5391 results about "Benzyl group" patented technology

Compounds of the formulaeLAn-Z-X—WwD and BZ-X—WwDwherein: D is a drug moiety; L is a ligand; B is a blocking group; A is an optional acyl unit; Z is an amino acid or a peptide residue; X is an aminobenzyl ether self-immolative spacer group; W is an optional second self-immolative group; n is an integer of 0 or 1; and w is an integer of 0 or 1, and compositions of said compounds with pharmaceutically acceptable carrier, diluent and / or excipient, and methods of delivery the drug D via the compounds.

This invention provides for prodrug Compounds I, pharmaceutical compositions thereof, and their use in treating HIV infection.wherein:X is C or N with the proviso that when X is N, R1 does not exist;W is C or N with the proviso that when W is N, R2 does not exist;V is C;E is hydrogen or a pharmaceutically acceptable salt thereof; andY is selected from the group consisting ofAlso, this invention provides for intermediate Compounds II useful in making prodrug Compounds I.wherein:L and M are independently selected from the group consisting of C1-C6 alkyl, phenyl, benzyl, trialkylsilyl, -2,2,2-trichloroethoxy and 2-trimethylsilylethoxy.

A class of 2′-fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae:whereinBase is a purine or pyrimidine base;R1 is OH, H, OR3, N3, CN, halogen, including F, or CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy, and base refers to a purine or pyrimidine base;R2 is H, phosphate, including monophosphate, diphosphate, triphosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of providing a compound wherein R2 is H or phosphate; sulfonate ester including alkyl or arylalkyl sulfonyl including methanesulfonyl, benzyl, wherein the phenyl group is optionally substituted with one or more substituents as described in the definition of aryl given above, a lipid, an amino acid, peptide, or cholesterol; andR3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group which when administered in vivo, is capable of being cleaved to the parent compound, or a pharmaceutically acceptable salt thereof.

Novel methods for identification of inhibitors or modulators of binding activities mediated by lectin domains of polypeptide GalNAc-transferases are disclosed. Direct binding activity of GalNAc-transferase lectins has been demonstrated for the first time and methods to measure lectin mediated binding of isolated lectins or enzymes with lectin domains are disclosed. The present invention specifically discloses a novel selective inhibitor of polypeptide GalNAc-transferase lectin domains, which provides a major advancement in that this inhibitor and related inhibitors sharing common characteristics of activity bind lectin domains without serving as acceptor substrate for glycosyltransferases involved in synthesis of O-glycans. This inhibitor is represented by the β-anomeric configuration of GalNAc-benzyl, GalNAcβ-benzyl. Methods for inhibiting intracellular transport, cell surface expression, and secretion of mucins and O-glycosylated glycoproteins without affecting O-glycosylation processing are disclosed using the novel selective inhibitor identified.

The present invention encompasses compounds of Formula (I) as well as the pharmaceutically acceptable salts and hydrates thereof. The compounds are useful for treating immune mediated diseases and conditions, such as bone marrow, organ and tissue transplant rejection. Pharmaceutical compositions and methods of use are included.

The present invention provides a non-radical photo-crosslinked hydrogel preparation method, comprising the following steps: a component A is dissolved in a biocompatible medium to obtain a solution A, component B-hydrazide, hydroxylamine or primary amine high molecular derivative is dissolved in a biocompatible medium to obtain a solution B; the solution A and the solution B are evenly mixed to obtain a hydrogel precursor solution; under illumination, aldehyde group produced by light excitation of o-nitrobenzyl in the component A of the hydrogel precursor solution is crosslinked with hydrazone, hydroxylamine or primary amine group in the component B in the form of respective formation of oxime and Schiff base to produce the hydrogel. The present invention also provides a kit for the hydrogel preparation, and application of the hydrogel in tissue repair, beauty and as a cell, protein or drug carrier. The tissue surface light-situ gel can be achieved by the hydrogel, in particular, wound surface in-situ thin glue formation can be achieved, and the hydrogel is especially suitable for clinical wound surface tissue repair and isolation.

The invention relates to crystalline forms of 1-chloro-4-(β-D-glucopyranos-1-yl)-2-[4-((R)-tetrahydrofuran-3-yloxy)-benzyl]-benzene, to a method for the preparation thereof, as well as to the use thereof for preparing medicaments.

This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1):or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.

The invention relates to a ketoxime ester photoinitiator, in particular to a ketoxime ester photoinitiator for a photo-curing material. The ketoxime ester photoinitiator has a chemical structural formula as the right, wherein in a R1 structure, n is an integer of between 0 and 5; m is an integer of between 1 and 6; R2 is methyl, phenyl, substituted phenyl, benzyl or substituted benzyl; and R3 is diphenyl sulfide group, substituted diphenyl sulfide group, carbazole group or substituted carbazole group. The ketoxime ester photoinitiator solves the problems of poor application performance and poor thermal stability of the prior OXE-1 ketoxime ester photoinitiator.

A novel monomethyl malonate derivative is represented by following Formula (I):wherein X is a halogen atom; and Me is methyl group. This compound can be prepared by the steps of (A) reacting a benzyl halide derivative represented by following Formula (II):wherein X and Y may be the same as or different from each other and are each a halogen atom, with dimethyl malonate in the presence of a base to yield a dimethyl malonate derivative represented by following Formula (III):wherein X and Me have the same meanings as defined above; and (B) hydrolyzing the dimethyl malonate derivative of Formula (III). The compound is useful in the production of an indanonecarboxylic acid ester having a halogen atom on the indanone ring.

The invention relates to an ethylene oligomerization catalyst composition and an application thereof. The composition comprises the following components: a component a contains chromium acetylacetonate, tetrahydrofuran chromium chloride and / or chromium 2-ethylhexanoate; in the formula of a component b, R1, R2, R3 and R4 are phenyl, benzyl or naphthyl; and R5 is isopropyl, butyl, cyclopropyl, cyclopentyl, cyclohexyl or fluorenyl; a component c contains methyl aluminoxane, ethyl aluminoxane, propyl aluminoxane and / or butyl aluminoxane; a component d has a formula X1R6X2, wherein X1 and X2 are F, Cl, Br, I or alkoxy, and R6 is alkyl or aryl; in the formula of a component e, R is a linking group and selected from alkyl and derivatives thereof as well as aryl and derivatives thereof; and the molar ratio is 1: (0.5-10): (50-3000): (0.5-10): (0.5-10). The catalyst has the catalytic activity being more than 5.0*10<6>g mol<-1>Cr.h<-1>, and the mass of 1-hexene and 1-octylene is more than 93%.

The invention discloses a quantitative detecting method for various metabolic components in a biological sample, and a metabolic chip used for the quantitative detecting method. The quantitative detecting method is characterized in that the biological sample is subjected to derivatization treatment, and the biological sample subjected to derivatization is detected through liquid chromatography andmass spectrometry combination; and during derivatization treatment, 3-nitrophenylhydrazine serves as a derivatization reagent, and 1-(3-dimethylaminopropyl)-3-ethly carbodiimide serves as a derivatization reaction catalyst. According to the quantitative detecting method, high-sensitivity detection can be achieved, and a plurality of level-crossing metabolic components can be covered during detection, and the quantitative detecting method is simple, fast and suitable for being applied to clinical and scientific research testing. The metabolic chip comprises a chip carrier microtitration plateand related reagents, and thus the multiple level-crossing metabolites such as amino acid, phenols, phenyl or benzyl derivatives, indole, organic acid, fatty acid, sugar and bile acid in the biological samples can be subjected to quantitative detection on the same microtitration plate.