JP2014534212A5 - - Google Patents
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- JP2014534212A5 JP2014534212A5 JP2014537731A JP2014537731A JP2014534212A5 JP 2014534212 A5 JP2014534212 A5 JP 2014534212A5 JP 2014537731 A JP2014537731 A JP 2014537731A JP 2014537731 A JP2014537731 A JP 2014537731A JP 2014534212 A5 JP2014534212 A5 JP 2014534212A5
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- Prior art keywords
- alkyl
- substituted
- alkoxy
- cancer
- halo
- Prior art date
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- 125000000217 alkyl group Chemical group 0.000 claims 358
- 125000003545 alkoxy group Chemical group 0.000 claims 58
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 54
- 150000001875 compounds Chemical class 0.000 claims 37
- 206010028980 Neoplasm Diseases 0.000 claims 29
- 201000011510 cancer Diseases 0.000 claims 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims 21
- 125000005843 halogen group Chemical group 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 125000001475 halogen functional group Chemical group 0.000 claims 14
- 150000002431 hydrogen Chemical class 0.000 claims 13
- 229910052760 oxygen Inorganic materials 0.000 claims 12
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 11
- 229910052736 halogen Inorganic materials 0.000 claims 11
- 150000002367 halogens Chemical class 0.000 claims 11
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 8
- 125000001424 substituent group Chemical group 0.000 claims 8
- 125000003342 alkenyl group Chemical group 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000002950 monocyclic group Chemical group 0.000 claims 7
- -1 C 1 Selected from N Inorganic materials 0.000 claims 6
- 230000002265 prevention Effects 0.000 claims 6
- 206010005003 Bladder cancer Diseases 0.000 claims 5
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 5
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 5
- 201000005112 urinary bladder cancer Diseases 0.000 claims 5
- 102100027842 Fibroblast growth factor receptor 3 Human genes 0.000 claims 4
- 101710182396 Fibroblast growth factor receptor 3 Proteins 0.000 claims 4
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 4
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 4
- 201000010099 disease Diseases 0.000 claims 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 4
- 229920006395 saturated elastomer Polymers 0.000 claims 4
- 206010006187 Breast cancer Diseases 0.000 claims 3
- 208000026310 Breast neoplasm Diseases 0.000 claims 3
- 206010009944 Colon cancer Diseases 0.000 claims 3
- 108091008794 FGF receptors Proteins 0.000 claims 3
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 3
- 208000034578 Multiple myelomas Diseases 0.000 claims 3
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 201000005202 lung cancer Diseases 0.000 claims 3
- 208000020816 lung neoplasm Diseases 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 229910052757 nitrogen Inorganic materials 0.000 claims 3
- 125000004076 pyridyl group Chemical group 0.000 claims 3
- ZEOWTGPWHLSLOG-UHFFFAOYSA-N Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F Chemical compound Cc1ccc(cc1-c1ccc2c(n[nH]c2c1)-c1cnn(c1)C1CC1)C(=O)Nc1cccc(c1)C(F)(F)F ZEOWTGPWHLSLOG-UHFFFAOYSA-N 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 102100023593 Fibroblast growth factor receptor 1 Human genes 0.000 claims 2
- 101710182386 Fibroblast growth factor receptor 1 Proteins 0.000 claims 2
- 102100023600 Fibroblast growth factor receptor 2 Human genes 0.000 claims 2
- 101710182389 Fibroblast growth factor receptor 2 Proteins 0.000 claims 2
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000000304 alkynyl group Chemical group 0.000 claims 2
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000004432 carbon atom Chemical group C* 0.000 claims 2
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 claims 2
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 0.000 claims 2
- 206010017758 gastric cancer Diseases 0.000 claims 2
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 125000001041 indolyl group Chemical group 0.000 claims 2
- 201000007270 liver cancer Diseases 0.000 claims 2
- 208000014018 liver neoplasm Diseases 0.000 claims 2
- 125000002757 morpholinyl group Chemical group 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 2
- 208000002154 non-small cell lung carcinoma Diseases 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000002971 oxazolyl group Chemical group 0.000 claims 2
- 125000004193 piperazinyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000003226 pyrazolyl group Chemical group 0.000 claims 2
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000000168 pyrrolyl group Chemical group 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 201000011549 stomach cancer Diseases 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000001425 triazolyl group Chemical group 0.000 claims 2
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 1
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 claims 1
- 206010014733 Endometrial cancer Diseases 0.000 claims 1
- 206010014759 Endometrial neoplasm Diseases 0.000 claims 1
- 102100027844 Fibroblast growth factor receptor 4 Human genes 0.000 claims 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 1
- 208000034951 Genetic Translocation Diseases 0.000 claims 1
