AR038052A1 - Derivados de quinazolina como inhibidores de auroraquinasas - Google Patents
Derivados de quinazolina como inhibidores de auroraquinasasInfo
- Publication number
- AR038052A1 AR038052A1 ARP020105081A ARP020105081A AR038052A1 AR 038052 A1 AR038052 A1 AR 038052A1 AR P020105081 A ARP020105081 A AR P020105081A AR P020105081 A ARP020105081 A AR P020105081A AR 038052 A1 AR038052 A1 AR 038052A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- hydroxy
- group
- alkoxy
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title 1
- JWVCLYRUEFBMGU-UHFFFAOYSA-N quinazoline Chemical class N1=CN=CC2=CC=CC=C21 JWVCLYRUEFBMGU-UHFFFAOYSA-N 0.000 title 1
- 125000000217 alkyl group Chemical group 0.000 abstract 31
- 125000006273 (C1-C3) alkyl group Chemical group 0.000 abstract 22
- 125000005843 halogen group Chemical group 0.000 abstract 18
- 229910052757 nitrogen Inorganic materials 0.000 abstract 13
- 125000000623 heterocyclic group Chemical group 0.000 abstract 12
- 125000004356 hydroxy functional group Chemical group O* 0.000 abstract 12
- -1 aryl-C1-10 alkyl Chemical group 0.000 abstract 10
- 125000004178 (C1-C4) alkyl group Chemical group 0.000 abstract 9
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 abstract 9
- 125000003118 aryl group Chemical group 0.000 abstract 8
- 125000001424 substituent group Chemical group 0.000 abstract 8
- 125000000304 alkynyl group Chemical group 0.000 abstract 7
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 7
- 229910052717 sulfur Inorganic materials 0.000 abstract 7
- 125000000229 (C1-C4)alkoxy group Chemical group 0.000 abstract 6
- 125000004043 oxo group Chemical group O=* 0.000 abstract 6
- 229910052760 oxygen Inorganic materials 0.000 abstract 6
- 125000002023 trifluoromethyl group Chemical group FC(F)(F)* 0.000 abstract 6
- 125000003342 alkenyl group Chemical group 0.000 abstract 5
- 229910052799 carbon Inorganic materials 0.000 abstract 5
- 125000005842 heteroatom Chemical group 0.000 abstract 5
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 5
- 125000002853 C1-C4 hydroxyalkyl group Chemical group 0.000 abstract 4
- 125000003545 alkoxy group Chemical group 0.000 abstract 4
- 125000004397 aminosulfonyl group Chemical group NS(=O)(=O)* 0.000 abstract 4
- 125000003917 carbamoyl group Chemical group [H]N([H])C(*)=O 0.000 abstract 4
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 4
- 229920006395 saturated elastomer Polymers 0.000 abstract 4
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 abstract 3
- 125000006274 (C1-C3)alkoxy group Chemical group 0.000 abstract 3
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 3
- 125000005913 (C3-C6) cycloalkyl group Chemical group 0.000 abstract 3
- 125000004423 acyloxy group Chemical group 0.000 abstract 3
- 125000004453 alkoxycarbonyl group Chemical group 0.000 abstract 3
- 125000000027 (C1-C10) alkoxy group Chemical group 0.000 abstract 2
- 125000002861 (C1-C4) alkanoyl group Chemical group 0.000 abstract 2
- 125000004760 (C1-C4) alkylsulfonylamino group Chemical group 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 2
- 125000002373 5 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000004070 6 membered heterocyclic group Chemical group 0.000 abstract 2
- 125000006374 C2-C10 alkenyl group Chemical group 0.000 abstract 2
- 125000006615 aromatic heterocyclic group Chemical group 0.000 abstract 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 2
- 125000001589 carboacyl group Chemical group 0.000 abstract 2
- 125000004432 carbon atom Chemical group C* 0.000 abstract 2
- 125000006413 ring segment Chemical group 0.000 abstract 2
- 125000004768 (C1-C4) alkylsulfinyl group Chemical group 0.000 abstract 1
