ES2535155T3 - Moduladores de receptores de estrógeno y usos de los mismos - Google Patents

Moduladores de receptores de estrógeno y usos de los mismos Download PDF

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Publication number
ES2535155T3
ES2535155T3 ES14155086.3T ES14155086T ES2535155T3 ES 2535155 T3 ES2535155 T3 ES 2535155T3 ES 14155086 T ES14155086 T ES 14155086T ES 2535155 T3 ES2535155 T3 ES 2535155T3
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Spain
Prior art keywords
phenyl
acid
acrylic
indazol
phenylbut
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ES14155086.3T
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Inventor
Nicholas D. Smith
Mehmet Kahraman
Steven P. Govek
Johnny Y. Nagasawa
Andiliy G. Lai
Jackaline D. Julien
Mark R. Herbert
Celine Bonnefous
Karensa L. Douglas
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Seragon Pharmaceuticals Inc
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Seragon Pharmaceuticals Inc
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/54—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings condensed with carbocyclic rings or ring systems
    • C07D231/56—Benzopyrazoles; Hydrogenated benzopyrazoles
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • A61K31/416—1,2-Diazoles condensed with carbocyclic ring systems, e.g. indazole
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    • C07D265/12—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems
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    • C07D265/18—1,3-Oxazines; Hydrogenated 1,3-oxazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring with hetero atoms directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D277/00—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D277/62—Benzothiazoles
    • C07D277/68—Benzothiazoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
    • C07D279/10—1,4-Thiazines; Hydrogenated 1,4-thiazines
    • C07D279/14—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems
    • C07D279/16—1,4-Thiazines; Hydrogenated 1,4-thiazines condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—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 two hetero rings
    • C07D403/10—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 two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/10—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
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    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems

Abstract

Un compuesto que tiene la estructura de Fórmula (XII):**Fórmula** en donde, X 1 es CH, CR3 o N; X2 es N, CH, o CR3; Z es -OH o -OR10; R2 es C1-C4alquilo, C1-C4fluoroalquilo, C1-C4deuteroalquilo, C3-C6cicloalquilo, o -C1-C4alquileno-W; W es hidroxi, halógeno, CN, C1-C4alquilo, C1-C4haloalquilo, C1-C4alcoxi, C1-C4haloalcoxi, y C3-C6cicloalquilo; cada R3 es independientemente halógeno, C1-C4alquilo, o C1-C4fluoroalquilo; cada R4 es independientemente halógeno, -CN, -OR9, -S(>=O)2R10, C1-C4alquilo, C1-C4fluoroalquilo, o C1-C4heteroalquilo; cada R5 es independientemente halógeno, -CN, -OR9, -S(>=O)2R10, C1-C4alquilo, C1-C4fluoroalquilo, o C1-C4heteroalquilo; R6 es H, C1-C4alquilo, o halógeno; R7 es H, C1-C4alquilo, o halógeno; R9 es H, C1-C6alquilo, C1-C6fluoroalquilo, o C3-C6cicloalquilo; R10 es C1-C6alquilo; m es 0, 1, o 2; n es 0, 1, 2, 3, o 4; y p es 0, 1, o 2; o una sal farmacéuticamente aceptable, o N-óxido del mismo.

Description

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E14155086
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El compuesto de Fórmula (II) puede tener la estructura de Fórmula (III) o (IV):
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El compuesto de Fórmula (I) puede tener la estructura de Fórmula (V):
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El compuesto de Fórmula (I) puede tener la estructura de Fórmula (XI):
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En algunos ejemplos, Y es –C(=O)–Z, tetrazolilo, piperidinilo sustituido opcionalmente, pirrolidinilo sustituido opcionalmente, –NR8R8’ , –AR–OH, –SO3H, y –P(=O)(OH)2 en donde AR es fenilo o heteroarilo monocíclico; Z es –OH, –OR10 , –NR8R8’ , – 10 NR8S(=O)2R10, o –NHOH; R8 y R8’ es independientemente H, C1–C6alquilo, C2–C6alquenilo, o C2–C6alquinilo.
En algunos ejemplos, R8 y R8’ es independientemente H, C1–C6alquilo sustituido o no sustituido, C2–C6alquenilo sustituido o no sustituido, C2–C6alquilo sustituido o no sustituido, C1–C6fluoroalquilo sustituido o no sustituido, C1–C6heteroalquilo sustituido o no sustituido, C3–C6cicloalquilo sustituido o no sustituido, fenilo sustituido o no sustituido, heteroarilo monocíclico sustituido o no sustituido, o bencilo sustituido o no sustituido,. En algunos ejemplos, R8 y R8’ son independientemente H, C1– 15 C6alquilo, C2–C6alquenilo, C2–C6alquinilo, C1–C6–fluoroalquilo, C1–C6heteroalquilo, C3–C6cicloalquilo, fenilo sustituido o no sustituido, heteroarilo monocíclico sustituido o no sustituido, o bencilo sustituido o no sustituido,. En algunos ejemplos, R8 es H, C1–C6alquilo, C1–C6–fluoroalquilo, C1–C6heteroalquilo, C3–C6cicloalquilo, fenol sustituido o no sustituido, heteroarilo monocíclico sustituido o no sustituido, o bencilo sustituido o no sustituido,. En algunos ejemplos , R8 es H, C1–C6alquilo, o
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E14155086
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
1
3–(4–((E)–1–(1H–indazol–5–il)–2–fenilbut–1– en–1–il)fenil)acrilato de (E)–Etilo imagen30 423
2
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)acrílico 395
3
Ácido (E)–3–(4–((E)–1–(1H– Benzo[d][1,2,3]triazol–5–il)–2–fenilbut–1–en– 1–il)fenil) acrílico imagen31 396
4
Ácido (E)–3–(4–((E)–2–(4–Fluorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico imagen32 413
5 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–6–il)–2– fenilbut–1–en–1–il)fenil)acrílico imagen33 395
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
6
Ácido (E)–3–(4–((E)–2–(4–Clorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico imagen34 429
7
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–metoxifenil)but–1–en–1–il)fenil)acrílico 425
8
Ácido (E)–3–(4–((E)–2–(3– (Hidroximetil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 425
9
Ácido (E)–3–(4–((E)–2–(4– (Hidroximetil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico imagen35 425
10
Ácido (E)–3–(4–((E)–2–(2– (Hidroximetil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 425
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
11
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (o–toluil)but–1–en–1–il)fenil)acrílico imagen36 409
12
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (m–toluil)but–1–en–1–il)fenil)acrílico imagen37 409
13
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (p–toluil)but–1–en–1–il)fenil)acrílico 409
14
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metoxifenil)but–1–en–1–il)fenil)acrílico imagen38 425
15
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–metoxifenil)but–1–en–1–il)fenil)acrílico 425
16-04-2015
(continuación) E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
16
Ácido ((E)–3–(4–((E)–2–(2–Clorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico imagen39 429
17
Ácido (E)–3–(4–((E)–2–(3–Clorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 429
18 *
Ácido (E)–3–(4–((E)–1–(1H–Indozol–4–il)–2– fenilbut–1–en–1–il)fenil)acrílico 395
19
Ácido (E)–3–(4–((E)–2–(2–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 413
20
Ácido (E)–3–(4((E)–2–(3–Fluorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 413
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
21 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–4–il)–2– (o–toluil)but–1–en–1–il)fenil)acrílico imagen40 409
22 *
Ácido (E)–3–(4–((E)–2–(2–Clorofenil)–1–(1H– indazol–4–il)but–1–en–1–il)fenil)acrílico 429
23 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (tiofen–2–il)but–1–en–1–il)fenil)acrílico 401
24 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (tiofen–3–il)but–1–en–1–il)fenil)acrílico 401
25 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (piridin–2–il)but–1–en–1–il)fenil)acrílico imagen41 396
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
26
Ácido (E)–3–(4–((E)–2–(2–Etilfenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico imagen42 423
27
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–(trifluorometil)fenil)but–1–en–1– il)fenil)acrílico 463
28 *
Ácido (E)–3–(4–((E)–2–([1,1’–Bifenil]–2–il)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 471
29
Ácido (E)–3–(4–((E)–4–Cloro–1–(1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 429
30 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1H–indazol–4–il)but–1–en–1– il)fenil)acrílico 447
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
31 *
Ácido (E)–3–(4–((E)–2–(2–Fluorofenil)–1–(1H– indazol–4–il)but–1–en–1–il)fenil)acrílico imagen43 413
32
Ácido (E)–3–(4((E)–2–(2–Cianofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico imagen44 420
33
Ácido (E)–3–(4–{(E)–2–(2,4–Difluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen45 431
34
Ácido (E)–3–(4–((E)–2–(2–Cloro–3– Fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen46 447
35
Ácido (E)–3–(4–((E)–2–Ciclopropilo–1–(1H– indazol–5–il)–2–fenilvinil)fenil)acrílico 407
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
36
Ácido (E)–3–(4–((E)–2–(4–Fluoro–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen47 427
37
Ácido (E)–3–(4–((E)–2–(2,6–Difluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen48 431
