MXPA05002574A - Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina. - Google Patents
Pirazolopirimidinas como inhibidores de cinasa dependientes de ciclina.Info
- Publication number
- MXPA05002574A MXPA05002574A MXPA05002574A MXPA05002574A MXPA05002574A MX PA05002574 A MXPA05002574 A MX PA05002574A MX PA05002574 A MXPA05002574 A MX PA05002574A MX PA05002574 A MXPA05002574 A MX PA05002574A MX PA05002574 A MXPA05002574 A MX PA05002574A
- Authority
- MX
- Mexico
- Prior art keywords
- aryl
- alkyl
- group
- cycloalkyl
- heteroaryl
- Prior art date
Links
- 229940043378 cyclin-dependent kinase inhibitor Drugs 0.000 title description 5
- 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 abstract description 148
- 102000003903 Cyclin-dependent kinases Human genes 0.000 claims abstract description 25
- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims abstract description 25
- 108091007914 CDKs Proteins 0.000 claims abstract description 22
- 238000011282 treatment Methods 0.000 claims abstract description 19
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- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 15
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 11
- 230000005764 inhibitory process Effects 0.000 claims abstract description 4
- 125000000217 alkyl group Chemical group 0.000 claims description 95
- 125000003118 aryl group Chemical group 0.000 claims description 75
- -1 -C (02) R6 Chemical group 0.000 claims description 58
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- 125000001072 heteroaryl group Chemical group 0.000 claims description 46
- 150000003839 salts Chemical class 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 33
- 229910052736 halogen Inorganic materials 0.000 claims description 32
- 150000002367 halogens Chemical class 0.000 claims description 32
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 28
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 26
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- 125000004446 heteroarylalkyl group Chemical group 0.000 claims description 18
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- 125000005038 alkynylalkyl group Chemical group 0.000 claims description 6
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- WYWHKKSPHMUBEB-UHFFFAOYSA-N tioguanine Chemical compound N1C(N)=NC(=S)C2=C1N=CN2 WYWHKKSPHMUBEB-UHFFFAOYSA-N 0.000 claims description 6
- PLHJCIYEEKOWNM-HHHXNRCGSA-N tipifarnib Chemical compound CN1C=NC=C1[C@](N)(C=1C=C2C(C=3C=C(Cl)C=CC=3)=CC(=O)N(C)C2=CC=1)C1=CC=C(Cl)C=C1 PLHJCIYEEKOWNM-HHHXNRCGSA-N 0.000 claims description 6
- GHASVSINZRGABV-UHFFFAOYSA-N Fluorouracil Chemical compound FC1=CNC(=O)NC1=O GHASVSINZRGABV-UHFFFAOYSA-N 0.000 claims description 5
- 125000003545 alkoxy group Chemical group 0.000 claims description 5
- 125000001559 cyclopropyl group Chemical group [H]C1([H])C([H])([H])C1([H])* 0.000 claims description 5
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims description 5
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- YOHYSYJDKVYCJI-UHFFFAOYSA-N n-[3-[[6-[3-(trifluoromethyl)anilino]pyrimidin-4-yl]amino]phenyl]cyclopropanecarboxamide Chemical compound FC(F)(F)C1=CC=CC(NC=2N=CN=C(NC=3C=C(NC(=O)C4CC4)C=CC=3)C=2)=C1 YOHYSYJDKVYCJI-UHFFFAOYSA-N 0.000 claims description 4
- DWAFYCQODLXJNR-BNTLRKBRSA-L oxaliplatin Chemical compound O1C(=O)C(=O)O[Pt]11N[C@@H]2CCCC[C@H]2N1 DWAFYCQODLXJNR-BNTLRKBRSA-L 0.000 claims description 4
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- FPVKHBSQESCIEP-UHFFFAOYSA-N (8S)-3-(2-deoxy-beta-D-erythro-pentofuranosyl)-3,6,7,8-tetrahydroimidazo[4,5-d][1,3]diazepin-8-ol Natural products C1C(O)C(CO)OC1N1C(NC=NCC2O)=C2N=C1 FPVKHBSQESCIEP-UHFFFAOYSA-N 0.000 claims description 3
