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100 条记录 (耗时 0.045 秒)

    Protease Stabilized, Pegylated Insulin Analogues
    71.
    发明申请
    Protease Stabilized, Pegylated Insulin Analogues 审中-公开
    蛋白酶稳定化，聚乙二醇化胰岛素类似物

    公开(公告)号：US20100216691A1

    公开(公告)日：2010-08-26

    申请号：US12669189

    申请日：2008-07-09

    申请人： Peter Madsen

    发明人： Peter Madsen

    IPC分类号： A61K38/28 ,  C07K14/62 ,  A61P3/10 ,  A61P3/04

    CPC分类号： A61K38/28 ,  A61K47/60 ,  C07K14/62

    摘要： Novel PEGylated insulin analogues exhibiting resistance towards proteases can, effectively, be administered pulmonary or orally. The insulin analogues contain B25H and A14E or A14H. The PEGylation is at B29K.

    摘要翻译： 对蛋白酶具有抗性的新型聚乙二醇化胰岛素类似物可以有效地被肺或口服给药。 胰岛素类似物含有B25H和A14E或A14H。 PEG化处于B29K。

    4,5,6,7-tetrahydro-thieno(2,3-C)pyridine derivatives
    76.
    发明授权
    4,5,6,7-tetrahydro-thieno(2,3-C)pyridine derivatives 失效
    4,5,6,7-四氢 - 噻吩并（2,3-C）吡啶衍生物

    公开(公告)号：US6090797A

    公开(公告)日：2000-07-18

    申请号：US387290

    申请日：1999-08-31

    申请人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergaard ,  Palle Jakobsen

    发明人： Peter Madsen ,  Jane Marie Lundbeck ,  Niels Westergaard ,  Palle Jakobsen

    IPC分类号： C07D495/04 ,  A61K31/435 ,  C07D471/04

    CPC分类号： C07D495/04

    摘要： Disclosed are compounds of formula (I) ##STR1## wherein R1 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, Q or aryl;R2 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, aralkyl or COR3;R3 is C.sub.1-8 -alkyl, C.sub.2-8 -alkenyl, C.sub.3-8 -cycloalkyl, C.sub.5-8 -cycloalkenyl, w or aryl;R5, R6 and R7 are independently selected from amino-C.sub.1-6 -alkyl, hydroxy-C.sub.1-6 -alkyl, hydrogen, C.sub.1-6 -alkyl, aryl, aralkyl, aryloxy, aryloxy-C.sub.1-6 -alkyl, benzyl, halogen, hydroxy, mercapto, cyano, nitro, carboxy, carbamoyl, CONHC.sub.1-4 -alkyl, CON(C.sub.1-4 alkyl).sub.2, C.sub.1-4 -acyl, C.sub.1-4 -alkoxy, C.sub.1-4 -alkylthio, --SOC.sub.1-6 -alkyl, --SO.sub.2 C.sub.1-6 -alkyl, C.sub.1-4 -alkoxycarbonyl, C.sub.1-4 -alkanoyloxy, amino, optionally substituted mono- or di-C.sub.1-6 -alkylamino, acylamino, --NC.sub.1-4 -alkylCOC.sub.1-4 -alkyl, --SO3H, --SO2NH--C.sub.1-6 -alkyl, tetrazolyl, perhalomethyl, perhalomethoxy;wherein R1, R2 and R3 are all optionally substituted with one or more substituents;or salt thereof with a pharmaceutically acceptable acid or base, or any optical isomer; a pharmaceutical composition containing them, and the use of these compounds for preparing medicaments for the treatment of diseases of the endocrinologic system, preferably hyperglycemia or diabetes.

    摘要翻译： 公开了式（I）的化合物，其中R 1是C 1-8烷基，C 2-8 - 烯基，C 3-8 - 环烷基，C 5-8 - 环烯基，Q或芳基; R 2是C 1-8 - 烷基，C 2-8 - 烯基，C 3-8 - 环烷基，C 5-8 - 环烯基，芳烷基或COR 3; R 3是C 1-8烷基，C 2-8 - 烯基，C 3-8 - 环烷基，C 5-8 - 环烯基，w或芳基; R 5，R 6和R 7独立地选自氨基-C 1-6 - 烷基，羟基-C 1-6 - 烷基，氢，C 1-6 - 烷基，芳基，芳烷基，芳氧基，芳氧基-C 1-6 - 烷基，苄基，卤素 ，羟基，巯基，氰基，硝基，羧基，氨基甲酰基，CONHC1-4-烷基，CON（C 1-4烷基）2，C 1-4 - 酰基，C 1-4 - 烷氧基，C 1-4 - 烷硫基，-SOC 1-6 - 烷基，-SO 2 C 1-6 - 烷基，C 1-4 - 烷氧基羰基，C 1-4 - 烷酰氧基，氨基，任选取代的一或二-C 1-6 - 烷基氨基，酰基氨基，-NC 1-4 - 烷基C 1 -C 1-4烷基 - SO 3 H，-SO 2 NH-C 1-6 - 烷基，四唑基，全卤代甲基，全卤代甲氧基; 其中R1，R2和R3全部被一个或多个取代基取代; 或其盐与药学上可接受的酸或碱，或任何旋光异构体; 含有它们的药物组合物，以及这些化合物用于制备用于治疗内分泌系统疾病，优选高血糖或糖尿病的药物的用途。