38
Ácido (E)–3–(4–((E)–2–(2,6–Diclorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 463
39
Ácido (E)–3–(4–((E)–4,4,4–Trideutero–1–(1H– indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 398
40
Ácido (E)–3–(4–((E)–2–(4–Fluoro–3– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen49 427
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
41
Ácido (E)–3–(4–((E)–2–(5–Fluoro–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen50 427
42
Ácido (E)–3–(4–((E)–2–(2,3–Difluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 431
43
Ácido (E)–3–(4–((E)–2–(2,5–Difluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 431
44
Ácido (E)–3–(4–((E)–2–(2–Cloro–5– fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 447
45
Ácido (E)–3–(4–((E)–2–(2–Cloro–6– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen51 443
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
46
Ácido (E)–3–(4–((E)–1–(7–Cloro–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen52 429
47
Ácido (E)–3–(4–((E)–1–(4–Metil–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 409
48
Ácido (E)–3–(4–((E)–1–(7–Metil–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 409
49
Ácido (E)–3–(4–((E)–1–(6–Metil–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 409
50 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (naftalen–1–il)but–1–en–1–il)fenil)acrílico 445
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
51
Ácido (E)–3–(4–((E)–1–(3–Metil–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen53 409
52
Ácido (E)–3–(4–((E)–1–(3–Cloro–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 429
53
Ácido (E)–3–(4–((E)–2–(4–(Cloro–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen54 443
54
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilprop–1–en–1–il)fenil)acrílico 381
55
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilpent–1–en–1–il)fenil)acrílico imagen55 409
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
56 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1H– pirazolo[3,4–b]piridin–4–il}but–1–en–1– il)fenil)acrílico imagen56 396
57
Ácido (E)–3–(4–((E)–2–(3–Cianofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 420
58
Ácido (E)–3–(4–((E)–2–(4–Cianofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 420
59
Ácido (E)–3–(4–((E)–4–Hidroxi–1–(1H– indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 411
60
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–4– metoxi–2–fenilbut–1–en–1–il)fenil)acrílico imagen57 425
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
61
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–3– metoxi–2–fenilprop–1–en–1–il)fenil)acrílico imagen58 411
62 *
Ácido (E)–3–(4–((E)–2–(4– (Dimetilamino)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 438
63
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen59 413
64
Ácido (E)–3–(4–((E)–1–(1H–)Indol–5–il)–2– fenilbut–1–en–1–il)fenil)acrílico imagen60 394
65
Ácido (E)–3–(4–((E)–1–(6–Cloro–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 429
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
66 *
Ácido (E)–3–(4((E)–1–(2–Oxo–2,3– dihidrobenzo[d]oxazol–6–il)–2–fenilbut–1–en– 1–il)fenil)acrílico imagen61 412
67 *
Ácido (E)–3–(4–((E)–2.Fenil–1–(1H– pirazolo[3,4–b]piridin–5–il)but–1–en–1– il)fenil)acrílico 396
68 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1H– pirrolo[2,3–b]piridin–5–il)but–1–en–1– il)fenil)acrílico 395
69
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–4– metil–2–fenilpent–1–en–1–il)fenil)acrílico 423
70 *
Ácido (E)–3–(4–((E)–2–Ciclopropilo–1–(1H– indazol–4–il)–2–fenilvinil)fenil)acrílico 407
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
71 *
Ácido (E)–3–(4–((E)–2–(2–Clorofenil)–2– ciclopropilo–1–(1H–indazol–4– il)vinil)fenil)acrílico imagen62 441
72
Ácido (E)–3–(4–((E)–1–(1H– Benzo[d][1,2,3]triazol–5–il)–2–(2–cloro–4– Fluorofenil)but–1–en–1–il)fenil)acrílico imagen63 448
73 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclopropilo–1–(1H–indazol–4– il)vinil)fenil)acrílico 459
74
Ácido (E)–3–(4–((E)–1–(4–Cloro–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen64 429
75 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–2,3– dihidrobenzo[d]tiazol–6–il)–2–fenilbut–1–en– 1–il)fenil)acrílico imagen65 428
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
76
Ácido (E)–3–(4–((E)–2–Ciclopentilo–1–(1H– indazol–5–il)–2–fenilvinil)fenil)acrílico imagen66 435
77
Ácido (E)–3–(4–((E)–2–Ciclohexilo–1–(1H– indazol–5–il)–2–fenilvinil)fenil)acrílico imagen67 449
78
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–3– metil–2–fenilbut–1–en–1–il)fenil)acrílico 409
79
Ácido (E)–3–(4–((E)–3–Ciclopropilo–1–(1H– indazol–5–il)–2–fenilprop–1–en–1– il)fenil)acrílico y imagen68 421
80
Ácido (E)–3–(4–((E)–2–(2–Clorofenil)–2– ciclopropilo–1–(1H–indazol–5– il)vinil)fenil)acrílico 441
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
81 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1H–il)but–1– en–1–il)fenil)acrílico imagen69 396
82
Ácido (E)–3–(4–((E)–1–(6–fluoro–1H–indazol– 5–il)–2–fenilbut–1–en–1–il)fenil)acrílico 413
83 *
Ácido (E)–3–(4–((E)–1–(1H– Benzo[d]imidazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen70 395
84
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilhex–1–en–1–il)fenil)acrílico imagen71 423
85
Ácido (E)–3–(4–((E)–3–Ciclopentilo–1–(1H– indazol–5–il)–2–fenilprop–1–en–1– il)fenil)acrílico imagen72 449
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
86 *
Ácido (E)–3–(4–((E)–1–(6–Fluoro–1H– indazol–4–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen73 413
87
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(4–fluoro–1H–indazol–5–il)but– en–1–il)fenil)acrílico imagen74 465
88 *
Ácido (E)–3–(4–((E)–1–(1H– Benzo[d][1,2,3]triazol–4–il)–2–fenilbut–1–en– 1–il)fenil)acrílico imagen75 396
89 *
Ácido (E)–3–(4–((E)–1–(1H– Benzo[d][1,2.3]triazol–4–il)–2–(2–cloro–4– Fluorofenil)but–1–en–1–il)fenil)acrílico 448
90 *
Ácido (E)–3–(4–((E)–1–(3–Oxo–2,3– dihidroisoquinolin–6–il)–2–fenilbut–1–en–1– il)fenil)acrílico 422
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
91
Ácido (E)–3–(4–((E)–1–(7–Fluoro–1H– indazol–5–il)–2–fenilbut–1–en–1– il)penil)acrílico imagen76 413
92
Ácido (E)–3–4–((E)–1–(7–Fluoro–1H–indol–5– il)–2–fenilbut–1–en–1–il)fenil)acrílico 412
93
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1H–indazol–5–il)–4–metilpent– 1–en–1–il)fenil)acrílico 475
94
Ácido (E)–3–(4–((Z)–3,3–Difluoro–1–(1H– indazol–5–il)–2–fenilprop–1–en–1– il)fenil)acrílico 417
95
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(7–fluoro–1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico imagen77 465
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
96 *
Ácido (E)–3–(4–((E)–2–(Benzofuran–4–il)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen78 435
97 *
Ácido (E)–3–(4–((E)–1–(1–Oxo–1,2– dihidroquinolin–6–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen79 422
98
Ácido (E)–3–(4–((E)–4–Fluoro–1–(1H– indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen80 413
99
Ácido (E)–3–(4–((E)–4–Cloro–2–(2–cloro–4– Fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen81 481
100 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–1,2,3,4– tetrahidroquinolin–6–il)–2–fenilbut–1–en–1– il)fenilo]acrílico imagen82 424
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
101 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–2,4–dihidro– 1H–benzo[d][1,3]oxazin–6–il)–2–fenilbut–1– en–1–il)fenil)acrílico imagen83 426
102 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–1,2– dihidroquinolin–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 422
103 *
Ácido (E)–3–(4–((E)–1–(3–Oxo.3,4–dihidro– 2H–benzo[b][1,4]tiazin–7–il)–2–fenilbut–1–en– 1–il)fenil)acrílico 442
104 *
Ácido (E)–3–(4–((E)–1–(3–Oxoisoindolin–5– il)–2–fenilbut–1–en–1–il)fenil)acrílico 410
105 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–1,2– dihidroquinolin–6–il)–2–fenilbut–1–en–1– il)fenil)acrílico 422
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
106
Ácido (E)–3–(4–((Z)–3,3,3–Trifluoro–1–(1H– indazol–5–il)–2–fenilprop–1–en–1– il)fenil)acrílico imagen84 no observado
107 *
Ácido (E)–3–(4–((E)–1–(3–Oxo–3,4–dihidro– 2H–benzo[b][1,4]oxazin–7–il)–2–fenilbut–1– en–1–il)fenil)acrílico no observado
108
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(4–floro–2–metilfenil)but–1– en–1–il)fenil)acrílico 445
109
Ácido (E)–3–(4–((E)–2–(4–Cloro–2– metilfenil)–1–(4–fluoro–1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 461
110 *
Ácido (E)–3–(4–((E)–1–(1–Oxoisoindolin–5– il)–2–fenilbut–1–en–1–il)fenil)acrílico 410
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
111
Ácido (E)–3–(4–((E)–2–Ciclopropilo–1–(4– fluoro–1H–indazol–5–il)–2–(4–fluoro–2– metilfenil)vinil)fenil)acrílico imagen85 457
112
Ácido (E)–3–(4–((E)–2–(4–Cloro–2– metilfenil)–2–ciclopropilo–1–(4–fluoro–1H– indazol–5–il)vinil)fenil)acrílico 473
113
Ácido (E)–3–(4–((E)–1–(4–Cloro–1H–indazol– 5–il)–2–(2–cloro–4–Fluorofenil)but–1–en–1– il)fenil)acrílico 481
114
Ácido (E)–3–(4–((Z)–2–(2–Cloro–4– Fluorofenil)–3,3–difluoro–1–(1H–indazol–5– il)prop–1–en–1–il)fenil)acrílico 469
115
Ácido (E)–3–(4–((E)–2–Ciclopropilo–1–(4– fluoro–1H–indazol–5–il)–2– fenilvinil)fenil)acrílico imagen86 425
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
116
Ácido (E)–3–(4–((E)–4–Cloro–1–(4–fluoro– 1H–indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen87 447
117
Ácido (E)–3–(4–((E)–4–Cloro–2–(2–cloro–4– Fluorofenil)–1–(4–fluoro–1H–indazol–5– il)but–1–en–1–il)fenil)acrílico 499
118 *
Ácido (E)–3–(4–((E)–2–(4–Fluorofenil)–1– (quinolin–6–il)but–1–en–1–il)fenil)acrílico imagen88 406
