JP2014503574A5 - - Google Patents
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- Publication number
- JP2014503574A5 JP2014503574A5 JP2013550886A JP2013550886A JP2014503574A5 JP 2014503574 A5 JP2014503574 A5 JP 2014503574A5 JP 2013550886 A JP2013550886 A JP 2013550886A JP 2013550886 A JP2013550886 A JP 2013550886A JP 2014503574 A5 JP2014503574 A5 JP 2014503574A5
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- JP
- Japan
- Prior art keywords
- compound
- group
- formula
- optionally substituted
- nitrogen atom
- 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
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- 150000001875 compounds Chemical class 0.000 claims 46
- 229910052757 nitrogen Inorganic materials 0.000 claims 11
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 11
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 10
- 125000004435 hydrogen atom Chemical group [H]* 0.000 claims 10
- 229910052717 sulfur Inorganic materials 0.000 claims 9
- 239000008194 pharmaceutical composition Substances 0.000 claims 8
- 150000003839 salts Chemical class 0.000 claims 8
- 238000000034 method Methods 0.000 claims 6
- 125000000623 heterocyclic group Chemical group 0.000 claims 5
- 125000005843 halogen group Chemical group 0.000 claims 4
- 239000000203 mixture Substances 0.000 claims 4
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 3
- 108091000080 Phosphotransferase Proteins 0.000 claims 3
- 125000003118 aryl group Chemical group 0.000 claims 3
- 102000020233 phosphotransferase Human genes 0.000 claims 3
- JUJWROOIHBZHMG-UHFFFAOYSA-N Pyridine Chemical group C1=CC=NC=C1 JUJWROOIHBZHMG-UHFFFAOYSA-N 0.000 claims 2
- 102000001332 SRC Human genes 0.000 claims 2
- 108060006706 SRC Proteins 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000004429 atom Chemical group 0.000 claims 2
- 230000008878 coupling Effects 0.000 claims 2
- 238000010168 coupling process Methods 0.000 claims 2
- 238000005859 coupling reaction Methods 0.000 claims 2
- 125000002485 formyl group Chemical class [H]C(*)=O 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 230000004770 neurodegeneration Effects 0.000 claims 2
- 208000015122 neurodegenerative disease Diseases 0.000 claims 2
- 229910052760 oxygen Inorganic materials 0.000 claims 2
- 239000012453 solvate Substances 0.000 claims 2
- 238000006467 substitution reaction Methods 0.000 claims 2
- 125000006652 (C3-C12) cycloalkyl group Chemical group 0.000 claims 1
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 239000002246 antineoplastic agent Substances 0.000 claims 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 238000010511 deprotection reaction Methods 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 229940043355 kinase inhibitor Drugs 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 1
- 239000003757 phosphotransferase inhibitor Substances 0.000 claims 1
- 238000006268 reductive amination reaction Methods 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 0 CC(Cc1ccc(*)cc1*)*C(C1=C)=**(*N)C1=* Chemical compound CC(Cc1ccc(*)cc1*)*C(C1=C)=**(*N)C1=* 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| FR1150651 | 2011-01-27 | ||
| FR1150651A FR2970967B1 (fr) | 2011-01-27 | 2011-01-27 | Derives de type azaindazole ou diazaindazole comme medicament |
| PCT/EP2012/051283 WO2012101239A1 (en) | 2011-01-27 | 2012-01-27 | Derivatives of azaindazole or diazaindazole type as medicament |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2014503574A JP2014503574A (ja) | 2014-02-13 |
| JP2014503574A5 true JP2014503574A5 (enExample) | 2015-02-26 |
| JP5931926B2 JP5931926B2 (ja) | 2016-06-08 |
Family
ID=44318089
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2013550886A Active JP5931926B2 (ja) | 2011-01-27 | 2012-01-27 | 医薬としてのアザインダゾールまたはジアザインダゾール型の誘導体 |
Country Status (30)
| Country | Link |
|---|---|
| US (2) | US20130172360A1 (enExample) |
| EP (1) | EP2668184B1 (enExample) |