- 125000004769 (C1-C4) alkylsulfonyl group Chemical group 0.000 abstract 1
- 125000006656 (C2-C4) alkenyl group Chemical group 0.000 abstract 1
- 125000006650 (C2-C4) alkynyl group Chemical group 0.000 abstract 1
- 125000006717 (C3-C10) cycloalkenyl group Chemical group 0.000 abstract 1
- 125000006569 (C5-C6) heterocyclic group Chemical group 0.000 abstract 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 abstract 1
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 1
- 125000005236 alkanoylamino group Chemical group 0.000 abstract 1
- 125000003302 alkenyloxy group Chemical group 0.000 abstract 1
- 125000004849 alkoxymethyl group Chemical group 0.000 abstract 1
- 125000003282 alkyl amino group Chemical group 0.000 abstract 1
- 125000004471 alkyl aminosulfonyl group Chemical group 0.000 abstract 1
- 125000005115 alkyl carbamoyl group Chemical group 0.000 abstract 1
- 125000004390 alkyl sulfonyl group Chemical group 0.000 abstract 1
- 125000005133 alkynyloxy group Chemical group 0.000 abstract 1
- 150000001408 amides Chemical class 0.000 abstract 1
- 125000004103 aminoalkyl group Chemical group 0.000 abstract 1
- 125000004104 aryloxy group Chemical group 0.000 abstract 1
- 125000002915 carbonyl group Chemical group [*:2]C([*:1])=O 0.000 abstract 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 125000004122 cyclic group Chemical group 0.000 abstract 1
- 125000000392 cycloalkenyl group Chemical group 0.000 abstract 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 abstract 1
- 125000001511 cyclopentyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C1([H])[H] 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
- 125000005553 heteroaryloxy group Chemical group 0.000 abstract 1
- 229910052739 hydrogen Inorganic materials 0.000 abstract 1
- 239000001257 hydrogen Substances 0.000 abstract 1
- 125000005113 hydroxyalkoxy group Chemical group 0.000 abstract 1
- AQYSYJUIMQTRMV-UHFFFAOYSA-N hypofluorous acid Chemical compound FO AQYSYJUIMQTRMV-UHFFFAOYSA-N 0.000 abstract 1
- 125000002632 imidazolidinyl group Chemical group 0.000 abstract 1
- LVWZTYCIRDMTEY-UHFFFAOYSA-N metamizole Chemical compound O=C1C(N(CS(O)(=O)=O)C)=C(C)N(C)N1C1=CC=CC=C1 LVWZTYCIRDMTEY-UHFFFAOYSA-N 0.000 abstract 1
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 abstract 1
- 125000004573 morpholin-4-yl group Chemical group N1(CCOCC1)* 0.000 abstract 1
- 125000004430 oxygen atom Chemical group O* 0.000 abstract 1
- 125000004193 piperazinyl group Chemical group 0.000 abstract 1
- 125000003386 piperidinyl group Chemical group 0.000 abstract 1
- 125000003072 pyrazolidinyl group Chemical group 0.000 abstract 1
- UBQKCCHYAOITMY-UHFFFAOYSA-N pyridin-2-ol Chemical group OC1=CC=CC=N1 UBQKCCHYAOITMY-UHFFFAOYSA-N 0.000 abstract 1
- 125000000719 pyrrolidinyl group Chemical group 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/517—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
-
- 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
-
- 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
- C07D403/12—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 linked by a chain containing hetero atoms as chain links
-