119
Ácido (E)–3–(4–((E)–4–Fluoro–2–(4– Fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen89 431
120 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1H– pirazolo[4,3–b]piridin–5–il)but–1–en–1– il)fenil)acrílico 396
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
121
Ácido (E)–3–(4–((E)–4–Fluoro–1–(4–fluoro– 1H–indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen90 431
122 *
Ácido (E)–3–(4–((E)–1–(2–Oxo–2,3–dihidro– 1H–benzo[d]imidazol–5–il)–2–fenilbut–1–en– 1–il)fenil)acrílico 411
123 *
Ácido (E)–3–(4–((E)–1–(Naftalen–2–il)–2– fenilbut–1–en–1–il)fenil)acrílico 404
124 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(quinoxalin– 6–il)but–1–en–1–il)fenil)acrílico 407
125 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(pirazolo[1,5– a]piridin–5–il)but–1–en–1–il)fenil)acrílico imagen91 395
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
126 *
Ácido (E)–3–(4–((E)–1–(Imidazo[1,2–a]piridin– 6–il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen92 395
127 *
Ácido (E)–3–(4–((E)–1–([1,2,4]–Triazolo[4,3– a]piridin–6–il)–2–fenilbut–1–en–1– il)fenil)acrílico 396
128 *
Ácido (E)–3–(4–((E)–1–(Benzo[d][1,3]dioxol– 5–il)–3–fenilbut–1–en–1–il)fenil)acrílico imagen93 397 (ES–)
129 *
Ácido (E)–3–(4–((E)–1–(Imidazo[1,2–a]piridin– 6–il)–2–(o–toluil)but–1–en–1–il)fenil)acrílico 409
130 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–6–il)– 2–fenilbut–1–en–1–il)fenil)acrílico 412
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
131 *
Ácido (E)–3–(4–((E)–1–([1,2,4]Triazolo[1,5– a]piridin–6–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen94 396
131 *
Ácido (E)–3–(4((E)–2–Fenil–1–(tetrazolo[1,5– a]piridin–6–il)but–1–en–1–il)fenil)acrílico imagen95 397
133 *
Ácido (E)–3–(4–((E)–1–(Imidazo[1,5–a]piridin– 6–il)–2–fenilbut–1–en–1–il)fenil)acrílico 395
134 *
Ácido (E)–3–(4–((E)–1–([1,2,4]Triazolo[4,3– a]piridin–7–il)–2–fenilbut–1–en–1– il)fenil)acrílico 396
135 *
Ácido (E)–3–(4–((E)–1–(Imidazo[1,5–a]piridin– 7–il)–2–fenilbut–1–en–1–il)fenil)acrílico 395
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
136 *
Ácido (E)–3–(4–((E)–1–([1,2,4]Triazolo[1,5– a]piridin–7–il)–2–fenilbut–1–en–1– il)fenil)acrílico imagen96 396
137 *
Ácido (E)–3–(4–((E)–1– (Benzo[c][1,2,5]oxadiazol–5–il)–2–fenilbut–1– en–1–il)fenil)acrílico 397
138 *
Ácido (E)–3–(4–((E)–1–([1,2,3]Triazolo[1,5– a]piridin–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 396
139
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–5– metoxi–2–fenilpent–1–en–1–il)fenil)acrílico 439
140
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–6– metoxi–2–fenitex–1–en–1–il)fenil)acrílico imagen97 453
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
141 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–fenilbut–1–en–1–il)fenil)acrílico imagen98 412
142 *
Ácido (E)–3–(4–((E)–1–(Benzo[b]tiofen–2–il)– 2–fenilbut–1–en–1–il)fenil)acrílico 409
143 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1–fenil–1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 471
144 *
Ácido (E)–3–(4–((E)–1– (Benzo[c][1,2,5]tiadiazol–5–il)–2–fenilbut–1– en–1–il)fenil)acrílico 413
145 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1–(piridin–3– il)–1H–indazul–5–il)but–1–en–1–il)fenil)acrílico 472
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
146 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]oxazol–5–il)– 2–fenilbut–1–en–1–il)fenil)acrílico imagen99 396
147 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–fenoxifenil)but–1–en–1–il)fenil)acrílico 487
148 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(pirazolo[1,5– a]piridin–3–il)but–1–il)fenil)acrílico imagen100 395
149 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(1H– pirazolo[4,3–d]pirimidin–5–il)but–1–en–1– il)fenil)acrílico 397
150 *
Ácido (E)–3–(4–((E)–2–(3– (Carboximetoxi)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico imagen101 345
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
151
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1H–indazol–5–il)–3–metilbut– 1–en–1–il)fenil)acrílico imagen102 461
152 *
Ácido (E)–3–(4–((E)–1–(6–Hidroxipiridin–3–il)– 2–fenilbut–1–en–1–il)fenil)acrílico imagen103 372
153
Ácido (E)–3–(4–((E)–1–(1H–Imdazol–5–il)–2– (3–(trifluorometoxi)fenil)but–1–en–1– il)fenil)acrílico 479
154 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–3– metil–2–(4–metiltiofen–3–il)but–1–en–1– il)fenil)acrílico 429
155
Ácido (E)–3–(4–((E)–2–Ciclobutil–1–(1H– indazol–5–il)–2–fenilvinil)fenil)acrílico imagen104 421
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
156 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]isotiazol–5– il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen105 412
157
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclobutilo–1–(1H–indazol–5– il)vinilfenil)acrílico 473
158
Ácido (E)–3–(4–((E)–1–(3–Fluoro–1H– indazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 413
159 *
Ácido (E)–3–(4–((E)–1–(2– Metilbenzo[d]biazol–5–il)–2–fenilbut–1–en–1– il)fenil)acrílico 426
160 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(4–(pirimidin–2–iloxi)fenil)but– 1–en–1–il)fenil)acrílico 507
16-04-2015 E14155086
Compuesto
Nombre Estructura LCMS [M+H]+
161 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(4–(pirazin–2–iloxi)fenil)but– 1–en–1–il)fenil)acrílico imagen106 507
162 *
Ácido (E)–3–(4–((E)–2–Ciclobutil–1–(1H– indazol–5–il)–2–(4–((5–(metilsulfonil)piridin– 2–il)oxi)fenil)vinil)fenil)acrílico 592
163 *
Ácido (E)–3–(4–((E)–1–(7– Metoxibenzofuran–3–il)–2–fenilbut–1–en–1– il)fenil)acrílico No observado
164 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(7–metoxibenzofuran–3– il)but–1–en–1–il)fenil)acrílico imagen107 477
165
Ácido (E)–3–(4–((E)–2–Ciclobutil–1–(3– fluoro–1H–indazol–5–il)–2– fenilvinil)fenil)acrílico 439
16-04-2015
Compuesto
Nombre Estructura LCMS [M+H]+
166
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(3–fluoro–1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico imagen108 465
167
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclobutilo–1–(3–fluoro–1H– indazol–5–il)vinil)fenil)acrílico 491
168 *
Ácido (E)–3–(4–((E)–1–(Isoquinolin–7–il)–2– fenilbut–1–en–1–il)fenil)acrílico imagen109 405
169 *
Ácido (E)–3–(4–((E)–1–(Benzofurin–2–il)–2– (2–cloro–4–Fluorofenil)but–1–en–1– il)fenil)acrílico imagen110 447
170 *
Ácido (E)–3–(4–((E)–1(Benzofuran–3–il)–2– (2–cloro–4–Fluorofenil)but–1–en–1– il)fenil)acrílico imagen111 447
Compuesto
Nombre Estructura LCMS [M+H]+
171
3–(4–((E)–2–(4–Fluorofenil)–1–(1H–indazol– 5–il)but–1–en–1–il)fenil)acrilato de (E)–Etilo imagen112 441
172 *
3–(4–((E)–1–(1H–indazol–6–il)–2–fenilbut–1– en–1–il)fenil)acrilato de (E)–Etilo 423
173
3–(4–((E)–1–(1H–Indazol–5–il)–2–(2– metoxifenil)but–1–en–1–il)fenil)acrilato de (E)–Etilo imagen113 453
174
3–(4–((E)–1–(1H–Indazol–5–il)–2–(4– metoxifenil)but–1–en–1–il)fenil)acrilato de (E)–Etilo 453
175 *
3–(4–((E)–1–(1H–Indalol–4–il)–2–fenilbut–1– en–1–il)fenil)acrilato de (E)–Etilo 423
Compuesto
Nombre Estructura LCMS [M+H]+
176
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)–2–metilacrílico imagen114 409
177
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en1–il)–3–metilfenil)acrílico imagen115 409
178
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–2–metilfenil)acrílico 409
179
Ácido (E)–3–(4–((Z)–1–(1H–indazol–5–il)–2– fenilbut–1–en–1–il)–2–clorofenil)acrílico 429
180 *
Ácido (E)–3–(6–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)naftalen–2–il)acrílico imagen116 445
Compuesto
Nombre Estructura LCMS [M+H]+
181
Ácido (Z)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–on–1–il)fenil)–2–fluoroacrílico imagen117 413
182
Ácido (Z)–3–(4–((E)–1–(1H–1–Indazol–5–il)– 2–fenilbut–1–en–1–il)fenil)–2–cloroacrílico 429
183
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–3–Fluorofenil)acrílico imagen118 413
184
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–2–flluorofenil)acrílico imagen119 413
185
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–2– (trifluorometil)fenil)acrílico 463
Compuesto
Nombre Estructura LCMS [M+H]+
186 *
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)tiofen–2–il)acrílico imagen120 401
187
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–3–metoxifenil)acrílico imagen121 425
188
Ácido (E)–3–(4–((Z)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)–2–metoxifenil)acrílico imagen122 425
189 *
Ácido (E)–3–(5–((Z)–1–(1H–Indazol–5–il])–2– fenilbut–1–en–1–il)piridin–2–il)acrílico imagen123 396
190
Ácido (E)–2–(4–(1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenoxi)acético 399
Compuesto
Nombre Estructura LCMS [M+H]+
191 *
(E)–5–(2–Fenil–1–(4–(2–(pirrolidin–1– il)etoxi)fenil)but–1–en–1–il)–1H–indazol imagen124 438
192 *
Ácido (E)–5–(1–(1H–Indazol–5–il)–2–fenilbut– 1–en–1–il)–2,3–dihidro–1H–indeno–2– carboxílico 409
193 *
3–(4–((E)–2–(2–cloro–4–Fluorofenil)–1–(1– (tetrahidro–2H–piran–2–il)–1H–indazol–5– il)but–1–en–1–il)fenil)acrilato de (E)–Etilo 475 [(M–THP+H)+H]+
194
Clorhidrato de 3–(4–((E)–2–(2–cloro–4– fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrilato de (E)–Etilo 475
195
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 447
Compuesto
Nombre Estructura LCMS [M+H]+
196
3–(4–((E)–2–(2,4–diclorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrilato de (E)–Etilo imagen125 49
197
Ácido (E)–3(4–(E)–2–(2,4–Diclorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen126 463
198
Ácido (E)–3(4((E)–2–(4–Cloro–2– (trifluorometil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 497
199
