DK2010493T3 - Pyridylamid t-type-calciumkanalantagonister - Google Patents
Pyridylamid t-type-calciumkanalantagonister Download PDFInfo
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- DK2010493T3 DK2010493T3 DK07775220.2T DK07775220T DK2010493T3 DK 2010493 T3 DK2010493 T3 DK 2010493T3 DK 07775220 T DK07775220 T DK 07775220T DK 2010493 T3 DK2010493 T3 DK 2010493T3
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- acetamide
- pyridin
- ethyl
- phenyl
- trifluoroethoxy
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Claims (16)
- -1- PYRIDYLAMID T-TYPE-CALCIUMKANALANTAGONISTER1. Forbindelse med formlen EI hvor: A er udvalgt fra gruppen bestående af phenyl og pyridyl; Rla, Rlb og Rlc uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) halogen, (3) phenyl eller naphthyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, Cj.6-alkyl, -0-Ci_6-alkyl, C3.6-cycloalkyl, -SH, -S-Ci_6-alkyl, -N02, -C02H eller -CN, (4) -O-phenyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, C, 6-alkyl, -O-Cj^-alkyl, -SH, -S-CM,-alkyl, -N02, -C02H eller -CN, (5) Ci_6-alkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl eller -O-Q. e-alkyl, (6) C3.6-cycloalkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl eller - O-C^-alkyl, (7) C2.4-alkenyl, der er ikke-substitueret eller substitueret med C3.6-cycloalkyl eller phenyl, (8) -NR10Rn, hvor R10 og R11 uafhængigt er udvalgt fra hydrogen og Ci_6-alkyl, (9) isoxazolyl, der er ikke-substitueret eller substitueret med Ci^-alkyl, (10) imidazolyl, der er ikke-substitueret eller substitueret med C^-alkyl, (11) morpholinyl, der er ikke-substitueret eller substitueret med Cj^-alkyl, (12) oxazolyl, der er ikke-substitueret eller substitueret med Ci_6-alkyl, (13) pyrazolyl, der er ikke-substitueret eller substitueret med C^-alkyl, (14) pyrrolidinyl, der er ikke-substitueret eller substitueret med halogen, (15) tetrazolyl, der er ikke-substitueret eller substitueret med Ci.6-alkyl, (16) thienyl, der er ikke-substitueret eller substitueret med Ci.6-alkyl, (17) benzothienyl, der er ikke-substitueret eller substitueret med Ci_6-alkyl, (18) thiophenyl, der er ikke-substitueret eller substitueret med Ci_6-alkyl, (19) triazolyl, der er ikke-substitueret eller substitueret med Ci_6-alkyl, (20) -N02 og -2- (21) -CN, eller Rla, og Rlb taget sammen danner en cyclopentyl-, cyclohexyl-, dihydrofuranyl- eller dihydropyranylring, der er ikke-substitueret eller substitueret med -CH3, (=CH2), keto eller hydroxyl; R2 og R3 uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) hydroxyl, (3) halogen (4) Q.j-alkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (5) C3_6-cycloalkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (6) -O-Cj^alkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (7) -O-C 3_6-cycloalkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, eller R2 og R3 og det carbonatom, hvortil de er bundet, danner en ketogruppe, eller R2 og R3 og det carbonatom, hvortil de er bundet, danner en C3_6-cycloalkylring, der er ikke-substitueret eller substitueret med R13; R4 er udvalgt fra gruppen bestående af: (1) Ci.6-alkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (2) -C3_6-cycloalkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (3) C2-6-alkenyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (4) C2_6-alkynyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (5) phenyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (6) -(C=O)-NR10Rn og (7) -(C=0)-0-Ci_6-alkyl, der er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, R5a, R5b og R5c uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) -On-C|.6-alkyl, hvor n er 0 eller 1 (hvor hvis n er 0, er en binding til stede) og hvor alkylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, -3- (5) -0„-C3-6-cycloalkyl, hvor n er 