AR039563A1 - Derivados de 4-(imidazol-5-il)-2-(4-sulfoanilino)pirimidina con actividad inhibidora de cdk - Google Patents
Derivados de 4-(imidazol-5-il)-2-(4-sulfoanilino)pirimidina con actividad inhibidora de cdkInfo
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- AR039563A1 AR039563A1 ARP030100799A ARP030100799A AR039563A1 AR 039563 A1 AR039563 A1 AR 039563A1 AR P030100799 A ARP030100799 A AR P030100799A AR P030100799 A ARP030100799 A AR P030100799A AR 039563 A1 AR039563 A1 AR 039563A1
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- alkyl
- ethyl
- heterocyclyl
- hydrogen
- optionally substituted
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Abstract
Derivados de 4-(imidazol-5-il)-2-(4-sulfoanilino)pirimidina y su uso como medicamentos, particularmente medicamentos para producir un efecto inhibidor del ciclo celular (anti-proliferación celular) en un animal de sangre caliente, por ejemplo un ser humano. Reivindicación 1: Un compuesto de la fórmula (2), (3), (4), (5), (6) y (7) de la estructura genérica de fórmula (1), donde: i) un compuesto de fórmula (2), donde: R1 es 2-(pirazolil-1-il)etilo, 3-(isoxazol-3-iloxi)propilo, 2-(isotiazol-3-iloxi)etilo, 2-(tiadiazol-3-iloxi)etilo, 1,3-dihidroxiprop-2-ilo, 1-metil-1-hidroximetiletilo, 1,1-dimetilpropilo, 1-metilciclopropilo, t-butilo, 2-morfolino-1,1-dimetiletilo, 2-pirrolidin-1-il-1,1-dimetiletilo, 2-metiltio-1,1-dimetiletilo, 1,3-dimetoxiprop-2-ilo, 1-metoxiprop-2-ilo, 1-hidroxiprop-2-ilo, 1-etoxiprop-2-ilo, 1-propoxiprop-2-ilo, etoxietilo o 2-metoxi-1,1-dimetiletilo; y R2 es hidrógeno; o R1 y R2 juntos forman 2,2-dimetilaziridin-1-ilo; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo; ii) un compuesto de fórmula (3) donde: R1 es pirid-2-ilmetilo, 2-(2-metil-1,2,4-triazol-5-il)etilo, 2-pirid-2-iletilo, 2-piridazin-3-iletilo, 2-(3,5-dimetiltriazol-4-il)etilo, 2-pirid-3-iletilo, 2-metoxietilo, 3-(5-metilpirazol-4-il)propilo, 2-trifluorometilpirid-5-ilmetilo, 2-piridazin-4-iletilo, 1,1-dimetilprop-2-inilo, 2-etoxietilo, 2-fenoxietilo, 2-(4-metoxifenoxi)etilo, 2-(2-metoxifenoxi)etilo, 2-(viniloxi)etilo, 2-(isopropoxi)etilo y 2-(propoxi)etilo; y R2 es hidrógeno o ciano; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo; con la salvedad de que cuando R1 es 2-metoxietilo, R2 es ciano; iii) un compuesto de fórmula (4), donde: R1 es hidrógeno, heterociclilo, alquilo C1-6 o alcoxi C1-6alquilo C1-6; donde R1 puede ser opcionalmente substituido sobre carbono por uno o más hidroxi, carboxi, alcoxi C1-6, alcoxicarbonilo C1-6, N,N-(alquil C1-6)2amino, heterociclilo, cicloalquilo C3-6 y alcoxi C1-6alcoxi C1-6; y donde si un heterociclilo contiene una porción -NH-, ese nitrógeno puede ser opcionalmente substituido por alquilo C1-6 o bencilo; R2 es hidrógeno, halo o ciano; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo ; con la salvedad de que cuando R1 es 2-metoxietilo, ciclopropilmetilo o pirid-2-ilmetilo, R2 no es hidrógeno; iv) un compuesto de fórmula (5), donde: R1 es hidrógeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, cicloalquil C3-6alquilo C1-3, un heterociclilo o heterociclilalquilo C1-3; donde R1 puede ser opcionalmente substituido sobre carbono por uno o más metilo, etilo, metoxi, etoxi, propoxi, trifluorometilo, trifluorometoxi, 