AR049097A1 - PIRIMIDINE DERIVATIVES TO TREAT ANOMALO CELLULAR GROWTH - Google Patents

PIRIMIDINE DERIVATIVES TO TREAT ANOMALO CELLULAR GROWTH

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AR049097A1
AR049097A1 ARP050101969A ARP050101969A AR049097A1 AR 049097 A1 AR049097 A1 AR 049097A1 AR P050101969 A ARP050101969 A AR P050101969A AR P050101969 A ARP050101969 A AR P050101969A AR 049097 A1 AR049097 A1 AR 049097A1
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alkyl
cycloalkyl
heterocyclyl
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heteroaryl
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Pfizer Prod Inc
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    • 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
    • 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
    • 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
    • C07D403/14—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
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

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Abstract

Derivados de pirimidina, método para usar dichos compuestos en el tratamiento del crecimiento celular anomalo en mamíferos, especialmente seres humanos, y a composiciones farmacéuticas que contienen dichos compuestos. Reivindicacion 1: Un compuesto de formula (1) o una de sus sales, solvatos, hidratos o profármacos farmacéuticamente aceptable, en la que n es un numero entero de 1 a 3; cada R1 es un sustituyente independientemente seleccionado del grupo que consiste en H, hidroxi, -alquilo C1- 6, -cicloalquilo C3-7, -heterociclilo C2-9, -Oalquilo C1-6, -Ocicloalquilo C3-7, -Oheterociclilo C2-9, -NR5R6, -SR7,-SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, y -NR12SO2R7; en la que dichos sustituyentes R1, -alquilo C1-6, - cicloalquilo C3-7, -heterociclilo C2-9, -Oalquilo C1-6, -Ocicloalquilo C3-7, -Oheterociclilo C2-9, -NR5R6, -SR7,-SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, y -NR12SO2R7, están opcionalmente sustituidos con 1 a 3 restos independientemente seleccionados del grupo que consiste en H, halogeno, hidroxi, -CF3, -CN, -alquilo C1-6, -NR5R6, -OR12, -cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, -CONR5R6 y -CONR5R8; cada R2 es un sustituyente independientemente seleccionado del grupo que consiste en H, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, y -CONR5R6; en la que dichos sustituyentes R2, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, - cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, y -CONR5R6, están opcionalmente sustituidos con 1 a 3 restos independientemente seleccionados del grupo que consiste en H, halogeno, hidroxi, -CF3, -NO2, -CN, -alquilo C1-6, -alquenilo C2-6, alquinilo C2-6, -C=N-OH, -C=N-O(alquilo C1-6), -NR5R6, -OR12, -cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, -CONR5R6, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, y -NR12SO2R7, en los que dichos restos de R2 -alquenilo C2-6 y - alquinilo C2-6 pueden estar opcionalmente