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    POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ASPIRIN
    4.
    发明申请
    POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF ASPIRIN 审中-公开
    积极收费的ASPIRIN水溶性产品

    公开(公告)号：WO2008007171A1

    公开(公告)日：2008-01-17

    申请号：PCT/IB2006/052318

    申请日：2006-07-09

    申请人： TECHFIELDS BIOCHEM CO. LTD ,  YU, Chongxi ,  XU, Lina

    发明人： YU, Chongxi ,  XU, Lina

    IPC分类号： C07C235/42 ,  C07C235/16 ,  C07C211/64

    CPC分类号： C07C219/14 ,  C07C235/60 ,  C07C327/30

    摘要： The novel positively charged prodrugs of acetylsalicylic acid and its analogues in the general formula(1) "Structure 1" were designed and synthesized. The compounds of the general formula(1) "Structure 1" indicated above can be prepared from functional derivatives of ASA or its analogues,(for example acid halides or mixed anhydrides), by reaction with suitable alcohols, thiols, or amines. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs, but also bonds to the negative charge on the phosphate head group of membranes and push the pro-drug into the cytosol. The experiment results suggest that the pro-drug, diethylaminoethyl acetylsalicylate.AcOH, diffuses through human skin ~400 times faster than acetylsalicylic acid itself and ~100 times faster than ethyl acetylsalicylate. In plasma, 80% of these pro-drugs can change back to the drug in a few minutes. The pro-drugs can be used medicinally in treating any aspirin-treatable conditions in humans or animals and be administered not only orally, but also transdermally for any kind of medical treatments and avoid most of the side effects of aspirin, most notably GI disturbances such as dyspepsia, gastroduodenal bleeding, gastric ulcerations, and gastritis. Controlled transdermal administration systems of the prodrug enables the aspirin to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of aspirin.

    摘要翻译： 设计并合成了通式（1）“结构1”中乙酰水杨酸及其类似物的新型带正电荷前体药物。 上述通式（1）“结构1”的化合物可以由ASA或其类似物的官能衍生物（例如酰卤或混合酸酐）通过与合适的醇，硫醇或胺的反应制备。 这些前药的带正电荷的氨基不仅大大增加药物的溶解度，而且还与磷酸盐头基上的负电荷键合，并将前药推入细胞溶质中。 实验结果表明，前药二乙氨基乙酰水杨酸AcAc通过人皮肤扩散至乙酰水杨酸本身的400倍，乙酰水杨酸乙酯比乙酰水杨酸乙酯快100倍。 在等离子体中，这些前药中有80％可以在几分钟内恢复药物。 前药可以在医学上用于治疗人或动物中的任何阿斯匹林可治疗的病症，并且不仅口服给药，而且经皮用于任何种类的治疗，并且避免阿司匹林的大部分副作用，特别是GI紊乱 如消化不良，胃十二指肠出血，胃溃疡和胃炎。 前药的控制透皮给药系统使得阿司匹林能够达到不断优化的治疗血液水平以增加有效性并降低阿司匹林的副作用。

    FLAVOUR MODULATING SUBSTANCES
    5.
    发明申请
    FLAVOUR MODULATING SUBSTANCES 审中-公开
    挥发性调节物质

    公开(公告)号：WO2006046853A1

    公开(公告)日：2006-05-04

    申请号：PCT/NL2005/000719

    申请日：2005-10-06

    申请人： QUEST INTERNATIONAL SERVICES B.V. ,  QUEST INTERNATIONAL B.V. ,  WINKEL, Chris ,  RENES, Harry

    发明人： WINKEL, Chris ,  RENES, Harry

    IPC分类号： A23L1/226 ,  C07C235/08 ,  C07C235/16

    CPC分类号： A23L17/10 ,  A23L27/204

    摘要： The present invention in a first aspect relates to novel flavour modulating subtances according to formula (I) and/or edible salts thereof: R 1 -CR 2 (OR 3 )-CO-NR 4 -Y-X (I). It was found that substances represented by formula (I) can advantageously be used to impart desirable flavour, especially taste attributes to foodstuffs, beverages, and pharmaceutics they are incorporated in. In addition said substances are capable of modulating and complementing the sensory impact of other, flavour imparting, substances. Thus, the present flavour modulating substances are advantageously applied in flavour compositions, foodstuffs, beverages and pharmaceutics. Typical examples of flavour modulating substances according to the present invention include N-lactoyl tyramine, N-gluconyl tyramine, N-lactoyl 4-hydroxybenzylamine, N-lactoyl vanillylamine and N-lactoyl-dopamine.