2,2,2-trifluoroetoxi o ciclopropilmetoxi; y donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede ser opcionalmente substituido por uno o más metilo, etilo, acetilo, 2,2,2-trifluoroetilo o metoxietilo; R2 es hidrógeno, halo o ciano; R3 es alquilo C2-6; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo; v) un compuesto de fórmula (6), donde: R1 es hidrógeno, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3, un heterociclilo o heterociclilalquilo C1-3; donde R1 puede ser opcionalmente substituido sobre carbono por uno o más metilo, etilo, metoxi, etoxi, propoxi, trifluorometilo, trifluorometoxi, 2,2,2-trifluoroetoxi o ciclopropilmetoxi; y donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede ser opcionalmente substituido por uno o más metilo, etilo, acetilo, 2,2,2-trifluoroetilo o metoxietilo; R2 es halo, ciano, alquilo C1-3 o alcoxi C1-3; p es 1-2; donde los valores de R2 pueden ser iguales o diferentes; R3 es hidrógeno, halo o ciano; R4 es alquilo C1-4; R5 es alquilo C1-6 o alquenilo C2-6; donde R5 puede ser opcionalmente substituido sobre carbono por uno o más metoxi, etoxi, propoxi, trifluorometilo, trifluorometoxi, 2,2, 2-trifluoroetoxi o ciclopropilmetoxi; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo; con la salvedad que dicho compuesto no es 4-(1,2-dimetilimidazol-5-il)-2-[2-metoxi-4-(N-metilsulfamoil)-5-metilanilino]pirimidina; vi) un compuesto de fórmula (7), donde: R1 es alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, cicloalquil C3-6alquilo C1-3, un heterociclilo o heterociclilalquilo C1-3; donde R1 puede ser opcionalmente substituido sobre carbono por uno o más metilo, etilo, metoxi, etoxi, propoxi, trifluorometilo, trifluorometoxi, dimetilamino, 2,2,2-trifluoroetoxi, fenil o ciclopropilmetoxi; y donde si dicho heterociclilo contiene una porción -NH- es nitrógeno puede ser opcionalmente substituido por uno o más metilo, etilo, acetilo, 2,2,2-trifluoroetilo o metoxietilo; R2 es halo, ciano, alquilo C1-3 o alcoxi C1-3; p es 0-2; donde los valores de R2 pueden ser iguales o diferentes; R3 es hidrógeno, halo o ciano; R4 es alquilo C2-6; R5 es alquilo C1-6 o alquenilo C2-6; donde R5 puede ser opcionalmente substituido sobre carbono por uno o más metoxi, etoxi, propoxi, trifluorometil, trifluorometoxi, 2,2,2-trifluoroetoxi o ciclopropilmetoxi; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo; vii) un compuesto de fórmula (8), donde: R1 es alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6, cicloalquil C3-6alquilo C1-3, un heterociclilo o heterociclilalquilo C1-3; donde R1 puede ser opcionalmente substituido sobre carbono por uno o más metilo, etilo, metoxi, etoxi, propoxi, trifluorometilo, trifluorometoxi, dimetilamino, 2,2,2-trifluoroetoxi, fenilo o ciclopropilmetoxi; y donde si dicho heterociclilo contiene una porción -NH- ese nitrógeno puede ser opcionalmente substituido por uno o más metilo, etilo, acetilo, 2,2,2-trifluoroetilo o metoxietilo; R2 es halo, ciano, alquilo C1-3 o alcoxi C1-3; p es 0-2; donde los valores de R2 pueden ser iguales o diferentes; R3 es hidrógeno, halo o ciano; R4 es n-propilo o alquilo C4-6; o una sal aceptable para uso farmacéutico o un éster hidrolizable in vivo del mismo.
