PE20090992A1 - Derivados de fenil-amino-pirimidina como agentes inhibidores de cinasa - Google Patents
Derivados de fenil-amino-pirimidina como agentes inhibidores de cinasaInfo
- Publication number
- PE20090992A1 PE20090992A1 PE2008001428A PE2008001428A PE20090992A1 PE 20090992 A1 PE20090992 A1 PE 20090992A1 PE 2008001428 A PE2008001428 A PE 2008001428A PE 2008001428 A PE2008001428 A PE 2008001428A PE 20090992 A1 PE20090992 A1 PE 20090992A1
- Authority
- PE
- Peru
- Prior art keywords
- phenyl
- amino
- disorder
- metoxy
- pyrimidin
- Prior art date
Links
- DMEGQEWPMXDRMO-UHFFFAOYSA-N 4-phenylpyrimidin-2-amine Chemical class NC1=NC=CC(C=2C=CC=CC=2)=N1 DMEGQEWPMXDRMO-UHFFFAOYSA-N 0.000 title abstract 2
- 108091000080 Phosphotransferase Proteins 0.000 title 1
- 230000002401 inhibitory effect Effects 0.000 title 1
- 102000020233 phosphotransferase Human genes 0.000 title 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 6
- 150000001875 compounds Chemical class 0.000 abstract 3
- -1 DIETHYL-AMINO Chemical class 0.000 abstract 2
- 201000010099 disease Diseases 0.000 abstract 2
- 101000692455 Homo sapiens Platelet-derived growth factor receptor beta Proteins 0.000 abstract 1
- 206010020751 Hypersensitivity Diseases 0.000 abstract 1
- 102100026547 Platelet-derived growth factor receptor beta Human genes 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 208000026935 allergic disease Diseases 0.000 abstract 1
- 230000007815 allergy Effects 0.000 abstract 1
- 230000001363 autoimmune Effects 0.000 abstract 1
- 230000003176 fibrotic effect Effects 0.000 abstract 1
- 210000003630 histaminocyte Anatomy 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 210000000936 intestine Anatomy 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 208000011580 syndromic disease Diseases 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
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- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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- Tropical Medicine & Parasitology (AREA)
Abstract
REFERIDA A COMPUESTOS DERIVADOS DE FENIL-AMINO-PIRIMIDINA DE FORMULA I, DONDE R1 ES HALOALQUILO CON 1 A 6 ATOMOS DE FLUOR; R2 ES ALQUILO(C1-C6), ALQUENILO(C2-C6), ALQUINILO(C2-C6), ENTRE OTROS; R3 ES -L-NR4R5, -X-NR-(O)R8 O -X-NR-C(O)NR4R5; L ES -X-C(O), -X-OC(O), -(CR2)j, ENTRE OTROS; X ES (CR2)j O [C(R)-(CR2OR)]; R4 Y R5 SON CADA UNO H, ALQUILO(C1-C6), ALQUENILO(C2-C6), ALQUINILO(C2-C6), ENTRE OTROS; R ES H, ALQUILO(C1-C6); j Y m SON CADA UNO DE 0 A 4. SON COMPUESTOS SELECCIONADOS: N-(4-(2-(DIETIL-AMINO)-ETOXI)-FENIL)-5-(4-(TRIFLUORO-METOXI)-FENIL)-PIRIMIDIN-2-AMINA, N-(4-(2-(DIETIL-AMINO)-ETOXI)-FENIL)-5-(4-(DIFLUORO-METOXI)-FENIL)-PIRIMIDIN-2-AMINA, ACIDO 1-(2-(4-(5-(4-(DIFLUORO-METOXI)-FENIL)-PIRIMIDIN-2-IL-AMINO)-FENOXI)-ETIL)-PIPERIDIN-4-CARBOXILICO, ENTRE OTROS. SE REFIERE TAMBIEN A SU PROCEDIMIENTO DE PREPARACION Y COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN. DICHOS COMPUESTOS SON INHIBIDORES DE C-KIT Y PDGFR SIENDO UTILES PARA EL TRATAMIENTO DE UNA ENFERMEDAD ASOCIADA CON LOS MASTOCITOS, UN TRASTORNO DE ALERGIA, SINDROME DE INTESTINO IRRITABLE (IBS), UNA ENFERMEDAD FIBROTICA, UN TRASTORNO NEOPLASICO, UN TRASTORNO INFLAMATORIO, UN TRASTORNO AUTOINMUNE, ENTRE OTROS
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| CN104458675A (zh) * | 2013-09-12 | 2015-03-25 | 中国药科大学 | 一种筛选干细胞因子受体激酶抑制剂高通量筛选方法 |
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| BRPI0815715A2 (pt) | 2017-06-13 |
| CA2697081A1 (en) | 2009-02-26 |
| ZA201001513B (en) | 2010-10-27 |
| CN101784530A (zh) | 2010-07-21 |
| AU2008289037A1 (en) | 2009-02-26 |
| WO2009026276A1 (en) | 2009-02-26 |
| AR068014A1 (es) | 2009-10-28 |
| AU2008289037B2 (en) | 2012-03-01 |
| KR20100043288A (ko) | 2010-04-28 |
| MA31704B1 (fr) | 2010-09-01 |
| RU2010110640A (ru) | 2011-09-27 |
| CL2008002478A1 (es) | 2009-05-15 |
| EP2190825B1 (en) | 2014-04-09 |
| KR101218926B1 (ko) | 2013-01-04 |
| EP2190825A1 (en) | 2010-06-02 |
| ES2477878T3 (es) | 2014-07-18 |
| KR20120107538A (ko) | 2012-10-02 |
| PL2190825T3 (pl) | 2014-09-30 |
| MX2010002004A (es) | 2010-03-11 |
| TW200914023A (en) | 2009-04-01 |
| US20110301175A1 (en) | 2011-12-08 |
| CR11264A (es) | 2010-04-19 |
| US8293757B2 (en) | 2012-10-23 |
| ECSP10010044A (es) | 2010-04-30 |
| RU2455288C2 (ru) | 2012-07-10 |
| BRPI0815715A8 (pt) | 2017-07-04 |
| JP2014177486A (ja) | 2014-09-25 |
| CO6260074A2 (es) | 2011-03-22 |
| PT2190825E (pt) | 2014-07-16 |
| TN2010000087A1 (en) | 2011-09-26 |
| CA2697081C (en) | 2013-04-23 |
| JP2010536867A (ja) | 2010-12-02 |
| JP5599312B2 (ja) | 2014-10-01 |
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