- 101000917134 Homo sapiens Fibroblast growth factor receptor 4 Proteins 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 208000014767 Myeloproliferative disease Diseases 0.000 claims 1
- 201000007224 Myeloproliferative neoplasm Diseases 0.000 claims 1
- 150000001204 N-oxides Chemical class 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000000102 Squamous Cell Carcinoma of Head and Neck Diseases 0.000 claims 1
- 125000003282 alkyl amino group Chemical group 0.000 claims 1
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 125000002619 bicyclic group Chemical group 0.000 claims 1
- 125000004452 carbocyclyl group Chemical group 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 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
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 238000000034 method Methods 0.000 claims 1
- 230000035772 mutation Effects 0.000 claims 1
- 201000002740 oral squamous cell carcinoma Diseases 0.000 claims 1
- 230000002018 overexpression Effects 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- 0 Cc(c(*)n[n]1*)c1I Chemical compound Cc(c(*)n[n]1*)c1I 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552873P | 2011-10-28 | 2011-10-28 | |
| GB1118654.1 | 2011-10-28 | ||
| US61/552,873 | 2011-10-28 | ||
| GBGB1118654.1A GB201118654D0 (en) | 2011-10-28 | 2011-10-28 | New compounds |
| PCT/GB2012/052673 WO2013061081A1 (en) | 2011-10-28 | 2012-10-26 | Anticancer benzopyrazines via the inhibition of fgfr kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014534212A JP2014534212A (ja) | 2014-12-18 |
| JP2014534212A5 true JP2014534212A5 (GUID-C5D7CC26-194C-43D0-91A1-9AE8C70A9BFF.html) | 2015-12-17 |
| JP6054406B2 JP6054406B2 (ja) | 2016-12-27 |
Family
ID=45373582
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014537731A Active JP6054406B2 (ja) | 2011-10-28 | 2012-10-26 | Ｆｇｆｒキナーゼ阻害を介した抗癌ベンゾピラジン |
Country Status (18)
Families Citing this family (34)
| 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 |
| GB201118652D0 (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 |
| 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 |
| 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 |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| SMT202100115T1 (it) | 2014-03-26 | 2021-05-07 | Astex Therapeutics Ltd | Combinazioni di inibitori di fgfr e cmet per il trattamento del cancro |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| RU2715893C2 (ru) | 2014-03-26 | 2020-03-04 | Астекс Терапьютикс Лтд | Комбинации ингибитора fgfr и ингибитора igf1r |
| KR102359214B1 (ko) | 2014-04-04 | 2022-02-07 | 델 마 파마슈티컬스 | 폐의 비소세포 암종 및 난소암을 치료하기 위한 디안하이드로갈락티톨 및 이의 유사체 또는 유도체 |
| KR102344105B1 (ko) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
| CN104370825B (zh) * | 2014-09-29 | 2017-04-19 | 人福医药集团股份公司 | 作为激酶抑制剂的取代杂环化合物及其制备方法和用途 |
| 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 |
| RU2712222C2 (ru) | 2015-03-25 | 2020-01-27 | Нэшнл Кэнсер Сентер | Терапевтическое средство против рака желчных протоков |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| WO2017050865A1 (en) | 2015-09-23 | 2017-03-30 | Janssen Pharmaceutica Nv | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| HRP20201157T1 (hr) | 2015-09-23 | 2020-11-13 | Janssen Pharmaceutica N.V. | Triciklički heterocikli za liječenje raka |
| KR102486722B1 (ko) | 2015-12-17 | 2023-01-11 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 유방암 치료제 |
| WO2017157885A1 (de) | 2016-03-16 | 2017-09-21 | Bayer Cropscience Aktiengesellschaft | N-(cyanbenzyl)-6-(cyclopropylcarbonylamino)-4-(phenyl)-pyridin-2-carboxamid-derivate und verwandte verbindungen als pestizide pflanzenschutzmittel |
| CA3039919A1 (en) * | 2016-10-10 | 2018-04-19 | Development Center For Biotechnology | Quinoxaline compounds as type iii receptor tyrosine kinase inhibitors |
| EP3284739A1 (de) | 2017-07-19 | 2018-02-21 | Bayer CropScience Aktiengesellschaft | Substituierte (het)arylverbindungen als schädlingsbekämpfungsmittel |
| EP3750880B1 (en) * | 2018-02-08 | 2022-12-21 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Pyrazine-2(1h)-ketone compound acting as fgfr inhibitor |
| AU2019241625A1 (en) | 2018-03-28 | 2020-09-03 | Eisai R&D Management Co., Ltd. | Therapeutic agent for hepatocellular carcinoma |
| JP2022515198A (ja) | 2018-12-19 | 2022-02-17 | アレイ バイオファーマ インコーポレイテッド | ＦＧＦＲチロシンキナーゼの阻害剤としての置換ピラゾロ［１，５－ａ］ピリジン化合物 |
| WO2020131674A1 (en) * | 2018-12-19 | 2020-06-25 | Array Biopharma Inc. | 7-((3,5-dimethoxyphenyl)amino)quinoxaline derivatives as fgfr inhibitors for treating cancer |
| US11603366B2 (en) | 2019-08-08 | 2023-03-14 | Zhangzhou Pien Tze Huang Pharmaceutical Co., Ltd. | Crystalline form and B crystalline form of pyrazine-2(1H)-ketone compound and preparation method thereof |
| CN110981819B (zh) * | 2019-12-24 | 2022-07-01 | 广西师范大学 | 一种喹喔啉类信号通路抑制剂及其制备方法和应用 |
| US20250313544A1 (en) * | 2022-05-10 | 2025-10-09 | H. Lee Moffitt Cancer Center And Research Institute, Inc. | Inhibitors of glutathione s-transferase zeta 1 (gstz1) and methods of use |
| WO2025019622A2 (en) * | 2023-07-18 | 2025-01-23 | Elixiron Immunotherapeutics Inc. | Method of enhanced absorption of quinoxaline type iii receptor tyrosine kinase inhibitors |
| WO2025067450A1 (zh) * | 2023-09-28 | 2025-04-03 | 福贝生物医药科技(北京)有限公司 | 一种固体分散体、药物组合物、其制备方法及其用途 |
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