Combination of PI3K-inhibitors

Patent metadata

Field	Value
Publication number	US-10117874-B2
Application number	US-201415101638-A
Country	US
Kind code	B2
Filing date	Nov 28, 2014
Priority date	Dec 3, 2013
Publication date	Nov 6, 2018
Grant date	Nov 6, 2018

Abstract

The present invention relates to combinations of at least two components, component A and component B, component A being an inhibitor of PI3K kinase, and component B being radium 223, particularly a pharmaceutically acceptable salt of radium-223. Another aspect of the present invention relates to the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of breast and prostate cancer as well as their bone metatases.

First claim

The invention claimed is:

1. A pharmaceutical combination comprising:
component A, which is 2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide,
or a physiologically acceptable salt, solvate, hydrate or stereoisomer thereof; and
component B, which is radium-223 dichloride.

2. The pharmaceutical combination according to claim 1 , wherein component A is
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide,
or a physiologically acceptable salt thereof.

3. The pharmaceutical combination according to claim 1 , wherein component A is
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide dihydrochloride.

4. The pharmaceutical combination according to claim 1 , wherein component A is
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide.

5. A method for treatment of hepatocyte carcinoma, lung cancer, non-small cell lung carcinoma, colorectal cancer, melanoma, pancreatic cancer, prostate cancer, breast cancer or metastases thereof, comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical combination according to claim 1 .

6. A kit comprising the pharmaceutical combination according to claim 1 , and optionally one or more further pharmaceutical agents C,
wherein optionally both or either of components A and B are in the form of a pharmaceutical formulation which is ready for use to be administered simultaneously, concurrently, separately or sequentially.

7. A pharmaceutical composition comprising the pharmaceutical combination according to claim 1 and a pharmaceutically acceptable ingredient.

8. A method for treatment of multiple myeloma, lung cancer, breast cancer, prostate cancer, or metastases thereof, comprising administering to a patient in need thereof a therapeutically effective amount of the pharmaceutical combination according to claim 1 .

9. The method according to claim 5 , wherein the metastases are bone metastases.

10. The method of claim 8 , wherein the prostate cancer is castration-resistant prostate cancer (CRPC).

11. The method of claim 5 , wherein the pharmaceutical combination comprises
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
or a physiologically acceptable salt thereof.

12. The kit of claim 6 , wherein the pharmaceutical combination comprises
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
or a physiologically acceptable salt thereof.

13. The pharmaceutical composition of claim 7 , wherein the pharmaceutical combination comprises
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
or a physiologically acceptable salt thereof.

14. The method of claim 8 , wherein the pharmaceutical combination comprises
2-amino-N-[7-methoxy-8-(3-morpholin-4-ylpropoxy)-2,3-dihydroimidazo[1,2-c]quinazolin-5-yl]pyrimidine-5-carboxamide
or a physiologically acceptable salt thereof.

Assignees

• Bayer Pharma AG

Inventors

• Liu Ningshu

Classifications

• A61P43/00

  Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 · CPC title

• A61P35/04

  specific for metastasis · CPC title

• A61P35/00

  Antineoplastic agents · CPC title

• A61K51/02

  characterised by the carrier {, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus} · CPC title

• A61K51/04

  Organic compounds · CPC title