JP2008525453A5 - - Google Patents
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- Publication number
- JP2008525453A5 JP2008525453A5 JP2007548311A JP2007548311A JP2008525453A5 JP 2008525453 A5 JP2008525453 A5 JP 2008525453A5 JP 2007548311 A JP2007548311 A JP 2007548311A JP 2007548311 A JP2007548311 A JP 2007548311A JP 2008525453 A5 JP2008525453 A5 JP 2008525453A5
- Authority
- JP
- Japan
- Prior art keywords
- mmol
- mixture
- diazepan
- ylcarbamate
- 500mhz
- 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.)
- Pending
Links
- YMWUJEATGCHHMB-UHFFFAOYSA-N Dichloromethane Chemical compound ClCCl YMWUJEATGCHHMB-UHFFFAOYSA-N 0.000 description 3
- XEKOWRVHYACXOJ-UHFFFAOYSA-N Ethyl acetate Chemical compound CCOC(C)=O XEKOWRVHYACXOJ-UHFFFAOYSA-N 0.000 description 3
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 3
- ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 3
- QGZKDVFQNNGYKY-UHFFFAOYSA-N Ammonia Chemical compound N QGZKDVFQNNGYKY-UHFFFAOYSA-N 0.000 description 2
- DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 description 2
- KWGKDLIKAYFUFQ-UHFFFAOYSA-M lithium chloride Chemical compound [Li+].[Cl-] KWGKDLIKAYFUFQ-UHFFFAOYSA-M 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- KXDHJXZQYSOELW-UHFFFAOYSA-M Carbamate Chemical compound NC([O-])=O KXDHJXZQYSOELW-UHFFFAOYSA-M 0.000 description 1
- PMZURENOXWZQFD-UHFFFAOYSA-L Sodium Sulfate Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 description 1
- 229910021529 ammonia Inorganic materials 0.000 description 1
- 239000012230 colorless oil Substances 0.000 description 1
- MKRTXPORKIRPDG-UHFFFAOYSA-N diphenylphosphoryl azide Chemical compound C=1C=CC=CC=1P(=O)(N=[N+]=[N-])C1=CC=CC=C1 MKRTXPORKIRPDG-UHFFFAOYSA-N 0.000 description 1
- 239000003480 eluent Substances 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 238000012746 preparative thin layer chromatography Methods 0.000 description 1
- 238000000746 purification Methods 0.000 description 1
- 229910052938 sodium sulfate Inorganic materials 0.000 description 1
- 235000011152 sodium sulphate Nutrition 0.000 description 1
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63938904P | 2004-12-27 | 2004-12-27 | |
| PCT/US2005/045384 WO2006071548A2 (en) | 2004-12-27 | 2005-12-14 | Aminopyrazine analogs for treating glaucoma and other rho kinase-mediated diseases |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008525453A JP2008525453A (ja) | 2008-07-17 |
| JP2008525453A5 true JP2008525453A5 (enExample) | 2009-02-12 |
Family
ID=36615388
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007548311A Pending JP2008525453A (ja) | 2004-12-27 | 2005-12-14 | 緑内障と、ｒｈｏキナーゼを媒介とした他の疾患および症状を治療するためのアミノピラジン・アナログ |
Country Status (16)
| Country | Link |
|---|---|
| US (2) | US20080269249A2 (enExample) |
| EP (1) | EP1830853B1 (enExample) |
| JP (1) | JP2008525453A (enExample) |
| KR (1) | KR100994173B1 (enExample) |
| CN (1) | CN101102773B (enExample) |
| AR (1) | AR053110A1 (enExample) |
| AT (1) | ATE519488T1 (enExample) |
| AU (1) | AU2005322338B2 (enExample) |
| BR (1) | BRPI0519508A2 (enExample) |
| CA (1) | CA2590261C (enExample) |
| ES (1) | ES2368338T3 (enExample) |
| MX (1) | MX2007007797A (enExample) |
| PL (1) | PL383491A1 (enExample) |
| TW (1) | TW200633709A (enExample) |
| WO (1) | WO2006071548A2 (enExample) |
