发明名称 IMMUNOSUPPRESSIVE COMPOUNDS AND THERAPEUTICS
摘要 Here provided are new immunosuppressive compounds and novel therapeutics for improving tissue transplantation.
申请公布号 US2016175281(A1) 申请公布日期 2016.06.23
申请号 US201414907015 申请日期 2014.07.23
申请人 UNIVERSITY OF TENNESSE RESEARCH FOUNDATION ;RXBIO, INC. 发明人 Miller Duane Douglas;Yates Charles Ryan
分类号 A61K31/365;A61K31/665 主分类号 A61K31/365
代理机构 代理人
主权项 1. A method for improving survival and function of a transplanted tissue, comprising administering to the tissue a therapeutically-effective amount of mycophenolic acid or its derivative or pro-drug thereof, and a compound of Formula I:wherein: (i) the ring may be singly, doubly, or completely saturated; (ii) R1, R2, R3, R4, R5, R6, R7, R8, and R9 are each independently selected from the group consisting of: a) H or OH;b) a straight- and branched-chain alkyl having one to twelve carbon atoms;c) an alkylidene that is a divalent radical having one to twelve carbon atoms;d) an alkenyl that is straight- and branched-chain alkenyl groups having from two to twelve carbon atoms;e) an alkynyl that is straight- and branched-chain alkynyl groups having from two to twelve carbon atoms;f) a cycloalkyl that is saturated or partially unsaturated carbocycles having from three to twelve carbon atoms, including bicyclic and tricyclic cycloalkyl structures;g) a heterocycloalkyl that is a saturated or partially unsaturated monocyclic radical containing carbon atoms, preferably with 4 or 5 ring carbon atoms, and with at least one heteroatom selected from nitrogen, oxygen (e.g., monosaccharide) and sulfur;h) an aryl or heteroaryl that have monocyclic and polycyclic unsaturated or aromatic ring structures, with “aryl” referring to those that are carbocycles and “heteroaryl” referring to those that are heterocycles;i) an alkoxy that is a radical —O-alkyl;j) an aryloxy;k) a cycloalkoxyl;l) an alkylthio;m) an alkylamino;n) an arylthio;o) an arylamino;p) a cycloalkylthio;q) a cycloalkylamino;r) a heteroarylthio;s) a heteroarylamino;t) a halogen; wherein every member in each group can be taken independently or combined via covalent bond in any order with some or all members of any group defined above to the extent that these combinations give rise to chemically feasible entities; and wherein each of the groups ‘b’ through ‘s’ can contain or be substituted by any one or more functional groups taken from the functional group pool listed below either singularly, in plurality or in combination with other members of the functional group, which functional group pool is consisting of ether, thioether, amine, nitro, nitrile, sulfoxides, sulfones, ester, amide, hydroxamic acid, sulfonamides, sulfamide, ureas, sulfimines, sulfonylureas, carbamates, thiocarbamates, carbonates and hydroxyl.
地址 Memphis TN US