0 eller 1 (hvor hvis n er 0, er en binding til stede), og hvor cycloalkylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (6) -C2_4-alkenyl, hvor alkenylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (7) -0„-phenyl eller -On-naphthyl, hvor n er 0 eller 1 (hvor hvis n er 0, er en binding til stede) og hvor phenylet eller naphthylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (8) -On-heterocyklus, hvor n er 0 eller 1 (hvor hvis n er 0, er en binding til stede) og hvor heterocyklussen er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R13, (9) -(C=O)-NR10Rn, (10) -NR10Rn, (11) -S(O)2-NR10Rn, (12) -NR10-S(O)2Rn, (13) -S(0)q-R12, hvor q er 0, 1 eller 2 og hvor R12 er udvalgt fra definitionerne af R10 og R11, (14) -C02H, (15) -CN, (16) -N02; (17) eller R5a og R5b taget sammen danner en pyrrolyl- eller imidazolylring, der er ikke-substitueret eller substitueret med -CH3, (=CH2), keto eller hydroxyl; R13 er udvalgt fra gruppen bestående af: (1) halogen, (2) hydroxyl, (3) -(C=0)m-0n-C1.6-alkyl, hvor m er 0 eller 1 og n er 0 eller 1 (hvor hvis m er 0 eller n er 0, er en binding til stede, og hvor hvis m er 0 og n er 0, er en enkelt binding til stede), hvor alkylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R14, (4) -On-(C i .3 iperfluoralkyl, (5) -(C=0)m-On-C3.6-cycloalkyl, hvor cycloalkylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R14, (6) -(C=0)m-C2^-alkenyl, hvor alkenylet er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R14, (7) -(C=0)m-0n-phenyl eller -(C=0)m-On-naphthyl, hvor phenylet eller naphthylen er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R14, (8) -(C=0)m-On-heterocyklus, hvor heterocyklussen er ikke-substitueret eller substitueret med én eller flere substituenter, der er udvalgt fra R14, (9) -(C=O)-NRI0Rn, (10) -NR10Rn, (11) -S(O)2-NR10Rn, (12) -S(0)q-R12, -4- (13) -C02H, (14) -CN og (15) -N02; R14 er udvalgt fra gruppen bestående af: (1) hydroxyl, (2) halogen, (3) Ci-6-alkyl, (4) -C3.6-cycloalkyl, (5) -0-Ci_6-alkyl, (6) -0(C=0)-C^-alkyl, (7) -NH-Cj.g-alkyl, (8) phenyl, (9) heterocyklus, (10) -C02H og (11) -CN; eller et farmaceutisk acceptabelt salt deraf.
- 2. Forbindelse ifølge kræ71 TU·Ib eller et farmaceutisk acceptabelt salt deraf.
- 3. Forbindelse ifølge krav 2 med formlen le:le eller et farmaceutisk acceptabelt salt deraf.
- 4. Forbindelse ifølge krav 1, hvor A er phenyl, Rla, er Ci_6-alkyl, Rlb er hydrogen, og Rlc er hydrogen.
- 5. Forbindelse ifølge krav 1, hvor R2 og R3 uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) halogen, -5- (3) Ci.6-alkyl, der er ikke-substitueret eller substitueret med halo, C3_6-cycloalkyl eller phenyl og (4) C3.6-cycloalkyl, der er ikke-substitueret eller substitueret med halo, C3.6-cycloalkyl eller phenyl.
- 6. Forbindelse ifølge krav 1, hvor R4 er i (R) retningen og er udvalgt fra gruppen bestående af: (1) Ci.6-alkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, -0-Ci_6-alkyl, C3_6-cycloalkyl, phenyl, eller -NR10Rn, hvor R10 og R11 uafliængigt er udvalgt fra gruppen bestående af hydrogen, og Ci_6-alkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl eller phenyl, (2) -C3_6-cycloalkyl, der er ikke-substitueret eller substitueret med halogen, Ci_6-alkyl eller phenyl, (3) -C2-6-alkenyl, (4) phenyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, C^-alkyl, -O-C^-alkyl eller -N02, (5) -(C=O)-NR10Rn og (6) -(C=0)-0-Ci_6-alkyl, der er ikke-substitueret eller substitueret med halogen, C3.6-cycloalkyl eller phenyl.
- 7. Forbindelse ifølge krav 6, hvor R4 er udvalgt fra gruppen bestående af: (1) CH3, (2) CH2OH, (3) CH2OCH3, (4) CH2CH3, (5) CH=CH2, (6) CH2CH2OH, (7) CH2CH=CH2, (8) CH2CH2F, (9) CH2CF2, (10) CH2-phenyl, (12) CFl2-cyclopropyl, (13) CFl2-cyclobutyl, (14) cyclopropyl, (15) cyclobutyl, (16) CH2CH2CH3 og (17) -(CO)-0-CH3.
