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    • 42. 发明申请
    • SURFACTANT CARBON HYDRATE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
    • 表面活性剂碳水化合物衍生物及其制备方法
    • WO1986002076A1
    • 1986-04-10
    • PCT/AT1985000036
    • 1985-10-01
    • EVIDENZBÜRO ÖSTERREICHISCHER ZUCKERFABRIKEN ...GREBER, GerdGRUBER, Heinrich
    • EVIDENZBÜRO ÖSTERREICHISCHER ZUCKERFABRIKEN ...
    • C07H15/04
    • C07H15/04C07H15/06C08B31/125
    • New carbon hydrate derivatives having the formula (I) are disclosed, wherein X1 is H, X, CH3, C2H5, CH2CH2OH, CH2CH(OH)CH3, CH2CH(OH)CH2OH, (A), or represents soluble starch rests with a medium molecular weight comprised between 1'000 and 30'000 and at least one X represents bound beta -alkylamido- or beta -N-alkylurea groups similar to ethers having the formula (II) wherein R1 and R2 are H, CH3, -(CH2)n-CH3, (n = 1-8) or branched aliphatic rests having from 3 to 10 atoms of carbon and Y is R3 or -NH-R3, R3 representing a linear or branched aliphatic rest having from 1 to 20 atoms of carbon and the other X, representing hydrogen. The new carbon hydrate derivatives (I) may be prepared by reacting the corresponding carbon hydrate derivatives (III) which have at least one ether-like bound beta -amynoethyl group having the general formula (IV) with an alkylcarbon acid or an alkylcarbon acid derivative, respectively an alkylisocyanate having the formula (V) or the formula (VI), wherein R3 has the meaning given hereabove and Z is hydroxy, halogen, alkoxy or alkoxy carbonyl. The new carbon hydrate derivatives (I) are excellent tensioactive agents which are very stable to hydrolysis, and which may be prepared in a simple way and are totally biodegradable.
    • 公开了具有式(I)的新的碳水化合物衍生物,其中X1是H,X,CH3,C2H5,CH2CH2OH,CH2CH(OH)CH3,CH2CH(OH)CH2OH,(A),或表示可溶性淀粉与中等 分子量在1 000至30 000之间,至少1个X表示与式(II)的醚类似的结合的β-烷基酰胺基或β-N-烷基脲基团,其中R 1和R 2为H,CH 3, - (CH 2 )n-CH 3,(n = 1-8)或具有3至10个碳原子的支链脂肪族残基,Y是R 3或-NH-R 3,R 3表示具有1至20个碳原子的直链或支链脂族基 而另一个X代表氢。 新的碳水化合物衍生物(I)可以通过使具有至少一个具有通式(Ⅳ)的醚状结合的β-氨基乙基的相应碳水化合物衍生物(III)与烷基碳酸或烷基碳酸衍生物 分别具有式(V)或式(VI)的烷基异氰酸酯,其中R 3具有上文给出的含义,Z是羟基,卤素,烷氧基或烷氧基羰基。 新的碳水化合物衍生物(I)是对水解非常稳定的优异的张力活性剂,可以以简单的方式制备并且是完全可生物降解的。
    • 47. 发明申请
    • METHODS FOR PREPARATION OF GLYCOSPHINGOLIPIDS AND USES THEREOF
    • 制备糖苷类化合物的方法及其用途
    • WO2012094540A3
    • 2012-08-30
    • PCT/US2012020388
    • 2012-01-05
    • LIANG PI-HUIUNIV NAT TAIWAN
    • LIANG PI-HUI
    • C07H15/06A61K39/39A61P31/04A61P31/12A61P35/00C07H15/04C07H15/18
    • C07H1/00A61K39/39C07B2200/07C07H15/04C07H15/06C07H15/18Y02P20/55A61K31/7028A61K31/715
    • Methods for synthesis and preparation of alpha-glycosphingolipids are provided. Methods for synthesis of a-galactosyl ceramides, and pharmaceutically active analogs and variants thereof are provided. Novel alpha-glycosphingolipids are provided, wherein the compounds are immunogenic compounds which serve as ligands for NKT (natural killer T) cells. A process for preparing a chiral compound comprising an R-form or S- form of a glycosphingolipid of formula (1 ) is provided, wherein R1=OH, NH2, NHCOR2, R2 = H or an alkyl, alkenyl, or alkyl terminating in aryl, substituted aryl, heteroaryl, or substituted heteroaryl, X=alkyl group, R3= OH or H, R4=OH or H, R5= aryl, substituted aryl, heteroaryl, or substituted heteroaryl, or a pharmaceutically acceptable salt thereof, wherein the compound of formula 1 is prepared by (a) deprotecting a compound of formula (2): wherein PG is a hydroxyl protecting group, with hydrogen under hydrogenation catalysis.
    • 提供了α-糖苷脂的合成和制备方法。 提供了α-半乳糖苷类神经酰胺的合成方法及其药物活性类似物及其变体。 提供了新的α-糖苷脂,其中所述化合物是用作NKT(天然杀伤T)细胞配体的免疫原性化合物。 提供了制备包含式(1)的R型或S-形式的鞘糖脂的手性化合物的方法,其中R 1 = OH,NH 2,NHCOR 2,R 2 = H或烷基,烯基或烷基,其末端芳基 ,取代的芳基,杂芳基或取代的杂芳基,X =烷基,R 3 = OH或H,R 4 = OH或H,R 5 =芳基,取代的芳基,杂芳基或取代的杂芳基或其药学上可接受的盐, 通过(a)在氢化催化下用氢去除保护式(2)的化合物:其中PG是羟基保护基。