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 (https=) | 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 (https=) |
| EP (1) | EP2403854B1 (https=) |
| JP (1) | JP2012519196A (https=) |
| CN (1) | CN102341398A (https=) |
| AR (1) | AR075539A1 (https=) |
| AU (1) | AU2010220561A1 (https=) |
| BR (1) | BRPI1010533A2 (https=) |
| CA (1) | CA2754330A1 (https=) |
| ES (1) | ES2437108T3 (https=) |
| IL (1) | IL214911A0 (https=) |
| MX (1) | MX305105B (https=) |
| PL (1) | PL2403854T3 (https=) |
| RU (1) | RU2011140061A (https=) |
| TW (1) | TW201035102A (https=) |
| WO (1) | WO2010099938A1 (https=) |
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 |
| US8754114B2 (en) | 2010-12-22 | 2014-06-17 | 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 |
| ES2704744T3 (es) | 2012-06-13 | 2019-03-19 | Incyte Holdings Corp | Compuestos tricíclicos sustituidos como inhibidores de FGFR |
| IN2014DN09346A (https=) | 2012-06-13 | 2015-07-17 | Hoffmann La Roche | |
| US9388185B2 (en) | 2012-08-10 | 2016-07-12 | Incyte Holdings Corporation | Substituted pyrrolo[2,3-b]pyrazines as FGFR inhibitors |
| KR102179599B1 (ko) | 2012-09-25 | 2020-11-19 | 에프. 호프만-라 로슈 아게 | 이환형 유도체 |
| 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 |
| EA035095B1 (ru) | 2013-04-19 | 2020-04-27 | Инсайт Холдингс Корпорейшн | Бициклические гетероциклы в качестве ингибиторов fgfr |
| AR098414A1 (es) | 2013-11-14 | 2016-05-26 | Bristol Myers Squibb Co | PIPERAZINAS DE PIRAZOLO SUSTITUIDO COMO INHIBIDORES DE CASEÍNA QUINASA 1 d/e |
| CN105764905B (zh) | 2013-11-26 | 2019-06-07 | 豪夫迈·罗氏有限公司 | 新的八氢-环丁二烯并[1，2-c；3，4-c’]二吡咯-2基 |
| CN106103446B (zh) | 2014-03-26 | 2019-07-30 | 豪夫迈·罗氏有限公司 | 作为自分泌运动因子(atx)和溶血磷脂酸(lpa)生产抑制剂的二环化合物 |
| WO2015144609A1 (en) | 2014-03-26 | 2015-10-01 | F. Hoffmann-La Roche Ag | Condensed [1,4]diazepine compounds as autotaxin (atx) and lysophosphatidic acid (lpa) production inhibitors |
| US10851105B2 (en) | 2014-10-22 | 2020-12-01 | Incyte Corporation | Bicyclic heterocycles as FGFR4 inhibitors |
| WO2016134294A1 (en) | 2015-02-20 | 2016-08-25 | 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 |
| MX373169B (es) | 2015-02-20 | 2020-04-24 | Incyte Holdings Corp | Heterociclos bicíclicos como inhibidores de receptores del factor de crecimiento fibroblástico (fgfr). |
| MA41898A (fr) | 2015-04-10 | 2018-02-13 | Hoffmann La Roche | Dérivés de quinazolinone bicyclique |
| CA2992889A1 (en) | 2015-09-04 | 2017-03-09 | F. Hoffmann-La Roche Ag | Phenoxymethyl derivatives |
| KR20180054830A (ko) | 2015-09-24 | 2018-05-24 | 에프. 호프만-라 로슈 아게 | 오토탁신(atx) 억제제로서의 이환형 화합물 |
| RU2018112230A (ru) | 2015-09-24 | 2019-10-30 | Ф. Хоффманн-Ля Рош Аг | Бициклические соединения в качестве ингибиторов atx |
| CR20180057A (es) | 2015-09-24 | 2018-04-02 | Hoffmann La Roche | Nuevos compuestos biciclicos como inhibidores duales de atx/ca. |
| AU2016328365B2 (en) | 2015-09-24 | 2020-04-23 | F. Hoffmann-La Roche Ag | New bicyclic compounds as dual ATX/CA inhibitors |
| JOP20190024A1 (ar) | 2016-08-26 | 2019-02-19 | Gilead Sciences Inc | مركبات بيروليزين بها استبدال واستخداماتها |