    摘要翻译： 本发明的第一方面涉及根据式（I）和/或其食用盐的新颖风味调节剂，其中R 1，R 2， 3-CO-NR 4 -YX（I）。 发现由式（I）表示的物质可以有利地用于赋予其所掺入的食品，饮料和药物所需的风味，特别是味道特性。此外，所述物质能够调节和补充其他物质的感官影响 ，赋香，物质。 因此，本发明的风味调节物质有利地用于风味组合物，食品，饮料和药物中。 根据本发明的风味调节物质的典型实例包括N-乳酰酪胺，N-葡萄糖酸酪胺，N-乳酰基-4-羟基苄胺，N-乳酰基香草胺和N-乳酰基多巴胺。

    HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF
    6.
    发明申请
    HALOGENATED SELECTIVE ANDROGEN RECEPTOR MODULATORS AND METHODS OF USE THEREOF 审中-公开
    选择性受体选择性受体调节剂及其使用方法

    公开(公告)号：WO2004035736A3

    公开(公告)日：2004-07-15

    申请号：PCT/US0332507

    申请日：2003-10-14

    申请人： UNIV TENNESSEE RES FOUNDATION ,  DALTON JAMES T ,  MILLER DUANE D ,  YIN DONGHUA ,  HE YALI ,  STEINER MITCHELL S ,  VEVERKA KAREN A

    发明人： DALTON JAMES T ,  MILLER DUANE D ,  YIN DONGHUA ,  HE YALI ,  STEINER MITCHELL S ,  VEVERKA KAREN A

    IPC分类号： A61K31/165 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/16 ,  C07C235/24 ,  C07C255/60 ,  C07C335/18 ,  C07D209/08 ,  C07D215/22 ,  C07D215/227 ,  C07D271/12 ,  C07C233/05 ,  A61K31/275 ,  C07C255/50

    CPC分类号： C07D215/227 ,  A61K31/165 ,  A61K31/404 ,  A61K31/4706 ,  A61K31/661 ,  C07C235/16 ,  C07C235/24 ,  C07C255/60 ,  C07C335/18 ,  C07D209/08 ,  C07D271/12

    摘要： This invention provides a class of androgen receptor targeting agents (ARTA). The agents define a new subclass of compounds, which are selective androgen receptor modulators (SARM). Several of the SARM compounds have been found to have an unexpected androgenic and anabolic activity of a nonsteroidal ligand for the androgen receptor. Other SARM compounds have been found to have an unexpected antiandrogenic activity of a nonsteroidal ligand for the androgen receptor. The SARM compounds, either alone or as a composition, are useful for a) male contraception; b) treatment of a variety of hormone-related conditions, for example conditions associated with Androgen Decline in Aging Male (ADAM), such as fatigue, depression, decreased libido, sexual dysfunction, erectile dysfunction, hypogonadism, osteoporosis, hair loss, anemia, obesity, sarcopenia, osteopenia, osteoporosis, benign prostate hyperplasia, alterations in mood and cognition and prostate cancer; c) treatment of conditions associated with Androgen Decline in Female (ADIF), such as sexual dysfunction, decreased sexual libido, hypogonadism, sarcopenia, osteopenia, osteoporosis, alterations in cognition and mood, depression, anemia, hair loss, obesity, endometriosis, breast cancer, uterine cancer and ovarian cancer; d) treatment and/or prevention of acute and/or chronic muscular wasting conditions; e) preventing and/or treating dry eye conditions; f) oral androgen replacement therapy; g) decreasing the incidence of, halting or causing a regression of prostate cancer; and/or h) inducing apoptosis in a cancer cell.

    摘要翻译： 本发明提供一类雄激素受体靶向剂（ARTA）。 这些药剂定义了一种新的化合物亚类，它们是选择性雄激素受体调节剂（SARM）。 已经发现几种SARM化合物对于雄激素受体具有非甾类化合物的意想不到的雄激素和合成代谢活性。 已经发现其他SARM化合物对于雄激素受体具有非甾类配体的意想不到的抗雄激素活性。 SARM化合物，单独或作为组合物，可用于a）男性避孕; b）治疗多种激素相关病症，例如与老年雄性雄激素降低有关的病症（ADAM），如疲劳，抑郁，性欲降低，性功能障碍，勃起功能障碍，性腺机能减退，骨质疏松症，脱发，贫血， 肥胖，肌营养不良，骨质减少，骨质疏松症，良性前列腺增生，情绪和认知和前列腺癌的改变; c）治疗与男性雄激素降低有关的疾病（ADIF），如性功能障碍，性欲降低，性腺机能减退，肌营养不良，骨质减少，骨质疏松症，认知和情绪改变，抑郁症，贫血，脱发，肥胖，子宫内膜异位症，乳腺癌 癌症，子宫癌和卵巢癌; d）治疗和/或预防急性和/或慢性肌肉消瘦病症; e）预防和/或治疗干眼症状; f）口服雄激素替代疗法; g）降低前列腺癌的发生率，停止或导致消退; 和/或h）诱导癌细胞凋亡。

