AR080945A1 - Pirimidinil y 1,3,5-triazinil benzimidazoles y su uso en la terapia contra el cancer - Google Patents
Pirimidinil y 1,3,5-triazinil benzimidazoles y su uso en la terapia contra el cancerInfo
- Publication number
- AR080945A1 AR080945A1 ARP100102428A ARP100102428A AR080945A1 AR 080945 A1 AR080945 A1 AR 080945A1 AR P100102428 A ARP100102428 A AR P100102428A AR P100102428 A ARP100102428 A AR P100102428A AR 080945 A1 AR080945 A1 AR 080945A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- independently
- nr1br1c
- nrfrg
- nrbrc
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- 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
- C07D401/14—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 three or more hetero rings
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- 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
- C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
Abstract
Composiciones farmacéuticas y usos. Reivindicacion 1: Un compuesto de la formula (1), (2) o (3), o un enantiomero, una mezcla de enantiomeros, o una mezcla de dos o más diastereomeros de éstos; o una sal, solvato, hidrato o profármaco farmacéuticamente aceptable de aquél; en donde cada R1 es, independientemente, hidrogeno, alquilo C1-6, -S-alquilo C1-6, -S(O)-alquilo C1-6 o -SO2-alquilo C1-6; cada R2 y R3 es, independientemente, (a) hidrogeno, ciano, halo o nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; o (c) -C(O)R1a, -C(O)OR1b, -C(O)NR1bR1c, -C(NRa)NR1bR1c, -OR1a, -OC(O)R1a, -OC(O)OR1a, -OC(O)NR1bR1c, -OC(=NR1a)NR1bR1c, -OS(O)R1a, -OS(O)2R1a, -OS(O)NR1bR1c, -OS(O)2NR1bR1c, -NR1bR1c, -NR1aC(O)R1d, -NR1aC(O)OR1d, -NR1aC(O)NR1bR1c, -NR1aC(=NR1d)NR1bR1c, -NR1aS(O)R1d, -NR1aS(O)2R1d, -NR1aS(O)NR1bR1c, -NR1aS(O)2NR1bR1c, -SR1a, -S(O)R1a, -S(O)2R1a, -S(O)NR1bR1c, o -S(O)2NR1bR1c; cada R4 y R5 es, independientemente, hidrogeno o alquilo C1-6; o R4 y R5 se unen para formar un enlace, alquileno C1-6, heteroalquileno C1-6, alquenileno C2-6 o heteroalquenileno C2-6; cada R6 es, independientemente, arilo C6-14, aralquilo C7-15, heteroarilo o heteroaril-alquilo C1-6; cada U es, independientemente, un enlace, -C(O)-, -C(O)O-, -C(O)NR1a-, -O-, -OC(O)O-, -OC(O)NR1a-, -NR1a-, -NR1aC(O)NR1d-, -NR1aS(O)-, -NR1aS(O)2-, -NR1aS(O)NR1d, -NR1aS(O)2NR1d, -S-, -S(O)- o -S(O)2-; cada X, Y y Z es, independientemente, N o CR7, siempre que al menos 2 de X, Y y Z sean átomos de nitrogeno; donde R7 es hidrogeno o alquilo C1-6; y cada A, B, D y E es, independientemente, un enlace, C, O, N, S, NR9, CR9 o CR9R10, en donde cada R9 y R10 es, independientemente, hidrogeno, halo, alquilo C1-6, alquenilo C2-6 o alquinilo C2-6; en donde los enlaces entre A, B, D y E pueden ser saturados o insaturados; siempre que no más de uno de A, B, D y E sea un enlace; cada R1a, R1b, R1c y R1d es, independientemente, hidrogeno; o alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; siempre que cuando uno de X, Y y Z sea CH, y U sea un enlace, R6 no sea fenilo; y que cuando X, Y y Z sean N, y R6 sea arilo C6-14o heteroarilo, entonces U no sea un enlace; en donde cada alquilo, alquileno, heteroalquileno, alquenilo, alquenileno, heteroalquenileno, alquinilo, cicloalquilo, arilo, aralquilo, heteroarilo y heterociclilo R1, R2, R3, R4, R5, R6, R7, R9, R10, R1a, R1b, R1c o R1d se sustituye opcionalmente con uno o más de los siguientes y cada uno se selecciona, independientemente, (a) ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo o heterociclilo; cada uno de los cuales también se sustituye opcionalmente con uno o más, en una forma de realizacion, 1, 