JP2011529918A5 - - Google Patents
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- JP2011529918A5 JP2011529918A5 JP2011521361A JP2011521361A JP2011529918A5 JP 2011529918 A5 JP2011529918 A5 JP 2011529918A5 JP 2011521361 A JP2011521361 A JP 2011521361A JP 2011521361 A JP2011521361 A JP 2011521361A JP 2011529918 A5 JP2011529918 A5 JP 2011529918A5
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- JP
- Japan
- Prior art keywords
- compound
- aryl
- heteroaryl
- lower alkyl
- formula
- 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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- 0 *c1ccnc2ncn[n]12 Chemical compound *c1ccnc2ncn[n]12 0.000 description 69
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- RNHNZDUJRXROJA-UHFFFAOYSA-N Cc1c2[o]nnc2ncc1 Chemical compound Cc1c2[o]nnc2ncc1 RNHNZDUJRXROJA-UHFFFAOYSA-N 0.000 description 2
- QAIZVTQMYGHGTG-UHFFFAOYSA-N Cc1c2[s]cnc2ncc1 Chemical compound Cc1c2[s]cnc2ncc1 QAIZVTQMYGHGTG-UHFFFAOYSA-N 0.000 description 2
- VAXIBUZVPFRMHZ-UHFFFAOYSA-N Cc1c2[s]cnc2ncn1 Chemical compound Cc1c2[s]cnc2ncn1 VAXIBUZVPFRMHZ-UHFFFAOYSA-N 0.000 description 2
- IYMQFDVVSJBOCJ-UHFFFAOYSA-N Cc1c2[s]ncc2ncc1 Chemical compound Cc1c2[s]ncc2ncc1 IYMQFDVVSJBOCJ-UHFFFAOYSA-N 0.000 description 2
- QPBHBVWTNWOHRK-UHFFFAOYSA-N Cc1c2[s]ncc2ncn1 Chemical compound Cc1c2[s]ncc2ncn1 QPBHBVWTNWOHRK-UHFFFAOYSA-N 0.000 description 2
- WXVQCFALDUVKSC-UHFFFAOYSA-N Cc1cc(C)nc2ncn[n]12 Chemical compound Cc1cc(C)nc2ncn[n]12 WXVQCFALDUVKSC-UHFFFAOYSA-N 0.000 description 2
- KEFHNNMOFZXQJA-UHFFFAOYSA-N Cc1cc(Cl)nc2ncc[n]12 Chemical compound Cc1cc(Cl)nc2ncc[n]12 KEFHNNMOFZXQJA-UHFFFAOYSA-N 0.000 description 2
- GKGGEVRMITWKIA-UHFFFAOYSA-N Cc1nc(F)n[n]2c1ccc2 Chemical compound Cc1nc(F)n[n]2c1ccc2 GKGGEVRMITWKIA-UHFFFAOYSA-N 0.000 description 2
- CZODODSACGXIMA-UHFFFAOYSA-N Cc1ncn[n]2c1ccc2 Chemical compound Cc1ncn[n]2c1ccc2 CZODODSACGXIMA-UHFFFAOYSA-N 0.000 description 2
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- IMJFYHXYUIXDER-UHFFFAOYSA-N Cc1ncn[n]2c1nnc2 Chemical compound Cc1ncn[n]2c1nnc2 IMJFYHXYUIXDER-UHFFFAOYSA-N 0.000 description 2
- YZEJFPWHRCHRRI-UHFFFAOYSA-N Cc1ncn[n]2ncnc12 Chemical compound Cc1ncn[n]2ncnc12 YZEJFPWHRCHRRI-UHFFFAOYSA-N 0.000 description 2
- NKNFAJHOXKRJJK-UHFFFAOYSA-N Ic1ccnc2ccn[n]12 Chemical compound Ic1ccnc2ccn[n]12 NKNFAJHOXKRJJK-UHFFFAOYSA-N 0.000 description 2
- RINRRWDHGQAUGT-UHFFFAOYSA-N Ic1ncn[n]2c1ccc2 Chemical compound Ic1ncn[n]2c1ccc2 RINRRWDHGQAUGT-UHFFFAOYSA-N 0.000 description 2
- COIRNGWSWUWRGE-UHFFFAOYSA-N Ic1ncn[n]2nccc12 Chemical compound Ic1ncn[n]2nccc12 COIRNGWSWUWRGE-UHFFFAOYSA-N 0.000 description 2
- AYRXNHGVHILSDU-UHFFFAOYSA-N Ic1ncnc2c1[nH]nc2 Chemical compound Ic1ncnc2c1[nH]nc2 AYRXNHGVHILSDU-UHFFFAOYSA-N 0.000 description 2
- QWZFYLPTEFARKF-UHFFFAOYSA-N Ic1ncnc2c1[o]cc2 Chemical compound Ic1ncnc2c1[o]cc2 QWZFYLPTEFARKF-UHFFFAOYSA-N 0.000 description 2
