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DK3207043T3 - Dihydropyrrolopyridin-inhibitorer af ror-gamma - Google Patents

Dihydropyrrolopyridin-inhibitorer af ror-gamma Download PDF

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Publication number
DK3207043T3
DK3207043T3 DK15785013.2T DK15785013T DK3207043T3 DK 3207043 T3 DK3207043 T3 DK 3207043T3 DK 15785013 T DK15785013 T DK 15785013T DK 3207043 T3 DK3207043 T3 DK 3207043T3
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mixture
mmol
tert
disease
compound
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DK15785013.2T
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DK3207043T6 (da
Inventor
David A Claremon
Lawrence Wayne Dillard
Chengguo Dong
Yi Fan
Lanqi Jia
Stephen D Lotesta
Andrew Marcus
Suresh B Singh
Colin M Tice
Jing Yuan
Wei Zhao
Yajun Zheng
Linghang Zhuang
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Vitae Pharmaceuticals Inc
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Claims (17)

1. Forbindelse med formlen:
eller et farmaceutisk acceptabelt salt deraf, hvor R2 er (Ci-C3)alkyl, hydroxy(Ci-C3)alkyl, halo(Ci-C3)alkyl, benzyl, (Ci-C3)alkoxy(Ci-C3)alkyl, tetrahydropyranyl, eller -CH2-tetrahydropyranyl; R3 og R4 er hver uafhængigt hydrogen eller methyl; Cy1 er phenyl eller pyridyl, hver substitueret med (Ci-C3)alkylsulfonyl; og Cy2 er hydrogen, halo(Ci-C3)alkyl, cyclohexyl, eller tetrahydropyranyl, hvor cyclohexyl og tetrahydropyranyl hver eventuelt er substitueret med en eller flere grupper valgt fra halo(Ci-C3)alkyl og Ci-C3(alkoxy).
2. Forbindelse ifølge krav 1, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
3. Forbindelse ifølge krav 1 eller 2, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
4. Forbindelse ifølge et hvilket som helst af kravene 1 til 3, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse ifølge et hvilket som helst af kravene 1 til 4, hvor Cy2 er cyclohexyl eller tetrahydropyranyl, hvoraf hver eventuelt er substitueret med en eller flere grupper valgt fra halo(Ci-C3)alkyl og Ci-C3(alkoxy).
6. Forbindelse ifølge et hvilket som helst af kravene 1 til 5, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf, hvor X er CH eller N; Y1 er O og Y2 er CH2, Y1 er CH2 og Y2 er O, eller Y1 og Y2 hver er CH2; R9 er halo(Ci-C3)alkyl; og R10 er (Ci-C3)alkylsulfonyl.
7. Forbindelse ifølge et hvilket som helst af kravene 1 til 6, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
8. Forbindelse ifølge et hvilket som helst af kravene 1 til 7, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge et hvilket som helst af kravene 1 til 8, hvor R2 er methyl, ethyl, benzyl eller isopropyl.
10. Forbindelse ifølge et hvilket som helst af kravene 1 til 9, hvor R2 er ethyl eller isopropyl.
11. Forbindelse ifølge et hvilket som helst af kravene 6 til 10, hvor R9 er CF3; og R10 er SOzEt eller SOzMe.
12. Forbindelse ifølge krav 1, hvor forbindelsen er valgt fra
eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelse ifølge krav 1, hvor forbindelsen har formlen:
eller et farmaceutisk acceptabelt salt deraf.
14. Farmaceutisk sammensætning omfattende en forbindelse ifølge et hvilket som helst af kravene 1 til 13, eller et farmaceutisk acceptabelt salt deraf, og en farmaceutisk acceptabel bærer.
15. Fremgangsmåde til behandling af en eller flere sygdomme eller lidelser hos et individ, omfattende indgivelse til individet af en terapeutisk effektiv mængde af en forbindelse ifølge et hvilket som helst af kravene 1 til 13, eller et farmaceutisk acceptabelt salt deraf.
16. Fremgangsmåde ifølge krav 15, hvor sygdommen eller lidelsen er valgt fra astma, kronisk obstruktiv lungesygdom (COPD), bronkitis, allergisk rhinitis, atopisk dermatitis, kontaktdermatitis, akne, nældefeber, cystisk fibrose, allograft-afstødning, multipel sklerose, scleroderma, arthritis, rheumatoid arthritis, juvenil rheumatoid arthritis, osteoarthritis, ankyloserende spondylitis, systemisk lupus erythematosus (SLE), psoriasis, Hashimotos sygdom, pancreatitis, autoimmun diabetes, type I diabetes, autoimmun øjensygdom, colitis ulcerosa, Crohns sygdom, regional enteritis, inflammatorisk tarmsygdom (IBD), inflammatorisk tarmsyndrom (IBS), Sjogrens syndrom, optisk neuritis, fedme, hepatosteatose, fedtvævs-associeret inflammation, insulinresistens, type II diabetes, neuromyelitis optica, myasthenia gravis, aldersrelated makulær degeneration, tørre øjne,
uveitis, Guillain-Barré syndrom, psoriasis, psoriatisk arthritis (PsA), steroidresistent astma, Graves' sygdom, scleritis, svær depression, sæsonrelateret affektiv lidelse, PTSD, bipolær lidelse, autisme, epilepsi, Alzheimers sygdom, CNS-lidelser associeret med ændrede søvn- og/eller døgnrytmer, endometriose, obstruktiv søvnapnøsyndrom (OSAS), Behgets sygdom, dermatomyositis, polymyocitis, graft-versus-host sygdom, primær biliær cholangitis, leverfibrose, ikke-alkoholisk fedtleversygdom (NAFLD), sarkoidose, primær skleroserende cholangitis, autoimmun thyroideasygdom, autoimmunt polyendokrint syndrom type I, autoimmunt polyendokrint syndrom type II, cøliaki, neuromyelitis, juvenil idiopatisk arthritis, systemisk sklerose, myokardieinfarkt, pulmonal hypertension, osteoarthritis, kutan leishmaniasis, sinonasal polypose og kræft.
17. Fremgangsmåde ifølge krav 16, hvor sygdommen eller lidelsen er valgt fra astma, atopisk dermatitis, akne, Crohns sygdom, regional enteritis, colitis ulcerosa, Sjogrens syndrom, uveitis, Behgets sygdom, dermatomyositis, multipel sklerose, ankyloserende spondylitis, systemisk lupus erythematosus (SLE), skleroderma, psoriasis, psoriatisk arthritis (PsA), steroid resistent astma og rheumatoid arthritis.
DK15785013.2T 2014-10-14 2015-10-14 Dihydropyrrolopyridin-inhibitorer af ror-gamma DK3207043T6 (da)

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US201462063912P 2014-10-14 2014-10-14
US201462074406P 2014-11-03 2014-11-03
PCT/US2015/055420 WO2016061160A1 (en) 2014-10-14 2015-10-14 Dihydropyrrolopyridine inhibitors of ror-gamma

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DK3207043T3 true DK3207043T3 (da) 2019-04-01
DK3207043T6 DK3207043T6 (da) 2020-01-20

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BR112014030473A2 (pt) 2012-06-13 2017-06-27 Hoffmann La Roche novo diazaespirocicloalcano e azaespirocicloalcano
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