发明名称 RAPAMYCIN ANALOGUES AND THEIR PHARMACEUTICAL USE
摘要 Novel rapamycin analogues and methods for their production with FKBP and/or MIP inhibitory activity with reduced mTOR inhibitory activity with therapeutic potential e.g. as bacterial virulence inhibitors.
申请公布号 US2016176893(A1) 申请公布日期 2016.06.23
申请号 US201414902998 申请日期 2014.07.09
申请人 Isomerase Therapeutics Limited 发明人 Gregory Matthew Alan;Kendrew Steven Gary;Moss Steven James;Wilkinson Barrie
分类号 C07D491/052;A61K45/06;A61K31/453;A61K31/436;C07D405/06 主分类号 C07D491/052
代理机构 代理人
主权项 1. A rapamycin analogue of formula (I) or a pharmaceutically acceptable salt thereof. wherein: R1 represents Me or H; R2 and R3 represent H or R2 and R3 taken together represent keto; X1 and X2 are connected by a moiety selected from: or X2 is connected as follows: and X1 is H; or X1 represents H and X2 represents Z; Ra is selected from H, OH and OMe; Z represents Y represents methylene or is absent; M is selected from bond, CH2, CHMe, CHF, CHOH, CH2CH2CH(OMe), CMe2, CHEt and CF2; Q is selected from bond, CH2, CHMe, CHF, CHOH, CH2CH2, 0, S, CHCH2OH, C(OH)Me and CH(OMe); provided that: (i) when Q is not O or S then one of M or Q must represent CHOH CHCH2OH or C(OH)Me; and (ii) if Q is O or S, then M does not represent CHF, CF2, CHOMe, CHOH; and (iii) M and Q do not both represent bond; either R4 represents CH2OH and R5 represents H or R4 represents H and R5 represents CH2OH; and either R6 represents OH, R7 represents NH2 or H and X represents CH; or R6 represents H, R7 represents H and X represents N.
地址 Cambridge GB