JP2005527565A5 - - Google Patents
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- Publication number
- JP2005527565A5 JP2005527565A5 JP2003580337A JP2003580337A JP2005527565A5 JP 2005527565 A5 JP2005527565 A5 JP 2005527565A5 JP 2003580337 A JP2003580337 A JP 2003580337A JP 2003580337 A JP2003580337 A JP 2003580337A JP 2005527565 A5 JP2005527565 A5 JP 2005527565A5
- Authority
- JP
- Japan
- Prior art keywords
- pyrimidine
- group
- acceptable salt
- pharmaceutically acceptable
- pyrazolo
- 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
- 150000001875 compounds Chemical class 0.000 claims description 8
- 238000000034 method Methods 0.000 claims description 8
- -1 hydroxy, methoxy, amino Chemical group 0.000 claims description 5
- 230000002401 inhibitory effect Effects 0.000 claims description 4
- 150000003839 salts Chemical class 0.000 claims 14
- DSKLYHDHQJANOE-UHFFFAOYSA-N pyrazolo[4,3-d]pyrimidine Chemical class C1=NC=N[C]2C=NN=C21 DSKLYHDHQJANOE-UHFFFAOYSA-N 0.000 claims 12
- 239000003814 drug Substances 0.000 claims 11
- ZMXDDKWLCZADIW-UHFFFAOYSA-N N,N-Dimethylformamide Chemical compound CN(C)C=O ZMXDDKWLCZADIW-UHFFFAOYSA-N 0.000 claims 9
- 238000002360 preparation method Methods 0.000 claims 9
- 239000003937 drug carrier Substances 0.000 claims 6
- 125000001424 substituent group Chemical group 0.000 claims 6
- CZPWVGJYEJSRLH-UHFFFAOYSA-N Pyrimidine Chemical compound C1=CN=CN=C1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 claims 4
- 125000000217 alkyl group Chemical group 0.000 claims 4
- 239000000460 chlorine Substances 0.000 claims 4
- 241000233866 Fungi Species 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 208000030852 Parasitic disease Diseases 0.000 claims 3
- 125000003710 aryl alkyl group Chemical group 0.000 claims 3
- 201000011510 cancer Diseases 0.000 claims 3
- 238000005660 chlorination reaction Methods 0.000 claims 3
- 125000001309 chloro group Chemical group Cl* 0.000 claims 3
- 208000027866 inflammatory disease Diseases 0.000 claims 3
- 210000004962 mammalian cell Anatomy 0.000 claims 3
- 238000004519 manufacturing process Methods 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 claims 2
- HEDRZPFGACZZDS-UHFFFAOYSA-N Chloroform Chemical compound ClC(Cl)Cl HEDRZPFGACZZDS-UHFFFAOYSA-N 0.000 claims 2
- 208000036142 Viral infection Diseases 0.000 claims 2
- 241000700605 Viruses Species 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 229910052801 chlorine Inorganic materials 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- RLOWWWKZYUNIDI-UHFFFAOYSA-N phosphinic chloride Chemical compound ClP=O RLOWWWKZYUNIDI-UHFFFAOYSA-N 0.000 claims 2
- 230000009385 viral infection Effects 0.000 claims 2
- 230000003612 virological effect Effects 0.000 claims 2
- FMCAFXHLMUOIGG-JTJHWIPRSA-N (2s)-2-[[(2r)-2-[[(2s)-2-[[(2r)-2-formamido-3-sulfanylpropanoyl]amino]-3-methylbutanoyl]amino]-3-(4-hydroxy-2,5-dimethylphenyl)propanoyl]amino]-4-methylsulfanylbutanoic acid Chemical compound O=CN[C@@H](CS)C(=O)N[C@@H](C(C)C)C(=O)N[C@@H](C(=O)N[C@@H](CCSC)C(O)=O)CC1=CC(C)=C(O)C=C1C FMCAFXHLMUOIGG-JTJHWIPRSA-N 0.000 claims 1
- JFZSDNLQDTYVEE-UHFFFAOYSA-N 1,4-dihydropyrazolo[4,3-d]pyrimidin-7-one Chemical compound O=C1N=CNC2=C1NN=C2 JFZSDNLQDTYVEE-UHFFFAOYSA-N 0.000 claims 1
- 108060003345 Adrenergic Receptor Proteins 0.000 claims 1
- 102000017910 Adrenergic receptor Human genes 0.000 claims 1
- 241000710831 Flavivirus Species 0.000 claims 1
- 241000700588 Human alphaherpesvirus 1 Species 0.000 claims 1
- 241000701074 Human alphaherpesvirus 2 Species 0.000 claims 1
- 241000701085 Human alphaherpesvirus 3 Species 0.000 claims 1