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclopropilo–1–(1H–indazol–5– il)vinil)fenil)acrílico imagen127 459
200
Ácido (E)–3–(4–((E)–2–(4–Fluoro–2– (trifluorometil)fenil)–1 –(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 481
Compuesto
Nombre Estructura LCMS [M+H]+
201
Ácido (E)–3–(4–(1–(4–Fluoro–1H–indazol–5– il)–2–(4–fluoro–2–(trifluometil) fenil)butil)fenil)acrílico imagen128 499
203
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)–1– (4–fluoro–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 481
203
Ácido (E)–3–(4–((E)–2–(4–Cloro–2– (trifluorometil)fenil)–1–(4–fluoro–1H–indazol– 5–il)but–1–en–1–il)fenil)acrílico 515
204 *
Ácido (E)–3–(4–((E)–2–(3–Cloropiridin–4–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 430
205
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–4–fluoro–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 465
Compuesto
Nombre Estructura LCMS [M+H]+
206
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– metoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen129 459
207 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(trifluorometil)piridin–3–il)but–1–en–1– il)fenil)acrílico 464
208 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (1–metil–1H–pirazol–5–il)but–1–en–1– il)fenil)acrílico imagen130 399
209
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)–4– fluoro–1–(4–fluoro–1H–indazol–5–il)but–1–en– 1–il)fenil)acrílico imagen131 499
210
Ácido (E)–3–(4–((E)–2–Ciclopropilo–2–(2,4– diclorofenil)–1–(4–fluoro–1H–indazol–5– il)vinil)fenil)acrílico 493
Compuesto
Nombre Estructura LCMS [M+H]+
211
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclopropilo–1–(4–fluoro–1H– indazol–5–il)vinil)fenil)acrílico imagen132 477
212 *
Ácido (E)–3–(4–((E)–2–(4–(Dimetilcarbamoil)– 2–Fluorofenil)–1–(1H–indazol–5–il)but–1–en– 1–il)fenil)acrílico 484
213 *
Ácido (E)–3–(4–((E)–2–(2–Fluoro–4– (metilcarbamoil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 470
214 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metiltiofen–3–il)but–1–en–1–il)fenil)acrílico imagen133 415
215
Ácido (E)–3–(4–((E)–2–Ciclopropilo–2–(2,4– diclorofenil)–1–(1H–indazol–5– il)vinil)fenil)acrílico 475
Compuesto
Nombre Estructura LCMS [M+H]+
216
Ácido (E)–3–(4–((E)–2–(4–Cloro–2– metilfenil)–3–ciclopropilo–1–(1H–indazol–5– il)vinil)fenil)acrílico imagen134 455
217 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metilpiridin–3–il)but–1–en–1–il)fenil)acrílico imagen135 410
218 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–metilpiridin–3–il)but–1–en–1–il)fenil)acrílico imagen136 410
219 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (pirazin–2–il)but–1–en–1–il)fenil)acrílico 397
220 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (pirimidin–5–il)but–1–en–1–il)fenil)acrílico imagen137 397
Compuesto
Nombre Estructura LCMS [M+H]+
221 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (1–metil–1H–1,2,3–triazol–5–il)but–1–en–1– il)fenil)acrílico imagen138 400
222 *
Ácido (E)–3–(4–((E)1–(1H–Indazol–5–il)–2– (2–(trifluorometil)piridin–3–il)but–1–en–1– il)fenil)acrílico imagen139 464
223 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–metiltiofen–3–il)but–1–en–1–il)fenil)acrílico 415
224 *
Ácido (E)–3–(4–((E)–1–(3–Cloropiridin–4–il)– 1–(4–fluoro–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 448
225 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (isotiazol–4–il)but–1–en–1–il)fenil)acrílico 402
Compuesto
Nombre Estructura LCMS [M+H]+
226 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–metilpiridin–4–il)but–1–en–1–il)fenil)acrílico imagen140 410
227 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (5–metiltiofen–2–il)but–1–en–1–il)fenil)acrílico 415
228
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metil–5–(metilsulfonil)fenil)but–1–en–1– il)fenil)acrílico imagen141 487
229 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metiltiazol–5–il)but–1–en–1–il)fenil)acrílico imagen142 416
230 *
Ácido (E)–3–(4–((E)–2–(3–Cloropiridin–4–il)– 4–fluoro–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 448
Compuesto
Nombre Estructura LCMS [M+H]+
231 *
Ácido (E)–3–(4–((E)–2–(3–Fluoropiridin–4–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen143 414
232 *
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)–1– (imidazo[1,2–a]piridin–6–il)but–1–en–1– il)fenil)acrílico 463
233 *
Ácido (E)–3–(4–((E)–2–(4–Fluoro–2– (trifluorometil)fenil)–1–(imidazo[1,2–a]piridin– 6–il)but–1–en–1–il)fenil)acrílico imagen144 481
234
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il(–2– (4–metoxi–2–metilfenil)but–1–en–1– il)fenil)acrílico imagen145 439
235
Ácido (E)–3–(4–((E)–2–(2–Fluoro–4– metoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 443
Compuesto
Nombre Estructura LCMS [M+H]+
236 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metoxipiridin–4–il)but–1–en–1– il)fenil)acrílico imagen146 426
237
Ácido (E)–3–(4–((E)–2–(2–Cloro–5– metoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen147 459
238
Ácido (E)–3–(4–((E)–2–(2–Fluoro–4– (metilsulfonil)fenil)–1–(1H–indazol–5–il)but–1– en–1–il)fenil)acrílico imagen148 491
239
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)– 3,3,4,4,4–pentadeutero–1–(1H–indazol–5– il)but–1–en–1–il)fenil)acrílico 468
240 *
Ácido (E)–3–(4–((E)–2–(Benzo[d][1,3]dioxol– 5–il)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 439
Compuesto
Nombre Estructura LCMS [M+H]+
241 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–metiltiofen–2–il)but–1–en–il)fenil)acrílico imagen149 415
242 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(4–metiltiofen–3–il)but–1–en– 1–il)fenil)acrílico 433
243
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(metilsulfonil)fenil)but–1–en–1– il)fenil)acrílico 473
244
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)–1– (7–fluoro–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen150 481
245 *
Ácido (E)–3–(4–((E)–2–(3–Cloropiridin–4–il)– 1–(7–fluoro–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen151 448
Compuesto
Nombre Estructura LCMS [M+H]+
246 *
Ácido (E)–3–(4–((E)–2–Fenil–1–(5H– pirolo[2,3–b]pirazin–2–il)but–1–en–1– il)fenil)acrílico imagen152 396
247 *
Ácido (E)–3–((E)–2–(Benzofuran–5–il)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 435
248
Ácido (E)–3–(4–((E)–2–(2–Cloro–3– metoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen153 459
249
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pirrolidin–1–il)fenil)but–1–en–1– il)fenil)acrílico 464
250 *
Ácido (E)–3–(4–((E)–2–(2,3– Dihidrobenzo[b][1,4]dioxin–6–il)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 453
Compuesto
Nombre Estructura LCMS [M+H]+
251 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (1H–indazol–6–il)but–1–en–1–il)fenil)acrílico imagen154 435
252
Ácido (E)–3–(4–((E)–2–(3–(1H–Pirazol–1– il)fenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 461
253
Ácido (E)–3–(4–((E)–2–(2,4–Diclorofenil)–1– (7–fluoro–1H–indol–5–il)but–1–en–1– il)fenil)acrílico 478
254
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(7–fluoro–1H–indom–5–il)but– 1–en–1–il)fenil)acrílico no observado
255 *
Ácido (E)–3–(4–((E)–2–(Benzo[d]tiazol–5–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 452
Compuesto
Nombre Estructura LCMS [M+M]+
256 *
Ácido (E)–3–(4–((E)–2–(2,3– Dihidrobenzofuran–5–il)–1–(1H–indazol–5– il)but–1–en–1–il)fenil)acrílico imagen155 437
257 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–4– metil–2–(4–metiltiofen–3–il)pent–1–en–1– il)fenil)acrílico 443
258 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (1–metil–1H–indazol–6–il)but–1–en–1– il)fenil)acrílico 449
259 *
Ácido (E)–3–(4–((E)–2–(Benzo[d]tiazol–6–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 452
260 *
Ácido (E)–3–(4–((E)–2–(Imidazo[1,2–a]piridin– 6–il)–1–(1H–indazol–5–y)but–1–en–1– il)fenil)acrílico 435
Compuesto
Nombre Estructura LCMS [M+M]+
261 *
Ácido (E)–3–(4–((E))–1–(1H–Indazol–5–il)–2– (3–fenoxifenil)but–1–en–1–il)fenil)acrílico imagen156 487
262 *
Ácido (E)–3–(4–((E)–1–(1H–indazol–5–il)–2– (4–metil–3–oxo–3,4–dihidro–2H– benzo[b][1,4]oxazin–6–il)but–1–en–1– il)fenil)acrílico imagen157 480
263 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–fenoxifenil)but–1–en–1–il)fenil)acrílico 487
264 *
Ácido (E)–3–(4–((E)–2–(4–(1H–Pyrazol–1– il)fenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen158 461
265 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–morfolinofenil)but–1–en–1–il)fenil)acrílico imagen159 480
Compuesto
Nombre Estructura LCMS [M+M]+
266 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (quinoxalin–6–il)but–1–en–1–il)fenil)acrílico imagen160 447
267 *
Ácido (E)–3–(4–((E)–2–(2–Clorotiofen–3–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 435
268 *
Ácido (E)–3–(4–((E)–2–(Benzo[b]tiofen–2–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen161 451
269 *
Ácido (E)–3–(4–((E)–2–(3–(4– Fluorofenoxi)fenil)–1–(1H–indazol–5–il)but–1– en–1–il)fenil)acrílico 505
270 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (5–metil–4,5,6,7–tetrahidrotieno[3,2–c]piridin– 2–il)but–1–en–1–il)fenil)acrílico 470
Compuesto
Nombre Estructura LCMS [M+M]+
271 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (5–feniltiofen–3–il)but–1–en–1–il)fenil)acrílico imagen162 477
272*
Ácido (E)–3–(4–((E)–2–(Benzo[b]tiofen–5–il)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen163 451
273*
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metilbenzo[d]tiazol–5–il)but–1–en–1– il)fenil)acrílico 466
274*
Ácido (E)–3–(4–((E)–2–(2,5–Dimetiltiofen–3– il)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 429
275*
