JP2011522866A5 - - Google Patents
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- JP2011522866A5 JP2011522866A5 JP2011512999A JP2011512999A JP2011522866A5 JP 2011522866 A5 JP2011522866 A5 JP 2011522866A5 JP 2011512999 A JP2011512999 A JP 2011512999A JP 2011512999 A JP2011512999 A JP 2011512999A JP 2011522866 A5 JP2011522866 A5 JP 2011522866A5
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- Japan
- Prior art keywords
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- alkyl
- optionally substituted
- halo
- conr
- 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 83
- 125000000623 heterocyclic group Chemical group 0.000 claims 23
- 150000001875 compounds Chemical class 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 125000003545 alkoxy group Chemical group 0.000 claims 16
- 125000005843 halogen group Chemical group 0.000 claims 15
- 125000006552 (C3-C8) cycloalkyl group Chemical group 0.000 claims 14
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 14
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 14
- 125000000392 cycloalkenyl group Chemical group 0.000 claims 14
- 229910052736 halogen Inorganic materials 0.000 claims 13
- 150000002367 halogens Chemical class 0.000 claims 13
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims 13
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 12
- 125000003118 aryl group Chemical group 0.000 claims 8
- 150000002431 hydrogen Chemical class 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 125000003349 3-pyridyl group Chemical group N1=C([H])C([*])=C([H])C([H])=C1[H] 0.000 claims 4
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 4
- 125000002837 carbocyclic group Chemical group 0.000 claims 3
- 125000004432 carbon atom Chemical group C* 0.000 claims 3
- 229910052801 chlorine Inorganic materials 0.000 claims 3
- 239000000460 chlorine Substances 0.000 claims 3
- 125000000753 cycloalkyl group Chemical group 0.000 claims 3
- 125000006371 dihalo methyl group Chemical group 0.000 claims 3
- 125000006372 monohalo methyl group Chemical group 0.000 claims 3
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 125000003226 pyrazolyl group Chemical group 0.000 claims 3
- 125000001963 4 membered heterocyclic group Chemical group 0.000 claims 2
- 125000000339 4-pyridyl group Chemical group N1=C([H])C([H])=C([*])C([H])=C1[H] 0.000 claims 2
- -1 Oxo-dihydro-pyridin-3-yl Chemical group 0.000 claims 2
- GLUUGHFHXGJENI-UHFFFAOYSA-N Piperazine Chemical compound C1CNCCN1 GLUUGHFHXGJENI-UHFFFAOYSA-N 0.000 claims 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 claims 2
- 125000001309 chloro group Chemical group Cl* 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 125000002883 imidazolyl group Chemical group 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- 125000001715 oxadiazolyl group Chemical group 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000001424 substituent group Chemical group 0.000 claims 2
- 125000003831 tetrazolyl group Chemical group 0.000 claims 2
- 238000002560 therapeutic procedure Methods 0.000 claims 2
- 125000001113 thiadiazolyl group Chemical group 0.000 claims 2
- 125000000335 thiazolyl group Chemical group 0.000 claims 2
- 125000004890 (C1-C6) alkylamino group Chemical group 0.000 claims 1
- 125000006564 (C4-C8) cycloalkyl group Chemical group 0.000 claims 1
- 125000004105 2-pyridyl group Chemical group N1=C([*])C([H])=C([H])C([H])=C1[H] 0.000 claims 1
- 125000002373 5 membered heterocyclic group Chemical group 0.000 claims 1
- 125000004070 6 membered heterocyclic group Chemical group 0.000 claims 1
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 1
