JP2014532640A5 - - Google Patents
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- JP2014532640A5 JP2014532640A5 JP2014537806A JP2014537806A JP2014532640A5 JP 2014532640 A5 JP2014532640 A5 JP 2014532640A5 JP 2014537806 A JP2014537806 A JP 2014537806A JP 2014537806 A JP2014537806 A JP 2014537806A JP 2014532640 A5 JP2014532640 A5 JP 2014532640A5
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- JP
- Japan
- Prior art keywords
- optionally substituted
- haloalkyl
- independently hydrogen
- alkyl
- halo
- 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.)
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 474
- 239000001257 hydrogen Substances 0.000 claims description 474
- 150000002431 hydrogen Chemical class 0.000 claims description 400
- 125000001188 haloalkyl group Chemical group 0.000 claims description 394
- 125000000217 alkyl group Chemical group 0.000 claims description 340
- 125000005843 halogen group Chemical group 0.000 claims description 290
- 150000001875 compounds Chemical class 0.000 claims description 193
- 125000001072 heteroaryl group Chemical group 0.000 claims description 122
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 120
- 125000000623 heterocyclic group Chemical group 0.000 claims description 120
- 125000003107 substituted aryl group Chemical group 0.000 claims description 102
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 84
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 74
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 69
- 239000000203 mixture Substances 0.000 claims description 61
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims description 58
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 56
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 56
- 208000002193 Pain Diseases 0.000 claims description 54
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 46
- 229910052757 nitrogen Inorganic materials 0.000 claims description 46
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims description 43
- 150000003839 salts Chemical class 0.000 claims description 38
- 239000000651 prodrug Substances 0.000 claims description 36
- 229940002612 prodrug Drugs 0.000 claims description 36
- 239000012453 solvate Substances 0.000 claims description 35
- 102000016913 Voltage-Gated Sodium Channels Human genes 0.000 claims description 28
- 108010053752 Voltage-Gated Sodium Channels Proteins 0.000 claims description 28
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims description 26
- 241000124008 Mammalia Species 0.000 claims description 23
- 229910052799 carbon Inorganic materials 0.000 claims description 23
- 125000002947 alkylene group Chemical group 0.000 claims description 22
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 16
- -1 1,2,4-thiadiazole-5 (4H) -ylidene Chemical group 0.000 claims description 14
- 201000010099 disease Diseases 0.000 claims description 14
- 125000000842 isoxazolyl group Chemical group 0.000 claims description 14
- 125000002098 pyridazinyl group Chemical group 0.000 claims description 14
- 125000004076 pyridyl group Chemical group 0.000 claims description 14
- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 14
- 125000003831 tetrazolyl group Chemical group 0.000 claims description 14
- 125000001113 thiadiazolyl group Chemical group 0.000 claims description 14
- 125000000335 thiazolyl group Chemical group 0.000 claims description 14
- 238000011282 treatment Methods 0.000 claims description 14
