Nitro Bonded To Carbon In Acid Moiety Patents (Class 560/20)
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Patent number: 9403757Abstract: The present invention relates to a process for the preparation of iodinated X-ray contrast agents and in particular to key intermediates thereof. It particularly relates to an improved process for preparation of 5-acetamido-N,N?-bis(2,3-dihydroxypropyl)-2,4,6-triiodoisophthalamide (Compound A) or N,N?-bis(2,3-dihydroxypropyl)-5-formamido-2,4,6-triiodoisophthalamide (Compound C), which are intermediates in the industrial preparation of non-ionic X-ray contrast agents. More particularly the invention provides a process for deacylation of the acylated hydroxyl groups of an intermediate compound of Compound A and Compound C.Type: GrantFiled: October 24, 2013Date of Patent: August 2, 2016Assignee: GE Healthcare ASInventor: Torfinn Haaland
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Publication number: 20150148550Abstract: Disclosed is a novel compound to function as a calcium-dependent chloride channel blocking agent.Type: ApplicationFiled: November 27, 2013Publication date: May 28, 2015Applicant: Korea Institute of Science and TechnologyInventors: Eun Joo ROH, Changjoon Justin LEE, Soo Jin OH, Jong Hoon JUNG
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Publication number: 20150119583Abstract: A catalyst for an organic reaction and a method of using a catalyst in an organic reaction are provided. The catalyst for an addition or condensation reaction includes a graphene oxide including an oxygen functional group, and the catalyst is configured to promote the addition or condensation reaction by bonding the oxygen functional group with an alkali metal ion or alkali earth metal ion during the addition or condensation reaction.Type: ApplicationFiled: May 8, 2014Publication date: April 30, 2015Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITYInventors: Hyoyoung LEE, Youngmin KIM, Surajit SOME
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Publication number: 20150112066Abstract: The present invention relates to asymmetric catalysts, including redox-reconfigurable asymmetric catalysts. Methods of producing compounds having one or more stereocenters using the asymmetric catalysts of the present invention are also disclosed.Type: ApplicationFiled: June 11, 2013Publication date: April 23, 2015Applicant: NEW YORK UNIVERSITYInventors: James Canary, Shahab Mortezaei
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Patent number: 9006477Abstract: A method for producing a nitrobenzene compound represented by general formula (2), wherein R1 and R5 are the same or different, and each is a halogen atom or another functional group, and R2, R3, and R4 are the same or different, and each is a hydrogen atom or another functional group, comprises oxidizing an aniline compound represented by general formula (1), wherein R1, R2, R3, R4, and R5 are the same as described above, with hydrogen peroxide in the presence of a tungsten compound under an acidic condition, followed by oxidation with hydrogen peroxide under a neutral to alkaline condition.Type: GrantFiled: July 4, 2012Date of Patent: April 14, 2015Assignee: Ihara Chemical Industry Co., Ltd.Inventors: Shinki Tani, Nami Yadomatsu, Akiko Ikumi, Yuuki Hirano, Takuya Ido
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Patent number: 8970937Abstract: Disclosed herein are novel electrochromic materials. The electrochromic materials produce various colors. The electrochromic materials can be used to form red electrochromic layers in a simple manner. Therefore, the electrochromic materials are suitable for use in the fabrication of RGB full-color electrochromic devices. Also disclosed herein are electrochromic devices fabricated using the electrochromic materials.Type: GrantFiled: October 29, 2008Date of Patent: March 3, 2015Assignee: Samsung Electronics Co., Ltd.Inventors: Seung Uk Son, Chang Ho Noh, Ji Min Lee
