82 results about "Thioester synthesis" patented technology

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphonic acid, phosphinic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, sp2 amine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, s-heterocyclic ring, thiophene, n-heterocyclic ring, pyrrole, o-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention / treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention / treatment of colon cancer.

The invention provides a composition having laser engraving properties, comprising a host material and an effective amount of a laser enhancing additive. The laser enhancing additive comprises a first quantity of least one of copper potassium iodide (CuKI3) or Copper Iodide (CuI), and a second quantity at least one substance selected from the group consisting of zinc sulfide (ZnS), barium sulfide (BaS), alkyl sulfonate, and thioester. The composition can be engraved with grayscale images by an Nd:Yag laser and can be added to laminates or coatings. The composition can be used during the manufacture of many articles of manufacture, including identification documents.

An in vivo method for labelling a protein having an N-terminal cysteine is disclosed. A probe comprising a thioester group and a detectable label is introduced into a cell expressing the N-terminal cysteine protein, allowing for the N-terminal cysteine to cleave the thioester bond and resulting in the label being covalently attached to the N-terminus of the protein by an amide bond.

A pharmaceutical composition comprising a co-crystal of an API and a co-crystal former; wherein the API has at least one functional group selected from ether, thioether, alcohol, thiol, aldehyde, ketone, thioketone, nitrate ester, phosphate ester, thiophosphate ester, ester, thioester, sulfate ester, carboxylic acid, phosphinic acid, phosphonic acid, sulfonic acid, amide, primary amine, secondary amine, ammonia, tertiary amine, imine, thiocyanate, cyanamide, oxime, nitrile diazo, organohalide, nitro, S-heterocyclic ring, thiophene, N-heterocyclic ring, pyrrole, 0-heterocyclic ring, furan, epoxide, peroxide, hydroxamic acid, imidazole, pyridine and the co-crystal former has at least one functional group selected from amine, amide, pyridine, imidazole, indole, pyrrolidine, carbonyl, carboxyl, hydroxyl, phenol, sulfone, sulfonyl, mercapto and methyl thio, such that the API and co-crystal former are capable of co-crystallizing from a solution phase under crystallization conditions.

The present invention provides new derivatives of 4- or 5-aminosalicylic acid, and a pharmaceutical composition containing these derivatives of 4- or 5-aminosalicylic acid as active ingredients, useful for the treatment of intestinal diseases such as inflammatory bowel disease (IBD) and irritable bowel syndrome (IBS) and for the prevention / treatment of colon cancer. More particularly, these derivatives comprise a hydrogen sulfide releasing moiety linked via an azo, an ester, an anhydride, a thioester or an amide linkage to a molecule of 4- or 5-aminosalicylic acid. Furthermore, the present invention provides a process for preparing these compounds and their use for treating IBD and IBS and the prevention / treatment of colon cancer.

A composition comprising:(a) polyethylene;(b) as a scorch inhibitor, [1,3,5-tris(4-tert-butyl-3-hydroxy-2,6-dimethylbenzyl)-1,3,5-triazine-2,4,6-(1H,3H,5H)-trione];(c) a thioester;(d) a hindered amine stabilizer; and(e) an organic peroxide.

The invention provides a composition having laser engraving properties, comprising a host material and an effective amount of a laser enhancing additive. The laser enhancing additive comprises a first quantity of least one of copper potassium iodide (CuKI3) or Copper Iodide (CuI), and a second quantity at least one substance selected from the group consisting of zinc sulfide (ZnS), barium sulfide (BaS), alkyl sulfonate, and thioester. The composition can be engraved with grayscale images by an Nd:Yag laser and can be added to laminates or coatings. The composition can be used during the manufacture of many articles of manufacture, including identification documents.

The invention at hand describes a method for the cyclization of peptides and proteins in which linear thioesters serve as substrates. The cyclization is catalyzed by thioesterase domains of NRPS or PKS cyclases. The substrates according to the present invention are composed of one linear peptide on which a charge-stabilized aromatic, heteroaromatic or araliphatic leaving group is bound. These substrates lead to higher yields and reaction rates than linear peptides able to be cyclized with methods known so far and, furthermore, allow the cyclization of such peptides which were previously not able to be cyclized.