- 8. Forbindelse ifølge krav 1 hvor R5a, R5b og R5c uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) halogen, (3) hydroxyl, (4) Ci_6-alkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl, -0-Ci.6-alkyl, -0-(C0)Ci_6-alkyl eller C3_6-cycloalkyl og -6- (5) -C^-alkcnyl.
- 9. Forbindelse ifølge krav 1, hvor R5a, R5b og R5c uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) -O-Cj^aLkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl, -O-Ci^-alkyl eller Ci^-cycloalkyl, (3) C3.6-cycloalkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl eller phenyl, (4) -NH-Ci_6-afkyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl, -O-Ci_6-afkyl, -0-(CO)Ci_6-alkyl eller C3_6-cycloalkyl, (5) -N(C1.6-afkyl)2, hvor hver afkyl uafhængigt er ikke-substitueret eller substitueret med halogen, hydroxyl, phenyl, -O-C^g-alkyl, -0-(C0)C1.6-alkyl, eller C3_6-cycloafkyl, (6) phenyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, C|.6-alkyl, -O-Ci^-afkyl eller -N02, (7) -O-phenyl, der er ikke-substitueret eller substitueret med halogen, hydroxyl, C].6-alkyl, -O-Ci^-alkyl eller -N02, (8) -S(0)2-NH-Ci_6-alkyl, (9) -S(0)2-N(Ci_6-alkyl)2 og (10) -S(0)2-Ci.6-alkyl.
- 10. Forbindelse ifølge krav 1, hvor R5a, R5b og R5c uafhængigt er udvalgt fra gruppen bestående af: (1) hydrogen, (2) heterocyklus, der er ikke-substitueret eller substitueret med halogen, hydroxyl, keto, Ci_6-alkyl eller -0-Ci.6-alkyl, (3) -O-heterocyklus, der er ikke-substitueret eller substitueret med halogen, hydroxyl, keto, C^-alkyl eller -0-Ci_6-alkyl og (4) -NH-heterocyklus, der er ikke-substitueret eller substitueret med halogen, hydroxyl, keto, Ci_6-alkyl eller -O-Ci^-alkyl.
- 11. Forbindelse ifølge krav 1, der er udvalgt fra gruppen bestående af: N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-[4-(5-methylisoxazol-4-yl)phenyl]acetamid; 2-[4-(5-methylisoxazol-4-yl)phenyl]-N-[(lR)-l-(5-vinylpyridin-2-yl)ethyl]acetamid; N-[(lR)-l-(5-ethylpyridin-2-yl)ethyl]-2-[4-(5-methylisoxazol-4-yl)phenyl]acetamid; N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-(4-isopropylphenyl)acetamid; 2-(4-isopropylphenyl)-N-((lR)-l-{5-[(2,2,2-trifluorethyl)amino]pyridin-2-yl}ethyl)acetamid; N-[( 1R)-1 -(3,3 ’-bipyridin-6-yl)ethyl] -2-(4-isopropylphenyl)acetamid; 2-(1,1 '-biphenyl-4-yl)-N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] acetamid; 2-(1,1 '-biphenyl-4-yl)-N-[( 1R)-1 -(5-hydroxypyridin-2-yl)ethyl] acetamid; 2-(1,1 '-biphenyl-4-yl)-N-[( 1R)-1 -(5-propoxypyridin-2-yl)ethyl] acetamid; 2-(1,1 ’-biphenyl-4-yl)-N-{(lR)-1 -[5-(pyridin-2-yloxy)pyridin-2-yl]ethyl} acetamid; 2-(4-isopropylphenyl)-N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]acetamid; -7- N-[(lR)-l-(5-hydroxypyridin-2-yl)ethyl]-2-(4-isopropylphenyl)acetamid; (2S)-2-(2-fluor-1,1 '-biphenyl-4-yl)-N-[( 1R)-1 -(5 -methoxypyridin-2-yl)ethyl]propanamid; (R)[(lS)-l-(5-methoxypyridin-2-yl)-2,2,2-trifluorethyl]-2-methylpropan-2-sulfinamid; N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]-2-(4-pyrrolidin-l-ylphenyl)acetamid; 2-(4-isopropylphenyl)-N-[(lR)-l-(5-(2,2,2-trifluorethoxy)pyridin-2-yl)ethyl]acetamid; 2-[4-( 1 -hydroxy-1 -methylethyl)phenyl] -N-[( 1R)-1 -(5-(2,2,2-trifluorethoxy)pyridin-2-yl)ethyl] acetamid; 2-(4-isopropenylphenyl)-N-[(lR)-l-(5-(2,2,2-trifluorethoxy)pyridin-2-yl)ethyl]acetamid; 