289 results about "Thiazolidine" patented technology

The invention discloses certain N-(substituted glycyl)-4-cyanothiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

The invention discloses certain N-(substituted glycyl)-thiazolidines, pharmaceutical compositions containing said compounds as an active ingredient thereof, and the use of said compounds in inhibiting dipeptidyl peptidase-IV.

A combination of one or more HMG-CoA reductase inhibitors (for example pravastatin, lovastatin, simvastatin, fluvastatin, rivastatin or atorvastatin) with one or more insulin sensitizers (for example troglitazone, pioglitazone, englitazone, BRL-49653, 5-(4-{2-[1-(4-2'-pyridylphenyl)ethylideneaminooxy]ethoxy}benzyl)thiazolidine-2,4-dione, 5-{4-(5-methoxy-3-methylimidazo[5,4-b]pyridin-2-ylmethoxy)benzyl}thiazolidine-2,4-dione or its hydrochloride, 5-[4-(6-methoxy-1-methylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione, 5-[4-(1-methylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione and 5-[4-(5-hydroxy-1,4,6,7-tetramethylbenzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione) exhibits a synergistic effect and is significantly better at preventing and / or treating arteriosclerosis and / or xanthoma than is either of the components of the combination alone.

Abstract of Disclosure The invention relates to compounds for topically influencing the activity of dipeptidyl peptidase of the general formula wherein A is an amino acid having at least one functional group in the side chain;B is a chemical compound covalently bound to a functional group of the side chain of A, chosen from the group consisting of (a) oligopeptides having a chain length of up to 20 amino acids, (b) homopolymers of glycine consisting of up to 6 glycine monomers, and (c) polyethylene glycols having molar masses of up to 20 000 g / mol; and C is a group amide-bonded to A chosen from the group consisting of thiazolidine, pyrrolidine, cyanopyrrolidine, hydroxyproline, dehydroproline or piperidine. The invention further relates to the use of said compounds for targeted intervention in local immunological processes (chemotaxis, inflammatory processes, autoimmune diseases), as well as effective and targeted treatment of pathophysiological and physiological processes related thereto (psoriasis, periodontitis, arthritis, allergies, inflammation), inter alia.

The present invention relates to compositions useful in treating hyperpigmentation and the various signs of dermatological aging in human skin. The present invention also relates to cosmetic compositions and methods of using such compositions that improve the aesthetic appearance of skin. Further, the present invention relates to methods of applying the compositions to the skin to effect treatment and to improve the aesthetic appearance of skin, particularly, by providing anti-aging benefits to the skin. These and other objects of the present invention are achieved by a method and composition that comprises (a) a de-pigmenting agent or anti-aging agent in an amount effective to prevent, treat and / or ameliorate pigmentation or the various signs of aging at an area of skin to which it is applied, and (b) a cosmetically or pharmaceutically acceptable vehicle. Suitable de-pigmenting agents include 3,3'-thiodipropionic acid, thiazolidine-2-carboxylic acid, Kaempferol-7-glucoside, perilla oil, and clofibrate and clofibrate analogs and / or derivatives, as well as those set forth below. Suitable anti-aging agents include 3,3'-thiodipropionic acid and / or its derivatives.

The invention relates to pharmaceutical compositions containing at least one thiazolidin-4-one derivative to prevent or treat disorders associated with an activated immune system. Furthermore, the invention relates to novel thiazolidin-4- one derivatives notably for use as pharmaceutically active compounds. Said compounds particularly act also as immunosuppressive agents.

Process for the hydrolytic ring cleavage of thiazolidine derivatives to give 2-aminomercaptan derivatives and carbonyl compounds, which comprisesbringing an aqueous solution of the thiazolidine derivative into contact with an acidic cation exchanger in the H+ form, giving a solution L1 which contains the carbonyl compound andeluting the cation exchanger with a suitable eluent, giving a solution L2 which contains the 2-aminomercaptan derivative.