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(2–cloro–4–Fluorofenil)but–1–en–1– il)fenil)acrílico 464
Compuesto
Nombre Estructura LCMS [M+M]+
276*
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(4–metiltiofen–3–il)but–1–en–1– il)fenil)acrílico imagen164 432
277
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–3,3,4,4,4–pentadeutero–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 452
278*
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(2–cloro–4–Fluorofenil)–2– ciclobutilovinil)fenil)acrílico 490
279*
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–ciclobutilo–2–(4–metiltiofen–3– il)vinil)fenil)acrílico imagen165 458
Compuesto
Nombre Estructura LCMS [M+H]+
280 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(2–clorofenil)but–1–en–1–il)fenil)acrílico imagen166 446
281 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(4–Fluorofenil)but–1–en–1–il)fenil)acrílico 430
282 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(4–fluoro–2–metilfenil)but–1–en–1– il)fenil)acrílico 444
283 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(o–toluil)but–1–en–1–il)fenil)acrílico 426
284 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(3–cloropiridin–4–il)but–1–en–1– il)fenil)acrílico 447
Compuesto
Nombre Estructura LCMS [M+H]+
285 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il– 2–(3–cloropiridin–4–il)but–1–en–1– il)fenil)acrílico imagen167 473
286 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–ciclobutilo–2–fenilvinil)fenil)acrílico 438
287 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1–oxoisoindolin–5–il)but–1– en–1–il)fenil)acrílico imagen168 462
288
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(4–((trifluorometil)sulfonil)fenoxi)fenil)but– 1–en–1–il)fenil)acrílico 527
289 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(quinolin–7–il)but–1–en–1– il)fenil)acrílico 458
Compuesto
Nombre Estructura LCMS [M+H]+
290 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(pirimidin–2–iloxifenil)but–1–en–1– il)fenil)acrílico imagen169 489
291 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– fenoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen170 521
292 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(piridin–3–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen171 488
293 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(pirazin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico 489
294 *
Ácido (E)–3–(4–((E)–2–(4–Fluoro–3– fenoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen172 505
Compuesto
Nombre Estructura LCMS [M+H]+
295 *
Ácido (E)–3–(4–((E)–2–(3–Fluoro–4– fenoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen173 505
296 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(4–(piridin–2–iloxi)fenil)but–1– en–1–il)fenil)acrílico 506
297 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–metil–5–fenoxifenil)but–1–en–1– il)fenil)acrílico 501
298 *
Ácido (E)–3–(4–((E)–2–(2–Fluoro–3– fenoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 505
299 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(3–fenoxifenil)but–1–en–1–il)fenil)acrílico 504
Compuesto
Nombre Estructura LCMS [M+H]+
300 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(3–(piridin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen174 505
301 *
Ácido (E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)– 2–(3–(pirazin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen175 506
302
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–((trifluorometil)sulfinil)fenil)but–1–en–1– il)fenil)acrílico imagen176 511
303
Ácido (E)–3–(4–((E)–2–(3–Cianopiridin–4–il)– 1–(1H–indazolol–5–il)but–1–en–1– il)fenil)acrílico imagen177 421
304 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(trifluorometil)piridin–4–il)but–1–en–1– il)fenil)acrílico 464
Compuesto
Nombre Estructura LCMS [M+H]+
305 *
Ácido (E)–3–(4–((E)–2–(3–Cloropiridin–4–il)– 2–ciclobutilo–1–(1H–indazol–5– il)vinil)fenil)acrílico imagen178 456
306 *
Ácido (E)–3–(4–((E)–2–(3–Cloropiridin–4–il)– 1–(3–fluoro–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 448
307 *
Ácido (E)–3–(4–((E)–1–(3–Cloropiridin–4–il)– 2–ciclobutilo–1–(3–fluoro–1H–indazol–5– il)vinil)fenil)acrílico 474
308
Ácido (E)–3–(4–((E)–2–(4–Cloro–2– cianofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 454
309
Ácido (E)–3–(4–((E)–(2–Ciano–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 438
Compuesto
Nombre Estructura LCMS [M+H]+
310
Ácido (E)–3–(4–((E)–2–(2–Ciano–4– (trifluorometil)fenil)–1–(1H–indazol–5–il)but–1– en–1–il)fenil)acrílico imagen179 488
311 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–2–ciclobutilo–1–(imidazo[1,2– a]piridin–6–il)vinil)fenil)acrílico 473
312 *
Ácido (E)–3–(4–((E)–1–(3–Fluoro–1H– indazol–5–il)–2–(4–metiltiofen–3–il)but–1–en– 1–il)fenil)acrílico 433
313 *
Ácido (E)–3–(4–((E)–2–Ciclobutil–1–(3–fluoro– 1H–indazol–5–il)–2–(4–metiltiofen–3– il)vinil)fenil)acrílico 459
314 *
Ácido (E)–3–(4–((E)–2–(Benzo[d]isotiazol–5– il)–1–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 452
Compuesto
Nombre Estructura LCMS [M+H]+
315 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(piridin–4–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen180 488
316 *
Ácido (E)–3–(4–((E)–1–(1H–Indalol–5–il)2–(4– (piridin–2–iloxi)fenil)but–1–en–1–il)fenil)acrílico 488
317 *
Ácido (E)–3–(4–((E)–2–(4–Bencilfenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrílico 485
318 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–metil–3–fenoxilfenil)but–1–en–1– il)fenil)acrílico imagen181 501
319 *
Ácido (E)–3–(4–((E)–1–(1H)–Indazol–5–il)–2– (2–metil–4–fenoxifenil)but–1–en–1– il)fenil)acrílico 501
Compuesto
Nombre Estructura LCMS [M+H]+
320 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–metil–4–fenoxifenil)but–1–en–1– il)fenil)acrílico imagen182 50]
321 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(3–(metilsulfonil)fenoxi)fenil)but–1–en–1– il)fenil)acrílico imagen183 565
322
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– cianofenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 454
323
Ácido (E)–3–(4–((E)–2–(3–Ciano–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen184 434
324
Ácido (E)–3–(4–((E)–2–(4–Ciano–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 434
Compuesto
Nombre Estructura LCMS [M+H]+
325
Ácido (E)–3–(4–((E)–2–(5–Ciano–2– metilfenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen185 434
326
Ácido (E)–3–(4–((E)–2–(2–Ciano–4– metoxifenil)–1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 450
327
Ácido (E)–3–(4–((E)–2–(3– (Carboximetil)fenil)–1–(1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 453
328
Ácido (E)–3–(4–((E)–2–(4–(Carboximetilfenil)– 1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 453
329 *
5–((E)–1–(4–((S)–2–((R)–3–Metilpirrolidin–1– il)propoxi)fenil)–2–fenilbut–1–en–1–il)–1H– indazol imagen186 466
Compuesto
Nombre Estructura LCMS [M+H]+
330 *
5–((E)–2–(2–Clorofenil)–1–(4–((S)–2–((R)–3– metilpirrolidin–1–il)propoxi)fenil)but–1–en–1– il)–1H–indazol imagen187 500
331 *
5–((E)–2–(3–Cloropiridin–4–il)–1–(4–((S)–2– ((R)–3–metilpirrolidin–1–il)propoxi)fenil)but– 1–en–1–il)–1H–indazol imagen188 501
332 *
Ácido (E)–1–(4–(2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1– il)fenoxi)ciclopropanocarboxílico 477
333 *
(E)–5–(4–(2–(2–Cloro–4–Fluorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)isoxazol–3–ol 460
334 *
(E)–3–(4–(2–(2–Cloro–4–Fluorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)isoxazol–5–ol 460
Compuesto
Nombre Estructura LCMS [M+H]+
335
Ácido (E)–3–(4–((E)–2–(3–Hidroxifenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen189 411
336
Ácido (E)–3–(4–((E)–2–(2–Hidroxifenil)–1– (1H)–indazol–5–il)but–1–en–1–il)fenil)acrílico 411
337
Ácido (E)–3–(4–((E)–2–(4–Hidroxifenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen190 411
338
Ácido (E)–3–(4–(1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)propanoico 397
339 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5– metoxietoxi)fenil)but–1–en–1–il)fenil)acrílico 469
Compuesto
Nombre Estructura LCMS [M+H]+
340 *
Ácido (E)–3–(4–(E)–1–(1H–Indazol–5–il)–2– (4–(3–metoxipropoxi)fenil)but–1–en–1– il)fenil)acrílico imagen191 483
341 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(2–metoxietoxi)fenil)but–1–en–1– il)fenil)acrílico 469
342 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(3–metoxipropoxi)fenil)but–1–en–1– il)fenil)acrílico imagen192 483
343 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(3–((1–metilpiperidin–4– il)oxi)fenil)but–1–en–1–il)fenil)acrílico imagen193 526
344 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–(3–((tetrahidro–2H–piran–4– il)oxi)fenil)but–1–en–1–il)fenil)acrílico imagen194 513
Compuesto
Nombre Estructura LCMS [M+H]+
345
Ácido (E)–3–(4–((E)–2–(3– (Ciclohexiloxi)fenil)–1–(4–fluoro–1H–indazol– 5–il)but–1–en–1–il)fenil)acrílico imagen195 511
346
Ácido (E)–3–(4–((E)–2–(3–Butoxifenil–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen196 467
347 *
Ácido (E)–3–(4–((E)–2–(3– (Carboximetoxi)fenil)–1–(1H–indazol–5– il)but–1–en–1–il)fenil)acrílico 469
348 *
Ácido (E)–3–(4–((E)–2–(4– (Carboximetoxi)fenil)–1–(1H–indazol–5– il)but–1–en–1–il)fenil)acrílico 469
349
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pentiloxi)fenil)but–1–en–1–il)fenil)acrílico imagen197 481
Compuesto
Nombre Estructura LCMS [M+H]+
350
Ácido (E)–3–(4–((E)–2–(3–(Hexiloxi)fenil)– 1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen198 495
351 *
Ácido 4–(3–((E)–1–(4–((E)–2– Carboxivinil)fenil)–1–(1H–indazol–5–il)but– 1–en–2–il)fenoxi)butanoico 497
352 *
