JP2017511794A5 - - Google Patents

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Publication number: JP2017511794A5
Authority: JP; Japan
Prior art keywords: optionally substituted; alkyl; amino; compound; alkoxy
Prior art date: 2015-02-12
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

Application number

JP2016551246A

Other languages

English (en)

Japanese (ja)

Other versions

JP6556154B2 (ja

JP2017511794A (ja

Filing date

2015-02-12

Publication date

2017-08-03

2015-02-12 Application filed filed Critical

2015-02-12 Priority claimed from PCT/US2015/015576 external-priority patent/WO2015123398A1/en

2017-04-27 Publication of JP2017511794A publication Critical patent/JP2017511794A/ja

2017-08-03 Publication of JP2017511794A5 publication Critical patent/JP2017511794A5/ja

2019-08-07 Application granted granted Critical

2019-08-07 Publication of JP6556154B2 publication Critical patent/JP6556154B2/ja

Status Active legal-status Critical Current

2035-02-12 Anticipated expiration legal-status Critical

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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

JP2016551246A 2014-02-12 2015-02-12 イソキノリン誘導体及びその使用 Active JP6556154B2 (ja)

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 (2)	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 (2)
EP (1)	EP3105217B1 (2)
JP (1)	JP6556154B2 (2)
CN (1)	CN106103422B (2)
AU (1)	AU2015217185B2 (2)
CA (1)	CA2939501C (2)
IL (1)	IL247252B (2)
WO (1)	WO2015123398A1 (2)

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