Phenylalanines Patents (Class 560/40)
  • Patent number: 9963422
    Abstract: The present invention relates to an improved process for the preparation of Melphalan, more specifically the invention relates to an efficient process for the preparation of substantially pure Melphalan hydrochloride (I).
    Type: Grant
    Filed: March 4, 2014
    Date of Patent: May 8, 2018
    Assignee: Biophore India Pharmaceuticals PVT. Ltd.
    Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Mecheril Valsan Nandakumar, Madhava Reddy Vedururi, Sreenu Samireddi
  • Patent number: 9580440
    Abstract: The present invention provides novel solvated forms of darunavir and processes for their preparation. The present invention also provides novel processes for the preparation of darunavir amorphous form and pharmaceutical compositions comprising it. Thus, for example, darunavir 2-methyl-2-butanol solvate was dissolved in methylene dichloride, distilled under vacuum at 45° C. to obtain a residue, cyclohexane was added to the residue and stirred for 30 hours at 20 to 25° C., and the separated solid was filtered, washed with cyclohexane and dried under vacuum at 50° C. for 12 hours to yield darunavir amorphous form.
    Type: Grant
    Filed: October 7, 2013
    Date of Patent: February 28, 2017
    Assignee: HETERO RESEARCH FOUNDATION
    Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
  • Patent number: 9428444
    Abstract: The present invention provides a novel process for the preparation of highly pure Levothyroxine Sodium, i.e., (S)-2-amino-3-[4-(4-hydroxy-3, 5-diiodophenoxy)-3,5-diiodophenyl] propanoic acid sodium salt via two process intermediates viz 3,5-Diiodo L-Tyrosine copper complex and novel Bis (p-anisyl) iodonium Iodide. The invention also provides levothyroxine pentahydrate free from genotoxic impurities and liothyronine levels below 0.04% wt/wt.
    Type: Grant
    Filed: January 30, 2014
    Date of Patent: August 30, 2016
    Assignee: AZICO BIOPHORE INDIA PRIVATE LIMITED
    Inventors: Ch. A. P. Rameswara Rao, Sreenath Dasari
  • Patent number: 8664426
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: July 25, 2013
    Date of Patent: March 4, 2014
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8575385
    Abstract: This invention provides a process of making optically pure melphalan of the formula by hydroxyethylation, in a regioselective manner, of the aromatic amino group rather than the glycinic amino group.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: November 5, 2013
    Assignee: Navinta LLC
    Inventors: Christopher N. Jobdevairakkam, Hero Velladurai
  • Patent number: 8519175
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 8, 2012
    Date of Patent: August 27, 2013
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8507715
    Abstract: An optically active ?-aminocarbonyl compound is obtained by a Mannich reaction between an aldimine in which: nitrogen is protected and a malonic acid diester, in the presence of optically active BINOL and dialkyl magnesium (in which two alkyl groups are the same or different) in an amount 1 to 2 molar times the amount of the BINOL.
    Type: Grant
    Filed: June 22, 2011
    Date of Patent: August 13, 2013
    Assignee: National University Corporation Nagoya University
    Inventors: Kazuaki Ishihara, Manabu Hatano, Takahiro Horibe
  • Patent number: 8435562
    Abstract: Pharmaceutical compositions and oral dosage forms of (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and methods of treating diseases comprising orally administering such pharmaceutical compositions and dosage forms are disclosed.
    Type: Grant
    Filed: November 8, 2010
    Date of Patent: May 7, 2013
    Assignee: XenoPort, Inc.
    Inventors: Chen Mao, Nikhil Pargaonkar, Laura E. Maurer, Sarina Grace Harris Ma
  • Patent number: 8399513
    Abstract: Crystalline (2R)-2-phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate, hydrate, methods of making the hydrate, pharmaceutical compositions containing the hydrate, and methods of using the hydrate to treat diseases or disorders such as Parkinson's disease are provided.
