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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- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
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- A61K31/454—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
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- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
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- A61K31/5375—1,4-Oxazines, e.g. morpholine
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Landscapes
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Applications Claiming Priority (2)
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| US79347106P | 2006-04-20 | 2006-04-20 | |
| PCT/US2007/066985 WO2007124369A2 (en) | 2006-04-20 | 2007-04-19 | Method of inhibiting c kit kinase |
Publications (1)
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| MX2008013528A true MX2008013528A (es) | 2008-10-29 |
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| SG (1) | SG171592A1 (enExample) |
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| CA2840029C (en) | 2011-07-27 | 2021-07-20 | Ab Science | Oxazole and thiazole derivatives as selective protein kinase inhibitors (c-kit) |
| 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 |
| US10259807B2 (en) | 2013-07-22 | 2019-04-16 | Idorsia Pharmaceuticals Ltd. | 1-(piperazin-1-yl)-2-([1,2,4]triazol-1-yl)-ethanone derivatives |
| EA032927B1 (ru) | 2015-01-15 | 2019-08-30 | Идорсия Фармасьютиклз Лтд | Производные гидроксиалкилпиперазина в качестве модуляторов cxcr3 рецептора |
| 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 |
| US20220143049A1 (en) | 2019-03-21 | 2022-05-12 | Onxeo | A dbait molecule in combination with kinase inhibitor for the treatment of cancer |
| EP4054579A1 (en) | 2019-11-08 | 2022-09-14 | Institut National de la Santé et de la Recherche Médicale (INSERM) | Methods for the treatment of cancers that have acquired resistance to kinase inhibitors |
| WO2021148581A1 (en) | 2020-01-22 | 2021-07-29 | Onxeo | Novel dbait molecule and its use |
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| ES2193143T3 (es) | 1992-03-05 | 2003-11-01 | Univ Texas | Uso de inmunoconjugados para la diagnosis y/o terapia de tumores vascularizaos. |
| US6342219B1 (en) | 1999-04-28 | 2002-01-29 | Board Of Regents, The University Of Texas System | Antibody compositions for selectively inhibiting VEGF |
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| ITMI992711A1 (it) * | 1999-12-27 | 2001-06-27 | Novartis Ag | Composti organici |
| CN100491374C (zh) * | 2002-08-02 | 2009-05-27 | Ab科学公司 | 2-(3-氨基芳基)氨基-4-芳基-噻唑及其作为c-kit抑制剂的应用 |
| WO2005040139A2 (en) * | 2003-10-23 | 2005-05-06 | Ab Science | 2-aminoaryloxazole compounds as tyrosine kinase inhibitors |
| GB0326601D0 (en) * | 2003-11-14 | 2003-12-17 | Novartis Ag | Organic compounds |
| BRPI0507271A (pt) * | 2004-01-30 | 2007-06-26 | Ab Science | 2-(3-substituìda-aril)amino-4-aril-tiazóis como inibidores de tirosina cinase |
| EP1807077B1 (en) * | 2004-10-22 | 2016-11-23 | Janssen Pharmaceutica NV | Inhibitors of c-fms kinase |
| US20060281788A1 (en) * | 2005-06-10 | 2006-12-14 | Baumann Christian A | Synergistic modulation of flt3 kinase using a flt3 inhibitor and a farnesyl transferase inhibitor |
| 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 |
| CN101466686A (zh) * | 2006-04-20 | 2009-06-24 | 詹森药业有限公司 | C-fms激酶抑制剂 |
| NZ572073A (en) * | 2006-04-20 | 2011-09-30 | Janssen Pharmaceutica Nv | Heterocyclic compounds as inhibitors of c-fms kinase |
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