BO PENG,BRIAN AQUILA,VICTOR KAMHI,TIMOTHY PONTZ,JAMAL CARLOS SAEH,KUMAR THAKUR,BIN YANG
申请号：
ARP110102793
公开号：
AR089550A1
申请日:
2011.08.02
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
2. Compounds, synthetic drugs and preparation methods: these compounds inhibit the belt activity of ALK, so they can be used in the treatment of cancer. 1. Characteristic requirement 1: a formula compound (1), whose characteristic is: X1 is selected from formula residues (2) and (3)；X2 is selected from - nh-y-n (rent c832131)；R1 is selected from H and c833218331c83248a；wherein said C₁₋₄ alkyl is optionally substituted with one or more hydroxy； R² is selected from H, C₁₋₄ alkyl,C₃₋₆ cycloalkyl and 4-7 membered heterocyclyl, wherein said C₁₋₄ alkyl is optionally substituted with one or more hydroxy； or R¹ and R² together with the nitrogen atom to which they are attached form a 4- to 7-membered heterocyclic ring, wherein said 4- to 7-membered heterocyclic ring is optionally substituted in carbon with one or more R²⁰ and where, if said heterocyclic ring 4 to 7 members contains a remainder -NH-,a. The nitrogen can be changed to r83204 *；R3: from h, halogen and methyl； r83088 from halogen-cn, methyl and trifluoroethane； r83099 from h, halogen and hydrocarbon；R²⁰ in each case is selected from halo and C₁₋₆ alkyl；R²⁰ * is selected from C₁₋₆ alkyl,1.3 to 6 members of cct-s (o) r8304； 7495y-s (o) 8322； - r83047495；and R²⁰ᵇ in each case is independently selected from C₁₋₆ alkyl and 3 to 6 membered carbocyclyl.Compuestos, composiciones farmacéuticas y métodos para su preparación. Estos compuestos inhiben la actividad cinasa de ALK y, por lo tanto, se pueden utilizar para tratar el cáncer. Reivindicación 1: Un compuesto de fórmula (1) caracterizado porque, o una sal farmacéuticamente aceptable de este, donde: X¹ se selecciona entre los restos de fórmula (2) y (3)； X² se selecciona entre -NH- y -N(alquilo C₁₋₄)-； R¹ se selecciona entre H y alquilo C₁₋₄, donde dicho alquilo C₁₋₄ está opcionalmente sustituido con uno o más hidroxi； R² se selecciona entre H, alquilo C₁₋₄, cicloalquilo C₃₋₆ y heterociclilo de 4 a 7 miembros, donde dicho alquilo C₁₋₄ está opcionalmente sustituido co