2-{4-[2-oxo-2-(((lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl)amino)ethyl]phenyl}- propionsyre; 2-[4-(2-hydroxy-1 -methylethyl)phenyl] -N-[( 1R)-1 -(5-(2,2,2-trifluorethoxy)pyridin-2-yl)ethyl] acetamid; 2-(4-cyclopropylphenyl)-N-((lR)-l-{5-[(2,2,2-trifluorethyl)oxo]pyridin-2-yl}ethyl)acetamid; 2-(4-cyclopropylphenyl)-N-{(lS)-2-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(5-fluor-6-pyrrolidin-1 -ylpyridin-3 -yl)-N - {(1R)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(6-chlor-5-fluorpyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifLuorethoxy)pyridin-2-yl]ethyl}acetamid; 2-{5-fluor-6-[(3R)-3-methylmorpholin-4-yl]pyridin-3-yl}-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2 -yl] ethyl} acetamid; 2-(4-cyclopropylphenyl)-N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl} acetamid; 2-[4-(l-methyl-lH-pyrazol-5-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(4-methyl-l,3-oxazol-5-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridm-2-yl]ethyl} acetamid; 2-(4-morpholin-4-ylphenyl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; methyl-4-[ 1,1 -difluor-2-oxo-2-({(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} amino)ethyl]benzoat 2,2-difluor-2-[4-( 1 -hydroxy-1 -methylethyl)phenyl] -N- {(1R)-1 -[5-(2,2,2-trifluorethoxy)-pyridin-2-yl]ethyl} acetamid; 2-[4-(lH-pyrazol-l-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-tert-butylphenyl)-N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] -acetamid; 2-(4-tert-butylphenyl)-N-[( 1 S)-2,2,2-trifluor-1 -(5 -methoxypyridin-2-yl)ethyl] acetamid; 2-(4-tert-butylphenyl)-N-[( 1R)-1 -(5-chlorpyridin-2-yl)ethyl] acetamid; N- [(1R) -1 - (5 -chlorpyridin-2-yl)ethyl] -2-hydroxy-2-[4-(3 -thienyl)phenyl] -propanamid 2-(4-tert-butylphenyl)-N-[(1R)-1 -(5-fluorpyridin-2-yl)ethyl] acetamid; -8- N-[( IR)-1 -(5-methoxypyridin-2-yl)butyl] -2-[4-(3 -thienyl)phenyl] -acetamid; N-[( 1R)-1 -(5-chlor-4-methoxypyridin-2-yl)ethyl] -2-[4-(3 -thienyl)phenyl] acetamid; 2-(3,4-dichlorphenyl)-N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] acetamid; 2-(4-tert-butylphenyl)-N-[(R)-cyclopropyl(5-methoxypyridin-2-yl)methyl]acetamid; N-[( 1 S)-1 -(5-chlorpyridin-2-yl)-2,2,2-trifluorethyl] -2-[4-( 1 -methyl-1 H-imidazol-5 -yl)phenyl] acetamid; 2-(4-vinylphenyl)-N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]acetamid; 2-(4-cyclopropylphenyl)-N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] acetamid; 2-(4-tert-butylphenyl)-N-{(lR)-l-[5-(fluormethoxy)pyridin-2-yl]ethyl}acetamid; N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]-2-[4-(5-methylisoxazol-4-yl)phenyl]acetamid; N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]-2-(5,6,7,8-tetrahydronaphthalen-2-yl)acetamid; N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]-2-[4-(lH-l,2,3-triazol-l-yl)phenyl]acetamid; 2-biphenyl-4-yl-N-[( 1R)-1 -(6-brompyridin-2-yl)ethyl]acetamid; N-[(lR)-l-(5-methoxypyridin-2-yl)etbyl]-2-[4-(l,2,4-oxadiazol-3-yl)phenyl]acetamid; 2-biphenyl-4-yl-N-[( 1R)-1 -(6-cyclopropylpyridin-2-yl)ethyl] acetamid; 2-biphenyl-4-yl-N-{(lR)-l-[6-(cyclopropylamino)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N- {(1R)-1 -[5-(bydroxymetbyl)pyridin-2-yl] ethyl} acetamid; N- {(1R)-1 -[5-(cyclobutyl-methoxy)pyridin-2-yl]ethyl} -2-(4-isopropylphenyl)acetamid; 6-{(lR)-l-[(2-biphenyl-4-ylacetyl)amino]ethyl}pyridin-3-yl-methansulfonat; 6- {(IR)-1 -[(biphenyl-4-ylacetyl)amino]ethyl} pyridin-3-yl-methylcarbonat; 2-(4-isopropylphenyl)-N-[(lR)-l-(5-propoxypyridin-2-yl)ethyl]acetamid; 2-biphenyl-4-yl-N-(2-hydroxy-1 -pyridin-2-ylethyl)acetamid; 2-biphenyl-4-yl-N-(2-methoxy-l-pyridin-2-ylethyl)acetamid; 2-(4-isopropylphenyl)-N-[(lR)-l-(5-fluormethoxypyridin-2-yl)ethyl]acetamid; 2-biphenyl-4-yl-N-[( 1 R)-l-(5-{[(1 S)-1 -methylpropyl]oxy}pyridin-2-yl)ethyl] acetamid; 2-[4-( 1 H-imidazol-1 -yl)phenyl] -N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] acetamid; 2-[4-(3 -fluorpyrrolidin-1 -yl)phenyl] -N-[( 1R)-1 -(5-methoxypyridin-2-yl)ethyl] acetamid; ethyl {[6-(( 1R)-1 - {[(4-isopropylphenyl)acetyl] amino} ethyl)pyridin-3 -yl]oxy} acetat; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(lH-pyrazol-4-yl)pyridin-2-yl]ethyl}acetamid; N-{(lR)-l-[5-(l,3-dioxolan-2-ylmethoxy)pyridin-2-yl]ethyl}-2-(4-isopropylphenyl)acetamid; N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-(4-oxo-3,4-dihydro-2H-chromen-7-yl)acetamid; N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-(4-hydroxy-3,4-dihydro-2H-chromen-7-yl)acetamid; N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-(4-hydroxy-4-methyl-3,4-dihydro-2H-chromen-7-yl)acetamid; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(lH-pyrrol-l-yl)pyridin-2-yl]ethyl} acetamid; 6-(( 1R)-1 - {[2-(4-isopropylphenyl)-acetyl] amino} ethyl)pyridin-3 -yl 4-methylbenzensulfonat; -9- N-[(lR)-l-(5-brompyridin-2-yl)ethyl]-2-(4-methylen-3,4-dihydro-2H-chromen-7-yl)acetamid; N-(( 1R)-1 - {5-[2-(isopropylamino)-2-oxoethoxy]pyridin-2-yl} ethyl)-2-(4-isopropylphenyl)acetamid; N-[(lR)-l-(5-tert-butoxypyridin-2-yl)ethyl]-2-(4-isopropylphenyl)acetamid; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(3-methyl-lH-pyrazol-l-yl)pyridin-2-yl]ethyl}acetamid; N-{(lR)-l-[5-(benzyloxy)pyridin-2-yl]ethyl}-2-(4-bromphenyl)acetamid; N- {(1R) -1 - [ 5 -(benzyloxy)pyridin-2-yl] ethyl}-2-[4-(lH -pyrrol-1 -yl)phenyl] acetamid; 2-(3,4-dichlorphenyl)-N-[( 1R)-1 -(5-propylpyridin-2-yl)ethyl]acetamid; 2-(4-isopropenylphenyl)-N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]acetamid; N-{(lR)-l-[5-(benzyloxy)pyridin-2-yl]ethyl}-2-(4-morpholin-4-ylphenyl)acetamid; 2-[4-(3-thienyl)phenyl]-N-[(lS)-2,2,2-trifluor-l-(5-hydroxypyridin-2-yl)ethyl]acetamid; N-[(lR)-l-(5-benzyloxypyridin-2-yl)ethyl]-2-(4-methylen-3,4-dihydro-2H-chromen-7-yl)acetamid; 2-[4-(3-thienyl)phenyl]-N-[(lS)-2,2,2-trifluor-l-(5-hydroxypyridin-2-yl)ethyl]acetamid; 2-(4-methyl-3,4-dihydro-2H-chromen-7-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-tert-butylphenyl)-N-(1 H-pyrrolo[2,3-c]pyridin-5-ylmethyl)acetamid; 2-(4-tert-butylphenyl)-N-({5-[(3,3-dimethylpropyl)amino]pyridin-2-yl}methyl)acetamid; 2-(4-tert-butylphenyl)-N-({5-[(3,3-dimethylbutyl)amino]pyridin-2-yl}methyl)ace tamid; 2-(3,4-dichlorphenyl)-N-({5-[(2,2-dimethylpropyl)amino]pyridin-2-yl}methyl)acetamid; 2-biphenyl-4-yl-N-{(1R)-1 -[5-(cyclopropylamino)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N-[( 1R)-1 -(5-pyrrolidin-1 -ylpyridin-2-yl)ethyl]acetamid; 2-biphenyl-4-yl-N-[( 1R)-1 -(5-morpholin-4-ylpyridin-2-yl)ethyl]acetamid; 2-biphenyl-4-yl-N-((1R)-1 - {5-[(3R)-3-methylmorpholin-4-yl]pyridin-2-yl} ethyl)ace tamid; 2-biphenyl-4-yl-N - {(1R)-1 -[5-(4-methylpiperazin-1 -yl)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N-{(1R)-1 -[5-(cyclopropylmethylamino)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N-{(1R)-1 -[5-(2-methylpyrolidin-1 -yl)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N - {(1R)-1 -[5-(l, 1 -dioxidothiomorpholin-4-yl)pyridin-2-yl]cthyl} acetamid; 2-biphenyl-4-yl-N-{(1R)-1 -[5-(3,3-difluorpyrrolidin-1 -yl)pyridin-2-yl]ethyl} acetamid; 2-biphenyl-4-yl-N-{(1R)-1 -[5-(pyridin-2-ylamino)pyridin-2-yl]ethyl} acetamid; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(pyridin-4-ylamino)pyridin-2-yl]ethyl} acetamid; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(pyridin-3-ylamino)pyridin-2-yl]ethyl} acetamid; 2-(4-isopropylphenyl)-N-{(lR)-l-[5-(3-oxopyrrolidin-l-yl)pyridin-2-yl]ethyl} acetamid; N-{(lR)-l-[5-(sec-butylamino)pyridin-2-yl]ethyl}-2-(4-isopropylphenyl)acetamid; 2-(4-cyclopropylphenyl)-N-((lR)-l-{5-[(2,2,2-trifluorethyl)amino]pyridin-2-yl}ethyl)acetamid; 2-(4-isopropylphenyl)-N-((lR)-l-{5-[methyl(methylsulfonyl)amino]pyridin-2-yl}ethyl)acetamid; N-[(lR)-l-(5-chlorpyridin-2-yl)ethyl]-2-[2-fLuor-4-(3-thienyl)phenyl]-2-oxoacetamid; -10- N-[(lR)-l-(5-methoxypyridin-2-yl)ethyl]-2-(2-phenyl-l,3-thiazol-5-yl)ace tamid; 2-[2-(4-fluorphenyl)-l,3-thiazol-4-yl]-N-[(lR)-l-(5-methoxypyridm-2-yl)ethyl]acetamid; methyl [(biphenyl-4-ylacetyl)amino]-(pyridin-2-yl)acetat N-[(lR)-3-(diethylamino)-l-(5-methoxypyridin-2-yl)propyl]-2-(4-isopropylphenyl)ace tamid; 2-(4-isopropylphenyl)-N-[phenyl(pyridin-2-yl)methyl]acetamid; 2-[4-(lH-pyrazol-l-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridiQ-2-yl]ethyl}acetamid; N-[( 1R)-1 -(5-chlor-4-methoxypyridin-2-yl)ethyl] -2-[4-(3 -thienyl)phenyl] acetamid 2-[4-(lH-pyrazol-5-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; 2-[4-(l,3-oxazol-2-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; 2-(3-fluor-4-morpholin-4-ylphenyl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl Jethyl} acetamid; N-{(lR)-l-[5-(2,2-difluorpropoxy)pyridin-2-yl]ethyl}-2-[4-(3-oxomorpholin-4- yl)phenyl]acetamid; 2-(4-pyridin-3-ylphenyl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; N-{3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]butyl}-2-(4-isopropylphenyl)acetamid; 2-(5-fluor-6-morpholin-4-ylpyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2- yljethyl} acetamid; 2-[4-(3-hydroxypyrrolidin-l-yl)phenyl]-N-{l-[5-(2,2,2-trifhiorethoxy)pyridin-2-yljethyl} acetamid; 2-(3,4-dichlorphenyl)-N-{(lR)-l-[5-(pyrazin-2-yloxy)pyridin-2-yl]ethyl}acetamid; 2-(2-pyrrolidin-1 -ylpyrimidin-5-yl)-N- {(IR)-1 -[5-(2,2,2-trifLuorethoxy)pyridin-2-yljethyl} acetamid; 2-{4-[(3S)-3-fluorpyrrolidin-l-yl]phenyl}-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-fluor-2-[4-(lH-pyrazol-4-yl)phenyl]-N-{l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; N-{(lR)-l-[5-(2,2,2-trifLuorethoxy)pyridin-2-yl]ethyl}-2-[4-(trifluormethyl)phenyl]acetamid; 2-(6-chlor-5-fluorpyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; 2-fluor-2-[4-(5-methylisoxazol-4-yl)phenyl]-N-{l-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-(6-chlorpyridin-3-yl)-N-{(IR)-1-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(2-oxopyrrolidin-1 -yl)phenyl]-N- {(IR)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-(6-pyrrolidin-l-ylpyridin-3-yl)-N-{(1R)-1-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-methyl-2-oxo-2H-chromen-7-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-(6-morpholin-4-ylpyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; 