Xanthurenic acid derivative pharmaceutical compositions and methods related thereto
申请人：Naturon, Inc.
公开号：US10370335B2
公开（公告）日：2019-08-06
The present invention relates to diuretic pharmaceutical compositions and methods and in particular to certain derivatives of the formula I
wherein R1, R2, R3, R5, R6 and R7 are independently X3R where R is selected from the group consisting of H, halo; optionally substituted saccharide, aliphatic, cycloalkyl, heterocycloalkyl, aryl and heteroaryl; —P(O)(ORa)(ORb) and —NRaRb, where Ra and Rb are independently H, optionally substituted aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl;
X1, X2 and X3 are independently —C(O)O—, —OC(O)—, —C(O)NH—, —NHC(O)—, —OC(O)NH—, —NHC(O)O—, —OS(O)y—, —S(O)y—, —O—, —NHC(O)—, —NHC(O)O—, —S(O)2NH—, a bond or absent; where y is an integer from 0 to 3; and
R4 and R8 are independently H, (═O); hydroxy; or optionally substituted saccharide, aliphatic, cycloalkyl, heterocycloalkyl, aryl or heteroaryl; or —P(O)(ORa)(ORb) or —NRaRb, where Ra and Rb are independently H, or optionally substituted aliphatic, cycloalkyl or heterocycloalkyl, aryl or heteroaryl; or
a prodrug or pharmaceutically acceptable salt thereof; and
a pharmaceutically acceptable carrier.
本发明涉及
利尿药物组合物和方法，尤其涉及式 I 的某些衍
生物
其中 R1、R2、R3、R5、R6 和 R7 独立地为 X3R，其中 R 选自由 H、卤素；任选取代的糖基、脂肪族、环烷基、杂环烷基、芳基和杂芳基；-P(O)(ORa)(ORb) 和 -NRaRb，其中 Ra 和 Rb 独立地为 H、任选取代的脂肪族、环烷基、杂环烷基、芳基或杂芳基；
X1、X2 和 X3 独立地为-C(O)O-、-OC(O)-、-C(O)NH-、-NHC(O)-、-OC(O)NH-、-NHC(O)O-、-OS(O)y-、-S(O)y-、-O-、-NHC(O)-、-NHC(O)O-、-S(O)2NH-、键或不存在；其中 y 为 0 至 3 的整数；以及
R4 和 R8 独立地为 H、(═O)；羟基；或任选取代的糖基、脂肪族、环烷基、杂环烷基、芳基或杂芳基；或-P(O)(ORa)(ORb) 或-NRaRb，其中 Ra 和 Rb 独立地为 H 或任选取代的脂肪族、环烷基或杂环烷基、芳基或杂芳基；或
其原药或药学上可接受的盐；以及
药学上可接受的载体。
