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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Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US9630929B2 (en) | 2011-10-31 | 2017-04-25 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| JP6014155B2 (ja) | 2011-10-31 | 2016-10-25 | ゼノン・ファーマシューティカルズ・インコーポレイテッドＸｅｎｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用 |
| US8889741B2 (en) * | 2012-02-09 | 2014-11-18 | Daiichi Sankyo Company, Limited | Cycloalkane derivatives |
| SG11201408284VA (en) | 2012-05-22 | 2015-02-27 | Xenon Pharmaceuticals Inc | N-substituted benzamides and their use in the treatment of pain |
| US10071957B2 (en) | 2012-07-06 | 2018-09-11 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
| US9388179B2 (en) | 2012-10-26 | 2016-07-12 | Merck Sharp & Dohme Corp. | N-substituted indazole sulfonamide compounds with selective activity in voltage-gated sodium channels |
| US9550775B2 (en) | 2013-03-14 | 2017-01-24 | Genentech, Inc. | Substituted triazolopyridines and methods of use thereof |
| EP2974730B1 (en) * | 2013-03-14 | 2018-01-31 | Daiichi Sankyo Company, Limited | Drug for respiratory diseases |
| MX2015010775A (es) | 2013-03-15 | 2016-04-25 | Genentech Inc | Benzoxazoles sustituidos y metodos para usarlos. |
| CR20160296A (es) | 2013-11-27 | 2016-09-20 | Genentech Inc | Benzamidas sustituidas y métodos para usarlas |
| WO2015077905A1 (en) * | 2013-11-29 | 2015-06-04 | Merck Sharp & Dohme Corp. | Bicycloamine-substituted-n-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels |
| CN106715418A (zh) | 2014-07-07 | 2017-05-24 | 基因泰克公司 | 治疗化合物及其使用方法 |
| JP2018520107A (ja) | 2015-05-22 | 2018-07-26 | ジェネンテック， インコーポレイテッド | 置換ベンズアミド及びその使用方法 |
| EP3341353A1 (en) | 2015-08-27 | 2018-07-04 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| RS63319B1 (sr) * | 2015-09-02 | 2022-07-29 | Trevena Inc | Jedinjenja koja modulišu delta-opioidni receptor, koja sadrže 6-člani aza-heterociklik, postupci njihove upotrebe i spravljanja |
| CN108290881B (zh) | 2015-09-28 | 2021-12-07 | 健泰科生物技术公司 | 治疗性化合物和其使用方法 |
| RU2724345C2 (ru) * | 2015-10-09 | 2020-06-23 | Галапагос Нв | N-СУЛЬФОНИЛИРОВАННЫЕ ПИРАЗОЛО[3,4-b]ПИРИДИН-6-КАРБОКСАМИДЫ И СПОСОБ ИХ ПРИМЕНЕНИЯ |
| US10316026B2 (en) | 2015-11-06 | 2019-06-11 | Daiichi Sankyo Company, Limited | Method for removing dimethoxybenzyl group |
| US10899732B2 (en) | 2015-11-25 | 2021-01-26 | Genentech, Inc. | Substituted benzamides useful as sodium channel blockers |
| EP3390374B1 (en) | 2015-12-18 | 2020-08-26 | Merck Sharp & Dohme Corp. | Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| EP3854782A1 (en) | 2016-03-30 | 2021-07-28 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| HRP20250505T1 (hr) * | 2016-05-20 | 2025-06-20 | Xenon Pharmaceuticals Inc. | Spojevi benzensulfonamida i njihova uporaba za terapijska sredstva |
