发明名称 N-Acylpyrrolidine Ether Tropomyosin-Related Kinase Inhibitors
摘要 The present invention relates to compounds of Formula I;;described herein and their pharmaceutically acceptable salts, and their use in medicine, in particular as Trk antagonists.
申请公布号 US2016221989(A1) 申请公布日期 2016.08.04
申请号 US201514817416 申请日期 2015.08.04
申请人 Pfizer Inc. 发明人 Bagal Sharanjeet Kaur;Omoto Kiyoyuki;Skerratt Sarah Elizabeth;Cui Jingrong Jean;Greasley Samantha Elizabeth;McAlpine Indrawan James;Nagata Asako;Ninkovic Sacha;Tran-Dubé Michelle Bich
分类号 C07D401/12;A61K31/4439 主分类号 C07D401/12
代理机构 代理人
主权项 1. A compound of Formula I: or a pharmaceutically acceptable salt thereof, wherein Q1 is N or CR1, Q2 is N or CR2, R1, R2, R4 and R5 are each independently H, halogen, CN, OH, NH2, C1-3 alkyl optionally substituted by one or more F, C3-7 cycloalkyloxy optionally substituted by one or more F, or C1-3 alkoxy optionally substituted by one or more F, R3 is H, halogen, CN, C1-4 alkyl optionally substituted by one or more F, C1-4 alkoxy optionally substituted by one or more F, C3-7 cycloalkyloxy optionally substituted by one or more F, or C1-4 alkylthio optionally substituted by one or more F, With the proviso that at least 2 of R1, R2, R3, R4 and R5 are H, Y is O, CH2O or OCH2 R6 and R7 can be attached at any point on the ring and are independently H, F, CN, OH, NH2, C1-3 alkyl optionally substituted by one or more F, or C1-3 alkoxy optionally substituted by one or more F, or R6 and R7 can be taken together, with the atoms to which they are attached, to form a 3- to 7-membered cycloalkane ring, X is CR101 or N, R101 is H or C1-3 alkyl, Z is CH2, CH(CH3), NH or O, A is C(O)NR103R104, R103 and R104 are each independently selected from H, (C1-6 alkyl optionally substituted by OH, C1-6 alkoxy, CN or by one or more F), and (C3-7 cycloalkyl optionally substituted by OH, C1-6 alkoxy or by one or more F).
地址 New York NY US