ES2659725T3 - Inhibidores de EGFR y procedimiento de tratamiento de trastornos - Google Patents

Inhibidores de EGFR y procedimiento de tratamiento de trastornos Download PDF

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Publication number
ES2659725T3
ES2659725T3 ES10772385.0T ES10772385T ES2659725T3 ES 2659725 T3 ES2659725 T3 ES 2659725T3 ES 10772385 T ES10772385 T ES 10772385T ES 2659725 T3 ES2659725 T3 ES 2659725T3
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treatment procedure
egfr inhibitors
disorder treatment
nmr
mhz
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Inventor
Wenjun Zhou
Nathanael S. Gray
Pasi Janne
Michael J. Eck
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Dana Farber Cancer Institute Inc
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Dana Farber Cancer Institute Inc
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    • C07D473/02—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6
    • C07D473/16—Heterocyclic compounds containing purine ring systems with oxygen, sulphur, or nitrogen atoms directly attached in positions 2 and 6 two nitrogen atoms
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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
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
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    • C07D403/14—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 three or more hetero rings

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Abstract

Un compuesto que tiene la siguiente estructura: **(Ver fórmula)** en la que X >= O e Y >= H, X >= O e Y >= OMe, o X >= S e Y >= H.

Description

imagen1
imagen2
imagen3
imagen4
imagen5
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imagen7
imagen8
imagen9
imagen10
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imagen12
imagen13
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imagen23
imagen24
imagen25
imagen26
imagen27
imagen28
imagen29
imagen30
En ciertas realizaciones, la invención proporciona los compuestos 2-1 (WZ 3146), 2-2 (WZ 4002) y 2-15 (WZ 8040), seleccionados de la tabla 2. En este documento se describen los compuestos enumerados en la tabla 1, tabla 2, tabla 3, tabla 4, tabla 5 y tabla 6.
Tabla 1
Número del compuesto
Estructura Datos físicos 1H RMN 600 MHz y/o MS (m/z)
1-1
MS m/z : 449.52 (M + 1).
1-2
MS m/z : 471.96 (M + 1).
1-3
MS m/z: 471.96 (M + 1).
1-4
imagen31 MS m/z : 473.54 (M + 1).
32
1-5
MS m/z: 463.55 (M + 1).
1-6
MS m/z : 463.55 (M + 1).
1-7
imagen32 MS m/z: 449.52 (M + 1).
1-8
imagen33 MS m/z: 439.53 (M + 1).
1-9
MS m/z: 472.98 (M + 1).
33
1-10
MS m/z : 462.56 (M + 1).
1-11
MS m/z : 490.57 (M + 1).
1-12
MS m/z: 313.37 (M + 1).
1-13
MS m/z: 471.53 (M + 1).
1-14
MS m/z : 463.59 (M + 1).
1-15
MS m/z : 463.59 (M + 1).
34
1-16
MS m/z: 501.57 (M + 1).
1-17
imagen34 MS m/z : 501.57 (M + 1).
1-18
imagen35 MS m/z : 524 (M + 1).
Tabla 2
Número del compuesto
Estructura Datos físicos 1H RMN 600 MHz y/o MS (m/z)
2-1
MS m/z: 465.95 (M + 1).
35
2-2
MS m/z : 495.97 (M + 1).
2-3
imagen36 MS m/z : 495.97 (M + 1).
2-4
imagen37 MS m/z: 431.5 (M + 1).
2-5
MS m/z: 430.52 (M + 1).
2-6
MS m/z : 444.54 (M + 1).
36
2-7
MS m/z: 430.52 (M + 1).
2-8
MS m/z: 444.54 (M + 1).
2-9
MS m/z : 479.97 (M + 1).
2-10
MS m/z : 432.49 (M + 1).
2-11
MS m/z: 431.50 (M + 1).
37
2-12
MS m/z : 510.39 (M + 1).
2-13
imagen38 MS m/z : 530.05 (M + 1)
2-14
imagen39 MS m/z : 466.93 (M + 1).
