41 results about "Vicinal" patented technology

Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W, R1 is (CH2)n—CH(OR2)—(CH2)mE1, —(CH)═C(OR2)—(CH2)mE, —(CH2)n—CH(Y)—(CH2)mE or (CH)═C(Y)—(CH2)mE; wherein E is COOR3, C1–C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1–C6 alkyl, haloalkyl and aryl-C0-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or C(S)NR5R6, R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O—, CH2—, —CH2CH2— or CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4–R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2

Disclosed is a compound represented by Structural Formula (I): Ar is a substituted or unsubstituted aromatic group. Q is a covalent bond, —CH2— or —CH2CH2—; W is a substituted or unsubstituted alkylene or a substituted or unsubstituted heteroalkylene linking group from two to ten atoms in length, preferably from two to seven atoms in length. Phenyl Ring A is optionally substituted with up to four substituents in addition to R1 and W, R2 is (CH2)n—CH(OR2)—(CH2)nE, —(CH)═C(OR2)—(CH2)nE, —(CH2)n—CH(Y)—(CH2)mE or (CH)═C(Y)(CH2)mE; wherein E is COOR3, C1-C3 alkylnitrile, carboxamide, sulfonamide, acylsulfonamide or tetrazole and wherein sulfonamide, acylsulfonamide and tetrazole are optionally substituted with one or more substituents independently selected from: C1-C6 alkyl, haloalkyl and aryl-Co-4-alkyl; R2 is H, an aliphatic group, a substituted aliphatic group, haloalkyl, an aromatic group, a substituted aromatic group, —COR4, —COOR4, —CONR5R6, —C(S)R4, —C(S)OR4 or C(S)NR5R6, R3 is H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. Y is O—, CH2—, CH2CH2— or CH═CH— and is bonded to a carbon atom in Phenyl Ring A that is ortho to R1. R4-R6 are independently H, an aliphatic group, a substituted aliphatic group, an aromatic group or a substituted aromatic group. n and m are independently 0, 1 or 2.

The invention provides an application of rubiaceous cyclopeptide RA-V (1) as a Hippo-YAP signal pathway inhibitor, a preparation method of the rubiaceous cyclopeptide and an application of the rubiaceous cyclopeptide to preparation of drugs for treating and preventing YAP abnormal activation related cancers. The rubiaceous cyclopeptide provided by the invention is formed by condensation of peptide bonds of one alpha-D-alanine, one alpha-L-alanine, three substituted N-methyl-alpha-L-tyrosine and one alpha-L-amino acid of other types, and six amino acids are condensed to form an eighteen-membered ring, wherein a benzene ring between two vicinal tyrosines is connected through an oxygen bridge to form a fourteen-membered ring. Compared with the prior art, the preparation method provided by the invention can be used for rapidly separating and purifying the target compound RA-V (1) and has the advantages of high efficiency, strong purposiveness, few separation step, convenience in operation, good controllability and repeatability, recyclable solvent, low cost and suitability for industrial production.

The invention discloses a method for generation of a ketone compound from a vicinal diol compound. The method includes: dissolving the vicinal diol compound in a solvent, and then under the action of the oxidizing agent 1-chloromethyl-4-fluoro-1, 4-diazabicyclo[2.2.2]octane bis(tetrafluoroborate), enabling carbon-carbon bond breakage of the vicinal diol compound to generate the ketone compound. The method provided by the invention has the advantages of no need for adding of a metal chelating agent, low reaction temperature, no by-product formation, high conversion rate, and a product yield of 56%-90%, thus being an environment-friendly method.

A composition and method for imparting a sunless tan to skin is described. The composition and method makes use of a sunless tanning agent like dihydroxyacetone in combination with an adjuvant which is a vicinal diamine.

