JP2010529088A5 - - Google Patents
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- Publication number
- JP2010529088A5 JP2010529088A5 JP2010510815A JP2010510815A JP2010529088A5 JP 2010529088 A5 JP2010529088 A5 JP 2010529088A5 JP 2010510815 A JP2010510815 A JP 2010510815A JP 2010510815 A JP2010510815 A JP 2010510815A JP 2010529088 A5 JP2010529088 A5 JP 2010529088A5
- Authority
- JP
- Japan
- Prior art keywords
- compounds
- drug
- isotope
- labeled compounds
- isotopes
- 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
Links
- 150000001875 compounds Chemical class 0.000 description 12
- 239000003814 drug Substances 0.000 description 4
- 229940079593 drug Drugs 0.000 description 4
- 238000004519 manufacturing process Methods 0.000 description 4
- 239000004480 active ingredient Substances 0.000 description 3
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 description 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 description 2
- NQRYJNQNLNOLGT-UHFFFAOYSA-N Piperidine Chemical compound C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 description 2
- 125000004429 atom Chemical group 0.000 description 2
- 239000003795 chemical substances by application Substances 0.000 description 2
- 239000000460 chlorine Substances 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 230000002503 metabolic effect Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000002285 radioactive effect Effects 0.000 description 2
- 238000002603 single-photon emission computed tomography Methods 0.000 description 2
- NBADVUZGEUFYPS-UHFFFAOYSA-N 1-cyclopropyl-4-[4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyrazol-1-yl]piperidine Chemical compound O1C(C)(C)C(C)(C)OB1C1=CN(C2CCN(CC2)C2CC2)N=C1 NBADVUZGEUFYPS-UHFFFAOYSA-N 0.000 description 1
- ZGQGAZMPTCQISM-UHFFFAOYSA-N 2-oxo-2-(3,4,5-trimethylphenyl)acetaldehyde;hydrate Chemical compound O.CC1=CC(C(=O)C=O)=CC(C)=C1C ZGQGAZMPTCQISM-UHFFFAOYSA-N 0.000 description 1
- XJKHMKCALGNWPT-UHFFFAOYSA-N 8-bromo-6-methyl-2-(3,4,5-trimethoxyphenyl)quinoxaline Chemical compound COC1=C(OC)C(OC)=CC(C=2N=C3C(Br)=CC(C)=CC3=NC=2)=C1 XJKHMKCALGNWPT-UHFFFAOYSA-N 0.000 description 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 description 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 description 1
- YZCKVEUIGOORGS-OUBTZVSYSA-N Deuterium Chemical compound [2H] YZCKVEUIGOORGS-OUBTZVSYSA-N 0.000 description 1
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical compound FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 description 1
- OAICVXFJPJFONN-UHFFFAOYSA-N Phosphorus Chemical compound [P] OAICVXFJPJFONN-UHFFFAOYSA-N 0.000 description 1
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical compound [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 229910052799 carbon Inorganic materials 0.000 description 1
- 229910052801 chlorine Inorganic materials 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 230000003247 decreasing effect Effects 0.000 description 1
- 238000001514 detection method Methods 0.000 description 1
- 229910052805 deuterium Inorganic materials 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- LLRANSBEYQZKFY-UHFFFAOYSA-N dodecanoic acid;propane-1,2-diol Chemical compound CC(O)CO.CCCCCCCCCCCC(O)=O LLRANSBEYQZKFY-UHFFFAOYSA-N 0.000 description 1
- 238000009513 drug distribution Methods 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 238000011049 filling Methods 0.000 description 1
- 238000001914 filtration Methods 0.000 description 1
