Disclosed is a crystalline form of sepiapterin, a method of preparing the crystalline form, pharmaceutical compositions containing the crystalline form, and a method for treating patients with a disease associated with low intracellular BH4 levels or with dysfunction of various BH4 dependent metabolic pathways, which involves administering to the patient an effective amount of the crystalline form.

The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and an amino acid ethyl ester like L-phenylalanine ethyl ester or L-methionine ethyl ester, wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to amino acid ethyl ester is from 1:0.3 to 1:3.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.

The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and an amino acid ethyl ester like L-phenylalanine ethyl ester or L-methionine ethyl ester, wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to amino acid ethyl ester is from 1:0.3 to 1:3.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.

The present invention relates to new pharmaceutical salts and/or co-crystals of sepiapterin which exhibit improved properties. In particular, the invention relates to salts of sepiapterin with improved stability. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts and/or co-crystals of sepiapterin, as well as methods of treating tetrahydrobiopterin-related disorders including administration of a sepiapterin salt and/or co-crystal of the invention to a subject in need thereof.

The present invention relates to new pharmaceutical salts and/or co-crystals of sepiapterin which exhibit improved properties. In particular, the invention relates to salts of sepiapterin with improved stability. The invention also relates to pharmaceutical compositions including a pharmaceutically effective amount of one or more salts and/or co-crystals of sepiapterin, as well as methods of treating tetrahydrobiopterin-related disorders including administration of a sepiapterin salt and/or co-crystal of the invention to a subject in need thereof.

The present invention is directed to crystalline salt of 5-methyl-(6S)-tetrahydrofolic acid comprising (i) 5-methyl-(6S)-tetrahydrofolic acid, (ii) sodium and (iii) an organic base having a pKa value from 6 to 11; wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the sodium is from 1:0.5 to 1:1.5 and the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the organic base is 1:0.5 to 1:1.5 and/or hydrates and/or solvates thereof, as well as, a processes of obtaining the same.

The present invention is directed to crystalline salt of 5-methyl-(6S)-tetrahydrofolic acid comprising (i) 5-methyl-(6S)-tetrahydrofolic acid, (ii) sodium and (iii) an organic base having a pKa value from 6 to 11; wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the sodium is from 1:0.5 to 1:1.5 and the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to the organic base is 1:0.5 to 1:1.5 and/or hydrates and/or solvates thereof, as well as, a processes of obtaining the same.

The present invention refers to a crystalline salt comprising 5-methyl-(6S)-tetrahydrofolic acid and 4-(2-hydroxyethyl)-morpholine wherein the molar ratio of 5-methyl-(6S)-tetrahydrofolic acid to 4-(2-hydroxyethyl)-morpholine is from 1:0.3 to 1:2.0 (in mol/mol) and/or hydrates and/or solvates thereof as well as to a process of obtaining the same.

The disclosure provides linked purine pterin compounds of Formula I that are novel inhibitors of HPPK, a kinase responsible for an essential step in the biosynthesis of folic acid. (Formula I) The variables, e.g., A1-A3, R1-R4, B1-B2, and L1 are defined in the disclosure. These linked purine pterin inhibitors bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing the HPPK inhibitors and methods of treating a bacterial infection in a patient with one or more of the HPPK inhibitors of the disclosure are also provided. ##STR00001##

The disclosure provides linked purine pterin compounds of Formula I that are novel inhibitors of HPPK, a kinase responsible for an essential step in the biosynthesis of folic acid. (Formula I) The variables, e.g., A1-A3, R1-R4, B1-B2, and L1 are defined in the disclosure. These linked purine pterin inhibitors bind to HPPK with high affinity and specificity. Pharmaceutical compositions containing the HPPK inhibitors and methods of treating a bacterial infection in a patient with one or more of the HPPK inhibitors of the disclosure are also provided. ##STR00001##