- PEHVGBZKEYRQSX-UHFFFAOYSA-N Nc1c(cc[nH]2)c2ncn1 Chemical compound Nc1c(cc[nH]2)c2ncn1 PEHVGBZKEYRQSX-UHFFFAOYSA-N 0.000 description 2
- VEFILPQJQRHUBK-UHFFFAOYSA-N Nc1c2[o]ncc2ncc1 Chemical compound Nc1c2[o]ncc2ncc1 VEFILPQJQRHUBK-UHFFFAOYSA-N 0.000 description 2
- WPFZGADUIUVTCF-UHFFFAOYSA-N Nc1ccnc2ccn[n]12 Chemical compound Nc1ccnc2ccn[n]12 WPFZGADUIUVTCF-UHFFFAOYSA-N 0.000 description 2
- QOXCEADXSTZKHA-UHFFFAOYSA-N Nc1ccnc2ncn[n]12 Chemical compound Nc1ccnc2ncn[n]12 QOXCEADXSTZKHA-UHFFFAOYSA-N 0.000 description 2
- HVWJATXZZQPVEL-UHFFFAOYSA-N Nc1ncnc2c1[o]cc2 Chemical compound Nc1ncnc2c1[o]cc2 HVWJATXZZQPVEL-UHFFFAOYSA-N 0.000 description 2
- VASAZSNMKDILTC-UHFFFAOYSA-O [NH3+]c1ccn[n]2nccc12 Chemical compound [NH3+]c1ccn[n]2nccc12 VASAZSNMKDILTC-UHFFFAOYSA-O 0.000 description 2
- KCSLHMLHJTWKLW-ZJUUUORDSA-N C[C@H](CCNC1)[C@H]1N(C)C=C=C Chemical compound C[C@H](CCNC1)[C@H]1N(C)C=C=C KCSLHMLHJTWKLW-ZJUUUORDSA-N 0.000 description 1
- DVKMEJAYUBJYIM-RQJHMYQMSA-N C[C@H](CCNC1)[C@H]1N(C)N Chemical compound C[C@H](CCNC1)[C@H]1N(C)N DVKMEJAYUBJYIM-RQJHMYQMSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US8570508P | 2008-08-01 | 2008-08-01 | |
| US61/085,705 | 2008-08-01 | ||
| US9856208P | 2008-09-19 | 2008-09-19 | |
| US61/098,562 | 2008-09-19 | ||
| PCT/US2009/052449 WO2010014930A2 (en) | 2008-08-01 | 2009-07-31 | Therapeutic agents |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2011529918A JP2011529918A (ja) | 2011-12-15 |
| JP2011529918A5 true JP2011529918A5 (enExample) | 2012-09-06 |
Family
ID=41170025
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011521361A Pending JP2011529918A (ja) | 2008-08-01 | 2009-07-31 | Ｊａｋ３阻害剤としてのピペリジン誘導体 |
Country Status (13)
| Country | Link |
|---|---|
| US (1) | US20110165183A1 (enExample) |
| EP (1) | EP2324020A2 (enExample) |
| JP (1) | JP2011529918A (enExample) |
| KR (1) | KR20110050654A (enExample) |
| CN (1) | CN102171211A (enExample) |
| AU (1) | AU2009276420A1 (enExample) |
| BR (1) | BRPI0916931A2 (enExample) |
| CA (1) | CA2732628A1 (enExample) |
| IL (1) | IL210990A0 (enExample) |
| MX (1) | MX2011001259A (enExample) |
| NZ (1) | NZ590922A (enExample) |
| RU (1) | RU2011105768A (enExample) |
| WO (1) | WO2010014930A2 (enExample) |
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| TW201107330A (en) | 2009-07-31 | 2011-03-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
| AR081428A1 (es) * | 2010-05-28 | 2012-08-29 | Biocryst Pharm Inc | Derivados heterociclicos condensados nitrogenados, composiciones farmaceuticas que los contienen y uso de los mismos para suprimir una respuesta inmune o tratar cancer. |
| JP2014513728A (ja) * | 2011-05-17 | 2014-06-05 | プリンシピア バイオファーマ インコーポレイテッド | チロシンキナーゼ阻害剤としてのアザインドール誘導体 |
| WO2013135671A1 (en) | 2012-03-13 | 2013-09-19 | Basf Se | Fungicidal pyrimidine compounds |
