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公开(公告)号：US20100256087A1
公开(公告)日：2010-10-07
申请号：US12676394
申请日：2008-08-27
IPC分类号： A61K31/7064 , C07H19/24 , A61P31/12
CPC分类号： C07K9/003 , A61K47/542 , A61K47/64 , C07H19/24 , C07H23/00 , C07K5/0808
摘要： A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H—[R4-R5]n—R6—, in which: H—[R4-R5]n— comprises an oligopeptide, R4 being an amino acid and R5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R6 is a neutral, non-polar amino acid moiety that is bonded to R5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R3 and R2 is H—[R4-R5]n-R6— or H; or a pharmaceutically acceptable salt thereof.
摘要翻译： 通式（III）的化合物：其中X是O，S，NH或CH 2; Y是O，S或NH; Z是O，S或CH 2; R1是C1-8烷基，特别是C1-6烷基，优选正烷基，例如正戊基或正己基; R2和R3中的至少一个是H- [R4-R5] n-R6-，其中：H- [R4-R5] n-包含寡肽，R4是氨基酸，R5是选自脯氨酸 ，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸，R6是中性，非极性氨基 通过肽键与R5结合的酸部分，n为1,2,3,4或5; R3和R2中的另一个是H- [R4-R5] n-R6-或H; 或其药学上可接受的盐。
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公开(公告)号：US08513215B2
公开(公告)日：2013-08-20
申请号：US12676394
申请日：2008-08-27
IPC分类号： C07H19/24
CPC分类号： C07K9/003 , A61K47/542 , A61K47/64 , C07H19/24 , C07H23/00 , C07K5/0808
摘要： A compound of the general formula (III): wherein X is O, S, NH or CH2; Y is O, S or NH; Z is O, S or CH2; R1 is C1-8 alkyl, especially C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl; at least one of R2 and R3 is H—[R4-R5]n—R6—, in which: H—[R4-R5]n— comprises an oligopeptide, R4 being an amino acid and R5 being an amino acid selected from proline, alanine, hydroxyproline, dihydroxyproline, thiazolidinecarboxylic acid (thioproline), dehydroproline, pipecolic acid (L-homoproline), azetidinecarboxylic acid, aziridinecarboxylic acid, glycine, serine, valine, leucine, isoleucine and threonine, R6 is a neutral, non-polar amino acid moiety that is bonded to R5 by a peptide bond, and n is 1, 2, 3, 4 or 5; and the other of R3 and R2 is H—[R4-R5]n-R6— or H; or a pharmaceutically acceptable salt thereof.
摘要翻译： 通式（III）的化合物：其中X是O，S，NH或CH 2; Y是O，S或NH; Z是O，S或CH 2; R1是C1-8烷基，特别是C1-6烷基，优选正烷基，例如正戊基或正己基; R2和R3中的至少一个是H- [R4-R5] n-R6-，其中：H- [R4-R5] n-包含寡肽，R4是氨基酸，R5是选自脯氨酸 ，丙氨酸，羟脯氨酸，二羟脯氨酸，噻唑烷羧酸（硫脯氨酸），脱氢脯氨酸，哌可酸（L-高脯氨酸），氮杂环丁烷羧酸，氮丙啶羧酸，甘氨酸，丝氨酸，缬氨酸，亮氨酸，异亮氨酸和苏氨酸，R6是中性，非极性氨基 通过肽键与R5结合的酸部分，n为1,2,3,4或5; R3和R2中的另一个是H- [R4-R5] n-R6-或H; 或其药学上可接受的盐。
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