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1. 发明授权

US08067467B2 Thiosuccinic acid derivatives and the use thereof 有权
标题翻译：硫代琥珀酸衍生物及其用途
公开(公告)号：US08067467B2
公开(公告)日：2011-11-29
申请号：US11914426
申请日：2006-05-03
申请人： Rajendra Kumar Joshi , Hans-Peter Strebel , Jitka Ulrichová , Thomas J. Schmidt
发明人： Rajendra Kumar Joshi , Hans-Peter Strebel , Jitka Ulrichová , Thomas J. Schmidt
IPC分类号： A61K31/225 , C07C323/02
CPC分类号： C07K14/001 , C07C323/58 , C07K5/0215
摘要： The present invention relates to compounds of the formula (I) wherein X1 and X2 independently represent O, NH or S, R1 and R2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X1 or X2 in this case being NH, and hydrogen, both radicals R1 and R2 preferably not being H, wherein R3 is a residue selected from group consisting of —S—R6, wherein R6 is a C1-C30 hydrocarbyl group, at least one of R1 and R2 not being H when X1 and X2 are oxygen, —S—CH2—CH(NH2)(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group, and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug and drugs containing the same.
摘要翻译：本发明涉及式（I）化合物，其中X 1和X 2独立地表示O，NH或S，R 1和R 2独立地选自C 1 -C 30烃基，通过酰胺键键合的氨基酸或通过酰胺键键合的肽，其各自具有多达200个氨基酸，在这种情况下，缀合的残基X1或X2为NH，氢为自由基R1和R2优选不为H，其中R3为选自的-S-R 6，其中R 6是C 1 -C 30烃基，当X 1和X 2是氧时，R 1和R 2中的至少一个不是H，-S-CH 2 -CH（NH 2）（COOH）（半胱氨酸-S- （例如N-乙酰半胱氨酸-S-基），具有至多200个氨基酸的肽，其含有至少一个具有硫醇基的氨基酸基团，优选半胱氨酸基团，并通过硫硫，优选经由半胱氨酸硫（肽-S-基），辅酶A，其通过硫醇基或脆片键合通过硫醇基键合的酰基载体蛋白和通过硫醇基键合的二氢硫辛酸及其药学上可接受的盐。本发明还涉及这些化合物用于制备药物的用途和含有这些化合物的药物。

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