    PROCESS FOR PREPARING SUBSTITUTED AROMATIC COMPOUNDS AND INTERMEDIATES THEREFOR
    7.
    发明申请
    PROCESS FOR PREPARING SUBSTITUTED AROMATIC COMPOUNDS AND INTERMEDIATES THEREFOR 审中-公开
    制备取代的芳族化合物及其中间体的方法

    公开(公告)号：WO02034712A1

    公开(公告)日：2002-05-02

    申请号：PCT/JP2001/009422

    申请日：2001-10-26

    IPC分类号： C07C209/58 ,  C07C221/00 ,  C07C231/08 ,  C07C231/12 ,  C07D215/20 ,  C07D215/60 ,  C07C211/52 ,  C07C215/38 ,  C07C215/60 ,  C07C225/20 ,  C07C225/22 ,  C07C235/16 ,  C07C235/20

    CPC分类号： C07D215/20 ,  C07C209/58 ,  C07C221/00 ,  C07C231/08 ,  C07C231/12 ,  C07D215/60

    摘要： A process for preparing substituted aromatic compounds of the general formula (¦¦) or salts thereof: (¦¦) [wherein A is an optionally substituted aromatic homo- or hetero-cycle; X is O- or the like; Y is NR - or the like; and B is an optionally substituted aromatic homo- or hetero-cycle, or optionally substituted ethylene] by subjecting compounds of the general formula (¦) or salts thereof: (¦) [wherein each symbol is as defined above] to Smiles rearrangement, characterized in that the Smiles rearrangement is conducted in the presence of a basic hydroxide in an amide solvent. According to this process, the problems of Smiles rearrangement can be solved and various aromatic compounds useful as drugs, agricultural chemicals, or intermediates for the production of various general-purpose chemicals can be efficiently prepared by Smiles rearrangement.

    摘要翻译： （||）的取代芳族化合物或其盐的制备方法：（||）[其中A是任选取代的芳族同 - 或异 - 循环; X是O-等; Y是NR 1 - 等; （|）的化合物或其盐：（|）[其中每个符号如上所定义]至Smiles重排，其特征在于，其中B是任​​选取代的芳族均聚或异环或任选取代的亚乙基 因为Smiles重排在碱性氢氧化物存在下在酰胺溶剂中进行。 根据该过程，可以解决微笑重排的问题，可以通过微笑重排有效地制备用作各种通用化学品生产的药物，农药或中间体的各种芳族化合物。

    NOVEL AMINOPHENOL DERIVATIVES
    8.
    发明申请
    NOVEL AMINOPHENOL DERIVATIVES 审中-公开
    新型氨基酚衍生物

    公开(公告)号：WO01072693A1

    公开(公告)日：2001-10-04

    申请号：PCT/JP2001/002408

    申请日：2001-03-26

    IPC分类号： C07C235/16 ,  C07C309/66 ,  C07C309/73

    CPC分类号： C07C235/16

    摘要： Aminophenol derivatives of the general formula (1) useful as intermediates in the production of drugs, agricultural chemicals and so on can be prepared at a low cost by condensing an amine of the general formula (2) with an ester of the general formula (3) without using a condensing agent.

    摘要翻译： 可以通过将通式（2）的胺与通式（3）的酯缩合而以低成本制备用作药物，农药等的中间体的通式（1）的氨基苯酚衍生物 ），而不使用冷凝剂。

    WATER-SOLUBLE CONTRAST MEDIA FOR X-RAY IMAGING
    9.
    发明申请
    WATER-SOLUBLE CONTRAST MEDIA FOR X-RAY IMAGING 审中-公开
    用于X射线成像的水溶性对比介质

    公开(公告)号：WO00037115A1

    公开(公告)日：2000-06-29

    申请号：PCT/GB1999/001699

    申请日：1999-05-28

    IPC分类号： A61K49/04 ,  C07C33/46 ,  C07C33/48 ,  C07C235/16 ,  C07C237/46

    CPC分类号： C07C33/46 ,  A61K49/0433 ,  A61K49/0452 ,  C07C33/483 ,  C07C235/16 ,  C07C237/46

    摘要： The invention provides low viscosity iodinated aryl compounds, useful as X-ray contrast agents, of formula (I) wherein n is 0 or 1; X is an amide group linked to the phenyl ring either by the nitrogen atom or by the carbon of the carbonyl group; R is H or a C1-4 alkyl group substituted by two or more -OH groups; R' is a C1-4 alkyl group optionally substituted by one or more -OH groups; R'' is a C2-4 alkyl group which may be straight chained or branched and is substituted by two or more -OH groups and isomers thereof.

    摘要翻译： 本发明提供低粘度碘化芳基化合物，其可用作式（I）的X射线造影剂，其中n为0或1; X是通过氮原子或羰基的碳与苯环连接的酰胺基; R是H或被两个或更多个-OH基取代的C 1-4烷基; R'是任选被一个或多个-OH基团取代的C 1-4烷基; R“是可以是直链或支链并被两个或更多个-OH基团及其异构体取代的C2-4烷基。