- 239000011737 fluorine Substances 0.000 description 1
- 229910052731 fluorine Inorganic materials 0.000 description 1
- 229910052739 hydrogen Inorganic materials 0.000 description 1
- 239000001257 hydrogen Substances 0.000 description 1
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 1
- 238000003384 imaging method Methods 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 238000001948 isotopic labelling Methods 0.000 description 1
- 230000003907 kidney function Effects 0.000 description 1
- 230000003908 liver function Effects 0.000 description 1
- 229910052757 nitrogen Inorganic materials 0.000 description 1
- 231100000252 nontoxic Toxicity 0.000 description 1
- 230000003000 nontoxic effect Effects 0.000 description 1
- 239000001301 oxygen Substances 0.000 description 1
- 229910052760 oxygen Inorganic materials 0.000 description 1
- 239000011574 phosphorus Substances 0.000 description 1
- 229910052698 phosphorus Inorganic materials 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 229940002612 prodrug Drugs 0.000 description 1
- 239000000651 prodrug Substances 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 238000003354 tissue distribution assay Methods 0.000 description 1
- 238000003325 tomography Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP07109880 | 2007-06-08 | ||
| EP07109880.0 | 2007-06-08 | ||
| EP07150266 | 2007-12-20 | ||
| EP07150266.0 | 2007-12-20 | ||
| PCT/EP2008/057058 WO2008148867A2 (en) | 2007-06-08 | 2008-06-06 | Quinoxaline derivatives as inhibitors of the tyrosine kinase activity of janus kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2010529088A JP2010529088A (ja) | 2010-08-26 |
| JP2010529088A5 true JP2010529088A5 (enExample) | 2012-07-05 |
| JP5574957B2 JP5574957B2 (ja) | 2014-08-20 |
Family
ID=39720643
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2010510815A Expired - Fee Related JP5574957B2 (ja) | 2007-06-08 | 2008-06-06 | Ｊａｎｕｓキナーゼのチロシンキナーゼ活性の阻害剤としてのキノキサリン誘導体 |
Country Status (17)
| Country | Link |
|---|---|
| US (1) | US8193189B2 (enExample) |
| EP (1) | EP2155201B1 (enExample) |
| JP (1) | JP5574957B2 (enExample) |
| KR (1) | KR20100020465A (enExample) |
| CN (1) | CN101678020B (enExample) |
| AR (1) | AR066879A1 (enExample) |
| AU (1) | AU2008258486B2 (enExample) |
| BR (1) | BRPI0812893A2 (enExample) |
| CA (1) | CA2690288A1 (enExample) |
| CL (1) | CL2008001659A1 (enExample) |
| EA (1) | EA200901608A1 (enExample) |
| ES (1) | ES2392570T3 (enExample) |
| MX (1) | MX2009013218A (enExample) |
| PA (1) | PA8783501A1 (enExample) |
| TW (1) | TW200904814A (enExample) |
| UY (1) | UY31126A1 (enExample) |
| WO (1) | WO2008148867A2 (enExample) |
Families Citing this family (50)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| BRPI0907892A2 (pt) | 2008-02-20 | 2015-07-28 | Actelion Pharmaceuticals Ltd | Composto antibiótico azatricíclico, medicamento, composição farmacêutica que o contém e uso do mesmo |
| AU2009248774B2 (en) | 2008-05-23 | 2012-05-31 | Novartis Ag | Derivatives of quinolines and quinoxalines as protein tyrosine kinase inhibitors |
| EP2298731A4 (en) * | 2008-06-25 | 2011-09-21 | Takeda Pharmaceutical | AMIDE COMPOUND |
| JP4833385B1 (ja) | 2008-10-07 | 2011-12-07 | アクテリオン ファーマシューティカルズ リミテッド | 三環式オキサゾリジノン抗生物質化合物 |
| EP2396004A4 (en) * | 2009-02-11 | 2012-07-25 | Reaction Biology Corp | SELECTIVE KINASE HEMMER |
| US20140128392A1 (en) | 2009-03-19 | 2014-05-08 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| DK2473504T3 (en) * | 2009-09-03 | 2015-03-16 | Bioenergenix | Heterocyclic Compounds for Inhibition of Passover |
