JP2013522372A5 - - Google Patents
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- Publication number
- JP2013522372A5 JP2013522372A5 JP2013501427A JP2013501427A JP2013522372A5 JP 2013522372 A5 JP2013522372 A5 JP 2013522372A5 JP 2013501427 A JP2013501427 A JP 2013501427A JP 2013501427 A JP2013501427 A JP 2013501427A JP 2013522372 A5 JP2013522372 A5 JP 2013522372A5
- Authority
- JP
- Japan
- Prior art keywords
- phenylethyl
- quinolinecarboxamide
- phenyl
- trifluoromethyl
- methyl
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 125000000217 alkyl group Chemical group 0.000 claims 33
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 125000002757 morpholinyl group Chemical group 0.000 claims 10
- 125000003386 piperidinyl group Chemical group 0.000 claims 10
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 10
- 150000001875 compounds Chemical class 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 239000011780 sodium chloride Substances 0.000 claims 8
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 7
- 239000008194 pharmaceutical composition Substances 0.000 claims 6
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 5
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 4
- 125000003342 alkenyl group Chemical group 0.000 claims 4
- 125000004093 cyano group Chemical group *C#N 0.000 claims 4
- 125000004634 hexahydroazepinyl group Chemical group N1(CCCCCC1)* 0.000 claims 4
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims 4
- 125000004193 piperazinyl group Chemical group 0.000 claims 4
- 229920000728 polyester Polymers 0.000 claims 4
- 125000003226 pyrazolyl group Chemical group 0.000 claims 4
- 125000004076 pyridyl group Chemical group 0.000 claims 4
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 4
- 125000000168 pyrrolyl group Chemical group 0.000 claims 4
- JDSAUQCGOKOYLM-DIPNUNPCSA-N 7-methoxy-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(=O)(=O)C(C)C)C(OC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 JDSAUQCGOKOYLM-DIPNUNPCSA-N 0.000 claims 3
- -1 1,4'-bipiperidin-1'-ylmethyl Chemical group 0.000 claims 2
- UKKAMGFMCVUMBQ-PSXMRANNSA-N 6-ethylsulfonyl-7-methoxy-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 UKKAMGFMCVUMBQ-PSXMRANNSA-N 0.000 claims 2
- LPKAEPRFTBYWAY-PSXMRANNSA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(C)(=O)=O)C(OC(C)C)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 LPKAEPRFTBYWAY-PSXMRANNSA-N 0.000 claims 2
- RONPGSRKGWGJMB-UUWRZZSWSA-N 6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 RONPGSRKGWGJMB-UUWRZZSWSA-N 0.000 claims 2
- FXNLNBXALPILQY-DIPNUNPCSA-N 7-ethoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(=O)(=O)C(C)C)C(OCC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 FXNLNBXALPILQY-DIPNUNPCSA-N 0.000 claims 2
- JWGHAKJOBMSMPM-PSXMRANNSA-N 7-ethoxy-6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 JWGHAKJOBMSMPM-PSXMRANNSA-N 0.000 claims 2
- HUCMAHIXUVKFHR-PSXMRANNSA-N 7-methoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(=O)(=O)C(C)C)C(OC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 HUCMAHIXUVKFHR-PSXMRANNSA-N 0.000 claims 2
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- GRVDJDISBSALJP-UHFFFAOYSA-N methyloxidanyl Chemical group [O]C GRVDJDISBSALJP-UHFFFAOYSA-N 0.000 claims 2
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 claims 2
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 2
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims 2
- ACMVPNMKEVODGF-MGBGTMOVSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(Cl)C(Cl)=C1 ACMVPNMKEVODGF-MGBGTMOVSA-N 0.000 claims 1
- CIRAVJSZYKFMCO-QHCPKHFHSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Cl)C(Cl)=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 CIRAVJSZYKFMCO-QHCPKHFHSA-N 0.000 claims 1
- LLKABDABGCYFDL-UUWRZZSWSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(Cl)C(Cl)=C1 LLKABDABGCYFDL-UUWRZZSWSA-N 0.000 claims 1
- SIMCDPCDBFVCCG-MGBGTMOVSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(Cl)C(Cl)=C1 SIMCDPCDBFVCCG-MGBGTMOVSA-N 0.000 claims 1
- ODUVOACVJMDMRC-DEOSSOPVSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Cl)C(Cl)=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 ODUVOACVJMDMRC-DEOSSOPVSA-N 0.000 claims 1
- ROVHOXPUQQFWDI-QHCPKHFHSA-N 2-(3,4-dichlorophenyl)-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Cl)C(Cl)=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCC1 ROVHOXPUQQFWDI-QHCPKHFHSA-N 0.000 claims 1
- GTZGUMBBQLIKLZ-MGBGTMOVSA-N 2-(3-bromophenyl)-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(Br)=C1 GTZGUMBBQLIKLZ-MGBGTMOVSA-N 0.000 claims 1
- IOCLYZCURRURNC-DEOSSOPVSA-N 2-(3-bromophenyl)-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Br)C=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 IOCLYZCURRURNC-DEOSSOPVSA-N 0.000 claims 1
- CZYFRDMRUNFOJR-UUWRZZSWSA-N 2-(3-bromophenyl)-6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(Br)=C1 CZYFRDMRUNFOJR-UUWRZZSWSA-N 0.000 claims 1
- JQQWCCZWUFFCIA-MGBGTMOVSA-N 2-(3-bromophenyl)-6-methylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(Br)=C1 JQQWCCZWUFFCIA-MGBGTMOVSA-N 0.000 claims 1
