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AR044506A1 - Inhibidores ciclicos de la proteina tirosina cinasa - Google Patents

Inhibidores ciclicos de la proteina tirosina cinasa

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Publication number
AR044506A1
AR044506A1 ARP040100964A ARP040100964A AR044506A1 AR 044506 A1 AR044506 A1 AR 044506A1 AR P040100964 A ARP040100964 A AR P040100964A AR P040100964 A ARP040100964 A AR P040100964A AR 044506 A1 AR044506 A1 AR 044506A1
Authority
AR
Argentina
Prior art keywords
alkyl
hydrogen
aryl
compound
formula
Prior art date
Application number
ARP040100964A
Other languages
English (en)
Inventor
Joel Barrish
Ramesh Padmanabha
Jagabandhu Das
Ping Chen
Derek J Norris
Aarthur M P Doweyko
John Wityak
Francis Y F Lee
Louis J Lombardo
Original Assignee
Bristol Myers Squibb Co
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=33096777&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR044506(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of AR044506A1 publication Critical patent/AR044506A1/es

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Abstract

Un compuesto cíclico de la siguiente fórmula (1) o una sal del mismo, en donde Q es: (1) un anillo de 5 miembros heteroarilo de 5 miembros; (2) un anillo heteroarilo de 6 miembros; o (3) un anillo arilo opcionalmente substituido con uno o más grupos R1; Z es: (1) un anillo simple; (2) -R15C=CH-; o (3) -(CH2)m-, en donde m es 1 hasta 2; X1 y X2 cada uno son hidrógeno, o de manera conjunta forman =O o =S; R1 es: (1) hidrógeno o R6, donde R6 es alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, cicloalquenilalquilo, arilo, aralquilo, heterociclo, o heterocicloalquilo, cada uno de los cuales está substituido o no substituido con Z1, Z2 y uno o más grupos Z3; (2) -OH o -OR6; (3) -SH o -SR6; (4) -C(O)2H, C(O)qR62 o O-C(O)qR6,en donde q es 1 o 2; (5) -SO3H ó -S(O)qR6; (6) halo; (7) ciano; (8) nitro; (9) -Z4-NR7R8; (10) -Z4-N(R9)-Z6-R10R11; (11) -Z4-N(R12)-Z5-R6; (12) -P(O)(OR6)2; R2 y R3 son cada uno independientemente: (1) hidrógeno o R6; (2) -Z4- R6; o (3) -Z13-NR7R8; R4 y R5: (1) son cada uno independientemente: hidrógeno o R6; (2) -Z4-N(R9)-Z5-NR10R11; (3) -N(R9)Z4R6; o (4) junto con el átomo de nitrógeno al cual se anexa, completa un anillo heterocíclico saturado o no saturado de 3 hasta 8 miembros que está substituido o no substituido con Z1, Z2 y Z3, cuyo anillo heterocíclico puede fusionar opcionalmente al anillo de benceno mismo, que está substituido o no substituido con Z1, Z2 y Z3; R7,R8, R9, R10, R11 y R12: (1) cada uno son independientemente: hidrógeno o R6; (2) R7 y R8 pueden ser de manera conjunta alquileno, alquenileno o heteroalquilo, completando un anillo de 3 hasta 8 miembros saturado o no saturado con el átomo de nitrógeno al cual está anexado, cuyo anillo está substituido o no substituido con Z1, Z2 y Z3; o (3) dos cualquiera de R9, R10 y R11 pueden ser de manera conjunta alquileno o alquenileno completando un anillo de 3 hasta 8 miembros saturado o no saturado junto con los átomos de nitrógeno al cual están anexos, cuyo anillo está substituido o no substituido con Z1, Z2 y Z3; R13 es: (1) ciano; (2) nitro; (3) -NH2; (4) -NHOalquilo; (5) -OH; (6) -NHOarilo; (7) -NHCOOalquilo; (8) -NHCOOarilo; (9) -HSO2alquilo; (10) -NHSO2arilo; (11) arilo; (12) heteroarilo; (13) -Oalquilo; o (14) -Oarilo; R14 es: (1) -NO2; (2) -COOalquilo; o (3) -COOarilo; R15 es: (1) hidrógeno; (2) alquilo; (3) arilo; (4) arilalquilo; o (5) cicloalquilo; Z1,Z2 y Z3 son cada uno independientemente: (1) hidrógeno o Z6, en donde Z6 es (i) alquilo, alquenilo, alquinilo, cicloalquilo, cicloalquilalquilo, cicloalquenilo, cicloalquenilalquilo, arilo, aralquilo, alquilarilo, cicloalquilarilo, heterociclo, o heterocicloalquilo; (ii) un grupo (i) que en si mismo está substituido por uno o más grupos (i) iguales o diferentes; o (iii) un grupo (i) o (ii) que está substituido por uno o más de los siguientes grupos (2) hasta (16) de la definición de Z1, Z2 y Z3; (2) -OH o -OZ6; (3) -SH o -SZ6; (4) -C(O)qH, -C(O)qZ6, o -O-C(O)qZ6; (5) -SO3H, -S(O)qZ6; o S(O)qN(Z9)Z6; (6) halo; (7) ciano; (8) nitro; (9) -Z4-NZ7Z8; (10) -Z4-N(Z9)-Z5-NZ7Z8; (11) -Z4-N(Z10)-Z5-Z6; (12) -Z4-N(Z10)-Z5-H; (13) oxo; (14) -O-C(O)-Z6; (15) dos cualquiera de Z1, Z2 y Z3 pueden de manera conjunta ser alquileno o alquenileno completando un anillo de 3 hasta 8 miembros saturado o no saturado con los átomos a los cuales se unen; o (16) dos cualquiera de Z1, Z2, y Z3 pueden de manera conjunta ser -O-(CH2)r-O-,en donde r es 1 hasta 5, completando un anillo de 4 hasta 8 miembros, saturado o no saturado junto con los átomos a los cuales se unen; Z4 y Z5 son cada uno independientemente: (1) un enlace sencillo; (2) Z11S(O)qZ12; (3) -Z11-C(O)-Z12-; (4) -Z11-C(S)-Z12-; (5) -Z11-O-Z12-; (6) -Z11-S-Z12-; (7) -Z11-O-C(O)-Z12-; o (8) -Z11-C(O)-O-Z12-; Z7, Z8, Z9 y Z10: (1) son cada uno independientemente: hidrógeno o Z6; (2) Z7 y Z8, o Z6 y Z10, pueden de manera conjunta ser alquileno o alquenileno, completando un anillo de 3 hasta 8 miembros saturado o no saturado junto con los átomos a los cuales está unido, cuyo anillo está substituido o no substituido con Z1, Z2 y Z3; o (3) Z7 o Z8, junto con Z9, pueden ser alquileno o alquenileno completando un anillo de 3 hasta 8 miembros saturado o no saturado junto con los átomos de nitrógeno a los cuales está enlazado, cuyo anillo está substituido o no substituido con Z1, Z2 y Z3; Z11 y Z12 cada uno son independientemente: (1) un enlace sencillo; (2) alquileno; (3) alquenileno; o (4) alquinileno; y Z13 es: (1) un enlace sencillo; (2) -Z11-S(O)q-Z12-; (3) -Z11-C(O)-Z12-; (4) -Z11-C(S)-Z12-; (5) -Z11-O-Z12-; (6) -Z11-S-Z12-; (7) -Z11-O-C(O)-Z12-; (8) -Z11-C(O)-O-Z12-; (9) -C(NR13)-; (10) -C(CHR14)-; o (11) -C(C(R14)2)-. con la condición de que el compuesto sea diferente a (a) un compuesto de la fórmula (2) en donde R1a es alquilo o -C(O)NHNH2; R2a y R3a son independientemente hidrógeno, alquilo, -C(O)-(alq); y R4a es hidrógeno y R5a es arilo, arilo substituido por alquilo, arilo substituido por halo, aralquilo, cicloalquilo o amino; o R4a es alquilo y R5a es alquilo o arilo; o R4a y R5a junto con el átomo de nitrógeno al cual se unen forman morfolino. (b) un compuesto de la fórmula (3) o (4) en donde X es oxígeno o azufre; R1b es hidrógeno, halógeno, alquilo o haloalquilo, R2b es hidrógeno, alquilo, arilo, aralquilo, heterociclo, heterocicloalquilo R3b es alquilo, arilo, aralquilo, heterociclo, heterocicloalquilo R4b es hidrógeno, alquilo, o aralquilo; y R5b es hidrógeno, alquilo, arilo, aralquilo, heterociclo o heterocicloalquilo (c) un compuesto de la fórmula (5) donde R4d y R5d son independientemente hidrógeno, alquilo, alquenilo, o fenilo; R27 es hidrógeno o alquilo; (d) un compuesto de la fórmula (6) en donde R3e es fenilo, piridilo o pirimidinilo opcionalmente substituido con halógeno o alquilo; R50 y R51 son cada uno independientemente hidrógeno, halógeno o alquilo; R52 y R53 son cada uno independientemente hidrógeno, halógeno, alquilo o haloalquilo; R54 y R56 son cada uno independientemente hidrógeno, halógeno, alquilo, nitro o amino; R55 es hidrógeno, halógeno, alquilo, haloalquilo, alcoxi, haloalcoxi, alquiltio, haloalquiltio, o