HRP20161774T1 - Novi diazaspirocikloalkan i azaspirocikloalkan - Google Patents
Novi diazaspirocikloalkan i azaspirocikloalkan Download PDFInfo
- Publication number
- HRP20161774T1 HRP20161774T1 HRP20161774TT HRP20161774T HRP20161774T1 HR P20161774 T1 HRP20161774 T1 HR P20161774T1 HR P20161774T T HRP20161774T T HR P20161774TT HR P20161774 T HRP20161774 T HR P20161774T HR P20161774 T1 HRP20161774 T1 HR P20161774T1
- Authority
- HR
- Croatia
- Prior art keywords
- diazaspiro
- carbonyl
- carboxylate
- benzo
- nonane
- Prior art date
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- -1 2,3-dihydro-1H-isoindol-2-yl Chemical group 0.000 claims 37
- 150000001875 compounds Chemical class 0.000 claims 19
- 125000000753 cycloalkyl group Chemical group 0.000 claims 19
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 150000003839 salts Chemical class 0.000 claims 5
- 125000004244 benzofuran-2-yl group Chemical group [H]C1=C(*)OC2=C([H])C([H])=C([H])C([H])=C12 0.000 claims 4
- 125000002249 indol-2-yl group Chemical group [H]C1=C([H])C([H])=C2N([H])C([*])=C([H])C2=C1[H] 0.000 claims 4
- 125000005359 phenoxyalkyl group Chemical group 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- 125000003884 phenylalkyl group Chemical group 0.000 claims 4
- CHMCNIRNOVQGFL-DAFODLJHSA-N (e)-1-[2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-3-(3,5-dichlorophenyl)prop-2-en-1-one Chemical compound ClC1=CC(Cl)=CC(\C=C\C(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 CHMCNIRNOVQGFL-DAFODLJHSA-N 0.000 claims 3
- ZVAPUQBYQNLXGP-UHFFFAOYSA-N [2-fluoro-4-(trifluoromethyl)phenyl]methyl 2-(4,5,6,7-tetrahydro-2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound FC1=CC(C(F)(F)F)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)C2CC3=NNN=C3CC2)CC1 ZVAPUQBYQNLXGP-UHFFFAOYSA-N 0.000 claims 3
- 125000004122 cyclic group Chemical group 0.000 claims 3
- WSFSSNUMVMOOMR-BJUDXGSMSA-N methanone Chemical compound O=[11CH2] WSFSSNUMVMOOMR-BJUDXGSMSA-N 0.000 claims 3
- FMWQENMZFHAGIB-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 FMWQENMZFHAGIB-UHFFFAOYSA-N 0.000 claims 2
- ZLQMWQUCFJPYJU-UHFFFAOYSA-N 3-[[2-fluoro-4-(trifluoromethoxy)phenyl]methyl]-2-(4,5,6,7-tetrahydro-2H-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylic acid Chemical compound OC(=O)N1CCC2(CN(C2Cc2ccc(OC(F)(F)F)cc2F)C(=O)C2CCc3n[nH]nc3C2)CC1 ZLQMWQUCFJPYJU-UHFFFAOYSA-N 0.000 claims 2
- LRBMHEFLWCPAKK-UHFFFAOYSA-N [2-methyl-4-(trifluoromethoxy)phenyl]methyl 2-(4,5,6,7-tetrahydro-2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound CC1=CC(OC(F)(F)F)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)C2CC3=NNN=C3CC2)CC1 LRBMHEFLWCPAKK-UHFFFAOYSA-N 0.000 claims 2
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 2
- 125000001188 haloalkyl group Chemical group 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 125000004076 pyridyl group Chemical group 0.000 claims 2
- 125000001544 thienyl group Chemical group 0.000 claims 2
- XHBMWGNALFPNJS-UHFFFAOYSA-N (2,6-dichloropyridin-4-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound ClC1=NC(Cl)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 XHBMWGNALFPNJS-UHFFFAOYSA-N 0.000 claims 1
- FDWYOSZDAODUPT-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-(2-oxo-3h-1,3-benzoxazole-6-carbonyl)-2,7-diazaspiro[3.4]octane-7-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CC3(CN(C3)C(=O)C=3C=C4OC(=O)NC4=CC=3)CC2)=C1 FDWYOSZDAODUPT-UHFFFAOYSA-N 0.000 claims 1
- BCWLOWIHVLLWJV-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-(2-oxo-3h-1,3-benzoxazole-6-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C=3C=C4OC(=O)NC4=CC=3)CC2)=C1 BCWLOWIHVLLWJV-UHFFFAOYSA-N 0.000 claims 1
- ZKCDXPLZDIFJFJ-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-(2h-triazol-4-ylmethylcarbamoyl)-7-azaspiro[3.5]nonane-7-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CCC3(CC(C3)C(=O)NCC3=NNN=C3)CC2)=C1 ZKCDXPLZDIFJFJ-UHFFFAOYSA-N 0.000 claims 1
- JUQSJACIWQDEDP-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-(4-amino-3-hydroxybenzoyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1=C(O)C(N)=CC=C1C(=O)N1CC2(CCN(CC2)C(=O)OCC=2C=C(Cl)C=C(Cl)C=2)C1 JUQSJACIWQDEDP-UHFFFAOYSA-N 0.000 claims 1