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Patent number: 8871964Abstract: The invention relates to a method for carrying out a chemical reaction for producing a target compound by heating in a reactor a reaction medium containing at least one first reactant, such that a chemical bond inside the first reactant or between the first and a second reactant is formed or modified. The reaction medium is brought into contact with a solid heating medium that can be warmed by electromagnetic induction and that is inside the reactor and is surrounded by the reaction medium. Said heating medium is heated by electromagnetic induction with the aid of an inductor and the target bond is formed from the first reactant or from the first and a second reactant and said target bond is separated from the heating medium.Type: GrantFiled: April 16, 2012Date of Patent: October 28, 2014Assignee: Henkel AG & Co. KGaAInventors: Carsten Friese, Andreas Kirschning, Jürgen Wichelhaus, Sascha Volkan Ceylan
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Publication number: 20140275603Abstract: A process for making a 2-nitro-1-ethanol derivative of formula III: wherein R3 is as described herein is provided. Novel 2-nitro-1-ethanol derivatives provided.Type: ApplicationFiled: March 26, 2012Publication date: September 18, 2014Applicant: ANGUS Chemical CompanyInventors: Raymond J. Swedo, George David Green, Charles E. Coburn
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Publication number: 20140213552Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: ApplicationFiled: March 20, 2014Publication date: July 31, 2014Applicant: Endo Pharmaceuticals Inc.Inventors: Scott Kevin Thompson, Roger Astbury Smith, Sandeep Gupta, Tony Priestley, Nicholas James Laping, Ashis K. Saha, Sonali Rudra
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Publication number: 20140155632Abstract: The invention relates to a process for preparing aryl- and heteroarylacetic acids and derivatives thereof by reaction of aryl or heteroaryl halides with malonic diesters in the presence of a palladium catalyst, of one or more bases and optionally of a phase transfer catalyst. This process enables the preparation of a multitude of functionalized aryl- and heteroarylacetic acids and derivatives thereof, especially also the preparation of arylacetic acids with sterically demanding substituents.Type: ApplicationFiled: February 27, 2012Publication date: June 5, 2014Inventors: Thomas Himmler, Lukas J. Goossen, Felix Rudolphi, Bingrui Song
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Publication number: 20130289278Abstract: Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphosphoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput.Type: ApplicationFiled: March 15, 2013Publication date: October 31, 2013Applicant: MANNKIND CORPInventors: Kelly Sullivan Kraft, John J. Freeman, Paul Serwinski, Vinnie Pavia, Otto Phanstiel, IV, Navneet Kaur
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Patent number: 8486998Abstract: The present invention, in one or more embodiments, comprises water-soluble derivatives of 3-n-pentadecylcatechol (poison ivy urushiol saturated congener) and/or 3-n-heptadecylcatechol (poison oak urushiol saturated congener) as compositions for the prevention and/or prophylactic treatment of contact dermatitis caused by poison ivy and poison oak. The present invention is also directed towards processes for making such compounds. Disclosed are compounds which are effective for tolerizing and desensitizing a subject against allergens contained in plants of the Anacardiaceae and Ginkgoaceae families comprising water soluble urushiol esters of general formula (I) Tolerizing and desensitizing mammals, including humans, to allergens contained in plants of the Anacardiaceae and Ginkgoaceae families is attained by administering a composition containing at least one water soluble urushiol ester compound.Type: GrantFiled: April 3, 2009Date of Patent: July 16, 2013Assignee: The University of MississippiInventors: Mahmoud A. Elsohly, Waseem Gul, Mohammad Khalid Ashfaq, Susan P. Manly
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Publication number: 20130101667Abstract: The present application provides novel compounds and methods for preparing and using these compounds. These compounds are useful in treating pain, itch, overactive bladder and/or interstitial cystitis in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) and a TRPV1 receptor activator. In one embodiment, the TRPV1 receptor activator is lidocaine.Type: ApplicationFiled: October 24, 2012Publication date: April 25, 2013Applicant: ENDO PHARMACEUTICALS, INC.Inventor: Endo Pharmaceuticals, Inc.
