BEHENNA, Douglas Carl,CHEN, Ping,FREEMAN-COOK, Kevin Daniel,HOFFMAN, Robert Louis,JALAIE, Mehran,NAGATA, Asako,NAIR, Sajiv Krishnan,NINKOVIC, Sacha,ORNELAS, Martha Alicia,PALMER, Cynthia Louise,RUI, E
申请号：
PE2019000359
公开号：
PE20190475A1
申请日:
2017.07.31
申请国别(地区):
PE
年份:
2019
代理人:
摘要：
It refers to formulation compounds (I) or pharmacologically acceptable formulation salts, in which R1 is an isomer substituting member 3 to 10； R2 is an independent F, O, C1-C4 tar； R3 is an H, F, CL, NH2, C1-C4 tar or C1-C4 calcium fluoride containing tar. C1-C4 and C1-C4 fluoropropyl sulfonates can be replaced by OH； alcoxi et al. of CN, C1-C4； tar of R4 for H, C1-C2 or fluoroquine of C1-C2； tar of R2A and R2B are independent H, OH or C1-C4； tar of P is 0.1, 2 or 4； Q is 0.1, 2 or 3； R is 0, 1 or 2. The most popular compound is 8-cyclopentyl-2-[1-(methylsulfur) piperidin-4-il] amine} pirido [2,3-d] pirimidin-7 (8h) -ona；4 - ({6 - (2-hydroxitil) - 8 - [(1R, 2S) - 2-methycyclopentil] - 7-oxo-7, 8-dihydropirid [2, 3-d] pirimidin-2-il} amino) - n-methylpiperidin-1-sulfonamida. These compounds inhibit the activity of CDK2, including CDK2, CDK4 and/or CDK6. He also mentioned a pharmacological synthesis that is useful for treating abnormal cell growth, especially breast and ovarian cancer.Se refiere a compuestos de las formulas (I) o una sal farmaceuticamente aceptable del mismo, en donde: R1 es heterociclilo de 3 a 10 miembros sustituido； R2 es independientemente F, OH, alquilo de C1-C4, entre otros； R3 es H, F, Cl, NH2, alquilo de C1-C4 o fluoroalquilo de C1-C4, en donde el alquilo de C1-C4 y fluoroalquilo de C1-C4 se sustituyen opcionalemente por OH； CN, alcoxi de C1-C4, entre otros； R4 es H, alquilo de C1-C2 o fluoroalquilo de C1-C2； R2A y R2B son independientemente H, OH o alquilo de C1-C4； p es 0,1, 2, 3 o 4； q es 0,1, 2 o 3； r es 0, 1 o 2. Son compuestos preferidos 8-ciclopentil-2-{[1-(metilsulfonil) piperidin-4-il] amino}pirido[2,3-d]pirimidin-7(8H)-ona； 4-({6-(2-hidroxietil)-8-[(1R,2S)-2-metilciclopentil]-7-oxo-7,8-dihidropirido[2,3-d]pirimidin-2-il}amino)-N-metilpiperidin-1-sulfonamida. Dichos compuestos pueden inhibir la actividad de CDK2, incluyendo CDK2, CDK4 y/o CDK6. Tambien se refiere a una composicion farmaceutica que es util para el tratamiento de creci
