JP2011530500A5 - - Google Patents
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- Publication number
- JP2011530500A5 JP2011530500A5 JP2011521675A JP2011521675A JP2011530500A5 JP 2011530500 A5 JP2011530500 A5 JP 2011530500A5 JP 2011521675 A JP2011521675 A JP 2011521675A JP 2011521675 A JP2011521675 A JP 2011521675A JP 2011530500 A5 JP2011530500 A5 JP 2011530500A5
- Authority
- JP
- Japan
- Prior art keywords
- chlorine
- fluorine
- alkyl
- group
- further substituted
- 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
Links
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical group [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims 45
- PXGOKWXKJXAPGV-UHFFFAOYSA-N Fluorine Chemical group FF PXGOKWXKJXAPGV-UHFFFAOYSA-N 0.000 claims 45
- 239000000460 chlorine Chemical group 0.000 claims 45
- 229910052801 chlorine Inorganic materials 0.000 claims 45
- 229910052731 fluorine Inorganic materials 0.000 claims 45
- 239000011737 fluorine Chemical group 0.000 claims 45
- 125000004093 cyano group Chemical group *C#N 0.000 claims 36
- 125000000623 heterocyclic group Chemical group 0.000 claims 25
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 claims 20
- 150000001875 compounds Chemical class 0.000 claims 20
- 229910052739 hydrogen Inorganic materials 0.000 claims 19
- 239000001257 hydrogen Substances 0.000 claims 19
- 150000003839 salts Chemical class 0.000 claims 18
- 125000006413 ring segment Chemical group 0.000 claims 16
- 150000002431 hydrogen Chemical group 0.000 claims 12
- 125000004474 heteroalkylene group Chemical group 0.000 claims 9
- 125000003161 (C1-C6) alkylene group Chemical group 0.000 claims 8
- 125000006714 (C3-C10) heterocyclyl group Chemical group 0.000 claims 8
- 125000006570 (C5-C6) heteroaryl group Chemical group 0.000 claims 8
- 125000001313 C5-C10 heteroaryl group Chemical group 0.000 claims 8
- 229910052757 nitrogen Inorganic materials 0.000 claims 8
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 7
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 6
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 6
- 125000002619 bicyclic group Chemical group 0.000 claims 6
- 125000004122 cyclic group Chemical group 0.000 claims 6
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 6
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 6
- 229910052799 carbon Inorganic materials 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- -1 (b) C 1 -C 6 alkyl Chemical group 0.000 claims 3
- 125000001072 heteroaryl group Chemical group 0.000 claims 3
- 125000003386 piperidinyl group Chemical group 0.000 claims 3
- 125000006163 5-membered heteroaryl group Chemical group 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- GOJUJUVQIVIZAV-UHFFFAOYSA-N 2-amino-4,6-dichloropyrimidine-5-carbaldehyde Chemical group NC1=NC(Cl)=C(C=O)C(Cl)=N1 GOJUJUVQIVIZAV-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 125000005842 heteroatom Chemical group 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8673208P | 2008-08-06 | 2008-08-06 | |
| US61/086,732 | 2008-08-06 | ||
| US22942809P | 2009-07-29 | 2009-07-29 | |
| US61/229,428 | 2009-07-29 | ||
| PCT/IB2009/053389 WO2010016005A1 (en) | 2008-08-06 | 2009-08-04 | 6 substituted 2-heterocyclylamino pyrazine compounds as chk-1 inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011530500A JP2011530500A (ja) | 2011-12-22 |
