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 |
|---|---|---|---|
| EP09003075.0 | 2009-03-04 | ||
| EP09003075 | 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 (44)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2013002446A (es) * | 2010-09-03 | 2013-04-08 | Gruenenthal Gmbh | Derivados de tetrahidropirrolopirazina sustituidos. |
| 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 |
| PL2861566T3 (pl) | 2012-06-13 | 2017-06-30 | F.Hoffmann-La Roche Ag | Nowy diazaspirocykloalkan i azaspirocykloalkan |
| UA125503C2 (uk) | 2012-06-13 | 2022-04-13 | Інсайт Холдинґс Корпорейшн | Заміщені трициклічні сполуки як інгібітори fgfr |
| 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 |
| MY181497A (en) | 2013-04-19 | 2020-12-23 | Incyte Holdings Corp | Bicyclic heterocycles as fgfr inhibitors |
| AR098414A1 (es) | 2013-11-14 | 2016-05-26 | Bristol Myers Squibb Co | PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e |
| HUE036117T2 (hu) | 2013-11-26 | 2018-06-28 | Hoffmann La Roche | Oktahidro-ciklobuta[1,2-C;3,4-C']dipirrol származékok, mint autotaxin inhibitorok |
| EA037928B1 (ru) | 2014-03-26 | 2021-06-08 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов продукции аутотаксина (atx) и лизофосфатидиловой кислоты (lpa) |
| JP6554481B2 (ja) | 2014-03-26 | 2019-07-31 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | オートタキシン(atx)及びリゾホスファチジン酸(lpa)産生の阻害剤としての縮合[1,4]ジアゼピン化合物 |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| US9580423B2 (en) | 2015-02-20 | 2017-02-28 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| CR20170390A (es) | 2015-02-20 | 2017-10-23 | Incyte Holdings Corp | Heterociclos biciclicos como inhibidores de fgfr |
| MA41551A (fr) | 2015-02-20 | 2017-12-26 | Incyte Corp | Hétérocycles bicycliques utilisés en tant qu'inhibiteurs de fgfr4 |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| CR20180058A (es) | 2015-09-04 | 2018-02-26 | Hoffmann La Roche | Nuevos derivados de fenoximetilo |
| MX2017015034A (es) | 2015-09-24 | 2018-04-13 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de autotaxina (atx)/anhidrasa carbonica (ca). |
| KR20180054830A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서의 이환형 화합물 |
| CN107922412B (zh) | 2015-09-24 | 2021-02-23 | 豪夫迈·罗氏有限公司 | 作为atx抑制剂的二环化合物 |
| EP3353178B1 (en) | 2015-09-24 | 2021-07-14 | F. Hoffmann-La Roche AG | Bicyclic compounds as dual atx/ca inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| EP3596060B1 (en) | 2017-03-16 | 2023-09-20 | F. Hoffmann-La Roche AG | New bicyclic compounds as atx inhibitors |
| RU2019132254A (ru) | 2017-03-16 | 2021-04-16 | Ф. Хоффманн-Ля Рош Аг | Гетероциклические соединения, пригодные в качестве дуальных ингибиторов atx/ca |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| KR102526964B1 (ko) | 2018-02-26 | 2023-04-28 | 길리애드 사이언시즈, 인코포레이티드 | Hbv 복제 억제제로서의 치환된 피롤리진 화합물 |
| BR112020022392A2 (pt) | 2018-05-04 | 2021-02-02 | Incyte Corporation | formas sólidas de um inibidor de fgfr e processos para preparação das mesmas |
| PE20210919A1 (es) | 2018-05-04 | 2021-05-19 | Incyte Corp | Sales de un inhibidor de fgfr |
| US11628162B2 (en) | 2019-03-08 | 2023-04-18 | Incyte Corporation | Methods of treating cancer with an FGFR inhibitor |
| 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 |
| GEP20247679B (en) | 2019-10-14 | 2024-10-10 | Incyte Corp | Bicyclic heterocycles as fgfr inhibitors |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| 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 |
| PE20221504A1 (es) | 2019-12-04 | 2022-09-30 | Incyte Corp | Derivados de un inhibidor de fgfr |
| WO2021146424A1 (en) | 2020-01-15 | 2021-07-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TW202304459A (zh) | 2021-04-12 | 2023-02-01 | 美商英塞特公司 | 包含fgfr抑制劑及nectin-4靶向劑之組合療法 |
| CA3220155A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| TW202313611A (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 |
| CN121175287A (zh) * | 2023-03-29 | 2025-12-19 | 安道麦阿甘有限公司 | 用于制备胺中间体的方法 |
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 |
| WO2007124423A2 (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 |
| PT2066659E (pt) * | 2006-09-29 | 2013-11-07 | Gruenenthal Gmbh | Derivados de sulfonamida substituídos |
| WO2008046573A1 (de) | 2006-10-16 | 2008-04-24 | Grünenthal GmbH | Substituierte sulfonamid-derivate als bradykinin 1 rezeptor modulatoren |
| EP2170350B1 (en) * | 2007-06-21 | 2013-09-11 | Cara Therapeutics, Inc. | Substituted imidazoheterocycles |
-
2010
- 2010-02-26 TW TW099105566A patent/TW201035102A/zh unknown
- 2010-03-03 BR BRPI1010533A patent/BRPI1010533A2/pt not_active IP Right Cessation
- 2010-03-03 RU RU2011140061/04A patent/RU2011140061A/ru not_active Application Discontinuation
- 2010-03-03 WO PCT/EP2010/001299 patent/WO2010099938A1/en not_active Ceased
- 2010-03-03 PL PL10708496T patent/PL2403854T3/pl unknown
- 2010-03-03 EP EP10708496.4A patent/EP2403854B1/en not_active Not-in-force
- 2010-03-03 ES ES10708496.4T patent/ES2437108T3/es active Active
- 2010-03-03 CN CN2010800106612A patent/CN102341398A/zh active Pending
- 2010-03-03 MX MX2011008864A patent/MX305105B/es active IP Right Grant
- 2010-03-03 AU AU2010220561A patent/AU2010220561A1/en not_active Abandoned
- 2010-03-03 JP JP2011552360A patent/JP2012519196A/ja not_active Withdrawn
- 2010-03-03 CA CA2754330A patent/CA2754330A1/en not_active Abandoned
- 2010-03-04 US US12/717,625 patent/US8158628B2/en not_active Expired - Fee Related
- 2010-03-04 AR ARP100100647A patent/AR075539A1/es not_active Application Discontinuation
-
2011
- 2011-09-01 IL IL214911A patent/IL214911A0/en unknown
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