Use of liver X receptor agonists
    1.
    发明授权
    Use of liver X receptor agonists 失效
    使用肝脏X受体激动剂

    公开(公告)号:US08030335B2

    公开(公告)日:2011-10-04

    申请号:US11920141

    申请日:2006-05-10

    IPC分类号: A61K31/44 A61K31/18

    摘要: The present invention generally relates to a novel therapeutical use of liver X receptor (LXR) agonsits. More specifically, the present invention relates to the use of LXR agonist for the preparation of a medicament useful for the treatment and/or the prevention of a disease associated with beta cells degeneration, such as diabetes, and a method for increasing ex vivo viability of pancreatic islet cells, comprising contacting said islet cells with a LXR agonist.

    摘要翻译: 本发明一般涉及肝X受体(LXR)治疗的新型治疗用途。 更具体地说,本发明涉及LXR激动剂在制备可用于治疗和/或预防与β细胞变性相关的疾病(例如糖尿病)的药物中的用途,以及增加体内存活力的方法 胰岛细胞,包括使所述胰岛细胞与LXR激动剂接触。

    Polypeptide derivatives of dog gastric lipase and pharmaceutical
compositions containing same
    4.
    发明授权
    Polypeptide derivatives of dog gastric lipase and pharmaceutical compositions containing same 失效
    狗胃脂肪酶的多肽衍生物和含有其的药物组合物

    公开(公告)号:US05998189A

    公开(公告)日:1999-12-07

    申请号:US73674

    申请日:1998-05-06

    IPC分类号: A61K38/00 C12N9/20 A61K38/46

    CPC分类号: C12N9/20 A61K38/00

    摘要: The present invention relates to polypeptide derivatives of dog gastric lipase as obtained by genetic engineering as well as to the nucleotide sequence encoding this recombinant DGL. It also relates to the use of this recombinant DGL for the production of pharmaceutical compositions intended especially for the treatment of pathologies linked to the insufficiency, or even the absence, of secretion of lipases in the body of an individual.

    摘要翻译: 本发明涉及通过遗传工程获得的狗胃脂肪酶的多肽衍生物以及编码该重组DGL的核苷酸序列。 它还涉及这种重组DGL用于制备药物组合物的用途,该药物组合物特别用于治疗与个体身体中脂肪酶分泌不足或甚至不存在相关的病理学。

    Diazepinoindoles as phosphodiesterase IV inhibitors
    5.
    发明授权
    Diazepinoindoles as phosphodiesterase IV inhibitors 失效
    二氮杂吲哚作为磷酸二酯酶IV抑制剂

    公开(公告)号:US5852190A

    公开(公告)日:1998-12-22

    申请号:US391865

    申请日:1995-02-22

    CPC分类号: C07D487/06 A61K31/5517

    摘要: The invention relates to diazepinoindoles of formula: ##STR1## in which R is hydrogen, lower alkyl or lower alkoxy; A is aryl or nitrogen-containing heteroaryl, each of which is optionally substituted by from one to three groups of halogen, lower alkyl, haloalkyl, lower alkoxy and acetamido, or their racemic forms, isomers or pharmaceutically acceptable salts, wherein for the racemic forms of the (S) configuration, A is not phenyl, haloalkyl, or 2-indolyl when R is hydrogen, and for the racemic forms of the (R) configuration, A is not 2-indolyl when R is hydrogen. Also, the invention relates to a method for inhibiting cyclic nucleotide phosphodiesterase activity by administering these compounds to a subject in an amount which is therapeutically effective to inhibit cyclic nucleotide phosphodiesterase activity.

    摘要翻译: 本发明涉及式为:其中R为氢,低级烷基或低级烷氧基的下式的二氮茚并吲哚; A是芳基或含氮杂芳基,其各自任选被一至三个卤素,低级烷基,卤代烷基,低级烷氧基和乙酰氨基取代,或其外消旋形式,异构体或药学上可接受的盐,其中对于外消旋形式 的(S)构型,当R是氢时,A不是苯基,卤代烷基或2-吲哚基,对于(R)构型的外消旋形式,当R是氢时,A不是2-吲哚基。 此外,本发明涉及通过以对治疗有效抑制环核苷酸磷酸二酯酶活性的量将这些化合物给予受试者来抑制环核苷酸磷酸二酯酶活性的方法。

    Allylaminoesters and their application in therapeutics
    9.
    发明授权
    Allylaminoesters and their application in therapeutics 失效
    烯丙基氨基酯及其在治疗中的应用

    公开(公告)号:US5472970A

    公开(公告)日:1995-12-05

    申请号:US309004

    申请日:1994-09-19

    摘要: Allylaminoesters of the formula (I): ##STR1## in which: R.sub.1 is H or low-molecular-weight alkyl,R.sub.2 is low-molecular-weight alkyl, cycloalkyl, or low-molecular-weight phenylcycloalkyl, pyridyl or phenyl, low-molecular-weight phenylalkyl, low-molecular-weight diphenylalkyl, low-molecular-weight phenylalkenyl, in which the phenyl cycle may be mono-, di- or trisubstituted by chlorine atoms, low-molecular-weight alkyl radicals, low-molecular-weight alkoxy, or trifluoromethyl, acetamide or acetyloxy radicals, their racemic forms, their (S) enantiomers and their addition salts. Also, antiallergic drugs containing the same.

    摘要翻译: 式(I)的烯丙基氨基酯:其中:R 1是H或低分子量烷基,R 2是低分子量烷基,环烷基或低分子量苯基环烷基,吡啶基或苯基 ,低分子量苯基烷基,低分子量二苯基烷基,低分子量苯基烯基,其中苯基周期可以被氯原子单,二或三取代,低分子量烷基,低分子量苯基烷基, 分子量的烷氧基或三氟甲基,乙酰胺或乙酰氧基,它们的外消旋体,它们的(S)对映体及其加成盐。 而且,含有相同的抗过敏药物。