- NBHVXJTURZSEKR-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 2-[(2-oxo-3h-1,3-benzoxazol-6-yl)methyl]-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CCC3(CN(CC=4C=C5OC(=O)NC5=CC=4)C3)CC2)=C1 NBHVXJTURZSEKR-UHFFFAOYSA-N 0.000 claims 1
- CBHHBVPSSNFVJH-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CC3(CC(C3)NC(=O)C3=CC4=NNN=C4C=C3)C2)=C1 CBHHBVPSSNFVJH-UHFFFAOYSA-N 0.000 claims 1
- MHRZSBMHABOVDN-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 6-[(2-oxo-3h-1,3-benzoxazole-6-carbonyl)amino]-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CC3(CC(C3)NC(=O)C=3C=C4OC(=O)NC4=CC=3)C2)=C1 MHRZSBMHABOVDN-UHFFFAOYSA-N 0.000 claims 1
- SIBYCEPFLIGWEY-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl 7-(2-oxo-3h-1,3-benzoxazole-6-carbonyl)-2,7-diazaspiro[3.5]nonane-2-carboxylate Chemical compound ClC1=CC(Cl)=CC(COC(=O)N2CC3(C2)CCN(CC3)C(=O)C=2C=C3OC(=O)NC3=CC=2)=C1 SIBYCEPFLIGWEY-UHFFFAOYSA-N 0.000 claims 1
- LLKASGYDVIKVNO-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl n-[2-(2h-benzotriazole-5-carbonyl)-2-azaspiro[3.3]heptan-6-yl]carbamate Chemical compound ClC1=CC(Cl)=CC(COC(=O)NC2CC3(C2)CN(C3)C(=O)C2=CC3=NNN=C3C=C2)=C1 LLKASGYDVIKVNO-UHFFFAOYSA-N 0.000 claims 1
- VAWHLBLARXWUKL-UHFFFAOYSA-N (3,5-dichlorophenyl)methyl n-[2-[(2-oxo-3h-1,3-benzoxazol-6-yl)sulfonyl]-2-azaspiro[3.3]heptan-6-yl]carbamate Chemical compound ClC1=CC(Cl)=CC(COC(=O)NC2CC3(C2)CN(C3)S(=O)(=O)C=2C=C3OC(=O)NC3=CC=2)=C1 VAWHLBLARXWUKL-UHFFFAOYSA-N 0.000 claims 1
- VVIDKHAAKSYKTM-UHFFFAOYSA-N (3-chloro-4-fluorophenyl)methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound C1=C(Cl)C(F)=CC=C1COC(=O)N1CC2(CC(C2)NC(=O)C2=CC3=NNN=C3C=C2)C1 VVIDKHAAKSYKTM-UHFFFAOYSA-N 0.000 claims 1
- UHEJWZYXFUKRNS-UHFFFAOYSA-N (3-chloro-4-methylphenyl)methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound C1=C(Cl)C(C)=CC=C1COC(=O)N1CC2(CC(C2)NC(=O)C2=CC3=NNN=C3C=C2)C1 UHEJWZYXFUKRNS-UHFFFAOYSA-N 0.000 claims 1
- CQWQPLALAGQBCT-UHFFFAOYSA-N (3-chloro-5-cyanophenyl)methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound N#CC1=CC(Cl)=CC(COC(=O)N2CC3(CC(C3)NC(=O)C3=CC4=NNN=C4C=C3)C2)=C1 CQWQPLALAGQBCT-UHFFFAOYSA-N 0.000 claims 1
- JUVRTXYUUUHSQR-UHFFFAOYSA-N (5,6-dichloropyridin-3-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound N1=C(Cl)C(Cl)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 JUVRTXYUUUHSQR-UHFFFAOYSA-N 0.000 claims 1
- DCHKTADRRIRKOH-UHFFFAOYSA-N (5-bromopyridin-3-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound BrC1=CN=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 DCHKTADRRIRKOH-UHFFFAOYSA-N 0.000 claims 1
- GIMIOPSJDCYEST-UHFFFAOYSA-N (5-bromothiophen-3-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound S1C(Br)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 GIMIOPSJDCYEST-UHFFFAOYSA-N 0.000 claims 1
- TWZGGFPYNFZHRE-UHFFFAOYSA-N (5-chlorothiophen-3-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound S1C(Cl)=CC(COC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 TWZGGFPYNFZHRE-UHFFFAOYSA-N 0.000 claims 1
- DRNZBDANNBJISL-UHFFFAOYSA-N (6-chloropyridin-3-yl)methyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1=NC(Cl)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CC1 DRNZBDANNBJISL-UHFFFAOYSA-N 0.000 claims 1
- COSPWWJGDNPZSN-UHFFFAOYSA-N 1-(3,5-dichlorophenyl)ethyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1CC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CCN1C(=O)OC(C)C1=CC(Cl)=CC(Cl)=C1 COSPWWJGDNPZSN-UHFFFAOYSA-N 0.000 claims 1
- YMNUUEPTOAODOJ-UHFFFAOYSA-N 1-[2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-2-(4-chloro-2-propan-2-ylphenoxy)ethanone Chemical compound CC(C)C1=CC(Cl)=CC=C1OCC(=O)N1CCC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CC1 YMNUUEPTOAODOJ-UHFFFAOYSA-N 0.000 claims 1
- MIWTUCTXRDTYFF-UHFFFAOYSA-N 1-[2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-3-(3,5-dichlorophenyl)propan-1-one Chemical compound ClC1=CC(Cl)=CC(CCC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 MIWTUCTXRDTYFF-UHFFFAOYSA-N 0.000 claims 1
- GTOOLRZGLJZZBK-UHFFFAOYSA-N 1-[2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-3-[4-(trifluoromethoxy)phenyl]propan-1-one Chemical compound C1=CC(OC(F)(F)F)=CC=C1CCC(=O)N1CCC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CC1 GTOOLRZGLJZZBK-UHFFFAOYSA-N 0.000 claims 1