| SMT201900344T1 (it) | 2012-09-10 | 2019-07-11 | Principia Biopharma Inc | Composti di pirazolopirimidina come inibitori di chinasi |
| US9550785B2 (en) * | 2012-11-20 | 2017-01-24 | Glaxosmithkline Llc | Pyrrolopyrimidines as therapeutic agents for the treatment of diseases |
| WO2014097150A1 (en) * | 2012-12-17 | 2014-06-26 | Ranbaxy Laboratories Limited | Process for the preparation of tofacitinib and intermediates thereof |
| WO2014102826A1 (en) * | 2012-12-28 | 2014-07-03 | Glenmark Pharmaceuticals Limited; | The present invention relates to process for the preparation of tofacitinib and intermediates thereof. |
| US20160221964A1 (en) | 2013-09-16 | 2016-08-04 | Basf Se | Fungicidal pyrimidine compounds |
| WO2015036059A1 (en) | 2013-09-16 | 2015-03-19 | Basf Se | Fungicidal pyrimidine compounds |
| CN106232122A (zh) * | 2013-09-27 | 2016-12-14 | 林伯士艾瑞斯公司 | Irak抑制剂和其用途 |
| EP3539965B1 (en) * | 2013-12-09 | 2021-01-20 | Unichem Laboratories Limited | An improved process for the preparation of (3r,4r)-(1-benzyl-4-methylpiperidin-3-yl)-methylamine |
| KR20160117614A (ko) | 2014-02-21 | 2016-10-10 | 프린시피아 바이오파마, 인코퍼레이티드 | Btk 억제제의 염 및 고체 형태 |
| CN104860950A (zh) * | 2014-02-24 | 2015-08-26 | 重庆医药工业研究院有限责任公司 | 一种制备4-氯吡咯[2,3-d]并嘧啶的方法 |
| CN104059016A (zh) * | 2014-06-20 | 2014-09-24 | 湖南天地恒一制药有限公司 | 制备托法替布的中间体及所述中间体的制备方法 |
| KR101710127B1 (ko) * | 2014-08-29 | 2017-02-27 | 한화제약주식회사 | 야누스인산화효소 억제제로서의 치환된 N-(피롤리딘-3-일)-7H-피롤로[2,3-d]피리미딘-4-아민 |
| MX381283B (es) | 2014-12-18 | 2025-03-12 | Principia Biopharma Inc | Tratamiento de pénfigo. |
| CN105732637B (zh) * | 2014-12-30 | 2020-04-21 | 广东东阳光药业有限公司 | 杂芳化合物及其在药物中的应用 |
| EP3078665A1 (en) * | 2015-04-10 | 2016-10-12 | OLON S.p.A. | Efficient method for the preparation of tofacitinib citrate |
| CN107709327A (zh) * | 2015-06-22 | 2018-02-16 | 小野药品工业株式会社 | Brk抑制性化合物 |
| TW201718572A (zh) | 2015-06-24 | 2017-06-01 | 普林斯匹亞生物製藥公司 | 酪胺酸激酶抑制劑 |
| WO2017004134A1 (en) * | 2015-06-29 | 2017-01-05 | Nimbus Iris, Inc. | Irak inhibitors and uses thereof |
| CN105622616A (zh) * | 2016-02-25 | 2016-06-01 | 上海雅本化学有限公司 | 一种4-氯吡咯并嘧啶的制备方法 |
| US20190231784A1 (en) | 2016-06-29 | 2019-08-01 | Principia Biopharma Inc. | Modified release formulations of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| GB201617758D0 (en) | 2016-10-20 | 2016-12-07 | Almac Discovery Limited | Pharmaceutical compounds |
| WO2019201194A1 (zh) * | 2018-04-16 | 2019-10-24 | 深圳市塔吉瑞生物医药有限公司 | 取代的吡咯并三嗪类化合物及其药物组合物及其用途 |
| IL291994A (en) | 2019-10-14 | 2022-06-01 | Principia Biopharma Inc | Methods for treating immune thrombocytopenia by administering (r)-2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)pyrazolo[3,4-d]pyrimidin-1-yl]piperidine- 1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| PH12022551787A1 (en) | 2020-01-22 | 2024-02-12 | Principia Biopharma Inc | Crystalline forms of 2-[3-[4-amino-3-(2-fluoro-4-phenoxy-phenyl)-1h-pyrazolo[3,4-d]pyrimidin-1-yl]piperidine-1-carbonyl]-4-methyl-4-[4-(oxetan-3-yl)piperazin-1-yl]pent-2-enenitrile |