- XFACHZOJZDSAFR-VWLOTQADSA-N 2-(3-bromophenyl)-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Br)C=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 XFACHZOJZDSAFR-VWLOTQADSA-N 0.000 claims 1
- CKCLHVGDFXFKKH-DEOSSOPVSA-N 2-(3-bromophenyl)-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(Br)C=CC=2)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCC1 CKCLHVGDFXFKKH-DEOSSOPVSA-N 0.000 claims 1
- HYCVLFCJLLHRLS-PGUFJCEWSA-N 2-(4-methoxyphenyl)-6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1=CC(OC)=CC=C1C1=NC2=CC=C(S(C)(=O)=O)C=C2C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C1CN1CCC(N2CCCCC2)CC1 HYCVLFCJLLHRLS-PGUFJCEWSA-N 0.000 claims 1
- PKJYVSDXVOOCEH-YFGIIPPGSA-N 3-[(3-methyl-4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)C(C)CN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 PKJYVSDXVOOCEH-YFGIIPPGSA-N 0.000 claims 1
- JCANIFRETPTWQD-XRTCKYLNSA-N 3-[(3-methyl-4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)C(C)CN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 JCANIFRETPTWQD-XRTCKYLNSA-N 0.000 claims 1
- BTQQXHWRFYAIPV-YFGIIPPGSA-N 3-[(3-methyl-4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)C(C)CN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 BTQQXHWRFYAIPV-YFGIIPPGSA-N 0.000 claims 1
- BPLTWYVXZNQCOP-PGUFJCEWSA-N 3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 BPLTWYVXZNQCOP-PGUFJCEWSA-N 0.000 claims 1
- BPLTWYVXZNQCOP-DHUJRADRSA-N 3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1S)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 BPLTWYVXZNQCOP-DHUJRADRSA-N 0.000 claims 1
- GWPLUWQSXVREOG-SANMLTNESA-N 3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@@H](C)C=2C=CC=CC=2)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 GWPLUWQSXVREOG-SANMLTNESA-N 0.000 claims 1
- PGENGVKSTFMSLY-PSXMRANNSA-N 3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 PGENGVKSTFMSLY-PSXMRANNSA-N 0.000 claims 1
- HJZSYCFCTBERBX-JGCGQSQUSA-N 3-[[4-(3,3-difluoropyrrolidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CC(F)(F)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 HJZSYCFCTBERBX-JGCGQSQUSA-N 0.000 claims 1
- QGQIMYJBQMPYLW-QHCPKHFHSA-N 3-[[4-(3,3-difluoropyrrolidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCC(F)(F)C1 QGQIMYJBQMPYLW-QHCPKHFHSA-N 0.000 claims 1
- RCMIQJNMOVOBPI-OMFPCOHASA-N 3-[[4-(3-fluoropiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CC(F)CCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 RCMIQJNMOVOBPI-OMFPCOHASA-N 0.000 claims 1
- VEEHGFXCSVCRIJ-LJDFVPJLSA-N 3-[[4-(3-methoxypiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1C(OC)CCCN1C1CCN(CC=2C(=C3C=C(C=CC3=NC=2C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)CC1 VEEHGFXCSVCRIJ-LJDFVPJLSA-N 0.000 claims 1
- SNOPNYYTBVYEIF-MGBGTMOVSA-N 3-[[4-(4,4-difluoropiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCC(F)(F)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 SNOPNYYTBVYEIF-MGBGTMOVSA-N 0.000 claims 1
- YYZRBBWSDWZZNP-DEOSSOPVSA-N 3-[[4-(4,4-difluoropiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCC(F)(F)CC1 YYZRBBWSDWZZNP-DEOSSOPVSA-N 0.000 claims 1
- UZZOIVXKAYHICS-UUWRZZSWSA-N 3-[[4-(4-fluoropiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCC(F)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 UZZOIVXKAYHICS-UUWRZZSWSA-N 0.000 claims 1
- JAKIYIXVTAFWIU-PGUFJCEWSA-N 3-[[4-(4-methoxypiperidin-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(OC)CCN1C1CCN(CC=2C(=C3C=C(C=CC3=NC=2C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)CC1 JAKIYIXVTAFWIU-PGUFJCEWSA-N 0.000 claims 1
- UPRWOUAKSNRBCT-PGUFJCEWSA-N 3-[[4-(azepan-1-yl)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 UPRWOUAKSNRBCT-PGUFJCEWSA-N 0.000 claims 1
- XTVIRJFIAJHEED-MGBGTMOVSA-N 3-[[4-(diethylamino)piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(CC)CC)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 XTVIRJFIAJHEED-MGBGTMOVSA-N 0.000 claims 1
- CSKDQPUTKSXKCT-QRRWFCJLSA-N 3-[[4-[(2R)-2-(hydroxymethyl)pyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2[C@H](CCC2)CO)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 CSKDQPUTKSXKCT-QRRWFCJLSA-N 0.000 claims 1
- KQLKMQOLIJLIDC-GRMGDBHTSA-N 3-[[4-[(2R)-2-methylpyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C[C@@H]1CCCN1C1CCN(CC=2C(=C3C=C(C=CC3=NC=2C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)CC1 KQLKMQOLIJLIDC-GRMGDBHTSA-N 0.000 claims 1
- CSKDQPUTKSXKCT-NDOVKIIASA-N 3-[[4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2[C@@H](CCC2)CO)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 CSKDQPUTKSXKCT-NDOVKIIASA-N 0.000 claims 1
- AKCRNXOABYLACD-JADSYQMUSA-N 3-[[4-[(2S)-2-(methoxymethyl)pyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound COC[C@@H]1CCCN1C1CCN(CC=2C(=C3C=C(C=CC3=NC=2C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)CC1 AKCRNXOABYLACD-JADSYQMUSA-N 0.000 claims 1
- KQLKMQOLIJLIDC-OHWKKVTOSA-N 3-[[4-[(2S)-2-methylpyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C[C@H]1CCCN1C1CCN(CC=2C(=C3C=C(C=CC3=NC=2C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)CC1 KQLKMQOLIJLIDC-OHWKKVTOSA-N 0.000 claims 1