The invention discloses a vicinal diol functionalized macroporous through-hole material as well as a preparation method and boric acid adsorption application thereof. The preparation method comprisesthe following steps: (1) adding an anionic surfactant into a polyethyleneimine aqueous solution; (2) adding microcrystalline cellulose into the system as a supporting material, and oscillating at a high speed for several minutes to form an air-in-water emulsion; (3) adding a cross-linking agent into the air-in-water emulsion, and oscillating at a high speed for several minutes to partially cross-link polyethyleneimine to cure the emulsion to form a block material; (4) forming a through-hole material through vacuum dehydration, wherein the microcrystalline cellulose can prevent the porous material from overall great shrinkage in the dehydration process, but local microscopic shrinkage still occurs, so that a porous through-hole structure is formed, and the anionic surfactant adsorbed on thesurface of holes is removed through alkaline washing; and (5) converting amino hydrogen on the surface of the porous material into vicinal diol functional groups through glycidyl ether treatment. Thevicinal diol functionalized macroporous through-hole material has the characteristics of simplicity and convenience in preparation, large adsorption capacity, mild regeneration conditions, repeated regeneration and no powder falling.

A compound of formula (II), and a method of preparation thereof, for use as a smooth muscle cell (SMC) proliferation-inhibiting drug:wherein: R1 to R6 are —H, —F, —CH3, —CF3, —CF2CH3, —OCH3, —COCH3, —C4H9, —COOC2H5, or —C6H5, or two vicinal residues from R1 to R6 form a saturated or unsaturated carbocyclic ring together with the two carbon atoms to which they are attached; R7 is OH, allyloxy, propargyl-oxy, 2,2-dimethylpropanoyloxy (pivaloyloxy), butanoyloxy, 3-methylbutanoyloxy, 2-buten-oyloxy, 2-methyl-2-butenoyloxy, 3-methyl-2-butenoyloxy, isopentanoyloxy, 2-ethylbutanoyl-oxy, 3,3-dimethylbutanoyloxy, cyclopropylcarbonyloxy, cyclobutylcarbonyloxy, cyclo-pentylcarbonyloxy, cyclopentenylcarbonyloxy, cyclohexylcarbonyloxy, cyclo-hexenylcarbonyloxy, adamantylethanoyloxy, 3-phenylpropenoyloxy (cinnamyloyloxy), 2-methylbenzoyloxy, or naphthoyloxy; wherein, in ring A and / or B, one or more carbon ring atoms are optionally replaced by heteroatoms; wherein the compounds of formula (II) are obtained by combining the residues R1 to R7 and which inhibit SMC proliferation at least 50% more effectively than EC proliferation.

The invention discloses a composite preservative containing amino acid derivatives. The composite preservative contains the amino acid derivatives, 1,2-vicinal diol and a solvent; the amino acid derivatives are octanoyl amino acid derivatives and / or lauroyl amino acid derivatives. The composite preservative can disturb and inhibit a physiological environment of a cell membrane, namely that the composite preservative is selectively gathered on an oil-water interface in an oil-in-water emulsion system, so that a food source for microorganisms in a region where the composite preservative is gathered is changed to result in being not in favor of growth of the microorganisms, and thereby, the growth of the microorganisms is inhibited; while after the 1,2-vicinal diol is compounded with the octanoyl amino acid derivatives and lauroyl amino acid derivatives dissolved in the solvent, a synergistic effect is generated, so that antisepsis and bacteriostasis effects of octyl chains in the octanoyl amino acid derivatives and lauryl chains in the lauroyl amino acid derivatives can be enhanced to make the composite preservative have a good antisepsis and bacteriostasis effect, and the compositepreservative is very safe and mild to use. The invention further provides a preparation method for the composite preservative and a cosmetic containing the composite preservative.

