JP2013543883A5 - - Google Patents
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- JP2013543883A5 JP2013543883A5 JP2013540440A JP2013540440A JP2013543883A5 JP 2013543883 A5 JP2013543883 A5 JP 2013543883A5 JP 2013540440 A JP2013540440 A JP 2013540440A JP 2013540440 A JP2013540440 A JP 2013540440A JP 2013543883 A5 JP2013543883 A5 JP 2013543883A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- alkoxy
- halo
- formula
- 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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- 125000000217 alkyl group Chemical group 0.000 claims 419
- 125000003545 alkoxy group Chemical group 0.000 claims 69
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 60
- CYRMSUTZVYGINF-UHFFFAOYSA-N trichlorofluoromethane Chemical compound FC(Cl)(Cl)Cl CYRMSUTZVYGINF-UHFFFAOYSA-N 0.000 claims 36
- 125000005843 halogen group Chemical group 0.000 claims 32
- 239000002904 solvent Substances 0.000 claims 29
- 150000001875 compounds Chemical class 0.000 claims 28
- 125000004093 cyano group Chemical group *C#N 0.000 claims 24
- 229910052739 hydrogen Inorganic materials 0.000 claims 22
- 239000001257 hydrogen Substances 0.000 claims 22
- 229910052760 oxygen Inorganic materials 0.000 claims 18
- 125000005842 heteroatom Chemical group 0.000 claims 17
- 125000001475 halogen functional group Chemical group 0.000 claims 16
- 150000002431 hydrogen Chemical class 0.000 claims 15
- 125000001424 substituent group Chemical group 0.000 claims 15
- 229910052717 sulfur Inorganic materials 0.000 claims 15
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 14
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 12
- 239000003054 catalyst Substances 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 8
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- -1 3,5-dimethoxy-phenyl Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000003342 alkenyl group Chemical group 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 4
- 239000002253 acid Substances 0.000 claims 4
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 239000003638 chemical reducing agent Substances 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 239000003446 ligand Substances 0.000 claims 4
- 238000004519 manufacturing process Methods 0.000 claims 4
- 125000001624 naphthyl group Chemical group 0.000 claims 4
- 125000006239 protecting group Chemical group 0.000 claims 4
- 150000003839 salts Chemical class 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 239000007787 solid Substances 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 108091008794 FGF receptors Proteins 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 125000004429 atom Chemical group 0.000 claims 3
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 2
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims 2
- 150000001204 N-oxides Chemical class 0.000 claims 2
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 125000002619 bicyclic group Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 2
- 239000011777 magnesium Substances 0.000 claims 2
- 229910052749 magnesium Inorganic materials 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- NNFCIKHAZHQZJG-UHFFFAOYSA-N potassium cyanide Chemical compound [K+].N#[C-] NNFCIKHAZHQZJG-UHFFFAOYSA-N 0.000 claims 2
- JCMSXZKRELRJFO-QHCPKHFHSA-N (3s)-3-(3,5-dimethoxyphenyl)-3-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-n-propan-2-ylpropan-1-amine Chemical compound COC1=CC(OC)=CC([C@@H](CCNC(C)C)C=2C=C3N=C(C=NC3=CC=2)C2=CN(C)N=C2)=C1 JCMSXZKRELRJFO-QHCPKHFHSA-N 0.000 claims 1
- JCMSXZKRELRJFO-UHFFFAOYSA-N 3-(3,5-dimethoxyphenyl)-3-[3-(1-methylpyrazol-4-yl)quinoxalin-6-yl]-n-propan-2-ylpropan-1-amine Chemical compound COC1=CC(OC)=CC(C(CCNC(C)C)C=2C=C3N=C(C=NC3=CC=2)C2=CN(C)N=C2)=C1 JCMSXZKRELRJFO-UHFFFAOYSA-N 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 229910052731 fluorine Inorganic materials 0.000 claims 1
- 239000011737 fluorine Substances 0.000 claims 1
- 125000001153 fluoro group Chemical group F* 0.000 claims 1
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000011877 solvent mixture Substances 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 0 C*C(*C)(c1ccccc1)c1cc(*=C(C)C(C(*)=*)=C(C)*)c(*=*)cc1 Chemical compound C*C(*C)(c1ccccc1)c1cc(*=C(C)C(C(*)=*)=C(C)*)c(*=*)cc1 0.000 description 6
- GNKOMWRJUVRGFO-UHFFFAOYSA-N CC(C)Cc1cccc(C(N)=O)c1 Chemical compound CC(C)Cc1cccc(C(N)=O)c1 GNKOMWRJUVRGFO-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US41774410P | 2010-11-29 | 2010-11-29 | |
| GBGB1020179.6A GB201020179D0 (en) | 2010-11-29 | 2010-11-29 | New compounds |
| US61/417,744 | 2010-11-29 | ||
| GB1020179.6 | 2010-11-29 | ||