| JP (1) | JP5931926B2 (enExample) |
| KR (2) | KR20180122028A (enExample) |
| CN (1) | CN103339129B (enExample) |
| AR (1) | AR084935A1 (enExample) |
| AU (1) | AU2012210467B2 (enExample) |
| BR (1) | BR112013018852B1 (enExample) |
| CA (1) | CA2823824C (enExample) |
| CY (1) | CY1120088T1 (enExample) |
| DK (1) | DK2668184T3 (enExample) |
| ES (1) | ES2661695T3 (enExample) |
| FR (1) | FR2970967B1 (enExample) |
| HR (1) | HRP20180524T1 (enExample) |
| HU (1) | HUE037153T2 (enExample) |
| IL (2) | IL227496B (enExample) |
| LT (1) | LT2668184T (enExample) |
| MA (1) | MA34903B1 (enExample) |
| MX (1) | MX356411B (enExample) |
| MY (1) | MY180666A (enExample) |
| PL (1) | PL2668184T3 (enExample) |
| PT (1) | PT2668184T (enExample) |
| RS (1) | RS57101B1 (enExample) |
| RU (1) | RU2600976C2 (enExample) |
| SI (1) | SI2668184T1 (enExample) |
| TN (1) | TN2013000293A1 (enExample) |
| TR (1) | TR201802944T4 (enExample) |
| TW (1) | TWI546303B (enExample) |
| UA (1) | UA109698C2 (enExample) |
| WO (1) | WO2012101239A1 (enExample) |
Families Citing this family (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| FR2970967B1 (fr) * | 2011-01-27 | 2013-02-15 | Pf Medicament | Derives de type azaindazole ou diazaindazole comme medicament |
| EP2817292B1 (en) | 2012-02-22 | 2019-12-18 | Sanford-Burnham Medical Research Institute | Sulfonamide compounds and uses as tnap inhibitors |
| HUE042374T2 (hu) | 2012-06-13 | 2019-06-28 | Incyte Holdings Corp | Szubsztituált triciklusos vegyületek mint FGFR inhibitorok |
| EP2689779A1 (en) | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindazole or diazaindazole type for treating a cancer overexpressing trk |
| EP2689778A1 (en) * | 2012-07-27 | 2014-01-29 | Pierre Fabre Medicament | Derivatives of azaindoles or diazaindoles for treating pain |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| KR102469849B1 (ko) | 2013-04-19 | 2022-11-23 | 인사이트 홀딩스 코포레이션 | Fgfr 저해제로서 이환식 헤테로사이클 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| EP3233840B1 (en) | 2014-12-16 | 2018-11-21 | Eudendron S.r.l. | Heterocyclic derivatives modulating activity of certain protein kinases |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| AU2016219822B2 (en) | 2015-02-20 | 2020-07-09 | Incyte Holdings Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | Incyte Corporation | Bicyclic heterocycles as fgfr4 inhibitors |
| US10211205B2 (en) * | 2016-04-27 | 2019-02-19 | International Business Machines Corporation | Field effect transistor structure for reducing contact resistance |
| CN108570052A (zh) * | 2017-03-13 | 2018-09-25 | 中国科学院上海药物研究所 | 五元杂环并吡嗪化合物、制备方法、中间体、组合和应用 |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| JP7322140B6 (ja) * | 2018-05-02 | 2024-02-21 | ジェイダブリュ ファーマシューティカル コーポレーション | 新規なヘテロサイクル誘導体 |
| EP4309737A3 (en) | 2018-05-04 | 2024-03-27 | Incyte Corporation | Solid forms of an fgfr inhibitor and processes for preparing the same |
| EP3788046B1 (en) | 2018-05-04 | 2025-12-10 | Incyte Corporation | Salts of an fgfr inhibitor |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| EP3725777A1 (en) * | 2019-04-17 | 2020-10-21 | Rottapharm Biotech S.r.l. | Benzo- and pyrido-pyrazoles as protein kinase inhibitors |
| US11591329B2 (en) | 2019-07-09 | 2023-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| WO2021076602A1 (en) | 2019-10-14 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| KR20220131900A (ko) | 2019-12-04 | 2022-09-29 | 인사이트 코포레이션 | Fgfr 억제제의 유도체 |
| JP7720840B2 (ja) | 2019-12-04 | 2025-08-08 | インサイト・コーポレイション | Ｆｇｆｒ阻害剤としての三環式複素環 |
| JP2023509421A (ja) * | 2019-12-31 | 2023-03-08 | アイエフエム デュー インコーポレイテッド | Ｓｔｉｎｇ活性に関連する状態を治療するための化合物および組成物 |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| CN115916771B (zh) * | 2020-04-02 | 2025-04-01 | 浙江华海药业股份有限公司 | 多靶点的抗肿瘤化合物及其制备方法和应用 |
| CN116745268A (zh) * | 2020-11-20 | 2023-09-12 | 2692372安大略公司 | 苯磺酰胺衍生物及其用途 |
