CA2702008A1 - Inhibitors of protein kinases - Google Patents
Inhibitors of protein kinases Download PDFInfo
- Publication number
- CA2702008A1 CA2702008A1 CA2702008A CA2702008A CA2702008A1 CA 2702008 A1 CA2702008 A1 CA 2702008A1 CA 2702008 A CA2702008 A CA 2702008A CA 2702008 A CA2702008 A CA 2702008A CA 2702008 A1 CA2702008 A1 CA 2702008A1
- Authority
- CA
- Canada
- Prior art keywords
- 4alkyl
- 6alkyl
- compound
- alkyl
- methoxy
- 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.)
- Abandoned
Links
- 239000003112 inhibitor Substances 0.000 title abstract description 39
- 102000001253 Protein Kinase Human genes 0.000 title description 4
- 108060006633 protein kinase Proteins 0.000 title description 4
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- 208000002193 Pain Diseases 0.000 claims abstract description 93
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- 108090000266 Cyclin-dependent kinases Proteins 0.000 claims abstract description 51
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims abstract description 43
- 108091007914 CDKs Proteins 0.000 claims abstract description 41
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- 208000015122 neurodegenerative disease Diseases 0.000 claims abstract description 20
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- 238000006243 chemical reaction Methods 0.000 claims description 54
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- C07D401/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
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- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
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- C07D—HETEROCYCLIC COMPOUNDS
- 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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- C—CHEMISTRY; METALLURGY
- 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
- C07D409/02—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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D471/04—Ortho-condensed systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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| 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 |
| EP2562265A1 (en) | 2011-08-22 | 2013-02-27 | Lead Discovery Center GmbH | Susceptibility to selective CDK9 inhibitors |
| 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 |
| US9328112B2 (en) | 2014-02-06 | 2016-05-03 | Abbvie Inc. | Tetracyclic CDK9 kinase inhibitors |
| CA2945128A1 (en) * | 2014-04-11 | 2015-10-15 | The University Of North Carolina At Chapel Hill | Mertk-specific pyrimidine compounds |
| US9346815B2 (en) | 2014-05-23 | 2016-05-24 | Genentech, Inc. | 5-chloro-2-difluoromethoxyphenyl pyrazolopyrimidine compounds, compositions and methods of use thereof |
| EP3206749B1 (en) | 2014-10-14 | 2021-09-08 | The Regents of the University of California | The cdk9 and brd4 inhibitors flavopiridol and jq1 to inhibit cartilage inflammation |
| US10308648B2 (en) * | 2014-10-16 | 2019-06-04 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| US9845331B2 (en) | 2015-06-29 | 2017-12-19 | Astrazeneca Ab | Chemical compounds |
| CR20180323A (es) | 2015-11-20 | 2018-08-06 | Idorsia Pharmaceuticals Ltd | Derivados de indol n-sustituídos como moduladores de los receptores de pge2 |
| US10709708B2 (en) | 2016-03-17 | 2020-07-14 | The University Of North Carolina At Chapel Hill | Method of treating cancer with a combination of MER tyrosine kinase inhibitor and an epidermal growth factor receptor (EGFR) inhibitor |
| AU2017245641A1 (en) * | 2016-04-07 | 2018-09-13 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridyl derivatives as bromodomain inhibitors |
| US11110108B2 (en) | 2016-09-27 | 2021-09-07 | Vertex Pharmaceuticals Incorporated | Method for treating cancer using a combination of DNA-damaging agents and DNA-PK inhibitors |
| BR112019005526A2 (pt) | 2016-10-20 | 2019-06-18 | Pfizer | agentes antiproliferativos para tratamento de pah |