| ZA (1) | ZA200704959B (enExample) |
Families Citing this family (47)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8921376B2 (en) * | 2005-05-20 | 2014-12-30 | Vertex Pharmaceuticals Incorporated | Pyrrolopyridines useful as inhibitors of protein kinase |
| KR20080077652A (ko) * | 2005-12-22 | 2008-08-25 | 알콘 리서치, 리미티드 | 로 키나제-매개 질환 및 증상 치료용 (인다졸-5-일)피라진및 (1,3-디하이드로인돌-2-온)피라진 |
| MX2008012658A (es) | 2006-03-31 | 2008-12-16 | Schering Corp | Inhibidores de cinasa. |
| US20080021026A1 (en) * | 2006-07-20 | 2008-01-24 | Mehmet Kahraman | Benzothiophene inhibitors of rho kinase |
| NZ575336A (en) | 2006-10-23 | 2012-04-27 | Sgx Pharmaceuticals Inc | Bicyclic triazoles as protein kinase modulators |
| KR20090127867A (ko) * | 2006-12-05 | 2009-12-14 | 네이셔널 치아오 텅 유니버시티 | 인다졸 화합물 |
| US8648069B2 (en) | 2007-06-08 | 2014-02-11 | Abbvie Inc. | 5-substituted indazoles as kinase inhibitors |
| MX2009013213A (es) * | 2007-06-08 | 2010-03-30 | Abbott Lab | Indazoles 5-sustituidos 5-heteroarilo como inhibidores de cinasa. |
| MX2011004953A (es) | 2008-11-10 | 2011-12-14 | Vertex Pharma | Compuestos utiles como inhibidores de cinasa atr. |
| MX2011006503A (es) | 2008-12-19 | 2011-09-06 | Vertex Pharma | Derivados de pirazina utiles como inhibidores de la cinasa de atr. |
| US8513271B2 (en) | 2009-10-30 | 2013-08-20 | Janssen Pharmaceutica, Nv | Pyrimidine compounds as delta opioid receptor modulators |
| WO2011053696A1 (en) * | 2009-10-30 | 2011-05-05 | Janssen Pharmaceutica Nv | Pyrazines as delta opioid receptor modulators |
| JP5770198B2 (ja) | 2009-10-30 | 2015-08-26 | ヤンセン ファーマシューティカ エヌ．ベー． | オピオイド受容体調節因子としてのフェノキシ置換ピリミジン |
| JP5856151B2 (ja) | 2010-05-12 | 2016-02-09 | 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼ阻害剤として有用な２−アミノピリジン誘導体 |
| NZ603477A (en) | 2010-05-12 | 2014-09-26 | Vertex Pharma | Compounds useful as inhibitors of atr kinase |
| WO2011143399A1 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2013529200A (ja) * | 2010-05-12 | 2013-07-18 | 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 |
| WO2011143425A2 (en) | 2010-05-12 | 2011-11-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| EP2569289A1 (en) | 2010-05-12 | 2013-03-20 | Vertex Pharmaceuticals Incorporated | Pyrazines useful as inhibitors of atr kinase |
| WO2011163527A1 (en) | 2010-06-23 | 2011-12-29 | Vertex Pharmaceuticals Incorporated | Pyrrolo- pyrazine derivatives useful as inhibitors of atr kinase |
| EP2694498B1 (en) | 2011-04-05 | 2016-03-30 | Vertex Pharmaceuticals Incorporated | Aminopyrazine compounds useful as inhibitors of tra kinase |
| JP2014517079A (ja) | 2011-06-22 | 2014-07-17 | 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 |
| EP2723747A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| EP2723745A1 (en) | 2011-06-22 | 2014-04-30 | Vertex Pharmaceuticals Inc. | Compounds useful as inhibitors of atr kinase |
| US8853217B2 (en) | 2011-09-30 | 2014-10-07 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2751099B1 (en) | 2011-09-30 | 2017-06-14 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| CA2850491C (en) | 2011-09-30 | 2020-10-27 | Vertex Pharmaceuticals Incorporated | Treating pancreatic cancer and non-small cell lung cancer with atr inhibiors |
| US8765751B2 (en) | 2011-09-30 | 2014-07-01 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| 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 |
