Polyhydroxy phenols and their use in binding p-selectin
    2.
    发明申请
    Polyhydroxy phenols and their use in binding p-selectin 失效
    多羟基酚及其在结合p-选择素中的应用

    公开(公告)号:US20060276545A1

    公开(公告)日:2006-12-07

    申请号:US10558495

    申请日:2004-05-07

    IPC分类号: A61K31/198 C07C237/02

    摘要: Polyhydroxy phenols, which are non-peptidic mimetics of galloyl peptides, and a process for the preparation of gallic acid derivatives using a gallic-acid providing moiety are provided as well as polyhydroxy phenol-containing pharmaceutical and nutraceutical compositions. The use of polyhydroxy phenols as a medicament and especially for the manufacture of a medicament for the prevention, treatment or diagnosis of a disease or a condition, wherein P-selectin is involved, is provided. The same compounds can also be used as targeting tools to P-selectin expressing cells or tissues in a composition, further comprising an active compound in a vehicle.

    摘要翻译: 提供作为酰基肽的非肽模拟物的多羟基酚,以及使用没食子酸提供部分制备没食子酸衍生物的方法以及含有多羟基苯酚的药物和营养组合物。 提供了使用多羟基酚作为药物,特别是制备用于预防,治疗或诊断其中涉及P-选择素的疾病或病症的药物。 相同的化合物也可以用作组合物中表达P-选择蛋白的细胞或组织的靶向工具,还包含载体中的活性化合物。

    Method of screening remedy for renal failure
    3.
    发明申请
    Method of screening remedy for renal failure 审中-公开
    筛查肾功能衰竭的方法

    公开(公告)号:US20050233304A1

    公开(公告)日:2005-10-20

    申请号:US10516517

    申请日:2003-10-09

    摘要: A screening tool and a convenient screening method for obtaining a renal failure treating agent, and a pharmaceutical composition for treating renal failure and a production method thereof are disclosed. The aforementioned screening tool is a G protein coupling type receptor FGK which is a polypeptide capable of activating CTGF promoter, a functionally equivalent modified substance thereof or a homologous polypeptide, or a cell expressing the aforementioned polypeptide. The screening method is a method which employs inhibition of the aforementioned polypeptide as the index.

    摘要翻译: 公开了筛选工具和用于获得肾衰竭治疗剂的方便的筛选方法,以及用于治疗肾衰竭的药物组合物及其制备方法。 上述筛选工具是G蛋白偶联型受体FGK,其是能够激活CTGF启动子,其功能等同的修饰物质或同源多肽或表达上述多肽的细胞的多肽。 筛选方法是采用上述多肽的抑制作为指标的方法。

    Tetrahydro-2H-thiopyran-4-carboxamide derivative
    4.
    发明授权
    Tetrahydro-2H-thiopyran-4-carboxamide derivative 有权
    四氢-2H-噻喃-4-甲酰胺衍生物

    公开(公告)号:US06903125B2

    公开(公告)日:2005-06-07

    申请号:US10912232

    申请日:2004-08-06

    CPC分类号: C07D335/02 C07D413/12

    摘要: A pharmaceutical drug, particularly a novel compound useful for the prophylaxis or therapeutic treatment of various diseases involving infections with viruses of the Herpesviridae family, specifically various herpesvirus infections such as varicella (chicken pox) via varicella zoster virus, varicella zoster via recurrent infection with latent varicella zoster virus, herpes labialis and herpes encephalitis via HSV-1 and genital herpes via HSV-2 infection. N-{2-[(4-Substituted phenyl)amino]-2-oxoethyl}tetrahydro-2H-thiopyran-4-carboxamide derivative where the phenyl group is substituted at position 4 with a specific five-membered or 6-membered heteroaryl group, has such great anti-virus activity that the oral dosing thereof at a low dose enabled the therapeutic treatment of the diseases.

    摘要翻译: 一种药物,特别是可用于预防或治疗涉及疱疹病毒科家族病毒感染的各种疾病的新型化合物,特别是各种疱疹病毒感染如通过水痘带状疱疹病毒的水痘(水痘),水痘带状疱疹通过潜在的复发性感染 水痘带状疱疹病毒,通过HSV-1和生殖器疱疹通过HSV-2感染的唇疱疹和疱疹脑炎。 N- {2 - [(4-取代的苯基)氨基] -2-氧代乙基}四氢-2H-噻喃-4-甲酰胺衍生物,其中苯基在4位被特定的5元或6元杂芳基取代 具有如此巨大的抗病毒活性,以低剂量的口服给药能够治疗疾病。

    Method for improving adsorption of a drug from ethylene oxide derivative
    5.
    发明申请
    Method for improving adsorption of a drug from ethylene oxide derivative 失效
    改善环氧乙烷衍生物吸收药物的方法

    公开(公告)号:US20050100607A1

    公开(公告)日:2005-05-12

    申请号:US10672398

    申请日:2003-09-26

    CPC分类号: A61K47/10 A61K9/0065

    摘要: The present invention relates to a method for improving adsorption on the gastrointestinal mucous layers of one or more selected from polyethylene glycol, polyethylene oxide, and polyoxyethylene polypropylene copolymer wherein the average number of repeating oxyethylene units of one ethylene oxide chain length is 17 or greater. It is possible to enhance pharmacological effects by using the present invention with drugs that have anti-H. pylori activity.