    Type: Grant
    Filed: October 19, 2009
    Date of Patent: March 19, 2013
    Assignee: XenoPort, Inc.
    Inventors: Sami Karaborni, Manshiu Leung, Chen Mao, Venkat Thalladi
  • Publication number: 20130041045
    Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Application
    Filed: September 5, 2012
    Publication date: February 14, 2013
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Patent number: 8324273
    Abstract: Catechol protected levodopa diester prodrugs pharmaceutical, compositions comprising catechol protected levodopa diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
    Type: Grant
    Filed: October 14, 2010
    Date of Patent: December 4, 2012
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
  • Patent number: 8323627
    Abstract: A compound of the formula (I): where m is an integer equal to 0 or 1, and p is an integer equal to 0, 1, 2 or 3. A method for preparing the compound of the formula (I), and the use thereof as a skin lightening agent. A cosmetic composition and a drug containing the compound of the formula (I).
    Type: Grant
    Filed: September 14, 2009
    Date of Patent: December 4, 2012
    Assignee: Societe d'Exploitation de Produits pour les Industries Chimiques SEPPIC
    Inventors: Sandy Dumont, Cecile Taillebois, Jerome Guilbot, Corinne Stoltz, Sebastien Kerverdo
  • Patent number: 8324272
    Abstract: Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
    Type: Grant
    Filed: March 18, 2010
    Date of Patent: December 4, 2012
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
  • Patent number: 8309754
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 24, 2011
    Date of Patent: November 13, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Patent number: 8268884
    Abstract: The present invention relates to compounds represented by formula (I), or isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof: in which each substituent of formula (I) is as defined in the specification. The present invention also relates to preparation methods of compounds represented by formula (I), a pharmaceutical composition comprising compounds represented by formula (I) and usage of compounds represented by formula (I) for treating chronic neurodegenerative diseases such as Alzheimer's disease and other diseases induced by aggregation or deposition of ?-amyloid peptide.
    Type: Grant
    Filed: February 5, 2007
    Date of Patent: September 18, 2012
    Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. China
    Inventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
  • Publication number: 20120226013
    Abstract: The present invention relates to new classes of monomeric compounds, which may be polymerized to form novel biodegradable and bioresorble polymers and copolymers. These polymers and co-polymers, while not limited thereto, may be adapted for radio-opacity and are useful for medical device applications and controlled release therapeutic formulations.
    Type: Application
    Filed: October 11, 2010
    Publication date: September 6, 2012
    Applicant: Rutgers, The State University of New Jersey
    Inventors: Joachim B. Kohn, Durgadas Bolikal
  • Patent number: 8247603
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically acceptable salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: February 16, 2007
    Date of Patent: August 21, 2012
    Assignee: Birds Pharma GmbH Berolina Innovative
    Inventors: Rudolf-Giesbert Alken, Frank Schneider
  • Publication number: 20120190861
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Application
    Filed: April 5, 2012
    Publication date: July 26, 2012
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Patent number: 8168820
    Abstract: The present invention concerns deuterated catecholamine derivatives as well as pharmaceuticals containing these compounds. In addition, the invention concerns the use of deuterated catecholamine derivatives as well as physiologically compatible salts thereof, and also pharmaceutical compositions, which contain these compounds, also in combination with enzyme inhibitors, for the treatment of dopamine deficiency diseases or diseases which are based on disrupted tyrosine transport or disrupted tyrosine decarboxylase, as well as other disorders.
    Type: Grant
    Filed: December 18, 2003
    Date of Patent: May 1, 2012
    Assignee: BDD Berolina Drug Development GmbH
    Inventor: Rudolf-Giesbert Alken
  • Publication number: 20120094994
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Application
    Filed: December 24, 2011
    Publication date: April 19, 2012
    Applicant: BEZWADA BIOMEDICAL, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20120052110
    Abstract: Provided herein are compositions and methods that inhibit expression of Adam12 gene products, such as ADAM12 mRNA and/or ADAM12 polypeptides, as a therapeutic approach for the treatment of, or promotion of healing of, wounds.
