C07D475/04

CRYSTALLINE SODIUM SALT OF 5-METHYL-(6S)-TETRAHYDROLIC ACID

The present invention is directed to a crystalline sodium salt of 5-methyl-(6S)-tetrahydrofolic acid wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to sodium is from 1:0.5 to 1:1.5 (in mol/mol) and/or hydrates and/or solvates thereof, as well as, a processes of obtaining the same.

Medicinal agent and beverage/food for preventing cerebral dysfunction and improving same

Disclosed is a means for improving the symptoms of a cerebral dysfunction. The present inventors made a new discovery that the activity of brain aromatic monoamines increases when sepiapterin is administered peripherally. Disclosed, therefore, is a medicinal agent, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Also disclosed is a beverage/food, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Unlike tetrahydrobiopterin and the like, sepiapterin can control reductions in the brain neuron levels of brain aromatic monoamines (serotonin, dopamine, noradrenaline, and the like) and increase the activity thereof even when administered peripherally. Therefore, sepiapterin may be effective for cerebral dysfunctions, which are due to reductions in the brain neuron levels of brain aromatic monoamines, such as depression, bulimia, autism, impaired consciousness and concentration, cognitive disorders and other central mental disorders, as well as myotonia, rigidity, tremors, and other central motor disorders.

Medicinal agent and beverage/food for preventing cerebral dysfunction and improving same

Disclosed is a means for improving the symptoms of a cerebral dysfunction. The present inventors made a new discovery that the activity of brain aromatic monoamines increases when sepiapterin is administered peripherally. Disclosed, therefore, is a medicinal agent, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Also disclosed is a beverage/food, which contains at least sepiapterin or a salt thereof, for preventing or improving cerebral dysfunction. Unlike tetrahydrobiopterin and the like, sepiapterin can control reductions in the brain neuron levels of brain aromatic monoamines (serotonin, dopamine, noradrenaline, and the like) and increase the activity thereof even when administered peripherally. Therefore, sepiapterin may be effective for cerebral dysfunctions, which are due to reductions in the brain neuron levels of brain aromatic monoamines, such as depression, bulimia, autism, impaired consciousness and concentration, cognitive disorders and other central mental disorders, as well as myotonia, rigidity, tremors, and other central motor disorders.

ALPHA POLYGLUTAMATED TETRAHYDROFOLATES AND USES THEREOF
20210346381 · 2021-11-11 ·

The disclosure relates generally to polyglutamated alpha tetrahydrofolate compositions, including delivery vehicles such as liposomes containing the polyglutamated alpha tetrahydrofolate, and methods of making and using the polyglutamated alpha tetrahydrofolate compositions to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., inflammation and autoimmune diseases such as rheumatoid arthritis). The disclosed compositions also have uses in combination therapy with one or more therapeutic agents to enhance the effectiveness or to reduce the toxicities associated with the therapeutic agent(s).

GAMMA POLYGLUTAMATED PRALATREXATE AND USES THEREOF
20210346294 · 2021-11-11 ·

The disclosure relates generally to gamma polyglutamated pralatrexate compositions, including delivery vehicles such as liposomes containing the gamma polyglutamated pralatrexate, and methods of making and using the gamma polyglutamated pralatrexate compositions to treat hyperproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., inflammation and autoimmune diseases such as rheumatoid arthritis).

METHODS OF MANUFACTURE AND SYNTHESIS OF FLUORESCENT DYE COMPOUNDS AND USES THEREOF
20210347766 · 2021-11-11 ·

The present disclosure relates to synthesizing and utilizing fluorescent dye compounds or pharmaceutically acceptable salts thereof. Conjugation of amino acid groups to the fluorescent dyes increase specificity and detection of the compound. Methods of manufacture and synthesis of the compounds for use thereof in diagnostic imaging are contemplated.

STABLE SALT OF 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID

The present invention is directed towards the hemisulfate salt of 5,10-methylene-(6R)-tetrahydrofolic acid, preferably in substantially crystalline form, as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.

STABLE SALT OF 5,10-METHYLENE-(6R)-TETRAHYDROFOLIC ACID

The present invention is directed towards the hemisulfate salt of 5,10-methylene-(6R)-tetrahydrofolic acid, preferably in substantially crystalline form, as well as pharmaceutical compositions and uses thereof in therapy, preferably chemotherapy.

Folate salts

The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.

Folate salts

The invention relates to crystalline folate salts. The salt consists of a folate anion and an organic cation. The folate anion is 5-methyl-(6S)-tetrahydrofolic acid, and the cation is an organic compound which is an alkanolamine selected from the group consisting of choline, N-methylaminoethanol, 2-amino-2-methylpropanol and 2-dimethylaminoethanol.