发明名称 L-GLUTAMIC ACID AND L-GLUTAMINE DERIVATIVE (III), USE THEREOF AND METHOD FOR OBTAINING THEM
摘要 The present invention relates to fluorinated glutamic acid (glutamate) and glutamine derivatives wherein the fluorine atom is 19F. The glutamic acid (glutamate) and glutamine derivatives are compound(s) of general Formula I, which encompasses all possible diastereoisomers and/or enantiomere derivatives or mixtures thereof.
申请公布号 US2014227191(A1) 申请公布日期 2014.08.14
申请号 US201414257431 申请日期 2014.04.21
申请人 BAYER SCHERING PHARMA AKTIENGESELLSCHAFT 发明人 DINKELBORG Ludger;SCHMITT-WILLICH Heribert;GRAHAM Keith;KOGLIN Norman;BERNDT Mathias;FRIEBE Matthias;MULLER Andre
分类号 C07C229/24;C07C227/16;A61K49/10 主分类号 C07C229/24
代理机构 代理人
主权项 1. Compound of the general Formula I wherein A is a) Hydroxyl, b) branched or unbranched C1-C5 alkoxy, c) branched or unbranched Hydroxy C1-C5 Alkoxy, d) branched or unbranched O—C1-C5 Alkyl-(O—C1-C4 alkyl)n-O—C1-C4 alkyl, e) N(C1-C5 Alkyl)2, f) NH2, g) N(H)-L, h) O-L or i) O—Z, and G is a) Hydroxyl, b) O—Z b) branched or unbranched O—C1-C5 Alkyl, c) branched or unbranched O—C2-C5 Alkenyl, d) branched or unbranched O—C1-C5 Alkyl-(O—C1-C4 alkyl)n-O—C1-C4 alkyl or e) branched or unbranched O—C2-C5 Alkinyl, and R1 and/or R2, independently separate are a) Hydrogen, b) branched or unbranched 19F—C1-C10 Alkoxy, c) branched or unbranched 19F—C1-C10 Alkyl, d) branched or unbranched 19F—C2-C10 Alkenyl, e) branched or unbranched 19F—C2-C10 Alkinyl, f) substituted or unsubstituted 19F—C6-C10 mono- or bicyclic Aryl, g) substituted or unsubstituted 19F-alkyl-C6-C10 mono- or bicyclic Aryl h) substituted or unsubstituted 19F—C5-C10 mono- or bicyclic Heteroaryl, i) substituted or unsubstituted 19F-alkyl-C5-C10 mono- or bicyclic Heteroaryl j) substituted or unsubstituted 19F—C3-C6 Cyclo-Alkyl, k) substituted or unsubstituted 19F-alkyl-C3-C6 Cyclo-Alkyl l) Hydroxyl, m) branched or unbranched C1-C5 Alkyl or n) branched or unbranched C1-C5 Alkoxy wherein alkyl is optionally interrupted or is replaced by O, S or N, with the proviso that one of the substituent R1 or R2 comprises 19F atom and the other substituent comprises no 19F atom, and L is a) branched or unbranched C1-C5 Alkyl, b) branched or unbranched C2-C5 Alkenyl, c) branched or unbranched C1-C5 Alkyl-(O—C1-C4 alkyl)n-O—C1-C4 alkyl or d) branched or unbranched C2-C5 Alkinyl, and Z is a metal ion equivalent, with the meaning of n=0, 1, 2 or 3, and wherein mixtures of all possible diastereomers and/or enantiomers as well as enantiomerically pure compounds and pharmaceutical salts thereof are comprised.
地址 Berlin DE