[1,3]diazino[5,4-d]pyrimidines as her2 inhibitors

Abstract

The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) wherein the groups R1, R2, R3 andR4have the meanings given in the claims and specification, their use as inhibitors of HER2 and its mutants, pharmaceutical compositions which contain such compounds and their use as medicaments, especially as agents for treatment and / or prevention of oncological diseases.

Claims

1. Use of a compound of formula (I) or a pharmaceutically acceptable salt thereof for the preparation of a medicament for the treatment and / or prevention of cancer, tumor or carcinoma of the lung, wherein R1 is selected from the group consisting of hydrogen, -CH3, -CCH, -OCH3 and halogen; R2 is hydrogen or halogen; R3 is selected from the group consisting of (i.1), (i.2), (i.3) and (i.4); R4 is selected from the group consisting of R4.a and R4.b, wherein R4.a is R4.a.1, wherein R6 is H or CH3, n is 1 or 2, m is 1 or 2; and R4.b is R4.b.1, wherein p is 1 or 2, q is 1 or 2; R5 is H or CH3; and at least one of R1 and R2 is not hydrogen.

2. As requested in item 1, wherein R1 is selected from the group consisting of -CH3, -CCH, -OCH3 and halogens.

3. As requested in item 1, where R1 is -CH3.

4. As requested in item 1, where R1 is -CCH.

5. As requested in item 1, where R1 is -OCH3.

6. As requested in item 1, wherein R1 is chlorine.

7. As requested in item 1, wherein R1 is fluorine.

8. As requested in item 1, wherein R2 is hydrogen.

9. As requested in item 1, wherein R2 is chlorine.

10. As claimed in claim 1, wherein the compound or a pharmaceutically acceptable salt thereof is selected from the group consisting of examples I-01 to I-19; 11. Use of a compound having the following structure for the preparation of a medicament for the treatment and / or prevention of lung cancer, tumors or carcinomas, I-01.

12. Use of a pharmaceutically acceptable salt of a compound having the following structure for the preparation of a medicament for the treatment and / or prevention of cancer, tumor or carcinoma of the lung, I-01.

13. For any of the uses of claims 1 to 12, wherein the cancer, tumor or carcinoma of the lung is non-small cell lung cancer (NSCLC).

14. For any of the uses of claims 1 to 12, wherein the cancer has HER2 overexpression and / or amplification.

15. For the purposes of any of claims 1 to 12, wherein the cancer is a HER2 exon 20 mutant cancer.