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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- 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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- 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
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- 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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- 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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| US60/998,821 | 2007-10-12 | ||
| PCT/EP2008/063715 WO2009047359A1 (en) | 2007-10-12 | 2008-10-13 | Inhibitors of protein kinases |
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| CA2702008A1 true CA2702008A1 (en) | 2009-04-16 |
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| CA2702008A Abandoned CA2702008A1 (en) | 2007-10-12 | 2008-10-13 | Inhibitors of protein kinases |
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| UA110324C2 (en) * | 2009-07-02 | 2015-12-25 | Genentech Inc | Jak inhibitory compounds based on pyrazolo pyrimidine |
| WO2011022348A1 (en) | 2009-08-18 | 2011-02-24 | Janssen Pharmaceutica Nv | Ethylene diamine modulators of fatty acid amide hydrolase |
| US9155724B2 (en) | 2010-02-05 | 2015-10-13 | Whitehead Institute For Biomedical Research | Combination methods for treatment of disease |
| NZ601924A (en) * | 2010-03-10 | 2014-10-31 | Astrazeneca Ab | 4-phenyl pyridine analogues as protein kinase inhibitors |
| 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 |
| MX358682B (es) * | 2010-07-13 | 2018-08-31 | Hoffmann La Roche | Derivados de pirazolo [1,5a]pirimidina y de tieno[3,2b] pirimidina como moduladores de la cinasa asociada al receptor de la interleucina 4 (irak4). |
| US20130303507A1 (en) * | 2011-01-28 | 2013-11-14 | Novartis Ag | Substituted hetero-biaryl compounds and their uses |
| 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 |
| AU2012318896B2 (en) | 2011-10-03 | 2017-03-02 | The University Of North Carolina At Chapel Hill | Pyrrolopyrimidine compounds for the treatment of cancer |
| US9498471B2 (en) | 2011-10-20 | 2016-11-22 | 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 |
| LT2841428T (lt) | 2012-04-24 | 2018-12-10 | Vertex Pharmaceuticals Incorporated | Dnr-pk inhibitoriai |
| EP2852579A4 (en) | 2012-05-22 | 2015-12-30 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| US9562047B2 (en) | 2012-10-17 | 2017-02-07 | The University Of North Carolina At Chapel Hill | Pyrazolopyrimidine compounds for the treatment of cancer |
| EP2925752A4 (en) | 2012-11-27 | 2016-06-01 | Univ North Carolina | PYRIMIDINE COMPOUNDS FOR CANCER TREATMENT |
| CN105246883B (zh) | 2013-03-12 | 2017-07-21 | 沃泰克斯药物股份有限公司 | Dna‑pk抑制剂 |
| EP2970200A1 (en) | 2013-03-13 | 2016-01-20 | Abbvie Inc. | Pyridine cdk9 kinase inhibitors |
| MX2015012386A (es) | 2013-03-13 | 2016-02-03 | Abbvie Inc | Inhibidores de la cinasa cdk9. |
| EP2970264A1 (en) | 2013-03-14 | 2016-01-20 | AbbVie Inc. | Pyrrolo[2,3-b]pyridine cdk9 kinase inhibitors |
| WO2014139328A1 (en) | 2013-03-14 | 2014-09-18 | Abbvie Inc. | Pyrrolo[2,3-b]pyridine cdk9 kinase inhibitors |
| BR112015023078A2 (pt) | 2013-03-14 | 2017-07-18 | Abbvie Inc | inibidores de pirrolopirimindina cdk9 quinase |
| GB2513403A (en) * | 2013-04-26 | 2014-10-29 | Agency Science Tech & Res | WNT pathway modulators |
| KR102411227B1 (ko) | 2013-10-17 | 2022-06-21 | 버텍스 파마슈티칼스 인코포레이티드 | Dna-pk 억제제로서 (s)-n-메틸-8-(1-((2'-메틸-[4,5'-비피리미딘]-6-일)아미노)프로판-2-일)퀴놀린-4-카복스아미드 및 이의 듀테로화된 유도체의 공결정 |
| WO2015119712A1 (en) | 2014-02-06 | 2015-08-13 | Abbvie Inc. | Tetracyclic cdk9 kinase inhibitors |
| US9555031B2 (en) | 2014-04-11 | 2017-01-31 | The University Of North Carolina At Chapel Hill | Therapeutic uses of selected pyrrolopyrimidine compounds with anti-mer tyrosine kinase activity |
| HRP20210935T1 (hr) | 2014-05-23 | 2021-08-06 | F. Hoffmann - La Roche Ag | Spojevi 5-kloro-2-difluorometoksifenil pirazolopirimidina koji predstavljaju inhibitore jak |
| JP6930913B2 (ja) | 2014-10-14 | 2021-09-01 | ザ リージェンツ オブ ザ ユニバーシティ オブ カリフォルニアＴｈｅ Ｒｅｇｅｎｔｓ Ｏｆ Ｔｈｅ Ｕｎｉｖｅｒｓｉｔｙ Ｏｆ Ｃａｌｉｆｏｒｎｉａ | 炎症を阻害するためのｃｄｋ９及びｂｒｄ４阻害剤の使用法 |
| US10308648B2 (en) * | 2014-10-16 | 2019-06-04 | Syros Pharmaceuticals, Inc. | Inhibitors of cyclin-dependent kinase 7 (CDK7) |
| LT3313838T (lt) | 2015-06-29 | 2019-06-10 | Astrazeneca Ab | Policikliniai amido dariniai, kaip cdk9 slopikliai |
| 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 |
| CA3018358A1 (en) * | 2016-04-07 | 2017-10-12 | Glaxosmithkline Intellectual Property (No.2) Limited | Pyridyl derivatives as bromodomain inhibitors |
