- A PROCESS FOR THE PREPARATION OF L-GLUTAMINE
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The present invention relates to a process for the preparation of L-Glutamine of Formula (I). The present invention also relates to an improved process for the purification of L-Glutamine of Formula (I) having specific bulk density and Hausner ratio.
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Page/Page column 14; 15
(2022/01/24)
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- COMPLEX
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PROBLEM TO BE SOLVED: To provide a substance that can be used in a simple quantitative method for desmosines. SOLUTION: In the complex of the present invention, desmosine is bound to a protein directly or via a linking group at the side chain terminal of the 4-position of the pyridine ring of desmosine. SELECTED DRAWING: None COPYRIGHT: (C)2020,JPOandINPIT
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- NOVEL JAK1 SELECTIVE INHIBITORS AND USES THEREOF
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The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic di
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Page/Page column 47
(2018/04/21)
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- Constrained Cyclic β,γ-Diamino Acids from Glutamic Acid: Synthesis of Both Diastereomers and Unexpected Kinetic Resolution
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We describe here an efficient synthesis of both diastereomers of cyclic β,γ-diamino acids starting from l-glutamic acid, based on the Blaise reaction. We show that by changing the protecting group, we can access either the five-membered-ring lactam, which
- Wan, Yang,Auberger, Nicolas,Thétiot-Laurent, Sophie,Bouillère, Francelin,Zulauf, Ana?s,He, Jiefang,Courtiol-Legourd, Stéphanie,Guillot, Régis,Kouklovsky, Cyrille,Cote des Combes, Sylvain,Pacaud, Christophe,Devillers, Ingrid,Alezra, Valérie
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p. 329 - 340
(2018/01/27)
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- Synthesis of ortho-carboranyl derivatives of (S)-asparagine and (S)-glutamine
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(S)-Asparagine and (S)-glutamine ortho-carboranyl derivatives with free amino and carboxy groups in the α-position were synthesized. By an example of Nγ-(1,2-dicarba-closo-dodecarboran-3-yl)-(S)-glutamine it was demonstrated that the developed synthetic approach carboranyl derivatives of amino acids allowed the preparation of optically pure isomers.
- Gruzdev,Levit,Olshevskaya,Krasnov
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p. 769 - 776
(2017/07/07)
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- LYSINE ISOTOPOLOGUES, COMPOSITIONS COMPRISING THE SAME AND METHODS OF SYNTHESIS
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This invention relates to lysine isotopologues of Formulas I and 1-A, as described herein, and processes for synthesizing the same and derivatives and intermediates involved therein. In one aspect, described herein is a chemical compound comprising an isotopically labeled analog, i.e., an isotopologue of a standard or naturally occurring lysine. The lysine isotopologue is synthetically formed to have stable isotopes of elements incorporated at selected positions. As such, the lysine isotopologue has a molecular mass different from the mass of a standard or naturally occurring lysine.
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Paragraph 0165-0166
(2016/02/12)
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- METHOD FOR PRODUCING DESMOSINE, ISODESMOSINE AND DERIVATIVES THEREOF
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A process for preparing a compound represented by the following general formula (I) or a salt thereof, which comprises reacting lysine or a protective product thereof or a salt thereof with allysine or a protective product thereof in the presence of a spe
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- Organomediated Enantioselective 18F Fluorination for PET Applications
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The first organomediated asymmetric 18F fluorination has been accomplished using a chiral imidazolidinone and [18F]N-fluorobenzenesulfonimide. The method provides access to enantioenriched 18F-labeled α-fluoroaldehydes (>90 % ee), which are versatile chiral 18F synthons for the synthesis of radiotracers. The utility of this process is demonstrated with the synthesis of the PET (positron emission tomography) tracer (2S,4S)-4-[18F]fluoroglutamic acid.
- Buckingham, Faye,Kirjavainen, Anna K.,Forsback, Sarita,Krzyczmonik, Anna,Keller, Thomas,Newington, Ian M.,Glaser, Matthias,Luthra, Sajinder K.,Solin, Olof,Gouverneur, Véronique
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p. 13366 - 13369
(2015/11/09)
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- Biomimetic chichibabin pyridine synthesis of the COPD biomarkers and elastin cross-linkers isodesmosine and desmosine
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The tetrasubstituted pyridinium amino acids isodesmosine and desmosine are cross-linkers of elastin and are attractive biomarkers for the diagnosis of chronic obstructive pulmonary disease (COPD). In this study, the biomimetic total synthesis of isodesmosine and desmosine via a lanthanide-promoted Chichibabin pyridine synthesis using the corresponding aldehyde and amine hydrochloride is reported.
