JP2005527565A - 新しいピラゾロ［４，３−ｄ］ピリミジン、その調整方法、及び治療方法 - Google Patents
新しいピラゾロ［４，３−ｄ］ピリミジン、その調整方法、及び治療方法 Download PDFInfo
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- JP2005527565A JP2005527565A JP2003580337A JP2003580337A JP2005527565A JP 2005527565 A JP2005527565 A JP 2005527565A JP 2003580337 A JP2003580337 A JP 2003580337A JP 2003580337 A JP2003580337 A JP 2003580337A JP 2005527565 A JP2005527565 A JP 2005527565A
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- amino
- group
- pyrimidine
- pyrazolo
- isopropyl
- 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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- DSKLYHDHQJANOE-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidine Chemical compound C1=NC=N[C]2C=NN=C21 DSKLYHDHQJANOE-UHFFFAOYSA-N 0.000 title claims description 232
- 238000000034 method Methods 0.000 title claims description 102
- -1 cycloheteroalkyl Chemical group 0.000 claims abstract description 539
- 229910052736 halogen Inorganic materials 0.000 claims abstract description 93
- 125000003545 alkoxy group Chemical group 0.000 claims abstract description 87
- 125000003282 alkyl amino group Chemical group 0.000 claims abstract description 84
- 125000000217 alkyl group Chemical group 0.000 claims abstract description 63
- 125000003342 alkenyl group Chemical group 0.000 claims abstract description 55
- 125000000304 alkynyl group Chemical group 0.000 claims abstract description 55
- 125000003118 aryl group Chemical group 0.000 claims abstract description 38
- 125000000753 cycloalkyl group Chemical group 0.000 claims abstract description 30
- 125000001072 heteroaryl group Chemical group 0.000 claims abstract description 27
- 125000003710 aryl alkyl group Chemical group 0.000 claims abstract description 23
- 125000000623 heterocyclic group Chemical group 0.000 claims abstract description 21
- 150000003839 salts Chemical class 0.000 claims abstract description 21
- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 claims abstract description 19
- 239000001257 hydrogen Substances 0.000 claims abstract description 19
- 229910052739 hydrogen Inorganic materials 0.000 claims abstract description 19
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims abstract description 16
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims abstract description 13
- 125000004404 heteroalkyl group Chemical group 0.000 claims abstract description 12
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims abstract description 7
- SNOOUWRIMMFWNE-UHFFFAOYSA-M sodium;6-[(3,4,5-trimethoxybenzoyl)amino]hexanoate Chemical compound [Na+].COC1=CC(C(=O)NCCCCCC([O-])=O)=CC(OC)=C1OC SNOOUWRIMMFWNE-UHFFFAOYSA-M 0.000 claims abstract description 7
- 125000005842 heteroatom Chemical group 0.000 claims abstract description 6
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- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 271
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 269
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- CISNNLXXANUBPI-UHFFFAOYSA-N cyano(nitro)azanide Chemical group [O-][N+](=O)[N-]C#N CISNNLXXANUBPI-UHFFFAOYSA-N 0.000 claims description 67