| JP2011530500A5 true JP2011530500A5 (OSRAM) | 2012-09-13 |
| JP5576370B2 JP5576370B2 (ja) | 2014-08-20 |
Family
ID=41171261
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011521675A Expired - Fee Related JP5576370B2 (ja) | 2008-08-06 | 2009-08-04 | Ｃｈｋ−１阻害剤としての６置換２−ヘテロシクリルアミノピラジン化合物 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US8518952B2 (OSRAM) |
| EP (1) | EP2328890B1 (OSRAM) |
| JP (1) | JP5576370B2 (OSRAM) |
| AT (1) | ATE542813T1 (OSRAM) |
| CA (1) | CA2731368C (OSRAM) |
| ES (1) | ES2378513T3 (OSRAM) |
| WO (1) | WO2010016005A1 (OSRAM) |
Families Citing this family (53)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| MX2011006503A (es) | 2008-12-19 | 2011-09-06 | Vertex Pharma | Derivados de pirazina utiles como inhibidores de la cinasa de atr. |
| CA2755285C (en) * | 2009-03-20 | 2014-02-11 | Yunxin Y. Bo | Inhibitors of pi3 kinase |
| EA020847B1 (ru) | 2009-10-30 | 2015-02-27 | Янссен Фармацевтика Нв | ПРОИЗВОДНЫЕ ИМИДАЗО[1,2-b]ПИРИДАЗИНА И ИХ ПРИМЕНЕНИЕ В КАЧЕСТВЕ ИНГИБИТОРОВ PDE10 |
| EP2338888A1 (en) * | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| EP2360158A1 (en) * | 2010-02-18 | 2011-08-24 | Almirall, S.A. | Pyrazole derivatives as jak inhibitors |
| UY33213A (es) | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| AR080754A1 (es) | 2010-03-09 | 2012-05-09 | Janssen Pharmaceutica Nv | Derivados de imidazo (1,2-a) pirazina y su uso como inhibidores de pde10 |
| US8247436B2 (en) | 2010-03-19 | 2012-08-21 | Novartis Ag | Pyridine and pyrazine derivative for the treatment of CF |
| NZ603477A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | Compounds useful as inhibitors of atr kinase |
| WO2011143425A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| WO2013000924A1 (en) | 2011-06-27 | 2013-01-03 | Janssen Pharmaceutica Nv | 1-ARYL-4-METHYL-[1,2,4]TRIAZOLO[4,3-a]QUINOXALINE DERIVATIVES |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| CA2850491C (en) | 2011-09-30 | 2020-10-27 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors |
| CN106496173A (zh) | 2011-09-30 | 2017-03-15 | 沃泰克斯药物股份有限公司 | 用于制备可用作atr激酶抑制剂的化合物的方法 |
| EP2773207B1 (en) | 2011-10-31 | 2018-03-07 | Merck Sharp & Dohme Corp. | Aminopyrimidinones as interleukin receptor-associated kinase inhibitors |
| WO2013152298A1 (en) | 2012-04-05 | 2013-10-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| EP2863909B1 (en) | 2012-06-26 | 2020-11-04 | Janssen Pharmaceutica N.V. | Combinations comprising 4-methyl-[1,2,4]triazolo[4,3-a]quinoxaline compounds as pde 2 inhibitors and pde 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| MX362197B (es) | 2012-07-09 | 2019-01-08 | Janssen Pharmaceutica Nv | Derivados de imidazo[1,2-b]piridazina e imidazo[1,2-a]pirazina como inhibidores de la fosfodiesterasa 10; y el uso de los mismos en el tratamiento de trastornos neurológicos, psiquiátricos y metabólicos. |
| DK2904406T3 (en) | 2012-10-04 | 2018-06-18 | Vertex Pharma | METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE |
| DK2922828T3 (da) | 2012-11-21 | 2020-08-31 | Ptc Therapeutics Inc | 4,6-diamino-pyrimidin-derivater som bmi-1-inhibitorer til at behandle cancer |
| CN103254121B (zh) * | 2013-04-08 | 2015-08-26 | 洛阳师范学院 | 一种合成(3r,4r)-n-pg-4-甲基-3-甲胺基哌啶的方法 |