sustituidos con uno a tres grupos R12; R1 y R2 se pueden considerar junto con el(los) átomo(s) al(los) que está(n) unido(s) para formar un grupo cíclico, -cicloalquilo C3-10 o -heterociclilo C2-9, en el que dicho grupo cíclico está opcionalmente sustituido con uno a tres restos independientemente seleccionados del grupo que consiste en H, halogeno, hidroxi, -CF3, -NO2, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -C=N-OH, -C=N-O(alquilo C1-6), - NR5R6, -OR12, -cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, -CONR5R6, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, y -NR12SO2R7, en los que dichos restos -alquenilo C2-6 y -alquinilo C2-6 de dicho grupo cíclico puede estar opcionalmente sustituido con uno a tres grupos R12, y dicho grupo cíclico está opcionalmente interrumpido con uno a tres elementos seleccionados del grupo que consiste en -(C=O), -SO2, -S-, -O-, -N-, -NH- y -NR12; R3 es un sustituyente seleccionado del grupo que consiste en: (a) H; (b) -arilo C6-10 o -heteroarilo C1-9, opcionalmente sustituidos con 1 a 3 restos independientemente seleccionados del grupo que consiste en halogeno, hidroxi, -alquilo C1-6, -alquil(C1-6)-P(O)(Oalquilo C1-6)2, - cicloalquilo C3-10, arilo C6-10, heterociclilo C2-9, -heteroarilo C1-9, -NR5R6, -NHSO2-alquilo C1-6, -NHSO2-cicloalquilo C3-6, -N(alquil C1-6)(SO2-alquilo C1-6), N-(alquil C1-6)(SO2-cicloalquilo C3-6), -N(cicloalquil C3-6)(SO2-alquilo C1-6), - N(cicloalquil C3-6)(SO2-cicloalquilo C3-6), -Oalquilo C1-6, -O-alquilo C1-6, -O-SO2-cicloalquilo C3-6, -(CO)-alquilo C1-6, -(CO)CF3, -(CO)-cicloalquilo C3-10, -(CO)-arilo C6-10, -(CO)-heterociclilo C2-9, -(CO)-heteroarilo C1-9, -(CO)O-alquilo C1-6, - (CO)O-cicloalquilo C3-10, -(CO)O-arilo C6-10, -(CO)O-heterociclilo C2-9, -(CO)O-heteroarilo C1-9, -(CO)-alquilo C1-6-Oalquilo C1-6, -SO2-alquilo C1-6, -SO2-cicloalquilo C3-6, -SO2CF3, -SO2NH2, -SO2NH-alquilo C1-6, -SO2NH-cicloalquilo C3-6, - SO2N(alquilo C1-6)2, -SO2N(alquilo C1-6)(cicloalquilo C3-6), -SO2N(cicloalquilo C3-6)2 y -SO2NR5R6, en el que dichos -arilo C6-10 o -heteroarilo C1-9 están opcionalmente interrumpidos con uno a tres elementos seleccionados del grupo que consiste en - S-, -O-, -N-, -NH- y -NR12; ( c ) -cicloalquilo C3-10, -heterociclilo C2-9, y -alquil C1-6-heterociclilo C2-9, opcionalmente sustituidos con uno a tres restos independientemente seleccionados del grupo que consiste en halogeno, hidroxi, -alquilo C1- 6, -alquil(C1-6)-P(O)(Oalquilo C1-6)2, -cicloalquilo C3-10, arilo C6-10, heterociclilo C2-9, -heteroarilo C1-9, -NR5R6, -NHSO2-alquilo C1-6, -NHSO2-cicloalquilo C3-6, -N(alquil C1-6)(SO2-alquilo C1-6), N-(alquil C1-6)(SO2-cicloalquilo C3-6), - N(cicloalquil C3-6)(SO2-alquilo C1-6), -N(cicloalquil C3-6)(SO2-cicloalquilo C3-6), -Oalquilo C1-6, -O-SO2-alquilo C1-6, -O-SO2-alquilo C1-6, -O-SO2-cicloalquilo C3-6, -(CO)-alquilo C1-6, -(CO)CF3, -(CO)-cicloalquilo C3-10, -(CO)-arilo C6-10), -(CO)- heterociclilo C2-9, -(CO)-heteroarilo C1-9, -(CO)O-alquilo C1-6, -(CO)O-cicloalquilo