JP2014532640A5 - - Google Patents
Download PDFInfo
- Publication number
- 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
- Authority
- 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.)
- Granted
Links
- 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
- 201000011510 cancer Diseases 0.000 claims description 8
- 150000002500 ions Chemical class 0.000 claims description 8
- 230000001404 mediated effect Effects 0.000 claims description 8
- 125000000956 methoxy group Chemical group [H]C([H])([H])O* 0.000 claims description 8
- 208000033808 peripheral neuropathy Diseases 0.000 claims description 8
- 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
- 201000006417 multiple sclerosis Diseases 0.000 claims description 6
- 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
- 208000019901 Anxiety disease Diseases 0.000 claims description 4
- 201000001320 Atherosclerosis Diseases 0.000 claims description 4
- 206010003658 Atrial Fibrillation Diseases 0.000 claims description 4
- 208000020925 Bipolar disease Diseases 0.000 claims description 4
- 206010058019 Cancer Pain Diseases 0.000 claims description 4
- 208000024172 Cardiovascular disease Diseases 0.000 claims description 4
- 208000000094 Chronic Pain Diseases 0.000 claims description 4
- 206010009900 Colitis ulcerative Diseases 0.000 claims description 4
- 208000011231 Crohn disease Diseases 0.000 claims description 4
- 208000032131 Diabetic Neuropathies Diseases 0.000 claims description 4
- 206010015150 Erythema Diseases 0.000 claims description 4
- 241000266331 Eugenia Species 0.000 claims description 4
- 208000001640 Fibromyalgia Diseases 0.000 claims description 4
- 206010019233 Headaches Diseases 0.000 claims description 4
- 101000620451 Homo sapiens Leucine-rich glioma-inactivated protein 1 Proteins 0.000 claims description 4
- 206010020844 Hyperthermia malignant Diseases 0.000 claims description 4
- 206010065390 Inflammatory pain Diseases 0.000 claims description 4
- 208000007914 Labor Pain Diseases 0.000 claims description 4
- 208000035945 Labour pain Diseases 0.000 claims description 4
- 102100022275 Leucine-rich glioma-inactivated protein 1 Human genes 0.000 claims description 4
- 208000026709 Liddle syndrome Diseases 0.000 claims description 4
- 208000018717 Malignant hyperthermia of anesthesia Diseases 0.000 claims description 4
- 208000019695 Migraine disease Diseases 0.000 claims description 4
- 206010028372 Muscular weakness Diseases 0.000 claims description 4
- 206010061533 Myotonia Diseases 0.000 claims description 4
- 208000000693 Neurogenic Urinary Bladder Diseases 0.000 claims description 4
- 206010029279 Neurogenic bladder Diseases 0.000 claims description 4
- 208000012075 Paroxysmal dystonia Diseases 0.000 claims description 4
- 208000010886 Peripheral nerve injury Diseases 0.000 claims description 4
- 208000004983 Phantom Limb Diseases 0.000 claims description 4
- 206010056238 Phantom pain Diseases 0.000 claims description 4
- 206010036376 Postherpetic Neuralgia Diseases 0.000 claims description 4
- 208000004550 Postoperative Pain Diseases 0.000 claims description 4
- 208000003251 Pruritus Diseases 0.000 claims description 4
- 206010037113 Pseudoaldosteronism Diseases 0.000 claims description 4
- 208000005793 Restless legs syndrome Diseases 0.000 claims description 4
- 206010039020 Rhabdomyolysis Diseases 0.000 claims description 4
- 206010040744 Sinus headache Diseases 0.000 claims description 4