    摘要翻译: 本发明涉及一种改善一个或多个选自聚乙二醇,聚环氧乙烷和聚氧乙烯聚丙烯共聚物中的一种或多种吸附的方法,其中一个环氧乙烷链长度的重复氧化乙烯单元的平均数为17或更大。 本发明可以通过具有抗-H的药物来提高药理作用。 幽门螺杆菌活动。

    Quick disintegrating tablet in buccal cavity and production process thereof
    6.
    发明申请
    Quick disintegrating tablet in buccal cavity and production process thereof 审中-公开
    颊腔快速崩解片及其制作方法

    公开(公告)号:US20050100598A1

    公开(公告)日:2005-05-12

    申请号:US10961875

    申请日:2004-10-07

    摘要: The present invention relates to a quick disintegrating tablet in buccal cavity, comprising: a mixture, comprising a drug, a sugar (A), and an amorphous sugar (B), and after it is forming a tablet, it is humidified and dried. In particularly, the present invention relates to a quick disintegrating tablet in buccal cavity comprising: a mixture; comprising a drug, a sugar (A), and an amorphous sugar (B) which an amorphous-forming sugar in crystalline state is dissolved in a medicinally permitted solvent, the amorphous sugar is obtained from this solution by removing the solvent, and after it is forming a tablet, and it is humidified and dried. The tablet in the present invention is to provide stability against moisture at preserved, because the amorphous sugar changed to the crystalline state in a nonreversible reaction after it is humidified and dried in a manufacturing process. The tablet in the present invention is to further provide a design for the pharmaceutical preparation with respect to the stability of a drug, because the tablet is manufactured by one kind of a sugar and an amorphous sugar. Furthermore, the tablet in the present invention is to provide a production process by utilizing a common granulating machine and by utilizing a common tablet machine.

    摘要翻译: 本发明涉及颊腔中的快速崩解片,其包含:包含药物,糖(A)和无定形糖(B)的混合物,在形成片剂之后,将其加湿干燥。 特别地,本发明涉及颊腔中的快速崩解片剂,其包含:混合物; 包含药物,糖(A)和无定形糖(B),其中结晶状态的无定形形成糖溶解在药物允许溶剂中,通过除去溶剂从该溶液获得无定形糖,之后 正在形成片剂,并且被加湿和干燥。 本发明中的片剂是为了提供在保存的水分中的稳定性,因为无定形糖在制造​​过程中被加湿干燥后,在不可逆反应中变为结晶状态。 本发明的片剂是为了进一步提供关于药物的稳定性的药物制剂的设计,因为片剂由一种糖和无定形糖制造。 此外,本发明中的片剂是通过利用普通的造粒机和利用普通的压片机来提供制造方法。

    Enteric sustained-release fine particles of tamsulosin and its salt and manufacturing method thereof
    9.
    发明申请
    Enteric sustained-release fine particles of tamsulosin and its salt and manufacturing method thereof 审中-公开
    肠溶缓慢释放的坦索罗辛缓释微粒及其盐及其制备方法

    公开(公告)号:US20040253309A1

    公开(公告)日:2004-12-16

    申请号:US10766201

    申请日:2004-01-27

    IPC分类号: A61K009/26

    摘要: The present invention relates to enteric sustained-release fine particles of tamsulosin or its salt that can be contained in tablets that disintegrate in the buccal cavity and a manufacturing method thereof. In further detail, the present invention relates to enteric sustained-release fine particles for tablets that disintegrate in the buccal cavity, which comprise (1) tamsulosin or its salt and at least (2) an enterosoluble substance, and when necessary contain (3) a water-insoluble substance, and which have the following characteristics: 1) a particle diameter of approximately 5 to 250 nullm 2) when dissolution tests are performed on tablets that disintegrate in the buccal cavity containing these particles by dissolution testing methods cited in the Japanese Pharmacopoeia, a) the dissolution rate of tamsulosin or its salt at a pH of 1.2 two hours after starting tests is 25% or less b) the time when 50% of the tamsulosin or its salt has dissolved at a pH of 6.8 is 0.5 to 5 hours, and a manufacturing method thereof.

    摘要翻译: 本发明涉及可以包含在颊腔中分解的片剂中的坦索罗辛或其盐的肠溶缓释微粒及其制造方法。 更详细地说,本发明涉及在颊腔中崩解的片剂的肠溶缓释微粒,其包含(1)坦洛新或其盐和至少(2)肠溶性物质,并且在必要时包含(3) 一种水不溶性物质,具有以下特征:1)粒径约5〜250μm2)当对含有这些颗粒的颊腔分解的片剂进行溶解试验时,通过日本的溶出试验方法 药典,a)在开始试验后两小时pH2.2时,坦索罗辛或其盐的溶解速率为25%以下b)当pH值为6.8时,坦索罗辛或其盐50%溶解的时间为0.5〜 5小时及其制造方法。