The present invention provides 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H -pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine (compound I) useful as a dipeptidyl peptidase-IV inhibitor, which has superior properties of stability and hygroscopicity, and reproducible crystal structure, and a production method thereof.

The invention provides α-amino esters of a hydroxypropylthiazolidine carboxamide derivative, (2S)-3-([1,1′-biphenyl]-4-ylsulfonyl)-N-[(1S)-3-hydroxy-1-phenylpropyl]-1,3-thiazolidine-2-carboxamide, as well as salts and crystal polymorphs thereof, that can be used to inhibit prostaglandin F receptor. The invention further encompasses methods of treating disorders such as pre-term labor at the early gestational stage by the administration of these substances to a patient in need of treatment.

The invention relates to a preparation method of an ultra-thin double-sided photoelectronic copper foil and the prepared copper foil. The method comprises the following steps of: adding alkylphenol polyoxyethylene ether sodium sulfonate, 1,3-thiazolidine-2-one and collagen in deionized water and dissolving to obtain an additive solution for ultra-thin copper foil production; under the condition of a copper sulphate electrolyte at a temperature of 20-90 DEG C, adding 5.0-10.0L of the additive solution in per cubic metre of the electrolyte per hour, uniformly stirring and then enabling the electrolyte to enter an electrolytic bath; and electrolysing the electrolyte in the electrolytic bath under an electrolytic current density of 2000-6000A / m<2>, and carrying out an electrochemical reaction to generate the ultra-thin double-sided photoelectronic copper foil. The ultra-thin double-sided photoelectronic copper foil manufactured by the process disclosed by the invention has the following performance: the thickness is small and uniform, the roughness of a rough surface is moderate and uniform, the two sides of the copper foil are smooth and bright, the surface tension of the copper foil is high, the adhesion force of lithium-ion negative electrode active materials can be effectively increased, the electric capacity and charge-discharge times of a battery are increased, and the service life of the battery is prolonged.

A therapeutic method is provided comprising treating a mammal subject to hypoxia with an amount of 2(R,S)-D-ribo-(1′,2′,3′,4′-tetrahydroxybutyl)thiazolidine-4(R)-carboxylic acid (RibCys) or a pharmaceutically acceptable salt thereof effective to both maintain, restore or increase both the ATP levels and the glutathione (GSH) levels in said tissue.

A modified ion exchange resin catalyst having an attached dimethyl thiazolidine promoter is disclosed. Also disclosed is a process for catalyzing condensation reactions between phenols and ketones, wherein reactants are contacted with a modified ion exchange resin catalyst having an attached dimethyl thiazolidine promoter. Also disclosed is a process for catalyzing condensation reactions between phenols and ketones that does not utilize a bulk promoter.

A method for the production of natural L-cysteine by fermentation in a production fermenter in which a microorganism strain is cultured in a fermentation medium, characterized in that the fraction of the compounds L-cysteine, L-cystine and thiazolidine in the fermentation medium is controlled in a targeted manner by an iron concentration of a maximum of 8 mg / l in the fermentation medium.

The invention relates to novel heterocyclic compounds having the structure illustrated by Formula (I) wherein the Ar1 radicals are substituted dihydronapthalene or isochroman radicals, the Ar2 radicals are aryl or heteroaryl radicals; and HAr is a 2,4-thiazolidinedione, 2-thioxo-thiazolidine-4-one, 2,4-imidazolidinedione or 2-thioxo-imidazolidine-4-one radical. The compounds of Formula (I) can have biological activity for advantageously regulating carbohydrate metabolism, including serum glucose level, and lipid metabolism, and can be useful for the treatment of hyperlipidemia and / or hypercholesterolemia, and Type II diabetes. The compounds of Formula (I) can also have utility in the treatment of diseases of uncontrolled proliferation, including cancer.

Aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are sodium channel blockers; pharmaceutical compositions that include an effective amount of the aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds and a pharmaceutically acceptable carrier, and a method of treatment of acute pain, chronic pain, visceral pain, inflammatory pain, or neuropathic pain, as well as initable bowel syndrome, Cnohns disease, epilepsy, partial and generalized tonic seizures, multiple sclerosis, bipolar depression, and tachy-arrhythmias by the administration of an effective amount of aryl-link-aryl thiazolidine-dione and aryl-link-aryl oxazolidine-dione compounds are described.

Substituted thiazolidinone carboxylic acid amides and substituted thiazolidine carboxylic acid amides according to formulae (I) and (II) are disclosed where the various substituent groups are as defined in the specification. Methods of making these compounds, pharmaceutical compositions containing the compounds, and their use, particularly for treating or preventing cancer, are also disclosed.

The invention discloses a process for the preparation of a pyridine derivative namely 5-{4-2(N-methyl-N(2-pyridyl)amino ethoxy]benzyl]thiazolidine-2,4-dione maleate comprising the steps of:(a) reacting 2-chloropyridine with 2-(N-methyl amino)ethanol;(b) coupling 2-(N-methyl-N-(2-pyridyl) amino)ethanol) obtained in step (a) and 4-fluorobenzaldehyde in an aprotic polar solvent with an alkali metal hydroxide or an alkali metal alkoxide as base.(c) isolating the product of the coupling reaction viz 4-[2-(N-methyl-N-(2-pyridyl) amino) ethoxy]benzaldehyde;(d) converting said isolated benzaldehyde compound of step (c) into 5-[4-[2-N-methyl-N-(2-pyridyl) amino)ethoxy]benzyl]thiazolidine-2,4-dione in a known manner and(e) converting said thiazolidine-2,4-dione compound obtained in step (d) into a pharmaceutically acceptable maleate salt.

The invention provides a method for preparing taurine and substituted taurine, which takes 1, 3-thiazolidine-2-thioketone and derivants thereof as raw material to prepare taurine and substituted taurine. The method has the advantages that the raw material can be obtained easily, the operation is convenient, the purification through desalination is not needed, and the method is particularly suitable for large-scale industrialized production and can be utilized to prepare optically active substituted taurine. The obtained compound can be used as nutritive matters, medicines, enzyme inhibitors, antimicrobials, surface active agents, plant growth regulators, raw material for preparing sulfono-peptides, etc.

A method for treating pulmonary hypertension and other diseases involving a defect in collagen metabolism, by administration of an effective amount of a liposome encapsulated copolymer conjugate antifibrotic composition, is disclosed. The antifibrotic agent is preferably proline analogs, such as cis-4-hydroxy-L-proline (CHOP), 3,4-dehydro-DL-proline (DHP), (R)-(-)-2-thiazolidine-4-carboxylic acid (THP), and (S)-(-)-2-azetidinecarboxylic acid (ACA). Consistent, high loadings (>90%) of the antifibrotic agent are achieved by first forming a dipeptide with L-lysine, after which the dipeptide is copolymerized with the polymer component to form the copolymer conjugate. The polymer is preferably poly(ethylene glycol) having a weight average molecular weight of from about 500 to about 15,000. Efficient delivery and consistent release of the antifibrotic agent inhibits collagen accumulation and treats the diseases involved. Accordingly, there is a substantial reduction in the quantity of antifibrotic agent necessary, and thus a corresponding reduction in the potential for toxicity that would otherwise result from its prolonged administration.

A concomitant agent to be used simultaneously or separately, comprising a combination of (a) 3-{(2S,4S)-4-[4-(3-methyl-1-phenyl-1H-pyrazol-5-yl)piperazin-1-yl]pyrrolidin-2-ylcarbonyl}thiazolidine, a salt of the compound with an organic or inorganic and mono- or di-basic acid or a solvate thereof, and(b) at least one kind of active ingredient selected from the group consisting of an active ingredient of a pharmaceutical agent selected from (i) an antidiabetic drug, (ii) a lipid lowering drug, (iii) an antihypertensive drug, (iv) a therapeutic drug for diabetic complications, (v) an antiobesity drug, (vi) an antiplatelet drug and (vii) an anticoagulant, a pharmaceutically acceptable salt thereof and a solvate thereof.