- 208000006011 Stroke Diseases 0.000 claims description 4
- 208000001871 Tachycardia Diseases 0.000 claims description 4
- 206010057040 Temperature intolerance Diseases 0.000 claims description 4
- 206010043269 Tension headache Diseases 0.000 claims description 4
- 208000008548 Tension-Type Headache Diseases 0.000 claims description 4
- 201000006704 Ulcerative Colitis Diseases 0.000 claims description 4
- 230000036506 anxiety Effects 0.000 claims description 4
- 206010003119 arrhythmia Diseases 0.000 claims description 4
- 230000006793 arrhythmia Effects 0.000 claims description 4
- 208000028683 bipolar I disease Diseases 0.000 claims description 4
- 208000025307 bipolar depression Diseases 0.000 claims description 4
- 210000004027 cell Anatomy 0.000 claims description 4
- 238000002512 chemotherapy Methods 0.000 claims description 4
- 230000035606 childbirth Effects 0.000 claims description 4
- 208000010118 dystonia Diseases 0.000 claims description 4
- 231100000321 erythema Toxicity 0.000 claims description 4
- 230000008543 heat sensitivity Effects 0.000 claims description 4
- 208000003532 hypothyroidism Diseases 0.000 claims description 4
- 230000002989 hypothyroidism Effects 0.000 claims description 4
- 208000002551 irritable bowel syndrome Diseases 0.000 claims description 4
- 230000000302 ischemic effect Effects 0.000 claims description 4
- 201000007004 malignant hyperthermia Diseases 0.000 claims description 4
- 206010027599 migraine Diseases 0.000 claims description 4
- 230000036473 myasthenia Effects 0.000 claims description 4
- 208000004296 neuralgia Diseases 0.000 claims description 4
- 208000021722 neuropathic pain Diseases 0.000 claims description 4
- 201000001119 neuropathy Diseases 0.000 claims description 4
- 230000007823 neuropathy Effects 0.000 claims description 4
- 201000008482 osteoarthritis Diseases 0.000 claims description 4
- 208000019865 paroxysmal extreme pain disease Diseases 0.000 claims description 4
- 230000002085 persistent effect Effects 0.000 claims description 4
- 208000020016 psychiatric disease Diseases 0.000 claims description 4
- 208000023504 respiratory system disease Diseases 0.000 claims description 4
- 206010039073 rheumatoid arthritis Diseases 0.000 claims description 4
- 201000000306 sarcoidosis Diseases 0.000 claims description 4
- 201000000980 schizophrenia Diseases 0.000 claims description 4
- 208000011580 syndromic disease Diseases 0.000 claims description 4
- 230000001225 therapeutic effect Effects 0.000 claims description 4
- 208000004371 toothache Diseases 0.000 claims description 4
- 239000003053 toxin Substances 0.000 claims description 4
- 231100000765 toxin Toxicity 0.000 claims description 4
- 230000000472 traumatic effect Effects 0.000 claims description 4
- 206010044652 trigeminal neuralgia Diseases 0.000 claims description 4
- 208000003663 ventricular fibrillation Diseases 0.000 claims description 4
- 208000009935 visceral pain Diseases 0.000 claims description 4
- 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
- ZSZLWLTYVQJWCE-ZFWWWQNUSA-N C1CN(C[C@H]([C@@H]1C2=CC=C(C=C2)Cl)COC3=CC(=C(C=C3F)S(=O)(=O)NC4=NC=NS4)F)C(=O)O Chemical compound C1CN(C[C@H]([C@@H]1C2=CC=C(C=C2)Cl)COC3=CC(=C(C=C3F)S(=O)(=O)NC4=NC=NS4)F)C(=O)O ZSZLWLTYVQJWCE-ZFWWWQNUSA-N 0.000 claims description 2
- 208000032170 Congenital Abnormalities Diseases 0.000 claims description 2
- 206010011732 Cyst Diseases 0.000 claims description 2