Ácido 5–(3–((E)–1–(4–((E)–2– Carboxivinil)fenil)–1–(1H–indazol–5–il)but– 1–en–2–il)fenoxi)pentanoico imagen199 511
353 *
Ácido 4–(4–((E)–1–(4–((E)–2– Carboxivinil)fenil)–1–(1H–indazol–5–il)but– 1–en–2–il)fenoxi)butanoico 497
354 *
Ácido 5–(4–((E)–1–(4–((E)–2– Carboxivinil)fenil)–1–(1H–indazol–5–il)but– 1–en–2–il)fenoxi)pentanoico imagen200 511
Compuesto
Nombre Estructura LCMS [M+H]+
355
Ácido (E)–3–(4–((E)–2–(4–Butoxifenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico imagen201 467
356
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(pentiloxi)fenil)but–1–en–1–il)fenil)acrílico 481
357
Ácido (E)–3–(4–((E)–1–(4–(Hexiloxi)fenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 495
358 *
Ácido (E)–3–(4–((E)–2–(3–(Benciloxi)fenil)– 1–(1H–indazol–5–il)but–1–en–1– il)fenil)acrílico 501
359 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–3–ilmetoxi)fenil)but–1–en–1– il)fenil)acrílico 502
Compuesto
Nombre Estructura L–CMS [M+H]+
360 *
Ácido (E)–3–(4–((E)–2–(4–(2– Hidroxietoxi)fenil)–1–(1H–indazol–5–il)but–1– en–1–il)fenil)acrílico imagen202 455
361
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (2–(metilsulfonil)fenil)but–1–en–1– il)fenil)acrílico 473
362 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen203 488
363 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pirimidin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico 489
364
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pirimidin–4–iloxi)fenil)but–1–en–1 il)fenil)acrílico 489
Compuesto
Nombre Estructura L–CMS [M+H]+
365 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–3–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen204 488
366 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–4–iloxi)fenil)but–1–en–1– il)fenil)acrílico 488
367 *
Ácido (E)–3–(4–((E)–2–(3–(2– Fluorofenoxi)fenil)–1–(1H)–indazol–5–il)but–1– en–1–il)fenil)acrílico 505
368 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(o–toliloxi)fenil)but–1–en–1–il)fenil)acrílico imagen205 501
369 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pirimidin–5–iloxi)fenil)but–1–en–1– il)fenil)acrílico 489
Compuesto
Nombre Estructura L–CMS [M+H]+
370 *
Ácido (E)–3–(4–((E)–]–1–(1H–Indazol–5–il)– 2–(3–(tiazol–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico imagen206 494
371 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(pirazin–2–iloxi)fenil)but–1–en–1– il)fenil)acrílico 489
372 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–((3–(trifluorometil)piridin–4–il)oxi)fenil)but– 1–en–1–il)fenil)acrílico 556
373 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(4–(metilsulfonil)fenoxi)fenil)but–1–en–1– il)fenil)acrílico 565
374 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(2–(metilsulfonil)fenoxi)fenil)but–1–en–1– en–il)fenil)acrílico imagen207 565
Compuesto
Nombre Estructura L–CMS [M+H]+
375 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(3–(piridin–2–iloxi)fenil)but–1– en–1–il)fenil)acrílico imagen208 506
376 *
Ácido (E)–3–(4–((E))–1–(4–fluoro–1H– indazol–5–il)–2–(3–(pirimidin–2–iloxi)fenil)but– 1–en–1–il)fenil)acrílico imagen209 507
377 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(3–(pirazin–2–iloxi)fenil)but– 1–en–1–il)fenil)acrílico 507
378 *
Ácido (E)–3–(4–((E)–1–(4–Fluoro–1H– indazol–5–il)–2–(3–((6–(metilsulfonil)piridin–3– il)oxi)fenil)but–1–en–1–il)fenil)acrílico 584
379 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–((5–(metilsulfonil)piridin–2–il)oxi)fenil)but– 1–en–1–il)fenil)acrílico 566
Compuesto
Nombre Estructura L–CMS [M+H]+
380 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–((6–(metilsulfonil)piridin–3–il)oxi)fenil)but– 1–en–1–il)fenil)acrílico imagen210 566
381 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–((5–(trifluorometil)piridin–2–il)oxi)fenil)but– 1–en–1–il)fenil)acrílico 556
382 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–((6–metilpiridin–3–il)oxi)fenil)but–1–en–1– il)fenil)acrílico imagen211 502
383 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(pirimidin–5–il)fenil)but–1–en–1– il)fenil)acrílico imagen212 473
Compuesto
Nombre Estructura LCMS [M+H]+
384 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5 il)–2– (4–(1–metil–1H–pirazol–4–il)fenil)but–1–en– 1–il)fenil)acrílico imagen213 475
385 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(piridin–2–il)fenil)but–1–en–1– il)fenil)acrílico 472
386 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(tiofen–3–il)fenil)but–1–en–1– il)fenil)acrílico 477
387 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(tiazol–2–il)fenil)but–1–en–1–il)fenil)acrílico 478
Compuesto
Nombre Estructura LCMS [M+H]+
388 *
Ácido (E)–3–(4–((E)–(1H–Indazol–5–il)–2–(4– (thiazol]–4–ilfenil)but–1–en–1–il)fenil)acrílico imagen214 478
389 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(pirazin–2–il)fenil)but–1–en–1– il)fenil)acrílico imagen215 473
390 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–2–il)fenil)but–1–en–1– il)fenil)acrílico 472
391 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5 il)–2– (3–(tiazol–2–il)fenil)but–1–en–1–il)fenil)acrílico 478
392 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(tiazol–4–il)fenil)but–1–en–1–il)fenil)acrílico 478
Compuesto
Nombre Estructura LCMS [M+H]+
393 *
Ácido (E)–3–(4–((E)–1–1H–Indazol–5–il)–2– (3–(piridin–3–il)fenil)but–1–en–1– il)fenil)acrílico imagen216 472
394 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (3–(piridin–4–il)fenil)but–1–en–1– il)(fenil)acrílico 472
395 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(isotiazol–4–il]fenil)but–1–en–1– il)fenil)acrílico 478
396 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(metil(fenil)amino)fenil)but–1–en–1– il)fenil)acrílico imagen217 500
397 *
Ácido (E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– (4–(fenilamino)fenil)but–1–en–1–ilfenil)acrílico 486
Compuesto
Nombre Estructura LCMS [M+H]+
398 *
Ácido (E)–3–(4–((E)–2–(2–Clorofenil)–1–(– metil–1H–indazol–5–il)but–1–en–1– il)fenil)acrílico imagen218 443
399 *
Ácido (E)–3–(4–((E)–2–Ciclobutil–1–(1–metil– 1H–indazol–5–il)–2–fenilvinil)fenil)acrílico 435
400 *
Ácido (E)–3–(4–((E)–2–(2–(2–Cloro–4– Fluorofenil)–1–(1–metil–1H–indazol–5–il)but– 1–en–1–il)fenil)acrílico 461
401 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1–(difluorometil)–1H–indazol– 5–il)but–1–en–1–il)fenil)acrílico imagen219 497
402 *
Ácido (E)–3–(4–((E)–2–Cloro–4–Fluorofenil)– 1–(2–(difluorometil)–2H–indazol–5–il)but–1– en–1–il)fenil)acrílico 497
Compuesto
Nombre Estructura LCMS [M+H]+
403 *
Ácido (E)–3–(4–((E)–1–(1–Acetil–1H–indazol– 5–il)–2–(2–cloro–4–Fluorofenil)but–1–en–1– il)fenil)acrílico imagen220 489
404 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1–isobutyril–1H–indazol–5– il)but–1–en–1–il)fenil)acrílico imagen221 517
405 *
Ácido (E)–3–(4–((E)–2–(2–(Cloro–4– Fluorofenil)–1–(1–pivaloil–1H–indazol–5– il)but–1–en–1–il)fenil)acrílico 531
406 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1–(etoxicarbonil)–1H–indazol– 5–il)but–1–en–1–il)fenil)acrílico imagen222 519
407 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(1–(tetrahidro–2H–piran–2–il)– 1H–indazol–5–il)but–1–en–1–il)fenil)acrílico 447 [(M–THP+H )+H]+
Compuesto
Nombre Estructura LCMS [M+H]+
408 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)–N– (metilsulfonil)acrilamida imagen223 524
409 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)–N– (propilsulfonil)acrilamida 552
410 *
(E)–3–(4–((E)–1–(2–Cloro–4–flurofenil)–1– (1H–indazol–5–il)but–1–en–1–fenil)–N– (pentilsulfonil)acrilamida imagen224 580
411 *
(E)–3–(4–((E)–2–Ciclobutil–1–(1–metil–1H– indazol–5–il)–2–fenilvinil)fenil)–N– metilacrilamida imagen225 448
412 *
(E)–3–(4–((E)–2–Ciclobutil–1–(1H–indazol– 5–il)–2–fenilvinil)fenil)fenil)–N– metilacrilamida 434
Compuesto
Nombre Estructura LCMS [M+H]+
413 *
(E)–3–(4–((E)–2–Ciclobutil–1–(3–fluoro–1H– indazol–5–il)–2–fenil)vinil)fenil)–N– ciclopropiloacrilamida imagen226 478
414 *
(E)–3–(4–((E)–2–Ciclobutil–1–(3–fluoro–1H– indazol–5–il)–2–fenilvinil)fenil)–N–(2– hidroxietil)acrilamida 482
415 *
(E)–3–(4–((E)–2–Ciclobutil–1–(3–fluoro–1H– indazol–5–il)–2–fenilvinil)fenil–N–(2,2,2,– trifluoroetil)acrilamida imagen227 520
416 *
(E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)–2–(2– cloro–4–Fluorofenil)but–1–en–1–il)fenil)–N– (metilsulfonil)acrilamida imagen228 541
417 *
(E)–3–(4–((E)–2–Cloro–4–Fluorofenil)–1–(1H– indazol–5–il)but–1–en–1–il)fenil)acrilamida 446
Compuesto
Nombre Estructura LCMS [M+H]+
418 *
(E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)–N–hidroxiacrilamida imagen229 410
419 *
(E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)–N–isopropilacrilamida 436
420 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)–N– metilacrilamida 460
421 *
(E)–3–(4–((E)–2–(2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)–N– metoxiacrilamida 476
422 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)–N– metoxi–N–metilacrilamida imagen230 490
Compuesto
Nombre Estructura LCMS [M+H]+
423 *
(E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)–N– (metilsulfonil)acrilamida imagen231 472
424 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1–metil–1H–indazol–5–il)but–1–en–1– il)fenil)–N–(metilsulfonil)acrilamida imagen232 538
425 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)fenil)–N– (2H–tetrazol–5–il)acrilamida 514
426 *
(E)–3–(4–((E)–1–(Benzo[d]tiazol–5–il)–2– fenilbut–1–co–1–il)fenil)acrilamida imagen233 41
427 *
(E)–3–[4–((E)–1–(Benzo[d]tiazol–5–il)–2– fenilbut–1–en–1–il)fenil)–N–metilacrilamida 425
Compuesto
Nombre Estructura LCMS [M+H]+
428 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)– N–(fenilsulfonil)acrilamida imagen234 586