- LQCOQFKKZATBDB-QRRWFCJLSA-N 3-[[4-[(3R)-3-hydroxypiperidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C[C@H](O)CCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 LQCOQFKKZATBDB-QRRWFCJLSA-N 0.000 claims 1
- JITXRFKHHLQNQE-PWUYWRBVSA-N 3-[[4-[(3R)-3-hydroxypiperidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCC[C@@H](O)C1 JITXRFKHHLQNQE-PWUYWRBVSA-N 0.000 claims 1
- SOYBQBMEXDLLLH-UTONBFNKSA-N 3-[[4-[(3R)-3-hydroxypyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C[C@H](O)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 SOYBQBMEXDLLLH-UTONBFNKSA-N 0.000 claims 1
- SCGBUUZJQJDVFO-OGVWKLGRSA-N 3-[[4-[(3S)-3-fluoropyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C[C@@H](F)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 SCGBUUZJQJDVFO-OGVWKLGRSA-N 0.000 claims 1
- INBUFGUMBYFIIW-HOFKKMOUSA-N 3-[[4-[(3S)-3-fluoropyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CC[C@H](F)C1 INBUFGUMBYFIIW-HOFKKMOUSA-N 0.000 claims 1
- LQCOQFKKZATBDB-NDOVKIIASA-N 3-[[4-[(3S)-3-hydroxypiperidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C[C@@H](O)CCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 LQCOQFKKZATBDB-NDOVKIIASA-N 0.000 claims 1
- JITXRFKHHLQNQE-OUTSHDOLSA-N 3-[[4-[(3S)-3-hydroxypiperidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCC[C@H](O)C1 JITXRFKHHLQNQE-OUTSHDOLSA-N 0.000 claims 1
- SOYBQBMEXDLLLH-OOOSNSGVSA-N 3-[[4-[(3S)-3-hydroxypyrrolidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C[C@@H](O)CC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 SOYBQBMEXDLLLH-OOOSNSGVSA-N 0.000 claims 1
- XICJDOPQDVXPCM-JGCGQSQUSA-N 3-[[4-[2-hydroxyethyl(methyl)amino]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(CCO)C)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 XICJDOPQDVXPCM-JGCGQSQUSA-N 0.000 claims 1
- QIZBPEXEFDMOOH-MGBGTMOVSA-N 3-[[4-[2-methoxyethyl(methyl)amino]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(C)CCOC)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 QIZBPEXEFDMOOH-MGBGTMOVSA-N 0.000 claims 1
- JXDPLNOXJMKGGH-HPHDRJMSSA-N 3-[[4-[3-(hydroxymethyl)piperidin-1-yl]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CC(CO)CCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 JXDPLNOXJMKGGH-HPHDRJMSSA-N 0.000 claims 1
- IMKLXTMETPLSDF-UUWRZZSWSA-N 3-[[4-[ethyl(propyl)amino]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(CC)CCC)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 IMKLXTMETPLSDF-UUWRZZSWSA-N 0.000 claims 1
- LMQUCHAOIRHKGJ-UUWRZZSWSA-N 3-[[4-[methyl(2-methylpropyl)amino]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(C)CC(C)C)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 LMQUCHAOIRHKGJ-UUWRZZSWSA-N 0.000 claims 1
- GFCFPEYLWCRPDR-MGBGTMOVSA-N 3-[[4-[methyl(propyl)amino]piperidin-1-yl]methyl]-6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N(C)CCC)CCN1CC1=C(C=2C=C(C=CC=2)C(F)(F)F)N=C(C=CC(=C2)S(C)(=O)=O)C2=C1C(=O)N[C@@H](C(F)(F)F)C1=CC=CC=C1 GFCFPEYLWCRPDR-MGBGTMOVSA-N 0.000 claims 1
- DOGWIPWWGMJXOU-UUWRZZSWSA-N 6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)CC)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 DOGWIPWWGMJXOU-UUWRZZSWSA-N 0.000 claims 1
- IFPIUYVHOAODEF-DIPNUNPCSA-N 6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 IFPIUYVHOAODEF-DIPNUNPCSA-N 0.000 claims 1
- RZTHYHQEMJDWRQ-VWLOTQADSA-N 6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@@H](C)C=2C=CC=CC=2)C2=CC(S(=O)(=O)CC)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 RZTHYHQEMJDWRQ-VWLOTQADSA-N 0.000 claims 1
- KRIJVMRDQPDCJA-MHZLTWQESA-N 6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)=CC=CC=C1 KRIJVMRDQPDCJA-MHZLTWQESA-N 0.000 claims 1
- INQFTJQNRXJCQO-PGUFJCEWSA-N 6-ethylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)CC)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 INQFTJQNRXJCQO-PGUFJCEWSA-N 0.000 claims 1
- JYNFVKSXEHAIBA-KXQOOQHDSA-N 6-ethylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 JYNFVKSXEHAIBA-KXQOOQHDSA-N 0.000 claims 1
- DSQXTAUJXNOKLD-PSXMRANNSA-N 6-ethylsulfonyl-3-[[4-(4-fluoropiperidin-1-yl)piperidin-1-yl]methyl]-7-methoxy-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCC(F)CC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 DSQXTAUJXNOKLD-PSXMRANNSA-N 0.000 claims 1
- WXPAECDEYMWCEN-VWLOTQADSA-N 6-ethylsulfonyl-3-[[4-(4-fluoropiperidin-1-yl)piperidin-1-yl]methyl]-7-methoxy-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCC(F)CC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)=CC=CC=C1 WXPAECDEYMWCEN-VWLOTQADSA-N 0.000 claims 1
- NZHYZQVZZCPHKQ-PGUFJCEWSA-N 6-ethylsulfonyl-7-methoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 NZHYZQVZZCPHKQ-PGUFJCEWSA-N 0.000 claims 1
- UKCHRCLRRIKCFS-VWLOTQADSA-N 6-ethylsulfonyl-7-methoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)=CC=CC=C1 UKCHRCLRRIKCFS-VWLOTQADSA-N 0.000 claims 1
- UEKSFUYSGJFQNZ-PGUFJCEWSA-N 6-ethylsulfonyl-7-methoxy-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 UEKSFUYSGJFQNZ-PGUFJCEWSA-N 0.000 claims 1
