64 results about "Thiomorpholine" patented technology

A polishing slurry containing a slurry dispersing particles of tetravalent metal hydroxide in a medium therein and an additive, characterized in that the additive is a polymer containing at least one kind of monomer component selected from a group of monomers represented with a general formulae (I) and (II) below (In the general formulae (I) and (II), R1 denotes hydrogen, a methyl group, a phenyl group, a benzil group, a chlorine group, a difluoromethyl group, a trifluoromethyl group or a cyano group, R2 and R3 denote hydrogen or an alkyl chain having 1 to 18 carbon atoms, a methylol group, an acetyl group or a diacetonyl group, and a case where both are hydrogen is not included. R4 denotes a morpholino group, a thiomorpholino group, a pyrrolidinyl group or a piperidino group.) The invention provides a polishing slurry in which particles form a chemical reaction layer with a polishing film to be removed with a very small mechanical action of the particles and mechanical removal by a pad without scratches and the additive realizes high planarity.

The present invention relates to methods of treating tuberculosis, including multi-drug resistant varieties and latent tuberculosis. More particularly, the present invention relates to a method of treating tuberculosis in a mammal comprising administering to said mammal in need thereof an effective amount of a compound of formula (I), (S)—N-[[3-[3-fluoro-4-(4-thiomorpholinyl)phenyl]-2-oxo-5-oxazolidinyl]methyl]acetamide, or a pharmaceutically acceptable salt thereof in combination with at least two agents useful in the treatment of tuberculosis. The present invention also relates to a pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof, (ii) a therapeutically effective amount of at least one agent useful in the treatment of tuberculosis and (iii) one or more pharmaceutically acceptable carriers or vehicles.

The present invention provides compositions comprising lanthionine ketimine derivatives and thiomorpholine dicarboxylic acid derivatives, as well as processes for the preparation of such compounds. The invention also concerns the use of lanthionine, lanthionine ketimine (LK), LK derivatives, thiomorpholine dicarboxylic acid (TMDCA), and TMDCA derivatives. It concerns the use of these compounds for the treatment and / or prevention diseases, including diseases affecting the central nervous system. The invention provides for compounds and methods having anti-oxidant, anti-neuroinflammatory and neuroprotective activities. It also provides for compounds having the ability to pass through and / or be transported through cellular membranes, such the blood-brain barrier.

The present invention provides compositions comprising lanthionine ketimine derivatives and thiomorpholine dicarboxylic acid derivatives, as well as processes for the preparation of such compounds. The invention also concerns the use of lanthionine, lanthionine ketimine (LK), LK derivatives, thiomorpholine dicarboxylic acid (TMDCA), and TMDCA derivatives. It concerns the use of these compounds for the treatment and / or prevention diseases, including diseases affecting the central nervous system. The invention provides for compounds and methods having anti-oxidant, anti-neuroinflammatory and neuroprotective activities. It also provides for compounds having the ability to pass through and / or be transported through cellular membranes, such the blood-brain barrier.

The invention relates to sulfomorpholine compounds, a preparation method thereof and a purpose thereof, and concretely relates to compounds of formula (I), or pharmaceutically acceptable salts thereof, free alkalis thereof, solvates thereof, esters thereof, prodrugs thereof, stereo isomers thereof, geometric isomers thereof and racemates thereof, wherein symbols in the formula (I) are shown in the specification. The invention also relates to a medicinal composition containing the compounds, a purpose of the compounds in the preparation of medicines for treating and / or preventing diseases or symptoms related with DPP-IV (dipeptidyl peptidase IV) hyperactivity or DPP-IV overexpression, and a method for treating relevant diseases with the compounds of the invention. The compounds of the invention can effectively inhibit the DPP-IV activity.

A novel one-stage process for preparing 10α-[4′-(S,S-dioxothiomorpholin-1′-yl)]-10-deoxo-10-dihydroartemisinin (1a) by reacting a compound of the formula (1b) in which X is a halogen atom with thiomorpholine dioxide at a temperature in the range of −30° C. to +20° C. is provided.

The invention relates to N-benzylbenzamide compounds represented by formula (I), a preparation method and a medicinal use thereof, and an anti-tuberculosis medicinal composition adopting the compounds as an effective component. The N-benzylbenzamide compounds are concretely characterized in that a substituent group in the para-position of a benzyl group of the N-benzylbenzamide compounds is a nitrogen-containing heterocyclic segment; and in the formula (I), R represents a trifluoromethyl group or a nitro group, and X represents a 4-thiomorpholinyl group, an octahydro-2H-isoindole-2-yl group, an isoindoline-2-yl group, a 4-substituted piperidine-1-yl group, a (4-substituted phenyl)piperidine-1-yl group or a (4-substituted phenyl)piperazine-1-yl group.