A thermoplastic resin molding composition comprising an alkylene aryl polyester, a core-shell impact modifier for enhancing heat resistance having a shell derived from an alkylacrylate and a rubbery acrylate core derived from an acrylate having 4 to 12 carbon atoms, an effective amount of a difunctional epoxy compound for enhancing hydrolysis resistance of the resin, and a combination of color enhancing stabilizers comprising a thioester stabilizer, a phosphite or phosphonite stabilizer and a hindered phenol stabilizer.

A coating comprising a polymer that comprises units derived from an aliphatic thioester on a medical device is provided.

the invention provides a composition having laser engraving properties, comprising a host material and a laser enhancing additive. The host material comprises a material, such as a polymer, modified by a first process, whereby the host material as modified by the first process has increased thermal conductivity as compared to the host material before the first process. The laser enhancing additive comprises a first quantity of at least one of copper potassium iodide (CuKI3), Copper Iodide (CuI), potassium iodide (KI), sodium iodide (NaI), and aluminum iodide (AlI), and a second quantity of at least one substance selected from the group consisting of zinc sulfide (ZnS), barium sulfide (BaS), alkyl sulfonate, and thioester.

Disclosed is method for controlling undesired vegetation of subfamily Mimosoideae comprising applying to the undesired vegetation or its environment a herbicidally effective amount of a mixture comprising (a) one or more compounds selected from the compound of Formula 1 and salts, esters and thioesters thereof:; and(b) at least one additional herbicide selected from the group consisting of(b1) fosamine and salts thereof;(b2) imazapyr and salts thereof;(b3) metsulfuron-methyl and salts thereof; and(b4) triclopyr and esters, thioesters and salts thereof.

A protein preparation method provided by the invention comprises the following steps to connect a first peptide with hydrazide group on C terminus and a second peptide with cysteine on N terminus: mixing the first peptide and the second peptide in a solution containing NaNO2 and adjusting the mixed solution pH to an acidic pH so as to converting the hydrazide group of the first peptide into acyl azide group to obtain a first reaction mixture; adding a solution containing a reducing agent into the first reaction mixture and adjusting the pH to a neutral pH, wherein the reducing agent contains mercapto group, so as to convert the acyl azide group of the first peptide into thioester group, and maintaining the neutral pH so as to conducting a connection reaction between the thioester on the Cterminus of the first peptide and the N terminus of the second peptide to produce proteins. A method for preparing polypeptide thioester compounds is also provided. According to the protein preparation method provided by the invention, proteins can be effectively synthesized.

A method for the ligation of expressed proteins which utilizes inteins, for example the RIR1 intein from Methanobacterium thermotrophicum , is provided. Constructs of the Mth RIR1 intein in which either the C-terminal asparagine or N-terminal cysteine of the intein are replaced with alanine enable the facile isolation of a protein with a specified N-terminal, for example, cysteine for use in the fusion of two or more expressed proteins. The method involves the steps of generating a C-terminal thioester-tagged target protein and a second target protein having a specified N-terminal via inteins, such as the modified Mth RIR1 intein, and ligating these proteins. A similar method for producing a cyclic or polymerized protein is provided. Modified inteins engineered to cleave at their C-terminus or N-terminus, respectively, and DNA and plasmids encoding these modified inteins are also provided.

The present invention provides methods of assembling oligopeptides or polypeptides in a native chemical ligation reaction that eliminates the formation of unwanted side products resulting from the presence of an unprotecte acidic C-terminal oligopeptide thioester. An important aspect of the present invention is providing side chain protected acidic C-terminal oligopeptide thioesters. The present invention is useful in methods for chemical synthesis of oligopeptides, polypeptides and proteins and improves the efficiency of native chemical ligation reactions, particularly where aspartyl or glutamyl peptide fragments are used to assemble an oligopeptide, polypeptide or protein product

The invention relates to a composition including at least one elastomer and at least one supramolecular polymer. The supramolecular polymer is obtained by the reaction of at least one trifunctional compound (A), having first and second functions, with: at least one compound (B) having at least one reactive group capable of reacting with the first functions of (A) and at least one associative group; and at least one at least bifunctional compound (C) having functions capable of reacting with the second functions of compound (A) in order to form ester, thioester and amide bridges.

