DK3001903T3 - 1h-pyrazolo[3,4-?]pyridiner og terapeutiske anvendelser deraf - Google Patents
1h-pyrazolo[3,4-?]pyridiner og terapeutiske anvendelser deraf Download PDFInfo
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- DK3001903T3 DK3001903T3 DK15174246.7T DK15174246T DK3001903T3 DK 3001903 T3 DK3001903 T3 DK 3001903T3 DK 15174246 T DK15174246 T DK 15174246T DK 3001903 T3 DK3001903 T3 DK 3001903T3
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- alkyl
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Claims (14)
1. Forbindelse eller farmaceutisk acceptabelt salt deraf med strukturen ifølge formel Ib:
hvor: R1, R2, R3, R5, R6 og R8 er valgt uafhængigt fra gruppen, der består af H, Ci-galkyl, halid, -CF3, - (Ci-galkyl) ncarbocyclyl-R12, - (Ci-galkyl) nheterocyclyl-R12, - (Ci-galkyl) naryl-R12, — (Ci- galkyl) nheteroaryl-R12, - (Ci-galkyl) n0R9, - (Ci-galkyl) nSR9, — (Ci- 9alkyl)nS (=0)R10, - (Ci-galkyl) nS02R9, - (Ci-galkyl) n (R9) SO2R9, - (Ci- galkyl) nS02N (R9) 2, - (Ci-gal kyl) nN (R9) 2, - (Ci- galkyl) nN (R9) C (=A) N (R9) 2, - (Ci-galkyl) nC (=A) N (R9) 2, - (Ci- galkyl) nN (R9) C (=A) R9, - (Ci-galkyl) nN (R9) C (=A) CH (R9) 2, -NO2, -CN, - (Ci-galkyl) nC02R9 og - (Ci-galkyl) nC (=A) R9; alternativt en af hver af R1 og R2, R2 og R3 eller R5 og R6 sammen danner en ring, der er valgt fra gruppen, der består af aryl, heteroaryl,
hvor hver binding som vist ved en stiplet og ubrudt linje er en binding valgt fra gruppen, der består af en enkeltbinding og en dobbeltbinding; hver R9 er valgt uafhængigt fra gruppen, der består af H, Ci-galkyl, -CF3, - (Ci-galkyl) ncarbocyclyl, - (Ci-galkyl) nheterocyclyl, - (Ci-galkyl) naryl og - (Ci-galkyl) nheteroaryl; alternativt to tilstødende R9 sammen med atomerne, hvortil de er bundet, kan danne en carbocyclyl eller heterocyclyl; hver R10 er valgt uafhængigt fra gruppen, der består af Ci-galkyl, -CF3, - (Ci-galkyl) ncarbocyclyl, - (Ci-galkyl) nheterocyclyl, - (Ci-galkyl) naryl og - (Ci-galkyl) nheteroaryl; hver R11 er valgt uafhængigt fra gruppen, der består af -OR9 og R9; hver R12 er 1-5 substituenter, der hver er valgt fra gruppen, der består af H, Ci-galkyl, halid, -CF3, carbocyclyl, heterocyclyl, aryl, heteroaryl, - (Ci-galkyl) n0R9, — (Ci- 9alkyl)nSR9, - (C1-gal kyl) nS (=0) R10, - (Ci-galkyl) nS02R9, - (Ci- galkyl) nN (R9) SO2R9, - (Ci-galkyl) nS02N (R9) 2, - (Ci-galkyl) nN (R9) 2, - (Ci-gal kyl) nN (R9) C (=A) N (R9) 2, - (Ci-gal kyl) nC (=A) N (R9) 2, - (Ci- 9alkyl)nN(R9)C(=A)R9, - (Ci-galkyl) nN (R9) C (=A) CH (R9) 2, -NO2, -CN, - (Ci-galkyl) nC02R9 og - (Ci-galkyl) nC (=A) R9; R14 og R15 er valgt uafhængigt fra gruppen, der består af H, Ci-galkyl, halid, -CF3, - (Ci-galkyl) ncarbocyclyl-R12, — (Ci- 9alkyl) nheterocyclyl-R12, - (Ci-9alkyl) naryl-R12, — (Ci- 9alkyl) nheteroaryl-R12, - (Ci-9alkyl) n0R9, - (Ci-9alkyl) nSR9, — (Ci- galkyl) nS (=0) R10, - (Ci-9alkyl) nS02R9, - (Ci-9alkyl) nN (R9) S02R9, - (Ci- galkyl) nS02N (R9) 2, - (Ci-9alkyl) nN (R9) 2, - (Ci- galkyl) nN (R9) C (=A) N (R9) 2, - (Ci-9alkyl) nC (=A) N (R9) 2, - (Ci- 9alkyl) nN (R9) C (=A) R9, - (Ci-galkyl) nN (R9) C (=A) CH (R9) 2, -N02, -CN, - (Ci-9alkyl) nC02R9 og - (Ci-9alkyl) nC (=A) R9; alternativt R14 og R15 sammen danner en ring, der er valgt fra gruppen, der består af benzen og pyridin; hver A er valgt uafhængigt blandt 0, S og NR11; Y1, Y2 og Y4 er C; Y1 2 er nitrogen, og R7 er fraværende; og hver n er 0 eller 1.
