Patent classifications
C07C57/02
NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES
The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:
##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
NOVEL FATTY ACIDS AND THEIR USE IN CONJUGATION TO BIOMOLECULES
The invention provides a conjugate comprising a biomolecule linked to a fatty acid via a linker wherein the fatty acid has the following Formulae A1, A2 or A3:
##STR00001## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Ak, n, m and p are defined herein. The invention also relates to a method for manufacturing the conjugate of the invention such as GDF15 conjugate, and its therapeutic uses such as treatment or prevention of metabolic disorders or diseases, type 2 diabetes mellitus, obesity, pancreatitis, dyslipidemia, alcoholic and nonalcoholic fatty liver disease/steatohepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose intolerance, hyperglycemia, metabolic syndrome, hypertension, cardiovascular disease, atherosclerosis, peripheral arterial disease, stroke, heart failure, coronary heart disease, diabetic complications (including but not limited to chronic kidney disease), neuropathy, gastroparesis and other metabolic disorders. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Method for producing carboxylic acid anhydride and method for producing carboxylic acid ester
Provided is a production method whereby corresponding carboxylic acid anhydrides and carboxylic acid esters can be obtained at high yield from various carboxylic acids even without a solvent and near room temperature. A method for producing a carboxylic acid anhydride represented by formula (II), the method comprising reacting a compound represented by formula (I) and a carboxylic acid in the presence of a Group II metal compound having an ionic ligand containing an oxygen atom. A method for producing a carboxylic acid ester, the method comprising reacting a carboxylic acid anhydride produced by the aforementioned method and an alcohol. In formula (I), R.sup.1 represents a C.sub.1-20 hydrocarbon group. In formula (II), R.sup.2 represents a C.sub.1-20 hydrocarbon group.
Method for producing carboxylic acid anhydride and method for producing carboxylic acid ester
Provided is a production method whereby corresponding carboxylic acid anhydrides and carboxylic acid esters can be obtained at high yield from various carboxylic acids even without a solvent and near room temperature. A method for producing a carboxylic acid anhydride represented by formula (II), the method comprising reacting a compound represented by formula (I) and a carboxylic acid in the presence of a Group II metal compound having an ionic ligand containing an oxygen atom. A method for producing a carboxylic acid ester, the method comprising reacting a carboxylic acid anhydride produced by the aforementioned method and an alcohol. In formula (I), R.sup.1 represents a C.sub.1-20 hydrocarbon group. In formula (II), R.sup.2 represents a C.sub.1-20 hydrocarbon group.
Optimized process for preparing methacrylic acid
The present invention relates to an optimized process for preparing methacrylic acid, wherein methacrolein is prepared in a first stage from propionaldehyde and formaldehyde by means of a Mannich reaction and oxidized in a second stage to methacrylic acid. More particularly, the present invention relates to the reduction in the amounts of catalyst to be used in the first stage, especially to the reduction in the amounts of acid to be used here, by virtue of the additional installation of recycling streams suitable for the purpose.
OIL COMPRISING POLYUNSATURATED FATTY ACIDS
The present invention relates to a process for producing ethyl esters of polyunsaturated fatty acids, comprising transesterifying triacylglycerols in extracted plant lipid.
CROSSLINKING MATERIALS FROM BIORENEWABLE ACONITIC ACID
A process includes forming a bio-derived crosslinking material from biorenewable aconitic acid. The process includes initiating a chemical reaction to form a bio-derived crosslinking material that includes multiple functional groups. The chemical reaction includes converting each carboxylic acid group of a biorenewable aconitic acid molecule to one of the multiple functional groups.
CROSSLINKING MATERIALS FROM BIORENEWABLE ACONITIC ACID
A process includes forming a bio-derived crosslinking material from biorenewable aconitic acid. The process includes initiating a chemical reaction to form a bio-derived crosslinking material that includes multiple functional groups. The chemical reaction includes converting each carboxylic acid group of a biorenewable aconitic acid molecule to one of the multiple functional groups.
CROSSLINKING MATERIALS FROM BIORENEWABLE ACONITIC ACID
A process includes forming a bio-derived crosslinking material from biorenewable aconitic acid. The process includes initiating a chemical reaction to form a bio-derived crosslinking material that includes multiple functional groups. The chemical reaction includes converting each carboxylic acid group of a biorenewable aconitic acid molecule to one of the multiple functional groups.
CROSSLINKING MATERIALS FROM BIORENEWABLE ACONITIC ACID
A process includes forming a bio-derived crosslinking material from biorenewable aconitic acid. The process includes initiating a chemical reaction to form a bio-derived crosslinking material that includes multiple functional groups. The chemical reaction includes converting each carboxylic acid group of a biorenewable aconitic acid molecule to one of the multiple functional groups.