The invention relates to A 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivative having the general Formula Iwherein R1 is H, (C1-6)alkyl (optionally substituted with oxo, OR4, COOR5, halogen or CN), (C2-6)alkenyl, (C2-6)alkynyl, (C3-6)cycloalkyl or (C3-6)cycloalkyl(C1-3)alkyl; R2 and R2′ are independently H or (C1-3)alkyl; or R2 and R2′ form together with the carbon atom to which they are bound a (C3-5)cycloalkyl group; R3 represents H or 1 to 4 F substituents; Y representsor NR8R9; X represents CHR6, CF2, O, S, SO or SO2; R4 and R5 are (C1-6)alkyl; R6 is H, OR7 or CN; R7 is (C1-3)alkyl; R8 is (C5-7)cycloalkyl comprising a heteroatom selected from O, S, SO and SO2; R9 is H or (C1-4)alkyl; o and m represent the ortho or meta position of the substituent Y—CH2; or a pharmaceutically acceptable salt thereof; as well as to the use of said 1-(biphenyl-4-ylmethyl)imidazolidine-2,4-dione derivatives in the treatment of pain such as for example peri-operative pain, chronic pain, neuropathic pain, cancer pain and pain and spasticity associated with multiple sclerosis.

The invention relates to the food and medical industries, medical cosmetics, dermatology, agriculture and the mixed feed industry. According to the invention vicinal dithioglycole (common formula RCH(SH)CH(SH)R−1 (I)) is used as a food additive, a food product, physiologically-active substances and active ingredients of forage additives and of forage, in cosmetic and / or dermatological and skin-therapeutic remedies. The invention comprises methods for producing such additives, products and remedies. The substance of formula (I) stimulates physiological processes, increases human and animal immunity, inhibits undesirable process in organisms and food products, produces curative and preventive action of skin, hair and nails and after vicinal dithioglycole is administered the intoxication effect of alcohol consumption known as hang-over is completely remored.

A process for the purification of a tetraol PFPE derivative [tetraol (T)] of formula (I): HO—CH2—CH(OH)—CH2—O—CH2—CF2—O—Rf—CF2—CH2O—CH2—CH(OH)—CH2OH, wherein Rf represents a fluoropolyoxyalkene chain (chain Rf), from a mixture (M) of hydroxyl (per)fluoropolyether derivatives, said mixture comprising said tetraol (T) and at least one hydroxyl (per)fluoropolyether [PFPE (OH)] comprising a chain Rf terminated with at least one end group of formula: —CF2CH2OH; —CF2CH2O—CH(OH)—CH2—O—CH2—CH(OH)—CH2OH; said process comprising: step 1: reacting the mixture (M) with ketones and / or aldehydes so as to selectively protect couples of hydroxyl groups on vicinal carbon atoms by forming corresponding cyclic ketal / acetal derivatives, so as to yield a protected mixture (P); step 2: reacting residual hydroxyl groups of the mixture (P) with suitable functionalizing agents enabling substantial volatility modification, so as to obtain a functionalized protected mixture (Pf); step 3: fractional distillation of the mixture (Pf) so as to isolate the cyclic acetal / ketal derivatives of tetraol (T); and step 4: hydrolyzing the acetal / ketal derivatives of tetraol (T) so as to recover pure tetraol (T).

A transfer hydrogenation process for forming vicinal diols by hydrogenating 1,2-dioxygenated organic compounds using alcohols as the reducing agent instead of the traditional H2 gas. The transfer hydrogenation is carried out under milder conditions of temperature and pressure than is typical for ester hydrogenation with H2. The milder conditions of operation provide benefits, such as lower operating and capital costs for industrial scale production as well as savings in product purification due to the avoidance of by-products from exposure of reaction mixtures and products to high temperatures.

The invention relates to a rubber composition based on at least one elastomer, a reinforcing filler, a crosslinking system and at least one polyphenolic compound, said polyphenolic compound comprising at least three aromatic rings, each bearing at least two vicinal hydroxyl groups.