- 108091008794 FGF receptors Proteins 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- KPCZJLGGXRGYIE-UHFFFAOYSA-N [C]1=CC=CN=C1 Chemical group [C]1=CC=CN=C1 KPCZJLGGXRGYIE-UHFFFAOYSA-N 0.000 claims 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 1
- 150000003053 piperidines Chemical class 0.000 claims 1
- 230000000069 prophylactic effect Effects 0.000 claims 1
- 238000011321 prophylaxis Methods 0.000 claims 1
- 125000003373 pyrazinyl group Chemical group 0.000 claims 1
- 125000002098 pyridazinyl group Chemical group 0.000 claims 1
- 125000004076 pyridyl group Chemical group 0.000 claims 1
- 125000000246 pyrimidin-2-yl group Chemical group [H]C1=NC(*)=NC([H])=C1[H] 0.000 claims 1
- 125000004527 pyrimidin-4-yl group Chemical group N1=CN=C(C=C1)* 0.000 claims 1
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 239000012453 solvate Substances 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- NQRYJNQNLNOLGT-UHFFFAOYSA-N tetrahydropyridine hydrochloride Natural products C1CCNCC1 NQRYJNQNLNOLGT-UHFFFAOYSA-N 0.000 claims 1
- 125000001544 thienyl group Chemical group 0.000 claims 1
- 125000004306 triazinyl group Chemical group 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US6118408P | 2008-06-13 | 2008-06-13 | |
| US61/061,184 | 2008-06-13 | ||
| GB0810902.7 | 2008-06-13 | ||
| GBGB0810902.7A GB0810902D0 (en) | 2008-06-13 | 2008-06-13 | New compounds |
| PCT/EP2009/057318 WO2009150240A1 (en) | 2008-06-13 | 2009-06-12 | Imidazopyridine derivatives as inhibitors of receptor tyrosine kinases |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011522866A JP2011522866A (ja) | 2011-08-04 |
| JP2011522866A5 true JP2011522866A5 (enExample) | 2012-05-17 |
| JP5596023B2 JP5596023B2 (ja) | 2014-09-24 |
Family
ID=39672279
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011512999A Expired - Fee Related JP5596023B2 (ja) | 2008-06-13 | 2009-06-12 | レセプターチロシンキナーゼのインヒビターとしてのイミダゾピリジン誘導体 |
Country Status (21)
| Country | Link |
|---|---|
| US (1) | US8796244B2 (enExample) |
| EP (1) | EP2300465B1 (enExample) |
| JP (1) | JP5596023B2 (enExample) |
| KR (1) | KR101745730B1 (enExample) |
| CN (1) | CN102137859B (enExample) |
| AU (1) | AU2009256584B2 (enExample) |
| BR (1) | BRPI0915084B8 (enExample) |
| CA (1) | CA2727062A1 (enExample) |
| DK (1) | DK2300465T3 (enExample) |
| ES (1) | ES2735979T3 (enExample) |
| GB (1) | GB0810902D0 (enExample) |
| HR (1) | HRP20191027T1 (enExample) |
| HU (1) | HUE045300T2 (enExample) |
| IL (1) | IL209864A (enExample) |
| LT (1) | LT2300465T (enExample) |
| MX (1) | MX2010013743A (enExample) |
| NZ (1) | NZ589781A (enExample) |
| RU (1) | RU2518089C2 (enExample) |
| SI (1) | SI2300465T1 (enExample) |
| WO (1) | WO2009150240A1 (enExample) |
| ZA (1) | ZA201008961B (enExample) |
Families Citing this family (67)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2672213C (en) | 2006-12-22 | 2016-02-16 | Astex Therapeutics Limited | Bicyclic amine derivatives as protein tyrosine kinase inhibitors |
| US8895745B2 (en) | 2006-12-22 | 2014-11-25 | Astex Therapeutics Limited | Bicyclic heterocyclic compounds as FGFR inhibitors |
| GB0720038D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New compounds |
| GB0720041D0 (en) | 2007-10-12 | 2007-11-21 | Astex Therapeutics Ltd | New Compounds |
| GB0810902D0 (en) | 2008-06-13 | 2008-07-23 | Astex Therapeutics Ltd | New compounds |
| MX2011009796A (es) * | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| GB0906470D0 (en) * | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| GB0906472D0 (en) | 2009-04-15 | 2009-05-20 | Astex Therapeutics Ltd | New compounds |
