35 results about "Propanoic Acid Derivatives" patented technology

The present invention provides a novel compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof having a superior GPR40 receptor function modulating action, which can be used as an insulin secretagogue, an agent for the prophylaxis or treatment of diabetes and the like. They unexpectedly show superior GPR40 receptor agonist activity, and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful pharmaceutical agents for the prophylaxis or treatment of GPR40 receptor related diseases in mammals.

The invention belongs to the field of medicament synthesis, and relates to Danshensu derivatives with a structure in the following formula, a synthesis method thereof, and application thereof in pharmacy. The synthesis method adopts a chiral synthesis method to synthesize the Danshensu derivatives with stable structures in high yield, in particular derivatives of dextrorotatory Danshensu with high optical purity. Through experiments of animal models with hypoxic myocardial cells, results show that the Danshensu derivatives can reduce LDH leakage of the hypoxic myocardial cells, improve the activity of hyperoxide dismutase in the cells, inhibit generation of a product of lipid peroxidation, promote the expression of anti-apoptotic gene bcl-2 mRNA and inhibit the expression of pro-apoptosisgene bax mRNA and apoptotic gene caspase-3mRNA; and the results prove that the Danshensu derivatives have an effect of protecting hypoxic cardiac muscle and can be used for preparing medicaments for treating ischemic heart disease.

The present disclosure provides a process for synthesis of 3-aryl-2-hydroxy propanoic acid derivatives of formula (S)-1. wherein R1 represents H or (C1-C5) alkyl groups and R2 represents (C1-C5) alkyl groups.

A compound of formula (I) or a salt thereof are provided:wherein R1, X and R3 are defined in the specification, useful in the treatment of disorders mediated by KMO such as acute pancreatitis, chronic kidney disease, other conditions associated with systemic inflammatory response syndrome (SIRS), Huntington's disease, Alzheimer's disease, spinocerebellar ataxias, Parkinson's disease, AIDS-dementia complex, amylotrophic lateral sclerosis (ALS), depression, schizophrenia, sepsis, cardiovascular shock, severe trauma, acute lung injury, acute respiratory distress syndrome, acute cholecystitis, severe burns, pneumonia, extensive surgical procedures, ischemic bowel, severe acute hepatic disease, severe acute hepatic encephalopathy or acute renal failure.

Process for the preparation of 2-phenyl-2-methyl propanoic acid derivatives, useful as intermediates in the preparation of fexofenadine hydrochloride.

The present invention relates to a kind of amphiphilic derivative of 3-((2-(dimethylamino) ethyl) (methyl) amino) propionic acid and its use; Prepared liposome; the use is the use of liposome as a drug carrier delivery system. The liposome prepared from the amphiphilic compound of the present invention can carry more positive charges at acidic pH, can better compound gene drug siRNA, and form a complex with smaller particle size and uniform particle size distribution. At the same time, it is electrically neutral under the pH7.4 environment, which increases the stability of the lipoplex in vivo and reduces the cytotoxicity caused by excessive positive charges. The liposome provided by the invention can specifically inhibit gene expression in human non-small cell lung cancer H1299‑Pgl3 cells in vitro, and can specifically transfer fluorescent gene drugs into normal mouse liver cells in vivo.

Novel homo-aza-steroidal esters with alkylating bis(2-chloroethyl)aminophenoxy propanoic acid and substituted derivatives, processes for their preparation, pharmaceutical compositions containing them and use thereof in the treatment of cancer.

The present invention provides a process for preparing 3-amino-2-hydroxypropionic acid derivatives (1) which does not use dangerous reagents, is economically advantageous, and is suitable for an industrial production, which process comprises: treating N-protected-3-amino-2-hydroxypropionic acid derivatives (2) having a steric configuration at 2-position carbon reverse to that of derivatives (1) with a leaving group-introducing agent to convert into N-protected-3-aminopropionic acid derivatives (3), then treating the derivatives with a basic substance to convert into substituted-3-amino-2-hydroxypropionic acid derivatives (4) having an inverted steric configuration at 2-position carbon, and then converting the derivatives into 3-amino-2-hydroxypropionic acid derivatives (1).

The problem to be solved by the present invention is to provide a compound suitable for a pharmaceutical composition, specifically a pharmaceutically composition for treating nocturia.The inventors have assumed that inhibition of nocturnal activity of placental leucine aminopeptidase (P-LAP), i.e. aminopeptidase that cleaves AVP, would maintain and / or increase an endogenous AVP level to enhance the antidiuretic effect, which would contribute to a decreased number of nocturnal voids, and have extensively studied compounds which inhibit P-LAP. As a result, the inventors have found that (2R)-3-amino-2-(bi-cyclic pyridylmethyl)-2-hydroxy-propanoic acid derivatives have excellent P-LAP inhibitory activity. The inventors have evaluated antidiuretic effects in water-loaded rats and have found that the compounds increase endogenous AVP levels by inhibiting P-LAP and consequently reduce urine production. The present invention therefore provides compounds expected to be used as an agent for treating nocturia based on P-LAP inhibition.

The invention discloses a 2-(4-methoxyphenoxy) propionic acid derivative with sweetness inhibitory effect and an industrial production method thereof. Its structural formula is as follows, where R represents C 1 -C 4 Alkyl, C 1 -C 4 alkoxy, nitro or halogen atom, X represents a hydrogen atom or C 1 -C 3 of alkyl. Mix p-methoxy substituted phenol, ethyl 2-bromoalkanoate, and potassium carbonate, react in dimethylformamide, and filter; add water and organic phase to the filtrate, separate liquid, and evaporate the organic phase. Obtain an ester compound; add the obtained ester and sodium hydroxide to ethanol, reflux reaction, and obtain 2-(4-methoxyphenoxy)propionic acid derivatives through steps such as acidification, extraction, and recrystallization. The derivative of the present invention is a brand-new sweetness-inhibiting compound, which has good sweetness-inhibiting effect on sucrose. The industrial method has mild reaction conditions, the temperature does not exceed 100°C, simple separation and purification, and high product purity.