Macrocyclic polyalkene homopolymers and copolymers can be formed and converted to macrocyclic polyalkanes or macrocyclic poly(alkane-co-alkene) upon hydrogenation or, when the macrocyclic polyalkene is reacted with an alkene in the presence of an olefin metathesis catalyst, to a macrocyclic poly(alkane-co-alkene) comprising vicinal -C(=CR2)-'s. Upon hydrogenation of a macrocyclic poly(alkane-co-alkene) comprising vicinal -C(=CR2)- 's, macrocyclic poly(alkane)s or poly(alkane-co-alkene)s with isolated -C(=CR2)- groups can be provided, depending on the degree of hydrogenation. The poly(alkane-co-alkene)s with isolated -C(=CR2)- units can be used to form poly(macrocyclic poly(alkane-co-alkene))s, poly(macrocyclic poly(alkane))s, and / or bi-, tri-, and / or multi-macrocyclic poly(alkane-co- alkene)s or bi-, tri-, and / or multi-macrocyclic poly(alkane)s.

Processes for producing polymer microcapsules using vicinal functional oligomers are also described. The vicinal functional oligomers can be made by polymerizing an acrylate monomer, a styrene monomer, or both in the presence of a chain transfer agent. The vicinal functional oligomers can be reacted with epichlorohydrin to form vicinal epoxies. The vicinal epoxies can be reacted with polyamines to form epoxy polymer microspheres. The vicinal epoxies can be reacted with carbon dioxide in the presence of a catalyst to form vicinal cyclic carbonates. The vicinal cyclic carbonates can be reacted with polyamines to form isocyanate-free polymer microspheres. Polymer microspheres made by the processes are also described.

The present invention relates to novel substituted quinoline derivatives according to the general formula (Ia) or the general formula (Ib) salts, quaternary amines, stereochemically isomeric forms, tautomeric forms and N-oxide forms thereof, wherein R1 is hydrogen, halo, haloalkyl, cyano, hydroxy, Ar, Het, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; p is 1, 2, 3 or 4; R2 is hydrogen, hydroxy, thio, alkyloxy, alkyloxyalkyloxy, alkylthio, mono or di(alkyl)amino or a radical of formula R3 is alkyl, Ar, Ar-alkyl, Het or Het-alkyl; R4 is hydrogen, alkyl or benzyl; R5 is hydrogen, halo, haloalkyl, hydroxy, Ar, alkyl, alkyloxy, alkylthio, alkyloxyalkyl, alkylthioalkyl, Ar-alkyl or di(Ar)alkyl; or two vicinal R5 radicals may be taken together to form together with the phenyl ring to which they are attached a naphthyl; r is 1, 2, 3, 4 or 5; R6 is hydrogen, alkyl, Ar or Het; R7 is hydrogen or alkyl; R8 is oxo; or R7 and R8 taken together form the radical CH═CH—N═; Z is CH2 or C(═O). The claimed compounds are useful for the treatment of mycobacterial diseases, particularly those diseases caused by pathogenic mycobacteria such as M. tuberculosis, M. bovis, M. avium, M. smegmatis and M. marinum. Also claimed is a pharmaceutical composition containing a compound of the present invention, the use of the claimed compounds or compositions for the manufacture of a medicament for the treatment of mycobacterial diseases and a process for preparing the claimed compounds.

The invention relates to a synthetic method of an ocean terpene natural product austrodoral, austordoric acid and a land terpene natural product 8-epi-11-nordriman-9-one and belongs to the field of chemical synthesis. Sesquiterpenes vicinal diol is prepared by selective ozonization reaction of sesquiterpenes enol, the land terpene natural product 8-epi-11-nordriman-9-one and the ocean terpene natural product austrodoral are synthesized by the selective rearrangement reaction of the sesquiterpenes vicinal diol, and the ocean terpene natural product austrodoric acid is synthesized by oxidation reaction of the austrodoral. The method has the characteristics of low production cost, simple process conditions, easiness in control, suitability for industrial production, high overall yield and the like.