| WO2013071093A1 (en) | 2011-11-09 | 2013-05-16 | Vertex Pharmaceuticals Incorporated | Pyrazine compounds useful as inhibitors of atr kinase |
| US8846918B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| US8846917B2 (en) | 2011-11-09 | 2014-09-30 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of ATR kinase |
| EP2776422A1 (en) | 2011-11-09 | 2014-09-17 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| JP2015502925A (ja) | 2011-11-09 | 2015-01-29 | 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Ｖｅｒｔｅｘ Ｐｈａｒｍａｃｅｕｔｉｃａｌｓ Ｉｎｃｏｒｐｏｒａｔｅｄ | Ａｔｒキナーゼの阻害剤として有用なピラジン化合物 |
| WO2013152298A1 (en) | 2012-04-05 | 2013-10-10 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase and combination therapies thereof |
| DK2904406T3 (en) | 2012-10-04 | 2018-06-18 | Vertex Pharma | METHOD OF DETERMINING THE ATR INHIBITION, INCREASED DNA DAMAGE |
| EP2909202A1 (en) | 2012-10-16 | 2015-08-26 | Vertex Pharmaceuticals Incorporated | Compounds useful as inhibitors of atr kinase |
| TR201807740T4 (tr) | 2012-12-07 | 2018-06-21 | Vertex Pharma | ATR kinaz inhibitörü olarak 2-amino-6-fluoro-n-(5-fluoro-4-(4-(4-(oksetan-3-il)piperazin-1-karbonil)piperidin-1-il)piridin-3-il)pirazolo[1,5alfa]pirimidin-3-karboksamid. |
| EP2970286A1 (en) | 2013-03-15 | 2016-01-20 | Vertex Pharmaceuticals Inc. | Fused pyrazolopyrimidine derivatives useful as inhibitors of atr kinase |
| KR101504722B1 (ko) | 2013-06-12 | 2015-03-24 | 한국화학연구원 | 카모로놀 화합물을 유효성분으로 포함하는 심혈관 질환의 예방 및 치료용 약학적 조성물 |
| WO2015085132A1 (en) | 2013-12-06 | 2015-06-11 | Vertex Pharmaceuticals Incorporated | 2-amino-6-fluoro-n-[5-fluoro-pyridin-3-yl]pyrazolo[1,5-a]pyrimidin-3-carboxamide compound useful as atr kinase inhibitor, its preparation, different solid forms and radiolabelled derivatives thereof |
| SI3152212T1 (sl) | 2014-06-05 | 2020-06-30 | Vertex Pharmaceuticals Inc. | Radioaktivno označeni derivati 2-amino-6-fluoro-N-(5-fluoro-piridin-3-IL)-pirazolo (1,5-A)pirimidin-3- karboksamidne spojine, koristni kot inhibitor kinaze ATR, priprava navedene spojine in njene različne trdne oblike |
| LT3157566T (lt) | 2014-06-17 | 2019-08-12 | Vertex Pharmaceuticals Incorporated | Vėžio gydymo būdas, panaudojant chk1 ir atr inhibitorių derinį |
| 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 |
| GB201715410D0 (en) | 2017-09-22 | 2017-11-08 | Syngenta Participations Ag | Improvements in or relating to organic compounds |
| WO2019119207A1 (en) | 2017-12-18 | 2019-06-27 | Merck Sharp & Dohme Corp. | Purine inhibitors of human phosphatidylinositol 3-kinase delta |
| CN112142716B (zh) * | 2020-10-29 | 2021-08-31 | 山东新时代药业有限公司 | 一种5元杂芳基取代的吡嗪衍生物及其应用 |
Family Cites Families (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6271224B1 (en) * | 1995-12-21 | 2001-08-07 | Alcon Laboratories, Inc. | Use of certain isoquinolinesulfonyl compounds for the treatment of glaucoma and ocular ischemia |
| US6586425B2 (en) * | 1996-02-21 | 2003-07-01 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| US5798380A (en) * | 1996-02-21 | 1998-08-25 | Wisconsin Alumni Research Foundation | Cytoskeletal active agents for glaucoma therapy |
| SI0956865T2 (sl) * | 1996-08-12 | 2011-04-29 | Mitsubishi Pharma Corp | Zdravila, ki obsegajo inhibitor Rho-kinaze |