- 241000701041 Human betaherpesvirus 7 Species 0.000 claims 1
- 241001502974 Human gammaherpesvirus 8 Species 0.000 claims 1
- 241000701027 Human herpesvirus 6 Species 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 102100037601 P2X purinoceptor 4 Human genes 0.000 claims 1
- 241001631646 Papillomaviridae Species 0.000 claims 1
- 108010080192 Purinergic Receptors Proteins 0.000 claims 1
- 241000700618 Vaccinia virus Species 0.000 claims 1
- 230000004913 activation Effects 0.000 claims 1
- 102000030621 adenylate cyclase Human genes 0.000 claims 1
- 108060000200 adenylate cyclase Proteins 0.000 claims 1
- 230000001800 adrenalinergic effect Effects 0.000 claims 1
- 230000032683 aging Effects 0.000 claims 1
- 125000003545 alkoxy group Chemical group 0.000 claims 1
- 125000003277 amino group Chemical group 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 210000002459 blastocyst Anatomy 0.000 claims 1
- 239000012830 cancer therapeutic Substances 0.000 claims 1
- 230000010261 cell growth Effects 0.000 claims 1
- 239000003795 chemical substances by application Substances 0.000 claims 1
- 238000010367 cloning Methods 0.000 claims 1
- 239000002537 cosmetic Substances 0.000 claims 1
- 238000002425 crystallisation Methods 0.000 claims 1
- 230000008025 crystallization Effects 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 238000000605 extraction Methods 0.000 claims 1
- 230000004720 fertilization Effects 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical group 0.000 claims 1
- 125000004404 heteroalkyl group Chemical group 0.000 claims 1
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 1
- 230000003308 immunostimulating effect Effects 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- 239000003112 inhibitor Substances 0.000 claims 1
- 238000002955 isolation Methods 0.000 claims 1
- 210000000287 oocyte Anatomy 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 230000000638 stimulation Effects 0.000 claims 1
- 238000006467 substitution reaction Methods 0.000 claims 1
- 241000701161 unidentified adenovirus Species 0.000 claims 1
- 241001529453 unidentified herpesvirus Species 0.000 claims 1
- 241001430294 unidentified retrovirus Species 0.000 claims 1
- OKKJLVBELUTLKV-UHFFFAOYSA-N Methanol Chemical compound OC OKKJLVBELUTLKV-UHFFFAOYSA-N 0.000 description 24
- BDAGIHXWWSANSR-UHFFFAOYSA-N Formic acid Chemical compound OC=O BDAGIHXWWSANSR-UHFFFAOYSA-N 0.000 description 4
- 235000019253 formic acid Nutrition 0.000 description 4
- 0 Cc1*(C)c(C(*)=N*2)c2c(O)n1 Chemical compound Cc1*(C)c(C(*)=N*2)c2c(O)n1 0.000 description 3
- 108091000080 Phosphotransferase Proteins 0.000 description 2
- 102000020233 phosphotransferase Human genes 0.000 description 2
- 229940083082 pyrimidine derivative acting on arteriolar smooth muscle Drugs 0.000 description 2
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP02007163A EP1348707B1 (en) | 2002-03-28 | 2002-03-28 | Pyrazolo[4,3-d]pyrimidines, processes for their preparation and methods for therapy |
| 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 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2005527565A JP2005527565A (ja) | 2005-09-15 |
| JP2005527565A5 true JP2005527565A5 (enExample) | 2010-02-18 |
Family
ID=27798825
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2003580337A Pending JP2005527565A (ja) | 2002-03-28 | 2003-03-27 | 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 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US7745450B2 (enExample) |
| EP (1) | EP1348707B1 (enExample) |
| JP (1) | JP2005527565A (enExample) |
| AT (1) | ATE478872T1 (enExample) |
| AU (1) | AU2003226731B2 (enExample) |
