Granted Patent B2

US 10,016,426 · App. 15/408,814 · Granted Jul 10, 2018

Inventor: Narmada R. Shenoy (Sunnyvale, CA)

Assignee: Resverlogix Corp.

A61K31/517A61K9/1611A61K9/1617A61K9/1652A61K9/485A61K9/4858A61K9/4866

Abstract

Claims (115)

1. A method for treating a cardiovascular-, cholesterol-, or lipid-related disease or disorder, comprising administering a pharmaceutical formulation comprising an active ingredient selected from:

2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;

and pharmaceutically acceptable salts, stereoisomers, hydrates, and tautomers thereof:

wherein the active ingredient is present:

(a) in an amount front about 10% to about 12% by weight and the formulation further comprises:

(i) about 82% to about 83% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(b) in an amount from about 20% to about 22% by weight and the formulation further comprises:

(i) about 70% to about 72% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(c) in an amount from about 31% to about 33% by weight and the formulation further comprises:

(i) about 60% to about 62% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

or

(d) in an amount from about 41% to about 43% by weight and the formulation further comprises:

(i) about 50% to about 51% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

and wherein the formulation is formulated for oral administration and immediate release.

2. The method of claim 1 , wherein the active ingredient is the hydrochloride salt of 2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one.

3. The method of claim 1 , wherein the active ingredient has a particle size from about 1-250 microns, about 1-100 microns, or about 1-10 microns.

4. The method of claim 1 , wherein the formulation comprises from about 25-100 mg of the active ingredient.

5. The method of claim 4 , wherein the active ingredient is present in the formulation in an amount selected from about 25, 50, 75, or 100 mg.

6. The method of claim 1 , wherein the formulation has a disintegration time of 120 seconds or less.

7. The method of claim 1 , wherein the cardiovascular-, cholesterol-, or lipid-related disease or disorder is selected from acute coronary syndrome, angina, arteriosclerosis, atherosclerosis, carotid atherosclerosis, cerebrovascular disease, cerebral infarction, congestive heart failure, congenital heart disease, coronary heart disease, coronary artery disease, coronary plaque stabilization, dyslipidemias, dyslipoproteinemias, endothelium dysfunctions, familial hypercholeasterolemia, familial combined hyperlipidemia, hypoalphalipoproteinemia, hypertriglyceridemia, hyperbetalipoproteinemia, hypercholesterolemia, hypertension, hyperlipidemia, intermittent claudication, ischemia, ischemia reperfusion injury, ischemic heart diseases, cardiac ischemia, multi-infarct dementia, myocardial infarction, obesity, peripheral vascular disease, reperfusion injury, restenosis, renal artery atherosclerosis, rheumatic heart disease, stroke, thrombotic disorder, transitory ischemic attacks, syndrome X, impotence, multiple sclerosis, and Parkinson's disease.

8. The method of claim 1 , wherein the cardiovascular-, cholesterol-, or lipid-related disease or disorder is metabolic syndrome.

9. The method of claim 1 , wherein the cardiovascular-, cholesterol-, or lipid-related disease or disorder is Alzheimer's disease.

10. The method of claim 1 , wherein the cardiovascular-, cholesterol-, or lipid-related disease or disorder is diabetes mellitus.

11. The method of claim 10 , wherein the diabetes mellitus is associated with a disease selected from hyperglycemia, hyperinsulinemia, hyperlipidemia, insulin resistance, impaired glucose metabolism, obesity, diabetic retinopathy, macular degeneration, cataracts, diabetic nephropathy, glomerulosclerosis, erectile dysfunction, premenstrual syndrome, vascular restenosis, ulcerative colitis, skin and connective tissue disorders, foot ulcerations, metabolic acidosis, arthritis, osteoporosis and impaired glucose tolerance.

12. A method for treating a cancer selected from midline carcinoma, aggressive human medulloblastoma, hematological cancer, lung cancer, breast cancer, colon carcinomas, and hepatic tumors, comprising administering a pharmaceutical formulation comprising an active ingredient selected from:

2-(4-(2-hydroxyethoxy)-3,5-dimethyphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;

and pharmaceutically acceptable salts, stereoisomers, hydrates, and tautomers thereof;

wherein the active ingredient is present:

(a) in an amount from about 10% to about 12by weight and the formulation further comprises:

(i) about 82% to about 83% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(b) in an amount from about 20% to about 22% by weight and the formulation further comprises:

about 70% to about 72% by weight microcrystalline cellulose;

about 2.5% by weight of colloidal silicon dioxide;

about 4.0% by weight of sodium starch glycolate; and

about 0.5% by weight of magnesium stearate;

(c) in an amount from about 31% to about 33% by weight and the formulation further comprises:

(i) about 60% to about 62% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

or

(d) in an amount from about 41% to about 43% by weight and the formulation further comprises:

(i) about 50% to about 51% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of a sodium starch glycolate; and

(iv) about 5% by weight of magnesium stearate;

and wherein the formulation is formulated for oral administration and immediate release.

13. The method of claim 12 , wherein the hematological cancer is selected from Burkitt's lymphoma, acute myelogenous leukemia, and multiple myeloma.

14. A method for treating an IL-6 mediated inflammatory disease, comprising administering a pharmaceutical formulation comprising an active ingredient selected from:

2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;

and pharmaceutically acceptable salts, stereoisomers, hydrates, and tautomers thereof;

wherein the active ingredient is present:

(a) in an amount from about 10% to about 12% by weight and the formulation further comprises:

(i) about 82% to about 83% by weight of microcrystalline cellulose;

(ii) about 2.5%, by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(b) in an amount from about 20% to about 22% by weight and the formulation further comprises:

(i) about 70% to about 72% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(c) in an amount from about 31% to about 33% by weight and the formulation further comprises:

(i) about 60% to about 62% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

or

(d) in an amount from about 41% to about 43% by weight and the formulation further comprises:

(i) about 50% to about 51% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

and wherein the formulation is formulated for oral administration and immediate release.

15. A method for treating a bacterial infection or a viral infection selected from human immunodeficiency virus (HIV), herpes virus, and papilloma virus, comprising administering a pharmaceutical formulation comprising an active ingredient selected from:

2-(4-(2-hydroxyethoxy)-3,5-dimethylphenyl)-5,7-dimethoxyquinazolin-4(3H)-one;

and pharmaceutically acceptable salts, stereoisomers, hydrates, and tautomers thereof;

wherein the active ingredient is present:

(a) in an amount from about 10% to about 12% by weight and the formulation further comprises:

(i) about 82% to about 83% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(b) in an amount from about 20% to about 22% by weight and the formulation further comprises:

(i) about 70% to about 72% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

(c) in an amount from about 31% to about 33% by weight and the formulation further comprises:

(i) about 60% to about 62% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

or

(d) in an amount from about 41% to about 43% by weight and the formulation further comprises:

(i) about 50% to about 51% by weight of microcrystalline cellulose;

(ii) about 2.5% by weight of colloidal silicon dioxide;

(iii) about 4.0% by weight of sodium starch glycolate; and

(iv) about 0.5% by weight of magnesium stearate;

and wherein the formulation is formulated for oral administration and immediate release.

Assignments (8)

Continuity (3)