C07C229/26

CO-CRYSTAL OF KETOPROFEN, LYSINE AND GABAPENTIN, PHARMACEUTICAL COMPOSITIONS AND THEIR MEDICAL USE

The present invention relates to a new co-crystal of Ketoprofen, Lysine and Gabapentin, to pharmaceutical compositions and to their use in the prevention, reduction or treatment of pain and/or inflammation.

CO-CRYSTAL OF KETOPROFEN, LYSINE AND GABAPENTIN, PHARMACEUTICAL COMPOSITIONS AND THEIR MEDICAL USE

The present invention relates to a new co-crystal of Ketoprofen, Lysine and Gabapentin, to pharmaceutical compositions and to their use in the prevention, reduction or treatment of pain and/or inflammation.

Salts formed by 2-(1-acyloxy-n-pentyl) benzoic acid and basic amino acid or aminoguanidine, and preparation method and application thereof

The present disclosure discloses salts formed by 2-(1-acyloxy-n-pentyl)benzoic acid and basic amino acid or aminoguanidine, a preparation method thereof, pharmaceutical preparations containing these salts, and application thereof in preparation of drugs for preventing or treating ischemic cardiovascular and cerebrovascular diseases, resisting thrombosis and improving cardio-cerebral circulation disorders. The compound of the present disclosure has excellent water solubility, aqueous solution stability and pharmacokinetic properties, also has significant anti-platelet aggregation, anti-thrombosis, anti-cerebral ischemia and neuroprotective activity. The compound of the present disclosure has significantly better effects than those of (S)-butylphthalide and potassium (R/S)-2-(1-hydroxy-n-pentyl) benzoate (PHPB), has significantly lower acute toxicity to mice by intravenous injection than that of butylphthalide and PHPB, has a lower inhibition rate of the hERG potassium channel in CHO-hERG cells than that of (S)-butylphthalide, and has a negative result in Bacterial Reverse Mutation Test (Ames test).

Separation of basic amino acids

The present invention relates to a method of separating amino acids from an aqueous solution comprising amino acids as well as proteins and/or protein decomposition products by combining phosphoric acid with the aqueous solution to precipitate an amino acid monophosphate. The precipitate so formed may be separated from the aqueous solution and used as such, e.g. in plant fertilizer compositions. The precipitate may be redissolved in a suitable liquid, after which phosphate and amino acid may be separated following conventional methods. In either case, the present invention enables highly selective precipitation of arginine and/or lysine monophosphate as crystals.

Separation of basic amino acids

The present invention relates to a method of separating amino acids from an aqueous solution comprising amino acids as well as proteins and/or protein decomposition products by combining phosphoric acid with the aqueous solution to precipitate an amino acid monophosphate. The precipitate so formed may be separated from the aqueous solution and used as such, e.g. in plant fertilizer compositions. The precipitate may be redissolved in a suitable liquid, after which phosphate and amino acid may be separated following conventional methods. In either case, the present invention enables highly selective precipitation of arginine and/or lysine monophosphate as crystals.

Method for producing amino acid aminoalkyl ester or inorganic acid salt thereof

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

Method for producing amino acid aminoalkyl ester or inorganic acid salt thereof

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

Method for producing amino acid aminoalkyl ester or inorganic acid salt thereof

The present invention provides a method for producing an amino acid aminoalkyl ester or an inorganic acid salt thereof by reacting a compound represented by general formula (I) shown below or a compound represented by general formula (III) shown below, or a salt thereof, and at least one compound selected from the group consisting of compounds represented by general formula (IV-I) shown below, compounds represented by general formula (IV-II) shown below, compounds represented by general formula (IV-III) shown below and compounds represented by general formula (IV-IV) shown below, or an inorganic acid salt thereof. ##STR00001##

3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS

A compound of formula (I) or a salt thereof are provided:

##STR00001##

wherein R.sup.1, X and R.sup.3 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.

3-(5-CHLORO-2-OXOBENZO[D]OXAZOL-3(2H)-YL) PROPANOIC ACID DERIVATIVES AS KMO INHIBITORS

A compound of formula (I) or a salt thereof are provided:

##STR00001##

wherein R.sup.1, X and R.sup.3 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.