156results about "Saccharide with acyclic radicals" patented technology

The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

The invention is directed to novel compounds of formulae (I), (II) and (III): wherein X is O or NH; R3 is OH or a monosaccharide and R4 is hydrogen, or R3 is hydrogen and R4 is OH or a monosaccharide; R5 is hydrogen or a monosaccharide; and pharmaceutically acceptable salts or esters thereof. The invention is also directed to the use of the compounds both directly and as immune adjuvants for treating cancer, infectious diseases and autoimmune diseases. The invention is also directed to syntheses of the intermediates which can be used to make these novel compounds.

The present invention is a compound of general formula (I) or a pharmaceutically acceptable salt of,wherein W represents carbon chain from 9 to 17 which containing double bond or hydroxy group occasionally; X represents carbon chain from 11 to 25 which containing double bond or hydroxy group occasionally; Y represents -(CH2)a-CH=CH-(CH2)a'-, -(CH2)a- (a, a' denotes an integer of 0-5 and a+a' is 5 and under.), -S(O)0-2CH2-, -NHCH2-; Z represents -CO-, -SO2-; R represents -CH2OH, CO2H, CH2OCH2CO2SO3H; R0 represents -OH, -NH2, -NHAc.

A monomer useful in prepaπng therapeutic compounds includes a diversity element which potentially binds to a target molecule with a dissociation constant of less than 300 11 M and a linker element connected to the diversity element The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to said diversity element, and is capable of forming a reversible covalent bond or noncovalent interaction with a binding partner of the linker element The monomers can be covalently or non-covalently linked together to form a therapeutic multimer or a precursor thereof

The invention relates to the field of pharmaceutical chemistry, and in particular to a lenalidomide derivative (I). G and n are defined in a direction book. Pharmacological tests show that the lenalidomide derivative plays an inhibiting role in vascular endothelial cell proliferation and can be used for clinical treatment of tumors or chronic inflammations.

The present invention is a compound of general formula (I) or a pharmaceutically acceptable salt of, wherein W represents carbon chain from 9 to 17 which containing double bond or hydroxy group occasionally; X represents carbon chain from 11 to 25 which containing double bond or hydroxy group occasionally; Y represents -(CH2)a-CH=CH-(CH2)a'-, -(CH2)a- (a, a' denotes an integer of 0-5 and a+a' is 5 and under.), -S(O)0-2CH2-, -NHCH2-; Z represents -CO-, -SO2-; R represents -CH2OH, CO2H, CH2OCH2CO2SO3H; R0 represents -OH, -NH2, -NHAc.

Disclosed are a therapeutic pharmaceutical agent for diseases associated with the decrease in the function of GNE protein, a food composition, and a food additive. The therapeutic pharmaceutical agent is characterized by comprising a compound capable of increasing the quantity of N-acetylneuraminic acid in cells. Examples of the compound to be contained in the therapeutic pharmaceutical agent include N-acetylneuraminic acid, an intermediate produced downstream from N-acetylmannosamine in an N-acetylneuraminic acid biosynthesis pathway, an N-acetylneuraminic acid derivative, an N-acetylmannosamine derivative, an N-acetylneuraminic acid-containing compound, an N-acetylneuraminic acid derivative-containing compound, an N-acetylmannosamine-containing compound, an N-acetylmannosamine derivative-containing compound, an inhibitor of a degrading enzyme for N-acetylneuraminic acid, an inhibitor of a degrading enzyme for N-acetylmannosamine, an inhibitor of a degrading enzyme for the intermediate, and others.

The present invention is directed to a monomer useful in preparing therapeutic compounds. The monomer includes a diversity element which potentially binds to a target molecule with a dissociation constant of less than 300 μM and a linker element connected to the diversity element. The linker element has a molecular weight less than 500 daltons, is connected, directly or indirectly through a connector, to said diversity element, and is capable of forming a reversible covalent bond or non-covalent interaction with a binding partner of the linker element. The monomers can be covalently or non-covalently linked together to form a therapeutic multimer or a precursor thereof. Also disclosed is a method of screening for therapeutic multimer precursors which bind to a target molecule associated with a condition and a method of screening for linker elements capable of binding to one another. The present invention additionally relates to a therapeutic multimer, which includes a plurality of covalently or non-covalently linked monomers, therapeutic monomers, and uses of such dimers and monomers.

Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl Lex, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

Disclosed herein is a class of linkable tetrasaccharide compounds that includes the amino phenyl glycoside of sialyl Lewis X (SLeX) and related analogs. These compounds have conjugatable nucleophilic groups, making them useful in preparing multimeric SLeX compositions. In particular, the disclosed SLeX compounds can be used to prepare selectin binding ligand conjugates by linking them to a reporter moiety, such as a contrast agent, a radiodiagnostic agent, or a cytotoxic or chemotherapeutic agent. The SLeX compounds and conjugates of the invention exhibit binding to selectin that is similar to native Sialyl LeX, and are, therefore, useful for diagnosing and treating selectin-mediated disorders and related conditions.

The invention discloses a Maillard reaction intermediate and the preparation method and application of the intermediate, relating to the organic chemical technical field. The invention discloses the preparation method of the Maillard reaction intermediate to lead the Maillard reaction to stay at the initial stage; the Maillard reaction intermediate with the structural formula of (I) or (II) is obtained; one or two mixtures in the Maillard reaction intermediate (I) or (II) are added into tobacco according to the proportion of 0.04 to 0.06 percent of the weight of the tobacco. The Maillard reaction intermediate obtained by the applicant is totally a novel substance undisclosed till now and the technical process adopted by the applicant to synthesize the Maillard reaction intermediate is totally novel. The Maillard reaction intermediate of the invention is firstly adopted as the additive of cigarette for application and the performance thereof is further better than that of the Maillard reaction high-grade outcome.

This invention discloses a method for decoloring polysialic acid hydrolysate. The method comprises: (1) performing aerobic fermentation on Escherichia coli strain to obtain fermented liquid containing polysialic acid, removing bacteria, precipitating with ethanol, and dissolving again in deionized water to prepare 2 wt.% polysialic acid solution; (2) hydrolyzing with an acid, neutralizing with an alkali, and centrifuging; (3) passing through an adsorption chromatographic column filled with attapulgite as the filler, eluting, collecting the eluant, and freeze-drying to obtain sialic acid product. Containing deep brown and red substances, the polysialic acid hydrolysate is treated by adsorption chromatography to obtain white powdery sialic acid product.

The invention discloses a method for preparing an Amadori compound by virtue of a temperature-variable water phase. According to a principle that cysteine can be combined with an Amadori rearrangement product (ARP) so as to inhibit the brown stain of Maillard reaction, water is taken as a solvent, cysteine is taken as a tracer agent, amino acid and sugar are heated under a certain condition to react, an intermediate is prepared in a water phase under an intermediate formation critical condition determined by virtue of the temperature-variable Maillard reaction, and after the reaction is finished, reduced pressure vaporization is carried out at a low temperature to remove moisture, so as to obtain an ARP solid product. According to a determination method of the critical condition formed by an ARP water phase, only a spectrophotometer is adopted, so that the operation is simple, the cost is low, and the application value is relatively high. According to a water phase synthesis technique disclosed by the invention, the production cost of the ARP is effectively lowered, the industrial requirements of environmental friendliness and sustainability are met; and meanwhile, the obtained ARP product is low in volatility and good in storage stability and has relatively high superiority, and the controllable formation of flavor processing can be realized.

Disclosed are linear discrete PEG constructs, which can be created and produced in a precise and reproducible way. Key to being able to do these things, where x in the discrete PEGx can vary from about 2 to about 64, is that the processes used to make each linear portion is controlled to give essentially one oligomer / one compound. Having a variable length linear discrete PEG construct that is (a) primarily an linear discrete PEG construct with diagnostic or therapeutic groups attached along a chain of attachment cores, which is attached to a preferential locator; (b) is an m-discrete PEG as the terminal construct on the linear portion, and “hidden”; (c or linear discrete PEG with a terminus group that can be either negatively or positively charged, or neutral; and any of the discrete PEG portions can be designed to be cleaved after entering the cell.

The invention relates to methods, compounds, compositions and vehicles for delivering 3-amino-1-propanesulfonic acid (3APS) in a subject, preferably a human subject. The invention encompasses compound that will yield or generate 3APS, either in vitro or in vivo. Preferred compounds include amino acid prodrugs of 3APS for use, including but not limited to the prevention and treatment of Alzheimer's disease

The present invention relates to pharmaceutical compositions containing tumor-selective targeted inhibitor glycoconjugates. These bioconjugates are ALK5 inhibitors covalently bound to biocompatible carrier molecules which selectively target and specifically bind to Muc4 that is overexpressed on a variety of tumor cell types. The ALK5 inhibitors are conjugated to tumor targetable glycans through a covalent linker. Preferably the acid-labile linker is designed to be stable in plasma and releases pharmacologically active inhibitors through acid-catalyzed hydrolysis in the acidic environment of the target tumor where the inhibitor activity is restored. Because the glycoconjugates are stable at physiological pH and in plasma, they advantageously reduce undesirable systemic ALK5 inhibitor activity; however, the preferable glycoconjugates are acid-labile conjugates that can be hydrolyzed upon reaching the more acid environment of the tumor.