The present invention provides novel compounds and pharmaceutical compositions for the prevention and / or treatment of cancer and precancerous conditions thereof, for the treatment of pain and fever, for the treatment of skin disorders, and for treating and / or preventing inflammation-related diseases and / or cardiovascular diseases. The compounds of the invention also have analgesic properties and anti-platelet properties. The compounds of the invention may be provided to animals, including mammals and humans, by administering a suitable pharmaceutical dose in a suitable pharmaceutical dosage form. The compounds of the invention have improved efficacy and safety, including higher potency and / or fewer or less severe side effects, than conventional therapies. The compounds of the invention comprise a biologically active moiety or portion (A) that has, or is modified to have at least one carboxyl group. The moiety A is preferably an aliphatic, aromatic or alkylaryl group, preferably derived from a non-steroidal anti-inflammatory drug or NSAID (A). The moiety A is bound to a linker moiety (B) via the carboxyl of group A and a linking atom that is selected from oxygen, nitrogen, and sulphur, to form a carboxylic ester, and amide, or a thioester, bond (X1) between groups A and B. Moiety B is a single bond, an aliphatic group, a substituted benzene, or an alkylene substituted hydrocarbon chain, which in turn is bound to functional moiety Z, which facilitates access of the compound into cells. The moiety Z can comprise, for example, a phosphorous-containing group, a nitrogen-containing group, or a folic acid residue.

Disclosed herein is a process for enzymatically resolving a mixture of R- and S-enantiomers of an α-substituted carboxylic acid or an ester or thioester thereof, in which a Carica papaya lipase is used as a biocatalyst to effect the resolution as desired.

Methods and compositions are provided for covalently linking a chemical species to a recombinant or synthetic polypeptide. The methods involve the reaction of a thioester-comprising polypeptide with a reagent comprising a reactive amino-thiol group connected to the chemical species which is to be covalently linked to the polypeptide, via a linker. Such chemical species can be a functional group, a label or tag molecule, a biological molecule, a ligand, or a solid support. Efficient and catalyst-free methods for C-terminal protein labeling are also provided. The methods expand current capabilities in the area of protein functionalization, providing useful and complementary tools for the isolation, detection, characterization, and analysis of proteins in a variety of in vitro and in vivo applications.

The present invention provides a cyclic peptide comprising the structure: wherein X is selected from the group consisting of an amino acid, an amino acid analog, a peptidomimetic and a non-amide isostere, Z is selected from the group consisting of a synthetic amino acid and a biosynthetic amino acid, R is selected from the group consisting of oxygen, nitrogen, sulfur and carbon, n is 0 to 10 and y is 1 to 10. The present invention also provides a cyclic peptide comprising the amino acid sequence of NH2—X(n)-Z-X(y)—COOH and a cyclic bond between the Z residue and COOH other than a thioester bond, wherein X is selected from the group consisting of an amino acid, an amino acid analog, a peptidomimetic and a non-amide isostere, Z is selected from the group consisting of a synthetic amino acid and a biosynthetic amino acid, n is 0 to 10 and y is 1 to 10. Methods of preparation including a cyclization protocol, and methods of use of the cyclic peptides of the invention are also disclosed.

The invention discloses rhodamine B intra-thioester, a preparation method and application thereof. The rhodamine B thioester has a structural formula as formula I. The method prepares intra-thioester compounds of a first rhodamine dye, an intra-thioester ring of the compounds can be selectively cut off by mercury ions, and the method improves the selectivity and sensitivity of the reaction compared with the prior reagent. Through introducing an active intra-thioester ring group on the rhodamine B, the method realizes optical response to the mercury ions, can realize quantitative detection for trace mercury ions with high sensitivity and high selectivity, and has huge application prospect in the fields such as quality, environment and biology.