| CN116768908B (zh) * | 2022-03-10 | 2025-11-18 | 石家庄迪斯凯威医药科技有限公司 | 一种含n多环化合物及其制备方法与用途 |
| CN117164519A (zh) * | 2023-08-18 | 2023-12-05 | 杭州小蓓医药科技有限公司 | 一种l-肌肽的合成方法 |
| CN117534603A (zh) * | 2023-11-10 | 2024-02-09 | 江苏海悦康医药科技有限公司 | 一种托法替布中间体的制备方法 |
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| DK1087970T3 (da) * | 1998-06-19 | 2004-08-02 | Pfizer Prod Inc | Pyrrol[2,3-d]pyrimidin forbindelser |
| AU777911B2 (en) * | 1999-12-10 | 2004-11-04 | Pfizer Products Inc. | Pyrrolo(2,3-d)pyrimidine compounds |
| AP1911A (en) * | 2000-06-26 | 2008-10-30 | Pfizer Prod Inc | Pyrrolo[2,3-d]pyrimidine compounds. |
| US7301023B2 (en) * | 2001-05-31 | 2007-11-27 | Pfizer Inc. | Chiral salt resolution |
| KR20050086784A (ko) * | 2002-11-26 | 2005-08-30 | 화이자 프로덕츠 인크. | 이식 거부반응의 치료 방법 |
| DE602004021585D1 (de) * | 2003-04-29 | 2009-07-30 | Pfizer Ltd | 5,7-DIAMINOPYRAZOLOi4,3-D PYRIMIDINE ZUR VERWENDUNG IN DER BEHANDLUNG VON BLUTHOCHDRUCK |
| WO2005051393A1 (en) * | 2003-11-25 | 2005-06-09 | Pfizer Products Inc. | Method of treatment of atherosclerosis |
| AR054416A1 (es) * | 2004-12-22 | 2007-06-27 | Incyte Corp | Pirrolo [2,3-b]piridin-4-il-aminas y pirrolo [2,3-b]pirimidin-4-il-aminas como inhibidores de las quinasas janus. composiciones farmaceuticas. |
| JP5071374B2 (ja) * | 2005-07-14 | 2012-11-14 | アステラス製薬株式会社 | ヘテロ環ヤヌスキナーゼ３阻害剤 |
| NL2000291C2 (nl) * | 2005-11-10 | 2009-02-17 | Pfizer Prod Inc | 1-(1-(2-ethoxyethyl)-3-ethyl-7-(4-methylpyridin-2-ylamino)-1H- pyrazool(4,3-d)pyrimidine-5-yl)piperidine-4-carbonzuur en zouten daarvan. |
| TW201111385A (en) * | 2009-08-27 | 2011-04-01 | Biocryst Pharm Inc | Heterocyclic compounds as janus kinase inhibitors |
| RU2013120966A (ru) * | 2010-10-08 | 2014-11-20 | Эббви Инк. | ФУРО[3,2-d]ПИРИМИДИНОВЫЕ СОЕДИНЕНИЯ |
-
2009
- 2009-07-31 NZ NZ590922A patent/NZ590922A/xx not_active IP Right Cessation
- 2009-07-31 AU AU2009276420A patent/AU2009276420A1/en not_active Abandoned
- 2009-07-31 US US13/057,100 patent/US20110165183A1/en not_active Abandoned
- 2009-07-31 CA CA2732628A patent/CA2732628A1/en not_active Abandoned
- 2009-07-31 EP EP09791064A patent/EP2324020A2/en not_active Withdrawn
- 2009-07-31 BR BRPI0916931A patent/BRPI0916931A2/pt not_active IP Right Cessation
- 2009-07-31 KR KR1020117004724A patent/KR20110050654A/ko not_active Withdrawn
- 2009-07-31 CN CN2009801396041A patent/CN102171211A/zh active Pending
- 2009-07-31 WO PCT/US2009/052449 patent/WO2010014930A2/en not_active Ceased
- 2009-07-31 JP JP2011521361A patent/JP2011529918A/ja active Pending
- 2009-07-31 MX MX2011001259A patent/MX2011001259A/es unknown
- 2009-07-31 RU RU2011105768/04A patent/RU2011105768A/ru not_active Application Discontinuation
-
2011
- 2011-02-01 IL IL210990A patent/IL210990A0/en unknown
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