| AU5198199A (en) * | 1998-08-17 | 2000-03-06 | Senju Pharmaceutical Co., Ltd. | Preventives/remedies for glaucoma |
| DE60045890D1 (de) * | 1999-04-27 | 2011-06-09 | Mitsubishi Tanabe Pharma Corp | Arzneimittel zur präventiven oder therapeutische Behandlung von Lebererkrankungen |
| US6348494B1 (en) * | 2000-11-21 | 2002-02-19 | American Home Products Corporation | Ethers of o-desmethyl venlafaxine |
| AU2001241183A1 (en) * | 2000-03-16 | 2001-09-24 | Mitsubishi Pharma Corporation | Amide compounds and use thereof |
| US6720341B2 (en) * | 2000-03-31 | 2004-04-13 | Mitsubishi Pharma Corporation | Preventives/remedies for kidney diseases |
| EP1403255A4 (en) * | 2001-06-12 | 2005-04-06 | Sumitomo Pharma | RHO KINASE INHIBITORS |
| WO2003045924A1 (en) * | 2001-11-21 | 2003-06-05 | Pharmacia & Upjohn Company | Substituted aryl 1,4-pyrazine derivatives |
| JP2005516936A (ja) * | 2001-12-18 | 2005-06-09 | アストラゼネカ・アクチエボラーグ | Ｎ−ピラジニル−チエニルスルホンアミドおよびケモカイン媒介疾患の治療におけるそれらの使用 |
| US7094789B2 (en) * | 2002-07-22 | 2006-08-22 | Asahi Kasei Pharma Corporation | 5-substituted isoquinoline derivatives |
| AU2003258307A1 (en) * | 2002-08-20 | 2004-03-11 | Neurogen Corp | 5-substituted-2-arylpyrazines as modulators of crf receptors |
| GB0219746D0 (en) * | 2002-08-23 | 2002-10-02 | Inst Of Ex Botany Ascr | Azapurine derivatives |
| EP1608622A4 (en) * | 2003-03-24 | 2009-04-01 | Merck & Co Inc | BIARYLSUBSTITUTED 6-LOW HETEROCYCLES AS SODIUM CHANNEL BLOCKERS |
| GB2400101A (en) * | 2003-03-28 | 2004-10-06 | Biofocus Discovery Ltd | Compounds capable of binding to the active site of protein kinases |
| CA2543644A1 (en) * | 2003-10-27 | 2005-05-06 | Astellas Pharma Inc. | Pyrazine derivatives and pharmaceutical use thereof |
| US20080194574A1 (en) * | 2003-12-16 | 2008-08-14 | Axxima Pharmaceuticals Ag | Pyrazine Derivatives As Effective Compounds Against Infectious Diseases |
| JP4978192B2 (ja) * | 2004-04-01 | 2012-07-18 | アステラス製薬株式会社 | ピラジン誘導体およびその医薬的使用 |
-
2005
- 2005-12-14 JP JP2007548311A patent/JP2008525453A/ja active Pending
- 2005-12-14 AU AU2005322338A patent/AU2005322338B2/en not_active Ceased
- 2005-12-14 CA CA2590261A patent/CA2590261C/en not_active Expired - Fee Related
- 2005-12-14 ES ES05854156T patent/ES2368338T3/es not_active Expired - Lifetime
- 2005-12-14 ZA ZA200704959A patent/ZA200704959B/xx unknown
- 2005-12-14 AT AT05854156T patent/ATE519488T1/de not_active IP Right Cessation
- 2005-12-14 CN CN200580046786XA patent/CN101102773B/zh not_active Expired - Fee Related
- 2005-12-14 EP EP05854156A patent/EP1830853B1/en not_active Expired - Lifetime
- 2005-12-14 BR BRPI0519508-0A patent/BRPI0519508A2/pt not_active IP Right Cessation
- 2005-12-14 WO PCT/US2005/045384 patent/WO2006071548A2/en not_active Ceased
- 2005-12-14 MX MX2007007797A patent/MX2007007797A/es active IP Right Grant
- 2005-12-14 KR KR1020077017035A patent/KR100994173B1/ko not_active Expired - Fee Related
- 2005-12-14 PL PL383491A patent/PL383491A1/pl not_active Application Discontinuation
- 2005-12-14 US US11/302,825 patent/US20080269249A2/en not_active Abandoned
- 2005-12-23 TW TW094146211A patent/TW200633709A/zh unknown
- 2005-12-26 AR ARP050105535A patent/AR053110A1/es not_active Application Discontinuation
-
2010
- 2010-05-05 US US12/774,399 patent/US20100216777A1/en not_active Abandoned
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