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Patent number: 8314214Abstract: Methods are disclosed for preparing compounds of Formula I: where R1, R3, and R4 are independently hydrogen or C1 to C4 alkyl, and R2 is: where R5 is selected from the group consisting of hydrogen and C1 to C4 alkyl, or where R6, R7 and R8 are independently hydrogen or C1 to C4 alkyl; or the esters or pharmacologically acceptable salts thereof. The methods can involve converting a suitably functionalized aniline compound to a diazonium salt (which aniline compound can be first formed by reduction of a nitrobenzene) and coupling the diazonium salt with a suitably functionalized benzene compound. The suitably functionalized aniline compound either includes a primary alcohol or aldehyde group, which is then oxidized to a carboxylic acid group, or includes a nitrile or amide group, which is hydrolyzed to a carboxylic acid group. The methods can also involve the direct coupling (via reduction of nitro groups to form an azo linkage) of suitably functionalized nitrobenzenes.Type: GrantFiled: April 26, 2011Date of Patent: November 20, 2012Assignee: Biocon LimitedInventors: Jennifer A. Riggs-Sauthier, Nnochiri N. Ekwuribe
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Patent number: 8274213Abstract: Disclosed herein are novel electrochromic materials. The electrochromic materials produce various colors and have bistability to achieve red-green-blue full colors. Therefore, the electrochromic materials can be used in a variety of electrochromic devices. Also disclosed herein are electrochromic devices fabricated using the electrochromic materials.Type: GrantFiled: April 13, 2009Date of Patent: September 25, 2012Assignee: Samsung Electronics Co., Ltd.Inventors: Seung Uk Son, Ji Min Lee, Chang Ho Noh
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Patent number: 8258162Abstract: The present invention provides compounds represented by general formula (I): or pharmaceutical acceptable salts thereof, wherein R1 and R2 are each hydrogen, lower acyl, lower alkoxycarbonyl or the like; R3 is lower alkyl, halo-lower alkyl, cycloalkyl, heterocycloalkyl, optionally substituted aryl, optionally substituted heteroaryl or the like; R4 is cyano, lower alkoxycarbonyl, carboxy or the like, which exhibit potent COMT inhibitory activities. The present invention also provides pharmaceutical compositions containing said compound, and uses thereof.Type: GrantFiled: June 26, 2009Date of Patent: September 4, 2012Assignee: Kissei Pharmaceutical Co., Ltd.Inventors: Takehiro Ishikawa, Satoko Kobayashi, Hitoshi Inoue, Yasunori Ueno, Masako Yoshida, Nobuyuki Tanaka
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Patent number: 8222200Abstract: Tertiary non-vinylic carbamates of molecular weight less than 350 are useful as fragrance ingredients. A method of preparation is also described.Type: GrantFiled: April 14, 2004Date of Patent: July 17, 2012Assignee: Givaudan SAInventors: Felix Flachsmann, Jean-Pierre Bachmann
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Publication number: 20120029211Abstract: A catalytic Wittig method utilizing a phosphine including the steps of providing a phosphine oxide precatalyst and reducing the phosphine oxide precatalyst to produce the phosphine; forming a phosphonium ylide precursor from the phosphine and a reactant; generating a phosphonium ylide from the phosphonium ylide precursor; reacting the phosphonium ylide precursor with the aldehyde, ketone, or ester to form the olefin and the phosphine oxide which then reenters the cycle. The invention is also directed to a Mitsunobu reaction catalytic in phosphine.Type: ApplicationFiled: April 6, 2010Publication date: February 2, 2012Inventor: Christopher J. O'Brien
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Publication number: 20110269834Abstract: Described herein are compounds and compositions, and methods for using the compounds and compositions, for treating respiratory diseases and illness, such as severe acute respiratory syndrome (SARS).Type: ApplicationFiled: August 21, 2009Publication date: November 3, 2011Applicants: THE BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS, PURDUE RESEARCH FOUNDATIONInventors: Arun K. Ghosh, Jun Takayama, Andrew David Mesecar, Michael E. Johnson, Kiira M. Ratia, Rima Chaudhuri, Debbie C. Mulhearn
