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40 条记录 (耗时 0.033 秒)

    Drug delivery formulations and targeting
    22.
    发明授权
    Drug delivery formulations and targeting 失效
    给药配方和靶向

    公开(公告)号：US06680068B2

    公开(公告)日：2004-01-20

    申请号：US09898107

    申请日：2001-07-03

    申请人： Robert B. Campbell ,  Rakesh K. Jain

    发明人： Robert B. Campbell ,  Rakesh K. Jain

    IPC分类号： A61K9127

    CPC分类号： A61K9/127 ,  A61K9/1272 ,  Y10S977/775 ,  Y10S977/808 ,  Y10S977/905 ,  Y10S977/907 ,  Y10S977/915

    摘要： The invention is based on the discovery that angiogenic vessels have heterogeneous surface charge and that cationic liposomes actually target human tumor blood vessels only in irregularly shaped patches. The invention thus features methods for delivering therapeutic compounds to angiogenic vascular endothelial surfaces using a mixture, or “cocktail”, of positively charged and neutral liposomes. The new methods can be used to target multiple regions on the same tumor vessel and/or clusters of vessels within the same tumor. Liposomes with different chemical and/or physical properties (e.g., charge, stability, solubility, diameter) can be delivered simultaneously, and can target tumor vessels and other angiogenic vessels with greater efficiency compared to cationic liposomes alone.

    摘要翻译： 本发明基于以下发现：血管生成血管具有不均匀的表面电荷，并且阳离子脂质体仅在不规则形状的斑块中实际靶向人肿瘤血管。 因此，本发明具有使用正电荷和中性脂质体的混合物或“混合物”将治疗性化合物递送到血管生成血管内皮表面的方法。 新方法可用于靶向同一肿瘤内相同肿瘤血管和/或血管簇的多个区域。 具有不同化学和/或物理性质（例如电荷，稳定性，溶解度，直径）的脂质体可以同时递送，并且与单独的阳离子脂质体相比，可以以更高的效率靶向肿瘤血管和其它血管生成血管。

    Synthetic core 2-like branched structures containing GalNAc-lewis.sup.x and Neu5Ac.alpha.2-3Gal.beta.1-3GalNAc sequences as novel ligands for selectins
    24.
    发明授权
    Synthetic core 2-like branched structures containing GalNAc-lewis.sup.x and Neu5Ac.alpha.2-3Gal.beta.1-3GalNAc sequences as novel ligands for selectins 失效
    含有GalNAc-lewisx和Neu5Acα2-3Galβ1-3GalNAc序列作为选择蛋白的新配体的合成核心2样支链结构

    公开(公告)号：US5972907A

    公开(公告)日：1999-10-26

    申请号：US962113

    申请日：1997-10-31

    申请人： Khushi L. Matta ,  Rakesh K. Jain

    发明人： Khushi L. Matta ,  Rakesh K. Jain

    IPC分类号： C07H15/04 ,  A61K31/00 ,  A61K31/70 ,  A61K31/7028 ,  A61P43/00 ,  C07H3/06 ,  A61K31/715 ,  C07H15/00

    CPC分类号： C07H3/06

    摘要： Compounds which bind to selectin receptors and thus may modulate the course of inflammation, cancer and related processes by intervening with cell-cell adhesion events. Further, such compounds can be used for identification and analysis of such receptors. In this regard the invention is directed to compounds of formula (I). ##STR1## wherein R.sup.1 is independently H, alkyl, aryl, an aryl alkyl, alkenyl or one or more additional saccharide residues; R.sup.2 =H or OH provided that when R.sup.2 is H, R.sup.3 is OH; R.sup.3 =H or OH provided that when R.sup.3 is H, R.sup.2 is OH; X=H, SO.sub.3.sup.- or PO.sub.4.sup.- ; Y is independently H, OH, OR.sup.4 or NHCOR.sup.4, wherein R.sup.4 is alkyl, and Z is an organic acid residue. .alpha.-L-Fucose residue can be modified or replaced with suitable bioisosters or a different saccharide residue such as D-mannose. Modification of L-fucose may include replacement of each or all of the hydroxyl groups with H or OR' wherein R' can be methyl, ethyl or allyl groups.

    摘要翻译： 与选择素受体结合的化合物可通过介入细胞粘附事件来调节炎症，癌症和相关过程的过程。 此外，这些化合物可用于鉴定和分析这些受体。 在这方面，本发明涉及式（I）的化合物。 其中R1独立地为H，烷基，芳基，芳基烷基，烯基或一个或多个另外的糖残基; R2 = H或OH，条件是当R2为H时，R3为OH; R3 = H或OH，条件是当R3为H时，R2为OH; X = H，SO 3 - 或PO 4 - ; Y独立地为H，OH，OR4或NHCOR4，其中R4为烷基，Z为有机酸残基。 α-L-岩藻糖残基可以用合适的生物分子筛或不同的糖残基如D-甘露糖进行修饰或替换。 L-岩藻糖的修饰可以包括用H或OR'取代每个或全部羟基，其中R'可以是甲基，乙基或烯丙基。

    N-formyl hydroxylamines compounds
    27.
    发明授权
    N-formyl hydroxylamines compounds 失效
    N-甲酰羟胺化合物

    公开(公告)号：US08044199B2

    公开(公告)日：2011-10-25

    申请号：US12476824

    申请日：2009-06-02

    申请人： Kathryn Rene Bracken ,  Simon Bushell ,  Karl Dean ,  Charles Francavilla ,  Rakesh K. Jain ,  Kwangho Lee ,  Mohindra Seepersaud ,  Lei Shu ,  Arathi Sundaram ,  Zhengyu Yuan