The invention discloses a synthesis method of biphenyl derivatives. According to the method, transition metal palladium is taken as a catalyst, aromatic carboxylic acid is subjected to a carboxyl-vicinal crossed dehydrogenate coupling and decarboxylic reaction, and a series of biphenyl derivatives are synthesized in one step simply, conveniently and efficiently. The synthesis method has the advantages that raw materials are simple and easy to obtain, operation is simple, environment-friendliness is realized and the like.

The invention relates to a method for synthesizing 1,2-o-diol compounds. The synthesis method comprises the following steps: (1) using a terminal olefin as a raw material, potassium hydrogen persulfate compound salt as an oxidizing agent, an inorganic salt as a catalyst, mixing water and a ketone organic solvent as a reaction solvent, and reacting at 30-100° C.; (2) After the reaction, add an inorganic base at 0-40°C to make the pH of the reaction system 10-14; (3) continue the reaction at 30-100°C, after the reaction, separate and purify to obtain 1,2-o-diol class of compounds. The synthesis method has mild reaction system, cheap and easy-to-obtain raw materials, environment-friendly oxidant, good reaction selectivity and high conversion rate.

A process for epitaxying GaSe on a [111]-oriented silicon substrate, includes a step of selecting a [111]-oriented silicon substrate resulting from cutting a silicon bar in a miscut direction which is one of the three [11-2] crystallographic directions, the miscut angle (α) being smaller than or equal to 0.1°, the obtained surface of the substrate forming a vicinal surface exhibiting a plurality of terraces and at least one step between two terraces; a passivation step consisting of depositing an atomic bilayer of gallium and of selenium on the vicinal surface of the silicon substrate so as to form a passivated vicinal surface made of silicon-gallium-selenium (Si—Ga—Se), said passivated vicinal surface exhibiting a plurality of passivated terraces and at least one passivated step between two passivated terraces; a step of forming a layer of two-dimensional GaSe by epitaxy on the passivated surface, said formation step comprising a step of nucleation from each passivated step and a step of lateral growth on the passivated terraces from the nuclei obtained in the nucleation step. A structure obtained by means of the epitaxying process is also provided.

The present invention relates to a gene encoding a protein having a vicinal diketone or diacetyl-reducing activity and use thereof, in particular, a brewery yeast for producing alcoholic beverages with superior flavor, alcoholic beverages produced with said yeast, and a method for producing said beverages. More particularly, the present invention relates to a yeast, whose capability of producing vicinal diketones, especially diacetyl, that are responsible for off-flavors in products, is reduced by amplifying expression level of MMF1 gene encoding a protein (Mmflp) having a vicinal diketone or diacetyl-reducing activity, especially the non-ScMMF1 gene or ScMMF1 gene specific to a lager brewing yeast, and to a method for producing alcoholic beverages with said yeast.

The present invention relates to the treatment of cachexia in a mammal by the use of a compound comprising a high density negatively charged domain of vicinally oriented radicals.

Urea-functional organopolysiloxanes containing units of the formulaRnSiO(4-n) / 2  (I),where R is a radical R1 or a radical —OR2 or a radical Q, Q is a urea-functional radical of the formula—R5—[NR4—R6—]xNR4R3  (II),where the radicals R4 are identical or different and are each a radical R4′ or a radical Ru, where R4′ is hydrogen or a monovalent C1-C6-hydrocarbon radical where Ru is radical of the formula —C(═O)—NH2, and where at least one urea-functional radical Q having a radical Ru is present per molecule are prepared by reacting amino-functional organopolysiloxanes comprising units of the formulaR′nSiO(4-n) / 2  (IV),where A is an amino-functional radical of the formula—R5—[NR4′—R6—]xNR4′R3  (V),with the proviso that at least one amino-functional radical A is present per molecule in the organopolysiloxanes made up of units of the formula (III),with ortho-substituted aryl carbamates of the formulaR7—Ar—O—C(═O)—NH2  (VI),where Ar is an ortho-substituted aryl radical.