The novel compositions comprise side-chain polymers of the general formula I —L1—D—L2—Cf wherein D comprises 1 to 4 carbon-carbon double bonds, Cf is a monovalent C4 to C20 fluorocarbon radical and L1 and L2 are linking groups. The invention further describes liquid crystal displays and other liquid crystal devices.Type: GrantFiled: December 19, 2000Date of Patent: March 30, 2004Assignee: Elsicon, Inc.Inventors: Wayne M. Gibbons, Patricia A. Rose, Paul J. Shannon, Hanxing Zheng
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Patent number: 6683099Abstract: 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 cycloalkyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 27, 2004Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6683113Abstract: The invention relates to substituted aryl and heteroaryl (R)-Chiral Halogenated 1-Substitutedamino-(n+1)-Alkanol 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. Novel high yield, stereoselective processes for the preparation of the chiral substituted alkanol compounds from chiral and achiral intermediates are described. Preferred (R)-Chiral 1-Substitutedamino-(n+1)-Alkanol compounds are substituted (R)-Chiral N,N-bis-benzyl aminoalcohols.Type: GrantFiled: December 12, 2001Date of Patent: January 27, 2004Assignee: Pharmacia CorporationInventors: James A. Sikorski, Richard C. Durley, Margaret L. Grapperhaus, Mark A. Massa, Emily J. Reinhard, Yvette M. Fobian, Michael B. Tollefson, Lijuan Wang, Brian S. Hickory, Monica B. Norton, William F. Vernier, Deborah A. Mischke, Michele A. Promo, Ashton T. Hamme, Dale P. Spangler, Melvin L. Rueppel
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Patent number: 6677375Abstract: 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-bis-benzyl aminoalcohols.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6677380Abstract: 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 mercapto amines.Type: GrantFiled: May 23, 2002Date of Patent: January 13, 2004Assignee: Pharmacia CorporationInventors: 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
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Patent number: 6515180Abstract: The invention relates to a method for symmetrically disubstituting carboxylic acid amides on the geminal carbonyl-C-atom using grignard reagents in the presence of a metal alcoholate compound used as a catalyst and in the presence of another organometalic compound used as a co-catalyst.Type: GrantFiled: March 7, 2001Date of Patent: February 4, 2003Assignee: Merck Patent GesellschaftInventors: Herwig Buchholz, Urs Welz-Biermann, Armin Meijere
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Patent number: 6512145Abstract: The invention relates to a method for asymmetrically disubstituting carboxylic acid amides on the geminal carbonyl-C-atom using two grignard reagents in the presence of a metal alcoholate compound used as a catalyst and in the presence of another organometalic compound used as a co-catalyst.Type: GrantFiled: February 23, 2001Date of Patent: January 28, 2003Assignee: Merck Patent GesellschaftInventors: Herwig Buchholz, Urs Welz-Biermann
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Patent number: 6479661Abstract: 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: GrantFiled: March 23, 2001Date of Patent: November 12, 2002Assignee: Merck Patent GesellschaftInventors: Herwig Buchholz, Urs Welz-Biermann, Armin Meijere, Vladimir Chaplinski
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Patent number: 6476075Abstract: 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-bis-benzyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: November 5, 2002Assignee: G.D. Searle & Co.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
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Patent number: 6476268Abstract: N-Benzylamines are prepared by a process in which (i) in a first step, a benzaldehyde is reacted with a primary amine to give the imine and (ii) in a second step, the imine is hydrogenated with hydrogen in the presence of a catalyst containing one or more metals of groups 8 to 10 of the Periodic Table of the Elements to give the N-benzylamine, wherein the iminization (i) is carried out in a water-miscible solvent and the resulting water of reaction is not removed, and the hydrogenation (ii) is carried out in the imine solution obtained in the iminization (i) and containing water of reaction.Type: GrantFiled: March 27, 2002Date of Patent: November 5, 2002Assignee: BASF AktiengesellschaftInventors: Harald Winsel, Wolfgang Siegel, Michael Bartsch
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Patent number: 6476057Abstract: The invention relates to use of 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 cycloalkyl aminoalcohols.Type: GrantFiled: November 14, 2001Date of Patent: November 5, 2002Assignee: G.D. Searle & Co.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
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Patent number: 6465693Abstract: A method is provided for the transition metal-catalyzed arylation, or vinylation, of hydrazines, hydrazones, and the like. Additionally, the invention provides a conceptually novel strategy, the cornerstone of which is the transition metal-catalyzed arylation or vinylation method, for the synthesis of indoles, carbazoles, and the like. The methods and strategies of the invention may be utilized in standard, parallel, and combinatorial synthetic protocols.Type: GrantFiled: January 18, 2001Date of Patent: October 15, 2002Assignee: Massachusetts Institute of TechnologyInventors: Stephen L. Buchwald, Seble Wagaw, O. Geis
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Patent number: 6462092Abstract: The invention relates to use of 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: GrantFiled: November 14, 2001Date of Patent: October 8, 2002Assignee: G.D. Searle & Co.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
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Patent number: 6458849Abstract: The invention relates to use of substituted polycyclic aryl and heteroaryl tertiary-heteroalkyamine 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 mercapto amines.Type: GrantFiled: November 14, 2001Date of Patent: October 1, 2002Assignee: G.D. Searle & Co.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
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Patent number: RE39530Abstract: 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: GrantFiled: September 11, 2003Date of Patent: March 27, 2007Assignee: Gruenenthal GmbHInventors: Bernd Sundermann, Hagen-Heinrich Hennies, Babette-Yvonne Koegel, Helmut Buschmann