65 results about "Glutamic Acid Derivatives" patented technology

Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.

The present invention provides an organic amine salt of monatin, or crystal form thereof, and its application as well as a method for resolving the stereoisomers of monatin by forming its salt. The present invention further provides a salt form of monatin that is useful as a sweetening agent or as the active ingredient of a sweetener. The present invention also provides a method for preparing a salt of a particular stereoisomer of monatin with an organic amine by utilizing the difference of crystallinity or solubility of the salt of the stereoisomer of monatin with the organic amine. The present invention also relates to a use of the salt in a method for preparing a metal salt of monatin in which the organic amine is replaced by a metal such as sodium, potassium, or the like.

A D-aminotransferase can be modified so as to efficiently produce (2R, 4R)-monatin having high sweetness intensity from 4-(indol-3-ylmethyl)-4-hydroxy-2-oxoglutaric acid by substituting an amino acid at least at one of positions (positions 100, 180 to 183,243 and 244) involved in efficiently producing the (2R, 4R)-monatin in an amino acid sequence of a wild-type D-aminotransferase represented in SEQ ID NO:2.

Production of N-(pyrrolo(2,3-d)pyramine-5-radical)acyl glutamic acid derivative and its intermediate are disclosed. The typical derivative is antineoplastic agent, Z is thienyl bi-radical and furan bi-radical or substituted or non-substituted 1,4-phenylene, R1 and R2 are hydrogen or carboxy protecting group, they can be same or different. Carbon atom with *mark is S type, R type or mixed type of S and R.

The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates thereof, and such compounds prepared by the novel methods.

Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.

Glutamic acid derivatives, in particular monatin, may be conveniently prepared by alkylating a 4-protected hydroxyl pyroglutamic acid derivative with an alkylating agent to prepare a 4-protected hydroxyl-4-alkylglutamic acid derivative, followed by the steps of hydrolysis and deprotection. The 4-protected hydroxyl pyroglutamic acid derivative is easy to produce from hydroxyproline. The 4-protected hydroxyl pyroglutamic acid derivative is particularly suitable for use in the efficient manufacture of monatin of high optical purity, since it can be alkylated selectively at the 4-position and stereoselectively and after its alkylation, it can easily be converted to a glutamic acid derivative.

The invention provides a preparation method of a small-molecule inhibitor for a prostate-specific membrane antigen. The preparation method comprises the following steps: taking a glutamic acid derivative and a lysine derivative as starting raw materials, and preparing a formula (IV) core structure Lys-Urea-Glu for a formula (I) small-molecule inhibitor by using a carbonyldiimidazole one-pot method; and removing a protecting group after the formula (IV) core structure Lys-Urea-Glu is connected with HYNIC with 99mTc chelating power through a connecting chain so as to obtain the formula (I) small-molecule inhibitor. If the small-molecule inhibitor (namely the formula (I) small-molecule inhibitor) for the prostate-specific membrane antigen prepared on the basis of the parathion method is marked by radioactive nuclide 99mTc, the small-molecule inhibitor can be used for the diagnosis of prostatic cancer clinically as a molecular imaging probe and has potential clinical application values.

The invention relates to novel diazoketone derivatives. The invention also relates to processes for homologation of these diazoketone derivatives. The processes are useful for preparing compounds that are caspase inhibitors.

The present invention provides a parakeratosis inhibitor, a pore-shrinking agent, and a rough skin inhibiting or ameliorating agent comprising, as an active ingredient, a compound that has excellent effects and high safety without safety problems such as sensory irritation, and provides an external composition for skin containing the same. The compound is selected from the glutamic acid derivatives represented by formula (1) or (2) and the salts thereof:wherein A represents a carbamoyl group, a benzyloxycarbonyl group, an alkyl group having 1 to 3 carbon atoms, an allyl group, or an amidino group;wherein Z represents an alkyl group having 1 to 4 carbon atoms, an alkenyl group having 2 to 4 carbon atoms, etc.; Y represents OH, an alkyloxy group having 1 to 3 carbon atoms, an allyloxy group, or NR3R4; R1 to R4 each independently represents H, an alkyl group having 1 to 3 carbon atoms, an allyl group, a cycloalkyl group having 3 to 7 carbon atoms, a cycloalkenyl group having 3 to 7 carbon atoms, a phenyl group, or a benzyl group, or R1 and R2, or R3 and R4, independently form a heterocycle.

Fluids are provided which resist phase separation by inclusion of a stabilizing amount of a glutamic acid derivative in the presence of ethanol. The fluids comprise an aqueous discontinuous phase, a silicone oil containing continuous phase, a glutamic acid derivative such as dibutyl ethylhexanoyl glutamide, and ethanol. The fluids may be prepared without heating to solubilize the glutamic acid derivative

Provided is a poly-γ-glutamic acid derivative having appropriately controlled hydrophilicity, which can be processed into a form of fine particles. Provided is a PGA derivative in a form of fine particles having a particle diameter of 50 to 1,000 nm, which is obtained by introducing cholesterol into poly-γ-glutamic acid (PGA). Thus, the PGA particles can be mixed with various biological materials (e.g., medicament) so as to be used in various applications in the field of biotechnology. Specifically, it can be used as a carrier of a medicament, or the like. Further, it is also made possible to use PGA in various applications in the field of nanotechnology that is studied in recent years.

The present invention relates to a composition for coating keratin fibres, more particularly the eyelashes, characterized in that it is present in the form of a wax-in-water emulsion comprising a combination of at least one glutamic acid derivative and / or salt thereof and at least one alkylpolyglycoside.