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Publication number: 20110245223Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.Type: ApplicationFiled: December 1, 2010Publication date: October 6, 2011Applicant: Japan Tobacco Inc.Inventors: Hiroshi Yamamoto, Yasuhiro Ohe, Hiroyuki Goto, Kazuhito Harada, Shinji Yata, Takashi Ito, Jun Nishiu, Makoto Kakutani, Shunsuke Fujii, Kota Asahina
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Publication number: 20110236400Abstract: Disclosed are novel gamma secretase inhibitors of the formula. Also disclosed are methods of inhibiting gamma-secretase, methods of treating neurodegenerative diseases, and methods of treating Alzheimer's Disease. Also disclosed are processes for preparing alkenes in one reaction step using a mixture of an aldehyde (or ketone) and an alkyl substituted with two electron withdrawing groups, and reacting the mixture with: (a) a sulfonyl halide (e.g., a sulfonyl chloride) and a basic tertiary amine, or, (b) a sulfonyl anhydride and a basic amine, or (c) an aryl-C(O)-halide and a basic tertiary amine, or (d) an aryl-C(O)—O—C(O)-aryl and a basic tertiary amine, or (e) an heteroaryl-C(O)-halide and a basic tertiary amine, or (f) a heteroaryl-C(O)—O—C(O)-heteroaryl and a basic tertiary amine.Type: ApplicationFiled: July 1, 2008Publication date: September 29, 2011Inventors: Wen-Lian Wu, Thomas A. Bara, Duane A. Burnett, John W. Clader, Martin S. Domalski, Yan Jin, Hubert B. Josien, Hongmei Li, Xian Liang, Dmitri A. Pissarnitski, Thavalakulamgara K. Sasikumar, Jesse K. Wong, Ruo Xu, Zhiqiang Zhao, Paul E. McNamara
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Patent number: 8022157Abstract: Disclosed herein is a surface functionalized poly(dimethylsiloxane) (PDMS) and methods for making the same. The surface functionalized poly(dimethylsiloxane) (PDMS) disclosed herein is applicable in the general field of microfluidics, bioMEMS (bio-microelectromechanical systems), soft lithography and other related biotechnology fields.Type: GrantFiled: August 29, 2008Date of Patent: September 20, 2011Assignee: Peking UniversityInventor: Hongwei Ma
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Patent number: 7968721Abstract: This invention relates to a process for preparing a selective androgen receptor modulator (SARM) compound represented by the structure of formula I: wherein X is O; and T, Z, Y, Q, R and R1 are defined herein. The process includes coupling between an amide of formula II and a phenol of formula III followed by a purification step consisting of precipitating the compound of formula (I) in a mixture of alcohol and water alone.Type: GrantFiled: January 12, 2004Date of Patent: June 28, 2011Assignee: University of Tennessee Research FoundationInventors: Duane D. Miller, Karen A. Veverka, Kiwon Chung
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Publication number: 20110136827Abstract: The invention provides certain bis-acylated hydroxylamine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the invention provides methods of using such compounds or pharmaceutical compositions for treating, preventing, or delaying the onset and/or develop of a disease or condition. In some embodiments, the disease or condition is selected from cardiovascular diseases, ischemia, reperfusion injury, cancerous disease, pulmonary hypertension and conditions responsive to nitroxyl therapy.Type: ApplicationFiled: December 7, 2010Publication date: June 9, 2011Inventors: John P. Toscano, Art Sutton, Vincent J. Kalish, Frederick Arthur Brookfield, Stephen Martin Courtney, Lisa Marie Frost
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Publication number: 20110092683Abstract: There are provided compounds of formulas (VA), (VIA), (VIIA) (IXA), (XIA), (XIIA), (XIIIA), and (XIVA): wherein A, Z, R2, X?, and L2 represent various different possibilities. Methods for using such compounds are also provided.Type: ApplicationFiled: December 21, 2010Publication date: April 21, 2011Applicant: VALORISATION-RECHERCHE, LIMITED PARTNERSHIPInventors: André Charette, Jean-Christophe Poupon, Alessandro Boezio