- TXHPORRYUKITDP-UHFFFAOYSA-N sulfamoylsulfamic acid Chemical group NS(=O)(=O)NS(O)(=O)=O TXHPORRYUKITDP-UHFFFAOYSA-N 0.000 claims description 60
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- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims description 9
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| PCT/EP2003/003207 WO2003082872A1 (en) | 2002-03-28 | 2003-03-27 | Novel pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy |
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| US20050154046A1 (en) * | 2004-01-12 | 2005-07-14 | Longgui Wang | Methods of treating an inflammatory-related disease |
| KR100824193B1 (ko) * | 2003-04-29 | 2008-04-21 | 화이자 인코포레이티드 | 고혈압 치료에 유용한5,7-디아미노피라졸로[4,3-ｄ]피리미딘 |
| EP2256106B1 (en) * | 2003-07-22 | 2015-05-06 | Astex Therapeutics Limited | 3,4-disubstituted 1H-pyrazole compounds and their use as cyclin dependent kinases (CDK) and glycogen synthase kinase-3 (GSK-3) modulators |
| US7572799B2 (en) | 2003-11-24 | 2009-08-11 | Pfizer Inc | Pyrazolo[4,3-d]pyrimidines as Phosphodiesterase Inhibitors |
| GB0327323D0 (en) * | 2003-11-24 | 2003-12-31 | Pfizer Ltd | Novel pharmaceuticals |
| GB0327319D0 (en) * | 2003-11-24 | 2003-12-24 | Pfizer Ltd | Novel pharmaceuticals |
| JP2007517052A (ja) * | 2003-12-23 | 2007-06-28 | ノバルティス アクチエンゲゼルシャフト | 二環式ヘテロ環式ｐ−３８キナーゼ阻害剤 |
| JP2007532526A (ja) | 2004-04-07 | 2007-11-15 | ファイザー・インク | ピラゾロ［４，３−ｄ］ピリミジン類 |
| MEP8409A (en) * | 2004-06-02 | 2011-12-20 | Fused heterocyclic compound | |
| JP5334414B2 (ja) | 2004-09-06 | 2013-11-06 | バイエル インテレクチュアル プロパティー ゲゼルシャフト ミット ベシュレンクテル ハフツング | 新規のピラゾロピリミジン |
| RU2425677C2 (ru) * | 2005-01-21 | 2011-08-10 | Астекс Терапьютикс Лимитед | Соединения, предназначенные для использования в фармацевтике |
| AR054425A1 (es) | 2005-01-21 | 2007-06-27 | Astex Therapeutics Ltd | Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico. |
| US8404718B2 (en) | 2005-01-21 | 2013-03-26 | Astex Therapeutics Limited | Combinations of pyrazole kinase inhibitors |
| PT1881985E (pt) * | 2005-05-12 | 2011-02-01 | Pfizer | Formas cristalinas anidras de n-[1-(2-etoxietil)-5-(n- -etil-n-metilamino)-7-(4-metilpiridin-2-il-amino)-1h- -pirazolo[4,3-d]pirimidino-3-carbonil]metanossulfonamida |
| US7932257B2 (en) | 2005-07-22 | 2011-04-26 | Sunesis Pharmaceuticals, Inc. | Substituted pyrazolo[4,3-d]pyrimidines as aurora kinase inhibitors |
| 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. |
| FR2899107B1 (fr) * | 2006-03-30 | 2008-06-13 | Neurokin Entpr Unipersonnelle | Utilisation de la (s)-roscovitine pour la fabrication d'un medicament |
| KR20090090336A (ko) | 2006-12-12 | 2009-08-25 | 다케다 야쿠힌 고교 가부시키가이샤 | 융합된 헤테로시클릭 화합물 |
| US20090099195A1 (en) * | 2007-05-08 | 2009-04-16 | Astrazeneca Ab | Therapeutic Compounds 570 |
| UA103195C2 (uk) | 2008-08-11 | 2013-09-25 | Глаксосмитклайн Ллк | Похідні пурину для застосування у лікуванні алергій, запальних та інфекційних захворювань |
| MX2011004680A (es) | 2008-11-06 | 2011-05-25 | Astrazeneca Ab | Moduladores de beta amiloide. |
