68 results about "Propionic acid derivatives" patented technology

A pharmaceutical dosage form comprising non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, along with a second active ingredient having a shorter therapeutically effective plasma concentration duration, such as phenylephrine, and methods of administering the same are provided. This method provides improved therapeutic effect, in particular pain relief along with decongestant relief, over extended time periods.

The present invention relates to the manufacture of the compounds of formula (I) said compounds of formula (I) being valuable intermediates in the manufacture of Dolastatin 10 analogues, which are useful in the treatment of cancer.

A method of administering non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, or acetaminophen via a liquid suspension is provided. This method provides improved therapeutic effect, in particular pain relief, over extended time periods.

The present invention aims at provision of a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, an agent for the prophylaxis or treatment of diabetes and the like. The compound represented by the formula: wherein each symbol is as defined in the description, a salt thereof, and a prodrug thereof of the present invention unexpectedly have a superior GPR40 receptor agonistic activity and superior properties as pharmaceutical products such as stability and the like, and can be safe and useful pharmaceutical agents as agents for the prophylaxis or treatment of GPR40 receptor-related pathology or diseases in mammals.

The present invention relates to stable emulsifiable concentrates comprising an oil adjuvant and at least one member selected from the group consisting of herbicidally active 2-[4[(5-chloro-3-fluoropyridin-2-yloxy)-phenoxy]-propionic acid derivatives and quinoline derivative safeners and to the use thereof as a pesticide.

Methods of treating adverse intestinal effects of a non-steroidal anti-inflammatory drugs (NSAID) in a subject by administering to the subject a therapeutically effective amount of a selective bacterial beta-glucuronidase inhibitor. The adverse intestinal effects to be treated include the formation or growth of an intestinal ulcer, increased intestinal permeability, the loss of intestinal villi, bleeding of the intestinal mucosa, and an increased intestinal inflammatory response. The methods are useful for treating the adverse effects of any NSAID such as propionic acid derivatives, carboxylic acid derivatives, enolic acid derivatives, fenamic acid derivatives, sulphonanilidies, and selective COX-2 inhibitors. The bacterial beta-glucuronidase inhibitors are selective for the inhibition of bacterial beta-glucuronidase enzymes and do not inhibit mammalian beta-glucuronidase.

Fumaric acid is added in amounts sufficient to reduce the burn sensation commonly associated with propionic acid derivatives.

A method of administering non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, or acetaminophen via a liquid suspension is provided. This method provides improved therapeutic effect, in particular pain relief, over extended time periods.

The invention discloses an aryl propionic acid derivative composition and a pharmaceutical purpose. Alcohol metabolites of Loxoprofen having highest activity in metabolism is used as a nuclear parent to produce a series of derivatives of phosphate, sulphonate, carbonic ester, and amino-acid ester. The derivatives are used to enhance pesticide effect of anti-inflammatory and analgesic effects, and reduce toxic reaction, and have good pharmacokinetic property. And at the same time, the stimulation of the medicine on the gastrointestinal tract, and medication compliance of patients is improved, and therefore the aryl propionic acid derivative composition is the non-steroidal anti-inflammatory drugs having potentials.

A compound represented by the following formula (1) or a salt thereof: wherein R1 represents a C1-12 alkyl group, phenyl group, 1-naphthyl group and the like, R2 represents a C2-12 alkyl group, (R3)b represents 0 to 4 substituents such as a halogen atom, R4 represents a lower alkyl group, R5 represents hydrogen atom or a lower alkyl group, n represents an integer from 2 to 4, and X represents —NH— or —O—, which has superior hypoglycemic action, hypolipidemic action and total cholesterol reducing action, and is useful as an active ingredient of a medicament for prophylactic and / or therapeutic treatment of diseases including diabetes mellitus, hyperlipidemia and the like.

The invention belongs to the technical field of fine chemical catalysis synthesis, and more specifically relates to a preparation method of a spiro indolone compound in a water phase. According to themethod, an indolone-derived compound containing active hydrogen functional groups or a 3-indole propionic acid derivative is used as a raw material, a quaternary ammonium iodide salt is used as a catalyst and a surfactant, a peroxide is used as an oxidizing agent, and reacting is performed in the water phase to obtain the spiro indolone compound. According to the method provided by the invention,any organic solvent can be completely avoided during reaction, and the method is green and environment-friendly, high in yield, mild in condition, simple and convenient to operate, good in reaction medium cycle performance and the like.

The present invention relates to compounds of formula I: wherein R1, R2, R3, R4, R5 and R6 are as defined in the specification and claims, which compounds are active on the GABAB receptor and are useful in the control or prevention of CNS illnesses, especially of illnesses and disorders comprising anxiety, depression, epilepsy, schizophrenia, and cognitive disorders.

The present invention provides a pharmaceutical formulation suitable for filling softgel capsules comprising: (a) a therapeutically effective amount of a non-steroidal anti-inflammatory drug selected from the group consisting of selected from the group consisting of (1) the propionic acid derivatives; (2) the acetic acid derivatives; (3) the fenamic acid derivatives; (4) the biphenylcarboxylic acid derivatives; and (5) the oxicams; as well as Cox 2 inhibitors and mixtures thereof; and (b) a solvent system comprising 40% to 60% by weight a polyoxyethylene ether of the formula: wherein n=1 to 6; 15% to 35% by weight of glycerin and 15% to 35% by weight water. In the case of compositions containing an NSAID having carboxyl function an alkaline hydroxide may be added to neutralize said hydroxide function.