- 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Uso de un compuesto de fórmula (1) o de una sal, un éster o una amida del mismo; en donde : X es O o S, S(O) o S(O)2, o NR6 donde R6 es H o alquilo C1-6; R5 es un grupo de fórmula (2) 0 (3): donde * indica el punto de enlace al grupo X en fórmula (1);R1, R2, R3, R4 se seleccionan en forma independiente de H, halo, ciano, nitro, trifluormetilo, alquilo C1-3, -NR7R8 o X1R9;R7 y R8 son independientemente H o alquilo C1-3; X1 es un enlace directo, -O-, -CH2-, -OCO-, carbonilo, -S-; -SO-, -SO2-, -NR10CO-,-CONR11-, -SO2NR12-, -NR13SO2- o -NR14-; R10, R11, R12, R13 y R14 son independientemente H, alquilo C1-3 o alcoxiC1-3-alquiloC2-3; R9 se selecciona de uno de los siguientes grupos: 1) H o alquilo C1-5 que puede no estar sustituido o puede estar sustituido con uno o más grupos seleccionados de hidroxi, flúor o amino; 2) alquiloC1-5X2COR15 (donde X2 representa -O- o -NR16-(en el que R15 representa H, alquilo C1-3 o alcoxiC1-3-alquiloC2-3) y R16 representa alquilo C1-3, -NR17R18 o -OR19 (donde R17, R18, y R19 que pueden ser iguales o diferentes y cada uno representa H, alquilo C1-3 o alcoxiC1-3-alquiloC2-3)); 3) alquilo C1-5X3R20 (donde X3 representa -O-, -S-, -SO-, -SO2-, -OCO-, -NR21CO-,-CONR22-, -SO2NR23-, -NR24SO2-, o -NR25- ( donde R21, R22, R23, R24 y R25 cada uno representa independientemente H, alquilo C1-3 o alcoxiC1-3-alquiloC2-3) y R20 representa H, alquilo C1-3, ciclopentilo, ciclohexilo o un grupo heterocíclico saturado con 5 o 6 miembros con 1 o 2 heteroátomos seleccionados independientemente de O, S, y N, donde el grupo alquiloC1-3 puede contener 1 o 2 sustituyentes seleccionados de oxo, hidroxi, halo, y alcoxi C1-4 y el grupo cíclico puede contener 1 o 2 sustituyentes seleccionados de oxo, hidroxi, halo, alquilo C1-4, hidroxialquilo C1-4 y alcoxiC1-4); 4) alquilo C1-5X4alquiloC1-5X5R26 (donde X4 y X5 que pueden ser iguales o diferentes son cada uno -O-, -S-, -SO,-SO2-, -NR27CO-, -CONR28-, -SO2NR29-, -NR30SO2- o -NR31- (donde R27, R28, R29, R30 y R31 cada uno representa independientemente H, alquilo C1-3 o alcoxiC1-3-alquiloC2-3) y R26 representa H o alquilo C1-3); 5) R32( donde R32 es un grupo heterocíclico saturado de 5 o 6 miembros (unido a través de carbono o N) con 1 o 2 heteroátomos seleccionados independientemente de O, S, y N, donde el grupo heterocíclico puede contener 1 o 2 sustituyentes seleccionados de oxo, hidroxi, halo, alquilo C1-4, hidroxialquilo C1-4, alcoxi C1-4, alcoxiC1-4alquiloC1-4 y alquilsulfonilC1-4alquiloC1-4); 6) alquilo C1-5R32 (donde R32 es como se definió anteriormente); 7) alqueniloC2-5R32 (donde R32 es como se definió anteriormente); 8) alquiniloC2-5R32 (donde R32 es como se definió anteriormente); 9) R33 (donde R33 representa un grupo piridona, un grupo fenilo o un grupo heterocíclico aromático de 5 o 6 miembros (unido a través de C o N) con 1, 2 o 3 heteroátomos seleccionados de O, N y S, donde el grupo piridona, fenilo o heterocíclico aromático puede contener hasta 5 sustituyentes sobre átomos de C disponibles seleccionados de hidroxi, halo, amino, alquiloC1-4, alcoxiC1-4, hidroxialquiloC1-4, aminoalquiloC1-4, alquilamino C1-4, hidroxialcoxi C1-4, carboxi, trifluormetilo, ciano, -CONR34R35 y NR36COR37 (donde R34, R35, R36 y R37, que pueden ser iguales o diferentes, cada uno representa H, alquiloC1-4 o alcoxiC1-3-alquiloC2-3)); 10) alquiloC1-5R33 (donde R33 es como se definió anteriormente): 11) alqueniloC2-5R33 (donde R33 es como se definió anteriormente); 12) alquiniloC2-5R33 (donde R33 es como se definió anteriormente); 13) alquiloC1-5X6R33 (donde X6 representa -O-, -S-, -SO-; -SO2-, -NR38CO-CONR39-, -SO2NR40, -NR41SO2- o NR42- ( donde R38, R39, R40 , R41 y R42 cada uno representa independientemente H, alquiloC1-3 o alcoxiC1-3-alquiloC2-3) y R33 es como se definió anteriormente): 14) alqueniloC2-5X7R33 (donde X7 representa -O-;-S-, -SO-, -SO2-, -NR43CO-, -CONR44-, -SO2NR45-, -NR46SO2- o -NR47-, (donde R43, R44, R45, R46 y R47 cada uno representa independientemente H, alquiloC1-3 o alcoxiC1-3alquiloC2-3) y R33 es como se definió anteriormente), 15) alquiniloC2-5X8R33 (donde X8 representa -O-,-S-,-SO-, -SO2-, -NR48CO-, -CONR49-, -SO2NR50-, -NR51SO2- o -NR52- (donde R48, R49, R50, R51 y R52 cada uno representa independientemente H, alquiloC1-3 o alcoxiC1-3-alquiloC2-3) y R33 es como se definió anteriormente); 16) alquiloC1-3X9alquiloC1-3R33 (donde X9 representa -O-; -S-, -SO.