JP2009534386A5 - - Google Patents
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- Publication number
- JP2009534386A5 JP2009534386A5 JP2009506558A JP2009506558A JP2009534386A5 JP 2009534386 A5 JP2009534386 A5 JP 2009534386A5 JP 2009506558 A JP2009506558 A JP 2009506558A JP 2009506558 A JP2009506558 A JP 2009506558A JP 2009534386 A5 JP2009534386 A5 JP 2009534386A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- substituted
- atoms
- unsubstituted
- hydrogen
- 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.)
- Granted
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- 229910052739 hydrogen Inorganic materials 0.000 claims description 65
- 239000001257 hydrogen Substances 0.000 claims description 65
- 125000000217 alkyl group Chemical group 0.000 claims description 57
- 125000004429 atom Chemical group 0.000 claims description 30
- 125000000623 heterocyclic group Chemical group 0.000 claims description 28
- 150000001875 compounds Chemical class 0.000 claims description 25
- 229910052736 halogen Inorganic materials 0.000 claims description 14
- 150000002367 halogens Chemical class 0.000 claims description 14
- 150000003839 salts Chemical class 0.000 claims description 9
- 229910052801 chlorine Inorganic materials 0.000 claims description 8
- 229910052731 fluorine Inorganic materials 0.000 claims description 8
- 125000001072 heteroaryl group Chemical group 0.000 claims description 8
- 125000003545 alkoxy group Chemical group 0.000 claims description 5
- 229910052740 iodine Inorganic materials 0.000 claims description 5
- 229910052760 oxygen Inorganic materials 0.000 claims description 3
- 150000002431 hydrogen Chemical class 0.000 claims 37
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 24
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 13
- 125000004430 oxygen atom Chemical group O* 0.000 claims 13
- 125000000026 trimethylsilyl group Chemical group [H]C([H])([H])[Si]([*])(C([H])([H])[H])C([H])([H])[H] 0.000 claims 9
- 125000004432 carbon atom Chemical group C* 0.000 claims 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 4
- -1 C 1 -C 6 alkyl Chemical group 0.000 claims 2
- 125000000882 C2-C6 alkenyl group Chemical group 0.000 claims 2
- 125000003601 C2-C6 alkynyl group Chemical group 0.000 claims 2
- 125000004093 cyano group Chemical group *C#N 0.000 claims 2
- 201000010099 disease Diseases 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 239000003814 drug Substances 0.000 claims 2
- 125000005842 heteroatom Chemical group 0.000 claims 2
- 230000003463 hyperproliferative effect Effects 0.000 claims 2
- 229910052757 nitrogen Inorganic materials 0.000 claims 2
- CCDCXGXEAROCCL-UHFFFAOYSA-N 5-[3-(2-fluoro-4-iodoanilino)pyridin-4-yl]-1,2-dihydro-1,2,4-triazol-3-one Chemical compound FC1=CC(I)=CC=C1NC1=CN=CC=C1C1=NNC(=O)N1 CCDCXGXEAROCCL-UHFFFAOYSA-N 0.000 claims 1