- 201000003883 Cystic fibrosis Diseases 0.000 claims description 2
- 206010061619 Deformity Diseases 0.000 claims description 2
- 206010016654 Fibrosis Diseases 0.000 claims description 2
- 208000012642 Sexual Trauma Diseases 0.000 claims description 2
- 206010049447 Tachyarrhythmia Diseases 0.000 claims description 2
- 206010003246 arthritis Diseases 0.000 claims description 2
- 208000031513 cyst Diseases 0.000 claims description 2
- 230000004761 fibrosis Effects 0.000 claims description 2
- 208000014674 injury Diseases 0.000 claims description 2
- 210000004962 mammalian cell Anatomy 0.000 claims description 2
- 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
- 230000000324 neuroprotective effect Effects 0.000 claims description 2
- 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
- 230000005764 inhibitory process Effects 0.000 claims 3
- 230000001419 dependent effect Effects 0.000 claims 2
- 230000004907 flux Effects 0.000 claims 2
- 208000005392 Spasm Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 238000013160 medical therapy Methods 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 230000001105 regulatory effect Effects 0.000 claims 1
- 238000000034 method Methods 0.000 description 26
- 230000002401 inhibitory effect Effects 0.000 description 2
- 239000002904 solvent Substances 0.000 description 2
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 150000003456 sulfonamides Chemical class 0.000 description 1
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 |
|---|---|
| JP2014532640A JP2014532640A (ja) | 2014-12-08 |
| JP2014532640A5 true JP2014532640A5 (OSRAM) | 2015-12-17 |
| JP6014154B2 JP6014154B2 (ja) | 2016-10-25 |
Family
ID=48191457
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014537806A Expired - Fee Related JP6014154B2 (ja) | 2011-10-31 | 2012-10-30 | ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US9630929B2 (OSRAM) |
| EP (1) | EP2773637B1 (OSRAM) |
| JP (1) | JP6014154B2 (OSRAM) |
| KR (1) | KR20140091022A (OSRAM) |
| CN (1) | CN104024251B (OSRAM) |
| BR (1) | BR112014010271A2 (OSRAM) |
| CA (1) | CA2853439A1 (OSRAM) |
| ES (1) | ES2586213T3 (OSRAM) |
| MX (1) | MX2014005297A (OSRAM) |
| RU (1) | RU2014121984A (OSRAM) |
| WO (1) | WO2013064983A1 (OSRAM) |
Families Citing this family (39)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8933236B2 (en) | 2012-05-22 | 2015-01-13 | Xenon Pharmaceuticals Inc. | N-substituted benzamides and methods of use thereof |
| WO2013064984A1 (en) | 2011-10-31 | 2013-05-10 | Xenon Pharmaceuticals Inc. | Biaryl ether sulfonamides and their use as therapeutic agents |
| JP6014154B2 (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． | ベンゼンスルホンアミド化合物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 |
| BR112015000187A2 (pt) | 2012-07-06 | 2017-06-27 | Genentech Inc | benzamidas substituídas com n e métodos de uso das mesmas |
| BR112015008987A2 (pt) | 2012-10-26 | 2017-07-04 | Merck Sharp & Dohme | composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso de uma composição farmacêutica |
| WO2014142221A1 (ja) * | 2013-03-14 | 2014-09-18 | 第一三共株式会社 | 呼吸器疾患用薬 |
| KR20150131233A (ko) | 2013-03-14 | 2015-11-24 | 제넨테크, 인크. | 치환된 트리아졸로피리딘 및 이의 사용 방법 |
| US9493429B2 (en) | 2013-03-15 | 2016-11-15 | Genentech, Inc. | Substituted benzoxazoles and methods of use thereof |
| 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 |
| WO2016007534A1 (en) | 2014-07-07 | 2016-01-14 | Genentech, Inc. | Therapeutic compounds and methods of use thereof |
| EP3297989A1 (en) | 2015-05-22 | 2018-03-28 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| CN108137477A (zh) | 2015-08-27 | 2018-06-08 | 基因泰克公司 | 治疗化合物及其使用方法 |
| JP6898310B2 (ja) * | 2015-09-02 | 2021-07-07 | トレベナ・インコーポレイテッドＴｒｅｖｅｎａ， Ｉｎｃ． | ６員アザヘテロ環を含有するデルタ−オピオイド受容体調節化合物、同化合物を使用する方法、および同化合物を作る方法 |
| 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 |
| TWI720032B (zh) * | 2015-10-09 | 2021-03-01 | 比利時商葛萊伯格有限公司 | Ｎ－磺醯化吡唑并﹝３，４－ｂ﹞吡啶－６－甲醯胺及其使用方法 |
| BR112018008448A2 (pt) * | 2015-11-06 | 2018-11-06 | Daiichi Sankyo Company, Limited | ?método para produzir um composto? |
| EP3380466A1 (en) | 2015-11-25 | 2018-10-03 | Genentech, Inc. | Substituted benzamides useful as sodium channel blockers |
| SG11201804936UA (en) | 2015-12-18 | 2018-07-30 | Merck Sharp & Dohme | Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels |
| US10766858B2 (en) | 2016-03-30 | 2020-09-08 | Genentech, Inc. | Substituted benzamides and methods of use thereof |
| CN109526219B (zh) * | 2016-05-20 | 2021-03-12 | 泽农医药公司 | 苯磺酰胺及其作为治疗剂的用途 |
| MX388175B (es) * | 2016-10-17 | 2025-03-19 | Genentech Inc | Compuestos terapéuticos y métodos para utilizarlos |
| ES2897998T3 (es) * | 2016-10-27 | 2022-03-03 | Bristol Myers Squibb Co | Inhibidores de la acilsulfonamida del NaV1.7 |
| SG10201912372XA (en) * | 2016-12-09 | 2020-02-27 | Xenon Pharmaceuticals Inc | Benzenesulfonamide compounds and their use as therapeutic agents |
| EP3582783B1 (en) | 2017-02-17 | 2023-06-07 | Trevena, Inc. | 7-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| CA3052480A1 (en) | 2017-02-17 | 2018-08-23 | Trevena, Inc. | 5-membered aza-heterocyclic containing delta-opioid receptor modulating compounds, methods of using and making the same |
| EP3601273B1 (en) | 2017-03-24 | 2021-12-01 | Genentech, Inc. | 4-piperidin-n-(pyrimidin-4-yl)chroman-7-sulfonamide derivatives as sodium channel inhibitors |
| CN112041313A (zh) | 2018-02-26 | 2020-12-04 | 基因泰克公司 | 吡啶-磺酰胺化合物及其针对疼痛和相关疾患的用途 |
| JP2021519788A (ja) | 2018-03-30 | 2021-08-12 | エフ．ホフマン−ラ ロシュ アーゲーＦ． Ｈｏｆｆｍａｎｎ−Ｌａ Ｒｏｃｈｅ Ａｋｔｉｅｎｇｅｓｅｌｌｓｃｈａｆｔ | ナトリウムチャネル阻害剤としての縮合環ヒドロピリド化合物 |
| 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 |
| UA127024C2 (uk) * | 2018-06-13 | 2023-03-15 | Ксенон Фармасьютікалз Інк. | Бензолсульфонамідні сполуки та їх застосування як терапевтичних агентів |
| WO2020047312A1 (en) | 2018-08-31 | 2020-03-05 | Xenon Pharmaceuticals Inc. | Heteroaryl-substituted sulfonamide compounds and their use as sodium channel inhibitors |
| PE20211066A1 (es) | 2018-08-31 | 2021-06-09 | Xenon Pharmaceuticals Inc | Compuestos de sulfonamida sustituidos con heteroarilo y su uso como agentes terapeuticos |
| WO2020117626A1 (en) | 2018-12-05 | 2020-06-11 | Merck Sharp & Dohme Corp. | 4-amino or 4-alkoxy-substituted aryl sulfonamide compounds with selective activity in voltage-gated 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 |
| WO2024040235A1 (en) * | 2022-08-19 | 2024-02-22 | Maze Therapeutics, Inc. | Apol1 inhibitors and methods of use |
| AR133184A1 (es) * | 2023-07-07 | 2025-09-03 | 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 |
| AU1625192A (en) | 1991-05-31 | 1992-12-03 | Zeneca Limited | 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 |
| WO1996006837A1 (en) | 1994-08-30 | 1996-03-07 | Sankyo Company, Limited | Isoxazoles |
| US5753653A (en) | 1995-12-08 | 1998-05-19 | Agouron Pharmaceuticals, Inc. | Metalloproteinase inhibitors, pharmaceutical compositions containing them and their pharmaceutical uses |
| JP2001524124A (ja) | 1997-05-07 | 2001-11-27 | ガレン（ケミカルズ）リミティド | テストステロンおよびテストステロン前駆体の投与のための膣内薬物送達用具 |
| GB9828442D0 (en) | 1998-12-24 | 1999-02-17 | Karobio Ab | Novel thyroid receptor ligands and method II |
| US8933236B2 (en) | 2012-05-22 | 2015-01-13 | Xenon Pharmaceuticals Inc. | N-substituted benzamides and methods of use thereof |
| 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 |
| CN1688580A (zh) | 2002-08-08 | 2005-10-26 | 记忆药物公司 | 作为磷酸二酯酶4抑制剂的2－三氟甲基－6－氨基嘌呤衍生物 |
| PE20040801A1 (es) | 2002-12-12 | 2004-11-25 | Hoffmann La Roche | Derivados de pirazina y piridina 5-sustituidos como activadores de glucoquinasa |
| AU2004230316A1 (en) | 2003-04-15 | 2004-10-28 | Pfizer Inc. | Alpha substituted carboxylic acid as PPAR modulators |
| CA2539227A1 (en) | 2003-08-08 | 2005-02-17 | Vertex Pharmaceuticals Incorporated | Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain |
| ZA200601942B (en) * | 2003-08-08 | 2007-05-30 | Vertex Pharma | Heteroarylaminosulfonylphenyl derivatives for use as sodium or calcium channel blockers in the treatment of pain |
| WO2005032488A2 (en) | 2003-10-03 | 2005-04-14 | Portola Pharmaceuticals, Inc. | 2,4-dioxo-3-quinazolinylaryl sulfonylureas |
| 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 |
| AU2005272786B2 (en) | 2004-08-12 | 2011-12-22 | Amgen Inc. | Bisaryl-sulfonamides |
| WO2006039212A2 (en) | 2004-09-29 | 2006-04-13 | Portola Pharmaceuticals, Inc. | Substituted 2h-1,3-benzoxazin-4(3h)-ones |
| 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 |
| WO2007030582A2 (en) | 2005-09-09 | 2007-03-15 | Bristol-Myers Squibb Company | Acyclic ikur inhibitors |
| 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 |
| KR20080109918A (ko) | 2006-04-11 | 2008-12-17 | 버텍스 파마슈티칼스 인코포레이티드 | 전압 개폐 나트륨 채널의 억제제로서 유용한 조성물 |
| ATE542818T1 (de) | 2006-10-11 | 2012-02-15 | Amgen Inc | Imidazo- und triazolopyridinverbindungen und verfahren zu deren anwendung |
| JP2010532312A (ja) | 2007-01-30 | 2010-10-07 | バイオジェン・アイデック・エムエイ・インコーポレイテッド | １−ｈ−ピラゾロ（３，４ｂ）ピリミジン誘導体および有糸分裂キナーゼの調節剤としてのその使用 |
| US20080194616A1 (en) | 2007-02-05 | 2008-08-14 | Xenon Pharmaceuticals Inc. | Pyridopyrimidinone compounds useful in treating sodium channel-mediated diseases or conditions |
| JP5361857B2 (ja) | 2007-03-23 | 2013-12-04 | ファイザー・リミテッド | イオンチャネルの阻害剤 |
| EP2158183A2 (en) | 2007-05-25 | 2010-03-03 | Vertex Pharmaceuticals Incorporated | Ion channel modulators and methods of use |
| WO2008149965A1 (ja) | 2007-06-07 | 2008-12-11 | Astellas Pharma Inc. | ピリドン化合物 |
| 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 |
| CA2693588C (en) * | 2007-07-13 | 2015-11-17 | Icagen, Inc. | Sodium channel inhibitors |
| JPWO2009022731A1 (ja) * | 2007-08-10 | 2010-11-18 | 日本ケミファ株式会社 | Ｐ２ｘ４受容体拮抗剤 |
| GB0720390D0 (en) | 2007-10-18 | 2007-11-28 | Prosidion Ltd | G-Protein coupled receptor agonists |
| JP2011507910A (ja) | 2007-12-21 | 2011-03-10 | ユニバーシティー オブ ロチェスター | 真核生物の寿命を変更するための方法 |
| KR20110027648A (ko) | 2008-06-23 | 2011-03-16 | 아스테라스 세이야쿠 가부시키가이샤 | 술폰아미드 화합물 또는 이의 염 |
| 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 |
| CN102348697B (zh) | 2009-01-12 | 2014-12-10 | 辉瑞股份有限公司 | 磺酰胺衍生物 |
| NZ598942A (en) | 2009-07-27 | 2014-02-28 | Gilead Sciences Inc | Fused heterocyclic compounds as ion channel modulators |
| US8809380B2 (en) | 2009-08-04 | 2014-08-19 | Raqualia Pharma Inc. | Picolinamide derivatives as TTX-S blockers |
| WO2011037192A1 (ja) | 2009-09-25 | 2011-03-31 | アステラス製薬株式会社 | 置換アミド化合物 |
| 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 |
| BR112012019529A2 (pt) | 2010-02-12 | 2019-09-24 | N30 Pharmaceuticals Llc | inibidores de d-nitrosoglutationa redutase |
| WO2011153588A1 (en) | 2010-06-10 | 2011-12-15 | Biota Scientific Management Pty Ltd | Viral polymerase inhibitors |
| EP2588186A1 (en) | 2010-06-30 | 2013-05-08 | Cardiac Pacemakers, Inc. | 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 |
| JP5830534B2 (ja) * | 2010-07-09 | 2015-12-09 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化合物 |
| ES2532356T3 (es) | 2010-07-09 | 2015-03-26 | Pfizer Limited | N-sulfonilbenzamidas como inhibidores de los canales de sodio dependientes de voltaje |
| JP5860045B2 (ja) | 2010-07-09 | 2016-02-16 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | 化合物 |
| ES2532357T3 (es) | 2010-07-12 | 2015-03-26 | Pfizer Limited | Derivados de sulfonamida como inhibidores de Nav1.7 para el tratamiento del dolor |
| CA2800971A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | Chemical compounds |
| US8772343B2 (en) | 2010-07-12 | 2014-07-08 | Pfizer Limited | Chemical compounds |
| US9096500B2 (en) | 2010-07-12 | 2015-08-04 | Pfizer Limited | Acyl sulfonamide compounds |
| WO2012007861A1 (en) | 2010-07-12 | 2012-01-19 | Pfizer Limited | N-sulfonylbenzamide derivatives useful as voltage gated sodium channel inhibitors |
| US9120752B2 (en) | 2010-07-16 | 2015-09-01 | Purdue Pharma, L.P. | Pyridine compounds as sodium channel blockers |
| HUE027256T2 (en) | 2010-09-13 | 2016-08-29 | Novartis Ag | Triazine-oxadiazoles |
| WO2012039657A1 (en) | 2010-09-22 | 2012-03-29 | Astrazeneca Ab | Novel chromane compound for the treatment of pain disorders |
| JP2014500303A (ja) | 2010-12-22 | 2014-01-09 | 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置換ピリジン |
| WO2012095781A1 (en) | 2011-01-13 | 2012-07-19 | Pfizer Limited | Indazole derivatives as sodium channel inhibitors |
| TW201604196A (zh) | 2011-02-02 | 2016-02-01 | 維泰克斯製藥公司 | 作為離子通道調節劑之吡咯并吡－螺環哌啶醯胺 |
| CA2844799A1 (en) | 2011-08-17 | 2013-02-21 | Amgen Inc. | Heteroaryl sodium channel inhibitors |
| EP2766018A4 (en) | 2011-10-13 | 2015-02-25 | Univ Case Western Reserve | RXR AGONIST COMPOUNDS AND METHOD THEREFOR |
| RU2014121489A (ru) | 2011-10-28 | 2015-12-10 | Мерк Шарп И Доум Корп. | Соединения бензоксазолинона с селективной активностью в отношении потенциалзависимых натриевых каналов |
| JP6014154B2 (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． | ベンゼンスルホンアミド化合物および治療剤としてのそれらの使用 |
| WO2013064984A1 (en) | 2011-10-31 | 2013-05-10 | Xenon Pharmaceuticals Inc. | Biaryl ether sulfonamides and their use as therapeutic agents |
| US9133131B2 (en) | 2011-11-15 | 2015-09-15 | Purdue Pharma L.P. | Pyrimidine diol amides as sodium channel blockers |
| WO2013086229A1 (en) | 2011-12-07 | 2013-06-13 | Amgen Inc. | Bicyclic aryl and heteroaryl sodium channel inhibitors |
| ES2593533T3 (es) | 2011-12-15 | 2016-12-09 | Pfizer Limited | Derivados de sulfonamida |
| JP6067031B2 (ja) | 2012-01-04 | 2017-01-25 | ファイザー・リミテッドＰｆｉｚｅｒ Ｌｉｍｉｔｅｄ | Ｎ−アミノスルホニルベンズアミド |
| 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 |
| BR112015000187A2 (pt) | 2012-07-06 | 2017-06-27 | Genentech Inc | benzamidas substituídas com n e métodos de uso das mesmas |
| WO2014014050A1 (ja) | 2012-07-19 | 2014-01-23 | 大日本住友製薬株式会社 | １－（シクロアルキルカルボニル）プロリン誘導体 |