C3-10, -(CO)O-arilo C6-10, -(CO)O-heterociclilo C2-9, -(CO)O-heteroarilo C1-9, -(CO)-alquil C1-6-Oalquilo C1-6, -SO2-alquilo C1-6, -SO2-cicloalquilo C3-6, -SO2CF3, - SO2NH2, -SO2NH-alquilo C1-6, -SO2NH-cicloalquilo C3-6, -SO2N(alquilo C1-6)2, -SO2N(alquil C1-6)(cicloalquilo C3-6), -SO2N(cicloalquilo C3-6)2 y -SO2NR5R6, en el que dichos -cicloalquilo C3-10, -heterociclilo C2-9, y -alquil C1-6-heterociclilo C2-9 están opcionalmente interrumpidos con uno a tres elementos seleccionados del grupo que consiste en --(C=O), -SO2, -S-, -O-, -N-, -NH- y -NR12; (e) -alquilo C1-6 opcionalmente sustituido con uno a tres restos seleccionados del grupo que consiste en halogeno, hidroxi, -alquilo C1-6, alquil(C1-6)-P(O)(Oalquilo C1-6)2, -cicloalquilo C3-10, arilo C6-10, heterociclilo C2-9, -heteroarilo C1-9, -NR5R6, -NHSO2-alquilo C1-6, -NHSO2-cicloalquilo C3-6, -N(alquil C1-6)(SO2-alquilo C1-6), N-(alquil C1- 6)(SO2-cicloalquilo C3-6), -N(cicloalquil C3-6)(SO2-alquilo C1-6), -N(cicloalquil C3-6)(SO2-cicloalquilo C3-6), -Oalquilo C1-6, -O-SO2-alquilo C1-6, -O-SO2-cicloalquilo C3-6, -(CO)-alquilo C1-6, -(CO)CF3, -(CO)-cicloalquilo C3-10, -(CO)-arilo C6-10, -(CO)-heterociclilo C2-9, -(CO)-heteroarilo C1-9, -(CO)O-alquilo C1-6, -(CO)O-cicloalquilo C3-10, -(CO)O-arilo C6-10, -(CO)O-heterociclilo C2-9, -(CO)O-heteroarilo C1-9, -(CO)-alquil C1-6-O-alquilo C1-6, -SO2-alquilo C1-6, -SO2-cicloalquilo C3-6, - SO2CF3, -SO2NH2, -SO2NH-alquilo C1-6, -SO2NH-cicloalquilo C3-6, -SO2N(alquilo C1-6)2, -SO2N(alquil C1-6)(cicloalquilo C3-6), -SO2N(cicloalquilo C3-6)2 y -SO2NR5R6, en el que dicho -alquilo C1-6 está opcionalmente sustituido con uno a tres elementos seleccionados del grupo que consiste en -(C=O), -SO2, -S-, -O-, -N-, -NH- y -NR12; y en la que cada sustituyente, resto o elemento R3 (b)-(d) está opcionalmente sustituido con uno a tres radicales independientemente seleccionados del grupo que consiste en H, halogeno, hidroxi, -CF3, -NO2, -CN, -alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -cicloalquilo C3-7, -heterociclilo C2-9, -arilo C6-10, heteroarilo C1-9, -Oalquilo C1-6, -Ocicloalquilo C3-7, -Oheterociclilo C2-9, -C=N-OH, -C=N- Oalquilo C1-6, -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR5, -NR12CONR5R6, y -NR12SO2R7; R4 es un sustituyente seleccionado del grupo que consiste en H, -alquilo C1-6, -cicloalquilo C3-7, y heterociclilo C2-9; en el que dichos sustituyentes R4 -alquilo C1-6, -cicloalquilo C3-7, y heterociclilo C2-9 están opcionalmente sustituidos con uno a tres restos independientemente seleccionados del grupo que consiste en H, halogeno, hidroxilo, -alquilo C1-6, -CN, -NR5R8, -OR5, - cicloalquilo C3-7, -heterociclilo C2-9, -CO2R12, -SO2NR5R6, -NR12SO2R7, -SO2R7 y -CONR5R8; en los que dichos R5 y R8 de dicho grupo -CONR5R8 se pueden considerar junto con los átomos a los que están unidos para formar un -heterociclilo C2-9; R5 y R6 son cada uno sustituyentes independientemente seleccionados del grupo que consiste en H, -alquilo C1-6, -cicloalquilo