| CA3215903A1 (en) | 2021-04-12 | 2022-10-20 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE242245T1 (de) * | 1997-03-19 | 2003-06-15 | Basf Ag | Pyrrolo(2,3-d)pyrimidine und ihre verwendung als tyrosinkinase-inhibitoren |
| EP1215208B1 (en) | 1997-10-27 | 2006-07-12 | Agouron Pharmaceuticals, Inc. | 4-Aminothiazole derivatives, their preparation and their use as inhibitors of cyclin-dependent kinases |
| CZ20024176A3 (cs) | 2000-06-22 | 2004-01-14 | Pfizer Inc. | Způsob výroby pyrazolopyrimidinonů |
| WO2003068773A1 (en) * | 2002-02-12 | 2003-08-21 | Glaxo Group Limited | Pyrazolopyridine derivatives |
| DE102004061288A1 (de) * | 2004-12-14 | 2006-06-29 | Schering Ag | 3-Amino-Pyrazolo[3,4b]pyridine als Inhibitoren von Proteintyrosinkinasen, deren Herstellung und Verwendung als Arzneimittel |
| MX2008002385A (es) * | 2005-08-25 | 2008-03-18 | Hoffmann La Roche | Inhibidores de proteinas cinasas activads por mitogenos p38 y metodos para utilizarlos. |
| EP2044068A4 (en) | 2006-07-17 | 2010-07-21 | Merck Sharp & Dohme | 1-HYDROXY Naphthyridine Compounds as Anti- HIV Drugs |
| DK2120932T3 (da) | 2006-12-20 | 2014-10-13 | Nerviano Medical Sciences Srl | Indazolderivater som kinasehæmmere til behandling af kræft |
| SG183049A1 (en) | 2007-07-20 | 2012-08-30 | Nerviano Medical Sciences Srl | Substituted indazole derivatives active as kinase inhibitors |
| US8354399B2 (en) | 2008-12-18 | 2013-01-15 | Nerviano Medical Sciences S.R.L. | Substituted indazole derivatives active as kinase inhibitors |
| FR2970967B1 (fr) * | 2011-01-27 | 2013-02-15 | Pf Medicament | Derives de type azaindazole ou diazaindazole comme medicament |
-
2011
- 2011-01-27 FR FR1150651A patent/FR2970967B1/fr active Active
-
2012
- 2012-01-20 TW TW101102531A patent/TWI546303B/zh active
- 2012-01-27 TR TR2018/02944T patent/TR201802944T4/tr unknown
- 2012-01-27 AR ARP120100272A patent/AR084935A1/es active IP Right Grant
- 2012-01-27 DK DK12701884.4T patent/DK2668184T3/en active
- 2012-01-27 RU RU2013138624/04A patent/RU2600976C2/ru active
- 2012-01-27 HR HRP20180524TT patent/HRP20180524T1/hr unknown
- 2012-01-27 PL PL12701884T patent/PL2668184T3/pl unknown
- 2012-01-27 KR KR1020187031264A patent/KR20180122028A/ko not_active Ceased
- 2012-01-27 JP JP2013550886A patent/JP5931926B2/ja active Active
- 2012-01-27 SI SI201231273T patent/SI2668184T1/en unknown
- 2012-01-27 BR BR112013018852-9A patent/BR112013018852B1/pt not_active IP Right Cessation
- 2012-01-27 EP EP12701884.4A patent/EP2668184B1/en active Active
- 2012-01-27 UA UAA201310425A patent/UA109698C2/ru unknown
- 2012-01-27 CN CN201280006671.8A patent/CN103339129B/zh active Active
- 2012-01-27 MY MYPI2013002799A patent/MY180666A/en unknown
- 2012-01-27 PT PT127018844T patent/PT2668184T/pt unknown
- 2012-01-27 CA CA2823824A patent/CA2823824C/en active Active
- 2012-01-27 WO PCT/EP2012/051283 patent/WO2012101239A1/en not_active Ceased
- 2012-01-27 ES ES12701884.4T patent/ES2661695T3/es active Active
- 2012-01-27 HU HUE12701884A patent/HUE037153T2/hu unknown
- 2012-01-27 RS RS20180418A patent/RS57101B1/sr unknown
- 2012-01-27 MX MX2013008673A patent/MX356411B/es active IP Right Grant
- 2012-01-27 MA MA36177A patent/MA34903B1/fr unknown
- 2012-01-27 KR KR1020137022330A patent/KR101923751B1/ko not_active Expired - Fee Related
- 2012-01-27 US US13/823,658 patent/US20130172360A1/en not_active Abandoned
- 2012-01-27 AU AU2012210467A patent/AU2012210467B2/en not_active Ceased
- 2012-01-27 LT LTEP12701884.4T patent/LT2668184T/lt unknown
- 2012-11-27 US US13/686,334 patent/US8883821B2/en active Active
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2013
- 2013-07-11 TN TNP2013000293A patent/TN2013000293A1/fr unknown
- 2013-07-16 IL IL227496A patent/IL227496B/en active IP Right Grant
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2018
- 2018-02-26 IL IL257748A patent/IL257748B/en active IP Right Grant
- 2018-03-26 CY CY20181100338T patent/CY1120088T1/el unknown