alcoxicarbonilo; y n es cero o 1. (e) un compuesto de la fórmula (7) en donde R2f y R3f son independientemente: hidrógeno o alquilo R4f es hidrógeno o alquilo; y R5f es alquilo, cicloalquilo, arilo, arilo substituido con alquilo, arilo substituido con haloalquilo, arilo substituido con halo, arilo substituido con alcoxi, arilo substituido con nitro, arilo substituido con arilo, aralquilo, o heteroarilo; o R4f y R5f junto con el átomo de nitrógeno al cual se enlazan forman un anillo morfolino (f) un compuesto de la fórmula (8) en donde R2g es H o -N=O; R3g es H o alquilo; R4g es H o alquilo; y R5g es alquilo, arilo, o aralquilo; (g) un compuesto de la fórmula (9) en donde R1h es alquilo o haloalquilo; y R57 es alquilo, alcoxi, alquenilo, aqueniloxi, alquinilo, alquiniloxi, cicloalquilo, cicloaquenilo, cicloalcoxi, cicloalqueniloxi, o fenilo (h) un compuesto de la fórmula (10) en donde R2i es hidrógeno o alquilo; R3i es -C(O)-NH-(alq); y R58 y R59 son independientemente hidrógeno, alquilo o halógeno. (i) un compuesto de la fórmula (11) en donde R5, es alquinilo; y R61 y R62 son independientemente alcoxi o haloalcoxi. (j) un compuesto de la fórmula (12) en donde R1k es hidrógeno, alquilo, arilo o aralquilo; R1k es alquilo, arilo o aralquilo; R3k y R5k son independientemente alquilo, arilo o aralquilo; (k) un compuesto de la fórmula (13) en donde R2m es hidrógeno o alquilo; y R3m es el radical de una materia colorante de antraquinona, ftalocianina, formazan, nitroarilo, dioxazina, fenazina o estilbeno; (l) un compuesto de la fórmula (14) en donde R1n es aralquilo o -(alq)C(O)-(arilo); R2n es hidrógeno, alquilo, alquenilo, hidroxialquilo; y R3n es aralquilo (m) un compuesto de la fórmula (15) en donde R2p y R3p son independientemente hidrógeno, alquilo, alquenilo, alcoxi, -CHO, -C(O)-(alq), -COO-(alq), -(alquil)-COO-(alq), alquiltioalquilo, o arilo; y R5p es fenilo opcionalmente substituido. (n) un compuesto de la fórmula (16), (17) o (18) en donde X es oxígeno o azufre; R2q es hidrógeno R3q es fenilo opcionalmente substituido; R4q es hidrógeno; R5q es fenilo opcionalmente substituido; R2r y R3r son cada uno independientemente hidrógeno, alquilo, o aralquilo; R4r es hidrógeno; y R5r es fenilo opcionalmente substituido; (o) un compuesto de la fórmula (19) en donde X es oxígeno o azufre, R2s es hidrógeno; R3s es fenilo opcionalmente substituido; R4s es hidrógeno; y R5s es fenilo opcionalmente substituido; (p) un compuesto del grupo de fórmulas (20); (q) un compuesto del grupo de fórmulas (21); (r) el compuesto de fórmula (22). Composición farmacéutica que comprende al compuesto cíclico de fórmula (1). Estos compuestos son útiles para tratar desórdenes asociados con la proteína tirosina cinasa, tal como el cáncer.
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FI1610780T4 (fi) 2023-02-16
EP1610780B2 (en) 2022-11-23
RS20050698A (sr) 2008-04-04
US7125875B2 (en) 2006-10-24
IL170873A (en) 2011-04-28
TWI351404B (en) 2011-11-01
SI1610780T2 (sl) 2023-01-31
CN1989969A (zh) 2007-07-04
UA87456C2 (uk) 2009-07-27
RU2365372C2 (ru) 2009-08-27
MXPA05010145A (es) 2005-11-16
SI1610780T1 (sl) 2010-11-30
HK1078491A1 (en) 2006-03-17
CN1764454A (zh) 2006-04-26
TW200510403A (en) 2005-03-16
ES2342937T5 (es) 2023-04-19
PE20041068A1 (es) 2005-01-21
MY139730A (en) 2009-10-30
CA2519898C (en) 2012-07-10
AU2004223828B2 (en) 2008-07-03
US20040054186A1 (en) 2004-03-18
EP1610780B1 (en) 2010-04-21
DE602004026703D1 (de) 2010-06-02
EP1610780A2 (en) 2006-01-04
AU2004223828A1 (en) 2004-10-07
KR20050115305A (ko) 2005-12-07

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