JP2014530896A5 - - Google Patents
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- JP2014530896A5 JP2014530896A5 JP2014537724A JP2014537724A JP2014530896A5 JP 2014530896 A5 JP2014530896 A5 JP 2014530896A5 JP 2014537724 A JP2014537724 A JP 2014537724A JP 2014537724 A JP2014537724 A JP 2014537724A JP 2014530896 A5 JP2014530896 A5 JP 2014530896A5
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- Prior art keywords
- alkyl
- substituted
- alkoxy
- cancer
- 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.)
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- 125000000217 alkyl group Chemical group 0.000 claims 319
- 125000003545 alkoxy group Chemical group 0.000 claims 55
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 52
- 150000001875 compounds Chemical class 0.000 claims 40
- 206010028980 Neoplasm Diseases 0.000 claims 29
- 201000011510 cancer Diseases 0.000 claims 26
- 125000004093 cyano group Chemical group *C#N 0.000 claims 20
- 238000011282 treatment Methods 0.000 claims 19
- 125000005843 halogen group Chemical group 0.000 claims 17
- 229910052739 hydrogen Inorganic materials 0.000 claims 17
- 239000001257 hydrogen Substances 0.000 claims 17
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 13
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000001475 halogen functional group Chemical group 0.000 claims 12
- 229910052760 oxygen Inorganic materials 0.000 claims 11
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 11
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 150000002431 hydrogen Chemical class 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 10
- 125000001424 substituent group Chemical group 0.000 claims 9
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 7
- 125000000623 heterocyclic group Chemical group 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000002950 monocyclic group Chemical group 0.000 claims 6
- 206010005003 Bladder cancer Diseases 0.000 claims 5
- -1 C 1 Selected from N Inorganic materials 0.000 claims 5
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 5
- 125000003342 alkenyl group Chemical group 0.000 claims 5
- 230000002265 prevention Effects 0.000 claims 5
- 229920006395 saturated elastomer Polymers 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
- 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
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 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
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 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
- 239000003814 drug Substances 0.000 claims 3
- 102000052178 fibroblast growth factor receptor activity proteins Human genes 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
- 239000002246 antineoplastic agent Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 125000002618 bicyclic heterocycle 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
- 125000001153 fluoro group Chemical group F* 0.000 claims 2
- 206010017758 gastric cancer Diseases 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
- 125000003226 pyrazolyl 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
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 claims 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 1
- 125000005943 1,2,3,6-tetrahydropyridyl group Chemical group 0.000 claims 1
- 125000005871 1,3-benzodioxolyl group Chemical group 0.000 claims 1
- 125000002373 5 membered heterocyclic 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
- WTKZEGDFNFYCGP-UHFFFAOYSA-N Pyrazole Chemical compound C=1C=NNC=1 WTKZEGDFNFYCGP-UHFFFAOYSA-N 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
- 125000005189 alkyl hydroxy group Chemical group 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 125000002393 azetidinyl 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
- 125000001309 chloro group Chemical group Cl* 0.000 claims 1
- 208000029742 colonic neoplasm Diseases 0.000 claims 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 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
- 125000002883 imidazolyl group Chemical group 0.000 claims 1
- 125000001041 indolyl group Chemical group 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
- 125000002971 oxazolyl group Chemical group 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 125000004193 piperazinyl group Chemical group 0.000 claims 1
- 125000003386 piperidinyl group Chemical group 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 125000000714 pyrimidinyl group Chemical group 0.000 claims 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 1
- 125000000168 pyrrolyl group Chemical group 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 125000000547 substituted alkyl group Chemical group 0.000 claims 1
