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    BETA-3-ADRENORECEPTOR AGONISTS, AGONIST COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME
    68.
    发明公开
    BETA-3-ADRENORECEPTOR AGONISTS, AGONIST COMPOSITIONS AND METHODS OF MAKING AND USING THE SAME 审中-公开
    BETA-3-ADRENOREZEPTOR-AGONISTEN，AGONISTISCHE ZUSAMMENSETZUNG UND VERFAHREN ZUR HERSTELLUNG UND ANWENDUNG

    公开(公告)号：EP1373212A4

    公开(公告)日：2004-06-23

    申请号：EP01964673

    申请日：2001-03-29

    Applicant: MOLECULAR DESIGN INT

    Inventor： FELLER DENNIS R ,  MILLER DUANE D

    IPC: C07D217/18 ,  C07D217/20 ,  C07D217/02 ,  A61K31/47

    CPC classification number: C07D217/18 ,  C07D217/20

    Abstract: Compounds which are highly potent and highly specific β3-Adrenoreceptor agonists are provided. The compounds are formulated into pharmaceutical preparations and administered for stimulating, regulating and modulating metabolism of fats in adipose tissues in animals, particularly humans and other mammals. The compounds of the invention have the structure (A). R1 and R2 are each independently members selected from the group consisting of H, OH, C1, NO2, CH3SO2NH, NH2, CH3O and weak acids of the structure R7-NH, where R7 is an acyl group, wherein at least one of R1 and R2 is OH. It is generally preferred that R2 be OH; R3, R4 and R5 are variously and independently members selected from I, Br, C1, F, OCH3, CH3, alkyl, alkylaryl, aminoalkyl, thioalkyl, and O-alkyl. Preferably, R4 and R5 are each a halogen, the same or different; R6 is an acid moiety which forms an acid salt with the NH group. R6 is desirably HC1 or (COOH)2. While the racemic mixtures are active, selective, and bioavailable, we have found that the isolated isomers are ordinarily of more particular interest. The S(-) isomers are preferred, as they will be found to have the highest selectivity and the highest bioavailability. The R(+) isomers are also of interest, as the R-isomers are in some cases easier to isolate. The compounds are formulated into pharmaceutical carriers to serve as highly selective, effective and safe β3-Adrenoreceptor agonists to provide long term weight control. In humans, the compositions are administered to control body fat levels, and to maintain acceptable body fat levels over time. In domesticated animals, the compositions are administered to attain desirably low fat content in carcass meats intended for human consumption.

    Abstract translation: 提供了高度有效和高度特异性β3-肾上腺素受体激动剂的化合物。 将这些化合物配制成药物制剂并施用用于刺激，调节和调节动物特别是人和其他哺乳动物脂肪组织中脂肪的代谢。 本发明的化合物具有结构（A）。 R 1和R 2各自独立地选自H，OH，Cl，NO 2，CH 3 SO 2 NH，NH 2，CH 3 O和结构R 7 -NH的弱酸，其中R 7为酰基，其中R 1和R 2中的至少一个 R2是OH。 一般优选R2为OH; R 3，R 4和R 5各自独立地选自I，Br，C 1，F，OCH 3，CH 3，烷基，烷基芳基，氨基烷基，硫代烷基和O-烷基。 优选地，R4和R5各自是相同或不同的卤素; R6是与NH基团形成酸式盐的酸性部分。 R6优选为HCl或（COOH）2。 尽管外消旋混合物具有活性，选择性和生物可利用性，但我们发现分离的异构体通常更具特殊意义。 S（ - ）异构体是优选的，因为它们将被发现具有最高的选择性和最高的生物利用度。 R（+）异构体也是有意义的，因为R-异构体在某些情况下更容易分离。 将这些化合物配制成药物载体，作为高度选择性，有效和安全的β3-肾上腺素受体激动剂，以提供长期的体重控制。 在人体中，施用组合物以控制体内脂肪水平，并随时间维持可接受的体脂肪水平。 在家养动物中，施用组合物以达到预期供人食用的屠体肉中理想的低脂肪含量。

    Isoquinolines and preparation thereof
    69.
    发明公开
    Isoquinolines and preparation thereof 失效
    Isochinoline und deren Herstellung

    公开(公告)号：EP1380573A2

    公开(公告)日：2004-01-14

    申请号：EP03020565.2

    申请日：1998-03-23

    Applicant: Avera Pharmaceuticals, Inc. ,  CORNELL RESEARCH FOUNDATION, INC.

    Inventor： The designation of the inventor has not yet been filed

    IPC: C07D217/20

    CPC classification number: C07D217/16 ,  C07D217/20

    Abstract: A compound of Formula (III):
    wherein Y is selected from the group consisting of hydrogen or methoxy, W comprises a chiral center selected from the group consisting of a carbon atom having an R configuration and a carbon atom having an S configuration, n comprises 0 or 1, and A - comprises a pharmaceutically acceptable anion and process of preparation.

    Abstract translation: 式（III）化合物：其中Y选自氢或甲氧基，W包含选自具有R构型的碳原子和具有S构型的碳原子的手性中心 ，n包括0或1，并且A 1包含药学上可接受的阴离子和制备方法。

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