The present invention disclosed compounds of Structural Formula (I), and enantiomer, racemic body, pharmaceutically acceptable salts, solvates or hydrates thereof, wherein variable groups are as defined within, as well as methods for preparing such compounds. The compounds are useful as PPARγ agonist, through activating PPAR-RXR heterodimers that intereacts with specific DNA response elements within promoter regions of target gene, particularly in the treatment and prevention of polycystic kidney and cancer.

The invention provides an application of a 3-[[2-[3-oxo-(1, 2-benzisoxazole-6-yl) methoxyl]-5-[(2-hydroxyl-4-cyclopentoxyl benzoyl)] phenyl] propionic acid (compound I) in preparation for treatment of connexin CX31 mediated skin disease. The connexin CX31 mediated skin disease comprises erythrokeratodermia variabilis or psoriasis. The pharmacological experiment proves that a low-dose group and a high-dose group of the compound I can remarkably reduce skin damage degree of a psoriasis animal sample; the content of TNF-alpha in murine serum can be restrained by the low-dose group of the compound I, then inflammatory cell infiltration is restrained, the inflammatory response is relieved, and the compound I has good psoriasis treatment effect and can be used for treating the connexin CX31 mediated skin disease.

The present invention provides a method for the synthesis of optically pure α-aryl propionic acid derivatives comprising subjecting the corresponding racemic α-aryl propionic acid derivatives to high sheer or impact forces, such as grinding.

A pharmaceutical dosage form comprising non-steroidal-anti-inflammatory drugs, in particular propionic acid derivatives such as ibuprofen, along with a second active ingredient having a shorter therapeutically effective plasma concentration duration, such as phenylephrine, and methods of administering the same are provided. This method provides improved therapeutic effect, in particular pain relief along with decongestant relief, over extended time periods.

The present invention is concerned with a novel process for the preparation of compounds of formula I comprising catalytic asymmetric hydrogenation of a compound of formula (II) in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and / or esters are pharmaceutically active substances.

The invention provides novel salts of (S)-2-methoxy-3-[4-{3-(4-methanesulfonyloxyphenyl)propylamino} phenyl] propionic acid, including Arginine salt of (S)-2-methoxy-3-[4-{3-(4-methanesulfonyloxyphenyl)propylamino} phenyl] propionic acid monohydrate, Arginine salt of (S)-2-methoxy-3-[4-{3-(4-methanesulfonyloxyphenyl) propylamino} phenyl] propionic acid, and (S)-2-methoxy-3-[4-{3-(4-methanesulfonyloxyphenyl)propylamino} phenyl] propionic acid monohydrate. Various aspects and embodiments are included. Compositions containing novel salts of (S)-2-methoxy-3-[4-{3-(4-methanesulfonyloxyphenyl) propylamino}phenyl] propionic acid are also provided.

The present invention is concerned with a novel process for the preparation of compounds of formula Icomprising catalytic asymmetric hydrogenation of a compound of formula (II)in the presence of a catalyst comprising ruthenium and a chiral diphosphine ligand or comprising rhodium and a chiral diphosphine ligand, wherein R1, R2, R3 and R4 are as defined in the specification and claims. The compounds of formula I and the corresponding salts and / or esters are pharmaceutically active substances.

The present invention relates to stable emulsifiable concentrates comprising an oil adjuvant and at least one member selected from the group consisting of herbicidally active 2-[4[(5-chloro-3-fluoropyridin-2-yloxy)-phenoxy]-propionic acid derivatives and quinoline derivative safeners and to the use thereof as a pesticide.

The present invention relates to 2-(substituted sulphur, sulphone or sulphoxide)-3-(substituted phenyl) propionic acid derivatives, 2-(substituted oxygen)-3-(substituted phenyl) propionic acid derivatives, benzoic acid derivatives, and derivatives of 2-methyl-2-(phenoxy or phenylthio)propanoic acid and 2-(methylor ethyl)-2-(phenoxy or phenylthio)butanoic acid, to processes for preparing such compounds, to their use in the treatment of inflammatory conditions, and to pharmaceutical compositions containing them.

The invention relates to a preparation method of an aryl propionic acid derivative, comprising the following step of: making a compound expressed by a formula II react according to the following route so as to prepare the aryl propionic acid derivative expressed by a formula I, wherein R1, R2, R3, R4 and R5 independently express hydrogen, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, halogen, trihalogenated methyl and nitryl; R7 and R8 independently express an ester group and a cyano group; R6 expresses carboxyl or a cyano group; X expresses fluorine, chlorine, bromine or iodine; when R7 and R8 both express the ester group or the cyano group, R6 expresses the carboxyl; and when R7 expresses the ester group and R8 expresses the cyano group, R6 expresses the cyano group. The preparation method of the aryl propionic acid derivative has the advantages that raw materials are easy to obtain and low in price, oxidation and reduction reaction are not needed, the route is simple, the reaction condition is moderate, the production equipment requirement is low, a small quantity of the three wastes is discharged and industrialized production can be realized easily, thereby the preparation method can be widely used for synthesizing medicaments, daily chemicals, and the like.

The invention belongs to the field of medicinal chemistry, and relates to a preparation method of a bilastine intermediate 2-(4-(2-hydroxyethyl) phenyl)-2-methyl propionic acid and derivatives thereof. The 2-(4-(2-hydroxyethyl) phenyl)-2-methyl propionic acid and the derivative thereof are obtained by taking a 4-halogenated phenyl-2-methyl propionic acid derivative as a raw material through the steps of alkylation, hydrolysis, reduction and the like, and the compound can be used for synthesizing bilastine.