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Application Number | Priority Date | Filing Date | Title |
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GBGB0205693.5A GB0205693D0 (en) | 2002-03-09 | 2002-03-09 | Chemical compounds |
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AR039563A1 true AR039563A1 (es) | 2005-02-23 |
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ARP030100799A AR039563A1 (es) | 2002-03-09 | 2003-03-07 | Derivados de 4-(imidazol-5-il)-2-(4-sulfoanilino)pirimidina con actividad inhibidora de cdk |
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US (1) | US7465728B2 (es) |
EP (1) | EP1487823A1 (es) |
JP (2) | JP3569524B1 (es) |
KR (1) | KR20040091114A (es) |
CN (1) | CN1649863A (es) |
AR (1) | AR039563A1 (es) |
AU (1) | AU2003214394A1 (es) |
BR (1) | BR0308212A (es) |
CA (1) | CA2478701A1 (es) |
GB (1) | GB0205693D0 (es) |
IL (1) | IL163910A0 (es) |
IS (1) | IS7439A (es) |
MX (1) | MXPA04008807A (es) |
NO (1) | NO20043851L (es) |
PL (1) | PL372703A1 (es) |
RU (1) | RU2004130440A (es) |
TW (1) | TW200306838A (es) |
UA (1) | UA78292C2 (es) |
UY (1) | UY27705A1 (es) |
WO (1) | WO2003076436A1 (es) |
ZA (1) | ZA200406937B (es) |
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GB0004887D0 (en) | 2000-03-01 | 2000-04-19 | Astrazeneca Uk Ltd | Chemical compounds |
GB0113041D0 (en) | 2001-05-30 | 2001-07-18 | Astrazeneca Ab | Chemical compounds |
GB0205690D0 (en) | 2002-03-09 | 2002-04-24 | Astrazeneca Ab | Chemical compounds |
AU2003208479A1 (en) | 2002-03-09 | 2003-09-22 | Astrazeneca Ab | 4- imidazolyl substuited pyrimidine derivatives with cdk inhibitiory activity |
GB0311274D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
GB0311276D0 (en) | 2003-05-16 | 2003-06-18 | Astrazeneca Ab | Chemical compounds |
TW200528101A (en) | 2004-02-03 | 2005-09-01 | Astrazeneca Ab | Chemical compounds |
GB0504753D0 (en) * | 2005-03-08 | 2005-04-13 | Astrazeneca Ab | Chemical compounds |
KR20080033450A (ko) | 2005-07-30 | 2008-04-16 | 아스트라제네카 아베 | 증식성 질환의 치료에 사용하기 위한 이미다졸릴-피리미딘화합물 |
CA2619731A1 (en) * | 2005-08-23 | 2007-03-01 | Ube Industries, Ltd. | Process for preparing 1-substituted 5-acylimidazole compounds |
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KR20040091114A (ko) | 2004-10-27 |
RU2004130440A (ru) | 2005-05-10 |
ZA200406937B (en) | 2006-02-22 |
TW200306838A (en) | 2003-12-01 |
UY27705A1 (es) | 2003-10-31 |
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US20050131000A1 (en) | 2005-06-16 |
CN1649863A (zh) | 2005-08-03 |
IS7439A (is) | 2004-09-07 |
US7465728B2 (en) | 2008-12-16 |
PL372703A1 (en) | 2005-07-25 |
UA78292C2 (en) | 2007-03-15 |
JP2004256550A (ja) | 2004-09-16 |
JP3569524B1 (ja) | 2004-09-22 |
JP2005519135A (ja) | 2005-06-30 |
AU2003214394A1 (en) | 2003-09-22 |
BR0308212A (pt) | 2004-12-21 |
CA2478701A1 (en) | 2003-09-18 |
IL163910A0 (en) | 2005-12-18 |
NO20043851L (no) | 2004-09-14 |
EP1487823A1 (en) | 2004-12-22 |
GB0205693D0 (en) | 2002-04-24 |
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