    发明人： Kathryn Rene Bracken ,  Simon Bushell ,  Karl Dean ,  Charles Francavilla ,  Rakesh K. Jain ,  Kwangho Lee ,  Mohindra Seepersaud ,  Lei Shu ,  Arathi Sundaram ,  Zhengyu Yuan

    IPC分类号： C07D403/02

    CPC分类号： C07D401/12 ,  C07D403/12

    摘要： Novel N-formyl hydroxylamine compounds of formula I: wherein R1 is hydrogen, alkyl, heteroaryl, heterocycloalkyl, aryl, heteroaryl or cycloalkyl; R3 is hydrogen, halogen or alkoxy; R4 is pyridazinyl; n is 0 to 3; and wherein one or more of the ring nitrogen heteroatoms of said pyridazinyl is optionally oxidized and their derivatives are disclosed. These N-formyl hydroxylamine compounds inhibit peptidyl deformylase (PDF), an enzyme present in prokaryotes. The compounds are useful as antimicrobials and antibiotics. The compounds of the invention display selective inhibition of peptidyl deformylase versus other metalloproteinases such as MMPs. Methods of preparation and use of the compounds are also disclosed.

    摘要翻译： 式I的新型N-甲酰基羟胺化合物：其中R 1是氢，烷基，杂芳基，杂环烷基，芳基，杂芳基或环烷基; R3是氢，卤素或烷氧基; R4是哒嗪基; n为0〜3; 并且其中所述哒嗪基的一个或多个环氮杂原子被任选地氧化并且其公开了它们的衍生物。 这些N-甲酰基羟胺化合物抑制肽原甲酰化酶（PDF），一种存在于原核生物中的酶。 这些化合物可用作抗微生物剂和抗生素。 本发明的化合物显示出对其它金属蛋白酶如MMP的肽基变性酶的选择性抑制。 还公开了化合物的制备和使用方法。

    Combinatorial library of moenomycin analogs and methods of producing same
    30.
    发明授权
    Combinatorial library of moenomycin analogs and methods of producing same 失效
    霉酚霉素类似物组合库及其生产方法

    公开(公告)号：US06114309A

    公开(公告)日：2000-09-05

    申请号：US975229

    申请日：1997-11-21

    申请人： Nigel Mark Allanson ,  Tin Yau Chan ,  Nicole T. Hatzenbuhler ,  Rakesh K. Jain ,  Ramesh Kakarla ,  Rui Liang ,  Dashan Liu ,  Domingos J. Silva ,  Michael J. Sofia

    发明人： Nigel Mark Allanson ,  Tin Yau Chan ,  Nicole T. Hatzenbuhler ,  Rakesh K. Jain ,  Ramesh Kakarla ,  Rui Liang ,  Dashan Liu ,  Domingos J. Silva ,  Michael J. Sofia

    IPC分类号： C12Q1/02 ,  A61K31/7016 ,  A61K31/702 ,  A61P31/04 ,  C07B61/00 ,  C07H1/02 ,  C07H5/08 ,  C07H11/04 ,  C07H15/04 ,  C07H15/203 ,  A61K31/70 ,  C07H13/00

    CPC分类号： C07H15/04 ,  C07H15/203 ,  C40B40/00

    摘要： A combinatorial chemical library of compounds structurally related to the moenomycin class of antibiotics has the formula ##STR1## wherein D is a donor mono- or disaccharide, A is an acceptor monosaccharide, and P-R is a lipophosphoglycerate mimetic group. Members of the library have a glycosidic linkage between the anomeric carbon of D and the C2 carbon of A, and the D-A moiety is in turn covalently linked through the anomeric carbon of A to the P-R group. Members of the library exhibit their greatest structural diversity in terms of substitutions occurring at the C3 position of the A residue, substitutions at the C2 position of the D residue, and different P-R groups used in assembling the compounds. Members of the library are preferably synthesized by solid phase techniques involving stepwise coupling of the respective units to a support, functionalizing the A and/or D saccharides either before or after immobilizing them on the support, and cleaving the assembled compounds from the support. Preferred functionalities attached to the sugar residues are amides, carbamates, ureas, sulfonamides, substituted amines, esters, carbonates, and sulfates. Exemplary P-R groups are derivatives of homoserine, glyceric acid, salicylates and mandelic acid. Members of the library can be screened for anti-microbial activity by contacting them with a culture of microbes and monitoring the growth rate of the microbes.

    摘要翻译： 结构上与新霉素类抗生素相关的化合物的组合化学文库具有下式：其中D是供体单糖或二糖，A是受体单糖，P-R是脂磷酸甘油酸酯模拟组。 文库成员在D的异头碳和A的C2碳之间具有糖苷键，D-A部分又通过A的端基异碳共价连接到P-R基团。 关于在A残基的C3位置发生的取代，在D残基的C2位置的取代以及用于组装化合物的不同的P-R基团，图书馆的成员表现出最大的结构多样性。 文库的成员优选通过固相技术合成，其包括将各单元逐步偶联到载体上，在将它们固定在载体上之前或之后将A和/或D糖功能化，并将载体化合物从载体上分离。 附着于糖残基的优选功能是酰胺，氨基甲酸酯，脲，磺酰胺，取代的胺，酯，碳酸酯和硫酸酯。 示例性的P-R基团是高丝氨酸，甘油酸，水杨酸盐和扁桃酸的衍生物。 通过与微生物培养物接触并监测微生物的生长速率，可以筛选图书馆成员的抗菌活性。