- TYASUZAFXLTWOR-SANMLTNESA-N 6-ethylsulfonyl-7-methoxy-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)=CC=CC=C1 TYASUZAFXLTWOR-SANMLTNESA-N 0.000 claims 1
- SMVYCVYOHKDTQP-VWLOTQADSA-N 6-ethylsulfonyl-7-methoxy-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC)S(=O)(=O)CC)=CC=CC=C1 SMVYCVYOHKDTQP-VWLOTQADSA-N 0.000 claims 1
- VODPNKIQICKRHZ-DIPNUNPCSA-N 6-ethylsulfonyl-7-propan-2-yloxy-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 VODPNKIQICKRHZ-DIPNUNPCSA-N 0.000 claims 1
- NAQFRUOBRUPQLI-SANMLTNESA-N 6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@@H](C)C=2C=CC=CC=2)C2=CC(S(=O)(=O)CC)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 NAQFRUOBRUPQLI-SANMLTNESA-N 0.000 claims 1
- IWMFDOKTDYTLGT-NDEPHWFRSA-N 6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)=CC=CC=C1 IWMFDOKTDYTLGT-NDEPHWFRSA-N 0.000 claims 1
- ONBREWUWVIRTHC-MHZLTWQESA-N 6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-7-propan-2-yloxy-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCC2)C=2C=C(C=CC=2)C(F)(F)F)OC(C)C)S(=O)(=O)CC)=CC=CC=C1 ONBREWUWVIRTHC-MHZLTWQESA-N 0.000 claims 1
- KOURCSKVXHWNSO-FULUQAKVSA-N 6-methylsulfonyl-2-[3-(trifluoromethyl)phenyl]-3-[[4-[2-(trifluoromethyl)pyrrolidin-1-yl]piperidin-1-yl]methyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2C(CCC2)C(F)(F)F)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 KOURCSKVXHWNSO-FULUQAKVSA-N 0.000 claims 1
- KMSYGALRFSIWMP-MGBGTMOVSA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 KMSYGALRFSIWMP-MGBGTMOVSA-N 0.000 claims 1
- JWHZLSHNJCGBMO-MGBGTMOVSA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[4-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCOCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(C(F)(F)F)C=C1 JWHZLSHNJCGBMO-MGBGTMOVSA-N 0.000 claims 1
- FXDCHTIDLTXSBD-DEOSSOPVSA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 FXDCHTIDLTXSBD-DEOSSOPVSA-N 0.000 claims 1
- QJUIRTRNDSGLLY-DEOSSOPVSA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[4-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=CC(=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 QJUIRTRNDSGLLY-DEOSSOPVSA-N 0.000 claims 1
- JADUJCUNFZHBCM-SANMLTNESA-N 6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C1=C2C=C(S(C)(=O)=O)C(OC(C)C)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 JADUJCUNFZHBCM-SANMLTNESA-N 0.000 claims 1
- RONPGSRKGWGJMB-UMSFTDKQSA-N 6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1S)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 RONPGSRKGWGJMB-UMSFTDKQSA-N 0.000 claims 1
- GTJBSASGPPRFBU-UUWRZZSWSA-N 6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[4-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(C(F)(F)F)C=C1 GTJBSASGPPRFBU-UUWRZZSWSA-N 0.000 claims 1
- SUCRBIFAPHLNDB-DIPNUNPCSA-N 6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(C)(=O)=O)C(OC(C)C)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 SUCRBIFAPHLNDB-DIPNUNPCSA-N 0.000 claims 1
- DJZJIBLBASHUSH-MGBGTMOVSA-N 6-methylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 DJZJIBLBASHUSH-MGBGTMOVSA-N 0.000 claims 1
- SKYDLOJNXDOWSM-MGBGTMOVSA-N 6-methylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[4-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C)=CC=C2N=C1C1=CC=C(C(F)(F)F)C=C1 SKYDLOJNXDOWSM-MGBGTMOVSA-N 0.000 claims 1
- XKVQUETXCPJDMK-SZGIACGNSA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]-3-[[4-[2-(trifluoromethyl)pyrrolidin-1-yl]piperidin-1-yl]methyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCC1C(F)(F)F XKVQUETXCPJDMK-SZGIACGNSA-N 0.000 claims 1
- MUWWPCDMOOLPFY-VWLOTQADSA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 MUWWPCDMOOLPFY-VWLOTQADSA-N 0.000 claims 1
- KYUCQULKUUFFOB-VWLOTQADSA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[4-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=CC(=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 KYUCQULKUUFFOB-VWLOTQADSA-N 0.000 claims 1
- DUAQAOPWYWNRFC-MHZLTWQESA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-7-propan-2-yloxy-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(C)(=O)=O)C(OC(C)C)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 DUAQAOPWYWNRFC-MHZLTWQESA-N 0.000 claims 1
- WGMSOQMWWCBALQ-DEOSSOPVSA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCC1 WGMSOQMWWCBALQ-DEOSSOPVSA-N 0.000 claims 1
- ULLJPUAYBCZWAI-DEOSSOPVSA-N 6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[4-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=CC=C1N=C1C=2C=CC(=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCC1 ULLJPUAYBCZWAI-DEOSSOPVSA-N 0.000 claims 1
- LCEZBGFOIRTJFG-PGUFJCEWSA-N 6-propan-2-ylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 LCEZBGFOIRTJFG-PGUFJCEWSA-N 0.000 claims 1
- PKASPNMMDJWTSQ-PGUFJCEWSA-N 7-chloro-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C(C)C)C(F)(F)F)=CC=CC=C1 PKASPNMMDJWTSQ-PGUFJCEWSA-N 0.000 claims 1
- UUOVCZSZBSCOQD-VWLOTQADSA-N 7-chloro-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C(C)C)=CC=CC=C1 UUOVCZSZBSCOQD-VWLOTQADSA-N 0.000 claims 1