| US10584115B2 (en) * | 2013-11-21 | 2020-03-10 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine BMI-1 inhibitors |
| ME02883B (me) | 2013-12-05 | 2018-04-20 | Pfizer | PIROLO[2,3-d]PIRIMIDINIL-, PIROLO[2,3-b]PIRAZINIL- I PIROLO[2,3-d] PIRIDINILAKRILAMIDI |
| US9145393B2 (en) * | 2014-01-24 | 2015-09-29 | Confluence Life Sciences, Inc. | Arylpyridinone ITK inhibitors for treating inflammation and cancer |
| US9758518B2 (en) | 2015-03-04 | 2017-09-12 | Pimera, Inc. | Compositions, uses and methods for making them |
| CN106459068B (zh) | 2014-05-09 | 2019-01-22 | 皮梅拉股份有限公司 | 新组合物、用途和制备它们的方法 |
| KR20170103838A (ko) | 2015-01-23 | 2017-09-13 | 컨플루언스 라이프 사이언시스, 인코포레이티드 | 염증 및 암의 치료를 위한 헤테로시클릭 itk 저해제 |
| JP6761815B2 (ja) | 2015-05-01 | 2020-09-30 | ファイザー・インク | ピロロ［２，３−ｄ］ピリミジニル、ピロロ［２，３−ｂ］ピラジニル、ピロロ［２，３−ｂ］ピリジニルアクリルアミド、およびそのエポキシド |
| CN105130991B (zh) * | 2015-07-10 | 2017-09-19 | 成都知普莱生物医药科技有限公司 | 一种合成骨形态发生蛋白受体抑制剂的方法 |
| AU2016331955B2 (en) | 2015-09-30 | 2022-07-21 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA damaging agents and ATR inhibitors |
| MY189118A (en) | 2016-02-24 | 2022-01-26 | Pfizer | Pyrazolo[1,5-a]pyrazin-4-yl derivatives |
| US10316038B2 (en) | 2017-01-25 | 2019-06-11 | Aclaris Therapeutics, Inc. | Pyrrolopyrimidine ITK inhibitors for treating inflammation and cancer |
| CN110709400A (zh) | 2017-03-28 | 2020-01-17 | 皮梅拉股份有限公司 | Pol1抑制剂的新型晶体形式 |
| CN107056681B (zh) * | 2017-03-30 | 2019-10-01 | 广州白云山光华制药股份有限公司 | 一种托法替布中间体的制备方法 |
| EP3668858A1 (en) | 2017-08-14 | 2020-06-24 | Pfizer Inc | Pyrazolo[1,5-a]pyrazin-4-yl and related derivatives |
| CN107474047B (zh) * | 2017-08-29 | 2019-10-29 | 浙江工业大学 | 1,2,4-三唑并杂环类化合物的合成方法 |
| CN107827811B (zh) * | 2017-11-15 | 2021-01-29 | 上海皓伯化工科技有限公司 | 一种制备n-取代-1,2,3,6-四氢吡啶的方法 |
| JP2021151955A (ja) * | 2018-05-22 | 2021-09-30 | 株式会社カネカ | 光学活性−ｃｉｓ−アミノピペリジンの製造方法 |
| WO2019236884A1 (en) * | 2018-06-07 | 2019-12-12 | Disarm Therapeutics, Inc. | Inhibitors of sarm1 |
| EP3608326A1 (en) | 2018-08-10 | 2020-02-12 | Irbm S.P.A. | Tricyclic inhibitors of hepatitis b virus |
| BR112021002630A2 (pt) | 2018-08-17 | 2021-05-11 | Ptc Therapeutics, Inc. | método para tratar câncer pancreático |
| EP3825318A1 (en) | 2019-11-25 | 2021-05-26 | Promidis S.r.l. | Oxalamido-substituted tricyclic inhibitors of hepatitis b virus |
| EP3741762A1 (en) | 2019-05-23 | 2020-11-25 | Irbm S.P.A. | Oxalamido-substituted tricyclic inhibitors of hepatitis b virus |
| UY38705A (es) | 2019-05-23 | 2020-12-31 | Irbm S P A | Inhibidores tricíclicos sustituidos con oxalamido del virus de hepatitis b |
| BR112022025238A2 (pt) * | 2020-06-11 | 2023-02-14 | Chdi Foundation Inc | Compostos heterocíclicos e agentes de imageamento para formar imagem da proteína huntingtina |
| US20230303563A1 (en) * | 2020-07-31 | 2023-09-28 | Children's Hospital Medical Center | Multi-cyclic irak and flt3 inhibiting compounds and uses thereof |
| KR102473645B1 (ko) * | 2020-08-28 | 2022-12-05 | (주)부흥산업사 | (2S,5R)-벤질 5-(t-부톡시카르보닐아미노)-2-메틸피페리딘-1-카르복실레이트의 제조방법 |
| WO2023009833A1 (en) * | 2021-07-30 | 2023-02-02 | Children's Hospital Medical Center | Multi-cyclic irak and flt3 inhibiting compounds and uses thereof |
| JP2025519537A (ja) * | 2022-06-10 | 2025-06-26 | インターライン セラピューティクス インコーポレイテッド | Ｒｉｐｋ２阻害剤としてのイミダゾ（１，２－１）ピリジン誘導体 |
| AR129535A1 (es) | 2022-06-21 | 2024-09-04 | Syngenta Crop Protection Ag | Derivados de carboxamida heterocíclicos bicíclicos microbiocidas |