| CA2795456A1 (en) | 2010-03-30 | 2011-10-06 | Novartis Ag | Pkc inhibitors for the treatment of b-cell lymphoma having chronic active b-cell-receptor signalling |
| 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 |
| WO2012094462A2 (en) * | 2011-01-05 | 2012-07-12 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| US8263298B1 (en) | 2011-02-24 | 2012-09-11 | Xerox Corporation | Electrically tunable and stable imaging members |
| EP2727920B1 (en) | 2011-07-29 | 2016-11-02 | FUJIFILM Corporation | 1,5-naphthyridine derivative or salt thereof |
| GB201118656D0 (en) | 2011-10-28 | 2011-12-07 | Astex Therapeutics Ltd | New compounds |
| GB201118652D0 (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 |
| GB201118675D0 (en) | 2011-10-28 | 2011-12-14 | Astex Therapeutics Ltd | New compounds |
| US20140343128A1 (en) | 2011-11-15 | 2014-11-20 | Novartis Ag | Combination of a phosphoinositide 3-kinase inhibitor and a modulator of the Janus Kinase 2 - Signal Transducer and Activator of Transcription 5 pathway |
| 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 |
| WO2014013014A1 (en) | 2012-07-18 | 2014-01-23 | Fundació Privada Centre De Regulació Genòmica (Crg) | Jak inhibitors for activation of epidermal stem cell populations |
| GB201307577D0 (en) | 2013-04-26 | 2013-06-12 | Astex Therapeutics Ltd | New compounds |
| US9776997B2 (en) | 2013-06-04 | 2017-10-03 | Bayer Pharma Aktiengesellschaft | 3-aryl-substituted imidazo[1,2-A]pyridines and their use |
| CN105873914B (zh) * | 2013-10-23 | 2018-10-19 | 拜耳作物科学股份公司 | 作为害虫防治剂的取代的喹喔啉衍生物 |
| CN106459090A (zh) | 2014-02-19 | 2017-02-22 | 拜耳制药股份公司 | 3‑(嘧啶‑2‑基)咪唑并[1,2‑a]吡啶 |
| US10736900B2 (en) | 2014-03-26 | 2020-08-11 | Astex Therapeutics Ltd | Combinations of an FGFR inhibitor and an IGF1R inhibitor |
| BR112016022056B1 (pt) | 2014-03-26 | 2023-04-11 | Astex Therapeutics Limited | Combinação, composição farmacêutica, uso de uma combinação ou uma composição farmacêutica, e, produto farmacêutico |
| JO3512B1 (ar) | 2014-03-26 | 2020-07-05 | Astex Therapeutics Ltd | مشتقات كينوكسالين مفيدة كمعدلات لإنزيم fgfr كيناز |
| WO2016087343A1 (de) | 2014-12-02 | 2016-06-09 | Bayer Pharma Aktiengesellschaft | Heteroaryl-substituierte imidazo[1,2-a]pyridine und ihre verwendung |
| TWI719960B (zh) | 2015-02-10 | 2021-03-01 | 英商阿斯迪克治療公司 | 新穎組成物 |
| US10478494B2 (en) | 2015-04-03 | 2019-11-19 | Astex Therapeutics Ltd | FGFR/PD-1 combination therapy for the treatment of cancer |
| EP3328839A1 (en) * | 2015-07-30 | 2018-06-06 | Bristol-Myers Squibb Company | Aryl substituted bicyclic heteroaryl compounds |
| HUE050567T2 (hu) | 2015-09-23 | 2020-12-28 | Janssen Pharmaceutica Nv | Triciklusos heterociklusok rák kezelésére |
| 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 |
| CN108472298B (zh) | 2015-11-24 | 2021-04-20 | 深圳阿拉丁医疗科技有限公司 | 选择性激酶抑制剂 |
| MX383747B (es) * | 2016-02-24 | 2025-03-14 | Pfizer | Derivados de pirazolo[1,5-a]pirazin-4-ilo como inhibidores de quinasas janus (jak) |
| WO2018041989A1 (en) | 2016-09-02 | 2018-03-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods for diagnosing and treating refractory celiac disease type 2 |
| WO2020077024A1 (en) | 2018-10-10 | 2020-04-16 | Albert Einstein College Of Medicine | Benzoxazole and related compounds useful as chaperone-mediated autophagy modulators |
| WO2020201362A2 (en) | 2019-04-02 | 2020-10-08 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Methods of predicting and preventing cancer in patients having premalignant lesions |
