RU-2026105123-A - SUBSTITUTED BICYCLIC HETEROCYCLIC INHIBITORS YAP-TEAD AND/OR TAZ-TEAD

Inventors

• ХАЙНРИХ Тимо
• УНСУЭ ЛОПЕС Андреа
• ГУНЕРА Якуб
• Бургдорф Ларс
• АЛЬБЕРС Лиза
• ГАМБАРДЕЛЛА Алессия
• ПЕТЕРССОН Карл

Assignees

• МЕРК ПАТЕНТ ГМБХ

Dates

Publication Date

20260507

Application Date

20240730

Priority Date

20230802

Claims (20)

1. 1. Compound of formula I
2. I,
3. Where
4. X 1 means N or CR X1 ;
5. R X1 is H, halogen, straight-chain or branched C 1-4 -alkyl, which is unsubstituted or substituted independently of each other by 1, 2 or 3 halogen atoms, and/or OH;
6. R 1 is halogen, -NH 2 , -CN, straight-chain or branched C 1-4 -alkyl, which is unsubstituted or substituted independently of each other by 1, 2 or 3 halogen atoms;
7. R 2 means H, Alk 2 , Ar 2 , Hetar 2 , Cyc 2 , Hetcyc 2 , -L 2 -Ar 2a , -S(=O) 2 R f ;
8. R 3 is H, -CN, -C(=O)-NH 2 or halogen;
9. A is 1,3-phenylene or a monocyclic divalent heteroaryl with 5 or 6 ring atoms, wherein 1, 2 or 3 of said ring atoms is/are a heteroatom(s) selected from N, O and/or S, and the remaining atoms are carbon atoms, wherein said 1,3-phenylene or monocyclic heteroaryl bears a bicyclic ring system of a compound of formula I in the 1-position and said L 1 -B radical of the compound of formula I in the 3-position relative to this bicyclic ring system, wherein each of said 1,3-phenylene or monocyclic heteroaryl may additionally be unsubstituted or mono- or disubstituted, independently of one another, by halogen, straight-chain or branched C 1-4 -alkyl, OC 1-4 -alkyl, SC 1-4 -alkyl, C 3-7 -cycloalkyl, OC 3-7 -cycloalkyl or SC 3-7 -cycloalkyl, wherein C 1-4 -alkyl, OC 1-4 -alkyl, SC 1-4 -alkyl, C 3-7 -cycloalkyl, OC 3-7 -cycloalkyl or SC 3-7 -cycloalkyl is unsubstituted or substituted by 1, 2 or 3 halogen atoms;
10. B means Ar 1 , Hetar 1 , Cyc 1 , Hetcyc 1 ;
11. L 1 means -O-, -S-, -N(R 4 )-, -O-CH 2 -, -O-CH(R 5 )-, -O-SO 2 -, -N(R 6 )-CH 2 -, -N(R 6 )-C(=O)-, -CH 2 -, -CH(R 7 )-, -CH 2 CH 2 -, -CH 2 -O-;
12. R 4 is H, straight-chain or branched C 1-6 -alkyl;
13. R 5 , R 6 , R 7 independently of each other denote straight-chain or branched C 1-6 -alkyl;
14. L 2 means the divalent group -S(=O) 2 -;
15. Alk 2 is a straight-chain or branched C 1-6 -alkyl, C 2-6 -alkenyl or C 2-6 -alkynyl, each of which may be unsubstituted or substituted independently of one another by R 2a1 , R 2a2 and/or R 2a3 ;
16. Ar 1 means mono- or bicyclic aryl with 5, 6, 7, 8, 9, 10 ring carbon atoms, wherein said aryl is substituted independently of each other by R C1 , R C2 and/or R C3 ;
17. Ar a , Ar 2 , Ar 2a independently of one another denote mono- or bicyclic aryl with 5, 6, 7, 8, 9, 10 ring carbon atoms, wherein said aryl may be unsubstituted or substituted independently of one another by R B1 , R B2 , R B3 , R B4 and/or R B5 ;
18. Hetar 1 means a mono- or bicyclic heteroaryl with 5, 6, 7, 8, 9, 10, 11, 12 ring atoms, where 1, 2, 3, 4, 5 of said ring atoms are(are) heteroatom(s) selected from N, O and/or S, and the remaining atoms are carbon atoms, where said heteroaryl is substituted independently of each other by R C1 , R C2 and/or R C3 ;
19. Hetar a , Hetar 2 , Hetar 2a independently of one another mean mono- or bicyclic heteroaryl with 5, 6, 7, 8, 9, 10, 11, 12 ring atoms, where 1, 2, 3, 4, 5 of said ring atoms are(are) heteroatom(s) selected from N, O and/or S, and the remaining atoms are carbon atoms, where said heteroaryl is unsubstituted or substituted independently of one another by R B1 , R B2 , R B3 , R B4 and/or R B5 ;
20. Cyc 1 means a saturated or partially unsaturated, mono-, bi- or tricyclic carbocycle with 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15 ring carbon atoms, wherein said carbocycle may be unsubstituted or substituted independently of each other by R C6 , R C7 , R C8 , R C9 , R C10 and/or R C11 ;