首页> 外国专利> FOERFARANDE Foer FRAMSTAELLNING AV TERAPEUTISKT ANVAENDBARA DISUBSTITUERADE XANTEN- OCH XANTONDERIVAT.

FOERFARANDE Foer FRAMSTAELLNING AV TERAPEUTISKT ANVAENDBARA DISUBSTITUERADE XANTEN- OCH XANTONDERIVAT.

机译:用于制备治疗上有用的取代的黄嘌呤和黄嘌呤衍生物的方法。

摘要

Tricyclic compounds of formula (I) IMAGE (I) wherein X1 is a carboxyl or 5-tetrazolyl group X2 is carbonyl or methylene X3 is hydroxyl or a group -X4(CnH2n)X5 where X4 is oxygen or sulphur X5 is hydrogen or a group -OX6 where X6 is hydrogen, alkanoyl of 1 to 4 carbon atoms or a group -(CmH2m)X7 where X7 is hydrogen or a group -OX8 where X8 is hydrogen or alkanoyl of 1 to 4 carbon atoms and m and n are each, independently, an integer from 1 to 4, together with salts thereof, provided that when X5 is a group -OX6 then n is always greater than 1 and X4 and X5 are attached to different carbon atoms and that when X7 is a group -OX8 then m is always greater than 1 and no single carbon atom in the radical -(CmH2m)- is attached to two oxygen atoms. These compounds are of value in medicine in circumstances where it is desirable to provide a more effective delivery of oxygen to the tissues; in vivo applications include the relief or amelioration of tissue hypoxia as in, for example, cardiac or cerebral ischaemia while in vitro they maintain the oxygen-delivery capacity of stored red blood cells and prolong the cells' useful storage life. The invention is also directed to methods for the preparation of the compounds, to pharmaceutical formulations and other presentation forms containing them and the preparation thereof, to the use of the compound in medicine, and to novel intermediates for the said compounds and the preparation thereof.
机译:式(I)的三环化合物(IIM),其中X 1是羧基或5-四唑基X 2是羰基或亚甲基X 3是羟基或基团-X 4(C n H 2n)X 5,其中X 4是氧或硫X 5是氢或-OX6基团,其中X6是氢,1-4个碳原子的烷酰基或-(CmH2m)X7基团,其中X7是氢或-OX8基团,其中X8是氢或1-4个碳原子的烷酰基,m和n为各自独立地为1至4的整数及其盐,但前提是当X5为-OX6基团时,n始终大于1并且X4和X5连接至不同的碳原子,并且当X7为-碳原子团时OX8则m始终大于1,并且-(CmH2m)-自由基中没有单个碳原子与两个氧原子相连。这些化合物在需要向组织提供更有效的氧气输送的情况下具有重要的医学价值。体内应用包括减轻或改善组织缺氧,例如在心脏或脑缺血中;而在体外,它们可保持储存的红细胞的氧气输送能力并延长细胞的有用储存寿命。本发明还涉及化合物的制备方法,包含它们的药物制剂和其他呈递形式及其制备,化合物在医学中的用途以及所述化合物的新中间体及其制备。

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