| CA (1) | CA2480409C (enExample) |
| DE (1) | DE60237425D1 (enExample) |
| DK (1) | DK1348707T3 (enExample) |
| WO (1) | WO2003082872A1 (enExample) |
Families Citing this family (38)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| EP3271017A4 (en) * | 2015-03-16 | 2018-11-14 | Monash University | Treatment of skin conditions |
| CZ307147B6 (cs) * | 2015-05-14 | 2018-02-07 | Ústav experimentální botaniky AV ČR, v. v. i. | 5-Substituované 7-[4-(2-pyridyl)fenylmethylamino]-3-isopropylpyrazolo[4,3-d]pyrimidiny, jejich použití jako léčiva, a farmaceutické přípravky |
| 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 |
Family Cites Families (19)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3988338A (en) * | 1974-04-24 | 1976-10-26 | Wisconsin Alumni Research Foundation | 4-Substituted amino-2-substituted thio-pyrrolo-[2,3-d]pyrimidine derivatives |
| GB9013750D0 (en) * | 1990-06-20 | 1990-08-08 | Pfizer Ltd | Therapeutic agents |
| US5276143A (en) | 1990-12-21 | 1994-01-04 | E. I. Du Pont De Nemours And Company | Dideoxyfructonucleosides and deoxyfructonucleotides |
| US5801015A (en) | 1995-06-05 | 1998-09-01 | Mitotix, Inc. | Nucleic acid encoding a Candida cell cycle regulatory protein, TYP1 polypeptide |
| US6200980B1 (en) | 1995-06-07 | 2001-03-13 | Cell Pathways, Inc. | Method of treating a patient having precancerous lesions with phenyl purinone derivatives |
| DK0778277T3 (da) * | 1995-12-08 | 2003-10-27 | Pfizer | Substituerede heterocycliske derivater som CRF antagonister |
| PL332040A1 (en) * | 1996-08-28 | 1999-08-16 | Pfizer | Substitution 6,5-heterobicyclic derivatives |
| US5723608A (en) * | 1996-12-31 | 1998-03-03 | Neurogen Corporation | 3-aryl substituted pyrazolo 4,3-d!pyrimidine derivatives; corticotropin-releasing factor receptor (CRF1) specific ligands |
| CA2288910C (en) * | 1997-04-25 | 2003-06-24 | Pfizer Inc. | Pyrazolopyrimidinones for sexual dysfunction |
| US5985848A (en) * | 1997-10-14 | 1999-11-16 | Albert Einstein College Of Medicine Of Yeshiva University | Inhibitors of nucleoside metabolism |
| ES2203078T3 (es) * | 1998-04-20 | 2004-04-01 | Pfizer Inc. | Parazolopirimidinonas inhibidoras de gmpc pde5 para el tratamiento de la disfuncion sexual. |
| ES2205945T3 (es) * | 1998-10-23 | 2004-05-01 | Pfizer Inc. | Pirazolopirimidinonas inhibidoras de gmpc pde5 para el tratamiento de disfunciones sexuales. |
| WO2001019827A1 (en) * | 1999-09-13 | 2001-03-22 | Cipla Ltd. | A novel process for the synthesis of sildenafil citrate |
| ES2272297T3 (es) * | 1999-10-12 | 2007-05-01 | Lilly Icos Llc | Medicamento destinado al tratamiento de neuropatias. |
| DE10060388A1 (de) * | 2000-12-05 | 2002-06-06 | Merck Patent Gmbh | Verwendung von Pyrazolo [4,3-d]pyrimidinen |
| BR0115995A (pt) * | 2000-12-19 | 2004-01-13 | Merck Patent Gmbh | Formulação farmacêutica compreendendo pirazolo[4,3-d]pirimidinas e antitrombóticos, antagonistas de cálcio, prostaglandinas ou derivados de prostaglandina |
| GB0106661D0 (en) * | 2001-03-16 | 2001-05-09 | Pfizer Ltd | Pharmaceutically active compounds |
| KR20040053210A (ko) * | 2001-11-02 | 2004-06-23 | 화이자 프로덕츠 인크. | Ｐｄｅ9 억제제를 사용한 인슐린 저항 증후군 및 2형당뇨병의 치료 |
| US20030195205A1 (en) * | 2001-11-02 | 2003-10-16 | Pfizer Inc. | PDE9 inhibitors for treating cardiovascular disorders |
-
2002
- 2002-03-28 AT AT02007163T patent/ATE478872T1/de not_active IP Right Cessation
- 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
-
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
-
2004
- 2004-09-28 US US10/952,087 patent/US7745450B2/en not_active Expired - Fee Related
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