JP2012519196A5 - - Google Patents
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- JP2012519196A5 JP2012519196A5 JP2011552360A JP2011552360A JP2012519196A5 JP 2012519196 A5 JP2012519196 A5 JP 2012519196A5 JP 2011552360 A JP2011552360 A JP 2011552360A JP 2011552360 A JP2011552360 A JP 2011552360A JP 2012519196 A5 JP2012519196 A5 JP 2012519196A5
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- JP
- Japan
- Prior art keywords
- mmol
- dcm
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- 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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- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- 239000000243 solution Substances 0.000 description 3
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 2
- 239000011541 reaction mixture Substances 0.000 description 2
- 229920006395 saturated elastomer Polymers 0.000 description 2
- 239000007821 HATU Substances 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- PNEYBMLMFCGWSK-UHFFFAOYSA-N aluminium oxide Inorganic materials [O-2].[O-2].[O-2].[Al+3].[Al+3] PNEYBMLMFCGWSK-UHFFFAOYSA-N 0.000 description 1
- 150000001412 amines Chemical class 0.000 description 1
- 239000012267 brine Substances 0.000 description 1
- 238000004440 column chromatography Methods 0.000 description 1
- 239000012043 crude product Substances 0.000 description 1
- 230000007935 neutral effect Effects 0.000 description 1
- 239000012044 organic layer Substances 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- HPALAKNZSZLMCH-UHFFFAOYSA-M sodium;chloride;hydrate Chemical compound O.[Na+].[Cl-] HPALAKNZSZLMCH-UHFFFAOYSA-M 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09003075 | 2009-03-04 | ||
| EP09003075.0 | 2009-03-04 | ||
| PCT/EP2010/001299 WO2010099938A1 (en) | 2009-03-04 | 2010-03-03 | Sulfonylated tetrahydroazolopyrazines and their use as medicinal products |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012519196A JP2012519196A (ja) | 2012-08-23 |
| JP2012519196A5 true JP2012519196A5 (enExample) | 2013-04-18 |
Family
ID=40716949
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011552360A Withdrawn JP2012519196A (ja) | 2009-03-04 | 2010-03-03 | スルホニル化されたテトラヒドロアゾロピラジンおよびその医薬としての使用 |
Country Status (15)
| Country | Link |
|---|---|
| US (1) | US8158628B2 (enExample) |
| EP (1) | EP2403854B1 (enExample) |
| JP (1) | JP2012519196A (enExample) |
| CN (1) | CN102341398A (enExample) |
| AR (1) | AR075539A1 (enExample) |
| AU (1) | AU2010220561A1 (enExample) |
| BR (1) | BRPI1010533A2 (enExample) |
| CA (1) | CA2754330A1 (enExample) |
| ES (1) | ES2437108T3 (enExample) |
| IL (1) | IL214911A0 (enExample) |
| MX (1) | MX305105B (enExample) |
| PL (1) | PL2403854T3 (enExample) |
| RU (1) | RU2011140061A (enExample) |
| TW (1) | TW201035102A (enExample) |
| WO (1) | WO2010099938A1 (enExample) |
Families Citing this family (45)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2012028331A1 (en) * | 2010-09-03 | 2012-03-08 | Grünenthal GmbH | Substituted tetrahydropyrrolopyrazine derivatives |
| WO2012088266A2 (en) | 2010-12-22 | 2012-06-28 | Incyte Corporation | Substituted imidazopyridazines and benzimidazoles as inhibitors of fgfr3 |
| DE102011082013A1 (de) * | 2011-09-01 | 2013-03-07 | Bayer Pharma AG | 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine |
| CA2876689C (en) | 2012-06-13 | 2022-04-26 | Incyte Corporation | Substituted tricyclic compounds as fgfr inhibitors |
| SI2861566T1 (sl) * | 2012-06-13 | 2017-03-31 | F. Hoffmann-La Roche Ag | Novi diazaspirocikloalkan in azaspirocikloalkan |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| PL2900669T3 (pl) | 2012-09-25 | 2020-01-31 | F. Hoffmann-La Roche Ag | Pochodne heksahydropirolo[3,4-C]pirolu i związki pokrewne jako inhibitory autotaksyny (ATX) oraz inhibitory produkcji kwasu lizofosfatydowego (LPA) do leczenia np. chorób nerek |
| US9266892B2 (en) | 2012-12-19 | 2016-02-23 | Incyte Holdings Corporation | Fused pyrazoles as FGFR inhibitors |
| CN103113324B (zh) * | 2013-02-07 | 2015-08-05 | 浙江工业大学 | 一种n-磺酰基取代的四氢吡咯类化合物的制备方法 |
| AR095079A1 (es) | 2013-03-12 | 2015-09-16 | Hoffmann La Roche | Derivados de octahidro-pirrolo[3,4-c]-pirrol y piridina-fenilo |
| PH12015502383B1 (en) | 2013-04-19 | 2023-02-03 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| UY35834A (es) | 2013-11-14 | 2015-05-29 | Bristol Myers Squibb Company Una Corporación Del Estado De Delaware | Piperazinas de pirazolo sustituido como inhibidores de caseína quinasa 1 delta y epsilon |
| AU2014356583B2 (en) | 2013-11-26 | 2019-02-28 | F. Hoffmann-La Roche Ag | New octahydro-cyclobuta (1,2-c;3,4-c')dipyrrol-2-yl |
| CR20160418A (es) | 2014-03-26 | 2016-11-07 | Hoffmann La Roche | Nuevos compuestos biciclicos de 7 eslabones |
