ZA200501854B - Pyrazolopyrimidines as cyclin dependent kinase inhibitors. - Google Patents
Pyrazolopyrimidines as cyclin dependent kinase inhibitors. Download PDFInfo
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- ZA200501854B ZA200501854B ZA200501854A ZA200501854A ZA200501854B ZA 200501854 B ZA200501854 B ZA 200501854B ZA 200501854 A ZA200501854 A ZA 200501854A ZA 200501854 A ZA200501854 A ZA 200501854A ZA 200501854 B ZA200501854 B ZA 200501854B
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- ZA
- South Africa
- Prior art keywords
- compound
- aryl
- alkyl
- group
- cycloalkyl
- Prior art date
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- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 title description 7
- APXRHPDHORGIEB-UHFFFAOYSA-N 1H-pyrazolo[4,3-d]pyrimidine Chemical class N1=CN=C2C=NNC2=C1 APXRHPDHORGIEB-UHFFFAOYSA-N 0.000 title description 3
- 239000002875 cyclin dependent kinase inhibitor Substances 0.000 title description 3
- 150000001875 compounds Chemical class 0.000 claims description 75
- 125000000217 alkyl group Chemical group 0.000 claims description 74
- 125000003118 aryl group Chemical group 0.000 claims description 62
- 125000000753 cycloalkyl group Chemical group 0.000 claims description 47
- 125000001072 heteroaryl group Chemical group 0.000 claims description 41
- 229910052736 halogen Inorganic materials 0.000 claims description 31
- 150000002367 halogens Chemical class 0.000 claims description 31
- 125000000623 heterocyclic group Chemical group 0.000 claims description 24
- 239000000203 mixture Substances 0.000 claims description 22
- 238000000034 method Methods 0.000 claims description 21
- 125000004415 heterocyclylalkyl group Chemical group 0.000 claims description 19
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims description 18
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims description 18
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 18
- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 18
- -1 -C(O2)R® Chemical group 0.000 claims description 17
- 238000011282 treatment Methods 0.000 claims description 17
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 15
- 108091007914 CDKs Proteins 0.000 claims description 13
- 201000010099 disease Diseases 0.000 claims description 13
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 13
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- 125000000304 alkynyl group Chemical group 0.000 claims description 10
- 150000003839 salts Chemical class 0.000 claims description 8
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- 201000011510 cancer Diseases 0.000 claims description 6
- 229910052739 hydrogen Inorganic materials 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 4
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 4
- 229910052757 nitrogen Inorganic materials 0.000 claims description 4
- 241000124008 Mammalia Species 0.000 claims description 3
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Landscapes
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| WO1999001124A1 (en) * | 1996-12-03 | 1999-01-14 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| DE60330407D1 (de) | 2002-08-23 | 2010-01-14 | Sloan Kettering Inst Cancer | Synthese von Epothilonen, Zwischenprodukte davon, Analoga und ihre Verwendung |
| US7196078B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| PE20051089A1 (es) * | 2004-01-22 | 2006-01-25 | Novartis Ag | Derivados de pirazolo [1,5-a] pirimidin-7-il-amina como inhibidores de quinasa de proteina |
| WO2005112936A1 (en) * | 2004-05-14 | 2005-12-01 | The Regents Of The University Of Michigan | Compositions and methods relating to protein kinase inhibitors |
| PL1799230T3 (pl) * | 2004-08-27 | 2013-05-31 | Cyclacel Ltd | Purynowe i pirymidynowe inhibitory CDK i ich zastosowanie do leczenia chorób autoimmunologicznych |
| AU2005281704A1 (en) * | 2004-09-06 | 2006-03-16 | Nycomed Gmbh | Novel pyrazolopyrimidines |
| BRPI0606379A2 (pt) | 2005-01-05 | 2009-06-23 | Nycomed Gmbh | triazolftalazinas |
| EP1874775B1 (en) | 2005-01-05 | 2012-10-10 | Nycomed GmbH | Triazolophthalazines as pde2-inhibitors |
| US20100075993A1 (en) * | 2005-06-30 | 2010-03-25 | Drexel University | Small molecule inhibitors against west nile virus replication |
| CA2621983A1 (en) * | 2005-09-09 | 2007-03-22 | Schering Corporation | Azafused cyclin dependent kinase inhibitors |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| AU2007307489A1 (en) * | 2006-10-06 | 2008-04-17 | Takeda Pharmaceutical Company Limited | Combination drug |
| EP2473041B1 (en) | 2009-09-04 | 2018-03-07 | Merck Sharp & Dohme Corp. | Modulators of cell cycle checkpoints and their use in combination with checkpoint kinase inhibitors |
