DK1680124T3 - Bicycliske [3.1.0]-derivater som glycin-transporter-inhibitorer - Google Patents
Bicycliske [3.1.0]-derivater som glycin-transporter-inhibitorer Download PDFInfo
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- DK1680124T3 DK1680124T3 DK04795270.0T DK04795270T DK1680124T3 DK 1680124 T3 DK1680124 T3 DK 1680124T3 DK 04795270 T DK04795270 T DK 04795270T DK 1680124 T3 DK1680124 T3 DK 1680124T3
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- ylmethyl
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- aza
- bicyclo
- amide
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Claims (7)
1. Forbindelse ifølge formel I:
hvor: Y er (R100)k-R1-(R6)m; k er 0 eller 1; I = 0, 1,2 eller 3; m = 1, 2 eller 3; n erO, 1,2, 3 eller 4; o er 0 eller 1; p er 0, 1,2 eller 3; q erO, 1,2, 3 eller4; r er 1 eller 2; s er 0, 1,2, 3 eller 4; t erO eller 1; u er 1, 2 eller 3; ver 1,2 eller3; R100 er -CH2-, -CH(CrC3)alkyl-, -C(=0)- eller -S02-; R1 er-(Ci-C6)alkyl, -(C3-C8)cycloalkyl, -(4 til 7-leddet) heterocycloalkyl,-(CH2)i-(Ce-Cioaryl) eller -(5 til 10-leddet) heteroaryl, eller -(5 til 10-leddet) tetrahydro-heteroaryl; hver R6 kan være identisk eller forskellige og er uafhængigt valgt blandt H, halogen, -(Ci-Ce)alkyl-B, (C1-C7) alkoxy-D, (C2-C4)alkenoxy, (Ci-C6)alkyl-OH, -OH, CN, -NO2, -CR7R8R9, -NR20R21, -NHCOalkyl(Ci-C3), NHS02alkyl(Ci-C3), C(=0)0R22, -R23-C(=0)0R22, -C(=0)NH2, phenyl-E, phenoxy-F, morpholine, -NR20R21, aryl, heteroaryl, -S-R24, og -SO2-R25; B og D er hver især uafhængigt H, OH, phenyl, diphenyl eller trifluor; E og F er hver især uafhængigt H, alkyl eller halogen; R7, R8 og R9 er hver især uafhængigt H, (C1-C4) alkyl, -OH, -0-(Ci-C4)alkyl,-CN, -NR26R27 og -NHC(=0) (CrC3)alkyl, hvor alkylgrupperne eventuelt er substituerede med OH, OCH3, NH2, NHC(=0)(Ci-C3)alkyl, eller R7 og R8 danner, sammen med de carbonatomer, hvortil de er forbundet, en (C3-C7)cycloalkylring, eller en (C4-C7)-heterocycloalkylring, som indeholder 1-3 heteroatomer valgt blandt N, O, S og eventuelt indeholder en C=0-gruppe; R20 og R21 er hver især uafhængigt H eller (Ci-C6)alkyl; eller R20 og R21 kan være forbundet med 4 til 7 carbonatomer, hvor fra ét til tre af de nævnte carbonatomer eventuelt kan være erstattede med O, N eller S, for dannelse af en heterocycloalkylring; eller R20 og R21 kan være forbundet med 3 til 7 atomer valgt blandt C, N, O eller S, for dannelse af en 5 til 10-leddet heteroarylring; R22, R23 og R24 er hver især uafhængigt H, eller (Ci-Cs)alkyl; R25 er (Ci-Cs)alkyl; R26 og R27 er hver især uafhængigt H eller (Ci-C3)alkyl; eller R26 og R27 kan være forbundet med 4 til 7 carbonatomer for dannelse af en heterocycloalkylring; R2 og R3 er hver især uafhængigt H eller (Ci-C3)alkyl; R4 og R5 er hver især uafhængigt H eller (C1-C3) alkyl; A er H; R12 og R13 er hver især uafhængigt H eller -(Ci-C4)alkyl; eller R12 og R13 kan være forbundet med 4 til 7 carbonatomer for dannelse af en heterocycloalkylring; X er en binding -CH2-(R29)P, -C(=0) eller -S02; R29 er -(Ci-C3)alkyl; W er -(C3-C6)cycloalkyl, -(3 til 7-leddet) heterocycloalkyl, -(3 til 7-leddet) hetero-cycloalkyl med 1 eller 2 C=0-grupper, phenyl, eller-(5 til 7-leddet) heteroaryl; R30 er -(Ci-C4)alkyl, -(Ci-C3)alkoxy, CN, -F, -Cl, -Br, -I, -NR18R19, -NHC(=0)R18, -SCH3 eller-C(=0)CH3; R18 og R19 er hver især uafhængigt H eller -(Ci-C3)alkyl; Q er en binding, -CH-(R31)r, -C(=0) eller -SO2; R31 er uafhængigt H eller -(Ci-C3)alkyl; Z er -(C3-C8)cycloalkyl, -(4 til 8-leddet) heterocycloalkyl, phenyl eller (5 til 7-leddet) heteroaryl; R14 er F, Cl, Br, I, V, H, -NR16R17, -OR16, -C(=0)NR16R17, -(S02)NR16R17 eller -NR32-C=0-R33, R15 er -(Ci-C3)alkyl, -(Ci-C3)alkoxy, -F, -Br, -Cl, -I -OH eller -CN; V er -(C3-C8)cycloalkyl, -(Ci-Cs)alkyl, (5 til 7-leddet) heterocycloalkyl, (5 til 7-leddet) heterocycloalkyl substitueret med 1 eller 2 C=0-grupper eller 1, 2, eller 3 (C1-C5)-alkylgrupper; R16 og R17 er hver især uafhængigt H, -(Ci-C6)alkyl-(R34)U eller (C3-C8)cycloalkyl-(R35)v; eller R16 og R17 danner sammen med det nitrogenatom, hvortil de er forbundet, en 4 til 7-leddet heterocycloalkylring, som eventuelt indeholder fra 1 til 3 yderligere heteroatomer uafhængigt valgt blandt N, S og O, og indeholder C=0, hvor den nævnte heterocycloalkylring eventuelt og uafhængigt er substitueret med 1 til 3 substituenter uafhængigt valgt blandt (Ci-C4)alkyl, OH, (Ci-C4)alkoxy, NH2, -NH(C=0)alkyl, -N-(Ci-C3)alkyl)2, -C(=0)CH3, CONH2, C02H, CH2OH, CH20alkyl(C2-C4) og (5 til 7-leddet) heterocycloalkyl; R32 og R33 er hver især uafhængigt H eller (Ci-Cs)alkyl; eller R32 og R33 kan tages sammen for dannelse af en 3-7-leddet cycloalkylring, en 3-7-leddet heterocycloalkylring med 1 til 3 heteroatomer eller en 5-7-leddet hetero-arylring med 1 til 3 heteroatomer; R34 og R35 er hver især uafhængigt H, OH, (Ci-Cs)alkyl, (C2-C4)alkoxy, NH2, NH(C=0)(Ci-C3)alkyl, eller en 5 til 7-leddet heterocycloalkyl; eller R34 og R35 kan tages sammen for dannelse af en bro indeholdende 1-2 carbonatomer; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse ifølge krav 1, hvor stereokemien er som i formel II: I II
