Phenylalanines Patents (Class 560/40)
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Patent number: 9963422Abstract: 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: GrantFiled: March 4, 2014Date of Patent: May 8, 2018Assignee: Biophore India Pharmaceuticals PVT. Ltd.Inventors: Manik Reddy Pullagurla, Jagadeesh Babu Rangisetty, Mecheril Valsan Nandakumar, Madhava Reddy Vedururi, Sreenu Samireddi
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Patent number: 9580440Abstract: 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: GrantFiled: October 7, 2013Date of Patent: February 28, 2017Assignee: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Rapolu Raji Reddy, Kesireddy Subash Chander Reddy, Bandi Vamsi Krishna
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Patent number: 9428444Abstract: 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: GrantFiled: January 30, 2014Date of Patent: August 30, 2016Assignee: AZICO BIOPHORE INDIA PRIVATE LIMITEDInventors: Ch. A. P. Rameswara Rao, Sreenath Dasari
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Patent number: 8664426Abstract: 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: GrantFiled: July 25, 2013Date of Patent: March 4, 2014Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Patent number: 8575385Abstract: 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: GrantFiled: March 20, 2009Date of Patent: November 5, 2013Assignee: Navinta LLCInventors: Christopher N. Jobdevairakkam, Hero Velladurai
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Patent number: 8519175Abstract: 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: GrantFiled: October 8, 2012Date of Patent: August 27, 2013Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Patent number: 8507715Abstract: 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: GrantFiled: June 22, 2011Date of Patent: August 13, 2013Assignee: National University Corporation Nagoya UniversityInventors: Kazuaki Ishihara, Manabu Hatano, Takahiro Horibe
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Patent number: 8435562Abstract: 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: GrantFiled: November 8, 2010Date of Patent: May 7, 2013Assignee: XenoPort, Inc.Inventors: Chen Mao, Nikhil Pargaonkar, Laura E. Maurer, Sarina Grace Harris Ma
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Patent number: 8399513Abstract: 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: GrantFiled: October 19, 2009Date of Patent: March 19, 2013Assignee: XenoPort, Inc.Inventors: Sami Karaborni, Manshiu Leung, Chen Mao, Venkat Thalladi
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Publication number: 20130041045Abstract: 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: ApplicationFiled: September 5, 2012Publication date: February 14, 2013Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Patent number: 8324272Abstract: 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: GrantFiled: March 18, 2010Date of Patent: December 4, 2012Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Patent number: 8324273Abstract: 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: GrantFiled: October 14, 2010Date of Patent: December 4, 2012Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Patent number: 8323627Abstract: 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: GrantFiled: September 14, 2009Date of Patent: December 4, 2012Assignee: Societe d'Exploitation de Produits pour les Industries Chimiques SEPPICInventors: Sandy Dumont, Cecile Taillebois, Jerome Guilbot, Corinne Stoltz, Sebastien Kerverdo
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Patent number: 8309754Abstract: 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: GrantFiled: December 24, 2011Date of Patent: November 13, 2012Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Patent number: 8268884Abstract: 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: GrantFiled: February 5, 2007Date of Patent: September 18, 2012Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.A. ChinaInventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
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Publication number: 20120226013Abstract: 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: ApplicationFiled: October 11, 2010Publication date: September 6, 2012Applicant: Rutgers, The State University of New JerseyInventors: Joachim B. Kohn, Durgadas Bolikal
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Patent number: 8247603Abstract: 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: GrantFiled: February 16, 2007Date of Patent: August 21, 2012Assignee: Birds Pharma GmbH Berolina InnovativeInventors: Rudolf-Giesbert Alken, Frank Schneider
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Publication number: 20120190861Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: ApplicationFiled: April 5, 2012Publication date: July 26, 2012Applicant: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Patent number: 8168820Abstract: 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: GrantFiled: December 18, 2003Date of Patent: May 1, 2012Assignee: BDD Berolina Drug Development GmbHInventor: Rudolf-Giesbert Alken
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Publication number: 20120094994Abstract: 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: ApplicationFiled: December 24, 2011Publication date: April 19, 2012Applicant: BEZWADA BIOMEDICAL, LLCInventor: Rao S. Bezwada
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Publication number: 20120052110Abstract: 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: ApplicationFiled: August 4, 2011Publication date: March 1, 2012Applicant: Hospital for Special SurgeryInventors: Marjana TOMIC, Carl Peter Blobel, Asheesh Harsha
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Patent number: 8093420Abstract: 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: GrantFiled: October 10, 2006Date of Patent: January 10, 2012Assignee: Bezwada Biomedical, LLCInventor: Rao S. Bezwada
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Publication number: 20110201817Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: ApplicationFiled: April 27, 2011Publication date: August 18, 2011Applicant: XenoPort, Inc.Inventors: Jia-Ning XIANG, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Publication number: 20110190505Abstract: 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: ApplicationFiled: February 4, 2011Publication date: August 4, 2011Inventor: Stephen DiMagno
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Patent number: 7968597Abstract: (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: GrantFiled: December 31, 2008Date of Patent: June 28, 2011Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
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Patent number: 7935843Abstract: 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: GrantFiled: December 8, 2006Date of Patent: May 3, 2011Assignee: Bezwada Biomedical, LLCInventor: Rao S Bezwada