The present invention relates to new medical use of (tetrahydropyran-4-yl)-[2-phenyl-5-(1,1-dioxo-thiomorpholine-4-yl)methyl-1H-indol-7-yl]amine, and more particularly, to a pharmaceutical composition containing the compound as an active ingredient, which is used for inhibiting an immune response, and / or for inducing differentiation into regulator T cells from undifferentiated T cells and / or promoting proliferation of regulator T cells.

The invention relates to substituted piperidine, piperazine, morpholine and thiomorpholine compounds useful in the treatment of Alzheimer's disease and more specifically to compounds that are capable of inhibiting beta-secretase, an enzyme that cleaves amyloid precursor protein to produce amyloid beta peptide (A-beta), a major component of the amyloid plaques found in the brains of Alzheimer's sufferers. One embodiment of the invention relates to compounds having the structure:where Z is CR or N, and R1, R2 and R3 are as described in the specification.

The invention provides a preparing method of Filgotinib. The preparing method comprises the following steps that (1), 2-amino-6-bromopyridine reacts with a p-methylbenzene derivative to prepare a compound 1; (2), the compound 1 reacts with ethoxycarbonyl isothiocyanate to prepare a compound 2; (3), the compound 2 reacts with hydroxylamine hydrochloride and N,N-diisopropylethylamine to prepare a compound 3; (4), the compound 3 reacts with cyclopropanecarbonyl chloride to obtain a compound 4; (5), the compound 4 reacts with N-bromosuccinimide and azodiisobutyronitrile to obtain a compound 5; (6), the compound 5 reacts with thiomorpholine-1,1-dioxide to obtain the Filgotinib. According to the synthesis route of the Filgotinib, firstly, coupling is conducted, then ring closing is conducted, the raw materials are cheap, the reaction operation is simple, and the product is easy to purify, high in yield and suitable for large-scale commercial production.

The present invention relates to new medical use of (tetrahydropyran-4-yl)-[2-phenyl-5-(1,1-dioxo-thiomorpholine-4-yl)methyl-1H-indol-7-yl]amine, and more particularly, to a pharmaceutical composition containing the compound as an active ingredient, which is used for inhibiting an immune response, and / or for inducing differentiation into regulator T cells from undifferentiated T cells and / or promoting proliferation of regulator T cells.

The invention discloses a method for synthesizing impurity enantiomers of bupropion hydrochloride, and belongs to the field of pharmaceutical and chemical engineering. The method includes carrying out mercapto protection, condensation and de-protection cyclization consecutive reaction on D-cysteine methyl ester hydrochloride (a compound I) which is used as a starting material; separating and hydrolyzing isomers by means of column chromatography to obtain (3S, 5S, 6S)-6-(3-chlorphenyl)-6-hydroxyl-5-methyl thiomorpholine-3-carboxylic acid and (3S, 5R, 6R)-6-(3-chlorphenyl)-6-hydroxyl-5-methyl thiomorpholine-3-carboxylic acid. The method has the advantages of concise and efficient synthetic route, stereospecific chiral control, high reaction yield and inexpensive and easily available materials, solvents and reagents. Besides, the impurity enantiomers can be used for controlling the quality of bupropion hydrochloride sustained-release tablets or can be used as impurity reference substances.

Peptides which exhibit high selectivity for the kappa opioid receptor (KOR) and long duration of peripheral action without significant entry into the brain are created which are sequences of four D-isomer amino acid residues having a C-terminus which is a mono- or di-substituted amide. Representative compounds, which have an affinity for the KOR at least 1,000 times their affinity for the mu opioid receptor and an ED50 of not greater than about 0.5 mg / kg, include H-D-Phe-D-Phe-D-Nle-D-Arg-NHEt, H-D-Phe-D-Phe-D-Nle-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NHPr, H-D-Phe-D-Phe-D-Nle-D-Arg-thiomorpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NEt2, H-D-Phe-D-Phe-D-Nle-D-Arg-NHMe, H-D-Phe-D-Phe-D-Leu-D-Orn-morpholinyl, H-D-4Fpa-D-Phe-D-Nle-D-Arg-NH-4-picolyl, H-D-Phe-D-Phe-D-Nle-D-Arg-NH-cyclopropyl, H-D-Ala-(2Thi)-D-3, 4Cpa-D-Leu-D-Arg-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Gmf-morpholinyl, H-D-Phe-D-Phe-D-Leu-D-Orn-NH(Aeb), H-D-Phe-D-Phe-D-Leu-D-Lys-morpholinyl, H-D-Phe-D-Phe-D-Nle-D-Arg-piperazinyl, and H-D-Phe-D-Phe-D-Nle-D-Arg-NH(Hoh).