| AU2017347549A1 (en) * | 2016-10-17 | 2019-05-02 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| ES2897998T3 (es) * | 2016-10-27 | 2022-03-03 | Bristol Myers Squibb Co | Inhibidores de la acilsulfonamida del NaV1.7 |
| ES2967410T3 (es) * | 2016-12-09 | 2024-04-30 | Xenon Pharmaceuticals Inc | Compuestos de bencenosulfonamida y sus usos en forma de agentes terapéuticos |
| CN110446495B (zh) | 2017-02-17 | 2023-09-05 | 特维娜有限公司 | 含有7元氮杂杂环的δ阿片受体调节化合物及其使用和制备方法 |
| AU2018221148B2 (en) | 2017-02-17 | 2022-05-05 | Trevena, Inc. | 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| JP2020511511A (ja) | 2017-03-24 | 2020-04-16 | ジェネンテック， インコーポレイテッド | ナトリウムチャネル阻害剤としての４−ピペリジン−ｎ−（ピリミジン−４−イル）クロマン−７−スルホンアミド誘導体 |
| AR114263A1 (es) | 2018-02-26 | 2020-08-12 | Genentech Inc | Compuestos terapéuticos y métodos para utilizarlos |
| WO2019191702A1 (en) | 2018-03-30 | 2019-10-03 | F. Hoffmann-La Roche Ag | Substituted hydro-pyrido-azines as sodium channel inhibitors |
| TW202003490A (zh) | 2018-05-22 | 2020-01-16 | 瑞士商赫孚孟拉羅股份公司 | 治療性化合物及其使用方法 |
| CN112262142B (zh) | 2018-06-13 | 2023-11-14 | 泽农医药公司 | 苯磺酰胺化合物及其作为治疗剂的用途 |
| MX2021001380A (es) | 2018-08-31 | 2021-05-27 | Xenon Pharmaceuticals Inc | Compuestos de sulfonamida sustituidos con heteroarilo y su uso como agentes terapeuticos. |
| MA53488A (fr) * | 2018-08-31 | 2021-12-08 | Xenon Pharmaceuticals Inc | Composés de sulfonamide substitués par hétéroaryle et leur utilisation en tant qu'inhibiteurs de canaux sodiques |
| EP3891157A4 (en) | 2018-12-05 | 2022-08-31 | Merck Sharp & Dohme Corp. | 4-AMINO- OR 4-ALKOXY-SUBSTITUTED ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATE SODIUM CHANNELS |
| WO2020248123A1 (en) | 2019-06-11 | 2020-12-17 | Merck Sharp & Dohme Corp. | Hydroxypyrrolidine-substituted arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| CA3224519A1 (en) * | 2021-07-06 | 2023-01-12 | Ralph A. Tripp | Compositions and methods for treating and preventing viral infections |
| US20260055083A1 (en) * | 2022-08-19 | 2026-02-26 | Maze Therapeutics, Inc. | Apol1 inhibitors and methods of use |
| CR20250551A (es) * | 2023-07-07 | 2026-01-19 | Novartis Ag | Bloqueadores de canales de sodio |
Family Cites Families (100)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3705185A (en) | 1969-04-14 | 1972-12-05 | Minnesota Mining & Mfg | N-aroyl sulfonamides |
| US3845770A (en) | 1972-06-05 | 1974-11-05 | Alza Corp | Osmatic dispensing device for releasing beneficial agent |
| US4326525A (en) | 1980-10-14 | 1982-04-27 | Alza Corporation | Osmotic device that improves delivery properties of agent in situ |
| GB8524157D0 (en) | 1984-10-19 | 1985-11-06 | Ici America Inc | Heterocyclic amides |
| DK24089D0 (da) | 1989-01-20 | 1989-01-20 | Hans Bundgaard | Novel prodrug derivatives of biologically active agents containing hydroxyl groups or nh-acidic groups |
| GB8911854D0 (en) | 1989-05-23 | 1989-07-12 | Ici Plc | Heterocyclic compounds |