2-(4-pyrimidin-2-ylphenyl)-N-{(IR)-1-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; -11- 2-[6-(cyclopropylamino)pyridin-3-yl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-isopropenyl-3-methoxyphenyl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(6-azetidin-l-ylpyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-cyclopropylphenyl)-N-{2,3-dihydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl} acetamid; N-{(lR)-3-amino-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl}-2-[4-(trifluormethyl)phenyl] acetamid; 2,2-diiluor-2-(4-isopropenylphenyl)-N - {(1R)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[6-( 1 -methyl-1 H-pyrazol-5-yl)pyridin-3 -yl] -N- {(1R)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; N-{(lS)-2-hydroxy-1-[5-(2,2,2-tri fluoretho xy)pyridin-2-yl] ethyl}-2-[4-(5-methylisoxazol-4-yl)phenyl] acetamid; 2- {4-[(3R)-3 -fluorpyrrolidin-1 -yl]phenyl} -N- {(IR)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[6-(3,3-difluorpyrrolidin-l-yl)pyridin-3-yl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-{6-[(2S)-2-(hydroxymethyl)pyrrolidin-l-yl]pyridin-3-yl}-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2 -yl] ethyl} acetamid; N-{(lS)-2-methoxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}-2-[4-(5-methylisoxazol-4-yl)phenyl] acetamid; 2-{4-[(2R)-2-(fluormethyl)pyrrolidiQ-l-yl]phenyl}-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; N-{3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]butyl}-2-[4-(trifluormethyl)phenyl] acetamid; 2-{5-fluor-6-[(2S)-2-(fluormethyl)pyrrolidin-l-yl]pyridin-3-yl}-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2 -yl] ethyl} acetamid; 2-[4-(3-methylisothiazol-4-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-tert-butylphenyl)-N - {(1 R)-3 -hydroxy-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl} acetamid; 2-(6-chlor-5-methoxypyridin-3-yl)-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-tert-butylphenyl)-N - {(1 R)-3 -hydroxy-1 -[5-(4-methyl-1,3 -oxazol-5 -yl)pyridin-2-yl]propyl} acetamid; 2-(4-tert-butylphenyl)-N-[( 1R)-1 -(5-cyclopropylpyridin-2-yl)-3 -hydro xypropyl] acetamid; -12- 2-(3',4'-difluorbiphenyl-4-yl)-N-{(lS)-2-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(l-hydroxycyclopropyl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(l-cyan-l-methylethyl)phenyl]-N-{l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}propanamid 2-(4-tert-butylphenyl)-N-(l-{5-[l-(hydroxymethyl)propoxy]pyridin-2-yl}ethyl)acetamid; 2-[4-(3 -methylisoxazol-4-yl)phenyl] -N- {(1R)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(aminomethyl)phenyl]-N-{(IR)-1-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[5-fluor-6-(3-fluorphenyl)pyridin-3-yl]-N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl} acetamid; 2-(4-tert-butylphenyl)-N-(l-{5-[l-(fluormethyl)propoxy]pyridin-2-yl}ethyl)acetamid; 2-[5-fluor-6-(l-methyl-lH-pyrazol-5-yl)pyridin-3-yl]-N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifLuorethoxy)pyridin-2-yl]propyl} acetamid; 2-[6-(3,4-difluorphenyl)pyridin-3-yl]-N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl} acetamid; N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl}-2-(2,3,,4'-trifluorbiphenyl-4- yl)acetamid; methyl-4-[2-({(lR)-l-[5-(2,2-difluor-3-hydroxypropoxy)pyridin-2-yl]ethyl}amino)-l,l-difluor-2- oxoethyl]benzoat; 