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 (https=) | 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 (https=) |
| EP (1) | EP2328890B1 (https=) |
| JP (1) | JP5576370B2 (https=) |
| AT (1) | ATE542813T1 (https=) |
| CA (1) | CA2731368C (https=) |
| ES (1) | ES2378513T3 (https=) |
| WO (1) | WO2010016005A1 (https=) |
Families Citing this family (54)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2663222T3 (es) | 2008-12-19 | 2018-04-11 | Vertex Pharmaceuticals Incorporated | Derivados de pirazina útiles como inhibidores de la quinasa ATR |
| MX2011009796A (es) | 2009-03-20 | 2011-12-14 | Amgen Inc | Inhibidores de la cinasa pi3. |
| PH12012500778A1 (en) | 2009-10-30 | 2012-11-26 | Janssen Pharmaceutica Nv | IMIDAZO[1,2-b]PYRIDAZINE DERIVATIVES AND THEIR USE AS PDE10 INHIBITORS |
| EP2338888A1 (en) * | 2009-12-24 | 2011-06-29 | Almirall, S.A. | Imidazopyridine derivatives as JAK inhibitors |
| UY33213A (es) * | 2010-02-18 | 2011-09-30 | Almirall Sa | Derivados de pirazol como inhibidores de jak |
| EP2360158A1 (en) * | 2010-02-18 | 2011-08-24 | Almirall, S.A. | Pyrazole derivatives as jak inhibitors |
| 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 |
| US9630956B2 (en) | 2010-05-12 | 2017-04-25 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| JP2013526540A (ja) * | 2010-05-12 | 2013-06-24 | バーテックス ファーマシューティカルズ インコーポレイテッド | Ａｔｒキナーゼ阻害剤として有用な化合物 |
| EP2463289A1 (en) | 2010-11-26 | 2012-06-13 | Almirall, S.A. | Imidazo[1,2-b]pyridazine derivatives as JAK inhibitors |
| BR112013033375B1 (pt) | 2011-06-27 | 2022-05-10 | Janssen Pharmaceutica N.V | Derivados de 1-aril-4-metil-[1,2,4]triazolo[4,3-a]quinoxa-lina, seu uso, composição farmacêutica que os compreende, processo de preparação dos mesmos, solução estéril e composto intermediário |
| EP2554544A1 (en) | 2011-08-01 | 2013-02-06 | Almirall, S.A. | Pyridin-2(1h)-one derivatives as jak inhibitors |
| WO2013049859A1 (en) | 2011-09-30 | 2013-04-04 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibitors |
| SG10201606774UA (en) | 2011-09-30 | 2016-10-28 | Vertex Pharma | Processes for making compounds useful as inhibitors of atr kinase |
| WO2013066729A1 (en) | 2011-10-31 | 2013-05-10 | Merck Sharp & Dohme Corp. | Aminopyrimidinones as interleukin receptor-associated kinase inhibitors |
| CA2869309C (en) | 2012-04-05 | 2021-02-09 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| HK1206250A1 (en) | 2012-06-26 | 2016-01-08 | Janssen Pharmaceutica Nv | Combinations comprising pde 2 inhibitors such as 1-aryl-4-methyl-[1,2,4] triazolo [4,3-a] quinoxaline compounds and ped 10 inhibitors for use in the treatment of neurological or metabolic disorders |
| WO2014009305A1 (en) | 2012-07-09 | 2014-01-16 | Janssen Pharmaceutica Nv | Inhibitors of phosphodiesterase 10 enzyme |
| US8999632B2 (en) | 2012-10-04 | 2015-04-07 | Vertex Pharmaceuticals Incorporated | Method for measuring ATR inhibition mediated increases in DNA damage |
| KR20220143164A (ko) | 2012-11-21 | 2022-10-24 | 피티씨 테라퓨틱스, 인크. | 치환된 리버스 피리미딘 ｂｍｉ-1 저해제 |
| 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 |
| WO2015076800A1 (en) | 2013-11-21 | 2015-05-28 | Ptc Therapeutics, Inc. | Substituted pyridine and pyrazine bmi-1 inhibitors |
| MX368464B (es) | 2013-12-05 | 2019-10-02 | Pfizer | Acrilamidas de pirrolo[2,3-d]pirimidinilo, pirrolo[2,3-b]pirazinil o y pirrolo[2,3-d]piridinilo. |
| 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 |
| PL3140305T3 (pl) | 2014-05-09 | 2018-10-31 | Pimera, Inc. | Nowe kompozycje, ich zastosowania i sposoby wytwarzania |
| CA2973597A1 (en) | 2015-01-23 | 2016-07-28 | Confluence Life Sciences, Inc. | Heterocyclic itk inhibitors for treating inflammation and cancer |
| US10703756B2 (en) | 2015-05-01 | 2020-07-07 | Pfizer Inc. | Pyrrolo[2,3-D]pyrimidinyl, pyrrolo[2,3-B]pyrazinyl, pyrrolo[2,3-B]pyridinyl acrylamides and epoxides thereof |
| 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 |
| HK1258570A1 (zh) | 2015-09-30 | 2019-11-15 | Vertex Pharmaceuticals Inc. | 使用dna损伤剂及atr抑制剂的组合治疗癌症的方法 |