| MA50635A (fr) | 2014-03-26 | 2020-08-12 | Hoffmann La Roche | Nouveaux composés bicycliques comme inhibiteurs de la production d'autotaxin (atx) et de l'acide lysophosphatidique |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| CA2976790C (en) | 2015-02-20 | 2024-02-27 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| EP3344619B1 (en) | 2015-09-04 | 2020-10-28 | H. Hoffnabb-La Roche Ag | Phenoxymethyl derivatives |
| MA42918A (fr) | 2015-09-24 | 2018-08-01 | Hoffmann La Roche | Composés bicycliques utilisés en tant qu'inhibiteurs d'atx |
| BR112018006080A2 (pt) | 2015-09-24 | 2018-10-09 | F. Hoffmann-La Roche Ag | novos compostos bicíclicos como inibidores de dupla ação de atx/ca |
| WO2017050747A1 (en) | 2015-09-24 | 2017-03-30 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual atx/ca inhibitors |
| AU2016328437A1 (en) | 2015-09-24 | 2018-01-25 | F. Hoffmann-La Roche Ag | Bicyclic compounds as ATX inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| JP7050165B2 (ja) | 2018-02-26 | 2022-04-07 | ギリアード サイエンシーズ， インコーポレイテッド | Ｈｂｖ複製阻害剤としての置換ピロリジン化合物 |
| KR102956194B1 (ko) | 2018-05-04 | 2026-04-23 | 인사이트 코포레이션 | Fgfr 억제제의 염 |
| RS66310B1 (sr) | 2018-05-04 | 2025-01-31 | Incyte Corp | Čvrsti oblici inhibitora fgfr i procesi za njegovu pripremu |
| WO2020185532A1 (en) | 2019-03-08 | 2020-09-17 | Incyte Corporation | Methods of treating cancer with an fgfr inhibitor |
| WO2021007269A1 (en) | 2019-07-09 | 2021-01-14 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| US12122767B2 (en) | 2019-10-01 | 2024-10-22 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| US11566028B2 (en) | 2019-10-16 | 2023-01-31 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| MX2022006691A (es) | 2019-12-04 | 2022-09-19 | Incyte Corp | Derivados de un inhibidor de receptores del factor de crecimiento de fibroblastos (fgfr). |
| WO2021113479A1 (en) | 2019-12-04 | 2021-06-10 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| US12012409B2 (en) | 2020-01-15 | 2024-06-18 | Incyte Corporation | Bicyclic heterocycles as FGFR inhibitors |
| EP4323405A1 (en) | 2021-04-12 | 2024-02-21 | Incyte Corporation | Combination therapy comprising an fgfr inhibitor and a nectin-4 targeting agent |
| CA3220274A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313610A (zh) | 2021-06-09 | 2023-04-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之三環雜環 |
| WO2024201469A1 (en) * | 2023-03-29 | 2024-10-03 | Adama Agan Ltd. | Process for the preparation of amine intermediates |
| CN119490446A (zh) * | 2024-09-23 | 2025-02-21 | 苏州艾缇克药物化学有限公司 | 一种左旋舒必利的重要中间体(S)-2-Boc-氨甲基吡咯烷的合成方法 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7563793B2 (en) * | 2004-12-20 | 2009-07-21 | Wyeth | Pyrrolo[1,2-a]quinoxalin-5-(4H)-yl)sulfonyls and carbonyls and their use as estrogenic agents |
| WO2007101007A2 (en) | 2006-02-23 | 2007-09-07 | Neurogen Corporation | Aryl sulfonyl heterocycles |
| CA2650007A1 (en) * | 2006-04-21 | 2007-11-01 | Smithkline Beecham Corporation | Il-8 receptor antagonists |
| WO2007140383A2 (en) | 2006-05-30 | 2007-12-06 | Neurogen Corporation | Spirocyclic sulfonamides and related compounds |
| BRPI0714764A2 (pt) * | 2006-09-29 | 2014-12-30 | Gruenenthal Gmbh | Derivados substituídos de sulfonamida |
| EP2086935A1 (de) | 2006-10-16 | 2009-08-12 | Grünenthal GmbH | Substituierte sulfonamid-derivate als bradykinin 1 rezeptor modulatoren |
| EA201000046A1 (ru) * | 2007-06-21 | 2011-02-28 | Кара Терапеутикс, Инк. | Замещенные имидазогетероциклы |
-
2010
- 2010-02-26 TW TW099105566A patent/TW201035102A/zh unknown
- 2010-03-03 AU AU2010220561A patent/AU2010220561A1/en not_active Abandoned
- 2010-03-03 CN CN2010800106612A patent/CN102341398A/zh active Pending
- 2010-03-03 JP JP2011552360A patent/JP2012519196A/ja not_active Withdrawn
- 2010-03-03 BR BRPI1010533A patent/BRPI1010533A2/pt not_active IP Right Cessation
- 2010-03-03 ES ES10708496.4T patent/ES2437108T3/es active Active
- 2010-03-03 WO PCT/EP2010/001299 patent/WO2010099938A1/en not_active Ceased
- 2010-03-03 CA CA2754330A patent/CA2754330A1/en not_active Abandoned
- 2010-03-03 MX MX2011008864A patent/MX305105B/es active IP Right Grant
- 2010-03-03 EP EP10708496.4A patent/EP2403854B1/en not_active Not-in-force
- 2010-03-03 PL PL10708496T patent/PL2403854T3/pl unknown
- 2010-03-03 RU RU2011140061/04A patent/RU2011140061A/ru not_active Application Discontinuation
- 2010-03-04 AR ARP100100647A patent/AR075539A1/es not_active Application Discontinuation
- 2010-03-04 US US12/717,625 patent/US8158628B2/en not_active Expired - Fee Related
-
2011
- 2011-09-01 IL IL214911A patent/IL214911A0/en unknown
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