| IL101860A0 (en) | 1991-05-31 | 1992-12-30 | Ici Plc | Heterocyclic derivatives |
| ES2187518T3 (es) | 1992-11-23 | 2003-06-16 | Aventis Pharma Inc | 3-(aminoalquilamino)-1-2-benzisoxazoles sustituidos y compuestos relacionados. |
| US5573653A (en) | 1994-07-11 | 1996-11-12 | Sandoz Ltd. | Electrochemical process for thiocyanating aminobenzene compounds |
| ES2208690T3 (es) | 1994-08-30 | 2004-06-16 | Sankyo Company Limited | Isoxazol. |
| US5753653A (en) | 1995-12-08 | 1998-05-19 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses |
| US6416780B1 (en) | 1997-05-07 | 2002-07-09 | Galen (Chemicals) Limited | Intravaginal drug delivery devices for the administration of testosterone and testosterone precursors |
| GB9828442D0 (en) | 1998-12-24 | 1999-02-17 | Karobio Ab | Novel thyroid receptor ligands and method II |
| KR100789567B1 (ko) | 2001-11-06 | 2007-12-28 | 동화약품공업주식회사 | 3-아미도-1,2-벤조이소옥사졸 유도체, 그 염, 제조방법 및 용도 |
| DE10201550A1 (de) | 2002-01-17 | 2003-07-31 | Merck Patent Gmbh | Phenoxy-Piperidine |
| US7332486B2 (en) | 2002-08-08 | 2008-02-19 | Memory Pharmaceuticals Corp. | Phosphodiesterase 4 inhibitors |
| MY141521A (en) | 2002-12-12 | 2010-05-14 | Hoffmann La Roche | 5-substituted-six-membered heteroaromatic glucokinase activators |
| AP2005003418A0 (en) | 2003-04-15 | 2005-12-31 | Pfizer | Alpha substituted carboxylic acids as ppar modulators. |
| EP1673357A2 (en) | 2003-08-08 | 2006-06-28 | Vertex Pharmaceuticals Incorporated | Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain |
| CN1863785A (zh) * | 2003-08-08 | 2006-11-15 | 沃泰克斯药物股份有限公司 | 在疼痛的治疗中用作钠或钙通道阻断剂的杂芳基氨基磺酰基苯基衍生物 |
| ES2334795T3 (es) | 2003-10-03 | 2010-03-16 | Portola Pharmaceuticals, Inc. | Sulfonilureas 2,4-dioxo-3-quinazolinilarilo. |
| US7081539B2 (en) | 2004-03-25 | 2006-07-25 | Dainippon Sumitomo Pharma Co., Ltd. | One-pot process for the preparation of 1,2-benzisoxazole-3-methanesulfonamide |
| US20080312286A1 (en) | 2004-07-30 | 2008-12-18 | Pinkerton Anthony B | Indanone Potentiators of Metabotropic Glutamate Receptors |
| WO2006020830A2 (en) | 2004-08-12 | 2006-02-23 | Amgen Inc. | Bisaryl-sulfonamides |
| EP1812429A4 (en) | 2004-09-29 | 2010-07-21 | Portola Pharm Inc | SUBSTITUTED 2H-1,3-BENZOXAZIN-4 (3H) -ONE |
| JP2008189549A (ja) | 2005-05-12 | 2008-08-21 | Astellas Pharma Inc | カルボン酸誘導体またはその塩 |
| DE102005038947A1 (de) | 2005-05-18 | 2006-11-30 | Grünenthal GmbH | Substituierte Benzo[d]isoxazol-3-yl-amin-Verbindungen und deren Verwendung in Arzneimitteln |
| US7632837B2 (en) | 2005-06-17 | 2009-12-15 | Bristol-Myers Squibb Company | Bicyclic heterocycles as cannabinoid-1 receptor modulators |
| CN101277939A (zh) | 2005-09-09 | 2008-10-01 | 布里斯托尔-迈尔斯斯奎布公司 | 无环ikur抑制剂 |
| CA2625039A1 (en) | 2005-10-19 | 2007-04-26 | F. Hoffmann-La Roche Ag | N-phenyl phenylacetamide non-nucleoside reverse transcriptase inihibitors |
