DK2925725T3 - Androgenreceptormodulatorer - Google Patents

Androgenreceptormodulatorer Download PDF

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DK2925725T3
DK2925725T3 DK13820949.9T DK13820949T DK2925725T3 DK 2925725 T3 DK2925725 T3 DK 2925725T3 DK 13820949 T DK13820949 T DK 13820949T DK 2925725 T3 DK2925725 T3 DK 2925725T3
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carbonitrile
isoquinoline
trifluoro
branched chain
linear
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Eugene Lvovich Piatnitski Chekler
Edmund L Ellsworth
Bruce Kipp Erickson
Adam Matthew Gilbert
Anthony P Ricketts
David P Thompson
Rayomand Jal Unwalla
Patrick Robert Verhoest
James Thomas Anderson
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Pfizer
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Claims (16)

1. Forbindelse med formel 1, 2 eller 3:
hvor A er N eller -CR0--, hvor R0 er hydrogen, C-|-C6 lineær eller forgrenet kæde alkyl, C-|-C6 lineær eller forgrenet kæde perfluoralkyl, aryl, perfluoraryl, alkylaryl, heteroaryl; eller alkylheteroaryl X og Y uafhængigt er -CH2--, -CHRa-- eller -CRaRb--, hvor Ra og Rb uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, aryl, alkylaryl, heteroaryl eller al kyl heteroaryl; eller Ra og Rb sammen danner en kæde omfattende --(CH2)y--, -(CHRc)y-- eller -(CRcRd)y--, hvor Rc og Rd uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, C-|-C6 lineær eller forgrenet kæde perfluoralkyl, aryl, alkylaryl, heteroaryl eller alkyl heteroaryl; hvor j er 2; 3, 4 eller 5 Z er -CRe eller -N--, hvor Re er hydrogen, C1-C6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, aryl, alkylaryl, hete-roaryl eller alkylheteroaryl; Ri er hydrogen, CrC6 lineær eller forgrenet kæde alkyl, aryl, CrCs lineær eller forgrenet kæde perfluoralkyl, alkylaryl, heteroaryl, alkylheteroaryl, CrC6 lineær eller forgrenet kæde alkoxylcarbonyl, CrC6 lineær eller forgrenet kæde alkylamino-carbonylamino, CrC6 lineær eller forgrenet kæde alkyloxycar-bonylamino, CrC6 lineær eller forgrenet kæde alkylcarbonylamino eller CrC6 lineær eller forgrenet kæde alkylaminocarbonyl; R2 uafhængigt er hydrogen eller CrC6 lineær eller forgrenet kæde alkyl; R3 og R4 uafhængigt er hydrogen, CrC6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, CrC6 lineær eller forgrenet kæde perfluoralkoxy, halogen, cyano, hydroxyl, amino, carboxy, aryl, heteroaryl, C-i-Ce lineær eller forgrenet kæde alkoxylcarbonyl, CrC6 lineær eller forgrenet kæde alkylamino-carbonylamino eller CrC6 lineær eller forgrenet kæde alkylaminocarbonyl;. R5 og R6 uafhængigt er hydrogen eller CrC6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, cyano, hydroxyl, amino, carboxy, aryl, heteroaryl, eller R5 og R6 sammen danner en kæde omfattende -(CH2)r-, ~(CHR7)/r- eller -(CR7aR7b)/r-, hvor R7, R7a, og R7b uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, aryl, alkylaryl, heteroaryl eller alkylheteroaryl; hvor k er 2; 3, 4 eller 5; R8 er hydrogen, C-|-C6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, aryl, aryl substitueret med et, to eller tre fluorinatomer, perfluoraryl, alkylaryl, heteroaryl; eller alkylheteroaryl; eller R1 og R8 sammen danner en kæde omfattende --(CH2)m-, -(CHRf)m-, eller -(CRfRg)m~, hvor Rf og Rg uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, aryl, alkylaryl, heteroaryl eller alkylheteroaryl; hvor m er 2; 3, 4 eller 5; R9 og R-io uafhængigt er hydrogen eller CrC6 lineær eller forgrenet kæde alkyl, CrC6 lineær eller forgrenet kæde perfluoralkyl, cyano, hydroxyl, amino, carboxy, aryl, heteroaryl, eller Rg og R10 sammen danner en kæde omfattende “(CH2)p~, -(CHRh)p- eller -(CRhRi)p--, hvor Rh og R, uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, aryl, alkylaryl, heteroaryl eller alkylheteroaryl; hvor per 2; 3, 4 eller 5; Q er --C0-, -(CH2)g~, --(CHRs)q- eller -(CRsRt)^--, hvor Rs og Rt uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, aryl, alkylaryl, heteroaryl eller al-kylheteroaryl; hvor q er 0, 1,2 eller 3; og hvor n er 0, 1,2, 3, 4 eller 5; eller a farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvilken forbindelse har formel 1, hvor Ri og R2 uafhængigt er CrC6 lineær eller forgrenet kæde alkyl; og R3 og R4 begge er hydrogen.