| WO2011104731A1 (en) * | 2010-02-26 | 2011-09-01 | Decode Genetics Ehf | Genetic variants as markers for use in urinary bladder cancer risk assessment, diagnosis, prognosis and treatment |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| WO2013018733A1 (ja) | 2011-07-29 | 2013-02-07 | 富士フイルム株式会社 | １，５－ナフチリジン誘導体又はその塩 |
| UA111382C2 (uk) | 2011-10-10 | 2016-04-25 | Оріон Корпорейшн | Інгібітори протеїнкінази |
| CN103214481B (zh) * | 2012-01-21 | 2016-08-03 | 中国科学院上海药物研究所 | 新型咪唑并[1,2-a]吡啶类化合物、其制备方法、包含此类化合物的药物组合物及其用途 |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| CN102786543B (zh) * | 2012-07-24 | 2016-04-27 | 上海瑞博化学有限公司 | 咪唑并[1，2-a]吡啶-6-硼酸频哪醇酯及其衍生物的制备方法 |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US8729263B2 (en) | 2012-08-13 | 2014-05-20 | Novartis Ag | 1,4-disubstituted pyridazine analogs there of and methods for treating SMN-deficiency-related conditions |
| CN104768548B (zh) | 2012-09-28 | 2018-08-10 | 范德比尔特大学 | 作为选择性bmp抑制剂的稠合杂环化合物 |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| JP6404230B2 (ja) | 2012-12-20 | 2018-10-10 | インセプション ２、 インコーポレイテッド | トリアゾロン化合物およびその使用 |
| CN103923078A (zh) * | 2013-01-15 | 2014-07-16 | 华东理工大学 | 3,4-二取代(1H-吡唑[3,4-b]吡啶)类化合物及其用途 |
| AR094812A1 (es) | 2013-02-20 | 2015-08-26 | Eisai R&D Man Co Ltd | Derivado de piridina monocíclico como inhibidor del fgfr |
| BR112015020716A2 (pt) | 2013-03-13 | 2017-07-18 | Hoffmann La Roche | processo para a preparação de (2-(4-(2-(1-isopropil-3-metil-1h-1,2,4-triazol-5-il)-5,6-diidrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-il)-1h-pirazol-1-il)-2-metilpropanamida (i) e composto |
| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| MX2020011652A (es) | 2013-07-31 | 2022-09-27 | Novartis Ag | Derivados de piridazina 1,4-disustituida, y su uso para el tratamiento de afecciones relacionadas con la deficiencia de smn. |
| AU2014369031A1 (en) | 2013-12-20 | 2016-07-07 | Signal Pharmaceuticals, Llc | Substituted Diaminopyrimidyl Compounds, compositions thereof, and methods of treatment therewith |
| LT3083616T (lt) * | 2013-12-20 | 2021-09-10 | Astex Therapeutics Limited | Bicikinių heterociklų junginiai ir jų panaudojimas terapijoje |
| KR102344105B1 (ko) | 2014-08-18 | 2021-12-29 | 에자이 알앤드디 매니지먼트 가부시키가이샤 | 모노시클릭 피리딘 유도체의 염 및 이의 결정 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
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| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| JP6791844B2 (ja) * | 2015-03-24 | 2020-11-25 | 株式会社ダイセル | 超臨界流体クロマトグラフィー用の固定相 |
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| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
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| CN114502555B (zh) * | 2019-10-15 | 2024-07-16 | 常州千红生化制药股份有限公司 | 用于治疗增殖性疾病和疾患的4-(咪唑并[1,2-a]吡啶-3-基)-N-(吡啶-3-基)嘧啶-2-胺的衍生物 |
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-
2008
- 2008-06-13 GB GBGB0810902.7A patent/GB0810902D0/en not_active Ceased
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2009
- 2009-06-12 LT LTEP09761801.1T patent/LT2300465T/lt unknown
- 2009-06-12 HU HUE09761801A patent/HUE045300T2/hu unknown
- 2009-06-12 NZ NZ589781A patent/NZ589781A/xx not_active IP Right Cessation
- 2009-06-12 WO PCT/EP2009/057318 patent/WO2009150240A1/en not_active Ceased
- 2009-06-12 RU RU2011100786/04A patent/RU2518089C2/ru active
- 2009-06-12 US US12/997,754 patent/US8796244B2/en active Active
- 2009-06-12 KR KR1020117000791A patent/KR101745730B1/ko not_active Expired - Fee Related
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- 2009-06-12 EP EP09761801.1A patent/EP2300465B1/en active Active
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