An object of the present invention is to provide a method for synthesizing a peptide thioester by using a compound that can be easily obtained within a relatively short time under conditions in which a side reaction is unlikely to occur. In the present invention, a thioester bond is formed by elongating a peptide chain using N-alkyl cysteine as the C-terminal amino acid according to the Fmoc method, carrying out deprotection, and then causing the peptide bond to undergo N—S transfer to the thiol group of N-alkyl cysteine under weak acidic conditions.

The present invention provides a catalyst component for ethylene polymerization, wherein magnesium halide is dissolved in an alcohol compound and an organic epoxy compound to form a uniform solution, and the obtained uniform solution acts with a titanium compound in the presence of a thioester compound so as to obtain the catalyst component. According to the present invention, the catalyst provides characteristics of high polymerization activity, good hydrogen response, good copolymerization performance, and good bulk density when the catalyst is used for ethylene polymerization at a high temperature; the thioester compound is added so as to improve the particle morphology of the catalyst, and improve the hydrogen response and the copolymerization performance of the catalyst; and the use of a lot of titanium tetrachloride to promote precipitate precipitation and the multiple uses of titanium tetrachloride to treat the precipitate are not required, such that the addition amount of titanium tetrachloride is substantially reduced so as to improve the production efficiency and the production benefits of the catalyst.

A high-resilience spandex slice mainly comprises 20-60 parts of aliphatic linear non-branched polyester dihydric alcohol with the molecular weight 2000-3000, wherein the repeating unit contains more than 11 carbon atoms; 15-45 parts of polyether polyol with the molecular weight 1000-2000; 20-40 parts of diisocyanate, 5-15 parts of a chain extender, wherein the chain extender is dihydric alcohol with the molecular weight of 80-400; 0.1-1.0 part of an antioxidant, wherein the antioxidant is at least two kinds of antioxidants including hindered phenolic antioxidant, hindered amine antioxidant, thioester antioxidant and phosphite antioxidant; 0.1-1.0 part of a lubricant, wherein the lubricant at least two kinds of lubricants including stearates type lubricants, stearamide type lubricants, montan wax type lubricants, stearates type lubricants, oleamide type lubricants and cyclic butylene terephthalate type lubricants. The high-resilience spandex slice also comprises an organic tin catalyst, wherein the weight of the organic tin catalyst accounts for 0.01-0.1% of the total weight of the other raw materials. According to the invention, the molecular weight and the variety of the molecular weight of the polyether polyol are controlled, the types of the chain extender are controlled, the aggregative state of the spandex slice is adjusted to control the rebound resilience of the spandexslice to be more than 40%, dry-spinning spandex yarns are replaced and the high-resilience spandex slice is used for the special field with relatively high rebound resilience requirements.

The invention relates to a preparation method of a modified polylactic acid material for 3D printing, having a metal effect. The method concretely comprises the following steps: preparing the following raw materials, by weight, 100 parts of polylactic acid, 80-150 parts of metal powder, 1-5 parts of a metal pigment, 8-18 parts of a soft-core and hard-shell type core-shell copolymer flexibilizer with methyl methacrylate as the shell, 0.5-2 parts of a coupling agent, 0.5-1.5 parts of a lubricant, 0.2-0.8 part of a hindered phenol antioxidant and 0.1-0.5 part of a phosphite or thioester antioxidant, mixing the metal powder with the metal pigment, spraying a coupling agent solution during mixing, drying the obtained material, mixing the obtained modified metal powder and metal pigment, the polylactic acid, the flexibilizer, the lubricant and the antioxidant, adding the obtained mixture into a double screw extruder, performing extruding granulation, drying obtained pellets, adding the driedpellets into a single screw extruder, extruding the pellets, and performing hot water treatment, cold water treatment and air drying to obtain wires. The modified polylactic acid material prepared inthe invention has the advantages of metal effect, good toughness and non-degradability.