AR080672A1 - Aminopirimidinas como inhibidores de syk - Google Patents

Aminopirimidinas como inhibidores de syk

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Publication number
AR080672A1
AR080672A1 ARP100104724A ARP100104724A AR080672A1 AR 080672 A1 AR080672 A1 AR 080672A1 AR P100104724 A ARP100104724 A AR P100104724A AR P100104724 A ARP100104724 A AR P100104724A AR 080672 A1 AR080672 A1 AR 080672A1
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Argentina
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alkyl
optionally substituted
independently selected
groups independently
co2ra
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Merck Frosst Canada Ltd
Merck Sharp & Dohme
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Application filed by Merck Frosst Canada Ltd, Merck Sharp & Dohme filed Critical Merck Frosst Canada Ltd
Publication of AR080672A1 publication Critical patent/AR080672A1/es

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Abstract

La presente proporciona pirimidina aminas de formula (1) que son potentes inhibidores de la tirosina quinasa del bazo, y son utiles en el tratamiento y prevencion de enfermedades mediadas por dicha enzima, tales como asma, COPD y artritis reumatoide. Composiciones farmacéuticas. Reivindicacion 1: Un compuesto de formula (1) o una sal farmacéuticamente aceptable del mismo, en la que: p es de 0 a 4; q es 0, 1 o 2; Cy se selecciona entre cicloalquilo C4-7, oxetanilo, pirrolidinilo, piperidinilo y azepanilo; R1 se selecciona entre H, alquilo C1-4, haloalquilo C1-4, cicloalquilo C3-6 y O-alquilo C1-4; R4 se selecciona entre H, alquilo C1-4 y cicloalquilo C3-4; Ry(a) es aminometilo, OH, OCH3, OCH2CH2OH, F, CN, CO2Ra(a), CONRb(a)Rc(a), NRa(a)Ra(a), NHC(O)alquilo C1-3 (opcionalmente sustituido con OH), NHC(O)NH2, NHSO2NH2, NHSO2-alquilo C1-3, o NHSO2-haloalquilo C1-3; Rz(a) se selecciona entre (A) alquilo C1-4 opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre OH, NH2, CN, CO2Ra(a) y CONH2, (B) fluoroalquilo C1-3, (C) halogeno, (D) CN, (E) CO-alquilo C1-4 (opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre ORa(a), CN, CO2Ra(a), CONRa(a)Ra(a) y NRa(a)Ra(a)), (F) CO-fenilo (opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre etinilo, CO2Ra(a), CN, F y OH), (G) CO-cicloalquilo C3-6 (opcionalmente sustituido con OH o CO2Ra(a)), (H) alquil C0-3-CO2Ra(a), (I) -C(O)NRb(a)Rc(a), (J) -ORa(a), (K) -OC(O)Ra(a), (L) -NRb(a)Rc(a), (M) -NHC(O)alquilo C1-4 (opcionalmente sustituido con uno a tres OH o un CONRa(a)Ra(a)), (N) -NHSO2-alquilo C1-3, (O) -NHSO2NH2, (P) oxo, (Q) 1,3,4-oxadiazol-2(3H)-ona, (R) 1,2,4-oxadiazol-5(4H)-ona, (S) SO2NH2, (T) SO2-alquilo C1-3, (U) SO2-haloalquilo C1-3, y (V) SO2Ph; Ra(a) H o alquilo C1-4; Rb(a) y Rc(a) se seleccionan independientemente entre (A) H, (B) cicloalquilo C3-6 opcionalmente sustituido con OH, (C) heteroarilo seleccionado entre imidazolilo, piridilo e indolilo, (D) tetrahidrofuranoilo, (E) bencilo, (F) fenilo opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre (CH2)0-2OH y F, (G1) alquilo C1-4 y (G2) haloalquilo C1-4, en el que cada uno de (G1) y (G2) está opcionalmente sustituido con uno a tres grupos seleccionados independientemente entre (i) OH, (ii) cicloalquilo C3-6 opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre alquilo C1-4, CONH2, CO2H y CH2OH, (iii) CONH2, (iv) SO2NH2, (v) SO2-alquilo C1-4, (vi) heterociclilo monocíclico de 4 a 7 miembros opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre oxo, (CH2)0-2OH y alquilo C1-4, (vii) un heteroarilo de 5 o 6 miembros opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre carboxi, (CH2)0-2OH y alquilo C1-4, (viii) CN, (ix) O-alquilo C1-4, (x) CO2H, (xi) NRa(a)-alquilo C1-4C(O), (xii) fenilo opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre (CH2)0-2OH, SO2NH2, CF3, F y Cl, (xiii) 1-pirrolidinilo opcionalmente sustituido con oxo, (xiv) 1-imidazolidinilo opcionalmente sustituido con oxo, (xv) 1-piperidinilo opcionalmente sustituido con oxo, y (xvi) 4-morfolinilo; o Rb(a) Rc(a) junto con el átomo de nitrogeno al que están unidos forman un heterociclo de 6 o 7 miembros que tiene de 0 a 1 heteroátomo adicional seleccionado entre N, O y S, donde dicho heterociclo está opcionalmente sustituido con uno o dos grupos seleccionados independientemente entre oxo, CN, (CH2)0-2OH, acetilo, bencilo, SO2-alquilo C1-4, CONH2, metoximetilo, carboximetilo, CO2Ra(a) y alquilo C1-4.
ARP100104724A 2009-12-17 2010-12-17 Aminopirimidinas como inhibidores de syk AR080672A1 (es)

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EP (1) EP2513098B1 (es)
JP (2) JP5242857B2 (es)
KR (1) KR101445012B1 (es)
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