The benzylidene-1,3-thiazolidine-2,4-dione compounds having the structural formula (I), or salt and / or solvate and / or isomer thereof: are useful active agents for inducing and / or stimulating the growth of mammalian keratin fibers and / or reducing the loss and / or increasing the density thereof, particularly of human head hair, beard hair, moustache hair, eyelashes and eyebrows, and advantageously are active agents for caring for or making up the hair or the eyelashes.

There is provided a topical composition for treating, preventing or ameliorating hyperpigmentation in human skin. The composition has a de-pigmenting agent in an amount effect to reduce or diminish pigmentation at an area of skin to which it is applied, and a cosmetically or pharmaceutically acceptable vehicle. Suitable de-pigmenting agents include 3,3'-thiodipropionic acid, thiazolidine-2-carboxylic acid, kaempferol-7-glucoside, perilla oil, and clofibrate and clofibrate analogs and derivatives. There is also provided methods for treating, preventing or ameliorating hyperpigmentation in human skin.

A N-oxyl carbon-2-thiazolidone derivative and its production are disclosed. The production is carried out by: 2- thiazolidone derivative condensing reacting with chloro-formate under action of acid catching agent in 0-10deg.C organic solvent, after-processing and obtaining products. It achieves higher sterilizing activity.

The present invention relates to a novel method of obtaining a factor involved in appetite control and / or body weight control, as well as genes obtained by said method, polypeptides encoded by said genes, or novel polypeptides obtained from the information on polypeptides encoded by said genes as a means for treating, controlling or diagnosing diseases associated with eating disorders and / or body weight control. Also the present invention relates to substances that inhibit the effects of said genes or said polypeptides as a means for treating, controlling or diagnosing diseases associated with appetite control and / or body weight control. By using thiazolidine diones having a PPAR γ agonist activity, genes and polypeptides involved in appetite regulation and / or body weight reduction can be obtained. NESFATIN or the like obtained by said method can be used as a means for treating, controlling or diagnosing diseases associated with eating disorders and / or body weight control.

The invention discloses a chiral zinc complex secondary structure hollow microsphere. The chemical formula of the microsphere is shown as ([ZnL(H2O)].0.5H2O) infinite, wherein L is 2,4-thiazolidine diacid anion; a zinc complex belongs to a tetragonal system, has a three-dimensional network structure and is formed by assembling ZnNO5 modules; the coordination geometric configuration of zinc ions is a deformed octahedron; and adjacent zinc ions are bridged through carboxyl to constitute a three-dimensional metal organic frame structure. In the preparation method, zinc acetate and H2L are taken as raw materials, water is taken as a solvent, PVP (Polyvinyl Pyrrolidone) is taken as a surfactant and acetone is taken as a precipitant. The invention has the advantages that: the chiral zinc complex secondary structure hollow microsphere represents stronger negative Cotton effect and larger specific surface area and has wide application prospect as a novel functional material; the preparation method is easy to operate and has low cost; the obtained product has a regular shape and high stability; and a new measure is explored for the introduction of a novel material.

The invention provides a nitrogen heterocyclic ring substituted aryl propenone compound (formula I), a preparation method and application thereof. The structural formula of the compound is shown in the formula I, wherein in the formula I, R in X (shown as formula on the right) is H, F, Cl, Br, CH3O, C2H5O, 2, 4-dichloro, NO2 and CH3; and in the formula I, Y is 2-nitroiminoimidazolidine, 2-cyanoimino-1, 3-thiazolidine, thiazolidine and other nitrogen heterocyclic rings. The compound has excellent chemical killing activity to aphid, tetranychus cinnabarinus, diamondback moth and other harmful pests, and biological activity of partial compound is equivalent to that of control insecticides. Furthermore, compared with effective constituents of natural Stellera chamaejasma L, the compound has the advantages that the compound has simple structure and easy acquisition, and can be actually applied to agricultural production.