    Type: Application
    Filed: August 4, 2011
    Publication date: March 1, 2012
    Applicant: Hospital for Special Surgery
    Inventors: Marjana TOMIC, Carl Peter Blobel, Asheesh Harsha
  • Patent number: 8093420
    Abstract: The present invention relates to compounds of formula I and II, which are functionalized amino acids, and polymers formed from the same. Polymers formed from the functionalized amino acids are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: October 10, 2006
    Date of Patent: January 10, 2012
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S. Bezwada
  • Publication number: 20110201817
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Application
    Filed: April 27, 2011
    Publication date: August 18, 2011
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning XIANG, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Publication number: 20110190505
    Abstract: This disclosure relates to compounds, reagents, and methods useful in the synthesis of aryl fluorides, for example, in the preparation of 18F labeled radiotracers. For example, this disclosure provides universal “locked” aryl substituents that result in StereoElectronic Control of Unidirectional Reductive Elimination (SECURE) from diaryliodonium salts. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.
    Type: Application
    Filed: February 4, 2011
    Publication date: August 4, 2011
    Inventor: Stephen DiMagno
  • Patent number: 7968597
    Abstract: (2R)-2-Phenylcarbonyloxypropyl (2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.
    Type: Grant
    Filed: December 31, 2008
    Date of Patent: June 28, 2011
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
  • Patent number: 7935843
    Abstract: The present invention relates to dephenolic compounds, an example of which is shown below, which are functionalized, and polymers formed from the same. Polymers formed from the functionalized diphenolics are expected to have controllable degradation profiles, enabling them to release an active component over a desired time range. The polymers are also expected to be useful in a variety of medical applications.
    Type: Grant
    Filed: December 8, 2006
    Date of Patent: May 3, 2011
    Assignee: Bezwada Biomedical, LLC
    Inventor: Rao S Bezwada
  • Publication number: 20100331345
    Abstract: The present invention relates to compounds represented by formula (I), or isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof: in which each substituent of formula (I) is as defined in the specification. The present invention also relates to preparation methods of compounds represented by formula (I), a pharmaceutical composition comprising compounds represented by formula (I) and usage of compounds represented by formula (I) for treating chronic neurodegenerative diseases such as Alzheimer's disease and other diseases induced by aggregation or deposition of ?-amyloid peptide.
    Type: Application
    Filed: February 5, 2007
    Publication date: December 30, 2010
    Inventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
  • Publication number: 20100298242
    Abstract: The invention relates to the use of sweeteners for masking the salty taste of compositions as well as compositions containing salt and defined sweeteners, the amount of sweeteners being suitable for masking the salty taste of the composition.
    Type: Application
    Filed: July 26, 2006
    Publication date: November 25, 2010
    Inventors: Reiner Postges, Richard Ammer, Joerg Breitkreutz, Dorothee Grueneberg Klinkowski
  • Publication number: 20100280108
    Abstract: A compound of general formula (I) wherein, R11, R12, R13, R14, R15, W, Y, R1, R2, R3, R4, R5, and R6 take various meanings for use in the treatment of cancer.
    Type: Application
    Filed: December 19, 2008
    Publication date: November 4, 2010
    Applicant: Pharma Mar, S.A.
    Inventors: Alberto Rodriguez Vicente, Maria Garranzo García-Ibarrola, Carmen Murcia Pérez, Francisco Sánchez Sancho, Maria del Carmen Cuevas Marchante, Cristina Mateo Urbano, Isabel Digón Juárez
  • Publication number: 20100222608
    Abstract: N—[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester is produced by hydrogenation of L-?-aspartyl-L-phenylalanine 1-methyl ester and 3,3-dimethylbutyraldehyde produced in situ by the hydrolysis or cleavage of a 3,3-dimethylbutyraldehyde precursor. The production method is efficient and low cost, as compared with conventional N—[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester synthesis.