3. Forbindelse ifølge krav 1, hvor stereokemien er som i formel III:
III
4. Forbindelse ifølge krav 1, valgt fra gruppen bestående af: Thiophen-2-carboxylsyre-(3-cyclohexylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methylbenzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methoxybenzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(1-hydroxy-cyclohexyl- methyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-pyridin-3-ylmethyl-3-aza- bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-[3-(4-chlor-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-fluor-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(2-ethyl-5-methyl-3H-imidazol-4-ylmethyl)-3-aza-bicyclo- [3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(2-p-tolyl-ethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-thiophen-2-ylmethyl-3-aza-bicyclo[3.1,0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-quinolin-2-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-nitrobenzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-methylbenzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3,4,5-trimethoxy-benzyl)- 3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-pyridin-2-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-[3-(3,4-dichlor-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-methoxybenzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(5-hydroxymethyl-furan-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(1H-indol-3-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-pyridin-4-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(2-methylbenzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-phenoxybenzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-naphthalen-1-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-phenethyl-3-aza-bicyclo- [3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-benzo[1,3]dioxol-5-ylmethyl-3-aza-bicyclo[3.1.0]hex-6- ylmethyl)-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-naphthalen-2-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-[3-(2,2-diphenyl-ethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-quinolin-4-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-quinolin-3-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-trifluormethoxy-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-methyl-benzo[b]-thiophen-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-benzofuran-2-ylmethyl-3-aza-bicyclo[3.1,0]hex-6-ylmethyl)-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-quinoxalin-6-ylmethyl-3-aza-bicyclo[3.1,0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(2-fluor-5-trifluormethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-{3-[4-(2-hydroxy-ethoxy)-benzyl]-3-aza-bicyclo[3.1.0]hex-6-ylmethyl}-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methansulfonyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(1-methyl-1 H-pyrrol-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-furan-3-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-thiophen-3-ylmethyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-trifluormethoxy-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butoxy-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-bromo-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-isopropyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-biphenyl-4-ylmethyl-3-aza-bicyclo[3.1,0]hex-6-ylmethyl)-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-cyano-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-hydroxybenzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-trifluormethyl-benzyl)- 3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-ethoxy-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methylsulfanyl-benzyl)- 3- aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-phenoxybenzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; 