ES2647664T3 - Compuestos de indol o análogos de los mismos útiles para el tratamiento de la degeneración macular relacionada con la edad (AMD) - Google Patents

Compuestos de indol o análogos de los mismos útiles para el tratamiento de la degeneración macular relacionada con la edad (AMD) Download PDF

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ES2647664T3
ES2647664T3 ES12700094.1T ES12700094T ES2647664T3 ES 2647664 T3 ES2647664 T3 ES 2647664T3 ES 12700094 T ES12700094 T ES 12700094T ES 2647664 T3 ES2647664 T3 ES 2647664T3
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carbon atoms
alkyl
alkoxy
atoms
hydrogen
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Eva Altmann
Ulrich Hommel
Edwige Liliane Jeanne Lorthiois
Juergen Klaus Maibaum
Nils Ostermann
Jean Quancard
Stefan Andreas Randl
Oliver Simic
Anna Vulpetti
Olivier Rogel
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Novartis AG
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Abstract

Un compuesto de la fórmula I: **Fórmula** o una sal farmacéuticamente aceptable del mismo, en donde: Z1 es C, y L es un residuo divalente seleccionado a partir del grupo que consiste en -N(H)- y -C(H)-(R1)-, o Z1 es N, y L es CH2; R1 es hidrógeno, hidroxilo, o amino; Z2 es C(R2) o N; Z3 es C o N, Z4 es C(R4) o N; Z5 es C(R5) o N, o un N-óxido del mismo; Z6 es C(R6) o N, o un N-óxido del mismo; Z7 es C(R7) o N, o un N-óxido del mismo; Z8 es C o N; Z9 es C o N; en donde uno de Z1, Z3, Z8 y Z9 es N, y tres de Z1, Z3, Z8 y Z9 son C; en donde 0, 1 o 2 o 3 de Z2, Z4, Z5, Z6 y Z7 son N; R2 es hidrógeno o alquilo de 1 a 6 átomos de carbono; R3 se selecciona a partir del grupo que consiste en hidrógeno, alquilo de 1 a 4 átomos de carbono, hidroxi- alquilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono-alquilo de 1 a 4 átomos de carbono, halo-alquilo de 1 a 4 átomos de carbono, amino, o metil-amino; R4 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, y alquilo de 1 a 6 átomos de carbono; R5 y R6 se seleccionan independientemente a partir del grupo que consiste en hidrógeno, halógeno, hidroxilo, NR8R9, ciano, CO2H, CONR10R11, SO2alquilo de 1 a 6 átomos de carbono, SO2NH2, SO2NR10R11, alcoxilo de 1 a 6 átomos de carbono-carbonilo, -C(NR10)NR8R9, alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alquenilo de 2 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, halo-alcoxilo de 1 a 6 átomos de carbono, y alqueniloxilo de 2 a 6 átomos de carbono, en donde cada alquilo, alquenilo, alcoxilo y alqueniloxilo está insustituido o sustituido con hasta 4 sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, ciano, tetrazol, alcoxilo de 1 a 4 átomos de carbono, halo- alcoxilo de 1 a 4 átomos de carbono, CO2H, alcoxilo de 1 a 6 átomos de carbono-carbonilo, C(O)NR10R11, NR8R9, fenilo opcionalmente sustituido, heterociclo opcionalmente sustituido que tiene de 4 a 7 átomos del anillo y 1, 2, o 3 heteroátomos del anillo seleccionados a partir de N, O o S, heteroarilo opcionalmente sustituido que tiene 5 o 6 átomos del anillo y 1, 2 o 3 heteroátomos del anillo seleccionados a partir de N, O o S, y en donde los sustituyentes opcionales de fenilo, heterociclo o heteroarilo se seleccionan a partir de halógeno, hidroxilo, alquilo de 1 a 4 átomos de carbono, alcoxilo de 1 a 4 átomos de carbono, y CO2H; R5 y R6, tomados en combinación con los átomos con los que están unidos, forman un ciclo que tiene de 4 a 7 átomos del anillo y 0, 1 o 2 átomos de N, O o S adicionales del anillo; R7 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, halo-alcoxilo de 1 a 6 átomos de carbono alcoxilo de 1 a 6 átomos de carbono-carbonilo, CO2H y C(O)NR10R11; R8 y R9 se seleccionan independientemente a partir del grupo que consiste en hidrógeno, y alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono-alquilo de 1 a 6 átomos de carbono, hidroxi-alquilo de 1 a 6 átomos de carbono, o NR8R9, tomados en combinación, forman un heterociclo que tiene de 4 a 7 átomos del anillo y 0 o 1 átomo de N, O o S adicional del anillo, cuyo heterociclo está sustituido con 0, 1 o 2 sustituyentes seleccionados independientemente a partir del grupo que consiste en alquilo de 1 a 4 átomos de carbono, halógeno, hidroxilo, alcoxilo de 1 a 4 átomos de carbono; R10 y R11 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrógeno y alquilo de 1 a 6 átomos de carbono, halo-alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono- alquilo de 1 a 6 átomos de carbono, o hidroxi-alquilo de 1 a 6 átomos de carbono; X1 es CR14R15 o azufre; X2 es CR16R17, oxígeno, azufre, N(H) o N(alquilo de 1 a 6 átomos de carbono), en donde al menos uno de X1 y X2 es carbono; o X1 y X2, en combinación, forman una olefina de la fórmula -C(R16)>=C(H)- o -C(R16)>=C(alquilo de 1 a 4 átomos de carbono)-, en donde el C(R16) está unido a X3; X3 es (CR18R19)m o N(H), en donde m es 0, 1 o 2, en donde X3 es CR18R19 o (CR18R19)2 cuando cualquiera de X1 o X2 es azufre o X2 es oxígeno; o X2 y X3, tomados en combinación, son -N>=C(H)- o -N>=C(alquilo de 1 a 4 átomos de carbono)-, en donde el C(H) o C(alquilo de 1 a 4 átomos de carbono) está unido a X1;
ES12700094.1T 2011-01-04 2012-01-02 Compuestos de indol o análogos de los mismos útiles para el tratamiento de la degeneración macular relacionada con la edad (AMD) Active ES2647664T3 (es)