- Usuki, Toyonobu,Sugimura, Takanori,Komatsu, Akira,Koseki, Yohei
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supporting information
p. 1672 - 1675
(2014/04/17)
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- Diaminodiacid-based solid-phase synthesis of peptide disulfide bond mimics
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The antimicrobial peptide tachyplesin I was used as a model to apply the title strategy, which was developed for the preparation of peptidic macrocycles with double disulfide surrogates. The folding and activity of the tachyplesin I analogues were found to be sensitive to the structure of the disulfide surrogates, thus underlining the necessity of a flexible synthetic route for generating disulfide bond surrogates with high structural diversity. Copyright
- Cui, Hong-Kui,Guo, Ye,He, Yao,Wang, Feng-Liang,Chang, Hao-Nan,Wang, Yu-Jia,Wu, Fang-Ming,Tian, Chang-Lin,Liu, Lei
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p. 9558 - 9562
(2013/09/23)
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- RENIN INHIBITORS
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Disclosed are aspartic protease inhibitors represented by the following structural formula: and pharmaceutically acceptable salts thereof. These compounds are orally active and bind to aspartic proteases to inhibit their activity. They are useful in the t
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Page/Page column 33-34
(2010/08/07)
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- Facile transformation of glutamic acid into proline residue inside a tripeptide backbone
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In this Letter we present a simple reaction pathway which allows the conversion of the glutamic acid residue of a tripeptide into a proline residue. The reaction was performed by using Boc-Val-Glu-Phe-NH2 as a starting material and is based on a NaH-induced intraresidue alkylation under reaction conditions analogous to that adopted during the Freidinger lactams formation.
- Mollica, Adriano,Stefanucci, Azzurra,Feliciani, Federica,Torino, Domenica,Cacciatore, Ivana,Pinnen, Francesco,Lucente, Gino
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scheme or table
p. 1333 - 1335
(2010/04/29)
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- Synthesis of novel carboranyl derivatives of α-amino acids
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New routes to closo-carboranyl derivatives of L-lysine and L-glutamic acid with free α-NH2 groups were proposed.
- Gruzdev,Levit,Bazhov,Demin,Sadretdinova,Ol'shevskaya,Kalinin,Krasnov,Chupakhina
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experimental part
p. 110 - 115
(2011/01/07)
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- Inhibition of glyoxalase I: The first low-nanomolar tight-binding inhibitors
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A series of rational modifications to the structure of known S-(N-aryl-N-hydroxycarbamoyl)glutathione-based glyoxalase I inhibitors culminated in the discovery of the first single-digit nanomolar inhibitor. This study makes available key information about possible means to address the issues of metabolic instability, low potency, and synthetic complexicity that have plagued the area of glyoxalase I inhibition. Knowledge garnered from this study has implications in the design of inhibitors with higher conformational definition and lower peptidic character.
- More, Swati S.,Vince, Robert
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supporting information; experimental part
p. 4650 - 4656
(2010/03/01)
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- Design, synthesis, and binding studies of bidentate Zn-chelating peptidic inhibitors of glyoxalase-I
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The known affinity of ethyl acetoacetate (ACC) toward divalent zinc prompted us to attempt its employment as a chelating moiety in the design of glyoxalase-I inhibitors. A practical synthetic route was developed to incorporate this pharmacophore into the side chain of glutamic acid, with flexibility to allow incorporation of additional functionality at the end-stage of the synthesis. Herein, the details of this synthetic approach as well as the evaluation of the resultant β-keto ester compounds are reported.