3. Forbindelse ifølge krav 2, hvor Ri og R2 uafhængigt er methyl, ethyl eller propyl.
4. Forbindelse ifølge krav 1, hvilken forbindelse har formel 2, hvor Q er —(CH2)g—, --(CHRsV-eller -(CRsRt)g~, hvor Rs og Rt uafhængigt er Ci-C6 lineær eller forgrenet kæde alkyl; og q er 1 eller 2.
5. Forbindelse ifølge krav 4, hvor Q er -CO-.
6. Forbindelse ifølge krav 1, hvilken forbindelse har formel 3, hvor X og Y uafhængigt er -CH2~, -CHRa~ eller -CRaRb--, hvor Ra og Rb uafhængigt er CrC6 lineær eller forgrenet kæde alkyl, aryl, alkylaryl, heteroaryl eller alkyl-heteroaryl.
7. Forbindelse ifølge krav 6, hvor X og Y uafhængigt er -CH2-, -CHRa-, eller -CRaRb-, hvor Ra og Rb uafhængigt er methyl, ethyl.
8. Forbindelse ifølge krav 1, udvalgt fra gruppen bestående af: 6-[(3S)-3-methyl-1,1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril; 6-[(3S)-3-ethyl-1,1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril 6-[(3R)-1,1 -dioxido-3-(2,2,2-trifluorethyl)-1,2,5-thiadiazolidin-2-yl]isoquinolin-1-carbonitril; 6-[(3R)-1,1 -dioxido-3-(2-phenylethyl)-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril; 6-[1 -methyl-(3S)-3-methyl-1,1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril; 6-{(3R)-1,1 -dioxido-3-[3-(trifluormethyl)phenyl]-1,2,5-thiadiazolidin-2-yl}isoquinolin-1 -carbonitril; 6-[(3S)-3-(4-chlorphenyl)-1,1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril; 6-[(3S)-3-methyl-1,1 -dioxido-1,2-thiazolidin-2-yl]isoquinolin-1 -carbonitril; 6-[(3S)-3-methyl-1,1 -dioxido-1,2,5-thiadiazolidin-2-yl]naphthalen-1 -carbonitril; 6-[(4R)-4-methyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-[(4S)-4-methyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-{(3R)-1,1 -dioxido-3-(3-phenyl)-1,2,5-thiadiazolidin-2-yl}isoquinolin-1 -carbonitril; 6-(4,4-dimethyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl)isoquinolin-1 -carbonitril; 6-(6,6-dioxido-6-thia-5,7-diazaspiro[2.5]oct-5-yl)isoquinolin-1-carbonitril; 6-[(4R)-4-(3-methylbenzyl)-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-[(4R)-6-ethyl-4-methyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-(5-methyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl)isoquinolin-1 -carbonitril; 6-[(4S)-4-(4-methylphenyl)-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-[(4R)-4-(4-methylphenyl)-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-[(4S)-4-(3-methylphenyl)-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; 6-[(4S)-4-ethyl-1,1 -dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1 -carbonitril; og 6-(1,1 -dioxido-4-propyl-1,2,6-thiadiazinan-2-yl)isoquinolin-1 -carbonitril, 6-{[(2R,3S)-4,4,4-trifluor-3-hydroxybutan-2-yl]amino}isoquinolin-1-carbonitril; 6-{(2R)-2-[(1 R)-2,2,2-trifluor-1 -hydroxyethyl]azetidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2S)-2-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]azetidin-1 -yl}isoquinolin-1 -carbonitril; 6-{methyl-[(2R,3R)-4,4,4-trifluor-3-hydroxybutan-2-yl]amino}isoquinolin-1- carbonitril; 6-{methyl-[(2R,3S)-4,4,4-trifluor-3-hydroxybutan-2-yl]amino}isoquinolin-1- carbonitril; 6-{(2R)-2-[(1 R)-2,2,2-trifluor-1 -hydroxyethyl]piperidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2R)-2-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]piperidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2R,5R)-2-methyl-5-[(1 R)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2R,5R)-2-[(11 R)-1 -hydroxyethyl]-5-methylpyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(5R)-2-oxo-5-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yljisoquinolin-1-carbonitril; 