The invention belongs to the technical field of nutrition products and particularly relates to a composition for improving glutathione concentration in a human body and a preparation method and an application thereof. The composition is composed of an A component and a gain agent, wherein the A component is composed of glutamic acid and / or glutamic acid derivatives, cystine and / or cystine derivatives, glycine and / or glycine derivatives. According to the composition disclosed by the invention, the A component is cooperatively used together with the gain agent to improve the solubility of the composition in the mouth, so as to promote the adsorption of a human body to the composition, improve the utilization rate of the composition, more effectively promote the synthesis of glutathione in vivo and improve the concentration level of the glutathione in the human body and further improve the immunity of the human body; and the composition disclosed by the invention has antioxygenation and detoxication. The combined use of the A component and the gain agent can also improve the taste of the composition, so that the composition is more suitable for direct taking of people. Since the glutathione is a very important antioxidant in the human body, and cellular oxidation is the root of aging and various diseases, the composition disclosed by the invention can be applied to prevention and auxiliary treatment of various diseases.

Many variations of compounds having CaSR agonistic activity are searched and a CaSR agonist agent, a pharmaceutical composition, a preventive or therapeutic agent for diarrhea, and a kokumi taste-imparting agent containing the compound are provided. The CaSR agonist agent, pharmaceutical composition, preventive or therapeutic agent for diarrhea, and kokumi taste-imparting agent, characterized by containing a glutamic acid derivative or a pharmaceutically acceptable salt thereof having CaSR agonistic activity.

The invention discloses a butyryl glutamic acid derivative as well as a composition and application thereof. The butyryl glutamic acid derivative disclosed by the invention or a racemic modification,stereisomer, geometric isomer, tautomer and solvate or feed-acceptable salt thereof can be applied in the preparation of novel feed additives and feeds. The invention further discloses a feed composition of the butyryl glutamic acid derivative or the racemic modification, the stereisomer, the geometric isomer, the tautomer and the solvate or the feed-acceptable salt thereof. When applied in animalhusbandry, the butyryl glutamic acid derivative provided by the invention has the effect of improving the production performance of animals, such as increasing animal weight increasing rate, decreasing feed conversion ratio and controlling diarrhea rate, and can be applied as an effective, safe novel feed additive.

The present invention relates to novel methods for the preparation of glutamic acid derivatives and intermediates thereof, and such compounds prepared by the novel methods.

This invention relates to methods, which provide access to F-18 labeled glutamic acid derivatives.

The invention discloses a glutamic acid derivative, a preparation method thereof, and a preparation method of a multi-scale porous structured TiO2 crystalline aerogel. The structural formula of the derivative is shown in the description; and in the formula, and n is an integer in a range of 7-13, m is 0, 1 or 2. The derivative has a self-assembling characteristic, and the preparation method of the derivative has the advantages of simplicity, and mild reaction conditions. The anatase TiO2 crystalline aerogel having three-dimensional continuous nanometer and nanometer pores is prepared through covalent grafting of the surface of TiO2 nano-particles with the above compound, centrifugal concentration, freeze drying and annealing, and the centrifugal rotating speed is adjusted to realize the regulation of the pore dimensions. The crystalline aerogel can be used for photocatalytic degradation of formaldehyde gas.

The invention relates to a preparation method of a novel glycoside ceramide analogue with immunoregulation activity and an application thereof, and belongs to the technical field of chemistry and medicine. Based on the structural analysis of a receptor and combined with molecular docking and molecular dynamics simulation technologies, a category of compound with modified sugar ring (tryptophan, glutamic acid derivative or p-hydroxyphenylpropionic acid are introduced into R1 or R2 sites respectively) is designed and synthesized. Biological activity research shows that such compound has Th2 selectivity and has potential for use in pharmaceuticals. The novel compound has the following main synthetic characteristics: R1 is a hydroxyl group or a tryptophan derivative linked through an amide condensation reaction; R2 is a hydroxyl group or an L-glutamic acid derivative linked through amide condensation reaction, or p-hydroxybenzoic acid; R3 is -OBn, R4 is -N3;or R3 is -N3, R4 is -OBn;R5 maybe a substituent such as SEt, S-iPr, SPh, STOL, OC (NH) CCl3, and the like.

There is provided FV derivatives that reduce blood clotting activity, by reducing thrombin generation, when compared to wild-type FV. In particular, the FV of the present invention comprises single-point and multi-point mutations, encompassed by aspartic acid 79 to glutamic acid 119. The derivatives can be used to treat patient with conditions necessitating reduced clotting activity.

Provided is a pharmaceutical preparation that is suitable for more effectively exhibiting the efficacy of a glutamic acid derivative, which is a GGT-recognizable prodrug, by producing a composition including a glutamic acid derivative capable of rapidly releasing a physiologically active substance by being recognized by GGT, or a pharmacologically acceptable salt thereof; and a block copolymer in which a polyethylene glycol segment is linked to a polyamino acid segment with a hydrophobic group. Particularly, the composition based on a glutamic acid derivative that uses an antitumor compound as a physiologically active substance is capable of effectively accumulating the glutamic acid derivative at a tumor affected area, exhibits a superior effect against tumors, and is capable of suppressing the release of a physiologically active substance in bone marrow tissue where the expression ratio of GGT is low. Therefore, side effects such as myelosuppression, which pose a problem in the use of antitumor drugs, may be avoided.

Disclosed relates to a process for preparing N(5)-ethylglutamines economically without a specific purification process via a simplified and safe process, in which glutamic acid derivatives, represented by formula 1, protected by phthaloyl groups react with ethylamine to cause an amidation and a deprotection reaction in turn under the same reaction condition, thus preparing N(5)-ethylglutamines.