MX2008013528A - Metodo para inhibir la cinasa del c-kit. - Google Patents
Metodo para inhibir la cinasa del c-kit.Info
- Publication number
- MX2008013528A MX2008013528A MX2008013528A MX2008013528A MX2008013528A MX 2008013528 A MX2008013528 A MX 2008013528A MX 2008013528 A MX2008013528 A MX 2008013528A MX 2008013528 A MX2008013528 A MX 2008013528A MX 2008013528 A MX2008013528 A MX 2008013528A
- Authority
- MX
- Mexico
- Prior art keywords
- phenyl
- absent
- cyano
- carboxylic acid
- mmol
- Prior art date
Links
- 238000000034 method Methods 0.000 title claims abstract description 91
- 230000002401 inhibitory effect Effects 0.000 title claims abstract description 12
- 102000016971 Proto-Oncogene Proteins c-kit Human genes 0.000 title description 14
- 108010014608 Proto-Oncogene Proteins c-kit Proteins 0.000 title description 14
- 150000001875 compounds Chemical class 0.000 claims abstract description 329
- 150000003839 salts Chemical class 0.000 claims abstract description 79
- 239000012453 solvate Substances 0.000 claims abstract description 35
- 108091000080 Phosphotransferase Proteins 0.000 claims abstract description 22
- 102000020233 phosphotransferase Human genes 0.000 claims abstract description 22
- 230000000694 effects Effects 0.000 claims abstract description 19
- 230000002062 proliferating effect Effects 0.000 claims abstract description 16
- -1 -CONH2 Chemical group 0.000 claims description 223
- 239000001257 hydrogen Substances 0.000 claims description 74
- 229910052739 hydrogen Inorganic materials 0.000 claims description 74
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims description 51
- 125000000217 alkyl group Chemical group 0.000 claims description 49
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 47
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims description 46
- 125000003277 amino group Chemical group 0.000 claims description 44
- 229910052757 nitrogen Inorganic materials 0.000 claims description 41
- 125000003118 aryl group Chemical group 0.000 claims description 39
- 125000003545 alkoxy group Chemical group 0.000 claims description 33
- 229920006395 saturated elastomer Polymers 0.000 claims description 32
- 229910052760 oxygen Inorganic materials 0.000 claims description 31
- 239000003814 drug Substances 0.000 claims description 30
- 125000002768 hydroxyalkyl group Chemical group 0.000 claims description 29
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims description 28
- 238000011282 treatment Methods 0.000 claims description 28
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims description 25
- 125000002541 furyl group Chemical group 0.000 claims description 25
- 150000002431 hydrogen Chemical class 0.000 claims description 25
- 125000003282 alkyl amino group Chemical group 0.000 claims description 24
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- 125000000753 cycloalkyl group Chemical group 0.000 claims description 23
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- 125000004076 pyridyl group Chemical group 0.000 claims description 22
- 238000006467 substitution reaction Methods 0.000 claims description 22
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- 239000011737 fluorine Substances 0.000 claims description 18
- 229910052731 fluorine Inorganic materials 0.000 claims description 18
- 125000005942 tetrahydropyridyl group Chemical group 0.000 claims description 18
- ZAMOUSCENKQFHK-UHFFFAOYSA-N Chlorine atom Chemical compound [Cl] ZAMOUSCENKQFHK-UHFFFAOYSA-N 0.000 claims description 17
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- 125000000842 isoxazolyl group Chemical group 0.000 claims description 17
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 17
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- 125000000168 pyrrolyl group Chemical group 0.000 claims description 17
- 125000004122 cyclic group Chemical group 0.000 claims description 16
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- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 claims description 8
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- 125000002757 morpholinyl group Chemical group 0.000 claims description 5
- 125000001376 1,2,4-triazolyl group Chemical group N1N=C(N=C1)* 0.000 claims description 4
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Landscapes
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| CN104370880A (zh) * | 2013-01-24 | 2015-02-25 | 韩冰 | 一类蛋白酶抑制剂及其制备方法和用途 |
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| CA2972952C (en) | 2015-01-15 | 2021-01-05 | Idorsia Pharmaceuticals Ltd | Hydroxyalkyl-piperazine derivatives as cxcr3 receptor modulators |
| AR103399A1 (es) | 2015-01-15 | 2017-05-10 | Actelion Pharmaceuticals Ltd | Derivados de (r)-2-metil-piperazina como moduladores del receptor cxcr3 |
| CN105753770A (zh) * | 2015-05-27 | 2016-07-13 | 上海佐林生物医药有限公司 | 蛋白激酶抑制剂制备方法、中间体、制备方法及应用 |
| 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 |
| US20220401436A1 (en) | 2019-11-08 | 2022-12-22 | INSERM (Institute National de la Santé et de la Recherche Médicale) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
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| DE69332948T2 (de) | 1992-03-05 | 2003-11-27 | Board Of Regents, The University Of Texas System | Verwendung von Immunokonjugate zur Diagnose und/oder Therapie der vaskularisierten Tumoren |
| WO2000064946A2 (en) | 1999-04-28 | 2000-11-02 | Board Of Regents, The University Of Texas System | Compositions and methods for cancer treatment by selectively inhibiting vegf |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
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| ATE465731T1 (de) * | 2003-10-23 | 2010-05-15 | Ab Science | 2-aminoaryloxazol-verbindungen als tyrosinkinase- hemmer |
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| JP2009511628A (ja) * | 2005-10-18 | 2009-03-19 | ジヤンセン・フアーマシユーチカ・ナームローゼ・フエンノートシヤツプ | Ｆｌｔ３キナーゼの阻害方法 |
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