A novel one-stage process for preparing 10α-[4′-(S,S-dioxothiomorpholin-1′-yl)]-10-deoxo-10-dihydroartemisinin (1a) by reacting a compound of the formula (1b)in which X is a halogen atom with thiomorpholine dioxide at a temperature in the range of −30° C. to +20° C. is provided.

The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof, and their use.

The invention belongs to the technical field of antiplatelet drugs and provides thiomorpholine-containing pyrrole derivatives and pharmaceutically acceptable salts thereof. The thiomorpholine-containing pyrrole derivatives have a general structural formula I. In the general structural formula I, m and R are defined in the patent specification. The invention relates to a preparation method of the thiomorpholine-containing pyrrole derivatives, discloses a drug composition containing the thiomorpholine-containing pyrrole derivatives or their pharmaceutically acceptable salts as active ingredients, and also discloses a use of the thiomorpholine-containing pyrrole derivatives and their pharmaceutically acceptable salts in antiplatelet drugs.

The invention discloses a preparation method of filgotinib. The preparation method provided by the invention comprises the following steps: in a mixed solvent of an alcohol solvent and water, in the presence of a palladium catalyst and alkali, enabling a compound A (N-(5-bromo-[1, 2, 4] triazolo [1, 5-a] pyridine-2-yl) cyclopropyl formamide) and a compound B (4-[4-(4, 4, 5, 5-tetramethyl [1, 3, 2] dioxaborolan-2-yl) benzyl] thiomorpholine-1, 1-dioxide) to react. The preparation method has the advantages of environmental friendliness, low cost, simplicity and convenience in operation, high product purity, low impurity content, facilitation of industrialization and the like.

Metabolites of a matrix metalloproteinase inhibitor prinomastat and their synthesis. These metabolites are: (3S)-N-hydroxy-4-(4-((1-oxy-pyrid-4-yl)oxy)benzenesulfonyl)-2,2-dimethyl-tetrahydro-2H-1,4-thiazine-3-carboxamide (M6); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(1-oxy-pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M7); (3S)-2,2-dimethyl-4-[4-(1-oxypyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M8); (3S)-2,2-dimethyl-1,1-dioxo-4-[4-(pyridin-4-yloxy)-benzenesulfonyl]-thiomorpholine-3-carboxylic acid amide (M2); and (3S)-2,2-dimethyl-4-[4-(pyridin-4yloxy)-benzenesulfonyl)-thiomorphpline-3-carboxylic acid amide (M3).

The present invention is relates to a compound of formula (I),whereinX1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1, X2 and X3 are N;Y is N or CH;W is H or F; with the proviso that when W is F, then X1, X2 and X3 are N;R1 and R2 are independently of each other(i) a morpholinyl of formula (II)wherein the arrow denotes the bond in formula (I); andwherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structureswherein the arrows denote the bonds in formula (II); or(ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue —R8R9— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2— or —O—CH2CH2—O—;with the proviso that at least one of R1 and R2 is a morpholinyl of formula II;and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in the prevention or treatment of a skin lesion in a subject.

The present invention relates to a compound of formula (I), wherein X1, X2 and X3 are, independently of each other, N or CH; with the proviso that at least two of X1X2 and X3 are N; Y is N or CH; W is H or F; with the proviso that when W is F, then Xi, X2 and X3 are N; R1 and R2 are independently of each other (i) a morpholinyl of formula (II) wherein the arrow denotes the bond in formula (I); and wherein R3 and R4 are independently of each other H, C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxy, C1-C2alkoxyC1-C3alkyl, CN, or C(O)O—C1-C2alkyl; or R3 and R4 form together a bivalent residue —R5R6— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2—, —CH2—NH—CH2—, or any of the structures wherein the arrows denote the bonds in formula (II); or (ii) a saturated 6-membered heterocyclic ring Z selected from thiomorpholinyl and piperazinyl, optionally substituted by 1 to 3 R7; wherein R7 is independently at each occurrence C1-C3alkyl optionally substituted with one or two OH, C1-C2fluoroalkyl, C1-C2alkoxyC1-C3alkyl, C3-C6cycloalkyl; or two R7 substituents form together a bivalent residue —R8R9— selected from C1-C3alkylene optionally substituted with 1 to 4 F, —CH2—O—CH2— or —O—CH2CH2—O—; with the proviso that at least one of R1 and R2 is a morpholinyl of formula II; and prodrugs, metabolites, tautomers, solvates and pharmaceutically acceptable salts thereof, for use in a method of treating a skin disorder in a subject, wherein said skin disorder is a genodermatosis, a vascular anomaly or a skin disorder selected from scleroderma, sclerodermatous chronic graft-versus-host disease, lichen sclerosus, lichen planus, lichen ruber planus and scars.

