DK3022192T3 - Piperidinylindolderivater og deres anvendelse som komplement faktor B inhibitorer - Google Patents
Piperidinylindolderivater og deres anvendelse som komplement faktor B inhibitorer Download PDFInfo
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- DK3022192T3 DK3022192T3 DK14744744.5T DK14744744T DK3022192T3 DK 3022192 T3 DK3022192 T3 DK 3022192T3 DK 14744744 T DK14744744 T DK 14744744T DK 3022192 T3 DK3022192 T3 DK 3022192T3
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- methyl
- indol
- methoxy
- piperidin
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Claims (20)
1. Forbindelse eller salt eller tautomer deraf ifølge formel I:
hvor n er 0, 1 eller 2; R er hydrogen, Ci-C4alkyl eller hydroxyCi-C4alkyl; R1 er halogen, hydroxy, CrCealkyl, C2-Cealkenyl, C3-C6cycloalkyl, Ci-C6alkoxy, halogenCrCealkyl, hydroxyCrCealkyl, aminoCi-C6alkyl, CrCealkoxyCrCealkyl, CrCealkoxyCi-Cealkoxy, Cs-CecycloalkyCrCealkoxy, halogenCrCealkoxy, -S(0)pCi-Cealkyl, -CH2NHC(0)Ci-C4alkyl eller -0CH2C(0)R7, p er 0, 1 eller 2; R2 er CrCealkyl, CrCealkoxy, hydroxyCrCealkyl eller halogen; R3 er hydrogen, halogen, cyano, Ci-C4alkyl, halogenCi-C4alkyl, -CH2C(0)R7, phenyl eller 5 eller 6 leddet heteroaryl med 1,2 eller 3 ringheteroatomer uafhængigt valgt blandt N, O eller S, hvor phenylet eller heteroarylet eventuelt er substitueret med 0, 1 eller 2 CrC4alkylgrupper, og hvor alkyl og halogenalkyl eventuelt er substitueret med 0 eller 1 hydroxy; R4 er phenyl, naphthyl eller heteroaryl, hvor heteroarylet er en fem eller seks leddet heteroaryl med 1,2 eller 3 ringheteroatomer uafhængigt valgt blandt N, O eller S, og hvor phenylet eller heteroarylet eventuelt er substitueret med R5 og yderligere substitueret med 0 eller 1 substituenter valgt blandt halogen, Ci-C4alkyl, Ci-C4alkoxy, hydroxy CrC4alkyl, hydroxy og cyanomethyl; R5 er -C(0)R8, -CH2C(0)R8, R9, -C(0)NHS02Ci-C4alkyl, -S02NHC(0)Ci-C4alkyl, -S02N(H)m(Ci-C4alkyl)2-m, -S02Ci-C4alkyl, cyano, halogen, hydroxyCi-C4alkyl og 5 leddet heteroaryl med 1-4 ringnitrogenatomer og 0 eller 1 ringsvovl eller-oxygenatomer; m er 0, 1 eller 2; W er O eller C(R6)2; R6 er uafhængigt valgt ved hver forekomst fra gruppen bestående af hydrogen, hydroxy, amino, mono- og di- Ci-C4alkylamino, Ci-C4alkyl, hydroxyCi-C4alkyl, cyanoCi-C4alkyl eller Ci-C4alkoxy; eller C(R6)2, taget i kombination, danner en spirocyclisk carbocyclus med 3 til 6 ringatomer; R7 er hydroxy, Ci-C4alkoxy, amino eller mono- og di-Ci-C4alkylamino; R8 er hydroxy, Ci-C4alkoxy, amino eller en 5 til 7 leddet mættet heterocyclus med 1, 2 eller 3 ringheteroatomer uafhængigt valgt blandt N, O eller S; eller R8 er mono- og di-Ci-C4alkylamino, som er usubstitueret eller substitueret med halogen, hydroxy eller Ci-C4alkyl; og R9 er en 5 leddet heteroaryl med 1 til 4 ringnitrogenatomer og 0 eller 1 ringoxygen eller -svovlatomer, hvilken heterocyclus eventuelt er substitueret med 0 til 2 Ci-C4alkylgrup-per.