429 *
(E)–N–(Bencilsulfonil)–3–(4–((E)–2–(2– cloro–4–Fluorofenil)–1–(1H–indazol–5– il)but–1–en–1–il)fenil)acrilamida imagen235 600
430 *
(E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil–N–(tiazol–2– il)acrilamida 477
431 *
(E)–3–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)–N– ciclopentiloacrilamida 462
432 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)– N–(piridin–2–ilsulfonil)acrilamida imagen236 587
Compuesto
Nombre Estructura LCMS [M+H]+
433 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)– N–(piridin–3–ilsulfonil)acrilamida imagen237 587
434 *
(E)–3–(4–((E)–2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)fenil)– N–(piridin–4–ilsulfonil)acrilamida imagen238 587
435 *
3–((E)–4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)estiril)–1,2,4–oxadiazol– 5(4H)–ona imagen239 435
436 *
3–((E)–4–((E)–1–(Benzo[d]tiazol–5–il)–2– (2–cloro–4–Fluorofenil)but–1–en–1– il)estiril)–1,2,4–oxadiazol–5(4H)–ona 504
437 *
3–((E)–4–((E)–2–(2–Cloro–4–Fluorofenil)– 1–(1H–indazol–5–il)but–1–en–1–il)estiril)– 1,2,4. oxadiazol–5(4H)–ona 487
Compuesto
Nombre Estructura LCMS [M+H]+
438 *
3–((E)–4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)estiril)–1–,2,4–tiadiazol– 5(4H)–ona imagen240 451
439 *
3–((E)–4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)estiril)–1,2,4– tiadiazol–5(4H)–ona 503
440 *
3–((E)–4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)estiril)–1,2,4–oxadiazol– 5(4H)–tiona 451
441 *
3–((E)–4–((E)–2–(2–Cloro–4–Fluorofenil)–1– (1H–indazol–5–il)but–1–en–1–il)estiril)–1,2,4– oxadiazol–5(4H)–tiona 503
442 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–fenilbut–1–en–1–il)–1H– indazol 419
Compuesto
Nombre Estructura LCMS [M+H]+
443 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–(2–clorofenil)but–1–en–1–il)– 1H–indazol imagen241 453
444 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–fenilbut–1–en–1– il)benzo[d]tiazol imagen242 436
445 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–(2–cloro–4–Fluorofenil)but–1– en–1–il)benzo[d]tiazol 488
446 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–(3–cloropiridin–4–il)but–1–en– 1–il)benzo[d]tiazol 471
447 *
5–((E)–1–(4–((E)–2–(2H–Tetrazol–5– il)vinil)fenil)–2–(4–metiltiofen–3–il)but–1–en– 1–il)benzo[d]tiazol imagen243 456
Compuesto
Nombre Estructura LCMS [M+H]+
448 *
5–((E)–1–((E)–2–(2H–Tetrazol–5–il)vinil)fenil)– 2–ciclobutilo–2–(4–metiltiofen–3– il)vinil)benzo[d]tiazol imagen244 482
449
Ácido (E)–6–(1–(1H–Indazol–5–il)–2–fenilbut– 1–en–1–il)–2–naftoico 419
450 *
Ácido (E)–3–(4–((E)–2–(2–Cloro–4– Fluorofenil)–1–(7–hidroxibenzofuran–3–il)but– 1–en–1–il)fenil)acrílico 463
451 *
Ácido (E)–3–(4–((E)–1–(7–Hidroxibenzofuran– 3–il)–2–fenilbut–1–en–1–il)fenil)acrílico imagen245 411
452 *
(E)–2–(4–((E)–1–(1H–Indazol–5–il)–2– fenilbut–1–en–1–il)fenil)etanosulfonamida 430
imagen246
imagen247
imagen248
imagen249
imagen250
imagen251
imagen252
imagen253
imagen254
imagen255
imagen256
imagen257
imagen258
imagen259
imagen260
imagen261
imagen262
imagen263
imagen264
imagen265
imagen266
imagen267
imagen268
imagen269
imagen270
imagen271
imagen272
imagen273
imagen274
imagen275
imagen276
imagen277
Un matraz de fondo redondo de 200 mL equipado con una barra agitadora magnética, un septum de goma y entrada de N2 se cargó con 5–etinil–1– (tetrahidro–2H–piran–2–il) –1H–benzo [d] [1,2,3]triazol (2.5 g, 11 mmol) y THF anhidro (110 mL). Esta solución se enfrió entonces hasta 0 ºC en un baño de hielo. Entonces, se agregó una solución de LiHMDS (27 mL, THF 5 1M, 27 mmol) gota a gota durante 15 minutos. La mezcla resultante se agitó durante 1 h a 0 ºC. A esta mezcla a 0 ºC, se agregó yodoetano (4.4 mL, 55 mmol) gota a gota durante 5 minutos. La mezcla se calentó gradualmente hasta temperatura ambiente, se agitó durante 1 h, y luego se calentó a reflujo durante la noche. La reacción se monitorizó por LCMS. Al terminar, la mezcla de reacción se enfrió hasta temperatura ambiente, se detuvo con agua (100 mL), y se extrajo con acetato de etilo (2x100 mL). Las fases orgánicas combinadas se lavaron con agua (100 mL), se lavaron con salmuera (50 10 mL), se secaron sobre sulfato de sodio, se filtraron, y se concentraron para dar el producto crudo. Este material crudo se purificó sobre una columna de sílica gel eluida con 5% de acetato de etilo en hexanos produciendo el compuesto del título en forma de un aceite de color amarillo pálido (1.6g). 1H RMN (300 MHz, DMSO–d6): δ 7.92 (s, 1H), 7.85 (dd, 1H), 7.33 (dd, 1H), 6.01 (dd, 1H), 3.86–3.80 (m, 1H), 3.75–3.64 (m, 1H), 2.45–2.36 (m, 3H), 2.08–1.91 (m, 2H), 1.74–1.62 (m, 1H), 1.58–
1.50 (m, 2H), 1.11 (t, 3H); LCMS: 172 [(M–THP+H)+H]+.
15 Los Intermediarios de la Tabla 2 se prepararon a partir de materiales de partida conocidos o comerciales siguiendo los procedimientos delineados para los Intermediarios 1–4.
Intermediario 5
6–(But–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H–indazol
Intermediario 6
4–(But–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H–indazol
Intermediario 7
1–(Tetrahidro–2H–piran–2–il)–5–(4,4,4–trideuterobut–1–in– 1–il)–1H–indazol imagen278
Intermediario 8
5–(But–1–in–1–il)–7–cloro–1–(tetrahidro–2H–piran–2–il)– 1H–indazol imagen279
Intermediario 9
5–(But–1–in–1–il)–7–metil–1–(tetrahidro–2H–piran–2–il)– 1H–indazol
Intermediario 10
5–(But–1–in–1–il)–3–metil–1–(tetrahidro–2H–piran–2–il)– 1H–indazol
Intermediario 11
5–(But–1–in–1–il)–3–cloro–1–(tetrahidro–2H–piran–2–il)– 1H–indazol imagen280
Intermediario 12
5–(Prop–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H– indazol
Intermediario 13
5–(Pent–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H– indazol imagen281
Intermediario 14
5–(Perdeuterobut–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)– 1H–indazol
Ejemplo 5: Preparación de 5–(But–1–in–1–il)–4–metil–1–(tetrahidro–2H–piran–2–il)–1H–indazol (Intermediario 15)
imagen282
Etapa 1: 4–Metil–1–(tetrahidro–2H–piran–2–il)–5–((trimetilsilil)etinil)–1H–indazol
imagen283
Una mezcla de 5–bromo–4–metil–1– (tetrahidro–2H–piran–2–il) –1H–indazol (915 mg, 3.10 mmol; preparada a partir de 5– bromo–4–metil–1H–indazol siguiendo el procedimiento delineado para el Intermediario 1), yoduro de cobre (72 mg, 0,38 mmol), tetracloropaladato de sodio (55 mg, 0.19 mmol), 2–(di–tert–butilfosfino)–1–fenil–1H–indol (128 mg, 0.379 mmol ), y TMEDA: H2O (9:1, 10 mL) se desgasificó con tres ciclos de vacío/nitrógeno. Se agregó etiniltrimetilsilano a la reacción, y la 10 mezcla se calentó hasta 80 ºC durante 90 min y luego se enfrió hasta temperatura ambiente. La mezcla de reacción se filtró a través de Celita y la Celita se lavó con acetato de etilo (100 mL). El filtrado se lavó (solución saturada de NaHCO3, 2 x 50 mL), se secó (Na2SO4), y se concentró bajo presión reducida. El material crudo se purificó sobre una columna de sílica gel
imagen284
imagen285
imagen286
En un tubo de alta presión, una mezcla de 5–bromo–4–fluoro–1– (tetrahidro–2H–piran–2–il)–H–indazol (8.0 g, 26.8 mmol; Intermediario 21), PdCl2(PPh)3)2 (3.7 g, 5.35 mmol), CuI (1.0 g, 5.35 mmol) y trietilamina (30 mL) se desoxigenó con tres ciclos de vacío/nitrógeno. Se agregó etinilciclopropano (8.9 g, 134 mmol) bajo atmósfera de N2. El tubo se selló y la mezcla de reacción se calentó a 120 ºC durante 63 horas. Al terminar, la mezcla de reacción se diluyó con acetato de etilo y se filtró 5 a través de Celita. El filtrado se concentró in vacuo y el residuo se purificó mediante cromatografía de columna sobre sílica gel (0~10% de acetato de etilo en éter de petróleo) produciendo el compuesto del título (4.3 g). 1H RMN (400MHz, DMSO– d6): δ 8.25 (s, 1H), 7.55 (d, 1H), 7.40 (dd, 1H), 5.88 (dd, 1H), 3.88–3.85 (m, 1H), 3.76–3.73 (m, 2H), 2.43–2.33 (m, 1H), 2.05–
1.95 (m, 2H), 1.76–1.72 (m, 1H), 1.62–1.56 (m, 3H), 0.93–0.89 (m, 2H), 0.79–0.74 (m, 2H); LCMS: 285 (M+H)+.
Los compuestos Intermediarios en la Tabla 4 se prepararon a partir del Intermediario 1 (o el isómero 4–bromo) siguiendo los 10 procedimientos delineados para los Intermediarios 17–20, 22.
Tabla 4.
Intermediario 23
4–(Ciclopropiloetinil)–1–(tetrahidro–2H–piran–2–il)–1H–indazol
Intermediario 24
5–(Ciclopentiloetinil)–1–(tetrahidro–2H–piran–2–il)–1H–indazol imagen287
Intermediario 25
5–(Ciclohexiloetinil)–1–(tetrahidro–2H–piran–2–il)–1H–indazol
Intermediario 26
5–(3–Metilbut–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H–indazol imagen288
Intermediario 27
5–(Hex–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H–indazol
Intermediario 28
5–(3–Ciclopentiloprop–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)– 1H–indazol

Ejemplo 12: Preparación de 5–(4–Clorobut–1–in–1–il)–1–(tetrahidro–2H–piran–2–il)–1H–indazol (Intermediario 29)
imagen289
imagen290
imagen291
imagen292
imagen293
imagen294
imagen295
imagen296
imagen297
imagen298
imagen299
imagen300
imagen301
imagen302
imagen303
imagen304
imagen305
imagen306
imagen307
imagen308
imagen309
mezcla se agitó a temperatura ambiente durante la noche, y luego se agregó ácido fenil borónico adicional (186, 1.53 mmol). La reacción se agitó a temperatura ambiente durante 7 horas adicionales y se filtró a través de Celita con diclorometano. El filtrado se concentró y se purificó por cromatografía en sílica gel (100% de hexanos) para dar 1–bromo–2–cloro–4– fenoxibenceno (90 mg) como un líquido transparente. 1H RMN (400 MHz, DMSO–d6): δ 7.75 (d, 1H), 7.42–7.47 (m, 2H),
7.27 (d, 1H), 7.23 (t, 1H), 7.11 (d, 2H), 6.92 (dd, 1H).
Los compuestos Intermediarios de la Tabla 9 se prepararon siguiendo el procedimiento delineado para el Intermediario 65.
Tabla 9.
