Claims for Patent: 11,608,343

Summary for Patent: 11,608,343

Title:	Substituted pyrimido[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 and R4 have 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.
Inventor(s):	Birgit Wilding, Dietrich BOESE, Harald Engelhardt, Julian Fuchs, Ralph NEUMUELLER, Mark PETRONCZKI, Dirk Scharn, Matthias Treu
Assignee:	Boehringer Ingelheim International GmbH
Application Number:	US17/223,132
Patent Claims:	1. A compound of Formula (I): or a pharmaceutically acceptable salt or stereoisomer thereof, wherein: R1 H, halogen, CH3, C≡CH, or OCH3; R2 is H or halogen; R3 is formula (i.1), formula (i.2), formula (i.3), or formula (i.4): R4 is R4.a or R4.b; Q is a 4- to 6-membered heterocyclyl, wherein the 4- to 6-membered heterocyclyl contains one nitrogen heteroatom, and further wherein one carbon atom of the 4- to 6-membered heterocyclyl is optionally substituted with CH3; Z is a 4- to 6-membered heterocyclyl, wherein the 4- to 6-membered heterocyclyl contains one nitrogen heteroatom, and further wherein one carbon atom of the 4- to 6-membered heterocyclyl is optionally substituted with CH3; and R5 is H or CH3; with the proviso that at least one of R1 and R2 is not H. 2. The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is halogen, CH3, C≡CH, or OCH3. 3. The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is F. 4. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is Cl. 5. The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is CH3. 6. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is C≡CH. 7. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R1 is OCH3. 8. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R2 is H. 9. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R2 is Cl. 10. A The compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, wherein R4 is R4.a or R4.b: wherein: R4.a is R4.a.1 wherein: R6 is H or CH3; m is 1 or 2; and n is 1 or 2; and R4.b is R4.b.1: wherein: p is 1 or 2; and q is 1 or 2. 11. The compound according to claim 1, or a stereoisomer thereof, wherein the compound, or stereoisomer thereof, is selected from the group consisting of: or a pharmaceutically acceptable salt thereof. 12. A pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof. 13. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof, and a pharmaceutically active substance selected from the group consisting of a cytostatic active substance and a cytotoxic active substance. 14. A method for treating cancer in a patient, wherein the method comprises administering to the patient in need thereof a therapeutically effective amount of a compound according to claim 1, or a pharmaceutically acceptable salt or stereoisomer thereof; wherein the cancer is selected from the group consisting of biliary cancer, bladder cancer, brain cancer, breast cancer, cervical cancer, colorectal cancer, endometrial cancer, an esophagus tumor, a gallbladder tumor, gastrointestinal cancer, a head and neck tumor, kidney cancer, liver cancer, lung cancer, prostate cancer, and skin cancer. 15. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 16. A compound having the following structure: 17. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 18. A compound having the following structure: 19. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 20. A compound having the following structure: 21. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 22. A compound having the following structure: 23. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 24. A compound having the following structure: 25. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 26. A compound having the following structure: 27. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 28. A compound having the following structure: 29. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 30. A compound having the following structure: 31. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 32. A compound having the following structure: 33. A compound having the following structure: or a pharmaceutically acceptable salt thereof. 34. A compound having the following structure: