JP2017511794A5 - - Google Patents
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- JP2017511794A5 JP2017511794A5 JP2016551246A JP2016551246A JP2017511794A5 JP 2017511794 A5 JP2017511794 A5 JP 2017511794A5 JP 2016551246 A JP2016551246 A JP 2016551246A JP 2016551246 A JP2016551246 A JP 2016551246A JP 2017511794 A5 JP2017511794 A5 JP 2017511794A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- alkyl
- amino
- compound
- alkoxy
- 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 66
- 150000001875 compounds Chemical class 0.000 claims 42
- 125000000623 heterocyclic group Chemical group 0.000 claims 33
- 125000003545 alkoxy group Chemical group 0.000 claims 27
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 23
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 claims 22
- -1 —S (O) m —R f Chemical group 0.000 claims 19
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 18
- 125000000547 substituted alkyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 125000001072 heteroaryl group Chemical group 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 150000003857 carboxamides Chemical class 0.000 claims 11
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 11
- 150000001204 N-oxides Chemical class 0.000 claims 9
- 229910052757 nitrogen Inorganic materials 0.000 claims 9
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 9
- 150000003839 salts Chemical class 0.000 claims 9
- 239000012453 solvate Substances 0.000 claims 9
- 208000002193 Pain Diseases 0.000 claims 8
- 125000001188 haloalkyl group Chemical group 0.000 claims 7
- 229940124530 sulfonamide Drugs 0.000 claims 7
- 150000003456 sulfonamides Chemical class 0.000 claims 7
- 125000000753 cycloalkyl group Chemical group 0.000 claims 6
- 125000004438 haloalkoxy group Chemical group 0.000 claims 6
- 230000036407 pain Effects 0.000 claims 6
- 125000003107 substituted aryl group Chemical group 0.000 claims 6
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 5
- 125000003118 aryl group Chemical group 0.000 claims 4
- 125000000472 sulfonyl group Chemical group *S(*)(=O)=O 0.000 claims 4
- XSQUKJJJFZCRTK-UHFFFAOYSA-N Urea Chemical compound NC(N)=O XSQUKJJJFZCRTK-UHFFFAOYSA-N 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 125000003396 thiol group Chemical group [H]S* 0.000 claims 3
- 125000005518 carboxamido group Chemical group 0.000 claims 2
- 239000003085 diluting agent Substances 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- 229920006395 saturated elastomer Polymers 0.000 claims 2
- UAOUIVVJBYDFKD-XKCDOFEDSA-N (1R,9R,10S,11R,12R,15S,18S,21R)-10,11,21-trihydroxy-8,8-dimethyl-14-methylidene-4-(prop-2-enylamino)-20-oxa-5-thia-3-azahexacyclo[9.7.2.112,15.01,9.02,6.012,18]henicosa-2(6),3-dien-13-one Chemical compound C([C@@H]1[C@@H](O)[C@@]23C(C1=C)=O)C[C@H]2[C@]12C(N=C(NCC=C)S4)=C4CC(C)(C)[C@H]1[C@H](O)[C@]3(O)OC2 UAOUIVVJBYDFKD-XKCDOFEDSA-N 0.000 claims 1
- ABJSOROVZZKJGI-OCYUSGCXSA-N (1r,2r,4r)-2-(4-bromophenyl)-n-[(4-chlorophenyl)-(2-fluoropyridin-4-yl)methyl]-4-morpholin-4-ylcyclohexane-1-carboxamide Chemical compound C1=NC(F)=CC(C(NC(=O)[C@H]2[C@@H](C[C@@H](CC2)N2CCOCC2)C=2C=CC(Br)=CC=2)C=2C=CC(Cl)=CC=2)=C1 ABJSOROVZZKJGI-OCYUSGCXSA-N 0.000 claims 1
- WWTBZEKOSBFBEM-SPWPXUSOSA-N (2s)-2-[[2-benzyl-3-[hydroxy-[(1r)-2-phenyl-1-(phenylmethoxycarbonylamino)ethyl]phosphoryl]propanoyl]amino]-3-(1h-indol-3-yl)propanoic acid Chemical compound N([C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)O)C(=O)C(CP(O)(=O)[C@H](CC=1C=CC=CC=1)NC(=O)OCC=1C=CC=CC=1)CC1=CC=CC=C1 WWTBZEKOSBFBEM-SPWPXUSOSA-N 0.000 claims 1
- STBLNCCBQMHSRC-BATDWUPUSA-N (2s)-n-[(3s,4s)-5-acetyl-7-cyano-4-methyl-1-[(2-methylnaphthalen-1-yl)methyl]-2-oxo-3,4-dihydro-1,5-benzodiazepin-3-yl]-2-(methylamino)propanamide Chemical compound O=C1[C@@H](NC(=O)[C@H](C)NC)[C@H](C)N(C(C)=O)C2=CC(C#N)=CC=C2N1CC1=C(C)C=CC2=CC=CC=C12 STBLNCCBQMHSRC-BATDWUPUSA-N 0.000 claims 1
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 claims 1
- KQZLRWGGWXJPOS-NLFPWZOASA-N 1-[(1R)-1-(2,4-dichlorophenyl)ethyl]-6-[(4S,5R)-4-[(2S)-2-(hydroxymethyl)pyrrolidin-1-yl]-5-methylcyclohexen-1-yl]pyrazolo[3,4-b]pyrazine-3-carbonitrile Chemical compound ClC1=C(C=CC(=C1)Cl)[C@@H](C)N1N=C(C=2C1=NC(=CN=2)C1=CC[C@@H]([C@@H](C1)C)N1[C@@H](CCC1)CO)C#N KQZLRWGGWXJPOS-NLFPWZOASA-N 0.000 claims 1
- RGICCULPCWNRAB-UHFFFAOYSA-N 2-[2-(2-hexoxyethoxy)ethoxy]ethanol Chemical compound CCCCCCOCCOCCOCCO RGICCULPCWNRAB-UHFFFAOYSA-N 0.000 claims 1
- YSUIQYOGTINQIN-UZFYAQMZSA-N 2-amino-9-[(1S,6R,8R,9S,10R,15R,17R,18R)-8-(6-aminopurin-9-yl)-9,18-difluoro-3,12-dihydroxy-3,12-bis(sulfanylidene)-2,4,7,11,13,16-hexaoxa-3lambda5,12lambda5-diphosphatricyclo[13.2.1.06,10]octadecan-17-yl]-1H-purin-6-one Chemical compound NC1=NC2=C(N=CN2[C@@H]2O[C@@H]3COP(S)(=O)O[C@@H]4[C@@H](COP(S)(=O)O[C@@H]2[C@@H]3F)O[C@H]([C@H]4F)N2C=NC3=C2N=CN=C3N)C(=O)N1 YSUIQYOGTINQIN-UZFYAQMZSA-N 0.000 claims 1
- TVTJUIAKQFIXCE-HUKYDQBMSA-N 2-amino-9-[(2R,3S,4S,5R)-4-fluoro-3-hydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-ynyl-1H-purine-6,8-dione Chemical compound NC=1NC(C=2N(C(N(C=2N=1)[C@@H]1O[C@@H]([C@H]([C@H]1O)F)CO)=O)CC#C)=O TVTJUIAKQFIXCE-HUKYDQBMSA-N 0.000 claims 1
- QBWKPGNFQQJGFY-QLFBSQMISA-N 3-[(1r)-1-[(2r,6s)-2,6-dimethylmorpholin-4-yl]ethyl]-n-[6-methyl-3-(1h-pyrazol-4-yl)imidazo[1,2-a]pyrazin-8-yl]-1,2-thiazol-5-amine Chemical compound N1([C@H](C)C2=NSC(NC=3C4=NC=C(N4C=C(C)N=3)C3=CNN=C3)=C2)C[C@H](C)O[C@H](C)C1 QBWKPGNFQQJGFY-QLFBSQMISA-N 0.000 claims 1
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 1
- BKZXMCAIWWDHSQ-JOCHJYFZSA-N 6-[(1S)-1,2-dihydroxyethyl]-4-[5-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-carboxamide Chemical compound O[C@H](CO)C1=CC(=CC(=N1)C(=O)N)N1CC2=CC=CC(=C2CC1)C1=CC=C(C=C1)C(F)(F)F BKZXMCAIWWDHSQ-JOCHJYFZSA-N 0.000 claims 1
- PDKJRCDTWHBSKE-UHFFFAOYSA-N 6-[5-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-carboxamide Chemical compound FC(C1=CC=C(C=C1)C1=C2CCN(CC2=CC=C1)C1=CC=CC(=N1)C(=O)N)(F)F PDKJRCDTWHBSKE-UHFFFAOYSA-N 0.000 claims 1
- HHIDIFCNHJJOIJ-AWEZNQCLSA-N 6-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-2-(5-cyclohexyl-3,4-dihydro-1H-isoquinolin-2-yl)pyrimidine-4-carboxamide Chemical compound NC([C@H](C)NC1=CC(=NC(=N1)N1CC2=CC=CC(=C2CC1)C1CCCCC1)C(=O)N)=O HHIDIFCNHJJOIJ-AWEZNQCLSA-N 0.000 claims 1
- ZLMXMGFQERVQES-LBPRGKRZSA-N 6-[[(2S)-1-amino-1-oxopropan-2-yl]amino]-2-[5-[5-(trifluoromethyl)pyridin-2-yl]-3,4-dihydro-1H-isoquinolin-2-yl]pyrimidine-4-carboxamide Chemical compound NC([C@H](C)NC1=CC(=NC(=N1)N1CC2=CC=CC(=C2CC1)C1=NC=C(C=C1)C(F)(F)F)C(=O)N)=O ZLMXMGFQERVQES-LBPRGKRZSA-N 0.000 claims 1
- 208000008822 Ankylosis Diseases 0.000 claims 1
- 206010003591 Ataxia Diseases 0.000 claims 1
- 208000020925 Bipolar disease Diseases 0.000 claims 1
- 102000014914 Carrier Proteins Human genes 0.000 claims 1
- 206010008027 Cerebellar atrophy Diseases 0.000 claims 1
- 208000000094 Chronic Pain Diseases 0.000 claims 1
- 206010010904 Convulsion Diseases 0.000 claims 1
- 206010019196 Head injury Diseases 0.000 claims 1
- 206010065390 Inflammatory pain Diseases 0.000 claims 1
- 206010023198 Joint ankylosis Diseases 0.000 claims 1
- 208000036626 Mental retardation Diseases 0.000 claims 1
- 208000019695 Migraine disease Diseases 0.000 claims 1
- 208000016285 Movement disease Diseases 0.000 claims 1
- SBKIFLXSGDXZHF-UHFFFAOYSA-N N-(1,2,4-thiadiazol-5-yl)-6-[5-[4-(trifluoromethyl)phenyl]-3,4-dihydro-1H-isoquinolin-2-yl]pyridine-2-sulfonamide Chemical compound S1N=CN=C1NS(=O)(=O)C1=NC(=CC=C1)N1CC2=CC=CC(=C2CC1)C1=CC=C(C=C1)C(F)(F)F SBKIFLXSGDXZHF-UHFFFAOYSA-N 0.000 claims 1
- 208000028389 Nerve injury Diseases 0.000 claims 1
- 208000009205 Tinnitus Diseases 0.000 claims 1
- LJOOWESTVASNOG-UFJKPHDISA-N [(1s,3r,4ar,7s,8s,8as)-3-hydroxy-8-[2-[(4r)-4-hydroxy-6-oxooxan-2-yl]ethyl]-7-methyl-1,2,3,4,4a,7,8,8a-octahydronaphthalen-1-yl] (2s)-2-methylbutanoate Chemical compound C([C@H]1[C@@H](C)C=C[C@H]2C[C@@H](O)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)CC1C[C@@H](O)CC(=O)O1 LJOOWESTVASNOG-UFJKPHDISA-N 0.000 claims 1
- 208000005298 acute pain Diseases 0.000 claims 1
- 206010003119 arrhythmia Diseases 0.000 claims 1
- 238000003556 assay Methods 0.000 claims 1
- XRWSZZJLZRKHHD-WVWIJVSJSA-N asunaprevir Chemical compound O=C([C@@H]1C[C@H](CN1C(=O)[C@@H](NC(=O)OC(C)(C)C)C(C)(C)C)OC1=NC=C(C2=CC=C(Cl)C=C21)OC)N[C@]1(C(=O)NS(=O)(=O)C2CC2)C[C@H]1C=C XRWSZZJLZRKHHD-WVWIJVSJSA-N 0.000 claims 1
- KGNDCEVUMONOKF-UGPLYTSKSA-N benzyl n-[(2r)-1-[(2s,4r)-2-[[(2s)-6-amino-1-(1,3-benzoxazol-2-yl)-1,1-dihydroxyhexan-2-yl]carbamoyl]-4-[(4-methylphenyl)methoxy]pyrrolidin-1-yl]-1-oxo-4-phenylbutan-2-yl]carbamate Chemical compound C1=CC(C)=CC=C1CO[C@H]1CN(C(=O)[C@@H](CCC=2C=CC=CC=2)NC(=O)OCC=2C=CC=CC=2)[C@H](C(=O)N[C@@H](CCCCN)C(O)(O)C=2OC3=CC=CC=C3N=2)C1 KGNDCEVUMONOKF-UGPLYTSKSA-N 0.000 claims 1
- 108091008324 binding proteins Proteins 0.000 claims 1
- 208000028683 bipolar I disease Diseases 0.000 claims 1
- 125000001951 carbamoylamino group Chemical group C(N)(=O)N* 0.000 claims 1
- 229940126208 compound 22 Drugs 0.000 claims 1
- 229940125833 compound 23 Drugs 0.000 claims 1
- 229940125961 compound 24 Drugs 0.000 claims 1
- 229940125846 compound 25 Drugs 0.000 claims 1
- 229940125851 compound 27 Drugs 0.000 claims 1
- 229940127204 compound 29 Drugs 0.000 claims 1
- 229940125877 compound 31 Drugs 0.000 claims 1
- 229940125878 compound 36 Drugs 0.000 claims 1
- 230000036461 convulsion Effects 0.000 claims 1
- 125000000596 cyclohexenyl group Chemical group C1(=CCCCC1)* 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 208000014617 hemorrhoid Diseases 0.000 claims 1
- 208000028867 ischemia Diseases 0.000 claims 1
- 230000002197 limbic effect Effects 0.000 claims 1
- 238000002690 local anesthesia Methods 0.000 claims 1
- 239000012528 membrane Substances 0.000 claims 1
- 206010027599 migraine Diseases 0.000 claims 1
- 210000003205 muscle Anatomy 0.000 claims 1
- 230000008764 nerve damage Effects 0.000 claims 1
- 208000004296 neuralgia Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 208000021722 neuropathic pain Diseases 0.000 claims 1
- 238000009116 palliative therapy Methods 0.000 claims 1
- 230000001314 paroxysmal effect Effects 0.000 claims 1
- 102000004169 proteins and genes Human genes 0.000 claims 1
- 108090000623 proteins and genes Proteins 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 238000000163 radioactive labelling Methods 0.000 claims 1
- 238000012216 screening Methods 0.000 claims 1
- 125000005415 substituted alkoxy group Chemical group 0.000 claims 1
- 231100000886 tinnitus Toxicity 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201461939082P | 2014-02-12 | 2014-02-12 | |
| US61/939,082 | 2014-02-12 | ||
| PCT/US2015/015576 WO2015123398A1 (en) | 2014-02-12 | 2015-02-12 | Isoquinoline derivatives and use thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2017511794A JP2017511794A (ja) | 2017-04-27 |
| JP2017511794A5 true JP2017511794A5 (enExample) | 2017-08-03 |
| JP6556154B2 JP6556154B2 (ja) | 2019-08-07 |
Family
ID=53800620
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2016551246A Active JP6556154B2 (ja) | 2014-02-12 | 2015-02-12 | イソキノリン誘導体及びその使用 |
Country Status (8)
| Country | Link |
|---|---|
| US (2) | US10738026B2 (enExample) |
| EP (1) | EP3105217B1 (enExample) |
| JP (1) | JP6556154B2 (enExample) |
| CN (1) | CN106103422B (enExample) |
| AU (1) | AU2015217185B2 (enExample) |
| CA (1) | CA2939501C (enExample) |
| IL (1) | IL247252B (enExample) |
| WO (1) | WO2015123398A1 (enExample) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10138207B2 (en) | 2012-11-09 | 2018-11-27 | Purdue Pharma, L.P. | Benzomorphan analogs and the use thereof |
| US9120786B2 (en) | 2013-03-04 | 2015-09-01 | Purdue Pharma, L.P. | Triazine carboxamides as sodium channel blockers |
| EP2968307A4 (en) | 2013-03-15 | 2017-01-04 | Purdue Pharma LP | Carboxamide derivatives and use thereof |
| CA2922567A1 (en) | 2013-08-26 | 2015-03-05 | Purdue Pharma L.P. | Azaspiro[4.5]decane derivatives and use thereof |
| US9828348B2 (en) | 2013-11-08 | 2017-11-28 | Purdue Pharma L.P. | Benzimidazole derivatives and use thereof |
| US9834543B2 (en) | 2013-12-23 | 2017-12-05 | Purdue Pharma L.P. | Indazoles and use thereof |
| US9862726B2 (en) | 2013-12-26 | 2018-01-09 | Purdue Pharma L.P. | Opioid receptor modulating oxabicyclo[2.2.2]octane morphinans |
| US9994571B2 (en) | 2013-12-26 | 2018-06-12 | Purdue Pharma L.P. | 10-substituted morphinan hydantoins |
| WO2015097548A1 (en) | 2013-12-26 | 2015-07-02 | Purdue Pharma L.P. | 7-beta-alkyl analogs of orvinols |
| EP3087057A4 (en) | 2013-12-26 | 2017-06-28 | Purdue Pharma LP | Ring-contracted morphinans and the use thereof |
| US10550088B2 (en) | 2013-12-27 | 2020-02-04 | Purdue Pharma L.P. | 6-substituted and 7-substituted morphinan analogs and the use thereof |
| CN106061944A (zh) | 2014-01-24 | 2016-10-26 | 普渡制药公司 | 吡啶类和嘧啶类物质及其用途 |
| EP3148535A4 (en) | 2014-05-27 | 2017-11-29 | Purdue Pharma LP | Spirocyclic morphinans and use thereof |
| MA40171A (fr) | 2014-06-13 | 2017-04-19 | Purdue Pharma Lp | Dérivés d'azamophinan et leur utilisation |
| MA41125A (fr) | 2014-12-05 | 2017-10-10 | Purdue Pharma Lp | Dérivés de 6.7-cyclomorphinane et leur utilisation |
| CA3048357A1 (en) | 2016-12-29 | 2018-07-05 | Minoryx Therapeutics S.L. | Heteroaryl compounds and their use |
| WO2018125716A1 (en) | 2017-01-02 | 2018-07-05 | Purdue Pharma L.P. | Morphinan derivatives and use thereof |
| TWI648265B (zh) * | 2017-03-03 | 2019-01-21 | 國立臺灣大學 | ８－苯基異喹啉及其醫藥組合物用於治療腸躁症候群 |
| US10793551B2 (en) | 2017-10-19 | 2020-10-06 | Effector Therapeutics Inc. | Benzimidazole-indole inhibitors of Mnk1 and Mnk2 |
| CN110372584A (zh) * | 2019-06-25 | 2019-10-25 | 南京普锐达医药科技有限公司 | 一种2,4-二氯-6-氰基嘧啶的合成方法 |
| IL314405A (en) * | 2022-01-18 | 2024-09-01 | Bsense Bio Therapeutics Ltd | Substances affecting the potassium channel and the TRPV1 channel and their uses |
| JP2025503945A (ja) * | 2022-01-28 | 2025-02-06 | オプナ バイオ ソシエテ アノニム | Ｙａｐ／ｔｅａｄ調節およびそれらの適応症のための化合物および方法 |
| WO2024210578A1 (ko) * | 2023-04-05 | 2024-10-10 | 주식회사 바오밥에이바이오 | 헤테로비시클릭 화합물 및 그를 포함하는 약제학적 조성물 |
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2015
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- 2015-02-12 EP EP15748728.1A patent/EP3105217B1/en active Active
- 2015-02-12 WO PCT/US2015/015576 patent/WO2015123398A1/en not_active Ceased
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2020
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