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    • 5. 发明授权
    • Sphingosine analogues
    • 鞘氨醇类似物
    • US06235912B1
    • 2001-05-22
    • US09380647
    • 1999-10-15
    • Kazutoh TakesakoToru KuromeNaoyuki AwazuIkunoshin Kato
    • Kazutoh TakesakoToru KuromeNaoyuki AwazuIkunoshin Kato
    • C07C23100
    • C07D307/33C07C215/10C07C215/24C07C229/22C07C229/30C07C237/08C07C237/22C07C251/08C07C271/22C07D263/06Y02P20/55
    • The present invention aims to provide a novel sphingosine analogue, which is useful as an intermediate for syntheses of novel lipid derivatives such as sphingolipid derivatives and the like that can regulate the effects of sphingolipid. The present invention relates to a sphingosine analogue represented by the general formula (I) described below. In the formula, as for Q1, Q2 and Q3, Q1 and Q2, which are the same or different each other, are hydrogen, alkyl groups having 1-4 of carbon atoms, acyl groups having 2-5 of carbon atoms, or protecting groups of the amino group, and Q3 is a hydrogen or a protecting group of the hydroxyl group; or Q2 and Q3 make up an isopropylidene group and Q1 is a hydrogen or a protecting group of the amino group. Q4 and Q5, which are the same or different each other, are hydroxyl groups, acyl groups having 2-5 of carbon atoms, —O—Q6, or hydrogen; or Q4 and Q5 make up a covalent bond. Q6 is a protecting group of the hydroxyl group. X1 is —COOH, —CONH2, —CO—Q7, —CH2OH, or —CH2O—Q8. Q7 is a protecting group of the carboxyl group, and Q8 is a protecting group of the hydroxyl group.
    • 本发明的目的在于提供一种新颖的鞘氨醇类似物,其可用作合成新型脂质衍生物的中间体,例如可以调节鞘脂的作用的鞘脂衍生物等。本发明涉及一般的鞘氨醇类似物 在该式中,对于Q1,Q2和Q3,Q1和Q2彼此相同或不同,为氢,具有1-4个碳原子的烷基,酰基具有2- 5个碳原子或氨基的保护基,Q3为氢或羟基的保护基; 或Q2和Q3构成异亚丙基,Q 1为氢或氨基的保护基。 Q4和Q5彼此相同或不同,是羟基,具有2-5个碳原子的酰基,-O-Q6或氢; 或Q4和Q5构成共价键。 Q6是羟基的保护基。 X 1是-COOH,-CONH 2,-CO-Q 7,-CH 2 OH或-CH 2 O-Q 8。 Q7是羧基的保护基,Q8是羟基的保护基。