The invention relates to an efficient and green preparation method of artemisinin sulfone. The preparation method is characterized by comprising two reaction steps: step 1, reacting dihydroartemisinin with thiomorpholine to generate dihydroartemisinin-thiomorpholine at a certain temperature in the presence of a certain solvent and catalyst; and step 2, oxidizing dihydroartemisinin-thiomorpholine to generate artemisinin sulfone at a certain temperature in the presence of an oxidant hydrogen peroxide, a catalyst metallic compound and a certain ketones solvent. The method has the main characteristics that in the reaction of step 2, oxidization of dihydroartemisinin-thiomorpholine can be realized by only adopting a series of low-price and environment-friendly raw materials such as hydrogen peroxide and the like without using expensive rare metal catalysts, transition metal oxidants or organic peroxides. The method has the characteristics of high oxidation rate, good selectivity, mild reaction conditions, simple and convenient experiment operations; besides the raw materials are low in price, easy to obtain, clean and environmentally friendly; the method has great application prospect.

An object of the present invention is to provide a rubber composition having excellent processability, a heterocycle-modified glycerin fatty acid ester, and a production method for the heterocycle-modified glycerin fatty acid ester. The present invention includes: a rubber composition containing a rubber, silica, and a heterocycle-modified glycerin fatty acid ester, in which an epoxy group is modified with a heterocyclic compound having a heterocycle having at least one H—N< bond, where the heterocycle is at least one selected from the group consisting of a piperazine ring, a morpholine ring, and a thiomorpholine ring, and the heterocycle may have a substituent; the heterocycle-modified glycerin fatty acid ester; and a production method therefor.

The present invention provides a rubber composition for a tire, the rubber composition containing: a diene rubber; silica; and a heterocyclic compound (where, the heterocyclic compound does not have a silicon atom) having a hydrocarbon group having from 3 to 30 carbons and at least one type of heterocycle selected from the group consisting of a piperazine ring, a morpholine ring, and a thiomorpholine ring; an average glass transition temperature of the diene rubber being −50° C. or higher; a content of the silica being from 80 to 200 parts by mass per 100 parts by mass of the diene rubber; and a content of the heterocyclic compound being from 0.5 to 20% by mass with respect to the content of the silica. Such rubber composition has excellent processability, exhibits excellent wet grip performance and has low rolling resistance when the rubber composition is formed into a tire.

The invention discloses an electrolyte, a positive electrode, a lithium ion battery and a vehicle. The electrolyte comprises a lithium salt, an organic solvent and an additive, the additive comprises a first additive, the first additive is an alkyl thiomorpholine ring compound, the structural formula of the alkyl thiomorpholine ring compound is as follows: R is selected from at least one of C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C10 cycloalkyl, C6-C30 aryl, C3-C10 thiazinyl and C4-C10 thienyl; hydrogen atoms in C1-C10 alkyl groups, C2-C10 alkenyl groups, C2-C10 alkynyl groups, C3-C10 cycloalkyl groups, C6-C30 aryl groups, C3-C10 thiazinyl groups and C4-C10 thienyl groups can be partially or completely substituted by substituent groups. The additive of the electrolyte has more substituent groups and complexing sites, is high in reduction potential, is favorable for forming an interface protection film on a negative electrode, and meanwhile, complexes metal ions dissolved out from a positive electrode, so that the cycling stability of the battery under high voltage is improved.

The invention discloses a 4-substituted pyrrolidine formyl thiomorpholine DPP-IV (Dipeptidyl Peptidase IV) inhibitor and a preparation method therefor and use thereof. Specifically, the invention relates to a compound represented by a formula (I) shown in the description, a stereoisomer thereof and pharmaceutically-acceptable salts thereof, wherein R1 and R2 are as defined in the description. The invention also relates to a pharmaceutical composition containing the compound disclosed by the invention, use of the compound disclosed by the invention in preparation of drugs for methods for treating and / or preventing too-high DPP-IV activity or DPP-IV overexpression related diseases or disease symptoms, and a method for treating related diseases by using the compound disclosed by the invention. The compound disclosed by the invention has effective DPP-IV inhibiting activity.