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

TW202626654APending Publication Date: 2026-07-01BOEHRINGER INGELHEIM INT GMBH
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Patent Information

Application Number
TW114152254
Authority / Receiving Office
TW · TW
Patent Type
Applications
Current Assignee / Owner
Priority Date
2020-04-24
Filing Date
2021-04-07
Publication Date
2026-07-01
Estimated Expiration
2041-04-06
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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.
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Claims

1. A pharmaceutical composition comprising a therapeutically effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof, and one or more pharmaceutically acceptable excipients, wherein R1 is selected from the group consisting of hydrogen, -CH3, -CCH, -OCH3 and halogens; R2 is hydrogen or a halogen; R3 is selected from the group consisting of formulas (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. The pharmaceutical composition of claim 1, wherein R1 is selected from the group consisting of -CH3, -CCH, -OCH3 and halogens.

3. The pharmaceutical composition of claim 1, wherein R1 is -CH3.

4. The pharmaceutical composition of claim 1, wherein R1 is -CCH.

5. The pharmaceutical composition of claim 1, wherein R1 is -OCH3.

6. The pharmaceutical composition of claim 1, wherein R1 is chlorine.

7. The pharmaceutical composition of claim 1, wherein R1 is fluorine.

8. The pharmaceutical composition of claim 1, wherein R2 is hydrogen.

9. The pharmaceutical composition of claim 1, wherein R2 is chlorine.

10. The pharmaceutical composition of claim 1, wherein the compound is selected from the group consisting of examples I-01 to I-19; 11. A pharmaceutical composition comprising a compound having the following structure, I-01.

12. A pharmaceutical composition comprising a pharmaceutically acceptable salt of a compound having the following structure, I-01.