    Type: Application
    Filed: May 12, 2010
    Publication date: September 2, 2010
    Applicant: THE NUTRASWEET COMPANY
    Inventors: INDRA PRAKASH, KENNETH E. FURLONG, HANDLEY E. JACKSON, III
  • Publication number: 20100197953
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Application
    Filed: February 2, 2009
    Publication date: August 5, 2010
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Publication number: 20100190725
    Abstract: Compounds of formula (I) or formula (II) have dopaminergic activity: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 is a group —C(?O)—NR3R4, or —S(?O)2—NR3R4; R3 and R4 are independently selected from hydrogen, optionally substituted C1-C6 alkyl, (C1-C5 fluoroalkyl)-CH2—, -Q, and —CH2Q, wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclic ring of (3) to (6) ring atoms; or R3 and R4 together with the nitrogen to which they are attached form an optionally substituted monocyclic cycloalkyl or non-aromatic heterocyclic ring of (3) to (8) ring atoms; R5 is hydrogen, or a natural or non-natural alpha amino acid residue linked via a peptide bond; R6 is hydrogen or a group R7C(?O)—; and R7 is C1-C6 alkyl, C1-C6 fluoroalkyl or cyclopropyl.
    Type: Application
    Filed: July 4, 2008
    Publication date: July 29, 2010
    Applicant: PROXIMAGEN LTD.
    Inventor: Christopher Hobbs
  • Publication number: 20100172916
    Abstract: The present invention relates to new substituted hydroxyphenylamine based modulators of hormone and/or pigment levels, pharmaceutical compositions thereof, and methods of use thereof.
    Type: Application
    Filed: November 9, 2009
    Publication date: July 8, 2010
    Applicant: AUSPEX PHARMACEUTICALS, INC.
    Inventors: Thomas G. Gant, Craig Hodulik, Soon Woo
  • Publication number: 20100173992
    Abstract: Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
    Type: Application
    Filed: March 18, 2010
    Publication date: July 8, 2010
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
  • Patent number: 7709527
    Abstract: Levodopa dimethyl-substituted diester prodrugs pharmaceutical, compositions comprising levodopa dimethyl-substituted diester prodrugs, and methods of using such prodrugs and pharmaceutical compositions for treating diseases such as Parkinson's disease are provided.
    Type: Grant
    Filed: December 20, 2007
    Date of Patent: May 4, 2010
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
  • Patent number: 7659396
    Abstract: The invention relates to an improved method for the production of 3-amidino- or 3-guanidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidino- or 3-guanidinophenylalanine derivatives.
    Type: Grant
    Filed: May 16, 2007
    Date of Patent: February 9, 2010
    Assignee: Wilex AG
    Inventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
  • Publication number: 20090240074
    Abstract: This invention provides a process of making 4-(bis-(2-hydroxyethyl)amino)-L-phenylalanine of the formula by hydroxyethylation, in a regioselective manner, of the aromatic amino group rather than the glycinic amino group.
    Type: Application
    Filed: March 20, 2009
    Publication date: September 24, 2009
    Inventors: Christopher N. Jobdevairakkam, Hero Velladurai
  • Patent number: 7563821
    Abstract: (2R)-2-Phenylcarbonyloxypropyl(2S)-2-amino-3-(3,4-dihydroxyphenyl)propanoate mesylate and crystalline form thereof, methods of making the same, pharmaceutical compositions thereof, and methods of using the same to treat diseases or disorders such as Parkinson's disease are provided.