- 125000003831 tetrazolyl group Chemical group 0.000 claims 1
- 238000002560 therapeutic procedure Methods 0.000 claims 1
- 125000000335 thiazolyl group Chemical group 0.000 claims 1
- 230000005945 translocation Effects 0.000 claims 1
- 125000001425 triazolyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552880P | 2011-10-28 | 2011-10-28 | |
| GB1118652.5 | 2011-10-28 | ||
| GBGB1118652.5A GB201118652D0 (en) | 2011-10-28 | 2011-10-28 | New compounds |
| US61/552,880 | 2011-10-28 | ||
| PCT/GB2012/052666 WO2013061074A1 (en) | 2011-10-28 | 2012-10-26 | Quinolines as fgfr kinase modulators |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014530896A JP2014530896A (ja) | 2014-11-20 |
| JP2014530896A5 true JP2014530896A5 (enExample) | 2015-12-17 |
| JP6067725B2 JP6067725B2 (ja) | 2017-01-25 |
Family
ID=45373580
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014537724A Active JP6067725B2 (ja) | 2011-10-28 | 2012-10-26 | Ｆｇｆｒキナーゼモジュレーターとしてのキノリン |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US9439896B2 (enExample) |
| EP (1) | EP2776397B1 (enExample) |
| JP (1) | JP6067725B2 (enExample) |
| KR (1) | KR102072869B1 (enExample) |
| CN (1) | CN104011025B (enExample) |
| AU (1) | AU2012328164B2 (enExample) |
| BR (1) | BR112014010177B1 (enExample) |
| CA (1) | CA2853366C (enExample) |
| DK (1) | DK2776397T3 (enExample) |
| ES (1) | ES2661003T3 (enExample) |
| GB (1) | GB201118652D0 (enExample) |
| HU (1) | HUE037458T2 (enExample) |
| IN (1) | IN2014MN00988A (enExample) |
| MX (1) | MX353806B (enExample) |
| RU (1) | RU2625303C2 (enExample) |
| WO (1) | WO2013061074A1 (enExample) |
Families Citing this family (35)
| 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 |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118654D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201209609D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| GB201209613D0 (en) | 2012-05-30 | 2012-07-11 | Astex Therapeutics Ltd | New compounds |
| EP2909189B8 (en) | 2012-10-16 | 2017-04-19 | Janssen Pharmaceutica NV | Heteroaryl linked quinolinyl modulators of ror-gamma-t |
| TWI606045B (zh) | 2012-10-16 | 2017-11-21 | 健生藥品公司 | ＲＯＲγｔ之亞甲基聯結的喹啉基調節劑 |
| WO2014062667A1 (en) | 2012-10-16 | 2014-04-24 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of ror-gamma-t |
| 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 |
| US9284308B2 (en) | 2013-10-15 | 2016-03-15 | Janssen Pharmaceutica Nv | Methylene linked quinolinyl modulators of RORγt |
| WO2015057629A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | ALKYL LINKED QUINOLINYL MODULATORS OF RORyt |
| US9221804B2 (en) | 2013-10-15 | 2015-12-29 | Janssen Pharmaceutica Nv | Secondary alcohol quinolinyl modulators of RORγt |
| US9403816B2 (en) | 2013-10-15 | 2016-08-02 | Janssen Pharmaceutica Nv | Phenyl linked quinolinyl modulators of RORγt |
| US10555941B2 (en) | 2013-10-15 | 2020-02-11 | Janssen Pharmaceutica Nv | Alkyl linked quinolinyl modulators of RORγt |
| WO2015057206A1 (en) * | 2013-10-15 | 2015-04-23 | Janssen Pharmaceutica Nv | SECONDARY ALCOHOL QUINOLINYL MODULATORS OF RORyt |
| US9328095B2 (en) | 2013-10-15 | 2016-05-03 | Janssen Pharmaceutica Nv | Heteroaryl linked quinolinyl modulators of RORgammat |
| EP3057422B1 (en) | 2013-10-15 | 2019-05-15 | Janssen Pharmaceutica NV | Quinolinyl modulators of ror(gamma)t |
| KR102479696B1 (ko) | 2014-03-26 | 2022-12-22 | 아스텍스 테라퓨틱스 리미티드 | Fgfr 억제제 및 igf1r 억제제의 조합물 |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| HUE053654T2 (hu) | 2014-03-26 | 2021-07-28 | Astex Therapeutics Ltd | FGFR- és CMET-inhibitorok kombinációi a rák kezelésére |
| BR112017002268B1 (pt) | 2014-08-18 | 2022-11-08 | Eisai R&D Management Co., Ltd | Sal de derivado de piridina monocíclica e cristal do mesmo |
| 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 |
| CA2996857C (en) * | 2015-09-23 | 2024-05-21 | Janssen Pharmaceutica Nv | Quinoxaline, quinoline and quinazolinone derivative compounds for the treatment of cancer |
| EP3353164B1 (en) * | 2015-09-23 | 2021-11-03 | Janssen Pharmaceutica, N.V. | Bi-heteroaryl substituted 1,4-benzodiazepines and uses thereof for the treatment of cancer |
| WO2017104739A1 (ja) | 2015-12-17 | 2017-06-22 | エーザイ・アール・アンド・ディー・マネジメント株式会社 | 乳がん治療剤 |
| CN108264510A (zh) * | 2017-01-02 | 2018-07-10 | 上海喆邺生物科技有限公司 | 一种选择性抑制激酶化合物及其用途 |
| BR112020017922A2 (pt) | 2018-03-28 | 2020-12-22 | Eisai R&D Management Co., Ltd. | Agente terapêutico para carcinoma hepatocelular |
| CN113087696A (zh) * | 2019-12-23 | 2021-07-09 | 江苏开元药业有限公司 | 喹啉类化合物及其应用 |
| JP2023512482A (ja) * | 2020-01-17 | 2023-03-27 | ベータ・ファーマ・インコーポレイテッド | Ｆｇｆｒキナーゼ阻害剤としてのピリダジンおよび１，２，４－トリアジン誘導体 |
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2012
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