Granted Patent B2

US 10,166,225 · App. 14/346,570 · Granted Jan 1, 2019

Inventors: Dana T. Aftab (San Rafael, CA); Douglas Clary (San Francisco, CA)

Assignee: Exelixis, Inc.

A61K31/47A61K9/2018A61K9/2054G01N33/6887G01N2333/78G01N2333/916G01N2800/108G01N2800/52

Abstract

Claims (17)

1. A method for treating osteoporosis, comprising administering to a patient in need of such treatment a once daily dose of 15, 10, or 5 mg of Compound 1:

N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

or a pharmaceutically acceptable salt thereof; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

2. The method of claim 1 , wherein Compound 1 is the (L)-malate salt.

3. The method of claim 1 , wherein Compound 1, or a pharmaceutically acceptable salt thereof, is administered as a pharmaceutical composition comprising a pharmaceutically acceptable carrier.

4. A method for treating osteoporosis in patients who have or are currently undergoing treatment for cancer, comprising administering a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

5. A method for ameliorating abnormal deposition of unstructured bone accompanied by increased skeletal fractures, spinal cord compression, and severe bone pain of osteoporosis, comprising administering to a patient in need of such treatment a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

6. A method for stimulating osteoblast differentiation and/or activity in a patient with osteoporosis in need of such treatment, comprising administering to the patient a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

7. A method for stimulating bone formation in a patient with osteoporosis in need of such treatment, comprising administering to the patient a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

8. A method for inhibiting osteoclast differentiation and/or activity in a patient with osteoporosis in need of such treatment, comprising administering to the patient a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

9. A method for modulating bone turnover toward bone formation in a patient with osteoporosis in need of such treatment, comprising administering to the patient a once daily dose of 15, 10, or 5 mg of Compound 1:

or the malate salt of Compound 1 or another pharmaceutically acceptable salt of Compound 1; wherein Compound 1 stimulates osteoblast differentiation and inhibits osteoclast differentiation.

Assignments (1)

Continuity (2)

Cited By (9)

US 12,275,706 US 12,415,784 US 12,486,233 US 12,516,025 US 12,516,026 US 12,522,567 US 12,552,749 US 12,661,350 US 12,741,938