6-{(5S)-2-oxo-5-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yljisoquinolin-1-carbonitril; 6-{(2R)-2-[(1 R)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2R)-2-[(11 S)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2S)-2-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2S)-2-[(1 R)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2S,5S)-2-methyl-5-[(1 S)-2,2,2-trifluor-1 -hydroxyethyl]pyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-{(2R,5R)-2-[(11 S)-1 -hydroxyethyl]-5-methylpyrrolidin-1 -yl}isoquinolin-1 -carbonitril; 6-((2R,3S)-4,4,4-trifluor-3-hydroxybutan-2-ylamino)-1-naphthonitril; 6-((R)-2-((R)-2,2,2-trifluor-1 -hydroxyethyl)azetidin-1 -yl)-1 -naphthonitril; 6-((S)-2-((S)-2,2,2-trifluor-1 -hydroxyethyl)azetidin-1 -yl)-1 -naphthonitril 6-(methyl((2R,3R)-4,4,4-trifluor-3-hydroxybutan-2-yl)amino)-1-naphthonitril; 6-(methyl((2R,3S)-4,4,4-trifluor-3-hydroxybutan-2-yl)amino)-1-naphthonitril; 6-((R)-2-((R)-2,2,2-trifluor-1-hydroxyethyl)piperidin-1-yl)-1-naphthonitril; 6-((R)-2-((S)-2,2,2-trifluor-1-hydroxyethyl)piperidin-1-yl)-1-naphthonitril; 6-((2R,5R)-2-methyl-5-((R)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((2R,5R)-2-((R)-1-hydroxyethyl)-5-methylpyrrolidin-1-yl)-1-naphthonitril; 6-((R)-2-oxo-5-((S)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((S)-2-oxo-5-((S)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((R)-2-((R)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((R)-2-((S)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((S)-2-((S)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((S)-2-((R)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; 6-((2S,5S)-2-methyl-5-((S)-2,2,2-trifluor-1 -hydroxyethyl)pyrrolidin-1 -yl)-1 -naphthonitril; og 6-((2R,5R)-2-((S)-1 -hydroxyethyl)-5-methylpyrrolidin-1 -yl)-1 -naphthonitril eller et farmaceutisk acceptabelt salt deraf.
9. Forbindelse ifølge krav 1, hvilken forbindelse omfatter 6-[(3R)-3-methyl- 1.1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril eller et farmaceutisk acceptabelt salt deraf.
10. Forbindelse ifølge krav 1, hvilken forbindelse omfatter 6-[(3S)-3-methyl- 1.1 -dioxido-1,2,5-thiadiazolidin-2-yl]isoquinolin-1 -carbonitril eller et farmaceutisk acceptabelt salt deraf.
11. Forbindelse ifølge krav 1, hvilken forbindelse omfatter 6-[(4R)-4-methyl- 1.1- dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1-carbonitril eller et farmaceutisk acceptabelt salt deraf.
12. Forbindelse ifølge krav 1, hvilken forbindelse omfatter 6-[(4S)-4-methyl- 1.1- dioxido-1,2,6-thiadiazinan-2-yl]isoquinolin-1-carbonitril eller et farmaceutisk acceptabelt salt deraf.
13. Forbindelse ifølge krav 1, hvilken forbindelse omfatter 6-(methyl-((2R,3R)-4,4,4-trifluor-3-hydroxybutan-2-yl)amino)-1 -naphthonitril eller et farmaceutisk acceptabelt salt deraf.
14. Forbindelse ifølge krav 1 til anvendelse som et farmaceutisk produkt.
15. Forbindelse ifølge krav 1 til anvendelse inden for moduleringen af en aktivitet af en androgenreceptor i et individ med behov herfor.
16. Forbindelse ifølge krav 1 til anvendelse inden for behandlingen af en sygdom eller tilstand i et individ, hvor sygdommen eller tilstanden er udvalgt blandt anæmi; anoreksi; arthritis; knoglesygdom; muskuloskeletal svækkelse; kakeksi; skrøbelighed; aldersrelateret funktionel forringelse hos ældre; væksthomonmangel; hæmatopoietiske forstyrrelser; hormonerstatning; tab af muskelstyrke og/eller -funktion; muskeldystrofier; muskeltab efter operation; muskelatrofi; neurodegenerative sygdomme; neuromuskulær sygdom; obesi-tet; osteoporose; og muskelsvind.
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