4- (6-{[(3-fluor-4-morpholin-4-yl-phenyl)-(thiophen-2-carbonyl)-amino]-methyl}-3-aza-bicyclo[3.1,0]hex-3-ylmethyl)-benzoesyre-methylester; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-isobutyl-benzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-acetylamino-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-imidazol-1-yl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-benzyloxy-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-pyridin-2-yl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-morpholin-4-yl-benzyl)- 3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-pyrimidin-5-yl-benzyl)- 3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4,5,6,7-tetrahydro- benzothiazol-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-propoxy-benzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(3-phenylpropyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(5-ethyl-thiophen-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(3-ethoxy-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-propoxy-benzyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-allyloxy-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-hexyl-3-aza-bicyclo- [3.1.0] hex-6-ylmethyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(4- morpholin-4-yl-benzyl)-amid; thiophen-2-carboxylsyre-(4-tert-butyl-phenyl)-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]- hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(4-piperidin-1 -yl-phenyl)-amid; thiophen-2-carboxylsyre-(4-diethylamino-phenyl)-[3-(4-ethyl-benzyl)-3-aza-bicyclo- [3.1.0] hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-[4-(4-ethyl-2,6-dioxo-piperidin-4-yl)-phenyl]-amid; thiophen-2-carboxylsyre-(4-benzyl-phenyl)-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex- 6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(5-benzyl-pyridin-2-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(6-p-tolyloxy-pyridin-3-ylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-cyclohexylmethyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre {3-[2-fluor-4-(1-hydroxy-1-methyl-ethyl)-benzyl]-3-aza-bicyclo- [3.1.0]hex-6-ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6- morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-{4- [ethyl-(2-hydroxy-ethyl)-amino]-phenyl}-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-[4-(2-oxo-pyrrolidin-1-yl)-phenyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-[4- (morpholin-4-carbonyl)-phenyl]-amid; thiophen-2-carboxylsyre-{3-[4-(cyano-dimethyl-methyl)-benzoyl]-3-aza-bicyclo[3.1.0]-hex-6-ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-{3-[4-(cyano-dimethyl-methyl)-benzoyl]-3-aza-bicyclo[3.1.0]-hex-6-ylmethyl}-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [4-(tetrahydro-pyran-4-yl)-phenyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [4-(2-oxo-pyrrolidin-1-yl)-phenyl]-amid; 3-chlor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [4-(morpholin-4-carbonyl)-phenyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (4-morpholin-4-ylmethyl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (6-thiomorpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (6-chlor-pyridin-3-yl)-amid; 5-fluor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; 5-methyl-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-[ 1 -(tetra hyd ro-py ra n-4-yl )-pyrrol id i n-3-y l]-a m id; N-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-4-methyl-N-(6- morpholin-4-yl-pyridin-3-yl)-benzamid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(3,6-dihydro-2H-pyran-4-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-ethyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(tetrahydro-pyran-4-yl)-pyridin-3-yl]-amid; furan-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; 1 -methyl-1 H-pyrrol-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; 4-methyl-[1,2,3]thiadiazol-5-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]- hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; pyridin-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6- morpholin-4-yl-pyridin-3-yl)-amid; 2-methyl-thiazol-4-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (4-morpholin-4-yl-cyclohexyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (4-morpholin-4-yl-cyclohexyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (6-morpholin-4-ylmethyl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(5-butyl-pyridin-2-carbonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-cyclohexancarbonyl)-3-aza-bicyclo[3.1.0]hex- 