AR045687A1 - Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen - Google Patents
Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienenInfo
- Publication number
- AR045687A1 AR045687A1 ARP040101806A ARP040101806A AR045687A1 AR 045687 A1 AR045687 A1 AR 045687A1 AR P040101806 A ARP040101806 A AR P040101806A AR P040101806 A ARP040101806 A AR P040101806A AR 045687 A1 AR045687 A1 AR 045687A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- optionally substituted
- amino
- alkyloxy
- hydroxy
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/06—Peri-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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/02—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C229/04—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C229/06—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton
- C07C229/10—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings
- C07C229/16—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one amino and one carboxyl group bound to the carbon skeleton the nitrogen atom of the amino group being further bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings to carbon atoms of hydrocarbon radicals substituted by amino or carboxyl groups, e.g. ethylenediamine-tetra-acetic acid, iminodiacetic acids
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
- C07C229/40—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/88—Oxygen atoms
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/93—Sulfur atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
- C07D239/72—Quinazolines; Hydrogenated quinazolines
- C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
- C07D239/94—Nitrogen atoms
Abstract
Proceso de preparación, y composiciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto que posee la fórmula (1), las formas de N-óxidos, las sales de adición farmacéuticamente aceptables y las formas estereoquímicamente isoméricas del mismo, donde Z representa O, CH2, NH o S; en particular Z representa NH; Y representa -alquilo C3-9-, -alquenilo C3-9-, --alquinilo C3-9-, -alquil C3-7-CO-NH- substituido en forma optativa con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-,-alquenil C3-7-CO-NH- opcionalmente substituido con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-, -alquinil C3-7-CO-NH- opcionalmente substituido con amino, mono- o di(alquil C1-4)amino o alquiloxicarbonilamino C1-4-, -alquiloxi C1-5-alquilo C1-5-, -alquil C1-5-NR13-alquilo C1-5-, -alquil C1-5-NR14-CO-alquilo C1-5-,-alquil C1-5-CO-NR15-alquilo C1-5-, -alquil C1-6-CO-NH-, -alquil C1-6-NH-CO-, - alquil C1-3-NH-CS-Het20-,-alquil C1-3-NH-CO-Het20-, alquil C1-2-CO-Het21-CO-, - Het22-CH2-CO-NH-alquilo C1-3-, -CO-NH-alquilo C1-6-, -NH-CO-alquilo C1-6-, -CO-alquilo C1-7-, -alquil C1-7-CO-, -alquil C1-6-CO-alquilo C1-6-, -alquil C1-2-NH-CO-CR16R17-NH-, -alquil C1-2-CO-NH-CR18R19-CO-, -alquil C1-2-CO-NR20-alquil C1-3-CO-, -alquil C1-2-NR21-CH2-CO-NH-alquilo C1-3-, o - alquil-NH-; X1 representa una unión directa, O, -O-alquilo C1-2-, CO, -CO-alquilo C1-2-, NR11, -NR11-alquilo C1-2-, -CH2-, -O-N=CH- o -alquilo C1-2-; X2 representa una unión directa, O, -O-alquilo C1-2-, CO, -CO-alquilo C1-2-, NR12, -NR12-alquilo C1-2-, -CH2-, -O-N=CH- o -alquilo C1-2-; R1 representa hidrógeno, ciano, halo, hidroxi, formilo, alcoxi C1-6-, alquilo