- SFWJESQUECBVOV-UHFFFAOYSA-N 1-[2-(4,5,6,7-tetrahydro-2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]-3-[4-(trifluoromethoxy)phenyl]propan-1-one Chemical compound C1=CC(OC(F)(F)F)=CC=C1CCC(=O)N1CCC2(CN(C2)C(=O)C2CC3=NNN=C3CC2)CC1 SFWJESQUECBVOV-UHFFFAOYSA-N 0.000 claims 1
- GDVCDYGMKVAHQS-UHFFFAOYSA-N 1-[2-(4-amino-3-hydroxybenzoyl)-2,7-diazaspiro[3.5]nonan-7-yl]-3-(3,5-dichlorophenyl)propan-1-one Chemical compound C1=C(O)C(N)=CC=C1C(=O)N1CC2(CCN(CC2)C(=O)CCC=2C=C(Cl)C=C(Cl)C=2)C1 GDVCDYGMKVAHQS-UHFFFAOYSA-N 0.000 claims 1
- PKUNUUKPRXYOJP-UHFFFAOYSA-N 2-(2H-benzotriazole-5-carbonyl)-3-[(3-chlorophenyl)methyl]-2,7-diazaspiro[3.5]nonane-7-carboxylic acid Chemical compound C1CN(CCC12CN(C2CC3=CC(=CC=C3)Cl)C(=O)C4=CC5=NNN=C5C=C4)C(=O)O PKUNUUKPRXYOJP-UHFFFAOYSA-N 0.000 claims 1
- QXJFWUBJFAHSGO-UHFFFAOYSA-N 2-(2H-benzotriazole-5-carbonyl)-3-[(4-chlorophenyl)methyl]-2,7-diazaspiro[3.5]nonane-7-carboxylic acid Chemical compound C1CN(CCC12CN(C2CC3=CC=C(C=C3)Cl)C(=O)C4=CC5=NNN=C5C=C4)C(=O)O QXJFWUBJFAHSGO-UHFFFAOYSA-N 0.000 claims 1
- YVMNKCFORDUTCB-UHFFFAOYSA-N 2-(2h-benzotriazole-5-carbonyl)-n-[(3,5-dichlorophenyl)methyl]-2,7-diazaspiro[3.5]nonane-7-carboxamide Chemical compound ClC1=CC(Cl)=CC(CNC(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 YVMNKCFORDUTCB-UHFFFAOYSA-N 0.000 claims 1
- CQATZYOPEZUCOU-UHFFFAOYSA-N 2-(4-chloro-2-propan-2-ylphenoxy)-1-[2-(4,5,6,7-tetrahydro-2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonan-7-yl]ethanone Chemical compound CC(C)C1=CC(Cl)=CC=C1OCC(=O)N1CCC2(CN(C2)C(=O)C2CC3=NNN=C3CC2)CC1 CQATZYOPEZUCOU-UHFFFAOYSA-N 0.000 claims 1
- OQHQOOLVQDEIGL-UHFFFAOYSA-N 2-methyl-2,7-diazaspiro[4.4]nonane Chemical compound C1N(C)CCC11CNCC1 OQHQOOLVQDEIGL-UHFFFAOYSA-N 0.000 claims 1
- CFSPZDAURKTLRA-UHFFFAOYSA-N 2-oxo-n-[2-(4-phenylbutanoyl)-2-azaspiro[3.3]heptan-6-yl]-3h-1,3-benzoxazole-6-sulfonamide Chemical compound C1C2(CC(C2)NS(=O)(=O)C=2C=C3OC(=O)NC3=CC=2)CN1C(=O)CCCC1=CC=CC=C1 CFSPZDAURKTLRA-UHFFFAOYSA-N 0.000 claims 1
- ZWNGWUHFAOBESL-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[2-(5-chloro-1-benzofuran-2-carbonyl)-2,7-diazaspiro[4.4]nonan-7-yl]methanone Chemical compound C1=CC2=NNN=C2C=C1C(=O)N(C1)CCC1(C1)CCN1C(=O)C1=CC2=CC(Cl)=CC=C2O1 ZWNGWUHFAOBESL-UHFFFAOYSA-N 0.000 claims 1
- FKJBPUXYUUDFRL-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[7-(3,5-dichlorobenzoyl)-2,7-diazaspiro[3.5]nonan-2-yl]methanone Chemical compound ClC1=CC(Cl)=CC(C(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 FKJBPUXYUUDFRL-UHFFFAOYSA-N 0.000 claims 1
- IJMSCUUGZYBRML-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[7-[2-(3-chlorophenyl)ethylsulfonyl]-2,7-diazaspiro[3.5]nonan-2-yl]methanone Chemical compound ClC1=CC=CC(CCS(=O)(=O)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 IJMSCUUGZYBRML-UHFFFAOYSA-N 0.000 claims 1
- WXEFNHJXTXKSAR-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[7-[5-(3,5-dichlorophenyl)-1,3,4-oxadiazol-2-yl]-2,7-diazaspiro[3.5]nonan-2-yl]methanone Chemical compound ClC1=CC(Cl)=CC(C=2OC(=NN=2)N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)=C1 WXEFNHJXTXKSAR-UHFFFAOYSA-N 0.000 claims 1
- UEEMHDQTRLSWSV-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[7-[5-(4-chlorophenyl)-1,3,4-oxadiazol-2-yl]-2,7-diazaspiro[3.5]nonan-2-yl]methanone Chemical compound C1=CC(Cl)=CC=C1C1=NN=C(N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)O1 UEEMHDQTRLSWSV-UHFFFAOYSA-N 0.000 claims 1
- YZFIDZNZVKFQOO-UHFFFAOYSA-N 2h-benzotriazol-5-yl-[7-[5-(4-chlorophenyl)-1,3,4-thiadiazol-2-yl]-2,7-diazaspiro[3.5]nonan-2-yl]methanone Chemical compound C1=CC(Cl)=CC=C1C1=NN=C(N2CCC3(CN(C3)C(=O)C3=CC4=NNN=C4C=C3)CC2)S1 YZFIDZNZVKFQOO-UHFFFAOYSA-N 0.000 claims 1
- NYTBQCGOVDPJFZ-UHFFFAOYSA-N 3-[[2-fluoro-4-(trifluoromethoxy)phenyl]methyl]-7-(4,5,6,7-tetrahydro-2H-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-2-carboxylic acid Chemical compound OC(=O)N1CC2(CCN(CC2)C(=O)C2CCc3n[nH]nc3C2)C1Cc1ccc(OC(F)(F)F)cc1F NYTBQCGOVDPJFZ-UHFFFAOYSA-N 0.000 claims 1
- BYIUMISFTNZECE-UHFFFAOYSA-N 6-(2H-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylic acid Chemical compound OC(=O)N1CC2(CC(C2)NC(=O)c2ccc3[nH]nnc3c2)C1 BYIUMISFTNZECE-UHFFFAOYSA-N 0.000 claims 1