2. Forbindelse ifølge krav 1 eller salt eller tautomer deraf, hvor n er 1.
3. Forbindelse ifølge enten krav 1 eller krav 2 eller et salt eller tautomer deraf, hvor W erCHR6 eller C(CH3)R6.
4. Forbindelse ifølge ethvert af kravene 1 til 3 eller salt eller tautomer deraf, hvor R1 er Ci-C4alkyl, CrC4alkoxy eller cyclopropyl.
5. Forbindelse ifølge ethvert af kravene 1 til 4 eller salt eller tautomer deraf, hvor R2 er methyl.
6. Forbindelse ifølge ethvert af kravene 1 til 5 eller salt eller tautomer deraf, hvor R3 er hydrogen, halogen eller Ci-C4alkyl.
7. Forbindelse ifølge ethvert af kravene 1 til 6 eller salt eller tautomer deraf, hvor R3 er hydrogen.
8. Forbindelse ifølge ethvert af kravene 1 til 7 eller salt eller tautomer deraf, ifølge formel Ila eller llb:
9. Forbindelse ifølge ethvert af kravene 1 til 8 eller salt eller tautomer deraf, ifølge formel Illa eller I Mb:
hvor X er N eller CH.
10. Forbindelse ifølge ethvert af kravene 1 til 8 eller salt eller tautomer deraf, hvor R4 er pyridin-3-yl, som er substitueret para- til piperidinringen med R5.
11. Forbindelse ifølge ethvert af kravene 1 til 8 eller salt eller tautomer deraf, hvor R4 er phenyl substitueret para- til piperidinringen med R5 og eventuelt substitueret med fluor, methoxy, hydroxymethyl eller hydroxy.
12. Forbindelse ifølge krav 11 eller salt eller tautomer deraf, hvor R4 er phenyl substitueret para- til piperidinringen med R5.
13. Forbindelse ifølge ethvert af kravene 1 til 12 eller salt eller tautomer deraf, hvor R5 er CO2H, CONH2, SO2NH2 eller tetrazolyl.
14. Forbindelse ifølge krav 1 eller salt eller tautomer deraf, hvilken forbindelse er valgt fra gruppen bestående af 1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-2-phenylpiperidin-4-ol; 4-((4-methoxy-2-phenylpiperidin-1-yl)methyl)-5,7-dimethyl-1/-/-indol; 5.7- dimethyl-4-((2-phenylpiperidin-1-yl)methyl)-1/-/-indol; 1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-2-phenyl-piperidin-4-yl)methanol; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzensulfonamid; 3- (1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzensulfonamid; 4- (1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-/V-methylbenzensulfonamid; 3- (1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-/V-methylbenzensulfonamid; 4- ((2-(4-fluorphenyl)-4-methoxypiperidin-1-yl)methyl)-5,7-dimethyl-1/-/-indol; (1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-2-phenylpiperidin-2-yl)methanol; (4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)methanol; 5.7- dimethyl-4-((2-(4-(methylsulfonyl)phenyl)piperidin-1-yl)methyl)-1/-/-indol; 4-((2-(4-(2H-tetrazol-5-yl)phenyl)piperidin-1-yl)methyl)-5,7-dimethyl-1/-/-indol; 1-((5,7-dimethyl-1H-indol-4-yl)methyl)-2-phenylpiperidin-4-amin; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzamid; 4-(1-((5-chlor-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzamid; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-4-methoxypiperidin-2-yl)benzamid; 4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4-methylpiperidin-2-yl)benzamid; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-4-hydroxypiperidin-2-yl)benzoesyre; 4-(1-((5-chlor-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; methyl 4-(1 -((5,7-dimethyl-1/-/-indol-4-yl)methyl)-4-methoxypiperidin-2-yl)benzoat; 4-(1-((5-cyclopropyl-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)-2-fluorbenzoesyre; 4- (1-((5-cyclopropyl-7-methyl-1H-indol-4-yl)methyl)pyrrolidin-2-yl)benzoesyre; 5- (1-((5-cyclopropyl-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)picolinsyre; 4-(1-((5-cyclopropyl-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)-3-methoxy-benzoesyre; 4- (1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 5- methoxy-7-methyl-4-((2-(pyridin-4-yl)piperidin-1-yl)methyl)-1/-/-indol; 5-methoxy-7-methyl-4-((2-(pyridin-3-yl)piperidin-1-yl)methyl)-1/-/-indol; 3- fluor-4-(1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4- (4-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)morpholin-3-yl)benzoesyre; 6-(1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)nicotinsyre; 4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4-propoxypiperidin-2-yl)benzoesyre; 