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Landscapes
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| CA2273083C (en) | 1996-12-03 | 2012-09-18 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| EP2186811A1 (en) | 2002-08-23 | 2010-05-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto, analogues and uses thereof |
| US7649006B2 (en) | 2002-08-23 | 2010-01-19 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US6921769B2 (en) | 2002-08-23 | 2005-07-26 | Sloan-Kettering Institute For Cancer Research | Synthesis of epothilones, intermediates thereto and analogues thereof |
| US7196078B2 (en) * | 2002-09-04 | 2007-03-27 | Schering Corpoartion | Trisubstituted and tetrasubstituted pyrazolopyrimidines as cyclin dependent kinase inhibitors |
| AR049769A1 (es) * | 2004-01-22 | 2006-09-06 | Novartis Ag | Derivados de pirazolo(1,5-a)pirimidin 7-il-amina para utilizarse en el tratamiento de enfermedades dependientes de la quinasa de proteina |
| US20080287405A1 (en) * | 2004-05-14 | 2008-11-20 | Thannickal Victor J | Compositions and Methods Relating to Protein Kinase Inhibitors |
| US20080125404A1 (en) * | 2004-08-27 | 2008-05-29 | Cyclacel Limited | Purine and Pyrimidine Cdk Inhitbitors and Their use for The Treatment of Autoimmune Diseases |
| ES2368930T3 (es) * | 2004-09-06 | 2011-11-23 | Bayer Pharma Aktiengesellschaft | Pirazolopirimidinas como inhibidores de proteína cinasa b (akt). |
| CN101103033B (zh) | 2005-01-05 | 2010-08-04 | 尼科梅德有限责任公司 | 作为pde2抑制剂的三唑并酞嗪 |
| CA2591991C (en) | 2005-01-05 | 2013-11-19 | Altana Pharma Ag | Triazolophthalazines |
| WO2007005541A2 (en) * | 2005-06-30 | 2007-01-11 | Philadelphia Health & Education Corporation, D/B/A Drexel University College Of Medicine | Small molecule inhibitors against west nile virus replication |
| JP2009507843A (ja) * | 2005-09-09 | 2009-02-26 | シェーリング コーポレイション | アザ縮合サイクリン依存性キナーゼ阻害剤 |
| WO2008037477A1 (en) | 2006-09-29 | 2008-04-03 | Novartis Ag | Pyrazolopyrimidines as p13k lipid kinase inhibitors |
| EA200970353A1 (ru) * | 2006-10-06 | 2009-10-30 | Такеда Фармасьютикал Компани Лимитед | Комбинированное лекарственное средство |
| 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 |
| US10953012B2 (en) | 2011-04-26 | 2021-03-23 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of pask |
| WO2014066743A1 (en) | 2012-10-25 | 2014-05-01 | Bioenergenix | Heterocyclic compounds for the inhibition of pask |
| US10392389B2 (en) | 2012-10-25 | 2019-08-27 | Bioenergenix Llc | Heterocyclic compounds for the inhibition of PASK |
| KR20150130491A (ko) | 2013-03-13 | 2015-11-23 | 제넨테크, 인크. | 피라졸로 화합물 및 그것의 용도 |
| SG11201607895PA (en) * | 2014-05-28 | 2016-12-29 | Novartis Ag | Novel pyrazolo pyrimidine derivatives and their use as malt1 inhibitors |
| MX2018006250A (es) | 2015-11-18 | 2018-09-05 | Genzyme Corp | Biomarcador de enfermedad poliquistica renal y usos del mismo. |
| SI3658557T1 (sl) | 2017-07-28 | 2024-10-30 | Takeda Pharmaceutical Company Limited | Zaviralci TYK2 in njihova uporaba |
| 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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|---|---|---|---|---|
| JPS4116288Y1 (https=) | 1964-11-07 | 1966-07-28 | ||
| AU651986B2 (en) | 1991-04-22 | 1994-08-11 | Otsuka Pharmaceutical Factory, Inc. | Pyrazolo{1,5-a}pyrimidine derivative and anti-inflammatory containing the same |
| US5571813A (en) * | 1993-06-10 | 1996-11-05 | Beiersdorf-Lilly Gmbh | Fused pyrimidine compounds and their use as pharmaceuticals |