C3-7, -heterociclilo C2-9, -arilo C6-10, -heteroarilo C1-9, -COR12 y -SO2R12; en los que dichos sustituyentes R5 o R6 -alquilo C1- 6, -cicloalquilo C3-7, -heterociclilo C2-9, -arilo C6-10, -heteroarilo C1-9, -COR12 y -SO2R12 están opcionalmente sustituidos con uno a tres restos independientemente seleccionados del grupo que consiste en H, halogeno, -CF3, -CN, -alquilo C1-6, -NH- alquilo C1-6, -NH-cicloalquilo C3-7, -NH-heterociclilo C2-9, -NH-arilo C6-10, -NH-heteroarilo C1-9, -N(alquilo C1-6)2, -N(cicloalquilo C3-7)2, -N(heterociclilo C2-9)2, -N(arilo C6-10)2, -N(heteroarilo C1-9)2, -Oalquilo C1-6, -Ocicloalquilo C3-7, - Oheterociclilo C2-9, -Oarilo C6-10, -Oheteroarilo C1-9, -cicloalquilo C3-7, -heterociclilo C2-9, -CO2R7, -SO2NR5R6, -NR12SO2R7, -SO2R7, -CONH2, -CONHR7, y -CONR7R8; en los que R7 y R8 de dicho grupo -CONR7R8 se pueden considerar junto con el átomo de N al que están unidos para formar un -heterociclilo C2-9; R5 y R6 se pueden considerar junto con el(los) átomo(s) al(los) que está(n) unido(s) para formar un -heterociclilo C2-9, en el que dicho grupo -heterociclilo C2-9 está opcionalmente sustituido con uno a tres restos seleccionados del grupo que consiste en H, halogeno, hidroxi, -CF3, -NO2, -CN, alquilo C1-6, -alquenilo C2-6, -alquinilo C2-6, -C=N-OH, -C=N-Oalquilo C1-6, -NR7R8, -OR12, -cicloalquilo C3-7, -heterociclilo C2-9, - CO2R12, -CONR7R8, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR7R8, -NHCOR12, -NR12CONR7R8, y -NR12SO2R7, en los que dichos restos -alquenilo C2-6 y -alquinilo C2-6 de dicho grupo -heterociclilo C2-9 pude estar opcionalmente sustituidos con uno a tres grupos R7, y dicho grupo -heterociclilo C2-9 está opcionalmente interrumpido con uno a tres elementos seleccionados del grupo que consiste en -(C=O), -SO2, -S-, -O-, -N-, -NH- y -NR12; R7 es un sustituyente seleccionado del grupo que consiste en - alquilo C1-6, -cicloalquilo C3-7, -heterociclilo C2-9, -arilo C6-10, y -heteroarilo C1-9; en el que dichos suPyrimidine derivatives, a method for using said compounds in the treatment of anomalous cell growth in mammals, especially humans, and pharmaceutical compositions containing said compounds. Claim 1: A compound of formula (1) or a pharmaceutically acceptable salt, solvate, hydrate or prodrug thereof, wherein n is an integer from 1 to 3; each R1 is a substituent independently selected from the group consisting of H, hydroxy, -C1-6alkyl, -C3-7cycloalkyl, -C2-9 heterocyclyl, -C1-6alkyl, -C3-7 -cycloalkyl, -C2- -heterocyclyl 9, -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, and -NR12SO2R7; wherein said substituents R1, -C1-6alkyl, -C3-7 cycloalkyl, -C2-9 heterocyclyl, -C1-6alkyl, -C3-7cycloalkyl, -O2 -9-heterocyclyl, -NR5R6, -SR7, - SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, and -NR12SO2R7, are optionally substituted with 1 to 3 moieties independently selected from the group consisting of H, halogen, hydroxy, -CF3, -CN , -C 1-6 alkyl, -NR5R6, -OR12, -C3-7 cycloalkyl, -C2-9 heterocyclyl, -CO2R12, -CONR5R6 