2-(4-phenyl-1 Η-1,2,3 -triazol-1 -yl)-N- {(IR)- l-[5-(2,2,2-tnfluorcthoxy)pyndm-2-yl]ethyl} acetamid; 2-[4-(3,5-dimethylisoxazol-4-yl)-3-fluorphenyl]-N-{(lR)-3-hydroxy-l-[5-(2,2,2- trifluorethoxy)pyridin-2-yl]propyl}acetamid; N-{(lR)-3-hydroxy-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]propyl}-2-[4-(4-methyl-l,3-oxazol-5- yl)phenyl]acetamid; 2-hydroxy-2-[4-( 1 -hydroxy-1 -methylethyl)phenyl]-N- {1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl}acetamid; 2-phenyl-N- {(1R)-1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-(4-cyclopropylphenyl)-2-hydroxy-N- {1 -[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[4-(l-methylcyclopropyl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yl]ethyl} acetamid; 2-[3-hydroxy-4-(lH-pyrazol-l-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-[3-methoxy-4-(lH-pyrazol-l-yl)phenyl]-N-{(lR)-l-[5-(2,2,2-trifluorethoxy)pyridin-2-yljethyl} acetamid; 2-[4-(lH-pyrazol-4-yl)phenyl]-N-{(lR)-l-[5-(3,3,3-trifluor-2-hydroxypropoxy)pyridin-2-yl]c thyl} acetamid, -13- 2,2-difluor-2-[4-( 1 -hydroxy-1 -methylethyl)phenyl] -N-[( 1R)-1 -(5- {[(1 S)-1 -methylpropyl]oxy}pyridin-2-yl)ethyl]acetamid; eller et farmaceutisk acceptabelt salt deraf.
- 12. Forbindelse ifølge krav 11, der er 2-(4-isopropylphenyl)-N-[(lR)-l-(5-(2,2,2-trifluorethoxy)pyridin-2 -yl)ethyl] acetamid.
- 13. Farmaceutisk sammensætning, der omfatter en inert bærer og en forbindelse ifølge et hvilket som helst af de foregående krav eller et farmaceutisk acceptabelt salt deraf.
- 14. Forbindelse ifølge et hvilket som helst af kravene 1-12 eller et farmaceutisk acceptabelt salt deraf til anvendelse i medicin.
- 15. Anvendelse af en forbindelse ifølge et hvilket som helst af kravene 1-12, eller et farmaceutisk acceptabelt salt deraf til fremstilling af et medikament til behandling eller styring af epilepsi; til behandling eller styring af smerte; eller til behandling eller forebyggelse af en søvnforstyrrelse.
- 16. Forbindelse ifølge et hvilket som helst af kravene 1-2 til anvendelse i en fremgangsmåde til behandling eller styring af epilepsi; til behandling eller styring af smerte; eller til behandling eller forebyggelse af en søvnforstyrrelse.
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US7875636B2 (en) | 2011-01-25 |
KR20080108539A (ko) | 2008-12-15 |
CA2648569A1 (en) | 2007-10-25 |
EP2010493B1 (en) | 2016-01-27 |
AU2007238755B2 (en) | 2012-07-12 |
AU2007238755A1 (en) | 2007-10-25 |
JP5269761B2 (ja) | 2013-08-21 |
CR10355A (es) | 2008-10-29 |
CN101466676A (zh) | 2009-06-24 |
WO2007120729A2 (en) | 2007-10-25 |
US20110112064A1 (en) | 2011-05-12 |
CA2648569C (en) | 2012-02-07 |
PL2010493T3 (pl) | 2016-08-31 |
IL194238A0 (en) | 2009-09-22 |
ES2566481T3 (es) | 2016-04-13 |
MA30462B1 (fr) | 2009-06-01 |
NO20084769L (no) | 2009-01-07 |
MX2008013238A (es) | 2008-10-21 |
WO2007120729A3 (en) | 2008-01-03 |
EP2010493A2 (en) | 2009-01-07 |
ECSP088804A (es) | 2008-11-27 |
CN101466676B (zh) | 2012-07-18 |
BRPI0710487A2 (pt) | 2012-06-05 |
GT200800214A (es) | 2009-02-25 |
RU2008144571A (ru) | 2010-05-20 |
JP2009534320A (ja) | 2009-09-24 |
US20090275550A1 (en) | 2009-11-05 |
US8263627B2 (en) | 2012-09-11 |
ZA200808024B (en) | 2009-11-25 |
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