- WMURCDCSMQNJQC-PSXMRANNSA-N 7-chloro-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C(C)C)C(F)(F)F)=CC=CC=C1 WMURCDCSMQNJQC-PSXMRANNSA-N 0.000 claims 1
- VYCYXJRKGWEUDQ-UUWRZZSWSA-N 7-chloro-6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 VYCYXJRKGWEUDQ-UUWRZZSWSA-N 0.000 claims 1
- PKILHDROTPXSRU-DEOSSOPVSA-N 7-chloro-6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)CC)=CC=CC=C1 PKILHDROTPXSRU-DEOSSOPVSA-N 0.000 claims 1
- LVEHCRDORAXWQQ-PGUFJCEWSA-N 7-chloro-6-ethylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 LVEHCRDORAXWQQ-PGUFJCEWSA-N 0.000 claims 1
- FFVXDKQWLCMRCU-VWLOTQADSA-N 7-chloro-6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)CC)=CC=CC=C1 FFVXDKQWLCMRCU-VWLOTQADSA-N 0.000 claims 1
- ZFQOZBGVRWYDED-MGBGTMOVSA-N 7-chloro-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C)C(F)(F)F)=CC=CC=C1 ZFQOZBGVRWYDED-MGBGTMOVSA-N 0.000 claims 1
- ZEEDRKVOOHXXLR-QHCPKHFHSA-N 7-chloro-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=C(Cl)C=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 ZEEDRKVOOHXXLR-QHCPKHFHSA-N 0.000 claims 1
- NITYQOZWOXIPOY-UUWRZZSWSA-N 7-chloro-6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C)C(F)(F)F)=CC=CC=C1 NITYQOZWOXIPOY-UUWRZZSWSA-N 0.000 claims 1
- MTSSBGBLVHOJTG-DEOSSOPVSA-N 7-chloro-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC(=C(Cl)C=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 MTSSBGBLVHOJTG-DEOSSOPVSA-N 0.000 claims 1
- VISBUXIVAPOQQY-SANMLTNESA-N 7-chloro-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C2=C3C=C(C(=CC3=NC(=C2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)Cl)S(=O)(=O)C(C)C)=CC=CC=C1 VISBUXIVAPOQQY-SANMLTNESA-N 0.000 claims 1
- BZBJMVGRNUGNEW-KXQOOQHDSA-N 7-ethoxy-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(=O)(=O)C(C)C)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 BZBJMVGRNUGNEW-KXQOOQHDSA-N 0.000 claims 1
- BSPXKLOUIIWPSL-SANMLTNESA-N 7-ethoxy-6-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C1=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 BSPXKLOUIIWPSL-SANMLTNESA-N 0.000 claims 1
- BYESLAOYMUQRPD-DIPNUNPCSA-N 7-ethoxy-6-ethylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 BYESLAOYMUQRPD-DIPNUNPCSA-N 0.000 claims 1
- VIQDFCPKKIVUIC-PSXMRANNSA-N 7-ethoxy-6-ethylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 VIQDFCPKKIVUIC-PSXMRANNSA-N 0.000 claims 1
- FTXJHNPKSQXULW-MHZLTWQESA-N 7-ethoxy-6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 FTXJHNPKSQXULW-MHZLTWQESA-N 0.000 claims 1
- OZQBNXWZMPCUOT-SANMLTNESA-N 7-ethoxy-6-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(=O)(=O)CC)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 OZQBNXWZMPCUOT-SANMLTNESA-N 0.000 claims 1
- HRLRUJFSHKMGPP-PGUFJCEWSA-N 7-ethoxy-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(C)(=O)=O)C(OCC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 HRLRUJFSHKMGPP-PGUFJCEWSA-N 0.000 claims 1
- XGTGLMLLEUDRFF-VWLOTQADSA-N 7-ethoxy-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C1=C2C=C(S(C)(=O)=O)C(OCC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 XGTGLMLLEUDRFF-VWLOTQADSA-N 0.000 claims 1
- GXOSMZTUFJMSHV-PSXMRANNSA-N 7-ethoxy-6-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(C)(=O)=O)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 GXOSMZTUFJMSHV-PSXMRANNSA-N 0.000 claims 1
- XLSWKDBDMWDVRJ-SANMLTNESA-N 7-ethoxy-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(C)(=O)=O)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 XLSWKDBDMWDVRJ-SANMLTNESA-N 0.000 claims 1
- FLIKERIGGIMLQL-DIPNUNPCSA-N 7-ethoxy-6-propan-2-ylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC=1C(C(=O)N[C@H](C=2C=CC=CC=2)C(F)(F)F)=C2C=C(S(=O)(=O)C(C)C)C(OCC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 FLIKERIGGIMLQL-DIPNUNPCSA-N 0.000 claims 1
- SLMSEXSKSYMYLJ-UUWRZZSWSA-N 7-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 SLMSEXSKSYMYLJ-UUWRZZSWSA-N 0.000 claims 1
- BNFUCGWTHXAPQJ-VWLOTQADSA-N 7-ethylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)CC)=CC=CC=C1 BNFUCGWTHXAPQJ-VWLOTQADSA-N 0.000 claims 1
- FJWBBMMTBLBAKR-PGUFJCEWSA-N 7-ethylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)CC)C(F)(F)F)=CC=CC=C1 FJWBBMMTBLBAKR-PGUFJCEWSA-N 0.000 claims 1
- QAGYIJGFPJCCTF-UHFFFAOYSA-N 7-ethylsulfonyl-N-(2-phenylpropan-2-yl)-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C=2C=C(C=CC=2)C(F)(F)F)=NC2=CC(S(=O)(=O)CC)=CC=C2C=1C(=O)NC(C)(C)C1=CC=CC=C1 QAGYIJGFPJCCTF-UHFFFAOYSA-N 0.000 claims 1
- JRQAXSNHEWOHLW-SANMLTNESA-N 7-ethylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1([C@H](C)NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)CC)=CC=CC=C1 JRQAXSNHEWOHLW-SANMLTNESA-N 0.000 claims 1
- HUCMAHIXUVKFHR-BHVANESWSA-N 7-methoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]-N-[(1S)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(=O)(=O)C(C)C)C(OC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 HUCMAHIXUVKFHR-BHVANESWSA-N 0.000 claims 1
- JJOJMXSVIFIODM-SANMLTNESA-N 7-methoxy-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C1=C2C=C(S(=O)(=O)C(C)C)C(OC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 JJOJMXSVIFIODM-SANMLTNESA-N 0.000 claims 1