- HHTJBEIYFAHLCN-UHFFFAOYSA-N 5-[3-(2-fluoro-4-iodoanilino)pyridin-4-yl]-1,3,4-oxadiazol-2-amine Chemical compound O1C(N)=NN=C1C1=CC=NC=C1NC1=CC=C(I)C=C1F HHTJBEIYFAHLCN-UHFFFAOYSA-N 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 229940079593 drug Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- HRTVQWGJLGWJKO-UHFFFAOYSA-N n-(2-fluoro-4-iodophenyl)-4-(5-methylsulfanyl-1,3,4-oxadiazol-2-yl)pyridin-3-amine Chemical compound O1C(SC)=NN=C1C1=CC=NC=C1NC1=CC=C(I)C=C1F HRTVQWGJLGWJKO-UHFFFAOYSA-N 0.000 claims 1
- FMNPLTKMWIDHBF-UHFFFAOYSA-N n-(2-fluoro-4-iodophenyl)-4-(5-morpholin-4-yl-1,3,4-oxadiazol-2-yl)pyridin-3-amine Chemical compound FC1=CC(I)=CC=C1NC1=CN=CC=C1C1=NN=C(N2CCOCC2)O1 FMNPLTKMWIDHBF-UHFFFAOYSA-N 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 229910052717 sulfur Inorganic materials 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 description 4
- 125000004435 hydrogen atom Chemical class [H]* 0.000 description 4
- 125000000753 cycloalkyl group Chemical group 0.000 description 2
- LDQPCRDUEQLGLQ-UHFFFAOYSA-N Fc(cc(cc1)I)c1Nc1cnccc1-c([o]1)nnc1I Chemical compound Fc(cc(cc1)I)c1Nc1cnccc1-c([o]1)nnc1I LDQPCRDUEQLGLQ-UHFFFAOYSA-N 0.000 description 1
- ILNVUPQJTOLEJT-UHFFFAOYSA-O Fc(cc(cc1)I)c1Nc1cnccc1C([NH2+]1)=NN=C1I Chemical compound Fc(cc(cc1)I)c1Nc1cnccc1C([NH2+]1)=NN=C1I ILNVUPQJTOLEJT-UHFFFAOYSA-O 0.000 description 1
- 125000000592 heterocycloalkyl group Chemical group 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US79307306P | 2006-04-19 | 2006-04-19 | |
| US60/793,073 | 2006-04-19 | ||
| PCT/US2007/009456 WO2007123936A1 (en) | 2006-04-19 | 2007-04-18 | Novel heteroaryl-substituted arylaminopyridine derivatives as mek inhibitors |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2009534386A JP2009534386A (ja) | 2009-09-24 |
| JP2009534386A5 true JP2009534386A5 (cg-RX-API-DMAC10.html) | 2013-09-12 |
| JP5525812B2 JP5525812B2 (ja) | 2014-06-18 |
Family
ID=38357968
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2009506558A Expired - Fee Related JP5525812B2 (ja) | 2006-04-19 | 2007-04-18 | Ｍｅｋインヒビターとしての新規ヘテロアリール置換アリールアミノピリジン誘導体 |
Country Status (14)
Families Citing this family (37)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7772233B2 (en) * | 2006-04-19 | 2010-08-10 | Merck Serono, S.A. | Arylamino N-heteroaryl compounds as MEK inhibitors |
| ES2374480T3 (es) * | 2007-12-07 | 2012-02-17 | Novartis Ag | Derivados pirazol y uso de los mismos como inhibidores de quinasas dependientes de ciclina. |
| EP2370568B1 (en) | 2008-12-10 | 2017-07-19 | Dana-Farber Cancer Institute, Inc. | Mek mutations conferring resistance to mek inhibitors |
| RU2571930C2 (ru) | 2010-02-25 | 2015-12-27 | Дана-Фарбер Кэнсер Инститьют, Инк. | Мутации braf, обеспечивающие резистентность к ингибиторам braf |
| US20130059851A1 (en) | 2010-03-09 | 2013-03-07 | Dana-Farber Cancer Institute, Inc. | Methods of Diagnosing and Treating Cancer in Patients Having or Developing Resistance to a First Cancer Therapy |
| AR081626A1 (es) | 2010-04-23 | 2012-10-10 | Cytokinetics Inc | Compuestos amino-piridazinicos, composiciones farmaceuticas que los contienen y uso de los mismos para tratar trastornos musculares cardiacos y esqueleticos |
| AR081331A1 (es) | 2010-04-23 | 2012-08-08 | Cytokinetics Inc | Amino- pirimidinas composiciones de las mismas y metodos para el uso de los mismos |