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US201161429730P 2011-01-04 2011-01-04
US201161429730P 2011-01-04
PCT/EP2012/050005 WO2012093101A1 (en) 2011-01-04 2012-01-02 Indole compounds or analogues thereof useful for the treatment of age-related macular degeneration (amd)

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US (1) US9085555B2 (es)
EP (1) EP2661433B1 (es)
JP (1) JP5921572B2 (es)
KR (1) KR20140027090A (es)
CN (1) CN103402996B (es)
AP (1) AP2013006986A0 (es)
AR (1) AR084768A1 (es)
AU (1) AU2012204920B2 (es)
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CA (1) CA2823665A1 (es)
CL (1) CL2013001891A1 (es)
CO (1) CO6791608A2 (es)
CR (1) CR20130333A (es)
CU (1) CU20130094A7 (es)
EA (1) EA023259B1 (es)
ES (1) ES2647664T3 (es)
GT (1) GT201300174A (es)
MA (1) MA34837B1 (es)
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AU2012204920B2 (en) 2014-08-07
US20120295884A1 (en) 2012-11-22
CR20130333A (es) 2013-09-04
CN103402996B (zh) 2015-02-11
ZA201304684B (en) 2014-03-26
GT201300174A (es) 2014-06-06
UY33858A (es) 2012-08-31
JP2014506877A (ja) 2014-03-20
KR20140027090A (ko) 2014-03-06
PE20140471A1 (es) 2014-04-13
EA023259B1 (ru) 2016-05-31
AR084768A1 (es) 2013-06-26
EP2661433A1 (en) 2013-11-13
AU2012204920A1 (en) 2013-07-18
TN2013000275A1 (en) 2014-11-10
CA2823665A1 (en) 2012-07-12
CN103402996A (zh) 2013-11-20
MA34837B1 (fr) 2014-01-02
CL2013001891A1 (es) 2014-09-05
AP2013006986A0 (en) 2013-07-31
SG191844A1 (en) 2013-08-30
BR112013017316A2 (pt) 2019-09-24
PL2661433T3 (pl) 2018-01-31
CU20130094A7 (es) 2013-10-29
MX2013007867A (es) 2013-07-17
PT2661433T (pt) 2017-10-24
NZ612899A (en) 2015-07-31
EP2661433B1 (en) 2017-08-16
CO6791608A2 (es) 2013-11-14
JP5921572B2 (ja) 2016-05-24
MX347391B (es) 2017-04-25
US9085555B2 (en) 2015-07-21
EA201391000A1 (ru) 2013-12-30
TW201242959A (en) 2012-11-01

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