4-(4-hydroxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-3-methylbenzoesyre; 4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-5-methylpiperidin-2-yl)benzoesyre; 4- (1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4-ethylpiperidin-2-yl)benzoesyre; 2-(4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)acetatsyre; 2-(3-(1 -((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)acetatsyre; 5- (1-((5-cyclopropyl-7-methyl-1H-indol-4-yl)methyl)-4-methoxypiperidin-2-yl)picolin-syre; 2-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)thiazol-4-carboxylsyre; 2- (1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)-4-methylthiazol-5-carboxylsyre; 3- (1 -((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4- (1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)azepan-2-yl)benzoesyre; 4-((2-(4-(1 W-pyrazol-4-yl)phenyl)piperidin-1-yl)methyl)-5-methoxy-7-methyl-1/-/-indol; 4-((2-(4-(1/-/-pyrazol-3-yl)phenyl)piperidin-1-yl)methyl)-5-methoxy-7-methyl-1/-/-indol; 4-(1-«5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-1-naphthoesyre; 1- (2,2,2-trifluor-1-(5-methoxy-7-methyl-1/-/-indol-4-yl)ethyl)piperidin-2-yl)benzoesyre; 2- methoxy-4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 2-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-2-phenylpiperidin-4-yl)acetonitril; 4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4-methylpiperidin-2-yl)benzoesyre; 4- (4-methoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 5- (4-ethoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)picolinsyre; 4-(1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4,4-dimethylpiperidin-2-yl)benzoe-syre; 4-(4-ethoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzonitril; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4-((4-ethoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4-(1 -((5,7-dimethyl-1/-/-indol-4-yl)methyl)-4-methoxypiperidin-2-yl)benzoesyre; 4-(1 -((5,7-dimethyl-1H-indol-4-yl)methyl)-4-ethoxypiperidin-2-yl)benzoesyre; 4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)-4-ethoxypiperidin-2-yl)benzoesyre; 4-(1-((5-cyclopropyl-7-methyl-1/-/-indol-4-yl)methyl)-4-methoxypiperidin-2-yl)benzoe- syre; 4-(1-((5-cyclopropyl-7-methyl-1/-/-indol-4-yl)methyl)-4-ethoxypiperidin-2-yl)benzoesyre; 4-(1-((5-cyclopropyl-7-methyl-1H-indol-4-yl)methyl)-4-ethoxypiperidin-2-yl)benzoesyre; 4-(5-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4-(5-methoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzamid; 4-(5-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 4-(5-hydroxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; 1-((5,7-dimethyl-1H-indol-4-yl)methyl)-/V-methyl-2-phenylpiperidin-4-arriin; (4-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)methanamin; (4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)-methanol; 4-((2-(3-(2H-tetrazol-5-yl)phenyl)piperidin-1-yl)methyl)-5,7-dimethyl-1H-indol; 3- (1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzamid; (3-(1-((5,7-dimethyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)methanol; (4-((2-(4-(1 H-tetrazol-5-yl)phenyl)-4-ethoxypiperidin-1-yl)methyl)-5-methoxy-7-methyl-1 /-/-indol; 4- (4-ethoxy-1-((5-methoxy-7-methyl-1H-indol-4-yl)methyl)piperidin-2-yl)-/V-(methylsul-fonyl)benzamid; 4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-A/-methyl- benzamid; 4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-/V,/V-di- methylbenzamid; (4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)- (morpholino)methanon; /V-(2-hydroxyethyl)-4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)- piperidin-2-yl)benzamid; 4-(4-methoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)-/V-(2- methoxyethyl)benzamid; A/-((4-(1-((5-cyclopropyl-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)phenyl)sulfonyl)- acetamid; 4-(6-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-6-azaspiro[2.5]octan-5-yl)benzoesyre; 4-ethyl-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre; ethyl 4-((2S,4R)-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)-4-methylpiperidin-2-yl)benzoat; ethyl 4-((2S,4S)-4-ethoxy-1 -((5-methoxy-7-methyl-1 /-/-indol-4-yl)methyl)piperidin-2-yl)benzoat og salte, stereoisomerer og tautomerer deraf.