6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-{3-[2-(4-tert-butyl-phenyl)-acetyl]-3-aza-bicyclo[3.1.0]hex-6- ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (4-diethylcarbamoyl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [1-(tetrahydro-pyran-4-yl)-piperidin-4-yl]-amid; 3-chlor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [3-(tetrahydro-pyran-4-yl)-3-aza-bicyclo[3.1.0]hex-6-yl]-amid; N-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-6-morpholin-4-yl-N- thiophen-2-ylmethyl-nicotinamid; thiophen-2-carboxylsyre {3-[3-(4-chlor-phenoxy)-benzensulfonyl]-3-aza-bicyclo[3.1.0]- hex-6-ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-trifluormethoxy- benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-cyano-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-butyl-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(toluen-4-sulfonyl)-3-aza- bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-{3-[4-(4-chlor-phenoxy)-benzensulfonyl]-3-aza-bicyclo[3.1.0]- hex-6-ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4'-fluor-biphenyl-4-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(1-methyl-1 H-imidazol-4-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-bromo-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-bromo-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(2-acetylamino-4-methyl-thiazol-5-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(4-diethylcarbamoyl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methylthiophen-2-sulfonyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-chlor-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 3-chlor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]-hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-fluor-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-[4-(2-oxo-pyrrolidin-1-yl)-phenyl]-amid; thiophen-2-carboxylsyre-[3-(benzo[b]thiophen-2-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(biphenyl-3-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-(3-phenylmethansulfonyl-3-aza-bicyclo[3.1.0]hex-6-ylmethyl)-amid; 3- chlor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]-hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-chlor-phenylmethansulfonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 5-fluor-thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]-hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-[4-(morpholin-4-carbonyl)-phenyl]-amid; 4- methyl-[1,2,3]thiadiazol-5-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; 1-methyl-1H-pyrrol-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo- [3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(quinolin-8-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-propyl-benzensul- fonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-methoxybenzen-sulfonyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(2-methoxy-4-methyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-trifluormethyl-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(isoquinolin-5-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-isopropyl-benzensul- fonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(5-brom-6-chlor-pyridin-3-sulfonyl)-3-aza-bicyclo[3.1.0]hex- 6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-ethyl-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-fluor-phenylmethan-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-nitrobenzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; 4-(6-{[(3-fluor-4-morpholin-4-yl-phenyl)-(thiophen-2-carbonyl)-amino]-methyl}-3-aza- bicyclo[3.1.0]hexan-3-sulfonyl)-benzoesyre; thiophen-2-carboxylsyre-[3-(biphenyl-4-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4-butoxy-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[3-(4'-chlor-biphenyl-3-sulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; cyclopropancarboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-pentyl-benzensul- fonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; cyclopentancarboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(4-phenoxy-benzen-sulfonyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-amid; cyclobutancarboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; 3-[4-(6-{[(3-fluor-4-morpholin-4-yl-phenyl)-(thiophen-2-carbonyl)-amino]-methyl}-3-aza- bicyclo[3.1.0]hexan-3-sulfonyl)-phenyl]-propionsyre-methylester; thiophen-2-carboxylsyre-[3-(4-acetylamino-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6- ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-4-methyl-N-(6- morpholin-4-yl-pyridin-3-yl)-benzamid; thiophen-2-carboxylsyre {3-[4-(1,1-dimethyl-propyl)-benzensulfonyl]-3-aza-bicyclo- [3.1.0] hex-6-ylmethyl}-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-(3-fluor-4-morpholin-4-yl-phenyl)-[3-(naphthalen-2-sulfonyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzensulfonyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(6-morpholin-4-yl-pyridin-3-yl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-isonicotinamid; furan-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 3-brom-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 3-methyl-furan-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3-fluor-4-morpholin-4-yl-phenyl)-amid; 5-methyl-isoxazol-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morphol in-4-yl-phenyl)-2-methoxy-benzamid; 3-methyl-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morphol in-4-yl-phenyl)-4-methoxy-benzamid; 2.5- dimethyl-furan-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-4-methyl-benzamid; 5-methyl-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 5-tert-butyl-2-methyl-2H-pyrazole-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo- [3.1.0] hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-3,5-dimethoxy-benzamid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morphol in-4-yl-phenyl)-3-methoxy-benzamid; 1.5- dimethyl-1H-pyrazol-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 3- ethoxy-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; isoxazol-5-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3- fluor-4-morpholin-4-yl-phenyl)-amid; 1 -methyl-1 H-imidazol-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; furan-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-2-methyl-benzamid; 4- cyano-N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morpho-lin-4-yl-phenyl)-benzamid; 4-ethyl-N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morpho-lin-4-yl-phenyl)-benzamid; 3- chlor-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-2-methylsulfanyl-nicotinamid; 1 -methyl-1 H-pyrazol-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-2,4-difluor-N-(3-fluor-4-morpholin-4-yl-phenyl)-benzamid; N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morpholin-4-yl-phenyl)-nicotinamid; 3,5-dimethyl-1 H-pyrrol-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 1 -methyl-1 H-pyrrol-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-yl-methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 2-methyl-thiazol-4-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 4- brom-N-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-N-(3-fluor-4-morpho-lin-4-yl-phenyl)-benzamid; 5- oxo-pyrrolidin-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 1-acetyl-pyrrolidin-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-3-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; 5-brom-thiophen-2-carboxylsyre-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-yl- methyl]-(3-fluor-4-morpholin-4-yl-phenyl)-amid; thiophen-2-carboxylsyre-[4-(4-acetyl-[1,4]diazepan-1-yl)-3-fluor-phenyl]-[3-(4-ethyl-benzyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[6-(4-acetyl-piperazin-1-yl)-pyridin-3-yl]-[3-(4-tert-butyl- benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- (3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-5'-yl)-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(4-methyl-piperazin-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- {6-[ethyl-(2-methoxy-ethyl)-amino]-pyridin-3-yl}-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-{6-[(1 H-imidazol-2-ylmethyl)-methyl-amino]-pyridin-3-yl}-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]-[6-(3-oxo-piperazin-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- {6-[(2-methoxy-ethyl)-methyl-amino]-pyridin-3-yl}-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(3-dimethylamino-pyrrolidin-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(4-methyl-[1,4]diazepan-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(3-diethylamino-pyrrolidin-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-(6-[1,3']bipyrrolidinyl-1'-yl-pyridin-3-yl)-[3-(4-tert-butyl-ben-zoyl)-3-aza-bicyclo[3.1,0]hex-6-ylmethyl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(3-morpholin-4-yl-azetidin-1-yl)-pyridin-3-yl]-amid; thiophen-2-carboxylsyre-[3-(4-tert-butyl-benzoyl)-3-aza-bicyclo[3.1.0]hex-6-ylmethyl]- [6-(3-morpholin-4-yl-pyrrolidin-1-yl)-pyridin-3-yl]-amid; eller et farmaceutisk acceptabelt salt deraf.