- XCGGPJPPGDCVNV-DAFODLJHSA-N 6-[7-[(e)-3-(3,5-dichlorophenyl)prop-2-enoyl]-2,7-diazaspiro[3.5]nonane-2-carbonyl]-3h-1,3-benzoxazol-2-one Chemical compound ClC1=CC(Cl)=CC(\C=C\C(=O)N2CCC3(CN(C3)C(=O)C=3C=C4OC(=O)NC4=CC=3)CC2)=C1 XCGGPJPPGDCVNV-DAFODLJHSA-N 0.000 claims 1
- DBPDXQVNPSOVIS-UHFFFAOYSA-N 6-[7-[3-(3,5-dichlorophenyl)propanoyl]-2,7-diazaspiro[3.5]nonane-2-carbonyl]-3h-1,3-benzoxazol-2-one Chemical compound ClC1=CC(Cl)=CC(CCC(=O)N2CCC3(CN(C3)C(=O)C=3C=C4OC(=O)NC4=CC=3)CC2)=C1 DBPDXQVNPSOVIS-UHFFFAOYSA-N 0.000 claims 1
- OZEOFYOYWSWOOH-UHFFFAOYSA-N 6-[[7-[3-(3,5-dichlorophenyl)propanoyl]-7-azaspiro[3.5]nonan-2-yl]amino]-3h-1,3-benzoxazol-2-one Chemical compound ClC1=CC(Cl)=CC(CCC(=O)N2CCC3(CC(C3)NC=3C=C4OC(=O)NC4=CC=3)CC2)=C1 OZEOFYOYWSWOOH-UHFFFAOYSA-N 0.000 claims 1
- IKHGUXGNUITLKF-UHFFFAOYSA-N Acetaldehyde Chemical compound CC=O IKHGUXGNUITLKF-UHFFFAOYSA-N 0.000 claims 1
- 208000012902 Nervous system disease Diseases 0.000 claims 1
- VXDVTTQURJJEAI-UHFFFAOYSA-N [2-fluoro-4-(trifluoromethoxy)phenyl]methyl 2-(2h-triazol-4-ylmethylcarbamoyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound FC1=CC(OC(F)(F)F)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)NCC2=NNN=C2)CC1 VXDVTTQURJJEAI-UHFFFAOYSA-N 0.000 claims 1
- WUFPYBVDYIRBPK-UHFFFAOYSA-N [3-chloro-5-(trifluoromethoxy)phenyl]methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound FC(F)(F)OC1=CC(Cl)=CC(COC(=O)N2CC3(CC(C3)NC(=O)C3=CC4=NNN=C4C=C3)C2)=C1 WUFPYBVDYIRBPK-UHFFFAOYSA-N 0.000 claims 1
- BKODHPGTWSKSPK-UHFFFAOYSA-N [3-fluoro-5-(trifluoromethyl)phenyl]methyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound FC(F)(F)C1=CC(F)=CC(COC(=O)N2CC3(CC(C3)NC(=O)C3=CC4=NNN=C4C=C3)C2)=C1 BKODHPGTWSKSPK-UHFFFAOYSA-N 0.000 claims 1
- WYFPTWWEAHNRRX-UHFFFAOYSA-N [4-(trifluoromethoxy)phenyl]methyl 2-(2,4,6,7-tetrahydrotriazolo[4,5-c]pyridine-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1=CC(OC(F)(F)F)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)N2CC3=NNN=C3CC2)CC1 WYFPTWWEAHNRRX-UHFFFAOYSA-N 0.000 claims 1
- SSLQCKHZXSLZAW-UHFFFAOYSA-N [4-(trifluoromethyl)phenyl]methyl 2-(3a,4,5,6,7,7a-hexahydro-3h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1=CC(C(F)(F)F)=CC=C1COC(=O)N1CCC2(CN(C2)C(=O)C2CC3NN=NC3CC2)CC1 SSLQCKHZXSLZAW-UHFFFAOYSA-N 0.000 claims 1
- 230000001154 acute effect Effects 0.000 claims 1
- FDMZXCHSDXLTPL-UHFFFAOYSA-N benzyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1CC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CCN1C(=O)OCC1=CC=CC=C1 FDMZXCHSDXLTPL-UHFFFAOYSA-N 0.000 claims 1
- ZEZOUNUNZHNTRM-UHFFFAOYSA-N benzyl 2-[(2-oxo-3h-1,3-benzoxazol-6-yl)amino]-7-azaspiro[3.5]nonane-7-carboxylate Chemical compound C1CC2(CC(C2)NC=2C=C3OC(=O)NC3=CC=2)CCN1C(=O)OCC1=CC=CC=C1 ZEZOUNUNZHNTRM-UHFFFAOYSA-N 0.000 claims 1
- PEAJYDVPJADIQG-UHFFFAOYSA-N benzyl 6-(2h-benzotriazole-5-carbonylamino)-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound C1C2(CC(C2)NC(=O)C2=CC3=NNN=C3C=C2)CN1C(=O)OCC1=CC=CC=C1 PEAJYDVPJADIQG-UHFFFAOYSA-N 0.000 claims 1
- ZUVJKJYJTFBRTK-UHFFFAOYSA-N benzyl 6-[(2-oxo-3h-1,3-benzoxazol-6-yl)sulfonylamino]-2-azaspiro[3.3]heptane-2-carboxylate Chemical compound C1C2(CC(C2)NS(=O)(=O)C=2C=C3OC(=O)NC3=CC=2)CN1C(=O)OCC1=CC=CC=C1 ZUVJKJYJTFBRTK-UHFFFAOYSA-N 0.000 claims 1
- XSXDULMNIUDYQH-UHFFFAOYSA-N benzyl n-[2-(2h-benzotriazole-5-carbonyl)-2-azaspiro[3.3]heptan-6-yl]carbamate Chemical compound C1C2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CC1NC(=O)OCC1=CC=CC=C1 XSXDULMNIUDYQH-UHFFFAOYSA-N 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 125000006254 cycloalkyl carbonyl group Chemical group 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 230000003176 fibrotic effect Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 208000027866 inflammatory disease Diseases 0.000 claims 1
- 208000017169 kidney disease Diseases 0.000 claims 1
- 201000006370 kidney failure Diseases 0.000 claims 1
- 208000019423 liver disease Diseases 0.000 claims 1
- 238000004519 manufacturing process Methods 0.000 claims 1
- SBMMOQITUGJLQI-UHFFFAOYSA-N n-[2-(4-phenylbutanoyl)-2-azaspiro[3.3]heptan-6-yl]-2h-benzotriazole-5-carboxamide Chemical compound C1C2(CC(C2)NC(=O)C2=CC3=NNN=C3C=C2)CN1C(=O)CCCC1=CC=CC=C1 SBMMOQITUGJLQI-UHFFFAOYSA-N 0.000 claims 1