- 125000005842 heteroatom Chemical group 0.000 claims description 12
- 125000003118 aryl group Chemical group 0.000 claims description 10
- 125000004516 1,2,4-thiadiazol-5-yl group Chemical group S1N=CN=C1* 0.000 claims description 8
- 206010028980 Neoplasm Diseases 0.000 claims description 8
- 150000001408 amides Chemical class 0.000 claims description 8
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- 150000002500 ions Chemical class 0.000 claims description 8
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- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
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- 102000018674 Sodium Channels Human genes 0.000 claims description 6
- 108010052164 Sodium Channels Proteins 0.000 claims description 6
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims description 6
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- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 6
- 125000000547 substituted alkyl group Chemical group 0.000 claims description 6
- HBAQYPYDRFILMT-UHFFFAOYSA-N 8-[3-(1-cyclopropylpyrazol-4-yl)-1H-pyrazolo[4,3-d]pyrimidin-5-yl]-3-methyl-3,8-diazabicyclo[3.2.1]octan-2-one Chemical class C1(CC1)N1N=CC(=C1)C1=NNC2=C1N=C(N=C2)N1C2C(N(CC1CC2)C)=O HBAQYPYDRFILMT-UHFFFAOYSA-N 0.000 claims description 5
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- 230000002085 persistent effect Effects 0.000 claims description 4
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- 239000003053 toxin Substances 0.000 claims description 4
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- 208000003663 ventricular fibrillation Diseases 0.000 claims description 4
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- KHBQMWCZKVMBLN-UHFFFAOYSA-N Benzenesulfonamide Chemical compound NS(=O)(=O)C1=CC=CC=C1 KHBQMWCZKVMBLN-UHFFFAOYSA-N 0.000 claims description 3
- 206010010904 Convulsion Diseases 0.000 claims description 3
- 230000036461 convulsion Effects 0.000 claims description 3
- 230000003449 preventive effect Effects 0.000 claims description 3
- 229940124530 sulfonamide Drugs 0.000 claims description 3
- 238000001356 surgical procedure Methods 0.000 claims description 3
- RXEGZIXPUZCKFO-RDJZCZTQSA-N (3s,4r)-3-[(2,5-difluoro-4-pyrazol-1-ylsulfonylphenoxy)methyl]-4-(4-fluorophenyl)piperidine Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C(=CC(=C(F)C=2)S(=O)(=O)N2N=CC=C2)F)CNCC1 RXEGZIXPUZCKFO-RDJZCZTQSA-N 0.000 claims description 2
- ONEVOOWUJAOPSN-HOCLYGCPSA-N 2,5-difluoro-4-[[(1r,2r)-2-(4-fluorophenyl)cyclohexyl]methoxy]-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C(=CC(=C(F)C=2)S(=O)(=O)NC=2SN=CN=2)F)CCCC1 ONEVOOWUJAOPSN-HOCLYGCPSA-N 0.000 claims description 2
- ZBELRVLBJKOYGL-VYRBHSGPSA-N 2,5-difluoro-4-[[(3S)-4-(4-methylphenyl)piperidin-3-yl]methoxy]-N-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound Cc1ccc(cc1)C1CCNC[C@H]1COc1cc(F)c(cc1F)S(=O)(=O)Nc1ncns1 ZBELRVLBJKOYGL-VYRBHSGPSA-N 0.000 claims description 2
- XSBUZAIFXFCWIN-ZFWWWQNUSA-N 2,5-difluoro-4-[[(3r,4r)-3-(4-fluorophenyl)piperidin-4-yl]methoxy]-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1=CC(F)=CC=C1[C@H]1[C@H](COC=2C(=CC(=C(F)C=2)S(=O)(=O)NC=2SN=CN=2)F)CCNC1 XSBUZAIFXFCWIN-ZFWWWQNUSA-N 0.000 claims description 2
- WNPQUCQKSFDNDS-GJZGRUSLSA-N 2,5-difluoro-4-[[(3s,4r)-4-phenylpiperidin-3-yl]methoxy]-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2SN=CN=2)=CC=CC=C1 WNPQUCQKSFDNDS-GJZGRUSLSA-N 0.000 claims description 2