2-15
MS m/z : 482.01 (M + 1).
2-16
MS m/z : 499.50 (M + 1).
38
2-17
MS m/z : 523.04 (M + 1).
2-18
imagen40 MS m/z : 579.10 (M + 1).
2-19
MS m/z : 494.98(M + 1).
2-20
imagen41 MS m/z: 511.05 (M + 1).
39
2-21
imagen42 MS m/z: 512.04 (M + 1).
2-22
imagen43 MS m/z : 496.96 (M + 1).
2-23
MS m/z: 493.96 (M + 1).
2-24
imagen44 MS m/z : 523.98 (M + 1).
2-25
MS m/z : 507.98 (M + 1).
40
2-26
MS m/z : 538.01 (M + 1).
2-27
imagen45 MS m/z : 466.94 (M + 1).
2-28
imagen46 MS m/z : 505.97 (M + 1).
2-29
MS m/z : 500.39 (M + 1).
41
2-30
MS m/z : 490.99 (M + 1).
Tabla 3
Número del compuesto
Estructura Datos físicos 1H RMN 600 MHz y/o MS (m/z)
3-1
imagen47 MS m/z : 407.42 (M + 1).
3-2
imagen48 MS m/z: 357.36 (M + 1).
3-3
MS m/z : 386.40 (M + 1).
42
3-4
MS m/z : 357.36 (M + 1).
3-5
imagen49 MS m/z : 407.42 (M + 1).
Tabla 4
4-1
MS m/z : 449.96 (M + 1).
4-2
imagen50 MS m/z: 494.99 (M + 1).
4-3
imagen51 MS m/z : 538.01 (M + 1).
43
Tabla 5
Número del compuesto
Estructura Datos físicos 1H RMN 600 MHz y/o MS (m/z)
5-1
imagen52 MS m/z : 482.93 (M + 1).
5-2
imagen53 MS m/z: 540.02 (M + 1).
5-3
imagen54 MS m/z: 509.01 (M + 1).
5-4
imagen55 MS m/z: 510.0 (M + 1).
44
5-5
MS m/z : 538.01 (M + 1).
5-6
MS m/z : 524.02 (M + 1).
5-7
MS m/z : 533.94 (M + 1).
5-8
imagen56 MS m/z : 499.56 (M + 1).
45
5-9
imagen57 MS m/z: 513.60 (M + 1).
5-10
MS m/z: 499.58 (M + 1)
5-11
imagen58 MS m/z: 513.60 (M + 1).
5-12
MS m/z : 494.98 (M + 1).
46
5-13
MS m/z : 512.97 (M + 1).
5-14
MS m/z : 512.97 (M + 1).
5-15
MS m/z: 513.96 (M + 1).
5-16
MS m/z: 513.96 (M + 1).
47
5-17
MS m/z : 494.99 (M + 1).
5-18
MS m/z: 494.00 (M + 1).
5-19
MS m/z: 508.03 (M + 1).
5-20
MS m/z : 527.99 (M + 1).
Tabla 6
48
6-1
MS m/z : 527.00 (M + 1).
6-2
MS m/z : 527.00 (M + 1).
6-3
MS m/z : 524.0 (M + 1).
6-4
MS m/z : 547.9(M + 1).
49
6-5
MS m/z: 543.0 (M + 1).
6-6
MS m/z: 553.4 (M + 1)
6-7
MS m/z : 511.9 (M + 1).
6-8
MS m/z : 554.0 (M + 1).
50
6-9
MS m/z : 507.98 (M + 1).
6-10
imagen59 MS m/z: 514.6 (M + 1).
6-11
MS m/z : 504.6 (M + 1).
6-12
imagen60 MS m/z: 494.9 (M + 1).
51
6-13
MS m/z : 508.02 (M + 1).
6-14
imagen61 MS m/z: 527.9 (M + 1).
6-15
MS m/z: 484.5 (M + 1).
6-16
MS m/z: 510.0 (M + 1).
52
6-17
MS m/z : 523.9 (M + 1).
6-18
imagen62 MS m/z: 595.1 (M + 1).
6-19
imagen63 MS m/z : 526.9(M + 1).
6-20
MS m/z : 564.1 (M + 1).
53
6-21
MS m/z: 510.9 (M + 1).
6-22
MS m/z : 497.9 (M + 1).
6-23
imagen64 MS m/z : 537.1 (M + 1).
6-24
imagen65 MS m/z: 592.1 (M + 1)
54
6-25
imagen66 MS m/z: 586.2 (M + 1).
6-26
MS m/z: 500.5 (M + 1).
6-27
MS m/z: 501.5 (M + 1).
6-28
MS m/z: 517.6 (M + 1).
55
6-29
imagen67 MS m/z: 531.6 (M + 1).
6-30
MS m/z : 532.6 (M + 1).
6-31
imagen68 MS m/z: 548.6 (M + 1).
6-32
MS m/z: 531.6 (M + 1).
56
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Claims (1)

  1. imagen1
ES10772385.0T 2009-05-05 2010-05-05 Inhibidores de EGFR y procedimiento de tratamiento de trastornos Active ES2659725T3 (es)

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US21541909P 2009-05-05 2009-05-05
US215419P 2009-05-05
PCT/US2010/001341 WO2010129053A2 (en) 2009-05-05 2010-05-05 Egfr inhibitors and methods of treating disorders

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EP (1) EP2440559B1 (es)
JP (1) JP5918693B2 (es)
KR (1) KR101705158B1 (es)
CN (1) CN102482277B (es)
CA (1) CA2760794C (es)
ES (1) ES2659725T3 (es)
IL (1) IL216140B (es)
WO (1) WO2010129053A2 (es)

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