15. Forbindelse ifølge krav 1, som er 4-((2S,4S)-4-ethoxy-1-((5-methoxy-7-methyl-1/-/-indol-4-yl)methyl)piperidin-2-yl)benzoesyre eller et farmaceutisk acceptabelt salt deraf.
16. Farmaceutisk sammensætning omfattende ét eller flere farmaceutisk acceptable bærestoffer og en terapeutisk effektiv mængde af en forbindelse ifølge ethvert af kravene 1 til 15.
17. Kombination, især en farmaceutisk kombination, omfattende en terapeutisk effektiv mængde af forbindelsen ifølge ethvert af kravene 1-15 og et andet terapeutisk aktivt middel.
18. Forbindelse ifølge ethvert af kravene 1-15 til anvendelse som et lægemiddel.
19. Forbindelse ifølge ethvert af kravene 1-15 til anvendelse ved behandling af en lidelse eller sygdom i et subjekt, som medieres ved aktivering af komplementsystemet eller aktiveringen af den alternative vej for komplementsystemet.
20. Forbindelse ifølge krav 1 til 15 til anvendelse ved behandlingen af aldersrelateret makulær degeneration, geografisk atropi, diabetisk retinopati, uveitis, retinitis pigmentosa, makular ødem, Behcet's uveitis, multifokal choroiditis, Vogt-Koyangi-Harada syndrom, uveitis imtermedia, birdshot retino-chorioditis, sympatisk ophthalmi, okular dicatricial pemphigoid, okular pemphigus, nonartertisk iskæmisk optisk neuro-pati, post-operativ inflammation, retinal veneokklusion, neurologiske lidelser, multipel sclerose, slagtilfælde, Guillain Barre syndrom, traumatisk hjerneskade, Parkinson's sygdom, lidelser med upassende eller uønskede komplementaktivering, hæmodialyse-komplikationer, hyperakut allograft afstødning, xenograft afstødning, interleukin-2 induceret toksicitet under IL-2 terapi, inflammatoriske lidelser, inflammation ved autoimmunsygdomme, Crohn's sygdom, voksen åndenødssyndrom, myocarditis, post-iskæmisk reperfusionstilstande, myocardial infarkt, ballonangioplasti, post-pump-syndrom ved kardiopulmonær bypass eller nyre bypass, atherosclerose, hæmo-dialyse, nyreiskæmi, mesenterial arterie reperfusion efter aortarekonstruktion, infektionslidelser eller sepsis, immunkomplekslidelser og autoimmunsygdomme, rheumatoid arthritis, systemisk lupus erythematosus (SLE), SLE nephritis, proliferativ nephritis, leverfibrose, hæmolytisk anæmi, myasthenia gravis, vævsregeneration, neural regeneration, dyspnø, hæmoptysis, ARDS, astma, kronisk obstruktiv pulmonær lidelse (COPD), emphysema, pulmonær embolisme og infarkt, pneumoni, fibrogene støvlidelser, pulmulær fibrose, astma, allergi, bronchokonstriktion, hypersensitivitet pneumonitis, parasitiske sygdomme, Goodpasture's syndrom, pulmonær vasculitis, Pauci-immun vasculitis, immunkompleks-associeret inflammation, antiphospholipid-syndrom, glomerulonephritis og obesitas.
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