- QSDZSKSAPMAMLJ-UHFFFAOYSA-N n-[2-[3-(3,5-dichlorophenyl)propanoyl]-2-azaspiro[3.3]heptan-6-yl]-2h-benzotriazole-5-carboxamide Chemical compound ClC1=CC(Cl)=CC(CCC(=O)N2CC3(CC(C3)NC(=O)C3=CC4=NNN=C4C=C3)C2)=C1 QSDZSKSAPMAMLJ-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 210000000056 organ Anatomy 0.000 claims 1
- 239000000825 pharmaceutical preparation Substances 0.000 claims 1
- 229910052698 phosphorus Inorganic materials 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 239000000126 substance Substances 0.000 claims 1
- RMRRXYBBRGHZSY-UHFFFAOYSA-N thiophen-3-ylmethyl 2-(2h-benzotriazole-5-carbonyl)-2,7-diazaspiro[3.5]nonane-7-carboxylate Chemical compound C1CC2(CN(C2)C(=O)C2=CC3=NNN=C3C=C2)CCN1C(=O)OCC=1C=CSC=1 RMRRXYBBRGHZSY-UHFFFAOYSA-N 0.000 claims 1
- 238000011282 treatment Methods 0.000 claims 1
Classifications
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
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- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4192—1,2,3-Triazoles
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- A61K31/435—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
- A61K31/438—The ring being spiro-condensed with carbocyclic or heterocyclic ring systems
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- A61P37/00—Drugs for immunological or allergic disorders
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- C07D249/16—Heterocyclic compounds containing five-membered rings having three nitrogen atoms as the only ring hetero atoms condensed with carbocyclic rings or ring systems
- C07D249/18—Benzotriazoles
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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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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Claims (15)
1. Spoj, naznačen time, da ima sljedeću formulu (I)
[image]
gdje
R1 je alkil, halogenalkil, cikloalkil, supstituirani fenil, supstituirani fenilalkil, supstituirani fenoksialkil, supstituirani fenilcikloalkil, supstituirani fenilalkenil, supstituirani fenilalkinil, supstituirani piridinil, supstituirani piridinilalkil, supstituirani piridinilalkenil, supstituirani piridinilalkinil, supstituirani tiofenil, supstituirani tiofenilalkil, supstituirani tiofenilalkenil, supstituirani tiofenilalkinil, supstituirani 2,3-dihidro-1H-izoindol-2-il, supstituirani 1H-indol-2-il ili supstituirani benzofuran-2-il, pri čemu su supstituirani fenil, supstituirani fenilalkil, supstituirani fenoksialkil, supstituirani fenilcikioalkil, supstituirani fenilalkenil, supstituirani fenilalkinil, supstituirani piridinil, supstituirani piridinilalkil, supstituirani piridinilalkenil, supstituirani piridinilalkinil, supstituirani tiofenil, supstituirani tiofenilalkil, supstituirani tiofenilalkenil, supstituirani tiofenilalkinil, supstituirani 2,3-dihidro-1H-izoindol-2-il, supstituirani 1H-indol-2-il i supstituirani benzofuran-2-il, supstituirani s R8, R9 i R10;
R2 je -(CR4RB)n-R3, -C(O)-R3, -S(O)2-R3 ili -C(O)-NR6R3;
Y je -OC(O)-; -NR14C(O)-, -C(C)-, -S(O)2-,
[image]
dok u slučaju kada je R1 supstituirani fenilalkenil, supstituirani piridinilalkenil ili supstituirani tiofenilalkenil, tada Y nije -OC(O)-;
W je odabran od jednog od sljedećih sustava prstena: GB/22.07.2015.
[image]
[image]
pri čemu, u slučaju kada W predstavlja sustav prstena O, tada
R2je-C(O)-NR6R3;
R3 je odabran od sljedećih skupina:
[image]
[image]
R4 i R5 su neovisno odabrani od sljedećih: H, halogen, alkil i cikloalkil;
R6, R7 i R14su neovisno odabrani od sljedećih: H; alkil i cikloalkil;
R8, R9 i R10 su neovisno odabrani od sljedećih: H, alkil, hidroksialkil, halogenalkil, cikloalkil, cikloalkilalkil, cikloalkilalkoksi, cikloalkoksi, cikloalkoksialkil, cikloalkilalkoksialkil, alkoksi, alkoksialkil, halogenalkoksi, halogenalkoksialkil, alkoksialkoksi, alkoksialkoksialkil, halogen, hidroksi, cijano, alkilsulfonil, cikloalkilsulfonil, supstituirani aminosulfonil, supstituirani amino i supstituirani aminoalkil, dok su supstituirani aminosulfonil, supstituirani amino i supstituirani aminoalkil, supstituirani na atomu dušika s jednim do dva supstituenta neovisno odabrana od sljedećih: vodik, alkil, cikloalkil, cikloalkilalkil, hidroksialkil, alkoksialkil, alkilkarbonil i cikloalkilkarbonil; n je nula, 1, 2 ili 3;
ili farmaceutski prikladne soli.
