首页> 外国专利> COMPOUNDS IN THE FORM OF HOMODIMERIC OR HETERODIMERIC PROPHARMACTS, PROCEDURE TO OBTAIN THESE PROFARMACTS AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND USE OF THE COMPOUNDS IN THE TREATMENT OF DISEASES OR DYSFUNCTION MEDIATED BY PHOSPHODIESTERS.

COMPOUNDS IN THE FORM OF HOMODIMERIC OR HETERODIMERIC PROPHARMACTS, PROCEDURE TO OBTAIN THESE PROFARMACTS AND THEIR PHARMACEUTICALLY ACCEPTABLE SALTS AND USE OF THE COMPOUNDS IN THE TREATMENT OF DISEASES OR DYSFUNCTION MEDIATED BY PHOSPHODIESTERS.

机译:均聚物或杂二聚物预示形式的化合物,获得这些预示及其药学上可接受的盐的方法,以及该化合物在治疗由细菌引起的疾病或功能障碍中的用途。

摘要

Homodimeric or heterodimeric prodrugs in which the monomer units are compounds of 1,6-dihydro-7H-pyrazolo [4,3-d] pyrimidin-7-one of the formula: (See formula) where R1 can be -H, - C1-C6 alkyl, -C1-C6-OH, or -C1-C6-NHR ", where R" may be -H, or -C1-C6 alkyl; R2 can be -H, -C1-C6 alkyl, -C1-C6-OH, or -C1-C6-NR '', where R '' can be -H, or -C1-C6 alkyl; where R3 is: (See formula) where R4 can be -H, C1-C6 alkyl, -C1-C6-OH or C1-C6-NHR '', where R '' can be -H, or C1- alkyl C6-; and R5 can be -H, -OH, -NHR '', -C1-C6 alkyl, -C1-C6-OH or C1-C6-NHR '', where R '' can be -H or C1-C6 alkyl- ; or R5 can be: (See formula) where R6 can be H, morpholine, piperidine, hydroxyalkylpiperazine, aminoalkylpiperazine, where alkyl can be from C1 to C6; in which the monomer units are linked together by bridges that are selected from the group consisting of carbonate (-O-COO-), carbamate (-O-CO-N-), urea (-N-CO-N-) or phosphate (-O-POO-O-), and in which the active drug is generated after excision "in vivo" of the bridges.
机译:单体单元为1,6-二氢-7H-吡唑并[4,3-d]嘧啶7-的化合物的同二聚或杂二聚前药,下式之一:(参见式)其中R1为-H,-C1 -C6烷基,-C1-C6-OH或-C1-C6-NHR“,其中R”可以是-H或-C1-C6烷基; R 2可以是-H,-C 1 -C 6烷基,-C 1 -C 6 -OH或-C 1 -C 6 -NR”,其中R”可以是-H或-C 1 -C 6烷基;其中R3是:(参见式)其中R4可以是-H,C1-C6烷基,-C1-C6-OH或C1-C6-NHR'',其中R''可以是-H或C1-烷基C6- ;和R5可以是-H,-OH,-NHR'',-C1-C6烷基,-C1-C6-OH或C1-C6-NHR'',其中R''可以是-H或C1-C6烷基- ;或R5可以是:(参见式),其中R6可以是H,吗啉,哌啶,羟烷基哌嗪,氨基烷基哌嗪,其中烷基可以是C1至C6;其中单体单元通过选自碳酸盐(-O-COO-),氨基甲酸酯(-O-CO-N-),尿素(-N-CO-N-)或磷酸盐的桥连接在一起(-O-POO-O-),其中活性药物是在桥“体内”切除后产生的。

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