| ES2896476T3 (es) | 2017-05-18 | 2022-02-24 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina |
| AR111808A1 (es) | 2017-05-18 | 2019-08-21 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina como moduladores del receptor de pge2 |
| US11325899B2 (en) | 2017-05-18 | 2022-05-10 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as PGE2 receptor modulators |
| HRP20211533T1 (hr) | 2017-05-18 | 2022-01-07 | Idorsia Pharmaceuticals Ltd | Derivati fenila kao modulatori receptora pge2 |
| BR112019024322A2 (pt) | 2017-05-22 | 2020-06-16 | F. Hoffmann-La Roche Ag | Compostos e composições terapêuticos e métodos de uso dos mesmos |
| JP6934261B2 (ja) * | 2017-05-24 | 2021-09-15 | アビスコ セラピューティクス カンパニー リミテッド | Ｎ−（アザアリール）シクロラクタム−１−カルボキサミド誘導体、その製造方法および応用 |
| CA3159628A1 (en) * | 2019-11-05 | 2021-05-14 | Dermira, Inc. | Mrgprx2 antagonists and uses thereof |
| CA3161351A1 (en) | 2019-12-09 | 2021-06-17 | Zhenyu Wang | Compound as cyclin-dependent kinase 9 inhibitor and use thereof |
| RU2754441C2 (ru) * | 2019-12-30 | 2021-09-02 | Закрытое Акционерное Общество "Биокад" | Новые ингибиторы cdk8/19 |
| CN115448874B (zh) * | 2021-06-09 | 2024-11-01 | 石药集团中奇制药技术（石家庄）有限公司 | 固体形式的周期蛋白依赖性激酶9抑制剂及其用途 |
| CN115703760B (zh) * | 2021-08-11 | 2024-05-31 | 山东大学 | 2,4-二取代嘧啶类细胞周期蛋白依赖性激酶酶抑制剂及其制备方法和应用 |
| CN115703738B (zh) * | 2021-08-16 | 2024-06-21 | 中国科学院上海药物研究所 | 含2-芳杂环取代的脲类化合物、其制备方法和用途 |
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| RU2277911C2 (ru) | 2000-02-25 | 2006-06-20 | Ф.Хоффманн-Ля Рош Аг | Модуляторы аденозиновых рецепторов |
| DE10114138C2 (de) | 2001-03-16 | 2003-03-27 | Schering Ag | Cdk-inhibitorische Indirubinderivate mit erhöhter Löslichkeit |
| DE10117204A1 (de) | 2001-04-06 | 2002-10-10 | Boehringer Ingelheim Pharma | In 6-Stellung substituierte Indolinone, ihre Herstellung und ihre Verwendung als Arzneimittel |
| WO2002094825A1 (en) | 2001-05-22 | 2002-11-28 | Banyu Pharmaceutical Co., Ltd. | Novel spiropiperidine derivative |
| DE10129028A1 (de) | 2001-06-11 | 2003-01-02 | Schering Ag | Lösliche Cdk-inhibitorische Indirubinderivate |
| US20040106647A1 (en) | 2002-06-28 | 2004-06-03 | Schneider Michael D. | Modulators of Cdk9 as a therapeutic target in cardiac hypertrophy |
| CN101468965A (zh) | 2003-03-24 | 2009-07-01 | 默克公司 | 联芳基取代的6元杂环钠通道阻滞剂 |
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| JP2007500179A (ja) | 2003-07-30 | 2007-01-11 | サイクラセル・リミテッド | キナーゼ阻害剤としての２−アミノフェニル−４−フェニルピリミジン |
| AU2004261482A1 (en) | 2003-07-30 | 2005-02-10 | Cyclacel Limited | Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors |
| EP1678147B1 (en) | 2003-09-15 | 2012-08-08 | Lead Discovery Center GmbH | Pharmaceutically active 4,6-disubstituted aminopyrimidine derivatives as modulators of protein kinases |
| JPWO2005040135A1 (ja) | 2003-10-24 | 2007-03-08 | 小野薬品工業株式会社 | 抗ストレス薬およびその医薬用途 |
| JP4879165B2 (ja) | 2004-04-20 | 2012-02-22 | トランス テック ファーマ，インコーポレイテッド | メラノコルチン受容体の調節因子としての置換チアゾール及びピリミジン誘導体 |
| GB0411791D0 (en) * | 2004-05-26 | 2004-06-30 | Cyclacel Ltd | Compounds |
| FR2878247B1 (fr) | 2004-11-19 | 2008-10-03 | Galderma Res & Dev | Nouveaux composes modulateurs des recepteurs de type ppary et leur utilisation dans des compositions cosmetiques ou pharmaceutiques |
| EP1901747A2 (en) | 2005-05-25 | 2008-03-26 | Ingenium Pharmaceuticals AG | Pyrimidine-based cdk inhibitors for treating pain |
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| IL204594A0 (en) | 2010-11-30 |
| CN101889004B (zh) | 2014-09-10 |
| 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 |
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| 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 |
| EA020439B1 (ru) | 2014-11-28 |
| EA201000554A1 (ru) | 2011-04-29 |
| BRPI0818543A2 (pt) | 2018-10-23 |
| CN101889004A (zh) | 2010-11-17 |
| NZ584454A (en) | 2011-09-30 |
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