A method was developed for the synthesis of hydroxy carboxylic acids by the addition of saturated alcohols and acids to 10-undecenoic acid and 10-undecen-1-ol.

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: wherein R1, R2, R3, R4, 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.

Free-radical addition of alcohols and acids to 10-undecenoic esters, 10-undecen-1-Ol, and 10-undecenyl acetate

Fatty acids and their use in conjugation to biomolecules

L'invention concerne un conjugue comprenant une biomolecule liee a un acide gras par l'intermediaire d'un lieur, les formules de l'acide gras etant les suivantes : A1, A2 ou A3 dans lesquelles R 1 , R 2 , R 3 , R 4 , Ak, n, m et p sont tels que definis dans la description. L'invention concerne egalement un procede de fabrication du conjugue de l'invention, tel que le conjugue GDF15, ainsi que ses utilisations therapeutiques telles que le traitement ou la prevention de troubles ou maladies metaboliques, du diabete sucre de type 2, de l'obesite, de la pancreatite, de la dyslipidemie, de la maladie du foie gras/steatohepatite, alcoolique et non alcoolique, et autres maladies du foie evolutives, de la resistance a l'insuline, de l'hyperinsulinemie, de l'intolerance au glucose, de l'hyperglycemie, dy syndrome metabolique, de l'hypertension, des maladies cardio-vasculaires, de l'atherosclerose, des maladies arterielles peripheriques, des accidents vasculaires cerebraux, de l'insuffisance cardiaque, des coronaropathies, des complications diabetiques (comprenant, entre autres, les maladie renales chroniques), des neuropathies, de la gastroparesie et d'autres troubles metaboliques. La presente invention concerne egalement une combinaison d'agents pharmacologiquement actifs et une composition pharmaceutique.

Acides gras et leur utilisation dans la conjugaison de biomolécules

The invention provides the conjugate for including the biomolecule being connected via linker with aliphatic acid, wherein the aliphatic acid has following formula A1, A2 or A3：Wherein R 1 、R 2 、R 3 、R 4 , Ak, n, m and p as defined herein.The invention further relates to the preparation method and its therapeutical uses of the conjugate such as GDF15 conjugates of the present invention as treated or prevented dysbolism or disease, diabetes B, it is fat, pancreatitis, dyslipidemia, Alcoholic and NASH disease/fat hepatitis and other progressive liver diseases, insulin resistance, hyperinsulinemia, glucose Intolerance, hyperglycaemia, metabolic syndrome, hypertension, angiocardiopathy, atherosclerosis, peripheral arterial disease, apoplexy, heart failure, coronary heart disease, diabetic complication (includes but is not limited to chronic kidney disease), neuropathy, gastroparesis and other dysbolisms.Present invention also offers the combination product of pharmacologically active agents and pharmaceutical composition.

Aliphatic acid and its purposes in being conjugated with biomolecule

Sur quelques acides polyméthylène‐dicarboniques monométhylés et quelques‐uns de leurs dérivés

Verschieden hoch hydroxylierte Stearinsauren wurden UR-spektrophotometrisch vermessen und das Verhaltnis der Intensitaten von OH- und CH-Valenzschwingung ermittelt, wobei sich ein gesetzmasiger Zusammenhang mit der Zahl der eingefuhrten Hydroxylgruppen ergab. Die daraus abzuleitenden Moglichkeiten einer Bestimmung des Hydroxylanteiles in Substanzen mit unbekanntem Hydroxylgehalt werden besprochen.

Free-radical addition of alcohols and acids to 10-undecenoic esters, 10-undecen-1-Ol, and 10-undecenyl acetate

Citations

Fatty acids and their use in conjugation to biomolecules

Acides gras et leur utilisation dans la conjugaison de biomolécules

Aliphatic acid and its purposes in being conjugated with biomolecule

References

Sur quelques acides polyméthylène‐dicarboniques monométhylés et quelques‐uns de leurs dérivés

Die UR-spektrometrische Bestimmbarkeit des Hydroxylgehaltes in C18-Fettsäuren und deren Estern