    Type: Grant
    Filed: December 4, 2006
    Date of Patent: July 21, 2009
    Assignee: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
  • Publication number: 20090170937
    Abstract: Compounds of formula (I) have activity in alleviating the effects of impaired dopaminergic signaling, for example in the treatment of Parkinsons Disease: wherein: R1 is a carboxyl, carboxyl ester, or carboxamide group; R2 and R3 are independently hydrogen, or a group —C(?O)R6 or —C(?O)OR6 wherein Re is C1-C6 alkyl, or a group —CH2Q wherein Q is an optionally substituted monocyclic carbocyclic or heterocyclyl ring of 3 to 6 ring atoms; R4 and R5 are independently (a) the side chain of a natural amino acid, or (b) optionally substituted C1-C4 alkyl, C2-C4 alkenyl, or C2-C4 alkynyl, or (c) —CH2XCH3, —CH2CH2XCH3, or —CH2XCH2CH3, wherein X is —O—, S, or —NR7 wherein R7 is hydrogen, methyl or ethyl; or (d) —CH2Q or CH2OQ wherein Q is as defined in relation to R6; or R4 and R5 taken together with the carbon atom to which they are attached form an optionally substituted cycloalkyl or heterocyclic ring of 3 to 8 ring atoms, optionally fused to a second, optionally substituted, carbocyclic or heterocyclic ring
    Type: Application
    Filed: January 23, 2007
    Publication date: July 2, 2009
    Applicants: Proximagen Ltd., Hodgkin Building,King`s College London,Guy`s Compus
    Inventor: Christopher Hobbs
  • Publication number: 20090137834
    Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.
    Type: Application
    Filed: February 2, 2009
    Publication date: May 28, 2009
    Applicant: XenoPort, Inc.
    Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
  • Publication number: 20090088548
    Abstract: The invention provides biocompatible resorbable polymers, comprising monomer units having formula (I), formula (II), formula (III) or formula (IV). The polymers degrade over time when implanted in the body, and are useful as components of implantable medical devices.
    Type: Application
    Filed: November 3, 2006
    Publication date: April 2, 2009
    Applicant: TyRx Pharma, Inc.
    Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
  • Publication number: 20090036684
    Abstract: The present invention provides a compound useful as a synthetic intermediate for an anti-HIV agent having an integrase inhibitory activity, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate. Specifically, for example, a compound represented by the formula (2?): wherein R is a fluorine atom or a methoxy group, and R400 is a hydrogen atom or a C1-C4 alkyl group, or a salt thereof, and a production method thereof, and a production method of an anti-HIV agent using the synthetic intermediate.
    Type: Application
    Filed: March 6, 2007
    Publication date: February 5, 2009
    Inventors: Koji Matsuda, Koji Ando, Shigeki Ohki, Jun-ichi Hoshi, Takahiro Yamasaki
  • Publication number: 20090030218
    Abstract: The present invention provides an industrial method for preparing aminoalcohol derivatives (I) having a biphenyl group, biphenyloxyacetaldehyde derivatives which are used therefore, preparing methods thereof, and intermediates used for the preparing method. The present invention also provides a preparing method including processes for preparing a 3-substituted biphenylcarboxylic acid derivative represented by the following general formula: by allowing a 3-fluorobiphenylcarboxylic acid derivative prepared from a 3-fluorobiphenylcarbonitrile derivative which can be prepared by allowing a 4-halophenol derivative to react with a 2-fluorobenzonitrile derivative which is substituted by a leaving group at 4-position to react with an organometallic reagent.
    Type: Application
    Filed: May 17, 2006
    Publication date: January 29, 2009
    Applicant: KISSEI PHARMACEUTICAL CO., LTD.
    Inventors: Kiyoshi Kasai, Minoru Kubota, Ritsu Suzuki, Tetsuji Ozawa, Takehiro Ishikawa, Makoto Kobayashi, Junichi Sonehara, Masahiro Kobayashi
  • Publication number: 20090005562
    Abstract: The invention relates to an improved method for the production of 3-amidino- or 3-guanidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidino- or 3-guanidinophenylalanine derivatives.
    Type: Application
    Filed: May 16, 2007
    Publication date: January 1, 2009
    Applicant: WILEX AG
    Inventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
  • Patent number: 7247724
    Abstract: The invention relates to an improved method for the production of 3-amidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidinophenylalanine derivatives.
