62 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 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 relates to methods of treating tuberculosis, including multidrug 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 (T), (S)—N-[[3-[3-fluoro-4-(4-thiomor-pholinyl)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.

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.

A method for repelling arthropods involving treating an object or area with an arthropod repelling effective amount of at least one compound having the formulawherein X is O, S, NH, N-NH2, N-CH3 or CH2, R′ is H or alkyl, R″ is alkyl, n is 0, 1, 2, 3 or 4, and mixtures thereof, optionally including a carrier material or carrier. The compound is preferably selected from homopiperazine, 1-methylhomopiperazine, 1-methylpyrrolidine, (R)-(−)-2-methylpiperazine, (S)-(+)-2-methylpiperazine, 2-methylpiperazine, 1-methylpiperazine, pyrrolidine, 1-methylpiperidine, piperidine, 1-ethylpiperazine, 1-methylimidazolidine, 1-methylthiomorpholine, 1,4-dimethylpiperazine, homopiperidine, imidazolidine, 4-methylpiperidine, thiomorpholine, 1-amino-4-methylpiperazine, 4-methylmorpholine, azocane, 2,6-dimethylpiperazine, 2,5-dimethylpiperazine, piperazine, 1-methlyhomopiperidine, or mixtures thereof.

The invention discloses a 1-aryl-3-substituent-5-substituted amino-4-pyrazole formamide compound and application thereof. The 1-aryl-3-substituent-5-substituted amino-4-pyrazole formamide compound has a general structural formula described in the specification, wherein R1 and R2 can be hydrogen, benzyl or alkyl independently, or can form the following groups comprising imidazolidinyl, 2-imidazolidinyl, 3-imidazolidinyl, pyrryl, 2H-pyrryl, 2-pyrrolinyl, pyrrolidyl, triazolyl, pyrazolyl, piperazinyl, pyridazinyl, pyrazinyl, triazinyl, morpholinyl and thio-morpholinyl, together with N connected with R1 and R2; R1 and R2 can be the same or different; R3 can be any one of H, CF3, Br, NO2, CH3 and OCH3; and R4 can be hydrogen, halogen, cyan, hydroxy, alkyl halide, alkoxy, alkoxy alkyl, alkyl sulphanyl or alkyl sulphanyl alkyl. The pharmacological activity result of the compound shows that the compound has an excellent restraining effect on tumor cell lines.

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 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 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.

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 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.

The invention discloses synthesis and application of indole-2, 3-dinitrile antineoplastic compounds containing fatty amino groups, and a preparation method of the indole-2, 3-dinitrile antineoplastic compounds comprises the following steps: taking aniline as a raw material to generate 2-(hydroxyethylamine)-N-phenylacetamide with chloral hydrate and hydroxylamine hydrochloride, cyclizing and hydrolyzing under an acidic condition to obtain isatin, taking ethanol as a solvent, adding glacial acetic acid and 2, 3-dinitrile according to a catalytic amount, and reacting at the temperature of 60-80 DEG C to obtain the fatty amino group-containing indole-2, 3-dinitrile antineoplastic compounds. According to the present invention, isatin is subjected to a reaction with 2, 3-diamino-maleic dinitrile to expand the conjugated structure of isatin, and finally the isatin is subjected to a reaction with different aliphatic amines to obtain different indole-2, 3-dinitrile antitumor compounds, and the aliphatic amines comprise dimethylamino, morpholinyl, thiomorpholinyl, diethylamino, N-methyl piperazinyl, pyrrolidinyl, piperidyl, pyrrolyl, imidazolyl and piperazinyl. The indole-2, 3-dinitrile anti-tumor compound containing fatty amino can be embedded into a DNA base pair to enhance the interaction between a drug molecule and a target, and an in-vitro anti-tumor test proves that the indole-2, 3-dinitrile anti-tumor compound has good tumor inhibition capability and biological safety, namely, the indole-2, 3-dinitrile anti-tumor compound has almost no toxicity to normal immune cells of mice.