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Publication number: 20110021730Abstract: Disclosed herein is a surface functionalized poly(dimethylsiloxane) (PDMS) and methods for making the same. The surface functionalized poly(dimethylsiloxane) (PDMS) disclosed herein is applicable in the general field of microfluidics, bioMEMS (bio-microelectromechanical systems), soft lithography and other related biotechnology fields.Type: ApplicationFiled: August 29, 2008Publication date: January 27, 2011Inventor: Hongwei Ma
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Publication number: 20100331218Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.Type: ApplicationFiled: September 14, 2010Publication date: December 30, 2010Applicant: Affymetrix, INC.Inventors: Glenn H. McGall, Andrea Cupoletti
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Publication number: 20100004428Abstract: The invention provides methods for preparing polymers bearing a terminal propionic acid. The method involves first reacting a water soluble and non-peptidic polymer comprising at least one hydroxyl group with a tertiary alkyl acrylate in the presence of a catalyst to form a propionic acid ester of the polymer, wherein the polymer has a weight average molecular weight of at least about 10,000 Da; and then treating the propionic acid ester of the polymer with a strong acid to form a propionic acid of the polymer.Type: ApplicationFiled: September 15, 2009Publication date: January 7, 2010Applicant: Nektar TherapeuticsInventors: Antoni Kozlowski, Samuel P. McManus
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Patent number: 7625988Abstract: The present invention is directed to novel flame retardant monomers and polymers, wherein the flame retardant properties of the polymers are provided by functionality in pendant groups attached to a polymer backbone (as opposed to the polymer backbone itself possessing flame retardant properties. The present invention is also directed to methods of making such polymers and monomers, and articles of manufacture incorporating such monomers and polymers.Type: GrantFiled: June 18, 2004Date of Patent: December 1, 2009Assignee: William Marsh Rice UniversityInventors: James M. Tour, Joshua L. Jurs, Jason J. Stephenson
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Publication number: 20090251046Abstract: Disclosed herein are novel electrochromic materials. The electrochromic materials produce various colors. The electrochromic materials can be used to form red electrochromic layers in a simple manner. Therefore, the electrochromic materials are suitable for use in the fabrication of RGB full-color electrochromic devices. Also disclosed herein are electrochromic devices fabricated using the electrochromic materials.Type: ApplicationFiled: October 29, 2008Publication date: October 8, 2009Applicant: SAMSUNG ELECTRONICS CO., LTD.Inventors: Seung Uk Son, Chang Ho Noh, Ji Min Lee
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Publication number: 20090062149Abstract: Compounds represented by the following structural formulas can be used as photoacid generators: Such compounds are useful, for example, in fabricating arrays of polymers.Type: ApplicationFiled: November 3, 2008Publication date: March 5, 2009Applicant: Affymetrix, INC.Inventors: Glenn H. McGall, Andrea Cuppoletti
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Patent number: 7432388Abstract: Compounds of the formula where the variables have the values described in the specification are antagonists of RAR?retinoid receptors.Type: GrantFiled: June 4, 2007Date of Patent: October 7, 2008Assignee: Allergan, Inc.Inventors: Kwok Yin Tsang, Santosh Sinha, Xiaoxia Liu, Smita Bhat, Roshantha A. Chandraratna
