EA020439B1 - Ингибиторы циклинзависимых киназ - Google Patents
Ингибиторы циклинзависимых киназ Download PDFInfo
- Publication number
- EA020439B1 EA020439B1 EA201000554A EA201000554A EA020439B1 EA 020439 B1 EA020439 B1 EA 020439B1 EA 201000554 A EA201000554 A EA 201000554A EA 201000554 A EA201000554 A EA 201000554A EA 020439 B1 EA020439 B1 EA 020439B1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- alkyl
- phenyl
- group
- pyrimidin
- methoxy
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 claims abstract description 276
- -1 pyrazolo [1,5-a] pyrimidinyl Chemical group 0.000 claims description 243
- 125000000217 alkyl group Chemical group 0.000 claims description 74
- 125000003118 aryl group Chemical group 0.000 claims description 45
- 125000001424 substituent group Chemical group 0.000 claims description 45
- 125000001072 heteroaryl group Chemical group 0.000 claims description 44
- 229910052736 halogen Inorganic materials 0.000 claims description 40
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 40
- 150000002367 halogens Chemical class 0.000 claims description 39
- 125000000623 heterocyclic group Chemical group 0.000 claims description 39
- 229910052739 hydrogen Inorganic materials 0.000 claims description 39
- 239000001257 hydrogen Substances 0.000 claims description 32
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 29
- 150000003839 salts Chemical class 0.000 claims description 27
- 125000004452 carbocyclyl group Chemical group 0.000 claims description 26
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 25
- 125000004076 pyridyl group Chemical group 0.000 claims description 23
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- 125000000714 pyrimidinyl group Chemical group 0.000 claims description 17
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- 125000004632 tetrahydrothiopyranyl group Chemical group S1C(CCCC1)* 0.000 claims description 10
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- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
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- C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
- C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
- C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
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- C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
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Landscapes
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| CN102272120B (zh) * | 2008-11-07 | 2013-12-25 | H.隆德贝克有限公司 | 生物活性酰胺 |
| UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| US8906914B2 (en) | 2009-08-18 | 2014-12-09 | Janssen Pharmaceutica Nv | Ethylene diamine modulators of fatty acid hydrolase |
| EP2544686A4 (en) | 2010-02-05 | 2013-06-26 | Whitehead Biomedical Inst | COMBINATION PROCEDURE FOR THE TREATMENT OF A DISEASE |
| CN102834380B (zh) * | 2010-03-10 | 2015-04-01 | 阿斯利康公司 | 蛋白激酶的抑制剂 |
| JP2013107824A (ja) * | 2010-03-17 | 2013-06-06 | Dainippon Sumitomo Pharma Co Ltd | 新規単環ピリミジン誘導体 |
| EP2571361A4 (en) | 2010-05-19 | 2013-11-13 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| CA2802641C (en) * | 2010-07-13 | 2019-03-12 | Nidhi Arora | Pyrazolo [1, 5a] pyrimidine and thieno [3, 2b] pyrimidine derivatives as irak4 modulators |
| CN103339110A (zh) * | 2011-01-28 | 2013-10-02 | 诺瓦提斯公司 | 作为cdk9抑制剂的取代的杂-联芳基化合物及其用途 |
