MUTHONI G. KAMAU,KYOUNG S. KIM,LIPING ZHANG,ROBERT M. BORZILLERI,YUFEN ZHAO,BRIAN E. FINK
申请号：
ARP150104241
公开号：
AR103232A1
申请日:
2015.12.21
申请国别(地区):
AR
年份:
2017
代理人:
摘要：
2. Compounds that regulate the activity of tgfbr-1 and tgfbr-2, pharmaceutical compounds containing these compounds, and methods to treat diffuse disorders and uncontrolled doomsday diseases (such as cancer) by using these compounds. Claim 1: a compound (1) having formula properties, wherein R is the remaining part (2) of the formula, or a heterocycle or heterocycle group substituted by 0-4r 2；X1,X2,X3 and x830808 are independent - cr83088；There's at least oneR¹ is hydrogen, C₁₋₆alkyl, C₃₋₈cycloalkyl, -CONHR⁹,-Coordination 8313,-COR⁹ or -SO₂R⁹,Any such substance, except hydrogen, shall be replaced by 0-3r739；Rˣ is hydrogen, halogen, -OH, halo-C₁₋₃alkyl, hydroxy-C₁₋₃alkyl, -amino-C₁₋₃alkyl or -CN； R² is independently one or more of hydrogen, -CD₃,OCD83323,Halogen, cf8323,-CHF₂,-CN, C₁₋₆alkyl, C₁₋₆alkoxy or -SO₂-C₁₋₆alkyl； R³ is independently one or more of hydrogen, CD₃,OCD83323,halogen, -CN, C₁₋₆alkyl, C₂₋₆alkenyl, C₁₋₆alkoxy, C₃₋₈cycloalkyl, hydroxy-C₁₋₃alkyl, C₁₋₆alkylamino-,C₁₋₆alkylamino-C₁₋₆alkyl, 5-6 membered heteroaryl, heterocyclyl, O-heterocyclyl, -NR⁵R⁶,-CONR⁵R⁶,-Coordination 83088；-Cor.8308；-SO₂R⁴,-CHCF COOCH OH o -CHCF CONHExcept for hydrogen, any such substance should be replaced by 0-4 r6966；Rʸ is hydrogen, halogen, -OH, C₁₋₃alkyl, halo-C₁₋₃alkyl, hydroxy-C₁₋₃alkyl, -amino-C₁₋₃alkyl, -NHCOOH or -CN； R⁴ is hydrogen or C₁₋₆alkyl； R⁵ and R⁶ are independently hydrogen, -C (O) alkyl or C₁₋₆alkyl； or R⁵ and R⁶ can be taken together with the nitrogen atom to which they are attached to form a 5-7 membered heterocycle ring； R⁷ is independently one or more of hydrogen, halogen, halo-C₁₋₆alkyl or -CN； R⁸ is hydrogen, C₁₋₆alkyl, C₃₋₈cycloalkyl, -CONHR⁹,-Coordination 8313,-COR⁹ or -SO₂R⁹；R⁹ is hydrogen, C₁₋₆alkyl, C₃₋₈cycloalkyl, heterocyclylalkyl-,heterocyclyl-C₁₋₃alkylamino-C₁₋₃alkyl- or C₁₋₃alkylamino-C₁₋₃alkyl； m is 0, 1, 2, 3 or 4； n is 0, 1, 2 or 3； and / or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof.Compuestos que modulan la activid