C1-6, halofenilcarbonilamino-, alcoxi C1-6- substituido con halo, alquilo C1-4 substituido con uno o cuando sea posible dos o más substituyentes seleccionados de hidroxi o halo; R2 representa hidrógeno, ciano, halo, hidroxi. hidroxicarbonilo-, Het16-carbonilo-, alquiloxicarbonilo C1-4-, alquilcarbonilo C1-4-, aminocarbonilo-, mono- o di(alquil C1-4)aminocarbonilo-, Het1, formilo, alquilo C1-4-, alquinilo C2-6-, cicloalquilo C3-6-, cicloalquiloxi C3-6-, alcoxi C1-6-, Ar5, Ar1-oxi-, dihidroxiborano, alcoxi C1-6- substituido con halo, alquilo C1-4 substituido con uno o cuando sea posible dos o más substituyentes seleccionados de halo, hidroxi o NR5R6, alquilcarbonilo C1-4-, donde dicho alquilo C1-4 está opcionalmente substituido con uno o cuando sea posible dos o más substituyentes seleccionados de hidroxi o alquiloxi C1-4-; R3 representa hidrógeno, alquilo C1-4, o alquilo C1-4 substituido con uno o más substituyentes seleccionados de halo, alquiloxi C1-4-, amino-, mono- o di(alquil C1-4)amino-, alquilsulfonilo C1-4- o fenilo; R4 representa hidrógeno, hidroxi, Ar3-oxi, Ar4-alquiloxi C1-4-, alquiloxi C1-4-, alqueniloxi C2-4- substituidos de manera opcional con Het12 o R4 representa alquiloxi C1-4 substituido con uno o cuando sea posible dos o más substituyentes seleccionados de alquiloxi C1-4-, hidroxi, halo, Het2-, NR7R8, -carbonil-NR9R10 o Het3-carbonilo-; R5 y R6 se selecciona cada uno independientemente de hidrógeno o alquilo C1-4; R7 y R8 se selecciona cada uno independientemente de hidrógeno, alquilo C1-4, Het8, aminosulfonilo-, mono- o di(alquil C1-4)-aminosulfonilo, hidroxi-alquilo C1-4-, alquiloxi C1-4-alquilo C1-4, hidroxicarbonilalquilo C1-4, cicloalquilo C3-6, Het9-carbonilalquilo C1-4, Het10-carbonilo, polihidroxialquilo C1-4, Het11-alquilo C1-4 o Ar2-alquilo C1-4; R9 y R10 se selecciona cada uno de manera independiente de hidrógeno, alquilo C1-4 cicloalquilo C3-6, Het4, hidroxialquilo C1-4, alquiloxi C1-4-alquilo C1-4 o polihidroxialquilo C1-4; R11 representa hidrógeno, alquilo C1-4, Het5, Het6-alquil C1-4-alquenilcarbonilo C2-4, substituido en forma opcional con Het7-alquilaminocarbonilo C1-4, alquenilsulfonilo C2-4, alquiloxi C1-4-alquilo C1-4 o fenilo substituido en forma opcional con uno o cuando sea posible dos o más substituyentes seleccionados de hidrógeno, hidroxi, amino, alquiloxi C1-4; R12 representa hidrógeno, alquilo C1-4, alquiloxi C1-4-carbonilo, Het16-alquilo C1-4, fenilalquiloxicarbonilo C1-4, Het17, alquenilcarbonilo C2-4 substituido de manera opcional con Het19 alquilaminocarbonilo, alquenilsulfonilo C2-4alquiloxi C1-4-alquilo C1-4 o fenilo substituido con uno o cuando sea posible dos o más substituyentes seleccionados de hidrógeno, hidroxi, amino o alquiloxi C1-4; R13 representa hidrógeno, alquilo C1-4, Het13, Het14-alquilo C1-4 o fenilo substituido de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de hidrógeno, hidroxi, amino o alquiloxi C1-4; R14 y R15 se seleccionan de manera independiente de hidrógeno, alquilo C1-4, Het15-alquilo C1-4 o alquiloxi C1-4-alquilo C1-4; R16 y R17 en forma independiente representan hidrógeno o alquilo C1-4 substituido de manera opcional con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amina, imidazoilo o guanidino; R18 y R19 cada uno de manera independiente representa hidrógeno o alquilo C1-4 substituido de