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    Deoxynojirimycin and D-arabinitol analogs and methods of using
    1.
    发明授权
    Deoxynojirimycin and D-arabinitol analogs and methods of using 有权
    脱氧野尻霉素和D-阿拉伯糖醇类似物及其使用方法

    公开(公告)号：US08975280B2

    公开(公告)日：2015-03-10

    申请号：US11752015

    申请日：2007-05-22

    申请人： Terry D. Butters ,  Raymond A. Dwek ,  George W. J. Fleet

    发明人： Terry D. Butters ,  Raymond A. Dwek ,  George W. J. Fleet

    IPC分类号： A61K31/445 ,  C07D211/48 ,  C07D211/46

    CPC分类号： C07D211/48 ,  C07D211/46

    摘要： A compound of Formula I are provided: wherein R is: R1 is a substituted or unsubstituted alkyl group; W1-4 are independently selected from hydrogen, substituted or unsubstituted alkyl groups, substituted or unsubstituted haloalkyl groups, substituted or unsubstituted alkanoyl groups, substituted or unsubstituted aroyl groups, or substituted or unsubstituted haloalkanoyl groups; X1-5 are independently selected from H, NO2, N3, and NH2; Y is absent or is a substituted or unsubstituted C1-alkyl group, other than carbonyl; Z is selected from a bond or NH, provided that when Z is a bond, Y is absent, and provided that when Z is NH, Y is a substituted or unsubstituted C1-alkyl group, other than carbonyl. Also provided are D-arabinitol compounds, methods for preparing such compounds and compositions of such compounds, and methods of using such compounds.

    摘要翻译： 提供式I化合物：其中R是：R 1是取代或未取代的烷基; 取代或未取代的烷基，取代或未取代的烷酰基，取代或未取代的烷酰基，取代或未取代的芳酰基，或取代或未取代的卤代烷酰基; X1-5独立地选自H，NO2，N3和NH2; Y不存在或是除羰基以外的取代或未取代的C 1 - 烷基; Z选自键或NH，条件是当Z为键时，Y不存在，条件是当Z为NH时，Y为除羰基以外的取代或未取代的C 1 - 烷基。 还提供了D-阿拉伯糖醇化合物，制备这些化合物的方法和这些化合物的组合物，以及使用这些化合物的方法。

    Heptitols
    4.
    发明授权
    Heptitols 失效
    七肽

    公开(公告)号：US5384417A

    公开(公告)日：1995-01-24

    申请号：US181716

    申请日：1994-01-18

    申请人： George W. J. Fleet ,  Bryan G. Winchester

    发明人： George W. J. Fleet ,  Bryan G. Winchester

    IPC分类号： C07D207/12 ,  C07D307/20

    CPC分类号： C07D207/12

    摘要： Novel heptitol analogues of mannofuranose and their syntheses from .delta.-lactones of heptonic acids are disclosed. The novel heptitols are (A) 2,5-dideoxy-2,5-imino-D-glycero-D-talo-heptitol and (b) 1-amino-2,5-anydro-1-deoxy-D-glycero-D-talo-heptitol. These novel heptitol compounds are useful inhibitors of glycosidases.

    摘要翻译： 公开了甘露糖醛糖的新型七糖醇类似物及其由庚糖酸的β-内酯的合成。 新型的庚硫醇是（A）2,5-二脱氧-2,5-亚氨基-D-甘油基-D-木糖醇和（b）1-氨基-2,5-脱氧-1-脱氧-D-甘油基 - D-谷 - 七糖醇。 这些新型的庚糖醇化合物是糖苷酶的有用抑制剂。

    Synthesis of nojirimycin derivatives
    5.
    发明授权
    Synthesis of nojirimycin derivatives 失效
    nojirimycin衍生物的合成