2, 3 o 4 sustituyentes Q; y (c) -C(O)Ra, -C(O)ORa, -C(O)NRbRc, -C(NRa)NRbRc, -ORa, -OC(O)Ra, -OC(O)ORa, -OC(O)NRbRc, -OC(=NRa)NRbRc, -OS(O)Ra, -OS(O)2Ra, -OS(O)NRbRc, -OS(O)2NRbRc, -NRbRc, -NRaC(O)Rd, -NRaC(O)ORd, -NRaC(O)NRbRc, -NRaC(=NRd)NRbRc, -NRaS(O)Rd, -NRaS(O)NRbRc, -SRa, -S(O)Ra, y -S(O)NRbRc, en donde cada Ra, Rb, Rc y Rd es, independientemente, (i) hidrogeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo, o heterociclilo, cada uno opcionalmente sustituido con uno o más, en una forma de realizacion, 1, 2, 3 o 4 sustituyentes Q; o (iii) Rb y Rc, junto con el átomo N al que están unidos, forman heterociclilo, opcionalmente sustituido con uno o más, en una forma de realizacion, 1, 2, 3 o 4 sustituyentes Q; en donde cada Q se selecciona, independientemente, del grupo que consiste en (a) ciano, halo y nitro; (b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo y heterociclilo; y (c) -C(O)Re, -C(O)ORe, -C(O)NRfRg, -C(NRe)NRfRg, -ORe, -OC(O)Re, -OC(O)ORe, -OC(O)NRfRg, -OC(=NRe)NRfRg, -OS(O)Re, -OS(O)2Re, -OS(O)NRfRg, -OS(O)2NRfRg, -NRfRg, -NReC(O)Rh, -NReC(O)ORh, -NReC(O)NRfRg, -NReC(=NRh)NRfRg, -NReS(O)Rh, -NReS(O)NRfRg, -SRe, -S(O)Re, y -S(O)NRfRg, en donde cada Re, Rf, Rg y Rh es, independientemente, (i) hidrogeno; (ii) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-7, arilo C6-14, aralquilo C7-15, heteroarilo, o heterociclilo; o (iii) Rf y Rg, junto con el átomo N al que están unidos, forman heterociclilo.
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US22368409P | 2009-07-07 | 2009-07-07 | |
US24744809P | 2009-09-30 | 2009-09-30 | |
US31819510P | 2010-03-26 | 2010-03-26 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR080945A1 true AR080945A1 (es) | 2012-05-23 |
Family
ID=42791020
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP100102428A AR080945A1 (es) | 2009-07-07 | 2010-07-06 | Pirimidinil y 1,3,5-triazinil benzimidazoles y su uso en la terapia contra el cancer |
Country Status (8)
Country | Link |
---|---|
US (1) | US8486939B2 (es) |
EP (3) | EP2451802A1 (es) |
AR (1) | AR080945A1 (es) |
CA (2) | CA2767008C (es) |
DK (1) | DK3072890T3 (es) |
ES (1) | ES2706185T3 (es) |
TW (1) | TW201105662A (es) |
WO (1) | WO2011005119A1 (es) |
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-
2010
- 2010-07-06 EP EP10742315A patent/EP2451802A1/en not_active Withdrawn
- 2010-07-06 CA CA2767008A patent/CA2767008C/en active Active
- 2010-07-06 ES ES14168117T patent/ES2706185T3/es active Active
- 2010-07-06 WO PCT/NZ2010/000139 patent/WO2011005119A1/en active Application Filing
- 2010-07-06 DK DK14168117.1T patent/DK3072890T3/en active
- 2010-07-06 EP EP12182995A patent/EP2532659A1/en not_active Withdrawn
- 2010-07-06 EP EP14168117.1A patent/EP3072890B1/en active Active
- 2010-07-06 CA CA2987503A patent/CA2987503C/en active Active
- 2010-07-06 US US12/831,128 patent/US8486939B2/en active Active
- 2010-07-06 AR ARP100102428A patent/AR080945A1/es not_active Application Discontinuation
- 2010-07-06 TW TW099122213A patent/TW201105662A/zh unknown
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CA2767008C (en) | 2018-01-30 |
TW201105662A (en) | 2011-02-16 |
ES2706185T3 (es) | 2019-03-27 |
CA2987503A1 (en) | 2011-01-13 |
DK3072890T3 (en) | 2019-02-11 |
EP3072890A1 (en) | 2016-09-28 |
EP3072890B1 (en) | 2018-10-17 |
CA2987503C (en) | 2019-02-26 |
EP2451802A1 (en) | 2012-05-16 |
WO2011005119A1 (en) | 2011-01-13 |
EP2532659A1 (en) | 2012-12-12 |
US20110009405A1 (en) | 2011-01-13 |
US8486939B2 (en) | 2013-07-16 |
CA2767008A1 (en) | 2011-01-13 |
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