Useful pharmaceutical salts of 7-[(3R, 4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3, 5-dihydro-pyrrolo [3, 2-D] pyrimidin-4-one
View Patent ↗The present disclosure provides novel hemi- and mono-salts of 7-[(3R,4R)-3-Hydroxy-4-hydroxymethyl-pyrrolidin-1-ylmethyl]-3,5-dihydro-pyrrolo[3,2- d ]pyrimidin-4-one (Compound 1) with various organic and inorganic acids. In one embodiment, the organic acid is a C4 organic diacids. The present disclosure further provides novel methods for preparing these salts. The novel monohydrates hemisalts of the C4 organic diacids are isostructural and can be prepared with different properties. Multiple acids can be used simultaneously and the proportion of acids can be varied offering the opportunity to select hemi-salts of compound 1 with desired properties.
1. A salt of compound 1:
wherein the salt of compound 1 is a hemi salt with a C 4 organic diacid, the C4 organic diacid being selected from the group consisting of succinic, fumaric, L-malic or a mixture thereof wherein the salt exhibits no polypmorphic variants or a reduced number of polymorphic variants.
2. The salt according to claim 1 , wherein the C 4 organic diacid is selected from the group consisting of succinic, fumaric, and L-malic acids.
3. The salt according to claim 1 , wherein the salt is a mixed salt.
4. The salt according to claim 3 , wherein the salt is selected from the group consisting of hemi(hemisuccinate, hemifumarate) monohydrate, hemi(hemisuccinate, hemimalate) monohydrate, and hemi(hemifumarate, hemimalate) monohydrate.
5. The salt according to claim 1 , wherein the salt is the hemisuccinate monohydrate.