| JP2015535251A (ja) | 2012-10-26 | 2015-12-10 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | 電位作動型ナトリウムチャネルにおいて選択的活性を有するベンゾオキサゾリノン化合物 |
| BR112015008987A2 (pt) | 2012-10-26 | 2017-07-04 | Merck Sharp & Dohme | composto ou um sal farmaceuticamente aceitável do mesmo, composição farmacêutica, e, uso de uma composição farmacêutica |
| EP2935257B1 (en) | 2012-12-20 | 2018-02-07 | Purdue Pharma LP | Cyclic sulfonamides as sodium channel blockers |
| ES2857687T3 (es) | 2013-01-31 | 2021-09-29 | Vertex Pharma | Piridona amidas como moduladores de los canales de sodio |
| US20140296266A1 (en) | 2013-03-01 | 2014-10-02 | Gilead Sciences, Inc. | Therapeutic compounds |
| KR20150131233A (ko) | 2013-03-14 | 2015-11-24 | 제넨테크, 인크. | 치환된 트리아졸로피리딘 및 이의 사용 방법 |
| RU2669367C2 (ru) | 2013-03-15 | 2018-10-11 | Хромоселл Корпорейшн | Модуляторы натриевого канала для лечения боли |
| US9493429B2 (en) | 2013-03-15 | 2016-11-15 | Genentech, Inc. | Substituted benzoxazoles and methods of use thereof |
| WO2015051043A1 (en) | 2013-10-01 | 2015-04-09 | 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 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 RU RU2014121984/04A patent/RU2014121984A/ru not_active Application Discontinuation
- 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 EP EP12845774.4A patent/EP2773637B1/en not_active Not-in-force
- 2012-10-30 WO PCT/IB2012/056031 patent/WO2013064983A1/en not_active Ceased
- 2012-10-30 ES ES12845774.4T patent/ES2586213T3/es active Active
- 2012-10-30 US US14/355,552 patent/US9630929B2/en not_active Expired - Fee Related
- 2012-10-30 MX MX2014005297A patent/MX2014005297A/es not_active Application Discontinuation
- 2012-10-30 KR KR1020147014213A patent/KR20140091022A/ko not_active Withdrawn
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| JP2014532640A5 (OSRAM) | ||
| RU2014121984A (ru) | Бензолсульфонамидные соединения и их применение в качестве терапевтических средств | |
| JP7150903B2 (ja) | Ｂ型肝炎ウイルスコアタンパク質モジュレーター | |
| US11970481B1 (en) | Substituted pyridine derivatives as SARM1 inhibitors | |
| US10995064B2 (en) | Sulfamoyl-arylamides and the use thereof as medicaments for the treatment of hepatitis B | |
| JP6697074B2 (ja) | ヒストン脱アセチル化酵素６阻害剤としてのオキサジアゾールアミン誘導体化合物及びこれを含有する薬剤学的組成物 | |
| TWI583670B (zh) | Partially saturated nitrogenous heterocyclic compounds | |
| KR100862879B1 (ko) | Ｈｉｖ 인테그라제의 ｎ-치환된 하이드록시피리미디논 카복스아미드 억제제 | |
| TWI471132B (zh) | ２－吡啶酮化合物 | |
| US20180141905A1 (en) | Sulphamoylpyrrolamide derivatives and the use thereof as medicaments for the treatment of hepatitis b | |
| JP2004502670A5 (OSRAM) | ||
| WO2011035900A1 (en) | New thiadiazole derivatives | |
| CZ2004627A3 (cs) | Dibenzylaminové sloučeniny a jejich farmaceutické použití | |
| JP2025102975A (ja) | Ｋｃｎｔ１阻害剤および使用する方法 | |
| JP2008513515A5 (OSRAM) | ||
| JP2010506918A5 (OSRAM) | ||
| TW201006804A (en) | Triazole derivative or salt thereof | |
| RU2018104868A (ru) | 2-амино-3-фтор-3-(фторметил)-6-метил-6-фенил-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 | |
| WO2012036278A1 (ja) | グリシントランスポーター阻害物質 | |
| RU2012122056A (ru) | Ингибиторы фермента диацилглицерин-о-ацилтрансферазы типа 1 | |
| HRP20161702T1 (hr) | Novi derivati pirazina | |
| WO2006011631A2 (en) | Thiazole derivatives having vap-1 inhibitory activity | |
| KR20190078646A (ko) | 디아실글리세리드 o-아실트랜스퍼라제 2의 억제제로서 유용한 인다졸 유도체 | |
| JP2021501183A5 (OSRAM) | ||
| JP2004516295A5 (OSRAM) |