Heterocyclic compounds and their uses
Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.
1. A pharmaceutical formulation comprising:
about 30.65 mg of omecamtiv mecarbil dihydrochloride hydrate;
a control release agent;
a pH modifying agent comprising maleic acid, fumaric acid, tartaric acid, glutamic acid, or a combination thereof;
a filler; and
a lubricant.
2. A method of treating a disease associated with systolic heart dysfunction, comprising administering the pharmaceutical formulation of claim 1 to a patient in need thereof.
3. The pharmaceutical formulation of claim 1 , wherein the omecamtiv mecarbil dihydrochloride hydrate is omecamtiv mecarbil dihydrochloride monohydrate.
4. The pharmaceutical formulation of claim 1 , wherein the control release agent comprises hydroxypropylmethylcellulose.
5. The pharmaceutical formulation of claim 1 , wherein the pH modifying agent is fumaric acid.
6. The pharmaceutical formulation of claim 1 , wherein the filler comprises microcrystalline cellulose, or lactose monohydrate, or a combination of microcrystalline cellulose and lactose monohydrate.
7. The pharmaceutical formulation of claim 1 , wherein the lubricant is magnesium stearate.
8. The pharmaceutical formulation of claim 1 , wherein the formulation is in the form of a tablet.
9. A pharmaceutical formulation comprising:
about 6.13% w/w of omecamtiv mecarbil dihydrochloride hydrate;
a control release agent;
a pH modifying agent comprising maleic acid, fumaric acid, tartaric acid, glutamic acid, or a combination thereof;
a filler; and
a lubricant.
10. A method of treating a disease associated with systolic heart dysfunction, comprising administering the pharmaceutical formulation of claim 9 to a patient in need thereof.
11. The pharmaceutical formulation of claim 9 , wherein the omecamtiv mecarbil dihydrochloride hydrate is omecamtiv mecarbil dihydrochloride monohydrate.
12. The pharmaceutical formulation of claim 9 , wherein the control release agent comprises hydroxypropylmethylcellulose.
13. The pharmaceutical formulation of claim 9 , wherein the pH modifying agent is fumaric acid.
14. The pharmaceutical formulation of claim 9 , wherein the filler comprises microcrystalline cellulose, or lactose monohydrate, or a combination of microcrystalline cellulose and lactose monohydrate.
15. The pharmaceutical formulation of claim 9 , wherein the lubricant is magnesium stearate.
16. The pharmaceutical formulation of claim 9 , wherein the formulation is in the form of a tablet.
17. A pharmaceutical formulation comprising:
about 30.65 mg or about 6.13% w/w of omecamtiv mecarbil dihydrochloride hydrate;
a control release agent comprising hydroxypropylmethylcellulose;
a pH modifying agent comprising fumaric acid;
a filler; and
a lubricant.
18. A method of treating a disease associated with systolic heart dysfunction, comprising administering the pharmaceutical formulation of claim 17 to a patient in need thereof.
19. The pharmaceutical formulation of claim 17 , wherein the omecamtiv mecarbil dihydrochloride hydrate is omecamtiv mecarbil dihydrochloride monohydrate.
20. The pharmaceutical formulation of claim 17 , wherein the filler comprises microcrystalline cellulose, or lactose monohydrate, or a combination of microcrystalline cellulose and lactose monohydrate.
21. The pharmaceutical formulation of claim 17 , wherein the lubricant is magnesium stearate.
22. The pharmaceutical formulation of claim 17 , wherein the formulation is in the form of a tablet.