-SO2-,NR53CO-, CONR54-, SO2NR55, -NR56SO2- o NR57 (donde R53, R54. R55. R56 y R57 cada uno representa independientemente H, alquiloC1-3 o alcoxiC1-3alquiloC2-3) y R33 es como se definió anteriormente); 17)alquilo C1-3X9alquilo C1-3R32 (donde X9 y R32 son como se definió anteriormente); 18) alquilo C1-3 opcionalmente sustituido con 1, 2, o 3 halo; 19) alquilo C1-5X10alquilo C1-5X11R90 (donde X10 y X11, que pueden ser iguales o diferentes son cada uno, -O-;-S-;-SO-; -SO2-, NR91CO, CONR92, SO2NR93, NR94SO2 o NR95 (donde R91, R92, R93, R94 y R95 cada uno representa independientemente alquilo C1-5, alquilo C1-3 (sustituido con 1, 2, o 3 halo, alquilo C1-4 o alcoxi C1-3 (y en donde hay 2 grupos alcoxi C1-4, los grupos alquilo C1-4 de alcoxi pueden formar juntos un grupo heterocíclico saturado con 5 o 6 miembros, con 2 átomos de oxígeno)), alquenilo C2-5, alquinilo C2-5, cicloalquilo C3-6 opcionalmente sustituido con halo, hidroxi, alquilo C1-3 o hidroxialquilo C1-4), cicloalquilo C3-6alquiloC1-3 (opcionalmente sustituido con halo, hidroxi, alquilo C1-3 o hidroxialquilo C1-4) o alcoxiC1-3alquiloC2-3) y R90 representa hidrógeno o alquilo C1-3; 20) cicloalquilo C3-6; 21) R96 (donde R96 es un grupo heterocíclico de 5 o 6 miembros que puede estar saturado o no saturado (unido a través de C o N ) con 1 o 2 heteroátomos seleccionados en forma independiente de O, S y N, donde el grupo heterocíclico puede contener 1 o 2 sustituyentes seleccionados de hidroxialquilo C1-4, alquilo C1-4, hidroxi y alcoxiC1-4alquiloC1-4; 22) alquiloC1-5R96 (donde R96 es como se definió anteriormente); y en donde: R60, R61 y R62 son independientemente H, nitro, ciano, halo, oxo, amino, trifluormetilo, alcoximetilo C1-4, di(alcoxi C1-4)metilo o alcanoilo C1-6 o un grupo seleccionado de alquilo C1-10, alquenilo C2-10, alquinilo C2-10, heterociclilo, heterociclilo-alquilo C1-10, alcoxi C1-10, aril-alquilo C1-10, arilo, cicloalquilo C3-10, cicloalquenilo C3-10 y cicloalquinilo C3-10 ( donde ese grupo está opcionalmente sustituido con 1, 2 o 3 sustituyentes independientemente seleccionados de halo, alquiloC1-4 (opcionalmente sustituido con 1, 2 o 3 halo), mercapto, hidroxi, carboxi, alcoxi C1-10, nitro, ciano, arilo, heteroarilo, heteroariloxi, alqueniloxi C2-10,alquiniloxi C2-10, alcoxiC1-4alcoxiC1-4, ariloxi ( donde el grupo arilo puede estar sustituido con halo, nitro, o hidroxi), amino, ciano, nitro, mono o di(alquiloC1-6)amino, oximino o S(O)y donde y es 0, 1, 2 o 3), o un grupo seleccionado de =CR78R79, C(O)xR77, OR77, S(O)yR77, NR78R79, C(O)NR78R79, OC(O)NR78R79, NOR77, -NR77C(O)xR78, -NR77CONR78R79, -N=CR78R79, S(O)yNR78R79 o NR77S(O)yR78 o un grupo seleccionado de fenilo, bencilo o grupo heterocíclico de 5 a 6 miembros con 1, 2 o 3 heteroátomos seleccionados independientemente de O, S, y N, donde el grupo heterocíclico puede ser aromático o no aromático y puede estar saturado (unido a través de un átomo de anillo de C o N) o no saturado (unido a través de un átomo de anillo de C), donde el fenilo, bencilo o el grupo heterocíclico puede contener en uno o más átomos de C de anillo hasta 5 sustituyentes seleccionados de hidroxi, halo, alquilo C1-3, alcoxi C1-3, alcanoiloxi C1-3, trifluormetilo, ciano, amino, nitro, alcanoilo C2-4, alcoxicarbonilo C1-4, alquilsulfonilo C1-14, alquilsulfinilo C1-4, alquilsulfonilo C1-4, carbamoilo, N-alquilcarbamoilo