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Publication number: 20080221322Abstract: The present invention relates to chemical processes for the manufacture of certain quinazoline derivatives, or pharmaceutically acceptable salts thereof. The invention also relates to processes for the manufacture of certain intermediates useful in the manufacture of the quinazoline derivatives and to processes for the manufacture of the quinazoline derivatives utilising said intermediates. In particular, the present invention relates to chemical processes and intermediates useful in the manufacture of the compound 4-(4-fluoro-2-methylindol-5-yloxy)-6-methoxy-7-(3-pyrrolidin-1-ylpropoxy)quinazoline.Type: ApplicationFiled: October 31, 2007Publication date: September 11, 2008Applicant: AstraZeneca ABInventors: Euan Alexander Arnott, John Crosby, Mathew Charles Evans, James Gair Ford, Martin Francis Jones, Kevin William Leslie, Ian Michael McFarlane, George Joseph Sependa
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Patent number: 7414040Abstract: Invented are non-peptide TPO mimetics. Also invented are novel processes and intermediates used in the preparation of the presently invented compounds. Also invented is a method of treating thrombocytopenia, in a mammal, including a human, in need thereof which comprises administering to such mammal an effective amount of a selected hydroxy-1-azobenzene derivative.Type: GrantFiled: June 6, 2003Date of Patent: August 19, 2008Assignee: SmithKline Beecham CorporationInventor: Dirk A. Heerding
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Publication number: 20080194859Abstract: The invention is directed to novel compounds that are used in the formation of polyurea compositions, including one-part and two-part polyurea compositions. The invention is also directed to polyureas formed from such compounds, cross-linked polyureas, and UV-stabilized polyureas.Type: ApplicationFiled: May 16, 2005Publication date: August 14, 2008Inventors: Kenneth I. Sawyer, Robert J. Kupper
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Patent number: 7351849Abstract: The present invention is to provide a method for producing the desired optically active ?-amino acid derivatives of high optical purities in high yields, without requiring a step of deprotection. More particularly, the present invention relates to a method for producing an optically active ?-amino acid derivative or a salt thereof represented by the formula (2): which comprises reacting an ?,?-unsaturated carboxylic acid derivative or a salt thereof represented by the formula (1): with an amines or a salt thereof in the presence of a chiral catalyst and in the presence or absence of an acid.Type: GrantFiled: August 18, 2004Date of Patent: April 1, 2008Assignee: Takasago International CorporationInventors: Mikiko Sodeoka, Yoshitaka Hamashima
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Patent number: 7314888Abstract: A compound or a salt thereof having the atom corresponding to N3 and the two or more atoms selected from N1, N2, N4 and N5, said atoms constitute the pharmacophore represented by the following formula: and inhibits the activity of transcription factor AP-1 and is useful as an agent for preventing and treating the diseases into which over expression of AP-1 participates and as an AP-1 inhibitor.Type: GrantFiled: November 5, 1999Date of Patent: January 1, 2008Assignee: Toyama Chemical Co., Ltd.Inventors: Hisaaki Chaki, Tadakazu Takakura, Keiichi Tsuchida, Hironori Kotsubo, Yukihiko Aikawa, Shuichi Hirono, Shunichi Shiozawa
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Patent number: 7282605Abstract: The present invention provides a process for producing an optically active 2-allylcarboxylic acid derivative, which is useful as a pharmaceutical intermediate, from readily available and inexpensive starting materials by the process which can be practiced on a commercial scale in a simple and easy manner, and certain 2-allylcarboxamide derivatives, which are novel and important intermediates in that process. An N-allylcarboxamide derivative undergoes rearrangement reaction diastereoselectively in the presence of a base to give a 2-allylcarboxamide derivative, the resulting derivative is subjected to a carbamation reaction and solvolysis to give an optically active 2-allylcarboxylic acid ester, and then the ester obtained is stereoselectively hydrolyzed using an enzyme to produce 2-allylcarboxylic acid having a high optical purity. In addition, the present invention provides a 2-allylcarboxamide derivative compound which is a novel intermediate in the process of the present invention.Type: GrantFiled: April 16, 2004Date of Patent: October 16, 2007Assignees: Kaneka Corporation, Ono Pharmaceutical Co., Ltd.Inventors: Kazumi Okuro, Susumu Amano, Noriyuki Kizaki, Teruaki Takesue, Masaru Mitsuda, Noriyuki Ito, Yoshihiko Yasohara