| TW201815418A (zh) | 2016-09-27 | 2018-05-01 | Vertex Pharma | 使用dna破壞劑及dna-pk抑制劑之組合治療癌症的方法 |
| CA3040815C (en) | 2016-10-20 | 2021-07-20 | Steven Martin Evans | Anti-proliferative agents for treating pah |
| KR102626982B1 (ko) | 2017-05-18 | 2024-01-18 | 이도르시아 파마슈티컬스 리미티드 | Pge2 수용체 조절제로서의 피리미딘 유도체 |
| WO2018210994A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Phenyl derivatives as pge2 receptor modulators |
| ES2896476T3 (es) | 2017-05-18 | 2022-02-24 | Idorsia Pharmaceuticals Ltd | Derivados de pirimidina |
| CA3063632A1 (en) | 2017-05-18 | 2018-11-22 | Idorsia Pharmaceuticals Ltd | Benzofurane and benzothiophene derivatives as pge2 receptor modulators |
| CA3061236A1 (en) | 2017-05-22 | 2018-11-29 | F. Hoffmann-La Roche Ag | Therapeutic compounds and compositions, and methods of use thereof |
| CA3063596C (en) * | 2017-05-24 | 2022-08-30 | Abbisko Therapeutics Co., Ltd. | N-(azaaryl)cyclolactam-1-carboxamide derivative, preparation method therefor, and use thereof |
| EP4054570A1 (en) * | 2019-11-05 | 2022-09-14 | Dermira, Inc | Mrgprx2 antagonists and uses thereof |
| EP4074699A4 (en) | 2019-12-09 | 2024-01-03 | CSPC Zhongqi Pharmaceutical Technology (Shijiazhuang) Co., Ltd. | COMPOUND USEFUL 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 |
| CN117396474A (zh) * | 2021-03-17 | 2024-01-12 | 武田药品工业株式会社 | 血浆激肽释放酶抑制剂 |
| 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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| ES2240449T3 (es) | 2000-02-25 | 2005-10-16 | F. Hoffmann-La Roche Ag | Moduladores receptores de adenosina. |
| 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 |
| GB0315966D0 (en) | 2003-07-08 | 2003-08-13 | Cyclacel Ltd | Compounds |
| EP1648887A1 (en) | 2003-07-30 | 2006-04-26 | Cyclacel Limited | Pyridinylamino-pyrimidine derivatives as protein kinase inhibitors |
| EP1648875A1 (en) | 2003-07-30 | 2006-04-26 | Cyclacel Limited | 2-aminophenyl-4-phenylpyrimidines as kinase inhibitors |
| US8084457B2 (en) | 2003-09-15 | 2011-12-27 | 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 |
| NZ550114A (en) | 2004-04-20 | 2011-02-25 | Transtech Pharma Inc | Substituted thiazole and pyrimidine derivatives as melanocortin receptor modulators |
| 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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2008
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- 2008-10-13 WO PCT/EP2008/063715 patent/WO2009047359A1/en not_active Ceased
- 2008-10-13 NZ NZ584454A patent/NZ584454A/en not_active IP Right Cessation
- 2008-10-13 AT AT08838451T patent/ATE510827T1/de not_active IP Right Cessation
- 2008-10-13 BR BRPI0818543A patent/BRPI0818543A2/pt not_active IP Right Cessation
- 2008-10-13 CN CN200880119493.3A patent/CN101889004B/zh not_active Expired - Fee Related
- 2008-10-13 JP JP2010528428A patent/JP5681855B2/ja not_active Expired - Fee Related
- 2008-10-13 AU AU2008309517A patent/AU2008309517B2/en not_active Ceased
- 2008-10-13 EP EP08838451A patent/EP2212297B1/en not_active Not-in-force
- 2008-10-13 EA EA201000554A patent/EA020439B1/ru not_active IP Right Cessation
- 2008-10-13 MX MX2010003987A patent/MX2010003987A/es active IP Right Grant
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- 2008-10-13 CA CA2702008A patent/CA2702008A1/en not_active Abandoned
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- 2014-09-03 JP JP2014178745A patent/JP2015038077A/ja active Pending
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|---|---|
| JP2015038077A (ja) | 2015-02-26 |
| JP2011500539A (ja) | 2011-01-06 |
| AU2008309517B2 (en) | 2013-03-14 |
| EP2212297B1 (en) | 2011-05-25 |
| US20100249149A1 (en) | 2010-09-30 |
| HK1150052A1 (en) | 2011-10-28 |
| NZ584454A (en) | 2011-09-30 |
| EA020439B1 (ru) | 2014-11-28 |
| BRPI0818543A2 (pt) | 2018-10-23 |
| SI2212297T1 (sl) | 2011-09-30 |
| CN101889004B (zh) | 2014-09-10 |
| JP5681855B2 (ja) | 2015-03-11 |
| CN104151293A (zh) | 2014-11-19 |
| KR20100090772A (ko) | 2010-08-17 |
| US20150038516A1 (en) | 2015-02-05 |
| ZA201001910B (en) | 2011-05-25 |
| DK2212297T3 (da) | 2011-09-05 |
| ATE510827T1 (de) | 2011-06-15 |
| IL204594A0 (en) | 2010-11-30 |
| MX2010003987A (es) | 2010-08-04 |
| HK1203950A1 (en) | 2015-11-06 |
| AU2008309517A1 (en) | 2009-04-16 |
| EA201000554A1 (ru) | 2011-04-29 |
| HRP20110470T1 (hr) | 2011-07-31 |
| WO2009047359A1 (en) | 2009-04-16 |
| US8716296B2 (en) | 2014-05-06 |
| EP2212297A1 (en) | 2010-08-04 |
| IL204594A (en) | 2013-12-31 |
| CN101889004A (zh) | 2010-11-17 |
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