C1-4, N,N-di(alquil C1-4)carbamoilo, aminosulfonilo, N-alquilaminosulfonilo C1-4, N,N-di(alquil C1-4)aminosulfonilo, alquilsulfonilamino C1-4 y un grupo heterocíclico saturado seleccionado de morfolino, tiomorfolino, pirrolidinilo, piperazinilo, piperidinilo, imidazolidinilo y pirazolidinilo, donde el grupo heterocíclico saturado puede contener 1 o 2 sustituyentes seleccionados de oxo, hidroxi, halo, alquilo C1-3, alcoxi C1-3, alcanoiloxi C1-3, trifluormetilo, ciano, amino, nitro, y alcoxicarbonilo C1-4, o un grupo de la sub-fórmula (4) o un grupo de la sub-fórmula (5), o un grupo de la sub-fórmula (6): donde: p y q son independientemente 0 o 1; r es 0, 1, 2, 3 o 4; R1´ y R1´´ son independientemente H, hidroxi, halo, ciano, alquilo C1-10, cicloalquilo C3-10, alquenilo C2-10 o alquinilo C2-10 (donde alquilo C1-10, cicloalquilo C3-10, alquenilo C2-10 o alquinilo C2-10 están opcionalmente sustituidos con halo, nitro, ciano, hidroxi, trifluormetilo, amino, carboxi, carbamoilo, mercapto, sulfamoilo, alquilo C1-4, alquenilo C2-4, alquinilo C2-4, cicloalquilo C3-6,cicloalquenilo C3-6, alcoxi C1-4, alcanoilo C1-4, alcanoiloxi C1-4, alcanoilamino C1-4, N,N-di(alcanoil C1-4)amino, N-(alquil C1-4)carbamoilo, N,N-di(alquil C1-4)carbamoilo, alquil C1-4S, alquil C1-4S(O), alquil C1-4S(O)2, alcoxicarbonilo C1-4, N-(alquilC1-4)sulfamoilo, N,N-di(alquil C1-4)sulfamoilo, alquilsulfonilamino C1-4 o heterociclilo); o R1´y R1´´ pueden conjuntamente formar un anillo de 3 a 6 miembros que puede estar saturado o no saturado; T es C=O, SOn (donde n es 0, 1 o 2), C(=NOR)CO, C(O)C(O), C=NCN o CV=NO; V es independientemente R63 o N(R63)R64; R63 y R64 se seleccionan en forma independiente de H, (CH2)q´R70 (q´es 0 o 1), arilo (opcionalmente sustituido con 1, 2 o 3 alquilo C1-6 (opcionalmente sustituidos con 1, 2 o 3 grupos hidroxi)), alquilo C1-10 (opcionalmente sustituido con 1, 2 o 3 grupos independientemente seleccionados de arilo o un grupo heterocíclico, donde el arilo y el grupo heterocíclico están opcionalmente sustituidos con 1, 2 o 3 grupos independientemente seleccionados de alquilo C1-6, nitro, ciano, halo, oxo, =CR78R79, C(O)xR77, OR77, S(O)yR77, NR78R79, C(O)NR78R79, OC(O)NR78R79, =NOR77, NR77C(O)xR78, NR77
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP01403357 | 2001-12-24 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR038052A1 true AR038052A1 (es) | 2004-12-22 |
Family
ID=8183051
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP020105081A AR038052A1 (es) | 2001-12-24 | 2002-12-23 | Derivados de quinazolina como inhibidores de auroraquinasas |
Country Status (31)
| Country | Link |
|---|---|
| US (2) | US7402585B2 (es) |
| EP (1) | EP1463506B1 (es) |
| JP (1) | JP4498741B2 (es) |
| KR (1) | KR101029281B1 (es) |
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| AT (1) | ATE446093T1 (es) |
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| UY (1) | UY27604A1 (es) |
| WO (1) | WO2003055491A1 (es) |
| ZA (1) | ZA200404923B (es) |
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-
2002
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- 2002-12-20 BR BRPI0215312A patent/BRPI0215312B8/pt not_active IP Right Cessation
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- 2002-12-20 HU HU0402454A patent/HU229477B1/hu unknown
- 2002-12-20 WO PCT/GB2002/005845 patent/WO2003055491A1/en not_active Ceased
- 2002-12-20 SI SI200230864T patent/SI1463506T1/sl unknown
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- 2002-12-20 AT AT02788214T patent/ATE446093T1/de active
- 2002-12-20 RU RU2004122926/04A patent/RU2323215C2/ru active
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