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    Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors
    5.
    发明授权
    Substituted amino bicyclic-&bgr;-lactam penam and cepham derivatives as cysteine protease inhibitors 失效
    取代的氨基双环β-内酰胺penam和cepham衍生物作为半胱氨酸蛋白酶抑制剂

    公开(公告)号：US06232305B1

    公开(公告)日：2001-05-15

    申请号：US09010993

    申请日：1998-01-22

    申请人： Rajeshwar Singh ,  Nian Zhou ,  Deqi Guo ,  Ronald G. Micetich

    发明人： Rajeshwar Singh ,  Nian Zhou ,  Deqi Guo ,  Ronald G. Micetich

    IPC分类号： C07D49940

    CPC分类号： C07D499/00 ,  C07D501/00

    摘要： The present invention provides substituted amino bicyclic-&bgr;-lactam penam derivatives and substituted amino bicyclic-&bgr;-lactam cepham derivatives and their diastereoisomers of formula I, as well as compositions, methods of making, and methods of using, which exhibit excellent cysteine protease inhibitory activity and which may be used for treatment of different diseases such as cancer (including cancer metastasis), osteoporosis, rheumatoid arthritis. muscular dystrophy, myocardial infarction, pulmonary emphysema, septic shock, cerebral ischemia, decreased memory function, Alzheimer, cataract, malaria, glomerular basement membrane degradation, bacterial infection, inflammatory diseases, parasitic infections and viral infections, wherein R is a peptidyl residue of a single natural &agr;-amino acid selected from a specific group of natural &agr;-amino acids or a peptidyl residue of a single non-natural amino acid selected from a specified group of non-natural amino acids, in which natural or non-natural peptidyl residue the terminal —NH2 group is unsubstituted or substituted once or twice with group R4, wherein R4 is selected from the group consisting of —COOR5, —COR5, —SO2R5, and —COR6, R6 is an amino group which is unsubstituted or substituted at least once with a C1-C6 alkyl group which is unsubstituted or substituted, R1 is selected from the group consisting of hydrogen, hydroxy, carboxy, —COOR6, —OR7, —CONHR7, and C1-C5 alkyl, in which the C1-C6 alkyl is unsubstituted or substituted, R2 and R3 are independently hydrogen or C1-C3 alkyl which is unsubstituted or substituted, n is 0, 1, or 2, and n1 is 0 or 1.

    摘要翻译： 本发明提供了取代的氨基双环β-内酰胺penam衍生物和取代的氨基双环-β-内酰胺头孢烯衍生物及其非对映异构体I，以及组合物，制备方法和使用方法，其表现出优异的半胱氨酸蛋白酶抑制 活性，其可用于治疗诸如癌症（包括癌症转移），骨质疏松症，类风湿性关节炎等不同疾病。 肌肉营养不良，心肌梗死，肺气肿，败血性休克，脑缺血，记忆功能下降，阿尔茨海默病，白内障，疟疾，肾小球基底膜降解，细菌感染，炎症性疾病，寄生虫感染和病毒感染，其中R是单一肽的肽基残基 选自特定天然α-氨基酸组的天然α-氨基酸或选自特定非天然氨基酸组的单一非天然氨基酸的肽基残基，其中天然或非天然肽基残基 末端-NH 2基团是未取代的或被基团R4取代一次或两次，其中R 4选自-COOR 5，-COR 5，-SO 2 R 5和-COR 6，R 6是未被取代或取代至少一次的氨基 与未取代或取代的C1-C6烷基，R1选自氢，羟基，羧基，-COOR6，-OR7，-CONHR7和C1-C5烷基，其中 C 1 -C 6烷基是未取代或取代的，R 2和R 3独立地是氢或未被取代或取代的C 1 -C 3烷基，n是0,1或2，且n 1是0或1。