| WO2012101064A1 (en) * | 2011-01-28 | 2012-08-02 | Novartis Ag | N-acyl pyrimidine biaryl compounds as protein kinase inhibitors |
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| EP2561867A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | CDK9 inhibitors in the treatment of midline carcinoma |
| CN103958510B (zh) | 2011-10-03 | 2016-10-19 | 北卡罗来纳大学教堂山分校 | 用于治疗癌症的吡咯并嘧啶化合物 |
| WO2013059634A1 (en) | 2011-10-20 | 2013-04-25 | The Regents Of The University Of California | Use of cdk9 inhibitors to reduce cartilage degradation |
| US8541577B2 (en) * | 2011-11-10 | 2013-09-24 | Allergan, Inc. | Aryl urea derivatives as N-formyl peptide receptors like-1 (FPRL-1) receptor modulators |
| SMT201800608T1 (it) | 2012-04-24 | 2019-01-11 | Vertex Pharma | Inibitori di dna-pk |
| BR112014028424A2 (pt) | 2012-05-22 | 2018-04-24 | Univ North Carolina Chapel Hill | compostos de pirimidina para o tratamento de câncer |
| EP2909211A4 (en) | 2012-10-17 | 2016-06-22 | Univ North Carolina | PYRAZOLOPYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| EP2925752A4 (en) | 2012-11-27 | 2016-06-01 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| AU2014244555B2 (en) | 2013-03-12 | 2018-06-28 | Vertex Pharmaceuticals Incorporated | DNA-PK inhibitors |
| MX2015012386A (es) | 2013-03-13 | 2016-02-03 | Abbvie Inc | Inhibidores de la cinasa cdk9. |
| CN105189481A (zh) | 2013-03-13 | 2015-12-23 | 艾伯维公司 | 吡啶cdk9激酶抑制剂 |
| BR112015023356A2 (pt) | 2013-03-14 | 2017-07-18 | Abbvie Inc | inibidores de quinase pirrol[2,3-b]piridina cdk9 |
| CA2903538A1 (en) | 2013-03-14 | 2014-10-02 | Abbvie Inc. | Pyrrolopyrimindine cdk9 kinase inhibitors |
| UY35419A (es) | 2013-03-14 | 2014-10-31 | Abbvie Inc | Inhibidores de cdk9 quinasa de pirrolo (2,3- b) piridina |
| GB2513403A (en) * | 2013-04-26 | 2014-10-29 | Agency Science Tech & Res | WNT pathway modulators |
| HUE041877T2 (hu) | 2013-10-17 | 2019-06-28 | Vertex Pharma | (S)-N-Metil-8-(1-((2'-metil-[4,5'-bipirimidin]-6-il)amino)propán-2-il)kinolin-4-karboxamid kokristályai és deuterált származékai DNS-PK inhibitorokként |
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| CA2945128A1 (en) * | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Mertk-specific pyrimidine compounds |
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| IL204594A0 (en) | 2010-11-30 |
| CN101889004B (zh) | 2014-09-10 |
| CA2702008A1 (en) | 2009-04-16 |
| US8716296B2 (en) | 2014-05-06 |
| WO2009047359A1 (en) | 2009-04-16 |
| EP2212297B1 (en) | 2011-05-25 |
| EP2212297A1 (en) | 2010-08-04 |
| DK2212297T3 (da) | 2011-09-05 |
| ATE510827T1 (de) | 2011-06-15 |
| HK1203950A1 (en) | 2015-11-06 |
| HK1150052A1 (en) | 2011-10-28 |
| MX2010003987A (es) | 2010-08-04 |
| CN104151293A (zh) | 2014-11-19 |
| IL204594A (en) | 2013-12-31 |
| JP5681855B2 (ja) | 2015-03-11 |
| SI2212297T1 (sl) | 2011-09-30 |
| ZA201001910B (en) | 2011-05-25 |
| US20150038516A1 (en) | 2015-02-05 |
| AU2008309517A1 (en) | 2009-04-16 |
| JP2011500539A (ja) | 2011-01-06 |
| US20100249149A1 (en) | 2010-09-30 |
| JP2015038077A (ja) | 2015-02-26 |
| HRP20110470T1 (hr) | 2011-07-31 |
| KR20100090772A (ko) | 2010-08-17 |
| AU2008309517B2 (en) | 2013-03-14 |
| EA201000554A1 (ru) | 2011-04-29 |
| BRPI0818543A2 (pt) | 2018-10-23 |
| CN101889004A (zh) | 2010-11-17 |
| NZ584454A (en) | 2011-09-30 |
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