- YKHBPEAAJKQFPN-UHFFFAOYSA-N 2,5-difluoro-4-[[3-fluoro-4-(4-fluorophenyl)piperidin-3-yl]methoxy]-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1=CC(F)=CC=C1C1C(COC=2C(=CC(=C(F)C=2)S(=O)(=O)NC=2SN=CN=2)F)(F)CNCC1 YKHBPEAAJKQFPN-UHFFFAOYSA-N 0.000 claims description 2
- LDZNFFGWKHAEMM-GDBMZVCRSA-N 4-[[(3r,4s)-4-(4-chlorophenyl)-1-methylpiperidin-3-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C([C@@H]1[C@H](CCN(C1)C)C=1C=CC(Cl)=CC=1)OC(C(=C1)F)=CC(F)=C1S(=O)(=O)NC1=NC=NS1 LDZNFFGWKHAEMM-GDBMZVCRSA-N 0.000 claims description 2
- OCGIYHGXHMLCPX-UKRRQHHQSA-N 4-[[(3r,4s)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1([C@H]2CCNC[C@@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2SN=CN=2)=CC=C(Cl)C=C1 OCGIYHGXHMLCPX-UKRRQHHQSA-N 0.000 claims description 2
- OWHQKZMRBOBBBR-HOCLYGCPSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)-1-(2,2,2-trifluoroethyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1([C@@H]2CCN(CC(F)(F)F)C[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2SN=CN=2)=CC=C(Cl)C=C1 OWHQKZMRBOBBBR-HOCLYGCPSA-N 0.000 claims description 2
- LDZNFFGWKHAEMM-HOCLYGCPSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)-1-methylpiperidin-3-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C([C@H]1[C@@H](CCN(C1)C)C=1C=CC(Cl)=CC=1)OC(C(=C1)F)=CC(F)=C1S(=O)(=O)NC1=NC=NS1 LDZNFFGWKHAEMM-HOCLYGCPSA-N 0.000 claims description 2
- OCGIYHGXHMLCPX-ZFWWWQNUSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2SN=CN=2)=CC=C(Cl)C=C1 OCGIYHGXHMLCPX-ZFWWWQNUSA-N 0.000 claims description 2
- QHQZPTNDCRWOPP-WMZOPIPTSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-(2-methylpropyl)benzenesulfonamide Chemical compound C1=C(F)C(S(=O)(=O)NCC(C)C)=CC(F)=C1OC[C@H]1[C@H](C=2C=CC(Cl)=CC=2)CCNC1 QHQZPTNDCRWOPP-WMZOPIPTSA-N 0.000 claims description 2
- OPEKIKRIMJMTHW-RDJZCZTQSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-(5-methyl-1,3-thiazol-2-yl)benzenesulfonamide Chemical compound S1C(C)=CN=C1NS(=O)(=O)C(C(=C1)F)=CC(F)=C1OC[C@H]1[C@H](C=2C=CC(Cl)=CC=2)CCNC1 OPEKIKRIMJMTHW-RDJZCZTQSA-N 0.000 claims description 2
- HGVRIBHCYYWMFY-RDJZCZTQSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluoro-n-pyrimidin-4-ylbenzenesulfonamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2N=CN=CC=2)=CC=C(Cl)C=C1 HGVRIBHCYYWMFY-RDJZCZTQSA-N 0.000 claims description 2
- OZYNNENNGZDQTQ-JSGCOSHPSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluorobenzenesulfonamide Chemical compound C1=C(F)C(S(=O)(=O)N)=CC(F)=C1OC[C@H]1[C@H](C=2C=CC(Cl)=CC=2)CCNC1 OZYNNENNGZDQTQ-JSGCOSHPSA-N 0.000 claims description 2
- ILFBDKXJABKTIM-RXVVDRJESA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-3-cyano-n-propan-2-ylbenzenesulfonamide Chemical compound N#CC1=CC(S(=O)(=O)NC(C)C)=CC=C1OC[C@H]1[C@H](C=2C=CC(Cl)=CC=2)CCNC1 ILFBDKXJABKTIM-RXVVDRJESA-N 0.000 claims description 2
- PWDWJKYTQFZCLL-YOEHRIQHSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-3-fluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC=C(C=C2F)S(=O)(=O)NC=2SN=CN=2)=CC=C(Cl)C=C1 PWDWJKYTQFZCLL-YOEHRIQHSA-N 0.000 claims description 2
- YNYVWCSZRIZIPK-ZFWWWQNUSA-N 4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-n-(5-chloro-1,3-thiazol-2-yl)-2,5-difluorobenzenesulfonamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC=2SC(Cl)=CN=2)=CC=C(Cl)C=C1 YNYVWCSZRIZIPK-ZFWWWQNUSA-N 0.000 claims description 2
- BODLISSZAMYJQE-UHFFFAOYSA-N 4-[[1-(4-chlorophenyl)piperazin-2-yl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound FC1=CC(S(=O)(=O)NC=2SN=CN=2)=C(F)C=C1OCC1CNCCN1C1=CC=C(Cl)C=C1 BODLISSZAMYJQE-UHFFFAOYSA-N 0.000 claims description 2