- NWLFYDXCSNOMOD-UUWRZZSWSA-N 7-methoxy-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound N([C@H](C=1C=CC=CC=1)C(F)(F)F)C(=O)C1=C2C=C(S(C)(=O)=O)C(OC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 NWLFYDXCSNOMOD-UUWRZZSWSA-N 0.000 claims 1
- XDBJGNAIAGBRAR-DEOSSOPVSA-N 7-methoxy-6-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C1=C2C=C(S(C)(=O)=O)C(OC)=CC2=NC(C=2C=C(C=CC=2)C(F)(F)F)=C1CN(CC1)CCC1N1CCOCC1 XDBJGNAIAGBRAR-DEOSSOPVSA-N 0.000 claims 1
- WICMDADAEMAUCO-VWLOTQADSA-N 7-methoxy-6-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(C)(=O)=O)C(OC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 WICMDADAEMAUCO-VWLOTQADSA-N 0.000 claims 1
- OPTOVUDUEAOENY-MHZLTWQESA-N 7-methoxy-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC=1C(C(=O)N[C@@H](C)C=2C=CC=CC=2)=C2C=C(S(=O)(=O)C(C)C)C(OC)=CC2=NC=1C1=CC=CC(C(F)(F)F)=C1 OPTOVUDUEAOENY-MHZLTWQESA-N 0.000 claims 1
- XZRKCSZUWLMVRG-MGBGTMOVSA-N 7-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCOCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)C)C(F)(F)F)=CC=CC=C1 XZRKCSZUWLMVRG-MGBGTMOVSA-N 0.000 claims 1
- DRWRVADTSZFVRT-DEOSSOPVSA-N 7-methylsulfonyl-3-[(4-morpholin-4-ylpiperidin-1-yl)methyl]-N-[(1S)-1-phenylethyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC=C(C=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCOCC1 DRWRVADTSZFVRT-DEOSSOPVSA-N 0.000 claims 1
- HQCMXXDVYKYYAV-UUWRZZSWSA-N 7-methylsulfonyl-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]-N-[(1R)-2,2,2-trifluoro-1-phenylethyl]quinoline-4-carboxamide Chemical compound C1([C@@H](NC(=O)C=2C3=CC=C(C=C3N=C(C=2CN2CCC(CC2)N2CCCCC2)C=2C=C(C=CC=2)C(F)(F)F)S(=O)(=O)C)C(F)(F)F)=CC=CC=C1 HQCMXXDVYKYYAV-UUWRZZSWSA-N 0.000 claims 1
- CZAMFTAXTORWKB-VWLOTQADSA-N 7-methylsulfonyl-N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound N([C@@H](C)C=1C=CC=CC=1)C(=O)C(C1=CC=C(C=C1N=C1C=2C=C(C=CC=2)C(F)(F)F)S(C)(=O)=O)=C1CN(CC1)CCC1N1CCCCC1 CZAMFTAXTORWKB-VWLOTQADSA-N 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000008787 Cardiovascular Disease Diseases 0.000 claims 1
- 206010020853 Hypertonic bladder Diseases 0.000 claims 1
- 210000002161 Motor Neurons Anatomy 0.000 claims 1
- KARKVOFOODPNHQ-MHZLTWQESA-N N-[(1S)-1-phenylethyl]-3-[(4-piperidin-1-ylpiperidin-1-yl)methyl]-6-propan-2-ylsulfonyl-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCCC2)CCN1CC1=C(C(=O)N[C@@H](C)C=2C=CC=CC=2)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 KARKVOFOODPNHQ-MHZLTWQESA-N 0.000 claims 1
- JRMWVBAJZVYHNG-SANMLTNESA-N N-[(1S)-1-phenylethyl]-6-propan-2-ylsulfonyl-3-[(4-pyrrolidin-1-ylpiperidin-1-yl)methyl]-2-[3-(trifluoromethyl)phenyl]quinoline-4-carboxamide Chemical compound C1CC(N2CCCC2)CCN1CC1=C(C(=O)N[C@@H](C)C=2C=CC=CC=2)C2=CC(S(=O)(=O)C(C)C)=CC=C2N=C1C1=CC=CC(C(F)(F)F)=C1 JRMWVBAJZVYHNG-SANMLTNESA-N 0.000 claims 1
- 208000009722 Overactive Urinary Bladder Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 201000006233 congestive heart failure Diseases 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 238000001990 intravenous administration Methods 0.000 claims 1
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 claims 1
- 201000008482 osteoarthritis Diseases 0.000 claims 1
- 239000000546 pharmaceutic aid Substances 0.000 claims 1
- SECXISVLQFMRJM-UHFFFAOYSA-N CN(CCC1)C1=O Chemical compound CN(CCC1)C1=O SECXISVLQFMRJM-UHFFFAOYSA-N 0.000 description 1
Claims (13)
- 式Iの化合物またはその薬学上許容される塩:
R1は、独立に、H、CF3またはMeであり;
R2は、独立に、OH、OC1−4アルキル、C1−4アルキル、CH2OH、F、CH2OC1−4アルキル、CF3またはCF2Hであり;
R3は、モルホリニル、ピペリジニル、ピロリジニル、またはヘキサヒドロアゼピニルであり;これらはすべて、非置換であっても、1個または2個のR8で置換されていてもよく;
あるいは、R3は、N(C1−6アルキル)2であり、ここで、C1−6アルキルは非置換であっても、OHまたは−OCH3で置換されていてもよく;
R4は、CF3、ハロ、OMe、またはC1−3アルキルであり;
R5は、
ここで、
R6は、独立に、C1−4アルキル、C3−6シクロアルキルであり;
R7は、独立に、ハロ、メチル、またはOMeであり;
R8は、独立に、OH、OC1−4アルキル、C1−4アルキル、CH2OH、F、CH2OC1−4アルキル、CF3、またはCF2Hであり;
R9は、独立に、ピロリジニル、モルホリニル、またはピペリジニルであり;
R10は、独立に、H、CF3、またはMeであり;
nは、独立に、0、1、または2であり;
Xは、NまたはCであり;
yは、1または2である]。 - R1が、独立に、CF3またはMeであり;
R2が、独立に、OH、OC1−4アルキル、C1−4アルキル、CH2OH、F、CH2OC1−4アルキル、CF3、またはCF2Hであり;
R3が、モルホリニル、ピペリジニル、ピロリジニル、またはヘキサヒドロアゼピニルであり;これらはすべて、非置換であっても、1個または2個のR8で置換されていてもよく;
あるいは、R3が、N(C1−6アルキル)2であり、ここで、C1−6アルキルは非置換であっても、OHまたは−OCH3で置換されていてもよく;
R4が、CF3またはハロであり;
R5が、
ここで、
R6が、独立に、C1−4アルキルまたはC3−6シクロアルキルであり;
R7が、独立に、ハロ、メチル、またはOMeであり;
R8が、独立に、OH、OC1−4アルキル、C1−4アルキル、CH2OH、F、CH2OC1−4アルキル、CF3またはCF2Hであり;
R9が、独立に、ピロリジニル、モルホリニル、またはピペリジニルであり;
R10が、Hであり;
nが、独立に、0または1であり;
Xが、NまたはCであり;かつ
yが、1または2である、請求項1に記載の式(I)の化合物またはその薬学上許容される塩。 - R1が、独立に、CF3またはMeであり;
R2が、独立に、C1−4アルキル、CF3、またはCF2Hであり;
R3が、モルホリニル、ピペリジニル、ピロリジニル、またはヘキサヒドロアゼピニルであり;これらはすべて、非置換であっても、1個または2個のR8で置換されていてもよく;
あるいは、R3が、N(C1−6アルキル)2であり、ここで、C1−6アルキルは非置換であっても、OHまたは−OCH3で置換されていてもよく;
R4が、CF3またはハロであり;
R5が、ハロ、シアノ、CF3、C1−5アルキル、C2−4アルケニル、OH、O−C1−4アルキル−OR6、OCF3、OCH2CF3、OCH2CN、またはOR6であり;
R6が、独立に、C1−4アルキルまたはC3−6シクロアルキルであり;
R7が、独立に、ハロ、メチル、またはOMeであり;
R8が、独立に、OH、OC1−4アルキル、C1−4アルキル、CH2OH、F、CH2OC1−4アルキル、CF3、またはCF2Hであり;
R10が、Hであり;
nが、独立に、0または1であり;
Xが、Nであり;かつ
yが、1または2である、請求項1に記載の式(I)の化合物またはその薬学上許容される塩。 - R1が、独立に、CF3またはMeであり;