and -CONR5R8; each R2 is a substituent independently selected from the group consisting of H, -C1-6alkyl, -C2-6alkenyl, -C2-6alkynyl, -C3-7cycloalkyl, -C2-9 heterocyclyl, -CO2R12, and -CONR5R6 ; wherein said substituents R2, -C1-6alkyl, -C2-6alkenyl, -C2-6alkynyl, -C3-7cycloalkyl, -C2-9 heterocyclyl, -CO2R12, and -CONR5R6, are optionally substituted with 1 to 3 residues independently selected from the group consisting of H, halogen, hydroxy, -CF3, -NO2, -CN, -C1-6 alkyl, -C2-6 alkenyl, C2-6 alkynyl, -C = N-OH, -C = NO (C1-6 alkyl), -NR5R6, -OR12, -C3-7 cycloalkyl, -C2-9 heterocyclyl, -CO2R12, -CONR5R6, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR5R6, -NHCOR12 , -NR12CONR5R6, and -NR12SO2R7, wherein said radicals of R2-C2-6 alkenyl and -C2-6 alkynyl can be optionally substituted with one to three R12 groups; R1 and R2 can be considered together with the atom (s) to which they are attached to form a cyclic group, -C3-10 -cycloalkyl or -C2-9 heterocyclyl, in which said cyclic group is optionally substituted with one to three moieties independently selected from the group consisting of H, halogen, hydroxy, -CF3, -NO2, -C 1-6 alkyl, -C2-6 alkenyl, -C2-6 alkynyl, -C = N-OH, -C = NO (C1-6 alkyl), - NR5R6, -OR12, -C3-7 cycloalkyl, C2-9 heterocyclyl, -CO2R12, -CONR5R6, -CONR5R8, -SR7, -SOR7, - SO2R7, -SO2NR5R6, -NHCOR12, -NR12CONR5R6, and -NR12SO2R7, wherein said -C2-6 and -C2-6 alkenyl moieties of said cyclic group may be optionally substituted with one to three R12 groups, and said cyclic group it is optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, -N-, -NH- and -NR12; R3 is a substituent selected from the group consisting of: (a) H; (b) -C6-10 aryl or -C 1-9 heteroaryl, optionally substituted with 1 to 3 moieties independently selected from the group consisting of halogen, hydroxy, -C 1-6 alkyl, -C 1-6 alkyl -P (O ) (C1-6 alkyl) 2, - C3-10 cycloalkyl, C6-10 aryl, C2-9 heterocyclyl, C1-9 heteroaryl, -NR5R6, -NHSO2-C1-6 alkyl, -NHSO2-C3-6 cycloalkyl, -N (C1-6 alkyl) (SO2-C1-6 alkyl), N- (C1-6 alkyl) (SO2-C3-6 cycloalkyl), -N (C3-6 cycloalkyl) (SO2-C1-6 alkyl) , - N (C3-6 cycloalkyl) (SO2-C3-6 cycloalkyl), -C1-6 alkyl, -O-C1-6 alkyl, -O-SO2-C3-6 cycloalkyl, - (CO) -C1 -alkyl 6, - (CO) CF3, - (CO) -C3-10 cycloalkyl, - (CO) -C6-10 aryl, - (CO) -C2-9 heterocyclyl, - (CO) -C1-9 heteroaryl, - ( CO) O-C1-6 alkyl, - (CO) O-C3-10 cycloalkyl, - (CO) O-C6-10 aryl, - (CO) O-C2-9 heterocyclyl, - (CO) O-C1 heteroaryl -9, - (CO) -C 1-6 alkyl-C 1-6 alkyl, -SO2-C 1-6 alkyl, -SO2-C3-6 cycloalkyl, -SO2CF3, -SO2NH2, -SO2NH-C1-6 alkyl, -SO2NH -C3-6 cycloalkyl, - SO2N (C1-6 alkyl) 2, -SO2N (C1-6 alkyl) (cycloalkyl C3-6), -SO2N (C3-6 cycloalkyl) 2 and -SO2NR5R6, wherein said C6-10 aryl or C1-9 heteroaryl are optionally interrupted with one to three elements selected from the group consisting of - S -, -O-, -N-, -NH- and -NR12; (c) -C3-10 cycloalkyl, -C2-9 heterocyclyl, and -C1-6 alkyl-C2-9 heterocyclyl, optionally substituted with one to three moieties