Disclosed are analgesic-related compositions and methods of using the compositions for modulation of analgesic receptor activity. The compositions and methods are useful for reducing pain, as well as for therapeutic intervention of addictions or other diseases or disorders amenable to treatment or prophylaxis by modulation of analgesic receptor signaling.

The present disclosure is directed to vaccines, antibodies, and / or immunogenic conjugate compositions targeting the SSEA3 / SSEA4 / GloboH associated epitopes (natural and modified) which elicit antibodies and / or binding fragment production useful for modulating the globo-series glycosphingolipid synthesis. The present disclosure relates to methods and compositions which can modulate the globo-series glycosphingolipid synthesis. Particularly, the present disclosure is directed to glycoenzyme inhibitor compound and compositions and methods of use thereof that can modulate the synthesis of globo-series glycosphingolipid SSEA3 / SSEA4 / GloboH in the biosynthetic pathway; particularly, the glycoenzyme inhibitors target the alpha-4GalT; beta-4GalNAcT-I; or beta-3GalT-V enzymes in the globo-series synthetic pathway. Moreover, the present disclosure is also directed to the method of using the compositions described herein for the treatment or detection of hyperproliferative diseases and / or conditions.

This invention relates to crystals comprising apo-LsrB and holo-LsrB. The structure of holo-LsrB identifies a tetrahydroxytetrahydrofuran derived from 4,5-dihydroxy-2,3-pentanedione (DPD) as the active autoinducer-2 (AI-2) molecule in Salmonella typhimurium. The X-ray crystallographic data can be used in a drug discovery method. Additionally the invention provides AI-2 analogs based on this discovery as well as pharmaceutical compositions containing those analogs.

The invention relates to novel humectant, namely 6-O-carboxymethyl-D-galactopyranose for tobacco and a preparation method of the humectant. D-galactose is used as material; isopropylidene is led to carry out protection and deprotection on the D-galactose hydroxyl, and the novel polyhydroxy humectant, namely 6-O-carboxymethyl-D-galactopyranose for tobacco is successfully synthetized. The humectant has good physical moisturizing action on a cigarette by physical moisturizing performance test and inner sense quality evaluation, irritation and miscellaneous gas of the cigarette can be reduced, and the round taste and comfort of cigarette smoke are improved.

The invention provides therapeutic methods and compositions for the prevention and treatment of Siglec-8 associated diseases and disorders such as asthma and allergic reactions. In particular, the invention provides methods and compositions for the prevention and treatment of diseases and disorders associated with Siglec-8 expressing cells in humans, as well as other animals, through the administration of one or more novel, carbohydrate-based compounds.

The invention provides an artificial synthesis method of arginyl-fructose (AF). The synthesis method is high in synthetic rate, environmentally-friendly and suitable for industrial production. According to the synthesis method, arginine and one or more monosaccharides are combined together and then react in one or more solvents, one or a mixture of more of vitamin C, sodium sulfite and edible organic acid can be added into a reaction system, the heating time is 120-200min, and the best reaction temperature is 80 DEG C, so that the AF can be generated. The synthesized AF is capable of well removing hydroxyl free radicals and superoxide anions, and can inhibit the growth of tumors of H22 tumor-bearing mice so as to improve the immunity of immunosuppressed mice.

The invention discloses a producing method of N-acetamino glucose methylal, including: neutralizing amino glucose hydrochloride and agent, obtaining amino glucose, acetylating the amino glucose by acetic anhydride to obtain N-acetamino glucose, making acetalation reaction on the N-acetamino glucose on condition of sulphuric acid and methanol existing, obtaining N-acetamino glucose methylal. It has simple producing method and high purity of product; high yield of product, up to 80% above.

The invention is directed to novel compounds of formulae (I), (II) and (III): wherein X is O or NH; R<3> is OH or a monosaccharide and R<4> is hydrogen, or R<3> is hydrogen and R<4> is OH or a monosaccharide; R<5> is hydrogen or a monosaccharide; and pharmaceutically acceptable salts or esters thereof. The invention is also directed to the use of the compounds both directly and as immune adjuvants for treating cancer, infectious diseases and autoimmune diseases. The invention is also directed to syntheses of the intermediates which can be used to make these novel compounds.