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Patent number: 7244864Abstract: The invention relates to a process for the preparation of a compound of formula (I), wherein R represents a 2,3-dihydroxy-1-propyl or a 1,3-dihydroxy-2-propyl radical, via direct amidation of a dialkyl ester of 5-amino-1,3-benzenedicarboxylic acid of formula (V), wherein R1 represents a straight or branched (C1-C4)-alkyl group, with at least the stoichiometric amount of an amine of formula H2NR.Type: GrantFiled: November 28, 2001Date of Patent: July 17, 2007Assignee: Bracco Imaging S.p.A.Inventors: Pier Lucio Anelli, Marino Brocchetta, Giovanna Lux, Enrico Cappelletti
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Patent number: 7138538Abstract: Process for the separation of enantiomers comprising at least one free functional group, in which process a reagent based on an enantiopure amino acid is reacted in basic medium with a mixture comprising enantiomers.Type: GrantFiled: May 7, 2004Date of Patent: November 21, 2006Assignee: Solvay (Societe Anonyme)Inventors: Thierry Delplanche, Roland Callens
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Patent number: 7094919Abstract: Methods for preparing substituted aromatic carboxylic acid esters are described. In particular, the invention relates a method for preparing a nitro-substituted aromatic carboxylic acid ester: Additionally the invention relates to a method for preparing a thioether-substituted aromatic carboxylic acid ester: Such aryl esters are useful in the preparation of various agrochemicals and agrochemical intermediates.Type: GrantFiled: December 6, 2001Date of Patent: August 22, 2006Assignee: Eastman Chemical CompanyInventors: Neil W. Boaz, M. Todd Coleman, Timothy R. Hightower
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Patent number: 7037938Abstract: The present invention relates to a compound formula [I]: wherein Y is bond, —O—(CH2)n— (in which n is 1, 2, 3 or 4), etc., Z is cyano, tetrazolyl, etc., R1 is hydrogen, lower alkyl, etc., R2 is hydrogen or an amino protective group, R3 is hydrogen or lower alkyl, R4 is hydrogen or lower alkyl, R5 and R8 are each independently hydrogen, halogen, hydroxy, lower alkyl, etc., R6 is hydrogen, lower alkyl, etc., R9 is hydrogen or lower alkyl, and i is 1 or 2, or a salt thereof. The compound [I] of the present invention and pharmaceutically acceptable salts thereof are useful for the prophylactic and/or the therapeutic treatment of pollakiurea or urinary incontinence.Type: GrantFiled: June 26, 2003Date of Patent: May 2, 2006Assignee: Astellas Pharma Inc.Inventors: Kouji Hattori, Yasuyo Tomishima, Masashi Imanishi
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Patent number: 7012151Abstract: The present invention relates to a process for the highly regioselective aromatic nitration of alkyl 4-alkanoylamino-3-alkyl-benzoates in the 5-position in a mixture containing nitric acid and the use of the resulting products for preparing, in particular, pharmaceutically active benzimidazole derivatives.Type: GrantFiled: April 12, 2000Date of Patent: March 14, 2006Assignee: Boehringer Ingelheim Pharma KGInventors: Margarete Schneider, Heinrich Schneider
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Patent number: 6949585Abstract: The present invention provides a compound which has cytokine production inhibitory activity and is useful for the treatment of diseases which is associated with cytokine. The compound is represented by the following general formula (I) [wherein A represents a cyclic group which may be substituted; the partial structure -DE- represents a group represented by —CH2CH2— or —CH?CH—; W represents a group represented by —CH2—, —CH2CH2—, —CH?CH— or —CH?; the partial structure >XY— represents a group represented by >CH—(CH2)n—, >C?CH—, >CH—CH2—CH(OH)—, >CH—CH2—C(?O)—, >CH—O— or >CH—O—CO—, provided that when W is —CH?, then XY— represents C—(CH2)p—; Z represents a divalent aliphatic hydrocarbon group; R1 and R2, which may be the same or different, each represents a hydrogen atom, or a hydroxyl, alkoxy or alkoxyalkoxy group; m is an integer of 0 or 1].Type: GrantFiled: April 1, 2002Date of Patent: September 27, 2005Assignee: Eisai Co., Ltd.Inventors: Yoshihito Eguchi, Ken-ichi Chiba, Masaki Goto, Hiroshi Obaishi, Yoshikazu Kuboi