| CR20180372A (es) | 2016-02-24 | 2018-09-19 | Pfizer | Derivados de pirazolo [1,5-a] pirazin-4-ilo |
| WO2018140648A1 (en) | 2017-01-25 | 2018-08-02 | Eric Jon Jacobsen | Pyrrolopyrimidine itk inhibitors for treating inflammation and cancer |
| CA3057741A1 (en) | 2017-03-28 | 2018-10-04 | Pimera, Inc. | Novel crystal forms of a pol1 inhibitor |
| 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 |
| WO2019034973A1 (en) | 2017-08-14 | 2019-02-21 | 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 |
| US12448374B2 (en) | 2018-06-07 | 2025-10-21 | Disarm Therapeutics, Inc. | Inhibitors of SARM1 |
| EP3608326A1 (en) | 2018-08-10 | 2020-02-12 | Irbm S.P.A. | Tricyclic inhibitors of hepatitis b virus |
| CN113164479A (zh) | 2018-08-17 | 2021-07-23 | Ptc医疗公司 | 用于治疗胰腺癌的方法 |
| EP3825318A1 (en) | 2019-11-25 | 2021-05-26 | Promidis S.r.l. | 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 |
| EP3741762A1 (en) | 2019-05-23 | 2020-11-25 | Irbm S.P.A. | Oxalamido-substituted tricyclic inhibitors of hepatitis b virus |
| WO2021252775A1 (en) * | 2020-06-11 | 2021-12-16 | Chdi Foundation, Inc. | Heterocyclic compounds and imaging agents for imaging huntingtin protein |
| EP4188926A4 (en) * | 2020-07-31 | 2024-08-21 | 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 |
| IL310425A (en) * | 2021-07-30 | 2024-03-01 | Childrens Hospital Med Ct | Multi-cyclic irak and flt3 inhibiting compounds and uses thereof |
| AU2023283393A1 (en) * | 2022-06-10 | 2025-01-02 | Interline Therapeutics, Inc. | Imidazo(1,2-a)pyridine derivatives as ripk2 inhibitors |
| AR129535A1 (es) | 2022-06-21 | 2024-09-04 | Syngenta Crop Protection Ag | Derivados de carboxamida heterocíclicos bicíclicos microbiocidas |
| WO2024089191A1 (en) | 2022-10-27 | 2024-05-02 | Syngenta Crop Protection Ag | Microbiocidal heterobicyclic dihydrooxadiazine derivatives |
| 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 |
| WO2026006247A1 (en) * | 2024-06-26 | 2026-01-02 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | 2-(piperidin-3-yl)isoindole-1,3-dione analogs and uses thereof |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR0166088B1 (ko) | 1990-01-23 | 1999-01-15 | . | 수용해도가 증가된 시클로덱스트린 유도체 및 이의 용도 |
| US5376645A (en) | 1990-01-23 | 1994-12-27 | University Of Kansas | Derivatives of cyclodextrins exhibiting enhanced aqueous solubility and the use thereof |
| 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 |
| EP1135135A4 (en) | 1998-09-18 | 2006-08-09 | Smithkline Beecham Corp | CHK1 KINASE INHIBITORS |
| US6682736B1 (en) * | 1998-12-23 | 2004-01-27 | Abgenix, Inc. | Human monoclonal antibodies to CTLA-4 |
| WO2001016306A2 (en) | 1999-08-27 | 2001-03-08 | Chiron Corporation | Chimeric antisense oligonucleotides and cell transfecting formulations thereof |
| JP4610828B2 (ja) | 1999-09-22 | 2011-01-12 | 株式会社 キャンバス | Ｇ２期細胞周期停止の阻害、およびｄｎａ損傷剤に対する細胞感作のための組成物および方法 |
| US6211164B1 (en) * | 2000-03-10 | 2001-04-03 | Abbott Laboratories | Antisense oligonucleotides of the human chk1 gene and uses thereof |
| BRPI0116728B1 (pt) | 2001-01-05 | 2018-10-30 | Pfizer Inc. | anticorpos para receptor de fator de crescimento i semelhante à insulina |
| 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 |
| EP1501514B1 (en) * | 2002-05-03 | 2012-12-19 | Exelixis, Inc. | Protein kinase modulators and methods of use |
| US7704995B2 (en) * | 2002-05-03 | 2010-04-27 | 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 |
| DK1641780T3 (da) | 2003-06-24 | 2009-02-02 | Pfizer Prod Inc | Fremgangsmåder til fremstilling af 1-[(benzimidazol-1yl)quinolin-8-yl]-piperidin-4-ylamin-derivater |
| 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 ES ES09786799T patent/ES2378513T3/es active Active
- 2009-08-04 JP JP2011521675A patent/JP5576370B2/ja not_active Expired - Fee Related
- 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 EP EP09786799A patent/EP2328890B1/en not_active Not-in-force
- 2009-08-04 WO PCT/IB2009/053389 patent/WO2010016005A1/en not_active Ceased
- 2009-08-04 US US13/057,558 patent/US8518952B2/en not_active Expired - Fee Related
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