2. Spoj prema zahtjevu 1, naznačen time, da R1 je supstituirani fenil, supstituirani fenilalkil, supstituirani fenoksialkil, supstituirani fenilcikloalkil, supstituirani fenilalkenil, supstituirani fenilalkinil, supstituirani piridinilalkil, supstituirani tiofenilalkil, supstituirani 2,3-dihidro-1H-izoindol-2-il, supstituirani 1H-indol-2-il ili supstituirani benzofuran-2-il, pri čemu su supstituirani fenil, supstituirani fenilalkil, supstituirani fenoksialkil, supstituirani fenilcikloalkil, supstituirani fenilalkenil, supstituirani piridinilalkil, supstituirani tiofenilalkil, supstituirani 2,3-dihidro-1H-izoindol-2-il, supstituirani 1H-indol-2-il i supstituirani benzofuran-2-il, supstituirani s R8, R9 i R10.
3. Spoj prema jednom od zahtjeva 1 do 2, naznačen time, da R2 je -C(O)-R3.
4. Spoj prema jednom od zahtjeva 1 do 3, naznačen time, da Y je -OC(O)- i R1 ne predstavlja supstituirani fenilalkenil, supstituirani piridinilalkenil ni supstituirani trofenilalkenil.
5. Spoj prema jednom od zahtjeva 1 do 4, naznačen time, da W je sustav prstena A.
6. Spoj prema jednom od zahtjeva 1 do 5, naznačen time, da je R3 odabran iz skupina S, U i AF.
7. Spoj, naznačen time, da je odabran od sljedećih:
3,5-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-S-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
4-klorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
1-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3,5-diklorfenil)propan-1-on;
1-(2-(4-amino-3-hidroksibenzoil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3,5-diklorfenil)propan-1-on;
3,5-diklorbenzil-2-(4-amino-3-hidroksibenzoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-benzilester;
N-(2-(4-fenilbutanoil)-2-azaspiro[3.3]heptan-6-il)-1H-benzo[d] [1,2,3]triazol-5-karboksamid;
3-klor-5-(metilsulfonil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2/7-diazaspiro[3.5]nonan-7-karboksilat;
[2-(1H-benzotriazol-5-karbonil)-2-azaspiro[3.3]hept-6-il]-karbaminska kiselina-benzilester;
N-(2-(3-(3,5-diklorfenil)propanoil)-2-azaspiro[3.3]heptan-6-il)-1H-benzo[d][1,2,3]-triazol-5-karboksamid;
[2-(1H-benzotriazol-5-karbonil)-2-azaspiro[3.3]hept-6-il]-karbaminska kiselina-3,5-diklor-benzilester;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3,5-diklor-benzilester;
3,5-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,6-diazaspiro[3.4]oktan-6-karboksilat;
3,5-diklorbenzil-7-(1H-benzo[d][1,2,3]triazol-S-karbonil)2,7-diazaspiro[3.5]nonan-2-karboksilat;
3,5-diklorbenzil-6-(4-amino-3-hidroksibenzamido)-2-azaspiro[3.3]heptan-2-karboksilat; 3-klor-5-(metilsulfonil)benzil-2-(4-sulfamoilbenzoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(3-sulfamoilbenzoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3,5-diklorbenzil-8-(1H-benzo[d][1,2,3]-triazol-S-karbonilL)-2,7-diazaspiro[4.5]dekan-2-karboksilat;
3-fluor-5-(trifluormetoksi)benzil-7-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[4.5]dekan-2-karboksilat;
(1H-benzotriazol-5-il)-{7-[2-(3-klor-fenil)-etansulfonil]-2,7-diazaspiro[3.5]non-2-il}-metanon;
3,5-diklorbenzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-karbonil)-2,6-diazaspiro[3.4]-oktan-6-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro [3.5]
nonan-7-karboksilat;
7-(2-okso-2,3-dihidro-benzoksazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-2-karboksilna kiselina-3,5-
diklor-benzilester;
3,5-diklorbenzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-ilsulfonil)-2/7-diazaspiro-[3.5] nonan-7-karboksilat;
2-okso-2,3-dihidro-benzoksazol-6-sulfonska kiselina-[2-(4-fenil-butiril)-2-azaspiro[3.3]-hept-6-il]-amid;
benzil-6-(2-okso-2,3-dihidrobenzo[d]oksazol-6-sulfonamido)-2-azaspiro[3.3]heptan-2-karboksilat;2-okso-2,3-dihidro-benzoksazol-6-sulfonska kiselina-{2-[3-(3,5-diklor-fenil)-propionil]-2-azaspiro[3.3]hept-6-il}-amid;
3,5-diklorbenzil-6-(2-okso-2,3-dihidrobenzo[d]oksazol-6-sulfonamido)-2-azaspiro-[3.3]heptan-2-karboksilat;
[2-(2-okso-2,3-dihidro-benzoksazol-6-sulfonil)-2-azaspiro[3,3]hept-6-il]-karbaminska kiselina-3,5-diklor-benzilester;
3-klor-5-(metilsulfonil)benzil-2-(2-okso-2,3-dihidrobenzo[d]tiazol-6-ilsulfonil)-2,7-diazaspiro[3.5]nonan-7-
karboksilat;
3;5-diklorbenzil-2-((2-okso-2,3-dihidrobenzo[d]oksazol-6-il)metil)-2,7-diazaspiro-[3.5]nonan-7-karboksilat;
3,5-diklorbenzil-2-(2-okso-2/3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro-[3.5]nonan-7-karboksilat;
6-(7-(3-(3,5-diklorfenil)propanoil)-2,7-diazaspiro[3.5]nonan-2-karbonil)benzo[d]-oksazol-2(3H)-on;
6-[(2-okso-2,3-dihidro-benzoksazol-6-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3,5-diklor-benzilester;