independently selected from the group consisting of halogen, hydroxy, -C1-6 alkyl , -C1-6 alkyl -P (O) (C1-6 alkyl) 2, -C3-10 cycloalkyl, C6-10 aryl, C2-9 heterocyclyl, C1-9 heteroaryl, -NR5R6, -NHSO2-alkyl C1-6, -NHSO2-C3-6 cycloalkyl, -N (C1-6 alkyl) (SO2-C1-6 alkyl), N- (C1-6 alkyl) (SO2-C3-6 cycloalkyl), - N (cycloalkyl C3-6) (SO2-C1-6 alkyl), -N (C3-6 cycloalkyl) (SO2-C3-6 cycloalkyl), -C1-6 alkyl, -O-SO2-C1-6 alkyl, -O-SO2 -C1-6 alkyl, -O-SO2-C3-6 cycloalkyl, - (CO) -C1-6 alkyl, - (CO) CF3, - (CO) -C3-10 cycloalkyl, - (CO) -C6 aryl 10), - (CO) - C2-9 heterocyclyl, - (CO) -C1-9 heteroaryl, - (CO) O-C1-6 alkyl, - (CO) O-C3-10 cycloalkyl, - (CO) O -C6-10 aryl, - (CO) C2-9 O-heterocyclyl, - (CO) C1-9 O-heteroaryl, - (CO) -C 1-6 alkyl-C 1-6 alkyl, -SO2-C 1-6 alkyl , -SO2-C3-6 cycloalkyl, -SO2CF3, - SO2NH2, -SO2NH-C1-6 alkyl, -SO 2NH-C3-6 cycloalkyl, -SO2N (C1-6 alkyl) 2, -SO2N (C1-6 alkyl) (C3-6 cycloalkyl), -SO2N (C3-6 cycloalkyl) 2 and -SO2NR5R6, wherein said - C3-10 cycloalkyl, -C2-9 heterocyclyl, and -C1-6 alkyl-C2-9 heterocyclyl are optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S- , -O-, -N-, -NH- and -NR12; (e) -C 1-6 alkyl optionally substituted with one to three moieties selected from the group consisting of halogen, hydroxy, -C 1-6 alkyl, (C 1-6) alkyl -P (O) (C 1-6 alkyl) 2, -C3-10 cycloalkyl, C6-10 aryl, C2-9 heterocyclyl, C1-9 heteroaryl, -NR5R6, -NHSO2-C1-6 alkyl, -NHSO2-C3-6 cycloalkyl, -N (C1-6 alkyl) ( SO2-C1-6 alkyl), N- (C1-6 alkyl) (SO2-C3-6 cycloalkyl), -N (C3-6 cycloalkyl) (SO2-C1-6 alkyl), -N (C3-6 cycloalkyl) (SO2-C3-6 cycloalkyl), -C1-6 alkyl, -O-SO2-C1-6 alkyl, -O-SO2-C3-6 cycloalkyl, - (CO) -C1-6 alkyl, - (CO) CF3 , - (CO) -C3-10 cycloalkyl, - (CO) -C6-10 aryl, - (CO) -C2-9 heterocyclyl, - (CO) -C1-9 heteroaryl, - (CO) O-C1-alkyl 6, - (CO) C3-10 O-cycloalkyl, - (CO) C6-10 O-aryl, - (CO) C2-9 O-heterocyclyl, - (CO) C1-9 O-heteroaryl, - (CO) -C1-6 alkyl-O-C1-6 alkyl, -SO2-C1-6 alkyl, -SO2-C3-6 cycloalkyl, -SO2CF3, -SO2NH2, -SO2NH-C1-6 alkyl, -SO2NH-C3-6 cycloalkyl , -SO2N (C1-6 alkyl) 2, -SO2N (C1-6 alkyl) (C3-6 cycloalkyl), -SO2N (C3-6 cycloalkyl) 2 and -SO2NR5R6, wherein said -C1-6 alkyl is optionally substituted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, -N-, - NH- and -NR12; and wherein each substituent, residue or element R3 (b) - (d) is optionally substituted with one to three radicals independently selected from the group consisting of H, halogen, hydroxy, -CF3, -NO2, -CN, -alkyl C 1-6, C 2-6 alkenyl, C 2-6 alkynyl, C 3-7 cycloalkyl, C 2-9 heterocyclyl, C 6-10 aryl, C 1-9 heteroaryl, C 1-6 alkyl, C 3-7 alkylcycloalkyl , -C2-9 heterocyclyl, -C = N-OH, -C = N- C1-6alkyl, -NR5R6, -SR7, -SOR7, -SO2R7, -CO2R12, -CONR5R6, -SO2NR5R6, -NHCOR5, -NR12CONR5R6 , and -NR12SO2R7; R4 is a substituent selected from the group consisting of H, -C1-6 alkyl, -C3-7 cycloalkyl, and C2-9 heterocyclyl; wherein said substituents R 4 -C 1-6 alkyl, -C 3-7 cycloalkyl, and C 2-9 heterocyclyl are optionally substituted with one to three