| EP2560488B1 (en) | 2010-04-23 | 2015-10-28 | Cytokinetics, Inc. | Certain amino-pyridines and amino-triazines, compositions thereof, and methods for their use |
| US8759380B2 (en) | 2011-04-22 | 2014-06-24 | Cytokinetics, Inc. | Certain heterocycles, compositions thereof, and methods for their use |
| WO2013169858A1 (en) | 2012-05-08 | 2013-11-14 | The Broad Institute, Inc. | Diagnostic and treatment methods in patients having or at risk of developing resistance to cancer therapy |
| JP6299591B2 (ja) * | 2012-07-03 | 2018-03-28 | 小野薬品工業株式会社 | ソマトスタチン受容体作動活性を有する化合物およびその医薬用途 |
| BR112017019307A2 (pt) * | 2015-03-10 | 2018-05-02 | Aurigene Discovery Technologies Limited | compostos de 1,3,4-oxadiazol 3-substituído e tiadiazol como imunomoduladores |
| SI3300500T1 (sl) | 2015-05-20 | 2020-07-31 | Amgen Inc. | Triazolni agonisti receptorja APJ |
| WO2017033113A1 (en) | 2015-08-21 | 2017-03-02 | Acerta Pharma B.V. | Therapeutic combinations of a mek inhibitor and a btk inhibitor |
| US10150754B2 (en) | 2016-04-19 | 2018-12-11 | Celgene Quanticel Research, Inc. | Histone demethylase inhibitors |
| WO2017192485A1 (en) | 2016-05-03 | 2017-11-09 | Amgen Inc. | Heterocyclic triazole compounds as agonists of the apj receptor |
| US11020395B2 (en) | 2016-11-16 | 2021-06-01 | Amgen Inc. | Cycloalkyl substituted triazole compounds as agonists of the APJ receptor |
| EP3541802B1 (en) | 2016-11-16 | 2025-01-01 | Amgen Inc. | Alkyl substituted triazole compounds as agonists of the apj receptor |
| US10906890B2 (en) | 2016-11-16 | 2021-02-02 | Amgen Inc. | Triazole phenyl compounds as agonists of the APJ receptor |
| US11046680B1 (en) | 2016-11-16 | 2021-06-29 | Amgen Inc. | Heteroaryl-substituted triazoles as APJ receptor agonists |
| WO2018097944A1 (en) | 2016-11-16 | 2018-05-31 | Amgen Inc. | Triazole furan compounds as agonists of the apj receptor |
| EP3541803B1 (en) | 2016-11-16 | 2020-12-23 | Amgen Inc. | Triazole pyridyl compounds as agonists of the apj receptor |
| EP3618818A4 (en) | 2017-05-03 | 2020-12-09 | Vivace Therapeutics, Inc. | NON-CONDENSED TRICYCLIC COMPOUNDS |
| CN111542315B (zh) | 2017-08-21 | 2023-05-12 | 维瓦斯治疗公司 | 苯并磺酰基化合物 |
| WO2019089335A1 (en) | 2017-11-03 | 2019-05-09 | Amgen Inc. | Fused triazole agonists of the apj receptor |
| US11524943B1 (en) | 2017-12-06 | 2022-12-13 | Vivace Therapeutics, Inc. | Benzocarbonyl compounds |
| DK3720438T3 (da) * | 2017-12-07 | 2023-10-02 | Amplyx Pharmaceuticals Inc | Svampedræbende midler, der er afledt af heterocyklus-substitueret pyridin |
| CN110317190A (zh) * | 2018-03-28 | 2019-10-11 | 首都医科大学 | 一种三唑-羧酸酯类衍生物在医药领域的应用 |
| WO2019213006A1 (en) | 2018-05-01 | 2019-11-07 | Amgen Inc. | Substituted pyrimidinones as agonists of the apj receptor |
| EP3793551A4 (en) | 2018-05-16 | 2022-01-26 | Vivace Therapeutics, Inc. | OXADIAZOLE COMPOUNDS |
| CN114364798A (zh) | 2019-03-21 | 2022-04-15 | 欧恩科斯欧公司 | 用于治疗癌症的Dbait分子与激酶抑制剂的组合 |
| JP2023500906A (ja) | 2019-11-08 | 2023-01-11 | インサーム（インスティテュ ナシオナル ドゥ ラ サンテ エ ドゥ ラ ルシェルシェ メディカル） | キナーゼ阻害剤に対する獲得抵抗性を有するがんの処置方法 |