| WO2020200291A1 (en) * | 2019-04-02 | 2020-10-08 | Cullgen (Shanghai) , Inc. | Compounds and methods of treating cancers |
| WO2020212395A1 (en) | 2019-04-16 | 2020-10-22 | INSERM (Institut National de la Santé et de la Recherche Médicale) | Use of jak inhibitors for the treatment of painful conditions involving nav1.7 channels |
| TWI865563B (zh) | 2019-07-30 | 2024-12-11 | 德商拜耳動物保健有限公司 | 新穎異喹啉衍生物 |
| CN110698418B (zh) * | 2019-09-11 | 2022-07-01 | 广西师范大学 | 一种3-芳胺基喹喔啉-2-甲酰胺类衍生物及其制备方法和应用 |
| CA3156007A1 (en) | 2019-09-27 | 2021-04-01 | Disc Medicine, Inc. | METHODS OF TREATING MYELOFIBROSE AND ASSOCIATED CONDITIONS |
| 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 |
| ES3075793T3 (en) | 2020-05-13 | 2026-08-07 | Disc Medicine Inc | Anti-hemojuvelin (hjv) antibodies for treating myelofibrosis |
| AU2021273014A1 (en) | 2020-05-13 | 2022-11-17 | AbbVie Deutschland GmbH & Co. KG | Anti-hemojuvelin (HJV) antibodies for treating anemia of chronic disease |
| US20250283174A1 (en) | 2022-05-16 | 2025-09-11 | Institut National de la Santé et de la Recherche Médicale | Methods for assessing the exhaustion of hematopoietic stem cells induced by chronic inflammation |
| CN115385863A (zh) * | 2022-08-17 | 2022-11-25 | 河南师范大学 | 一种3-(二乙氧基甲基)-1-烷基-2(1h)-喹喔啉酮衍生物的合成方法 |
| WO2026093435A1 (en) | 2024-10-31 | 2026-05-07 | Institut National de la Santé et de la Recherche Médicale | Use of jak inhibitors for enhancing the potency of immunotherapy in the treament of cancer |
Family Cites Families (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE4321030A1 (de) | 1993-06-24 | 1995-01-05 | Bayer Ag | 4-bicyclisch substituierte Dihydropyridine, Verfahren zu ihrer Herstellung und ihre Verwendung in Arzneimittel |
| SE9800836D0 (sv) * | 1998-03-13 | 1998-03-13 | Astra Ab | New Compounds |
| JP4361276B2 (ja) * | 2001-04-10 | 2009-11-11 | メルク エンド カムパニー インコーポレーテッド | Ａｋｔ活性の阻害物質 |
| CN1902193B (zh) | 2003-12-04 | 2011-07-13 | 沃泰克斯药物股份有限公司 | 可用作蛋白激酶抑制剂的喹喔啉 |
| HRP20140975T1 (hr) * | 2005-10-07 | 2014-11-21 | Exelixis, Inc. | Derivati n-(3-amino-hinoksalin-2-il)-sulfonamida i njihova uporaba kao inhibitora fosfatidilinozitol 3-kinaze |
-
2008
- 2008-06-05 AR ARP080102398A patent/AR066879A1/es unknown
- 2008-06-06 CA CA2690288A patent/CA2690288A1/en not_active Abandoned
- 2008-06-06 JP JP2010510815A patent/JP5574957B2/ja not_active Expired - Fee Related
- 2008-06-06 US US12/663,698 patent/US8193189B2/en not_active Expired - Fee Related
- 2008-06-06 CN CN2008800193524A patent/CN101678020B/zh not_active Expired - Fee Related
- 2008-06-06 TW TW097121299A patent/TW200904814A/zh unknown
- 2008-06-06 CL CL2008001659A patent/CL2008001659A1/es unknown
- 2008-06-06 WO PCT/EP2008/057058 patent/WO2008148867A2/en not_active Ceased
- 2008-06-06 AU AU2008258486A patent/AU2008258486B2/en not_active Ceased
- 2008-06-06 MX MX2009013218A patent/MX2009013218A/es not_active Application Discontinuation
- 2008-06-06 BR BRPI0812893-6A2A patent/BRPI0812893A2/pt not_active IP Right Cessation
- 2008-06-06 EP EP08760632A patent/EP2155201B1/en not_active Not-in-force
- 2008-06-06 UY UY31126A patent/UY31126A1/es not_active Application Discontinuation
- 2008-06-06 ES ES08760632T patent/ES2392570T3/es active Active
- 2008-06-06 KR KR1020097025493A patent/KR20100020465A/ko not_active Withdrawn
- 2008-06-06 EA EA200901608A patent/EA200901608A1/ru unknown
- 2008-06-06 PA PA20088783501A patent/PA8783501A1/es unknown
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