IP Library Granted Patent US 10,413,532
Granted Patent B2
US 10,413,532 · App. 16/013,607 · Granted Sep 17, 2019

Pharmaceutical compositions containing a PDE4 inhibitor and a PI3 delta or dual PI3 delta-gamma kinase inhibitor

Inventors: Swaroop K. Vakkalanka (La Chaux-de-Fonds, CH); Srikant Viswanadha (Hyderabad, IN)
Assignee: RHIZEN PHARMACEUTICALS SA
A61K31/44A61K31/519A61K31/52A61K45/06A61K2300/00
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Quick Facts
Patent No.
US 10,413,532
App. No.
16/013,607
Granted
Sep 17, 2019
Kind
B2
Abstract

This present invention relates to a method of treating a autoimmune, respiratory and/or inflammatory disease or condition (e.g., psoriasis, rheumatoid arthritis, asthma, COPD). The method comprises administering a PI3K Delta inhibitor or a dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor. The present invention also relates to pharmaceutical compositions containing a PI3K Delta or dual PI3K Delta-Gamma inhibitor and a PDE4 inhibitor.

Claims (18)

1. A method of treating an autoimmune, respiratory and/or inflammatory disease or condition selected from asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, inflammatory bowel disease, glomerulonephritis, neuroinflammatory diseases, multiple sclerosis, uveitis, psoriasis, arthritis, vasculitis, dermatitis, osteoarthritis, inflammatory muscle disease, allergic rhinitis, vaginitis, interstitial cystitis, scleroderma, osteoporosis, eczema, allogeneic or xenogeneic transplantation (organ, bone marrow, stem cells and other cells and tissues) graft rejection, graft-versus-host disease, lupus erythematosus, inflammatory disease, type I diabetes, pulmonary fibrosis, dermatomyositis, Sjogren's syndrome, thyroiditis, myasthenia gravis, autoimmune hemolytic anemia, cystic fibrosis, chronic relapsing hepatitis, primary biliary cirrhosis, allergic conjunctivitis, atopic dermatitis, and combinations thereof,

the method comprising administering to a subject in need thereof a therapeutically effective amount of (i) a dual PI3K Delta and Gamma inhibitor, and (ii) a PDE4 inhibitor, wherein

the dual PI3K Delta and Gamma inhibitor is (+)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof; and

the PDE4 inhibitor is selected from roflumilast, apremilast, and pharmaceutically acceptable salts thereof.

2. The method according to claim 1 , wherein the PDE4 inhibitor is roflumilast or a pharmaceutically acceptable salt thereof.

3. The method according to claim 1 , wherein the PDE4 inhibitor is apremilast or a pharmaceutically acceptable salt thereof.

4. The method according to claim 1 , wherein the therapeutically effective amount of the dual PI3K Delta and Gamma inhibitor and the therapeutically effective amount of PDE4 inhibitor are administered simultaneously as a combined formulation.

5. The method according to claim 1 , wherein the therapeutically effective amount of dual PI3K Delta and Gamma inhibitor and the therapeutically effective amount of PDE4 inhibitor are administered sequentially.

6. The method according to claim 5 , wherein the therapeutically effective amount of PDE4 inhibitor is administered before the therapeutically effective amount of Dual PI3K Delta and Gamma inhibitor.

7. The method according to claim 1 , wherein the therapeutically effective amount of dual PI3K Delta and Gamma inhibitor is administered twice daily to once every three weeks, and the therapeutically effective amount of the PDE4 inhibitor is administered twice daily to once every three weeks.

8. The method according to claim 1 , wherein the autoimmune, respiratory and/or inflammatory disease or condition is selected from asthma, allergic rhinitis, non-allergic rhinitis, rheumatoid arthritis, chronic obstructive pulmonary disease, and atopic dermatitis.

9. The method according to claim 1 , wherein the dual PI3K Delta and Gamma inhibitor and at the PDE4 inhibitor are each administered in an amount ranging from about 0.01 mg to about 1000 mg.

10. The method of claim 1 , wherein the dual PI3K Delta and Gamma inhibitor and the PDE4 inhibitor are administered at a ratio of about 1:100 to about 100:1 by weight.

11. The method of claim 1 , wherein the autoimmune, respiratory and/or inflammatory disease or condition is asthma.

12. The method of claim 1 , wherein the autoimmune, respiratory and/or inflammatory disease or condition is chronic obstructive pulmonary disease.

13. The method according to claim 1 , wherein the PDE4 inhibitor is apremilast.

14. A method of treating an autoimmune, respiratory and/or inflammatory disease or condition selected from asthma, chronic obstructive pulmonary disease, rheumatoid arthritis, inflammatory bowel disease, glomerulonephritis, neuroinflammatory diseases, multiple sclerosis, uveitis, psoriasis, arthritis, vasculitis, dermatitis, osteoarthritis, inflammatory muscle disease, allergic rhinitis, vaginitis, interstitial cystitis, scleroderma, osteoporosis, eczema, allogeneic or xenogeneic transplantation (organ, bone marrow, stem cells and other cells and tissues) graft rejection, graft-versus-host disease, lupus erythematosus, inflammatory disease, type I diabetes, pulmonary fibrosis, dermatomyositis, Sjogren's syndrome, thyroiditis, myasthenia gravis, autoimmune hemolytic anemia, cystic fibrosis, chronic relapsing hepatitis, primary biliary cirrhosis, allergic conjunctivitis, atopic dermatitis, and combinations thereof,

the method comprising administering to a subject in need thereof a therapeutically effective amount of (i) (+)-2-(1-(4-amino-3-(3-fluoro-4-isopropoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)ethyl)-5-fluoro-3-(3-fluorophenyl)-4H-chromen-4-one or a pharmaceutically acceptable salt thereof, and (ii) apremilast.

Assignments (2)
CHANGE OF ADDRESS Recorded Oct 6, 2021
From: RHIZEN PHARMACEUTICALS AG
To: RHIZEN PHARMACEUTICALS AG
Reel/Frame 057836/0286 →
CHANGE OF ADDRESS Recorded Mar 22, 2021
From: RHIZEN PHARMACEUTICALS SA
To: RHIZEN PHARMACEUTICALS SA
Reel/Frame 056775/0375 →
Priority Claims (2)
IN 2762/CHE/2012 · Nov 8, 2012 · national
IN 4688/CHE/2012 · Nov 8, 2012 · national
Continuity (3)
Continuation 15654181 · Jul 19, 2017
Continuation 14441758
Related Publication 20190083475A1 · Mar 21, 2019