    Type: Grant
    Filed: July 25, 2003
    Date of Patent: July 24, 2007
    Assignee: Wilex AG
    Inventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
  • Patent number: 7193103
    Abstract: Synthesis of N-[N-(3,3-dimethylbutyl)-L-?-aspartyl]-L-phenylalanine 1-methyl ester by treating N-(3,3-dimethylbutyl)-L-aspartic acid with ketones to give oxazolidinone derivatives, which are condensed with L-phenylalanine methyl ester.
    Type: Grant
    Filed: July 30, 2004
    Date of Patent: March 20, 2007
    Assignee: The Nutrasweet Company
    Inventor: Indra Prakash
  • Patent number: 7183425
    Abstract: This invention describes a reductive amination process whereby perfluorinated ketones or ketals are combined with ?-aminoesters under basic conditions to form metal carboxylates. Diastereoselective reductions of the metal carboxylates enable access to two diastereomers, depending on the reducing conditions.
    Type: Grant
    Filed: July 29, 2005
    Date of Patent: February 27, 2007
    Assignee: Merck Frosst Canada Ltd.
    Inventors: Cheng Yi Chen, Paul N. Devine, Bruce S. Foster, Greg Hughes, Paul O'Shea
  • Patent number: 7141263
    Abstract: A process for conveniently and efficiently producing a highly pure cinnamaldehyde derivative, for example, (2E)-(3-hydroxy-4-methoxy)cinnamaldehyde, which comprises reacting a benzaldehyde derivative, such as isovanillin and the like, with acetaldehyde in the presence of an alkali, in particular preferably, dropping acetaldehyde little by little thereto in an aqueous solution at a low temperature for the reaction thereof. The cinnamaldehyde derivative thus obtained is selectively reduced to produce 3-(3-hydroxy-4-substituted (with methoxy group or the like)phenyl)propionaldehyde. Further, through a reductive alkylation reaction of the compound thus produced with an aspartame, N-[N-[3-(3-hydroxy-4-substituted (with methoxy group or the like)phenyl)propyl]-L-aspartyl]-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high sweetening potency, can be industrially and efficiently produced. The processes therefor are also provided.
    Type: Grant
    Filed: June 17, 2005
    Date of Patent: November 28, 2006
    Assignee: Ajinomoto Co., Inc.
    Inventors: Kenichi Mori, Shinji Fujita, Nao Funakoshi, Tadashi Takemoto
  • Patent number: 7115296
    Abstract: The present invention relates to a novel N-alkylaspartyl amide derivative, a salt form thereof, a sweetening agent containing the same and a sweetened food or drink containing the N-alkylaspartyl amide derivative as an effective ingredient.
    Type: Grant
    Filed: August 8, 2003
    Date of Patent: October 3, 2006
    Assignee: Ajinomoto Co., Inc.
    Inventors: Yusuke Amino, Kazuko Yuzawa
  • Patent number: 7057038
    Abstract: One aspect of the present invention relates to a method for the kinetic resolution of racemic and diastereomeric mixtures of chiral compounds. The critical elements of the method are: a non-racemic chiral tertiary-amine-containing catalyst; a racemic or diastereomeric mixture of a chiral substrate, e.g., a cyclic carbonate or cyclic carbamate; and a nucleophile, e.g., an alcohol, amine or thiol. A preferred embodiment of the present invention relates to a method for achieving the kinetic resolution of racemic and diastereomeric mixtures of derivatives of ?- and ?-amino, hydroxy, and thio carboxylic acids. In certain embodiments, the methods of the present invention achieve dynamic kinetic resolution of a racemic or diastereomeric mixture of a substrate, i.e.
    Type: Grant
    Filed: May 26, 2004
    Date of Patent: June 6, 2006
    Assignee: Brandeis University
    Inventors: Li Deng, Jianfeng Hang, Liang Tang