2. Forbindelse ifølge krav 1, hvor R1 og R3 er H, og R2 er valgt fra gruppen, der består af -carbocyclyl-R12, heterocyclyl-R12, -aryl-R12 og -heteroaryl-R12.
3. Forbindelse ifølge krav 2, hvor R2 er -heteroaryl-R12, og heteroaryl er pyridin.
4. Forbindelse ifølge krav 3, hvor R12 er valgt fra gruppen, der består af -NHC (=0) N (R9) 2, -C (=0) N (R9) 2, -NHC(=0)R9, NHC (=0) CH (R9) 2 og -NHS02R9. 1 Forbindelse ifølge krav 4, hvor R9 er valgt fra gruppen, 2 der består af H, -Ci-4alkyl, carbocyclyl og -heterocyclyl.
6. Forbindelse ifølge et hvilket som helst af kravene 1-5, hvor R6 og R8 er H, og R5 er valgt fra gruppen, der består af H, -heterocyclyl-R1, -aryl-R1, -heteroaryl-R1, N (R9) C (=0)N (R9) 2, -C (=0)N (R9) 2, -N (R9) C (=0) R9, -N (R9) C (=0) CH (R9) 2, -CN,-C02R9 og -C(=0)R9.
7. Forbindelse ifølge krav 6, hvor R5 er valgt fra gruppen, der består af -heterocyclyl-R1, -aryl-R1 og -heteroaryl-R1.
8. Forbindelse ifølge krav 7, hvor heteroaryl er pyridin.
9. Forbindelse ifølge et hvilket som helst af krav 7 eller 8, hvor R1 er valgt fra gruppen, der består af H og halid.
10. Forbindelse ifølge krav 6, hvor R5 er valgt fra gruppen, der består af H, -C(=0)N(R9)2 og -CN.
11. Forbindelse ifølge krav 10, hvor R9 er valgt fra gruppen, der består af H og -Ci-4alkyl, alternativt R9 sammen med nitrogen danner en fusioneret ring. 1 Forbindelse ifølge krav 1, der har en struktur valgt fra gruppen, der består af:
og
eller et farmaceutisk acceptabelt salt deraf.
13. Farmaceutisk sammensætning, der omfatter en forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf og et farmaceutisk acceptabelt excipiens.
14. Forbindelse ifølge et hvilket som helst af kravene 1 til 12 til anvendelse i medicin.
15. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf til anvendelse til behandling af en forstyrrelse eller sygdom, hvor forstyrrelsen eller sygdommen er valgt fra gruppen, der består af lungefibrose, rheumatoid arthritis, psoriasis, en knogle- eller brusksygdom, osteoarthritis og cancer.
16. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf til anvendelse til behandling af en forstyrrelse eller sygdom, hvor forstyrrelsen eller sygdommen er valgt blandt: polyposis coli, retinal angiogenese, odonto-onyko-dermal dysplasi, Wilms tumor, skeletdysplasi og fokal dermal hypoplasi.
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