R2が、独立に、C1−4アルキルであり;
R3が、モルホリニル、ピペリジニル、ピロリジニル、またはヘキサヒドロアゼピニルであり;これらはすべて、非置換であっても、1個または2個のR8で置換されていてもよく;
R4が、CF3またはハロであり;
R5が、ハロ、シアノ、CF3、C1−5アルキル、C2−4アルケニル、OH、O−C1−4アルキル−OR6、OCF3、OCH2CF3、OCH2CN、またはOR6であり;
R6が、独立に、C1−4アルキルまたはC3−6シクロアルキルであり;
R7に関しては、Nが、0であり;
R8が、独立に、OH、C1−4アルキル、F、CF3、またはCF2Hであり;
R10が、Hであり;
nが、独立に、0または1であり;
Xが、Nであり;かつ
yが、1または2である、請求項1に記載の式(I)の化合物またはその薬学上許容される塩。 - 3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(メチルオキシ)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(メチルオキシ)−6−(メチルスルホニル)−2−[3−トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(メチルオキシ)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(メチルオキシ)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−7−(メチルオキシ)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルオキシ)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルオキシ)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−[(1−メチルエチル)オキシ]−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−[(1−メチルエチル)オキシ]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−[(1−メチルエチル)オキシ]−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−[(1−メチルエチル)オキシ]−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルオキシ)−6−[(1−メチルエチル)スルホニル]−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−[(1−メチルエチル)スルホニル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルオキシ)−6−(エチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルオキシ)−6−(エチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(エチルスルホニル)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(エチルスルホニル)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−[(1−メチルエチル)オキシ]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[3−メチル−4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[3−メチル−4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(3’−メチル−1,4’−ビピペリジン−1’−イル)メチル]−6−[(1−メチルエチル)スルホニル]−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルスルホニル)−N−(1−メチル−1−フェニルエチル)−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−(エチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−クロロ−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−クロロ−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1S)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−(エチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−(エチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−クロロ−6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
7−クロロ−6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−[(1−メチルエチル)スルホニル]−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−7−クロロ−6−[(1−メチルエチル)スルホニル]−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−クロロ−6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
72)7−クロロ−6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−({4−[(3S)−3−フルオロ−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(3S)−3−フルオロ−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−[(4,4−ジフルオロ−1,4’−ビピペリジン−1’−イル)メチル]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(4,4−ジフルオロ−1,4’−ビピペリジン−1’−イル)メチル]−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−{[(3S)−3−ヒドロキシ−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[(3S)−3−ヒドロキシ−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−{[(3R)−3−ヒドロキシ−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[(3R)−3−ヒドロキシ−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−3−({4−[2−(トリフルオロメチル)−1−ピロリジニル]−1−ピペリジニル}メチル)−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−3−({4−[2−(トリフルオロメチル)−1−ピロリジニル]−1−ピペリジニル}メチル)−4−キノリンカルボキサミド;
3−{[3−(メチルオキシ)−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(4−フルオロ−1,4’−ビピペリジン−1’−イル)メチル]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[4−(ジエチルアミノ)−1−ピペリジニル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[4−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−2−[4−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−2−[4−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[4−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[4−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[4−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−2−[4−(メチルオキシ)フェニル]−6−(メチルスルホニル)−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3,4−ジクロロフェニル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1S)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[4−(3,3−ジフルオロ−1−ピロリジニル)−1−ピペリジニル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[4−(3,3−ジフルオロ−1−ピロリジニル)−1−ピペリジニル]メチル}−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
3−({4−[(3R)−3−ヒドロキシ−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(3S)−3−ヒドロキシ−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3−ブロモフェニル)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
2−(3−ブロモフェニル)−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−N−[(1S)−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−2−(3−ブロモフェニル)−6−(メチルスルホニル)−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−2−(3−ブロモフェニル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3−ブロモフェニル)−6−(メチルスルホニル)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