- More, Swati S.,Vince, Robert
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p. 3793 - 3797
(2008/02/13)
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- Synthesis, characterization and cytolytic activity of α-helical amphiphilic peptide nanostructures containing crown ethers
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Many natural α-helical amphiphilic peptides are known to have lytic activity toward different cells. Herein, we describe the synthesis and the characterization of synthetic α-helical amphiphilic peptide nanostructures containing crown ethers, as well as t
- Boudreault, Pierre-Luc,Voyer, Normand
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p. 1459 - 1465
(2008/02/08)
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- HALOARYL SUBSTITUTED AMINOPURINES, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH
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Provided herein are Aminopurine Compounds having the following structure: (I) wherein R1 , R2 and and R3 are as defined herein, compositions comprising an effective amount of an Aminopurine Compound and methods for treating or preventing cancer, a cardiovascular disease, a renal disease, an autoimmune condition, an inflammatory condition, macular degeneration, ischemia-reperfusion injury, pain and related syndromes, disease-related wasting, an asbestos-related condition, pulmonary hypertension or a condition treatable or preventable by inhibition of the JNK pathway comprising administering an effective amount of an Aminopurine Compound to a patient in need thereof.
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Page/Page column 150-151
(2008/06/13)
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- Copper(I) mediated cross-coupling of amino acid derived organozinc reagents with acid chlorides
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This paper describes the development of a straightforward experimental protocol for copper-mediated cross-coupling of amino acid derived β-amido-alkylzinc iodides 1 and 3 with a range of acid chlorides. The present method uses CuCN·2LiCl as the copper source and for organozinc reagent 1 the methodology appears to be limited to reaction with more stable acid chlorides, providing the desired products in moderate yields. When applied to organozinc reagent 3, however, the protocol is more general and provides the products in good yields in all but one of the cases tested. The Royal Society of Chemistry 2006.
- Hjelmgaard, Thomas,Tanner, David
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p. 1796 - 1805
(2008/02/05)
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- COMBINATION THERAPY WITH INHIBITORS OF INDUCIBLE NITRIC OXIDE SYNTHASE AND ALKYLATING AGENTS
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A combination therapy comprising administration of a carbamoylating chemotherapeutic agent in conjunction with administration of a selective iNOS inhibitor compound is disclosed. Optionally, resection and radiation therapy are provided with the therapeutic combination. A medicament comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound together with a pharmaceutically acceptable carrier is further disclosed. A kit comprising a carbamoylating chemotherapeutic agent and a selective iNOS inhibitor compound is further disclosed.
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Page/Page column 60-61
(2010/02/11)
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- Enzymatic removal of carboxyl protecting groups. 2. Cleavage of the benzyl and methyl moieties
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Enzymes are versatile reagents for the efficient removal of methyl and benzyl protecting groups. An esterase from Bacillus subtilis (BS2) and a lipase from Candida antarctica (CAL-A) allow a mild and selective removal of these moieties in high yields without affecting other functional groups.
- Barbayianni, Efrosini,Fotakopoulou, Irene,Schmidt, Marlen,Constantinou-Kokotou, Violetta,Bornscheuer, Uwe T.,Kokotos, George
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p. 8730 - 8733
(2007/10/03)
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- METHODS FOR TREATMENT AND PREVENTION OF GASTROINTESTINAL CONDITIONS
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Therapeutic methods for the prevention ad treatment of conditions and diseases of the gastrointestinal tract involving an overproduction of nitric oxide by inducible nitric oxide synthase are described, the methods including administering to a subject in need thereof a therapeutically effective amount of a selective inhibitor of inducible nitric oxide synthase (iNOS). The methods also include the use of selective inhibitors of iNOs in combination with other therapeutic agents, including antimicrobial agents and antisecretory agents.
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Page/Page column 53-54
(2010/02/06)
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- Utility of tetrathiomolybdate and tetraselenotungstate: Efficient synthesis of cystine, selenocystine, and their higher homologues
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Efficient synthesis of cystine, selenocystine, and their higher homologues like homo and bishomo amino acid derivatives from natural amino acid derivatives using tetrathiomolybdate and tetraselenotungstate reagents under mild and neutral conditions is reported. The generality of the reaction has been studied by capping various groups to amino and carboxyl components of canonical amino acids.