5. Farmaceutisk sammensætning omfattende en forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, og et farmaceutisk acceptabelt bærestof eller fortyndingsmiddel.
6. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, til anvendelse som et lægemiddel.
7. Forbindelse ifølge krav 1 eller et farmaceutisk acceptabelt salt deraf, til anvendelse ved behandlingen af en lidelse eller tilstand valgt blandt psykose, skizofreni, adfærdslidelse, destruktiv adfærdslidelse, bipolær lidelse, psykotiske episoder med angst, angst associeret med psykose, psykotiske humørlidelser, alvorlige depressive lidelser, humørlidelser associeret med psykotiske lidelser, akut mani, depression associeret med bipolar lidelse, humørlidelser associeret med skizofreni, opførselsmæssige manifestationer af mental retardering, opførselslidelser, autistiske lidelser, bevægelseslidelser, Tourette's syndrom, akinetisk-rigid syndrom, bevægelseslidelser associeret med Parkinson's syge, sendyskinesi, andre medikamentinducerede og neurodegenerations-baserede dyskinesier, opmærksomheds-deficit hyperaktivitetslidelse, kognitive lidelser, demens og hukommelseslidelser.
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NZ546012A (en) * | 2003-10-14 | 2009-12-24 | Pfizer Prod Inc | Bicyclic [3.1.0] derivatives as glycine transporter inhibitors |
GB0408772D0 (en) * | 2004-04-20 | 2004-05-26 | Glaxo Group Ltd | Compounds |
GB0408774D0 (en) * | 2004-04-20 | 2004-05-26 | Glaxo Group Ltd | Compounds |
JP2008503585A (ja) * | 2004-06-22 | 2008-02-07 | シェーリング コーポレイション | カンナビノイドレセプターリガンド |
JP4193949B2 (ja) * | 2005-04-08 | 2008-12-10 | ファイザー・プロダクツ・インク | I型グリシン輸送阻害剤としての二環式[3.1.0]ヘテロアリールアミド |
WO2007053499A2 (en) | 2005-11-01 | 2007-05-10 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of ccr2 |
US8067457B2 (en) | 2005-11-01 | 2011-11-29 | Millennium Pharmaceuticals, Inc. | Compounds useful as antagonists of CCR2 |
WO2007135527A2 (en) * | 2006-05-23 | 2007-11-29 | Pfizer Products Inc. | Benzimidazolyl compounds |
WO2008065500A2 (en) * | 2006-11-30 | 2008-06-05 | Pfizer Products Inc. | Heteroaryl amides as type i glycine transport inhibitors |
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CA2746444A1 (en) * | 2008-12-12 | 2010-06-17 | Vanderbilt University | 3.3.0 bicyclic glyt1 inhibitors and methods of making and using same |
WO2010078348A1 (en) * | 2008-12-29 | 2010-07-08 | Vanderbilt University | 3.1.0 bicyclic glyt1 inhibitors and methods of making and using same |
FR2944283B1 (fr) * | 2009-04-14 | 2011-05-06 | Sanofi Aventis | Derives de n-°(2-aza-bicyclo°2.1.1!hex-1-yl)-aryl-methyl!- heterobenzamide, leur preparation et leur application en therapeutique |
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