| PCT/GB2011/052356 WO2012073017A1 (en) | 2010-11-29 | 2011-11-29 | Substituted benzopyrazin derivatives as fgfr kinase inhibitors for the treatment of cancer diseases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2013543883A JP2013543883A (ja) | 2013-12-09 |
| JP2013543883A5 true JP2013543883A5 (enExample) | 2015-01-22 |
| JP5868992B2 JP5868992B2 (ja) | 2016-02-24 |
Family
ID=43500774
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013540440A Active JP5868992B2 (ja) | 2010-11-29 | 2011-11-29 | 癌疾患の治療のためのｆｇｆｒキナーゼ阻害剤としての置換ベンゾピラジン誘導体 |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US9290478B2 (enExample) |
| EP (1) | EP2646432B1 (enExample) |
| JP (1) | JP5868992B2 (enExample) |
| KR (1) | KR101914720B1 (enExample) |
| CN (1) | CN103370314B (enExample) |
| AU (1) | AU2011334624B2 (enExample) |
| BR (1) | BR112013013435B1 (enExample) |
| CA (1) | CA2819009C (enExample) |
| DK (1) | DK2646432T3 (enExample) |
| ES (1) | ES2541493T3 (enExample) |
| GB (1) | GB201020179D0 (enExample) |
| HR (1) | HRP20150692T8 (enExample) |
| HU (1) | HUE025091T2 (enExample) |
| MX (1) | MX2013005897A (enExample) |
| RU (1) | RU2602233C2 (enExample) |
| SI (1) | SI2646432T1 (enExample) |
| SM (1) | SMT201500191B (enExample) |
| WO (1) | WO2012073017A1 (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB201007286D0 (en) | 2010-04-30 | 2010-06-16 | Astex Therapeutics Ltd | New compounds |
| GB201020179D0 (en) | 2010-11-29 | 2011-01-12 | Astex Therapeutics Ltd | New compounds |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| CA2846574C (en) * | 2011-08-26 | 2020-07-07 | Neupharma, Inc. | Quinoxaline sulfonamide derivates for use as kinase inhibitors |
| CN115403531A (zh) | 2011-09-14 | 2022-11-29 | 润新生物公司 | 作为激酶抑制剂的化学实体、组合物及方法 |
| EP2757885B1 (en) | 2011-09-21 | 2017-03-15 | Neupharma, Inc. | Certain chemical entites, compositions, and methods |
| US9249111B2 (en) * | 2011-09-30 | 2016-02-02 | Neupharma, Inc. | Substituted quinoxalines as B-RAF kinase inhibitors |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| WO2013112950A2 (en) | 2012-01-25 | 2013-08-01 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| GB201209613D0 (en) * | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| ES2984771T3 (es) | 2012-06-13 | 2024-10-31 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| WO2014026125A1 (en) | 2012-08-10 | 2014-02-13 | Incyte Corporation | Pyrazine derivatives as fgfr inhibitors |
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| CN104812389B (zh) | 2012-09-24 | 2020-07-17 | 润新生物公司 | 某些化学实体、组合物及方法 |
| EP2916838B1 (en) | 2012-11-12 | 2019-03-13 | Neupharma, Inc. | Certain chemical entities, compositions, and methods |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
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| EP2924038A1 (en) | 2014-03-24 | 2015-09-30 | Evotec (UK) Ltd. | Preparation of pyrrolo[2,3-b]pyrazine and pyrrolo[2,3-b]pyridine derivatives as FGFR inhibitors |
| ES3014202T3 (en) | 2014-03-26 | 2025-04-21 | Astex Therapeutics Ltd | Cmet-inhibitors for use in delaying the emergence in resistance to fgfr inhibitors |
| HUE053653T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR inhibitor és IGF1R inhibitor kombinációi |
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| SMT202200177T1 (it) * | 2014-09-26 | 2022-05-12 | Janssen Pharmaceutica Nv | Uso di gruppi di geni mutanti del fgfr nell'identificazione di pazienti affetti da cancro che saranno responsivi al trattamento con un inibitore del fgfr |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| JOP20200201A1 (ar) | 2015-02-10 | 2017-06-16 | Astex Therapeutics Ltd | تركيبات صيدلانية تشتمل على n-(3.5- ثنائي ميثوكسي فينيل)-n'-(1-ميثيل إيثيل)-n-[3-(ميثيل-1h-بيرازول-4-يل) كينوكسالين-6-يل]إيثان-1.2-ثنائي الأمين |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| EA038045B1 (ru) | 2015-02-20 | 2021-06-28 | Инсайт Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
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| EP3275442B1 (en) | 2015-03-25 | 2021-07-28 | National Cancer Center | Therapeutic agent for bile duct cancer |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| AU2016300175A1 (en) * | 2015-07-24 | 2018-03-01 | Debiopharm International Sa | FGFR expression and susceptibility to an FGFR inhibitor |
| HRP20201157T1 (hr) | 2015-09-23 | 2020-11-13 | Janssen Pharmaceutica N.V. | Triciklički heterocikli za liječenje raka |
| RU2747644C2 (ru) * | 2015-09-23 | 2021-05-11 | Янссен Фармацевтика Нв | Бигетероарил-замещенные 1,4-бензодиазепины и пути их применения для лечения рака |
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2010
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2011
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