| US8883801B2 (en) | 2010-08-23 | 2014-11-11 | Merck Sharp & Dohme Corp. | Substituted pyrazolo[1,5-a]pyrimidines as mTOR inhibitors |
| WO2012149157A2 (en) | 2011-04-26 | 2012-11-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2014066795A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2014066743A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| WO2014139326A1 (en) * | 2013-03-13 | 2014-09-18 | Genentech, Inc. | Pyrazolo compounds and uses thereof |
| ES2738695T3 (es) * | 2014-05-28 | 2020-01-24 | Novartis Ag | Nuevos Derivados de Pirazolo Pirimidina y su uso como inhibidores de MALT1 |
| EA201891170A1 (ru) | 2015-11-18 | 2018-11-30 | Джензим Корпорейшн | Биомаркер поликистозной болезни почек и варианты его применения |
| KR102717819B1 (ko) | 2017-07-28 | 2024-10-14 | 다케다 야쿠힌 고교 가부시키가이샤 | Tyk2 억제제 및 이의 용도 |
| CN113248500B (zh) * | 2021-06-10 | 2021-10-19 | 中国药科大学 | 氮杂吲哚嘧啶胺杂环化合物及其制备方法和应用 |
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| US5571813A (en) | 1993-06-10 | 1996-11-05 | Beiersdorf-Lilly Gmbh | Fused pyrimidine compounds and their use as pharmaceuticals |
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| GB9325074D0 (en) * | 1993-12-07 | 1994-02-02 | Zeneca Ltd | Bicyclic heterocycles |
| US5707997A (en) | 1994-06-21 | 1998-01-13 | Otsuka Pharmaceutical Factory, Inc. | Pyrazolo 1,5-a!pyrimidine derivative |
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| US5919815A (en) | 1996-05-22 | 1999-07-06 | Neuromedica, Inc. | Taxane compounds and compositions |
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| DK1140938T3 (da) | 1999-01-11 | 2003-12-22 | Univ Princeton | Højaffinitetsinhibitorer for målvalidering og anvendelser heraf |
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| PL365170A1 (en) | 2000-07-26 | 2004-12-27 | Bristol-Myers Squibb Company | N-[5-[[[5-alkyl-2-oxazolyl]methyl]thio]-2-thiazolyl] carboxamide inhibitors of cyclin dependent kinases |
| US7067520B2 (en) | 2000-11-17 | 2006-06-27 | Ishihara Sangyo Kaisha, Ltd. | Preventive or therapeutic medicines for diabetes containing fused-heterocyclic compounds or their salts |
| FR2817469B1 (fr) | 2000-12-04 | 2003-04-18 | Oreal | Composition de coloration, procede d'obtention et utilisation pour la coloration de fibres keratiniques |
| EP1345941A1 (fr) | 2000-12-20 | 2003-09-24 | Societe De Conseils De Recherches Et D'applications Scientifiques (S.C.R.A.S.) | Inhibiteurs de kinases dependantes des cylines (cdk) et de la glycogene synthase kinase-3 (gsk-3) |
| EP1505068A4 (en) | 2002-04-23 | 2008-03-19 | Shionogi & Co | PYRAZOLO (1,5-a) PYRIMIDINE DERIVATIVE AND INHIBITOR OF NAD (P) H OXIDASE CONTAINING SAID DERIVATIVE |
| DE10223917A1 (de) | 2002-05-29 | 2003-12-11 | Bayer Cropscience Ag | Pyrazolopyrimidine |
-
2003
- 2003-09-03 NZ NZ539163A patent/NZ539163A/en unknown
- 2003-09-03 TW TW092124350A patent/TW200412966A/zh unknown
- 2003-09-03 WO PCT/US2003/027564 patent/WO2004022062A1/en not_active Ceased
- 2003-09-03 EP EP03794594A patent/EP1545533A1/en not_active Withdrawn
- 2003-09-03 US US10/654,163 patent/US7084271B2/en not_active Expired - Fee Related
- 2003-09-03 CA CA002497539A patent/CA2497539A1/en not_active Abandoned
- 2003-09-03 JP JP2004534490A patent/JP2006500391A/ja not_active Ceased
- 2003-09-03 KR KR1020057003548A patent/KR20050057072A/ko not_active Withdrawn
- 2003-09-03 MX MXPA05002574A patent/MXPA05002574A/es active IP Right Grant
- 2003-09-03 AU AU2003265901A patent/AU2003265901B2/en not_active Ceased
- 2003-09-03 AR ARP030103190A patent/AR041135A1/es unknown
- 2003-09-03 CN CNA038249081A patent/CN1694705A/zh active Pending
- 2003-09-04 PE PE2003000898A patent/PE20040998A1/es not_active Application Discontinuation
-
2005
- 2005-03-03 ZA ZA200501854A patent/ZA200501854B/en unknown
-
2006
- 2006-03-31 US US11/395,965 patent/US7468372B2/en not_active Expired - Fee Related
-
2011
- 2011-01-13 JP JP2011005344A patent/JP2011074088A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| US20060173017A1 (en) | 2006-08-03 |
| US7468372B2 (en) | 2008-12-23 |
| AR041135A1 (es) | 2005-05-04 |
| JP2011074088A (ja) | 2011-04-14 |
| TW200412966A (en) | 2004-08-01 |
| AU2003265901A1 (en) | 2004-03-29 |
| KR20050057072A (ko) | 2005-06-16 |
| NZ539163A (en) | 2007-03-30 |
| AU2003265901B2 (en) | 2006-09-14 |
| CN1694705A (zh) | 2005-11-09 |
| JP2006500391A (ja) | 2006-01-05 |
| PE20040998A1 (es) | 2004-12-30 |
| EP1545533A1 (en) | 2005-06-29 |
| US7084271B2 (en) | 2006-08-01 |
| US20040102452A1 (en) | 2004-05-27 |
| CA2497539A1 (en) | 2004-03-18 |
| MXPA05002574A (es) | 2005-09-08 |
| WO2004022062A1 (en) | 2004-03-18 |
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