| WO2018167113A1 (en) | 2017-03-16 | 2018-09-20 | F. Hoffmann-La Roche Ag | New bicyclic compounds as atx inhibitors |
| SG11201908560SA (en) | 2017-03-16 | 2019-10-30 | Hoffmann La Roche | Heterocyclic compounds useful as dual atx/ca inhibitors |
| AR111960A1 (es) | 2017-05-26 | 2019-09-04 | Incyte Corp | Formas cristalinas de un inhibidor de fgfr y procesos para su preparación |
| PL3759109T3 (pl) | 2018-02-26 | 2024-03-04 | Gilead Sciences, Inc. | Podstawione związki pirolizyny jako inhibitory replikacji hbv |
| MA52493A (fr) | 2018-05-04 | 2021-03-10 | Incyte Corp | Sels d'un inhibiteur de fgfr |
| CR20200590A (es) | 2018-05-04 | 2021-04-26 | Incyte Corp | Formas sólidas de un inhibidor de fgfr y procesos para prepararlas |
| 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 |
| WO2021067374A1 (en) | 2019-10-01 | 2021-04-08 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| TWI891666B (zh) | 2019-10-14 | 2025-08-01 | 美商英塞特公司 | 作為ｆｇｆｒ抑制劑之雙環雜環 |
| WO2021076728A1 (en) | 2019-10-16 | 2021-04-22 | Incyte Corporation | Bicyclic heterocycles as fgfr inhibitors |
| BR112022010664A2 (pt) | 2019-12-04 | 2022-08-16 | Incyte Corp | Derivados de um inibidor de fgfr |
| EP4069696A1 (en) | 2019-12-04 | 2022-10-12 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| 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 |
| WO2022261159A1 (en) | 2021-06-09 | 2022-12-15 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| EP4352059A1 (en) | 2021-06-09 | 2024-04-17 | Incyte Corporation | Tricyclic heterocycles as fgfr inhibitors |
| 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 |
| 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 |
|---|---|---|---|---|
| WO2006068928A1 (en) * | 2004-12-20 | 2006-06-29 | 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 |
| US8097626B2 (en) * | 2006-04-21 | 2012-01-17 | Glaxosmithkline Llc | IL-8 receptor antagonists |
| WO2007140383A2 (en) | 2006-05-30 | 2007-12-06 | Neurogen Corporation | Spirocyclic sulfonamides and related compounds |
| EP2383267A1 (de) * | 2006-09-29 | 2011-11-02 | Grünenthal GmbH | Substituierte Sulfonamid-Derivate |
| EP2086935A1 (de) | 2006-10-16 | 2009-08-12 | 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 PL PL10708496T patent/PL2403854T3/pl unknown
- 2010-03-03 MX MX2011008864A patent/MX305105B/es active IP Right Grant
- 2010-03-03 CN CN2010800106612A patent/CN102341398A/zh active Pending
- 2010-03-03 AU AU2010220561A patent/AU2010220561A1/en not_active Abandoned
- 2010-03-03 CA CA2754330A patent/CA2754330A1/en not_active Abandoned
- 2010-03-03 EP EP10708496.4A patent/EP2403854B1/en not_active Not-in-force
- 2010-03-03 WO PCT/EP2010/001299 patent/WO2010099938A1/en not_active Ceased
- 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 ES ES10708496.4T patent/ES2437108T3/es active Active
- 2010-03-03 JP JP2011552360A patent/JP2012519196A/ja not_active Withdrawn
- 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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