| EP0628559B1 (en) | 1993-06-10 | 2002-04-03 | Beiersdorf-Lilly GmbH | Pyrimidine compounds and their use as pharmaceuticals |
| GB9325074D0 (en) * | 1993-12-07 | 1994-02-02 | Zeneca Ltd | Bicyclic heterocycles |
| WO1995035298A1 (en) * | 1994-06-21 | 1995-12-28 | Otsuka Pharmaceutical Factory, Inc. | PYRAZOLO[1,5-a]PYRIMIDINE DERIVATIVE |
| US5502137A (en) | 1994-11-25 | 1996-03-26 | Eastman Chemical Company | Polyether glycols and alcohols derived from 3,4-epoxy-1-butene, tetrahydrofuran and an initiator |
| US5919815A (en) * | 1996-05-22 | 1999-07-06 | Neuromedica, Inc. | Taxane compounds and compositions |
| US6191131B1 (en) | 1997-07-23 | 2001-02-20 | Dupont Pharmaceuticals Company | Azolo triazines and pyrimidines |
| US6262096B1 (en) * | 1997-11-12 | 2001-07-17 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6040321A (en) * | 1997-11-12 | 2000-03-21 | Bristol-Myers Squibb Company | Aminothiazole inhibitors of cyclin dependent kinases |
| US6413974B1 (en) * | 1998-02-26 | 2002-07-02 | Aventis Pharmaceuticals Inc. | 6,9,-disubstituted 2-[trans-(4-aminocyclohexyl) amino] purines |
| US6383790B1 (en) | 1999-01-11 | 2002-05-07 | Princeton University | High affinity protein kinase inhibitors |
| CA2380389A1 (en) | 1999-07-26 | 2001-02-01 | Banyu Pharmaceutical Co., Ltd. | Biarylurea derivatives |
| FR2805160B1 (fr) | 2000-02-23 | 2002-04-05 | Oreal | Compositions pour la teinture d'oxydation des fibres keratiniques comprenant un n(2-hydroxybenzene)-carbramate ou un n-(2-hydroxybenzene)-uree et une pyrazolopyrimidine, et procedes de teinture |
| CA2417254A1 (en) | 2000-07-26 | 2002-02-07 | 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) |
| US7662826B2 (en) | 2002-04-23 | 2010-02-16 | Shionogi & Co., Ltd. | Pyrazolo [1,5-a] pyrimidine derivative and nad (p) h oxidase inhibitor containing the same |
| DE10223917A1 (de) | 2002-05-29 | 2003-12-11 | Bayer Cropscience Ag | Pyrazolopyrimidine |
-
2003
- 2003-09-03 CA CA002497539A patent/CA2497539A1/en not_active Abandoned
- 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 TW TW092124350A patent/TW200412966A/zh unknown
- 2003-09-03 JP JP2004534490A patent/JP2006500391A/ja not_active Ceased
- 2003-09-03 US US10/654,163 patent/US7084271B2/en not_active Expired - Fee Related
- 2003-09-03 MX MXPA05002574A patent/MXPA05002574A/es active IP Right Grant
- 2003-09-03 NZ NZ539163A patent/NZ539163A/en unknown
- 2003-09-03 CN CNA038249081A patent/CN1694705A/zh active Pending
- 2003-09-03 AU AU2003265901A patent/AU2003265901B2/en not_active Ceased
- 2003-09-03 AR ARP030103190A patent/AR041135A1/es unknown
- 2003-09-03 KR KR1020057003548A patent/KR20050057072A/ko not_active Withdrawn
- 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 |
|---|---|
| WO2004022062A1 (en) | 2004-03-18 |
| AU2003265901A1 (en) | 2004-03-29 |
| ZA200501854B (en) | 2005-09-12 |
| AR041135A1 (es) | 2005-05-04 |
| US7468372B2 (en) | 2008-12-23 |
| US20060173017A1 (en) | 2006-08-03 |
| PE20040998A1 (es) | 2004-12-30 |
| NZ539163A (en) | 2007-03-30 |
| EP1545533A1 (en) | 2005-06-29 |
| US20040102452A1 (en) | 2004-05-27 |
| JP2006500391A (ja) | 2006-01-05 |
| CN1694705A (zh) | 2005-11-09 |
| US7084271B2 (en) | 2006-08-01 |
| JP2011074088A (ja) | 2011-04-14 |
| CA2497539A1 (en) | 2004-03-18 |
| KR20050057072A (ko) | 2005-06-16 |
| AU2003265901B2 (en) | 2006-09-14 |
| TW200412966A (en) | 2004-08-01 |
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Legal Events
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| FG | Grant or registration |