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Patent number: 6855842Abstract: The invention concerns novel nitroaromatic compounds of general formula (I?) wherein: R, R?1, R2, Z and n are as defined in claim 1. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further concerns the use of said compounds for preparing heterocyclic benzofuran or benzothiophene derivatives nitrated in position 5. The invention concerns particularly the preparation of 2-alkyl-5-nitrobezofuran.Type: GrantFiled: October 23, 2000Date of Patent: February 15, 2005Assignee: Rhodia ChimieInventors: Thierry Schlama, Armand Mettling, Philippe Karrer
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Publication number: 20040204604Abstract: An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.Type: ApplicationFiled: April 8, 2004Publication date: October 14, 2004Inventors: Daqing Che, Bhaskar Reddy Guntoori, K. S. Keshava Murthy
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Publication number: 20040204370Abstract: Certain N-deacetylcolchicine and N-deacetylthiocolchine derivatives are described wherein the 7-N position on the B ring is substituted with the group —C(O)—(CHR4)m-AR, wherein m is an integer of 0-10, A is S, O, N or a covalent bond; R1 is substituted phenyl or substituted benzoyl; optionally substituted cycloalkyl of 3-7 carbons; optionally substituted naphtyl; an optionally substituted imide ring; an optionally substituted 5 or 6 member heterocycle with at least one N, S, or O in the ring; or an optionally substituted fused heterocyclic or fused carboxyclic ring system; R2 (at the 2-position of the A ring) is methoxy, hydroxy, or methylenedioxy when taken together with R3; R3 (at the 3-position of the A ring) is methoxy, hydroxy, a monosaccharide radical, or is methylenedioxy when taken together with R2; and R4 is H or is H or methyl when m is 1. Also dimers of such compounds are disclosed.Type: ApplicationFiled: April 14, 2003Publication date: October 14, 2004Inventor: Li-Xi Yang
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Publication number: 20040171865Abstract: The present invention relates to a method of preparing a phenoxy alkanoic, alkenoic, or alkynoic acid or a salt thereof from a phenoxy containing compound via a dicarboxylate intermediate. The phenoxy alkanoic, alkenoic, and alkynoic acids and salts thereof prepared by this method are suitable for use in composition for delivering active agents via oral or other routes of administration to animals. Furthermore, the present invention relates to phenoxy dicarboxylic acids and their salts for delivering active agents, such as biologically or chemically active agents, to a target.Type: ApplicationFiled: April 7, 2004Publication date: September 2, 2004Inventor: Joseph N. Bernadino
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Publication number: 20040127737Abstract: Carboxylic acid benzyl esters can be prepared by reacting dibenzyl ethers with carboxylic anhydrides in the presence of acid, optionally applied to a support, as catalyst.Type: ApplicationFiled: September 17, 2003Publication date: July 1, 2004Inventors: Pieter Ooms, Bernd-Ulrich Schenke
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Patent number: 6753347Abstract: This invention provides a process for the preparation of a benzimidazole derivative (I) or a pharmaceutically acceptable salt thereof, wherein R1 is C1-C6 alkyl, C1-C6 alkoxyl, etc., R2 is C1-C6 alkyl, and R3 is hydrogen or a protecting group, which exhibits excellent hyopoglycemic action, said process comprising condensation of an amine derivative (III) with a carboxylic acid derivatives (II) to afford a compound (IV), followed by cyclization of compound (IV) in the presence of an acid.Type: GrantFiled: October 16, 2002Date of Patent: June 22, 2004Assignee: Sankyo Company, LimitedInventors: Naoyuki Kishi, Yoshitaka Nakamura, Narumi Abe, Toyonori Takebayashi