发明名称 DERIVATIVES OF 1-AMINO-2-CYCLOBUTYLETHYLBORONIC ACID
摘要 The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.
申请公布号 US2014194387(A1) 申请公布日期 2014.07.10
申请号 US201414153752 申请日期 2014.01.13
申请人 Millennium Pharmaceuticals, Inc. 发明人 Fleming Paul E.;Li Jing
分类号 C07F5/02;C07F5/04 主分类号 C07F5/02
代理机构 代理人
主权项 1. A compound of formula (I): or a pharmaceutically acceptable salt or boronic acid anhydride thereof, wherein: A is 0, 1, or 2; P is hydrogen or an amino-group-blocking moiety; Ra1 is C1-6 aliphatic, C1-6 fluoroaliphatic, —(CH2)m—CH2—RB, —(CH2)m—CH2—NHC(═NR4)NH—Y, —(CH2)m—CH2—CON(R4)2, —(CH2)m—CH2—N(R4)CON(R4)2, —(CH2)m, —CH(R6)N(R4)2, —(CH2)m—CH(R)—OR5, or —(CH2)m—CH(R5)—SR5; each Ra2 independently is hydrogen, C1-6 aliphatic, C1-6 fluoroaliphatic, —(CH2)m—CH2—RB, —(CH2)m—CH2—NHC(═NR4)NH—Y, —(CH2)m—CH2—CON(R4)2, —(CH2)m—CH2—N(R4)CON(R4)2, —(CH2)m—CH(R6)N(R4)2, —(CH2)m—CH(R5)—OR5, or —(CH2)m—CH(R5)—SR5; each Y independently is hydrogen, —CN, —NO2, or —S(O)2—R10; each RB independently is a substituted or unsubstituted mono- or bicyclic ring system; each R4 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group; or two R4 on the same nitrogen atom, taken together with the nitrogen atom, form a substituted or unsubstituted 4- to 8-membered heterocyclyl ring having, in addition to the nitrogen atom, 0-2 ring heteroatoms independently selected from N, O, and S; each R5 independently is hydrogen or a substituted or unsubstituted aliphatic, aryl, heteroaryl, or heterocyclyl group; each R6 independently is a substituted or unsubstituted aliphatic, aryl, or heteroaryl group; each R10 independently is C1-6 aliphatic, C6-10 aryl, or —N(R4)2; m is 0, 1, or 2; Z1 and Z2 are each independently hydroxy, alkoxy, aryloxy, or aralkoxy; or Z1 and Z2 together form a moiety derived from a boronic acid complexing agent.
地址 Cambridge MA US