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Publication number: 20100331345Abstract: 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: ApplicationFiled: February 5, 2007Publication date: December 30, 2010Inventors: Song Li, Guochao Liao, Junhai Xiao, Aihua Nie, Lili Wang, Wu Zhong, Zhibing Zheng
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Publication number: 20100298242Abstract: 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: ApplicationFiled: July 26, 2006Publication date: November 25, 2010Inventors: Reiner Postges, Richard Ammer, Joerg Breitkreutz, Dorothee Grueneberg Klinkowski
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Publication number: 20100280108Abstract: 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: ApplicationFiled: December 19, 2008Publication date: November 4, 2010Applicant: 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
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Publication number: 20100222608Abstract: 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: ApplicationFiled: May 12, 2010Publication date: September 2, 2010Applicant: THE NUTRASWEET COMPANYInventors: INDRA PRAKASH, KENNETH E. FURLONG, HANDLEY E. JACKSON, III
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Publication number: 20100197953Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: ApplicationFiled: February 2, 2009Publication date: August 5, 2010Applicant: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Publication number: 20100190725Abstract: 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: ApplicationFiled: July 4, 2008Publication date: July 29, 2010Applicant: PROXIMAGEN LTD.Inventor: Christopher Hobbs
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Publication number: 20100173992Abstract: 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: ApplicationFiled: March 18, 2010Publication date: July 8, 2010Applicant: XenoPort, Inc.Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Publication number: 20100172916Abstract: 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: ApplicationFiled: November 9, 2009Publication date: July 8, 2010Applicant: AUSPEX PHARMACEUTICALS, INC.Inventors: Thomas G. Gant, Craig Hodulik, Soon Woo
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Patent number: 7709527Abstract: 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: GrantFiled: December 20, 2007Date of Patent: May 4, 2010Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Cindy X. Zhou, Fenmei Yao, Mark Q. Nguyen
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Patent number: 7659396Abstract: 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: GrantFiled: May 16, 2007Date of Patent: February 9, 2010Assignee: Wilex AGInventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
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Publication number: 20090240074Abstract: 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: ApplicationFiled: March 20, 2009Publication date: September 24, 2009Inventors: Christopher N. Jobdevairakkam, Hero Velladurai
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Patent number: 7563821Abstract: (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: GrantFiled: December 4, 2006Date of Patent: July 21, 2009Assignee: XenoPort, Inc.Inventors: Jia-Ning Xiang, Xuedong Dai, Cindy X. Zhou, Jianhua Li, Mark Q. Nguyen
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Publication number: 20090170937Abstract: 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 ringType: ApplicationFiled: January 23, 2007Publication date: July 2, 2009Applicants: Proximagen Ltd., Hodgkin Building,King`s College London,Guy`s CompusInventor: Christopher Hobbs
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Publication number: 20090137834Abstract: Prodrugs of levodopa, methods of making prodrugs of levodopa, methods of using prodrugs of levodopa, and compositions of prodrugs of levodopa are disclosed.Type: ApplicationFiled: February 2, 2009Publication date: May 28, 2009Applicant: XenoPort, Inc.Inventors: Jia-Ning Xiang, Mark A. Gallop, Cindy X. Zhou, Mark Nguyen, Xuedong Dai, Jianhua Li, Kenneth C. Cundy, Nelson L. Jumbe
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Publication number: 20090088548Abstract: 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: ApplicationFiled: November 3, 2006Publication date: April 2, 2009Applicant: TyRx Pharma, Inc.Inventors: Arikha Moses, Satish Pulapura, Arthur Schwartz, Qing Ge, Irene Shatova
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Publication number: 20090036684Abstract: 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: ApplicationFiled: March 6, 2007Publication date: February 5, 2009Inventors: Koji Matsuda, Koji Ando, Shigeki Ohki, Jun-ichi Hoshi, Takahiro Yamasaki
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Publication number: 20090030218Abstract: 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: ApplicationFiled: May 17, 2006Publication date: January 29, 2009Applicant: KISSEI PHARMACEUTICAL CO., LTD.Inventors: Kiyoshi Kasai, Minoru Kubota, Ritsu Suzuki, Tetsuji Ozawa, Takehiro Ishikawa, Makoto Kobayashi, Junichi Sonehara, Masahiro Kobayashi
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Publication number: 20090005562Abstract: 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: ApplicationFiled: May 16, 2007Publication date: January 1, 2009Applicant: WILEX AGInventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
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Patent number: 7247724Abstract: The invention relates to an improved method for the production of 3-amidinophenylalanine derivatives, especially triisopropylphenyl-sulfonyl-substituted 3-amidinophenylalanine derivatives.Type: GrantFiled: July 25, 2003Date of Patent: July 24, 2007Assignee: Wilex AGInventors: Katja Wosikowski-Buters, Stefan Sperl, Joachim Sommer
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Patent number: 7193103Abstract: 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: GrantFiled: July 30, 2004Date of Patent: March 20, 2007Assignee: The Nutrasweet CompanyInventor: Indra Prakash
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Patent number: 7183425Abstract: 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: GrantFiled: July 29, 2005Date of Patent: February 27, 2007Assignee: Merck Frosst Canada Ltd.Inventors: Cheng Yi Chen, Paul N. Devine, Bruce S. Foster, Greg Hughes, Paul O'Shea
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Patent number: 7141263Abstract: 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: GrantFiled: June 17, 2005Date of Patent: November 28, 2006Assignee: Ajinomoto Co., Inc.Inventors: Kenichi Mori, Shinji Fujita, Nao Funakoshi, Tadashi Takemoto
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Patent number: 7115296Abstract: 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: GrantFiled: August 8, 2003Date of Patent: October 3, 2006Assignee: Ajinomoto Co., Inc.Inventors: Yusuke Amino, Kazuko Yuzawa
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Patent number: 7057038Abstract: 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: GrantFiled: May 26, 2004Date of Patent: June 6, 2006Assignee: Brandeis UniversityInventors: Li Deng, Jianfeng Hang, Liang Tang