Heterocyclic compounds and their uses

Patent metadata

Field	Value
Publication number	US-9895308-B2
Application number	US-201414773444-A
Country	US
Kind code	B2
Filing date	Mar 14, 2014
Priority date	Mar 14, 2013
Publication date	Feb 20, 2018
Grant date	Feb 20, 2018

Abstract

Provided are certain pharmaceutical formulations of omecamtiv mecarbil and methods for their preparation and use.

First claim

What is claimed:

1. A pharmaceutical tablet formulation comprising:
a drug layer, comprising omecamtiv mecarbil dihydrochloride hydrate;
a sweller layer; and
a semi-permeable membrane coating having at least one delivery port,

wherein the semi-permeable membrane coating comprises 80% insoluble polymer and 20% pore forming polymer.

2. A pharmaceutical tablet formulation according to claim 1 , wherein the drug layer comprises:
omecamtiv mecarbil dihydrochloride hydrate;
a drug layer polymer; and
a lubricant.

3. A pharmaceutical tablet formulation according to claim 1 , wherein the sweller layer comprises:
a sweller layer polymer;
an osmotic agent;
a diluent; and
a lubricant.

4. A pharmaceutical tablet formulation according to claim 1 , where the
insoluble polymer comprises cellulose acetate.

5. A pharmaceutical tablet formulation according to claim 1 , wherein the pore forming polymer comprises polyethylene glycol.

6. A pharmaceutical tablet formulation comprising:
a drug layer comprising:
omecamtiv mecarbil dihydrochloride hydrate;
a drug layer polymer; and
a lubricant;

a sweller layer comprising:
a sweller layer polymer;
an osmotic agent;
a diluent; and
a lubricant; and

a semi-permeable membrane coating having at least one delivery port comprising:
an insoluble polymer comprising cellulose acetate; and
a pore forming polymer comprising polyethylene glycol,

wherein the semi-permeable membrane coating comprises 80% the insoluble polymer and 20% the pore forming polymer.

7. A pharmaceutical tablet formulation comprising
a drug layer comprising:
14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate;
48-55 (w/w%) polyethylene oxide; and
0.1-0.5% (w/w%) lubricant;

a sweller layer comprising:
18-25 (w/w%) polyethylene oxide;
4-9 (w/w%) an osmotic agent;
3-6 (w/w%) microcrystalline cellulose; and
0.1-0.5 (w/w%) lubricant; and

a semi-permeable membrane having at least one delivery port comprising:
8-10 (w/w%) cellulose acetate;
0.5-3 (w/w%) polyethylene glycol.

8. The pharmaceutical tablet formulation of claim 7 , wherein the polyethylene glycol of the semi-permeable membrane has an average molecular weight of 3350.

9. The pharmaceutical tablet formulation of claim 7 , wherein the osmotic agent comprises sodium chloride.

10. The pharmaceutical tablet formulation of claim 7 , having one to 10 delivery ports.

11. The pharmaceutical tablet formulation according to claim 1 , wherein the tablet comprises 14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate.

12. The pharmaceutical tablet formulation according to claim 1 , wherein the insoluble polymer comprises cellulose acetate and the pore forming polymer comprises polyethylene glycol.

13. The pharmaceutical tablet formulation according to claim 1 , having one to 10 delivery ports.

14. The pharmaceutical tablet formulation according to claim 12 , wherein the tablet comprises 14-17 (w/w%) omecamtiv mecarbil dihydrochloride hydrate.

15. The pharmaceutical tablet formulation according to claim 14 , wherein the polyethylene glycol of the semi-permeable membrane has an average molecular weight of 3350.

Assignees

• Amgen Inc

Inventors

• Caldwell William Brett

Classifications

• A61P9/04

  Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure · CPC title

• A61K9/2866

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K9/0004 Primary

  Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas · CPC title

• A61K9/2054

  Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose · CPC title

• A61K31/496

  Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin · CPC title