| US20230106583A1 (en) * | 2019-11-20 | 2023-04-06 | Vivace Therapeutics, Inc. | Heteroaryl compounds |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
| JP2024521788A (ja) | 2021-05-27 | 2024-06-04 | ミラティ セラピューティクス， インコーポレイテッド | 併用療法 |
| WO2025054260A1 (en) * | 2023-09-07 | 2025-03-13 | Kinnate Biopharma Inc. | Inhibitors of mek kinase |
| WO2025073765A1 (en) | 2023-10-03 | 2025-04-10 | Institut National de la Santé et de la Recherche Médicale | Methods of prognosis and treatment of patients suffering from melanoma |
Family Cites Families (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ES2249060T3 (es) | 1999-01-13 | 2006-03-16 | Warner-Lambert Company Llc | Diarilaminas sustituidas con 1-heterociclo. |
| GB2373245A (en) | 2001-03-12 | 2002-09-18 | Bayer Ag | Pyridinyl pyrazoles and their use for the treatment of COPD |
| AU2003260472A1 (en) * | 2002-09-10 | 2004-04-30 | Pharmacia Italia S.P.A. | Substituted pyridine derivatives as antitumor agent |
| WO2004052280A2 (en) * | 2002-12-10 | 2004-06-24 | Imclone Systems Incorporated | Anti-angiogenic compounds and their use in cancer treatment |
| US20050004186A1 (en) * | 2002-12-20 | 2005-01-06 | Pfizer Inc | MEK inhibiting compounds |
| EP1611123B8 (en) * | 2003-04-09 | 2013-11-13 | Exelixis, Inc. | Tie-2 modulators and methods of use |
| WO2005000818A1 (en) | 2003-06-27 | 2005-01-06 | Warner-Lambert Company Llc | 5-substituted-4-`(substituted phenyl)!amino!-2-pyridone deviatives for use as mek inhibitors |
| WO2005004818A2 (en) * | 2003-07-09 | 2005-01-20 | Imclone Systems Incorporated | Heterocyclic compounds and their use as anticancer agents |
| AU2004293018B2 (en) | 2003-11-19 | 2010-02-18 | Array Biopharma Inc. | Heterocyclic inhibitors of MEK and methods of use thereof |
| UA94571C2 (en) * | 2004-10-20 | 2011-05-25 | Мерк Сероно С.А. | 3-arylamino pyridine derivatives |
-
2007
- 2007-04-18 EP EP07755648A patent/EP2013180A1/en not_active Withdrawn
- 2007-04-18 JP JP2009506558A patent/JP5525812B2/ja not_active Expired - Fee Related
- 2007-04-18 ZA ZA200807263A patent/ZA200807263B/xx unknown
- 2007-04-18 CA CA002644425A patent/CA2644425A1/en not_active Abandoned
- 2007-04-18 CN CN201210488042.5A patent/CN103121996B/zh not_active Expired - Fee Related
- 2007-04-18 EA EA200802050A patent/EA200802050A1/ru unknown
- 2007-04-18 US US11/788,032 patent/US8076486B2/en not_active Expired - Fee Related
- 2007-04-18 KR KR1020087028187A patent/KR20090005195A/ko not_active Withdrawn
- 2007-04-18 BR BRPI0711625-0A patent/BRPI0711625A2/pt not_active IP Right Cessation
- 2007-04-18 MX MX2008013308A patent/MX2008013308A/es not_active Application Discontinuation
- 2007-04-18 WO PCT/US2007/009456 patent/WO2007123936A1/en not_active Ceased
- 2007-04-18 AU AU2007240860A patent/AU2007240860A1/en not_active Abandoned
- 2007-04-18 CN CN200780014073.4A patent/CN101426766B/zh not_active Expired - Fee Related
- 2007-04-19 AR ARP070101677A patent/AR060807A1/es unknown
-
2008
- 2008-10-06 IL IL194546A patent/IL194546A0/en unknown