| CA2630234A1 (en) | 2005-11-23 | 2007-05-31 | Ligand Pharmaceuticals Inc. | Thrombopoietin activity modulating compounds and methods |
| AR058296A1 (es) * | 2005-12-09 | 2008-01-30 | Kalypsys Inc | Inhibidores de histona desacetilasa y composicion farmaceutica |
| EP2004596A2 (en) | 2006-04-11 | 2008-12-24 | Vertex Pharmaceuticals Incorporated | Compositions useful as inhibitors of voltage-gated sodium channels |
| WO2008045393A2 (en) | 2006-10-11 | 2008-04-17 | Amgen Inc. | Imidazo- and triazolo-pyridine compounds and methods of use therof |
| CA2676665A1 (en) | 2007-01-30 | 2008-08-07 | Biogen Idec Ma Inc. | Modulators of mitotic kinases |
| AU2008213836A1 (en) | 2007-02-05 | 2008-08-14 | Xenon Pharmaceuticals Inc. | Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions |
| EP1995241B1 (en) | 2007-03-23 | 2010-03-17 | ICAgen, Inc. | Inhibitors of ion channels |
| MX2009012678A (es) | 2007-05-25 | 2012-09-20 | Vertex Pharma | Moduladores de canal de ion y metodos de uso. |
| US20100179137A1 (en) | 2007-06-07 | 2010-07-15 | Takashi Kamikubo | Pyridone compound |
| US20090012103A1 (en) | 2007-07-05 | 2009-01-08 | Matthew Abelman | Substituted heterocyclic compounds |
| WO2009010784A1 (en) | 2007-07-13 | 2009-01-22 | Astrazeneca Ab | New compounds 955 |
| US8124610B2 (en) | 2007-07-13 | 2012-02-28 | Icagen Inc. | Sodium channel inhibitors |
| US20110092703A1 (en) * | 2007-08-10 | 2011-04-21 | Nippon Chemiphar Co., Ltd. | P2x4 receptor antagonist |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| WO2009086303A2 (en) | 2007-12-21 | 2009-07-09 | University Of Rochester | Method for altering the lifespan of eukaryotic organisms |
| JP5304785B2 (ja) | 2008-06-23 | 2013-10-02 | アステラス製薬株式会社 | スルホンアミド化合物又はその塩 |
| WO2010022055A2 (en) | 2008-08-20 | 2010-02-25 | Amgen Inc. | Inhibitors of voltage-gated sodium channels |
| CN101653458A (zh) | 2008-08-22 | 2010-02-24 | 天津生机集团股份有限公司 | 一种提高种猪繁殖性能的微量元素组合物 |
| PE20120008A1 (es) * | 2009-01-12 | 2012-01-24 | Icagen Inc | Derivados de fenoxi bencenosulfonamida |
| ES2642586T3 (es) | 2009-07-27 | 2017-11-16 | Gilead Sciences, Inc. | Compuestos heterocíclicos condensados como moduladores de canales iónicos |
| WO2011016234A1 (en) | 2009-08-04 | 2011-02-10 | Raqualia Pharma Inc. | Picolinamide derivatives as ttx-s blockers |
| KR101678255B1 (ko) | 2009-09-25 | 2016-11-21 | 아스텔라스세이야쿠 가부시키가이샤 | 치환 아미드 화합물 |
| WO2011059042A1 (ja) | 2009-11-12 | 2011-05-19 | 武田薬品工業株式会社 | 芳香環化合物 |
| WO2011063001A1 (en) | 2009-11-18 | 2011-05-26 | Concert Pharmaceuticals, Inc. | Niacin prodrugs and deuterated versions thereof |
| TW201139406A (en) | 2010-01-14 | 2011-11-16 | Glaxo Group Ltd | Voltage-gated sodium channel blockers |
| HUE029012T2 (en) | 2010-02-12 | 2017-02-28 | Nivalis Therapeutics Inc | New S-nitrosoglutathion reductase inhibitors |