- DHAFMZGQYJAEFS-UHFFFAOYSA-N 4-[[2-(4-chlorophenyl)-5-oxocyclohexyl]methoxy]-2,5-difluoro-n-(1,2,4-thiadiazol-5-yl)benzenesulfonamide Chemical compound FC1=CC(S(=O)(=O)NC=2SN=CN=2)=C(F)C=C1OCC1CC(=O)CCC1C1=CC=C(Cl)C=C1 DHAFMZGQYJAEFS-UHFFFAOYSA-N 0.000 claims description 2
- CAQCNSRXCSSIQR-WCQYABFASA-N C1CN(C[C@H]([C@@H]1C2=CC(=C(C=C2F)F)F)COC3=C(C=CC(=C3)F)F)C4=NC=NS4 Chemical compound C1CN(C[C@H]([C@@H]1C2=CC(=C(C=C2F)F)F)COC3=C(C=CC(=C3)F)F)C4=NC=NS4 CAQCNSRXCSSIQR-WCQYABFASA-N 0.000 claims description 2
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- GOAIBJBKJNXGFS-HOCLYGCPSA-N n-[4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluorophenyl]sulfonylacetamide Chemical compound C1=C(F)C(S(=O)(=O)NC(=O)C)=CC(F)=C1OC[C@H]1[C@H](C=2C=CC(Cl)=CC=2)CCNC1 GOAIBJBKJNXGFS-HOCLYGCPSA-N 0.000 claims description 2
- RLJLEWLDIPDGDN-ICSRJNTNSA-N n-[4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluorophenyl]sulfonylbenzamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC(=O)C=2C=CC=CC=2)=CC=C(Cl)C=C1 RLJLEWLDIPDGDN-ICSRJNTNSA-N 0.000 claims description 2
- QPUNFLXJVJVFBE-WMZOPIPTSA-N n-[4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluorophenyl]sulfonylpyridine-2-carboxamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC(=O)C=2N=CC=CC=2)=CC=C(Cl)C=C1 QPUNFLXJVJVFBE-WMZOPIPTSA-N 0.000 claims description 2
- FAOBNWUCNFYVIZ-HKUYNNGSSA-N n-[4-[[(3s,4r)-4-(4-chlorophenyl)piperidin-3-yl]methoxy]-2,5-difluorophenyl]sulfonylpyridine-3-carboxamide Chemical compound C1([C@@H]2CCNC[C@H]2COC2=CC(F)=C(C=C2F)S(=O)(=O)NC(=O)C=2C=NC=CC=2)=CC=C(Cl)C=C1 FAOBNWUCNFYVIZ-HKUYNNGSSA-N 0.000 claims description 2
- 230000000926 neurological effect Effects 0.000 claims description 2
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- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims description 2
- 230000008733 trauma Effects 0.000 claims description 2
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 23
- 238000002560 therapeutic procedure Methods 0.000 claims 5
- 229910021386 carbon form Inorganic materials 0.000 claims 3
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- 229940079593 drug Drugs 0.000 claims 1
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- 230000001105 regulatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 26
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Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161553616P | 2011-10-31 | 2011-10-31 | |
| US61/553,616 | 2011-10-31 | ||
| PCT/IB2012/056031 WO2013064983A1 (en) | 2011-10-31 | 2012-10-30 | Benzenesulfonamide compounds and their use as therapeutic agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
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- 2012-10-30 BR BR112014010271A patent/BR112014010271A2/pt not_active IP Right Cessation
- 2012-10-30 CN CN201280065434.9A patent/CN104024251B/zh not_active Expired - Fee Related
- 2012-10-30 CA CA2853439A patent/CA2853439A1/en not_active Abandoned
- 2012-10-30 ES ES12845774.4T patent/ES2586213T3/es active Active
- 2012-10-30 WO PCT/IB2012/056031 patent/WO2013064983A1/en not_active Ceased
- 2012-10-30 EP EP12845774.4A patent/EP2773637B1/en not_active Not-in-force
- 2012-10-30 US US14/355,552 patent/US9630929B2/en not_active Expired - Fee Related
- 2012-10-30 KR KR1020147014213A patent/KR20140091022A/ko not_active Withdrawn
- 2012-10-30 JP JP2014537806A patent/JP6014154B2/ja not_active Expired - Fee Related
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