Intermediario 66
4–Bromo–1–fluoro–2–fenoxibenceno
Intermediario 67
4–Bromo–2–fluoro–1–fenoxibenceno
Intermediario 68
2–Bromo–1–metil–4–fenoxibenceno
Intermediario 69
1–Bromo–2–fluoro–3–fenoxibenceno
Intermediario 70
4–Bromo–1–metil–2–fenoxibenceno
Intermediario 71
1–Bromo–2–metil–4–fenoxibenceno
Intermediario 72
4–Bromo–2–metil–1–fenoxibenceno
Intermediario 73
(1–Yodo–3–(3– (metilsulfonil)fenoxi)benceno

Ejemplo 42: Preparación de 2–Bromo–5–metil–4,5,6,7–tetrahidrotieno[3,2–c]piridina (Intermediario 74)
imagen310
imagen311
imagen312
imagen313
imagen314
imagen315
imagen316
imagen317
imagen318
imagen319
imagen320
imagen321
imagen322
imagen323
imagen324
imagen325
imagen326
imagen327
imagen328
imagen329
imagen330
imagen331
imagen332
imagen333
imagen334
imagen335
imagen336
imagen337
imagen338
imagen339
imagen340
imagen341
imagen342
imagen343
imagen344
imagen345
imagen346
imagen347
imagen348
imagen349
imagen350
imagen351
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
1
A + A ++
2
A ++ A ++
3
A ++ A ++
4
A ++ A ++
5
B ++ B ++
6
A ++ A ++
7
A ++ A ++
8
B ++ A ++
9
A ++ A ++
10
B ++ A ++
11
A ++ A ++
12
A ++ A ++
13
A ++ A ++
14
A ++ A ++
15
A ++ A ++
16
A ++ A ++
17
A ++ A ++
18
A ++ A ++
19
A ++ A ++
20
A ++ A ++
21
A ++ A ++
22
A ++ A ++
23
A ++ A ++
24
A ++ A ++
25
B ++ B ++
26
A ++ A ++
27
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
28
B ++ B ++
29
A ++ A ++
30
A ++ A ++
31
A ++ A ++
32
A ++ A ++
33
A ++ A ++
34
A ++ A ++
35
A ++ A ++
36
A ++ A ++
37
A ++ A ++
38
A ++ A ++
39
A ++ A ++
40
A ++ A ++
41
A ++ A ++
42
A ++ A ++
43
A ++ A ++
44
A ++ A ++
45
A ++ A ++
46
A ++ A ++
47
A ++ A ++
48
A ++ A ++
49
B ++ B ++
50
A ++ A ++
51
B ++ B ++
52
B ++ B ++
53
A ++ A ++
54
A ++ A ++
55
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
56
B ++ A ++
57
A ++ A ++
58
A ++ A ++
59
B + B ++
60
A ++ A ++
61
A ++ A ++
62
B ++ B ++
63
A ++ A ++
64
A ++ A ++
65
A ++ A ++
66
A ++ A ++
67
B ++ B ++
68
B ++ B ++
69
A ++ A ++
70
A ++ A ++
71
A ++ A ++
72
A ++ A ++
73
A ++ A ++
74
A ++ A ++
75
B ++ B ++
76
A ++ A ++
77
A ++ A ++
78
A ++ A ++
79
A ++ A ++
80
A ++ A ++
81
B ++ B ++
82
A ++ A ++
83
B ++ B ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
84
A ++ A ++
85
A ++ A ++
86
A ++ A ++
87
A ++ A ++
88
B ++ B ++
89
A ++ A ++
90
B ++ B ++
91
A ++ A ++
92
A ++ A ++
93
A ++ A ++
94
A ++ A ++
95
A ++ A ++
96
A ++ A ++
97
A ++ B ++
98
A ++ A ++
99
A ++ A ++
100
B ++ B ++
101
B ++ B ++
102
B + B ++
103
B ++ B ++
104
B ++ B ++
105
B ++ B ++
106
A ++ A ++
107
B ++ B ++
108
A ++ A ++
109
A ++ A ++
110
A ++ A ++
111
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
112
A ++ A ++
113
A ++ A ++
114
A ++ A ++
115
A ++ A ++
116
A ++ A ++
117
A ++ A ++
118
B ++ B ++
119
A ++ A ++
120
A ++ A ++
121
A ++ A ++
122
B ++ B ++
123
B ++ A ++
124
B + B ++
125
B ++ B ++
126
B ++ A ++
127
B + B +
128
B ++ B ++
129
B ++ A ++
130
B ++ B ++
131
B ++ B ++
131
B + B +
133
B ++ B ++
134
B + B +
135
A + B ++
136
B + B ++
137
B + B ++
138
B + B ++
139
B ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
140
B ++ A ++
141
A ++ A ++
142
A ++ A ++
143
B ++ B ++
144
B ++ B ++
145
B ++ B ++
146
B ++ B ++
147
A ++ A ++
148
B ++ B ++
149
B + B ++
150
B + B ++
151
A ++ A ++
152
B + B ++
153
A ++ A ++
154
A ++ A ++
155
A ++ A ++
156
B ++ B ++
157
A ++ A ++
158
A ++ A ++
159
B ++ B ++
160
A ++ A ++
161
A ++ A ++
162
A ++ A ++
163
A ++ A ++
164
A ++ A ++
165
A ++ A ++
166
A ++ A ++
167
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
168
B ++ B ++
169
A ++ A ++
170
A ++ A ++
171
A + A ++
172
A + B ++
173
A +
174
A +
175
A + A ++
176
A ++ A ++
177
A ++ A ++
178
A ++ A ++
179
A ++ A ++
180
A ++ A ++
181
B ++ A ++
182
B ++ A ++
183
A ++ A ++
184
A ++ A ++
185
B ++ A ++
186
B + B ++
187
A ++ A ++
188
A ++ A ++
189
B ++ B ++
190
B ++ B ++
191
A ++ A ++
192
B ++ B ++
193
A + B ++
194
A + A ++
195
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
196
A + A ++
197
A ++ A ++
198
A ++ A ++
199
A ++ A ++
200
A ++ A ++
201
A ++ A ++
202
A ++ A ++
203
A ++ A ++
204
A ++ A ++
205
A ++ A ++
206
A ++ A ++
207
A ++ A ++
208
B + B ++
209
A ++ A ++
210
A ++ A ++
211
A ++ A ++
212
B ++ B ++
213
B + B ++
214
A ++ A ++
215
A ++ A ++
216
A ++ A ++
217
B ++ B ++
218
B ++ B ++
219
B ++ B ++
220
B + B +
221
B + B +
222
A ++ A ++
223
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
224
A ++ A ++
225
B ++ B ++
226
A ++ A ++
227
A ++ A ++
228
B + B +
229
B ++ B ++
230
A ++ A ++
231
A ++ A ++
232
A ++ A ++
233
A ++ A ++
234
A ++ A ++
235
A ++ A ++
236
A ++ A ++
237
A ++ A ++
238
B ++ B ++
239
A ++ A ++
240
A ++ A ++
241
A ++ A ++
242
A ++ A ++
243
B + B ++
244
A ++ A ++
245
A ++ A ++
246
B + B ++
247
A ++ A ++
248
A ++ A ++
249
B ++ A ++
250
A ++ A ++
251
B ++ B ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
252
B ++ A ++
253
A ++ A ++
254
A ++ A ++
255
A ++ A ++
256
A ++ A ++
257
A ++ A ++
258
B ++ A ++
259
A ++ A ++
260
B + B +
261
A ++ A ++
262
B ++ B ++
263
A ++ A ++
264
B ++ B ++
265
B ++ B ++
266
A ++ A ++
267
A ++ A ++
268
B ++ A ++
269
A ++ A ++
270
B ++ B ++
271
A ++ A ++
272
A ++ A ++
273
A ++ A ++
274
A ++ A ++
275
A ++ A ++
276
A ++ A ++
277
A ++ A ++
278
A ++ A ++
279
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
280
A ++ A ++
281
B ++ A ++
282
A ++ A ++
283
A ++ A ++
284
A ++ A ++
285
A ++ A ++
286
A ++ A ++
287
A ++ A ++
288
B ++ A ++
289
B ++ A ++
290
A ++ A ++
291
A ++ A ++
292
A ++ A ++
293
A ++ A ++
294
A ++ A ++
295
A ++ A ++
296
A ++ A ++
297
A ++ A ++
298
A ++ A ++
299
B ++ A ++
300
B ++ A ++
301
B ++ A ++
302
A ++ A ++
303
B ++ B ++
304
A ++ A ++
305
A ++ A ++
306
A ++ A ++
307
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
308
A ++ A ++
309
A ++ A ++
310
A ++ A ++
311
A ++ A ++
312
A ++ A ++
313
A ++ A ++
314
A ++ A ++
315
A ++ A ++
316
A ++ A ++
317
A ++ A ++
318
B ++ A ++
319
A ++ A ++
320
A ++ A ++
321
A ++ A ++
322
A ++ A ++
323
B ++ A ++
324
A ++ A ++
325
B ++ A ++
326
A ++ A ++
327
B + B +
328
B + B +
329
A ++ A ++
330
A ++ A ++
331
A ++ A ++
332
B ++ B ++
333
A ++ A ++
334
B + A ++
335
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
336
B ++ A ++
337
A ++ A ++
338
B ++ A ++
339
A ++ A ++
340
A ++ A ++
341
A ++ A ++
342
A ++ A ++
343
B ++ B ++
344
B ++ A ++
345
A ++ A ++
346
A ++ A ++
347
B + B +
348
B + B +
349
A ++ A ++
350
B ++ A ++
351
B + B ++
352
B + B ++
353
B + B ++
354
B + B ++
355
A ++ A ++
356
B ++ A ++
357
B ++ B ++
358
A ++ A ++
359
A ++ A ++
360
B ++ B ++
361
A ++ A ++
362
A ++ A ++
363
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
364
A ++ A ++
365
A ++ A ++
366
A ++ A ++
367
A ++ A ++
368
A ++ A ++
369
B ++ A ++
370
A ++ A ++
371
A ++ A ++
372
B ++ A ++
373
A ++ A ++
374
B ++ B ++
375
A ++ A ++
376
A ++ A ++
377
A ++ A ++
378
A ++ A ++
379
A ++ A ++
380
B ++ A ++
381
A ++ A ++
382
A ++ A ++
383
B ++ B ++
384
B ++ B ++
385
B ++ A ++
386
B ++ A ++
387
B ++ A ++
388
B ++ A ++
389
B ++ A ++
390
A ++ A ++
391
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
392
A ++ A ++
393
A ++ A ++
394
B ++ A ++
395
B ++ A ++
396
B ++ B ++
397
A ++ A ++
398
A ++ A ++
399
A ++ A ++
400
A ++ A ++
401
B ++ A ++
402
A ++ A ++
403
A ++ A ++
404
A ++ A ++
405
A ++ A ++
406
A ++ A ++
407
408
A ++ A ++
409
A ++ A ++
410
A ++ A ++
411
A ++ A ++
412
A ++ A ++
413
A ++ A ++
414
A ++ A ++
415
A ++ A ++
416
A ++ A ++
417
A ++ A ++
418
A ++ A ++
419
A ++ A ++
Compuesto
Ensayo de viabilidad de MCF7 ER–α en ensayo Western de células (SP1)
IC50
Respuesta máxima IC50 Respuesta máxima
420
A ++ A ++
421
A ++ A ++
422
A ++ A ++
423
A ++ A ++
424
B ++ A ++
425
A ++ A ++
426
A ++ A ++
427
A ++ A ++
428
A ++ A ++
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A ++ A ++
430
A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A ++ A ++
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A + A ++
441
A + A ++
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A ++ A ++
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A ++ A ++
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B ++ A ++
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A ++ A ++
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A ++ A ++
447
A ++ A ++
imagen352
imagen353
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imagen358

Claims (1)

  1. imagen1
    imagen2
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    imagen5
    imagen6
    imagen7
    imagen8
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    imagen10
    imagen11
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