| WO2011153588A1 (en) | 2010-06-10 | 2011-12-15 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
| US20120004714A1 (en) | 2010-06-30 | 2012-01-05 | Ryan Kleve | Lead having coil electrode with preferential bending region |
| US9279003B2 (en) | 2010-07-07 | 2016-03-08 | Purdue Pharma L.P. | Analogs of sodium channel peptide toxin |
| JP5872552B2 (ja) | 2010-07-09 | 2016-03-01 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化学化合物 |
| CA2804593C (en) | 2010-07-09 | 2015-11-24 | Pfizer Limited | Biphenyloxybenzensulphonamide derivatives useful as sodium channel inhibitors |
| ES2526675T3 (es) | 2010-07-09 | 2015-01-14 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje |
| CA2804351A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Chemical compounds |
| JP2013531030A (ja) | 2010-07-12 | 2013-08-01 | ファイザー・リミテッド | 電位開口型ナトリウムチャネルの阻害剤としてのｎ−スルホニルベンズアミド |
| JP2013532184A (ja) | 2010-07-12 | 2013-08-15 | ファイザー・リミテッド | 電位開口型ナトリウムチャネル阻害剤として有用なｎ−スルホニルベンズアミド誘導体 |
| JP2013536165A (ja) | 2010-07-12 | 2013-09-19 | ファイザー・リミテッド | 痛みの処置のためのｎａｖ１．７阻害薬としてのスルホンアミド誘導体 |
| JP2013532185A (ja) | 2010-07-12 | 2013-08-15 | ファイザー・リミテッド | 化合物 |
| JP2013531687A (ja) | 2010-07-16 | 2013-08-08 | パーデュー、ファーマ、リミテッド、パートナーシップ | ナトリウムチャネル遮断剤としてのピリジン化合物 |
| PT2616465E (pt) | 2010-09-13 | 2016-03-09 | Novartis Ag | Triazino-oxadiazoles |
| WO2012039657A1 (en) | 2010-09-22 | 2012-03-29 | Astrazeneca Ab | Novel chromane compound for the treatment of pain disorders |
| EP2655330B1 (en) | 2010-12-22 | 2016-02-10 | Purdue Pharma LP | Substituted pyridines as sodium channel blockers |
| WO2012095781A1 (en) | 2011-01-13 | 2012-07-19 | Pfizer Limited | Indazole derivatives as sodium channel inhibitors |
| KR101923367B1 (ko) | 2011-02-02 | 2018-12-04 | 버텍스 파마슈티칼스 인코포레이티드 | 이온 채널의 조절제로서의 피롤로피라진―스피로사이클릭 피페리딘 아미드 |
| MX2014001851A (es) | 2011-08-17 | 2014-10-24 | Amgen Inc | Inhibidores del canal de heteroarilo sodio. |
| WO2013056232A2 (en) | 2011-10-13 | 2013-04-18 | Case Western Reserve University | Rxr agonists compounds and methods |
| IN2014CN02959A (https=) | 2011-10-28 | 2015-07-03 | Merck Sharp & Dohme | |
| US9630929B2 (en) | 2011-10-31 | 2017-04-25 | Xenon Pharmaceuticals Inc. | Benzenesulfonamide compounds and their use as therapeutic agents |
| JP6014155B2 (ja) | 2011-10-31 | 2016-10-25 | ゼノン・ファーマシューティカルズ・インコーポレイテッドＸｅｎｏｎ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃ． | ビアリールエーテルスルホンアミドおよび治療剤としてのそれらの使用 |
| US9133131B2 (en) | 2011-11-15 | 2015-09-15 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| US9012443B2 (en) | 2011-12-07 | 2015-04-21 | Amgen Inc. | Bicyclic aryl and heteroaryl sodium channel inhibitors |
| WO2013088315A1 (en) | 2011-12-15 | 2013-06-20 | Pfizer Limited | Sulfonamide derivatives |
| US20150291514A1 (en) | 2012-01-04 | 2015-10-15 | Pfizer Limted | N-Aminosulfonyl Benzamides |
| JP2015083542A (ja) | 2012-02-08 | 2015-04-30 | 大日本住友製薬株式会社 | ３位置換プロリン誘導体 |
