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    Hesperetin pro-forms with enhanced bioavailablility
    85.
    发明授权
    Hesperetin pro-forms with enhanced bioavailablility 失效
    Hesperetin原型具有增强的生物利用度

    公开(公告)号：US06831098B1

    公开(公告)日：2004-12-14

    申请号：US09890479

    申请日：2002-02-08

    Applicant: Jan E. Zielinski

    Inventor： Jan E. Zielinski

    IPC: A61K31352

    CPC classification number: C07D311/32

    Abstract: A hesperitin pro-form is provided. The invention provides both a hydrophilic and lipophilic hesperetin pro-form. A pharmaceutical composition is provided which is suitable for topical or oral administration in an individual, the composition comprising a hydrophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A pharmaceutical composition is also provided which is suitable for topical or oral administration in an individual, the composition including a lipophilic hesperetin pro-form and a pharmaceutically acceptable carrier. A method is provided for treating a subject having or at risk of having a cell proliferative disorder, including administering to the subject a therapeutically effective amount of a hesperetin pro-form.

    Abstract translation: 提供了hesperitin pro-form。 本发明提供亲水和亲脂性的橙皮素原型。 提供了适合于在个体中局部或口服给药的药物组合物，该组合物包含亲水的橙皮素原型和药学上可接受的载体。 还提供了适合于个体局部或口服给药的药物组合物，该组合物包括亲脂性橙皮素原型和药学上可接受的载体。 提供了一种治疗患有或具有细胞增殖性疾病风险的受试者的方法，包括向受试者施用治疗有效量的橙皮素原型。

    Synthetic methods for polyphenols
    86.
    发明申请
    Synthetic methods for polyphenols 失效
    多酚的合成方法

    公开(公告)号：US20040236123A1

    公开(公告)日：2004-11-25

    申请号：US10858449

    申请日：2004-05-28

    Applicant: M&M/Mars Inc.

    Inventor： Leo J. Romanczyk JR. ,  Alan P. Kozikowski ,  Werner Tueckmantel ,  Marc E. Lippman

    IPC: C07D45/14

    CPC classification number: C07H17/06 ,  A61K31/35 ,  C07D311/32 ,  C07D311/60 ,  C07D311/62

    Abstract: A process is disclosed for the production of polyphenol oligomers having n polyphenol monomeric units, n being an integer from 2-18. The process includes coupling of a protected polyphenol, having protected phenolic hydroxyl groups, with a C-4 functionalized polyphenol monomer. The protected polyphenol may be a protected polyphenol monomer or a protected polyphenol oligomer having 2-17 monomeric units. Advantageously, polyphenol monomeric units forming the polyphenol oligomers may be the same or different flavanoid compounds.

    Abstract translation: 公开了用于生产具有多酚单体单元的多酚低聚物的方法，n为2-18的整数。 该方法包括将被保护的酚羟基的被保护的多酚与C-4官能化的多酚单体的偶联。 受保护的多酚可以是受保护的多酚单体或具有2-17单体单元的被保护的多酚低聚物。 有利地，形成多酚低聚物的多酚单体单元可以是相同或不同的类黄酮化合物。

    Inhibition by 3-deoxyflavonoids of T-lymphocyte activation and therapies related thereto
    87.
    发明申请
    Inhibition by 3-deoxyflavonoids of T-lymphocyte activation and therapies related thereto 审中-公开
    3-脱氧黄酮对T淋巴细胞活化的抑制作用及与之相关的疗法

    公开(公告)号：US20040102386A1

    公开(公告)日：2004-05-27

    申请号：US10652624

    申请日：2003-08-29

    Inventor： Thomas Lahey ,  Vithal J. Rajadhyaksha

    IPC: A61K031/7048 ,  A61K031/4178 ,  A61K031/405 ,  A61K031/353

    CPC classification number: C07D493/04 ,  A61K31/352 ,  A61K31/353 ,  C07D311/30 ,  C07D311/32 ,  C07D311/36 ,  C07D407/04 ,  C07F9/65522

    Abstract: 3-Deoxyflavonoid compounds and methods for inhibiting T-cell activity and treating diseases and disorders (e.g., autoimmune disorders, inflammatory disorders, diabetes, ALS, MS, rheumatoid arthritis, etc.). In some cases the efficacy and/or duration of action of luteolin and/or other 3-deoxyflavonoid compounds may be increased by administering such compounds along with Rutin, a Rutin congener and/or a Rutin derivative. Also, in some cases, first pass metabolism of luteolin or other 3-deoxyflavonoids may be avoided by administering such compounds by parenteral routes (e.g., routes wherein absorption occurs at sites other than the stomach or intestinal mucosa, such as sublingual, buccal, intranasal, injection, etc.).