moieties independently selected from the group consisting of H, halogen, hydroxyl, -C 1-6 alkyl, -CN, -NR5R8, -OR5, - C3-7 cycloalkyl, C2-9 heterocyclyl, -CO2R12, -SO2NR5R6, -NR12SO2R7, -SO2R7 and -CONR5R8; wherein said R5 and R8 of said group -CONR5R8 can be considered together with the atoms to which they are attached to form a C2-9 heterocyclyl; R5 and R6 are each substituents independently selected from the group consisting of H, -C1-6 alkyl, -C3-7cycloalkyl, -C2-9 heterocyclyl, -C6-10 aryl, -C1-9 heteroaryl, -COR12 and - SO2R12; wherein said substituents R5 or R6 -C1-6 alkyl, -C3-7 cycloalkyl, -C2-9 heterocyclyl, -C6-10 aryl, -C1-9 heteroaryl, -COR12 and -SO2R12 are optionally substituted with one to three residues independently selected from the group consisting of H, halogen, -CF3, -CN, -C1-6 alkyl, -NH- C1-6 alkyl, -NH-C3-7 cycloalkyl, -NH-C2-9 heterocyclyl, -NH -C6-10 aryl, -NH-C1-9 heteroaryl, -N (C1-6 alkyl) 2, -N (C3-7 cycloalkyl) 2, -N (C2-9 heterocyclyl) 2, -N (C6 aryl- 10) 2, -N (C1-9 heteroaryl) 2, -C1-6alkyl, -C3-7cycloalkyl, -C2-9 -heterocyclyl, -C6-10 -aryl, -C1-9 -heteroaryl, -C3-7 -cycloalkyl, -C2-9 heterocyclyl, -CO2R7, -SO2NR5R6, -NR12SO2R7, -SO2R7, -CONH2, -CONHR7, and -CONR7R8; wherein R7 and R8 of said group -CONR7R8 can be considered together with the N atom to which they are attached to form a C2-9 -heterocyclyl; R5 and R6 can be considered together with the atom (s) to which they are attached to form a C2-9 heterocyclyl, in which said C2-9 heterocyclyl group is optionally substituted with one to three moieties selected from the group consisting of H, halogen, hydroxy, -CF3, -NO2, -CN, C1-6 alkyl, -C2-6 alkenyl, -C2-6 alkynyl, -C = N-OH , -C = N-O-C1-6alkyl, -NR7R8, -OR12, -C3-7cycloalkyl, C2-9 heterocyclyl, - CO2R12, -CONR7R8, -CONR5R8, -SR7, -SOR7, -SO2R7, -SO2NR7R8, -NHCOR12, -NR12CONR7R8, and -NR12SO2R7, wherein said radicals -C2-6 alkenyl and -C2-6 alkynyl of said group -C2-9 heterocyclyl can be optionally substituted with one to three R7 groups, and said -heterocyclyl group C2-9 is optionally interrupted with one to three elements selected from the group consisting of - (C = O), -SO2, -S-, -O-, -N-, -NH- and -NR12; R7 is a substituent selected from the group consisting of - C1-6 alkyl, - C3-7 cycloalkyl, - C2-9 heterocyclyl, - C6-10 aryl, and - C1-9 heteroaryl; in which you say your

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WO2005118544A2 (en) * 2004-05-18 2005-12-15 Rigel Pharmaceuticals, Inc. Cycloalkyl substituted pyrimidinediamine compounds and their uses
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WO2009143389A1 (en) * 2008-05-21 2009-11-26 Ariad Pharmaceuticals, Inc. Phosphorous derivatives as kinase inhibitors
US8410126B2 (en) * 2009-05-29 2013-04-02 Boehringer Ingelheim International Gmbh Pyrimidine inhibitors of PKTK2
US8933227B2 (en) 2009-08-14 2015-01-13 Boehringer Ingelheim International Gmbh Selective synthesis of functionalized pyrimidines
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