COURTER, Joel R.,WU, Liangxing,SHEN, Bo,HE, Chunhong,QIAN, Ding-Quan,WANG, Xiaozhao,YAO, Wenqing,ZHANG, Fenglei
申请号：
PE0014662016
公开号：
PE15732016A1
申请日:
2015.02.12
申请国别(地区):
PE
年份:
2017
代理人:
摘要：
Ciclopropilaminas refers to compounds of formula (i) where the ring a is aryl or heteroaryl C6 C10 5-10 members comprising 1 to 4 heteroatoms selected from N, o and S The Ring B is heterocicloalquilo 4 - 10 members comprising 1 to 3 heteroatoms selected N, o and S The Ring C is aryl C3 C6 C10, cycloalkyl - C10, among others l is alquileno C1 - C4- C (= o) -, among others r1 is alkyl, Halo, C1 - C6, among others R2 is Halo, CN, among others R3 is Halo, alquenilo C2 - C6, among others R4 is c1-c6 alkyl, aryl C6 C10, among others R5 and R6 are H Halo, cianoalquilo c1-c4, among others Q is 0 to 2 RZ is H, alkyl of C1 - C6, among others M is 0 to 2 n and P are 0 to 3.Preferred compounds are: acid, 4 - [(3 - [(2 - {trans} azetidin fenilciclopropil) amino] methyl] - 1 - yl) methyl benzoic acid n - [1 - (4-fluorobenzyl) azetidin - 3 - il] methyl} - trans - 2 - fenilciclopropanamina among others. It also relates to a Pharmaceutical composition.These compounds are inhibitors of the demethylase specific lysines 1 (LSD1) being useful in the treatment of acute Lymphocytic Leukemia, acute myeloid leukemiaSE REFIERE A COMPUESTOS DERIVADOS DE CICLOPROPILAMINAS DE FORMULA (I) DONDE EL ANILLO A ES ARILO C6-C10 O HETEROARILO DE 5-10 MIEMBROS QUE COMPRENDE DE 1 A 4 HETEROATOMOS SELECCIONADOS DE N, O Y S EL ANILLO B ES HETEROCICLOALQUILO DE 4-10 MIEMBROS QUE COMPRENDE DE 1 A 3 HETEROATOMOS SELECCIONADOS DE N, O Y S EL ANILLO C ES ARILO C6-C10, CICLOALQUILO C3-C10, ENTRE OTROS L ES ALQUILENO C1-C4, -C(=O)-, ENTRE OTROS R1 ES HALO, ALQUILO C1-C6, ENTRE OTROS R2 ES HALO, CN, ENTRE OTROS R3 ES HALO, ALQUENILO C2-C6, ENTRE OTROS R4 ES ALQUILO C1-C6, ARILO C6-C10, ENTRE OTROS R5 Y R6 SON H, HALO, CIANOALQUILO C1-C4, ENTRE OTROS q ES DE 0 A 2 RZ ES H, ALQUILO C1-C6, ENTRE OTROS m ES DE 0 A 2 n Y p SON DE 0 A 3. SON COMPUESTOS PREFERIDOS: ACIDO-4-[(3-{[(TRANS-2-FENILCICLOPROPIL)AMINO]METIL}AZETIDIN-1-IL)METIL]BENZOICO N-{[1-(4-FLUOROBENCIL)AZETIDIN-3-IL]METIL}-TRANS-2-FENILCICLOPROPANAMINA ENTR