(E)-1-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3,5-diklorfenil)prop-2-en-l-on;
6-(7-(3-(3,5-diklorfenil)propanoil)-7-azaspiro[3.5]nonan-2-ilamino)benzo[d]oksazol-2(3H)-on;
l-(2-(1H-benzo[d][l/2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-2-(3,5-diklorfenoksi)etanon;
(2-(1H-benzo[d][l,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)(3,5-diklor-fenil)metanon;
6-{7-[(E)-3-(3,5-diklor-fenil)-akriloil]-2,7-diazaspiro[3.5]nonan-2-karbonil}-3H-benzoksazol-2-on;
(2-(1H-benzo[d][l,2i3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)(trans-2-(3,5-difluorfenil)ciklopropil)metanon;
(7-(1H-benzo[d][l,2/3]triazol-5-karbonil)-2,7-diazaspiro[4.4]nonan-2-il)(5-klor-1H-indol-2-il)metanon;
(7-(1H-benzo[d][l,2,3]triazol-5-karbonil)-2,7-diazaspiro[4.4]nonan-2-il)(5-klorbenzo-furan-2-il)metanon;
(E)-N-((1H-l,2/3-triazol-5-il)metil)-7-(3-(4-(trifluormetoksi)fenil)akriloil)-7-azaspiro[3.5]nonan-2-karboksamid;
(1H-benzo[d][1,2,3]triazol-5-il)(7-(5-(3,5-diklorfenil)-1,3,4-oksadiazol-2-il)-2,7-diazaspiro[3.5]nonan-2-il)metanon;
(1H-benzo[d][1,2,3]triazol-5-il)(7-(5-(4-klorfenil)-1,3,4-oksadiazol-2-il)-2,7-diazaspiro[3.5]nonan-2-il)metanon;
(1H-benzo[d][1,2,3]triazol-5-il)(7-(5-(4-klorfenil)-1,3,4-tiadiazol-2-il)-2,7-diazaspiro[3.5]nonan-2-il)metanon;
2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-N-(3,5-diklorbenzil)-2,7-diazaspiro-[3.5]nonan-7-karboksamid;
(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2/7-diazaspiro[3.5]nonan-7-il)(5-klorizoindolin-2-il)metanon;
benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-ilamino)-7-azaspiro[3.5]nonan-7-karboksilat;
3-klor-3-fluorbenzil-2-(1H-benzo[d][1,2,3]-triazol-5-karbonil)-2,7-diazaspiro-[3.5] nonan-7-karboksilat;
(2,6-diklorpiridin-4-il)metil-2-(1H-benzo(d)(1,2,3)triazol-5-karbonil)-2,7-diazaspiro [3.5] nonan-7-karboksilat;
3,4-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5] nonan-7-karboksilat;
(5,6-diklorpiridin-3-il)metil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5] nonan-7-karboksilat;
2,4-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
(6-klorpiridin-3-il)metil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
4-klor-3-(metilsulfonil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
l-(3,5-diklorfenil)etil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
(5-klorpiridin-3-il)metil-2-(1H-benzot[d][1,2,3]triazol-S-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
(5-brompiridin-3-il)metil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
(4,6-diklorpiridin-2-il)metil-2-il-(1H-benzot[d][1,2,3]triazol-S-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-4-fluorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro-[3.5]nonan-7-karboksilat;
(5-klortiofen-3-il)metil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
tiofen-3-ilmetil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3,5]nonan-7-karboksilat;
(5-bromtiofen-3-il)metil-2-(1H-benzo[d][l,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat; 4-(trifluormetil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat; 3,5-diklorbenzil-7-(1H-benzo[d][1,2,3]triazol-S-karbonil)-2,7-diazaspiro[4.4]nonan-2-karboksilat; 2,4,6-triklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2/7-diazaspiro[3.5]nonan-7-karboksilat;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-klor-5-trifluormetoksi-benzilester;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-trifluor-metil-benzilester;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-klor-5-cijano-benzilester;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-klor-4-fluor-benzilester;
4-(trifluormetil)benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-fluor-5-trifluormetil-benzilester;
6-[(1H-benzotriazol-5-karbonil)-amino]-2-azaspiro[3.3]heptan-2-karboksilna kiselina-3-klor-4-metil-benzilester;
3-(metilsulfonil)-5-(trifluormetil)benzil-2-(1H-benzo[d][l;2/3-triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-
karboksilat;
3-(metilsulfonil)-5-(trifluormetil)benzil-2-(2-okso-2/3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-2-(metilsulfonil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-klor-4-(metilsulfonil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3,5-diklorbenzil-6-(1H-benzo[d][1,2,3]triazol-5-ilkarbamoil)spiro[3.3]heptan-2-ilkarbamat;
2-fluor-5-(trifluormetoksi)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[4.5]dekan-7-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-ilsulfonil)- 2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-[(3H-[1,2,3]triazol-4-ilmetil)-karbamoil]-7-azaspiro[3.5]nonan-7-karboksilna kiselina-3,5-diklor-benzilester;
i njegove farmaceutski prikladne soli.