| CZ2009358A3 (cs) * | 2009-06-03 | 2010-12-15 | C3 Bio Gmbh | 5,7-Disubstituované 3-isopropylpyrazolo[4,3-d]pyrimidiny pro použití jako lécivo a farmaceutické prípravky tyto látky obsahující |
| CZ302711B6 (cs) * | 2009-06-03 | 2011-09-14 | Univerzita Palackého v Olomouci | Substituované deriváty 6-(2-hydroxybenzylamino)purinu, jejich použití jako léciva a farmaceutické prípravky tyto slouceniny obsahující |
| AU2012244550C1 (en) * | 2011-04-21 | 2017-06-22 | Origenis Gmbh | Pyrazolo [4, 3-d] pyrimidines useful as kinase inhibitors |
| WO2013014052A1 (en) | 2011-07-22 | 2013-01-31 | Glaxosmithkline Llc | Composition |
| AR090650A1 (es) * | 2012-04-12 | 2014-11-26 | Alcon Res Ltd | Tratamiento para respuestas inflamatorias inducidas por microbios en el ojo |
| US9173872B2 (en) | 2012-08-24 | 2015-11-03 | Glaxosmithkline Llc | Pyrazolopyrimidine compounds |
| WO2014060112A1 (en) * | 2012-10-19 | 2014-04-24 | Origenis Gmbh | Pyrazolo[4,3-d]pyrimidines as kinase inhibitors |
| SMT201700378T1 (it) | 2012-11-20 | 2017-09-07 | Glaxosmithkline Llc | Nuovi composti |
| KR20150085081A (ko) | 2012-11-20 | 2015-07-22 | 글락소스미스클라인 엘엘씨 | 신규 화합물 |
| JP6216387B2 (ja) | 2012-11-20 | 2017-10-18 | グラクソスミスクライン・リミテッド・ライアビリティ・カンパニーＧｌａｘｏＳｍｉｔｈＫｌｉｎｅ ＬＬＣ | 新規化合物 |
| CN103405439B (zh) * | 2013-08-02 | 2014-12-31 | 上海市第十人民医院 | 嘧啶类化合物在制备真菌药物的应用 |
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| CN109996546B (zh) | 2016-09-30 | 2023-06-27 | 阿沙纳生物科学公司 | P2x3和/或p2x2/3化合物及方法 |
| CZ308484B6 (cs) * | 2018-02-05 | 2020-09-16 | Univerzita PalackĂ©ho v Olomouci | 5-Alkylthio-7-[(4-arylbenzyl)amino]-1(2)H-pyrazolo[4,3-d]pyrimidiny pro léčení lymfomů |
| EP3797776B1 (en) * | 2019-09-30 | 2025-07-23 | Universitätsmedizin Mainz | Cdk4/6 inhibitors for the treatment of psoriasis |
| WO2026123091A1 (pt) * | 2024-12-12 | 2026-06-18 | Centro Nacional De Pesquisa Em Energia E Materiais | Compostos inibidores da adenosina quinase, composição farmacêutica e seus usos |
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- 2002-03-28 DE DE60237425T patent/DE60237425D1/de not_active Expired - Lifetime
- 2002-03-28 EP EP02007163A patent/EP1348707B1/en not_active Expired - Lifetime
- 2002-03-28 DK DK02007163.5T patent/DK1348707T3/da active
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2003
- 2003-03-27 JP JP2003580337A patent/JP2005527565A/ja active Pending
- 2003-03-27 AU AU2003226731A patent/AU2003226731B2/en not_active Ceased
- 2003-03-27 WO PCT/EP2003/003207 patent/WO2003082872A1/en not_active Ceased
- 2003-03-27 CA CA2480409A patent/CA2480409C/en not_active Expired - Fee Related
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Also Published As
| Publication number | Publication date |
|---|---|
| ATE478872T1 (de) | 2010-09-15 |
| CA2480409A1 (en) | 2003-10-09 |
| EP1348707A1 (en) | 2003-10-01 |
| US20050080097A1 (en) | 2005-04-14 |
| AU2003226731A1 (en) | 2003-10-13 |
| AU2003226731B2 (en) | 2008-05-22 |
| CA2480409C (en) | 2010-06-22 |
| WO2003082872A1 (en) | 2003-10-09 |
| DK1348707T3 (da) | 2010-12-13 |
| DE60237425D1 (de) | 2010-10-07 |
| US7745450B2 (en) | 2010-06-29 |
| EP1348707B1 (en) | 2010-08-25 |
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