    公开(公告)号：US5248779A

    公开(公告)日：1993-09-28

    申请号：US949953

    申请日：1992-09-24

    申请人： George W. J. Fleet

    发明人： George W. J. Fleet

    IPC分类号： C07D211/46 ,  C07D211/74 ,  C07H11/00 ,  C07H15/18

    CPC分类号： C07H15/18 ,  C07D211/46 ,  C07D211/74 ,  C07H11/00

    摘要： Nojirimycin .delta.-lactam and deoxynojirimycin are each synthesized from 5,6-anhydro-3-O-benzyl-1,2-O-isopropylidene-L-idofuranose as a divergent intermediate by a method which comprises formation of the piperidine ring by connection of nitrogen between C-1 and C-5 with inversion of configuration at C-5 to form nojirimycin .delta.-lactam or between C-2 and C-6 with inversion of configuration at C-2.

    摘要翻译： 诺依霉素三聚体内酰胺和脱氧野尻霉素分别由5,6-脱氢-3-O-苄基-1,2-邻异丙叉基-L-异呋喃糖作为发散中间体合成，包括通过连接形成哌啶环 C-1和C-5之间的氮，C-5反型构型，以形成NojirimycinΔ-内酰胺，C-2和C-6之间形成C-2反型。

    D-rhamnono-1,5-lactone
    6.
    发明授权
    D-rhamnono-1,5-lactone 失效
    D-鼠李糖-1,5-内酯

    公开(公告)号：US5210089A

    公开(公告)日：1993-05-11

    申请号：US830826

    申请日：1992-02-04

    申请人： George W. J. Fleet ,  Bryan G. Winchester

    发明人： George W. J. Fleet ,  Bryan G. Winchester

    IPC分类号： C07D211/76

    CPC分类号： C07D211/76

    摘要： The novel D-rhamnono-? ,5-lactone and a novel method of synthesis of said compound from the monoacetonide of L-gulono-.gamma.-lactone is disclosed. D-Rhamnono-1,5-lactone is a potent inhibitor of .alpha.-and .beta.-mannosidases but not of .alpha.-rhamnosidase.

    摘要翻译： 小说D-rhamnono- 公开了从L-古洛糖-γ-内酯的单丙酮化合物合成所述化合物的新方法。 D-鼠李糖-1,5-内酯是α-和β-甘露糖苷酶的有效抑制剂，但不是α-鼠李糖苷酶。

    Synthesis of mannojirimycin derivatives
    8.
    发明授权
    Synthesis of mannojirimycin derivatives 失效
    mannojirimycin衍生物的合成

    公开(公告)号：US5101027A

    公开(公告)日：1992-03-31

    申请号：US628523

    申请日：1990-12-17

    申请人： George W. J. Fleet ,  Ian Bruce

    发明人： George W. J. Fleet ,  Ian Bruce

    IPC分类号： C07D487/04 ,  C07D491/22 ,  C07F7/18

    CPC分类号： C07D487/04 ,  C07F7/1856

    摘要： .alpha.-Homojirimycin and 6-dpi-homojirimycin are each synthesized from 2 az ido-2-deoxy-3,4:6,7-di-O-isopropylidene-D-glycero-D-talo-heptono-1,5-lactone in which the side chain acetonide is hydrolyzed to give the corresponding diol which is then protected with a silyl protecting agent to form a silyl ether. The latter compound is used as a divergent intermediate in which the piperidine ring is formed by joining the nitrogen function at C-2 to C-6 (A) with inversion of configuration at C-6 to form 6-epi-homomannojirimycin or (B) with retension of configuration at C-6 to form .alpha.-homomannojirimycin.

    摘要翻译： α-Homojirimycin和6-dpi-homojirimycin分别由2α偶氮-2-脱氧-3,4：6,7-二-O-异亚丙基-D-甘油基-D-庚酰基-1,5- 其中侧链缩酮化合物被水解得到相应的二醇，然后用甲硅烷基保护剂保护以形成甲硅烷基醚。 后一种化合物用作发散中间体，其中哌啶环通过在C-2至C-6（A）处连接氮官能团并以C-6的构型反转形成6-外延 - 同型异丙酰霉素或（B ），在C-6处具有延长的配置以形成α-低聚单元霉素。