    Abstract translation: 3-脱氧黄酮化合物和抑制T细胞活性和治疗疾病和病症（例如自身免疫性疾病，炎症性疾病，糖尿病，ALS，MS，类风湿性关节炎等）的方法。 在一些情况下，可以通过将这些化合物与芦丁，芦丁同类物和/或芦丁衍生物一起施用来增加木犀草素和/或其它3-脱氧黄酮类化合物的功效和/或作用持续时间。 此外，在一些情况下，通过肠胃外途径（例如其中吸收发生在除胃或肠粘膜之外的位置，如舌下，口腔，鼻内）的途径可以避免木犀草素或其他3-脱氧黄酮的首次通过代谢 ，注射等）。

    Flavanol and cysteamine conjugates
    88.
    发明申请
    Flavanol and cysteamine conjugates 失效
    黄烷醇和半胱胺共轭物

    公开(公告)号：US20040077711A1

    公开(公告)日：2004-04-22

    申请号：US10451475

    申请日：2003-12-03

    Inventor： Jose Luis Torres Simon

    IPC: A61K031/353 ,  C07D311/74

    CPC classification number: A61K8/46 ,  A61K8/4926 ,  A61K2800/522 ,  A61Q19/08 ,  C07D311/32

    Abstract: The present invention refers to new products generated by the conjugation of flavanols with molecules that contain the thiol group. New molecules are obtained from polyphenolic plant extracts rich in oligomeric and polymeric procyanidines and prodelfinidins. In this way, new products are generated with antioxidant properties for application as protective agents for the organism against disorders such as cancer, cardiovascular diseases and premature aging. The invention also refers to obtaining these new agents from waste material generated by the agroalimentary industry. Since these waste materials are highly complex mixtures a simple and effective method is described to isolate and purify these, based on the physico-chemical characteristics of the new molecules.

    Abstract translation: 本发明涉及通过将黄烷醇与含有硫醇基的分子缀合产生的新产物。 新分子可从富含低聚和聚合原花青素和prodelfinidins的多酚植物提取物中获得。 以这种方式，产生具有抗氧化性质的新产品用作生物体的保护剂，以防止诸如癌症，心血管疾病和过早衰老的疾病。 本发明还涉及由农业工业生产的废料获得这些新药。 由于这些废料是高度复杂的混合物，所以基于新分子的物理化学特性，描述了简单有效的方法来分离和纯化这些。

    Novel flavanoids as chemotherapeutic, chemopreventive, and antiangiogenic agents
    89.
    发明申请
    Novel flavanoids as chemotherapeutic, chemopreventive, and antiangiogenic agents 审中-公开
    新型黄烷类化学治疗，化学预防和抗血管生成剂

    公开(公告)号：US20030229136A1

    公开(公告)日：2003-12-11

    申请号：US10126407

    申请日：2002-04-18

    Inventor： Nurulain Zaveri ,  Wan-Ru Chao

    IPC: A61K031/353 ,  A61K031/47 ,  C07D311/04 ,  C07C049/237 ,  A61K031/12

    CPC classification number: C07C45/30 ,  C07C45/46 ,  C07C45/71 ,  C07C45/74 ,  C07C49/835 ,  C07C49/84 ,  C07D311/32 ,  C07D311/92 ,  C07D311/94 ,  C07D491/04 ,  C07C47/575 ,  C07C49/83

    Abstract: Novel compounds useful as chemotherapeutic, chemopreventive, and antiangiogenic agents are provided. The compounds are flavanoids, including flavanones, flavanols, and chalcones. The compounds have the structure of formula (I) 1 wherein R1 through R3 and R5 through R11 are defined herein, and null, null and null are optional bonds, providing that when null is absent, null is present, and when null is absent, null is present. When null is present, preferred R4 moieties are selected from O, S, NH and CH2, and when null is absent, preferred R4 groups are selected from OH, SH, NH2 and CH3. When null is present, the preferred R5 substituent is O, while when null is absent, the preferred R5 substituent is OH. Pharmaceutical compositions are provided as well, as are methods of synthesis and use.

    Abstract translation: 提供了可用作化学治疗，化学预防和抗血管生成剂的新型化合物。 化合物是类黄酮，包括黄烷酮，黄烷醇和查尔酮。 这些化合物具有式（I）的结构，其中R 1至R 3和R 5至R 11在本文中定义，并且α，β和γ是任选的键，条件是当α不存在时 ，β存在，当β不存在时，存在α。 当存在α时，优选的R 4部分选自O，S，NH和CH 2，当不存在α时，优选的R 4选自OH，SH，NH 2和CH 3。 当存在γ时，优选的R 5取代基是O，而当不存在γ时，优选的R 5取代基是OH。 还提供药物组合物，以及合成和使用的方法。

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