8. Spoj, naznačen time, da je odabran od sljedećih:
4-(trifluormetoksi)benzil-2-(4-sulfamoilbenzoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-fluor-4-(trifluormetoksi)benzil-2-(4-sulfamoilbenzoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
l-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(4-(trifluormetoksi)fenil)propan-1-on;
2-izopropil-4-(2-okso-2-(2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)
etoksi)benzonitril;
l-(2-(1H-benzo[d][l,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-2-(4-klor-2-izopropilfenoksi)etanon;
2-(4-klor-2-izopropilfenoksi)-l-(2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)etanon;
l-(2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]-nonan-7-il)-3-(4-(trifluormetoksi)
fenil)propan-l-on;
l-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3-klorfenil)prop-2-in-1-on;
l-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(4-klorfenil)prop-2-in-1-on;
3-fluor-4-(trifluormetoksi)benzil-7-(4,5,6/7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2;7-diazaspiro[3.5]nonan-2-karboksilat;
4-(trifluormetoksi)benzil-7-(4,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-2-
karboksilat;
[4-(trifluormetil)fenil]metil-2-(3a,4,5,6,7,7a-heksahidro-1H-benzotriazol-5-karbonil)-2,7-diazaspiro[3.5] nonan-7-karboksilat;
[2-fluor-4-(trifluormetil)fenil]metil-2-(4,5,6,7-tetrahidro-1H-benzotriazol-5-karbonii)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
[2-metil-4-(trifluormetoksi)fenil]metil-2-(4,5,6,7-tetrahidro-1H-benzotriazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-fluor-4-(2,2;2-trifluoretoksi)benzil-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
4-(2,2,2-trifluoretoksi)benzil-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-fluor-4-(2,2,2-trifluoretoksi)benzil-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-6-karbonil)-2,7-diazaspiro(3.5)nonan-2-karboksilat;
2-fluor-4-(trifluormetoksi)benzil-7-(4,5,6,7-tetrahidro-1H-benzo[d] [1,2,3]triazol-5-karbonil)-2,7-diazaspiro
[3.5]nonan-2-karboksilat;
2-fluor-4-(trifluormetoksi)benzil-2-(4,5;6/7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
4-(trifluormetoksi)benzii-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-klor-5-(trifluormetil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-(metilsulfonil)-5-(trifluormetil)benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazoi-6-ilsulfonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
4-(trifluormetoksi)benzil-2-(4,5,6,7-tetrahidro-1H-[1,2,3]triazol[4,5-c]piridin-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-fluor-4-(trifluormetoksi)benzil-2-(4,5/6,7-tetrahidro-1H-[l;2,3]triazol[4,5-c]-piridin-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
[4-(trifluormetoksilfenil)metil-2-((1H-triazol-4-ilmetil)karbamoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
[2-fluor-4-(trifluormetoksi)fenil]metil-2-((1H-triazol-4-ilmetil)karbamoil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
(-)-2-fluor-4-(trifluormetoksi)benzil-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]
nonan-7-karboksilat;
(+)-2-fluor-4-(trifluormetoksi)benzil-2-(4;5/6,7-tetrahidro-1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
[2-fluor-4-(trifluormetil)fenil]metil-2-[4,5,6,7-tetrahidro-1H-benzotriazol-5-karbonil]-2,7-diazaspiro[3.5]nonan-7-
karboksilat (enantiomer A);
[2-fluor-4-(trifluormetil)fenil]metil-2-[4,5,6,7-tetrahidro-1H-benzotriazol-5-karbonil]-2,7-diazaspiro[3.5]nonan-7-
karboksilat (enantiomer B);
i njegove farmaceutski prikladne soli.
9. Spoj prema jednom od zahtjeva 1 do 8, naznačen time, da je odabran od sljedećih:
3,5-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
2-klor-5-(metilsulfonil)benzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(2-okso-2;3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3,5-diklorbenzil-2-(2-okso-2;3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro-[3.5]nonan-7-karboksilat;
(E)-1-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3,5-diklorfenil)prop-2-en-l-on;
3-(metilsulfonil)-5-(trifluormetil)benzil-2-(1H-benzo[d][1,2,3-triazol-5-karboni!)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
[2-metil-4-(trifluormetoksi)fenil]metil-2-(4,5,6,7-tetrahidro-1H-benzotriazol-5-karbonil)-2,7-diazaspiro [3.5]
nonan-7-karboksilat;
(+)-2-fluor-4-(trifluormetoksi)benzil-2-(4,5,6,7-tetrahidro-1H-benzo[d][1,2,3]
triazol-5-karbonil)-2,7-diazaspiro[3.5] nonan-7-karboksilat; i njegove farmaceutski prikladne soli.
10. Spoj prema jednom od zahtjeva 1 do 6 i 8, naznačen time, da je odabran od sljedećih:
3,5-diklorbenzil-2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(1H-benzo(d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-karboksilat;
3-klor-5-(metilsulfonil)benzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro[3.5]nonan-7-
karboksilat;
3,5-diklorbenzil-2-(2-okso-2,3-dihidrobenzo[d]oksazol-6-karbonil)-2,7-diazaspiro-[3.5] nonan-7-karboksilat;
(E)-1-(2-(1H-benzo[d][1,2,3]triazol-5-karbonil)-2,7-diazaspiro[3.5]nonan-7-il)-3-(3,5-diklorfenil)prop-2-en-1-on;
3-(metilsulfonil)-5-(trifluormetil)benzil-2-(1H-benzo[d][1,2,3]-triazol-5-karbonil)-2,7-diazaspiro[3.5] nonan-7-karboksilat;
i njegove farmaceutski prikladne soli.
11. Postupak za proizvodnju spoja prema jednom od zahtjeva 1 do 10, naznačen time, da obuhvaća sljedeće:
a) reakcija spoja formule (II) u prisutnosti spoja formule (III);
[image]
ili b) reakcija spoja formule (IV) u prisutnosti spoja formule (V);
[image]
pri čemu u koraku a), R1, R2 i W su definirani kao u zahtjevu 1, Y predstavlja -C(O)- i pri čemu u koraku b), R1 i Y su definirani kao u zahtjevu, W predstavlja A, B, C, D, E, F, G, H, I, J, K, L, M, N, P ili Q, a R2 predstavlja -C(O)-R3.
12. Spoj prema jednom od zahtjeva 1 do 10, naznačen time, da se upotrebljava kao terapeutski djelotvorna tvar.
13. Farmaceutski pripravak, naznačen time, da obuhvaća spoj prema bilo kojem od zahtjeva 1 do 10, i terapeutski inertan nosač.
14. Spoj prema jednom od zahtjeva 1 do 10, naznačen time, da se upotrebljava za liječenje ili profilaksu stanja kod poremećaja bubrega, poremećaja jetre, upalnih poremećaja, poremećaja nervnog sustava, fibroznih bolesti i akutnih i kroničnih odbacivanja transplatiranih organa.
15. Spoj prema jednom od zahtjeva 1 do 10, naznačen time, da se proizvodi putem postupka prema zahtjevu 11.
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