manera opcional con fenilo, indolilo, metilsulfuro, hidroxi, tiol, hidroxifenilo, aminocarbonilo, hidroxicarbonilo, amino, imidazoilo o guanidino; R20 y R22 de manera independiente representa cada uno hidrógeno o alquilo C1-4 substituido de manera opcional con hidroxi o alquiloxi C1-4; R21 representa hidrógeno, alquilo C1-4, Het23-alquilcarbonilo C1-4 o R21 representa mono- o di(alquil C1-4)aminoalquil C1-4-carbonilo substituidos de manera opcional con hidroxi, pirimidinilo, dimetilamino o alquiloxi C1-4; Het1 representa un heterociclo seleccionado de piperidinilo, morfolinilo, piperazinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo donde dicho Het1 está substituido de manera opcional con amino, alquilo C1-4, hidroxialquilo, fenilo, fenilalquilo C1-4, alquiloxi C1-4-alquilo C1-4, mono- o di(alquil C1-4)amino- o aminocarbonilo; Het2 representa un heterociclo seleccionado de morfolinilo, piperazinilo, piperidinilo, pirrolidinilo, tiomorfolinilo o ditianilo donde dicho Het2 está substituido de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de hidroxi, halo, amino, alquilo C1-4, hidroxialquilo C1-4-, alquiloxi C1-4alquilo C1-4-, hidroxialquiloxi C1-4-alquilo C1-4-, mono- o di(alquil C1-4)amino-, mono- o di(alquil C1-4)amino-alquilo C1-4-, aminoalquilo C1-4-, mono- o di(alquil C1-4)amino-sulfonilo, aminosulfonilo; Het3, Het4 y Het8 cada uno de manera independiente representa un heterociclo seleccionado de morfolinilo, piperazinilo, piperidinilo, furanilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo donde dicho Het3, Het4 o Het8 están substituidos de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de hidroxi-, amino-, alquilo C1-4, cicloalquil C3-6alquilo C1-4, aminosulfonilo, mono- o di(alquil C1-4)aminosulfonilo o aminoalquilo C1-4; Het5 representa un heterociclo seleccionado de pirrolidinilo o piperidinilo substituido de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo C3-6, hidroxialquilo C1-4, alquiloxi C1-4alquilo C1-4 o polihidroxi-alquilo C1-4; Het6 y Het7 cada uno independientemente representan un heterociclo seleccionado de morfolinilo, pirrolidinilo, piperazinilo o piperidinilo substituido de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo C3-6, hidroxialquilo C1-4-, alquiloxi C1-4alquilo C1-4 o polihidroxialquilo C1-4- ;Het9 y Het10 cada uno independientemente representan un heterociclo seleccionado de furanilo, piperidinilo, morfolinilo, piperazinilo, pirazolilo, dioxolanilo, tiazolilo, oxazolilo, imidazolilo, isoxazolilo, oxadiazolilo, piridinilo o pirrolidinilo donde dichos Het9 o Het10 están substituidos en forma opcional con alquilo C1-4, cicloalquil C3-6alquilo C1-4- o aminoalquilo C1-4; Het11 representa un heterociclo seleccionado de indolilo o de fórmula (2); Het12 representa un heterociclo seleccionado de morfolinilo, piperazinilo, piperidinilo, pirrolidinilo, tiomorfolinilo o ditianilo donde dicho Het12 está substituido de manera optativa con uno o cuando sea posible dos o más substituyentes seleccionados de hidroxi, halo, amino, alquilo C1-4-, hidroxialquilo C1-4-, alquiloxi C1-4alquilo C1-4, hidroxialquiloxi C1-4-alquilo C1-4, mono- o di(alquil C1-4)amino- o mono- o di(alquil C1-4)amino-alquilo C1-4-; Het13 representa un heterociclo seleccionado de pirrolidinilo o piperidinilo substituidos de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo C3-6, hidroxialquilo C1-4-, alquiloxi C1-4alquilo C1-4 o polihidroxialquilo C1-4; Het14 representa un heterociclo seleccionado de morfolinilo, pirrolidinilo, piperazinilo o piperidinilo substituidos de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo C3-6, hidroxialquilo C1-4, alquiloxi C1-4-alquilo C1-4 o polihidroxialquilo C1-4; Het15 representa un heterociclo seleccionado de morfolinilo, pirrolidinilo, piperazinilo o piperidinilo substituidos de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo C3-6, hidroxialquilo C1-4, alquiloxi C1-4-alquilo C1-4 o polihidroxialquilo C1-4; Het16 representa un heterociclo seleccionado de morfolinilo, pirrolidinilo, piperazinilo 1,3,2-dioxaborolano o piperidinilo donde dicho heterociclo se encuentra substituido de manera opcional con uno o más substituyentes seleccionados de alquilo C1-4; y Het17 representa un heterociclo seleccionado de pirrolidinilo o piperidinilo substituidos de manera opcional con uno o cuando sea posible dos o más substituyentes seleccionados de alquilo C1-4, cicloalquilo
Applications Claiming Priority (3)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP0305723 | 2003-05-27 | ||
EP0310266 | 2003-09-15 | ||
EP0351061 | 2003-12-18 |
Publications (1)
Publication Number | Publication Date |
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AR045687A1 true AR045687A1 (es) | 2005-11-09 |
Family
ID=33493782
Family Applications (2)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP040101806A AR045687A1 (es) | 2003-05-27 | 2004-05-26 | Macrociclos derivados de la quinazolina, procesos de preparacion y composiciones farmaceuticas que los contienen |
ARP130102897A AR092137A2 (es) | 2003-05-27 | 2013-08-15 | Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos |
Family Applications After (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP130102897A AR092137A2 (es) | 2003-05-27 | 2013-08-15 | Derivados macrociclicos de quinazolina utiles como agentes antiproliferativos |
Country Status (32)
Country | Link |
---|---|
US (4) | US7648975B2 (es) |
EP (2) | EP2305687A1 (es) |
JP (1) | JP4887151B2 (es) |
KR (1) | KR101143878B1 (es) |
CN (1) | CN102718775B (es) |
AR (2) | AR045687A1 (es) |
AT (1) | ATE544454T1 (es) |
AU (1) | AU2004243487B2 (es) |
BR (1) | BRPI0410714B8 (es) |
CA (1) | CA2525214C (es) |
CL (1) | CL2004001267A1 (es) |
CO (1) | CO5640038A2 (es) |
CY (1) | CY1113002T1 (es) |
DK (1) | DK1633365T3 (es) |
EA (1) | EA009064B1 (es) |
ES (1) | ES2381976T3 (es) |
HK (1) | HK1176350A1 (es) |
HR (1) | HRP20120351T1 (es) |
IL (3) | IL172154A0 (es) |
IS (1) | IS3030B (es) |
JO (1) | JO2785B1 (es) |
MX (1) | MXPA05012762A (es) |
MY (1) | MY148633A (es) |
NO (1) | NO334209B1 (es) |
NZ (1) | NZ544154A (es) |
PA (1) | PA8603801A1 (es) |
PL (1) | PL1633365T3 (es) |
PT (1) | PT1633365E (es) |
SI (1) | SI1633365T1 (es) |
TW (3) | TWI468372B (es) |
UA (1) | UA84010C2 (es) |
WO (1) | WO2004105765A1 (es) |
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MXPA06007017A (es) | 2003-12-18 | 2006-08-31 | Janssen Pharmaceutica Nv | Derivados de pirido y pirimidopirimidina como agentes antiproliferativos. |
JO3088B1 (ar) * | 2004-12-08 | 2017-03-15 | Janssen Pharmaceutica Nv | مشتقات كوينازولين كبيرة الحلقات و استعمالها بصفتها موانع كينيز متعددة الاهداف |
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