- Bhat, Ramakrishna G.,Porhiel, Emmanuel,Saravanan, Vadivelu,Chandrasekaran, Srinivasan
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p. 5251 - 5253
(2007/10/03)
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- Sulfonylamino derivatives which inhibit matrix-degrading metalloproteinases
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Compounds of formula (I) wherein W is —OH or —NHOH; X is an optionally substituted heterocycle, NR1SO2R2, heterocyclylalkythio, CONR2R3or NR1COR2; Y, Z, R1-R3and n are as defined in the application. Compounds (I) are inhibitors of matrix-degrading metalloproteinases and are use for the treatment of related conditions.
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- Design and synthesis of novel tubular and cage structures based on thiazole-containing macrolactams related to marine cyclopeptides
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Tubular and cage structures, i.e. 16 and 18, have been synthesised from modified cyclic peptides following selective cyclotrimerisations of L-ornithine and L-glutamic acid thiazole amino acids under high dilution conditions.
- Pattenden,Thompson
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p. 717 - 718
(2007/10/03)
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- SYNTHESE DE L'ACIDE 3-(3,6-DIOXOPIPERAZIN-2-YL) PROPANOIQUE
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The 3-(3,6-dioxopiperazin-2-yl) propanoic acid (8) was synthesized from L-5-methyl glutamate (1) and ethyl glycinate.The regioselectivity was controled by using t-BOC-ON and EEDQ.
- Jerumanis, Stanislas,Lefebvre, Jean
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p. 127 - 130
(2007/10/02)
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- Synthesis of enantiomerically pure β- and γ-amino acids from aspartic and glutamic acid derivatives
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An efficient synthesis of enantiomerically pure β- and γ-amino acids starting from commercially available aspartic and glutamic acid derivatives is described. The acid function, α to the amino group, is first transformed to a good leaving group and the pr
- El Marini,Roumestant,Viallefont,Razafindramboa,Bonato,Follet
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p. 1104 - 1108
(2007/10/02)
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- Synthesis of Four Diastereomeric L-2-(Carboxycyclopropyl)glycines. Conformationally Constrained L-Glutamate Analogues
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To determine what conformations of L-glutamate (L-Glu) activate that compound's different receptors in the mammalian central nervous system, four diastereochemically L-2-(carboxycyclopropyl)glycines, 1-4, which are conformationally constrained analogues o
- Shimamoto, Keiko,Ishida, Michiko,Shinozaki, Haruhikio,Ohfune, Yasufumi
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p. 4167 - 4176
(2007/10/02)
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- NEW ROUTES TO THE SYNTHESES OF CIS-α-(CARBOXYCYCLOPROPYL)GLYCINES FROM L-GLUTAMIC ACID. CONFORMATIONALLY RESTRICTED ANALOGUES OF THE EXCITATORY NEUROTRANSMITTER L-GLUTAMIC ACID
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Potent neuroactive amino acids, (2S,2S,4R) and (2S,3R,4S) isomers of α-(carboxycyclopropyl)glycines (CCG-III and CCG-IV), were synthesized from L-glutamic acid via a palladium(II) catalyzed cyclopropanation of the α,β-unsaturated pyrrolidone and γ-amino-δ-lactone derivatives, respectively.
- Shimamoto, Keiko,Ohfune, Yasufumi
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p. 3803 - 3804
(2007/10/02)
-
- Glucosamine peptide derivatives, their production and use
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Novel glucosamine-peptide derivatives of the formula: STR1 wherein m is 0 or 1; n is 0 or an integer of 1 to 9; R is lower alkyl which may be substituted with hydroxyl, or aryl; R1 is hydrogen or acyl having an acyclic hydrocarbon group, the terminal of which may be substituted with a cyclic hydrocarbon group directly, via a carbonyl group or via an oxygen atom; provided that when R1 is hydrogen m is 1; R2 is hydrogen or lower alkyl which may form a ring by connecting its terminal with the α-nitrogen atom when n is 0, or hydrogen when n is an integer of 1 to 9; R3 is hydrogen or lower alkyl; R4 and R5 are each hydrogen or lower alkyl which may be substituted with hydroxyl or benzyloxyl; R6 is hydrogen or lower alkyl; R7 is alkyl which may be substituted with lower alkoxyl or aralkyl; R8 and R9 are each hydrogen, lower alkyl or aralkyl; and (D) and (L) each indicate configurations if their respective carbon atoms are asymmetric; or an acid addition salt thereof, have immunostimulatory activity.
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