2−(3−ブロモフェニル)−6−(メチルスルホニル)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1S)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(2R)−2−メチル−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(3−フルオロ−1,4’−ビピペリジン−1’−イル)メチル]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(2S)−2−メチル−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(2S)−2−(ヒドロキシメチル)−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(2R)−2−(ヒドロキシメチル)−1−ピロリジニル]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[3−(ヒドロキシメチル)−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(4−{メチル[2−(メチルオキシ)エチル]アミノ}−1−ピペリジニル)メチル]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[エチル(プロピル)アミノ]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[メチル(2−メチルプロピル)アミノ]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[4−(ヘキサヒドロ−1H−アゼピン−1−イル)−1−ピペリジニル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−{[4−(メチルオキシ)−1,4’−ビピペリジン−1’−イル]メチル}−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[メチル(プロピル)アミノ]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−[(4−{(2S)−2−[(メチルオキシ)メチル]−1−ピロリジニル}−1−ピペリジニル)メチル]−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−({4−[(2−ヒドロキシエチル)(メチル)アミノ]−1−ピペリジニル}メチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−(メチルオキシ)−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−7−(メチルオキシ)−N−[(1S)−1−フェニルエチル]−3−{[4−(1−ピロリジニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド;
6−(エチルスルホニル)−3−[(4−フルオロ−1,4’−ビピペリジン−1’−イル)メチル]−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;および
6−(エチルスルホニル)−3−[(4−フルオロ−1,4’−ビピペリジン−1’−イル)メチル]−7−(メチルオキシ)−N−[(1S)−1−フェニルエチル]−2−[3−(トリフルオロメチル)フェニル]−4−キノリンカルボキサミド
からなる群から選択される請求項1に記載の化合物またはその薬学上許容される塩。 - 3−(1,4’−ビピペリジン−1’−イルメチル)−6−(メチルスルホニル)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−(エチルスルホニル)−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−[(1−メチルエチル)オキシ]−6−(メチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−[(1−メチルエチル)スルホニル]−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
7−(エチルオキシ)−6−(エチルスルホニル)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−3−{[3−メチル−4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド
からなる群から選択される請求項1に記載の化合物またはその薬学上許容される塩。 - 3−(1,4’−ビピペリジン−1’−イルメチル)−6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド;
6−[(1−メチルエチル)スルホニル]−7−(メチルオキシ)−3−{[4−(4−モルホリニル)−1−ピペリジニル]メチル}−2−[3−(トリフルオロメチル)フェニル]−N−[(1R)−2,2,2−トリフルオロ−1−フェニルエチル]−4−キノリンカルボキサミド
からなる群から選択される請求項1に記載の化合物またはその薬学上許容される塩。 - 請求項1〜7のいずれか一項に記載の化合物またはその薬学上許容される塩を含んでなる、医薬組成物。
- 薬学上許容される担体または賦形剤をさらに含んでなる、請求項8に記載の医薬組成物。
- うっ血性心不全、過活動膀胱、疼痛、心血管疾患、運動ニューロン障害、または変形性関節症の処置に用いるための、請求項8または9に記載の医薬組成物。
- 経口投与するための、請求項10に記載の医薬組成物。
- 静脈内投与するための、請求項10に記載の医薬組成物。
- 吸入により投与するための、請求項10に記載の医薬組成物。
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Families Citing this family (6)
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WO2013146754A1 (ja) | 2012-03-27 | 2013-10-03 | 塩野義製薬株式会社 | Trpv4阻害活性を有する芳香族複素5員環誘導体 |
US10335414B2 (en) | 2012-12-03 | 2019-07-02 | Indiana University Research And Technology Corporation | Use of TRPV4 antagonists to ameliorate hydrocephalus and related materials and methods |
JPWO2015046193A1 (ja) | 2013-09-25 | 2017-03-09 | 塩野義製薬株式会社 | Trpv4阻害活性を有する芳香族複素環式アミン誘導体 |
WO2018156401A1 (en) | 2017-02-24 | 2018-08-30 | Indiana University Research And Technology Corporation | Methods of inhibiting serum glucocorticoid induced kinase 1 (sgk1) as a treatment for salt and water balance diseases |
CN115427409A (zh) | 2020-04-30 | 2022-12-02 | 拉夸里亚创药株式会社 | 作为trpv4拮抗剂的嘧啶-4(3h)-酮衍生物 |
MX2023000610A (es) | 2020-07-16 | 2023-02-13 | Raqualia Pharma Inc | Inhibidor de trpv4 como agente terapeutico para enfermedades oculares. |
Family Cites Families (8)
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TW531537B (en) * | 1995-12-27 | 2003-05-11 | Janssen Pharmaceutica Nv | 1-(1,2-disubstituted piperidinyl)-4-substituted piperidine derivatives |
HUP0104959A3 (en) * | 1998-11-20 | 2003-01-28 | Glaxosmithkline Lab | Quinoline-4-carboxamide derivatives their preparation, their use as nk-3 and nk-2 receptor antagonists and medicaments containing them |
US6511649B1 (en) * | 1998-12-18 | 2003-01-28 | Thomas D. Harris | Vitronectin receptor antagonist pharmaceuticals |
SE0004054D0 (sv) | 2000-11-06 | 2000-11-06 | Astrazeneca Ab | N-type calcium channel antagonists for the treatment of pain |
GB0028964D0 (en) * | 2000-11-28 | 2001-01-10 | Smithkline Beecham Spa | Novel compounds |
EP1968968A1 (en) | 2005-12-21 | 2008-09-17 | PainCeptor Pharma Corp. | Compositions and methods for modulating gated ion channels |
JP5607046B2 (ja) * | 2008-07-25 | 2014-10-15 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニー | Trpv4拮抗薬 |
WO2011119693A1 (en) * | 2010-03-23 | 2011-09-29 | Glaxosmithkline Llc | Trpv4 antagonists |
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2011
- 2011-03-23 US US13/635,952 patent/US8658636B2/en not_active Expired - Fee Related
- 2011-03-23 WO PCT/US2011/029579 patent/WO2011119701A1/en active Application Filing
- 2011-03-23 EP EP11760129.4A patent/EP2549872B1/en not_active Not-in-force
- 2011-03-23 JP JP2013501427A patent/JP5819397B2/ja not_active Expired - Fee Related
- 2011-03-23 ES ES11760129.4T patent/ES2561674T3/es active Active
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