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    Process of Preparing Esters and Ethers of Probucol and Derivatives Thereof
    1.
    发明申请
    Process of Preparing Esters and Ethers of Probucol and Derivatives Thereof 失效
    Probucol及其衍生物的酯和醚的制备方法

    公开(公告)号：US20080009642A1

    公开(公告)日：2008-01-10

    申请号：US11854939

    申请日：2007-09-13

    申请人： James Sikorski ,  M. Weingarten

    发明人： James Sikorski ,  M. Weingarten

    IPC分类号： C07D301/02 ,  C07C323/31 ,  C07C409/42

    CPC分类号： C07C319/20 ,  C07C323/20

    摘要： A probucol or a probucol derivative can be efficiently converted to a monoester or monoether of probucol by reacting the free hydroxyl-containing probucol or a derivative thereof (by which is meant a probucol compound with at least one substituent that is different from that on the parent probucol molecule but which maintains the two free hydroxyl groups) with a Grignard reagent or a lithium reagent that produces a magnesium bromide or lithium salt of probucol or the probucol derivative. The probucol compound anion anion is then reacted with an ester or ether forming compound.

    摘要翻译： 普罗布考或普罗布考衍生物可以通过游离含羟基的普罗布考或其衍生物的反应而有效地转化成普罗布考的单酯或单醚（通过这种方法将普罗布考化合物与至少一个不同于母体的取代基的化合物反应 普罗布考分子，但其保持两个游离羟基）与格氏试剂或锂试剂反应产生溴丙醇或普罗布考的锂盐或丙磺舒酚衍生物。 然后将普罗布考复合阴离子阴离子与酯或醚形成化合物反应。

    1,3-Bis-(substituted-phenyl)-2-propen-1-ones and their use to treat VCAM-1 mediated disorders
    7.
    发明申请
    1,3-Bis-(substituted-phenyl)-2-propen-1-ones and their use to treat VCAM-1 mediated disorders 审中-公开
    1,3-二（取代苯基）-2-丙烯-1-酮及其用于治疗VCAM-1介导的病症的用途

    公开(公告)号：US20060258735A1

    公开(公告)日：2006-11-16

    申请号：US11485940

    申请日：2006-07-13

    申请人： Charles Meng ,  Liming Ni ,  James Sikorski ,  Lee Hoong

    发明人： Charles Meng ,  Liming Ni ,  James Sikorski ,  Lee Hoong

    IPC分类号： A61K31/381

    CPC分类号： C07D409/10 ,  A61K9/0031 ,  A61K9/0034 ,  A61K31/381 ,  A61K31/44 ,  A61K31/505 ,  A61K31/513 ,  A61K45/06 ,  C07C49/796 ,  C07C49/813 ,  C07C49/835 ,  C07C49/84 ,  C07C49/86 ,  C07C205/45 ,  C07D309/06 ,  C07D317/44 ,  C07D333/16 ,  C07D333/56 ,  C07D413/10 ,  C07D417/10 ,  C07D493/04 ,  A61K2300/00

    摘要： It has been discovered certain 1,3-bis-(substituted-phenyl)-2-propen-1-ones, including compounds of formula (I) inhibit the expression of VCAM-1, and thus can be used to treat a patient with a disorder mediated by VCAM-1. Examples of inflammatory disorders that are mediated by VCAM-1 include, but are not limited to arthritis, asthma, dermatitis, cystic fibrosis, post transplantation late and chronic solid organ rejection, multiple sclerosis, systemic lupus erythematosis, inflammatory bowel diseases, autoimmune diabetes, diabetic retinopathy, rhinitis, ischemia-reperfusion injury, post-angioplasty restenosis, chronic obstructive pulmonary disease (COPD), glomerulonephritis, Graves disease, gastrointestinal allergies, conjunctivitis, atherosclerosis, coronary artery disease, angina and small artery disease.

    摘要翻译： 已经发现某些1,3-双（取代苯基）-2-丙烯-1-酮，包括式（I）化合物抑制VCAM-1的表达，因此可用于治疗患有 由VCAM-1介导的病症。 由VCAM-1介导的炎性病症的实例包括但不限于关节炎，哮喘，皮炎，囊性纤维化，移植后晚期和慢性固体器官排斥，多发性硬化，系统性红斑狼疮，炎性肠病，自身免疫性糖尿病， 糖尿病性视网膜病变，鼻炎，缺血再灌注损伤，血管成形术后再狭窄，慢性阻塞性肺疾病（COPD），肾小球性肾炎，格雷夫斯病，胃肠道过敏，结膜炎，动脉粥样硬化，冠状动脉疾病，心绞痛和小动脉疾病。