| US8889741B2 (en) | 2012-02-09 | 2014-11-18 | Daiichi Sankyo Company, Limited | Cycloalkane derivatives |
| WO2013122897A1 (en) | 2012-02-13 | 2013-08-22 | Amgen Inc. | Dihydrobenzoxazine and tetrahydroquinoxaline sodium channel inhibitors |
| WO2013134518A1 (en) | 2012-03-09 | 2013-09-12 | Amgen Inc. | Sulfamide sodium channel inhibitors |
| WO2013146969A1 (ja) | 2012-03-29 | 2013-10-03 | 第一三共株式会社 | 新規二置換シクロヘキサン誘導体 |
| SG11201408284VA (en) | 2012-05-22 | 2015-02-27 | Xenon Pharmaceuticals Inc | N-substituted benzamides and their use in the treatment of pain |
| US10071957B2 (en) | 2012-07-06 | 2018-09-11 | Genentech, Inc. | N-substituted benzamides and methods of use thereof |
| CN104640843A (zh) | 2012-07-19 | 2015-05-20 | 大日本住友制药株式会社 | 1-(环烷基羰基)脯氨酸衍生物 |
| CA2889378A1 (en) | 2012-10-26 | 2014-05-01 | Merck Sharp & Dohme Corp. | Benzoxazolinone compounds with selective activity in voltage-gated sodium channels |
| US9388179B2 (en) | 2012-10-26 | 2016-07-12 | Merck Sharp & Dohme Corp. | N-substituted indazole sulfonamide compounds with selective activity in voltage-gated sodium channels |
| EP2935257B1 (en) | 2012-12-20 | 2018-02-07 | Purdue Pharma LP | Cyclic sulfonamides as sodium channel blockers |
| RS56015B1 (sr) | 2013-01-31 | 2017-09-29 | Vertex Pharma | Piridon amidi kao modulatori natrijumovih kanala |
| US20140296266A1 (en) | 2013-03-01 | 2014-10-02 | Gilead Sciences, Inc. | Therapeutic compounds |
| US9550775B2 (en) | 2013-03-14 | 2017-01-24 | Genentech, Inc. | Substituted triazolopyridines and methods of use thereof |
| ES2687481T3 (es) | 2013-03-15 | 2018-10-25 | Chromocell Corporation | Moduladores del canal de sodio para el tratamiento del dolor |
| MX2015010775A (es) | 2013-03-15 | 2016-04-25 | Genentech Inc | Benzoxazoles sustituidos y metodos para usarlos. |
| US9663508B2 (en) | 2013-10-01 | 2017-05-30 | Amgen Inc. | Biaryl acyl-sulfonamide compounds as sodium channel inhibitors |
| CR20160296A (es) | 2013-11-27 | 2016-09-20 | Genentech Inc | Benzamidas sustituidas y métodos para usarlas |
-
2012
- 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 CN CN201280065434.9A patent/CN104024251B/zh not_active Expired - Fee Related
- 2012-10-30 EP EP12845774.4A patent/EP2773637B1/en not_active Not-in-force
- 2012-10-30 JP JP2014537806A patent/JP6014154B2/ja not_active Expired - Fee Related
- 2012-10-30 BR BR112014010271A patent/BR112014010271A2/pt not_active IP Right Cessation
- 2012-10-30 CA CA2853439A patent/CA2853439A1/en not_active Abandoned
- 2012-10-30 MX MX2014005297A patent/MX2014005297A/es not_active Application Discontinuation
- 2012-10-30 RU RU2014121984/04A patent/RU2014121984A/ru not_active Application Discontinuation
- 2012-10-30 ES ES12845774.4T patent/ES2586213T3/es active Active
- 2012-10-30 WO PCT/IB2012/056031 patent/WO2013064983A1/en not_active Ceased
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