| CN120476119A (zh) | 2022-10-27 | 2025-08-12 | 先正达农作物保护股份公司 | 杀微生物的杂双环二氢噁二嗪衍生物 |
| CN116478076A (zh) * | 2023-04-26 | 2023-07-25 | 南京优氟医药科技有限公司 | 一种(2s,4s)-1-叔丁氧羰基-2-(二氟甲基)-4-羟基吡咯烷的制备方法 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| GB9518953D0 (en) | 1995-09-15 | 1995-11-15 | Pfizer Ltd | Pharmaceutical formulations |
| WO2000035298A1 (en) | 1996-11-27 | 2000-06-22 | Wm. Wrigley Jr. Company | Chewing gum containing medicament active agents |
| GB9711643D0 (en) | 1997-06-05 | 1997-07-30 | Janssen Pharmaceutica Nv | Glass thermoplastic systems |
| GB9722320D0 (en) | 1997-10-22 | 1997-12-17 | Janssen Pharmaceutica Nv | Human cell cycle checkpoint proteins |
| US6383744B1 (en) | 1998-07-10 | 2002-05-07 | Incyte Genomics, Inc. | Human checkpoint kinase |
| WO2000016781A1 (en) | 1998-09-18 | 2000-03-30 | Smithkline Beecham Corporation | Chk1 kinase inhibitors |
| EE05627B1 (et) | 1998-12-23 | 2013-02-15 | Pfizer Inc. | CTLA-4 vastased inimese monoklonaalsed antikehad |
| ES2302699T3 (es) | 1999-08-27 | 2008-08-01 | Novartis Vaccines And Diagnostics, Inc. | Oligonucleotidos quimericos antisentido y formulaciones de transfeccion celular de los mismos. |
| DE60019318T2 (de) | 1999-09-22 | 2006-03-09 | Canbas Co., Ltd., Numazu | Zusammensetzungen und verfahren zur inhibierung vom zellulären g2-übergang und sensitisierung von zellen gegen dna-schädigenden wirkstoffe |
| US6211164B1 (en) | 2000-03-10 | 2001-04-03 | Abbott Laboratories | Antisense oligonucleotides of the human chk1 gene and uses thereof |
| MA26040A1 (fr) | 2001-01-05 | 2004-04-01 | Pfizer | Des anticorps pour recepteur i de facteur de croissance insulinique |
| UA76977C2 (en) | 2001-03-02 | 2006-10-16 | Icos Corp | Aryl- and heteroaryl substituted chk1 inhibitors and their use as radiosensitizers and chemosensitizers |
| AR039067A1 (es) | 2001-11-09 | 2005-02-09 | Pfizer Prod Inc | Anticuerpos para cd40 |
| US7704995B2 (en) | 2002-05-03 | 2010-04-27 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| WO2003093297A2 (en) * | 2002-05-03 | 2003-11-13 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| CA2512683C (en) | 2003-01-09 | 2010-03-16 | Pfizer Inc. | Tricyclic compounds protein kinase inhibitors for enhancing the efficacy of anti-neoplastic agents and radiation therapy |
| CA2529032C (en) | 2003-06-24 | 2009-12-22 | Pfizer Products Inc. | Processes for the preparation of 1-[2-benzimidazol-1-yl) quinolin-8-yl] piperidin-4-ylamine derivatives |
| WO2008024974A1 (en) * | 2006-08-24 | 2008-02-28 | Serenex, Inc. | Pyrimidine and pyrazine derivatives |
| US8183245B2 (en) | 2007-10-25 | 2012-05-22 | Merck Sharp & Dohme Corp. | Pyrazine substituted pyrrolopyridines as inhibitors of JAK and PDK1 |
-
2009
- 2009-08-04 AT AT09786799T patent/ATE542813T1/de active
- 2009-08-04 CA CA2731368A patent/CA2731368C/en not_active Expired - Fee Related
- 2009-08-04 WO PCT/IB2009/053389 patent/WO2010016005A1/en not_active Ceased
- 2009-08-04 EP EP09786799A patent/EP2328890B1/en not_active Not-in-force
- 2009-08-04 JP JP2011521675A patent/JP5576370B2/ja not_active Expired - Fee Related
- 2009-08-04 US US13/057,558 patent/US8518952B2/en not_active Expired - Fee Related
- 2009-08-04 ES ES09786799T patent/ES2378513T3/es active Active
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